Abstract

2A, and is used for preparing a drug for treating schizophrenia.

IPC Classes  ?

• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 213/87 - HydrazidesThio or imino analogues thereof in position 3
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

Disclosed are a benzonitric heterocyclic compound, a preparation method therefor and the use thereof. Provided in the present invention is a benzonitric heterocyclic compound represented by formula I, or a pharmaceutically acceptable salt thereof, which can be used as a histone deacetylase inhibitor, has a selective inhibitory effect on HDAC6, and has characteristics such as a high efficiency, low toxicity and ideal pharmacokinetic properties. Disclosed are a benzonitric heterocyclic compound, a preparation method therefor and the use thereof. Provided in the present invention is a benzonitric heterocyclic compound represented by formula I, or a pharmaceutically acceptable salt thereof, which can be used as a histone deacetylase inhibitor, has a selective inhibitory effect on HDAC6, and has characteristics such as a high efficiency, low toxicity and ideal pharmacokinetic properties.

IPC Classes  ?

• C07D 225/06 - Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with one six-membered ring
• C07D 267/14 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
• C07D 281/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring

Abstract

1-4 alkoxy. The compound has a low critical micelle concentration (CMC) and good dilution resistance and is capable of enclosing an insoluble drug to form a small-molecule micelle having a high drug loading capacity and good stability.

IPC Classes  ?

• C07C 309/18 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing carboxyl groups bound to the carbon skeleton containing amino groups bound to the same carbon skeleton
• A61K 9/107 - Emulsions
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• A61P 35/04 - Antineoplastic agents specific for metastasis

Abstract

Disclosed are an intermediate of pregabalin and a preparation method therefor. Provided are a compound as represented by formula (I) and a preparation method therefor. The preparation method for the compound as represented by formula (I) is any one of the following methods: method (1), comprising the following steps: reacting a compound as represented by formula (III) with nitromethane in an organic solvent in the presence of a base, and obtaining the compound as represented by formula (I) by means of chiral separation; and method (2), comprising the following steps: reacting the compound as represented by formula (III) with nitromethane in an organic solvent in the presence of a base under the action of a catalyst as represented by formula (II). The methods have moderate reaction conditions and low-toxicity, simple and readily available raw materials, are easy to operate, are easily used for production in a large scale, and can be used for synthesizing pregablin.

IPC Classes  ?

• C07D 263/26 - Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
• C07C 205/51 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being saturated

Abstract

Disclosed is a method for preparing a saccharin compound. Provided is a method for preparing a saccharin compound as shown in formula (1). The method is characterized by comprising the following step: carrying out, in water in the presence of tungstate and/or tungstic acid, an oxidation reaction on a compound as shown in formula (2) and hydrogen peroxide, to obtain a saccharin compound as shown in formula (1).

IPC Classes  ?

• C07D 275/06 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom

Abstract

232A2A, and is used for preparing a drug for treating schizophrenia.

IPC Classes  ?

• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

Disclosed are a benzonitric heterocyclic compound, a preparation method therefor and the use thereof. Provided in the present invention is a benzonitric heterocyclic compound represented by formula I, or a pharmaceutically acceptable salt thereof, which can be used as a histone deacetylase inhibitor, has a selective inhibitory effect on HDAC6, and has characteristics such as a high efficiency, low toxicity and ideal pharmacokinetic properties.

IPC Classes  ?

• C07D 223/16 - BenzazepinesHydrogenated benzazepines
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 267/14 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
• C07D 281/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
• C07D 243/12 - 1,5-BenzodiazepinesHydrogenated 1,5-benzodiazepines
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61P 37/02 - Immunomodulators
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
• A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep

Abstract

Provided is a biological peptide for treating lung diseases and an application thereof. Also provided is a preparation method and an application of the polypeptide, as well as a pharmaceutical composition containing the polypeptide. The polypeptide of the present invention has many advantages, such as small molecular weight, low production cost, excellent water solubility, excellent stability, long half-life, low immunogenicity, low toxic side effects, and strong tissue penetration. Moreover, the polypeptide of the present invention has significant functions of preventing, treating, and/or alleviating lung diseases such as asthma and chronic obstructive pulmonary disease.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61P 11/06 - Antiasthmatics

Abstract

A phenyl-containing compound, an intermediate thereof, a preparation method therefor and an application thereof. Provided is a compound represented by formula I or a pharmaceutically acceptable salt thereof, where R 1, R 2, R 3, R 4and R 516166 alkoxy or C(=O)OR 8; where R 8144 alkyl; R 6is (II), (III) or (IV); and R 723321-41-4 alkoxy. The compound has a low critical micelle concentration (CMC) and good dilution resistance and is capable of enclosing an insoluble drug to form a small-molecule micelle having a high drug loading capacity and good stability. (I)

IPC Classes  ?

• C07C 309/18 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing carboxyl groups bound to the carbon skeleton containing amino groups bound to the same carbon skeleton
• C07C 303/22 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof from sulfonic acids by reactions not involving the formation of sulfo or halosulfonyl groups
• C07C 69/96 - Esters of carbonic or haloformic acids
• C07C 68/00 - Preparation of esters of carbonic or haloformic acids
• A61K 9/107 - Emulsions
• A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• A61P 35/00 - Antineoplastic agents
• A61P 35/04 - Antineoplastic agents specific for metastasis

Abstract

Disclosed is the use of chlorophyll dihydroporphin as a plant growth regulator. Compared with the prior art, a class of new type plant growth regulators are provided; since the direct decomposition product of chlorophyll is used as a product, the preparation and processing thereof are easier, the structure is relatively simple, and tedious reactions and preparations such as further chemical coordination/chelation/purification are eliminated, so that the product is more environmentally friendly and safer; the product has a better solubility than the corresponding metal chelate and has a more convenient method of use, making it more convenient to be used in the fields; the stability of the product has been improved, with stable quality assurance and a longer shelf life; the product has a natural source and uses a low amount of same due to a low effective dosage, thereby improving the utilization rate of silkworm excrement resources.

IPC Classes  ?

• A01P 21/00 - Plant growth regulators
• A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system

Abstract

The present disclosure relates to the field of medicine, and specifically relates to an amphotericin B peptide derivative and a preparation method therefor. The amphotericin B peptide derivative has a broad-spectrum and highly effective bactericidal effect on drug-resistant bacteria and fungi.

IPC Classes  ?

• C07H 17/08 - Hetero rings containing eight or more ring members, e.g. erythromycins
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61K 38/04 - Peptides having up to 20 amino acids in a fully defined sequenceDerivatives thereof
• A61P 31/10 - Antimycotics

Abstract

An application of ginsenoside CK in preparation of an oral medication for treating moderate-severe psoriasis vulgaris.

IPC Classes  ?

• A61K 31/7032 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a polyol, i.e. compounds having two or more free or esterified hydroxy groups, including the hydroxy group involved in the glycosidic linkage, e.g. monoglucosyl-diacylglycerides, lactobionic acid, gangliosides
• A61P 17/06 - Antipsoriatics

Abstract

The present invention relates to a hydrate (a compound shown in formula 2) of 4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylic acid ethyl ester, and a preparation method therefor and use thereof. The compound can be obtained from crystallization in an organic solvent in mutual solubility with water such as a mixed solvent of acetone and water. The hydrate of 4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylic acid ethyl ester obtained in the present invention is high in purity and yield, thereby facilitating the subsequent synthesis of olmesartan medoxomil.

IPC Classes  ?

• C07D 233/90 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

The present invention relates to a novel rhodamine dye and an application thereof against pathogenic bacteria. In particular, the present invention relates to a compound represented by the following formula A. In the formula, X-19 9 are as described in the specification. The novel rhodamine dye of the present invention has bacteriostatic and bactericidal effect on gram-positive and gram-negative bacteria and antibacterial synergistic effect.

IPC Classes  ?

• C07D 311/82 - Xanthenes
• C07D 493/08 - Bridged systems
• A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
• A61P 31/04 - Antibacterial agents

Abstract

The present invention discloses a salt derivative of 1-(3-methanesulfonamidobenzyl)-6-methoxy-7-benzyloxy-1,2,3,4-tetrahydroisoquinoline. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL.

IPC Classes  ?

• C07D 217/18 - Aralkyl radicals
• A61P 9/06 - Antiarrhythmics
• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine

Abstract

The present invention belongs to the field of medicines, and relates to a polymyxin analogue having high antibacterial activity, and a preparation method therefor and an application thereof. The polymyxin analogue has a broad-spectrum and high-efficiency bactericidal effect on drug-resistant bacteria and fungi.

IPC Classes  ?

• C07K 7/62 - PolymyxinsRelated peptides
• A61K 38/12 - Cyclic peptides
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Abstract

A microbial agent containing selenium-rich bifidobacteria, which is used for prevention and/or treatment of intestinal mucosal injury caused by chemotherapy, adjuvant treatment of tumors, mitigation of side effects of tumor chemotherapy, prevention or treatment of alcoholic liver diseases, enhancement of immunity, regulation of intestinal floras, and serves as a protective agent for intestinal epithelial cells.

IPC Classes  ?

• C12N 1/20 - BacteriaCulture media therefor
• C12R 1/01 - Bacteria or actinomycetales
• A61P 35/00 - Antineoplastic agents

Abstract

Intermediate compounds for the preparation of Praziquantel are provided. In particular, the intermediate compounds provided include a compound of formula (IV) and a compound of formula (V). Also provided are processes for preparing the intermediate compounds. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound Praziquantel is high, so that industrialized mass production of Praziquantel using the intermediate compounds is easy to achieve.

IPC Classes  ?

• C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
• C07D 471/04 - Ortho-condensed systems
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• C07C 231/14 - Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups

Abstract

A process for the preparation of a novel androgen receptor antagonist is provided, comprising essentially conducting cyclization reaction of a compound of formula V to obtain a compound of formula VI. This method has the advantages of easily obtainable starting material, high atomic utilization rate, mild reaction conditions, and simply post-treatment. In addition, ODM-201 and its single isomers can be synthesized directionally by controlling the stereochemistry of starting material, with the advantages of simple and controllable process and suitability for industrial production.

IPC Classes  ?

• C07D 231/14 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond

Abstract

Provided are a high-titer polymyxin E2 sodium methanesulfonate, preparation method and use thereof in preparing a medicament for treating gram-negative bacterial infection.

IPC Classes  ?

• C07K 7/62 - PolymyxinsRelated peptides
• C07K 1/34 - ExtractionSeparationPurification by filtration, ultrafiltration or reverse osmosis
• C07K 1/36 - ExtractionSeparationPurification by a combination of two or more processes of different types
• C07K 1/16 - ExtractionSeparationPurification by chromatography
• A61K 38/12 - Cyclic peptides
• A61P 31/04 - Antibacterial agents

Abstract

Provided is a method for biologically preparing (1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine D-mandelate (I), comprising: (a) performing an asymmetric reduction reaction with a compound of formula (VI) as a substrate in the presence of a coenzyme under the catalysis of a carbonyl reductase in a liquid reaction system, so as to form a compound of formula (V); (b) reacting the compound of formula (V) with triethyl phosphonoacetate to obtain a compound of formula (IV); and (c) subjecting the compound of formula (IV) to ammonolysis and Hofmann degradation, and then salt formation with D-mandelic acid to obtain a compound of formula (I). The reaction system comprises: (i) an aqueous solvent; (ii) a substrate, which is a compound of formula (VI); (iii) a coenzyme; (iv) a carbonyl reductase; (v) a cosubstrate; and (vi) an enzyme for the regeneration of the coenzyme.

IPC Classes  ?

• C12P 7/22 - Preparation of oxygen-containing organic compounds containing a hydroxy group aromatic
• C07C 33/46 - Halogenated unsaturated alcohols containing only six-membered aromatic rings as cyclic part
• C07C 29/143 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen-containing functional group of C=O containing groups, e.g. —COOH of ketones
• C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
• C07C 59/50 - Mandelic acid
• C07C 209/58 - Preparation of compounds containing amino groups bound to a carbon skeleton by rearrangement reactions from or via amides
• C07C 209/68 - Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
• C07C 209/62 - Preparation of compounds containing amino groups bound to a carbon skeleton by cleaving carbon-to-nitrogen, sulfur-to-nitrogen, or phosphorus-to-nitrogen bonds, e.g. hydrolysis of amides, N-dealkylation of amines or quaternary ammonium compounds
• C07C 211/40 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing only non-condensed rings
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• C07C 233/58 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals

Abstract

The present invention discloses a salt derivative of 1-(3-methanesulfonamidobenzyl)-6-methoxy-7-benzyloxy-1,2,3,4-tetrahydroisoquinoline shown in formula I. The salt derivative has a solubility in water of not less than 3.0 nmol/mL or 1.8 mg/mL.

IPC Classes  ?

• C07D 217/18 - Aralkyl radicals
• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
• A61P 9/06 - Antiarrhythmics

Abstract

Disclosed is a preparation method for praziquantel and intermediates thereof. The method includes: obtaining a target product praziquantel by using β-phenethylamine as an initial raw material through a condensation reaction with chloroacetyl chloride, a substitution reaction with ethanolamine, and an acylation reaction with cyclohexanecarbonyl chloride, followed by an oxidation reaction and cyclization reaction. Also disclosed are two key intermediates, namely, a compound of formula IV and a compound of formula V for preparing praziquantel. The preparation method is reasonable and simple in its technological design, uses moderate reaction conditions, and is economical and environmentally friendly. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound praziquantel is high, so that industrialized mass production is easy to achieve.

IPC Classes  ?

• C07D 471/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups
• C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
• C07D 471/04 - Ortho-condensed systems
• C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• C07C 231/14 - Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines

Abstract

Provided in the present invention is a new method for preparing a trabectedin, using safracin B as the starting material and through a series of reactions synthesizing trabectedin. The method easily obtains raw materials, has fewer synthesis steps, does not use highly toxic organotin reagents, is safe and low-cost, and has high value in industrial applications.

IPC Classes  ?

• C07D 471/18 - Bridged systems
• C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
• C07D 497/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

Abstract

Provided is a process for preparing a dapagliflozin eutectic, comprising: 1) using a 4-chloro-3-(4-ethoxybenzyl)phenyl halide 6 as a raw material, reacting 6 with lithium alkylide and a zinc salt via an X/Li/Zn exchange reaction in an appropriate solvent to prepare an organozinc reagent - bis[4-chloro-3-(4-ethoxybenzyl)phenyl]zinc, and then reacting same with 2,3,4,6-tetra-O-pivaloyl-α-D-bromoglucopyranose 4 by a nucleophilic substitution reaction to prepare a compound 3; and 2) removing the pivaloyl protecting group of the compound 3 to obtain dapagliflozin 2, and directly reacting same with (S)-1,2-propanediol and water in an appropriate solvent to prepare a dapagliflozin eutectic 1. The synthetic route is as follows: formula (I). In the formula, X in the 4-chloro-3-(4-ethoxybenzyl)phenyl halide 6 is selected from Br or I. The reagents used are all conventional bulk reagents, cheap and easily accessible, the route is simplified, the route cost is greatly reduced, the product yield and purity are relatively high, and the products do not contain diastereoisomers, and are suitable for industrial production.

IPC Classes  ?

• C07D 309/10 - Oxygen atoms
• A61K 31/70 - CarbohydratesSugarsDerivatives thereof
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The present invention discloses a method and an intermediate for the preparation of an epirubicin hydrochloride. The method comprises the following step: in an organic solvent and under an action of an alkali, subjecting compound 4 and a trifluoromethanesulfonic anhydride to an esterification shown below to obtain compound 4'. The preparation method of the present invention has the advantages of short reaction routes, high yield, ready availability of reaction raw materials, no need to use other expensive reagents, low costs, mild reaction conditions, and simple operations, facilitating industrial production.

IPC Classes  ?

• C07H 15/252 - Naphthacene radicals, e.g. daunomycins, adriamycins
• C07H 1/06 - SeparationPurification

Abstract

3 alkyl alcohol solution of methylamine in an organic solvent, wherein, X=chlorine, bromine, or iodine. Also disclosed are an intermediate compound 3 and a preparation method thereof. The method for preparing a dabigatran etexilate intermediate of the present invention has the advantages of simple process, easy operation, high yield, and easy purification, thus being suitable for industrial production.

IPC Classes  ?

• C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates

Abstract

Provided are a separation and purification method for epirubicin or hydrochloride thereof. The method comprises: 1) taking epirubicin or a hydrochloride crude product thereof, and sampling macroporous absorption resin; and 2) carrying out elution by using an organic solvent water solution at a volume percent of 5% to 50%, collecting and combining an eluent, and carrying out separation to obtain epirubicin. The method is economical and efficient, and has very good selectivity and a very good separation effect on purities of epirubicin or hydrochloride thereof, epirubicin hydrochloride of a pharmaceutical-grade purity can be obtained by performing separation and purification for one time, and the yield is high.

IPC Classes  ?

• C07H 15/252 - Naphthacene radicals, e.g. daunomycins, adriamycins
• C07H 1/06 - SeparationPurification

Abstract

Disclosed is a method for separating a diastereoisomer A of Bedaquiline. The method comprises the following steps: (1) adding a reversed-phase solvent into a Bedaquiline reaction liquid comprising diastereoisomers A and B, so as to precipitate out the diastereoisomer B; and (2) removing the diastereoisomer B precipitated out in step (1), so as to obtain the diastereoisomer A. The separation method of the present invention is easy to operate and is stable, and has higher industrialization value compared with separation and purification in a conventional column chromatography method, and can resolve the problems of difficulty in purifying and separating Bedaquiline due to the small amount of a product caused by an excessively low conversion rate because preparation condition of Bedaquiline is harsh and the conversion rate is difficult to ensure; raw material residuals can be easily removed, the yield is high, and the purity of the diastereoisomer A is high, which facilitates the split; split can be further carried out to obtain a qualified Bedaquiline product with a purity greater than or equal to 99.0%, wherein the impurities of the diastereoisomers are lower than or equal to 0.1%.

IPC Classes  ?

• C07D 215/227 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
• C07F 1/02 - Lithium compounds

Abstract

Provided in the present invention is an ipragliflozin synthesis method. The method comprises: (1) 4-fluoro-3-(2-benzothiophene)methylphenyl halide 5 is used as raw material, and 5 is reacted with alkyl lithium in a proper solvent, and then reacted with zinc salt to prepare an organic zinc reagent di[4-fluoro-3-(2-benzothiophene)methylphenyl]zinc, then is subjected to a nucleophilic substitution reaction with 2,3,4,6-tetra-O-pivaloyl-α-D-glucopyranose bromide 4 to prepare an ipragliflozin intermediate 3; (2) a pivaloyl protecting group of the compound 3 is removed by an organic base to prepare the ipragliflozin 2; wherein, X in the structure of 4-fluoro-3-(2-benzothiophene)methylphenyl halide 5 is selected from bromine or iodine; synthetic route (I) is used. The method in the present invention avoids the steps of methylation of hydroxyl groups on an anomeric carbon of a sugar ring, acetylation of hydroxyl groups on the sugar ring, reduction of methoxyl groups on the anomeric carbon and the ultra-low reaction temperature, and thus the synthesis process is greatly simplified, the synthesis cost is significantly reduced, the product yield and the purity of the compound are improved and the present invention is suitable for industrial production.

IPC Classes  ?

• C07D 409/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

Abstract

Disclosed are a preparation method for praziquantel and intermediates thereof. The method comprises: a target product praziquantel is obtained by using β-phenylethylamine as an initial raw material through the condensation reaction with chloroacetyl chloride, the substitution reaction with ethanolamine, and the acylation reaction with cyclohexanecarbonyl chloride, and then followed by the oxidation reaction and the cyclization reaction. Also disclosed are two key intermediates, namely, a formula IV compound and a formula V compound for preparing the praziquantel. The preparation method is reasonable and simple in technological design, moderate in reaction conditions, economical and environment-friendly; raw materials are inexpensive and easy to get, the key intermediates are easy to prepare, the total reaction yield is high (≥ 60％), and the purity of the obtained target product formula I compound praziquantel is high (the HPLC determined purity ≥ 99.8％), so that the industrialized mass production is easy to realize.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61P 33/00 - Antiparasitic agents
• A61P 33/12 - Schistosomicides

Abstract

The present invention provides a method for preparing an intermediate compound of sitagliptin represented by formula I. The preparation method comprises: dissolving a compound represented by formula II into an organic solvent; and under the catalysis of fatty acid and effect of chlorosilane, performing a reduction reaction of carbon-carbon double bonds, so as to obtain the intermediate compound of sitagliptin represented by formula I, R being methyl or formoxyl. The preparation method of the present invention avoids precious metal as a catalyst, and accordingly, the cost is low, the post-treatment is simple, the product has a high yield, chemical purity and optical purity, and de % is greater than 99.6%, and the preparation method can be used in synthesis of sitagliptin and is suitable for industrial production.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems

Abstract

Disclosed are a platinum (II) compound, a preparation method therefor, and a pharmaceutical composition and an application thereof. The preparation method comprises the following steps: enabling dihydrate diammine platinum nitrate (4) to react with the carboxylate ligand derivative (5) in water, to produce a platinum (II) compound. Also provided are an application of the platinum (II) compound in preparation of an antitumor drug, and a pharmaceutical composition. The pharmaceutical composition contains an active component and a medicinal carrier, the active component containing the platinum (II) compound, and the mass percentage of the active component being 0.1%-95%. The platinum (II) compound of the present invention is well water-soluble, low toxic, easily prepared, and efficient in antitumor activity.

IPC Classes  ?

• C07F 15/00 - Compounds containing elements of Groups 8, 9, 10 or 18 of the Periodic Table
• A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/282 - Platinum compounds
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present invention relates to new forms of co-crystals of agomelatine and p-toluenesulphonic acid, to a process for their preparation and to pharmaceutical compositions containing them. The co-crystals according to the invention have better solubility than agomelatine and are therefore more suitable for the preparation of pharmaceutical compositions. They also have better stability and purity and, moreover, are obtained by a simple process which does not include any difficult steps.

IPC Classes  ?

• C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
• C07C 309/30 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
• C07C 303/32 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
• C07C 231/22 - SeparationPurificationStabilisationUse of additives

Abstract

Complexes of agomelatine and sulphonic acids of formula (I): Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.

IPC Classes  ?

• C07C 309/35 - Naphthalene sulfonic acids
• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
• C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
• C07C 303/22 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof from sulfonic acids by reactions not involving the formation of sulfo or halosulfonyl groups
• C07C 309/29 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings

Abstract

The present invention provides a key new intermediate (a compound of formula III) of 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound), a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity.

IPC Classes  ?

• C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• C07C 237/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• C07D 241/08 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
• C07D 471/04 - Ortho-condensed systems
• C07C 231/10 - Preparation of carboxylic acid amides from compounds not provided for in groups

Abstract

Disclosed are a method of preparing a dabigatran etexilate intermediate and an intermediate compound. The method of preparing a dabigatran etexilate intermediate 4 comprises the following steps: reacting a compound 3 with a C1-C3 alkyl alcohol solution of methylamine in an organic solvent, X = chlorine, bromine or iodine. Also disclosed are an intermediate compound 3 and preparation method thereof. The method of preparing a dabigatran etexilate intermediate is simple, easy to operate with high yield, is easy to purify, and suitable for industrial production.

IPC Classes  ?

• C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates

Abstract

5 is the same as that of the specification. The glycopeptide compound of the present invention has in-vitro antibacterial activity and has important significance for development of new antibacterial agents.

IPC Classes  ?

• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof
• C07K 11/00 - Depsipeptides having up to 20 amino acids in a fully defined sequenceDerivatives thereof
• C07K 14/00 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
• C07K 11/02 - Depsipeptides having up to 20 amino acids in a fully defined sequenceDerivatives thereof cyclic, e.g. valinomycins
• A61K 38/00 - Medicinal preparations containing peptides

Abstract

Disclosed in the present invention is a podophyllotoxin derivative, and a preparation method, pharmaceutical composition and use thereof. The preparation method disclosed in the present invention comprises the following step: in an organic solvent, in the presence of a base, carrying out a condensation reaction between the compound as shown in formula II and the compound as shown in formula III under the action of a condensating agent. The pharmaceutical composition disclosed in the present invention comprises the podophyllotoxin derivative as shown in formula I and a pharmaceutically acceptable excipient. Also disclosed in the present invention is the use of the podophyllotoxin derivative as shown in formula I in the preparation of a drug for treating a cancer. The podophyllotoxin derivative of the present invention has a good tumour cell inhibitory activity, and the preparation method and post-treatment thereof are simple, with good prospects for market development.

IPC Classes  ?

• C07D 493/04 - Ortho-condensed systems
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/365 - Lactones
• A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Disclosed in the invention are a mirabegron-related substance as shown in formula (I) or a salt thereof, and a preparation method and a use thereof. The method for preparing the mirabegron-related substance or the salt thereof disclosed by the invention comprises the following step: in a solvent, carrying out a condensation reaction as shown below between a compound as shown in formula (6) and a compound as shown in formula (7) or an active ester thereof under the action of a condensing agent to obtain the mirabegron-related substance as shown in formula (I); alternatively, in the solvent, carrying out the condensation reaction between the salt of the compound as shown in the formula (6) and the compound as shown in the formula (7) or the active ester thereof under the action of the condensing agent to obtain the salt of the mirabegron-related substance as shown in formula (I). The mirabegron-related substance of the invention is capable of effectively identifying impurities generated in the synthesis of the mirabegron so as to control the medicinal quality of the mirabegron.

IPC Classes  ?

• C07D 277/40 - Unsubstituted amino or imino radicals
• C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
• C07C 57/15 - Fumaric acid
• C07C 59/255 - Tartaric acid
• C07C 55/10 - Succinic acid

Abstract

Disclosed in the present invention is a podophyliotoxin derivative as shown by formula I, and a preparation method, pharmaceutical composition and use thereof. In the podophyliotoxin derivative as shown by formula I of the present invention, X is oxygen or nitrogen; R1 is mono-substituted or polysubstituted, and the substitutional position is arbitrary, being one or more of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and hydroxyl; and R2 is hydrogen or C1-C4 alkyl. The podophyliotoxin derivative of the present invention has a good tumour cell inhibitory activity, and the anti-tumour activities of some compounds are obviously better than etoposide, and a part of the compounds have a good inhibitory activity against human lung cancer cells, especially non-small-cell lung cancer cell line A549, which provides new research directions for developing a broad spectrum, high-efficiency and low toxicity podophyliotoxin derivative, and the method for preparing the podophyliotoxin derivative of the present invention is simple, and has good prospects for market development.

IPC Classes  ?

• C07D 493/04 - Ortho-condensed systems
• A61P 35/00 - Antineoplastic agents
• A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin

Abstract

During the long-term commercial process for producing dextromethorphan hydrobromide, large amounts of endo-(14S)-3-methoxy-17-methylmorphinan are required for use in the aspects of quality control, however, endo-(14S)-3-methoxy-17-methylmorphinan is unstable, inconvenience for storage, and also goes against the execution of the testing procedure, and hence it is imperative to solve the practical problem generated in this production process in the art. In view of this, disclosed in the present invention is endo-(14S)-3-methoxy-17-methylmorphinan picrate in the form of a solid and a preparation method and use thereof, i.e. being used for detecting endo-(14S)-3-methoxy-17-methylmorphinan in the process for synthesizing dextromethorphan.

IPC Classes  ?

• C07D 221/28 - Morphinans

Abstract

Disclosed in the present invention is a 3-cyanoanilinoalkylarylpiperazine derivatives and use thereof in preparing drugs; the 3-cyanoanilinoalkylarylpiperazine derivatives disclosed by the present invention has very useful pharmaceutical properties and good tolerance, especially the use as novel analgesic drugs, novel antidepressants, and novel analgesic and antidepressive drugs. This class of compounds are central analgesics regulating 5-hydroxytrptamine, and also are novel antidepressants regulating 5-hydroxytrptamine. This class of compounds also has less toxic and side effects and a higher safety range. The 3-cyanoanilinoalkylarylpiperazine derivative is a compound shown as formula (III) or free base or salt thereof:

IPC Classes  ?

• C07D 295/13 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
• C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• C07D 239/34 - One oxygen atom
• C07D 295/125 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings

Abstract

The present invention provides a method for preparing an intermediate compound of sitagliptin represented by formula I. The preparation method comprises: dissolving a compound represented by formula II into an organic solvent; and under the catalysis of fatty acid and effect of chlorosilane, performing a reduction reaction of carbon-carbon double bonds, so as to obtain the intermediate compound of sitagliptin represented by formula I, R being methyl or formoxyl. Te preparation method of the present invention avoids precious metal as a catalyst, and accordingly, the cost is low, the post-treatment is simple, the product has a high yield, chemical purity and optical purity, and de% is greater than 99.6%, and the preparation method can be used in synthesis of sitagliptin and is suitable for industrial production.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems

Abstract

A method for preparing a Rivaroxaban intermediate I is presented, including the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20° C. to 60° C., where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.

IPC Classes  ?

• C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

The present invention concerns novel forms of co-crystals of agomelatine and p-toluenesulphonic acid, the method for preparing same and the pharmaceutical compositions containing same. The co-crystals according to the invention have better solubility than agomelatine and are therefore more suitable for developing pharmaceutical compositions. They have a higher level of stability and purity, and are moreover obtained by a simple method that comprises no difficult steps.

IPC Classes  ?

• C07C 303/32 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
• C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton

Abstract

Disclosed are agomelatine sulfonic acids complexes having the specific stoichiometry of 2 molar equivalents of agomelatine for 1 molar equivalent of sulfonic acids. Those complexes show excellent solubility, stability and purity, making them favourable for use in the manufacture of pharmaceutical formulations containing agomelatine.

IPC Classes  ?

• C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
• C07C 309/29 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
• C07C 309/35 - Naphthalene sulfonic acids
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61P 25/24 - Antidepressants

Abstract

The present invention relates to the p-toluenesulfonic acid co-crystals of agomelatine of formula (I), preparation and use thereof, and to pharmaceutical composition containing it. The p-toluenesulfonic acid co-crystals of agomelatine obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys good stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps.

IPC Classes  ?

• C07C 309/30 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
• C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61P 25/24 - Antidepressants
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics

Abstract

The present invention discloses a macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof. The present invention provides a method for preparing a macrolide compound 1, a macrolide compound 1', or a salt thereof; also provided are a macrolide compound 2, macrolide compound 2', or salt thereof, a pharmaceutical composition containing said compound or salt, and the application thereof in the preparation of a pharmaceutical for inhibiting methicillin-resistant Staphylococcus aureus. When one or more of the macrolide compound 2, the macrolide compound 2', the macrolide compound 2 salt, and the macrolide compound 2' salt of the present invention is used together with a β-lactam antibiotic, the inhibiting effect of the β-lactam antibiotic on methicillin-resistant Staphylococcus aureus is significantly increased. This is a new class of potentiator having a good potentiating effect in vitro, alleviating methicillin-resistant Staphylococcus aureus resistance to β-lactam antibiotics, and having good prospects for market development.

IPC Classes  ?

• C07H 17/08 - Hetero rings containing eight or more ring members, e.g. erythromycins
• A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61K 31/431 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems containing further heterocyclic ring systems, e.g. ticarcillin, azlocillin, oxacillin
• A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
• A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
• A61K 31/545 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
• A61P 31/04 - Antibacterial agents

Abstract

Novel complexes of agomelatine and sulphonic acids of formula (I). Drugs.

IPC Classes  ?

• C07C 303/32 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
• C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton

Abstract

Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production.

IPC Classes  ?

• C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 263/20 - Oxygen atoms attached in position 2

Abstract

The present invention provides a 4-Benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) key new intermediate formula III compound, a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-Benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity.

IPC Classes  ?

• C07C 237/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• C07D 241/08 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
• C07D 471/04 - Ortho-condensed systems

Abstract

Disclosed are a platinum(II) compound, a preparation method therefor, and a pharmaceutical composition and an application thereof. The preparation method comprises the following steps: enabling dihydrate diammineplatinum nitrate (4) to react with the carboxylate ligand derivative (5) in water, to produce a platinum(II) compound. Also provided are an application of the platinum(II) compound in preparation of an antitumor drug, and a pharmaceutical composition. The pharmaceutical composition contains an active component and a medicinal carrier, the active component containing the platinum(II) compound, and the mass percentage of the active component being 0.1%-95%. The platinum(II) compound of the present invention is well water-soluble, low toxic, easily prepared, and efficient in antitumor activity.

IPC Classes  ?

• C07F 15/00 - Compounds containing elements of Groups 8, 9, 10 or 18 of the Periodic Table
• A61K 31/282 - Platinum compounds
• A61P 35/00 - Antineoplastic agents

Abstract

An HE3235 solid preparation comprising HE3235, a water-soluble dispersion carrier, and a sucrose compound. The HE3235 solid preparation is free of surfactant, but still provides great dissolution and bioavailability, thus increases greatly the safeness and compliance of the solid preparation. The solid preparation is easy to prepare, is of readily available raw materials, and thus has a significant advantage in commercialized production.

IPC Classes  ?

• A61K 31/566 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol having an oxo group in position 17, e.g. oestrone
• A61K 9/14 - Particulate form, e.g. powders
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are benzoisothiazole compounds and a use in the preparation of anti-schizophrenia drugs. The benzoisothiazole compounds of the present invention not only have strong affinity for dopamine D3 receptor, 5-HT1A receptor and 5-HT2A receptor, but also can observably improve the symptoms of schizophrenia relevant to apomorphine model and MK-801 model mice, with oral absorption being good, safety being high and side-effect being less, and having developmental value as new anti-neurotic disease drugs. The present invention is the compounds having a structure of general formula (I), or geometric isomers, free alkalies, salts, hydrates or solvates thereof.

IPC Classes  ?

• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 275/04 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61P 25/24 - Antidepressants
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• A61P 25/22 - Anxiolytics
• A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/16 - Anti-Parkinson drugs

Abstract

Provided is a racemization method of a chiral 2-[(4,6-dimethylpyrimidine-2-yl)oxy]-3-methoxy-3,3-diphenyl propionic acid, comprising the following steps: adding a 2-[(4,6-dimethylpyrimidine-2-yl)oxy]-3-methoxy-3,3-diphenyl propionic acid with a high rotation value to a specific solvent; performing the racemization at a specific temperature under stirring for a period of time; and after post-processing, a racemization product with a lower rotation or zero rotation value is obtained.

IPC Classes  ?

• C07D 239/34 - One oxygen atom

Abstract

The present invention relates to the field of chemical synthesis, and discloses a preparation method of ambrisentan. In the preparation method, using (S)-phenethylamine as a resolving agent, to form two diastereomers with 2-[(4,6-dimethyl pyrimidine-2-yl)oxy]-3-methoxy-3,3-diphenyl propionic acid in a specific solvent; re-crystallising the same to obtain diastereomers with a lower solubility; followed by acid ionization to obtain ambrisentan. The method of the present invention has a yield of about 30%, uses a cheap resolving agent which is easy to obtain and recover, and is suitable for industrialized production.

IPC Classes  ?

• C07D 239/34 - One oxygen atom
• C07B 57/00 - Separation of optically-active organic compounds

Abstract

Disclosed in the invention are a fused ring compound containing pyrimidine or pyridine and the use thereof as an anti-tumour drug. teT fused ring compound is a compound as shown by formula (I) or a pharmaceutical acceptable salt thereof; the compound of the present invention, when used as an anti-tumour drug, has a stronger anti-tumour activity and less side effects, and is more easily used as an anti-tumour drug.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 471/04 - Ortho-condensed systems
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
• C07D 495/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 31/4355 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61P 35/00 - Antineoplastic agents
• A61P 5/00 - Drugs for disorders of the endocrine system
• A61P 37/02 - Immunomodulators
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

Provided are an ophthalmic preparation comprising 0.01 wt.% to 1.5 wt.% 17α-ethynyl-androst-5-ene-3β,7β,17β-triol and a preparation method thereof. The ophthalmic preparation is used for treating ophthalmic diseases.

IPC Classes  ?

• A61K 31/569 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone substituted in position 17 alpha, e.g. ethisterone
• A61K 9/08 - Solutions
• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient
• A61P 27/02 - Ophthalmic agents
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Abstract

An amorphous asiatic tromethamine salt and the preparation method thereof. The method includes the steps of: (1) dissolving asiatic acid in an organic solvent; step (2) mixing with tromethamine; step (3) stirring and salifying the same, and then removing the organic solvent. The method for preparing the amorphous asiatic tromethamine salt is easy and effective, and the water solubility and bioavailability of the asiatic tromethamine salt thus obtained are greatly compared with the prior art.

IPC Classes  ?

• C07C 227/14 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
• C07C 215/10 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
• C07C 229/38 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
• C07J 63/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms

Abstract

The present invention provides a glycopeptide compound or a pharmaceutical salt thereof, as shown in Formula (I) or (II), and a method for preparing same, and pharmaceutical compositions and applications thereof. The glycopeptide compound of the present invention has in-vitro antibacterial activity.

IPC Classes  ?

• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof

Abstract

Disclosed are a cyclohexane amine compound and an application thereof for anti-schizophrenia drugs. The cyclohexane amine compound of the present invention has high affinity for a dopamine D3 receptor and 5-ΗΤ1Α, and a lead compound has high height selectivity for the D3/D2 receptor. In vivo tests show that a lead compound such as I-1 can obviously mitigate relevant symptoms of apomorphine model and MK-801 model mice. The compound of the present invention has a desirable anti-schizophrenia effect, low acute toxicity, high safety, and a development value for highly-efficient low-toxicity model antipsychotic disease drugs. The cyclohexane amine compound is a compound having the general structural formula (I) or a geometrical isomer, free base, hydrate or salt thereof.

IPC Classes  ?

• C07D 275/04 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• A61P 25/24 - Antidepressants
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 25/22 - Anxiolytics
• A61P 25/16 - Anti-Parkinson drugs

Abstract

Emtricitabine sylicylate crystalline, preparing methods and uses thereof are disclosed. The chemical structure of emtricitabine sylicylate is shown in formula 2, wherein, when n=0, formula 2 represents anhydrous emtricitabine sylicylate, and when n=1, it represents emtricitabine sylicylate monohydrate.

IPC Classes  ?

• C07D 411/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond

Abstract

5, Q, X and n are defined as in the description. Also disclosed are a method for preparing the compounds of formula I, a composition containing the compounds, and the uses of the same in the preparation of medicaments for regulating blood lipid and/or preventing gallstone. The compounds of formula I disclosed in the present invention have stability in vitro, good solubility in the pharmaceutical organic solvents and favorable bioavailability in animals.

IPC Classes  ?

• C07C 235/84 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
• A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
• C07C 325/02 - ThioketonesOxides thereof
• C07C 235/20 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• C07C 235/26 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being saturated and containing rings
• C07C 251/24 - Compounds containing nitrogen atoms doubly- bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines

Abstract

An oral formulation, preparation method therefor and use thereof. The oral formulation comprises a pharmaceutically acceptable carrier and 17α-ethynyl-androst-5-ene-3β, 7β, 17β-triol as active ingredient; the formulation is not released or is substantially not released in an acidic medium.

IPC Classes  ?

• A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
• A61K 9/28 - DrageesCoated pills or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 47/30 - Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

Stabilised amorphous form of the compound of formula (I): Medicaments.

IPC Classes  ?

• A61K 47/30 - Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
• A61K 9/20 - Pills, lozenges or tablets
• C07C 231/00 - Preparation of carboxylic acid amides

Abstract

The present invention relates to the stabilised amorphous form of the compound of formula (I), to a process for its preparation and also to pharmaceutical compositions or medicaments containing it.

IPC Classes  ?

• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• A61K 47/38 - CelluloseDerivatives thereof
• A61K 47/30 - Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics
• A61P 25/24 - Antidepressants
• A61P 35/00 - Antineoplastic agents
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 3/04 - AnorexiantsAntiobesity agents

Abstract

Provided are a benazepine compound, a composition containing the compound and a use of the compound in the preparation of anti-tumor drugs. The benazepine compound is a compound shown in formula (I) or a pharmaceutically acceptable salt thereof, which has a stronger anti-tumor activity and selectivity, and a lower toxic side effect.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 513/04 - Ortho-condensed systems
• C07D 498/04 - Ortho-condensed systems
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
• A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are a benazepine compound and an application thereof. The benazepine compound, as a synthon for preparing a novel compound with an anti-tumor activity, results in a compound that has a significantly improved ex vivo enzyme-inhibiting activity, and shows a multi-target inhibitory effect, and thus has a notable scientific advancement and a value of in-depth research and development. The benazepine compound is a compound shown in formula (I) or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• C07D 487/14 - Ortho-condensed systems
• C07D 498/14 - Ortho-condensed systems
• C07D 513/14 - Ortho-condensed systems

Abstract

The present invention provides a new crystalline form VII of agomelatine, its method of preparation, application and pharmaceutical composition. This new crystalline form offers high purity, a stable crystalline structure and good reproducibility, while its method of production lends itself well to large scale production. In terms of stability and purity, it is superior to the numerous crystalline forms which have hitherto been reported. As a result, the crystalline form VII of the present invention possesses advantages in pharmaceutical preparation.

IPC Classes  ?

• C07C 231/24 - SeparationPurification
• C07C 233/22 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

Disclosed in the present invention are a Pyrimidobenzoazepine compound and the use thereof as an antitumour drug. The advantage of the present invention consists in that the compound and the pharmaceutical agent thereof have good effects on treating diseases caused by gene expression abnormity, such as tumours, endocrine disturbance, immune system diseases, genetic diseases and nervous system diseases. When used as an antitumour drug, it has a stronger antitumour activity and lower toxic side effects, and is more easily used as an antitumour drug. The compound containing pyrimidobenzoazepine is the compound of formula (I) and the pharmaceutically acceptable salts thereof.

IPC Classes  ?

• C07D 487/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains two hetero rings
• C07D 513/04 - Ortho-condensed systems
• A61K 31/5513 - 1,4-Benzodiazepines, e.g. diazepam
• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
• A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are a fused ring-structured benzamide compound and an application thereof. Pharmacological experiments show that the compound of the present invention provides great histone deacetylase 1 (HDAC1) inhibitory activity, weak inhibition against normal cells, reduced toxicity, should provide further reduced toxic side effects when applied as an antineoplastic medicament, and further facilitates use as the antineoplastic medicament. The present invention provides great efficacy in the treatment of diseases induced by abnormal gene expression, such as: tumors, endocrine disorders, immune system diseases, genetic diseases, and neurological diseases. The fused ring-structured benzamide compound is a compound as represented by formula (V) or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• C07D 235/06 - BenzimidazolesHydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
• C07D 235/08 - Radicals containing only hydrogen and carbon atoms
• C07D 235/18 - BenzimidazolesHydrogenated benzimidazoles with aryl radicals directly attached in position 2
• C07D 235/26 - Oxygen atoms
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are an intermediate IV for preparing ambrisentan, a preparing method of the intermediate, and a preparing method of ambrisentan. The intermediate compound is a compound of S-configuration, and can be directly synthesized into ambrisentan without being split, which overcomes the defects in the prior art, improves the atom utilization rate of synthesis, reduces the cost, and is applicable to industrial production. Also disclosed are other intermediates VI, VII, VIII for preparing ambrisentan, and two preparing methods of ambrisentan.

IPC Classes  ?

• C07D 239/34 - One oxygen atom
• C07D 239/32 - One oxygen, sulfur or nitrogen atom
• C07D 317/10 - Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
• C07D 317/22 - Radicals substituted by singly bound oxygen or sulfur atoms etherified
• C07C 43/04 - Saturated ethers
• C07C 41/02 - Preparation of ethers from oxiranes
• A61P 9/12 - Antihypertensives

Abstract

Provided is a 4-aminoquinazoline hydroxamic acid compound as represented by formula (V) or a pharmaceutically acceptable salt thereof. The compound provides great histone deacetylase inhibitory activity, great inhibitory activities against various tumor cells of the human body, weak inhibition against normal cells, and reduced toxicity, and is applicable for development as an antineoplastic medicament. In addition, the compound also provides great efficacy in the treatment of diseases induced by abnormal gene expression.

IPC Classes  ?

• C07D 239/94 - Nitrogen atoms
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed in the present invention is a fused ring quinazoline hydroximic acid compound. The compound is part of a class of dual inhibitors of protein tyrosine kinases and histone deacetylases, and the fused ring quinazoline hydroximic acid compound can be used in the preparation of drugs for treating neoplastic diseases in mammals. The dual inhibitors of protein tyrosine kinases and histone deacetylases are compounds of general structural formula (I) or salts thereof.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed in the present invention is a 3-cyanoanilinoalkylarylpiperazine derivative and use thereof in preparing drugs; the 3-cyanoanilinoalkylarylpiperazine derivative disclosed by the present invention has very useful pharmaceutical properties and good tolerance, especially the use as novel analgesics, novel antidepressants, and novel analgesic and antidepressive drugs. This class of compounds are central analgesics regulating 5-hydroxytryptamine, and also are novel antidepressants regulating 5-hydroxytryptamine. This class of compounds also has less toxic and side effects and a higher safety range. The 3-cyanoanilinoalkylarylpiperazine derivative is a compound shown as formula （III） or free base or salt thereof.

IPC Classes  ?

• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• C07D 401/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group
• C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

Abstract

The present invention relates to a separation and purification method for an organic compound in the chemical field. Specifically, the present invention relates to a separation and purification method for dalfopristin and an intermediate thereof. The method of the present invention is economical and highly-efficient, and achieves ideal selectivity and purification effects on isomer impurities in the crude product of dalfopristin or dalfopristin intermediate. The dalfopristin or dalfopristin intermediate product having purity higher than 99% can be obtained by performing separation and purification for once, and the yield is high.

IPC Classes  ?

• C07K 5/078 - Dipeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• C07K 5/12 - Cyclic peptides
• B01D 15/08 - Selective adsorption, e.g. chromatography
• A61P 31/04 - Antibacterial agents

Abstract

A molecule with neuro activities, especially 4-substituent-2-hydroxylmorpholine-3-one, as a new intermediate of neurokinin-1 receptor antagonist Aprepitant, and preparation method thereof.

IPC Classes  ?

• C07D 265/32 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
• C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

Disclosed is a method for preparing a Rivaroxaban intermediate I, comprising the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone(Ⅱ) and (s)-epoxy compound(Ⅲ), the reation temperature ranging from 20℃ to 160℃, where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.

IPC Classes  ?

• C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-((3-(3-Fluoro-4-Morpholine phenyl)-2-oxy-5-oxazoline)) (I), wherein the intermediate (I) is obtained by the cyclisation of a 3-Fluoro-4-morpholine phenyl isocyanate (II) and epoxy compound (III). This process has a short route, low cost, easy operation, and high yield, so is suitable for large-scale industrial production.

IPC Classes  ?

• C07D 263/20 - Oxygen atoms attached in position 2
• C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
• C07D 303/36 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
• C07D 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
• C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 295/155 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• C07D 413/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms

Abstract

Disclosed are a crystal of dapoxetine hydrochloride and an amorphous dapoxetine hydrochloride. Also disclosed is a preparation method for both. The stability of the crystal of the present invention is greater than that of the polymorph of the prior art; the aqueous solubility of the amorphous substance is significantly greater than that of existing dapoxetine hydrochloride.

IPC Classes  ?

• C07C 217/48 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings
• C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups

Abstract

Disclosed are acid salts of dapoxetine hydrochloride and preparation methods therefor. Specifically, disclosed are a dapoxetine succinate crystal and a preparation method therefor, an amorphous dapoxetine succinate crystal and a preparation method therefor, a dapoxetine phosphate crystal and a preparation method therefor, a dapoxetine fumarate crystal and a preparation method therefor, a dapoxetine benzoate crystal and a preparation therefor, and a dapoxetine salicylate crystal and a preparation method therefor. The acid salts of the present invention have increased aqueous solubility, significantly greater than that of dapoxetine free base, and have improved stability and hygroscopicity.

IPC Classes  ?

• C07C 217/48 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings
• C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups

Abstract

Disclosed are crystals of acid salts and the acid salts of dapoxetine and preparation methods therefor. The crystals are crystals of methanesulfonate, nitrate, and hydrobromide of dapoxetine, and crystals of gentisate, orotate, cyclamate, acetyl salicylate, hippurate, or 1,5-naphthalene sulfonate. The acid salts of dapoxetine are gentisate, orotate, acetyl salicylate, hippurate, or 1,5-naphthalene sulfonate of dapoxetine. The aqueous solubility of the several salts and crystals of dapoxetine of the present invention are all significantly greater than the solubility of dapoxitine free base, and have improved stability and hygroscopicity.

IPC Classes  ?

• C07C 217/48 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings
• C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups

Abstract

Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof; the inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, hereditary diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula or salt thereof (I).

IPC Classes  ?

• C07D 209/04 - IndolesHydrogenated indoles
• C07D 213/02 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
• C07D 235/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
• C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
• C07D 283/00 - Heterocyclic compounds containing rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms, according to more than one of groups
• C07D 307/77 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
• C07D 327/02 - Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms one oxygen atom and one sulfur atom
• C07D 333/52 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes
• C07C 233/88 - Carboxylic acid amides having nitrogen atoms of carboxamide groups bound to an acyclic carbon atom and to a carbon atom of a six-membered aromatic ring wherein at least one ortho-hydrogen atom has been replaced
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
• A61P 5/00 - Drugs for disorders of the endocrine system
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Disclosed in the present invention is an amide compound, its preparation method and uses thereof, specifically, the compound of formula I or the pharmaceutically acceptable salts thereof, where R1, R2, R3, R4, R5, Q, X, N are defined as in the description. Also disclosed in the present invention are a preparation method for the compound of formula I, compositions containing same and the uses of same in the preparation of medicines for regulating blood lipids and/or preventing gallstones. The compound of formula I disclosed by the present invention is stable in vitro, shows good solubility in pharmaceutical organic solvents, and has favorable bioavailability in animals.

IPC Classes  ?

• C07C 235/20 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
• A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

Disclosed is a crystal form A of asiatic acid trometamol salt, showing main peaks at diffraction angle (2θ) of 5.98, 6.87, 9.12, 10.38, 12.00, 12.47, 12.93, 13.42, 14.72, 15.10, 17.01 and 18.14 degree, and minor peaks at diffraction angle (2θ) of 3.44, 13.87, 15.89, 19.04, 19.64, 20.17, 20.94, 21.75, 22.56, 23.33, 24.18, 26.38, 26.98 and 27.75 degree. Also disclosed is a crystal form B of asiatic acid trometamol salt, showing main peaks at diffraction angle (2θ) of 3.54, 7.05, 10.04, 11.88, 13.38, 14.29 and 15.18 degree, and minor peaks at diffraction angle (2θ) of 9.28, 9.59, 12.43, 16.68, 17.03, 17.57, 18.16, 18.91, 19.24, 20.07, 20.68, 22.46, 24.84, 25.20, 26.86, 27.73, 28.30, 28.85, 30.43, 30.83 and 33.93 degree. Also disclosed are the preparation methods of said crystal form A and form B. The crystal form A and form B of asiatic acid trometamol salt are new and have excellent stability. The preparation methods are easily operated and realized.

IPC Classes  ?

• C07J 63/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
• C07C 215/10 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
• C07C 213/10 - SeparationPurificationStabilisationUse of additives

Abstract

Disclosed are 4-aminoquinazoline derivatives and uses thereof. The results of pharmacological tests show that the said compounds or their salts in the present invention not only have the inhibition effect on Histone deacetylase, but also have the activities of inducing differentiation and anti-proliferation of some tumor cells. The said compounds and their salts can be used for treating cancer and the diseases associated with differentiation and proliferation, especially leukaemia and solid tumor. Animal tests show that the toxicity of the said compounds or their salts in the present invention is little. The general chemical structural formula is shown as below:

IPC Classes  ?

• C07D 239/94 - Nitrogen atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides a preparation method for N-methyl-N-ethyl-carbamic acid 3-[(S)-1(dimethylamino)ethyl] phenyl ester (as represented by the compound in formula X). The present invention also provides the following intermediates thereof: N-[S)-1-(3-methoxyphenyl)ethyl]-N,N-dimethyl-N-[(S)-1-phenylethylamino] ammonium salt (as represented by the compound in formula VI), N-[(S)-1-(3-hydroxyphenyl)ethyl]-N,N-dimethyl-N-[(S)-1- phenylethylamino] ammonium salt (as represented by the compound in formula VIII), and N-{(S)-1-[3-(N'-methyl-N'-ethylaminoformyloxy)phenyl]ethyl}-N, N-dimethyl-N-[(S)-1- phenylethylamino] ammonium salt (as represented by the compound in formula IX), as well as a method for using said compound in formula IX in the preparation of Rivastigmine, which can be used for treating Alzheimer's disease. The preparation method for Rivastigmine is of sound design. The materials needed for said method are easy to procure, the total yield therefrom is high, the chemical and optical purity of the resulting Rivastigmine is high, and the product can be produced in industry on a large scale.

IPC Classes  ?

• C07C 211/27 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by saturated carbon chains
• C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
• C07C 271/44 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
• A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

Compounds of the formula (I) or pharmaceutically acceptable salts thereof are disclosed. In the formula (I), R1, R2, R3, R4, R5 and n are defined as the specification. The preparation method for the compounds of the formula (I), the composition containing the compounds and the use of the compounds in preparing medicaments for regulating blood fat and preventing and treating biliary calculus are disclosed. The compounds of the formula (I) are stable in vitro, have good dissolubility in pharmaceutically applied organic solvents, and have good bioavailability in vivo.

IPC Classes  ?

• C07C 233/73 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
• C07C 69/738 - Esters of keto-carboxylic acids
• C07C 69/712 - Ethers the hydroxy group of the ester being etherified with a hydroxy compound having the hydroxy group bound to a carbon atom of a six-membered aromatic ring
• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
• C07C 67/08 - Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with the hydroxy or O-metal group of organic compounds
• C07C 67/14 - Preparation of carboxylic acid esters from carboxylic acid halides
• C07D 295/108 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulfur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
• A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61P 3/06 - Antihyperlipidemics
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

Disclosed are urea compounds represented by formula I or pharmaceutically acceptable salts, polymorphic forms, solvates or stereoisomers thereof; as well as preparation methods, intermediates and uses thereof. The urea compounds according to the present invention show various degrees of inhibitory activity against a variety of protein kinases in biological tests, and showed various degrees of activity against tumor cell growth and against angiogenesis in in vitro tests on resistance to the proliferation of human tumor cell line and human umbilical vein endothelial cells (HUVECs) respectively, and also exhibit good antitumor activity in vivo in animals.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• C07D 239/48 - Two nitrogen atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are quinolinone derivatives and use thereof as a medicament against schizophrenia. The quinolinone derivatives of the present invention have a high affinity to dopamine d2 receptors, not only showing a relatively strong antagonist activity, but also exhibiting partial activation of d2 receptors. The compounds have good oral absorption and exhibit low acute toxicity (LD50 > 1500 mg/kg, a single gavage in mice) that is equivalent to aripiprazole and ziprasidone and far lower than risperidone, thus having the potential to be developed into a novel medicament against schizophrenia. The general structure is as follows:

IPC Classes  ?

• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• A61P 25/22 - Anxiolytics
• A61P 25/24 - Antidepressants

Abstract

The present invention provides a new crystal form VII of agomelatine, the preparation method and use thereof and a pharmaceutical composition containing the same. The new crystal form has a good purity, a stable crystal form and good reproducibility; the preparation method thereof is easy to amplify; and it is superior to most previously reported crystal forms in terms of stability and solubility. Therefore, the crystal form VII of the present invention has an advantage in terms of preparation.

IPC Classes  ?

• C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
• C07C 231/24 - SeparationPurification
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 25/24 - Antidepressants

Abstract

Disclosed are an amorphous asiatic tromethamine salt and the preparation method thereof. The method comprises the steps of: (1) dissolving asiatic acid in an organic solvent; (2) mixing with tromethamine; (3) stirring and salifying the same, and then removing the organic solvent. The method for preparing the amorphous asiatic tromethamine salt is easy and effective, and the water solubility and bioavailability of the asiatic tromethamine salt thus obtained are greatly improved compared with the prior art.

IPC Classes  ?

• C07J 63/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
• C07C 215/10 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
• C07C 213/10 - SeparationPurificationStabilisationUse of additives

Abstract

The present invention provides a mixed crystal agomelatine (Form-VIII), the preparation method and use thereof and a pharmaceutical composition containing the same, wherein the mixed crystal mainly contains an agomelatine crystal form VI. The mixed crystal is stable and has good reproducibility, and is found through a stability test to be superior to a crystal form VI in terms of stability. Therefore, the Form-VIII of the present invention has an advantage in terms of preparation.

IPC Classes  ?

• C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
• C07C 231/24 - SeparationPurification
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 25/24 - Antidepressants

Abstract

The present invention provides a method for separating and purifying a cyclic hexapeptide compound or a pharmaceutically acceptable salt thereof. The cyclohexapeptide compound is preferably caspofungin.

IPC Classes  ?

• C07K 1/16 - ExtractionSeparationPurification by chromatography
• C07K 7/56 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid

Abstract

Disclosed in the present invention is an arylurea compound represented by formula I, or a pharmaceutically acceptable salt, a polymorph, a solvate or a stereoisomer thereof, and an intermediate and use thereof. The arylurea compound I of the present invention has protein kinase inhibiting activity, and antitumor and anti-angiogenesis activity.

IPC Classes  ?

• C07D 239/94 - Nitrogen atoms
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07C 273/18 - Preparation of urea or its derivatives, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups of substituted ureas
• C07C 275/40 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
• C07C 275/30 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by halogen atoms, or by nitro or nitroso groups
• C07D 295/13 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
• C07D 295/16 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
• C07D 277/44 - Acylated amino or imino radicals
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 35/00 - Antineoplastic agents
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 37/02 - Immunomodulators
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 27/02 - Ophthalmic agents
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 17/06 - Antipsoriatics

Abstract

Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.

IPC Classes  ?

• C07D 295/104 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulfur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

Abstract

Fused quinazoline derivatives and uses thereof as protein tyrosine kinase inhibitors and aurora kinase inhibitors are disclosed. Said protein tyrosine kinase inhibitors and aurora kinase inhibitors can be used in treating cancers, leukaemia and the diseases relevant to differentiation and proliferation. Said protein tyrosine kinase and aurora kinase dual inhibitors are the compounds represented by the following general formula or salts thereof.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Aralkyl diamine derivatives of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressant. The derivatives have triplex inhibiting activities on the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.

IPC Classes  ?

• C07D 333/58 - Radicals substituted by nitrogen atoms
• C07D 295/13 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
• C07D 295/073 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• C07D 295/02 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
• C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
• C07D 307/81 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
• C07D 317/58 - Radicals substituted by nitrogen atoms
• C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
• A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
• A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/4453 - Non-condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
• A61P 25/24 - Antidepressants

Abstract

Disclosed is a novel 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c] pyridine hydrochloride acetic acid solvate or its crystalline, and the preparation method of the solvate or its crystalline. The Prasugrel hydrochloride acetic acid solvate or its crystalline has better stability and solubility than Prasugrel hydrochloride. Furthermore, its pharmaceutical preparation has better dissolution and bioavailability than commercial preparation.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors