Abstract

An impurity A, an impurity B and an impurity G and preparation methods therefor, and an application as a reference standard for quality control of a compound as represented by formula VI are described. An impurity A, an impurity B and an impurity G and preparation methods therefor, and an application as a reference standard for quality control of a compound as represented by formula VI are described.

IPC Classes  ?

• 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 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
• C07D 217/24 - Oxygen atoms
• G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups

Abstract

The present invention relates to crystal form A of a propionamide derivative and a preparation method therefor. The crystal form A of the compound of formula (1) obtained in the present invention has good crystalline stability and chemical stability, and can be better used in clinical treatment. The present invention relates to crystal form A of a propionamide derivative and a preparation method therefor. The crystal form A of the compound of formula (1) obtained in the present invention has good crystalline stability and chemical stability, and can be better used in clinical treatment.

IPC Classes  ?

• 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
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

Provided are a 5-((1,2,3,4-tetrahydroisoquinoline-7-yl)amino)pyridin-2(1H)-one derivative, a preparation method therefor, and the use thereof. The derivative has the structure of a compound as shown by formula (I'). This compound has high pharmacological activity and selectivity for sigma-1 receptors, can be used for treating and preventing central nervous system diseases, and can particularly be used for preparing anti-depressant and anti-anxiety drugs.

IPC Classes  ?

• C07D 217/04 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
• C07D 217/02 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines
• C07D 217/08 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with a hetero atom directly attached to the ring nitrogen atom
• C07D 217/22 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
• C07D 213/64 - One oxygen atom attached in position 2 or 6
• C07D 213/72 - Nitrogen atoms
• A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
• A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
• A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
• A61P 25/22 - Anxiolytics
• A61P 25/24 - Antidepressants

Abstract

Provided are a co-amorphous substance of celecoxib and pregabalin and a preparation method therefor. The co-amorphous substance, especially the co-amorphous substance, of which the molar ratio of celecoxib to pregabalin is 2:1, is stable in structure, thereby improving the water solubility of celecoxib and providing a convenient physical form for combined administration of celecoxib and pregabalin.

IPC Classes  ?

• C07D 231/12 - 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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• C07C 229/08 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 25/06 - Antimigraine agents
• A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
• A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid

Abstract

2A2C2A2A is superior or similar to pimavanserin. The derivative is used for treating schizophrenia or Parkinson's disease, dementia-related behavioral disorders, and psychosis. The antipsychotic activity of the compound of the present application is equivalent to that of pimavanserin, the side effects of sedation and worsening of exercise are less than those of pimavanserin, and the cardiotoxicity is less than that of pimavanserin.

IPC Classes  ?

• 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 401/06 - 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 carbon chain containing only aliphatic carbon atoms
• C07D 401/14 - 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 three or more hetero rings
• C07D 243/04 - Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 3
• C07D 243/10 - Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• 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

Disclosed are a vortioxetine prodrug and the use thereof. The compound has a structure as shown in formula (A), and can be used to prepare a drug for treating neurological and psychotic diseases.

IPC Classes  ?

• C07D 295/185 - Radicals derived from carboxylic acids from aliphatic carboxylic acids
• C07D 295/192 - Radicals derived from carboxylic acids from aromatic carboxylic acids
• 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 25/24 - Antidepressants
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• A61P 25/22 - Anxiolytics
• 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

A preparation method for a paliperidone palmitate suspension, which uses piston slit high-pressure homogenization to prepare and obtain a paliperidone palmitate suspension. The obtained suspension has a suitable particle size distribution and can have an ideal sustained-release effect.

IPC Classes  ?

• A61K 9/10 - DispersionsEmulsions
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

A 1',2'-dihydro-3'H-spiro[cyclobutane 1,4'-isoquinoline]-3'-one derivative and an application thereof; the derivative has the structure represented by formula (A), and said class of compound can be used to prepare a drug for treating neuropsychiatric diseases.

IPC Classes  ?

• C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
• C07D 471/00 - 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 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
• A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
• A61K 31/435 - 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
• A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/22 - Anxiolytics
• A61P 25/24 - Antidepressants
• 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 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence

Abstract

The present invention falls within the medical field, and specifically relates to a fused heterocyclic derivative and a use thereof. The fused heterocyclic derivative has the structure of a compound as shown in formula (I), wherein the compound can be used to prepare drugs for treating neuropsychiatric diseases.

IPC Classes  ?

• C07D 455/04 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
• C07D 471/06 - Peri-condensed systems
• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

Provided is a co-crystal formed by flupentixol dihydrochloride and melitracen hydrochloride, wherein the molar ratio of flupentixol dihydrochloride and melitracen hydrochloride in the co-crystal is 1:1. The co-crystal has a good stability and a high solubility, and has a pharmaceutical effect superior to that of commercially available Deanxit tablets and with less side effects.

IPC Classes  ?

• C07D 335/20 - Thioxanthenes with hydrocarbon radicals, substituted by amino radicals, directly attached in position 9
• C07C 209/00 - Preparation of compounds containing amino groups bound to a carbon skeleton
• C07C 209/84 - Purification
• C07C 211/31 - 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 the six-membered aromatic ring being part of a condensed ring system formed by at least three rings
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
• A61P 25/24 - Antidepressants
• A61P 25/22 - Anxiolytics
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

An impurity A, an impurity B, and an impurity C and preparation methods therefor, and an application as a reference standard for quality control of a compound as represented by formula VI.

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
• 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 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 221/04 - Ortho- or peri-condensed ring systems
• C07D 217/00 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems

Abstract

Provided are a compound as represented by formula VI and a preparation method for an intermediate thereof. By using the method, the compound as represented by formula VI can be prepared and obtained efficiently, conveniently, and safely, and the purity of the compound as represented by final product formula VI is significantly improved.

IPC Classes  ?

• C07D 217/24 - Oxygen atoms
• 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 relates to crystal form A of a propanamide derivative and a preparation method therefor. The crystal form A of the compound of formula (1) obtained in the present invention has good crystalline stability and chemical stability, and can be better used in clinical treatment.

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
• C07D 217/24 - Oxygen 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 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

The present invention relates to crystal form A of a propionamide derivative and a preparation method therefor. The crystal form A of the compound of formula (1) obtained in the present invention has good crystalline stability and chemical stability, and can be better used in clinical treatment.

IPC Classes  ?

• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• C07D 217/24 - Oxygen 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 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

161818, pharmaceutical compositions comprising the crystal forms, preparation methods and the use of the crystal forms in the preparation of drugs for treating epilepsy, migraine, bipolar cell disease or pain.

IPC Classes  ?

• C07F 9/10 - Phosphatides, e.g. lecithin
• A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 25/06 - Antimigraine agents
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

A GLYX-13 preparation method and an intermediate compound thereof. According to the provided method, Fmoc-O-tert-butyl-L-threonine, Fmoc-L-proline, N-carboxybenzyl-L-threonine amide, and proline benzyl ester hydrochloride are used as starting materials; in virtue of eight easy-to-operate and economical synthetic steps, GLYX-13 can be prepared on a commercial scale and with a high yield, without using any expensive peptide condensation agent or any controlled precursor or aggressive deprotection agent.

IPC Classes  ?

• C07K 5/103 - Tetrapeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
• C07K 1/06 - General processes for the preparation of peptides using protecting groups or activating agents
• A61K 38/07 - Tetrapeptides
• A61P 25/24 - Antidepressants

Abstract

The present invention relates to a lactam compound derivative, a medicine composition comprising the lactam compound derivative, and uses of the composition and the lactam compound derivative in preparation of a medicine for preventing or treating schizophrenia, the lactam compound derivative having a structure as shown in Formula I.

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
• C07D 221/04 - Ortho- or peri-condensed ring systems
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• C07D 217/24 - Oxygen 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 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 239/88 - Oxygen atoms
• C07D 239/90 - Oxygen atoms with acyclic radicals attached in position 2 or 3
• 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 409/12 - 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 chain containing hetero atoms as chain links

Abstract

The present invention relates to the field of pharmaceutical chemistry, and specifically relates to a fused heterocyclic compound derivative and an application thereof. The fused heterocyclic compound derivative has the structure of general formula (I), and can be used to treat neuropsychiatric diseases.

IPC Classes  ?

• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• C07D 455/04 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
• C07D 471/06 - Peri-condensed systems
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

Abstract

The present invention relates to 3-[(benzo[d][1,3]dioxolan-4-yl)-oxy]-3-arylpropylamine compounds of formula I or pharmaceutically acceptable salts thereof and use thereof. The compound may be used to prepare an antidepressant agent.

IPC Classes  ?

• C07D 317/64 - Oxygen atoms
• A61P 25/24 - Antidepressants
• C07D 319/08 - 1,3-DioxanesHydrogenated 1,3-dioxanes condensed with carbocyclic rings or ring systems
• 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 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin

Abstract

The present invention relates to a lactam compound derivative, a medicine composition comprising the lactam compound derivative, and uses of the composition and the lactam compound derivative in preparation of a medicine for preventing or treating schizophrenia, the lactam compound derivative having a structure as shown in Formula I.

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
• C07D 217/24 - Oxygen atoms
• 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 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 239/88 - Oxygen atoms
• C07D 239/90 - Oxygen atoms with acyclic radicals attached in position 2 or 3
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin

Abstract

The present invention relates to the field of pharmaceutical chemistry, and specifically relates to a fused heterocyclic compound derivative and an application thereof. The fused heterocyclic compound derivative has the structure of general formula (I), and can be used to treat neuropsychiatric diseases.

IPC Classes  ?

• C07D 455/04 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
• C07D 471/06 - Peri-condensed systems
• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

The present invention relates to 3-[(benzo[d][1,3]dioxolane-4-yl)-oxy]-3-arylaniline type compounds of Formula I or pharmaceutical acceptable salts thereof and applications thereof. The compound may be used to prepare antidepressants.

IPC Classes  ?

• C07D 317/64 - Oxygen atoms
• A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
• A61P 25/24 - Antidepressants

Abstract

The present invention discloses use of a compound represented by formula I, or pharmaceutically acceptable salts thereof in the manufacture of medicaments for the treatment of depression. Specifically it relates to the triple inhibition effect of compounds of formula I on the reuptake of 5-HT, NE and DA. Their antidepressive effects may have broader indications and smaller neurotoxic side effects than single target antidepressants (such as fluoxetine) and dual targets antidepressants (such as duloxetine) currently used in clinic.

IPC Classes  ?

• 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 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• C07D 409/06 - 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 only aliphatic carbon atoms
• C07D 405/06 - 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 carbon chain containing only aliphatic carbon atoms
• A61P 25/24 - Antidepressants

Abstract

Disclosed in the present invention is a compound for preparing 4-(2-(4-methylphenylthio))phenylpiperidine, and a preparation method and use thereof. Provided in the present invention are two intermediates for preparing 4-(2-(4-methylphenylthio))phenylpiperidine: 3-(2-(4-methylphenylsulfhydryl))phenyl glutaric acid and 4-(2-(4-methylphenylsulfhydryl))phenylpiperidine-2,6-dione, and the preparation and use thereof. The method has a high yield, safe and convenient operation, small environmental pollution and is suitable for industrial production.

IPC Classes  ?

• C07D 211/20 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
• C07D 211/88 - Oxygen atoms attached in positions 2 and 6, e.g. glutarimide
• C07C 323/62 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton

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 belongs to pharmaceutical chemistry field. Paliperidone amino acids derivates and use thereof are disclosed After experiment, it is found that the compounds can be used for preparing medicant for treating mental diseases.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

The present invention belongs to the field of pharmaceutical chemistry, and, in particular, disclosed therein are a flavonoid derivative and use thereof. Disclosed is a flavonoid derivative having the structure of general formula (I) or a pharmaceutically acceptable salt thereof. This compound can be used in the preparation of drugs for preventing or treating central nervous system diseases.

IPC Classes  ?

• 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 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 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen 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 413/14 - 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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

50 is higher and therapeutic index is greater in animal models of catalepsy.

IPC Classes  ?

• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• C07D 311/94 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
• 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 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 417/14 - 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 three or more hetero 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
• C07D 311/80 - DibenzopyransHydrogenated dibenzopyrans
• C07D 409/12 - 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 chain containing hetero atoms as chain links

Abstract

The present invention relates to the field of pharmaceutical chemistry, and in particular, to a benzopyrone derivative and a use thereof. The benzopyrone derivative is compound having a structure of formula (I) or a pharmaceutically acceptable salt thereof. It has been found by experiments that, this type of compounds is useful in prevention or treatment of neuropsychical diseases.

IPC Classes  ?

• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• 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 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
• 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
• 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 417/14 - 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 three or more hetero rings

Abstract

The present invention belongs to the medicinal chemistry field, and specifically discloses a [1,3,4]oxadiazole derivative with the structure of general formula (I) and pharmaceutically acceptable salt thereof. The compound can be used to prepare a medicine for preventing or treating a disease of the central nervous system.

IPC Classes  ?

• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• 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
• 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 417/14 - 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 three or more hetero rings

Abstract

The present invention relates to a preparation method of tapentadol hydrochloride and compounds for preparation of the tapentadol hydrochloride. The preparation method comprises steps using a compound in a formula V or a hydrochloride thereof as a raw material for preparation of the tapentadol hydrochloride, and is characterized in that the preparation method of the hydrochloride of the compound in the formula V comprises the following step that in solvent, a hydrochloride of a compound in a formula IV reacts with a hydrogenolysis reagent under existence of a catalytic agent. According to the process, chiral column separation is not needed, a removal condition of protecting group allyl is mild, yield is high, and industrialization production is benefited.

IPC Classes  ?

• C07C 215/54 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
• C07C 215/58 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
• 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
• C07C 217/72 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms with singly-bound oxygen atoms and six-membered aromatic rings bound to the same carbon atom of the carbon chain linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
• C07C 225/16 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
• C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
• C07C 49/84 - Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups
• C07C 45/71 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by isomerisationPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups

Abstract

Provided are a benzodioxane compound as shown by the general formula (I), a pharmaceutical composition comprising same and the use thereof in treating psychotic and neuropathic diseases, particularly depression.

IPC Classes  ?

• 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
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• 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 25/00 - Drugs for disorders of the nervous system

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

Disclosed are a substituted benzopyran derivative and the use thereof. The substituted benzopyran derivative has the structure of formula (I). It has been found in experiments that the derivative can be used to prepare drugs for treating psychotic conditions.

IPC Classes  ?

• C07D 311/16 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted in position 7
• C07D 311/18 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted otherwise than in position 3 or 7
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• A61P 25/22 - Anxiolytics
• A61P 25/24 - Antidepressants
• A61P 25/06 - Antimigraine agents
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• 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 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

Abstract

Disclosed are alicyclic[c] benzopyrone derivatives and uses thereof. The said alicyclic[c] benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve climbing symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and climbing symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.

IPC Classes  ?

• C07D 311/94 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
• 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 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
• C07D 311/80 - DibenzopyransHydrogenated dibenzopyrans
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• A61P 25/22 - Anxiolytics
• A61P 25/24 - Antidepressants
• A61P 25/06 - Antimigraine agents
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• 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 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

Abstract

The present invention relates to the field of pharmaceutical chemistry, and in particular, to a benzopyrone derivative and a use thereof. The benzopyrone derivative is compound having a structure of formula (I) or a pharmaceutically acceptable salt thereof. It has been found by experiments that, this type of compounds is useful in prevention or treatment of neuropsychical diseases.

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
• 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 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

The present invention belongs to the medicinal chemistry field, and specifically discloses a [1,3,4] oxadiazole derivative with the structure of general formula （I） and pharmaceutically acceptable salt thereof. The compound can be used to prepare a medicine for preventing or treating a disease of the central nervous system.

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 417/14 - 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 three or more hetero 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
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate, 3 and Ar are as defined in the specification. The derivative is non-opioid analgesic, has good analgesic effect and relatively small side effects. The invention also relates to a composition comprising the derivative and its use.

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
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• C07D 295/088 - 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 bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
• C07D 403/08 - 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 carbon chain containing alicyclic rings
• C07D 417/08 - 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 carbon chain containing alicyclic rings

Abstract

A process for the manufacture of agomelatine and its intermediate N-[2-(7-methoxy- 1-naphthy)ethyl]phthalimide is provided and inclues reacting 7-methoxy-1-naphthyl ethanol (III) with benzenesulfonyl chloride to obtain 7-methoxy-1 -naphthylethyl benzene sulfonate (IV), which is reacted with potassium phthalimide to produce N-[2-(7-methoxy-1-naphthy)ethyl]phthalimide (II); and subjecting N-[2-(7-methoxy-1-naphthy)ethyl]phthalimide (II) to alkaline hydrolysis and acetylation, to obtain agomelatine.

IPC Classes  ?

• C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide

Abstract

The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects.

IPC Classes  ?

• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• C07D 211/48 - Oxygen atoms attached in position 4 having an acyclic carbon atom attached in position 4

Abstract

The substituted phenyl piperazinyl aralkylone derivatives shown as the following formula, and the salts and hydrates thereof are disclosed, in which R, R1, R2, R3 and A are defined as the description. The pharmaceutical compositions containing such derivatives and the uses thereof are also disclosed.

IPC Classes  ?

• 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
• C07D 295/182 - Radicals derived from carboxylic acids
• C07D 213/38 - Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
• 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
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

The use of aryl piperazines of formula (I) in manufacturing a medicament for treating acute pain, neuropathic pain or receptive nociceptive pain in mammals including human beings is disclosed.

IPC Classes  ?

• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/00 - Medicinal preparations containing organic active ingredients
• A01N 43/00 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds

Abstract

Preparation methods of rivastigmine tartrate and its intermediate and the intermediate itself are disclosed. More specifically, the intermediate compound [1-(3-benzyloxy-phenyl)-ethyl]-dimethylamine, its preparation method and methods for preparing 3-(1-(dimethylamino) ethyl) phenol and rivastigmine tartrate using the intermediate compound are disclosed.

IPC Classes  ?

• C07C 217/58 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
• C07C 213/02 - 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 involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
• C07C 213/06 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton from hydroxy amines by reactions involving the etherification or esterification of hydroxy groups
• C07C 269/00 - 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
• C07C 215/50 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
• 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

Abstract

The invention provides benzisoxazole piperidinyl derivatives, their salts and their hydrates: Wherein R, X, Y, R’ and T have the same definition as that described in the description. The kind of compounds has antagonistic effect on 5-HT2A and has mediating effect on 5-hydroxytryptamine system such as reuptake inhibiting effect of 5-HT and so on. The compounds of the present invention possess excellent analgesia, sedation activity, minimal toxicity and side effects. The invention also provides pharmaceutical compositions comprising the derivatives and their use.

IPC Classes  ?

• C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
• A61K 31/435 - 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
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The substituted phenylpiperazinyl aralkylalcohol derivatives shown as the following formula (I), and the salts and hydrates thereof, in which C1 and C2 are chiral carbon atoms, the compound is one of six isomer of (1RS, 2SR), (1RS, 2RS), (1R,2S), (1S, 2S), (1R, 2R), or (1S, 2R), and R, R1, R2, R3 and Ar are defined as the definition in description, These derivatives are non-opioid analgesics, and they have good analgesic effects and lower toxicity and side effects. The pharmaceutical compositions containing such derivatives and the uses thereof.

IPC Classes  ?

• C07D 295/092 - 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 bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings with aromatic radicals attached to the chain
• C07D 209/34 - Oxygen atoms in position 2
• C07D 235/26 - Oxygen atoms
• C07D 277/68 - Benzothiazoles 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 in position 2
• 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 31/428 - Thiazoles condensed with carbocyclic rings
• A61K 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

The process for the manufacture of agomelatine and its intermediate N-[2-(7-methoxy-1-naphthyl)-ethyl]phthalimide comprises 7-methoxy-1-naphthyl ethanol(III) reacting with benzene sulfonyl chloride to obtain 7-methoxy-1-naphthyl-ethyl benzene sulfonate(IV), then IV reacting with potassic salt of phthalimide to produce N-[2-(7-methoxy-1-naphthyl)-ethyl]phthalimide (II), which being hydrolyzed under alkali, then being acetylated to obtain agomelatine.

IPC Classes  ?

• C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide

Abstract

The invention provides a process for preparing osemozotan and its pharmaceutically acceptable salts. The invention also provides an intermediate, (2R)-N-[3-(1,3- benzodioxol-5-yloxy)propyl]-1,4-benzodioxin-2-formamide, used in the process and its preparation.

IPC Classes  ?

• C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen 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 319/20 - 1,4-DioxanesHydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring with substituents attached to the hetero ring

Abstract

Aralkyl piperidine derivatives, compositions containing them, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are free alkalis or salts as the following formula. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects.

IPC Classes  ?

• C07D 211/48 - Oxygen atoms attached in position 4 having an acyclic carbon atom attached in position 4
• C07D 401/10 - 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 carbon chain containing aromatic rings
• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
• A61P 25/20 - HypnoticsSedatives
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

The use of the aryl piperazine compounds of fomula (I) in manufacturing medicant for treating acute pain, nerve ache or nociceptive pain in mammals including human is disclosed.

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
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

A process for preparation of gabapentin hydrochloride by converting 1,5-dicyano-2,4-dioxo-3-azaspiro[5,5]-undecane into 1,5-diaminoformyl-2,4-dioxo-3-azaspiro[5,5]-undecane at a temperature of 65° C. to 85° C. in the presence of a strong acid, and then carrying out Hofmann rearrangement under an alkaline condition. The starting material of the process is readily available. The process is simple, and can reduce the purification procedure of intermediates, reduce production cost, and obtain product with higher purity.

IPC Classes  ?

• C07C 53/134 - Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing rings monocyclic
• C07D 221/20 - Spiro-condensed ring systems

Abstract

The present invention provided a process for the preparation of gabapentin hydrochloride. The process comprises: conventing 1,5-dicyano-2,4-dioxo-3-azaspiro⏧5,5]undecane into 1,5-dicarbamoyl-2,4-dioxo-3-azaspiro⏧5,5]undecane at a temperature between 65 to 85 and in the presence of strong acid, then carrying out the Hoffmann rearrangement reaction in the presence of base. The starting material of present process is readily available. The process is simple, and can decrease the purification procedure for the intermediate, reduce the cost, and obtain the product with high purity.

IPC Classes  ?

• C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
• C07C 227/22 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from lactams, cyclic ketones or cyclic oximes, e.g. by reaction involving Beckmann rearrangement
• C07C 233/00 - Carboxylic acid amides
• C07C 231/10 - Preparation of carboxylic acid amides from compounds not provided for in groups
• C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
• C07D 221/20 - Spiro-condensed ring systems

Abstract

3-isobutyl-glutaryl imine i.e.4-isobutyl-piperidine-2,6-dione useful as intermediate in preparation of pregabalin useful for treating epilepsy and neuropathic pain and its preparation method. The method includes 3-isobutyl-glutaric acid reacts with nitrogen-containing reactant via forming-ring reaction to obtain 4-isobutyl-piperidine-2,6-dione, the later via Hoffman rearrangement reaction and resolution to give S-(+)-3-isobutyl-᜼-amino-butyric acid. The method is simple in process. The intermediate and the end product both are easy to be separated from reaction solvent or recrystal solvent. The method is cost-efficient and is suitable for mass production.

IPC Classes  ?

• C07D 211/88 - Oxygen atoms attached in positions 2 and 6, e.g. glutarimide
• C07C 227/22 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from lactams, cyclic ketones or cyclic oximes, e.g. by reaction involving Beckmann rearrangement