SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Li, Jianqi
Wang, Guan
He, Chasheng
Zhai, Ziran
Zhou, Yang
Du, Xinli
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.
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
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Zhang, Fuli
Zhang, Tao
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).
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
3.
BIOLOGICAL PEPTIDE FOR TREATING LUNG DISEASES AND APPLICATION THEREOF
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Liu, Li
Mei, Qibing
Ma, Shumei
Li, Liang
Liu, Nan
Gu, Fenghua
Wang, Jiahui
Xu, Wenqi
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.
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
China State Institute of Pharmaceutical Industry (China)
Shanghai Institute of Pharmaceutical Industry (China)
Inventor
Xie, Meihua
Zhang, Fuli
Wu, Taizhi
Zhong, Jialiang
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.
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Zhang, Fuli
Ni, Guowei
Chen, Shaoxin
Ju, Dianwen
Tang, Jiawei
Tan, Zhimin
Zou, Jie
Guo, Xiang
Wang, Zhengwen
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.
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 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
7.
SALT DERIVATIVE OF TETRAHYDROISOQUINOLINE AND CRYSTALLINE THEREOF AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Xie, Meihua
Zhang, Fuli
Wu, Taizhi
Zhong, Jialiang
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.
SHANGHAI INSTITUTE OF PHARMACEUICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Ma, Shuai
Pan, Jing
Liu, Zhenren
Zhou, Weicheng
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.
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD. (China)
Inventor
Guo, Yajun
Shan, Hanbin
Zhu, Xueyan
Yuan, Zhedong
Yu, Xiong
Guo, Meng
Hu, Mingtong
Wang, Duzheng
Huang, Yu
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.
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Ma, Shuai
Zhou, Weicheng
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.
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
11.
Platinum (II) compound, preparation method therefor, and pharmaceutical composition and application thereof
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Zhu, Baoquan
Shu, Yongzhi
Lin, Jun
Hu, Haifeng
Liu, Quanhai
Zhou, Bin
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.
SHANGHAI INSITITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD (China)
Inventor
Guo, Yajun
Shan, Hanbin
Zhu, Xueyan
Yuan, Zhedong
Yu, Xiong
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.
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Xiao, Xuhua
Sun, Yafei
Yao, Lixia
Shen, Shunyi
Liu, Quanhai
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.
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
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Xiao, Xuhua
Sun, Yafei
Shen, Shunyi
Liu, Quanhai
Xiao, Lin
Fan, Qianyong
Zhang, Zhihong
Ren, Yansong
Yao, Lixia
Zhang, Kaiting
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.
SHANGHAI INSITITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Shen, Shunyi
Chen, Daijie
Ge, Han
Zhang, Zhihong
Ren, Yansong
Li, Zhonglei
Fan, Qianyong
Zhang, Yun
Xu, Yijun
Li, Dan
Li, Jian
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.
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
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Zhu, Baoquan
Shu, Yongzhi
Lin, Jun
Hu, Haifeng
Liu, Quanhai
Zhou, Bin
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.
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Jin, Fang
Deng, Wangding
Yu, Xiong
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.
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
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Jin, Fang
Wang, Xiaowei
Yu, Xiong
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.
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 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
Shanghai Institute of Phamaceutical Industry (China)
China State Institute of Pharmaceutical Industry (China)
Inventor
Yu, Zhenpeng
Wang, Gouping
Zhang, Zhen
Liu, Minyu
Huang, Xiaoling
Liu, Ying
Xiao, Lin
Cai, Li
Wu, Xuejun
Deng, Yifang
Pan, Mianli
Chen, Renhai
Tang, Shenrong
Liu, Quanhai
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.
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 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
CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
Inventor
Jin, Fang
Fan, Ying
Yu, Xiong
Peng, Cheng
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.
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
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (China)
CHINA STATE INSTITUTE OF PRARMACEUTICAL INDUSTRY (China)
Inventor
Yu, Zhenpeng
Wang, Guoping
Zhang, Zhen
Liu, Minyu
Huang, Xiaoling
Liu, Ying
Xiao, Lin
Cai, Li
Wu, Xuejun
Deng, Yifang
Pan, Mianli
Chen, Renhai
Tang, Shenrong
Liu, Quanhai
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.
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