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Patent
Shanghai Institute of Pharmaceutical Industry, China State Institute Of Pharmaceutical Industry and Chia Tai Tianqing Pharmaceutical Group Co. | Date: 2017-05-10

Disclosed are a method for preparing a dabigatran etexilate intermediate, and an intermediate compound. The method for preparing a dabigatran etexilate intermediate 4 comprises: reacting a compound 3 with a C_(1)-C_(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.


Patent
Zhejiang Medicine Co., Shanghai Health Creation Center for Biopharmaceutical R & D Co. and Shanghai Institute of Pharmaceutical Industry | Date: 2015-11-04

The present invention provides a glycopeptide compound or pharmaceutically acceptable salt thereof as shown in Formula (I) or (II), and a method for preparing same, and pharmaceutical compositions and applications thereof, wherein the definition of R_(1), R_(2), R_(3), R_(4), R_(5) is the same as that of the specification. The glycopeptide compound of the present invention has in-vitro antibacterial activity and has important significance for development of new antibacterial agents.


Patent
Zhejiang Medicine Co. and Shanghai Institute of Pharmaceutical Industry | Date: 2016-07-20

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


Patent
China National Medicines Guorui Pharmaceutical Co. and Shanghai Institute of Pharmaceutical Industry | Date: 2015-02-18

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


Patent
Versitech Ltd and Shanghai Institute of Pharmaceutical Industry | Date: 2015-08-05

Water-soluble derivatives and/or prodrugs of Formula I are described herein.m and n are independently an integer from 0 to 3;X is O or N or S;R^(1) and R^(2) are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, aryl, alkaryl, arylalkyl, carboxyalkyl, amino, aminoalkyl, alkylamino, dialkylamino, arylamino, diarylamino, alkylarylamino, hydroxyalkyl, alkoxyalkyl, PO_(3)H_(2), PO_(3)^(2-)M, where M is one or more ammonium ions, alkali metal ions, or alkaline earth metal ions, phosphate ester,SO_(3)H, SO_(3) ^(-)M, where M is an ammonium ion, alkali metal ion, or alkaline earth metal ion, sulfonic ester, sulfonic ester, sulfonamide, -C(=O)-A^(1), or -C(=O)-L-A^(2).The compounds can be used as cardioprotection agents against myocardial infarction induced by ischemia-reperfusion. In one embodiment the compounds are used to treat ischemic cardiac diseases. In the preferred embodiment, the compounds are used to treat and/or prevent myocardial infarction in humans.


Patent
Zhejiang Hisun Pharmaceutical Co. and Shanghai Institute of Pharmaceutical Industry | Date: 2015-02-18

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


Patent
Zhejiang Hisun Pharmaceutical Co. and Shanghai Institute of Pharmaceutical Industry | Date: 2014-06-23

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


Patent
Zhejiang Hisun Pharmaceutical Co. and Shanghai Institute of Pharmaceutical Industry | Date: 2016-05-04

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


Patent
Shanghai Institute of Pharmaceutical Industry | Date: 2016-03-16

Disclosed are benzoisothiazole compounds and a use in the preparation of anti-schizophrenia drugs. The benzoisothiazole compounds of the present invention not only have strong affinity for dopamine D_(3) receptor, 5-HT_(1A) receptor and 5-HT_(2A) receptor, but also can observably improve the symptoms of schizophrenia relevant to apomorphine model and MK-801 model mice, with oral absorption being good, safety being high and side-effect being less, and having developmental value as new anti-neurotic disease drugs. The present invention is the compounds having a structure of general formula (I), or geometric isomers, free alkalies, salts, hydrates or solvates thereof.


Patent
Shanghai Institute of Pharmaceutical Industry and Li | Date: 2015-01-14

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

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