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Patent
Tianjin Institute of Pharmaceutical Research | Date: 2016-11-11

The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R^(1)-R^(7 )are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.


Patent
Tianjin Institute of Pharmaceutical Research | Date: 2015-07-15

Provided are a glucagon-like peptide-1 (GLP-1) analogue monomer and dimmer, a preparation method thereof, and an application thereof. The GLP-1 analogue monomer comprises one cysteine; and the dimer is formed by two monomer molecules connected via an intermolecular disulfide bond formed by the cysteine. The GLP-1 monomer comprising cysteine has the following general formula: ^(7)HAEX_(10)TFTSX_(15)VSSYLEX_(22)X_(23)AAKEFIX_(30)WLX_(33)KGRG^(37), wherein X_(10) is glycine or cysteine, X_(15) is aspartate or cysteine, X_(22) is glycine or cysteine, X_(23) is glutamine or cysteine, X_(30) is alanine or cysteine, and X_(33) is valine or cysteine; and only one of X_(10), X_(15), X_(22), X_(23), X_(30), and X_(33) is cysteine. The glucagon-like peptide-1 analogue dimer of the present invention has an in vivo half-life of more than 8 to 96 hours, thus facilitating clinical promotion and application.


Patent
Tianjin Institute of Pharmaceutical Research | Date: 2015-07-15

Provided is a GLP-1 analogue having the structure as shown in the general formula A:^(7)HAEX_(10)TFTSX_(15)VSSYLEX_(22)QAAKEFIX_(30)WLX_(33)KGRG^(37)n_(1)X_(1)Cn_(2)X_(2)(general 1 formula A),wherein X_(10) is glycine or cysteine, X_(15) is aspartic acid or cysteine, X_(22) is glycine or cysteine, X_(30) is alanine or cysteine, X_(33) is valine or cysteine, and at least one of X_(10), X_(15), X_(22), X_(30) and X_(33) is cysteine, X_(1) and X_(2) respectively is glycine, alanine or valine, n_(1)=1-30, n_(2)=1-30. The general formula A contains two cysteines to form disulfide bonds. Also provided are the preparation methods and the use of said GLP-1 analogue. Said GLP-1 analogue has a prolonged blood half-life compared with GLP-1, and can be used for the treatment of diabetes and obesity.


Patent
Tianjin Institute of Pharmaceutical Research | Date: 2013-12-05

The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R^(1)-R^(7 )are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.


Patent
Tianjin Institute of Pharmaceutical Research | Date: 2012-02-08

Provided is a GLP-1 analogue having the structure as shown in the general formula A: ^(7)HAEX_(10)TFTSX_(15)VSSYLEX_(22)QAAKEFIX_(30)WLX_(33)KGRG^(37)n_(1)X_(1)Cn_(2)X_(2 )(general formula A), wherein X_(10 )is glycine or cysteine, X_(15 )is aspartic acid or cysteine, X_(22 )is glycine or cysteine, X_(30 )is alanine or cysteine, X_(33 )is valine or cysteine, and at least one of X_(10), X_(15), X_(22), X_(30 )and X_(33 )is cysteine, X_(1 )and X_(2 )respectively is glycine, alanine or valine, n_(1)=1-30, n_(2)=1-30. The general formula A contains two cysteines to form disulfide bonds. Also provided are the preparation methods and the use of said GLP-1 analogue. Said GLP-1 analogue has a prolonged blood half-life compared with GLP-1, and can be used for the treatment of diabetes and obesity.


Patent
Tianjin Institute of Pharmaceutical Research | Date: 2013-03-20

A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation.


Patent
Tianjin Institute of Pharmaceutical Research | Date: 2012-12-05

The present invention relates to a sodium glucose cotransporter 2 (SGLT2) inhibitor with a phenyl C-glucoside structure, its preparation method, a pharmaceutical composition containing the same, and its use in treating diabetes and preparing an anti-diabetes medicament. The invention provides a compound with the structure of general formula I and a pharmaceutically acceptable salt and prodrug ester thereof,wherein, the definitions of R^(5) and R^(6) are selected from the following:(1) R5 = R6 = Me; (2) R5 =Me, R6 = OMe; (3) R5 =Me, R6 = H; (4) R5 =Me, R6 = F; (5) R5 = F, R6 = H; and (6) R5 = OMe, R6 = H.


Patent
Tianjin Institute of Pharmaceutical Research | Date: 2015-10-21

The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R^(1)-R^(7) are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.


Patent
Tianjin Institute of Pharmaceutical Research | Date: 2012-12-21

Provided is a pharmaceutical composition comprising candesartan or ester thereof and chlorthalidone, and use thereof, wherein the weight ratio of candesartan or ester thereof to chlorthalidone is 5.3:1 to 1:6.25. The pharmaceutical composition has a synergistic antihypertensive effect, and can enhance the antihypertensive effect and extend duration of antihypertension.


Patent
Tianjin Institute of Pharmaceutical Research | Date: 2012-01-11

The present invention relates to the field of the drugs associated with the diabetes. Particularly, the present invention relates to a dipeptidyl peptidase-IV inhibitor having the structure shown by formula (I), which contains amide thiazole structure and has an effect on treating diabetes, and a preparation method and a pharmaceutical composition containing it, as well as use thereof in manufacture of the drugs for treating the diabetes,_(1) is hydrogen, halogen, C_(1)-C_(5) alkyl, COOR_(3) or phenyl, wherein R_(3) is C_(1)-C_(5) alkyl; R_(2) is phenyl, substituted phenyl, 2-furanyl, substituted 2-furanyl, 2-thienyl, substituted 2-thienyl, 2-pyrrolyl, or substituted 2-pyrrolyl.

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