公开(公告)号：US5693812A

公开(公告)日：1997-12-02

申请号：US684125

申请日：1996-06-03

申请人： Gerald S. Brenner ,  Louis S. Crocker ,  Hossain Jahansouz ,  Robert D. Larsen ,  Chris H. Senanayake ,  Andrew S. Thompson ,  Karen C. Thompson ,  Thomas R. Verhoeven

发明人： Gerald S. Brenner ,  Louis S. Crocker ,  Hossain Jahansouz ,  Robert D. Larsen ,  Chris H. Senanayake ,  Andrew S. Thompson ,  Karen C. Thompson ,  Thomas R. Verhoeven

IPC分类号： C07D471/04 ,  C07D491/02

CPC分类号： C07D471/04

摘要： Polymorphic forms of the angiotensin II receptor antagonist, 3-�2'-(N-benzoyl)sulfonamidobiphenyl-4-yl!methyl-5,7-dimethyl-2-ethyl-3H-imidazo�4,5-b!pyridine and a method for the preparation of these crystal forms.

摘要翻译： 血管紧张素II受体拮抗剂3- [2' - （N-苯甲酰基）磺酰氨基联苯-4-基]甲基-5,7-二甲基-2-乙基-3H-咪唑并[4,5-b]吡啶的多晶型形式和 一种制备这些晶体形式的方法。

公开(公告)号：US20100137197A1

公开(公告)日：2010-06-03

申请号：US12666426

申请日：2008-06-23

申请人： Sachin Mittal ,  Hossain Jahansouz ,  Suttilug Sotthivirat

发明人： Sachin Mittal ,  Hossain Jahansouz ,  Suttilug Sotthivirat

IPC分类号： A61K38/12

CPC分类号： A61K38/12 ,  A61K9/0019 ,  A61K9/19 ,  A61K47/12 ,  A61K47/26

摘要： A lyophilized anti-fungal composition comprises (A) caspofungin, or a pharmaceutically acceptable salt thereof, in an effective amount; (B) one or more non-reducing sugars having a glass transition temperature Tg(s) of at least about 90° C.; and (C) an acetate buffer in an amount effective to provide a pH in a range of from about 5 to about 7; wherein the weight ratio of the one or more non-reducing sugars to caspofungin is in a range of from about 1.1:1 to about 10:1; the composition has a moisture content of about 0.8 wt. % or less; and the composition has a glass transition temperature Tg(c) of at least about 55° C. The lyophilized composition has good storage stability at temperatures up to and including room temperature. The composition can be reconstituted for use in preventing or treating fungal infections.

摘要翻译： 冻干的抗真菌组合物包含有效量的（A）卡泊芬净或其药学上可接受的盐; （B）玻璃化转变温度Tg（s）至少约90℃的一种或多种非还原糖; 和（C）有效提供约5至约7范围内的pH的乙酸盐缓冲液; 其中所述一种或多种非还原性糖与卡泊芬净的重量比在约1.1:1至约10:1的范围内; 该组合物的水分含量为约0.8wt。 ％ 或更少; 并且所述组合物的玻璃化转变温度Tg（c）为至少约55℃。所述冻干组合物在高达并且包括室温的温度下具有良好的储存稳定性。 该组合物可以重构用于预防或治疗真菌感染。

公开(公告)号：US20130023462A1

公开(公告)日：2013-01-24

申请号：US13628592

申请日：2012-09-27

申请人： Sachin Mittal ,  Hossain Jahansouz ,  Sutthilug Sotthivirat

发明人： Sachin Mittal ,  Hossain Jahansouz ,  Sutthilug Sotthivirat

IPC分类号： A61K38/12 ,  A61P31/10

CPC分类号： A61K38/12 ,  A61K9/0019 ,  A61K9/19 ,  A61K47/12 ,  A61K47/26

摘要： A lyophilized anti-fungal composition comprises (A) caspofungin, or a pharmaceutically acceptable salt thereof, in an effective amount; (B) one or more non-reducing sugars having a glass transition temperature Tg(s) of at least about 90° C.; and (C) an acetate buffer in an amount effective to provide a pH in a range of from about 5 to about 7; wherein the weight ratio of the one or more non-reducing sugars to caspofungin is in a range of from about 1.1:1 to about 10:1; the composition has a moisture content of about 0.8 wt. % or less; and the composition has a glass transition temperature Tg(c) of at least about 55° C. The lyophilized composition has good storage stability at temperatures up to and including room temperature. The composition can be reconstituted for use in preventing or treating fungal infections.

摘要翻译： 冻干的抗真菌组合物包含有效量的（A）卡泊芬净或其药学上可接受的盐; （B）玻璃化转变温度Tg（s）至少约90℃的一种或多种非还原糖; 和（C）有效提供约5至约7范围内的pH的乙酸盐缓冲液; 其中所述一种或多种非还原性糖与卡泊芬净的重量比在约1.1:1至约10:1的范围内; 该组合物的水分含量为约0.8wt。 ％ 或更少; 并且所述组合物的玻璃化转变温度Tg（c）为至少约55℃。所述冻干组合物在高达并且包括室温的温度下具有良好的储存稳定性。 该组合物可以重构用于预防或治疗真菌感染。

公开(公告)号：US20090123538A1

公开(公告)日：2009-05-14

申请号：US11886553

申请日：2006-04-14

申请人： Laman L. Alani ,  David C. Dubost ,  Bruce S. Foster ,  Soumojeet Ghosh ,  Hossain Jahansouz ,  Nazaneen Pourkavoos ,  Bhagwant Rege ,  Aditya Tatavarti

发明人： Laman L. Alani ,  David C. Dubost ,  Bruce S. Foster ,  Soumojeet Ghosh ,  Hossain Jahansouz ,  Nazaneen Pourkavoos ,  Bhagwant Rege ,  Aditya Tatavarti

IPC分类号： A61K9/20 ,  C07D257/04 ,  A61K31/41 ,  A61P9/12 ,  A61K9/16

CPC分类号： C07D403/10

摘要： The compounds of the present invention are polymorphic crystalline forms of the compound 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid, which has the structure (I). Specifically, the compounds of the invention are selected from the group consisting of 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid of Claim 3 selected from the group consisting of 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form I, 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form II, 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form III, and 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form IV, 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form V, 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VI, 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VII, and 2-butyl-4-chloro-1-[(2′-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VIII.

摘要翻译： 本发明的化合物是2-丁基-4-氯-1 - （（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-1-基的化合物的多晶型形式， 其具有结构（I）。 具体地说，本发明化合物选自2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑 -5-羧酸，其选自2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑 -5-甲酸盐酸盐形式I，2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸 盐酸盐形式II，2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸盐酸盐形式III和 2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式IV，2-丁基-4 - 氯 - 1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式V，2-丁基-4-氯-1- 甲基] - 咪唑-5-羧酸一水合物形式VI，2-丁基-4-氯-1 - [（2' - （1H-四唑-5-基）联苯-4-基） （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5- c 羧酸一水合物形式VII和2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式 八，