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1. 发明授权

US06130333A Bicyclic imidazolyl derivatives as phosphodiesterase inhibitors, pharmaceutical compositions and method of use 失效
标题翻译：作为磷酸二酯酶抑制剂的双环咪唑基衍生物，药物组合物和使用方法
公开(公告)号：US06130333A
公开(公告)日：2000-10-10
申请号：US200863
申请日：1998-11-27
申请人： Horng-Chih Huang , Timothy S. Chamberlain , Steven Lynn Settle , William Dean Joy , Ned R. Siegel , Leslie D. Bell
发明人： Horng-Chih Huang , Timothy S. Chamberlain , Steven Lynn Settle , William Dean Joy , Ned R. Siegel , Leslie D. Bell
IPC分类号： A61K31/4184 , C07D405/04 , C07D405/14 , C07D471/04 , C07D235/04 , A61K31/443 , C07D401/06 , C07D471/02 , A61K81/437 , A61N27/06
CPC分类号： C07D405/04 , A61K31/4184 , C07D405/14 , C07D471/04
摘要： The present invention provides for compounds having the following Formulae I-III, ##STR1## and ##STR2## The compounds of the present invention are useful in the treatment of a variety of disease such as glaucoma, sexual dysfunction, asthma and cardiovascular disorders such as stable-, unstable- and variant-angina, hypertension, pulmonary hypertension, congestive heart failure, atherosclerosis, and thrombosis.
摘要翻译：本发明提供具有以下式I-III的化合物，本发明化合物可用于治疗各种疾病，如青光眼，性功能障碍，哮喘和心血管疾病如稳定，不稳定和变异型心绞痛，高血压，肺动脉高压，充血性心力衰竭，动脉粥样硬化和血栓形成。

2. 发明申请

US20050267123A1 6-Membered heterocyclic compounds useful for selective inhibition of the coagulation cascade 审中-公开
标题翻译：可用于选择性抑制凝血级联的6-元杂环化合物
公开(公告)号：US20050267123A1
公开(公告)日：2005-12-01
申请号：US11159877
申请日：2005-06-23
申请人： Michael South , Ronald Webber , Horng-Chih Huang , Mihaly Toth , Alan Moormann , Jeffery Snyder , Jeffrey Scholten , Danny Garland , Melvin Rueppel , William Neumann , Scott Long , Wei Huang , John Trujillo , John Parlow , Darin Jones , Brenda Case , Michael Hayes
发明人： Michael South , Ronald Webber , Horng-Chih Huang , Mihaly Toth , Alan Moormann , Jeffery Snyder , Jeffrey Scholten , Danny Garland , Melvin Rueppel , William Neumann , Scott Long , Wei Huang , John Trujillo , John Parlow , Darin Jones , Brenda Case , Michael Hayes
IPC分类号： C07D249/12 , A61K31/451 , A61K31/495 , A61K31/50 , A61K31/513 , A61K31/53 , A61K31/535 , A61K45/00 , A61P7/02 , A61P9/10 , A61P43/00 , C07C257/18 , C07D207/32 , C07D211/56 , C07D211/98 , C07D213/74 , C07D231/38 , C07D231/48 , C07D237/04 , C07D239/10 , C07D239/22 , C07D241/04 , C07D241/20 , C07D249/14 , C07D253/06 , C07D253/075 , C07D263/48 , C07D265/02 , C07D277/42 , C07D307/22 , C07D333/36 , C07D401/12 , C07D403/10 , C07D413/12 , C07D471/04 , C07D43/02
CPC分类号： C07D213/74 , C07C257/18 , C07C2601/04 , C07C2601/10 , C07D207/32 , C07D211/56 , C07D211/98 , C07D231/38 , C07D231/48 , C07D237/04 , C07D239/10 , C07D239/22 , C07D241/04 , C07D241/20 , C07D249/14 , C07D253/06 , C07D253/075 , C07D263/48 , C07D265/02 , C07D277/42 , C07D307/22 , C07D333/36 , C07D401/12 , C07D403/10 , C07D413/12 , C07D471/04
摘要： The present invention relates to compounds, and prodrugs thereof, compositions and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
摘要翻译：本发明涉及化合物及其前药，可用于预防和治疗哺乳动物血栓形成病症的组合物和方法。本发明的化合物及其前药选择性地抑制凝血级联的某些蛋白酶。

3. 发明授权

US5684195A Method of preparing sulfmonamides from sulfones 失效
标题翻译：从砜制备磺胺甲酰胺的方法
公开(公告)号：US5684195A
公开(公告)日：1997-11-04
申请号：US455460
申请日：1995-05-31
申请人： Horng-Chih Huang , Scott R. Harring
发明人： Horng-Chih Huang , Scott R. Harring
IPC分类号： C07C303/36 , C07C311/16 , C07C313/04 , C07D333/18
CPC分类号： C07D333/18 , C07C303/36 , C07C313/04 , C07C2101/10 , C07C2102/50
摘要： A one-pot synthesis of sulfonamides from sulfones has been developed. Conversion of sulfones to the corresponding sulfinic acid salts is followed by oxidative-amination to give the sulfonamides.
摘要翻译：已经开发了一种从砜合成磺胺类药物。将砜转化为相应的亚磺酸盐，然后进行氧化 - 胺化得到磺酰胺。

4. 发明授权

US5674879A Compositions including and methods of using conformationally restricted angiotensin II antagonist 失效
标题翻译：组合物包括使用构象限制性血管紧张素II拮抗剂的方法
公开(公告)号：US5674879A
公开(公告)日：1997-10-07
申请号：US398031
申请日：1995-03-03
申请人： Robert E. Manning , Horng-Chih Huang
发明人： Robert E. Manning , Horng-Chih Huang
IPC分类号： A61K31/437 , C07D471/04 , C07D487/04 , A61K31/435
CPC分类号： A61K31/437 , C07D471/04 , C07D487/04
摘要： Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders.
摘要翻译：描述了构形限制的化合物，其作为用于治疗循环系统疾病的血管紧张素II拮抗剂是治疗有效的。

5. 发明授权

US5576339A Pyridyl substituted cyclopentadienes for the treatment of inflamation 失效
标题翻译：吡啶基取代环戊二烯用于治疗炎症
公开(公告)号：US5576339A
公开(公告)日：1996-11-19
申请号：US417341
申请日：1995-04-05
申请人： Horng-Chih Huang , David R. Reitz
发明人： Horng-Chih Huang , David R. Reitz
IPC分类号： C07C311/16 , C07C317/14 , A61K31/44
CPC分类号： C07C317/14 , C07C311/16 , C07C2101/10
摘要： A class of 2,3-substituted cyclopenta-2,4-dienyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, lower alkyl, lower hydroxyalkyl, halo, lower haloalkyl, lower alkoxycarbonyl and carboxyl; and wherein each of R.sup.3 through R.sup.12 is independently selected from hydrido, halo, lower alkyl, lower alkylthio, cyano, hydroxyl, mercapto, lower haloalkyl, lower haloalkoxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower alkylsulfonyl, lower haloalkylsulfonyl and sulfamyl; provided R.sup.5 and R.sup.10 are not both hydrido or methoxy; or a pharmaceutically suitable salt or prodrug thereof.
摘要翻译：描述了一类2,3-取代的环戊二烯-2,4-二烯基化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式II定义：倾向选自氢化，低级烷基，低级羟烷基，卤素，低级卤代烷基，低级烷氧基羰基和羧基; R 3至R 12各自独立地选自氢，卤素，低级烷基，低级烷硫基，氰基，羟基，巯基，低级卤代烷基，低级卤代烷氧基，低级烷氧基，低级羟烷基，低级烷氧基烷基，低级烷基磺酰基，低级卤代烷基磺酰基和氨磺酰基。条件是R 5和R 10不同时为氢或甲氧基; 或其药学上合适的盐或前药。

6. 发明授权

US5512561A Aryl substituted dibenzoxazepine compounds, pharmaceutical compositions and methods of use 失效
公开(公告)号：US5512561A
公开(公告)日：1996-04-30
申请号：US402257
申请日：1995-03-10
申请人： Nizal S. Chandrakumar , Horng-Chih Huang , Richard A. Mueller
发明人： Nizal S. Chandrakumar , Horng-Chih Huang , Richard A. Mueller
IPC分类号： C07D267/20 , C07D413/06 , C07D413/12 , C07D413/14 , A61K31/55 , C07D281/14
CPC分类号： C07D413/12 , C07D267/20 , C07D413/06 , C07D413/14
摘要： The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and for the treatment of prostaglandin E.sub.2 -mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin E.sub.2 -mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

7. 发明授权

US08633206B2 Pyrrolo[2,3-D]pyrimidine compounds 有权
标题翻译：吡咯并[2,3-D]嘧啶化合物
公开(公告)号：US08633206B2
公开(公告)日：2014-01-21
申请号：US12903554
申请日：2010-10-13
申请人： Michele Ann Promo , Jin Xie , Brad A. Acker , Susan J. Hartmann , Sergey Gregory Wolfson , Horng-Chih Huang , Eric Jon Jacobsen
发明人： Michele Ann Promo , Jin Xie , Brad A. Acker , Susan J. Hartmann , Sergey Gregory Wolfson , Horng-Chih Huang , Eric Jon Jacobsen
IPC分类号： C07D487/04 , A61K31/519 , A61P37/06 , A61P17/06 , A61P29/00
CPC分类号： C07D487/04
摘要： Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.
摘要翻译：本文描述的是吡咯并[2,3-d]嘧啶化合物，它们用作Janus Kinase（JAK）抑制剂，含有这些化合物的药物组合物及其制备方法。

8. 发明申请

US20050153965A1 Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade 审中-公开
标题翻译：用于选择性抑制凝血级联的取代的多环芳基和杂芳基吡啶
公开(公告)号：US20050153965A1
公开(公告)日：2005-07-14
申请号：US11004437
申请日：2004-12-03
申请人： Michael South , Brenda Case , Danny Garland , Michael Hayes , Horng-Chih Huang , Wei Huang , Darin Jones , William Neumann , John Parlow , David Reitz , Melvin Rueppel , Ronald Webber
发明人： Michael South , Brenda Case , Danny Garland , Michael Hayes , Horng-Chih Huang , Wei Huang , Darin Jones , William Neumann , John Parlow , David Reitz , Melvin Rueppel , Ronald Webber
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61K45/00 , A61P7/02 , A61P9/10 , A61P11/00 , A61P35/00 , A61P43/00 , C07D213/74 , C07D213/89 , C07D401/10 , C07D409/04 , C07D43/02 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D41/02
CPC分类号： C07D213/74 , C07D213/89
摘要： The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
摘要翻译：本发明涉及化合物及其前药，可用于预防和治疗哺乳动物血栓形成病症的组合物和方法。本发明的化合物及其前药选择性地抑制凝血级联的某些蛋白酶。

9. 发明授权

US5670510A Pyridyl substituted spirodienes for the treatment of inflammation 失效
标题翻译：吡啶基取代螺旋体用于治疗炎症
公开(公告)号：US5670510A
公开(公告)日：1997-09-23
申请号：US679410
申请日：1996-07-09
申请人： Horng-Chih Huang , David R. Reitz
发明人： Horng-Chih Huang , David R. Reitz
IPC分类号： C07C311/16 , C07C311/29 , C07C317/14 , C07C317/22 , C07C317/44 , C07C323/65 , C07C323/67 , C07D213/34 , C07D213/61 , C07D213/71 , A61K31/44 , C07D213/00 , C07D213/57 , C07D213/62
CPC分类号： C07C317/44 , C07C311/16 , C07C311/29 , C07C317/14 , C07C317/22 , C07C323/65 , C07C323/67 , C07D213/34 , C07D213/61 , C07D213/71
摘要： A class of substituted spirodienes is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein A is selected from ##STR2## wherein each of R.sup.1 through R.sup.10 is independently selected from hydrido, halo, alkyl, alkoxy, alkylthio, cyano, haloalkyl, haloalkoxy, hydroxyalkyl; alkoxyalkyl, hydroxyl, mercapto, alkylsulfonyl, haloalkylsulfonyl, and sulfamyl; and wherein n is a number selected from 0, 1, 2 and 3; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类取代的螺旋体用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式I定义：其中A选自，其中R 1至R 10各自独立地选自氢，卤，烷基，烷氧基，烷硫基，氰基，卤代烷基，卤代烷氧基，羟烷基; 烷氧基烷基，羟基，巯基，烷基磺酰基，卤代烷基磺酰基和氨磺酰基; 并且其中n是选自0,1,2和3的数; 或其药学上可接受的盐。

10. 发明申请

US20110294826A1 PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS 失效
标题翻译：吡咯并[2,3-D]吡嗪化合物
公开(公告)号：US20110294826A1
公开(公告)日：2011-12-01
申请号：US12964841
申请日：2010-12-10
申请人： Jin Xie , Michele Ann Promo , Eric Jon Jacobsen , Horng-Chih Huang , Todd M. Maddux
发明人： Jin Xie , Michele Ann Promo , Eric Jon Jacobsen , Horng-Chih Huang , Todd M. Maddux
IPC分类号： A61K31/519 , A61P25/28 , A61P19/02 , A61P35/00 , A61P3/10 , A61P31/12 , A61P25/00 , A61P31/00 , A61P29/00 , A61P37/00 , A61P37/08 , C07D487/04 , A61P35/02
CPC分类号： C07D487/04
摘要： Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.
摘要翻译：本文描述的是吡咯并[2,3-d]嘧啶化合物，它们用作Janus Kinase（JAK）抑制剂，含有这些化合物的药物组合物及其制备方法。

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