公开(公告)号：US20070281938A1

公开(公告)日：2007-12-06

申请号：US11596982

申请日：2005-05-24

Applicant: Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallagarda ,  Meredith Williams ,  Christopher Fostsch ,  Eric Bercot ,  Aiwen Li ,  Guolin Cai ,  Randall Hungate ,  Chester Yuan ,  Christopher Tegley ,  David St. Jean ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael Bartberger ,  George Moniz ,  Matthew Frizzle

Inventor： Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallagarda ,  Meredith Williams ,  Christopher Fostsch ,  Eric Bercot ,  Aiwen Li ,  Guolin Cai ,  Randall Hungate ,  Chester Yuan ,  Christopher Tegley ,  David St. Jean ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael Bartberger ,  George Moniz ,  Matthew Frizzle

IPC: C07D277/60 ,  A61K31/426 ,  A61K31/4436 ,  A61K31/4535 ,  A61K31/497 ,  A61K31/5377 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D417/02 ,  C07D413/02 ,  C07D401/02 ,  A61P17/02 ,  C07D211/68 ,  C07D277/02 ,  C07D277/08

CPC classification number: C07D417/06 ,  C07D263/34 ,  C07D263/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/54 ,  C07D277/60 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  C07F7/1804

Abstract: The present invention relates to compounds with the formula (I) wherein R1, R2, R3, R4, and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Abstract translation: 本发明涉及具有式（I）的化合物，其中R 1，R 2，R 3，R 4， SUP>和Z如本文所定义，并且还涉及包含该化合物的药物组合物，以及该化合物在医药中的用途以及用于制备作用于人类11-β-羟基类固醇脱氢酶1型的药物 酶。

公开(公告)号：US07265138B2

公开(公告)日：2007-09-04

申请号：US10775980

申请日：2004-02-09

Applicant: Elizabeth M. Doherty ,  Christopher H. Fotsch ,  Nianhe Han ,  Randall W. Hungate ,  Qingyian Liu ,  Mark H. Norman ,  Ning Xi ,  Shimin Xu

Inventor： Elizabeth M. Doherty ,  Christopher H. Fotsch ,  Nianhe Han ,  Randall W. Hungate ,  Qingyian Liu ,  Mark H. Norman ,  Ning Xi ,  Shimin Xu

IPC: A61K31/425 ,  C07D277/04

CPC classification number: C07D233/90 ,  C07D263/34 ,  C07D277/56 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

Abstract translation: 具有一般结构和含有它们的组合物的化合物，用于治疗急性，炎性和神经性疼痛，牙痛，一般头痛，偏头痛，丛集性头痛，混合血管和非血管综合征，紧张性头痛，一般炎症，关节炎，风湿性 疾病，骨关节炎，炎症性肠病，炎症性眼病，炎症性或不稳定性膀胱病，银屑病，皮肤炎症成分炎症，慢性炎性病症，炎性疼痛及相关的痛觉过敏和异常性疼痛，神经性疼痛及相关的痛觉过敏和异常性疼痛，糖尿病性神经病疼痛， 咳嗽痛，交感神经痛，交感综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸系统内脏运动紊乱，泌尿生殖道，胃肠道或血管区，伤口，烧伤，过敏性皮肤反应，瘙痒，白癜风，一般胃肠道疾病， G 腹部溃疡，十二指肠溃疡，腹泻，坏死因子诱发的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。

公开(公告)号：US07199244B2

公开(公告)日：2007-04-03

申请号：US10823372

申请日：2004-04-12

Applicant: Robert D. Groneberg ,  James Zhan ,  Benny C. Askew, Jr. ,  Derin C. D'Amico ,  Nianhe Han ,  Christopher H. Fotsch ,  Qingyian Liu ,  Babak Riahi ,  Jiawang Zhu ,  Kevin Yang ,  Jian Jeffrey Chen ,  Rana Nomak

Inventor： Robert D. Groneberg ,  James Zhan ,  Benny C. Askew, Jr. ,  Derin C. D'Amico ,  Nianhe Han ,  Christopher H. Fotsch ,  Qingyian Liu ,  Babak Riahi ,  Jiawang Zhu ,  Kevin Yang ,  Jian Jeffrey Chen ,  Rana Nomak

IPC: C07D211/08 ,  C07D405/00

CPC classification number: C07D207/48 ,  C07D211/96 ,  C07D215/58 ,  C07D217/22 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于治疗疼痛和疾病如炎症介导的疾病是有效的。 本发明包括新的化合物，类似物，前药和其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及疼痛，炎症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US06583154B1

公开(公告)日：2003-06-24

申请号：US09640263

申请日：2000-08-16

Applicant: Mark Henry Norman ,  Clarence R. Hurt ,  Ning Chen ,  Christopher H. Fotsch ,  Nianhe Han ,  Tracy J. Jenkins ,  Longbin Liu ,  Ofir A. Moreno

Inventor： Mark Henry Norman ,  Clarence R. Hurt ,  Ning Chen ,  Christopher H. Fotsch ,  Nianhe Han ,  Tracy J. Jenkins ,  Longbin Liu ,  Ofir A. Moreno

IPC: A61K3144

CPC classification number: C07D491/04 ,  A61K31/437 ,  A61K31/519 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: There are provided compounds, compositions and methods of use thereof in the modulation of feeding behavior, obesity, diabetes, cancer (tumor), inflammatory disorders, depression, stress related disorders, Alzheimer's disease and other disease conditions.

Abstract translation: 提供了在调节进食行为，肥胖症，糖尿病，癌症（肿瘤），炎症性疾病，抑郁症，应激相关疾病，阿尔茨海默氏病和其他疾病状况中使用的化合物，组合物和方法。

公开(公告)号：US08686011B2

公开(公告)日：2014-04-01

申请号：US13233699

申请日：2011-09-15

Applicant: Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric A. Bercot ,  Christopher H. Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall W. Hungate ,  Chester Chenguang Yuan ,  Christopher Tegley ,  David J. St. Jean, Jr. ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael D. Bartberger ,  George A. Moniz ,  Matthew J. Frizzle

Inventor： Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric A. Bercot ,  Christopher H. Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall W. Hungate ,  Chester Chenguang Yuan ,  Christopher Tegley ,  David J. St. Jean, Jr. ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael D. Bartberger ,  George A. Moniz ,  Matthew J. Frizzle

IPC: A61K31/427 ,  C07D277/34 ,  C07D277/38 ,  C07D277/42

CPC classification number: C07D277/54 ,  C07D263/34 ,  C07D275/03 ,  C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10

Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Abstract translation: 本发明涉及具有式（I），（II），（III）或（IV）的化合物：其中R1，R2，R3，R4，R5，R6，R7，X和Z如本文所定义， 涉及包含该化合物的药物组合物，以及该化合物用于治疗与人类11-羟基类固醇脱氢酶1型酶相关的病症的用途和用于制备作用于人类11- 羟类固醇脱氢酶1型酶。

公开(公告)号：US20120302534A1

公开(公告)日：2012-11-29

申请号：US13577452

申请日：2011-02-09

Applicant: Daxin Gao ,  Nianhe Han ,  Zhimin Jin ,  Fangxian Ning ,  Jun Tang ,  Yongyong Wu ,  Heping Yang

Inventor： Daxin Gao ,  Nianhe Han ,  Zhimin Jin ,  Fangxian Ning ,  Jun Tang ,  Yongyong Wu ,  Heping Yang

IPC: A61K31/568 ,  A61P31/18 ,  A61K31/58 ,  C07J53/00

CPC classification number: A61K31/50 ,  A61K31/56 ,  C07C225/14 ,  C07C233/76 ,  C07C235/78 ,  C07C275/30 ,  C07C311/04 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/52 ,  C07D205/04 ,  C07D213/40 ,  C07D231/12 ,  C07D295/185 ,  C07D295/26 ,  C07D333/20

Abstract: The present invention relates to a compound characterized by the following Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X, and Y are as described herein. Compounds of the present invention are useful for the treatment of HIV-1.

Abstract translation: 本发明涉及以下式I表征的化合物或其药学上可接受的盐，其中R 1，R 2，R 3，X和Y如本文所述。 本发明的化合物可用于治疗HIV-1。

公开(公告)号：US08084479B2

公开(公告)日：2011-12-27

申请号：US12378195

申请日：2009-02-11

Applicant: Qingping Zeng ,  John G. Allen ,  Matthew P. Bourbeau ,  Celia Dominguez ,  Christopher H. Fotsch ,  Nianhe Han ,  Fang-Tsao Hong ,  Xin Huang ,  Matthew R. Lee ,  Aiwen Li ,  Qingyian Liu ,  James T. Rider ,  Seifu Tadesse ,  Andrew S. Tasker ,  Vellarkad N. Viswanadhan ,  Xianghong Wang ,  Kurt E. Weiler ,  George E. Wohlhieter ,  Guomin Yao ,  Chester Chenguang Yuan

Inventor： Qingping Zeng ,  John G. Allen ,  Matthew P. Bourbeau ,  Celia Dominguez ,  Christopher H. Fotsch ,  Nianhe Han ,  Fang-Tsao Hong ,  Xin Huang ,  Matthew R. Lee ,  Aiwen Li ,  Qingyian Liu ,  James T. Rider ,  Seifu Tadesse ,  Andrew S. Tasker ,  Vellarkad N. Viswanadhan ,  Xianghong Wang ,  Kurt E. Weiler ,  George E. Wohlhieter ,  Guomin Yao ,  Chester Chenguang Yuan

IPC: A01N43/38 ,  A01N43/78 ,  A61K31/405 ,  A61K31/425 ,  C07D277/00

CPC classification number: C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

Abstract: The invention relates to methods of using thiazole compounds of Formula I and Formula II and compositions thereof for treating diseases mediated by protein kinase B (PKB) such as cancer and other proliferative disorders where the variables have the definitions provided herein.

Abstract translation: 本发明涉及使用式I和式II的噻唑化合物及其组合物用于治疗由蛋白激酶B（PKB）介导的疾病，例如癌症和其它增殖性疾病，其中变量具有本文提供的定义。

公开(公告)号：US07662811B2

公开(公告)日：2010-02-16

申请号：US11182216

申请日：2005-07-15

Applicant: Benny C. Askew, Jr. ,  Toshihiro Aya ,  Kaustav Biswas ,  Guolin Cai ,  Jian J. Chen ,  Nianhe Han ,  Qingyian Liu ,  Thomas Nguyen ,  Nobuko Nishimura ,  Rana Nomak ,  Tanya Peterkin ,  Wenyuan Qian ,  Kevin Yang ,  Chester Chenguang Yuan ,  Jiawang Zhu ,  Derin C. D'Amico ,  Jason B. Human ,  Qi Huang

Inventor： Benny C. Askew, Jr. ,  Toshihiro Aya ,  Kaustav Biswas ,  Guolin Cai ,  Jian J. Chen ,  Nianhe Han ,  Qingyian Liu ,  Thomas Nguyen ,  Nobuko Nishimura ,  Rana Nomak ,  Tanya Peterkin ,  Wenyuan Qian ,  Kevin Yang ,  Chester Chenguang Yuan ,  Jiawang Zhu ,  Derin C. D'Amico ,  Jason B. Human ,  Qi Huang

IPC: A01N43/00 ,  A61K31/00 ,  A61K31/55 ,  A61K31/4965 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

CPC classification number: C07D221/10 ,  C07D221/08 ,  C07D239/74 ,  C07D241/08 ,  C07D243/08 ,  C07D249/08 ,  C07D295/135 ,  C07D311/96 ,  C07D335/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D491/04

Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于治疗疼痛和疾病如炎症介导的疾病是有效的。 本发明包括新的化合物，类似物，前药和其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及疼痛，炎症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US07393852B2

公开(公告)日：2008-07-01

申请号：US10874086

申请日：2004-06-21

Applicant: Jian J. Chen ,  Ben C. Askew ,  Kaustav Biswas ,  Jennifer N. Chau ,  Derin C. D'Amico ,  Scott Harried ,  Thomas Nguyen ,  Wenyuan Qian ,  Jiawang Zhu ,  Christopher H. Fotsch ,  Aiwen Li ,  Qingyian Liu ,  Nobuku Nishimura ,  Tanya Peterkin ,  Babak Riahi ,  Chester Chenguang Yuan ,  Nianhe Han ,  Rana Nomak ,  Kevin Yang

Inventor： Jian J. Chen ,  Ben C. Askew ,  Kaustav Biswas ,  Jennifer N. Chau ,  Derin C. D'Amico ,  Scott Harried ,  Thomas Nguyen ,  Wenyuan Qian ,  Jiawang Zhu ,  Christopher H. Fotsch ,  Aiwen Li ,  Qingyian Liu ,  Nobuku Nishimura ,  Tanya Peterkin ,  Babak Riahi ,  Chester Chenguang Yuan ,  Nianhe Han ,  Rana Nomak ,  Kevin Yang

IPC: A61K31/54 ,  A61K31/4965 ,  C07D241/04 ,  C07D265/30 ,  C07D279/12

CPC classification number: C07D241/08 ,  C07D243/08 ,  C07D245/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14

Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于治疗疼痛和疾病如炎症介导的疾病是有效的。 本发明包括新的化合物，类似物，前药和其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及疼痛，炎症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US07253196B2

公开(公告)日：2007-08-07

申请号：US11135662

申请日：2005-05-24

Applicant: Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric A. Bercot ,  Christopher H. Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall W. Hungate ,  Chester Chenguang Yuan ,  Christopher Tegley ,  David J. St. Jean, Jr. ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael D. Bartberger ,  George A. Moniz ,  Matthew J. Frizzle

Inventor： Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric A. Bercot ,  Christopher H. Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall W. Hungate ,  Chester Chenguang Yuan ,  Christopher Tegley ,  David J. St. Jean, Jr. ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael D. Bartberger ,  George A. Moniz ,  Matthew J. Frizzle

IPC: A61K31/426 ,  C07D279/06

CPC classification number: C07D417/06 ,  C07D263/34 ,  C07D263/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/54 ,  C07D277/60 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  C07F7/1804

Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Abstract translation: 本发明涉及具有式（I），（II），（III）或（IV）的化合物：其中R 1，R 2，R 2， 3，R 4，R 5，R 6，R 7，X和Z分别为 以及包含该化合物的药物组合物的使用方法，以及该化合物用于治疗与人类11-β-羟基类固醇脱氢酶1型酶相关的病症和用于制备作用于人的药物的方法 11-β-羟基类固醇脱氢酶1型酶。