公开(公告)号：US20060211682A1

公开(公告)日：2006-09-21

申请号：US10566235

申请日：2004-07-27

申请人： Gui-Bai Liang ,  Tesfaye Biftu ,  Danqing Feng ,  Ann Weber

发明人： Gui-Bai Liang ,  Tesfaye Biftu ,  Danqing Feng ,  Ann Weber

IPC分类号： A61K31/551 ,  C07D403/02 ,  C07D243/02

CPC分类号： C07D243/14 ,  C07D401/06 ,  C07D487/04

摘要： The present invention is directed to hexahydrodiazepinone compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DPP-IV抑制剂”）的抑制剂的六氢二氮杂酮化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如 糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US06432980B1

公开(公告)日：2002-08-13

申请号：US09710165

申请日：2000-11-10

申请人： Tesfaye Biftu ,  Danqing D. Feng ,  Gui-Bai Liang ,  Mitree M. Ponpipom ,  Xiaoxia Qian ,  Narindar Girotra ,  Michael H. Fischer ,  Matthew J. Wyvratt

发明人： Tesfaye Biftu ,  Danqing D. Feng ,  Gui-Bai Liang ,  Mitree M. Ponpipom ,  Xiaoxia Qian ,  Narindar Girotra ,  Michael H. Fischer ,  Matthew J. Wyvratt

IPC分类号： A61K314523

CPC分类号： C07D401/14 ,  A61K31/4545 ,  C07D413/14 ,  Y02A50/491

摘要： Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.

摘要翻译： 三取代吡咯是可用于治疗和预防人类和动物中的原生动物疾病的抗原虫剂，包括控制家禽中的球虫病。

公开(公告)号：US07196095B2

公开(公告)日：2007-03-27

申请号：US10477367

申请日：2002-06-21

申请人： Tesfaye Biftu ,  Richard Beresis ,  Richard Berger ,  Steven L. Colletti ,  James B. Doherty ,  Dennis D. Feng ,  Gui-Bai Liang ,  Dennis M. Schmatz ,  Xiaoxia Qian ,  David A. Claremon ,  Nigel J. Liverton ,  Charles J. McIntyre ,  Ernest W. Kovacs

发明人： Tesfaye Biftu ,  Richard Beresis ,  Richard Berger ,  Steven L. Colletti ,  James B. Doherty ,  Dennis D. Feng ,  Gui-Bai Liang ,  Dennis M. Schmatz ,  Xiaoxia Qian ,  David A. Claremon ,  Nigel J. Liverton ,  Charles J. McIntyre ,  Ernest W. Kovacs

IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D417/14 ,  A61K31/506 ,  A61P19/02

CPC分类号： C07D403/04 ,  A23K20/10 ,  A23K20/111 ,  A61K31/429 ,  A61K31/4355 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  C07D453/02 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D513/04 ,  A61K2300/00

摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are useful in the treatment of cytokine mediated diseases such as arthritis and in the treatment and/or prevention of protozoal diseases such as coccidiosis

摘要翻译： 式（I）化合物及其药学上可接受的盐可用于治疗细胞因子介导的疾病如关节炎和治疗和/或预防原虫感染疾病如球虫病

公开(公告)号：US6034106A

公开(公告)日：2000-03-07

申请号：US868556

申请日：1997-06-04

申请人： Tesfaye Biftu ,  Michael H. Fisher ,  Danqing Dennis Feng ,  Chan-Hwa Kuo ,  Gui-Bai Liang ,  Elizabeth M. Naylor ,  Ann E. Weber

发明人： Tesfaye Biftu ,  Michael H. Fisher ,  Danqing Dennis Feng ,  Chan-Hwa Kuo ,  Gui-Bai Liang ,  Elizabeth M. Naylor ,  Ann E. Weber

IPC分类号： C07D413/12 ,  C07D413/10 ,  A61K31/44

CPC分类号： C07D413/12

摘要： Oxadiazole substituted benzenesulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

摘要翻译： 恶二唑取代的苯磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂，因此化合物能够增加细胞中的脂肪分解和能量消耗。 因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。 通过将氨基烷基苯基磺酰胺与适当取代的环氧化物偶合来制备化合物。 还公开了用于治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或增加肠蠕动的组合物和方法。

公开(公告)号：US07259160B2

公开(公告)日：2007-08-21

申请号：US10566235

申请日：2004-07-27

申请人： Gui-Bai Liang ,  Tesfaye Biftu ,  Danqing Dennis Feng ,  Ann E. Weber

发明人： Gui-Bai Liang ,  Tesfaye Biftu ,  Danqing Dennis Feng ,  Ann E. Weber

IPC分类号： C07D243/08 ,  A61K31/551 ,  A61P3/10

CPC分类号： C07D243/14 ,  C07D401/06 ,  C07D487/04

摘要： The present invention is directed to hexahydrodiazepinone compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DPP-IV抑制剂”）的抑制剂的六氢二氮杂酮化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如 糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US07101871B2

公开(公告)日：2006-09-05

申请号：US10501059

申请日：2003-10-14

申请人： Tesfaye Biftu ,  Gui-Bai Liang ,  Xiaoxia Qian ,  Ann E. Weber ,  Danqing Dennis Feng

发明人： Tesfaye Biftu ,  Gui-Bai Liang ,  Xiaoxia Qian ,  Ann E. Weber ,  Danqing Dennis Feng

IPC分类号： C07D243/08 ,  A61K31/551 ,  A61P3/10

CPC分类号： C07D243/08 ,  C07D401/06 ,  C07D403/06 ,  C07K5/06191

摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

公开(公告)号：US06291480B1

公开(公告)日：2001-09-18

申请号：US09710147

申请日：2000-11-10

申请人： Tesfaye Biftu ,  Danqing Dennis Feng ,  Gui-Bai Liang ,  Mitree M. Ponpipom ,  Xiaoxia Qian ,  Michael H. Fisher ,  Matthew J. Wyvratt

发明人： Tesfaye Biftu ,  Danqing Dennis Feng ,  Gui-Bai Liang ,  Mitree M. Ponpipom ,  Xiaoxia Qian ,  Michael H. Fisher ,  Matthew J. Wyvratt

IPC分类号： C07D40104

CPC分类号： C07D401/14 ,  A23K20/116 ,  A23K50/75 ,  A61K45/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.

摘要翻译： 三取代吡咯是可用于治疗和预防人类和动物中的原生动物疾病的抗原虫剂，包括控制家禽中的球虫病。

公开(公告)号：US20070265332A1

公开(公告)日：2007-11-15

申请号：US11801841

申请日：2007-05-11

申请人： Min Ge ,  Jiafang He ,  Fiona Wai Yu Lau ,  Gui-Bai Liang ,  Songnian Lin ,  Weiguo Liu ,  Shawn P. Walsh ,  Lihu Yang

发明人： Min Ge ,  Jiafang He ,  Fiona Wai Yu Lau ,  Gui-Bai Liang ,  Songnian Lin ,  Weiguo Liu ,  Shawn P. Walsh ,  Lihu Yang

IPC分类号： A61K31/381 ,  A61K31/343 ,  A61K31/192 ,  A61K31/195

CPC分类号： C07D213/643 ,  C07C62/34 ,  C07C62/38 ,  C07C229/50 ,  C07C2603/08 ,  C07D307/93 ,  C07D311/94 ,  C07D333/78 ,  C07D405/04 ,  C07D407/12 ,  C07D413/12 ,  C07D417/12

摘要： Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

摘要翻译： 与环双环稠合的环状羧酸或羧酸衍生物（如酰胺）的三环化合物（包括其药学上可接受的盐和前体药物）是G-蛋白偶联受体40（GPR40）的激动剂，可用作治疗性化合物，特别是在 2型糖尿病的治疗，以及经常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合或糖尿病性血脂异常，高脂血症，高胆固醇血症和高甘油三酯血症。

公开(公告)号：US20210023079A1

公开(公告)日：2021-01-28

申请号：US17062291

申请日：2020-10-02

申请人： Gui-Bai Liang

发明人： Gui-Bai Liang

IPC分类号： A61K31/496 ,  A61P11/00 ,  A61K9/00 ,  A61K31/4418

摘要： Provided is a pharmaceutical composition comprising an effective amount of itraconazole, and a pharmaceutically acceptable excipient. The use of the pharmaceutical composition for treatment of idiopathic pulmonary fibrosis is also provided.

公开(公告)号：US08759539B2

公开(公告)日：2014-06-24

申请号：US13125088

申请日：2009-11-11

申请人： Jiafang He ,  John Bawiec ,  Weiguo Liu ,  Gui-Bai Liang ,  Lihu Yang

发明人： Jiafang He ,  John Bawiec ,  Weiguo Liu ,  Gui-Bai Liang ,  Lihu Yang

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D209/52 ,  C07D413/12 ,  C07D417/12 ,  A61K31/403 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/423

CPC分类号： C07D401/12 ,  C07D209/52 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.

摘要翻译： 本文描述的是取代的双环胺。 特别地，本文描述的是作为SSTR5的拮抗剂有效的取代的双环胺，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍，肥胖，动脉粥样硬化，代谢 综合征，抑郁症和焦虑症。