公开(公告)号：US06900223B2

公开(公告)日：2005-05-31

申请号：US10629227

申请日：2003-07-28

申请人： Neal Jeffrey Green ,  Steve Yikkai Tam ,  Jason Shaoyun Xiang ,  Audrey Molina Davies ,  Lihren Chen ,  Gary Paul Stack

发明人： Neal Jeffrey Green ,  Steve Yikkai Tam ,  Jason Shaoyun Xiang ,  Audrey Molina Davies ,  Lihren Chen ,  Gary Paul Stack

IPC分类号： C07D471/14 ,  A61K31/437 ,  A61P37/00

CPC分类号： C07D471/14

摘要： The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection, autoimmune disease or graft vs. host disease.

摘要翻译： 本发明提供式I化合物及其用于免疫治疗移植排斥反应，自身免疫性疾病或移植物抗宿主病的用途。

公开(公告)号：US20090042895A1

公开(公告)日：2009-02-12

申请号：US12254118

申请日：2008-10-20

申请人： Michael Byron Webb ,  Gary Paul Stack ,  Magda Asselin ,  Deborah A. Evrard

发明人： Michael Byron Webb ,  Gary Paul Stack ,  Magda Asselin ,  Deborah A. Evrard

IPC分类号： A61K31/4985 ,  C07D491/056 ,  A61K31/436 ,  C07D498/04 ,  A61K31/454 ,  A61P25/24

CPC分类号： C07D491/04

摘要： Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

摘要翻译： 式的化合物可用于治疗抑郁症（包括但不限于严重抑郁症，儿童抑郁症和抑郁症），焦虑症，惊恐障碍，创伤后应激障碍，经前期焦虑障碍（也称为月经前综合征 ），注意力缺陷障碍（伴有和不伴有多动症），强迫症，社会焦虑症，广泛性焦虑症，肥胖症，进食障碍如神经性厌食症和神经性贪食症，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍及相关疾病。

公开(公告)号：US06911445B2

公开(公告)日：2005-06-28

申请号：US10659174

申请日：2003-09-10

申请人： Deborah Ann Evrard ,  Gary Paul Stack ,  Uresh Shantilal Shah

发明人： Deborah Ann Evrard ,  Gary Paul Stack ,  Uresh Shantilal Shah

IPC分类号： A61K31/4741 ,  A61P25/22 ,  A61P25/24 ,  C07D491/04 ,  C07D498/04 ,  A61K31/495 ,  C07D235/02 ,  C07D241/46 ,  C07D491/08

CPC分类号： C07D491/04

摘要： Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

摘要翻译： 下式的化合物可用于治疗抑郁症（包括但不限于重度抑郁症，儿童抑郁症和心境恶劣），焦虑症，惊恐障碍，创伤后应激障碍，经前焦虑症（也称为月经前综合征 ），注意力缺陷障碍（伴有和不伴有多动症），强迫症，社会焦虑症，广泛性焦虑症，肥胖症，进食障碍，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍和相关疾病。

公开(公告)号：US06800637B2

公开(公告)日：2004-10-05

申请号：US10659238

申请日：2003-09-10

申请人： Gary Paul Stack ,  Michael Byron Webb ,  Deborah Ann Evrard ,  Dahul Zhou

发明人： Gary Paul Stack ,  Michael Byron Webb ,  Deborah Ann Evrard ,  Dahul Zhou

IPC分类号： C07D49102

CPC分类号： C07D491/04

摘要： Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

摘要翻译： 下式的化合物可用于治疗抑郁症（包括但不限于重度抑郁症，儿童抑郁症和心境恶劣），焦虑症，惊恐障碍，创伤后应激障碍，经前焦虑症（也称为月经前综合征 ），注意力缺陷障碍（伴有和不伴有多动症），强迫症，社会焦虑症，广泛性焦虑症，肥胖症，进食障碍如神经性厌食症，神经性贪食症，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍和相关疾病。

公开(公告)号：US07470799B2

公开(公告)日：2008-12-30

申请号：US11408653

申请日：2006-04-21

申请人： Gary Paul Stack ,  Jonathan Laird Gross

发明人： Gary Paul Stack ,  Jonathan Laird Gross

IPC分类号： C07D307/00 ,  A61K31/34

CPC分类号： C07D307/81 ,  C12P17/04 ,  C12P17/14

摘要： Compounds of formula I are provided: wherein each of R1, R2, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of melatoninergic receptors. The compounds, and compositions containing the compounds, can be used to treat melatoninergic disorders.

摘要翻译： 提供了式I化合物：其中R 1，R 2，Y，m，n和Ar各自如本文中的类别和亚类所定义和描述，其为褪黑激素受体的激动剂或部分激动剂。 化合物和含有这些化合物的组合物可用于治疗褪黑激素障碍。

公开(公告)号：US07365095B2

公开(公告)日：2008-04-29

申请号：US11409467

申请日：2006-04-21

申请人： Gavin David Heffernan ,  Gary Paul Stack ,  Jonathan Laird Gross ,  Dahui Zhou ,  Hong Gao

发明人： Gavin David Heffernan ,  Gary Paul Stack ,  Jonathan Laird Gross ,  Dahui Zhou ,  Hong Gao

IPC分类号： A61K31/44 ,  A61K43/40 ,  A01N43/02 ,  A01N43/16 ,  A61N31/335

CPC分类号： C07D311/04 ,  C07D311/20 ,  C07D311/58 ,  C07D313/08 ,  C07D401/04 ,  C07D405/04

摘要： Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.

摘要翻译： 提供式I化合物或其药学上可接受的盐：其中R 1，R 2，R 3，R 4， y，m，n和Ar如上所定义，并且在本文的类别和亚类中描述，它们是脑5-羟色胺受体的2C亚型的激动剂或部分激动剂。 化合物和含有这些化合物的组合物可用于治疗各种中枢神经系统疾病如精神分裂症。

公开(公告)号：US07135479B2

公开(公告)日：2006-11-14

申请号：US10659167

申请日：2003-09-10

申请人： Dahui Zhou ,  Gary Paul Stack

发明人： Dahui Zhou ,  Gary Paul Stack

IPC分类号： A61K31/44 ,  A61K31/445 ,  A61K31/40 ,  A61K31/405 ,  A61K31/335 ,  A61K31/35 ,  C07D261/20 ,  C07D411/00 ,  C07D405/00 ,  C07D409/00 ,  C07D205/00 ,  C07D333/52 ,  C07D319/14 ,  C07D307/78

CPC分类号： C07D491/04

摘要： Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

摘要翻译： 式的化合物可用于治疗抑郁症（包括但不限于严重抑郁症，儿童抑郁症和抑郁症），焦虑症，惊恐障碍，创伤后应激障碍，经前期焦虑障碍（也称为月经前综合征 ），注意力缺陷障碍（伴有和不伴有多动症），强迫症，社会焦虑症，广泛性焦虑症，肥胖症，进食障碍如神经性厌食症和神经性贪食症，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍及相关疾病。

公开(公告)号：US07041697B2

公开(公告)日：2006-05-09

申请号：US10659193

申请日：2003-09-10

申请人： Deborah Ann Evrard ,  Uresh Shantilal Shah ,  Gary Paul Stack

发明人： Deborah Ann Evrard ,  Uresh Shantilal Shah ,  Gary Paul Stack

IPC分类号： A61K31/40 ,  C07D209/10

CPC分类号： C07D405/12

摘要： Compounds of the Formula I: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

公开(公告)号：US06407066B1

公开(公告)日：2002-06-18

申请号：US09489164

申请日：2000-01-21

申请人： Darren B. Dressen ,  Anthony Kreft ,  Dennis Kubrak ,  Charles William Mann ,  Michael A. Pleiss ,  Gary Paul Stack ,  Eugene D. Thorsett

发明人： Darren B. Dressen ,  Anthony Kreft ,  Dennis Kubrak ,  Charles William Mann ,  Michael A. Pleiss ,  Gary Paul Stack ,  Eugene D. Thorsett

IPC分类号： C07K506

CPC分类号： C07K5/06173 ,  A61K38/00 ,  C07K5/06139

摘要： Disclosed are pyroglutamic acid derivatives and related compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

摘要翻译： 披露了结合VLA-4的焦谷氨酸衍生物和相关化合物。 这些化合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。

公开(公告)号：US20100035871A1

公开(公告)日：2010-02-11

申请号：US12446947

申请日：2007-10-24

申请人： Gary Paul Stack ,  Dahui Zhou ,  Nicole Theriault Hatzenbuhler

发明人： Gary Paul Stack ,  Dahui Zhou ,  Nicole Theriault Hatzenbuhler

IPC分类号： A61K31/536 ,  C07D265/36 ,  A61P25/00 ,  A61P3/04

CPC分类号： C07D265/36

摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of Z, X, R1, R2, R3, R4, y, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions thereof, are useful for treating a variety of central nervous system disorders such as schizophrenia.

摘要翻译： 提供了式（I）化合物或其药学上可接受的盐，其中Z，X，R 1，R 2，R 3，R 4，Y，n和Ar各自如本文所定义和描述，其为激动剂 或部分激动剂的2C亚型脑血清素受体。 化合物及其组合物可用于治疗各种中枢神经系统疾病如精神分裂症。