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1. 发明申请

US20070043014A1 3,5-Aryl, heteroaryl or cycloalkyl substituted-1,2,4-oxadiazoles as s1p receptor agonists 审中-公开
标题翻译： 3,5-芳基，杂芳基或环烷基取代的-1,2,4-恶二唑作为s1p受体激动剂
公开(公告)号：US20070043014A1
公开(公告)日：2007-02-22
申请号：US10571334
申请日：2004-09-27
申请人： George Doherty , Jeffrey Hale , Irene Legiec , Christopher Lynch , Leslie Toth
发明人： George Doherty , Jeffrey Hale , Irene Legiec , Christopher Lynch , Leslie Toth
IPC分类号： A61K31/506 , A61K31/501 , A61K31/497 , A61K31/4709 , A61K31/4745 , A61K31/4439 , A61K31/4245 , C07D413/04
CPC分类号： C07D413/04 , C07D271/06
摘要： The present invention encompasses compounds of Formula I: (I) as well as the pharmaceutically acceptable salts thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括式I化合物：（I）及其药学上可接受的盐。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

2. 发明申请

US20050070506A1 Selective s1p1/edg1 receptor agonists 审中-公开
标题翻译：选择性s1p1 / edg1受体激动剂
公开(公告)号：US20050070506A1
公开(公告)日：2005-03-31
申请号：US10501176
申请日：2003-01-14
申请人： George Doherty , Michael Forrest , Richard Hajdu , Jeffrey Hale , Li Zhen , Susanne Mandala , Sander Mills , Hugh Rosen , Edward Scolnick
发明人： George Doherty , Michael Forrest , Richard Hajdu , Jeffrey Hale , Li Zhen , Susanne Mandala , Sander Mills , Hugh Rosen , Edward Scolnick
IPC分类号： A61K31/00 , A61K31/66 , G01N33/566
CPC分类号： A61K31/66 , A61K31/00 , G01N33/566 , G01N2500/04
摘要： The present invention encompasses a method of treating an immunoregulatory abnormality in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said immunoregulatory abnormality, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor, said compound administered in an amount effective for treating said immunoregulatory abnormality. Pharmaceutical compositions are included. The invention also encompasses a method of identifying candidate compounds that are agonists of the S1P1/Edg1 receptor and which possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor. The invention further encompasses a method of treating a respiratory disease or condition in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said respiratory disease or condition, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor.
摘要翻译：本发明包括在需要这种治疗的哺乳动物患者中治疗免疫调节异常的方法，包括以有效治疗所述免疫调节异常的量向所述患者施用作为S1P1 / Edg1受体激动剂的化合物，其中所述化合物对S1P1 / Edg1受体具有S1PR3 / Edg1受体的选择性，所述化合物以有效治疗所述免疫调节异常的量给药。包括药物组合物。本发明还包括鉴定作为S1P1 / Edg1受体的激动剂的候选化合物的方法，并且其具有S1P1 / Edg1受体超过S1PR3 / Edg3受体的选择性。本发明还包括治疗需要这种治疗的哺乳动物患者的呼吸系统疾病或病症的方法，包括向所述患者施用有效治疗所述呼吸系统疾病或病症的S1P1 / Edg1受体激动剂的化合物其中所述化合物对S1P1 / Edg1受体具有超过S1PR3 / Edg3受体的选择性。

3. 发明申请

US20050107345A1 Aminoalkylphosphonates and related compounds as edg receptor agonists 审中-公开
标题翻译：氨基烷基膦酸盐和相关化合物作为edg受体激动剂
公开(公告)号：US20050107345A1
公开(公告)日：2005-05-19
申请号：US10505268
申请日：2003-02-25
申请人： George Doherty , Jeffrey Hale
发明人： George Doherty , Jeffrey Hale
IPC分类号： A61K31/18 , A61K31/197 , A61K31/41 , A61K31/4164 , A61K31/4192 , A61K31/4196 , A61K31/661 , A61K31/662 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/04 , A61P3/10 , A61P5/14 , A61P7/06 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P17/10 , A61P17/14 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/06 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/14 , A61P31/18 , A61P31/20 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , C07C229/34 , C07C233/11 , C07C309/24 , C07C311/51 , C07D233/84 , C07D249/04 , C07D249/12 , C07D257/04 , C07D257/06 , C07F9/09 , C07F9/38 , A61K31/433 , A61K31/20 , A61K31/42 , A61K31/4245
CPC分类号： A61K9/4825 , A61K31/66 , C07C229/34 , C07C309/24 , C07C311/51 , C07D233/84 , C07D249/04 , C07D249/12 , C07D257/04 , C07D257/06 , C07F9/094 , C07F9/3808 , C07F9/3826 , C07F9/3882
摘要： The present invention encompasses compounds of formula (II); as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括式（II）的化合物; 以及其药学上可接受的盐和水合物。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

4. 发明申请

US20050020837A1 N-(benzyl)aminoalkylcarboxylates, phosphinates, phosphonates and tetrazoles as edg receptor agonists 失效
标题翻译： N-（苄基）氨基烷基羧酸盐，次膦酸盐，膦酸盐和四唑作为EDG受体激动剂
公开(公告)号：US20050020837A1
公开(公告)日：2005-01-27
申请号：US10500811
申请日：2003-01-14
申请人： George Doherty , Zhen Li , Jeffrey Hale , Sander Mills
发明人： George Doherty , Zhen Li , Jeffrey Hale , Sander Mills
IPC分类号： A61K31/197 , A61K31/41 , A61K31/4245 , A61K31/662 , A61P1/04 , A61P1/18 , A61P3/10 , A61P11/06 , A61P17/06 , A61P21/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , C07C229/10 , C07C229/14 , C07C229/20 , C07C229/22 , C07D257/04 , C07D333/16 , C07D413/04 , C07F9/30 , C07F9/38 , C07F9/48 , C07F9/59 , C07F9/6553 , C07F9/6558 , C07F9/28 , C07D257/02 , C07C229/34
CPC分类号： C07D413/04 , C07C229/14 , C07C229/20 , C07C229/22 , C07D333/16 , C07F9/301 , C07F9/307 , C07F9/3808 , C07F9/4816 , C07F9/59 , C07F9/655345 , C07F9/65586
摘要： The present invention encompasses compounds of Formula (I) as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括式（I）的化合物及其药学上可接受的盐和水合物。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

5. 发明申请

US20070224263A1 Aminoalkylphosphonates and related compounds as Edg receptor agonists 审中-公开
标题翻译：氨基烷基膦酸盐和相关化合物作为Edg受体激动剂
公开(公告)号：US20070224263A1
公开(公告)日：2007-09-27
申请号：US11803060
申请日：2007-05-11
申请人： George Doherty , Jeffrey Hale
发明人： George Doherty , Jeffrey Hale
IPC分类号： A61K9/64 , A61K31/66 , C07C53/00 , C07F9/02 , C07D285/10 , A61K9/48
CPC分类号： A61K9/4825 , A61K31/66 , C07C229/34 , C07C309/24 , C07C311/51 , C07D233/84 , C07D249/04 , C07D249/12 , C07D257/04 , C07D257/06 , C07F9/094 , C07F9/3808 , C07F9/3826 , C07F9/3882
摘要： The present invention encompasses compounds of Formula II: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括式II的化合物及其药学上可接受的盐和水合物。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

6. 发明申请

US20060161005A1 1-(Amino)indanes and (1,2-dihydro-3-amino)-benzofurans, benzothiophenes and indoles as edg receptor agonists 失效
标题翻译： 1-（氨基）茚满和（1,2-二氢-3-氨基） - 苯并呋喃，苯并噻吩和吲哚作为EDG受体激动剂
公开(公告)号：US20060161005A1
公开(公告)日：2006-07-20
申请号：US10536730
申请日：2003-12-16
申请人： George Doherty , Jeffrey Hale , Sander Mills
发明人： George Doherty , Jeffrey Hale , Sander Mills
IPC分类号： C07D417/02 , C07D413/02 , C07D409/02 , C07D405/02
CPC分类号： C07D205/04 , C07D333/16 , C07D409/10 , C07D409/12 , C07D413/10 , C07D413/14
摘要： The present invention encompasses compounds of Formula (I): as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括式（I）的化合物：及其药学上可接受的盐和水合物。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

7. 发明申请

US20050033055A1 Edg receptor agonists 失效
标题翻译： Edg受体激动剂
公开(公告)号：US20050033055A1
公开(公告)日：2005-02-10
申请号：US10500895
申请日：2003-01-15
申请人： Robert Bugianesi , George Doherty , Amy Gentry , Jeffrey Hale , Christopher Lynch , Sander Mills , William Neway III
发明人： Robert Bugianesi , George Doherty , Amy Gentry , Jeffrey Hale , Christopher Lynch , Sander Mills , William Neway III
IPC分类号： A61K31/397 , A61K31/40 , A61K31/4025 , A61K31/41 , A61K31/4155 , A61K31/4245 , A61K31/675 , A61P1/02 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/14 , A61P19/02 , A61P19/10 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/06 , A61P27/02 , A61P27/12 , A61P29/00 , A61P31/14 , A61P31/20 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/06 , A61P37/08 , C07D205/04 , C07D207/16 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/14 , C07F9/572 , C07F9/6558 , C07F9/547 , C07D207/08 , C07D211/34
CPC分类号： C07D403/04 , C07D205/04 , C07D207/16 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/14 , C07F9/572 , C07F9/65586
摘要： The present invention encompasses compounds of Formula 1: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括式1的化合物及其药学上可接受的盐和水合物。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

8. 发明申请

US20060252741A1 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists 审中-公开
标题翻译： 3-（2-氨基-1-氮杂环丙基）-5-芳基-1,2,4-恶二唑作为s1p受体激动剂
公开(公告)号：US20060252741A1
公开(公告)日：2006-11-09
申请号：US10554665
申请日：2004-05-12
申请人： Vincent Colandrea , George Doherty , Jeffrey Hale , Christopher Lynch , Sander Mills , William Neway III , Leslie Toth
发明人： Vincent Colandrea , George Doherty , Jeffrey Hale , Christopher Lynch , Sander Mills , William Neway III , Leslie Toth
IPC分类号： A61K31/4439 , C07D413/04 , C07D413/14
CPC分类号： C07D413/04 , C07D271/06 , C07D413/14
摘要： The present invention encompasses compounds of Formula (I): as well as the pharmaceutically acceptable salts thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括式（I）的化合物及其药学上可接受的盐。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

9. 发明申请

US20060089334A1 Aminoalkylphosphonates and related compounds as edg receptor agonists 失效
标题翻译：氨基烷基膦酸盐和相关化合物作为edg受体激动剂
公开(公告)号：US20060089334A1
公开(公告)日：2006-04-27
申请号：US10505257
申请日：2003-02-27
申请人： Richard Budhu , George Doherty , Jeffrey Hale , Christopher Lynch , Sander Mills , William Neway
发明人： Richard Budhu , George Doherty , Jeffrey Hale , Christopher Lynch , Sander Mills , William Neway
IPC分类号： A61K31/433 , A61K31/426 , A61K31/4245 , A61K31/421 , A61K31/4172 , A61K31/4152
CPC分类号： C07D257/04 , C07C229/34 , C07C309/24 , C07C311/51 , C07D233/84 , C07D249/04 , C07D249/12 , C07D257/06 , C07F9/094 , C07F9/3808 , C07F9/3826 , C07F9/3882
摘要： The present invention encompasses compounds or Formula (I): as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
摘要翻译：本发明包括化合物或式（I）：及其药学上可接受的盐和水合物。该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。包括药物组合物和使用方法。

10. 发明申请

US20070123505A1 Heterocycle-substituted 3-alkyl azetidine derivatives 失效
标题翻译：杂环取代的3-烷基氮杂环丁烷衍生物
公开(公告)号：US20070123505A1
公开(公告)日：2007-05-31
申请号：US11602577
申请日：2006-11-21
申请人： Robert Baker , Jeffrey Hale , Shouwu Miao , Kathleen Rupprecht
发明人： Robert Baker , Jeffrey Hale , Shouwu Miao , Kathleen Rupprecht
IPC分类号： A61K31/506 , A61K31/501 , A61K31/497 , A61K31/4439 , A61K31/427 , A61K31/4178 , C07D403/02 , A61K31/397
CPC分类号： C07D257/04 , C07D271/06 , C07D271/07 , C07D271/10 , C07D271/113 , C07D403/10 , C07D413/10 , C07D417/04 , C07D417/06 , C07D417/14
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), and non-alcoholic steatohepatitis (NASH).
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，阿尔茨海默病，偏头痛，神经病，包括多发性硬化症和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症的中枢作用药物脑血管意外，头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻，肝硬化，非酒精性脂肪性肝病（NAFLD ）和非酒精性脂肪性肝炎（NASH）。

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