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1. 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。

2. 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。

3. 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。

4. 发明申请

US20050245575A1 1-((5-aryl-1,2,4-oxadiazol-3-yl) benzyl)azetidine-3-carboxylates and 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl) pyrrolidine-3-carboxylates as edg receptor agonists 失效
标题翻译： 1 - （（5-芳基-1,2,4-恶二唑-3-基）苄基）氮杂环丁烷-3-羧酸酯和1 - （（5-芳基-1,2,4-恶二唑-3-基）苄基）吡咯烷-3-羧酸盐作为edg受体激动剂
公开(公告)号：US20050245575A1
公开(公告)日：2005-11-03
申请号：US10515192
申请日：2003-06-16
申请人： Weirong Chen , Jeffrey Hale , Zhen Li , Christopher Lynch , Sander Mills , William Neway
发明人： Weirong Chen , Jeffrey Hale , Zhen Li , Christopher Lynch , Sander Mills , William Neway
IPC分类号： A61K31/4245 , A61K31/454 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/06 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P17/14 , A61P19/02 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/06 , A61P25/28 , A61P27/02 , A61P27/12 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D413/02 , C07D413/10 , C07D413/14
CPC分类号： C07D413/10 , A61K31/4245 , 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。

5. 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。

6. 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。

7. 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。

8. 发明授权

US5877191A Phenyl spiroethercycloalkyl tachykinin receptor antagonists 失效
标题翻译：苯基螺醚醚环烷基速激肽受体拮抗剂
公开(公告)号：US5877191A
公开(公告)日：1999-03-02
申请号：US955898
申请日：1997-10-22
申请人： Charles G. Caldwell , Yuan-Ching Chiang , Conrad Dorn , Paul Finke , Jeffrey Hale , Malcolm Maccoss , Sander Mills , Albert Robichaud
发明人： Charles G. Caldwell , Yuan-Ching Chiang , Conrad Dorn , Paul Finke , Jeffrey Hale , Malcolm Maccoss , Sander Mills , Albert Robichaud
IPC分类号： C07D307/94 , C07D405/10 , C07D405/12 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12 , A61K31/36 , C07D285/04 , C07D311/96
CPC分类号： C07D307/94 , C07D405/10 , C07D405/12 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
摘要翻译：本发明涉及由结构式I表示的某些新化合物：其中R3，R6，R7，R8，R11，R12，R13，m，n和虚线在本文中定义。本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。本发明化合物是速激肽受体拮抗剂，可用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐。

9. 发明授权

US5747485A Substituted azetidiones as anti-inflammatory and antidegenerative agents 失效
标题翻译：取代的氮杂环丁酮作为抗炎剂和抗再生剂
公开(公告)号：US5747485A
公开(公告)日：1998-05-05
申请号：US848076
申请日：1997-06-05
申请人： James Doherty , Conrad Dorn , Philippe Durette , Paul Finke , Malcolm Maccoss , Sander Mills , Shrenik Shah , Soumya Sahoo , William Hagmann , Jeffrey Hale , Thomas Lanza
发明人： James Doherty , Conrad Dorn , Philippe Durette , Paul Finke , Malcolm Maccoss , Sander Mills , Shrenik Shah , Soumya Sahoo , William Hagmann , Jeffrey Hale , Thomas Lanza
IPC分类号： A61K31/397 , A61K31/496 , A61K31/5377 , A61K31/395
CPC分类号： A61K31/496 , A61K31/397 , A61K31/5377
摘要： Substituted azetidinones are herein disclosed for use in the treatment of various elastase-mediated diseases.
摘要翻译：本文公开了取代的氮杂环丁酮，用于治疗各种弹性蛋白酶介导的疾病。

10. 发明申请

US20070179158A1 2,6-Disubstituted piperiddines as modulators 失效
标题翻译： 2,6-二取代的哌啶作为调节剂
公开(公告)号：US20070179158A1
公开(公告)日：2007-08-02
申请号：US10586765
申请日：2005-01-14
申请人： Lihu Yang , Sander Mills , Changyou Zhou , Stephen Goble , Alexander Pasternak
发明人： Lihu Yang , Sander Mills , Changyou Zhou , Stephen Goble , Alexander Pasternak
IPC分类号： A61K31/506 , A61K31/4745 , A61K31/46 , C07D471/02
CPC分类号： C07D519/00 , C07D451/02 , C07D451/04 , C07D451/06
摘要： The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R18, R19, R20, R21 and R22 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. 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 chemokine receptors are involved.
摘要翻译：本发明还涉及式（I）的化合物：其中R 1，R 2，R 3，R 4， R 5，R 6，R 7，R 8，R 9，R 9， R 10，R 16，R 17，R 18，R 19，R 16， R 20，R 21，R 22和R 22如本文所定义），其是趋化因子受体活性的调节剂，并且可用于预防或治疗某些炎性和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及自身免疫病态如类风湿性关节炎和动脉粥样硬化。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趋化因子受体的疾病中的用途。

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