公开(公告)号：US20070161695A1

公开(公告)日：2007-07-12

申请号：US11714352

申请日：2007-03-06

申请人： Jaime Bunda ,  Robert DeVita ,  Jinlong Jiang ,  Sander Mills

发明人： Jaime Bunda ,  Robert DeVita ,  Jinlong Jiang ,  Sander Mills

IPC分类号： A61K31/4035 ,  C07D209/44

CPC分类号： C07D209/44

摘要： The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

公开(公告)号：US20070155731A1

公开(公告)日：2007-07-05

申请号：US10587118

申请日：2005-01-26

申请人： Gabor Butora ,  Deodialsingh Guiadeen ,  Shankaran Kothandaraman ,  Malcolm MacCoss ,  Sander Mills ,  Lihu Yang

发明人： Gabor Butora ,  Deodialsingh Guiadeen ,  Shankaran Kothandaraman ,  Malcolm MacCoss ,  Sander Mills ,  Lihu Yang

IPC分类号： A61K31/549 ,  A61K31/538 ,  A61K31/498 ,  C07D498/04 ,  C07D491/04 ,  C07D487/04

CPC分类号： C07D471/04

摘要： Compounds of Formula I and Formula II (wherein A, E, j, k, m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, X, Y and Z 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： 式I和式II化合物（其中A，E，j，k，m，n，R 1，R 2，R 3， R 4，R 5，R 6，R 7，R 8， R 9，R 10，R 15，R 16，R 17， ，R 18，R 19，R 24，R 25，R 26， R 27，R 28，R 29，R 30，R 31， ，R 32，R 33，R 34，X，Y和Z如本文所定义），其是趋化因子受体活性的调节剂，并且是 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。

公开(公告)号：US20070149529A1

公开(公告)日：2007-06-28

申请号：US10589406

申请日：2005-02-08

申请人： Lihu Yang ,  Alexander Pasternak ,  Sander Mills

发明人： Lihu Yang ,  Alexander Pasternak ,  Sander Mills

IPC分类号： A61K31/53 ,  A61K31/506 ,  A61K31/501 ,  A61K31/497 ,  A61K31/496 ,  A61K31/4545 ,  C07D403/02 ,  C07D401/02

CPC分类号： C07D307/24 ,  C07D207/16 ,  C07D401/04 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04

摘要： Compounds of Formula I and Formula II: (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R33, R34, R35, R36, R37, R38, A, j, k, m, n, X, Y and Z 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： 式I和式II化合物：其中n，R 1，R 2，R 3，R 4，R 5， R 6，R 7，R 8，R 9，R 10，R 9， R 15，R 16，R 17，R 18，R 19， R 24，R 25，R 26，R 27，R 28，R 24， R 29，R 30，R 33，R 34，R 35， R 30，R 37，R 38，A，j，k，m，n，X，Y和Z分别为 可以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，特应性疾病，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及自身免疫病理学 作为类风湿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。

公开(公告)号：US20060178363A1

公开(公告)日：2006-08-10

申请号：US10550111

申请日：2004-03-12

申请人： Stephen Goble ,  Alexander Pasternak ,  Sander Mills ,  Changyou Zhou ,  Lihu Yang

发明人： Stephen Goble ,  Alexander Pasternak ,  Sander Mills ,  Changyou Zhou ,  Lihu Yang

IPC分类号： A61K31/538 ,  C07D491/02 ,  C07D413/02

CPC分类号： C07D413/12 ,  C07D405/12 ,  C07D417/12 ,  C07D471/04

摘要： The present invention is directed to compounds of the formula (1) Wherein A, B, D, X, Y, n, R1, R3, R4, R5, R15, R16, R17, R18 and the dashed line are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

摘要翻译： 本发明涉及式（1）的化合物，其中A，B，D，X，Y，n，R 1，R 3， R 4，R 5，R 15，R 16，R 17，R 16， 18和虚线如本文所定义，其可用作趋化因子受体活性的调节剂。 特别地，这些化合物可用作趋化因子受体CCR-2的调节剂。

公开(公告)号：US5929094A

公开(公告)日：1999-07-27

申请号：US956181

申请日：1997-10-22

申请人： Philippe Durette ,  Ihor Kopka ,  Malcolm MacCoss ,  Sander Mills

发明人： Philippe Durette ,  Ihor Kopka ,  Malcolm MacCoss ,  Sander Mills

IPC分类号： C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D413/04 ,  A61K31/44

CPC分类号： C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D413/04

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, A, 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表示的某些新型化合物或其药学上可接受的盐，其中R3，R6，R7，R8，R11，R12，R13，A，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。