公开(公告)号：US07741493B2

公开(公告)日：2010-06-22

申请号：US11947442

申请日：2007-11-29

申请人： Patrick Shum ,  Alexandre Gross ,  Liang Ma ,  Daniel G. McGarry ,  Gregory H. Merriman ,  David Rampe ,  Garth Ringheim ,  Jeffrey Stephen Sabol ,  Francis A. Volz

发明人： Patrick Shum ,  Alexandre Gross ,  Liang Ma ,  Daniel G. McGarry ,  Gregory H. Merriman ,  David Rampe ,  Garth Ringheim ,  Jeffrey Stephen Sabol ,  Francis A. Volz

IPC分类号： A61K31/4184 ,  C07D235/02

CPC分类号： C07D401/04 ,  C07D233/20 ,  C07D233/22 ,  C07D233/24 ,  C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D235/30 ,  C07D401/06 ,  C07D405/06 ,  C07D405/12 ,  C07D409/10

摘要： The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.

摘要翻译： 本发明涉及式II的新一系列4,5-二苯基-2-氨基-4,5-二氢咪唑衍生物：其中R，R 1，R 2，R 3，R 4，R 5，X和Y为 本文定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是P2X7离子通道阻断剂，因此可用作药剂，特别是用于治疗和/或预防各种具有炎症成分的疾病，包括炎性肠病，类风湿性关节炎和与中枢相关的疾病状况 神经系统，如中风，阿尔茨海默病等

公开(公告)号：US07326792B2

公开(公告)日：2008-02-05

申请号：US10896166

申请日：2004-07-21

申请人： Patrick Shum ,  Alexandre Gross ,  Liang Ma ,  Daniel G. McGarry ,  Gregory H. Merriman ,  David Rampe ,  Garth Ringheim ,  Jeffrey Stephen Sabol ,  Francis A. Volz

发明人： Patrick Shum ,  Alexandre Gross ,  Liang Ma ,  Daniel G. McGarry ,  Gregory H. Merriman ,  David Rampe ,  Garth Ringheim ,  Jeffrey Stephen Sabol ,  Francis A. Volz

IPC分类号： A61K31/4168 ,  A61K31/417 ,  C07D233/24 ,  C07D233/50

CPC分类号： C07D401/04 ,  C07D233/20 ,  C07D233/22 ,  C07D233/24 ,  C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D235/30 ,  C07D401/06 ,  C07D405/06 ,  C07D405/12 ,  C07D409/10

摘要： The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.

摘要翻译： 本发明涉及式II的新一系列4,5-二苯基-2-氨基-4,5-二氢 - 咪唑衍生物：其中R 1，R 2，R 2 R 3，R 4，R 5，X和Y如本文所定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是P2X7离子通道阻断剂，因此可用作药剂，特别是用于治疗和/或预防各种具有炎症成分的疾病，包括炎性肠病，类风湿性关节炎和与中枢相关的疾病状况 神经系统，如中风，阿尔茨海默病等

公开(公告)号：US5216015A

公开(公告)日：1993-06-01

申请号：US650494

申请日：1991-02-05

申请人： Daniel G. McGarry ,  Francis A. Volz ,  John R. Regan ,  Michael N. Chang

发明人： Daniel G. McGarry ,  Francis A. Volz ,  John R. Regan ,  Michael N. Chang

IPC分类号： C07J9/00 ,  C07J13/00 ,  C07J17/00 ,  C07J31/00 ,  C07J51/00 ,  C07J63/00

CPC分类号： C07J9/00 ,  C07J13/005 ,  C07J17/00 ,  C07J31/006 ,  C07J51/00 ,  C07J63/008 ,  C07J9/005

摘要： This invention relates to compounds which are steroidyl derivatives of 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one and the corresponding ring-opened hydroxy acid form thereof which are useful as antihypercholesterolemic agents, to pharmaceutical compositions including such compounds, and to their use in treating hypercholesterolemia.

摘要翻译： 本发明涉及作为抗高胆固醇血症药物使用的4-羟基-3,4,5,6-四氢-2H-吡喃-2-酮的类固醇衍生物及其相应的开环羟基酸形式的化合物， 包括这些化合物的组合物及其在治疗高胆固醇血症中的用途。

公开(公告)号：US06599918B2

公开(公告)日：2003-07-29

申请号：US10081113

申请日：2002-02-22

申请人： Christopher J. Burns ,  William P. Dankulich ,  Daniel G. McGarry ,  Francis A. Volz

发明人： Christopher J. Burns ,  William P. Dankulich ,  Daniel G. McGarry ,  Francis A. Volz

IPC分类号： A61K31443

CPC分类号： C07D405/12 ,  C07D307/81 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D471/04

摘要： This invention is directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans that inhibit Factor Xa, pharmaceutical compositions comprising these compounds and their use for inhibiting Factor Xa or treating pathological conditions in a patient that may be ameliorated by administration of such compounds. This invention is also is also directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans which directly inhibit both Factor Xa and Factor IIa (thrombin), to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds and to a method of simultaneously directly inhibiting both Factor Xa and Factor IIa (thrombin).

公开(公告)号：US06541505B1

公开(公告)日：2003-04-01

申请号：US09609103

申请日：2000-06-30

申请人： William P. Dankulich ,  Daniel G. McGarry ,  Christopher Burns ,  Timothy F. Gallagher ,  Francis A. Volz

发明人： William P. Dankulich ,  Daniel G. McGarry ,  Christopher Burns ,  Timothy F. Gallagher ,  Francis A. Volz

IPC分类号： A61K31405

CPC分类号： C07D231/12 ,  C07D209/42 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

摘要： This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

摘要翻译： 本发明涉及式I的（氨基亚氨基甲基或氨基甲基）苯并杂芳基化合物，其可用于通过将所述化合物与含有因子Xa的组合物组合来抑制因子Xa的活性。 本发明还涉及包含式I化合物的组合物，其制备方法，其用途，例如抑制凝血酶的形成或用于治疗患有或与生理学相关的疾病状态患者或受其影响的患者 有害的过量凝血酶。