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1. 发明授权

US06534510B2 Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US06534510B2
公开(公告)日：2003-03-18
申请号：US09815404
申请日：2001-03-22
申请人： James C. Barrow , Bruce D. Dorsey , Harold G. Selnick , Phung L. Ngo
发明人： James C. Barrow , Bruce D. Dorsey , Harold G. Selnick , Phung L. Ngo
IPC分类号： C07D40100
CPC分类号： C07D401/12 , C07D401/14 , C07D471/04
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of: or a pharmaceutically acceptable salt thereof, wherein A is
摘要翻译：本发明的化合物可用于抑制凝血酶和相关的血栓闭塞，并且选自：或其药学上可接受的盐，其中A是

2. 发明授权

US06610701B2 Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US06610701B2
公开(公告)日：2003-08-26
申请号：US10071422
申请日：2002-02-08
申请人： James C. Barrow , Craig Coburn , Harold G. Selnick , Phung L. Ngo
发明人： James C. Barrow , Craig Coburn , Harold G. Selnick , Phung L. Ngo
IPC分类号： A61K314375
CPC分类号： C07D213/75 , C07D213/26 , C07D213/89 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D471/04
摘要： Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.
摘要翻译：本发明化合物可用于抑制凝血酶和治疗凝血和心血管疾病，并具有以下结构：其中R 3为氢或卤素，u为N或CH。

3. 发明授权

US07084134B2 Thrombin inhibitors 失效
公开(公告)号：US07084134B2
公开(公告)日：2006-08-01
申请号：US10427435
申请日：2003-05-01
申请人： James C. Barrow , Philippe G. Nantermet , Harold G. Selnick
发明人： James C. Barrow , Philippe G. Nantermet , Harold G. Selnick
IPC分类号： A61K38/00
CPC分类号： C07K5/12 , A61K38/00 , A61K38/55
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof.

4. 发明授权

US06462050B1 Thrombin inhibitors 失效
公开(公告)号：US06462050B1
公开(公告)日：2002-10-08
申请号：US09916745
申请日：2001-07-27
申请人： Richard C. Isaacs , Kellie Cutrona , James C. Barrow , Harold G. Selnick
发明人： Richard C. Isaacs , Kellie Cutrona , James C. Barrow , Harold G. Selnick
IPC分类号： A61K31497
CPC分类号： C07D401/12 , A61K38/00 , C07D401/14 , C07K5/06191
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure:

5. 发明授权

US07550481B2 Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease 有权
标题翻译：苯酰胺和吡啶酰胺β-分泌酶抑制剂治疗阿尔茨海默病
公开(公告)号：US07550481B2
公开(公告)日：2009-06-23
申请号：US10582856
申请日：2004-12-15
申请人： James C. Barrow , Craig A. Coburn , Philippe G. Nantermet , Harold G. Selnick , Shawn J. Stachel , Matthew G. Stanton , Shaun R. Stauffer , Linghang Zhuang , Jennifer R. Davis
发明人： James C. Barrow , Craig A. Coburn , Philippe G. Nantermet , Harold G. Selnick , Shawn J. Stachel , Matthew G. Stanton , Shaun R. Stauffer , Linghang Zhuang , Jennifer R. Davis
IPC分类号： C07D401/02 , A61K31/44
CPC分类号： C07D213/81 , C07D213/75 , C07D257/04 , C07D401/04 , C07D409/12 , C07D413/12
摘要： The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译：本发明涉及苯酰胺和吡啶酰胺衍生物化合物，其是β-分泌酶的抑制剂，可用于治疗其中涉及β-分泌酶的疾病，例如阿尔茨海默氏病。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治疗涉及β-分泌酶的疾病中的用途。

6. 发明授权

US06403612B2 Thrombin receptor antagonists 失效
标题翻译：凝血酶受体拮抗剂
公开(公告)号：US06403612B2
公开(公告)日：2002-06-11
申请号：US09772352
申请日：2001-01-30
申请人： Philippe G. Nantermet , James C. Barrow , Harold G. Selnick
发明人： Philippe G. Nantermet , James C. Barrow , Harold G. Selnick
IPC分类号： A61K3154
CPC分类号： C07D207/08 , A61K45/06 , C07D207/12 , C07D211/22 , C07D211/42 , C07D277/04
摘要： A thrombin receptor antagonist having the formula or a pharmaceutically acceptable salt thereof, useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.
摘要翻译：具有下式的凝血酶受体拮抗剂或其药学上可接受的盐，其可用于抑制血小板聚集。该化合物可用于作用于凝血酶受体的方法，该方法包括向哺乳动物，优选人类施用治疗有效但无毒量的此类化合物。

7. 发明授权

US08114887B2 Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease 有权
标题翻译：可用作β-分泌酶抑制剂的Spiropiperidine化合物用于治疗阿尔茨海默病
公开(公告)号：US08114887B2
公开(公告)日：2012-02-14
申请号：US11663388
申请日：2005-10-12
申请人： James C. Barrow , Craig A. Coburn , Melissa S. Egbertson , Georgia B. McGaughey , Melody A. McWherter , Lou Anne Neilson , Kenneth E. Rittle , Harold G. Selnick , Shaun R. Stauffer , Zhi-Qiang Yang , Wenjin Yang , Wanli Lu , Bruce Fahr
发明人： James C. Barrow , Craig A. Coburn , Melissa S. Egbertson , Georgia B. McGaughey , Melody A. McWherter , Lou Anne Neilson , Kenneth E. Rittle , Harold G. Selnick , Shaun R. Stauffer , Zhi-Qiang Yang , Wenjin Yang , Wanli Lu , Bruce Fahr
IPC分类号： A61K31/438 , C07D411/02
CPC分类号： C07D471/10
摘要： The present invention is directed to spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译：本发明涉及作为β-分泌酶的抑制剂并且可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的式（I）的哌啶哌啶化合物。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治疗涉及β-分泌酶的疾病中的用途。

8. 发明授权

US07847100B2 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease 有权
标题翻译：可用作治疗阿尔茨海默病的β-分泌酶抑制剂的1,3,5-取代苯基衍生物化合物
公开(公告)号：US07847100B2
公开(公告)日：2010-12-07
申请号：US11578559
申请日：2005-04-15
申请人： James C. Barrow , Georgia B. McGaughey , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer , Craig A. Coburn
发明人： James C. Barrow , Georgia B. McGaughey , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer , Craig A. Coburn
IPC分类号： A61K31/4245 , C07D271/10 , C07D271/06
CPC分类号： C07D271/10 , C07D249/06 , C07D249/08 , C07D263/32 , C07D263/62 , C07D271/06 , C07D285/12 , C07D307/14 , C07D307/42 , C07D307/44 , C07D307/52 , C07D307/54 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14
摘要： The present invention is directed to 1,3,5-phenyl substituted derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译：本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的1,3,5-苯基取代的衍生物化合物。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治疗涉及β-分泌酶的疾病中的用途。

9. 发明授权

US06339090B1 Alpha 1A adrenergic receptor antagonists 失效
标题翻译： α1A肾上腺素能受体拮抗剂
公开(公告)号：US06339090B1
公开(公告)日：2002-01-15
申请号：US09363631
申请日：1999-07-29
申请人： James C. Barrow , Harold G. Selnick , Philippe G. Nantermet
发明人： James C. Barrow , Harold G. Selnick , Philippe G. Nantermet
IPC分类号： A01N4354
CPC分类号： C07D239/22 , C07D211/18 , C07D211/34 , C07D211/52 , C07D211/64 , C07D401/04 , C07D401/12 , C07D401/14
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为α1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物具有选择性地放松富集α1a受体亚型的平滑肌组织的能力，而不会同时引起低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

10. 发明授权

US08394837B2 2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease 有权
标题翻译：用作治疗阿尔茨海默氏病的β-分泌酶抑制剂的2,3,4,6-取代的吡啶衍生物化合物
公开(公告)号：US08394837B2
公开(公告)日：2013-03-12
申请号：US11791204
申请日：2005-11-18
申请人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , James C. Barrow , Shaun R. Stauffer , Joseph P. Vacca , Keith P. Moore , Shawn J. Stachel , Mattahew G. Stanton
发明人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , James C. Barrow , Shaun R. Stauffer , Joseph P. Vacca , Keith P. Moore , Shawn J. Stachel , Mattahew G. Stanton
IPC分类号： A61K31/4439 , C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is directed to 2,3,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译：本发明涉及2,3,4,6-取代的吡啶基衍生物化合物，其是β-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默病。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治疗涉及β-分泌酶的疾病中的用途。

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