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公开(公告)号：US07834007B2
公开(公告)日：2010-11-16
申请号：US11508568
申请日：2006-08-23
IPC分类号： A61K31/54 , A61K31/535 , A61K31/50 , A61K31/435 , A61K31/41 , A01N43/66 , A01N43/58 , A01N43/40 , A01N43/64 , C07D417/00 , C07D413/00 , C07D403/00 , C07D241/02 , C07D401/00
CPC分类号： C07D401/14 , C07D413/14 , C07D471/04
摘要： The present invention encompasses compounds of Formula I which are antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
摘要翻译： 本发明包括作为降钙素基因相关肽受体（“CGRP受体”）的拮抗剂的式I化合物，包含它们的药物组合物，鉴定它们的方法，使用它们的治疗方法及其在治疗神经源性治疗中的用途 血管舒张，神经源性炎症，偏头痛和其他头痛，热损伤，循环休克，与更年期相关的潮红，气道炎症性疾病如哮喘和慢性阻塞性肺病（COPD）以及治疗可通过拮抗作用的其他病症 的CGRP受体。
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12.发明授权.alpha.-heteroaryloxymethyl ketones as interleukin - 1 .beta. converting enzyme inhibitors 失效α-杂环氧基甲基酮作为白细胞介素-1β转换酶抑制剂
公开(公告)号：US5677283A
公开(公告)日：1997-10-14
申请号：US732173
申请日：1996-10-16
申请人： Roland E. Dolle , Jasbir Singh , David A. Whipple , Catherine Prouty , Prasad V. Chaturvedula , Stanley J. Schmidt , Mohamed M. A. Awad , Denton W. Hoyer , Tina Morgan Ross
发明人： Roland E. Dolle , Jasbir Singh , David A. Whipple , Catherine Prouty , Prasad V. Chaturvedula , Stanley J. Schmidt , Mohamed M. A. Awad , Denton W. Hoyer , Tina Morgan Ross
IPC分类号： C12N9/99 , A61K31/397 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/47 , A61K31/472 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61K38/00 , A61P29/00 , A61P37/00 , A61P43/00 , C07D205/04 , C07D207/38 , C07D209/12 , C07D215/14 , C07D217/16 , C07D223/08 , C07D231/20 , C07D231/22 , C07D261/12 , C07D263/06 , C07D265/06 , C07D265/30 , C07D311/46 , C07D311/50 , C07D311/56 , C07D401/12 , C07D409/12 , C07D413/04 , C07D417/12 , C07D453/02 , C07D471/04 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/078 , C07K5/08 , C07K5/083 , C07K5/09 , C07K5/097 , C07D231/04 , C07K5/00
CPC分类号： C07D401/12 , C07D207/38 , C07D231/20 , C07D231/22 , C07D261/12 , C07D311/46 , C07D311/56 , C07D409/12 , C07D413/04 , C07D417/12 , C07D453/02 , C07K5/0202 , A61K38/00
摘要： Compounds which Inhibit interleukin-1.beta. protease activity, pharmaceutical compositions containing the compounds and methods using the compounds are provided. The compounds have the formula ##STR1## wherein n is 0-2; each AA is Independently L-valine or L-alanine; R.sub.1 is selected from the group consisting of N-�4(N,N-dimethylaminomethyl)!benzoyl, N-benzoyloxycarbonyl, N-methyl-N-�4-(pyridyl)methyl!, N-�4-(pyddyl)methyl!carbonyl, N-3-(piperidinopropionyl), N-�4-(morpholinoethoxy)benzoyl, N-2-(quinuclidinyl)carbonyl, N-(3-pyridyl)methoxy carbonyl, N-(2-pyddyl)methoxy carbonyl, N-methyl-N-benzyl carbonyl, N-methyl-N-�2-(4-pyridyl)ethyl!carbonyl, and N-(N-phenylpiperazino) carbonyl; and R.sub.8, R.sub.9 and R.sub.10 are as defined below.
摘要翻译： 提供了抑制白细胞介素-1β蛋白酶活性的化合物，含有这些化合物的药物组合物和使用该化合物的方法。 化合物具有式（1）其中n为0-2; 每个AA是独立的L-缬氨酸或L-丙氨酸; R1选自N- [4（N，N-二甲基氨基甲基）]苯甲酰基，N-苯甲酰氧基羰基，N-甲基-N- [4-（吡啶基）甲基]，N- [4-（吡啶基）甲基 ]羰基，N-3-（哌啶基丙酰基），N- [4-（吗啉代乙氧基）苯甲酰基，N-2-（奎宁环基）羰基，N-（3-吡啶基）甲氧基羰基，N-（2- N-甲基-N-苄基羰基，N-甲基-N- [2-（4-吡啶基）乙基]羰基和N-（N-苯基哌嗪基）羰基; 并且R 8，R 9和R 10如下所定义。
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13.发明授权Fused-bicyclic lactams as interleukin-1.beta. converting enzyme inhibitors 失效融合双环内酰胺作为白细胞介素-1β转换酶抑制剂
公开(公告)号：US5639745A
公开(公告)日：1997-06-17
申请号：US451108
申请日：1995-05-25
IPC分类号： C07D487/04 , A61K31/535 , A61K31/55 , A61K38/00 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D471/04 , C07D513/04 , C07K5/02 , C07K5/06 , C07K5/078
CPC分类号： C07K5/06139 , C07K5/0202 , C07K5/021 , C07K5/06191 , A61K38/00
摘要： Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.
摘要翻译： 公开了抑制白细胞介素-1β蛋白酶活性的化合物，组合物和方法。 醛和α-取代的甲基酮的化合物，双环衍生物具有本文所述的式（A）。
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公开(公告)号：US07470679B2
公开(公告)日：2008-12-30
申请号：US11742615
申请日：2007-05-01
IPC分类号： C07D487/04 , C07D401/14 , C07D519/00 , A61K31/55 , A61P25/06
CPC分类号： C07D491/04 , C07D487/04
摘要： The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
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公开(公告)号：US07384931B2
公开(公告)日：2008-06-10
申请号：US11417326
申请日：2006-05-03
IPC分类号： C07D487/04 , C07D401/14 , C07D519/00 , A61K31/55 , A61P25/06
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors
摘要翻译： 本发明包括受限制的双环和三环CGRP受体拮抗剂，鉴定它们的方法，包含它们的药物组合物及其用于治疗偏头痛和其他头痛，神经源性血管舒张，神经源性炎症，热损伤，循环休克，冲洗的方法 与更年期，气道炎症性疾病如哮喘和慢性阻塞性肺疾病（COPD）有关的其他病症，其治疗可以通过CGRP受体的拮抗作用
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16.发明授权Benzodiazepinone &bgr;-amyloid inhibitors: arylacetamidoalanyl derivatives 有权苯并二氮丙酮β-淀粉样蛋白抑制剂：芳基乙酰氨基丙氨酰基衍生物公开(公告)号：US06432944B1
公开(公告)日：2002-08-13
申请号：US09897545
申请日：2001-07-02
申请人： Prasad V. Chaturvedula , Suresh Yeola , Shikha Vig
发明人： Prasad V. Chaturvedula , Suresh Yeola , Shikha Vig
IPC分类号： A61K3155
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06191 , C07K5/0812 , C07K5/0827
摘要： There is provided a series of arylacetamidoalanyl derivatives of benzodiazepinones of Formula I wherein R1 through R7 and n are defined herein, which are inhibitors of &bgr;-amyloid peptide (&bgr;-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions characterized by aberrant extract cellular deposition of amyloid.
摘要翻译： 提供了一系列式I的苯并二氮杂酮的芳基乙酰氨基丙氨酰基衍生物，其中R1至R7和n定义在本文中，其为β-淀粉样蛋白肽（β-AP）产生的抑制剂，并且可用于治疗阿尔茨海默氏病和其他特征为 淀粉样蛋白异常提取细胞沉积。
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17.发明授权N-(pyrimidinyl)-aspartic acid analogs as interleukin-1.beta. converting enzyme inhibitors 失效N-（嘧啶基） - 天冬氨酸类似物作为白细胞介素-1β转换酶抑制剂
公开(公告)号：US06162800A
公开(公告)日：2000-12-19
申请号：US877380
申请日：1997-06-17
IPC分类号： C07D239/47 , A61K31/505 , A61K31/506 , A61K38/00 , A61P29/00 , A61P37/00 , A61P43/00 , C07D401/04 , C07D403/12 , C07D405/12 , C07D409/04 , C07F9/6512 , C07K5/02 , C07K5/06 , C07K5/078 , A61K31/513 , C07D239/36
CPC分类号： C07K5/06139 , A61K38/00 , C07F9/6512 , C07K5/0202 , C07K5/06191
摘要： Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. (IL-.beta.) protease activity. The compounds, N-(pyrimidinyl)-aspartic acid .alpha.-substituted methyl ketones and aspartic acid aldehydes, have the formula (I) set out herein. These compounds are inhibitors of 1.beta.-converting enzyme and as such are useful whenever such inhibition is desired. For example, they may be used as research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which 1L-.beta. protease activity is implicated.
摘要翻译： 公开了抑制白细胞介素-1β（IL-β）蛋白酶活性的化合物，组合物和方法。 化合物N-（嘧啶基） - 天冬氨酸α-取代甲基酮和天冬氨酸醛具有式（I）。 这些化合物是1β-转化酶的抑制剂，因此当需要这种抑制时是有用的。 例如，它们可以用作药理学，诊断学和相关研究中的研究工具以及涉及1L-β蛋白酶活性的哺乳动物疾病的治疗。
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18.发明授权
公开(公告)号：US5985838A
公开(公告)日：1999-11-16
申请号：US679350
申请日：1996-07-10
申请人： Roland E. Dolle , Irennegbe K. Osifo , Stanley J. Schmidt , Denton W. Hoyer , Tina Morgan Ross , Prasad V. Chaturvedula , Catherine P. Prouty , Mohamed M. A. Awad , Joseph M. Salvino , James M. Rinker , Eric P. Lodge , Jasbir Singh , Mark A. Ator
发明人： Roland E. Dolle , Irennegbe K. Osifo , Stanley J. Schmidt , Denton W. Hoyer , Tina Morgan Ross , Prasad V. Chaturvedula , Catherine P. Prouty , Mohamed M. A. Awad , Joseph M. Salvino , James M. Rinker , Eric P. Lodge , Jasbir Singh , Mark A. Ator
IPC分类号： A61P31/00 , C07C233/51 , C07C235/12 , C07C237/36 , C07C271/22 , C07C311/16 , C07C311/19 , C07D233/54 , C07D295/092 , C07D295/30 , C07D307/68 , C07D333/36 , C07D333/38 , C07K5/06 , A61K38/05
CPC分类号： C07D233/64 , C07C233/51 , C07C235/12 , C07C237/36 , C07C271/22 , C07C311/16 , C07C311/19 , C07D295/088 , C07D295/30 , C07D307/68 , C07D333/36 , C07D333/38 , C07K5/06191
摘要： Disclosed are compounds, compositions and methods for inhi.beta.iting interleukin-1.beta. protease activity, the compounds .alpha.-substituted methyl ketones having the formula (I) set forth herein. These compounds are inhibitors of IL-1.beta. converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.
摘要翻译： 公开了化合物，组合物和方法，用于测定白细胞介素-1β蛋白酶活性，化合物具有式（I）的α-取代的甲基酮。 这些化合物是IL-1β转换酶的抑制剂，因此可用作某些感染性疾病的治疗剂。
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19.发明授权Processes for the preparation of CGRP-receptor antagonists and intermediates thereof 有权制备CGRP受体拮抗剂及其中间体的方法公开(公告)号：US07449586B2
公开(公告)日：2008-11-11
申请号：US11291670
申请日：2005-12-01
IPC分类号： C07D231/56
CPC分类号： C07D471/04 , C07D231/56 , C07D401/12 , C07D401/14
摘要： The invention relates to novel processes for the preparation of small molecule antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”) and intermediates thereof.
摘要翻译： 本发明涉及制备降钙素基因相关肽受体（“CGRP受体”）及其中间体的小分子拮抗剂的新方法。
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公开(公告)号：US08592423B2
公开(公告)日：2013-11-26
申请号：US13525976
申请日：2012-06-18
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： PDE10 inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit PDE10 are also disclosed.
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