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1. 发明授权

US07160888B2 [1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia 失效
标题翻译： [1,8]萘啶-2-酮和相关化合物用于治疗精神分裂症
公开(公告)号：US07160888B2
公开(公告)日：2007-01-09
申请号：US10900210
申请日：2004-07-28
申请人： Douglas S. Johnson , Joseph Thomas Repine , Andrew David White
发明人： Douglas S. Johnson , Joseph Thomas Repine , Andrew David White
IPC分类号： A61K31/496 , C07D471/04
CPC分类号： C07D471/04
摘要： This invention relates to compounds of the formula 1 wherein G, D, A, Z, Q, X, Y, R1, and R4 through R7 are defined as in the specification, processes for preparing the same and intermediates used in making the same, and pharmaceutical compositions containing such compounds and their use in the treatment of central nervous system disorders and other disorders.
摘要翻译：本发明涉及式1的化合物，其中G，D，A，Z，Q，X，Y，R 1和R 4至R 7 在说明书中定义，其制备方法和用于制备其的中间体，以及含有这些化合物的药物组合物及其在治疗中枢神经系统疾病和其它疾病中的用途。

2. 发明授权

US06943183B2 5-substituted tetralones as inhibitors of ras farnesyl transferase 失效
标题翻译： 5-取代的四氢萘酮作为法尼基转移酶的抑制剂
公开(公告)号：US06943183B2
公开(公告)日：2005-09-13
申请号：US10257301
申请日：2001-04-16
申请人： William Alexander Denny , Richard H. Hutchings , Douglas S. Johnson , James Stanley Kaltenbronn , Ho Huat Lee , Daniele Marie Leonard , Jared Bruce John Milbank , Joseph Thomas Repine , Gordon William Rewcastle , Andrew David White
发明人： William Alexander Denny , Richard H. Hutchings , Douglas S. Johnson , James Stanley Kaltenbronn , Ho Huat Lee , Daniele Marie Leonard , Jared Bruce John Milbank , Joseph Thomas Repine , Gordon William Rewcastle , Andrew David White
IPC分类号： C07D233/60 , A61K31/4164 , A61K31/4178 , A61K31/422 , A61K31/4439 , A61K31/4725 , A61K31/496 , A61K31/497 , A61P9/10 , A61P13/00 , A61P13/08 , A61P17/06 , A61P27/02 , A61P31/12 , A61P35/00 , A61P43/00 , C07D233/54 , C07D233/91 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14 , C07D521/00 , C07D233/64
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D233/91 , C07D249/08 , C07D401/12
摘要： The present invention provides novel 5-substituted tetralones of Formulas I, II, III, and IV and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis. Specifically, the present invention relates to compounds that inhibit the farnesyl transferase enzyme
摘要翻译：本发明提供式I，II，III和IV的新型5-取代四氢萘酮及其药学上可接受的盐，酯，酰胺和前药，其可用于治疗和预防组织如癌症的不受控制或异常增殖，动脉粥样硬化，再狭窄和牛皮癣。具体地，本发明涉及抑制法呢基转移酶的化合物

3. 发明授权

US06528535B2 Bicyclic inhibitors of protein farnesyl transferase 失效
标题翻译：蛋白质法呢基转移酶的双环抑制剂
公开(公告)号：US06528535B2
公开(公告)日：2003-03-04
申请号：US09910967
申请日：2001-07-23
申请人： Jack Bikker , Ellen Myra Dobrusin , Annette Marian Doherty , Matthew Drowns , James Stanley Kaltenbronn , Juergen Kleinschroth , Dennis Joseph McNamara , John Quin, III , Joseph Thomas Repine , Marcin Stasiak
发明人： Jack Bikker , Ellen Myra Dobrusin , Annette Marian Doherty , Matthew Drowns , James Stanley Kaltenbronn , Juergen Kleinschroth , Dennis Joseph McNamara , John Quin, III , Joseph Thomas Repine , Marcin Stasiak
IPC分类号： A61K31415
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/12 , C07D409/12
摘要： The present invention provide compounds of Formula I The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.
摘要翻译：本发明提供式I化合物本发明还提供了治疗癌症和治疗或预防再狭窄或动脉粥样硬化的方法。本发明还提供了含有式I化合物的药学上可接受的组合物。

4. 发明授权

US06265422B1 Bicyclic inhibitors of protein farnesyl transferase 失效
标题翻译：蛋白质法呢基转移酶的双环抑制剂
公开(公告)号：US06265422B1
公开(公告)日：2001-07-24
申请号：US09560606
申请日：2000-04-28
申请人： Jack Bikker , Ellen Myra Dobrusin , Annette Marian Doherty , Matthew Drowns , James Stanley Kaltenbronn , Juergen Kleinschroth , Dennis Joseph McNamara , John Quin, III , Joseph Thomas Repine , Marcin Stasiak
发明人： Jack Bikker , Ellen Myra Dobrusin , Annette Marian Doherty , Matthew Drowns , James Stanley Kaltenbronn , Juergen Kleinschroth , Dennis Joseph McNamara , John Quin, III , Joseph Thomas Repine , Marcin Stasiak
IPC分类号： A61K3144
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/12 , C07D409/12
摘要： The present invention provides compounds of Formula I The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.
摘要翻译：本发明提供式I化合物本发明还提供了治疗癌症和治疗或预防再狭窄或动脉粥样硬化的方法。本发明还提供了含有式I化合物的药学上可接受的组合物。

5. 发明授权

US5691373A Nonpeptide endothelin antagonists I 失效
标题翻译：非肽内皮素拮抗剂
公开(公告)号：US5691373A
公开(公告)日：1997-11-25
申请号：US384083
申请日：1995-02-06
申请人： Kent Alan Berryman , Annette Marian Doherty , Jeremy John Edmunds , William Chester Patt , Mark Stephen Plummer , Joseph Thomas Repine
发明人： Kent Alan Berryman , Annette Marian Doherty , Jeremy John Edmunds , William Chester Patt , Mark Stephen Plummer , Joseph Thomas Repine
IPC分类号： C07D317/60 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/54 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P37/00 , A61P43/00 , C07C45/41 , C07C45/71 , C07C45/74 , C07C47/11 , C07C47/235 , C07C47/575 , C07C49/813 , C07C49/84 , C07C59/90 , C07D307/60 , C07D333/32 , C07D405/04 , C07D405/06 , C07D405/14 , C07D407/04 , C07D407/06 , C07D407/14 , C07D409/04 , C07D409/14 , A61K31/36 , A61K31/535
CPC分类号： C07D405/04 , C07C45/41 , C07C45/71 , C07C45/74 , C07C47/11 , C07C47/235 , C07C47/575 , C07C49/813 , C07C49/84 , C07C59/90 , C07D307/60 , C07D405/06 , C07D405/14 , C07D407/04 , C07D407/06 , C07D407/14 , C07D409/04 , C07D409/14
摘要： Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.
摘要翻译：描述了内皮素I的新型非肽拮抗剂，以及其制备方法及其药物组合物，其可用于治疗高水平的内皮素，急性和慢性肾衰竭，高血压，心肌梗死，心肌缺血，脑血管痉挛，脑缺血，脑梗死，肝硬化，败血性休克，充血性心力衰竭，内毒素性休克，蛛网膜下腔出血，心律失常，哮喘，先兆子痫，动脉粥样硬化疾病包括雷诺氏病和再狭窄，心绞痛，癌症，肺动脉高压，缺血性疾病，胃粘膜损伤，出血休克，缺血性肠病，中风，良性前列腺增生（BPH）和糖尿病。

6. 发明授权

US06936612B2 2-(Pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones 有权
标题翻译： 2-（吡啶-2-基氨基） - 吡啶并[2,3-d]嘧啶-7-酮
公开(公告)号：US06936612B2
公开(公告)日：2005-08-30
申请号：US10345778
申请日：2003-01-16
申请人： Mark Barvian , Richard John Booth , John Quin, III , Joseph Thomas Repine , Derek J. Sheehan , Peter Laurence Toogood , Scott Norman Vanderwel , Hairong Zhou
发明人： Mark Barvian , Richard John Booth , John Quin, III , Joseph Thomas Repine , Derek J. Sheehan , Peter Laurence Toogood , Scott Norman Vanderwel , Hairong Zhou
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/551 , A61K31/675 , A61P3/10 , A61P9/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/10 , A61P31/12 , A61P31/18 , A61P31/22 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00 , C07D471/04 , C07F9/6561 , C07D401/14 , A61K31/444
CPC分类号： C07D471/04 , A61K31/519 , A61K31/675
摘要： The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (cdk4)
摘要翻译：本发明提供了可用于治疗细胞增殖性疾病的取代的2-氨基吡啶。本发明的新化合物是细胞周期蛋白依赖性激酶4（cdk4）的有效抑制剂，

7. 发明授权

US06440962B2 Certain benzothiazine dioxide endothelin antagonists and processes for their preparation 失效
标题翻译：某些苯并噻嗪二氧化物内皮素拮抗剂及其制备方法
公开(公告)号：US06440962B2
公开(公告)日：2002-08-27
申请号：US09818394
申请日：2001-03-27
申请人： Amy Mae Bunker , Xue-Min Cheng , Annette Marian Doherty , Jeremy John Edmunds , Gerald David Kanter , Chitase Lee , Joseph Thomas Repine , Richard William Skeean
发明人： Amy Mae Bunker , Xue-Min Cheng , Annette Marian Doherty , Jeremy John Edmunds , Gerald David Kanter , Chitase Lee , Joseph Thomas Repine , Richard William Skeean
IPC分类号： C07D27902
CPC分类号： C07D417/04 , C07C303/40 , C07D279/02 , C07D417/10 , C07C311/21
摘要： The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula I The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.
摘要翻译：本发明是一系列苯并噻嗪二氧化物或其药学上可接受的盐，其是具有深度体外活性的有效的内皮素A拮抗剂，并且对于式It化合物的改进的合成可用于治疗升高的内皮素水平，必需的血管性恶性和肺动脉高压，脑梗塞，脑缺血，充血性心力衰竭和蛛网膜下腔出血。

8. 发明授权

US06297274B1 Nonpeptide endothelin antagonists with increased water solubility 失效
标题翻译：具有增加的水溶性的非肽内皮素拮抗剂
公开(公告)号：US06297274B1
公开(公告)日：2001-10-02
申请号：US09117667
申请日：1998-08-04
申请人： Xue-Min Cheng , Annette Marian Doherty , William Chester Patt , Joseph Thomas Repine
发明人： Xue-Min Cheng , Annette Marian Doherty , William Chester Patt , Joseph Thomas Repine
IPC分类号： A61K3134
CPC分类号： C07D407/04 , C07D307/60
摘要： Novel nonpeptide endothelin I antagonists of Formula are described wherein R1 is unsubstituted or substituted cycloalkyl, phenyl, naphthyl or heteroaryl, R2 is unsubstituted or substituted alkyl, aryl or heteroaryl, R3 is unsubstituted or substituted alkyl, cycloalkyl, aryl or heteroayl, and R1 and/or R2 and/or R3 are independently substituted by a total of from 1 to 4 substituents which enhance aqueous solubility with the proviso that when R2 is alkyl and is substituted, the substituent is not oxygen at the &agr;-position of the furanone ring. Further described are methods for the preparation and pharmaceutical compositions of compounds of Formula I, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, glaucoma, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemic bowel disease, Chrohn's disease, male penile erectile dysfunction, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, cancer, especially malignant hemangioendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nephrotoxcity, endotoxic, septic hemorrhagic shock, angina, preeclampsia, asthma, arrhythmias, benign prostatic hyperplasia, and elevated levels of endothelin.
摘要翻译：苯基，萘基或杂芳基，R2为未取代或取代的烷基，芳基或杂芳基，R3为未取代或取代的烷基，环烷基，芳基或杂芳基，R1和/ 或R 2和/或R 3独立地被总共1至4个增强水溶性的取代基取代，条件是当R 2是烷基且被取代时，该取代基不是在呋喃酮环的α-位上的氧。进一步描述了用于制备治疗动脉粥样硬化，再狭窄，雷诺现象，轻度或重度充血性心力衰竭，脑缺血，脑梗死，栓塞性中风，脑血管痉挛，青光眼，蛛网膜下腔出血出血性，出血性中风，糖尿病，胃溃疡和粘膜损伤，缺血性肠病，克罗恩病，男性阴茎勃起功能障碍，基本或恶性高血压，肺动脉高压，旁路后肺动脉高压，癌症，特别是恶性血管内皮瘤或前列腺癌，心肌梗塞或缺血，急性或慢性肾衰竭，肾缺血，放射性对照诱导的肾毒性，内毒素性，败血性出血性休克，心绞痛，先兆子痫，哮喘，心律失常，良性前列腺增生和内皮素水平升高。

9. 发明授权

US06252070B1 Certain benzothiazine dioxide endothelin antagonists and processes for their preparation 失效
标题翻译：某些苯并噻嗪二氧化物内皮素拮抗剂及其制备方法
公开(公告)号：US06252070B1
公开(公告)日：2001-06-26
申请号：US09633720
申请日：2000-08-07
申请人： Amy Mae Bunker , Xue-Min Cheng , Annette Marian Doherty , Jeremy John Edmunds , Gerald David Kanter , Chitase Lee , Joseph Thomas Repine , Richard William Skeean
发明人： Amy Mae Bunker , Xue-Min Cheng , Annette Marian Doherty , Jeremy John Edmunds , Gerald David Kanter , Chitase Lee , Joseph Thomas Repine , Richard William Skeean
IPC分类号： C07D27916
CPC分类号： C07D417/04 , C07C303/40 , C07D279/02 , C07D417/10 , C07C311/21
摘要： The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.
摘要翻译：本发明是一系列苯并噻嗪二氧化物或其药学上可接受的盐，其是具有深度体外活性的有效的内皮素A拮抗剂，以及式1的改进的合成。该化合物可用于治疗升高的内皮素水平，必需的血管性恶性和肺动脉高压，脑梗塞，脑缺血，充血性心力衰竭和蛛网膜下腔出血。

10. 发明授权

US06545150B2 Certain benzothiazine dioxide endothelin antagonists and processes for their preparation 失效
标题翻译：某些苯并噻嗪二氧化物内皮素拮抗剂及其制备方法
公开(公告)号：US06545150B2
公开(公告)日：2003-04-08
申请号：US10006589
申请日：2001-12-05
申请人： Amy Mae Bunker , Xue-Min Cheng , Annette Marian Doherty , Jeremy John Edmunds , Gerald David Kanter , Chitase Lee , Joseph Thomas Repine , Richard William Skeean
发明人： Amy Mae Bunker , Xue-Min Cheng , Annette Marian Doherty , Jeremy John Edmunds , Gerald David Kanter , Chitase Lee , Joseph Thomas Repine , Richard William Skeean
IPC分类号： C07D27916
CPC分类号： C07D417/04 , C07C303/40 , C07D279/02 , C07D417/10 , C07C311/21
摘要： The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.
摘要翻译：本发明是一系列苯并噻嗪二氧化物或其药学上可接受的盐，其是具有深度体外活性的有效的内皮素A拮抗剂，以及式1的改进的合成。该化合物可用于治疗升高的内皮素水平，必需的血管性恶性和肺动脉高压，脑梗塞，脑缺血，充血性心力衰竭和蛛网膜下腔出血。

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