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61. 发明申请

US20100168124A1 NOVEL HETEROCYCLIC SUBSTITUTED PYRIDINE COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY 有权
标题翻译：具有CXCR3拮抗剂活性的新型杂环取代的吡啶化合物
公开(公告)号：US20100168124A1
公开(公告)日：2010-07-01
申请号：US12642931
申请日：2009-12-21
申请人： Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
发明人： Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
IPC分类号： A61K31/496 , C07D413/14 , C07D401/14 , C07D417/14 , A61P19/02 , A61P17/06 , A61P11/00
CPC分类号： C07D401/14 , C07D413/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构：或其药学上可接受的盐，溶剂合物或酯。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

62. 发明授权

US08614229B2 Substituted indole derivatives and methods of use thereof 有权
标题翻译：取代的吲哚衍生物及其使用方法
公开(公告)号：US08614229B2
公开(公告)日：2013-12-24
申请号：US12675891
申请日：2008-08-27
申请人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih
发明人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih
IPC分类号： A61K31/47 , A61K31/4402 , A61K31/426 , A61K31/428 , A61K31/4184 , A61K31/404 , C07D239/96 , C07D239/88 , C07D241/44 , C07D471/04 , C07D215/18 , C07D401/04 , C07D211/88 , C07D277/18 , C07D487/04 , C07D275/04 , C07D249/18
CPC分类号： C07D403/04 , C07D401/04
摘要： The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及取代的吲哚衍生物，包含至少一种取代的吲哚衍生物的组合物，以及使用这些取代的吲哚衍生物来治疗或预防患者的病毒感染或病毒相关病症的方法。

63. 发明授权

US08557848B2 4,5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections 有权
标题翻译：用于治疗或预防HCV和相关病毒感染的4,5环环状吲哚衍生物
公开(公告)号：US08557848B2
公开(公告)日：2013-10-15
申请号：US12519715
申请日：2007-12-17
申请人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
发明人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
IPC分类号： A61K31/497 , A61K31/4353 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/498 , A61K31/517 , C07D215/12 , C07D401/14 , C07D241/44 , C07D239/88
CPC分类号： C07D491/04 , C07D401/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.
摘要翻译：本发明涉及4,5-环环状吲哚衍生物，包含至少一种4,5-环环状吲哚衍生物的组合物，以及使用4,5-环环状吲哚衍生物治疗或预防病毒感染或患者病毒相关疾病。其中式（I）的Z环是环戊基，环戊烯基，5元杂环烷基，5元杂环烯基或5元杂芳基环。

64. 发明授权

US08017616B2 Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity 有权
标题翻译：具有CXCR3拮抗活性的杂环取代的吡啶化合物
公开(公告)号：US08017616B2
公开(公告)日：2011-09-13
申请号：US12642931
申请日：2009-12-21
申请人： Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
发明人： Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
IPC分类号： A61K31/496 , C07D413/14
CPC分类号： C07D401/14 , C07D413/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构：或其药学上可接受的盐，溶剂合物或酯。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

65. 发明申请

US20100322901A1 5, 6-RING ANNULATED INDOLE DERIVATIVES AND USE THEREOF 有权
标题翻译： 5，6环结构的吲哚衍生物及其用途
公开(公告)号：US20100322901A1
公开(公告)日：2010-12-23
申请号：US12519975
申请日：2007-12-17
申请人： Frank Bennett , Srikanth Venkatraman , F. George Njoroge , Kevin X. Chen , Neng-Yang Shih , Stuart B. Rosenblum , Joseph A. Kozlowski
发明人： Frank Bennett , Srikanth Venkatraman , F. George Njoroge , Kevin X. Chen , Neng-Yang Shih , Stuart B. Rosenblum , Joseph A. Kozlowski
IPC分类号： A61K31/4439 , C07D401/04 , C07D491/048 , C07D513/04 , C07D417/14 , C07D401/14 , C07D471/04 , A61K31/444 , A61K31/4709 , A61K31/519 , A61K31/517 , A61K31/4375 , A61K31/437 , A61K38/21 , A61K31/7088 , A61K39/00 , A61K39/395 , A61P31/12
CPC分类号： C07D513/04 , C07D401/04 , C07D471/04 , C07D491/04
摘要： The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及式（I）的5,6环环状吲哚衍生物，包含至少一种5,6环环状吲哚衍生物的组合物，以及使用5,6环环状吲哚衍生物用于治疗或预防患者的病毒感染或病毒相关疾病。

66. 发明授权

US07750158B2 Cannabinoid receptor ligands 失效
标题翻译：大麻素受体配体
公开(公告)号：US07750158B2
公开(公告)日：2010-07-06
申请号：US11157510
申请日：2005-06-21
申请人： Bandarpalle B. Shankar , Eric Gilbert , Razia K. Rizvi , Chunli Huang , Joseph A. Kozlowski , Stuart McCombie , Neng-Yang Shih
发明人： Bandarpalle B. Shankar , Eric Gilbert , Razia K. Rizvi , Chunli Huang , Joseph A. Kozlowski , Stuart McCombie , Neng-Yang Shih
IPC分类号： C07D221/00 , A61K31/44
CPC分类号： C07D221/20 , C07D209/52 , C07D401/12 , C07D471/08
摘要： Compounds of Formula I: and/or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions containing such compounds exhibit anti-inflammatory and immunomodulatory activity, and can be effective in treating cancer and inflammatory, immunomodulatory or respiratory diseases or conditions.
摘要翻译：式I化合物和/或其药学上可接受的盐，溶剂化物或前药，或含有这些化合物的药物组合物表现出抗炎和免疫调节活性，并且可有效治疗癌症和炎症，免疫调节或呼吸系统疾病或病症。

67. 发明申请

US20100098661A1 4,5-RING ANNULATED INDOLE DERIVATIVES FOR TREATING OR PREVENTING OF HCV AND RELATED VIRAL INFECTIONS 有权
标题翻译：用于治疗或预防HCV和相关病毒感染的4,5环结构吲哚类衍生物
公开(公告)号：US20100098661A1
公开(公告)日：2010-04-22
申请号：US12519715
申请日：2007-12-17
申请人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
发明人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
IPC分类号： A61K38/21 , C07D401/02 , A61K31/4439 , C07D417/14 , A61K31/4436 , C07D215/00 , A61K31/47 , C07D241/36 , A61K31/498 , C07D401/14 , A61K31/517 , A61K31/444 , A61K39/00 , A61K39/395 , A61P31/12
CPC分类号： C07D491/04 , C07D401/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.
摘要翻译：本发明涉及4,5-环环状吲哚衍生物，包含至少一个4,5-环环状吲哚衍生物的组合物，以及使用4,5-环环状吲哚衍生物治疗或预防病毒感染或患者病毒相关疾病。其中式（I）的Z环是环戊基，环戊烯基，5元杂环烷基，5元杂环烯基或5元杂芳基环。

68. 发明授权

US09254292B2 Fused tetracycle derivatives and methods of use thereof for the treatment of viral diseases 有权
标题翻译：熔融四环衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：US09254292B2
公开(公告)日：2016-02-09
申请号：US13876931
申请日：2011-09-28
申请人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
发明人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
IPC分类号： A61K31/553 , C07D403/14 , C07D405/14 , C07D493/04 , C07D498/04 , A61K31/4178 , A61K31/5517 , A61K45/06 , C07D487/04
CPC分类号： A61K31/553 , A61K31/4178 , A61K31/5517 , A61K45/06 , C07D403/14 , C07D405/14 , C07D487/04 , C07D493/04 , C07D498/04 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A′, B, G, R1, U, V, W, W′, X, X′, Y and Y′ are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新型熔融四环衍生物及其药学上可接受的盐，其中A，A'，B，G，R 1，U，V，W，W'，X，X'，Y和Y '如本文所定义。本发明还涉及包含至少一种熔融四环衍生物的组合物，以及使用熔融四环衍生物治疗或预防患者HCV感染的方法。

69. 发明申请

US20140170111A1 FUSED TETRACYCLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译：融合的四氢吡啶衍生物及其用于治疗病毒的方法
公开(公告)号：US20140170111A1
公开(公告)日：2014-06-19
申请号：US13876931
申请日：2011-09-28
申请人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
发明人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
IPC分类号： A61K31/553 , A61K31/4178 , C07D493/04 , A61K45/06 , C07D498/04 , C07D487/04 , A61K31/5517 , C07D403/14 , C07D405/14
CPC分类号： A61K31/553 , A61K31/4178 , A61K31/5517 , A61K45/06 , C07D403/14 , C07D405/14 , C07D487/04 , C07D493/04 , C07D498/04 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A′, B, G, R1, U, V, W, W′, X, X′, Y and Y′ are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新型熔融四环衍生物及其药学上可接受的盐，其中A，A'，B，G，R 1，U，V，W，W'，X，X'，Y和Y '如本文所定义。本发明还涉及包含至少一种熔融四环衍生物的组合物，以及使用熔融四环衍生物治疗或预防患者HCV感染的方法。

70. 发明授权

US5530125A Synthesis of .alpha.-substituted-aryl ethylamines 失效
标题翻译： α-取代的芳基乙胺的合成
公开(公告)号：US5530125A
公开(公告)日：1996-06-25
申请号：US290894
申请日：1994-08-19
申请人： Joel G. Berger , Wei K. Chang , Joseph A. Kozlowski , Guowei Zhou
发明人： Joel G. Berger , Wei K. Chang , Joseph A. Kozlowski , Guowei Zhou
IPC分类号： C07D217/24 , A61K31/55 , A61P25/00 , A61P25/18 , B01J31/24 , C07B61/00 , C07C231/12 , C07D209/34 , C07D213/56 , C07D223/16 , C07D225/06 , C07D233/64 , C07D277/30 , C07D307/54 , C07D333/24 , C07D491/056
CPC分类号： C07D223/16
摘要： A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.
摘要翻译： PCT No.PCT / US93 / 01425 Sec。 371日期：1994年8月19日 102（e）日期1994年8月19日PCT提交1993年2月23日PCT公布。公开号WO93 / 16997 日期：1993年9月2日。一种制备α-取代芳基乙酰胺的新方法，其中取代基是芳基或1-烯基或1-环烯基，其中氮原子不携带氢原子包括芳基乙酰胺在α-碳原子上具有一个或两个氢原子，其中氮原子不携带氢原子，在惰性非质子有机溶剂中具有强碱，随后与零价过渡金属催化剂反应，然后与式 R4-X，其中R4选自芳族基团，1-烯基和1-环烯基，X是特定的离去基团，特别是三氟甲磺酸酯基团。 α-取代的芳基乙酰胺可用作制备（通过还原）具有药理活性的α-取代的芳基乙胺，例如1-取代-2,3,4,5-四氢-1H-3-苯并氮杂的中间体。其中1-取代基R4是1-（1-环烯基）的某些苯并氮杂是新的。

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