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1. 发明授权

US06982251B2 Substituted 2-azetidinones useful as hypocholesterolemic agents 失效
公开(公告)号：US06982251B2
公开(公告)日：2006-01-03
申请号：US10166942
申请日：2002-06-11
申请人： Anima Ghosal , Shmuel Zbaida , Swapan K. Chowdhury , Robert M. Iannucci , Wenqing Feng , Kevin B. Alton , James E. Patrick , Harry R. Davis
发明人： Anima Ghosal , Shmuel Zbaida , Swapan K. Chowdhury , Robert M. Iannucci , Wenqing Feng , Kevin B. Alton , James E. Patrick , Harry R. Davis
IPC分类号： A61K31/7056 , A61K31/397 , A61K31/675 , C07H17/02 , C07D25/08
CPC分类号： A61K31/70 , A61K45/06 , C07H15/26
摘要： Hypocholesterolemic substituted 2-azetidinone compounds of the formula: are disclosed, as well as a methods of lowering cholesterol by administering said compounds, pharmaceutical compositions containing them, and the combination of a substituted 2-azetidinone cholesterol-lowering agent and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis.

2. 发明授权

US07271174B2 Metabolites of tricyclic amides useful for inhibition of G-protein function and methods of treatment of proliferative diseases 失效
标题翻译：用于抑制G蛋白功能的三环酰胺的代谢物和治疗增殖性疾病的方法
公开(公告)号：US07271174B2
公开(公告)日：2007-09-18
申请号：US10874556
申请日：2004-06-23
申请人： Swapan K. Chowdhury , Anima Ghosal , Robert M. Iannucci , Wenqing Feng , Tze-Ming Chan , Shmuel Zbaida , Kevin B. Alton , Ronald J. Doll , Keith P. Minor
发明人： Swapan K. Chowdhury , Anima Ghosal , Robert M. Iannucci , Wenqing Feng , Tze-Ming Chan , Shmuel Zbaida , Kevin B. Alton , Ronald J. Doll , Keith P. Minor
IPC分类号： C07D221/06 , A61K31/435
CPC分类号： C07D401/14
摘要： The present invention relates to metabolites of tricyclic amides, and structurally related compounds, represented by the structural formula (I): and pharmaceutically acceptable isomers, salts, solvates or esters of the compound of formula (I), wherein: R1 is selected from the group consisting of H and ═O; R2-R5 can be the same or different, each being independently selected from the group consisting of H, —OH, halide, —NH2 and ═O; and, the combination solid-dashed lines independently represent either single bonds or double bonds, wherein the number of combination solid-dashed lines that are double bonds is not greater than 2, and when, the double bonds are not adjacent, and when 0, one of R1-R5 is not H. Also disclosed are methods of treatment of proliferative diseases and methods for inhibiting the abnormal growth of cells, and for inhibiting farnesyl protein transferase using the novel compounds.
摘要翻译：本发明涉及由结构式（I）表示的三环酰胺的代谢物和结构相关的化合物：和式（I）化合物的药学上可接受的异构体，盐，溶剂化物或酯，其中：R 1 选自H和-O; R 2 -R 5可以相同或不同，各自独立地选自H，-OH，卤化物，-NH 2， SUB>和-O; 并且，组合虚线独立地表示单键或双键，其中双键的组合实线的数目不大于2，当双键不相邻时，当为0时， R 1〜R 5之一不是H.还公开了治疗增殖性疾病的方法和抑制细胞异常生长的方法，以及用于抑制法呢基蛋白转移酶使用新型化合物。

3. 发明授权

US07312223B2 Metabolite of xanthine Phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction 失效
标题翻译：黄嘌呤的代谢物磷酸二酯酶5抑制剂及其衍生物可用于治疗勃起功能障碍
公开(公告)号：US07312223B2
公开(公告)日：2007-12-25
申请号：US10901574
申请日：2004-07-29
申请人： Anima Ghosal , Wei Tong , Swapan K. Chowdhury , Shmuel Zbaida , Mark A. Wirth , Kevin B. Alton , James E. Patrick , Craig D. Boyle , Andrew Stamford
发明人： Anima Ghosal , Wei Tong , Swapan K. Chowdhury , Shmuel Zbaida , Mark A. Wirth , Kevin B. Alton , James E. Patrick , Craig D. Boyle , Andrew Stamford
IPC分类号： C07D473/06 , A61K31/522 , A61P9/10 , A61P9/12
CPC分类号： C07D473/06
摘要： The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same. Further disclosed are methods of treating a physiological disorder, symptom or disease in a patient, comprising administering to the patient an effective amount of the above compound, wherein the physiological disorder, symptom or disease is a urogenital, cardiovascular, cerebrovascular or peripheral vascular disorder, angina pectoris, hypertension, restenosis post angioplasty, endarterectomy, stent introduction, cerebral stroke, a respiratory tract disorder such as an allergic condition associated with atopy, pulmonary hypertension, an ischemic heart disorder, impaired glucose tolerance, diabetes and its related complication, insulin resistance syndrome, hyperglycemia, polycystic ovarian syndrome, a glomerular disorder, renal insufficiency, nephritis, a tubular interstitial disorder, an autoimmune disorder, glaucoma, intestinal motility, cachexia or cancer.
摘要翻译：本发明涉及具有以下结构衍生物的黄嘌呤磷酸二酯酶5型抑制剂的代谢物及其制剂及其制备方法。进一步公开的是治疗患者的生理障碍，症状或疾病的方法，包括向患者施用有效量的上述化合物，其中所述生理障碍，症状或疾病是泌尿生殖系统，心血管，脑血管或外周血管疾病，心绞痛，高血压，血管成形术后再狭窄，内膜切除术，支架引入，脑中风，呼吸道疾病如与过敏相关的过敏性疾病，肺动脉高压，缺血性心脏病，糖耐量异常，糖尿病及其相关并发症，胰岛素抵抗综合征，高血糖症，多囊卵巢综合征，肾小球疾病，肾功能不全，肾炎，管状间质性疾病，自身免疫性疾病，青光眼，肠蠕动，恶病质或癌症。

4. 发明授权

US07825121B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
公开(公告)号：US07825121B2
公开(公告)日：2010-11-02
申请号：US11255643
申请日：2005-10-21
申请人： Ragulan Ramanathan , Anima Ghosal , Michael W. Miller , Swapan K. Chowdhury , Kevin B. Alton
发明人： Ragulan Ramanathan , Anima Ghosal , Michael W. Miller , Swapan K. Chowdhury , Kevin B. Alton
IPC分类号： A61K31/497 , A01N43/54 , C07D403/00 , C07D239/00
CPC分类号： C07D401/14 , C07D401/06 , C07H17/02
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R4，R5和R7是氢或烷基; R6是氢，烷基或烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

5. 发明申请

US20050026939A1 Metabolite of xanthine phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction 失效
标题翻译：用于治疗勃起功能障碍的黄嘌呤磷酸二酯酶5抑制剂及其衍生物的代谢物
公开(公告)号：US20050026939A1
公开(公告)日：2005-02-03
申请号：US10901574
申请日：2004-07-29
申请人： Anima Ghosal , Wei Tong , Swapan Chowdhury , Shmuel Zbaida , Mark Wirth , Kevin Alton , James Patrick , Craig Boyle , Andrew Stamford
发明人： Anima Ghosal , Wei Tong , Swapan Chowdhury , Shmuel Zbaida , Mark Wirth , Kevin Alton , James Patrick , Craig Boyle , Andrew Stamford
IPC分类号： C07D473/06 , A61K31/522 , C07D473/02
CPC分类号： C07D473/06
摘要： The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same. Further disclosed are methods of treating a physiological disorder, symptom or disease in a patient, comprising administering to the patient an effective amount of the above compound, wherein the physiological disorder, symptom or disease is a urogenital, cardiovascular, cerebrovascular or peripheral vascular disorder, angina pectoris, hypertension, restenosis post angioplasty, endarterectomy, stent introduction, cerebral stroke, a respiratory tract disorder such as an allergic condition associated with atopy, pulmonary hypertension, an ischemic heart disorder, impaired glucose tolerance, diabetes and its related complication, insulin resistance syndrome, hyperglycemia, polycystic ovarian syndrome, a glomerular disorder, renal insufficiency, nephritis, a tubular interstitial disorder, an autoimmune disorder, glaucoma, intestinal motility, cachexia or cancer.
摘要翻译：本发明涉及具有以下结构衍生物的黄嘌呤磷酸二酯酶5型抑制剂的代谢物及其制剂及其制备方法。进一步公开的是治疗患者的生理障碍，症状或疾病的方法，包括向患者施用有效量的上述化合物，其中所述生理障碍，症状或疾病是泌尿生殖系统，心血管，脑血管或外周血管疾病，心绞痛，高血压，血管成形术后再狭窄，内膜切除术，支架引入，脑中风，呼吸道疾病如与过敏相关的过敏性疾病，肺动脉高压，缺血性心脏病，糖耐量异常，糖尿病及其相关并发症，胰岛素抵抗综合征，高血糖症，多囊卵巢综合征，肾小球疾病，肾功能不全，肾炎，管状间质性疾病，自身免疫性疾病，青光眼，肠蠕动，恶病质或癌症。

6. 发明申请

US20070287664A1 Combinations of HCV protease inhibitor(s) and CYP3A4 inhibitor(s), and methods of treatment related thereto 审中-公开
标题翻译： HCV蛋白酶抑制剂和CYP3A4抑制剂的组合以及与之相关的治疗方法
公开(公告)号：US20070287664A1
公开(公告)日：2007-12-13
申请号：US11725518
申请日：2007-03-19
申请人： Robert Ralston , Julie Strizki , Jaromir Vlach , Samir Gupta , Edward O'Mara , Anima Ghosal , Michelle Treitel , James McLeod , Ronald White
发明人： Robert Ralston , Julie Strizki , Jaromir Vlach , Samir Gupta , Edward O'Mara , Anima Ghosal , Michelle Treitel , James McLeod , Ronald White
IPC分类号： A61K38/12 , A61K31/44 , A61P31/00 , C07D221/02
CPC分类号： A61K31/496 , A61K31/16 , A61K31/192 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/427 , A61K31/4965 , A61K38/07 , A61K45/06 , A61K2300/00
摘要： Disclosed are medicaments, pharmaceutical compositions, pharmaceutical kits, and methods based on combinations comprising, separately or together: (a) a CYP3A4 inhibitor; and (b) a HCV protease inhibitor; for concurrent or consecutive administration in treating a human subject infected with HCV.
摘要翻译：公开了药物，药物组合物，药物试剂盒和基于组合的方法，所述组合包括，单独或一起：（a）CYP3A4抑制剂; 和（b）HCV蛋白酶抑制剂; 用于同时或连续给药以治疗感染HCV的人类受试者。

7. 发明申请

US20070232527A1 Medicaments and methods combining a HCV protease inhibitor and an AKR competitor 审中-公开
公开(公告)号：US20070232527A1
公开(公告)日：2007-10-04
申请号：US11502562
申请日：2006-08-10
申请人： Anima Ghosal , Narendra Kishnani , Kevin Alton , Ronald White
发明人： Anima Ghosal , Narendra Kishnani , Kevin Alton , Ronald White
IPC分类号： A61K38/12 , A61K38/04
CPC分类号： A61K38/55 , A61K38/05 , A61K38/06 , A61K45/06 , A61K2300/00
摘要： Disclosed are medicaments, pharmaceutical compositions, pharmaceutical kits, and methods based on combinations of a hepatitis C virus (HCV) protease inhibitor and an aldo-keto reductase (AKR) competitor, for concurrent or consecutive administration in treating, preventing, or ameliorating one or more symptoms of HCV, treating disorders associated with HCV, or inhibiting cathepsin activity in a subject.

8. 发明申请

US20060105964A1 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
公开(公告)号：US20060105964A1
公开(公告)日：2006-05-18
申请号：US11255643
申请日：2005-10-21
申请人： Ragulan Ramanathan , Anima Ghosal , Michael Miller , Swapan Chowdhury , Kevin Alton
发明人： Ragulan Ramanathan , Anima Ghosal , Michael Miller , Swapan Chowdhury , Kevin Alton
IPC分类号： A61K31/7052 , A61K31/513 , A61K31/506 , C07D403/14
CPC分类号： C07D401/14 , C07D401/06 , C07H17/02
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5和R 7是氢或烷基; R 6是氢，烷基或链烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

9. 发明申请

US20060276404A1 Medicaments and methods combining a HCV protease inhibitor and an AKR competitor 审中-公开
标题翻译：结合HCV蛋白酶抑制剂和AKR竞争剂的药物和方法
公开(公告)号：US20060276404A1
公开(公告)日：2006-12-07
申请号：US11443647
申请日：2006-05-31
申请人： Anima Ghosal , Narendra Kishnani , Kevin Alton , Ronald White
发明人： Anima Ghosal , Narendra Kishnani , Kevin Alton , Ronald White
IPC分类号： A61K38/05 , A61K38/04 , A61K31/4709
CPC分类号： A61K38/04 , A61K31/00 , A61K31/19 , A61K31/4709 , A61K38/05 , A61K45/06 , A61K2300/00
摘要： Disclosed are medicaments, pharmaceutical compositions, pharmaceutical kits, and methods based on combinations of a hepatitis C virus (HCV) protease inhibitor and an aldo-keto reductase (AKR) competitor, for concurrent or consecutive administration in treating, preventing, or ameliorating one or more symptoms of HCV, treating disorders associated with HCV, or inhibiting cathepsin activity in a subject.
摘要翻译：公开了药物，药物组合物，药物试剂盒和基于丙型肝炎病毒（HCV）蛋白酶抑制剂和醛酮还原酶（AKR）竞争剂的组合的方法，用于同时或连续施用以治疗，预防或改善其中一种或 HCV的更多症状，治疗与HCV相关的疾病或抑制受试者中的组织蛋白酶活性。

10. 发明申请

US20140162942A1 INHIBITION OF CYP3A DRUG METABOLISM 审中-公开
标题翻译： CYP3A药物代谢的抑制作用
公开(公告)号：US20140162942A1
公开(公告)日：2014-06-12
申请号：US13812221
申请日：2011-07-25
申请人： Anima Ghosal , Samir Gupta , Narendra Kishnani , Claudia Kasserra , Edward O'Mara
发明人： Anima Ghosal , Samir Gupta , Narendra Kishnani , Claudia Kasserra , Edward O'Mara
IPC分类号： A61K38/06 , A61K45/06
CPC分类号： A61K38/06 , A61K38/07 , A61K45/06 , A61K2300/00
摘要： The present invention provides methods, pharmaceutical compositions, medicaments, and pharmaceutical kits that employ the use of boceprevir as a CYP3A4/5 inhibitor to improve the pharmacokinetics of therapeutic compounds metabolized by cytochrome P450 3A4/5 (CYP3A4/5) enzymes.
摘要翻译：本发明提供使用波普瑞韦作为CYP3A4 / 5抑制剂来改善由细胞色素P450 3A4 / 5（CYP3A4 / 5）酶代谢的治疗性化合物的药代动力学的方法，药物组合物，药物和药物试剂盒。

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