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1. 发明申请

WO2006130666A3 MEDICAMENTS AND METHODS COMBINING A HCV PROTEASE INHIBITOR AND AN AKR COMPETITOR 审中-公开
标题翻译：组合HCV蛋白酶抑制剂和AKR竞争者的药物和方法
公开(公告)号：WO2006130666A3
公开(公告)日：2007-06-21
申请号：PCT/US2006021083
申请日：2006-05-31
申请人： SCHERING CORP , GHOSAL ANIMA , KISHNANI NARENDRA S , ALTON KEVIN B , WHITE RONALD E
发明人： GHOSAL ANIMA , KISHNANI NARENDRA S , ALTON KEVIN B , WHITE RONALD E
IPC分类号： A61K38/04 , A61K31/00 , A61K31/19 , A61K31/192 , A61K38/21 , A61P31/12
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。

2. 发明申请

WO2006130666A2 MEDICAMENTS AND METHODS COMBINING A HCV PROTEASE INHIBITOR AND AN AKR COMPETITOR 审中-公开
标题翻译：组合HCV蛋白酶抑制剂和AKR竞争者的药物和方法
公开(公告)号：WO2006130666A2
公开(公告)日：2006-12-07
申请号：PCT/US2006/021083
申请日：2006-05-31
申请人： SCHERING CORPORATION , GHOSAL, Anima , KISHNANI, Narendra, S. , ALTON, Kevin, B. , WHITE, Ronald, E.
发明人： GHOSAL, Anima , KISHNANI, Narendra, S. , ALTON, Kevin, B. , WHITE, Ronald, E.
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。

3. 发明申请

WO2005012303A1 METABOLITE OF XANTHINE PHOSPHODIESTERASE 5 INHIBITOR AND DERIVATIVES THEREOF USEFUL FOR TREATMENT OF ERECTILE DYSFUNCTION 审中-公开
标题翻译： XANTHINE磷酸二酯酶5抑制剂及其衍生物的代谢物有用于治疗溃疡性功能障碍
公开(公告)号：WO2005012303A1
公开(公告)日：2005-02-10
申请号：PCT/US2004/024525
申请日：2004-07-29
申请人： SCHERING CORPORATION , GHOSAL, Anima , TONG, Wei , CHOWDHURY, Swapan, K. , ZBAIDA, Shmuel , WIRTH, Mark, A. , ALTON, Kevin, B. , PATRICK, James, E. , BOYLE, Craig, D. , STAMFORD, Andrew
发明人： GHOSAL, Anima , TONG, Wei , CHOWDHURY, Swapan, K. , ZBAIDA, Shmuel , WIRTH, Mark, A. , ALTON, Kevin, B. , PATRICK, James, E. , BOYLE, Craig, D. , STAMFORD, Andrew
IPC分类号： C07D473/06
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. 发明申请

WO2005003120A3 METABOLITES OF TRICYCLIC AMIDES USEFUL FOR INHIBITION OF G-PROTEIN FUNCTION AND METHODS OF TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
公开(公告)号：WO2005003120A3
公开(公告)日：2005-01-13
申请号：PCT/US2004/020032
申请日：2004-06-23
申请人： SCHERING CORPORATION , CHOWDHURY, Swapan, K. , GHOSAL, Anima , IANNUCCI, Robert, M. , FENG, Wenqing , CHAN, Tze-Ming , ZBAIDA, Shmuel , ALTON, Kevin, B. , DOLL, Ronald, J. , MINOR, Keith, P.
发明人： CHOWDHURY, Swapan, K. , GHOSAL, Anima , IANNUCCI, Robert, M. , FENG, Wenqing , CHAN, Tze-Ming , ZBAIDA, Shmuel , ALTON, Kevin, B. , DOLL, Ronald, J. , MINOR, Keith, P.
IPC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: R 1 is selected from the group consisting of H and =O; R 2 -R 5 can be the same or different, each being independently selected from the group consisting of H, -OH, halide, -NH 2 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 2, the double bonds are not adjacent, and when 0, one of R 1 -R 5 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.

5. 发明申请

WO2007100739A1 CCR5 ANTAGONISTS USEFUL FOR TREATING HIV 审中-公开
标题翻译： CCR5有效治疗艾滋病毒的拮抗剂
公开(公告)号：WO2007100739A1
公开(公告)日：2007-09-07
申请号：PCT/US2007/004859
申请日：2007-02-22
申请人： SCHERING CORPORATION , RAMANATHAN, Ragulan , MILLER, Michael, W. , CHOWDHURY, Swapan, K. , ALTON, Kevin, B. , GROTZ, Diane , RINDGEN, Diane , TENDOLKAR, Amol
发明人： RAMANATHAN, Ragulan , MILLER, Michael, W. , CHOWDHURY, Swapan, K. , ALTON, Kevin, B. , GROTZ, Diane , RINDGEN, Diane , TENDOLKAR, Amol
IPC分类号： C07D401/14 , C07D403/06 , C07D409/14 , C07D417/14
CPC分类号： C07D401/14 , C07D409/14
摘要： In its many embodiments, the present invention provides a novel class of compounds of structural formula I [Chemical formula should be inserted here as it appears on abstract in paper form.] as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with CCR5 using such compounds or pharmaceutical compositions. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的结构式I的化合物[作为CCR5受体的抑制剂的化学式应该被插入到这里，它以纸的形式抽象出来]，制备这些化合物的方法，药物组合物含有一种或多种这样的化合物，制备包含一种或多种这样的化合物的药物制剂的方法，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CCR5相关的一种或多种疾病的方法。本发明还涉及本发明化合物与一种或多种可用于治疗人类免疫缺陷病毒（HIV）的抗病毒剂或其它药剂的组合的用途。本发明还涉及本发明化合物单独或与另一种药剂组合用于治疗实体器官移植排斥，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。

6. 发明申请

WO2007050375A2 PIPERAZINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS 审中-公开
标题翻译：哌嗪衍生物作为CCR5拮抗剂有用
公开(公告)号：WO2007050375A2
公开(公告)日：2007-05-03
申请号：PCT/US2006/040636
申请日：2006-10-18
申请人： SCHERING CORPORATION , RAMANTHAN, Ragulan , GHOSAL, Anima , MILLER, Michael, W. , CHOWDHURY, Swapan, K. , ALTON, Kevin, B.
发明人： RAMANTHAN, Ragulan , GHOSAL, Anima , MILLER, Michael, W. , CHOWDHURY, Swapan, K. , ALTON, Kevin, B.
IPC分类号： C07D401/14 , C07H17/02 , A61K31/506 , A61P31/18 , A61P37/06
CPC分类号： C07D401/14 , C07D401/06 , C07H17/02
摘要： The use of CCR5 antagonists of the formula (Chemical formula I ). 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：使用式（化学式I）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。

7. 发明申请

WO2007050375A3 PIPERAZINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS 审中-公开
标题翻译：哌嗪衍生物作为CCR5拮抗剂有用
公开(公告)号：WO2007050375A3
公开(公告)日：2007-06-14
申请号：PCT/US2006040636
申请日：2006-10-18
申请人： SCHERING CORP , RAMANTHAN RAGULAN , GHOSAL ANIMA , MILLER MICHAEL W , CHOWDHURY SWAPAN K , ALTON KEVIN B
发明人： RAMANTHAN RAGULAN , GHOSAL ANIMA , MILLER MICHAEL W , CHOWDHURY SWAPAN K , ALTON KEVIN B
IPC分类号： C07D401/14 , A61K31/506 , A61P31/18 , A61P37/06 , C07H17/02
CPC分类号： C07D401/14 , C07D401/06 , C07H17/02
摘要： CCR5 antagonists having the following core structure Formula (I) (AA) are claimed, 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 .
摘要翻译：要求具有以下核心结构式（I）（AA）的CCR5拮抗剂用于治疗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，炎性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化。

8. 发明申请

WO2005003120A2 METABOLITES OF TRICYCLIC AMIDES USEFUL FOR INHIBITION OF G-PROTEIN FUNCTION AND METHODS OF TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于抑制G蛋白功能的三酰胺的代谢和治疗增殖性疾病的方法
公开(公告)号：WO2005003120A2
公开(公告)日：2005-01-13
申请号：PCT/US2004020032
申请日：2004-06-23
申请人： SCHERING CORP , CHOWDHURY SWAPAN K , GHOSAL ANIMA , IANNUCCI ROBERT M , FENG WENQING , CHAN TZE-MING , ZBAIDA SHMUEL , ALTON KEVIN B , DOLL RONALD J , MINOR KEITH P
发明人： CHOWDHURY SWAPAN K , GHOSAL ANIMA , IANNUCCI ROBERT M , FENG WENQING , CHAN TZE-MING , ZBAIDA SHMUEL , ALTON KEVIN B , DOLL RONALD J , MINOR KEITH P
IPC分类号： A61P35/00 , C07D401/14 , A61K31/4545
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 2, 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）表示的三环酰胺和结构相关化合物的代谢物和式（I）化合物的药学上可接受的异构体，盐，溶剂合物或酯，其中：R1选自由H和= O组成; 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和= O; 并且组合实线独立地表示单键或双键，其中作为双键的组合实线的数目不大于2，当2表示双键不相邻时，当0表示0时 R1-R5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，以及使用新化合物抑制法呢基蛋白转移酶。

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