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1. 发明申请

WO2008156715A1 CETP INHIBITORS DERIVED FROM BENZOXAZOLE ARYLAMIDES 审中-公开
标题翻译：苯并噻唑衍生的CETP抑制剂
公开(公告)号：WO2008156715A1
公开(公告)日：2008-12-24
申请号：PCT/US2008/007467
申请日：2008-06-16
申请人： MERCK & CO., INC. , HUNT, Julianne, A. , SWEIS, Ramzi, F. , KIM, Dooseop , KALLASHI, Florida , SINCLAIR, Peter, J.
发明人： HUNT, Julianne, A. , SWEIS, Ramzi, F. , KIM, Dooseop , KALLASHI, Florida , SINCLAIR, Peter, J.
IPC分类号： A01N43/16
CPC分类号： C07D413/14 , C07D413/10 , C07D413/12
摘要： Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems ofthe industrialized world In formula I, A-B is an arylamide moiety
摘要翻译：具有式I结构的化合物，包括化合物的药学上可接受的盐，是有效的CETP（胆固醇酯转移蛋白）抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，并用于治疗或预防动脉粥样硬化。动脉粥样硬化及其临床后果，冠心病（CHD），中风和血管性血管疾病对工业化世界的医疗保健系统来说是一个真正巨大的负担在式I中，AB是芳基酰胺部分

2. 发明申请

WO2003011285A1 BENZIMIDAZO[4,5-f]ISOQUINOLINONE DERIVATIVES 审中-公开
标题翻译：苯并咪唑[4,5-f]异喹啉酮衍生物
公开(公告)号：WO2003011285A1
公开(公告)日：2003-02-13
申请号：PCT/US2002/023876
申请日：2002-07-26
申请人： MERCK & CO., INC. , GOULET, Joung, L. , HONG, Xingfang , SINCLAIR, Peter, J. , THOMPSON, James, E. , CUBBON, Rose, M. , CUMMINGS, Richard, T.
发明人： GOULET, Joung, L. , HONG, Xingfang , SINCLAIR, Peter, J. , THOMPSON, James, E. , CUBBON, Rose, M. , CUMMINGS, Richard, T.
IPC分类号： A61K31/407
CPC分类号： C07D471/04 , A61K31/4745 , C07D471/14
摘要： Benzimidazo[4,5-f]isoquinolinone derivatives are inhibitors of Janus protein tyrosine kinases (Jak), and as such are useful as immunosuppressants, and in the treatment of diseases including asthma, allergies, autoimmune diseases .
摘要翻译：苯并咪唑并[4,5-f]异喹啉酮衍生物是Janus蛋白酪氨酸激酶（Jak）的抑制剂，因此可用作免疫抑制剂，并用于治疗包括哮喘，过敏，自身免疫疾病在内的疾病。

3. 发明申请

WO1993005058A1 O-HETEROARYL, O-ALKYLHETEROARYL, O-ALKENYLHETEROARYL AND O-ALKYNYLHETEROARYLMACROLIDES 审中-公开
标题翻译： O-异丙基，O-烷基乙酰基，O-亚烷基二异氰酸酯和O-亚烷基二异氰酸酯
公开(公告)号：WO1993005058A1
公开(公告)日：1993-03-18
申请号：PCT/US1992007508
申请日：1992-09-02
申请人： MERCK & CO., INC.
发明人： MERCK & CO., INC. , SINCLAIR, Peter, J. , WONG, Frederick , GOULET, Joung , GOULET, Mark , PARSONS, Williams, H. , WYVRATT, Matthew, J.
IPC分类号： C07H19/01
CPC分类号： C07H19/01
摘要： O-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides of general structural formula (I) have been prepared from suitable precursors by alkylation and/or arylation at C-3'' and/or C-4'' of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

4. 发明申请

WO2007081570A2 CHOLESTERYL ESTER TRANSFER PROTEIN INHIBITORS 审中-公开
标题翻译：胆固醇转运蛋白抑制剂
公开(公告)号：WO2007081570A2
公开(公告)日：2007-07-19
申请号：PCT/US2006/049504
申请日：2006-12-29
申请人： MERCK & CO., INC. , ALI, Amjad , SINCLAIR, Peter, J. , TAYLOR, Gayle, E.
发明人： ALI, Amjad , SINCLAIR, Peter, J. , TAYLOR, Gayle, E.
IPC分类号： A61K31/5375 , A61K31/513
CPC分类号： C07D265/10 , C07D413/06
摘要： Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A 1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.
摘要翻译：包括化合物的药学上可接受的盐的式（I）化合物是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式（I）的化合物中，A 1是环状基团，B是直接或通过亚甲基与杂环连接的环状基团。

5. 发明申请

WO2007070173A3 CETP INHIBITORS 审中-公开
公开(公告)号：WO2007070173A3
公开(公告)日：2007-06-21
申请号：PCT/US2006/042208
申请日：2006-10-30
申请人： MERCK & CO., INC. , ALI, Amjad , HUNT, Julianne, A. , KALLASHI, Florida , KOWALCHICK, Jennifer, E. , KIM, Dooseop , SMITH, Cameron, J. , SINCLAIR, Peter, J. , SWEIS, Ramzi, F. , TAYLOR, Gayle, E. , THOMPSON, Christopher, F. , CHEN, Liya , QURAISHI, Nazia
发明人： ALI, Amjad , HUNT, Julianne, A. , KALLASHI, Florida , KOWALCHICK, Jennifer, E. , KIM, Dooseop , SMITH, Cameron, J. , SINCLAIR, Peter, J. , SWEIS, Ramzi, F. , TAYLOR, Gayle, E. , THOMPSON, Christopher, F. , CHEN, Liya , QURAISHI, Nazia
IPC分类号： A61K31/41
摘要： Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. I

6. 发明申请

WO2006014357A1 CETP INHIBITORS 审中-公开
标题翻译： CETP抑制剂
公开(公告)号：WO2006014357A1
公开(公告)日：2006-02-09
申请号：PCT/US2005/023546
申请日：2005-07-01
申请人： MERCK & CO., INC. , ALI, Amjad , NAPOLITANO, Joann, M. , DENG, Qiaolin , LU, Zhijian , SINCLAIR, Peter, J. , TAYLOR, Gayle, E. , THOMPSON, Christopher, F. , QURAISHI, Nazia , SMITH, Cameron, J. , HUNT, Julianne, A.
发明人： ALI, Amjad , NAPOLITANO, Joann, M. , DENG, Qiaolin , LU, Zhijian , SINCLAIR, Peter, J. , TAYLOR, Gayle, E. , THOMPSON, Christopher, F. , QURAISHI, Nazia , SMITH, Cameron, J. , HUNT, Julianne, A.
IPC分类号： C07D263/20
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R 2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalky substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalky substituent connected directly to the ring or attached to the ring through a -CH 2 -.
摘要翻译：具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R 2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基或通过-CH 2 - 2连接到环上。

7. 发明申请

WO2007081571A3 CETP INHIBITORS 审中-公开
公开(公告)号：WO2007081571A3
公开(公告)日：2007-07-19
申请号：PCT/US2006/049505
申请日：2006-12-29
申请人： MERCK & CO., INC. , ALI, Amjad , LU, Zhijian , SINCLAIR, Peter, J. , TAYLOR, Gayle, E. , THOMPSON, Christopher, F. , SMITH, Cameron, J. , DOWST, Adrian, A. , CHEN, Yi-heng
发明人： ALI, Amjad , LU, Zhijian , SINCLAIR, Peter, J. , TAYLOR, Gayle, E. , THOMPSON, Christopher, F. , SMITH, Cameron, J. , DOWST, Adrian, A. , CHEN, Yi-heng
IPC分类号： C07D263/16 , A61K31/421
摘要： Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B or R 2 is a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or R 2 is also a cyclic group.

8. 发明申请

WO2007041494A2 CHOLESTERYL ESTER TRANSFER PROTEIN INHIBITORS 审中-公开
标题翻译：胆固醇转运蛋白抑制剂
公开(公告)号：WO2007041494A2
公开(公告)日：2007-04-12
申请号：PCT/US2006/038435
申请日：2006-09-28
申请人： MERCK & CO., INC. , ALI, Amjad , SINCLAIR, Peter, J.
发明人： ALI, Amjad , SINCLAIR, Peter, J.
IPC分类号： A61K31/55 , A61K31/541
CPC分类号： C07D257/06 , C07D249/04 , C07D261/14 , C07D401/12
摘要： Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A 1 and A 2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring, and Z is an aromatic or heterocyclic ring.
摘要翻译：包括化合物的药学上可接受的盐的式（I）化合物是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式（I）的化合物中，A 1和A 2各自为芳环，5-6元杂环，与杂环稠合的芳环环，与杂环稠合的苯环或环烷基环，Z是芳族或杂环。

9. 发明申请

WO2004026248A2 OCTAHYDRO-2-H-NAPHTHO[1,2-F] INDOLE-4-CARBOXAMIDE DERIVATIVES AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS 审中-公开
标题翻译： OCTAHYDRO-2-H-NAPHTHO [1,2-F]吲哚-4-羧酰胺衍生物作为选择性糖皮质激素受体调节剂
公开(公告)号：WO2004026248A2
公开(公告)日：2004-04-01
申请号：PCT/US2003/029494
申请日：2003-09-17
申请人： MERCK & CO., INC. , ALI, Amjad , ASTER, Susan, D. , BALKOVEC, James, M. , GRAHAM, Donald, W. , HUNT, Julianne, A. , KALLASHI, Florida , SINCLAIR, Peter, J. , TATA, James, R. , TAYLOR, Gayle, E. , GOULET, Joung, L.
发明人： ALI, Amjad , ASTER, Susan, D. , BALKOVEC, James, M. , GRAHAM, Donald, W. , HUNT, Julianne, A. , KALLASHI, Florida , SINCLAIR, Peter, J. , TATA, James, R. , TAYLOR, Gayle, E. , GOULET, Joung, L.
IPC分类号： A61K
CPC分类号： C07J71/0047 , C07D231/54 , C07D401/12 , C07D403/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D491/113
摘要： The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明包括式I化合物或其药学上可接受的盐或水合物，其可用作选择性糖皮质激素受体配体以治疗多种自身免疫性和炎症性疾病或病症。药物组合物和使用方法也包括在内。

10. 发明申请

WO1992020688A1 AMINO O-ARYL, O-ALKYL, O-ALKENYL AND O-ALKYNYL MACROLIDES 审中-公开
标题翻译：氨基O-亚胺基，O-烷基，O-亚苄基和O-烷基亚胺
公开(公告)号：WO1992020688A1
公开(公告)日：1992-11-26
申请号：PCT/US1992003918
申请日：1992-05-11
申请人： MERCK & CO., INC.
发明人： MERCK & CO., INC. , SINCLAIR, Peter, J. , WYVRATT, Matthew, J. , GOULET, Mark , ORGAN, Helen, M.
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： Amino O-aryl, O-alkyl, O-alkenyl and O-alkynyl macrolides of general structural formula (I) have been prepared from suitable precursors by arylation or alkylation and amination at C-3''/C-4'' of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma; as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis; in the reversal of multidrug resistance of tumor cells; in treatment of inflammation of mucosa and blood vessels, gastric ulcers, vascular damage, ischemic bowel disease, inflammatory bowel disease, necrotizing enterocolitis, intestinal lesions associated with thermal burns; in the treatment of cytomegalovirus infection; and in the treatment of idiopathic thrombocytopenic purpura and Basedow's disease.
摘要翻译：通过结构式（I）的氨基O-芳基，O-烷基，O-烯基和O-炔基大环内酯由合适的前体通过芳基化或烷基化和胺化在C-3“/ C-4” 环己基环。这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病和/或预防外来器官移植排斥反应。此外，这些大环内酯类免疫抑制剂可用于局部治疗炎性和过度增生性皮肤病以及免疫介导疾病的皮肤表现。此外，这些大环内酯可用于治疗可逆性阻塞性气道疾病，特别是哮喘; 作为头发活化剂，特别是在治疗男性脱发或脱发性秃发症中，在逆转肿瘤细胞的多药耐药性; 治疗粘膜和血管的炎症，胃溃疡，血管损伤，缺血性肠病，炎性肠病，坏死性小肠结肠炎，与热灼伤相关的肠道损伤; 在治疗巨细胞病毒感染; 并在治疗特发性血小板减少性紫癜和基诺病。

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