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1. 发明申请

WO2012082436A3 MODULATORS OF HISTONE METHYLTRANSFERASE, AND METHODS OF USE THEREOF 审中-公开
标题翻译： HISTONE甲基转移酶的调节剂及其使用方法
公开(公告)号：WO2012082436A3
公开(公告)日：2012-09-20
申请号：PCT/US2011063309
申请日：2011-12-05
申请人： EPIZYME INC , CHESWORTH RICHARD , KUNTZ KEVIN WAYNE , OLHAVA EDWARD JAMES , PATANE MICHAEL A
发明人： CHESWORTH RICHARD , KUNTZ KEVIN WAYNE , OLHAVA EDWARD JAMES , PATANE MICHAEL A
IPC分类号： C07H19/16 , A61K31/7076 , A61P35/00 , C07D473/34 , C07H19/167
CPC分类号： C07H19/16 , C07D473/34 , C07H19/167
摘要： Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.
摘要翻译：公开了化合物，含有这些化合物的药物组合物，以及化合物和组合物作为组蛋白甲基转移酶调节剂的用途，以及用于治疗受组蛋白甲基转移酶活性调节影响的疾病。

2. 发明申请

WO2003037271A2 COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREFOR 审中-公开
标题翻译：化合物，药物组合物及其使用方法
公开(公告)号：WO2003037271A2
公开(公告)日：2003-05-08
申请号：PCT/US2002/034845
申请日：2002-10-30
申请人： MILLENNIUM PHARMACEUTICALS, INC. , GHOSH, Shomir , PATANE, Michael, A. , CARSON, Kenneth, G. , CHI, I-Cheng, Shannon , YE, Qing , ELDER, Amy, M. , JENKINS, Tracy, J.
发明人： GHOSH, Shomir , PATANE, Michael, A. , CARSON, Kenneth, G. , CHI, I-Cheng, Shannon , YE, Qing , ELDER, Amy, M. , JENKINS, Tracy, J.
IPC分类号： A61K
CPC分类号： C07D223/16 , C04B35/632 , C07D205/04 , C07D207/14 , C07D211/26 , C07D211/28 , C07D211/52 , C07D211/56 , C07D211/58 , C07D211/62 , C07D243/08 , C07D295/185 , C07D295/205 , C07D295/26 , C07D295/30 , C07D295/32 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D405/04 , C07D409/12 , C07D413/04 , C07D413/10 , C07D417/04 , C07D471/10 , C07D491/10
摘要： The invention relates to compounds having the formula (I). Preferred compounds are antagonists of C-C chemokine receptor 8. The invention also relates to a method for treating a subjected having an inflammatory disorder or viral disorder comprising administering to a subject in need thereof an effective amount of a compound of the invention.
摘要翻译：本发明涉及具有式（I）的化合物。优选的化合物是C-C趋化因子受体8的拮抗剂。本发明还涉及用于治疗患有炎性病症或病毒病症的受治疗者的方法，包括向有需要的受试者施用有效量的本发明化合物。

3. 发明申请

WO1997021687A1 PROCESS FOR MAKING DIHYDROPYRIMIDINONES 审中-公开
标题翻译：制备二氢嘧啶酮的方法
公开(公告)号：WO1997021687A1
公开(公告)日：1997-06-19
申请号：PCT/US1996019651
申请日：1996-12-12
申请人： MERCK & CO., INC. , HU, Essa, H. , SIDLER, Daniel, R. , DOLLING, Ulf, H. , PATANE, Michael, A.
发明人： MERCK & CO., INC.
IPC分类号： C07D239/36
CPC分类号： C07D239/22
摘要： The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a beta -keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu2O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.
摘要翻译：本发明提供了通过将β-酮酯或二酮组合形成5-（烷基或烷氧基）羰基-6-烷基-4-（芳基或烷基）-3,4-2（1H） - 二氢嘧啶酮的方法，醛和尿素在硼试剂，金属盐（例如Cu 2 O）和催化剂（例如酸）的存在下进行。该反应通常在一锅中在溶剂中进行，以更高的产率提供二氢嘧啶酮，并且比以前已知的方法更容易处理。

4. 发明申请

WO1997018209A1 ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO1997018209A1
公开(公告)日：1997-05-22
申请号：PCT/US1996018346
申请日：1996-11-12
申请人： MERCK & CO., INC. , BOCK, Mark, G. , PATANE, Michael, A.
发明人： MERCK & CO., INC.
IPC分类号： C07D417/06
CPC分类号： C07D275/06 , C07D295/13
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为选择性α1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

5. 发明申请

WO1996040135A1 ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO1996040135A1
公开(公告)日：1996-12-19
申请号：PCT/US1996009363
申请日：1996-06-04
申请人： MERCK & CO., INC. , PATANE, Michael, A. , BOCK, Mark, G. , FREIDINGER, Roger, M.
发明人： MERCK & CO., INC.
IPC分类号： A61K31/445
CPC分类号： C07D417/06 , A61K31/58 , C07D211/60 , A61K31/50 , A61K31/44 , A61K2300/00
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha-1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为选择性α-1a肾上腺素能受体拮抗剂的用途。这些化合物的一种应用是治疗良性前列腺增生。这些化合物在能够松弛富含α-1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个效用是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人类5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，从而实现了从良性前列腺增生的作用的急性和慢性缓解。

6. 发明申请

WO2012075500A2 7-DEAZAPURINE MODULATORS OF HISTONE METHYLTRANSFERASE, AND METHODS OF USE THEREOF 审中-公开
标题翻译：组蛋白甲基转移酶7-脱氧胞苷调节剂及其使用方法
公开(公告)号：WO2012075500A2
公开(公告)日：2012-06-07
申请号：PCT/US2011/063314
申请日：2011-12-05
申请人： EPIZYME, INC. , CHESWORTH, Richard , KUNTZ, Kevin, Wayne , OLHAVA, Edward, James , PATANE, Michael, A.
发明人： CHESWORTH, Richard , KUNTZ, Kevin, Wayne , OLHAVA, Edward, James , PATANE, Michael, A.
IPC分类号： C07H19/14 , C07D487/04 , C07D405/14 , A61K31/7052 , A61K31/519 , A61P35/00 , A61P25/28
CPC分类号： C07H19/14 , C07D487/04
摘要： Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransf erases, and methods for treating diseases influenced by modulation of histone methyltransferase activity.
摘要翻译：公开了化合物，含有所述化合物的药物组合物，所述化合物和组合物作为组蛋白甲基转移酶调节剂的用途，以及治疗受组蛋白甲基转移酶活性调节影响的疾病的方法。

7. 发明申请

WO2007142986A3 AMINOTHIAZOLE DERIVATIVES AND THEIR USES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：氨基噻唑衍生物及其作为抗菌剂
公开(公告)号：WO2007142986A3
公开(公告)日：2008-04-10
申请号：PCT/US2007012768
申请日：2007-05-30
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , LAMARCHE MATTHEW J , BUSHELL SIMON , PATANE MICHAEL A , WHITEHEAD LEWIS
发明人： LAMARCHE MATTHEW J , BUSHELL SIMON , PATANE MICHAEL A , WHITEHEAD LEWIS
IPC分类号： C07K5/06 , A61K38/00 , A61P31/00
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.
摘要翻译：本申请描述了可用于治疗，预防和/或改善疾病的有机化合物。

8. 发明申请

WO2007142986A2 AMINOTHIAZOLES AND THEIR USES 审中-公开
标题翻译：氨基酸及其用途
公开(公告)号：WO2007142986A2
公开(公告)日：2007-12-13
申请号：PCT/US2007/012768
申请日：2007-05-30
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , LAMARCHE, Matthew, J. , BUSHELL, Simon , PATANE, Michael, A. , WHITEHEAD, Lewis
发明人： LAMARCHE, Matthew, J. , BUSHELL, Simon , PATANE, Michael, A. , WHITEHEAD, Lewis
IPC分类号： C07K5/06 , A61K38/00 , A61P31/00
CPC分类号： C07K5/06139 , A61K38/00 , Y02A50/473
摘要： The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.
摘要翻译：本申请描述了可用于治疗，预防和/或改善疾病的有机化合物。

9. 发明申请

WO2006041773A3 LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
公开(公告)号：WO2006041773A3
公开(公告)日：2006-04-20
申请号：PCT/US2005/035458
申请日：2005-10-03
申请人： MILLENNIUM PHARMACEUTICALS, INC. , BLACKBURN, Christopher , CLAIBORNE, Christopher, F. , CULLIS, Courtney, A. , DALES, Natalie, A. , PATANE, Michael, A. , STIRLING, Matthew , STRADELLA, Omar, G. , WEATHERHEAD, Gabriel, S.
发明人： BLACKBURN, Christopher , CLAIBORNE, Christopher, F. , CULLIS, Courtney, A. , DALES, Natalie, A. , PATANE, Michael, A. , STIRLING, Matthew , STRADELLA, Omar, G. , WEATHERHEAD, Gabriel, S.
IPC分类号： C07D487/04 , A61K31/55
摘要： The present invention provides novel compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A, R e , R b , R c , R d , G 1 , Y 1 , and Y 2 have the meaning as given in the claims useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

10. 发明申请

WO03037271A3 COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREFOR 审中-公开
标题翻译：化合物，药物组合物及其使用方法
公开(公告)号：WO03037271A3
公开(公告)日：2003-10-16
申请号：PCT/US0234845
申请日：2002-10-30
申请人： MILLENNIUM PHARM INC , GHOSH SHOMIR , PATANE MICHAEL A , CARSON KENNETH G , CHI I-CHENG SHANNON , YE QING , ELDER AMY M , JENKINS TRACY J
发明人： GHOSH SHOMIR , PATANE MICHAEL A , CARSON KENNETH G , CHI I-CHENG SHANNON , YE QING , ELDER AMY M , JENKINS TRACY J
IPC分类号： A61K31/445 , A61K31/495 , A61K31/55 , C07D205/04 , C07D207/14 , C07D211/26 , C07D211/28 , C07D211/52 , C07D211/56 , C07D211/58 , C07D211/62 , C07D223/16 , C07D243/08 , C07D295/185 , C07D295/205 , C07D295/26 , C07D295/30 , C07D295/32 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D405/04 , C07D409/12 , C07D413/04 , C07D413/10 , C07D417/04 , C07D471/10 , C07D471/18 , C07D491/10 , C07D498/10 , A61K31/438 , A61K31/4468 , A61K31/4535 , A61K31/454
CPC分类号： C07D223/16 , C04B35/632 , C07D205/04 , C07D207/14 , C07D211/26 , C07D211/28 , C07D211/52 , C07D211/56 , C07D211/58 , C07D211/62 , C07D243/08 , C07D295/185 , C07D295/205 , C07D295/26 , C07D295/30 , C07D295/32 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D405/04 , C07D409/12 , C07D413/04 , C07D413/10 , C07D417/04 , C07D471/10 , C07D491/10
摘要： The invention relates to compounds having the formula (I). Preferred compounds are antagonists of C-C chemokine receptor 8. The invention also relates to a method for treating a subjected having an inflammatory disorder or viral disorder comprising administering to a subject in need thereof an effective amount of a compound of the invention.
摘要翻译：本发明涉及具有式（I）的化合物。优选的化合物是CC趋化因子受体8的拮抗剂。本发明还涉及用于治疗患有炎性病症或病毒性病症的方法，所述方法包括向有需要的受试者施用有效量的本发明化合物。

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