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1. 发明申请

WO2006114774A3 PYRIMIDINE DERIVATIVES AND THEIR USE AS P2Y12 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡嗪衍生物及其作为P2Y12受体拮抗剂的用途
公开(公告)号：WO2006114774A3
公开(公告)日：2007-02-08
申请号：PCT/IB2006051318
申请日：2006-04-27
申请人： ACTELION PHARMACEUTICALS LTD , CAROFF EVA , FRETZ HEINZ , HILPERT KURT , HOUILLE OLIVIER , HUBLER FRANCIS , MEYER EMMANUEL
发明人： CAROFF EVA , FRETZ HEINZ , HILPERT KURT , HOUILLE OLIVIER , HUBLER FRANCIS , MEYER EMMANUEL
IPC分类号： C07K5/078 , A61K38/05 , A61P9/10
CPC分类号： C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D401/04 , C07D403/04
摘要： The invention relates to 4-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. Formule (I).
摘要翻译：本发明涉及4-氨基羰基 - 嘧啶衍生物及其作为P2Y12受体拮抗剂用于治疗和/或预防和/或治疗心血管和脑血管疾病的内脏，肝和肾血管的外周血管，与血小板聚集相关的病症，包括人类和其他哺乳动物的血栓形成。 Formule（I）。

2. 发明申请

WO2005002574A1 PYRAZOLIDINEDIONE DERIVATIVES AND THEIR USE AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：吡唑啉酮衍生物及其作为抗肿瘤抑制剂的用途
公开(公告)号：WO2005002574A1
公开(公告)日：2005-01-13
申请号：PCT/EP2003/006616
申请日：2003-06-24
申请人： ACTELION PHARMACEUTICALS LTD , HOUILLE, Olivier , FRETZ, Heinz , HILPERT, Kurt , RIEDERER, Markus , GILLER, Thomas , VALDENAIRE, Olivier
发明人： HOUILLE, Olivier , FRETZ, Heinz , HILPERT, Kurt , RIEDERER, Markus , GILLER, Thomas , VALDENAIRE, Olivier
IPC分类号： A61K31/4152
CPC分类号： C07D401/04 , A61K31/4152 , A61K31/4155 , C07C45/00 , C07C45/62 , C07C45/673 , C07C45/68 , C07C45/71 , C07C47/542 , C07C47/548 , C07C47/565 , C07C47/575 , C07C309/65 , C07C2601/08 , C07D231/32
摘要： Pyrazolidinedione derivatives of the general formula (I), wherein R 1 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl; and R 2 is aryl or heteroaryl; tautomers thereof; geometric isomers thereof and tautomers of these geometric isomers, including mixtures of individual compounds of formula (I), or tautomers thereof, and their geometric isomers, or tautomers thereof; pharmaceutically acceptable acid addition salts of compounds which are basic; pharmaceutically acceptable salts of compounds containing acidic groups with bases; pharmaceutically acceptable esters of compounds containing hydroxy or carboxy groups; prodrugs of compounds in which a prodrug forming group is present; as well as hydrates or solvates thereof; are active as platelet adenosine diphosphate receptor antagonists and can be used for the prevention and/or treatment of peripheral vascular, of visceral-, hepaticand renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, particularly thrombosis, and, respectively, for the manufacture of corresponding medicaments. Some, albeit not all, of the compounds of the above formula (I) are novel.
摘要翻译：通式（I）的吡唑烷二酮衍生物，其中R 1是氢，任选取代的烷基，环烷基，芳基，芳基烷基，杂芳基或杂芳基烷基; 并且R 2是芳基或杂芳基; 互变异构体其几何异构体和这些几何异构体的互变异构体，包括式（I）的单独化合物或其互变异构体的混合物及其几何异构体或互变异构体; 碱性化合物的药学上可接受的酸加成盐; 含有酸性基团的化合物的药学上可接受的盐与碱; 含有羟基或羧基的化合物的药学上可接受的酯; 其中存在前药形成基团的化合物的前药; 以及其水合物或溶剂合物; 作为血小板二磷酸腺苷受体拮抗剂是有活性的，可用于预防和/或治疗心血管和脑血管疾病或与血小板聚集特别是血栓形成相关的病症的内脏，肝和肾血管的外周血管，分别用于制造相应的药物。一些（尽管不是全部）上述式（I）的化合物是新的。

3. 发明申请

WO2006114774A2 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO2006114774A2
公开(公告)日：2006-11-02
申请号：PCT/IB2006/051318
申请日：2006-04-27
申请人： ACTELION PHARMACEUTICALS LTD , CAROFF, Eva , FRETZ, Heinz , HILPERT, Kurt , HOUILLE, Olivier , HUBLER, Francis , MEYER, Emmanuel
发明人： CAROFF, Eva , FRETZ, Heinz , HILPERT, Kurt , HOUILLE, Olivier , HUBLER, Francis , MEYER, Emmanuel
CPC分类号： C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D401/04 , C07D403/04
摘要： The invention relates to 4-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
摘要翻译：本发明涉及4-氨基羰基 - 嘧啶衍生物及其作为P2Y12受体拮抗剂用于治疗和/或预防和/或治疗心血管和脑血管疾病的内脏，肝和肾血管的外周血管，与血小板聚集相关的病症，包括人类和其他哺乳动物的血栓形成。

4. 发明申请

WO2005000281A3 PYRAZOLIDINEDIONE DERIVATIVES AND THEIR USE AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：吡唑啉酮衍生物及其作为抗肿瘤抑制剂的用途
公开(公告)号：WO2005000281A3
公开(公告)日：2005-04-14
申请号：PCT/EP2004006471
申请日：2004-06-16
申请人： ACTELION PHARMACEUTICALS LTD , HOUILLE OLIVIER , FRETZ HEINZ , HILPERT KURT , RIEDERER MARKUS , GILLER THOMAS , VALDENAIRE OLIVER
发明人： HOUILLE OLIVIER , FRETZ HEINZ , HILPERT KURT , RIEDERER MARKUS , GILLER THOMAS , VALDENAIRE OLIVER
IPC分类号： A61K31/4152 , A61K31/4155 , A61P7/02 , C07C45/00 , C07C45/62 , C07C45/67 , C07C45/68 , C07C45/71 , C07C47/542 , C07C47/548 , C07C47/565 , C07C47/575 , C07C309/65 , C07D231/32 , C07D401/04 , C07D231/34 , C07D231/36
CPC分类号： C07D401/04 , A61K31/4152 , A61K31/4155 , C07C45/00 , C07C45/62 , C07C45/673 , C07C45/68 , C07C45/71 , C07C47/542 , C07C47/548 , C07C47/565 , C07C47/575 , C07C309/65 , C07C2601/08 , C07D231/32
摘要： Pyrazolidinedione derivatives of the general formula (I), wherein R1 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl or alkanoyl; and R2 is aryl or heteroaryl; tautomers thereof; geometric isomers thereof and tautomers of these geometric isomers, including mixtures of individual compounds of formula (I), or tautomers thereof, and their geometric isomers, or tautomers thereof, pharmaceutically acceptable acid addition salts of compounds which are basic; pharmaceutically acceptable salts of compounds containing acidic groups with bases; pharmaceutically acceptable esters of compounds containing hydroxy or carboxy groups; prodrugs of compounds in which a prodrug forming group is present; as well as hydrates or solvates thereof; are active as platelet adenosine diphosphate receptor antagonists and can be used for the prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, particularly thrombosis, and, respectively, for the manufacture of corresponding medicaments. Some, albeit not all, of the compounds of the above formula (I) are novel.
摘要翻译：通式（I）的吡唑烷二酮衍生物，其中R 1是氢，任选取代的烷基，环烷基，芳基，芳基烷基，杂芳基，杂芳基烷基或烷酰基; 并且R 2是芳基或杂芳基; 互变异构体其几何异构体和这些几何异构体的互变异构体，包括式（I）的单独化合物或其互变异构体的混合物及其几何异构体或互变异构体，其为碱性化合物的药学上可接受的酸加成盐; 含有酸性基团的化合物的药学上可接受的盐与碱; 含有羟基或羧基的化合物的药学上可接受的酯; 其中存在前药形成基团的化合物的前药; 以及其水合物或溶剂合物; 作为血小板二磷酸腺苷受体拮抗剂是有活性的，可用于预防和/或治疗心血管和脑血管疾病或与血小板聚集相关的病症，特别是血栓形成的内脏，肝和肾血管的周围血管，分别用于制造相应的药物。一些（尽管不是全部）上述式（I）的化合物是新的。

5. 发明申请

WO2005000281A2 PYRAZOLIDINEDIONE DERIVATIVES 审中-公开
标题翻译：吡咯烷酮衍生物
公开(公告)号：WO2005000281A2
公开(公告)日：2005-01-06
申请号：PCT/EP2004/006471
申请日：2004-06-16
申请人： ACTELION PHARMACEUTICALS LTD. , HOUILLE, Olivier , FRETZ, Heinz , HILPERT, Kurt , RIEDERER, Markus , GILLER, Thomas , VALDENAIRE, Oliver
发明人： HOUILLE, Olivier , FRETZ, Heinz , HILPERT, Kurt , RIEDERER, Markus , GILLER, Thomas , VALDENAIRE, Oliver
IPC分类号： A61K31/00
CPC分类号： C07D401/04 , A61K31/4152 , A61K31/4155 , C07C45/00 , C07C45/62 , C07C45/673 , C07C45/68 , C07C45/71 , C07C47/542 , C07C47/548 , C07C47/565 , C07C47/575 , C07C309/65 , C07C2601/08 , C07D231/32
摘要： Pyrazolidinedione derivatives of the general formula (I), wherein R 1 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl or alkanoyl; and R 2 is aryl or heteroaryl; tautomers thereof; geometric isomers thereof and tautomers of these geometric isomers, including mixtures of individual compounds of formula (I), or tautomers thereof, and their geometric isomers, or tautomers thereof, pharmaceutically acceptable acid addition salts of compounds which are basic; pharmaceutically acceptable salts of compounds containing acidic groups with bases; pharmaceutically acceptable esters of compounds containing hydroxy or carboxy groups; prodrugs of compounds in which a prodrug forming group is present; as well as hydrates or solvates thereof; are active as platelet adenosine diphosphate receptor antagonists and can be used for the prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, particularly thrombosis, and, respectively, for the manufacture of corresponding medicaments. Some, albeit not all, of the compounds of the above formula (I) are novel.
摘要翻译：通式（I）的吡唑烷二酮衍生物，其中R 1是氢，任选取代的烷基，环烷基，芳基，芳基烷基，杂芳基，杂芳基烷基或烷酰基; 并且R 2是芳基或杂芳基; 互变异构体其几何异构体和这些几何异构体的互变异构体，包括式（I）的单独化合物或其互变异构体的混合物及其几何异构体或其互变异构体，其为碱性化合物的药学上可接受的酸加成盐; 含有酸性基团的化合物的药学上可接受的盐与碱; 含有羟基或羧基的化合物的药学上可接受的酯; 其中存在前药形成基团的化合物的前药; 以及其水合物或溶剂合物; 作为血小板二磷酸腺苷受体拮抗剂是有活性的，可用于预防和/或治疗心血管和脑血管疾病或与血小板聚集相关的病症，特别是血栓形成的内脏，肝和肾血管的周围血管，分别用于制造相应的药物。一些（尽管不是全部）上述式（I）的化合物是新的。

6. 发明申请

WO2003000688A1 AZAINDOLES 审中-公开
标题翻译：氮杂吲哚
公开(公告)号：WO2003000688A1
公开(公告)日：2003-01-03
申请号：PCT/GB2002/002799
申请日：2002-06-20
申请人： AVENTIS PHARMA LIMITED , COX, Paul, Joseph , MAJID, Tahir, Nadeem , LAI, Justine, Yeun, Quai , MORLEY, Andrew , AMENDOLA, Shelley , DEPRETS, Stephanie, Daniele , EDLIN, Chris , GARDNER, Charles, J. , KOMINOS, Dorothea , PEDGRIFT, Brian, Leslie , HALLEY, Frank , GILLESPY, Timothy, Alan , EDWARDS, Michael , CLERC, Francois, Frederic , NEMECEK, Conception , HOUILLE, Olivier , DAMOUR, Dominique , BOUCHARD, Hervé , BEZARD, Daniel , CARREZ, Chantal
发明人： COX, Paul, Joseph , MAJID, Tahir, Nadeem , LAI, Justine, Yeun, Quai , MORLEY, Andrew , AMENDOLA, Shelley , DEPRETS, Stephanie, Daniele , EDLIN, Chris , GARDNER, Charles, J. , KOMINOS, Dorothea , PEDGRIFT, Brian, Leslie , HALLEY, Frank , GILLESPY, Timothy, Alan , EDWARDS, Michael , CLERC, Francois, Frederic , NEMECEK, Conception , HOUILLE, Olivier , DAMOUR, Dominique , BOUCHARD, Hervé , BEZARD, Daniel , CARREZ, Chantal
IPC分类号： C07D471/04
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04
摘要： The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译：本发明涉及通式（I）的生理活性化合物：和含有这些化合物的组合物; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

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