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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

WO2010116328A2 6-(3-AZA-BICYCLO[3.1.0]HEX-3-YL)-2-PHENYL-PYRIMIDINES 审中-公开
标题翻译： 6-（3-氮杂 - 二环[3.1.0]己-3-基）-2-苯基 - 嘧啶
公开(公告)号：WO2010116328A2
公开(公告)日：2010-10-14
申请号：PCT/IB2010051499
申请日：2010-04-07
申请人： ACTELION PHARMACEUTICALS LTD , CAROFF EVA , HILPERT KURT , HUBLER FRANCIS , MEYER EMMANUEL , RENNEBERG DORTE
发明人： CAROFF EVA , HILPERT KURT , HUBLER FRANCIS , MEYER EMMANUEL , RENNEBERG DORTE
IPC分类号： C07D403/14
CPC分类号： C07D403/14 , A61K31/506
摘要： The present invention relates to 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention 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6-（3-氮杂 - 双环[3.1.0]己-3-基）-2-苯基 - 嘧啶衍生物及其作为P2Y12受体拮抗剂治疗和/或预防外周血管的用途内脏，肝和肾血管，心血管和脑血管疾病或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。

3. 发明申请

WO2010046869A3 TETRAHYDRONAPHTHALENE COMPOUNDS 审中-公开
标题翻译：四氢萘醌化合物
公开(公告)号：WO2010046869A3
公开(公告)日：2010-06-17
申请号：PCT/IB2009054668
申请日：2009-10-22
申请人： ACTELION PHARMACEUTICALS LTD , HILPERT KURT , HUBLER FRANCIS , RENNEBERG DORTE
发明人： HILPERT KURT , HUBLER FRANCIS , RENNEBERG DORTE
IPC分类号： C07C217/42 , A61K31/133 , A61K31/221 , A61P9/00 , C07C219/24
CPC分类号： C07C217/42 , A61K31/133 , A61K31/221 , C07C219/24 , C07C2602/10
摘要： The invention relates to compounds of Formula (I) wherein R1, R2, R3, R4, R 5, m and n are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.
摘要翻译：本发明涉及式（I）化合物及其可药用盐，其中R 1，R 2，R 3，R 4，R 5，m和n如说明书中所定义。这些化合物可用作钙通道阻断剂。

4. 发明申请

WO02085928A2 PRO-DRUG AND USE THEREOF AS A MEDICAMENT 审中-公开
标题翻译：作为药物的药物及其用途
公开(公告)号：WO02085928A2
公开(公告)日：2002-10-31
申请号：PCT/CH0200222
申请日：2002-04-22
申请人： DEBIOPHARM SA , WENGER ROLAND , MUTTER MANFRED , HAMEL ARNAUD , HUBLER FRANCIS
发明人： WENGER ROLAND , MUTTER MANFRED , HAMEL ARNAUD , HUBLER FRANCIS
IPC分类号： A61K38/00 , A61K38/13 , A61P27/02 , A61P31/18 , A61P43/00 , C07K7/64
CPC分类号： C07K7/645 , A61K38/00
摘要： The invention relates to a pro-drug comprising a cyclic undecapeptide wherein the peptide chain thereof comprises at least one amino acid residue of general formula (1) wherein the carbon atom C is one of the links in said undecapeptide cycle; - substituents Y individually represent a hydrogen atom or form a bond together; - substitutents R and R independently represent a hydrogen atom, an aralkyl group, an alkaryl group, a heteroalkyl group, a heterocyclic group, a heterocyclic alkyl group, an alkyl heterocyclic group or an alkyl group having 1-6 carbon atoms which is linear or branched, and which is optionally substituted by at least one of the groups chosen from among -COOH, -CONHR , -NHC0=NH(NH2), -NHC=NR (NH2), -NH2, -NHR , -NR 2, -N R 3, -OH, -OPO(OR )2, -OPO(OH)(OR ), -OPO(OH)2, -OSO(OR )2, -OSO(OH)(OR ), -OSO(OH)2, and the different salts produced therefrom, each of the substituents R independently representing an alkyl group which is linear or ramified having 1 - 6 carbon atoms; - substituents R and R independently represent a hydrogen atom, an alkaryl group or an alkyl group having 1 - 6 carbon atoms which is linear or branched; - the substituents R and R individually represent a hydrogen atom, an aralkyl group, an alkyl group having 1-6 carbon atoms which is linear or branched; and substituent R represents an alkaryl group, a heteroalkyl group, a heterocylic group,a heterocylic alkyl group, an alkyl heterocyclic group or an alkyl group having1 - 6 carbon atoms which is linear or branched.
摘要翻译：本发明涉及包含环状十一肽的前体药物，其中肽链包含至少一个通式（1）的氨基酸残基，其中碳原子C a是所述十一肽循环中的连接之一; - 取代基Y分别表示氢原子或一起形成键; 取代基R 1和R 3独立地表示氢原子，芳烷基，烷芳基，杂烷基，杂环基，杂环烷基，烷基杂环基或具有1-6个碳原子的烷基碳原子是直链或支链的，并且其任选被至少一个选自-COOH，-CONHR 8，-NHC 0 = NH（NH 2），-NHC = NR 8（NH 2）的基团取代，，-NH 2，-NHR 8，-NR 8 2，-N + R 8，-OH，-OPO（OR 8）2，-OPO（OH）（OR 8 >），-OPO（OH）2，-OSO（OR 8）2，-OSO（OH）（OR 8），-OSO（OH）2及其生成的不同的盐， R 8独立地表示具有1-6个碳原子的直链或支链的烷基; - 取代基R 2和R 4独立地表示氢原子，烷芳基或具有1-6个碳原子的直链或支链烷基; - 取代基R 5和R 6分别表示氢原子，芳烷基，具有1-6个碳原子的直链或支链烷基; 取代基R 7表示直链或支链的烷芳基，杂烷基，杂环基，杂环烷基，烷基杂环基或具有1-6个碳原子的烷基。

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