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37 条记录 (耗时 0.024 秒)

    BICYCLIC AND TRICYCLIC DERIVATIVES AS THROMBIN RECEPTOR ANTAGONISTS
    22.
    发明公开
    BICYCLIC AND TRICYCLIC DERIVATIVES AS THROMBIN RECEPTOR ANTAGONISTS 有权
    二环和三环衍生物作为凝血酶受体拮抗剂

    公开(公告)号：EP2069326A2

    公开(公告)日：2009-06-17

    申请号：EP07867202.9

    申请日：2007-10-02

    申请人： Schering Corporation

    发明人： CHACKALAMANNIL, Samuel ,  CHELLIAH, Mariappan, V. ,  WANG, Yuguguang ,  XIA, Yan

    IPC分类号： C07D401/06 ,  C07D417/06 ,  A61K31/443 ,  A61P7/00

    CPC分类号： C07D401/06 ,  C07D417/06

    摘要： Heterocyclic-substituted tricyclics of the formula (I) or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.

    HIMBACINE ANALOGUES AS THROMBIN RECEPTOR ANTAGONISTS
    24.
    发明公开
    HIMBACINE ANALOGUES AS THROMBIN RECEPTOR ANTAGONISTS 有权
    氨基胍类似物作为血栓素受体拮抗剂

    公开(公告)号：EP1436298A1

    公开(公告)日：2004-07-14

    申请号：EP02801732.5

    申请日：2002-10-16

    申请人： SCHERING CORPORATION

    发明人： CHACKALAMANNIL, Samuel ,  CHELLIAH, Mariappan, V. ,  CLASBY, Martin, C. ,  XIA, Yan

    IPC分类号： C07D491/04 ,  A61K31/445 ,  A61K31/34 ,  A61P29/00 ,  A61P19/02 ,  A61P9/00

    CPC分类号： C07D491/04 ,  C07D493/04 ,  C07D495/04

    摘要： Heterocyclic-substituted tricyclics of the formula (I) or a pharmaceutically acceptable salts thereof, wherein: n1 and n2 are independently 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is alkyl or optionally substituted alkenyl; R22 is -COR23 or a carboxy, sulfinyl, sulfonyl, sulfonamide or amino acid derivative; R23 is haloalkyl; alkenyl; haloalkenyl; alkynyl; optionally substituted cycloalkyl; cycloalkyl-alkyl; aryl; arylalkyl; heteroaryl; heterocycloalkyl; or -COOH and/or -SO¿3?H substituted alkyl; R?1, R2, R3, R9, R10 and R11¿ are as defined in the specification; are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds.

    摘要翻译： 式（I）的杂环取代的三环或其药学上可接受的盐，其中：n1和n2独立地为0-2; Het是任选取代的单环，双环或三环杂芳族基团; B是烷基或任选取代的链烯基; R22是-COR23或羧基，亚磺酰基，磺酰基，磺酰胺或氨基酸衍生物; R23是卤代烷基; 烯基; 卤代链; 炔基; 任选取代的环烷基 环烷基 - 烷基; 芳基; 芳; 杂; 杂环; 或-COOH和/或-SO 3 H取代的烷基; R 1，R 2，R 3，R 9，R 10和R 11如说明书中所定义; 以及含有它们的药物组合物以及通过施用所述化合物治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭和癌症相关的疾病的方法。

    ADENOSINE A2A RECEPTOR ANTAGONISTS
    26.
    发明公开
    ADENOSINE A2A RECEPTOR ANTAGONISTS 有权
    腺苷A2A受体拮抗剂

    公开(公告)号：EP1283839A1

    公开(公告)日：2003-02-19

    申请号：EP01945991.6

    申请日：2001-05-24

    申请人： SCHERING CORPORATION

    发明人： NEUSTADT, Bernard, R. ,  LINDO, Neil, A. ,  GREENLEE, William, J. ,  TULSHIAN, Deen ,  SILVERMAN, Lisa, S. ,  XIA, Yan ,  BOYLE, Craig, D. ,  CHACKALAMANNIL, Samuel

    IPC分类号： C07D487/14 ,  A61K31/505 ,  A61P25/28

    CPC分类号： C07D487/14

    摘要： Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or -C(O)CH2-;Y is -N(R2)CH2CH2N(R3)-, -OCH¿2?CH2N(R?2¿)-, -O-, -S-, -CH¿2?S-, -(CH2)2-NH-, or optionally substituted,(Ia), m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R?6¿-C(O)-, R6-SO2-, R6-OC(O)-, R7-N(R8)-C(O)-, R7-N(R8)-C(S)-, phenyl-CH(OH)-, or phenyl-C(=NOR2)-; or when Q is CH, (Ib),phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R?2, R3, R6, R7, and R8¿ are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula (I).

    2-BENZYL-POLYCYCLIC GUANINE DERIVATIVES AND PROCESS FOR PREPARING THEM
    27.
    发明公开
    2-BENZYL-POLYCYCLIC GUANINE DERIVATIVES AND PROCESS FOR PREPARING THEM 失效
    2 BENZYLPOLYCYCLISCH鸟嘌呤及其制备方法

    公开(公告)号：EP0686157A1

    公开(公告)日：1995-12-13

    申请号：EP94910124.0

    申请日：1994-02-24

    申请人： SCHERING CORPORATION

    发明人： TULSHIAN, Deen ,  McKITTRICK, Brian, A. ,  XIA, Yan ,  CHACKALAMANNIL, Samuel ,  GALA, Dinesh ,  DIBENEDETTO, Donald, J. ,  KUGELMAN, Max

    IPC分类号： C07D239 ,  C07D473 ,  C07D487

    CPC分类号： C07D487/14 ,  C07D239/54 ,  C07D473/40

    摘要： Antihypertensive and bronchodilating compounds of formula (I) or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein: R1, R2 and R3 are hydrogen, lower alkyl, lower alkoxy, halogeno, hydroxy, (di-lower alkyl)amino, 4-morpholinyl, 1-pyrrolidinyl, 1-pyrrolyl, -CF3, -OCF3, phenyl or methoxyphenyl; or R1 and R2 together are methylenedioxy; or R1 and R2 together with the carbon atoms to which they are attached form a benzene ring; and Ra is hydrogen and R?b and Rc¿, together with the carbon atoms to which they are attached, form a saturated ring of 5 carbons; or Ra is lower alkyl, Rb is hydrogen or lower alkyl, and Rc is hydrogen; or Ra, Rb and the carbon atom to which they are attached form a saturated ring of 5-7 carbons, and Rc is hydrogen; or Ra is hydrogen, and Rb, Rc and the carbon atoms to which they are attached form a tetrahydrofuran ring; or R?a and Rb¿, together with the carbon atom to which they are attached, and R?b and Rc¿, together with the carbon atoms to which they are attached, each form a saturated ring of 5-7 carbons; pharmaceutical compositions containing said compounds: methods of treatment using said compounds; and a process for preparing polycyclic guanines comprising a) reducing a nitrosopyrimidine, and treating the reduced nitrosopyrimidine with an acylating reagent to give the amidopyrimidine; b) reacting the amidopyrimidine with a halogenating/cyclizing reagent to give a halopurine; c) reacting, in the presence of a base, the halopurine with an amine to give the substituted aminopurine; and d) closing the ring of the substituted aminopurine with a suitable dehydrating agent.