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    PYRAZOLO[1,5-A]PYRIMIDINE ADENOSINE A2a RECEPTOR ANTAGONISTS
    71.
    发明公开
    PYRAZOLO[1,5-A]PYRIMIDINE ADENOSINE A2a RECEPTOR ANTAGONISTS 有权
    并[1,5-A]腺苷A2A受体的嘧啶类拮抗剂

    公开(公告)号：EP1836205A2

    公开(公告)日：2007-09-26

    申请号：EP05854388.5

    申请日：2005-12-19

    申请人： Schering Corporation

    发明人： CLASBY, Martin, C. ,  CHACKALAMANNIL, Samuel ,  NEUSTADT, Bernard, R. ,  GAO, Xiaobang

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： Compounds having the structural formula (I) are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is -C(O)- or -S(O)2-; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or -CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

    CONSTRAINED HIMBACINE ANALOGS AS THROMBIN RECEPTOR ANTAGONISTS
    72.
    发明公开
    CONSTRAINED HIMBACINE ANALOGS AS THROMBIN RECEPTOR ANTAGONISTS 有权
    受限制的巴比妥类似物作为凝血酶受体拮抗剂

    公开(公告)号：EP1751144A1

    公开(公告)日：2007-02-14

    申请号：EP05755642.5

    申请日：2005-05-25

    申请人： SCHERING CORPORATION

    发明人： CHELLIAH, Mariappan, V. ,  CHACKALAMANNIL, Samuel ,  XIA, Yan ,  CLASBY, Martin, C. ,  GREENLEE, William, J. ,  WANG, Yuguang ,  VELTRI, Enrico, P. ,  WU, Wenxue ,  GRAZIANO, Michael, P. ,  KOSOGLOU, Teddy ,  CHINTALA, Madhu

    IPC分类号： C07D405/08 ,  C07D493/04 ,  A61K31/443 ,  A61K31/4433 ,  A61P9/00 ,  A61P25/28 ,  A61P11/00

    CPC分类号： C07D493/04 ,  C07D405/06

    摘要： A compound represented by the structural formula (Chemical formula should be inserted here as it appears on abstract in paper form) and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line between the ring carbons to which R10 and R34 are attached represents either a single bond or a double bond; the double-dashed line between X and the carbon to which Y is attached represents either a single bond or an absent bond; X is -O- or -NR6- when the double-dashed line represents a single bond; X is H, -OH or -NHR20 when the double-dashed line represents an absent bond; and other parameters are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing said compounds and their uses as thrombin receptor antagonists and binders to cannabinoid receptors.

    摘要翻译： 公开了由结构式（化学式应当插入本文作为摘要以纸形式出现）的化合物及其药学上可接受的盐和溶剂，其中：R10和R34所代表的环碳之间的单点划线 连接表示单键或双键; X与Y所连接的碳之间的双点划线表示单键或无键; 当双虚线表示单键时，X是-O-或-NR6-; 当双虚线表示无键时，X是H，-OH或-NHR20; 和其他参数如本文所定义。 还公开了含有所述化合物及其作为凝血酶受体拮抗剂和大麻素受体结合剂的用途的药物组合物和组合。

    THROMBIN RECEPTOR ANTAGONISTS
    75.
    发明公开
    THROMBIN RECEPTOR ANTAGONISTS 有权
    THROMBIN受体拮抗剂

    公开(公告)号：EP1663965A2

    公开(公告)日：2006-06-07

    申请号：EP04789042.1

    申请日：2004-09-23

    申请人： SCHERING CORPORATION

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

    IPC分类号： C07D201/00

    CPC分类号： C07D417/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/06 ,  C07D405/14 ,  C07D413/14

    摘要： A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.

    摘要翻译： 公开了一系列由结构式表示的化合物及其药学上可接受的异构体，盐，溶剂化物和多晶型物。 还公开了含有所述化合物及其作为凝血酶受体拮抗剂和大麻素受体结合剂的用途的药物组合物。

    ADENOSINE A2A RECEPTOR ANTAGONISTS
    77.
    发明授权
    ADENOSINE A2A RECEPTOR ANTAGONISTS 有权
    腺苷A2A受体拮抗剂

    公开(公告)号：EP1283839B1

    公开(公告)日：2005-04-20

    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).

    TRICYCLIC THROMBIN RECEPTOR ANTAGONISTS
    78.
    发明公开
    TRICYCLIC THROMBIN RECEPTOR ANTAGONISTS 有权
    凝血酶受体拮抗剂的三环

    公开(公告)号：EP1495018A1

    公开(公告)日：2005-01-12

    申请号：EP03718393.6

    申请日：2003-04-14

    申请人： SCHERING CORPORATION

    发明人： CHACKALAMANNIL, Samuel ,  CLASBY, Martin, C. ,  GREENLEE, William, J. ,  WANG, Yuguang ,  XIA, Yan ,  VELTRI, Enrico, P. ,  CHELLIAH, Mariappan ,  WU, Wenxue

    IPC分类号： C07D405/06 ,  A61K31/44 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P35/00 ,  A61P43/00

    CPC分类号： C07D405/06 ,  C07D405/14 ,  C07D417/14

    摘要： Heterocyclic-substituted tricyclics of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; (a) represents an optional double bond; n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; each R13 is independently selected from H, (C1-C6)alkyl, (C3-C8)cycloalkyl, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4, haloalkyl and halogen; each R14 is independently selected from H, (C1-C6)alkyl, -OH, (C1-C6)alkoxy, R27-aryl (C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4, halogen and haloalkyl; or R13 and R14 taken together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms; wherein at least one of R13 or R14 is selected from the group consisting of -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5, and -(CH2)n6C(O)NR28R29 where n6 is 0-4; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein 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.