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123 条记录 (耗时 0.038 秒)

    Adenosine Aa2 receptor antagonists
    1.
    发明授权
    Adenosine Aa2 receptor antagonists 有权
    腺苷Aa2受体拮抗剂

    公开(公告)号：US07713985B2

    公开(公告)日：2010-05-11

    申请号：US11767624

    申请日：2007-06-25

    申请人： Martin C. Clasby ,  Samuel Chackalamannil ,  Andrew Stamford

    发明人： Martin C. Clasby ,  Samuel Chackalamannil ,  Andrew Stamford

    IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D491/00

    CPC分类号： C07D487/04

    摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein: X1 and X2 are 1-3 substituents independently selected from the group consisting of H, alkyl, halo, —CF3, —OCF3, alkoxy, —OH and —CN; n is 0, 1 or 2; and R and R1 are H or alkyl; also disclosed is the use of the compounds in the treatment of CNS diseases such as Parkinson's disease, alone or in combination with other agents for treating CNS diseases, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

    摘要翻译： 具有结构式I的化合物或其药学上可接受的盐，其中：X 1和X 2是1-3个独立地选自H，烷基，卤素，-CF 3，-OCF 3，烷氧基，-OH和-CN的取代基; n为0,1或2; 且R和R 1为H或烷基; 还公开了该化合物在治疗CNS疾病如帕金森病中的用途，单独或与其它用于治疗CNS疾病的药物组合，其包含它们的药物组合物和包含组合组分的试剂盒的使用。

    ADENOSINE A2A RECEPTOR ANTAGONISTS
    2.
    发明申请
    ADENOSINE A2A RECEPTOR ANTAGONISTS 有权
    腺苷A2A受体拮抗剂

    公开(公告)号：US20080255156A1

    公开(公告)日：2008-10-16

    申请号：US11767624

    申请日：2007-06-25

    申请人： Martin C. Clasby ,  Samuel Chackalamannil ,  Andrew Stamford

    发明人： Martin C. Clasby ,  Samuel Chackalamannil ,  Andrew Stamford

    IPC分类号： A61K31/519 ,  C07D487/02 ,  A61P25/00

    CPC分类号： C07D487/04

    摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein: X1 and X2 are 1-3 substituents independently selected from the group consisting of H, alkyl, halo, —CF3, —OCF3, alkoxy, —OH and —CN; n is 0, 1 or 2; and R and R1 are H or alkyl; also disclosed is the use of the compounds in the treatment of CNS diseases such as Parkinson's disease, alone or in combination with other agents for treating CNS diseases, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

    摘要翻译： 具有结构式I的化合物或其药学上可接受的盐，其中：X 1和X 2是1-3个独立地选自H，烷基， 卤素，-CF 3，-OCF 3，烷氧基，-OH和-CN; n为0,1或2; 且R和R 1为H或烷基; 还公开了该化合物在治疗CNS疾病如帕金森病中的用途，单独或与其它用于治疗CNS疾病的药物组合，其包含它们的药物组合物和包含组合组分的试剂盒的使用。

    Thrombin receptor antagonists
    7.
    发明授权
    Thrombin receptor antagonists 有权
    凝血酶受体拮抗剂

    公开(公告)号：US06326380B1

    公开(公告)日：2001-12-04

    申请号：US09545720

    申请日：2000-04-07

    申请人： Samuel Chackalamannil ,  Theodros Asberom ,  Yan Xia ,  Dario Doller ,  Martin C. Clasby ,  Michael F. Czarniecki

    发明人： Samuel Chackalamannil ,  Theodros Asberom ,  Yan Xia ,  Dario Doller ,  Martin C. Clasby ,  Michael F. Czarniecki

    IPC分类号： A61K3147

    CPC分类号： C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04 ,  C07D491/04 ,  C07D493/10

    摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Q is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is —(CH2)n3—, wherein n3 is 0-5, —CH2—O—, —CH2S—, —CH2—NR6—, —C(O)NR6—, —NR6C(O)—,  optionally substituted alkenyl or optionally substituted alkynyl; X is —O— or —NR6— when the double dotted line represents a single bond, or X is —OH or —NHR20 when the bond is absent; Y is ═O, ═S, (H, H), (H, OH) or (H, C1-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is ═O, (H, H), (H, OH), (H, SH) or (H, C1-C6 alkoxy); R15 is absent when the double dotted line represents a single bond and is H, —NR18R19, or —OR17 when the bond is absent; or Y is  or  and R15 is H or C1-C6 alkyl; 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2的杂环取代的三环或其药学上可接受的盐，其中：单点线表示任选的双键;双点划线表示任选的单键; n为0-2; Q为任选取代的环烷基，杂环烷基，芳基 或杂芳基; Het是任选取代的单，双或三环杂芳族基团; B是 - （CH 2）n3-，其中n3是0-5，-CH2-O-，-CH2S-，-CH2-NR6-， -C（O）NR 6 - ，-NR 6 C（O） - ，任选取代的烯基或任选取代的炔基;当双点划线表示单键时，X为-O-或-NR6-，或X为-OH或-NHR20 当双键虚线表示单键时，当不存在键时，Y为= O，= S，（H，H），（H，OH）或（H，C 1 -C 6烷氧基） ，Y为= O，（H，H），（H，OH），（H，SH）或（H，C1-C6烷氧基）;当双点表示单键且为H时， NR18R19或-OR17，当该键不存在时; 或Y为或R 15为H或C 1 -C 6烷基;以及含有它们的药物组合物和治疗与血栓形成，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 通过施用所述化合物。

    Pyrazolo [1,5-A]pyrimidine adenosine A2a receptor antagonists
    9.
    发明授权
    Pyrazolo [1,5-A]pyrimidine adenosine A2a receptor antagonists 有权
    吡唑并[1,5-A]嘧啶腺苷A2a受体拮抗剂

    公开(公告)号：US07741318B2

    公开(公告)日：2010-06-22

    申请号：US11311195

    申请日：2005-12-19

    申请人： Martin C. Clasby ,  Samuel Chackalamannil ,  Bernard R. Neustadt ,  Xiaobang Gao

    发明人： Martin C. Clasby ,  Samuel Chackalamannil ,  Bernard R. Neustadt ,  Xiaobang Gao

    IPC分类号： C07D243/08 ,  C07D295/02 ,  C07D295/16 ,  C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/5513 ,  A61P25/16

    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.

    摘要翻译： 公开了具有结构式I的化合物，其中A是亚烷基或任选取代的亚芳基，亚环烷基或杂芳基二基; X是-C（O） - 或-S（O）2 - ; R1是烷基或环烷基; R2是氢，卤素或-CN; R3是氢或烷基; R4是氢，烷基，烷氧基，羟基烷基，氨基烷基 - ，环烷基，杂环烷基，被烷基取代的杂环烷基，任选取代的芳基烷基或任选取代的杂芳基烷基; 或R 3和R 4形成任选取代的5-7元环，所述环任选地包含另外的杂原子环成员; R 7是烷基，任选取代的苯基，任选取代的杂芳基，环烷基，卤素，吗啉基，任选取代的哌嗪基或任选取代的氮杂环烷基。 还公开了化合物在治疗帕金森病中的用途，单独或与其他治疗帕金森病的药物组合，包含它们的药物组合物和包含组合组分的试剂盒的用途。