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568 条记录 (耗时 0.042 秒)

    Aminoheterocyclic derivatives as antithrombotic or anticoagulant agents
    51.
    发明申请
    Aminoheterocyclic derivatives as antithrombotic or anticoagulant agents 审中-公开
    氨基杂环衍生物作为抗血栓形成或抗凝血剂

    公开(公告)号：US20030207882A1

    公开(公告)日：2003-11-06

    申请号：US10427991

    申请日：2003-05-02

    申请人： ZENECA LIMITED

    发明人： Andrew Stocker ,  John Preston ,  Michael James Smithers

    IPC分类号： A61K031/5377 ,  A61K031/53 ,  A61K031/506 ,  A61K031/501 ,  A61K031/497 ,  A61K031/496 ,  A61K031/4545 ,  A61K031/4439 ,  C07D43/02 ,  C07D413/02 ,  C07D41/02

    CPC分类号： C07D401/14 ,  C07D213/74 ,  C07D237/20 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12

    摘要： Compounds of formula (I), wherein G1 is CH or N; G2 is CH or N; R1 is a variety of optional substituents, L1 is (1-4C)alkylene; T1 is CH or N; R2 and R3 are independently hydrogen or (1-4C)alkyl or are joined to form a ring; X1 and X2 represent various linking groups; Ar is phenylene or certain heteroaryl rings and Q represents a variety of aromatic or heterocyclic rings systems, and pharmaceutically acceptable salts thereof are described as useful antithrombotic and anticoagulant agents, and are selective Factor Xa inhibitors. Processes for their preparation and pharmaceutical compositions containing them are also described. 1

    摘要翻译： 式（I）的化合物，其中G 1是CH或N; G 2是CH或N; R 1是多种任选的取代基，L 1是（1-4C）亚烷基; T 1是CH或N; R 2和R 3独立地是氢或（1-4C）烷基或连接形成环; X 1和X 2代表各种连接基团; Ar是亚苯基或某些杂芳基环，Q表示各种芳族或杂环体系，其药学上可接受的盐被描述为有用的抗血栓形成和抗凝血剂，并且是选择性因子Xa抑制剂。 还描述了其制备方法和含有它们的药物组合物。

    Pyrimidine derivatives having antitumor effect
    52.
    发明申请
    Pyrimidine derivatives having antitumor effect 失效
    具有抗肿瘤作用的嘧啶衍生物

    公开(公告)号：US20030203894A1

    公开(公告)日：2003-10-30

    申请号：US10169993

    申请日：2002-07-12

    发明人： Hidekazu Tanaka ,  Kazuo Ueda ,  Shinji Suzuki ,  Hideyuki Takenaka

    IPC分类号： A61K031/55 ,  A61K031/506 ,  A61K031/505 ,  C07D43/02

    CPC分类号： C07D413/12

    摘要： A compound represented by the formula (I): 1 wherein, for example, R1, R2, R3, and R4 are each independently hydrogen atom, alkyl, and the like, R5 and R6 are each independently hydrogen atom, alkyl, and the like, RB and RC are each independently hydrogen atom, alkyl, and the like, X is nullOnull, nullSnull, and the like, Y is 5-membered heteroaryl-diyl and the like, Z is optionally substituted aryl and the like, their pharmaceutically acceptable salts, or their solvates.

    摘要翻译： 由式（I）表示的化合物：其中，例如R 1，R 2，R 3和R 4各自独立地为氢原子，烷基等，R 5 >和R 6各自独立地为氢原子，烷基等，R B和R C各自独立地为氢原子，烷基等，X为-O - ， - S-，和 Y为5元杂芳基 - 二基等，Z为任选取代的芳基等，其药学上可接受的盐或其溶剂合物。

    Azetidinyl diamines useful as ligands of the nociceptin receptor ORL-1
    55.
    发明申请
    Azetidinyl diamines useful as ligands of the nociceptin receptor ORL-1 审中-公开
    可用作伤害感受肽受体ORL-1的配体的氮杂环丁烷二胺

    公开(公告)号：US20030195185A1

    公开(公告)日：2003-10-16

    申请号：US10294814

    申请日：2002-11-14

    申请人： Schering Corporation

    发明人： Duane A. Burnett ,  Mary Ann Caplen ,  Michael F. Czarniecki ,  Martin S. Domalksi ,  Ginny D. Ho ,  Deen Tulshian ,  Wen-Lian Wu

    IPC分类号： A61K031/506 ,  A61K031/454 ,  A61K031/397 ,  C07D43/02 ,  C07D205/00

    CPC分类号： C07D231/12 ,  C07D205/04 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

    摘要： Disclosed are nociceptin ORL-1 receptor agonists of the formula 1 wherein: (a) R1 is optionally substituted alkyl, fluorenyl, pyrimidinyl or optionally substituted piperidinyl; R2 is H; and R3 is nullC(H)(R)nullNR7R8; R is H, optionally substituted aryl or arylalkyl, or heteroaryl; R7 is null(CH2)xR9, optionally substituted tetrahydronaphthyl, or cycloalkyl; and R8 is H; or R7 and R8 together form a substituted piperidinyl or piperazinyl ring; x is 0-10; and R9 is H, alkoxy, optionally substituted phenyl, naphthyl, heteroaryl, pyrrolidinyl, pyrrolidonyl, optionally substituted piperidinyl or diphenylmethyl; or (b) R2is nullNHR7or 2 and R3 is H; pharmaceutical compositions; and methods of using the compounds to treat cough and pain.

    摘要翻译： 公开了下式的伤害感受肽ORL-1受体激动剂，其中：（a）R <下标> 1是任选取代的烷基，芴基，嘧啶基或任选取代的哌啶基; R <下标> 2 是H; 并且R <下标3 是-C（H）（R）-NR <下标> 7 R <下标> 8 ; R是H，任选取代的芳基或芳烷基或杂芳基; R <下标> 7 是 - （CH <下标> 2 ）<下标> x R <下标> 9 ，任选取代的四氢萘基或环烷基; 而R 8>是H; 或R <下标7 和R <下标8 一起形成取代的哌啶基或哌嗪基环; x为0-10; 并且R <下标9是H，烷氧基，任选取代的苯基，萘基，杂芳基，吡咯烷基，吡咯烷酮基，任选取代的哌啶基或二苯基甲基; 或（b）R <下标> 2 是-NHR <下标> 7 ，或者R <下标> 3 是H; 药物组合物; 以及使用该化合物治疗咳嗽和疼痛的方法。

    Use of organic compounds
    56.
    发明申请
    Use of organic compounds 审中-公开
    使用有机化合物

    公开(公告)号：US20030191131A1

    公开(公告)日：2003-10-09

    申请号：US10395525

    申请日：2003-03-24

    发明人： Michael Heinrich

    IPC分类号： A61K031/506

    CPC分类号： A61K31/506

    摘要： 4-(4-methylpiperazin-1-ylmethyl)-N-null4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenylnull-benzamide of the formula I 1 or a pharmaceutically acceptable salt thereof can be used in the treatment of canine mast cell neoplasms.

    摘要翻译： 4-（4-甲基哌嗪-1-基甲基）-N- [4-甲基-3-（4-吡啶-3-基）嘧啶-2-基氨基）苯基] - 苯甲酰胺或其药学上可接受的盐 可用于治疗犬肥大细胞肿瘤。

    Piperdines for use as orexin receptor antagonists
    57.
    发明申请
    Piperdines for use as orexin receptor antagonists 失效
    用作食欲肽受体拮抗剂的Pi子

    公开(公告)号：US20030186964A1

    公开(公告)日：2003-10-02

    申请号：US10311445

    申请日：2002-12-16

    发明人： Clive Leslie Branch ,  Christopher Norbert Johnson ,  Geoffrey Stemp ,  Kevin Thewlis

    IPC分类号： A61K031/55 ,  A61K031/506 ,  A61K031/454 ,  A61K031/451 ,  C07D43/02 ,  C07D45/02

    CPC分类号： C07D401/06 ,  C07D211/26 ,  C07D401/10 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04

    摘要： Compounds of formula (I) wherein Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R3 and R4 is hydrogen or optionally substituted (C1-4)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R3 and R4 together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted; R2 represents phenyl or a 5- or 6-membered hereroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R5 represents an optionally substituted (C1-4)alkoxy, halo, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing up to 3 heteroatoms selected from N, O and S; or pharmaceutically acceptable salts thereof.

    摘要翻译： 其中Y表示基团（CH 2）n的式（I）化合物，其中n表示0,1或2; R 1是苯基，萘基，含有至多3个选自N，O和S的杂原子的单或双环杂芳基; 或NR 3或R 4基团，其中R 3和R 4中的一个是氢或任选取代的（C 1-4）烷基，另一个是苯基，萘基或含有上述的单或双环杂芳基 至3个选自N，O和S的杂原子，或R 3和R 4与它们所连接的N原子一起形成具有任选稠合的苯环的5至7元环胺; 任何R 1可以任选被取代; R 2表示苯基或含有至多3个选自N，O和S的杂原子的5或6元杂芳基，其中苯基或杂芳基被R 5取代，还有任选的取代基; 或R 2表示含有至多3个选自N，O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 5表示任选取代的（C 1-4）烷氧基，卤素，任选取代的（C 1-6）烷基，任选取代的苯基或任选取代的含有至多3个选自N ，O和S; 或其药学上可接受的盐。

    Angiogenesis inhibiting 5-substituted-1,2,4-thiadiazolyl derivatives
    58.
    发明申请
    Angiogenesis inhibiting 5-substituted-1,2,4-thiadiazolyl derivatives 失效
    血管发生抑制5-取代-1,2,4-噻二唑衍生物

    公开(公告)号：US20030181460A1

    公开(公告)日：2003-09-25

    申请号：US10387703

    申请日：2003-03-13

    发明人： Raymond Antoine Stokbroekx ,  Marc Andre Ceusters ,  Marcel Jozef Maria Van der Aa ,  Marcel Gerebernus Maria Luyckx ,  Marc Willems ,  Robert W. Tuman

    IPC分类号： A61K031/506 ,  A61K031/497 ,  A61K031/496 ,  A61K031/454 ,  C07D417/14

    CPC分类号： C07D285/08 ,  A61K31/454 ,  A61K31/496 ,  C07D285/135 ,  C07D417/04

    摘要： This invention concerns compounds of formula 1 the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CU or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NHnull, C3-6cycloalkyl, hydroxymethyl or beizyloxymethyl; R2 is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; 2 is Ar2, Ar2CH2null or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中X为CU或N; R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，单或二（C 1-6烷基）氨基，Ar 1，Ar 1 NH-，C 3-6环烷基，羟甲基或 甲氧基甲基; R 2是氢，C 1-6烷基，氨基，氨基羰基，一或二（C 1-6烷基）氨基，C 1-6烷氧基羰基，C 1-6烷基羰基氨基，羟基或C 1-6烷氧基; R 3，R 4和R 5各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基 ，C 1-6烷氧基羰基或Het 1; Ar 2，Ar 2 CH 2 - 或Het 2; Ar 1和Ar 2任选取代的苯基; Het 1和Het 2是任选取代的单环杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

    Pyridylpyrimidine derivatives as effective compounds against prion diseases
    59.
    发明申请
    Pyridylpyrimidine derivatives as effective compounds against prion diseases 审中-公开
    吡啶基嘧啶衍生物作为抗朊病毒疾病的有效化合物

    公开(公告)号：US20030176443A1

    公开(公告)日：2003-09-18

    申请号：US10204041

    申请日：2002-08-16

    发明人： Matthias Stein-Gerlach ,  Konstadinos Salassidis ,  Gerald Bacher ,  Stefan Muller

    IPC分类号： A61K031/506 ,  C07D43/14 ,  C07D43/02

    摘要： The present invention relates to pyridylpyrimidine derivatives of the general formula (I): 1 wherein R represents hydrogen or methyl and Z represents nitrogen containing functional groups, the use of the pyridylpyrimidine derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of prion infections and prion diseases, as well as compositions containing at least one pyridylpyrimidine derivative and/or pharmaceutically acceptable salt thereof. Furthermore, the present invention is directed to methods for preventing and/or treating prion infections and prion diseases using said pyridylpyrimidine derivatives. Human cellular protein kinases, phosphatases and cellular signal transduction molecules are disclosed as targets for detecting, preventing and/or treating prion infections and diseases, especially BSE, vCJD, or CJD which can be inhibited by the inventive pyridylpyrimidine derivatives.

    摘要翻译： 本发明涉及通式（I）的吡啶基嘧啶衍生物：其中R代表氢或甲基，Z代表含氮官能团，使用吡啶基嘧啶衍生物作为药物活性剂，特别是用于预防和/或治疗朊病毒 感染和朊病毒疾病，以及含有至少一种吡啶基嘧啶衍生物和/或其药学上可接受的盐的组合物。 此外，本发明涉及使用所述吡啶基嘧啶衍生物预防和/或治疗朊病毒感染和朊病毒疾病的方法。 公开了人细胞蛋白激酶，磷酸酶和细胞信号转导分子作为检测，预防和/或治疗可被本发明的吡啶基嘧啶衍生物抑制的朊病毒感染和疾病，特别是BSE，vCJD或CJD的靶标。