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27 条记录 (耗时 0.031 秒)

    Phthalazinone derivatives
    1.
    发明授权
    Phthalazinone derivatives 失效
    酞嗪衍生物

    公开(公告)号：US07902193B2

    公开(公告)日：2011-03-08

    申请号：US12271308

    申请日：2008-11-14

    申请人： Muhammad Hashim Javaid ,  Keith Allan Menear ,  Sylvie Gomez ,  Marc Geoffrey Hummersone ,  Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Xiao-Ling Fan Cockcroft ,  Frank Kerrigan

    发明人： Muhammad Hashim Javaid ,  Keith Allan Menear ,  Sylvie Gomez ,  Marc Geoffrey Hummersone ,  Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Xiao-Ling Fan Cockcroft ,  Frank Kerrigan

    IPC分类号： C07D237/32 ,  A61K31/502 ,  A61P35/00

    CPC分类号： C07D403/10 ,  C07D403/14 ,  C07D411/14 ,  C07D413/14 ,  C07D487/04

    摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C═O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2. RC1 and RC2 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocylic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, such that there is a double bond between the atoms substituted by RC1 and RC3.

    摘要翻译： 式（I）的化合物：其中：A和B一起表示任选取代的稠合芳环; D选自：（i）其中Y1选自CH和N，Y2选自CH和N，Y3选自CH，CF和N; 和（ii）其中Q为O或S; RD是：其中RN1选自H和任选取代的C 1-10烷基; X选自单键NRN2，CRC3RC4和C = O; RN2选自H和任选取代的C 1-10烷基; RC3和RC4独立地选自H，R，C（= O）OR，其中R是任选取代的C 1-10烷基，任选取代的C 5-20芳基或任选取代的C 3-20杂环基; Y选自NRN3和CRC1RC2。 RC1和RC2独立地选自H，R，C（= O）OR，其中R是任选取代的C 1-10烷基，任选取代的C 5-20芳基或任选取代的C 3-20杂环基; RC1和RC2与它们所连接的碳原子一起可以形成任选取代的螺 - 稠合的C 5-7碳环或杂环; 当X是单键时，RN1和RC2可以与它们所结合的N和C原子一起形成任选被取代的C5-7杂环; 并且当X是CRC3RC4时，RC2和RC4可以一起形成附加键，使得在被RC1和RC3取代的原子之间存在双键。

    Heterocyclcarboxamide derivatives and their use as therapeutic agents
    5.
    发明授权
    Heterocyclcarboxamide derivatives and their use as therapeutic agents 失效
    杂环甲酰胺衍生物及其作为治疗剂的用途

    公开(公告)号：US5935973A

    公开(公告)日：1999-08-10

    申请号：US981671

    申请日：1998-01-05

    申请人： Alan Martin Birch ,  David John Heal ,  Frank Kerrigan ,  Keith Frank Martin ,  Patricia Lesley Needham ,  Bruce Jeremy Sargent

    发明人： Alan Martin Birch ,  David John Heal ,  Frank Kerrigan ,  Keith Frank Martin ,  Patricia Lesley Needham ,  Bruce Jeremy Sargent

    IPC分类号： A61K31/335 ,  A61K31/44 ,  A61K31/443 ,  A61K31/445 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/18 ,  C07D405/14 ,  C07D409/14 ,  C07D207/04 ,  C07D207/50 ,  C07D211/06 ,  C07D211/98 ,  C07D319/20

    CPC分类号： C07D405/14 ,  C07D409/14

    摘要： Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.

    摘要翻译： PCT No.PCT / EP96 / 02890 Sec。 371日期：1998年1月5日 102（e）1998年1月5日PCT PCT 1996年7月2日PCT公布。 公开号WO97 / 03071 日期1997年1月30日，式I化合物及其药学上可接受的盐，其中A为亚甲基或O; B是亚甲基或O; g为0,1,2,3或4; R1是任选的取代基; U是任选被一个或多个烷基取代的亚烷基链; Q表示含有氮原子的二价基团; T代表CO.HET，可用于治疗中枢神经系统疾病，例如抑郁症，焦虑症，精神病（例如精神分裂症），迟发性运动障碍，帕金森病，肥胖症，高血压，图雷特综合征，性功能障碍，药物成瘾， 药物滥用，认知障碍，阿尔茨海默氏病，老年痴呆症，强迫症，恐慌发作，社交恐怖症，进食障碍和厌食症，心血管和脑血管障碍，非胰岛素依赖性糖尿病，高血糖症，便秘，心律失常，神经内分泌障碍 系统，压力，前列腺肥大和痉挛状态。

    Condensed thiazole derivatives, having 5-HT receptor affinity
    6.
    发明授权
    Condensed thiazole derivatives, having 5-HT receptor affinity 失效
    具有5-HT受体亲和力的缩合噻唑衍生物

    公开(公告)号：US5869492A

    公开(公告)日：1999-02-09

    申请号：US973960

    申请日：1997-12-15

    申请人： Frank Kerrigan ,  Sharon Crawford Cheetham ,  Roy Victor Davies

    发明人： Frank Kerrigan ,  Sharon Crawford Cheetham ,  Roy Victor Davies

    IPC分类号： A61K31/425 ,  A61K31/505 ,  A61P3/04 ,  A61P3/08 ,  A61P11/10 ,  A61P21/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D513/04 ,  A61K31/495 ,  C07D513/06

    CPC分类号： C07D513/04

    摘要： Compounds of formula I ##STR1## in which A is S(O).sub.p or O;p is 0, 1 or 2;g is 0, 1, 2, 3, or 4;n is 2 or 3; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are optional substituents have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, cerebral ischemia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, non-insulin dependent diabetes mellitus, hyperglycemia, and stress.

    摘要翻译： PCT No.PCT / EP96 / 02676 Sec。 371 1997年12月15日第 102（e）日期1997年12月15日PCT提交1996年6月20日PCT公布。 出版物WO97 / 02269 日期1997年1月23日公式I I的化合物，其中A为S（O）p或O; p为0,1或2; g为0,1,2,3或4; n为2或3; R1，R2，R3，R4和R5是可用于治疗中枢神经系统疾病，例如抑郁，焦虑，精神病（例如精神分裂症），迟发性运动障碍，肥胖症，药物成瘾，药物滥用，认知障碍 老年痴呆，老年痴呆，脑缺血，强迫症，恐慌发作，社交恐怖症，进食障碍和厌食症，非胰岛素依赖性糖尿病，高血糖症和压力。

    Substituted 4-arylmethylene-2-imino-2,3-dihydrothiazoles and derivatives and their pharmaceutical use
    10.
    发明授权
    Substituted 4-arylmethylene-2-imino-2,3-dihydrothiazoles and derivatives and their pharmaceutical use 失效
    取代的4-芳基亚甲基-2-亚氨基-2,3-二氢噻唑及其衍生物及其药物用途

    公开(公告)号：US06187802B1

    公开(公告)日：2001-02-13

    申请号：US09380967

    申请日：1999-09-14

    申请人： Sharon Crawford Cheetham ,  Frank Kerrigan ,  Colin Gerhart Pryce Jones

    发明人： Sharon Crawford Cheetham ,  Frank Kerrigan ,  Colin Gerhart Pryce Jones

    IPC分类号： A61K31426

    CPC分类号： C07D417/12 ,  C07D277/42 ,  C07D417/14 ,  C07D513/04

    摘要： Compounds of Formula I including pharmaceutically acceptable salts thereof in the form of individual enantiomers, racemates, or other mixtures of enantiomers, in which Ar is phenyl, naphthyl or benzo[b]thiophenyl, each of which may be optionally substituted; R1 and R2, which may be the same or different, independently are a) H, b) an alkyl group containing 1 to 6 carbon atoms, c) an alkenyl group containing 3 to 6 carbon atoms, d) a cycloalkyl group containing 3 to 7 carbon atoms, e) a cycloalkylmethyl group in which the ring contains 3 to 7 carbon atoms, f) an aryl or heteroaryl group optionally substituted g) an arylalkyl or heteroarylalkyl group each optionally substituted; or R1 and R2 form an alkylene chain optionally substituted by one or more alkyl groups each containing 1 to 3 carbon atoms, such that, together with the atoms to which they are attached, they form a 5 or 6 membered ring; R3 is a) H, b) an aryl or heteroaryl group each optionally substituted c) an optionally substituted arylmethyl group; or d) an alkoxyalkyl group containing 3 to 6 carbon atoms; and R4 and R5, which may be the same or different, independently are an alkyl group containing 1 to 3 carbon atoms, or R4 and R5 together with the atom to which they are attached form a cycloalkyl ring containing 3 to 6 carbon atoms; processes to prepare such compounds; compositions containing such compounds and their use in the treatment of depression, anxiety, Parkinson's disease, obesity, cognitive disorders, seizures, neurological disorders and as neuroprotective agents; are described.

    摘要翻译： 式I化合物包括其单体对映异构体，外消旋体或对映异构体的其它混合物形式的药学上可接受的盐，其中Ar是苯基，萘基或苯并[b]噻吩基，其各自可以任选被取代; R 1和R 2可以相同或不同，独立地为a）H，b）含有1至6个碳原子的烷基，c）含有3至6个碳原子的链烯基，d）包含3至 7个碳原子，e）其中环包含3至7个碳原子的环烷基甲基，f）任选取代的芳基或杂芳基; g）各自任选取代的芳基烷基或杂芳基烷基; 或R 1和R 2形成任选被一个或多个含有1至3个碳原子的烷基取代的亚烷基链，使得它们与它们连接的原子一起形成5或6元环; R 3是a）H，b）任选取代的芳基或杂芳基c）任选取代的芳基甲基; 或d）含有3至6个碳原子的烷氧基烷基; 和R 4和R 5可以相同或不同，独立地为含有1至3个碳原子的烷基，或者R 4和R 5与它们所连接的原子一起形成含有3至6个碳原子的环烷基环; 制备这些化合物的方法; 含有这些化合物的组合物及其用于治疗抑郁症，焦虑症，帕金森病，肥胖症，认知障碍，癫痫发作，神经障碍和神经保护剂的用途; 被描述。