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354 条记录 (耗时 0.026 秒)

    Certain 1-azabicyclo[2.2.1]heptanes and 1-azabicyclo[2.2.2]octanes
    1.
    发明授权
    Certain 1-azabicyclo[2.2.1]heptanes and 1-azabicyclo[2.2.2]octanes 失效
    某些1-氮杂双环[2.2.1]庚烷和1-氮杂双环[2.2.2]辛烷

    公开(公告)号：US5541194A

    公开(公告)日：1996-07-30

    申请号：US369290

    申请日：1995-01-06

    申请人： Barry S. Orlek ,  Paul A. Wyman ,  Harry J. Wadsworth

    发明人： Barry S. Orlek ,  Paul A. Wyman ,  Harry J. Wadsworth

    IPC分类号： A61K31/395 ,  A61K31/435 ,  A61K31/55 ,  A61P25/02 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08 ,  A61K31/44 ,  C07D221/02

    CPC分类号： C07D487/08 ,  C07D453/02

    摘要： Novel compounds of formula (I), processes for their preparation, and their use as pharmaceutical agents are described: ##STR1## in which p represents an integer of 2 to 4; r represents an integer of 1 or 2; s represents 0 or 1; and X represents a group ##STR2## in which A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.1 and the other is nitrogen or CR.sub.2, or A.sub.2 is oxygen or sulphur, A.sub.1 is CH and A.sub.3 is CR.sub.1, where R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1-2 alkyl, with the proviso that when r is 2, R.sub.1 and R.sub.2 are hydrogen or methyl. The novel compounds of this invention may be used to treat or to prevent dementia in mammals.

    摘要翻译： 描述了新的式（I）化合物，其制备方法及其作为药剂的用途：其中p表示2至4的整数; r表示1或2的整数; s表示0或1; X表示A1为氧或硫的基团，其中A2和A3为CR1，另一个为氮或CR2，或A2为氧或硫，A1为CH，A3为CR1，其中R1和R2为 独立地选自氢和C 1-2烷基，条件是当r为2时，R 1和R 2为氢或甲基。 本发明的新化合物可用于治疗或预防哺乳动物的痴呆症。

    Method for treatment of atherosclerosis
    2.
    发明授权
    Method for treatment of atherosclerosis 失效
    治疗动脉粥样硬化的方法

    公开(公告)号：US5521201A

    公开(公告)日：1996-05-28

    申请号：US457387

    申请日：1995-06-01

    申请人： Richard M. Hindley ,  Michael A. Cawthorne

    发明人： Richard M. Hindley ,  Michael A. Cawthorne

    IPC分类号： A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  C07D277/20 ,  C07D277/42 ,  C07D277/82 ,  C07D417/12 ,  A61K31/44

    CPC分类号： A61K31/426 ,  A61K31/427 ,  C07D277/20 ,  C07D277/42 ,  C07D277/82 ,  C07D417/12

    摘要： A method is provided for the treatment and/or prophylaxis of cardiovascular diseases in a human or non-human mammal, which comprises administering to a human or non-human mammal in need thereof, an effective, non-toxic amount of a compound of formula (I): ##STR1## or a tautomeric form thereof and/or a pharmaceuticlaly acceptable salt thereof and/or a pharmaceutically acceptable solvate thereof, in which A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group; R.sup.1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond; A.sup.2 represents a benzene ring having in total up to five substituents; and n represents an integer in the range of from 2 to 6.

    摘要翻译： 提供了用于治疗和/或预防人或非人哺乳动物心血管疾病的方法，其包括对有需要的人或非人哺乳动物施用有效的无毒量的式 （I）化合物：其中A 1表示取代或未取代的芳族杂环基;（I）化合物或其互变异构形式和/或其药物可接受的盐和/或其药学上可接受的溶剂化物， R1表示氢原子，烷基，酰基，芳烷基，其中芳基部分可以是取代或未取代的，或取代或未取代的芳基; R2和R3各自表示氢，或R2和R3一起表示键; A2代表总共有五个取代基的苯环; n表示2〜6的整数。

    Heterocyclic compounds which have useful pharmaceutical utility
    5.
    发明授权
    Heterocyclic compounds which have useful pharmaceutical utility 失效
    具有有用药物效用的杂环化合物

    公开(公告)号：US5264436A

    公开(公告)日：1993-11-23

    申请号：US760405

    申请日：1991-09-16

    申请人： John M. Berge ,  Lee J. Beeley

    发明人： John M. Berge ,  Lee J. Beeley

    IPC分类号： C07D403/06 ,  A61K31/47 ,  C07D401/06

    CPC分类号： C07D403/06

    摘要： A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, or a pharmaceutically acceptable solvate thereof, wherein:Z represents a residue of a substituted or unsubstituted aryl group,A.sub.1 represents a substituted or unsubstituted methylene group or a substituted or unsubstituted ethylene group;A.sub.2 represents a substituted or unsubstituted methylene group or a substituted or unsubstituted ethylene group;providing that at least one of A.sup.1 or A.sup.2 represents a substituted methylene group or a substituted ethylene group,X represents O or NR.sup.o wherein R.sup.o represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkanoyl group substituted or unsubstituted in the alkyl moiety, or an arylalkyl moiety substituted or unsubstituted in the aryl moiety,p represents an integer 2 or 3, andq represents an integer in the range of from 1 to 12;a process for preparing such a compound, a composition comprising such a compound and the use of such a compound in medicine.

    摘要翻译： 式（I）化合物：其中：Z表示取代或未取代的芳基的残基，A1表示取代或未取代的芳基， 或未取代的亚甲基或取代或未取代的亚乙基; A2表示取代或未取代的亚甲基或取代或未取代的亚乙基; 条件是A1或A2中的至少一个表示取代的亚甲基或取代的亚乙基，X表示O或NRo，其中Ro表示氢原子，取代或未取代的烷基，取代或未取代的芳基，取代的烷酰基 或在烷基部分未取代，或在芳基部分取代或未取代的芳烷基部分，p表示2或3的整数，q表示1至12的整数; 制备这种化合物的方法，包含这种化合物的组合物和这种化合物在医药中的用途。

    Indolyl carboxamides useful treating migraine, cluster headache, trigeminal neuralgia or emesis
    9.
    发明授权
    Indolyl carboxamides useful treating migraine, cluster headache, trigeminal neuralgia or emesis 失效
    吲哚甲酰胺可用于治疗偏头痛，丛集性头痛，三叉神经痛或呕吐

    公开(公告)号：US5200413A

    公开(公告)日：1993-04-06

    申请号：US740397

    申请日：1991-08-05

    申请人： Francis D. King ,  Karen A. Joiner

    发明人： Francis D. King ,  Karen A. Joiner

    IPC分类号： C07D451/04

    CPC分类号： C07D451/04

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH;X and Y are independently selected from hydrogen or C.sub.1-4 alkyl, or together are a bond;R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl-C.sub.1-4 alkyl, or together are C.sub.2-4 polymethylene;R.sub.3 and R.sub.4 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.4-5 polymethylene;Z is a group of formula (a) ##STR2## wherein n is 2 or 3;p is 1 or 2;q is 1 to 3;r is 1 to 3; andR.sub.5 or R.sub.6 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl or C.sub.2-7 alkenyl-C.sub.1-4 alkyl;having 5-HT M-receptor antagonist activity.

    摘要翻译： 式（I）化合物及其药学上可接受的盐：其中L是NH; X和Y独立地选自氢或C 1-4烷基，或一起是一个键; R 1和R 2独立地选自氢，C 1-6烷基，C 2-6烯基-C 1-4烷基，或一起是C 2-4亚甲基; R 3和R 4独立地选自氢，卤素，CF 3，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，C 1-7酰基，C 1-7酰氨基，C 1-6烷基磺酰基氨基，N-（C 1-6烷基磺酰基 ）-N-C 1-4烷基氨基，C 1-6烷基亚磺酰基，羟基，硝基或氨基，氨基羰基，氨基磺酰基，氨基磺酰基氨基或N-（氨基磺酰基）-C 1-4烷基氨基，其任选地被一个或两个选自C 1-6 烷基，C 3-8环烷基，C 3-8环烷基C 1-4烷基，苯基或苯基C 1-4烷基或任选被C 4-5多亚甲基N-二取代; Z是式（a）的基团，其中n为2或3; p为1或2; q为1〜3; r为1〜3; 且R 5或R 6为C 1-7烷基，C 3-8环烷基，C 3-8环烷基-C 1-2烷基或C 2-7烯基-C 1-4烷基; 具有5-HT M受体拮抗剂活性。

    Lactam derivatives
    10.
    发明授权
    Lactam derivatives 失效
    LACTAM衍生物

    公开(公告)号：US5190937A

    公开(公告)日：1993-03-02

    申请号：US640069

    申请日：1991-01-11

    申请人： Roger E. Markwell ,  Ian Hughes

    发明人： Roger E. Markwell ,  Ian Hughes

    IPC分类号： A61K31/395 ,  A61P29/00 ,  A61P43/00 ,  C07D223/12 ,  C07D225/02 ,  C12N9/99

    CPC分类号： C07D223/12 ,  C07D225/02

    摘要： Novel compounds of formula (I), and pharmaceutically acceptable salts thereof; their preparation; compositions containing them; and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R.sub.1 is --OH; alkoxy; aryloxy or aralkyloxy in each of which the aryl group is optionally substituted; --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is independently hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom or an optionally substituted second nitrogen atom in the ring; or a group:--NH--CH(R.sub.8)--C(O)--R.sub.9where R.sub.8 is hydrogen; alkyl optionally substituted by --OH, alkoxy, --NR.sub.6 R.sub.7 as defined for R.sub.1, guanidine, --CO.sub.2 H, --CONH.sub.2, --SH, or --S--alkyl; or --CH.sub.2 --Ar where Ar is optionally substituted aryl or heteroaryl; and R.sub.9 is alkoxy; --OH; or --NR.sub.6 R.sub.7 as defined for R.sub.1 ; R.sub.2 is hydrogen; C.sub.2-8 alkanoyl; or optionally substituted aroyl; R.sub.3 is C.sub.3-6 alkyl; and R.sub.4 is --(CH.sub.2).sub.m -- where m is an integer from 4 to 12.