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131 条记录 (耗时 0.03 秒)

    SULFONYLBENZENE COMPOUNDS AS ANTI-INFLAMMATORY/ANALGESIC AGENTS
    43.
    发明申请
    SULFONYLBENZENE COMPOUNDS AS ANTI-INFLAMMATORY/ANALGESIC AGENTS 审中-公开
    磺酰苯类化合物作为抗炎/灭菌剂

    公开(公告)号：WO99064415A1

    公开(公告)日：1999-12-16

    申请号：PCT/IB1999/000970

    申请日：1999-05-31

    IPC分类号： C07D409/10 ,  A61K31/085 ,  A61K31/135 ,  A61K31/33 ,  A61K31/335 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/395 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/45 ,  A61P1/02 ,  A61P19/06 ,  A61P21/00 ,  A61P29/00 ,  A61P43/00 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D405/10 ,  C07D413/10 ,  C07D417/10

    CPC分类号： C07C311/39 ,  C07C317/36 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D417/10

    摘要： This invention provides a compound of formula (I) or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R is heteroaryl; R is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R , R and R are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R , R and R are taken together with atoms to which they are attached and form a 4-7 membered ring; R and R are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

    摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中A是部分不饱和或不饱和的五元杂环或部分不饱和或不饱和五元碳环，其中4-（磺酰基）苯基和4-取代 式（I）中的苯基与环A相邻的环原子连接; R 1是任选取代的芳基或杂芳基，条件是当A是吡唑时，R 1是杂芳基; R 2是C 1-4烷基，卤素取代的C 1-4烷基，C 1-4烷基氨基，C 1-4二烷基氨基或氨基; R 3，R 4和R 5独立地是氢，卤素，C 1-4烷基，卤素取代的C 1-4烷基等; 或R 3，R 4和R 5中的两个与它们所连接的原子一起形成4-7元环; R 6和R 7独立地是氢，卤素，C 1-4烷基，卤素取代的C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-4烷基氨基或N，N-二C1- 4烷基氨基; m和n分别为1,2,3或4.本发明还提供了一种药物组合物，其用于治疗前列腺素涉及病原体的医疗状况。

    SULFONAMIDE DERIVATIVES AND THEIR USE
    44.
    发明申请
    SULFONAMIDE DERIVATIVES AND THEIR USE 审中-公开
    磺酰胺衍生物及其用途

    公开(公告)号：WO1995024186A1

    公开(公告)日：1995-09-14

    申请号：PCT/US1995003223

    申请日：1995-03-10

    申请人： PHARMACOPEIA, INC. ,  BALDWIN, John, J. ,  OHLMEYER, Michael, H., J. ,  HENDERSON, Ian

    发明人： PHARMACOPEIA, INC.

    IPC分类号： A61K31/095

    CPC分类号： C07D285/125 ,  C07C205/59 ,  C07C311/16 ,  C07C311/39 ,  C07D211/22 ,  C07D211/46 ,  C07D211/62 ,  C07D307/68 ,  C07D333/38 ,  C07D401/12 ,  C07D401/14 ,  C40B40/00

    摘要： Combinatorial libraries are disclosed which are represented by the formula (I): (T'-L)q- -C(O)-L'-II' wherein: is a solid support; T'-L- is an identifier residue; and -L'-II' is a ligand/linker residue. These libraries contain aryl sulfonamides, N-acyl derivatives, and N-substituted pyrrolidines and piperidines of the formula: Y-A-CO-R which are inhibitors of serine proteases and carbonic anhydrase isozymes. They are useful in the treatment of hyper-coagulation disease and ocular diseases such as glaucoma.

    摘要翻译： 公开了由式（I）表示的组合文库：（T'-L）q -C（O）-L'-II'其中：S是固体载体; T'-L-是标识符残基; 和-L'-II'是配体/接头残基。 这些文库含有作为丝氨酸蛋白酶和碳酸酐酶同功酶抑制剂的芳基磺酰胺，N-酰基衍生物和N-取代的吡咯烷和下式的分子式为：Y-A-CO-R 1的哌啶。 它们可用于治疗高凝血性疾病和眼部疾病如青光眼。

    2-(2-AMINOPHENOXY)-3-CHLORONAPHTHALENE-1,4-DIONE COMPOUNDS HAVING OREXIN 2 RECEPTOR AGONIST ACTIVITY
    46.
    发明申请
    2-(2-AMINOPHENOXY)-3-CHLORONAPHTHALENE-1,4-DIONE COMPOUNDS HAVING OREXIN 2 RECEPTOR AGONIST ACTIVITY 审中-公开
    具有OREXIN 2受体激动剂活性的2-（2-氨基苯氧基）-3-氯代萘基-1,4-二酮化合物

    公开(公告)号：WO2014198880A1

    公开(公告)日：2014-12-18

    申请号：PCT/EP2014/062349

    申请日：2014-06-13

    申请人： FERRER INTERNACIONAL, S.A.

    发明人： CANO, Montserrat ,  GRIMA, Pedro Manuel ,  PALOMER BENET, Albert

    IPC分类号： C07C255/59 ,  C07C205/38 ,  C07C311/16 ,  C07C217/52 ,  C07C217/76 ,  C07C225/20 ,  C07C229/60 ,  A61P3/04 ,  A61P25/00

    CPC分类号： C07C255/59 ,  C07C217/88 ,  C07C217/94 ,  C07C225/22 ,  C07C229/64 ,  C07C235/38 ,  C07C311/39

    摘要： The invention provides a compound of formula (I) wherein R 2 -R 10 represent different meanings, and pharmaceutically acceptable salts thereof. The invention also provides synthetic procedures for preparing the compounds of formula (I), pharmaceutical compositions comprising them, their use as medicaments, their use as therapeutic active substances for the treatment of conditions mediated by agonizing the orexin 2 receptor, and their use as therapeutic active substances for the treatment of narcolepsy, excessive daytime sleepiness, nighttime insomnia, depression, sleep apnea and jet lag, for promoting wakefulness and emergence from anesthesia, and for preventing diet-induced obesity.

    摘要翻译： 本发明提供其中R 2 -R 10表示不同含义的式（I）化合物及其药学上可接受的盐。 本发明还提供了制备式（I）化合物的合成方法，包含它们的药物组合物，它们作为药物的用途，它们作为用于治疗通过激素食欲肽2受体介导的病症的治疗活性物质的用途及其作为治疗剂 用于治疗发作性睡眠，白天嗜睡，夜间失眠，抑郁，睡眠呼吸暂停和时差的活性物质，用于促进睡眠和麻醉出现，以及用于预防饮食诱导的肥胖。