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9 条记录 (耗时 0.029 秒)

    Diazepinoindoles as phosphodiesterase IV inhibitors
    4.
    发明授权
    Diazepinoindoles as phosphodiesterase IV inhibitors 失效
    二氮杂吲哚作为磷酸二酯酶IV抑制剂

    公开(公告)号：US5852190A

    公开(公告)日：1998-12-22

    申请号：US391865

    申请日：1995-02-22

    申请人： Yves Pascal ,  Indres Moodley ,  Alain Calvet ,  Jean-Louis Junien

    发明人： Yves Pascal ,  Indres Moodley ,  Alain Calvet ,  Jean-Louis Junien

    IPC分类号： A61K31/55 ,  A61K31/5517 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D487/06 ,  C07D243/24

    CPC分类号： C07D487/06 ,  A61K31/5517

    摘要： The invention relates to diazepinoindoles of formula: ##STR1## in which R is hydrogen, lower alkyl or lower alkoxy; A is aryl or nitrogen-containing heteroaryl, each of which is optionally substituted by from one to three groups of halogen, lower alkyl, haloalkyl, lower alkoxy and acetamido, or their racemic forms, isomers or pharmaceutically acceptable salts, wherein for the racemic forms of the (S) configuration, A is not phenyl, haloalkyl, or 2-indolyl when R is hydrogen, and for the racemic forms of the (R) configuration, A is not 2-indolyl when R is hydrogen. Also, the invention relates to a method for inhibiting cyclic nucleotide phosphodiesterase activity by administering these compounds to a subject in an amount which is therapeutically effective to inhibit cyclic nucleotide phosphodiesterase activity.

    摘要翻译： 本发明涉及式为：其中R为氢，低级烷基或低级烷氧基的下式的二氮茚并吲哚; A是芳基或含氮杂芳基，其各自任选被一至三个卤素，低级烷基，卤代烷基，低级烷氧基和乙酰氨基取代，或其外消旋形式，异构体或药学上可接受的盐，其中对于外消旋形式 的（S）构型，当R是氢时，A不是苯基，卤代烷基或2-吲哚基，对于（R）构型的外消旋形式，当R是氢时，A不是2-吲哚基。 此外，本发明涉及通过以对治疗有效抑制环核苷酸磷酸二酯酶活性的量将这些化合物给予受试者来抑制环核苷酸磷酸二酯酶活性的方法。

    Propanamines, their pharmacological properties and their application for therapeutic in particular antidiarrheal, purposes
    8.
    发明授权
    Propanamines, their pharmacological properties and their application for therapeutic in particular antidiarrheal, purposes 失效
    丙氨酸，其药理学特性及其在特异性抗病毒治疗中的应用，目的

    公开(公告)号：US5143938A

    公开(公告)日：1992-09-01

    申请号：US660873

    申请日：1991-02-26

    申请人： Alain Calvet ,  Agnes Grouhel ,  Henri Jacobelli ,  Jean-Louis Junien ,  Xavier Pascaud

    发明人： Alain Calvet ,  Agnes Grouhel ,  Henri Jacobelli ,  Jean-Louis Junien ,  Xavier Pascaud

    IPC分类号： A61K31/135 ,  A61K31/335 ,  A61K31/357 ,  A61K31/385 ,  C07C205/04 ,  C07C205/09 ,  C07C205/32 ,  C07C205/45 ,  C07C215/30 ,  C07C217/72 ,  C07C225/16 ,  C07C225/18 ,  C07C323/29 ,  C07D317/28 ,  C07D339/06

    CPC分类号： C07C225/16 ,  C07C205/04 ,  C07C205/09 ,  C07C205/32 ,  C07C205/45 ,  C07C217/72 ,  C07D317/28

    摘要： A compound which is a propanamine of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted,or is a 5- or 6-membered monocyclic heteroaryl radical in which the single heteroatom is nitrogen, oxygen or sulfur,R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkylalkyl radical,or, together with the nitrogen atom to which they are attached, form a saturated 5- to 6-membered heterocycle comprising only one heteroatom,R5 is a 5- to 7-membered cycloalkyl radical, a phenyl radical or a 5- or 6-membered monocyclic heteroaryl radical,and W representsa group .dbd.CH--QH,or a heterocycle .dbd.C[Q--(CH2)n--Q],or a group .dbd.C.dbd.Q, in which groupsQ is an oxygen or sulfur atom,n has the value 2 or 3,W being .dbd.C.dbd.Q only when R3 and R4 are not both hydrogen, and their additions salts with pharmaceutically acceptable acids.A pharmaceutical composition comprising a compound of general formula (I) with the above definitions for the treatment of diarrheal states.

    摘要翻译： 作为通式（I）的丙胺的化合物，其中：R 1是任选被一个，二或三取代的苯基，或是5或6元单环杂芳基，其中 单个杂原子是氮，氧或硫，R2是低级烷基，R3和R4是氢原子或低级烷基，低级烯基或低级环烷基烷基，或者与它们相连的氮原子一起形成 饱和的5至6元杂环，仅包含一个杂原子，R 5为5-至7-元环烷基，苯基或5-或6-元单环杂芳基，W表示基团= CH-QH， 或杂环= C [Q-（CH 2）nQ]或基团= C = Q，其中基团Q是氧或硫原子，n具有值2或3，W仅当R 3为 和R4不同时为氢，并且它们与药学上可接受的酸相加。 一种药物组合物，其包含具有上述定义用于治疗腹泻状态的通式（I）的化合物。

    Derivatives of midecamycine
    9.
    发明授权
    Derivatives of midecamycine 失效
    美沙昔明的衍生物

    公开(公告)号：US4141971A

    公开(公告)日：1979-02-27

    申请号：US701291

    申请日：1976-06-30

    申请人： Francois Krausz ,  Alain Calvet

    发明人： Francois Krausz ,  Alain Calvet

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： Novel derivatives of midecamycine, of the formula: ##STR1## wherein X represents an oxygen atom or a sulphur atom, R.sub.1 represents a straight or branched alkyl group, an alkenyl group or an aryl group, R.sub.2 represents a hydrogen atom or a lower acyl group, the dotted lines represent the possible presence of double bonds, it being understood that the 2 double bonds at the 10,11 position on the one hand and the 12,13 position on the other either exist simultaneously or neither of them exists, which give by oral administration plasma rates which are higher than midecamycine and which lack its bitter taste, together with their process of preparation.

    摘要翻译： 其中X代表氧原子或硫原子，R1代表直链或支链烷基，链烯基或芳基，R2代表（I）+（R） 氢原子或低级酰基，虚线表示可能存在双键，据了解，一方面在10,11位置的2个双键和另一方面的12,13位置同时存在 或者它们都不存在，其通过口服给药的血浆速率高于美沙昔星并且其缺乏苦味，以及它们的制备方法。