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19 条记录 (耗时 0.035 秒)

    Benzazepinone derivatives
    1.
    发明授权
    Benzazepinone derivatives 失效

    公开(公告)号：US5610153A

    公开(公告)日：1997-03-11

    申请号：US454106

    申请日：1994-07-12

    申请人： Peter Buhlmayer ,  Pascal Furet

    发明人： Peter Buhlmayer ,  Pascal Furet

    IPC分类号： A61K31/55 ,  A61K31/554 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/28 ,  A61P43/00 ,  C07D267/14 ,  C07D281/10 ,  C07D513/04

    CPC分类号： C07D267/14 ,  C07D281/10

    摘要： The invention relates to substituted 3-amino-1-arylalkyl-benzazepin-2-ones of the general formula ##STR1## wherein Ar is aryl;X is --O-- or --S(O).sub.n -- and n is 0, 1 or 2;X.sub.1 is C.sub.1 -C.sub.2 alkylene or a direct bond;R.sub.1 is hydrogen, lower alkyl, aryl-lower alkyl or acyl;R.sub.2 is lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkoxy-lower alkyl, aryl-lower alkyl or C.sub.3 -C.sub.7 cycloalkyl-lower alkyl;R.sub.3 is carboxy; lower alkoxycarbonyl; lower alkoxy-lower alkoxycarbonyl; aryl-lower alkoxycarbonyl; aryloxycarbonyl; carbamoyl; carbamoyl that (i) is monosubstituted by hydroxy, lower alkanesulfonyl, halo-lower alkanesulfonyl or by arylsulfonyl, (ii) is monosubstituted or disubstituted, the substituents being independent of one another, by lower alkyl, lower alkenyl, lower alkynyl or by phenyl-lower alkyl or (iii) is disubstituted by lower alkylene or by lower alkylene-Z.sub.1 -lower alkylene, Z.sub.1 being O, S or NH; 5-tetrazolyl; PO.sub.2 H.sub.2 ; PO.sub.3 H.sub.2 or SO.sub.3 H.sub.2 ; the ring A and aromatic radicals are, independently of one another, unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of: lower alkyl, aryl-lower alkyl, lower alkoxy-lower alkyl, lower alkoxy, lower alkoxy-lower alkoxy, aryl-lower alkoxy, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl-lower alkyl, nitro, halogen, trifluoromethyl, amino and amino that is monosubstituted or disubstituted, the substituents being independent of one another, by lower alkyl, aryl-lower alkyl or by aryl, or disubstituted by lower alkylene or by lower alkyleneoxy-lower alkylene;or a salt thereof; to processes for the preparation thereof; and to the use thereof as well as to pharmaceutical compositions that comprise compounds of formula (I) or pharmaceutically acceptable salts thereof.

    Substituted benzazepinones
    2.
    发明授权
    Substituted benzazepinones 失效
    取代苯并氮杂酮

    公开(公告)号：US5683997A

    公开(公告)日：1997-11-04

    申请号：US446700

    申请日：1995-06-09

    申请人： Peter Buhlmayer ,  Pascal Furet

    发明人： Peter Buhlmayer ,  Pascal Furet

    IPC分类号： A61K31/55 ,  A61P43/00 ,  C07D223/16

    CPC分类号： C07D223/16

    摘要： The invention relates to substituted 3-amino-1-arylalkyl-benzazepin-2-ones of the general formula ##STR1## wherein the substituents are defined in the specification; or salts thereof; to processes for the preparation thereof; and to the use thereof as well as to pharmaceutical compositions that comprise compounds of formula (I) or pharmaceutically acceptable salts thereof.

    摘要翻译： PCT No.PCT / EP93 / 03425 371日期：1995年7月12日 102（e）日期1995年7月12日PCT 1993年12月6日PCT PCT。 公开号WO94 / 13642 日期1994年6月23日本发明涉及通式（I）的取代的3-氨基-1-芳烷基 - 苯并氮杂-2-酮，其中取代基在说明书中定义; 或其盐; 其制备方法; 以及其用途以及包含式（I）化合物或其药学上可接受的盐的药物组合物。

    Selective NPY (Y5) antagonists
    5.
    发明申请
    Selective NPY (Y5) antagonists 失效
    选择性NPY（Y5）拮抗剂

    公开(公告)号：US20050137240A1

    公开(公告)日：2005-06-23

    申请号：US11040328

    申请日：2005-01-20

    申请人： Mohammad Marzabadi ,  Wai Wong ,  Stewart Noble ,  Peter Buhlmayer ,  Heinrich Rueger ,  Yasuchika Yamaguchi ,  Walter Schilling

    发明人： Mohammad Marzabadi ,  Wai Wong ,  Stewart Noble ,  Peter Buhlmayer ,  Heinrich Rueger ,  Yasuchika Yamaguchi ,  Walter Schilling

    IPC分类号： C07D277/42 ,  C07D277/60 ,  C07D417/12 ,  C07D513/04 ,  A61K31/426 ,  C07D277/38

    CPC分类号： C07D277/60 ,  C07D277/42 ,  C07D417/12 ,  C07D513/04

    摘要： This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. The invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.

    摘要翻译： 本发明涉及作为NPY（Y5）受体的选择性拮抗剂的双环和三环化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明提供通过将治疗有效量的本发明化合物和药学上可接受的载体组合而制备的药物组合物。 本发明提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了本发明化合物用于制备用于治疗异常的药物组合物的用途，其中所述异常通过降低人Y5受体的活性而减轻。

    Acyl compounds
    9.
    发明授权
    Acyl compounds 失效
    酰基化合物

    公开(公告)号：US5399578A

    公开(公告)日：1995-03-21

    申请号：US998755

    申请日：1992-12-29

    申请人： Peter Buhlmayer ,  Franz Ostermayer ,  Tibur Schmidlin

    发明人： Peter Buhlmayer ,  Franz Ostermayer ,  Tibur Schmidlin

    IPC分类号： A61K31/195 ,  A61K31/41 ,  A61K31/44 ,  A61K31/47 ,  A61K31/535 ,  A61K31/675 ,  A61P9/12 ,  C07C229/38 ,  C07C231/00 ,  C07C233/47 ,  C07C233/51 ,  C07C233/54 ,  C07C235/04 ,  C07C271/10 ,  C07C311/48 ,  C07D233/54 ,  C07D233/58 ,  C07D233/64 ,  C07D257/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07F9/6524

    CPC分类号： C07D233/64 ,  C07C229/38 ,  C07C233/54 ,  C07D257/04 ,  C07D401/12

    摘要： Compounds of the formula ##STR1## in which R.sub.1 is an aliphatic hydrocarbon radical which is unsubstituted or substituted by halogen or hydroxyl, or a cycloaliphatic or araliphatic hydrocarbon radical; X.sub.1 is CO, SO.sub.2, or --O--C(.dbd.O)-- with the carbon atom of the carbonyl group being attached to the nitrogen atom shown in formula I; X.sub.2 is a divalent aliphatic hydrocarbon radical which is unsubstituted or substituted by hydroxyl, carboxyl, amino, guanidino or a cycloaliphatic or aromatic radical, or is a divalent cycloaliphatic hydrocarbon radical, it being possible for a carbon atom of the aliphatic hydrocarbon radical to be additionally bridged by a divalent aliphatic hydrocarbon radical; R.sub.2 is carboxyl which, if desired, is esterified or amidated, substituted or unsubstituted amino, formyl which, if desired, is acetalized, 1H-tetrazol-5-yl, pyridyl, hydroxyl which, if desired, is etherified, S(O).sub.m --R where m is 0, 1 or 2 and R is hydrogen or an aliphatic hydrocarbon radical, alkanoyl, unsubstituted or N-substituted sulfamoyl or PO.sub.n H.sub.2 where n is 2 or 3; X.sub.3 is a divalent aliphatic hydrocarbon; R.sub.3 is carboxyl, 5-tetrazolyl, SO.sub.3 H, PO.sub.2 H.sub.2, PO.sub.3 H.sub.2 or haloalkylsulfamoyl; and the rings A and B independently of one another are substituted or unsubstituted; in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as medicament active ingredients.

    摘要翻译： 式（I）的化合物，其中R 1是未被取代或被卤素或羟基取代的脂族烃基，或脂环族或芳脂族烃基; X 1是CO，SO 2或-O-C（= O） - ，其中羰基的碳原子连接到式I所示的氮原子上; X2是未取代的或被羟基，羧基，氨基，胍基或脂环族或芳族基团取代的二价脂族烃基，或者是二价脂环族烃基，脂族烃基的碳原子可能另外 由二价脂族烃基桥连; R 2是羧基，如果需要，其被酯化或酰胺化，取代或未取代的氨基，如果需要，缩醛化的甲酰基，1H-四唑-5-基，吡啶基，羟基，如果需要，其醚化，S（O） mR，其中m为0,1或2，R为氢或脂族烃基，烷酰基，未取代的或N-取代的氨磺酰基或POnH 2，其中n为2或3; X3是二价脂族烃; R3是羧基，5-四唑基，SO3H，PO2H2，PO3H2或卤代烷基氨磺酰; 环A和B彼此独立地是取代或未取代的; 游离形式或盐形式可以以本身已知的方式制备，并且可以用作例如药物活性成分。