(Aminopropyl)methylphosphinic acids
    1.
    发明授权
    (Aminopropyl)methylphosphinic acids 失效
    (氨基丙基)甲基次膦酸

    公开(公告)号:US06596711B1

    公开(公告)日:2003-07-22

    申请号:US09786220

    申请日:2001-03-01

    CPC classification number: C07C271/16 C07C215/08 C07F9/301

    Abstract: Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)methylphosphinic acid; ii) (S)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iii) (R)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iv) (3-amino-2-hydroxypropyl)difluoromethylphosphinic acid; and v) (3-amino-2-oxopropyl)methylphosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.

    Abstract translation: (3-氨基-2-羟丙基)甲基次膦酸的外消旋物; ii)(S) - (3-氨基-2-羟丙基)甲基次膦酸; iii)(R) - (3-氨基-2-羟丙基)甲基次膦酸; iv)(3-氨基-2-羟丙基)二氟甲基次膦酸; 对于一种或多种GABA B受体具有亲和性,它们的药学上可接受的盐,溶剂合物和立体异构体,以及它们的制备方法,含有所述治疗活性化合物的药物组合物和 所述活性化合物在治疗中的用途。

    Imidazo pyridine derivatives which inhibit gastric acid secretion
    4.
    发明授权
    Imidazo pyridine derivatives which inhibit gastric acid secretion 失效
    抑制胃酸分泌的咪唑吡啶衍生物

    公开(公告)号:US06313136B1

    公开(公告)日:2001-11-06

    申请号:US09319890

    申请日:1999-06-14

    CPC classification number: C07D471/04

    Abstract: The present invention relates to imidazo pyridine derivatives of the formula (I), in which the phenyl moiety is substituted, and in which the imidazo pyridine moiety is substituted with a carboxamide group in 6-position, which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.

    Abstract translation: 本发明涉及式(I)的咪唑并吡啶衍生物,其中苯基部分被取代,其中咪唑并吡啶部分被6位的羧酰胺基团取代,其抑制外源或内源性刺激的胃酸分泌 因此可用于预防和治疗胃肠道炎性疾病。

    Heterocyclic Sulfonamide Derivatives as Inhibitors of Factor Xa

    公开(公告)号:US20080214495A1

    公开(公告)日:2008-09-04

    申请号:US11994846

    申请日:2006-07-05

    CPC classification number: C07D409/14 C07D401/04 C07D401/14

    Abstract: The invention relates to compounds of formula (I), wherein R1 and R3 are independently selected from carbon and nitrogen; R2 is oxo or thioxo; n is 0, 1 or 2; each R10 is independently selected from hydrogen and C1-3alkyl; R4 and R5 are each selected from carbon and nitrogen, wherein at least one of R4 and R5 is nitrogen; R6 is hydrogen or oxo; R7 is an aliphatic, partially saturated or aromatic carbocyclic ring, said carbocyclic ring having 0, 1 or 2 hetero nitrogen; m is 0, 1 or 2; each R11 is independently selected from hydrogen, hydroxy, oxo, C1-5alkyl, carboxy, hydroxyC1-5alkyl, carboxyC1-5alkyl, C1-5alkoxy-oxoC1-5alkyl, carbamoyl, C1-5alkylcarbamoyl, di (C1-5 alkyl)carbamoyl, carbamoylC1-4alkyl,C1-5alkylcarbamoylC1-4alkyl, di(C1-5alkyl)carbamoylC1-4alkyl, hydroxyC1-5alkylcarbamoyl, C1-5 alkoxyC1-5alkylcarbamoyl, hydroxyC1-5alkylcarbamoylC1-4alkyl, C1-5alkoxyC1-5 alkylcarbamoylC1-4 alkyl, CONR80(CH2)xS(O)pR90, CONH(CH2)qNR100R100, —C1-5 alkyl-Y1, —COOCHR170R180 and —CON R170R180; R8 is a bond, C1-4alkylene or C2-6alkenylene; R9 is an aromatic ring system having 0, 1 or 2 hetero atoms; wherein R9 is substituted by 0 or 1 halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.

    Imidazo[1,2-a]pyridine compounds
    10.
    发明授权
    Imidazo[1,2-a]pyridine compounds 有权
    咪唑并[1,2-a]吡啶化合物

    公开(公告)号:US06613775B1

    公开(公告)日:2003-09-02

    申请号:US09403510

    申请日:1999-10-22

    CPC classification number: C07D471/04

    Abstract: The present invention relates to novel compounds, and therapeutically acceptable salts thereof of the formula (I), which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.

    Abstract translation: 本发明涉及抑制外源性或内源性刺激的胃酸分泌的式(I)的新化合物及其治疗上可接受的盐,因此可用于预防和治疗胃肠炎性疾病。

Patent Agency Ranking