4-aminopyridazines, method of preparing them and drugs containing these
compounds
    1.
    发明授权
    4-aminopyridazines, method of preparing them and drugs containing these compounds 失效
    4-氨基哒嗪,其制备方法和含有这些化合物的药物

    公开(公告)号:US5795892A

    公开(公告)日:1998-08-18

    申请号:US793445

    申请日:1997-02-28

    摘要: The invention concerns new 4-aminopyridazines of the general formula I ##STR1## in which R.sup.1 denotes an R.sup.2 --SO.sub.2 --O-- or R.sup.2 --SO.sub.2 --NR.sup.3 -- group in which R.sup.2 denotes a cycloalkyl residue, an unsubstituted or substituted aryl or heteroaryl residue, R.sup.3 denotes a hydrogen atom, an alkyl or alkyloxyalkyl group which can be unsubstituted or substituted once or several times by hydroxy groups wherein the hydroxy groups can be substituted by alkyl, hydroxyalkyl, alkyloxyalkyl, hydroxyalkyloxyalkyl or alkylcarbonyl groups and wherein in each case two vicinal hydroxy groups can be linked together by alkylidene groups, as well as hydrates, solvates and physiologically tolerated salts thereof. The invention also concerns the optically active forms, racemates and mixtures of diastereomers of these compounds, processes for their production and pharmaceutical agents containing these compounds having a thrombin-inhibiting action.

    摘要翻译: PCT No.PCT / EP95 / 03383 Sec。 371日期1997年2月28日 102(e)日期1997年2月28日PCT 1995年8月26日PCT PCT。 公开号WO96 / 06832 日期1996年3月7日本发明涉及通式Ⅰ(I)的新的4-氨基哒嗪,其中R1表示R2-SO2-O-或R2-SO2-NR3-基团,其中R2表示环烷基残基, 未取代或取代的芳基或杂芳基残基,R3表示氢原子,烷基或烷氧基烷基,其可以是未取代的或被羟基取代一次或几次,其中羟基可以被烷基,羟烷基,烷氧基烷基,羟基烷氧基烷基或烷基羰基 基团,并且其中在每种情况下,两个邻位羟基可以通过亚烷基连接在一起,以及其水合物,溶剂化物和生理上耐受的盐。 本发明还涉及这些化合物的光学活性形式,外消旋物和非对映异构体的混合物,其制备方法和含有这些具有凝血酶抑制作用的化合物的药剂。

    Phosphonates, process for preparing the same and medicaments
    2.
    发明授权
    Phosphonates, process for preparing the same and medicaments 失效
    膦酸盐,其制备方法和药物

    公开(公告)号:US6037334A

    公开(公告)日:2000-03-14

    申请号:US297089

    申请日:1999-07-15

    摘要: Compounds of formula I ##STR1## in which R.sub.1, R.sup.2 are the same or different and denote a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, an alkenyl group, an alkinyl group or an aralkyl group or R.sup.1 and R.sup.2 together denote an alkylene residue which, together with the bound oxygen atoms and the phosphorus atom carrying the oxygen atoms, forms a saturated 5-membered to 8-membered ring;R.sup.3 denotes an optionally substituted amino group, an alkyl group, a cycloalkyl residue or an optionally substituted aryl residue;n denotes an integer between 1 and 4,as well as hydrates, solvates and physiologically tolerated salts thereof, their optically active forms, processes for their production as well as pharmaceutical preparations having factor Xa-inhibitory properties which contain these compounds.

    摘要翻译: PCT No.PCT / EP97 / 06365 Sec。 371日期:1999年7月15日 102(e)日期1999年7月15日PCT 1997年11月14日PCT PCT。 第WO98 / 22483号公报 日期1998年5月28日,式I化合物,其中R 1,R 2相同或不同,表示氢原子,烷基,环烷基,羟基烷基,烯基,炔基或芳烷基或R 1和 R2一起表示亚烷基残基,其与结合的氧原子和携带氧原子的磷原子一起形成饱和的5元至8元环; R3表示任选取代的氨基,烷基,环烷基残基或任选取代的芳基残基; n表示1和4之间的整数,以及其水合物,溶剂化物和生理上耐受的盐,它们的光学活性形式,其制备方法以及含有这些化合物的具有因子Xa抑制性质的药物制剂。

    1,2-diamino compounds, processes for their preparation and
pharmaceutical compositions containing them

    公开(公告)号:US4927834A

    公开(公告)日:1990-05-22

    申请号:US230946

    申请日:1988-08-11

    摘要: The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical which can be substituted by phenyl, naphthyl or a C.sub.3 -C.sub.7 -cycloalkyl radical; a straight-chained or branched C.sub.2 -C.sub.6 -alkenyl radical which can be substituted by a C.sub.3 -C.sub.7 -cycloalkyl radical or a phenyl or naphthyl radical; a C.sub.3 -C.sub.7 -cycloalkyl radical or a mono- or bicyclic aromatic radical which is unsubstituted or substituted one or more times, the substituents being C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl or carbethoxy, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.6 -alkyl radicals which are optionally substituted by hydroxyl, C.sub.1 -C.sub.3 -alkoxy or C.sub.1 -C.sub.3 -alkoxy-C.sub.1 -C.sub.3 -alkoxy or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and is optionally substituted by a lower alkyl or lower alkoxy radical or by an oxygen atom, A is a valency bond or a straight-chained or branched alkylene radical containing up to 6 and preferably up to 3 carbon atoms, R.sub.4 is a mono- or bicyclic aromatic or heteroaromatic radical which is unsubstituted or substituted one or more times, whereby the substituents are alkyl, C.sub.2 -C.sub.6 -alkenyl, alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, hydroxyalkyl, C.sub.2 -C.sub.6 -alkylenedioxy, hydroxyalkoxy, alkoxyethoxy, alkylamino, dialkylamino, alkoxycarbonylethyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulphonyloxy, carboxyl, alkoxycarbonyl, aminocarbonyl, mono- or dialkylaminocarbonyl, haloalkyl or cyano, as well as halogen atoms, such as chlorine, bromine or fluorine, X is a valency bond or a straight-chained or branched, saturated or unsaturated hydrocarbon radical containing up to 6 carbon atoms, Y is a valency bond or an oxygen atom and R.sub.5 is a C.sub.3 -C.sub.7 -cycloalkyl radical or a mono- or bicyclic aromatic or heteroaromatic radical which is unsubstituted or substituted one or more times, the substituents being alkyl, alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, aralkoxy, hydroxyl, hydroxyalkoxy, alkoxyalkoxy, alkoxycarbonylalkoxy, C.sub.1 -C.sub.2 -alkenylenedioxy, dialkylamino, alkylthio, alkylsulphinyl, alkyl-sulphonyl, alkylsulphonyloxy, hydroxyalkyl, carboxyl, alkoxycarbonyl, aminocarbonyl, mono- or dialkylaminocarbonyl or cyano, as well as halogen atoms, such as chlorine, bromine or fluorine, with the proviso that Y cannot be an oxygen atom when X is a valency bond and that when R.sub.1 is a saturated hydrocarbon radical, X must be a radical with at least 2 carbon atoms; as well as the pharmacologically acceptable salts thereof and the optical isomers thereof.The present invention also provides processes for the preparation of these 1,2-diamino compounds and pharmaceutical compositions containing them.

    Use of thiazoloisoindolinone derivatives as antiviral medicaments
    10.
    发明授权
    Use of thiazoloisoindolinone derivatives as antiviral medicaments 失效
    噻唑并二吲哚啉酮衍生物作为抗病毒药物的使用

    公开(公告)号:US5397794A

    公开(公告)日:1995-03-14

    申请号:US50067

    申请日:1993-07-20

    CPC分类号: A61K31/425 Y10S514/934

    摘要: The present invention concerns the use of compounds of the general formula I ##STR1## for the preparation of medicaments for the treatment of viral or retroviral infections, whereby R signifies a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl radical with 1-7 carbon atoms, which can possibly be substituted by phenyl, or a phenyl ring which can possibly be substituted one or more times by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, hydroxyl, trifluoromethyl, methylsulphonyl or halogen, such as fluorine, chlorine or bromine, n stands for the numbers 0, 1 or 2, as well as of their pharmacologically compatible salts or tautomers.

    摘要翻译: PCT No.PCT / EP91 / 02101 Sec。 371日期:1993年7月20日 102(e)日期1993年7月20日PCT 1991年11月6日PCT PCT。 公开号WO92 / 08457 日期:1992年5月29日。本发明涉及通式I的化合物(I)用于制备用于治疗病毒或逆转录病毒感染的药物,其中R表示氢原子或直链 或具有1-7个碳原子的支链,饱和或不饱和的烷基,其可以被苯基取代,或可以被C1-C4-烷基,C1-C4-烷氧基,羟基取代一次或多次的苯环 ,三氟甲基,甲基磺酰基或卤素如氟,氯或溴,n代表数字0,1或2,以及它们的药理学上相容的盐或互变异构体。