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    Substituted Aminoalkyl- and Amidoalkyl-Benzopyran Derivatives
    12.
    发明申请
    Substituted Aminoalkyl- and Amidoalkyl-Benzopyran Derivatives 审中-公开
    取代的氨基烷基 - 和酰胺基 - 苯并吡喃衍生物

    公开(公告)号：US20090005436A1

    公开(公告)日：2009-01-01

    申请号：US11909095

    申请日：2006-02-22

    申请人： Angelo Carotti ,  Piero Melloni ,  Florian Thaler ,  Carla Caccia ,  Sara Maestroni ,  Patricia Salvati

    发明人： Angelo Carotti ,  Piero Melloni ,  Florian Thaler ,  Carla Caccia ,  Sara Maestroni ,  Patricia Salvati

    IPC分类号： A61K31/353 ,  C07D311/04 ,  A61P25/28

    CPC分类号： C07D311/16 ,  C07D311/58

    摘要： This invention is related to novel aminoalkyl- and amidoalkyl-benzopyran derivatives of the following general formula (I) wherein: the group  is a substituent in position 6 or 7 wherein: R is an aromatic mono- or bi-cyclic carbocyclic ring or a mono- or bi-cyclic heterocyclic ring radical, said rings being optionally substituted by one or two substituents selected from (C1-C5) straight or branched alkyl, (C1-C5) straight or branched alkoxy, hydroxy, halogen and trifluoromethyl; m is zero or an integer from 1 to 3; n, p, R1 and R2 are as herein indicated and R3 and R4 are both hydrogen or taken together represent an oxygen atom, and the pharmaceutically acceptable salts thereof. The compounds that are active as selective and reversible MAO-B inhibitors in vitro and in vivo, are useful as medicaments for the prevention and the treatment of CNS degenerative disorders.

    摘要翻译： 本发明涉及以下通式（I）的新型氨基烷基 - 和酰氨基烷基 - 苯并吡喃衍生物，其中：该基团是6或7位的取代基，其中：R是芳族单环或双环碳环或单 所述环任选被一个或两个选自（C1-C5）直链或支链烷基，（C1-C5）直链或支链烷氧基，羟基，卤素和三氟甲基的取代基取代; m为0或1〜3的整数; n，p，R1和R2如本文所示，R 3和R 4均为氢或一起代表氧原子，及其药学上可接受的盐。 在体外和体内作为选择性和可逆MAO-B抑制剂活性的化合物可用作预防和治疗CNS退行性疾病的药物。

    17-iminomethylalkenyl-5 .beta., 14 .beta.-androstane and 17-iminoalkyl-5 .beta., 14 .beta.-androstane derivatives active on the cardiovascular system, and pharmaceutical compositions containing same
    15.
    发明授权
    17-iminomethylalkenyl-5 .beta., 14 .beta.-androstane and 17-iminoalkyl-5 .beta., 14 .beta.-androstane derivatives active on the cardiovascular system, and pharmaceutical compositions containing same 失效

    公开(公告)号：US5583127A

    公开(公告)日：1996-12-10

    申请号：US363060

    申请日：1994-12-23

    申请人： Alberto Cerri ,  Giuseppe Bianchi ,  Patrizia Ferrari ,  Elena Folpini ,  Piero Melloni

    发明人： Alberto Cerri ,  Giuseppe Bianchi ,  Patrizia Ferrari ,  Elena Folpini ,  Piero Melloni

    IPC分类号： A61K31/575 ,  A61K31/573 ,  A61K31/58 ,  A61P9/00 ,  A61P9/12 ,  C07J41/00 ,  C07J43/00 ,  C07J75/00 ,  A61K31/57 ,  C07J9/00

    CPC分类号： C07J41/005 ,  C07J43/003 ,  C07K2319/00

    摘要： Disclosed are 17-iminomethylalkenyl and 17-iminoalkyl-14.beta.-hydroxy-5.beta.-androstane derivatives of the formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration or a Z or E configuration; A represents (CH.sub.2).sub.m or --(CH.dbd.CH).sub.n --; m represents an integer number from 1 to 6; n represents an integer number from 1 to 3; R.sup.2 represents hydrogen or hydroxy; R.sup.1 represents hydrogen, C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5, which may be the same or different, represent hydrogen, C.sub.1 -C.sub.4 alkyl or R.sup.4 and R.sup.5 may form, when taken together with the nitrogen atom, a five- or six- membered heterocyclic ring optionally containing one or more heteroatoms selected from oxygen and nitrogen; R.sup.3 represents NHC(.dbd.X)NR.sup.6 R.sup.7 or OR.sup.8 wherein R.sup.6 and R.sup.7, which may be the same or different, represent hydrogen, methyl, or C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 have the previously defined meanings; R.sup.8 represents hydrogen, methyl, C.sub.2 -C.sub.6 alkyl, unsubstituted or substituted by one or more NR.sup.4 R.sup.5 or NHC(.dbd.NH)NH.sub.2, wherein R.sup.4 and R.sup.5 have the previously defined meanings; X represents O, S, or NR.sup.9 ; R.sup.9 represents hydrogen, methyl, C.sub.2 -C.sub.4 alkyl, C.sub.2 -C.sub.4 acyl or phenyl, where the C.sub.2 -C.sub.4 alkyl and C.sub.2 -C.sub.4 acyl are unsubstituted or substituted by NR.sup.4 R.sup.5, wherein R.sup.4 and R.sup.5 have the previously defined means; and R.sup.6, R.sup.7, and R.sup.9, taken two by two, may form, together with the heteroatoms to which they are linked, a five- , six- , or seven-membered heterocyclic ring; or mixtures of .alpha. and .beta. isomers at the 3-position; or mixtures of Z and E isomers of the group A--CH.dbd.NR.sup.3 ; or pharmaceutically acceptable salts thereof. The compounds are useful for the treatment of cardiovascular disorders, such as heart failure and hypertension. Also, disclosed is a process for preparing the derivatives by reaction of the corresponding 17-alkyl or 17-methylalkenyl aldehyde with a compound of the formula H.sub.2 NNHC(.dbd.X)NR.sup.6 R.sup.7 or H.sub.2 NOR.sup.8.