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13 条记录 (耗时 0.069 秒)

    Mineralocorticoid Receptor Antagonists
    2.
    发明申请
    Mineralocorticoid Receptor Antagonists 审中-公开
    盐皮质激素受体拮抗剂

    公开(公告)号：US20100120736A1

    公开(公告)日：2010-05-13

    申请号：US12593746

    申请日：2007-03-29

    申请人： Bernardus Wijnand Machijs Marie Peeters ,  Marinus Bernard Groen ,  Ralf Plate

    发明人： Bernardus Wijnand Machijs Marie Peeters ,  Marinus Bernard Groen ,  Ralf Plate

    IPC分类号： A61K31/57 ,  C07J7/00 ,  A61P43/00

    CPC分类号： C07J7/00 ,  A61K31/56 ,  Y02P20/582

    摘要： Compounds of the formula (I) are provided having a steroid skeleton and substitution characteristics in the A and B rings of the steroid skeleton effective for mineralocorticoid receptor antagonism, and rings C and D of the steroid skeleton having substituents thereon according to formula (I), wherein R1 is —OH or ═O; R2 is (C1-3)alkyl or (C2-3)alkenyl; R3 is selected from formulas (IIa), (IIb), (IIc). These compounds are useful in the treatment of inter alia aldosteronism, hypokalemia, hypertension, congestive heart failure, heart fibrosis, renal failure and restenosis.

    摘要翻译： 提供式（I）化合物，其具有类固醇骨架和在类固醇骨架的A环和B环中有效用于盐皮质激素受体拮抗作用的取代特性，并且具有根据式（I）的取代基的类固醇骨架的环C和D， 其中R 1为-OH或= O; R2是（C1-3）烷基或（C2-3）烯基; R3选自式（IIa），（IIb），（IIc）。 这些化合物可用于治疗尤其是醛固酮增多症，低钾血症，高血压，充血性心力衰竭，心脏纤维化，肾衰竭和再狭窄。

    3-quinuclidine derivatives
    3.
    发明授权
    3-quinuclidine derivatives 失效
    3-奎宁环衍生物

    公开(公告)号：US5258392A

    公开(公告)日：1993-11-02

    申请号：US830107

    申请日：1992-01-31

    申请人： Johannes H. Wieringa ,  Sjoerd F. van Aelst ,  Ralf Plate

    发明人： Johannes H. Wieringa ,  Sjoerd F. van Aelst ,  Ralf Plate

    IPC分类号： A61K31/435 ,  A61P25/28 ,  C07D453/02 ,  A61K31/445

    CPC分类号： C07D453/02 ,  Y10S514/879

    摘要： The invention relates to a 3-quinuclidine derivative having the formula I ##STR1## wherein X is O or S, and R represents one to five substituents independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower aralkyloxy, lower alkanoyloxy, halogen, NO.sub.2, CF.sub.3, CN, NR.sub.1 R.sub.2, and COR.sub.3, in which R.sub.1 and R.sub.2 are independently selected from hydrogen, lower alkyl, and lower alkanoyl, and R.sub.3 is selected from OH, lower alkyl, lower alkoxy, and NR.sub.4 R.sub.5, wherein R.sub.4 and R.sub.5 are independently hydrogen or lower alkyl; or pharmaceutically acceptable salts thereof.

    3-methylene steroid derivatives
    6.
    发明授权
    3-methylene steroid derivatives 失效
    3-亚甲基类固醇衍生物

    公开(公告)号：US06579864B1

    公开(公告)日：2003-06-17

    申请号：US10148247

    申请日：2002-05-29

    申请人： Ralf Plate ,  Wilhelmina Maria Bagchus

    发明人： Ralf Plate ,  Wilhelmina Maria Bagchus

    IPC分类号： A61K3156

    CPC分类号： C07J71/001 ,  C07J1/007 ,  C07J1/0096

    摘要： The invention concerns a 3-methylene steroid derivative having general formula (1) wherein R1 is H or together with R3 forms a &bgr;-epoxide or R1 is absent if there is a 5-10 or 4-5 double bond; R2 is (C1-C5) alkyl or CF3; R3 is &bgr;H, &bgr;CH3 or together with R1 forms a &bgr;-epoxide or R3 is absent if there is a 5-10 double bond; R4 is H, lower alkyl; Y is [H, H], [OH, H], ═O, [OH, lower alkyl], [OH, (C2-C5)alkenyl], [OH, (C2-C5)alkynyl] or (C1-C6) alkylidene, whereby said alkyl, alkenyl, alkynyl and alkylidene is optionally halogenated; ═NOR5, whereby R5 is H, lower alkyl; dotted lines represent an optional double bond, or prodrugs thereof for the treatment of arthritic diseases and/or autoimmune diseases.

    摘要翻译： 本发明涉及具有通式（1）的3-亚甲基类固醇衍生物，其中R 1为H或与R 3一起形成β-环氧化物，如果存在5-10或4-5个双键，则R1不存在; R2是（C1-C5）烷基或CF3; R3是βH，βCH3或与R1一起形成β-环氧化物，如果存在5-10个双键，则R3不存在; R4是H，低级烷基; Y是[H，H]，[OH，H]，= O，[OH，低级烷基]，[OH，（C 2 -C 5）烯基]，[OH，（C 2 -C 5）炔基]或（C 1 -C 6 ）亚烷基，其中所述烷基，烯基，炔基和亚烷基任选被卤化; = NOR5，其中R5是H，低级烷基; 虚线代表任选的双键或其用于治疗关节炎疾病和/或自身免疫疾病的前药。

    Tetrahydropyrimidine derivatives
    7.
    发明授权
    Tetrahydropyrimidine derivatives 失效
    四氢嘧啶衍生物

    公开(公告)号：US5470856A

    公开(公告)日：1995-11-28

    申请号：US25707

    申请日：1993-03-03

    申请人： Ralf Plate

    发明人： Ralf Plate

    IPC分类号： A61K31/505 ,  A61P25/04 ,  A61P25/20 ,  A61P25/28 ,  A61P27/02 ,  A61P27/06 ,  C07D239/06 ,  C07D239/14 ,  C07D239/48 ,  C07D239/42

    CPC分类号： C07D239/06 ,  C07D239/14

    摘要： The invention is concerned with a tetrahydropyrimidine derivative having formula I ##STR1## wherein R.sub.1 is hydrogen;R.sub.2 is hydrogen, a lower alkyl group, or lower acyl; orR.sub.1 and R.sub.2 represent together a bond;R.sub.3 is hydrogen, a lower hydrocarbon group optionally substituted with halogen, CN, aryl, or COR.sub.7 ;R.sub.4 is hydrogen, a lower alk(en)yl group, or aryl;R.sub.5 is hydrogen, amino, lower alkyl substituted amino, or a lower alkyl group; andR.sub.6 is hydrogen or methyl;R.sub.7 is amino, lower alkyl substituted amino, or a lower alkyl group; ora pharmaceutically acceptable salt thereof.The compounds of this invention have muscarinic properties and can be used for the treatment of cognition disorders, and for the treatment of cholinergic deficiencies.

    摘要翻译： 本发明涉及具有式I的四氢嘧啶衍生物，其中R1是氢; R2是氢，低级烷基或低级酰基; 或R 1和R 2一起表示键; R3是氢，任选被卤素，CN，芳基或COR7取代的低级烃基; R4是氢，低级（en）基或芳基; R5是氢，氨基，低级烷基取代的氨基或低级烷基; R6为氢或甲基; R7是氨基，低级烷基取代的氨基或低级烷基; 或其药学上可接受的盐。 本发明的化合物具有毒蕈碱性质，可用于治疗认知障碍和治疗胆碱能缺陷。

    NON STEROIDAL GLUCOCORTICOID RECEPTOR MODULATORS
    9.
    发明申请
    NON STEROIDAL GLUCOCORTICOID RECEPTOR MODULATORS 失效

    公开(公告)号：US20090062262A1

    公开(公告)日：2009-03-05

    申请号：US11816113

    申请日：2006-02-14

    申请人： Ralf Plate ,  Guido Jenny Rudolf Zaman ,  Pedro Harold Han Hermkens ,  Christiaan Gerardus Johannes Maria Jans ,  Rogier Christian Buijsman ,  Adrianus Petrus Antonius De Man ,  Paolo Giovanni Martino Conti ,  Scott James Lusher ,  Willem Hendrik Abraham Dokter

    发明人： Ralf Plate ,  Guido Jenny Rudolf Zaman ,  Pedro Harold Han Hermkens ,  Christiaan Gerardus Johannes Maria Jans ,  Rogier Christian Buijsman ,  Adrianus Petrus Antonius De Man ,  Paolo Giovanni Martino Conti ,  Scott James Lusher ,  Willem Hendrik Abraham Dokter

    IPC分类号： A61K31/551 ,  C07D471/04 ,  A61P29/00 ,  A61P37/00

    CPC分类号： C07D471/04

    摘要： The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. In this formula R1 is H or (1-4C)alkyl; R2 is —C(O)R15 or —S(O)2R15; R3 is H, (1-4C)alkyl or —OR16; R4 is H, (1-4C)alkyl or —OR16; R6 is H or —C(H)NOR16; R7 is H or halogen, cyano; (1-6C)alkyl, (2-6C)alkenyl or (2-6C)alkynyl, all three optionally substituted with OH, halogen or NH2; —C(H)NOR16, —OR16, —C(O)R16, or —C(O)OR16; R8 is H, cyano, halogen, nitro; (1-6C) alkyl, (2-6C)alkenyl, (2-6C)alkynyl or —O(1-6C)alkyl, all optionally substituted with amino, hydroxyl or halogen; (hetero)aryl, optionally substituted with cyano, halogen, (1-4C)alkyl, (1-4C)alkoxy, (1-4C)alkoxy(1-4C)alkyl; —C(O)R18, —C(O)OR19, —C(O)NHR17, —NHC(O)R20, —C(1-4C)alkylNOR21; —C(H)NOR16, or —NHS(O)2R21; R9 is H, halogen, cyano or (1-4C)alkyl optionally substituted with halogen; R10 is H or (1-4C)alkyl; R11 is H; R12 is H, cyano or (1-4C)alkyl; R13 is H, (1-4C)alkyl, halogen or formyl; R14 is H, halogen, cyano, (1-4C)alkyl, (2-6C)alkenyl, C(O)R21 or (hetero)aryl; R15 is H; (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, —O(2-6C)alkyl, —O(2-6C)alkenyl or —O(2-6C)alkynyl, all optionally substituted with one or more OH, halogen, cyano or (hetero)aryl, (hetero)aryl, optionally substituted with (1-4C)alkyl, halogen, cyano, nitro or amino, NH2, (di)(1-4C)alkylamino, (1-4C)alkyl(1-4C)alkoxyamine, (1-4C)alkylthio(1-4C)alkyl or (1-4C)alkoxy(1-4C)alkyl; R16 is H, (1-6C)alkyl, (2-6C)alkenyl or (2-6C)alkynyl; R17 is H, (1-6C)alkyl, optionally substituted with halogen, (1-4C)alkoxy or (hetero)aryl, optionally substituted with halogen, (1-4C)alkyl or (1-25 4C)alkoxy; (3-6C)cycloalkyl or (hetero)aryl, optionally substituted with halogen, (1-4C)alkyl or (1-4C)alkoxy; R18 is H, NH2, C(O)R21 or (1-4C)alkyl, optionally substituted with OH, halogen, cyano or —S(1-4C)alkyl; R19 is H or (1-6C)alkyl, optionally substituted with OH or halogen; R20 is H, (1-6C)alkyl or (2-6C)alkenyl, both optionally substituted by halogen, O(1-6C)alkyl, (hetero)aryl, optionally substituted with (1-4C)alkyl or halogen; (3-6C)cycloalkyl; (1-6C)alkoxy; (1-6C)alkenyloxy; or (hetero)aryl, optionally substituted with (1-4C)alkyl); NH2, —NH(1-6C)alkyl or —NH(hetero)aryl and R21 is H or (1-6C)alkyl. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocorticoid receptor activity.