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    Cyanopyrroles
    41.
    发明授权
    Cyanopyrroles 有权
    青色

    公开(公告)号：US06407101B1

    公开(公告)日：2002-06-18

    申请号：US09552544

    申请日：2000-04-19

    Applicant: Mark A. Collins ,  Valerie A. Mackner ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

    Inventor： Mark A. Collins ,  Valerie A. Mackner ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

    IPC: C07D41310

    CPC classification number: C07D403/04 ,  A61K31/405 ,  A61K31/5415 ,  C07D413/04

    Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alky, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, allyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alko, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof

    Abstract translation: 本发明提供具有其中T为O，S或不存在的结构的式1的孕酮受体拮抗剂; R 1和R 2各自独立地为氢，烷基，取代的烷基; 或R 1和R 2一起形成环，并且一起含有-CH 2（CH 2）n CH 2 - ， - CH 2 CH 2 CH 2 CH 2 CH 2 - ， - O（CH 2）p CH 2 - ， - O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - 或-CH 2 CH 2 NR 7 CH 2 CH 2 - n = 1-5; p = 1-4; q = 1-4; R 3是氢，OH，NH 2，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基或CORA; RA是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的 R5是氢，烯丙基或取代的烷基; R6是氢，烷基，取代的烷基或CORB; R是氢，烷基，取代的烷基，或烷氧基，取代的烷氧基， RB是氢，烷基，取代的烷基，烷基，取代的烷氧基，氨基烷基或取代的氨基烷基; R7是氢或烷基; 或其药学上可接受的盐

    Benzimidazolones and analogues
    42.
    发明授权
    Benzimidazolones and analogues 失效
    苯并咪唑酮和类似物

    公开(公告)号：US06380235B1

    公开(公告)日：2002-04-30

    申请号：US09552546

    申请日：2000-04-19

    Applicant: Puwen Zhang ,  Reinhold H. W. Bender ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

    Inventor： Puwen Zhang ,  Reinhold H. W. Bender ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

    IPC: A61K31415

    CPC classification number: C07D263/58 ,  C07C215/76 ,  C07C229/18 ,  C07D235/26 ,  C07D235/28 ,  C07D241/44 ,  C07D277/68 ,  C07D279/16 ,  C07D409/04 ,  C07D487/04

    Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt thereof. The invention also includes methods of contraception and methods of treating or preventing maladies associated with the progesterone receptor.

    Abstract translation: 本发明提供可用作孕酮受体激动剂和拮抗剂并具有以下通式的化合物和药物制剂：其中：A为O，S或NR4; B为A和C = Q之间的键，或部分CR5R6; R4， R5，R5独立地选自H或任选取代的C1至C6烷基，C2至C6烯基，C2至C6炔基，C3至C8环烷基，取代C3至C8环烷基，芳基或杂环基，或通过将R4 和R5至5至7元环; R1选自H，OH，NH2，C1至C6烷基，取代C1至C6烷基，C3至C6烯基，取代C1至C6烯基，炔基，取代的炔基，-COH或任选取代的-CO（C 1至C 3烷基 ），-CO（芳基），-CO（C 1〜C 3烷氧基）或-CO（C 1〜C 3氨基烷基） R 2选自H，卤素，CN，NO 2或任选取代的C 1至C 6烷基，C 1至C 6烷氧基或C 1至C 6氨基烷基; R3选自三取代苯环; 或含有1或2个取代基的5或6元杂芳环; Q是O，S，NR8或CR9R10; 或其药学上可接受的盐。 本发明还包括避孕方法和治疗或预防与孕酮受体相关的疾病的方法。

    Quinazolinone and benzoxazine derivatives as progesterone receptor modulators
    43.
    发明授权
    Quinazolinone and benzoxazine derivatives as progesterone receptor modulators 失效
    喹唑啉酮和苯并恶嗪衍生物作为孕酮受体调节剂

    公开(公告)号：US06358948B1

    公开(公告)日：2002-03-19

    申请号：US09552629

    申请日：2000-04-19

    Applicant: Puwen Zhang ,  Andrew Fensome ,  Eugene A. Terefenko ,  Jay E. Wrobel ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    Inventor： Puwen Zhang ,  Andrew Fensome ,  Eugene A. Terefenko ,  Jay E. Wrobel ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    IPC: C07D26516

    CPC classification number: C07D215/227 ,  A61K31/4704 ,  A61K31/517 ,  A61K31/536 ,  C07D215/38 ,  C07D239/80 ,  C07D265/16 ,  C07D413/04

    Abstract: This invention provides compounds which are agonists and antagonists of the progesterone receptor having the general structure: wherein: R1 and R2 are independently selected from H, CORA, or NRBCORA, or optionally substituted alkyl, alkenyl, alknyl, cycloalklyl, aryl, or heterocyclic moieties; or R1 and R2 are fused to form: 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic rings; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl groups; RB is H, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R3 is H, OH, NH2, CORC or optionally substituted alkyl, alkenyl, or alkynyl; RC is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted alkyl, alkynyl, alkoxy, amino or aminoalkyl; R5 is an optionally substituted benzene or five or six membered ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2 or NR6; R6 is H or C1 to C3 alkyl; G1 is O, NR7, or CR7R8; G2 is CO, CS, or CR7R8; provided that when G1 is O, G2 is CR7R8, and G1 and G2 cannot both be CR7R8; R7 and R8 are H or an optionally substituted alkyl, aryl, or heterocyclic moiety; or pharmaceutically acceptable salt thereof, and methods using these compounds in mammals as agonists or antagonists of the progesterone receptor.

    Abstract translation: 本发明提供作为孕酮受体的激动剂和拮抗剂的化合物，其具有以下通式结构：其中：R 1和R 2独立地选自H，CORA或NRBCORA，或任选取代的烷基，烯基，炔基，环烯基，芳基或杂环部分 ;或R1和R2稠合形成：3至8元螺环烷基，烯基或杂环; RA为H或任选取代的烷基，芳基，烷氧基或氨基烷基; RB是H，C 1至C 3烷基或取代的C 1至C 3烷基; R3是H，OH，NH2，CORC或任选取代的烷基，烯基或炔基; RC为H或任选取代的烷基，芳基，烷氧基或氨基烷基; R 4是H，卤素，CN，NO 2或任选取代的烷基，炔基，烷氧基，氨基或氨基烷基; R5是任选取代的苯或具有1,2或3个选自O，S，SO，SO 2或NR 6的杂原子的五元或六元环; R6是H或C1-C3烷基; G1是O，NR7或CR7R8; G2是CO，CS或CR7R8; 条件是当G1为O时，G2为CR7R8，G1和G2不能为CR7R8; R7和R8是H或任选取代的烷基，芳基或杂环部分;或其药学上可接受的盐，以及在哺乳动物中使用这些化合物作为孕酮受体的激动剂或拮抗剂的方法。

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