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    Benzimidazolones and analogues
    41.
    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
    42.
    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。

    Substituted propylamine derivatives and methods of their use
    43.
    发明授权
    Substituted propylamine derivatives and methods of their use 失效
    取代的丙胺衍生物及其使用方法

    公开(公告)号：US07687529B2

    公开(公告)日：2010-03-30

    申请号：US11529450

    申请日：2006-09-27

    Applicant: Casey Cameron McComas ,  Puwen Zhang ,  Eugene Anthony Terefenko ,  An Thien Vu ,  Stephen Todd Cohn

    Inventor： Casey Cameron McComas ,  Puwen Zhang ,  Eugene Anthony Terefenko ,  An Thien Vu ,  Stephen Todd Cohn

    IPC: A61K31/4184 ,  C07D235/04 ,  C07D209/04

    CPC classification number: C07D209/96 ,  C07D209/08 ,  C07D209/34 ,  C07D235/26 ,  C07D235/30 ,  C07D277/68

    Abstract: The present invention is directed to substituted propylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

    Abstract translation: 本发明涉及式I的取代丙胺衍生物：或其药学上可接受的盐，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，其中尤其包括血管舒缩症状（VMS） 特别是那些选自重症抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛等症状的那些疾病 ，糖尿病性神经病，及其组合。

    6-amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators
    46.
    发明授权
    6-amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators 失效
    6-氨基-1,4-二氢 - 苯并[d] [1,3]恶嗪-2-酮和可用作孕酮受体调节剂的类似物

    公开(公告)号：US07247625B2

    公开(公告)日：2007-07-24

    申请号：US10946476

    申请日：2004-09-21

    Applicant: Puwen Zhang ,  Jeffrey Kern

    Inventor： Puwen Zhang ,  Jeffrey Kern

    IPC: C07D265/18 ,  A61K31/537 ,  A61K31/536

    CPC classification number: A61K31/538 ,  A61K31/517 ,  C07D265/18

    Abstract: Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions.

    Abstract translation: 提供具有式I结构的化合物。 在式I中，R 1是H，OH，取代或未取代的C 1至C 3烷基，C 1或N 2 C 3至C 3全氟烷基或COR 6; R 6是H，取代或未取代的C 1至C 4烷基，芳基，取代或未取代的C 1〜 至C 4烷氧基，取代或未取代的C 1至C 3氨基烷基; R 2和R 3均为H，取代或未取代的C 1至C 6烷基，C 1至C 6烷基， C 6至C 6全氟烷基，取代或未取代的C 2至C 6链烯基，取代或未取代的C 2， 取代或未取代的C 3至C 6环烷基，取代或未取代的芳基或取代或未取代的杂环基; 或R 2和R 3 3稠合形成螺环; R 4是NHR 7，OR 7，NHSO 2 R 7，或 OSO 2 R 7; Q是O，S，NR 8或CR 9 R 10; 或其药学上可接受的盐，酯或前药。 这些化合物可用作孕酮受体调节剂和用于治疗孕酮受体相关病症。

    5-Aryl-indan-1-ol and analogs useful as progesterone receptor modulators
    49.
    发明申请
    5-Aryl-indan-1-ol and analogs useful as progesterone receptor modulators 审中-公开
    5-芳基 - 茚满-1-醇和可用作孕酮受体调节剂的类似物

    公开(公告)号：US20070066628A1

    公开(公告)日：2007-03-22

    申请号：US11522881

    申请日：2006-09-18

    Applicant: Puwen Zhang ,  Jeffrey Kern ,  Eugene Terefenko ,  Eugene Trybulski

    Inventor： Puwen Zhang ,  Jeffrey Kern ,  Eugene Terefenko ,  Eugene Trybulski

    IPC: A61K31/44 ,  C07D213/63

    CPC classification number: C07D207/34 ,  C07C255/53 ,  C07D409/10

    Abstract: Compounds of formula I are provided, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R3-R5, R10, and R11 are defined herein.

    Abstract translation: 提供式I化合物，其中R 1〜R 9和n如本文所定义，以及含有这些化合物的药物组合物和试剂盒。 还提供了使用式I或式II化合物诱导避孕，提供激素替代疗法，治疗周期相关症状或治疗或预防良性或恶性肿瘤疾病的方法，其中R 3〜 本文定义的是5，R 10和R 11。

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