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    Cyclic urea and cyclic amide derivatives
    12.
    发明授权
    Cyclic urea and cyclic amide derivatives 失效
    环状脲和环状酰胺衍生物

    公开(公告)号：US06369056B1

    公开(公告)日：2002-04-09

    申请号：US09552356

    申请日：2000-04-19

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

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

    IPC: A61K31535

    CPC classification number: C07D498/04

    Abstract: This invention provides compounds of the formula: wherein: A, B and D are N or CH, with the proviso that A, B and D can not all be CH; R1 and R2 are independent substituents selected from H, CORA, NRBCORA, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or groups; or R1 and R2 are fused to form an optionally substituted 3 to 8 membered spirocyclic or heterocyclic ring; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RB is H, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R3 is H, OH, NH2, or optionally substituted alkyl, or alkenyl, or CORC; RC is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R4 is a substituted benzene ring or a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR5; RF is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RG is H, alkyl, or substituted alkyl; R5 is H or alkyl; Q is O, S, NR6, or CR7R8; R6 is CN, SO2CF3, or optionally substituted alkyl, cycloalkyl, aryl, or heterocyclic ring; R7 and R8 are H, NO2, CN CO2R9, or optionally substituted alkyl, cycloalkyl, aryl, or heterocyclic; R9 is C1 to C3 alkyl; or CR7R8 form a six membered ring of the structure below: W is O or a chemical bond; or a pharmaceutically acceptable salt thereof, as well as their use and pharmaceutical compositions as agonists and antagonists of the progesterone receptor.

    Abstract translation: 本发明提供下式的化合物：其中：A，B和D为N或CH，条件是A，B和D不能全部为CH; R1和R2是选自H，CORA，NRBCORA或任选取代的烷基，烯基，炔基，环烷基，芳基或基团的独立取代基; 或R 1和R 2稠合形成任选取代的3至8元螺环或杂环; 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或任选取代的烷基或烯基或CORC; RC为H或任选取代的烷基，芳基，烷氧基或氨基烷基; R4是取代的苯环或具有1,2或3个杂原子的五或六元环，所述杂原子包括O，S，SO，SO 2或NR 5; RF是H或任选取代的烷基，芳基，烷氧基或氨基烷基; RG是H，烷基或取代的烷基; R5是H或烷基; Q是O，S，NR6或CR7R8; R6是CN，SO2CF3或任选取代的烷基，环烷基，芳基或杂环; R 7和R 8是H，NO 2，CN CO 2 R 9或任选取代的烷基，环烷基，芳基或杂环; R9为C1至C3烷基; 或CR7R8形成以下结构的六元环：W为O或化学键; 或其药学上可接受的盐，以及它们的用途和药物组合物作为孕激素受体的激动剂和拮抗剂。

    Cyclocarbamate and cyclic amide derivatives
    13.
    发明授权
    Cyclocarbamate and cyclic amide derivatives 失效
    环氨基甲酸酯和环酰胺衍生物

    公开(公告)号：US06306851B1

    公开(公告)日：2001-10-23

    申请号：US09552036

    申请日：2000-04-19

    Applicant: Arthur A. Santilli ,  Andrew Q. Viet ,  Puwen Zhang ,  Andrew Fensome ,  Jay E. Wrobel ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    Inventor： Arthur A. Santilli ,  Andrew Q. Viet ,  Puwen Zhang ,  Andrew Fensome ,  Jay E. Wrobel ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    IPC: C07D49804

    CPC classification number: C07D498/04 ,  A61K31/5365

    Abstract: This invention provides compounds of the formula: wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, CORA, or NRBCORA; or R1 and R2 are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof. The compounds of this invention are useful as agonists and antagonists of the progesterone receptor and in methods of inducing contraception and in the treatment or prevention of benign or malignant neoplastic diseases.

    Abstract translation: 本发明提供下式的化合物：其中A和B是选自S，CH或N的独立取代基; 条件是当A为S时，B为CH或N; 当B为S时，A为CH或N; A和B不能同时为CH; 并且当A和B均等于N时，一个N可以任选地被C 1至C 6烷基取代; R1和R2是选自H，C1至C6烷基，取代C1至C6烷基，C2至C6烯基，取代C2至C6烯基，C2至C6炔基，取代C2至C6炔基，C3至C8环烷基的独立取代基 取代的C 3至C 8环烷基，芳基，取代的芳基，杂环，取代的杂环，CORA或NRBCORA; 或R 1和R 2稠合形成任选取代的3至8元螺环烷基，烯基或杂环，所述杂环含有一至三个选自O，S和N的杂原子; 或其药学上有用的盐。 本发明的化合物可用作孕激素受体的激动剂和拮抗剂以及诱导避孕和治疗或预防良性或恶性肿瘤疾病的方法。

    6-Amino-1,4-dihydro-benzo[d][1,3]oxazin-2-ones and analogs useful as progesterone receptor modulators
    17.
    发明申请
    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：US20070225281A1

    公开(公告)日：2007-09-27

    申请号：US11804831

    申请日：2007-05-21

    Applicant: Puwen Zhang ,  Jeffrey Kern

    Inventor： Puwen Zhang ,  Jeffrey Kern

    IPC: A61K31/535 ,  C07D265/18

    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。

    Benzothiadiazolylphenylalkylamine derivatives and methods of their use
    18.
    发明申请
    Benzothiadiazolylphenylalkylamine derivatives and methods of their use 失效
    苯并噻二唑基苯基烷基胺衍生物及其使用方法

    公开(公告)号：US20070072918A1

    公开(公告)日：2007-03-29

    申请号：US11528792

    申请日：2006-09-27

    Applicant: Casey McComas ,  Puwen Zhang ,  Eugene Trybulski ,  An Vu ,  Eugene Terefenko

    Inventor： Casey McComas ,  Puwen Zhang ,  Eugene Trybulski ,  An Vu ,  Eugene Terefenko

    IPC: C07D275/04 ,  C07D271/12 ,  A61K31/433 ,  A61K31/425

    CPC classification number: C07D285/14

    Abstract: The present invention is directed to benzothiadiazolylphenylalkylamine 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的苯并噻二唑基苯基烷基胺衍生物：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，所述方法尤其包括血管舒缩症状（VMS） 特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛等的那些情况，特别是选自以下的那些病症：血管紧张素转换酶，抑制性功能障碍，性功能障碍，胃肠道和泌尿生殖系统疾病，慢性疲劳综合征，纤维瘤病综合征，神经系统疾病及其组合， 糖尿病性神经病变及其组合。

    Cyclothiocarbamate derivatives as progesterone receptor modulators
    19.
    发明授权
    Cyclothiocarbamate derivatives as progesterone receptor modulators 失效
    环硫代氨基甲酸酯衍生物作为孕酮受体调节剂

    公开(公告)号：US07081457B2

    公开(公告)日：2006-07-25

    申请号：US10140034

    申请日：2002-05-06

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

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

    IPC: A61K31/535 ,  C07D295/00 ,  C07D265/12

    CPC classification number: A61K31/536 ,  A61K31/538 ,  C07D265/18 ,  C07D413/04

    Abstract: Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1 and R2 are selected from the group of H, optionally substituted C1 to C6 alkyl, alkenyl, alkynyl, or alkynyl groups C3 to C8 cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or CORA or NRBCORA; or R1 and R2 are fused to form an optionally substituted ring structure as defined herein; RA and RB are as defined herein; R3 is H, OH, NH2, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; RC is as defined herein; Q1 is S, NR7, or CR8R9; R5 is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring.

    Abstract translation: 提供使用孕酮受体激动剂用于避孕的化合物和单独或与雌​​激素受体激动剂或孕酮受体拮抗剂联合治疗孕激素相关性疾病的方法。 这些化合物具有以下结构：其中R 1和R 2选自H，任选取代的C 1至C 1 - C 6烷基，链烯基，炔基或炔基C 3至C 8环烷基，芳基，取代的芳基或杂环基，或COR A 或或 B 或R 1和R 2 2稠合形成如本文所定义的任选取代的环结构; R＆lt; A＆gt;和＆lt; B＆gt; B＆gt;如本文所定义; R 3是H，OH，NH 2，COR C或任选取代的C 1至C

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