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    1,2,3,4-tetrahydro-2-thioxo-quinolinyl and 1,2,3,4-tetrahydro-2-oxo-quinolinyl derivatives as progesterone receptor modulators
    23.
    发明授权
    1,2,3,4-tetrahydro-2-thioxo-quinolinyl and 1,2,3,4-tetrahydro-2-oxo-quinolinyl derivatives as progesterone receptor modulators 失效
    1,2,3,4-四氢-2-硫代 - 喹啉基和1,2,3,4-四氢-2-氧代喹啉基衍生物作为孕酮受体调节剂

    公开(公告)号：US06693103B2

    公开(公告)日：2004-02-17

    申请号：US10023063

    申请日：2001-12-17

    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: C07D215227

    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, alkynyl, cycloalkyl, 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，COR A或NR C COR 3， 或任选取代的烷基，烯基，炔基，环烷基，芳基或杂环部分;或R 1和R 2稠合形成：3至8元螺环烷基，烯基或杂环; R A是H或任选取代的烷基，芳基，烷氧基或氨基烷基; R B是H，C 1至C 3烷基或取代的C 1至C 3烷基; R 3是H，OH，NH 2，COR C或任选取代的烷基，烯基或炔基; R C是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; R 5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的杂原子的五或六元环; R 6是H或C 1至C 3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; R 7和R 8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。

    Cyclic regimens using quinazolinone and benzoxazine derivatives
    24.
    发明授权
    Cyclic regimens using quinazolinone and benzoxazine derivatives 失效
    使用喹唑啉酮和苯并恶嗪衍生物的循环方案

    公开(公告)号：US06498154B1

    公开(公告)日：2002-12-24

    申请号：US09552357

    申请日：2000-04-19

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

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

    IPC: A61K3156

    CPC classification number: A61K31/565 ,  A61K31/57 ,  A61K45/06 ,  A61K2300/00

    Abstract: This invention relates to cyclic combination therapies utilizing, in combination with progestins, estrogens, or both, compounds which are progesterone receptor antagonists of the general structure: wherein: R1 and R2 are H, CORA, or NRBCORA, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic; or R1 and R2 fuse 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 or alkyl; R3 is H, OH, NH2, CORC or alkyl, alkenyl, or alkynyl; RC is H, alkyl, aryl, alkoxy, or aminoalkyl; R4 is H, halogen, CN, NO2, alkyl, alkynyl, alkoxy, amino or aminoalkyl; R5 is benzene or 5- or 6-membered heterocyclic ring; R6 is H or alkyl; G1 is O, NR7, or CR7R8; G2 is CO 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. These methods may be used for contraception or treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.

    Abstract translation: 本发明涉及利用与孕激素，雌激素或两者作为一般结构的孕酮受体拮抗剂的化合物的环状组合疗法：其中：R1和R2是H，CORA或NRBCORA，烷基，烯基，炔基，环烷基 ，芳基或杂环基; 或R1和R2融合形成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或烷基; R3是H，OH，NH2，CORC或烷基，烯基或炔基; RC是H，烷基，芳基，烷氧基或氨基烷基; R4是H，卤素，CN，NO2，烷基，炔基，烷氧基，氨基或氨基烷基; R5是苯或5-或6-元杂环; R6是H或烷基; G1是O，NR7或CR7R8; G2为CO或CR7R8; 条件是当G1为O时，G2为CR7R8，G1和G2不能为CR7R8; R 7和R 8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。 这些方法可用于避孕或治疗和/或预防继发性闭经，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症; 多囊卵巢综合征，子宫内膜，卵巢，乳腺，结肠，前列腺的癌和腺癌，或副作用最小化或周期性月经出血。 本发明的额外用途包括刺激食物摄取。

    Cyclic regimens using cyclocarbamate and cyclic amide derivatives
    25.
    发明授权
    Cyclic regimens using cyclocarbamate and cyclic amide derivatives 失效
    使用环状氨基甲酸酯和环状酰胺衍生物的循环方案

    公开(公告)号：US06380178B1

    公开(公告)日：2002-04-30

    申请号：US09552545

    申请日：2000-04-19

    Applicant: Gary S. Grubb ,  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： Gary S. Grubb ,  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: A61K3156

    CPC classification number: A61K31/56 ,  A61K31/40 ,  A61K31/445 ,  A61K31/535 ,  A61K31/565 ,  A61K45/06 ,  A61K2300/00

    Abstract: This invention relates to cyclic combination therapies and regimens utilizing, in combination with progestins, substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: where 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. These methods of treatment may be used for contraception.

    Abstract translation: 本发明涉及利用与孕激素组合的取代二氢吲哚衍生物化合物的循环组合疗法和方案，所述二氢吲哚衍生化合物是具有以下通式结构的孕酮受体的拮抗剂：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。 这些治疗方法可用于避孕。

    Benzothiadiazolylphenylalkylamine derivatives and methods of their use
    28.
    发明授权
    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：US07601744B2

    公开(公告)日：2009-10-13

    申请号：US11528792

    申请日：2006-09-27

    Applicant: Casey Cameron McComas ,  Puwen Zhang ,  Eugene John Trybulski ,  An Thien Vu ,  Eugene Anthony Terefenko

    Inventor： Casey Cameron McComas ,  Puwen Zhang ,  Eugene John Trybulski ,  An Thien Vu ,  Eugene Anthony Terefenko

    IPC: A61K31/41 ,  C07D285/06

    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, fibromyalgia 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，疼痛等的那些病症，其中，所述疾病，性功能障碍，胃肠道和泌尿生殖系统疾病，慢性疲劳综合征，纤维肌痛综合征，神经系统疾病及其组合， 糖尿病性神经病变及其组合。

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