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    • 3. 发明授权
    • Combination regimens using progesterone receptor modulators
    • 使用孕酮受体调节剂的联合治疗方案
    • US06444668B1
    • 2002-09-03
    • US09552350
    • 2000-04-19
    • Gary S. GrubbPuwen ZhangEugene A. TerefenkoAndrew FensomeJay E. WrobelHorace Fletcher, IIIJames P. EdwardsTodd K. JonesChristopher M. TegleyLin Zhi
    • Gary S. GrubbPuwen ZhangEugene A. TerefenkoAndrew FensomeJay E. WrobelHorace Fletcher, IIIJames P. EdwardsTodd K. JonesChristopher M. TegleyLin Zhi
    • A61K31535
    • A61K31/535A61K31/56Y10S514/843A61K2300/00
    • This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 allyl C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alknyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, CORF, or NRGCORF; or pharmaceutically acceptable salt thereof. These methods of treatment may be used for contraception or for the 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 inmization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.
    • 本发明涉及使用具有以下通式结构的孕酮受体的拮抗剂的取代的二氢吲哚衍生物化合物的环状组合疗法和方案:其中R1和R2可以是单取代基或稠合形成螺环或异 - 螺环; R 3是H,OH,NH 2,C 1至C 6烷基,取代的C 1 -C 6烯丙基C 3至C 6烯基,取代的C 1至C 6烯基,炔基或取代的烷基,CORC; RC为H,C1至C3烷基,取代C1至C3烷基,芳基,取代芳基,C1至C3烷氧基,取代C1至C3烷氧基,C1至C3氨基烷基或取代C1至C3氨基烷基; R 4是H,卤素,CN,NO 2,C 1至C 6烷基,取代的C 1至C 6烷基炔基或取代的炔基,C 1至C 6烷氧基,取代的C 1至C 6烷氧基,氨基,C 1至C 6氨基烷基或取代的C 1至C 6氨基烷基 ; 并且R 5选自具有1,2或3个杂原子的五元或六元环的三取代苯环,所述杂原子包括O,S,SO,SO 2或NR 6,并且包含一个或两个独立的取代基,包括H, 卤素,CN,NO 2,氨基和C 1至C 3烷基,C 1至C 3烷氧基,C 1至C 3氨基烷基,CORF或NRGCORF; 或其药学上可接受的盐。 这些治疗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,子宫内膜癌,卵巢癌,乳腺癌,结肠癌,前列腺癌,腺癌,副作用或周期性月经出血。 本发明的额外用途包括刺激食物摄取。
    • 4. 发明授权
    • Combination therapies using benzimidazolones
    • 联合治疗使用苯并咪唑酮
    • US06423699B1
    • 2002-07-23
    • US09552355
    • 2000-04-19
    • Gary S. GrubbPuwen ZhangReinhold R. W. BenderJay E. WrobelJames P. EdwardsTodd K. JonesChristopher M. TegleyLin Zhi
    • Gary S. GrubbPuwen ZhangReinhold R. W. BenderJay E. WrobelJames P. EdwardsTodd K. JonesChristopher M. TegleyLin Zhi
    • A61K3156
    • A61K45/06A61K31/415A61K31/535A61K31/54A61K31/56A61K31/57A61K2300/00
    • This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R6 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, 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 alkynyl, —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 heteroaromnatic ring containing 1 or 2 substituents; or a pharmaceutically acceptable salt thereof, in combination with a progestational agent, an estrogen, or both or for the 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. These combinations may also be used to in methods of contraception, to stimulate food intake or for minimization of side effects or cyclic menstrual bleeding.
    • 本发明涉及使用具有以下通式结构的孕酮受体的拮抗剂的取代的二氢吲哚衍生物化合物的循环组合疗法和方案:其中:A是O,S或NR4; B是A和C = Q之间的键,或 CR5R6部分; R4,R5,R6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,或由 将R4和R5与5至7元环融合; 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) R2选自H,卤素,CN,NO2或任选取代的C1至C6烷基C1至C6烷氧基或C1至C6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-元杂芳族环; 或其药学上可接受的盐与促孕剂,雌激素或两者组合,或用于治疗和/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,前列腺癌和腺癌。 这些组合也可用于避孕方法,刺激食物摄取或最小化副作用或周期性月经出血。
    • 7. 发明授权
    • Antiprogestin cyclophasic hormonal regimen
    • 抗孕激素环状激素方案
    • US5521166A
    • 1996-05-28
    • US359159
    • 1994-12-19
    • Gary S. Grubb
    • Gary S. Grubb
    • A61K31/565A61K31/567A61K31/57A61K31/56
    • A61K31/565A61K31/567Y10S514/01Y10S514/863Y10S514/899
    • The present invention is directed to cyclophasic hormonal regimens which comprise antiprogestin and progestin for human contraception whereby progestin is administered in the alternating presence and absence of an antiprogestin in effective amounts to upregulate steroid receptor levels or is alternatively dosed with effective amounts of antiprogestin to upregulate steroid receptor levels. The present invention also provides an estrogen containing cyclophasic hormonal regimen for climacteric or menopausal hormone replacement therapy comprising the administration of an effective hormone replacement amount of estrogen in alternating doses with a combined amount of estrogen and an effective amount of antiprogestin to inhibit proliferation of endometrial tissue caused by the administration of the estrogen.
    • 本发明涉及包含抗孕激素和孕激素用于人体避孕的环状激素方案,其中孕激素在交替存在和不存在抗孕激素时有效量地上调类固醇受体水平,或者替代地将有效量的抗孕激素施用于上调类固醇 受体水平。 本发明还提供了一种用于更年期或绝经期激素替代疗法的含雌激素的环状激素方案,其包括以合剂量的雌激素和有效量的抗孕激素施用交替剂量的有效激素替代量的雌激素以抑制子宫内膜组织增殖 由施用雌激素引起。
    • 9. 发明授权
    • Cyclic regimens using quinazolinone and benzoxazine derivatives
    • 使用喹唑啉酮和苯并恶嗪衍生物的循环方案
    • US06498154B1
    • 2002-12-24
    • US09552357
    • 2000-04-19
    • Gary S. GrubbLin ZhiTodd K. JonesPuwen ZhangJames P. EdwardsAndrew FensomeEugene A. TerefenkoJay E. WrobelChristopher M. Tegley
    • Gary S. GrubbLin ZhiTodd K. JonesPuwen ZhangJames P. EdwardsAndrew FensomeEugene A. TerefenkoJay E. WrobelChristopher M. Tegley
    • A61K3156
    • A61K31/565A61K31/57A61K45/06A61K2300/00
    • 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.
    • 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。