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1. 发明授权

US08242098B2 Methods of treating hormone-related conditions using thio-oxindole derivatives 失效
标题翻译：使用硫代羟吲哚衍生物治疗激素相关病症的方法
公开(公告)号：US08242098B2
公开(公告)日：2012-08-14
申请号：US12336588
申请日：2008-12-17
申请人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
发明人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
IPC分类号： A61K31/56
CPC分类号： A61K31/404 , A61K45/06
摘要： The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
摘要翻译：本发明提供了诱导避孕的方法，其包括将包含式I化合物或其互变异构体的组合物递送给女性，该方案涉及递送一种或多种选择性雌激素受体调节剂，其中式I是：并且其中 R1-R5和Q1如本文所述定义。提供了提供激素替代疗法和治疗癌症，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症和多囊卵巢综合征的方法，其包括递送式I化合物和选择性雌激素受体调节剂。

2. 发明授权

US07297688B2 Starter kit for low dose oral contraceptives 失效
标题翻译：低剂量口服避孕药入门套件
公开(公告)号：US07297688B2
公开(公告)日：2007-11-20
申请号：US09872250
申请日：2001-06-01
申请人： Gary S. Grubb
发明人： Gary S. Grubb
IPC分类号： A61K33/56
CPC分类号： A61K31/565 , A61K31/56 , A61K31/57 , A61K31/575 , A61K2300/00
摘要： The present invention provides a contraceptive kit which helps to overcome or ameliorate the problem of breakthrough bleeding and spotting associated with lowest dose (15-20 ug EE) estrogen contraceptives.
摘要翻译：本发明提供了一种避孕药具，其有助于克服或改善与最低剂量（15-20ug EE）雌激素避孕药相关的突破性出血和斑点问题。

3. 发明授权

US06444668B1 Combination regimens using progesterone receptor modulators 失效
标题翻译：使用孕酮受体调节剂的联合治疗方案
公开(公告)号：US06444668B1
公开(公告)日：2002-09-03
申请号：US09552350
申请日：2000-04-19
申请人： Gary S. Grubb , Puwen Zhang , Eugene A. Terefenko , Andrew Fensome , Jay E. Wrobel , Horace Fletcher, III , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Puwen Zhang , Eugene A. Terefenko , Andrew Fensome , Jay E. Wrobel , Horace Fletcher, III , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： A61K31535
CPC分类号： A61K31/535 , A61K31/56 , Y10S514/843 , A61K2300/00
摘要： 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.
摘要翻译：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

US06423699B1 Combination therapies using benzimidazolones 失效
标题翻译：联合治疗使用苯并咪唑酮
公开(公告)号：US06423699B1
公开(公告)日：2002-07-23
申请号：US09552355
申请日：2000-04-19
申请人： Gary S. Grubb , Puwen Zhang , Reinhold R. W. Bender , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Gary S. Grubb , Puwen Zhang , Reinhold R. W. Bender , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： A61K3156
CPC分类号： A61K45/06 , A61K31/415 , A61K31/535 , A61K31/54 , A61K31/56 , A61K31/57 , A61K2300/00
摘要： 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.
摘要翻译：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。

5. 发明授权

US06399593B1 Cyclic regimens using cyclic urea and cyclic amide derivatives 失效
标题翻译：使用环状脲和环状酰胺衍生物的循环方案
公开(公告)号：US06399593B1
公开(公告)日：2002-06-04
申请号：US09552037
申请日：2000-04-19
申请人： Gary S. Grubb , 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
发明人： Gary S. Grubb , 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分类号： A61K3156
CPC分类号： A61K45/06 , A61K31/565 , A61K31/57 , A61K31/535 , A61K2300/00
摘要： This invention concerns cyclic combination therapies using progestational agents and indoline derivatives which are progesterone receptor antagonists of the general structure: wherein: A, B and D are N or CH, though not all can be CH; R1 and R2 are H, CORA, NRBCORA, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, or aryl groups; or R1 and R2 form a spirocyclic ring; RA is H or optionally substituted alkyl aryl, alkoxy, or aminoalkyl; RB is H, alkyl alkyl; R3 is H, OH, NH2, alkyl, alkenyl, or CORC; RC is H, alkyl, aryl, alkoxy, or aminoalkyl; R4 is benzene or a 5 or 6 membered heteroaromatic ring; RF is H, alkyl, aryl, alkoxy, or aminoalkyl; RG is H or alkyl; R5 is H or alkyl; W is O or a chemical bond; or a pharmaceutically acceptable salt thereof. These methods may be used for contraception.
摘要翻译：本发明涉及使用孕激素和二氢吲哚衍生物的循环联合疗法，其为一般结构的孕酮受体拮抗剂：其中：A，B和D为N或CH，尽管不是全部可以是CH; R1和R2是H，CORA，NRBCORA或任选取代的烷基，烯基，炔基，环烷基或芳基; 或R 1和R 2形成螺环; RA为H或任选取代的烷基芳基，烷氧基或氨基烷基; RB是H，烷基烷基; R3是H，OH，NH2，烷基，烯基或CORC; RC是H，烷基，芳基，烷氧基或氨基烷基; R4是苯或5或6元杂芳环; RF是H，烷基，芳基，烷氧基或氨基烷基; RG为H或烷基; R5是H或烷基; W是O或化学键; 或其药学上可接受的盐。这些方法可用于避孕。

6. 发明授权

US06319912B1 Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides 失效
标题翻译：使用2,1-苯并异噻唑啉二氧化物的环状方案
公开(公告)号：US06319912B1
公开(公告)日：2001-11-20
申请号：US09552038
申请日：2000-04-19
申请人： Gary S. Grubb , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley , Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel
发明人： Gary S. Grubb , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley , Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel
IPC分类号： A61K3156
CPC分类号： A61K31/565 , A61K31/425 , A61K31/535 , A61K31/56 , A61K31/57 , A61K45/06 , A61K31/428 , A61K2300/00
摘要： This invention relates to cyclic combination therapies utilizing, in combination with a progestin, an estrogen, or both, progesterone receptor antagonists of the general structure: wherein the substituents are as defined herein, or pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及利用与孕激素，雌激素或两者一起使用的一般结构的孕酮受体拮抗剂的环状组合疗法：其中取代基如本文所定义，或其药学上可接受的盐。

7. 发明授权

US5521166A Antiprogestin cyclophasic hormonal regimen 失效
标题翻译：抗孕激素环状激素方案
公开(公告)号：US5521166A
公开(公告)日：1996-05-28
申请号：US359159
申请日：1994-12-19
申请人： Gary S. Grubb
发明人： Gary S. Grubb
IPC分类号： A61K31/565 , A61K31/567 , A61K31/57 , A61K31/56
CPC分类号： A61K31/565 , A61K31/567 , Y10S514/01 , Y10S514/863 , Y10S514/899
摘要： 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.
摘要翻译：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。

8. 发明申请

US20090099223A1 METHODS OF TREATING HORMONE-RELATED CONDITIONS USING THIO-OXINDOLE DERIVATIVES 失效
标题翻译：使用氧代衍生物处理与HORMONE相关的条件的方法
公开(公告)号：US20090099223A1
公开(公告)日：2009-04-16
申请号：US12336588
申请日：2008-12-17
申请人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
发明人： Andrew Fensome , Gary S. Grubb , Diane Deborah Harrison , Richard Craig Winneker
IPC分类号： A61K31/438 , A61K31/403
CPC分类号： A61K31/404 , A61K45/06
摘要： The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
摘要翻译：本发明提供了诱导避孕的方法，其包括将包含式I化合物或其互变异构体的组合物递送给女性，该方案涉及递送一种或多种选择性雌激素受体调节剂，其中式I是：并且其中 R1-R5和Q1如本文所述定义。提供了提供激素替代疗法和治疗癌症，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症和多囊卵巢综合征的方法，其包括递送式I化合物和选择性雌激素受体调节剂。

9. 发明授权

US06498154B1 Cyclic regimens using quinazolinone and benzoxazine derivatives 失效
标题翻译：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
申请人： Gary S. Grubb , Lin Zhi , Todd K. Jones , Puwen Zhang , James P. Edwards , Andrew Fensome , Eugene A. Terefenko , Jay E. Wrobel , Christopher M. Tegley
发明人： 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分类号： A61K3156
CPC分类号： A61K31/565 , A61K31/57 , A61K45/06 , A61K2300/00
摘要： 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.
摘要翻译：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。

10. 发明授权

US06380178B1 Cyclic regimens using cyclocarbamate and cyclic amide derivatives 失效
标题翻译：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
申请人： 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
发明人： 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分类号： A61K3156
CPC分类号： A61K31/56 , A61K31/40 , A61K31/445 , A61K31/535 , A61K31/565 , A61K45/06 , A61K2300/00
摘要： 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.
摘要翻译：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。

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