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111. 发明授权

US06441019B2 Cyclocarbamate and cyclic amide derivatives 失效
标题翻译：环氨基甲酸酯和环酰胺衍生物
公开(公告)号：US06441019B2
公开(公告)日：2002-08-27
申请号：US09906875
申请日：2001-07-17
申请人： 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： 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： A61K31535
CPC分类号： C07D498/04 , A61K31/5365
摘要： 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.
摘要翻译：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。

112. 发明授权

US06436929B1 Cyclothiocarbamate derivatives as progesterone receptor modulators 有权
标题翻译：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：US06436929B1
公开(公告)日：2002-08-20
申请号：US09552354
申请日：2000-04-19
申请人： Puwen Zhang , Andrew Fensome , Eugene A. Terefenko , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley , Jay E. Wrobel , Mark A. Collins
发明人： 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分类号： A61K31535
CPC分类号： A61K31/536 , A61K31/538 , C07D265/18 , C07D413/04
摘要： The present invention provides compounds which are agonists of the progesterone receptor and have the structures: wherein R1 and R2 are independent substituents 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 3 to 8 membered Spiro cyclic alkyl or alkenyl ring or a Spiro cyclic ring containing one to three heteroatoms selected from O, S and N; RA is selected from H, amino, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl groups; RB is H, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R3 is H, OH, NH2, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; RC is selected from H or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl groups; Q1 is S, NR7, or CR8R9; R5 is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring with 1, 2, or 3 ring heteroatoms selected from the group of O, S, SO, SO2 or NR6; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds for contraception and the treatment of progesterone-related maladies.
摘要翻译：本发明提供作为孕酮受体的激动剂并具有以下结构的化合物：其中R 1和R 2是选自H，任选取代的C 1至C 6烷基，烯基，炔基或炔基的独立取代基C 3至C 8环烷基，芳基，取代的芳基或杂环基，或CORA或NRBCORA; 或R 1和R 2稠合形成任选取代的3至8元螺环烷基或烯基环或含有一至三个选自O，S和N的杂原子的螺环; RA选自H，氨基或任选取代的C 1至C 3烷基，芳基，C 1至C 3烷氧基或C 1至C 3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; R 3是H，OH，NH 2，CORC或任选取代的C 1至C 6烷基，C 3至C 6烯基或炔基; RC选自H或任选取代的C 1至C 3烷基，芳基，C 1至C 3烷氧基或C 1至C 3氨基烷基; Q1是S，NR7或CR8R9; R5是任选的三取代的苯环或具有1,2或3个选自O，S，SO，SO 2或NR 6的环杂原子的任选取代的五元或六元杂环; 或其药学上可接受的盐，以及使用这些化合物用于避孕和治疗孕酮相关性疾病的方法。

113. 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。

114. 发明授权

US06417214B1 3,3-substituted indoline derivatives 失效
标题翻译： 3,3-取代的二氢吲哚衍生物
公开(公告)号：US06417214B1
公开(公告)日：2002-07-09
申请号：US09552352
申请日：2000-04-19
申请人： John W. Ullrich , Andrew Fensome , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： John W. Ullrich , Andrew Fensome , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K3142
CPC分类号： C07D209/08
摘要： This invention provides compounds of the formula 1: wherein: R1 and R2 are chosen independently from each other from H, OH; OAc; alkylaryl; alkylheteroaryl; 1-propynyl; 3-propynyl; and optionally substituted alkyl, O(alkyl); aryl; or heteroaryl groups; or R1 and R2 are joined to form a ring comprising —CH2(CH2)nCH2— where n=0-5; —CH2CH2CMe2CH2CH2—; —O(CH2)mCH2— where m=1-4; O(CH2)pO— where p=1-4; —CH2CH2OCH2CH2—; —CH2CH2N(H or alkyl)CH2CH2—; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl groups; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is selected from optionally substituted benzene ring; a five or six membered heterocyclic ring; a 4 or 7-substituted indole or a substituted benzothiophene; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of using the compounds as progesterone receptor antagonists.
摘要翻译：本发明提供式1化合物：其中：R 1和R 2彼此独立地选自H，OH; OAc; 烷基芳基烷基杂芳基 1-丙炔基; 3-丙炔基; 和任选取代的烷基，O（烷基）; 芳基; 或杂芳基; 或R 1和R 2连接形成包含-CH 2（CH 2）n CH 2 - 的环，其中n = 0-5; -CH2CH2CMe2CH2CH2-; -O（CH 2）m CH 2 - ，其中m = 1-4; O（CH 2）p O-，其中p = 1-4; -CH2CH2OCH2CH2-; -CH 2 CH 2 N（H或烷基）CH 2 CH 2 - ;或R 1和R 2一起包含与CMe2的双键; C（环烷基），O或C（环醚）; R 3是H，OH，NH 2，CORA或任选取代的烯基或炔基; RA = H或任选取代的烷基，烷氧基或氨基烷基; R 4 = H，，CN，NH 2或任选取代的烷基，烷氧基或氨基烷基; R 5选自任选取代的苯环; 五元或六元杂环; 4或7-取代的吲哚或取代的苯并噻吩; 或其药学上可接受的盐，以及使用该化合物作为孕酮受体拮抗剂的药物组合物和方法。

115. 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。

116. 发明授权

US06355648B1 Thio-oxindole derivatives 有权
标题翻译：硫氧吲哚衍生物
公开(公告)号：US06355648B1
公开(公告)日：2002-03-12
申请号：US09552033
申请日：2000-04-19
申请人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Lin Zhi , Todd K. Jones , Jay E. Wrobel , Christopher M. Tegley , James P. Edwards , Edward G. Melenski
发明人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Lin Zhi , Todd K. Jones , Jay E. Wrobel , Christopher M. Tegley , James P. Edwards , Edward G. Melenski
IPC分类号： A61K31505
CPC分类号： C07D209/40 , C07D209/08 , C07D209/30
摘要： This invention relates to compounds which are agonists of the progesterone receptor which have the general structures: wherein: R1 and R2 are H, alkyl, substituted alkyl; OH; O(alkyl); O(substituted alkyl); OAc; aryl; substituted aryl; heteroaryl; substituted heteroaryl; alkylaryl; alkylheteroaryl; 1-propynyl; or 3-propynyl; or R1 and R2 are joined to form an alkyl, alkenyl or heterocyclic ring; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, substituted alkynyl, or CORA; RA is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NH2, NO2, C1 to C6 alkyl, or substituted C1 to C6 alkyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; R5 is optionally substituted and selected from a benzene ring, a five or six membered heterocyclic ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2 or NR6; or an indol-4-yl, indol-7-yl or benzo-2-thiophene moiety; Q1 is S, NR7, CR8R9; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
摘要翻译：本发明涉及作为孕酮受体激动剂的化合物，其具有以下通式结构：其中：R 1和R 2为H，烷基，取代的烷基; 哦; O（烷基）; O（取代的烷基）; OAc; 芳基; 取代芳基; 杂芳基; 取代的杂芳基; 烷基芳基烷基杂芳基 1-丙炔基; 或3-丙炔基; 或R 1和R 2连接形成烷基，链烯基或杂环; 或R1和R2一起包含与CMe2的双键; C（环烷基），O或C（环醚）; R 3是H，OH，NH 2，C 1 -C 6烷基，取代的C 1 -C 6烷基，C 3至C 6烯基，炔基，取代的炔基或CORA; RA为H，C1至C3烷基，取代C1至C3烷基，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，NH 2，NO 2，C 1至C 6烷基或取代的C 1 -C 6烷基，C 1至C 6烷氧基，取代的C 1至C 6烷氧基，C 1至C 6氨基烷基或取代的C 1至C 6氨基烷基; R5任选被取代并选自苯环，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杂环; 或吲哚基-4-基，吲哚-7-基或苯并-2-噻吩部分; Q1是S，NR7，CR8R9; 或其药学上可接受的盐，以及使用这些化合物诱导避孕或治疗孕酮相关的癌和腺癌的方法。

117. 发明授权

US06339098B1 2,1-benzisothiazoline 2,2-dioxides 失效
标题翻译： 2,1-苯并异噻唑啉2,2-二氧化物
公开(公告)号：US06339098B1
公开(公告)日：2002-01-15
申请号：US09552630
申请日：2000-04-19
申请人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
发明人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , James P. Edwards , Todd K. Jones , Christopher M. Tegley , Lin Zhi
IPC分类号： A61K31428
CPC分类号： C07D275/06 , C07D413/04
摘要： This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, heteroarylalkyl, and alkynyl. R1 and R2 may be taken together to form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)PCH2—, O(CH2)qO—, —CH2CH2OCH2CH2—, —CH2CH2NR7CH2CH2—. R1 and R2 may be taken together to form a double bond, the double bond having two methyl groups bonded to the terminal end, having a cycloalkyl group bonded to the terminal end, having an oxygen bonded to the terminal end, or having a cycloether bonded to the terminal end; or a double bond. R3 is hydrogen, hydroxyl, NH2, alkyl, substituted alkyl, alkenyl, alkynyl, substituted or, CORA. R4 is hydrogen, halogen, —CN, —NH2, alkyl, substituted alkyl, alkoxy, alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is a trisubstituted phenyl ring having the structure, or is a five or six membered heteroaryl ring, containing 1, 2, or 3 heteroatoms selected from the group consisting of O, S, SO, SO2 and NR6, or pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了具有其中R1的结构的式1的孕酮受体拮抗剂，R 2各自独立地为氢，烷基，取代的烷基，羟基，烷氧基，取代的烷氧基，芳基，取代的芳基，杂芳基，取代的杂芳基，芳基烷基，杂芳基烷基，和炔基。 R 1和R 2可以一起形成环，并且一起含有-CH 2（CH 2）n CH 2 - ， - CH 2 CH 2 CH 2 CH 2 CH 2 - ， - O（CH 2）PCH 2 - ，O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - ， - CH 2 CH 2 NR 7 CH 2 CH 2 - 。 R1和R2可以一起形成双键，该双键具有与末端键合的两个甲基，具有与末端键合的环烷基，具有与末端结合的氧，或具有环醚键合到终端; 或双键。 R3是氢，羟基，NH2，烷基，取代的烷基，烯基，炔基，取代的或CORA。 R4是氢，卤素，-CN，-NH2，烷基，取代的烷基，烷氧基，烷氧基，氨基烷基或取代的氨基烷基; R5是具有结构的三取代的苯环，或是含有1,2或3个选自O，S，SO，SO 2和NR 6的杂原子的五或六元杂芳基环，或其药学上可接受的盐。

118. 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。

119. 发明授权

US06268497B1 Process for the preparation of C(5)-substituted 1,2-dihydro-5H-chromeno[3,4-f]quinolines 失效
标题翻译：制备C（5） - 取代的1,2-二氢-5H-色烯并[3,4-f]喹啉的方法
公开(公告)号：US06268497B1
公开(公告)日：2001-07-31
申请号：US09547568
申请日：2000-04-12
申请人： James P. Edwards , Todd K. Jones
发明人： James P. Edwards , Todd K. Jones
IPC分类号： C07D47100
CPC分类号： C07D491/04
摘要： A method for preparing C(5)-substituted 1,2-dihydro-5H-chromeno[3,4-ƒ]quinolines from a lactol precursor is provided. The method comprises converting the lactol to one of a select number of mixed acetal derivatives, and then treating the acetals with a Grignard reagent. The new process provides products in higher yield and greater purity. Novel intermediates of this method are also claimed.
摘要翻译：提供了从乳糖前体制备C（5） - 取代的1,2-二氢-5H-色烯并[3,4-f]喹啉的方法。该方法包括将乳糖转化为选定数量的混合缩醛衍生物之一，然后用格氏试剂处理该缩醛。新工艺提供了更高产量和更高纯度的产品。还要求保护该方法的新型中间体。

120. 发明授权

US5688810A Steroid receptor modulator compounds and methods 失效
标题翻译：类固醇受体调节剂化合物及方法
公开(公告)号：US5688810A
公开(公告)日：1997-11-18
申请号：US464541
申请日：1995-06-05
申请人： Todd K. Jones , Mark E. Goldman , Charlotte L.F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi
发明人： Todd K. Jones , Mark E. Goldman , Charlotte L.F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi
IPC分类号： C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , A61K31/47 , C07D215/12 , C07D215/18 , C07D215/36 , C07D215/38
CPC分类号： C07D401/04 , C07D215/06 , C07D221/18 , C07D311/80 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04
摘要： Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
摘要翻译：公开了用于类固醇受体的高亲和力，高选择性调节剂的非甾体化合物。还公开了掺入这种化合物的药物组合物，使用所公开的化合物的方法和用于治疗需要类固醇受体激动剂或拮抗剂治疗的患者的组合物，可用于制备化合物的中间体和用于制备类固醇受体调节剂化合物的方法。

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