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61. 发明申请

US20070129539A1 THROMBOPOIETIN ACTIVITY MODULATING COMPOUNDS AND METHODS 有权
标题翻译：血小板活化调节化合物和方法
公开(公告)号：US20070129539A1
公开(公告)日：2007-06-07
申请号：US11562327
申请日：2006-11-21
申请人： Lin Zhi , E. Kallel , Dean Phillips
发明人： Lin Zhi , E. Kallel , Dean Phillips
IPC分类号： C07D231/38
CPC分类号： C07D231/38 , C07D231/46 , C07D403/12
摘要： Disclosed herein are novel diazenyl pyrazole compounds and related compounds. Also disclosed herein are methods of using these compounds for the treatment of diseases and conditions associated with modulating a thrombopoietin activity.
摘要翻译：本文公开的是新的二唑基吡唑化合物和相关化合物。本文还公开了使用这些化合物来治疗与调节血小板生成素活性相关的疾病和病症的方法。

62. 发明申请

US20070072849A1 Tricyclic quinolinone and tricyclic quinoline androgen receptor modulator compounds and methods 审中-公开
标题翻译：三环喹啉酮和三环喹啉雄激素受体调节剂的化合物及方法
公开(公告)号：US20070072849A1
公开(公告)日：2007-03-29
申请号：US11601251
申请日：2006-11-17
申请人： Robert Higuchi , Lin Zhi , Donald Karanewsky , Anthony Thompson , Thomas Caferro , Neelakandha Mani , Jyun-Hung Chen , Marquis Cummings , James Edwards , Mark Adams , Charlotte Deckhut
发明人： Robert Higuchi , Lin Zhi , Donald Karanewsky , Anthony Thompson , Thomas Caferro , Neelakandha Mani , Jyun-Hung Chen , Marquis Cummings , James Edwards , Mark Adams , Charlotte Deckhut
IPC分类号： A61K31/542 , A61K31/5383 , A61K31/498 , C07D498/02 , C07D487/02
CPC分类号： C07D498/04 , C07D498/14 , Y02P20/582
摘要： Non-steroidal tricyclic quinolinone and tricyclic quinoline compounds and compositions that are agonists, partial agonists and/or antagonists for androgen receptors (AR), their preparation and their uses are described.
摘要翻译：描述了非甾体三环喹啉酮和三环喹啉化合物以及作为雄激素受体（AR）的激动剂，部分激动剂和/或拮抗剂及其用途的组合物及其用途。

63. 发明申请

US20070066650A1 6-Cycloamino-2-quinolinone derivatives as androgen receptor modulator compounds 有权
标题翻译： 6-环氨基-2-喹啉酮衍生物作为雄激素受体调节剂化合物
公开(公告)号：US20070066650A1
公开(公告)日：2007-03-22
申请号：US10566569
申请日：2004-08-23
申请人： Lin Zhi , Esther Martinborough , Yixing Shen , Thomas Lau , Min Wu , Yun Long
发明人： Lin Zhi , Esther Martinborough , Yixing Shen , Thomas Lau , Min Wu , Yun Long
IPC分类号： A61K31/4709 , C07D401/02
CPC分类号： C07D401/04
摘要： The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR. Also provided are methods of making such compounds and pharmaceutical compositions.
摘要翻译：本发明涉及用于调节由AR介导的过程的化合物，药物组合物和方法。还提供了制备这些化合物和药物组合物的方法。

64. 发明授权

US07084151B2 5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-5H-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds 有权
标题翻译：作为选择性孕酮受体调节剂化合物的5-（1'，1'-环烷基/烯基）亚甲基1,2-二氢-5H-色烯[3,4-f]
公开(公告)号：US07084151B2
公开(公告)日：2006-08-01
申请号：US10684227
申请日：2003-10-10
申请人： Lin Zhi , Cornelis Arjan Van Oeveren
发明人： Lin Zhi , Cornelis Arjan Van Oeveren
IPC分类号： A61K31/4741 , C07D491/02
CPC分类号： C07D491/04 , G01N33/743
摘要： The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such compounds and pharmaceutical compositions.
摘要翻译：本发明涉及用于调节由孕酮受体介导的过程的化合物，药物组合物和方法。还提供了制备这些化合物和药物组合物的方法。

65. 发明申请

US20060128740A1 Tricyclic androgen receptor modulator compounds and methods 有权
公开(公告)号：US20060128740A1
公开(公告)日：2006-06-15
申请号：US11344690
申请日：2006-01-31
申请人： Lin Zhi , Cornelis Van Oeveren , Jyun-Hung Chen , Robert Higuchi
发明人： Lin Zhi , Cornelis Van Oeveren , Jyun-Hung Chen , Robert Higuchi
IPC分类号： A61K31/4743 , A61K31/4741 , A61K31/382 , A61K31/366 , C07D495/02 , C07D493/02 , C07D491/02
CPC分类号： C07D471/04 , C07D491/04 , C07D493/04
摘要： This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.

66. 发明授权

US07026484B2 Tricyclic androgen receptor modulator compounds and methods 有权
公开(公告)号：US07026484B2
公开(公告)日：2006-04-11
申请号：US10080926
申请日：2002-02-22
申请人： Lin Zhi , Cornelis Arjan Van Oeveren , Jyun-Hung Chen , Robert I. Higuchi
发明人： Lin Zhi , Cornelis Arjan Van Oeveren , Jyun-Hung Chen , Robert I. Higuchi
IPC分类号： C07D455/04 , C07D221/18 , C07D471/00 , A61K31/44
CPC分类号： C07D471/04 , C07D491/04 , C07D493/04
摘要： This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.

67. 发明授权

US06794373B2 Contraceptive methods using benzimidazolones 失效
标题翻译：使用苯并咪唑酮的避孕方法
公开(公告)号：US06794373B2
公开(公告)日：2004-09-21
申请号：US10091222
申请日：2002-03-01
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 indoline compounds which are antagonists of the progesterone receptor and having the general structure: A is O, S, or NR4; B is a bond or CR5R6; R4, to R6 are H, C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, aryl, or heterocyclic, or R4 and R5 are fused to form a ring; R1 is H, OH, NH2, C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, or CORA; RA is as defined; R2 is H, halogen, CN, NO2, C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl; R3 is a substituted benzene ring, or heteroaromatic ring, in combination with a progestational agent and/or an estrogen to treat or prevent secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas and adenocarcinomas, and contraception, among others.
摘要翻译：本发明涉及使用作为孕酮受体的拮抗剂并具有以下一般结构的二氢吲哚化合物的环组合疗法和方案：A是O，S或NR 4; B是键或CR 5 R 6; R 4至R 6是H，C 1至C 6烷基，C 2至C 6烯基，C 2至C 6炔基，C 3至C 8环烷基，芳基或杂环或R 4和R 5稠合形成环; R 1是H，OH，NH 2，C 1至C 6烷基，C 3至C 6烯基，炔基或COR 3; R 如定义; R 2是H，卤素，CN，NO 2，C 1至C 6烷基，C 1至C 6烷氧基或C 1至C 6氨基烷基; R 3是与促孕剂和/或雌激素组合的取代苯环或杂芳环，用于治疗或预防继发性闭经，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，癌和腺癌，以及避孕等等。

68. 发明授权

US06566372B1 Bicyclic androgen and progesterone receptor modulator compounds and methods 有权
标题翻译：双环雄激素和孕激素受体调节剂的化合物和方法
公开(公告)号：US06566372B1
公开(公告)日：2003-05-20
申请号：US09649466
申请日：2000-08-24
申请人： Lin Zhi , Christopher Tegley , Barbara Pio , Cornelis Arjan Van Oeveren , Mehrnouch Motamedi , Esther Martinborough , Sarah West
发明人： Lin Zhi , Christopher Tegley , Barbara Pio , Cornelis Arjan Van Oeveren , Mehrnouch Motamedi , Esther Martinborough , Sarah West
IPC分类号： A61K3147
CPC分类号： C07D215/227 , C07D209/34 , C07D209/96 , C07D215/36 , C07D215/38 , C07D239/80 , C07D265/18 , C07D265/36 , C07D277/68 , C07D311/14 , C07D311/20 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04
摘要： The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.
摘要翻译：本发明涉及用于调节由AR和PR介导的过程的化合物，药物组合物和方法。更具体地，本发明涉及非甾类化合物和组合物，其是高亲和力，高特异性激动剂，部分激动剂（即部分激活剂和/或组织特异性激活剂）和AR和PR的拮抗剂。还提供制备这些化合物和药物组合物的方法，以及用于其合成的关键中间体。

69. 发明授权

US06407101B1 Cyanopyrroles 有权
标题翻译：青色
公开(公告)号：US06407101B1
公开(公告)日：2002-06-18
申请号：US09552544
申请日：2000-04-19
申请人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： C07D41310
CPC分类号： C07D403/04 , A61K31/405 , A61K31/5415 , C07D413/04
摘要： This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alky, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, allyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alko, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof
摘要翻译：本发明提供具有其中T为O，S或不存在的结构的式1的孕酮受体拮抗剂; R 1和R 2各自独立地为氢，烷基，取代的烷基; 或R 1和R 2一起形成环，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）p CH 2 - ， - O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - 或-CH 2 CH 2 NR 7 CH 2 CH 2 - n = 1-5; p = 1-4; q = 1-4; R 3是氢，OH，NH 2，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基或CORA; RA是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的 R5是氢，烯丙基或取代的烷基; R6是氢，烷基，取代的烷基或CORB; R是氢，烷基，取代的烷基，或烷氧基，取代的烷氧基， RB是氢，烷基，取代的烷基，烷基，取代的烷氧基，氨基烷基或取代的氨基烷基; R7是氢或烷基; 或其药学上可接受的盐

70. 发明授权

US06380235B1 Benzimidazolones and analogues 失效
标题翻译：苯并咪唑酮和类似物
公开(公告)号：US06380235B1
公开(公告)日：2002-04-30
申请号：US09552546
申请日：2000-04-19
申请人： Puwen Zhang , Reinhold H. W. Bender , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Puwen Zhang , Reinhold H. W. Bender , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K31415
CPC分类号： C07D263/58 , C07C215/76 , C07C229/18 , C07D235/26 , C07D235/28 , C07D241/44 , C07D277/68 , C07D279/16 , C07D409/04 , C07D487/04
摘要： The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, 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 alknyl, —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 heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt thereof. The invention also includes methods of contraception and methods of treating or preventing maladies associated with the progesterone receptor.
摘要翻译：本发明提供可用作孕酮受体激动剂和拮抗剂并具有以下通式的化合物和药物制剂：其中：A为O，S或NR4; B为A和C = Q之间的键，或部分CR5R6; R4， R5，R5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，或通过将R4 和R5至5至7元环; 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，取代的炔基，-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） R 2选自H，卤素，CN，NO 2或任选取代的C 1至C 6烷基，C 1至C 6烷氧基或C 1至C 6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元杂芳环; Q是O，S，NR8或CR9R10; 或其药学上可接受的盐。本发明还包括避孕方法和治疗或预防与孕酮受体相关的疾病的方法。

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