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1. 发明申请

WO2009082437A2 SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) AND USES THEREOF 审中-公开
标题翻译：选择性雄激素受体调节剂（SARMS）及其用途
公开(公告)号：WO2009082437A2
公开(公告)日：2009-07-02
申请号：PCT/US2008013657
申请日：2008-12-12
申请人： LIGAND PHARM INC , ZHI LIN
发明人： ZHI LIN
IPC分类号： C07D207/08 , A61K31/402 , A61P5/26 , C07D207/09 , C07D498/04
CPC分类号： C07D207/09 , A61K31/401 , A61K31/402 , A61K31/5383 , A61K45/06 , C07D207/08 , C07D207/16 , C07D498/04
摘要： Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors; and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
摘要翻译：本文提供了结合雄激素受体和/或调节雄激素受体活性的化合物; 以及制备和使用这些化合物的方法。还提供了包括这些化合物的组合物和用于制备和使用这些组合物的方法。

2. 发明申请

WO2007106564A2 SYNTHESIS OF THROMBOPOIETIN ACTIVITY MODULATING COMPOUNDS 审中-公开
标题翻译：血小板活化调节化合物的合成
公开(公告)号：WO2007106564A2
公开(公告)日：2007-09-20
申请号：PCT/US2007/006547
申请日：2007-03-14
申请人： LIGAND PHARMACEUTICALS INC. , PHILLIPS, Dean , ZHI, Lin , DALGARD, Jackline E.
发明人： PHILLIPS, Dean , ZHI, Lin , DALGARD, Jackline E.
IPC分类号： C07D209/40
CPC分类号： C07D209/40
摘要： Disclosed herein are various methods for synthesizing compounds that modulate thrombopoietin activity. Also disclosed are intermediates useful for the preparation of these compounds.
摘要翻译：本文公开了用于合成调节血小板生成素活性的化合物的各种方法。还公开了可用于制备这些化合物的中间体。

3. 发明申请

WO2005018573A3 6-CYCLOAMINO-2-QUINOLINONE DERIVATIVES AS ANDROGEN RECEPTOR MODULATOR COMPOUNDS 审中-公开
标题翻译：作为雄激素受体调节剂化合物的6-环脒基-2-喹啉酮衍生物
公开(公告)号：WO2005018573A3
公开(公告)日：2005-05-06
申请号：PCT/US2004027483
申请日：2004-08-23
申请人： LIGAND PHARM INC , ZHI LIN , MARTINBOROUGH ESTHER , SHEN YIXING , STEVENS LAU THOMAS LOT , WU MIN , LONG YUN OLIVER
发明人： ZHI LIN , MARTINBOROUGH ESTHER , SHEN YIXING , STEVENS LAU THOMAS LOT , WU MIN , LONG YUN OLIVER
IPC分类号： A61K20060101 , A61K31/47 , C07D215/12 , C07D215/16
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。还提供了制备这种化合物和药物组合物的方法。

4. 发明申请

WO0066225A8 CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC CARBAMATES AND AMIDE DERIVATIVES 审中-公开
标题翻译：含有环状碳酸酯和酰胺衍生物的合成组合物
公开(公告)号：WO0066225A8
公开(公告)日：2002-05-30
申请号：PCT/US0011846
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC , GRUBB GARY S , ZHI LIN , JONES TODD K , SANTILLI ARTHUR A , TEGLEY CHRISTOPHER M , VIET ANDREW Q , ZHANG PUWEN , FENSOME ANDREW , WROBEL JAY E , EDWARDS JAMES P
发明人： GRUBB GARY S , ZHI LIN , JONES TODD K , SANTILLI ARTHUR A , TEGLEY CHRISTOPHER M , VIET ANDREW Q , ZHANG PUWEN , FENSOME ANDREW , WROBEL JAY E , EDWARDS JAMES P
IPC分类号： C07D498/04 , A61K31/40 , A61K31/445 , A61K31/535 , A61K31/5365 , A61K31/56 , A61K45/06 , A61P15/18 , A61K31/565 , A61K31/57
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, estrogens, or both, substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (I) 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 a 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, COR , or NR COR ; or R and R 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 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 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，雌激素或两者作为孕酮受体的拮抗剂的代用药物，其具有一般结构（I）的循环组合疗法和方案，其中A和B是选自S，CH 或N; 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，杂环基，取代的杂环基，COR A或NR C CORA; 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。

5. 发明申请

WO0066564A8 BENZIMIDAZOLONES AND ANALOGUES AND THEIR USE AS PROGESTERONE RECEPTOR LIGANDS 审中-公开
标题翻译：苯并咪唑和类似物及其作为孕酮受体配体使用
公开(公告)号：WO0066564A8
公开(公告)日：2001-08-02
申请号：PCT/US0011824
申请日：2000-05-01
申请人： AMERICAN HOME PROD , LIGAND PHARM INC , ZHANG PUWEN , BENDER REINHOLD H W , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , WROBEL JAY E , EDWARDS JAMES P
发明人： ZHANG PUWEN , BENDER REINHOLD H W , ZHI LIN , JONES TODD K , TEGLEY CHRISTOPHER M , WROBEL JAY E , EDWARDS JAMES P
IPC分类号： A61K31/136 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/498 , A61K31/4985 , A61K31/5415 , A61P5/00 , A61P5/24 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07C215/76 , C07C229/18 , C07D235/26 , C07D235/28 , C07D241/44 , C07D263/58 , C07D277/68 , C07D279/16 , C07D409/04 , C07D487/04 , A61K31/429
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 general formula (a): wherein A is O, S, or NR ; B is a bond between A and C=Q, or the moiety CR R ; R , R , R 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 heteorcyclic groups, or cyclic alkyl constructed by fusing R and R to from a 5 to 7 membered ring; R is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituded 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 toC3 aminoalkyl) groups; R is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R is selected from a trisubstituted benzene ring; or a 5- or 6- membered heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR , or CR R ; 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通式（a）的化合物和药物制剂：其中A是O，S或NR 4; B是A和C = Q之间的键，或部分CR 5 R 6; R 4，R 5，R 6独立地选自H或任选取代的C 1 -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，取代的C 3至C 8环烷基，芳基，或杂环基团，或通过将R 4和R 5与5至7元环稠合而构成的环状烷基; R 1选自H，OH，NH 2，C 1至C 6烷基，取代的C 1 -C 6烷基，C 3至C 6烯基，取代的C 1至C 6烯基，炔基，取代的炔基，-COH或任选取代的-CO 至C 3烷基），-CO（芳基），-CO（C 1至C 3烷氧基）或-CO（C 1至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; R 3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; Q是O，S，NR 8或CR 9 R 10; 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。

6. 发明申请

WO2012068406A3 USE OF HEMATOPOIETIC GROWTH FACTOR MIMETICS 审中-公开
标题翻译： HEMATOPOIETIC GROWTH FACTOR MIME的使用
公开(公告)号：WO2012068406A3
公开(公告)日：2012-11-01
申请号：PCT/US2011061247
申请日：2011-11-17
申请人： LIGAND PHARM INC , BISSONNETTE REID P , HUDSON ANDREW R , MARSCHKE KEITH B , RUNGTA DEEPA , ZHI LIN
发明人： BISSONNETTE REID P , HUDSON ANDREW R , MARSCHKE KEITH B , RUNGTA DEEPA , ZHI LIN
IPC分类号： A61K31/4184 , A61K31/4188 , A61K31/495 , A61K31/53 , A61P7/00 , A61P43/00
CPC分类号： C07C243/38 , A61K31/00 , A61K31/166 , A61K31/167 , A61K31/194 , A61K31/36 , A61K31/402 , A61K31/404 , A61K31/4155 , A61K31/4184 , A61K31/4192 , A61K31/4245 , A61K31/4402 , A61K31/496 , A61K31/5377 , C07D207/27 , C07D207/327 , C07D209/08 , C07D233/61 , C07D235/18 , C07D295/155 , C07D317/68 , C07D401/10 , C07D413/04 , C07D413/12 , C07D491/113
摘要： The present invention relates to uses of small molecule mimetics of hematopoietic growth factors. In particular the present invention relates to uses of small molecule mimetics of erythropoietin.
摘要翻译：本发明涉及造血生长因子的小分子模拟物的用途。特别地，本发明涉及促红细胞生成素的小分子模拟物的用途。

7. 发明申请

WO2012068406A2 USE OF HEMATOPOIETIC GROWTH FACTOR MIMETICS 审中-公开
标题翻译：使用造血生长因子模拟物
公开(公告)号：WO2012068406A2
公开(公告)日：2012-05-24
申请号：PCT/US2011/061247
申请日：2011-11-17
申请人： LIGAND PHARMACEUTICALS INCORPORATED , BISSONNETTE, Reid, P. , HUDSON, Andrew, R. , MARSCHKE, Keith, B. , RUNGTA, Deepa , ZHI, Lin
发明人： BISSONNETTE, Reid, P. , HUDSON, Andrew, R. , MARSCHKE, Keith, B. , RUNGTA, Deepa , ZHI, Lin
IPC分类号： A61K31/421
CPC分类号： C07C243/38 , A61K31/00 , A61K31/166 , A61K31/167 , A61K31/194 , A61K31/36 , A61K31/402 , A61K31/404 , A61K31/4155 , A61K31/4184 , A61K31/4192 , A61K31/4245 , A61K31/4402 , A61K31/496 , A61K31/5377 , C07D207/27 , C07D207/327 , C07D209/08 , C07D233/61 , C07D235/18 , C07D295/155 , C07D317/68 , C07D401/10 , C07D413/04 , C07D413/12 , C07D491/113
摘要： The present invention relates to uses of small molecule mimetics of hematopoietic growth factors. In particular the present invention relates to uses of small molecule mimetics of erythropoietin.
摘要翻译：本发明涉及造血生长因子的小分子模拟物的用途。具体而言，本发明涉及促红细胞生成素的小分子模拟物的用途。

8. 发明申请

WO2010135350A2 BIPHENYL INTERMEDIATE COMPOUNDS AND METHODS FOR THE PREPARATION OF A DUAL ANGIOTENSIN II AND ENDOTHELIN A RECEPTOR ANTAGONIST 审中-公开
标题翻译：联苯胺中间体化合物和制备双抗血管素II和内皮素受体拮抗剂的方法
公开(公告)号：WO2010135350A2
公开(公告)日：2010-11-25
申请号：PCT/US2010/035294
申请日：2010-05-18
申请人： PHARMACOPEIA, LLC , ZHI, Lin , PICKENS, Jason , VAN OEVEREN, Cornelius, A. , HENDERSON, Ian
发明人： ZHI, Lin , PICKENS, Jason , VAN OEVEREN, Cornelius, A. , HENDERSON, Ian
IPC分类号： C07C309/86 , C07D327/08 , C07C309/87 , C07C43/174 , C07D233/70
CPC分类号： C07D413/12 , C07C43/1786 , C07C309/32 , C07C309/42 , C07C309/66 , C07C309/73 , C07D235/02 , C07D327/02
摘要： Disclosed herein are methods and compounds useful in preparing N-(3,4-dimethyl-5-isoxazolyl)-2-(4-(2-butyl-4-oxo-l,3-diazospiro[4.4]non-l-en-3yl)methyl-2-ethoxymethylphenyl)phenylsulfonamide.
摘要翻译：本文公开了可用于制备N-（3,4-二甲基-5-异恶唑基）-2-（4-（2-丁基-4-氧代-1,3-二氮杂螺环[4.4]壬-1-烯 -3yl）甲基-2-乙氧基甲基苯基）苯磺酰胺。

9. 发明申请

WO2009103007A2 STEROID HORMONE RECEPTOR MODULATOR COMPOUNDS AND METHODS 审中-公开
标题翻译：甾体激素受体调节剂化合物和方法
公开(公告)号：WO2009103007A2
公开(公告)日：2009-08-20
申请号：PCT/US2009/034131
申请日：2009-02-13
申请人： LIGAND PHARMACEUTICALS INCORPORATED , ROACH, Steven, L. , HUDSON, Andrew, R. , VALDEZ, Lino J. , HIGUCHI, Robert, I. , ZHI, Lin , VASSAR, Angie, C. , LANDRY-BAYLE, Adrienne , ADAMS, Mark, E. , ROWLEY, Charlene, V. , LAMER, Ryan, B. , GRANT, Virginia, Heather Sharron
发明人： ROACH, Steven, L. , HUDSON, Andrew, R. , VALDEZ, Lino J. , HIGUCHI, Robert, I. , ZHI, Lin , VASSAR, Angie, C. , LANDRY-BAYLE, Adrienne , ADAMS, Mark, E. , ROWLEY, Charlene, V. , LAMER, Ryan, B. , GRANT, Virginia, Heather Sharron
IPC分类号： C07D401/04 , C07D401/14 , C07D407/14 , C07D413/04 , C07D413/14 , C07D417/14 , A61K31/4709 , A61P37/02
CPC分类号： C07D401/04 , C07D401/14 , C07D407/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14
摘要： This invention relates to compounds that bind to intracellular receptors and/or modulate activity of intracellular receptors, and to methods for making and using such compounds.
摘要翻译：本发明涉及与细胞内受体结合和/或调节细胞内受体活性的化合物，以及制备和使用此类化合物的方法。

10. 发明申请

WO2007106564A3 SYNTHESIS OF THROMBOPOIETIN ACTIVITY MODULATING COMPOUNDS 审中-公开
标题翻译：血小板活化调节化合物的合成
公开(公告)号：WO2007106564A3
公开(公告)日：2008-02-14
申请号：PCT/US2007006547
申请日：2007-03-14
申请人： LIGAND PHARM INC , PHILLIPS DEAN , ZHI LIN , DALGARD JACKLINE E
发明人： PHILLIPS DEAN , ZHI LIN , DALGARD JACKLINE E
IPC分类号： C07D209/40
CPC分类号： C07D209/40
摘要： Disclosed herein are various methods for synthesizing compounds that modulate thrombopoietin activity. Also disclosed are intermediates of the following formula useful for the preparation of these compounds.
摘要翻译：本文公开了用于合成调节血小板生成素活性的化合物的各种方法。还公开了可用于制备这些化合物的下式的中间体。

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