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1. 发明申请

WO2007126988A3 SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性雄激素受体调节剂及其使用方法
公开(公告)号：WO2007126988A3
公开(公告)日：2008-09-04
申请号：PCT/US2007007813
申请日：2007-03-29
申请人： UNIV TENNESSEE RES FOUNDATION , DALTON JAMES T , MILLER DUANE D , MARHEFKA CRAIG A , GAO WENQING
发明人： DALTON JAMES T , MILLER DUANE D , MARHEFKA CRAIG A , GAO WENQING
IPC分类号： A61K31/165 , A61K31/275 , A61K31/415 , A61K31/44 , A61K31/505 , A61K31/65 , C07C51/16 , C07C233/05 , C07D211/72 , C07D233/44 , C07D239/02
CPC分类号： A61K31/275 , A61K31/277 , A61K31/415 , A61K31/421 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/505 , A61K31/557 , A61K31/65 , A61K31/66 , C07C255/60 , C07D211/72 , C07D233/44 , C07D239/02
摘要： This invention provides a class of androgen receptor targeting agents (ARTA). The compounds are selective androgen receptor modulators (SARM) useful for, inter-alia, suppressing spermatogenesis, treating a subject having a hormone related condition, treating a subject suffering from prostate cancer, delaying the progression of prostate cancer, preventing the recurrence of prostate cancer, and treating the recurrence of prostate cancer.
摘要翻译：本发明提供一类雄激素受体靶向剂（ARTA）。这些化合物是选择性雄激素受体调节剂（SARM），其用于除其他外抑制精子发生，治疗具有激素相关病症的受试者，治疗患有前列腺癌的受试者，延缓前列腺癌的进展，预防前列腺癌的复发，并治疗前列腺癌的复发。

2. 发明申请

WO2005103050A2 AZAINDOLES USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES 审中-公开
标题翻译：亚胺醇作为岩石和其他蛋白激酶的抑制剂有用
公开(公告)号：WO2005103050A2
公开(公告)日：2005-11-03
申请号：PCT/US2005/011358
申请日：2005-04-04
申请人： VERTEX PHARMACEUTICALS INCORPORATED , GREEN, Jeremy , MILLER, Andrew , JIMENEZ, Juan-Miguel , MARHEFKA, Craig , CAO, Jingrong , COURT, John, J. , BANDARAGE, Upul, K. , GAO, Huai , NANTHAKUMAR, Suganthini
发明人： GREEN, Jeremy , MILLER, Andrew , JIMENEZ, Juan-Miguel , MARHEFKA, Craig , CAO, Jingrong , COURT, John, J. , BANDARAGE, Upul, K. , GAO, Huai , NANTHAKUMAR, Suganthini
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

3. 发明申请

WO2003049675A3 TREATING MUSCLE WASTING WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2003049675A3
公开(公告)日：2003-06-19
申请号：PCT/US2002/036147
申请日：2002-12-05
申请人： GTX, INC. , STEINER, Mitchell, S. , VEVERKA, Karen, A. , DALTON, James, T. , MILLER, Duane, D. , CHEN, Jiyun , FISHER, Scott , KIM, Juhyun , OKOLICANY, Juraj , MARHEFKA, Craig , HWANG, Dong Jin , CHUNG, Kiwon
发明人： STEINER, Mitchell, S. , VEVERKA, Karen, A. , DALTON, James, T. , MILLER, Duane, D. , CHEN, Jiyun , FISHER, Scott , KIM, Juhyun , OKOLICANY, Juraj , MARHEFKA, Craig , HWANG, Dong Jin , CHUNG, Kiwon
IPC分类号： A61K31/32
摘要： This invention provides: a method of treating a subject suffering from a muscle wasting disorder; a method of preventing a muscle wasting disorder in a subject; a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide or any combination thereof, as described herein.

4. 发明申请

WO2007133622A2 SELECTIVE INHIBITORS OF ROCK PROTEIN KINASE AND USES THEREOF 审中-公开
标题翻译：岩石蛋白激酶的选择性抑制剂及其用途
公开(公告)号：WO2007133622A2
公开(公告)日：2007-11-22
申请号：PCT/US2007011285
申请日：2007-05-10
申请人： VERTEX PHARMA , GREEN JEREMY , CAO JINGRONG , BANDARAGE UPUL , COME JON , MARHEFKA CRAIG
发明人： GREEN JEREMY , CAO JINGRONG , BANDARAGE UPUL , COME JON , MARHEFKA CRAIG
IPC分类号： C07D409/04 , A61K31/427 , A61P35/00 , C07D417/04 , C07D417/14
CPC分类号： C07D409/04 , C07D409/14 , C07D417/04 , C07D417/14
摘要： Described herein are compounds that are useful as ROCK inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including cardiovascular, inflammatory, neurological, or proliferative diseases or disorders.
摘要翻译：本文描述的是可用作ROCK抑制剂的化合物。这些化合物及其药学上可接受的组合物可用于治疗或减轻各种障碍（包括心血管，炎症，神经或增殖性疾病或病症）的严重性。

5. 发明申请

WO2007126988A2 SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性雄激素受体调节剂及其使用方法
公开(公告)号：WO2007126988A2
公开(公告)日：2007-11-08
申请号：PCT/US2007/007813
申请日：2007-03-29
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION , DALTON, James, T. , MILLER, Duane, D. , MARHEFKA, Craig, A. , GAO, Wenqing
发明人： DALTON, James, T. , MILLER, Duane, D. , MARHEFKA, Craig, A. , GAO, Wenqing
IPC分类号： A61K31/66 , A61K31/277 , A61K31/433 , A61K31/426 , A61K31/421 , A61K31/557 , A61K31/275
CPC分类号： A61K31/275 , A61K31/277 , A61K31/415 , A61K31/421 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/505 , A61K31/557 , A61K31/65 , A61K31/66 , C07C255/60 , C07D211/72 , C07D233/44 , C07D239/02
摘要： This invention provides a class of androgen receptor targeting agents (ARTA). The compounds are selective androgen receptor modulators (SARM) useful for, inter-alia , suppressing spermatogenesis, treating a subject having a hormone related condition, treating a subject suffering from prostate cancer, delaying the progression of prostate cancer, preventing the recurrence of prostate cancer, and treating the recurrence of prostate cancer.
摘要翻译：本发明提供一类雄激素受体靶向剂（ARTA）。这些化合物是选择性雄激素受体调节剂（SARM），其用于除其他外抑制精子发生，治疗具有激素相关病症的受试者，治疗患有前列腺癌的受试者，延缓前列腺癌的进展，预防前列腺癌的复发，并治疗前列腺癌的复发。

6. 发明申请

WO2004041813A1 COMPOSITIONS USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES 审中-公开
标题翻译：组合物作为岩石和其他蛋白激酶的抑制剂有用
公开(公告)号：WO2004041813A1
公开(公告)日：2004-05-21
申请号：PCT/US2003/034319
申请日：2003-10-30
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CAO, Jingrong , GAO, Huai , GREEN, Jeremy , MARHEFKA, Craig
发明人： CAO, Jingrong , GAO, Huai , GREEN, Jeremy , MARHEFKA, Craig
IPC分类号： C07D409/04
CPC分类号： C07D417/14 , C07D409/04 , C07D409/14 , C07D417/04
摘要： The present invention relates to substitute thiazole and thiophene derivatives useful as inhibitors of rock and other protein kinaeses. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders, including proliferative, cardiac and neurodegenerative diseases.
摘要翻译：本发明涉及可用作岩石和其他蛋白质猕猴桃的抑制剂的噻唑和噻吩衍生物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症（包括增殖性，心脏和神经变性疾病）的方法。

7. 发明申请

WO2005103050A3 AZAINDOLES USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES 审中-公开
标题翻译：亚胺醇作为岩石和其他蛋白激酶的抑制剂有用
公开(公告)号：WO2005103050A3
公开(公告)日：2006-10-05
申请号：PCT/US2005011358
申请日：2005-04-04
申请人： VERTEX PHARMA , GREEN JEREMY , MILLER ANDREW , JIMENEZ JUAN-MIGUEL , MARHEFKA CRAIG , CAO JINGRONG , COURT JOHN J , BANDARAGE UPUL K , GAO HUAI , NANTHAKUMAR SUGANTHINI
发明人： GREEN JEREMY , MILLER ANDREW , JIMENEZ JUAN-MIGUEL , MARHEFKA CRAIG , CAO JINGRONG , COURT JOHN J , BANDARAGE UPUL K , GAO HUAI , NANTHAKUMAR SUGANTHINI
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P37/08
CPC分类号： C07D471/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

8. 发明申请

WO2005039564A1 PHTHALIMIDE COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂有用的邻苯二胺化合物
公开(公告)号：WO2005039564A1
公开(公告)日：2005-05-06
申请号：PCT/US2004/032548
申请日：2004-10-04
申请人： VERTEX PHARMACEUTICALS INCORPORATED , GREEN, Jeremy , MARHEFKA, Craig
发明人： GREEN, Jeremy , MARHEFKA, Craig
IPC分类号： A61K31/4035
CPC分类号： C04B35/632 , C07D209/46 , C07D209/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04
摘要： The present invention provides compounds of formula I as inhibitors of protein kinase, particularly inhibitors of AKT, PDK1, p70S6K, or ROCK kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides processes for preparing the compounds of the invention, pharmaceutical compositions comprising the compounds, and methods of utilizing those compounds and compositions in the treatment of various disorders.
摘要翻译：本发明提供式I化合物作为蛋白激酶的抑制剂，特别是AKT，PDK1，p70S6K或ROCK激酶的抑制剂，涉及增殖性和神经变性疾病的哺乳动物蛋白激酶。本发明还提供了制备本发明化合物的方法，包含该化合物的药物组合物，以及利用这些化合物和组合物治疗各种疾病的方法。

9. 发明申请

WO2005019190A2 AMINOFURAZAN COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：氨基脲类化合物可用作蛋白激酶抑制剂
公开(公告)号：WO2005019190A2
公开(公告)日：2005-03-03
申请号：PCT/US2004/027182
申请日：2004-08-20
申请人： VERTEX PHARMACEUTICALS INCORPORATED , COME, Jon, H. , GREEN, Jeremy , MARHEFKA, Craig , HARBESON, Scott, L. , PHAM, Ly
发明人： COME, Jon, H. , GREEN, Jeremy , MARHEFKA, Craig , HARBESON, Scott, L. , PHAM, Ly
IPC分类号： C07D271/00
CPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用于蛋白激酶抑制剂的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

10. 发明申请

WO2003106401A1 N-BRIDGED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译： N-桥选择性受体调节剂及其使用方法
公开(公告)号：WO2003106401A1
公开(公告)日：2003-12-24
申请号：PCT/US2003/016219
申请日：2003-06-17
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION , DALTON, James , MILLER, Duane, D. , MARHEFKA, Craig, A. , GAO, Wenqing
发明人： DALTON, James , MILLER, Duane, D. , MARHEFKA, Craig, A. , GAO, Wenqing
IPC分类号： C07C233/05
CPC分类号： C07D211/72 , A61K31/415 , A61K31/44 , A61K31/505 , A61K31/65 , C07C237/10 , C07C255/60 , C07D233/44 , C07D239/02
摘要： This invention provides a class of androgen receptor targeting agents (ARTA) The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy, and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.
摘要翻译：本发明提供了一类雄激素受体靶向剂（ARTA）。该药物定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。已经发现几种SARM化合物对雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。已经发现其他SARM化合物对雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 SARM化合物，单独或作为组合物，可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与雄激素降解有关的疾病（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌肉减少症，骨质减少症，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法，和/或g）降低前列腺癌的发作，停止或导致消退。

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