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公开(公告)号:US20060030545A1
公开(公告)日:2006-02-09
申请号:US11170247
申请日:2005-06-29
申请人: Xiaoqin Cheng , Gary Cook , Manoj Desai , Edward Doerffler , Gong-Xin He , Choung Kim , William Lee , John Rohloff , Jianying Wang , Zheng-Yu Yang
发明人: Xiaoqin Cheng , Gary Cook , Manoj Desai , Edward Doerffler , Gong-Xin He , Choung Kim , William Lee , John Rohloff , Jianying Wang , Zheng-Yu Yang
IPC分类号: A61K31/675 , C07F9/6512
CPC分类号: C07F9/65616 , Y02P20/55
摘要: Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1; RX1 is RX; RX2 is alkenyl of 2 to 18 carbon atoms or alkynyl of 2 to 18 carbon atoms; Y1 is ═O, —O(RX), ═S, —N(RX), —N(O)(RX), —N(ORX), —N(O)(ORX), or —N(N(RX)(RX)); RX is independently R1, R2, R4, W3, or a protecting group; R1 is independently —H or alkyl of 1 to 18 carbon atoms; R2 is independently R3 or R4 wherein each R4 is independently substituted with 0 to 3 R3 groups or taken together at a carbon atom, two R2 groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R3 groups; R3 is R3a, R3b, R3c or R3d, provided that when R3 is bound to a heteroatom, then R3 is R3c or R3d; R3a is —H, —F, —Cl, —Br, —I, —CF3, —CN, N3, —NO2, or —OR4; R3b is ═O, —O(R4), ═S, —N(R4), —N(O)(R4), —N(OR4), —N(O)(OR4), or —N(N(R4)(R4)); R3c is —R4, —N(R4)(R4), —SR4, —S(O)R4, —S(O)2R4, —S(O)(OR4), —S(O)2(OR4), —OC(R3b)R4, —OC(R3b)OR4, —OC(R3b)(N(R4)(R4)), —SC(R3b)R4, —SC(R3b)OR4, —SC(R3b)(N(R4)(R4)), —N(R4)C(R3b)R4, —N(R4)C(R3b)OR4, —N(R4)C(R3b)(N(R4)(R4)), W3 or —R5W3; R3d is —C(R3b)R4, —C(R3b)OR4, —C(R3b)W3, —C(R3b)OW3 or —C(R3b)(N(R4)(R4)); R4 is —H, or an alkyl of 1 to 18 carbon atoms, alkenyl of 2 to 18 carbon atoms, or alkynyl of 2 to 18 carbon atoms; R5 is alkylene of 1 to 18 carbon atoms, alkenylene of 2 to 18 carbon atoms, or alkynylene of 2 to 18 carbon atoms; W3 is W4 or W5; W4 is R6, —C(R3b)R6, —C(R3b)W5, —SOM2R6, or —SOM2W5, wherein R6 is R4 wherein each R4 is substituted with 0 to 3 R3 groups; W5 is carbocycle or heterocycle wherein W5 is independently substituted with 0 to 3 R2 groups; and M2 is 0, 1 or 2; or pharmaceutically acceptable salts thereof.
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公开(公告)号:US20050222090A1
公开(公告)日:2005-10-06
申请号:US11026303
申请日:2004-12-29
申请人: Xiaqin Cheng , Gary Cook , Manoj Desai , Edward Doerffler , Gong-Xin He , Choung Kim , William Lee , John Rohloff , Jianying Wang , Zheng-Yu Yang
发明人: Xiaqin Cheng , Gary Cook , Manoj Desai , Edward Doerffler , Gong-Xin He , Choung Kim , William Lee , John Rohloff , Jianying Wang , Zheng-Yu Yang
IPC分类号: A61K31/66 , A61K31/675 , C07F9/44 , C07F9/6561
CPC分类号: C07F9/65616 , Y02P20/55
摘要: Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1; RX1 and RX2 are independently RX; Y1 is ═O, —O(RX), ═S, —N(RX), —N(O)(RX), —N(ORX), —N(O)(ORX), or —N(N(RX)(RX)); RX is independently R1, R2, R4, W3, or a protecting group; R1 is independently —H or alkyl of 1 to 18 carbon atoms; R2 is independently R3 or R4 wherein each R4 is independently substituted with 0 to 3 R3 groups or taken together at a carbon atom, two R2 groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R3 groups; R3 is R3a, R3b, R3c or R3d, provided that when R3 is bound to a heteroatom, then R3 is R3c or R3d; R3a is —H, —F, —Cl, —Br, —I, —CF3, —CN, N3, —NO2, or —OR4; R3b is ═O, —O(R4), ═S, —N(R4), —N(O)(R4), —N(OR4), —N(O)(OR4), or —N(N(R4)(R4)); R3c is —R4, —N(R4)(R4), —SR4, —S(O)R4, —S(O)2R4, —S(O)(OR4), —S(O)2(OR4), —OC(R3b)R4, —OC(R3b)OR4, —OC(R3b)(N(R4)(R4)), —SC(R3b)R4, —SC(R3b)OR4, —SC(R3b)(N(R4)(R4)), —N(R4)C(R3b)R4, —N(R4)C(R3b)OR4, N(R4)C(R3b)(N(R4)(R4)), W3 or —R5W3; R3d is —C(R3b)R4, —C(R3b)OR4, —C(R3b)W3, —C(R3b)OW3 or —C(R3b)(N(R4)(R4)); R4 is —H, or an alkyl of 1 to 18 carbon atoms, alkenyl of 2 to 18 carbon atoms, or alkynyl of 2 to 18 carbon atoms; R5 is alkylene of 1 to 18 carbon atoms, alkenylene of 2 to 18 carbon atoms, or alkynylene of 2 to 18 carbon atoms; W3 is W4 or W5; W4 is R6, —C(R3b)R6, —C(R3b)W5, —SOM2R6, or —SOM2W5, wherein R6 is R4 wherein each R4 is substituted with 0 to 3 R3 groups; W5 is carbocycle or heterocycle wherein W5 is independently substituted with 0 to 3 R2 groups; and M2 is 0, 1 or 2; and pharmaceutically acceptable salts thereof.
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公开(公告)号:US20060264404A1
公开(公告)日:2006-11-23
申请号:US11258621
申请日:2005-10-25
申请人: Constantine Boojamra , Carina Cannizzaro , James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Manoj Desai , Maria Fardis , Craig Gibbs , Ralph Hirschmann , Alan Huang , Haolun Jin , Choung Kim , Thorsten Kirschberg , Steven Krawczyk , Christopher Lee , William Lee , Kuei-Ying Lin , Richard Mackman , David Markevitch , Peter Nelson , David Oare , Vidya Prasad , Hyung-Jung Pyun , Adrian Ray , Rosemarie Sherlock , Sundaramoorthi Swaminathan , William Watkins , Jennifer Zhang , Lijun Zhang
发明人: Constantine Boojamra , Carina Cannizzaro , James Chen , Xiaowu Chen , Aesop Cho , Lee Chong , Manoj Desai , Maria Fardis , Craig Gibbs , Ralph Hirschmann , Alan Huang , Haolun Jin , Choung Kim , Thorsten Kirschberg , Steven Krawczyk , Christopher Lee , William Lee , Kuei-Ying Lin , Richard Mackman , David Markevitch , Peter Nelson , David Oare , Vidya Prasad , Hyung-Jung Pyun , Adrian Ray , Rosemarie Sherlock , Sundaramoorthi Swaminathan , William Watkins , Jennifer Zhang , Lijun Zhang
IPC分类号: A61K31/675 , C07F9/6512
CPC分类号: C07F9/65616 , C07F9/4006 , C07F9/4465 , C07F9/5304 , C07F9/650952 , C07F9/653 , C07F9/65507 , C07F9/65515 , C07F9/65517 , C07F9/65583 , C07F9/65586 , C07F9/6561
摘要: The invention is related to phosphorus substituted therapeutic agents, compositions containing such phosphorus substituted agents, and therapeutic methods that include the administration of such phosphorus substituted agents, as well as to processes and intermediates useful for preparing such agents.
摘要翻译: 本发明涉及磷取代的治疗剂,含有这种磷取代剂的组合物,以及包括施用这种磷取代剂的治疗方法,以及可用于制备这种药剂的方法和中间体。
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公开(公告)号:US07417055B2
公开(公告)日:2008-08-26
申请号:US10832811
申请日:2004-04-26
申请人: Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Manoj Desai , Maria Fardis , Thorsten Kirschberg , Richard L. Mackman , Sundaramoorthi Swaminathan , William J. Watkins
发明人: Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Manoj Desai , Maria Fardis , Thorsten Kirschberg , Richard L. Mackman , Sundaramoorthi Swaminathan , William J. Watkins
IPC分类号: A61K31/44 , C07D239/72
CPC分类号: A61K31/662 , A61K47/54 , A61K47/548 , C07F9/58 , C07F9/6561
摘要: The invention is related to phosphorus substituted kinase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译: 本发明涉及磷取代的激酶抑制化合物,含有这些化合物的组合物,以及包括施用这些化合物的治疗方法,以及可用于制备这些化合物的方法和中间体。
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公开(公告)号:US20070244109A1
公开(公告)日:2007-10-18
申请号:US11761937
申请日:2007-06-12
申请人: Manoj Desai , Simon Ng , Zhi-Jie Ni , Keith Pfister , Savithri Ramurthy , Sharadha Subramanian , Allan Wagman
发明人: Manoj Desai , Simon Ng , Zhi-Jie Ni , Keith Pfister , Savithri Ramurthy , Sharadha Subramanian , Allan Wagman
IPC分类号: A61K31/44 , A61K31/445 , A61K31/497 , A61K31/535 , A61P25/28 , A61P3/10
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D453/02 , C07D487/08
摘要: New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
摘要翻译: 提供了新的基于吡咯的化合物,组合物和抑制糖原合酶激酶(GSK3)活性并在体内治疗GSK3介导的病症的方法。 本发明的方法,化合物和组合物可以单独使用或与其它药理活性剂组合用于治疗由GSK3活性介导的病症,例如糖尿病,阿尔茨海默病和其他神经变性疾病,肥胖症,动脉粥样硬化性心血管疾病,必需的 高血压,多囊卵巢综合征,X综合征,缺血,创伤性脑损伤,双相情感障碍,免疫缺陷或癌症。
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公开(公告)号:US06869969B2
公开(公告)日:2005-03-22
申请号:US10713621
申请日:2003-11-13
申请人: Verena D. Huebner , Xiaodong Lin , Ian James , Liya Chen , Manoj Desai , Jennifer C. Moore , Beata Krywult , Thayalan Navaratnam , Rajinder Singh , Rob Trainor , Liang Wang
发明人: Verena D. Huebner , Xiaodong Lin , Ian James , Liya Chen , Manoj Desai , Jennifer C. Moore , Beata Krywult , Thayalan Navaratnam , Rajinder Singh , Rob Trainor , Liang Wang
IPC分类号: A61K31/42 , A61K31/422 , A61K31/423 , A61K31/424 , A61K31/4433 , A61K31/4439 , A61K31/454 , A61K31/4745 , A61P5/30 , A61P19/10 , A61P25/28 , A61P43/00 , C07D261/08 , C07D261/10 , C07D261/18 , C07D261/20 , C07D409/04 , C07D413/04 , C07D413/12 , C07D498/04 , C07D261/02 , C07D261/06
CPC分类号: C07D261/10 , C07D261/08 , C07D261/18 , C07D261/20 , C07D413/04 , C07D413/12
摘要: Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.
摘要翻译: 描述了在调节雌激素受体活性方面具有出人意料的和惊人的活性的异恶唑雌激素受体激动剂和拮抗剂化合物。 此外,公开了治疗或预防雌激素受体介导的病症的方法和组合物。 本发明的化合物,方法和组合物可用于预防或治疗雌激素受体介导的障碍,例如骨质疏松症,乳腺和子宫内膜癌,动脉粥样硬化和阿尔茨海默氏病。
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公开(公告)号:US06387920B2
公开(公告)日:2002-05-14
申请号:US09833392
申请日:2001-04-11
申请人: Verena D. Huebner , Xiaodong Lin , Ian James , Liya Chen , Manoj Desai , Jennifer C. Moore , Beata Krywult , Thayalan Navaratnam , Rajinder Singh , Rob Trainor , Liang Wang
发明人: Verena D. Huebner , Xiaodong Lin , Ian James , Liya Chen , Manoj Desai , Jennifer C. Moore , Beata Krywult , Thayalan Navaratnam , Rajinder Singh , Rob Trainor , Liang Wang
IPC分类号: A61K3144
CPC分类号: C07D261/10 , C07D261/08 , C07D261/18 , C07D261/20 , C07D413/04 , C07D413/12
摘要: Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.
摘要翻译: 描述了在调节雌激素受体活性方面具有出人意料的和惊人的活性的异恶唑雌激素受体激动剂和拮抗剂化合物。 此外,公开了治疗或预防雌激素受体介导的病症的方法和组合物。 本发明的化合物,方法和组合物可用于预防或治疗雌激素受体介导的障碍,例如骨质疏松症,乳腺和子宫内膜癌,动脉粥样硬化和阿尔茨海默氏病。
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公开(公告)号:US20090181930A1
公开(公告)日:2009-07-16
申请号:US12167038
申请日:2008-07-02
申请人: Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Manoj Desai , Maria Fardis , Thorsten Kirschberg , Richard L. Mackman , Sundaramoorthi Swaminathan , William J. Watkins
发明人: Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Manoj Desai , Maria Fardis , Thorsten Kirschberg , Richard L. Mackman , Sundaramoorthi Swaminathan , William J. Watkins
IPC分类号: C07F9/6512 , A61K31/675
CPC分类号: A61K31/662 , A61K47/54 , A61K47/548 , C07F9/58 , C07F9/6561
摘要: The invention is related to phosphorus substituted kinase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译: 本发明涉及磷取代的激酶抑制化合物,含有这些化合物的组合物,以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。
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公开(公告)号:US07470724B2
公开(公告)日:2008-12-30
申请号:US10833295
申请日:2004-04-26
申请人: Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Manoj Desai , Maria Fardis , Alan X. Huang , Thorsten Kirschberg , Christopher P. Lee , Richard L. Mackman , Peter H. Nelson , Hyung-Jung Pyun , Adrian S. Ray , William J. Watkins , Jennifer R. Zhang , Sundaramoorthi Swaminathan
发明人: Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Manoj Desai , Maria Fardis , Alan X. Huang , Thorsten Kirschberg , Christopher P. Lee , Richard L. Mackman , Peter H. Nelson , Hyung-Jung Pyun , Adrian S. Ray , William J. Watkins , Jennifer R. Zhang , Sundaramoorthi Swaminathan
IPC分类号: A61K31/27
CPC分类号: A61K47/548 , A61K47/542
摘要: The invention is related to phosphonate substituted compounds having immuno-modulatory activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译: 本发明涉及具有免疫调节活性的膦酸酯取代的化合物,含有这些化合物的组合物,以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。
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公开(公告)号:US20080070910A1
公开(公告)日:2008-03-20
申请号:US11880743
申请日:2007-07-24
IPC分类号: C07D493/04 , A61K31/341 , A61K31/352 , A61K31/357 , A61K31/427 , A61K31/536 , C12N9/99 , A61P31/18 , C07D277/22 , C07D307/02 , C07D307/77 , C07D413/00
CPC分类号: C07D493/04
摘要: The present invention provides compounds of Formula (I): wherein A, X, Q, R2-R6, m, and W have the values described herein, as well as compositions comprising such compounds. The compounds are protease inhibitors and are useful for inhibiting the development of drug resistance in animals.
摘要翻译: 本发明提供式(I)的化合物:其中A,X,Q,R 2,R 6,M和W也具有本文所述的值 作为包含这些化合物的组合物。 这些化合物是蛋白酶抑制剂,可用于抑制动物耐药性的发展。
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