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公开(公告)号:US20100120778A1
公开(公告)日:2010-05-13
申请号:US12614167
申请日:2009-11-06
申请人: Baihua Hu , Jay Edward Wrobel , James Winfield Jetter , David John O'Neill , Charles William Mann , Rayomand Jal Unwalla
发明人: Baihua Hu , Jay Edward Wrobel , James Winfield Jetter , David John O'Neill , Charles William Mann , Rayomand Jal Unwalla
IPC分类号: A61K31/498 , C07D241/36 , A61P1/16 , A61P9/10 , A61P9/00 , A61P3/04 , A61P3/06 , A61P25/28 , A61P3/10 , A61P29/00 , A61P19/04
CPC分类号: C07D241/44 , C07D241/42
摘要: Disclosed are quinoxaline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): wherein: each of L1 and L2 is, independently, a bond, —O— or —NH—; R2 is C6-C10 aryl or heteroaryl including 5-10 atoms, each of which is (i) substituted with 1 R9, and (ii) optionally further substituted with from 1-4 Re; and each of R4 and R5 is, independently (i) hydrogen; or (ii) halo; or (iii) C1-C6 alkyl or C1-C6 haloalkyl, each of which is optionally substituted with from 1-3 Ra; and R1, R3, R6, R9, Ra and Re are defined herein. In general, these compounds can be used for treating or preventing one or more diseases, disorders, conditions or symptoms mediated by LXRs.
摘要翻译: 公开了基于喹喔啉的肝脏X受体调节剂(LXR)和相关方法。 调节剂包括式(I)的化合物:其中:L1和L2各自独立地是键,-O-或-NH-; R 2是包括5-10个原子的C 6 -C 10芳基或杂芳基,其各自为(i)被1个R9取代,和(ii)任选地被1-4个Re取代; 并且R 4和R 5各自独立地是(i)氢; 或(ii)卤素; 或(iii)C 1 -C 6烷基或C 1 -C 6卤代烷基,其各自任选被1-3个R a取代; 并且R1,R3,R6,R9,Ra和Re在本文中定义。 通常,这些化合物可用于治疗或预防由LXR介导的一种或多种疾病,病症,病症或症状。
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公开(公告)号:US20100184786A1
公开(公告)日:2010-07-22
申请号:US12622058
申请日:2009-11-19
申请人: Jeremy Mark Travins , Ronald Charles Bernotas , Jay Edward Wrobel , David Harry Kaufman , Baihua Hu , James Winfield Jetter , David John O'Neill , Charles William Mann
发明人: Jeremy Mark Travins , Ronald Charles Bernotas , Jay Edward Wrobel , David Harry Kaufman , Baihua Hu , James Winfield Jetter , David John O'Neill , Charles William Mann
IPC分类号: A61K31/517 , C07D239/74 , A61P9/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P29/00 , A61Q19/08 , A61K8/49
CPC分类号: C07D239/72
摘要: Disclosed are polar quinazoline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): in which, R1, R2, R3, R4, R5, R6, R22, R23, R24, R25, R26, R27, R28, R29, W, W1, W2, Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, Ri, Rj, Rm, Rn, Ro, Rp, Rq, Rr, Rs, Rt, Ru, and n can be as defined anywhere herein. In general, these compounds can be used for treating or preventing one or more diseases, disorders, conditions or symptoms mediated by LXRs.
摘要翻译: 公开了基于极性喹唑啉的肝脏X受体调节剂(LXR)及相关方法。 调节剂包括式(I)化合物:其中R1,R2,R3,R4,R5,R6,R22,R23,R24,R25,R26,R27,R28,R29,W,W1,W2,Ra,Rb ,Rc,Rd,Re,Rf,Rg,Rh,Ri,Rj,Rm,Rn,Ro,Rp,Rq,Rr,Rs,Rt,Ru和n可以如本文任何地方所定义。 通常,这些化合物可用于治疗或预防由LXR介导的一种或多种疾病,病症,病症或症状。
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公开(公告)号:US20090069373A1
公开(公告)日:2009-03-12
申请号:US12039347
申请日:2008-02-28
申请人: Jay E. Wrobel , Baihua Hu , Michael David Collini , James Winfield Jetter , Ronald Charles Bernotas , David Harry Kaufman , Robert Ray Singhaus, JR. , John William Ullrich , Robert Lester Morris , Rayomand J. Unwalla
发明人: Jay E. Wrobel , Baihua Hu , Michael David Collini , James Winfield Jetter , Ronald Charles Bernotas , David Harry Kaufman , Robert Ray Singhaus, JR. , John William Ullrich , Robert Lester Morris , Rayomand J. Unwalla
IPC分类号: A61K31/47 , C07D215/12 , C07D401/02 , A61P9/00 , A61P25/28 , A61K31/4709 , A61P3/00 , A61P29/00 , A61P17/00
CPC分类号: C07D215/14 , C07D215/12 , C07D401/04 , C07D401/12 , C07D409/04 , C07D409/12
摘要: This invention relates generally to quinoline-based modulators of Liver X receptors (LXRs) and related methods.
摘要翻译: 本发明一般涉及基于喹啉的肝X受体调节剂(LXR)和相关方法。
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公开(公告)号:US07268159B2
公开(公告)日:2007-09-11
申请号:US10947726
申请日:2004-09-23
申请人: Baihua Hu , James Winfield Jetter
发明人: Baihua Hu , James Winfield Jetter
IPC分类号: A61K31/404 , C07D209/04
CPC分类号: C07D209/42 , C07D209/08 , C07D403/10 , C07D409/04
摘要: The present invention relates generally to substituted indoles and methods of using them.
摘要翻译: 本发明一般涉及取代的吲哚及其使用方法。
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公开(公告)号:US20080319046A1
公开(公告)日:2008-12-25
申请号:US12200164
申请日:2008-08-28
申请人: Baihua Hu
发明人: Baihua Hu
IPC分类号: A61K31/405 , C07D209/42 , A61P3/10
CPC分类号: C07D209/42 , C07D403/04
摘要: The present invention relates generally to substituted sulfonamide indoles such as substituted sulfonamide indoles, and methods of using them.
摘要翻译: 本发明一般涉及取代磺酰胺吲哚如取代磺酰胺吲哚,以及使用它们的方法。
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公开(公告)号:US07285682B2
公开(公告)日:2007-10-23
申请号:US11352887
申请日:2006-02-13
申请人: Baihua Hu
发明人: Baihua Hu
IPC分类号: C07C279/10 , A61K31/155
CPC分类号: C07C279/22 , C07C279/24
摘要: The present invention provides terphenyl guanidine compounds of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
摘要翻译: 本发明提供式I的三联苯胍化合物本发明还提供了用于抑制β-分泌酶(BACE)和治疗β-淀粉样沉积物和神经原纤维缠结的方法。
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公开(公告)号:US07022716B2
公开(公告)日:2006-04-04
申请号:US10330576
申请日:2002-12-27
申请人: Baihua Hu , Fuk-Wah Sum , Michael Sotirios Malamas
发明人: Baihua Hu , Fuk-Wah Sum , Michael Sotirios Malamas
IPC分类号: A61K31/4468 , C07D213/72
CPC分类号: C07D401/10 , C07D211/58 , C07D223/12 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/10 , C07D417/14
摘要: This invention provides compounds of Formula I having the structure wherein, R1, R2, R3, R4, R5, T, T1, T2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.
摘要翻译: 本发明提供具有以下结构的式I化合物:其中R 1,R 2,R 3,R 4, >,R 5,T,T 1,T 2和X如上所定义,或其药学上可接受的盐,它们是 可用于治疗或抑制与胰岛素抵抗或高血糖相关的代谢紊乱(通常与肥胖或葡萄糖不耐受相关),动脉粥样硬化,胃肠道疾病,神经源性炎症,青光眼,高眼压症和尿频; 并且特别可用于治疗或抑制II型糖尿病。
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公开(公告)号:US20050131014A1
公开(公告)日:2005-06-16
申请号:US11010236
申请日:2004-12-10
申请人: Michael Collini , Robert Singhaus , Baihua Hu , James Jetter , Robert Morris , David Kaufman , Christopher Miller , John Ullrich , Rayomand Unwalla , Jay Wrobel , Elaine Quinet , Ponnal Nambi , Ronald Bernotas , Merle Elloso
发明人: Michael Collini , Robert Singhaus , Baihua Hu , James Jetter , Robert Morris , David Kaufman , Christopher Miller , John Ullrich , Rayomand Unwalla , Jay Wrobel , Elaine Quinet , Ponnal Nambi , Ronald Bernotas , Merle Elloso
IPC分类号: A61K31/47 , A61K31/4709 , C07D215/14 , C07D215/54 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/04 , C07D413/06 , C07D417/12 , C07D41/02
CPC分类号: C07D401/04 , C07D215/14 , C07D215/54 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/04 , C07D413/06 , C07D417/12
摘要: This invention provides compounds of formula I that are useful in the treatment or inhibition of LXR mediated diseases.
摘要翻译: 本发明提供可用于治疗或抑制LXR介导的疾病的式I化合物。
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公开(公告)号:US20050096377A1
公开(公告)日:2005-05-05
申请号:US10947839
申请日:2004-09-23
申请人: Baihua Hu
发明人: Baihua Hu
IPC分类号: A61P3/10 , A61P7/02 , A61P9/10 , A61P25/28 , C07D209/42 , C07D401/12 , C07D403/04 , C07D43/02 , A61K31/405
CPC分类号: C07D209/42 , C07D403/04
摘要: The present invention relates generally to substituted sulfonamide indoles such as substituted sulfonamide indoles, and methods of using them.
摘要翻译: 本发明一般涉及取代磺酰胺吲哚如取代磺酰胺吲哚,以及使用它们的方法。
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公开(公告)号:US07700595B2
公开(公告)日:2010-04-20
申请号:US11365750
申请日:2006-03-01
IPC分类号: C07D237/28 , C07D413/12 , A61K31/502 , A61K31/5355 , A61P9/10 , A61P3/10 , A61P25/28
CPC分类号: C07D413/12 , C07D237/28 , C07D403/12 , C07D409/12
摘要: This invention relates generally to cinnoline-based modulators of Liver X receptors (LXRs) and related methods.
摘要翻译: 本发明一般涉及基于噌啉的肝X受体调节剂(LXR)及相关方法。
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