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公开(公告)号:US06995269B2
公开(公告)日:2006-02-07
申请号:US10379397
申请日:2003-03-04
申请人: Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , David Duhl
发明人: Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , David Duhl
IPC分类号: C07D211/72 , C07D295/20 , A61K31/44
CPC分类号: C07D233/64 , C07B2200/07 , C07B2200/09 , C07C279/18 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D209/16 , C07D215/12 , C07D241/08 , C07D241/42 , C07D295/215 , C07D307/24 , C07D309/14 , C07D333/20 , C07D487/04 , C07D487/08
摘要: Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.
摘要翻译: 式IIA和IIB的化合物是新的胍化合物,化学式id =“CHEM-US-00001”num =“000
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公开(公告)号:US06638927B2
公开(公告)日:2003-10-28
申请号:US09945384
申请日:2001-08-31
申请人: Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , Zhi-Jie Ni , David Duhl , Effie Tozzo , Kirk Johnson , David C. Myles
发明人: Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , Zhi-Jie Ni , David Duhl , Effie Tozzo , Kirk Johnson , David C. Myles
IPC分类号: C07D29520
CPC分类号: C07D233/64 , C07B2200/07 , C07B2200/09 , C07C279/18 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D209/16 , C07D215/12 , C07D241/08 , C07D241/42 , C07D295/215 , C07D307/24 , C07D309/14 , C07D333/20 , C07D487/04 , C07D487/08
摘要: Compounds of formula IA and IB are new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.
摘要翻译: 式IA和IB的化合物是新的,其中变量R 1至R 10具有本文所述的值。 这些化合物可用于治疗诸如肥胖症和II型糖尿病的疾病,并且可以作为药物制剂与药学上可接受的载体一起提供。
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公开(公告)号:US06716840B2
公开(公告)日:2004-04-06
申请号:US10118730
申请日:2002-04-08
申请人: Daniel Chu , Rustum S. Boyce , David Duhl , Bryan H. Chang
发明人: Daniel Chu , Rustum S. Boyce , David Duhl , Bryan H. Chang
IPC分类号: A61K315375
CPC分类号: C07D209/46 , C07D209/48 , C07D217/24 , C07D235/08 , C07D235/10
摘要: Compounds having the general structure I are provided: X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of and L is selected from the group consisting of N, O, S, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r”) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
摘要翻译: 提供具有通式结构I的化合物:X和Y独立地选自CH 2,N,NR 9,C = O,C = S,S = O,SO 2,S,O, (R 6 R 7)n,C(= O) - (CR 6 R 7)n和C(= S) - (CR 6 R 7)n,其中n为1 W选自N,O,S,S = O,SO 2,C(O),NC(O),NC(S),OC (O),OC(S),C(NR 10),C(NOR 10))和共价键。 Z 1,Z 2和Z 3独立地选自取代的碳和氮。 式I化合物是黑皮质素-4受体(“MC-4r”)的激动剂,因此可能具有控制人类MC-4r作用相关疾病如肥胖和II型糖尿病的有用性质。
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公开(公告)号:US07034033B2
公开(公告)日:2006-04-25
申请号:US10444495
申请日:2003-05-23
申请人: Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
发明人: Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
IPC分类号: C07D239/90 , A61K31/517 , A61P3/04 , A61P3/10
CPC分类号: C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
摘要: A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.
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公开(公告)号:US07858631B2
公开(公告)日:2010-12-28
申请号:US10515434
申请日:2003-05-23
申请人: Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
发明人: Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
IPC分类号: A61K31/519
CPC分类号: C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
摘要: A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure of Formulas (IA), (IB), or (IC): where the values of the variable are defined herein.
摘要翻译: 提供了能够作为MC4-R激动剂的各种低分子量含胍基分子。 该化合物可用于治疗MC4-R介导的疾病。 化合物具有式(IA),(IB)或(IC)的结构:其中变量的值在本文中定义。
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公开(公告)号:US20100105654A1
公开(公告)日:2010-04-29
申请号:US12605174
申请日:2009-10-23
申请人: Rustum S. BOYCE , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher R. Conlee , Brian D. Thompson , Judith de Armas Kuntz , David L. Musso , Kevin K. Barvian , Stephen A. Thomson , William R. Swain , Kien S. Du , Brian A. Chauder , Jason D. Speake , Michael J. Bishop
发明人: Rustum S. BOYCE , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher R. Conlee , Brian D. Thompson , Judith de Armas Kuntz , David L. Musso , Kevin K. Barvian , Stephen A. Thomson , William R. Swain , Kien S. Du , Brian A. Chauder , Jason D. Speake , Michael J. Bishop
IPC分类号: A61K31/517 , C07D403/12 , C07D239/86 , C07D403/14 , C07D413/14 , C07D417/14 , A61K31/5377 , A61P3/04 , A61P3/10
CPC分类号: C07D217/24 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要: A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structures VA, VB, VIIA and VIIB where the values of the variables are defined herein.
摘要翻译: 提供了能够作为MC4-R激动剂的各种小分子,含胍分子。 当给予受试者时,这些化合物可用于治疗MC4-R介导的疾病。 化合物具有结构VA,VB,VIIA和VIIB,其中变量的值在本文中定义。
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公开(公告)号:US07858641B2
公开(公告)日:2010-12-28
申请号:US11248040
申请日:2005-10-11
申请人: Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
发明人: Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
IPC分类号: A61K31/47
CPC分类号: C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
摘要: A variety of low molecular weight, guanidino-containing dihydroisoquinolinoines capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure ID where the values of the variable are defined herein.
摘要翻译: 提供了能够作为MC4-R激动剂的各种低分子量含胍基的二氢异喹啉基。 该化合物可用于治疗MC4-R介导的疾病。 化合物具有其中在此定义变量的值的结构ID。
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公开(公告)号:US07625909B2
公开(公告)日:2009-12-01
申请号:US10850967
申请日:2004-05-21
申请人: Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher R. Conlee , Brian D. Thompson , Judith de Armas Kuntz , David L. Musso , Kevin K. Barvian , Stephen A. Thomson , William R. Swain , Kien S. Du , Brian A. Chauder , Jason D. Speake , Michael J. Bishop
发明人: Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher R. Conlee , Brian D. Thompson , Judith de Armas Kuntz , David L. Musso , Kevin K. Barvian , Stephen A. Thomson , William R. Swain , Kien S. Du , Brian A. Chauder , Jason D. Speake , Michael J. Bishop
IPC分类号: A61K31/517 , A61K31/519 , A61P5/50 , C07D239/88 , C07D239/95 , C07D471/04 , C07D487/04
CPC分类号: C07D217/24 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要: A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structure IA, IB, and IC where the values of the variables are defined herein.
摘要翻译: 提供了能够作为MC4-R激动剂的各种小分子,含胍分子。 当给予受试者时,这些化合物可用于治疗MC4-R介导的疾病。 化合物具有结构IA,IB和IC,其中变量的值在本文中定义。
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公开(公告)号:US07456183B2
公开(公告)日:2008-11-25
申请号:US10474331
申请日:2002-04-08
申请人: Daniel Chu , Rustum Boyce , David Duhl , Bryan Chang
发明人: Daniel Chu , Rustum Boyce , David Duhl , Bryan Chang
IPC分类号: A61K31/47 , A61K31/425 , A61K31/415 , A61K31/40 , A61P7/00 , C07D209/02 , C07D209/44 , C07D209/46 , C07D209/48 , C07D217/22 , C07D235/24 , C07D235/28 , C07D277/62 , C07D403/02
CPC分类号: C07D209/46 , C07D209/48 , C07D217/24 , C07D235/08 , C07D235/10
摘要: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
摘要翻译: 提供具有一般结构I的化合物。 X和Y独立地选自CH 2,N,NR 9,CO,CS,SO,SO 2,S ,(O) - (CR 6),(O) - (CR 6) C(-S) - (CR 6 R 7)N O>,和C(-S) - (CR 6) 其中n为1,2或3.W选自(式I),L选自N,O,SO,SO 2, C(O),NC(O),NC(S),OC(O),OC(S),C(NR 10) ,和共价键。 Z 1,Z 2,Z 3和Z 3独立地选自取代的碳和氮。 式I化合物是黑皮质素-4受体(“MC-4r2”)的激动剂,因此可能具有控制人类MC-4r作用相关疾病如肥胖和II型糖尿病的有用性质。
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公开(公告)号:US08765945B2
公开(公告)日:2014-07-01
申请号:US13023140
申请日:2011-02-08
申请人: Bing Wang , Daniel Chu , Yongbo Liu , Quan Jiang , Lei Lu
发明人: Bing Wang , Daniel Chu , Yongbo Liu , Quan Jiang , Lei Lu
IPC分类号: C07D237/36
CPC分类号: C07D405/06 , C07D249/08 , C07D401/04 , C07D403/06 , C07D471/06
摘要: Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.
摘要翻译: 本文提供了合成二氢吡啶并二氮杂萘酮衍生物的方法,例如5-氟-8-(4-氟苯基)-9-(1-甲基-1H-1,2,4-三唑-5-基) 9-二氢-2H-吡啶并[4,3,2-de]酞嗪-3(7H) - 酮及其立体异构体,它们是有效的聚(ADP-核糖)聚合酶(PARP)抑制剂以及新的合成中间体化合物。
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