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公开(公告)号:US20110237566A1
公开(公告)日:2011-09-29
申请号:US13130144
申请日:2009-11-24
IPC分类号: A61K31/553 , C07D313/00 , C07D413/14 , C07D405/14 , C07D267/10 , C07D243/08 , A61K31/336 , A61K31/5355 , A61K31/497 , A61K31/4523 , A61K31/551 , A61P35/00
CPC分类号: C07D407/06 , C07D403/14 , C07D405/14 , C07D413/14
摘要: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain macrolide compounds (for convenience, collectively referred to herein as “MC compounds”), which, inter alia, are useful in treatment of cancer. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to treat proliferative conditions such as cancer, and in the treatment of diseases and conditions that are mediated by the regulation (e.g. inhibition) of cell proliferation, optionally in combination with another agent.
摘要翻译: 本发明一般涉及治疗化合物的领域,更具体地涉及某些大环内酯类化合物(为方便起见,本文统称为“MC化合物”),其尤其可用于治疗癌症。 本发明还涉及包含这些化合物的药物组合物,以及这些化合物和组合物在体外和体内的用途,以治疗增殖性疾病如癌症,以及治疗由调节介导的疾病和病症 (例如抑制)细胞增殖,任选与另一种试剂组合。
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公开(公告)号:US08921309B2
公开(公告)日:2014-12-30
申请号:US13128661
申请日:2009-11-24
摘要: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain lipopeptide compounds comprising a cyclic peptide bearing a lipid side chain (for convenience, collectively referred to herein as “LP compounds”), which, inter alia, are antimicrobial, particularly antibacterial. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to provide an antimicrobial function, particularly an antibacterial function, and in the treatment of diseases and conditions that are mediated by microbes, particularly bacteria, that are ameliorated by the antimicrobial function, particularly an antibacterial function, including bacterial diseases, optionally in combination with another agent, for example, another antibacterial agent.
摘要翻译: 本发明一般涉及治疗化合物领域,更具体地涉及包含带有脂质侧链的环状肽(为方便起见,统称为“LP化合物”)的某些脂肽化合物,其特别是抗微生物剂 ,特别是抗菌。 本发明还涉及包含这种化合物的药物组合物,以及这些化合物和组合物在体外和体内的用途,以提供抗微生物功能,特别是抗菌功能,以及用于治疗介导的疾病和病症 特别是通过抗微生物功能改善的微生物,特别是细菌,特别是抗菌功能,包括细菌疾病,任选地与另一种试剂,例如另一种抗菌剂组合。
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公开(公告)号:US20110224129A1
公开(公告)日:2011-09-15
申请号:US13128661
申请日:2009-11-24
摘要: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain lipopeptide compounds comprising a cyclic peptide bearing a lipid side chain (for convenience, collectively referred to herein as “LP compounds”), which, inter alia, are antimicrobial, particularly antibacterial. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to provide an antimicrobial function, particularly an antibacterial function, and in the treatment of diseases and conditions that are mediated by microbes, particularly bacteria, that are ameliorated by the antimicrobial function, particularly an antibacterial function, including bacterial diseases, optionally in combination with another agent, for example, another antibacterial agent.
摘要翻译: 本发明一般涉及治疗化合物领域,更具体地涉及包含带有脂质侧链的环状肽(为方便起见,统称为“LP化合物”)的某些脂肽化合物,其特别是抗微生物剂 ,特别是抗菌。 本发明还涉及包含这种化合物的药物组合物,以及这些化合物和组合物在体外和体内的用途,以提供抗微生物功能,特别是抗菌功能,以及用于治疗介导的疾病和病症 特别是通过抗微生物功能改善的微生物,特别是细菌,特别是抗菌功能,包括细菌疾病,任选地与另一种试剂,例如另一种抗菌剂组合。
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公开(公告)号:US07037918B2
公开(公告)日:2006-05-02
申请号:US10309535
申请日:2002-12-03
申请人: John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
发明人: John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
IPC分类号: A61K31/505 , A61K31/535 , A61K31/47 , A61K31/475 , A61K31/52
CPC分类号: C07D213/74 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12
摘要: New pyrimidine or pyridine 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 in the treatment of 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.
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公开(公告)号:US06489344B1
公开(公告)日:2002-12-03
申请号:US09336098
申请日:1999-06-18
申请人: John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
发明人: John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
IPC分类号: C07D40104
CPC分类号: C07D213/74 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12
摘要: New pyrimidine or pyridine 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 in the treatment of 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: 提供了新的嘧啶或吡啶类化合物,体外抑制糖原合成酶激酶(GSK3)活性和体内GSK3介导的病症治疗的组合物和方法。 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,例如治疗糖尿病,阿尔茨海默病和其他神经变性疾病,肥胖症,动脉粥样硬化 心血管疾病,原发性高血压,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: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:US20080317744A1
公开(公告)日:2008-12-25
申请号:US11665956
申请日:2005-10-14
申请人: Rustum S. Boyce , Yi Xia , Hongyan Guo , Kris G. Mendenhall , Annette O. Walter , Weibo Wang
发明人: Rustum S. Boyce , Yi Xia , Hongyan Guo , Kris G. Mendenhall , Annette O. Walter , Weibo Wang
IPC分类号: C07D401/12 , C07D209/14 , C07D403/12 , C07D235/04 , A61K31/4184 , A61K31/404 , A61K35/00 , A61K39/395
CPC分类号: C07D403/12 , C07D209/14 , C07D235/14 , C07D401/12 , C07D403/04 , C07D403/14
摘要: The present invention relates to new indole and benzimidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula:
摘要翻译: 本发明涉及新的吲哚和苯并咪唑化合物及其药学上可接受的盐,酯或前药,新化合物的组合物和药学上可接受的载体,以及新化合物的用途。 本发明的化合物具有以下通式:
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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:US08735599B2
公开(公告)日:2014-05-27
申请号:US13613977
申请日:2012-09-13
申请人: Weibo Wang , Paul A. Barsanti , Xia Yia , Rustum S. Boyce , Sabina Pecchi , Nathan Brammeier , Megan C. Phillips , Kris Mendenhall , Kelly Wayman , Liana Marie Lagnition , Ryan N. Constantine , Hong Yang , Elizabeth Mieuli , Savithri Ramurthy , Elisa Jazan , Anu Sharma , Rama Jain , Sharadha Subramanian , Paul A. Renhowe , Kenneth W. Bair , David Duhl , Annette Walter , Tinya Abrams , Kay Huh , Eric Martin , Mark Knapp , Vincent P. Le
发明人: Weibo Wang , Paul A. Barsanti , Xia Yia , Rustum S. Boyce , Sabina Pecchi , Nathan Brammeier , Megan C. Phillips , Kris Mendenhall , Kelly Wayman , Liana Marie Lagnition , Ryan N. Constantine , Hong Yang , Elizabeth Mieuli , Savithri Ramurthy , Elisa Jazan , Anu Sharma , Rama Jain , Sharadha Subramanian , Paul A. Renhowe , Kenneth W. Bair , David Duhl , Annette Walter , Tinya Abrams , Kay Huh , Eric Martin , Mark Knapp , Vincent P. Le
IPC分类号: A61K31/4174 , C07D233/00 , C07D233/54
CPC分类号: C07D233/54 , C07D233/24 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/10
摘要: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula:
摘要翻译: 本发明涉及新的取代的咪唑化合物及其药学上可接受的盐,酯或前药,新化合物的组合物和药学上可接受的载体,以及新化合物的用途。 本发明的化合物具有以下通式:
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公开(公告)号:US07608723B2
公开(公告)日:2009-10-27
申请号:US11251440
申请日:2005-10-14
申请人: Rustum S. Boyce , Yi Xia , Hongyan Guo , Kris G. Mendenhull , Annette O. Walter , Weibo Wang
发明人: Rustum S. Boyce , Yi Xia , Hongyan Guo , Kris G. Mendenhull , Annette O. Walter , Weibo Wang
IPC分类号: C07D209/10 , C07D235/14 , A61K31/33
CPC分类号: C07D403/12 , C07D209/14 , C07D235/14 , C07D401/12 , C07D403/04 , C07D403/14
摘要: The present invention relates to new indole and benzimidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula:
摘要翻译: 本发明涉及新的吲哚和苯并咪唑化合物及其药学上可接受的盐,酯或前药,新化合物的组合物和药学上可接受的载体,以及新化合物的用途。 本发明的化合物具有以下通式:
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