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公开(公告)号:US20090105124A1
公开(公告)日:2009-04-23
申请号:US12193579
申请日:2008-08-18
申请人: Nicholas D. Smith , Joseph E. Payne , Timothy Z. Hoffman , Celine Bonnefous , Anothony B. Pinkerton , Dana L. Siegel
发明人: Nicholas D. Smith , Joseph E. Payne , Timothy Z. Hoffman , Celine Bonnefous , Anothony B. Pinkerton , Dana L. Siegel
IPC分类号: A61K38/28 , C07D475/02 , C07D471/04 , A61P3/10 , A61P19/02 , A61P3/00 , A61P29/00 , A61K31/4985 , A61K31/5025
CPC分类号: C07D471/04 , C07D487/04 , C07D495/04
摘要: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulation of TGR5 activity in a human or animal subject are also provided for the treatment diseases mediated by TGR5.
摘要翻译: 本文公开了新的杂环化合物和组合物及其作为用于治疗疾病的药物的应用。 人类或动物受试者中TGR5活性的调节方法也用于由TGR5介导的治疗疾病。
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2.
公开(公告)号:US20080139558A1
公开(公告)日:2008-06-12
申请号:US11678572
申请日:2007-02-23
申请人: Nicholas D. Smith , Jeffrey R. Roppe , Celine Bonnefous , Joseph E. Payne , Hui Zhuang , Xiaohong Chen , Andrew K. Lindstrom , Sergio G. Duron , Christian A. Hassig , Stewart A. Noble
发明人: Nicholas D. Smith , Jeffrey R. Roppe , Celine Bonnefous , Joseph E. Payne , Hui Zhuang , Xiaohong Chen , Andrew K. Lindstrom , Sergio G. Duron , Christian A. Hassig , Stewart A. Noble
IPC分类号: A61K31/47 , A61K31/5377 , A61P11/06 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/14 , A61P29/02 , A61P3/10 , A61P31/00 , A61P31/12 , A61P31/22 , A61P37/00 , A61P37/08 , A61P9/10 , C07D215/227 , C07D295/00 , C07D471/04
CPC分类号: C07D405/12 , A61K31/4704 , A61K31/4709 , C07D215/227 , C07D401/06 , C07D401/12 , C07D409/12
摘要: The present invention relates to novel quinolones of Formula I that inhibit inducible NOS synthase together with methods of synthesizing and using the compounds including methods for inhibiting or modulating nitric oxide synthesis and/or lowering nitric oxide levels in a patient by administering the compounds for the treatment of disease.
摘要翻译: 本发明涉及抑制诱导型NOS合酶的新型喹诺酮,以及通过给予治疗化合物来合成和使用包括抑制或调节一氧化氮合成和/或降低一氧化氮水平的方法的化合物的方法 的疾病
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公开(公告)号:US20110230526A1
公开(公告)日:2011-09-22
申请号:US13016304
申请日:2011-01-28
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: A61K31/4439 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/28
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于它们在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
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4.
公开(公告)号:US20080132488A1
公开(公告)日:2008-06-05
申请号:US11667814
申请日:2005-11-10
IPC分类号: A61K31/215 , C07C69/02 , A61K31/216 , A61K31/165 , A61P25/00 , A61K31/551 , C07D401/02
CPC分类号: C07C69/24 , C07C53/128 , C07C257/14 , C07C317/46 , C07D217/02 , C07D311/80
摘要: Disclosed are prodrugs of (2R)—2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.
摘要翻译: 公开了(2R)-2-丙基辛酸的前药和包含它们的药物组合物,其可有效调节中风生化级联中的多个事件。 还公开了通过施用本发明的化合物或组合物来治疗患有中风或有卒中风险的患者的方法。
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5.
公开(公告)号:US20120289696A1
公开(公告)日:2012-11-15
申请号:US13558537
申请日:2012-07-26
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: C07D417/06 , C07D417/14 , C07D471/04
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
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公开(公告)号:US07879882B2
公开(公告)日:2011-02-01
申请号:US11664902
申请日:2005-10-06
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: A61P25/00 , A61K31/44 , C07D417/14
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于它们在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
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公开(公告)号:US08609852B2
公开(公告)日:2013-12-17
申请号:US13558537
申请日:2012-07-26
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: A61P25/00 , A61K31/55 , A61K31/54 , A61K31/505 , A61K31/44 , A61K31/47 , A61K31/445 , C07D401/00 , C07D403/00 , C07D417/00 , C07D239/02 , C07D211/00
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
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8.
公开(公告)号:US07495029B2
公开(公告)日:2009-02-24
申请号:US11667814
申请日:2005-11-10
IPC分类号: A61K31/235 , C07J71/00 , C07D311/80 , C07C381/00 , C07C69/02
CPC分类号: C07C69/24 , C07C53/128 , C07C257/14 , C07C317/46 , C07D217/02 , C07D311/80
摘要: Disclosed are prodrugs of (2R)-2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.
摘要翻译: 公开了(2R)-2-丙基辛酸的前药和包含它们的药物组合物,其可有效调节中风生化级联中的多个事件。 还公开了通过施用本发明的化合物或组合物来治疗患有中风或有卒中风险的患者的方法。
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9.
公开(公告)号:US09393315B2
公开(公告)日:2016-07-19
申请号:US13492424
申请日:2012-06-08
申请人: Yoshiro Niitsu , Joseph E. Payne , John A. Gaudette , Zheng Hou , Victor Knopov , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Yasunobu Tanaka , Violetta Akopian
发明人: Yoshiro Niitsu , Joseph E. Payne , John A. Gaudette , Zheng Hou , Victor Knopov , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Yasunobu Tanaka , Violetta Akopian
IPC分类号: A61K9/127 , C07C235/30 , A61K31/166 , A61K31/23 , A61P1/16 , A61P1/18 , A61P11/04 , C07F9/10 , A61K31/685 , A61K31/713 , C07C229/32 , C07C235/48 , A61K47/48 , C07C237/22 , C07C235/08
CPC分类号: C07C237/22 , A61K9/127 , A61K9/1271 , A61K31/07 , A61K31/713 , A61K47/551 , C07C233/21 , C07C235/08 , C07C235/48 , C07C2601/16 , C07F9/10 , C12N15/113 , C12N2310/14 , C12N2320/32 , Y10S977/773 , Y10S977/906 , Y10S977/907
摘要: Here described are compounds consisting of the structure (targeting molecule)m-linker-(targeting molecule)n, wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including these compounds which are useful for the targeting and delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.
摘要翻译: 这里描述的是由结构(靶向分子)m-连接体(靶向分子)n组成的化合物,其中靶向分子是靶细胞上具有特异性受体的类视黄醇或脂溶性维生素; 其中m和n独立地为0,1,2或3; 并且其中所述接头包含聚乙二醇(PEG)或PEG样分子,以及包含这些化合物的组合物和药物制剂,其可用于治疗剂的靶向和递送; 以及使用这些组合物和药物制剂的方法。
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公开(公告)号:US09011903B2
公开(公告)日:2015-04-21
申请号:US13492650
申请日:2012-06-08
申请人: Yoshiro Niitsu , Victor Knopov , Joseph E. Payne , Zheng Hou , John A. Gaudette , Violetta Akopian , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Yasunobu Tanaka , Priya Karmali , Sridhar C. Nagarajan
发明人: Yoshiro Niitsu , Victor Knopov , Joseph E. Payne , Zheng Hou , John A. Gaudette , Violetta Akopian , Richard P. Witte , Mohammad Ahmadian , Loren A. Perelman , Yasunobu Tanaka , Priya Karmali , Sridhar C. Nagarajan
IPC分类号: A61K31/225 , C07C69/34 , A61K9/127 , A61K31/7052 , A61K47/18 , A61K9/00 , A61K9/10 , A61K31/713 , C12N15/113
CPC分类号: C07C237/08 , A61K9/0019 , A61K9/10 , A61K9/1271 , A61K31/713 , A61K47/186 , A61K47/543 , C07C323/60 , C07C333/04 , C12N15/113
摘要: Here described are compounds of formula I: wherein R1 and R2 is independently selected from a group consisting of C10 to C18 alkyl, C12 to C18 alkenyl, and oleyl group; wherein R3 and R4 are independently selected from a group consisting of C1 to C6 alkyl, and C2 to C6 alkanol; wherein X is selected from a group consisting of —CH2—, —S—, and —O— or absent; wherein Y is selected from —(CH2)n, —S(CH2)n, —O(CH2)n—, thiophene, —SO2(CH2)n—, and ester, wherein n=1-4; wherein a=1-4; wherein b=1-4; wherein c=1-4; and wherein Z is a counterion; as well as compositions and pharmaceutical formulations including compounds of formula I which are useful for the delivery of therapeutic agents; and methods of using these compositions and formulations.
摘要翻译: 这里描述的是式I化合物:其中R 1和R 2独立地选自C 10至C 18烷基,C 12至C 18烯基和油基; 其中R3和R4独立地选自C1-C6烷基和C2-C6链烷醇; 其中X选自-CH 2 - , - S-和-O-或不存在; 其中Y选自 - (CH 2)n,-S(CH 2)n,-O(CH 2)n - ,噻吩,-SO 2(CH 2)n - 和酯,其中n = 1-4; 其中a = 1-4; 其中b = 1-4; 其中c = 1-4; 并且其中Z是抗衡离子; 以及包含可用于递送治疗剂的式I化合物的组合物和药物制剂; 以及使用这些组合物和制剂的方法。
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