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公开(公告)号：US07544707B2
公开(公告)日：2009-06-09
申请号：US10596322
申请日：2004-12-16
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07D409/12 , C07D231/56
摘要： The present invention is directed to compounds represented by the following structural formula, Formula (I), and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) R2 is selected from the group consisting of C0-C8 alkyl and C1-4-heteroalkyl; (b) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (c) U is an aliphatic linker wherein one carbon atom of the aliphatic linker is optionally replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with from one to four substituents each independently selected from R30; (d) Y is selected from the group consisting of C, O, S, NH and a single bond; and (e) E is C(R3)(R4)A or A.
摘要翻译： 本发明涉及由下列结构式（I）表示的化合物及其立体异构体，药学上可接受的盐，溶剂化物和水合物，其中：（a）R 2选自C 0 -C 8烷基和C 1 -C 8烷基 -4-杂烷基; （b）X选自单键O，S，S（O）2和N; （c）U是脂族连接体，其中脂族连接体的一个碳原子任选被O，NH或S取代，并且其中这种脂族连接体任选地被1至4个独立地选自R 30的取代基取代; （d）Y选自C，O，S，NH和单键; 和（e）E是C（R3）（R4）A或A。
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公开(公告)号：US20100204207A1
公开(公告)日：2010-08-12
申请号：US12763344
申请日：2010-04-20
申请人： Xinchao Chen , Christopher Lawrence Cioffi , Sean Richard Dinn , Ana Maria Escribano , Maria Carmen Fernandez , Todd Fields , Robert Jason Herr , Nathan Bryan Mantlo , Eva Maria Martin De La Nava , Ana Isabel Mateo Herranz , Saravanan Parthasarathy , Xiaodong Wang
发明人： Xinchao Chen , Christopher Lawrence Cioffi , Sean Richard Dinn , Ana Maria Escribano , Maria Carmen Fernandez , Todd Fields , Robert Jason Herr , Nathan Bryan Mantlo , Eva Maria Martin De La Nava , Ana Isabel Mateo Herranz , Saravanan Parthasarathy , Xiaodong Wang
IPC分类号： A61K31/55 , C07D403/12 , C07D417/12 , C07D491/048 , C07D405/14 , C07D413/12 , C07D401/14 , A61P3/00 , A61P9/10
CPC分类号： C07D401/14 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D491/04
摘要： Compounds of Formula (I): wherein n, m, p, q, Y, R1, R2, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.
摘要翻译： 式（I）化合物：其中n，m，p，q，Y，R 1，R 2，R 3a，R 3b，R 4，R 5和R 6如本文所定义，并公开了其药物组合物和使用方法。
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公开(公告)号：US07749992B2
公开(公告)日：2010-07-06
申请号：US10574649
申请日：2004-10-07
申请人： Guoqing Cao , Ana Maria Escribano , Maria Carmen Fernandez , Todd Fields , Douglas Linn Gernert , Christopher Lawrence Cioffi , Robert Jason Herr , Nathan Bryan Mantlo , Eva Maria Martin De La Nava , Ana Isabel Mateo Herranz , Daniel Ray Mayhugh , Xiaodong Wang
发明人： Guoqing Cao , Ana Maria Escribano , Maria Carmen Fernandez , Todd Fields , Douglas Linn Gernert , Christopher Lawrence Cioffi , Robert Jason Herr , Nathan Bryan Mantlo , Eva Maria Martin De La Nava , Ana Isabel Mateo Herranz , Daniel Ray Mayhugh , Xiaodong Wang
IPC分类号： A61P3/06 , A61P9/10 , A61K31/55 , C07D223/14 , C07D223/16 , C07D223/32 , C07D225/06 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/04 , C07D491/04
CPC分类号： C07D223/16 , C07D223/14 , C07D223/32 , C07D225/06 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/04 , C07D491/04
摘要： Compounds of formula I wherein n, m, p, q, y, R1 R2, R3, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating artherosclerosis and its sequelae.
摘要翻译： 其中n，m，p，q，y，R 1，R 2，R 3，R 4，R 5和R 6如本文所定义的式I化合物，其药物组合物和使用方法被公开用于治疗动脉粥样硬化及其后遗症。
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4.发明授权Compounds, methods and formulations for the oral delivery of a glucagon-like peptide (Glp)-1 compound or a melanocortin-4 receptor (Mc4) agonist peptide 有权用于口服递送胰高血糖素样肽（Glp）-1化合物或黑皮质素-4受体（Mc4）激动剂肽的化合物，方法和制剂公开(公告)号：US08546581B2
公开(公告)日：2013-10-01
申请号：US13087255
申请日：2011-04-14
申请人： Louis Nickolaus Jungheim , John Mcneill McGill, III , Kenneth Jeff Thrasher , Robert Jason Herr , Muralikrishna Valluri
发明人： Louis Nickolaus Jungheim , John Mcneill McGill, III , Kenneth Jeff Thrasher , Robert Jason Herr , Muralikrishna Valluri
IPC分类号： C07D271/06 , C07D401/00 , C07D409/00
CPC分类号： C07D233/64 , A61K47/22 , C07D249/06 , C07D249/08 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/24 , C07D285/12 , C07D409/04 , C07D413/04
摘要： The present application relates to novel compounds, methods and formulations useful for the oral delivery of a glucagon like peptide-1 compound or a melanocortin 4 receptor agonist peptide.
摘要翻译： 本申请涉及可用于胰高血糖素样肽-1化合物或黑皮质素4受体激动剂肽的口服递送的新化合物，方法和制剂。
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5.发明授权Compounds, methods and formulations for the oral delivery of a glucagon-like peptide (GLP)-1 compound or a melanocortin-4 receptor (MC4) agonist peptide 有权胰高血糖素样肽（GLP）-1化合物或黑皮质素-4受体（MC4）激动剂肽的口服递送的化合物，方法和制剂公开(公告)号：US07947841B2
公开(公告)日：2011-05-24
申请号：US12263722
申请日：2008-11-03
申请人： Louis Nickolaus Jungheim , John McNeill McGill, III , Kenneth Jeff Thrasher , Robert Jason Herr , Valluri Muralikrishna
发明人： Louis Nickolaus Jungheim , John McNeill McGill, III , Kenneth Jeff Thrasher , Robert Jason Herr , Valluri Muralikrishna
IPC分类号： C07D263/34 , C07D213/00 , C07D409/00
CPC分类号： C07D233/64 , A61K47/22 , C07D249/06 , C07D249/08 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/24 , C07D285/12 , C07D409/04 , C07D413/04
摘要： The present application relates to novel compounds, methods and formulations useful for the oral delivery of a glucagon like peptide-1 compound or a melanocortin 4 receptor agonist peptide.
摘要翻译： 本申请涉及可用于胰高血糖素样肽-1化合物或黑皮质素4受体激动剂肽的口服递送的新化合物，方法和制剂。
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公开(公告)号：US20110312995A1
公开(公告)日：2011-12-22
申请号：US13145359
申请日：2010-01-21
申请人： Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Robert Jason Herr , Jason L. Davis , Kai Deng , Ming Min Hsia , Shuangyi Wan
发明人： Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Robert Jason Herr , Jason L. Davis , Kai Deng , Ming Min Hsia , Shuangyi Wan
IPC分类号： A61K31/4545 , C07D417/14 , C07D417/12 , A61K31/4709 , A61P3/00 , A61K31/4439 , A61P5/48 , A61P3/10 , A61P3/04 , A61P3/06 , C07D401/14 , A61K31/454
CPC分类号： C07D417/12 , C07D215/233 , C07D417/14
摘要： This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译： 本发明提供了一些式（I）的桥连和稠合杂环化合物或其药学上可接受的盐，酯溶剂合物或前药，其中：L是：（II），其它变量在本文中定义; 本发明化合物是G蛋白偶联受体40（GPR40，也称为游离脂肪酸受体FFAR）的激动剂。 本发明还涉及含有这些化合物的药物组合物，以及这些化合物在哺乳动物体内调节胰岛素水平的用途。 该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症，例如胰岛素抵抗，肥胖症和脂质疾病。
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公开(公告)号：US08232274B2
公开(公告)日：2012-07-31
申请号：US12046755
申请日：2008-03-12
申请人： Pauline C. Ting , Robert G. Aslanian , Jianhua Cao , David Won-Shik Kim , Rongze Kuang , Gang Zhou , Robert Jason Herr , Andrew John Zych , Jinhai Yang , Heping Wu , Nicolas Zorn
发明人： Pauline C. Ting , Robert G. Aslanian , Jianhua Cao , David Won-Shik Kim , Rongze Kuang , Gang Zhou , Robert Jason Herr , Andrew John Zych , Jinhai Yang , Heping Wu , Nicolas Zorn
IPC分类号： A61K31/501 , A61K31/5377 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D413/14 , A61P31/00
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D515/22
摘要： Disclosed is a set of compounds useful as glucan synthase inhibitors having the generic structure of Formula I: wherein the various moieties A, D, R6, etc., are as defined in the specification. These compounds are useful in treating or preventing fungal infections in a patient.
摘要翻译： 公开了一组可用作具有式I的通式结构的葡聚糖合酶抑制剂的化合物：其中各个部分A，D，R 6等如说明书中所定义。 这些化合物可用于治疗或预防患者的真菌感染。
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8.发明授权Compounds, methods and formulations for the oral delivery of a glucagon-like peptide (GLP)-1 compound or a melanocortin-4 receptor (MC4) agonist peptide 有权胰高血糖素样肽（GLP）-1化合物或黑皮质素-4受体（MC4）激动剂肽的口服递送的化合物，方法和制剂公开(公告)号：US07662771B2
公开(公告)日：2010-02-16
申请号：US10566342
申请日：2004-08-18
申请人： Robert Jason Herr , Louis Nickolaus Jungheim , John McNeill McGill, III , Kenneth Jeff Thrasher , Muralikrishna Valluri
发明人： Robert Jason Herr , Louis Nickolaus Jungheim , John McNeill McGill, III , Kenneth Jeff Thrasher , Muralikrishna Valluri
IPC分类号： A61K38/00 , A61K31/421 , C07D263/30
CPC分类号： C07D263/48 , A61K31/4164 , A61K38/22 , A61K38/26 , A61K47/22 , C07D233/64 , C07D249/06 , C07D249/08 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/24 , C07D285/12 , C07D409/04 , C07D413/04
摘要： The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide.
摘要翻译： 本发明涉及可用于口服递送GLP-1化合物或MC4激动剂肽的新化合物，方法和制剂。
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公开(公告)号：US20090170861A1
公开(公告)日：2009-07-02
申请号：US12046755
申请日：2008-03-12
申请人： Pauline C. Ting , Robert G. Aslanian , Jianhua Cao , David Won-Shik Kim , Rongze Kuang , Gang Zhou , Robert Jason Herr , Andrew John Zych , Jinhai Yang , Heping Wu , Nicolas Zorn
发明人： Pauline C. Ting , Robert G. Aslanian , Jianhua Cao , David Won-Shik Kim , Rongze Kuang , Gang Zhou , Robert Jason Herr , Andrew John Zych , Jinhai Yang , Heping Wu , Nicolas Zorn
IPC分类号： A61K31/501 , C07D403/04 , A01N43/58 , A01P3/00 , A61P31/10
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D515/22
摘要： In its many embodiments, the present invention provides -substituted pyridazinone compounds as glucan synthase inhibitors, methods of preparing such compounds, pharmaceutical including one or more of such compounds, methods of preparing pharmaceutical formulations including one or more such compounds or one or more such compounds along with other antifungal agents, and methods of treatment, prevention, inhibition, or amelioration of one or more fungal infections associated with glucan synthase using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了作为葡聚糖合酶抑制剂的取代的哒嗪酮化合物，制备这些化合物的方法，包括一种或多种这些化合物的药物，制备药物制剂的方法，包括一种或多种这样的化合物或一种或多种这样的化合物 以及其他抗真菌剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与葡聚糖合酶相关的一种或多种真菌感染的方法。
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公开(公告)号：US10472346B2
公开(公告)日：2019-11-12
申请号：US15522969
申请日：2015-10-30
申请人： The General Hospital Coporation , The Regents of the University of California , Steven L. Wagner , William C. Mobley , Rudolph E. Tanzi , Graham Johnson , Ronald Buckle , Nicholas Mayhew , Robert Jason Herr
发明人： Steven L. Wagner , William C. Mobley , Rudolph E. Tanzi , Graham Johnson , Ronald Buckle , Nicholas Mayhew , Robert Jason Herr , Kevin D. Rynearson
IPC分类号： C07D401/14 , C07D413/14 , C07D487/04 , A61P25/28
摘要： Provided herein are compounds and methods for treating a disorder associated with aberrant A3 peptide levels, including Alzheimer's disease. Provided herein are compositions and methods for treating a disorder associated with aberrant Aβ peptide levels, including AD. Provided herein are compounds of Formula (A) or a pharmaceutically acceptable salt thereof, wherein, L′ is selected from the group consisting of C(O), C(R1)(R2), substituted or unsubstituted —C2-6 alkylene-, and substituted or unsubstituted —C3-6 cycloalkylene.
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