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1. 发明申请

US20140288081A1 THERAPEUTIC COMPOUNDS AND COMPOSITIONS 有权
标题翻译：治疗化合物和组合物
公开(公告)号：US20140288081A1
公开(公告)日：2014-09-25
申请号：US14210583
申请日：2014-03-14
申请人： Giovanni Cianchetta , Janeta Popovici-Muller , Robert Zahler , Sheldon Cao , Xiaolei Wang , Zhixiong Ye
发明人： Giovanni Cianchetta , Janeta Popovici-Muller , Robert Zahler , Sheldon Cao , Xiaolei Wang , Zhixiong Ye
IPC分类号： C07D211/52 , C07D401/14 , C07D417/14 , C07D413/12 , C07D211/48 , C07D405/12 , C07D401/12 , C07D417/12
CPC分类号： C07D401/12 , C07D211/48 , C07D211/52 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D513/04 , C07F9/65583
摘要： Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
摘要翻译：本文描述了通式I的化合物和包含调节丙酮酸激酶的通式I化合物的组合物。本文还描述了使用调节丙酮酸激酶的化合物治疗疾病的方法。

2. 发明申请

US20070281942A1 GLUCOKINASE ACTIVATORS 失效
公开(公告)号：US20070281942A1
公开(公告)日：2007-12-06
申请号：US11754205
申请日：2007-05-25
申请人： Sheldon Cao , Jun Feng , Stephen Gwaltney , David Hosfield , Robert Skene , Jeffrey Stafford , Mingnam Tang
发明人： Sheldon Cao , Jun Feng , Stephen Gwaltney , David Hosfield , Robert Skene , Jeffrey Stafford , Mingnam Tang
IPC分类号： A61K31/519 , A61K31/498 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号： C07D417/12 , C07D401/12 , C07D471/04 , C07D487/04
摘要： Compounds are provided for use with hexokinases that comprise: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
摘要翻译：提供了与己糖激酶一起使用的化合物，其包含：其中变量如本文所定义。还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

3. 发明申请

US20060041137A1 Kinase inhibitors 失效
标题翻译：激酶抑制剂
公开(公告)号：US20060041137A1
公开(公告)日：2006-02-23
申请号：US11208437
申请日：2005-08-18
申请人： Sheldon Cao , Anthony Gangloff , Bheema Paraselli , Jeffrey Stafford , Hasanthi Wijesekera
发明人： Sheldon Cao , Anthony Gangloff , Bheema Paraselli , Jeffrey Stafford , Hasanthi Wijesekera
IPC分类号： C07D403/04 , A61K31/4709
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with kinases that comprise a compound of the formula: wherein R1, R2, R3, Q, U, V, W, X, and Y are as defined herein.
摘要翻译：提供化合物，药物组合物，试剂盒和方法用于包含下式化合物的激酶：其中R 1，R 2，R 3， SUB，Q，U，V，W，X和Y如本文所定义。

4. 发明申请

US20050137232A1 Histone deacetylase inhibitors 失效
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US20050137232A1
公开(公告)日：2005-06-23
申请号：US10803580
申请日：2004-03-17
申请人： Jerome Bressi , Jason Brown , Sheldon Cao , Anthony Gangloff , Andrew Jennings , Jeffrey Stafford , Phong Vu , Xiao-Yi Xiao
发明人： Jerome Bressi , Jason Brown , Sheldon Cao , Anthony Gangloff , Andrew Jennings , Jeffrey Stafford , Phong Vu , Xiao-Yi Xiao
IPC分类号： A61K20060101 , A61K31/4184 , A61K31/454 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/535 , C07D235/18 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号： C07D235/18 , C07D401/04 , C07D401/06 , C07D403/06 , C07D403/10
摘要： Compounds that may be used to inhibit histone deacetylase having the formula Z-Q-L-M or Z-L-M wherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0-10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.
摘要翻译：可用于抑制组氨酸脱乙酰酶的化合物，其具有式<？in-line-formula description =“In-line Formulas”end =“lead”？> ZQLM或ZLM <？in-line-formula description =“In-line 式“end =”tail“？>其中M是能够与脱乙酰酶催化部位和/或金属离子络合的取代基; L是在M取代基和化合物的其余部分之间分离0-10个原子之间的取代基; Z和Q如本文所定义。

5. 发明申请

US20160046579A1 THERAPEUTIC COMPOUNDS AND COMPOSITIONS 审中-公开
标题翻译：治疗化合物和组合物
公开(公告)号：US20160046579A1
公开(公告)日：2016-02-18
申请号：US14776635
申请日：2014-03-13
申请人： Giovanni CIANCHETTA , Janeta POPOVICI-MULLER , Robert ZAHLER , Sheldon CAO , Xiaolei WANG , Zhixiong YE , AGIOS PHARMACEUTICALS, INC.
发明人： Giovanni Cianchetta , Janeta Popovici-Muller , Robert Zahler , Sheldon Cao , Xiaolei Wang , Zhixiong Ye
IPC分类号： C07D211/48 , C07D405/12 , C07D417/12 , C07D401/14 , C07D417/14 , C07F9/6558 , C07D405/14 , C07D413/12 , C07D471/04 , C07D513/04 , C07D413/14 , C07D401/12 , C07D495/04
CPC分类号： C07D401/12 , C07D211/48 , C07D211/52 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D513/04 , C07F9/65583
摘要： Compounds of general formula (I) and compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
摘要翻译：本文描述了通式（I）的化合物和包含调节丙酮酸激酶的通式（I）化合物的组合物。本文还描述了使用调节丙酮酸激酶的化合物治疗疾病的方法。

6. 发明授权

US09108921B2 Therapeutic compounds and compositions 有权
标题翻译：治疗化合物和组合物
公开(公告)号：US09108921B2
公开(公告)日：2015-08-18
申请号：US14210583
申请日：2014-03-14
申请人： Giovanni Cianchetta , Janeta Popovici-Muller , Robert Zahler , Sheldon Cao , Xiaolei Wang , Zhixiong Ye
发明人： Giovanni Cianchetta , Janeta Popovici-Muller , Robert Zahler , Sheldon Cao , Xiaolei Wang , Zhixiong Ye
IPC分类号： A61K31/4709 , C07D401/12 , C07D211/52 , C07D401/14 , C07D417/12 , C07D413/12 , C07D211/48 , C07D405/12 , C07D417/14
CPC分类号： C07D401/12 , C07D211/48 , C07D211/52 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D513/04 , C07F9/65583
摘要： Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
摘要翻译：本文描述了通式I的化合物和包含调节丙酮酸激酶的通式I化合物的组合物。本文还描述了使用调节丙酮酸激酶的化合物治疗疾病的方法。

7. 发明申请

US20110301155A1 INDAZOLE COMPOUNDS FOR ACTIVATING GLUCOKINASE 审中-公开
标题翻译：用于激活GLUCOKINASE的INDAZOLE化合物
公开(公告)号：US20110301155A1
公开(公告)日：2011-12-08
申请号：US12452174
申请日：2008-06-18
申请人： Tsuneo Yasuma , Shigekazu Sasaki , Osamu Ujikawa , Yasufumi Miyamoto , Stephen L. Gwaltney , Sheldon Cao , Andy Jennings
发明人： Tsuneo Yasuma , Shigekazu Sasaki , Osamu Ujikawa , Yasufumi Miyamoto , Stephen L. Gwaltney , Sheldon Cao , Andy Jennings
IPC分类号： A61K31/541 , A61K31/427 , A61K31/4439 , C07D417/12 , A61K31/496 , A61K31/5377 , A61K31/4545 , A61K31/444 , C07D498/04 , A61K31/5383 , A61K31/4985 , C07D401/14 , A61P3/04 , A61P3/10 , C07D417/14
CPC分类号： C07D409/14 , C07D231/56 , C07D401/04 , C07D401/14 , C07D403/12 , C07D417/12 , C07D417/14 , C07D491/10 , C07D498/04
摘要： The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.A compound represented by the formula (I): wherein R1 is an optionally substituted 4- to 7-membered nitrogen-containing heterocyclic group, optionally substituted carbamoyl, or optionally substituted sulfamoyl; R2 is optionally substituted alkyl, optionally substituted alkoxy, an optionally substituted 3- to 7-membered cyclic group, —SR′, —SOR′, or —SO2R′ (R′ is a substituent); R3 is hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxy, —O-Cy (Cy is an optionally substituted 3- to 7-membered cyclic group which may be condensed with benzene), —SR″, —SOR″, or —SO2R″ (R″ is a substituent), or an optionally substituted 3- to 7-membered cyclic group which may be condensed with benzene; R4 is hydrogen, or optionally substituted alkyl; provided that when R3 is hydrogen, halogen, or methoxy, then R2 is not optionally substituted alkyl, or optionally substituted alkoxy; further provided that 5-[5-{[(2S)-2-amino-3-phenylpropyl]oxy}-2-(3-furyl)pyridin-3-yl]-N-pyridin-4-yl-1H-indazol-3-amine and 5-[5-{[(2S)-2-amino-3-phenylpropyl]oxy}-2-(3-furyl)pyridin-3-yl]-1-(4-methoxybenzyl)-N-pyridin-4-yl-1H-indazol-3-amine are excluded; or a salt thereof.
摘要翻译：本发明的目的在于提供一种用作药剂的糖激酶活化剂，例如用于预防或治疗糖尿病，肥胖症等的药剂。由式（I）表示的化合物：其中R1是任选取代的4-至7-元含氮杂环基，任选取代的氨基甲酰基或任选取代的氨磺酰基; R 2是任选取代的烷基，任选取代的烷氧基，任选取代的3-至7-元环基，-SR'，-SOR'或-SO 2 R'（R'是取代基）; R3是氢，卤素，任选取代的烷基，任选取代的烯基，任选取代的烷氧基，-O-Cy（Cy是可以与苯缩合的任选取代的3-至7-元环基），-SR“，-SOR “或-SO 2 R”（R“是取代基），或可以与苯稠合的任选取代的3-至7-元环基; R4是氢或任选取代的烷基; 条件是当R 3为氢，卤素或甲氧基时，则R 2不是任选取代的烷基或任选取代的烷氧基; 进一步提供，5- [5 - {[（2S）-2-氨基-3-苯基丙基]氧基} -2-（3-呋喃基）吡啶-3-基] -N-吡啶-4-基-1H-吲唑 -3-胺和5- [5 - {[（2S）-2-氨基-3-苯基丙基]氧基} -2-（3-呋喃基）吡啶-3-基] -1-（4-甲氧基苄基）-N - 吡啶-4-基-1H-吲唑-3-胺; 或其盐。

8. 发明申请

US20070197532A1 GLUCOKINASE ACTIVATORS 审中-公开
公开(公告)号：US20070197532A1
公开(公告)日：2007-08-23
申请号：US11561307
申请日：2006-11-17
申请人： Sheldon Cao , Jun Feng , Yasuhiro Imaeda , Stephen Gwaltney , David Hosfield , Nobuyuki Takakura , Mingnam Tang
发明人： Sheldon Cao , Jun Feng , Yasuhiro Imaeda , Stephen Gwaltney , David Hosfield , Nobuyuki Takakura , Mingnam Tang
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/4439 , A61K31/4196 , A61K31/4152 , C07D413/02 , C07D403/02
CPC分类号： C07D249/12 , C07D231/12 , C07D231/20 , C07D249/08 , C07D249/14 , C07D401/04 , C07D401/12 , C07D407/04 , C07D409/12 , C07D417/12
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.

9. 发明申请

US20070149495A1 HISTONE DEACETYLASE INHIBITORS 失效
标题翻译： HISTONE脱乙酰酶抑制剂
公开(公告)号：US20070149495A1
公开(公告)日：2007-06-28
申请号：US11557402
申请日：2006-11-07
申请人： Jerome Bressi , Sheldon Cao , Jeffrey Stafford , Phong Vu
发明人： Jerome Bressi , Sheldon Cao , Jeffrey Stafford , Phong Vu
IPC分类号： A61K31/55 , A61K31/445 , A61K31/401 , A61K31/397 , A61K31/396 , A61K31/395
CPC分类号： C07C259/06 , C07D231/16 , C07D239/38 , C07D241/44
摘要： Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen; R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3-12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.
摘要翻译：提供组蛋白脱乙酰酶抑制剂及其用途，其具有以下通式：其中R 1，R 2，R 3和R 4， / SUB>各自独立地选自氢，取代或未取代的直链C 1-12烷基，C 2-12-12氨基烷基或C 1 -C 12烷基， 2-12个氧杂烷基，以及取代和未取代的3,4,5,6,7或8元环，条件是R 3和R 4 不是氢; R 5选自羰基，取代或未取代的C 1-3烷基，取代或未取代的C 1-3烷基，烷基-C（O），取代或未取代的-C（O）-C 1-3烷基和取代或未取代的-C（O）C（O）C 1-3烷基; M是能与蛋白质金属离子络合的取代基; L是包含连接M取代基与L取代基的α原子的3-12个原子的链的取代基。

10. 发明授权

US09662327B2 Phenyl and pyridinyl substituted piperidines and piperazines as inhibitors of IDH1 mutants and their use in treating cancer 有权
公开(公告)号：US09662327B2
公开(公告)日：2017-05-30
申请号：US14126791
申请日：2012-06-18
申请人： Sheldon Cao , Janeta Popovici-Muller , Francesco G. Salituro , Jeffrey O. Saunders , Xuefei Tan , Jeremy Travins , Shunqi Yan , Zhixiong Ye
发明人： Sheldon Cao , Janeta Popovici-Muller , Francesco G. Salituro , Jeffrey O. Saunders , Xuefei Tan , Jeremy Travins , Shunqi Yan , Zhixiong Ye
IPC分类号： C07D491/052 , C07D401/04 , C07D519/00 , C07D217/22 , C07D471/04 , C07D405/12 , A61K31/496 , A61K31/519 , C07D217/26 , C07D413/04 , A61K31/551
CPC分类号： C07D491/052 , A61K31/496 , A61K31/519 , A61K31/551 , C07D217/22 , C07D217/26 , C07D401/04 , C07D405/12 , C07D413/04 , C07D471/04 , C07D519/00
摘要： Provided are compounds of formula (I), wherein X, Y, Z, W, V, R2, R3 and m are defined as in the description. Their pharmaceutical compositions and their uses for treating cancers are also provided.

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