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1. 发明专利

IL255613A Heterocyclic inhibitors of erk1 and erk2 and their use in the treatment of cancer 未知
公开(公告)号：IL255613A
公开(公告)日：2021-03-25
申请号：IL25561317
申请日：2017-11-12
申请人： ASANA BIOSCIENCES LLC , ARANAPAKAM M VENKATESAN , SCOTT K THOMPSON , ROGER A SMITH , SANJEEVA P REDDY , PURUSHOTTAM M DEWANG , GURULINGAPPA HALLUR , CHANDRIKA MULAKALA , RAGHAVA REDDY KETHIRI , RAMESH MULLANGI , MOHD ZAINUDDIN
发明人： ARANAPAKAM M VENKATESAN , SCOTT K THOMPSON , ROGER A SMITH , SANJEEVA P REDDY , PURUSHOTTAM M DEWANG , GURULINGAPPA HALLUR , CHANDRIKA MULAKALA , RAGHAVA REDDY KETHIRI , RAMESH MULLANGI , MOHD ZAINUDDIN
IPC分类号： A61K31/4439 , A61K31/443 , A61K31/444 , A61K31/506 , A61K31/5377 , A61P35/00 , A61P43/00
摘要： The present application provides a compound that is N-(2-amino-1-(3 -chloro-5 -fluorophenyl)ethyl)-1-(5-methyl-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-1H-imidazole-4-carboxamide (shown below), or a pharmaceutically acceptable salt or stereoisomer thereof. Also provided are methods for preparing the compound. The compound is useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of the compound, the compouns is effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using the compound and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

2. 发明专利

IL255613D0 Heterocyclic inhibitors of erk1 and erk2 and their use in the treatment of cancer 未知
公开(公告)号：IL255613D0
公开(公告)日：2018-01-31
申请号：IL25561317
申请日：2017-11-12
申请人： ASANA BIOSCIENCES LLC , ARANAPAKAM M VENKATESAN , SCOTT K THOMPSON , ROGER A SMITH , SANJEEVA P REDDY , PURUSHOTTAM M DEWANG , GURULINGAPPA HALLUR , CHANDRIKA MULAKALA , RAGHAVA REDDY KETHIRI , RAMESH MULLANGI , MOHD ZAINUDDIN
发明人： ARANAPAKAM M VENKATESAN , SCOTT K THOMPSON , ROGER A SMITH , SANJEEVA P REDDY , PURUSHOTTAM M DEWANG , GURULINGAPPA HALLUR , CHANDRIKA MULAKALA , RAGHAVA REDDY KETHIRI , RAMESH MULLANGI , MOHD ZAINUDDIN
IPC分类号： C07D20060101
摘要： The present application provides a compound that is N-(2-amino-1-(3 -chloro-5 -fluorophenyl)ethyl)-1-(5-methyl-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-1H-imidazole-4-carboxamide (shown below), or a pharmaceutically acceptable salt or stereoisomer thereof. Also provided are methods for preparing the compound. The compound is useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of the compound, the compouns is effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using the compound and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

3. 发明申请

US20080234300A1 Pyrimido[5,4-c] Quinoline-2, 4-Diamine Derivatives and Methods of Use Thereof 审中-公开
标题翻译：嘧啶并[5,4-c]喹啉-2,4-二胺衍生物及其使用方法
公开(公告)号：US20080234300A1
公开(公告)日：2008-09-25
申请号：US12042092
申请日：2008-03-04
申请人： Allan WISSNER , Aranapakam M. VENKATESAN
发明人： Allan WISSNER , Aranapakam M. VENKATESAN
IPC分类号： A61K31/519 , C07D471/04 , A61P35/00
CPC分类号： C07D471/04
摘要： The present invention relates to pyrimido[5,4-c]quinoline-2,4-diamine derivatives, compositions comprising an effective amount of a Pyrimido[5,4-c]quinoline-2,4-diamine Derivative, methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof an effective amount of an Pyrimido[5,4-c]quinoline-2,4-diamine Derivative, methods for modulating PDK-1 activity, comprising administering to a subject in need thereof an effective amount of a Pyrimido[5,4-c]quinoline-2,4-diamine Derivative. The invention also relates to a process for preparing a Pyrimido[5,4-c]quinoline-2,4-diamine Derivative.
摘要翻译：本发明涉及嘧啶并[5,4-c]喹啉-2,4-二胺衍生物，包含有效量的嘧啶并[5,4-c]喹啉-2,4-二胺衍生物的组合物，预防增殖性疾病，包括向有需要的受试者施用有效量的嘧啶并[5,4-c]喹啉-2,4-二胺衍生物，用于调节PDK-1活性的方法，包括对需要的受试者施用其具有有效量的嘧啶并[5,4-c]喹啉-2,4-二胺衍生物。本发明还涉及制备嘧啶并[5,4-c]喹啉-2,4-二胺衍生物的方法。

4. 发明授权

US06939870B2 Substituted-3-indolyl-4-piperidino-alkyl heterocycles for the treatment of depression 失效
公开(公告)号：US06939870B2
公开(公告)日：2005-09-06
申请号：US10652424
申请日：2003-08-29
申请人： Aranapakam M. Venkatesan , Jamie M. Davis , Yansong Gu
发明人： Aranapakam M. Venkatesan , Jamie M. Davis , Yansong Gu
IPC分类号： C07D401/14 , C07D471/04 , C07D417/14 , A61K31/53 , A61K31/549 , A61P25/24 , C07D403/14
CPC分类号： C07D401/14 , A61K31/4745 , A61K31/517 , A61K31/53 , A61K31/549 , C07D471/04
摘要： A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.

5. 发明授权

US06358980B1 Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase/tace inhibitors 失效
标题翻译：含有异羟肟酸化合物的炔基作为基质金属蛋白酶/抑制剂
公开(公告)号：US06358980B1
公开(公告)日：2002-03-19
申请号：US09492686
申请日：2000-01-27
申请人： Jeremy I. Levin , Aranapakam M. Venkatesan , James M. Chen , Arie Zask , Vincent P. Sandanayaka , Mila T. Du , Jannie L. Baker
发明人： Jeremy I. Levin , Aranapakam M. Venkatesan , James M. Chen , Arie Zask , Vincent P. Sandanayaka , Mila T. Du , Jannie L. Baker
IPC分类号： A61K31445
CPC分类号： C07D309/08 , A61K31/351 , A61K31/435 , A61K31/445 , A61K31/496 , C07D211/60 , C07D211/62 , C07D211/66
摘要： Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
摘要翻译：下列化合物：可用于治疗关节炎，肿瘤转移，组织溃疡，创伤愈合异常，牙周病，骨病，糖尿病（胰岛素抵抗）和HIV感染。

6. 发明授权

US06825354B2 Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase and TACE inhibitors 失效
标题翻译：含有异羟肟酸的炔基作为基质金属蛋白酶和TACE抑制剂
公开(公告)号：US06825354B2
公开(公告)日：2004-11-30
申请号：US10055502
申请日：2001-11-13
申请人： Jeremy I. Levin , Aranapakam M. Venkatesan , Derek C. Cole , James M. Chen , Jamie M. Davis , George T. Grosu
发明人： Jeremy I. Levin , Aranapakam M. Venkatesan , Derek C. Cole , James M. Chen , Jamie M. Davis , George T. Grosu
IPC分类号： C07D21172
CPC分类号： C07D209/48 , C07C317/44 , C07C317/50 , C07C323/60 , C07C2601/14 , C07D207/34 , C07D213/56 , C07D215/48 , C07D215/54 , C07D217/26 , C07D295/088 , C07D309/04 , C07D311/84 , C07D333/20 , C07D333/60 , C07D335/02
摘要： Compounds of the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
摘要翻译：该化合物可用于治疗由TNF-α介导的疾病状况，例如类风湿性关节炎，骨关节炎，败血症，AIDS，溃疡性结肠炎，多发性硬化，克罗恩病和退行性软骨损失。

7. 发明授权

US6083975A Substituted benzo[1,4]dioxines as antiobesity agents 失效
标题翻译：取代的苯并[1,4]二恶烷作为抗肥胖剂
公开(公告)号：US6083975A
公开(公告)日：2000-07-04
申请号：US324471
申请日：1999-06-01
申请人： Aranapakam M. Venkatesan
发明人： Aranapakam M. Venkatesan
IPC分类号： A61K31/357 , C07D319/20
CPC分类号： C07D319/20 , A61K31/357
摘要： This invention relates to novel substituted 1,4-benzodioxine compounds having antidiabetic, antihyperglycemic, and antiobesity properties represented by the formula ##STR1## wherein R.sup.1 and R.sup.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen;R.sup.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl; R.sup.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl;or R.sup.2 and R.sup.3 are joined to form the oxazolidinone ring ##STR2## R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl;R.sup.7 and R.sup.8 are independently OR.sup.9 or NR.sup.10 R.sup.11 ;R.sup.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, phenyl, naphthyl, phenyl C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy C.sub.1 to C.sub.6 alkyl, pyridyl, thiophenyl, furanyl, imidazolyl, oxazolyl, --CHR.sup.12 COOR.sup.13, --CHR.sup.12 C(O)R.sup.13, --CHR.sup.12 CONR.sup.10 R.sup.11, --CHR.sup.12 OCOOR.sup.13, or --CHR.sup.12 OC(O)R.sup.13 ;R.sup.10 and R.sup.11 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, phenyl, naphthyl, phenyl-C.sub.1, to C.sub.6 alkyl, furanylalkyl, or alkoxycarbonylalkyl;R.sup.12 and R.sup.13 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, phenyl, naphthyl, or phenyl-C.sub.1 to C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof,a salt thereof;an enantiomer thereof, the racemic mixtures thereof, and the diastereomeric mixtures thereof.The present invention also relates to a pharmaceutical composition, and methods for treating diabetes and/or hyperglycemia and/or obesity in mammals and producing lean meat in edible domestic animals.
摘要翻译：本发明涉及具有由下式表示的抗糖尿病，抗高血糖和抗肥胖特性的新型取代的1,4-苯并二恶英化合物，其中R 1和R 6独立地是氢，C 1至C 6烷基，三氟甲基，氰基，C 1至C 6烷氧基或卤素; R2是氢或C1-C6三烷基甲硅烷基; R3是氢或C1-C6烷氧基羰基; 或R 2和R 3连接形成恶唑烷酮环R4和R5独立地是氢或C1-C6烷基; R7和R8独立地是OR9或NR10R11; R9是氢，C1至C12烷基，C1至C12环烷基，C1至C12甲硅烷基烷基，苯基，萘基，苯基C1至C6烷基，C1至C6烷氧基C1至C6烷基，吡啶基，噻吩基，呋喃基，咪唑基，恶唑基，-CHR12COOR13 ，-CHR 12 C（O）R 13，-CHR 12 CONR 10 R 11，-CHR 12 COOOR 13或-CHR 12 OC（O）R 13; R 10和R 11独立地为氢，C 1至C 12烷基，苯基，萘基，苯基-C 1至C 6烷基，呋喃基烷基或烷氧基羰基烷基; R 12和R 13独立地是氢，C 1至C 12烷基，苯基，萘基或苯基-C 1至C 6烷基; 及其药学上可接受的盐，其盐; 其对映异构体，其外消旋混合物及其非对映体混合物。本发明还涉及药物组合物，以及用于治疗哺乳动物中的糖尿病和/或高血糖症和/或肥胖症并在食用家畜中生产瘦肉的方法。

8. 发明授权

US6020361A Substituted benzo[1,4]dioxines as antiobesity agents 失效
标题翻译：取代的苯并[1,4]二恶烷作为抗肥胖剂
公开(公告)号：US6020361A
公开(公告)日：2000-02-01
申请号：US323463
申请日：1999-06-01
申请人： Aranapakam M. Venkatesan
发明人： Aranapakam M. Venkatesan
IPC分类号： A61K31/357 , C07D319/20 , A61K31/335
CPC分类号： C07D319/20 , A61K31/357
摘要： This invention relates to novel substituted 1,4-benzodioxine compounds having antidiabetic, andihyperglycemic, and antiobesity properties represented by the formula ##STR1## wherein R.sup.1 and R.sup.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen;R.sup.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl; R.sup.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl;or R.sup.2 and R.sup.3 are joined to form the oxazolidinone ring ##STR2## R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl; R.sup.7 and R.sup.8 are independently hydrogen OR.sup.9 or NR.sup.10 R.sup.11 ;R.sup.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, phenyl, naphthyl, phenyl C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy C.sub.1 to C.sub.6 alkyl, pyridyl, thiophenyl, furanyl, imidazolyl, oxazolyl, --CHR.sup.12 COOR.sup.13, --CHR.sup.12 C(O)R.sup.13, --CHR.sup.12 CONR.sup.10 R.sup.11, --CHR.sup.12 OCOOR.sup.13, or --CHR.sup.12 OC(O)R.sup.13 ; R.sup.10 and R.sup.11 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, phenyl, naphthyl, phenyl-C.sub.1 to C.sub.6 alkyl, furanylalkyl, or alkoxycarbonylalkyl;R.sup.12 and R.sup.13 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, phenyl, naphthyl, or phenyl-C.sub.1 to C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof,a salt thereof;an enantiomer thereof, the racemic mixtures thereof, and the diastereomeric mixtures thereof.The present invention also relates to a pharmaceutical composition, and methods for treating diabetes and/or hyperglycemia and/or obesity in mammals and producing lean meat in edible domestic animals.
摘要翻译：本发明涉及具有抗糖尿病，高血糖和抗肥胖特性的新型取代的1,4-苯并二恶英化合物，其由下式表示：其中R 1和R 6独立地为氢，C 1至C 6烷基，三氟甲基，氰基，C 1至C 6烷氧基或卤素; R2是氢或C1-C6三烷基甲硅烷基; R3是氢或C1-C6烷氧基羰基; 或R 2和R 3连接形成恶唑烷酮环R4和R5独立地为氢或C1至C6烷基; R7和R8独立地是氢OR9或NR10R11; R9是氢，C1至C12烷基，C1至C12环烷基，C1至C12甲硅烷基烷基，苯基，萘基，苯基C1至C6烷基，C1至C6烷氧基C1至C6烷基，吡啶基，噻吩基，呋喃基，咪唑基，恶唑基，-CHR12COOR13 ，-CHR 12 C（O）R 13，-CHR 12 CONR 10 R 11，-CHR 12 COOOR 13或-CHR 12 OC（O）R 13; R 10和R 11独立地为氢，C 1至C 12烷基，苯基，萘基，苯基-C 1至C 6烷基，呋喃基烷基或烷氧基羰基烷基; R 12和R 13独立地是氢，C 1至C 12烷基，苯基，萘基或苯基-C 1至C 6烷基; 及其药学上可接受的盐，其盐; 其对映异构体，其外消旋混合物及其非对映体混合物。本发明还涉及药物组合物，以及用于治疗哺乳动物中的糖尿病和/或高血糖症和/或肥胖症并在食用家畜中生产瘦肉的方法。

9. 发明授权

US5965607A Substituted Benzo[1,4]dioxines as antiobesity agents 失效
标题翻译：取代的苯并[1,4]二恶烷作为抗肥胖剂
公开(公告)号：US5965607A
公开(公告)日：1999-10-12
申请号：US993481
申请日：1997-12-18
申请人： Aranapakam M. Venkatesan
发明人： Aranapakam M. Venkatesan
IPC分类号： A61K31/357 , C07D319/20 , A61K31/335
CPC分类号： C07D319/20 , A61K31/357
摘要： This invention relates to novel substituted 1,4-benzodioxine compounds having antidiabetic, antihyperglycemic, and antiobesity properties represented by the formula ##STR1## wherein R.sup.1 and R.sup.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen;R.sup.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl; R.sup.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl;or R.sub.2 and R.sup.3 are joined to form the oxazolidinone ring ##STR2## R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl;R.sup.7 and R.sup.8 are independently OR.sup.9 or NR.sup.10 R.sup.11 ;R.sup.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, phenyl, naphthyl phenyl C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy C.sub.1 to C.sub.6 alkyl, pyridyl, thiophenyl, furanyl, imidazolyl, oxazolyl, --CHR.sup.12 COOR.sup.13 --CHR.sup.12 C(O)R.sup.13, --CHR.sup.12 CONR.sup.10 R.sup.11, --CHR.sup.12 OCOOR.sup.13, or --CHR.sup.12 OC(O)R.sup.13 ;R.sup.10 and R.sup.11 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, phenyl, naphthyl, phenyl-C.sub.1 to C.sub.6 alkyl, furanylalkyl, or alkoxycarbonylalkyl;R.sup.12 and R.sup.13 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, phenyl, naphthyl, or phenyl-C.sub.1 to C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, a salt thereof;an enantiomer thereof, the racemic mixtures thereof, and the diastereomeric mixtures thereof. The present invention also relates to a pharmaceutical composition, and methods for treating diabetes and/or hyperglycemia and/or obesity in mammals and producing lean meat in edible domestic animals.
摘要翻译：本发明涉及具有由下式表示的抗糖尿病，抗高血糖和抗肥胖特性的新的取代的1,4-苯并二恶英化合物，其中R 1和R 6独立地是氢，C 1至C 6烷基，三氟甲基，氰基，C 1至C 6烷氧基或卤素; R2是氢或C1-C6三烷基甲硅烷基; R3是氢或C1-C6烷氧基羰基; 或R 2和R 3连接形成恶唑烷酮环R4和R5独立地是氢或C1-C6烷基; R7和R8独立地是OR9或NR10R11; R9是氢，C1至C12烷基，C1至C12环烷基，C1至C12甲硅烷基烷基，苯基，萘基苯基C1至C6烷基，C1至C6烷氧基C1至C6烷基，吡啶基，噻吩基，呋喃基，咪唑基，恶唑基，-CHR12COOR13- CHR 12 C（O）R 13，-CHR 12 CONR 10 R 11，-CHR 12 COOOR 13或-CHR 12 OC（O）R 13; R 10和R 11独立地为氢，C 1至C 12烷基，苯基，萘基，苯基-C 1至C 6烷基，呋喃基烷基或烷氧基羰基烷基; R 12和R 13独立地是氢，C 1至C 12烷基，苯基，萘基或苯基-C 1至C 6烷基; 及其药学上可接受的盐，其盐; 其对映异构体，其外消旋混合物及其非对映体混合物。本发明还涉及药物组合物，以及用于治疗哺乳动物中的糖尿病和/或高血糖症和/或肥胖症并在食用家畜中生产瘦肉的方法。

10. 发明授权

US5849735A Tricyclic benzazepine vasopressin antagonists 失效
公开(公告)号：US5849735A
公开(公告)日：1998-12-15
申请号：US548805
申请日：1995-12-22
申请人： Jay D. Albright , Aranapakam M. Venkatesan , Efren G. Delos Santos
发明人： Jay D. Albright , Aranapakam M. Venkatesan , Efren G. Delos Santos
IPC分类号： C07D223/20 , C07D223/28 , C07D243/38 , C07D267/20 , C07D401/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , A61K31/55 , A61K31/675
CPC分类号： C07D401/12 , C07D223/20 , C07D223/28 , C07D243/38 , C07D267/20 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

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