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1. 发明申请

WO2010103547A2 SUBSTITUTED FUSED PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：取代的氟化吡啶化合物
公开(公告)号：WO2010103547A2
公开(公告)日：2010-09-16
申请号：PCT/IN2010/000145
申请日：2010-03-12
申请人： ADVINUS THERAPEUTICS PRIVATE LIMITED , PALLE, Venkata , RAMDAS, Vidya , BARAWKAR, Dinesh , BASU, Sujay , KOUL, Summon , WAMAN, Yogesh , PATEL, Meena , PANMAND, Anil
发明人： PALLE, Venkata , RAMDAS, Vidya , BARAWKAR, Dinesh , BASU, Sujay , KOUL, Summon , WAMAN, Yogesh , PATEL, Meena , PANMAND, Anil
IPC分类号： C07D473/30
CPC分类号： C07D473/40 , A61K31/522 , A61K31/5377 , C07D473/06 , C07D473/18 , C07D473/30
摘要： The present invention discloses substituted fused pyrimidine compounds of formula I, their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The present invention also provides provide the use of compounds of formula (II), or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, for the treatment of a pathological disease susceptible to improvement by antagonism of adenosine receptors. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
摘要翻译：本发明公开了式I的取代的稠合嘧啶化合物，其互变异构体，多晶型物，立体异构体，前药，溶剂合物，药学上可接受的盐或含有它们的药物组合物以及治疗由腺苷受体（AR）活性介导的病症和疾病的方法。本发明还提供式（II）化合物或其互变异构体，多晶型物，立体异构体，前药，溶剂化物或其药学上可接受的盐在治疗易受腺苷受体拮抗作用改善的病理疾病中的用途。本发明的化合物可用于治疗，预防或抑制可能易受腺苷受体拮抗作用改善的疾病和病症，例如哮喘，慢性阻塞性肺病，血管生成，肺纤维化，肺气肿，过敏性疾病，炎症，再灌注损伤，心肌缺血，动脉粥样硬化，高血压，充血性心力衰竭，视网膜病变，糖尿病，肥胖，炎性胃肠道疾病和/或自身免疫性疾病。

2. 发明申请

WO2009118759A2 HETEROCYCLIC COMPOUNDS AS ADENOSINE RECEPTOR ANTAGONIST 审中-公开
标题翻译：作为腺苷受体拮抗剂的杂环化合物
公开(公告)号：WO2009118759A2
公开(公告)日：2009-10-01
申请号：PCT/IN2009/000192
申请日：2009-03-23
申请人： ADVINUS THERAPEUTICS PVT. LTD., , PALLE, Venkata , BASU, Sujay , WAMAN, Yogesh , RAMDAS, Vidya , BARAWKAR, Dinesh
发明人： PALLE, Venkata , BASU, Sujay , WAMAN, Yogesh , RAMDAS, Vidya , BARAWKAR, Dinesh
IPC分类号： C07D473/06 , C07D473/08 , A61K31/522 , A61P3/10 , A61P9/12 , A61P11/06
CPC分类号： C07D473/06 , C07D473/08
摘要： Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.
摘要翻译：作为腺苷受体拮抗剂，本公开的化合物是式（I）的稠合嘧啶化合物，其互变异构体，多晶型物，立体异构体，前药，溶剂合物或其药学上可接受的盐。本发明还描述了其制备方法。

3. 发明申请

WO2011095997A1 BENZAMIDE COMPOUNDS AS GLUCOKINASE ACTIVATORS AND THEIR PHARMACEUTICAL APPLICATION 审中-公开
标题翻译：苯甲酸化合物作为GLUCOKINASE激活剂及其药物应用
公开(公告)号：WO2011095997A1
公开(公告)日：2011-08-11
申请号：PCT/IN2011/000086
申请日：2011-02-07
申请人： ADVINUS THERAPEUTICS PRIVATE LIMITED , DESHPANDE, Anil , KANDALKAR, Sachin , NAIK, Keshav , DAVE, Bhavesh , BHUNIYA, Debnath , PALLE, Venkata
发明人： DESHPANDE, Anil , KANDALKAR, Sachin , NAIK, Keshav , DAVE, Bhavesh , BHUNIYA, Debnath , PALLE, Venkata
IPC分类号： C07D213/80 , C07D401/12 , C07D417/12 , C07D417/14 , C07D513/04 , A61K31/4439 , A61P3/10 , A61P3/04
CPC分类号： C07D417/12 , C07D213/80 , C07D401/12 , C07D417/14 , C07D513/04
摘要： Benzamide compounds of formula (I), their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof useful as Glucokinase activators or modulators are disclosed. The disclosure further relates to process of preparation of the benzamide compounds.
摘要翻译：公开了可用作葡糖激酶活化剂或调节剂的式（I）的苯甲酰胺化合物，其立体异构体，互变异构体，前药，药学上可接受的盐，多晶型物，溶剂合物和制剂。本公开进一步涉及苯甲酰胺化合物的制备方法。

4. 发明申请

WO2011080755A1 FUSED NITROGEN HETEROCYCLIC COMPOUNDS, PROCESS OF PREPARATION AND USES THEREOF 审中-公开
标题翻译：熔融氮杂环化合物，其制备方法及其用途
公开(公告)号：WO2011080755A1
公开(公告)日：2011-07-07
申请号：PCT/IN2010/000844
申请日：2010-12-22
申请人： ADVINUS THERAPEUTICS PRIVATE LIMITED , DAVE, Bhavesh , DESHPANDE, Anil , KURHADE, Santosh , KOBAL, Balasaheb , BHUNIYA, Debnath , PALLE, Venkata
发明人： DAVE, Bhavesh , DESHPANDE, Anil , KURHADE, Santosh , KOBAL, Balasaheb , BHUNIYA, Debnath , PALLE, Venkata
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/4985 , A61K31/519 , A61K31/5025 , A61P3/10 , A61P9/12 , A61P3/06
CPC分类号： C07D487/04 , C07D471/04
摘要： Fused nitrogen heterocyclic compounds, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof, useful as Glucokinase activators or modulators, which are beneficial for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, such as diabetes, metabolic syndrome, and/or diabetes-related complications including retinopathy, nephropathy, neuropathy, ischemic heart disease, arteriosclerosis, β-cell dysfunction, and as therapeutic and/or prophylactic agents for obesity are disclosed. The invention also relates to process of preparation of the fused nitrogen heterocyclic compounds.
摘要翻译：可用作葡糖激酶活化剂或调节剂的富氮氮杂环化合物，其立体异构体，互变异构体，前药，药学上可接受的盐，多晶型物，溶剂合物和制剂，其有利于预防，治疗，控制进展或辅助治疗疾病和/或葡萄糖激酶的活化如糖尿病，代谢综合征和/或糖尿病相关并发症（包括视网膜病变，肾病，神经病，缺血性心脏病，动脉硬化，β细胞功能障碍）和/或治疗和/ 公开了用于肥胖症的预防剂。本发明还涉及稠合氮杂环化合物的制备方法。

5. 发明申请

WO2004007519A1 PARTIAL AND FULL AGONISTS OF A1 ADENOSINE RECEPTORS 审中-公开
标题翻译： A1腺苷受体的部分和全身激素
公开(公告)号：WO2004007519A1
公开(公告)日：2004-01-22
申请号：PCT/US2003/011810
申请日：2003-04-15
申请人： CV THERAPEUTICS, INC. , ELZEIN, Elfatih , IBRAHIM, Prabha , PALLE, Venkata , VARKHEDKAR, Vaibhav , ZABLOCKI, Jeff
发明人： ELZEIN, Elfatih , IBRAHIM, Prabha , PALLE, Venkata , VARKHEDKAR, Vaibhav , ZABLOCKI, Jeff
IPC分类号： C07H19/16
CPC分类号： C07H19/16 , C07D473/16
摘要： Disclosed are novel compounds that are partial and full A 1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infraction.
摘要翻译：公开了作为部分和全部A1腺苷受体激动剂的新型化合物，其可用于治疗各种疾病状态，特别是心动过速和心房扑动，心绞痛和心肌梗死。

6. 发明申请

WO2006117653A1 AZOLE-BASED PHOSPHODIESTERASE INHIBITORS 审中-公开
标题翻译：基于AZOLE的磷酸酯酶抑制剂
公开(公告)号：WO2006117653A1
公开(公告)日：2006-11-09
申请号：PCT/IB2006/001133
申请日：2006-05-03
申请人： RANBAXY LABORATORIES LIMITED , PALLE, Venkata , BALACHANDRAN, Sarala , MUTHUKAMA, Nagarajan , RAY, Abhijit , DASTIDAR, Sunanda Ghose
发明人： PALLE, Venkata , BALACHANDRAN, Sarala , MUTHUKAMA, Nagarajan , RAY, Abhijit , DASTIDAR, Sunanda Ghose
IPC分类号： C07D413/12 , A61K31/4439 , A61P11/00 , A61P31/00
CPC分类号： C07D413/12
摘要： The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds of Formula (I), pharmaceutical compositions containing the compounds described herein and their use as PDE type IV selective inhibitors are provided.
摘要翻译：本发明涉及磷酸二酯酶（PDE）IV型选择性抑制剂。提供了所公开的式（I）化合物的制备方法，含有本文所述化合物的药物组合物及其作为PDE IV型选择性抑制剂的用途。

7. 发明申请

WO2003002566A1 PURINE DERIVATIVES AS A2B ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：嘌呤衍生物作为A2B腺苷受体拮抗剂
公开(公告)号：WO2003002566A1
公开(公告)日：2003-01-09
申请号：PCT/US2002/020631
申请日：2002-06-27
申请人： CV THERAPEUTICS, INC. , PALLE, Venkata , VARKHEDKAR, Vaibhav , ZABLOCKI, Jeff, A. , XIAO, Dengming
发明人： PALLE, Venkata , VARKHEDKAR, Vaibhav , ZABLOCKI, Jeff, A. , XIAO, Dengming
IPC分类号： C07D473/16
CPC分类号： C07D473/16
摘要： Disclosed are novel compounds of formula I that are A 2B adenosine receptor antagonists, useful for treating various disease states, in particular asthma and diarrhea.
摘要翻译：公开了作为A2B腺苷受体拮抗剂的新颖的式I化合物，其可用于治疗各种疾病状态，特别是哮喘和腹泻。

8. 发明申请

WO2008077050A1 ADENOSINE DERIVATIVES AS PARTIAL AND FULL AGONISTS OF A1 ADENOSINE RECEPTORS 审中-公开
标题翻译：腺苷衍生物作为A1腺苷受体的部分和全部激素
公开(公告)号：WO2008077050A1
公开(公告)日：2008-06-26
申请号：PCT/US2007/087957
申请日：2007-12-18
申请人： CV THERAPEUTICS, INC. , DHALLA, Arvinder , ELZEIN, Elfatih , IBRAHIM, Prabha , PALLE, Venkata , VARKHEDKAR, Vaibhav , ZABLOCKI, Jeff
发明人： DHALLA, Arvinder , ELZEIN, Elfatih , IBRAHIM, Prabha , PALLE, Venkata , VARKHEDKAR, Vaibhav , ZABLOCKI, Jeff
IPC分类号： A61K31/52 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P15/08 , A61P25/08
CPC分类号： A61K31/52 , A61K31/7076
摘要： Disclosed are novel compounds a compound of Formula I that are partial and full A 1 adenosine receptor agonists, useful for treating various disease states, in particular dyslipidemia, diabetes, decreased insulin sensitivity, Polycystic Ovarian Syndrome, Stein-Leventhal syndrome, and obesity.
摘要翻译：公开了作为部分和全部A 1 N 2腺苷受体激动剂的新颖化合物，其可用于治疗各种疾病状态，特别是血脂异常，糖尿病，胰岛素敏感性降低，多囊卵巢综合征，Stein- Leventhal综合征和肥胖症。

9. 发明申请

WO2004069818A1 SUBSTITUTED HETEROCYCLIC COMPOUNDS USEFUL IN THE TREATMENT OF CARDIOVASCULAR DISEASES 审中-公开
标题翻译：用于治疗心血管疾病的替代性杂环化合物
公开(公告)号：WO2004069818A1
公开(公告)日：2004-08-19
申请号：PCT/US2004/001147
申请日：2004-01-16
申请人： CV THERAPEUTICS INC. , JIANG, Robert , MARQUART, Tim , ZABLOCKI, Jeff , ELZEIN, Elfatih , PALLE, Venkata , IBRAHIM, Prabha
发明人： JIANG, Robert , MARQUART, Tim , ZABLOCKI, Jeff , ELZEIN, Elfatih , PALLE, Venkata , IBRAHIM, Prabha
IPC分类号： C07D277/64
CPC分类号： C07D417/12 , C07D277/64
摘要： wherein: a.o. T is oxygen, sulfur, or NR 11 , in which R 11 is hydrogen or lower alkyl; V is -N 1 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; X 2 is optionally substituted aryl or optionally substituted heteroaryl; Y is optionally substituted dihydroheteroarcyl; and Z 1 and Z 2 are independently optionally substituted alkylene of 1-4 carbon atoms, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal’s (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.
摘要翻译：其中：a.o. T是氧，硫或NR 11，其中R 11是氢或低级烷基; V是-N <， - CH - ， - NH- X 1是氢，任选取代的低级烷基，任选取代的环烷基，任选取代的芳基或任选取代的杂芳基; X 2是任选取代的芳基或任选取代的杂芳基; Y是任选取代的二氢异喹啉基; Z 1和Z 2独立地是1-4个碳原子的任意取代的亚烷基，可用于治疗各种疾病状态，特别是心血管疾病如心房和室性心律失常，间歇性跛行，Prinzmetal（变体）心绞痛，稳定和不稳定的心绞痛，运动诱发的心绞痛，充血性心脏病和心肌梗死。该化合物也可用于治疗糖尿病。

10. 发明申请

WO2003008411A1 SUBSTITUTED PIPERAZINE COMPOUNDS AND THEIR USE AS FATTY ACID OXIDATION INHIBITORS 审中-公开
标题翻译：替代哌嗪化合物及其作为脂肪酸氧化抑制剂的用途
公开(公告)号：WO2003008411A1
公开(公告)日：2003-01-30
申请号：PCT/US2002/022897
申请日：2002-07-18
申请人： CV THERAPEUTICS, INC. , IBRAHIM, Prabha , SHENK, Kevin , ELZEIN, Elfatih , PALLE, Venkata , ZABLOCKI, Jeff , REHDER, Kenneth
发明人： IBRAHIM, Prabha , SHENK, Kevin , ELZEIN, Elfatih , PALLE, Venkata , ZABLOCKI, Jeff , REHDER, Kenneth
IPC分类号： C07D417/12
CPC分类号： C07D263/57 , C07D271/06 , C07D277/64 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Disclosed are novel heterocyclic derivatives of the formula (I), wherein amongst others R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are hydrogen; T is oxygen, sulfur, or NR 11 , in which R 11 is hydrogen or lower alkyl; V is N 1 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; X 2 is optionally substituted aryl or optionally substituted heteroaryl; Y is optionally substituted monocyclic heteroarylenyl; and Z 1 and Z 2 are independently optionally substituted alkylene or 1-4 carbon atoms. The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes, and for increasing HDL plasma levels in mammals.
摘要翻译：公开了式（I）的新型杂环衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，和R 8是氢; T是氧，硫或NR 11，其中R 11是氢或低级烷基; V是N <，-CH <或N-CH; X 1是氢，任选取代的低级烷基，任选取代的环烷基，任选取代的芳基或任选取代的杂芳基; X 2是任选取代的芳基或任选取代的杂芳基; Y是任选取代的单环杂芳基烯基; Z 1和Z 2独立地是任意取代的亚烷基或1-4个碳原子。这些化合物可用于治疗各种疾病状态，特别是心血管疾病如心房和室性心律失常，间歇性跛行，Prinzmetal（变异）心绞痛，稳定和不稳定心绞痛，运动诱发的心绞痛，充血性心脏病和心肌梗死。该化合物还可用于治疗糖尿病，并且用于增加哺乳动物的HDL血浆水平。

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