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公开(公告)号：US06855818B2
公开(公告)日：2005-02-15
申请号：US09812176
申请日：2001-03-19
IPC分类号： C07H19/067 , A61K31/7076 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/10 , C07H19/16
CPC分类号： C07H19/16
摘要： 2-adenosine C-pyrazole compositions having the following formula: and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
摘要翻译： 具有下式的2-腺苷C-吡唑组合物：以及用于作为A2A受体激动剂的组合物用于刺激哺乳动物冠状血管扩张用于治疗目的和用于成像心脏的方法。
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公开(公告)号：US06852723B2
公开(公告)日：2005-02-08
申请号：US10365344
申请日：2003-02-11
申请人： Jeff Zablocki , Elfatih Elzein , Brent K. Blackburn , Tim Marquart , Prabha N. Ibrahim , Venkata P. Palle
发明人： Jeff Zablocki , Elfatih Elzein , Brent K. Blackburn , Tim Marquart , Prabha N. Ibrahim , Venkata P. Palle
IPC分类号： C07D241/04 , C07D241/08 , C07D241/42 , C07D295/15 , C07D317/54 , C07D317/58 , A61K31/495 , A61K31/496
CPC分类号： C07D295/15 , C07D241/04 , C07D241/08 , C07D241/42 , C07D317/54 , C07D317/58
摘要： Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.
摘要翻译： 新的通式化合物及其药学上可接受的酸加成盐，其中所述化合物可用于治疗以保护骨骼肌免受创伤损伤或保护肌肉或全身性疾病如间歇性跛行后的骨骼肌，以治疗休克 条件，以维持移植物中使用的供体组织和器官，治疗包括心房和室性心律失常的心血管疾病，Prinzmetal（变体）心绞痛，稳定性心绞痛和运动诱发的心绞痛，充血性心脏病和心肌梗塞。
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公开(公告)号：US06770634B1
公开(公告)日：2004-08-03
申请号：US10018758
申请日：2002-03-12
IPC分类号： A01N4304
CPC分类号： C07H19/16
摘要： 2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
摘要翻译： 具有式（a）的2-腺苷C-吡唑化合物和使用该化合物作为A2A受体激动剂的方法，用于刺激哺乳动物冠状血管扩张用于治疗目的和用于成像心脏的目的。
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24.发明授权Partial or full A1agonists-N-6 heterocyclic 5′-thio substituted adenosine derivatives 失效部分或全部的Alagonists-N-6杂环5'-硫取代的腺苷衍生物公开(公告)号：US06605597B1
公开(公告)日：2003-08-12
申请号：US09454136
申请日：1999-12-03
IPC分类号： A61K5170
CPC分类号： C07H19/16
摘要： N6 heterocyclic 5′ modified adenosine derivatives that are adenosine A1 receptor partial or full agonists, and as such, are useful for modifying cardiac activity, modifying adipocyte function, treating central nervous system disorders, and treating diabetic disorders and obesity in mammals, and especially in humans.
摘要翻译： 作为腺苷A1受体部分或全部激动剂的N6杂环5'修饰的腺苷衍生物，因此可用于改善心脏活动，改善脂肪细胞功能，治疗中枢神经系统疾病，以及治疗哺乳动物的糖尿病病症和肥胖症，特别是在 人类。
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公开(公告)号：US06440948B1
公开(公告)日：2002-08-27
申请号：US09597436
申请日：2000-06-20
IPC分类号： A61K3170
CPC分类号： C07H19/16 , A61K49/0004
摘要： 2-(3-,4-(substituted)-5-alkylthienyl)adenosines and the 5′-uronic acid amide analogues thereof having the following formula: are disclosed herein. Additionally disclosed are medicinal methods of treatment wherein the adenosine A2A agonist activity of the noted compounds stimulates mammalian coronary vasodilation for therapeutic purposes and for purposes of imaging the heart.
摘要翻译： 2-（3-，4-（取代的）-5-烷基噻吩基）腺苷及其具有下式的5'-糖醛酸酰胺类似物：本文公开。 另外公开了药物治疗方法，其中所述化合物的腺苷A2A激动剂活性刺激哺乳动物冠状动脉血管舒张用于治疗目的和用于成像心脏的目的。
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公开(公告)号：US06403567B1
公开(公告)日：2002-06-11
申请号：US09338185
申请日：1999-06-22
IPC分类号： A61K3170
CPC分类号： C07H19/16 , C07D473/34
摘要： 2-adenosine N-pyrazole compositions having the following formula: and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
摘要翻译： 具有下式的2-腺苷N-吡唑组合物和使用该组合物作为A2A受体激动剂刺激哺乳动物冠状动脉血管扩张治疗目的和用于心脏成像的方法。
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公开(公告)号：US08569260B2
公开(公告)日：2013-10-29
申请号：US13598451
申请日：2012-08-29
IPC分类号： A61K31/70 , C07H19/167 , C07H19/173
CPC分类号： C07H19/16 , C07D473/34
摘要： The present disclosure provides a process for the preparation of 2-adenosine N-pyrazole compounds exemplified by the structure shown below that are potent and selective agonists for A2A adenosine receptor, compositions comprising these compounds, and methods for using these compounds to stimulate mammalian coronary vasodilation for imaging the heart.
摘要翻译： 本公开提供了制备2-腺苷N-吡唑化合物的方法，其以下列结构为例，其为A2A腺苷受体的有效和选择性激动剂，包含这些化合物的组合物，以及使用这些化合物刺激哺乳动物冠状动脉血管扩张的方法 为心脏成像。
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28.发明授权公开(公告)号：US08420666B2
公开(公告)日：2013-04-16
申请号：US12531043
申请日：2008-03-14
申请人： Sonali Rudra , Nidhi Gupta , Lalit Kumar Baregama , Ritu Agarwal , Vinayak Vasantrao Khairnar , Mandadapu Raghu Ramaiah , Venkata P. Palle , Sarala Balachandran , Atul Kondaskar , Manohar Salla , Abhijit Ray , Sunanda G. Dastidar , Lalitha Vijaykrishnan
发明人： Sonali Rudra , Nidhi Gupta , Lalit Kumar Baregama , Ritu Agarwal , Vinayak Vasantrao Khairnar , Mandadapu Raghu Ramaiah , Venkata P. Palle , Sarala Balachandran , Atul Kondaskar , Manohar Salla , Abhijit Ray , Sunanda G. Dastidar , Lalitha Vijaykrishnan
IPC分类号： C07D513/02 , C07D515/02 , A01N43/42 , A61K31/44
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formula 1: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE type 4/PDE type 7 inhibitors are provided.
摘要翻译： 本发明涉及磷酸二酯酶（PDE）4型，磷酸二酯酶（PDE）7型和双重PDE型4 / PDE型7型抑制剂。 本文公开的具有式1结构的化合物可用于治疗，预防，抑制或抑制CNS疾病，例如多发性硬化; 各种病理状况如影响免疫系统的疾病，包括艾滋病，移植排斥反应，自身免疫性疾病如T细胞相关疾病，例如类风湿性关节炎; 炎性疾病如呼吸道炎症疾病，包括慢性阻塞性肺疾病（COPD），哮喘，支气管炎，过敏性鼻炎，成人呼吸窘迫综合征（ARDS）和其他炎性疾病，包括但不限于银屑病，休克，特应性皮炎，嗜酸性肉芽肿，过敏性 结膜炎，骨关节炎; 胃肠道炎症性疾病如克罗恩病，结肠炎，胰腺炎以及不同类型的癌症，包括白血病; 特别是在人类。 提供了制备所公开的化合物的方法，含有所公开的化合物的药物组合物及其作为PDE 4型，PDE型7和双重PDE型4 / PDE 7型抑制剂的用途。
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公开(公告)号：US20100081810A1
公开(公告)日：2010-04-01
申请号：US12491791
申请日：2009-06-25
IPC分类号： C07D473/34
CPC分类号： C07H19/16
摘要： 2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
摘要翻译： 具有式（a）的2-腺苷C-吡唑化合物和使用该化合物作为A2A受体激动剂的方法，用于刺激哺乳动物冠状血管扩张用于治疗目的和用于成像心脏的目的。
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公开(公告)号：US20100081610A1
公开(公告)日：2010-04-01
申请号：US12438182
申请日：2007-08-21
申请人： Viswajanani J. Sattigeri , Venkata P. Palle , Manoj Kumar Khera , Ranaheer Reddy , Manoj Kumar Tiwari , Ajay Soni , Abdul Rehman Abdul Rauf , Sony Joseph , Arpita Musib , Sunanda G. Dastidar , Punit Kumar Srivastava
发明人： Viswajanani J. Sattigeri , Venkata P. Palle , Manoj Kumar Khera , Ranaheer Reddy , Manoj Kumar Tiwari , Ajay Soni , Abdul Rehman Abdul Rauf , Sony Joseph , Arpita Musib , Sunanda G. Dastidar , Punit Kumar Srivastava
IPC分类号： A61K38/13 , C07D253/08 , A61K31/53 , C07D401/02 , A61K31/4439 , C07D209/44 , A61K31/404 , A61K31/5415 , A61K31/56 , C07D277/00 , A61P29/00 , A61P37/06
CPC分类号： A61K31/4155 , A61K31/4035 , A61K31/41 , A61K31/438 , A61K31/4439 , A61K31/444 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/53 , A61K31/536 , A61K45/06 , C07D209/44 , C07D209/48 , C07D253/08 , C07D265/26 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/10
摘要： The present invention relates to β-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure β-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.
摘要翻译： 本发明涉及作为基质金属蛋白酶抑制剂，特别是非对映体纯的β-羟基羧酸的羟基和氨基取代的羧酸，用于合成含有本发明化合物的药物组合物的相应方法。 本发明的化合物可用于治疗各种炎性，自身免疫性和过敏性疾病，例如治疗哮喘，类风湿性关节炎，COPD，鼻炎，骨关节炎，牛皮癣关节炎，牛皮癣，肺纤维化，伤口愈合障碍，肺部炎症， 急性呼吸窘迫综合征，牙周炎，多发性硬化症，牙龈炎，动脉粥样硬化，新生内膜增生，其导致再狭窄和缺血性心力衰竭，中风，肾脏疾病，肿瘤转移和其他炎症性疾病，其特征在于过度表达和过度激活 使用该化合物的基质金属蛋白酶。
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