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1. 发明专利

IL161608A SYNTHESIS AND THERAPEUTIC USE OF 2-ARALKOXYADENOSINES AND 2-ALKOXYADENOSINES 未知
公开(公告)号：IL161608A
公开(公告)日：2010-05-31
申请号：IL16160804
申请日：2004-04-25
申请人： KING PHARMACEUTICALS RES & DEV , MOORMAN ALLAN R
发明人： MOORMAN ALLAN R
IPC分类号： C07H19/167 , C07H19/16 , C07H19/173
摘要： The invention provides new methods for synthesis of 2-aralkyloxyadenosines and 2-alkoxyadenosines. The invention is particularly useful for synthesis of 2-[2-(4-chlorophenyl)ethoxy]adenosine. Preferred methods of the invention include activating a guanosine compound followed by hydrolysis; alkylating the hydrolyzed compound with subsequent animation to provide a 2-aralkyloxyadenosine or a 2-alkoxyadenosine compound.

2. 发明申请

WO2009015004A1 CRYSTALS OF (2-AMINO-4,5,6,7-TETRAHYDROBENZO[B]THIEN-3-YL)(4-CHLOROPHENYL)METHANONE 审中-公开
标题翻译：（2-氨基-4,5,6,7-四氢苯并[b]噻吩-3-基）（4-氯苯基）甲酮的晶体
公开(公告)号：WO2009015004A1
公开(公告)日：2009-01-29
申请号：PCT/US2008/070423
申请日：2008-07-18
申请人： KING PHARMACEUTICALS RESEARCH AND DEVELOPMENT, INC. , LAURENCE, George , MOORMAN, Allan, R. , PARK, Aeri
发明人： LAURENCE, George , MOORMAN, Allan, R. , PARK, Aeri
IPC分类号： C07D223/00
CPC分类号： C07D333/66
摘要： The present invention provides crystal forms of (2-amino-4, 5,6,7- tetrahydrobenzo[b]thiophen-3-yl)(4-chlorophenyl)methanone of the formula: Formula (I); processes for the production of such crystal forms; pharmaceutical compositions comprising such crystal forms; and methods of treating diseases or conditions modulated by the adenosine A1 receptor, in particular neuropathic pain, in a mammal in need thereof, by employing such crystal forms, or pharmaceutical compositions comprising such.
摘要翻译：本发明提供下式（I）的（2-氨基-4,5,6,7-四氢苯并[b]噻吩-3-基）（4-氯苯基）甲酮的结晶形式。生产这种晶形的方法; 包含这种晶体形式的药物组合物; 以及通过使用这种结晶形式治疗由有需要的哺乳动物中由腺苷A1受体调节的疾病或病症，特别是神经性疼痛的方法或包含其的药物组合物的方法。

3. 发明申请

WO2008063984A3 ALLOSTERIC MODULATORS OF THE A1 ADENOSINE RECEPTOR 审中-公开
标题翻译： A1腺苷受体的免疫调节剂
公开(公告)号：WO2008063984A3
公开(公告)日：2008-08-14
申请号：PCT/US2007084490
申请日：2007-11-13
申请人： KING PHARMACEUTICALS RES & DEV , BARALDI PIER GIOVANNI , MOORMAN ALLAN R , ROMAGNOLI ROMEO
发明人： BARALDI PIER GIOVANNI , MOORMAN ALLAN R , ROMAGNOLI ROMEO
IPC分类号： A61K31/497
CPC分类号： C07D333/36 , C07D409/12 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/113
摘要： The present invention provides compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A 1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A 1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.
摘要翻译：本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4，和Q具有本说明书中定义的含义。式（I）化合物是A 1 N 2腺苷受体的变构调节剂，因此可用于治疗由Aβ1腺苷受体介导的病症。因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛; 心脏疾病或障碍，例如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗塞和中风; 神经系统疾病或损伤; 睡眠障碍; 癫痫; 和抑郁症。

4. 发明专利

IL158186A POLYCYCLIC THIOPHENE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE FOR TREATING NEUROPATHIC PAIN IN MAMMALS 未知
公开(公告)号：IL158186A
公开(公告)日：2011-03-31
申请号：IL15818603
申请日：2003-09-30
申请人： BARALDI PIER GIOVANNI , KING PHARMACEUTICALS RES & DEV , MOORMAN ALLAN R , ROMAGNOLI ROMEO
发明人： BARALDI PIER GIOVANNI , MOORMAN ALLAN R , ROMAGNOLI ROMEO
IPC分类号： C07D333/78 , A61K31/381 , A61K31/4365 , A61K31/4743 , A61P3/10 , A61P9/00 , A61P25/00 , A61P25/02 , A61P25/20 , A61P29/00 , A61P43/00 , C07D333/74 , C07D333/80 , C07D495/06
摘要： New fused thiophene compounds are provided and methods of using those compounds for a variety of therapeutic indications. Compounds of the invention are particularly useful for treatment of neuropathic pain.

5. 发明申请

WO2008121748A3 ADENOSINE A2A RECEPTOR ANTAGONISTS 审中-公开
标题翻译：腺苷A2A受体拮抗剂
公开(公告)号：WO2008121748A3
公开(公告)日：2009-09-11
申请号：PCT/US2008058544
申请日：2008-03-28
申请人： KING PHARMACEUTICALS RES & DEV , MOORMAN ALLAN R
发明人： MOORMAN ALLAN R
IPC分类号： A01N43/50
CPC分类号： C07D487/14
摘要： The present invention provides compounds of the formula (I) wherein R1 and R2 have meaning as defined herein in the specification. The compounds of formula (I) are adenosine A2A receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2A receptor activity. Such conditions include, but are not limited to, diseases of the central nervous system such as depression, cognitive function diseases and neurodegenerative diseases such as Parkinson's disease, senile dementia as in Alzheimer's disease or psychoses and stroke. The compounds of the present invention may also be employed for the treatment of attention related disorders such as attention deficit disorder (ADD) and attention deficit hyperactivity disorder (ADHD), extra pyramidal syndrome, e.g., dystonia, akathisia, pseudoparkinsonism and tardive dyskinesia, and disorders of abnormal movement such as restless leg syndrome (RLS) and periodic limb movement in sleep (PLMS); cirrhosis, and fibrosis and fatty liver; dermal fibrosis in diseases such as scleroderma; and the mitigation of addictive behavior. In particular, the compounds of the present invention may be employed to improve motor-impairment due to neurodegenerative diseases such as Parkinson's disease.
摘要翻译：本发明提供式（I）化合物，其中R 1和R 2具有本说明书中定义的含义。式（I）化合物是腺苷A 2A受体拮抗剂，因此可用于治疗由腺苷A 2A受体活性介导的病症和疾病。这些病症包括但不限于中枢神经系统的疾病如抑郁症，认知功能疾病和神经变性疾病如帕金森病，老年痴呆症如阿尔茨海默病或精神病和中风。本发明的化合物还可用于治疗注意力相关疾病如注意力缺陷障碍（ADD）和注意缺陷多动障碍（ADHD），额外的锥体综合征，例如肌张力障碍，厌食症，假性帕金森综合征和迟发性运动障碍，以及异常运动障碍，如不宁腿综合征（RLS）和睡眠周期性肢体运动（PLMS）; 肝硬化，纤维化和脂肪肝; 皮肤纤维化等疾病如硬皮病; 并减轻上瘾行为。特别地，本发明的化合物可用于改善由于神经变性疾病如帕金森病引起的运动障碍。

6. 发明申请

WO2009108829A3 CRYSTAL FORMS OF 2-{2-[(CYCLOHEXYL)METHYLENE]HYDRAZINO}ADENOSINE 审中-公开
标题翻译： 2- {2 - [（环己基）甲基]乙酰胺}腺苷的晶体形式
公开(公告)号：WO2009108829A3
公开(公告)日：2010-06-10
申请号：PCT/US2009035396
申请日：2009-02-27
申请人： KING PHARMACEUTICALS RES & DEV , MOORMAN ALLAN R , O'NEILL MICHAEL H
发明人： MOORMAN ALLAN R , O'NEILL MICHAEL H
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07H19/167 , A61K31/7076 , A61K49/00
摘要： The present invention provides novel crystalline polymorphic forms of 2- cyclohexylmethylidenehydrazino adenosine, also known as binodenoson, methods of making the same, and methods for the manufacture of a pharmaceutical composition by employing such crystal forms, in particular, for the use of binodenoson in a subject, in need thereof, as a pharmacological stress agent to produce coronary vasodilation.
摘要翻译：本发明提供新的2-环己基亚甲基肼基腺苷的结晶多晶型物，也称为二十二碳烯酮，其制备方法，以及通过使用这种晶型来制备药物组合物的方法，特别是用于将二十二碳烯酮用于受试者，需要其作为产生冠状动脉血管扩张的药理学应激剂。

7. 发明申请

WO2008002902A2 ADENOSINE A2B RECEPTOR ANTAGONISTS 审中-公开
标题翻译：腺苷A2B受体拮抗剂
公开(公告)号：WO2008002902A2
公开(公告)日：2008-01-03
申请号：PCT/US2007/072094
申请日：2007-06-26
申请人： KING PHARMACEUTICALS RESEARCH AND DEVELOPMENT, INC. , BARALDI, Pier, Giovanni , BOREA, Pier, Andrea , MOORMAN, Allan, R , TABRIZI, Mojgan, Aghazadeh
发明人： BARALDI, Pier, Giovanni , BOREA, Pier, Andrea , MOORMAN, Allan, R , TABRIZI, Mojgan, Aghazadeh
IPC分类号： E21B33/03
CPC分类号： C07D473/06 , C07D473/08
摘要： The present invention provides compounds of the formula (I) which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A 2B receptor activity, Such conditions include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g. , asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e g , type 2 diabetes, non-insulin dependent diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e g , solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosis; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A 2B receptors, e g , retinopathy of prematurity, macuiar degeneration, and diabetic retinopathy; and cardiac diseases including hyperplasia consequent to hypertension, arteriosclerosis, and heart attack
摘要翻译：本发明提供了式（I）化合物，其为腺苷A2B受体拮抗剂，因此可用于治疗由腺苷A 2B 2B介导的病症和疾病，这些病症包括但不限于涉及肥大细胞脱粒的慢性和急性炎性疾病，例如哮喘，过敏性鼻炎和过敏性皮炎; 对胰岛素，例如2型糖尿病，非胰岛素依赖性糖尿病，糖尿病前期状态和葡萄糖耐量降低的敏感性受损; 其中血管发生是发病机制的关键组成部分的疾病，例如实体瘤和血管生成性视网膜病; 早产儿的呼吸暂停; 心肌再灌注损伤; 炎症性肠病; 自身免疫性疾病，如类风湿性关节炎，多发性硬化症和红斑狼疮; 涉及由腺苷A 2B受体介导的视网膜微血管异常的疾病，例如早产儿视网膜病，巨细胞变性和糖尿病性视网膜病; 和心脏疾病，包括因高血压，动脉硬化和心脏病发作导致的增生

8. 发明申请

WO2005028489A3 NOVEL ADENOSINE A3 RECEPTOR AGONISTS 审中-公开
标题翻译：新亚苯醌A3受体激动剂
公开(公告)号：WO2005028489A3
公开(公告)日：2006-09-28
申请号：PCT/US2004030514
申请日：2004-09-17
申请人： KING PHARMACEUTICALS RES & DEV , BARALDI PIER GIOVANNI , MOORMAN ALLAN R , BOREA PIER A
发明人： BARALDI PIER GIOVANNI , MOORMAN ALLAN R , BOREA PIER A
IPC分类号： A61K31/70 , A01N43/90 , A61K31/7076 , C07H20060101 , C07H1/00 , C07H19/16 , G01N33/74
CPC分类号： C07H19/16 , A61K31/7076 , C07H1/00 , G01N33/74 , G01N2333/726
摘要： The invention realizes that a series of sulfonamido derivatives with a conserved uronamide group at the 5' position provide superior A 3 receptor affinity as well as selectivity. These new adenosine agonists are sulfonamido deritatives N-substituted with aliphatic groups (cyclic or linear) or aromatic radicals.
摘要翻译：本发明意识到在5'位置具有保守的脲醛酰胺基团的一系列亚磺酰氨基衍生物提供优异的A 3 S 3受体亲和力以及选择性。这些新的腺苷激动剂是被脂肪族基团（环状或直链）或芳族基团N-取代的亚磺酰氨基衍生物。

9. 发明申请

WO2009137782A2 ALLOSTERIC ENHANCERS OF THE A1 ADENOSINE RECEPTOR 审中-公开
标题翻译： A1腺苷受体的独立增强剂
公开(公告)号：WO2009137782A2
公开(公告)日：2009-11-12
申请号：PCT/US2009/043320
申请日：2009-05-08
申请人： KING PHARMACEUTICALS RESEARCH AND DEVELOPMENT, INC. , BARALDI, Pier, Giovanni , MOORMAN, Allan, R. , ROMAGNOLI, Romeo
发明人： BARALDI, Pier, Giovanni , MOORMAN, Allan, R. , ROMAGNOLI, Romeo
IPC分类号： A61K31/4436 , C07D333/36 , A61K31/381 , C07D409/04 , A61P25/00
CPC分类号： C07D333/36 , C07D409/04
摘要： The present invention provides compounds of formula (I) wherein W, R 1 , R 5 and R 6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A 1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A 1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.
摘要翻译：本发明提供式（I）化合物，其中W，R 1，R 5和R 6具有本说明书中定义的含义。式（I）化合物是A1腺苷受体的变构增强子，因此可用于治疗由A1腺苷受体介导的病症。因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛，例如神经性疼痛，炎症性疼痛，心脏疾病或障碍，例如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死和中风，神经系统疾病或损伤，睡眠障碍，癫痫和抑郁症。

10. 发明申请

WO2009108829A2 CRYSTAL FORMS OF 2-{2-[(CYCLOHEXYL)METHYLENE]HYDRAZINO}ADENOSINE 审中-公开
标题翻译： 2- {2 - [（环己基）甲基]乙酰胺}腺苷的晶体形式
公开(公告)号：WO2009108829A2
公开(公告)日：2009-09-03
申请号：PCT/US2009/035396
申请日：2009-02-27
申请人： KING PHARMACEUTICALS RESEARCH AND DEVELOPMENT, INC. , MOORMAN, Allan, R. , O'NEILL, Michael, H.
发明人： MOORMAN, Allan, R. , O'NEILL, Michael, H.
IPC分类号： A61K31/7076
CPC分类号： C07H19/167 , A61K31/7076 , A61K49/00
摘要： The present invention provides novel crystalline polymorphic forms of 2- cyclohexylmethylidenehydrazino adenosine, also known as binodenoson, methods of making the same, and methods for the manufacture of a pharmaceutical composition by employing such crystal forms, in particular, for the use of binodenoson in a subject, in need thereof, as a pharmacological stress agent to produce coronary vasodilation.
摘要翻译：本发明提供新的2-环己基亚甲基肼基腺苷的结晶多晶型物，也称为二十二碳烯酮，其制备方法，以及通过使用这种晶型来制备药物组合物的方法，特别是用于将二十二碳烯酮用于受试者，需要其作为产生冠状动脉血管扩张的药理学应激剂。

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