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1. 发明申请

US20040067972A1 Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US20040067972A1
公开(公告)日：2004-04-08
申请号：US10425376
申请日：2003-04-28
申请人： Schering Corporation
发明人： Craig D. Boyle , William J. Greenlee , Samuel Chackalamannil
IPC分类号： A61K031/4747 , C07D471/12
CPC分类号： C07D221/20 , C07D211/96
摘要： The invention described herein are compounds in accordance with formula I: 1 wherein R1, R2, R3, R4, R5, R6, R2, R8, R9, n, X, and Z are as defined herein, pharmaceutical compositions containing at least one compound of formula I, methods of preparation thereof, and methods of treating disorders with at least one compound of formula I or at least one compound of formula I in association with at least one acetylcholinesterase inhibitor.
摘要翻译：本文所述的本发明是根据式I的化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 2， 8，R 9，n，X和Z如本文所定义，含有至少一种式I化合物的药物组合物，其制备方法，以及用至少一种式I化合物治疗病症的方法或至少一种式I化合物与至少一种乙酰胆碱酯酶抑制剂联合。

2. 发明申请

US20040176418A1 Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist 有权
标题翻译：凝血酶受体拮抗剂硫酸氢盐的结晶多晶型物
公开(公告)号：US20040176418A1
公开(公告)日：2004-09-09
申请号：US10755066
申请日：2004-01-09
申请人： Schering Corporation
发明人： Tiruvettipuram K. Thiruvengadam , Wenxue Wu , Tao Wang , John S. Chiu , Susan Bogdanowich-Knipp , Anastasia Pavlovsky , William J. Greenlee , Michael P. Graziano , Teddy Kosoglou , Madhu Chintala , Samuel Chackalamannil
IPC分类号： C07D45/02 , A61K031/4433
CPC分类号： C07D417/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06 , C07D405/14 , C07D413/14
摘要： A crystalline polymorph of a bislulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. 1, or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG. 3, and is represented by the formula for Compound 2: 1 and processes for preparing Compound 2 are disclosed. Pharmaceutical compositions comprising the polymorph of the bisulfate salt and at least one excipient or carrier, and methods of using the polymorph of Compound 2 to treat a variety of physiological disorders, such as thrombosis, are also disclosed.
摘要翻译：凝血酶受体拮抗剂化合物的双硫酸盐的结晶多晶型物，其呈现与图1所示基本相同的粉末x射线衍射图。 1，或者显示与图1所示基本相同的差示扫描量热分析图。 3，由化合物2的式表示：公开了制备化合物2的方法。还公开了包含硫酸氢盐和至少一种赋形剂或载体的多晶型物的药物组合物，以及使用化合物2的多晶型物来治疗各种生理学疾病如血栓形成的方法。

3. 发明申请

US20040058906A1 Selective D1/D5 receptor antagonists for the treatment of obesity and CNS disorders 失效
标题翻译：选择性D1 / D5受体拮抗剂用于治疗肥胖和CNS疾病
公开(公告)号：US20040058906A1
公开(公告)日：2004-03-25
申请号：US10649495
申请日：2003-08-27
申请人： Schering Corporation
发明人： Wen-Lian Wu , Duane A. Burnett , William J. Greenlee , Thavalakulam K. Sasikumar
IPC分类号： A61K031/55 , C07D487/02
CPC分类号： C07D487/04 , C07D513/04
摘要： The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
摘要翻译：本发明提供了作为D1 / D5受体的新型拮抗剂的化合物以及制备这些化合物的方法。在另一个实施方案中，本发明提供包含这种D1 / D5受体拮抗剂的药物组合物以及使用它们治疗CNS障碍，肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

4. 发明申请

US20030216437A1 Thrombin receptor antagonists 有权
标题翻译：凝血酶受体拮抗剂
公开(公告)号：US20030216437A1
公开(公告)日：2003-11-20
申请号：US10412982
申请日：2003-04-14
申请人： SCHERING CORPORATION
发明人： Samuel Chackalamannil , Martin C. Clasby , William J. Greenlee , Yuguang Wang , Yan Xia , Enrico P. Veltri , Mariappan V. Chelliah
IPC分类号： A61K031/444 , A61K031/4433 , A61K031/365 , C07D45/14 , C07D45/02
CPC分类号： C07D405/06 , C07D405/14 , C07D417/14
摘要： Heterocyclic-substituted tricyclics of the formula 1 or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond; n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1-C6)alkyl, (C3-C8)cycloalkyl, nullOH, (C1-C6)alkoxy, R27-aryl(C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译：具有下式的杂环取代的三环或其药学上可接受的盐，其中：虚线表示任选的单键; 表示可选的双键; n为0-2; Q是环烷基，任选被R 13和R 14取代; R 13和R 14独立地选自（C 1 -C 6）烷基，（C 3 -C 8）环烷基，-OH，（C 1 -C 6）烷氧基，R 27 - 芳基（C 1 -C 6）杂芳基，杂芳基烷基，杂环基，杂环基烷基，卤素和卤代烷基; 或R 13和R 14一起形成3-6个原子的螺环或异环环; Het是单或双环任选取代的杂芳基; 和B是键，亚烷基或任选取代的亚烯基或亚炔基，其中剩余的取代基如说明书中所定义，以及含有它们的药物组合物和治疗与血栓形成，动脉粥样硬化，再狭窄有关的疾病的方法，高血压，心绞痛，心律失常，心力衰竭和癌症。还要求与其它心血管药物联合治疗。

5. 发明申请

US20030212059A1 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US20030212059A1
公开(公告)日：2003-11-13
申请号：US10304931
申请日：2002-11-26
申请人： Schering Corporation
发明人： Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Unmesh G. Shah , Yan Xia
IPC分类号： A61K031/55 , A61K031/519 , C07D487/14
CPC分类号： C07D487/14
摘要： Disclosed herein are compounds having the structural formula A 1 including pharmaceutically acceptable salts or solvates of said compound, wherein X, Y, Q and R are as defined in the specification; pharmaceutical compositions thereof; methods of treating central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment, and processes for preparing the compound of this invention.
摘要翻译：本文公开的是具有结构式A的化合物，包括所述化合物的药学上可接受的盐或溶剂合物，其中X，Y，Q和R如说明书中所定义; 其药物组合物; 通过将本发明化合物给予需要这种治疗的患者来治疗中枢神经系统疾病的方法，以及制备本发明化合物的方法。

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