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1. 发明授权

US06337405B1 Process for preparing 2-phenyl-3-naphthylpropionic acid derivatives 失效
标题翻译： 2-苯基-3-萘基丙酸衍生物的制备方法
公开(公告)号：US06337405B1
公开(公告)日：2002-01-08
申请号：US09742348
申请日：2000-12-22
申请人： Yukio Yokoyama , Tatsuya Kobayashi , Takeo Koyama
发明人： Yukio Yokoyama , Tatsuya Kobayashi , Takeo Koyama
IPC分类号： C07D20708
CPC分类号： C07C255/50 , C07C253/30 , C07D207/12 , Y02P20/55 , C07C255/52
摘要： A process for preparing a compound represented by general formulae (5) and (6) in the following reaction scheme or salts thereof, wherein R1 represents a protective group for a nitrogen atom; R2 represents a methanesulfonyl group or p-toluenesulfonyl group; R3 represents a hydrogen atom, an aralkyl group, or an alkyl group having 1 to 6 carbon atoms; and X represents a halogen atom. Reaction Scheme: The above process is useful as an industrial process for preparing intermediates of anticoagulant aromatic amidine derivatives described in Japanese Patent Application Laid-Open (kokai) No. 208946/1993.
摘要翻译：在下列反应方案中制备由通式（5）和（6）表示的化合物或其盐的方法，其中R 1表示氮原子的保护基; R2表示甲磺酰基或对甲苯磺酰基; R3表示氢原子，芳烷基或碳原子数1〜6的烷基。 X表示卤素原子。反应方案：上述方法可用作制备日本专利申请公开（kokai）208946/1993中所述的抗凝血芳香族脒衍生物的中间体的工业方法。

2. 发明授权

US06599910B1 Substituted triazole compounds 失效
标题翻译：取代三唑化合物
公开(公告)号：US06599910B1
公开(公告)日：2003-07-29
申请号：US09762809
申请日：2001-06-11
申请人： Jerry L. Adams , Dennis Lee
发明人： Jerry L. Adams , Dennis Lee
IPC分类号： C07D20708
CPC分类号： C07D401/04 , B82Y15/00 , C07D403/04
摘要： Novel substitued triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
摘要翻译：新型取代的三唑化合物和用作CSBP / p38激酶抑制剂治疗的组合物。

3. 发明授权

US06515142B2 Process for preparing 2-phenyl-3-naphthylpropionic acid derivatives 失效
标题翻译： 2-苯基-3-萘基丙酸衍生物的制备方法
公开(公告)号：US06515142B2
公开(公告)日：2003-02-04
申请号：US09986075
申请日：2001-11-07
申请人： Yukio Yokoyama , Tatsuya Kobayashi , Takeo Koyama
发明人： Yukio Yokoyama , Tatsuya Kobayashi , Takeo Koyama
IPC分类号： C07D20708
CPC分类号： C07C255/50 , C07C253/30 , C07D207/12 , Y02P20/55 , C07C255/52
摘要： A process for preparing a compound represented by general formulae (5) and (6) in the following reaction scheme or salts thereof, wherein R1 represents a protective group for a nitrogen atom; R2 represents a methanesulfonyl group or p-toluenesulfonyl group; R1 represents a hydrogen atom, an aralkyl group, or an alkyl group having 1 to 6 carbon atoms; and X represents a halogen atom. The above process is useful as an industrial process for preparing intermediates of anticoagulant aromatic amidine derivatives described in Japanese Patent Application Laid-Open (kokai) No. 208946/1993.
摘要翻译：在下列反应方案中制备由通式（5）和（6）表示的化合物或其盐的方法，其中R 1表示氮原子的保护基; R2表示甲磺酰基或对甲苯磺酰基; R1表示氢原子，芳烷基或碳原子数1〜6的烷基。并且X表示卤素原子。上述方法可用作制备日本专利申请公开（kokai）208946/1993中描述的抗凝血性芳族脒衍生物的中间体的工业方法。

4. 发明授权

US06350882B1 Synthesis of substituted prolines 失效
标题翻译：取代脯氨酸的合成
公开(公告)号：US06350882B1
公开(公告)日：2002-02-26
申请号：US09566220
申请日：2000-05-05
申请人： Khateeta Emerson , Guo-Jie Ho
发明人： Khateeta Emerson , Guo-Jie Ho
IPC分类号： C07D20708
CPC分类号： C07D207/16
摘要： The instant invention is directed to a process for synthesizing substituted prolines, in particular, optically pure substituted prolines, which comprises the steps of: a) adding an unsubstituted or substituted proline alkali salt and an alkali halide to a solution of dialkylacylamidomalonate; and b) adding &agr;, &bgr; unsaturated aldehyde to produce an adduct.
摘要翻译：本发明涉及一种合成取代的脯氨酸，特别是光学纯取代的脯氨酸的方法，该方法包括以下步骤：a）将未取代或取代的脯氨酸碱金属盐和碱金属卤化物加入到二烷基酰氨基马来酸酐的溶液中; 和b）加入α，β不饱和醛以产生加合物。

5. 发明授权

US06255496B1 Trifluoromethyl ketone analogs as selective cPLA2 inhibitors 失效
标题翻译：三氟甲基酮类似物作为选择性cPLA2抑制剂
公开(公告)号：US06255496B1
公开(公告)日：2001-07-03
申请号：US09300111
申请日：1999-04-27
申请人： Jacques Banville , Yonghua Gai , Graham Johnson , Fred Christopher Zusi , James R. Burke
发明人： Jacques Banville , Yonghua Gai , Graham Johnson , Fred Christopher Zusi , James R. Burke
IPC分类号： C07D20708
CPC分类号： C07D207/08 , C07C17/269 , C07C25/18 , C07C45/515 , C07C45/673 , C07C45/74 , C07C49/245 , C07C49/248 , C07C49/255 , C07C69/63 , C07C69/712 , C07C69/738 , C07C217/22 , C07C229/12 , C07C233/18 , C07C235/20 , C07C311/04 , C07C317/18 , C07C323/12 , C07D207/12 , C07D207/16 , C07D211/14 , C07D211/46 , C07D215/14 , C07D231/12 , C07D271/06 , C07D277/04 , C07D311/20 , C07D313/08 , C07D317/34 , C07F7/1804 , C07F9/113 , C07F9/2458
摘要： Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula
摘要翻译：提供cPLA2酶的选择性抑制剂，其可用于控制多种炎性疾病。本发明的抑制剂具有通式

6. 发明授权

US06429317B1 Indane derivatives for antipsychotic compositions 失效
标题翻译：吲哚衍生物用于抗精神病药物组合物
公开(公告)号：US06429317B1
公开(公告)日：2002-08-06
申请号：US09117089
申请日：2000-09-05
申请人： Sean P. Hollinshead , Michael A. Staszak , John S. Ward , Joseph W. Wilson , Bret E. Huff , Philip F. Hughes , Jose S. Mendoza , Charles H. Mitch
发明人： Sean P. Hollinshead , Michael A. Staszak , John S. Ward , Joseph W. Wilson , Bret E. Huff , Philip F. Hughes , Jose S. Mendoza , Charles H. Mitch
IPC分类号： C07D20708
CPC分类号： C07D213/82 , C07C257/12 , C07C311/20 , C07C2602/08 , C07C2602/10 , C07D295/13 , C07D333/38 , C07D333/70 , C40B40/00
摘要： The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.
摘要翻译：本发明提供了可用于治疗与调节毒蕈碱受体相关的精神病和其它病症的新型吲哚类化合物。本发明提供了使用新化合物的制剂和方法。

7. 发明授权

US06316490B1 Substituted aryl compounds useful as modulators of acetylcholine receptors 失效
标题翻译：可用作乙酰胆碱受体调节剂的取代芳基化合物
公开(公告)号：US06316490B1
公开(公告)日：2001-11-13
申请号：US08860954
申请日：1997-07-08
申请人： Jean-Michel Vernier , Ian A. McDonald
发明人： Jean-Michel Vernier , Ian A. McDonald
IPC分类号： C07D20708
CPC分类号： B64C23/06 , Y02T50/162
摘要： In accordance with the present invention, a novel class of substituted aryl compounds (containing ether, ester, amide, ketone or thioether substitution) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect, compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of displacing one or more acetylcholine receptor ligands, e.g., 3H-nicotine, from mammalian neuronal membrane binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors. Therapeutic indications for compounds with activity as acetylcholine receptors include diseases of the central nervous system such as Alzheimer's disease and other diseases involving memory loss and/or dementia (including AIDS dementia); cognitive dysfunction (including disorders of attention, focus and concentration), disorders of extrapyramidal motor function such as Parkinson's disease, progressive supramuscular palsy, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, anxiety and psychosis; substance abuse including withdrawal symptoms and substitution therapy; neurocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of nociception and control of pain; autonomic disorders including dysfimction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma, cardiovascular dysfunction including hypertension and cardiac arrhythmias, as well as co-medication uses in surgical applications.
摘要翻译：根据本发明，已经发现了促进参与神经传递的配体释放的新一类取代的芳基化合物（含有醚，酯，酰胺，酮或硫醚取代基）。在特定方面，本发明的化合物能调节乙酰胆碱受体。本发明的化合物能够从哺乳动物神经元膜结合位点置换一个或多个乙酰胆碱受体配体，例如3H-烟碱。本发明化合物可以充当乙酰胆碱受体的激动剂，部分激动剂，拮抗剂或变构调节剂。具有作为乙酰胆碱受体活性的化合物的治疗适应症包括中枢神经系统的疾病如阿尔茨海默病和涉及记忆丧失和/或痴呆（包括AIDS痴呆）的其它疾病; 认知功能障碍（包括注意力集中和集中注意力障碍），帕特森氏病，锥体运动功能障碍，进行性肌肉麻痹，亨廷顿疾病，吉列斯·杜列特综合征和迟发性运动障碍; 情绪和情绪障碍，如抑郁，焦虑和精神病; 药物滥用，包括戒断症状和替代治疗; 神经分泌障碍和食物摄入异常，包括贪食症和厌食症; 伤害感受障碍和疼痛控制; 自主神经障碍包括消化道运动功能障碍和功能如炎症性肠病，肠易激综合征，腹泻，便秘，胃酸分泌和溃疡; 嗜铬细胞瘤，包括高血压和心律失常的心血管功能障碍，以及在外科应用中的共用药用途。

8. 发明授权

US06479667B2 Crystalline forms of antibiotic side chain intermediates 失效
标题翻译：抗生素侧链中间体的结晶形式
公开(公告)号：US06479667B2
公开(公告)日：2002-11-12
申请号：US09796006
申请日：2001-02-28
申请人： Karel J. M. Brands , Karen M. Conrad , John M. Williams
发明人： Karel J. M. Brands , Karen M. Conrad , John M. Williams
IPC分类号： C07D20708
CPC分类号： C07D207/16
摘要： Crystalline 2S-cis-3-[[(4-mercapto-2-pyrrolidinyl)carbonyl]-amino]benzoic acid and salts and solvates thereof are disclosed. A crystalline type is described.
摘要翻译：公开了结晶2S-顺-3 - [[（4-巯基-2-吡咯烷基）羰基] - 氨基]苯甲酸及其盐和溶剂合物。描述了晶体类型。

9. 发明授权

US06455472B1 Phenyl-substituted cyclic enaminones 失效
标题翻译：苯基取代的环状烯胺
公开(公告)号：US06455472B1
公开(公告)日：2002-09-24
申请号：US09831261
申请日：2001-07-16
申请人： Reiner Fischer , Ralf Wischnat , Mark Wilhelm Drewes , Markus Dollinger , Christoph Erdelen , Dieter Feucht , Ingo Wetcholowsky , Ulrike Wachendorff-Neumann , Ulrich Philipp , Olga-Tatjana Rauch
发明人： Reiner Fischer , Ralf Wischnat , Mark Wilhelm Drewes , Markus Dollinger , Christoph Erdelen , Dieter Feucht , Ingo Wetcholowsky , Ulrike Wachendorff-Neumann , Ulrich Philipp , Olga-Tatjana Rauch
IPC分类号： C07D20708
CPC分类号： C07D401/06 , C07C255/40 , C07C317/44 , C07C323/62 , C07D207/20 , C07D207/22 , C07D211/70 , C07D215/14 , C07D223/04 , C07D401/10 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D417/14 , E04B1/043
摘要： The present invention relates to novel phenyl-substituted cyclic enaminones of the formula (I): in which Ar, X, Z, Y, K, n and m are each as defined in the description, to a plurality of processes and intermediates for their preparation and to their use as herbicides and pesticides.
摘要翻译：本发明涉及式（I）的新型苯基取代的环状烯胺：其中Ar，X，Z，Y，K，n和m各自如说明书中所定义，涉及多种制备方法和中间体并用作除草剂和杀虫剂。

10. 发明授权

US06291511B1 Biarylalkanoic acids as cell adhesion inhibitors 失效
标题翻译：双芳基链烷酸作为细胞粘附抑制剂
公开(公告)号：US06291511B1
公开(公告)日：2001-09-18
申请号：US09359015
申请日：1999-07-22
申请人： Philippe L. Durette , William K. Hagmann , Malcolm MacCoss , Sander G. Mills , Richard A. Mumford
发明人： Philippe L. Durette , William K. Hagmann , Malcolm MacCoss , Sander G. Mills , Richard A. Mumford
IPC分类号： C07D20708
CPC分类号： C07K5/06165 , A61K38/00 , C07K5/06139 , C07K5/06191
摘要： Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
摘要翻译：式I的化合物是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。这些化合物可以配制成药物组合物，并且适用于治疗哮喘，过敏，炎症，多发性硬化以及其它炎性和自身免疫性疾病。

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