公开(公告)号：US07144882B2

公开(公告)日：2006-12-05

申请号：US10336532

申请日：2003-01-03

申请人： Jotham Wadsworth Coe ,  Paige Roanne Palmer Brooks

发明人： Jotham Wadsworth Coe ,  Paige Roanne Palmer Brooks

IPC分类号： A61P25/30 ,  A61K31/495 ,  A61K31/44 ,  C07D241/36 ,  C07D221/22

CPC分类号： C07D513/08 ,  C07D221/22 ,  C07D221/24 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/04 ,  C07D471/08

摘要： This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

摘要翻译： 本发明涉及式（I）化合物及其可药用盐，其中R 1，R 2和R 3， 如本文所定义; 用于合成这些化合物的中间体，含有这些化合物的药物组合物; 以及使用这些化合物治疗神经和心理障碍的方法。

公开(公告)号：US20060270851A1

公开(公告)日：2006-11-30

申请号：US10571863

申请日：2004-08-16

申请人： Ernest Cleugh

发明人： Ernest Cleugh

IPC分类号： C07D241/36 ,  C07D263/52 ,  C07D213/78 ,  C07C69/76

CPC分类号： C07D213/643 ,  C07C51/367 ,  C07C59/68

摘要： A process for producing optically pure R-hydroxyphenoxypropanoic acid or a salt or ester thereof by reaction of hydroquinone or a salt thereof with an S-halopropanoic acid or a salt thereof in the presence of a mild reducing agent.

摘要翻译： 在温和还原剂存在下，通过氢醌或其盐与S-卤代丙酸或其盐的反应制备光学纯的R-羟基苯氧基丙酸或其盐或酯的方法。

公开(公告)号：US20060229311A1

公开(公告)日：2006-10-12

申请号：US11453892

申请日：2006-06-16

申请人： Mette Gronborg ,  Dan Peters ,  Arne Moller

发明人： Mette Gronborg ,  Dan Peters ,  Arne Moller

IPC分类号： A61K31/498 ,  A61K31/404 ,  C07D241/36 ,  C07D209/44

CPC分类号： C07D471/04 ,  C07D209/60 ,  C07D487/04

摘要： The present invention relates to novel isatin derivatives, pharmaceutical compositions comprising the isatin derivatives of the invention, methods of preparing the isatin derivatives of the invention, their use in the treatment of neurodegenerative diseases and for the regeneration or prevention of degeneration of lesioned and damaged neurons, and methods of treatment of neurodegenerative diseases and for the regeneration or prevention of degeneration of lesioned and damaged neurons.

公开(公告)号：US07071180B2

公开(公告)日：2006-07-04

申请号：US10873852

申请日：2004-06-22

申请人： Björn Nilsson ,  Jan Tejbrant ,  Benjamin Pelcman ,  Erik Ringberg ,  Markus Thor ,  Jonas Nilsson ,  Mattias Jönsson

发明人： Björn Nilsson ,  Jan Tejbrant ,  Benjamin Pelcman ,  Erik Ringberg ,  Markus Thor ,  Jonas Nilsson ,  Mattias Jönsson

IPC分类号： A61K31/33 ,  A61K31/502 ,  A61K31/497 ,  C07D401/04 ,  C07D241/36

CPC分类号： C07D401/12 ,  C07D241/18 ,  C07D241/20 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/04

摘要： The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).

公开(公告)号：US20060058524A1

公开(公告)日：2006-03-16

申请号：US10526955

申请日：2003-08-20

申请人： Aurelie Falcou ,  Jochen Schwaiget ,  Andrea Ritter

发明人： Aurelie Falcou ,  Jochen Schwaiget ,  Andrea Ritter

IPC分类号： C07D271/12 ,  C07D239/02 ,  C07D241/36

CPC分类号： C08G61/122 ,  C08G61/02 ,  C08G61/128 ,  C09K11/06 ,  C09K2211/1408 ,  C09K2211/1416 ,  C09K2211/1425 ,  C09K2211/1433 ,  H01L51/0039 ,  H01L51/005 ,  H01L51/0052 ,  H01L51/0059

摘要： The present invention relates to a process for preparing aryl-aryl-coupled compounds and materials. These materials play an important role in industry, for instance as liquid crystals, pharmaceuticals, agrochemicals and as organic semiconductors. The aryl-aryl couplings hitherto carried out by means of Yamamoto coupling require specific additives in order to give a product suitable for the subsequent use. Particularly in the electronics industry, the Yamamoto coupling needs to meet particular requirements.

摘要翻译： 芳基 - 芳基偶合化合物和材料的制备方法技术领域本发明涉及芳基 - 芳基偶合化合物和材料的制备方法。 这些材料在工业中起着重要作用，例如液晶，药物，农用化学品和有机半导体。 迄今为止通过Yamamoto联结进行的芳基 - 芳基偶合物需要特定的添加剂，以便产生适于随后使用的产品。 特别是在电子行业中，山本联轴器需要满足特殊要求。

公开(公告)号：US20050288294A1

公开(公告)日：2005-12-29

申请号：US10530252

申请日：2003-10-24

申请人： Mark Duggan ,  Craig Lindsley ,  Zhijian Zhao

发明人： Mark Duggan ,  Craig Lindsley ,  Zhijian Zhao

IPC分类号： A61K31/495 ,  A61K31/498 ,  A61K45/06 ,  C07D241/36 ,  C07D487/02 ,  C07D487/04 ,  C07D495/04 ,  C07D519/00

CPC分类号： A61K31/495 ,  A61K45/06 ,  C07D487/04 ,  C07D495/04

摘要： The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyrazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

摘要翻译： 本发明涉及含有与被抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代的吡嗪部分稠合的五元杂环的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。

公开(公告)号：US20050227335A1

公开(公告)日：2005-10-13

申请号：US10888786

申请日：2004-07-09

申请人： Natarajan Sakthivel ,  Radhakrishnan Kumar

发明人： Natarajan Sakthivel ,  Radhakrishnan Kumar

IPC分类号： C07D241/36 ,  C07D241/46 ,  C07D487/04 ,  C12P17/16 ,  C12P17/18

CPC分类号： C12P17/182

摘要： A dimer of phenazine-1-carboyxlic acid natural products from fluorescent pseudomonad bacterium and a method of preparing a dimer of phenazine-1-carboxylic acid natural product are disclosed herein. The method comprises growing the bacterium in a water based liquid medium under favorable pH and temperature with continuous agitation, extracting the dimer of phenazine-1-carboyxlic acid natural product from the medium by centrifugation using organic solvents, filtering the resultant emulsion to separate the aqueous layer in a separation funnel, isolating the crude dimer of phenazine-1-carboyxlic acid natural product from the organic layer by evaporating the organic solvent, and purifying the dimer of phenazine-1-carboxylic acid natural product by chromatography.

摘要翻译： 本文公开了荧光假单胞菌属的吩嗪-1-羧酸天然产物的二聚体和吩嗪-1-羧酸天然产物的二聚体的制备方法。 该方法包括在有利的pH和温度下在连续搅拌下在水基液体培养基中生长细菌，通过使用有机溶剂离心从培养基中提取吩嗪-1-甲氧基酸天然产物的二聚体，过滤所得乳液以分离水溶液 层，分离漏斗，通过蒸发有机溶剂从有机层中分离出吩嗪-1-羧酸天然产物的粗二聚体，并通过色谱法纯化吩嗪-1-羧酸天然产物的二聚体。

公开(公告)号：US06903099B2

公开(公告)日：2005-06-07

申请号：US10297735

申请日：2001-05-15

申请人： Mark W. Orme ,  Jason Scott Sawyer ,  Lisa M. Schultze

发明人： Mark W. Orme ,  Jason Scott Sawyer ,  Lisa M. Schultze

IPC分类号： A61K31/4985 ,  A61P1/04 ,  A61P9/00 ,  A61P15/00 ,  A61P15/08 ,  A61P15/10 ,  A61P37/08 ,  C07D471/04 ,  C07D471/14 ,  C07D471/22 ,  C07D487/14 ,  C07D491/14 ,  C07D491/147 ,  C07D495/14 ,  A61K31/50 ,  C07D241/36

CPC分类号： C07D471/04 ,  C07D471/14 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14

摘要： Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.

摘要翻译： 一般结构式（I）的化合物及其化合物及其盐和溶剂化物的用途作为治疗剂。

公开(公告)号：US20050038032A1

公开(公告)日：2005-02-17

申请号：US10910925

申请日：2004-08-04

申请人： Brett Allison ,  Michael Hack ,  Victor Phuong ,  Michael Rabinowitz ,  Mark Rosen

发明人： Brett Allison ,  Michael Hack ,  Victor Phuong ,  Michael Rabinowitz ,  Mark Rosen

IPC分类号： A61P1/04 ,  A61P1/18 ,  A61P25/22 ,  C07D241/42 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  A61K31/498 ,  C07D241/36

CPC分类号： C04B35/632 ,  C07D241/42 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： Certain amidophenyl-sulfonylamino-quinoxaline compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.

摘要翻译： 苯基磺酰氨基 - 喹喔啉化合物中的某些化合物是可用于治疗CCK2介导的疾病的CCK2调节剂。

公开(公告)号：US06852712B2

公开(公告)日：2005-02-08

申请号：US10357882

申请日：2003-02-04

申请人： Michael R. Myers ,  Wei He ,  Alfred P. Spada ,  Martin P. Maguire

发明人： Michael R. Myers ,  Wei He ,  Alfred P. Spada ,  Martin P. Maguire

IPC分类号： A61F2/84 ,  A61K31/47 ,  A61K31/495 ,  A61K31/498 ,  A61K31/5377 ,  A61M25/00 ,  A61P9/00 ,  A61P9/10 ,  A61P17/06 ,  A61P19/08 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07D215/20 ,  C07D215/38 ,  C07D241/42 ,  C07D241/44 ,  C07D241/52 ,  C07D241/54 ,  C07D403/04 ,  C07D405/10 ,  C07D405/12 ,  C07D453/06 ,  C07D471/08 ,  A61K31/33 ,  C07D241/36

CPC分类号： C07D215/38 ,  C07D215/20 ,  C07D241/42 ,  C07D241/44 ,  C07D241/52 ,  C07D241/54 ,  C07D403/04 ,  C07D405/12 ,  C07D453/06

摘要： This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.

摘要翻译： 本发明涉及抑制血小板衍生生长因子或p56酪氨酸激酶活性的喹啉/喹喔啉化合物，包含这些化合物的药物组合物，以及这些化合物用于治疗患有或患有疾病/ 涉及细胞分化，增殖，细胞外基质产生或介体释放和/或T细胞活化和增殖的条件。