公开(公告)号：US20060016025A1

公开(公告)日：2006-01-26

申请号：US11159267

申请日：2005-06-23

申请人： Andrew Greaves ,  Herve David

发明人： Andrew Greaves ,  Herve David

IPC分类号： A61K7/13 ,  C09B44/02 ,  C07D43/14

CPC分类号： C09B44/16 ,  A61K8/4926 ,  A61K8/4946 ,  A61K2800/4324 ,  A61Q5/065 ,  A61Q5/10 ,  C07D401/14 ,  C09B44/126 ,  C09B67/0076

摘要： Disclosed are cationic diazo compounds of the following formula Dye1-LK-Dye2  (I) in which Dye1 and Dye2 represent: Also herein disclosed are dye compositions comprising the cationic diazo compounds as direct dye, a process for dyeing keratin fibers using this composition, and a multi-compartment device.

摘要翻译： 公开了下列式的阳离子重氮化合物：式中：“In-line formula”end =“lead”→Dye1-LK-Dye2（I）<？in-line-formula description =“In Dyl1和Dye2代表的“-line”=“tail”？>，其中还公开了包含阳离子重氮化合物作为直接染料的染料组合物，使用该组合物染色角蛋白纤维的方法和多室装置。

公开(公告)号：US20060009453A1

公开(公告)日：2006-01-12

申请号：US11126000

申请日：2005-05-09

申请人： Stephanie Geuns-Meyer ,  Brian Hodous ,  Stuart Chaffee ,  Paul Tempest ,  Philip Olivieri ,  Rebecca Johnson ,  Brian Albrecht ,  Vinod Patel ,  Victor Cee ,  Joseph Kim ,  Steven Bellon ,  Xiaotian Zhu ,  Yuan Cheng ,  Ning Xi ,  Karina Romero ,  Hanh Nguyen ,  Holly Deak

发明人： Stephanie Geuns-Meyer ,  Brian Hodous ,  Stuart Chaffee ,  Paul Tempest ,  Philip Olivieri ,  Rebecca Johnson ,  Brian Albrecht ,  Vinod Patel ,  Victor Cee ,  Joseph Kim ,  Steven Bellon ,  Xiaotian Zhu ,  Yuan Cheng ,  Ning Xi ,  Karina Romero ,  Hanh Nguyen ,  Holly Deak

IPC分类号： A61K31/53 ,  A61K31/506 ,  C07D43/14

CPC分类号： C07D213/73 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04

摘要： The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other poliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.

摘要翻译： 本发明涉及具有通式I的化合物，其中A，B，D，E，G，H 1-5和R 1-4如本文所定义， 和合成中间体，其能够调节各种蛋白激酶受体酶，从而影响与这些激酶的活性相关的各种疾病状态和状况。 例如，这些化合物能够调节激酶，从而影响血管生成过程并治疗血管生成相关疾病和其它包括癌症和炎症的复发性疾病。 本发明还包括药物组合物，包括该化合物，以及治疗与蛋白激酶活性有关的疾病状态的方法。

公开(公告)号：US20060004043A1

公开(公告)日：2006-01-05

申请号：US10993981

申请日：2004-11-19

申请人： Shripad Bhagwat ,  Yoshitaka Satoh ,  Steven Sakata ,  Chris Buhr ,  Ronald Albers ,  John Sapienza ,  Veronique Plantevin ,  Qi Chao ,  Kiran Sahasrabudhe ,  Rachel Stengone ,  Rama Narla

发明人： Shripad Bhagwat ,  Yoshitaka Satoh ,  Steven Sakata ,  Chris Buhr ,  Ronald Albers ,  John Sapienza ,  Veronique Plantevin ,  Qi Chao ,  Kiran Sahasrabudhe ,  Rachel Stengone ,  Rama Narla

IPC分类号： C07D215/12 ,  C07D43/14 ,  A61K31/4709 ,  A61K31/4196

CPC分类号： C07D403/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

摘要： This invention is directed to Indazole Compounds or pharmaceutically acceptable salts, solvates and hydrates thereof. The Indazole Compounds have utility in the treatment or prevention of a wide range of diseases and disorders that are responsive to the inhibition, modulation or regulation of kinases, such as inflammatory diseases, abnormal angiogenesis and diseases related thereto, cancer, atherosclerosis, a cardiovascular disease, a renal disease, an autoimmune condition, macular degeneration, disease-related wasting, an asbestos-related condition, pulmonary hypertension, diabetes, obesity, pain and others. Thus, methods of treating or preventing such diseases and disorders are also disclosed, as are pharmaceutical compositions comprising one or more of the Indazole Compounds. This invention is based, in part, upon the discovery of a novel class of 5-triazolyl substituted indazole molecules that have potent activity with respect to the modulation of protein kinases. Thus, the invention encompasses orally active molecules as well as parenterally active molecules which can be used at lower doses or serum concentrations for treating diseses or disorders associated with protein kinase signal transduction.

摘要翻译： 本发明涉及吲唑化合物或其药学上可接受的盐，溶剂化物和水合物。 吲唑化合物可用于治疗或预防对抑制，调节或调节激酶（例如炎性疾病，异常血管生成和与之相关的疾病，癌症，动脉粥样硬化，心血管疾病）的各种疾病和病症 肾脏疾病，自身免疫性疾病，黄斑变性，疾病相关性消耗，石棉相关病症，肺动脉高压，糖尿病，肥胖，疼痛等。 因此，还公开了治疗或预防这些疾病和病症的方法，以及包含一种或多种吲唑化合物的药物组合物。 本发明部分基于发现关于蛋白激酶调节具有强力活性的新一类5-三唑基取代的吲唑分子。 因此，本发明包括口服活性分子以及肠胃外活性分子，其可以以较低剂量或血清浓度使用，用于治疗与蛋白激酶信号转导相关的疾病或障碍。

公开(公告)号：US20050256310A1

公开(公告)日：2005-11-17

申请号：US11129277

申请日：2005-05-12

申请人： Bernard Hulin ,  David Piotrowski

发明人： Bernard Hulin ,  David Piotrowski

IPC分类号： C07D207/14 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/02 ,  C07D487/04 ,  C07D487/14 ,  C07D498/04 ,  C07D43/14

CPC分类号： C07D207/14 ,  C07D275/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.

摘要翻译： 本发明提供式（I）化合物，其前体药物和立体异构体，以及化合物，前药和立体异构体的药学上可接受的盐，其中R 1，R 2， R 3，HET，n，Q，X，Y和Z如本文所述; 组合物; 及其用于治疗糖尿病性神经病变，糖尿病性肾病，糖尿病性微血管病变等糖尿病并发症的用途。

公开(公告)号：US20050215546A1

公开(公告)日：2005-09-29

申请号：US11138868

申请日：2005-05-26

申请人： Rudolf Hurnaus ,  Klaus Rudolf ,  Stephan Mueller ,  Dirk Stenkamp ,  Phillipp Lustenberger ,  Alexander Dreyer ,  Kai Gerlach ,  Marcus Schindler ,  Kirsten Arndt ,  Eckhart Bauer

发明人： Rudolf Hurnaus ,  Klaus Rudolf ,  Stephan Mueller ,  Dirk Stenkamp ,  Phillipp Lustenberger ,  Alexander Dreyer ,  Kai Gerlach ,  Marcus Schindler ,  Kirsten Arndt ,  Eckhart Bauer

IPC分类号： C07D401/14 ,  C07D471/04 ,  A61K31/5513 ,  A61K31/517 ,  C07D43/14

CPC分类号： C07D471/04 ,  C07D401/14

摘要： The present invention relates to substituted piperidines of general formula wherein R, R2 to R5, A, X, Z and n are defined as in claim 1, the tautomers, diastereomers, enantiomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.

摘要翻译： 本发明涉及通式如下的取代的哌啶：其中R，R 2至R 5，A，X，Z和n如权利要求1所定义，互变异构体， 非对映异构体，对映异构体，其混合物和盐，特别是其与具有有价值的药理学特性，特别是CGRP拮抗性质的无机或有机酸或碱的生理上可接受的盐，含有这些化合物的药物组合物，其用途及其制备方法。

公开(公告)号：US20050209452A1

公开(公告)日：2005-09-22

申请号：US10502291

申请日：2003-01-22

申请人： Klaus Bornsen ,  Peter End ,  Gerhard Gross ,  Ulrike Pfaar ,  Paul Manley ,  Jurg Zimmermann

发明人： Klaus Bornsen ,  Peter End ,  Gerhard Gross ,  Ulrike Pfaar ,  Paul Manley ,  Jurg Zimmermann

IPC分类号： A61K31/506 ,  A61P9/10 ,  A61P11/00 ,  A61P35/00 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  A61K31/5377 ,  C07D413/14 ,  C07D43/14

CPC分类号： C07D401/04 ,  C07D401/14

摘要： The invention relates to N-phenyl-2-pyrimidine-amine derivatives in which at least one nitrogen atom carries an oxygen atom to form the corresponding N-oxides, to processes for the preparation thereof, to pharmaceutical compositions comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.

摘要翻译： 本发明涉及N-苯基-2-嘧啶 - 胺衍生物，其中至少一个氮原子携带氧原子以形成相应的N-氧化物，其制备方法，包含这些化合物的药物组合物，以及 其用于制备用于治疗治疗温血动物（包括人）的药物组合物。

公开(公告)号：US20050203221A1

公开(公告)日：2005-09-15

申请号：US10515898

申请日：2003-06-03

申请人： Fabienne Cuesta ,  Roland Naef ,  Ted Deisenroth ,  Peter Rohringer ,  Marc Grienenberger ,  Serge Schroeder

发明人： Fabienne Cuesta ,  Roland Naef ,  Ted Deisenroth ,  Peter Rohringer ,  Marc Grienenberger ,  Serge Schroeder

IPC分类号： C09B23/14 ,  C09B57/00 ,  C09B67/24 ,  C09B69/10 ,  D06L3/12 ,  D06M13/355 ,  D06M15/423 ,  D06P1/44 ,  D21H17/51 ,  D21H19/36 ,  D21H19/42 ,  D21H21/30 ,  C07D413/14 ,  C08K5/34 ,  C07D43/14

CPC分类号： D06P1/44 ,  D06L4/60 ,  D06M13/355 ,  D21H19/42 ,  D21H21/30

摘要： The present invention relates to novel whitening pigments comprising the reaction product of (a) a melamine-formaldehyde and/or a melamine-urea polycondensation product and (b) a water-soluble fluorescent whitening agent of the formula (1) wherein R1 represents —OH, —OC1-C4alkyl, —Oaryl, —NH2, —NHC1-C4alkyl, —N(C1-C4alkyl)2, —NHC2-C4hydroxyalkyl, —N(C2-C4hydroxyalkyl)2, —N(C1-C4alkyl)(C2-C4hydroxyalkyl), —NHC1-C4alkoxy-C1-C4alkyl, —N(C1-C4alkoxy-C1-C4alkyl)2, morpholino, piperidino, pyrrolidino or the residue of an amino acid from which a hydrogen atom has been abstracted from the amino group, R2 represents —CONH2, —CONHC1-C4alkyl, —COOM, —SO2NH2 or —SO2NHC1-C4alkyl and M is hydrogen, sodium, potassium, calcium, magnesium, ammonium, mono-di-, tri- or tetra-substituted C1-C4alkylammonium or C2-C4hydroxyalkylammonium or mixtures thereof, a process for preparation of the whitening pigments and their use for the fluorescent whitening of paper, especially in coating, for the fluorescent whitening and improvement of sun protection factors of textile materials and for improving the aspect of solid detergent compositions. Further disclosed are certain novel fluorescent whitening agents suitable for preparation of the whitening pigments and a process for their preparation.

公开(公告)号：US20050192305A1

公开(公告)日：2005-09-01

申请号：US11111400

申请日：2005-04-21

申请人： Koenraad Jozef Andries ,  Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Marcel Janssen ,  Paul Janssen ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

发明人： Koenraad Jozef Andries ,  Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Marcel Janssen ,  Paul Janssen ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

IPC分类号： C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  A61K31/506 ,  C07D43/14

CPC分类号： C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/49 ,  C07D239/50 ,  C07D401/12

摘要： This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted: or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxy-carbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl: or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical: for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

公开(公告)号：US20050176802A1

公开(公告)日：2005-08-11

申请号：US11028477

申请日：2005-01-04

申请人： Peng Cho Tang ,  Todd Miller ,  Xiaoyuan Li ,  Li Sun ,  Chung Chen Wei ,  Shahrzad Shirazian ,  Congxin Liang ,  Tomas Vojkovsky ,  Asaad Nematalla ,  Michael Hawley

发明人： Peng Cho Tang ,  Todd Miller ,  Xiaoyuan Li ,  Li Sun ,  Chung Chen Wei ,  Shahrzad Shirazian ,  Congxin Liang ,  Tomas Vojkovsky ,  Asaad Nematalla ,  Michael Hawley

IPC分类号： C07D401/14 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61P3/10 ,  A61P9/00 ,  A61P17/06 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07D207/32 ,  C07D207/33 ,  C07D209/44 ,  C07D401/12 ,  C07D403/00 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D521/00 ,  C07D43/14

CPC分类号： C07D233/56 ,  C07D207/33 ,  C07D209/44 ,  C07D231/12 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14

摘要： The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

摘要翻译： 本发明涉及吡咯取代的2-二氢吲哚酮化合物及其药学上可接受的盐，其调节蛋白激酶的活性，因此预期可用于预防和治疗与蛋白激酶相关的细胞病症例如癌症。

公开(公告)号：US20050176765A1

公开(公告)日：2005-08-11

申请号：US10515127

申请日：2003-06-17

申请人： Miller Ogidigben ,  Takeru Yamakawa ,  Yufu Sagara

发明人： Miller Ogidigben ,  Takeru Yamakawa ,  Yufu Sagara

IPC分类号： A61K9/08 ,  A61K9/10 ,  A61K31/4545 ,  A61K31/4747 ,  A61K45/00 ,  A61K47/36 ,  A61P1/04 ,  A61P9/10 ,  A61P25/02 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P27/06 ,  C07D235/26 ,  C07D271/10 ,  C07D271/107 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D495/04 ,  C07D43/14

CPC分类号： C07D271/107 ,  C07D235/26 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D495/04

摘要： This invention relates to selective m1 muscarinic agonist, their use or a formulation thereof in the treatment of glaucoma and/or other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans. In addition, the present invention relates to the use of the compounds in the treatment of dementia such as Alzheimer's disease and vascular dementia, depression, attention deficit disorder, sleep disorder, schizophrenia, pain, ischemia, atrophic gastritis, and atony of gastrointestinal tract.

摘要翻译： 本发明涉及选择性m1毒蕈碱激动剂，它们在治疗与患者眼睛中眼内压升高相关的青光眼和/或其他病症中的用途或制剂。 本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。 此外，本发明涉及该化合物在治疗诸如阿尔茨海默病和血管性痴呆，抑郁症，注意力缺陷障碍，睡眠障碍，精神分裂症，疼痛，局部缺血，萎缩性胃炎和胃肠道疾病的痴呆中的用途。