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41. 发明申请

US20030114492A1 Method of using neurotrophic sulfonamide compounds 审中-公开
标题翻译：使用神经营养磺酰胺化合物的方法
公开(公告)号：US20030114492A1
公开(公告)日：2003-06-19
申请号：US09814954
申请日：2001-03-23
发明人： Gregory S. Hamilton , Jia-He Li , Joseph P. Steiner
IPC分类号： A61K031/4545 , A61K031/445 , A61K031/4439 , A61K031/401 , A61K031/4025
CPC分类号： A61K31/40 , A61K31/18 , A61K31/44 , A61K31/4439 , A61K31/445
摘要： This invention relates to a method of using neurotrophic low molecular weight, small molecule sulfonamide compounds having an affinity for FKBP-type immunophilins, as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
摘要翻译：本发明涉及使用具有与FKBP型免疫亲和素亲和力的神经营养性低分子量磺酰胺化合物作为与免疫亲和素蛋白特异性肽基 - 脯氨酰异构酶或旋转异构酶相关的酶活性的抑制剂的酶的活性的方法。

42. 发明申请

US20030109569A1 Preparation of pharmaceutically acceptable atorvastatin salts in non-crystalline form 失效
标题翻译：以非结晶形式制备药学上可接受的阿托伐他汀盐
公开(公告)号：US20030109569A1
公开(公告)日：2003-06-12
申请号：US10323444
申请日：2002-12-18
发明人： Gorazd Sorsak
IPC分类号： A61K031/401 , C07D27/333
CPC分类号： C07D207/34 , Y02P20/55
摘要： Non-crystalline, in particular amorphous, pharmaceutically acceptable atorvastatin salts, especially the calcium salt, are prepared from atorvastatin lactone or from a compound of formula (I) 1 where A denotes a common protecting group or separate protecting groups for the two hydroxy groups, and B denotes a carboxylic acid protecting group, without the need of prior formation of atorvastatin lactone, the crystalline form of the atorvastatin salt, or a mixture of amorphous and crystalline forms of the atorvastatin salt. Pharmaceutical formulations are prepared from these salts.
摘要翻译：非结晶的，特别是无定形的药学上可接受的阿托伐他汀盐，特别是钙盐，由阿托伐他汀内酯或式（I）化合物制备，其中A表示常见保护基或两个羟基的单独保护基， B表示羧酸保护基团，而不需要先前形成阿托伐他汀内酯，阿托伐他汀盐的结晶形式或阿托伐他汀盐的无定形和结晶形式的混合物。药物制剂由这些盐制备。

43. 发明申请

US20030105142A1 Amide derivatives useful as inhibitors of the production of cytokines 失效
公开(公告)号：US20030105142A1
公开(公告)日：2003-06-05
申请号：US10192495
申请日：2002-07-11
申请人： ASTRAZENECA AB
发明人： Dearg S. Brown , George R. Brown
IPC分类号： C07D213/63 , A61K031/44 , A61K031/401 , C07D27/14
CPC分类号： C07D213/81 , C07D213/82 , C07D215/48 , C07D239/74 , C07D241/44 , C07D261/18 , C07D277/68 , C07D333/38 , C07D401/12 , C07D401/14 , C07D413/12
摘要： The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q1 is heteroaryl which is optionally substituted with 1, 2, 3, or 4 substituents such as hydroxy, halogeno, trifluoromethyl, (1-6C)alkyl, (1-6C)alkoxy, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, amino-(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, heteroaryl and heterocyclyl; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and Q2 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

44. 发明申请

US20030100598A1 Novel esters derived from (rr,ss)-2-hydroxybenzoate of 3-(2-dimethylaminomethyl-1-hydroxycyclohexyl)phenyl 失效
标题翻译：衍生自3-（2-二甲基氨基甲基-1-羟基环己基）苯基的（rr，ss）-2-羟基苯甲酸酯的新型酯
公开(公告)号：US20030100598A1
公开(公告)日：2003-05-29
申请号：US10169177
申请日：2002-06-27
发明人： Marisabel Mourelle Mancini , Elisabet De Ramon Amat , Juan Huguet Clotet
IPC分类号： A61K031/401 , A61K031/24 , C07C229/38
CPC分类号： C07C219/28 , C07B2200/07 , C07C2601/14
摘要： New esters derived from substituted phenyl-cyclohexyl compounds, which are derived from Tramadol, process for obtaining them and their use for preparing a drug with analgesic properties. These new compounds of general formula (I) have a higher analgesic activity, a lower toxicity and a longer effective time period than Tramadol.
摘要翻译：衍生自衍生自曲马多的取代的苯基 - 环己基化合物的新酯，用于获得它们的方法及其用于制备具有止痛性质的药物的用途。这些新的通式（I）化合物与曲马多相比具有较高的镇痛活性，较低的毒性和较长的有效时间。

45. 发明申请

US20030100538A1 Substituted chalcones as therapeutic compounds 失效
标题翻译：取代的查尔酮作为治疗化合物
公开(公告)号：US20030100538A1
公开(公告)日：2003-05-29
申请号：US10239757
申请日：2002-09-26
发明人： Gerard Andrew Potter , Paul Crispin Butler , Elugba Wanogho
IPC分类号： A61K031/66 , C07F009/02 , A61K031/44 , A61K031/401 , A61K031/18 , A61K031/12 , A61K031/235
CPC分类号： G01N33/574 , A61K31/12 , A61K31/15 , A61K31/222 , C07C69/017 , C07C251/40 , C07C305/24 , C07F9/12 , G01N2333/90209
摘要： This invention pertains to substituted chalcones, specifically substituted 1-(4-methoxyphenyl)-3-(3,5-dimethoxyphenyl)prop-1-en-3-ones, which have therapeutic application, for example, as potent antiproliferative agents and antiinflammatory agents, and which have the formula (I) wherein: X is nullH, nullOH, nullOC(nullO)R3, nullOS(nullO)2OH, or nullOP(nullO)2(OH)2; Y is nullH or a C1-4alkyl group; Z is nullH or nullOCH3; R1 is nullH, a C1-4alkyl group, or C1-4fluoroalkyl group; R2 is nullH, a C1-4alkyl group, or C1-4fluoroalkyl group; and, R3 is nullH, a C1-6alkyl group, a C3-20 heterocyclyl group, or a C5-20aryl group; and pharmaceutically acceptable salts, esters, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.
摘要翻译：本发明涉及具有治疗应用的取代的查尔酮，特异性取代的1-（4-甲氧基苯基）-3-（3,5-二甲氧基苯基）丙-1-烯-3-酮，例如作为有效的抗增殖剂和抗炎药（O）2 OH或-OP（= O）2（OH）2）的化合物，其具有式（I）其中：X为-H，-OH，-OC（= O） Y是-H或C 1-4烷基; Z是-H或-OCH 3; R1是-H，C1-4烷基或C1-4氟烷基; R2是-H，C1-4烷基或C1-4氟烷基; 且R 3为-H，C 1-6烷基，C 3-20杂环基或C 5-20芳基; 和其药学上可接受的盐，酯和保护形式。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内用于诊断和治疗例如增生性疾病如癌症和炎性病症的用途。

46. 发明申请

US20030096802A1 Pentanoic acid derivatives 失效
标题翻译：戊酸衍生物
公开(公告)号：US20030096802A1
公开(公告)日：2003-05-22
申请号：US10194247
申请日：2002-07-15
申请人： ONO PHARMACEUTICAL CO., LTD.
发明人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
IPC分类号： A61K031/54 , A61K031/551 , A61K031/55 , A61K031/537 , A61K031/496 , A61K031/445 , A61K031/401
CPC分类号： C07D213/75 , A61K31/19 , C07C53/21 , C07C69/612 , C07C69/63 , C07C69/708 , C07C233/05 , C07C233/11 , C07C233/25 , C07C233/47 , C07C233/54 , C07C323/52 , C07D295/185
摘要： The compound of the formula (I) 1 wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together a saturated heterocyclic ring or amino acid residues; and non-toxic salts thereof and acid addition salts thereof. The compounds of the present invention of the formula (I) and the compounds of the formula (X): 2 wherein n is 0 or 1, R11 is hydrogen and chlorine, R5 is R7nullCH2null or R8, or R5 and R11, taken together is alkylidene; R6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR9R10, in which R9, R10 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R9 and R10, taken together a saturated heterocyclic ring or amino acid residues, R7 is (i) Fnull(CH2)mnull or F3CnullCH2null, (ii) alkyl substituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R8 is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy; non-toxic salts and acid addition salts thereof are useful for prevention and/or treatment for neurodegenerarive disease (Alzheimer's disease etc.) and neuronal dysfunction by stroke or traumic injury (Multiple sclerosis etc.) etc.
摘要翻译：其中R1是被氟取代的烷基的式（Ⅰ）化合物; R2是羟基，烷氧基，被苯基取代的烷氧基，NR3R4，其中R3，R4是（i）氢，（ii）烷基，（iii）苯基，（iv）被烷氧基或羧基取代的苯基;（v）氮原子，（vi）被苯基取代的烷基，被烷氧基或羧基取代的苯基，含有氮原子的杂环，（vii）与R 3和R 4键合的氮原子一起构成饱和杂环或氨基酸残基; 及其无毒盐及其酸加成盐。式（I）的本发明化合物和式（X）化合物：其中n为0或1，R11为氢和氯，R5为R7-CH2-或R8，或R5和R11取代一起是亚烷基; R6是羟基，烷氧基，被苯基取代的烷氧基，NR9R10，其中R9，R10是（i）氢，（ii）烷基，（iii）苯基，（iv）被烷氧基或羧基取代的苯基，（v）氮原子，（vi）被苯基取代的烷基，被烷氧基或羧基取代的苯基，含有氮原子的杂环，（vii）与R 9和R 10结合的氮一起为饱和杂环或氨基酸残基，R7为（ i）F-（CH 2）m - 或F3C-CH 2 - ，（ii）被氯取代的烷基，（iii）被烷氧基，环烷基，苯基，苯氧基取代的烷基; R8是烷基，烯基，烷氧基，烷硫基，环烷基，苯基，苯氧基; 无毒盐及其酸加成盐可用于预防和/或治疗神经变性疾病（阿尔茨海默氏病等）和脑卒中或外伤性损伤（多发性硬化症等）的神经元功能障碍。

47. 发明申请

US20030092757A1 Favorable modulation of health-related quality of life and health-related quality-adjusted time-to-progression of disease in patients with prostate cancer 审中-公开
公开(公告)号：US20030092757A1
公开(公告)日：2003-05-15
申请号：US10118300
申请日：2002-04-08
发明人： Amitabh Singh , Robert J. Padley , Talat Ashraf
IPC分类号： A61K031/401
CPC分类号： A61K31/40 , A61K31/00
摘要： Disclosed herein is a method for favorably modulating the health-related quality of life and the health-related quality-adjusted time-to-disease progression in a patient having prostate cancer and a method for measuring of the health-related quality-adjusted time-to-disease progression.

48. 发明申请

US20030092704A1 Novel arylglycinamide derivatives, method of producing said derivatives and pharmaceutical compositions containing these compounds 失效
标题翻译：新型芳基甘氨酰胺衍生物，所述衍生物的制备方法和含有这些化合物的药物组合物
公开(公告)号：US20030092704A1
公开(公告)日：2003-05-15
申请号：US10235053
申请日：2002-09-05
申请人： Boehringer Ingelheim Pharma KG
发明人： Franz Esser , Gerd Schnorrenberg , Kurt Schromm , Horst Dollinger , Birgit Jung , Georg Speck
IPC分类号： A61K031/551 , A61K031/55 , A61K031/495 , A61K031/445 , A61K031/4172 , A61K031/401
CPC分类号： C07D221/14 , C07D211/46 , C07D211/58 , C07D213/74 , C07D239/42 , C07D241/08 , C07D243/08 , C07D295/145 , C07D295/185 , C07D295/30 , C07D317/60
摘要： The invention relates to new arylglycinamide derivatives of general formula I 1 and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula 2 in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
摘要翻译：本发明涉及通式I的新型芳基甘氨酰胺衍生物及其药学上可接受的盐，其中R 1和R 2与它们所连接的N一起形成下式的环，其中R 3，R 4，R 5，Ar，R 6，R 7 ，R8，R9，R10，R11，r，s和t具有说明书及其制备和用途中给出的含义。新化合物是有价值的神经激肽（速激肽）拮抗剂。

49. 发明申请

US20030092703A1 Caspase inhibitors and uses thereof 失效
标题翻译：胱天蛋白酶抑制剂及其用途
公开(公告)号：US20030092703A1
公开(公告)日：2003-05-15
申请号：US10153971
申请日：2002-05-23
发明人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
IPC分类号： A61K031/55 , A61K031/541 , A61K031/5377 , A61K031/496 , A61K031/454 , A61K031/401 , A61K031/397
CPC分类号： A61K31/55 , A61K31/4015 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/45 , A61K31/498 , A61K31/5025 , A61K31/538 , A61K31/54 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： This invention provides compounds of formula I: 1 wherein Z is oxygen or sulfur; R1 is hydrogen, nullCHN2, R, CH2OR, CH2SR, or nullCH2Y; next to R3 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1null secretion.
摘要翻译：本发明提供式I化合物：其中Z是氧或硫; R1是氢，-CHN2，R，CH2OR，CH2SR或-CH2Y; R3旁边表示单键或双键; Y是电负离子团; R2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; R3是能够适应胱天蛋白酶的S2亚位点的基团; R4是氢或C1-6烷基或R3和R4一起形成环; 环A和环B各自为杂环，R和R 5如说明书所述。这些化合物是凋亡和IL-1β分泌的有效抑制剂。

50. 发明申请

US20030087950A1 New alpha-amino acid sulphonyl compounds 失效
标题翻译：新的α-氨基酸磺酰化合物
公开(公告)号：US20030087950A1
公开(公告)日：2003-05-08
申请号：US10109407
申请日：2002-03-28
发明人： Guillaume DeNanteuil , Bernard Portevin , Alain Benoist , Nigel Levens , Olivier Nosjean , Bernadette Husson-Robert
IPC分类号： A61K031/4025 , A61K031/401 , C07D27/12 , C07D43/02
CPC分类号： C07D277/04 , C07D207/16 , C07D231/04 , C07D233/06 , C07D277/06 , C07D277/10 , Y02P20/55
摘要： Compound of formula (I): 1 wherein: 2 represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or phenylalanylprolyl, Ak represents an alkylene or heteroalkylene chain, X represents a single bond or optionally substituted phenylene, R2 represents optionally substituted alkyl, (C3-C10)cycloalkyl, or nullNR2aR2b wherein R2a and R2b, which may be the same or different, each represent hydrogen or alkyl or, together with the nitrogen atom carrying them, form a nitrogen-containing heterocycle, 3 R3 represents hydrogen or a group selected from alkyl, (C3-C7) cycloalkyl and aryl, R4, R5 and R6, which may be the same or different, each represent hydrogen or alkyl, or R4 and R6, or R5 and R6, together with the atoms carrying them, form an imidazolidine or dihydrobenzimidazole ring, its optical isomers and addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful as inhibitors of dipeptidyl-peptidase IV.
摘要翻译：式（I）化合物：其中：表示任选取代的5元含氮杂环，R 1表示氢，烷基，酰基，脯氨酰基，丙氨酰，组氨酰脯氨酰基或苯丙氨酰脯氨酰基，Ak表示亚烷基或杂亚烷基链，X表示单键或任选取代的亚苯基，R 2表示任选取代的烷基，（C 3 -C 10）环烷基或-NR 2 a R 2b，其中可以相同或不同的R 2a和R 2b各自代表氢或烷基，或与携带它们的氮原子一起，形成含氮杂环，R 3表示氢或选自烷基，（C 3 -C 7）环烷基和芳基的基团，R 4，R 5和R 6可以相同或不同，各自表示氢或烷基，或R 4和 R6或R5和R6与携带它们的原子一起形成咪唑烷或二氢苯并咪唑环，其光学异构体及其药学上可接受的酸的加成盐，以及含有相同w 可用作二肽基肽酶IV的抑制剂。

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