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1. 发明授权

US06531609B2 Process for the preparation of thiazolidinedione derivatives 失效
标题翻译：噻唑烷二酮衍生物的制备方法
公开(公告)号：US06531609B2
公开(公告)日：2003-03-11
申请号：US09814907
申请日：2001-03-22
申请人： Michelangelo Scalone
发明人： Michelangelo Scalone
IPC分类号： C07D27704
CPC分类号： C07D417/14
摘要： The present invention is concerned with a novel process for the preparation of compounds of formula I comprising bromomethylation or chloromethylation of a compound of formula II and subsequent reaction with a compound of formula IV The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances.
摘要翻译：本发明涉及制备具有式II化合物的溴甲基化或氯甲基化的式I化合物的新方法，随后与式IV化合物的反应。式I化合物及其相应的盐，例如，钠盐是药物活性物质。

2. 发明授权

US06489485B2 Para-amine substituted phenylamide glucokinase activators 失效
标题翻译：对胺取代苯酰胺葡萄糖激酶激活剂
公开(公告)号：US06489485B2
公开(公告)日：2002-12-03
申请号：US09846820
申请日：2001-05-01
申请人： Fred Thomas Bizzarro , Nancy-Ellen Haynes , Ramakanth Sarabu
发明人： Fred Thomas Bizzarro , Nancy-Ellen Haynes , Ramakanth Sarabu
IPC分类号： C07D27704
CPC分类号： C07D213/82 , C07D277/46 , C07D417/12
摘要： Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
摘要翻译：对烷基，芳基，环杂烷基或杂芳基[羰基或磺酰基]氨基取代的苯基酰胺作为葡萄糖激酶活化剂起作用，以增加胰岛素分泌，使其可用于治疗II型糖尿病。

3. 发明授权

US06639081B1 Method for producing 4-cyano-2-aminomethylthiazole 有权
标题翻译： 4-氰基-2-氨基甲基噻唑的制备方法
公开(公告)号：US06639081B1
公开(公告)日：2003-10-28
申请号：US10031703
申请日：2002-04-30
申请人： Monika Knopp , Stefan Koser , Bernd Schaefer
发明人： Monika Knopp , Stefan Koser , Bernd Schaefer
IPC分类号： C07D27704
CPC分类号： C07D277/56
摘要： The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ib in which n=1 or 2 and for n=1, X is chloride, bromide, triflate and hydrogen sulfate and for n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula II is stirred with a cysteine ester of the formula III, in which R1 is branched or linear C1-10-alkyl or where n=0, 1 or 2 and R2 is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.
摘要翻译：本发明涉及制备2-氨基甲基-4-氰基噻唑及其盐，其中n = 1或2，n = 1，X为氯化物，溴化物，三氟甲磺酸酯和硫酸氢盐，n = 2，X为硫酸盐，其包括其中式II的氨基腈与式III的半胱氨酸酯一起搅拌的方法步骤，其中R 1是支链或直链的C 1-10 - 烷基或其中n = 0,1或2， 2>是在0℃至80℃的碱存在下，在惰性溶剂中的支链或直链C 1 -C 10 C 10 - 烷基或C 1 -C 4 - 烷氧基或C 1 -C 4 - 二烷基氨基，直到反应基本上进行以及式Ia和Ib的化合物。

4. 发明授权

US06586602B2 Benzyl compounds which inhibit leukocyte adhesion mediated by VLA-4 失效
公开(公告)号：US06586602B2
公开(公告)日：2003-07-01
申请号：US10043275
申请日：2002-01-14
申请人： Eugene D. Thorsett , Christopher M. Semko , Michael A. Pleiss , Louis John Lombardo , Andrei W. Konradi , Francine S. Grant , Darren B. Dressen , Michael S. Dappen
发明人： Eugene D. Thorsett , Christopher M. Semko , Michael A. Pleiss , Louis John Lombardo , Andrei W. Konradi , Francine S. Grant , Darren B. Dressen , Michael S. Dappen
IPC分类号： C07D27704
CPC分类号： C07K5/06165 , A61K38/00 , C07K5/06139
摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, wherein the disease may be, for example, asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

5. 发明授权

US06362341B1 Benzyl compounds which inhibit leukocyte adhesion mediated by VLA-4 失效
标题翻译：抑制由VLA-4介导的白细胞粘附的苄基化合物
公开(公告)号：US06362341B1
公开(公告)日：2002-03-26
申请号：US09127601
申请日：1998-07-31
申请人： Eugene D. Thorsett , Christopher M. Semko , Michael A. Pleiss , Louis John Lombardo , Andrei W. Konradi , Francine S. Grant , Darren B. Dressen , Michael S. Dappen
发明人： Eugene D. Thorsett , Christopher M. Semko , Michael A. Pleiss , Louis John Lombardo , Andrei W. Konradi , Francine S. Grant , Darren B. Dressen , Michael S. Dappen
IPC分类号： C07D27704
CPC分类号： C07K5/06165 , A61K38/00 , C07K5/06139
摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, wherein the disease may be, for example, asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
摘要翻译：公开了结合VLA-4的化合物。这些化合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。这样的化合物可用于治疗哺乳动物患者（例如人）中的炎性疾病，其中疾病可以是例如哮喘，阿尔茨海默病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血。化合物也可以用于治疗炎性脑疾病如多发性硬化症。

6. 发明授权

US06642388B1 Method for producing 2-aminomethyl-4-cyano-thiazol 有权
标题翻译： 2-氨基甲基-4-氰基 - 噻唑的制备方法
公开(公告)号：US06642388B1
公开(公告)日：2003-11-04
申请号：US10031700
申请日：2002-05-10
申请人： Thomas Pfeiffer
发明人： Thomas Pfeiffer
IPC分类号： C07D27704
CPC分类号： C07D277/56 , C07K5/06078
摘要： The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ib in which n=1 or 2 and, for n=1, X is chloride, bromide, triflate and hydrogen sulfate and for n=2, X is sulfate, comprising the process step where the thioamide of the formula IV is stirred with a bromopyruvate of the formula V, in which R1 is branched or linear C1-4-alkyl in an alcohol R2OH in which R2 is branched or linear C1-8-alkyl, HO—CH2—CH2—, HO—CH2—CH2—CH2— or C1-4-alkyl- O—CH2—CH2— at from −5° C. to 40° C. until the conversion of the thioamide IV has essentially gone to completion, and to the compounds of the formulae Ia and Ib.
摘要翻译：本发明涉及制备2-氨基甲基-4-氰基噻唑及其式Ⅰa和Ⅰb盐的方法，其中n = 1或2，对于n = 1，X是氯化物，溴化物，三氟甲磺酸酯和硫酸氢盐，n = 2， X是硫酸盐，其包括其中式IV的硫代酰胺与式V的溴丙酮酸盐搅拌的方法步骤，其中R 1在醇R 2 OH中是支链或直链C 1-4 - 烷基，其中R 在-5℃至40℃时，支链或直链C 1-8烷基，HO-CH 2 -CH 2 - ，HO-CH 2 -CH 2 - 或C 1-4 - 烷基-O-CH 2 -CH 2 - 直到硫代酰胺IV的转化基本上已经完成，以及式Ia和Ib的化合物。

7. 发明授权

US06534659B2 Sufidomaidocarboxylic acids, method for production thereof, and use therefor 失效
标题翻译： Sufidomaidocarboxylic acid，其制备方法及其用途
公开(公告)号：US06534659B2
公开(公告)日：2003-03-18
申请号：US09840402
申请日：2001-04-23
申请人： Yoshihisa Oda
发明人： Yoshihisa Oda
IPC分类号： C07D27704
CPC分类号： C23F11/16 , C07D277/04 , C23F11/10 , C23F11/165
摘要： Novel sulfidoamidocarboxylic acids (salts), a method for the production thereof, and uses therefor are provided. Sulfidoamidocarboxylic acids (salt) with a thiazolidine residue such as dimethylthiazolidine or methylthiazolidine or thiazolidine residue (residues), or a polycarboxylic acid (salt) residue such as dicarboboxylic acid (salt) or tricarboxylic acid (salt) or tetracarboxylic acid (salt) residue, a method for the production thereof, and uses therefor are also provided.
摘要翻译：提供了新的硫酰胺基羧酸（盐），其制备方法及其用途。亚硫酰氨基羧酸（盐）与噻唑烷残基如二甲基噻唑烷或甲基噻唑烷或噻唑烷残基（残基），或多羧酸（盐）残基如二羧酸（盐）或三羧酸（盐）或四羧酸（盐）还提供了其制备方法及其用途。

8. 发明授权

US06313306B1 N-(2-Mercaptoethyl)-1,3-thiazolidines and their use as odorants and flavorings 失效
标题翻译： N-（2-巯基乙基）-1,3-噻唑烷及其作为气味剂和调味剂的用途
公开(公告)号：US06313306B1
公开(公告)日：2001-11-06
申请号：US09610757
申请日：2000-07-06
申请人： Wolfgang Engel , Peter Schieberle , Matthias Güntert , Stefan Lambrecht
发明人： Wolfgang Engel , Peter Schieberle , Matthias Güntert , Stefan Lambrecht
IPC分类号： C07D27704
CPC分类号： C11B9/0096 , C07D277/04
摘要： Substituted N-Mercaptoethyl-1,3-thiazolidines are novel compounds which can be used in odorants and flavorings.
摘要翻译：取代的N-巯基乙基-1,3-噻唑烷是可用于气味剂和调味剂的新型化合物。

9. 发明授权

US06706742B2 Alpha-amino-acid compounds 失效
标题翻译： α-氨基酸化合物
公开(公告)号：US06706742B2
公开(公告)日：2004-03-16
申请号：US10146272
申请日：2002-05-15
申请人： Guillaume De Nanteuil , Bernard Portevin , Alain Benoist , Nigel Levens , Olivier Nosjean , Bernadette Husson-Robert , Michelle Boulanger
发明人： Guillaume De Nanteuil , Bernard Portevin , Alain Benoist , Nigel Levens , Olivier Nosjean , Bernadette Husson-Robert , Michelle Boulanger
IPC分类号： C07D27704
CPC分类号： C07D295/185 , C07D207/16 , C07D277/04 , C07D277/06 , Y02P20/55
摘要： Compound selected from those of formula (I): wherein: represents an optionally substituted 5-membered nitrogen-containing heterocycle, Ak represents an alkylene chain, X represents a single bond or phenylene, R1 and R2, which may be identical or different, each represent hydrogen or alkyl, R3 represents alkyl, nitro or cyano, Y represents NR4 or CHNO2, R4 represents hydrogen or alkyl, its tautomers when they exist, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid, with the exclusion of compounds wherein, simultaneously, represents an unsubstituted 5-membered nitrogen-containing heterocycle, Ak represents —(CH2)3—, X represents a single bond, Y represents NH and R3 represents nitro. Medicinal products containing the same which are useful as dipeptidyl peptidase IV inhibitors.
摘要翻译：选自式（I）的化合物的化合物：其中：表示任选取代的5元含氮杂环，Ak表示亚烷基链，X表示单键或亚苯基，R 1和R 2可以相同或不同，各自相同或不同代表氢或烷基，R3代表烷基，硝基或氰基，Y代表NR4或CHNO2，R4代表氢或烷基，其互变异构体存在时，其光学异构体及其与药学上可接受的酸的加成盐，排除化合物其中，同时代表未取代的5元含氮杂环，Ak表示 - （CH2）3-，X表示单键，Y表示NH，R3表示硝基。含有该二价基团的肽酶IV 抑制剂。

10. 发明授权

US06632947B2 Process for the preparation of substituted thiazolidinedione 失效
标题翻译：制备取代噻唑烷二酮的方法
公开(公告)号：US06632947B2
公开(公告)日：2003-10-14
申请号：US10005686
申请日：2001-11-08
申请人： Robert Gordon Giles , Norman John Lewis , Stephen Moore , Colin Ripley Pool , John Kirby Quick , Michael Urquhart
发明人： Robert Gordon Giles , Norman John Lewis , Stephen Moore , Colin Ripley Pool , John Kirby Quick , Michael Urquhart
IPC分类号： C07D27704
CPC分类号： C07D417/06 , C07D277/34 , C07D417/10 , C07D417/12 , C07D417/14
摘要： A process for preparing a compound of formula (I, I) or a tautomeric form thereof or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, wherein: J represents O or S; T represents a substituted or unsubstituted aryl group and T1 is O or S; which process comprises reducing a compound of formula (II, II) or a tautomeric form thereof or a salt thereof or a solvate thereof, wherein T and T1 are as defined in relation to formula (I), with a complex hydride reducing agent or a source of a complex hydride reducing agent; and thereafter, as required, preparing a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate of the compound of formula (I) or a tautomeric form thereof.
摘要翻译：制备式（I，I）化合物或其互变异构体或其药学上可接受的盐或其药学上可接受的溶剂化物的方法，其中：J表示O或S; T表示取代或未取代的芳基，并且T为H或S; 该方法包括还原式（II，II）化合物或其互变异构形式或其盐或其溶剂合物，其中T和T 如式（I），与复合氢化物还原剂或复合氢化物还原剂的来源; 然后根据需要制备式（I）化合物或其互变异构体的药学上可接受的盐或药学上可接受的溶剂合物。

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