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1. 发明授权

US06593312B2 Cyclic &agr;-amino-&ggr;-hydroxyamide compounds 失效
标题翻译：环状α-氨基-γ-羟基酰胺化合物
公开(公告)号：US06593312B2
公开(公告)日：2003-07-15
申请号：US10173993
申请日：2002-06-18
申请人： Michel Wierzbicki , Jean-Marie Fourquez , Nigel Levens , Bernadette Husson-Robert , Olivier Nosjean , Michelle Boulanger
发明人： Michel Wierzbicki , Jean-Marie Fourquez , Nigel Levens , Bernadette Husson-Robert , Olivier Nosjean , Michelle Boulanger
IPC分类号： A61K31425
CPC分类号： C07C237/14 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/20 , C07D209/52 , C07D277/04 , C07D295/185
摘要： A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R1 and R4, which may be identical or different, each represents hydrogen or acyl, R2 and R3, which may be identical or different, each represents hydrogen or alkyl, R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle, stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.
摘要翻译：式（I）的化合物：其中：表示任选取代的具有4至8个环成员的饱和碳环，可以相同或不同的R 1和R 4各自表示氢或酰基，R 2和R 3可以相同或不同的，各自表示氢或烷基，R 5和R 6可以相同或不同，各自表示氢或烷基，或者R 5和R 6一起与带有氮原子一起形成任选取代的含氮杂环，其立体异构体，以及其与药学上可接受的酸的加成盐。含有该药物的药物可用于治疗葡萄糖不耐症或与高血糖相关的病症。

2. 发明授权

US5385920A Diacylglycerol nicotinates 失效
标题翻译：二酰基甘油烟酸酯
公开(公告)号：US5385920A
公开(公告)日：1995-01-31
申请号：US73894
申请日：1993-06-09
申请人： Alex Cordi , Jean-Michel Lacoste , Jacques Duhault , Joseph Espinal , Michelle Boulanger
发明人： Alex Cordi , Jean-Michel Lacoste , Jacques Duhault , Joseph Espinal , Michelle Boulanger
IPC分类号： A61K31/44 , A61K31/4406 , A61K31/495 , A61K31/50 , A61P9/10 , C07D213/80 , C07D241/24 , C07D213/02
CPC分类号： C07D213/80
摘要： Compounds of formula (I): ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent a higher alkyl or higher alkenyl radical,R.sub.3 represents a pyridyl or pyrazinyl radical,their isomers and their addition salts with a pharmaceutically acceptable acid and medicaments for the reduction of plasma lipids containing the same.
摘要翻译：式（I）化合物：其中：R1和R2相同或不同，代表高级烷基或更高级的烯基，R3代表吡啶基或吡嗪基，它们的异构体及其加成盐与用于还原含有其的血浆脂质的药学上可接受的酸和药物。

3. 发明授权

US4505921A Sulfonylurea compounds and their use in treating diabetes 失效
标题翻译：磺酰脲类化合物及其在治疗糖尿病中的应用
公开(公告)号：US4505921A
公开(公告)日：1985-03-19
申请号：US529735
申请日：1983-09-06
申请人： Laszlo Beregi , Pierre Hugon , Jacques Duhault , Michelle Boulanger
发明人： Laszlo Beregi , Pierre Hugon , Jacques Duhault , Michelle Boulanger
IPC分类号： A61K31/64 , A61P3/08 , A61P3/10 , C07D209/46 , C07D209/48 , C07D401/04 , C07D405/04 , C07D409/04 , C07D491/048 , A61K31/395 , C07D519/00
CPC分类号： C07D209/48 , C07D209/46 , C07D401/04 , C07D405/04 , C07D409/04 , Y10S514/866
摘要： New sulfonylurea compounds of the formula: ##STR1## in which n is 1 or 2,R is thienyl, furyl, pyridyl or phenyl optionally mono or disubstituted,R.sub.1 and R.sub.2, the same or different, each are hydrogen, halogen, (C.sub.1 to C.sub.5)-alkyl, (C.sub.1 to C.sub.5)-alkoxy, or trifluoromethyl, or together represent --CH.sub.2 --O--CH.sub.2 --,R.sub.3 is hydrogen, or hydroxy, andR.sub.4 is (C.sub.1 to C.sub.5)-alkyl, (C.sub.3 to C.sub.8)-cycloalkyl or azacycloalkyl of the formula: ##STR2## in which p is zero or an integer from 1 to 5, or azabicycloalkyl of the formula: ##STR3## in which m is 1, 2, or 3. These new compounds and physiologically tolerable salts thereof may be used as medicines especially in the treatment of diabetes.
摘要翻译：新的具有下式的磺酰脲化合物：其中n为1或2，R为噻吩基，呋喃基，吡啶基或苯基，任选单取代或二取代，R 1和R 2相同或不同，各自为氢，卤素，（C 1至 C 1 -C 5） - 烷基，（C 1 -C 5） - 烷氧基或三氟甲基，或一起表示-CH 2 -O-CH 2 - ，R 3为氢或羟基，且R 4为（C 1至C 5） - 烷基，（C 3至C 8）环烷基或氮杂环烷基，其中p为0或1至5的整数，或下式的氮杂双环烷基：其中m为1,2或3.这些新化合物和生理上可耐受的其盐可以用作药物，特别是用于治疗糖尿病。

4. 发明授权

US4338323A Piperidylbenzimidazolinone derivatives 失效
标题翻译：哌啶基苯并咪唑啉酮衍生物
公开(公告)号：US4338323A
公开(公告)日：1982-07-06
申请号：US205725
申请日：1980-11-10
申请人： Gilbert Regnier , Alain Dhainaut , Jacques Duhault , Michelle Boulanger
发明人： Gilbert Regnier , Alain Dhainaut , Jacques Duhault , Michelle Boulanger
IPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D405/14 , A61K31/445 , C07D211/58
CPC分类号： C07D401/04 , C07D401/14 , Y10S514/826
摘要： Piperidylbenzimidazolinone derivatives of the formula: ##STR1## in which: R.sub.1 is lower alkyl, phenyl, halophenyl, lower alkylphenyl, lower alkoxyphenyl, methylenedioxyphenyl, ethylenedioxyphenyl, thienyl, furyl or pyridyl.R.sub.2 is R'.sub.1 COO-- or R'.sub.1 --COO--CH.sub.2 -- in which R'.sub.1 has the same meanings as R.sub.1, R.sub.1 and R'.sub.1 being the same or different, or R.sub.3 NH-- in which R.sub.3 is formyl, acetyl mesyl, carbamoyl, sulfamoyl or ethoxalyl.Z is hydrogen, lower-alkyl or lower alkenyl, andT is hydrogen, lower alkyl or lower alkoxy.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of autoimmune, allergic and antiinflammatory diseases and in the treatment of dyspnea especially asthmatic and bronchial dyspnea.
摘要翻译：下式的哌啶基苯并咪唑啉酮衍生物：其中：R1是低级烷基，苯基，卤代苯基，低级烷基苯基，低级烷氧基苯基，亚甲二氧基苯基，亚乙二氧基苯基，噻吩基，呋喃基或吡啶基。 R2是R'1COO-或R'1-COO-CH2-，其中R'1具有与R1相同的含义，R1和R'1相同或不同，或R3NH-，其中R3是甲酰基，乙酰基甲磺酰基，氨基甲酰基，氨磺酰基或乙氧基。 Z是氢，低级烷基或低级烯基，T是氢，低级烷基或低级烷氧基。这些化合物和其生理上可耐受的酸加成盐可以用作药物，特别是用于治疗自身免疫性，过敏性和抗炎性疾病以及治疗呼吸困难，特别是哮喘和支气管呼吸困难。

5. 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。

6. 发明授权

US5266591A Ethanolamine benzoate compounds 失效
标题翻译：乙醇胺苯甲酸酯化合物
公开(公告)号：US5266591A
公开(公告)日：1993-11-30
申请号：US979202
申请日：1992-11-20
申请人： Michel Wierzbicki , Pierre Hugon , Jacques Duhault , Michelle Boulanger , Francoise Lacour
发明人： Michel Wierzbicki , Pierre Hugon , Jacques Duhault , Michelle Boulanger , Francoise Lacour
IPC分类号： A61K31/24 , A61P3/06 , A61P3/08 , A61P7/00 , A61P9/12 , C07C233/51 , C07C235/34
CPC分类号： C07C233/51 , C07C2103/18
摘要： The compounds are ethanolamine benzoate compounds useful for the treatment of syndrome X, and of hypertension in patients who are insulin resistant or have one or more metabolic anomalies.A compound disclosed is S-1-(m-trifluoromethylphenyl)-2-{.beta.-{4-[2-(N-(3,3-diphenylpropionyl)amino)ethyl] benzoyloxy}ethylamino} propane.
摘要翻译：这些化合物是可用于治疗综合征X的乙醇胺苯甲酸酯化合物，以及患有胰岛素抵抗或具有一种或多种代谢异常的患者的高血压。所公开的化合物是S-1-（间三氟甲基苯基）-2- {β-（4- [2-（N-（3,3-二苯基丙酰基）氨基）乙基]苯甲酰氧基}乙基氨基}丙烷。

7. 发明授权

US4064245A N-Phenoxyphenyl-piperazines 失效
标题翻译： N-苯氧基苯基 - 哌嗪
公开(公告)号：US4064245A
公开(公告)日：1977-12-20
申请号：US705330
申请日：1976-07-14
申请人： Laszlo Beregi , Pierre Hugon , Jacques Duhault , Michelle Boulanger
发明人： Laszlo Beregi , Pierre Hugon , Jacques Duhault , Michelle Boulanger
IPC分类号： C07D295/08 , A61K31/495 , A61P3/04 , A61P3/06 , A61P3/08 , A61P9/10 , C07D295/096 , C07D295/14 , C07D295/155
CPC分类号： C07D295/096 , C07D295/155
摘要： Phenoxy compounds of the formula: ##STR1## wherein R and R', which are the same or different, are hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylthio, nitro, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, lower alkoxy-carbonyl or dimethylsulfamoyl.These compounds are used as medicines especially in the treatment of glucid -- and lipid -- metabolism disorders.
摘要翻译：下式的苯氧基化合物：其中R和R'相同或不同，为氢，卤素，低级烷基，低级烷氧基，低级烷硫基，硝基，三氟甲基，三氟甲硫基，三氟甲氧基，低级烷氧羰基或二甲基氨磺酰。

8. 发明授权

US5266718A Ethanolamine benzoate compounds 失效
标题翻译：乙醇胺苯甲酸酯化合物
公开(公告)号：US5266718A
公开(公告)日：1993-11-30
申请号：US898916
申请日：1992-06-12
申请人： Michel Wierzbicki , Pierre Hugon , Jacques Duhault , Francoise Lacour , Michelle Boulanger
发明人： Michel Wierzbicki , Pierre Hugon , Jacques Duhault , Francoise Lacour , Michelle Boulanger
IPC分类号： C07C219/14 , C07C233/51 , C07C235/34 , C07C101/34
CPC分类号： C07C219/14 , C07C233/51 , C07C235/34 , C07C2103/18
摘要： New ethanolamine benzoate compounds which can be used as medicaments and correspond to the formula: ##STR1## wherein R is as defined in the description, in the form of racemic compounds and enantiomers. These new compounds and their physiologically tolerable salts can be used therapeutically for treatment of insulin-resistance states.
摘要翻译：新的可用作药物的乙醇胺苯甲酸酯化合物，其对应于下式：其中R如说明书中所定义，以外消旋化合物和对映体的形式。这些新化合物及其生理上可耐受的盐可用于治疗胰岛素抵抗状态。

9. 发明授权

US4548820A Xanthine compounds 失效
标题翻译：黄嘌呤化合物
公开(公告)号：US4548820A
公开(公告)日：1985-10-22
申请号：US516946
申请日：1983-07-25
申请人： Gilbert Regnier , Claude Guillonneau , Jacques Duhault , Michelle Boulanger
发明人： Gilbert Regnier , Claude Guillonneau , Jacques Duhault , Michelle Boulanger
IPC分类号： C07D473/04 , A61K31/52 , A61K31/522 , A61K31/55 , A61P11/00 , A61P11/08 , A61P37/00 , A61P37/08 , A61P43/00 , C07D239/54 , C07D239/545 , C07D295/02 , C07D473/06 , C07D473/08 , C07D473/10 , C07D473/12 , C12N9/99
CPC分类号： C07D239/545 , C07D473/06 , C07D473/08 , C07D473/10 , C07D473/12
摘要： New xanthine compounds of the formula: ##STR1## in which: R.sub.1 is hydrogen or alkyl from C.sub.1 to C.sub.5 inclusive;R.sub.2 is a hydrocarbon radical up to C.sub.6 having optionally a double bond, phenyl or benzyl;R.sub.3 is hydrogen, alkyl, hydroxyalkyl or dihydroxyalkyl each from C.sub.1 to C.sub.5R.sub.4 represents: ##STR2## in which: Y is hydrogen, halogen, alkyl or alkoxy from C.sub.1 to C.sub.5 or hydroxyl;Z is methylene or a straight or branched hydrocarbon radical from C.sub.2 to C.sub.5 optionally substituted by hydroxyl; andA is an amino group of the formula: ##STR3## p being 2 or 3; ##STR4## in which q is 1 or 2, and X is a single bond, oxygen or ##STR5## in which R.sub.5 is hydrogen, alkyl or alkylene up to C.sub.5, or ##STR6## in which m is an integer from 2 to 6 and R.sub.6 is alkyl from C.sub.1 to C.sub.5.These new compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of all diseases where it is necessary to inhibit the antigenic antibody reactions.
摘要翻译：新的黄嘌呤化合物，其结构式如下：其中：R1为氢或C1至C5的烷基，包括端值; R 2是直到C 6的任选具有双键的烃基，苯基或苄基; R3为氢，C1至C5 R4为氢，烷基，羟基烷基或二羟基烷基，其中：Y为氢，卤素，C1至C5的烷基或烷氧基或羟基; Z是亚甲基或任选被羟基取代的C 2至C 5的直链或支链烃基; A是下式的氨基： p为2或3; 其中q是1或2，X是单键，氧或者其中R5是氢，烷基或亚烷基直到C5，或者其中m是2-6的整数的“IMAGE” R6是C1至C5的烷基。这些新化合物和其生理上可耐受的酸加成盐可以用作药物，特别是在需要抑制抗原抗体反应的所有疾病的治疗中。

10. 发明授权

US4264613A Piperidylbenzimidazolinone compounds 失效
标题翻译：哌啶基苯并咪唑啉酮化合物
公开(公告)号：US4264613A
公开(公告)日：1981-04-28
申请号：US62878
申请日：1979-08-01
申请人： Gilbert Regnier , Alain Dhainaut , Jacques Duhault , Michelle Boulanger
发明人： Gilbert Regnier , Alain Dhainaut , Jacques Duhault , Michelle Boulanger
IPC分类号： C07D401/04 , A61K31/445
CPC分类号： C07D401/04
摘要： Piperidylbenzimidazolinone compounds of the formula: ##STR1## in which: R is hydrogen, hydroxy, hydroxymethyl, methoxycarbonyl, formamido, acetamido, mesylamino, oxalamino, ethoxalylamino, carbamoyl ##STR2## ureido ##STR3## or sulfamoylamino ##STR4## in which R' and R" are hydrogen or lower alkyl, T is hydrogen, halogen, lower alkyl or lower alkoxy, andZ is hydrogen, lower alkyl or lower alkenyl each in straight or branched chain.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of autoimmune, allergic and inflammatory diseases and in the treatment of respiratory insufficiency of asthma.
摘要翻译：其中：R为氢，羟基，羟甲基，甲氧基羰基，甲酰氨基，乙酰氨基，甲磺酰氨基，草酰氨基，乙氧基氨基，氨基甲酰基或脲基氨基，其中R' 和R“为氢或低级烷基，T为氢，卤素，低级烷基或低级烷氧基，Z为氢，低级烷基或低级链烯基，分别为直链或支链。这些化合物和其生理上可耐受的酸加成盐可以用作药物，特别是用于治疗自身免疫性，过敏性和炎性疾病以及治疗哮喘的呼吸功能不全。

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