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1. 发明申请

US20110313040A1 ORGANIC NUTRIENT SALTS, METHODS OF PREPARATION AND USES 审中-公开
标题翻译：有机营养盐，制备方法和用途
公开(公告)号：US20110313040A1
公开(公告)日：2011-12-22
申请号：US13129243
申请日：2009-11-13
申请人： Xianqi Kong , Nigel Levens , Serge Lamothe , Ahmed Aman
发明人： Xianqi Kong , Nigel Levens , Serge Lamothe , Ahmed Aman
IPC分类号： A61K31/205 , C07C303/44 , A23L1/304 , A61P25/00 , A61P25/28 , A23L1/237 , C07C309/14 , C07C303/02
CPC分类号： C07C309/14 , A23L33/10 , A23L33/175 , A23V2002/00 , A23V2200/322 , A23V2250/0644 , A23V2250/0612
摘要： The invention relates to organic nutrient salts, to compositions containing the same, to their preparation as well as their use. Preferred compositions include nutraceutical compositions and dietary supplements for use in neuroprotection and for improving or protecting cognitive and memory function.
摘要翻译：本发明涉及有机营养盐，含有它们的组合物，其制备方法及其用途。优选的组合物包括用于神经保护和用于改善或保护认知和记忆功能的营养组合物和膳食补充剂。

2. 发明申请

US20120208850A1 METHODS, COMPOUNDS, AND COMPOSITIONS FOR DELIVERING 1,3-PROPANEDISULFONIC ACID 有权
标题翻译：用于递送1,3-丙二酸的方法，化合物和组合物
公开(公告)号：US20120208850A1
公开(公告)日：2012-08-16
申请号：US13389606
申请日：2010-08-06
申请人： Xianqi Kong , Nigel Levens , Abderrahim Bouzide , Stephane Ciblat , Richard Frenette , Johanne Renaud
发明人： Xianqi Kong , Nigel Levens , Abderrahim Bouzide , Stephane Ciblat , Richard Frenette , Johanne Renaud
IPC分类号： A61K31/255 , C07C309/69 , A61K31/27 , A61K31/265 , C07D327/00 , A61K31/385 , C07D311/00 , A61K31/366 , C07D401/12 , A61K31/444 , A61P13/12 , A61P3/06 , A61P3/00 , A61P3/10 , A61P5/50 , A61P1/18 , C07C309/65
CPC分类号： C07C309/65 , A61K31/255 , A61K31/351 , A61K31/365 , A61K31/366 , C07C309/05 , C07C311/06 , C07C311/51 , C07C2601/04 , C07C2601/14 , C07D213/64 , C07D213/65 , C07D231/12 , C07D307/00 , C07D307/33 , C07D307/58 , C07D307/77 , C07D309/22 , C07D319/06 , C07D327/00 , C07D327/10 , C07F9/091 , C07F9/4006 , C07F9/4043
摘要： The invention relates to methods, compounds, and compositions for delivering 1,3-propanedisulfonic acid (1,3PDS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 1,3PDS, either in vitro or in vivo. The invention also relates to sulfonate ester prodrugs of 1,3PDS as well as Gemini dimmers and oligomers of 1,3PDS for the prevention or treatment of associated diseases and conditions.
摘要翻译：本发明涉及在受试者，优选人受试者中递送1,3-丙二磺酸（1,3PDS）的方法，化合物和组合物。本发明包括在体外或体内产生或产生1,3PDS的化合物。本发明还涉及1,3PDS的磺酸酯前药以及用于预防或治疗相关疾病和病症的1,3PDS的双子座二聚体和寡聚体。

3. 发明授权

US09051248B2 Methods, compounds, and compositions for delivering 1,3-propanedisulfonic acid 有权
标题翻译：用于递送1,3-丙二磺酸的方法，化合物和组合物
公开(公告)号：US09051248B2
公开(公告)日：2015-06-09
申请号：US13389606
申请日：2010-08-06
申请人： Xianqi Kong , Nigel Levens , Abderrahim Bouzide , Stephane Ciblat , Richard Frenette , Johanne Renaud
发明人： Xianqi Kong , Nigel Levens , Abderrahim Bouzide , Stephane Ciblat , Richard Frenette , Johanne Renaud
IPC分类号： C07C309/65 , C07D319/06 , A61K31/366 , A61K31/365 , A61K31/255 , C07D309/22 , A61K31/351 , C07C309/05 , C07C311/06 , C07C311/51 , C07D213/64 , C07D213/65 , C07D231/12 , C07D307/33 , C07D307/58 , C07D307/77 , C07D327/10 , C07F9/09 , C07F9/40
CPC分类号： C07C309/65 , A61K31/255 , A61K31/351 , A61K31/365 , A61K31/366 , C07C309/05 , C07C311/06 , C07C311/51 , C07C2601/04 , C07C2601/14 , C07D213/64 , C07D213/65 , C07D231/12 , C07D307/00 , C07D307/33 , C07D307/58 , C07D307/77 , C07D309/22 , C07D319/06 , C07D327/00 , C07D327/10 , C07F9/091 , C07F9/4006 , C07F9/4043
摘要： The invention relates to methods, compounds, and compositions for delivering 1,3-propanedisulfonic acid (1,3PDS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 1,3PDS, either in vitro or in vivo. The invention also relates to sulfonate ester prodrugs of 1,3PDS as well as Gemini dimmers and oligomers of 1,3PDS for the prevention or treatment of associated diseases and conditions.
摘要翻译：本发明涉及在受试者，优选人受试者中递送1,3-丙二磺酸（1,3PDS）的方法，化合物和组合物。本发明包括在体外或体内产生或产生1,3PDS的化合物。本发明还涉及1,3PDS的磺酸酯前药以及用于预防或治疗相关疾病和病症的1,3PDS的双子座二聚体和寡聚体。

4. 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。

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

US06596749B2 Aminotriazole compounds 失效
标题翻译：氨基三唑化合物
公开(公告)号：US06596749B2
公开(公告)日：2003-07-22
申请号：US09799199
申请日：2001-03-05
申请人： Jean-Luc Fauchere , Jean-Claude Ortuno , Jacques Duhault , Jean Albert Boutin , Nigel Levens
发明人： Jean-Luc Fauchere , Jean-Claude Ortuno , Jacques Duhault , Jean Albert Boutin , Nigel Levens
IPC分类号： A61K314196
CPC分类号： C07D401/12 , C07D249/14 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , Y02P20/55
摘要： Method of treating with compounds of formula (I): wherein: n is 0 or 1, W represents —CO— or S(O)q and q is 0, 1 or 2, G represents a G1, G2, G3 or G4 group as defined in the description, Z represents alkyl, aryl, heteroaryl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylakenyl, heteroarylalkynyl or heteroarylalkyl each optionally substituted, A represents a grouping selected from —A2—, —A1—A2—, —A2—A1—, and —A1—A2—A1— wherein A1 is alkylene and A2 represents phenylene, cycloalkylene, naphthylene or heteroarylene each optionally substituted, R represents hydrogen, alkyl, aryl, heteroaryl, arylalkyl arylalkenyl, arylalkynyl, heteroarylakenyl, heteroarylalkynyl or heteroarylalkyl each optionally substituted, R1 represents alkyl, aryl, heteroaryl, arylalkyl arylalkenyl, arylalkynyl, heteroarylakenyl, heteroarylalkynyl or heteroarylalkyl each optionally substituted, and medicinal products containing the same are useful as Neuropeptide Y receptor ligands.
摘要翻译：用式（I）化合物处理的方法：其中：n为0或1，W为-CO-或S（O）q，q为0,1或2，G为G1，G2，G3或G4基团 Z表示烷基，芳基，杂芳基，芳基烷基，芳基烯基，芳基炔基，杂芳基酰基，杂芳基炔基或杂芳基烷基，各自任选取代，A表示选自-A2-，-A1-A2-，-A2-A1- 和-A1-A2-A1-，其中A1是亚烷基，A2代表亚苯基，亚环烷基，亚萘基或亚杂芳基，各自任选取代，R表示氢，烷基，芳基，杂芳基，芳基烷基芳基烯基，芳基炔基，杂芳基酰基，杂芳基炔基或杂芳基烷基， R 1表示烷基，芳基，杂芳基，芳基烷基芳基烯基，芳基炔基，杂芳基酰基，杂芳基炔基或杂芳基烷基，各自任选被取代，并且含有它们的医药产品可用作神经肽Y受体配体。

7. 发明授权

US06919362B2 Heterocyclic derivatives, preparation method and pharmaceutical compositions containing same 失效
标题翻译：杂环衍生物，制备方法和含有它们的药物组合物
公开(公告)号：US06919362B2
公开(公告)日：2005-07-19
申请号：US10203113
申请日：2001-02-01
申请人： Daniel Lesieur , Elodie Blanc-Delmas , Said Yous , Patrick Depreux , Gérald Guillaumet , Catherine Dacquet , Nigel Levens , Jean Albert Boutin , Caroline Bennejean , Pierre Renard
发明人： Daniel Lesieur , Elodie Blanc-Delmas , Said Yous , Patrick Depreux , Gérald Guillaumet , Catherine Dacquet , Nigel Levens , Jean Albert Boutin , Caroline Bennejean , Pierre Renard
IPC分类号： A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4439 , A61P1/00 , A61P1/04 , A61P1/14 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/10 , A61P9/14 , A61P13/00 , A61P13/12 , A61P15/00 , A61P17/06 , A61P19/10 , A61P21/00 , A61P21/04 , A61P25/28 , A61P35/00 , A61P43/00 , C07B61/00 , C07D263/58 , C07D277/68 , C07D417/06 , C07D471/04 , C07D498/04
CPC分类号： C07D263/58 , C07D277/68 , C07D471/04
摘要： Compounds of formula (I): wherein: X represents an oxygen or a sulphur or CH2 or R1 and R2 represent a hydrogen atom, or a group as defined in the description, A represents an alkylene chain as described in the description, B is as defined in the description, R3 and R4 represent a hydrogen atom or a group as defined in the description, D represents an optionally substituted benzene, optionally substituted pyrazine, optionally substituted pyrimidine or optionally substituted pyridazine and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.
摘要翻译：式（I）化合物：其中：X表示氧或硫或CH 2或R 1和R 2表示氢原子或说明书中所定义的基团，A表示如说明书中所述的亚烷基链，B如说明书中所定义，R 3和R 4代表氢原子或描述中定义的基团，D表示任选取代的苯，任选取代的吡嗪，任选取代的嘧啶或任选取代的哒嗪及其可用于治疗或预防褪黑激素障碍的药用产品。

8. 发明申请

US20050085644A1 Novel 3-aryl-2,5-dihydroxy-1,4-benzoquinone derivatives, their preparation method and pharmaceutical compositions containing same 审中-公开
标题翻译：新型3-芳基-2,5-二羟基-1,4-苯醌衍生物及其制备方法和含有它们的药物组合物
公开(公告)号：US20050085644A1
公开(公告)日：2005-04-21
申请号：US10503527
申请日：2003-02-04
申请人： Alexandra Dassonville , Anne Breteche , Muriel Duflos , Guillaume Le Baut , Bruno Pfeiffer , Pierre Renard , Nigel Levens , Bernadette Husson-Robert
发明人： Alexandra Dassonville , Anne Breteche , Muriel Duflos , Guillaume Le Baut , Bruno Pfeiffer , Pierre Renard , Nigel Levens , Bernadette Husson-Robert
IPC分类号： A61K31/122 , A61K31/222 , A61K31/4402 , A61P3/10 , C07C45/00 , C07C45/28 , C07C46/00 , C07C46/10 , C07C50/28 , C07C50/30 , C07D213/50 , C07C50/38 , C07D207/00 , C07D213/46
CPC分类号： C07D213/50 , C07C45/00 , C07C45/28 , C07C46/00 , C07C50/28 , C07C49/245
摘要： Compound of formula (I): wherein: R1 and R2, which may be identical or different, each represents hydrogen, acyl or alkyl, Ar represents aryl or heteroaryl, A represents a group selected from: R4 represents hydrogen or alkyl, R5 represents hydrogen, alkyl, aryl or heteroaryl, R3 represents aryl, heteroaryl, dicyclopropylmethyl or benzhydryl, or A-R3 represents an optionally substituted naphthyl group, with the exclusion of 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-phenylethenyl)-1,4-benzoquinone, 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-naphthyl)-1,4-benzoquinone and 2,5-dihydroxy-3-(2-naphthyl)-6-phenyl-1,4-benzoquinone. Medicinal products containing the same which are useful in the treatment of diseases associated with a deregulation of glycaemia.
摘要翻译：式（I）化合物：其中：R 1和R 2可以相同或不同，各自表示氢，酰基或烷基，Ar表示芳基或杂芳基， A表示选自以下的基团：R 4表示氢或烷基，R 5表示氢，烷基，芳基或杂芳基，R 3表示芳基，杂芳基，二环丙基甲基或二苯甲基或AR 3 3表示任选取代的萘基，排除2,5-二羟基-3-（4-甲氧基苯基）-6-（2-苯基乙烯基）-6- 1,4-苯醌，2,5-二羟基-3-（4-甲氧基苯基）-6-（2-萘基）-1,4-苯醌和2,5-二羟基-3-（2-萘基）-6- 苯基-1,4-苯醌。含有该药物的药物可用于治疗与血糖失调相关的疾病。

9. 发明授权

US06770444B2 Methods of identifying or screening for agents that binds the Ob-Re 失效
标题翻译：鉴定或筛选结合Ob-Re的药剂的方法
公开(公告)号：US06770444B2
公开(公告)日：2004-08-03
申请号：US09116676
申请日：1998-07-16
申请人： Nika Adham , Beth Borowsky , Nigel Levens , Radek Ctirad Skoda
发明人： Nika Adham , Beth Borowsky , Nigel Levens , Radek Ctirad Skoda
IPC分类号： G01N3353
CPC分类号： A61K31/70 , A61K38/00 , C07K14/705 , C12N2799/026
摘要： This invention provides an isolated nucleic acid encoding a polypeptide, a purified polypeptide, vectors comprising isolated nucleic acid encoding a polypeptide, cells comprising such vectors, antibodies directed to a polypeptide, nucleic acid probes useful for detecting nucleic acid encoding a polypeptide, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding a polypeptide, nonhuman transgenic animals which express DNA encoding a normal or a mutant polypeptide, methods of isolating a polypeptide, methods of treatment eating disorders as well as methods of determining binding of compounds to polypeptides.
摘要翻译：本发明提供了编码多肽的分离的核酸，纯化的多肽，包含分离的编码多肽的核酸，包含此类载体的细胞，针对多肽的抗体，可用于检测编码多肽的核酸的核酸探针，反义寡核苷酸互补编码多肽的独特的核酸序列，表达编码正常或突变多肽的DNA的非人类转基因动物，分离多肽的方法，进食障碍的治疗方法以及确定化合物与多肽结合的方法。

10. 发明授权

US06716843B2 Alpha-amino acid sulphonyl compounds 失效
标题翻译： α-氨基酸磺酰基化合物
公开(公告)号：US06716843B2
公开(公告)日：2004-04-06
申请号：US10109407
申请日：2002-03-28
申请人： Guillaume De Nanteuil , Bernard Portevin , Alain Benoist , Nigel Levens , Olivier Nosjean , Bernadette Husson-Robert
发明人： Guillaume De Nanteuil , Bernard Portevin , Alain Benoist , Nigel Levens , Olivier Nosjean , Bernadette Husson-Robert
IPC分类号： A61K3140
CPC分类号： C07D277/04 , C07D207/16 , C07D231/04 , C07D233/06 , C07D277/06 , C07D277/10 , Y02P20/55
摘要： Compound of formula (I): wherein: 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 —NR2aR2b 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, Y represents 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. 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，Y表示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，其光学异构体及其与药学上可接受的酸的加成盐。含有相同的喔 ch可用作二肽基肽酶IV的抑制剂。

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