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1. 发明授权

US08247441B2 Chromene compounds, a process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：色烯化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US08247441B2
公开(公告)日：2012-08-21
申请号：US12804355
申请日：2010-07-20
申请人： Guillaume De Nanteuil , Bernard Cimetiere , Anne Dekeyne , Mark Millan
发明人： Guillaume De Nanteuil , Bernard Cimetiere , Anne Dekeyne , Mark Millan
IPC分类号： A61K31/407 , C07D209/58
CPC分类号： C07D491/04
摘要： The invention relates to compounds of formula (I): wherein R1 and R2 together form the following carbon-containing chain: wherein: R3 represents a hydrogen atom or an alkyl group, R4 represents a hydrogen atom or an alkyl, aryl, heteroaryl, 3,4-dioxocyclobutenyl, alkylcarbonyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, benzoyl, arylsulphonyl or heteroarylsulphonyl group, each of those groups optionally being substituted, or R3 and R4 together with the nitrogen atom carrying them form a 5- to 8-membered ring, the ring thereby formed optionally being substituted. Medicinal products containing the same which are useful in treating conditions requiring a D3 receptor antagonist.
摘要翻译：本发明涉及式（I）化合物：其中R 1和R 2一起形成以下含碳链：其中：R 3表示氢原子或烷基，R 4表示氢原子或烷基，芳基，杂芳基，3 ，4-二氧环戊烯基，烷基羰基，环烷基羰基，杂环烷基羰基，苯甲酰基，芳基磺酰基或杂芳基磺酰基，这些基团任选被取代，或者R3和R4与携带它们的氮原子一起形成5-至8-元环，形成任选地被取代。含有该药物的药物可用于治疗需要D3受体拮抗剂的病症。

2. 发明授权

US07498330B2 4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds 失效
标题翻译： 4-氧代-4,6,7,8-四氢 - 吡咯并[1,2-a]吡嗪-6-甲酰胺化合物
公开(公告)号：US07498330B2
公开(公告)日：2009-03-03
申请号：US11079638
申请日：2005-03-14
申请人： Guillaume De Nanteuil , Philippe Gloanec , Jean-Gilles Parmentier , Alain Benoist , Alain Rupin , Marie-Odile Vallez , Tony Verbeuren
发明人： Guillaume De Nanteuil , Philippe Gloanec , Jean-Gilles Parmentier , Alain Benoist , Alain Rupin , Marie-Odile Vallez , Tony Verbeuren
IPC分类号： A01N43/66 , A61K31/53 , C07D241/36
CPC分类号： C07D487/04
摘要： Compound of formula (I): wherein: represents 1-oxidopyridyl substituted by the remainder of the molecule in any one of the positions 2, 3 and 4, m and n, which may be identical or different, each represent an integer of from 1 to 3, R1 represents hydrogen or alkyl, R2 and R3, which may be identical or different, each represent an atom or group selected from hydrogen, halogen, alkyl, hydroxy, acyloxy and alkoxy, or, together with the carbon atom carrying them, form a cycloalkane having from 3 to 6 carbon atoms, R4 and R5 each represent hydrogen, or are adjacent and, together with the carbon atoms carrying them, form a benzo ring, Ar represents aryl or heteroaryl. Medicinal products containing the same which are useful as thrombin inhibitors.
摘要翻译：式（I）的化合物：其中：表示由位置2,3和4中的任一个中的分子的其余部分取代的1-氧化吡啶基，m和n可以相同或不同，各自表示1的整数至3，R 1表示氢或烷基，可以相同或不同的R 2和R 3各自表示选自氢，卤素，烷基，羟基，酰氧基和烷氧基的原子或基团，或者与携带它们的碳原子一起，形成具有3至6个碳原子的环烷烃，R 4和R 5各自表示氢或邻近，并且与携带它们的碳原子一起形成苯并环，Ar表示芳基或杂芳基。含有该药物的药物可用作凝血酶抑制剂。

3. 发明授权

US07439263B2 Pyrrolidine and thiazolidine compounds 失效
标题翻译：吡咯烷和噻唑烷化合物
公开(公告)号：US07439263B2
公开(公告)日：2008-10-21
申请号：US11131510
申请日：2005-05-18
申请人： Guillaume De Nanteuil , Alain Benoist , Murielle Combettes , Elizabeth Harley
发明人： Guillaume De Nanteuil , Alain Benoist , Murielle Combettes , Elizabeth Harley
IPC分类号： A61K31/40 , C07D207/04
CPC分类号： C07D405/12 , C07D207/10 , C07D207/16 , C07D277/12 , C07D295/185 , C07D403/12 , C07D409/12 , C07D417/12
摘要： Compounds of formula (I): wherein: X1 represents an atom or group selected from CR4aR4b, O, S(O)q1 and NR5, wherein R4a, R4b, q1 and R5 are as defined in the description, m1 represents zero or an integer from 1 to 4 inclusive, m2 represents an integer from 1 to 4 inclusive, n1 and n2, which may be identical or different, each represent an integer from 1 to 3 inclusive, R1 represents hydrogen or a group selected from carboxy, alkoxycarbonyl, optionally substituted carbamoyl and optionally substituted alkyl, R2 represents hydrogen or alkyl, Ak represents an optionally substituted alkylene chain, p represents zero, 1 or 2, R3 represents hydrogen or cyano, X2 and X3, which may be identical or different, each represent either S(O)q2, or CR6aR6b, wherein q2, R6a and R6b are as defined in the description, its optical isomers, where they exist, and its addition salts with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful as DPP-IV inhibitors.
摘要翻译：式（I）的化合物：其中：X 1表示选自CR 4a R 4a，O，S（O） q1和NR5，其中R 4a 4a，R 4b，q 1和...， R 5如描述中所定义，m 1表示0或1至4的整数，其中m 2表示1的整数，至4个，其中可以相同或不同的n 1和n 2各自表示1至3的整数，包括1和3的整数，R 1，表示氢或选自羧基，烷氧基羰基，任选取代的氨基甲酰基和任选取代的烷基的基团，R 2表示氢或烷基，Ak表示任选取代的亚烷基链，p表示0,1或2，R 3或3表示氢或氰基，X 2和X 3可以相同或不同，各自表示S（O） q2，或CR 6a R 6b，其中q2

4. 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。

5. 发明授权

US5866587A Metalloprotease inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US5866587A
公开(公告)日：1999-02-02
申请号：US842982
申请日：1997-04-25
申请人： Guillaume de Nanteuil , Joseph Paladino , Georges Remond , Ghanem Atassi , Alain Pierre , Gordon Tucker , Jacqueline Bonnet , Massimo Sabatini
发明人： Guillaume de Nanteuil , Joseph Paladino , Georges Remond , Ghanem Atassi , Alain Pierre , Gordon Tucker , Jacqueline Bonnet , Massimo Sabatini
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/473 , A61P9/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D209/42 , C07D217/26 , C07D221/08 , C07D221/10 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04
CPC分类号： C07D471/04 , C07D209/42 , C07D217/26 , C07D221/10 , C07D491/04 , C07D495/04
摘要： Compound of formula (I): ##STR1## in which: m, n, which are identical or different, represent 0, 1 or 2,R.sub.1, R.sub.2, which are identical or different, represent hydrogen, optionally substituted alkyl, aryl, or form with the carbon atom carrying them carbonyl or (C.sub.3 -C.sub.7)cycloalkyl,R.sub.3 represents hydrogen, alkyl, hydroxyl or aryl,R.sub.4 represents any of the groups as defined in the description,X represents --SO.sub.2 --, --CO-- or --SO.sub.2 NH--,R.sub.5 represents optionally substituted alkyl, (C.sub.3 -C.sub.7)cycloalkyl, aryl or heterocyclic,A represents an aryl ring or a heterocycle,its isomers as well as its addition salts with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitors.
摘要翻译：式（I）化合物：其中：m，n相同或不同，表示0,1或2，相同或不同的R 1，R 2表示氢，任选取代的烷基，芳基或与其中带有羰基或（C3-C7）环烷基的碳原子形成，R3表示氢，烷基，羟基或芳基，R4表示说明中定义的任何基团，X表示-SO 2 - ， - 或-SO 2 NH-，R 5表示任选取代的烷基，（C 3 -C 7）环烷基，芳基或杂环，A表示芳基环或杂环，其异构体以及其与药学上可接受的酸或碱的加成盐和含有这同样可用作金属蛋白酶抑制剂。

6. 发明授权

US5652246A Piperidine compounds 失效
标题翻译：哌啶化合物
公开(公告)号：US5652246A
公开(公告)日：1997-07-29
申请号：US546263
申请日：1995-10-20
申请人： Guillaume de Nanteuil , Georges Remond , Bernard Portevin , Jacqueline Bonnet , Emmanuel Canet , Graham Birrell
发明人： Guillaume de Nanteuil , Georges Remond , Bernard Portevin , Jacqueline Bonnet , Emmanuel Canet , Graham Birrell
IPC分类号： A61K31/4427 , A61K31/445 , A61P1/00 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D401/06 , C07D471/04 , C07D471/02 , A61K31/415 , A61K31/44 , C07D235/22
CPC分类号： C07D401/06 , C07D471/04
摘要： The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 represents alkyl, phenyl, naphthyl, pyridyl or thienyl group, each phenyl, naphthyl, pyridyl or thienyl optionally being substituted,R.sub.2 represents a hydrogen atom or a substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, cycloalkyl, piperidino or substituted or unsubstituted amino group,X represents CO or SO.sub.2,R.sub.3 represents hydrogen or alkyl,R.sub.4 represents alkyl, substituted or unsubstituted phenyl or trihalomethyl, or else R.sub.3 and R.sub.4 form, together with the carbon atoms which carry them, cyclo(C.sub.3 -C.sub.7)alkenyl,A represents phenyl, naphthyl or pyridyl ring, each phenyl, naphthyl or pyridyl ring optionally being substituted,their isomers, the corresponding quaternary ammonium salts of the piperidine and their addition salts with a pharmaceutically acceptable acid, an medicinal products containing the same are useful as antagonists of NK.sub.1 receptors.
摘要翻译：本发明涉及式（I）化合物：其中：R 1表示烷基，苯基，萘基，吡啶基或噻吩基，每个苯基，萘基，吡啶基或噻吩基任选被取代，R 2表示氢原子或取代或未取代的烷基，取代或未取代的苯基，环烷基，哌啶子基或取代或未取代的氨基，X表示CO或SO 2，R 3表示氢或烷基，R 4表示烷基，取代或未取代的苯基或三卤甲基， R 4与携带它们的碳原子一起形成环（C 3 -C 7）链烯基，A代表苯基，萘基或吡啶环，每个苯基，萘基或吡啶基任选被取代，它们的异构体是相应的季铵盐哌啶及其与药学上可接受的酸的加成盐，含有它们的药物可用作NK1受体的拮抗剂。

7. 发明授权

US5468761A 4-methyl-5-substituted-1,3-oxazoles having anti-inflammatory activity 失效
标题翻译：具有抗炎活性的4-甲基-5-取代-1,3-恶唑
公开(公告)号：US5468761A
公开(公告)日：1995-11-21
申请号：US164464
申请日：1993-12-09
申请人： Guillaume de Nanteuil , Michel Vincent , Christine Lila , Jacqueline Bonnet , Armel Fradin
发明人： Guillaume de Nanteuil , Michel Vincent , Christine Lila , Jacqueline Bonnet , Armel Fradin
IPC分类号： A61K31/42 , A61K31/421 , A61P29/00 , C07D263/32
CPC分类号： C07D263/32 , A61K31/42
摘要： Compound of formula (I): ##STR1## in which: R.sub.1 represents 1-adamantyl, dicyclopropylmethyl, substituted or unsubstituted (C.sub.3 -C.sub.6) cycloalkyl or substituted or unsubstituted bicyclo[2.2.2]oct-1-yl,R.sub.2 represents: ##STR2## in which: m represents 1, 2 or 3,X represents oxygen or sulfur or N--R,R.sub.3 or R.sub.4, which are identical or different, represent hydrogen, (C.sub.1 -C.sub.6) alkyl or trifluoromethyl, ##STR3## n represents 0, 1 or 2, R.sub.5 represents hydroxy, or (C.sub.1 -C.sub.6) alkoxy, and anti-inflammatory medicinal products containing the same.
摘要翻译：式（I）化合物：其中：R1表示1-金刚烷基，二环丙基甲基，取代或未取代的（C3-C6）环烷基或取代或未取代的双环[2.2.2]辛-1-基，R2 表示：其中：m表示1,2或3，X表示氧或硫或NR，R3或R4相同或不同，表示氢，（C1-C6）烷基或三氟甲基， IMAGE> n表示0,1或2，R 5表示羟基或（C 1 -C 6）烷氧基，和含有它们的抗炎药物。

8. 发明授权

US5192775A New aminomethylpiperidine compounds 失效
标题翻译：新的氨基哌啶化合物
公开(公告)号：US5192775A
公开(公告)日：1993-03-09
申请号：US661494
申请日：1991-02-26
申请人： Charles Malen , Guillaume de Nanteuil , Francis Colpaert
发明人： Charles Malen , Guillaume de Nanteuil , Francis Colpaert
IPC分类号： A61K31/35 , A61K31/34 , A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/445 , A61P9/00 , A61P9/12 , A61P25/04 , A61P25/18 , A61P25/24 , A61P25/26 , A61P43/00 , C07D235/30 , C07D263/58 , C07D277/82 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
CPC分类号： C07D401/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The invention relates to compounds of general formula (I). ##STR1## in which X represents an atom of sulfur or oxygen, or a substituted or unsubstituted amino group;R represents a hydrogen atom or any one of groups A, B, C, D, E, F, or G;R' represents a hydrogen atom, an alkyl group or any one of groups A, B, C, D, E or F, with R'=H when R=G;or R and R' form, with the nitrogen atom to which they are attached, an optionally substituted piperazine ring. Medicaments.
摘要翻译：本发明涉及通式（I）的化合物。（I）其中X表示硫或氧原子，或取代或未取代的氨基; R代表氢原子或A，B，C，D，E，F或G组之一; R'表示氢原子，烷基或基团A，B，C，D，E或F中的任一个，当R = G时，R'= H; 或R和R'与它们所连接的氮原子一起形成任选取代的哌嗪环。药剂

9. 发明授权

US07442692B2 Indanyl-piperazine compounds 失效
标题翻译：茚基 - 哌嗪化合物
公开(公告)号：US07442692B2
公开(公告)日：2008-10-28
申请号：US11391916
申请日：2006-03-29
申请人： Guillaume De Nanteuil , Bernard Portevin , Philippe Gloanec , Mark Millan , Jean-Claude Ortuno , Clotilde Mannoury La Cour , Alain Gobert
发明人： Guillaume De Nanteuil , Bernard Portevin , Philippe Gloanec , Mark Millan , Jean-Claude Ortuno , Clotilde Mannoury La Cour , Alain Gobert
IPC分类号： A61K31/551 , A61K31/495 , A61K31/496 , C07D295/084 , C07D295/125 , C07D295/145
CPC分类号： C07D213/40 , C07D295/096 , C07D295/135 , C07D295/155 , C07D333/20
摘要： A compound selected from those of formula (I): wherein: R3 represents a hydrogen atom, and R1 and R2 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, or R1 represents a hydrogen atom, and R2 and R3 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, n represents 1 or 2, —X— represents a group selected from —(CH2)m—O-Ak-, —(CH2)m—NR4-Ak-, —(CO)—NR4-Ak- and —(CH2)m—NR4-(CO)—, m represents an integer between 1 and 6 inclusive, Ak represents an optionally substituted alkylene chain, and R4 represents a hydrogen atom or an alkyl group, Ar represents an aryl or heteroaryl group, its enantiomers, diasteroisomers, and addition salts thereof with a pharmaceutically acceptable acid. Medical products containing the same which are useful in the treatment of conditions requiring a serotonin reuptake inhibitor and/or NK1 antagonist.
摘要翻译：选自式（I）的化合物的化合物：其中：R 3表示氢原子，R 1和R 2与带有它们的碳原子形成苯，萘或喹啉环结构，每个环结构任选被取代，或R 1表示氢原子，R 2和R 2 3个与携带它们的碳原子一起形成苯，萘或喹啉环结构，每个环结构可以被取代，n表示1或2，-X-表示选自 - （ CH 2 - （CH 2）n -O - ， - （CH 2 CH 2）m -NR 2 -Ak-， - （CO）-NR 4 - 和 - （CH 2）2 -N （CO） - ，m表示1和6之间的整数，包括1和6，Ak表示任选取代的亚烷基链，并且R 4表示氢原子或烷基，Ar 表示芳基或杂芳基，其对映异构体，diastero 异构体及其与药学上可接受的酸的加成盐。含有该药物的医药产品可用于治疗需要5-羟色胺再摄取抑制剂和/或NK1拮抗剂的病症。

10. 发明授权

US07265220B2 Amino acid derivatives, method for production thereof and pharmaceutical compositions comprising said derivative 失效
标题翻译：氨基酸衍生物，其生产方法和包含所述衍生物的药物组合物
公开(公告)号：US07265220B2
公开(公告)日：2007-09-04
申请号：US10505005
申请日：2003-02-17
申请人： Guillaume De Nanteuil , Philippe Gloanec , Tony Verbeuren , Alain Rupin
发明人： Guillaume De Nanteuil , Philippe Gloanec , Tony Verbeuren , Alain Rupin
IPC分类号： C07C257/18 , C07C311/13 , C07C311/19 , C07C259/18 , A61K31/196 , A61P7/04 , C07D213/34 , C07D295/22 , C07D261/20
CPC分类号： C07D295/26 , A61K38/00 , C07C257/18 , C07C259/18 , C07C311/10 , C07C311/13 , C07C311/19 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2603/14 , C07C2603/28 , C07D213/34 , C07D261/20 , C07K5/06034 , C07K5/06078
摘要： Compound of formula (I): wherein: R1 represents aryl, heteroaryl or alkyl which is optionally substituted, or a group of formula —(CO)—CR6R7NR8R9 wherein R6, R7, R8 and R9 are as defined in the description, R2 represents hydrogen or alkyl, R3 represents hydrogen or optionally substituted alkyl, R4 represents a saturated or unsaturated, 7- to 15-membered bicyclic system or optionally substituted alkyl, or R3 and R4, together with the carbon atom carrying them, form a saturated or unsaturated, 3- to 18-membered, mono-, bi- or tri-cyclic system optionally containing one or more hetero atoms selected from O, S and N and optionally substituted, n represents 1 or 2, Ar represents aryl or heteroaryl, R5 represents amino, guanidino, cyano or amidino which is optionally substituted, its optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in pathological conditions involving activated protein C.
摘要翻译：式（I）的化合物：其中：R 1表示任选取代的芳基，杂芳基或烷基，或式 - （CO）-CR 6 R' 其中R 6，R 7，R 3，R 3，R 7， 8和R 9如在说明书中所定义，R 2表示氢或烷基，R 3表示氢或任选取代的烷基，R 4表示饱和或不饱和的，7至15元双环体系或任选取代的烷基，或R 3和R 4，与携带它们的碳原子一起形成任选含有一个或多个选自O，S和N的杂原子的任选被取代的饱和或不饱和的3至18元单，双，三环体系， n表示1或2，Ar表示芳基或杂芳基，R 5表示任选取代的氨基，胍基，氰基或脒基，其旋光异构体，以及其中的加成盐与药学上可接受的酸。含有相同功能的药物，可用于涉及活化蛋白C的病理状况。

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