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1. 发明授权

US06686348B2 Metalloprotease inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US06686348B2
公开(公告)日：2004-02-03
申请号：US10036689
申请日：2001-12-21
申请人： Guillaume De Nanteuil , Alain Benoist , Philippe Pastoureau , Massimo Sabatini , John Hickman , Alain Pierre , Gordon Tucker
发明人： Guillaume De Nanteuil , Alain Benoist , Philippe Pastoureau , Massimo Sabatini , John Hickman , Alain Pierre , Gordon Tucker
IPC分类号： A61K3133
CPC分类号： C07D417/14 , C07D405/14 , C07D491/04
摘要： A compound of formula (I): wherein: R1 represents hydrogen, halogen, alkyl or alkoxy, X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.
摘要翻译：式（I）的化合物：其中：R1表示氢，卤素，烷基或烷氧基，X表示氧，硫或NR，其中R表示氢或烷基，A表示说明书中所述的任何一种基团，其异构体和加成其与药学上可接受的酸或碱的盐和含有它们的药物可用作金属蛋白酶抑制剂。

2. 发明授权

US06339092B1 Metalloprotease inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US06339092B1
公开(公告)日：2002-01-15
申请号：US09608240
申请日：2000-06-30
申请人： Guillaume de Nanteuil , Alain Benoist , Jacqueline Bonnet , Massimo Sabatini , Ghanem Atassi , Alain Pierre
发明人： Guillaume de Nanteuil , Alain Benoist , Jacqueline Bonnet , Massimo Sabatini , Ghanem Atassi , Alain Pierre
IPC分类号： A61K31435
CPC分类号： C07D491/04
摘要： A compound selected from those of the formula (I): wherein: R1 represents hydrogen or halogen, or alkyl or alkoxy, R2 represents hydroxy, alkoxy or —NHOH, Ar1 represents phenylene or biphenylene, X represents oxygen or sulphur, NR, —C≡C— or a bond, R represents hydrogen or alkyl, n is an integer from 0 to 6 inclusive, Ar2 represents any one of the groups as defined in the description, its isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as metalloprotease inhibitors.
摘要翻译：选自式（I）的化合物：其中：R1表示氢或卤素，或烷基或烷氧基，R2表示羟基，烷氧基或-NHOH，Ar1表示亚苯基或亚联苯基，X表示氧或硫，NR，-C = C-或键，R表示氢或烷基，n为0至6的整数，Ar2表示在说明书中定义的基团中的任何一个，其异构体和与药学上可接受的酸或碱的加成盐，以及含有该金属蛋白酶抑制剂的药物。

3. 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。

4. 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

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

US07981920B2 Addition salts of angiotensin-converting enzyme inhibitors with no donor acids, a process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：不含供体酸的血管紧张素转换酶抑制剂的加成盐，其制备方法和含有它们的药物组合物
公开(公告)号：US07981920B2
公开(公告)日：2011-07-19
申请号：US12283928
申请日：2008-09-17
申请人： Guillaume De Nanteuil , Bernard Portevin , Philippe Gloanec , Jean-Gilles Parmentier , Alain Benoist , Tony Verbeuren , Alain Rupin , Christine Courchay , Serge Simonet
发明人： Guillaume De Nanteuil , Bernard Portevin , Philippe Gloanec , Jean-Gilles Parmentier , Alain Benoist , Tony Verbeuren , Alain Rupin , Christine Courchay , Serge Simonet
IPC分类号： A61K31/404 , C07D209/12
CPC分类号： C07D207/09 , C07D209/42 , C07D209/52 , C07D217/26 , C07D233/36 , C07D271/08 , C07D495/10
摘要： Compounds of formula (I): (A)m·(B)n (I) wherein A represents an angiotensin-converting enzyme inhibitor compound containing at least one salt-forming basic function, B represents a compound containing at least one salt-forming acid function and at least one NO donor group, m represents the number of acid functions of B that have been converted to a salt and n represents the number of basic functions of A that have been converted to a salt, the bond or bonds between A and B being of the ionic type. Medicinal products containing the same which are useful in treating cardiovascular pathologies.
摘要翻译：式（I）化合物：（A）m·（B）n（I）其中A代表含有至少一种成盐碱性官能团的血管紧张素转换酶抑制剂化合物，B代表含有至少一种成盐酸功能和至少一个NO供体基团，m表示已转化为盐的B的酸官能团数，n表示已转化为盐的A的基本功能数，A或B之间的键或键而B为离子型。含有该药物的药物可用于治疗心血管病变。

7. 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。

8. 发明申请

US20090131668A1 4-oxo-4,6,7,8-Tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds 审中-公开
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：US20090131668A1
公开(公告)日：2009-05-21
申请号：US12321607
申请日：2009-01-22
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： C07D487/04
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。

9. 发明申请

US20090082393A1 New addition salts of angiotensin-converting enzyme inhibitors with no donor acids, a process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：不含供体酸的血管紧张素转换酶抑制剂的新加成盐，其制备方法和含有它们的药物组合物
公开(公告)号：US20090082393A1
公开(公告)日：2009-03-26
申请号：US12283928
申请日：2008-09-17
申请人： Guillaume De Nanteuil , Bernard Portevin , Philippe Gloanec , Jean-Gilles Parmentier , Alain Benoist , Tony Verbeuren , Alain Rupin , Christine Courchay , Serge Simonet
发明人： Guillaume De Nanteuil , Bernard Portevin , Philippe Gloanec , Jean-Gilles Parmentier , Alain Benoist , Tony Verbeuren , Alain Rupin , Christine Courchay , Serge Simonet
IPC分类号： A61K31/345 , C07D207/16 , C07D209/42 , C07D495/10 , C07D233/32 , C07D217/26 , C07D271/02 , C07D493/04 , A61P29/00 , A61P9/00 , A61K31/40 , A61K31/403 , A61K31/407 , A61K31/4166 , A61K31/472 , A61K31/4245
CPC分类号： C07D207/09 , C07D209/42 , C07D209/52 , C07D217/26 , C07D233/36 , C07D271/08 , C07D495/10
摘要： Compounds of formula (I): (A)m·(B)n (I) wherein A represents an angiotensin-converting enzyme inhibitor compound containing at least one salt-forming basic function, B represents a compound containing at least one salt-forming acid function and at least one NO donor group, m represents the number of acid functions of B that have been converted to a salt and n represents the number of basic functions of A that have been converted to a salt, the bond or bonds between A and B being of the ionic type. Medicinal products containing the same which are useful in treating cardiovascular pathologies.
摘要翻译：式（I）化合物：<？in-line-formula description =“In-line formula”end =“lead”？>（A）m。（B）n（I） “In-line Formulas”end =“tail”？>其中A表示含有至少一种成盐碱性官能团的血管紧张素转换酶抑制剂化合物，B代表含有至少一种成盐酸功能的化合物和至少一种 NO供体基团，m表示已转化为盐的B的酸官能团数，n表示已转化为盐的A的基本功能数，A和B之间的键或离子为离子类型。含有该药物的药物可用于治疗心血管病变。

10. 发明申请

US20050261501A1 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：US20050261501A1
公开(公告)日：2005-11-24
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： C07D295/18 , A61K31/40 , A61K31/4025 , A61K31/426 , A61K31/427 , A61K31/438 , A61P3/10 , A61P43/00 , C07D207/06 , C07D207/10 , C07D207/16 , C07D277/06 , C07D277/12 , C07D295/185 , C07D311/96 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D211/22
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

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