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1. 发明授权

US5814622A Compounds derived from boronic acid 失效
标题翻译：衍生自硼酸的化合物
公开(公告)号：US5814622A
公开(公告)日：1998-09-29
申请号：US807569
申请日：1997-02-27
申请人： Guillaume de Nanteuil , Philippe Gloanec , Christine Lila , Bernard Portevin , Tony Verbeuren , Alain Rupin , Serge Simonet
发明人： Guillaume de Nanteuil , Philippe Gloanec , Christine Lila , Bernard Portevin , Tony Verbeuren , Alain Rupin , Serge Simonet
IPC分类号： A61K31/69 , A61P7/02 , A61P9/08 , A61P9/10 , A61P43/00 , C07F5/02 , C07F5/04
CPC分类号： C07F5/025
摘要： Compound of formula (I) ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent hydrogen or alkyl or alternatively R.sub.1 and R.sub.2 form, with the carbon atom which bears them, cycloalkyl, R.sub.3 represents hydrogen or alkyl, phenyl or benzyl, R.sub.4 represents: optionally substituted amino, optionally substituted amindino, optionally substituted guanidino, optionally substituted isothioureido, optionally substituted iminomethylamino, mercapto substituted with heterocyclic, or heterocyclic, R.sub.5 and R.sub.6 each represent hydrogen or alkyl, or ##STR2## forms a boronic ester of pinanediol, m represents an integer such that 0.ltoreq.m.ltoreq.6, n represents an integer such that 1.ltoreq.n.ltoreq.6, A represents any one of the following groups: * optionally substituted bicycloalkyl (C.sub.5 -C.sub.10)phenyl, * or a group of formula: ##STR3## A.sub.1 represents --CO--, --CS--, --SO.sub.2 --, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful as trypsin-like serine proteases.
摘要翻译：式（I）化合物其中：R 1和R 2相同或不同，代表氢或烷基，或者R1和R2与带有它们的碳原子形成环烷基，R3代表氢或烷基，苯基或苄基，R4表示：任选取代的氨基，任选取代的氨基，任选取代的胍基，任选取代的异硫脲基，任选取代的亚氨基甲基氨基，被杂环或杂环取代的巯基，R 5和R 6各自表示氢或烷基，形成蒎二醇的硼酸酯，m表示0≤n≤6的整数，n表示1≤n≤6的整数，A表示以下基团中的任一个：*任选地取代的双环烷基（C 5 -C 10）苯基，或下式的基团：A 1表示-CO - ， - CS-，-SO 2 - ，其异构体及其与药学上可接受的酸或碱的加成盐，和使用含有该药物的药用产品作为胰蛋白酶样丝氨酸蛋白酶。

2. 发明授权

US5585360A Peptide compounds derived from boronic acid 失效
标题翻译：衍生自硼酸的肽化合物
公开(公告)号：US5585360A
公开(公告)日：1996-12-17
申请号：US458504
申请日：1995-06-02
申请人： Guillaume de Nanteuil , Christine Lila , Philippe Gloanec , Michel Laubie , Tony Verbeuren , Serge Simonet , Alain Rupin
发明人： Guillaume de Nanteuil , Christine Lila , Philippe Gloanec , Michel Laubie , Tony Verbeuren , Serge Simonet , Alain Rupin
IPC分类号： A61K38/55 , A61K38/00 , A61P7/04 , C07K1/06 , C07K5/06 , C07K5/065 , C07K14/81 , A61K38/06 , C07F9/22
CPC分类号： C07K5/06191 , A61K38/00
摘要： The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 denotes hydrogen, acyl, alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl or linear or branched C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted, or R.sub.6 SO.sub.2 -- in which R.sub.6 denotes alkyl, naphthyl, phenyl, benzyl or morpholine,R.sub.2 denotes hydrogen or phenyl, substituted or unsubstituted benzyl, thienylmethyl, (pyridyl)methyl, diphenylmethyl, fluorenyl, naphthylmethyl, benzocyclobutyl, (dicyclopropylmethyl)methyl, indanyl or (C.sub.3 -C.sub.7 cycloalkyl)methyl,R'.sub.2 denotes hydrogen or elseR.sub.2 and R'.sub.2 together denote C.sub.6 H.sub.5 --CH.dbd.,R.sub.3 denotes any one of the groups as defined in the description, each of R.sub.4 and R.sub.5 denotes hydrogen or alkyl, or ##STR2## forms a boronic ester of pinanediol, A denotes the following group: ##STR3## in which n and A.sub.2 are as defined in the description, and medicinal products containing the same are useful as thrombin inhibitors.
摘要翻译：本发明涉及式（I）的化合物：其中：R1表示氢，酰基，烷氧基羰基，苄氧基羰基，苯氧基羰基或直链或支链C1-C6烷基，取代或未取代的或R6SO2-，其中R6 （吡啶基）甲基，二苯基甲基，芴基，萘基甲基，苯并环丁基，（二环丙基甲基）甲基，二氢化茚基或（C 3 -C 7环烷基）甲基，R'2表示氢，或者R2和R'2一起表示C 6 H 5 -CH =，R 3表示说明书中定义的基团中的任一个，R 4和R 5各自表示氢或烷基，或者形成蒎二醇的硼酸酯，A表示以下基团：其中n和A2如说明书中所定义的，含有它们的药物可用作凝血酶抑制剂。

3. 发明授权

US5444049A Peptide compounds derived from boronic acid 失效
标题翻译：衍生自硼酸的肽化合物
公开(公告)号：US5444049A
公开(公告)日：1995-08-22
申请号：US199473
申请日：1994-02-22
申请人： Guillaume de Nanteuil , Christine Lila , Michel Laubie , Tony Verbeuren , Serge Simonet , Alain Rupin , Bernard Portevin
发明人： Guillaume de Nanteuil , Christine Lila , Michel Laubie , Tony Verbeuren , Serge Simonet , Alain Rupin , Bernard Portevin
IPC分类号： A61K38/55 , A61K38/00 , A61P7/02 , C07F5/02 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/078 , C07K14/81 , A61K38/06
CPC分类号： C07K5/06191 , C07F5/025 , A61K38/00
摘要： A compound of formula (I): ##STR1## in which: R.sub.1 represents hydrogen or acyl, alkyl, benzyl, alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl, 5-[(dimethyl)amino]naphthylsulfonyl, alkoxycarbonylmethyl or carboxymethyl,R.sub.2 represents hydrogen or phenyl, substituted or unsubstituted benzyl, 3-thienylmethyl, 2-pyridylmethyl, diphenylmethyl, fluorenyl, naphthylmethyl, benzocyclobutyl, (dicyclopropylmethyl)methyl, indanyl or (C.sub.3 -C.sub.7 cycloalkyl)methyl,R'.sub.2 represents hydrogen or benzylor alternativelyR.sub.2 and R'.sub.2 together represent C.sub.6 H.sub.5 --CH.dbd.,R.sub.3 represents substituted alkyl or guanidinophenyl, amidinophenyl, aminophenyl, guanidinobenzyl, amidinobenzyl, aminobenzyl or cycloalkyl,R.sub.4 and R.sub.5 each represent hydrogen or alkyl, or ##STR2## forms a boronic ester of pinanediol, A represents any one of the groups as defined in the description.Medicinal products.
摘要翻译：式（I）化合物：其中：R 1表示氢或酰基，烷基，苄基，烷氧基羰基，苄氧基羰基，苯氧基羰基，5 - [（二甲基）氨基]萘基磺酰基，烷氧基羰基甲基或羧甲基，或苯基，取代或未取代的苄基，3-噻吩基甲基，2-吡啶基甲基，二苯基甲基，芴基，萘基甲基，苯并环丁基，（二环丙基甲基）甲基，茚满基或（C 3 -C 7环烷基）甲基，R 12代表氢或苄基， R 2一起代表C 6 H 5 -CH =，R 3表示取代的烷基或胍基苯基，脒基苯基，氨基苯基，胍基苄基，脒基苄基，氨基苄基或环烷基，R 4和R 5各自代表氢或烷基，或者“IMAGE”形成蒎二醇的硼酸酯表示说明书中定义的组中的任何一个。药用产品。

4. 发明授权

US06302837B1 Benzothiophene, benzofuran and indole compounds 失效
标题翻译：苯并噻吩，苯并呋喃和吲哚化合物
公开(公告)号：US06302837B1
公开(公告)日：2001-10-16
申请号：US09687308
申请日：2000-10-13
申请人： Guillaume De Nanteuil , Christine Lila , Tony Verbeuren , Alain Rupin
发明人： Guillaume De Nanteuil , Christine Lila , Tony Verbeuren , Alain Rupin
IPC分类号： A61K314436
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D333/58 , C07D333/60 , C07D401/06 , C07D409/06 , C07D409/14
摘要： A compound selected from those of formula (I): wherein: X represents oxygen, sulphur, or NR3 wherein R3 is as defined in the description, Y represents oxygen, sulphur, NR3, or may represent single bond in certain cases, T represents nitrogen, carbon, or CH, A represents single bond, alkylene, arylene, cycloalkylene, heterocycloalkylene, heteroarylene, or —SO2—R4— wherein R4 is as defined in the description, W represents hydroxy, alkoxy, aryloxy, arylalkoxy, cycloalkyloxy, heterocycloalkyloxy or heteroaryloxy, or hydroxyamino, U1 represents hetero, or alkylene wherein one or more of carbon may optionally be replaced by one or more hetero atoms, V1 represents arylene, heteroarylene,or heterocycloalkylene, U2 represents single bond, hetero or alkylene wherein one or more carbon may optionally be replaced by one or more hetero atoms, V2 represents aryl, heteroaryl, or heterocycloalkyl, Ra, Rb, Rc, which may be identical or different, each independently of the others represents a group as defined in the description, R1 represents aryl substituted by from one to five substituents, 1,3-dihydro-2H-indol-2-one, 3,4-dihydro-2(1H)-quinolinone, 1-hydroxy-2(1H)-pyridinone group, or heteroaryl, R2 represents halogen, alkyl, aryl, arylalkyl, cycloalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroarylalkyl, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful as inhibitors of PAI-1 in the treatment of thrombosis, pathologies for which the origin is thrombosis, or pathologies causing an increase in risk of thrombosis.
摘要翻译：选自式（I）的化合物：其中：X表示氧，硫或NR 3，其中R3如说明书中所定义，Y表示氧，硫，NR 3，或在某些情况下可表示单键，T表示氮，碳或CH，A表示单键，亚烷基，亚芳基，亚环烷基，亚杂环亚烷基，亚杂芳基或-SO 2 -R 4 - ，其中R 4如说明书中所定义，W表示羟基，烷氧基，芳氧基，芳基烷氧基，环烷氧基，杂芳基氧基或羟基氨基，U1表示杂或亚烷基，其中一个或多个碳可以任选被一个或多个杂原子替代，V 1表示亚芳基，亚杂芳基或杂环亚烷基，U 2表示单键，杂或亚烷基，其中一个或多个碳可任选地被一个或多个杂原子替代，V 2表示芳基，杂芳基或杂环烷基，R a，R b，R c可以相同或不同，各自独立地表示t定义的基团他描述，R1代表被1至5个取代基取代的芳基，1,3-二氢-2H-吲哚-2-酮，3,4-二氢-2（1H） - 喹啉酮，1-羟基-2（1H） - 吡啶酮基或杂芳基，R 2表示卤素，烷基，芳基，芳基烷基，环烷基，杂环烷基，杂环烷基烷基，杂芳基或杂芳基烷基，其异构体及其药学上可接受的酸或碱加成盐，以及含有它们的药物作为治疗血栓形成的PAI-1的抑制剂，来自血栓形成的病理学，或导致血栓形成风险增加的病理学。

5. 发明授权

US6048875A Benzothiophene, benzofuran and indole compounds 失效
标题翻译：苯并噻吩，苯并呋喃和吲哚化合物
公开(公告)号：US6048875A
公开(公告)日：2000-04-11
申请号：US299271
申请日：1999-04-26
申请人： Guillaume De Manteuil , Christine Lila , Tony Verbeuren , Alain Rupin
发明人： Guillaume De Manteuil , Christine Lila , Tony Verbeuren , Alain Rupin
IPC分类号： C07D333/58 , A61K31/00 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/506 , A61P7/00 , A61P7/02 , A61P43/00 , C07D333/60 , C07D333/64 , C07D401/06 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D495/04 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D333/64 , C07D401/06 , C07D409/06 , C07D409/14
摘要： A compound of formula (I): ##STR1## wherein: X represents oxygen, sulphur, or NR.sub.3 wherein R.sub.3 is as defined in the description,Y represents oxygen, sulphur, NR.sub.3, or may a single bond when X represents NR.sub.3,Z represents nitrogen, carbon, or CH,A represents a single bond, alkylene (optionally substituted), arylene, cycloalkylene, heterocycle, or --SO.sub.2 --R.sub.4 -- wherein R.sub.4 is as defined in the description,W represents hydroxy, alkoxy, aryloxy, arylalkoxy, cycloalkyloxy, heterocycle bonded to oxygen, amino, or hydroxyamino,Ra, Rb, Rc, Rd, which may be the same or different, each independently of the others are as defined in the description,R.sub.1 represents aryl substituted by one to five identical or different substituents, each independently of the others,R.sub.2 represents hydrogen, alkyl, aryl, arylalkyl, cycloalkyl, heterocycle, heterocycloalkyl, or another group as defined in the description,isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful in the treatment of thrombosis, pathologies for which the origin is thrombosis, or pathologies causing an increase in risk of thrombosis.
摘要翻译：式（I）的化合物：其中：X表示氧，硫或NR 3，其中R3如说明书中所定义，Y表示氧，硫，NR 3，或当X表示NR 3时可以是单键，Z表示氮，碳或CH，A表示单键，亚烷基（任选取代的），亚芳基，亚环烷基，杂环或-SO 2 -R 4 - ，其中R 4如说明书中所定义，W表示羟基，烷氧基，芳氧基，芳基烷氧基，环烷氧基，杂环与氧，氨基或羟基氨基键合的R a，R b，R c，R d各自独立地相同或不同，如说明书中所定义，R 1表示被1至5个相同或不同取代基取代的芳基， R 2代表氢，烷基，芳基，芳基烷基，环烷基，杂环，杂环烷基或说明书中定义的另一基团，其与药学上可接受的酸或碱的异构体和加成盐，以及药用产品可用于治疗血栓形成，起源于血栓形成的病理学，或导致血栓形成风险增加的病理学。

6. 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。

7. 发明授权

US5403953A 1-phenylbicyclo[2.2.2]octane compounds 失效
标题翻译： 1-苯基双环[2.2.2]辛烷化合物
公开(公告)号：US5403953A
公开(公告)日：1995-04-04
申请号：US156299
申请日：1993-11-23
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： A61K31/13 , A61K31/16 , A61K31/19 , A61K31/235 , A61K31/275 , A61K31/47 , A61P29/00 , C07C17/16 , C07C23/32 , C07C43/196 , C07C45/45 , C07C45/56 , C07C45/59 , C07C45/71 , C07C47/575 , C07C49/657 , C07C49/753 , C07C49/84 , C07C57/46 , C07C59/54 , C07C59/72 , C07C62/34 , C07C65/26 , C07C69/708 , C07C69/757 , C07C229/14 , C07C229/38 , C07C229/48 , C07C233/58 , C07C235/06 , C07C235/40 , C07C235/42 , C07C237/24 , C07C255/47 , C07C321/22 , C07C323/52 , C07D215/48 , C07D215/50 , C07D307/24 , C07D307/30 , C07D307/80 , C07D307/84 , C07D309/08 , C07D309/28 , C07D311/76 , C07C62/06
CPC分类号： C07D307/80 , C07C17/16 , C07C23/32 , C07C235/06 , C07C235/42 , C07C323/52 , C07C43/196 , C07C45/45 , C07C45/565 , C07C45/59 , C07C45/71 , C07C47/575 , C07C49/657 , C07C49/753 , C07C49/84 , C07C59/54 , C07C59/72 , C07C65/26 , C07C69/708 , C07D215/50 , C07C2102/44
摘要： Compound of formula (I): ##STR1## in which: R.sub.1 represents halogen, or hydroxy, alkyl, alkoxy, cyano, amino, mercapto, alkylthio or phenoxy,R.sub.2 and R'.sub.2 represent two hydrogen when the ring is unsaturated, or alternatively identical or different, represent hydrogen or halogen, or hydroxy, alkyl, alkoxy, cyano, amino or oxo when the ring is saturated,R.sub.3 represents any one of the following groups: ##STR2## in which: m represents 1, 2 or 3,X represents oxygen or sulfur or N-R, R.sub.5 or R.sub.6, which are identical or different, represent hydrogen or alkyl or trifluoromethyl or form (C.sub.3 -C.sub.6) cycloalkyl,n represents 0, 1 or 2,R.sub.7 represents hydroxy, alkoxy, amino, or --O--CH.sub.2 --CO--NRR',R.sub.4 represents hydrogen or halogen or alkyl, alkoxy or trihaloalkyl.
摘要翻译：式（I）化合物：其中：R 1表示卤素，或羟基，烷基，烷氧基，氰基，氨基，巯基，烷硫基或苯氧基，当环为不饱和时，R 2和R'2表示两个氢或者相同或不同，当环饱和时，R 3表示氢或氢，羟基，烷基，烷氧基，氰基，氨基或氧代，R 3表示以下基团中的任何一个：CO 2 H CONHCH 2 CO 2 H（CH 2）m CO 2 H

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