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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

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。

3. 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。

4. 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。

5. 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。

6. 发明授权

US5786330A Peptide compounds which are therapeutically active in the cascade of blood coagulation, process for preparing them and pharmaceutical compositions containing them 失效
标题翻译：在凝血级联中具有治疗活性的肽化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US5786330A
公开(公告)日：1998-07-28
申请号：US619683
申请日：1996-04-02
申请人： Jean-Luc Fauchere , Christophe Thurieau , Tony Verbeuren , Alain Rupin , Serge Simonet
发明人： Jean-Luc Fauchere , Christophe Thurieau , Tony Verbeuren , Alain Rupin , Serge Simonet
IPC分类号： A61K38/55 , A61K38/00 , A61P7/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P43/00 , C07K7/08 , C07K14/745 , C07K14/815
CPC分类号： C07K14/815 , A61K38/00 , Y10S514/822
摘要： The invention relates to the compounds of formula (I) (SEQ ID NO: I: H-phe-A.sub.1 -Arg-Pro-(Gly).sub.4 -Asn-Gly-Asp-Phe-Glu-Abo-Ile-Pro-Glu-Glu-A.sub.2 -Leu-glu-OH(I) in which A.sub.1 and A.sub.2 are as defined in the description. Medicinal products containing the same are useful as anticoagulants.
摘要翻译： PCT No.PCT / FR94 / 01166 Sec。 371日期：1996年4月2日 102（e）日期1996年4月2日PCT 1994年10月6日PCT PCT。公开号WO95 / 09869 日期：1995年04月13日本发明涉及式（I）化合物（SEQ ID NO：I：H-phe-A1-Arg-Pro-（Gly）4-Asn-Gly-Asp-Phe-Glu-Abo- Ile-Pro-Glu-Glu-A2-Leu-glu-OH（I）其中A1和A2如说明书中所定义，其药物含量可用作抗凝剂。

7. 发明授权

US08288433B2 Diazeniumdiolate compounds, a process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：二氮烯鎓二硫酸酯化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US08288433B2
公开(公告)日：2012-10-16
申请号：US12735048
申请日：2008-12-10
申请人： Alexis Cordi , Laure Haberkorn , Tony Verbeuren , Christine Courchay , Serge Simonet
发明人： Alexis Cordi , Laure Haberkorn , Tony Verbeuren , Christine Courchay , Serge Simonet
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D209/08
摘要： Compounds of formula (I): wherein: R1 represents a hydrogen atom or a —COOR group, R2 represents a group G or a linear or branched (C1-C6)alkyl group substituted by a group G, wherein G represents a —(CH2)n-A-(CH2)m—B—(CR4R5)p—(CH2)o—R6 group as defined in the description, R3 represents a hydrogen atom, an alkyl group or an NO2 group. Medicinal products containing the same which are useful in treating hypertension and cardiovascular pathologies.
摘要翻译：式（I）化合物：其中：R1表示氢原子或-COOR基团，R2表示基团G或被基团G取代的直链或支链（C1-C6）烷基，其中G表示 - （CH2 ）nA-（CH 2）m -B-（CR 4 R 5）对 - （CH 2）o -R 6基团，R 3表示氢原子，烷基或NO 2基团。含有该药物的药物可用于治疗高血压和心血管病变。

8. 发明授权

US5472979A 1,2,3,4-tetrahydronaphthalene compounds 失效
标题翻译： 1,2,3,4-四氢萘化合物
公开(公告)号：US5472979A
公开(公告)日：1995-12-05
申请号：US323508
申请日：1994-10-14
申请人： Gilbert Lavielle , Thierry Dubuffet , Olivier Muller , Michel Laubie , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
发明人： Gilbert Lavielle , Thierry Dubuffet , Olivier Muller , Michel Laubie , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
IPC分类号： A61K31/18 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/382 , A61P7/02 , A61P9/00 , A61P43/00 , C07C311/02 , C07C311/14 , C07C311/20 , C07C311/29 , C07D213/55 , C07D311/58 , C07D335/06 , A61K31/14
CPC分类号： C07D335/06 , C07C311/20 , C07D213/55 , C07D311/58
摘要： R.sub.1 and R.sub.2 form, with the carbon atoms to which they are attached, cyclopentane or cyclohexane,R.sub.3 represents hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or unsubstituted or substituted amino,R.sub.4 represents alkyl, unsubstituted or substituted phenyl, naphthyl, pyridyl or thienyl, X represents methylene or oxygen or sulfur,its enantiomers and its addition salts with a pharmaceutically acceptable base, and medicinal products containing the same are useful as anti-thrombotic.
摘要翻译：其中：R 1和R 2可以相同或不同，表示氢或卤素，烷基，取代或未取代的苯基，苄基，吡啶基甲基或咪唑基甲基或噻唑基甲基，吡啶基，咪唑基或噻唑基，或者R1 和R 2与它们所连接的碳原子形成环戊烷或环己烷，R 3表示羟基，直链或支链（C 1 -C 6）烷氧基或未取代或取代的氨基，R 4表示烷基，未取代或取代的苯基，萘基，吡啶基或噻吩基，X表示亚甲基或氧或硫，其对映体及其与药学上可接受的碱的加成盐，以及含有它们的药物可用作抗血栓形成。

9. 发明授权

US06589956B2 Benzenesulphonamide compounds 失效
标题翻译：苯磺酰胺化合物
公开(公告)号：US06589956B2
公开(公告)日：2003-07-08
申请号：US10195031
申请日：2002-07-12
申请人： Gilbert Lavielle , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Christine Vayssettes-Courchay
发明人： Gilbert Lavielle , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Christine Vayssettes-Courchay
IPC分类号： A61K31496
CPC分类号： C07D401/06 , C07D209/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： A compound of formula (I): wherein: Ra represents a hydroxy, alkoxy, aryloxy or arylalkyloxy group, A represents a CH group or a nitrogen atom, in which case R1 is as defined in the description, or R1—A together represent an oxygen atom or a group, wherein R3 and R4 are as defined in the description, R2 being a hydrogen atom or an alkyl group, Rb and Rc, which may be identical or different, each represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a hydroxy group or a trihaloalkyl group, n is an integer of from 2 to 6 inclusive, m and p are integers of from 0 to 6 inclusive, its enantiomers, diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful as a TXA2 receptor antagonist and 5-HT2 receptor antagonist.
摘要翻译：式（I）的化合物：其中：R a表示羟基，烷氧基，芳氧基或芳烷氧基，A表示CH基或氮原子，在这种情况下，R1如说明书中所定义，或者R 1 -A一起表示氧原子或基团，其中R 3和R 4如说明书中所定义，R 2为氢原子或烷基，R b和R c可以相同或不同，各自表示氢原子，卤素原子，烷基基团，烷氧基，羟基或三卤代烷基，n为2-6以下的整数，m和p为0〜6的整数，其对映体，非对映异构体及其加成盐与药学上可接受的酸或碱，以及含有它们的药物，其可用作TXA2受体拮抗剂和5-HT2受体拮抗剂。

10. 发明授权

US06541471B1 Benzenesulphonamide compounds 失效
标题翻译：苯磺酰胺化合物
公开(公告)号：US06541471B1
公开(公告)日：2003-04-01
申请号：US10195018
申请日：2002-07-12
申请人： Gilbert Lavielle , Thierry Dubuffet , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Christine Vayssettes-Courchay
发明人： Gilbert Lavielle , Thierry Dubuffet , Bernard Cimetiere , Tony Verbeuren , Serge Simonet , Christine Vayssettes-Courchay
IPC分类号： A61K315375
CPC分类号： C07D275/06 , C07C311/19 , C07D295/088 , C07D413/04 , C07D417/04
摘要： A compound of formula (I): wherein: G represents a group such as: wherein R1 and R2 independently represent a hydrogen atom or an alkyl, cycloalkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl or heteroarylalkyl group, or, R1 and R2 together with the nitrogen atom form a heterocycloalkyl group, R3 represents a hydrogen atom or an alkyl or optionally substituted phenyl group, Ra represents a hydroxy group, a linear or branched (C1-C6)alkoxy group or an amino group, Rb and Rc, which may be identical or different, each represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a hydroxy group or a trihaloalkyl group, m is an integer of from 0 to 1 inclusive, n and q are integers of from 0 to 6 inclusive, p and r are integers of from 1 to 6 inclusive, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base; and medicinal products containing the same which are useful as a TXA2 receptor antagonist and a 5-HT2 receptor antagonist.
摘要翻译：式（I）的化合物：其中：G表示如下基团：其中R1和R2独立地表示氢原子或烷基，环烷基，芳基，芳基烷基，环烷基，环烷基烷基，杂芳基或杂芳基烷基，或R1和R2 与氮原子一起形成杂环烷基，R 3表示氢原子或烷基或任选取代的苯基，R a表示羟基，直链或支链（C 1 -C 6）烷氧基或氨基，R b和R c，可以相同或不同，分别表示氢原子，卤素原子，烷基，烷氧基，羟基或三卤代烷基，m为0〜1的整数，n和q为 0〜6，p和r为1〜6的整数，其对映异构体和非对映异构体及其与药学上可接受的酸或碱的加成盐; 和含有它们的药物，其可用作TXA2受体拮抗剂和5-HT2受体拮抗剂。

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