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31. 发明授权

US06936626B2 Retinoic acid mimetic anilides 有权
公开(公告)号：US06936626B2
公开(公告)日：2005-08-30
申请号：US09962551
申请日：2001-09-25
申请人： Dominique Mabire , Christophe Denis Adelinet , Imré Christian Csoka , Marc Gaston Venet
发明人： Dominique Mabire , Christophe Denis Adelinet , Imré Christian Csoka , Marc Gaston Venet
IPC分类号： A61K31/4164 , A61K31/4196 , A61K31/427 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61P17/00 , A61P43/00 , C07D207/335 , C07D207/337 , C07D213/40 , C07D233/56 , C07D233/61 , C07D249/08 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D521/00 , C07D213/02 , A61K31/44
CPC分类号： C07D231/12 , C07D233/56 , C07D233/61 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk—NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het represents an optionally substituted unsaturated heterocycle; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

32. 发明授权

US06486187B1 N-[4-(heteroarylmethyl)phenyl]-heteroarylamines 有权
标题翻译： N- [4-（杂芳基甲基）苯基] - 杂芳基胺
公开(公告)号：US06486187B1
公开(公告)日：2002-11-26
申请号：US09624966
申请日：2000-07-25
申请人： Marc Gaston Venet , Dominique Jean-Pierre Mabire , Jean Fernand Armand Lacrampe , Gerard Charles Sanz
发明人： Marc Gaston Venet , Dominique Jean-Pierre Mabire , Jean Fernand Armand Lacrampe , Gerard Charles Sanz
IPC分类号： A61K31422
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.
摘要翻译：本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环;是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

33. 发明授权

US06319939B1 Retinoic acid mimetic anlides 有权
标题翻译：视黄酸模拟物
公开(公告)号：US06319939B1
公开(公告)日：2001-11-20
申请号：US09555775
申请日：2000-06-01
申请人： Dominique Mabire , Christophe Denis Adelinet , Imré Christian Csoka , Marc Gaston Venet
发明人： Dominique Mabire , Christophe Denis Adelinet , Imré Christian Csoka , Marc Gaston Venet
IPC分类号： C07D22354
CPC分类号： C07D231/12 , C07D233/56 , C07D233/61 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het represents an optionally substituted unsaturated heterocycle; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中X表示O，S或NR 3; R 1表示氢，羟基，C 1-6烷基或芳基; R2表示氢; 任选取代的C 1-12烷基; C 3-7环烷基; C2-8烯基; 芳基; Het1; 或者R 1和R 2一起形成式 - （CH 2）n - 的二价基团，其中n为2,3,4,5或6; R 3表示氢，任选取代的C 1-6烷基，芳基，Het 1; R4代表氢; 羟基; 巯基 C 1-6烷氧基; C 1-6烷硫基; 芳氧基芳硫基 Het1-oxy; Het1-硫代任选取代的C 1-12烷基; 任选取代的C 2-8烯基; 任选取代的C 2-8炔基; 任选取代的C 3-7环烷基; 任选取代的C 5-7环烯基; 芳基; Het1; 或-Alk-NR 3 R 5（i）或-NR 3 R 5（ii）其中Alk表示C 1-6烷二基; 并且R 5表示氢，C 1-6烷基，芳基，Het 1，（芳基或Het 1）C 1-6烷基，（芳基或Het 1）羰基或（芳基或Het 1）C 1-6烷氧基羰基; 芳基表示任选取代的茚满基，茚基，萘基，5,6,7,8-四氢-2-萘基或苯基; Het表示任选取代的不饱和杂环; 且Het1表示任选取代的单环或双环杂环; 具有视黄酸模拟活性; 其制剂，含有它们的组合物及其作为药物的用途。

34. 发明授权

US06169096A Farnesyl protein transferase inhibiting (imidazol-5-yl)methyl-2-quinolinone derivatives 有权
标题翻译：法呢基蛋白转移酶抑制（咪唑-5-基）甲基-2-喹啉酮衍生物
公开(公告)号：US06169096A
公开(公告)日：2001-01-02
申请号：US09363353
申请日：1999-07-29
申请人： Marc Gaston Venet , Patrick Ren{acute over (e)} Angibaud , Philippe Muller , G{acute over (e)}rard Charles Sanz
发明人： Marc Gaston Venet , Patrick Ren{acute over (e)} Angibaud , Philippe Muller , G{acute over (e)}rard Charles Sanz
IPC分类号： A01N4342
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/14 , Y02P20/55
摘要： This invention comprises the novel compounds of formula (I) wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 is hydrogen, C1-12alkyl, Ar1, Ar2C1-6alkyl, quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula —Alk1—C(═O)—R9, —Alk1—S(O)—R9 or —Alk1—S(O)2—R9; R2, R3 and R16 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, aminoC1-6alkyloxy, mono-or di(C1-6alkyl)aminoC1-6alkyloxy,Ar1, Ar2C1-6alkyl, Ar2oxy, Ar2C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; R4 and R5 each independently are hydrogen, halo, Ar1, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1-6alkylS(O)2C1-6alkyl; R6 and R7 each independently are hydrogen, halo, cyano, C1-6alkyl, 4,4-dimethyl-oxazolyl, C1-6alkyloxy or Ar2oxy; R8 is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl, cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, carboxyC1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, imidazolyl, haloC1-6alkyl, C1-6alkyloxyC1-6alkyl, aminocarbonylC1-6alkyl, or a radical of formula —O—R10, —S—R10, —N—R11R12; R17 is hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxycarbonyl, Ar1; R18 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R19 is hydrogen or C1-6alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中虚线表示任选的键; X是氧或硫; R1是氢，C1-12烷基，Ar1，Ar2C1-6烷基，喹啉基C 1-6烷基，吡啶基C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，一或二（C 1-6烷基）氨基C 1-6烷基，氨基C 1-6烷基或式-Alk1-C（= O）-R9，-Alk1-S（O）-R9或-Alk1-S（O）2-R9的基团; R 2，R 3和R 16各自独立地为氢，羟基，卤素，氰基，C 1-6烷基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，氨基C 1-6烷氧基，单 - 或二（C 1-6烷基）氨基C 1-6烷氧基 Ar 1，Ar 2 C 1-6烷基，Ar 2氧基，Ar 2 C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基，三卤代甲基，三卤代甲氧基，C 2-6烯基; R 4和R 5各自独立地为氢，卤素，Ar 1，C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基S（O） C 1-6烷基或C 1-6烷基S（O）2 C 1-6烷基; R 6和R 7各自独立地为氢，卤素，氰基，C 1-6烷基，4,4-二甲基 - 恶唑基，C 1-6烷氧基或Ar 2氧基; R 8是氢，C 1-6烷基，氰基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基C 1-6

35. 发明授权

US5968952A Farnesyl transferase inhibiting 2-quinolone derivatives 失效
公开(公告)号：US5968952A
公开(公告)日：1999-10-19
申请号：US66441
申请日：1998-04-29
申请人： Marc Gaston Venet , Patrick Rene Angibaud , Gerard Charles Sanz , David William End
发明人： Marc Gaston Venet , Patrick Rene Angibaud , Gerard Charles Sanz , David William End
IPC分类号： A61K31/00 , A61K31/47 , A61K31/4709 , A61P35/00 , A61P43/00 , C07D401/06 , C07D521/00 , C07D215/16 , C07D215/04 , C07D215/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06
摘要： The present invention is concerned with compounds of formula (I), ##STR1## the stereoisomeric forms thereof and the pharmaceutically acceptable acid or base addition salts thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R.sup.1 is hydrogen, C.sub.1-12 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, quinolinylC.sub.1-6 alkyl, pyridylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)-aminoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, or a radical of formula --Alk.sup.1 --C(.dbd.O)--R.sup.9, --Alk.sup.1 --S(O)--R.sup.9 or --Alk.sup.1 --S(O).sub.2 --R.sup.9 ; R.sup.2 and R.sup.3 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxy-C.sub.1-6 alkyloxy, aminoC.sub.1-6 alkyloxy, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, Ar.sup.2 oxy, Ar.sup.2 C.sub.1-6 alkyloxy, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C.sub.2-6 alkenyl; or when on adjacent positions R.sup.2 and R.sup.3 taken together may form a bivalent radical; R.sup.4 and R.sup.5 each independently are hydrogen, Ar.sup.1, C.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkylS(O)C.sub.1-6 alkyl or C.sub.1-6 alkylS(O).sub.2 --C.sub.1-6 alkyl; R.sup.6 and R.sup.7 each independently are hydrogen, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or Ar.sup.2 oxy; R.sup.8 is hydrogen, C.sub.1-6 alkyl, cyano, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkylcarbonylC.sub.1-6 alkyl, cyanoC.sub.1-6 alkyl, C.sub.1-6 alkyloxy-carbonylC.sub.1-6 alkyl, hydroxycarbonylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, haloC.sub.1-6 alkyl, C.sub.1-6 alkyloxy-C.sub.1-6 alkyl, aminocarbonylC.sub.1-6 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyloxyC.sub.1-6 alkyl, C.sub.1-6 alkylthioC.sub.1-6 alkyl; R.sup.10 is hydrogen, C.sub.1-6 alkyl or halo; R.sup.11 is hydrogen or C.sub.1-6 alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

36. 发明授权

US5746840A Process for preparing enantiomerically pure 6-{4-chlorophenyl) (1 H-1,2,4-triazol-1-YL) methyl}-1-methyl-1 H-benzotriazole 失效
标题翻译：制备对映体纯的6- {4-氯苯基）（1H-1,2,4-三唑-1-基）甲基} -1-甲基-1H-苯并三唑的方法
公开(公告)号：US5746840A
公开(公告)日：1998-05-05
申请号：US827204
申请日：1997-03-28
申请人： Albert Louis Anna Willemsens , Walter Louis Antoine Verstappen , Alex Herman Copmans , Anna Maria Jozefa Vandendriessche , Alfons Gaston Maria De Knaep , Marc Gaston Venet
发明人： Albert Louis Anna Willemsens , Walter Louis Antoine Verstappen , Alex Herman Copmans , Anna Maria Jozefa Vandendriessche , Alfons Gaston Maria De Knaep , Marc Gaston Venet
IPC分类号： C07B57/00 , C07D249/18 , C07D403/06 , C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/18
摘要： A process for preparing (+)-6-�(4-chlorophenyl)(1H- 1,2,4-triazol-1-yl)methyl!-1-methyl-1H-benzotriazole comprising the resolution of (.+-.)-6-!(4-chlorophenyl)-hydrazinomethyl)-1-methyl-1H-benzotriazole and converting the appropriate enantiomerically pure hydrazine intermediate into (+)-6-�(4-chlorophenyl)(H- 1,2,4-triazol-1-yl)methyl!-1-methyl-1H-benzotriazole.
摘要翻译：制备（+） - 6 - [（4-氯苯基）（1 + E，H + EE-1,2,4-三唑-1-基）甲基] -1-甲基-1- H + EE-苯并三唑包括（+/-） - 6 - ]（4-氯苯基） - 肼基甲基）-1-甲基-1E'，非H + EE-苯并三唑的拆分，并将合适的对映体纯的肼中间体转化为（+） - 6 - [（4-氯苯基）（+ E，H + EE-1,2,4-三唑-1-基）甲基] -1-甲基-1E，H + EE-苯并三唑。

37. 发明授权

US07579352B2 Retinoic acid mimetic anilides 有权
标题翻译：视黄酸模拟苯胺
公开(公告)号：US07579352B2
公开(公告)日：2009-08-25
申请号：US11926699
申请日：2007-10-29
申请人： Dominique Mabire , Christophe Denis Adelinet , Imré Christian Csoka , Marc Gaston Venet
发明人： Dominique Mabire , Christophe Denis Adelinet , Imré Christian Csoka , Marc Gaston Venet
IPC分类号： A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/4196 , C07D403/02 , C07D401/06 , C07D401/02 , C07D249/08
CPC分类号： C07D231/12 , C07D233/56 , C07D233/61 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het is triazolyl; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及式I化合物的N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中X代表O，S或NR 3; R 1表示氢，羟基，C 1-6烷基或芳基; R2表示氢; 任选取代的C 1-12烷基; C 3-7环烷基; C2-8烯基; 芳基; Het1; R 3表示氢，任选取代的C 1-6烷基，芳基，Het 1; R4代表氢; 羟基; 巯基 C 1-6烷氧基; C 1-6烷硫基; 芳氧基芳硫基; Het1-oxy; Het1-硫代任选取代的C 1-12烷基; 任选取代的C 2-8烯基; 任选取代的C 2-8炔基; 任选取代的C 3-7环烷基; 任选取代的C 5-7环烯基; 芳基; Het1; 或-Alk-NR 3 R 5（i）或-NR 3 R 5（ii）其中Alk表示C 1-6烷二基; 并且R 5表示氢，C 1-6烷基，芳基，Het 1，（芳基或Het 1）C 1-6烷基，（芳基或Het 1）羰基或（芳基或Het 1）C 1-6烷氧基羰基; 芳基表示任选取代的茚满基，茚基，萘基，5,6,7,8-四氢-2-萘基或苯基; Het是三唑基; 且Het1表示任选取代的单环或双环杂环; 具有视黄酸模拟活性; 其制剂，含有它们的组合物及其作为药物的用途。

38. 发明申请

US20080114009A1 Farnesyl Transferase Inhibiting 1,2-Annelated Quinoline Enantiomer 有权
标题翻译：法呢基转移酶抑制1,2-苯胺喹啉对映体
公开(公告)号：US20080114009A1
公开(公告)日：2008-05-15
申请号：US11926741
申请日：2007-10-29
申请人： Marc Gaston Venet , Patrick Rene Angibaud , David William End
发明人： Marc Gaston Venet , Patrick Rene Angibaud , David William End
IPC分类号： A61K31/519 , C07D487/14 , A61P35/00
CPC分类号： C07D487/14 , C07D487/04
摘要： (−)-5-(3-Chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)tetrazolo-[1,5-a]quinazoline-7-methanamine and its pharmaceutically acceptable acid addition salts, and the use of such compounds in medicine especially for the treatment of cancer
摘要翻译：（ - ） - 5-（3-氯苯基）-α-（4-氯苯基）-α-（1-甲基-1H-咪唑-5-基）四唑并[1,5-a]喹唑啉-7-甲胺和其药学上可接受的酸加成盐，以及这些化合物在医药中的用途，特别是用于治疗癌症

39. 发明授权

US07179825B2 Retinoic acid mimetic anilides 有权
公开(公告)号：US07179825B2
公开(公告)日：2007-02-20
申请号：US11081393
申请日：2005-03-16
申请人： Dominique Mabire , Christophe Denis Adelinet , Imré Christian Csoka , Marc Gaston Venet
发明人： Dominique Mabire , Christophe Denis Adelinet , Imré Christian Csoka , Marc Gaston Venet
IPC分类号： C07D213/02 , A61K31/44
CPC分类号： C07D231/12 , C07D233/56 , C07D233/61 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het represents an optionally substituted unsaturated heterocycle; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

40. 发明授权

US06894046B2 IL-5 inhibiting 6-azauracil derivatives 失效
公开(公告)号：US06894046B2
公开(公告)日：2005-05-17
申请号：US09812731
申请日：2001-03-19
申请人： Eddy Jean Edgard Freyne , Jean Fernand Armand Lacrampe , Frederik Dirk Deroose , Marc Gaston Venet
发明人： Eddy Jean Edgard Freyne , Jean Fernand Armand Lacrampe , Frederik Dirk Deroose , Marc Gaston Venet
IPC分类号： C07D253/06 , A61K31/53 , A61K31/7028 , A61K31/706 , A61K51/00 , A61P17/00 , A61P27/02 , A61P27/16 , A61P29/00 , A61P37/00 , C07D253/075 , C07D401/10 , C07D403/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07H15/26 , C07D253/07
CPC分类号： C07D253/075 , C07D401/10 , C07D413/10 , C07D417/10 , C07D417/14
摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 4; X is O, S, NR5 or a direct bond; Y is O, S, NR5 or S(O)2; R1 independently is C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is Het1, C3-7cycloalkyl or optionally substituted C1-6alkyl and if X is O, S or NR5, then R2 may also represent aminocarbonyl, aminothiocarbonyl, C1-4alkylcarbonyl, C1-4alkylthiocarbonyl, arylcarbonyl, arylthiocarbonyl, Het1carbonyl or Het1thiocarbonyl; R3 and R4 independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; R3 and R4 form a C2-6alkanediyl; R5 is hydrogen or C1-4alkyl; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y—C1-4alkanediyl-C(═O)—O—R14, Het3, Het4 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl-C(═O)—O—R14, —C(═O)—O—R14, —Y—C1-4alkanediyl-C(═O)—O—R14, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R14 is hydrogen, C1-4alkyl, C3-7cycloalkyl, aminocarbonylmethylene or mono- or di(C1-4alkyl)aminocarbonylmethylene; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het4 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

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