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11. 发明授权

US07655654B2 Farnesyl transferase inhibiting tricyclic quinazoline derivatives substituted with carbon-linked imidazoles or triazoles 有权
标题翻译：被碳链接的咪唑或三唑取代的法呢基转移酶抑制性三环喹唑啉衍生物
公开(公告)号：US07655654B2
公开(公告)日：2010-02-02
申请号：US11776416
申请日：2007-07-11
申请人： Patrick René Angibaud , Marc Gaston Venet , Jean Michel Jacques Raymond Argoullon
发明人： Patrick René Angibaud , Marc Gaston Venet , Jean Michel Jacques Raymond Argoullon
IPC分类号： C07D471/00 , A61K31/495
CPC分类号： C07D487/04 , A61K31/519 , Y02A50/411
摘要： This invention comprises the novel compounds of formula (I) wherein r, s, t, R1, R2, R3, R4, R5, and R6 have defined meanings, 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r，s，t，R 1，R 2，R 3，R 4，R 5和R 6具有定义的含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

12. 发明授权

US07511138B2 Farnesyl transferase inhibiting tricyclic quinazoline derivatives substituted with carbon-linked imidazoles or triazoles 有权
标题翻译：被碳链接的咪唑或三唑取代的法呢基转移酶抑制性三环喹唑啉衍生物
公开(公告)号：US07511138B2
公开(公告)日：2009-03-31
申请号：US10509365
申请日：2003-04-14
申请人： Patrick René Angibaud , Marc Gaston Venet , Jean Michel Jacques Raymond Argoullon
发明人： Patrick René Angibaud , Marc Gaston Venet , Jean Michel Jacques Raymond Argoullon
IPC分类号： C07D471/00 , C07D487/00 , A01N43/58 , A61K31/50
CPC分类号： C07D487/04 , A61K31/519 , Y02A50/411
摘要： This invention comprises the novel compounds of formula (I) wherein r, s, t, R1, R2, R3, R4, R5, and R6 have defined meanings, 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r，s，t，R 1，R 2，R 3，R 4，R 5和R 6具有定义的含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

13. 发明授权

US07408063B2 1,8-annelated quinoline derivatives substituted with carbon-linked triazoles as farnesyl transferase inhibitors 有权
标题翻译：用碳链连接的三唑作为法呢基转移酶抑制剂取代的1,8-环化喹啉衍生物
公开(公告)号：US07408063B2
公开(公告)日：2008-08-05
申请号：US10498535
申请日：2002-12-11
申请人： Patrick René Angibaud , Marc Gaston Venet
发明人： Patrick René Angibaud , Marc Gaston Venet
IPC分类号： C07D413/04 , C07D471/06 , C07D487/06 , A61K31/4355 , A61K31/435
CPC分类号： C07D471/06 , A61K31/47 , Y02A50/411
摘要： This invention comprises the novel compounds of formula (I) wherein r, s, A, X, Y1, Y2, R1, R2, R3, and R4 have defined meanings, 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r，s，A，X，Y 1，Y 2，R 1， R 2，R 3，R 4和R 4具有具有法呢基转移酶抑制活性的定义; 其制剂，含有它们的组合物及其作为药物的用途。

14. 发明授权

US07241777B2 Benzylimidazolyl substituted 2-quinoline and quinazoline derivatives for use as farnesyl transferase inhibitors 有权
标题翻译：苄基咪唑基取代的2-喹啉和喹唑啉衍生物，用作法呢基转移酶抑制剂
公开(公告)号：US07241777B2
公开(公告)日：2007-07-10
申请号：US10508185
申请日：2003-03-18
申请人： Patrick René Angibaud , Marc Gaston Venet , Christophe Meyer , Henry Joseph Breslin
发明人： Patrick René Angibaud , Marc Gaston Venet , Christophe Meyer , Henry Joseph Breslin
IPC分类号： A01N43/42 , A61K31/47 , C07D215/00 , A61K31/498 , C07D43/02
CPC分类号： C07D401/06 , C07D401/14 , C07D471/04
摘要： This invention comprises the novel compounds of formula (I) wherein r, t, Y1, Y2, R1, R2, R3, R5, R6and R7 have defined meanings, 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r，t，Y 1，Y 2，R 1，R 2， 2，R 3，R 5，R 6和R 7具有定义的含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

15. 发明授权

US06914066B2 1,2-annelated quinoline derivatives 有权
公开(公告)号：US06914066B2
公开(公告)日：2005-07-05
申请号：US10179444
申请日：2002-06-24
申请人： Patrick René Angibaud , Marc Gaston Venet , Xavier Marc Bourdrez
发明人： Patrick René Angibaud , Marc Gaston Venet , Xavier Marc Bourdrez
IPC分类号： C07D215/06 , A61K31/4365 , A61K31/4709 , A61K31/4745 , A61K31/498 , A61K31/519 , A61P35/00 , C07D215/18 , C07D401/06 , C07D403/06 , C07D471/04 , C07D487/04 , A61K31/435 , A61K31/517
CPC分类号： C07D401/06 , A61K31/4745 , A61K31/498 , A61K31/519 , C07D403/06 , C07D471/04 , C07D487/04
摘要： This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein ═X1—X2—X3— is a trivalent radical,; >Y1—Y2— is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R1 and R2 are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkylaminoC1-6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl; or two R1 or R2 on adjacent positions form together a bivalent radical; R3 is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkylthio-C1-6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxycarbonylC1-6alkyl, C1-6alkyoxycarbonylC1-6alkyl, C1-6alkylcarbonylC1-6alkyl, C1-6alkyloxycarbonyl, aryl, arylC1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, or a radical of formula —O—R10, —S—R10 or —NR11R12; R4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

16. 发明授权

US08329714B2 Farnesyl transferase inhibiting 1,2-annelated quinoline enantiomer 有权
公开(公告)号：US08329714B2
公开(公告)日：2012-12-11
申请号：US11669587
申请日：2007-01-31
申请人： Marc Gaston Venet , Patrick René Angibaud , David William End
发明人： Marc Gaston Venet , Patrick René Angibaud , David William End
IPC分类号： A01N43/54 , A61K31/505 , C07D491/00
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.

17. 发明授权

US06458800B1 1,2-annelated quinoline derivatives 有权
标题翻译： 1,2-annelated喹啉衍生物
公开(公告)号：US06458800B1
公开(公告)日：2002-10-01
申请号：US09868992
申请日：2001-08-29
申请人： Patrick René Angibaud , Marc Gaston Venet , Xavier Marc Bourdrez
发明人： Patrick René Angibaud , Marc Gaston Venet , Xavier Marc Bourdrez
IPC分类号： C07D47104
CPC分类号： C07D401/06 , A61K31/4745 , A61K31/498 , A61K31/519 , C07D403/06 , C07D471/04 , C07D487/04
摘要： This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein ═X1—X2—X3— is a trivalent radical,; >Y1—Y2— is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R1 and R2 are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl; or two R1 or R2 on adjacent positions form together a bivalent radical; R3 is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkylthio-C1-6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxycarbonylC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C1-6alkylcarbonylC1-6alkyl, C1-6alkyloxycarbonyl, aryl, arylC1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, or a radical of formula —O—R10, —S—R10 or —NR11R12; R4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及配制药学上可接受的酸加成盐和其立体化学异构形式的化合物，其中= X 1 -X 2 -X 3 - 是三价基团; Y1-Y2-是三价基; r和s各自独立地为0,1,2,3,4或5; t为0,1,2或3; 每个R 1和R 2独立地是羟基，卤素，氰基，C 1-6烷基，三卤甲基，三卤甲氧基，C 2-6烯基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷硫基，C 1-6烷氧基C 1-6烷氧基，C 1-6烷氧基羰基，氨基C 1-6烷氧基，单或二（C 1-6烷基）氨基，单或二（C 1-6烷基）氨基C 1-6烷氧基，芳基，芳基C 1-6烷基，芳氧基或芳基C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基; 或相邻位置上的两个R1或R2一起形成二价基团; R 3是氢，卤素，C 1-6烷基，氰基，卤代C 1-6烷基，羟基C 1-6烷基，氰基C 1-6烷基，氨基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基-C 1-6烷基，氨基羰基C 1-6烷基，羟基羰基，羟基羰基C1- C 1-6烷氧基羰基C 1-6烷基，C 1-6烷基羰基C 1-6烷基，C 1-6烷氧基羰基，芳基，芳基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，或式-O-R 10基团， S-R10或-NR11R12; R4是任选取代的咪唑基; 芳基是任选取代的苯基或萘基; 具有法呢基转移酶和香叶基香叶基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

18. 发明授权

US06444812B1 Intermediate compounds in the preparation of farnnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N-or C linked imidazoles 有权
标题翻译：中间体化合物制备法尼烯基转移酶抑制被N-或C连接的咪唑取代的1,8-环化喹啉酮衍生物
公开(公告)号：US06444812B1
公开(公告)日：2002-09-03
申请号：US09725391
申请日：2000-11-29
申请人： Marc Gaston Venet , Patrick René Angibaud , Yannick Aimé Eddy Ligny , Virginie Sophie Poncelet , Gerard Charles Sanz
发明人： Marc Gaston Venet , Patrick René Angibaud , Yannick Aimé Eddy Ligny , Virginie Sophie Poncelet , Gerard Charles Sanz
IPC分类号： C07D26538
CPC分类号： C07D471/06 , C07D455/04
摘要： This invention concerns intermediates in the preparation of compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyl; R6 hydrogen, hydroxy, halo, cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar; or a radical of formula —O—R7, —S—R8, —N—R8R9; and Ar is optionally substituted phenyl; and of the preparation, thereof.
摘要翻译：本发明涉及制备药学上可接受的酸加成盐及其立体化学异构形式的化合物的中间体，其中虚线表示任选的键; X是氧或硫; -A-是式的二价基团; R 1和R 2各自独立地为氢，羟基，卤素，氰基，C 1-6烷基，三卤代甲基，三卤甲氧基，C 2-6烯基，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，C 1-6烷氧基羰基，氨基C 1-6烷氧基，或二（C 1-6烷基）氨基C 1-6烷氧基，Ar，Ar-C 1-6烷基，Ar-氧基，Ar-C 1-6烷氧基; 或者当在相邻位置R1和R2一起可以形成二价基团时; R 3和R 4各自独立地为氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基，Ar-氧基，C 1-6烷硫基，二（C 1-6烷基）氨基，三卤甲基，三卤甲氧基，可形成二价基团; R5是被氢或C1-6烷基取代的咪唑基; R6，氢，羟基，卤素，氰基，任选取代的C 1-6烷基，C 1-6烷氧基羰基或Ar; 或式-O-R7，-S-R8，-N-R8R9的基团; 和Ar是任选取代的苯基; 及其制备方法。

19. 发明授权

US06358961B1 Farnesyltransferase inhibiting quinazolinones 有权
标题翻译：法呢基转移酶抑制喹唑啉酮
公开(公告)号：US06358961B1
公开(公告)日：2002-03-19
申请号：US09687153
申请日：2000-10-13
申请人： Patrick René Angibaud , Marc Gaston Venet , Eddy Jean Edgard Freyne
发明人： Patrick René Angibaud , Marc Gaston Venet , Eddy Jean Edgard Freyne
IPC分类号： A61K31505
CPC分类号： C07D231/12 , C07D233/56 , C07D239/82 , C07D249/08 , C07D403/06 , C07D405/04
摘要： This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar1, Ar1C1-6alkyl, Ar1oxy, Ar1C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar1oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy; R5 is hydrogen, halo, cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar1; or a radical of formula —OR10, —SR10, —NR11R12; R6 is an optionally substituted imidazolyl moiety; R7 is hydrogen or C1-6alkyl provided that the dotted line does not represent a bond; R8 is hydrogen, C1-6alkyl or Ar2CH2 Het1CH2; R9 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo, or R8 and R9 taken together may form a bivalent radical; Ar1 and Ar2 are optionally substituted phenyl and Het1 is optionally substituted pyridinyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及配制药学上可接受的酸加成盐和其立体化学异构形式的化合物，其中虚线表示任选的键; X是氧或硫; R 1和R 2各自独立地为氢，羟基，卤素，氰基，C 1-6烷基，三卤代甲基，三卤甲氧基，C 2-6烯基，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，C 1-6烷氧基羰基，氨基C 1-6烷氧基，或二（C 1-6烷基）氨基C 1-6烷氧基，Ar 1，Ar 1 C 1-6烷基，Ar 1氧基，Ar 1 C 1-6烷氧基; 或者当在相邻位置R1和R2一起可以形成二价基团时; R 3和R 4各自独立地为氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基，Ar 1氧基，C 1-6烷硫基，二（C 1-6烷基）氨基，三卤甲基，三卤甲氧基; R5是氢，卤素，氰基，任意取代的C 1-6烷基，C 1-6烷氧基羰基或Ar 1; 或式-OR 10，-SR 10，-NR 11 R 12的基团; R6是任选取代的咪唑基部分; R 7是氢或C 1-6烷基，条件是虚线不代表键; R8是氢，C1-6烷基或Ar2CH2Het1CH2; R9是氢，C1-6烷基，C1-6烷氧基或卤素，或R8和R9一起可以形成二价基; Ar1和Ar2是任选取代的苯基，Het1是任选取代的吡啶基; 具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

20. 发明授权

US07378433B2 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：US07378433B2
公开(公告)日：2008-05-27
申请号：US11639043
申请日：2006-12-13
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： A61K31/425 , C07D257/04
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R 1是氢，羟基，C 1-6 - 烷基或芳基; R 2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8链烯基，任选取代的吡咯烷基或芳基; R 3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。

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