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1. 发明授权

US06187786B1 Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles 有权
标题翻译：抑制由N-或C-连接的咪唑取代的1,8-环化喹啉酮衍生物的法呢基转移酶
公开(公告)号：US06187786B1
公开(公告)日：2001-02-13
申请号：US09380856
申请日：1999-12-20
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： A61K31473
CPC分类号： C07D471/06 , C07D455/04
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; —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; 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; -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; 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。

2. 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。

3. 发明授权

US07153958B2 Farnesyl transferase inhibiting benzoheterocyclic derivatives 有权
标题翻译：法呢基转移酶抑制苯并杂环衍生物
公开(公告)号：US07153958B2
公开(公告)日：2006-12-26
申请号：US10432292
申请日：2001-11-15
申请人： Patrick René Angibaud , Marc Gaston Venet , Virginie Sophie Poncelet
发明人： Patrick René Angibaud , Marc Gaston Venet , Virginie Sophie Poncelet
IPC分类号： C07D223/00 , C07D487/02
CPC分类号： C07D403/06 , C07D413/06 , C07D417/06
摘要： This invention comprises the novel compounds of formula (I) wherein r, s, t, X, Z, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括新的式（I）化合物，其中r，s，t，X，Z，R 1，R 2，R 3， >，R 4，R 5，R 6和R 7具有定义的含义，其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。

4. 发明授权

US08318753B2 Farnesyl transferase inhibiting 1,2-annelated quinoline enantiomer 有权
标题翻译：法呢基转移酶抑制1,2-环状喹啉对映异构体
公开(公告)号：US08318753B2
公开(公告)日：2012-11-27
申请号：US11926741
申请日：2007-10-29
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.
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。

5. 发明授权

US06420387B1 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：US06420387B1
公开(公告)日：2002-07-16
申请号：US09689211
申请日：2000-10-12
申请人： Marc Gaston Venet , Patrick René Angibaud , Philippe Muller , Gérard Charles Sanz
发明人： Marc Gaston Venet , Patrick René Angibaud , Philippe Muller , Gérard Charles Sanz
IPC分类号： A61K31445
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, hydroxyC1-6akyloxy, 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, —SR10, —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各自独立地是氢，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，一或二（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各自独立地是氢，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

6. 发明授权

US07943635B2 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：US07943635B2
公开(公告)日：2011-05-17
申请号：US11758346
申请日：2007-06-05
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： A61K31/44 , C07D471/16 , C07D487/16
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, R6 and 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，Y1，Y2，R 1，R 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。

7. 发明授权

US07129356B2 Farnesyl transferase inhibiting 4-substituted quinoline and quinazoline derivatives 有权
标题翻译：法呢基转移酶抑制4-取代喹啉和喹唑啉衍生物
公开(公告)号：US07129356B2
公开(公告)日：2006-10-31
申请号：US10451902
申请日：2001-12-21
申请人： Patrick René Angibaud , Marc Gaston Venet
发明人： Patrick René Angibaud , Marc Gaston Venet
IPC分类号： C07D215/16 , C07D215/20 , C07D401/02 , A61K31/47
CPC分类号： C07D401/06 , C07D471/04
摘要： This invention comprises the novel compounds of formula (I) wherein r, s, t, Y1, Y2, Z, R1, R2, R3, R4, R5, R6 and 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，s，t，Y 1，Y 2，Z，R 1， R 2，R 3，R 4，R 5，R 6和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。

8. 发明授权

US07053105B2 Farnesyl transferase inhibiting quinoline and quinazoline derivatives as farnesyl transferase inhibitors 有权
标题翻译：法呢基转移酶抑制喹啉和喹唑啉衍生物作为法呢基转移酶抑制剂
公开(公告)号：US07053105B2
公开(公告)日：2006-05-30
申请号：US10381363
申请日：2001-09-18
申请人： Patrick René Angibaud , Marc Gaston Venet , Isabelle Noëlle Constance Pilatte
发明人： Patrick René Angibaud , Marc Gaston Venet , Isabelle Noëlle Constance Pilatte
IPC分类号： A61K31/47 , C07D215/38 , C07D215/20
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D417/14
摘要： This invention comprises the novel compounds of formula (I) wherein r, s, t, Y1—Y2, R1, R2, R3, R4, R5 and 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，s，t，Y 1，...，R 2，R 1， SUP> 2，R 3，R 4，R 5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。

9. 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。

10. 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。

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