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1. 发明授权

US07592356B2 Triazoles as farnesyl transferase inhibitors 有权
标题翻译：三唑作为法呢基转移酶抑制剂
公开(公告)号：US07592356B2
公开(公告)日：2009-09-22
申请号：US11926858
申请日：2007-10-29
申请人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
发明人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
IPC分类号： A61K31/47 , C07D249/08
CPC分类号： C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12
摘要： a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ═Z1—Z2═Z3— represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2), wherein n is 1 to 4, C(═O), C(═S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.
摘要翻译：前药，N-氧化物，加成盐，季胺或其立体化学异构形式，其中L 1和L 2是R 1 -Y-，其中每个（R 1 -Y） - 取代基独立地彼此定义; Y是C1-4烷二基，C2-4亚烯基，C2-4炔二基，C（-O）或直接键; R1是氢，氰基，芳基或取代或未取代的C1-14杂环; -Z1-Z2-Z3-表示式-N-N-CH-（a-1），-N-CH-N-（a-2），-CH-N-N-（a-3） X是SO 2，（CH 2），其中n是1至4，C（-O），C（-S）或直接键; R 2是芳基，C 3-7环烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，羟基C 1-6烷基，羟基C 1-6烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷氧基羰基，C 1-6烷硫基，羟基C 1-6烷基，羟基C 1-6烷氧基，羟基C 1-6烷硫基和芳基C 1-6烷硫基; R3是芳基，-NR5R6，取代或未取代的C1-14杂环，或被取代或未取代的C1-14杂环或芳基取代的C2-4亚烯基; R4是氢，芳基，C3-7环烷基，C1-6烷基或被C3-7环烷基取代的C1-6烷基，羟基羰基，C1-4烷氧基羰基或芳基; R 5和R 6各自独立地选自氢，取代或未取代的C 1-14杂环，芳基，C 1-12烷基和被一个或多个选自羟基，芳基，芳氧基或取代或未取代的C 1-14杂环的取代基取代的C 1-12烷基。

2. 发明授权

US07511061B2 Triazoles as farnesyl transferase inhibitors 有权
标题翻译：三唑作为法呢基转移酶抑制剂
公开(公告)号：US07511061B2
公开(公告)日：2009-03-31
申请号：US11143814
申请日：2005-06-02
申请人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
发明人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
IPC分类号： A61K31/4196 , A61K31/47 , C07D215/00 , C07D249/06
CPC分类号： C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12
摘要： A prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; =Z1-Z2=Z3- represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(═O), C(═S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.
摘要翻译：前药，N-氧化物，加成盐，季胺或其立体化学异构形式，其中L 1和L 2是R 1 -Y-，其中每个（R 1 -Y） - 取代基独立地彼此定义; Y是C1-4烷二基，C2-4亚烯基，C2-4炔二基，C（-O）或直接键; R1是氢，氰基，芳基或取代或未取代的C1-14杂环; = Z1-Z2 = Z3-表示式-N-N-CH-（a-1），-N-CH-N-（a-2），-CH-N-N-（a-3） X是SO 2，（CH 2）n，其中n是1至4，C（-O），C（-S）或直接键; R 2是芳基，C 3-7环烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，羟基C 1-6烷基，羟基C 1-6烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷氧基羰基，C 1-6烷硫基，羟基C 1-6烷基，羟基C 1-6烷氧基，羟基C 1-6烷硫基和芳基C 1-6烷硫基; R3是芳基，-NR5R6，取代或未取代的C1-14杂环，或被取代或未取代的C1-14杂环或芳基取代的C2-4亚烯基; R4是氢，芳基，C3-7环烷基，C1-6烷基或被C3-7环烷基取代的C1-6烷基，羟基羰基，C1-4烷氧基羰基或芳基; R 5和R 6各自独立地选自氢，取代或未取代的C 1-14杂环，芳基，C 1-12烷基和被一个或多个选自羟基，芳基，芳氧基或取代或未取代的C 1-14杂环的取代基取代的C 1-12烷基。

3. 发明授权

US07049324B1 Triazoles as farnesyl transferase inhibitors 有权
公开(公告)号：US07049324B1
公开(公告)日：2006-05-23
申请号：US10130322
申请日：2000-11-15
申请人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
发明人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
IPC分类号： A61K31/47 , C07D215/38 , C07D249/08
CPC分类号： C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D487/14
摘要： a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ═Z1—Z2═Z3— represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(═O), C(═S), or a direct bond, R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.

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

US06365600B1 (Imidazol-5-yl)methyl-2-quinolinone derivatives as inhibitors of smooth muscle cell proliferation 有权
标题翻译：（咪唑-5-基）甲基-2-喹啉酮衍生物作为平滑肌细胞增殖抑制剂
公开(公告)号：US06365600B1
公开(公告)日：2002-04-02
申请号：US09445009
申请日：1999-11-30
申请人： David William End , Michael J. Zelesko
发明人： David William End , Michael J. Zelesko
IPC分类号： A61K3147
CPC分类号： A61K31/4709
摘要： This invention comprises the use of 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, quinolinylC1-6alkyul, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula —Alk1—C(=))—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, Ar1Ar2C1-6alkyl, Ar2-oxy, Ar2C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; R4 and R5 each independently are hydrogen, halo, Ar1, C1-6-alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbony, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkul or C1-6alkylS(O)2C1-6alkyl; R6 and R7 independenly are hydrogen, halo, cyano, C1-6alkyl, 4,4-dimethyl-oxazolyl, C1-6alkyloxy or Ar2oxyl 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, C106alkyloxycarbonyl, Ar1; R18 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R19 is hydrogen or C1-6alkyl; for the manufacture of a medicament to inhibit smooth muscle cell proliferation.
摘要翻译：本发明包括使用式（I）的化合物，其中虚线表示任选的键; X是氧或硫; R 1是氢，C 1-12烷基，Ar 1，Ar 2 C 1-6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（=））-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，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，三卤甲基，三卤甲氧基，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; R6和R7独立地是氢，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烷基，氰基C 1-6烷基，C 1-6

6. 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.

7. 发明申请

US20120108634A1 FARNESYL PROTEIN TRANSFERASE INHIBITOR COMBINATIONS WITH ANTIESTROGEN AGENTS 审中-公开
标题翻译：肉桂蛋白转移抑制剂与安定剂代谢物的组合
公开(公告)号：US20120108634A1
公开(公告)日：2012-05-03
申请号：US13343125
申请日：2012-01-04
申请人： David William End
发明人： David William End
IPC分类号： A61K31/4709 , A61P35/00
CPC分类号： A61K31/135 , A61K31/47 , A61K31/505 , A61K2300/00
摘要： The present invention is concerned with combinations of a farnesyl transferase inhibitor and an antiestrogen agent for inhibiting the growth of tumor cells, useful in the treatment of cancer.
摘要翻译：本发明涉及法尼基转移酶抑制剂和抗雌激素剂的组合，用于抑制肿瘤细胞的生长，其可用于治疗癌症。

8. 发明授权

US06743805B2 Method of use of (imidazol-5-yl)methyl-2-quinolinone derivatives to inhibit smooth muscle cell proliferation 有权
标题翻译：（咪唑-5-基）甲基-2-喹啉酮衍生物抑制平滑肌细胞增殖的方法
公开(公告)号：US06743805B2
公开(公告)日：2004-06-01
申请号：US09996147
申请日：2001-11-28
申请人： David William End , Michael J. Zelesko
发明人： David William End , Michael J. Zelesko
IPC分类号： A61K3147
CPC分类号： A61K31/4709
摘要： This invention comprises the use of 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; for the manufacture of a medicament to inhibit smooth muscle cell proliferation.
摘要翻译：本发明包括使用式（I）的化合物，其中虚线表示任选的键; X是氧或硫; R 1是氢，C 1-12烷基，Ar 1，Ar 2 C 1-6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，单或二（C 1-6烷基）氨基C 1-6烷基，氨基C 1-6烷基或式-Ak 1 -C（= O）-R 9，-AlK 1 -S（O）-R 9或-Alk （O）2 -R 9; 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，三卤甲基，三卤甲氧基，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烷基，氰基C

9. 发明授权

US06451812B1 Farnesyl protein transferase inhibitors for treating arthropathies 有权
标题翻译：用于治疗关节病的法呢基蛋白转移酶抑制剂
公开(公告)号：US06451812B1
公开(公告)日：2002-09-17
申请号：US09743077
申请日：2001-01-03
申请人： David William End , Marina Lucie Louise Cools , Jean Pierre Frans Van Wauwe
发明人： David William End , Marina Lucie Louise Cools , Jean Pierre Frans Van Wauwe
IPC分类号： A61K3147
CPC分类号： A61K31/4709 , A61K31/47 , A61K31/4704
摘要： The present invention is concerned with the finding that farnesyl protein transferase inhibitors are useful for preparing a pharmaceutical composition for treating arthropathies such as rheumatoid arthritis, osteoarthritis, juvenile arthritis, and gout.
摘要翻译：本发明涉及法呢基蛋白转移酶抑制剂可用于制备治疗关节病如药物性关节炎，骨关节炎，幼年关节炎和痛风的药物组合物。

10. 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.

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