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公开(公告)号:US08003789B2
公开(公告)日:2011-08-23
申请号:US11930835
申请日:2007-10-31
申请人: Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries
发明人: Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号: C07D239/48 , A61K31/505 , A61K31/506 , A61P31/18
CPC分类号: A61K31/505 , A61K31/5513
摘要: This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono-or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, 13 NHC(═O)R6,—C(═NH)R6, aryl; for the treatment of subjects suffering from HIV infection.
摘要翻译: 本发明涉及式I化合物的N-氧化物,药学上可接受的加成盐,季胺,其立体化学异构体形式的用途,其中-a1 = a2-a3 = a4形成苯基,吡啶基,嘧啶基,哒嗪基,吡嗪基, 乙烯基; n为0〜5; R 1是氢,芳基,甲酰基,C 1-6烷基羰基,C 1-6烷基,C 1-6烷氧基羰基,取代的C 1-6烷基,取代的C 1-6烷氧基C 1-6烷基羰基; R2是羟基,卤素,任选取代的C 1-6烷基,C 2-6烯基或C 2-6炔基,C 3-7环烷基,C 1-6烷氧基,C 1-6烷氧基羰基,羧基,氰基,硝基,氨基,单或二(C 1-6烷基)氨基 ,多卤代甲基,多卤代甲氧基,多卤甲硫基,-S(= O)pR 6,-NH-S(= O)pR 6,-C(= O)R 6,-NHC(= O)H,-C(= O)NHNH 2, NHC(= O)R 6,-C(= NH)R 6,5元杂环; L是任选取代的C 1-10烷基,C 2-10烯基,C 2-10炔基或C 3-7环烷基; 或-X-R 3; Q是氢,C 1-6烷基,卤素,多卤代-C 1-6烷基,任选取代的氨基; Y表示羟基,卤素,C 3-7环烷基,任选取代的C 1-6烷基,C 2-6烯基或C 2-6炔基,C 1-6烷氧基,C 1-6烷氧基羰基,羧基,氰基,硝基,氨基,单 - 或二(C 1-6烷基)氨基 ,多卤甲基,多卤代甲氧基,多卤甲硫基,-S(= O)pR 6,-NH-S(= O)pR 6,-C(= O)R 6,-NHC(= O)H,-C(= O)NHNH 2, NHC(= O)R 6,-C(= NH)R 6,芳基; 用于治疗患有艾滋病毒感染的受试者。
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公开(公告)号:US20110263625A1
公开(公告)日:2011-10-27
申请号:US13177188
申请日:2011-07-06
申请人: Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries , Frank Xavier Jozef Herwig Arts
发明人: Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries , Frank Xavier Jozef Herwig Arts
IPC分类号: A61K31/505 , A61P31/18 , C07D239/50 , C07D239/48 , C07D239/47
CPC分类号: A61K31/505 , A61K31/5513
摘要: This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C3-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
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公开(公告)号:US08530655B2
公开(公告)日:2013-09-10
申请号:US13177188
申请日:2011-07-06
申请人: Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries , Frank Xavier Jozef Herwig Arts
发明人: Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号: C07D401/12 , C07D403/12 , A61K31/506 , A61P31/18
CPC分类号: A61K31/505 , A61K31/5513
摘要: This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
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公开(公告)号:US07015221B2
公开(公告)日:2006-03-21
申请号:US10649017
申请日:2003-08-27
申请人: Bart De Corte , Marc René de Jonge , Jan Heeres , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
发明人: Bart De Corte , Marc René de Jonge , Jan Heeres , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
IPC分类号: C07D251/16 , C07D251/18 , A61K31/53 , A61P31/18
CPC分类号: A61K9/146 , Y10S977/775 , Y10S977/915
摘要: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR4, —NH—S(═O)pR4, —C(═O)R4, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R4, —C(═NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(=O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
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公开(公告)号:US06638932B1
公开(公告)日:2003-10-28
申请号:US09831808
申请日:2001-08-02
申请人: Bart De Corte , Marc René de Jonge , Jan Heeres , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
发明人: Bart De Corte , Marc René de Jonge , Jan Heeres , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
IPC分类号: C07D25116
CPC分类号: A61K9/146 , Y10S977/775 , Y10S977/915
摘要: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein —a1═a2—a3═a4— forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR4, —NH—S(═O)pR4, —C(═O)R4, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R4, —C(═NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl, or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
摘要翻译: 本发明涉及配制N-氧化物的化合物,药学上可接受的加成盐,季胺及其立体化学异构形式的用途,其中-a 1 = a 2 -a 3 = a 4 - 与连接的乙烯基形成苯基,吡啶基,嘧啶基,哒嗪基或吡嗪基; n为0〜4; 并在可能的情况下5; R 1是氢,芳基,甲酰基,C 1-6烷基羰基,C 1-6烷基,C 1-6烷氧基羰基或取代的C 1-6烷基; 每个R 2独立地是羟基,卤素,任选取代的C 1-6烷基,C 2-6烯基或C 2-6炔基,C 3-7环烷基,C 1-6烷氧基,C 1-6烷氧基羰基,羧基,氰基,硝基,氨基,单或二( C 1-6烷基)氨基,多卤代甲基,多卤甲氧基,多卤甲硫基,-S(= O)p R 4,-NH-S(= O)p R 4,-C(= O)R 4, = O)H,-C(= O)NHNH 2,-NHC(= O)R 4,-C(= NH)R 4或5元杂环; p为1或2; L是任选取代的C 1-10烷基,C 2-10烯基,C 2-10炔基或C 3-7环烷基; 或L是-X-R 3,其中R 3是任选取代的苯基,吡啶基,嘧啶基,吡嗪基或哒嗪基; X是-NR 1 - , - NH-NH-,-N = N-,-O-,-C(= O) - , - CHOH-,-S-,-S(= O) - 或 - S(= O)2-; 芳基是任选取代的苯基; 用于制造用于治疗患有HIV(人类免疫缺陷病毒)感染的受试者的药物。
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公开(公告)号:US07034019B2
公开(公告)日:2006-04-25
申请号:US10275333
申请日:2001-05-03
申请人: Michael Joseph Kukla , Donald William Ludovici , Robert William Kavash , Bart Lieven Daniel De Corte , Jan Heeres , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Marc René de Jonge , Koen Jeanne Alfons Van Aken , Alain Krief
发明人: Michael Joseph Kukla , Donald William Ludovici , Robert William Kavash , Bart Lieven Daniel De Corte , Jan Heeres , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Marc René de Jonge , Koen Jeanne Alfons Van Aken , Alain Krief
IPC分类号: C07D239/46 , C07D239/48 , C07D401/12 , A61K31/505
CPC分类号: C07D239/47 , C07D239/48 , C07D401/12
摘要: The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(═O)—R8; —S(═O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula
摘要翻译: 本发明涉及式(A 1 1)(A 2 N)NR 1(I)的化合物,N-氧化物形式,药学上 可接受的加成盐,季胺和其立体化学异构形式,其中R 1是取代的C 1-6烷基; -S(-O)-R 8; -S(-O)2 -R 8; C 12-12烷基羰基; 任选取代的C 1-6烷氧基羰基C 1-6烷基羰基; 其中R 8是C 1-6烷基,芳基1或Het 1; (A 1 N 2)(A 2 N)N-是式(A 1 SUB)的相应中间体的共价键合形式(A 2)NH,其是具有下式的HIV复制抑制性嘧啶
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公开(公告)号:US07276510B2
公开(公告)日:2007-10-02
申请号:US10275931
申请日:2001-05-03
申请人: Michael Joseph Kukla , Donald William Ludovici , Robert William Kavash , Bart Lieven Daniel De Corte , Jan Heeres , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Marc René de Jonge , Koen Jeanne Alfons Van Aken , Alain Krief , Ruben Gerardus George Leenders
发明人: Michael Joseph Kukla , Donald William Ludovici , Robert William Kavash , Bart Lieven Daniel De Corte , Jan Heeres , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Marc René de Jonge , Koen Jeanne Alfons Van Aken , Alain Krief , Ruben Gerardus George Leenders
IPC分类号: C07D239/46 , C07D239/48 , A61K31/505 , C07D401/12
CPC分类号: C07D239/47 , C07D239/48 , C07D251/16 , C07D251/50 , C07D401/12
摘要: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, provided that when Q is halo then Z is N; or when Q is polyhaloC1-6alkyl then Y is hydrogen or C1-6alkyl; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
摘要翻译: 本发明涉及具有N-氧化物,药学上可接受的加成盐,季胺及其立体化学异构形式的式的HIV复制抑制剂,条件是当Q为卤素时,Z为N; 或当Q为多卤C 1-6烷基时,则Y为氢或C 1-6烷基; 它们作为药物的用途,其制备方法和包含它们的药物组合物。
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公开(公告)号:US07763631B2
公开(公告)日:2010-07-27
申请号:US11225839
申请日:2005-09-13
申请人: Michael Joseph Kukla , Donald William Ludovici , Robert William Kavash , Bart Lieven Daniel De Corte , Jan Heeres , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Marc René de Jonge , Koen Jeanne Alfons Van Aken , Alain Krief
发明人: Michael Joseph Kukla , Donald William Ludovici , Robert William Kavash , Bart Lieven Daniel De Corte , Jan Heeres , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Marc René de Jonge , Koen Jeanne Alfons Van Aken , Alain Krief
IPC分类号: C07D401/12 , A61K31/444
CPC分类号: C07D239/47 , C07D239/48 , C07D401/12
摘要: The present invention concerns compounds of formula (A1)(A2)N—R1 (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(═O)—R8; —S(═O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula
摘要翻译: 本发明涉及式(A1)(A2)(A2)(I)的化合物,N-氧化物形式,其药学上可接受的加成盐,季胺及其立体化学异构形式,其中R 1为取代的C 1-6烷基; -S(= O)-R8; -S(= O)2-R8; C7-12烷基羰基; 任选取代的C 1-6烷氧基羰基C 1-6烷基羰基; 其中R8是C1-6烷基,芳基或Het1; (A1)(A2)N-是式(A1)(A2)N-H的相应中间体的共价键合形式,其是式(I)的HIV复制抑制性嘧啶
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公开(公告)号:US08026245B2
公开(公告)日:2011-09-27
申请号:US10573364
申请日:2004-09-21
申请人: Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative , Paulus Joannes Lewi , Marc René de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Jan Heeres , Hendrik Maarten Vinkers , Ruben Gerardus George Leenders , Dirk Alfons Leo Vandenput
发明人: Paul Adriaan Jan Janssen , Paulus Joannes Lewi , Marc René de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Jan Heeres , Hendrik Maarten Vinkers , Ruben Gerardus George Leenders , Dirk Alfons Leo Vandenput
IPC分类号: C07D473/16 , C07D473/18 , A61K31/52 , A61K31/522 , A61P31/18 , C07D473/40
CPC分类号: A61K31/52 , C07D473/00 , C07D473/16 , C07D473/18
摘要: The present invention relates to the use of a compound of formula (I) for the manufacture of a medicament for the prevention or the treatment of HIV infection wherein the compound of formula (I) is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A and B each represents a radical of formula and wherein —C-D- represents a bivalent radical of formula —N═CH—NR17— (c-1); or —NR17—CH═N— (c-2); provided that when A represents a radical of formula (a) then B represents a radical of formula (b) and when A represents a radical of formula (b) then B represents a radical of formula (a).
摘要翻译: 本发明涉及式(I)化合物在制备用于预防或治疗HIV感染的药物中的用途,其中式(I)化合物为式I化合物,N-氧化物,药学上 其中A和B各自表示式的基团,其中-CD-表示式-N = CH-NR 17 - (c-1)的二价基团; 或-NR17-CH = N-(c-2); 条件是当A表示式(a)的基团时,B表示式(b)的基团,并且当A表示式(b)的基团时,B表示式(a)的基团。
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公开(公告)号:US07923554B2
公开(公告)日:2011-04-12
申请号:US11573224
申请日:2005-08-10
申请人: Georges Joseph Cornelius Hoornaert , Amuri Kilonda , Jan Heeres , Paulus Joannes Lewi , Marc René de Jonge , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Lucien Maria Henricus Koymans , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative
发明人: Georges Joseph Cornelius Hoornaert , Amuri Kilonda , Jan Heeres , Paulus Joannes Lewi , Marc René de Jonge , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Lucien Maria Henricus Koymans , Paul Adriaan Jan Janssen
IPC分类号: C07D253/07 , C07D253/065 , A61K31/53 , A61P31/18
CPC分类号: C07D253/075
摘要: The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(═O)pR6; —NH—S(═O)pR6; —C(═O)R6; —NHC(═O)H; —C(═O)NHNH2; NHC(═O)R6; C(═NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14; —C(═O)—NHR13; —C(═O)—NR13R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 or X2 represents —NR1—; —NH—NH—; —N═N—; —O—; —C(═O)—; —C1-4alkanediyl-; —CHOH—; —S—; —S(═O)p—; —X4—C1-4alkanediyl-; —C1-4alkanediyl-X4—; or —C1-4alkanediyl-X4—C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.
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