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1. 发明授权

US6150360A Trisubstituted 1,3,5-Triazine Derivatives 失效
标题翻译：三取代1,3,5-三嗪衍生物
公开(公告)号：US6150360A
公开(公告)日：2000-11-21
申请号：US276362
申请日：1999-03-25
申请人： Frederik Frans Desire Daeyaert , Bart De Corte , Marc Rene De Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici
发明人： Frederik Frans Desire Daeyaert , Bart De Corte , Marc Rene De Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici
IPC分类号： A61K31/53 , A61P31/18 , C07D251/42 , C07D251/50 , C07D251/52 , C07D251/66 , C07D251/70 , C07D401/12 , C07D403/12 , C07D413/14 , C07D31/54
CPC分类号： C07D251/42 , C07D251/50 , C07D251/52 , C07D251/66 , C07D251/70 , C07D403/12
摘要： This invention concerns the use of the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR.sup.4 or N; n is 0, 1, 2, 3 or 4; R.sup.1 and R.sup.2 are each independently selected from hydrogen, hydroxy, C.sub.1-12 alkyl, C.sub.1-12 alkyloxy, C.sub.1-12 alkylcarbonyl, C.sub.1-12 -alkyloxycarbonyl, aryl, amino, mono- or di(C.sub.1-12 alkyl)amino, mono- or di(C.sub.1-12 alkyl)aminocarbonyl wherein each of the aforementioned C.sub.1-12 alkyl groups may optionally and each individually be substituted; or R.sup.1 and R.sup.2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C.sub.1-12 alkyl)aminoC.sub.1-4 alkylidene; R.sup.3 is hydrogen, aryl, C.sub.1-6 alkylcarbonyl, optionally substituted C.sub.1-6 alkyl; and each R.sup.4 independently is hydroxy, halo, C.sub.1-6 alkyl, C.sub.1-6 -alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is --X--R.sup.5 or --X--Alk--R.sup.6 ; wherein R.sup.5 and R.sup.6 each independently are indanyl, indolyl or phenyl; each of said indanyl, indolyl or phenyl may be substituted; and X is --NR.sup.3 --, --NH--NH--, --N.dbd.N--, --O--, --S--, --S(.dbd.O)-- or --S(.dbd.O).sub.2 --; aryl is optionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物在N-氧化物，其药学上可接受的加成盐和立体化学异构形式中的用途，其中A是CH，CR 4或N; n为0,1,2,3或4; R 1和R 2各自独立地选自氢，羟基，C 1-12烷基，C 1-12烷氧基，C 1-12烷基羰基，C 1-12烷氧基羰基，芳基，氨基，单或二（C 1-12烷基）氨基，单或二 C 1-12烷基）氨基羰基，其中每个上述C 1-12烷基可以任选地和各自独立地被取代; 或R 1和R 2可以一起形成吡咯烷基，哌啶基，吗啉基，叠氮基或单或二（C 1-12烷基）氨基C 1-4亚烷基; R3是氢，芳基，C1-6烷基羰基，任选取代的C 1-6烷基; 并且每个R 4独立地是羟基，卤素，C 1-6烷基，C 1-6 - 烷氧基，氰基，氨基羰基，硝基，氨基，三卤代甲基或三卤代甲氧基; L是-X-R5或-X-Alk-R6; 其中R 5和R 6各自独立地为茚满基，吲哚基或苯基; 所述二氢化茚基，吲哚基或苯基中的每一个可以被取代; 并且X是-NR 3 - ， - NH-NH - ， - N = N - ， - O - ， - S - ， - S（= O） - 或-S（= O）芳基是任选取代的苯基; Het是任选取代的脂族或芳族杂环基; 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。它还涉及作为式（I）化合物的亚组的新化合物，其制备方法和包含它们的药物组合物。

2. 发明申请

US20080176880A1 HIV REPLICATION INHIBITING PYRIMIDINES 有权
公开(公告)号：US20080176880A1
公开(公告)日：2008-07-24
申请号：US11930835
申请日：2007-10-31
申请人： Bart De Corte , Marc Rene 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
发明人： Bart De Corte , Marc Rene 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
IPC分类号： A61K31/505 , C07D239/42 , 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, al, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, 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(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═CO)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, —C(—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.

3. 发明授权

US07037917B2 HIV replication inhibiting pyrimidines 有权
公开(公告)号：US07037917B2
公开(公告)日：2006-05-02
申请号：US10634682
申请日：2003-08-05
申请人： Bart De Corte , Marc Rene 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
发明人： Bart De Corte , Marc Rene 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
IPC分类号： C07D239/48 , 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(C1-6alkyl)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 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.

4. 发明授权

US06878717B2 HIV replication inhibiting pyrimidines 有权
标题翻译： HIV复制抑制嘧啶
公开(公告)号：US06878717B2
公开(公告)日：2005-04-12
申请号：US09430966
申请日：1999-11-01
申请人： Bart De Corte , Marc Rene 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
发明人： Bart De Corte , Marc Rene 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
IPC分类号： C07D239/47 , A61K20060101 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/551 , A61K31/5513 , A61K31/675 , A61K31/715 , A61P31/18 , C07D20060101 , C07D239/42 , C07D239/46 , C07D239/48 , C07D239/50 , C07D239/80 , C07D401/12 , C07D403/12
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, C1-6alkyloxy-carbonyl, 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(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —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.
摘要翻译：本发明涉及下式化合物的用途：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，其中-a 1 = -a 2 -a 3 = a < 与所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，取代的C 1-6烷基或取代的C 1-6烷氧基C 1-6烷基羰基; 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，多卤代甲硫基，-S（= O）p R 6，-NH-S（= O）p R 6，-C（= O）R 6， NHC（= O）H，-C（= O）NHNH 2，-NHC（= O）R 6，-C（= NH）R 6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-; Q是氢，C 1-6烷基，卤素，多卤代-C 1-6烷基或任选取代的氨基; 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，多卤甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）pR 6，-C（= O）R 6，-NHC（= O） -C（= O）NHNH

5. 发明授权

US06372729B1 Trisubstituted 1,3,5,-triazine derivatives 失效
标题翻译：三取代1,3,5， - 三嗪衍生物
公开(公告)号：US06372729B1
公开(公告)日：2002-04-16
申请号：US09634340
申请日：2000-08-08
申请人： Frederik Frans Desiré Daeyaert , 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
发明人： Frederik Frans Desiré Daeyaert , 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
IPC分类号： C07D25166
CPC分类号： C07D251/42 , C07D251/50 , C07D251/52 , C07D251/66 , C07D251/70 , C07D403/12
摘要： This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0, 1, 2, 3 or 4; R1 and R2 are each independently selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each of the aforementioned C1-12alkyl groups may optionally and each individually be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl; and each R4 independently is hydroxy, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is —X—R5 or —X-Alk-R6; wherein R5 and R6 each independently are indanyl, indolyl or phenyl; each of said indanyl, indolyl or phenyl may be substituted; and X is —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; aryl is optionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及N-氧化物，其药学上可接受的加成盐和立体化学异构形式的化合物的用途，其中A是CH，CR 4或N; n为0,1,2,3或4; R1和R2各自独立地选自氢，羟基，C1-12烷基，C1-12烷氧基，C1-12烷基羰基，C1-12烷氧基羰基，芳基，氨基，单或二（C1-12烷基）氨基，单或二（C1- 12烷基）氨基羰基，其中各个上述C 1-12烷基可以任选地和各自独立地被取代; 或R 1和R 2可以一起形成吡咯烷基，哌啶基，吗啉基，叠氮基或单或二（C 1-12烷基）氨基C 1-4亚烷基; R3是氢，芳基，C1-6烷基羰基，任选取代的C 1-6烷基; 每个R 4独立地是羟基，卤素，C 1-6烷基，C 1-6烷氧基，氰基，氨基羰基，硝基，氨基，三卤代甲基或三卤代甲氧基; L是-X-R5或-X-Alk-R6; 其中R 5和R 6各自独立地为茚满基，吲哚基或苯基; 所述二氢化茚基，吲哚基或苯基中的每一个可以被取代; 并且X是-NR 3 - ， - NH-NH - ， - N = N - ， - O - ， - S - ， - S（= O） - 或-S（= O）芳基是任选取代的苯基; Het是任选取代的脂族或芳族杂环基; 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。它还涉及作为式（I）化合物的亚组的新化合物，其制备方法和包含它们的药物组合物。

6. 发明申请

US20110263625A1 HIV REPLICATION INHIBITING PYRIMIDINES 有权
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.

7. 发明授权

US08003789B2 HIV replication inhibiting pyrimidines 有权
标题翻译： HIV复制抑制嘧啶
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。

8. 发明授权

US06774235B2 Trisubstituted 1,3,5-triazine derivatives 失效
标题翻译：三取代1,3,5-三嗪衍生物
公开(公告)号：US06774235B2
公开(公告)日：2004-08-10
申请号：US10067383
申请日：2002-02-05
申请人： Frederik Frans Desiré Daeyaert , 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
发明人： Frederik Frans Desiré Daeyaert , 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
IPC分类号： C07D25166
CPC分类号： C07D251/42 , C07D251/50 , C07D251/52 , C07D251/66 , C07D251/70 , C07D403/12
摘要： This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0, 1, 2, 3 or 4; R1 and R2 are each independently selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each of the aforementioned C1-12alkyl groups may optionally and each individually be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl; and each R4 independently is hydroxy, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is —X—R5 or —X—Alk—R6; wherein R5 and R6 each independently are indanyl, indolyl or phenyl; each of said indanyl, indolyl or phenyl may be substituted; and X is —NR3—, —NH—NH—, —N═N—, —O—, —S —, —S(═O)— or —S(═O)2—; aryl is optionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and pharmaceutical compositions comprising them.
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A是CH，CR 4或N; n为0,1,2,3或4; R 1和R 2各自独立地选自氢，羟基，C 1-12烷基，C 1-12烷氧基，C 1-12烷基羰基，C 1-12烷氧基羰基，芳基，氨基，单或二（C 1-12烷基）氨基，单 - 或二（C 1-12烷基）氨基羰基，其中每个上述C 1-12烷基可以任选地和各自独立地被取代; 或R 1和R 2一起可以形成吡咯烷基，哌啶基，吗啉基，叠氮基或单或二（C 1-12烷基）氨基C 1-4亚烷基; R 3是氢，芳基，C 1-6烷基羰基，任选取代的C 1-6烷基; 每个R 4独立地是羟基，卤素，C 1-6烷基，C 1-6烷氧基，氰基，氨基羰基，硝基，氨基，三卤代甲基或三卤代甲氧基; L是-X-R 5或-X-Alk-R 6; 其中R 5和R 6各自独立地为茚满基，吲哚基或苯基; 所述二氢化茚基，吲哚基或苯基中的每一个可以被取代; 并且X是-NR 3 - ， - NH-NH - ， - N = N - ， - O - ， - S - ， - S（= O） - 或-S（= O）芳基是任选取代的苯基; Het是任选取代的脂族或芳族杂环基; 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。它还涉及作为式（I）化合物的亚组的新化合物，其制备方法和包含它们的药物组合物。

9. 发明授权

US07015221B2 2,4-disubstituted triazine derivatives 失效
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.

10. 发明授权

US06638932B1 2,4-disubstituted triazine derivatives 失效
标题翻译： 2,4-二取代的三嗪衍生物
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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