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1. 发明授权

US07276510B2 HIV replication inhibitors 有权
标题翻译： HIV复制抑制剂
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。

2. 发明授权

US07034019B2 Prodrugs of HIV replication inhibiting pyrimidines 有权
标题翻译： HIV复制抑制嘧啶的药物
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}}

3. 发明授权

US07763631B2 Prodrugs of HIV replication inhibiting pyrimidines 有权
标题翻译： HIV复制抑制嘧啶的药物
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

4. 发明授权

US08026248B2 HIV inhibiting pyrimidine derivatives 有权
标题翻译： HIV抑制嘧啶衍生物
公开(公告)号：US08026248B2
公开(公告)日：2011-09-27
申请号：US11111358
申请日：2005-04-21
申请人： Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
发明人： Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
IPC分类号： A01N43/54 , A61K31/505 , C07D239/02 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D239/49 , C07D239/50 , C07D401/12
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 to 4; Q is hydrogen or —NR1R2; R1 and R2 are 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 C1-12alkyl may optionally 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, C1-6alkyloxy-carbonyl; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; 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 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0〜4; Q是氢或-NR1R2; R1和R2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，其中每个C 1-12烷基可以任选被取代; 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; R 3是氢，芳基，C 1-6烷基羰基，任选取代的C 1-6烷基，C 1-6烷氧基羰基; R4为羟基，卤素，任选取代的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，三卤代甲氧基; R5是氢或C1-4烷基; L是任选取代的C 1-10烷基，C 3-10烯基，C 3-10炔基，C 3-7环烷基; 或L是-X1-R6或-X2-Alk-R7，其中R6和R7是任选取代的苯基; X 1和X 2是-NR 3 - ， - NH-NH - ， - N - ， - O - ， - S - ， - S（= O） - 或-S（= O） Alk是C1-4烷二基; 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组合物。

5. 发明授权

US06903213B2 HIV inhibiting pyrimidine derivatives 有权
公开(公告)号：US06903213B2
公开(公告)日：2005-06-07
申请号：US10185528
申请日：2002-06-28
申请人： Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
发明人： Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
IPC分类号： C07D239/42 , C07D239/46 , C07D239/48 , C07D239/50 , C07D401/12 , D07D239/42
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D239/49 , C07D239/50 , C07D401/12
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 to 4; Q is hydrogen or —NR1R2; R1 and R2 are 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 C1-12alkyl may optionally 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, C16alkyloxy-carbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is potionally 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 compositions comprising them.

6. 发明授权

US06440986B2 HIV Inhibiting pyrimidine derivatives 有权
标题翻译： HIV抑制嘧啶衍生物
公开(公告)号：US06440986B2
公开(公告)日：2002-08-27
申请号：US09749181
申请日：2000-12-27
申请人： Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
发明人： Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
IPC分类号： C07D23928
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D239/49 , C07D239/50 , C07D401/12
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 to 4; Q is hydrogen or —NR1R2; R1 and R2 are 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 C1-12alkyl may optionally 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, C1-6alkyloxycarbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2—Alk—R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is potionally 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 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0〜4; Q是氢或-NR1R2; R1和R2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，一或二（C1-12烷基）氨基，单或二（C1-12烷基）其中每个C 1-12烷基可以任选被取代; 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; R 3是氢，芳基，C 1-6烷基羰基，任选取代的C 1-6烷基，C 1-6烷氧基羰基。 R4为羟基，卤素，任选取代的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，三卤代甲氧基; R5是氢或C1-4烷基; L是任选取代的C 1-10烷基，C 3-10烯基，C 3-10炔基，C 3-7环烷基; 或L是-X1-R6或-X2-Alk-R7，其中R6和R7是任选取代的苯基; X1和X2是-NR3-，-NH-NH-，-N = N-，-O - ， - S - ， - S（= O） - 或-S（= O） Alk是C1-4烷二基; 芳基是取代的苯基; Het是任选取代的脂族或芳族杂环基团：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组合物。

7. 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.

8. 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。

9. 发明授权

US06197779B1 HIV inhibiting pyrimidine derivative 有权
标题翻译： HIV抑制嘧啶衍生物
公开(公告)号：US06197779B1
公开(公告)日：2001-03-06
申请号：US09276360
申请日：1999-03-25
申请人： Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
发明人： Koenraad Jozef Lodewijk Marcel Andries , Bart De Corte , Marc René De Jonge , Jan Heeres , Chih Yung Ho , Marcel August Constant Janssen , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken
IPC分类号： A61K31506
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D239/49 , C07D239/50 , C07D401/12
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 to 4; Q is hydrogen or —NR1R2; R1 and R2 are 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 C1-12alkyl may optionally 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, C1-6alkyloxycarbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is potionally 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 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0〜4; Q是氢或-NR1R2; R1和R2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，一或二（C1-12烷基）氨基，单或二（C1-12烷基）其中每个C 1-12烷基可以任选被取代; 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; R 3是氢，芳基，C 1-6烷基羰基，任选取代的C 1-6烷基，C 1-6烷氧基羰基。 R4为羟基，卤素，任选取代的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，三卤代甲氧基; R5是氢或C1-4烷基; L是任选取代的C 1-10烷基，C 3-10烯基，C 3-10炔基，C 3-7环烷基; 或L是-X1-R6或-X2-Alk-R7，其中R6和R7是任选取代的苯基; X1和X2是-NR3-，-NH-NH-，-N = N-，-O - ， - S - ， - S（= O） - 或-S（= O） Alk是C1-4烷二基; 芳基是取代的苯基; 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组合物。

10. 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.

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