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1. 发明申请

WO0185700A3 HIV REPLICATION INHIBITING PYRIMIDINES AND TRIAZINES 审中-公开
标题翻译：艾滋病毒复制抑制吡嗪和三氮唑
公开(公告)号：WO0185700A3
公开(公告)日：2002-02-07
申请号：PCT/EP0104991
申请日：2001-05-03
申请人： JANSSEN PHARMACEUTICA NV , KUKLA MICHAEL JOSEPH , LUDOVICI DONALD WILLIAM , KAVASH ROBERT W , CORTE BART LIEVEN DANIEL DE , HEERES JAN , JANSSEN PAUL ADRIAAN JAN , KOYMANS LUCIEN MARIA HENRICUS , JONGE MARC RENE DE , AKEN KOEN JEANNE ALFONS VAN , KRIEF ALAIN , LEENDERS RUBEN GERARDUS GEORGE
发明人： KUKLA MICHAEL JOSEPH , LUDOVICI DONALD WILLIAM , KAVASH ROBERT W , DE CORTE BART LIEVEN DANIEL , HEERES JAN , JANSSEN PAUL ADRIAAN JAN , KOYMANS LUCIEN MARIA HENRICUS , DE JONGE MARC RENE , VAN AKEN KOEN JEANNE ALFONS , KRIEF ALAIN , LEENDERS RUBEN GERARDUS GEORGE
IPC分类号： A61K31/505 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K45/00 , A61P31/18 , C07D239/46 , C07D239/47 , C07D239/48 , C07D251/16 , C07D251/18 , C07D251/22 , C07D251/46 , C07D251/50 , C07D251/52 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/12
CPC分类号： C07D239/47 , C07D239/48 , C07D251/16 , C07D251/50 , C07D401/12
摘要： This invention concerns HIV replication inhibitors of formula (I)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：本发明涉及式（I）的HIV复制抑制剂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，条件是当Q为卤素时，Z为N; 或当Q为多卤代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. 发明申请

WO0185699A3 PRODRUGS OF HIV REPLICATION INHIBITING PYRIMIDINES 审中-公开
标题翻译：艾滋病毒复制抑制抑制剂的制剂
公开(公告)号：WO0185699A3
公开(公告)日：2002-02-28
申请号：PCT/EP0104990
申请日：2001-05-03
申请人： JANSSEN PHARMACEUTICA NV , KUKLA MICHAEL JOSEPH , LUDOVICI DONALD WILLIAM , KAVASH ROBERT W , CORTE BART LIEVEN DANIEL DE , HEERES JAN , JANSSEN PAUL ADRIAAN JAN , KOYMANS LUCIEN MARIA HENRICUS , JONGE MARC RENE DE , AKEN KOEN JEANNE ALFONS VAN , KRIEF ALAIN
发明人： KUKLA MICHAEL JOSEPH , LUDOVICI DONALD WILLIAM , KAVASH ROBERT W , DE CORTE BART LIEVEN DANIEL , HEERES JAN , JANSSEN PAUL ADRIAAN JAN , KOYMANS LUCIEN MARIA HENRICUS , DE JONGE MARC RENE , VAN AKEN KOEN JEANNE ALFONS , KRIEF ALAIN
IPC分类号： C07D239/47 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/00 , A61K47/48 , A61P31/18 , A61P43/00 , C07D239/46 , C07D239/48 , C07D401/12 , C07D403/12
CPC分类号： C07D239/47 , C07D239/48 , C07D401/12
摘要： The present invention concerns compounds of the formula (I): (A1)(A2)N-R , the N -oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R is substituted C1-6alkyl; -S(=O)-R ; -S(=O)2-R ; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R being C1-6alkyl, aryl or Het ; (A1)(A2)N- is the covalently bonded form of the corresponding intermediate of the formula (A1)(A2)N-H, which is a HIV replication inhibiting pyrimidine of formula (II).
摘要翻译：本发明涉及式（I）化合物：（A1）（A2）NR 1，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是取代的C 1-6烷基; -S（= O）-R <8>; -S（= O）2-R <8>; C7-12alkylcarbonyl; 任选取代的C 1-6烷氧基羰基C 1-6烷基羰基; R 8为C 1-6烷基，芳基1或Het 1; （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（II）的HIV复制抑制性嘧啶。

3. 发明申请

WO0027828A2 2,4-DISUBSTITUTED TRIAZINE DERIVATIVES 审中-公开
标题翻译： 2,4-取代的三氮唑衍生物
公开(公告)号：WO0027828A2
公开(公告)日：2000-05-18
申请号：PCT/EP9908688
申请日：1999-11-04
申请人： JANSSEN PHARMACEUTICA NV , CORTE BART DE , JONGE MARC RENE DE , HEERES JAN , JANSSEN PAUL ADRIAAN JAN , KAVASH ROBERT W , KOYMANS LUCIEN MARIA HENRICUS , KUKLA MICHAEL JOSEPH , LUDOVICI DONALD WILLIAM , AKEN KOEN JEANNE ALFONS VAN
发明人： DE CORTE BART , DE JONGE MARC RENE , HEERES JAN , JANSSEN PAUL ADRIAAN JAN , KAVASH ROBERT W , KOYMANS LUCIEN MARIA HENRICUS , KUKLA MICHAEL JOSEPH , LUDOVICI DONALD WILLIAM , VAN AKEN KOEN JEANNE ALFONS
IPC分类号： C07D251/46 , A61K9/14 , A61K31/53 , A61P31/18 , C07D251/16 , C07D251/18 , C07D251/48 , C07D251/00
CPC分类号： A61K9/146 , Y10S977/775 , Y10S977/915
摘要： This invention concerns the use of the compounds of formula (I), the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a =a -a =a - forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R 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)pR , -NH-S(=O)pR , -C(=O)R , -NHC(=O)H, -C(=O)NHNH2, -NHC(=O)R , -C(=NH)R 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-R wherein R is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is -NR -, -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：本发明涉及式（I）化合物，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用途，其中-a 1 = a 2 -a 3 = a 4 - 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。

4. 发明申请

WO2004074266A8 HIV INHIBITING 1,2,4-TRIAZINES 审中-公开
标题翻译： HIV抑制1,2,4-三氮烯
公开(公告)号：WO2004074266A8
公开(公告)日：2004-11-11
申请号：PCT/EP2004050084
申请日：2004-02-05
申请人： JANSSEN PHARMACEUTICA NV , LEWI PAULUS JOANNES , ARTS THEODORA JOANNA FRANCISCA , JANSSEN GRAZIELLA MARIA CONSTA , JANSSEN HERWIG JOSEPHUS MARGAR , JANSSEN JASMINE JOSEE WERNER H , JANSSEN PAUL PETER MARIA HM , JANSSEN MAROUSSIA GODELIEVE FR , DE JONGE MARC RENE , KOYMANS LUCIEN MARIA HENRICUS , VINKERS HENDRIK MAARTEN , DAEYAERT FREDERIK FRANS DESIRE , HEERES JAN , LEENDERS RUBEN GERARDUS GEORGE , HOORNAERT GEORGES JOSEPH CORNE , KILONDA AMURI , LUDOVICI DONALD WILLIAM
发明人： LEWI PAULUS JOANNES , JANSSEN PAUL ADRIAAN JAN DI , DE JONGE MARC RENE , KOYMANS LUCIEN MARIA HENRICUS , VINKERS HENDRIK MAARTEN , DAEYAERT FREDERIK FRANS DESIRE , HEERES JAN , LEENDERS RUBEN GERARDUS GEORGE , HOORNAERT GEORGES JOSEPH CORNE , KILONDA AMURI , LUDOVICI DONALD WILLIAM
IPC分类号： A61K31/53 , C07D253/06 , C07D253/07 , C07D253/075
CPC分类号： A61K31/53 , C07D253/07 , C07D253/075
摘要： The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及如说明书中所定义的式（I）的HIV复制抑制剂作为药物的用途，它们的制备方法和包含它们的药物组合物。

5. 发明申请

WO2005028479A3 HIV REPLICATION INHIBITING PURINE DERIVATIVES 审中-公开
标题翻译：艾滋病毒复制抑制嘌呤衍生物
公开(公告)号：WO2005028479A3
公开(公告)日：2005-06-16
申请号：PCT/EP2004052262
申请日：2004-09-21
申请人： JANSSEN PHARMACEUTICA NV , ARTS FRANK XAVIER JOZEF HERWIG , LEWI PAULUS JOANNES , DE JONGE MARC RENE , KOYMANS LUCIEN MARIA HENRICUS , DAEYAERT FREDERIK FRANS DESIRE , HEERES JAN , VINKERS HENDRIK MAARTEN , LEENDERS RUBEN GERARDUS GEORGE , VANDENPUT DIRK ALFONS LEO
发明人： LEWI PAULUS JOANNES , DE JONGE MARC RENE , KOYMANS LUCIEN MARIA HENRICUS , DAEYAERT FREDERIK FRANS DESIRE , HEERES JAN , VINKERS HENDRIK MAARTEN , LEENDERS RUBEN GERARDUS GEORGE , VANDENPUT DIRK ALFONS LEO , JANSSEN PAUL ADRIAAN JAN DI
IPC分类号： A61K31/52 , C07D473/00 , C07D473/16 , C07D473/18 , A61P31/18
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 (I) 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 (a) or (b) and wherein -C-D- represents a bivalent radical of formula -N=CH-NR - (c-1); or -NR -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，其药学上可接受的加成盐，季胺或其立体化学异构形式，其中A和B各自表示式（a）或（b）的基团，其中-CD-表示式-N = CH- NR 17 - （c-1）; 或-NR 17 -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，当A表示式（b）的基团时，B表示式（a）的基团。

6. 发明申请

WO03037891A8 HETEROARYL AMINES AS GLYCOGEN SYNTHASE KINASE 3BETA INHIBITORS (GSK3 INHIBITORS) 审中-公开
标题翻译：作为GLYCOGEN SYNTHASE KINASE 3BETA抑制剂（GSK3抑制剂）的HETEROARYL AMINES
公开(公告)号：WO03037891A8
公开(公告)日：2003-09-04
申请号：PCT/EP0212077
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA NV , FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA , LOVE CHRISTOPHER JOHN , JANSSEN PAUL ADRIAAN JAN , LEWI PAULUS JOANNES , HEERES JAN , DE JONGE MARC RENE , KOYMANS LUCIEN MARIA HENRICUS , VINKERS HENDRIK MAARTEN , VAN AKEN KOEN JEANNE ALFONS , DIELS GASTON STANISLAS MARCELL
发明人： FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA , LOVE CHRISTOPHER JOHN , JANSSEN PAUL ADRIAAN JAN , LEWI PAULUS JOANNES , HEERES JAN , DE JONGE MARC RENE , KOYMANS LUCIEN MARIA HENRICUS , VINKERS HENDRIK MAARTEN , VAN AKEN KOEN JEANNE ALFONS , DIELS GASTON STANISLAS MARCELL
IPC分类号： A61K31/435 , A61K31/4406 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P17/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , C07D213/53 , C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： This invention concerns a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxy C1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C1-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C1-6alkyl; R21-O-; R21-S-; R21-C(=0)-; R21-S(=0)p-; R7-S =O R7-S(=O)p-NH-; R21-S(=O)p-NH-; R7-C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R7-C(=O)-NH-; R21-C(=O)-NH-; -C(=NH)R7; -C(=NH)R21; R° is an optionally substituted heterocycle provided that -X-R2 and/or R3 is other than hydrogen;their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式（I）化合物，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，其中环A为6-元杂环; R1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是直接键或连接原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 1-6烯基或C 2-6炔基; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C 1-6烷基; R21-O-; R21-S-; R21-C（= O） - ; R21-S（= O）p - ; R7-S = O R7-S（= O）p-NH-; R21-S（= O）P-NH-; R7-C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; R7-C（= O）-NH-; R21-C（= O）-NH-; -C（= NH）R 7; -C（= NH）R 21; R°是任选取代的杂环，条件是-X-R 2和/或R 3不是氢;它们的用途，包含它们的药物组合物及其制备方法。

7. 发明申请

WO2008152081A3 ANTHELMINTIC BENZO[D]ISOXAZOLYL BENZAMIDE DERIVATIVES 审中-公开
标题翻译：苯乙烯衍生物[D]异辛基苯甲酰衍生物
公开(公告)号：WO2008152081A3
公开(公告)日：2009-05-28
申请号：PCT/EP2008057348
申请日：2008-06-12
申请人： JANSSEN PHARMACEUTICA NV , HEERES JAN , LEWI PAULUS JOANNES
发明人： HEERES JAN , LEWI PAULUS JOANNES
IPC分类号： C07D261/20 , A61K31/423
CPC分类号： C07D261/20
摘要： The present invention is concerned with novel anthelmintic N-benzo[d]isoxazol-6-yl-benzamide derivatives and the pharmaceutically acceptable acid addition salts thereof, compositions comprising said novel Compounds, processes for preparing said Compounds and compositions, and the use thereof as a medicine, in particular in treatment, control and prevention of endo- and ectoparasite infections in warm-blooded animals.
摘要翻译：本发明涉及新的驱虫N-苯并[d]异恶唑-6-基 - 苯甲酰胺衍生物及其药学上可接受的酸加成盐，包含所述新化合物的组合物，制备所述化合物和组合物的方法及其用途为一种药物，特别是治疗，控制和预防温血动物的内寄生虫和外寄生虫感染。

8. 发明申请

WO2006035067A3 HIV INHIBITING 5-HETEROCYCLYL PYRIMIDINES 审中-公开
标题翻译：艾滋病毒抑制5-杂环亚氨基嘧啶
公开(公告)号：WO2006035067A3
公开(公告)日：2006-08-24
申请号：PCT/EP2005054930
申请日：2005-09-29
申请人： TIBOTEC PHARM LTD , GUILLEMONT JEROME EMILE GEORGE , HEERES JAN , LEWI PAULUS JOANNES
发明人： GUILLEMONT JEROME EMILE GEORGE , HEERES JAN , LEWI PAULUS JOANNES
IPC分类号： C07D401/04 , A61K31/505 , A61P31/18 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04
CPC分类号： C07D405/04 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04
摘要： HIV replication inhibitors of formula (I), N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a 1 =a 2 -a 3 =a 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; -b 1 =b 2 -b 3 =b 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; R 2 is OH; halo; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; -S(=O) P R 6 ; C(=NH)R 6 ; R 2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(O)-R 16 ; optionally substituted C 1-6 alkyloxyC 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 or -X 3 -R 7 ; X 1 is -NR 1 -, -O-, -C(=O)-, -CH 2 -, -CHOH-, -S-, -S(=O) P - R 3 is CN; amino; C 1-6 alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(O)-R 16 ; substituted C 1-6 alkyl; optionally substituted C 1-6 alkyloxyC 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 ; -X 3 -R 7 ; R 4 is halo; OH; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; C 3-7 cycloalkyl; C 1-6 alkyloxy; CN; nitro; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C 1-4 alkyl)amino or R 7 ; R 5 is a 5- or 6-membered completely unsaturated ring system wherein 1 - 4 ring members are nitrogen, oxygen or sulfur; which ring may optionally be substituted and may optionally be annelated with a benzene ring; methods for their preparation and pharmaceutical compositions comprising them. The invention also relates to the use of these compounds for the prevention or the treatment of HIV infection.
摘要翻译：式（I）的HIV复制抑制剂，N-氧化物，药学上可接受的加成盐，季胺或其立体异构形式，其中-a-1-a-SUP- 是-CH = CH-CH = CH-，-N = CH-CH = CH-，-N = CH-N = CH - ， - N = CH-CH = N - ， - N = N-CH = CH-; b = 1〜3 = b 4 - 是-CH = CH-CH = CH - ，-N = CH-CH = CH-，-N = CH-N = CH-，-N = CH-CH = N-，-N = N-CH = CH-; R 1是氢; 芳基; 甲酰基; ç_{1-6 烷基羰基; 任选取代的C 1-6烷基; ç_{1-6 烷氧基羰基; R 2是OH; 光环; 任选取代的C 1-6烷基，C 2-6 - 烯基或C 2-6 - 亚炔基; 取代的羰基; 羧基; CN; 硝基; 氨基; 取代氨基; 多卤代; polyhalomethylthio; -S（= O）_{P - [R ^{6 ; C（= NH）R ^{6 ; R 2a是CN; 氨基; 取代氨基; 任选取代的C 1-6烷基; 光环; 任选取代的C 1-6烷氧基; 取代的羰基; -CH = N-NH-C（O）-R ^{16 ; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6亚炔基; -C（= N-O-R ^{8 ） - c _{1-4 烷基; R 7或-X 3 -R 7; X 1是-NR 1 - ， - O - ， - C（= O） - ， - CH 2 - ， - CHOH-， -S - ， - S（= O）P 3 - （CH 3）3 CN是CN; 氨基; ç_{1-6 烷基; 光环; 任选取代的C 1-6烷氧基; 取代的羰基; -CH = N-NH-C（O）-R ^{16 ; 取代的C 1-6烷基; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6亚炔基; -C（= N-O-R ^{8 ） - c _{1-4 烷基; [R ^{7 ; -X 3→7→7; R 4是卤素; 哦; 任选取代的C 1-6烷基，C 2-6 - 烯基或C 2-6 - 亚炔基; ç_{3-7 环烷基; ç_{1-6 烷氧基; CN; 硝基; 多卤代_{1-6 烷基; 多卤代_{1-6 烷氧基; 取代的羰基; 甲酰基; 氨基; 单或二（C 1-4烷基）氨基或R 7; R 5是5-或6-元完全不饱和的环系，其中1-4个环成员是氮，氧或硫; 该环可以任选地被取代，并且可以任选被苯环取代; 其制备方法和包含它们的药物组合物。本发明还涉及这些化合物用于预防或治疗HIV感染的用途。}}}}}}}}}}}}}}}}}

9. 发明申请

WO2006035068A3 HIV INHIBITING 5-CARBO- OR HETEROCYCLIC SUBSTITUTED PYRIMIDINES 审中-公开
标题翻译：艾滋病毒抑制5-碳环或杂环取代的吡咯啉
公开(公告)号：WO2006035068A3
公开(公告)日：2006-08-31
申请号：PCT/EP2005054931
申请日：2005-09-29
申请人： TIBOTEC PHARM LTD , GUILLEMONT JEROME EMILE GEORGE , HEERES JAN , LEWI PAULUS JOANNES
发明人： GUILLEMONT JEROME EMILE GEORGE , HEERES JAN , LEWI PAULUS JOANNES
IPC分类号： C07D239/48 , A61K31/505 , A61P31/18 , C07D239/50 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/14 , C07D417/12
CPC分类号： C07D403/12 , C07D239/48 , C07D239/50 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/14 , C07D417/12
摘要： HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a 1 =a 2 -a 3 =a 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH- CH=N-, -N=N-CH=CH-; -b 1 =b 2 -b 3 =b 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally subst ituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; R 2 is OH; halo; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalo methylt hio; -S(=O)rR 6 ; C(=NH)R 6 ; R 2a is CN; amino; substituted amino; optionally subst ituted C 1-6 alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R 16 ; optionally substituted C 1-6 alkyloxy C 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 or -X 3 -R 7 ; X 1 is -NR 1 -, -O-, -C(=O)-, CH 2 , -CHOH-, -S-, -S(=O) r -; R 3 is CN; amino; C 1-6 alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R 16 ; substituted C 1-6 alkyl; optionally substituted C 1-6 alkyloxy C 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 ; -X 3 -R 7 ; R 4 is halo; OH; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; C 3-7 cycloalkyl; C 1-6 alkyloxy; CN; nitro; polyhalo C 1-6 alkyl; polyhalo C 1-6 alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C 1-4 alkyl)amino or R 7 ; R 5 is-Y-C q H2 q -L or -C q H 2q -Y-C r H 2r -L; L is aryl or Het; processes for the preparation of these compounds, pharmaceut ical compositions comprising these compounds as active ingredient and the use of these compounds for the prevention or the treatment of HIV infection.
摘要翻译：式（I）的HIV复制抑制剂N-氧化物，药学上可接受的加成盐，季胺或其立体异构形式，其中-a-1-a-2 -a 是-CH = CH-CH = CH-，-N = CH-CH = CH-，-N = CH-N = CH-， -N = CH-CH = N-，-N = N-CH = CH-; b = 1〜3 = b 4 - 是-CH = CH-CH = CH - ，-N = CH-CH = CH-，-N = CH-N = CH-，-N = CH-CH = N-，-N = N-CH = CH-; R 1是氢; 芳基; 甲酰基; ç_{1-6 烷基羰基; 任选地取代C 1-6烷基; ç_{1-6 烷氧基羰基; R 2是OH; 光环; 任选取代的C 1-6烷基，C 2-6 - 烯基或C 2-6 - 亚炔基; 取代的羰基; 羧基; CN; 硝基; 氨基; 取代氨基; 多卤代; 多卤代甲基 -S（= O）RR ^{6 ; C（= NH）R ^{6 ; R 2a是CN; 氨基; 取代氨基; 任选地取代C 1-6烷基; 光环; 任选取代的C 1-6烷氧基; 取代的羰基; -CH = N-NH-C（= O）-R ^{16 ; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6亚炔基; -C（= N-O-R ^{8 ） - c _{1-4 烷基; R 7或-X 3 -R 7; X 1是-NR 1 - ， - O - ， - C（= O） - ，CH 2，-CHOH - ，-S - ， - （= O） - ， - R 3是CN; 氨基; ç_{1-6 烷基; 光环; 任选取代的C 1-6烷氧基; 取代的羰基; -CH = N-NH-C（= O）-R ^{16 ; 取代的C 1-6烷基; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6亚炔基; -C（= N-O-R ^{8 ） - c _{1-4 烷基; [R ^{7 ; -X _{3 -R ^{7 ; R 4是卤素; 哦; 任选取代的C 1-6烷基，C 2-6 - 烯基或C 2-6 - 亚炔基; ç_{3-7 环烷基; ç_{1-6 烷氧基; CN; 硝基; 多卤C 1-6烷基; 多卤C 1-6烷氧基; 取代的羰基; 甲酰基; 氨基; 单或二（C 1-4烷基）氨基或R 7; R 5是-Y C q H 2 q -L或-C Q 2 H 2 q / SUB > -YC _{- [R ħ_{2R -L; L是芳基或Het; 这些化合物的制备方法，包含这些化合物作为活性成分的药物组合物以及这些化合物用于预防或治疗HIV感染的用途。}}}}}}}}}}}}}}}}}}

10. 发明申请

WO2006106103A3 PREVENTION OF HIV- INFECTION WITH TMC278 审中-公开
标题翻译：用TMC278预防艾滋病毒感染
公开(公告)号：WO2006106103A3
公开(公告)日：2007-06-07
申请号：PCT/EP2006061303
申请日：2006-04-04
申请人： TIBOTEC PHARM LTD , BAERT LIEVEN ELVIRE COLETTE , LEWI PAULUS JOANNES , HEERES JAN
发明人： BAERT LIEVEN ELVIRE COLETTE , LEWI PAULUS JOANNES , HEERES JAN
IPC分类号： A61K47/10 , A61K31/505 , A61K47/16 , A61P31/18
CPC分类号： A61K31/505 , A61K9/0019 , A61K47/10 , A61K47/16
摘要： This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.
摘要翻译：本发明涉及包含NNRTI TMC278的肠胃外制剂在HIV感染风险的受试者中长期预防HIV感染的用途，其包括以长时间间隔间歇施用所述制剂。

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