公开(公告)号：US20060009474A1

公开(公告)日：2006-01-12

申请号：US11225839

申请日：2005-09-13

申请人： Michael Kukla ,  Donald Ludovici ,  Robert Kavash ,  Bart De Corte ,  Jan Heeres ,  Paul Janssen ,  Lucien Koymans ,  Marc de Jonge ,  Koen Van Aken ,  Alain Krief

发明人： Michael Kukla ,  Donald Ludovici ,  Robert Kavash ,  Bart De Corte ,  Jan Heeres ,  Paul Janssen ,  Lucien Koymans ,  Marc de Jonge ,  Koen Van Aken ,  Alain Krief

IPC分类号： A61K31/519 ,  C07D487/02 ,  A61K31/506 ,  C07D239/42

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}

公开(公告)号：US20050277641A1

公开(公告)日：2005-12-15

申请号：US10649017

申请日：2003-08-27

申请人： Bart De Corte ,  Marc de Jonge ,  Jan Heeres ,  Paul Janssen ,  Robert Kavash ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

发明人： Bart De Corte ,  Marc de Jonge ,  Jan Heeres ,  Paul Janssen ,  Robert Kavash ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

IPC分类号： C07D251/46 ,  A61K9/14 ,  A61K31/53 ,  A61P31/18 ,  C07D251/16 ,  C07D251/18 ,  C07D251/48 ,  C07D43/02

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.

公开(公告)号：US20050288278A1

公开(公告)日：2005-12-29

申请号：US11204513

申请日：2005-08-16

申请人： Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Paul Janssen ,  Robert Kavash ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

发明人： Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Paul Janssen ,  Robert Kavash ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen 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.

公开(公告)号：US20050192305A1

公开(公告)日：2005-09-01

申请号：US11111400

申请日：2005-04-21

申请人： Koenraad Jozef Andries ,  Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Marcel Janssen ,  Paul Janssen ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

发明人： Koenraad Jozef Andries ,  Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Marcel Janssen ,  Paul Janssen ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

IPC分类号： C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  A61K31/506 ,  C07D43/14

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 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.

公开(公告)号：US20050197354A1

公开(公告)日：2005-09-08

申请号：US11111358

申请日：2005-04-21

申请人： Koenraad Jozef Andries ,  Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Marcel Janssen ,  Paul Janssen ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

发明人： Koenraad Jozef Andries ,  Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Marcel Janssen ,  Paul Janssen ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

IPC分类号： C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  A61K31/506 ,  C07D43/02

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 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.

公开(公告)号：US20060063789A1

公开(公告)日：2006-03-23

申请号：US10493446

申请日：2002-10-29

申请人： Eddy Jean Freyne ,  Peter Antonius ,  Marc Willems ,  Werner Johan ,  Paul Janssen ,  Paulus Joannes ,  Jan Heeres ,  Marc de Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Michael Kukla ,  Hugo Gabriel ,  Bony Nuydens ,  Marc Mercken ,  Donald Ludovici ,  Herwig Janssen ,  Paul Maria ,  Graziella Janssen ,  Jasmine Werner ,  Maroussia Janssen ,  Theodora Arts

发明人： Eddy Jean Freyne ,  Peter Antonius ,  Marc Willems ,  Werner Johan ,  Paul Janssen ,  Paulus Joannes ,  Jan Heeres ,  Marc de Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Michael Kukla ,  Hugo Gabriel ,  Bony Nuydens ,  Marc Mercken ,  Donald Ludovici ,  Herwig Janssen ,  Paul Maria ,  Graziella Janssen ,  Jasmine Werner ,  Maroussia Janssen ,  Theodora Arts

IPC分类号： A61K31/655 ,  A61K31/50 ,  A61K31/4965 ,  A61K31/513 ,  C07D241/18 ,  C07D239/47

CPC分类号： C07D239/42 ,  A61K31/506 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D403/12

摘要： This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; 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 C2-6alkenyl 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(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7; —C(═NH)R21; R4a or R4b each independently represent hydrogen, R8, —Y1—NR9—Y2—NR10R11, —Y1—NR9—Y1—R8, —Y1—NR9R10; 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： 本发明涉及式的化合物

公开(公告)号：US20050004125A1

公开(公告)日：2005-01-06

申请号：US10493452

申请日：2002-10-29

申请人： Eddy Jean Edgard Freyne ,  Peter Jacobus Buijnsters ,  Marc Willems ,  Werner Embrechts ,  Christopher Love ,  Paul Janssen ,  Paulus Lewi ,  Jan Heeres ,  Marc de Jonge ,  Lucien Koymans ,  Hendrik Vinkers ,  Koen Van Aken ,  Gaston Diels

发明人： Eddy Jean Edgard Freyne ,  Peter Jacobus Buijnsters ,  Marc Willems ,  Werner Embrechts ,  Christopher Love ,  Paul Janssen ,  Paulus Lewi ,  Jan Heeres ,  Marc de Jonge ,  Lucien Koymans ,  Hendrik Vinkers ,  Koen Van Aken ,  Gaston Diels

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 ,  A61K31/4965

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 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 C1-6alkyloxyC1-6alkylcarbonyl; 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 C2-6alkenyl 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(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7—C(═NH)R21; R4 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： 本发明涉及式的化合物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是6-元杂环; R 1是氢; 芳基; 甲酰基 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; 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; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 2-6烯基或C 2-6炔基; C 1-6烷氧基; C 1-6烷硫基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; 羧基; 氰基; 硝基 氨基; 单或二（C 1-6烷基）氨基; 多卤代C 1-6烷基; 多卤代C 1-6烷氧基; 多卤代C 1-6烷硫基; R 21; R 21 -C 1-6烷基; R 21 -O- R 21 -S-; R 21 -C（= O） - ; R 21 -S（= O）p - ; R 7 -S（= O）p-; R 7 -S（= O）p-NH-; R 21 -S（= O）p -NH-; R 7 -C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; R 7 -C（= O）-NH-; R 21 -C（= O）-NH-; -C（= NH）R 7 -C（= NH）R 21; R 4是任选取代的杂环，条件是-X-R 2和/或R 3不是氢; 其用途，包含它们的药物组合物及其制备方法。

公开(公告)号：US20060252764A1

公开(公告)日：2006-11-09

申请号：US11474855

申请日：2006-06-26

申请人： Jerome Guillemont ,  Patrice Palandijian ,  Marc De Jonge ,  Lucien Koymans ,  Hendrik Vinkers ,  Frederik Daeyaert ,  Jan Heeres ,  Koen Van Aken ,  Paulus Lewi ,  Paul Janssen ,  Frank Xavier Arts

发明人： Jerome Guillemont ,  Patrice Palandijian ,  Marc De Jonge ,  Lucien Koymans ,  Hendrik Vinkers ,  Frederik Daeyaert ,  Jan Heeres ,  Koen Van Aken ,  Paulus Lewi ,  Paul Janssen ,  Frank Xavier Arts

IPC分类号： A61K31/506 ,  C07D403/02

CPC分类号： C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07C255/42 ,  C07C257/12 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

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, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl;n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted 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 a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N═N—, —O—, —C(═O)—, C1-4alkanediyl, —CHOH—, —S—, —S(═O)p—, —X2—C1-4alkanediyl- or —C1-4alkanediyl-X2—; R3 is NHR13; NR13R14; —C(═O)—NHR13; —C(═O)—NR13R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl; substituted C2-6alkynyl; C1-6alkyl substituted with hydroxy and a second substituent; —C(═N—O—R8)—C1-4alkyl; R7; or —X3—R7; R4 is halo, hydroxy, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxy, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, formyl, amino, mono- or di(C1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

公开(公告)号：US20060293330A1

公开(公告)日：2006-12-28

申请号：US10573364

申请日：2004-09-21

申请人： Paul Janssen ,  Marc De Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Jan Heeres ,  Hendrik Vinkers ,  Ruben Leenders ,  Dirk Vandenput ,  Paul Janssen

发明人： Paul Janssen ,  Marc De Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Jan Heeres ,  Hendrik Vinkers ,  Ruben Leenders ,  Dirk Vandenput ,  Paul Janssen

IPC分类号： A61K31/519 ,  A61K31/525 ,  C07D487/02

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 —NR7—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各自表示下式的基团，其中-CD-表示式<β的二价基团。在线式描述=“在线式” - 末端=“铅”→N-CH-NR 17 - （c-1）; 或<？in-line-formula description =“In-line Formulas”end =“tail”？> <？in-line-formula description =“In-line Formulas”end =“lead”？> - NR < 7 -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表示基团时，<？in-line-formula description =“In-line Formulas”end =“tail” 式（b）所示的B为式（a）的基团。

公开(公告)号：US20070021449A1

公开(公告)日：2007-01-25

申请号：US10544735

申请日：2004-02-04

申请人： Jan Heeres ,  Paulus Lewi ,  Paul Janssen ,  Marc de Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Hendrik Vinkers ,  Jerome Guillemont ,  Elisabeth Pasquier ,  Frank Xavier Arts

发明人： Jan Heeres ,  Paulus Lewi ,  Paul Janssen ,  Marc de Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Hendrik Vinkers ,  Jerome Guillemont ,  Elisabeth Pasquier ,  Frank Xavier Arts

IPC分类号： A61K31/513 ,  C07D239/47

CPC分类号： A61K31/513 ,  C07D239/47 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： This invention concerns the use of a compound for the manufacture of a medicament for the prevention of HIV infection via sexual intercourse and related intimate contact between partners, wherein the compound is a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; and pharmaceutical compositions comprising them.

摘要翻译： 本发明涉及化合物在制备药物中的用途，所述药物通过性交和伴侣之间的相关紧密接触来预防HIV感染，其中所述化合物是式（I）的化合物，N-氧化物，药学上可接受的添加剂 盐，季胺及其立体化学异构形式，其中含-a 1〜 > 4 - 和 - b 1 - b 2 - b 3 - b 4 - 表示 苯基，吡啶基，嘧啶基，吡嗪基，哒嗪基; 和包含它们的药物组合物。