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公开(公告)号:US08153640B2
公开(公告)日:2012-04-10
申请号:US11718181
申请日:2005-10-27
申请人: Jerôme Emile Georges Guillemont , Mikaël Paugam , Bruno Francois Marie Delest , Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative
发明人: Jerôme Emile Georges Guillemont , Mikaël Paugam , Bruno Francois Marie Delest , Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen
IPC分类号: C07D473/32 , A61K31/52 , A61P31/18
CPC分类号: C07D487/04 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/34
摘要: HIV replication inhibitors of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0, 1, 2, 3 and in certain cases also 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; -A-B— is —CR5═N—, —N═N—, —CH2—CH2—, —CS—NH—, —CO—NH—, —CH═CH—; pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.
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公开(公告)号:US09487518B2
公开(公告)日:2016-11-08
申请号:US13410779
申请日:2012-03-02
申请人: Jerôme Emile Georges Guillemont , Mikaël Paugam , Bruno Francois Marie Delest , Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
发明人: Jerôme Emile Georges Guillemont , Mikaël Paugam , Bruno Francois Marie Delest , Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen
IPC分类号: C07D487/04 , A61K31/519 , C07D473/00 , C07D473/34 , A61P31/18 , A61K31/52
CPC分类号: C07D487/04 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/34
摘要: HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH═N—NH—C(═O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; -A-B— is —CR5═N—, —N═N—, —CH2—CH2—, —CS—NH—, —CO—NH—, —CH═CH—; and the use of these compounds for the prevention or the treatment of HIV infection.
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公开(公告)号:US20120076835A1
公开(公告)日:2012-03-29
申请号:US13249796
申请日:2011-09-30
申请人: Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
发明人: Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
IPC分类号: A61K9/14 , A61K31/505 , C07D405/12 , A61K31/506 , C07D417/12 , A61K31/541 , C07D401/12 , C07D409/12 , C07D413/12 , A61K31/5377 , C07D403/12 , A61K31/551 , C07D401/14 , C07D403/14 , C07D239/47 , A61P31/18 , C07D239/48 , B82Y5/00
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; 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II的HIV复制抑制剂; 它们作为药物的用途,其制备方法和包含它们的药物组合物。
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公开(公告)号:US08026245B2
公开(公告)日:2011-09-27
申请号:US10573364
申请日:2004-09-21
申请人: Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative , Paulus Joannes Lewi , Marc René de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Jan Heeres , Hendrik Maarten Vinkers , Ruben Gerardus George Leenders , Dirk Alfons Leo Vandenput
发明人: Paul Adriaan Jan Janssen , Paulus Joannes Lewi , Marc René de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Jan Heeres , Hendrik Maarten Vinkers , Ruben Gerardus George Leenders , Dirk Alfons Leo Vandenput
IPC分类号: C07D473/16 , C07D473/18 , A61K31/52 , A61K31/522 , A61P31/18 , C07D473/40
CPC分类号: A61K31/52 , C07D473/00 , C07D473/16 , C07D473/18
摘要: The present invention relates to the use of a compound of formula (I) for the manufacture of a medicament for the prevention or the treatment of HIV infection wherein the compound of formula (I) is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A and B each represents a radical of formula and wherein —C-D- represents a bivalent radical of formula —N═CH—NR17— (c-1); or —NR17—CH═N— (c-2); provided that when A represents a radical of formula (a) then B represents a radical of formula (b) and when A represents a radical of formula (b) then B represents a radical of formula (a).
摘要翻译: 本发明涉及式(I)化合物在制备用于预防或治疗HIV感染的药物中的用途,其中式(I)化合物为式I化合物,N-氧化物,药学上 其中A和B各自表示式的基团,其中-CD-表示式-N = CH-NR 17 - (c-1)的二价基团; 或-NR17-CH = N-(c-2); 条件是当A表示式(a)的基团时,B表示式(b)的基团,并且当A表示式(b)的基团时,B表示式(a)的基团。
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公开(公告)号:US20100034810A1
公开(公告)日:2010-02-11
申请号:US12567051
申请日:2009-09-25
申请人: Jan HEERES , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts , Marc Rene de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desire Daeyaert , Hendrik Maarten Vinkers , Jerome Emile Georges Gullemont , Elisabeth Theresa Jeanne Pasquier
发明人: Jan HEERES , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts , Marc Rene de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desire Daeyaert , Hendrik Maarten Vinkers , Jerome Emile Georges Gullemont , Elisabeth Theresa Jeanne Pasquier
IPC分类号: A61K31/506 , A61K39/395 , A61K38/00 , A61K31/551 , A61K31/5377 , A61K31/505 , A61P31/18
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 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; 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; and pharmaceutical compositions comprising them.
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公开(公告)号:US08080551B2
公开(公告)日:2011-12-20
申请号:US11474855
申请日:2006-06-26
申请人: Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative
发明人: Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen
IPC分类号: A61K31/501 , A61K31/497 , C07D417/12 , C07D417/14 , C07D417/06 , C07D401/12 , C07D401/14 , C07D401/06 , C07D403/12 , C07D403/14 , C07D403/06 , C07D405/12 , C07D405/14 , C07D405/06 , C07D409/14 , C07D409/12 , C07D409/06 , C07D237/20 , C07F9/02 , C07D413/06 , C07D413/12 , C07D413/14 , C07C257/06 , C07C211/40 , C07C233/03 , C07C235/06 , C07C237/20 , C07C239/08 , C07C229/34 , C07C255/49 , C07C207/02
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: HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.
摘要翻译: 公开了具有本文定义的式(I)的HIV复制抑制剂。 含有HIV复制抑制剂的药物组合物; 使用HIV复制抑制剂治疗艾滋病毒; 还公开了制备HIV复制抑制剂的方法。
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公开(公告)号:US07923554B2
公开(公告)日:2011-04-12
申请号:US11573224
申请日:2005-08-10
申请人: Georges Joseph Cornelius Hoornaert , Amuri Kilonda , Jan Heeres , Paulus Joannes Lewi , Marc René de Jonge , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Lucien Maria Henricus Koymans , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative
发明人: Georges Joseph Cornelius Hoornaert , Amuri Kilonda , Jan Heeres , Paulus Joannes Lewi , Marc René de Jonge , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Lucien Maria Henricus Koymans , Paul Adriaan Jan Janssen
IPC分类号: C07D253/07 , C07D253/065 , A61K31/53 , A61P31/18
CPC分类号: C07D253/075
摘要: The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(═O)pR6; —NH—S(═O)pR6; —C(═O)R6; —NHC(═O)H; —C(═O)NHNH2; NHC(═O)R6; C(═NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14; —C(═O)—NHR13; —C(═O)—NR13R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 or X2 represents —NR1—; —NH—NH—; —N═N—; —O—; —C(═O)—; —C1-4alkanediyl-; —CHOH—; —S—; —S(═O)p—; —X4—C1-4alkanediyl-; —C1-4alkanediyl-X4—; or —C1-4alkanediyl-X4—C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.
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8.
公开(公告)号:US20090124644A1
公开(公告)日:2009-05-14
申请号:US11813772
申请日:2006-01-27
申请人: Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts , Rudolf Leemans , Luc Jozef Raphael Moens
发明人: Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts , Rudolf Leemans , Luc Jozef Raphael Moens
IPC分类号: A61K31/505 , C07D239/24 , A61P31/18
CPC分类号: C07D239/50 , C07D239/48
摘要: HIV replication inhibitors of formula pharmaceutically acceptable addition salts or stereochemically isomeric forms thereof, wherein X is NR4, S, SO or SO2; the preparation of these compounds as well as pharmaceutical compositions comprising these compounds; the use of these compounds for the prevention or the treatment of HIV infection.
摘要翻译: 其药学上可接受的加成盐或立体化学异构形式的HIV复制抑制剂,其中X为NR4,S,SO或SO2; 这些化合物的制备以及包含这些化合物的药物组合物; 使用这些化合物预防或治疗艾滋病毒感染。
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公开(公告)号:US20090012092A1
公开(公告)日:2009-01-08
申请号:US11573224
申请日:2005-08-10
申请人: Georges Joseph Cornelius Hoornaert , Amuri Kilonda , Jan Heeres , Paulus Joannes Lewi , Marc Rene de Jonge , Frederik Frans Desire Daeyaert , Hendrik Maarten Vinkers , Lucien Maria Henricus Koymans , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
发明人: Georges Joseph Cornelius Hoornaert , Amuri Kilonda , Jan Heeres , Paulus Joannes Lewi , Marc Rene de Jonge , Frederik Frans Desire Daeyaert , Hendrik Maarten Vinkers , Lucien Maria Henricus Koymans , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
IPC分类号: A61K31/53 , C07D253/06 , A61P31/18
CPC分类号: C07D253/075
摘要: The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(═O)pR6; —NH—S(═O)pR6; —C(═O)R6; —NHC(═O)H; —C(═O)NHNH2; NHC(═O)R6; C(═NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14 —C(═O)—NHR13; —C(═O)—NR13 R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 or X2 represents —NR1—; —NH—NH—; —N═N—; —O—; —C(═O)—; —C1-4alkanediyl-; —CHOH—; —S—; —S(═O)p—; —X4—C1-4alkanediyl-; —C1-4alkanediyl-X4—; or —C1-4alkanediyl-X4—C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.
摘要翻译: 本发明涉及式N-氧化物的HIV复制抑制剂,其药学上可接受的加成盐,季胺或其立体化学异构形式,其中环A和环B表示苯基,吡啶基,哒嗪基,嘧啶基或吡嗪基; n和m为1〜4; R1表示氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷氧基羰基; 任选取代的C 1-6烷基; 被C 1-6烷氧基羰基取代的C 1-6烷氧基C 1-6烷基羰基; R2或R4代表氢; 羟基; 光环; 任选取代的C 1-6烷基; 任选取代的C 2-6烯基; 任选取代的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; 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 1-4烷基; 多卤代1-4烷基氧基; 多卤代 -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R7; R2a或R3表示氰基; 氨基羰基; 氨基; 光环; NHR13; NR 13 R 14 -C(-O)-NHR 13; -C( - ) - NR 13 R 14; -C(-O)-R 15; -CH-N-NH-C(-O)-R16; 任选取代的C 1-6烷基; 任选取代的C 1-6烷氧基; 任选取代的C 1-6烷氧基C 1-6烷基; 任选取代的C 2-6烯基; 任选取代的C 2-6炔基; -C(-N-O-R 8)-C 1-4烷基; R7或-X3-R7; X1或X2表示-NR1-; -NH-NH-; -N-N- -O-; -C(-O) - ; -C 1-4烷二基 -CHOH-; -S-; -S(-O)p - ; -X4-C1-4烷二基 -C 1-4烷二基-X4-; 或-C1-4烷二基-X4-C1-4烷二基; 它们作为药物的用途,它们用于制备用于治疗或预防HIV感染的药物的用途; 其制备方法和包含它们的药物组合物。
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公开(公告)号:US20080287511A1
公开(公告)日:2008-11-20
申请号:US11814617
申请日:2006-01-26
申请人: Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Kathleen Marie Jeanne Alice Vlaminck , Pierre Josef Hektor Valere Ottevaere , Oscar Franz Joseph Vanparijs , Frank Xavier Jozef Herwig Arts
发明人: Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Kathleen Marie Jeanne Alice Vlaminck , Pierre Josef Hektor Valere Ottevaere , Oscar Franz Joseph Vanparijs , Frank Xavier Jozef Herwig Arts
IPC分类号: A61K31/429 , C07D513/02 , A61P33/14
CPC分类号: C07D513/04
摘要: The present invention relates to the novel anthelmintic compound tetrahydro-furan-2-carboxylic acid-[3-(2,3,5,6-tetrahydro-imidazo[2,1-b]thiazol-6-yl)-phenyl]-amide and the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, as well as pharmaceutical compositions comprising said novel compound, processes for preparing said compound 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: 本发明涉及新型驱肠虫化合物四氢 - 呋喃-2-羧酸 - [3-(2,3,5,6-四氢 - 咪唑并[2,1-b]噻唑-6-基) - 苯基] 酰胺和其药学上可接受的酸加成盐及其立体化学异构形式,以及包含所述新化合物的药物组合物,制备所述化合物和组合物的方法及其作为药物的用途,特别是在治疗,控制和预防 温血动物的内寄生虫和外寄生虫感染。
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