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1. 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。

2. 发明申请

US20090298874A1 BACTERIAL ATP SYNTHASE BINDING DOMAIN 有权
标题翻译：细菌ATP合酶结合域
公开(公告)号：US20090298874A1
公开(公告)日：2009-12-03
申请号：US11576023
申请日：2005-09-28
申请人： Koenraad Jozef Lodewijk Marcel Andries , Hinrich Wilhelm Helmut Göhlmann , Jean-Marc Edmond Fernand Marie Neefs , Peter Karel Maria Verhasselt , Johann Winkler , Marc René De Jonge , Lucien Marie Henricus Koymans
发明人： Koenraad Jozef Lodewijk Marcel Andries , Hinrich Wilhelm Helmut Göhlmann , Jean-Marc Edmond Fernand Marie Neefs , Peter Karel Maria Verhasselt , Johann Winkler , Marc René De Jonge , Lucien Marie Henricus Koymans
IPC分类号： A61K31/47 , C12N9/14 , G01N33/566 , C12N15/55 , C12N15/85 , C12N5/10 , A61P31/04
CPC分类号： C07K14/35 , A61K38/00 , C12N9/14
摘要： This invention provides an isolated mutant atpE protein and departing from said mutant atpE protein the identification of an ATPase binding domain. This invention also provides related nucleic acids, vectors, host cells, pharmaceutical compositions and articles of manufacture. This invention further provides methods for determining whether a test compound interacts with an atpE protein, i.e. with the ATPase binding domain of the present invention, as well as pharmaceuticals compositions comprising said test compound, in particular as antimicrobials, more particular as antimycobacterial agent, even more particular for treating tuberculosis in a subject.
摘要翻译：本发明提供了一种分离的突变型atpE蛋白，并从所述突变型atpE蛋白中脱离鉴定ATP酶结合结构域。本发明还提供了相关的核酸，载体，宿主细胞，药物组合物和制品。本发明还提供了用于确定测试化合物是否与atpE蛋白（即与本发明的ATP酶结合结构域）相互作用的方法，以及包含所述测试化合物，特别是作为抗微生物剂的药物组合物，更特别地作为抗分枝杆菌剂，甚至更具体地用于治疗受试者的结核病。

3. 发明授权

US07585861B2 HIV inhibiting 1,2,4-triazines 有权
标题翻译： HIV抑制1,2,4-三嗪
公开(公告)号：US07585861B2
公开(公告)日：2009-09-08
申请号：US10544584
申请日：2004-02-05
申请人： Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Jozef Herwig Arts, legal representative , Marc René de Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Ruben Gerardus George Leenders , Georges Joseph Cornelius Hoomaert , Amuri Kilonda , Donald William Ludovici
发明人： Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Marc René de Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Ruben Gerardus George Leenders , Georges Joseph Cornelius Hoomaert , Amuri Kilonda , Donald William Ludovici
IPC分类号： C07D253/075 , A61K31/53 , A61P31/18 , C07D403/12 , C07D403/14
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：本发明涉及如本说明书中定义的式（I）的HIV复制抑制剂，其用作药物，其制备方法和包含它们的药物组合物。

4. 发明授权

US07442705B2 HIV replication inhibiting pyrimidines and triazines 有权
标题翻译： HIV复制抑制嘧啶和三嗪
公开(公告)号：US07442705B2
公开(公告)日：2008-10-28
申请号：US10545358
申请日：2004-02-20
申请人： Jerôme Emile Georges Guillemont , Elisabeth Thérese Jeanne Pasquier , Jan Heeres , Kurt Hertogs , Eva Bettens , Paulus Joannes Lewi , Marc René De Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Frank Xavier Jozef Herwig, legal representative
发明人： Paul Adriaan Jan Janssen
IPC分类号： C07D239/47 , C07D239/48 , C07D407/12 , A61K31/505 , A61P31/18
CPC分类号： C07D239/47 , C07D239/48 , C07D413/12
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, 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N-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，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。

5. 发明授权

US07105522B2 HIV inhibiting pyrazinone derivatives 有权
公开(公告)号：US07105522B2
公开(公告)日：2006-09-12
申请号：US10468447
申请日：2002-03-13
申请人： Paul Adriaan Jan Janssen , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Lucien Maria Henricus Koymans , Marc René de Jonge , Jan Heeres , Frederik Frans Desire Daeyaert , Georges Joseph Cornelius Hoornaert , Frans Josef Cornelius Compernolle , Amuri Kilonda
发明人： Paul Adriaan Jan Janssen , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Lucien Maria Henricus Koymans , Marc René de Jonge , Jan Heeres , Frederik Frans Desire Daeyaert , Georges Joseph Cornelius Hoornaert , Frans Josef Cornelius Compernolle , Amuri Kilonda
IPC分类号： A61K31/4965 , C07D401/00 , C07D403/00 , C07D405/00 , C07D241/02
CPC分类号： C07D241/20
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 R1 is hydrogen, hydroxy, cyano, amino, mono-or di(C1-4alkyl)amino, formyl, carboxyl, C1-6alkyl, hydroxyC1-6alkyl, polyhaloC1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkylcarbonyl, aminocarbonyl, —S(═O)m—NH2, mono-or di(C1-4alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy, aryl, arylC1-6alkyl or aryloxy; R2 is hydrogen; halo; mercapto; formyl; cyano; carboxy; azido; hydroxy; oxiranyl; amino; mono- or di(C1-4alkyl)amino; formylamino; R5R6N—C(═O)—; R7—N═C(R8)—; C1-6alkyl-S(═O)m; aryl-S(═O)m; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C1-6alkyloxy; hydroxyC1-6alkyloxy; aminoC1-6alkyloxy; mono- or di(C1-4alkyl)amino-C1-6alkyloxy; C1-6alkylcarbonyl; arylcarbonyl; Het1carbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aryl; aryloxy; arylC1-6alkyloxy; arylthio; arylC1-6alkylthio; mono- or di(aryl)amino; Het1; Het1oxy; Het1thio; Het1C1-6alkyloxy; Het1C1-6alkylthio; mono- or di(Het1)amino; C3-7cycloalkyl; C3-7cycloalkyloxy; C3-7cycloalkylthio; C1-6alkylthio; hydroxyC1-6alkylthio; aminoC1-6alkylthio; mono- or di(C1-4alkyl)aminoC1-6alkylthio; optionally substituted C1-6alkyl; R3 or R4 each independently represent optionally be substituted phenyl, pyridyl, pyrimidinyl, pyrazinyl or pyridazinyl; —X— is a bivalent radical selected from —NR14—, —NH—NH—, —N═N—, —O—, —C1-6alkanediyl-, —C(═O)—, —CHOH—, —S—, —S(═O)m—; aryl is optionally substituted phenyl; Het1, Het2 or Het3 represent an optionally substituted monocyclic or bicyclic heterocycle; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

6. 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。

7. 发明申请

US20120076835A1 HIV INHIBITING PYRIMIDINES DERIVATIVES 审中-公开
标题翻译：艾滋病毒抑制吡啶衍生物
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。

8. 发明授权

US08080551B2 HIV inhibiting pyrimidines derivatives 有权
标题翻译： HIV抑制嘧啶衍生物
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。

9. 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.

10. 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。

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