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公开(公告)号：US20060194804A1
公开(公告)日：2006-08-31
申请号：US10545358
申请日：2004-02-20
申请人： Jerome Guillemont , Elisabeth Pasquier , Jan Heeres , Kurt Hertogs , Eva Bettens , Paulus Lewi , Marc De Jonge , Lucien Maria Koymans , Frederik Daeyaert , Hendrik Vinkers , Adriaan Janssen , Frank Zavier Jozef Arts
发明人： Jerome Guillemont , Elisabeth Pasquier , Jan Heeres , Kurt Hertogs , Eva Bettens , Paulus Lewi , Marc De Jonge , Lucien Maria Koymans , Frederik Daeyaert , Hendrik Vinkers , Adriaan Janssen , Frank Zavier Jozef Arts
IPC分类号： A61K31/53 , A61K31/506 , C07D405/14
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。
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公开(公告)号：US20060142571A1
公开(公告)日：2006-06-29
申请号：US10545719
申请日：2004-02-20
申请人： Jerome Guillemont , Elisabeth Therese Pasquier , Jan Heeres , Kurt Hertogs , Eva Bettens , Paulus Lewi , Marc De Jonge , Lucien Maria Koymans , Frederik Frans Daeyaert , Hendrik Vinkers , Frank Xavier Jozef Arts
发明人： Jerome Guillemont , Elisabeth Therese Pasquier , Jan Heeres , Kurt Hertogs , Eva Bettens , Paulus Lewi , Marc De Jonge , Lucien Maria Koymans , Frederik Frans Daeyaert , Hendrik Vinkers , Frank Xavier Jozef Arts
IPC分类号： C07D403/02
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，其作为药物的用途，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：US20050148581A1
公开(公告)日：2005-07-07
申请号：US11007026
申请日：2004-12-08
申请人： Jozef Van Gestel , Jerome Guillemont , Marc Venet , Herve Jean Poignet , Laurence Francoise Decrane , Daniel Vernier , Frank Odds
发明人： Jozef Van Gestel , Jerome Guillemont , Marc Venet , Herve Jean Poignet , Laurence Francoise Decrane , Daniel Vernier , Frank Odds
IPC分类号： A61K31/47 , A61K31/4706 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P31/06 , C07D215/22 , C07D215/227 , C07D215/36 , C07D215/48 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/02 , C07D417/02 , C07D471/04 , C07D521/00 , C07D43/02
CPC分类号： C07D215/227 , C07D215/36 , C07D215/48 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D471/04
摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. In particular, compounds are claimed in which, independently from each other, R1 is bromo, p=1, R2 is alkyloxy, R3 is optionally substituted naphthyl or phenyl, q=1, R4 and R5 each independently are hydrogen, methyl or ethyl, R6 is hydrogen, r is equal to 0 or 1 and R7 is hydrogen. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.
摘要翻译： 本发明涉及根据通式（Ia）或通式（Ib）的药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构形式和N-氧化物形式的新的取代喹啉衍生物 其中。 所要求保护的化合物可用于治疗分枝杆菌疾病，特别是由致病性分枝杆菌引起的疾病如结核分枝杆菌，牛分枝杆菌，鸟分枝杆菌和马氏海马。 特别地，要求保护的化合物，其中R 1彼此独立地是溴，p = 1，R 2是烷氧基，R 3 O >为任选取代的萘基或苯基，q = 1，R 4和R 5各自独立地为氢，甲基或乙基，R 6为 氢，r等于0或1，R 7是氢。 还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的要求保护的化合物的组合物，所要求保护的化合物或组合物在制备用于治疗分枝杆菌疾病的药物中的用途以及制备方法 要求保护的化合物。
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公开(公告)号：US5292897A
公开(公告)日：1994-03-08
申请号：US858406
申请日：1992-03-27
IPC分类号： C07D295/02 , B01J27/02 , B01J27/06 , B01J31/02 , C07B61/00 , C07C41/50 , C07C43/313 , C07C45/56 , C07C251/12 , C07C251/30 , C07D295/06 , C07D295/067 , C07D317/16 , C07F9/06 , C07F9/40 , C07F9/655
CPC分类号： C07D295/067 , C07C403/14 , C07C43/313 , C07C45/56 , C07D317/16 , C07F9/65515 , C07C2101/16
摘要： The present invention relates to a process for preparing halo acetals of ethylenic aldehydes by reaction of a halogen cation with enamine followed by a hydrolysis and reaction with an alcohol, a glycol or an orthoformate. These halo acetals are used as intermediate for the synthesis of vitamins A and E.It also relates to a new compound of formula (IV), ##STR1## to a process for preparing it from halo acetals of ethylenic aldehydes by reaction with triethyl phosphate, and to its use for the preparation of retinal by reaction with .beta.-ionylideneacetaldehyde.
摘要翻译： 本发明涉及通过卤素阳离子与烯胺的反应，然后与醇，二醇或原甲酸酯进行水解和反应来制备烯属醛的卤代缩醛的方法。 这些卤代乙醛用作合成维生素A和E的中间体。它还涉及一种新的式（IV）化合物，（*化学结构*）（Ⅳ），其由乙烯醛的卤代缩醛制备的方法 通过与磷酸三乙酯反应，以及其用于通过与（β） - 亚氨基乙醛反应来制备视网膜的用途。
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公开(公告)号：US5145972A
公开(公告)日：1992-09-08
申请号：US620610
申请日：1990-12-03
IPC分类号： C07D295/02 , B01J27/02 , B01J27/06 , B01J31/02 , C07B61/00 , C07C41/50 , C07C43/313 , C07C45/56 , C07C251/12 , C07C251/30 , C07D295/06 , C07D295/067 , C07D317/16 , C07F9/06 , C07F9/40 , C07F9/655
CPC分类号： C07D295/067 , C07C403/14 , C07C43/313 , C07C45/56 , C07D317/16 , C07F9/65515 , C07C2101/16
摘要： The present invention relates to a process for preparing halo acetals of ethylenic aldehydes by reaction of a halogen cation with enamine followed by a hydrolysis and reaction with an alcohol, a glycol or an orthoformate. These halo acetals are used as intermediate for the synthesis of vitamins A and E.It also relates to a new compound of formula (IV), ##STR1## to a process for preparing it from halo acetals of ethylenic aldehydes by reaction with triethyl phosphate, and to its use for the preparation of retinal by reaction with .beta.-ionylideneacetaldehyde.
摘要翻译： 本发明涉及通过卤素阳离子与烯胺的反应，然后与醇，二醇或原甲酸酯进行水解和反应来制备烯属醛的卤代缩醛的方法。 这些卤代乙醛用作合成维生素A和E的中间体。它还涉及一种新的式（IV）化合物，其作用是通过与乙烯醛的卤代缩醛反应制备该化合物， 磷酸三乙酯，以及其用于通过与β-亚硫酰基乙醛反应制备视网膜的用途。
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