- 6-Benzylamino 4-oxo-1,4-dihydro-1,8-naphthyridines and 4-oxo-1,4- dihydroquinolines as HIV integrase inhibitors
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SAR studies on the quinolone carboxylic acid class of HIV-1 integrase inhibitors focused on improving the metabolic stability and led to the discovery of 27 and 38.
- Nagasawa, Johnny Y.,Song, Jenny,Chen, Huanming,Kim, Hong-Woo,Blazel, Julie,Ouk, Samedy,Groschel, Bettina,Borges, Virginia,Ong, Voon,Yeh, Li-Tain,Girardet, Jean-Luc,Vernier, Jean-Michel,Raney, Anneke K.,Pinkerton, Anthony B.
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scheme or table
p. 760 - 763
(2011/03/18)
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- Synthesis of pyridodiazepinediones by using the ugi multicomponent reaction
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Benzodiazepines show a broad spectrum of biological activities. In an ongoing effort to extend molecular diversity in this type of systems, we developed a strategy for synthesizing 3,4-dihydro-1H-pyrido[2,3-e][1,4] diazepine-2,5-dione compounds starting from 2-hydroxynicotinic acid and by using an Ugi reaction as a key step in the synthesis. We opted to use 2isocyanophenyl benzoate instead of Armstrong's convertible isocyanide in this multicomponent reaction.
- Van Den Bogaert, An M.,Nelissen, Jo,Ovaere, Margriet,Van Meervelt, Luc,Compernolle, Frans,De Borggraeve, Wim M.
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scheme or table
p. 5397 - 5401
(2010/11/18)
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- HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF
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Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
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Page/Page column 113
(2010/12/26)
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- Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors
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A series of novel tetrahydronaphthyridine-based histamine H3 ligands that have serotonin reuptake transporter inhibitor activity is described. The 1,2,3,4-tetrahydro-2,6-naphthyridine scaffold is assembled via the addition of a nitrostyrene to a metalated pyridine followed by reduction and cyclization to form the naphthyridine. In vitro biological data for these novel compounds are discussed.
- Letavic, Michael A.,Keith, John M.,Ly, Kiev S.,Barbier, Ann J.,Boggs, Jamin D.,Wilson, Sandy J.,Lord, Brian,Lovenberg, Timothy W.,Carruthers, Nicholas I.
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p. 2566 - 2569
(2008/02/01)
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- NAPHTHYRIDINE COMPOUNDS
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Certain naphthyridine compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.
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Page/Page column 26
(2010/11/25)
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- Substituted alkylamine derivatives and methods of use
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Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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- Substituted alkylamine derivatives and methods of use
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Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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- HALOGENATION OF 2-HYDROXYNICOTINIC ACID
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A convenient method to prepare 5-halo-2-hydroxynicotinic acid is described.
- Gero, Thomas W.,Jaques, Larry W.,Mays, Richard P.,Reid, Debra H.,Shamblee, Dwight A.,et al.
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p. 553 - 560
(2007/10/02)
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- Benzo- and pyrido-1,4-oxazepin-5-ones and -thiones: Synthesis and structure-activity relationships of a new series of H1 antihistamines
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A series of novel benzo- and pyrido-1,4-oxazepinones and -thiones which represents a new structural class of compounds possessing H1 antihistaminic acitivy was synthesized, and the SARs were evaluated. The antihistamine activity was determined by blockade of histamine-induced lethality in guinea pigs. The sedative potential was determined by comparison of the EEG profiles of the compounds with those of known sedating and nonsedating antihistamines. Several of the compounds were shown to possess potent H1 antihistaminic activity and to be free of the cortical slowing with synchronized waves and spindling activity found in the EEG of sedative antihistamines. One compound, 2-[2-(dimethylamino)ethyl]-3,4-dihydro-4-methylpyrido[3,2-f]-1,4-oxazeN pine-5(2H)-thione (rocastine) is currently undergoing clinical evaluation as a nonsedating H1 antihistamine.
- Cale Jr.,Gero,Walker,Lo,Welstead Jr.,Jaques,Johnson,Leonard,Nolan,Johnson
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p. 2178 - 2199
(2007/10/02)
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- Fused aromatic oxazepinones, thiazepinones, diazepinones and sulfur analogs thereof
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Aromatic azepinones and thiones having the formula STR1 wherein; A is benzene, naphthalene, quinoline or pyridine; B is oxygen or sulfur; E is oxygen, sulfur or STR2 n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen-containing radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; Y is halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracetylamino, trifluoromethyl, phenyl or phenyl substituted by one to three Y' radicals selected from halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracylamino or trifluoromethyl; and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.
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- Fused aromatic oxazepinones, thiazepinones, diazepinones and sulfur analogs thereof
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Aromatic azepinones and thiones having the formula STR1 wherein; A is benzene, naphthalene, quinoline or pyridine; B is oxygen or sulfur; E is oxygen, sulfur or STR2 n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen containing radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.
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