- Methods for treating neisseria gonorrhoeae infection with substituted 1,2-dihydro-2A,5,8A-triazaacenaphthylene-3,8-diones
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The present invention relates to methods for treating Neisseria Gonorrhoeae infection which comprises administering to a subject in need thereof novel 1,2-dihydro-2a,5,8a-triazaacenaphthylene-3,8-dione compounds: or pharmaceutically acceptable salts thereof and/or corresponding pharmaceutical compositions.
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Page/Page column 72
(2020/07/21)
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- Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3- b ]pyrazine-2,3-dione as a novel potent d -amino acid oxidase inhibitor
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A series of 5-azaquinoxaline-2,3-dione derivatives were synthesized and evaluated on d-amino acid oxidase (DAAO) inhibition as potential α-hydroxylactam-based inhibitors. The potent inhibitory activities in vitro suggested that 5-nitrogen could significantly enhance the binding affinity by strengthening relevant hydrogen bond interactions. The analgesic effects of intrathecal and systemic injection of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione, a representative molecule of 5-azaquinoxaline-2,3-dione, were investigated in rodents. This research not only confirmed the analgesic effect of the DAAO inhibitors but provided a new class of chemical entities with oral application potential for the treatment of chronic pain and morphine analgesic tolerance.
- Xie, Dongsheng,Lu, Jun,Xie, Jin,Cui, Junjun,Li, Teng-Fei,Wang, Yan-Chao,Chen, Yuan,Gong, Nian,Li, Xin-Yan,Fu, Lei,Wang, Yong-Xiang
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- INHIBITORS OF DNA GYRASE FOR THE TREATMENT OF BACTERIAL INFECTIONS
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The present invention relates to compounds which specifically inhibit bacterial DNA Gyrase and can be used for the treatment of respiratory tract infections.
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Page/Page column 47
(2014/05/07)
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- Diversified synthesis of novel quinoline and dibenzo thiazepine derivatives using known active intermediates
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The novel drug development to control resisting infections in conventional drug therapy is a need of today. Few antiulcer relative derivatives developed by approaching convergent synthesis. The derivatives synthesized successfully are dibenzo thiazepine-pyridine (SLN11-SLN15) and benzimidazole-hydroquinoline based derivatives (SLN16-SLN20). It involved the coupling through microwave, sonication and conventional techniques at final step. The efficient technology identified as sonication technique basically time and yield. The reported compounds were structural characterized by elemental analysis and spectral studies such as 1H, 13C NMR and MS.
- Sharada,Satyanarayana Reddy,Sammaiah,Sumalatha
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p. 7959 - 7966
(2013/09/23)
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- TRICYCLIC NITROGEN COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS
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Tricyclic nitrogen containing compounds and their use as antibacterials.
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Page/Page column 47-48
(2009/09/04)
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- COMPOUNDS
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Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof: (relative chemistry shown) pharmaceutical compositions comprising them, their use in therapy especially against tuberculosis, and methods of preparing them are described.
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Page/Page column 21
(2009/12/24)
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- COMPOUNDS
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Bicyclic nitrogen containing compounds and their use as antibacterials.
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Page/Page column 24; 85
(2008/12/08)
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- TRICYCLIC NITROGEN CONTAINING COMPOUNDS AS ANTIBACTERIAL AGENTS
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Tricyclic nitrogen containing compounds and their use as antibacterials. Z1and Z2 are independently selected from CH and N.
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Page/Page column 55-56
(2008/12/08)
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- Methods for Chk2 inhibitor patient selection
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The present invention contemplates a method to identify subjects that either have a tumor, or are at risk for tumor development, that are responsive to various inhibitors of an activated-Chk2 protein. Such Chk2 inhibitors may comprise a benzimidazole core structure, and derivatives thereof. Other Chk2 inhibitors may comprise nucleic acids, such as silencing interference RNA's specific for a Chk2 expression. Other Chk2 inhibitors may comprises proteins, such as antibodies. For example, the present invention contemplates that when a Chk2 inhibitor is administered during, or after, ionizing radiation tumor cell apoptosis is increased.
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Page/Page column 18
(2008/12/05)
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- Novel non-benzimidazole chk2 kinase inhibitors
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In a recent paper, [Arienti, K. L.; Brunmark, A.; Axe, F. U.; McClure, K. M.; Lee, A.; Blevitt, J.; Neff, D. K.; Huang, L.; Crawford, S.; Chennagiri, R. P.; Karlsson, L.; Brietenbucher, J. G. J. Med. Chem. 2005, 48, 1873], we described the discovery of a class of benzimidazole chk2 kinase inhibitors, exemplified by compound 1, which had radio-protective effects in human T-cells subjected to ionizing radiation. Here, a series of non-benzimidazole analogs intended to define the scope of the SAR about this new series of inhibitor, and allow for refinement of the binding model of these compounds to the chk2 kinase is described.
- McClure, Kelly J.,Huang, Liming,Arienti, Kristen L.,Axe, Frank U.,Brunmark, Anders,Blevitt, Jon,Guy Breitenbucher
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p. 1924 - 1928
(2007/10/03)
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- Process for producing 2,3-diamino-6-methoxypyridine
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The present invention relates to a novel process for producing 2,3-diamino-6-methxoypyridine. The process comprises neutralizing 2,3-diamino-6-methoxy pyridine dihydrochloride, which, in turn, is prepared by the reduction of 2-amino-6-methoxy-3-nitropyridine. The 2-amino-6-methoxy-3-nitropyridine is further prepared by methoxylation of 2-amino-6-chloro-3-nitropyridine by sodium methoxide in methanol.
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Page/Page column 3
(2008/06/13)
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- IMIDAZOPYRIDINE COMPOUND
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A compound represented by the following general formula (1), or a salt or hydrate thereof: wherein R1 represents a C1-C6 alkyl group or C2-C6 alkynyl group which may be substituted, or a phenyl group which may be substituted, R2 represents a hydrogen atom or a C1-C6 alkyl group, R3 represents methyl or ethyl group, R4 represents a C1-C6 alkyl group, R5 represents a hydrogen atom, provided that a compound wherein R1 is a C1-C6 alkyl group unsubstituted or substituted with a halogen atom and R2 is a hydrogen atom is excluded.
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Page/Page column 102-103
(2010/02/14)
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- CGRP RECEPTOR ANTAGONISTS
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The present invention is directed to compounds of Formula (I) and Formula (II) (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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- Substituted benzimidazoles and imidazo-[4,5]-pyridines
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2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.
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- Zinc-promoted direct amination of nitropyridines with methoxyamine via vicarious nucleophilic substitution
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Direct animation of nitropyridines with methoxyamine in the presence of a stoichiometric amount of zinc(II) chloride under basic conditions proceeds to give aminonitropyridines.
- Seko, Shinzo,Miyake, Kunihito
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p. 1519 - 1520
(2007/10/03)
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- Nitroarylamines via the Vicarious Nucleophilic Substitution of Hydrogen: Amination, Alkylamination, and Arylamination of Nitroarenes with Sulfenamides
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A new reaction of sulfenamides with electrophilic arenes under basic conditions is described. The σ adducts formed from nitroarenes and the anions of sulfenamides undergo elimination of thiol to produce the corresponding o- and/or p-nitroanilines. This reaction is analogous to the known alkylation and hydroxylation of nitroarenes via the vicarious nucleophilic substitution of hydrogen (VNS). The reaction gives access to a wide range of substituted nitroanilines, nitronaphthylamines, and aminoheterocycles. By means of the reaction with N-alkyl- and N-arylsulfenamides, it is possible to obtain N-alkylnitroanilines and nitrodiarylamines. By varying the structure of sulfenamide and the reaction conditions, particularly the nature and concentration of the base, it is possible to control the orientation of animation.
- Makosza, Mieczyslaw,Bialecki, Maciej
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p. 4878 - 4888
(2007/10/03)
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- Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines
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In continuation of our previous work on piperazinopyrrolothienopyrazine derivatives, three series of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines were prepared and evaluated as 5-HT3 receptor ligands. The chemical modifications performed within these new series led to structure-activity relationships regarding both high affinity and selectivity for the 5-HT3 receptors that are in agreement with those established previously for the pyrrolothienopyrazine series. The best compound (8a) obtained in these new series is in the picomolar range of affinity for 5-HT3 receptors with a selectivity higher than 106. Four of the high-affinity 5-HT3 ligands (8a, 15a,b, and 16d) were selected in both the pyridopyrrolopyrazine and the pyrroloquinoxaline series and were characterized in vitro and in vivo as agonists or partial agonists. Compound 8a was also evaluated in the light/dark test where it showed potential anxiolytic-like activity at very low doses per os.
- Prunier, Hervé,Rault, Sylvain,Lancelot, Jean-Charles,Robba, Max,Renard, Pierre,Delagrange, Philippe,Pfeiffer, Bruno,Caignard, Daniel-Henri,Misslin, René,Guardiola-Lemaitre, Béatrice,Hamon, Michel
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p. 1808 - 1819
(2007/10/03)
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- Process for producing aminonitropyridines
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A process for producing an aminonitropyridine represented by the general formula [1], which comprises reacting a nitropyridine represented by the general formula [2] (wherein X1, X2 and X3 indicate a hydrogen atom, a halogen atom, a nitro group, a cyano group, an aryl group, an aromatic heterocycle or an alkyl group, etc.; Y is an oxygen atom; and n is 0 or 1) with an O-substituted hydroxylamine represented by the general formula [3] (wherein R4 is a hydrogen atom, an alkyl group, a cycloalkyl group or an aralkyl group; and R5 is an alkyl group or an aralkyl group) or a salt thereof in the presence of a base and a metal catalyst. STR1
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- Tricyclic pyrrolopyrazine 5-HT3 -active compounds
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The present invention relates to a compound selected from these of formula (I): STR1 in which A and R1 are as defined in the description, and medicinal product containing the same which is useful for treating a disorder linked to the 5-HT3 receptors.
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- Novel α-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonists: Synthesis and structure-activity relationships of 6-(1H- imidazol-1-yl)-7-nitro-2,3(1H,4H)-pyrido[2,3-b]pyrazinedione and related compounds
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We have synthesized and evaluated azaquinoxalinediones 3a-c for their activity in inhibiting [3H]AMPA binding from rat whole brain. It was found that the azaquinoxalinedione nucleus functions as a bioisostere for quinoxalinedione in AMPA receptor binding. The detailed structure-activity relationships of 6- and/or 7-substituted 2,3(1H,4H)-pyrido[2,3- b]pyrazinedione derivatives 4, 7-10, 13, 15, and 16 showed some differences in comparison with those of the corresponding substituted quinoxalinediones, including 6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione (1) (YM90K). The X-ray study exhibited that conformation of the 7-nitro group of 1 · HCl was nearly coplanar with the quinoxaline ring, whereas the 6- imidazol1-yl group was rotated with respect to the aromatic ring. From the glycine site on NMDA receptor binding study, it is indicated that bulkiness of 6-substituents on pyridopyrazinediones may be responsible for the selectivity against the glycine site. Among the series of azaquinoxalinediones, 6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-pyrido[2,3- b]pyrazinedione (8c) exhibited a combination of the best affinity to the AMPA receptors with a K(i) value of 0.14 μM and selectivity against the glycine site (no affinity at 10 μM). In vivo, 8c also protected against sound- induced seizure in DBA/2 mice (minimum effective dose, 10 mg/kg ip).
- Ohmori,Kubota,Shimizu-Sasamata,Okada,Sakamoto
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p. 1331 - 1338
(2007/10/03)
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- Regioselectivity of the Amination of Some 3-Nitropyridines by Liquid Ammonia / Potassium Permanganate
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3-Nitropyridine and some of its derivatives are aminated in a liquid ammonia solution of potassium permanganate to the corresponding 2- and (or) 4- and (or) 6-amino compounds.Quantumchemical calculations for a few 3-nitropyridines suggest that the experimentally observed regioselectivity of the amination is controlled by Coulombic interaction. --- Key Words: Amination / Nitropyridines / Reactivity indices / Calculations, MNDO
- Wozniak, Marian,Baranski, Andrzej,Szpakiewicz, Barbara
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p. 875 - 878
(2007/10/02)
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- Substituent Effects on the Isomer Ratios in the Rearrangement of Some 2- and 4-Nitraminopyridines
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The preparation, and rearrangement in 92percent sulfuric acid, of 4-X-2-nitramino- (1), 2-X-4-nitramino- (2), and 6-X-2-nitramino-pyridines (3) is reported (X=H,Me,MeO,Br,Cl,CO2H).The product isomer ratios can be explained by differential electronic stabilization of the appropriate ? complexes for aromatic nitration and steric effects seem relatively unimportant.Deuteration had no effect on the product distribution
- Deady, Leslie W.,Korytsky, Olga L.,Rowe, Jeffrey E.
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p. 2025 - 2034
(2007/10/02)
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