- 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 137
(2020/07/21)
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- THYROID HORMONE RECEPTOR AGONISTS AND USES THEREOF
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Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with thyroid hormone receptor activity. The methods and compositions disclosed herein include the use of at least one thyroid hormone receptor agonist.
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Paragraph 00333; 00382
(2020/01/08)
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- A general approach to access 5,6-dihydroindolo-naphthyridine ring system
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We report a general approach for the synthesis of 5,6-dihydroindolo-naphthyridine ring system via an intramolecular cyclization of the indole NH to an alkene moiety as the key step.
- He, Shuwen,Li, Peng,Dai, Xing,Liu, Hong,Lai, Zhong,Xiao, Dong,McComas, Casey C.,Du, Chunyan,Liu, Yuehui,Yin, Jingjun,Dang, Qun,Zorn, Nicolas,Peng, Xuanjia,Nargund, Ravi P.,Palani, Anandan
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supporting information
p. 1373 - 1375
(2017/03/17)
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- Synthesis of new derivatives of 10H-benzo[b]pyridazino[3,4-e][1,4]thiazines
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New 10H-benzo[b]pyridazino[3,4-e][1,4]thiazines were prepared and evaluated for inhibitory activity against soybean 15-lipoxygenase enzyme. These compounds were synthesized by the sequential treatment of 4-bromo-3,6-dichloropyridazine with 2-aminothiophenol and a secondary amine with the subsequent heterocyclization in the presence of sodium amide.
- Arghiani, Zahra,Seyedi, Seyed Mohammad,Bakavoli, Mehdi,Nikpour, Mohsen
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p. 215 - 218
(2015/08/24)
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- Access to 4-alkylaminopyridazine derivatives via nitrogen-assisted regioselective pd-catalyzed reactions
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3-Substituted, 6-substituted, and unsymmetrical 3,6-disubstituted 4-alkylaminopyridazines were prepared from a sequence of three chemo- and regioselective reactions combining amination and palladium-catalyzed cross-coupling reactions, such as reductive dehalogenation and Suzuki-Miyaura reactions. Extension of the methodology to Sonogashira reaction yielded a novel class of 3-substituted pyrrolopyridazines.
- Blaise, Emilie,Kümmerle, Arthur E.,Hammoud, Hassan,De Arajo-Jnior, Jo Xavier,Bihel, Frdric,Bourguignon, Jean-Jacques,Schmitt, Martine
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p. 10311 - 10322
(2015/02/19)
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- MAP KINASE MODULATORS AND USES THEREOF
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The invention provides for novel MAP kinase inhibitors and compositions comprising the same. In some embodiments, the MAP kinase inhibitors are p38a MAP kinase inhibitors. The invention further provides for methods for treatment of diseases comprising adm
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Paragraph 00207; 00290
(2014/09/29)
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- TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C
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The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Page/Page column 90
(2014/08/20)
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- TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Page/Page column 90
(2014/08/20)
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- COMPOUNDS
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Tricyclic nitrogen containing compounds and their use as antibacterials.
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Page/Page column 16-17
(2010/04/23)
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- AZATRICYCLIC COMPOUNDS AND THEIR USE
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Tricyclic nitrogen containing compounds),of formula (I) or a pharmaceutically, acceptable salt, solvate and/or N-oxide thereof: and their use as antibacterials.
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Page/Page column 34
(2008/06/13)
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- SUBSTITUTED 1-METHYL-1H-QUINOLIN-2-ONES AND 1-METHYL-1H-1,5-NAPHTHYRIDIN-2-ONES AS ANTIBACTERIALS
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Bicyclic nitrogen containing compounds of formula (I) and their use as antibacterials.
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Page/Page column 53
(2008/06/13)
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- Compounds
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Tricyclic nitrogen containing compounds and their use as antibacterials
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Page/Page column 18
(2008/12/08)
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- DERIVATIVES AND ANALOGS OF N-ETHYLQUINOLONES AND N-ETHYLAZAQUINOLONES
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Bicyclic nitrogen containing compounds and their use as antibacterials.
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Page/Page column 38
(2008/06/13)
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- TRICYCLIC NITROGEN CONTAINING HETEROCYCLES AS ANTIBACTERIAL AGENTS
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Tricyclic nitrogen containing compounds and their use as antibacterials.
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Page/Page column 31-32
(2008/12/08)
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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 54
(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 123
(2008/12/08)
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- Pyrrolo[3,2,1-ij]quinoline-4-one derivatives for treating tuberculosis
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Tricyclic nitrogen-containing compounds of Formula (I) and pharmaceutically acceptable derivatives thereof: compositions containing them, their use in the treatment of tuberculosis, and methods for the preparation of such compounds.
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- HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIALS
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Tricyclic nitrogen containing compounds of formula (I) and their use as antibacterials .
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Page/Page column 72
(2008/06/13)
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- PYRROLO-QUINOXALINONE DERIVATIVES AS ANTIBACTERIALS
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Tricyclic nitrogen containing compounds of the following Formula (I) and their use as antibacterials.
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Page/Page column 30
(2008/06/13)
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- 9-Amino-podophyllotoxin derivatives, method for the production thereof and pharmaceutical compositions containing said derivatives
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The invention relates to compounds of formula (I), wherein R1 is a group selected from hydrogen, alkyl, aryl, aryalkil, heteroaryl, heteroarylalkyl, alkylcarbonyl, arylcarbonyl, arylalkylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, heterocycloalkoxycarbonyl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl, phosphonic and Si(Ra)2Rb, Y is a group selected from HN—NH and N—R2, R3 is a hydrogen atom, an alkyl, cycloalkyl, aryl, arylalkyl group, R4 is hydrogen atom or an alkyl group, enantiomers, diastereoisomers and the salts thereof.
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Page/Page column 6
(2008/06/13)
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- Triazolo-pyridazine derivatives as ligands for GABA receptors
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1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, an optionally substituted N-linked nitrogen-containing aliphat
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- Triazolo-pyridazine derivatives as ligands for GABA receptors
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1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-alkoxy moiety at the 6-position, are selective ligands for GABAAreceptors, in particular having high affinity for the α2
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- Triazolo-pyridazine derivatives as ligands for GABA receptors
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1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by wherein Z represents cyclobutyl or pyrrolidin-1-yl, are selective ligands for GABAAreceptors, in particular having high affinity for the α2 and/or α3 subunit thereof, are useful in the
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- Triazolo-pyridazine derivatives as ligands for GABA receptors
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1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by wherein Z represents an optionally substituted tetrahydropyridinyl substituent, are selective ligands for GABAAreceptors, in particular having high affinity for the α2 and/or α3 subuni
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- Substituted triazolo-pyridazine derivatives as ligands for GABA receptors
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Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the α2 and/or α3 subunits.
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- Triazolo-pyridazine derivatives as ligands for GABA receptors
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1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by wherein Z represents cyclobutyl, 1-methylcyclopentyl or pyrrolidin-1-yl, are selective ligands for GABAAreceptors, in particular having high affinity for the α2 and/or α3 subunit there
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- Synthesis of 2',3'-dideoxy- and 3'-azido-2',3'-dideoxy-pyridazine nucleosides as potential antiviral agents
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The synthesis of 4-methoxy-, 4-amino-3-chloro-, and 4-amino-1-(2,3- dideoxy-β-D-glycero-pentofuranosyl)pyridazin-6-one nucleosides, 6, 19 and 20 is described. The synthesis of 3,4-dichloropyridazin-6-one (10) was accomplished in 44% overall yield using bromomaleic anhydride (17) as the starting material. The condensation of the silylated base of 10 with the halogenose 12 in the presence of trimethylsilyl triflate as a catalyst afforded a mixture of 3,4-dichloro-1-(3,5-di-O-p-toluoyl-2-deoxy-β-D- erythro-pentofuranosyl)pyridazin-6-one (13) in 67% and its α-anomer 14 in 12% yield, respectively. A series of 3'-sulfonate esters were prepared to explore the synthesis of 3-chloro-4-hydroxy-1-(3-azido-2,3-dideoxy-β-D- erythro-pentofuranosyl)pyridazin-6-one (32) via 6,3-anhydronucleoside analogues. Compounds 15, 19 and 20 were evaluated against human immunodeficiency virus, human cytomegalovirus, and herpes simplex virus type 1 but were inactive.
- Kasnar,Wise,Kucera,Drach,Townsend
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p. 459 - 479
(2007/10/02)
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