- UREA DERIVATIVES AND USES THEREOF
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The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
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Paragraph 00582
(2015/01/09)
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- Exploring the unexplored practical and alternative synthesis of 3-(trifluoromethyl)-triazolopiperazine the key intermediate for Sitagliptin
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The practical synthesis of 3-(trifluoromethyl)-triazolopiperazine the key intermediate of Sitagliptin and 3-(trifluoromethyl)-triazolopyridine was carried out employing industrially feasible transformations. The other advantage of this method is the new environment friendly approach to synthesize triazolopiperazine and triazolopyridines by eliminating the commonly used trifluoroacetic anhydride and polyphosphoric acid.
- Nitlikar, Lakshmikant H.,Darandale, Sunil N.,Shinde, Devanand B.
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p. 348 - 352
(2013/07/26)
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- Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists
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Previously disclosed C6 amido and benzimidazole dihydropyrazolopyrimidines were potent and selective blockers of IKur current. Syntheses and SAR for C6 triazolo and imidazo dihydropyrazolopyrimidines series are described. Trifluoromethylcyclohexyl N(1) triazole, compound 51, was identified as a potent and selective Kv1.5 inhibitor with an acceptable PK and liability profile.
- Finlay, Heather J.,Jiang, Ji,Caringal, Yolanda,Kover, Alexander,Conder, Mary Lee,Xing, Dezhi,Levesque, Paul,Harper, Timothy,Hsueh, Mei Mann,Atwal, Karnail,Blanar, Michael,Wexler, Ruth,Lloyd, John
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supporting information
p. 1743 - 1747
(2013/04/10)
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- SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, A and B are as defined herein. The invention also r
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Page/Page column 52
(2012/09/22)
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- Synthesis and studies on the anticonvulsant activity of 5-alkoxy-[1,2,4]triazolo[4,3-a]pyridine derivatives
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In this study, a series of new 5-alkoxy-[1,2,4]triazolo[4,3-a]pyridine derivatives was synthesized and their anticonvulsant activity and neurotoxicity was evaluated with the maximal electroshock and rotarod tests, respectively. The most promising compounds, 3p (5-(4-chlorophenoxy)-[1,2,4]triazolo[4,3-a] pyridine) and 3r (5-(4-bromophenoxy)-[1,2,4]triazolo[4,3-a]pyridine), showed a median effective dose of 13.2 and 15.8 mg/kg and had a protective index value of 4.8 and 6.9, respectively. For exploring the putative mechanism of action, compounds 3n, 3p and 3r were tested in chemically induced models. Georg Thieme Verlag KG Stuttgart.New York.
- Guan,Zhang,Sun,Chang,Sui
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p. 372 - 377
(2012/10/29)
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- UV-vis, IR and 1H NMR spectroscopic studies of some 6-chloro,2-pyridyl hydrazones
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The electronic absorption spectra of some 6-chloro,2-pyridyl hydrazones are studied in seven organic solvents of different polarity. The absorption bands are assigned to the corresponding electronic transitions and the effect of solvent parameters on the charge transfer energy (ECT) is investigated. The spectra in buffer solutions of varied pH are also studied and utilized for the determination of the acid dissociation constants of the compounds under study. The fluorescence spectra were recorded for one of the studied compounds in six solvents, the solvent effect on the photoquantum yield and spectral pattern are also studied. Bands of diagnostic importance in the IR spectra and signals in the 1H NMR spectra are assigned. The results of the present investigation are supported by some MO calculations using the atom super position and electron delocalization molecular orbital theory (ASED-MO) and Gaussian 94 program. The geometry is optimized using the PM3 method.
- Issa, Raafat M.,Hassanein, Ahmed A.,El-Mehasseb, Ibrahim M.,El-Wadoud, Reham I. Abed.
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p. 206 - 214
(2007/10/03)
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- Synthesis of 1,3-diazepines and ring contraction to cyanopyrroles
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Several tetrazolo[1,5-a]pyridines/2-azidopyridines undergo photochemical nitrogen elimination and ring expansion to 1,3-diazacyclohepta-1,2,4, 6-tetraenes (7,10,13,16,19,22) as well as ring cleavage to cyanovinylketenimines (8,17,20b) in low temperature Ar matrices. 6,8-Dichlorotetrazolo[1,5-a]pyridine/2-azido-3,5-dichloropridine 6 undergoes ready exchange of the chlorine in position 8 (3) with ROH/RONa. 8-Chloro-6-trifluoromethylletrazolo[1,5-a]pyridine 15 undergoes solvolysis of the CF3 group to afford 8-chloro-6-methoxycarbonyltetrazolo[1,5-a]pyridine 18. Several tetrazolopyridines/2-azidopyridines afford 1H- or 5H-1,3-diazepines in good yields on photolysis in the presence of alcohols or amines (11,14,23,25). 5-Chlorotetrazolo[1,5-a]pyridines/2-azido-6-chloropyridines 21 and 38 undergo a rearrangement to 1H-and 3H-3-cyanopyrroles 27 and 45, respectively. The mechanism of this rearrangement was investigated by 15N-labelling and takes place via transient 1,3-diazepines. The structures of 6,8-dichloro-tetrazolo[1,5-a]pyridine 6T, 6-chloro-8-ethoxytetrazoIo[1,5-a]pyridine 9Tb, dipyrrolylmethane 28, and 2-isopropoxy-4-dimethylamino-5H-1,3-diazepine 25b were determined by X-ray crystallography. In the latter case, this represents the first reported X-ray crystal structure of a 5H-1,3-diazepine.
- Reisinger, Ales,Bernhardt, Paul V.,Wentrup, Curt
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p. 246 - 256
(2007/10/03)
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- Condensed pyrazole derivatives, process for producing the same and use thereof
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Novel pharmaceutical compositions for inhibiting Th2-selective immune response and pharmaceutical compositions for inhibiting cyclooxygenase comprising condensed pyrazole derivatives represented by the general formula (I): or salts thereof.
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- Substituted 2-acylpyridine-α-(N)-hetarlyhydrazones and medicaments containing the same
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Substituted 2-acylpyridine-α-(N)-hetarylhydrazones are described, which are suitable as active substances for the treatment of antimicrobial and in particular antimycobacterial diseases, as well as active substances for the treatment of malaria or malignant tumours. The compounds have a marked synergistic activity combined with inhibitors of folate synthase, dihydrofolic acid reductase, DNA-synthesis and RNA-synthesis.
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- Novel (1H-1,2,3-triazol-1-yl)pyridines
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Pyridine ring substituted (1H-1,2,3-triazol-1-yl)pyridines were prepared and found to have insecticidal utility. 2-Chloro-6-(1H-1,2,3-triazol-1-yl)pyridine, for example, was prepared from 2-azio-6-chloropyridine and methyl propiolate by sequential condensation, hydrolysis, and decarboxylation and found to control aster leafhoppers.
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- Heterocyclic substituted-amino-pyrazolines
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This invention relates to novel 3-amino-1-heteroaryl-2-pyrazolines and their C4 and C5 analogs, useful for meliorating the inflammation and/or the progressive joint deterioration characteristic of arthritic disease, preventing the onset of asthmatic symptoms and allergic diseases, or as analgesic, antibacterial or antifungal agents.
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- Novel 3-substituted amino-1-substituted heteroaryl-2-pyrazolines
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This disclosure describes novel 3-substituted amino-1-substituted heteroaryl-2-pyrazolines and their C4 and C5 analogs, effective as agents that ameliorate inflammation, analgesic agents, antibacterial agents and/or anti-fungal agents.
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- 2-Pyridylhydrazides
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2-Pyridylhydrazides useful as antiinflammatory agents.
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