136818-50-3Relevant academic research and scientific papers
ARYL-BIPYRIDINE AMINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS
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Paragraph 0535, (2019/07/13)
The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula (I): wherein A, X, Y, Z, Q, R1, R2, R3, R4, R5, and n are described herein.
HETEROCYCLIC COMPOUNDS AS PAD INHIBITORS
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Paragraph 000297, (2019/04/16)
Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis.
IMIDAZO-PYRIDINE COMPOUNDS AS PAD INHIBITORS
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Paragraph 000133; 000297, (2019/05/10)
Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis. The process of preparation of the compounds of Formula (I), (II), and (III), their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof, along with a pharmaceutical composition comprising a compound of Formula (I), Formula (II), Formula (III), or a pharmaceutically acceptable salt thereof have also been described.
Method for synthesizing intermediate 7-azaindole
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Paragraph 0022; 0031; 0037; 0040; 0049; 0058, (2018/03/24)
The invention discloses a method for synthesizing an intermediate 7-azaindole. The method comprises the following steps: mixing 2-amino-3-methylpyridine and ethanol, adding a catalyst, heating to 40-60 DEG C, adding oxalate into the mixture, uniformly mixing, carrying out reflux reaction for 1-2 hours, filtering, performing reduced pressure distillation on the filtrate, and recrystallizing to obtain 2-aminopyridine-3-pyruvate; adding the prepared 2-aminopyridine-3-pyruvate into DMF (Dimethyl Formamide), adding acetic acid to be uniformly stirred, adding Ce2O3, heating to 80 DEG C, stirring andcarrying out the reflux reaction for 2-3 hours, filtering, and performing reduced pressure distillation on the filtrate so as to obtain 7-azaindole-2-formic acid; mixing the prepared 7-azaindole-2-formic acid and methylbenzene, heating to 80-90 DEG C, adding ZnO, uniformly mixing, stirring and carrying out the reflux reaction for 2-3 hours, filtering, and performing reduced pressure distillationon the filtrate, thereby obtaining 7-azaindole. The synthetic method disclosed by the invention is simple to operate, mild in conditions, less in by-products, high in product purity and high in product yield.
Desulfonylation of indoles and 7-azaindoles using sodium tert-butoxide
Chaulet, Charlotte,Croix, Cécile,Basset, Joan,Pujol, Maria-Dolores,Viaud-Massuard, Marie-Claude
experimental part, p. 1481 - 1484 (2010/08/22)
A mild method for the desulfonylation of N-indoles and N-azaindoles is described. Deprotection is carried out under basic conditions, using sodium tert-butoxide in dioxane. Several functionalized indoles and 7-azaindoles were efficiently deprotected by this method, which is mild enough to be used to deprotect compounds including functions that are known to be sensitive to acidic or basic conditions.
PYRROLOPYRIDINE CARBOXYLIC ACID DERIVATIVES
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Page/Page column 86, (2010/04/03)
Disclosed are compounds and pharmaceutically acceptable salts of Formula (I) wherein R1, R2, R3, and RN are as defined herein. Compounds of Formula (I) are useful in the prevention and/or treatment of neurological and psychiatric disorder, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the disclosure and methods of treating the aforementioned conditions using such compounds.
PYRROLOPYRIDINE-2-CARBOXYLIC ACID AMIDE INHIBITORS OF GLYCOGEN PHOSHORYLASE
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Page 41, (2008/06/13)
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.
Aminopiperidine quinolines and their azaisosteric analogues with antibacterical activity
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, (2008/06/13)
Aminopiperidine derivatives of formula (I) and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
NITROGEN-CONTAINING BICYCLIC HETEROCYCLES FOR USE AS ANTIBACTERIALS
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Page/Page column 40, (2010/02/07)
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives hereof useful in methods of treatment of bacterial infections in mammals, particularly man.
Anti-aids piperazines
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, (2008/06/13)
The present invention includes diaromatic substituted heterocyclic compounds (III) STR1 which are useful in treating individuals infected with the HIV virus. The invention includes certain previously generically disclosed anti-AIDS piperazinyl compounds (V) and a method of treating HIV infected individuals with the indoles of formula (V) and the anti-AIDS amines (X).
