78686-77-8

Usage

Uses

Methyl 5-Bromo-6-chloronicotinate can be used to treat diseases related to S1PR1.

InChI:InChI=1/C7H5BrClNO2/c1-12-7(11)4-2-5(8)6(9)10-3-4/h2-3H,1H3

Upstream product

• 67-56-1 methanol 
• 5006-66-6 6-hydroxynicotinic acid 
• 5006-66-6 6-hydroxy-3-pyridinecarboxylic acid 
• 66171-50-4 methyl 6-hydroxynicotinate 
• 365413-29-2 6-chloro-5-iodonicotinic acid methyl ester 
• 41668-13-7 5-bromo-6-hydroxy-3-pyridinecarboxylic acid 
• 29241-62-1 5-bromo-6-chloronicotinic acid 
• 74-88-4 methyl iodide 
• 381247-99-0 methyl 5-bromo-6-hydroxypyridine-3-carboxylate 
• 17282-03-0 3-bromo-2-chloro-5-methyl-pyridine 
• 381247-99-0 methyl 5-bromo-6-oxo-1,6-dihydropyridine-3-carboxylate 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 73781-91-6 6-Chloronicotinic acid methyl ester 
• 78686-84-7 3-bromo-2-chloro-5-pyridinecarbonyl chloride 

Downstream Products

• 93349-99-6 methyl 5-bromo-6-methoxy-pyridine-3-carboxylate 
• 93350-00-6 Methyl 5-Bromo-6-(phenylthio)nicotinate 
• 1143564-20-8 6-benzylamino-5-bromo-nicotinic acid 
• 912454-34-3 5-bromo-6-(2-methoxyethoxy)-3-pyridinecarboxylic acid 
• 1244016-90-7 methyl 5-bromo-6-(methylamino)pyridine-3-carboxylate 
• 1012792-56-1 6-chloro-5-(4-chlorophenyl)-3-pyridinecarboxylic acid 
• 1018782-81-4 6-chloro-5-(4-fluorophenyl)-3-pyridinecarboxylic acid 
• 1018782-76-7 5-(4-chlorophenyl)-6-(cyclopropylmethoxy)-3-pyridinecarboxylic acid 
• 1018782-82-5 5-(4-chlorophenyl)-6-(2,2,2-trifluoroethoxy)-3-pyridinecarboxylic acid 
• 1012792-57-2 6-chloro-5-(4-chlorophenyl)-N-[(1R,2R)-2-hydroxycyclohexyl]-3-pyridine carboxamide 
• 1018782-80-3 6-chloro-5-(4-fluorophenyl)-3-pyridinecarboxylic acid methyl ester 

Relevant academic research and scientific papers

Iron-Catalyzed Amination of Strong Aliphatic C(sp3)-H Bonds

A concept for intramolecular denitrogenative C(sp3)-H amination of 1,2,3,4-tetrazoles bearing unactivated primary, secondary, and tertiary C-H bonds is discovered. This catalytic amination follows an unprecedented metalloradical activation mechanism. The utility of the method is showcased with the short synthesis of a bioactive molecule. Moreover, an initial effort has been embarked on for the enantioselective C(sp3)-H amination through the catalyst design. Collectively, this study underlines the development of C(sp3)-H bond functionalization chemistry that should find wide application in the context of drug discovery and natural product synthesis.

OXADIAZOLE MODULATORS OF S1P METHODS OF MAKING AND USING

The invention is directed to Compounds of Formula (I): wherein each variable is defined herein, as well as methods of making and using the compounds as agonists of S1P1 and/or S1P5 for instance for treating graft versus host disease and autoimmune diseases.

BICYCLIC HYDROXAMIC ACIDS USEFUL AS INHIBITORS OF MAMMALIAN HISTONE DEACETYLASE ACTIVITY

A compound of formula (Ia) or (Ib) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of a histone deacetylase, and as such is useful in terepy, e.g. in the treatment of autoimmune disorders, mental disorders, neurodegenerative disorders, and hyperproliferative disorders.

PYRAZOLYL-SUBSTITUTED PYRIDONE COMPOUNDS AS SERINE PROTEASE INHIBITORS

There are provided inter alia pyrazolyl-substituted pyridone compounds, which exhibit biological activity, e.g., inhibitory action, against serine proteases, including thrombin and various kallikreins. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of serine proteases, including thrombin and various kallikreins.

Design, Synthesis, and Evaluation of Novel Auxin Mimic Herbicides

Due to the key roles of auxins as master regulators of plant growth, there is considerable interest in the development of compounds with auxin-like properties for growth management and weed control applications. Herein, we describe the design and multiste

Design and structural analysis of aromatic inhibitors of type II dehydroquinase from mycobacterium tuberculosis

3-Dehydroquinase, the third enzyme in the shikimate pathway, is a potential target for drugs against tuberculosis. Whilst a number of potent inhibitors of the Mycobacterium tuberculosis enzyme based on a 3-dehydroquinate core have been identified, they generally show little or no in vivo activity, and were synthetically complex to prepare. This report describes studies to develop tractable and drug-like aromatic analogues of the most potent inhibitors. A range of carbon-carbon linked biaryl analogues were prepared to investigate the effect of hydrogen bond acceptor and donor patterns on inhibition. These exhibited inhibitory activity in the high-micromolar range. The addition of flexible linkers in the compounds led to the identification of more potent 3-nitrobenzylgallate- and 5-aminoiso-phthalate-based analogues.

Development of a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl)nicotinate: Trifluoromethylation on kilogram scale

Reported herein is a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl)nicotinate, an intermediate in the synthesis of novel anti-infective agents. The key to this process is the trifluoromethylation of an aryl iodide using an inexpensive methyl chlorodifluoroacetate (MCDFA)/KF/CuI system, with an emphasis on the development work which led to this effective process.

6-alkoxy-5-aryl-3-pyridinecarboxamides, a new series of bioavailable cannabinoid receptor type 1 (CB1) antagonists including peripherally selective compounds

We identified 6-alkoxy-5-aryl-3-pyridinecarboxamides as potent CB1 receptor antagonists with high selectivity over CB2 receptors. The series was optimized to reduce lipophilicity compared to rimonabant to achieve peripherally active molecules with minimal central effects. Several compounds that showed high plasma exposures in rats were evaluated in vivo to probe the contribution of central vs peripheral CB1 agonism to metabolic improvement. Both rimonabant and 14g, a potent brain penetrant CB1 receptor antagonist, significantly reduced the rate of body weight gain. However, 14h, a molecule with markedly reduced brain exposure, had no significant effect on body weight. PK studies confirmed similarly high exposure of both 14h and 14g in the periphery but 10-fold lower exposure in the brain for 14h. On the basis of these data, which are consistent with reported effects in tissue-specific CB1 receptor KO mice, we conclude that the metabolic benefits of CB1 receptor antagonists are primarily centrally mediated as originally believed.

HYDROXAMIC ACID DERIVATIVES AS GRAM-NEGATIVE ANTIBACTERIAL AGENTS

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3-Pyridinecarboxamide derivatives as HDL-cholesterol raising agents

The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.