183608-47-1

Usage

Uses

Used in Pharmaceutical Industry:
5-BROMO-N-METHOXY-N-METHYLNICOTINAMIDE is used as a reagent for the preparation and discovery of potent, selective, and peripherally restricted pan-Trk inhibitors, such as PF-06273340. These inhibitors are essential in the treatment of pain, as they help to alleviate discomfort and improve the quality of life for patients suffering from various painful conditions.

Upstream product

• 39620-02-5 5-bromonicotinoyl chloride 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 20826-04-4 5-bromo-3-pyridinecarboxylic acid 
• 1117-97-1 N,0-dimethylhydroxylamine 

Downstream Products

• 113118-81-3 5-bromopyridine-3-carbaldehyde 
• 329942-49-6 (5-bromo-3-pyridinyl)(5-chloro-2-hydroxyphenyl)methanone 
• 38940-62-4 3-acetyl-5-bromopyridine 
• 886374-05-6 (rac)-1-(5-bromo-pyridin-3-yl)-ethylamine 
• 1402445-23-1 (5-aminopyridin-3-yl){7-(2-{[tert-butyl(dimethyl)silyl]oxy}-1,1-dimethylethyl)-2-[(2,4-dimethoxybenzyl)amino]-7H-pyrrolo[2,3-d]pyrimidin-5-yl}methanone 
• 1402438-74-7 PF-06273340 
• 917772-69-1 3-bromo-5-(prop-1-yn-1-yl)pyridine 
• 1379615-30-1 7-methoxy-3-methyl-2-(5-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)quinolin-4(1H)-one 
• 1379615-51-6 1-(5-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)-propan-1-one 
• 908864-98-2 1-(5-bromopyridin-3-yl)-N,N-dimethylmethanamine 
• 59105-50-9 (5-bromopyridin-3-yl)(phenyl)methanone 
• 229008-14-4 N-methyl-N-methoxy-5-(4-methylphenyl)pyridine-3-carboxamide 
• 329946-06-7 5-[(5-chloro-2-hydroxyphenyl)carbonyl]-3-pyridinecarbonitrile 

Relevant academic research and scientific papers

SOLID FORMS OF 1-(5-(3-(7-(3-FLUOROPHENYL)-3H-IMIDAZO[4,5-C]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-B]PYRIDIN-5-YL)PYRIDIN-3-YL)-N,N-DIMETHYLMETHANAMINE

The present application relates to two crystalline polymorphic forms, crystalline methanol, ethanol and tetrahydrofuran solvates and a crystalline hydrate of the compound l-(5-(3-(7-(3-fluorophenyl)-3H- imidazo[4,5-c]pyridin-2-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3- yl)-N,N-dimethylmethanamine (Ipivivint), to a pharmaceutical composition comprising them and their medical use for the treatment of disorders characterized by the activation of of the Wnt signaling pathway selected from cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis and idiopathic pulmonary fibrosis. Also claimed is a process for the preparation of compounds of Formula (I) by reacting a starting material of Formula (A1) with a compound of Formula (A2).

Antituberculosis Activity of the Antimalaria Cytochrome bcc Oxidase Inhibitor SCR0911

The ability to respire and generate adenosine triphosphate (ATP) is essential for the physiology, persistence, and pathogenicity of Mycobacterium tuberculosis, which causes tuberculosis. By employing a lead repurposing strategy, the malarial cytochrome bc

Pleuromutilin derivatives such, its pharmaceutical composition and synthetic method and use thereof

The present invention relates to a class of pleuromytilin compounds represented by the following general formula (I), pharmaceutically acceptable salts and preparation methods thereof, and compositions comprising the compound represented by the general fo

HETEROARYLS AND USES THEREOF

The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

HETEROARYLS AND USES THEREOF

The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

DIHYDROQUINOLINE-2-ONE DERIVATIVES

The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.

NEW DIHYDROQUINOLINE-2-ONE DERIVATIVES

The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4? R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.

Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor

Despite the progress of the past two decades, there is still considerable need for safe, efficacious drugs that target human immunodeficiency virus (HIV). This is particularly true for the growing number of patients infected with virus resistant to currently approved HIV drugs. Our high throughput screening effort identified a benzophenone template as a potential nonnucleoside reverse transcriptase inhibitor (NNRTI). This manuscript describes our extensive exploration of the benzophenone structure-activity relationships, which culminated in the identification of several compounds with very potent inhibition of both wild type and clinically relevant NNRTI-resistant mutant strains of HIV. These potent inhibitors include 70h (GW678248), which has in vitro antiviral assay IC50 values of 0.5 nM against wild-type HIV, 1 nM against the K103N mutant associated with clinical resistance to efavirenz, and 0.7 nM against the Y181C mutant associated with clinical resistance to nevirapine. Compound 70h has also demonstrated relatively low clearance in intravenous pharmacokinetic studies in three species, and it is the active component of a drug candidate which has progressed to phase 2 clinical studies.

NOVEL AZALIDE AND AZALACTAM DERIVATIVES AND PROCESS FOR THE PRODUCTION OF THE SAME

A compound represented by the following general formula (1) or a pharmaceutically acceptable salt thereof, which is useful for a prophylactic and/or therapeutic treatment of a microbial infectious disease. [R1 is hydrogen atom, or a linear C1-6 alkylcarbonyl group; R2 is hydrogen atom, or a C1-6 alkylcarbonyl group; R3 is hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C1-6 alkenyl group, a C2-6 alkenylcarbonyl group, a C2-6 alkynyl group, or an Ar-B- group (Ar represents an aryl group, or a heterocyclic group, and B is a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C2-6 alkenyl group, a C2-6 alkenylcarbonyl group, or a C2-6 alkynyl group); R5, R6, R7, and R8 represent hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or an Ar-B'- group (B' is a C1-6 alkyl group, a C2-6 alkenyl group, or a C2-6 alkynyl group); X is oxygen atom, or an -NR4- group (R4 is hydrogen atom, a C1-6 alkyl group, or a C1-6 alkyl group which may be substituted with an Ar group); and R4' is hydrogen atom, or a group represented by the aforementioned formula (a) (R3" and R4" represent hydrogen atom, or a linear or branched C1-6 alkylcarbonyl group)]

Vitamin D analogues

The invention relates to novel bicyclic compounds having the general formula (I): as well as to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, in carcinology and in the field of autoimmune diseases and that of organ or tissue transplants in particular), or alternatively in cosmetic compositions.