37407-24-2

Upstream product

• 771-94-8 3-methylsulfanyl-4-nitrophenol 
• 394-41-2 3-fluoro-4-nitrophenol 

Downstream Products

• 18232-06-9 2-methylthio-p-benzoquinone 
• 37407-25-3 4-acetoxy-1-acetylamino-2-methylsulfanyl-benzene 
• 18231-99-7 1,4-dihydroxy-2-(methylthio)benzene 
• 1160825-76-2 tert-butyl N-(4-hydroxy-2-methylsulfanylphenyl)carbamate 
• 884340-41-4 4-(4-amino-3-(methylthio)phenoxy)-3-nitropyridin-2-amine 

Relevant academic research and scientific papers

POLYAROMATIC UREA DERIVATIVES AND THEIR USE IN THE TREATMENT OF MUSCLE DISEASES

The current invention provides urea derivatives, in particular compounds having the core structure heteroaryl-NH-CO-NH-aryl-O- heteroaryl, for use in treating, ameliorating, delaying, curing and/ or preventing a disease or condition associated with muscle cells and/or satellite cells, such as Duchenne muscular dystrophy, Becker muscular dystrophy, cachexia or sarcopenia.

Novel potent BRAF inhibitors: Toward 1 nM compounds through optimization of the central phenyl ring

BRAF, a serine/threonine specific protein kinase that is part of the MAPK pathway and acts as a downstream effector of RAS, is a potential therapeutic target in melanoma. We have developed a series of small-molecule BRAF inhibitors based on a 1H-imidazo[4,5-b]pyridine-2(3H)-one scaffold (ring A) as the hinge binding moiety and a number of substituted phenyl rings C that interact with the allosteric binding site. The introduction of various groups on the central phenyl ring B combined with appropriate A- and C-ring modifications afford very potent compounds that inhibit V600EBRAF kinase activity in vitro and oncogenic BRAF signaling in melanoma cells. Substitution on the central phenyl ring of a 3-fluoro, a naphthyl, or a 3-thiomethyl group improves activity to yield compounds with an IC50 of 1 nM for purified V 600EBRAF and nanomolar activity in cells.

PYRIDO[2,3-B]PYRAZINE-8-SUBSTITUTED COMPOUNDS AND THEIR USE

The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

IMIDAZO[4,5-B]PYRIDIN-2-ONE AND OXAZOLO[4,5-B]PYRIDIN-2-ONE COMPOUNDS AND ANALOGS THEREOF AS THERAPEUTIC COMPOUNDS

The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formula (I): wherein: J is independently -O- or -NRN1-; RN1, if present, is independently -H or a substituent; RN2 is independently -H or a substituent; Y is independently -CH= or -N=; Q is independently -(CH2)j-M-(CH2)k- wherein: j is independently 0, 1 or 2; k is independently 0, 1, or 2; j+k is 0, 1, or 2; M is independently -O-, -S-, -NH-, -NMe-, or -CH2-; each of RP1, RP2, RP3, and RP4 is independently -H or a substituent; and additionally RP1 and RP2 taken together may be -CH=CH-CH=CH-; L is independently: a linker group formed by a chain of 2, 3, or 4 linker moieties; each linker moiety is independently -CH2-,-NRN-, -C(=X)-, or -S(=O)2-; exactly one linker moiety is -NRN-, or: exactly two linker moieties are -NRN-; exactly one linker moiety is -C(=X)-, and no linker moiety is -S(=O)2-; or: exactly one linker moiety is -S(=O)2-, and no linker moiety is -C(=X)-; no two adjacent linker moieties are -NRN-; X is independently =O or =S; each RN is independently -H or a substituent; A is independently: C6-14carboaryl, C5-14heteroaryl, C3-12carbocyclic, C3-12heterocyclic; and is independently unsubstituted or substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.