221024-31-3

Upstream product

• 221024-29-9 1-acetyl-5-bromo-7-chloro-indoline 
• 22190-38-1 5-bromo-N-acetylindoline 
• 22190-33-6 5-bromoindoline 

Downstream Products

• 424834-57-1 5-formyl-7-chloroindole 
• 180623-89-6 5-bromo-7-chloro-1H-indole 

Relevant academic research and scientific papers

COMPOUND HAVING ERK KINASE INHIBITORY ACTIVITY AND USE THEREOF

The invention relates to a compound of formula (I): wherein variables are as defined in the specification. The compound is an inhibitor of an ERK kinase, e.g. ERK1 and/or ERK2 kinase. The invention also relates to the use of the compound and a method for preparing the compound, and a pharmaceutical composition containing the compound.

METHOD OF PREPARING 1-(INDOLIN-5-YL)PROPAN-2-OL DERIVATIVES

The present invention relates to a novel method of preparing an indoline derivative usable as a synthetic intermediate of silodosin used in a medicine for dysuresia accompanied with prostatomegaly. The present invention can prepare an optically pure compound represented by a chemical formula (III) from a compound represented by a chemical formula (IV); then prepare a compound represented by a chemical formula (II) by making an alcohol group of the compound represented by chemical formula (III) act as a leaving group; and then prepare a high purity compound represented by a chemical formula (I) under a warm reaction condition. A, P, R_1, R_2 and Y in the chemical formulae are the same as defined in the specification.COPYRIGHT KIPO 2015

Potent, orally active heterocycle-based combretastatin A-4 analogues: Synthesis, structure - Activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation

The synthesis and structure - activity relationship study of a series of compounds with heterocycles in place of the cis double bond in combretastatin A-4 (CA-4) are described. Substituted tosylmethyl isocyanides were found to be the key intermediates in construction of the heterocycles. Cytotoxicities of the heterocycle-based CA-4 analogues were evaluated against NCI-H460 and HCT-15 cancer cell lines. 3-Amino-4-methoxyphenyl and N-methyl-indol-5-yl were the best replacements for the 3-hydroxy-4-methoxyphenyl in CA-4. 4,5-Disubstituted imidazole was found to be the best for the replacement of the cis double bond in CA-4. Medicinal chemistry efforts led to the discovery of compounds 24h and 25f that were found to be 32 and 82% bioavailable, respectively, in rat. Evaluation of 24h and 25f against murine M5076 reticulum sarcoma in mice revealed that both compounds were orally efficacious with an increase in life span of 38.5 and 40.5%, respectively.

Oxazoline antiproliferative agents

Compounds having Formula I are useful for treating cancer. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of treating cancer in a mammal.

Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone(CRH) antagonists, useful for treating CNS and stress-related disorders

Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.