148367-08-2

Upstream product

• 558-13-4 carbon tetrabromide 
• 148367-04-8 1-(4-Isobutylphenyl)pentan-1-ol 
• 538-93-2 1-phenyl-2-methylpropane 
• 148367-01-5 1-(4-isobutylphenyl)pentan-1-one 
• 638-29-9 n-valeryl chloride 

Downstream Products

• 148366-62-5 ethyl 4-[3-[4-[1-(4-isobutylphenyl)pentyloxy]benzoyl]indol-1-yl]butyrate 
• 146939-45-9 ethyl 4-[1-[4-[1-(4-isobutylphenyl)pentyloxy]benzoyl]indolizin-3-yl]butyrate 
• 159894-77-6 3-[1-(4-isobutylphenyl)pentyloxy]propanol 

Relevant academic research and scientific papers

4-(Benzoylindolizinyl)butyric acids; novel nonsteroidal inhibitors of steroid 5α-reductase. III

A novel series of indolizinebutyric acids with various benzoyl substituents was synthesized to develop nonsteroidal inhibitors of steroid 5α-reductase, and the structure-activity relationships in this series were studied. We previously reported the structure-activity relationships in a series of indolebutyric acids as well as the discovery of the novel nonsteroidal 5α-reductase inhibitor, FK143. We have now made other modifications to this compound to improve in vivo inhibitory activity. By altering the heterocyclic nucleus and changing the benzoyl substituent we have succeeded in identifying the strongly active compound, FK687, (S)-4-[1-[4-[[1-(4-isobutylphenyl)butyl]oxy]benzoyl]indolizin-3-yllbutyric acid, which displays strong in vitro inhibitory activity against the human enzyme and in vivo inhibitory activity against the castrated young rat model. This compound should be a useful agent for the treatment of benign prostatic hyperplasia.

Indole derivatives useful as testosterone 5α-reductase inhibitors

A compound of the formula (I): STR1 wherein R 1 is an optionally protected carboxy(lower)alkyl, R 2 is a hydrogen, an optionally substituted aryl or a carboxy,X is a bond, --0--, --NH-- or a cycloalkylene, andY is an alkylene which may be interrupted by an oxygen atom, an alkenylene or an alkadienylene,or a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a testosterone 5α-reductase inhibitor and effective against testosterone 5α-reductase-mediated diseases such as prostatism, prostatic hypertrophy, prostatic cancer, alopecia, hirsutism (e.g. female hirsutism), androgenic alopecia (or male-pattern baldness), acne (e.g. acne vulgaris, pimple), and other hyperandrogenisms.

INDOLE DERIVATIVES AND THEIR USE FOR TESTOSTERONE 5-ALPHA-REDUCTASE-MEDIATED DISEASES

Indole derivatives of the formula and pharmaceutical compositions thereof. They are useful for treating or preventing testosterone 5-alpha-reductase-mediated diseases, such as alopecia, acnes and prostatism