112290-16-1

Upstream product

• 112290-15-0 4-(2-nitrophenoxy)butanoic acid ethyl ester 
• 88-75-5 2-hydroxynitrobenzene 
• 2969-81-5 Ethyl 4-bromobutyrate 

Downstream Products

• 1026378-36-8 4-{2-[(E)-3-(1-Methyl-1H-indol-5-yl)-but-2-enoylamino]-phenoxy}-butyric acid ethyl ester 
• 156674-28-1 ethyl 4-[2-(indole-5-carboxamido)phenoxy]butyrate 
• 170366-65-1 ethyl (Z)-4-{2-[[4,4,4-trifluoro-3-[1-(1-propyl)butylindol-5-yl]-1-oxo-2-butenyl]amino]phenoxy}butyrate 

Relevant academic research and scientific papers

Method of treatment for prostatic cancer

Disclosed is a new treatment for men with prostatic cancer involving combination therapy of a 5α-reductase inhibitor, i.e., a 17β-substituted 4-azasteroid, a 17β-substituted non-azasteroid, 17β-acyl-3-carboxyandrost-3,5-diene, benzoylaminophenoxybutanoic acid derivative, fused benz(thio)amide or cinnamoylamide derivative, aromatic 1,2-diethers or thioethers, aromatic ortho acylaminophenoxy alkanoic acids, ortho thioalkylacylamino-phenoxy alkanoic acids, pharmaceutically acceptable salts and esters thereof, and particularly finasteride, in combination with an antiandrogen, i.e. flutamide. Pharmaceutical compositions useful for treatment are also disclosed.

Method of treatment for benign prostatic hyperplasia

Disclosed is an improved treatment for men with benign prostatic hyperplasia (BPH), involving combination therapy of a 5α-reductase inhibitor, e.g. a 17β-substituted 4-azasteroid, a 17β-substituted non-azasteroid, 17β-acyl-3-carboxy-androst-3,5-diene, benzoylaminophenoxybutanoic acid derivative, fused benz(thio)amide or cinnamoylamide derivative, aromatic 1,2-diethers or thioethers, aromatic ortho acylaminophenoxy alkanoic acids, ortho thioalkylacylaminophenoxy alkanoic acids, pharmaceutically acceptable salts and esters thereof, and particularly finasteride, in combination with an α1 -adrenergic receptor blocker, i.e., terazosin. The combination provides therapy at the molecular level for the underlying cause of the disease as well as providing symptomatic relief. Pharmaceutical compositions useful for treatment are also disclosed.

Steroid 5α-reductase: Comparative study of mechanism of inhibition by nonsteroids ONO-3805 and LY191704

Two nonsteroids, ONO-3805 and LY191704, were evaluated as inhibitors of the human and rat 5α-reductases (5αR). ONO-3805 was prepared in a 12-step convergent synthesis. This compound is a potent inhibitor of the human and rat 5αRs, with more potent inhibition seen against the rat enzymes. The inhibition patterns of this compound were best fit to an uncompetitive model which suggests binding in a ternary complex with enzyme and NADP+. Apparent K(i) values of 27, 31, 1, and 0.5 nM versus testosterone were obtained with human type 1, human type 2, rat type 1, and rat type 2 5αR, respectively. Multiple inhibition studies with ONO-3805 and NADP+ support synergistic binding of these two inhibitors with all isozymes. LY191704 was also evaluated as an inhibitor of the human and rat 5αRs. This compound is a selective, competitive inhibitor of human type 1 5αR. Poor inhibition was observed with human type 2 and rat types 1 and 2 5αR.

New sulphur containing nonsteroidal drugs as 5-alpha reductase inhibitors

Described are new non-steroidal drugs for treatment of benign prostatic hyperplasia and other disorders mediated by high 5-a reductase activity, high DHT levels and other conditions of hyperandrogenic stimulation, of the formula: wherein A,D,X,R,R',R'',Ra

New non-steroidal agents as 5-alpha reductase inhibitors

Not available

BENZOYLAMINOPHENOXYBUTANOIC ACID DERIVATIVES

A benzoylaminophenoxybutanoic acid derivative of general formula I or non-toxic salts thereof possess an inhibitory activity on 5alpha-reductase, and therefore be useful for treating and/or preventing agent for alopecia, acnes or prostatic hypertrophy