94841-17-5

Usage

Uses

Used in Pharmaceutical Industry:
Spirapril hydrochloride is used as an antihypertensive agent for the treatment of hypertension. It functions as an ACE inhibitor, helping to lower blood pressure and providing a therapeutic option for patients with hypertension.
Used in Cardiology:
In the field of cardiology, spirapril hydrochloride is utilized for its beneficial hemodynamic effects in patients with severe congestive heart failure. Its extended duration of action, over 24 hours, makes it a valuable treatment option for managing heart failure symptoms and improving patient outcomes.

Originator

Schering-Plough (U.S.A.)

InChI:InChI=1/C22H30N2O5S2.ClH/c1-3-29-21(28)17(10-9-16-7-5-4-6-8-16)23-15(2)19(25)24-14-22(30-11-12-31-22)13-18(24)20(26)27;/h4-8,15,17-18,23H,3,9-14H2,1-2H3,(H,26,27);1H/t15-,17-,18-;/m0./s1

Upstream product

• 83647-97-6 spirapril 
• 64187-47-9 1-benzyloxycarbonyl-4-keto-L-proline 
• 89371-34-6 N-succinimidyl (2S)-2-{N-[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino}propionate 
• 83507-90-8 N-<(phenylmethoxy)carbonyl>-1,4-dithia-7-azaspiro<4.4>nonane-8(S)-carboxylic acid ethyl ester 
• 83507-89-5 N-<(phenylmethoxy)carbonyl>-4-oxo-(S)-proline ethyl ester 
• 83552-44-7 1,4-dithia-7-azaspiro<4.4>nonane-8(S)-carboxylic acid 
• 82717-96-2 [1(S)-(ethoxycarbonyl)-3-phenylpropyl]-(S)-alanine 

Relevant academic research and scientific papers

POLYMORPHIC FORMS OF SPIRAPRIL HYDROCHLORIDE

The present invention is concerned with new polymorphic forms of spirapril hydrochloride, processes for preparing the new polymorphic forms, pharmaceutical compositions containing them, therapeutic uses thereof and methods of treatment employing them.

Angiotensin Converting Enzyme Inhibitors: Spirapril and Related Compounds

The synthesis of spirapril (5), spiraprilat (25), their RSS stereoisomers, and their glycyl (18b) and lysyl (36, 37) analogues is described.These compounds were evaluated in vivo for inhibition of angiotensin converting enzyme (ACE), and selected compounds were evaluated for in vitro ACE inhibition (spirapril ID50 16 μg/kg; spiraprilat IC50 0.8 nM, ID50 8 μg/kg).In anesthetized rats, iv, esters 5 and 36 are more potent than enalapril, and diacids 25 and 37 are more potent than enalaprilat in vitro.In the conscious rats, orally, 5 and enalapril (2) showed potent and sustained activity at doses of 0.03-1 and 0.1-1 mg/kg, respectively.From this work, spirapril was selected for clinical evaluation as an antihypertensive agent.