Enzyme inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...

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Details

C514S550000, C560S150000, C562S556000

Reissue Patent

active

10407204

ABSTRACT:
A compound of formula (I)whereinR1is a C1-6straight or branched chain alkyl group, a C2-6alkenyl group, a C2-6alkynyl group, a C3-6cycloalkyl group or a C3-6cycloalkylC1-6alkyl group, each optionally substituted by one to three groups independently selected from: —CN; —NO2; a group —COR2wherein R2is hydrogen, C1-6alkyl, —OR3wherein R3is hydrogen or C1-6alkyl or NR4R5wherein R4and R5are independently selected from hydrogen or C1-6alkyl; a group —S(O)mR6wherein m is 0, 1 or 2, R6is hydrogen, C1-6alkyl, hydroxy or NR7R8wherein R7and R8are independently hydrogen or C1-6alkyl; a group PO(OR9)2wherein R9is hydrogen or C1-6alkyl; a group NR10R11wherein R10and R11are independently selected from hydrogen, C1-6alkyl, —COR12wherein R12is hydrogen or C1-6alkyl, or —S(O)m′R13wherein m′ is 0, 1 or 2 and R13is hydrogen or C1-6alkyl; halo; or a group —OR14wherein R14is hydrogen, C1-6alkyl optionally substituted by one to three halo atoms, C6-10aryl or —COR15wherein R15is hydrogen or C1-6alkyl; p is 2 or 3, q is 1 or 2 and n is 0 or 1 and all salts, esters, amides and physiologically acceptable prodrugs thereof; pharmaceutical uses and formulations therefor; and processes for their preparation are disclosed.

REFERENCES:
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Tanaka et al, J. Biol. Chem. 249 (16) 5285-9 (1974).
‘Houben-Weyl “Methoden der organischen Chemie”, Bd E5’, 1985, George Thieme Vergag, Stuttgart.
Chemcial Abstracts, vol. 72, No. 13, Mar. 30, 1970, Abstract No. 67238p, Hermann, Peter et al, ‘Synthesis of some sulfur-containing amino acid analogs’, p. 438; col. 1 & J. Prakt. Chem., vol. 311, No. 6, 1969, pp. 1018-1028.
Chemical Abstracts, vol. 66, No. 21, May 22, 1967, Columbus, Ohio, Abstract No. 91926h, Donald T. Elmore et al, ‘Kinetics and mechanism of catalysis by proteolytic enzymes . . . ’, p. 8590; col. 1; see abstract & Biochem J., vol. 102, 1967, pp. 728-734.

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