Hepatitis C inhibitor tri-peptides

Details Hepatitis C inhibitor tri-peptides Hepatitis C inhibitor tri-peptides

2008-09-30

2008-09-30

Lambkin, Deborah C (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C514S312000, C514S314000, C514S339000, C514S370000, C514S425000, C546S153000, C546S159000, C546S171000, C546S175000, C546S276400, C548S517000, C548S519000, C548S523000, C548S571000

Reissue Patent

active

11241899

ABSTRACT:
A racemate diastereoisomer and optical isomer of a compound of formula (I):wherein B is H, a C6or C10aryl, C7-16aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6alkyl; C1-6alkoxy; C1-6alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6alkyl; amido; or (lower alkyl)amide; orB is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5is H or C1-6alkyl; andY is H or C1-6alkyl;R3is C1-8alkyl, C3-7cycloalkyl, or C4-10alkylcycloalkyl, all optionally substituted with hydroxy, C1-6alkoxy, C1-6thioalkyl, amido, (lower alkyl)amido, C6or C10aryl, or C7-16aralkyl;R2is C2—R20, NH—R20, O—R20or S—R20, wherein R20is a saturated or unsaturated C3-7cycloalkyl or C4-10(alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21,or R20is a C6or C10aryl or C7-14aralkyl optionally substituted, or R20is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6or C10 aryl, C7-14aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; andR1is H; C1-6alkyl, C3-7cycloalkyl, C2-6alkenyl, or C2-6alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.

REFERENCES:
patent: 6767991 (2004-07-01), Llinas-Brunet et al.
patent: 196 00 034 (1997-07-01), None
patent: 05 155827 (1993-06-01), None
patent: WO 98 17679 (1998-04-01), None
patent: WO 99 07733 (1999-02-01), None
Gaucher et al: “Palladium (0) Catalyzed Tandem Alkylation and SN Cyclization of 1,4-Dichlorobut -2-ene by the N-(Diphenylmethylene) acetonitrile. A Stereoselective Synthesis of 1-Aminocyclo- propanecarboxylic Acids”;Tetrahedron Letters, vol. 36, No. 17,pp. 2979-2982; 1995.
Fliche, Et Al; “Enantioselective synthesis of (1R,2S) and (1S,2S) dehydrocoronamic acids”, Synthetic Communications; vol. 24, No. 20, 1994, pp. 2873-2876.
Chen, Et Al; “Chirally selective hydrolysis of D, L amino acid esters by alkaline protease”; J. Chem, Soc. Chem. Commun., vol. 20, 1986, pp. 1514-1516.
Chen, Et Al; “Kinetic resolution of esters of amino acids in t-butanol containing 5% water catalyzed by a stable industrial alkaline protease”; Chirality, vol. 6, 1994, pp. 572-576.
Linas-Brunet, M., Et Al; “Peptide-based inhibitors of the hepatitis C virus serine protease”, Bioorganic & Medicinal Chemistry Letters, vol. 8, No. 13, pp. 1713-1718; 1998.
Gershonov Et Al; “1-Aminocyclobutanecarboxylic acid derivates as novel structural elements in bioactive peptides; application to tuftsin analogs”; Journal of Medicinal Chemistry, vol. 39, No. 24, 1996, pp. 4833-4843.
Ogawa, Tomohisa Et Al; “2,3-Methanophenylalanine And.Alpha., .Beta.-Dehdrophenylalanine Derivatives As Chymotrypsin Inhibitor”; Pept. Chem. (1990), vol. 27; pp. 379-382.

Affiliated with

Also associated with

Rating

Hepatitis C inhibitor tri-peptides does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Hepatitis C inhibitor tri-peptides, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Hepatitis C inhibitor tri-peptides will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-3927889