Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Synthesis of peptides
Patent
1998-08-21
1999-10-05
Budens, Robert D.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Synthesis of peptides
4241851, 514 19, 530333, 530336, 2609982, C07K 106, C07K 506, A61K 3805
Patent
active
059626402
ABSTRACT:
The present invention provides a novel dipeptide compound or pharmaceutically acceptable salt thereof which exhibits an excellent HIV protease inhibitory activity and an excellent bioavailability from digestive tracts, and an anti-AIDS agent comprising said dipeptide compound as an effective ingredient. ##STR1## (wherein R.sub.1 represents 5-membered or 6-membered monocyclic hydrocarbon group or heterocyclic group wherein more than one carbon atom of said monocyclic hydrocarbon group is substituted with hetero atom. X represents methylene group (--CH.sub.2 --), chloromethylene group(--CH(Cl)--), oxygen atom sulfur atom or sulfonyl group (--SO.sub.2 --). R.sub.21 and R.sub.22 each represents hydrogen atom or aliphatic hydrocarbon group having 1-6 carbons. R.sub.3 represents aliphatic hydrocarbon group or monovalent group derived from aromatic monocyclic hydrocarbon having 1-6 carbons.)
REFERENCES:
patent: 4963655 (1990-10-01), Kinder et al.
patent: 5086165 (1992-02-01), Marshall et al.
patent: 5126326 (1992-06-01), Anderson et al.
patent: 5132400 (1992-07-01), Gammill et al.
patent: 5145951 (1992-09-01), Voges et al.
patent: 5187074 (1993-02-01), Treiber et al.
patent: 5188950 (1993-02-01), Balani et al.
patent: 5192668 (1993-03-01), Treiber et al.
patent: 5212157 (1993-05-01), Anderson et al.
patent: 5342922 (1994-08-01), Marshall et al.
patent: 5434265 (1995-07-01), Fritz et al.
patent: 5438118 (1995-08-01), Callahan et al.
patent: 5475013 (1995-12-01), Talley et al.
patent: 5476874 (1995-12-01), Hungate et al.
patent: 5491166 (1996-02-01), Kaldor et al.
patent: 5492910 (1996-02-01), Barrish et al.
patent: 5502060 (1996-03-01), Thompson et al.
patent: 5502061 (1996-03-01), Hui et al.
patent: 5514802 (1996-05-01), Fritz et al.
patent: 5644028 (1997-07-01), Mimoto et al.
N.A. Roberts et al., "Rational Design of Peptide-Based HIV Proteinase Inhibitors" Science 248:358-362 (1990).
T. Robins et al., "HIV Protase Inhibitors: Their Anti-HIV Activity and Potential Role in Treatment" J. Acquired Immune Deficiency Syndromes 6(2):162-170 (1993).
Communications to the Editor, "Intriguing Structure--Activity Relations Underlie the Potent Inhibition of HIV Protease by Norstatine-Based Peptides" J. Med. Chem. 35:1318-1320 (1992).
Baldwin et al. (1995),"Structure of HIV-1 Protease With KNI-272, A Tight-Binding Transition-State Analog Containing Allophenylnorstatine," 3 Structure 581-590.
Kiso (1995), "Design and Synthesis of HIV Protease Inhibitors Containing Allophenylnorstatine As A Transition-State Mimic," Aspartic Proteinases Structure, Function, Biology and Biomedical Implications, Ed. Kenji Takahashi, Plenum Press, NY, pp. 413-423.
Gulnik et al. (1995), "Kinetic Characterization and Cross-Resistance Patterns of HIV-1 Protease Mutant Selected under Drug Pressure," Biochemistry, vol. 34, No. 29, 9282-9287.
Kageyama et al. (1993), "In Vitro Anti-Human Immunodeficiency Virus (HIV) Activities of Transition State Mimetic HIV Protease Inhibitors Containing Allophenylnorstatine," 37 Antimicrob. Agents & Chemo. 4:810-817.
Humphrey et al. (1997), "Removal of Human Immunodeficiency Virus Type I (HIV-1) Protease Inhibitors From Preparations of Immature HIV-1 Virions Does Not Result in an Increase in Infectivity or the Appearance of Mature Morphology," 41 Antibmicrob. Agents & Chemo. 5:1017-1023.
Uchida et al. (1997), "HIV-1 Protease Does Not Play A Critical Role In The Early Stages of HIV-1 Infection," 36 Antiviral Research 107-113.
Fahey et al., "Status of Immune-Based Therapies In HIV Infection and AIDS," Clin. Exp. Immunol., 88:1-5 (1992).
Fox, J.L., "No Winners Against AIDS," Bio/Technolgy, 12:128(Feb., 1994).
Haynes et al., "Update On The Issues of HIV Vaccine Development," Ann. Med., 28:39-41 (1996).
Fukazawa Tominaga
Kato Ryohei
Kiso Yoshiaki
Mimoto Tsutomu
Morohashi Naoko
Budens Robert D.
Japan Energy Corporation
LandOfFree
Methods for preparing novel dipeptide compounds or pharmacuetica does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Methods for preparing novel dipeptide compounds or pharmacuetica, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Methods for preparing novel dipeptide compounds or pharmacuetica will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1172950