Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-05-31
1998-07-07
Ramsuet, Robert W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514330, A61K 31445, A61K 31535
Patent
active
057769338
ABSTRACT:
Novel aminediol compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds in inhibiting retroviral protease, particularly useful in the treatment and/or prevention of HIV infection (AIDS).
REFERENCES:
patent: 2046720 (1936-07-01), Bottoms
patent: 2715631 (1955-08-01), Coxall et al.
patent: 4483850 (1984-11-01), Patchett et al.
patent: 4528282 (1985-07-01), Preston et al.
patent: 4602002 (1986-07-01), Patchett et al.
patent: 4644055 (1987-02-01), Kettner et al.
patent: 4665055 (1987-05-01), Evans
patent: 4719288 (1988-01-01), Fuhrer et al.
patent: 4727060 (1988-02-01), Buhlmeyer et al.
patent: 4855286 (1989-08-01), Wagner et al.
patent: 5098924 (1992-03-01), Poss
patent: 5142056 (1992-08-01), Kempe et al.
patent: 5157041 (1992-10-01), Handa et al.
patent: 5169952 (1992-12-01), Askin et al.
patent: 5196438 (1993-03-01), Martin et al.
Goldman et al., L-696,229 Specifically Inhibits Human Immunodeficiency Virus Type 1 Reverse Transcriptase and Possesses Antiviral Activity In Vitro, Antimicrobial Agents Chemotherapy, pp. 1019-1023(1992).
Grobelny, et al., Selecive Phosphinate Transiion-State Analogue Inhibitors of the Protease of Human Immunodeficiency Virus; Biochemical and Biophysical Research Communications; vol. 169, No. 3, pp. 1111-1116(1990).
Hui, et al., A Rational Approach in the Search for Potent Inhibitors Against HIV proteinase; The FASEB Journal, vol.5, pp. 2606-2610(1991).
Humber, et al., Penicillin Derived C.sub.2 -Symmetric Dimers as Novel Inhibitors of HIV-1 Proteinase, J. Med. Chem., 35, pp. 3080-3081 (1992). Replacement: Potent Slow-Binding Inhibition of the HIV Protease, J. Am. Chem. Soc., 114, pp. 7604-7606 (1992).
Kotler, et al., Synthetic Peptides as a Substrates and Inhibitors of a Retroviral Protease; Proc. Natl. Acad. Sci., vol. 85, pp. 4185-4189(1988).
Kahn, et al., Examination of HIV-1 Protease Secondary Structure Specificity Using Conformationally Constrained Inhibitors; J. Med. Chem., , pp. 3395-3399(1991).
Kempf, et al., Structure-Based, C.sub.2 Symmetric Inhibitors of HIV Protease; J. Med. Chem., 33, pp. 2687-2689(1990).
Kempf, et al., Antiviral and Pharmacokinetic Properties of C.sub.2 Symmetric Inhibitors of the Human Immunodeficiency Virus Type 1 Protease; Antimicrobial Agents and Chemotherapy , vol. 35, No. 11, pp. 2209-2214(1991).
Korant, et al., Virus-specified protease in poliovirus-infected HeLa cells; Proc. Natl. Acad. Sci. USA, vol. 76, No. 6, pp.2992-2995(1979).
Krohn, et al., Novel Binding Mode of Highly Potent HIV-Proteinase Inhibitors Incorporating the (R)-Hydroxyethylamine Isostere; J. Med. Chem. 34, pp. 3340-3342(1991).
Lambert, et al., Human Immunodeficiency Virus Type 1 Protease Inhibitors Irreversibly Block Infectivity of Purified Viriond from Chronically Infected Cels; Antimicrobial Agents and Chemotherapy, pp. 982-988(1992) (absract only).
Lingham, et al., HIV-1 Protease Inhibitory Activity of L-694,746, A Novel Metabolite of L-689,502; Biochemical and Biophysical Research Comm., vol. 181, No. 3, pp. 1456-1461(1991).
Lingham, et al., L-696,474, A Novel Cytochalasin as an Inhibitor of HIV-1 Protease III. Biological Activity; J. of Antibiotics, p. 686(1992).
Lyle, et al, Benzocycloalkyl Amines as Novel C-Termini for HIV Protease Inhibitors; J. Med. Chem., 34, pp. 1228-1230(1991).
McLeod, et al., Phosphonamidates and Phosphonamidate Esters as HIV-1 Protease Inhibitors; Bioorganic & Medicinal Chemistry Letters, vol. 1, No.11, pp. 653-658(1991).
Mimoto, et al., KNI-102 A Novel Tripeptide HIV Protease Inhibitor Containing Allophenylnorstatine as a Transition-State Mimic; Chem. Pharm. Bull. vol. 39, No. 11, pp. 3088-3090(1991).
Mimoto, et al., Rational Design and Synthesis of a Novel Class of Active Site-Targeted HIV Proease Inhibitors Containing a Hydroxymethylcarbonyl Isotere. Use of Phenylnorstatine or Allophenylnorstatine as a Transition-State Mimic; Chem. Pharm. Bull. vol. 39, No. 9, pp.2465-2467(1991).
Moore, et al. Peptide Substrates and Inhibitors of the HIV-1 Protease; Biochemical and Biophysical Research Communications; vol. 159, No. 2, pp. 420-425(1989).
Ondeyka, et al., L-696,474, A Novel Cytochalasin as an Inhibitor of HIV-1 Protease II. Isolation and Structure; J. of Antibiotics, vol. 45, No. 5, p.679(1992).
Owens, et al., The Rapid Identification of HIV Protease Inhibitors Through the Synthesis and Screening of Defined Peptide Mixtures; Biochemical and Biophysical Research Communications; vol. 181, No. 1 pp. 402-408 (1991).
Peyman, et al., C.sub.2 -Symmetric Phosphinic Acid Inhibitors of HIV Protease; Tetrahedron Letters, vol. 33, No. 32, pp. 4549-4552(1992).
Raju, et al., Substrate Analog Inhibitors of HIV-1 Protease Containing Phenylnorstatine as a Transition State Element; Biochemical and Biophysical Research Communications; vol. 180, No. 1, pp. 181-186(1991).
Raju, et al., Investigating the Stereochemistry of Binding to HIV-1 Protease with Inhibitors Containing Isomers of 4-Amino-3-hydroxy-5-phenylpentanoic Acid,, Biochemical and Biophysical Research Communications, vol. 180, No. 1, pp. 187-190(1991).
Rich, et al., Hydroxyethamine Analogues of the p17/p24 Substrate Cleavage Site Are Tight-Binding Inhibitors of HIV Protease; J. Med. Chem., 33, pp. 1285 -1288. (1990).
Rich, et al., Effect of Hydroxyl Group Configuraton in Hydroxyethylamine Dipeptide Isosteres on HIV Protease Inhibition. Evidence for Multiple Binding Modes; J. Med. Chem., 34, pp. 1222 -1225 (1991).
Roberts, et al., Rational Design of Peptide -Based HIV Proteinase Inhibitors; Science, vol. 248, pp. 358 -361 (1990).
Schramm, et al., Inhibition of HIV-1 Protease By Short Peptides Derived From the Terminal Segments of the Protease; Biochemical and Biophysical Research Comm., vol. 184, No. 2, pp. 980 -985 (1992).
Sham, et al., Potent HIV-1 Protease Inhibitors with Antiviral Activities In Vitro; Biochemical and Biophysical Research Communications; vol. 175, No. 3, pp. 914 -919 (1991).
Tam, et al., Intriguing Structure-Activity Relations Underlie the Potent Inhibition of HIV Protease by Norstatine-Based Peptides; J. of Medicinal Chemistry, vol. 35, No. 7, pp. 1318 -1320 (1992).
Thaisirivongs, et al., Inhibitors of the Protease from Human Immunodeficiency Virus: Design and Modeling of a Compound Containing a Dihydroxyethelene Isostere Insert with High Binding Affinity and Effective Antiviral Activity; J. Med. Chem., 34, pp. 2344-2356 (1991).
Thompson, et al., Synthesis and Antiviral Activit of a Series of HIV-1 Protease Inhibitors with Functionality Tethered to the P.sub.1 or P.sub.1 'Phenyl Substituents: X-ray Crystal Structure Assisted Design; J. Med. Chem., 35, pp. 1685 -1701 (1992).
Tomaselli, et al., Specificity and Inhibition of Proteases from Human Immunodeficiency Viruses 1 and 2; The Journal of Biochemical Chemistry vol. 265, pp. 14675-14683 (1990).
Tucker, et al., A. Series of Potent HIV-1 Protease Inhibitors Containing a Hydroxyethyl Secondary Amine Transition State Isotere: Synthesis, Enzyme Inhibition, and Antiviral Activity, J. Med. Chem., 35, 2525-2533 (1992).
Urban, et al., Reduced-bond Tight-Binding Inhibitors of HIV-1 Protease, Fine Tuning of the Subsite Specificity; FEBS Letters, vol.298, No. 1, pp. 9 -13 (1992).
Vacca, et al., L-687,908, a Potent Hydroxyethylene-Containing HIV Protease Inhibitor; J. Med. Chem., 34, pp. 1225 -1228 (1991).
Young, et al., HIV-1 Potease Inhibitors Based on Hydroxythylene Dipeptide Isosteres: An Investigation into the Role of the P.sub.1 'Side Chain on Structure-Activity; J. Med. Chem., 35, pp. 1702 -1709 (1992).
Ghosh, et al., 3-Tetrahydrofuran and Pyran Urethanes as High-Affinity P.sub.2 --Ligands for HIV-1 Protease Inhibitors, J. Med. Chem., 36, 292-294 (1993).
Getman et al., Discovery of a Novel Class of Potent HIV-1 Protease Inhibitors Containing the (R)-(Hydroxyethyl)urea Isostere, J. Med. Chem., 36, 288-291 (1993).
Ghosh et al., Cyclic Sulfolanes as Novel and High Affinity P.sub.2 -Ligands for HIV-1 Protease Inhibitors, J. Med. Chem., 36, 924-927 (1993).
Martin, Antiviral. Res., 17, 265-278 (1992).
Gordon et al., Biochem. Biophys. Res. Commun., 126(1), 419-426 (
Barrish Joel C.
Bisacchi Gregory S.
Gordon Eric M.
Sun Chong-Qing
Tino Joseph A.
Babajko Suzanne E.
E. R. Squibb & Sons Inc.
Ramsuet Robert W.
LandOfFree
Method of inhibiting protease does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Method of inhibiting protease, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Method of inhibiting protease will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1206142