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Last Updated: September 20, 2020

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Patent: 8,183,252

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Summary for Patent: 8,183,252
Title:Heterocyclic aspartyl protease inhibitors
Abstract: Disclosed are compounds of the formula I ##STR00001## or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, --C(.dbd.S)--, --S(O)--, --S(O).sub.2--, --C(.dbd.O)--, --O--, --C(R.sup.6)(R.sup.7)--, --N(R.sup.5)-- or --C(.dbd.N(R.sup.5))--; X is --O--, --N(R.sup.5)-- or --C(R.sup.6)(R.sup.7)--; provided that when X is --O--, U is not --O--, --S(O)--, --S(O).sub.2--, --C(.dbd.O)-- or --C(.dbd.NR.sup.5)--; U is a bond, --S(O)--, --S(O).sub.2--, --C(O)--, --O--, --P(O)(OR.sup.15)--, --C(.dbd.NR.sup.5)--, --(C(R.sup.6)(R.sup.7)).sub.b-- or --N(R.sup.5)--; wherein b is 1 or 2; provided that when W is --S(O)--, --S(O).sub.2--, --O--, or --N(R.sup.5)--, U is not --S(O)--, --S(O).sub.2--, --O--, or --N(R.sup.5)--; provided that when X is --N(R.sup.5)-- and W is --S(O)--, --S(O).sub.2--, --O--, or --N(R.sup.5)--, then U is not a bond; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m.sub.1 agonist or m.sub.2 antagonist.
Inventor(s): Zhu; Zhaoning (Plainsboro, NJ), Sun; Zhong-Yue (Parlin, NJ), Stamford; Andrew (Chatham Township, NJ), Greenlee; William J. (Teaneck, NJ), Cumming; Jared N. (Garwood, NJ), Wang; Lingyan (East Brunswick, NJ), Iserloh; Ulrich (Hoboken, NJ), Liu; Xiaoxiang (River Vale, NJ), Huang; Ying (Berkeley Heights, NJ), Li; Guoqing (Belle Mead, NJ), Pan; Jianping (Monmouth Junction, NJ)
Assignee: Schering Corporation (Kenilworth, NJ) Pharmacopeia Inc. (La Jolla, CA)
Application Number:12/693,874
Patent Claims:see list of patent claims

Details for Patent 8,183,252

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Jubilant Hollisterstier Llc POSITIVE SKIN TEST CONTROL - HISTAMINE histamine INJECTION 103891 1 1995-06-15   Start Trial Schering Corporation (Kenilworth, NJ) Pharmacopeia Inc. (La Jolla, CA) 2027-02-23 search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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