TH135020A - Heterocyclic aspartyl protease inhibitors - Google Patents

Abstract

DC60 (06/11/55) has been revealed as a compound with formula I (formula) I or stereoisomer, tautomer or salt or solvate of matter. These are acceptable. Pharmacy, where W is a bond, -C (= S) -, - S (O) -, - S (O2) -, - C (= O) -, - O -, - C (R6) ( R7) -, - N (R5) - or -C (= N (R5)) -; X is -O -, - N (R5) -, or -C (R6) (R7) -; With the indication that when X is -O-, U is not -O-, -S (O), -S (O2) -, -C (= O), - C (= O) - or -C ( = NR5) -; U is the bond, -S (O) -, S (O2) -, - C (O), - O -, - P (O) (OR15) -, - C (= NR5) -, - (C (R6) (R7)) b- or -N (R5) - where b is 1 or 2; Provided that when W is -S (O) -, S (O2) -, -O- or -N (R5) -U is not -S (O) -, -S (O2) -, - O-. , Or -N (R5) -; provided that when X is -N (R5) - and W is -S (O) -, S (O2) -, - O- or -N (R5) - then U It is not bonded, and R1, R2, R3, R4, R5, R6. And R7 are as they have been defined in detail; And pharmaceutical components The compound, which also contains the compound formula I, has also been disclosed as a method of inhibiting aspartyl protease (aspartyl protease) and especially a co-cardiovascular method. Blood fasting, disease related Perception and nervous breakdown And methods of Ka Inhibition of human immunodeficiency virus, plasmapin, cathetersin D and enzyme-protozol have also been disclosed as a method of detoxification. Cognitive and neurodegenerative therapies using a compound with formula I in combination with a revealed choline esterase inhibitor or an anti-muscarinic agent. Is a compound with formula I (formula) I or stereoisomer, tau thomer or salt or salvate of These are acceptable. Pharmacy, where W is a bond, -C (= S) -, - S (O) -, - S (O2) -, - C (= O) -, - O -, - C (R6) ( R7) -, - N (R5) - or -C (= N (R5)) -; X is -O -, - N (R5) -, or), - C (R6) (R7) -; Provided that when X is -O-, U is not -O-, -S (O) 2-, C (= O), - C (= O) - or -C (= NR5) -; U Is a bond, -S (O) -, S (O) 2 -, - C (O) -, - O -, - P (O) (OR15) -, - C (= N (R5) -, - ( C (R6) (R7)) b- or -N (R5) - where b is 1 or 2; Provided that when W is -S (O) -, S (O) 2-, -O- or -N (R5) -U is not -S (O) -, -S (O) 2 -, -. O-, or -N (R5) -; provided that when X is -N (R5) - and W is -S (O) -, S (O) 2 -, - O- or -N ( R5) - then U is not bonded and R1, R2, R3, R4, R5, R6. And R7, as such, has been defined in detail; And pharmaceutical components The compound, which also contains the compound formula I, has also been disclosed as a method of inhibition of aspartyl protease and especially as a means of the therapy of co-hemorrhagic disease, disease. Cognitive impairment And methods of Ka Inhibition of human immunodeficiency virus, plasmapin, cathetersin D and enzyme-protozol have also been disclosed as a method of detoxification. A neurodegenerative and neurodegenerative therapy that uses a compound with formula I in combination with a choline esterase inhibitor or a patented drug-resistant choline esterase.

Claims (1)

: DC60 (06/11/55) has been revealed as a compound with formula I (formula) I or stereoisomer, tautomer, or salt or salvate of matter. These are acceptable. Pharmacy, where W is a bond, -C (= S) -, - S (O) -, - S (O2) -, - C (= O) -, - O -, - C (R6) ( R7) -, - N (R5) - or -C (= N (R5)) -; X is -O -, - N (R5) -, or -C (R6) (R7) -; With the indication that when X is -O-, U is not -O-, -S (O), -S (O2) -, -C (= O), - C (= O) - or -C ( = NR5) -; U is the bond, -S (O) -, S (O2) -, - C (O), - O -, - P (O) (OR15) -, - C (= NR5) -, - (C (R6) (R7)) b- or -N (R5) - where b is 1 or 2; Provided that when W is -S (O) -, S (O2) -, -O- or -N (R5) -U is not -S (O) -, -S (O2) -, - O-. , Or -N (R5) -; provided that when X is -N (R5) - and W is -S (O) -, S (O2) -, - O- or -N (R5) - then U It is not bonded, and R1, R2, R3, R4, R5, R 6. and R7 are, as they have been defined in detail; And pharmaceutical components The compound, which also contains the compound formula I, has also been disclosed as a method of inhibiting aspartyl protease (aspartyl protease) and especially a co-cardiovascular method. Blood fasting, disease related Perception and nervous breakdown And methods of Ka Inhibition of human immunodeficiency virus, plasmapin, cathetersin D and enzyme-protozol have also been disclosed as a method of detoxification. Cognitive and neurodegenerative therapies using a compound with formula I in combination with a revealed choline esterase inhibitor or an anti-muscarinic agent. Is a compound with formula I (formula) I or stereoisomer, tau thomer or salt or salvate of These are acceptable. Pharmacy, where W is a bond, -C (= S) -, - S (O) -, - S (O2) -, - C (= O) -, - O -, - C (R6) ( R7) -, - N (R5) - or -C (= N (R5)) -; X is -O -, - N (R5) -, or), - C (R6) (R7) -; Provided that when X is -O-, U is not -O-, -S (O) 2-, C (= O), - C (= O) - or -C (= NR5) -; U Is a bond, -S (O) -, S (O) 2 -, - C (O) -, - O -, - P (O) (OR15) -, - C (= N (R5) -, - ( C (R6) (R7)) b- or -N (R5) - where b is 1 or 2; Provided that when W is -S (O) -, S (O) 2-, -O- or -N (R5) -U is not -S (O) -, -S (O) 2 -, -. O-, or -N (R5) -; provided that when X is -N (R5) - and W is -S (O) -, S (O) 2 -, - O- or -N ( R5) - then U is not bonded and R1, R2, R3, R4, R5, R 1. Compounds having the structural formula (formula) I or sterioisomer, tau thomer, or its salts or salvates. These are pharmacologically acceptable where W is a bond, - C (= S), - S (O) -,, -S (O) 2-, C (= O) -, - O-. , -C (R6) (R7) -, -N (R5) -, or -C (= N (R5)) -; X is -O -, - N (R5) -, or), - C (R6 ) (R7) -; Provided that when X is -O-, U is not -O-, -S (O) 2-, -S (O) 2-, -C (= O), - or -C (= (R5) )) -; U is a bond, -S (O) -, S (O) 2 -, - C (O Tag: drug patent