Candida acid protease inhibiting compounds
Patent 5120718 Issued on June 9, 1992. Estimated Expiration Date: 
June 13, 2011. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
June 13, 2011. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.Patent References[[4 -[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]-methyl]-1H- imidazoles and 1H-1,2,4-triazoles having antimicrobial properties 2-Azolylmethyl-2-aryl-1,3-dioxolanes and the salts thereof, agents containing same, and the use thereof 1-[1-aryl-1-hydroxy-2-azolyl-ethyl]-1-aryl-cyclopropane derivatives, and their fungicidal use thereof Patent #: 4870088 InventorsApplicationNo. 714820 filed on 06/13/1991US Classes:514/32, Oxygen of the saccharide radical bonded to a nonsaccharide hetero ring by acyclic carbon bonding514/247, Hetero ring is six-membered consisting of two nitrogens and four carbon atoms (e.g., pyridazines, etc.)514/252.11, Plural 1,4-diazine rings attached directly or indirectly to each other by nonionic bonding514/253.01, The additional hetero ring is six-membered consisting of one nitrogen and five carbon atoms514/253.06, Quinolines (including hydrogenated)514/254.01, The additional hetero ring is five-membered having ring nitrogen514/254.02, The additional five-membered hetero ring also has chalcogen as a ring member514/254.05, Plural nitrogens in the additional five-membered hetero ring514/255.01, Nitrogen or -C(=X)-, wherein X is chalcogen, bonded directly to the piperazine ring514/255.02, Chalcogen bonded directly to a piperazine ring carbon514/277, Hetero ring is six-membered consisting of one nitrogen and five carbon atoms514/408, The five-membered hetero ring consists of one nitrogen and four carbons514/410, Polycyclo ring system having the five-membered hetero ring as one of the cyclos514/422, Additional hetero ring514/426Nitrogen bonded directly to the five-membered hetero ring by nonionic bondingExaminersPrimary: Nutter, Nathan M.Attorney, Agent or FirmForeign Patent References
International ClassesA61K 031/395A61K 031/415 A61K 031/425 A61K 031/44 AbstractCompounds which inhibit Candida acid protease are disclosed which have the formula: ##STR1## wherein R1 is loweralkyl, loweralkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, arylalkyl or (heterocyclic)alkyl;R2 is loweralkyl, cycloalkylalkyl or arylalkyl;R3 is --OH or --NH2 ;R4 is(a) --CH(OH)--R5 wherein R5 is loweralkyl, cycloalkyl or cycloalkylalkyl or(b) --CH2 CH(R6)C(O)NHR7 wherein R6 is loweralkyl and R7 is loweralkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, cyanoalkyl or (heterocyclic)alkyl; andA is ##STR2## wherein R8 is arylalkyl, B is --C(O) or --S(O)2 -- and R9 is aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl; or ##STR3## wherein R10 is arylalkyl and R11 is (a) --C(O)R12 wherein R12 is alkoxy, arylalkoxy, aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl or (b) --S(O)2 --R13 wherein R13 is aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl; or a pharmaceutically acceptable salt, ester or prodrug thereof.Other References
Field of SearchOxygen of the saccharide radical bonded to a nonsaccharide hetero ring by acyclic carbon bondingHetero ring is six-membered consisting of one nitrogen and five carbon atoms The five-membered hetero ring consists of one nitrogen and four carbons Polycyclo ring system having the five-membered hetero ring as one of the cyclos Additional hetero ring Nitrogen bonded directly to the five-membered hetero ring by nonionic bonding Hetero ring is six-membered consisting of two nitrogens and four carbon atoms (e.g., pyridazines, etc.) | |
