http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-046327-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c76ecadad74a1a35270b3e3a34d60f37 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D263-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D263-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 |
| filingDate | 2004-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f18397c170e170aa3ece3801ea135c29 |
| publicationDate | 2005-12-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-046327-A1 |
| titleOfInvention | OXAZOL COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS |
| abstract | Pharmaceutical compositions and methods for treating neurodegenerative diseases, i.e. Alzheimer's disease, in a mammal. Claim 1: A compound of formula (1) wherein Z is selected from -C (= O) CHR1R2, -C (= S) CHR1R2, - (C = NR8) CHR1R2, - C (= O) C (= O ) R1 and -S (O) 2-R1; R1 is selected from C1-20 alkyl, C2-20 alkenyl, -C2-20 alkynyl, -C1-20 alkoxy, -C2-20 -alkoxy, -C2-20 -alkyloxy, -C3-20 -cycloalkyl, -C4-20 -cycloalkenyl, bi- or C10-20 tricycloalkyl, bi- or C10-20 tricycloalkenyl, 4-20 membered heterocycloalkyl, -C6-20 aryl and 5-20 membered heteroaryl; wherein R1 is optionally and independently substituted with one to six fluorine atoms or with one to three substituents independently selected from the group R1a; R1a is selected in each instance independently of -OH, -C1-12 alkyl, -C2-12 alkenyl, -C2-12 alkynyl, -C 1-6 alkoxy, -C2-6 alkenoxy, -C 1-6 alkyloxy, -F, -Cl, -Br, -I, -CN, -NO2, -NR9R10, -C (= O) NR9R10, -S (O) n-NR9R10, - C (= O) R11, -S (O) n- R11, -C (= O) OR12, -C3-15 cycloalkyl, -C4-15 -cycloalkenyl, C- or 11-6 tricycloalkyl, C7-11-tricycloalkenyl, 4- to 20-membered heterocycloalkyl, -C6 -aryl 15, 5 to 15-membered heteroaryl, C6-15 -aryloxy and 5 to 15-membered heteroaryloxy, wherein said cycloalkyl, cycloalkenyl, bi- or tricycloalkyl, bi- or tricycloalkenyl, heterocycloalkyl, aryl, heteroaryl, aryloxy and heteroaryloxy they are optionally and independently substituted with one to three substituents selected from the group R1b; R1b is selected in each instance independently of -OH, -C1-6 alkyl, -C2-6 alkenyl, -C2-6 alkynyl, -C1-6 alkoxy, -C2-6 alkenoxy, -C2-6 alkynoxy, -C1-hydroxyalkyl -6, -F, -Cl, -Br, -I, - CN, -NO2, -NR9R10, -C (= O) NR9R10, -C (= O) R11, -S (O) nNR9R10, -S ( O) n-R11, -C6-15 -aryloxy and 5-15 membered heteroaryloxy, wherein said alkyl, alkenyl and alkynyl are optionally and independently substituted with one to six fluorine atoms or with one to two substituents independently selected from -alkoxy, or with a hydroxy group; R9 and R10 are selected in each instance independently of -H, -C1-12 alkyl, -C2-12 alkenyl, -C2-12 alkynyl, -CF3, -C (= O) R11, - S (O) n-R11 , -C (= O) OR, C (= O) NR11R12, -S (O) n-NR11R12, - (C0-4 alkylene) - (cycloalkyl), - (C0-4 alkylene) - (cycloalkenyl), - (C0-4 alkylene) - (bi- or C5-11 tricycloalkyl), - (C0-4 alkylene) - (bi- or C7-11 tricycloalkenyl), - (C0-4 alkylene) - (5-10 membered heterocycloalkyl) ), - (C0-4 alkylene) - (C6-10 aryl) and - (C0-4 alkylene) - (5-10 membered heteroaryl), wherein said alkyl, alkenyl and alkynyl are optionally and independently substituted with each other. six fluorine atoms or with one to two substituents independently selected from -C 1-4 alkoxy, or with a hydroxy group, and wherein said cycloalkyl, cycloalkenyl, bi- or tricycloalkyl, bi- or tricycloalkenyl, heterocycloalkyl, aryl and heteroaryl are substituted optionally and independently with one to three substituents independently selected from -OH, -C1-12 alkyl, -alq C2-12 uenyl, -C2-12 alkynyl, -C1-6 alkoxy, -C2-6 alkenoxy, -C2-6 alkyloxy, C1-6 hydroxyalkyl, -F, -Cl, -Br, - I, -CN, -NO2, -CF3, -NH2, -C (= O) NH2, -S (O) n-NH2, -C (= O) H and -C (= O) OH, wherein said alkyl, alkenyl and substituents alkynyl is further optionally and independently substituted with one to six fluorine atoms or with one to two substituents independently selected from -C 1-4 alkoxy, or with a hydroxy group; or NR9R10 can optionally and independently form a four to ten membered heterocycloalkyl moiety, said heterocycloalkyl moiety containing one or two additional heteroatoms independently selected from N, O and S, and optionally containing from one to three double bonds, wherein the Carbon atoms of the NR9R10 heterocycloalkyl moiety are optionally and independently substituted with one to three substituents independently selected from -OH, -C1-12 alkyl, -C2-12 alkenyl, -C2-12 alkynyl, -C1-6 alkoxy, -alkenoxy C2-6, -C2-6alkyloxy, -F, -Cl, -Br, -I, -CF3, -NH2, -C (= O) NH2, -S (O) n-NH2, -C (= O ) R11, - S (O) n-R11, (C0-4 alkylene) - (C6-10 aryl), (C0-4 alkylene) - (5 to 10 membered heteroaryl), (C0-4 alkylene) - ( C6-10 cycloalkyl) and (C0-4 alkylene) - (5-10 membered heterocycloalkyl), and wherein the substituent (C0-4 alkylene) - (5-10 membered heterocycloalkyl) and the nitrogen atoms of said moiety heterocycloalkyl of NR9R10 are independently and optionally substituted with a substituent independently selected from -C12-12 alkyl, -C2-12 alkenyl, -C2-12 alkynyl, -C (= O) NH2, -S (O) n-NH2, -C (= O) R11, -S (O) n-R11, (C0-4 alkylene) - (C6-10 aryl), (C0-4 alkylene) - (5-10 membered heteroaryl), (C0-4 alkylene ) - (C6-10 cycloalkyl) and (C0-4 alkylene) - (5-10 membered heterocycloalkyl), and wherein said alkyl, alkenyl and alkynyl substituents are optionally and independently substituted in addition to one to six fluorine atoms, or with one to two substituents independently selected from -C 1-4 alkoxy, or with a hydroxy group; R11 and R12 are independently selected in each instance from C1-15 alkyl (straight or branched chain), C2-6 alkenyl, C2-6 alkynyl, (C0-4 alkylene) - (C3-15 cycloalkyl), (alkylene C0-4) - (C4-8 cycloalkenyl), (C0-4 alkylene) - (C5-11 tricycloalkyl), (C0-4 alkylene) - (C7-11 tricycloalkenyl), (C0- alkylene 4) - (5-15 membered heterocycloalkyl), (C0-4 alkylene) - (C6-15 aryl) and (C0-4 alkylene) - (5-15 membered heteroaryl); wherein R11 and R12 are optionally and independently substituted with one to three substituents independently selected from the group R1b, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bi- or tricycloalkyl, bi- or tricycloalkenyl, heterocycloalkyl, aryl and heteroaryl, are each optionally and independently substituted with one to three substituents independently selected from -OH, -C1-12 alkyl, -C2-12 alkenyl, -C2-12 alkynyl, -C1-6 alkoxy, -C2-6 alkenoxy, -alkyloxy C2-6, -C1-6 hydroxyalkyl, -F, -Cl, -Br, -I, -CN, -NO2, -CF3, -NH2, -NH (C1-6 alkyl), -N (C1-6 alkyl ) 2, -C (= O) NH (C1-6 alkyl), -C (= O) N (C1-6 alkyl) 2, -NR9R10, -C (= O) NR9R10, -C (= O) R11 , -S (O) n-NR9R10, -S (O) n-R11, C6-15 aryloxy and 5-15 membered heteroaryloxy, -S (O) 2NH2, -S (O) NH (C1-6 alkyl) , -S (O) N (C1-6 alkyl) 2, -C (= O) H, -C (= O) OH and -C (= O) O (C1-6 alkyl) wherein said alkyl, alkenyl , alkynyl, cycloalkyl and cycloalkenyl are optional ndependently substituted by one to six fluorine atoms, or with one to two substituents independently selected from -C 1-4 alkoxy, or with a hydroxy group; NR11R12 can optionally independently form a four to ten membered heterocycloalkyl moiety, said heterocycloalkyl moiety containing one or two additional atoms independently selected from N, O and S, and optionally containing one to three double bonds, wherein the atoms Carbon of the heterocycloalkyl moiety of NR9R10 are optionally and independently substituted with one to three substituents independently selected from -OH, -C1-12 alkyl, -C2-12 alkenyl, -C2-12 alkynyl, -C1-6 alkoxy, -C2 alkenoxy -6, -C2-6alkyloxy, -C1-6 hydroxyalkyl, -F, -Cl, -Br, -I, -CN, -NO2, -CF3, -NH2, -NH (C1-6 alkyl), -N (C1-6 alkyl) 2, -C (= O) NH2, -C (= O) NH (C1-6 alkyl), -C (= O) N (C1-6 alkyl) 2, -S (O) 2NH2, -S (O) NH (C1-6 alkyl), -S (O) N (C1-6 alkyl) 2, -C (= O) H, - C (= O) OH and -C (= O ) O (C1-6 alkyl) wherein said alkyl, alkenyl, alkynyl, cycloalkyl and cycloalkenyl are optionally and independently substituted by each other. s fluorine atoms, or with one to two substituents independently selected from -C 1-4 alkoxy, or with a hydroxy group; R2 is selected from -H, -OH, -NH2, -CH2OH, -OC (= O) CH3, -C (CH3) 2OH, - (CH3) (CH2CH3) (OH), -C (OH) ( C0-4 alkyl) (C0-4 alkyl), -OC (= O) R4 and -OC (= O) OR4, wherein said -OC (= O) R4 and -OC (= O) OR4 may optionally be a prodrug of the corresponding OH of R2; R4 is selected from -C1-4 alkyl, -CH (OH) (C1-4 alkyl), -CH (OH) (C5-6 aryl), -CH (OH) (5-6 membered heteroaryl), -CH (OH) (C5-6 cycloalkyl), -CH (OH) (5-6 membered heterocycloalkyl); R3 is selected from -C1-6 alkyl, -C2-6 alkenyl, -C2-6 alkynyl and - (C0-4 alkylene) - (C3-6 cycloalkyl), wherein when R3 is alkyl, alkenyl, allyl, or alkynyl , R3 is optionally and independently substituted with a substituent independently selected from -C 1-4 alkoxy, -OH and -S (C 1-4 alkyl); R5 is selected from -H, -C1-4alkyl, -C2-4alkenyl, -C2-4alkyl, -C (= O) (C1-4alkyl), -C6-10 -aryl, -5-20 heteroaryl members, -S (O) n- (C6-10 aryl), -S (O) n- (5-20 member heteroaryl), -S (O) n-CH2- (C6-20 aryl) and -S (O) n-CH2- (5-20 membered heteroaryl); R6 is selected from -H, -C1-4alkyl, -C2-4alkenyl, -C2-4alkynyl, -F, -Cl, -Br, -I, -CN, -CF3, -C (= O) NR9R10 , -S (O) n-NR9R10, - C (= O) R11, -S (O) n-R11, -C (= O) OR12, - (alkylene C0-4) -C (= O) OR12, -C3-20 cycloalkyl, -C4-20 -cycloalkenyl and -C6-10 -aryl, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl and aryl are optionally and independently substituted with one to three substituents independently selected from the group R1b; R7 is selected from -H, -C1-20 alkyl, -C2-20 alkenyl, -C2-20 alkynyl, -C1-20 alkoxy, -C2-20 alkenoxy, -C2-20 alkynoxy, -F, -Cl, - Br, -I, -CN, -NO2, -CF3, -NR9R10, -C (= O) NR9R10, -C (= O) R11, -C (= O) OR12, C3-15 cycloalkyl, C0-4 alkylene -C3-20 cycloalkyl, 3-15 membered heterocycloalkyl, C6-15 aryl, 5-15 membered heteroaryl, -CHO, C0-4 alkylene-C3-20 cycloalkyl, C0-4 alkylene-C4-20 alkylene, C0 alkylene -4- (B10- or C10-20 tricycloalkyl), C0-4 alkylene C10-20 cycloalkenyl, C0-4 alkyl 3- to 20 membered heterocycloalkyl, alkyl |
| priorityDate | 2003-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 32.