http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2377988-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_938a6d7a15cbc93a74abe1953eb25d47 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-505 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-06 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-04 |
| filingDate | 2006-11-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2012-04-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb4d67e6d399d32ef6d36c1231b1ff73 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_998f5ca64d71a39a00b7381bc0c4cf6e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_04e2d2317d9dabf401eff48a79d07285 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_40686618e7487ab7ff21bd31617f17c4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1345f8ec5d99512587be79ab69367bd1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_df6f5f2196b90184f099597f2603f4c5 |
| publicationDate | 2012-04-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2377988-T3 |
| titleOfInvention | Quinazolines useful as voltage controlled ion channel modulators |
| abstract | A compound of formula IA or formula IB: or a pharmaceutically acceptable salt thereof, wherein: z is 0-3; RYZ is a C1-C6 aliphatic group, optionally substituted with w4 independent occurrences of -R14, in which w4 is 0-3; in which up to two methylene units in RYZ are optionally replaced by -NR-, -O-, -COO, -OCO-, - NRCO-, -CONR-, -SO2NR-, or -NRSO2-; x e y are each independently 0-4; 10 W is halogen, -ORXY, -CHF2-, or -CF3; in which: each of WA, WB. WC, and WD is independently 0 or 1; each M is independently selected from hydrogen, Li, Na, K, Mg, Ca, Ba, -N (R7) 4, -C1-C12-alkyl, -C2-C12-alkenyl-, or -R6; wherein 1 to 4 -CH2 radicals of the alkyl or alkenyl group, other than -CH2 that is attached to Z, are optionally replaced by a heteroatom group selected from O, S, S (O), S (O2), or N (R7); and wherein any hydrogen in said alkyl, alkenyl or R6 is optionally replaced by a substituent selected from oxo, -OR7, -R7, -N (R7) 2, -N (R7) 3, -R7OH, -CN, - CO2 R7, -C (O) -N (R7) 2, -S (O) 2-N (R7) 2, -N (R7) -C (O) -R7, -C (O) R7, -S (O) n-R7, -OCF3, -S (O) n-R6, -N (R7) -S (O) 2 (R7), halogen, -CF3, or -NO2; n is 0-2; M 'is H, -C1-C12-alkyl, -C2-C12-alkenyl, or -R6; wherein 1 to 4 -CH2 radicals of the alkyl or alkenyl group are optionally replaced by a heteroatom group selected from O, S, S (O), S (O2), or N (R7); and wherein any hydrogen in said alkyl, alkenyl or R6 is optionally replaced by a substituent selected from oxo, -OR7, -R7, -N (R7) 2, -N (R7) 3, -R7OH, -CN, - CO2 R7, -C (O) -N (R7) 2, -S (O) 2-N (R7) 2, -N (R7) -C (O) -R7 C (O) R7, -S (O ) n-R7, -OCF3, -S (O) n-R6, -N (R7) -S (O) 2 (R7), halogen, -CF3, or -NO2; Z is -CH2-, -O-, -S-, N (R7) 2-; or, when M is absent, then Z is hydrogen, = O, or = S; Y is P or S, in which when Y is S, then Z is not S; 83 X is O or S; each R7 is independently selected from hydrogen, or a C1-C4 aliphatic group, optionally substituted with up to two Q1; each Q1 is independently selected from a system of unsaturated, partially saturated or saturated 3-7 membered carbocyclic rings; or an unsaturated, partially saturated or saturated 5-7 membered heterocyclic ring containing one or more heteroatoms or heteroatom groups selected from O, N, NH, S, SO, or SO2; wherein Q1 is optionally substituted with up to three substituents selected from oxo, -OH, O (C1-C4 aliphatic group), -C1-C4 aliphatic group, -NH2, -NH (C1-C4 aliphatic group), -N ( C1-C4 aliphatic group) 2, -N (C1-C4 aliphatic group) -C (O) - (C1-C4 aliphatic group), - (C1-C4 aliphatic group) -OH, -CN, -CO2H-, - CO2 (C1-C4 aliphatic group), C (O) -NH2, -C (O) -NH (C1-C4 aliphatic group), -C (O) -N (C1-C4 aliphatic group) 2, halogen, or -CF3; R6 is an unsaturated, partially saturated or saturated 5-6 membered heterocyclic or carbocyclic ring system, or an unsaturated, partially saturated or saturated 8-10 membered bicyclic ring system; wherein any one of said heterocyclic ring systems contains one or more heteroatoms selected from O, N, S, S (O) n, or N (R7); and wherein any of said ring systems optionally contains 1 to 4 substituents independently selected from OH, -C1-C4 alkyl, -O-C1-C4 alkyl, or -O-C (O) -C1-C4 alkyl; R9 is C (R7) 2, O, or N (R7); Each occurrence of R14, R3, R4, and R5 is independently Q-RX; wherein Q is a bond or is a C1-C6 alkylidene chain in which up to two non-adjacent methylene units of Q are optionally and independently replaced by -NR-, -S-, -O-, -CS-, -CO2 -, -OCO-, -CO-, -COCO-, -CONR-, -NRCO-, -NRCO2-, -SO2NR-, -NRSO2-, -CONRNR-, -NRCONR-, -OCONR-, -NRNR-, -NRSO2NR - SO-, -SO2-, -PO-, -PO2-, -OP (O) (OR) -, or -POR; and each occurrence of RX is independently selected from -R ', halogen, = NR', -NO2, -CN, -OR ', -SR', -N (R ') 2, -NR'COR', -NR ' WITH (R ') 2, -NR'CO2R', -COR ', -CO2R', -OCOR ', -CON (R') 2, -OCON (R ') 2, -SOR', -SO2R ', - SO2N (R ') 2NR'SO2R', -NR'SO2N (R ') 2, -COCOR', -COCH2COR ', -OP (O) (OR') 2, -P (O) (OR ') 2, -OP (O) 2OR ', -P (O) 2OR', -PO (R ') 2, or -OPO (R') 2; and each occurrence of R is independently hydrogen or a C1-C6 aliphatic group having up to three substituents; and each occurrence of R 'is independently hydrogen or a C1-C6 aliphatic group, a fully unsaturated, partially unsaturated or saturated 3-8 membered monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a fully unsaturated, partially unsaturated or saturated 8-12 membered bicyclic ring system having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur, in which R 'has up to four substituents; or R and R ', two occurrences of R, or two occurrences of R', are taken in conjunction with the atom or atoms to which they are attached to form a fully unsaturated, partially unsaturated or saturated 3-12 membered monocyclic or bicyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; with the proviso that the following compounds are excluded: [(3R) -1- [2- (2-hydroxyphenyl) -7-methyl-4-quinazolinyl] -3-pyrrolidinyl] carbamic acid phenylmethyl ester; [(3R) -1- [2- (2-hydroxyphenyl) -7-methyl-4-quinazolinyl] -3-pyrrolidinyl] carbamic acid phenylmethyl monohydrochloride; 1 (1S) -1- [2- (2-hydroxyphenyl) -7-methyl-4-quinazolinyl] -3-pyrrolidinyl] carbamic acid 1,1-dimethylethyl ester; 1,1 (1R) -1- [2- (2-hydroxyphenyl) -7-methyl-4-quinazolinyl] -3-pyrrolidinyl] carbamic acid 1,1-dimethylethyl ester; 1,1 (1R) -1- [6-fluoro-2- (2-hydroxyphenyl) -4-quinazolinyl] -3-pyrrolidinyl] carbamic acid 1,1-dimethylethyl ester; 1,1 (1R) -1- [2- (2-fluoro-6-hydroxyphenyl) -7-methyl-4-quinazolinyl] -3-pyrrolidinyl] carbamic acid 1,1-dimethylethyl ester; (salt) trifluoroacetate of the [(3R) -1- [2- (2-hydroxyphenyl) -7-methyl-4-quinazolinyl] -3-pyrrolidinyl] carbamic acid 3-pyridinylmethyl ester; (salt) trifluoroacetate of the [(3R) -1- [2- (2-hydroxyphenyl) -7-methyl-4-quinazolinyl] -3-pyrrolidinyl] carbamic acid 4-pyridinylmethyl ester; (salt) 1,3-benzodioxol-4-ylmethyl acid trifluoroacetate [(3R) -1- [2- (2-hydroxyphenyl) -7-methyl-4-quinazolinyl] -3-pyrrolidinyl] carbamic acid ester; (salt) [(3R) -1- [6-fluoro-2- (2-hydroxyphenyl) -4quinazolinyl] -3-pyrrolidinyl] carbamic acid trifluoroacetate ester (tetrahydro-2H-pyran-2-yl) methyl; and [(3R) -1- [2- (2-hydroxyphenyl) -7-methyl-4-quinazolinyl] -3-pyrrolidinyl] carbamic acid (tetrahydro-2H-pyran-2-yl) methyl ester. |
| priorityDate | 2005-11-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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