http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-095014-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0597f9c318d2aeca86db94711c516383 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5355 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-28 |
| filingDate | 2014-03-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9dc041f0e521f5b435200f935c27b286 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6b693887de00500624d76689f822b8a5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5f73f8f6da2d4744562f420efda57012 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0ec61ab4203a8aeb1bc225f3a3bdfa4e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_026dd51726f1281552d87383bf259672 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_df15a45b648a7a0bbfa9ebc9f599571a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1b6caecf57f22024cb87928c9760c2fd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e90af2206aaa94b68cef7ed1f5e15cee http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_862514ea343cdc524d216f65c2c25c91 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6317095905c5b7558fc22ff00973a1c2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ce63f011ce50b1d062be67feb1ecb394 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6365514ac3b2cdffea75d15042875860 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5178fe0114e561f69178800f4224c0dd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_32f254203b6f7858be071ea1e6ed0256 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3c724f643fc5d4a91916a6ed1115e465 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4d68fc4563d0f804907964414400d3c5 |
| publicationDate | 2015-09-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-095014-A1 |
| titleOfInvention | PERFORMED COMPOUNDS OF 5,6-DIHIDRO-4H-1,3-OXAZIN-2-AMINA AS B-SECRETASE INHIBITORS AND METHODS OF USE |
| abstract | Pharmaceutical compositions comprising the compounds, and the corresponding uses of the compounds and compositions for the treatment of disorders and / or conditions associated with the formation and deposition of plaque A-b resulting from the biological activity of BACE. Such BACE-mediated disorders include, for example, Alzheimer's disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions. Processes and methods useful for the preparation of the compounds described in the claims. Claim 1: A compound of formula (1), or a stereoisomer, tautomer, hydrate, solvate or pharmaceutically acceptable salt thereof, wherein A⁴ is CR⁴ or N; A⁵ is CR⁵ or N; A⁶ is CR⁶ or N; A⁸ is CR⁸ or N, as long as no more than two of A⁴, A⁵, A⁶ and A⁸ is N; one R¹ is C₁₋₃ haloalkyl and the other R¹ is H, F, Cl, C₁₋₆ alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, CN, -CH₂O-C₁₋₆ alkyl, -O-C₁₋₆ alkyl , -S (O) ₒ -C₁₋₆ alkyl, -NH-C₁₋₆ alkyl or -C (O) -C₁₋₆ alkyl, where each of C₁₋₆ alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl , and C₁₋₆ alkyl of -CH₂O-C₁₋₆ alkyl, -O-C₁₋₆ alkyl, -S (O) ₒ -C₁₋₆ alkyl, -NH-C₁₋₆ alkyl and -C (O) -alkyl C₁₋₆ are optionally substituted with 1-4 substituents of F, oxo or OH; alternatively, each R¹ considered together with the carbon atom to which they are attached form a spirocarbocyclic ring C₃₋₆ that optionally includes a heteroatom to be selected from O and N and optionally substituted with 1-4 atoms of F in carbon atoms and optionally substituted with a substituent to be selected from C₁₋₃ alkyl, CH₂O-C₁₋₂ alkyl or C halo haloalkyl in the nitrogen atom; each R², independently, is H, F, Cl, C₁₋₆ alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, CN, -CH₂O-C₁₋₆ alkyl, -O-C₁₋₆ alkyl, -S ( O) ₒ -C₁₋₆ alkyl, -NH-C₁₋₆ alkyl or -C (O) -C₁₋₆ alkyl, where each of C₁₋₆ alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, and C₁ alkyl ₋₆ of -CH₂O-C₁₋₆ alkyl, -O-C₁₋₆ alkyl, -S (O) ₒ -C₁₋₆ alkyl, -NH-C₁₋₆ alkyl and -C (O) -C₁₋₆ alkyl are optionally substituted with 1-4 substituents of F, oxo or OH; alternatively, each R² considered together with the carbon atom to which they are attached form a spirocarbocyclic ring C₃₋₆ that optionally includes a heteroatom to be selected from O and N and optionally substituted with 1-4 atoms of F in carbon atoms and optionally substituted with a substituent to be selected from C₁₋₃ alkyl, CH₂O-C₁₋₂ alkyl or C halo haloalkyl in the nitrogen atom; R³ is C₁₋₄ alkyl, CH₂O-C₁₋₄ alkyl, CH₂OH, C₁₋₄ haloalkyl or cyclopropyl, where each of C₁₋₄ alkyl, CH₂O-C₁₋₄ alkyl, C₁₋₄ haloalkyl and cyclopropyl is optionally substituted with 1-4 F atoms; each of R⁴, R⁵, R⁶ and R⁸, independently, is H, halo, haloalkyl, haloalkoxy, C₁₋₄ alkyl, CN, OH, O-C₁₋₄ alkyl, S (O) ₒ-C alquilo alkyl , NH-C₁₋₄ or C (O) -C₁₋₄ alkyl; R⁷ is -NH-R⁹, -NH-C (= O) -R⁹, -C (= O) NH-R⁹, -NH-C (= S) -R⁹, -O-R⁹ or -S-R⁹; R⁹ is acetyl, C₁₋₆ alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl or a monocyclic ring of 3, 4, 5, 6 or 7 members or bicyclic of 8, 9 or 10 members totally or partially unsaturated formed of atoms of carbon, wherein said ring optionally includes 1-4 heteroatoms if it is monocyclic or 1-5 heteroatoms if it is bicyclic, said heteroatoms to be selected from O, N or S, where C₁₋₆ alkyl, C₂₋₄ alkenyl, C₂ alkynyl ₋₄ and the ring are optionally substituted, independently, with 1-5 R¹⁰ substituents; and each R¹⁰, independently, is H, halo, haloalkyl, CN, OH, NO₂, NH₂, SF₅, acetyl, -C (O) NHCH₃, oxo, cyclopropylmethoxy, 2-propynyloxy, 2-butyloxy, C alquilo alkyl , C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl, C₁₋₆amino- alkyl, C₁₋₆amino dialkyl-, C₁₋₆ alkoxy, C₁₋₆ thioalkoxy, morpholinyl, pyrazolyl, isoxazolyl, dihydropyranyl, pyrrolyl, pyrrolidinyl, tetrahydropyrrolyl, piperazinyl, oxetan-3-yl, imidazo-pyridinyl or dioxolyl, where each of cyclopropylmethoxy, 2-butyloxy, C₁₋₆ alkyl, C₂₋₆ alkenyl, C alqu alkynyl, C₃₋₆ cycloalkyl, C₁₋₆amino alkyl -, Cquilamino dialkyl-, C alco alkoxy, C₁₋₆ thioalkoxy, morpholinyl, pyrazolyl, isoxazolyl, dihydropyranyl, pyrrolidinyl, oxetan-3-yl or dioxolyl, optionally substituted independently with 1-5 F substituents , Cl, CN, NO₂, NH₂, OH, oxo, CF₃, CHF₂, CH₂F, methyl or, methoxy, ethyl, ethoxy, CH₂CF₃, CH₂CHF₂, propyl, propoxy, isopropyl, isopropoxy, cyclopropyl, butyl, butoxy, cyclobutyl, isobutoxy, tert-butoxy, isobutyl, sec-butyl, tert-butyl, C-amino alkyl, dialkyl C₁₋₃amino, thioalkoxyl C₁₋₃ oxazolyl, or oxetan-3-yl; as long as, if A⁴ is CR⁴, A⁵ is CR⁵, A⁶ is CR⁶ and A⁸ is CR⁸, and each of R⁶ and R⁸, independently, is H, then R⁵ is not H. |
| priorityDate | 2013-03-01-04:00^^<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: 47.