JP2016503785A5 - - Google Patents

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Publication number: JP2016503785A5
Authority: JP; Japan
Prior art keywords: tautomer; compound; fluoro; alkyl; pharmaceutically acceptable
Prior art date: 2013-12-04
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Granted

Application number

JP2015548807A

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English (en)

Japanese (ja)

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JP6162820B2 (ja

JP2016503785A (ja

Filing date

2013-12-04

Publication date

2016-10-13

2013-12-04 Application filed filed Critical

2013-12-04 Priority claimed from PCT/IB2013/060633 external-priority patent/WO2014097038A1/en

2016-02-08 Publication of JP2016503785A publication Critical patent/JP2016503785A/ja

2016-10-13 Publication of JP2016503785A5 publication Critical patent/JP2016503785A5/ja

2017-07-12 Application granted granted Critical

2017-07-12 Publication of JP6162820B2 publication Critical patent/JP6162820B2/ja

Status Expired - Fee Related legal-status Critical Current

2033-12-04 Anticipated expiration legal-status Critical

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150000001875 compounds Chemical class 0.000 claims 35
125000001153 fluoro group Chemical group F* 0.000 claims 18
150000003839 salts Chemical class 0.000 claims 18
125000000592 heterocycloalkyl group Chemical group 0.000 claims 11
125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 10
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
229910052739 hydrogen Inorganic materials 0.000 claims 8
239000001257 hydrogen Substances 0.000 claims 8
239000008194 pharmaceutical composition Substances 0.000 claims 6
125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 5
125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 5
150000002431 hydrogen Chemical group 0.000 claims 5
125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
QKFOHTNLZOIEHZ-UHFFFAOYSA-N 2h-1,3-thiazin-2-amine Chemical compound NC1SC=CC=N1 QKFOHTNLZOIEHZ-UHFFFAOYSA-N 0.000 claims 4
125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 3
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
125000000217 alkyl group Chemical group 0.000 claims 3
229910052736 halogen Inorganic materials 0.000 claims 3
150000002367 halogens Chemical class 0.000 claims 3
125000005842 heteroatom Chemical group 0.000 claims 3
230000004770 neurodegeneration Effects 0.000 claims 3
208000015122 neurodegenerative disease Diseases 0.000 claims 3
125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
125000003545 alkoxy group Chemical group 0.000 claims 2
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 2
206010012601 diabetes mellitus Diseases 0.000 claims 2
125000003566 oxetanyl group Chemical group 0.000 claims 2
125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
YUFWDCBIDOXDCY-VAHXTSCQSA-N (4ar,6r,8as)-6-cyclopropyl-8a-(2,4,6-trifluorophenyl)-4a,5,6,8-tetrahydro-4h-pyrano[3,4-d][1,3]thiazin-2-amine Chemical compound C1([C@@H]2OC[C@@]3(N=C(SC[C@@H]3C2)N)C=2C(=CC(F)=CC=2F)F)CC1 YUFWDCBIDOXDCY-VAHXTSCQSA-N 0.000 claims 1
RHJJDGACVHKXNA-JJMVLAAESA-N (4ar,6r,8as)-6-cyclopropyl-8a-(2,4-difluorophenyl)-4a,5,6,8-tetrahydro-4h-pyrano[3,4-d][1,3]thiazin-2-amine Chemical compound C1([C@@H]2OC[C@@]3(N=C(SC[C@@H]3C2)N)C=2C(=CC(F)=CC=2)F)CC1 RHJJDGACVHKXNA-JJMVLAAESA-N 0.000 claims 1
WAKCJWZQPHOJBN-JJMVLAAESA-N (4ar,6r,8as)-6-cyclopropyl-8a-(2,5-difluorophenyl)-4a,5,6,8-tetrahydro-4h-pyrano[3,4-d][1,3]thiazin-2-amine Chemical compound C1([C@@H]2OC[C@@]3(N=C(SC[C@@H]3C2)N)C=2C(=CC=C(F)C=2)F)CC1 WAKCJWZQPHOJBN-JJMVLAAESA-N 0.000 claims 1
CEUHNOFRRAIAQB-WNMQOVRZSA-N (4ar,6r,8as)-6-cyclopropyl-8a-(2,6-difluorophenyl)-4a,5,6,8-tetrahydro-4h-pyrano[3,4-d][1,3]thiazin-2-amine Chemical compound C1([C@@H]2OC[C@@]3(N=C(SC[C@@H]3C2)N)C=2C(=CC=CC=2F)F)CC1 CEUHNOFRRAIAQB-WNMQOVRZSA-N 0.000 claims 1
JRBPZKILTJVDPX-MJEQTWJJSA-N (4ar,6r,8as)-6-cyclopropyl-8a-(2-fluoro-4-methylphenyl)-4a,5,6,8-tetrahydro-4h-pyrano[3,4-d][1,3]thiazin-2-amine Chemical compound FC1=CC(C)=CC=C1[C@@]1(N=C(N)SC2)[C@H]2C[C@H](C2CC2)OC1 JRBPZKILTJVDPX-MJEQTWJJSA-N 0.000 claims 1
FHXGFQTXPUMEKT-PEYYIBSZSA-N (4ar,6r,8as)-6-cyclopropyl-8a-(2-fluorophenyl)-4a,5,6,8-tetrahydro-4h-pyrano[3,4-d][1,3]thiazin-2-amine Chemical compound C1([C@@H]2OC[C@@]3(N=C(SC[C@@H]3C2)N)C=2C(=CC=CC=2)F)CC1 FHXGFQTXPUMEKT-PEYYIBSZSA-N 0.000 claims 1
FTTYFEBEIFPZEG-JGGQBBKZSA-N (4ar,6r,8as)-6-cyclopropyl-8a-(4-fluorophenyl)-4a,5,6,8-tetrahydro-4h-pyrano[3,4-d][1,3]thiazin-2-amine Chemical compound C1([C@@H]2OC[C@@]3(N=C(SC[C@@H]3C2)N)C=2C=CC(F)=CC=2)CC1 FTTYFEBEIFPZEG-JGGQBBKZSA-N 0.000 claims 1
DXFOXQOXOOZOFO-SQWLQELKSA-N (4ar,6r,8as)-6-cyclopropyl-8a-phenyl-4a,5,6,8-tetrahydro-4h-pyrano[3,4-d][1,3]thiazin-2-amine Chemical compound C1([C@@H]2OC[C@@]3(N=C(SC[C@@H]3C2)N)C=2C=CC=CC=2)CC1 DXFOXQOXOOZOFO-SQWLQELKSA-N 0.000 claims 1
HENOYKTZLIYYIJ-URNHKWKMSA-N (4r,4ar,6r,8as)-6-cyclopropyl-8a-(2,4-difluorophenyl)-4-methyl-4a,5,6,8-tetrahydro-4h-pyrano[3,4-d][1,3]thiazin-2-amine Chemical compound C1([C@@H]2OC[C@@]3(N=C(N)S[C@@H]([C@@H]3C2)C)C=2C(=CC(F)=CC=2)F)CC1 HENOYKTZLIYYIJ-URNHKWKMSA-N 0.000 claims 1
ZOKDMAYUPFRZKD-DPAVQSFQSA-N (4s,4ar,6r,8as)-6-cyclopropyl-8a-(2,4-difluorophenyl)-4-(fluoromethyl)-4a,5,6,8-tetrahydro-4h-pyrano[3,4-d][1,3]thiazin-2-amine Chemical compound C1([C@@H]2OC[C@@]3(N=C(S[C@H](CF)[C@@H]3C2)N)C=2C(=CC(F)=CC=2)F)CC1 ZOKDMAYUPFRZKD-DPAVQSFQSA-N 0.000 claims 1
125000006432 1-methyl cyclopropyl group Chemical group [H]C([H])([H])C1(*)C([H])([H])C1([H])[H] 0.000 claims 1
-1 3-fluoro-4-methylphenyl Chemical group 0.000 claims 1
208000024827 Alzheimer disease Diseases 0.000 claims 1
102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
102100021257 Beta-secretase 1 Human genes 0.000 claims 1
102100021277 Beta-secretase 2 Human genes 0.000 claims 1
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 claims 1
101000894883 Homo sapiens Beta-secretase 2 Proteins 0.000 claims 1
208000008589 Obesity Diseases 0.000 claims 1
239000000654 additive Substances 0.000 claims 1
230000000996 additive effect Effects 0.000 claims 1
229910052799 carbon Inorganic materials 0.000 claims 1
125000004093 cyano group Chemical group *C#N 0.000 claims 1
125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 1
208000037765 diseases and disorders Diseases 0.000 claims 1
239000003814 drug Substances 0.000 claims 1
230000000694 effects Effects 0.000 claims 1
230000002401 inhibitory effect Effects 0.000 claims 1
125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
235000020824 obesity Nutrition 0.000 claims 1
125000004274 oxetan-2-yl group Chemical group [H]C1([H])OC([H])(*)C1([H])[H] 0.000 claims 1
238000011321 prophylaxis Methods 0.000 claims 1
125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
230000001225 therapeutic effect Effects 0.000 claims 1
238000011282 treatment Methods 0.000 claims 1
208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1

JP2015548807A 2012-12-19 2013-12-04 炭素環式および複素環式置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物 Expired - Fee Related JP6162820B2 (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US201261739053P	2012-12-19	2012-12-19
US61/739,053		2012-12-19
PCT/IB2013/060633 WO2014097038A1 (en)	2012-12-19	2013-12-04	CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS

Publications (3)

Publication Number	Publication Date
JP2016503785A JP2016503785A (ja)	2016-02-08
JP2016503785A5 true JP2016503785A5 (2)	2016-10-13
JP6162820B2 JP6162820B2 (ja)	2017-07-12

Family

ID=49917680

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2015548807A Expired - Fee Related JP6162820B2 (ja)	2012-12-19	2013-12-04	炭素環式および複素環式置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物

Country Status (5)

Country	Link
US (1)	US9403846B2 (2)
EP (1)	EP2935282A1 (2)
JP (1)	JP6162820B2 (2)
CA (1)	CA2893333C (2)
WO (1)	WO2014097038A1 (2)

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