JP2017512803A5 - - Google Patents

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Publication number: JP2017512803A5
Authority: JP; Japan
Prior art keywords: alkyl; alkoxy; hydroxy; halo; cycloalkyl
Prior art date: 2015-03-18
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

JP2016559879A

Other languages

English (en)

Japanese (ja)

Other versions

JP2017512803A (ja

JP6643247B2 (ja

Filing date

2015-03-18

Publication date

2018-04-26

2015-03-18 Application filed filed Critical

2015-03-18 Priority claimed from PCT/IB2015/051988 external-priority patent/WO2015150957A1/en

2017-05-25 Publication of JP2017512803A publication Critical patent/JP2017512803A/ja

2018-04-26 Publication of JP2017512803A5 publication Critical patent/JP2017512803A5/ja

2020-02-12 Application granted granted Critical

2020-02-12 Publication of JP6643247B2 publication Critical patent/JP6643247B2/ja

Status Expired - Fee Related legal-status Critical Current

2035-03-18 Anticipated expiration legal-status Critical

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125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 80
125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 48
229910052736 halogen Inorganic materials 0.000 claims 38
150000002367 halogens Chemical class 0.000 claims 37
125000002887 hydroxy group Chemical group [H]O* 0.000 claims 34
125000001424 substituent group Chemical group 0.000 claims 29
229910052799 carbon Inorganic materials 0.000 claims 26
229910052739 hydrogen Inorganic materials 0.000 claims 26
239000001257 hydrogen Substances 0.000 claims 26
125000000592 heterocycloalkyl group Chemical group 0.000 claims 25
125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 24
125000000217 alkyl group Chemical group 0.000 claims 23
150000001721 carbon Chemical group 0.000 claims 21
125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 20
125000001153 fluoro group Chemical group F* 0.000 claims 19
150000002431 hydrogen Chemical class 0.000 claims 19
150000001875 compounds Chemical class 0.000 claims 18
-1 cyano, hydroxy Chemical group 0.000 claims 18
150000003839 salts Chemical class 0.000 claims 18
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 17
125000000753 cycloalkyl group Chemical group 0.000 claims 14
125000003545 alkoxy group Chemical group 0.000 claims 13
125000001072 heteroaryl group Chemical group 0.000 claims 12
125000004093 cyano group Chemical group *C#N 0.000 claims 11
125000005843 halogen group Chemical group 0.000 claims 10
125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 7
125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 6
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
125000002883 imidazolyl group Chemical group 0.000 claims 6
125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 4
125000005842 heteroatom Chemical group 0.000 claims 4
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
238000006467 substitution reaction Methods 0.000 claims 4
125000004205 trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 4
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
125000001309 chloro group Chemical group Cl* 0.000 claims 3
229910052760 oxygen Chemical group 0.000 claims 3
239000001301 oxygen Chemical group 0.000 claims 3
125000004430 oxygen atom Chemical group O* 0.000 claims 3
239000008194 pharmaceutical composition Substances 0.000 claims 3
125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
125000004432 carbon atom Chemical group C* 0.000 claims 2
125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
125000006006 difluoroethoxy group Chemical group 0.000 claims 2
125000006005 fluoroethoxy group Chemical group 0.000 claims 2
125000004785 fluoromethoxy group Chemical group [H]C([H])(F)O* 0.000 claims 2
125000002541 furyl group Chemical group 0.000 claims 2
125000001786 isothiazolyl group Chemical group 0.000 claims 2
125000000842 isoxazolyl group Chemical group 0.000 claims 2
125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
125000002971 oxazolyl group Chemical group 0.000 claims 2
125000003566 oxetanyl group Chemical group 0.000 claims 2
125000003226 pyrazolyl group Chemical group 0.000 claims 2
125000000335 thiazolyl group Chemical group 0.000 claims 2
125000001544 thienyl group Chemical group 0.000 claims 2
125000001425 triazolyl group Chemical group 0.000 claims 2
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
SIQJUJBSEDNWPI-UHFFFAOYSA-N CC1(OC2=CC=C(C=C2C(=C1)CN1C(C=2N(CC1)C(C(=CC2)N2C=NC(=C2)C)=O)=O)C(F)(F)F)C Chemical compound CC1(OC2=CC=C(C=C2C(=C1)CN1C(C=2N(CC1)C(C(=CC2)N2C=NC(=C2)C)=O)=O)C(F)(F)F)C SIQJUJBSEDNWPI-UHFFFAOYSA-N 0.000 claims 1
NGCLDKLLCXHWGU-UHFFFAOYSA-N CC1(OC2=CC=C(C=C2C(=C1)CN1C(C=2N(CC1)C(C(=CC2)N2C=NC(=C2)C)=O)=O)OC(F)(F)F)C Chemical compound CC1(OC2=CC=C(C=C2C(=C1)CN1C(C=2N(CC1)C(C(=CC2)N2C=NC(=C2)C)=O)=O)OC(F)(F)F)C NGCLDKLLCXHWGU-UHFFFAOYSA-N 0.000 claims 1
OXAMLWSJBGIHNL-INIZCTEOSA-N CC1(OC2=CC=C(C=C2C(=C1)[C@H](C)N1C(C=2N(CC1)C(C(=CC2)N2C=NC(=C2)C)=O)=O)C(F)(F)F)C Chemical compound CC1(OC2=CC=C(C=C2C(=C1)[C@H](C)N1C(C=2N(CC1)C(C(=CC2)N2C=NC(=C2)C)=O)=O)C(F)(F)F)C OXAMLWSJBGIHNL-INIZCTEOSA-N 0.000 claims 1
LHTSLMHEFKNOOX-PXDATVDWSA-N CC1(OC=2C=CC(=CC2[C@]2([C@@H]1C2)CN2C(C=1N(CC2)C(C(=CC1)N1C=NC(=C1)C)=O)=O)C(F)(F)F)C Chemical compound CC1(OC=2C=CC(=CC2[C@]2([C@@H]1C2)CN2C(C=1N(CC2)C(C(=CC1)N1C=NC(=C1)C)=O)=O)C(F)(F)F)C LHTSLMHEFKNOOX-PXDATVDWSA-N 0.000 claims 1
ORLKJYBPSXUASX-PXDATVDWSA-N CC1(OC=2C=CC(=CC2[C@]2([C@@H]1C2)CN2C(C=1N(CC2)C(C(=CC1)N1C=NC(=C1)C)=O)=O)OC(F)(F)F)C Chemical compound CC1(OC=2C=CC(=CC2[C@]2([C@@H]1C2)CN2C(C=1N(CC2)C(C(=CC1)N1C=NC(=C1)C)=O)=O)OC(F)(F)F)C ORLKJYBPSXUASX-PXDATVDWSA-N 0.000 claims 1
MLZHNNLTXCDNLL-AVRWGWEMSA-N CC=1N=CN(C1)C1=CC=C2N(CCN(C2=O)C[C@]23[C@H](COC=4C=CC(=CC24)C2(CC2)C(F)(F)F)C3)C1=O Chemical compound CC=1N=CN(C1)C1=CC=C2N(CCN(C2=O)C[C@]23[C@H](COC=4C=CC(=CC24)C2(CC2)C(F)(F)F)C3)C1=O MLZHNNLTXCDNLL-AVRWGWEMSA-N 0.000 claims 1
FRPPYXDKNYDZHE-CMJOXMDJSA-N ClC1=CC(=CC=2[C@]3([C@@H](COC12)C3)CN3C(C=1N(CC3)C(C(=CC1)N1C=NC(=C1)C)=O)=O)C(F)(F)F Chemical compound ClC1=CC(=CC=2[C@]3([C@@H](COC12)C3)CN3C(C=1N(CC3)C(C(=CC1)N1C=NC(=C1)C)=O)=O)C(F)(F)F FRPPYXDKNYDZHE-CMJOXMDJSA-N 0.000 claims 1
MZPMUGOGQIVILU-UHFFFAOYSA-N ClC=1C=C2C(=CC(OC2=C(C1)F)(C)C)CN1C(C=2N(CC1)C(C(=CC2)N2C=NC(=C2)C)=O)=O Chemical compound ClC=1C=C2C(=CC(OC2=C(C1)F)(C)C)CN1C(C=2N(CC1)C(C(=CC2)N2C=NC(=C2)C)=O)=O MZPMUGOGQIVILU-UHFFFAOYSA-N 0.000 claims 1
LCNNBFCDMJIFBF-CPJLOUKISA-N FC(C)(OC1=CC=2[C@]3([C@@H](COC2C=C1)C3)CN3C(C=1N(CC3)C(C(=CC1)N1C=NC(=C1)C)=O)=O)F Chemical compound FC(C)(OC1=CC=2[C@]3([C@@H](COC2C=C1)C3)CN3C(C=1N(CC3)C(C(=CC1)N1C=NC(=C1)C)=O)=O)F LCNNBFCDMJIFBF-CPJLOUKISA-N 0.000 claims 1
201000010099 disease Diseases 0.000 claims 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
239000000546 pharmaceutical excipient Substances 0.000 claims 1
125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1

JP2016559879A 2014-04-01 2015-03-18 ガンマセクレターゼモジュレーターとしてのクロメンおよび１，１ａ，２，７Ｂ−テトラヒドロシクロプロパ［Ｃ］クロメンピリドピラジンジオン Expired - Fee Related JP6643247B2 (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US201461973436P	2014-04-01	2014-04-01
US61/973,436		2014-04-01
PCT/IB2015/051988 WO2015150957A1 (en)	2014-04-01	2015-03-18	Chromene and 1,1 a,2,7b-tetrahydrocyclopropa[c]chromene pyridopyrazinediones as gamma-secretase modulators

Publications (3)

Publication Number	Publication Date
JP2017512803A JP2017512803A (ja)	2017-05-25
JP2017512803A5 true JP2017512803A5 (2)	2018-04-26
JP6643247B2 JP6643247B2 (ja)	2020-02-12

Family

ID=52815058

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2016559879A Expired - Fee Related JP6643247B2 (ja)	2014-04-01	2015-03-18	ガンマセクレターゼモジュレーターとしてのクロメンおよび１，１ａ，２，７Ｂ−テトラヒドロシクロプロパ［Ｃ］クロメンピリドピラジンジオン

Country Status (29)

Country	Link
US (2)	US20150274721A1 (2)
EP (1)	EP3126361B1 (2)
JP (1)	JP6643247B2 (2)
KR (1)	KR101886945B1 (2)
CN (1)	CN106211770B (2)
AP (1)	AP2016009465A0 (2)
AR (1)	AR099874A1 (2)
AU (1)	AU2015242330B2 (2)
BR (1)	BR112016022519A8 (2)
CA (1)	CA2944308A1 (2)
CL (1)	CL2016002422A1 (2)
CR (1)	CR20160454A (2)
CU (1)	CU20160140A7 (2)
DK (1)	DK3126361T3 (2)
DO (1)	DOP2016000266A (2)
EA (1)	EA031419B1 (2)
EC (1)	ECSP16078289A (2)
ES (1)	ES2759277T3 (2)
IL (1)	IL248154B (2)
MD (1)	MD20160102A2 (2)
MX (1)	MX369074B (2)
NI (1)	NI201600149A (2)
PE (1)	PE20161364A1 (2)
PH (1)	PH12016501864A1 (2)
SG (1)	SG11201607465UA (2)
TW (1)	TWI568733B (2)
UY (1)	UY36054A (2)
WO (1)	WO2015150957A1 (2)
ZA (1)	ZA201606252B (2)

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2015
- 2015-03-18 AP AP2016009465A patent/AP2016009465A0/en unknown
- 2015-03-18 AU AU2015242330A patent/AU2015242330B2/en not_active Ceased
- 2015-03-18 DK DK15714951.9T patent/DK3126361T3/da active
- 2015-03-18 JP JP2016559879A patent/JP6643247B2/ja not_active Expired - Fee Related
- 2015-03-18 CR CR20160454A patent/CR20160454A/es unknown
- 2015-03-18 KR KR1020167030135A patent/KR101886945B1/ko not_active Expired - Fee Related
- 2015-03-18 SG SG11201607465UA patent/SG11201607465UA/en unknown
- 2015-03-18 MD MDA20160102A patent/MD20160102A2/ro not_active Application Discontinuation
- 2015-03-18 BR BR112016022519A patent/BR112016022519A8/pt not_active IP Right Cessation
- 2015-03-18 ES ES15714951T patent/ES2759277T3/es active Active
- 2015-03-18 CN CN201580018466.7A patent/CN106211770B/zh not_active Expired - Fee Related
- 2015-03-18 PE PE2016001895A patent/PE20161364A1/es not_active Application Discontinuation
- 2015-03-18 EA EA201600619A patent/EA031419B1/ru not_active IP Right Cessation
- 2015-03-18 EP EP15714951.9A patent/EP3126361B1/en active Active
- 2015-03-18 WO PCT/IB2015/051988 patent/WO2015150957A1/en not_active Ceased
- 2015-03-18 MX MX2016012904A patent/MX369074B/es active IP Right Grant
- 2015-03-18 CA CA2944308A patent/CA2944308A1/en not_active Withdrawn
- 2015-03-27 AR ARP150100922A patent/AR099874A1/es unknown
- 2015-03-27 UY UY0001036054A patent/UY36054A/es not_active Application Discontinuation
- 2015-03-27 US US14/670,746 patent/US20150274721A1/en not_active Abandoned
- 2015-03-31 TW TW104110551A patent/TWI568733B/zh not_active IP Right Cessation
2016
- 2016-09-09 ZA ZA2016/06252A patent/ZA201606252B/en unknown
- 2016-09-22 CU CUP2016000140A patent/CU20160140A7/es unknown
- 2016-09-22 PH PH12016501864A patent/PH12016501864A1/en unknown
- 2016-09-27 CL CL2016002422A patent/CL2016002422A1/es unknown
- 2016-09-29 NI NI201600149A patent/NI201600149A/es unknown
- 2016-09-29 DO DO2016000266A patent/DOP2016000266A/es unknown
- 2016-09-29 IL IL248154A patent/IL248154B/en active IP Right Grant
- 2016-09-30 EC ECIEPI201678289A patent/ECSP16078289A/es unknown
2017
- 2017-02-24 US US15/441,882 patent/US20170166566A1/en not_active Abandoned

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