JP2016500109A5 - - Google Patents
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- Publication number
- JP2016500109A5 JP2016500109A5 JP2015544141A JP2015544141A JP2016500109A5 JP 2016500109 A5 JP2016500109 A5 JP 2016500109A5 JP 2015544141 A JP2015544141 A JP 2015544141A JP 2015544141 A JP2015544141 A JP 2015544141A JP 2016500109 A5 JP2016500109 A5 JP 2016500109A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- dihydropyrimido
- indol
- oxazepin
- oxazepine
- Prior art date
- 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
Links
- VZJJHNNFKSSGBO-UHFFFAOYSA-N 6,7-dihydro-2h-oxazepin-5-one Chemical compound O=C1CCONC=C1 VZJJHNNFKSSGBO-UHFFFAOYSA-N 0.000 claims 74
- -1 1-propyl-1H-indol-5-yl Chemical group 0.000 claims 73
- 150000003839 salts Chemical class 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 3
- WXLCDTBTIVJDCE-UHFFFAOYSA-N 1,4-oxazepine Chemical compound O1C=CC=NC=C1 WXLCDTBTIVJDCE-UHFFFAOYSA-N 0.000 claims 3
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl 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
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000001113 thiadiazolyl 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
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 1
- QHXILXDHCYOAQA-UHFFFAOYSA-N 2h-1,4-oxazepin-5-one Chemical compound O=C1C=COCC=N1 QHXILXDHCYOAQA-UHFFFAOYSA-N 0.000 claims 1
- REVKWYWODJDFMM-UHFFFAOYSA-N 3-[5-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6-yl)indol-1-yl]propanoic acid Chemical compound O=C1C=2C(N)=NC=NC=2OCCN1C1=CC=C(N(CCC(O)=O)C=C2)C2=C1 REVKWYWODJDFMM-UHFFFAOYSA-N 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- VQCAQUBHKSWBLC-UHFFFAOYSA-N 4-amino-6-[1-[6-(2-hydroxypropan-2-yl)pyridin-3-yl]indol-5-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one Chemical compound C1=NC(C(C)(O)C)=CC=C1N1C2=CC=C(N3C(C4=C(N)N=CN=C4OCC3)=O)C=C2C=C1 VQCAQUBHKSWBLC-UHFFFAOYSA-N 0.000 claims 1
- 125000004938 5-pyridyl group Chemical group N1=CC=CC(=C1)* 0.000 claims 1
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- AIMMVWOEOZMVMS-UHFFFAOYSA-N cyclopropanecarboxamide Chemical compound NC(=O)C1CC1 AIMMVWOEOZMVMS-UHFFFAOYSA-N 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- SDWGLUQVAVEYSU-UHFFFAOYSA-N n-[5-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6-yl)-1-propan-2-ylindol-7-yl]cyclopropanecarboxamide Chemical compound C=12N(C(C)C)C=CC2=CC(N2C(C3=C(N)N=CN=C3OCC2)=O)=CC=1NC(=O)C1CC1 SDWGLUQVAVEYSU-UHFFFAOYSA-N 0.000 claims 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 0 CC(C)(C[n](ccc1c2)c1ccc2N(CCO1)C2=*C3N(C)C=NC1=C23)O Chemical compound CC(C)(C[n](ccc1c2)c1ccc2N(CCO1)C2=*C3N(C)C=NC1=C23)O 0.000 description 4
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN3593/DEL/2012 | 2012-11-23 | ||
| IN3593DE2012 | 2012-11-23 | ||
| IN750DE2013 | 2013-03-14 | ||
| IN750/DEL/2013 | 2013-03-14 | ||
| IN3172/DEL/2013 | 2013-10-25 | ||
| IN3172DE2013 | 2013-10-25 | ||
| PCT/US2013/071376 WO2014081994A1 (en) | 2012-11-23 | 2013-11-22 | Novel compounds as diacylglycerol acyltransferase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016500109A JP2016500109A (ja) | 2016-01-07 |
| JP2016500109A5 true JP2016500109A5 (enExample) | 2017-01-12 |
| JP6279600B2 JP6279600B2 (ja) | 2018-02-14 |
Family
ID=50776577
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015544141A Expired - Fee Related JP6279600B2 (ja) | 2012-11-23 | 2013-11-22 | ジアシルグリセロールアシルトランスフェラーゼ阻害剤としての新規化合物 |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US20150322082A1 (enExample) |
| EP (2) | EP3492474B1 (enExample) |
| JP (1) | JP6279600B2 (enExample) |
| KR (1) | KR102176463B1 (enExample) |
| CN (1) | CN104918620B (enExample) |
| AU (1) | AU2013347843B2 (enExample) |
| BR (1) | BR112015011982A8 (enExample) |
| CA (1) | CA2892304C (enExample) |
| CL (1) | CL2015001397A1 (enExample) |
| CY (1) | CY1121426T1 (enExample) |
| DK (1) | DK2922551T3 (enExample) |
| EA (1) | EA031114B1 (enExample) |
| ES (1) | ES2708626T3 (enExample) |
| HR (1) | HRP20190099T1 (enExample) |
| HU (1) | HUE042483T2 (enExample) |
| IL (1) | IL238835B (enExample) |
| LT (1) | LT2922551T (enExample) |
| ME (1) | ME03315B (enExample) |
| MX (1) | MX363484B (enExample) |
| NZ (1) | NZ630436A (enExample) |
| PE (1) | PE20150967A1 (enExample) |
| PH (1) | PH12015501109A1 (enExample) |
| PL (1) | PL2922551T3 (enExample) |
| PT (1) | PT2922551T (enExample) |
| RS (1) | RS58539B1 (enExample) |
| SG (1) | SG11201503761WA (enExample) |
| SI (1) | SI2922551T1 (enExample) |
| SM (1) | SMT201900230T1 (enExample) |
| UA (1) | UA115079C2 (enExample) |
| WO (1) | WO2014081994A1 (enExample) |
| ZA (1) | ZA201503304B (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018052818A (ja) * | 2015-01-28 | 2018-04-05 | 武田薬品工業株式会社 | スルホンアミド化合物 |
| MX2019005679A (es) | 2016-11-18 | 2019-08-14 | Merck Sharp & Dohme | Derivados de indol de utilidad como inhibidores de diacilglicerido o-aciltransferasa 2. |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100795462B1 (ko) * | 2006-09-27 | 2008-01-16 | 한국생명공학연구원 | 인돌 유도체, 이의 제조방법 및 이를 유효성분으로함유하는 대사성 질환 예방 및 치료용 약학적 조성물 |
| US20090036425A1 (en) * | 2007-08-02 | 2009-02-05 | Pfizer Inc | Substituted bicyclolactam compounds |
| US20090076275A1 (en) * | 2007-09-19 | 2009-03-19 | David Robert Bolin | Diacylglycerol acyltransferase inhibitors |
| AR066169A1 (es) * | 2007-09-28 | 2009-07-29 | Novartis Ag | Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat |
| US8324385B2 (en) * | 2008-10-30 | 2012-12-04 | Madrigal Pharmaceuticals, Inc. | Diacylglycerol acyltransferase inhibitors |
| TW201038580A (en) * | 2009-02-02 | 2010-11-01 | Pfizer | 4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl derivatives |
| WO2011121350A1 (en) | 2010-04-01 | 2011-10-06 | Astrazeneca Ab | 4 -amino -7,8- dihydropyrimido [5, 4 - f] [1, 4] oxazepin- 5 ( 6h) - one based dgat1 inhibitors |
| RS55006B1 (sr) * | 2011-05-20 | 2016-11-30 | Glaxosmithkline Intellectual Property (No 2) Ltd | Nova jedinjenja kao inhibitori diacilglicerol aciltransferaze |
-
2013
- 2013-11-22 EP EP18203369.6A patent/EP3492474B1/en active Active
- 2013-11-22 LT LTEP13856479.4T patent/LT2922551T/lt unknown
- 2013-11-22 WO PCT/US2013/071376 patent/WO2014081994A1/en not_active Ceased
- 2013-11-22 PT PT13856479T patent/PT2922551T/pt unknown
- 2013-11-22 PE PE2015000657A patent/PE20150967A1/es unknown
- 2013-11-22 HU HUE13856479A patent/HUE042483T2/hu unknown
- 2013-11-22 MX MX2015006533A patent/MX363484B/es unknown
- 2013-11-22 HR HRP20190099TT patent/HRP20190099T1/hr unknown
- 2013-11-22 UA UAA201506216A patent/UA115079C2/uk unknown
- 2013-11-22 NZ NZ630436A patent/NZ630436A/en not_active IP Right Cessation
- 2013-11-22 EP EP13856479.4A patent/EP2922551B1/en active Active
- 2013-11-22 US US14/646,403 patent/US20150322082A1/en not_active Abandoned
- 2013-11-22 JP JP2015544141A patent/JP6279600B2/ja not_active Expired - Fee Related
- 2013-11-22 BR BR112015011982A patent/BR112015011982A8/pt active Search and Examination
- 2013-11-22 CA CA2892304A patent/CA2892304C/en not_active Expired - Fee Related
- 2013-11-22 KR KR1020157016270A patent/KR102176463B1/ko not_active Expired - Fee Related
- 2013-11-22 CN CN201380069807.4A patent/CN104918620B/zh not_active Expired - Fee Related
- 2013-11-22 PL PL13856479T patent/PL2922551T3/pl unknown
- 2013-11-22 SM SM20190230T patent/SMT201900230T1/it unknown
- 2013-11-22 DK DK13856479.4T patent/DK2922551T3/en active
- 2013-11-22 ES ES13856479T patent/ES2708626T3/es active Active
- 2013-11-22 ME MEP-2019-14A patent/ME03315B/me unknown
- 2013-11-22 RS RS20190081A patent/RS58539B1/sr unknown
- 2013-11-22 AU AU2013347843A patent/AU2013347843B2/en not_active Ceased
- 2013-11-22 EA EA201590982A patent/EA031114B1/ru unknown
- 2013-11-22 SI SI201331321T patent/SI2922551T1/sl unknown
- 2013-11-22 SG SG11201503761WA patent/SG11201503761WA/en unknown
-
2015
- 2015-05-12 ZA ZA2015/03304A patent/ZA201503304B/en unknown
- 2015-05-14 IL IL238835A patent/IL238835B/en active IP Right Grant
- 2015-05-19 PH PH12015501109A patent/PH12015501109A1/en unknown
- 2015-05-22 CL CL2015001397A patent/CL2015001397A1/es unknown
-
2019
- 2019-01-29 CY CY20191100120T patent/CY1121426T1/el unknown
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