JP2015506382A5 - - Google Patents
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- JP2015506382A5 JP2015506382A5 JP2014556628A JP2014556628A JP2015506382A5 JP 2015506382 A5 JP2015506382 A5 JP 2015506382A5 JP 2014556628 A JP2014556628 A JP 2014556628A JP 2014556628 A JP2014556628 A JP 2014556628A JP 2015506382 A5 JP2015506382 A5 JP 2015506382A5
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- JP
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- Prior art keywords
- hydrate
- salt
- compound according
- alkyl
- independently
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 61
- -1 (C 1-4 ) acylamide Chemical group 0.000 claims description 52
- 150000003839 salts Chemical class 0.000 claims description 46
- 108050000742 Orexin Receptor Proteins 0.000 claims description 23
- 102000008834 Orexin receptor Human genes 0.000 claims description 23
- 125000002619 bicyclic group Chemical group 0.000 claims description 23
- 125000002950 monocyclic group Chemical group 0.000 claims description 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 17
- 125000000217 alkyl group Chemical group 0.000 claims description 16
- 125000003118 aryl group Chemical group 0.000 claims description 16
- 229910052757 nitrogen Inorganic materials 0.000 claims description 15
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 15
- 208000011117 substance-related disease Diseases 0.000 claims description 15
- 125000001072 heteroaryl group Chemical group 0.000 claims description 14
- 125000004076 pyridyl group Chemical group 0.000 claims description 14
- 125000000623 heterocyclic group Chemical group 0.000 claims description 13
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims description 12
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims description 12
- 125000004122 cyclic group Chemical group 0.000 claims description 11
- 201000010099 disease Diseases 0.000 claims description 11
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims description 10
- 125000005493 quinolyl group Chemical group 0.000 claims description 10
- 229910052717 sulfur Inorganic materials 0.000 claims description 10
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims description 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 9
- 206010013663 drug dependence Diseases 0.000 claims description 9
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 9
- 125000002252 acyl group Chemical group 0.000 claims description 8
- 208000020016 psychiatric disease Diseases 0.000 claims description 8
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 8
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 8
- 125000001424 substituent group Chemical group 0.000 claims description 8
- 206010013654 Drug abuse Diseases 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 206010012335 Dependence Diseases 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 208000007848 Alcoholism Diseases 0.000 claims description 5
- 208000024827 Alzheimer disease Diseases 0.000 claims description 5
- 208000019901 Anxiety disease Diseases 0.000 claims description 5
- 208000020925 Bipolar disease Diseases 0.000 claims description 5
- 206010012289 Dementia Diseases 0.000 claims description 5
- 208000030814 Eating disease Diseases 0.000 claims description 5
- 208000019454 Feeding and Eating disease Diseases 0.000 claims description 5
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 5
- 206010019233 Headaches Diseases 0.000 claims description 5
- 208000023105 Huntington disease Diseases 0.000 claims description 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 206010020772 Hypertension Diseases 0.000 claims description 5
- 206010061218 Inflammation Diseases 0.000 claims description 5
- 208000019695 Migraine disease Diseases 0.000 claims description 5
- 208000019022 Mood disease Diseases 0.000 claims description 5
- 208000012902 Nervous system disease Diseases 0.000 claims description 5
- 208000008589 Obesity Diseases 0.000 claims description 5
- 208000002193 Pain Diseases 0.000 claims description 5
- 208000018737 Parkinson disease Diseases 0.000 claims description 5
- 206010034912 Phobia Diseases 0.000 claims description 5
- 201000007930 alcohol dependence Diseases 0.000 claims description 5
- 208000028505 alcohol-related disease Diseases 0.000 claims description 5
- 230000036506 anxiety Effects 0.000 claims description 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 5
- 230000003542 behavioural effect Effects 0.000 claims description 5
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 5
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 5
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 5
- 208000028683 bipolar I disease Diseases 0.000 claims description 5
- 229960003920 cocaine Drugs 0.000 claims description 5
- 208000010877 cognitive disease Diseases 0.000 claims description 5
- 208000010643 digestive system disease Diseases 0.000 claims description 5
- 235000014632 disordered eating Nutrition 0.000 claims description 5
- 230000002124 endocrine Effects 0.000 claims description 5
- 206010015037 epilepsy Diseases 0.000 claims description 5
- 208000018685 gastrointestinal system disease Diseases 0.000 claims description 5
- 150000002367 halogens Chemical class 0.000 claims description 5
- 231100000869 headache Toxicity 0.000 claims description 5
- 229910052739 hydrogen Inorganic materials 0.000 claims description 5
- 239000001257 hydrogen Substances 0.000 claims description 5
- 125000002883 imidazolyl group Chemical group 0.000 claims description 5
- 230000004054 inflammatory process Effects 0.000 claims description 5
- 208000017169 kidney disease Diseases 0.000 claims description 5
- 206010027599 migraine Diseases 0.000 claims description 5
- 235000020824 obesity Nutrition 0.000 claims description 5
- 125000002971 oxazolyl group Chemical group 0.000 claims description 5
- 125000004043 oxo group Chemical group O=* 0.000 claims description 5
- 208000019899 phobic disease Diseases 0.000 claims description 5
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 5
- 201000000980 schizophrenia Diseases 0.000 claims description 5
- 208000012201 sexual and gender identity disease Diseases 0.000 claims description 5
- 208000015891 sexual disease Diseases 0.000 claims description 5
- 208000019116 sleep disease Diseases 0.000 claims description 5
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims description 4
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 125000005843 halogen group Chemical group 0.000 claims description 4
- 229960002715 nicotine Drugs 0.000 claims description 4
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 208000020685 sleep-wake disease Diseases 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000006717 (C3-C10) cycloalkenyl group Chemical group 0.000 claims description 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 239000008896 Opium Substances 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 3
- 229960001027 opium Drugs 0.000 claims description 3
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 3
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 2
- 125000004423 acyloxy group Chemical group 0.000 claims description 2
- 125000003435 aroyl group Chemical group 0.000 claims description 2
- 125000004104 aryloxy group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 0.000 claims description 2
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 2
- 238000001727 in vivo Methods 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 229940127240 opiate Drugs 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000005543 phthalimide group Chemical group 0.000 claims description 2
- 125000005544 phthalimido group Chemical group 0.000 claims description 2
- 102000005962 receptors Human genes 0.000 claims description 2
- 108020003175 receptors Proteins 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 15
- 230000003042 antagnostic effect Effects 0.000 claims 3
- 208000028017 Psychotic disease Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 241000238366 Cephalopoda Species 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 description 12
- 230000008485 antagonism Effects 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 1
- KWTSXDURSIMDCE-QMMMGPOBSA-N (S)-amphetamine Chemical compound C[C@H](N)CC1=CC=CC=C1 KWTSXDURSIMDCE-QMMMGPOBSA-N 0.000 description 1
- 208000029197 Amphetamine-Related disease Diseases 0.000 description 1
- 208000025966 Neurological disease Diseases 0.000 description 1
- 206010043903 Tobacco abuse Diseases 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 229940025084 amphetamine Drugs 0.000 description 1
- 201000002472 amphetamine abuse Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261596062P | 2012-02-07 | 2012-02-07 | |
| US61/596,062 | 2012-02-07 | ||
| PCT/US2013/024903 WO2013119639A1 (en) | 2012-02-07 | 2013-02-06 | Substituted prolines / piperidines as orexin receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015506382A JP2015506382A (ja) | 2015-03-02 |
| JP2015506382A5 true JP2015506382A5 (enExample) | 2016-11-24 |
| JP6346862B2 JP6346862B2 (ja) | 2018-06-20 |
Family
ID=48947950
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014556628A Active JP6346862B2 (ja) | 2012-02-07 | 2013-02-06 | オレキシンレセプターアンタゴニストとしての置換プロリン／ピペリジン |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US9499517B2 (enExample) |
| EP (1) | EP2811997B1 (enExample) |
| JP (1) | JP6346862B2 (enExample) |
| KR (1) | KR20140124398A (enExample) |
| CN (1) | CN104220065A (enExample) |
| AR (1) | AR099466A1 (enExample) |
| AU (1) | AU2013217323A1 (enExample) |
| BR (1) | BR112014019426A8 (enExample) |
| CA (1) | CA2863413A1 (enExample) |
| ES (1) | ES2672732T3 (enExample) |
| HK (1) | HK1204955A1 (enExample) |
| IL (1) | IL234025A0 (enExample) |
| MX (1) | MX2014009281A (enExample) |
| NZ (1) | NZ628491A (enExample) |
| PH (1) | PH12014501784A1 (enExample) |
| RU (1) | RU2014136339A (enExample) |
| SG (1) | SG11201404738QA (enExample) |
| WO (1) | WO2013119639A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8653263B2 (en) | 2009-10-23 | 2014-02-18 | Janssen Pharmaceutica | Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| ES2672732T3 (es) | 2012-02-07 | 2018-06-15 | Eolas Therapeutics Inc. | Prolinas/piperidinas sustituidas como antagonistas del receptor de orexina |
| ITMI20120322A1 (it) * | 2012-03-01 | 2013-09-02 | Rottapharm Spa | Composti di 4,4-difluoro piperidina |
| WO2014085208A1 (en) * | 2012-11-27 | 2014-06-05 | Merck Sharp & Dohme Corp. | 2-pyridylamino-4-nitrile-piperidinyl orexin receptor antagonists |
| WO2015018027A1 (en) * | 2013-08-08 | 2015-02-12 | Merck Sharp & Dohme Corp. | Thiazole orexin receptor antagonists |
| JP2017001954A (ja) * | 2013-11-08 | 2017-01-05 | 石原産業株式会社 | 含窒素飽和複素環化合物 |
| JP2017024990A (ja) * | 2013-12-13 | 2017-02-02 | 大正製薬株式会社 | オキサゾリジン及びオキサジナン誘導体 |
| WO2015123355A1 (en) * | 2014-02-12 | 2015-08-20 | Eolas Therapeutics, Inc. | Substituted prolines / piperidines as orexin receptor antagonists |
| UY36272A (es) * | 2014-08-13 | 2016-02-29 | Eolas Therapeutics Inc | Difluoropirrolidinas como moduladores de los receptores de orexinas |
| EP3191468B1 (en) * | 2014-09-11 | 2018-12-12 | Janssen Pharmaceutica NV | Substituted 2-azabicycles and their use as orexin receptor modulators |
| JP2018016544A (ja) * | 2014-12-03 | 2018-02-01 | 持田製薬株式会社 | 新規ジアザビシクロ［２．２．２］オクタン誘導体 |
| CN104557744B (zh) * | 2014-12-23 | 2017-04-12 | 广东东阳光药业有限公司 | 一种三氮唑化合物的制备方法 |
| TWI710557B (zh) * | 2016-02-12 | 2020-11-21 | 美商伊歐拉斯治療學公司 | 作為食慾素受體調節劑之經鹵素取代之六氫吡啶 |
| BR112018067906A2 (pt) | 2016-03-10 | 2019-01-29 | Janssen Pharmaceutica Nv | métodos de tratamento de depressão usando antagonistas do receptor de orexina-2 |
| RU2738646C2 (ru) * | 2016-04-01 | 2020-12-15 | РЕКЬЮРИУМ АйПи ХОЛДИНГС, ЛЛС | Модуляторы эстрогеновых рецепторов |
| CN109640998A (zh) * | 2016-05-12 | 2019-04-16 | 卫材研究发展管理有限公司 | 治疗昼夜节律性睡眠障碍的方法 |
| MD3676261T2 (ro) * | 2017-09-01 | 2025-05-31 | Chronos Therapeutics Ltd | 2-azabiciclo[3.1.1]heptan substituit și derivați de 2-azabiciclo[3.2.1]octan ca antagoniști ai receptoriului orexinei |
| GB2558975B (en) * | 2017-09-01 | 2019-01-23 | Chronos Therapeutics Ltd | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
| US12187737B2 (en) | 2019-06-04 | 2025-01-07 | Hager Biosciences, Llc | Imidazolo derivatives, compositions and methods as orexin antagonists |
| SG11202112828SA (en) * | 2019-06-04 | 2021-12-30 | Hager Biosciences Llc | Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists |
| EP4353309A4 (en) * | 2021-05-26 | 2025-05-07 | Sumitomo Pharma Co., Ltd. | PHENYLUREA DERIVATIVE |
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| GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| GB0124463D0 (en) | 2001-10-11 | 2001-12-05 | Smithkline Beecham Plc | Compounds |
| GB0126292D0 (en) | 2001-11-01 | 2002-01-02 | Smithkline Beecham Plc | Compounds |
| GB0127145D0 (en) | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Compounds |
| GB0130335D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| GB0130341D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
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-
2013
- 2013-02-06 ES ES13746989.6T patent/ES2672732T3/es active Active
- 2013-02-06 HK HK15105691.4A patent/HK1204955A1/xx unknown
- 2013-02-06 JP JP2014556628A patent/JP6346862B2/ja active Active
- 2013-02-06 CA CA2863413A patent/CA2863413A1/en not_active Abandoned
- 2013-02-06 EP EP13746989.6A patent/EP2811997B1/en active Active
- 2013-02-06 KR KR1020147025072A patent/KR20140124398A/ko not_active Withdrawn
- 2013-02-06 AU AU2013217323A patent/AU2013217323A1/en not_active Abandoned
- 2013-02-06 SG SG11201404738QA patent/SG11201404738QA/en unknown
- 2013-02-06 WO PCT/US2013/024903 patent/WO2013119639A1/en not_active Ceased
- 2013-02-06 CN CN201380018420.6A patent/CN104220065A/zh active Pending
- 2013-02-06 RU RU2014136339A patent/RU2014136339A/ru not_active Application Discontinuation
- 2013-02-06 NZ NZ628491A patent/NZ628491A/en not_active IP Right Cessation
- 2013-02-06 MX MX2014009281A patent/MX2014009281A/es unknown
- 2013-02-06 BR BR112014019426A patent/BR112014019426A8/pt not_active IP Right Cessation
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2016
- 2016-10-20 US US15/299,230 patent/US9896452B2/en active Active
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