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 |
|---|---|---|---|---|
| MX2012004753A (es) | 2009-10-23 | 2012-09-07 | Janssen Pharmaceutica Nv | Octahidropirrolo[3,4-c]pirrolos disustituidos como moduladores del receptor de orexina. |
| RU2014136339A (ru) | 2012-02-07 | 2016-03-27 | Иолас Терапьютикс, Инк. | Замещенные пролины/пиперидины как антагонисты орексиновых рецепторов |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| ITMI20120322A1 (it) * | 2012-03-01 | 2013-09-02 | Rottapharm Spa | Composti di 4,4-difluoro piperidina |
| EP2925321A4 (en) * | 2012-11-27 | 2016-04-27 | Merck Sharp & Dohme | 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 |
| UY35993A (es) * | 2014-02-12 | 2015-08-31 | Eolas Therapeutics Inc | Prolinas / piperidinas sustituidas como antagonistas del receptor de orexina |
| EP3180332B1 (en) | 2014-08-13 | 2021-10-27 | Eolas Therapeutics Inc. | Difluoropyrrolidines as orexin receptor modulators |
| WO2016040789A1 (en) * | 2014-09-11 | 2016-03-17 | 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 |
| KR102738491B1 (ko) * | 2016-02-12 | 2024-12-03 | 아스트라제네카 아베 | 오렉신 수용체 조정제로서의 할로-치환된 피페리딘 |
| RS63296B1 (sr) | 2016-03-10 | 2022-07-29 | Janssen Pharmaceutica Nv | Metode lečenja depresije korišćenjem antagonista receptora oreksin-2 |
| CA3017388C (en) * | 2016-04-01 | 2024-03-12 | Zeno Royalties & Milestones, LLC | Estrogen receptor modulators |
| RU2763493C2 (ru) * | 2016-05-12 | 2021-12-29 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Способы лечения расстройств циркадного ритма сна |
| SMT202500122T1 (it) | 2017-09-01 | 2025-05-12 | Chronos Therapeutics Ltd | Derivati di 2-azabiciclo[3.1.1]eptano e 2-azabiciclo[3.2.1]ottano sostituiti come antagonisti del recettore di oressina |
| 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 |
| JP2022534709A (ja) * | 2019-06-04 | 2022-08-03 | ヘイガー バイオサイエンシズ,エルエルシー | オレキシンアンタゴニストとしてのピラゾール及びイミダゾール誘導体、組成物、並びに方法 |
| MX2023013975A (es) * | 2021-05-26 | 2023-12-11 | Sumitomo Pharma Co Ltd | Derivado de fenil urea. |
Family Cites Families (146)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5049578A (en) * | 1990-03-09 | 1991-09-17 | E. R. Squibb & Sons, Inc. | 1-aroyl or 1-acyl-2-2pyrrolidinyl-3,5-dihydroxy alkanoic and alkenoic acids, salts, esters and lactones |
| EP1075478B1 (en) | 1998-05-08 | 2003-04-16 | SmithKline Beecham plc | Phenylurea and phenylthio urea derivatives |
| WO2000047576A1 (en) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Cinnamide derivatives as orexin-1 receptors antagonists |
| DE60015927T2 (de) | 1999-02-12 | 2005-04-07 | Smithkline Beecham P.L.C., Brentford | Phenylharnstoff und phenylthioharnstoffderivate |
| ES2226785T3 (es) | 1999-02-12 | 2005-04-01 | Smithkline Beecham Plc | Derivados de fenilurea como antagonistas de los receptores de orexina. |
| JP2003500386A (ja) * | 1999-05-24 | 2003-01-07 | シーオーアール セラピューティクス インコーポレイテッド | Xa因子阻害剤 |
| EP1288202A4 (en) | 2000-05-11 | 2003-07-02 | Banyu Pharma Co Ltd | N-acyltetrahydroisoquinoline derivatives |
| ES2238458T3 (es) * | 2000-06-16 | 2005-09-01 | Smithkline Beecham Plc | Piperidinas para uso como antagonistas de los receptores de orexina. |
| AU2002224885A1 (en) | 2000-11-28 | 2002-06-11 | Smithkline Beecham Plc | Morpholine derivatives as antagonists of orexin receptors |
| WO2002051232A2 (en) | 2000-12-27 | 2002-07-04 | Actelion Pharmaceuticals Ltd. | Novel benzazepines and related heterocyclic derivatives |
| MXPA03010129A (es) * | 2001-05-05 | 2004-03-10 | Smithkline Beecham Plc | N-aroilaminas-ciclicas. |
| EP1435955A2 (en) | 2001-05-05 | 2004-07-14 | SmithKline Beecham P.L.C. | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| 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 |
| GB0130341D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| GB0130335D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| GB0130393D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| ES2278197T3 (es) | 2002-07-09 | 2007-08-01 | Actelion Pharmaceuticals Ltd. | Derivados de 7,8,9,10-tetrahidro-6h-azepino, 6,7,8,9-tetrahidro-pirido y 2,3-dihidro-2h-pirrolo(1,2-b)-quinazolinona. |
| US20060040937A1 (en) * | 2002-09-18 | 2006-02-23 | Glaxo Group Limited | N-aroyl cyclic amines as orexin receptor antagonists |
| WO2004033418A2 (en) | 2002-10-11 | 2004-04-22 | Actelion Pharmaceuticals Ltd. | Sulfonylamino-acetic derivatives and their use as orexin receptor antagonists |
| GB0225938D0 (en) | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| GB0225884D0 (en) * | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| GB0225944D0 (en) | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| AU2003299648A1 (en) | 2002-12-12 | 2004-06-30 | Janssen Pharmaceutica, N.V. | Substituted 4-phenyl-(1,3)-dioxanes |
| KR20050114242A (ko) | 2003-03-26 | 2005-12-05 | 액테리온 파마슈티칼 리미티드 | 오렉신 수용체 길항제로서 이용되는테트라하이드로이소퀴놀릴 아세트아마이드 유도체 |
| CA2520839A1 (en) | 2003-04-28 | 2004-11-11 | Actelion Pharmaceuticals Ltd | Quinoxalinone-3- one derivatives as orexin receptor antagonists |
| HUP0304101A3 (en) | 2003-12-22 | 2008-10-28 | Sanofi Aventis | Pyrazole derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates |
| HUP0400405A3 (en) | 2004-02-10 | 2009-03-30 | Sanofi Synthelabo | Pyrimidine derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates |
| US7763638B2 (en) | 2004-03-01 | 2010-07-27 | Actelion Pharmaceuticals Ltd. | Substituted 1,2,3,4-tetrahydroisoquinoline derivatives |
| WO2006067224A2 (en) | 2004-12-23 | 2006-06-29 | Biovitrum Ab (Publ) | Spiro-benzodioxole and spiro-benzodioxane compounds as orexin receptor antagonists |
| JP2008538361A (ja) | 2005-04-12 | 2008-10-23 | メルク エンド カムパニー インコーポレーテッド | アミドプロポキシフェニルオレキシン受容体アンタゴニスト |
| US7968289B2 (en) | 2005-05-03 | 2011-06-28 | Ensemble Therapeutics Corporation | Turn over probes and use thereof for nucleic acid detection |
| WO2006127550A1 (en) | 2005-05-23 | 2006-11-30 | Merck & Co., Inc. | Proline bis-amide orexin receptor antagonists |
| AU2006278575A1 (en) | 2005-08-04 | 2007-02-15 | Merck & Co., Inc. | Aminoethane sulfonamide orexin receptor antagonists |
| JP2009506061A (ja) | 2005-08-26 | 2009-02-12 | メルク エンド カムパニー インコーポレーテッド | ジアザスピロデカンオレキシン受容体拮抗薬 |
| US20090088452A1 (en) | 2005-11-22 | 2009-04-02 | Coleman Paul J | Indole Orexin Receptor Antagonists |
| CN101009515A (zh) | 2006-01-24 | 2007-08-01 | 华为技术有限公司 | 通信终端设备管理方法及通信终端 |
| TW200800020A (en) | 2006-01-26 | 2008-01-01 | Basf Ag | Methods to use 3-pyridyl derivatives as pesticides |
| FR2896798A1 (fr) | 2006-01-27 | 2007-08-03 | Sanofi Aventis Sa | Derives de sulfonamides, leur preparation et leur application en therapeutique |
| FR2896799B1 (fr) | 2006-02-02 | 2008-03-28 | Sanofi Aventis Sa | Derives de sulfonamides, leur preparation et leur application en therapeutique |
| US20090105318A1 (en) | 2006-03-29 | 2009-04-23 | Coleman Paul J | Amidoethylthioether Orexin Receptor Antagonists |
| US8003654B2 (en) | 2006-04-11 | 2011-08-23 | Actelion Pharmaceuticals Ltd. | N-glycinsulfonamide derivatives and uses as orexin receptor antagonists |
| CN101432285A (zh) | 2006-04-26 | 2009-05-13 | 埃科特莱茵药品有限公司 | 作为食欲素受体拮抗剂的吡唑并-四氢吡啶衍生物 |
| WO2007143813A1 (en) | 2006-06-16 | 2007-12-21 | Husky Injection Molding Systems Ltd. | Preventative maintenance update system |
| DK2049529T3 (da) | 2006-07-14 | 2010-11-29 | Merck Sharp & Dohme | Substituerede diazepan-orexin-receptor- antagonister |
| EP2049110B1 (en) | 2006-07-14 | 2014-08-20 | Merck Sharp & Dohme Corp. | Bridged diazepan orexin receptor antagonists |
| AU2007272795A1 (en) | 2006-07-14 | 2008-01-17 | Merck & Co., Inc. | 2-substituted proline bis-amide orexin receptor antagonists |
| KR101113626B1 (ko) | 2006-08-15 | 2012-02-17 | 액테리온 파마슈티칼 리미티드 | 오렉신 수용체 길항제로서 아제티딘 화합물 |
| WO2008026149A1 (en) | 2006-08-28 | 2008-03-06 | Actelion Pharmaceuticals Ltd | 1,4,5,6, 7,8-hexahydro-i^1s-triaza-azulene derivatives as orexin receptor antagonists |
| TW200823227A (en) | 2006-09-29 | 2008-06-01 | Actelion Pharmaceuticals Ltd | 3-aza-bicyclo[3.1.0]hexane derivatives |
| PE20081229A1 (es) | 2006-12-01 | 2008-08-28 | Merck & Co Inc | Antagonistas de receptor de orexina de diazepam sustituido |
| ATE496043T1 (de) | 2006-12-01 | 2011-02-15 | Actelion Pharmaceuticals Ltd | 3-heteroaryl (amino bzw. amido)-1- (biphenyl bzw. phenylthiazolyl) carbonylpiperdinderivate als orexinrezeptor-inhibitoren |
| CA2669561A1 (en) | 2006-12-22 | 2008-07-03 | Actelion Pharmaceuticals Ltd | 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives |
| TW200833328A (en) | 2006-12-28 | 2008-08-16 | Actelion Pharmaceuticals Ltd | 2-aza-bicyclo[3.1.0]hexane derivatives |
| WO2008087611A2 (en) * | 2007-01-19 | 2008-07-24 | Actelion Pharmaceuticals Ltd | Pyrrolidine- and piperidine- bis-amide derivatives |
| JP2010520206A (ja) | 2007-03-02 | 2010-06-10 | メルク・シャープ・エンド・ドーム・コーポレイション | ビピリジンカルボキサミドオレキシン受容体アンタゴニスト |
| MX2009009121A (es) | 2007-03-05 | 2009-09-03 | Hoffmann La Roche | Aminoamidas como antagonistas de orexina. |
| JP5148636B2 (ja) | 2007-03-15 | 2013-02-20 | エフ.ホフマン−ラ ロシュ アーゲー | オレキシンアンタゴニストとしてのマロンアミド |
| CL2008000836A1 (es) | 2007-03-26 | 2008-11-07 | Actelion Pharmaceuticals Ltd | Compuestos derivados de tiazolidina, antagonistas del receptor de orexina; composicion farmaceutica que los comprende; y su uso en el tratamiento de neurosis emocional, depresion grave, trastornos psicoticos, alzheimer, parkinson, dolor, entre otras. |
| AU2008235528B2 (en) | 2007-04-04 | 2012-11-08 | F. Hoffmann-La Roche Ag | Heterocycles as orexin antagonists |
| DE602008002934D1 (de) | 2007-05-14 | 2010-11-18 | Actelion Pharmaceuticals Ltd | 2-cyclopropylthiazolderivate |
| EP2150114A4 (en) | 2007-05-18 | 2012-01-18 | Merck Sharp & Dohme | OXO-BRIDGED DIAZEPANOREXINE RECEPTOR ANTAGONISTS |
| JP2010528007A (ja) * | 2007-05-23 | 2010-08-19 | メルク・シャープ・エンド・ドーム・コーポレイション | シクロプロピルピロリジンオレキシン受容体アンタゴニスト |
| NZ580887A (en) * | 2007-05-23 | 2012-03-30 | Merck Sharp & Dohme | Pyridyl piperidine orexin receptor antagonists |
| ES2371514T3 (es) * | 2007-07-03 | 2012-01-04 | Actelion Pharmaceuticals Ltd. | Compuestos de 3-aza-biciclo[3.3.0]octano. |
| CN101874028B (zh) | 2007-07-27 | 2012-11-14 | 埃科特莱茵药品有限公司 | 2-氮杂-二环[3.3.0]辛烷衍生物 |
| ATE493386T1 (de) | 2007-07-27 | 2011-01-15 | Actelion Pharmaceuticals Ltd | Trans-3-aza-bicyclo-ä3.1.0ü-hexan-derivate |
| US20090036422A1 (en) | 2007-08-02 | 2009-02-05 | Henner Knust | Monoamide derivatives as orexin receptor antagonists |
| JP2010535769A (ja) | 2007-08-09 | 2010-11-25 | メルク・シャープ・エンド・ドーム・コーポレイション | ピリジンカルボキサミドオレキシン受容体アンタゴニスト |
| BRPI0823262A2 (pt) * | 2007-08-10 | 2013-09-24 | Cortex Pharma Inc | mÉtodo de tratamento de depressço respiratària e uso de um composto na fabricaÇço de um medicamento para o tratamento de depressço respiratària |
| ES2400830T3 (es) | 2007-08-15 | 2013-04-12 | Actelion Pharmaceuticals Ltd. | Derivados de 1,2-diamido-etileno como antagonistas de orexina |
| US8288411B2 (en) | 2007-09-24 | 2012-10-16 | Actelion Pharmaceuticals Ltd. | Pyrrolidines and piperidines as orexin receptor antagonists |
| JP2011502146A (ja) | 2007-10-29 | 2011-01-20 | メルク・シャープ・エンド・ドーム・コーポレイション | 置換ジアゼパンオレキシン受容体アンタゴニスト |
| US8084464B2 (en) | 2007-12-18 | 2011-12-27 | Concert Pharmaceuticals, Inc. | Tetrahydroisoquinoline derivatives |
| WO2009080533A1 (en) | 2007-12-21 | 2009-07-02 | F. Hoffmann-La Roche Ag | Heteroaryl derivatives as orexin receptor antagonists |
| WO2009092642A1 (en) | 2008-01-21 | 2009-07-30 | F. Hoffmann-La Roche Ag | Sulfonamides as orexin antagonists |
| ATE517090T1 (de) | 2008-02-12 | 2011-08-15 | Hoffmann La Roche | Piperidinsulfonamidderivate |
| CN101965343A (zh) * | 2008-02-21 | 2011-02-02 | 埃科特莱茵药品有限公司 | 2-氮杂-双环[2.2.1]庚烷衍生物 |
| GB0806536D0 (en) | 2008-04-10 | 2008-05-14 | Glaxo Group Ltd | Novel compounds |
| CN102056920A (zh) | 2008-06-11 | 2011-05-11 | 埃科特莱茵药品有限公司 | 用作食欲素受体拮抗剂的四唑化合物 |
| JP2011524398A (ja) | 2008-06-16 | 2011-09-01 | エフ.ホフマン−ラ ロシュ アーゲー | オレキシニン受容体アンタゴニストとしてのヘテロ芳香族モノアミド |
| KR20110036069A (ko) | 2008-06-25 | 2011-04-06 | 액테리온 파마슈티칼 리미티드 | 5,6,7,8-테트라히드로-이미다조[1,5-a]피라진 화합물 |
| CN102083827A (zh) | 2008-07-07 | 2011-06-01 | 埃科特莱茵药品有限公司 | 作为食欲素受体拮抗剂的噻唑烷化合物 |
| MX2011000462A (es) | 2008-07-29 | 2011-04-05 | Hoffmann La Roche | Pirrolidin-3-ilmetil-amina como antagonista de orexina. |
| AR072899A1 (es) | 2008-08-07 | 2010-09-29 | Merck Sharp & Dohme | Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad. |
| EP2161266A1 (en) | 2008-08-22 | 2010-03-10 | EVOTEC Neurosciences GmbH | Benzofuran derivatives as orexin receptor antagonists |
| BRPI0920183A2 (pt) | 2008-10-14 | 2018-05-22 | Actelion Pharmaceuticals Ltd | derivados de fenetilamida e seus analogos heterociclicos |
| EP2349270B1 (en) | 2008-10-21 | 2015-09-09 | Merck Sharp & Dohme Corp. | 2,5-disubstituted morpholine orexin receptor antagonists |
| US8623863B2 (en) | 2008-10-21 | 2014-01-07 | Merck Sharp & Dohme Corp. | Disubstituted azepan orexin receptor antagonists |
| CA2739916A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| WO2010048014A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,4-disubstituted pyrrolidine orexin receptor antagonists |
| EP2350061B1 (en) | 2008-10-21 | 2013-08-14 | Merck Sharp & Dohme Corp. | 2,3-disubstituted piperidine orexin receptor antagonists |
| JP2012506374A (ja) | 2008-10-21 | 2012-03-15 | メルク・シャープ・エンド・ドーム・コーポレイション | 2,5−二置換ピペリジンオレキシン受容体アンタゴニスト |
| EP2349262B1 (en) | 2008-10-30 | 2014-06-25 | Merck Sharp & Dohme Corp. | 2,5-disubstituted phenyl carboxamide orexin receptor antagonists |
| US8703770B2 (en) | 2008-10-30 | 2014-04-22 | Merck Sharp & Dohme Corp. | Pyridazine carboxamide orexin receptor antagonists |
| MX2011004551A (es) | 2008-10-30 | 2011-05-25 | Merck Sharp & Dohme | Antagonistas del receptor de orexina de isonicotinamida. |
| WO2010060470A1 (en) | 2008-11-26 | 2010-06-03 | Glaxo Group Limited | Piperidine derivatives useful as orexin receptor antagonists |
| JP2012509912A (ja) | 2008-11-26 | 2012-04-26 | グラクソ グループ リミテッド | 新規の化合物 |
| JP2012509911A (ja) | 2008-11-26 | 2012-04-26 | グラクソ グループ リミテッド | 新規の化合物 |
| AU2009324239A1 (en) | 2008-12-02 | 2010-06-10 | Glaxo Group Limited | N-{[(IR,4S,6R-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof |
| AU2009324238A1 (en) | 2008-12-02 | 2010-06-10 | Glaxo Group Limited | N-{[(IR,4S,6R-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0] hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof |
| JP2010155827A (ja) | 2008-12-04 | 2010-07-15 | Takeda Chem Ind Ltd | スピロ環化合物 |
| GB0823467D0 (en) | 2008-12-23 | 2009-01-28 | Glaxo Group Ltd | Novel Compounds |
| UY32404A (es) | 2009-01-30 | 2010-08-31 | Novartis Ag | 4-aril-butan-1,3-diamidas |
| EA201171293A1 (ru) | 2009-04-24 | 2012-05-30 | Глэксо Груп Лимитед | 3-азабицикло[4.1.0]гептаны, применяемые в качестве антагонистов орексина |
| WO2011005636A1 (en) | 2009-07-09 | 2011-01-13 | Merck Sharp & Dohme Corp. | Tetrahydronapthyridine orexin receptor antagonists |
| EP2275421A1 (en) | 2009-07-15 | 2011-01-19 | Rottapharm S.p.A. | Spiro amino compounds suitable for the treatment of inter alia sleep disorders and drug addiction |
| WO2011016234A1 (en) * | 2009-08-04 | 2011-02-10 | Raqualia Pharma Inc. | Picolinamide derivatives as ttx-s blockers |
| US20120149711A1 (en) * | 2009-08-24 | 2012-06-14 | Glaxo Group Limited | Piperidine derivatives used as orexin antagonists |
| JP2013502447A (ja) * | 2009-08-24 | 2013-01-24 | グラクソ グループ リミテッド | 睡眠障害の治療のためのオレキシン受容体アンタゴニストとしての5−メチル−ピペリジン誘導体 |
| WO2011050202A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| WO2011050200A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| MX2012004753A (es) | 2009-10-23 | 2012-09-07 | Janssen Pharmaceutica Nv | Octahidropirrolo[3,4-c]pirrolos disustituidos como moduladores del receptor de orexina. |
| US20120196901A1 (en) | 2009-10-29 | 2012-08-02 | Merck Sharp & Dohme Corp. | Tertiary amide orexin receptor antagonists |
| EP2504316A1 (en) | 2009-11-23 | 2012-10-03 | MSD Oss B.V. | Heterocylic compounds as antagonists of the orexin receptors |
| WO2011073316A1 (en) | 2009-12-18 | 2011-06-23 | Novartis Ag | 4-aryl-butane-1,3-diamides |
| ES2459496T3 (es) | 2009-12-21 | 2014-05-09 | Novartis Ag | Diaza-espiro[5.5]undecanos como antagonistas del receptor de orexina |
| JP2013515032A (ja) | 2009-12-21 | 2013-05-02 | ノバルティス アーゲー | 二置換ヘテロアリール縮合ピリジン類 |
| WO2011138266A1 (en) | 2010-05-03 | 2011-11-10 | Evotec Ag | Indolizine and imidazopyridine derivatives as orexin receptor antagonists |
| WO2011138265A2 (en) | 2010-05-03 | 2011-11-10 | Evotec Ag | Indole and indazole derivatives as orexin receptor antagonists |
| EP2653469A4 (en) | 2010-12-17 | 2014-05-07 | Taisho Pharmaceutical Co Ltd | PYRAZOLE DERIVATIVE |
| US20120165339A1 (en) | 2010-12-22 | 2012-06-28 | Eisai R&D Management Co., Ltd. | Cyclopropane derivatives |
| WO2012085857A1 (en) | 2010-12-22 | 2012-06-28 | Actelion Pharmaceuticals Ltd | 3,8-diaza-bicyclo[4.2.0]oct-3-yl amides |
| US20120165331A1 (en) | 2010-12-22 | 2012-06-28 | Sangamesh Badiger | Di/tri-aza-spiro-C9-C11alkanes |
| WO2012089606A1 (en) | 2010-12-28 | 2012-07-05 | Glaxo Group Limited | Azabicyclo [4.1.0] hept - 4 - yl derivatives as human orexin receptor antagonists |
| WO2012089607A1 (en) | 2010-12-28 | 2012-07-05 | Glaxo Group Limited | Novel compounds with a 3a-azabicyclo [4.1.0] heptane core acting on orexin receptors |
| CN103380130B (zh) | 2011-02-18 | 2015-06-17 | 埃科特莱茵药品有限公司 | 用作为食欲素拮抗剂的新颖的吡唑和咪唑衍生物 |
| WO2012114252A1 (en) | 2011-02-21 | 2012-08-30 | Actelion Pharmaceuticals Ltd | Novel indole and pyrrolopyridine amides |
| US9586962B2 (en) | 2011-04-20 | 2017-03-07 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators |
| JPWO2012153729A1 (ja) | 2011-05-10 | 2014-07-31 | 大正製薬株式会社 | ヘテロ芳香環誘導体 |
| TW201315730A (zh) | 2011-07-05 | 2013-04-16 | 大正製藥股份有限公司 | 甲基哌啶衍生物 |
| WO2013050938A1 (en) | 2011-10-04 | 2013-04-11 | Actelion Pharmaceuticals Ltd | 3,7-diazabicyclo[3.3.1]nonane and 9-oxa-3,7-diazabicyclo[3.3.1]nonane derivatives |
| AR088352A1 (es) | 2011-10-19 | 2014-05-28 | Merck Sharp & Dohme | Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina |
| WO2013059163A1 (en) | 2011-10-21 | 2013-04-25 | Merck Sharp & Dohme Corp. | 2,5-disubstituted thiomorpholine orexin receptor antagonists |
| WO2013062858A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Isoxazolopyridine orexin receptor antagonists |
| EP2771001A4 (en) | 2011-10-25 | 2015-03-25 | Merck Sharp & Dohme | PIPERIDINYL-alkyne-orexin |
| EA024106B1 (ru) | 2011-11-08 | 2016-08-31 | Актелион Фармасьютиклз Лтд. | Производные 2-(1,2,3-триазол-2-ил)бензамида и 3-(1,2,3-триазол-2-ил)пиколинамида |
| ITMI20112329A1 (it) | 2011-12-21 | 2013-06-22 | Rottapharm Spa | Nuovi derivati spiro amminici |
| RU2014136339A (ru) * | 2012-02-07 | 2016-03-27 | Иолас Терапьютикс, Инк. | Замещенные пролины/пиперидины как антагонисты орексиновых рецепторов |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| ES2733750T3 (es) | 2012-02-17 | 2019-12-02 | Eisai R&D Man Co Ltd | Métodos y compuestos útiles en la síntesis de antagonistas del receptor de orexina-2 |
| ITMI20120322A1 (it) | 2012-03-01 | 2013-09-02 | Rottapharm Spa | Composti di 4,4-difluoro piperidina |
| ITMI20120424A1 (it) | 2012-03-19 | 2013-09-20 | Rottapharm Spa | Composti chimici |
| UY35993A (es) | 2014-02-12 | 2015-08-31 | Eolas Therapeutics Inc | Prolinas / piperidinas sustituidas como antagonistas del receptor de orexina |
-
2013
- 2013-02-06 RU RU2014136339A patent/RU2014136339A/ru not_active Application Discontinuation
- 2013-02-06 BR BR112014019426A patent/BR112014019426A8/pt not_active IP Right Cessation
- 2013-02-06 NZ NZ628491A patent/NZ628491A/en not_active IP Right Cessation
- 2013-02-06 JP JP2014556628A patent/JP6346862B2/ja active Active
- 2013-02-06 WO PCT/US2013/024903 patent/WO2013119639A1/en not_active Ceased
- 2013-02-06 MX MX2014009281A patent/MX2014009281A/es unknown
- 2013-02-06 EP EP13746989.6A patent/EP2811997B1/en active Active
- 2013-02-06 ES ES13746989.6T patent/ES2672732T3/es active Active
- 2013-02-06 KR KR1020147025072A patent/KR20140124398A/ko not_active Withdrawn
- 2013-02-06 HK HK15105691.4A patent/HK1204955A1/xx unknown
- 2013-02-06 SG SG11201404738QA patent/SG11201404738QA/en unknown
- 2013-02-06 CN CN201380018420.6A patent/CN104220065A/zh active Pending
- 2013-02-06 CA CA2863413A patent/CA2863413A1/en not_active Abandoned
- 2013-02-06 AU AU2013217323A patent/AU2013217323A1/en not_active Abandoned
-
2014
- 2014-02-12 US US14/179,432 patent/US9499517B2/en active Active
- 2014-08-07 PH PH12014501784A patent/PH12014501784A1/en unknown
- 2014-08-07 IL IL234025A patent/IL234025A0/en unknown
-
2015
- 2015-02-11 AR ARP150100403A patent/AR099466A1/es unknown
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2016
- 2016-10-20 US US15/299,230 patent/US9896452B2/en active Active
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