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 (https=) | 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 (https=) |
| EP (1) | EP2811997B1 (https=) |
| JP (1) | JP6346862B2 (https=) |
| KR (1) | KR20140124398A (https=) |
| CN (1) | CN104220065A (https=) |
| AR (1) | AR099466A1 (https=) |
| AU (1) | AU2013217323A1 (https=) |
| BR (1) | BR112014019426A8 (https=) |
| CA (1) | CA2863413A1 (https=) |
| ES (1) | ES2672732T3 (https=) |
| HK (1) | HK1204955A1 (https=) |
| IL (1) | IL234025A0 (https=) |
| MX (1) | MX2014009281A (https=) |
| NZ (1) | NZ628491A (https=) |
| PH (1) | PH12014501784A1 (https=) |
| RU (1) | RU2014136339A (https=) |
| SG (1) | SG11201404738QA (https=) |
| WO (1) | WO2013119639A1 (https=) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2585806T3 (es) | 2009-10-23 | 2016-10-10 | Janssen Pharmaceutica N.V. | Octahidropirrolo [3,4-c] pirroles disustituidos como moduladores de receptores de orexina |
| 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 |
| JP6663909B2 (ja) * | 2014-08-13 | 2020-03-13 | エオラス セラピューティクス， インコーポレイテッド | オレキシンレセプターモジュレーターとしてのジフルオロピロリジン |
| AU2015314851B2 (en) * | 2014-09-11 | 2020-01-02 | 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 |
| MX2018009656A (es) | 2016-02-12 | 2019-02-20 | Astrazeneca Ab | Piperidinas halo-sustituidas como moduladores de los receptores de orexinas. |
| US10828302B2 (en) | 2016-03-10 | 2020-11-10 | Janssen Pharmaceutica Nv | Methods of treating depression using orexin-2 receptor antagonists |
| CN112745316A (zh) * | 2016-04-01 | 2021-05-04 | 里科瑞尔姆Ip控股有限责任公司 | 雌激素受体调节剂 |
| CA3022068A1 (en) * | 2016-05-12 | 2017-11-16 | Eisai R&D Management Co., Ltd. | Methods of treating circadian rhythm sleep disorders |
| AU2018326734B2 (en) | 2017-09-01 | 2023-08-17 | Chronos Therapeutics Limited | Substituted 2-azabicyclo(3.1.1)heptane and 2-azabicyclo(3.2.1)octane derivatives as orexin receptor antagonists |
| 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 |
| US20220315602A1 (en) * | 2019-06-04 | 2022-10-06 | Hager Biosciences, Llc | Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists |
| CN114286675A (zh) | 2019-06-04 | 2022-04-05 | 海格生物科学有限责任公司 | 作为食欲肽拮抗剂的咪唑衍生物、组合物以及方法 |
| WO2022250108A1 (ja) * | 2021-05-26 | 2022-12-01 | 住友ファーマ株式会社 | フェニルウレア誘導体 |
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 |
| ES2196806T3 (es) | 1998-05-08 | 2003-12-16 | Smithkline Beecham Plc | Derivados de fenilurea y de feniltiourea. |
| DE60015927T2 (de) | 1999-02-12 | 2005-04-07 | Smithkline Beecham P.L.C., Brentford | Phenylharnstoff und phenylthioharnstoffderivate |
| WO2000047576A1 (en) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Cinnamide derivatives as orexin-1 receptors antagonists |
| AU2804400A (en) | 1999-02-12 | 2000-08-29 | Smithkline Beecham Plc | Phenyl urea and phenyl thiourea derivatives as orexin receptor antagonists |
| EP1185509A2 (en) * | 1999-05-24 | 2002-03-13 | Cor Therapeutics, Inc. | INHIBITORS OF FACTOR Xa |
| EP1288202A4 (en) | 2000-05-11 | 2003-07-02 | Banyu Pharma Co Ltd | N-acyltetrahydroisoquinoline derivatives |
| US6677354B2 (en) * | 2000-06-16 | 2004-01-13 | Smithkline Beecham P.L.C. | Piperdines for use as orexin receptor antagonists |
| JP4246490B2 (ja) | 2000-11-28 | 2009-04-02 | スミスクライン ビーチャム ピー エル シー | オレキシン受容体のアンタゴニストとしてのモルホリン誘導体 |
| WO2002051232A2 (en) | 2000-12-27 | 2002-07-04 | Actelion Pharmaceuticals Ltd. | Novel benzazepines and related heterocyclic derivatives |
| IL158463A0 (en) * | 2001-05-05 | 2004-05-12 | Smithkline Beecham Plc | N-aroyl cyclic amines |
| US20040192673A1 (en) * | 2001-05-05 | 2004-09-30 | Pascale Gaillard | 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 |
| US7279578B2 (en) | 2002-10-11 | 2007-10-09 | Actelion Pharmaceuticals Ltd. | Sulfonylamino-acetic acid derivatives |
| GB0225938D0 (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 |
| GB0225884D0 (en) * | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| WO2004052876A1 (en) | 2002-12-12 | 2004-06-24 | Janssen Pharmaceutica, N.V. | Substituted 4-phenyl-[1,3]-dioxanes |
| MXPA05010137A (es) | 2003-03-26 | 2005-11-16 | Actelion Pharmaceuticals Ltd | Derivados de tetrahidroisoquinolil acetamida para usarse como antagonistas del receptor de orexina. |
| DE602004011204T2 (de) | 2003-04-28 | 2008-12-24 | Actelion Pharmaceuticals Ltd. | Quinoxalin-3-on-verdindungen als orexin-rezeptor antagonisten. |
| 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 |
| PT1751111E (pt) | 2004-03-01 | 2015-04-01 | Actelion Pharmaceuticals Ltd | Derivados de 1,2,3,4-tetrahidroisoquinolina substituída |
| WO2006067224A2 (en) | 2004-12-23 | 2006-06-29 | Biovitrum Ab (Publ) | Spiro-benzodioxole and spiro-benzodioxane compounds as orexin receptor antagonists |
| WO2006110626A1 (en) | 2005-04-12 | 2006-10-19 | Merck & Co., Inc. | Amidopropoxyphenyl orexin receptor antagonists |
| JP2008541698A (ja) | 2005-05-03 | 2008-11-27 | アンサンブル ディスカバリー コーポレイション | 核酸検出のためのターンオーバープローブおよびその使用 |
| WO2006127550A1 (en) | 2005-05-23 | 2006-11-30 | Merck & Co., Inc. | Proline bis-amide orexin receptor antagonists |
| JP2009503106A (ja) | 2005-08-04 | 2009-01-29 | メルク エンド カムパニー インコーポレーテッド | アミノエタンスルホンアミドオレキシン受容体アンタゴニスト |
| 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 |
| AU2006316321A1 (en) | 2005-11-22 | 2007-05-31 | Merck & Co., Inc. | 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 |
| WO2007126934A2 (en) | 2006-03-29 | 2007-11-08 | Merck & Co., Inc. | Amidoethylthioether orexin receptor antagonists |
| CA2646917A1 (en) | 2006-04-11 | 2007-10-18 | Actelion Pharmaceuticals Ltd | Novel sulfonamide compounds |
| ATE496051T1 (de) | 2006-04-26 | 2011-02-15 | Actelion Pharmaceuticals Ltd | Pyrazolotetrahydropyridinderivate als orexinrezeptorantagonisten |
| WO2007143813A1 (en) | 2006-06-16 | 2007-12-21 | Husky Injection Molding Systems Ltd. | Preventative maintenance update system |
| PL2049529T3 (pl) | 2006-07-14 | 2011-01-31 | Merck Sharp & Dohme | Podstawione związki diazepanowe - antagoniści receptora oreksyny |
| CA2657787A1 (en) | 2006-07-14 | 2008-01-17 | Merck And Co., Inc. | 2-substituted proline bis-amide orexin receptor antagonists |
| CA2657623A1 (en) | 2006-07-14 | 2008-01-17 | Merck & Co., Inc. | Bridged diazepan orexin receptor antagonists |
| DE602007012910D1 (de) | 2006-08-15 | 2011-04-14 | Actelion Pharmaceuticals Ltd | Azetidinverbindungen als orexin-rezeptor-antagonisten |
| 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 |
| CA2669060A1 (en) | 2006-12-01 | 2008-06-05 | Actelion Pharmaceuticals Ltd | Piperidine compounds |
| PE20081229A1 (es) | 2006-12-01 | 2008-08-28 | Merck & Co Inc | Antagonistas de receptor de orexina de diazepam sustituido |
| ATE545647T1 (de) | 2006-12-22 | 2012-03-15 | Actelion Pharmaceuticals Ltd | 5,6,7,8-tetrahydro-imidazoä1,5-aüpyrazinderivat |
| CL2007003827A1 (es) | 2006-12-28 | 2008-09-26 | Actelion Pharmaceuticals Ltd | Compuestos derivados de n-(2-aza-biciclo(3.1.0)hex-3-ilmetil)amida; y su uso para prevenir o tratar la depresion, neurosis, esquizofrenia, ansiedad, adicciones, epilepsia, dolor, enfermedades cardiacas, entre otras. |
| WO2008087611A2 (en) * | 2007-01-19 | 2008-07-24 | Actelion Pharmaceuticals Ltd | Pyrrolidine- and piperidine- bis-amide derivatives |
| US8410142B2 (en) | 2007-03-02 | 2013-04-02 | Merck Sharp & Dohme Corp. | Bipyridine carboxamide orexin receptor antagonists |
| CN101627007A (zh) | 2007-03-05 | 2010-01-13 | 弗·哈夫曼-拉罗切有限公司 | 用作食欲肽拮抗剂的氨基酰胺 |
| WO2008110488A1 (en) | 2007-03-15 | 2008-09-18 | F. Hoffmann-La Roche Ag | Malonamides as orexin antagonists |
| 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. |
| CN101646668A (zh) | 2007-04-04 | 2010-02-10 | 弗·哈夫曼-拉罗切有限公司 | 作为食欲肽拮抗剂的杂环类 |
| ATE483707T1 (de) | 2007-05-14 | 2010-10-15 | Actelion Pharmaceuticals Ltd | 2-cyclopropylthiazolderivate |
| CA2688776A1 (en) | 2007-05-18 | 2008-11-27 | Merck & Co., Inc. | Oxo bridged diazepan orexin receptor antagonists |
| WO2008150364A1 (en) | 2007-05-23 | 2008-12-11 | Merck & Co., Inc. | Cyclopropyl pyrrolidine orexin receptor antagonists |
| JP4881476B2 (ja) | 2007-05-23 | 2012-02-22 | メルク・シャープ・エンド・ドーム・コーポレイション | ピリジルピペリジン・オレキシン受容体アンタゴニスト |
| ATE524466T1 (de) * | 2007-07-03 | 2011-09-15 | Actelion Pharmaceuticals Ltd | 3-azabicycloä3.3.0üoktanverbindungen |
| KR20100046047A (ko) | 2007-07-27 | 2010-05-04 | 액테리온 파마슈티칼 리미티드 | 2-아자-비시클로[3.3.0]옥탄 유도체 |
| CA2693817A1 (en) | 2007-07-27 | 2009-02-05 | Actelion Pharmaceuticals Ltd | Trans-3-aza-bicyclo[3.1.0]hexane derivatives |
| US20090036422A1 (en) | 2007-08-02 | 2009-02-05 | Henner Knust | Monoamide derivatives as orexin receptor antagonists |
| US8003797B2 (en) | 2007-08-09 | 2011-08-23 | Merck Sharp & Dohme Corp. | Pyridine carboxamide orexin receptor antagonists |
| CA2695742C (en) | 2007-08-10 | 2012-11-27 | Rudolf Mueller | Bicyclic amides for enhancing glutamatergic synaptic responses |
| AU2008288151A1 (en) | 2007-08-15 | 2009-02-19 | Actelion Pharmaceuticals Ltd | 1,2-diamido-ethylene derivatives as orexin antagonists |
| WO2009040730A2 (en) | 2007-09-24 | 2009-04-02 | Actelion Pharmaceuticals Ltd | Pyrrolidines and piperidines as orexin receptor antagonists |
| EP2214676B1 (en) | 2007-10-29 | 2012-11-21 | Merck Sharp & Dohme Corp. | Substituted diazepan orexin receptor antagonists |
| EP2231155A4 (en) | 2007-12-18 | 2011-09-14 | Concert Pharmaceuticals Inc | Tetrahydroisoquinoline DERIVATIVES |
| CN101903372B (zh) | 2007-12-21 | 2014-06-18 | 弗·哈夫曼-拉罗切有限公司 | 作为食欲肽受体拮抗剂的杂芳基衍生物 |
| ATE511500T1 (de) | 2008-01-21 | 2011-06-15 | Hoffmann La Roche | Sulfonamide als orexin-antagonisten |
| EP2252587B1 (en) | 2008-02-12 | 2011-07-20 | F. Hoffmann-La Roche AG | Piperidine sulfonamide derivatives |
| MX2010008993A (es) | 2008-02-21 | 2010-09-07 | Actelion Pharmaceuticals Ltd | Derivados de 2-aza-biciclo-[2.2.1]heptano. |
| GB0806536D0 (en) * | 2008-04-10 | 2008-05-14 | Glaxo Group Ltd | Novel compounds |
| JP2011522878A (ja) | 2008-06-11 | 2011-08-04 | アクテリオン ファーマシューティカルズ リミテッド | オレキシン受容体拮抗薬としてのテトラゾール化合物 |
| MX2010013192A (es) | 2008-06-16 | 2010-12-17 | Hoffmann La Roche | Monoamidas heteroaromaticas como antagonistas de receptor orexinina. |
| 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 |
| ES2386526T3 (es) | 2008-07-29 | 2012-08-22 | F. Hoffmann-La Roche Ag | Pirrolidin-3-ilmetilaminas, como antagonistas 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 |
| KR20110071004A (ko) | 2008-10-14 | 2011-06-27 | 액테리온 파마슈티칼 리미티드 | 페네틸아미드 유도체 및 이의 헤테로시클릭 유사체 |
| EP2349269A4 (en) | 2008-10-21 | 2012-04-25 | Merck Sharp & Dohme | 2,5-DISUBSTITUTED PIPERIDINOREXINE RECEPTOR ANTAGONISTS |
| AU2009307913A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| AU2009307918A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,4-disubstituted pyrrolidine orexin receptor antagonists |
| JP2012506379A (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 | 二置換アゼパンオレキシン受容体アンタゴニスト |
| EP2350061B1 (en) | 2008-10-21 | 2013-08-14 | Merck Sharp & Dohme Corp. | 2,3-disubstituted piperidine orexin receptor antagonists |
| AU2009307916A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted morpholine orexin receptor antagonists |
| US8703770B2 (en) | 2008-10-30 | 2014-04-22 | Merck Sharp & Dohme Corp. | Pyridazine carboxamide orexin receptor antagonists |
| JP5635991B2 (ja) | 2008-10-30 | 2014-12-03 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | イソニコチンアミドオレキシン受容体アンタゴニスト |
| US8399494B2 (en) | 2008-10-30 | 2013-03-19 | Merck Sharp & Dohme Corp. | 2,5-disubstituted phenyl carboxamide orexin receptor antagonists |
| WO2010060472A1 (en) | 2008-11-26 | 2010-06-03 | Glaxo Group Limited | Imidazopyridazine derivatives acting as orexin antagonists |
| 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 |
| JP2012509910A (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 |
| JP2012510494A (ja) | 2008-12-02 | 2012-05-10 | グラクソ グループ リミテッド | Ｎ−｛［（ｉｒ、４ｓ、６ｒ）−３−（２−ピリジニルカルボニル）−３−アザビシクロ［４．１．０］ヘプタ−４−イル］メチル｝−２−ヘテロアリールアミン誘導体およびその使用 |
| AR074426A1 (es) | 2008-12-02 | 2011-01-19 | Glaxo Group Ltd | Compuesto de n-(((1s,4s,6s)-3-(2-piridinilcarbonil)3-azabiciclo (4,1.0)hept-4-il) metil)-2-heteroarilamina, su uso para la prepracion de un medicamento para el tratamiento de una enfermedad que requiere un antagonista de un receptor de orexina humana y composicion farmaceutica que lo comprende |
| 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 |
| AR077525A1 (es) | 2009-01-30 | 2011-09-07 | Novartis Ag | 4-aril-butan-1,3-diamidas y composiciones farmaceuticas |
| WO2010122151A1 (en) | 2009-04-24 | 2010-10-28 | Glaxo Group Limited | 3 -azabicyclo [4.1.0] heptanes used as orexin antagonists |
| US20120101106A1 (en) | 2009-07-09 | 2012-04-26 | Mercer Swati P | 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 |
| WO2011023585A1 (en) * | 2009-08-24 | 2011-03-03 | Glaxo Group Limited | Piperidine derivatives used as orexin antagonists |
| WO2011023578A1 (en) * | 2009-08-24 | 2011-03-03 | Glaxo Group Limited | 5-methyl-piperidine derivatives as orexin receptor antagonists for the treatment of sleep disorder |
| 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 |
| ES2585806T3 (es) | 2009-10-23 | 2016-10-10 | Janssen Pharmaceutica N.V. | Octahidropirrolo [3,4-c] pirroles disustituidos como moduladores de receptores 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 |
| EP2516437B1 (en) | 2009-12-21 | 2014-01-29 | Novartis AG | Disubstituted heteroaryl-fused pyridines |
| ES2459496T3 (es) | 2009-12-21 | 2014-05-09 | Novartis Ag | Diaza-espiro[5.5]undecanos como antagonistas del receptor de orexina |
| WO2011138265A2 (en) | 2010-05-03 | 2011-11-10 | Evotec Ag | Indole and indazole derivatives as orexin receptor antagonists |
| WO2011138266A1 (en) | 2010-05-03 | 2011-11-10 | Evotec Ag | Indolizine and imidazopyridine derivatives as orexin receptor antagonists |
| PH12013501206A1 (en) | 2010-12-17 | 2018-04-11 | Taisho Pharmaceutical Co Ltd | Pyrazole derivative |
| US20120165331A1 (en) | 2010-12-22 | 2012-06-28 | Sangamesh Badiger | Di/tri-aza-spiro-C9-C11alkanes |
| US20120165339A1 (en) | 2010-12-22 | 2012-06-28 | Eisai R&D Management Co., Ltd. | Cyclopropane derivatives |
| WO2012085852A1 (en) | 2010-12-22 | 2012-06-28 | Actelion Pharmaceuticals Ltd | 3,8-diaza-bicyclo[4.2.0]oct-8-yl amides |
| 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 |
| KR101873083B1 (ko) | 2011-02-18 | 2018-06-29 | 이도르시아 파마슈티컬스 리미티드 | 오렉신 길항제로서 유용한 신규 피라졸 및 이미다졸 유도체 |
| 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 |
| EP2708537A4 (en) | 2011-05-10 | 2014-10-01 | Taisho Pharmaceutical Co Ltd | HETEROAROMATIC RING DERIVATIVE |
| EP2730573A4 (en) | 2011-07-05 | 2014-12-03 | Taisho Pharmaceutical Co Ltd | METHYLPIPERIDINDERIVAT |
| 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 |
| US9029364B2 (en) | 2011-10-21 | 2015-05-12 | Merck Sharp & Dohme Corp. | 2,5-disubstituted thiomorpholine orexin receptor antagonists |
| EP2771001A4 (en) | 2011-10-25 | 2015-03-25 | Merck Sharp & Dohme | PIPERIDINYL-alkyne-orexin |
| WO2013062858A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Isoxazolopyridine orexin receptor antagonists |
| TWI565703B (zh) | 2011-11-08 | 2017-01-11 | 艾克泰聯製藥有限公司 | ２-（１，２，３-三唑-２-基）苯甲醯胺及３-（１，２，３-三唑-２-基）吡啶醯胺衍生物 |
| ITMI20112329A1 (it) | 2011-12-21 | 2013-06-22 | Rottapharm Spa | Nuovi derivati spiro amminici |
| ES2672732T3 (es) | 2012-02-07 | 2018-06-15 | Eolas Therapeutics Inc. | Prolinas/piperidinas sustituidas como antagonistas del receptor de orexina |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| JP6147279B2 (ja) | 2012-02-17 | 2017-06-14 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | オレキシン−２受容体アンタゴニストの合成において有用な方法および化合物 |
| 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 |
| WO2015123355A1 (en) | 2014-02-12 | 2015-08-20 | Eolas Therapeutics, Inc. | Substituted prolines / piperidines as orexin receptor antagonists |
-
2013
- 2013-02-06 ES ES13746989.6T patent/ES2672732T3/es active Active
- 2013-02-06 CN CN201380018420.6A patent/CN104220065A/zh active Pending
- 2013-02-06 SG SG11201404738QA patent/SG11201404738QA/en unknown
- 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 MX MX2014009281A patent/MX2014009281A/es unknown
- 2013-02-06 AU AU2013217323A patent/AU2013217323A1/en not_active Abandoned
- 2013-02-06 RU RU2014136339A patent/RU2014136339A/ru not_active Application Discontinuation
- 2013-02-06 CA CA2863413A patent/CA2863413A1/en not_active Abandoned
- 2013-02-06 WO PCT/US2013/024903 patent/WO2013119639A1/en not_active Ceased
- 2013-02-06 BR BR112014019426A patent/BR112014019426A8/pt not_active IP Right Cessation
- 2013-02-06 KR KR1020147025072A patent/KR20140124398A/ko not_active Withdrawn
- 2013-02-06 HK HK15105691.4A patent/HK1204955A1/xx unknown
- 2013-02-06 EP EP13746989.6A patent/EP2811997B1/en active Active
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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
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- 2015-02-11 AR ARP150100403A patent/AR099466A1/es unknown
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2016
- 2016-10-20 US US15/299,230 patent/US9896452B2/en not_active Expired - Fee Related
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