WO2012089606A1 - Dérivés azabicyclo [4.1.0] hept-4-yle en tant qu'antagonistes du récepteur humain de l'orexine - Google Patents
Dérivés azabicyclo [4.1.0] hept-4-yle en tant qu'antagonistes du récepteur humain de l'orexine Download PDFInfo
- Publication number
- WO2012089606A1 WO2012089606A1 PCT/EP2011/073736 EP2011073736W WO2012089606A1 WO 2012089606 A1 WO2012089606 A1 WO 2012089606A1 EP 2011073736 W EP2011073736 W EP 2011073736W WO 2012089606 A1 WO2012089606 A1 WO 2012089606A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- methyl
- mmol
- pharmaceutically acceptable
- azabicyclo
- disorder
- Prior art date
Links
- 0 CC1(C)OC[C@](CC=C)N1C(C**)=O Chemical compound CC1(C)OC[C@](CC=C)N1C(C**)=O 0.000 description 11
- WCZXECFPTUZDMM-YFKPBYRVSA-N C=CC[C@@H](CO)N Chemical compound C=CC[C@@H](CO)N WCZXECFPTUZDMM-YFKPBYRVSA-N 0.000 description 2
- OFXOXGYVZIPXDB-NSHDSACASA-N CC(C)(C)OC(NCC(N1C(C)(C)OC[C@@H]1CC=C)=O)=O Chemical compound CC(C)(C)OC(NCC(N1C(C)(C)OC[C@@H]1CC=C)=O)=O OFXOXGYVZIPXDB-NSHDSACASA-N 0.000 description 2
- CYGUVCJBXVVHAK-SNAWJCMRSA-N C/C(/C(O)=O)=C(/C(OC)=O)\N=C Chemical compound C/C(/C(O)=O)=C(/C(OC)=O)\N=C CYGUVCJBXVVHAK-SNAWJCMRSA-N 0.000 description 1
- WNNNWFKQCKFSDK-BYPYZUCNSA-N C=CC[C@@H](C(O)=O)N Chemical compound C=CC[C@@H](C(O)=O)N WNNNWFKQCKFSDK-BYPYZUCNSA-N 0.000 description 1
- UEMNCMYSSFWTCS-YFKPBYRVSA-N C=CC[C@@H](CC(O)=O)N Chemical compound C=CC[C@@H](CC(O)=O)N UEMNCMYSSFWTCS-YFKPBYRVSA-N 0.000 description 1
- SSYLTDCVONDKNS-QMMMGPOBSA-N CC(C)(C)OC(N(CC=CC1)[C@@H]1C(O)=O)=O Chemical compound CC(C)(C)OC(N(CC=CC1)[C@@H]1C(O)=O)=O SSYLTDCVONDKNS-QMMMGPOBSA-N 0.000 description 1
- VFGXZEMSDNAXQZ-VIFPVBQESA-N CC(C)(C)OC(N(CC=CC1)[C@@H]1C(OC)=O)=O Chemical compound CC(C)(C)OC(N(CC=CC1)[C@@H]1C(OC)=O)=O VFGXZEMSDNAXQZ-VIFPVBQESA-N 0.000 description 1
- BNBLVDDATMKIKM-AWEZNQCLSA-N CC(C)(C)OC(N1[C@H](CN(C(c2c3cccc2)=O)C3=O)CCC2(CC2)C1)=O Chemical compound CC(C)(C)OC(N1[C@H](CN(C(c2c3cccc2)=O)C3=O)CCC2(CC2)C1)=O BNBLVDDATMKIKM-AWEZNQCLSA-N 0.000 description 1
- LTMIDZWWNNIEPG-VIFPVBQESA-N CC(C)(C)OC(N1[C@H](CO)CC=CC1)=O Chemical compound CC(C)(C)OC(N1[C@H](CO)CC=CC1)=O LTMIDZWWNNIEPG-VIFPVBQESA-N 0.000 description 1
- WKMASGCUWYNSDU-FBKFWFMHSA-N CC(C)(C)OC(N1[C@H](CO)CC[C@H](C2)C2C1)=O Chemical compound CC(C)(C)OC(N1[C@H](CO)CC[C@H](C2)C2C1)=O WKMASGCUWYNSDU-FBKFWFMHSA-N 0.000 description 1
- BZBCPEOLGUYTCB-VIFPVBQESA-N CC(C)(C)OC(NCC(N[C@@H](CC=C)CO)=O)=O Chemical compound CC(C)(C)OC(NCC(N[C@@H](CC=C)CO)=O)=O BZBCPEOLGUYTCB-VIFPVBQESA-N 0.000 description 1
- LJCWRJYVPJJTMB-UHFFFAOYSA-N CC(C)(C)OC(NCC(ON(C(CC1)=O)C1=O)=O)=O Chemical compound CC(C)(C)OC(NCC(ON(C(CC1)=O)C1=O)=O)=O LJCWRJYVPJJTMB-UHFFFAOYSA-N 0.000 description 1
- HWPGPOYMSMWFNB-PVHODMMVSA-N CC(C)(C)[Si](c1ccccc1)(c1ccccc1)OC[C@H](C[C@@H](C1)[C@@H]1C1)N1C(c1nc(C)ccc1-c1ncccn1)=O Chemical compound CC(C)(C)[Si](c1ccccc1)(c1ccccc1)OC[C@H](C[C@@H](C1)[C@@H]1C1)N1C(c1nc(C)ccc1-c1ncccn1)=O HWPGPOYMSMWFNB-PVHODMMVSA-N 0.000 description 1
- NCKJPIPCHXSNTJ-ARTQYDKTSA-N CC1(C)OC[C@H](CC2(C3)C33C2)N1C3=O Chemical compound CC1(C)OC[C@H](CC2(C3)C33C2)N1C3=O NCKJPIPCHXSNTJ-ARTQYDKTSA-N 0.000 description 1
- HZDHEHWWBMEPTP-JVIMKECRSA-N CC1(C)OC[C@H](CC2=C[C@@H]22)N1C2O Chemical compound CC1(C)OC[C@H](CC2=C[C@@H]22)N1C2O HZDHEHWWBMEPTP-JVIMKECRSA-N 0.000 description 1
- LBDBOBOIHMQPRS-BIIVOSGPSA-N CC1(C)OC[C@H](C[C@@H]2[C@H]3C2)N1C3=O Chemical compound CC1(C)OC[C@H](C[C@@H]2[C@H]3C2)N1C3=O LBDBOBOIHMQPRS-BIIVOSGPSA-N 0.000 description 1
- SUWBHOBTIVQHBH-VIFPVBQESA-N CCC(N1C(C)(C)OC[C@@H]1CC=C)=O Chemical compound CCC(N1C(C)(C)OC[C@@H]1CC=C)=O SUWBHOBTIVQHBH-VIFPVBQESA-N 0.000 description 1
- LJLOXXVVYMDCRO-UWVGGRQHSA-N C[C@@H](CC1)C[C@@H](CN)N1C(OC(C)(C)C)=O Chemical compound C[C@@H](CC1)C[C@@H](CN)N1C(OC(C)(C)C)=O LJLOXXVVYMDCRO-UWVGGRQHSA-N 0.000 description 1
- LSXNPNYIMZPUAD-GELOPOQCSA-N Cc(nc1C(N(C[C@@H]2[IH][C@@H]2C2)/C2=C/Nc2nnc(C(F)(F)F)[s]2)=O)ccc1-c1ncccn1 Chemical compound Cc(nc1C(N(C[C@@H]2[IH][C@@H]2C2)/C2=C/Nc2nnc(C(F)(F)F)[s]2)=O)ccc1-c1ncccn1 LSXNPNYIMZPUAD-GELOPOQCSA-N 0.000 description 1
- MAMIGJZTUJBLFS-JADALISFSA-N OC[C@H](CC1(C2)C22C1)NC2=O Chemical compound OC[C@H](CC1(C2)C22C1)NC2=O MAMIGJZTUJBLFS-JADALISFSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La présente invention a pour objet des dérivés azabicyclo [4.1.0] hept-4-yle et leur utilisation en tant que produits pharmaceutiques.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201061427786P | 2010-12-28 | 2010-12-28 | |
| US61/427,786 | 2010-12-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2012089606A1 true WO2012089606A1 (fr) | 2012-07-05 |
Family
ID=45470538
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP2011/073736 WO2012089606A1 (fr) | 2010-12-28 | 2011-12-22 | Dérivés azabicyclo [4.1.0] hept-4-yle en tant qu'antagonistes du récepteur humain de l'orexine |
Country Status (1)
| Country | Link |
|---|---|
| WO (1) | WO2012089606A1 (fr) |
Cited By (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103012293A (zh) * | 2012-12-13 | 2013-04-03 | 同济大学 | 一种抗失眠药物mk-4305中间体的合成方法 |
| WO2014066196A1 (fr) * | 2012-10-23 | 2014-05-01 | Merck Sharp & Dohme Corp. | Antagonistes du récepteur de la 2-pyridyloxy-3-substituée-4-nitrile oréxine |
| US8969352B2 (en) | 2013-03-13 | 2015-03-03 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| US9062078B2 (en) | 2013-03-13 | 2015-06-23 | Janssen Pharmaceutica Nv | Substituted 7-azabicyles and their use as orexin receptor modulators |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| US9499517B2 (en) | 2012-02-07 | 2016-11-22 | Eolas Therapeutics, Inc. | Substituted prolines / piperidines as orexin receptor antagonists |
| US9611251B2 (en) | 2013-03-13 | 2017-04-04 | Janssen Pharmaceutica Nv | Substituted piperidine compounds and their use as orexin receptor modulators |
| US9611262B2 (en) | 2014-09-11 | 2017-04-04 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| WO2017159669A1 (fr) * | 2016-03-15 | 2017-09-21 | 塩野義製薬株式会社 | Procédé de production d'un dérivé de phénoxyéthanol |
| GB2558975A (en) * | 2017-09-01 | 2018-07-25 | Chronos Therapeutics Ltd | New compounds |
| US10221170B2 (en) | 2014-08-13 | 2019-03-05 | Eolas Therapeutics, Inc. | Difluoropyrrolidines as orexin receptor modulators |
| WO2019081575A1 (fr) | 2017-10-27 | 2019-05-02 | Syngenta Participations Ag | Compositions de lutte contre les porteurs, procédés et produits mettant en œuvre celles-ci |
| US10828302B2 (en) | 2016-03-10 | 2020-11-10 | Janssen Pharmaceutica Nv | Methods of treating depression using orexin-2 receptor antagonists |
| US10894789B2 (en) | 2016-02-12 | 2021-01-19 | Astrazeneca Ab | Halo-substituted piperidines as orexin receptor modulators |
| US11059828B2 (en) | 2009-10-23 | 2021-07-13 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo[3,4-C]pyrroles as orexin receptor modulators |
| US11660293B2 (en) | 2017-09-01 | 2023-05-30 | Chronos Therapeutics Limited | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
Citations (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1992001810A1 (fr) | 1990-07-19 | 1992-02-06 | Lerner Michael R | Procedes d'identification de composes agissant comme agonistes ou antagonistes sur des proteines impliquees dans la transduction de signaux biologiques |
| WO1996034877A1 (fr) | 1995-05-05 | 1996-11-07 | Human Genome Sciences, Inc. | Recepteur de neuropeptides humain |
| EP0849361A2 (fr) | 1996-12-17 | 1998-06-24 | Smithkline Beecham Corporation | Nouveaux ligands du recepteur de neuropeptides HFGAN72 |
| EP0875566A2 (fr) | 1997-04-30 | 1998-11-04 | Smithkline Beecham Corporation | Nouveau récepteur couplé à la protéine G |
| EP0875565A2 (fr) | 1997-04-30 | 1998-11-04 | Smithkline Beecham Corporation | Nouveau récepteur couplé à la protéine G (HFGAN72Y) |
| EP0893498A2 (fr) | 1997-07-25 | 1999-01-27 | Smithkline Beecham Corporation | Clone de cADN MY1 codant pour un récepteur 7-transmembranaire humain |
| WO1999009024A1 (fr) | 1997-08-14 | 1999-02-25 | Smithkline Beecham Plc | Derives de phenyluree et de phenylthiouree utilises en tant qu'antagonistes de hfgan72 |
| WO1999058533A1 (fr) | 1998-05-08 | 1999-11-18 | Smithkline Beecham Plc | Derives de phenyluree et de (phenylthio)uree |
| WO2000047576A1 (fr) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Derives de cinnamide utilises en tant qu'antagonistes des recepteurs de l'orexine-1 |
| WO2000047577A1 (fr) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Derives de phenyluree et de phenylthiouree utilises comme antagonistes des recepteurs de l'orexine |
| WO2000047580A2 (fr) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Derives de phenyluree et de phenylthiouree |
| WO2001096302A1 (fr) | 2000-06-16 | 2001-12-20 | Smithkline Beecham P.L.C. | Piperidines utiles en tant qu'antagonistes du recepteur d'orexine |
| WO2002044172A1 (fr) | 2000-11-28 | 2002-06-06 | Smithkline Beecham P.L.C. | Derives de la morpholine utilises comme antagonistes des recepteurs de l'orexine |
| WO2002089800A2 (fr) | 2001-05-05 | 2002-11-14 | Smithkline Beecham P.L.C. | Derives d'amines cycliques n-aroyl utilises comme antagonistes du recepteur d'orexine |
| WO2003002561A1 (fr) | 2001-06-28 | 2003-01-09 | Smithkline Beecham P.L.C. | Derives d'amine cycliques n-aroyle utilises comme antagonistes du recepteur de l'orexine |
| WO2003002559A2 (fr) | 2001-06-28 | 2003-01-09 | Smithkline Beecham P.L.C. | Composes |
| WO2003032991A1 (fr) | 2001-10-11 | 2003-04-24 | Smithkline Beecham Plc | Derives de n-aroylpiperazine utilises comme antagonistes du recepteur de l'orexine |
| WO2003037847A1 (fr) | 2001-11-01 | 2003-05-08 | Smithkline Beecham P.L.C. | Derives de benzamide utilises comme antagonistes des recepteurs de l'orexine |
| WO2003041711A1 (fr) | 2001-11-10 | 2003-05-22 | Smithkline Beecham P.L.C. | Derives bis-amide de piperazine et leur utilisation en tant qu'antagonistes du recepteur d'orexine |
| WO2005118548A1 (fr) | 2004-03-01 | 2005-12-15 | Actelion Pharmaceuticals Ltd | Derives de 1,2,3,4-tétrahydroisoquinoléine substitués |
| WO2008038251A2 (fr) | 2006-09-29 | 2008-04-03 | Actelion Pharmaceuticals Ltd | Dérivés du 3-aza-bicyclo[3.1.0]hexane |
| WO2008150364A1 (fr) * | 2007-05-23 | 2008-12-11 | Merck & Co., Inc. | Antagonistes du récepteur de la cyclopropylpyrrolidine orexine |
| WO2009003993A1 (fr) | 2007-07-03 | 2009-01-08 | Glaxo Group Limited | Dérivés de pipéridine utiles comme antagonistes vis-àvis des récepteurs de l'orexine |
| WO2009003997A1 (fr) | 2007-07-03 | 2009-01-08 | Glaxo Group Limited | Imidazo [1, 2-c] pyrimidin-2-ylméthylpipéridines comme antagonistes vis-à-vis des récepteurs de l'orexine |
| WO2009124956A1 (fr) | 2008-04-10 | 2009-10-15 | Glaxo Group Limited | Dérivés de pyridine utilisés pour traiter des troubles liés aux orexines |
| WO2010063662A1 (fr) * | 2008-12-02 | 2010-06-10 | Glaxo Group Limited | Dérivés de n-{[(1s,4s,6s)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine et leurs utilisations |
| WO2010122151A1 (fr) * | 2009-04-24 | 2010-10-28 | Glaxo Group Limited | 3 -azabicyclo [4.1.0] heptanes utilisés comme antagonistes de l'orexine |
-
2011
- 2011-12-22 WO PCT/EP2011/073736 patent/WO2012089606A1/fr active Application Filing
Patent Citations (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1992001810A1 (fr) | 1990-07-19 | 1992-02-06 | Lerner Michael R | Procedes d'identification de composes agissant comme agonistes ou antagonistes sur des proteines impliquees dans la transduction de signaux biologiques |
| WO1996034877A1 (fr) | 1995-05-05 | 1996-11-07 | Human Genome Sciences, Inc. | Recepteur de neuropeptides humain |
| EP0849361A2 (fr) | 1996-12-17 | 1998-06-24 | Smithkline Beecham Corporation | Nouveaux ligands du recepteur de neuropeptides HFGAN72 |
| EP0875566A2 (fr) | 1997-04-30 | 1998-11-04 | Smithkline Beecham Corporation | Nouveau récepteur couplé à la protéine G |
| EP0875565A2 (fr) | 1997-04-30 | 1998-11-04 | Smithkline Beecham Corporation | Nouveau récepteur couplé à la protéine G (HFGAN72Y) |
| EP0893498A2 (fr) | 1997-07-25 | 1999-01-27 | Smithkline Beecham Corporation | Clone de cADN MY1 codant pour un récepteur 7-transmembranaire humain |
| WO1999009024A1 (fr) | 1997-08-14 | 1999-02-25 | Smithkline Beecham Plc | Derives de phenyluree et de phenylthiouree utilises en tant qu'antagonistes de hfgan72 |
| WO1999058533A1 (fr) | 1998-05-08 | 1999-11-18 | Smithkline Beecham Plc | Derives de phenyluree et de (phenylthio)uree |
| WO2000047576A1 (fr) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Derives de cinnamide utilises en tant qu'antagonistes des recepteurs de l'orexine-1 |
| WO2000047577A1 (fr) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Derives de phenyluree et de phenylthiouree utilises comme antagonistes des recepteurs de l'orexine |
| WO2000047580A2 (fr) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Derives de phenyluree et de phenylthiouree |
| WO2001096302A1 (fr) | 2000-06-16 | 2001-12-20 | Smithkline Beecham P.L.C. | Piperidines utiles en tant qu'antagonistes du recepteur d'orexine |
| WO2002044172A1 (fr) | 2000-11-28 | 2002-06-06 | Smithkline Beecham P.L.C. | Derives de la morpholine utilises comme antagonistes des recepteurs de l'orexine |
| WO2002089800A2 (fr) | 2001-05-05 | 2002-11-14 | Smithkline Beecham P.L.C. | Derives d'amines cycliques n-aroyl utilises comme antagonistes du recepteur d'orexine |
| WO2003002561A1 (fr) | 2001-06-28 | 2003-01-09 | Smithkline Beecham P.L.C. | Derives d'amine cycliques n-aroyle utilises comme antagonistes du recepteur de l'orexine |
| WO2003002559A2 (fr) | 2001-06-28 | 2003-01-09 | Smithkline Beecham P.L.C. | Composes |
| WO2003032991A1 (fr) | 2001-10-11 | 2003-04-24 | Smithkline Beecham Plc | Derives de n-aroylpiperazine utilises comme antagonistes du recepteur de l'orexine |
| WO2003037847A1 (fr) | 2001-11-01 | 2003-05-08 | Smithkline Beecham P.L.C. | Derives de benzamide utilises comme antagonistes des recepteurs de l'orexine |
| WO2003041711A1 (fr) | 2001-11-10 | 2003-05-22 | Smithkline Beecham P.L.C. | Derives bis-amide de piperazine et leur utilisation en tant qu'antagonistes du recepteur d'orexine |
| WO2005118548A1 (fr) | 2004-03-01 | 2005-12-15 | Actelion Pharmaceuticals Ltd | Derives de 1,2,3,4-tétrahydroisoquinoléine substitués |
| WO2008038251A2 (fr) | 2006-09-29 | 2008-04-03 | Actelion Pharmaceuticals Ltd | Dérivés du 3-aza-bicyclo[3.1.0]hexane |
| WO2008150364A1 (fr) * | 2007-05-23 | 2008-12-11 | Merck & Co., Inc. | Antagonistes du récepteur de la cyclopropylpyrrolidine orexine |
| WO2009003993A1 (fr) | 2007-07-03 | 2009-01-08 | Glaxo Group Limited | Dérivés de pipéridine utiles comme antagonistes vis-àvis des récepteurs de l'orexine |
| WO2009003997A1 (fr) | 2007-07-03 | 2009-01-08 | Glaxo Group Limited | Imidazo [1, 2-c] pyrimidin-2-ylméthylpipéridines comme antagonistes vis-à-vis des récepteurs de l'orexine |
| WO2009124956A1 (fr) | 2008-04-10 | 2009-10-15 | Glaxo Group Limited | Dérivés de pyridine utilisés pour traiter des troubles liés aux orexines |
| WO2010063662A1 (fr) * | 2008-12-02 | 2010-06-10 | Glaxo Group Limited | Dérivés de n-{[(1s,4s,6s)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine et leurs utilisations |
| WO2010122151A1 (fr) * | 2009-04-24 | 2010-10-28 | Glaxo Group Limited | 3 -azabicyclo [4.1.0] heptanes utilisés comme antagonistes de l'orexine |
Non-Patent Citations (23)
| Title |
|---|
| "Diagnostic and Statistical Manual of Mental Disorders", AMERICAN PSYCHIATRIC ASSOCIATION |
| BERGE; BIGHLEY; MONKHOUSE, J.PHARM.SCI, vol. 66, 1977, pages 1 - 19 |
| BIOCHEM. PHARMACOL., vol. 22, 1973, pages 3099 - 3108 |
| BORGLAND ET AL., NEURON, vol. 49, no. 4, 2006, pages 589 - 601 |
| BOUTREL ET AL., PROC.NATL.ACAD.SCI., vol. 102, no. 52, 2005 |
| BOWEN WP; JERMAN JC.: "Nonlinear regression using spreadsheets", TRENDS PHARMACOL. SCI., vol. 16, 1995, pages 413 - 417, XP004207565, DOI: doi:10.1016/S0165-6147(00)89091-4 |
| BRISBARE-ROCH ET AL., NATURE MEDICINE, vol. 13, no. 2, 2007, pages 150 - 155 |
| CHEMELLI ET AL., CELL, vol. 98, 1999, pages 437 - 451 |
| HAGAN ET AL., PROC.NATL.ACAD.SCI., vol. 96, 1999, pages 10911 - 10916 |
| HARRI ET AL., NATURE, vol. 437, 2005, pages 556 - 559 |
| LEE ET AL., J. NEUROSCIENCE, vol. 25, 2005, pages 6716 - 6720 |
| NAIR ET AL.: "British Journal of Pharmacology", 28 January 2008 |
| OHNO; SAKURAI, FRONT. NEUROENDOCRINOLOGY, vol. 29, 2008, pages 70 - 87 |
| PEYRON ET AL., J. NEUROSCIENCES, vol. 18, 1998, pages 9996 - 10015 |
| PIPER ET AL., EUROPEAN J NEUROSCIENCE, vol. 12, 2000, pages 726 - 730 |
| SAKURAI, NATURE REVIEWS NEUROSCIENCE, vol. 8, 2007, pages 171 - 181 |
| SAKURAI, T. ET AL., CELL, vol. 92, 1998, pages 573 - 585 |
| SMART ET AL., BRITISH JOURNAL OF PHARMACOLOGY, vol. 128, 1999, pages 1 - 3 |
| SMART; JERMAN, PHARMACOLOGY AND THERAPEUTICS, vol. 94, 2002, pages 51 - 61 |
| SMITH ET AL., NEUROSCIENCE LETTERS, vol. 341, 2003, pages 256 - 258 |
| SULLIVAN E; TUCKER EM; DALE IL.: "Calcium Signaling Protocols.", 1999, HUMANA PRESS, article "Measurement of [Ca2+]¡ using the fluometric imaging plate reader (FLIPR", pages: 125 - 136 |
| WHITE ET AL., PEPTIDES, vol. 26, 2005, pages 2231 - 2238 |
| WILLIE ET AL., ANN. REV. NEUROSCIENCES, vol. 24, 2001, pages 429 - 458 |
Cited By (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11667644B2 (en) | 2009-10-23 | 2023-06-06 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators |
| USRE48841E1 (en) | 2009-10-23 | 2021-12-07 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators |
| US11059828B2 (en) | 2009-10-23 | 2021-07-13 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo[3,4-C]pyrroles as orexin receptor modulators |
| US9499517B2 (en) | 2012-02-07 | 2016-11-22 | Eolas Therapeutics, Inc. | Substituted prolines / piperidines as orexin receptor antagonists |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| US9896452B2 (en) | 2012-02-07 | 2018-02-20 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| US9546152B2 (en) | 2012-10-23 | 2017-01-17 | Merck Sharp & Dohme Corp. | 2-pyridyloxy-3-substituted-4-nitrile orexin receptor antagonists |
| WO2014066196A1 (fr) * | 2012-10-23 | 2014-05-01 | Merck Sharp & Dohme Corp. | Antagonistes du récepteur de la 2-pyridyloxy-3-substituée-4-nitrile oréxine |
| CN103012293A (zh) * | 2012-12-13 | 2013-04-03 | 同济大学 | 一种抗失眠药物mk-4305中间体的合成方法 |
| US10183953B2 (en) | 2013-03-13 | 2019-01-22 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| US9611251B2 (en) | 2013-03-13 | 2017-04-04 | Janssen Pharmaceutica Nv | Substituted piperidine compounds and their use as orexin receptor modulators |
| US9611277B2 (en) | 2013-03-13 | 2017-04-04 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| US9637496B2 (en) | 2013-03-13 | 2017-05-02 | Janssen Pharmaceutica Nv | Substituted 7-azabicycles and their use as orexin receptor modulators |
| US9695183B2 (en) | 2013-03-13 | 2017-07-04 | Janssen Pharmaceutica Nv | Substituted 7-azabicycles and their use as orexin receptor modulators |
| US8969352B2 (en) | 2013-03-13 | 2015-03-03 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| US9845333B2 (en) | 2013-03-13 | 2017-12-19 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| US9447117B2 (en) | 2013-03-13 | 2016-09-20 | Janssen Pharmaceuticals Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| US9062078B2 (en) | 2013-03-13 | 2015-06-23 | Janssen Pharmaceutica Nv | Substituted 7-azabicyles and their use as orexin receptor modulators |
| US9475819B2 (en) | 2013-03-13 | 2016-10-25 | Janssen Pharmaceutica Nv | Substituted 7-azabicycles and their use as orexin receptor modulators |
| US10221170B2 (en) | 2014-08-13 | 2019-03-05 | Eolas Therapeutics, Inc. | Difluoropyrrolidines as orexin receptor modulators |
| US9611262B2 (en) | 2014-09-11 | 2017-04-04 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| US10894789B2 (en) | 2016-02-12 | 2021-01-19 | Astrazeneca Ab | Halo-substituted piperidines as orexin receptor modulators |
| US11434236B2 (en) | 2016-02-12 | 2022-09-06 | Astrazeneca Ab | Halo-substituted piperidines as orexin receptor modulators |
| US11241432B2 (en) | 2016-03-10 | 2022-02-08 | Janssen Pharmaceutica Nv | Methods of treating depression using orexin-2 receptor antagonists |
| US10828302B2 (en) | 2016-03-10 | 2020-11-10 | Janssen Pharmaceutica Nv | Methods of treating depression using orexin-2 receptor antagonists |
| US10472312B2 (en) | 2016-03-15 | 2019-11-12 | Shionogi & Co., Ltd. | Method for producing phenoxyethanol derivative |
| CN108137457A (zh) * | 2016-03-15 | 2018-06-08 | 盐野义制药株式会社 | 苯氧乙醇衍生物的制造方法 |
| EA039048B1 (ru) * | 2016-03-15 | 2021-11-26 | Сионоги Энд Ко., Лтд. | Способ получения производных феноксиэтанола |
| WO2017159669A1 (fr) * | 2016-03-15 | 2017-09-21 | 塩野義製薬株式会社 | Procédé de production d'un dérivé de phénoxyéthanol |
| CN108137457B (zh) * | 2016-03-15 | 2022-09-06 | 盐野义制药株式会社 | 苯氧乙醇衍生物的制造方法 |
| 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 |
| US11660293B2 (en) | 2017-09-01 | 2023-05-30 | Chronos Therapeutics Limited | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
| GB2558975A (en) * | 2017-09-01 | 2018-07-25 | Chronos Therapeutics Ltd | New compounds |
| US11369113B2 (en) | 2017-10-27 | 2022-06-28 | Syngenta Participations Ag | Vector control compositions, methods and products utilizing same |
| WO2019081575A1 (fr) | 2017-10-27 | 2019-05-02 | Syngenta Participations Ag | Compositions de lutte contre les porteurs, procédés et produits mettant en œuvre celles-ci |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| WO2012089606A1 (fr) | Dérivés azabicyclo [4.1.0] hept-4-yle en tant qu'antagonistes du récepteur humain de l'orexine | |
| US8133908B2 (en) | Heteroaryl derivatives of N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-amine | |
| US20120040991A1 (en) | 3-azabicyclo [4.1.0] heptanes used as orexin antagonists | |
| US20110257198A1 (en) | Piperidine derivatives useful as orexin antagonists | |
| US20100144760A1 (en) | Novel compounds | |
| US20110053979A1 (en) | Pyridine derivatives used to treat orexin related disorders | |
| US20100210667A1 (en) | Imidazo [1, 2-c] pyrimidin-2-ylmethylpiperidines as orexin receptor antagonists | |
| US20120095034A1 (en) | Piperidine derivatives useful as orexin receptor antagonists | |
| EP2358711A1 (fr) | Dérivés de la pipéridine utiles en tant qu antagonistes du récepteur de l orexine | |
| EP2358712A1 (fr) | Dérivés de la pipéridine utiles en tant qu antagonistes du récepteur de l orexine | |
| US20120149723A1 (en) | 5-methyl-piperidine derivatives as orexin receptor antagonists for the treatment of sleep disorder | |
| WO2012089607A1 (fr) | Nouveaux composés dotés d'un cœur 3a-azabicyclo[4.1.0]heptane agissant sur les récepteurs d'orexine | |
| US20120149711A1 (en) | Piperidine derivatives used as orexin antagonists |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 121 | Ep: the epo has been informed by wipo that ep was designated in this application |
Ref document number: 11807687 Country of ref document: EP Kind code of ref document: A1 |
|
| NENP | Non-entry into the national phase |
Ref country code: DE |
|
| 122 | Ep: pct application non-entry in european phase |
Ref document number: 11807687 Country of ref document: EP Kind code of ref document: A1 |