AR065904A1 - Heterociclos como antagonistas de orexina - Google Patents
Heterociclos como antagonistas de orexinaInfo
- Publication number
- AR065904A1 AR065904A1 ARP080101356A ARP080101356A AR065904A1 AR 065904 A1 AR065904 A1 AR 065904A1 AR P080101356 A ARP080101356 A AR P080101356A AR P080101356 A ARP080101356 A AR P080101356A AR 065904 A1 AR065904 A1 AR 065904A1
- Authority
- AR
- Argentina
- Prior art keywords
- halogen
- lower alkyl
- compounds
- lower alkoxy
- substituted
- Prior art date
Links
- SDCMHPPKMQZPPJ-UHFFFAOYSA-N 3-phenyl-4h-quinazoline Chemical compound C1=NC2=CC=CC=C2CN1C1=CC=CC=C1 SDCMHPPKMQZPPJ-UHFFFAOYSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 102000002512 Orexin Human genes 0.000 abstract 1
- 229940123730 Orexin receptor antagonist Drugs 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 230000007246 mechanism Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 108060005714 orexin Proteins 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Addiction (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Psychology (AREA)
- Emergency Medicine (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente se refiere a compuestos de la formula 1 en la que R1 y R2 son con independencia entre sí hidrogeno o alquilo inferior; R3 con independencia del numero de sustituyentes es hidrogeno, halogeno, alquilo inferior, alquilo inferior sustituidopor halogeno, alcoxi inferior o alcoxi inferior sustituido por halogeno; R4 es halogeno, alquilo inferior, alquilo inferior sustituido por halogeno, alcoxi inferior o alcoxi inferior sustituido por halogeno; hetarilo es un anillo heteroaromático quetiene uno o dos ciclos, está conectado a los átomos de carbono del resto piperidina y se elige entre el grupo formado por el grupo de formulas (2) o a las sales de adicion de ácido farmacéuticamente idoneas, los enantiomeros opticamente puros, losracematos o mezclas diastereoméricas del mismo. Se ha encontrado que los compuestos de la formula 1 son antagonistas de receptor de orexina y los compuestos en cuestion pueden ser utiles para el tratamiento de trastornos, en los que intervienen losmecanismos de la orexina, por ejemplo los trastornos del sueno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07105596 | 2007-04-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR065904A1 true AR065904A1 (es) | 2009-07-08 |
Family
ID=39469467
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080101356A AR065904A1 (es) | 2007-04-04 | 2008-04-01 | Heterociclos como antagonistas de orexina |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8067598B2 (es) |
| EP (1) | EP2144906B1 (es) |
| JP (1) | JP2010523518A (es) |
| KR (1) | KR101158976B1 (es) |
| CN (1) | CN101646668A (es) |
| AR (1) | AR065904A1 (es) |
| AT (1) | ATE512963T1 (es) |
| AU (1) | AU2008235528B2 (es) |
| CA (1) | CA2681163A1 (es) |
| CL (1) | CL2008000957A1 (es) |
| ES (1) | ES2365444T3 (es) |
| IL (1) | IL200781A0 (es) |
| MX (1) | MX2009010727A (es) |
| PE (1) | PE20081900A1 (es) |
| TW (1) | TW200845973A (es) |
| WO (1) | WO2008122513A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009097995A1 (de) * | 2008-02-07 | 2009-08-13 | Sanofi-Aventis | Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2011005636A1 (en) * | 2009-07-09 | 2011-01-13 | Merck Sharp & Dohme Corp. | Tetrahydronapthyridine orexin receptor antagonists |
| EP2504316A1 (en) | 2009-11-23 | 2012-10-03 | MSD Oss B.V. | Heterocylic compounds as antagonists of the orexin receptors |
| US20120101110A1 (en) * | 2010-10-26 | 2012-04-26 | Sangamesh Badiger | Diaza-spiro[5.5]undecanes |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| HK1204955A1 (zh) | 2012-02-07 | 2015-12-11 | Eolas Therapeutics Inc. | 取代的脯氨酸/哌啶用作食慾素受體拮抗劑 |
| US10221170B2 (en) | 2014-08-13 | 2019-03-05 | Eolas Therapeutics, Inc. | Difluoropyrrolidines as orexin receptor modulators |
| PL3414241T3 (pl) | 2016-02-12 | 2022-10-03 | Astrazeneca Ab | Piperydyny podstawione halo jako modulatory receptora oreksyny |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20070087103A (ko) * | 2000-03-14 | 2007-08-27 | 액테리온 파마슈티칼 리미티드 | 1,2,3,4-테트라하이드로이소퀴놀린 유도체 |
| WO2002051232A2 (en) * | 2000-12-27 | 2002-07-04 | Actelion Pharmaceuticals Ltd. | Novel benzazepines and related heterocyclic derivatives |
| JP3876872B2 (ja) * | 2002-10-15 | 2007-02-07 | ソニーケミカル&インフォメーションデバイス株式会社 | エレクトロルミネスセンスポリマー、ビスフルオレニルシラン化合物及び有機el素子 |
| MXPA05010137A (es) * | 2003-03-26 | 2005-11-16 | Actelion Pharmaceuticals Ltd | Derivados de tetrahidroisoquinolil acetamida para usarse como antagonistas del receptor de orexina. |
| WO2005118548A1 (en) | 2004-03-01 | 2005-12-15 | Actelion Pharmaceuticals Ltd | Substituted 1,2,3,4-tetrahydroisoquinoline derivatives |
| AU2007226203A1 (en) * | 2006-03-15 | 2007-09-20 | Actelion Pharmaceuticals Ltd | Tetrahydroisoquinoline derivatives to enhance memory function |
| CA2647077A1 (en) * | 2006-04-26 | 2007-11-01 | Actelion Pharmaceuticals Ltd | Pyrazolo-tetrahydro pyridine derivatives as orexin receptor antagonists |
-
2008
- 2008-03-26 CA CA002681163A patent/CA2681163A1/en not_active Abandoned
- 2008-03-26 KR KR1020097020475A patent/KR101158976B1/ko not_active Expired - Fee Related
- 2008-03-26 WO PCT/EP2008/053545 patent/WO2008122513A1/en not_active Ceased
- 2008-03-26 AT AT08718218T patent/ATE512963T1/de active
- 2008-03-26 AU AU2008235528A patent/AU2008235528B2/en not_active Ceased
- 2008-03-26 CN CN200880010269A patent/CN101646668A/zh active Pending
- 2008-03-26 ES ES08718218T patent/ES2365444T3/es active Active
- 2008-03-26 MX MX2009010727A patent/MX2009010727A/es active IP Right Grant
- 2008-03-26 JP JP2010501480A patent/JP2010523518A/ja not_active Ceased
- 2008-03-26 EP EP08718218A patent/EP2144906B1/en not_active Not-in-force
- 2008-03-27 US US12/056,324 patent/US8067598B2/en not_active Expired - Fee Related
- 2008-04-01 AR ARP080101356A patent/AR065904A1/es unknown
- 2008-04-01 TW TW097111894A patent/TW200845973A/zh unknown
- 2008-04-02 CL CL200800957A patent/CL2008000957A1/es unknown
- 2008-04-03 PE PE2008000605A patent/PE20081900A1/es not_active Application Discontinuation
-
2009
- 2009-09-07 IL IL200781A patent/IL200781A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2008235528A1 (en) | 2008-10-16 |
| US8067598B2 (en) | 2011-11-29 |
| TW200845973A (en) | 2008-12-01 |
| ES2365444T3 (es) | 2011-10-05 |
| WO2008122513A1 (en) | 2008-10-16 |
| KR101158976B1 (ko) | 2012-06-21 |
| CL2008000957A1 (es) | 2008-10-10 |
| MX2009010727A (es) | 2009-10-26 |
| CA2681163A1 (en) | 2008-10-16 |
| EP2144906A1 (en) | 2010-01-20 |
| JP2010523518A (ja) | 2010-07-15 |
| PE20081900A1 (es) | 2009-01-26 |
| KR20090127313A (ko) | 2009-12-10 |
| EP2144906B1 (en) | 2011-06-15 |
| CN101646668A (zh) | 2010-02-10 |
| ATE512963T1 (de) | 2011-07-15 |
| AU2008235528B2 (en) | 2012-11-08 |
| IL200781A0 (en) | 2010-05-17 |
| US20080249125A1 (en) | 2008-10-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |