PE20151069A1 - Nuevos compuestos inhibidores de la fosfodiesterasa del tipo 10a - Google Patents
Nuevos compuestos inhibidores de la fosfodiesterasa del tipo 10aInfo
- Publication number
- PE20151069A1 PE20151069A1 PE2015000204A PE2015000204A PE20151069A1 PE 20151069 A1 PE20151069 A1 PE 20151069A1 PE 2015000204 A PE2015000204 A PE 2015000204A PE 2015000204 A PE2015000204 A PE 2015000204A PE 20151069 A1 PE20151069 A1 PE 20151069A1
- Authority
- PE
- Peru
- Prior art keywords
- disorders
- formula
- new type
- inhibiting compounds
- compounds
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 title abstract 2
- 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 150000001204 N-oxides Chemical class 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
Classifications
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61P25/18—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
- A61P25/24—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
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Addiction (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
La invencion se refiere a compuestos de la formula (I), N-oxidos, tautomeros, prodrogas y sales farmaceuticamente aceptables de los mismos, a donde en la formula l las variables R1, R2, R3, R4 y R5 son como se definen en las reivindicaciones y donde X es C-R6 o N, Y es C-R7 o N, donde R6 y R7 son, entre otros, hidrogeno, halogeno, alcoxi, haloalcoxi y semejantes. Los compuestos de la formula l, los N-oxidos, los tautomeros, las prodrogas y las sales farmaceuticamente aceptables de los mismos son inhibidores de la fosfodiesterasa de tipo 10A y su uso en la elaboracion de un medicamento los vuelve adecuados para tratar o controlar los trastornos medicos seleccionados entre trastornos neurologicos y trastornos psiquiatricos, para aliviar los sintomas asociados con dichos trastornos y para reducir el riesgo de dicho trastornos
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261684290P | 2012-08-17 | 2012-08-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20151069A1 true PE20151069A1 (es) | 2015-08-29 |
Family
ID=48986145
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015000204A PE20151069A1 (es) | 2012-08-17 | 2013-08-16 | Nuevos compuestos inhibidores de la fosfodiesterasa del tipo 10a |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US9464085B2 (es) |
| EP (1) | EP2885299B1 (es) |
| JP (1) | JP2015524833A (es) |
| KR (1) | KR20150042798A (es) |
| CN (1) | CN104684912A (es) |
| AR (1) | AR092167A1 (es) |
| AU (1) | AU2013304043A1 (es) |
| BR (1) | BR112015003236A2 (es) |
| CA (1) | CA2879485A1 (es) |
| CL (1) | CL2015000370A1 (es) |
| CR (1) | CR20150082A (es) |
| DO (1) | DOP2015000029A (es) |
| EC (1) | ECSP15010205A (es) |
| HK (1) | HK1211284A1 (es) |
| IL (1) | IL236946A0 (es) |
| IN (1) | IN2015DN00337A (es) |
| MX (1) | MX2015002000A (es) |
| PE (1) | PE20151069A1 (es) |
| PH (1) | PH12015500348A1 (es) |
| RU (1) | RU2015109135A (es) |
| SG (1) | SG11201501111YA (es) |
| TW (1) | TW201412742A (es) |
| UY (1) | UY34980A (es) |
| WO (1) | WO2014027078A1 (es) |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030032579A1 (en) | 2001-04-20 | 2003-02-13 | Pfizer Inc. | Therapeutic use of selective PDE10 inhibitors |
| US20030166476A1 (en) | 2002-01-31 | 2003-09-04 | Winemiller Mark D. | Lubricating oil compositions with improved friction properties |
| WO2005012485A2 (en) | 2003-07-31 | 2005-02-10 | Bayer Pharmaceuticals Corporation | Methods for treating diabetes and related disorders using pde10a inhibitors |
| US20090075980A1 (en) | 2003-10-03 | 2009-03-19 | Coley Pharmaceutical Group, Inc. | Pyrazolopyridines and Analogs Thereof |
| EP1755611A1 (en) | 2004-06-07 | 2007-02-28 | Pfizer Products Inc. | Phosphodiesterase 10 inhibition as treatment for obesity-related and metabolic syndrome-related conditions |
| AU2005282721A1 (en) | 2004-09-03 | 2006-03-16 | Memory Pharmaceuticals Corporation | 4-substituted 4, 6-dialkoxy-cinnoline derivatives as phospodiesterase 10 inhibitors for the treatment of psychiatric or neurological syndroms |
| JP2009504759A (ja) | 2005-08-16 | 2009-02-05 | メモリ ファーマセチカル コーポレーション | ホスホジエステラーゼ１０阻害剤 |
| NL2000397C2 (nl) | 2006-01-05 | 2007-10-30 | Pfizer Prod Inc | Bicyclische heteroarylverbindingen als PDE10 inhibitoren. |
| WO2007082546A1 (en) | 2006-01-20 | 2007-07-26 | H. Lundbeck A/S | Use of tofisopam as a pde10a inhibitor |
| BRPI0707223A2 (pt) | 2006-01-27 | 2011-04-26 | Pfizer Prod Inc | compostos de derivados de aminoftalazina |
| WO2007098169A1 (en) | 2006-02-21 | 2007-08-30 | Amgen Inc. | Cinnoline derivatives as phosphodiesterase 10 inhibitors |
| JP2009527562A (ja) | 2006-02-21 | 2009-07-30 | アムゲン インコーポレイティッド | ホスホジエステラーゼ１０阻害剤としてのシンノリン誘導体 |
| WO2007096743A1 (en) | 2006-02-23 | 2007-08-30 | Pfizer Products Inc. | Substituted quinazolines as pde10 inhibitors |
| AU2007221049A1 (en) | 2006-02-28 | 2007-09-07 | Amgen Inc. | Cinnoline and quinazoline derivates as phosphodiesterase 10 inhibitors |
| US20070265258A1 (en) | 2006-03-06 | 2007-11-15 | Ruiping Liu | Quinazoline derivatives as phosphodiesterase 10 inhibitors |
| WO2007103554A1 (en) | 2006-03-08 | 2007-09-13 | Amgen Inc. | Quinoline and isoquinoline derivatives as phosphodiesterase 10 inhibitors |
| TW200817400A (en) * | 2006-05-30 | 2008-04-16 | Elbion Ag | Pyrido [3,2-e] pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them |
| TW200815436A (en) | 2006-05-30 | 2008-04-01 | Elbion Ag | 4-amino-pyrido[3,2-e]pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them |
| WO2008001182A1 (en) | 2006-06-26 | 2008-01-03 | Pfizer Products Inc. | Tricyclic heteroaryl compounds as pde10 inhibitors |
| US20080090834A1 (en) | 2006-07-06 | 2008-04-17 | Pfizer Inc | Selective azole pde10a inhibitor compounds |
| US8492394B2 (en) | 2006-07-10 | 2013-07-23 | H. Lundbeck A/S | (3-aryl-piperazin-1-yl), (2-aryl-morpholin-4-yl) and (2-aryl-thiomorpholin-4-yl) derivatives of 6,7-dialkoxy-quinazoline, 6,7-dialkoxyphtalazine and 6,7-dialkoxyisoquinoline as PDE10A enzyme inhibitors |
| WO2008020302A2 (en) | 2006-08-17 | 2008-02-21 | Pfizer Products Inc. | Heteroaromatic quinoline-based compounds as phosphodiesterase (pde) inhibitors |
| WO2009025823A1 (en) | 2007-08-21 | 2009-02-26 | Amgen Inc. | Phosphodiesterase 10 inhibitors |
| US20090062291A1 (en) | 2007-08-22 | 2009-03-05 | Essa Hu | Phosphodiesterase 10 inhibitors |
| WO2009029214A1 (en) | 2007-08-23 | 2009-03-05 | Amgen Inc. | Isoquinolone derivatives as phosphodiesterase 10 inhibitors |
| TW200918519A (en) | 2007-09-19 | 2009-05-01 | Lundbeck & Co As H | Cyanoisoquinoline |
| WO2009068246A2 (en) | 2007-11-30 | 2009-06-04 | Elbion Gmbh | Methods of treating obesity and metabolic disorders |
| WO2009068320A1 (en) | 2007-11-30 | 2009-06-04 | Elbion Gmbh | Aryl and heteroaryl fused imidazo (1,5-a) pyrazines as inhibitors of phosphodiesterase 10 |
| US20090143361A1 (en) | 2007-11-30 | 2009-06-04 | Elbion Gmbh | Pyrido[3,2-E]Pyrazines, Process For Preparing The Same, And Their Use As Inhibitors Of Phosphodiesterase 10 |
| WO2009070584A1 (en) | 2007-11-30 | 2009-06-04 | Wyeth | Aryl and heteroaryl fused imidazo[1,5-a]pyrazines as inhibitors of phosphodiesterase 10 |
| WO2010054260A1 (en) | 2008-11-07 | 2010-05-14 | Biotie Therapies Gmbh | Imidazo[5,1-c][1,2,4]benzotriazine derivatives as inhibitors of phosphodiesterases |
| WO2011008597A1 (en) | 2009-07-14 | 2011-01-20 | Schering Corporation | Dihydroimidazoisoquinoline derivatives useful as pde10 inhibitors |
| TW201204727A (en) | 2010-03-10 | 2012-02-01 | Kalypsys Inc | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
| DE102010025786A1 (de) | 2010-07-01 | 2012-01-05 | Merck Patent Gmbh | Pyrazolochinoline |
-
2013
- 2013-08-15 US US13/968,242 patent/US9464085B2/en not_active Expired - Fee Related
- 2013-08-15 UY UY0001034980A patent/UY34980A/es not_active Application Discontinuation
- 2013-08-16 WO PCT/EP2013/067122 patent/WO2014027078A1/en not_active Ceased
- 2013-08-16 EP EP13750071.6A patent/EP2885299B1/en not_active Not-in-force
- 2013-08-16 AU AU2013304043A patent/AU2013304043A1/en not_active Abandoned
- 2013-08-16 CA CA2879485A patent/CA2879485A1/en not_active Abandoned
- 2013-08-16 BR BR112015003236A patent/BR112015003236A2/pt not_active IP Right Cessation
- 2013-08-16 TW TW102129554A patent/TW201412742A/zh unknown
- 2013-08-16 PE PE2015000204A patent/PE20151069A1/es not_active Application Discontinuation
- 2013-08-16 MX MX2015002000A patent/MX2015002000A/es unknown
- 2013-08-16 RU RU2015109135A patent/RU2015109135A/ru not_active Application Discontinuation
- 2013-08-16 AR ARP130102932A patent/AR092167A1/es unknown
- 2013-08-16 HK HK15111990.0A patent/HK1211284A1/xx unknown
- 2013-08-16 JP JP2015526996A patent/JP2015524833A/ja not_active Withdrawn
- 2013-08-16 IN IN337DEN2015 patent/IN2015DN00337A/en unknown
- 2013-08-16 KR KR20157004416A patent/KR20150042798A/ko not_active Withdrawn
- 2013-08-16 SG SG11201501111YA patent/SG11201501111YA/en unknown
- 2013-08-16 CN CN201380043926.2A patent/CN104684912A/zh active Pending
-
2015
- 2015-01-27 IL IL236946A patent/IL236946A0/en unknown
- 2015-02-16 CL CL2015000370A patent/CL2015000370A1/es unknown
- 2015-02-16 DO DO2015000029A patent/DOP2015000029A/es unknown
- 2015-02-17 PH PH12015500348A patent/PH12015500348A1/en unknown
- 2015-02-19 CR CR20150082A patent/CR20150082A/es unknown
- 2015-03-17 EC ECIEPI201510205A patent/ECSP15010205A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| UY34980A (es) | 2014-03-31 |
| IL236946A0 (en) | 2015-03-31 |
| EP2885299A1 (en) | 2015-06-24 |
| WO2014027078A1 (en) | 2014-02-20 |
| RU2015109135A (ru) | 2016-10-10 |
| CA2879485A1 (en) | 2014-02-20 |
| CN104684912A (zh) | 2015-06-03 |
| SG11201501111YA (en) | 2015-03-30 |
| US20140051695A1 (en) | 2014-02-20 |
| CL2015000370A1 (es) | 2015-10-02 |
| IN2015DN00337A (es) | 2015-06-12 |
| EP2885299B1 (en) | 2017-04-05 |
| ECSP15010205A (es) | 2016-01-29 |
| TW201412742A (zh) | 2014-04-01 |
| AU2013304043A1 (en) | 2015-02-05 |
| AR092167A1 (es) | 2015-03-25 |
| KR20150042798A (ko) | 2015-04-21 |
| PH12015500348A1 (en) | 2015-04-20 |
| HK1211284A1 (en) | 2016-05-20 |
| US9464085B2 (en) | 2016-10-11 |
| CR20150082A (es) | 2015-05-25 |
| BR112015003236A2 (pt) | 2017-07-04 |
| JP2015524833A (ja) | 2015-08-27 |
| DOP2015000029A (es) | 2015-03-15 |
| MX2015002000A (es) | 2015-10-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |