PE20141945A1 - Derivados de quinolina como inhibidores de la enzima pde10a - Google Patents
Derivados de quinolina como inhibidores de la enzima pde10aInfo
- Publication number
- PE20141945A1 PE20141945A1 PE2014000989A PE2014000989A PE20141945A1 PE 20141945 A1 PE20141945 A1 PE 20141945A1 PE 2014000989 A PE2014000989 A PE 2014000989A PE 2014000989 A PE2014000989 A PE 2014000989A PE 20141945 A1 PE20141945 A1 PE 20141945A1
- Authority
- PE
- Peru
- Prior art keywords
- inhibitors
- quinoline
- pde10a enzyme
- quinoline derivatives
- compounds
- Prior art date
Links
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical class N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 title abstract 3
- 101001072037 Homo sapiens cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 229940027991 antiseptic and disinfectant quinoline derivative Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- TUJKJAMUKRIRHC-UHFFFAOYSA-N hydroxyl Chemical class [OH] TUJKJAMUKRIRHC-UHFFFAOYSA-N 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 229920002554 vinyl polymer Polymers 0.000 abstract 1
Classifications
-
- 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
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61K31/4741—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
- A61P25/18—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
- A61P25/28—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE QUINOLINA DE FORMULA (I) DONDE R1, R2, R3, R4, R5 Y R6 SON CADA UNO H, HIDROXILO, CN, ALCOXI(C1-C6), ENTRE OTROS; L ES UN CONECTOR TAL COMO -CH2-CH2- O -CH=CH-; HET ES UN COMPUESTO DE FORMULA (i), (ii), ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS. SON COMPUESTOS PREFERIDOS: 2-[(E)-2-(5,8-DIMETIL-[1,2,4]TRIAZOLO[1,5-a]PIRAZIN-2-IL)-VINIL]-6-TRIFLUOROMETIL-QUINOLINA; 6-[2-(5,8-DIMETIL-[1,2,4]TRIAZOLO[1,5-a]PIRAZIN-2-IL)-ETIL]-1,3-DIOXOLO[4,5-g]QUINOLINA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ENZIMA PDE10A SIENDO UTILES EN EL TRATAMIENTO DE TRANSTORNOS PSIQUIATRICOS O NEURODEGENERATIVOS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201100990 | 2011-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20141945A1 true PE20141945A1 (es) | 2014-12-18 |
Family
ID=48667762
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2014000989A PE20141945A1 (es) | 2011-12-21 | 2012-12-21 | Derivados de quinolina como inhibidores de la enzima pde10a |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US9216986B1 (es) |
| EP (1) | EP2794606A1 (es) |
| JP (1) | JP6073918B2 (es) |
| KR (1) | KR20140105574A (es) |
| CN (1) | CN104114554A (es) |
| AP (1) | AP2014007697A0 (es) |
| AR (1) | AR089361A1 (es) |
| AU (1) | AU2012356885B2 (es) |
| BR (1) | BR112014015192A8 (es) |
| CA (1) | CA2859702A1 (es) |
| CL (1) | CL2014001643A1 (es) |
| CO (1) | CO6990727A2 (es) |
| CR (1) | CR20140289A (es) |
| DO (1) | DOP2014000141A (es) |
| EA (1) | EA028824B1 (es) |
| EC (1) | ECSP14010000A (es) |
| GE (1) | GEP201706657B (es) |
| HK (1) | HK1202861A1 (es) |
| IL (1) | IL233226A (es) |
| MA (1) | MA35860B1 (es) |
| MD (1) | MD20140070A2 (es) |
| MX (1) | MX348792B (es) |
| MY (1) | MY165216A (es) |
| PE (1) | PE20141945A1 (es) |
| PH (1) | PH12014501434A1 (es) |
| RU (1) | RU2624440C2 (es) |
| SG (1) | SG11201403339YA (es) |
| TN (1) | TN2014000268A1 (es) |
| TW (1) | TWI570124B (es) |
| UA (1) | UA111871C2 (es) |
| WO (1) | WO2013092974A1 (es) |
| ZA (1) | ZA201404533B (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI570124B (zh) | 2011-12-21 | 2017-02-11 | Ｈ 朗德貝克公司 | 作為ｐｄｅ１０ａ酵素抑制劑的喹啉衍生物 |
| US9670230B2 (en) | 2012-11-29 | 2017-06-06 | Sunovion Pharmaceuticals Inc. | Heteroaryl compounds and methods of use thereof |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030032579A1 (en) | 2001-04-20 | 2003-02-13 | Pfizer Inc. | Therapeutic use of selective PDE10 inhibitors |
| KR20060030483A (ko) | 2003-06-30 | 2006-04-10 | 알타나 파마 아게 | Ｐｄｅ10 억제제로서 피롤로디히드로이소퀴놀린 |
| CA2530114A1 (en) | 2003-06-30 | 2005-01-13 | Altana Pharma Ag | Pyrrolo-dihydroisoquinoline derivatives as pde10 inhibitors |
| WO2005012485A2 (en) | 2003-07-31 | 2005-02-10 | Bayer Pharmaceuticals Corporation | Methods for treating diabetes and related disorders using pde10a inhibitors |
| JP2007523152A (ja) | 2004-02-18 | 2007-08-16 | ファイザー・プロダクツ・インク | キナゾリンおよびイソキノリンのテトラヒドロイソキノリニル誘導体 |
| EP1755611A1 (en) | 2004-06-07 | 2007-02-28 | Pfizer Products Inc. | Phosphodiesterase 10 inhibition as treatment for obesity-related and metabolic syndrome-related conditions |
| US20060019975A1 (en) | 2004-07-23 | 2006-01-26 | Pfizer Inc | Novel piperidyl derivatives of quinazoline and isoquinoline |
| 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 |
| US8598355B2 (en) * | 2008-05-14 | 2013-12-03 | Astellas Pharma Inc. | Amide compound |
| TWI501965B (zh) | 2008-06-20 | 2015-10-01 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑之新穎苯基咪唑衍生物 |
| WO2010145668A1 (en) | 2009-06-19 | 2010-12-23 | H. Lundbeck A/S | Novel phenylimidazole derivative as pde10a enzyme inhibitor |
| TWI481607B (zh) | 2009-12-17 | 2015-04-21 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑的２－芳基咪唑衍生物 |
| TWI485151B (zh) | 2009-12-17 | 2015-05-21 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑之雜芳香族苯基咪唑衍生物 |
| JP2011201873A (ja) * | 2010-03-03 | 2011-10-13 | Mitsubishi Tanabe Pharma Corp | 三置換ピリミジン化合物及びそのｐｄｅ１０阻害薬としての使用 |
| CA2800618C (en) * | 2010-05-26 | 2018-08-28 | Sunovion Pharmaceuticals Inc. | Heteroaryl compounds and methods of use thereof |
| TWI570124B (zh) | 2011-12-21 | 2017-02-11 | Ｈ 朗德貝克公司 | 作為ｐｄｅ１０ａ酵素抑制劑的喹啉衍生物 |
-
2012
- 2012-12-20 TW TW101148618A patent/TWI570124B/zh not_active IP Right Cessation
- 2012-12-20 AR ARP120104861A patent/AR089361A1/es unknown
- 2012-12-21 AP AP2014007697A patent/AP2014007697A0/xx unknown
- 2012-12-21 EP EP12815695.7A patent/EP2794606A1/en not_active Withdrawn
- 2012-12-21 MX MX2014007409A patent/MX348792B/es active IP Right Grant
- 2012-12-21 KR KR1020147019800A patent/KR20140105574A/ko not_active Ceased
- 2012-12-21 GE GEAP201213526A patent/GEP201706657B/en unknown
- 2012-12-21 PE PE2014000989A patent/PE20141945A1/es not_active Application Discontinuation
- 2012-12-21 MD MDA20140070A patent/MD20140070A2/ro not_active Application Discontinuation
- 2012-12-21 BR BR112014015192A patent/BR112014015192A8/pt active Search and Examination
- 2012-12-21 HK HK15103345.9A patent/HK1202861A1/xx unknown
- 2012-12-21 MY MYPI2014001793A patent/MY165216A/en unknown
- 2012-12-21 SG SG11201403339YA patent/SG11201403339YA/en unknown
- 2012-12-21 EA EA201491152A patent/EA028824B1/ru not_active IP Right Cessation
- 2012-12-21 AU AU2012356885A patent/AU2012356885B2/en not_active Ceased
- 2012-12-21 WO PCT/EP2012/076590 patent/WO2013092974A1/en not_active Ceased
- 2012-12-21 RU RU2014127984A patent/RU2624440C2/ru not_active IP Right Cessation
- 2012-12-21 UA UAA201407913A patent/UA111871C2/uk unknown
- 2012-12-21 US US14/305,736 patent/US9216986B1/en not_active Expired - Fee Related
- 2012-12-21 CA CA2859702A patent/CA2859702A1/en not_active Abandoned
- 2012-12-21 CN CN201280069658.7A patent/CN104114554A/zh active Pending
- 2012-12-21 JP JP2014548059A patent/JP6073918B2/ja not_active Expired - Fee Related
-
2014
- 2014-06-16 TN TNP2014000268A patent/TN2014000268A1/en unknown
- 2014-06-17 DO DO2014000141A patent/DOP2014000141A/es unknown
- 2014-06-17 CR CR20140289A patent/CR20140289A/es unknown
- 2014-06-18 IL IL233226A patent/IL233226A/en not_active IP Right Cessation
- 2014-06-19 CL CL2014001643A patent/CL2014001643A1/es unknown
- 2014-06-20 PH PH12014501434A patent/PH12014501434A1/en unknown
- 2014-06-20 ZA ZA2014/04533A patent/ZA201404533B/en unknown
- 2014-06-20 CO CO14134658A patent/CO6990727A2/es unknown
- 2014-07-11 MA MA37201A patent/MA35860B1/fr unknown
- 2014-07-18 EC ECIEPI201410000A patent/ECSP14010000A/es unknown
-
2015
- 2015-11-13 US US14/940,272 patent/US9801878B2/en not_active Expired - Fee Related
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |