AR089361A1 - Derivados de quinolina como inhibidores de la enzima pde10a - Google Patents
Derivados de quinolina como inhibidores de la enzima pde10aInfo
- Publication number
- AR089361A1 AR089361A1 ARP120104861A ARP120104861A AR089361A1 AR 089361 A1 AR089361 A1 AR 089361A1 AR P120104861 A ARP120104861 A AR P120104861A AR P120104861 A ARP120104861 A AR P120104861A AR 089361 A1 AR089361 A1 AR 089361A1
- Authority
- AR
- Argentina
- Prior art keywords
- present
- compounds
- inhibitors
- het
- cyano
- Prior art date
Links
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
- C07D471/02—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
- A61K31/495—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
- A61K31/435—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
- A61K31/505—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
- 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
La presente proporciona derivados de quinolina de fórmula (1) que son inhibidores de la enzima PDE10A y, como tales, son útiles para tratar trastornos psiquiátricos y neurodegenerativos. En especial, la presente proporciona compuestos que son altamente selectivos para PDE10 respecto de otros subtipos de PDE. La presente proporciona además composiciones farmacéuticas que comprenden compuestos de la presente y métodos para tratar trastornos empleando los compuestos de la presente. Reivindicación 1: Un compuesto que tiene la estructura de fórmula (1) donde R¹, R², R³, R⁴, R⁵ y R⁶ se seleccionan en forma individual del grupo integrado por hidrógeno, hidroxilo, ciano, alquilo C₁₋₆, alcoxi C₁₋₆, halógeno, metilendioxi, difluorometilendioxi y etilendioxi, donde -L- es un conector seleccionado entre -CH₂-CH₂- y -CH=CH-, donde HET se selecciona del grupo de formulas (2), donde uno o varios de los hidrógenos unidos a carbono en el HET pueden estar opcionalmente sustituidos con hasta tres sustituyentes R⁷, R⁸ y R⁹ seleccionados de manera individual de alquilo C₁₋₆, halógeno, ciano, haloalquilo C₁₋₆, arilo, alcoxi e hidroxialquilo C₁₋₆, y donde * señala el punto de unión; y sus tautómeros y sales farmacéuticamente aceptables, y sus formas polimórficas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201100990 | 2011-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR089361A1 true AR089361A1 (es) | 2014-08-20 |
Family
ID=48667762
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120104861A AR089361A1 (es) | 2011-12-21 | 2012-12-20 | 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) | BR112014015192A2 (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) | PH12014501434B1 (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 |
|---|---|---|---|---|
| AR089361A1 (es) | 2011-12-21 | 2014-08-20 | Lundbeck & Co As H | Derivados de quinolina como inhibidores de la enzima pde10a |
| CN105051042A (zh) * | 2012-11-29 | 2015-11-11 | 桑诺维恩药品公司 | 适用于治疗中枢神经系统病症的三唑并-吡嗪衍生物 |
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 |
| CA2530317A1 (en) | 2003-06-30 | 2005-01-13 | Altana Pharma Ag | Pyrrolodihydroisoquinolines useful in the treatment of cancer |
| US20070105840A1 (en) | 2003-06-30 | 2007-05-10 | Altana Pharma Ag | Pyrrolo-dihydroisoquinoline derivatives as pde10 inhibitors |
| EP1651251A4 (en) | 2003-07-31 | 2008-06-18 | Bayer Pharmaceuticals Corp | METHOD FOR THE TREATMENT OF DIABETES AND RELATED DISEASES USING PDE 10A INHIBITORS |
| WO2005082883A2 (en) | 2004-02-18 | 2005-09-09 | Pfizer Products Inc. | Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline |
| JP2008501776A (ja) | 2004-06-07 | 2008-01-24 | ファイザー・プロダクツ・インク | 肥満に関連し、かつメタボリックシンドロームに関連する状態の治療としてのホスホジエステラーゼ１０の阻害 |
| 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 |
| UA102693C2 (ru) | 2008-06-20 | 2013-08-12 | Х. Луннбек А/С | Производные фенилимидазола как ингибиторы фермента pde10a |
| 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 |
| MX351368B (es) * | 2010-05-26 | 2017-10-12 | Sunovion Pharmaceuticals Inc | Compuestos heteroarilo y metodos para utilizarlos. |
| AR089361A1 (es) | 2011-12-21 | 2014-08-20 | Lundbeck & Co As H | Derivados de quinolina como inhibidores de la enzima pde10a |
-
2012
- 2012-12-20 AR ARP120104861A patent/AR089361A1/es unknown
- 2012-12-20 TW TW101148618A patent/TWI570124B/zh not_active IP Right Cessation
- 2012-12-21 GE GEAP201213526A patent/GEP201706657B/en unknown
- 2012-12-21 AU AU2012356885A patent/AU2012356885B2/en not_active Ceased
- 2012-12-21 AP AP2014007697A patent/AP2014007697A0/xx unknown
- 2012-12-21 MD MDA20140070A patent/MD20140070A2/ro not_active Application Discontinuation
- 2012-12-21 KR KR1020147019800A patent/KR20140105574A/ko not_active Application Discontinuation
- 2012-12-21 JP JP2014548059A patent/JP6073918B2/ja not_active Expired - Fee Related
- 2012-12-21 EP EP12815695.7A patent/EP2794606A1/en not_active Withdrawn
- 2012-12-21 BR BR112014015192A patent/BR112014015192A2/pt active Search and Examination
- 2012-12-21 WO PCT/EP2012/076590 patent/WO2013092974A1/en active Application Filing
- 2012-12-21 CA CA2859702A patent/CA2859702A1/en not_active Abandoned
- 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 PE PE2014000989A patent/PE20141945A1/es not_active Application Discontinuation
- 2012-12-21 CN CN201280069658.7A patent/CN104114554A/zh active Pending
- 2012-12-21 UA UAA201407913A patent/UA111871C2/uk unknown
- 2012-12-21 RU RU2014127984A patent/RU2624440C2/ru not_active IP Right Cessation
- 2012-12-21 US US14/305,736 patent/US9216986B1/en not_active Expired - Fee Related
- 2012-12-21 MX MX2014007409A patent/MX348792B/es active IP Right Grant
- 2012-12-21 MY MYPI2014001793A patent/MY165216A/en unknown
-
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 CO CO14134658A patent/CO6990727A2/es unknown
- 2014-06-20 ZA ZA2014/04533A patent/ZA201404533B/en unknown
- 2014-06-20 PH PH12014501434A patent/PH12014501434B1/en unknown
- 2014-07-11 MA MA37201A patent/MA35860B1/fr unknown
- 2014-07-18 EC ECIEPI201410000A patent/ECSP14010000A/es unknown
-
2015
- 2015-04-02 HK HK15103345.9A patent/HK1202861A1/xx unknown
- 2015-11-13 US US14/940,272 patent/US9801878B2/en not_active Expired - Fee Related
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