PE20161380A1 - Quinazolin-thf-aminas halogenadas como inhibidores de pde1 - Google Patents
Quinazolin-thf-aminas halogenadas como inhibidores de pde1Info
- Publication number
- PE20161380A1 PE20161380A1 PE2016001906A PE2016001906A PE20161380A1 PE 20161380 A1 PE20161380 A1 PE 20161380A1 PE 2016001906 A PE2016001906 A PE 2016001906A PE 2016001906 A PE2016001906 A PE 2016001906A PE 20161380 A1 PE20161380 A1 PE 20161380A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- optionally substituted
- quinazolin
- thf
- fluoro
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed 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
- A61K31/495—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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61P25/14—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
- A61P25/24—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- 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
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
La presente invencion se refiere a compuestos quinazolin-THF-aminas halogenadas de formula (I) donde: X es halogeno tal como F, Cl, o Br; R1 es H o alquilo C1-C3 opcionalmente sustituido con fluor; R2 es H o alquilo C1-C4 opcionalmente sustituido o R2 y R9 forman un anillo de 5 miembros; R3 es H o alquilo C1-C6 opcionalmente sustituido; R4 y R5 son H, alquilo C1-C6 opcionalmente sustituido, entre otros; R6 y R7 son H o alquilo C1-C6 opcionalmente sustituido, entre otros; R8 y R9 son H o alquilo C1-C6. Son compuestos preferidos: 8-fluoro-7-metoxi-N-(3-metiltetrahidrofuran-3-il)quinazolin-4-amina; 8-fluoro-7-metoxi-N-metil-N-(tetrahidrofuran-3-il)quinazolin-4-amina; entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos inhiben la enzima fosfodiesterasa 1 (PDE1) siendo utiles para el tratamiento de trastornos neurodegenerativos y psiquiatricos
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201400194 | 2014-04-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20161380A1 true PE20161380A1 (es) | 2017-01-15 |
Family
ID=52779655
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016001906A PE20161380A1 (es) | 2014-04-04 | 2015-03-27 | Quinazolin-thf-aminas halogenadas como inhibidores de pde1 |
Country Status (39)
| Country | Link |
|---|---|
| US (2) | US10005764B2 (es) |
| EP (1) | EP3126354B1 (es) |
| JP (1) | JP6554116B2 (es) |
| KR (1) | KR20160138084A (es) |
| CN (2) | CN106132953B (es) |
| AP (1) | AP2016009521A0 (es) |
| AR (1) | AR101155A1 (es) |
| AU (1) | AU2015239696B2 (es) |
| CA (1) | CA2943011A1 (es) |
| CL (1) | CL2016002515A1 (es) |
| CR (1) | CR20160463A (es) |
| CY (1) | CY1122784T1 (es) |
| DK (1) | DK3126354T3 (es) |
| DO (1) | DOP2016000263A (es) |
| EA (1) | EA032579B1 (es) |
| EC (1) | ECSP16082599A (es) |
| ES (1) | ES2776359T3 (es) |
| GE (2) | GEP20186920B (es) |
| GT (1) | GT201600213A (es) |
| HR (1) | HRP20200369T1 (es) |
| IL (1) | IL248078B (es) |
| JO (1) | JO3628B1 (es) |
| LT (1) | LT3126354T (es) |
| MA (1) | MA39837B1 (es) |
| MX (1) | MX364519B (es) |
| PE (1) | PE20161380A1 (es) |
| PH (1) | PH12016501938A1 (es) |
| PL (1) | PL3126354T3 (es) |
| PT (1) | PT3126354T (es) |
| RS (1) | RS60017B1 (es) |
| RU (1) | RU2692808C2 (es) |
| SG (1) | SG11201608190YA (es) |
| SI (1) | SI3126354T1 (es) |
| SM (1) | SMT202000132T1 (es) |
| SV (1) | SV2016005297A (es) |
| TW (1) | TWI664178B (es) |
| UA (1) | UA119166C2 (es) |
| WO (1) | WO2015150254A1 (es) |
| ZA (1) | ZA201606566B (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3126354B1 (en) | 2014-04-04 | 2020-01-22 | H. Lundbeck A/S | Halogenated quinazolin-thf-amines as pde1 inhibitors |
| KR102590848B1 (ko) | 2016-12-28 | 2023-10-19 | 다트 뉴로사이언스, 엘엘씨 | Pde2 억제제로서 치환된 피라졸로피리미디논 화합물 |
| ES2902365T3 (es) * | 2017-11-27 | 2022-03-28 | Dart Neuroscience Llc | Compuestos de furanopirimidina sustituidos como inhibidores de PDE1 |
| AU2019275453B2 (en) | 2018-05-25 | 2023-12-21 | Intra-Cellular Therapies, Inc. | Organic compounds |
| JP7706375B2 (ja) | 2019-04-12 | 2025-07-11 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 有機化合物 |
| CN117105809B (zh) * | 2023-10-20 | 2024-05-03 | 中国农业大学 | 一种苯甲酰苯胺化合物及其制备方法和应用 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10042058A1 (de) * | 2000-08-26 | 2002-03-07 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| GB0229281D0 (en) * | 2002-12-16 | 2003-01-22 | Novartis Ag | Organic compounds |
| CN1784391B (zh) * | 2003-03-03 | 2010-06-09 | 沃泰克斯药物股份有限公司 | 可用作离子通道调控剂的喹唑啉 |
| GB0327319D0 (en) * | 2003-11-24 | 2003-12-24 | Pfizer Ltd | Novel pharmaceuticals |
| US20060019975A1 (en) * | 2004-07-23 | 2006-01-26 | Pfizer Inc | Novel piperidyl derivatives of quinazoline and isoquinoline |
| US20060183763A1 (en) * | 2004-12-31 | 2006-08-17 | Pfizer Inc | Novel pyrrolidyl derivatives of heteroaromatic compounds |
| EP1996587A1 (en) * | 2006-02-23 | 2008-12-03 | Pfizer Products Incorporated | Substituted quinazolines as pde10 inhibitors |
| US20070265258A1 (en) | 2006-03-06 | 2007-11-15 | Ruiping Liu | Quinazoline derivatives as phosphodiesterase 10 inhibitors |
| JP2013505909A (ja) * | 2009-09-24 | 2013-02-21 | ビーエーエスエフ ソシエタス・ヨーロピア | 無脊椎動物害虫を駆除するためのアミノキナゾリン化合物 |
| US20130116241A1 (en) * | 2011-11-09 | 2013-05-09 | Abbvie Inc. | Novel inhibitor compounds of phosphodiesterase type 10a |
| TW201609713A (zh) * | 2013-12-19 | 2016-03-16 | Ｈ 朗德貝克公司 | 作爲ｐｄｅ１抑制劑之喹唑啉－ｔｈｆ－胺 |
| TW201611834A (en) | 2014-02-07 | 2016-04-01 | Lundbeck & Co As H | Hexahydrofuropyrroles as PDE1 inhibitors |
| AR099937A1 (es) | 2014-04-04 | 2016-08-31 | Sanofi Sa | Compuestos de isoindolinona como moduladores de gpr119 para el tratamiento de diabetes, obesidad, dislipidemia y trastornos relacionados |
| MA39843A (fr) | 2014-04-04 | 2017-02-08 | Hoffmann La Roche | Pyridine-2-amides utiles comme agonistes de cb2 |
| RS58597B1 (sr) | 2014-04-04 | 2019-05-31 | Pfizer | Biciklično-spojena heteroaril ili aril jedinjenja i njihova upotreba kao irak4 inhibitora |
| AR099936A1 (es) | 2014-04-04 | 2016-08-31 | Sanofi Sa | Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y trastornos relacionados |
| EP3126354B1 (en) | 2014-04-04 | 2020-01-22 | H. Lundbeck A/S | Halogenated quinazolin-thf-amines as pde1 inhibitors |
| SG11201608246VA (en) | 2014-04-04 | 2016-10-28 | Hoffmann La Roche | 5,6-disubstituted pyridine-2-carboxamides as cannabinoid receptor agonists |
-
2015
- 2015-03-27 EP EP15713186.3A patent/EP3126354B1/en active Active
- 2015-03-27 UA UAA201610191A patent/UA119166C2/uk unknown
- 2015-03-27 SI SI201531112T patent/SI3126354T1/sl unknown
- 2015-03-27 CR CR20160463A patent/CR20160463A/es unknown
- 2015-03-27 AP AP2016009521A patent/AP2016009521A0/en unknown
- 2015-03-27 SG SG11201608190YA patent/SG11201608190YA/en unknown
- 2015-03-27 US US15/301,210 patent/US10005764B2/en active Active
- 2015-03-27 JP JP2016560728A patent/JP6554116B2/ja not_active Expired - Fee Related
- 2015-03-27 AU AU2015239696A patent/AU2015239696B2/en not_active Ceased
- 2015-03-27 PL PL15713186T patent/PL3126354T3/pl unknown
- 2015-03-27 GE GEAP201514286A patent/GEP20186920B/en unknown
- 2015-03-27 CN CN201580017454.2A patent/CN106132953B/zh active Active
- 2015-03-27 PE PE2016001906A patent/PE20161380A1/es unknown
- 2015-03-27 LT LTEP15713186.3T patent/LT3126354T/lt unknown
- 2015-03-27 GE GEAP201814286A patent/GEAP201814286A/en unknown
- 2015-03-27 SM SM20200132T patent/SMT202000132T1/it unknown
- 2015-03-27 RS RS20200239A patent/RS60017B1/sr unknown
- 2015-03-27 EA EA201691773A patent/EA032579B1/ru not_active IP Right Cessation
- 2015-03-27 HR HRP20200369TT patent/HRP20200369T1/hr unknown
- 2015-03-27 PT PT157131863T patent/PT3126354T/pt unknown
- 2015-03-27 DK DK15713186.3T patent/DK3126354T3/da active
- 2015-03-27 MX MX2016012955A patent/MX364519B/es active IP Right Grant
- 2015-03-27 CA CA2943011A patent/CA2943011A1/en not_active Abandoned
- 2015-03-27 WO PCT/EP2015/056713 patent/WO2015150254A1/en not_active Ceased
- 2015-03-27 RU RU2016138743A patent/RU2692808C2/ru active
- 2015-03-27 KR KR1020167027262A patent/KR20160138084A/ko not_active Ceased
- 2015-03-27 ES ES15713186T patent/ES2776359T3/es active Active
- 2015-03-27 CN CN201910110735.2A patent/CN109999039A/zh active Pending
- 2015-03-27 MA MA39837A patent/MA39837B1/fr unknown
- 2015-03-30 JO JOP/2015/0058A patent/JO3628B1/ar active
- 2015-03-31 TW TW104110439A patent/TWI664178B/zh not_active IP Right Cessation
- 2015-04-01 AR ARP150101009A patent/AR101155A1/es unknown
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2016
- 2016-09-22 ZA ZA2016/06566A patent/ZA201606566B/en unknown
- 2016-09-27 IL IL248078A patent/IL248078B/en active IP Right Grant
- 2016-09-27 DO DO2016000263A patent/DOP2016000263A/es unknown
- 2016-09-29 PH PH12016501938A patent/PH12016501938A1/en unknown
- 2016-10-03 GT GT201600213A patent/GT201600213A/es unknown
- 2016-10-03 SV SV2016005297A patent/SV2016005297A/es unknown
- 2016-10-03 CL CL2016002515A patent/CL2016002515A1/es unknown
- 2016-10-20 EC ECIEPI201682599A patent/ECSP16082599A/es unknown
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2018
- 2018-06-13 US US16/007,561 patent/US10526319B2/en active Active
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2020
- 2020-03-04 CY CY20201100196T patent/CY1122784T1/el unknown
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