AR101155A1 - Quinazolin-thf-aminas halogenadas como inhibidores de pde1 - Google Patents
Quinazolin-thf-aminas halogenadas como inhibidores de pde1Info
- Publication number
- AR101155A1 AR101155A1 ARP150101009A ARP150101009A AR101155A1 AR 101155 A1 AR101155 A1 AR 101155A1 AR P150101009 A ARP150101009 A AR P150101009A AR P150101009 A ARP150101009 A AR P150101009A AR 101155 A1 AR101155 A1 AR 101155A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- fluorine
- chlorine
- cycloalkyl
- Prior art date
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Classifications
-
- 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
- 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
- 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 proporciona quinazolin-THF-aminas halogenadas como inhibidores de PDE1 y su uso como un medicamento, en particular para el tratamiento de trastornos neurodegenerativos y trastornos psiquiátricos. Reivindicación 1: Un compuesto que tiene la estructura de fórmula (1), donde X es halógeno, preferentemente flúor o cloro o bromo; R¹ se selecciona del grupo constituido por H y alquilo C₁₋₃, donde el alquilo puede estar sustituido opcionalmente una, dos o tres veces con flúor; R² se selecciona del grupo constituido por H y alquilo C₁₋₄, donde el alquilo C₁₋₄ está sustituido opcionalmente una o más veces con uno o más sustituyentes seleccionados independientemente del grupo constituido por fenilo, heteroarilo monocíclico de 5 ó 6 miembros, cicloalquilo C₃₋₆, flúor, cloro y alcoxi de la forma -OR¹⁰, donde R¹⁰ es alquilo C₁₋₅; o R² junto con R⁹ y los átomos que los conectan forman un anillo de cinco miembros saturado; R³ se selecciona del grupo constituido por H y alquilo C₁₋₆, donde el alquilo C₁₋₆ esta sustituido opcionalmente una o más veces con uno o más sustituyentes seleccionados independientemente del grupo constituido por fenilo, heteroarilo monocíclico de 5 ó 6 miembros, cicloalquilo C₃₋₆, flúor, cloro y alcoxi de la forma -OR¹⁰, donde R¹⁰ es alquilo C₁₋₅; R⁴ y R⁵, independientemente el uno del otro, se seleccionan del grupo constituido por H, alquilo C₁₋₆, cicloalquilo C₃₋₆, flúor, cloro, hidroxi y alcoxi de la forma -OR¹⁰, donde el alquilo C₁₋₆ está sustituido opcionalmente una o más veces con uno o más sustituyentes seleccionados independientemente del grupo constituido por fenilo, heteroarilo monocíclico de 5 ó 6 miembros, cicloalquilo C₃₋₆, flúor, cloro y alcoxi de la forma -OR¹⁰, donde R¹⁰ es alquilo C₁₋₅; R⁶ y R⁷, independientemente el uno del otro, se seleccionan del grupo constituido por H y alquilo C₁₋₆, donde el alquilo C₁₋₆ está sustituido opcionalmente una o más veces con uno o más sustituyentes seleccionados independientemente del grupo constituido por cicloalquilo C₃₋₆, flúor, cloro y alcoxi de la forma -OR¹⁰, donde R¹⁰ es alquilo C₁₋₅; R⁸ y R⁹, independientemente el uno del otro, se seleccionan del grupo constituido por H y alquilo C₁₋₆, donde R⁹, cuando R⁹ es un alquilo C₁₋₆, puede formar un anillo alifático de cinco miembros saturado con R², donde el alquilo C₁₋₆ está sustituido opcionalmente una o más veces con uno o más sustituyentes seleccionados independientemente del grupo constituido por cicloalquilo C₃₋₆, flúor, cloro y alcoxi de la forma -OR¹⁰, donde R¹⁰ es alquilo C₁₋₅; y sales de adición de ácido farmacéuticamente aceptables del compuesto de fórmula (1), mezclas racémicas del compuesto de fórmula (1), o el isómero óptico y/o enantiómero correspondiente del compuesto de fórmula (1), y formas polimórficas del compuesto de fórmula (1), así como también formas tautoméricas del compuesto de fórmula (1).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201400194 | 2014-04-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR101155A1 true AR101155A1 (es) | 2016-11-30 |
Family
ID=52779655
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150101009A AR101155A1 (es) | 2014-04-04 | 2015-04-01 | Quinazolin-thf-aminas halogenadas como inhibidores de pde1 |
Country Status (38)
| 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 (1) | 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) |
| SV (1) | SV2016005297A (es) |
| TW (1) | TWI664178B (es) |
| UA (1) | UA119166C2 (es) |
| WO (1) | WO2015150254A1 (es) |
| ZA (1) | ZA201606566B (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3126354T3 (da) | 2014-04-04 | 2020-03-09 | H Lundbeck As | Halogenerede quinazolin-thf-aminer som pde1-inhibitorer |
| JP7111720B2 (ja) | 2016-12-28 | 2022-08-02 | ダート・ニューロサイエンス・エルエルシー | Ｐｄｅ２阻害剤としての置換ピラゾロピリミジノン化合物 |
| CA3120971A1 (en) * | 2017-11-27 | 2019-05-31 | Dart Neuroscience, Llc | Substituted furanopyrimidine compounds as pde1 inhibitors |
| 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 |
| EP2480537A1 (en) * | 2009-09-24 | 2012-08-01 | Basf Se | Aminoquinazoline compounds for combating invertebrate pests |
| 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 |
| EA032559B1 (ru) | 2014-04-04 | 2019-06-28 | Пфайзер Инк. | Бициклические аннелированные гетероарильные или арильные соединения и их применение в качестве ингибиторов irak4 |
| DK3126354T3 (da) | 2014-04-04 | 2020-03-09 | H Lundbeck As | Halogenerede quinazolin-thf-aminer som pde1-inhibitorer |
| 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 |
| 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 |
| CA2944256A1 (en) | 2014-04-04 | 2015-10-08 | F. Hoffmann-La Roche Ag | 5,6-disubstituted pyridine-2-carboxamides as cannabinoid receptor agonists |
| MX2016012689A (es) | 2014-04-04 | 2016-12-14 | Hoffmann La Roche | Piridin-2-amidas utiles como agonistas del receptor 2 cannabinoide (cb2). |
-
2015
- 2015-03-27 DK DK15713186.3T patent/DK3126354T3/da active
- 2015-03-27 PT PT157131863T patent/PT3126354T/pt unknown
- 2015-03-27 JP JP2016560728A patent/JP6554116B2/ja active Active
- 2015-03-27 SI SI201531112T patent/SI3126354T1/sl unknown
- 2015-03-27 LT LTEP15713186.3T patent/LT3126354T/lt unknown
- 2015-03-27 RU RU2016138743A patent/RU2692808C2/ru active
- 2015-03-27 CA CA2943011A patent/CA2943011A1/en not_active Abandoned
- 2015-03-27 RS RS20200239A patent/RS60017B1/sr unknown
- 2015-03-27 CN CN201580017454.2A patent/CN106132953B/zh active Active
- 2015-03-27 MX MX2016012955A patent/MX364519B/es active IP Right Grant
- 2015-03-27 EA EA201691773A patent/EA032579B1/ru not_active IP Right Cessation
- 2015-03-27 UA UAA201610191A patent/UA119166C2/uk unknown
- 2015-03-27 SG SG11201608190YA patent/SG11201608190YA/en unknown
- 2015-03-27 MA MA39837A patent/MA39837B1/fr unknown
- 2015-03-27 WO PCT/EP2015/056713 patent/WO2015150254A1/en active Application Filing
- 2015-03-27 EP EP15713186.3A patent/EP3126354B1/en active Active
- 2015-03-27 CN CN201910110735.2A patent/CN109999039A/zh active Pending
- 2015-03-27 US US15/301,210 patent/US10005764B2/en active Active
- 2015-03-27 AU AU2015239696A patent/AU2015239696B2/en not_active Ceased
- 2015-03-27 ES ES15713186T patent/ES2776359T3/es active Active
- 2015-03-27 PL PL15713186T patent/PL3126354T3/pl unknown
- 2015-03-27 GE GEAP201514286A patent/GEP20186920B/en unknown
- 2015-03-27 CR CR20160463A patent/CR20160463A/es unknown
- 2015-03-27 AP AP2016009521A patent/AP2016009521A0/en unknown
- 2015-03-27 PE PE2016001906A patent/PE20161380A1/es unknown
- 2015-03-27 KR KR1020167027262A patent/KR20160138084A/ko not_active Application Discontinuation
- 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
-
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 CL CL2016002515A patent/CL2016002515A1/es unknown
- 2016-10-03 SV SV2016005297A patent/SV2016005297A/es unknown
- 2016-10-03 GT GT201600213A patent/GT201600213A/es unknown
- 2016-10-20 EC ECIEPI201682599A patent/ECSP16082599A/es unknown
-
2018
- 2018-06-13 US US16/007,561 patent/US10526319B2/en active Active
-
2020
- 2020-03-04 HR HRP20200369TT patent/HRP20200369T1/hr unknown
- 2020-03-04 CY CY20201100196T patent/CY1122784T1/el unknown
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