MX381326B - Derivados de 7h-imidazo[1-5-a]pirazin-8-ona como inhibidores de la fosfodiesterasa 9(pde9); y el uso de los mismos en el tratamiento de trastornos neurodegenerativos - Google Patents
Derivados de 7h-imidazo[1-5-a]pirazin-8-ona como inhibidores de la fosfodiesterasa 9(pde9); y el uso de los mismos en el tratamiento de trastornos neurodegenerativosInfo
- Publication number
- MX381326B MX381326B MX2019014982A MX2019014982A MX381326B MX 381326 B MX381326 B MX 381326B MX 2019014982 A MX2019014982 A MX 2019014982A MX 2019014982 A MX2019014982 A MX 2019014982A MX 381326 B MX381326 B MX 381326B
- Authority
- MX
- Mexico
- Prior art keywords
- pde9
- inhibitors
- pyrazin
- phosphodiesterase
- imidazo
- Prior art date
Links
- 208000015122 neurodegenerative disease Diseases 0.000 title abstract 2
- 101001117256 Drosophila melanogaster High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A Proteins 0.000 title 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 238000000034 method Methods 0.000 abstract 3
- 101100407341 Drosophila melanogaster Pde9 gene Proteins 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 239000002532 enzyme inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
Classifications
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- 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
- 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
- A61P25/18—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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- 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
- A61P25/36—Opioid-abuse
-
- 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
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invención se dirige a compuestos que son inhibidores de la enzima PDE9. La invención proporciona una composición farmacéutica que comprende una cantidad terapéuticamente eficaz de un compuesto de la invención y un transportador farmacéuticamente aceptable. La presente invención proporciona también procesos para la preparación de los compuestos de fórmula (I). La presente invención proporciona además a un método para tratar un sujeto que padece un trastorno neurodegenerativo que comprende administrar al sujeto una cantidad terapéuticamente eficaz de un compuesto de fórmula (I). La presente invención proporciona además un método para tratar un paciente que padece un trastorno psiquiátrico que comprende administrar al sujeto una cantidad terapéuticamente eficaz de un compuesto de fórmula (I).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011001692 | 2011-10-10 | ||
| PCT/EP2012/069936 WO2013053690A1 (en) | 2011-10-10 | 2012-10-09 | Pde9i with imidazo pyrazinone backbone |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2019014982A MX2019014982A (es) | 2020-02-24 |
| MX381326B true MX381326B (es) | 2025-03-12 |
Family
ID=47019007
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2015004422A MX370433B (es) | 2011-10-10 | 2012-10-09 | Derivados de 7h-imidazo [1-5-a] pirazin-8-ona como inhibidores de la fosfodiasterasa 9(pde9); y el uso de los mismos en el tratamiento de trastornos neurodegenerativos. |
| MX2019014982A MX381326B (es) | 2011-10-10 | 2012-10-09 | Derivados de 7h-imidazo[1-5-a]pirazin-8-ona como inhibidores de la fosfodiesterasa 9(pde9); y el uso de los mismos en el tratamiento de trastornos neurodegenerativos |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2015004422A MX370433B (es) | 2011-10-10 | 2012-10-09 | Derivados de 7h-imidazo [1-5-a] pirazin-8-ona como inhibidores de la fosfodiasterasa 9(pde9); y el uso de los mismos en el tratamiento de trastornos neurodegenerativos. |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9643970B2 (es) |
| EP (2) | EP3121178B1 (es) |
| JP (1) | JP2015531401A (es) |
| CN (2) | CN104703987B (es) |
| AU (2) | AU2012323085B2 (es) |
| BR (1) | BR112015007731B1 (es) |
| CA (1) | CA2886885C (es) |
| HK (1) | HK1211023A1 (es) |
| IL (2) | IL237836A (es) |
| IN (1) | IN2015DN02829A (es) |
| MA (1) | MA37958B1 (es) |
| MX (2) | MX370433B (es) |
| SG (1) | SG11201502728WA (es) |
| TN (1) | TN2015000100A1 (es) |
| WO (1) | WO2013053690A1 (es) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HK1211023A1 (zh) * | 2011-10-10 | 2016-05-13 | H. Lundbeck A/S | 具有咪唑并吡嗪骨架pde9i |
| TWI720451B (zh) | 2014-02-13 | 2021-03-01 | 美商英塞特控股公司 | 作為lsd1抑制劑之環丙胺 |
| WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| WO2015123408A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| US9670210B2 (en) | 2014-02-13 | 2017-06-06 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TW201629064A (zh) | 2014-10-10 | 2016-08-16 | Ｈ 朗德貝克公司 | 作爲ｐｄｅ１抑制劑之三唑並吡酮 |
| MX373154B (es) | 2015-04-03 | 2020-04-22 | Incyte Holdings Corp | Compuestos heterocíclicos como inhibidores de demetilasa 1 específica de lisina (lsd1). |
| JO3627B1 (ar) | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| LT3865484T (lt) * | 2015-07-07 | 2024-02-12 | H. Lundbeck A/S | Pde9 inhibitorius su imidazopirazinono karkasu, skirtas periferinių ligų gydymui |
| TW201717948A (zh) * | 2015-08-10 | 2017-06-01 | Ｈ 朗德貝克公司 | 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療 |
| LT3334709T (lt) | 2015-08-12 | 2025-03-10 | Incyte Holdings Corporation | Lsd1 inhibitoriaus druskos |
| PE20181288A1 (es) * | 2015-11-09 | 2018-08-07 | Astrazeneca Ab | Derivados de dihidroimidazopirazinona usados en el tratamiento del cancer |
| TWI729109B (zh) | 2016-04-12 | 2021-06-01 | 丹麥商Ｈ 朗德貝克公司 | 作爲PDE1抑制劑的1,5-二氫-4H-吡唑并[3,4-d]嘧啶-4-酮和1,5-二氫-4H-吡唑并[4,3-c]吡啶-4-酮 |
| UA125559C2 (uk) | 2016-04-22 | 2022-04-20 | Інсайт Корпорейшн | Композиції інгібітора lsd1 |
| IL295973A (en) * | 2016-07-06 | 2022-10-01 | H Lundbeck As | pde9 inhibitors for the treatment of peripheral diseases |
| EP3529250B1 (en) | 2016-10-18 | 2023-12-06 | H. Lundbeck A/S | Imidazopyrazinones, pyrazolopyrimidinones and pyrazolopyridinones as pde1 inhibitors |
| HUE050403T2 (hu) | 2016-10-28 | 2020-12-28 | H Lundbeck As | Imidazopirazinonokkal végzett kombinációs kezelések pszichiátriai és/vagy kognitív betegségek kezelésére |
| WO2018078042A1 (en) * | 2016-10-28 | 2018-05-03 | H. Lundbeck A/S | Combination treatments comprising administration of imidazopyrazinones |
| CA3045745A1 (en) * | 2017-02-27 | 2018-08-30 | Janssen Pharmaceutica Nv | [1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazin as oga inhibitors |
| US11370795B2 (en) * | 2017-05-26 | 2022-06-28 | Imara Inc. | Process for the synthesis of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-3-tetrahydropyran-4-yl-7H-imidazo[1,5-a]pyrazin-8-one |
| AU2018281131B2 (en) | 2017-06-08 | 2022-01-20 | Merck Sharp & Dohme Corp. | Pyrazolopyrimidine PDE9 inhibitors |
| US11147275B2 (en) | 2017-11-23 | 2021-10-19 | Basf Se | Substituted trifluoromethyloxadiazoles for combating phytopathogenic fungi |
| HRP20240363T1 (hr) | 2018-05-25 | 2024-06-07 | Cardurion Pharmaceuticals, Inc. | Monohidratni i kristalni oblici 6-[(3s,4s)-4-metil-1-(pirimidin-2-ilmetil)pirolidin-3-il]-3-tetrahidropiran-4-il-7h-imidazo [1,5-a] pirazin-8-ona |
| MA52936A (fr) * | 2018-06-20 | 2021-04-28 | Janssen Pharmaceutica Nv | Composés inhibiteurs d'oga |
| WO2020047311A1 (en) | 2018-08-31 | 2020-03-05 | Imara Inc. | Pde9 inhibitors for treating sickle cell disease |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| CA3136128A1 (en) * | 2019-04-05 | 2020-10-08 | Imara Inc. | Pde9 inhibitors for treating sickle cell disease |
| EP3965768A1 (en) * | 2019-05-07 | 2022-03-16 | Imara Inc. | Pde9 inhibitors for treating thalassemia |
| WO2022036111A1 (en) * | 2020-08-13 | 2022-02-17 | Imara Inc. | Methods and compositions for treating sickle cell disease |
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| HRP20020585B1 (hr) | 1997-11-12 | 2013-02-28 | Bayer Schering Pharma Aktiengesellschaft | 2-fenil supstituirani imidazotriazinoni kao inhibitori fosfodiesteraze |
| KR20010101603A (ko) | 1999-01-20 | 2001-11-14 | 노왈드 | 이미다조[1,5-ａ]-피리도[3,2-ｅ]-피라지논의 약제로서의용도 |
| BR0213817A (pt) | 2001-11-02 | 2004-10-19 | Pfizer Prod Inc | Tratamento de sìndrome de resistência à insulina e diabete do tipo 2 com inibidores da pde9 |
| HN2002000317A (es) | 2001-11-02 | 2003-05-21 | Pfizer | Inhibidores de pde9 para tratamiento de trastornos cardiovasculares |
| GB2388111A (en) | 2002-05-01 | 2003-11-05 | Bayer Ag | Novel imidazotriazinone compounds |
| US20040220186A1 (en) | 2003-04-30 | 2004-11-04 | Pfizer Inc. | PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease |
| EP1686998A1 (en) | 2003-10-31 | 2006-08-09 | Pfizer Products Inc. | Phosphodiesterase 9 inhibition as treatment for obesity-related conditions |
| WO2007028051A2 (en) | 2005-09-02 | 2007-03-08 | Abbott Laboratories | Novel imidazo based heterocycles |
| 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 |
| US7947577B2 (en) | 2006-09-08 | 2011-05-24 | Tokuyama Corporation | Method and apparatus for producing group III nitride |
| JPWO2008072778A1 (ja) * | 2006-12-13 | 2010-04-02 | あすか製薬株式会社 | 尿路系疾患の処置剤 |
| WO2008072779A1 (ja) | 2006-12-13 | 2008-06-19 | Aska Pharmaceutical Co., Ltd. | キノキサリン誘導体 |
| PT2152712E (pt) | 2007-05-11 | 2012-02-29 | Pfizer | Compostos amino-heterocíclicos |
| DE102007032349A1 (de) | 2007-07-11 | 2009-01-15 | Bayer Healthcare Ag | Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung |
| TWI404721B (zh) | 2009-01-26 | 2013-08-11 | Pfizer | 胺基－雜環化合物 |
| US9260432B2 (en) | 2009-09-02 | 2016-02-16 | Concert Pharmaceuticals, Inc. | Substituted derivatives of bicyclic [4.3.0] heteroaryl compounds |
| EP3181566A1 (en) | 2010-09-20 | 2017-06-21 | Ironwood Pharmaceuticals, Inc. | Imidazotriazinone compounds |
| WO2013051639A1 (ja) | 2011-10-07 | 2013-04-11 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ピラゾロキノリン誘導体 |
| HK1211023A1 (zh) * | 2011-10-10 | 2016-05-13 | H. Lundbeck A/S | 具有咪唑并吡嗪骨架pde9i |
| HK1199879A1 (en) | 2012-01-26 | 2015-07-24 | H.隆德贝克有限公司 | Pde9 inhibitors with imidazo triazinone backbone |
| EP2828262A4 (en) | 2012-03-19 | 2015-09-23 | Forum Pharmaceuticals Inc | IMIDAZOTRIAZINONVERBINDUNGEN |
-
2012
- 2012-10-09 HK HK15111740.3A patent/HK1211023A1/xx unknown
- 2012-10-09 CA CA2886885A patent/CA2886885C/en active Active
- 2012-10-09 CN CN201280076285.6A patent/CN104703987B/zh active Active
- 2012-10-09 BR BR112015007731-5A patent/BR112015007731B1/pt active IP Right Grant
- 2012-10-09 IN IN2829DEN2015 patent/IN2015DN02829A/en unknown
- 2012-10-09 AU AU2012323085A patent/AU2012323085B2/en active Active
- 2012-10-09 JP JP2015535994A patent/JP2015531401A/ja active Pending
- 2012-10-09 US US14/434,308 patent/US9643970B2/en active Active
- 2012-10-09 CN CN201710247417.1A patent/CN106905324B/zh active Active
- 2012-10-09 EP EP16185105.0A patent/EP3121178B1/en active Active
- 2012-10-09 EP EP12772769.1A patent/EP2906562B1/en active Active
- 2012-10-09 MX MX2015004422A patent/MX370433B/es active IP Right Grant
- 2012-10-09 SG SG11201502728WA patent/SG11201502728WA/en unknown
- 2012-10-09 MX MX2019014982A patent/MX381326B/es unknown
- 2012-10-09 MA MA37958A patent/MA37958B1/fr unknown
- 2012-10-09 WO PCT/EP2012/069936 patent/WO2013053690A1/en not_active Ceased
-
2015
- 2015-03-16 TN TNP2015000100A patent/TN2015000100A1/fr unknown
- 2015-03-19 IL IL237836A patent/IL237836A/en active IP Right Grant
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2017
- 2017-03-08 US US15/452,827 patent/US9993477B2/en active Active
- 2017-03-20 AU AU2017201873A patent/AU2017201873C1/en active Active
- 2017-07-12 IL IL253448A patent/IL253448A0/en unknown
Also Published As
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