MX370433B - 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. - Google Patents
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.Info
- Publication number
- MX370433B MX370433B MX2015004422A MX2015004422A MX370433B MX 370433 B MX370433 B MX 370433B MX 2015004422 A MX2015004422 A MX 2015004422A MX 2015004422 A MX2015004422 A MX 2015004422A MX 370433 B MX370433 B MX 370433B
- Authority
- MX
- Mexico
- Prior art keywords
- compound
- formula
- effective amount
- therapeutically effective
- pde9i
- Prior art date
Links
- MPWOBEOETVOESI-UHFFFAOYSA-N imidazo[4,5-b]pyrazin-2-one Chemical group N1=CC=NC2=NC(=O)N=C21 MPWOBEOETVOESI-UHFFFAOYSA-N 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
- 208000015122 neurodegenerative disease Diseases 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
-
- 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
-
- 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
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)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (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 |
|---|---|
| MX2015004422A MX2015004422A (es) | 2015-10-15 |
| MX370433B true MX370433B (es) | 2019-12-13 |
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 After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9643970B2 (es) |
| EP (2) | EP3121178B1 (es) |
| JP (1) | JP2015531401A (es) |
| CN (2) | CN106905324B (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 |
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| AU2012323085B2 (en) * | 2011-10-10 | 2017-03-09 | H. Lundbeck A/S | PDE9i with imidazo pyrazinone backbone |
| TW201613860A (en) | 2014-02-13 | 2016-04-16 | Incyte Corp | Cyclopropylamines as LSD1 inhibitors |
| PT3105226T (pt) | 2014-02-13 | 2019-11-06 | Incyte Corp | Ciclopropilaminas como inibidores de lsd1 |
| ME03654B (me) | 2014-02-13 | 2020-07-20 | Incyte Corp | Ciklopropilamini kao lsd1 inhibitori |
| WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| WO2016007722A1 (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 |
| AU2016243939B2 (en) | 2015-04-03 | 2020-09-03 | Incyte Holdings Corporation | Heterocyclic compounds as LSD1 inhibitors |
| JO3627B1 (ar) * | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| US10513524B2 (en) * | 2015-07-07 | 2019-12-24 | H. Lundbeck A/S | PDE9 inhibitors with imidazo triazinone backbone and imidazo pyrazinone backbone for treatment of peripheral diseases |
| 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 |
| KR102710120B1 (ko) | 2015-08-12 | 2024-09-27 | 인사이트 홀딩스 코포레이션 | Lsd1 저해제의 염 |
| SI3374359T1 (sl) * | 2015-11-09 | 2020-04-30 | Astrazeneca Ab | Derivati dihidroimidazopirazinona uporabni pri zdravljenju raka |
| 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 |
| AR109452A1 (es) | 2016-04-22 | 2018-12-12 | Incyte Corp | Formulación farmacéutica de un inhibidor de lsd1 y método de tratamiento |
| CA3025586A1 (en) * | 2016-07-06 | 2018-01-11 | Imara, Inc. | Pde9 inhibitors for treatment of peripheral diseases |
| WO2018073251A1 (en) | 2016-10-18 | 2018-04-26 | H. Lundbeck A/S | Imidazopyrazinones, pyrazolopyrimidinones and pyrazolopyridinones as pde1 inhibitors |
| DK3532064T3 (da) * | 2016-10-28 | 2020-08-24 | H Lundbeck As | Kombinationsbehandlinger omfattende imidazopyrazinoner til behandlingen af psykiatriske og/eller kognitive lidelser |
| EP3532053A1 (en) | 2016-10-28 | 2019-09-04 | 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 |
| RS65143B1 (sr) | 2017-05-26 | 2024-02-29 | Cardurion Pharmaceuticals Inc | Postupci izrade i upotrebe pde9 inhibitora |
| MX2019014597A (es) | 2017-06-08 | 2020-02-05 | Merck Sharp & Dohme | Inhibidores de pirazolopirimidina de pde9. |
| EP3713936B1 (en) | 2017-11-23 | 2021-10-20 | Basf Se | Substituted trifluoromethyloxadiazoles for combating phytopathogenic fungi |
| JP2021526134A (ja) * | 2018-05-25 | 2021-09-30 | イマラ インク． | ６−［（３Ｓ，４Ｓ）−４−メチル−ｌ−（ピリミジン−２−イルメチル）ピロリジン−３−イル］−３−テトラヒドロピラン−４−イル−７Ｈ−イミダゾ［ｌ，５−Ａ］ピラジン−８−オンの一水和物および結晶形態 |
| CN112312908A (zh) * | 2018-06-20 | 2021-02-02 | 詹森药业有限公司 | Oga抑制剂化合物 |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| KR20250108770A (ko) | 2018-08-31 | 2025-07-15 | 카듀리온 파마슈티칼스, 인크. | 겸상 세포 질환의 치료를 위한 pde9 억제제 |
| CA3136128A1 (en) * | 2019-04-05 | 2020-10-08 | Imara Inc. | Pde9 inhibitors for treating sickle cell disease |
| CN114072151A (zh) * | 2019-05-07 | 2022-02-18 | 伊马拉公司 | 用于治疗地中海贫血的pde9抑制剂 |
| WO2022036111A1 (en) * | 2020-08-13 | 2022-02-17 | Imara Inc. | Methods and compositions for treating sickle cell disease |
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| WO2003037432A1 (en) | 2001-11-02 | 2003-05-08 | Pfizer Products Inc. | Treatment of insulin resistance syndrome and type 2 diabetes with pde9 inhibitors |
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| 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 |
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| 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 |
| CA2662594A1 (en) | 2006-09-08 | 2008-03-13 | Tokuyama Corporation | Method and apparatus for producing a group iii nitride |
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| MY147330A (en) | 2007-05-11 | 2012-11-30 | Pfizer | Amino-heterocyclic compounds |
| 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 |
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| US20120157458A1 (en) | 2010-09-20 | 2012-06-21 | Amy Ripka | Imidazotriazinone compounds |
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| AU2012323085B2 (en) * | 2011-10-10 | 2017-03-09 | H. Lundbeck A/S | PDE9i with imidazo pyrazinone backbone |
| AP2014007820A0 (en) | 2012-01-26 | 2014-07-31 | Lundbeck & Co As H | PDE9 inhibitors with imidazo triazinone backbone |
| WO2013142269A1 (en) | 2012-03-19 | 2013-09-26 | Envivo Pharmaceuticals, Inc. | Imidazotriazinone compounds |
-
2012
- 2012-10-09 AU AU2012323085A patent/AU2012323085B2/en active Active
- 2012-10-09 MA MA37958A patent/MA37958B1/fr unknown
- 2012-10-09 CA CA2886885A patent/CA2886885C/en active Active
- 2012-10-09 EP EP16185105.0A patent/EP3121178B1/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 CN CN201710247417.1A patent/CN106905324B/zh active Active
- 2012-10-09 HK HK15111740.3A patent/HK1211023A1/xx unknown
- 2012-10-09 IN IN2829DEN2015 patent/IN2015DN02829A/en unknown
- 2012-10-09 EP EP12772769.1A patent/EP2906562B1/en active Active
- 2012-10-09 US US14/434,308 patent/US9643970B2/en active Active
- 2012-10-09 WO PCT/EP2012/069936 patent/WO2013053690A1/en not_active Ceased
- 2012-10-09 JP JP2015535994A patent/JP2015531401A/ja active Pending
- 2012-10-09 CN CN201280076285.6A patent/CN104703987B/zh active Active
- 2012-10-09 MX MX2019014982A patent/MX381326B/es unknown
- 2012-10-09 BR BR112015007731-5A patent/BR112015007731B1/pt active IP Right Grant
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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
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