PE20181853A1 - 1,5-dihidro-4h-pirazolo[3,4-d]pirimidin-4-onas y 1,5-dihidro-4h-pirazolo[4,3-c]piridin-4-onas como inhibidores de pde1 - Google Patents
1,5-dihidro-4h-pirazolo[3,4-d]pirimidin-4-onas y 1,5-dihidro-4h-pirazolo[4,3-c]piridin-4-onas como inhibidores de pde1Info
- Publication number
- PE20181853A1 PE20181853A1 PE2018001912A PE2018001912A PE20181853A1 PE 20181853 A1 PE20181853 A1 PE 20181853A1 PE 2018001912 A PE2018001912 A PE 2018001912A PE 2018001912 A PE2018001912 A PE 2018001912A PE 20181853 A1 PE20181853 A1 PE 20181853A1
- Authority
- PE
- Peru
- Prior art keywords
- onas
- dihydro
- pirazolo
- pyrimidin
- pyrazole
- Prior art date
Links
- MCGBIXXDQFWVDW-UHFFFAOYSA-N 4,5-dihydro-1h-pyrazole Chemical compound C1CC=NN1 MCGBIXXDQFWVDW-UHFFFAOYSA-N 0.000 title 1
- 229940121836 Phosphodiesterase 1 inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229940082638 cardiac stimulant phosphodiesterase inhibitors Drugs 0.000 abstract 2
- 239000002571 phosphodiesterase inhibitor Substances 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- 208000023105 Huntington disease Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- 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
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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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
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- 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
- A61P25/22—Anxiolytics
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- 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
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- 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
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- 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
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)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se refiere a compuestos de formula (I) donde Y es N o CH; R1 es alquilo C2-C8 lineal o ramificado, cicloalquilo C3-C8 monociclico saturado, entre otros; R2 es C1-C8 lineal o ramificado, fenilo, entre otros; R3 es alquilo C1-C3 y cicloalquilo C3-C8 monociclico saturado; cada uno de los cuales puede estar opcionalmente sustituido con un sustituyente seleccionado de halogeno, alcoxi C1-C3, entre otros. Tambien se refiere a una sal farmaceuticamente aceptable del mismo y a una composicion farmaceutica que contiene un compuesto de formula (I). Dichos compuestos son inhibidores de las fosfodiesterasas (PDE) y son utiles para el tratamiento de trastornos neurodegenerativos tales como alzheimer, parkinson y enfermedad de Huntington y trastornos psiquiatricos tales como depresion, nacolepsia, deterioro cognitivo, entre otros
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201600221 | 2016-04-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20181853A1 true PE20181853A1 (es) | 2018-12-03 |
Family
ID=58489694
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018001912A PE20181853A1 (es) | 2016-04-12 | 2017-04-07 | 1,5-dihidro-4h-pirazolo[3,4-d]pirimidin-4-onas y 1,5-dihidro-4h-pirazolo[4,3-c]piridin-4-onas como inhibidores de pde1 |
Country Status (43)
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| JO3627B1 (ar) | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| 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 |
| US10633382B2 (en) | 2016-10-18 | 2020-04-28 | H. Lundbeck A/S | Imidazopyrazinones, pyrazolopyrimidinones and pyrazolopyridinones as PDE1 inhibitors |
| KR20190075068A (ko) | 2016-10-28 | 2019-06-28 | 하. 룬드벡 아크티에셀스카브 | 정신 및/또는 인지 장애의 치료를 위한 이미다조피라지논을 포함하는 병용 치료 |
| MA46621A (fr) | 2016-10-28 | 2021-06-02 | H Lundbeck As | Traitements combinés comprenant l'administration d'imidazopyrazinones |
| CA3047408A1 (en) | 2016-12-28 | 2018-07-05 | Dart Neuroscience, Llc | Substituted pyrazolopyrimidinone compounds as pde2 inhibitors |
| KR102794907B1 (ko) | 2017-11-27 | 2025-04-14 | 다트 뉴로사이언스, 엘엘씨 | Pde1 억제제로서의 치환된 푸라노피리미딘 화합물 |
| JP7493460B2 (ja) | 2018-05-25 | 2024-05-31 | 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 |
| CN115304607B (zh) * | 2022-07-06 | 2023-06-27 | 华南农业大学 | 吡唑并嘧啶衍生物的制备方法 |
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| DE19709877A1 (de) | 1997-03-11 | 1998-09-17 | Bayer Ag | 1,5-Dihydro-pyrazolo[3,4-d]-pyrimidinon-derivate |
| DE10238723A1 (de) * | 2002-08-23 | 2004-03-11 | Bayer Ag | Phenyl-substituierte Pyrazolyprimidine |
| DE10238722A1 (de) * | 2002-08-23 | 2004-03-11 | Bayer Ag | Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse |
| DE10238724A1 (de) * | 2002-08-23 | 2004-03-04 | Bayer Ag | Alkyl-substituierte Pyrazolpyrimidine |
| AU2004235915B2 (en) * | 2003-05-09 | 2010-08-05 | Boehringer Ingelheim International Gmbh | 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines |
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| EA201100446A1 (ru) | 2008-09-08 | 2011-10-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Пиразолопиримидины и их применение для лечения нарушений цнс |
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| JP5783297B2 (ja) | 2013-08-06 | 2015-09-24 | 株式会社デンソー | 力学量センサ |
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| CA2961186A1 (en) | 2014-09-18 | 2016-03-24 | Sunovion Pharmaceuticals Inc. | Tricyclic derivative |
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| TW201639851A (zh) | 2015-03-16 | 2016-11-16 | 大日本住友製藥股份有限公司 | 雙環咪唑衍生物 |
| US20160311831A1 (en) | 2015-04-22 | 2016-10-27 | H. Lundbeck A/S | Imidazotriazinones as PDE1 Inhibitors |
| JO3627B1 (ar) | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| AR107456A1 (es) | 2016-02-12 | 2018-05-02 | Lilly Co Eli | Inhibidor de pde1 |
| 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 |
| JP2018076285A (ja) | 2016-09-14 | 2018-05-17 | 大日本住友製薬株式会社 | 二環性イミダゾロ誘導体を含む医薬 |
| US10633382B2 (en) | 2016-10-18 | 2020-04-28 | H. Lundbeck A/S | Imidazopyrazinones, pyrazolopyrimidinones and pyrazolopyridinones as PDE1 inhibitors |
| MA46621A (fr) | 2016-10-28 | 2021-06-02 | H Lundbeck As | Traitements combinés comprenant l'administration d'imidazopyrazinones |
| KR20190075068A (ko) | 2016-10-28 | 2019-06-28 | 하. 룬드벡 아크티에셀스카브 | 정신 및/또는 인지 장애의 치료를 위한 이미다조피라지논을 포함하는 병용 치료 |
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2017
- 2017-04-05 TW TW106111366A patent/TWI729109B/zh not_active IP Right Cessation
- 2017-04-06 US US15/481,083 patent/US20170291901A1/en not_active Abandoned
- 2017-04-07 SG SG11201808221QA patent/SG11201808221QA/en unknown
- 2017-04-07 LT LTEP17715943.1T patent/LT3442975T/lt unknown
- 2017-04-07 SM SM20200446T patent/SMT202000446T1/it unknown
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- 2017-04-07 UA UAA201809742A patent/UA121925C2/uk unknown
- 2017-04-07 DK DK17715943.1T patent/DK3442975T3/da active
- 2017-04-07 KR KR1020187029341A patent/KR20180133413A/ko not_active Ceased
- 2017-04-07 AU AU2017250431A patent/AU2017250431B2/en not_active Ceased
- 2017-04-07 EA EA201891897A patent/EA035197B1/ru not_active IP Right Cessation
- 2017-04-07 MA MA44656A patent/MA44656B1/fr unknown
- 2017-04-07 ES ES17715943T patent/ES2814289T3/es active Active
- 2017-04-07 PT PT177159431T patent/PT3442975T/pt unknown
- 2017-04-07 PE PE2018001912A patent/PE20181853A1/es unknown
- 2017-04-07 MY MYPI2018001605A patent/MY194722A/en unknown
- 2017-04-07 RS RS20200994A patent/RS60714B1/sr unknown
- 2017-04-07 PL PL17715943T patent/PL3442975T3/pl unknown
- 2017-04-07 WO PCT/EP2017/058332 patent/WO2017178350A1/en active Application Filing
- 2017-04-07 RU RU2018133391A patent/RU2018133391A/ru unknown
- 2017-04-07 ME MEP-2020-169A patent/ME03820B/me unknown
- 2017-04-07 SI SI201730387T patent/SI3442975T1/sl unknown
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2019
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2020
- 2020-08-20 CY CY20201100779T patent/CY1123269T1/el unknown
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