EA201891897A1 - 1,5-ДИГИДРО-4H-ПИРАЗОЛО[3,4-d]ПИРИМИДИН-4-ОНЫ И 1,5-ДИГИДРО-4H-ПИРАЗОЛО[4,3-c]ПИРИДИН-4-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE1 - Google Patents
1,5-ДИГИДРО-4H-ПИРАЗОЛО[3,4-d]ПИРИМИДИН-4-ОНЫ И 1,5-ДИГИДРО-4H-ПИРАЗОЛО[4,3-c]ПИРИДИН-4-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE1Info
- Publication number
- EA201891897A1 EA201891897A1 EA201891897A EA201891897A EA201891897A1 EA 201891897 A1 EA201891897 A1 EA 201891897A1 EA 201891897 A EA201891897 A EA 201891897A EA 201891897 A EA201891897 A EA 201891897A EA 201891897 A1 EA201891897 A1 EA 201891897A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- pyrazolo
- dihydro
- pyrimidin
- pyridin
- digidro
- Prior art date
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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
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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
-
- 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
-
- 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
-
- 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
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Настоящее изобретение обеспечивает 1,5-дигидро-4H-пиразоло[3,4-d]пиримидин-4-оны и 1,5-дигидро-4H-пиразоло[4,3-c]пиридин-4-оны формулы (I) в качестве ингибиторов PDE1 и их применение в качестве лекарственного средства, в частности, для лечения нейродегенеративных расстройств и психических расстройств.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201600221 | 2016-04-12 | ||
| PCT/EP2017/058332 WO2017178350A1 (en) | 2016-04-12 | 2017-04-07 | 1,5-dihydro-4h-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4h-pyrazolo[4,3-c]pyridin-4-ones as pde1 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201891897A1 true EA201891897A1 (ru) | 2019-03-29 |
| EA035197B1 EA035197B1 (ru) | 2020-05-14 |
Family
ID=58489694
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201891897A EA035197B1 (ru) | 2016-04-12 | 2017-04-07 | 1,5-ДИГИДРО-4H-ПИРАЗОЛО[3,4-d]ПИРИМИДИН-4-ОНЫ И 1,5-ДИГИДРО-4H-ПИРАЗОЛО[4,3-c]ПИРИДИН-4-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE1 |
Country Status (42)
Families Citing this family (9)
| 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 |
| WO2018073251A1 (en) | 2016-10-18 | 2018-04-26 | H. Lundbeck A/S | Imidazopyrazinones, pyrazolopyrimidinones and pyrazolopyridinones as pde1 inhibitors |
| CN109803653A (zh) | 2016-10-28 | 2019-05-24 | H.隆德贝克有限公司 | 包括给予咪唑并吡嗪酮的组合治疗 |
| MX2019004763A (es) | 2016-10-28 | 2019-07-01 | H Lundbeck As | Tratamientos de combinacion que comprenden imidazopirazinonas para el tratamiento de trastornos psiquiatricos y/o cognitivos. |
| EP3562828A1 (en) | 2016-12-28 | 2019-11-06 | Dart NeuroScience LLC | Substituted pyrazolopyrimidinone compounds as pde2 inhibitors |
| US11434247B1 (en) | 2017-11-27 | 2022-09-06 | Dart Neuroscience Llc | Substituted furanopyrimidine compounds as PDE1 inhibitors |
| 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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| GB973361A (en) * | 1960-05-11 | 1964-10-28 | Ciba Ltd | Pyrazolo-pyrimidines and process for their manufacture |
| 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 |
| WO2004099211A1 (de) * | 2003-05-09 | 2004-11-18 | Bayer Healthcare Ag | 6-cyclylmethyl- und 6-alkylmethyl-substituierte pyrazolopyrimidine |
| WO2006068978A2 (en) | 2004-12-21 | 2006-06-29 | Takeda Pharmaceutial Company Limited | Dipeptidyl peptidase inhibitors |
| EP1919287A4 (en) | 2005-08-23 | 2010-04-28 | Intra Cellular Therapies Inc | ORGANIC COMPOUNDS FOR TREATING A REDUCED DOPAMINE RECEPTOR SIGNALING ACTIVITY |
| US8012936B2 (en) | 2006-03-29 | 2011-09-06 | New York University | Tau fragments for immunotherapy |
| US9006258B2 (en) | 2006-12-05 | 2015-04-14 | Intra-Cellular Therapies, Inc. | Method of treating female sexual dysfunction with a PDE1 inhibitor |
| ATE540954T1 (de) * | 2007-05-11 | 2012-01-15 | Pfizer | Aminoheterocyclische verbindungen |
| WO2009068320A1 (en) | 2007-11-30 | 2009-06-04 | Elbion Gmbh | Aryl and heteroaryl fused imidazo (1,5-a) pyrazines as inhibitors of phosphodiesterase 10 |
| UA105362C2 (en) | 2008-04-02 | 2014-05-12 | Бьорингер Ингельхайм Интернациональ Гмбх | 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| EA201100446A1 (ru) | 2008-09-08 | 2011-10-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Пиразолопиримидины и их применение для лечения нарушений цнс |
| GEP20146046B (en) | 2008-12-06 | 2014-02-25 | Intracellular Therapies Inc | Organic compounds |
| TWI404721B (zh) | 2009-01-26 | 2013-08-11 | Pfizer | 胺基－雜環化合物 |
| JP5879336B2 (ja) * | 2010-05-31 | 2016-03-08 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 有機化合物 |
| AR083058A1 (es) | 2010-09-20 | 2013-01-30 | Envivo Pharmaceuticals Inc | Compuestos de estructura de imidazotriazinona |
| EP2619204A4 (en) | 2010-09-21 | 2014-08-27 | Merck Sharp & Dohme | TRIAZOLOPYRAZINONES AS ANTAGONISTS OF P2X7 RECEPTORS |
| JO3089B1 (ar) | 2010-11-19 | 2017-03-15 | H Lundbeck As | مشتقات ايميدازول كمثبطات لانزيمات pde10a |
| US9499610B2 (en) | 2011-04-08 | 2016-11-22 | H. Lundbeck A/S | Antibodies specific to pyroglutamated Aβ |
| JP6051210B2 (ja) | 2011-06-10 | 2016-12-27 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 有機化合物 |
| CA2886885C (en) | 2011-10-10 | 2019-07-16 | H. Lundbeck A/S | Pde9i with imidazo pyrazinone backbone |
| EP2807163B1 (en) | 2012-01-26 | 2017-03-22 | H. Lundbeck A/S | Pde9 inhibitors with imidazo triazinone backbone |
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| AU2014234990B2 (en) | 2013-03-15 | 2017-11-16 | Intra-Cellular Therapies, Inc. | Organic compounds |
| JP5783297B2 (ja) | 2013-08-06 | 2015-09-24 | 株式会社デンソー | 力学量センサ |
| 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 |
| JP5797815B1 (ja) | 2014-06-27 | 2015-10-21 | 細田建設株式会社 | 後施工アンカー及びその施工方法 |
| US20160083400A1 (en) | 2014-09-18 | 2016-03-24 | Sunovion Pharmaceuticals Inc. | Tricyclic guanidine derivative |
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| US20160083391A1 (en) | 2014-09-18 | 2016-03-24 | Sunovion Pharmaceuticals Inc. | Tricyclic piperazine derivative |
| 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 |
| WO2016147659A1 (en) | 2015-03-16 | 2016-09-22 | Sumitomo Dainippon Pharma Co., Ltd. | Bicyclic imidazolo derivative |
| TW201643167A (zh) | 2015-04-22 | 2016-12-16 | Ｈ 朗德貝克公司 | 作爲ｐｄｅ１抑制劑之咪唑並三酮 |
| 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 |
| WO2018073251A1 (en) | 2016-10-18 | 2018-04-26 | H. Lundbeck A/S | Imidazopyrazinones, pyrazolopyrimidinones and pyrazolopyridinones as pde1 inhibitors |
| CN109803653A (zh) | 2016-10-28 | 2019-05-24 | H.隆德贝克有限公司 | 包括给予咪唑并吡嗪酮的组合治疗 |
| MX2019004763A (es) | 2016-10-28 | 2019-07-01 | H Lundbeck As | Tratamientos de combinacion que comprenden imidazopirazinonas para el tratamiento de trastornos psiquiatricos y/o cognitivos. |
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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 DK DK17715943.1T patent/DK3442975T3/da active
- 2017-04-07 MY MYPI2018001605A patent/MY194722A/en unknown
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- 2017-04-07 WO PCT/EP2017/058332 patent/WO2017178350A1/en active Application Filing
- 2017-04-07 ES ES17715943T patent/ES2814289T3/es active Active
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- 2017-04-07 MX MX2018012496A patent/MX2018012496A/es active IP Right Grant
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