JO3116B1 - مشتق بيرازولوكينولين كمثبطات ل pde9 - Google Patents
مشتق بيرازولوكينولين كمثبطات ل pde9Info
- Publication number
- JO3116B1 JO3116B1 JOP/2012/0302A JOP20120302A JO3116B1 JO 3116 B1 JO3116 B1 JO 3116B1 JO P20120302 A JOP20120302 A JO P20120302A JO 3116 B1 JO3116 B1 JO 3116B1
- Authority
- JO
- Jordan
- Prior art keywords
- hydrogen atom
- pde9
- pyrazolokinoline
- inhibitors
- derived
- Prior art date
Links
- 101100407341 Drosophila melanogaster Pde9 gene Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000003551 oxepanyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- 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
- 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
- A61P25/28—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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
يتعلق الاختراع بمركب أو ملح مقبول فسيولوجيا منه ممثل بالصيغة (I) بتأثير تثبيط PDE9 ويكون مفيد كعامل تحسين في مرض ألزهايمر. حيث R1 عبارة عن ذرة هيدروجين؛ R2 عبارة عن مجموعة حلقة اروماتية، إلخ؛ R3 عبارة عن ذرة هيدروجين، إلخ؛ R4 عبارة عن ذرة هيدروجين؛ R5 عبارة عن مجموعة أوكسيبانيل، إلخ؛ R6 عبارة عن ذرة هيدروجين.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161544860P | 2011-10-07 | 2011-10-07 | |
| US201161550623P | 2011-10-24 | 2011-10-24 | |
| US201161558110P | 2011-11-10 | 2011-11-10 | |
| US201161580903P | 2011-12-28 | 2011-12-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JO3116B1 true JO3116B1 (ar) | 2017-09-20 |
Family
ID=48043792
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2012/0302A JO3116B1 (ar) | 2011-10-07 | 2012-10-04 | مشتق بيرازولوكينولين كمثبطات ل pde9 |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US8563565B2 (ar) |
| EP (1) | EP2769980B1 (ar) |
| JP (1) | JP5546693B2 (ar) |
| KR (1) | KR101943680B1 (ar) |
| CN (1) | CN103930423B (ar) |
| AR (1) | AR088235A1 (ar) |
| AU (1) | AU2012319549B2 (ar) |
| BR (1) | BR112014007912B1 (ar) |
| CA (1) | CA2861795C (ar) |
| CL (1) | CL2014000821A1 (ar) |
| CO (1) | CO6910200A2 (ar) |
| CY (1) | CY1117427T1 (ar) |
| DK (1) | DK2769980T3 (ar) |
| ES (1) | ES2568015T3 (ar) |
| HR (1) | HRP20160273T1 (ar) |
| HU (1) | HUE028555T2 (ar) |
| IL (1) | IL231650A (ar) |
| IN (1) | IN2014CN02463A (ar) |
| JO (1) | JO3116B1 (ar) |
| ME (1) | ME02394B (ar) |
| MX (1) | MX358149B (ar) |
| MY (1) | MY167698A (ar) |
| PE (1) | PE20141557A1 (ar) |
| PH (1) | PH12014500580A1 (ar) |
| PL (1) | PL2769980T3 (ar) |
| RS (1) | RS54702B1 (ar) |
| RU (1) | RU2605096C2 (ar) |
| SG (1) | SG11201400717QA (ar) |
| SI (1) | SI2769980T1 (ar) |
| SM (1) | SMT201600108B (ar) |
| TW (1) | TWI562993B (ar) |
| WO (1) | WO2013051639A1 (ar) |
| ZA (1) | ZA201402439B (ar) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX381326B (es) | 2011-10-10 | 2025-03-12 | H Lundbeck As | 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 |
| JP5666755B1 (ja) * | 2013-04-05 | 2015-02-12 | 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の塩およびその結晶 |
| ES2654094T3 (es) * | 2013-04-05 | 2018-02-12 | Eisai R&D Management Co., Ltd. | Compuestos piridinilpirazoloquinolina |
| GB201406486D0 (en) | 2014-04-10 | 2014-05-28 | Redx Pharma Ltd | Antibacterial compounds |
| WO2016021192A1 (en) * | 2014-08-08 | 2016-02-11 | Eisai R&D Management Co., Ltd. | Process for production of (s)-(tetrahydrofuran-3-yl)hydrazine |
| CA2990521C (en) | 2015-07-07 | 2023-10-10 | H. Lundbeck A/S | Pde9 inhibitors with imidazo triazinone backbone and imidazo pyrazinone backbone for treatment of peripheral diseases |
| WO2017046606A1 (en) * | 2015-09-18 | 2017-03-23 | Redx Pharma Plc | Antibacterial compounds |
| CN107056690A (zh) * | 2017-03-22 | 2017-08-18 | 上海康鹏科技有限公司 | 一种6‑溴吡啶‑3‑甲醛的制备方法 |
| JP7177772B2 (ja) * | 2017-06-01 | 2022-11-24 | 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とメマンチンの併用による認知症治療剤 |
| BR112019023569A2 (pt) * | 2017-06-01 | 2020-06-02 | Eisai R&D Management Co., Ltd. | Agente terapêutico da demência combinando derivados de pirazoloquinolina e donepezila |
| CN116585316A (zh) | 2017-06-01 | 2023-08-15 | 卫材R&D管理有限公司 | 包含pde9抑制剂的药物组合物 |
| KR20200010220A (ko) | 2017-06-01 | 2020-01-30 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 피라졸로퀴놀린 유도체를 함유하는 루이소체 질병 치료제 |
| US11591312B2 (en) | 2018-01-23 | 2023-02-28 | Basf Se | Halogenation of pyridine derivatives |
| BR112020024019A2 (pt) | 2018-05-25 | 2021-02-23 | Imara Inc. | monoidrato e formas cristalinas de 6-[(3s,4s)-4-metil-1-(pirimidin-2-ilmetil)pirrolidin-3-il]-3-tetra-hidropiran-4-il-7h-imidazo[1,5-a]pirazin-8-ona |
| KR20250108770A (ko) | 2018-08-31 | 2025-07-15 | 카듀리온 파마슈티칼스, 인크. | 겸상 세포 질환의 치료를 위한 pde9 억제제 |
| CN113227077B (zh) * | 2018-12-13 | 2024-10-29 | 英特维特国际股份有限公司 | 一种制备1-[(3r,4s)-4-氰基四氢吡喃-3-基]-3-[(2-氟-6-甲氧基-4-吡啶基)氨基]吡唑-4-甲酰胺的方法 |
| US10919882B2 (en) | 2019-05-09 | 2021-02-16 | The Feinstein Institutes For Medical Research | Compounds for use in synthesis of peptidomimetics |
| IL322277A (en) | 2019-05-09 | 2025-09-01 | Feinstein Institutes For Medical Research | Thio-semicarbazide compounds and their use |
| US11471508B2 (en) | 2019-05-09 | 2022-10-18 | The Feinstein Institutes For Medical Research | HMGB1 antagonist treatment of diabetic peripheral neuropathy |
| US11883461B2 (en) | 2019-05-09 | 2024-01-30 | The Feinstein Institutes For Medical Research | HMGB1 antagonist treatment of severe sepsis |
| WO2021150613A1 (en) | 2020-01-20 | 2021-07-29 | Incyte Corporation | Spiro compounds as inhibitors of kras |
| CN121270550A (zh) * | 2020-04-16 | 2026-01-06 | 因赛特公司 | 稠合三环kras抑制剂 |
| EP4146629A4 (en) | 2020-05-08 | 2024-10-23 | The Feinstein Institutes for Medical Research | Dimers for use in synthesis of peptidomimetics |
| WO2021231526A1 (en) | 2020-05-13 | 2021-11-18 | Incyte Corporation | Fused pyrimidine compounds as kras inhibitors |
| MX2022016551A (es) | 2020-06-30 | 2023-02-01 | Bayer Ag | Heteroariloxipiridinas sustituidas, asi como sus sales y su uso como principios activos herbicidas. |
| WO2022047093A1 (en) | 2020-08-28 | 2022-03-03 | Incyte Corporation | Vinyl imidazole compounds as inhibitors of kras |
| WO2022072783A1 (en) | 2020-10-02 | 2022-04-07 | Incyte Corporation | Bicyclic dione compounds as inhibitors of kras |
| WO2022204112A1 (en) | 2021-03-22 | 2022-09-29 | Incyte Corporation | Imidazole and triazole kras inhibitors |
| WO2023283213A1 (en) | 2021-07-07 | 2023-01-12 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| CA3224841A1 (en) | 2021-07-14 | 2023-01-19 | Zhenwu Li | Tricyclic compounds as inhibitors of kras |
| CA3229855A1 (en) | 2021-08-31 | 2023-03-09 | Incyte Corporation | Naphthyridine compounds as inhibitors of kras |
| US12030883B2 (en) | 2021-09-21 | 2024-07-09 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of KRAS |
| US12030884B2 (en) | 2021-10-01 | 2024-07-09 | Incyte Corporation | Pyrazoloquinoline KRAS inhibitors |
| KR20240101561A (ko) | 2021-10-14 | 2024-07-02 | 인사이트 코포레이션 | Kras의 저해제로서의 퀴놀린 화합물 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2426734C2 (ru) * | 2003-10-03 | 2011-08-20 | Зм Инновейтив Пропертиз Компани | Пиразолопиридины и их аналоги |
| US20060035920A1 (en) * | 2004-05-28 | 2006-02-16 | Millennium Pharmaceuticals, Inc. | Chk-1 inhibitors |
| WO2007032466A1 (ja) | 2005-09-15 | 2007-03-22 | Aska Pharmaceutical Co., Ltd. | 複素環化合物、その製造方法並びに用途 |
| JP2009184924A (ja) | 2006-05-31 | 2009-08-20 | Eisai R & D Management Co Ltd | 生物学的試薬用化合物 |
| 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 |
| 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 |
| AU2010219598A1 (en) * | 2009-03-05 | 2011-09-22 | Astellas Pharma Inc. | Quinoxaline compounds |
| UY32531A (es) | 2009-03-31 | 2010-10-29 | Boehringer Ingelheim Int | Nuevos compuestos para el tratamiento de trastornos del snc |
| US8880976B2 (en) | 2009-09-25 | 2014-11-04 | Stmicroelectronics, Inc. | Method and apparatus for encoding LBA information into the parity of a LDPC system |
| ES2583528T3 (es) | 2010-09-07 | 2016-09-21 | Astellas Pharma Inc. | Compuesto de pirazoloquinolina |
| JP6042060B2 (ja) * | 2011-09-26 | 2016-12-14 | サノフイ | ピラゾロキノリノン誘導体、その調製および治療上の使用 |
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2012
- 2012-10-04 CN CN201280046653.2A patent/CN103930423B/zh active Active
- 2012-10-04 SI SI201230501A patent/SI2769980T1/sl unknown
- 2012-10-04 ES ES12837953.4T patent/ES2568015T3/es active Active
- 2012-10-04 PL PL12837953T patent/PL2769980T3/pl unknown
- 2012-10-04 JO JOP/2012/0302A patent/JO3116B1/ar active
- 2012-10-04 US US13/644,745 patent/US8563565B2/en active Active
- 2012-10-04 BR BR112014007912-9A patent/BR112014007912B1/pt active IP Right Grant
- 2012-10-04 CA CA2861795A patent/CA2861795C/en active Active
- 2012-10-04 RU RU2014112931/04A patent/RU2605096C2/ru active
- 2012-10-04 MY MYPI2014700702A patent/MY167698A/en unknown
- 2012-10-04 WO PCT/JP2012/075748 patent/WO2013051639A1/ja not_active Ceased
- 2012-10-04 AU AU2012319549A patent/AU2012319549B2/en active Active
- 2012-10-04 DK DK12837953.4T patent/DK2769980T3/en active
- 2012-10-04 RS RS20160232A patent/RS54702B1/sr unknown
- 2012-10-04 SG SG11201400717QA patent/SG11201400717QA/en unknown
- 2012-10-04 AR ARP120103702A patent/AR088235A1/es active IP Right Grant
- 2012-10-04 ME MEP-2016-65A patent/ME02394B/me unknown
- 2012-10-04 EP EP12837953.4A patent/EP2769980B1/en active Active
- 2012-10-04 HR HRP20160273TT patent/HRP20160273T1/hr unknown
- 2012-10-04 PE PE2014000408A patent/PE20141557A1/es active IP Right Grant
- 2012-10-04 PH PH1/2014/500580A patent/PH12014500580A1/en unknown
- 2012-10-04 KR KR1020147008769A patent/KR101943680B1/ko active Active
- 2012-10-04 TW TW101136747A patent/TWI562993B/zh active
- 2012-10-04 IN IN2463CHN2014 patent/IN2014CN02463A/en unknown
- 2012-10-04 JP JP2013537544A patent/JP5546693B2/ja active Active
- 2012-10-04 MX MX2014003800A patent/MX358149B/es active IP Right Grant
- 2012-10-04 HU HUE12837953A patent/HUE028555T2/en unknown
-
2013
- 2013-06-11 US US13/914,898 patent/US20130296352A1/en not_active Abandoned
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2014
- 2014-03-19 CO CO14059034A patent/CO6910200A2/es active IP Right Grant
- 2014-03-20 IL IL231650A patent/IL231650A/en active IP Right Grant
- 2014-04-02 ZA ZA2014/02439A patent/ZA201402439B/en unknown
- 2014-04-03 CL CL2014000821A patent/CL2014000821A1/es unknown
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2016
- 2016-04-12 CY CY20161100302T patent/CY1117427T1/el unknown
- 2016-04-14 SM SM201600108T patent/SMT201600108B/xx unknown
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