MX358149B - Derivado de pirazoloquinolina. - Google Patents
Derivado de pirazoloquinolina.Info
- Publication number
- MX358149B MX358149B MX2014003800A MX2014003800A MX358149B MX 358149 B MX358149 B MX 358149B MX 2014003800 A MX2014003800 A MX 2014003800A MX 2014003800 A MX2014003800 A MX 2014003800A MX 358149 B MX358149 B MX 358149B
- Authority
- MX
- Mexico
- Prior art keywords
- hydrogen atom
- pde9
- acceptable salt
- formula
- inhibitory effect
- Prior art date
Links
- UXYHZIYEDDINQH-UHFFFAOYSA-N C1=CNC2=C3C=NN=C3C=CC2=C1 Chemical class C1=CNC2=C3C=NN=C3C=CC2=C1 UXYHZIYEDDINQH-UHFFFAOYSA-N 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 abstract 2
- 101100407341 Drosophila melanogaster Pde9 gene Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 230000006399 behavior Effects 0.000 abstract 1
- 210000004556 brain Anatomy 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 125000003551 oxepanyl group Chemical group 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
Un compuesto representado por la fórmula (I) o una de sus sales farmacéuticamente aceptables que ejerce un efecto inhibitorio sobre PDE9 y, por lo tanto, cabe esperar que sea capaz de incrementar el nivel de cGMP en el cerebro. Debido a que el efecto inhibitorio sobre PDE9 y un aumento en el nivel de cGMP contribuyen a mejorar el comportamiento de aprendizaje y memoria, el compuesto mencionado anteriormente o una de sus sales farmacéuticamente aceptables estaría disponible como remedio para la disfunción cognitiva en zzzzzla enfermedad de Alzheimer. En la fórmula (I): R1 representa un átomo de hidrógeno; R2 representa un grupo de anillo aromático, etc.; R3 representa un átomo de hidrógeno, etc.; R4 representa un átomo de hidrógeno; R5 representa un grupo oxepanilo, etc.; y R6 representa un átomo de hidrógeno. (ver Fórmula).
Applications Claiming Priority (5)
| 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 | |
| PCT/JP2012/075748 WO2013051639A1 (ja) | 2011-10-07 | 2012-10-04 | ピラゾロキノリン誘導体 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2014003800A MX2014003800A (es) | 2014-07-28 |
| MX358149B true MX358149B (es) | 2018-08-07 |
Family
ID=48043792
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2014003800A MX358149B (es) | 2011-10-07 | 2012-10-04 | Derivado de pirazoloquinolina. |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US8563565B2 (es) |
| EP (1) | EP2769980B1 (es) |
| JP (1) | JP5546693B2 (es) |
| KR (1) | KR101943680B1 (es) |
| CN (1) | CN103930423B (es) |
| AR (1) | AR088235A1 (es) |
| AU (1) | AU2012319549B2 (es) |
| BR (1) | BR112014007912B1 (es) |
| CA (1) | CA2861795C (es) |
| CL (1) | CL2014000821A1 (es) |
| CO (1) | CO6910200A2 (es) |
| CY (1) | CY1117427T1 (es) |
| DK (1) | DK2769980T3 (es) |
| ES (1) | ES2568015T3 (es) |
| HR (1) | HRP20160273T1 (es) |
| HU (1) | HUE028555T2 (es) |
| IL (1) | IL231650A (es) |
| IN (1) | IN2014CN02463A (es) |
| JO (1) | JO3116B1 (es) |
| ME (1) | ME02394B (es) |
| MX (1) | MX358149B (es) |
| MY (1) | MY167698A (es) |
| PE (1) | PE20141557A1 (es) |
| PH (1) | PH12014500580A1 (es) |
| PL (1) | PL2769980T3 (es) |
| RS (1) | RS54702B1 (es) |
| RU (1) | RU2605096C2 (es) |
| SG (1) | SG11201400717QA (es) |
| SI (1) | SI2769980T1 (es) |
| SM (1) | SMT201600108B (es) |
| TW (1) | TWI562993B (es) |
| WO (1) | WO2013051639A1 (es) |
| ZA (1) | ZA201402439B (es) |
Families Citing this family (32)
| 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 |
| KR101997955B1 (ko) * | 2013-04-05 | 2019-07-08 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 피라졸로퀴놀린 유도체의 염, 및 이의 결정 |
| US9550776B2 (en) * | 2013-04-05 | 2017-01-24 | Eisai R&D Management Co., Ltd. | Pyridinylpyrazoloquinoline compounds |
| 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 |
| IL280619B2 (en) | 2015-07-07 | 2023-10-01 | H Lundbeck As | Phosphodiesterase 9 inhibitors with an imidazo triazinon or imidazo pyrazinone skeleton for the 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 |
| 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 |
| AU2018276565A1 (en) * | 2017-06-01 | 2019-11-07 | Eisai R&D Management Co., Ltd. | Dementia therapeutic agent combining pyrazoloquinoline derivative and donepezil |
| 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 |
| ES2961554T3 (es) * | 2017-06-01 | 2024-03-12 | Eisai R&D Man Co Ltd | Agente terapéutico para enfermedad con cuerpos de Lewy que contiene derivado de pirazoloquinolina |
| US11591312B2 (en) | 2018-01-23 | 2023-02-28 | Basf Se | Halogenation of pyridine derivatives |
| EP4349403A3 (en) | 2018-05-25 | 2024-06-05 | Cardurion Pharmaceuticals, Inc. | Monohydrate and crystalline forms of 6-[(3s,4s)-4-methyl-1- (pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-3-tetrahydropyran-4-yl- 7h-imid azo [1,5- a] pyrazin-8-one |
| MA53501A (fr) | 2018-08-31 | 2021-07-07 | Imara Inc | Inhibiteurs de pde9 pour le traitement de la drépanocytose |
| EP3894403A1 (en) | 2018-12-13 | 2021-10-20 | Intervet International B.V. | Process for preparing 1-[(3r,4s)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl)amino]p yrazole-4-carboxamide |
| IL287617B2 (en) | 2019-05-09 | 2024-11-01 | Feinstein Institutes For Medical Research | Hmgb1 antagonist |
| US10919882B2 (en) | 2019-05-09 | 2021-02-16 | The Feinstein Institutes For Medical Research | Compounds for use in synthesis of peptidomimetics |
| US11883461B2 (en) | 2019-05-09 | 2024-01-30 | The Feinstein Institutes For Medical Research | HMGB1 antagonist treatment of severe sepsis |
| EP3966201A4 (en) | 2019-05-09 | 2023-01-18 | The Feinstein Institutes for Medical Research | THIOSEMICARBAZATE AND THEIR USES |
| WO2021150613A1 (en) | 2020-01-20 | 2021-07-29 | Incyte Corporation | Spiro compounds as inhibitors of kras |
| IL297165A (en) * | 2020-04-16 | 2022-12-01 | Incyte Corp | Soysag tricyclic CRS inhibitors |
| US11739102B2 (en) | 2020-05-13 | 2023-08-29 | Incyte Corporation | Fused pyrimidine compounds as KRAS inhibitors |
| CA3188782A1 (en) | 2020-06-30 | 2022-01-06 | Bayer Aktiengesellschaft | Substituted heteroaryloxypyridines, the salts thereof and their use as herbicidal agents |
| WO2022047093A1 (en) | 2020-08-28 | 2022-03-03 | Incyte Corporation | Vinyl imidazole compounds as inhibitors of kras |
| US11767320B2 (en) | 2020-10-02 | 2023-09-26 | Incyte Corporation | Bicyclic dione compounds as inhibitors of KRAS |
| WO2022204112A1 (en) | 2021-03-22 | 2022-09-29 | Incyte Corporation | Imidazole and triazole kras inhibitors |
| CA3224674A1 (en) | 2021-07-07 | 2023-01-12 | Pei Gan | 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 |
| WO2023056421A1 (en) | 2021-10-01 | 2023-04-06 | Incyte Corporation | Pyrazoloquinoline kras inhibitors |
| IL312114A (en) | 2021-10-14 | 2024-06-01 | Incyte Corp | Quinoline compounds as Kras inhibitors |
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 |
| WO2005118583A1 (en) * | 2004-05-28 | 2005-12-15 | Millennium Pharmaceuticals, Inc. | 2, 5-dihydro-pyrazolo`4, 3-c!quinolin-4-ones as chk-1 inhibitors |
| CN101268073B (zh) | 2005-09-15 | 2011-10-19 | Aska制药株式会社 | 杂环化合物、制备方法及其用途 |
| JP2009184924A (ja) | 2006-05-31 | 2009-08-20 | Eisai R & D Management Co Ltd | 生物学的試薬用化合物 |
| CA2671980C (en) | 2006-12-13 | 2015-05-05 | Aska Pharmaceutical Co., Ltd. | Quinoxaline derivatives |
| DK2152712T3 (da) | 2007-05-11 | 2012-03-26 | Pfizer | Aminoheterocykliske fobindelser |
| 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 |
| ES2612954T3 (es) * | 2009-03-05 | 2017-05-19 | Astellas Pharma Inc. | Compuestos de quinoxalina |
| CA2757231A1 (en) | 2009-03-31 | 2010-10-07 | Boehringer Ingelheim International Gmbh | 1-heterocyclyl-1,5-dihydro-pyrazolo [3,4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| US8880976B2 (en) | 2009-09-25 | 2014-11-04 | Stmicroelectronics, Inc. | Method and apparatus for encoding LBA information into the parity of a LDPC system |
| EP2615089B1 (en) * | 2010-09-07 | 2016-04-27 | Astellas Pharma Inc. | Pyrazoloquinoline compounds |
| 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 |
-
2012
- 2012-10-04 EP EP12837953.4A patent/EP2769980B1/en active Active
- 2012-10-04 MX MX2014003800A patent/MX358149B/es active IP Right Grant
- 2012-10-04 AR ARP120103702A patent/AR088235A1/es active IP Right Grant
- 2012-10-04 IN IN2463CHN2014 patent/IN2014CN02463A/en unknown
- 2012-10-04 RS RS20160232A patent/RS54702B1/sr unknown
- 2012-10-04 JP JP2013537544A patent/JP5546693B2/ja active Active
- 2012-10-04 PH PH1/2014/500580A patent/PH12014500580A1/en unknown
- 2012-10-04 PL PL12837953T patent/PL2769980T3/pl unknown
- 2012-10-04 CA CA2861795A patent/CA2861795C/en active Active
- 2012-10-04 JO JOP/2012/0302A patent/JO3116B1/ar active
- 2012-10-04 SG SG11201400717QA patent/SG11201400717QA/en unknown
- 2012-10-04 RU RU2014112931/04A patent/RU2605096C2/ru active
- 2012-10-04 DK DK12837953.4T patent/DK2769980T3/en active
- 2012-10-04 US US13/644,745 patent/US8563565B2/en active Active
- 2012-10-04 MY MYPI2014700702A patent/MY167698A/en unknown
- 2012-10-04 ME MEP-2016-65A patent/ME02394B/me unknown
- 2012-10-04 KR KR1020147008769A patent/KR101943680B1/ko active Active
- 2012-10-04 HR HRP20160273TT patent/HRP20160273T1/hr unknown
- 2012-10-04 ES ES12837953.4T patent/ES2568015T3/es active Active
- 2012-10-04 HU HUE12837953A patent/HUE028555T2/en unknown
- 2012-10-04 SI SI201230501A patent/SI2769980T1/sl unknown
- 2012-10-04 AU AU2012319549A patent/AU2012319549B2/en active Active
- 2012-10-04 PE PE2014000408A patent/PE20141557A1/es active IP Right Grant
- 2012-10-04 BR BR112014007912-9A patent/BR112014007912B1/pt active IP Right Grant
- 2012-10-04 TW TW101136747A patent/TWI562993B/zh active
- 2012-10-04 CN CN201280046653.2A patent/CN103930423B/zh active Active
- 2012-10-04 WO PCT/JP2012/075748 patent/WO2013051639A1/ja not_active Ceased
-
2013
- 2013-06-11 US US13/914,898 patent/US20130296352A1/en not_active Abandoned
-
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
-
2016
- 2016-04-12 CY CY20161100302T patent/CY1117427T1/el unknown
- 2016-04-14 SM SM201600108T patent/SMT201600108B/xx unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |