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 |
|---|---|---|---|---|
| CN106905324B (zh) | 2011-10-10 | 2018-09-25 | H.隆德贝克有限公司 | 具有咪唑并吡嗪酮骨架的pde9抑制剂 |
| SG11201507897SA (en) * | 2013-04-05 | 2015-11-27 | Eisai R&D Man Co Ltd | Salt of pyrazoloquinoline derivative, and crystal thereof |
| KR102234131B1 (ko) * | 2013-04-05 | 2021-04-01 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 피리디닐피라졸로퀴놀린 화합물 |
| 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 |
| HRP20210543T1 (hr) | 2015-07-07 | 2021-05-14 | H. Lundbeck A/S | Inhibitori pde9 s imidazo triazinonskom okosnicom i imidazo pirazinonskom okosnicom za liječenje perifernih bolesti |
| 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 |
| CA3060183A1 (en) * | 2017-06-01 | 2018-12-06 | Eisai R&D Management Co., Ltd. | Dementia therapeutic agent combining pyrazoloquinoline derivative and memantine |
| CN110612102A (zh) * | 2017-06-01 | 2019-12-24 | 卫材R&D管理有限公司 | 含有吡唑并喹啉衍生物的路易氏体病治疗剂 |
| IL270395B (en) * | 2017-06-01 | 2022-08-01 | Eisai R&D Man Co Ltd | Dementia therapeutic agent combining pyrazoloquinoline derivative and donepezil |
| SG11201909359YA (en) * | 2017-06-01 | 2019-11-28 | Eisai R&D Man Co Ltd | Pharmaceutical composition comprising pde9 inhibitor |
| WO2019145176A1 (en) * | 2018-01-23 | 2019-08-01 | Basf Se | Halogenation of pyridine derivatives |
| 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 |
| EP3843737A4 (en) * | 2018-08-31 | 2022-06-01 | Imara Inc. | PDE9 INHIBITORS FOR THE TREATMENT OF SICKLE CELL DISEASE |
| CN119350306A (zh) | 2018-12-13 | 2025-01-24 | 英特维特国际股份有限公司 | 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-甲酰胺制备方法 |
| WO2020227592A1 (en) | 2019-05-09 | 2020-11-12 | The Feinstein Institutes For Medical Research | Thiosemicarbazates and uses thereof |
| US11883461B2 (en) | 2019-05-09 | 2024-01-30 | The Feinstein Institutes For Medical Research | HMGB1 antagonist treatment of severe sepsis |
| US11524048B2 (en) | 2019-05-09 | 2022-12-13 | The Feinstein Institutes For Medical Research | HMGB1 antagonist treatment of severe sepsis |
| AU2020268409A1 (en) * | 2019-05-09 | 2021-11-25 | The Feinstein Institutes For Medical Research | Compounds for use in synthesis of peptidomimetics |
| US11530218B2 (en) | 2020-01-20 | 2022-12-20 | Incyte Corporation | Spiro compounds as inhibitors of KRAS |
| PH12022552739A1 (en) * | 2020-04-16 | 2024-03-25 | Incyte Corp | Fused tricyclic kras inhibitors |
| US11739102B2 (en) | 2020-05-13 | 2023-08-29 | Incyte Corporation | Fused pyrimidine compounds as KRAS inhibitors |
| AU2021298813A1 (en) | 2020-06-30 | 2023-02-02 | 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 |
| 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 |
| US12441742B2 (en) | 2021-08-31 | 2025-10-14 | 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 |
| JP2024537824A (ja) | 2021-10-01 | 2024-10-16 | インサイト・コーポレイション | ピラゾロキノリンｋｒａｓ阻害剤 |
| MX2024004444A (es) | 2021-10-14 | 2024-05-08 | Incyte Corp | Compuestos de quinolina como inhibidores de la proteina del virus de sarcoma de rata kirsten (kras). |
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 |
| 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 |
| ES2599054T3 (es) * | 2006-12-13 | 2017-01-31 | Aska Pharmaceutical Co., Ltd. | Derivados de quinoxalina |
| SI2152712T1 (sl) | 2007-05-11 | 2012-03-30 | Pfizer | Amino heterociklične spojine |
| 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 |
| CN102341399A (zh) * | 2009-03-05 | 2012-02-01 | 安斯泰来制药株式会社 | 喹喔啉化合物 |
| PE20120505A1 (es) | 2009-03-31 | 2012-05-09 | Boehringer Ingelheim Int | Derivados de 1-heterociclil-1,5-dihidro-pirazolo[3,4-d]pirimidin-4-ona como moduladores de pde9a |
| 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 JO JOP/2012/0302A patent/JO3116B1/ar active
- 2012-10-04 TW TW101136747A patent/TWI562993B/zh active
- 2012-10-04 AU AU2012319549A patent/AU2012319549B2/en active Active
- 2012-10-04 RU RU2014112931/04A patent/RU2605096C2/ru active
- 2012-10-04 JP JP2013537544A patent/JP5546693B2/ja active Active
- 2012-10-04 ES ES12837953.4T patent/ES2568015T3/es active Active
- 2012-10-04 SG SG11201400717QA patent/SG11201400717QA/en unknown
- 2012-10-04 KR KR1020147008769A patent/KR101943680B1/ko active Active
- 2012-10-04 IN IN2463CHN2014 patent/IN2014CN02463A/en unknown
- 2012-10-04 CN CN201280046653.2A patent/CN103930423B/zh active Active
- 2012-10-04 SI SI201230501A patent/SI2769980T1/sl unknown
- 2012-10-04 EP EP12837953.4A patent/EP2769980B1/en active Active
- 2012-10-04 US US13/644,745 patent/US8563565B2/en active Active
- 2012-10-04 PH PH1/2014/500580A patent/PH12014500580A1/en unknown
- 2012-10-04 PE PE2014000408A patent/PE20141557A1/es active IP Right Grant
- 2012-10-04 HR HRP20160273TT patent/HRP20160273T1/hr unknown
- 2012-10-04 PL PL12837953T patent/PL2769980T3/pl unknown
- 2012-10-04 CA CA2861795A patent/CA2861795C/en active Active
- 2012-10-04 RS RS20160232A patent/RS54702B1/sr unknown
- 2012-10-04 HU HUE12837953A patent/HUE028555T2/en unknown
- 2012-10-04 AR ARP120103702A patent/AR088235A1/es active IP Right Grant
- 2012-10-04 MY MYPI2014700702A patent/MY167698A/en unknown
- 2012-10-04 ME MEP-2016-65A patent/ME02394B/me unknown
- 2012-10-04 BR BR112014007912-9A patent/BR112014007912B1/pt active IP Right Grant
- 2012-10-04 DK DK12837953.4T patent/DK2769980T3/en active
- 2012-10-04 WO PCT/JP2012/075748 patent/WO2013051639A1/ja not_active Ceased
- 2012-10-04 MX MX2014003800A patent/MX358149B/es active IP Right Grant
-
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 |