BR112014007912A2 - derivados de pirazoloquinolina - Google Patents
derivados de pirazoloquinolinaInfo
- Publication number
- BR112014007912A2 BR112014007912A2 BR112014007912A BR112014007912A BR112014007912A2 BR 112014007912 A2 BR112014007912 A2 BR 112014007912A2 BR 112014007912 A BR112014007912 A BR 112014007912A BR 112014007912 A BR112014007912 A BR 112014007912A BR 112014007912 A2 BR112014007912 A2 BR 112014007912A2
- Authority
- BR
- Brazil
- Prior art keywords
- hydrogen atom
- cgmp
- acceptable salt
- level
- pde9
- Prior art date
Links
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
resumo derivados de pirazoloquinolina um composto, representado pela fórmula (i), ou um sal farmacologicamente aceitável do mesmo, que tem ação inibidora de pde9, de modo que é previsível que seja capaz de elevar o nível de cgmp no cérebro. uma vez que a ação inibitória sobre o pde9 e um aumento do nível de cgmp contribuem para a melhoria dos comportamentos de aprendizagem e memória, o composto (i) acima citado, ou um sal farmacologicamente aceitável do mesmo, estará disponível como medicamento para disfunções cognitivas na doença de alzheimer. em que r1 representa um átomo de hidrogênio; r2 representa um grupo de anel aromático, etc.; r3 representa um átomo de hidrogênio, etc.; r4 representa um é um átomo de hidrogênio; r5 representa um grupo oxepanila, etc.; r6 representa um átomo de hidrogênio.
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161544860P | 2011-10-07 | 2011-10-07 | |
| US61/544.860 | 2011-10-07 | ||
| US201161550623P | 2011-10-24 | 2011-10-24 | |
| US61/550.623 | 2011-10-24 | ||
| US201161558110P | 2011-11-10 | 2011-11-10 | |
| US61/558.110 | 2011-11-10 | ||
| US201161580903P | 2011-12-28 | 2011-12-28 | |
| US61/580.903 | 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 |
|---|---|
| BR112014007912A2 true BR112014007912A2 (pt) | 2017-04-04 |
| BR112014007912B1 BR112014007912B1 (pt) | 2022-06-07 |
Family
ID=48043792
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112014007912-9A BR112014007912B1 (pt) | 2011-10-07 | 2012-10-04 | Derivados de pirazoloquinolina |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US8563565B2 (pt) |
| EP (1) | EP2769980B1 (pt) |
| JP (1) | JP5546693B2 (pt) |
| KR (1) | KR101943680B1 (pt) |
| CN (1) | CN103930423B (pt) |
| AR (1) | AR088235A1 (pt) |
| AU (1) | AU2012319549B2 (pt) |
| BR (1) | BR112014007912B1 (pt) |
| CA (1) | CA2861795C (pt) |
| CL (1) | CL2014000821A1 (pt) |
| CO (1) | CO6910200A2 (pt) |
| CY (1) | CY1117427T1 (pt) |
| DK (1) | DK2769980T3 (pt) |
| ES (1) | ES2568015T3 (pt) |
| HK (1) | HK1199018A1 (pt) |
| HR (1) | HRP20160273T1 (pt) |
| HU (1) | HUE028555T2 (pt) |
| IL (1) | IL231650A (pt) |
| IN (1) | IN2014CN02463A (pt) |
| JO (1) | JO3116B1 (pt) |
| ME (1) | ME02394B (pt) |
| MX (1) | MX358149B (pt) |
| MY (1) | MY167698A (pt) |
| PE (1) | PE20141557A1 (pt) |
| PL (1) | PL2769980T3 (pt) |
| RS (1) | RS54702B1 (pt) |
| RU (1) | RU2605096C2 (pt) |
| SG (1) | SG11201400717QA (pt) |
| SI (1) | SI2769980T1 (pt) |
| SM (1) | SMT201600108B (pt) |
| TW (1) | TWI562993B (pt) |
| WO (1) | WO2013051639A1 (pt) |
| ZA (1) | ZA201402439B (pt) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201502728WA (en) | 2011-10-10 | 2015-05-28 | Lundbeck & Co As H | Pde9i with imidazo pyrazinone backbone |
| SG11201507897SA (en) * | 2013-04-05 | 2015-11-27 | Eisai R&D Man Co Ltd | Salt of pyrazoloquinoline derivative, and crystal thereof |
| CN105189496B (zh) * | 2013-04-05 | 2017-03-29 | 卫材R&D管理有限公司 | 吡啶基吡唑并喹啉化合物 |
| 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 |
| PT3865484T (pt) | 2015-07-07 | 2024-01-30 | H Lundbeck As | Inibidor da pde9 com esqueleto de imidazo pirazinona para tratamento de doenças periféricas |
| 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 |
| BR112019023557A2 (pt) | 2017-06-01 | 2020-06-02 | Eisai R&D Management Co., Ltd. | Composição farmacêutica compreendendo inibidor de pde9 |
| MX2019013397A (es) * | 2017-06-01 | 2020-02-07 | Eisai R&D Man Co Ltd | Agente terapeutico para enfermedad con cuerpos de lewy que contiene derivado de pirazoloquinolina. |
| 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 |
| ES2980131T3 (es) * | 2017-06-01 | 2024-09-30 | Eisai R&D Man Co Ltd | Agente terapéutico para la demencia que combina derivado de pirazoloquinolina y donepezilo |
| CN111630042A (zh) | 2018-01-23 | 2020-09-04 | 巴斯夫欧洲公司 | 吡啶衍生物的卤化 |
| SI3801526T1 (sl) | 2018-05-25 | 2024-05-31 | Cardurion Pharmaceuticals, Inc. | Monohidratne in kristalinične oblike 6-((3s, 4s)-4-metil-1-(pirimidin-2-ilmetil)pirolidin-3-il)-3-tetrahidropiran-4- il-7h-imidazo (1.5 - a) pirazin-8-ona |
| EP3843737A4 (en) * | 2018-08-31 | 2022-06-01 | Imara Inc. | PDE9 INHIBITORS FOR THE TREATMENT OF SICKLE CELL DISEASE |
| CA3122183A1 (en) * | 2018-12-13 | 2020-06-18 | 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 |
| EP3965770A4 (en) | 2019-05-09 | 2023-01-18 | The Feinstein Institutes for Medical Research | COMPOUNDS FOR USE IN THE SYNTHESIS OF PEPTIDOMIMETICS |
| CA3139109A1 (en) | 2019-05-09 | 2020-11-12 | The Feinstein Institutes For Medical Research | Hmgb1 antagonist |
| AU2020270125A1 (en) | 2019-05-09 | 2021-11-25 | 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 |
| WO2021150613A1 (en) | 2020-01-20 | 2021-07-29 | Incyte Corporation | Spiro compounds as inhibitors of kras |
| US20210355121A1 (en) * | 2020-04-16 | 2021-11-18 | Incyte Corporation | Fused tricyclic kras inhibitors |
| US11739102B2 (en) | 2020-05-13 | 2023-08-29 | 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. |
| US11999752B2 (en) | 2020-08-28 | 2024-06-04 | 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 |
| US12077539B2 (en) | 2021-03-22 | 2024-09-03 | Incyte Corporation | Imidazole and triazole KRAS inhibitors |
| WO2023049697A1 (en) | 2021-09-21 | 2023-03-30 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of kras |
| WO2023056421A1 (en) | 2021-10-01 | 2023-04-06 | 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 |
| CA2622605A1 (en) * | 2005-09-15 | 2007-03-22 | Aska Pharmaceutical Co., Ltd. | Heterocycle compound, and production process and application thereof |
| 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 |
| JP4579346B2 (ja) | 2007-05-11 | 2010-11-10 | ファイザー・インク | アミノ複素環式化合物 |
| 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 |
| ES2460019T3 (es) | 2009-03-31 | 2014-05-13 | Boehringer Ingelheim International Gmbh | Derivados de 1-heterociclil-1,5-dihidro-pirazolo[3,4-d]pirimidin-4-ona y su uso 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 |
| SI2615089T1 (sl) | 2010-09-07 | 2016-08-31 | Astellas Pharma Inc. | Spojine pirazolokinolina |
| 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 IN IN2463CHN2014 patent/IN2014CN02463A/en unknown
- 2012-10-04 SI SI201230501A patent/SI2769980T1/sl unknown
- 2012-10-04 RS RS20160232A patent/RS54702B1/en unknown
- 2012-10-04 JP JP2013537544A patent/JP5546693B2/ja active Active
- 2012-10-04 MY MYPI2014700702A patent/MY167698A/en unknown
- 2012-10-04 RU RU2014112931/04A patent/RU2605096C2/ru active
- 2012-10-04 TW TW101136747A patent/TWI562993B/zh active
- 2012-10-04 MX MX2014003800A patent/MX358149B/es active IP Right Grant
- 2012-10-04 BR BR112014007912-9A patent/BR112014007912B1/pt active IP Right Grant
- 2012-10-04 US US13/644,745 patent/US8563565B2/en active Active
- 2012-10-04 ES ES12837953.4T patent/ES2568015T3/es active Active
- 2012-10-04 WO PCT/JP2012/075748 patent/WO2013051639A1/ja active Application Filing
- 2012-10-04 PE PE2014000408A patent/PE20141557A1/es active IP Right Grant
- 2012-10-04 JO JOP/2012/0302A patent/JO3116B1/ar active
- 2012-10-04 DK DK12837953.4T patent/DK2769980T3/en active
- 2012-10-04 CA CA2861795A patent/CA2861795C/en active Active
- 2012-10-04 AR ARP120103702A patent/AR088235A1/es active IP Right Grant
- 2012-10-04 AU AU2012319549A patent/AU2012319549B2/en active Active
- 2012-10-04 ME MEP-2016-65A patent/ME02394B/me unknown
- 2012-10-04 HU HUE12837953A patent/HUE028555T2/en unknown
- 2012-10-04 EP EP12837953.4A patent/EP2769980B1/en active Active
- 2012-10-04 PL PL12837953T patent/PL2769980T3/pl unknown
- 2012-10-04 KR KR1020147008769A patent/KR101943680B1/ko active IP Right Grant
- 2012-10-04 CN CN201280046653.2A patent/CN103930423B/zh active Active
- 2012-10-04 SG SG11201400717QA patent/SG11201400717QA/en unknown
-
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
- 2014-12-08 HK HK14112316.6A patent/HK1199018A1/zh unknown
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2016
- 2016-03-17 HR HRP20160273TT patent/HRP20160273T1/hr unknown
- 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 |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
|
| B06T | Formal requirements before examination [chapter 6.20 patent gazette] | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 04/10/2012, OBSERVADAS AS CONDICOES LEGAIS |