JP6322275B2 - ヤヌスキナーゼ阻害剤としてのn−(2−シアノヘテロシクリル)ピラゾロピリドン - Google Patents
ヤヌスキナーゼ阻害剤としてのn−(2−シアノヘテロシクリル)ピラゾロピリドン Download PDFInfo
- Publication number
- JP6322275B2 JP6322275B2 JP2016503522A JP2016503522A JP6322275B2 JP 6322275 B2 JP6322275 B2 JP 6322275B2 JP 2016503522 A JP2016503522 A JP 2016503522A JP 2016503522 A JP2016503522 A JP 2016503522A JP 6322275 B2 JP6322275 B2 JP 6322275B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amino
- oxo
- dihydro
- pyrazolo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 0 NC1OC1**1CC1 Chemical compound NC1OC1**1CC1 0.000 description 5
- CJWUEYVSXIFIEQ-UHFFFAOYSA-N FC(C1(c(cc2)ccc2Br)NCCCC1)(F)F Chemical compound FC(C1(c(cc2)ccc2Br)NCCCC1)(F)F CJWUEYVSXIFIEQ-UHFFFAOYSA-N 0.000 description 2
- FTNJQNQLEGKTGD-UHFFFAOYSA-N C1Oc(cccc2)c2O1 Chemical compound C1Oc(cccc2)c2O1 FTNJQNQLEGKTGD-UHFFFAOYSA-N 0.000 description 1
- ZWLWJQBJGOXGMA-UHFFFAOYSA-N CC(C(F)(F)F)(c(cc1)ccc1Br)O Chemical compound CC(C(F)(F)F)(c(cc1)ccc1Br)O ZWLWJQBJGOXGMA-UHFFFAOYSA-N 0.000 description 1
- NDMYZUAGQDLNFK-LBAUFKAWSA-N C[C@@H]1C(C[n](c2c3c(OCc4ccccc4)ncc2)nc3N)COCC1 Chemical compound C[C@@H]1C(C[n](c2c3c(OCc4ccccc4)ncc2)nc3N)COCC1 NDMYZUAGQDLNFK-LBAUFKAWSA-N 0.000 description 1
- WVJDAMKIMYNHDG-UHFFFAOYSA-N Cc(cc1CN2)ccc1S2(=O)=O Chemical compound Cc(cc1CN2)ccc1S2(=O)=O WVJDAMKIMYNHDG-UHFFFAOYSA-N 0.000 description 1
- MODBIOPSUQSMJX-LBAUFKAWSA-N Nc1n[n](C(COCC2)[C@@H]2C#N)c2c1c(OCc1ccccc1)ncc2 Chemical compound Nc1n[n](C(COCC2)[C@@H]2C#N)c2c1c(OCc1ccccc1)ncc2 MODBIOPSUQSMJX-LBAUFKAWSA-N 0.000 description 1
- PHWPRSZULISLMK-UHFFFAOYSA-N OC(C(F)(F)F)c(cc1)ccc1Br Chemical compound OC(C(F)(F)F)c(cc1)ccc1Br PHWPRSZULISLMK-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361803226P | 2013-03-19 | 2013-03-19 | |
| US61/803,226 | 2013-03-19 | ||
| PCT/CN2014/000298 WO2014146492A1 (en) | 2013-03-19 | 2014-03-19 | N-(2-cyano heterocyclyl)pyrazolo pyridones as janus kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016514710A JP2016514710A (ja) | 2016-05-23 |
| JP2016514710A5 JP2016514710A5 (enExample) | 2017-04-13 |
| JP6322275B2 true JP6322275B2 (ja) | 2018-05-09 |
Family
ID=51579321
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016503522A Active JP6322275B2 (ja) | 2013-03-19 | 2014-03-19 | ヤヌスキナーゼ阻害剤としてのn−(2−シアノヘテロシクリル)ピラゾロピリドン |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9957265B2 (enExample) |
| EP (1) | EP2976338B1 (enExample) |
| JP (1) | JP6322275B2 (enExample) |
| KR (1) | KR20150130311A (enExample) |
| CN (1) | CN105189497B (enExample) |
| AU (1) | AU2014234908B2 (enExample) |
| BR (1) | BR112015023878A2 (enExample) |
| CA (1) | CA2901766A1 (enExample) |
| MX (1) | MX2015013414A (enExample) |
| RU (1) | RU2669922C2 (enExample) |
| WO (1) | WO2014146492A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014146246A1 (en) * | 2013-03-19 | 2014-09-25 | Merck Sharp & Dohme Corp. | Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors |
| WO2016061751A1 (en) | 2014-10-22 | 2016-04-28 | Merck Sharp & Dohme Corp. | Ethyl n-boc piperidinyl pyrazolo pyridones as janus kinase inhibitors |
| WO2018111663A1 (en) * | 2016-12-14 | 2018-06-21 | Merck Sharp & Dohme Corp. | Aminopyrazoles as janus kinase inhibitors |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN111499592B (zh) * | 2020-03-14 | 2023-06-23 | 江苏省农用激素工程技术研究中心有限公司 | 5-氨甲基糖精的合成方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2759227B2 (ja) | 1990-09-28 | 1998-05-28 | 大鵬薬品工業株式会社 | ピラゾロピリジン誘導体 |
| CN1636005A (zh) | 1999-06-03 | 2005-07-06 | 克诺尔股份有限公司 | 苯并噻嗪酮和苯并噁嗪酮化合物 |
| AU2003217863B9 (en) | 2002-02-28 | 2009-10-29 | Biota Scientific Management Pty Ltd | Nucleotide mimics and their prodrugs |
| TW200406385A (en) | 2002-05-31 | 2004-05-01 | Eisai Co Ltd | Pyrazole compound and pharmaceutical composition containing the same |
| JP4139185B2 (ja) | 2002-10-17 | 2008-08-27 | 京セラ株式会社 | 配線基板の製造方法 |
| NZ601687A (en) * | 2006-01-17 | 2014-03-28 | Vertex Pharma | Azaindoles useful as inhibitors of janus kinases |
| JP5287253B2 (ja) | 2007-01-12 | 2013-09-11 | アステラス製薬株式会社 | 縮合ピリジン化合物 |
| US9346809B2 (en) | 2009-07-08 | 2016-05-24 | Leo Pharma A/S | Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors |
| PH12015502575A1 (en) | 2010-03-10 | 2017-04-24 | Incyte Corp | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| WO2012127506A1 (en) | 2011-03-22 | 2012-09-27 | Advinus Therapeutics Limited | Substituted fused tricyclic compounds, compositions and medicinal applications thereof |
| ES2633793T3 (es) * | 2011-09-22 | 2017-09-25 | Merck Sharp & Dohme Corp. | Pirazol carboxamidas como inhibidores de quinasa Janus |
| EP2857400A4 (en) | 2012-06-01 | 2015-12-09 | Takeda Pharmaceutical | HETEROCYCLIC CONNECTION |
| WO2014146246A1 (en) * | 2013-03-19 | 2014-09-25 | Merck Sharp & Dohme Corp. | Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors |
-
2014
- 2014-03-19 US US14/778,052 patent/US9957265B2/en active Active
- 2014-03-19 AU AU2014234908A patent/AU2014234908B2/en not_active Ceased
- 2014-03-19 KR KR1020157025519A patent/KR20150130311A/ko not_active Withdrawn
- 2014-03-19 CN CN201480016754.4A patent/CN105189497B/zh not_active Expired - Fee Related
- 2014-03-19 EP EP14767458.4A patent/EP2976338B1/en active Active
- 2014-03-19 RU RU2015144483A patent/RU2669922C2/ru not_active IP Right Cessation
- 2014-03-19 CA CA2901766A patent/CA2901766A1/en not_active Abandoned
- 2014-03-19 WO PCT/CN2014/000298 patent/WO2014146492A1/en not_active Ceased
- 2014-03-19 BR BR112015023878A patent/BR112015023878A2/pt not_active Application Discontinuation
- 2014-03-19 JP JP2016503522A patent/JP6322275B2/ja active Active
- 2014-03-19 MX MX2015013414A patent/MX2015013414A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US9957265B2 (en) | 2018-05-01 |
| JP2016514710A (ja) | 2016-05-23 |
| EP2976338A4 (en) | 2016-08-31 |
| AU2014234908A1 (en) | 2015-08-13 |
| RU2015144483A (ru) | 2017-04-25 |
| RU2669922C2 (ru) | 2018-10-17 |
| US20160272633A1 (en) | 2016-09-22 |
| BR112015023878A2 (pt) | 2017-07-18 |
| CN105189497A (zh) | 2015-12-23 |
| EP2976338A1 (en) | 2016-01-27 |
| CN105189497B (zh) | 2019-05-03 |
| WO2014146492A1 (en) | 2014-09-25 |
| CA2901766A1 (en) | 2014-09-25 |
| KR20150130311A (ko) | 2015-11-23 |
| EP2976338B1 (en) | 2018-01-03 |
| AU2014234908B2 (en) | 2017-08-17 |
| MX2015013414A (es) | 2016-02-26 |
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