TWI487701B - 作為蛋白質激酶抑制劑之化合物及組合物 - Google Patents
作為蛋白質激酶抑制劑之化合物及組合物 Download PDFInfo
- Publication number
- TWI487701B TWI487701B TW099128938A TW99128938A TWI487701B TW I487701 B TWI487701 B TW I487701B TW 099128938 A TW099128938 A TW 099128938A TW 99128938 A TW99128938 A TW 99128938A TW I487701 B TWI487701 B TW I487701B
- Authority
- TW
- Taiwan
- Prior art keywords
- methyl
- imidazol
- pyrimidin
- cyclopropyl
- propan
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P25/24—Antidepressants
-
- 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
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23808309P | 2009-08-28 | 2009-08-28 | |
| US31306110P | 2010-03-11 | 2010-03-11 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201111365A TW201111365A (en) | 2011-04-01 |
| TWI487701B true TWI487701B (zh) | 2015-06-11 |
Family
ID=42829939
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW099128938A TWI487701B (zh) | 2009-08-28 | 2010-08-27 | 作為蛋白質激酶抑制劑之化合物及組合物 |
Country Status (19)
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR077975A1 (es) | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| BR112012021411A2 (pt) | 2010-02-25 | 2017-04-18 | Dana Farber Cancer Inst Inc | mutações braf que conferem resistência a inibidores braf. |
| WO2013059634A1 (en) | 2011-10-20 | 2013-04-25 | The Regents Of The University Of California | Use of cdk9 inhibitors to reduce cartilage degradation |
| EP2776037B1 (en) | 2011-11-11 | 2019-01-09 | Novartis AG | Method of treating a proliferative disease |
| KR102091295B1 (ko) | 2011-11-23 | 2020-03-19 | 어레이 바이오파마 인크. | 제약 제제 |
| US9408885B2 (en) | 2011-12-01 | 2016-08-09 | Vib Vzw | Combinations of therapeutic agents for treating melanoma |
| US20150232452A1 (en) * | 2012-09-19 | 2015-08-20 | Ruga Corporation | Novel raf kinase inhibitors |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| WO2014194127A1 (en) * | 2013-05-30 | 2014-12-04 | Plexxikon Inc. | Compounds for kinase modulation, and indications therefor |
| AR096721A1 (es) | 2013-06-25 | 2016-01-27 | Bristol Myers Squibb Co | Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos |
| AU2014302550A1 (en) | 2013-06-25 | 2016-02-11 | Bristol-Myers Squibb Company | Carbazole carboxamide compounds useful as kinase inhibitors |
| LT3038622T (lt) * | 2013-08-28 | 2018-07-25 | Medivation Technologies Llc | Heterocikliniai junginiai ir jų naudojimo būdai |
| GB2517988A (en) * | 2013-09-09 | 2015-03-11 | Redx Pharma Ltd | Compounds |
| UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
| US10300073B2 (en) | 2014-10-14 | 2019-05-28 | The Regents Of The University Of California | Use of CDK9 and BRD4 inhibitors to inhibit inflammation |
| CN104402920B (zh) * | 2014-11-27 | 2018-04-03 | 河南科技学院 | 一种合成2‑卤代‑3‑频那醇硼酸酯‑5‑氯苯胺的方法 |
| AU2017329090B9 (en) | 2016-09-19 | 2019-09-05 | Novartis Ag | Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor |
| WO2018146253A1 (en) | 2017-02-10 | 2018-08-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway |
| US11725185B2 (en) | 2017-12-28 | 2023-08-15 | University Of Houston System | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
| WO2020124397A1 (en) * | 2018-12-19 | 2020-06-25 | Inventisbio Shanghai Ltd. | C-terminal src kinase inhibitors |
| US20230303551A1 (en) * | 2020-08-13 | 2023-09-28 | Albert Einstein College Of Medicine | N-cyclyl-sulfonamides useful for inhibiting raf |
| WO2023240024A1 (en) | 2022-06-08 | 2023-12-14 | Nikang Therapeutics, Inc. | Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2659739A (en) | 1950-04-14 | 1953-11-17 | Eastman Kodak Co | 1-hydroxy-4-beta-cyanopropylamino-anthraquinone and process for preparing same |
| US6358932B1 (en) | 1994-05-31 | 2002-03-19 | Isis Pharmaceticals, Inc. | Antisense oligonucleotide inhibition of raf gene expression |
| US6391636B1 (en) | 1994-05-31 | 2002-05-21 | Isis Pharmaceuticals, Inc. | Antisense oligonucleotide modulation of raf gene expression |
| US6037136A (en) | 1994-10-24 | 2000-03-14 | Cold Spring Harbor Laboratory | Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto |
| US5717100A (en) | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
| GB2306108A (en) * | 1995-10-13 | 1997-04-30 | Merck & Co Inc | Treatment of Raf-mediated cancers with imidazole derivatives |
| WO1997044058A1 (en) | 1996-05-23 | 1997-11-27 | Applied Research Systems Ars Holding N.V. | Compounds that inhibit the binding of raf-1 or 14-3-3 proteins to the beta chain of il-2 receptor, and pharmaceutical compositions containing same |
| AR012634A1 (es) | 1997-05-02 | 2000-11-08 | Sugen Inc | Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion |
| US6187799B1 (en) | 1997-05-23 | 2001-02-13 | Onyx Pharmaceuticals | Inhibition of raf kinase activity using aryl ureas |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| US6022884A (en) | 1997-11-07 | 2000-02-08 | Amgen Inc. | Substituted pyridine compounds and methods of use |
| US6204467B1 (en) | 1998-03-24 | 2001-03-20 | Ford Global Technologies, Inc. | Method and apparatus for resistive welding |
| ME00275B (me) | 1999-01-13 | 2011-02-10 | Bayer Corp | ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE |
| WO2002018654A1 (en) | 2000-08-30 | 2002-03-07 | The Board Of Trustees Of The University Of Arkansas | Induction of ldl receptor expression by extracellular-signal regulated kinase, erk-1/2 |
| HUE025767T2 (en) | 2002-03-13 | 2016-05-30 | Array Biopharma Inc | N3-alkylated benzimidazole derivatives as MEK inhibitors |
| US6644516B1 (en) | 2002-11-06 | 2003-11-11 | Continental Afa Dispensing Company | Foaming liquid dispenser |
| AU2006217742A1 (en) | 2005-02-25 | 2006-08-31 | Kudos Pharmaceuticals Limited | Hydrazinomethyl, HYDR zonomethyl and 5-membered heterocylic compounds which act as MTOR inhibitors and their use as anti cancer agents |
| AU2006217744A1 (en) | 2005-02-25 | 2006-08-31 | Kudos Pharmaceuticals Limited | 2,4-diamino-pyridopyrimidine derivatives and their use as MTOR inhibitors |
| CA2628920C (en) | 2005-11-22 | 2015-12-29 | Kudos Pharmaceuticals Limited | Pyrido-,pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors |
| CA2635997A1 (en) | 2006-01-11 | 2007-07-19 | Astrazeneca Ab | Morpholino pyrimidine derivatives and their use in therapy |
| MY148688A (en) | 2006-08-23 | 2013-05-31 | Kudos Pharm Ltd | 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors |
| TW200922582A (en) | 2007-08-20 | 2009-06-01 | Organon Nv | N-benzyl, N'-arylcarbonylpiperazine derivatives |
| US8129394B2 (en) * | 2008-03-21 | 2012-03-06 | Novartis Ag | Heteroaryl-substituted imidazole compounds and uses thereof |
| UA103319C2 (en) | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| ATE557015T1 (de) | 2008-07-24 | 2012-05-15 | Nerviano Medical Sciences Srl | 3,4-diarylpyrazole als proteinkinaseinhibitoren |
-
2010
- 2010-08-24 US US12/862,418 patent/US8242260B2/en not_active Expired - Fee Related
- 2010-08-26 MX MX2012002542A patent/MX2012002542A/es active IP Right Grant
- 2010-08-26 JP JP2012526067A patent/JP5726190B2/ja active Active
- 2010-08-26 PL PL10745280T patent/PL2470528T3/pl unknown
- 2010-08-26 AU AU2010288455A patent/AU2010288455B2/en not_active Ceased
- 2010-08-26 WO PCT/EP2010/062495 patent/WO2011023773A1/en active Application Filing
- 2010-08-26 BR BR112012004448A patent/BR112012004448A2/pt not_active Application Discontinuation
- 2010-08-26 ES ES10745280.7T patent/ES2527176T3/es active Active
- 2010-08-26 JO JOP/2010/0298A patent/JO3007B1/ar active
- 2010-08-26 CN CN201080038235.XA patent/CN102596937B/zh active Active
- 2010-08-26 IN IN869DEN2012 patent/IN2012DN00869A/en unknown
- 2010-08-26 PT PT107452807T patent/PT2470528E/pt unknown
- 2010-08-26 CA CA2771673A patent/CA2771673C/en not_active Expired - Fee Related
- 2010-08-26 AR ARP100103125A patent/AR077977A1/es unknown
- 2010-08-26 EP EP10745280.7A patent/EP2470528B1/en active Active
- 2010-08-26 EA EA201200323A patent/EA020479B1/ru not_active IP Right Cessation
- 2010-08-26 KR KR1020127007838A patent/KR101714107B1/ko active IP Right Grant
- 2010-08-27 UY UY0001032859A patent/UY32859A/es not_active Application Discontinuation
- 2010-08-27 TW TW099128938A patent/TWI487701B/zh not_active IP Right Cessation
-
2012
- 2012-05-16 US US13/473,230 patent/US8563553B2/en active Active
-
2013
- 2013-09-10 US US14/022,540 patent/US8859548B2/en active Active
Non-Patent Citations (1)
| Title |
|---|
| Bioorganic & Medicinal Chemistry Letters, 2008,Vol:18, Nr:9, Page(s):2825 – 2829 * |
Also Published As
| Publication number | Publication date |
|---|---|
| UY32859A (es) | 2011-03-31 |
| US8859548B2 (en) | 2014-10-14 |
| JP2013503139A (ja) | 2013-01-31 |
| US20140011825A1 (en) | 2014-01-09 |
| EA201200323A1 (ru) | 2012-09-28 |
| EP2470528B1 (en) | 2014-10-01 |
| ES2527176T3 (es) | 2015-01-21 |
| WO2011023773A1 (en) | 2011-03-03 |
| PT2470528E (pt) | 2014-12-29 |
| KR101714107B1 (ko) | 2017-03-08 |
| IN2012DN00869A (US07122547-20061017-C00088.png) | 2015-07-10 |
| JP5726190B2 (ja) | 2015-05-27 |
| TW201111365A (en) | 2011-04-01 |
| US8563553B2 (en) | 2013-10-22 |
| BR112012004448A2 (pt) | 2017-05-30 |
| US20120225899A1 (en) | 2012-09-06 |
| CN102596937B (zh) | 2014-02-12 |
| JO3007B1 (ar) | 2016-09-05 |
| EP2470528A1 (en) | 2012-07-04 |
| KR20120092577A (ko) | 2012-08-21 |
| CN102596937A (zh) | 2012-07-18 |
| US20110052578A1 (en) | 2011-03-03 |
| PL2470528T3 (pl) | 2015-03-31 |
| MX2012002542A (es) | 2012-04-02 |
| US8242260B2 (en) | 2012-08-14 |
| CA2771673C (en) | 2016-07-12 |
| CA2771673A1 (en) | 2011-03-03 |
| EA020479B1 (ru) | 2014-11-28 |
| AU2010288455B2 (en) | 2013-01-31 |
| AR077977A1 (es) | 2011-10-05 |
| AU2010288455A1 (en) | 2012-02-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Annulment or lapse of patent due to non-payment of fees |