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 PDF

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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
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TW
Taiwan
Prior art keywords
methyl
imidazol
pyrimidin
cyclopropyl
propan
Prior art date
Application number
TW099128938A
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English (en)
Chinese (zh)
Other versions
TW201111365A (en
Inventor
Abran Q Costales
Shenlin Huang
Jeff Xianming Jin
Zuosheng Liu
Sabina Pecchi
Daniel Poon
John TELLEW
Original Assignee
Novartis Ag
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Application filed by Novartis Ag filed Critical Novartis Ag
Publication of TW201111365A publication Critical patent/TW201111365A/zh
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Publication of TWI487701B publication Critical patent/TWI487701B/zh

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    • 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

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  • 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)
TW099128938A 2009-08-28 2010-08-27 作為蛋白質激酶抑制劑之化合物及組合物 TWI487701B (zh)

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

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Family Applications (1)

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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)

Country Link
US (3) US8242260B2 (enExample)
EP (1) EP2470528B1 (enExample)
JP (1) JP5726190B2 (enExample)
KR (1) KR101714107B1 (enExample)
CN (1) CN102596937B (enExample)
AR (1) AR077977A1 (enExample)
AU (1) AU2010288455B2 (enExample)
BR (1) BR112012004448A2 (enExample)
CA (1) CA2771673C (enExample)
EA (1) EA020479B1 (enExample)
ES (1) ES2527176T3 (enExample)
IN (1) IN2012DN00869A (enExample)
JO (1) JO3007B1 (enExample)
MX (1) MX2012002542A (enExample)
PL (1) PL2470528T3 (enExample)
PT (1) PT2470528E (enExample)
TW (1) TWI487701B (enExample)
UY (1) UY32859A (enExample)
WO (1) WO2011023773A1 (enExample)

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US9498471B2 (en) 2011-10-20 2016-11-22 The Regents Of The University Of California Use of CDK9 inhibitors to reduce cartilage degradation
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RS58048B1 (sr) 2011-11-23 2019-02-28 Array Biopharma Inc Farmaceutske formulacije
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
RU2015149937A (ru) 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
TWI648272B (zh) 2013-06-25 2019-01-21 美商必治妥美雅史谷比公司 經取代之四氫咔唑及咔唑甲醯胺化合物
CN105473573B (zh) 2013-06-25 2018-03-16 百时美施贵宝公司 用作激酶抑制剂的咔唑甲酰胺化合物
WO2015031650A1 (en) * 2013-08-28 2015-03-05 Sarvajit Chakravarty Heterocyclic compounds and methods of use
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
WO2016061144A1 (en) 2014-10-14 2016-04-21 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
ES2974991T3 (es) 2016-09-19 2024-07-02 Novartis Ag Combinaciones terapéuticas que comprenden un inhibidor de RAF y un inhibidor de ERK
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
IL270224B1 (en) 2017-05-02 2024-04-01 Novartis Ag Combination therapy employing trametinib and a defined raf inhibitor
CA3086765A1 (en) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. 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
AU2020276695B2 (en) 2019-05-13 2025-12-18 Novartis Ag New crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as RAF inhibitors for the treatment of cancer
US20230303551A1 (en) * 2020-08-13 2023-09-28 Albert Einstein College Of Medicine N-cyclyl-sulfonamides useful for inhibiting raf
EP4499634A1 (en) 2022-03-28 2025-02-05 Nikang Therapeutics, Inc. Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors
CN119790053A (zh) 2022-06-08 2025-04-08 霖康疗法公司 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰胺衍生物
WO2025072462A1 (en) 2023-09-27 2025-04-03 Nikang Therapeutics, Inc. Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors

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Also Published As

Publication number Publication date
US8563553B2 (en) 2013-10-22
JP2013503139A (ja) 2013-01-31
EP2470528A1 (en) 2012-07-04
JP5726190B2 (ja) 2015-05-27
EA020479B1 (ru) 2014-11-28
US20120225899A1 (en) 2012-09-06
AU2010288455A1 (en) 2012-02-23
KR20120092577A (ko) 2012-08-21
US8859548B2 (en) 2014-10-14
CN102596937B (zh) 2014-02-12
AR077977A1 (es) 2011-10-05
CN102596937A (zh) 2012-07-18
BR112012004448A2 (pt) 2017-05-30
TW201111365A (en) 2011-04-01
US20140011825A1 (en) 2014-01-09
CA2771673A1 (en) 2011-03-03
PT2470528E (pt) 2014-12-29
PL2470528T3 (pl) 2015-03-31
CA2771673C (en) 2016-07-12
WO2011023773A1 (en) 2011-03-03
US8242260B2 (en) 2012-08-14
JO3007B1 (ar) 2016-09-05
MX2012002542A (es) 2012-04-02
EA201200323A1 (ru) 2012-09-28
EP2470528B1 (en) 2014-10-01
ES2527176T3 (es) 2015-01-21
AU2010288455B2 (en) 2013-01-31
KR101714107B1 (ko) 2017-03-08
UY32859A (es) 2011-03-31
US20110052578A1 (en) 2011-03-03
IN2012DN00869A (enExample) 2015-07-10

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