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

Info

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
Application number
TW099128938A
Other languages
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
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of TW201111365A publication Critical patent/TW201111365A/zh
Application granted granted Critical
Publication of TWI487701B publication Critical patent/TWI487701B/zh

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)
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

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)

Country Link
US (3) US8242260B2 (cg-RX-API-DMAC7.html)
EP (1) EP2470528B1 (cg-RX-API-DMAC7.html)
JP (1) JP5726190B2 (cg-RX-API-DMAC7.html)
KR (1) KR101714107B1 (cg-RX-API-DMAC7.html)
CN (1) CN102596937B (cg-RX-API-DMAC7.html)
AR (1) AR077977A1 (cg-RX-API-DMAC7.html)
AU (1) AU2010288455B2 (cg-RX-API-DMAC7.html)
BR (1) BR112012004448A2 (cg-RX-API-DMAC7.html)
CA (1) CA2771673C (cg-RX-API-DMAC7.html)
EA (1) EA020479B1 (cg-RX-API-DMAC7.html)
ES (1) ES2527176T3 (cg-RX-API-DMAC7.html)
IN (1) IN2012DN00869A (cg-RX-API-DMAC7.html)
JO (1) JO3007B1 (cg-RX-API-DMAC7.html)
MX (1) MX2012002542A (cg-RX-API-DMAC7.html)
PL (1) PL2470528T3 (cg-RX-API-DMAC7.html)
PT (1) PT2470528E (cg-RX-API-DMAC7.html)
TW (1) TWI487701B (cg-RX-API-DMAC7.html)
UY (1) UY32859A (cg-RX-API-DMAC7.html)
WO (1) WO2011023773A1 (cg-RX-API-DMAC7.html)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
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
MX340392B (es) 2010-02-25 2016-07-06 Dana Farber Cancer Inst Inc Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf.
US9498471B2 (en) 2011-10-20 2016-11-22 The Regents Of The University Of California Use of CDK9 inhibitors to reduce cartilage degradation
CA2855243C (en) 2011-11-11 2020-04-14 Novartis Ag Method of treating a proliferative disease
PE20141994A1 (es) 2011-11-23 2014-12-24 Novartis Ag Formulaciones farmaceuticas
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
EP3013815B1 (en) 2013-06-25 2017-05-03 Bristol-Myers Squibb Company Carbazole carboxamide compounds useful as kinase inhibitors
UY35625A (es) 2013-06-25 2014-12-31 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos como inhibidores de quinasa
TR201809185T4 (tr) * 2013-08-28 2018-07-23 Medivation Tech Llc Heterosiklik bileşikler ve kullanım yöntemleri.
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
JP6930913B2 (ja) 2014-10-14 2021-09-01 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアＴｈｅ Ｒｅｇｅｎｔｓ Ｏｆ Ｔｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｃａｌｉｆｏｒｎｉａ 炎症を阻害するためのｃｄｋ９及びｂｒｄ４阻害剤の使用法
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
EP3515446B1 (en) 2016-09-19 2023-12-20 Novartis AG Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
US11471538B2 (en) 2017-02-10 2022-10-18 INSERM (Institut National de la Santéet de la Recherche Medicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the MAPK pathway
DK3618875T3 (da) 2017-05-02 2023-07-10 Novartis Ag Kombinationsterapi omfattende en raf-inhibitor og trametinib
EP3732285A1 (en) 2017-12-28 2020-11-04 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
KR102881316B1 (ko) 2019-05-13 2025-11-05 노파르티스 아게 암 치료를 위한 raf 억제제로서의 n-(3-(2-(2-하이드록시에톡시)-6-모르폴리노피리딘-4-일)-4-메틸페닐)-2 (트리플루오로메틸)이소니코틴아미드의 새로운 결정질 형태
WO2022036176A1 (en) * 2020-08-13 2022-02-17 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
EP4536363A1 (en) 2022-06-08 2025-04-16 Nikang Therapeutics, Inc. Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors
WO2025072462A1 (en) 2023-09-27 2025-04-03 Nikang Therapeutics, Inc. Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors

Family Cites Families (25)

* Cited by examiner, † Cited by third party
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
US6391636B1 (en) 1994-05-31 2002-05-21 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
US6358932B1 (en) 1994-05-31 2002-03-19 Isis Pharmaceticals, Inc. Antisense oligonucleotide inhibition 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
IL127210A0 (en) 1996-05-23 1999-09-22 Applied Research Systems Compounds inhibiting the binding of raf-1 or 13-3-3 proteins to the beta-chain of il-2 pharmaceutical compositions containing them and their use
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
US6756410B2 (en) 2000-08-30 2004-06-29 Kamal D. Mehta Induction of LDL receptor expression by extracellular-signal regulated kinase, ERK-1/2
TWI350285B (en) 2002-03-13 2011-10-11 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
JP2008531538A (ja) 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド ２，４−ジアミノ−ピリドピリミジン誘導体とｍＴＯＲ阻害剤としてのその使用
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
HRP20120963T1 (hr) 2005-11-22 2012-12-31 Kudos Pharmaceuticals Ltd PIRIDO-, PIRAZO- I PIRIMIDOPIRIMIDINSKI DERIVATI KAO mTOR INHIBITORI
KR20080083188A (ko) 2006-01-11 2008-09-16 아스트라제네카 아베 모르폴리노 피리미딘 유도체 및 요법에서의 그 유도체의용도
BRPI0715888B1 (pt) 2006-08-23 2021-11-03 Kudos Pharmaceuticals Limited Composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, uso de um composto
TW200922582A (en) 2007-08-20 2009-06-01 Organon Nv N-benzyl, N'-arylcarbonylpiperazine derivatives
KR20130040258A (ko) * 2008-03-21 2013-04-23 노파르티스 아게 신규한 헤테로시클릭 화합물 및 그의 용도
UA103319C2 (en) * 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
HRP20120577T1 (hr) * 2008-07-24 2012-08-31 Nerviano Medical Sciences S.R.L. 3,4-diarilpirazoli kao inhibitori proteinskih kinaza

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Bioorganic & Medicinal Chemistry Letters, 2008,Vol:18, Nr:9, Page(s):2825 – 2829 *

Also Published As

Publication number Publication date
JP5726190B2 (ja) 2015-05-27
KR20120092577A (ko) 2012-08-21
JP2013503139A (ja) 2013-01-31
CN102596937B (zh) 2014-02-12
US20140011825A1 (en) 2014-01-09
US8563553B2 (en) 2013-10-22
US20120225899A1 (en) 2012-09-06
MX2012002542A (es) 2012-04-02
AR077977A1 (es) 2011-10-05
TW201111365A (en) 2011-04-01
CA2771673A1 (en) 2011-03-03
UY32859A (es) 2011-03-31
PL2470528T3 (pl) 2015-03-31
US8242260B2 (en) 2012-08-14
AU2010288455B2 (en) 2013-01-31
AU2010288455A1 (en) 2012-02-23
US8859548B2 (en) 2014-10-14
KR101714107B1 (ko) 2017-03-08
CN102596937A (zh) 2012-07-18
JO3007B1 (ar) 2016-09-05
PT2470528E (pt) 2014-12-29
WO2011023773A1 (en) 2011-03-03
EP2470528A1 (en) 2012-07-04
IN2012DN00869A (cg-RX-API-DMAC7.html) 2015-07-10
EA201200323A1 (ru) 2012-09-28
EP2470528B1 (en) 2014-10-01
ES2527176T3 (es) 2015-01-21
US20110052578A1 (en) 2011-03-03
CA2771673C (en) 2016-07-12
EA020479B1 (ru) 2014-11-28
BR112012004448A2 (pt) 2017-05-30

Similar Documents

Publication Publication Date Title
TWI487701B (zh) 作為蛋白質激酶抑制劑之化合物及組合物
JP6181862B2 (ja) ピラゾロピロリジン誘導体および疾患の処置におけるその使用
JP6667573B2 (ja) 新規なアミノピリミジン誘導体
US10590079B2 (en) Cyano-substituted indoles as LSD1 inhibitors
AU2015320863B2 (en) Naphthyridine derivatives as alpha v beta 6 integrin antagonists for the treatment of e.g. fibrotic diseases
US20130096149A1 (en) Heteroaryl compounds and compositions as protein kinase inhibitors
MXPA05005477A (es) Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-cinasa y su uso en el tratamiento del cancer.
US9550796B2 (en) Pyrrolopyrrolone derivatives and their use as BET inhibitors
CN103270026A (zh) 作为vps34抑制剂的联-杂芳基化合物
CN102482286B (zh) 新型1,2,3,4-四氢嘧啶并{1,2-a}嘧啶-6-酮衍生物、其制备以及其医药用途
WO2018019222A1 (zh) 作为jak抑制剂杂环化合物，该化合物的盐类及其治疗用途
CN108290898A (zh) 作为磷脂酰肌醇3-激酶抑制剂的喹啉类似物
JP7545570B2 (ja) ヘテロアリール置換スピロピペリジニル誘導体及びその薬学的使用
CN103459396B (zh) 作为c-Met酪氨酸激酶抑制剂的[1,2,4]三唑并[4,3-b]哒嗪化合物

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees