EA201170617A1 - Пиразолиламинопиридины в качестве ингибиторов fak - Google Patents

Пиразолиламинопиридины в качестве ингибиторов fak

Info

Publication number
EA201170617A1
EA201170617A1 EA201170617A EA201170617A EA201170617A1 EA 201170617 A1 EA201170617 A1 EA 201170617A1 EA 201170617 A EA201170617 A EA 201170617A EA 201170617 A EA201170617 A EA 201170617A EA 201170617 A1 EA201170617 A1 EA 201170617A1
Authority
EA
Eurasian Patent Office
Prior art keywords
pyrazolylaminopiridine
fak inhibitors
present
fak
inhibitors
Prior art date
Application number
EA201170617A
Other languages
English (en)
Other versions
EA021927B1 (ru
Inventor
Джерри Лерой Адамс
Томас Х. Фейт
Нейл В. Джонсон
Хун Линь
Иржи Каспарек
Марк Меллинджер
Синь Пэн
Жэнь Се
Original Assignee
ГЛЭКСОСМИТКЛАЙН ЭлЭлСи
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42132177&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201170617(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by ГЛЭКСОСМИТКЛАЙН ЭлЭлСи filed Critical ГЛЭКСОСМИТКЛАЙН ЭлЭлСи
Publication of EA201170617A1 publication Critical patent/EA201170617A1/ru
Publication of EA021927B1 publication Critical patent/EA021927B1/ru

Links

Classifications

    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57407—Specifically defined cancers
    • G01N33/57423—Specifically defined cancers of lung

Abstract

Настоящее изобретение относится к соединению формулы (I)или к его фармацевтически приемлемой соли, где R, R, R, R, R, R, Q, Z и р являются такими, как описано в настоящем документе. Соединения по настоящему изобретению пригодны для лечения злокачественных опухолей.
EA201170617A 2008-10-27 2009-10-27 2-[(5-хлор-2-{[3-метил-1-(1-метилэтил)-1н-пиразол-5-ил]амино}-4-пиридинил)амино]-n-(метилокси)бензамид в качестве ингибиторов fak и содержащая его фармацевтическая композиция EA021927B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US10856808P 2008-10-27 2008-10-27
US17851709P 2009-05-15 2009-05-15
US24243209P 2009-09-15 2009-09-15
PCT/US2009/062163 WO2010062578A1 (en) 2008-10-27 2009-10-27 Pyrazolylaminopyridines as inhibitors of fak

Publications (2)

Publication Number Publication Date
EA201170617A1 true EA201170617A1 (ru) 2011-12-30
EA021927B1 EA021927B1 (ru) 2015-09-30

Family

ID=42132177

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170617A EA021927B1 (ru) 2008-10-27 2009-10-27 2-[(5-хлор-2-{[3-метил-1-(1-метилэтил)-1н-пиразол-5-ил]амино}-4-пиридинил)амино]-n-(метилокси)бензамид в качестве ингибиторов fak и содержащая его фармацевтическая композиция

Country Status (36)

Country Link
US (6) US20110207743A1 (ru)
EP (1) EP2421537B1 (ru)
JP (1) JP5642689B2 (ru)
KR (1) KR101512217B1 (ru)
CN (1) CN102264371B (ru)
AR (1) AR073993A1 (ru)
AU (1) AU2009320144B2 (ru)
BR (1) BRPI0920053B8 (ru)
CA (1) CA2741760C (ru)
CL (1) CL2011000933A1 (ru)
CO (1) CO6361929A2 (ru)
CR (1) CR20110264A (ru)
CY (1) CY1116399T1 (ru)
DK (1) DK2421537T3 (ru)
DO (1) DOP2011000113A (ru)
EA (1) EA021927B1 (ru)
ES (1) ES2539835T3 (ru)
HK (1) HK1161680A1 (ru)
HR (1) HRP20150531T1 (ru)
IL (1) IL212444A (ru)
JO (1) JO3067B1 (ru)
MA (1) MA32727B1 (ru)
MX (1) MX2011004369A (ru)
MY (1) MY161890A (ru)
NZ (1) NZ592477A (ru)
PE (1) PE20110941A1 (ru)
PL (1) PL2421537T3 (ru)
PT (1) PT2421537E (ru)
RS (1) RS54045B1 (ru)
SG (1) SG195608A1 (ru)
SI (1) SI2421537T1 (ru)
SM (1) SMT201500157B (ru)
TW (1) TWI454467B (ru)
UY (1) UY32200A (ru)
WO (1) WO2010062578A1 (ru)
ZA (1) ZA201102892B (ru)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8338441B2 (en) 2009-05-15 2012-12-25 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
US20120244141A1 (en) 2010-09-28 2012-09-27 Boehringer Ingelheim International Gmbh Stratification of cancer patients for susceptibility to therapy with PTK2 inhibitors
MX2013008654A (es) * 2011-01-26 2013-09-02 Glaxosmithkline Intellectual Property Ltd Combinaciones.
EP2675794B1 (en) 2011-02-17 2019-02-13 Cancer Therapeutics Crc Pty Limited Selective fak inhibitors
CA2827171C (en) 2011-02-17 2019-04-09 Cancer Therapeutics Crc Pty Limited Fak inhibitors
KR20140043929A (ko) * 2011-06-28 2014-04-11 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 투여 및 치료 방법
US10106834B2 (en) 2013-10-09 2018-10-23 The General Hospital Corporation Methods of diagnosing and treating B cell acute lymphoblastic leukemia
EP3313404A4 (en) 2015-06-29 2019-08-07 Verastem, Inc. THERAPEUTIC COMPOSITIONS, ASSOCIATIONS AND METHODS OF USE
CN108948019B (zh) * 2017-05-18 2022-07-08 广东东阳光药业有限公司 黏着斑激酶抑制剂及其用途
WO2019117813A1 (en) * 2017-12-15 2019-06-20 National University Of Singapore Focal adhesion kinase targeted therapeutics for the treatment of glaucoma and fibrosis
US20210030703A1 (en) 2018-03-12 2021-02-04 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of caloric restriction mimetics for potentiating chemo-immunotherapy for the treatment of cancers
CN108912095B (zh) * 2018-08-09 2019-08-20 广州安岩仁医药科技有限公司 苯并咪唑类化合物及其制备方法和应用
CA3109617A1 (en) * 2018-09-27 2020-04-02 Dana-Farber Cancer Institute, Inc. Degradation of fak or fak and alk by conjugation of fak and alk inhibitors with e3 ligase ligands and methods of use
CN113387947B (zh) * 2021-07-12 2022-07-01 中国科学院成都生物研究所 调节雌激素受体合成活性的吡唑并吡啶衍生物

Family Cites Families (10)

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US166139A (en) * 1875-07-27 Improvement in dental pluggers
ATE310018T1 (de) * 1998-09-08 2005-12-15 Agouron Pharma Modifikationen des vegf-rezeptor-2 proteins und verfahren zu seiner verwendung
US7102009B2 (en) * 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
MXPA06001759A (es) * 2003-08-15 2006-05-12 Novartis Ag 2,4-pirimidinadiaminas utiles en el tratamiento de enfermedades neoplasticas, desordenes del sistema inmune e inflamatorios.
GB0419160D0 (en) * 2004-08-27 2004-09-29 Novartis Ag Organic compounds
GB0419161D0 (en) * 2004-08-27 2004-09-29 Novartis Ag Organic compounds
EP1746096A1 (en) * 2005-07-15 2007-01-24 4Sc Ag 2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer
CA2681015C (en) * 2007-03-16 2016-06-21 The Scripps Research Institute Inhibitors of focal adhesion kinase
EP2249650A4 (en) * 2008-02-19 2012-01-11 Glaxosmithkline Llc ANILINOPYRIDINE AS A FAK HEMMER
EA020807B1 (ru) * 2008-06-17 2015-01-30 Астразенека Аб Соединения пиридина

Also Published As

Publication number Publication date
JP2012506876A (ja) 2012-03-22
IL212444A (en) 2015-11-30
CA2741760C (en) 2016-02-23
KR20110080172A (ko) 2011-07-12
IL212444A0 (en) 2011-06-30
MX2011004369A (es) 2011-05-25
HRP20150531T1 (hr) 2015-06-19
JP5642689B2 (ja) 2014-12-17
AU2009320144B2 (en) 2013-11-21
EA021927B1 (ru) 2015-09-30
US9012479B2 (en) 2015-04-21
ES2539835T3 (es) 2015-07-06
US20110269774A1 (en) 2011-11-03
CN102264371A (zh) 2011-11-30
BRPI0920053B8 (pt) 2021-05-25
US20150265589A1 (en) 2015-09-24
JO3067B1 (ar) 2017-03-15
CL2011000933A1 (es) 2011-10-21
PL2421537T3 (pl) 2015-08-31
SMT201500157B (it) 2015-09-07
AR073993A1 (es) 2010-12-15
CA2741760A1 (en) 2010-06-03
DK2421537T3 (da) 2015-06-22
CY1116399T1 (el) 2017-02-08
HK1161680A1 (en) 2012-08-03
BRPI0920053B1 (pt) 2019-11-26
WO2010062578A1 (en) 2010-06-03
MA32727B1 (fr) 2011-10-02
BRPI0920053A2 (pt) 2015-12-15
US20100113475A1 (en) 2010-05-06
AU2009320144A1 (en) 2010-06-03
EP2421537A1 (en) 2012-02-29
PE20110941A1 (es) 2012-02-08
PT2421537E (pt) 2015-07-03
US20160095841A1 (en) 2016-04-07
RS54045B1 (en) 2015-10-30
ZA201102892B (en) 2012-02-29
TW201028394A (en) 2010-08-01
EP2421537B1 (en) 2015-04-08
NZ592477A (en) 2013-01-25
US20110207743A1 (en) 2011-08-25
MY161890A (en) 2017-05-15
TWI454467B (zh) 2014-10-01
EP2421537A4 (en) 2012-06-13
SI2421537T1 (sl) 2015-06-30
CN102264371B (zh) 2013-10-02
KR101512217B1 (ko) 2015-04-15
SG195608A1 (en) 2013-12-30
US20140107131A1 (en) 2014-04-17
DOP2011000113A (es) 2011-07-15
CO6361929A2 (es) 2012-01-20
UY32200A (es) 2010-05-31
US9446034B2 (en) 2016-09-20
CR20110264A (es) 2011-10-04

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU