EA200970595A1 - Производные замещенных индазолов, активные в качестве ингибиторов киназ - Google Patents

Производные замещенных индазолов, активные в качестве ингибиторов киназ

Info

Publication number
EA200970595A1
EA200970595A1 EA200970595A EA200970595A EA200970595A1 EA 200970595 A1 EA200970595 A1 EA 200970595A1 EA 200970595 A EA200970595 A EA 200970595A EA 200970595 A EA200970595 A EA 200970595A EA 200970595 A1 EA200970595 A1 EA 200970595A1
Authority
EA
Eurasian Patent Office
Prior art keywords
derivatives
substituted
indazols
active
kinaz
Prior art date
Application number
EA200970595A
Other languages
English (en)
Other versions
EA017852B1 (ru
Inventor
Тициано Бандьера
Борджиа Андреа Ломбарди
Марчелла Нези
Этторе Перроне
Роберто Босси
Паоло Получчи
Original Assignee
НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
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 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. filed Critical НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
Publication of EA200970595A1 publication Critical patent/EA200970595A1/ru
Publication of EA017852B1 publication Critical patent/EA017852B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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

Abstract

Описаны производные замещенных индазолов формулы (I) и их фармацевтически приемлемые соли, указываемые в описании, способ их получения и содержащие их фармацевтические композиции; соединения изобретения могут быть применимыми в терапии при лечении заболеваний, связанных с нарушенной активностью протеинкиназ, подобных раку.
EA200970595A 2006-12-20 2007-12-14 Производные замещенных индазолов, активные в качестве ингибиторов киназ EA017852B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06126701 2006-12-20
PCT/EP2007/063998 WO2008074749A1 (en) 2006-12-20 2007-12-14 Indazole derivatives as kinase inhibitors for the treatment of cancer

Publications (2)

Publication Number Publication Date
EA200970595A1 true EA200970595A1 (ru) 2010-02-26
EA017852B1 EA017852B1 (ru) 2013-03-29

Family

ID=39245139

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200970595A EA017852B1 (ru) 2006-12-20 2007-12-14 Производные замещенных индазолов, активные в качестве ингибиторов киназ

Country Status (15)

Country Link
US (1) US8114865B2 (ru)
EP (1) EP2120932B1 (ru)
JP (1) JP5302896B2 (ru)
CN (1) CN101594862B (ru)
AU (1) AU2007336335B8 (ru)
BR (1) BRPI0720589A2 (ru)
CA (1) CA2673095C (ru)
DK (1) DK2120932T3 (ru)
EA (1) EA017852B1 (ru)
ES (1) ES2509820T3 (ru)
MX (1) MX2009006401A (ru)
PL (1) PL2120932T3 (ru)
PT (1) PT2120932E (ru)
SI (1) SI2120932T1 (ru)
WO (1) WO2008074749A1 (ru)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7638541B2 (en) 2006-12-28 2009-12-29 Metabolex Inc. 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
US8183381B2 (en) * 2007-07-19 2012-05-22 Metabolex Inc. N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders
NZ583450A (en) 2007-07-20 2012-05-25 Nerviano Medical Sciences Srl Substituted indazole derivatives active as kinase inhibitors
ES2630026T3 (es) * 2008-12-18 2017-08-17 Nerviano Medical Sciences S.R.L. Derivados indazólicos sustituidos activos como inhibidores de cinasa
JO2860B1 (en) 2009-05-07 2015-03-15 ايلي ليلي اند كومباني Phenylendazolyl compounds
CN102666553B (zh) 2009-10-01 2015-05-06 赛马拜制药公司 取代的四唑-1-基-苯氧基甲基-噻唑-2-基-哌啶基-嘧啶盐
EP2519517B1 (en) 2009-12-29 2015-03-25 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
EA201290919A1 (ru) * 2010-03-16 2013-03-29 Дана-Фарбер Кэнсер Инститьют, Инк. Индазольные соединения и их применение
WO2012075318A2 (en) * 2010-12-01 2012-06-07 Cell Signaling Technology, Inc. Fn1 and alk gene translocations in cancer and alk kinase expression in ovarian cancer
FR2970967B1 (fr) 2011-01-27 2013-02-15 Pf Medicament Derives de type azaindazole ou diazaindazole comme medicament
ES2611779T3 (es) * 2011-05-12 2017-05-10 Nerviano Medical Sciences S.R.L. Derivados de indazol sustituidos activos como inhibidores de quinasas
JP6165733B2 (ja) 2011-09-16 2017-07-19 ノバルティス アーゲー Ｎ−置換ヘテロシクリルカルボキサミド類
JP6106685B2 (ja) 2011-11-17 2017-04-05 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド Ｃ−ｊｕｎ−ｎ−末端キナーゼ（ｊｎｋ）の阻害剤
ES2755719T3 (es) * 2012-04-05 2020-04-23 Nerviano Medical Sciences Srl Nuevos agentes alquilantes
KR102151963B1 (ko) * 2012-05-23 2020-09-07 네르비아노 메디칼 사이언시스 에스.알.엘. Ｎ-[5-(3,5-디플루오로-벤질)-1ｈ-인다졸-3-일]-4-(4-메틸-피페라진-1-일)-2-(테트라하이드로-피란-4-일아미노)-벤즈아미드의 제조 방법
KR101936851B1 (ko) * 2012-07-16 2019-01-11 한국과학기술연구원 단백질 키나아제 저해제인 신규 피라졸로피리딘 유도체 또는 인다졸 유도체
EP2689779A1 (en) 2012-07-27 2014-01-29 Pierre Fabre Medicament Derivatives of azaindazole or diazaindazole type for treating a cancer overexpressing trk
EP2689778A1 (en) 2012-07-27 2014-01-29 Pierre Fabre Medicament Derivatives of azaindoles or diazaindoles for treating pain
JP6371284B2 (ja) 2012-08-22 2018-08-08 コーネル ユニヴァーシティー ファスシンを阻害する方法
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2015110467A1 (en) * 2014-01-23 2015-07-30 Nerviano Medical Sciences S.R.L. Process for the preparation of substituted n-(5-benzenesulfonyl-1h-indazol-3-yl)-benzamides
TWI672141B (zh) * 2014-02-20 2019-09-21 美商醫科泰生技 投予ｒｏｓ１突變癌細胞之分子
ES2868882T3 (es) 2014-02-20 2021-10-22 Cornell Univ Cornell Center For Technology Enterprise & Commercialization Cctec Compuestos y métodos para inhibir fascina
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
CN107207471B (zh) 2014-12-02 2020-06-26 伊尼塔公司 用于治疗神经母细胞瘤的组合
EP3233840B1 (en) 2014-12-16 2018-11-21 Eudendron S.r.l. Heterocyclic derivatives modulating activity of certain protein kinases
EP3236959A4 (en) 2014-12-23 2018-04-25 Dana Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CN104530045A (zh) * 2015-01-14 2015-04-22 中国药科大学 吡唑并[4,3-c]四氢吡啶类c-Met激酶抑制剂及其制备方法和用途
WO2016123629A1 (en) * 2015-01-30 2016-08-04 Vanderbilt University Indazole and azaindazole substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. ASSOCIATION THERAPY USING TRANSCRIPTION INHIBITORS AND KINASE INHIBITORS
JP7028766B2 (ja) 2015-09-09 2022-03-02 ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼの阻害剤
JP7061068B2 (ja) 2015-12-18 2022-04-27 イグナイタ インコーポレイテッド 癌治療のための併用薬
JP2019527693A (ja) 2016-08-03 2019-10-03 サイマベイ・セラピューティクス・インコーポレイテッドＣｙｍａＢａｙ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． 炎症性胃腸疾患または胃腸状態を治療するためのオキシメチレンアリール化合物
AU2018302170B2 (en) 2017-07-19 2024-02-29 Ignyta, Inc. Pharmaceutical compositions comprising entrectinib
US10508105B2 (en) 2017-08-16 2019-12-17 Vanderbilt University Indazole compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
WO2019077506A1 (en) 2017-10-17 2019-04-25 Ignyta, Inc. PHARMACEUTICAL COMPOSITIONS AND SOLID GALENIC FORMS
CN110452176A (zh) * 2018-05-07 2019-11-15 四川大学 吲唑类衍生物及其制备方法和用途
EP3725777A1 (en) * 2019-04-17 2020-10-21 Rottapharm Biotech S.r.l. Benzo- and pyrido-pyrazoles as protein kinase inhibitors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ531765A (en) * 2001-09-26 2006-02-24 Pharmacia Italia S Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
FR2836915B1 (fr) * 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
TW200501960A (en) * 2002-10-02 2005-01-16 Bristol Myers Squibb Co Synergistic kits and compositions for treating cancer
CA2517517C (en) * 2003-03-03 2012-12-18 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
FR2871158A1 (fr) 2004-06-04 2005-12-09 Aventis Pharma Sa Indazoles substitues, compositions les contenant, procede de fabrication et utilisation
CA2599987A1 (en) * 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Fused heterocyclic compounds and their use as sirtuin modulators
CL2009001158A1 (es) * 2008-05-15 2009-10-23 Nerviano Medical Sciences Srl Compuestos derivados de los acidos carboxilicos, tales como 5,6-dihiro-4h-pirrolo[3,4-c]pirazol, furo[3,2-c]pirazol, tieno[2,3-c]pirazol, 4,5,6,7-tetrahidropirazol[4,3-c]piridina e indazol; composicion farmaceutica; y su uso en el tratamiento de trastornos proliferativos celulares asociados a la actividad de proteina quinasa alterada, tal como el cancer.

Also Published As

Publication number Publication date
AU2007336335A2 (en) 2009-08-06
JP2010530840A (ja) 2010-09-16
US8114865B2 (en) 2012-02-14
AU2007336335B2 (en) 2013-05-30
CA2673095C (en) 2016-03-15
CA2673095A1 (en) 2008-06-26
DK2120932T3 (da) 2014-10-13
JP5302896B2 (ja) 2013-10-02
US20100197665A1 (en) 2010-08-05
CN101594862B (zh) 2015-11-25
PL2120932T3 (pl) 2015-02-27
EA017852B1 (ru) 2013-03-29
SI2120932T1 (sl) 2014-09-30
WO2008074749A1 (en) 2008-06-26
WO2008074749A9 (en) 2009-05-07
ES2509820T3 (es) 2014-10-20
CN101594862A (zh) 2009-12-02
EP2120932A1 (en) 2009-11-25
MX2009006401A (es) 2009-06-23
EP2120932B1 (en) 2014-07-09
AU2007336335A8 (en) 2014-07-24
BRPI0720589A2 (pt) 2014-02-25
AU2007336335A1 (en) 2008-06-26
PT2120932E (pt) 2014-10-10
AU2007336335B8 (en) 2014-07-24

Similar Documents

Publication Publication Date Title
EA200970595A1 (ru) Производные замещенных индазолов, активные в качестве ингибиторов киназ
EA201070167A1 (ru) Замещенные производные индазола, активные как ингибиторы киназы
EA200501849A1 (ru) Производные пиразолохиназолина: способ получения и применение в качестве ингибиторов киназ
ATE514699T1 (de) Substituierte pyrrolopyrazolderivate als kinaseinhibitoren
DK2324008T3 (da) Diarylpyrazol som protein kinase inhibitorer
HK1136292A1 (en) Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
DE602004017194D1 (de) Pyridylpyrrol-derivate als wirksame kinase-hemmer
MXPA06000302A (es) Derivados de pirazolil-indol activos como inhibidores de cinasa, procedimientos para su preparacion y composiciones farmaceuticas que los comprenden.
WO2009071480A3 (en) Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors
EA201100971A1 (ru) Производные пиримидининдола для лечения злокачественного новообразования
EA201000091A1 (ru) ПРОИЗВОДНЫЕ МОРФОЛИНОПИРИМИДИНА, ИСПОЛЬЗУЕМЫЕ ПРИ ЗАБОЛЕВАНИЯХ, СВЯЗАННЫХ С mTOR КИНАЗОЙ И/ИЛИ PI3K
EA201000092A1 (ru) Тризамещенные пиримидиновые производные для лечения пролиферативных заболеваний
EA201000090A1 (ru) Тризамещенные производные пиримидина для лечения пролиферативных заболеваний
MX2007005546A (es) Tiazoles de 5-heteroarilo y su uso como inhibidores p13k.
MX2008012422A (es) Derivados de furano y tiofeno, pirrol substituido con pirimidinil y piridil como inhibidores de cinasa.
PA8622801A1 (es) Derivados 1h-tieno(2,3-c)pirazol utiles como inhibidores de quinasa
BRPI0413438A (pt) derivados de pirimidilpirrol ativos como inibidores de cinase
UA102219C2 (ru) Замещенные пиразолохиназолиновые производные, способ их получения и их применения как ингибиторов киназы
ATE496899T1 (de) Tetrahydro- und dihydrochinazolinone
CU20060152A7 (es) Derivados 1h-tieno[2,3-c]pirazol útiles como inhibidores de quinasa
CU23596A3 (es) Derivados de pirazol-quinazolina y proceso para su preparación
EA201990219A3 (ru) Ингибиторы mek и способы их применения

Legal Events

Date Code Title Description
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): AM AZ KG TJ TM