[go: up one dir, main page]

EA201391682A1 - Замещенные производные индазола, активные в качестве ингибиторов киназы - Google Patents

Замещенные производные индазола, активные в качестве ингибиторов киназы

Info

Publication number
EA201391682A1
EA201391682A1 EA201391682A EA201391682A EA201391682A1 EA 201391682 A1 EA201391682 A1 EA 201391682A1 EA 201391682 A EA201391682 A EA 201391682A EA 201391682 A EA201391682 A EA 201391682A EA 201391682 A1 EA201391682 A1 EA 201391682A1
Authority
EA
Eurasian Patent Office
Prior art keywords
indazols
active
compounds
kinase inhibitors
substituted derivatives
Prior art date
Application number
EA201391682A
Other languages
English (en)
Other versions
EA023579B1 (ru
Inventor
Борджиа Андреа Ломбарди
Марина Чиомеи
Даниеле Донати
Марчелла Нези
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46025764&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201391682(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. filed Critical НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
Publication of EA201391682A1 publication Critical patent/EA201391682A1/ru
Publication of EA023579B1 publication Critical patent/EA023579B1/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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • 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
    • 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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
    • C12Y207/10—Protein-tyrosine kinases (2.7.10)
    • C12Y207/10001—Receptor protein-tyrosine kinase (2.7.10.1)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Изобретение относится к замещенным соединениям индазола, которые модулируют активность протеинкиназ, и поэтому их можно использовать при лечении заболеваний, вызванных разрегулированием активности протеинкиназ, сходной с раковой. В настоящем изобретении также предложены способы получения указанных соединений, включающих указанные соединения фармацевтических композиций, и способы лечения заболеваний с использованием таких указанных соединений или содержащих их фармацевтических композиций.
EA201391682A 2011-05-12 2012-05-07 Замещенные производные индазола, активные в качестве ингибиторов киназы EA023579B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11165882 2011-05-12
PCT/EP2012/058389 WO2012152763A1 (en) 2011-05-12 2012-05-07 Substituted indazole derivatives active as kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201391682A1 true EA201391682A1 (ru) 2014-04-30
EA023579B1 EA023579B1 (ru) 2016-06-30

Family

ID=46025764

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201391682A EA023579B1 (ru) 2011-05-12 2012-05-07 Замещенные производные индазола, активные в качестве ингибиторов киназы

Country Status (23)

Country Link
US (4) US9408850B2 (ru)
EP (1) EP2707359B1 (ru)
JP (1) JP6396210B2 (ru)
KR (1) KR101953272B1 (ru)
CN (1) CN103534239B (ru)
AR (1) AR086357A1 (ru)
AU (1) AU2012252468B2 (ru)
BR (1) BR112013028733B1 (ru)
CA (1) CA2835478C (ru)
CL (1) CL2013003227A1 (ru)
DK (1) DK2707359T3 (ru)
EA (1) EA023579B1 (ru)
ES (1) ES2611779T3 (ru)
HU (1) HUE031166T2 (ru)
IL (1) IL229252A (ru)
MX (1) MX342509B (ru)
PL (1) PL2707359T3 (ru)
PT (1) PT2707359T (ru)
SG (1) SG194911A1 (ru)
SI (1) SI2707359T1 (ru)
TW (1) TWI573790B (ru)
WO (1) WO2012152763A1 (ru)
ZA (1) ZA201309345B (ru)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
PT2707359T (pt) 2011-05-12 2017-01-09 Nerviano Medical Sciences Srl Derivados de indazol substituídos ativos como inibidores de quinase
CN103739550B (zh) * 2014-01-02 2016-06-01 中国药科大学 2,3-二甲基-6-脲-2h-吲唑类化合物及其制备方法与应用
EA035049B1 (ru) 2015-07-16 2020-04-22 Аррэй Байофарма Инк. СОЕДИНЕНИЯ ЗАМЕЩЕННОГО ПИРАЗОЛО[1,5-a]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ RET КИНАЗЫ
DE102015012050A1 (de) * 2015-09-15 2017-03-16 Merck Patent Gmbh Verbindungen als ASIC-Inhibitoren und deren Verwendungen
KR20180102544A (ko) 2015-10-26 2018-09-17 더 리전츠 오브 더 유니버시티 오브 콜로라도, 어 바디 코퍼레이트 Trk 억제제-내성 암에서의 점 돌연변이 및 이의 관련 방법
NZ747135A (en) 2016-04-04 2025-05-02 Loxo Oncology Inc Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
PL3439663T3 (pl) 2016-04-04 2024-11-18 Loxo Oncology, Inc. Sposoby leczenia nowotworów wieku dziecięcego
RS61463B1 (sr) 2016-05-18 2021-03-31 Loxo Oncology Inc Priprema (s)-n-(5-((r)-2-(2,5-difluorofenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3-il) -3-hidroksipirolidin-1-karboksamida
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
TWI876442B (zh) 2017-10-10 2025-03-11 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
CN111971286B (zh) 2018-01-18 2023-04-14 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物
WO2019143991A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
JP7286755B2 (ja) 2018-07-31 2023-06-05 ロクソ オンコロジー， インコーポレイテッド （ｓ）－５－アミノ－３－（４－（（５－フルオロ－２－メトキシベンズアミド）メチル）フェニル）－１－（１，１，１－トリフルオロプロパン－２－イル）－１ｈ－ピラゾール－４－カルボキサミドの噴霧乾燥分散体および製剤
JP2022500383A (ja) 2018-09-10 2022-01-04 アレイ バイオファーマ インコーポレイテッド Ｒｅｔキナーゼ阻害剤としての縮合複素環式化合物
US12180207B2 (en) 2018-12-19 2024-12-31 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3725777A1 (en) * 2019-04-17 2020-10-21 Rottapharm Biotech S.r.l. Benzo- and pyrido-pyrazoles as protein kinase inhibitors
CN114391009A (zh) * 2019-08-08 2022-04-22 Bci制药公司 作为蛋白激酶抑制剂的喹啉衍生物
CN112794820B (zh) * 2019-11-14 2022-06-07 四川大学 吲唑类衍生物及其制备方法和用途
EP4069369A4 (en) 2019-12-06 2024-02-14 Schrödinger, Inc. CYCLIC COMPOUNDS AND METHODS OF USE THEREOF
CN111116734A (zh) * 2019-12-23 2020-05-08 维塔恩(广州)医药有限公司 肿瘤相关基因c-kit突变相关抗原短肽及其应用
JP2023509886A (ja) 2019-12-27 2023-03-10 シュレーディンガー， インコーポレイテッド 環式化合物およびその使用方法
WO2022033472A1 (zh) * 2020-08-11 2022-02-17 河南迈英诺医药科技有限公司 Fgfr抑制剂化合物及其用途
EP4211140A1 (en) 2020-09-10 2023-07-19 Schrödinger, Inc. Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer
WO2022164789A1 (en) 2021-01-26 2022-08-04 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disoders
TW202300150A (zh) 2021-03-18 2023-01-01 美商薛定諤公司 環狀化合物及其使用方法
WO2024088829A2 (en) 2022-10-25 2024-05-02 Nerviano Medical Sciences S.R.L. Salts and polymorphs of 4-(4-methyl-piperazin-1-yl)-n-{6-[2-(4-trifluoromethyl-benzyloxy)-ethoxy]-1h-indazol-3-yl}-benzamide
WO2025012029A1 (en) 2023-07-11 2025-01-16 Nerviano Medical Sciences S.R.L. Therapeutic combination comprising 4-(4-methyl-piperazin-1-yl)-n-{6-[2-(4-trifluoromethyl-benzyloxy)-ethoxy]-1h-indazol-3-yl}-benzamide and an antineoplastic agent
WO2025059027A1 (en) 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL368347A1 (en) * 2001-09-26 2005-03-21 Pharmacia Italia S.P.A. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
JP2007518823A (ja) * 2004-01-23 2007-07-12 アムゲン インコーポレイテッド キノリン、キナゾリン、ピリジン、及びピリミジン化合物と炎症、血管新生、及び癌に対する治療におけるそれら化合物の用途
KR20060114022A (ko) 2004-02-27 2006-11-03 에프. 호프만-라 로슈 아게 인다졸 유도체 및 그들을 함유하는 약학 조성물
DE102006030479A1 (de) 2006-07-01 2008-03-20 Merck Patent Gmbh Indazolderivate
PL2120932T3 (pl) * 2006-12-20 2015-02-27 Nerviano Medical Sciences Srl Indazolowe pochodne jako inhibitory kinazy do leczenia raka
EP2176231B1 (en) * 2007-07-20 2016-10-19 Nerviano Medical Sciences S.r.l. Substituted indazole derivatives active as kinase inhibitors
AR071780A1 (es) * 2008-05-15 2010-07-14 Nerviano Medical Sciences Srl Derivados de carbamoilo de carbonilamino-pirazoles biciclicos como profarmacos
JP5580332B2 (ja) 2008-12-18 2014-08-27 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性な置換インダゾール誘導体
PT2707359T (pt) 2011-05-12 2017-01-09 Nerviano Medical Sciences Srl Derivados de indazol substituídos ativos como inibidores de quinase

Also Published As

Publication number Publication date
US10028934B2 (en) 2018-07-24
US9597317B2 (en) 2017-03-21
BR112013028733A2 (ru) 2017-08-29
TWI573790B (zh) 2017-03-11
KR20140037871A (ko) 2014-03-27
HK1193812A1 (zh) 2014-10-03
ZA201309345B (en) 2015-03-25
US10478423B2 (en) 2019-11-19
WO2012152763A1 (en) 2012-11-15
HUE031166T2 (hu) 2017-07-28
AU2012252468B2 (en) 2017-03-16
US20160311776A1 (en) 2016-10-27
SI2707359T1 (sl) 2017-02-28
AU2012252468A1 (en) 2014-01-09
PT2707359T (pt) 2017-01-09
CN103534239A (zh) 2014-01-22
CL2013003227A1 (es) 2014-06-27
JP6396210B2 (ja) 2018-09-26
US20160310465A1 (en) 2016-10-27
JP2014514353A (ja) 2014-06-19
CA2835478A1 (en) 2012-11-15
EA023579B1 (ru) 2016-06-30
PL2707359T3 (pl) 2017-05-31
SG194911A1 (en) 2013-12-30
CA2835478C (en) 2019-02-05
IL229252A (en) 2017-05-29
EP2707359B1 (en) 2016-11-30
CN103534239B (zh) 2016-04-20
MX2013012981A (es) 2013-12-12
EP2707359A1 (en) 2014-03-19
MX342509B (es) 2016-10-03
US9408850B2 (en) 2016-08-09
US20140080807A1 (en) 2014-03-20
TW201249806A (en) 2012-12-16
DK2707359T3 (en) 2017-01-23
ES2611779T3 (es) 2017-05-10
AR086357A1 (es) 2013-12-04
US20180289672A1 (en) 2018-10-11
BR112013028733B1 (pt) 2022-05-10
KR101953272B1 (ko) 2019-02-28
IL229252A0 (en) 2014-01-30

Similar Documents

Publication Publication Date Title
EA201391682A1 (ru) Замещенные производные индазола, активные в качестве ингибиторов киназы
EA201791018A1 (ru) Производные 6-амино-7-бицикло-7-деазапурина в качестве ингибиторов протеинкиназы
EA201490545A1 (ru) СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ С-Kit
EA201692166A1 (ru) Гетероциклические ингибиторы глютаминазы
JOP20120246B1 (ar) مركبات و تركيبات كمثبطات كيناز c-Kit
EA201490542A1 (ru) Соединения и композиции в качестве pdgfr киназных ингибиторов
EA201400707A1 (ru) Дизамещенные бензотиенил-пирролотриазины и их применение в качестве ингибиторов киназы рфрф
BR112015002152A2 (pt) pirróis substituídos ativos como inibidores de quinases
EA201590748A1 (ru) Противовирусные соединения против rsv
EA201290103A1 (ru) Гетероциклические соединения и их использование
EA201391416A1 (ru) Новые соединения в качестве модуляторов протеинкиназ
EA201591727A1 (ru) Соединения биариламида в качестве ингибиторов киназы
EA201690752A1 (ru) Ингибиторы g12c kras
EA201400412A1 (ru) ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ
EA201591753A1 (ru) 3-пиримидин-4-илоксазолидин-2-оны в качестве ингибиторов мутантного idh
EA201500394A1 (ru) Ингибиторы деметилаз гистонов
EA201491579A1 (ru) Соединения оксазолидин-2-она и их применения в качестве ингибиторов pi3k
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
EA201590855A1 (ru) Соединения пирролопиримидина как ингибиторы киназ
MX2013008296A (es) Diarilacetileno hidracido que contiene inhibidores de tirosina quinasa.
EA201592068A1 (ru) Ингибиторы энхансера zeste гомолога 2
EA201391285A1 (ru) Производные тетрагидрохинолина, полезные в качестве ингибиторов бромодомена
EA201790599A1 (ru) Соединения и композиции в качестве ингибиторов киназ
UA99141C2 (ru) Замещенные производные индазола, активные в качестве ингибиторов киназы
EA201490537A1 (ru) СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ C-Kit