EA021421B1 - Производные хинолинов и хиноксалинов в качестве ингибиторов протеинтирозинкиназы, способ их получения, содержащая их фармацевтическая композиция и способ лечения заболеваний с применением таких соединений - Google Patents

Производные хинолинов и хиноксалинов в качестве ингибиторов протеинтирозинкиназы, способ их получения, содержащая их фармацевтическая композиция и способ лечения заболеваний с применением таких соединений Download PDF

Info

Publication number
EA021421B1
EA021421B1 EA201001769A EA201001769A EA021421B1 EA 021421 B1 EA021421 B1 EA 021421B1 EA 201001769 A EA201001769 A EA 201001769A EA 201001769 A EA201001769 A EA 201001769A EA 021421 B1 EA021421 B1 EA 021421B1
Authority
EA
Eurasian Patent Office
Prior art keywords
carboxylic acid
dimethoxyphenyl
quinoxaline
amide
formula
Prior art date
Application number
EA201001769A
Other languages
English (en)
Russian (ru)
Other versions
EA201001769A1 (ru
Inventor
Паскаль Фюре
Диана Граус-Порта
Вито Гуаньяно
Original Assignee
Новартис Аг
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 Новартис Аг filed Critical Новартис Аг
Publication of EA201001769A1 publication Critical patent/EA201001769A1/ru
Publication of EA021421B1 publication Critical patent/EA021421B1/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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • A61K31/495—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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • 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
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/06—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
EA201001769A 2008-05-23 2009-05-20 Производные хинолинов и хиноксалинов в качестве ингибиторов протеинтирозинкиназы, способ их получения, содержащая их фармацевтическая композиция и способ лечения заболеваний с применением таких соединений EA021421B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08156846 2008-05-23
PCT/EP2009/056154 WO2009141386A1 (en) 2008-05-23 2009-05-20 Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201001769A1 EA201001769A1 (ru) 2011-06-30
EA021421B1 true EA021421B1 (ru) 2015-06-30

Family

ID=39643838

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201001769A EA021421B1 (ru) 2008-05-23 2009-05-20 Производные хинолинов и хиноксалинов в качестве ингибиторов протеинтирозинкиназы, способ их получения, содержащая их фармацевтическая композиция и способ лечения заболеваний с применением таких соединений

Country Status (33)

Country Link
US (4) US8273882B2 (enExample)
EP (1) EP2282995B1 (enExample)
JP (1) JP5351254B2 (enExample)
KR (1) KR101257158B1 (enExample)
CN (1) CN102036963B (enExample)
AR (1) AR071867A1 (enExample)
AU (1) AU2009248774B2 (enExample)
BR (1) BRPI0913031A2 (enExample)
CA (1) CA2725185C (enExample)
CO (1) CO6321283A2 (enExample)
CR (1) CR11727A (enExample)
CU (1) CU24001B1 (enExample)
DO (1) DOP2010000343A (enExample)
EA (1) EA021421B1 (enExample)
EC (1) ECSP10010627A (enExample)
ES (1) ES2554513T3 (enExample)
GE (1) GEP20125502B (enExample)
HN (1) HN2010002491A (enExample)
IL (1) IL209124A (enExample)
MA (1) MA32306B1 (enExample)
MX (1) MX2010012699A (enExample)
MY (1) MY155535A (enExample)
NI (1) NI201000190A (enExample)
NZ (1) NZ588511A (enExample)
PA (1) PA8827901A1 (enExample)
PE (1) PE20091955A1 (enExample)
SM (1) SMP201000124B (enExample)
SV (1) SV2010003741A (enExample)
TW (1) TWI448460B (enExample)
UA (1) UA103478C2 (enExample)
UY (1) UY31838A (enExample)
WO (1) WO2009141386A1 (enExample)
ZA (1) ZA201007086B (enExample)

Families Citing this family (121)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2554513T3 (es) 2008-05-23 2015-12-21 Novartis Ag Derivados de quinolinas y quinoxalinas como inhibidores de la proteína tirosina quinasa
SI2350075T1 (sl) 2008-09-22 2014-06-30 Array Biopharma, Inc. Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
EP2648754A4 (en) 2010-12-07 2016-02-24 Philadelphia Health & Educatio METHOD OF INHIBITING CANCER METASTASES
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US9340500B2 (en) 2011-04-20 2016-05-17 Shionogi & Co., Ltd. Aromatic heterocyclic derivative having TRPV4-inhibiting activity
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
WO2013063003A1 (en) 2011-10-28 2013-05-02 Novartis Ag Method of treating gastrointestinal stromal tumors
JP2014532647A (ja) 2011-10-28 2014-12-08 ノバルティス アーゲー 消化管間質腫瘍を治療する方法
BR112014015720B1 (pt) 2011-12-30 2020-03-17 Hanmi Pharm. Co., Ltd. Derivados de tieno[3,2-d]pirimidina, composição farmacêutica e uso dos mesmos para a prevenção ou tratamento de uma doença causada por ativação anormal de uma proteína quinase
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
PE20190736A1 (es) 2012-06-13 2019-05-23 Incyte Holdings Corp Compuestos triciclicos sustituidos como inhibidores del receptor del factor de crecimiento de fibroblastos (fgfr)
KR20150036014A (ko) 2012-07-11 2015-04-07 노파르티스 아게 위장 기질 종양을 치료하는 방법
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
AU2014228746B2 (en) * 2013-03-15 2018-08-30 Celgene Car Llc Heteroaryl compounds and uses thereof
ES2892423T3 (es) 2013-03-15 2022-02-04 Celgene Car Llc Compuestos de heteroarilo y usos de los mismos
KR102269032B1 (ko) 2013-04-19 2021-06-24 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
EP3757130A1 (en) 2013-09-26 2020-12-30 Costim Pharmaceuticals Inc. Methods for treating hematologic cancers
AU2014360743C1 (en) 2013-12-02 2021-01-28 Chemocentryx, Inc. CCR6 compounds
MX2016008362A (es) 2013-12-23 2016-09-08 Novartis Ag Combinaciones farmaceuticas.
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
ME03558B (me) 2014-03-14 2020-07-20 Novartis Ag Molekuli anti-lag-3 antiтela i njihove upotrebe
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
MX370099B (es) 2014-03-26 2019-12-02 Astex Therapeutics Ltd Combinación que comprende un inhibidor de fgfr y un inhibidor de cmet para el tratamiento del cáncer.
KR102479696B1 (ko) 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 Fgfr 억제제 및 igf1r 억제제의 조합물
ES2914072T3 (es) 2014-08-18 2022-06-07 Eisai R&D Man Co Ltd Sal de derivado de piridina monocíclico y su cristal
KR20170060042A (ko) 2014-09-13 2017-05-31 노파르티스 아게 Alk 억제제의 조합 요법
EA201790737A1 (ru) 2014-10-03 2017-08-31 Новартис Аг Комбинированная терапия
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
MX389663B (es) 2014-10-14 2025-03-20 Novartis Ag Moleculas de anticuerpo que se unen a pd-l1 y usos de las mismas.
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
ES2895769T3 (es) 2015-02-20 2022-02-22 Incyte Corp Heterociclos bicíclicos como inhibidores de FGFR
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10449211B2 (en) 2015-03-10 2019-10-22 Aduro Biotech, Inc. Compositions and methods for activating “stimulator of interferon gene”—dependent signalling
EP3275442B1 (en) 2015-03-25 2021-07-28 National Cancer Center Therapeutic agent for bile duct cancer
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
HK1255034A1 (zh) * 2015-07-01 2019-08-02 Crinetics Pharmaceuticals, Inc. 生长抑素调节剂及其用途
DK3322706T3 (da) 2015-07-16 2021-02-01 Array Biopharma Inc Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer
US20180222982A1 (en) 2015-07-29 2018-08-09 Novartis Ag Combination therapies comprising antibody molecules to pd-1
DK3317301T3 (da) 2015-07-29 2021-06-28 Immutep Sas Kombinationsterapier omfattende antistofmolekyler mod lag-3
EP3878465A1 (en) 2015-07-29 2021-09-15 Novartis AG Combination therapies comprising antibody molecules to tim-3
JP2018525371A (ja) * 2015-07-30 2018-09-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アリール置換された二環式ヘテロアリール化合物
CA2996857C (en) 2015-09-23 2024-05-21 Janssen Pharmaceutica Nv Quinoxaline, quinoline and quinazolinone derivative compounds for the treatment of cancer
KR102691777B1 (ko) 2015-09-23 2024-08-02 얀센 파마슈티카 엔브이 비-헤테로아릴 치환된 1,4-벤조디아제핀 및 암의 치료를 위한 이의 용도
JP2018534296A (ja) 2015-10-26 2018-11-22 ロクソ オンコロジー， インコーポレイテッドＬｏｘｏ Ｏｎｃｏｌｏｇｙ， Ｉｎｃ． Ｔｒｋ阻害薬耐性がんにおける点変異およびそれに関連する方法
RU2730503C2 (ru) 2015-12-17 2020-08-24 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Терапевтическое средство для лечения рака молочной железы
EP3389712B1 (en) 2015-12-17 2024-04-10 Novartis AG Antibody molecules to pd-1 and uses thereof
RS65988B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Postupak lečenja pedijatrijskih karcinoma
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
MX386416B (es) 2016-04-04 2025-03-18 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida.
HUE063877T2 (hu) 2016-05-18 2024-02-28 Loxo Oncology Inc (S)-N-(5-((R)-2-(2,5-dlfluorofenil)pirolidin-1-il)plrazolo[1,5-A]pirimidin-3-il) -3-hidroxipirolidin-1-karboxamid elõállítása
US11098077B2 (en) 2016-07-05 2021-08-24 Chinook Therapeutics, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
US10730868B2 (en) 2016-07-14 2020-08-04 Bristol-Myers Squibb Company Bicyclic heteroaryl substituted compounds
JP7058256B2 (ja) 2016-07-14 2022-04-21 ブリストル－マイヤーズ スクイブ カンパニー 二環式ヘテロアリール置換化合物
WO2018013776A1 (en) 2016-07-14 2018-01-18 Bristol-Myers Squibb Company Tricyclic heteroaryl-substituted quinoline and azaquinoline compounds as par4 inhibitors
IL264950B2 (en) * 2016-08-23 2024-01-01 Eisai R&D Man Co Ltd Combined treatments for the treatment of malignant liver cell carcinoma
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
WO2018071348A1 (en) * 2016-10-10 2018-04-19 Development Center For Biotechnology Quinoxaline compounds as type iii receptor tyrosine kinase inhibitors
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
CA3049136C (en) 2017-01-18 2022-06-14 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
US11267817B2 (en) 2017-05-02 2022-03-08 Drexel University Substituted pyrrolo[1,2-a]quinoxalin-4(5H)-ones as CX3CR1 antagonists
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2018237173A1 (en) 2017-06-22 2018-12-27 Novartis Ag Antibody molecules to cd73 and uses thereof
WO2019023278A1 (en) * 2017-07-25 2019-01-31 Crinetics Pharmaceuticals, Inc. MODULATORS OF SOMATOSTATIN AND USES THEREOF
TWI812649B (zh) 2017-10-10 2023-08-21 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
CA3087578C (en) 2018-01-18 2023-08-08 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
WO2019143994A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
CA3087354C (en) 2018-01-18 2023-01-03 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
EP3777860A4 (en) 2018-03-28 2021-12-15 Eisai R&D Management Co., Ltd. THERAPEUTIC FOR HEPATOCELLULAR CARCINOMA
SG11202010882XA (en) 2018-05-04 2020-11-27 Incyte Corp Salts of an fgfr inhibitor
SI3788047T1 (sl) 2018-05-04 2024-11-29 Incyte Corporation Trdne oblike inhibitorja fgfr in postopki priprave le-teh
TWI869346B (zh) 2018-05-30 2025-01-11 瑞士商諾華公司 Ｅｎｔｐｄ２抗體、組合療法、及使用該等抗體和組合療法之方法
KR102545594B1 (ko) 2018-07-31 2023-06-21 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제
CN112996794A (zh) 2018-09-10 2021-06-18 阿雷生物药品公司 作为ret激酶抑制剂的稠合杂环化合物
JP2022515197A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US20220348651A1 (en) 2019-09-18 2022-11-03 Novartis Ag Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11607416B2 (en) 2019-10-14 2023-03-21 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN110840876A (zh) * 2019-11-18 2020-02-28 青海民族大学 圆孢蘑菇中的没食子酸在cdc25磷酸蛋白酶上应用
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
WO2021134004A1 (en) 2019-12-27 2021-07-01 Schrodinger, Inc. Cyclic compounds and methods of using same
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN117903123A (zh) * 2020-02-20 2024-04-19 广州白云山医药集团股份有限公司白云山制药总厂 喹啉类化合物
US20240226098A1 (en) * 2020-02-28 2024-07-11 Remix Therapeutics Inc. Compounds and methods for modulating splicing
CN111646945A (zh) * 2020-05-29 2020-09-11 凯美克(上海)医药科技有限公司 一种4-溴-2-硝基-1h-咪唑的合成方法
JP2023541047A (ja) 2020-09-10 2023-09-27 シュレーディンガー， インコーポレイテッド がんの治療のための複素環式ペリ縮環ｃｄｃ７キナーゼ阻害剤
US20240148732A1 (en) 2021-01-26 2024-05-09 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
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
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20240102938A (ko) * 2021-08-30 2024-07-03 레믹스 테라퓨틱스 인크. 스플라이싱 조절을 위한 화합물 및 방법
CN114605391B (zh) * 2022-02-21 2024-01-26 广州六顺生物科技股份有限公司 喹喔啉类衍生物及其制备方法和应用
CN117510471B (zh) * 2022-07-29 2025-02-25 江苏天士力帝益药业有限公司 一种阿贝西利的合成方法
CN117865881A (zh) * 2022-10-12 2024-04-12 重庆博腾制药科技股份有限公司 一种阿贝西利中间体的制备方法
WO2025019622A2 (en) * 2023-07-18 2025-01-23 Elixiron Immunotherapeutics Inc. Method of enhanced absorption of quinoxaline type iii receptor tyrosine kinase inhibitors
WO2025059027A1 (en) 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005056547A2 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9823871D0 (en) * 1998-10-30 1998-12-23 Pharmacia & Upjohn Spa 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents
DE60004340T2 (de) * 1999-04-06 2004-06-09 Abbott Gmbh & Co. Kg Substituierte 1,4-dihydroindeno[1,2-c]pyrazole als inhibitoren von tyrosinkinase
GB0104422D0 (en) 2001-02-22 2001-04-11 Glaxo Group Ltd Quinoline derivative
EP1408986B1 (en) 2001-05-08 2008-09-24 Yale University Proteomimetic compounds and methods
WO2003007955A2 (en) 2001-07-20 2003-01-30 Cancer Research Technology Limited Biphenyl apurinic/apyrimidinic site endonuclease inhibitors to treat cancer
WO2003024446A1 (en) 2001-09-11 2003-03-27 Mitsubishi Pharma Corporation Oxidation stress inhibitor and method of measuring oxidation stress
CA2465978C (en) 2001-09-14 2015-04-07 Soon Hyung Woo Inhibitors of histone deacetylase
ATE511840T1 (de) 2001-10-09 2011-06-15 Amgen Inc Imidazolderivate als entzündungshemmende mittel
WO2004098494A2 (en) 2003-04-30 2004-11-18 Cytokinetics, Inc. Compounds, compositions, and methods
AR046845A1 (es) * 2003-11-21 2005-12-28 Novartis Ag Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas
US7501416B2 (en) 2004-02-06 2009-03-10 Bristol-Myers Squibb Company Quinoxaline compounds and methods of using them
WO2005087742A1 (en) 2004-03-08 2005-09-22 Exelixis, Inc. Metabolic kinase modulators and methods of use as pesticides
SE0401345D0 (sv) * 2004-05-25 2004-05-25 Astrazeneca Ab Therapeutic compounds: Pyridine as scaffold
US20070066646A1 (en) * 2005-08-02 2007-03-22 Genmedica Therapeutics Sl Compounds for Inhibiting Copper-Containing Amine Oxidases and Uses Thereof
AR058051A1 (es) 2005-09-21 2008-01-23 Astrazeneca Ab Quinolinas de alquilnitrilo.proceso de obtencion y composiciones farmaceuticas.
AR060358A1 (es) 2006-04-06 2008-06-11 Novartis Vaccines & Diagnostic Quinazolinas para la inhibicion de pdk 1
AR066879A1 (es) * 2007-06-08 2009-09-16 Novartis Ag Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus
KR20100072090A (ko) 2007-11-26 2010-06-29 화이자 인코포레이티드 5-ｌｏ 억제제로서의 피라졸 유도체
ES2554513T3 (es) * 2008-05-23 2015-12-21 Novartis Ag Derivados de quinolinas y quinoxalinas como inhibidores de la proteína tirosina quinasa
ES2455496T3 (es) 2008-05-23 2014-04-15 Glaxo Group Limited Compuestos tricíclicos que contienen nitrógeno y su uso como agentes antibacterianos
US8236792B2 (en) 2008-05-23 2012-08-07 Janssen Pharmaceutica Nv Substituted pyrrolidine amides as modulators of the histamine H3 receptor
US20110160249A1 (en) 2008-05-23 2011-06-30 Schaab Kevin Murray 5-lipoxygenase-activating protein inhibitor
EP2300483A1 (en) 2008-05-23 2011-03-30 Wyeth LLC Triazine compounds as p13 kinase and mtor inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005056547A2 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SUPURAN A. ET AL.: "Protein tyrosine kinase inhibitors as anticancer agents", EXPERT OPINION ON THERAPEUTIC PATENTS, ASHLEY PUBLICATIONS, GB, vol. 14, no. 1, 1 January 2004 (2004-01-01), pages 35-53, XP002336074, ISSN: 1354-3776, page 41; examples 23-25, page 49; examples 78, 79 *

Also Published As

Publication number Publication date
CU24001B1 (es) 2014-06-27
DOP2010000343A (es) 2010-11-30
NZ588511A (en) 2012-04-27
CA2725185C (en) 2016-10-25
US20100105667A1 (en) 2010-04-29
NI201000190A (es) 2011-08-01
ES2554513T3 (es) 2015-12-21
TWI448460B (zh) 2014-08-11
BRPI0913031A2 (pt) 2019-11-26
SMAP201000124A (it) 2011-01-19
AU2009248774A1 (en) 2009-11-26
KR20100135929A (ko) 2010-12-27
MX2010012699A (es) 2010-12-07
UA103478C2 (ru) 2013-10-25
CN102036963B (zh) 2013-08-21
PA8827901A1 (es) 2009-12-16
IL209124A0 (en) 2011-01-31
GEP20125502B (en) 2012-04-25
MA32306B1 (fr) 2011-05-02
US8273882B2 (en) 2012-09-25
CN102036963A (zh) 2011-04-27
EP2282995A1 (en) 2011-02-16
HN2010002491A (es) 2013-01-28
ECSP10010627A (es) 2010-12-30
US8815901B2 (en) 2014-08-26
ZA201007086B (en) 2011-12-28
WO2009141386A1 (en) 2009-11-26
AU2009248774B2 (en) 2012-05-31
KR101257158B1 (ko) 2013-04-23
US8536175B2 (en) 2013-09-17
CU20100219A7 (es) 2011-11-15
US8674099B2 (en) 2014-03-18
TW201000468A (en) 2010-01-01
JP5351254B2 (ja) 2013-11-27
CA2725185A1 (en) 2009-11-26
CO6321283A2 (es) 2011-09-20
IL209124A (en) 2014-06-30
PE20091955A1 (es) 2010-01-09
US20120309766A1 (en) 2012-12-06
MY155535A (en) 2015-10-30
EA201001769A1 (ru) 2011-06-30
EP2282995B1 (en) 2015-08-26
UY31838A (es) 2010-01-05
AR071867A1 (es) 2010-07-21
US20120309741A1 (en) 2012-12-06
SV2010003741A (es) 2011-07-05
US20130324519A1 (en) 2013-12-05
JP2011520941A (ja) 2011-07-21
CR11727A (es) 2010-12-29
SMP201000124B (it) 2011-09-09

Similar Documents

Publication Publication Date Title
EA021421B1 (ru) Производные хинолинов и хиноксалинов в качестве ингибиторов протеинтирозинкиназы, способ их получения, содержащая их фармацевтическая композиция и способ лечения заболеваний с применением таких соединений
US20230116233A1 (en) Compounds And Compositions As Protein Kinase Inhibitors
KR101530117B1 (ko) 야누스 키나제 억제제 화합물 및 방법
EA017952B1 (ru) ПИРРОЛО[2,3-d]ПИРИДИНЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ТИРОЗИНКИНАЗЫ
WO2017049462A1 (zh) 一类新型的flt3激酶抑制剂及其用途
US9550796B2 (en) Pyrrolopyrrolone derivatives and their use as BET inhibitors
JP2015518895A (ja) Ｅｇｆｒ活性を調節するための化合物および組成物
JP2014528446A (ja) １，３−置換アゼチジンｐｄｅ１０阻害剤
WO2010007374A1 (en) Pharmaceutical compounds
WO2023230477A1 (en) Pyridine checkpoint kinase 1 (chk1) inhibitors and uses thereof
CN102316738A (zh) 作为激酶抑制剂的酰胺类
HK1191936B (en) Compounds and compositions as protein kinase inhibitors
HK1167390B (en) Compounds and compositions as protein kinase inhibitors
HK1191936A (en) Compounds and compositions as protein kinase inhibitors

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 BY KZ KG MD TJ TM

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