IL236611A - Inhibitors of fibroblast growth factor receptor - Google Patents

Inhibitors of fibroblast growth factor receptor

Info

Publication number
IL236611A
IL236611A IL236611A IL23661115A IL236611A IL 236611 A IL236611 A IL 236611A IL 236611 A IL236611 A IL 236611A IL 23661115 A IL23661115 A IL 23661115A IL 236611 A IL236611 A IL 236611A
Authority
IL
Israel
Prior art keywords
inhibitors
growth factor
factor receptor
fibroblast growth
fibroblast
Prior art date
Application number
IL236611A
Other languages
English (en)
Hebrew (he)
Other versions
IL236611A0 (en
Original Assignee
Blueprint Medicines Corp
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 Blueprint Medicines Corp filed Critical Blueprint Medicines Corp
Publication of IL236611A0 publication Critical patent/IL236611A0/en
Publication of IL236611A publication Critical patent/IL236611A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/71—Receptors; Cell surface antigens; Cell surface determinants for growth factors; for growth regulators
    • 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
    • A61K31/4353—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
    • A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Cell Biology (AREA)
  • Immunology (AREA)
  • Toxicology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
IL236611A 2012-07-11 2015-01-11 Inhibitors of fibroblast growth factor receptor IL236611A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261670379P 2012-07-11 2012-07-11
US201261746666P 2012-12-28 2012-12-28
PCT/US2013/050106 WO2014011900A2 (en) 2012-07-11 2013-07-11 Inhibitors of the fibroblast growth factor receptor

Publications (2)

Publication Number Publication Date
IL236611A0 IL236611A0 (en) 2015-02-26
IL236611A true IL236611A (en) 2017-02-28

Family

ID=48874535

Family Applications (1)

Application Number Title Priority Date Filing Date
IL236611A IL236611A (en) 2012-07-11 2015-01-11 Inhibitors of fibroblast growth factor receptor

Country Status (26)

Country Link
US (6) US8802697B2 (enExample)
EP (1) EP2872491B1 (enExample)
JP (1) JP6104377B2 (enExample)
KR (2) KR102163776B1 (enExample)
CN (2) CN109627239B (enExample)
AU (2) AU2013290074A1 (enExample)
BR (1) BR112015000653A2 (enExample)
CA (1) CA2878412A1 (enExample)
CY (1) CY1124414T1 (enExample)
DK (1) DK2872491T3 (enExample)
ES (1) ES2916220T3 (enExample)
HR (1) HRP20211218T1 (enExample)
HU (1) HUE055502T2 (enExample)
IL (1) IL236611A (enExample)
LT (1) LT2872491T (enExample)
MX (1) MX369472B (enExample)
NZ (1) NZ703495A (enExample)
PL (1) PL2872491T3 (enExample)
PT (1) PT2872491T (enExample)
RS (1) RS62233B1 (enExample)
RU (2) RU2019102203A (enExample)
SG (1) SG11201500125QA (enExample)
SI (1) SI2872491T1 (enExample)
SM (1) SMT202100451T1 (enExample)
WO (1) WO2014011900A2 (enExample)
ZA (1) ZA201500215B (enExample)

Families Citing this family (188)

* 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
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
US8951966B2 (en) 2011-07-01 2015-02-10 Ngm Biopharmaceuticals, Inc. Compositions comprising variants and fusions of FGF19 polypeptides, and uses and methods thereof for treatment of metabolic disorders and diseases
CA2876689C (en) 2012-06-13 2022-04-26 Incyte Corporation Substituted tricyclic compounds as fgfr inhibitors
NZ703495A (en) 2012-07-11 2018-02-23 Blueprint Medicines Corp Inhibitors of the fibroblast growth factor receptor
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
EP3798228A1 (en) 2012-11-28 2021-03-31 NGM Biopharmaceuticals, Inc. Compositions and methods for treatment of metabolic disorders and diseases
US9290557B2 (en) 2012-11-28 2016-03-22 Ngm Biopharmaceuticals, Inc. Compositions comprising variants and fusions of FGF19 polypeptides
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US9273107B2 (en) 2012-12-27 2016-03-01 Ngm Biopharmaceuticals, Inc. Uses and methods for modulating bile acid homeostasis and treatment of bile acid disorders and diseases
MX383664B (es) 2012-12-27 2025-03-14 Ngm Biopharmaceuticals Inc Uso de un péptido para modular la homeostasis de los ácidos biliares o tratamiento de una enfermedad relacionada con los ácidos biliares.
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
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
MY181020A (en) 2013-03-15 2020-12-16 Sanofi Sa Heteroaryl compounds and uses thereof
WO2014160521A1 (en) 2013-03-15 2014-10-02 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
AU2014287209B2 (en) * 2013-07-09 2019-01-24 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
ES3069593T3 (en) 2013-08-23 2026-06-09 Neupharma Inc Quinazolin-8-yl derivatives for use in methods of treating melanoma, non-small cell lung cancer, thyroid cancer, ovarian cancer, or colon cancer
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
MX365614B (es) 2013-10-17 2019-06-07 Blueprint Medicines Corp Composiciones utiles para tratar trastornos relacionados con kit.
SG11201602069WA (en) 2013-10-18 2016-04-28 Eisai R&D Man Co Ltd Pyrimidine fgfr4 inhibitors
PT3395814T (pt) 2013-10-25 2022-07-27 Blueprint Medicines Corp Inibidores do recetor do fator de crescimento de fibroblastos
CN105683188B (zh) 2013-10-25 2018-02-09 诺华股份有限公司 作为fgfr4抑制剂的稠环二环吡啶基衍生物
NZ718962A (en) 2013-10-28 2019-12-20 Ngm Biopharmaceuticals Inc Cancer models and associated methods
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
US9828363B2 (en) 2014-01-20 2017-11-28 Cleave Biosciences, Inc. Fused pyrimidines as inhibitors of P97 complex
RS60593B1 (sr) 2014-01-24 2020-08-31 Ngm Biopharmaceuticals Inc Antitela koja vezuju domen 2 beta-kloto i postupci za njihovu upotrebu
DK3102577T3 (en) * 2014-02-07 2018-11-12 Principia Biopharma Inc QUINOLONDERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS
EP3114124A1 (en) 2014-03-03 2017-01-11 Principia Biopharma, Inc. BENZIMIDAZOLE DERIVATIVES AS RLK and ITK INHIBITORS
MA38393B1 (fr) 2014-03-13 2018-11-30 Sanofi Sa Composés hétéroaryle et utilisations associées
US10398758B2 (en) 2014-05-28 2019-09-03 Ngm Biopharmaceuticals, Inc. Compositions comprising variants of FGF19 polypeptides and uses thereof for the treatment of hyperglycemic conditions
EP3155005A4 (en) 2014-06-16 2018-07-11 NGM Biopharmaceuticals, Inc. Methods and uses for modulating bile acid homeostasis and treatment of bile acid disorders and diseases
CN105017227B (zh) * 2014-07-08 2018-03-09 四川百利药业有限责任公司 N‑(1h‑吡唑‑5‑基)喹唑啉‑4‑胺类化合物
WO2016027781A1 (ja) 2014-08-18 2016-02-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 単環ピリジン誘導体の塩およびその結晶
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
ES2756748T3 (es) 2014-10-03 2020-04-27 Novartis Ag Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
SG11201702757YA (en) 2014-10-23 2017-05-30 Ngm Biopharmaceuticals Inc Pharmaceutical compositions comprising peptide variants and methods of use thereof
US10434144B2 (en) 2014-11-07 2019-10-08 Ngm Biopharmaceuticals, Inc. Methods for treatment of bile acid-related disorders and prediction of clinical sensitivity to treatment of bile acid-related disorders
WO2016115412A1 (en) * 2015-01-18 2016-07-21 Newave Pharmaceutical Llc Dual-warhead covalent inhibitors of fgfr-4
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
EP3270694A4 (en) * 2015-02-17 2018-09-05 Neupharma, Inc. Certain chemical entities, compositions, and methods
CA2976790C (en) 2015-02-20 2024-02-27 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9802917B2 (en) 2015-03-25 2017-10-31 Novartis Ag Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide
EP3274344B1 (en) 2015-03-25 2019-04-24 Novartis Ag Formylated n-heterocyclic derivatives as fgfr4 inhibitors
CN114984013A (zh) 2015-03-25 2022-09-02 国立癌症研究中心 胆管癌治疗剂
AU2016245864C1 (en) 2015-04-10 2021-09-09 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
CN107660200B (zh) 2015-04-14 2022-01-11 卫材R&D管理有限公司 结晶fgfr4抑制剂化合物和其用途
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
US10538517B2 (en) 2015-05-22 2020-01-21 Principia Biopharma, Inc. Quinolone derivatives as FGFR inhibitors
EP3912979B1 (en) 2015-06-03 2026-03-25 Principia Biopharma Inc. Tyrosine kinase inhibitors
CA2992586A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
BR112018001190A2 (pt) 2015-07-24 2018-09-11 Blueprint Medicines Corp composições úteis para tratar distúrbios relacionados a kit e pdfgr
US10800843B2 (en) 2015-07-29 2020-10-13 Ngm Biopharmaceuticals, Inc. Beta klotho-binding proteins
EP3334735B1 (en) * 2015-08-11 2025-08-13 Principia Biopharma Inc. Processes for preparing an fgfr inhibitor
WO2017035354A1 (en) 2015-08-26 2017-03-02 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058768A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3365335B1 (en) * 2015-10-23 2024-02-14 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
RS65069B1 (sr) 2015-11-02 2024-02-29 Blueprint Medicines Corp Inhibitori ret-a
JP6728352B2 (ja) 2015-11-09 2020-07-22 エヌジーエム バイオファーマシューティカルス，インコーポレーテッド 胆汁酸に関係した障害の治療方法
KR102932353B1 (ko) 2015-11-16 2026-02-27 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
SG10201912607SA (en) 2015-11-19 2020-02-27 Blueprint Medicines Corp Compounds and compositions useful for treating disorders related to ntrk
AU2016374441B2 (en) 2015-12-17 2021-10-21 Eisai R&D Management Co., Ltd. Therapeutic agent for breast cancer
CN105669566A (zh) * 2016-03-09 2016-06-15 华东师范大学 一种医药中间体n-芳基喹唑啉-2-胺化合物的制备方法
AR107912A1 (es) 2016-03-17 2018-06-28 Blueprint Medicines Corp Inhibidores de ret
UA125026C2 (uk) 2016-04-04 2021-12-29 Локсо Онколоджі, Інк. РІДКІ КОМПОЗИЦІЇ (S)-N-(5-((R)-2-(2,5-ДИФТОРФЕНІЛ)ПІРОЛІДИН-1-ІЛ)ПІРАЗОЛО[1,5-a]ПІРИМІДИН-3-ІЛ)-3-ГІДРОКСИПІРОЛІДИН-1-КАРБОКСАМІДУ
UA125025C2 (uk) 2016-04-04 2021-12-29 Локсо Онколоджі, Інк. Способи лікування дитячих ракових захворювань
FI3442977T3 (fi) 2016-04-15 2023-09-26 Blueprint Medicines Corp Aktiviinireseptorin kaltaisen kinaasin estäjät
JP7372740B2 (ja) 2016-05-10 2023-11-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 細胞生存性及び／又は細胞増殖を低減するための薬物の組み合わせ
MX392604B (es) 2016-05-18 2025-03-24 Array Biopharma Inc Procesos para la preparacion de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo.
KR20180002053A (ko) * 2016-06-28 2018-01-05 한미약품 주식회사 신규한 헤테로시클릭 유도체 화합물 및 이의 용도
WO2018004258A1 (ko) * 2016-06-28 2018-01-04 한미약품 주식회사 신규한 헤테로시클릭 유도체 화합물 및 이의 용도
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
WO2018017983A1 (en) 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
US10035789B2 (en) 2016-07-27 2018-07-31 Blueprint Medicines Corporation Compounds useful for treating disorders related to RET
CN109843858B (zh) 2016-08-15 2023-05-05 润新生物公司 某些化学实体、组合物及方法
US11370841B2 (en) 2016-08-26 2022-06-28 Ngm Biopharmaceuticals, Inc. Methods of treating fibroblast growth factor 19-mediated cancers and tumors
JP6751977B2 (ja) * 2016-09-01 2020-09-09 南京薬捷安康生物科技有限公司 線維芽細胞増殖因子受容体の阻害剤及びそれらの使用
CN110022900A (zh) * 2016-09-08 2019-07-16 蓝图药品公司 成纤维细胞生长因子受体4抑制剂与细胞周期蛋白依赖性激酶抑制剂的组合
WO2018055503A1 (en) 2016-09-20 2018-03-29 Novartis Ag Combination comprising a pd-1 antagonist and an fgfr4 inhibitor
JP2019529484A (ja) 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
TWI752098B (zh) 2016-10-10 2022-01-11 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
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
WO2018072707A1 (zh) * 2016-10-18 2018-04-26 保诺科技（北京）有限公司 芳香族醚类衍生物、其制备方法及其在医药上的应用
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JP7394623B2 (ja) 2016-11-02 2023-12-08 ノバルティス アーゲー Ｆｇｆｒ４インヒビターおよび胆汁酸捕捉薬の組合せ
MX389403B (es) * 2016-11-17 2025-03-20 Guangdong Zhongsheng Pharmaceutical Co Ltd Inhibidor del receptor del factor de crecimiento de fibroblastos 4 (fgfr4) y metodo de preparacion y uso del mismo
KR101812266B1 (ko) 2016-11-25 2017-12-27 한국과학기술연구원 4-((2-아크릴아미도페닐)아미노)티에노[3,2-d]피리미딘-7-카복스아미드 유도체 및 그의 약학적 활용
RU2747260C2 (ru) * 2016-12-19 2021-04-29 Аббиско Тхерапеутицс Цо., Лтд. Ингибитор рфрф4, способ его получения и его фармацевтическое применение
CN108239069B (zh) * 2016-12-26 2021-01-05 南京药捷安康生物科技有限公司 一种用于成纤维细胞生长因子受体的抑制剂及其用途
CN108264511B (zh) * 2017-01-03 2021-04-13 浙江海正药业股份有限公司 杂环类衍生物及其制备方法和其在医药上的用途
JP6888101B2 (ja) 2017-01-18 2021-06-16 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置換ピラゾロ［１，５−ａ］ピラジン化合物
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
CN108503593B (zh) * 2017-02-28 2021-04-27 暨南大学 2-氨基嘧啶类化合物及其应用
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
WO2018183712A1 (en) 2017-03-31 2018-10-04 Blueprint Medicines Corporation Pyrrolo[1,2-b]pyridazine compounds and compositions useful for treating disorders related to kit and pdgfr
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
TW201906832A (zh) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 用於癌症治療之化合物及其使用方法
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3444275A1 (en) 2017-08-16 2019-02-20 Exiris S.r.l. Monoclonal antibody anti-fgfr4
CN110997637B (zh) * 2017-09-05 2022-09-27 保仕健生物科技(上海)有限公司 芳香类衍生物、其制备方法及其在医药上的应用
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
KR102717072B1 (ko) 2017-10-18 2024-10-15 인사이트 코포레이션 Pi3k-감마 저해제로서의 3차 하이드록시기로 치환된 축합된 이미다졸 유도체
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
EP3697786B1 (en) 2017-10-18 2022-08-31 Blueprint Medicines Corporation Substituted pyrrolopyridines as inhibitors of activin receptor-like kinase
CN109721600B (zh) * 2017-10-30 2021-04-27 上海凌达生物医药有限公司 一类含氮稠环化合物及其制备方法和用途
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
EP3740486A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
CN111630054B (zh) 2018-01-18 2023-05-09 奥瑞生物药品公司 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物
CN111683928B (zh) * 2018-02-08 2021-12-10 漳州片仔癀药业股份有限公司 作为fgfr抑制剂的吡嗪-2(1h)-酮类化合物
BR112020017922A2 (pt) 2018-03-28 2020-12-22 Eisai R&D Management Co., Ltd. Agente terapêutico para carcinoma hepatocelular
SG11202009681YA (en) 2018-04-03 2020-10-29 Blueprint Medicines Corp Ret inhibitor for use in treating cancer having a ret alteration
CN110386921A (zh) * 2018-04-23 2019-10-29 南京药捷安康生物科技有限公司 成纤维细胞生长因子受体抑制剂化合物
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
KR102956194B1 (ko) 2018-05-04 2026-04-23 인사이트 코포레이션 Fgfr 억제제의 염
WO2019223766A1 (zh) * 2018-05-25 2019-11-28 上海和誉生物医药科技有限公司 一种fgfr抑制剂、其制备方法和在药学上的应用
CN110577524B (zh) * 2018-06-07 2022-01-28 北京大学深圳研究生院 一种激酶选择性抑制剂
WO2019242689A1 (zh) * 2018-06-22 2019-12-26 北京赛特明强医药科技有限公司 一种氰基取代吡啶及氰基取代嘧啶类化合物、制备方法及其应用
CA3108065C (en) 2018-07-31 2025-10-07 Loxo Oncology, Inc. SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
ES2922314T3 (es) 2018-09-10 2022-09-13 Array Biopharma Inc Compuestos heterocíclicos condensados como inhibidores de cinasa RET
WO2020052349A1 (zh) * 2018-09-14 2020-03-19 上海和誉生物医药科技有限公司 Fgfr抑制剂、其制备方法和应用
CN110950867A (zh) * 2018-09-27 2020-04-03 首药控股(北京)有限公司 一种fgfr4激酶抑制剂及其制备方法和用途
CN111138459B (zh) * 2018-11-06 2022-10-18 南京圣和药业股份有限公司 Fgfr4抑制剂的光学异构体及其应用
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
WO2020119606A1 (en) * 2018-12-10 2020-06-18 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heterocyclic compounds as inhibitors of fibroblast growth factor receptor
WO2020131627A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
WO2020177067A1 (en) * 2019-03-05 2020-09-10 Bioardis Llc Aromatic derivatives, preparation methods, and medical uses thereof
EP3936509B1 (en) * 2019-03-08 2024-07-31 Shouyao Holdings (Beijing) Co., Ltd. Fgfr4 kinase inhibitor, preparation method therefor and use thereof
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
HUE064283T2 (hu) 2019-04-12 2024-02-28 Blueprint Medicines Corp Az (S)-1-(4-fluorofenil)-1-(2-(4-(6-(1-metil-1H-pirazol-4-il)pirrolo[2,1-f][1,2,4]triazin-4-il) piperazinil)-pirimidin-5-il)etán-1-amin kristályos formái és elõállítási eljárásai
CN110317176A (zh) * 2019-07-04 2019-10-11 沈阳药科大学 2-氨基嘧啶类化合物及其用途
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US12378241B2 (en) 2019-07-26 2025-08-05 Cgenetech (Suzhou,China) Co., Ltd. Pyridine derivative as FGFR and VEGFR dual inhibitors
WO2021023195A1 (zh) * 2019-08-08 2021-02-11 漳州片仔癀药业股份有限公司 吡嗪-2（1h）-酮类化合物的d晶型及其制备方法
WO2021023193A1 (zh) * 2019-08-08 2021-02-11 漳州片仔癀药业股份有限公司 吡嗪-2(1h)-酮类化合物的制备方法
WO2021023192A1 (zh) * 2019-08-08 2021-02-11 漳州片仔癀药业股份有限公司 吡嗪-2(1h)-酮类化合物的a晶型和b晶型及其制备方法
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN112759593A (zh) 2019-11-01 2021-05-07 北京伯汇生物技术有限公司 桥环并醛基吡啶衍生物及其应用
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
MX2022006691A (es) 2019-12-04 2022-09-19 Incyte Corp Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr).
US20230101747A1 (en) 2019-12-06 2023-03-30 Schrödinger, Inc. Cyclic compounds and methods of using same
AU2020414132B2 (en) 2019-12-23 2024-02-15 Beijing Scitech-Mq Pharmaceuticals Limited Cyano-substituted pyridine and cyano-substituted pyrimidine compound and preparation method therefor and application thereof
IL294214B2 (en) 2019-12-27 2026-04-01 Schrodinger Inc Cyclic compounds and methods of using same
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021243192A1 (en) 2020-05-29 2021-12-02 Blueprint Medicines Corporation Solid forms of pralsetinib
CR20220666A (es) 2020-05-29 2023-05-05 Blueprint Medicines Corp Composiciones farmacéuticas de pralsetinib
EP4161657A1 (en) * 2020-06-05 2023-04-12 Kinnate Biopharma Inc. Inhibitors of fibroblast growth factor receptor kinases
CN116490507A (zh) 2020-09-10 2023-07-25 薛定谔公司 用于治疗癌症的杂环包缩合cdc7激酶抑制剂
CN112851587A (zh) * 2021-01-21 2021-05-28 药雅科技(上海)有限公司 一种用于治疗癌症的炔类杂环化合物及其制备方法与用途
EP4284804A1 (en) 2021-01-26 2023-12-06 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
WO2022161408A1 (zh) * 2021-01-26 2022-08-04 南京明德新药研发有限公司 甲基吡唑取代的吡啶并咪唑类化合物的晶型及其制备方法
CN114853740B (zh) * 2021-02-03 2023-08-01 药雅科技(上海)有限公司 炔类嘧啶化合物作为fgfr抑制剂的制备方法和用途
AR125588A1 (es) * 2021-03-04 2023-08-02 Lilly Co Eli Compuestos inhibidores de fgfr3
WO2022194160A1 (zh) * 2021-03-16 2022-09-22 上海启晟合研医药科技有限公司 非索替尼固体形式及其制备方法
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
AU2021436754B2 (en) * 2021-03-26 2024-11-07 Apeloa Pharmaceutical Co., Ltd. Bicyclic heterocyclic fgfr4 inhibitor, pharmaceutical composition and preparation comprising same, and application thereof
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313610A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之三環雜環
CN113912602B (zh) * 2021-10-14 2023-05-05 温州医科大学 一种2-氧代-1,2-二氢-1,6-萘啶-7-基类化合物及其制备方法和用途
WO2024242495A1 (ko) * 2023-05-25 2024-11-28 주식회사 매직불릿테라퓨틱스 단백질 키나아제 억제용 신규 화합물 및 이를 포함하는 약학조성물
TWI896159B (zh) * 2023-06-09 2025-09-01 大陸商上海和譽生物醫藥科技有限公司 一種fgfr4抑制劑組合物、其製備方法和在藥學上的應用
EP4509142A1 (en) 2023-08-16 2025-02-19 Ona Therapeutics S.L. Fgfr4 as target in cancer treatment
CN122003418A (zh) 2023-09-11 2026-05-08 薛定谔公司 作为malt1抑制剂的环戊并[e]吡唑并[1,5-a]嘧啶衍生物

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US173074A (en) * 1876-02-01 Improvement in flour and meal bolts
FI971953A7 (fi) * 1994-11-14 1997-05-12 Warner Lambert Co Proteiinityrosiinikinaasin välittämää soluproliferaatiota inhiboivat 6 -aryyli-pyrido(2,3-d)pyrimidiinit ja naftyridiinit
IL117923A (en) * 1995-05-03 2000-06-01 Warner Lambert Co Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds
GB9708917D0 (en) * 1997-05-01 1997-06-25 Pfizer Ltd Compounds useful in therapy
DE69939168D1 (de) * 1998-05-26 2008-09-04 Warner Lambert Co Bicyclische pyrimidine und bicyclische 3,4-dihydropyrimidine als inhibitoren der zellvermehrung
US6403799B1 (en) 1999-10-21 2002-06-11 Agouron Pharmaceuticals, Inc. Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors
DE60033307T2 (de) * 1999-10-21 2007-07-12 F. Hoffmann-La Roche Ag Heteroalkylamino-substituierte bicyclische stickstoffheterocyclen als p38-proteinkinase-inhibitoren
CA2386955A1 (en) 1999-11-22 2001-05-31 Warner-Lambert Company Quinazolines and their use for inhibiting cyclin-dependent kinase enzymes
AU2001245401A1 (en) 2000-03-01 2001-09-12 Sumitomo Pharmaceuticals Company, Limited Hydrazones and analogs as cholesterol lowering agents
JP2004519422A (ja) 2000-08-04 2004-07-02 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー ２−（４−ピリジル）アミノ−６−ジアルコキシフェニルピリド〔２，３−ｄ〕ピリミジン−７−オン
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
NZ534069A (en) 2002-01-22 2007-03-30 Warner Lambert Co 2-(Pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones to be used to treat neurodegenerative disorders, viruses and cancer
WO2004063195A1 (en) * 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
WO2005030131A2 (en) 2003-09-23 2005-04-07 Replidyne, Inc Bis-quinazoline compounds for the treatment of bacterial infections
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
EP1878727A4 (en) * 2005-04-28 2013-11-13 Kyowa Hakko Kirin Co Ltd 2-AMINOQUINAZOLINE DERIVATIVES
PT2049502E (pt) * 2006-07-28 2012-04-02 Novartis Ag Quinazolinas 2,4-substituídas como inibidores da lípido cinase
CA2673003A1 (en) * 2006-12-22 2008-07-03 Novartis Ag Quinazolines for pdk1 inhibition
CN101679408B (zh) 2006-12-22 2016-04-27 Astex治疗学有限公司 作为fgfr抑制剂的双环杂环化合物
US20110160232A1 (en) 2007-10-04 2011-06-30 Pingda Ren Certain chemical entities and therapeutic uses thereof
AU2009262068C1 (en) * 2008-06-27 2015-07-02 Celgene Car Llc Heteroaryl compounds and uses thereof
CN102224170A (zh) 2008-09-03 2011-10-19 利琴蒂亚有限公司 抑制与fgfr4相关的癌细胞侵袭的材料和方法
JP2012501654A (ja) * 2008-09-05 2012-01-26 アビラ セラピューティクス， インコーポレイテッド 不可逆的インヒビターの設計のためのアルゴリズム
CA2748319A1 (en) 2008-12-29 2010-07-08 Fovea Pharmaceuticals Substituted quinazoline compounds of general formula (i) and uses thereof for treating disorders relating to tyrosine kinase dysregulation
HRP20151258T1 (hr) 2009-08-07 2016-02-26 Chugai Seiyaku Kabushiki Kaisha Derivat aminopirazola
CN102713618B (zh) 2009-09-16 2015-07-15 新基阿维罗米克斯研究公司 蛋白激酶复合物和抑制剂
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
SI3505528T1 (sl) 2011-04-21 2021-04-30 Glaxo Group Limited Modulacija izražanja virusa hepatitisa B (HBV)
DK2710007T3 (da) * 2011-05-17 2020-01-27 Principia Biopharma Inc Kinasehæmmere
FR2985257B1 (fr) * 2011-12-28 2014-02-14 Sanofi Sa Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique
AU2013210403B2 (en) 2012-01-19 2016-01-14 Taiho Pharmaceutical Co., Ltd. 3,5-disubstituted alkynylbenzene compound and salt thereof
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
NZ703495A (en) 2012-07-11 2018-02-23 Blueprint Medicines Corp Inhibitors of the fibroblast growth factor receptor
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
WO2014044846A1 (en) 2012-09-24 2014-03-27 Evotec (Uk) Ltd. 3-(aryl- or heteroaryl-amino)-7-(3,5-dimethoxyphenyl)isoquinoline derivatives as fgfr inhibitors useful for the treatment of proliferative disorders or dysplasia
TWI629266B (zh) * 2012-12-28 2018-07-11 藍印藥品公司 纖維母細胞生長因子受體之抑制劑
DK3431475T3 (da) 2013-02-21 2021-05-25 Pfizer Faste former af en selektiv CDK4/6-hæmmer
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
WO2014160521A1 (en) 2013-03-15 2014-10-02 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
WO2015008992A1 (ko) 2013-07-14 2015-01-22 엘지전자 주식회사 매시브 안테나를 지원하는 무선 접속 시스템에서 안테나 상관도를 이용한 데이터 심볼 송수신 방법
US9334263B2 (en) 2013-10-17 2016-05-10 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
MX365614B (es) 2013-10-17 2019-06-07 Blueprint Medicines Corp Composiciones utiles para tratar trastornos relacionados con kit.
SG11201602069WA (en) 2013-10-18 2016-04-28 Eisai R&D Man Co Ltd Pyrimidine fgfr4 inhibitors
CN105683188B (zh) 2013-10-25 2018-02-09 诺华股份有限公司 作为fgfr4抑制剂的稠环二环吡啶基衍生物
PT3395814T (pt) * 2013-10-25 2022-07-27 Blueprint Medicines Corp Inibidores do recetor do fator de crescimento de fibroblastos
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
MA38393B1 (fr) 2014-03-13 2018-11-30 Sanofi Sa Composés hétéroaryle et utilisations associées
US9688680B2 (en) 2014-08-04 2017-06-27 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
WO2016064960A1 (en) 2014-10-22 2016-04-28 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CA2976790C (en) 2015-02-20 2024-02-27 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
BR112018001190A2 (pt) 2015-07-24 2018-09-11 Blueprint Medicines Corp composições úteis para tratar distúrbios relacionados a kit e pdfgr
WO2017035354A1 (en) 2015-08-26 2017-03-02 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
EP3365335B1 (en) 2015-10-23 2024-02-14 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases
RS65069B1 (sr) 2015-11-02 2024-02-29 Blueprint Medicines Corp Inhibitori ret-a
SG10201912607SA (en) 2015-11-19 2020-02-27 Blueprint Medicines Corp Compounds and compositions useful for treating disorders related to ntrk
AR107912A1 (es) 2016-03-17 2018-06-28 Blueprint Medicines Corp Inhibidores de ret
FI3442977T3 (fi) 2016-04-15 2023-09-26 Blueprint Medicines Corp Aktiviinireseptorin kaltaisen kinaasin estäjät
WO2018017983A1 (en) 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
US10035789B2 (en) 2016-07-27 2018-07-31 Blueprint Medicines Corporation Compounds useful for treating disorders related to RET
CN110022900A (zh) 2016-09-08 2019-07-16 蓝图药品公司 成纤维细胞生长因子受体4抑制剂与细胞周期蛋白依赖性激酶抑制剂的组合

Also Published As

Publication number Publication date
US20180362613A1 (en) 2018-12-20
WO2014011900A2 (en) 2014-01-16
HRP20211218T1 (hr) 2021-10-29
DK2872491T3 (da) 2021-08-09
JP2015523383A (ja) 2015-08-13
US9340514B2 (en) 2016-05-17
SMT202100451T1 (it) 2021-09-14
RU2679130C2 (ru) 2019-02-06
JP6104377B2 (ja) 2017-03-29
ES2916220T3 (es) 2022-06-29
IL236611A0 (en) 2015-02-26
AU2017272281B2 (en) 2019-07-04
US20150210694A1 (en) 2015-07-30
US20140378481A1 (en) 2014-12-25
US9126951B2 (en) 2015-09-08
WO2014011900A3 (en) 2014-02-27
CN109627239B (zh) 2021-10-12
CA2878412A1 (en) 2014-01-16
ZA201500215B (en) 2017-11-29
MX369472B (es) 2019-11-08
HK1206023A1 (en) 2015-12-31
NZ703495A (en) 2018-02-23
AU2013290074A1 (en) 2015-01-29
HUE055502T2 (hu) 2021-11-29
RU2019102203A (ru) 2019-03-05
SI2872491T1 (sl) 2021-11-30
CN104540809A (zh) 2015-04-22
AU2017272281A1 (en) 2018-01-04
US10196436B2 (en) 2019-02-05
US20140088100A1 (en) 2014-03-27
RU2015104342A (ru) 2016-08-27
LT2872491T (lt) 2021-08-25
CN109627239A (zh) 2019-04-16
PL2872491T3 (pl) 2021-12-13
US8802697B2 (en) 2014-08-12
KR20150029030A (ko) 2015-03-17
RS62233B1 (sr) 2021-09-30
PT2872491T (pt) 2021-08-05
KR20200117067A (ko) 2020-10-13
KR102163776B1 (ko) 2020-10-12
US20170066812A1 (en) 2017-03-09
MX2015000405A (es) 2015-07-14
EP2872491A2 (en) 2015-05-20
EP2872491B1 (en) 2021-05-05
BR112015000653A2 (pt) 2019-11-05
SG11201500125QA (en) 2015-02-27
US20190359682A1 (en) 2019-11-28
CN104540809B (zh) 2018-12-11
CY1124414T1 (el) 2022-07-22

Similar Documents

Publication Publication Date Title
ZA201500215B (en) Inhibitors of the fibroblast growth factor receptor
IL244738B (en) Inhibitors of the fibroblast growth factor receptor
ZA201501009B (en) Imidazotriazinecarbonitriles useful as kinase inhibitors
PL2710007T3 (pl) Inhibitory kinazy
ZA201404156B (en) Kinase inhibitors
ZA201407441B (en) Solid forms of an epidermal growth factor receptor kinase inhibitor
ZA201407938B (en) Fibroblast growth factor 21 variants
IL229028A0 (en) Kinase inhibitors
GB201009731D0 (en) Kinase inhibitors
GB201211310D0 (en) CSF-1R kinase inhibitors
SG11201500973WA (en) Amino-quinolines as kinase inhibitors
EP2903970A4 (en) SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS
ZA201404157B (en) Kinase inhibitors
EP2885291A4 (en) INHIBITORS OF VEGFR3
EP2900243A4 (en) BICYCLIC OXA LACTAM KINASE HEMMER
EP2885292A4 (en) VEGFR3 INHIBITORS
GB201208881D0 (en) Cyfamagusta

Legal Events

Date Code Title Description
FF Patent granted
KB Patent renewed
KB Patent renewed