CN109627239B - 成纤维细胞生长因子受体的抑制剂 - Google Patents

成纤维细胞生长因子受体的抑制剂 Download PDF

Info

Publication number
CN109627239B
CN109627239B CN201811201617.4A CN201811201617A CN109627239B CN 109627239 B CN109627239 B CN 109627239B CN 201811201617 A CN201811201617 A CN 201811201617A CN 109627239 B CN109627239 B CN 109627239B
Authority
CN
China
Prior art keywords
compound
dimethoxyphenyl
fgfr
synthesis
amino
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201811201617.4A
Other languages
English (en)
Chinese (zh)
Other versions
CN109627239A (zh
Inventor
小尼尔·比富尔科
娜塔莎·布鲁杰孟
布赖恩·L·霍道什
约瑟夫·L·基姆
昌德拉塞卡·V·曼德拉
史蒂文·M·翁劳斯基
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cable Chart Pharmaceutical Co
Original Assignee
Cable Chart Pharmaceutical Co
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 Cable Chart Pharmaceutical Co filed Critical Cable Chart Pharmaceutical Co
Publication of CN109627239A publication Critical patent/CN109627239A/zh
Application granted granted Critical
Publication of CN109627239B publication Critical patent/CN109627239B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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
    • A61K31/4353—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
    • 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
    • A61K31/437—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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Toxicology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Steroid Compounds (AREA)
CN201811201617.4A 2012-07-11 2013-07-11 成纤维细胞生长因子受体的抑制剂 Active CN109627239B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261670379P 2012-07-11 2012-07-11
US61/670,379 2012-07-11
US201261746666P 2012-12-28 2012-12-28
US61/746,666 2012-12-28
CN201380042618.8A CN104540809B (zh) 2012-07-11 2013-07-11 成纤维细胞生长因子受体的抑制剂

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201380042618.8A Division CN104540809B (zh) 2012-07-11 2013-07-11 成纤维细胞生长因子受体的抑制剂

Publications (2)

Publication Number Publication Date
CN109627239A CN109627239A (zh) 2019-04-16
CN109627239B true CN109627239B (zh) 2021-10-12

Family

ID=48874535

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201811201617.4A Active CN109627239B (zh) 2012-07-11 2013-07-11 成纤维细胞生长因子受体的抑制剂
CN201380042618.8A Active CN104540809B (zh) 2012-07-11 2013-07-11 成纤维细胞生长因子受体的抑制剂

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201380042618.8A Active CN104540809B (zh) 2012-07-11 2013-07-11 成纤维细胞生长因子受体的抑制剂

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 (187)

* 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
JP6254524B2 (ja) 2011-07-01 2017-12-27 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 代謝障害及び疾患の治療のための組成物、使用及び方法
SMT201700146T1 (it) 2012-06-13 2017-05-08 Incyte Holdings Corp Composti triciclici sostituiti come inibitori di fgfr
CA2878412A1 (en) * 2012-07-11 2014-01-16 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
HK1214832A1 (zh) 2012-11-28 2016-08-05 恩格姆生物制药公司 用於代謝病症和疾病治療的組合物和方法
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
IL292303A (en) 2012-12-27 2022-06-01 Ngm Biopharmaceuticals Inc Methods for modulating bile acid homeostatsis and treatment of bile acid disorders and disease
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
AR095464A1 (es) 2013-03-15 2015-10-21 Celgene Avilomics Res Inc Compuestos de heteroarilo y usos de los mismos
MX374558B (es) * 2013-03-15 2025-03-06 Sanofi Sa Compuestos de heteroarilo y sus usos.
EP2970231A1 (en) 2013-03-15 2016-01-20 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
UA120248C2 (uk) * 2013-03-15 2019-11-11 Селджен Кар Ллс Гетероарильні сполуки та їх застосування
CA2909207C (en) 2013-04-19 2021-11-02 Incyte Corporation 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
CN111285813A (zh) 2013-08-23 2020-06-16 润新生物公司 化学实体、组合物和方法
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
SI3057969T1 (sl) 2013-10-17 2018-10-30 Blueprint Medicines Corporation Sestavki, uporabni za zdravljenje motenj, povezanih s KIT
HUE039268T2 (hu) 2013-10-18 2018-12-28 Eisai R&D Man Co Ltd Pirimidin FGFR4 inhibitorok
EP3060563B1 (en) 2013-10-25 2018-05-02 Novartis AG Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
LT3395814T (lt) 2013-10-25 2022-07-25 Blueprint Medicines Corporation Fibroblastų augimo faktoriaus receptoriaus inhibitoriai
MX377380B (es) 2013-10-28 2025-03-10 Ngm Biopharmaceuticals Inc Modelos de cáncer y métodos asociados.
US9695165B2 (en) * 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
EA031317B1 (ru) 2014-01-20 2018-12-28 Клив Байосайенсиз, Инк. КОНДЕНСИРОВАННЫЕ ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ КОМПЛЕКСА p97
MX375032B (es) 2014-01-24 2025-03-06 Ngm Biopharmaceuticals Inc Proteínas de unión y métodos para utilizarlas.
ES2689421T3 (es) 2014-02-07 2018-11-14 Principia Biopharma Inc. Derivados de quinolina como inhibidores de los receptores de los factores de crecimiento de fibroblastos
WO2015134210A1 (en) 2014-03-03 2015-09-11 Principia Biopharma, Inc. BENZIMIDAZOLE DERIVATIVES AS RLK and ITK INHIBITORS
WO2015183890A2 (en) 2014-05-28 2015-12-03 Ngm Biopharmaceuticals, Inc. Methods and compositions for the treatment of metabolic disorders and diseases
US10456449B2 (en) 2014-06-16 2019-10-29 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
CA2956270C (en) 2014-08-18 2022-08-09 Eisai R&D Management Co., Ltd. Salt of monocyclic pyridine derivative and crystal thereof
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
US20180185341A1 (en) 2014-10-03 2018-07-05 Novartis Ag Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CN114129709A (zh) 2014-10-23 2022-03-04 恩格姆生物制药公司 包含肽变异体的药物组合物及其使用方法
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
WO2016127074A1 (en) 2015-02-06 2016-08-11 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors
WO2016133935A1 (en) 2015-02-17 2016-08-25 Neupharma, Inc. Certain chemical entities, compositions, and methods
UA121669C2 (uk) 2015-02-20 2020-07-10 Інсайт Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
MA41551A (fr) * 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
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
JP6503450B2 (ja) 2015-03-25 2019-04-17 国立研究開発法人国立がん研究センター 胆管癌治療剤
BR112017016817A2 (pt) 2015-03-25 2018-04-03 Novartis Ag derivados heterocíclicos formilados como inibidores de fgfr4
JP2018513853A (ja) 2015-04-10 2018-05-31 アラクセス ファーマ エルエルシー 置換キナゾリン化合物およびその使用方法
JP6431622B2 (ja) 2015-04-14 2018-11-28 エーザイ・アール・アンド・ディー・マネジメント株式会社 結晶性ｆｇｆｒ４阻害剤化合物およびその使用
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
WO2016191172A1 (en) * 2015-05-22 2016-12-01 Principia Biopharma Inc. Quinolone derivatives as fibroblast growth factor receptor inhibitors
SG10201912443XA (en) 2015-06-03 2020-02-27 Principia Biopharma Inc Tyrosine kinase inhibitors
ES2857081T3 (es) 2015-07-16 2021-09-28 Array Biopharma Inc Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
AU2016297754A1 (en) 2015-07-24 2018-02-15 Blueprint Medicines Corporation Compounds useful for treating disorders related to KIT and PDGFR
WO2017019957A2 (en) 2015-07-29 2017-02-02 Ngm Biopharmaceuticals, Inc. Binding proteins and methods of use thereof
CN118388481A (zh) * 2015-08-11 2024-07-26 普林斯匹亚生物制药公司 用于制备fgfr抑制剂的方法
HK1255330A1 (zh) 2015-08-26 2019-08-16 缆图药品公司 适用於治疗与ntrk相关的病症的化合物和组合物
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 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
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356339A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
MX382526B (es) 2015-10-23 2025-03-13 Array Biopharma Inc Compuestos de 2-piridazin-3(2h)-ona 2-aril sustituidas y 2-heteroaril sustituidas como inhibidores de las tirosina quinasas fgfr
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
WO2017079140A1 (en) 2015-11-02 2017-05-11 Blueprint Medicines Corporation Inhibitors of ret
EP3888672A1 (en) 2015-11-09 2021-10-06 NGM Biopharmaceuticals, Inc. Methods for treatment of bile acid-related disorders
CA3005089A1 (en) 2015-11-16 2017-05-26 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
CA3005741A1 (en) 2015-11-19 2017-05-26 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
CN108367000A (zh) 2015-12-17 2018-08-03 卫材R&D管理有限公司 用于乳腺癌的治疗剂
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
UY37155A (es) 2016-03-17 2017-10-31 Blueprint Medicines Corp Inhibidores de ret
CU20180125A7 (es) 2016-04-04 2019-05-03 Loxo Oncology Inc Formulaciones líquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil) -pirrolidin-1-il)-pirazolo[1,5-alpirimidin-3-il)-3 hidroxipirrolidina-1-carboxamida
HRP20241295T1 (hr) 2016-04-04 2024-12-06 Loxo Oncology, Inc. Postupci za liječenje pedijatrijskih karcinoma
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
KR102426043B1 (ko) 2016-04-15 2022-07-27 블루프린트 메디신즈 코포레이션 액티빈 수용체 유사 키나아제의 저해제
EP3454898B1 (en) 2016-05-10 2021-11-10 Eisai R&D Management Co., Ltd. Drug combinations for reducing cell viability and/or cell proliferation
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
WO2018022761A1 (en) 2016-07-27 2018-02-01 Blueprint Medicines Corporation Substituted cyclopentane-amides 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
CA3034399A1 (en) 2016-08-26 2018-03-01 Ngm Biopharmaceuticals, Inc. Methods of treating fibroblast growth factor 19-mediated cancers and tumors
AU2017317864B2 (en) * 2016-09-01 2020-01-16 Transthera Sciences (Nanjing), Inc. Inhibitors of fibroblast growth factor receptor and use thereof
WO2018049233A1 (en) 2016-09-08 2018-03-15 Nicolas Stransky Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors
WO2018055503A1 (en) 2016-09-20 2018-03-29 Novartis Ag Combination comprising a pd-1 antagonist and an fgfr4 inhibitor
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
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
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
US11229643B2 (en) 2016-11-02 2022-01-25 Novartis Ag Combinations of FGFR4 inhibitors and bile acid sequestrants
CA3043948C (en) * 2016-11-17 2021-08-31 Guangdong Zhongsheng Pharmaceutical Co., Ltd Fgfr4 inhibitor and preparation method and use thereof
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
DK3524603T3 (da) 2016-12-19 2022-07-04 Abbisko Therapeutics Co Ltd Fgfr4-hæmmer, fremgangsmåde til fremstilling deraf og farmaceutisk anvendelse deraf
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
ES2948194T3 (es) 2017-01-18 2023-09-01 Array Biopharma Inc Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET
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
EP3573970A1 (en) * 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140600A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused hetero-hetero bicyclic compounds and methods of use thereof
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole 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
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
US10736897B2 (en) 2017-05-25 2020-08-11 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
BR112019024674A2 (pt) 2017-05-25 2020-06-16 Araxes Pharma Llc Inibidores covalentes da kras
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
CA3074885A1 (en) * 2017-09-05 2019-03-14 Bioardis Llc Aromatic derivative, preparation method for same, and medical applications 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
JOP20180094A1 (ar) 2017-10-18 2019-04-18 Hk Inno N Corp مركب حلقي غير متجانس كمثبط بروتين كيناز
WO2019079649A1 (en) 2017-10-18 2019-04-25 Blueprint Medicines Corporation SUBSTITUTED PYRROLOPYRIDINES AS INHIBITORS OF ACTIVIN RECEPTOR-RELATED KINASE
WO2019085894A1 (zh) * 2017-10-30 2019-05-09 如东凌达生物医药科技有限公司 一类含氮稠环化合物及其制备方法和用途
US11603374B2 (en) 2018-01-18 2023-03-14 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
CA3087578C (en) 2018-01-18 2023-08-08 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
TW201932464A (zh) 2018-01-18 2019-08-16 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基[4,3-c]吡啶化合物
US11286248B2 (en) 2018-02-08 2022-03-29 Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. Pyrazine-2(1H)-ketone compound acting as FGFR inhibitor
SG11202007591RA (en) 2018-03-28 2020-09-29 Eisai R&D Man Co Ltd Therapeutic agent for hepatocellular carcinoma
CA3096043A1 (en) 2018-04-03 2019-10-10 Blueprint Medicines Corporation 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
SMT202400507T1 (it) 2018-05-04 2025-01-14 Incyte Corp Forme solide di un inibitore di fgfr e procedimenti per preparare le stesse
SG11202010882XA (en) 2018-05-04 2020-11-27 Incyte Corp Salts of an fgfr inhibitor
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
KR102612513B1 (ko) 2018-07-31 2023-12-12 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
JP2021532157A (ja) 2018-08-01 2021-11-25 アラクセス ファーマ エルエルシー がんを処置するための複素環式スピロ化合物およびその使用方法
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
EP3849986B1 (en) 2018-09-10 2022-06-08 Array Biopharma, Inc. Fused heterocyclic compounds as ret kinase inhibitors
JP7152794B2 (ja) * 2018-09-14 2022-10-13 アビスコ セラピューティクス カンパニー リミテッド Ｆｇｆｒ阻害剤、その製造方法および応用
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
CN113474337A (zh) 2018-12-19 2021-10-01 奥瑞生物药品公司 作为fgfr抑制剂用于治疗癌症的7-((3，5-二甲氧基苯基)氨基)喹喔啉衍生物
WO2020177067A1 (en) * 2019-03-05 2020-09-10 Bioardis Llc Aromatic derivatives, preparation methods, and medical uses thereof
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
KR20210131369A (ko) * 2019-03-08 2021-11-02 쇼우야오 홀딩스 (베이징) 코., 엘티디. Fgfr4 키나아제 억제제 및 이의 제조 방법과 용도
FI3856341T3 (fi) 2019-04-12 2023-11-30 Blueprint Medicines Corp (s)-1-(4-fluorifenyyli)-1-(2-(4-(6-(1-metyyli-1h-pyratsol-4-yyli)pyrrolo[2,1-f][1,2,4]triatsin-4-yyli)piperatsinyyli)pyrimidin-5-yyli)etaani-1-amiinin kidemuotoja ja valmistusmenetelmiä
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
CA3145680C (en) * 2019-07-26 2024-03-12 Zhengxia CHEN Pyridine derivative as fgfr and vegfr dual inhibitors
CN114174270B (zh) * 2019-08-08 2023-06-06 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
US11597722B2 (en) 2019-08-08 2023-03-07 Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. Crystal form D of pyrazine-2(1H)-ketone compound and preparation method therefor
ES3007814T3 (en) 2019-08-08 2025-03-20 Zhangzhou Pien Tze Huang Pharm Pyrazine-2(1h)-ketone compound preparation method
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation 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
US11897891B2 (en) 2019-12-04 2024-02-13 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
EP4069369A4 (en) 2019-12-06 2024-02-14 Schrödinger, Inc. CYCLIC COMPOUNDS AND METHODS OF USE THEREOF
CN113087671B (zh) * 2019-12-23 2022-10-21 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
WO2021134004A1 (en) 2019-12-27 2021-07-01 Schrodinger, Inc. Cyclic compounds and methods of using same
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TW202210468A (zh) 2020-05-29 2022-03-16 美商纜圖藥品公司 普拉替尼之固體形式
US20230374015A1 (en) * 2020-06-05 2023-11-23 Kinnate Biopharma Inc. Inhibitors of fibroblast growth factor receptor kinases
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
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
EP4286382A4 (en) * 2021-01-26 2025-01-08 CGeneTech (Suzhou, China) Co., Ltd. CRYSTAL FORM OF A METHYLPYRAZOLE-SUBSTITUTED PYRIDOIMIDAZOLE COMPOUND AND METHOD FOR PREPARING THE SAME
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
TW202402754A (zh) * 2021-03-04 2024-01-16 美商美國禮來大藥廠 Fgfr3抑制劑化合物
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
CA3213379A1 (en) * 2021-03-26 2022-09-29 Weiqiang Zhan Bicyclic heterocyclic fgfr4 inhibitor, pharmaceutical composition and preparation, and a use thereof
CA3215903A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
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
WO2025059027A1 (en) 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1183099A (zh) * 1995-05-03 1998-05-27 沃尼尔·朗伯公司 抑制蛋白质酪氨酸激酶介导的细胞增殖的吡啶并[2,3－d]嘧啶
CN1302301A (zh) * 1998-05-26 2001-07-04 沃尼尔·朗伯公司 用作细胞增殖抑制剂的二环嘧啶及二环3,4－二氢嘧啶化合物
WO2004063195A1 (en) * 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
CN101490016A (zh) * 2006-07-28 2009-07-22 诺瓦提斯公司 作为脂激酶抑制剂的2,4-取代的喹唑啉
CN102083800A (zh) * 2008-06-27 2011-06-01 阿维拉制药公司 杂芳基化合物和其用途

Family Cites Families (59)

* 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
GB9708917D0 (en) * 1997-05-01 1997-06-25 Pfizer Ltd Compounds useful in therapy
US6403799B1 (en) 1999-10-21 2002-06-11 Agouron Pharmaceuticals, Inc. Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors
WO2001029042A1 (en) * 1999-10-21 2001-04-26 F. Hoffmann-La Roche Ag Heteroalkylamino-substituted bicyclic nitrogen heterocycles as inhibitors of p38 protein kinase
WO2001038315A1 (en) 1999-11-22 2001-05-31 Warner-Lambert Company Quinazolines and their use for inhibiting cyclin-dependent kinase enzymes
US6605615B2 (en) 2000-03-01 2003-08-12 Tularik Inc. Hydrazones and analogs as cholesterol lowering agents
US7022711B2 (en) 2000-08-04 2006-04-04 Warner-Lambert Company 2-(4-Pyridyl)amino-6-dialkoxyphenyl-pyrido[2,3-d]pyrimidin-7-ones
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
DK1470124T3 (da) 2002-01-22 2006-04-18 Warner Lambert Co 2-(Pyridin-2-yl amino)-pyrido[2,3]pyrimidin-7-oner
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
WO2006118256A1 (ja) * 2005-04-28 2006-11-09 Kyowa Hakko Kogyo Co., Ltd. 2-アミノキナゾリン誘導体
CA2672172C (en) 2006-12-22 2016-05-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
CN101652352A (zh) * 2006-12-22 2010-02-17 诺瓦提斯公司 用于抑制pdk1的喹唑啉类
US20110160232A1 (en) 2007-10-04 2011-06-30 Pingda Ren Certain chemical entities and therapeutic uses thereof
CA2738034A1 (en) 2008-09-03 2010-03-11 Licentia Ltd. Materials and methods for inhibiting cancer cell invasion related to fgfr4
BRPI0918970A2 (pt) * 2008-09-05 2019-09-24 Avila Therapeutics Inc algoritmo para projeto de inibidores irreversíveis
SG172415A1 (en) 2008-12-29 2011-07-28 Fovea Pharmaceuticals Sa Substituted quinazoline compounds
ES2561659T3 (es) 2009-08-07 2016-02-29 Chugai Seiyaku Kabushiki Kaisha Derivados de aminopirazol
NZ598705A (en) * 2009-09-16 2014-06-27 Celgene Avilomics Res Inc Protein kinase conjugates and inhibitors
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
SG194555A1 (en) 2011-04-21 2013-12-30 Isis Pharmaceuticals Inc Modulation of hepatitis b virus (hbv) expression
ES2770550T3 (es) * 2011-05-17 2020-07-02 Univ California Inhibidores de quinasa
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
CA2854093C (en) 2012-01-19 2016-07-05 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
CA2878412A1 (en) * 2012-07-11 2014-01-16 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives 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
HUE054212T2 (hu) 2013-02-21 2021-08-30 Pfizer Szelektív CDK4/6 inhibitor szilárd formái
AR095464A1 (es) * 2013-03-15 2015-10-21 Celgene Avilomics Res Inc Compuestos de heteroarilo y usos de los mismos
MX374558B (es) 2013-03-15 2025-03-06 Sanofi Sa Compuestos de heteroarilo y sus usos.
EP2970231A1 (en) 2013-03-15 2016-01-20 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
KR20160032007A (ko) 2013-07-14 2016-03-23 엘지전자 주식회사 매시브 안테나를 지원하는 무선 접속 시스템에서 안테나 상관도를 이용한 데이터 심볼 송수신 방법
SI3057969T1 (sl) 2013-10-17 2018-10-30 Blueprint Medicines Corporation Sestavki, uporabni za zdravljenje motenj, povezanih s KIT
US9334263B2 (en) 2013-10-17 2016-05-10 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
HUE039268T2 (hu) 2013-10-18 2018-12-28 Eisai R&D Man Co Ltd Pirimidin FGFR4 inhibitorok
EP3060563B1 (en) * 2013-10-25 2018-05-02 Novartis AG Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
LT3395814T (lt) * 2013-10-25 2022-07-25 Blueprint Medicines Corporation Fibroblastų augimo faktoriaus receptoriaus inhibitoriai
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
WO2016022569A1 (en) 2014-08-04 2016-02-11 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
US20160115164A1 (en) 2014-10-22 2016-04-28 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
WO2016127074A1 (en) 2015-02-06 2016-08-11 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
UA121669C2 (uk) 2015-02-20 2020-07-10 Інсайт Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
AU2016297754A1 (en) 2015-07-24 2018-02-15 Blueprint Medicines Corporation Compounds useful for treating disorders related to KIT and PDGFR
HK1255330A1 (zh) 2015-08-26 2019-08-16 缆图药品公司 适用於治疗与ntrk相关的病症的化合物和组合物
MX382526B (es) 2015-10-23 2025-03-13 Array Biopharma Inc Compuestos de 2-piridazin-3(2h)-ona 2-aril sustituidas y 2-heteroaril sustituidas como inhibidores de las tirosina quinasas fgfr
WO2017079140A1 (en) 2015-11-02 2017-05-11 Blueprint Medicines Corporation Inhibitors of ret
CA3005741A1 (en) 2015-11-19 2017-05-26 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
UY37155A (es) 2016-03-17 2017-10-31 Blueprint Medicines Corp Inhibidores de ret
KR102426043B1 (ko) 2016-04-15 2022-07-27 블루프린트 메디신즈 코포레이션 액티빈 수용체 유사 키나아제의 저해제
WO2018017983A1 (en) 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
WO2018022761A1 (en) 2016-07-27 2018-02-01 Blueprint Medicines Corporation Substituted cyclopentane-amides for treating disorders related to ret
WO2018049233A1 (en) 2016-09-08 2018-03-15 Nicolas Stransky Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1183099A (zh) * 1995-05-03 1998-05-27 沃尼尔·朗伯公司 抑制蛋白质酪氨酸激酶介导的细胞增殖的吡啶并[2,3－d]嘧啶
CN1302301A (zh) * 1998-05-26 2001-07-04 沃尼尔·朗伯公司 用作细胞增殖抑制剂的二环嘧啶及二环3,4－二氢嘧啶化合物
WO2004063195A1 (en) * 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
CN101490016A (zh) * 2006-07-28 2009-07-22 诺瓦提斯公司 作为脂激酶抑制剂的2,4-取代的喹唑啉
CN102083800A (zh) * 2008-06-27 2011-06-01 阿维拉制药公司 杂芳基化合物和其用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Soluble 2-Substituted Aminopyrido[2,3-d]pyrimidin-7-yl Ureas.Structure-Activity Relationships against Selected Tyrosine Kinases and Exploration of in Vitro and in Vivo Anticancer Activity;Mel C. Schroeder等;《J. Med. Chem.》;20010505;第44卷;第1915-1926页 *

Also Published As

Publication number Publication date
JP6104377B2 (ja) 2017-03-29
US20180362613A1 (en) 2018-12-20
IL236611A (en) 2017-02-28
RU2679130C2 (ru) 2019-02-06
EP2872491A2 (en) 2015-05-20
CY1124414T1 (el) 2022-07-22
AU2017272281B2 (en) 2019-07-04
AU2017272281A1 (en) 2018-01-04
SG11201500125QA (en) 2015-02-27
PT2872491T (pt) 2021-08-05
SI2872491T1 (sl) 2021-11-30
US10196436B2 (en) 2019-02-05
CN104540809A (zh) 2015-04-22
MX369472B (es) 2019-11-08
KR20200117067A (ko) 2020-10-13
US8802697B2 (en) 2014-08-12
CN104540809B (zh) 2018-12-11
RS62233B1 (sr) 2021-09-30
US9126951B2 (en) 2015-09-08
US20170066812A1 (en) 2017-03-09
WO2014011900A2 (en) 2014-01-16
US20140088100A1 (en) 2014-03-27
US9340514B2 (en) 2016-05-17
AU2013290074A1 (en) 2015-01-29
HRP20211218T1 (hr) 2021-10-29
US20190359682A1 (en) 2019-11-28
ZA201500215B (en) 2017-11-29
KR20150029030A (ko) 2015-03-17
SMT202100451T1 (it) 2021-09-14
MX2015000405A (es) 2015-07-14
JP2015523383A (ja) 2015-08-13
BR112015000653A2 (pt) 2019-11-05
IL236611A0 (en) 2015-02-26
CA2878412A1 (en) 2014-01-16
US20150210694A1 (en) 2015-07-30
WO2014011900A3 (en) 2014-02-27
ES2916220T3 (es) 2022-06-29
DK2872491T3 (da) 2021-08-09
US20140378481A1 (en) 2014-12-25
KR102163776B1 (ko) 2020-10-12
CN109627239A (zh) 2019-04-16
EP2872491B1 (en) 2021-05-05
NZ703495A (en) 2018-02-23
HK1206023A1 (en) 2015-12-31
RU2019102203A (ru) 2019-03-05
RU2015104342A (ru) 2016-08-27
PL2872491T3 (pl) 2021-12-13
LT2872491T (lt) 2021-08-25
HUE055502T2 (hu) 2021-11-29

Similar Documents

Publication Publication Date Title
CN109627239B (zh) 成纤维细胞生长因子受体的抑制剂
TWI629266B (zh) 纖維母細胞生長因子受體之抑制劑
US10000490B2 (en) Inhibitors of the fibroblast growth factor receptor
US20150119405A1 (en) Inhibitors of the fibroblast growth factor receptor
CN111635408A (zh) 三唑并-嘧啶化合物和其用途
HK40007301A (en) Inhibitors of the fibroblast growth factor receptor
HK1206023B (zh) 成纤维细胞生长因子受体的抑制剂
HK40045058B (en) Triazolo-pyrimidine compounds and uses thereof
HK40027808A (en) Triazolo-pyrimidine compounds and uses thereof
HK40027808B (en) Triazolo-pyrimidine compounds and uses thereof

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40007301

Country of ref document: HK

CB02 Change of applicant information
CB02 Change of applicant information

Address after: Massachusetts, USA

Applicant after: Cable chart pharmaceutical Co.

Address before: Massachusetts, USA

Applicant before: BLUEPRINT MEDICINES Corp.

GR01 Patent grant
GR01 Patent grant