AU2013290074A1 - Inhibitors of the fibroblast growth factor receptor - Google Patents

Inhibitors of the fibroblast growth factor receptor Download PDF

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Publication number
AU2013290074A1
AU2013290074A1 AU2013290074A AU2013290074A AU2013290074A1 AU 2013290074 A1 AU2013290074 A1 AU 2013290074A1 AU 2013290074 A AU2013290074 A AU 2013290074A AU 2013290074 A AU2013290074 A AU 2013290074A AU 2013290074 A1 AU2013290074 A1 AU 2013290074A1
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AU
Australia
Prior art keywords
compound
optionally substituted
fgfr
alkyl
warhead
Prior art date
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Abandoned
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AU2013290074A
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English (en)
Inventor
Neil Bifulco Jr.
Natasja Brooijmans
Brian L. Hodous
Joseph L. Kim
Chandrasekhar V. Miduturu
Steven Mark Wenglowsky
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Blueprint Medicines Corp
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Blueprint Medicines Corp
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Publication of AU2013290074A1 publication Critical patent/AU2013290074A1/en
Priority to AU2017272281A priority Critical patent/AU2017272281B2/en
Abandoned legal-status Critical Current

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    • 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
    • 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
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    • 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
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
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    • 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

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  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
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  • Biophysics (AREA)
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  • Zoology (AREA)
  • Cell Biology (AREA)
  • Immunology (AREA)
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  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
AU2013290074A 2012-07-11 2013-07-11 Inhibitors of the fibroblast growth factor receptor Abandoned AU2013290074A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2017272281A AU2017272281B2 (en) 2012-07-11 2017-12-07 Inhibitors Of The Fibroblast Growth Factor Receptor

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
PCT/US2013/050106 WO2014011900A2 (en) 2012-07-11 2013-07-11 Inhibitors of the fibroblast growth factor receptor

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2017272281A Division AU2017272281B2 (en) 2012-07-11 2017-12-07 Inhibitors Of The Fibroblast Growth Factor Receptor

Publications (1)

Publication Number Publication Date
AU2013290074A1 true AU2013290074A1 (en) 2015-01-29

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ID=48874535

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AU2013290074A Abandoned AU2013290074A1 (en) 2012-07-11 2013-07-11 Inhibitors of the fibroblast growth factor receptor
AU2017272281A Ceased AU2017272281B2 (en) 2012-07-11 2017-12-07 Inhibitors Of The Fibroblast Growth Factor Receptor

Family Applications After (1)

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AU2017272281A Ceased AU2017272281B2 (en) 2012-07-11 2017-12-07 Inhibitors Of The Fibroblast Growth Factor Receptor

Country Status (26)

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US (6) US8802697B2 (enExample)
EP (1) EP2872491B1 (enExample)
JP (1) JP6104377B2 (enExample)
KR (2) KR20200117067A (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
ES2748038T3 (es) 2011-07-01 2020-03-12 Ngm Biopharmaceuticals Inc Composiciones, usos y métodos para el tratamiento de trastornos y enfermedades metabólicos
ES2984771T3 (es) 2012-06-13 2024-10-31 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
RU2019102203A (ru) * 2012-07-11 2019-03-05 Блюпринт Медсинс Корпорейшн Ингибиторы рецептора фактора роста фибробластов
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9290557B2 (en) 2012-11-28 2016-03-22 Ngm Biopharmaceuticals, Inc. Compositions comprising variants and fusions of FGF19 polypeptides
EP2925775B1 (en) 2012-11-28 2020-09-16 NGM Biopharmaceuticals, Inc. Compositions and methods for treatment of metabolic disorders and diseases
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
EP2938740B1 (en) 2012-12-27 2022-04-20 NGM Biopharmaceuticals, Inc. Chimeric fgf19 peptides for use in treating bile acid disorders
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
CN111793068A (zh) * 2013-03-15 2020-10-20 西建卡尔有限责任公司 杂芳基化合物和其用途
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
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
KR102350704B1 (ko) * 2013-03-15 2022-01-13 셀젠 카르 엘엘씨 헤테로아릴 화합물 및 이의 용도
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
AU2014287209B2 (en) 2013-07-09 2019-01-24 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
US20170050936A1 (en) 2013-08-23 2017-02-23 Neupharma, Inc. Certain chemical entities, compositions, and methods
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
WO2015057873A1 (en) 2013-10-17 2015-04-23 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
AR098048A1 (es) 2013-10-18 2016-04-27 Eisai R&D Man Co Ltd Inhibidores de fgfr4
PT3395814T (pt) 2013-10-25 2022-07-27 Blueprint Medicines Corp Inibidores do recetor do fator de crescimento de fibroblastos
TR201810944T4 (tr) 2013-10-25 2018-08-27 Novartis Ag Fgfr4 inhibitörleri olarak halka-füzyonlu bisiklik piridil türevleri.
KR102178945B1 (ko) 2013-10-28 2020-11-13 엔지엠 바이오파마슈티컬스, 아이엔씨. 암 모델 및 관련 방법
WO2015108992A1 (en) * 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
CN106458996B (zh) 2014-01-20 2020-11-03 克里弗生物科学公司 作为p97复合物的抑制剂的稠合嘧啶
PE20170256A1 (es) 2014-01-24 2017-04-22 Ngm Biopharmaceuticals Inc Proteinas de union y sus metodos de uso
KR102046448B1 (ko) * 2014-02-07 2019-11-19 프린시피아 바이오파마, 인코퍼레이티드 섬유모세포 성장 인자 수용체 저해제로서 퀴놀론 유도체들
US9932329B2 (en) 2014-03-03 2018-04-03 Principia Biopharma, Inc. Benzimidazole derivatives as RLK and ITK inhibitors
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
WO2015195509A2 (en) 2014-06-16 2015-12-23 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
US9951047B2 (en) 2014-08-18 2018-04-24 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
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
IL251834B2 (en) 2014-10-23 2023-09-01 Ngm Biopharmaceuticals Inc Pharmaceutical compositions containing peptide variants and methods of using them
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
CN107613769A (zh) * 2015-02-17 2018-01-19 润新生物公司 某些化学实体、组合物和方法
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
EA038045B1 (ru) 2015-02-20 2021-06-28 Инсайт Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
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
EP3275442B1 (en) 2015-03-25 2021-07-28 National Cancer Center Therapeutic agent for bile duct cancer
MX2017012295A (es) 2015-03-25 2018-01-09 Novartis Ag Derivados formilados n-heterociclicos como inhibidores de fgfr4.
EP3280708B1 (en) 2015-04-10 2021-09-01 Araxes Pharma LLC Substituted quinazoline compounds and methods of use thereof
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
KR20240070721A (ko) 2015-06-03 2024-05-21 프린시피아 바이오파마, 인코퍼레이티드 티로신 키나제 억제제
EP3322706B1 (en) 2015-07-16 2020-11-11 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
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
WO2017027567A1 (en) * 2015-08-11 2017-02-16 Principia Biopharma, Inc. Processes for preparing an fgfr inhibitor
AU2016311426B2 (en) 2015-08-26 2021-05-20 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to NTRK
US10730867B2 (en) 2015-09-28 2020-08-04 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
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 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
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
CA3002560A1 (en) * 2015-10-23 2017-04-27 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
TWI757256B (zh) 2015-11-02 2022-03-11 美商纜圖藥品公司 轉染過程重排之抑制劑
ES2871036T3 (es) 2015-11-09 2021-10-28 Ngm Biopharmaceuticals Inc Método para el tratamiento de trastornos relacionados con ácidos biliares
EA038635B9 (ru) 2015-11-16 2021-10-26 Араксис Фарма Ллк 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
EP3377497A1 (en) 2015-11-19 2018-09-26 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
WO2017104739A1 (ja) 2015-12-17 2017-06-22 エーザイ・アール・アンド・ディー・マネジメント株式会社 乳がん治療剤
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
TW201738228A (zh) 2016-03-17 2017-11-01 藍圖醫藥公司 Ｒｅｔ之抑制劑
RS65988B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Postupak lečenja pedijatrijskih karcinoma
HUE068971T2 (hu) 2016-04-04 2025-02-28 Loxo Oncology Inc (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid folyékony készítményei
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
EP3442977B1 (en) 2016-04-15 2023-06-28 Blueprint Medicines Corporation Inhibitors of activin receptor-like kinase
US11357769B2 (en) 2016-05-10 2022-06-14 Eisai R&D Management Co., Ltd. Drug combinations for reducing cell viability and/or cell proliferation
SI3458456T1 (sl) 2016-05-18 2021-04-30 Loxo Oncology, Inc. Priprava (S)-N-(5-((R)-2-(2,5-difluorofenil) pirolidin-1-il) pirazolo (1,5-A) pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
WO2018004258A1 (ko) * 2016-06-28 2018-01-04 한미약품 주식회사 신규한 헤테로시클릭 유도체 화합물 및 이의 용도
KR20180002053A (ko) * 2016-06-28 2018-01-05 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
US10227329B2 (en) 2016-07-22 2019-03-12 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
WO2018035061A1 (en) 2016-08-15 2018-02-22 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2018039557A1 (en) 2016-08-26 2018-03-01 Ngm Biopharmaceuticals, Inc. Methods of treating fibroblast growth factor 19-mediated cancers and tumors
RU2732127C1 (ru) * 2016-09-01 2020-09-11 Наньцзин Транстера Биосайенсиз Ко. Лтд. Ингибиторы рецептора фактора роста фибробластов и их применение
US20190192522A1 (en) * 2016-09-08 2019-06-27 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor 4 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
JP2019534260A (ja) 2016-10-07 2019-11-28 アラクセス ファーマ エルエルシー Ｒａｓの阻害剤としての複素環式化合物およびその使用方法
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
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
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
CN110267960B (zh) 2017-01-18 2022-04-26 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
WO2018140512A1 (en) 2017-01-26 2018-08-02 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
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
WO2018140514A1 (en) * 2017-01-26 2018-08-02 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
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
AU2018271990A1 (en) 2017-05-25 2019-12-12 Araxes Pharma Llc Covalent inhibitors of KRAS
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
US11639346B2 (en) 2017-05-25 2023-05-02 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
JP7346420B2 (ja) * 2017-09-05 2023-09-19 バイオアーディス エルエルシー 芳香族誘導体、その調製方法、およびその医学的適用
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
US11236086B2 (en) 2017-10-18 2022-02-01 Blueprint Medicines Corporation Substituted pyrrolopyridines as inhibitors of activin receptor-like kinase
JOP20180094A1 (ar) 2017-10-18 2019-04-18 Hk Inno N Corp مركب حلقي غير متجانس كمثبط بروتين كيناز
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
CN111971286B (zh) 2018-01-18 2023-04-14 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物
WO2019143994A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
TW201938169A (zh) 2018-01-18 2019-10-01 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[3,4-d]嘧啶化合物
EP3750880B1 (en) * 2018-02-08 2022-12-21 Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. Pyrazine-2(1h)-ketone compound acting as fgfr inhibitor
BR112020017922A2 (pt) 2018-03-28 2020-12-22 Eisai R&D Management Co., Ltd. Agente terapêutico para carcinoma hepatocelular
JP7422084B2 (ja) 2018-04-03 2024-01-25 ブループリント メディシンズ コーポレイション Ｒｅｔ変化を有する癌の処置において使用するためのｒｅｔ阻害剤
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
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
CN111868058B (zh) * 2018-05-25 2023-06-13 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
KR102653681B1 (ko) 2018-07-31 2024-04-03 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제
US12134620B2 (en) 2018-08-01 2024-11-05 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
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
KR102531596B1 (ko) * 2018-09-14 2023-05-11 아비스코 테라퓨틱스 컴퍼니 리미티드 Fgfr억제제, 그 제조 방법 및 용도
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
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine 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
WO2020185532A1 (en) 2019-03-08 2020-09-17 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
SMT202300447T1 (it) 2019-04-12 2024-01-10 Blueprint Medicines Corp Forme cristalline di (s)-1-(4-fluorofenil)-1-(2-(4-(6-(1-metil-1h-pirazol-4-yl)pirrolo[2,1-f][1,2,4]triazin-4-il)piperazinil)-pirimidin-5-il)etan-1-ammina e metodi di produzione
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
WO2021018047A1 (zh) 2019-07-26 2021-02-04 南京明德新药研发有限公司 作为fgfr和vegfr双重抑制剂的吡啶衍生物
ES3007814T3 (en) 2019-08-08 2025-03-20 Zhangzhou Pien Tze Huang Pharm Pyrazine-2(1h)-ketone compound preparation method
ES2954774T3 (es) * 2019-08-08 2023-11-24 Zhangzhou Pien Tze Huang Pharm Forma cristalina A y forma cristalina B del compuesto de pirazina-2(1H)-cetona y su método de preparación
EP4011869B1 (en) 2019-08-08 2023-11-15 Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. Crystal form d of pyrazine-2(1h)-ketone compound and preparation method therefor
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
PH12022550892A1 (en) 2019-10-14 2023-05-03 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
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021113492A1 (en) 2019-12-06 2021-06-10 Schrödinger, Inc. Cyclic compounds and methods of using same
CA3162851A1 (en) * 2019-12-23 2021-07-01 Qiang Zhang Cyano-substituted pyridine and cyano-substituted pyrimidine compound and preparation method therefor and application thereof
MX2022007171A (es) 2019-12-27 2022-08-22 Schroedinger Inc Compuestos cíclicos y métodos de uso de estos.
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3183728A1 (en) 2020-05-29 2021-12-02 Blueprint Medicines Corporation Solid forms of pralsetinib
CN116096707A (zh) * 2020-06-05 2023-05-09 金耐特生物制药公司 成纤维细胞生长因子受体激酶的抑制剂
EP4211140A1 (en) 2020-09-10 2023-07-19 Schrödinger, Inc. Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer
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
AU2022213682C1 (en) * 2021-01-26 2025-04-17 Cgenetech (Suzhou, China) Co., Ltd Crystal form of methylpyrazole-substituted pyridoimidazole compound and preparation method therefor
EP4284804A1 (en) 2021-01-26 2023-12-06 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
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
TWI820622B (zh) * 2021-03-04 2023-11-01 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
MX2023011342A (es) * 2021-03-26 2023-10-04 Hangzhou Apeloa Medicine Res Institute Co Ltd Inhibidor heterociclico biciclico de fgfr4, su composicion farmaceutica y formulacion, y sus aplicaciones.
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Ｆｇｆｒ阻害剤及びネクチン－４標的化剤を含む併用療法
WO2022261160A1 (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
WO2025059027A1 (en) 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors

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
ES2146782T3 (es) * 1994-11-14 2000-08-16 Warner Lambert Co 6-aril-pirido(2,3-d)pirimidinas y naftiridinas para la inhibicion de la proliferacion celular inducida por la proteina tirosina quinasa.
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
CN1138778C (zh) * 1998-05-26 2004-02-18 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及用途
US6403799B1 (en) 1999-10-21 2002-06-11 Agouron Pharmaceuticals, Inc. Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors
ATE353329T1 (de) * 1999-10-21 2007-02-15 Hoffmann La Roche Heteroalkylamino-substituierte bicyclische stickstoffheterocyclen
AU1462101A (en) 1999-11-22 2001-06-04 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
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
GEP20063909B (en) 2002-01-22 2006-08-25 Warner Lambert Co 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d] PYRIMIDIN-7-ONES
WO2004063195A1 (en) * 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
US20050124562A1 (en) 2003-09-23 2005-06-09 Joseph Guiles 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
JP5079500B2 (ja) * 2005-04-28 2012-11-21 協和発酵キリン株式会社 ２−アミノキナゾリン誘導体
US20090258882A1 (en) * 2006-07-28 2009-10-15 Novartis Ag 2,4-Substituted Quinazolines as Lipid Kinase Inhibitors
HRP20150642T1 (hr) 2006-12-22 2015-08-14 Astex Therapeutics Limited BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a
US20100216767A1 (en) 2006-12-22 2010-08-26 Mina Aikawa Quinazolines for pdk1 inhibition
GB2467670B (en) 2007-10-04 2012-08-01 Intellikine Inc Chemical entities and therapeutic uses thereof
TWI458721B (zh) * 2008-06-27 2014-11-01 Celgene Avilomics Res Inc 雜芳基化合物及其用途
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
CN102405284B (zh) * 2008-09-05 2016-01-20 新基阿维罗米克斯研究公司 设计不可逆抑制剂的算法
PE20120424A1 (es) 2008-12-29 2012-05-04 Fovea Pharmaceuticals Compuestos de quinazolina sustituidos
KR101529767B1 (ko) 2009-08-07 2015-06-17 추가이 세이야쿠 가부시키가이샤 아미노피라졸 유도체
EP2478361A4 (en) * 2009-09-16 2014-05-21 Celgene Avilomics Res Inc CONJUGATES AND INHIBITORS OF PROTEIN KINASE
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
MX340408B (es) 2011-04-21 2016-07-07 Ionis Pharmaceuticals Inc Modulacion de la expresion del virus de hepatitis b (vhb).
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
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
RU2019102203A (ru) * 2012-07-11 2019-03-05 Блюпринт Медсинс Корпорейшн Ингибиторы рецептора фактора роста фибробластов
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
HUE040434T2 (hu) 2013-02-21 2019-03-28 Pfizer Szelektív CDK4/6 inhibitor szilárd alakjai
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
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
CN111793068A (zh) 2013-03-15 2020-10-20 西建卡尔有限责任公司 杂芳基化合物和其用途
EP3024155B1 (en) 2013-07-14 2018-10-03 LG Electronics Inc. Method for transmitting data symbol using antenna correlation in wireless access system which supports massive antenna
WO2015057873A1 (en) 2013-10-17 2015-04-23 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
US9334263B2 (en) 2013-10-17 2016-05-10 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
AR098048A1 (es) 2013-10-18 2016-04-27 Eisai R&D Man Co Ltd Inhibidores de fgfr4
TR201810944T4 (tr) 2013-10-25 2018-08-27 Novartis Ag Fgfr4 inhibitörleri olarak halka-füzyonlu bisiklik piridil türevleri.
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
US9688680B2 (en) 2014-08-04 2017-06-27 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
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET 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
EA038045B1 (ru) 2015-02-20 2021-06-28 Инсайт Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
AU2016297754A1 (en) 2015-07-24 2018-02-15 Blueprint Medicines Corporation Compounds useful for treating disorders related to KIT and PDGFR
AU2016311426B2 (en) 2015-08-26 2021-05-20 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to NTRK
CA3002560A1 (en) 2015-10-23 2017-04-27 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases
TWI757256B (zh) 2015-11-02 2022-03-11 美商纜圖藥品公司 轉染過程重排之抑制劑
EP3377497A1 (en) 2015-11-19 2018-09-26 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
TW201738228A (zh) 2016-03-17 2017-11-01 藍圖醫藥公司 Ｒｅｔ之抑制劑
EP3442977B1 (en) 2016-04-15 2023-06-28 Blueprint Medicines Corporation Inhibitors of activin receptor-like kinase
US10227329B2 (en) 2016-07-22 2019-03-12 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
US20190192522A1 (en) 2016-09-08 2019-06-27 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor 4 in combination with cyclin-dependent kinase inhibitors

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