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TWI562994B - Fgf receptor (fgfr) agonist dimeric compounds, process for the preparation thereof and therapeutic use thereof - Google Patents

Fgf receptor (fgfr) agonist dimeric compounds, process for the preparation thereof and therapeutic use thereof

Info

Publication number
TWI562994B
TWI562994B TW101150736A TW101150736A TWI562994B TW I562994 B TWI562994 B TW I562994B TW 101150736 A TW101150736 A TW 101150736A TW 101150736 A TW101150736 A TW 101150736A TW I562994 B TWI562994 B TW I562994B
Authority
TW
Taiwan
Prior art keywords
fgfr
preparation
therapeutic use
fgf receptor
dimeric compounds
Prior art date
Application number
TW101150736A
Other languages
English (en)
Other versions
TW201333006A (zh
Inventor
Marie-Line Clary-Ceccato
Nathalie Guillo
Original Assignee
Sanofi Sa
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 Sanofi Sa filed Critical Sanofi Sa
Publication of TW201333006A publication Critical patent/TW201333006A/zh
Application granted granted Critical
Publication of TWI562994B publication Critical patent/TWI562994B/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
TW101150736A 2011-12-28 2012-12-27 Fgf receptor (fgfr) agonist dimeric compounds, process for the preparation thereof and therapeutic use thereof TWI562994B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR1162485A FR2985257B1 (fr) 2011-12-28 2011-12-28 Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique

Publications (2)

Publication Number Publication Date
TW201333006A TW201333006A (zh) 2013-08-16
TWI562994B true TWI562994B (en) 2016-12-21

Family

ID=47716121

Family Applications (1)

Application Number Title Priority Date Filing Date
TW101150736A TWI562994B (en) 2011-12-28 2012-12-27 Fgf receptor (fgfr) agonist dimeric compounds, process for the preparation thereof and therapeutic use thereof

Country Status (27)

Country Link
US (1) US9034898B2 (zh)
EP (1) EP2797917B1 (zh)
JP (1) JP6049756B2 (zh)
KR (1) KR20140105578A (zh)
CN (1) CN104136434B (zh)
AR (1) AR089452A1 (zh)
AU (1) AU2012360095B2 (zh)
BR (1) BR112014015882A8 (zh)
CA (1) CA2861718C (zh)
CY (1) CY1119301T1 (zh)
DK (1) DK2797917T3 (zh)
ES (1) ES2602798T3 (zh)
FR (1) FR2985257B1 (zh)
HK (1) HK1198649A1 (zh)
HR (1) HRP20161463T1 (zh)
HU (1) HUE029515T2 (zh)
IL (1) IL233324A (zh)
LT (1) LT2797917T (zh)
MX (1) MX356656B (zh)
PL (1) PL2797917T3 (zh)
PT (1) PT2797917T (zh)
RU (1) RU2014131065A (zh)
SG (1) SG11201403572RA (zh)
SI (1) SI2797917T1 (zh)
TW (1) TWI562994B (zh)
UY (1) UY34561A (zh)
WO (1) WO2013098764A1 (zh)

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WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
BR112014030812B1 (pt) 2012-06-13 2022-11-08 Incyte Holdings Corporation Compostos tricíclicos substituídos como inibidores de fgfr, seus usos, composição farmacêutica e método para inibir uma enzima fgfr
CN109627239B (zh) 2012-07-11 2021-10-12 缆图药品公司 成纤维细胞生长因子受体的抑制剂
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
ME03015B (me) 2013-04-19 2018-10-20 Incyte Holdings Corp Biciklični heterocikli kao fgfr inhibitori
WO2014200682A1 (en) * 2013-05-24 2014-12-18 The Scripps Research Institute Bidentate-binding modulators of lrrk2 and jnk kinases
PH12016500739B1 (en) 2013-10-25 2022-04-29 Blueprint Medicines Corp Inhibitors of the fibrolast growth factor receptor
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
US10851105B2 (en) 2014-10-22 2020-12-01 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
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CA3006897A1 (en) 2017-08-04 2019-02-04 University Health Network Generation of oligodendrogenic neural progenitor cells
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
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
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313611A (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
CN113651810B (zh) * 2021-07-16 2023-10-13 上海毕得医药科技股份有限公司 一种3-甲酰基-1H-吡唑并[3,4-b]吡啶-5-羧酸甲酯的合成方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007080325A1 (fr) * 2006-01-13 2007-07-19 Sanofi-Aventis Composes dimeres agonistes des recepteurs des fgfs
WO2011023081A1 (en) * 2009-08-24 2011-03-03 Ascepion Pharmaceuticals, Inc. 5,6-bicyclic heteroaryl-containing urea compounds as kinase inhibitors
WO2011045344A1 (en) * 2009-10-13 2011-04-21 Pierre Fabre Medicament Pyrazolopyridine derivatives as anticancer agent

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PE20010306A1 (es) * 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
US20070066641A1 (en) * 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
GB0402137D0 (en) * 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
MX2010004260A (es) * 2007-10-16 2010-04-30 Wyeth Llc Compuestos de tienopirimidina y pirazolopirimidina y su uso como inhibidores de mtor cinasa y pi3 cinasa.
ES2652287T3 (es) * 2009-12-21 2018-02-01 Samumed, Llc 1H-pirazol [3,4-b] piridinas y usos terapéuticos de las mismas

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007080325A1 (fr) * 2006-01-13 2007-07-19 Sanofi-Aventis Composes dimeres agonistes des recepteurs des fgfs
WO2011023081A1 (en) * 2009-08-24 2011-03-03 Ascepion Pharmaceuticals, Inc. 5,6-bicyclic heteroaryl-containing urea compounds as kinase inhibitors
WO2011045344A1 (en) * 2009-10-13 2011-04-21 Pierre Fabre Medicament Pyrazolopyridine derivatives as anticancer agent

Also Published As

Publication number Publication date
US20150011579A1 (en) 2015-01-08
ES2602798T3 (es) 2017-02-22
BR112014015882A8 (pt) 2017-07-04
CA2861718C (en) 2019-09-17
HUE029515T2 (en) 2017-02-28
JP2015503546A (ja) 2015-02-02
SI2797917T1 (sl) 2016-12-30
EP2797917A1 (en) 2014-11-05
FR2985257A1 (fr) 2013-07-05
CA2861718A1 (en) 2013-07-04
KR20140105578A (ko) 2014-09-01
AU2012360095A1 (en) 2014-07-24
WO2013098764A1 (en) 2013-07-04
JP6049756B2 (ja) 2016-12-21
AR089452A1 (es) 2014-08-27
HK1198649A1 (zh) 2015-05-22
US9034898B2 (en) 2015-05-19
MX2014007843A (es) 2014-11-25
AU2012360095B2 (en) 2017-02-02
TW201333006A (zh) 2013-08-16
EP2797917B1 (en) 2016-08-10
IL233324A (en) 2017-03-30
FR2985257B1 (fr) 2014-02-14
HRP20161463T1 (hr) 2016-12-16
PT2797917T (pt) 2016-11-15
PL2797917T3 (pl) 2017-08-31
CY1119301T1 (el) 2018-02-14
IL233324A0 (en) 2014-08-31
SG11201403572RA (en) 2014-07-30
MX356656B (es) 2018-06-07
UY34561A (es) 2013-07-31
DK2797917T3 (en) 2016-12-05
LT2797917T (lt) 2016-11-25
CN104136434B (zh) 2016-07-06
RU2014131065A (ru) 2016-02-20
BR112014015882A2 (pt) 2017-06-13
CN104136434A (zh) 2014-11-05

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