WO2010125216A3 - Preparación de compuestos 5,6-dihidropirido[2,3-d]pirimidin-7(8h)-ona sustituidos - Google Patents

Preparación de compuestos 5,6-dihidropirido[2,3-d]pirimidin-7(8h)-ona sustituidos Download PDF

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Publication number
WO2010125216A3
WO2010125216A3 PCT/ES2010/070238 ES2010070238W WO2010125216A3 WO 2010125216 A3 WO2010125216 A3 WO 2010125216A3 ES 2010070238 W ES2010070238 W ES 2010070238W WO 2010125216 A3 WO2010125216 A3 WO 2010125216A3
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WO
WIPO (PCT)
Prior art keywords
general formula
dihydropyrido
pyrimidin
substituted
compounds
Prior art date
Application number
PCT/ES2010/070238
Other languages
English (en)
French (fr)
Other versions
WO2010125216A2 (es
Inventor
Xavier Berzosa Rodriguez
Jos Ignacio Borrell Bilbao
Original Assignee
Universitat Ramon Llull, Fundacio Privada
Institut Quimic De Sarria Cets, Fundacio Privada
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 Universitat Ramon Llull, Fundacio Privada, Institut Quimic De Sarria Cets, Fundacio Privada filed Critical Universitat Ramon Llull, Fundacio Privada
Publication of WO2010125216A2 publication Critical patent/WO2010125216A2/es
Publication of WO2010125216A3 publication Critical patent/WO2010125216A3/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C253/00—Preparation of carboxylic acid nitriles
    • C07C253/30—Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/19—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and carboxyl groups, other than cyano groups, bound to the same saturated acyclic carbon skeleton
    • C07C255/20—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and carboxyl groups, other than cyano groups, bound to the same saturated acyclic carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/23—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and carboxyl groups, other than cyano groups, bound to the same unsaturated acyclic carbon skeleton
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La invención describe un procedimiento para la preparación de compuestos 5,6-dihidropirido[2,3-d]pirimidin-7(8H)-ona sustituidos de fórmula general (3) útiles como inhibidores selectivos de las Proteína Quinasas, que comprende condensar un éster α,β-insaturado de fórmula general (4) con un propionitrilo de fórmula general (5) en presencia de una base concreta y hacer reaccionar el intermedio resultante con un compuesto guanidina de fórmula general (6) o una sal del mismo en presencia de otra base. La invención describe asimismo nuevos intermedios de síntesis de fórmula general (1) y de fórmula general (2).
PCT/ES2010/070238 2009-04-29 2010-04-19 Preparación de compuestos 5,6-dihidropirido[2,3-d]pirimidin-7(8h)-ona sustituidos WO2010125216A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ES200901191A ES2347630B1 (es) 2009-04-29 2009-04-29 Sintesis y usos de 4-cianopentanoatos y 4-cianopentenoatos sustituidos.
ESP200901191 2009-04-29

Publications (2)

Publication Number Publication Date
WO2010125216A2 WO2010125216A2 (es) 2010-11-04
WO2010125216A3 true WO2010125216A3 (es) 2012-12-27

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/ES2010/070238 WO2010125216A2 (es) 2009-04-29 2010-04-19 Preparación de compuestos 5,6-dihidropirido[2,3-d]pirimidin-7(8h)-ona sustituidos

Country Status (2)

Country Link
ES (1) ES2347630B1 (es)
WO (1) WO2010125216A2 (es)

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US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
CN107383009B (zh) 2012-06-13 2020-06-09 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
CN105263931B (zh) 2013-04-19 2019-01-25 因赛特公司 作为fgfr抑制剂的双环杂环
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3617205B1 (en) 2015-02-20 2021-08-04 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 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
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
JP2021523118A (ja) 2018-05-04 2021-09-02 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｆｇｆｒ阻害剤の塩
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
AU2020366006A1 (en) 2019-10-14 2022-04-21 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
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
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996015128A2 (en) * 1994-11-14 1996-05-23 Warner-Lambert Company 6-ARYL PYRIDO[2,3-d]PYRIMIDINES AND NAPHTHYRIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996015128A2 (en) * 1994-11-14 1996-05-23 Warner-Lambert Company 6-ARYL PYRIDO[2,3-d]PYRIMIDINES AND NAPHTHYRIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
J L FALCO ET AL.: "Solid-phase synthesis of 2- substituted 4-amino-7-exo-5,6,7,8- tetrahydropyrido[2,3-d]pyrimidines: An example of cyclization-assisted cleavage", MOLECULAR DIVERSITY, vol. 6, 2003, pages 3 - 11 *
N MONT ET AL.: "A one-pot microwave- assisted synthesis of pyrido[2,3-d]pyrimidines", MOLECULAR DIVERSITY, vol. 7, 2003, pages 153 - 159 *

Also Published As

Publication number Publication date
WO2010125216A2 (es) 2010-11-04
ES2347630B1 (es) 2011-09-08
ES2347630A1 (es) 2010-11-02

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