AR115019A2 - 2- (2,4,5-ANILINE SUBSTITUTED) PYRIMIDINE COMPOUNDS - Google Patents

2- (2,4,5-ANILINE SUBSTITUTED) PYRIMIDINE COMPOUNDS

Info

Publication number
AR115019A2
AR115019A2 ARP190100759A ARP190100759A AR115019A2 AR 115019 A2 AR115019 A2 AR 115019A2 AR P190100759 A ARP190100759 A AR P190100759A AR P190100759 A ARP190100759 A AR P190100759A AR 115019 A2 AR115019 A2 AR 115019A2
Authority
AR
Argentina
Prior art keywords
methyl
compounds
dimethylamino
amino
salts
Prior art date
Application number
ARP190100759A
Other languages
Spanish (es)
Inventor
Heather Marie Redfearn
Andiappan Murugan
Reddy C Chandrashekar
Vasantha Krishna Kadambar
Richard Andrew Ward
Maurice R V Finlay
Sam Butterworth
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR115019A2 publication Critical patent/AR115019A2/en

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D487/10—Spiro-condensed systems

Abstract

La presente se refiere a ciertos compuestos de 2-(2,4,5-anilino sustituido)pirimidina y sales farmacéuticamente aceptables de los mismos que pueden ser útiles en el tratamiento o prevención de una enfermedad o afección médica mediada por ciertas formas mutadas de receptor del factor de crecimiento epidérmico (por ejemplo el mutante activante L858R, el mutante activante de la supresión Exon19 y el mutante de resistencia T790M). Tales compuestos y sales de los mismos pueden ser útiles en el tratamiento o prevención de un número de diferentes cánceres. La presente también se refiere a composiciones farmacéuticas que comprenden dichos compuestos y sales de los mismos, especialmente formas polimórficas útiles de estos compuestos y sales, a intermedios útiles en la fabricación de dichos compuestos, y a métodos de tratamiento de enfermedades mediadas por diversas formas diferentes de EGFR usando dichos compuestos y sales de los mismos. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque: G se selecciona de 4,5,6,7-tetrahidropirazolo[1,5-a]piridin-3-ilo, 1H-indol-3-ilo, 1-metil-1H-indol-3-ilo y pirazolo[1,5-a]piridin-3-ilo; R¹ se selecciona de hidrógeno, flúor, cloro, metilo y ciano; R² se selecciona de metoxi y metilo; y R³ se selecciona de (3R)-3-(dimetilamino)pirrolidin-1-ilo, (3S)-3-(dimetil-amino)pirrolidin-1-ilo, 3-(dimetilamino)azetidin-1-ilo, [2-(dimetilamino)etil]-(metil)amino, [2-(metilamino)etil](metil)amino, 5-metil-2,5-diazaespiro[3.4]oct-2-ilo, (3aR,6aR)-5-metilhexa-hidro-pirrolo[3,4-b]pirrol-1(2H)-ilo, 1-metil-1,2,3,6-tetrahidropiridin-4-ilo, 4-metilpiperizin-1-ilo, 4-[2-(dimetilamino)-2-oxoetil]piperazin-1-ilo, metil[2-(4-metilpiperazin-1-il)etil]amino, metil[2-(morfolin-4-il)etil]amino, 1-amino-1,2,3,6-tetrahidropiridin-4-ilo y 4-[(2S)-2-aminopropanoil]piperazin-1-ilo; o una sal farmacéuticamente aceptable del mismo.This refers to certain 2- (2,4,5-substituted anilino) pyrimidine compounds and pharmaceutically acceptable salts thereof that may be useful in the treatment or prevention of a disease or medical condition mediated by certain mutated forms of receptor. epidermal growth factor (eg activating mutant L858R, activating deletion mutant Exon19, and resistance mutant T790M). Such compounds and salts thereof can be useful in the treatment or prevention of a number of different cancers. The present also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, to intermediates useful in the manufacture of said compounds, and to methods of treating diseases mediated by various different forms of EGFR using said compounds and salts thereof. Claim 1: A compound of formula (1) characterized in that: G is selected from 4,5,6,7-tetrahydropyrazolo [1,5-a] pyridin-3-yl, 1H-indol-3-yl, 1-methyl -1H-indol-3-yl and pyrazolo [1,5-a] pyridin-3-yl; R¹ is selected from hydrogen, fluorine, chlorine, methyl, and cyano; R² is selected from methoxy and methyl; and R³ is selected from (3R) -3- (dimethylamino) pyrrolidin-1-yl, (3S) -3- (dimethylamino) pyrrolidin-1-yl, 3- (dimethylamino) azetidin-1-yl, [2 - (dimethylamino) ethyl] - (methyl) amino, [2- (methylamino) ethyl] (methyl) amino, 5-methyl-2,5-diazaspiro [3.4] oct-2-yl, (3aR, 6aR) -5 -methylhexa-hydro-pyrrolo [3,4-b] pyrrole-1 (2H) -yl, 1-methyl-1,2,3,6-tetrahydropyridin-4-yl, 4-methylpiperizin-1-yl, 4- [2- (dimethylamino) -2-oxoethyl] piperazin-1-yl, methyl [2- (4-methylpiperazin-1-yl) ethyl] amino, methyl [2- (morpholin-4-yl) ethyl] amino, 1 -amino-1,2,3,6-tetrahydropyridin-4-yl and 4 - [(2S) -2-aminopropanoyl] piperazin-1-yl; or a pharmaceutically acceptable salt thereof.

ARP190100759A 2011-07-27 2019-03-26 2- (2,4,5-ANILINE SUBSTITUTED) PYRIMIDINE COMPOUNDS AR115019A2 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161512061P 2011-07-27 2011-07-27

Publications (1)

Publication Number Publication Date
AR115019A2 true AR115019A2 (en) 2020-11-18

Family

ID=53675818

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP190100759A AR115019A2 (en) 2011-07-27 2019-03-26 2- (2,4,5-ANILINE SUBSTITUTED) PYRIMIDINE COMPOUNDS

Country Status (2)

Country Link
AR (1) AR115019A2 (en)
UA (3) UA106710C2 (en)

Also Published As

Publication number Publication date
UA109736C2 (en) 2015-09-25
UA108954C2 (en) 2015-06-25
UA106710C2 (en) 2014-09-25

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