AR058624A1 - PIRIMIDINE DERIVATIVES AS INHIBITORS OF PIRIMIDIN QUINASA SUBSTITUTES. PROCESSES OF OBTAINING AND PHARMACEUTICAL COMPOSITIONS. - Google Patents

PIRIMIDINE DERIVATIVES AS INHIBITORS OF PIRIMIDIN QUINASA SUBSTITUTES. PROCESSES OF OBTAINING AND PHARMACEUTICAL COMPOSITIONS.

Info

Publication number
AR058624A1
AR058624A1 ARP060105731A ARP060105731A AR058624A1 AR 058624 A1 AR058624 A1 AR 058624A1 AR P060105731 A ARP060105731 A AR P060105731A AR P060105731 A ARP060105731 A AR P060105731A AR 058624 A1 AR058624 A1 AR 058624A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
aryl
amino
heteroaryl
Prior art date
Application number
ARP060105731A
Other languages
Spanish (es)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR058624A1 publication Critical patent/AR058624A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Abstract

Su síntesis y uso para tratar, prevenir o mejorar una enfermedad, trastorno o alteracion cronica o aguda intermediada por proteinquinasas. Reivindicacion 1: Un compuesto de formula (1) y formas de éste, donde L está seleccionado entre un enlace, alquilo C1-6 o halo-alquilo C1-6; Ar está seleccionado entre arilo, heteroarilo, heterociclilo benzofusionado o cicloalquilo C3-12 benzofusionado, donde la porcion de anillo benceno del sistema de anillo benzofusionado está unida a la variable L; RA está seleccionado entre C=N-O-R1 o ciano; R1 está seleccionado entre H, alquilo C1-8, alquenilo C1-8, alcoxi C1-8, alcoxi C1-8-alquilo C1-8, hidroxi-alquilo C1-8, hidroxi-alcoxi C1-8, amino-alquilo C1-8, alquilo C1-8-amino-alquilo C1-8, alcoxi C1-8- alquilo C1-8-amino-alquilo C1-8, alquilo C1-8-sulfonil-alquilo C1-8, alquilo C1-8-sulfoniloxi-alquilo C1-8, arilo, aril-alquilo C1-8, ariloxi-alquilo C1-8, heterociclil-alquilo C1-8, heterociclil-carbonil-alquilo C1-8 o heteroaril-alquilo C1-8; donde aril-alquilo C1-8 está opcionalmente sustituido en el arilo con 1, 2, 3, 4 o 5 sustituyentes cada uno seleccionado entre hidroxi, alquilo C1-8, alcoxi C1-8, amino, alquilo C1-8-amino o alcoxicarbonilo C1-8, y donde hetrociclil-alquilo C1-8 está opcionalmente sustituido en el heterociclilo con 1, 2, 3 o 4 sustituyentes cada uno seleccionado entre hidroxi, alquilo C1-8, alcoxi C1-8, amino, alquilo C1-8-amino o alcoxicarbonilo C1-8; R2 esta selecionado de H, alquilo C1-8 o alcoxi C1-8; y R3, R4, R5, R6 y R7 está cada uno seleccionado de H, halogeno, hidroxi, alquilo C1-8, alcoxi C1-8, alcoxi C1-8-alquilo C1-8, hidroxi-alquilo C1-8, halo-alquilo C1-8, hidroxi-alcoxi C1-8, halo-alcoxi C1-8, amino, alquilo C1-8-amino, amino-alquilo C1- 8, alquilo C1-8-amino-alquilo C1-8, carboxi, acilo C1-8, alcoxicarbonilo C1-8, cicloalquilo C3-12, arilo, ariloxi, aril-alquilo C1-8, aril-alcoxi C1-8, aril-amido, heteroarilo, heteroariloxi, hteroaril-C1-8-alcoxi o heterociclilo, donde arilo, ariloxi, aril-alquilo C1-8 y aril-alcoxi C1-8 están cada uno opcionalmente sustituidos en el arilo con 1, 2, 3, 4 o 5 sustituyentes cada uno seleccionado entre ciano, halogeno, hidroxi, alquilo C1-8, alcoxi C1-8, amino, alquilo C1-8-amino, amino- alquilo C1-8, alquilo C1-8-amino-alquilo C1-8 o alcoxicarbonilo C1-8 y donde el heteroarilo y el heteroariloxi está cada uno opcionalmente sustituido en el heteroarilo con 1, 2, 3, 4 o 5 sustituyentes cada uno seleccionado entre alquilo C1-8, amino- alquilo C1-8, alquilo C1-8-amino-alquilo C1-8, carboxi C1-8 o alcoxicarbonilo C1-8.Its synthesis and use to treat, prevent or improve a chronic or acute disease, disorder or alteration mediated by protein kinases. Claim 1: A compound of formula (1) and forms thereof, wherein L is selected from a bond, C1-6 alkyl or halo- C1-6 alkyl; Ar is selected from aryl, heteroaryl, benzofused heterocyclyl or benzofused C3-12 cycloalkyl, where the benzene ring portion of the benzofused ring system is linked to the variable L; RA is selected from C = N-O-R1 or cyano; R 1 is selected from H, C 1-8 alkyl, C 1-8 alkenyl, C 1-8 alkoxy, C 1-8 alkoxy-C 1-8 alkyl, hydroxyC 1-8 alkyl, hydroxyC 1-8 alkoxy, aminoC 1-6 alkyl 8, C1-8-amino-C1-8-alkyl, C1-8-alkoxy-C1-8-alkyl-C1-8-alkyl, C1-8-sulfonyl-C1-8-alkyl, C1-8-sulfonyloxy-alkyl C 1-8 alkyl, aryl, aryl C 1-8 alkyl, aryloxy C 1-8 alkyl, heterocyclyl C 1-8 alkyl, heterocyclyl carbonyl C 1-8 alkyl or heteroaryl C 1-8 alkyl; where aryl-C1-8 alkyl is optionally substituted in the aryl with 1, 2, 3, 4 or 5 substituents each selected from hydroxy, C1-8 alkyl, C1-8 alkoxy, amino, C1-8-amino alkyl or alkoxycarbonyl C1-8, and where hetrocyclyl-C1-8 alkyl is optionally substituted in the heterocyclyl with 1, 2, 3 or 4 substituents each selected from hydroxy, C1-8 alkyl, C1-8 alkoxy, amino, C1-8 alkyl amino or C1-8 alkoxycarbonyl; R2 is selected from H, C1-8 alkyl or C1-8 alkoxy; and R3, R4, R5, R6 and R7 are each selected from H, halogen, hydroxy, C1-8 alkyl, C1-8 alkoxy, C1-8 alkoxy-C1-8 alkyl, hydroxy-C1-8 alkyl, halo- C1-8 alkyl, hydroxy-C1-8 alkoxy, halo-C1-8 alkoxy, amino, C1-8-amino alkyl, amino-C1-8 alkyl, C1-8-amino-C1-8 alkyl, carboxy, acyl C1-8, C1-8 alkoxycarbonyl, C3-12 cycloalkyl, aryl, aryloxy, aryl-C1-8 alkyl, aryl-C1-8 alkoxy, aryl amido, heteroaryl, heteroaryloxy, heteroaryl-C1-8-alkoxy or heterocyclyl, where aryl, aryloxy, aryl-C1-8 alkyl and aryl-C1-8 alkoxy are each optionally substituted in the aryl with 1, 2, 3, 4 or 5 substituents each selected from cyano, halogen, hydroxy, C1- alkyl 8, C 1-8 alkoxy, amino, C 1-8 alkyl, amino C 1-8 alkyl, C 1-8 alkyl-C 1-8 alkyl or C 1-8 alkoxycarbonyl and where the heteroaryl and heteroaryloxy are each optionally substituted in the heteroaryl with 1, 2, 3, 4 or 5 substituents each selected from C 1-8 alkyl, amino-alkyl C1-8 yl, C1-8 alkyl-amino- C1-8 alkyl, C1-8 carboxy or C1-8 alkoxycarbonyl.

ARP060105731A 2005-12-21 2006-12-21 PIRIMIDINE DERIVATIVES AS INHIBITORS OF PIRIMIDIN QUINASA SUBSTITUTES. PROCESSES OF OBTAINING AND PHARMACEUTICAL COMPOSITIONS. AR058624A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US75263305P 2005-12-21 2005-12-21

Publications (1)

Publication Number Publication Date
AR058624A1 true AR058624A1 (en) 2008-02-13

Family

ID=38256842

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060105731A AR058624A1 (en) 2005-12-21 2006-12-21 PIRIMIDINE DERIVATIVES AS INHIBITORS OF PIRIMIDIN QUINASA SUBSTITUTES. PROCESSES OF OBTAINING AND PHARMACEUTICAL COMPOSITIONS.

Country Status (3)

Country Link
AR (1) AR058624A1 (en)
TW (1) TW200800919A (en)
WO (1) WO2007081630A2 (en)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI475996B (en) 2007-10-19 2015-03-11 Celgene Avilomics Res Inc Heteroaryl compounds and uses thereof
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
WO2009055299A1 (en) * 2007-10-23 2009-04-30 Janssen Pharmaceutica N.V. Substituted pyrimidine-5-carboxamide and 5-carboxylic ester kinase inhibitors
WO2012087833A1 (en) 2010-12-22 2012-06-28 Abbott Laboratories Hepatitis c inhibitors and uses thereof
US8951993B2 (en) * 2011-02-24 2015-02-10 Jiangsu Hansoh Pharmaceutical Co., Ltd. Phosphorus containing compounds as protein kinase inhibitors
CA2829755A1 (en) 2011-03-23 2012-09-27 Semorex Technologies Ltd. Treatment of proliferative disorders with a chemiluminescent agent
CN103058935B (en) * 2013-01-15 2015-05-06 四川大学 Pyrimidine compound as well as preparation method and use for same
CN105073728A (en) 2013-03-15 2015-11-18 全球血液疗法股份有限公司 Compounds and uses thereof for the modulation of hemoglobin
AR096654A1 (en) 2013-06-20 2016-01-27 Ab Science DERIVATIVES OF BENZIMIDAZOL AS SELECTIVE INHIBITORS OF PROTEIN QUINASA
EA201992707A1 (en) 2013-11-18 2020-06-30 Глобал Блад Терапьютикс, Инк. COMPOUNDS AND THEIR APPLICATIONS FOR HEMOGLOBIN MODULATION
CN104744446B (en) * 2013-12-30 2019-06-25 广东东阳光药业有限公司 Heteroaryl compound and its application in drug
US9840474B2 (en) 2014-04-24 2017-12-12 Sichuan University Pyrimidine compounds and use as anti-cervical cancer thereof
BR112020021194A2 (en) 2018-04-18 2021-03-23 Constallation Pharmaceuticals, Inc. modulators of methyl modifying enzymes, compositions and uses thereof
CN112262143A (en) 2018-05-21 2021-01-22 星座制药公司 Modulators of methyl-modified enzymes, compositions and uses thereof
WO2021038419A1 (en) * 2019-08-23 2021-03-04 Insilico Medicine Ip Limited Kinase inhibitors and methods of synthesis and treatment
TWI750905B (en) * 2020-11-19 2021-12-21 財團法人國家衛生研究院 Thiazole compounds as protein kinase inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6878714B2 (en) * 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
AU2002319183B2 (en) * 2001-06-01 2007-05-10 F. Hoffmann-La Roche Ag Pyrimidine, triazine and pyrazine derivatives as glutamate receptors
CA2451128A1 (en) * 2001-06-26 2003-01-09 Bristol-Myers Squibb Company N-heterocyclic inhibitors of tnf-alpha expression

Also Published As

Publication number Publication date
WO2007081630A3 (en) 2007-12-21
TW200800919A (en) 2008-01-01
WO2007081630A2 (en) 2007-07-19

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