AR107965A2 - PIRIMIDINE DERIVATIVES - Google Patents

PIRIMIDINE DERIVATIVES

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Publication number
AR107965A2
AR107965A2 ARP170100728A ARP170100728A AR107965A2 AR 107965 A2 AR107965 A2 AR 107965A2 AR P170100728 A ARP170100728 A AR P170100728A AR P170100728 A ARP170100728 A AR P170100728A AR 107965 A2 AR107965 A2 AR 107965A2
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AR
Argentina
Prior art keywords
unsubstituted
substituted
alkoxy
alkyl
cycloalkyl
Prior art date
Application number
ARP170100728A
Other languages
Spanish (es)
Original Assignee
Novartis Ag
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR107965A2 publication Critical patent/AR107965A2/en

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Abstract

Reivindicación 1: Un compuesto de formula (1) donde cada uno de R⁰, R¹, R² y R³ es independientemente hidrógeno, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈ cicloalquilo C₃₋₈, cicloalquilo C₃₋₈ alquilo C₁₋₃, aril C₅₋₁₀-alquilo C₁₋₈, hidroxialquilo C₁₋₈, alcoxi C₁₋₈-alquilo C₁₋₈, aminoalquilo C₁₋₈, haloalquilo C₁₋₈, arilo C₅₋₁₀ no sustituido o sustituido, heterociclilo de 5 ó 6 miembros no sustituido o sustituido que comprende 1, 2 ó 3 heteroátomos seleccionados de N, O y S, hidroxi, alcoxi C₁₋₈, hidroxialcoxi C₁₋₈, alcoxi C₁₋₈-alcoxi C₁₋₈, haloalcoxi C₁₋₈, aril C₅₋₁₀-alcoxi C₁₋₆ no sustituido o sustituido, heterocicliloxi no sustituido o sustituido, o heterociclilalcoxi C₁₋₈ no sustituido o sustituido, amino no sustituido o sustituido, alquiltio C₁₋₈, alquilsulfinilo C₁₋₈, alquilsulfonilo C₁₋₈, arilsulfonilo C₅₋₁₀, halógeno, carboxi, alcoxicarbonilo C₁₋₈, carbamoilo no sustituido o sustituido, sulfamoilo no sustituido o sustituido ciano o nitro: o R⁰ y R¹, R¹ y R², y/o R² y R³ forman, junto con los átomos de carbono a los cuales están unidos, un anillo carbocíclico o heterocíclico de 5 ó 6 miembros que comprende 0, 1, 2 ó 3 heteroátomos seleccionados de N, O y S; R⁴ es hidrógeno o alquilo C₁₋₈; cada uno de R⁵ y R⁶ independientemente es hidrógeno, alquilo C₁₋₈, alcoxi C₁₋₈-alquilo C₁₋₈, haloalquilo C₁₋₈, alcoxi C₁₋₈, halógeno, carboxi, alcoxicarbonilo C₁₋₈, carbamoilo no sustituido o sustituido, ciano, o nitro; y cada uno de R⁷, R⁸, R⁹ y R¹⁰ independientemente es alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₈, cicloalquilo C₃₋₈-alquilo C₁₋₆, arilo C₅₋₁₀-alquilo C₁₋₈, hidroxialquilo C₁₋₈, alcoxi C₁₋₈-alquilo C₁₋₈, aminoalquilo C₁₋₈ haloalquilo C₁₋₈ arilo C₅₋₁₀ no sustituido o sustituido, heterociclilo de 5 ó 6 miembros no sustituido o sustituido que comprende 1, 2 ó 3 heteroátomos seleccionados de N, O y S, hidroxi, alcoxi C₁₋₈, hidroxialcoxi C₁₋₈, alcoxi C₁₋₈-alcoxi C₁₋₈, haloalcoxi C₁₋₈, arilo C₅₋₁₀-alcoxi C₁₋₈ no sustituido o sustituido, heterocicliloxi no sustituido o sustituido, o heterociclilalcoxi C₁₋₈ no sustituido o sustituido, amino no sustituido o sustituido, alquiltio C₁₋₈, alquilsulfinilo C₁₋₈, alquilsulfonilo C₁₋₈, arilsulfonilo C₅₋₁₀, halógeno, carboxi, alcoxicarbonilo C₁₋₈, carbamoilo no sustituido o sustituido, sulfamoilo no sustituido o sustituido, ciano o nitro; donde R⁷, R⁸ y R⁹ independientemente entre sí también pueden ser hidrógeno; o R⁷ y R⁸, R⁸ y R⁹ y/o R⁹ y R¹⁰ forman junto con los átomos de carbono a los cuales están unidos, un anillo carbocíclico o heterocíclico de 5 ó 6 miembros que comprende 0, 1, 2 ó 3 heteroátomos seleccionados de N, O y S; A es C o N; y sus sales.Claim 1: A compound of formula (1) wherein each of R⁰, R¹, R² and R³ is independently hydrogen, C₁₋₈ alkyl, C₂₋₈ alkenyl, C₂₋₈ alkynyl C₃₋₈ cycloalkyl, C₃₋₈ cycloalkyl C₁ alkyl ₋₃, C₅₋₁₀-Cil-C alquilo alkyl, C hidro hydroxyalkyl, C₁₋₈ alkoxy-C₁₋₈ alkyl, C₁₋₈ aminoalkyl, C₁₋₈ haloalkyl, unsubstituted or substituted C₅₋₁₀ aryl, 5-heterocyclyl or 6 unsubstituted or substituted members comprising 1, 2 or 3 heteroatoms selected from N, O and S, hydroxy, C₁₋₈ alkoxy, C₁₋₈ hydroxyalkoxy, C₁₋₈ alkoxy-C₁₋₈ alkoxy, C₁₋₈ haloalkoxy, unsubstituted or substituted Cil-C₅₋₁₀-alkoxy, unsubstituted or substituted heterocyclyloxy, or unsubstituted or substituted C o heterocyclylalkoxy, unsubstituted or substituted amino, C₁₋₈ alkylthio, C₁₋₈ alkylsulfinyl, C₁₋₈ alkylsulfonyl , Cils arylsulfonyl , halogen, carboxy, C₁₋₈ alkoxycarbonyl, unsubstituted or substituted carbamoyl, unsubstituted or substituted sulfamoyl cyano or nitro: or R⁰ and R¹, R¹ and R², and / or R² and R³ form, together with the carbon atoms at which are attached, a 5 or 6 membered carbocyclic or heterocyclic ring comprising 0, 1, 2 or 3 heteroatoms selected from N, O and S; R⁴ is hydrogen or C₁₋₈ alkyl; each of R⁵ and R⁶ independently is hydrogen, C₁₋₈ alkyl, C₁₋₈ alkoxy-C alquilo alkyl, C₁₋₈ haloalkyl, C₁₋₈ alkoxy, halogen, carboxy, C₁₋₈ alkoxycarbonyl, unsubstituted or substituted carbamoyl, cyano, or nitro; and each of R⁷, R⁸, R⁹ and R¹⁰ independently is C₁₋₈ alkyl, C₂₋₈ alkenyl, C₂₋₈ alkynyl, C₃₋₈ cycloalkyl, C₃₋₈ cycloalkyl-C₁₋₆ alkyl, C₅₋₁₀ aryl-C alquilo alkyl ₋₈, C₁₋₈ hydroxyalkyl, C₁₋₈ alkoxy-C alco alkyl, C amino aminoalkyl C₁₋₈ haloalkyl unsubstituted or substituted, unsubstituted or substituted 5- or 6-membered heterocyclyl comprising 1, 2 or 3 heteroatoms selected from N, O and S, hydroxy, C₁₋₈ alkoxy, C₁₋₈ hydroxyalkoxy, C₁₋₈-C alco alkoxy, C₁₋₈ haloalkoxy, unsubstituted C₅₋₁₀-C₅₋₁₀ alkoxy or substituted, unsubstituted or substituted heterocyclyloxy, or unsubstituted or substituted Cc heterocyclylalkoxy, unsubstituted or substituted amino, Cilt alkylthio, C₁₋₈ alkylsulfinyl, C₁₋₈ alkylsulfonyl, C₅₋₁₀ arylsulfonyl, halogen, carboxy, C₁ alkoxycarbonyl ₋₈, carbamo unsubstituted or substituted yl, unsubstituted or substituted sulfamoyl, cyano or nitro; where R⁷, R⁸ and R⁹ independently of one another can also be hydrogen; or R⁷ and R⁸, R⁸ and R⁹ and / or R⁹ and R¹⁰ together with the carbon atoms to which they are attached, a 5 or 6 membered carbocyclic or heterocyclic ring comprising 0, 1, 2 or 3 heteroatoms selected from N , O and S; A is C or N; And its salts.

ARP170100728A 2003-08-15 2017-03-23 PIRIMIDINE DERIVATIVES AR107965A2 (en)

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GB0319227A GB0319227D0 (en) 2003-08-15 2003-08-15 Organic compounds

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GB (1) GB0319227D0 (en)

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PT2091918E (en) * 2006-12-08 2014-11-24 Irm Llc Compounds and compositions as protein kinase inhibitors
BRPI1012140A2 (en) * 2009-05-15 2016-05-03 Insight Genetics Inc methods and compositions related to alkaline fusions for cancer diagnosis and treatment
EP2917210B1 (en) * 2012-11-06 2019-02-27 Shanghai Fochon Pharmaceutical Co. Ltd Alk kinase inhibitors
ES2738493T3 (en) * 2013-03-14 2020-01-23 Tolero Pharmaceuticals Inc JAK2 and ALK2 inhibitors and methods for their use
CN104628657A (en) * 2013-11-06 2015-05-20 韩冰 Class of compounds for treating ischemic brain damage and purpose thereof
CN104926794B (en) * 2014-03-17 2017-12-05 广东东阳光药业有限公司 Substituted heteroaryl compound and combinations thereof and purposes
CN106008503B (en) * 2015-03-31 2020-09-01 齐鲁制药有限公司 Spirocyclic aryl sulfones as protein kinase inhibitors
CN106146525B (en) * 2015-04-10 2018-11-02 山东轩竹医药科技有限公司 Three and ring class anaplastic lymphoma kinase inhibitor
CN106187915A (en) * 2015-05-27 2016-12-07 上海翰森生物医药科技有限公司 There is inhibitor of ALK Yu EGFR double activity and its preparation method and application
CN106349224A (en) * 2016-08-03 2017-01-25 山东大学 JAK kinase inhibitor with 4-amino-(1H)-pyrazole structure and preparation method and application thereof
CN110092759A (en) * 2018-01-31 2019-08-06 陆柯潮 The chloro- 2,4- pyrimidine derivatives of 5- as anti-tumor drug
CN114716385B (en) * 2022-04-08 2024-03-12 北京师范大学 Compound of targeted focal adhesion kinase, preparation method and application

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CN1832929B (en) 2012-11-07
GB0319227D0 (en) 2003-09-17
CN1832929A (en) 2006-09-13

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