AR092365A1 - Derivados de piridopirimidina - Google Patents

Derivados de piridopirimidina

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Publication number
AR092365A1
AR092365A1 ARP130102804A ARP130102804A AR092365A1 AR 092365 A1 AR092365 A1 AR 092365A1 AR P130102804 A ARP130102804 A AR P130102804A AR P130102804 A ARP130102804 A AR P130102804A AR 092365 A1 AR092365 A1 AR 092365A1
Authority
AR
Argentina
Prior art keywords
denotes
dihydro
atoms
mono
oxazinyl
Prior art date
Application number
ARP130102804A
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English (en)
Inventor
Dr Burgdorf Lars
Dr Kuhn Daniel
Dra Ross Tatjana
Dr Deutsch Carl
Original Assignee
Merck Patent Ges Mit Beschränkter Haftung
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Application filed by Merck Patent Ges Mit Beschränkter Haftung filed Critical Merck Patent Ges Mit Beschränkter Haftung
Publication of AR092365A1 publication Critical patent/AR092365A1/es

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    • 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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Abstract

Son inhibidores de Syk (tirosina quinasa del bazo) y se pueden emplear, inter alia, para el tratamiento de cáncer, artritis reumatoidea y/o lupus sistémico. Reivindicación 1: Compuestos de la fórmula (1) en donde R denota H, OH, A o NR⁴R⁴; R¹ denota Ar¹, Het¹, CN, A o -CºC-Ar¹; R² denota Het², NR³Cyc, NR³CR³CON(R³)₂, NR³[C(R³)₂]ₚCR³(NH₂)CH₂OA o NR³[C(R³)₂]ₚN(R³)₂; Ar¹ denota fenilo, que está mono-, di- o trisustituido con A, (CH₂)ₙHet³, [C(R³)₂]ₙOR³, [C(R³)₂]ₙN(R³)₂, NO₂, CN, Hal, COOR³, CON(R³)₂, NR³COA, NR³SO₂A, SO₂N(R³)₂ y/O S(O)ₘA; Het¹ denota 3,6-dihidro-2H-piranilo, tetrahidropiridinilo, 1,3-dihidro-bencimidazolilo, pirazolilo, cromanilo, 1,2,3,4-tetrahidro-pirazolo[1,5-a]piridinilo, 6,7-dihidro-4H-pirazolo[5,1-c][1,4]-oxazinilo, 1,4-dihidro-benzo[d][1,3]oxazinilo, 4H-benzo[1,4]oxazinilo, bencimidazolilo, piridilo, pirimidinilo, imidazolilo, pirazolito, furilo, tiazolilo, triazolilo, benzotriazolilo, indolilo, indazolilo, 1,3- ó 2,3-dihidro-indolilo, cada uno de los cuales puede no estar sustituido o puede estar mono-, di-, tri- o tetrasustituido con A, CN, OH, OA, Hal, SO₂NH₂, (CH₂)ₙNH₂, (CH₂)ₙNHA, (CH₂)ₙNA₂ y/u =O; Het² denota piperidinilo, piperazinilo, pirrolidinilo, morfolinilo, tetrahidropiranilo, pirazolilo, indazolilo, azetidinilo u octahidro-bencimidazolilo, cada uno de los cuales está mono-, di- o trisustituido con Hal, A, (CH₂)ₙNH₂, (CH₂)ₙNHA, (CH₂)ₙNA₂, (CH₂)ₙOH y/o (CH₂)ₙOA; Het³ denota piperidinilo, piperazinilo, pirrolidinilo, morfolinilo, imidazolidinilo, piridilo, pirimidinilo, imidazolilo, pirazolilo, furilo, tiazolilo o triazolilo, cada uno de los cuales no está sustituido o está mono- o disustituido con A y/u =O; R³ denota H o alquilo que tiene 1, 2, 3 ó 4 átomos de C; R⁴, R⁴ denotan cada uno, de modo independiente entre sí, H o A; A denota alquilo no ramificado o ramificado que tiene 1 - 10 átomos de C, en donde 1 - 7 átomos de H pueden estar reemplazados por F y/o en donde uno o dos grupos CH₂ no adyacentes pueden estar reemplazados por O y/o NH, o alquilo cíclico que tiene 3 - 7 átomos de C; Cyc denota alquilo cíclico que tiene 3 - 7 átomos de C, que puede no estar sustituido o que puede estar monosustituido con NH₂, CN, CONH₂ u OH; m denota 0, 1 ó 2; n denota 0, 1, 2, 3 ó 4; p denota 1, 2, 3 ó 4; y sus solvatos, sales, enantiómeros, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP130102804A 2012-08-07 2013-08-07 Derivados de piridopirimidina AR092365A1 (es)

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EP12005716 2012-08-07

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AR092365A1 true AR092365A1 (es) 2015-04-15

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US (1) US9725462B2 (es)
EP (1) EP2882746B1 (es)
JP (2) JP6374384B2 (es)
CN (1) CN104507942B (es)
AR (1) AR092365A1 (es)
AU (1) AU2013301865B2 (es)
CA (1) CA2881279C (es)
ES (1) ES2618004T3 (es)
IL (1) IL237073A (es)
WO (1) WO2014023385A1 (es)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2817308B1 (en) * 2012-02-23 2016-09-07 AbbVie Inc. Pyridopyrimidinone inhibitors of kinases
ES2618004T3 (es) * 2012-08-07 2017-06-20 Merck Patent Gmbh Derivados de piridopirimidina como inhibidores de proteínas quinasas
KR20140027714A (ko) * 2012-08-27 2014-03-07 주식회사 홍인터내셔날 외부 디바이스와 연동하는 다트 게임 장치
CN106366093B (zh) 2015-07-21 2020-08-18 广州再极医药科技有限公司 稠环嘧啶类化合物、中间体、其制备方法、组合物和应用
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