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AR091093A1 - Tienopirimidinas - Google Patents

Tienopirimidinas

Info

Publication number
AR091093A1
AR091093A1 ARP130101735A AR091093A1 AR 091093 A1 AR091093 A1 AR 091093A1 AR P130101735 A ARP130101735 A AR P130101735A AR 091093 A1 AR091093 A1 AR 091093A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
cycloalkyl
hydrogen atom
compounds
Prior art date
Application number
Other languages
English (en)
Inventor
Dr Kettschau Georg
Dr Phler Florian
Dr Eis Knut
Dr Klar Ulrich
Dr Kosemund Dirk
Dr Slzle Detlev
Dr Lienau Philip
Dra Hgebarth Andrea
Dr Bmer Ulf
Original Assignee
Bayer Pharma Aktiengellschaft
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 Bayer Pharma Aktiengellschaft filed Critical Bayer Pharma Aktiengellschaft
Publication of AR091093A1 publication Critical patent/AR091093A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Compuestos de tienopirimidina sustituidos de la fórmula general (1) que se describen y definen en la presente, métodos de preparación de dichos compuestos, compuestos intermediarios de utilidad para preparar dichos compuestos, composiciones y combinaciones farmacéuticas que comprenden dichos compuestos y el uso de dichos compuestos en la elaboración de una composición farmacéutica para el tratamiento o la profilaxis de una enfermedad, en particular de un trastorno hiperproliferativo y/o de angiogénesis, como agente único o en combinación con otros ingredientes activos. Reivindicación 1: Un compuesto de fórmula general (1) en donde: R¹ representa un grupo seleccionado entre: -C(=O)O-R³, -C(=O)N(H)R³, -C(=O)NR³R⁴; R²ᵃ, R²ᵇ, R²ᶜ, R²ᵈ representan, en forma independiente entre sí, un átomo de hidrógeno o un grupo seleccionado entre: alquilo C₁₋₃, alcoxi C₁₋₃, halo, hidroxi, halo-alquilo C₁₋₃, halo-alcoxi C₁₋₃, ciano, -N(H)R⁵, -NR⁵R⁴; R³ representa un átomo de hidrógeno o un grupo seleccionado entre: alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, -(CH₂)q-(cicloalquilo C₃₋₇), -(CH₂)q-O-(cicloalquilo C₃₋₇), -(CH₂)q-(cicloalquenilo C₄₋₇), -(CH₂)q-O-(cicloalquenilo C₄₋₇), -(CH₂)q-(heterocicloalquilo de entre 3 y 10 miembros), -(CH₂)q-O-(heterocicloalquilo de entre 3 y 10 miembros), -(CH₂)q-(heterocicloalquenilo de entre 4 y 10 miembros), -(CH₂)q-O-(heterocicloalquenilo de entre 4 y 10 miembros), -(CH₂)q-arilo, -(CH₂)q-O-arilo, -(CH₂)q-heteroarilo, -(CH₂)q-O-heteroarilo; donde dicho grupo seleccionado está opcionalmente sustituido; R⁴ representa un grupo seleccionado entre: alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, halo-alquilo C₁₋₆, hidroxi-alquilo C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆; donde dicho grupo seleccionado está opcionalmente sustituido; o NR³R⁴ juntos representan un grupo heterocicloalquilo opcionalmente sustituido de entre 3 y 10 miembros o un heterocicloalquenilo opcionalmente sustituido de entre 4 y 10 miembros; R⁵ representa un átomo de hidrógeno, un grupo alquilo C₁₋₆ o un cicloalquilo C₃₋₇; R⁶ representa un átomo de hidrógeno, un grupo alquilo C₁₋₆ o un cicloalquilo C₃₋₇; R⁷ representa un átomo de hidrógeno, un grupo alquilo C₁₋₆ o un cicloalquilo C₃₋₇; o NR⁶R⁷ juntos representan un grupo heterocicloalquilo de entre 3 y 10 miembros o heterocicloalquenilo de entre 4 y 10 miembros; p representa el entero 1 ó 2; y q representa el entero 0, 1, 2 ó 3; o un tautómero, un N-óxido, un hidrato, un solvato o una sal del mismo, o una mezcla de los mismos.
ARP130101735 2012-05-21 2013-05-20 Tienopirimidinas AR091093A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12168670 2012-05-21
EP13153607 2013-02-01

Publications (1)

Publication Number Publication Date
AR091093A1 true AR091093A1 (es) 2015-01-14

Family

ID=48537948

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130101735 AR091093A1 (es) 2012-05-21 2013-05-20 Tienopirimidinas

Country Status (10)

Country Link
US (1) US9540392B2 (es)
EP (1) EP2852596B1 (es)
JP (1) JP6234444B2 (es)
CN (1) CN104507950B (es)
AR (1) AR091093A1 (es)
CA (1) CA2873975A1 (es)
ES (1) ES2591129T3 (es)
HK (1) HK1206723A1 (es)
UY (1) UY34817A (es)
WO (1) WO2013174744A1 (es)

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TW201412740A (zh) 2012-09-20 2014-04-01 Bayer Pharma AG 經取代之吡咯并嘧啶胺基苯并噻唑酮
CA2899665A1 (en) * 2013-02-01 2014-08-07 Bayer Pharma Aktiengesellschaft Substituted thienopyrimidines and pharmaceutical use thereof
HK1222173A1 (zh) 2013-02-01 2017-06-23 Bayer Pharma Aktiengesellschaft 取代的吡唑并嘧啶基氨基-吲唑类
JP2016512491A (ja) 2013-03-06 2016-04-28 バイエル・ファルマ・アクティエンゲゼルシャフト 置換チアゾロピリミジン類
TW201605867A (zh) * 2013-11-20 2016-02-16 拜耳製藥公司 噻吩并嘧啶
JP6479854B2 (ja) 2014-05-07 2019-03-06 エヴォテック・インターナショナル・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＥｖｏｔｅｃ Ｉｎｔｅｒｎａｔｉｏｎａｌ ＧｍｂＨ 医薬組成物のためのスルホキシイミン置換キナゾリン
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WO2016096721A1 (en) 2014-12-19 2016-06-23 Bayer Pharma Aktiengesellschaft Pyrazolopyridinamines as mknk1 and mknk2 inhibitors
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TW201412740A (zh) 2012-09-20 2014-04-01 Bayer Pharma AG 經取代之吡咯并嘧啶胺基苯并噻唑酮
CN104837841A (zh) 2012-09-26 2015-08-12 拜耳制药股份公司 用于治疗过度增殖性疾病的取代的吲唑-吡咯并嘧啶
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HK1222173A1 (zh) 2013-02-01 2017-06-23 Bayer Pharma Aktiengesellschaft 取代的吡唑并嘧啶基氨基-吲唑类
JP2016512491A (ja) 2013-03-06 2016-04-28 バイエル・ファルマ・アクティエンゲゼルシャフト 置換チアゾロピリミジン類

Also Published As

Publication number Publication date
JP6234444B2 (ja) 2017-11-22
EP2852596B1 (en) 2016-06-22
CN104507950A (zh) 2015-04-08
WO2013174744A1 (en) 2013-11-28
UY34817A (es) 2013-12-31
CA2873975A1 (en) 2013-11-28
US20150133425A1 (en) 2015-05-14
ES2591129T3 (es) 2016-11-25
JP2015517545A (ja) 2015-06-22
US9540392B2 (en) 2017-01-10
HK1206723A1 (en) 2016-01-15
EP2852596A1 (en) 2015-04-01
CN104507950B (zh) 2017-03-22

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