DK2922848T3 - Oxazolidin-2-on-pyrimidinderivater - Google Patents

Oxazolidin-2-on-pyrimidinderivater Download PDF

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Publication number
DK2922848T3
DK2922848T3 DK13795867.4T DK13795867T DK2922848T3 DK 2922848 T3 DK2922848 T3 DK 2922848T3 DK 13795867 T DK13795867 T DK 13795867T DK 2922848 T3 DK2922848 T3 DK 2922848T3
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Prior art keywords
alkoxy
trifluoromethyl
amino
oxazolidin
compound according
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DK13795867.4T
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English (en)
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DK2922848T5 (da
Inventor
Robin Alec Fairhurst
Pascal Furet
Frank Stephan Dr Kalthoff
Andreas Lerchner
Heinrich Rueeger
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Novartis Ag
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    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Description

Claims (15)

1. Forbindelse af formlen I og/eller et farmaceutisk acceptabelt salt og/eller solvat deraf,
(I) hvor, R1 er methyl, ethyl eller hydroxymethyl; R2 er phenyl, som er usubstitueret eller substitueret i meta- og/eller para-positioner med 1 eller 2 substituenter uafhængigt valgt blandt D, F eller methoxy for metapositionen og blandt D, F, CrCs-alkoxy, hydroxy-C2-C4-alkoxy eller Ci-C2-alkoxy-C2-C4-alkoxy for para-positionen, eller pyridyl, som er usubstitueret eller substitueret i meta- og/eller para-positionerne med 1 eller 2 substituenter uafhængigt valgt blandt D, F eller methoxy for meta-positionen og blandt D, F, C-i-Cs-alkoxy, hydroxy-C2-C4-alkoxy eller Ci-C2-alkoxy-C2-C4-alkoxy for para-positionen, eller en 5-leddet monocyclisk heteroaryl indeholdende 2 til 3 heteroatomer valgt blandt N, O eller S, som er usubstitueret eller substitueret med 1 til 2 substituenter uafhængigt valgt blandt D eller F; og R3 er Fl eller methyl.
2. Forbindelse ifølge krav 1, af formlen Ib
(Ib).
3. Forbindelse ifølge krav 1 eller krav 2, hvor R2 er phenyl, som er usubstitueret eller substitueret i meta- og/eller para-positioner med 1 eller 2 substituenter uafhængigt valgt blandt D, F eller methoxy for metapositionen og blandt D, F, Ci-Cs-alkoxy, hydroxy-C2-C4-alkoxy eller Ci-C2-alkoxy-C2-C4-alkoxy for para-positionen.
4. Forbindelse ifølge krav 1 eller krav 2, hvor R2 er pyridyl, som er usubstitueret eller substitueret i meta- og/eller para-positioner med 1 eller 2 substituenter uafhængigt valgt blandt D, F eller methoxy for metapositionen og blandt D, F, C-i-Cs-alkoxy, hydroxy-C2-C4-alkoxy eller CrC2-alkoxy-C2-C4-alkoxy for para-positionen.
5. Forbindelse ifølge krav 1 eller krav 2, hvor R2 er en 5-leddet monocyclisk heteroaryl, som indeholder 2 til 3 heteroatomer valgt blandt N, O eller S, som er usubstitueret eller substitueret med 1 til 2 substituenter uafhængigt valgt blandt D eller F.
6. Forbindelse ifølge ethvert af kravene 1 til 5, hvor R1 er methyl.
7. Forbindelse ifølge ethvert af kravene 1 til 5, hvor R1 er ethyl.
8. Forbindelse ifølge ethvert af kravene 1 til 5, hvor R1 er hydroxymethyl.
9. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge krav 1, valgt blandt (4S,5R)-3-(2,-amino-2-morpholin-4-yl-4,-trifluormethyl-[4,5,]bipyrimidinyl-6-yl)-4-methyl- 5-thiazol-2-yl-oxazolidin-2-on, (4S*,5S*)-3-(2,-amino-2-morpholino-4,-(trifluormethyl)-[4,5,-bipyrimidin]-6-yl)-4-ethyl-5- (4-methoxyphenyl)oxazolidin-2-on, (45.55) -3-(2,-amino-2-morpholino-4'-(trifluormethyl)-[4,5,-bipyrimidin]-6-yl)-4-(hydroxymethyl)-5-(4-methoxyphenyl)oxazolidin-2-on, (4S*,5R*)-3-(2'-amino-2-morpholino-4,-(trifluormethyl)-[4,5,-bipyrimidin]-6-yl)-4-ethyl-5- phenyloxazolidin-2-on, (45.55) -3-(2,-amino-2-morpholino-4'-(trifluormethyl)-[4,5,-bipyrimidin]-6-yl)-4-methyl-5-phenyloxazolidin-2-on, (4R*,5R*)-3-(2,-amino-2-morpholino-4,-(trifluormethyl)-[4,5'-bipyrimidin]-6-yl)-4-ethyl-5- (3-methoxyphenyl)oxazolidin-2-on, (4S,5R)-3-(2'-amino-2-morpholino-4,-(trifluormethyl)-[4,5'-bipyrimidin]-6-yl)-4-ethyl-5- (thiazol-2-yl)oxazolidin-2-on, 3-(2,-amino-2-morpholin-4-yl-4,-trifluormethyl-[4,5']bipyrimidinyl-6-yl)-4-ethyl-5-pyridin-3-yl-oxazol id i n-2-on, 3-(2'-amino-2-morpholin-4-yl-4'-trifluormethyl-[4,5,]bipyrimidinyl-6-yl)-4-methyl-5-pyrid in-3-yl-oxazolid in-2-on, (45.55) -3-(2'-amino-2-morpholin-4-yl-4'-trifluormethyl-[4,5']bipyrimidinyl-6-yl)-4-hydroxymethyl-5-phenyl-oxazolidin-2-on, (45.55) -3-(2'-amino-2-morpholin-4-yl-4'-trifluormethyl-[4,5']bipyrimidinyl-6-yl)-4-methyl-5-thiazol-2-yl-oxazolidin-2-on, (45.55) -3-(2'-amino-2-morpholino-4'-(trifluormethyl)-[4,5'-bipyrimidin]-6-yl)-4-(hydroxymethyl)-5-(4-(2-methoxyethoxy)phenyl)oxazolidin-2-on, (45.55) -3-(2'-amino-2-morpholino-4'-(trifluormethyl)-[4,5'-bipyrimidin]-6-yl)-5-(4-(2-hydroxyethoxy)phenyl)-4-(hydroxymethyl)oxazolidin-2-on eller (45.55) -3-(2'-amino-2-morpholino-4'-(trifluormethyl)-[4,5'-bipyrimidin]-6-yl)-4-(hydroxymethyl)-5-(4-(3-hydroxypropoxy)phenyl)oxazolidin-2-on.
10. Forbindelse, eller et farmaceutisk acceptabelt salt deraf, ifølge krav 1, som er (4S,5R)-3-(2'-amino-2-morpholin-4-yl-4'-trifluormethyl-[4,5,]bipyrimidinyl-6-yl)-4-methyl-5-thiazol-2-yl-oxazolidin-2-on.
11. Farmaceutisk sammensætning omfattende en terapeutisk effektiv mængde af en forbindelse ifølge ethvert af kravene 1 til 10 eller et farmaceutisk acceptabelt salt deraf, og ét eller flere farmaceutisk acceptable bærestoffer.
12. Kombination omfattende en terapeutisk effektiv mængde af en forbindelse ifølge ethvert af kravene 1 til 10 eller et farmaceutisk acceptabelt salt deraf, og ét eller flere terapeutisk aktive co-agenser.
13. Forbindelse ifølge ethvert af kravene 1 til 10 eller et farmaceutisk acceptabelt salt deraf, til anvendelse som et lægemiddel.
14. Forbindelse ifølge ethvert af kravene 1 til 10 eller et farmaceutisk acceptabelt salt deraf, til anvendelse ved behandlingen af ikke-melanom hudcancer eller præ-maligne stadier af ikke-melanom hudcancer.
15. Forbindelse til anvendelse ifølge krav 14, hvor den ikke-melanome hudcancer er pladeepithelcarcinom og det præ-maligne stadie af ikke-melanom hudcancer er aktinisk keratose.
DK13795867.4T 2012-11-12 2013-11-11 Oxazolidin-2-on-pyrimidinderivater DK2922848T5 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261725113P 2012-11-12 2012-11-12
PCT/IB2013/060052 WO2014072956A1 (en) 2012-11-12 2013-11-11 Oxazolidin-2-one-pyrimidine derivatives

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DK2922848T5 DK2922848T5 (da) 2017-10-30

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MX355945B (es) 2013-03-14 2018-05-07 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante.
EP3352755A4 (en) * 2015-09-24 2019-04-03 Drexel University Novel Compositions and Methods for the Treatment and Prevention of Skin Diseases
BR112018073549A8 (pt) 2016-05-18 2023-01-10 Univ Pennsylvania Uso de inibidores seletivos e específicos de mtor e/ou de inibidores duplos de pi3k/mtor, e composição farmacêutica
TW201929861A (zh) 2017-11-06 2019-08-01 瑞士商諾華公司 包含㗁唑啶-2-酮-嘧啶衍生物之調配物
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