DK2619182T3 - Farmaceutisk sammensætning - Google Patents

Farmaceutisk sammensætning Download PDF

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Publication number
DK2619182T3
DK2619182T3 DK11760631.9T DK11760631T DK2619182T3 DK 2619182 T3 DK2619182 T3 DK 2619182T3 DK 11760631 T DK11760631 T DK 11760631T DK 2619182 T3 DK2619182 T3 DK 2619182T3
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methyl
hydrogen
compound
pharmaceutically acceptable
cancer
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DK11760631.9T
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English (en)
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Mark Spyvee
Takashi Satoh
Jonathan Eric Carlson
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Eisai R&D Man Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18One oxygen or sulfur atom
    • C07D231/20One oxygen atom attached in position 3 or 5
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18One oxygen or sulfur atom
    • C07D231/20One oxygen atom attached in position 3 or 5
    • C07D231/22One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41521,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (20)

1. Forbindelse med formel I:
hvor: den ene af Rid og Rib er hydrogen, og den anden er methyl; eller Ria og Rib sammen danner en cyclopropylring; R2 er methyl eller fluormethyl; Rs er methyl; R4 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; Rs er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; R6 er hydrogen, halogen, methyl eller methoxy; R7 er hydrogen, halogen, methyl eller methoxy; og X er oxygen; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, hvor den ene af Ri£ og Rib er hydrogen, og den anden er methyl; R2 er methyl, difluormethyl eller trifluormethyl; R3 er methyl; R4 er chlor, fluor, trifluormethyl, difluormethyl, methyl, methoxy, difluormethoxy eller trifluormethoxy; Rs er hydrogen, chlor, fluor, methyl eller methoxy; Re og R7 er hydrogen; eller et farmaceutisk acceptabelt salt deraf.
3. Forbindelse ifølge krav 2, hvor Rs er hydrogen; eller et farmaceutisk acceptabelt salt deraf.
4. Forbindelse ifølge krav 3, hvor R4 er udvalgt blandt chlor, trifluormethyl, difluormethyl, difluormethoxy og trifluormethoxy; eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse ifølge et hvilket som helst af kravene 1-4, hvor den ene af Ria og Rib er hydrogen, og den anden er methyl, og forbindelsen med formel I består af en blanding af stereoisomerer; eller et farmaceutisk acceptabelt salt deraf.
6. Forbindelse ifølge et hvilket som helst af kravene 1-4, hvor den ene af Ria og Rib er hydrogen, og den anden er methyl, og forbindelsen med formel I består af en i det væsentlige ren stereoisomer; eller et farmaceutisk acceptabelt salt deraf.
7. Forbindelse ifølge krav 6, hvor den ene af Ria og Rib er hydrogen, og den anden er methyl, og carbonatomet i forbindelsen med formel I markeret med en * har i det væsentlige S-konfigurationen; eller et farmaceutisk acceptabelt salt deraf.
8. Forbindelse ifølge krav 6, hvor den ene af Ria og Rib er hydrogen, og den anden er methyl, og carbonatomet i forbindelsen med formel I markeret med en * har i det væsentlige R-konfigurationen; eller et farmaceutisk acceptabelt salt deraf.
9. Forbindelse ifølge krav 1, hvor Ria og Rib sammen danner en cyclopropylring; R2 er methyl, trifluormethyl eller difluormethyl; R.3 er methyl; R4 er trifluormethyl, difluormethyl, chlor eller fluor; Re og R7 er hydrogen; eller et farmaceutisk acceptabelt salt deraf.
10. Forbindelse ifølge krav 1 udvalgt fra gruppen, der består af:
og farmaceutisk acceptable salte deraf.
11. Forbindelse ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf.
12. Forbindelse ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf.
13. Farmaceutical sammensætning, der omfatter: (a) en forbindelse med formel I:
hvor: den ene af Ri^ og Rib er hydrogen, og den anden er methyl; eller Ria og Rib sammen danner en cyclopropylring; R2 er methyl eller fluormethyl; R3 er methyl; R4 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; Rs er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; Re er hydrogen, halogen, methyl eller methoxy; R7 er hydrogen, halogen, methyl eller methoxy; og X er oxygen; eller et farmaceutisk acceptabelt salt deraf; og et farmaceutisk acceptabelt bæremateriale eller (b) en forbindelse ifølge krav 10 eller et farmaceutisk acceptabelt salt deraf; og et farmaceutisk acceptabelt bæremateriale eller (c) forbindelsen, som er:
eller et farmaceutisk acceptabelt salt deraf; og et farmaceutisk acceptabelt bæremateriale.
14. Farmaceutisk sammensætning, der omfatter forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf; og et farmaceutisk acceptabelt bæremateriale.
15. Farmaceutisk sammensætning, der omfatter: (a) en forbindelse med formel I:
hvor: den ene af Ria og Rib er hydrogen, og den anden er methyl; eller Ria og Rib sammen danner en cyclopropylring; R2 er methyl eller fluormethyl; Ra er methyl; R4 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; R5 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; Re er hydrogen, halogen, methyl eller methoxy; R7 er hydrogen, halogen, methyl eller methoxy; og X er oxygen; eller et farmaceutisk acceptabelt salt deraf eller (b) en forbindelse ifølge krav 10; eller et farmaceutisk acceptabelt salt deraf eller (c) forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf eller (d) forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf, til anvendelse til behandling af multipel sklerose hos et pattedyr.
16. Farmaceutisk sammensætning, der omfatter: (a) en forbindelse med formel I:
hvor: den ene af Ria og Rib er hydrogen, og den anden er methyl; eller Ria og Rib sammen danner en cyclopropylring; R2 er methyl eller fluormethyl; R3 er methyl; R4 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; R5 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; Re er hydrogen, halogen, methyl eller methoxy; R7 er hydrogen, halogen, methyl eller methoxy; og X er oxygen; eller farmaceutisk acceptable salte deraf eller (b) en forbindelse ifølge krav 10; eller et farmaceutisk acceptabelt salt deraf eller (c) forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf eller (d) forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf, til anvendelse til behandling af rheumatoid arthritis hos et pattedyr.
17. Farmaceutisk sammensætning, der omfatter: (a) en forbindelse med formel I:
hvor: den ene af Ri£ og Rib er hydrogen, og den anden er methyl; eller Ria og Rib sammen danner en cyclopropylring; R2 er methyl eller fluormethyl; R3 er methyl; R4 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; R5 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; R.6 er hydrogen, halogen, methyl eller methoxy; R7 er hydrogen, halogen, methyl eller methoxy; og X er oxygen; eller farmaceutisk acceptable salte deraf eller (b) en forbindelse ifølge krav 10; eller et farmaceutisk acceptabelt salt deraf, til anvendelse til behandling af cancer hos et pattedyr, hvor canceren eventuelt er udvalgt fra gruppen, der består af hudcancer, brystcancer, colorektal cancer, prostatacancer, nyrecancer, ovariecancer, cervixcancer, endometriumcancer, glioblastom, lungecancer, hoved- og halscancer, medulloblastom og urinvejscancer.
18. Farmaceutisk sammensætning, der omfatter forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf, til anvendelse til behandling af cancer hos et pattedyr.
19. Farmaceutisk sammensætning ifølge krav 18, hvor canceren er udvalgt fra gruppen, der består af hudcancer, brystcancer, colorektal cancer, prostatacancer, nyrecancer, ovariecancer, cervixcancer, endometriumcancer, glioblastom, lungecancer, hoved- og halscancer, medulloblastom og urinvejscancer.
20. Farmaceutisk sammensætning, der omfatter forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf, til anvendelse til behandling af cancer hos et pattedyr, hvor canceren eventuelt er udvalgt fra gruppen, der består af hudcancer, brystcancer, colorektal cancer, prostatacancer, nyrecancer, ovariecancer, cervixcancer, endometriumcancer, glioblastom, lungecancer, hoved- og halscancer, medulloblastom og urinvejscancer.
DK11760631.9T 2010-09-21 2011-09-12 Farmaceutisk sammensætning DK2619182T3 (da)

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Application Number Priority Date Filing Date Title
US38478110P 2010-09-21 2010-09-21
PCT/US2011/051163 WO2012039972A1 (en) 2010-09-21 2011-09-12 Pharmaceutical composition

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US (2) US8686018B2 (da)
EP (2) EP2619182B1 (da)
JP (1) JP5956448B2 (da)
KR (1) KR101911105B1 (da)
CN (1) CN103097358B (da)
AU (1) AU2011305872B2 (da)
BR (1) BR112013002484B1 (da)
CA (1) CA2806121C (da)
CL (1) CL2013000675A1 (da)
CY (1) CY1118680T1 (da)
DK (1) DK2619182T3 (da)
ES (1) ES2610185T3 (da)
HR (1) HRP20170042T1 (da)
HU (1) HUE031408T2 (da)
IL (1) IL224288A (da)
LT (1) LT2619182T (da)
ME (1) ME02575B (da)
MX (1) MX2013003162A (da)
MY (1) MY162146A (da)
NZ (1) NZ606629A (da)
PE (1) PE20131343A1 (da)
PL (1) PL2619182T3 (da)
PT (1) PT2619182T (da)
RS (1) RS55566B1 (da)
RU (1) RU2606510C2 (da)
SG (1) SG188188A1 (da)
SI (1) SI2619182T1 (da)
SM (1) SMT201700008B (da)
UA (1) UA113499C2 (da)
WO (1) WO2012039972A1 (da)

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US20140155452A1 (en) 2014-06-05
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JP5956448B2 (ja) 2016-07-27
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EP2619182B1 (en) 2016-11-09
RU2013118209A (ru) 2014-10-27
BR112013002484A2 (pt) 2016-05-31
EP2619182A1 (en) 2013-07-31
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