HRP20141034T1 - Spojevi koji sadrže (s)-2-amino-1-(4-klorofenil)-1-[4-(1h-pirazol-4-il)-fenil]-etanol kao modulator proteinskih kinaza - Google Patents

Spojevi koji sadrže (s)-2-amino-1-(4-klorofenil)-1-[4-(1h-pirazol-4-il)-fenil]-etanol kao modulator proteinskih kinaza Download PDF

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Publication number
HRP20141034T1
HRP20141034T1 HRP20141034AT HRP20141034T HRP20141034T1 HR P20141034 T1 HRP20141034 T1 HR P20141034T1 HR P20141034A T HRP20141034A T HR P20141034AT HR P20141034 T HRP20141034 T HR P20141034T HR P20141034 T1 HRP20141034 T1 HR P20141034T1
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Prior art keywords
compound
carcinoma
compound according
phenyl
preparation
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HRP20141034AT
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English (en)
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Steven John Woodhead
Davis Charles Rees
Martyn Frederickson
Kyla Merriom Grimshaw
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Astex Therapeutics Limited
The Institute Of Cancer Research : The Royal Cancer Hospital
Cancer Research Technology Limited
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Application filed by Astex Therapeutics Limited, The Institute Of Cancer Research : The Royal Cancer Hospital, Cancer Research Technology Limited filed Critical Astex Therapeutics Limited
Publication of HRP20141034T1 publication Critical patent/HRP20141034T1/hr

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    • 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
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/22Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
    • C07C215/28Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
    • C07C215/30Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
    • C07C215/32Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton containing hydroxy groups and carbon atoms of two six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C247/00Compounds containing azido groups
    • C07C247/02Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C247/08Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being unsaturated
    • C07C247/10Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being unsaturated and containing rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • 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
    • C07D231/12Heterocyclic 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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
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  • Hospice & Palliative Care (AREA)
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  • Psychiatry (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Claims (13)

1. Pripravak koji sadrži 2-amino-1-(4-klorlo-fenil)-1-[4-(1H-pirazol-4-il)-fenil]-etanol ili neku njegovu sol, solvat, tautomer ili N-oksid, od kojih je najmanje 90% u obliku S-enantiomera.
2. Pripravak prema zahtjevu 1 naznačen time da je najmanje 98% u obliku S-enantiomera.
3. Pripravak prema zahtjevu 1 naznačen time da je najmanje 99% u obliku S-enantiomera.
4. Pripravak prema bilo kojem od prethodnih zahtjeva naznačen time da je (S)-2-amino-1-(4-klorlo-fenil)-1-[4-(1Hpirazol-4-il)-fenil]-etanol u obliku aditivne soli neke slobodne baze ili kiseline.
5. Spoj čija je formula (I): [image] ili neka njegova sol, solvat, tautomer ili N-oksid, naznačen time da taj spoj ima enantiomernu čistoću od najmanje 90%.
6. Spoj prema zahtjevu 5, naznačen time da taj spoj ima enantiomernu čistoću od najmanje 98%.
7. Spoj prema zahtjevu 5, naznačen time da taj spoj ima enantiomernu čistoću od najmanje 99%.
8. Spoj formule (I) prema bilo kojem od zahtjeva 5 do 7, u obliku neke slobodne baze ili njene soli, solvata ili tautomera.
9. Spoj prema bilo kojem od zahtjeva 5 do 8 koji je di-sol oblikovana s klorovodičnom kiselinom.
10. Farmaceutski pripravak koji sadrži spoj prema bilo kojem od zahtjeva 1 do 4 ili spoj prema bilo kojem od zahtjeva 5 do 9 i neki farmaceutski prihvatljiv nosač.
11. Pripravak prema bilo kojem od zahtjeva 1 do 4 ili spoj prema bilo kojem od zahtjeva 5 do 9 za primjenu u medicini.
12. Pripravak prema bilo kojem od zahtjeva 1 do 4 ili spoj prema bilo kojem od zahtjeva 5 do 9, za primjenu u profilaksi ili liječenju nekog bolesnog stanja ili bolesti iz skupine u koju spadaju karcinom mokraćnog mjehura, dojke, debelog crijeva, bubrega, epidermalni karcinom, karcinom jetre, pluća, jednjaka, žučnog mjehura, jajnika, gušterače, želuca, grlića maternice, sluznice maternice, štitnjače, prostate ili kože, hematopoetski tumor limfoidnog podrijetla, hematopoetski tumor mijeloidnog podrijetla, folikularni karcinom štitnjače, tumor mezenhimalnog podrijetla, tumor središnjeg ili perifernog živčanog sustava, melanom, seminom, teratokarcinom, osteosarkom, kseroderma pigmentosum, keratoktantom, folikularni karcinom štitnjače ili Kaposijev sarkom, karcinom dojke, karconom jajnika, karcinom debelog crijeva, karcinom jednjaka, karcinom skvamoznih stanica i nesitnostanični karcinomi pluća.
13. Uporaba pripravka prema bilo kojem od zahtjeva 1 do 4 ili spoja prema bilo kojem od zahtjeva 5 do 9 za proizvodnju nekog lijeka za profilaksu ili liječenje bilo kojeg od bolesnih stanja ili bolesti navedenih u zahtjevu 12.
HRP20141034AT 2007-03-14 2014-10-27 Spojevi koji sadrže (s)-2-amino-1-(4-klorofenil)-1-[4-(1h-pirazol-4-il)-fenil]-etanol kao modulator proteinskih kinaza HRP20141034T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US89475207P 2007-03-14 2007-03-14
GBGB0704932.3A GB0704932D0 (en) 2007-03-14 2007-03-14 Pharmaceutical compounds
PCT/GB2008/050180 WO2008110846A2 (en) 2007-03-14 2008-03-14 Compositions comprising (s)-2-amino-1-(4-chlorophenyl)-1-[4-(1h-pyrazol-4-yl)-phenyl]-ethanol as modulator of protein kinases

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HRP20141034T1 true HRP20141034T1 (hr) 2014-12-19

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US (2) US20100113551A1 (hr)
EP (2) EP2134339B1 (hr)
JP (2) JP2010521446A (hr)
KR (1) KR20100014720A (hr)
CN (1) CN101686965B (hr)
AU (1) AU2008224657B2 (hr)
BR (1) BRPI0808802A2 (hr)
CA (1) CA2679878A1 (hr)
CY (1) CY1115877T1 (hr)
DK (1) DK2134339T3 (hr)
ES (1) ES2511817T3 (hr)
GB (1) GB0704932D0 (hr)
HK (1) HK1133828A1 (hr)
HR (1) HRP20141034T1 (hr)
IL (1) IL200822A (hr)
MX (1) MX2009009874A (hr)
NZ (1) NZ579341A (hr)
PL (1) PL2134339T3 (hr)
PT (1) PT2134339E (hr)
RS (1) RS53580B1 (hr)
RU (1) RU2527151C2 (hr)
SI (1) SI2134339T1 (hr)
WO (1) WO2008110846A2 (hr)
ZA (1) ZA200906303B (hr)

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