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HRP20110768T1 - Pirazolopirimidinonski inhibitor kinaze - Google Patents

Pirazolopirimidinonski inhibitor kinaze Download PDF

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Publication number
HRP20110768T1
HRP20110768T1 HR20110768T HRP20110768T HRP20110768T1 HR P20110768 T1 HRP20110768 T1 HR P20110768T1 HR 20110768 T HR20110768 T HR 20110768T HR P20110768 T HRP20110768 T HR P20110768T HR P20110768 T1 HRP20110768 T1 HR P20110768T1
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Croatia
Prior art keywords
compound
individual
pharmaceutically acceptable
active substance
acceptable salt
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Application number
HR20110768T
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English (en)
Inventor
F. Kluge Arthur
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Agennix Ag
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Publication date
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Publication of HRP20110768T1 publication Critical patent/HRP20110768T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28Oxygen atom
    • C07D473/30Oxygen atom attached in position 6, e.g. hypoxanthine

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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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Spoj koji je (i) spoj formule (I),ili (ii) tautomer spoja pod (i). Patent sadrži još 16 patentnih zahtjeva.

Claims (17)

1. Spoj koji je (i) spoj formule (I), [image] ili (ii) tautomer spoja pod (i).
2. Farmaceutski prihvatljiva sol spoja prema zahtjevu 1, posebno klorovodična sol ili maleat spoja prema zahtjevu 1.
3. Prolijek spoja prema zahtjevu 1, ili farmaceutski prihvatljiva sol prema zahtjevu 2, pri čemu je prolijek (i) acetatni, formijatni ili benzoatni derivat fenolne hidroksilne skupine, ili (ii) N-aciloksialkil piridinij derivat.
4. Farmaceutska smjesa koja sadrži (i) djelatnu tvar koja se izabire između: spoja prema zahtjevu 1, farmaceutski prihvatljive soli prema zahtjevu 2, i prolijeka prema zahtjevu 3; i (ii) farmaceutski prihvatljivo punilo, pomoćnu tvar ili nosač.
5. Farmaceutska smjesa prema zahtjevu 4, koja je oblikovana (i) za oralnu primjenu ili (ii) za intravensku primjenu.
6. Farmaceutska smjesa prema zahtjevu 4 ili 5, koja sadrži terapijski učinkovitu količinu spomenute djelatne tvari.
7. Farmaceutska smjesa prema zahtjevu 6, oblikovana za primjenu pojedincu kojemu je potrebna, posebno kada se radi o primjeni pojedincu koji boluje od raka.
8. Farmaceutska smjesa prema zahtjevu 7, pri čemu je spomenuti pojedinac čovjek.
9. (a) Djelatna tvar izabrana između: spoja prema zahtjevu 1, farmaceutski prihvatljive soli prema zahtjevu 2, i prolijeka prema zahtjevu 3; ili (b) farmaceutska smjesa prema bilo kojem od zahtjeva 4 do 8, za uporabu u liječenju pojedinca koji boluje od raka, posebno kada je taj pojedinac sisavac izabran iz grupe koja obuhvaća: domaće životinje, glodavce i ljude, posebno kada je taj pojedinac čovjek.
10. Postupak ubijanja ili inhibicije proliferacije ili rasta tumorskih stanica, koji obuhvaća dovođenje u doticaj tumorske stanice sa spojem prema zahtjevu 1 ili njegovim oblikom soli, pri čemu se in vitro ta tumorska stanica izlaže spoju ili njegovoj soli, posebno kada je tumorska stanica maligna stanica pojedinca.
11. Postupak prema zahtjevu 10, pri čemu je pojedinac sisavac izabran iz grupe koja obuhvaća: domaće životinje, glodavce i ljude, posebno kada je taj pojedinac čovjek.
12. (a) Djelatna tvar izabrana između: spoja prema zahtjevu 1, farmaceutski prihvatljive soli prema zahtjevu 2, i prolijeka prema zahtjevu 3; ili (b) farmaceutska smjesa prema bilo kojem od zahtjeva 4 do 8, za uporabu u liječenju pojedinca koji boluje od poremećaja ili bolesti povezanih s aktivnošću jedne ili više ciklin ovisnih kinaza izabranih između: CDK1, CDK2, CDK4, CDK7 i CDK9, posebno kada je poremećaj ili bolest rak.
13. Djelatna tvar ili farmaceutska smjesa prema zahtjevu 12, pri čemu je poremećaj ili bolest povezana s aktivnošću CDK9.
14. Djelatna tvar ili farmaceutska smjesa prema zahtjevu 12 ili 13, pri čemu je pojedinac sisavac izabran iz grupe koja obuhvaća: domaće životinje, glodavce i ljude, posebno kada je taj pojedinac čovjek.
15. Uporaba djelatne tvari izabrane između: spoja prema zahtjevu 1, farmaceutski prihvatljive soli prema zahtjevu 2, i prolijeka prema zahtjevu 3; za pripremu lijeka za liječenje pojedinca koji boluje od raka.
16. Postupak sinteze spoja prema zahtjevu 1, ili po izboru njegove soli, koji obuhvaća korak reakcije spoja čija je struktura predstavljena formulom (II) sa spojem čija je struktura predstavljena formulom (III), [image] pri čemu se X bira između -O-alkil, -O-alkenil, -O-alkinil, -O-acil i halogena, posebno X je -OEt; i, po izboru, reakciju tako dobivenog spoja s kiselinom kako bi se dobila sol te kiseline.
17. Postupak sinteze farmaceutski prihvatljive soli prema 2, koji obuhvaća korak reakcije spoja prema zahtjevu 1 s kiselinom, posebno kada je kiselina klorovodična ili maleinska kiselina.
HR20110768T 2007-05-29 2011-10-24 Pirazolopirimidinonski inhibitor kinaze HRP20110768T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US93215507P 2007-05-29 2007-05-29
EP07113226A EP2019101A1 (en) 2007-07-26 2007-07-26 Pyrazol[3,4-d]pyrimidin-4-one useful as Kinase Inhibitor
PCT/EP2008/056569 WO2008145678A1 (en) 2007-05-29 2008-05-28 Pyrazolopyrimidinone kinase inhibitor

Publications (1)

Publication Number Publication Date
HRP20110768T1 true HRP20110768T1 (hr) 2011-11-30

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Application Number Title Priority Date Filing Date
HR20110768T HRP20110768T1 (hr) 2007-05-29 2011-10-24 Pirazolopirimidinonski inhibitor kinaze

Country Status (19)

Country Link
US (2) US8304418B2 (hr)
EP (2) EP2019101A1 (hr)
JP (1) JP2010528088A (hr)
KR (1) KR20100040806A (hr)
CN (1) CN101765600A (hr)
AR (1) AR066737A1 (hr)
AT (1) ATE522533T1 (hr)
AU (1) AU2008257534A1 (hr)
CA (1) CA2689090A1 (hr)
DK (1) DK2170891T3 (hr)
EA (1) EA200901536A1 (hr)
ES (1) ES2370677T3 (hr)
HR (1) HRP20110768T1 (hr)
IL (1) IL202375A0 (hr)
MX (1) MX2009012832A (hr)
SI (1) SI2170891T1 (hr)
TW (1) TW200906831A (hr)
WO (1) WO2008145678A1 (hr)
ZA (1) ZA200908943B (hr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8586598B2 (en) * 2009-04-29 2013-11-19 Nerviano Medical Sciences S.R.L. CDK inhibitor salts
WO2013059634A1 (en) 2011-10-20 2013-04-25 The Regents Of The University Of California Use of cdk9 inhibitors to reduce cartilage degradation
WO2015172713A1 (zh) * 2014-05-13 2015-11-19 广东东阳光药业有限公司 一种中间体的制备方法
JP6930913B2 (ja) 2014-10-14 2021-09-01 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアThe Regents Of The University Of California 炎症を阻害するためのcdk9及びbrd4阻害剤の使用法

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Also Published As

Publication number Publication date
EP2170891B1 (en) 2011-08-31
US8304418B2 (en) 2012-11-06
DK2170891T3 (da) 2011-12-12
AU2008257534A1 (en) 2008-12-04
ES2370677T3 (es) 2011-12-21
SI2170891T1 (sl) 2011-12-30
MX2009012832A (es) 2010-05-17
ZA200908943B (en) 2010-08-25
AR066737A1 (es) 2009-09-09
IL202375A0 (en) 2010-06-30
EA200901536A1 (ru) 2010-06-30
WO2008145678A1 (en) 2008-12-04
CA2689090A1 (en) 2008-12-04
JP2010528088A (ja) 2010-08-19
EP2170891A1 (en) 2010-04-07
TW200906831A (en) 2009-02-16
CN101765600A (zh) 2010-06-30
EP2019101A1 (en) 2009-01-28
US20130035349A1 (en) 2013-02-07
ATE522533T1 (de) 2011-09-15
KR20100040806A (ko) 2010-04-21
US20100160350A1 (en) 2010-06-24

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