HRP20121021T1 - SPOJ 3-FENILPIRAZOLO[5,1-b]TIAZOLA - Google Patents

SPOJ 3-FENILPIRAZOLO[5,1-b]TIAZOLA Download PDF

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HRP20121021T1
HRP20121021T1 HRP20121021AT HRP20121021T HRP20121021T1 HR P20121021 T1 HRP20121021 T1 HR P20121021T1 HR P20121021A T HRP20121021A T HR P20121021AT HR P20121021 T HRP20121021 T HR P20121021T HR P20121021 T1 HRP20121021 T1 HR P20121021T1
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compound
compound according
methoxy
salt
thiazol
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HRP20121021AT
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Hisashi Shibata
Kodo Shikata
Akira Inomata
Kogyoku Shin
Taro Terauchi
Yoshinori Takahashi
Minako Hashizume
Kunitoshi Takeda
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Eisai R&D Management Co., Ltd.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Addiction (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (18)

1. Spoj prikazan sa formulom (I) ili njegova sol: [image] naznačen time da R1 predstavlja formulu -A11-A12; R2 predstavlja tetrahidrofurilmetil, tetrahidropiranilmetil ili tetrahidropiranil; A11 predstavlja jednostruku vezu, metilen ili 1,2-etilen; A12 predstavlja C1-6 alkil, C3-6 cikloalkil, ili C3-6 cikloalkil supstituiran sa metilnom skupinom; R3 predstavlja metoksi, cijano, ciklobutiloksimetil, metoksimetil ili etoksimetil; i R4 predstavlja metoksi ili klor.
2. Spoj prema zahtjevu 1, naznačen time da R2 je tetrahidropiran-4-il, tetrahidropiran-3-il, (tetrahidropiran-4-il)metil ili (tetrahidrofuran-3-il)metil.
3. Spoj prema zahtjevu 1 ili zahtjevu 2, naznačen time da R1 je n-propil, n-butil, n-pentil, ciklopropilmetil, ciklobutilmetil, 2-(ciklopropil)etil ili (2-metilciklopropil)metil.
4. Spoj prema zahtjevu 1, naznačen time da spoj je N-butil-3-[2,6-dimetoksi-4-(metoksimetil)fenil]-6-metoksi-N-(tetrahidro-2H-piran-4-il)pirazolo[5,1-b][1,3]tiazol-7-amin ili njegova sol.
5. Spoj prema zahtjevu 1, naznačen time da spoj je N-butil-3-[4-(etoksimetil)-2,6-dimetoksifenil]-6-metoksi-N-(tetrahidro-2H-piran-4-il)pirazolo[5,1-b][1,3]tiazol-7-amin ili njegova sol.
6. Spoj prema zahtjevu 1, naznačen time da spoj je N-(2-ciklopropiletil)-3-[4-(etoksimetil)-2,6-dimetoksifenil]-6-metoksi-N-(tetrahidro-2H-piran-4-il)pirazolo[5,1-b][1,3]tiazol-7-amin ili njegova sol.
7. Spoj prema zahtjevu 1, naznačen time da spoj je 3-[4-(etoksimetil)-2,6-dimetoksifenil]-6-metoksi-N-propil-N-(tetrahidro-2H-piran-3-il)pirazolo[5,1-b][1,3]tiazol-7-amin ili njegova sol.
8. Spoj prema zahtjevu 1, naznačen time da spoj je N-(ciklobutilmetil)-3-[2,6-dimetoksi-4-(metoksimetil)fenil]-6-metoksi-N-(tetrahidro-2H-piran-4-il)pirazolo[5,1-b][1,3]tiazol-7-amin ili njegova sol.
9. Spoj prema zahtjevu 1, naznačen time da spoj je N-(ciklopropilmetil)-3-[2,6-dimetoksi-4-(metoksimetil)fenil]-6-metoksi-N-(tetrahidro-2H-piran-4-il)pirazolo[5,1-b][1,3]tiazol-7-amin ili njegova sol.
10. Spoj prema zahtjevu 1, naznačen time da spoj je 3-[2,6-dimetoksi-4-(metoksimetil)fenil]-6-metoksi-N-propil-N-(tetrahidro-2H-piran-4-il)pirazolo[5,1-b][1,3]tiazol-7-amin ili njegova sol.
11. Spoj prema zahtjevu 1, naznačen time da spoj je 3-[2-chloro-6-metoksi-4-(metoksimetil)fenil]-6-metoksi-N-propil-N-(tetrahidro-2H-piran-4-il)pirazolo[5,1-b][1,3]tiazol-7-amin ili njegova sol.
12. Spoj prema zahtjevu 1, naznačen time da spoj je 4-{7-[(ciklopropilmetil)(tetrahidrofuran-3-ilmetil)amino]-6-metoksipirazolo[5,1-b][1,3]tiazol-3-il}-3,5-dimetoksibenzonitril ili njegova sol.
13. Spoj prema zahtjevu 1, naznačen time da spoj je N-(ciklopropilmetil)-6-metoksi-N-(tetrahidro-2H-piran-4-ilmetil)-3-(2,4,6-trimetoksifenil)-pirazolo[5,1-b][1,3]tiazol-7-amin ili njegova sol.
14. Farmaceutski pripravak naznačen time da sadrži spoj prema bilo kojem od zahtjeva 1-13 kao aktivni sastojak.
15. Terapeutsko ili profilaktičko sredstvo koje sadrži spoj prema bilo kojem od zahtjeva 1-13 naznačeno time da je za uporabu kod liječenja ili sprečavanja depresije, simptoma depresije, tjeskobe, sindroma iritabilnog crijeva, poremećaja spavanja, nesanice, ovisnosti o alkoholu, simptoma odvikavanja od alkohola, ovisnosti o drogama, simptoma odvikavanja od droga, probavnih poremećaja vezanih uz stres, anoreksije, poremećaja prehrane, postoperativnog ileusa, ishemijske neuropatije, apopleksije, ekscitotoksične neuropatije, konvulzija, epilepsije, hipertenzije, shizofrenije, bipolarnog poremećaja ili demencije.
16. Terapeutsko ili profilaktičko sredstvo za uporabu prema zahtjevu 15, naznačeno time da terapeutsko ili profilaktičko sredstvo je za uporabu kod liječenja ili sprečavanja depresije, simptoma depresije, tjeskobe ili sindroma iritabilnog crijeva.
17. Spoj prema bilo kojem od zahtjeva 1-13 naznačen time da je za uporabu kod liječenja ili sprečavanja depresije, simptoma depresije, tjeskobe, sindroma iritabilnog crijeva, poremećaja spavanja, nesanice, ovisnosti o alkoholu, simptoma odvikavanja od alkohola, ovisnosti o drogama, simptoma odvikavanja od droga, probavnih poremećaja vezanih uz stres, anoreksije, poremećaja prehrane, postoperativnog ileusa, ishemijske neuropatije, apopleksije, ekscitotoksične neuropatije, konvulzija, epilepsije, hipertenzije, shizofrenije, bipolarnog poremećaja ili demencije.
18. Spoj za uporabu prema zahtjevu 17, naznačen time da je spoj za uporabu kod liječenja ili sprečavanja depresije, simptoma depresije, tjeskobe ili sindroma iritabilnog crijeva.
HRP20121021AT 2008-04-15 2012-12-12 SPOJ 3-FENILPIRAZOLO[5,1-b]TIAZOLA HRP20121021T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US4508408P 2008-04-15 2008-04-15
JP2008106080 2008-04-15
PCT/JP2009/057270 WO2009128383A1 (ja) 2008-04-15 2009-04-09 3-フェニルピラゾロ[5,1-b]チアゾール化合物

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HRP20121021T1 true HRP20121021T1 (hr) 2013-01-31

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US (1) US8431603B2 (hr)
EP (1) EP2266990B1 (hr)
JP (1) JP4654325B2 (hr)
KR (1) KR101601994B1 (hr)
CN (1) CN102007133B (hr)
AR (1) AR071655A1 (hr)
AU (1) AU2009237050B2 (hr)
BR (1) BRPI0911659B8 (hr)
CA (1) CA2721670C (hr)
CL (1) CL2009000896A1 (hr)
CY (1) CY1113484T1 (hr)
DK (1) DK2266990T3 (hr)
ES (1) ES2396126T3 (hr)
HK (2) HK1150310A1 (hr)
HR (1) HRP20121021T1 (hr)
IL (1) IL208393A (hr)
MX (1) MX2010011089A (hr)
MY (1) MY152687A (hr)
NZ (1) NZ588376A (hr)
PE (1) PE20091890A1 (hr)
PL (1) PL2266990T3 (hr)
PT (1) PT2266990E (hr)
RS (1) RS52561B (hr)
RU (1) RU2482120C2 (hr)
SI (1) SI2266990T1 (hr)
TW (1) TW201004964A (hr)
UA (1) UA101836C2 (hr)
WO (1) WO2009128383A1 (hr)
ZA (1) ZA201006764B (hr)

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