SI2448941T1 - Pirazolopirimidinske spojine, ki zavirajo JAK, in postopki - Google Patents

Pirazolopirimidinske spojine, ki zavirajo JAK, in postopki Download PDF

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Publication number
SI2448941T1
SI2448941T1 SI201031625T SI201031625T SI2448941T1 SI 2448941 T1 SI2448941 T1 SI 2448941T1 SI 201031625 T SI201031625 T SI 201031625T SI 201031625 T SI201031625 T SI 201031625T SI 2448941 T1 SI2448941 T1 SI 2448941T1
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SI
Slovenia
Prior art keywords
disease
colitis
pyrazolo
carboxamide
methoxyphenyl
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SI201031625T
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English (en)
Inventor
Paul Gibbons
Emily Hanan
Wendy Liu
Joseph P. Lyssikatos
Steven R. Magnuson
Rohan Mendonca
Richard Pastor
Thomas E. Rawson
Michael Siu
Mark E. Zak
Aihe Zhou
Bing-Yan Zhu
Christopher Hurley
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Genentech, Inc.
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Publication of SI2448941T1 publication Critical patent/SI2448941T1/sl

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material 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)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (6)

  1. EP 2448941 BI Pirazolopirimidinske spojine, ki zavirajo JAK, in postopki Patentni zahtevki
    1. Spojina, izbrana izmed: N-(4-(5-kloro-2-metoksifenil)-2-(2-hidroksi-2-metilpropil)tiazol-5-il)pirazolo[l,5- a]pirimidin-3 -karboksamida; N-(4-(5-kloro-2-metoksifenil)-2-(2-metilprop-l-enil)tiazol-5-il)pirazolo[l,5- a]pirimidin-3-karboksamida; N-(2-bromo-4-(5-kloro-2-metoksifenil)tiazol-5-il)pirazolo[l,5-a]pirimidin-3- karboksamida; N-(4-(5-kloro-2-metoksifenil)tiazol-5-il)pirazolo[l,5-a]pirimidin-3-karboksamida; N-(4-(5-kloro-2-metoksifenil)-2-metiltiazol-5-il)pirazolo[l,5-a]pirimidin-3- karboksamida; N-(4-(5-kloro-2-metoksifenil)-2-(tetrahidro-2H-piran-4-il)tiazol-5-il)pirazolo[l,5- a]pirimidin-3-karboksamida; in farmacevtsko sprejemljivih soli le-teh.
  2. 2. Farmacevtski sestavek, ki obsega spojino po zahtevku 1 in farmacevtsko sprejemljiv nosilec, adjuvant ali podlago.
  3. 3. Spojina po zahtevku 1 za uporabo v medicini.
  4. 4. Terapevtsko učinkovita količina spojine po zahtevku 1 za uporabo pri preprečevanju, zdravljenju ali zmanjševanju težavnosti bolezni ali stanja, izbranega izmed kapi, diabetesa, hepatomegalije, kardiovaskularne bolezni, cistične fibroze, virusne bolezni, avtoimunskih bolezni, alergijskih motenj, vnetja, nevroloških motenj, bolezni, povezanih s hormoni, stanj, povezanih s transplantacijo organov, motenj imunske pomanjkljivosti, destruktivnih kostnih motenj, proliferativnih motenj, infekcioznih bolezni, stanj, povezanih s celično smrtjo, trombinsko inducirane agregacije trombocitov, jetrne bolezni, patoloških imunskih stanj, ki vključujejo aktivacijo celic T, motenj CŽS ali mieloproliferativne motnje.
  5. 5. Spojina za uporabo po zahtevku 4, kjer je bolezen ali stanje izbrano izmed: raka; kardiovaskularne bolezni, izbrane izmed restenoze, kardiomegalije, ateroskleroze, miokardnega infarkta ali kongestivne srčne odpovedi; nevrološke motnje, ki je nevrodegenerativna bolezen, izbrana izmed Alzheimerjeve bolezni, Parkinsonove bolezni, amiotrofične lateralne skleroze, Huntingtonove bolezni in cerebralne ishemije; vnetja, ki je vnetna bolezen, izbrana izmed vnetne črevesne bolezni, revmatoidnega artritisa, psoriaze, kontaktnega dermatitisa ali zapoznelih preobčutljivostnih reakcij; avtoimunske bolezni, izbrane izmed lupusa ali multiple skleroze, Crohnove bolezni, ulceroznega kolitisa, kolagenoznega kolitisa, limfocitnega kolitisa, ishemičnega kolitisa, diverzijskega kolitisa, Behfetovega sindroma, infekcioznega kolitisa in nedoločljivega kolitisa; in psoriaze.
  6. 6. Spojina za uporabo po zahtevku 3 za uporabo pri preprečevanju, zdravljenju ali zmanjševanju težavnosti bolezni ali stanja, izbranega izmed raka, prave policitemije, esencialne trombocitoze, mielofibroze, kronične mielogene levkemije (CML), revmatoidnega artritisa, vnetnega črevesnega sindroma, Crohnove bolezni, psoriaze, kontaktnega dermatitisa ali zapoznelih preobčutljivostnih reakcij.
SI201031625T 2009-07-02 2010-07-02 Pirazolopirimidinske spojine, ki zavirajo JAK, in postopki SI2448941T1 (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22291809P 2009-07-02 2009-07-02
PCT/US2010/040906 WO2011003065A2 (en) 2009-07-02 2010-07-02 Pyrazolopyrimidine jak inhibitor compounds and methods
EP10794815.0A EP2448941B1 (en) 2009-07-02 2010-07-02 Pyrazolopyrimidine jak inhibitor compounds and methods

Publications (1)

Publication Number Publication Date
SI2448941T1 true SI2448941T1 (sl) 2018-02-28

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SI201031625T SI2448941T1 (sl) 2009-07-02 2010-07-02 Pirazolopirimidinske spojine, ki zavirajo JAK, in postopki

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US (6) US8999998B2 (sl)
EP (3) EP2448941B1 (sl)
JP (4) JP5769261B2 (sl)
KR (3) KR101903305B1 (sl)
CN (2) CN102482284B (sl)
AU (1) AU2010266188B2 (sl)
BR (1) BRPI1010197A2 (sl)
CA (1) CA2767097A1 (sl)
CL (1) CL2012000001A1 (sl)
CO (1) CO6491081A2 (sl)
CR (2) CR20170115A (sl)
DK (1) DK2448941T3 (sl)
EC (1) ECSP12011645A (sl)
ES (1) ES2657839T3 (sl)
HR (1) HRP20180157T1 (sl)
HU (1) HUE035537T2 (sl)
IL (3) IL217224B (sl)
IN (1) IN2012DN00755A (sl)
LT (1) LT2448941T (sl)
MA (1) MA33502B1 (sl)
MX (1) MX2012000169A (sl)
MY (1) MY160156A (sl)
NO (1) NO2448941T3 (sl)
NZ (4) NZ706218A (sl)
PE (2) PE20120575A1 (sl)
PH (1) PH12015500666A1 (sl)
PL (1) PL2448941T3 (sl)
PT (1) PT2448941T (sl)
RS (1) RS56671B1 (sl)
RU (2) RU2675857C2 (sl)
SG (2) SG10201509607XA (sl)
SI (1) SI2448941T1 (sl)
UA (1) UA110324C2 (sl)
WO (1) WO2011003065A2 (sl)
ZA (2) ZA201200490B (sl)

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