HUE035537T2 - Pirazolopirimidin JAK inhibitor vegyületek és eljárások - Google Patents

Pirazolopirimidin JAK inhibitor vegyületek és eljárások Download PDF

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Publication number
HUE035537T2
HUE035537T2 HUE10794815A HUE10794815A HUE035537T2 HU E035537 T2 HUE035537 T2 HU E035537T2 HU E10794815 A HUE10794815 A HU E10794815A HU E10794815 A HUE10794815 A HU E10794815A HU E035537 T2 HUE035537 T2 HU E035537T2
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Hungary
Prior art keywords
disease
chloro
methoxyphenyl
compound
carboxamide
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HUE10794815A
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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 HUE035537T2 publication Critical patent/HUE035537T2/hu

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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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (6)

  1. PIRAZGLÖPIRIIWÉDIN JAK INHIBITOR VEGYÜLETEK ÉS ELJÁRÁSOK Szabadalmi igénypontok:
    1, Vegyűlet, amelyet az: N~(4-(5-klór~2~metoxífenil)-2-{2-hídroxí-2-metiípropil)tiazol-5-il)pirazolo[1,5- ajpirímidin~3-karboxamid; N-^-CS-któr^-metoxIfeniO-^-CS-metilprop-l-enilttíazolSiljpirazofo^Lb- a]pirirnídín~3~karboxamid; Ν··(2··0Γ0Γη·-4“(5~ΚΙ0Γ~2'4ηο1οχίίοπίΙ)ί!3Ζ.οΙ-5~!θρΐΓάΖθίοΠ!5'9]ρίΓΗ'ηί0ίη~3·' karboxamid; N~(4-'(5~klór~-2'-metoxifeníi)tiazol-5 ii)pirazolo[1,5-a]pirimidin~3-karboxamid; N-(4-(6-któr~2~metoxlfeníl)~2-metiltiazol-5-il)pirazolop1,5a]pídmidin-3· karboxamid; N-(4-(5-klór-2”metoxifenií)~2-(tetrabidro-2H~pfrán-4-ii)tiazoi-5~íí)pirazoío[1,5~ a] p I ri m id i π -3- karboxamid ; és gyógyászatílag elfogadható sóik közül választunk.
  2. 2, Gyógyászati készítmény, amely tartalmaz az 1, igénypont szerinti vegyüíetet és gyógyászatílag elfogadható hordozóanyagot, adjuvárisi vagy vivöanyagot.
  3. 3, Az 1. igénypont szerinti vegyűlet gyógyászatban való alkalmazásra.
  4. 4, Az 1. igénypont szerinti vegyűlet terápiásán hatásos mennyisége olyan betegség vagy állapot megelőzésében, kezelésében vagy súlyosságának csökkentésében való alkalmazásra, amelyet a sztrók, cukorbetegség, hepatomegálía, kardlovaszkuíárís betegség, cisztás íibrozis, vírusos betegség, autoimmun betegségek, allergiás rendellenességek, gyulladás, neurológiai rendellenességek, hormonnal kapcsolatos betegség, szervátültetéssel összefüggő állapotok, irnmundefíciencíávai járó rendellenességek, destruktív csontrendelienességek, proliferativ rendellenességek, fertőzése® betegségek, sejtelhalássai összefüggő állapotok, trombin által kiváltott vériemezke-aggregáció, májbefegség, T-sejt aktívádét magukba foglaló patológiás imrnunállapotok, CNS rendellenességek vagy myeloproliferativ rendellenesség,
  5. 5. Vegyülef alkalmazásra a 4, igénypont szerint, ahol a betegséget vagy állapotot a: rák; kardiovaszkuíáris betegség, amelyet a resztenózís, eardiomegália, atherosclerosis, szívizom-infarktus vagy kongeszt'iv szívelégtelenség közül választunk; neurológiai rendellenesség, amely olyan neurodegeneratlv betegség, amelyet az Alzheimer-kór, Parkínson-kór, amiotrófiás laterális szklerózls, Huntington-kór és cerebralis ischaemia közül választunk; gyulladás, amely olyan gyulladásos betegség, amelyet a gyulladásos béíbetegség, rheumatoid arthritis, pszoriázis, kontakt dermatitis vagy késleltetett túlérzékenységi reakciók közül választunk; autoimmun betegség, amelyet a lupus vagy sclerosis multiplex, Crohn-betegség, uiceratív colitis, kciiagéces colitis, limfocliás colitis, ischaemias colitis, diverziós colitis, Behçet-szindrôma, fertőző colitis és indeformicált colitis; és pszoriázis közül választjuk,
  6. 6, Ä vegyülef alkalmazásra a 3. igénypont szerint olyan betegség vagy állapot megelőzésében, kezelésében vagy súlyosságának csökkentésében való alkalmazásra, amelyet a rák, polycythemia vers, esszenciális trombccitózis, myelofibrosis, krónikus mielogén leukémia (CML), rheumatoid arthritis, gyulladásos bél szindróma, Crohn-betegség, pszoriázis, kontakt dermatitis vagy késleltetett túlérzékenységi reakciók közül választunk.
HUE10794815A 2009-07-02 2010-07-02 Pirazolopirimidin JAK inhibitor vegyületek és eljárások HUE035537T2 (hu)

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EP (3) EP2448941B1 (hu)
JP (4) JP5769261B2 (hu)
KR (3) KR101903305B1 (hu)
CN (2) CN102482284B (hu)
AU (1) AU2010266188B2 (hu)
BR (1) BRPI1010197A2 (hu)
CA (1) CA2767097A1 (hu)
CL (1) CL2012000001A1 (hu)
CO (1) CO6491081A2 (hu)
CR (2) CR20170115A (hu)
DK (1) DK2448941T3 (hu)
EC (1) ECSP12011645A (hu)
ES (1) ES2657839T3 (hu)
HR (1) HRP20180157T1 (hu)
HU (1) HUE035537T2 (hu)
IL (3) IL217224B (hu)
IN (1) IN2012DN00755A (hu)
LT (1) LT2448941T (hu)
MA (1) MA33502B1 (hu)
MX (1) MX2012000169A (hu)
MY (1) MY160156A (hu)
NO (1) NO2448941T3 (hu)
NZ (4) NZ738778A (hu)
PE (2) PE20120575A1 (hu)
PH (1) PH12015500666A1 (hu)
PL (1) PL2448941T3 (hu)
PT (1) PT2448941T (hu)
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RU (2) RU2567238C2 (hu)
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