HRP20120900T1 - Inhibitori p38 kinaze bazirani na peteroäślanom heterociklu - Google Patents

Inhibitori p38 kinaze bazirani na peteroäślanom heterociklu Download PDF

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HRP20120900T1
HRP20120900T1 HRP20120900TT HRP20120900T HRP20120900T1 HR P20120900 T1 HRP20120900 T1 HR P20120900T1 HR P20120900T T HRP20120900T T HR P20120900TT HR P20120900 T HRP20120900 T HR P20120900T HR P20120900 T1 HRP20120900 T1 HR P20120900T1
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HR
Croatia
Prior art keywords
disease
compound
arthritis
chronic
hepatitis
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HRP20120900TT
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English (en)
Inventor
Olga M. Fryszman
Hengyuan Lang
Jiong Lan
Edcon Chang
Yunfeng Fang
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Novartis Ag
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Application filed by Novartis Ag filed Critical Novartis Ag
Publication of HRP20120900T1 publication Critical patent/HRP20120900T1/hr

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Claims (4)

1. Spoj, naznačen time, da ima formulu (I): [image] gdje: C je pirazol-prsten ili imidazol-prsten; A je aril-prsten; B je aril-prsten; D je -C(O)NR80R81, pri čemu su svaki od R80 i R81 međusobno neovisno vodik, cikloalkil ili alkoksi; R1 je H ili acil; R2 je H ili alkil; R3 je vodik, 2-dioksolanil, pirimidinil, piridil, pirazinil, cijano, oksadiazolil, triazolil, metiltio, metansulfonil, 5-metiloksadiazolil, metil, CHO, jodo, kloro, metoksi, benziloksi, etoksi, ciklopropoksi, t-butoksikarbonilbutoksi ili karbamoilmetoksi; R4 je vodik; R5 je alkil; i R6 je vodik, ili njegov farmaceutski prihvatljiv derivat, koji je njegova sol, njegov solvat ili hidrat; za uporabu u postupku liječenja stanja povezanih s p38, odabranih iz skupine koju čine pankreatitis (akutni ili kronični), astma, alergije, sindrom zastoja dišnog sustava kod odraslih, kronična opstrukcijska plućna bolest, glomerulonefritis, reumatoidni artritis, sistemski eritemski lupus, skleroderma, kronični tiroiditis, Grave-ova bolest, autoimuni gastritis, dijabetes, autoimuna hemolitička anemija, autoimuna neutropenija, trombocitopenija, atopični dermatitis, kronični aktivni hepatitis, miastenija gravis, multipla skleroza, upalna bolest crijeva, ulcerativni kolitis, Chron-ova bolest, psorijaza, bolest kada stanica domaćina odbacuje presadak, upalna reakcija potaknuta endotoksinom, tuberkuloza, ateroskleroza, mišićna degeneracija, kaheksija, psorijatični artritis, Reiter-ov sindrom, giht, traumatski artritis, rubeola artritis, akutni sinovitis, bolest β-stanica gušterače; bolesti koje karakterizira masivna infiltracija neutrofila; reumatoidni spondilitis; artritis kod gihta i ostala stanja kod artritisa; cerebralna malarija; kronična upalna plućna bolest, silikoza, plućna sarkoidoza, bolest resorpcije kostiju, odbijanja transplantata, groznica i mialgija zbog infekcije, kaheksija kao sekundarna bolest nakon infekcije, meloidne tvorbe, tvorbe oko tkiva kod ožiljka, ulcerativni kolitis, pireksija, gripa, osteoporoza, osteoartritis i koštani poremećaj povezan s multiple mijelomom, akutna mijelogena leukemija, kronična mijelogena leukemija, metastazni melanom, Kaposi-jev sarkom, multiple mijelom, sepsa, septički šok, i Šigeloza; Alzheimer-ova bolest, Parkinson-ova bolest, cerebralna ishemija ili neurodegenerativna bolest uzrokovana traumatskom ozljedom; angiogenski poremećaj uključujući čvrste tumore, očna neovaskulizacija, i dječji hemangiomi; virusne bolesti uključujući akutnu hepatitis infekciju (uključujući hepatitis A, hepatitis B i hepatitis C), HIV infekcija i CMV retinitis, AIDS, SARS, ARC ili zloćudne tvorbe, i herpes; udar, miokardijalna ishemija, ishemija napada srčanog udara, hipoksija organa, vaskularna hiperplazija, kardijska i renalna reperfuzijska ozljeda, tromboza, kardijska hipertrofija, agregacija krvnih pločica potaknuta trombinom, endotoksemija i/ili sindrom toksičnog šoka, i stanja povezana sa sintezom-2 endoperoksidaze prostaglandina.
2. Spoj formule I ili njegov farmaceutski prihvatljiv derivat za uporabu prema zahtjevu 1, naznačen time, da C je pirazol-prsten i preostali supstituenti određeni u zahtjevu 1.
3. Spoj formule I, naznačen time, da je to spoj 3-(5-amino-4-benzoil-pirazol-1-il)-N-ciklopropil-4-metil-benzamid, ili njegov farmaceutski prihvatljiv derivat određen u zahtjevu 1, te da je za uporabu prema zahtjevu 1.
4. Spoj formule I, naznačen time, da je to spoj 3-[5-amino-4-(3-cijanobenzoil)-pirazol-1-il]-N-ciklopropil-4-metil-benzamid, ili njegov farmaceutski prihvatljiv derivat određen u zahtjevu 1, te da je za uporabu prema zahtjevu 1.
HRP20120900TT 2003-06-26 2012-11-08 Inhibitori p38 kinaze bazirani na peteroäślanom heterociklu HRP20120900T1 (hr)

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