HRP20180109T1 - Inhibitori gsk-3 - Google Patents

Inhibitori gsk-3 Download PDF

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Publication number
HRP20180109T1
HRP20180109T1 HRP20180109TT HRP20180109T HRP20180109T1 HR P20180109 T1 HRP20180109 T1 HR P20180109T1 HR P20180109T T HRP20180109T T HR P20180109TT HR P20180109 T HRP20180109 T HR P20180109T HR P20180109 T1 HRP20180109 T1 HR P20180109T1
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disease
substituted
unsubstituted
compound
use according
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HRP20180109TT
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Ana MARTÍNEZ GIL
Miguel Medina Padilla
Mercedes Alonso Cascón
Ana Fuertes Huerta
María Luisa NAVARRO RICO
María José PÉREZ PUERTO
Ana Castro Morera
Ester MARTÍN APARICIO
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Asd Therapeutics Partners Llc
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/17Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61P17/00Drugs for dermatological disorders
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
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    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
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    • 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
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/66Nitrogen atoms not forming part of a nitro radical

Claims (15)

1. Upotreba spoja formule (I) [image] , ili bilo koje njegove farmaceutski prihvatljive soli ili solvata, gdje: RB je skupina koju se bira između [image] ; R3, R4, R’2, R’3, R’4, R’5 i R’6 se bira između vodika, supstituiranog ili nesupstituiranog alkila, supstituiranog ili nesupstituiranog cikloalkila, supstituiranog ili nesupstituiranog alkenila, supstituiranog ili nesupstituiranog arila, supstituiranog ili nesupstituiranog heterocikla, -C(=O)R7, -C(=O)OR8, -C(=O)NR9R10, -C=NR11, -CN, -OR12, -OC(=O)R13, -S(O)t-R14,-NR15R16, -NR17C(=O)R18, -NO2, -N=CR19R20 ili halogena, gdje R3 i R4 zajedno mogu tvoriti skupinu =O, te gdje bilo koji par kojeg čine R3R’2, R3R’6, R4R’2, R4R’6, R’2R’3, R’3R’4, R’4R’5, R’5R’6, R15R16, R17R18 ili R19R20 može zajedno tvoriti prstenasti supstituent; t je 0, 1, 2, 3; R7, R8, R9, R10, R11, R13, R14, R15, R16, R17, R18, R19 i R20 se bira između vodika, supstituiranog ili nesupstituiranog alkila, supstituiranog ili nesupstituiranog cikloalkila, supstituiranog ili nesupstituiranog alkenila, supstituiranog ili nesupstituiranog arila, supstituiranog ili nesupstituiranog heterocikla, supstituiranog ili nesupstituiranog alkoksi, supstituiranog ili nesupstituiranog ariloksi, halogena; R12 se bira između vodika, nesupstituiranog alkila, supstituiranog ili nesupstituiranog cikloalkila, supstituiranog ili nesupstituiranog alkenila, supstituiranog ili nesupstituiranog arila, supstituiranog ili nesupstituiranog heterocikla, halogena; naznačena time što je spoj namijenjen proizvodnji medikamenta za liječenje i/ili sprječavanje bolesti ili stanja povezanog s GSK-3, gdje se bolest ili stanje bira iz skupine koju čine dijabetes, stanja povezana s dijabetesom, kronična neurodegenerativna stanja, uključujući demencije, poput Alzheimerove bolesti, Parkinsonove bolesti, progresivne supranuklearne paralize, subakutnog sklerozirajućeg panencefalitičkog parkinsonizma, postencefalitičkog parkinsonizma, pugilističkog encefalitisa, guamskog kompleksa parkinsonizma s demencijom, Pickove bolesti, kortikobazalne degeneracije, frontotemporalne demencije, Huntingtonove bolesti, demencije povezane s AIDS-om, amiotrofna lateralne skleroze, multiple skleroze i neurotraumatske bolesti, poput akutnog inzulta, epilepsije, poremećaji raspoloženja, poput depresije, shizofrenije i bipolarnih poremećaja, poticanje funkcionalnog oporavka nakon inzulta, krvarenje u velikom mozgu, primjerice zbog pojedinačne cerebralne amiloidne angiopatije, gubitak kose, pretilost, hipertenzija, sindrom policističnih jajnika, sindrom X, ishemija, ozljeda mozga, traumatska ozljeda mozga, rak, leukopenija, Downov sindrom, bolest Lewyjevih tijela, upala, kronične upalne bolesti, rak i hiperproliferativne bolesti poput hiperplazija i imunodeficijencija.
2. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što su R3 i R4 H.
3. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što se R’2, R’3, R’4, R’5 i R’6 bira između vodika, supstituiranog ili nesupstituiranog alkila, -C(=O)R7, -C(=O)OR8, -OR12, -NR15R16 ili halogena, gdje su R7, R8, R12, R15 i R16 definirani kao u patentnom zahtjevu 1.
4. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što su R’2, R’3, R’4, R’5 i R’6 H.
5. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što se spoj formule (I) bira između: [image]
6. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što je bolest Alzheimerova bolest.
7. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što je bolest dijabetes tip II.
8. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što je bolest depresija.
9. Upotreba u skladu s patentnim zahtjevom 1, naznačena time što je bolest ozljeda mozga.
10. Spoj, naznačen time što je spoj formule [image] .
11. Spoj formule [image] , naznačen time što je namijenjen upotrebi kao medikament.
12. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 10 do 11, kao i farmaceutski prihvatljivu podlogu, adjuvans ili vehikulum.
13. Farmaceutski pripravak u skladu s patentnim zahtjevom 12, naznačen time što je namijenjen oralnoj primjeni.
14. Upotreba spoja formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačena time što se spoj upotrebljava kao reagens za inhibiranje GSK-3 u biološkim ispitivanjima.
15. Spoj formule (I) u skladu s patentnim zahtjevima 1 do 5, ili njegov farmaceutski pripravak, naznačeni time što su namijenjeni upotrebi u liječenju ili sprječavanju bolesti ili stanja povezanog s GSK-3, gdje se bolest ili stanje bira iz skupine koju čine dijabetes, stanja povezana s dijabetesom, kronična neurodegenerativna stanja, uključujući demencije, poput Alzheimerove bolesti, Parkinsonove bolesti, progresivne supranuklearne paralize, subakutnog sklerozirajućeg panencefalitičkog parkinsonizma, postencefalitičkog parkinsonizma, pugilističkog encefalitisa, guamskog kompleksa parkinsonizma s demencijom, Pickove bolesti, kortikobazalne degeneracije, frontotemporalne demencije, Huntingtonove bolesti, demencije povezane s AIDS-om, amiotrofna lateralne skleroze, multiple skleroze i neurotraumatske bolesti, poput akutnog inzulta, epilepsije, poremećaji raspoloženja, poput depresije, shizofrenije i bipolarnih poremećaja, poticanje funkcionalnog oporavka nakon inzulta, krvarenje u velikom mozgu, primjerice zbog pojedinačne cerebralne amiloidne angiopatije, gubitak kose, pretilost, hipertenzija, sindrom policističnih jajnika, sindrom X, ishemija, ozljeda mozga, traumatska ozljeda mozga, rak, leukopenija, Downov sindrom, bolest Lewyjevih tijela, upala, kronične upalne bolesti, rak i hiperproliferativne bolesti poput hiperplazija i imunodeficijencija.
HRP20180109TT 2005-07-29 2018-01-22 Inhibitori gsk-3 HRP20180109T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP05380176A EP1749523A1 (en) 2005-07-29 2005-07-29 GSK-3 inhibitors
PCT/EP2006/007520 WO2007017145A2 (en) 2005-07-29 2006-07-28 Gsk-3 inhibitors
EP06776492.8A EP1919465B1 (en) 2005-07-29 2006-07-28 Gsk-3 inhibitors

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HRP20180109T1 true HRP20180109T1 (hr) 2018-04-20

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US (1) US8686042B2 (hr)
EP (2) EP1749523A1 (hr)
JP (1) JP5484726B2 (hr)
KR (1) KR101471999B1 (hr)
CN (1) CN101257900B (hr)
AU (1) AU2006278829B2 (hr)
BR (1) BRPI0615968B1 (hr)
CA (1) CA2616451C (hr)
CY (1) CY1119971T1 (hr)
DK (1) DK1919465T3 (hr)
ES (1) ES2661326T3 (hr)
HK (1) HK1124761A1 (hr)
HR (1) HRP20180109T1 (hr)
HU (1) HUE036844T2 (hr)
IL (1) IL189048A (hr)
LT (1) LT1919465T (hr)
NO (1) NO341454B1 (hr)
NZ (1) NZ566380A (hr)
PL (1) PL1919465T3 (hr)
PT (1) PT1919465T (hr)
RU (1) RU2449998C2 (hr)
SI (1) SI1919465T1 (hr)
WO (1) WO2007017145A2 (hr)
ZA (1) ZA200800983B (hr)

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PL1919465T3 (pl) 2018-06-29
KR101471999B1 (ko) 2014-12-10
HK1124761A1 (en) 2009-07-24
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