HUE027445T2 - 1H-indazol-3-karboxamid-vegyületek alkalmazása glikogén-szintáz kináz 3-béta inhibitorként - Google Patents
1H-indazol-3-karboxamid-vegyületek alkalmazása glikogén-szintáz kináz 3-béta inhibitorként Download PDFInfo
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- HUE027445T2 HUE027445T2 HUE13703799A HUE13703799A HUE027445T2 HU E027445 T2 HUE027445 T2 HU E027445T2 HU E13703799 A HUE13703799 A HU E13703799A HU E13703799 A HUE13703799 A HU E13703799A HU E027445 T2 HUE027445 T2 HU E027445T2
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Claims (5)
- ^ $ V ν' í V j £ f!4411/DK EP 2 Sí? 301 B1 1 H“®áa^E3-k^b0xai»Iá~vegyildel: alkalmazása, glikogétt-szlMaz Mnéz 3-beta inhibitorokként SZABADALMI IDÉMYFON' ΓΟΚ L A (1) Utalásos képlett 1 II-lödazol-S-kmlxjxamM vegyuletekPl ahol 1¾ M Eís'azoBos vagy Milösbözo, és jetetésife bEffögeaBlota' balogénaiom; M szénaíomos slkllcsöpörk Mi szénaiomos alkemlesopott* 2M széaatomns alkmilesopett «agy 1 szénatomos alkoxtcsoport, adott estbe» szuhsztlttAéYgy vagy több.. a Lőve#azS eso|?oAbő| .'kiválasztott szubsztituenssei: hatogénaiora, |MtpxÍ~, ~NH?, és 1-3 sxénaíomos alkoxkspport;; karbodkiusos vagy heterociklusos akiás vagy aromlá,: 3-12 tagú gyűrű, mely adott esetben egy vagy több, a hálögérmtom, bidroxi-, 1-i Szinátötnos alktE, 1-6 szioátomöS alkoxi, -1¾¾ -0(0)01-1, - 0(0)01.¾ és ~€<ö)N.RjR2 csoportból választott sxtÉsziiMéhssel lehet szubszfcllva; Y jelentése egy kötés, ]~6 szénatomos aikiL, 2-í szénatomos alkeml-yagy 2-i Sziftatoxaes alkínilcsopori, adott esetben egy vagy több, a hálogénatom, hidroxil*, -MBy, is 1 »3 szénatomos aikoxlesoport csoportból válasziótt szúbsztítaenssel. szttbsxtiéllvat Rí> 3-12 tagú karbodfeteos vagy betetödMttsos,alifás vagy aromás* 341 szénatomos gyűrű, mely egy vagy több, a halogétiatom, hidroxíl-, miro-, dano-, -CPj, 1-6 sxénatomos alkoxi-. benziloxl-J-4 szendomps . alkik, 2-4 szénatomos alkesi~, és |~4 szénaiomos alklni!-, ~MliSÖ2Ci%, -S02NH2, -Z-€(0)0H, -Z-C(0)0Ri és ~ZC(0)NRsR2 “aWljeteiese o-kÖí# vagy 1-3 szénatomos alkilcsoport - csoportból kiválasztott s^íbsztltuepssel van sznbsztltuálva; t:j és R> f&ggetienQlhidrogénatomot» 14 szénatótüos alktiesoporiot, alkeniesoponot, 24 szénatomos alkioilesöportót, vágj? frnjtesopmtet jelem; és 0 vegytó(^; eílbga#ató szerves és szervetlen savakkal és bázisokkal képezett sddielps sói; θ$Κ>·3β szabályozatlan aktivitása vagy iúlexptésszlója mül kialakuló, az (I) inzbllm rezisztaocia betegségek; pl); Marödegener&Civ beíepégefe; (ili) baognlat zavarok; (iv) skizofrén zavarok; (v) rákos betegségek; (vi) gyulladás, (vlxj kábítószerrel való visszaélés betegségek; és (vili) epilepsziák kezelésében való alkalmazásra, 2, iíi“indazöl»3"karbözamid az 1, igénypont szerinti alkataiazásra, attól az említett iinzulin-reziszteaeia betegségek a 24ípüSü diabétesz, X szindróma, eünzottság, és polielsztás péteiészek szindróma: csoportból vannak, kiválasztva, 3, tltdadazöl44arboxs.mid az L igénypont szerinti alkalmazásra, ahol az említett oeuxodegeneradv betegségek a FarkinsookónAlzheirner kór, Huntington kór, és spmális nemrrdegenerauv betegségek csoportból vannak kiválasztva.
- 4, IHÓRdazobB-karboxamid: a 3. igénypont szerinti alkateazásm5: áboi az említeti neürodépneratív betegségek az amiotrófiás laterális szklerézls, sciemzls mnlbplex, geánm iZömsörvadás és gerincvelő sérülés következtében létrejött aeareiegeaeráeld csoportból vadnak kiválasztva. 5.1 l:frí«dazob3»karbóxamid: az 1, igénypont szmánti alkalmazásra, abol az említett hangulat zavarok a bipoláris zavarok és a depresszív zavarok csoportból vannak kiválasztva, 6. ÍH^Iiáazol“3“k8rÍáxaiai4i m $« %É$|aPRt szerinti alkalmazásra, abol az említett bipoláris zavarok a bipoláris I zavar, bipoláris II zavar, ciklusos elmeállapot és másként meg nem határozható bipoláris zavarok (BD-NOS) csoportból vannak kiválasztva, ?x. ilddadazoi-B-'karboxamid m S, igénypont szerinti alkalmazásra, aboi az említett depressziós renrfellenességek a major depressz.lv zavar (MDD), aiipusos depresszió (AD), melmikoiikas depresszió, pszkhoíibus major depressziós zavar (FMD), katalán depresszió, szülés utáni depresszió (PPD}, szezonális affektív zavar (SAÖ), dysthymla, és másként meg nem katározbaró depressziós rendellenességek (DDdsIöS) csoportból vannak kiválasztva, ÜL ÍlÍ-Índazoh3--karboxamid az i. igénypont szerinti alkalmazásra, abol a visszaélési rendeléPésségek a pszíehostinudánsokkál váló visszaélés következtében kialakult rendeilénésségek közül vannak kiválasztva.
- 9, I ax 1, Igéin pont szerinti aMmaMsm, ahól m. említett sMtófés zavarok a paranoid skizofrénia, rendezetlen Sklxöiénia* katatőn skizoitori;*, egyszerű skizofrénia* rezíiuáits tósoMiiák és diíferenetilsiaP skizofrénia esöporlból vannak kiválasztva, 10, Í||é|kia2ölO»lÉif|^8iöíd az 1,: Igénypont szeriig. ^φψφ^, aM, m eialtett rákos betegségek a prosztata, hasnyábrsirigy, petefészek és vastagbehyégMI rák* és MLL-társait lenkémla csoporiboi vannak kiválasztva,
- 11. Gyógyszerkészítmény, mely legalább egy l:. Igénypont szerinti (I) állalános képlett Végyüktet* a· mák győgyásxatiiag elfogadható szérves vagy szervetlen savval vagy bázissal képezett sóját* vágy egy észter ptodrugjáí, IsdeplátÉ) egy inert, gyógyászátilág elfogadható exeipienst fártaltPáz, CISKtóp szabályozaiaa aktivitása vagy túiexpréssziója miatt kialakuló, az (1} inzuiirnrezisztancsa betegségek, mint 2-típusú diabétesz* X»szindróma< elhizottság* és poücisztás petelsszek szindróma; ;||i| neurodegenemllv betegségek* mint Parkinson kór* Alzheimer kér*, inntingion kór* és spináik petnodegeoerativ feeíepégek; iiangnlát zavarok* ndnt bi poláris zavarok és depressziós zavarók; (ív) skizofrén zavarok; (v) rákos bóiégsépk* mint prosztata,/hasnyálmirigy, petefészek, vastagbél-végbél rak és MLiU társnlilébkémia; (vl) gyűl ládán, (kdi) kábítészerfel való visszaélés betegségek; és (yifi) epilepsziát kezelésében való afkaftnazásM,
- 12. Az aiábbl IH-miazoí'ó-karbóáamlá vegyölemfe -H-{iid2,4-diklörbe.!iziI)"piperid.Ín-4"ilj~meíllÍ"5'ntetoxitóli4ndazoltó)'karbosaroid, és
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| MX351288B (es) * | 2012-02-21 | 2017-10-09 | Acraf | Uso de compuestos de 1h-indazol-3-carboxamida como beta inhibidores de glucogeno sintasa quinasa 3 beta. |
| US10954240B2 (en) | 2014-09-03 | 2021-03-23 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| AU2016275764B8 (en) | 2015-06-11 | 2021-03-04 | Basilea Pharmaceutica International AG | Efflux-pump inhibitors and therapeutic uses thereof |
| WO2017093157A1 (en) * | 2015-11-30 | 2017-06-08 | Basilea Pharmaceutica Ag | Piperidine, pyrrolidine and 2-oxo-1,3-oxazinane derivatives as inhibitors of bacterial efflux-pumps for the treatment of microbial infections |
| EP3468960B1 (en) * | 2016-06-08 | 2022-03-23 | GlaxoSmithKline Intellectual Property Development Limited | Chemical compounds as atf4 pathway inhibitors |
| EA202092422A1 (ru) | 2018-05-07 | 2021-02-12 | Ацьенде Кимике Рьюните Анджелини Франческо - А.К.Р.А.Ф. С.П.А. | 1h-индазол-3-карбоксамидные соединения в качестве ингибиторов киназы гликогенсинтазы 3-бета |
| CN117186027B (zh) * | 2023-09-11 | 2024-04-19 | 上海蓝木化工有限公司 | 一种糖原合酶激酶-3抑制剂及其制备方法 |
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| WO1994010174A1 (en) | 1992-11-05 | 1994-05-11 | Smithkline Beecham Plc | Piperidine derivatives as 5-ht4 receptor antagonists |
| KR19990022096A (ko) * | 1995-05-31 | 1999-03-25 | 쇼다 오사무 | 모노시클릭 아미노기를 갖는 인다졸 유도체 |
| IT1291569B1 (it) * | 1997-04-15 | 1999-01-11 | Angelini Ricerche Spa | Indazolammidi come agenti serotoninergici |
| GB0218625D0 (en) | 2002-08-10 | 2002-09-18 | Astex Technology Ltd | Pharmaceutical compounds |
| ITMI20030287A1 (it) | 2003-02-18 | 2004-08-19 | Acraf | Indazolammidi dotate di attivita' analgesica metodo, per |
| ITMI20030972A1 (it) | 2003-05-15 | 2004-11-16 | Acraf | Indazolo dotato di attivita' analgesica, metodo per prepararlo e composizione farmaceutica che lo comprende. |
| UA99927C2 (uk) | 2007-11-12 | 2012-10-25 | Ацьенде Кимике Риуните Анджелини Франческо А.Чи.Р.А.Ф. С.П.А. | Медикамент, який є активним при невропатичному болі |
| TW201040191A (en) | 2009-03-27 | 2010-11-16 | Abbott Gmbh & Co Kg | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
| US7947728B1 (en) * | 2009-11-11 | 2011-05-24 | Hoffmann-La Roche Inc. | Indole and indazole analogs as glycogen synthase activators |
| PL2817302T3 (pl) | 2012-02-21 | 2016-06-30 | Acraf | Związki 1H-indazolo-3-karboksyamidowe jako inhibitory kinazy syntazy glikogenu 3-beta |
| MX351288B (es) * | 2012-02-21 | 2017-10-09 | Acraf | Uso de compuestos de 1h-indazol-3-carboxamida como beta inhibidores de glucogeno sintasa quinasa 3 beta. |
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