FI2044043T5 - 1-[2-(2,4-dimetyylifenyylisulfanyyli)fenyyli]piperatsiini yhdisteenä, jolla on yhdistetty serotonin takaisinotto-, 5-HT3- ja 5-HT1A -aktiivisuus käytettäväksi kognitiivisten häiriöiden hoitoon - Google Patents

1-[2-(2,4-dimetyylifenyylisulfanyyli)fenyyli]piperatsiini yhdisteenä, jolla on yhdistetty serotonin takaisinotto-, 5-HT3- ja 5-HT1A -aktiivisuus käytettäväksi kognitiivisten häiriöiden hoitoon Download PDF

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FI2044043T5
FI2044043T5 FIEP07764495.3T FI07764495T FI2044043T5 FI 2044043 T5 FI2044043 T5 FI 2044043T5 FI 07764495 T FI07764495 T FI 07764495T FI 2044043 T5 FI2044043 T5 FI 2044043T5
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compound
dimethylphenylsulfanyl
mixture
piperazine
phenyl
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FI2044043T3 (fi
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Benny Bang-Andersen
André Faldt
Arne Mørk
De Diego Heidi Lopez
René Holm
Tine Bryan Stensbøl
Lone Munch Ringgaard
Michael J Mealy
Michael Harold Rock
Jørgen Brodersen
Morten Jørgensen
Nicholas Moore
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H Lundbeck A/S
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Claims (16)

Patenttivaatimukset
1. 1-[2-(2,4-dimetyylifenyylisulfanyyli)fenyyli]piperatsiinin vetybromidisuola, joka yhdiste on kiteisessä muodossa ja yhdisteellä on XRPD-heijasteet kohdissa noin 6,89, 9,73, 13,78 ja 14,64 (*20).
2. Patenttivaatimuksen 1 mukainen kiteinen 1-[2-(2,4- dimetyylifenyylisulfanyyli)fenyylilpiperatsiinin vetybromidisuola käytettäväksi sairauden hoidossa, joka sairaus on valittu mielialahäiriöistä, masennuksesta, vakavasta masennuksesta (MDD), synnytyksen jälkeisestä masennuksesta; kaksisuuntaiseen mielialahäiriöön, Alzheimerin tautiin, psykoosiin, syöpään, ikään tai Parkinsonin tautiin — liittyvästä masennuksesta, ahdistuneisuudesta, yleisestä ahdistuneisuushäiriöstä, sosiaalisten = tilanteiden = pelosta, pakko-oireisesta = häiriöstä, — paniikkihäiriöstä, paniikkikohtauksista, fobiasta, sosiaalisesta fobiasta, agorafobiasta, ponnistusvirtsainkontinenssista, oksentelusta, ärtyneen suolen oireyhtymästä (IBS), syömishäiriöistä, kroonisesta kivusta, osittaisesta hoitovasteesta, hoitoresistentistä — masennuksesta, Alzheimerin taudista, kognitiivisesta heikentymisestä, tarkkaavaisuus- ja ylivilkkaushäiriöstä (ADHD), melankoliasta, posttraumaattisesta stressihäiriöstä (PTSD), kuumista aalloista, uniapneasta, alkoholi, nikotiini- tai hiilihydraattihimosta, aineiden väärinkäytöstä ja alkoholin tai huumeiden väärinkäytöstä.
3. Menetelmä kiteisen 1-[2-(2,4-dimetyylifenyylisulfanyyli)fenyylilpiperatsiinin tai sen — farmaseuttisen hyväksyttävän suolan valmistamiseksi () N GO joka menetelmä käsittää, että saatetaan yhdiste II [ti] jossa R' on vety tai yksiarvoinen metalli-ioni, reagoimaan yhdisteen, jolla on kaava III,
Xz Hy jossa X: ja Xz ovat itsenäisesti halogeeni, ja yhdisteen, jolla on kaava IV R e N [iv] jossa R on vety tai suojaryhmä, kanssa liuottimen, emäksen ja palladiumkatalyytin, joka koostuu palladiumlähteestä ja fosfiiniligandista, läsnä ollessa lämpötilassa välillä 60- 130 °C. 4 Patenttivaatimuksen 3 mukainen menetelmä, jossa yhdiste II ja yhdiste III saatetaan reagoimaan ensimmäisessä reaktiossa, ja jossa mainitun ensimmäisen reaktion reaktiotuote X, valinnaisesti eristetään ja puhdistetaan, mitä seuraa seuraava reaktio yhdisteen IV kanssa.
5. Patenttivaatimuksen 3 mukainen menetelmä, jossa yhdiste II, yhdiste III ja yhdiste IV — sekoitetaan yhteen menetelmän alussa.
6. Minkä tahansa patenttivaatimuksen 3-5 mukainen menetelmä, jossa X, ja Xz ovat itsenäisesti Br tai I.
7. Minkä tahansa patenttivaatimuksen 3-6 mukainen menetelmä, jossa mainittu liuotin on aproottinen liuotin.
8. Minkä tahansa patenttivaatimuksen 3-7 mukainen menetelmä, jossa palladiumlähde valitaan joukosta Pddba,, Pd(OAc)2 ja Pdzdbas.
9. Minkä tahansa patenttivaatimuksen 3-8 mukainen menetelmä, jossa mainittu fosfiiniligandi valitaan joukosta 2,2'-bis-difenyylifosfanyyli-[1,1']binaftalenyyli (rac-BINAP),
1,1'-bis(difenyylifosfino)ferroseeni (DPPF), bis-(2-difenyylifosfinofenyyli)eetteri (DPEphos), tri-t-butyylifosfiini (Fu:n suola), bifenyyli-2-yylidi-t-butyylifosfiini, bifenyyli-2-yylidisykloheksyylifosfiini, (2?-disykloheksyylifosfanyylibifenyyli-2-yyli)dimetyyliamiini [2?-(di-t-butyylifosfanyyli)bifenyyli-2-yyli]-dimetyyliamiini ja disykloheksyyli-(2?,4',6?-tripropyylibifenyyli-2-yyli)fosfaani.
10. Minkä tahansa patenttivaatimuksen 3-9 mukainen menetelmä, jossa mainittu emäs — on valittu joukosta NaO(t-Bu), KO(t-Bu), Cs2COs, DBU ja DABCO.
11. Minkä tahansa patenttivaatimuksen 3-10 mukainen menetelmä, jossa R on vety.
12. Minkä tahansa patenttivaatimuksen 3-10 mukainen menetelmä, jossa R on suojaryhmä, joka on valittu joukosta Boc, Bn, Cbz, C(=O)OET ja Me.
13. Minkä tahansa patenttivaatimuksen 3-12 mukainen menetelmä, jossa R' on vety.
14. Patenttivaatimuksen 5 mukainen menetelmä, jossa 2-5 ekvivalenttia NaO(t-Bu):a, 2- 5 ekvivalenttia piperatsiinia, 0,2-0,6 mooli-% Pddbaz:a ja 0,6-1 mooli-% rac-BINAP:a on dispergoitu tolueeniin, jolloin saadaan seos A’, johon seokseen lisätään noin 1 ekvivalenttia 2-bromijodibentseeniä, jolloin saadaan seos B', johon seokseen lisätään 1 ekvivalenttia 2,4- dimetyylitiofenolia ja saatua seosta kuumennetaan refluksoiden 3-7 tuntia, jolloin saadaan 1-[2-02,4-dimetyylifenyylisulfanyyli)fenyyli]-piperatsiinia.
15. Patenttivaatimuksen 14 mukainen menetelmä, jossa mainittua saatua seosta kuumennetaan refluksoiden 4-6 tuntia, ja jota menetelmää seuraa seuraava vaihe, jossa saatu tuote saatetaan vielä reagoimaan HBr:n vesiliuoksen kanssa, jolloin saadaan vastaava bromivetyhappoadditiosuola.
16. Menetelmä 1-[2-(2,4-dimetyylifenyylisulfanyyli)fenyyli]piperatsiinin bromivetyhappo- additiosuolan valmistamiseksi, jossa menetelmässä 2-5 ekvivalenttia NaO(t-Bu):a, 2-5 ekvivalenttia piperatsiinia, 0,2-0,6 mooli-% Pddbaza ja 0,6-1 mooli-% rac-BINAP:a on dispergoitu tolueeniin, jolloin saadaan seos A’, johon seokseen lisätään noin 1 ekvivalenttia 2-bromijodibentseeniä, jolloin saadaan seos B', johon seokseen lisätään 1 ekvivalenttia 2,4- — dimetyylitiofenolia ja saatua seosta kuumennetaan refluksoiden 4-6 tuntia, jolloin saadaan 1-[2-(2,4-dimetyylifenyylisulfanyyli)fenyylilpiperatsiinia, joka saatetaan vielä reagoimaan HBr:n vesiliuoksen kanssa.
FIEP07764495.3T 2006-06-16 2007-06-15 1-[2-(2,4-dimetyylifenyylisulfanyyli)fenyyli]piperatsiini yhdisteenä, jolla on yhdistetty serotonin takaisinotto-, 5-HT3- ja 5-HT1A -aktiivisuus käytettäväksi kognitiivisten häiriöiden hoitoon FI2044043T5 (fi)

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