SI20975B - N-/5-///5-alkil-2-oksazolil/metil/tio/-2-tiazolil/-karboksamidni inhibitorji ciklodekstrin odvisne kinaze - Google Patents

N-/5-///5-alkil-2-oksazolil/metil/tio/-2-tiazolil/-karboksamidni inhibitorji ciklodekstrin odvisne kinaze Download PDF

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SI20975B
SI20975B SI200020060A SI200020060A SI20975B SI 20975 B SI20975 B SI 20975B SI 200020060 A SI200020060 A SI 200020060A SI 200020060 A SI200020060 A SI 200020060A SI 20975 B SI20975 B SI 20975B
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methyl
medicament
dimethylethyl
oxazolyl
thio
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S David Kimball
Kyoung S Kim
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Bristol Myers Squibb Co
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Abstract

Izum opisuje spojine s formulo (I) in njene enantiomere, diastereomere in farmacevtsko sprejemljivesoli. Spojine s formulo (I) so inhibitorji protein kinaze in so uporabne pri zdravljenju proliferativnih oziroma hitro napredujocih bolezni, kot na primer raka, vnetij in artritisa. Uporabne so tudi pri zdravljenju Alzheimerjeve bolezni, plesavosti povzrocene s kemoterapijo in kardiovaskularnih bolezni.

Description

* V tem dokumentu so objavljeni spremenjeni zahtevki patenta 20975 A. Zahtevki so bili spremenjeni na podlagi ugotovitvene odločbe, izdane po členu 93(1 )(b) Zakona o industrijski lastnini (Uradni list RS, št. 102/04)

Claims (29)

1. Spojina s formulo I in njene enantiomere, diastereoizomere in farmacevtsko sprejemljive soli, značilna po tem, da je:
R alkilni radikal, ki vsebuje od 1 do 12 ogljikovih atornov;
R,i. in R2 sta vsak neodvisno vodik ali alkilni radikal, ki vsebuje od 1 do 12 ogljikovih atomov;
Ra je vodik ali alkilni radikal,, ki vsebuje od 1 do 12 ogljikovih atomov in
Rzi je alkilni radikal, ki vsebuje od 1 do 12 ogljikovih atomov, substituiran 2 eno ali dvema hidroksi skupinama ali - eno NR^Re skupino ali pa sta R3 in R« združena z dušikovim atomom, na katerega sta vezana tako, da tvorita 4- do 7-členske heterociklične obroče, kjer je R3R4 predstavljen s -(CH2)n-, kjer je n celo število 3, 4, 5 ali 6;
R5 in R6 sta vsak neodvisno:
- vodik ali
- alkilni radikal, ki vsebuje od 1 do 12 ogljikovih atomov, po izbiri substituiran s substituenti iz skupine v kateri so: halogen, haloalkil, alkoksi, alkiltio, hidroksi, karboksi, alkilkarbonil, alkoksikarbonil, alkilkarboniloksi, amirto, karbamoil, urea, amidinil in tiol ali cikloalkil, ki vsebuje 3 do 15 ogljikovih atomov ali cikloalkil, ki vsebuje 3 do 15 ogljikovih atomov, substituiran s substituenti iz skupine v kateri so: halogen, alkil, alkoksi, alkil hidroksi, amino, nitro, ciano, tiol in alkiltio ali pa sta R5 in R6 združena z dušikovim atomom, na katerega sta vezana tako, da tvorita 4- do 7-členske heterociklične obroče, kjer je R5R6 predstavljen s -(CH2)m-, kjer je m celo število 3, 4, 5 ali 6; in
X je CH ali N.
2. Spojina po zahtevku 1, značilna po tem, da je: R je terc-butil;
Rx in R2 sta vsak neodvisno vodik ali metil;
R3 je vodik in
R4 je -CH2C (CH3) 2CH2OH, -CH2CH2OH, -C (CH3) 2CH2OH, CH(CH2OH)2, -CH2CH (OH) CH2OH, -CH(CH3)CH2OH ali
-CH2CH2N ali pa sta R3 in R4 združena z dušikovim atomom, na katerega sta vezana tako, da tvorita 5-členski heterociklični obroč, kjer je R3R4 predstavljen s -(CH2)4~; in
X je CH ali N.
3. Spojina po zahtevku 1 s formulo la in njene enantiomere, diastereoizomere in farmacevtsko sprejemljive soli, značilna po tem, da je:
Ri in R2 sta vsak neodvisno vodik ali metil; in
R3 je vodik in
R4 je -CH2C (CH3) 2CH2OH, -CH2CH2OH, -C (CH3) 2CH2OH, CH(CH2OH)2, -CH2CH(OH)CH2OH, -CH (CH3) CH2OH ali
-CH2CH2N
ali pa sta R3 in R4 združena z dušikovim atomom, na katerega sta vezana tako, da tvorita 5-členske heterociklične obroče, kjer je R3R4 predstavljen s
-(CH2)4-.
in njene enantiomere, diastereoizomere in farmacevtsko sprejemljive soli, značilna po tem, da je:
Ri in R2 sta vsak neodvisno vodik ali metil; in R3 je vodik
R4 je -CH2C(CH3)2CH2OH, -CH2CH2OH, -C (CH3) 2CH2OH, -CH(CH2OH)2, -CH2CH (OH) CH2OH, -CH(CH3)CH2OH ali
-CH2CH2N // ali pa sta R3 in R4 katerega sta vezana heterociklične obroče, združena z dušikovim atomom, na tako, da tvorita 5-členske kjer je R3R4 enak -(CH2)4-.
in njene enantiomere, diastereoizomere in farmacevtsko sprejemljive soli, značilna po tem, da je:
Ri in R2 sta vsak neodvisno vodik ali metil; in R3 je vodik in
R4 je -CH2C (CH3) 2CH2OH, -CH2CH2OH, -C (CH3) 2CH2OH, -CH(CH2OH)2, -CH2CH (OH) CH2OH, -CH (CH3) CH2OH ali
-CH2CH2N ali pa sta R3 in R4 združena z dušikovim atomom, na katerega sta vezana tako, da tvorita 5-členske heterociklične obroče, kjer je R3R4 enak - (CH2) 4-.
6. Spojina po zahtevku 1, značilna po tem, da je izbrana iz skupine, ki vsebuje:
N—[5—[[[5— (1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[[2-hidroksi-l-(hidroksimetil)etil]amino]metil]benzenacetamid;
4-[[(2,3-dihidroksipropil)amino]metil]-N-[
5-[([5-(1, 1dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil] benzenacetamid;
(R) -4-[[(2,3-dihidroksipropil)amino]metil]-N-[5-[[[5- (1,1 dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil]benzenacetamid;
(S) -4- [ [ (2,3-dihidroksipropil)amino]metil]-N-[5-[[[5-(1,1 dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil]benzenacetamid;
N-[5-[[[5-(l,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil-4-[[[3-hidroksi-2,2-dimetilpropil)amino]metil]benzenacetamid;
N—[5—[[[5—(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-(1-pirolidinilmetil)benzenacetamid;
N-[5-[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksietil)amino]metil]benzenacetamid;
N—[5—[[[5—(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-(1-pirolidinil)etil)amino]metil]benzenacetamid;
N—[5—[[[5—(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksi-l,1-dimetiletil)amino]metil]benzenacetamid;
N-[5-[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-3-[[ (2-hidroksietil)amino]metil]benzenacetamid;
N—[5—[[[5— (1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-3-[[(3-hidroksi-2,2-dimetilpropil)amino]metil]benzenacetamid;
N-[5-[[[5 —(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksi-l-metiletil) amino]metil]benzenacetamid;
N—[5 —[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[1-[(2-hidroksietil)amino]etil]benzenacetamid;
N-[5-[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[1-[(2-hidroksi-l-metiletil)amino]etil]benzenacetamid;
(S)-N-[5-[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksietil)amino]metil]-a-metilbenzenacetamid;
N-[5-[[[5-(l,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-
6- [ [ (2-hidroksietil)amino]metil]-3piridinacetamid; in
N-[5-[[[5-(l,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksietil)amino]metil]-a-metilbenzenacetamid;
ter njihove farmacevtsko sprejemljive soli.
7. Spojina po zahtevku 1, značilna po tem, da ima formulo N—[5—[[[5—(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[[2-hidroksi-l-(hidroksimetil)-etil]amino]metil]benzenacetamid in njene farmacevtsko sprejemljive soli.
8. Spojina po zahtevku 1, značilna po tem, da ima formulo N-[5-[[[5 —(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksi-l,1-dimetiletil)amino]metil]benzenacetamid in njene farmacevtsko sprejemljive soli.
9. Spojina po zahtevku 1, značilna po tem, da ima formulo 4-[[(2,3-dihidroksipropil)amino]metil]-N-[5-[[[5-(1,1dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil]benzenacetamid in njene farmacevtsko sprejemljive soli.
10. Spojina po zahtevku 1, značilna po tem, da ima formulo (R)-4-[[(2,3-dihidroksipropil)amino]metil]-N-[5[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil]benzenacetamid in njene farmacevtsko sprejemljive soli.
ϊ
11. Spojina po zahtevku 1, značilna po tem, da ima formulo (S) -4-[ [ (2,3-dihidroksipropil)amino]metil]-N- [5[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil]benzenacetamid in njene farmacevtsko sprejemljive soli.
12. Farmacevtska zmes, značilna Po tem, da sestoji iz spoj in po zahtevkih od 1 do 11 in farmacevtsko sprejemljivega nosilca. 13. Farmacevtska zmes, značilna po tem, da vsebuje spoj ine po kateremkoli od zahtevkov od 1 do 11 v kombinaciji
s farmacevtsko sprejemljivim nosilcem in sredstvom proti raku v določeni količini.
14. Farmacevtska zmes, značilna po tem, da vsebuje spojine po kateremkoli od zahtevkov od 1 do 11 v kombinaciji s farmacevtsko sprejemljivim nosilcem in modulatorjem transaktivacij e p53 v določeni količini.
15. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z modulacijo apoptoze.
16. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo protein kinaz.
17. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo ciklin odvisnih kinaz.
18. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdc2 (cdkl).
19. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdk2.
20. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdk3.
21. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdk4.
22. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdk5.
23. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdk6.
24. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicij o cdk7.
25. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicij o cdk8.
26. Uporaba spojine po kateremkoli od zahtevkov od 12 do 14 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje proliferativnih bolezni.
27. Uporaba spojine po kateremkoli od zahtevkov od 12 do 14 za izdelavo zdravila, značilna po tem, da_se omenjeno zdravilo uporablja za zdravljenje raka.
28. Uporaba spojine po kateremkoli od zahtevkov od 12 do 14 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje vnetja, vnetnih bolezni črevesja ali zavrnitev presadkov.
29. Uporaba spojine po kateremkoli od zahtevkov od 12 do 14 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje artritisa.
30. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje nepravilnosti povezanih s ciklin odvisnimi kinazami.
31. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje alopecije, trombocitopenij e in mukozitisa povzročenih s kemoterapijo
SI200020060A 1999-12-15 2000-12-07 N-/5-///5-alkil-2-oksazolil/metil/tio/-2-tiazolil/-karboksamidni inhibitorji ciklodekstrin odvisne kinaze SI20975B (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US09/464,511 US6262096B1 (en) 1997-11-12 1999-12-15 Aminothiazole inhibitors of cyclin dependent kinases
US09/616,629 US6214852B1 (en) 1998-10-21 2000-07-26 N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
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ATE294800T1 (de) 2005-05-15
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UY26480A1 (es) 2001-07-31
US6214852B1 (en) 2001-04-10
CO5251464A1 (es) 2003-02-28
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CA2394544A1 (en) 2001-06-21
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SI20975A (sl) 2003-02-28
CN1433415A (zh) 2003-07-30

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