SI20876B - Derivati propanojske kisline, ki inhibirajo vezavo integrinov na njihove receptorje - Google Patents

Derivati propanojske kisline, ki inhibirajo vezavo integrinov na njihove receptorje Download PDF

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SI20876B
SI20876B SI200020020A SI200020020A SI20876B SI 20876 B SI20876 B SI 20876B SI 200020020 A SI200020020 A SI 200020020A SI 200020020 A SI200020020 A SI 200020020A SI 20876 B SI20876 B SI 20876B
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alkyl
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Ronald J Biediger
George W Holland
Jamal M Kassir
Wen Li
Robert V Market
Ian L Scott
Chengde Wu
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Texas Biotechnology Corp
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Abstract

Postopek za inhibicijo vezave alfa4beta1-integrina na njegove receptorje, npr. VCAM-1 (vaskularna celična adhezijska molekula-1) in fibronektin; spojine, ki inhibirajo to vezavo; farmacevtsko aktivni sestavki, ki obsegajo take spojine; in uporaba takih spojin, kot so bodisi zgoraj ali v formulacijah, za kontrolo ali preprečevanje bolezenskih stanj, v katere je vključen alfa4beta1.

Claims (8)

1 PATENTNI ZAHTEVKI 1. Spojina s strukturo:
kjer je obroč, ki vključuje Y, monociklični heterocikel, ki sestoji iz po izbiri substituiranega oksopiridinila s formulo IV:
IV q je celo število od 0 do 4 T je izbran iz skupine, ki jo sestavlja -(CH2)b, kjer je b celo število od 0 do 3 L je izbran iz skupine, ki jo sestavljajo -O-, -NR -, -S- in -(CH2)n, kjer je n celo število 0 ali 1, in B, R*, R4, R6, R9, R^9, R1 1 in R13 so neodvisno izbrani iz skupine, ki jo sestavljajo vodik, halogen, hidroksil, alkil, alkenil, alkinil, alkoksi, alkenoksi, alkinoksi, tioalkoksi, hidroksialkil, alifatski acil, -CF3, nitro, amino, ciano, karboksi, 2 -N(C1-C3alkil)-C(0)(CrC3alkil), -NHC(0)NH(C,-C3alkil), -NHC(0)N(C,-C3alkil)C(0)-NH(Ci-C3alkil), -Ci-C3alkilamino, alkenilamino, alkinilamino, di(C!-C3alkil)amino, -C(0)0-(CrC3)alkil, -C(0)NH-(Ci-C3)alkil, -CH=NOH, -P03H2, -0P03H2, -C(0)N(CrC3alkil)2, haloalkil, alkoksialkoksi, karboksaldehid, karboksamid, cikloalkil, cikloalkenil, cikloalkinil, cikloalkilalkil, aril, aroil, ariloksi, arilamino, biaril, tioaril, diarilamino, heterociklil, alkilaril, aralkenil, aralkil, alkilheterociklil, heterociklilalkil, sulfonil, -S02-(Ci-C3alkil), -S03-(Ci-C3alkil), sulfonamido, ariloksialkil, karboksil, karbamat in -C(0)NH(benzil), R8 je neodvisno izbran iz skupine, ki jo sestavljajo halogen, hidroksil, alkil, alkenil, alkinil, alkoksi, alkenoksi, alkinoksi, tioalkoksi, hidroksialkil, alifatski acil, -CF3, nitro, amino, ciano, karboksi, -N(C1-C3alkil)-C(0)(C1-C3alkil), -NHC(0)NH(CrC3alkil), -NHC(0)N(C i -C3alkil)C(0)-NH(C i -C3alkil), -C i -C3alkilamino, alkenilamino, alkinilamino, di(Ci-C3alkil)amino, -C(0)0-(Ci-C3alkil), -C(0)NH-(Ci- C3)alkil, -CH=NOH, -P03H2, -0P03H2, -C(0)N(Ci-C3alkil)2, haloalkil, alkoksialkoksi, karboksaldehid, karboksamid, cikloalkil, cikloalkenil, cikloalkinil, cikloalkilalkil, aril, aroil, ariloksi, arilamino, biaril, tioaril, diarilamino, heterociklil, alkilaril, aralkenil, aralkil, alkilheterociklil, heterociklilalkil, sulfonil, -S02-(Ci-C3alkil), -S03-(Ci-C3alkil), sulfonamido, ariloksialkil, karboksil, karbamat in -C(0)NH(benzil), kjer, kadar je L -NR13-, lahko R4 in R13, vzeta skupaj, tvorita obroč in kjer R6 in R8, vzeta skupaj, lahko tvorita obroč in kjer R9 in R10, vzeta skupaj, lahko tvorita obroč, ali njena farmacevtsko sprejemljiva sol.
2. Spojina po zahtevku 1, ki je derivat le-te, izbran izmed estrov, karbamatov in aminalov.
3. Spojina s strukturo: 3
kjer je krog Q obroč, ki sestoji iz:
kjer je q celo število od nič do 4 in so B, R1, R6, R8, R9, R10 in R11 vsak neodvisno izbrani iz skupine, ki jo sestavljajo vodik, halogen, hidroksil, alkil, alkenil, alkinil, alkoksi, alkenoksi, alkinoksi, tioalkoksi, hidroksialkil, alifatski acil, -CF3, nitro, amino, ciano, karboksi, -N(Ci-C3alkil)-C(0)(Ci-C3alkil), -NHC(0)NH(Ci-C3alkil), -NHC(0)N(Ci-C3alkil)C(0)-NH(CrC3alkil), -CrC3alkilamino, alkenilamino, alkinilamino, di(C1-C3alkil)amino, -C(0)0-(Ci-C3alkil), -C(0)NH-(Ci- C3)alkil, -CH=NOH, -P03H2, -0P03H2, -C(0)N(CrC3alkil)2, haloalkil, alkoksialkoksi, karboksaldehid, karboksamid, cikloalkil, cikloalkenil, cikloalkinil, cikloalkilalkil, aril, aroil, ariloksi, arilamino, biaril, tioaril, diarilamino, heterociklil, alkilaril, aralkenil, aralkil, alkilheterociklil, heterociklilalkil, sulfonil, -S02-(CrC3alkil), -S03-(Ci-C3alkil), sulfonamido, ariloksialkil, karboksil, karbamat in -C(0)NH(benzil), kjer R in R , vzeta skupaj, lahko tvorita obroč 4 in kjer R1 in R2, vzeta skupaj, lahko tvorita obroč, ali njena farmacevtsko sprejemljiva sol.
4. Spojina po zahtevku 3, ki je derivat le-te, izbran izmed estrov, karbamatov in aminalov.
5. Spojina po zahtevku 3, kjer so R6, R8, R1, R2 in R11 vsak neodvisno izbrani iz skupine, ki jo sestavljata vodik in alkil, in je R1 pri vsakem pojavljanju neodvisno izbran iz skupine, ki jo sestavljajo vodik, 2-tienilmetil, benzil in metil.
6. Spojina, izbrana iz skupine, ki jo sestavljajo (3S)-3-(l,3-benzodioksol-5-il)-3-((2R,S)-2-(3 -benzil- 5 -metil-2-okso-1 (2H)-piridinil)heksanoilamino)propanoj ska kislina, (3S)-3-( 1,3-benzodioksol-5-il)-3-((2R,S)-2-(3-(3-klorobenzil)-5-metil-2-okso-l(2H)-piridinil)heksanoilamino)propanojska kislina, (3S)-3-(l,3-benzodioksol-5-il)-3-(((2S)-2-(2-okso-3-(fenilmetil)-l-(2H)-piridinil)heksanoil)amino)propanojska kislina, (3S)-3-(l,3-benzodioksol-5-il)-3-((2-(3-klorofenil)metil)-5-metil-2-okso-l(2H)-piridinil)heksanoil)amino)propanojska kislina in njihove farmacevtsko sprejemljive soli.
7. Spojina po zahtevku 6, ki je derivat le-te, izbran iz skupine, ki jo sestavljajo estri, karbamati in aminali.
8. Farmacevtski sestavek, ki obsega spojino po zahtevku 1 v farmacevtsko sprejemljivem nosilcu. 1 Uporaba spojine po zahtevku 1 za pripravo zdravila za selektivno inhibiranje 2 vezave a4Pi-integrina pri sesalcu.
SI200020020A 1999-05-07 2000-05-05 Derivati propanojske kisline, ki inhibirajo vezavo integrinov na njihove receptorje SI20876B (sl)

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US13296799P 1999-05-07 1999-05-07
US17044199P 1999-12-10 1999-12-10
PCT/US2000/012464 WO2000068188A1 (en) 1999-05-07 2000-05-05 Propanoic acid derivatives that inhibit the binding of integrins to their receptors

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SI20876B true SI20876B (sl) 2009-08-31

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NO20015419L (no) 2001-12-20
IL146312A0 (en) 2002-07-25
CA2373180A1 (en) 2000-11-16
KR100767199B1 (ko) 2007-10-17
WO2000068188A9 (en) 2002-08-29
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SK288186B6 (sk) 2014-05-06
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CN100360499C (zh) 2008-01-09
BR0010349A (pt) 2003-07-08
ATE277923T1 (de) 2004-10-15
WO2000068188A1 (en) 2000-11-16
TR200103427T2 (tr) 2002-10-21
DE60014369D1 (de) 2004-11-04
HUP0202184A2 (hu) 2002-12-28
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BR0010349C1 (pt) 2003-11-04
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