HUE027811T2 - Kinoxalinon származékok mint az inzulin szekréció stimulálói, eljárások elõállításukra és alkalmazásuk diabétesz kezelésére - Google Patents

Kinoxalinon származékok mint az inzulin szekréció stimulálói, eljárások elõállításukra és alkalmazásuk diabétesz kezelésére Download PDF

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HUE027811T2
HUE027811T2 HUE09718118A HUE09718118A HUE027811T2 HU E027811 T2 HUE027811 T2 HU E027811T2 HU E09718118 A HUE09718118 A HU E09718118A HU E09718118 A HUE09718118 A HU E09718118A HU E027811 T2 HUE027811 T2 HU E027811T2
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ethyl
quinoxalin
mass spectrometry
diabetes
chinoxalin
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HUE09718118A
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Gerard Botton
Eric Valeur
Micheline Kergoat
Christine Charon
Samer Elbawab
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Merck Patent Gmbh
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    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines 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 carbon atoms of the hetero ring
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings

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Claims (6)

  1. Sæsbaâsimi iggayf^mok; í, Vagyaiét, amely a kdvetkéæb vagyületek ki£8t vaîas.2îotk 3 -·ϊ 4-k idrièad ))-1 ~{2,2-di ilxiia'etîl1 ikmx>sali?i-2( ! B)-on 3^44;iMèaïi)-l»ciki©pTôpsl-kiîHssal:i5-2(î^jN>s l -buíH>3~(4*fl«oxíeas0kmösaM8*2( 3 HVo» 3-(4-fti:orferiil)· 1 -í2í222-di:öüond:!Í)kiaexalíH-2{UI)--0!:í l'-eíi:S-6í?”d!Fa-K8'”3“(4-f]xK5,ríéTá:))kHKmaíia-2(sH)-<B5 I -eáö^-íiéw^^-kiórfeíilíkíBOxalla^ ) M)-oïî I -cskl0päx>pil”3'fe«i;ki«öx.a):äi5-2f ! 1-1)-¾¾ 1 -eii3~3~lim8v2-13~ki«ftsai3o-2( iV))-ms 1 -eiIk5-i1«oi>3-<4-üuö}fss>:8:)kä»öKÄ-2( I HH» kcikkgïfopll-3-(4-0uork^:xil)kÍHx>x3lÍK--2( 113)--00 i -bu{H-3-W-ktôrismî>kinoxaHn-2nH)-oii 3-(4 -klôrbe«2.ü )- i-ôîî î-k jfiosa1m>2(} H)·»» 3-{4-kiôfffiiSïi}'M2%2,2~{rinuôreJiJ)kinoxatin-2CS H K>« 1 “(2,2,2'·;?ί íluoretíl )--3--(4--triil8i>xm»d Ifeail .ikLai>xa)ixs--2( 1H ) -on I -(2,2-di)2soretli)-3 -(4 - Π aorie-nil ?kim5xaüss-2( ! H .s-o« :M4-klMerül:V 1 -etó-5-»fíuóriiöuxalÍ8-2( ? HVos 3-(4-kl.órfea)l:)·-1 -eiil-kin«x<!liiï-2( 's ü)-<m 3-f2-kíór&amp;ail)·· i -euVkHíSíX<ilÍR-2( 1 s O-cm I -edi-3-(4- îlaorfe?:i)ki«exal3îï-2( 1 34Vím i ~edi-3-(4-medlfeail)kÍ8í>xaf )κ-2( 3 H H»n. 3 -et5l'-3-{4-f!uor'2-a5eîdfèai3)kàâisxalîfâ-2(l >3)-<:m :! ~etsi-3 -(4-kiér-2 -met) liesM}k3aoxalm-2( 334}~os :k-0îîl-3-C4-3rSl3i»>t'fiK^iï33ertil)ksfXixa3s8-2p4-.3)--<;jR !-ïïtU-3-iV-meiVaas'e ifdkl!-iVffil)kimmaiiô- 2( 311)-(¾ 3-i2.-kdimeioxi-p[n!fiidin-5--i: M-vtu-kisoxaHs-2( i Hî-on. 3 -etil - 3 - (4- etiitsal 3 )kmoxa lia-23' 1 H)-<àJ 1-e4:.il'3'âira8-3-il-klnîXxa3:iT^-2t 311: t-oiî 3- -i3,4“d3mel:exifetii)-1 -etil-kmoxalm-^ 1 33)-00 4- -(4--etil-3-<íxa-3/Í-<ií:híílro-kía0XaÍ!fi--2-íl:)--beözoesav 3 -etil-3-( i ~nu4i 1-1 H-p!raxo3~4”33)fckmxals«-2í 1 3-p-klórfömS)·-1 -eul-kiaoxalia-^C IMJ-os 1 -etil-3-pjnd'in-3 -))-kinoxa3iö~2( S 33 Von 3 -(2.3 -diiVmds-ml)-1 -etil -kisK>xalia-2( IH Vos i-eiii-341 H-mdol -6-il íkmoxaiuk-K i H )»« 1.-etikM i H- isxk>V5-il)kiaoxalm-2( i H H>n 1 -et.n-3 -(4-iKeiill5es:xil)kisQxal:m-2(i 1-.()-¾¾ I -ei:iV3-(4-axerfoIin-4-îirxx41)kinoxidin-2(l H *m 3 -p,3-PlMdiX>- 1 :,ddíenzodsofo®-ó~í 1)- 1 -etikfoöxal io~2pM)--8S 3-(l,3-b«8zodioxol-->ii}- l-etilkinoxaiin~2nïO-<m I -cdl-3-betîziikiooxaHn -21 1 Η)-οη valamim tacém tonnái, Umimneres. enaanomerei, diasztereomerei, epimerei és jplimfojai, és ke veséké i, ésgs%pa^®Äiteg:idfi^acisatö sál
  2. 2. Μ !.. igénypont szennít vegyidet, ameers kivetkező vegydíetek kiMd választom: i-eikiop'opik3-'feiiiiK8xsi;in"2|iH)-ofi 1'Ρΐ1-3-Ρ^«οη-3-^δίΒΐη«ΙΪ^Ιίΐη0Χ0ΐ«):·2(ΪΙϊ}'<ΐη i <-td-3"{4-f]nof{èïni}kiiiisx£din-2( 1 H}~on l:-eísl-3-|é-y:8p^í^:őiíi&amp;mÍ3fes8ö3íalÍ8-2(lí-13-on 3-(4-ki&amp;iésé:î3-1 -(2,2-dîll5iOfôîîPfà5«salin-2( 1 H)-<m 3-(d-klórÍénd3- 1 Pil-klnoxalm-ât 1! l)-on 1 'eiil-3-(4-klör-2-8í«tlíléí8!)kittos3ÍÍK-2{l li>-oo valamint racém formák tantönserei, eoanîfomesei, díássáétéafosm, epimerei és polimorfjai, és kevésékei, és gyógyszerészeti leg elfogadható sói.
  3. 3., Μ 1. iggisypmrlfe#n ofogháífoözoit: vegyidet, valamim racétn fontÄ lamsfofoisi, «mmîfomerei, diasztefemssesei, ephnereíés poiímoríjai, és keverékei, és gyógyszerészeti leg eifogssdható sós, hiperglikémiához kapcsolódó patológiás áílapofok megelőzésében és/vagy kezelésébe« történd alkalmazásra.
  4. 4. sk 3. igékypopt Szerinti vegyaM, gibkőz kóáeemrfolöfo adóit válaszként az: mzalin szefcfééfo Ipsfukálásában történd alkaiptazdsrm
  5. 5. A 3; vagy 4, Igésiypoiá séétísd: kégyidétj d köyetkeÄ foegelózés#óf5és/vagy kezeiéfofeén történő alkalmazásra: diabétesz, 11 llpasti dmhétesss, meiaböiildk léndédenésségelibez kapesoiődó pátölégiás ál&amp;potök, hiperköieszterinentia, ibperlipidétmá,, amelyekét fokoz a KipetiazMliöéiaia és kipö^iikéiniai: disztipidérnia, cikkás, 'kardtovaszkuMris betegségek, amelyek tartalmazzák az ateroséklemzlsi, mfokafoiálss iseltaenöái, es a diabétesszel ősszedlggő mikmvaszkáMris Is maktövaszknldris szövődmények közül váíásrtoít betegségekéi, amely szövődmények közé tartozik az artériás kipertenziói: alemszkicfpztSj gpdiadasos folyamatok:, milrösnitopáíla, makrőaogfopátkk tednopátis és netsízspátiai valamiét hipergiíkéntk esskkentöseben tödétfo alkalmazásra,
  6. 6. Oyógyszefészetí készítmény, áfoely tartalmaz; iegatÄ: égy i -2. igénypont; szedxtti vegyidefet és gyógyszemszetdeg elfogasiiafo segédanyagot.
HUE09718118A 2008-03-05 2009-01-15 Kinoxalinon származékok mint az inzulin szekréció stimulálói, eljárások elõállításukra és alkalmazásuk diabétesz kezelésére HUE027811T2 (hu)

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US (2) US8415352B2 (hu)
EP (1) EP2247580B1 (hu)
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CN (1) CN101952258B (hu)
AR (1) AR070797A1 (hu)
AU (1) AU2009221327B2 (hu)
BR (1) BRPI0908406B8 (hu)
CA (1) CA2717718C (hu)
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MX2010009576A (es) 2010-09-24
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BRPI0908406A2 (pt) 2015-08-11
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