HUE030400T2 - Ciklusos amidok mint MetAP-2 inhibitorok - Google Patents

Ciklusos amidok mint MetAP-2 inhibitorok Download PDF

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Publication number
HUE030400T2
HUE030400T2 HUE13711291A HUE13711291A HUE030400T2 HU E030400 T2 HUE030400 T2 HU E030400T2 HU E13711291 A HUE13711291 A HU E13711291A HU E13711291 A HUE13711291 A HU E13711291A HU E030400 T2 HUE030400 T2 HU E030400T2
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tris tris
compounds
formula
compound
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HUE13711291A
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Inventor
Timo Heinrich
Frank Zenke
Mireille Krier
Manja Friese-Hamim
Jeyaprakashnarayanan Seenisamy
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Merck Patent Gmbh
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Publication of HUE030400T2 publication Critical patent/HUE030400T2/hu

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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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    • A61K31/402—1-aryl substituted, e.g. piretanide
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Claims (6)

  1. «MtaVfl IGÉNYPONTOK
    S , î k ép le ai V egy ületek i amelyben R jdentése NR2R\ Alk, aCH:i){Ci^hlAr, HeÉ. 0[(.'(ίΓ);·j^AR vagy OA. X jelentése CO vagy 0¾ Y jelentése CÖ vap 0¾ R’ jelentése II {CH2)„Cyet [CfR4}, ΗΟίΧΙΗ, [CCRÓéAÖNHArk jC(R“);]i:CöNH?. [CűOy^BA. [QilÔ^^.OÇCCÔj^. [0(¾4¾]¾ iCíR^HCOOiCH^A^ [ΟίΙ^Ι,ΟΟΜΗΗΚ^,ΙρΟ»]^ [CiRÓjj;X.X>NHCR4[iCrí/)!(N{R'%jGOA;(Rí)s. R; jelentése H. [0(R4}?]*M (CHj}flCOHeí!, {0Η?.)«00Α^,|0Η^Α^ vap PlO*», R* jdenlése OH vagy OCöA, íO jelentése M vap alkil 1,2, 3 vagy 4 0 atótnmal R3 ès R4 jelentése épüli alküés 1, 3,4 vagy 3 Ç aionnnal, alni ep CHj csöpri helyett N(CH0,«OH vagy SO? is állhat, R\ R^ jéldiOse epéíikéatis: egymástól függetlenül H. F vagy A, R4 Is R* jelentése együtt aíkiíén:¾,¾ 4 vagy I: € atonnnaRalókégy OHj csoport helyett NCÖA vagy 0 s>; állhat, R7 jelentése H vagy A, Ar* jelentése fenil,· amely sauhsätttallätlän vágy mene-, di-, tri-, tetra- vagy pemaszubsatiiuáh Hal, DH, OA, CONHá, OONHA, CONA*, 1PÍ»>A, CÖMMCyo, NHSQjCye, GONHAr2, COlW és/vap NASOjA ssmhxztituenssd, Af5 jelentése fetal, arüeiy saabsztítisálatlán vagy mono-, di-, tri-, tetra- vap perslasarfesatituâlt Hal, A, 00141¾ p/väp OAH sáufesztiménssél, Al jelenlêse fenti, MfH szuhs^ínrerssaei, Met jefemése mono- vap biciklusos telített, telile;leu vagy aromás heteroeikius 1 - 4 N és/vagy O és/vagy S atommal, amely srunsztkuálaüan vagy mono-, di- vagy ímzubszíituált Hal, A, ÖA, CN, AH2, NHA,:Ä:54405,€N, OOÖH, COOA, (CíD.-CONtF, (Cl ILONKA, (OHOoCOXAíf N! ICO V COA, CHÖ. HcÀ SO>A, SO?Nlk, SOjNHA. SO;NA3, COMIMF, CONHAr, “O ês/vagy Ar Nztsl's/iitueH-sseC I le11 , döntése monociklusos telített heíeroeiklús 1 - 4 N es/vagy O ést vagy S atonanak amely a/nbs/uUsaiatlam vagÿ mono-, di- vagy triszuhsztiiuált ::;0 és/vagy C()0A xzubsztit nenssek He· je)cntése ixoindoiil, \ jelentésé egyenes OH, CHO, COA, COOA, ON, CONA?, CÍM81 is/vagy CÜNfkB állat, ê^va^«0!fNR.«gÿ'y8iy kát nem szomszédos CH és/vagy CI% ©söpört helyett O is álilmt, vagy Cyc, Alk jelentése aikenU 2, 3. 4,5 vagy é C atoMBiaí. Cye jelentése ciklusos alkil !-? C atommal, amely szdbsxíítuáladsn vagy mono-·, <Üt> vagy triszubsztiruált NHCOA, Ni» OH, OA, A, M%* NHA, NA2> C0ÖA, COOH és/vagy CONIfA szdbsztítueiissei,: Hal jdientéís© f, Cl, Br vagy ,1, m jelentése 1, 2, |l vagy 4, π jelentése 0, 1,2, 3 vagy 4, p jelentése 1, 2 vagy 3, valamint ezek; gyógyszetészetdegalkalmazható sói, ta&amp;ipmer .és ékek tetszőleges arányú keverékeit,-ahol ki vaunak zárva a kővetkező yegyiíeték’ o:iedb345idroxipiperidií:t'3'-karbi:!xíiát1 lAéíudiiíblOmjetil Siydïkjxipiperîdid^ J^ilsartexillk terc-butil"3-aUíi-3-hi«roxipirro]idín-1 -karbuxdät, terc'biuil-3'allíl"3-hloroxipipeddín-i karboxihit.
  2. 2, Az 1. igényponiszerintl:' vegyöletek,. amelyekben. Hét jelentése pijíaziml, pirazolil, betízimidgzold, piridil, ipdölil, dilddroindoltl, benzofttranii, tetígiiidropiíuml, dilildrokldóíidii dihidrdlzbkii5biiiulí: tetnshídrok555olmik tetráhidföizökmolhbi, índazolsk iimidazblih pltTplÜ, oxazöíil, oxadiaxolil, izoxazold, benzotiazolil, pjperidhMdi, pimdidin·' óik 3,4-díhídro ~ΊΙ-ρη «.»>[3,? b IgHoxazíník 3,1 >h ' om 311 be /ο 1 ow od, berLzoiiü'aitil, a/duhnü. 3-sizahieik)o[3.2.0]hexii, pirroloí3,3-b]piridini 1, tetrahidrofuranil, tetrahidr©*! »imaüridjöjlj d.iCdíhtdrobenzoízotiazoUk » ,2*lr4“tetr3h}drobeo/otiazmii vagy hexahldrobenzo-! ,3Atioxoiik«gyen* két5i valamennyi xzubxzdraáíaílan vágy mono-, dl- vagy íríszubszlituált Hal, A, OA,:0NvNH2s ΝΜΛ, N'ku N();, CN, COOH, COÜ (CH^CONHj. (CHy)„CONHA. (CH3)„CONAn NHCOA, C0A, CHO, let5, S03A, S0*M!%302NRA, SO.>NA2, CONHNH:, CONHAr', ===0 ésAagy Ar:i szubsztituenssel, valamint ezek gyógyszer észetileg alfedmazhaiö sói, tautomer és szlereoizómek Ionnál, beleértve ezek tetszőleges arányú1 kévétekéit:.
  3. 3. Az 1. vagyigénypont szened vegyületaii, amelyekben Hét' jelentése piridtszimk puazoliL pirkiíi, plperazlnit, ibrik tlfeml, imidazdli'k pÚTotíl> oxazoük oxadiazoltl, ieoxazoíik bazélil, triázelik tetraxöld, tiadiazok pipcridm-] dl pi.rroiidin-1 ~il< tetruhsdropiranih I.2--iAazinam2-iL 1,2,5-osadiaxinait-2 -í 1, 1 J-osazinan-d-ü vagy hexaididi^piriHndlnií égypnké&amp;t vagy mötiö*,; dk Vágy tti&amp;zutatltnák A és/vagy ÛÀ sxobsztibtenssel, Yákmmt eaekgyöiysxerés^eiüeg alkalmazható sdiiíaBiomer#S2terepiz0mer formái, beleértve ezek 1 ets/öl eges atáiyl iéveíékéii 4'í:-.Az í, igénypont szerinti vegyűletek. amelyekben R jelentése NR"!R4. Alt Cr^^lH-OtaR^blArÁ/Hét^OOT^j^Vagy^. X jelentése CO vagy CIL·, Y jelentése CO vagy €11?« R; jelentése ík [C(R<h]fiAri, iCH;)„Het, ((dldhCye^iCiR^^COtDM, [€(R'j2jfiCabíMAr', fCCRÁjRCONH:, ÍCiRlfoNHA, [ClR^laNAfcOpl^i^ijCpl^OR7, [C(.R4)jfeC»· (CHA:,Ar? [C(R4 pjX.'OOA, [C{R%]flCONlI[C(R4)dP-CON(I^vagy [C{R'1>.:];;CONHCR‘1[(CHj}„N{R4)j']C’ÖN(R4}í, R1 jelentése H, [C(RA,j;1Ar\ {CH^COHet', (Cl^OSM R? jelentése OH vagy OCX) A, R" jelentése 11 vagy alktl 1, 2, 3 vagy 4 C atommal, R és R4 jelentése együtt alkilén 2. 3,4 vagy 5 C atommaî, aíM egy 0¾ esopotl Helyett N(CH;;)i«OH vagy SO; is állhat, R \ R* jelentése egyenként és egymástól foggetíeutll H, F vagy A, R' és R0 jelentése együtt alkilén 2,3,4 sttgy 5 C afoínmai, ahol e0;.CÂ:'isdRO!É%élyett HCOA vagy 0 is állhat, R' jelentése M vágy: A, Μ! :MteJy mtbsztRuáiadan vagy tnottor, dR, tii-, tetra- vagy petnasxubsaíitualt ttal, OU OA, ΓΟΝΗ;. CONIIA. COM V, \1IS0}A. COMlCvc, NÍISO-Cye, CONHArx COHek étvágy NASO.;A saubsatituenssel. Árjelentése fenik amely szobsztitnátetlnn vagy mono··, dl··, tri-, tetra· vagy pentaszubsztituált Hal, A, CONlk és/vagy OAr' szbbsztituenssek Ar4 jelentése fenil, amely szobszliútálatltm vagy nronosxuhsatttttlltMH; szübszîimemïsei ítét jelentése pitazinilsptM^ piridik tétralsdtppimntl, diMdrbkfoolMkdtlhdt^^ tetmlndrokinolimk tetaabidrofodkiinólmik ifcdäÄlyl^iteohl, pirrolik okääsolU, oxadlazolii, izoxastdÜi, Ise^Ktïtil^oOJ^^p^iiîér^^Pkipli^întiidin-i!*Uy $j4é$iMár0-2H·ρ1π0ο[3,2^}Κΐ,4“0Κάζ1|1|| 3,4-dibidm-2H-benzó-l\4-oísáemík benzoforanil, azetidinü, 3 -azabici klo[3.2.ö]hexü„ plrrolo[2,3-b jpiridiniU tetmRidfil^a6iirtétttbldrő*Íj^tmÍiíidíni^ 2,3-dihidrO'benzoizotiaxaíil, vagy hexahidrobenzo-1,3-dioxoiiL egyenként valamennyi szübszíifuáláilan vagy mono-, di- vagy tnszubsztituált Hal, Λ, OA, CN, NHg, NHA, NA;í, NO,. CN, COOH, CODA. tCHj)ftCONlK CCÜ-}„CONHA. (CHdXONAj, NHCOA, COA, CHO, Met’, SOy\, SO;.NH,s S02NHA, SO A V, CONHNHj, CONMAr’, -O ésAagy M( szubsztituensseL Hét- Jeient^epirMa^ÄpteMSI pMdi% pipem-dmi, morMiniipiBibiÄib: fbril, tienil, mhdaxotil ρητοΐιΐ, oxazoMl, oxadiazôîiÇfeôxaâôlii, tiazoíö^M^íiyMiiliilipiádiaZö!, plpeodimHh pirro.Udin-1-il, teírahkiropinmil l,2-oxazman-2-i!, l,2.S-oxadiazinan-2-Ü, 1,3-oxazinan-3-ü vagy hexahkiroptfimldiml, e^^iÉ^'^fefne«»yiszutóft#W»s:'.»^:pono«, dl- vagy trisznbsptoált A és/vagy ÖA szubsztiUtenssek lier jelentése izomdotil, A jelentése egyenes vagy ellpzl alkil ! -I 0 € atommal, amelyben i-7 H atom helyett F, CL Br, OH, CHO, COA, CODA, CN, CONA2l CONBA és/vagy CGNH? is állhat, és/vagy amelyben egy vagy két nem szomszédos CH és/vagy CMj eaoport helyett ö is lilhah vagy Cyc, Alk jelentése alkeni! 2, 3,4, ő vágyé C atommal, lejelentése ciklusos alkil 3^7 ColomiML amely ssÉfsztltPlatlan vagy mono-, di- vagy trísjrubsztnuált NHCOA, ®SCb, OÏL OA, A, NIC. NHA, NA2, COOA. COOH és/vagy CONHA ssmbszutuensse!. Hal jelentése F. Cl, Br vagy I, s n j etentése 1,2,3 vagy 4, n jelentése 0, 1, 2, 3 vagy 4, p jelentése i, 2 vagy 3, val§]ÂI^#:i^^SÂiteétileiiMbi^hàtd soi, tautomer és sgtemoizotner formái, beleértve ezek tetszőleges oMoyÉ jke veréke il-
  4. 5, Az 1. Igénypont szerinti vegyietek, az alábbi csoporttól megválasztva i Vegyitie! Név száma >!AS6" (S)-3d!,l-Dioxo--.L6-tíomorroiín~4~karbonilV3-hidmxi-l-tcnilpirroHdm*'2-on f "A ST- (S)-3-Hidroxi-3-|4-t2-htdrexieti!)piperazin-i karbonilH -tentlplrrolidin-2-Qn ; "A58n N-(3-lnttdazôiA-iipropitî4S)“3-hidroxi'2"Oxo-l-ferùlpinOhdin--3-karboxamid ”A59" NN(243imetílamínoeti|)-(S)vI-hidmxi>,24>xö-14enilpin'olidín-3'karboxttmiá !'A03" N-|.244~Fenoxtfenil}etirKS)''3''hidroxi-'2-o,xo-1 -remlpinxdtdm''3-karboxamid : "A61 ” N"[{2,Dimetiiamihoeiil)metil]-(S3-3dtidmxi-2-oxoO -ÎemlpinOjidtnOAaAoxarmd
    .6. Eljárás, az i~3, igénypontok sprinti i képletü vppöietek, valamint c/ek gyógy szerészeiilog alkat- mazliaié sóL tautomer és sztereoizomer femái eiőáiistásáru,: aKKaÍ|e|loníezve, hogy ay oIyáaXj^Íeilw§yöí#^c.előállításához, amelyekben Y jelentèNe CO es H jelentése NRR \
    Π képletusegy eletet §i amelyben X, R\ R\ R\ R\ R: es p jelentése az 1, igénypontbanMegadott, és L jelentése CL Br, 1 vagy szabad vagy reakcióképesen: áiíimmnálísanm»gv|ltoztatott OH csoport, III képietíi v^gyölettel rsagaltalunk Ärf m amelyben R~ és R4 jelentése az 1. igénypontban megadom vagy
    b) IV képlet« vegyúieist ÍV amelyben Rk R\ R’:>, R:, R. X« Y és p jelentése az 1. igénypontban megadott, oxidálunk, vagy e) olyan I képletti vegyületek előállításához, amelyekben. X ás Y jelentése CHj, olyan ! képiéin vegyületek amelyben X és Y jelentése CO, redukálunk, és/vagy 1 kéjdetű bázist vagy savat sóvá alakiunk. ?. Gyógysze.rkészínnésw, amely legalább egy,: az !··5. igénypontok szerinti (!) kép le tu vegytiiétet ég/vagy ennek gyógyszerészctiíeg alkalmazható sójá|yMlíií«W'::Vá0''íblölájáh bélééfte w ezek; tetszőleges arányú keverékeit, tartalmazza adob esdiaen hordozóanyag éslvagy segédanyag mdiei. :8. áz4»&amp; Igénypontok szerinti I képieiü vegytiletek, valamint ezek gyógyszerészetileg aikálmazbaíő só|a, íaatomer vagy sztereoizomer lbmrái% beióértve ezek tetszőleges arányú keverékeit, tumorok, tumor áttételek, ,a: mesangial is sejtek proliferativ betegséget, hemangioma. proliferativ retinopába, reumás izületi gyulladás. aterosvddemtikus neovaszkularizáció, pszoriazts. okulárig jteovaszkularizáció. oszteopotozA,: diabétesz és elhívás. í indáid ieuk|tKÍ^1ÍT:ná>ö^^:malari.a c« prosztaihi pertro l la kezeiéiben történő alkalmazásra.
    0. A A igénypont szerinti vegyületek az: adóit alkalmazásra, ahoi a tumor betegség az alábbi csoportból megválasztott: pikkelyes, epithelium, hólyag, mmmor, vese, fej és nyak* nyelőcső, milipyak, pajzstnIrigy, bél. mi), agy, prosztata, húgy-ivarszervi traktus, nyiroktetidszer* gyomor, gége, tödő* bor tumor, nmuosejfes íeukéiUta, tüdő adénokarcinoma, kissejtes tüdő karcinenuu hasnyálmirigy rák, gíioblasztoma, mell kareluőíüa, akut tnieloíiküs leukémia, krónikus mielotifeus leukémia, akut limíMikus leukémia, krónikus iimiaükus leukemia, ikaigkin-limkuna, nem ifodgkin-iindoma.
  5. 10. Az 1-5. igénypontok szerinti I képletü vegyületek, valamint ezek győgyszereszciiieg alkalmazható sója, tumorok kezelésében történő alkalmazásra, abol egy 1 képiéin^ yegguiet teripiasan h meímylaégét egy vegyülette! .ai»ély: 1) őszrnageu receptor modulátor, 2j androgen receptor modulátor. 3} retinoid receptor modulátor, 4) citotoxikum, fj antiproíiierativ szer, (}) prcnil-protetn taroszferáz inhibitor, 3} iiMGA3ô$t*^dfâ^ S)'HIV-pioieäsrziÄbitor, 9j reverz transzkiptáz inhibitor, valamint 10) további ^ttgldptlé^'lilllMíöif'öSöportből megválasztőtb
  6. 11, Az 1 -S igénypontok szerinti 1 képié# vegyületek, valamint e^,pógyszeré$z#ieg.iII#liEP^Mé: sáp, tumorok kezelésében történő alkalmazásra, ahol egy I képiéin vegyidet terápiásán hatékony mennyiséget radiotétáplával és egy vegyületté! kombinációban adagoljuk, -amely i) ősztrogén receptor modulátor, 2) androgen reeéptor íPödulálbr, 3) retinoid receptor modulátor^ 4) éitőfökiknm, Sj ardipíolilerativ szét, d) prenil-proteín tamszferáz inhibitor, 7} HMö-CoAredukiáz inhibitor, 8) HÍV-proteáz inhibitor, 9) reverz transzkiptgz inhibitor, valamint 10) további angiogenézis inhibitor cm>-pattból megválasztott.
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