HUE025466T2 - Nitro-pirokatechin származékok, mint comt inhibitorok - Google Patents

Nitro-pirokatechin származékok, mint comt inhibitorok Download PDF

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Publication number
HUE025466T2
HUE025466T2 HUE06769520A HUE06769520A HUE025466T2 HU E025466 T2 HUE025466 T2 HU E025466T2 HU E06769520 A HUE06769520 A HU E06769520A HU E06769520 A HUE06769520 A HU E06769520A HU E025466 T2 HUE025466 T2 HU E025466T2
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Prior art keywords
oxide
dihydroxy
nitrophenyl
trifluoromethyl
pyridine
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HUE06769520A
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English (en)
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David Alexander Learmonth
Laszlo Erno Kiss
Palma Pedro Nuno Leal
Santos Ferreira Humberto Dos
Soares Da Silva Patricio Manuel Vieira Araujo
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Bial-Portela & Ca S A
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Priority claimed from GB0515327A external-priority patent/GB0515327D0/en
Application filed by Bial-Portela & Ca S A filed Critical Bial-Portela & Ca S A
Publication of HUE025466T2 publication Critical patent/HUE025466T2/hu

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
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    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
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    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
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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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

Claims (4)

  1. SΠ' $0·PIRÓKATeürin származékok, mint comt INHIBITOROK SZABADALMI IGÉNYPONTOK 1. (Ij általános Xédetű vegyietek:
    ahol a képletben R? és Rs jelentése egymástól íüggeileayl hierogénatorn;; X jelentése metüérs-csopeft; Y jelentése oxigén- vagy kénatem. a értéké ö, 1, 2 vagy % és a; értéke 0 vagy 1; :¾ jelentése piriéin-N-exid esoporj as A, B vagy C képlet sxerim, amelyek égy kaeeselédnak, ahogyan exek egy jelölésien: kötés révén jelese vannak:
    ahoi a: képietekben R*, Rs, Rs ès R? jelentése egymástól: iaggetlené; hidrogénatom, halogénatom vagy Ci oalkíK Onstiosíkik C?. «.átok Cs-tí annexé vaov C&1? tioariksoeorh Cisaikanoil- vmrOw arotooöot amlno-. Cr« alkíl-amsho. Cr« diaíki-aminc?. (à;« eiSssM-amfes- vagy wes ««»r, -ww* tm^^^or,·**««»· msük Si ansn tm- vagy hetemafft-csc^ vagy anoint vagy Éöbía gyök az Ry. % M és Ur gy&soK «. együttesed mié s vagy éstércafífás#íiráM vagy aromás vagy setsroammás gyüRíkaí aikoiPskt és ebe! Fpferdése egy Mzpenti egység, ameiy s mÁmm tm válásai ki; 1,2í4-oxadls2G>i,31S-tííi; és f&*9*f93H2£4il regioteornefjei (avagy helyet: izomerjai; avagy S2^a2ët^^#i)> és aW a«zp« egység n#to«n«fpi %i$ák mindkét fűzőmért, szivek a bitem pkokatechln és a -{X}„-;V},rR:i rész cseréje révéé resíMiémék, Ute 1 tgénypmd szedrét vegyietek ik&, i^ivagyiyc áilalaass képiekéi,
    válamíÉiezek gyégyásaatííegiííöpdéai soi, add! a képíétéfe R«, R«, Rs és R? jelentése az 1, ígénygöeiban ^eghatárezott és ako! B* m F% jelentés* progêbâtorn. |, Az |* igénypÉ éiérW wgyfek, amelyek á kővetkezők közöl vlisszibSiék ki: msí1öln4ei4mximíri^ |1 .2..4joxadiazok5a;j-benzoi- 1,2-áioi; §^i3~{2-kiör»6- fnaiii'1"0xi"Piasin--3di}‘i1,2,4]oxaöiazoi'S>5!^-att®Ä2öM:,2Ai^;: «itro^eep^i-l^öi; .241ö^ediszoi^íl|beosski2-dioi; S-p;-(2-metí!-i-exl·^. ÉryÍ^öf-m©ííbpiööjfí^íí)-p<2,4|oxg^a^bS-S!^^t^beö^-15'dsöl; (1,2:4loxadiazoi-5 iäj-3-aikö*benzoi-1,2-dioi; 5~^3'(2Λ^"0ίη'=ΐ5ΐ»'1'θχ^4 trifiuor-m^täi-plndiri'a-sri'tl.S^joxgsilia^oi'ö-ri-S-fHirc-benzcn-l,2-d;ci: §-|3Ηΐ4ϊδ$4'0χ;44ΒηΙΐ44τ|&amp;βΓ·Γρβ^ 5^|3-(6-me«l-1 oxí-2~ förtí^'töS-Jör-mö^bpiödsfí^S-ily-ll^jöJoxaála^obS-^S-nibxs-beFs^ívt^öfök; 5i3-(2^íém^^eá®-1'gxApindip'3di}, 4i6-<áSrrteÖi-1 ©xi: pl}içriô‘-3^si)rf 1,2,4iö«aö^Kbi-S-ij^ro-ibéöSQÍ-'s2^öioír #3i; :&amp;{lKÏ^Éa-^Â4,8Âe^ s^^Sirsriin-3-iî)~{1,a.4joxad;szol-S' 1Π-3 πitro bensöbl :2-Öíök és Den.îOi-1;2-i3tc>L 4. t &amp; %:φ$χ®ΐ mmâ :-máf §; 1,:^ypöSi»)#V^Ä 7.1. igényponíszedn?! v«gy% erbéiy S#:í2-klér4.l3i«eiiM-ö^ a. 1 Igpnypnissgfgitysgpfei. amely &amp;iéiíq4|£$^S^ δ, 1. igénypont szenníi vsgyuíei, amely mn4^0<m-^m^i-0^^ïï^;àAp^z^Mlimzol4,2^ 10.1. i^pypont:S^ínS -is^iy -5^^^^<ί}ΗΙόΓ^ί^ΐ^^1ΐ0.χ^ρ0#ι^|^ΐ(^4|οχ^θ|<«£©ΐ·'!§^Ι^ί^ίΓφ^^32^^152*^. 11.1. igénypont szedni vegyiket, ameiy δ-Ρ-ίΡ^^ίτν'δ-ίΐΙδΓ^^^ίΐΤϊ^ΐίΟ-1-'Q^-pid^}nv3>ÍJJ4;l:^i4]oxsdía^o^grH1-$rn;!;i^ ,2-diót
  2. 12, Syôgyaszail kippzieiè, amely éli egy. az Mf, igénypontok; bárms|Éo szerinti vegyiMbők kombinálva egy gyógyászaitag eífögadhato: :lmídezóval IS. A12: ipénpopí ssgrinl gyógyászati:ks$p2teió( Ä § gyégyászsiiiag elfogadásiiöfóozé szilárd, timàftiegféÂs a sziifb készítmény pof ésAmgy tabletták Kapszóiákfcnfsáiioan van, 14: Az t-11, igénypontok feáaneiyiks szerinti vágyóiét fafesaznéisrs: aléíápSbsn. 1| ite 141. IgénypetÉst -bÉrpePí8-S2eÉ$ m0&amp; *sp 8 1I> ^ HoigémgjÉrt .szerinti ;^^t«iâ-'^^3®ââ®râ -a|p személy kszsloséhsn, aki központi vagy penféris idegrendszeri ropdaiispasségekPés szán vad IS. Az 1-11. igénypontok bármely*« szerinti vegyülei vágy é 12 vagy 13. igénypont szerinti kornpozic-6 felhasználásra hangulati rendefeessegek (maod disorder}, Afkipsop-lkóf; Psrkinaon'kAr|e;iagCi Tgnd8Ífenassigsk (parkinsonian disorder}., nyugtalan láb SZiodtgms {restless leg syndroms). gyomom és bélrendszert renssfeseségek. ódémakspző állapotok (edema femsafen state » vagy magas vérnyomás kezelésében. 1?. Az 1-1:1. igénypontok bármelyike szerinti vegyidet felhasználásra COMT ícaiecriinMmetiRrsnszferáz (catechol'-D-methyl transferase}; inhibitorként 1B Az 1-11. igénypontok bármelyike szerinti vegyidet vagy a 12. vagy 13. igénypont szerinti kompszísió fetriasználásrá: ^rkmeoo-kó? kezelésére. 1:¾ Az 1-11. Igénypontok: bérmápé szelni vegyiét vagy a: 12: vagy113, igénypont szerinti kompozt# feiasznliásra ^íirirfSön-feór i^}«g7Í reíííÍs;i«n^sSégsiH:Í^ :M Az Ml igényponMrbàîfnélyik® szabni vagyaiét vagy a 12, vagy lg: igénypont szedni kompoztöis fpésznáiásrá: nyugtalan láb szindróma kezelésére.
  3. 21. Az 1-11. îgényponîok bármelyike szerinti végétet vagy s 12. vagy 13. .génypai szerinti ikompozído felhasználásra Ódémsképzó állapotok vagy magas vérnyomás kezelésére.
  4. 22, Vagyaié? vagy kompozíció a 16. vagy fi. igénypont szedeti alkalmazásra: atyán betegekben, akik ikezeiésert mennek kereszti l-ÖOrA-vai fh-3,4ifhidro)<h1e?íihafánin) vagy egy perifériás AADC (aromás aminosau dekarboxiiáz) inhibitorral, 23, f. Igénypont szadii vegyiéi, ahol a vegyiét 3'13"(2i'dikl0r4itolrnetlito-oxi'pindin-341)41)2,4:oxaiazo05a|3-n:ifro·' benzo!4,2-dior feibasznáiésfa Parklnson-kórhsa olyas betegekben, akik kezelésen mennek keresztül l-OOPA-val vagy egy perifériás AADC Inhltotorral. 24. 12. igénypont szeri?! gyógyászat kompozíció, ahol a vegyiket 54342.idik{ór4.6toimetíA -CA'-pirléiá4-il/-[1l2.4]a^ad!á20f~ ó'!i]-3-ni?rO'benzoi-'12~dioí, toihásználasra Parkioscn-korban olyan betegekben, akik kezelésen mennek keresztül L-OOPA-val vagy egy perifériás AABC Inhibitorral,
HUE06769520A 2005-07-26 2006-07-26 Nitro-pirokatechin származékok, mint comt inhibitorok HUE025466T2 (hu)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0515327A GB0515327D0 (en) 2005-07-26 2005-07-26 Comt inhibitors
EP06008203 2006-04-20
EP06011073 2006-05-30

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HUE025466T2 true HUE025466T2 (hu) 2016-02-29

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HUE06769520A HUE025466T2 (hu) 2005-07-26 2006-07-26 Nitro-pirokatechin származékok, mint comt inhibitorok
HUS1600056C HUS000502I2 (hu) 2005-07-26 2016-12-13 Opikapon vagy egy gyógyászatilag elfogadható sója

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HUS1600056C HUS000502I2 (hu) 2005-07-26 2016-12-13 Opikapon vagy egy gyógyászatilag elfogadható sója

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EP (2) EP1907382B1 (hu)
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