HUE030794T2 - Dihidro-pirido-ftalazinon-származékok szintetizálási folyamatai - Google Patents

Dihidro-pirido-ftalazinon-származékok szintetizálási folyamatai Download PDF

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HUE030794T2
HUE030794T2 HUE11740513A HUE11740513A HUE030794T2 HU E030794 T2 HUE030794 T2 HU E030794T2 HU E11740513 A HUE11740513 A HU E11740513A HU E11740513 A HUE11740513 A HU E11740513A HU E030794 T2 HUE030794 T2 HU E030794T2
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fej
compound
formula
acid
methyl
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HUE11740513A
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Bing Wang
Daniel Chu
Yongbo Liu
Quan Jiang
Lei Lu
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Medivation Technologies Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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 only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/06Peri-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Claims (6)

1. MédSSSî· 4 }'áy Mppgí Vágyáig
•IlllliiSi; Πλ vagy|ä égy aà|ï3 aldiiMalísk aMk s rnadsae? « kàvaPeadkbd; âi; ss 4;-óv lépjaiá átgyilglái:
(5), vagy emsak spy ·§ϋ# IddssPsasedpgisrsMal magákafái ahaä & pleads« SS-aikii ápol m: vlpös képkáP vegyviais! vagy asaak sgjél ágy ék&k silk aogy a iggss kègfetâ vagypaívt
|4 4 vsgy ásnák agy spÉ pgqkékiskP ê§ WW vágy ágy Lawís-sgy JsiegpiglPg fá^apggk, aköi R spárgása ϋΗ'8'aM. 2, .¾ 1 Jgésíyggní sagdpti: aiggsgag adói a ;adak;5i«asa; a) agy fgmsgaiogga^/sips aggg y aagîaa a fgnplpfegspg TiÇiS vagy SaQil vagy b) vsspöt. vagy al gpsogén agy ^aPáíasváías jafeaitálsaa, sági *oaU vsPkea a parkaplisafe a Kaassrao cvogaráP: váiassfptk palMam.. rákap ás piaiba; vagy <!} MCN8H3. ahol Ma kávét*«* osoppt váis«tett: y. Ns: Kés 8s4bi. , . ,,.Λ . S. Αχ s. tgènypb «eàbs rsábsssy sh«: a ssvvsy sav a köveiké csaíx<?tbói vasasa: HCi. Hör. mf;-h^y4·** H3P04. 4, mCagy sxsrm táv a kèvafcszâ csep&amp;ïlbêi viasza·; ^mmm», vajssv» febyor-s^isav, p-ioïvalsjoivsiisav es n^PPfcnsav: vagy b) aboi a Levis· sav a kévô^ad ceoponixs v^?«:íA{Ci3, .TíC;4 ^Ci4. sab ZnCiJ
5, Az 1 #aypoa; abci a i4m» taps» vegyül»** vagy *«Κ·«ά$$ % **>* m? â $*** *ô$^· végÿiMèb
(3K vggy m «W* m sav Kte&amp;ése» S-OH-vss üs5# ahol R a kavard csontból vágott, mű P; p(p ippropi butít âs isobutS; és s sav a kévePzO «soporSP vaitmbb: HD. atslsav. p4o:Psv:;Pe$av és eiaoH^taav, 4 Ár * > XX^ * s'e X * sto** *>? a 4 î* -¾. ^ ''Λ* <> '* *' açv a - s , ' » \- a - w κβριρ v«ovùS(?M:
(Í műmnek «l '«*» ui-1,2.4-^^*5-safb^^ <μ£*ι$*.
7. A δ. :çàfîypont szmtè m a ks^^as kosyiinény â ***·»»&amp; jafesb: agy fete? hasznába v^esukSi w Jpaièfâbea kóréibetüt 60 as 90 X *ëzm aho! a fete aao8 aPPt thiamin és a vbsaegkôiè mt · -jv· v< I: Métisse? &amp;ε i l H* sépleSs vepypj:
t(l)v ,5 (8}·§>% k*H&amp;*ïû
(8), V8g §gï«séiâr^¥.:feMSsi ħ«i|äu c; a 8, igényper $£Âi méáíef, aho= s ös^í> &amp;ït s; 3ïioî s (ényksHXÍOás ado* a*s3>s« a kávetkszö v<,op*;!0öi vaSasaot:: ^abCO'i K2C03 ô? C%2C08 vagy bï aiu2 a ián>!2ádd addteseihao N&amp;H vggy HH. 10. Ä? » i$H* «W®·** VÎW #«* ^ fc&amp;jak «t* kogv s (?}$$ tepielMßfefeft?
ÏÏh '.' '? ^-î-yi'ù! \ *:&amp;'">> ! \y^as A' ^ »-""-Λ ^aalù vagyáé' ^a*y ^ad, «1 fesgy a }>' - y6§ÿp#5k
i.>n va§ftm«Ée<?y soiâi egy sav *gag»juk} ^*i«»d&amp;«MÉp umé^^ed^ vài^Â^savgMfesciàfesv# HCl ¢3 pHoiuolsiriilfefisav.
18, Mtes? as (1}.¾¾ kâpietO v%§yi|ï«&amp;
ί'5 \ C'Uj vagy wak «gys-pfa slagiiaagfey Pel· s aiáassa a si: ai (Ca» kégieSü v%gy;.ás>sí:
(5), yggy ef;:*:?:·>·. agy spjéthrldîàïgÎfÎ-mèïf'îôhldrêlfsïî algáiknak. aks? R Jgkídksya 01·<:8ν#4 apai sz |Sj:% kàpMp vagygiglatvggy sgagk sóját ágy Pipák *21, Η<%$ g (iPgg Hapsi vggyigte
(9), vagy esnék agy sóját agy mag oCsgsapsn agy mdgkaiosaastei avsgánpuk kotgipeidi Q ég 148 ':C kpgsltí timêrsèkifePîé, kêpbgif Ces 4Bóía kökdít; ÄärPÄ körgadös; apP R Jéígalgae CiRCCgRil. 1|. Aa 12. ?g&amp;í:ypont avednk mods», aboi a fediRCPsaar al agy fègvbgdydrki. áf®s a#!fö§aSea alM^dPapd RaBH4 vagy CgCCBHS; vagy p vaspör; vagy a) T;CC vagy SnCC. vagy d) hidrogén agy pmppifé® aPgkeéRl gsaibaa ga ataienak %® a pvsiap cgaggr&amp;á! vliaacötk pliêfpp mkkekia piagaa.
14. Modakar ál (1)·'©8 képiatü ysayalèt:
íl% vagy ennek Sgÿ gps eltekátea. shoi antetersktePSÄtiP áll: M |§}PP képei vagyuiste
vágy snmp agy $δ§|1pagils§ak; ai5p R pfápáss Clpptei ansi as sptekêpei yágyníáleiyaiy anaat: aóját úgy pipák sis, Slgy a Π 0) -es képsi vëgpièM
{10 K vagy ennek s§y sept agy mdu kälteste teSPite· gap R ipsa psg Pi-PPapI. IP az tg, igéaypsnt ss&amp;Nati aPïisagk ahP g teakPStek al saspn vagy p agy fênviètend ; : ahi adat! eseten a SámPáPinl Ra8H4; y eg y p PÉôgèa sgy átmeneti te pieniéîéSem iÉai aded eseten aa âimsnsk îlrn a kôtekte eseggrte teasaipk tePÄRn Pkki ás pains,
11, Aa 14, igeeygeai saeriei m&amp;àœmÆ®-à (löte képiéi vegyteist vagy snnsk spàî lay álljak sip aogy a pyes képei yegyiaiât "î:· k -y- y" (/> f- p ;k J§ I I I 11 * 1 1 *: 1 8 I fr- S' S: -SS: ψ % f Ï ï S- I: I 1 I * f i 1¾. * ff if 3 O rn S S ç
".V; S IS ë> SI- i? 8 s if
·;; 8 s S o s· S ,¾
i f f « i : I 111
&amp; B 8 I :~r % to I c: « s S ff Ψ w S si i f- i £ ti Ilit f s fii i ' f t i f f % 1 f 1111 I I f t I Í f f I § ë &amp; ky Ψ "X sr. S· ··.» O g &amp; ,,... a t » II i : r f f f :k. m ív- %L· Ä I i i: t S t i i· i I I il: Q g· g: If *ξ y SV » 0 B if' I If " i 8 ivr» w ?>> <<\f s**' if; i 1111 ? ! .Ç cy· ΐΰ· ^ ^ ® i if 1 8 ! I 8 § :f III f I R S I I I f s I i p ï e I S T f: g 8 self
(ό;ύ »aj* «MMi «w sasi a***·» MMtHmààmm&amp;Çk. m r i ******c !'c'5'Ää S A 18 «w* «MT. s»i * '« ««. «*> «rnt «swa*» « ä,!"·*Ä ·“» **» felbontást végïwnk «
(5). *. a ?ö, wnon mom^r. *»*§» iMst^ al isolt çÿelbeo o nasser tartalmasa mèc agy kiáss m tos marnám <s. anoi a kiraás ásó **"> '-Η · '"'" ’ 'Kw ockfep fitiol nácit cwíhcn a GH;RAoKAK$je$<ooís K/ vs§y AV >·*&amp;* ( ^. .f ^.,.. ,;.T. fej a*« «w» a «wm* ax««» m* *» ™»9· «Λ * *·* a 22 a is fénypont sssrisá mécséé; snoi a ünss ?$inoo|ást egy ^,muî^:î mcágmsteges Kfomatcgtá»^ v Bed chtmm^y " * «Ο*·* * m,QHmiPMë ^ mmmrn zmx&amp;Wémmm g§r« állófej m * «W '; ' öíSíXH) adói Sdíit eembí-o a CHlRAtPAKi o«fop IC ötffcp. vagy M ** ««s» » m*m art««» 'SS <w mcass (Sá mw** ****** «»»»»* 2' :,;;-,:Á::: sfeie’f : <0 aíÍ’A:' :' AXAi'': -fe:A';:;:·’
m , λ · tQ
shö! ^jsfentèsfc Cl'CS-sM
HUE11740513A 2010-02-08 2011-02-08 Dihidro-pirido-ftalazinon-származékok szintetizálási folyamatai HUE030794T2 (hu)

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US30245710P 2010-02-08 2010-02-08

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US (2) US8765945B2 (hu)
EP (1) EP2533640B1 (hu)
JP (1) JP5735988B2 (hu)
KR (1) KR101826652B1 (hu)
CN (1) CN102834008B (hu)
AU (1) AU2011213584B2 (hu)
BR (1) BR112012019648B1 (hu)
CA (1) CA2788114C (hu)
CY (1) CY1118575T1 (hu)
DK (1) DK2533640T3 (hu)
ES (1) ES2606174T3 (hu)
HU (1) HUE030794T2 (hu)
IL (1) IL221170A (hu)
MX (1) MX340319B (hu)
PL (1) PL2533640T3 (hu)
PT (1) PT2533640T (hu)
RU (1) RU2561732C2 (hu)
SG (1) SG182784A1 (hu)
SI (1) SI2533640T1 (hu)
WO (1) WO2011097602A1 (hu)
ZA (1) ZA201205538B (hu)

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CA2787844C (en) 2010-02-03 2019-08-27 Biomarin Pharmaceutical Inc. Dihydropyridophthalazinone inhibitors of poly(adp-ribose) polymerase (parp) for use in treatment of diseases associated with a pten deficiency
AU2011213584B2 (en) 2010-02-08 2016-05-12 Medivation Technologies Llc Processes of synthesizing dihydropyridophthalazinone derivatives
SI2630146T1 (sl) 2010-10-21 2020-12-31 Medivation Technologies Llc Kristalinična tosilatna sol (8S,9R)-5-fluoro-8-(4-fluorofenil)-9-(1-metil-1H-1,2,4-triazol-5-IL)- 8,9-dihidro-2H-pirido(4,3,2-DE)ftalazin-3(7H)-ON
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