HUE031976T2 - Humán EZH2 hisztonmetil-transzferáz inhibitor só formája - Google Patents

Humán EZH2 hisztonmetil-transzferáz inhibitor só formája Download PDF

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Publication number
HUE031976T2
HUE031976T2 HUE13774979A HUE13774979A HUE031976T2 HU E031976 T2 HUE031976 T2 HU E031976T2 HU E13774979 A HUE13774979 A HU E13774979A HU E13774979 A HUE13774979 A HU E13774979A HU E031976 T2 HUE031976 T2 HU E031976T2
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HU
Hungary
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degrees
cancer
polymorph
árd
compound
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HUE13774979A
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English (en)
Inventor
Kevin Wayne Kuntz
Kuan-Chun Huang
Hyeong Wook Choi
Kristen Sanders
Steven Mathieu
Arani Chanda
Frank Fang
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Epizyme Inc
Eisai R&D Man Co Ltd
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Publication of HUE031976T2 publication Critical patent/HUE031976T2/hu

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Claims (4)

  1. ... J'S'iOrtΐΗίΠΊϊό'ΐί*^»^* ! ' p-kOSm iW o-3 * pox' - »t\onn»v'^ mm ti Î "4-'-^ îï^ i i I-11 ^ 1: Φ i feí íí 1 }-3 ssi^b k! r obr^micl, :2. \t ! sggnxpom s/e ,",k kgx nice ^nan monohids.'btee,\f ' ' ' η,οοχροοο \ o>> ke mti^ x »V m <! x^gx.dc« kos. fűm 4 At előző igénypontok Nn«{|Iishal •men rés; ?. \t cio<fo igénypontok bármelyike sxermti vegyüld. almi &amp; vegyülef 'hiUCályos. szftárd a«y;xg és lényegében mentes amorf K· · 4,6-jimeril-2-oxo·· 1fo-dilodropirldin 3 Iffon: tiI)->4ebl{veír;ihidrü' 74I-ρίίοπ·4--4ΐηοηη>ο··4-η5^ΐΐ!···ΐ'·! mrsribim&amp;ineiiSH I 4 ' ο ο í ο η 4 y 3 · k;n h Ολ ô ηή ;ό h ί 4 ;\ · t n i ; \5 i d 16 L
  2. 6. Oyágyszetkészítmény. amely uxrmlma?.2a az 1-5. igéixypomok Amelyike e-uintl xegySdetek és
  3. 7. Eljátás as 1, igéhypontszeîôitl:v®gyi4«kélsàlliÂàrax:Sineiy taÄmnz^ sziisdlpés^ hagy l^fAdk: bnnmiS- 3 o xo s 3·dihklr^pn»dm-3»»l)metiP)*5dyiti.ktetraindm-'SH^mmv-d·»ll)amhio)4>nieni-4·^ iinof.kk Ísn.'ínou'i t i, i bsSend) 7 k.o hexánodét Indi egonl^ nnn.ldxl kombinálunk : 8- l44C:^~hMimefíb2^os0> 1,2^iílh4mpkidí®3yli)n5eí il)“5deî4(îetmhÎdrO'-2ll'piîan:sisU3amiPp)''^-“iî5e" Sü4'*(nn.*rintinomediH 1< S 'dbfeoii3 4anx>xarnld0ndfobfonnd Λ polimorf fomuija. 4, 71 8, sgéixypemS vwrioii ^ipiarf äibdl áppISinorf rÖnlgenspi^flfíIflMcIós Kepe g£y ypgf fop jéltimző csúcsot tartalmaz 2-théta· fokokban ki fejese nhmegy t0. óv- Q.fi. fok, iomteiy f fok, és mintegy 22,0 »;- 0,3 3--;héis fok értéknél 103 ¾ 8¾ igénypontok bármelyike eserlsíl polimorf) ahol spotlntorf röntgensugár por ötifískmos kejx pdvn»'v * u« \m t.ux.dnnv . p\t » U ».okpan kiXieno onPO>'X * a. ' a<k, nnnfex"' < s * ~ 0,3 fok, és mintegy 22 fi *f~ 0,3 c-theSa Ónk értéknek II. A 8. igénypont szerinti polimorf, aboi a polimorf röntgensugár pót diffrakciós képe egy vagy több x'iiom'ó <. ,o<.oOt kntabna? Γ than ΙοΚΆ&amp;ή kdepvxe numen ' ^ ' *?>,>. m ntegx +.' 5 ' fok, mintegy 18.7 H~ 0,3 fok mintegy 33.3 +/- 0 3 Sok, és mintegy 23,0 *'- 0J 2-méta fok értőknél. ^ \ 8 ,e<. í n > 'ZC' * ' ári ah<l* »mH' mu ι i s é Si 'v os U >e lo x< »0 s ,'Ό o c > i\ e tan dnn ' Ou», k u mcu 1 ''* - A,'tek, t> » b' e.< n t , V ' 0 s t ^ k » ' t0k t ‘ 0 3 K j; 4‘ 0 ' toi 3 N » > * \ a 0,3 Oik, 33.,3 »,·' 0J fok és 37,4 +;. (}f3 2·thêta fok értéknél ' * \ '3 i*,x ' Γ Hi? ifo |V HO io«^Y '< , fofoH is <;$ Î fo'> 1 '* ílemjt csúcsot t&amp;nsinw 2dhsta fokokban kifofosvo mmtegv 3.9 J- 0,3 (ok, Híj r‘' ‘3-* fok. foj m fok. i ?,5 +/- 0,5 fok, 18,7 *Λ 0J fok, 2Û.6 fo- 0.5 fok. 20,9 - - 0 3 fok. 2U — f»3 fok, 32.0 ·; ··- 0 "* fos U - 0 ' Ok 'x ^'.í' ' *' ' .' ΠΛ-i ! k . k \' N. Λ 8. igénypont sæermii polimorf, ahoi &amp; polimorf röntgensugár por diffrakciós kope legalább / jen ir*» ' ^ .a .' vei o U üí y ' * 1 * ' toi 0 4 n h k 'k' J, . ' * 0 1 ick, 'S ' - - -- 3 fok, « o ' '' ' vk 20" > ' tok " s - - OJ ink J J0 * - JJ fok. 23,3 H- 0,3 tok cs 23,6 s··'-· ο,3 2--dtéta fok értéknél 15. Λ 8. igenypcmt szerinti polimorf, «aboi s polimorf tömgettsngár por drífetkofos kúp« legalább 8 jel- fon -o * kH sfoï ' '3 , ä \'s,oU'U' k?fo|0 ',0 'T 1 .J * * **-k, ä i 0 ' fo\ t 0J fok« 1?«5 +A 0,3 fok, ISJ 0,3 fok. 2Ô/S *.·· 0,3 fok, 2Ô,« ·ι/- 0,3 fok 21.8 OJ fok, 22,0-·*Α O, 3 fok, 23.3 +Λ 0,3 fok és 23,0 t .--9.3 2-foéia fok hiitmÉt 16, A 8, igénypont surfod polimorf ahol 3 polimorf römgensupr por dittrakciés kepe legalább v jel- \hv>< οήκ'χ,η Ontalma/ 3 thm fok^KKm ktfofo.'sv mmkpx \ú ' - 0J íok 10 ' 'fok fo ' 0,3 fok. 1 íj +/- 0,3 fok. SEJ :.-0.3 fok, 20,6 -h·'- 0,3 fok, 20,4 m- o,3 fok. 31,8 * -- <l> fok, 22/1 ·*’- * ' Ί, - » ' fok v 2\o 0 12 lem \sk e.-Lknci Π, 8. igénypont .ur nrfo polimorf, »bői sí polimorf röntgensugár pót fofímkeios 8^γΙ£^Ϊ$^.^-JeiknsKrö csúcsot tartalma,’ 3 shem tbk.mo-m kstoc/sc mmtegs >J - o,; Ofo, loj · , oj fok, M.t - - 0 3 tok, fofo * - 0.1 fok. iS," ♦ - 0J fol. 20 o - - oj Pfo. 20.0 * . oJ fok. 21.8 »- 0 t ink, „2,0 fo'- 0,3 fok. 23,3 -J- 0,3 fok és 23,0 Ή- 0,3 2-íhéta fok ériéknéh ít. Λ 8, igé^>paöf polimorf rânigensugar por Jifoaksiós képe /dkíozi' esa- csíh laaahH;v 2-tbéu lokokhan ksfoscevo minier 3,9 ; - o. t fok. Híj - oj fok. '4.3 - - i\j Ù k, Γ ^ -0 t ksk, iHJ ' -i í fo^ 39,0 - χΜ '3c »-, j.xk. Ifo ' X J isk, ,0 Ifok X 0JfokvS,_'6 X 1 Sx 4 x-x.U.MS U \ S lk v \pHHOh ,-íSHx X k X x'ä 0 5 ,V * , S \ »hmm XX' 'xS4( f IM xíí í ,-\x xs képe lényegéi»e.n az 1. ábra szennts. 30. A 8-19, igénypontok bármd.vlke sxcrlü.piÄbll|:::#bl-«:;í cnpe Sien í-s 1 tabla,-as x<\nfo' 21. A 8-20, ígéísypontiJJbafofolyikc foerh'ü poHnterf, áhof n poIBnotf dÜTcrenclâ? pasjfeú kafosfo: meirids termograotmja jeiiemzö csúcsot tnutai Aí eg/ ségeklx-;» kHcjexve 255 s '- :V;c bórnérséMctesc 22 : A 8-2 ?. JígéM^pöíStöskíifeám'iíöl^· I ppilpfof I ; alto; a pofonod dfocrencuU pásdáoO kaion- •mèirî«1> tcnnpi'ï-pmxfoplfofoegébço a 3, ábra.míámi·. 22 Kijárás « «-22, igénypontok bármelyike saeriorï polimorf előállítására, amely lartalmaíjsa *« a p*^, hogy Ν'-o kfwiimeublhoxrfc-í ,$49hidntyM»* * ' *«**Η«ΛΜΐ»»Λν·:i l-pu jk.-** tl'wx * ?, r.bfóei tj.3 .karhoxamidct bidrc^mbmmutdal koailnoáUnik
  4. 24. Kijárás a H-22. igénypontok bármelyike forint* ρ<ίΗιν»ο?Γ aikT^alyo3íl^áf%«^ következő kiseket- úsí Λ polimorfot ej*y első oldószerben oldunk ds ok!ós?.ssl úgy, hog;- s? említett polhaoif âtkmiàlyosodik.. 25, A 24. igln^poí#;s^í^^;:ey^Sj}^oha^,glsdp:dfslfe®f vtanok ês a második oldószer kt * ho,, 2ô. Λ ló. ;gô?opork szerinti ujatas, ameh íurtshon-v» a kő', cd ózó lépc-vAo); u· k pc-Fur'-h'i <',’-noUiem oldunk (.h* ni\^.liíi.'k'!i|ik , k*o > \ΊΛ_ , íí ι^Λ s x ' " * K polänkfiM: iaitpljdíkd esap:d|kdk||jsgg:lhlls |^:#iPap%#^|:.:II$riök úgy, Ikíklálydsodlk 5"? \'"· OgcscA. k o \ 'íO'k ";\ un,h no (oh ou c-o a 4-T."' »gern pontok harm oh o,o a - í. őrá poFnsuBOc cs \v\'u's ,* \' 'ul a no hot,, v» , m 11 Λ t a' ok Az 1-5. igénypontok bármelyike szárirai vegyiig »·^i2i%«oypoo^ldbÄrnilfm** *>0sS'" morf, vagy a 6. vagy 27. igénypontok bármelyik« szerinti gyógy.mniészdmény rák kezetek eljárásúban (ooénö alkakn.v,,,n -, f.9 Λ 2«. igényponti, szófiait vegyidet, ptosork vagy gyogyszortisghhgghy ak adnh aftatroaabia, ahol u rák oem-Hodgkio hmforoa, töszós iimtorna (FI..}, dittos nagy B-copes. I unions a íl>hB(. L) vagy om sírok. I n*t\ \ y ‘ í! oimeí i ' '\o 1 ^0^1),^)((4)0^00^((0-^,,1^,.1^5,510 Ή Γ ívP h)M>*r no}-4-matU'4'-t'niorfoimomelilHkivl>>fcmij-s»-karboKamiá előállítására, amely mrhdh't^^ azt a le-pást, hogy 5uetü(teímbfiárO-2H-pínm-4'Ü>am«io|-4-metíl-4'-<morrolítm»et8..t-f:l:S:fehbif<‘t'*^";í“^ar^ms·’ ,-,oal ο; Oamisiomt oOkP-dmseol dihOn, poidío-2(Πh-on Ónnal reagalhnunk
HUE13774979A 2012-04-13 2013-04-11 Humán EZH2 hisztonmetil-transzferáz inhibitor só formája HUE031976T2 (hu)

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US201261624215P 2012-04-13 2012-04-13

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Application Number Title Priority Date Filing Date
HUE13774979A HUE031976T2 (hu) 2012-04-13 2013-04-11 Humán EZH2 hisztonmetil-transzferáz inhibitor só formája
HUE16191716A HUE045353T2 (hu) 2012-04-13 2013-04-11 N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)-metil)-5-(etil-(tetrahidro-2H-pirán-4-il) -amino)-4-metil-4'-(morfolino-metil)-[1,1'-bifenil]-3-karboxamid-hidrobromid a hematológiai rendszer egy sejtszaporodásos rendellenességének kezelésében való alkalmazásra
HUE19180479A HUE060881T2 (hu) 2012-04-13 2013-04-11 Sóforma az EZH2 gátláshoz

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Application Number Title Priority Date Filing Date
HUE16191716A HUE045353T2 (hu) 2012-04-13 2013-04-11 N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)-metil)-5-(etil-(tetrahidro-2H-pirán-4-il) -amino)-4-metil-4'-(morfolino-metil)-[1,1'-bifenil]-3-karboxamid-hidrobromid a hematológiai rendszer egy sejtszaporodásos rendellenességének kezelésében való alkalmazásra
HUE19180479A HUE060881T2 (hu) 2012-04-13 2013-04-11 Sóforma az EZH2 gátláshoz

Country Status (25)

Country Link
US (6) US9394283B2 (hu)
EP (4) EP2836491B1 (hu)
JP (3) JP6255382B2 (hu)
KR (3) KR102438340B1 (hu)
CN (2) CN104603130B (hu)
AU (2) AU2013245878B2 (hu)
BR (1) BR112014025508B1 (hu)
CA (1) CA2870005C (hu)
CY (2) CY1119383T1 (hu)
DK (3) DK3628670T3 (hu)
ES (3) ES2745016T3 (hu)
HR (2) HRP20170295T1 (hu)
HU (3) HUE031976T2 (hu)
IL (4) IL296199A (hu)
IN (1) IN2014DN09068A (hu)
LT (2) LT2836491T (hu)
MX (1) MX362339B (hu)
NZ (1) NZ700761A (hu)
PL (3) PL3184523T3 (hu)
PT (3) PT3184523T (hu)
RS (2) RS55690B1 (hu)
RU (1) RU2658911C2 (hu)
SG (3) SG11201406468YA (hu)
SI (2) SI3184523T1 (hu)
WO (1) WO2013155317A1 (hu)

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