HRP20211449T1 - Derivati supstituiranih karbonukleozida korisni kao sredstva protiv raka - Google Patents

Derivati supstituiranih karbonukleozida korisni kao sredstva protiv raka Download PDF

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HRP20211449T1
HRP20211449T1 HRP20211449TT HRP20211449T HRP20211449T1 HR P20211449 T1 HRP20211449 T1 HR P20211449T1 HR P20211449T T HRP20211449T T HR P20211449TT HR P20211449 T HRP20211449 T HR P20211449T HR P20211449 T1 HRP20211449 T1 HR P20211449T1
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image
cancer
pharmaceutically acceptable
compound
acceptable salt
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HRP20211449TT
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Robert Arnold Kumpf
Indrawan James Mcalpine
Michele Ann Mctigue
Ryan Patman
Eugene Yuanjin Rui
John Howard Tatlock
Michelle Bich Tran-Dube
Martin James Wythes
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Pfizer Inc.
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07C255/34—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring with cyano groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
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    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
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    • C07D239/72—Quinazolines; Hydrogenated quinazolines
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    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
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    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
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    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • C07D251/18—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
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    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
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Claims (21)

1. Spoj formule (IV): [image] , ili njegova farmaceutski prihvatljiva sol, naznačen time što: svakog R1 se neovisno bira iz skupine koju čine (C1-C8)alkil, (C1-C8)halogenalkil, hidroksi, (C1-C8)alkoksi, (C5-C12)aril, 5-12-eročlani heteroaril, (C3-C10)cikloalkil, 3-12-eročlani heterociklil, OR4, SR4 i N(R4)2; R2 je vodik, halogen, (C1-C8)alkil, hidroksi, (C1-C8)alkoksi ili N(R5)2, gdje je svaki R5 neovisno vodik ili (C1-C8)alkil, ili se dva R5 spaja kako bi tvorili 4-6-eročlani heterociklički prsten koji sadrži 1-3 heteroatoma koje se bira između N, O i S; svaki R3 je neovisno vodik, hidroksi ili NH2; ili kada D je C(R3)2, gdje se R3 dodatno bira između fluora; svaki R9 je neovisno vodik ili fluor; D je C(R3)2, O, ili S(O)1-2; B je N ili C; E je NR1, CH2, C(R1)2, O ili -S(O)2; svaki R8 je odsutan ili ga se neovisno bira iz skupine koju čine (C1-C8)alkil, (C1-C8)halogenalkil, hidroksi, (C1-C8)alkoksi, (C5-C12)aril, 5-12-eročlani heteroaril, (C3-C10)cikloalkil, 3-12-eročlani heterociklil, OR4, SR4, N(R4)2, CN, halogen i CON(R4)2, gdje se dva R8 mogu spojiti kako bi tvorili 4-6-eročlani spiro-cikloalkilni prsten, cikloalkilni kondenzirani prsten, ili alkilenski most, te gdje se dva R8 mogu spojiti kako bi tvorili karbonil; svaki R4 je neovisno A-R14, gdje A je odsutan, (C1-C3)alkil, -C(O)- ili -SO2-, a R14 je vodik, (C1-C8)alkil, (C5-C12)aril, 5-12-eročlani heteroaril, (C3-C10)cikloalkil ili 3-12-eročlani heterociklil, ili se dva R4 spoje kako bi tvorili 4-6-eročlani heterociklički prsten koji sadrži 1-3 heteroatoma koje se bira između N, O i S; Q je odsutan ili je dvovalentni ostatak kojeg se bira između O, S, NH i (C1-C8)alkilena; V je N ili C, gdje ako V tvori dvostruku vezu V je ugljik; W je N ili C, gdje ako W tvori dvostruku vezu W je ugljik; X je N ili C, gdje ako X tvori dvostruku vezu X je ugljik; Y je CR10, N, NR10, O ili S, gdje se svakog R10 neovisno bira između vodika, (C1-C8)alkila, hidroksi, (C1-C8)alkoksi, halogena, SH, S-(C1-C8)alkila i N(R11)2 ako je Y CR10, gdje Y tvori dvostruku vezu sa susjednim članom prstena kada je Y CR10 ili N, te gdje je svaki R11 neovisno vodik, (C1-C8)alkil, (C5-C12)aril ili 5-12-eročlani heteroaril ili se dva R11 spajaju kako bi tvorili 4-6-eročlani heterociklički prsten koji sadrži 1-3 heteroatoma koje se bira između N, O i S, ili Y je C(R10)2, a dva R10 i ugljik na kojeg su vezani tvore karbonil ili tiokarbonil; Z je CR12, N, NR12, O ili S, gdje se svakog R12 neovisno bira između vodika, (C1-C8)alkila, hidroksi, (C1-C8)alkoksi, fluora, klora, broma, SH, S-(C1-C8)alkil i N(R13)2, gdje Z tvori dvostruku vezu sa susjednim članom prstena ako je CR12 ili N, gdje je svaki R13 neovisno vodik, (C1-C8)alkil, (C5-C12)aril ili 5-12-eročlani heteroaril, ili se dva R13 spoje kako bi tvorili 4-6-eročlani heterociklički prsten koji sadrži 1-3 heteroatoma koje se bira između N, O i S, te gdje Z nije NR12 ako je X N, V je C, W je C, a Y je CR10, ili je Z C(R12)2, a dva R12 i ugljik na kojeg su vezani tvore karbonil ili tiokarbonil; i svaki ----- je izborna veza, gdje može biti prisutno najviše dva nesusjedna -----.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima formulu (III): [image] , ili njegova farmaceutski prihvatljiva sol.
3. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s bilo kojim od patentnih zahtjeva 1-2, naznačen time što: [image] se bira između: [image] [image] [image] [image] , [image] , [image] , [image] [image] [image]
4. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 3, naznačen time što: [image] se bira između: [image]
5. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 4, naznačen time što: [image] je: [image] .
6. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 2, naznačen time što: [image] se bira između: [image] [image] [image] [image] [image] , [image] , [image] , [image] [image] [image] [image] , [image] , [image] , [image] , [image] [image] [image] [image] [image] , [image] , [image] , [image] [image] [image] [image] , [image] , [image] , [image] [image] [image] [image] [image] [image]
7. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 6, naznačen time što: [image] je: [image] ili [image] .
8. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 7, naznačen time što: [image] je: [image] .
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira između: [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , te [image] , ili njihovih farmaceutski prihvatljivih soli.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira između: [image] , [image] , [image] , [image] , [image] , [image] , te [image] , ili njihovih farmaceutski prihvatljivih soli.
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira između: [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , te [image] , ili njihovih farmaceutski prihvatljivih soli.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (1S,2S,3S,5R)-3-((6-(difluormetil)-5-fluor-1,2,3,4-tetrahidroizokinolin-8-il)oksi)-5-(4-metil-7H-pirolo[2,3-d]pirimidin-7-il)ciklopentan-1,2-diol, ili njegova farmaceutski prihvatljiva sol.
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima strukturu: [image] .
14. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s bilo kojim od patentnih zahtjeva 1-13, naznačen time što se navedenu sol bira između acetatne, aspartatne, benzoatne, besilatne, bikarbonatne/karbonatne, bisulfatne/sulfatne, boratne, kamsilatne, citratne, edisilatne, esilatne, formijatne, fumaratne, gluceptatne, glukonatne, glukuronatne, heksafluorofosfatne, hibenzatne, hidroklorid/klorid, hidrobromid/bromid, hidrojodid/jodid, izetionatne, laktatne, malatne, maleatne, malonatne, mesilatne, metil-sulfatne, naftilatne, 2-napsilatne, nikotinatne, nitratne, orotatne, oksalatne, palmitatne, pamoatne, fosfatne/vodikfosfatne/divodikfosfatne, saharatne, stearatne, sukcinatne, tartaratne, tosilatne, trifluoracetatne, aluminijeve, arginin, benzatin, kalcijeve, kolinove, dietilaminske, diolaminske, glicinske, lizinske, magnezijeve, megluminske, olaminske, kalijeve, natrijeve, trometaminske i cinkove soli.
15. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 14, naznačen time što se navedenu sol bira između hidrokloridne, tosilatne i mesilatne soli.
16. Farmaceutski pripravak, naznačen time što sadrži spoj, ili njegovu farmaceutski prihvatljivu sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 15, kao i farmaceutski prihvatljivi nosač.
17. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 15, naznačen time što je namijenjen upotrebi u liječenju abnormalnog staničnog rasta kod sisavca.
18. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 17, naznačen time što je abnormalni stanični rast rak.
19. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 18, naznačen time što je rak rak pluća, rak kostiju, rak gušterače, rak kože, rak glave ili vrata, kutani ili intraokularni melanom, rak maternice, rak jajnika, rak rektuma, rak analnog područja, rak želuca, rak debelog crijeva, rak dojke, rak maternice, karcinom jajovoda, karcinom endometrija, karcinom vrata maternice, karcinom vagine, karcinom vulve, Hodgkinova bolest, rak jednjaka, rak tankog crijeva, rak endokrinog sustava, rak štitnjače, rak nusštitnjače, rak nadbubrežne žlijezde, sarkom mekog tkiva, rak mokraćne cijevi, rak penisa, rak prostate, kronična ili akutna leukemija, limfocitni limfomi, rak mokraćnog mjehura, rak bubrega ili mokraćovoda, karcinom bubrežnih stanica, karcinom nakapnice, novotvor središnjeg živčanog sustava (CNS), primarni limfom CNS-a, tumori leđne moždine, gliom moždanog debla ili adenom hipofize.
20. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 19, naznačen time što je rak rak pluća, rak glave ili vrata, rak dojke, karcinom endometrija, karcinom vrata maternice, rak jednjaka ili rak mokraćnog mjehura.
21. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 20, naznačen time što je rak rak pluća.
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Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111542525B (zh) 2017-10-26 2023-06-27 普莱鲁德疗法有限公司 蛋白质精氨酸甲基转移酶5(prmt5)的选择性抑制剂
EP3720495A4 (en) * 2017-12-05 2021-06-02 Angex Pharmaceutical, Inc. HETEROCYCLIC COMPOUNDS AS PRMT5 INHIBITORS
CN108997309A (zh) * 2018-07-17 2018-12-14 中国科学技术大学苏州研究院 一种吡唑-4-芳基衍生物的制备方法
WO2020033285A1 (en) * 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
SG11202107226VA (en) * 2019-01-23 2021-08-30 Pfizer Polymorph form of a monophosphate hydrate salt of a known tetrahydroisoquinoline derivative
KR20210145787A (ko) 2019-04-02 2021-12-02 알리고스 테라퓨틱스 인코포레이티드 Prmt5를 표적으로 하는 화합물
JP2022534998A (ja) * 2019-05-30 2022-08-04 エンジェクス ファーマシューティカル インコーポレイテッド Ｐｒｍｔ５阻害剤としての複素環式化合物
JP2022536337A (ja) 2019-06-10 2022-08-15 ルピン・リミテッド Ｐｒｍｔ５阻害剤
ES2969732T3 (es) 2019-12-18 2024-05-22 Pfizer Régimen de tratamiento del cáncer una vez al día con un inhibidor de PRMT5
IL294400A (en) * 2020-01-07 2022-08-01 Pfizer A prmt5 inhibitor for use in the treatment of psoriasis and other autoimmune conditions
CN111138355A (zh) * 2020-01-17 2020-05-12 成都睿智化学研究有限公司 一种甲醛取代的氮杂稠环类化合物的制备方法
WO2021152055A1 (en) 2020-01-31 2021-08-05 Solvay Sa Process for the manufacture of haloalkyl substituted pyridine compounds
WO2021202480A1 (en) * 2020-04-01 2021-10-07 Aligos Therapeutics, Inc. Compounds targeting prmt5
WO2022013691A1 (en) 2020-07-15 2022-01-20 Pfizer Inc. Polymorph of (1s,2s,3s,5r)-3-((6-(difluoromethyl)-5-flu­oro-1,2,3,4-tetrahydroisoquinolin-8-yl)oxy)-5-(4-methyl-7h-pyrrolo[2,3-d]­pyrimidin-7-yl)cyclopentane-1,2-diol
WO2022013692A1 (en) 2020-07-15 2022-01-20 Pfizer Inc. Polymorphs of (1s,2s,3s,5r)-3-((6-(difluoromethyl)-5-flu­oro-1,2,3,4-tetrahydroisoquinolin-8-yl)oxy)-5-(4-methyl-7h-pyrrolo[2,3-d]­pyrimidin-7-yl)cyclopentane-1,2-diol mono-hydrochloride
WO2022153161A1 (en) 2021-01-14 2022-07-21 Pfizer Inc. Treatment of cancer using a prmt5 inhibitor
CN113234079B (zh) * 2021-04-30 2022-02-01 上海湃隆生物科技有限公司 用作prmt5抑制剂的核苷类似物
WO2024118943A2 (en) * 2022-11-30 2024-06-06 Ideaya Biosciences, Inc. Combination therapy comprising a mat2a inhibitor and a prmt5 inhibitor
WO2024170488A1 (en) 2023-02-13 2024-08-22 Astrazeneca Ab Prmt5 inhibitor for use in cancer therapy

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
US6143749A (en) * 1995-06-07 2000-11-07 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
WO2000035296A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Improved release of medicament active agents from a chewing gum coating
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
SI1370531T1 (sl) 2001-02-22 2007-08-31 Ucb Pharma Sa Derivati fenilalanin enamida s ciklobutensko skupino, za uporabo kot integrin inhibitorji
US20040043959A1 (en) * 2002-03-04 2004-03-04 Bloom Laura A. Combination therapies for treating methylthioadenosine phosphorylase deficient cells
EP1987717A1 (de) 2007-04-30 2008-11-05 Bayer CropScience AG Pyridoncarboxamide, diese enthaltende nutzpflanzenschützende Mittel und Verfahren zu ihrer Herstellung und deren Verwendung
WO2010100475A1 (en) 2009-03-02 2010-09-10 Astrazeneca Ab Hydroxamic acid derivatives as gram-negative antibacterial agents
US9216981B2 (en) * 2010-12-02 2015-12-22 Medpacto, Inc. Purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition with inhibitory activity against Raf kinase, containing same as active ingredient
AU2013250726B2 (en) 2012-04-20 2017-01-05 Advinus Therapeutics Limited Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
DK2935222T3 (en) 2012-12-21 2019-01-07 Epizyme Inc PRMT5 INHIBITORS AND APPLICATIONS THEREOF
WO2015013256A1 (en) 2013-07-22 2015-01-29 Baylor College Of Medicine Non-ribose containing inhibitors of histone methyltransferase dot1l for cancer treatment
EP3160477A4 (en) 2014-06-25 2018-07-04 Epizyme, Inc. Prmt5 inhibitors and uses thereof
EP4306934A3 (en) * 2015-02-25 2024-03-27 Outsense Diagnostics Ltd. Bodily emission analysis
TW202321249A (zh) 2015-08-26 2023-06-01 比利時商健生藥品公司 使用作為ｐｒｍｔ５抑制劑之新穎經６－６雙環芳香環取代之核苷類似物

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