EA201500394A1 - Ингибиторы деметилаз гистонов - Google Patents

Ингибиторы деметилаз гистонов

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Publication number
EA201500394A1
EA201500394A1 EA201500394A EA201500394A EA201500394A1 EA 201500394 A1 EA201500394 A1 EA 201500394A1 EA 201500394 A EA201500394 A EA 201500394A EA 201500394 A EA201500394 A EA 201500394A EA 201500394 A1 EA201500394 A1 EA 201500394A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
hystones
distemylase
inhibitors
hdme
Prior art date
Application number
EA201500394A
Other languages
English (en)
Other versions
EA030698B1 (ru
Inventor
Марк Лабель
Томас Босен
Мукунд Мехротра
Казим Кхан
Фарман Уллах
Original Assignee
Эпитерапьютикс Апс
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Publication date
Application filed by Эпитерапьютикс Апс filed Critical Эпитерапьютикс Апс
Publication of EA201500394A1 publication Critical patent/EA201500394A1/ru
Publication of EA030698B1 publication Critical patent/EA030698B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • 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
    • C07D213/04—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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/12—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 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
    • C07D405/02—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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms
    • 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

Abstract

В настоящей заявке предложены соединения, способные модулировать активность деметилаз гистонов (HDME), которые подходят для предотвращения и/или лечения заболеваний, в патогенезе которых задействована дисрегуляция генома, таких как, например, рак. В настоящей заявке также предложены фармацевтические композиции, содержащие указанные соединения, и применение указанных соединений в качестве лекарственного средства. Соединения имеют формулу (I)
EA201500394A 2012-10-02 2013-10-01 Ингибиторы деметилаз гистонов EA030698B1 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261708806P 2012-10-02 2012-10-02
DKPA201200599 2012-10-02
US201361770050P 2013-02-27 2013-02-27
DKPA201370112 2013-02-27
PCT/EP2013/070457 WO2014053491A1 (en) 2012-10-02 2013-10-01 Inhibitors of histone demethylases

Publications (2)

Publication Number Publication Date
EA201500394A1 true EA201500394A1 (ru) 2015-11-30
EA030698B1 EA030698B1 (ru) 2018-09-28

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201500394A EA030698B1 (ru) 2012-10-02 2013-10-01 Ингибиторы деметилаз гистонов

Country Status (32)

Country Link
US (3) US20150203453A1 (ru)
EP (3) EP3023415B1 (ru)
JP (2) JP6530313B2 (ru)
KR (1) KR102160320B1 (ru)
CN (2) CN104981458B (ru)
AP (1) AP2015008389A0 (ru)
BR (1) BR112015007083A2 (ru)
CA (2) CA2885969C (ru)
CL (1) CL2015000829A1 (ru)
CR (1) CR20150217A (ru)
CY (1) CY1118695T1 (ru)
DK (1) DK2903968T3 (ru)
EA (1) EA030698B1 (ru)
ES (2) ES2617905T3 (ru)
HK (3) HK1207373A1 (ru)
HR (1) HRP20170358T1 (ru)
HU (1) HUE033380T2 (ru)
IL (2) IL237831A (ru)
LT (1) LT2903968T (ru)
MD (1) MD20150043A2 (ru)
ME (1) ME02597B (ru)
MX (1) MX2015003959A (ru)
NZ (1) NZ706635A (ru)
PE (1) PE20150998A1 (ru)
PH (2) PH12015500730A1 (ru)
PL (2) PL2903968T3 (ru)
PT (2) PT3023415T (ru)
RS (1) RS55764B1 (ru)
SG (2) SG10201703682YA (ru)
SI (2) SI3023415T1 (ru)
SM (1) SMT201700109B (ru)
WO (1) WO2014053491A1 (ru)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE033380T2 (en) 2012-10-02 2017-11-28 Gilead Sciences Inc Inhibitors of histone demethylases
PE20151667A1 (es) 2013-02-27 2015-11-27 Epitherapeutics Aps Inhibidores de histona desmetilasas
JP2017512804A (ja) * 2014-03-31 2017-05-25 ギリアード サイエンシーズ， インコーポレイテッド ヒストン脱メチル化酵素の阻害剤
KR20170040805A (ko) 2014-08-27 2017-04-13 길리애드 사이언시즈, 인코포레이티드 히스톤 데메틸라제를 억제하기 위한 화합물 및 방법
SG11201702147TA (en) 2014-09-17 2017-04-27 Celgene Quanticel Res Inc Histone demethylase inhibitors
US10030017B2 (en) 2014-09-17 2018-07-24 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
ES2751464T3 (es) 2014-09-17 2020-03-31 Celgene Quanticel Res Inc Inhibidores de histona desmetilasa
CA2962917C (en) 2014-10-29 2019-04-30 Dong-A St Co., Ltd. Novel pyridopyrimidinone compounds for modulating the catalytic activity of histone lysine demethylases (kdms)
EP3212789B1 (en) * 2014-10-31 2020-04-22 Massachusetts Institute of Technology Massively parallel combinatorial genetics for crispr
JP2018511621A (ja) * 2015-04-14 2018-04-26 ギリアード サイエンシーズ， インコーポレイテッド Ｂ型肝炎ウイルスを処置する方法
US10206930B2 (en) * 2015-08-14 2019-02-19 New York University Methods for treating T-cell acute lymphoblastic leukemia
EP3386594B1 (en) 2015-12-11 2023-05-03 The General Hospital Corporation Combination of a platelet-derived growth factor receptor alpha inhibitor and a histone lysine demethylase inhibitor for treating drug-tolerant glioblastoma
WO2017117154A1 (en) 2015-12-28 2017-07-06 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
EP3430008B1 (en) * 2016-03-15 2022-05-18 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
WO2017198785A1 (en) * 2016-05-18 2017-11-23 Ieo - Istituto Europeo Di Oncologia S.R.L. Oxime derivatives useful as inhibitors of histone demethylase kdm4c
CA3025633C (en) 2016-05-27 2021-02-23 Gilead Sciences, Inc. Methods for treating hepatitis b virus infections using ns5a, ns5b or ns3 inhibitors
BR102017010009A2 (pt) 2016-05-27 2017-12-12 Gilead Sciences, Inc. Compounds for the treatment of hepatitis b virus infection
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
CA3035346A1 (en) 2016-09-02 2018-03-08 Gilead Sciences, Inc. Toll like receptor modulator compounds
ES2826748T3 (es) 2016-09-02 2021-05-19 Gilead Sciences Inc Derivados de 4,6-diamino-pirido[3,2-d]pirimidina como moduladores de receptores de tipo Toll
PE20191353A1 (es) 2016-10-14 2019-10-01 Prec Biosciences Inc Meganucleasas disenadas especificamente para el reconocimiento de secuencias en el genoma del virus de la hepatitis b
AR110768A1 (es) 2017-01-31 2019-05-02 Gilead Sciences Inc Formas cristalinas de tenofovir alafenamida
JOP20180008A1 (ar) 2017-02-02 2019-01-30 Gilead Sciences Inc مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
AU2018392213B2 (en) 2017-12-20 2021-03-04 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein
CA3084582A1 (en) 2017-12-20 2019-06-27 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
JP7062792B2 (ja) 2018-02-13 2022-05-06 ギリアード サイエンシーズ， インコーポレイテッド Ｐｄ－１／ｐｄ－ｌ１阻害剤
PL3759109T3 (pl) 2018-02-26 2024-03-04 Gilead Sciences, Inc. Podstawione związki pirolizyny jako inhibitory replikacji hbv
US10870691B2 (en) 2018-04-05 2020-12-22 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis B virus protein X
CN111954675A (zh) 2018-04-06 2020-11-17 捷克共和国有机化学与生物化学研究所 3’3’-环二核苷酸
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 ２，２，─環二核苷酸
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
CN108464984A (zh) * 2018-04-09 2018-08-31 徐州维康生物科技有限公司 一种治疗骨肉瘤的表观遗传药物
CN108186643B (zh) * 2018-04-09 2021-04-20 徐州维康生物科技有限公司 一种具有协同抗骨肉瘤功效的药物组合物及其应用
TW201945388A (zh) 2018-04-12 2019-12-01 美商精密生物科學公司 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶
WO2019204609A1 (en) 2018-04-19 2019-10-24 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
WO2019211799A1 (en) 2018-05-03 2019-11-07 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide
CN108530381B (zh) * 2018-05-07 2021-09-21 上海科技大学 一种由酰胺酯制备二胺衍生物的方法
CN112399874B (zh) 2018-07-13 2024-03-22 吉利德科学公司 Pd-1/pd-l1抑制剂
WO2020028097A1 (en) 2018-08-01 2020-02-06 Gilead Sciences, Inc. Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid
EP3833347A4 (en) * 2018-08-06 2022-04-27 Dana-Farber Cancer Institute, Inc. HISTONE-DEMETHYLAS-5 INHIBITORS AND USES THEREOF
CN109234313A (zh) * 2018-09-25 2019-01-18 上海交通大学医学院附属第九人民医院 共转染载体及其在抗骨肉瘤药物中的应用
KR102635333B1 (ko) 2018-10-24 2024-02-15 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
CA3116347A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
TWI721623B (zh) 2018-10-31 2021-03-11 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
CN113543851A (zh) 2019-03-07 2021-10-22 捷克共和国有机化学与生物化学研究所 2’3’-环二核苷酸及其前药
KR20210137518A (ko) 2019-03-07 2021-11-17 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. 3'3'-사이클릭 다이뉴클레오티드 및 이의 프로드럭
WO2020178768A1 (en) 2019-03-07 2020-09-10 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
TWI751517B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TWI751516B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
WO2020263830A1 (en) 2019-06-25 2020-12-30 Gilead Sciences, Inc. Flt3l-fc fusion proteins and methods of use
WO2021011891A1 (en) 2019-07-18 2021-01-21 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
EP4017476A1 (en) 2019-08-19 2022-06-29 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
AR120096A1 (es) 2019-09-30 2022-02-02 Gilead Sciences Inc Vacunas para vhb y métodos de tratamiento de vhb
US20230031465A1 (en) 2019-12-06 2023-02-02 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome
AU2021237718B2 (en) 2020-03-20 2023-09-21 Gilead Sciences, Inc. Prodrugs of 4'-C-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same
KR20230029659A (ko) 2020-05-26 2023-03-03 가부시키가이샤 헤리오스 저면역원성 세포
IL299980A (en) 2020-08-07 2023-03-01 Gilead Sciences Inc Preparations of phosphonamide nucleotide analogues and their medicinal use
CN111905102A (zh) * 2020-09-04 2020-11-10 福建医科大学附属第一医院 Ezh2抑制剂在治疗胶质瘤中的应用
TWI815194B (zh) 2020-10-22 2023-09-11 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
KR20240006683A (ko) 2021-05-13 2024-01-15 길리애드 사이언시즈, 인코포레이티드 TLR8 조절 화합물과 항-HBV siRNA 치료제의 조합물
US11926628B2 (en) 2021-06-23 2024-03-12 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
CA3222439A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
WO2022271684A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
US11932634B2 (en) 2021-06-23 2024-03-19 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
CN114907317B (zh) * 2022-06-01 2023-06-13 郑州大学 一种吡唑-乙烯基-异烟酸衍生物及其制备方法和应用

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
DE3372965D1 (en) 1982-07-23 1987-09-17 Ici Plc Amide derivatives
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
GB8717374D0 (en) * 1987-07-22 1987-08-26 Smith Kline French Lab Pharmaceutically active compounds
US5010099A (en) 1989-08-11 1991-04-23 Harbor Branch Oceanographic Institution, Inc. Discodermolide compounds, compositions containing same and method of preparation and use
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
AU716610B2 (en) 1996-08-30 2000-03-02 Novartis Ag Method for producing epothilones, and intermediate products obtained during the production process
DE69724269T2 (de) 1996-09-06 2004-06-09 Obducat Ab Verfahren für das anisotrope ätzen von strukturen in leitende materialien
US5874438A (en) 1996-10-11 1999-02-23 Bayer Aktiengesellschaft 2,2'-bridged bis-2,4-diaminoquinazolines
EP1367057B1 (de) 1996-11-18 2008-09-17 Gesellschaft für biotechnologische Forschung mbH (GBF) Epothilone E und F
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
ATE307123T1 (de) 1998-02-25 2005-11-15 Sloan Kettering Inst Cancer Synthese von epothilonen, ihren zwischenprodukten und analogen verbindungen
KR100851418B1 (ko) 1998-11-20 2008-08-08 코산 바이오사이언시즈, 인코포레이티드 에포틸론 및 에포틸론 유도체의 생산을 위한 재조합 방법 및 물질
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
US6620811B2 (en) 2001-11-19 2003-09-16 Hoffmann-La Roche Inc. Isonicotin- and nicotinamide derivatives of benzothiazoles
PT3000810T (pt) 2002-03-13 2017-10-25 Array Biopharma Inc Derivados de benzimidazole alquilado n3 como inibidores de mek
US7696210B2 (en) * 2004-06-17 2010-04-13 Wyeth Gonadotropin releasing hormone receptor antagonists
WO2008002671A2 (en) 2006-06-29 2008-01-03 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors
JPWO2009119088A1 (ja) * 2008-03-25 2011-07-21 武田薬品工業株式会社 複素環化合物
SA109300195B1 (ar) 2008-03-28 2013-04-20 Astrazeneca Ab تركيبة صيدلانية جديدة مضادة للسرطان
BRPI0919625A2 (pt) * 2008-10-29 2015-12-01 Sirtris Pharmaceutical Inc piriridina, piridina bicíclica e análogos relacionados como moduladores de sirtuína
US20120164148A1 (en) 2009-08-07 2012-06-28 The Wistar Institute Compositions Containing JARID1B Inhibitors and Methods for Treating Cancer
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
SI3354652T1 (sl) 2010-03-10 2020-08-31 Incyte Holdings Corporation Derivati piperidin-4-il azetidina kot inhibitorji JAK1
US9365553B2 (en) * 2010-05-27 2016-06-14 Aska Pharmaceutical Co., Ltd. Heterocyclic compound and H1 receptor antagonist
WO2012007007A1 (en) * 2010-07-15 2012-01-19 Epitherapeutics Aps Inhibitors of hdme
US20130303545A1 (en) 2010-09-30 2013-11-14 Tamara Maes Cyclopropylamine derivatives useful as lsd1 inhibitors
WO2012047156A1 (en) * 2010-10-04 2012-04-12 Astrazeneca Ab Isoxazol-3(2h)-one analogs as plasminogen inhibitors and their use in the treatment of fibrinolysis related diseases
WO2012071469A2 (en) 2010-11-23 2012-05-31 Nevada Cancer Institute Histone demethylase inhibitors and uses thereof for treatment o f cancer
SG193241A1 (en) 2011-03-25 2013-10-30 Glaxosmithkline Ip No 2 Ltd Cyclopropylamines as lsd1 inhibitors
ES2821548T3 (es) 2011-08-15 2021-04-26 Univ Utah Res Found Análogos de (E)-N'-(1-feniletiliden) benzohidrazida sustituida como inhibidores de desmetilasas de histonas
EA023955B1 (ru) 2011-10-27 2016-07-29 Астеллас Фарма Инк. Производное аминоалкилзамещенного n-тиенилбензамида
WO2013081091A1 (ja) * 2011-12-01 2013-06-06 国立大学法人 千葉大学 非特異的腎集積が低減された放射性標識ポリペプチド作製用薬剤
CN102585150B (zh) * 2012-02-01 2013-09-04 嘉兴学院 织物涂饰用阴离子水性聚氨酯分散体的制备方法
WO2013123411A1 (en) 2012-02-17 2013-08-22 Board Of Regents, The University Of Texas System Methods for diagnosing and treating cancer
WO2013129435A1 (ja) * 2012-02-28 2013-09-06 協和発酵キリン株式会社 縮環チオフェン誘導体
HUE033380T2 (en) 2012-10-02 2017-11-28 Gilead Sciences Inc Inhibitors of histone demethylases
US8987461B2 (en) 2012-12-06 2015-03-24 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
PL2934145T3 (pl) 2012-12-19 2018-04-30 Celgene Quanticel Research, Inc. Inhibitory demetylazy histonowej
JP6273621B2 (ja) 2012-12-21 2018-02-07 セルジーン クオンティセル リサーチ，インク． ヒストンデメチラーゼ阻害剤
PE20151667A1 (es) 2013-02-27 2015-11-27 Epitherapeutics Aps Inhibidores de histona desmetilasas
ES2644828T3 (es) 2013-03-15 2017-11-30 Quanticel Pharmaceuticals Inc Inhibidores de histona desmetilasa
US9505767B2 (en) 2013-09-05 2016-11-29 Genentech, Inc. Pyrazolo[1,5-A]pyrimidin-7(4H)-onehistone demethylase inhibitors
JP2017512804A (ja) 2014-03-31 2017-05-25 ギリアード サイエンシーズ， インコーポレイテッド ヒストン脱メチル化酵素の阻害剤

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