AU2018200876C1 - Inhibitors of histone demethylases - Google Patents

Inhibitors of histone demethylases Download PDF

Info

Publication number
AU2018200876C1
AU2018200876C1 AU2018200876A AU2018200876A AU2018200876C1 AU 2018200876 C1 AU2018200876 C1 AU 2018200876C1 AU 2018200876 A AU2018200876 A AU 2018200876A AU 2018200876 A AU2018200876 A AU 2018200876A AU 2018200876 C1 AU2018200876 C1 AU 2018200876C1
Authority
AU
Australia
Prior art keywords
methyl
ethyl
pharmaceutically acceptable
pyridine
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
AU2018200876A
Other languages
English (en)
Other versions
AU2018200876A1 (en
AU2018200876B2 (en
Inventor
Thomas Boesen
Qasim Khan
Marc Labelle
Mukund Mehrotra
Farman ULLAH
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gilead Sciences Inc
Original Assignee
Gilead Sciences Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AU2018200876A1 publication Critical patent/AU2018200876A1/en
Application granted granted Critical
Publication of AU2018200876B2 publication Critical patent/AU2018200876B2/en
Assigned to GILEAD SCIENCES, INC. reassignment GILEAD SCIENCES, INC. Request for Assignment Assignors: EPITHERAPEUTICS APS
Publication of AU2018200876C1 publication Critical patent/AU2018200876C1/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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 or sparfloxacin
    • 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

Landscapes

  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
AU2018200876A 2012-10-02 2018-02-06 Inhibitors of histone demethylases Active AU2018200876C1 (en)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US201261708806P 2012-10-02 2012-10-02
DKPA201200599 2012-10-02
US61/708,806 2012-10-02
DKPA201200599 2012-10-02
US201361770050P 2013-02-27 2013-02-27
US61/770,050 2013-02-27
DKPA201370112 2013-02-27
DKPA201370112 2013-02-27

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
AU2013326554A Division AU2013326554A1 (en) 2012-10-02 2013-10-01 Inhibitors of histone demethylases

Publications (3)

Publication Number Publication Date
AU2018200876A1 AU2018200876A1 (en) 2018-02-22
AU2018200876B2 AU2018200876B2 (en) 2019-09-19
AU2018200876C1 true AU2018200876C1 (en) 2020-02-06

Family

ID=52781382

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2018200876A Active AU2018200876C1 (en) 2012-10-02 2018-02-06 Inhibitors of histone demethylases

Country Status (33)

Country Link
US (3) US20150203453A1 (enExample)
EP (3) EP2903968B1 (enExample)
JP (2) JP6530313B2 (enExample)
KR (1) KR102160320B1 (enExample)
CN (2) CN107434803B (enExample)
AP (1) AP2015008389A0 (enExample)
AU (1) AU2018200876C1 (enExample)
BR (1) BR112015007083A2 (enExample)
CA (2) CA3095019C (enExample)
CL (1) CL2015000829A1 (enExample)
CR (1) CR20150217A (enExample)
CY (1) CY1118695T1 (enExample)
DK (1) DK2903968T3 (enExample)
EA (1) EA030698B1 (enExample)
ES (2) ES2654143T3 (enExample)
HK (1) HK1215710A1 (enExample)
HR (1) HRP20170358T1 (enExample)
HU (1) HUE033380T2 (enExample)
IL (2) IL237831A (enExample)
LT (1) LT2903968T (enExample)
MD (1) MD20150043A2 (enExample)
ME (1) ME02597B (enExample)
MX (1) MX2015003959A (enExample)
NZ (1) NZ706635A (enExample)
PE (1) PE20150998A1 (enExample)
PH (2) PH12015500730A1 (enExample)
PL (2) PL2903968T3 (enExample)
PT (2) PT2903968T (enExample)
RS (1) RS55764B1 (enExample)
SG (2) SG10201703682YA (enExample)
SI (2) SI2903968T1 (enExample)
SM (2) SMT201700109T1 (enExample)
WO (1) WO2014053491A1 (enExample)

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2903968T3 (en) 2012-10-02 2017-01-30 Gilead Sciences Inc INHIBITORS OF HISTON DEMETHYLASES
EA030451B1 (ru) 2013-02-27 2018-08-31 Эпитерапьютикс Апс Ингибиторы гистондеметилаз
AU2015241022A1 (en) * 2014-03-31 2016-10-27 Gilead Sciences, Inc. Inhibitors of histone demethylases
BR112017003442A2 (pt) 2014-08-27 2017-11-28 Gilead Sciences Inc compostos e métodos para inibir histona desmetilases
AU2015317806A1 (en) 2014-09-17 2017-04-13 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
US10030017B2 (en) 2014-09-17 2018-07-24 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
JP6723663B2 (ja) * 2014-09-17 2020-07-15 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
US9834550B2 (en) 2014-10-29 2017-12-05 Dong-A St Co., Ltd. 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
MA43925A (fr) * 2015-04-14 2018-12-05 Gilead Sciences Inc Procã‰dã‰s de traitement du virus de l'hã‰patite b
US10206930B2 (en) * 2015-08-14 2019-02-19 New York University Methods for treating T-cell acute lymphoblastic leukemia
WO2017099829A1 (en) 2015-12-11 2017-06-15 The General Hospital Corporation Compositions and methods for treating drug-tolerant glioblastoma
CN108698997A (zh) 2015-12-28 2018-10-23 赛尔基因昆蒂赛尔研究公司 组蛋白脱甲基酶抑制剂
ES2921009T3 (es) * 2016-03-15 2022-08-16 Celgene Quanticel Res Inc Inhibidores de desmetilasas de histonas
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
MA45088A (fr) 2016-05-27 2019-04-10 Gilead Sciences Inc Méthodes pour traiter des infections par le virus de l'hépatite b au moyen d'inhibiteurs de ns5a, ns5b ou ns3
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
ES2906581T3 (es) 2016-09-02 2022-04-19 Gilead Sciences Inc Compuestos moduladores de los receptores tipo Toll
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
SG11201903042VA (en) 2016-10-14 2019-05-30 Precision Biosciences Inc Engineered meganucleases specific for recognition sequences in the hepatitis b virus genome
TWI820984B (zh) 2017-01-31 2023-11-01 美商基利科學股份有限公司 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型
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
WO2019123340A1 (en) 2017-12-20 2019-06-27 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
US11203610B2 (en) 2017-12-20 2021-12-21 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
MX2020008404A (es) 2018-02-13 2020-09-25 Gilead Sciences Inc Inhibidores de molecula de muerte programada 1 (pd-1)/ligando de molecula de muerte programada 1 (pd-l1).
CN111788204B (zh) 2018-02-26 2023-05-05 吉利德科学公司 作为hbv复制抑制剂的取代吡咯嗪化合物
WO2019195181A1 (en) 2018-04-05 2019-10-10 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis b virus protein x
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-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
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
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
US11142750B2 (en) 2018-04-12 2021-10-12 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome
ES3035911T3 (en) 2018-04-19 2025-09-11 Gilead Sciences Inc Pd-1/pd-l1 inhibitors
US20190359645A1 (en) 2018-05-03 2019-11-28 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotides comprising carbocyclic 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
US12466869B2 (en) 2018-06-28 2025-11-11 Dana-Farber Cancer Institute, Inc. Targeting of multiple antigens with multiplex CAR T cells in solid and liquid malignancies
SI3820572T1 (sl) 2018-07-13 2023-12-29 Gilead Sciences, Inc. Inhibitorji pd-1/pd-l1
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
AU2019318046B2 (en) * 2018-08-06 2025-02-13 Dana-Farber Cancer Institute, Inc. Histone demethylase 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
JP7158577B2 (ja) 2018-10-24 2022-10-21 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
LT3873903T (lt) 2018-10-31 2024-05-10 Gilead Sciences, Inc. Pakeistieji 6-azabenzimidazolo junginiai, kaip hpk1 inhibitoriai
CN117105933A (zh) 2018-10-31 2023-11-24 吉利德科学公司 具有hpk1抑制活性的取代的6-氮杂苯并咪唑化合物
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
CA3129022C (en) 2019-03-07 2023-08-01 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotides and prodrugs thereof
EP3935066A1 (en) 2019-03-07 2022-01-12 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
TW202212339A (zh) 2019-04-17 2022-04-01 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
TWI826690B (zh) 2019-05-23 2023-12-21 美商基利科學股份有限公司 經取代之烯吲哚酮化物及其用途
JP7295283B2 (ja) 2019-06-25 2023-06-20 ギリアード サイエンシーズ， インコーポレイテッド Ｆｌｔ３ｌ－ｆｃ融合タンパク質及び使用方法
WO2021011891A1 (en) 2019-07-18 2021-01-21 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
WO2021034804A1 (en) 2019-08-19 2021-02-25 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
CR20220129A (es) 2019-09-30 2022-05-06 Gilead Sciences Inc Vacunas para vhb y métodos de tratamiento de vhb
CN110652589A (zh) * 2019-10-12 2020-01-07 中国人民解放军陆军军医大学 Gasc1抑制剂在制备治疗肝癌的药物中的应用
EP4069729B1 (en) 2019-12-06 2025-01-22 Precision BioSciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome
CN111073900B (zh) * 2019-12-09 2023-05-02 温氏食品集团股份有限公司 一种提高猪克隆胚胎发育效率的方法
TW202421168A (zh) 2020-03-20 2024-06-01 美商基利科學股份有限公司 4’-c-經取代-2-鹵基-2’-去氧腺苷核苷之前藥及其製造與使用方法
JP7742651B2 (ja) 2020-05-26 2025-09-22 株式会社ヘリオス 低免疫原性細胞
CN116194144A (zh) 2020-08-07 2023-05-30 吉利德科学公司 膦酰胺核苷酸类似物的前药及其药物用途
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
TW202406932A (zh) 2020-10-22 2024-02-16 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
AU2022274607A1 (en) 2021-05-13 2023-11-16 Gilead Sciences, Inc. COMBINATION OF A TLR8 MODULATING COMPOUND AND ANTI-HBV siRNA THERAPEUTICS
AU2022299051B2 (en) 2021-06-23 2025-03-13 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
US11999733B2 (en) 2021-06-23 2024-06-04 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
US11932634B2 (en) 2021-06-23 2024-03-19 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
US11926628B2 (en) 2021-06-23 2024-03-12 Gilead Sciences, Inc. Diacylglyercol 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
CN115806522B (zh) * 2022-11-24 2025-05-13 中国药科大学 一种取代吡啶衍生物及其应用
WO2025240242A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
WO2025240246A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
US20250345390A1 (en) 2024-05-13 2025-11-13 Gilead Sciences, Inc. Combination therapies
WO2025240243A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with bulevirtide and an inhibitory nucleic acid targeting hepatitis b virus

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010056549A1 (en) * 2008-10-29 2010-05-20 Sirtris Pharmaceuticals, Inc. Pyridine, bicyclic pyridine and related analogs as sirtuin modulators
WO2012007007A1 (en) * 2010-07-15 2012-01-19 Epitherapeutics Aps Inhibitors of hdme
CN102585150A (zh) * 2012-02-01 2012-07-18 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
EP2578569A1 (en) * 2010-05-27 2013-04-10 ASKA Pharmaceutical Co., Ltd. Heterocyclic ring compound and h1 receptor antagonist

Family Cites Families (42)

* 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
EP0100172B1 (en) 1982-07-23 1987-08-12 Imperial Chemical Industries 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
WO1998008849A1 (de) 1996-08-30 1998-03-05 Novartis Aktiengesellschaft Verfahren zur herstellung von epothilonen und zwischenprodukte innerhalb des verfahrens
DE938597T1 (de) 1996-09-06 2000-03-09 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
ATE267197T1 (de) 1996-11-18 2004-06-15 Biotechnolog Forschung Gmbh Epothilon d, dessen herstellung und dessen verwendung als cytostatisches mittel bzw. als pflanzenschutzmittel
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
NZ506742A (en) 1998-02-25 2003-09-26 Sloan Kettering Inst Cancer Synthesis of desoxyepothilones and hydroxy acid derivative intermediates
WO2000031247A2 (en) 1998-11-20 2000-06-02 Kosan Biosciences, Inc. Recombinant methods and materials for producing epothilone and epothilone derivatives
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
SI2130537T1 (sl) 2002-03-13 2013-01-31 Array Biopharma, Inc. N3-alkilirani derivati benzimidazola kot inhibitorji mek
JP2008503469A (ja) 2004-06-17 2008-02-07 ワイス ゴナドトロピン放出ホルモン受容体アンタゴニスト
AU2007265368A1 (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
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
PE20130038A1 (es) 2010-03-10 2013-01-28 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de jak1
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
JP5813855B2 (ja) 2011-03-25 2015-11-17 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｎｏ．２ Ｌｉｍｉｔｅｄ Ｌｓｄ１阻害剤としてのシクロプロピルアミン
BR112014003382B1 (pt) 2011-08-15 2022-03-15 University Of Utah Research Foundation Análogos de (e)-n-(1-feniletilideno) benzo-hidrazida substituída como inibidores de histona desmetilase e composições farmacêuticas compreendendo-os
BR112014010169B1 (pt) * 2011-10-27 2021-12-07 Astellas Pharma Inc Compostos de derivado n-tienilbenzamida substituída com aminoalquil, composição contendo os ditos compostos e uso dos mesmos para prevenir ou tratar hiperfosfatemia
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
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
DK2903968T3 (en) 2012-10-02 2017-01-30 Gilead Sciences Inc INHIBITORS OF HISTON DEMETHYLASES
JP6256771B2 (ja) 2012-12-06 2018-01-10 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
US8969343B2 (en) 2012-12-19 2015-03-03 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
SG11201504946VA (en) 2012-12-21 2015-07-30 Quanticel Pharmaceuticals Inc Histone demethylase inhibitors
EA030451B1 (ru) 2013-02-27 2018-08-31 Эпитерапьютикс Апс Ингибиторы гистондеметилаз
HRP20171609T1 (hr) 2013-03-15 2017-12-15 Quanticel Pharmaceuticals Inc Inhibitori histon demetilaze
CN105611933B (zh) 2013-09-05 2019-01-25 基因泰克公司 抗增生性化合物
AU2015241022A1 (en) 2014-03-31 2016-10-27 Gilead Sciences, Inc. Inhibitors of histone demethylases

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010056549A1 (en) * 2008-10-29 2010-05-20 Sirtris Pharmaceuticals, Inc. Pyridine, bicyclic pyridine and related analogs as sirtuin modulators
EP2578569A1 (en) * 2010-05-27 2013-04-10 ASKA Pharmaceutical Co., Ltd. Heterocyclic ring compound and h1 receptor antagonist
WO2012007007A1 (en) * 2010-07-15 2012-01-19 Epitherapeutics Aps Inhibitors of hdme
CN102585150A (zh) * 2012-02-01 2012-07-18 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

Also Published As

Publication number Publication date
EA030698B1 (ru) 2018-09-28
SMT201700109T1 (it) 2017-03-08
MD20150043A2 (ro) 2015-08-31
HK1215710A1 (zh) 2016-09-09
IL237831A (en) 2017-10-31
IL253259A0 (en) 2017-08-31
CN107434803B (zh) 2020-05-05
PL3023415T3 (pl) 2018-06-29
CA3095019C (en) 2022-06-14
CA3095019A1 (en) 2014-04-10
ME02597B (me) 2017-06-20
EP2903968A1 (en) 2015-08-12
MX2015003959A (es) 2015-11-16
IL253259B (en) 2018-04-30
CN104981458A (zh) 2015-10-14
SMT201700109B (it) 2017-03-08
CR20150217A (es) 2015-06-11
US20170320827A1 (en) 2017-11-09
EP3150582A1 (en) 2017-04-05
KR102160320B1 (ko) 2020-09-28
AU2018200876A1 (en) 2018-02-22
NZ706635A (en) 2018-08-31
CL2015000829A1 (es) 2015-12-04
PT3023415T (pt) 2018-02-27
US10189787B2 (en) 2019-01-29
AP2015008389A0 (en) 2015-04-30
US10221139B2 (en) 2019-03-05
HK1223612A1 (en) 2017-08-04
CA2885969A1 (en) 2014-04-10
US20150203453A1 (en) 2015-07-23
CY1118695T1 (el) 2017-07-12
ES2617905T3 (es) 2017-06-20
KR20150063517A (ko) 2015-06-09
EA201500394A1 (ru) 2015-11-30
EP2903968B1 (en) 2016-12-07
BR112015007083A2 (pt) 2017-07-04
DK2903968T3 (en) 2017-01-30
PE20150998A1 (es) 2015-06-29
ES2654143T3 (es) 2018-02-12
WO2014053491A1 (en) 2014-04-10
CN107434803A (zh) 2017-12-05
EP3023415A1 (en) 2016-05-25
LT2903968T (lt) 2017-02-27
PL2903968T3 (pl) 2017-05-31
JP2015532295A (ja) 2015-11-09
SG11201502452RA (en) 2015-05-28
SI2903968T1 (sl) 2017-03-31
PH12015500730A1 (en) 2015-06-01
SG10201703682YA (en) 2017-06-29
PT2903968T (pt) 2017-03-13
US20140371195A1 (en) 2014-12-18
HRP20170358T1 (hr) 2017-04-21
CN104981458B (zh) 2017-07-21
AU2018200876B2 (en) 2019-09-19
SI3023415T1 (en) 2018-01-31
HK1207373A1 (en) 2016-01-29
CA2885969C (en) 2021-04-06
RS55764B1 (sr) 2017-07-31
EP3023415B1 (en) 2017-12-06
HUE033380T2 (en) 2017-11-28
JP2018016661A (ja) 2018-02-01
PH12017501306A1 (en) 2019-02-27
JP6530313B2 (ja) 2019-06-12

Similar Documents

Publication Publication Date Title
AU2018200876C1 (en) Inhibitors of histone demethylases
EP2961736B1 (en) Inhibitors of histone demethylases
CA2957947A1 (en) Compounds and methods for inhibiting histone demethylases
Class et al. Patent application title: INHIBITORS OF HISTONE DEMETHYLASES
HK1235404A1 (en) Inhibitors of histone demethylases
HK1223612B (en) Inhibitors of histone demethylases
HK1207373B (en) Inhibitors of histone demethylases
OA17265A (en) Inhibitors of histone demethylases.
HK1247920B (zh) 组蛋白去甲基化酶抑制剂
HK1236522A1 (en) Ethyl pyridine-4-carboxylate compound as inhibitor of histone demethylases
HK1247920A1 (zh) 组蛋白去甲基化酶抑制剂
HK1218539B (en) Inhibitors of histone demethylases

Legal Events

Date Code Title Description
DA2 Applications for amendment section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 24 OCT 2019

PC1 Assignment before grant (sect. 113)

Owner name: GILEAD SCIENCES, INC.

Free format text: FORMER APPLICANT(S): EPITHERAPEUTICS APS

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT FILED 24 OCT 2019

FGA Letters patent sealed or granted (standard patent)