PL2961736T3 - Inhibitory demetylaz histonowych - Google Patents

Inhibitory demetylaz histonowych

Info

Publication number
PL2961736T3
PL2961736T3 PL14706607T PL14706607T PL2961736T3 PL 2961736 T3 PL2961736 T3 PL 2961736T3 PL 14706607 T PL14706607 T PL 14706607T PL 14706607 T PL14706607 T PL 14706607T PL 2961736 T3 PL2961736 T3 PL 2961736T3
Authority
PL
Poland
Prior art keywords
inhibitors
histone demethylases
demethylases
histone
Prior art date
Application number
PL14706607T
Other languages
English (en)
Inventor
Marc Labelle
Thomas Boesen
Qasim Khan
Ramkrishna Reddy VAKITI
Utpal SHARMA
Ying Yang
Mukund Mehrotra
Neerja Saraswat
Farman ULLAH
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 PL2961736T3 publication Critical patent/PL2961736T3/pl

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40Acylated substituent nitrogen atom
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79Acids; Esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/537Heterocyclic 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 spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
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    • C07C55/06Oxalic acid
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    • C07C59/235Saturated compounds containing more than one carboxyl group
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    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
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    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D307/56Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or 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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    • C07D401/12Heterocyclic 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
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
PL14706607T 2013-02-27 2014-02-26 Inhibitory demetylaz histonowych PL2961736T3 (pl)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201361770065P 2013-02-27 2013-02-27
US201361770067P 2013-02-27 2013-02-27
US201361770058P 2013-02-27 2013-02-27
DKPA201370115 2013-02-27
DKPA201370114 2013-02-27
DKPA201370113 2013-02-27
US201461931126P 2014-01-24 2014-01-24
PCT/EP2014/053674 WO2014131777A1 (en) 2013-02-27 2014-02-26 Inhibitors of histone demethylases
EP14706607.0A EP2961736B1 (en) 2013-02-27 2014-02-26 Inhibitors of histone demethylases

Publications (1)

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PL2961736T3 true PL2961736T3 (pl) 2018-08-31

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US (2) US9650339B2 (pl)
EP (2) EP3170811A1 (pl)
JP (2) JP6514117B2 (pl)
KR (1) KR102229992B1 (pl)
CN (1) CN105263906B (pl)
AP (1) AP2015008676A0 (pl)
AU (2) AU2014222756B2 (pl)
BR (1) BR112015020650A2 (pl)
CA (1) CA2901022C (pl)
CL (1) CL2015002394A1 (pl)
CR (1) CR20150507A (pl)
EA (1) EA030451B1 (pl)
ES (1) ES2670864T3 (pl)
IL (1) IL240439A0 (pl)
MD (1) MD20150085A2 (pl)
MX (1) MX2015011097A (pl)
PE (1) PE20151667A1 (pl)
PH (1) PH12015501868A1 (pl)
PL (1) PL2961736T3 (pl)
SG (2) SG11201506717UA (pl)
SI (1) SI2961736T1 (pl)
TR (1) TR201808599T4 (pl)
WO (1) WO2014131777A1 (pl)

Families Citing this family (56)

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Publication number Priority date Publication date Assignee Title
CN107434803B (zh) 2012-10-02 2020-05-05 吉利德科学公司 组蛋白去甲基化酶抑制剂
EP3170811A1 (en) 2013-02-27 2017-05-24 Gilead Sciences, Inc. Ethyl pyridine-4-carboxylate compound as inhibitor of histone demethylases
WO2015153498A1 (en) * 2014-03-31 2015-10-08 Epitherapeutics, Aps Inhibitors of histone demethylases
EA201790154A1 (ru) 2014-08-27 2017-08-31 Джилид Сайэнс, Инк. Соединения и способы для ингибирования гистоновых деметилаз
CN107001358A (zh) 2014-10-29 2017-08-01 东亚St株式会社 调节组蛋白赖氨酸脱甲基酶(kdm)催化活性的新型吡啶并嘧啶酮化合物
MA43925A (fr) * 2015-04-14 2018-12-05 Gilead Sciences Inc Procã‰dã‰s de traitement du virus de l'hã‰patite b
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
BR102017010009A2 (pt) 2016-05-27 2017-12-12 Gilead Sciences, Inc. Compounds for the treatment of hepatitis b virus infection
CN118178444A (zh) 2016-05-27 2024-06-14 吉利德科学公司 使用ns5a、ns5b或ns3抑制剂治疗乙型肝炎病毒感染的方法
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
WO2018045150A1 (en) 2016-09-02 2018-03-08 Gilead Sciences, Inc. 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators
CN117402852A (zh) 2016-10-14 2024-01-16 精密生物科学公司 对乙肝病毒基因组中的识别序列特异性的工程化大范围核酸酶
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
US20200155526A1 (en) * 2017-05-31 2020-05-21 The Children's Medical Center Corporation Targeting lysine demethylases (kdms) as a therapeutic strategy for diffuse large b-cell lymphoma
CN111278811B (zh) 2017-09-06 2024-08-23 转化药物开发有限责任公司 氨基苯并咪唑衍生物、治疗和抑制组蛋白脱乙酰基酶的方法
KR102492187B1 (ko) 2017-12-20 2023-01-27 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. Sting 어댑터 단백질을 활성화하는 포스포네이트 결합을 가진 3'3' 사이클릭 다이뉴클레오티드
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
WO2019154261A1 (zh) * 2018-02-09 2019-08-15 南京明德新药研发股份有限公司 与kmd5通路相关的吡啶衍生物
EP4227302A1 (en) 2018-02-13 2023-08-16 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
KR102526964B1 (ko) 2018-02-26 2023-04-28 길리애드 사이언시즈, 인코포레이티드 Hbv 복제 억제제로서의 치환된 피롤리진 화합물
EP3774883A1 (en) 2018-04-05 2021-02-17 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
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
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
CN112041311B (zh) 2018-04-19 2023-10-03 吉利德科学公司 Pd-1/pd-l1抑制剂
TW202014193A (zh) 2018-05-03 2020-04-16 捷克科學院有機化學與生物化學研究所 包含碳環核苷酸之2’3’-環二核苷酸
CA3103286C (en) 2018-07-13 2023-05-09 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
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
JP2021534084A (ja) * 2018-08-06 2021-12-09 ダナ−ファーバー キャンサー インスティテュート,インコーポレイテッド ヒストンデメチラーゼ5阻害剤およびその使用
CN112955435B (zh) 2018-10-24 2024-09-06 吉利德科学公司 Pd-1/pd-l1抑制剂
JP7273172B2 (ja) 2018-10-31 2023-05-12 ギリアード サイエンシーズ, インコーポレイテッド Hpk1阻害活性を有する置換6-アザベンゾイミダゾール化合物
DK3873903T3 (da) 2018-10-31 2024-04-02 Gilead Sciences Inc Substituerede 6-azabenzimidazolforbindelser som hpk1-hæmmere
CN109852662B (zh) * 2018-12-25 2021-02-19 华南农业大学 组蛋白甲基化H3K4me3在猪卵巢颗粒细胞中的应用
US11766447B2 (en) 2019-03-07 2023-09-26 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3′3′-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
WO2020178769A1 (en) 2019-03-07 2020-09-10 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotides and prodrugs thereof
AU2020231115B2 (en) 2019-03-07 2025-02-20 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
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
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
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
CR20210687A (es) 2019-06-25 2022-03-03 Gilead Sciences Inc PROTEÍNAS DE FUSIÓN FLT3L-Fc Y MÉTODOS DE USO
WO2021011891A1 (en) 2019-07-18 2021-01-21 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
US20220296619A1 (en) 2019-08-19 2022-09-22 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
US11497808B2 (en) 2019-09-30 2022-11-15 Gilead Sciences, Inc. HBV vaccines and methods treating HBV
CN116057068A (zh) 2019-12-06 2023-05-02 精密生物科学公司 对乙型肝炎病毒基因组中的识别序列具有特异性的优化的工程化大范围核酸酶
WO2021188959A1 (en) 2020-03-20 2021-09-23 Gilead Sciences, Inc. Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same
US20230303599A1 (en) 2020-08-07 2023-09-28 Gilead Sciences, Inc. Prodrugs of phosphonamide nucleotide analogues and their pharmaceutical use
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
WO2022241134A1 (en) 2021-05-13 2022-11-17 Gilead Sciences, Inc. COMBINATION OF A TLR8 MODULATING COMPOUND AND ANTI-HBV siRNA THERAPEUTICS
EP4359413A1 (en) 2021-06-23 2024-05-01 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
JP7651018B2 (ja) 2021-06-23 2025-03-25 ギリアード サイエンシーズ, インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
WO2022271677A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
JP7654118B2 (ja) 2021-06-23 2025-03-31 ギリアード サイエンシーズ, インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物

Family Cites Families (44)

* 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
LU88769I2 (fr) 1982-07-23 1996-11-05 Zeneca Ltd Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R))
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
AU3732889A (en) * 1988-11-11 1990-05-28 Banyu Pharmaceutical Co., Ltd. Substituted allylamine derivatives, process for their preparation and their use
JPH03173865A (ja) * 1988-11-11 1991-07-29 Banyu Pharmaceut Co Ltd 置換アリルアミン誘導体、その製造法及びその用途
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
JP2001500851A (ja) 1996-08-30 2001-01-23 ノバルティス アクチエンゲゼルシャフト エポシロンの製造法および製造過程中に得られる中間生産物
EP0938597B1 (en) 1996-09-06 2003-08-20 Obducat Aktiebolag Method for anisotropic etching of structures in conducting materials
US5874438A (en) * 1996-10-11 1999-02-23 Bayer Aktiengesellschaft 2,2'-bridged bis-2,4-diaminoquinazolines
US5756517A (en) * 1996-10-25 1998-05-26 Bayer Aktiengesellschaft Use of bisquinoline compounds in the treatment of cerebral disorders
ES2312695T3 (es) 1996-11-18 2009-03-01 Gesellschaft Fur Biotechnologische Forschung Mbh (Gbf) Epotilones e y 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
MXPA00008365A (es) 1998-02-25 2002-11-07 Sloan Kettering Inst Cancer Sintesis de epotilonas, intermediarios y analogos de las mismas.
JP4662635B2 (ja) 1998-11-20 2011-03-30 コーサン バイオサイエンシーズ, インコーポレイテッド エポチロンおよびエポチロン誘導体を生成するための組換え方法および材料
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
EA200400648A1 (ru) * 2001-11-08 2005-04-28 Элан Фармасьютикалз, Инк. N, n'-замещенные производные 1,3-диамино-2-гидроксипропана
DOP2003000613A (es) 2002-03-13 2003-09-30 Array Biopharma Inc Derivados de bencimidazol n3 alquilado como inhibidores de mek (n3 alkylated benzimidazole derivatives as mek inhibitors)
WO2006129842A1 (ja) * 2005-06-01 2006-12-07 Banyu Pharmaceutical Co., Ltd. オーロラa選択的阻害作用を有する新規アミノピリジン誘導体
AU2007265368A1 (en) 2006-06-29 2008-01-03 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors
SA109300195B1 (ar) 2008-03-28 2013-04-20 Astrazeneca Ab تركيبة صيدلانية جديدة مضادة للسرطان
MX2011004553A (es) 2008-10-29 2011-07-20 Sirtris Pharmaceuticals Inc Piridina, piridina biciclica y analogos relacionados como moduladores de sirtuina.
AU2010279359A1 (en) 2009-08-07 2012-02-16 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
TWI592413B (zh) 2010-03-10 2017-07-21 英塞特公司 作為jak1抑制劑之哌啶-4-基三亞甲亞胺衍生物
WO2011148888A1 (ja) 2010-05-27 2011-12-01 あすか製薬株式会社 複素環化合物及びh1受容体拮抗剤
WO2012007008A1 (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
GB201112607D0 (en) * 2011-07-22 2011-09-07 Glaxo Group Ltd Novel compounds
WO2012071469A2 (en) 2010-11-23 2012-05-31 Nevada Cancer Institute Histone demethylase inhibitors and uses thereof for treatment o f cancer
WO2012135113A2 (en) 2011-03-25 2012-10-04 Glaxosmithkline Llc Cyclopropylamines as lsd1 inhibitors
HRP20201433T1 (hr) * 2011-08-15 2020-12-11 University Of Utah Research Foundation Supstituirani (e)-n´- (1-feniletiliden) analozi benzohidrazida kao inhibitori histonske demetilaze
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
CN107434803B (zh) 2012-10-02 2020-05-05 吉利德科学公司 组蛋白去甲基化酶抑制剂
ES2834959T3 (es) 2012-12-06 2021-06-21 Celgene Quanticel Res Inc Inhibidores de histona desmetilasa
ES2658597T3 (es) 2012-12-19 2018-03-12 Celgene Quanticel Research, Inc. Inhibidores de histona desmetilasa
EP2935217B1 (en) 2012-12-21 2019-02-27 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
EP3170811A1 (en) 2013-02-27 2017-05-24 Gilead Sciences, Inc. Ethyl pyridine-4-carboxylate compound as inhibitor of histone demethylases
CA2903465A1 (en) 2013-03-15 2014-09-25 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
CN105611933B (zh) 2013-09-05 2019-01-25 基因泰克公司 抗增生性化合物
WO2015153498A1 (en) 2014-03-31 2015-10-08 Epitherapeutics, Aps Inhibitors of histone demethylases

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