CA3060416A1 - Combination therapies with ehmt2 inhibitors - Google Patents

Combination therapies with ehmt2 inhibitors Download PDF

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Publication number
CA3060416A1
CA3060416A1 CA3060416A CA3060416A CA3060416A1 CA 3060416 A1 CA3060416 A1 CA 3060416A1 CA 3060416 A CA3060416 A CA 3060416A CA 3060416 A CA3060416 A CA 3060416A CA 3060416 A1 CA3060416 A1 CA 3060416A1
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CA
Canada
Prior art keywords
inhibitor
halo
optionally substituted
alkyl
independently
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.)
Pending
Application number
CA3060416A
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English (en)
French (fr)
Inventor
John Emmerson CAMPBELL
Kenneth William Duncan
Maria Alejandra Raimondi
Christine Klaus
Elayne Penebre
Original Assignee
Epizyme Inc
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Publication of CA3060416A1 publication Critical patent/CA3060416A1/en
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A61K31/203—Retinoic acids ; Salts thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/444—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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CA3060416A 2017-04-21 2018-04-20 Combination therapies with ehmt2 inhibitors Pending CA3060416A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762488679P 2017-04-21 2017-04-21
US62/488,679 2017-04-21
US201762574147P 2017-10-18 2017-10-18
US62/574,147 2017-10-18
PCT/US2018/028609 WO2018195450A1 (en) 2017-04-21 2018-04-20 Combination therapies with ehmt2 inhibitors

Publications (1)

Publication Number Publication Date
CA3060416A1 true CA3060416A1 (en) 2018-10-25

Family

ID=63856173

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3060416A Pending CA3060416A1 (en) 2017-04-21 2018-04-20 Combination therapies with ehmt2 inhibitors

Country Status (7)

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US (2) US11672800B2 (enExample)
EP (1) EP3612181A4 (enExample)
JP (2) JP2020517618A (enExample)
CN (2) CN110621316B (enExample)
AU (1) AU2018254577B2 (enExample)
CA (1) CA3060416A1 (enExample)
WO (1) WO2018195450A1 (enExample)

Families Citing this family (96)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016298175B2 (en) 2015-07-28 2022-01-06 University Of Iowa Research Foundation Compositions and methods of treating cancer
IL297201A (en) 2016-03-01 2022-12-01 Corcept Therapeutics Inc Use of glucocorticoid receptor modulators to increase the activity of checkpoint inhibitors
JP2019533022A (ja) 2016-10-24 2019-11-14 ユマニティ セラピューティクス，インコーポレーテッド 化合物及びその使用
EP3566055B1 (en) 2017-01-06 2025-03-12 Janssen Pharmaceutica NV Scd inhibitor for the treatment of neurological disorders
WO2019050924A1 (en) * 2017-09-05 2019-03-14 Epizyme, Inc. POLY THERAPY FOR THE TREATMENT OF CANCER
CA3079260A1 (en) * 2017-10-17 2019-04-25 Epizyme, Inc. Amine-substituted heterocyclic compounds as ehmt2 inhibitors and derivatives thereof
AU2018353139A1 (en) * 2017-10-18 2020-06-04 Epizyme, Inc. Methods of using EHMT2 inhibitors in immunotherapies
JP2021500326A (ja) * 2017-10-18 2021-01-07 エピザイム，インコーポレイティド 血液障害の予防又は処置にｅｈｍｔ２阻害剤を使用する方法
CA3083000A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. Compounds and uses thereof
CN118416236A (zh) 2018-01-31 2024-08-02 德西费拉制药有限责任公司 治疗胃肠道间质瘤的组合疗法
IL276398B2 (en) 2018-01-31 2026-03-01 Deciphera Pharmaceuticals Llc Combination therapy for mastocytosis
CN112105602A (zh) * 2018-03-01 2020-12-18 反应生物公司 基于喹啉和异喹啉的hdac抑制剂及其使用方法
WO2019183587A1 (en) 2018-03-23 2019-09-26 Yumanity Therapeutics, Inc. Compounds and uses thereof
CN117285467A (zh) 2018-07-31 2023-12-26 罗索肿瘤学公司 喷雾干燥的分散体和制剂
CA3109605A1 (en) 2018-08-13 2020-02-20 Beijing Percans Oncology Co. Ltd. Biomarkers for cancer therapy
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11476430B2 (en) * 2018-10-15 2022-10-18 Universal Display Corporation Organic electroluminescent materials and devices
US12522583B2 (en) 2018-11-07 2026-01-13 Dana-Farber Cancer Institute, Inc. Benzimidazole derivatives and aza-benzimidazole derivatives as Janus kinase 2 inhibitors and uses thereof
EP3877371A4 (en) 2018-11-07 2022-07-27 Dana-Farber Cancer Institute, Inc. IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF
EP3876939A4 (en) 2018-11-07 2022-08-10 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
WO2020154571A1 (en) 2019-01-24 2020-07-30 Yumanity Therapeutics, Inc. Compounds and uses thereof
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020185812A1 (en) 2019-03-11 2020-09-17 Teva Pharmaceuticals International Gmbh Solid state forms of ripretinib
WO2020198026A1 (en) * 2019-03-22 2020-10-01 Yumanity Therapeutics, Inc. Compounds and uses thereof
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
WO2020216669A1 (de) 2019-04-23 2020-10-29 Bayer Aktiengesellschaft Phenylsubstituierte imidazopyridinamide und ihre verwendung
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
EP3886946A1 (en) 2019-06-05 2021-10-06 Regeneron Pharmaceuticals, Inc. Devices and methods for precision dose delivery
WO2020259683A1 (zh) * 2019-06-28 2020-12-30 成都赜灵生物医药科技有限公司 2，4-二取代嘧啶衍生物及其制备方法和用途
US12527818B2 (en) * 2019-07-11 2026-01-20 Emory University Platinum-based chemotherapy, mast binding agents, glucocorticoid receptor (GR) binding agents, and/or HSP90 binding agents for uses in treating cancer
US12377063B2 (en) * 2019-07-11 2025-08-05 Emory University Combination therapies for managing cancer
TWI878335B (zh) 2019-08-12 2025-04-01 美商迪賽孚爾製藥有限公司 治療胃腸道基質瘤方法
EP4013412B1 (en) 2019-08-12 2026-01-28 Deciphera Pharmaceuticals, LLC Ripretinib for treating gastrointestinal stromal tumors
CA3150681A1 (en) 2019-08-14 2021-02-18 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
CN110623942B (zh) * 2019-09-30 2020-09-22 武汉大学 一种全反式维甲酸纳米药物制剂、其制备方法及应用
EP4041399A1 (en) 2019-10-02 2022-08-17 Tolremo Therapeutics AG Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment or amelioration of cancer
US11851426B2 (en) 2019-10-11 2023-12-26 Incyte Corporation Bicyclic amines as CDK2 inhibitors
KR20220098755A (ko) * 2019-11-05 2022-07-12 애브비 인코포레이티드 나비토클락스를 사용한 골수섬유증 및 mpn 관련 장애 치료에 사용하기 위한 투약 레지멘
EA202192047A1 (ru) 2019-11-13 2021-12-08 Юманити Терапьютикс, Инк. Соединения и их применение
US12064507B2 (en) 2019-11-19 2024-08-20 Provectus Pharmatech, Inc. Composition and method for oral treatment of leukemia
WO2021102674A1 (zh) * 2019-11-26 2021-06-03 深圳先进技术研究院 靶向AMPK的抑制剂/siRNA与蛋白酶体抑制剂组合在抗肿瘤中的应用
BR112022010924A2 (pt) 2019-12-06 2022-09-06 Vertex Pharma Tetra-hidrofuranos substituídos como moduladores de canais de sódio
EP4084779B1 (en) 2019-12-30 2024-10-09 Deciphera Pharmaceuticals, LLC Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
MX2022008103A (es) 2019-12-30 2022-09-19 Deciphera Pharmaceuticals Llc Formulaciones de inhibidores de la cinasa amorfa y metodos de estas.
BR112022015011A2 (pt) * 2020-01-29 2022-09-20 Corcept Therapeutics Inc Método para tratar um sujeito que sofre de tumor de carcinoma adrenocortical e tendo excesso de cortisol, e, composição farmacêutica para tratar carcinoma adrenocortical
EP4117718A4 (en) * 2020-03-09 2024-05-08 University of Houston System INFLAMMATORY BOWEL DISEASE (IBD)-ASSOCIATED STEM CELLS, AGENTS TARGETING IBD-ASSOCIATED STEM CELLS AND RELATED USES THEREOF
CN113372364B (zh) * 2020-03-10 2024-05-31 明慧医药（上海）有限公司 一类jak激酶抑制剂及其制备和应用
TW202208355A (zh) 2020-05-04 2022-03-01 美商安進公司 作為骨髓細胞觸發受體2促效劑之雜環化合物及使用方法
JP7741100B2 (ja) 2020-05-04 2025-09-17 アムジェン インコーポレイテッド ミエロイド細胞に発現するトリガー受容体２アゴニストとしての複素環化合物及び使用方法
US11691963B2 (en) 2020-05-06 2023-07-04 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
AU2021280314A1 (en) * 2020-05-28 2022-12-08 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
WO2021249240A1 (zh) * 2020-06-11 2021-12-16 养生堂有限公司 Palovarotene在抗hbv病毒治疗中的用途
BR112022025911A2 (pt) * 2020-06-25 2023-01-10 Tolremo Therapeutics Ag Combinação de um inibidor de bromodomínio de cbp/p300 e um inibidor de egfr para uso no tratamento de um cpcnp com egfr mutante
KR20230028798A (ko) 2020-06-25 2023-03-02 톨레모 테라퓨틱스 아게 암 치료를 위한 CBP/p300 브로모도메인 억제제 및 KRAS 억제제의 조합물
EP4178958A4 (en) * 2020-07-10 2024-12-11 Blossomhill Therapeutics, Inc. MACROCYCLES AND THEIR USE
US11529335B2 (en) * 2020-07-31 2022-12-20 University Of Iowa Research Foundation Compositions and methods for treating cancer
AR123185A1 (es) 2020-08-10 2022-11-09 Novartis Ag Compuestos y composiciones para inhibir ezh2
EP4230624A4 (en) * 2020-09-21 2024-07-10 The Asan Foundation Quinazoline-2,4-diamine derivative and pharmaceutical composition for preventing or treating cancer comprising same as active ingredient
CN112274517A (zh) * 2020-10-30 2021-01-29 江苏大学 一种治疗套细胞淋巴瘤的药物组合物
CN116761607A (zh) * 2020-12-11 2023-09-15 阿尔维纳斯运营股份有限公司 治疗前列腺癌的方法
US12043632B2 (en) 2020-12-23 2024-07-23 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
CN116888107B (zh) * 2021-02-19 2026-04-21 微境生物医药科技(上海)有限公司 作为Wee-1抑制剂的稠环化合物
CA3208361A1 (en) 2021-02-19 2022-08-25 Anjali Pandey Tyk2 inhibitors and uses thereof
EP4294806A1 (en) 2021-02-19 2023-12-27 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof
AU2022222470A1 (en) 2021-02-19 2023-09-21 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof
IL307402A (en) 2021-04-07 2023-12-01 Tolremo Therapeutics Ag The tercyclic derivatives, pharmaceutical compounds and their use in the treatment or amelioration of cancer
MX2022012945A (es) * 2021-04-16 2023-03-16 Provectus Pharmatech Inc Composición y método para el tratamiento de la leucemia oral.
CN113288871B (zh) * 2021-05-28 2022-09-16 华中科技大学 用于调控表观遗传与免疫检查点的药物组合物脂质体制剂
SMT202500481T1 (it) 2021-06-04 2026-01-12 Vertex Pharma N-(idrossialchil(etero)aril)tetraidrofuran carbossammidi come modulatori di canali del sodio
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
JP2024525368A (ja) * 2021-07-01 2024-07-12 エアリー ファーマシューティカルズ インコーポレイテッド アゼチジニルピリミジンおよびその使用
CN113425851B (zh) * 2021-07-09 2021-12-17 南京市儿童医院 修饰bix-01294的金纳米星制备方法及其应用
CN113735859A (zh) * 2021-08-12 2021-12-03 安徽医科大学 一种激酶抑制剂
EP4134077A1 (en) * 2021-08-13 2023-02-15 ScandiEdge Therapeutics AB Small molecule treatment of fatty liver disease and hcc
US20230062911A1 (en) * 2021-09-02 2023-03-02 Rutgers, The State University Of New Jersey Compositions and methods for treating, preventing, and/or ameliorating chemotherapy-induced premature ovarian failure (pof)
JP2024538128A (ja) * 2021-10-15 2024-10-18 タンゴ セラピューティクス， インコーポレイテッド Ｅｈｍｔ１及びｅｈｍｔ２の新規調節因子及びその治療用途
PT4426434T (pt) 2021-11-02 2025-11-24 Flare Therapeutics Inc Agonistas inversos de pparg e suas utilizações
US12162881B2 (en) 2021-11-09 2024-12-10 Ajax Therapeutics, Inc. Forms and compositions of inhibitors of JAK2
WO2023086319A1 (en) 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. 6-he tero aryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
WO2023092394A1 (en) * 2021-11-25 2023-06-01 Guo Dagang Methods and compositions for treating ewing family of tumors
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
MX2024008057A (es) 2021-12-30 2024-08-28 Biomea Fusion Inc Compuestos de pirazina como inhibidores de flt3.
MX2024008868A (es) 2022-01-18 2024-09-23 Maze Therapeutics Inc Inhibidores de la apolipoproteína l1 (apol1) y métodos de uso.
CN115137731B (zh) * 2022-05-19 2023-11-21 上海交通大学医学院附属新华医院 Flt3抑制剂及其药学上可接受的盐在制备治疗皮肤t细胞淋巴瘤药物中的应用
CN115300493A (zh) * 2022-07-12 2022-11-08 厦门大学 核受体RXRα配体的应用及抗肿瘤药物
CN115197167B (zh) * 2022-07-22 2023-07-28 中国药科大学 1,2,4-噻二唑烷-3,5-二酮化合物及其制备方法和应用
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors
CN117800894A (zh) * 2022-09-30 2024-04-02 苏州阿尔脉生物科技有限公司 饱和环类衍生物、包含其的药物组合物及其医药用途
CN115487185A (zh) * 2022-10-18 2022-12-20 四川大学华西医院 G007-lk在治疗小细胞肺癌中的应用
USD1120314S1 (en) 2022-11-30 2026-03-24 Regeneron Pharmaceuticals, Inc. Dose delivery device
WO2025015106A2 (en) * 2023-07-11 2025-01-16 Maze Therapeutics, Inc. Apol1 inhibitors and methods of use thereof
WO2025043183A1 (en) * 2023-08-23 2025-02-27 Eigen Therapeutics Inc. Methods and compositions for treating hematological cancers
KR20250088371A (ko) * 2023-12-08 2025-06-17 인제대학교 산학협력단 Ezh2 저해제 및 jak3 억제제를 포함하는 암의 예방 또는 치료용 약학적 조성물

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2443305A (en) 1948-06-15 Pyrimidine derivatives
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
SE8604566D0 (sv) 1986-10-27 1986-10-27 Haessle Ab Novel compunds
GB8820231D0 (en) 1988-08-25 1988-09-28 Fujisawa Pharmaceutical Co New benzazole compounds processes for preparation thereof & pharmaceutical composition comprising same
US5247083A (en) 1992-07-10 1993-09-21 Syntex (U.S.A.) Inc. Direct esterification of mycophenolic acid
EP0585500A1 (en) 1992-09-04 1994-03-09 Merrell Dow Pharmaceuticals Inc. Diaryl piperazineacetamides as antimuscarinic agents
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
AU2207897A (en) 1996-03-11 1997-10-01 Eli Lilly And Company Methods of treating or preventing interstitial cystitis
KR100643419B1 (ko) 1998-03-27 2006-11-10 얀센 파마슈티카 엔.브이. Ｈｉｖ를 억제하는 피리미딘 유도체
WO2000025780A1 (en) 1998-10-29 2000-05-11 Bristol-Myers Squibb Company Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
US6596747B2 (en) 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
US6391907B1 (en) 1999-05-04 2002-05-21 American Home Products Corporation Indoline derivatives
US6355648B1 (en) 1999-05-04 2002-03-12 American Home Products Corporation Thio-oxindole derivatives
US6906067B2 (en) 1999-12-28 2005-06-14 Bristol-Myers Squibb Company N-heterocyclic inhibitors of TNF-α expression
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
WO2001055119A2 (en) 2000-01-25 2001-08-02 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
TW593278B (en) 2001-01-23 2004-06-21 Wyeth Corp 1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
MXPA03007513A (es) 2001-02-21 2004-07-30 Nps Pharma Inc Compuestos heteropoliciclicos y su uso como antagonistas del receptor metabotropico de glutamato.
WO2003040141A1 (en) 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
WO2003032994A2 (de) 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg 5-substituierte 4-amino-2-phenylamino-pyrimidinderivate und ihre verwendung als beta-amyloid modulatoren
FR2833948B1 (fr) 2001-12-21 2004-02-06 Sod Conseils Rech Applic Nouveaux derives de benzimidazole et leur utilisation en tant que medicament
EP1470121B1 (en) 2002-01-23 2012-07-11 Bayer HealthCare LLC Pyrimidine derivatives as rho-kinase inhibitors
AR039540A1 (es) 2002-05-13 2005-02-23 Tibotec Pharm Ltd Compuestos microbicidas con contenido de pirimidina o triazina
US20040082627A1 (en) 2002-06-21 2004-04-29 Darrow James W. Certain aromatic monocycles as kinase modulators
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
US7419984B2 (en) 2002-10-17 2008-09-02 Cell Therapeutics, Inc. Pyrimidines and uses thereof
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
ATE506953T1 (de) 2003-08-07 2011-05-15 Rigel Pharmaceuticals Inc 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
US20070105839A1 (en) 2003-09-18 2007-05-10 Patricia Imbach 2, 4-Di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
KR20060118472A (ko) 2003-10-16 2006-11-23 카이론 코포레이션 치환 벤자졸 및 ｒａｆ 키나아제의 저해제로서 그것의 사용
US20070293484A1 (en) 2004-05-20 2007-12-20 Sugen, Inc. Thiophene Heteroaryl Amines
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
JP2008511659A (ja) 2004-09-01 2008-04-17 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物の合成
US20070032493A1 (en) 2005-05-26 2007-02-08 Synta Pharmaceuticals Corp. Method for treating B cell regulated autoimmune disorders
EP1746096A1 (en) 2005-07-15 2007-01-24 4Sc Ag 2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer
DK1910384T3 (da) 2005-08-04 2012-12-17 Sirtris Pharmaceuticals Inc Imidazo [2,1-b] thiazol-derivater som sirtuinmodulerende forbindelser
WO2007038387A2 (en) 2005-09-23 2007-04-05 Yale University Compounds and methods for the treatment of viruses and cancer
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
JP5191391B2 (ja) 2005-11-01 2013-05-08 ターゲジェン インコーポレーティッド キナーゼのビ−アリールメタ−ピリミジン阻害剤
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
FR2897061B1 (fr) 2006-02-03 2010-09-03 Sanofi Aventis Derives de n-heteroaryl-carboxamides tricycliques contenant un motif benzimidazole, leur preparation et leur application en therapeutique.
PE20081636A1 (es) 2007-01-26 2009-01-10 Smithkline Beecham Corp Inhibidores de antranilamida para aurora quinasa
JP5450381B2 (ja) 2007-04-30 2014-03-26 プロメティック・バイオサイエンスィズ・インコーポレーテッド 化合物、そのような化合物を含有する組成物、及びそのような化合物を用いるがん及び自己免疫疾患の治療法
JP5389785B2 (ja) 2007-05-02 2014-01-15 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤として有用なチアゾールおよびピラゾール
JP5710251B2 (ja) 2007-06-07 2015-04-30 イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． 新規ヘテロ環化合物およびその使用
CN101903357A (zh) 2007-07-17 2010-12-01 里格尔药品股份有限公司 作为pkc抑制剂的环状胺取代的嘧啶二胺
JP5328816B2 (ja) 2008-02-22 2013-10-30 エフ．ホフマン−ラ ロシュ アーゲー アミロイドβの調節薬
WO2009126537A1 (en) 2008-04-07 2009-10-15 Syndax Pharmaceuticals, Inc. Administration of an inhibitor of hdac and an hmt inhibitor
SG165655A1 (en) 2008-04-16 2010-11-29 Portola Pharm Inc 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors
WO2010002985A1 (en) 2008-07-01 2010-01-07 Ptc Therapeutics, Inc. Bmi-1 protein expression modulators
UY31982A (es) 2008-07-16 2010-02-26 Boehringer Ingelheim Int Derivados de 1,2-dihidropiridin-3-carboxamidas n-sustituidas
AU2009279825A1 (en) 2008-08-05 2010-02-11 Targegen, Inc. Methods of treating thalassemia
KR20110049905A (ko) 2008-09-03 2011-05-12 바이엘 크롭사이언스 아게 4-알킬-치환된 디아미노피리미딘
JP5781942B2 (ja) 2009-01-14 2015-09-24 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物を用いた炎症性障害の治療法
JP5781943B2 (ja) 2009-01-21 2015-09-24 ライジェル ファーマシューティカルズ， インコーポレイテッド 炎症性疾患、自己免疫疾患または増殖性疾患の治療に有用なｎ２−（３−ピリジルまたはフェニル）−ｎ４−（４−ピペリジル）−２，４−ピリミジンジアミン誘導体
BRPI1006942A2 (pt) 2009-01-23 2016-04-12 Rigel Pharmaceuticals Inc composto, composição farmacêutica, kit, métodos para inibir uma atividade de uma jak quinase, para tratar uma doença, para tratar a rejeição de transplante de aloenxerto em um receptor de transplante, para tratar uma reação de hipersensibilidade, e para inibir uma cascata de transdução de sinal, e, uso do composto
US20100317706A1 (en) 2009-04-30 2010-12-16 Bumham Institute For Medical Research HNF4alpha MODULATORS AND METHODS OF USE
US8367689B2 (en) 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK
JP2012197231A (ja) 2009-08-06 2012-10-18 Oncotherapy Science Ltd Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体
WO2011032169A2 (en) 2009-09-14 2011-03-17 Phusis Therapeutics Inc. Pharmaceutical compositions and formulations including inhibitors of the pleckstrin homology domain and methods for using same
AT509266B1 (de) 2009-12-28 2014-07-15 Univ Wien Tech Substituierte pyridine und pyrimidine
JP2013523657A (ja) 2010-03-26 2013-06-17 グラクソ グループ リミテッド キナーゼ阻害剤としてのインダゾリル‐ピリミジン
CN102242146B (zh) 2010-05-10 2015-11-25 高丽大学校产学协力团 组合物和用其产生诱导全能干细胞的方法
WO2012023285A1 (en) * 2010-08-20 2012-02-23 Oncotherapy Science, Inc. Ehmt2 as a target gene for cancer therapy and diagnosis
BR112013005806B1 (pt) 2010-09-10 2022-05-10 Epizyme, Inc Métodos para detectar se um indivíduo é um candidato para o tratamento com ou responsivo a um inibidor de ezh2 e usos terapêuticos do dito inibidor de ezh2
WO2012038417A1 (en) 2010-09-20 2012-03-29 Institut National De La Sante Et De La Recherche Medicale (Inserm) Substituted amino - benzoic acid derivatives as inhibitors of dna methyltransferases
WO2012044936A1 (en) 2010-09-30 2012-04-05 Portola Pharmaceuticals, Inc. Combination therapy with 4-(3-(2h-1,2,3-triazol-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide
US9714427B2 (en) 2010-11-11 2017-07-25 The University Of North Carolina At Chapel Hill Methods and compositions for unsilencing imprinted genes
US20130310379A1 (en) 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
KR101682417B1 (ko) 2011-02-25 2016-12-06 주식회사유한양행 다이아미노피리미딘 유도체 및 그의 제조방법
TW201733984A (zh) * 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
JO3363B1 (ar) * 2011-04-13 2019-03-13 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
IN2014CN02646A (enExample) 2011-09-14 2015-08-07 Samumed Llc
WO2013070852A2 (en) 2011-11-08 2013-05-16 Emory University Compounds and compositions used to epigenetically transform cells and methods related thereto
CA2856306A1 (en) 2011-11-23 2013-05-30 Portola Pharmaceuticals, Inc. Selective kinase inhibitors
KR101452235B1 (ko) 2012-02-03 2014-10-22 서울대학교산학협력단 신규한 피리미딘계 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 ｒａｇｅ 수용체 관련 질환의 예방 또는 치료용 약학적 조성물
AU2013237226A1 (en) 2012-03-19 2014-10-09 Emory University Quinazoline compounds and their use in therapy
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
EP2863913B1 (en) 2012-06-20 2018-09-12 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
WO2014058921A2 (en) 2012-10-08 2014-04-17 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
US9145412B2 (en) 2012-11-02 2015-09-29 Acetylon Pharmaceuticals, Inc. Selective HDAC1 and HDAC2 inhibitors
EP2928891B1 (en) 2012-12-04 2019-02-20 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
MX2015009952A (es) 2013-02-08 2015-10-05 Celgene Avilomics Res Inc Inhibidores de cinasas reguladas por señales extracelulares (erk) y sus usos.
CN103172637B (zh) 2013-03-13 2015-05-27 上海大学 嘧啶并[1,2-a]苯并咪唑类化合物及其制备方法
CA2904610A1 (en) 2013-03-14 2014-09-25 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
US20150087673A1 (en) 2013-09-26 2015-03-26 Rigel Pharmaceuticals, Inc. Methods for using and biomarkers for ampk-activating compounds
US9556126B2 (en) 2013-12-20 2017-01-31 Signal Pharmaceuticals, Llc Substituted diaminopyrimidyl compounds, compositions thereof, and methods of treatment therewith
US20150250824A1 (en) 2014-03-07 2015-09-10 The Research Foundation For The State University Of New York Methods and compositions for expansion of stem cells and other cells
US9284272B2 (en) * 2014-03-28 2016-03-15 Abbvie Inc. Inhibitors of histone methyltransferase G9a
CN106536509B (zh) 2014-06-16 2020-06-09 基础应用医学研究基金会 作为组蛋白甲基转移酶和dna甲基转移酶的双重抑制剂的新型化合物
EP3157524A4 (en) * 2014-06-23 2017-12-06 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
WO2016073956A1 (en) 2014-11-06 2016-05-12 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
WO2017061957A1 (en) * 2015-10-09 2017-04-13 Agency For Science, Technology And Research Compounds for treatment of cancer and epigenetics
AU2016356884A1 (en) 2015-11-16 2018-06-21 Fundación Para La Investigación Médica Aplicada Novel compounds as inhibitors of dna methyltransferases
WO2017090719A1 (ja) 2015-11-27 2017-06-01 大鵬薬品工業株式会社 縮環ピリミジン化合物又はその塩
US20190127354A1 (en) 2015-12-14 2019-05-02 Fundación Para La Investigación Médica Aplicada 2,4,6,7-tetrasubstituted quinoline compounds as inhibitors of dna methyltransferases
EP3416963B1 (en) 2016-02-17 2021-07-28 Global Blood Therapeutics, Inc. Histone methyltransferase inhibitors
CN108884074B (zh) 2016-04-15 2021-07-02 先正达参股股份有限公司 除草哒嗪酮化合物
PT3442972T (pt) 2016-04-15 2020-05-29 Abbvie Inc Inibidores de bromodomínio
CN109311889B (zh) 2016-04-15 2021-11-16 缆图药品公司 激活素受体样激酶抑制剂
PL3442947T3 (pl) * 2016-04-15 2023-10-02 Epizyme, Inc. Związki arylowe lub heteroarylowe podstawione aminą jako inhibitory ehmt1 i ehmt2
AU2017251155B2 (en) 2016-04-15 2021-08-05 Elanco Animal Health Gmbh Pyrazolopyrimidine derivatives
IL263412B (en) 2016-06-03 2022-08-01 Univ Columbia Treatment methods for Freder Willi syndrome
FR3052452B1 (fr) 2016-06-10 2018-06-22 Les Laboratoires Servier Nouveaux derives de piperidinyle, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
GEP20207161B (en) 2016-06-10 2020-10-12 Servier Lab New (hetero)aryl-substituted-piperidinyl derivatives, a process for their preparation and pharmaceutical compositions containing them
CA3028228A1 (en) 2016-06-10 2017-12-14 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
CA3037587A1 (en) 2016-09-30 2018-04-05 Epizyme, Inc. Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors
US10537590B2 (en) 2016-09-30 2020-01-21 Boehringer Ingelheim International Gmbh Cyclic dinucleotide compounds
US20200039998A1 (en) 2016-12-19 2020-02-06 Epizyme, Inc. Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
JP7091336B2 (ja) 2016-12-22 2022-06-27 グローバル ブラッド セラピューティクス インコーポレイテッド ヒストンメチルトランスフェラーゼ阻害剤
WO2018119263A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds derivatives as pd-l1 internalization inducers
US20200113901A1 (en) 2017-03-31 2020-04-16 Epizyme, Inc. Methods of using ehmt2 inhibitors
EP3668863B1 (en) 2017-08-15 2025-03-19 Global Blood Therapeutics, Inc. Tricyclic compounds as histone methyl-transferase inhibitors
CA3079260A1 (en) 2017-10-17 2019-04-25 Epizyme, Inc. Amine-substituted heterocyclic compounds as ehmt2 inhibitors and derivatives thereof
JP2021500326A (ja) 2017-10-18 2021-01-07 エピザイム，インコーポレイティド 血液障害の予防又は処置にｅｈｍｔ２阻害剤を使用する方法
AU2018353139A1 (en) 2017-10-18 2020-06-04 Epizyme, Inc. Methods of using EHMT2 inhibitors in immunotherapies
JP2021500334A (ja) 2017-10-18 2021-01-07 エピザイム，インコーポレイティド Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法

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