JP2020517618A - Ｅｈｍｔ２阻害剤との併用療法 - Google Patents

Ｅｈｍｔ２阻害剤との併用療法 Download PDF

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JP2020517618A
JP2020517618A JP2019556647A JP2019556647A JP2020517618A JP 2020517618 A JP2020517618 A JP 2020517618A JP 2019556647 A JP2019556647 A JP 2019556647A JP 2019556647 A JP2019556647 A JP 2019556647A JP 2020517618 A JP2020517618 A JP 2020517618A
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inhibitor
halo
alkyl
optionally substituted
independently
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JP2020517618A5 (Direct
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ジョン エマーソン キャンベル，
ジョン エマーソン キャンベル，
ケネス ウィリアム ダンカン，
ケネス ウィリアム ダンカン，
マリア アレジャンドラ ライモンディ，
マリア アレジャンドラ ライモンディ，
クリスティーン クラウス，
クリスティーン クラウス，
エレイン ペネブレ，
エレイン ペネブレ，
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エピザイム，インコーポレイティド
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
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    • 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
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    • 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
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    • 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
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  • 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 Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
JP2019556647A 2017-04-21 2018-04-20 Ｅｈｍｔ２阻害剤との併用療法 Withdrawn JP2020517618A (ja)

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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

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023532946A (ja) * 2020-07-10 2023-08-01 ブロッサムヒル・セラピューティクス・インコーポレイテッド 大員環分子およびそれらの使用

Families Citing this family (89)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017019664A1 (en) 2015-07-28 2017-02-02 University Of Iowa Research Foundation Compositions and methods of treating cancer
AU2017228329B2 (en) 2016-03-01 2021-03-11 Corcept Therapeutics, Inc. The use of glucocorticoid receptor modulators to potentiate checkpoint inhibitors
MA46589A (fr) 2016-10-24 2019-08-28 Yumanity Therapeutics Inc Composés et utilisations de ces derniers
AU2018205275B2 (en) 2017-01-06 2024-05-02 Janssen Pharmaceutica Nv Methods for the treatment of neurological disorders
EP3678663A4 (en) * 2017-09-05 2021-06-02 Epizyme, Inc. POLYTHERAPY FOR CANCER TREATMENT
WO2019079485A1 (en) * 2017-10-17 2019-04-25 Epizyme, Inc. AMINO-SUBSTITUTED HETEROCYCLIC COMPOUNDS AS EHMT2 INHIBITORS AND DERIVATIVES THEREOF
JP2021500327A (ja) * 2017-10-18 2021-01-07 エピザイム，インコーポレイティド 免疫療法にｅｈｍｔ２阻害剤を使用する方法
CA3081946A1 (en) * 2017-10-18 2019-04-25 Epizyme, Inc. Methods of using ehmt2 inhibitors in preventing or treating blood disorders
WO2019084157A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. COMPOUNDS AND USES THEREOF
AU2019215081B2 (en) 2018-01-31 2024-07-25 Deciphera Pharmaceuticals, Llc. Combination therapy for the treatment of gastrointestinal stromal tumors
CN111886006B (zh) 2018-01-31 2024-07-09 德西费拉制药有限责任公司 治疗肥大细胞增多症的组合疗法
WO2019169267A1 (en) * 2018-03-01 2019-09-06 Reaction Biology Corp. Quinoline and isoquinoline based hdac inhibitors and methods of use thereof
EA202092225A1 (ru) 2018-03-23 2021-02-09 Юманити Терапьютикс, Инк. Соединения и их применение
CN113194928A (zh) 2018-07-31 2021-07-30 罗索肿瘤学公司 (s)-5-氨基-3-(4-((5-氟-2-甲氧基苯甲酰胺基)甲基)苯基)-1-(1,1,1-三氟丙-2-基)-1h-吡唑-4-甲酰胺的喷雾干燥的分散体和制剂
JP7507145B2 (ja) 2018-08-13 2024-06-27 ベイジン パーカンズ オンコロジー カンパニー リミテッド 癌治療のためのバイオマーカー
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
EP3876930A4 (en) 2018-11-07 2022-07-20 Dana-Farber Cancer Institute, Inc. BENZIMIDAZOLE DERIVATIVES AND AZA-BENZIMIDAZOLE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND THEIR USES
EP3877371A4 (en) 2018-11-07 2022-07-27 Dana-Farber Cancer Institute, Inc. IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES USED AS JANUS KINASE 2 INHIBITORS AND ASSOCIATED USES
US12415816B2 (en) 2018-11-07 2025-09-16 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
US12098146B2 (en) 2019-01-24 2024-09-24 Janssen Pharmaceutica Nv Compounds and uses thereof
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020185812A1 (en) 2019-03-11 2020-09-17 Teva Pharmaceuticals International Gmbh Solid state forms of ripretinib
BR112021018591A2 (pt) * 2019-03-22 2021-11-23 Yumanity Therapeutics Inc Compostos e usos dos mesmos
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
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
US12428394B2 (en) 2019-06-28 2025-09-30 Chengdu Zenitar Biomedical Technology Co., Ltd. 2,4-disubstituted pyrimidine derivative, preparation method therefor and use thereof
US12377063B2 (en) * 2019-07-11 2025-08-05 Emory University Combination therapies for managing cancer
MX2022001863A (es) 2019-08-12 2022-05-30 Deciphera Pharmaceuticals Llc Metodos para tratar los tumores del estroma gastrointestinal.
WO2021030405A1 (en) 2019-08-12 2021-02-18 Deciphera Pharmaceuticals, Llc Ripretinib for treating gastrointestinal stromal tumors
TW202115024A (zh) 2019-08-14 2021-04-16 美商英塞特公司 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物
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
PE20221905A1 (es) 2019-10-11 2022-12-23 Incyte Corp Aminas biciclicas como inhibidoras de la cdk2
AU2020378279A1 (en) * 2019-11-05 2022-05-26 AbbVie Deutschland GmbH & Co. KG Dosing regimens for use in treating myelofibrosis and MPN-related disorders with navitoclax
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
PH12022551379A1 (en) 2019-12-06 2023-05-03 Vertex Pharma Substituted tetrahydrofurans as modulators of sodium channels
FI4084779T3 (fi) 2019-12-30 2024-12-16 Deciphera Pharmaceuticals Llc 1-(4-bromi-5-(1-etyyli-7-(metyyliamino)-2-okso-1,2-dihydro-1,6-naftyridin-3-yyli)-2-fluorifenyyli)-3-fenyyliurean koostumuksia
CN119970649A (zh) 2019-12-30 2025-05-13 德西费拉制药有限责任公司 非晶型激酶抑制剂制剂及其使用方法
WO2021154750A1 (en) * 2020-01-29 2021-08-05 Corcept Therapeutics Incorporated TREATMENT OF ADRENOCORTICAL CARCINOMA WITH SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS (SGRMs) AND ANTIBODY CHECKPOINT INHIBITORS
WO2021183474A1 (en) * 2020-03-09 2021-09-16 University Of Houston System Inflammatory bowel disease stem cells, agents which target ibd stem cells, and uses related thereto
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
BR112022022338A2 (pt) 2020-05-04 2023-01-10 Amgen Inc Compostos heterocíclicos como receptor desencadeador expresso em agonistas de células mieloides 2 e métodos de uso
WO2021226261A1 (en) 2020-05-06 2021-11-11 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
EP4157466A4 (en) * 2020-05-28 2024-07-31 Epizyme, Inc. USE OF EZH2 INHIBITORS TO TREAT CANCER
CN115697329B (zh) * 2020-06-11 2025-05-27 养生堂有限公司 Palovarotene在抗HBV病毒治疗中的用途
JP2023533464A (ja) 2020-06-25 2023-08-03 トルレモ・セラピューティクス・アクチェンゲゼルシャフト がんを治療するための、ＣＢＰ／ｐ３００ブロモドメイン阻害剤およびＫＲＡＳ阻害剤の組合せ
US20230255966A1 (en) * 2020-06-25 2023-08-17 Tolremo Therapeutics Ag A combination of a cbp/p300 bromodomain inhibitor and an egfr inhibitor for use in treating egfr-mutant nsclc
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
KR102695540B1 (ko) * 2020-09-21 2024-08-14 재단법인 아산사회복지재단 퀴나졸린-2,4-다이아민 유도체 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
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
EP4267574B1 (en) 2020-12-23 2025-04-23 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
TWI823255B (zh) * 2021-02-19 2023-11-21 大陸商微境生物醫藥科技(上海)有限公司 作為Wee-1抑制劑的稠環化合物
IL305165A (en) 2021-02-19 2023-10-01 Sudo Biosciences Ltd Tyk2 inhibitors and uses thereof
KR20230159419A (ko) 2021-02-19 2023-11-21 수도 바이오사이언시즈 리미티드 Tyk2 억제제 및 이의 용도
AU2021440597A1 (en) * 2021-04-16 2022-11-10 Provectus Pharmatech, Inc. Composition and method for oral treatment of leukemia
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
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
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)
KR20240148310A (ko) * 2021-10-15 2024-10-11 탱고 테라퓨틱스, 인크. Ehmt1 및 ehmt2의 신규 조절제 및 그의 치료 용도
FI4426434T3 (fi) 2021-11-02 2025-11-24 Flare Therapeutics Inc Pparg:n käänteisagonisteja ja niiden käyttöjä
WO2023086320A1 (en) 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. Forms and compositions of inhibitors of jak2
JP7782035B2 (ja) 2021-11-09 2025-12-08 エイジャックス セラピューティクス， インコーポレイテッド Ｊａｋ２阻害剤としての６－ヘテロアリールオキシベンゾイミダゾール及びアザベンゾイミダゾール
WO2023092394A1 (en) * 2021-11-25 2023-06-01 Guo Dagang Methods and compositions for treating ewing family of tumors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
AU2022426699A1 (en) 2021-12-30 2024-07-11 Biomea Fusion, Inc. Pyrazine compounds as inhibitors of flt3
IL314330A (en) 2022-01-18 2024-09-01 Maze Therapeutics Inc Apol1 inhibitors and methods of use
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
CN116675653B (zh) * 2022-07-22 2024-10-01 中国药科大学 氨基烷基取代的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
WO2024067566A1 (zh) * 2022-09-30 2024-04-04 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
TW202517642A (zh) * 2023-07-11 2025-05-01 美商梅斯治療股份有限公司 Ａｐｏｌ１抑制劑及其使用方法
WO2025043183A1 (en) * 2023-08-23 2025-02-27 Eigen Therapeutics Inc. Methods and compositions for treating hematological cancers
WO2025121805A1 (ko) * 2023-12-08 2025-06-12 인제대학교 산학협력단 Ezh2 저해제 및 jak3 억제제를 포함하는 암의 예방 또는 치료용 약학적 조성물

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017181177A1 (en) * 2016-04-15 2017-10-19 Epizyme, Inc. Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors

Family Cites Families (117)

* 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
US6025379A (en) 1996-03-11 2000-02-15 Eli Lilly And Company Methods of treating or preventing interstitial cystitis
ES2361146T3 (es) 1998-03-27 2011-06-14 Janssen Pharmaceutica Nv Derivados de la piramidina inhibitatoria de vih.
US6596747B2 (en) 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
EP1126843A4 (en) 1998-10-29 2005-06-15 Bristol Myers Squibb Co AMINO-CELL DERIVATIVE COMPOUNDS INHIBITORS OF ENZYME IMPDH
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
ATE548357T1 (de) 2000-01-25 2012-03-15 Neurocrine Biosciences Inc Gonadotropin freisetzende hormon rezeptor antagonisten und ihre verwandten verfahren
TW593278B (en) 2001-01-23 2004-06-21 Wyeth Corp 1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
BR0207390A (pt) 2001-02-21 2004-10-13 Nps Pharma Inc Compostos, composições farmacêuticas e métodos de tratatamento de doença associada a ativação e a ativação do grupo i mg1ur
WO2003040141A1 (en) 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
EP1453516A2 (de) 2001-10-17 2004-09-08 Boehringer Ingelheim Pharma GmbH & Co.KG 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate 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
CA2473510A1 (en) 2002-01-23 2003-07-31 Bayer Pharmaceuticals Corporation 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
JP2006514989A (ja) 2002-07-29 2006-05-18 ライジェル ファーマシューティカルズ ２，４−ピリミジンジアミン化合物による自己免疫疾患の治療および予防方法
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
SI1663242T1 (sl) 2003-08-07 2011-09-30 Rigel Pharmaceuticals Inc 2,4-pirimidindiaminske spojine in uporabe kot antiproliferativna sredstva
EP1663992A1 (en) 2003-09-18 2006-06-07 Novartis AG 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
BRPI0510032A (pt) 2004-05-20 2007-10-02 Sugen Inc tiofeno heteroaril aminas
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
CA2578349A1 (en) 2004-09-01 2006-03-16 Rigel Pharmaceuticals, Inc. Synthesis of 2,4-pyrimidinediamine compounds
WO2006128172A2 (en) 2005-05-26 2006-11-30 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
JP5203193B2 (ja) 2005-08-04 2013-06-05 サートリス ファーマシューティカルズ， インコーポレイテッド サーチュイン調節化合物としてのイミダゾ［２，１−ｂ］チアゾール誘導体
WO2007038387A2 (en) 2005-09-23 2007-04-05 Yale University Compounds and methods for the treatment of viruses and cancer
MX391408B (es) 2005-11-01 2025-03-21 Impact Biomedicines Inc Inhibidores de biaril meta-pirimidina de cinasas.
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
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
CN101679321B (zh) 2007-04-30 2012-10-03 普罗米蒂克生物科学公司 三嗪衍生物、含所述衍生物的组合物以及所述衍生物在制备用于治疗癌症和自身免疫性疾病药物中的应用
MX2009011810A (es) 2007-05-02 2010-01-14 Vertex Pharma Tiazoles y pirazoles utiles como inhibidores de cinasa.
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
NZ582485A (en) 2007-07-17 2012-05-25 Rigel Pharmaceuticals Inc Cyclic amine substituted pyrimidinediamines as pkc inhibitors
CA2713716A1 (en) 2008-02-22 2009-08-27 F. Hoffmann-La Roche Ag Modulators for amyloid beta
WO2009126537A1 (en) 2008-04-07 2009-10-15 Syndax Pharmaceuticals, Inc. Administration of an inhibitor of hdac and an hmt inhibitor
EP2323993B1 (en) 2008-04-16 2015-06-03 Portola Pharmaceuticals, Inc. 2,6-diamino- pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors
EP2306836B1 (en) 2008-07-01 2016-09-07 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
WO2010017122A2 (en) 2008-08-05 2010-02-11 Targegen Inc. Methods of treating thalassemia
EA201100438A1 (ru) 2008-09-03 2011-10-31 Байер Кропсайенс Аг 4-алкилзамещенные диаминопиримидины
CA2749248A1 (en) 2009-01-14 2010-07-22 Rigel Pharmaceuticals, Inc. Methods for treating inflammatory disorders using 2,4-pyrimidinediamine compounds
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
PE20110924A1 (es) 2009-01-23 2011-12-24 Rigel Pharmaceuticals Inc Derivados de 2, 4-diamino-pirimidina n2, n4-disustituidos como inhibidores de jak3
US20100317706A1 (en) 2009-04-30 2010-12-16 Bumham Institute For Medical Research HNF4alpha MODULATORS AND METHODS OF USE
AR076550A1 (es) 2009-05-06 2011-06-22 Portola Pharm Inc Inhibidores de la janus tirosina kinasa (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
US20120189670A1 (en) 2009-09-14 2012-07-26 Kirkpatrick D Lynn 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
EP2552211A4 (en) 2010-03-26 2013-10-23 Glaxo Group Ltd INDAZOLYL-PYRIMIDINE AS KINASEHEMMER
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
JP6389036B2 (ja) 2010-09-10 2018-09-12 エピザイム インコーポレイテッド ヒトｅｚｈ２の阻害剤、およびその使用方法
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
WO2012064806A2 (en) 2010-11-11 2012-05-18 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
TWI598336B (zh) * 2011-04-13 2017-09-11 雅酶股份有限公司 經取代之苯化合物
JO3438B1 (ar) * 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
PL2755483T3 (pl) 2011-09-14 2019-06-28 Samumed, Llc Indazolo-3-karboksyamidy i ich zastosowanie jako inhibitorów szlaków sygnalizacji WNT/B-kateniny
US9458131B2 (en) 2011-11-08 2016-10-04 Emory University Compounds and compositions used to epigenetically transform cells and methods related thereto
US20140323418A1 (en) 2011-11-23 2014-10-30 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
EP2828250B1 (en) 2012-03-19 2021-03-10 Imperial College Innovations Limited 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
WO2014089112A1 (en) 2012-12-04 2014-06-12 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
KR20150119012A (ko) 2013-02-08 2015-10-23 셀진 아빌로믹스 리서치, 인코포레이티드 Erk 억제제 및 이의 용도
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
WO2014151900A1 (en) 2013-03-14 2014-09-25 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
WO2015048547A2 (en) 2013-09-26 2015-04-02 Rigel Pharmaceuticals, Inc. Methods for using and biomarkers for ampk-activating compounds
WO2015095679A1 (en) 2013-12-20 2015-06-25 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
JP6527534B2 (ja) 2014-06-16 2019-06-05 ファンダシオン パラ ラ インベスティガシオン メディカ アプリカダＦｕｎｄａｃｉｏｎ Ｐａｒａ Ｌａ Ｉｎｖｅｓｔｉｇａｓｉｏｎ Ｍｅｄｉｃａ Ａｐｌｉｃａｄａ ヒストンメチルトランスフェラーゼ及びｄｎａメチルトランスフェラーゼの二重阻害剤としての新規化合物
CA2952474A1 (en) 2014-06-23 2015-12-30 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
KR20170081213A (ko) 2014-11-06 2017-07-11 다나-파버 캔서 인스티튜트 인크. Ezh2 억제제 및 그의 용도
SG11201802952TA (en) * 2015-10-09 2018-05-30 Agency Science Tech & Res Compounds for treatment of cancer and epigenetics
US10407423B2 (en) 2015-11-16 2019-09-10 Fundación Para La Investigación Médica Aplicada Compounds as inhibitors of DNA methyltransferases
US10370372B2 (en) 2015-11-27 2019-08-06 Taiho Pharmaceutical Co., Ltd. Fused pyrimidine compound or salt thereof
AU2016372280A1 (en) 2015-12-14 2018-07-12 Fundación Para La Investigación Médica Aplicada 2,4,6,7-tetrasubstituted quinoline compounds as inhibitors of DNA methyltransferases
ES2883450T3 (es) 2016-02-17 2021-12-07 Global Blood Therapeutics Inc Inhibidores de histona metiltransferasa
AU2017251155B2 (en) 2016-04-15 2021-08-05 Elanco Animal Health Gmbh Pyrazolopyrimidine derivatives
BR112018071216A2 (pt) 2016-04-15 2019-02-05 Abbvie Inc inibidores de bromodomínios
JP6855504B2 (ja) 2016-04-15 2021-04-07 シンジェンタ パーティシペーションズ アーゲー 除草性ピリダジノン化合物
SG11201808907PA (en) 2016-04-15 2018-11-29 Blueprint Medicines Corp Inhibitors of activin receptor-like kinase
KR102478186B1 (ko) 2016-06-03 2022-12-15 더 트러스티스 오브 컬럼비아 유니버시티 인 더 시티 오브 뉴욕 프라더-윌리 증후군을 치료하는 방법
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
KR102003532B1 (ko) 2016-06-10 2019-07-24 르 라보레또레 쎄르비에르 새로운 (헤테로)아릴-치환된-피페리디닐 유도체, 이의 제조를 위한 방법 및 이를 함유하는 약학적 조성물
BR112018075465A2 (pt) 2016-06-10 2019-03-19 Enanta Pharmaceuticals, Inc. agentes antivirais de hepatite b
WO2018064557A1 (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
PL3555070T3 (pl) 2016-12-19 2023-11-06 Epizyme, Inc. Związki heteroarylowe podstawione aminą jako inhibitory ehmt2 i sposoby ich zastosowania
EP3558971B1 (en) 2016-12-22 2022-02-23 Global Blood Therapeutics, Inc. Histone methyltransferase inhibitors
US20180177784A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018183923A1 (en) 2017-03-31 2018-10-04 Epizyme, Inc. Methods of using ehmt2 inhibitors
SG11202001090WA (en) 2017-08-15 2020-03-30 Global Blood Therapeutics Inc Tricyclic compounds as histone methyl-transferase inhibitors
WO2019079485A1 (en) 2017-10-17 2019-04-25 Epizyme, Inc. AMINO-SUBSTITUTED HETEROCYCLIC COMPOUNDS AS EHMT2 INHIBITORS AND DERIVATIVES THEREOF
JP2021500327A (ja) 2017-10-18 2021-01-07 エピザイム，インコーポレイティド 免疫療法にｅｈｍｔ２阻害剤を使用する方法
CA3081946A1 (en) 2017-10-18 2019-04-25 Epizyme, Inc. Methods of using ehmt2 inhibitors in preventing or treating blood disorders
BR112020007632A2 (pt) 2017-10-18 2020-09-29 Epizyme, Inc. composto, composição farmacêutica, método para inibir um dentre ou tanto ehmt1 quanto ehmt2, método para prevenir ou tratar um distúrbio sanguíneo, método para prevenir ou tratar um câncer e uso do composto

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017181177A1 (en) * 2016-04-15 2017-10-19 Epizyme, Inc. Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
CANCER RESEARCH, vol. 77, JPN6022019770, January 2017 (2017-01-01), pages 470 - 481, ISSN: 0004776923 *
CELL DEATH AND DISEASE, vol. ４, JPN6022019769, 2013, pages 690, ISSN: 0004776922 *
CLINICAL EPIGENETICS, vol. 84, JPN6022019775, 2015, pages 7, ISSN: 0004776927 *
CURRENT TOPICS IN MEDICAL CHEMISTRY, vol. 15, JPN6022019774, 2015, pages 720 - 744, ISSN: 0004776926 *
INTERNATIONAL JOURNAL OF CANCER, vol. 134, JPN6022019772, 2013, pages 1257 - 1269, ISSN: 0004776925 *
ONCOTARGET, vol. 7, JPN6022019771, 2016, pages 39706 - 39808, ISSN: 0004776924 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023532946A (ja) * 2020-07-10 2023-08-01 ブロッサムヒル・セラピューティクス・インコーポレイテッド 大員環分子およびそれらの使用
JP7713619B2 (ja) 2020-07-10 2025-07-28 ブロッサムヒル・セラピューティクス・インコーポレイテッド 大員環分子およびそれらの使用

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