AU2016341520C1 - Benzolactam compounds as protein kinase inhibitors - Google Patents

Benzolactam compounds as protein kinase inhibitors Download PDF

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Publication number
AU2016341520C1
AU2016341520C1 AU2016341520A AU2016341520A AU2016341520C1 AU 2016341520 C1 AU2016341520 C1 AU 2016341520C1 AU 2016341520 A AU2016341520 A AU 2016341520A AU 2016341520 A AU2016341520 A AU 2016341520A AU 2016341520 C1 AU2016341520 C1 AU 2016341520C1
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Prior art keywords
pyrimidin
chloro
dihydro
amino
isoindol
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AU2016341520A
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AU2016341520B2 (en
AU2016341520A1 (en
Inventor
Valerio Berdini
Ildiko Maria Buck
Michael Liam COOKE
David Cousin
James Edward Harvey DAY
Charlotte Mary Griffiths-Jones
Thomas Daniel Heightman
Steven Howard
Christopher William Murray
David Norton
Marc O'reilly
Stuart Thomas Onions
Jonathan Martin SHANNON
John Paul Watts
Alison Jo-Anne Woolford
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Otsuka Pharmaceutical Co Ltd
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Otsuka Pharmaceutical Co Ltd
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Priority claimed from GBGB1518676.0A external-priority patent/GB201518676D0/en
Priority claimed from GBGB1611351.6A external-priority patent/GB201611351D0/en
Application filed by Otsuka Pharmaceutical Co Ltd filed Critical Otsuka Pharmaceutical Co Ltd
Publication of AU2016341520A1 publication Critical patent/AU2016341520A1/en
Publication of AU2016341520B2 publication Critical patent/AU2016341520B2/en
Priority to AU2021200951A priority Critical patent/AU2021200951B2/en
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    • 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
    • A61K31/495Heterocyclic 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
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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
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/4035Isoindoles, e.g. phthalimide
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    • A61K31/33Heterocyclic compounds
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    • 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
    • A61K31/444Non 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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    • 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
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    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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AU2016341520A 2015-10-21 2016-10-20 Benzolactam compounds as protein kinase inhibitors Active AU2016341520C1 (en)

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AU2021200951A AU2021200951B2 (en) 2015-10-21 2021-02-12 Benzolactam compounds as protein kinase inhibitors

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Application Number Priority Date Filing Date Title
GBGB1518676.0A GB201518676D0 (en) 2015-10-21 2015-10-21 Benzolactam compounds
GB1518676.0 2015-10-21
GBGB1611351.6A GB201611351D0 (en) 2016-06-30 2016-06-30 Benzolactam compounds
GB1611351.6 2016-06-30
PCT/IB2016/001507 WO2017068412A1 (en) 2015-10-21 2016-10-20 Benzolactam compounds as protein kinase inhibitors

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AU2016341520B2 AU2016341520B2 (en) 2020-11-12
AU2016341520C1 true AU2016341520C1 (en) 2021-07-22

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Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0811643D0 (en) 2008-06-25 2008-07-30 Cancer Rec Tech Ltd New therapeutic agents
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
EP3280708B1 (en) 2015-04-10 2021-09-01 Araxes Pharma LLC Substituted quinazoline compounds and methods of use thereof
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
GB201517216D0 (en) 2015-09-29 2015-11-11 Cancer Res Technology Ltd And Astex Therapeutics Ltd Pharmaceutical compounds
GB201517217D0 (en) 2015-09-29 2015-11-11 Astex Therapeutics Ltd And Cancer Res Technology Ltd Pharmaceutical compounds
WO2017068412A1 (en) * 2015-10-21 2017-04-27 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
EA038635B9 (ru) 2015-11-16 2021-10-26 Араксис Фарма Ллк 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
WO2018019204A1 (zh) * 2016-07-26 2018-02-01 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
KR102539877B1 (ko) 2016-09-12 2023-06-05 인테그랄 헬스 인코퍼레이티드 Gpr120 조정제로서 유용한 이환형 화합물
KR102537985B1 (ko) 2016-09-12 2023-05-30 인테그랄 헬스 인코퍼레이티드 Gpr120 조정제로서 유용한 단환형 화합물
WO2018064510A1 (en) 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2018068017A1 (en) * 2016-10-07 2018-04-12 Araxes Pharma Llc Heterocyclic compounds as inhibitors of ras and methods of use thereof
CN106588884B (zh) * 2016-11-10 2019-04-09 浙江大学 2-多取代芳环-嘧啶类衍生物及制备和医药用途
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US11059819B2 (en) 2017-01-26 2021-07-13 Janssen Biotech, Inc. Fused hetero-hetero bicyclic compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
GB201704965D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
GB201704966D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
GB201706327D0 (en) * 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
EP3630745A2 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Covalent inhibitors of kras
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
HUE067314T2 (hu) 2017-09-22 2024-10-28 Jubilant Epipad LLC Heterociklusos vegyületek mint PAD gátlók
KR102782563B1 (ko) 2017-10-18 2025-03-14 주빌런트 에피파드 엘엘씨 Pad 억제제로서의 이미다조-피리딘 화합물
KR20200085836A (ko) 2017-11-06 2020-07-15 주빌런트 프로델 엘엘씨 Pd1/pd-l1 활성화 억제제로서의 피리미딘 유도체
BR112020010322A2 (pt) 2017-11-24 2020-11-17 Jubilant Episcribe Llc composto da fórmula i; composto da fórmula ia; composto da fórmula ib; processo de preparação de compostos da fórmula i; composição farmacêutica; método para o tratamento e/ou prevenção de várias doenças; uso dos compostos; método para o tratamento de câncer; e método para o tratamento e/ou prevenção de uma afecção mediada por prmt5 ou um distúrbio proliferativo ou câncer
EP3738961B1 (en) * 2018-01-03 2022-08-31 Medshine Discovery Inc. Heterocyclic compound as csf-1r inhibitor and use thereof
SG11202008950PA (en) 2018-03-13 2020-10-29 Jubilant Prodel LLC Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation
WO2019195384A1 (en) * 2018-04-05 2019-10-10 Tarveda Therapeutics, Inc. Hsp90-targeting conjugates and formulations thereof
AU2019272303B2 (en) * 2018-05-22 2024-11-07 Js Innomed Holdings Ltd. Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
TWI707683B (zh) 2018-06-13 2020-10-21 美商輝瑞股份有限公司 Glp-1受體促效劑及其用途
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
CN109377846B (zh) * 2018-10-11 2020-12-08 内蒙古科技大学包头医学院 人体解剖学内脏标本的制作方法
CN109608444B (zh) * 2018-11-27 2022-02-11 中国药科大学 含异吲哚啉酮的erk抑制剂及其制备方法与用途
IL283901B2 (en) * 2018-12-18 2025-03-01 Astrazeneca Ab Process and intermediates for the preparation of 4-{4-[(3R)-3-methylmorpholin-4-yl]-6-[1-((R)-S-methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl}-1H-pyrrolo[2,3-b]pyridine
CN111057048B (zh) * 2019-01-30 2022-03-18 上海凌达生物医药有限公司 一类氨基吡嗪/吡啶类化合物、制备方法和用途
JP7426398B2 (ja) * 2019-02-26 2024-02-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ras阻害剤としての新規イソインドリノン置換インドールおよび誘導体
CA3135174A1 (en) * 2019-04-03 2020-10-08 Tarveda Therapeutics, Inc. Hsp90-binding conjugates and formulations thereof
EP3978498A1 (en) * 2019-05-24 2022-04-06 Jiangsu Hengrui Medicine Co., Ltd. Substituted fused bicyclic derivative, preparation method therefor, and application thereof in medicines
CN113544130B (zh) * 2019-05-31 2024-01-09 西藏海思科制药有限公司 一种btk抑制剂环衍生物及其制备方法和药学上的应用
CN114206852A (zh) 2019-08-09 2022-03-18 卡尔维斯塔制药有限公司 血浆激肽释放酶抑制剂
WO2021055728A1 (en) 2019-09-18 2021-03-25 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
CN112574207B (zh) * 2019-09-30 2023-04-11 南京药石科技股份有限公司 Erk1/2蛋白激酶抑制剂及其用途
IL291783A (en) * 2019-10-02 2022-06-01 Domain Therapeutics ep4 prostaglandin e2 receptor antagonists
CA3158793A1 (en) 2019-10-28 2021-05-06 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
JP2023515235A (ja) 2019-10-31 2023-04-12 大鵬薬品工業株式会社 4-アミノブタ-2-エンアミド誘導体及びその塩
WO2021106231A1 (en) 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
WO2021110169A1 (zh) * 2019-12-06 2021-06-10 南京明德新药研发有限公司 作为erk抑制剂的噻唑并内酰胺类化合物及其应用
WO2021215545A1 (en) 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Anticancer combination therapy with n-(1-acryloyl-azetidin-3-yl)-2-((1h-indazol-3-yl)amino)methyl)-1h-imidazole-5-carboxamide inhibitor of kras-g12c
EP4139299B1 (en) 2020-04-24 2025-12-17 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
AU2021262977B2 (en) * 2020-04-30 2023-07-13 Suzhou Genhouse Bio Co., Ltd. Compounds containing benzosultam
WO2021224818A1 (en) * 2020-05-08 2021-11-11 Pfizer Inc. Isoindolone compounds as hpk1 inhibitors
JP2023538137A (ja) 2020-08-21 2023-09-06 シャンハイ リンジーン バイオファーマ カンパニー リミテッド 芳香環ラクタム系化合物、その製造方法及び使用
CN114516856B (zh) * 2020-11-20 2025-05-23 安徽中科拓苒药物科学研究有限公司 二氢异喹啉酮和异吲哚啉酮衍生物及其用途
EP4347041A1 (en) 2021-05-28 2024-04-10 Taiho Pharmaceutical Co., Ltd. Small molecule inhibitors of kras mutated proteins
TWI809904B (zh) * 2021-06-02 2023-07-21 大陸商南京明德新藥研發有限公司 一種二甲基取代的噻唑並吡咯酮類化合物的晶型及其製備方法
CA3222540A1 (en) 2021-06-11 2022-12-15 Otsuka Pharmaceutical Co., Ltd. Process for preparing an erk inhibitor
WO2023039548A1 (en) * 2021-09-10 2023-03-16 Fred Hutchinson Cancer Center Kinase inhibitors for the treatment of prostate cancer
US20240415835A1 (en) 2021-10-26 2024-12-19 Otsuka Pharmaceutical Co., Ltd. Compositions comprising an erk inhibitor
IL319546A (en) 2022-09-13 2025-05-01 Amphista Therapeutics Ltd Materials for targeted protein degradation
EP4596554A4 (en) * 2022-09-29 2025-12-10 Suzhou Arkbiopharmaceutical Co Ltd Fused AZA Cyclic Compound, its Preparation Process and its Use in Medicine
CN119790049A (zh) * 2022-09-30 2025-04-08 楚浦创制(武汉)医药科技有限公司 2-氨基嘧啶类化合物及其应用、药用组合物
WO2024220866A1 (en) * 2023-04-19 2024-10-24 Accutar Biotechnology Inc. Novel aminopyrimidine derivatives as cyclin-dependent kinase inhibitors
WO2025085748A1 (en) 2023-10-20 2025-04-24 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011075784A1 (en) * 2009-12-23 2011-06-30 Peter Maccallum Cancer Institute Compounds, preparations and uses thereof
WO2013000994A1 (en) * 2011-06-30 2013-01-03 Abbott Gmbh & Co. Kg Novel inhibitor compounds of phosphodiesterase type 10a
WO2015108861A1 (en) * 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
US5463063A (en) 1993-07-02 1995-10-31 Celgene Corporation Ring closure of N-phthaloylglutamines
US5958934A (en) 1996-05-23 1999-09-28 Syntex (U.S.A.) Inc. Aryl pyrimidine derivatives and uses thereof
JP2003504301A (ja) 1998-04-01 2003-02-04 ブリストル−マイヤーズ スクイブ ファーマ カンパニー インテグリンアンタゴニスト
HUP0402352A2 (hu) 2001-06-19 2005-02-28 Bristol-Myers Squibb Co. Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények
EP1618094B1 (en) 2003-04-30 2007-09-05 The Institutes for Pharmaceutical Discovery, LLC Substituted heteroaryls as inhibitors of protein tyrosine phosphatases
US7504401B2 (en) 2003-08-29 2009-03-17 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
AU2004268621C1 (en) 2003-08-29 2011-08-18 Exelixis, Inc. c-Kit modulators and methods of use
US7354939B2 (en) 2004-05-14 2008-04-08 Vertex Pharmaceuticals Incorporated Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto
US20060235036A1 (en) 2005-04-15 2006-10-19 Doherty Elizabeth M Vanilloid receptor ligands and their use in treatments
ATE527240T1 (de) 2005-12-13 2011-10-15 Schering Corp Polyzyklische indazol-derivate als erk-hemmer
US20080280891A1 (en) 2006-06-27 2008-11-13 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
JP2009542604A (ja) 2006-07-06 2009-12-03 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 4−ヘテロシクロアルキルピリミジン、それらの調製方法及び医薬としての使用
WO2008008059A1 (en) 2006-07-12 2008-01-17 Locus Pharmaceuticals, Inc. Anti-cancer agents ans uses thereof
WO2008124085A2 (en) 2007-04-03 2008-10-16 Exelixis, Inc. Methods of using combinations of mek and jak-2 inhibitors
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
WO2009039635A1 (en) 2007-09-24 2009-04-02 Painceptor Pharma Corporation Methods of modulating neurotrophin-mediated activity
WO2009042907A1 (en) * 2007-09-27 2009-04-02 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Isoindoline compounds for the treatment of spinal muscular atrophy and other uses
PL2231640T3 (pl) 2008-01-24 2012-09-28 Merck Patent Gmbh Pochodne beta-aminokwasowe do leczenia cukrzycy
NZ589843A (en) 2008-06-27 2012-12-21 Avila Therapeutics Inc Pyrimidine heteroaryl compounds and uses thereof as protein kinase inhibitors
US8338439B2 (en) * 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
GB0815369D0 (en) 2008-08-22 2008-10-01 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶,其組合物及使用其之治療方法
GB0821307D0 (en) 2008-11-21 2008-12-31 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
JP5487214B2 (ja) 2008-12-19 2014-05-07 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ阻害剤として有用なカルバゾールカルボキシアミド化合物
JP5713999B2 (ja) 2009-05-15 2015-05-07 コリア リサーチ インスティテュート オブ ケミカル テクノロジー アミド化合物、その製造方法及びそれを含む薬学組成物
WO2010151747A1 (en) 2009-06-26 2010-12-29 Cystic Fibrosis Foundation Therapeutics, Inc. Pyrimine compounds and methods of making and using same
WO2011008931A2 (en) 2009-07-15 2011-01-20 Cystic Fibrosis Foundation Therapeutics, Inc. Arylpyrimidine compounds and combination therapy comprising same for treating cystic fibrosis & related disorders
KR101758046B1 (ko) 2009-12-22 2017-07-14 버텍스 파마슈티칼스 인코포레이티드 포스파티딜이노시톨 3-키나제의 이소인돌리논 억제제
KR20120125618A (ko) 2009-12-31 2012-11-16 피라말 헬쓰케어 리미티드 디아실글리세롤 아실 전이효소의 억제제
CN102985405B (zh) 2010-07-02 2016-07-06 Aska制药株式会社 杂环化合物及p27Kip1分解抑制剂
KR101764952B1 (ko) 2010-07-29 2017-08-03 리겔 파마슈티칼스, 인크. Ampk-활성화 헤테로시클릭 화합물 및 그의 사용 방법
PT2820009T (pt) 2012-03-01 2018-04-12 Array Biopharma Inc Inibidores de serina/treonina quinases
IN2014KN02601A (enExample) * 2012-04-24 2015-05-08 Vertex Pharma
WO2014040555A1 (zh) 2012-09-12 2014-03-20 山东亨利医药科技有限责任公司 作为酪氨酸激酶抑制剂的含氮杂芳环衍生物
US20150272939A1 (en) 2012-10-02 2015-10-01 Yale University Identification of Small Molecule Inhibitors of Jumonji AT-Rich Interactive Domain 1A (JARID1A) and 1B (JARID1B) Histone Demethylase
CA2890105C (en) 2012-11-01 2023-03-21 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
AU2014214846A1 (en) 2013-02-08 2015-07-23 Celgene Avilomics Research, Inc. ERK inhibitors and uses thereof
WO2014130856A2 (en) 2013-02-21 2014-08-28 Wayne Rothbaum Treatment of skeletal-related disorders
JP6524094B2 (ja) 2013-08-30 2019-06-05 ピーティーシー セラピューティクス, インコーポレイテッド 置換ピリミジンBmi−1阻害剤
WO2015048547A2 (en) 2013-09-26 2015-04-02 Rigel Pharmaceuticals, Inc. Methods for using and biomarkers for ampk-activating compounds
WO2015154038A1 (en) 2014-04-04 2015-10-08 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2015157556A1 (en) 2014-04-09 2015-10-15 Kadmon Corporation, Llc Treatment of gvhd
WO2016025649A1 (en) 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Combinations of an erk inhibitor and a dot1l inhibitor and related methods
TWI704151B (zh) 2014-12-22 2020-09-11 美商美國禮來大藥廠 Erk抑制劑
WO2016162325A1 (en) 2015-04-07 2016-10-13 Astrazeneca Ab Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1 (2h)-one derivatives as kinase inhibitors
DK3307727T3 (da) 2015-06-15 2024-01-08 Asana Biosciences Llc Heterocykliske inhibitorer af erk1 og erk2 og deres anvendelse i behandlingen af kræft
WO2017068412A1 (en) 2015-10-21 2017-04-27 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
SG11201803066VA (en) 2015-11-09 2018-05-30 Astrazeneca Ab Dihydroimidazopyrazinone derivatives useful in the treatment of cancer
WO2018019204A1 (zh) 2016-07-26 2018-02-01 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011075784A1 (en) * 2009-12-23 2011-06-30 Peter Maccallum Cancer Institute Compounds, preparations and uses thereof
WO2013000994A1 (en) * 2011-06-30 2013-01-03 Abbott Gmbh & Co. Kg Novel inhibitor compounds of phosphodiesterase type 10a
WO2015108861A1 (en) * 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof

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