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MX2018004643A - Compuestos de benzolactama como inhibidores de la proteina cinasa. - Google Patents

Compuestos de benzolactama como inhibidores de la proteina cinasa.

Info

Publication number
MX2018004643A
MX2018004643A MX2018004643A MX2018004643A MX2018004643A MX 2018004643 A MX2018004643 A MX 2018004643A MX 2018004643 A MX2018004643 A MX 2018004643A MX 2018004643 A MX2018004643 A MX 2018004643A MX 2018004643 A MX2018004643 A MX 2018004643A
Authority
MX
Mexico
Prior art keywords
protein kinase
kinase inhibitors
compounds
benzolactam compounds
benzolactam
Prior art date
Application number
MX2018004643A
Other languages
English (en)
Other versions
MX382927B (es
Inventor
Berdini Valerio
Howard Steven
Maria Buck Ildiko
O''reilly Marc
Jo-Anne Woolford Alison
Daniel Heightman Thomas
Norton David
Martin SHANNON Jonathan
Cousin David
Liam Cooke Michael
Edward Harvey Day James
Thomas Onions Stuart
William Murray Christopher
Mary Griffiths-Jones Charlotte
Paul Watts John
Original Assignee
Otsuka Pharma Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB1518676.0A external-priority patent/GB201518676D0/en
Priority claimed from GBGB1611351.6A external-priority patent/GB201611351D0/en
Application filed by Otsuka Pharma Co Ltd filed Critical Otsuka Pharma Co Ltd
Publication of MX2018004643A publication Critical patent/MX2018004643A/es
Publication of MX382927B publication Critical patent/MX382927B/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • A61K31/40Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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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    • A61K31/395Heterocyclic 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
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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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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic 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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    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • 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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

La invención proporciona un compuesto de la fórmula (0):(ver formula) o una sal, N-óxido o tautómero farmacéuticamente aceptable de este. Los compuestos son inhibidores de las ERK1/2 cinasas y serán útiles en el tratamiento de las afecciones mediadas por ERK1/2. Los compuestos son, por lo tanto, útiles en la terapia, en particular en el tratamiento de cáncer.
MX2018004643A 2015-10-21 2016-10-20 Compuestos de benzolactama como inhibidores de la proteína cinasa. MX382927B (es)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
MX2018004643A true MX2018004643A (es) 2018-08-01
MX382927B MX382927B (es) 2025-03-13

Family

ID=57218943

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018004643A MX382927B (es) 2015-10-21 2016-10-20 Compuestos de benzolactama como inhibidores de la proteína cinasa.

Country Status (25)

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US (4) US10457669B2 (es)
EP (1) EP3365334B1 (es)
JP (2) JP6931646B2 (es)
KR (1) KR102769567B1 (es)
CN (2) CN114948963B (es)
AU (2) AU2016341520C1 (es)
CA (1) CA3001799A1 (es)
DK (1) DK3365334T3 (es)
ES (1) ES2989326T3 (es)
FI (1) FI3365334T3 (es)
HR (1) HRP20241210T1 (es)
HU (1) HUE068392T2 (es)
IL (2) IL291017B2 (es)
LT (1) LT3365334T (es)
MA (1) MA47013A (es)
MX (1) MX382927B (es)
MY (1) MY204050A (es)
PH (1) PH12018500792A1 (es)
PL (1) PL3365334T3 (es)
PT (1) PT3365334T (es)
SA (1) SA518391342B1 (es)
SG (1) SG10201912959QA (es)
SI (1) SI3365334T1 (es)
TW (1) TWI747846B (es)
WO (1) WO2017068412A1 (es)

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
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
MX382355B (es) 2015-04-10 2025-03-13 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos.
MX2017013275A (es) 2015-04-15 2018-01-26 Araxes Pharma Llc Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos.
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
GB201517217D0 (en) 2015-09-29 2015-11-11 Astex Therapeutics Ltd And Cancer Res Technology Ltd Pharmaceutical compounds
GB201517216D0 (en) 2015-09-29 2015-11-11 Cancer Res Technology Ltd And Astex Therapeutics Ltd Pharmaceutical compounds
HUE068392T2 (hu) 2015-10-21 2024-12-28 Otsuka Pharma Co Ltd Benzolaktám vegyületek mint fehérje kináz gátlók
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
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
JP6740452B2 (ja) * 2016-07-26 2020-08-12 深▲セン▼市塔吉瑞生物医▲薬▼有限公司Shenzhen TargetRx,Inc. プロテインチロシンキナーゼの活性を阻害するためのアミノピリミジン系化合物
KR102537985B1 (ko) 2016-09-12 2023-05-30 인테그랄 헬스 인코퍼레이티드 Gpr120 조정제로서 유용한 단환형 화합물
EP3509588B1 (en) 2016-09-12 2023-06-07 Integral Health,Inc. Bicyclic compounds useful as gpr120 modulators
JP2019529484A (ja) 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Kras g12c変異体タンパク質の阻害剤
US10377743B2 (en) * 2016-10-07 2019-08-13 Araxes Pharma Llc 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
WO2018140600A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 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
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
GB201704966D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
GB201704965D0 (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
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
KR20200010306A (ko) 2017-05-25 2020-01-30 아락세스 파마 엘엘씨 Kras의 공유적 억제제
PT3684767T (pt) 2017-09-22 2024-07-29 Jubilant Epipad LLC Compostos heterocíclicos como inibidores de pad
CA3076476A1 (en) 2017-10-18 2019-04-25 Jubilant Epipad LLC Imidazo-pyridine compounds as pad inhibitors
US11629135B2 (en) 2017-11-06 2023-04-18 Jubilant Prodell Llc Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation
AU2018372211B2 (en) 2017-11-24 2023-02-02 Jubilant Episcribe LLC, Heterocyclic compounds as PRMT5 inhibitors
US11384065B2 (en) 2018-01-03 2022-07-12 Medshine Discovery Inc. Heterocyclic compound as CSF-1R inhibitor and use thereof
JP7279063B6 (ja) 2018-03-13 2024-02-15 ジュビラント プローデル エルエルシー Pd1/pd-l1相互作用/活性化の阻害剤としての二環式化合物
TW202005667A (zh) * 2018-04-05 2020-02-01 美商塔維達治療公司 Hsp90-靶向共軛體及其調合物
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
CA3045644C (en) 2018-06-13 2024-01-16 Pfizer Inc. Glp-1 receptor agonists and uses thereof
US12134620B2 (en) 2018-08-01 2024-11-05 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
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
US12365678B2 (en) * 2018-12-18 2025-07-22 Astrazeneca Ab Pharmaceutical process 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 and intermediates
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
US12281099B2 (en) * 2019-02-26 2025-04-22 Boehringer Ingelheim International Gmbh Isoindolinone substituted indoles and derivatives as RAS inhibitors
EP3946320A4 (en) * 2019-04-03 2022-12-28 Tva (Abc), Llc CONJUGATES RELATED TO HSP90 AND FORMULATIONS THEREOF
WO2020238776A1 (zh) * 2019-05-24 2020-12-03 江苏恒瑞医药股份有限公司 取代的稠合双环类衍生物、其制备方法及其在医药上的应用
CN118027041A (zh) * 2019-05-31 2024-05-14 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
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
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
KR20220077140A (ko) 2019-10-02 2022-06-08 도메인 테라퓨틱스 프로스타글란딘 e2(pge2) ep4 수용체 길항제
CA3158793A1 (en) 2019-10-28 2021-05-06 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
CN115551500A (zh) 2019-10-31 2022-12-30 大鹏药品工业株式会社 4-氨基丁-2-烯酰胺衍生物及其盐
WO2021106231A1 (en) 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
CN114829365B (zh) * 2019-12-06 2023-04-25 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
EP4139299B1 (en) 2020-04-24 2025-12-17 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
US20230181536A1 (en) 2020-04-24 2023-06-15 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
CA3177298C (en) * 2020-04-30 2023-11-21 Xile LIU Compounds containing benzosultam as erk inhibitors
WO2021224818A1 (en) * 2020-05-08 2021-11-11 Pfizer Inc. Isoindolone compounds as hpk1 inhibitors
CA3190001A1 (en) * 2020-08-21 2022-02-24 Shanghai Ringene Biopharma Co., Ltd. Aromatic ring-lactam compound, preparation method therefor and use thereof
JP7728027B2 (ja) * 2020-11-20 2025-08-22 安徽中科拓苒▲薬▼物科学研究有限公司 ジヒドロイソキノリノン及びイソインドリノン誘導体並びにそれらの使用
EP4347041A1 (en) 2021-05-28 2024-04-10 Taiho Pharmaceutical Co., Ltd. Small molecule inhibitors of kras mutated proteins
WO2022253186A1 (zh) * 2021-06-02 2022-12-08 南京明德新药研发有限公司 一种二甲基取代的噻唑并吡咯酮类化合物的晶型及其制备方法
EP4352052A1 (en) 2021-06-11 2024-04-17 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
WO2024067660A1 (zh) * 2022-09-29 2024-04-04 苏州爱科百发生物医药技术有限公司 氮杂稠环类化合物、其制备方法及其在医药上的应用
WO2024066986A1 (zh) * 2022-09-30 2024-04-04 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
US12466840B2 (en) 2023-10-20 2025-11-11 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS proteins

Family Cites Families (57)

* 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
EP1054871A2 (en) 1998-04-01 2000-11-29 Du Pont Pharmaceuticals Company Pyrimidines and triazines as integrin antagonists
JP2005500294A (ja) 2001-06-19 2005-01-06 ブリストル−マイヤーズ スクイブ カンパニー ホスホジエステラーゼ7に対するピリミジン阻害剤
ES2290743T3 (es) 2003-04-30 2008-02-16 The Institutes For Pharmaceutical Discovery, Llc Heteroarilos sustituidos como inhibidores de las proteina-tirosina fosfatasas.
US7504401B2 (en) 2003-08-29 2009-03-17 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
JP5010917B2 (ja) 2003-08-29 2012-08-29 エグゼリクシス, インコーポレイテッド c−Kit調節因子および使用方法
ES2651439T3 (es) 2004-05-14 2018-01-26 Vertex Pharmaceuticals Incorporated Compuestos de pirrol como inhibidores de proteínas cinasas ERK y composiciones farmacéuticas que contienen esos compuestos
US20060235036A1 (en) 2005-04-15 2006-10-19 Doherty Elizabeth M Vanilloid receptor ligands and their use in treatments
EP1966151B1 (en) 2005-12-13 2011-10-05 Schering Corporation Polycyclic indazole derivatives that are erk inhibitors
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
AU2008304231A1 (en) * 2007-09-27 2009-04-02 Albany Molecular Research, Inc. Isoindoline compounds for the treatment of spinal muscular atrophy and other uses
WO2009092432A1 (en) 2008-01-24 2009-07-30 Merck Patent Gmbh Beta-amino acid derivatives for treatment of diabetes
BRPI0914682B8 (pt) * 2008-06-27 2021-05-25 Avila Therapeutics Inc compostos de heteroarila e composições compreendendo os referidos compostos
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
SG171815A1 (en) 2008-12-19 2011-07-28 Bristol Myers Squibb Co Carbazole carboxamide compounds useful as kinase inhibitors
EP2429987A4 (en) 2009-05-15 2012-10-03 Korea Res Inst Chem Tech AMIDE COMPOUND, PROCESS FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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
US20120040950A1 (en) 2009-12-22 2012-02-16 Vertex Pharmaceuticals Incorporated Isoindolinone inhibitors of phosphatidylinositol 3-kinase
WO2011075784A1 (en) * 2009-12-23 2011-06-30 Peter Maccallum Cancer Institute Compounds, preparations and uses thereof
RU2012132682A (ru) * 2009-12-31 2014-02-10 Пирамал Энтерпрайзис Лимитед Ингибиторы диацилглицерин ацилтрансферазы
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
AU2011283684B2 (en) 2010-07-29 2015-08-27 Rigel Pharmaceuticals, Inc. AMPK-activating heterocyclic compounds and methods for using the same
US9938269B2 (en) 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
MY191936A (en) 2012-03-01 2022-07-19 Genentech Inc Serine/threonine kinase inhibitors
US9296701B2 (en) * 2012-04-24 2016-03-29 Vertex Pharmaceuticals Incorporated DNA-PK inhibitors
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
WO2014055634A1 (en) 2012-10-02 2014-04-10 Yale University Identification of small molecule inhibitors of jumonji at-rich interactive domain 1a (jarid1a) and 1b (jarid1b) histone demethylase
RU2702908C2 (ru) 2012-11-01 2019-10-14 Инфинити Фармасьютикалз, Инк. Лечение злокачественных опухолей с использованием модуляторов изоформ pi3-киназы
CA2900012A1 (en) 2013-02-08 2014-08-14 Celgene Avilomics Research, Inc. Erk inhibitors and uses thereof
WO2014130856A2 (en) 2013-02-21 2014-08-28 Wayne Rothbaum Treatment of skeletal-related disorders
US10370371B2 (en) 2013-08-30 2019-08-06 Ptc Therapeutics, Inc. Substituted pyrimidine Bmi-1 inhibitors
US20150087673A1 (en) 2013-09-26 2015-03-26 Rigel Pharmaceuticals, Inc. Methods for using and biomarkers for ampk-activating compounds
AP2016009368A0 (en) 2014-01-14 2016-08-31 Millennium Pharm Inc Heteroaryls and uses thereof
ES2702951T3 (es) 2014-04-04 2019-03-06 Syros Pharmaceuticals Inc Inhibidores de quinasas dependientes de ciclina 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
ES2930050T3 (es) 2015-06-15 2022-12-05 Asana Biosciences Llc Inhibidores heterocíclicos de ERK1 y ERK2 y su uso en el tratamiento de cáncer
EP3317273B1 (en) * 2015-06-30 2021-12-29 Dana-Farber Cancer Institute, Inc. Inhibitors of egfr and methods of use thereof
HUE068392T2 (hu) 2015-10-21 2024-12-28 Otsuka Pharma Co Ltd Benzolaktám vegyületek mint fehérje kináz gátlók
CA3003549A1 (en) 2015-11-09 2017-05-18 Astrazeneca Ab Dihydroimidazopyrazinone derivatives useful in the treatment of cancer
JP6740452B2 (ja) 2016-07-26 2020-08-12 深▲セン▼市塔吉瑞生物医▲薬▼有限公司Shenzhen TargetRx,Inc. プロテインチロシンキナーゼの活性を阻害するためのアミノピリミジン系化合物
GB201706327D0 (en) * 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
EP4352052A1 (en) * 2021-06-11 2024-04-17 Otsuka Pharmaceutical Co., Ltd. Process for preparing an erk inhibitor
US20240415835A1 (en) * 2021-10-26 2024-12-19 Otsuka Pharmaceutical Co., Ltd. Compositions comprising an erk inhibitor

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