CA2689989A1 - Heterocyclic compounds and uses thereof - Google Patents

Heterocyclic compounds and uses thereof Download PDF

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Publication number
CA2689989A1
CA2689989A1 CA2689989A CA2689989A CA2689989A1 CA 2689989 A1 CA2689989 A1 CA 2689989A1 CA 2689989 A CA2689989 A CA 2689989A CA 2689989 A CA2689989 A CA 2689989A CA 2689989 A1 CA2689989 A1 CA 2689989A1
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CA
Canada
Prior art keywords
halogen
compound
pdgfr
oxo
nhc
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Abandoned
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CA2689989A
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English (en)
French (fr)
Inventor
Juswinder Singh
Shomir Ghosh
Arthur F. Kluge
Russell C. Petter
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Celgene Avilomics Research Inc
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Individual
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Publication of CA2689989A1 publication Critical patent/CA2689989A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
CA2689989A 2007-06-04 2008-06-03 Heterocyclic compounds and uses thereof Abandoned CA2689989A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US94187307P 2007-06-04 2007-06-04
US60/941,873 2007-06-04
US97204807P 2007-09-13 2007-09-13
US60/972,048 2007-09-13
PCT/US2008/065646 WO2008151183A1 (en) 2007-06-04 2008-06-03 Heterocyclic compounds and uses thereof

Publications (1)

Publication Number Publication Date
CA2689989A1 true CA2689989A1 (en) 2008-12-11

Family

ID=40089003

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2689989A Abandoned CA2689989A1 (en) 2007-06-04 2008-06-03 Heterocyclic compounds and uses thereof

Country Status (6)

Country Link
US (4) US8242271B2 (enExample)
EP (1) EP2152079A4 (enExample)
JP (3) JP5526020B2 (enExample)
CA (1) CA2689989A1 (enExample)
TW (1) TWI433677B (enExample)
WO (1) WO2008151183A1 (enExample)

Families Citing this family (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2152079A4 (en) * 2007-06-04 2011-03-09 Avila Therapeutics Inc HETEROCYCLIC COMPOUNDS AND USES THEREOF
EP2300013B2 (en) 2008-05-21 2024-11-13 Takeda Pharmaceutical Company Limited Phosphorous derivatives as kinase inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US8338439B2 (en) * 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
KR101341876B1 (ko) * 2008-09-05 2013-12-20 셀진 아빌로믹스 리서치, 인코포레이티드 비가역 인히비터 디자인을 위한 알고리즘
WO2010039545A2 (en) * 2008-09-23 2010-04-08 Georgetown University 1,2-benzisothiazolinone and isoindolinone derivatives
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Egfr阻害剤及び疾患の治療方法
EP2440058A4 (en) 2009-06-12 2012-11-21 Dana Farber Cancer Inst Inc MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
CN101928277B (zh) * 2009-06-24 2012-09-19 浙江九洲药业股份有限公司 4-甲基-3-[[4-(3-吡啶基)-2-嘧啶基]氨基]安息香酸的制备方法、相关中间体及其应用
CN102548987B (zh) * 2009-07-14 2014-04-16 江苏迈度药物研发有限公司 作为激酶抑制剂的氟取代化合物及其使用方法
RU2595718C2 (ru) * 2009-09-09 2016-08-27 Селджен Авиломикс Рисерч,Инк. Ингибиторы pi3-киназы и их применение
US9556426B2 (en) * 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
AU2010339456A1 (en) 2009-12-30 2012-07-05 Celgene Avilomics Research, Inc. Ligand-directed covalent modification of protein
CN105566229A (zh) 2010-08-10 2016-05-11 西建阿维拉米斯研究公司 Btk抑制剂的苯磺酸盐及其用途和制备方法
SG10201508958WA (en) 2010-11-01 2015-11-27 Celgene Avilomics Res Inc Heterocyclic Compounds And Uses Thereof
US9238629B2 (en) 2010-11-01 2016-01-19 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
US9428472B2 (en) 2011-08-16 2016-08-30 Georgetown University Methods of treating bacterial infections with 1,2-benzisothiazolinone and isoindolinone derivatives
JP2014532658A (ja) 2011-10-28 2014-12-08 セルジーン アヴィロミクス リサーチ, インコーポレイテッド ブルトン型チロシンキナーゼ疾患または障害を治療する方法
WO2013074986A1 (en) * 2011-11-17 2013-05-23 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
JP6317319B2 (ja) 2012-03-15 2018-04-25 セルジーン シーエーアール エルエルシー 上皮成長因子受容体キナーゼ阻害剤の固体形態
CA2866857C (en) 2012-03-15 2021-03-09 Celgene Avilomics Research, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Egfr発動性がんの細胞増殖阻害用化合物
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
EP2935226A4 (en) 2012-12-21 2016-11-02 Celgene Avilomics Res Inc HETEROARYL COMPOUNDS AND USES THEREOF
US9561228B2 (en) 2013-02-08 2017-02-07 Celgene Avilomics Research, Inc. ERK inhibitors and uses thereof
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
IN2013MU02611A (enExample) 2013-08-07 2015-06-12 Cadila Healthcare Ltd
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
RU2016141934A (ru) 2014-04-04 2018-05-07 Сирос Фармасьютикалз, Инк. Ингибиторы циклин-зависимой киназы 7 (cdk7)
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2016020791A1 (en) * 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
US10005760B2 (en) 2014-08-13 2018-06-26 Celgene Car Llc Forms and compositions of an ERK inhibitor
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND CHINESE INHIBITORS
WO2017030892A1 (en) 2015-08-14 2017-02-23 Reaction Biology Corp. Histone deacetylase inhibitors and methods for use thereof
JP7028766B2 (ja) 2015-09-09 2022-03-02 ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド サイクリン依存性キナーゼの阻害剤
MA46205A (fr) * 2016-09-08 2019-07-17 Sabila Biosciences Llc Composés 1,2-dithiolane utiles dans la neuroprotection, les maladies et les états auto-immuns et cancéreux
CN107805240A (zh) * 2016-09-08 2018-03-16 中国科学院合肥物质科学研究院 一种新型的pdgfr激酶抑制剂及其用途
GB201616511D0 (en) 2016-09-29 2016-11-16 Mission Therapeutics Limited Novel compounds
GB201616627D0 (en) 2016-09-30 2016-11-16 Mission Therapeutics Limited Novel compounds
GB201708652D0 (en) 2017-05-31 2017-07-12 Mission Therapeutics Ltd Novel compounds and uses
CN110831936B (zh) 2017-06-20 2023-03-28 特殊治疗有限公司 具有dub抑制剂活性的取代氰基吡咯烷
EP3801503A4 (en) 2018-06-07 2021-12-08 Disarm Therapeutics, Inc. INHIBITORS OF SARM1
CN108623490A (zh) * 2018-06-22 2018-10-09 苏州市贝克生物科技有限公司 (2z)-4-(二甲基氨基)-2-丁烯酸盐酸盐的合成方法
JP7590185B2 (ja) 2018-06-25 2024-11-26 ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド Taireファミリーキナーゼインヒビターおよびそれらの使用
CN113164508B (zh) 2018-12-19 2025-07-08 达萨玛治疗公司 与神经保护剂组合的sarm1抑制剂
WO2020140098A1 (en) 2018-12-28 2020-07-02 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
GB201905371D0 (en) 2019-04-16 2019-05-29 Mission Therapeutics Ltd Novel compounds
GB201905375D0 (en) 2019-04-16 2019-05-29 Mission Therapeutics Ltd Novel compounds
US12624025B2 (en) 2019-06-06 2026-05-12 Disarm Therapeutics, Inc. Inhibitors of SARM1
GB201912674D0 (en) 2019-09-04 2019-10-16 Mission Therapeutics Ltd Novel compounds
CN111253335B (zh) * 2020-03-12 2023-06-06 浙江扬帆新材料股份有限公司 一种n-取代苯并异噻唑啉-3-酮衍生物的新合成方法
CN111269217B (zh) * 2020-04-07 2021-01-08 苏州信诺维医药科技有限公司 一种嘧啶胺类化合物、其制备方法及应用
BR112022020058A2 (pt) 2020-04-08 2022-11-22 Mission Therapeutics Ltd N-cianopirrolidinas com atividade como inibidores de usp30
BR112022020644A2 (pt) 2020-05-28 2022-12-06 Mission Therapeutics Ltd Derivados de n-(1-ciano-pirrolidin-3-il)-5-(3-(trifluorometil)fenil) oxazol-2-carboxamida e os correspondentes derivados de oxadiazol como inibidores de usp30 para o tratamento de disfunção mitocondrial
JP7796047B2 (ja) 2020-06-04 2026-01-08 ミッション セラピューティクス リミティド Usp30阻害剤としての活性を有するn-シアノピロリジン
DK4161929T3 (da) 2020-06-08 2025-08-18 Mission Therapeutics Ltd 1-(5-(2-cyanopyridin-4-yl)oxazol-2-carbonyl)-4-methylhexahydropyrrolo[3,4-b]pyrrol-5(1h)-carbonitril som usp30-hæmmer til anvendelse i behandling af mitokondriedysfunktion, cancer og fibrose
GB202016800D0 (en) 2020-10-22 2020-12-09 Mission Therapeutics Ltd Novel compounds
JP2024544660A (ja) 2021-12-01 2024-12-03 ミッション セラピューティクス リミティド Usp30阻害剤としての活性を有する置換n-シアノピロリジン
AU2023309768A1 (en) * 2022-07-19 2025-02-27 Chiesi Farmaceutici S.P.A. HETEROARYL DERIVATIVES AS DDRs INHIBITORS
GB202408928D0 (en) 2024-06-21 2024-08-07 Mission Therapeutics Ltd Novel compounds
GB202411060D0 (en) 2024-07-29 2024-09-11 Mission Therapeutics Ltd Novel compounds

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
GB0022438D0 (en) * 2000-09-13 2000-11-01 Novartis Ag Organic Compounds
US20040157855A1 (en) * 2001-04-05 2004-08-12 Michael Heinrich Use of n-phenyl-2-pyrimidineamine derivativea against mast cell-based diseases like allergic disorders
CA2446939C (en) * 2001-05-16 2005-08-02 Matthias Stein-Gerlach Pyridylpyrimidine derivatives as effective compounds against prion diseases
US6878697B2 (en) * 2001-06-21 2005-04-12 Ariad Pharmaceuticals, Inc. Phenylamino-pyrimidines and uses thereof
DK1442024T3 (da) 2001-11-01 2008-06-30 Janssen Pharmaceutica Nv Aminobenzamidderivater som glycogensystasekinase 3 beta-inhibitorer
MXPA04004178A (es) * 2001-11-01 2004-09-06 Janssen Pharmaceutica Nv Heteroarilaminas como inhibidores de glucogeno cintasa cinasa 3beta.
GB0201508D0 (en) * 2002-01-23 2002-03-13 Novartis Ag Organic compounds
GB0202873D0 (en) * 2002-02-07 2002-03-27 Novartis Ag Organic compounds
GB0215676D0 (en) * 2002-07-05 2002-08-14 Novartis Ag Organic compounds
EP1527345A2 (en) * 2002-07-29 2005-05-04 Axxima Pharmaceuticals AG Method for isolating atp binding proteins by means of immobilized protein inhibitors
MY139563A (en) * 2002-09-04 2009-10-30 Bristol Myers Squibb Co Heterocyclic aromatic compounds useful as growth hormone secretagogues
CA2439440A1 (en) * 2002-09-05 2004-03-05 Emory University Treatment of tuberous sclerosis associated neoplasms
GB0222514D0 (en) 2002-09-27 2002-11-06 Novartis Ag Organic compounds
US7279576B2 (en) * 2002-12-31 2007-10-09 Deciphera Pharmaceuticals, Llc Anti-cancer medicaments
US7144911B2 (en) * 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
WO2005065074A2 (en) 2003-09-09 2005-07-21 Temple University Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
GB0325031D0 (en) * 2003-10-27 2003-12-03 Novartis Ag Organic compounds
WO2005049021A1 (en) 2003-11-03 2005-06-02 Oy Helsinki Transplantation R & D Ltd Materials and methods for inhibiting neointimal hyperplasia
JPWO2005063709A1 (ja) * 2003-12-25 2007-07-19 日本新薬株式会社 アミド誘導体及び医薬
JPWO2005063720A1 (ja) 2003-12-25 2007-07-19 日本新薬株式会社 アミド誘導体及び医薬
WO2005072826A2 (en) 2004-01-21 2005-08-11 Emory University Compositions and use of tyrosine kinase inhibitors to treat pathogenic infection
AU2005245386B2 (en) * 2004-05-07 2008-11-27 Amgen Inc. Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer
WO2005115385A1 (en) 2004-05-24 2005-12-08 Ab Science Use of c-kit inhibitors for treating acne
WO2006017353A2 (en) 2004-07-13 2006-02-16 GOVERNMENT OF THE UNITED STATES, as represented byTHE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES Treatment of viral infections
WO2006021458A2 (en) 2004-08-27 2006-03-02 Gpc Biotech Ag Pyrimidine derivatives
BRPI0606872A2 (pt) 2005-01-28 2009-07-21 Novartis Ag uso de pirimidilaminobenzamidas para o tratamento de doenças que respondem à modulação de atividade de tie-2 quinase
MX2007011866A (es) 2005-02-25 2007-10-10 Novartis Ag Combinacion farmaceutica de inhibidores de bcr-abl y raf.
CN103638028A (zh) 2005-05-02 2014-03-19 诺瓦提斯公司 嘧啶基氨基苯甲酰胺衍生物用于治疗全身性肥大细胞增多症的应用
SA06270147B1 (ar) 2005-06-09 2009-12-22 نوفارتيس ايه جي عملية لتخليق 5-(مثيل–1h–إيميدازول–1-يل )–3-(ثلاثي فلـورو مثيل)–بنزامـين
JP2009501766A (ja) 2005-07-20 2009-01-22 ノバルティス アクチエンゲゼルシャフト 増殖性疾患の処置のためのピリミジルアミノベンズアミドおよびFlt−3阻害剤を含む組合せ剤
KR100674813B1 (ko) 2005-08-05 2007-01-29 일양약품주식회사 N-페닐-2-피리미딘-아민 유도체 및 그의 제조방법
WO2007065898A1 (en) 2005-12-06 2007-06-14 Novartis Ag Pyrimidylaminobenzamide derivatives for the treatment of neurofibromatosis
AU2007317349B2 (en) * 2006-11-03 2011-10-20 Irm Llc Compounds and compositions as protein kinase inhibitors
EP2152079A4 (en) * 2007-06-04 2011-03-09 Avila Therapeutics Inc HETEROCYCLIC COMPOUNDS AND USES THEREOF
KR101341876B1 (ko) * 2008-09-05 2013-12-20 셀진 아빌로믹스 리서치, 인코포레이티드 비가역 인히비터 디자인을 위한 알고리즘

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