KR20170055549A - 화합물 - Google Patents

화합물 Download PDF

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Publication number
KR20170055549A
KR20170055549A KR1020177010949A KR20177010949A KR20170055549A KR 20170055549 A KR20170055549 A KR 20170055549A KR 1020177010949 A KR1020177010949 A KR 1020177010949A KR 20177010949 A KR20177010949 A KR 20177010949A KR 20170055549 A KR20170055549 A KR 20170055549A
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KR
South Korea
Prior art keywords
methyloxy
chlorophenyl
methyl
triazolo
benzodiazepin
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
KR1020177010949A
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English (en)
Korean (ko)
Inventor
고세트 아우구스투스 캠벨
아사 엘리자베스 글래드윈
Original Assignee
글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드
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Application filed by 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 filed Critical 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드
Publication of KR20170055549A publication Critical patent/KR20170055549A/ko
Withdrawn legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020177010949A 2014-10-02 2015-09-30 화합물 Withdrawn KR20170055549A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462058753P 2014-10-02 2014-10-02
US62/058,753 2014-10-02
PCT/EP2015/072515 WO2016050821A1 (en) 2014-10-02 2015-09-30 Compound

Publications (1)

Publication Number Publication Date
KR20170055549A true KR20170055549A (ko) 2017-05-19

Family

ID=54238438

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020177010949A Withdrawn KR20170055549A (ko) 2014-10-02 2015-09-30 화합물

Country Status (10)

Country Link
US (3) US9975901B2 (enExample)
EP (1) EP3201199A1 (enExample)
JP (1) JP2017530155A (enExample)
KR (1) KR20170055549A (enExample)
CN (1) CN106715439A (enExample)
AU (1) AU2015326910B2 (enExample)
BR (1) BR112017006342A2 (enExample)
CA (1) CA2960090A1 (enExample)
RU (1) RU2697393C2 (enExample)
WO (1) WO2016050821A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HK1208875A1 (en) 2012-01-12 2016-03-18 耶鲁大学 Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2016090219A1 (en) 2014-12-05 2016-06-09 H. Lee Moffitt Cancer Center And Research Institute, Inc. Bromodomain inhibitor as adjuvant in cancer immunotherapy
CN108601764A (zh) 2015-03-18 2018-09-28 阿尔维纳斯股份有限公司 用于靶蛋白的增强降解的化合物和方法
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
EP3539960A4 (en) 2016-11-10 2020-03-18 Luoxin Pharmaceutical (Shanghai) Co., Ltd. NITROGEN MACROCYCLIC COMPOUND, ITS PREPARATION METHOD, ITS PHARMACEUTICAL COMPOSITION AND ITS APPLICATION
CA3050309A1 (en) 2017-01-31 2018-08-09 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
EP3743066A4 (en) 2018-01-26 2021-09-08 Yale University IMIDE-BASED PROTEOLYSIS MODULATORS AND RELATED METHODS OF USE
JP2021521192A (ja) 2018-04-13 2021-08-26 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． セレブロンリガンドおよび同リガンドを含む二機能性化合物
CR20220353A (es) 2019-12-19 2022-10-20 Arvinas Operations Inc Compuestos y métodos para la degradación dirigida del receptor de andrógenos
CN111533745A (zh) * 2020-05-20 2020-08-14 成都药明康德新药开发有限公司 叔丁基-3-(氨基甲基)二氢-5h-三唑并二氮杂卓-8(9h)-甲酸基酯制法
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR9710453A (pt) * 1996-06-12 1999-08-17 Japan Tobacco Inc Inhibidor de produ-Æo de citocina composto de triazepina e intermedi rio para o mesmo
JP5478262B2 (ja) * 2007-12-28 2014-04-23 田辺三菱製薬株式会社 抗癌剤
HUE026967T2 (en) * 2009-11-05 2016-07-28 Glaxosmithkline Llc Benzodiazepine Bromodomain inhibitor
DK2722334T3 (en) * 2009-11-05 2016-03-07 Glaxosmithkline Llc benzodiazepine bromdomæneinhibitor
GB201106743D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
AU2012330885B2 (en) * 2011-11-01 2016-10-06 Resverlogix Corp. Oral immediate release formulations for substituted quinazolinones
US9492460B2 (en) * 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors

Also Published As

Publication number Publication date
AU2015326910B2 (en) 2018-03-01
BR112017006342A2 (pt) 2017-12-19
US20170298071A1 (en) 2017-10-19
RU2697393C2 (ru) 2019-08-14
RU2017107760A3 (enExample) 2019-03-01
US9975901B2 (en) 2018-05-22
RU2017107760A (ru) 2018-11-02
US20180305365A1 (en) 2018-10-25
CN106715439A (zh) 2017-05-24
WO2016050821A1 (en) 2016-04-07
JP2017530155A (ja) 2017-10-12
US20190389870A1 (en) 2019-12-26
AU2015326910A1 (en) 2017-03-30
CA2960090A1 (en) 2016-04-07
EP3201199A1 (en) 2017-08-09
US10450319B2 (en) 2019-10-22

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Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20170421

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination