JP6395731B2 - ブロモドメイン阻害剤として有用なカルバゾール化合物 - Google Patents

ブロモドメイン阻害剤として有用なカルバゾール化合物 Download PDF

Info

Publication number
JP6395731B2
JP6395731B2 JP2015560285A JP2015560285A JP6395731B2 JP 6395731 B2 JP6395731 B2 JP 6395731B2 JP 2015560285 A JP2015560285 A JP 2015560285A JP 2015560285 A JP2015560285 A JP 2015560285A JP 6395731 B2 JP6395731 B2 JP 6395731B2
Authority
JP
Japan
Prior art keywords
carbazole
dimethyl
carboxamide
oxazol
carbonyl
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.)
Active
Application number
JP2015560285A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016515098A (ja
JP2016515098A5 (https=
Inventor
マイケル・エイ・ポス
デイビッド・アール・トートラニ
ダームパル・エス・ドッド
クリストファー・ピー・マッサリ
ジョン・エス・トカルスキー
アシュビニクマール・ブイ・ガバイ
ユーフェン・ジャオ
ジョージ・ブイ・デルッカ
ダニエル・オマリー
デレク・ジェイ・ノリス
パトリス・ジル
クロード・ア・ケスネル
ウェン−チン・ハン
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.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
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
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of JP2016515098A publication Critical patent/JP2016515098A/ja
Publication of JP2016515098A5 publication Critical patent/JP2016515098A5/ja
Application granted granted Critical
Publication of JP6395731B2 publication Critical patent/JP6395731B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • A61K31/553—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic 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
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
JP2015560285A 2013-02-27 2014-02-27 ブロモドメイン阻害剤として有用なカルバゾール化合物 Active JP6395731B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361769996P 2013-02-27 2013-02-27
US61/769,996 2013-02-27
US14/190,477 2014-02-26
US14/190,477 US9492460B2 (en) 2013-02-27 2014-02-26 Carbazole compounds useful as bromodomain inhibitors
PCT/US2014/018820 WO2014134232A1 (en) 2013-02-27 2014-02-27 Carbazole compounds useful as bromodomain inhibitors

Publications (3)

Publication Number Publication Date
JP2016515098A JP2016515098A (ja) 2016-05-26
JP2016515098A5 JP2016515098A5 (https=) 2017-03-30
JP6395731B2 true JP6395731B2 (ja) 2018-09-26

Family

ID=50382555

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015560285A Active JP6395731B2 (ja) 2013-02-27 2014-02-27 ブロモドメイン阻害剤として有用なカルバゾール化合物

Country Status (10)

Country Link
US (1) US9492460B2 (https=)
EP (1) EP2961748B1 (https=)
JP (1) JP6395731B2 (https=)
CN (1) CN105008352B (https=)
BR (1) BR112015020389A8 (https=)
CA (1) CA2902737A1 (https=)
EA (1) EA027345B1 (https=)
ES (1) ES2669189T3 (https=)
MX (1) MX2015010921A (https=)
WO (1) WO2014134232A1 (https=)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2861066C (en) 2012-01-12 2024-01-02 Yale University Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
AU2013365926B9 (en) 2012-12-21 2019-01-17 Zenith Epigenetics Ltd. Novel heterocyclic compounds as bromodomain inhibitors
CN105189488B (zh) 2013-02-27 2018-07-24 百时美施贵宝公司 用作溴区结构域抑制剂的咔唑化合物
EP2970312B1 (en) 2013-03-11 2017-11-15 The Regents of The University of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
EP3010918B1 (en) 2013-06-21 2018-08-15 Zenith Epigenetics Ltd. Novel substituted bicyclic compounds as bromodomain inhibitors
CA2915838C (en) 2013-06-21 2023-04-18 Zenith Epigenetics Corp. Bicyclic bromodomain inhibitors
AR096837A1 (es) 2013-07-08 2016-02-03 Incyte Corp Heterociclos tricíclicos como inhibidores de proteínas bet
JP6542212B2 (ja) 2013-07-31 2019-07-10 ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． ブロモドメイン阻害剤としての新規キナゾリノン
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
US9458156B2 (en) 2014-12-23 2016-10-04 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
ES2857848T3 (es) * 2013-12-24 2021-09-29 Bristol Myers Squibb Co Compuestos tricíclicos como agentes antineoplásicos
US9580430B2 (en) 2014-02-28 2017-02-28 The Regents Of The University Of Michigan 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
EA034972B1 (ru) 2014-04-23 2020-04-13 Инсайт Корпорейшн 1h-пирроло[2,3-c]пиридин-7(6h)-оны в качестве ингибиторов белков bet
CA2947970A1 (en) * 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating triple-negative breast cancer using thienotriazolodiazepine compounds
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
AU2015326910B2 (en) * 2014-10-02 2018-03-01 Glaxosmithkline Intellectual Property (No.2) Limited Compound
EP3227281A4 (en) 2014-12-01 2018-05-30 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
HK1246273B (en) 2014-12-01 2019-12-06 恒翼生物医药(上海)股份有限公司 Substituted pyridines as bromodomain inhibitors
EP3230277B1 (en) 2014-12-11 2019-09-18 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
HK1245247A1 (zh) 2014-12-17 2018-08-24 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
US10730870B2 (en) 2015-03-18 2020-08-04 Arvinas Operations, Inc. Compounds and methods for the enhanced degradation of targeted proteins
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
EP3294736B1 (en) * 2015-05-11 2020-07-22 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
EP3307740B1 (en) 2015-05-12 2019-12-18 Bristol-Myers Squibb Company 5h-pyrido[3,2-b]indole compounds as anticancer agents
US9725449B2 (en) * 2015-05-12 2017-08-08 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
WO2017011371A1 (en) 2015-07-10 2017-01-19 Arvinas, Inc Mdm2-based modulators of proteolysis and associated methods of use
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
US10550091B2 (en) 2016-03-25 2020-02-04 St. Jude Children's Research Hospital 1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor
WO2017172914A1 (en) 2016-03-30 2017-10-05 Wisconsin Alumni Research Foundation Methods and compositions for modulating frataxin expression
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
KR102643344B1 (ko) 2016-06-20 2024-03-07 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
BR112019015484A2 (pt) 2017-01-31 2020-04-28 Arvinas Operations Inc ligantes de cereblon e compostos bifuncionais compreendendo os mesmos
WO2018183679A1 (en) 2017-03-29 2018-10-04 Wisconsin Alumni Research Foundation Methods and compositions for modulating gene expression
US11220515B2 (en) 2018-01-26 2022-01-11 Yale University Imide-based modulators of proteolysis and associated methods of use
CA3165168A1 (en) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN111809182B (zh) * 2020-07-08 2025-04-18 江苏和达电子科技有限公司 一种用于铜/钼（铌）/igzo膜层的刻蚀液及其制备方法和应用
US12016847B2 (en) 2021-03-12 2024-06-25 Bristol-Myers Squibb Company Methods of treating prostate cancer
AU2023273729A1 (en) * 2022-05-20 2024-12-05 University Of Puerto Rico 1,4,5-trisubstituted-1,2,3-triazoles and uses thereof
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
US20260092058A1 (en) 2024-09-30 2026-04-02 St. Jude Children's Research Hospital, Inc. Small Molecule Degraders and Fluorescent Probes of PXR

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9310635D0 (en) * 1993-05-21 1993-07-07 Glaxo Group Ltd Chemical compounds
US6177440B1 (en) 1996-10-30 2001-01-23 Eli Lilly And Company Substituted tricyclics
DE60130891T2 (de) * 2000-06-29 2008-07-17 Anthera Pharmaceuticals Inc., San Mateo Heilmittel für krebs
CA2441077A1 (en) * 2001-03-28 2002-10-10 Eli Lilly And Company Substituted carbazoles as inhibitors of spla2
US6602619B2 (en) 2001-10-19 2003-08-05 Lightronik Technology Inc. Organic EL device
CA2542682A1 (en) 2003-10-18 2005-05-06 Bayer Healthcare Ag 5-substituted 2-(phenylmethyl) thio-4-phenyl-4h-1,2,4-triazole derivatives and related compounds as gaba-agonists for the treatment of urinary incontinence and related diseases
WO2006012310A2 (en) * 2004-06-25 2006-02-02 Genzyme Corporation Carbazole derivatives for treating polycystic kidney disease
US8815840B2 (en) * 2008-12-19 2014-08-26 Bristol-Myers Squibb Company Carbazole and carboline kinase inhibitors
ES2563057T3 (es) * 2009-11-05 2016-03-10 Glaxosmithkline Llc Inhibidor de bromodominio de benzodiazepina
EP2566858A2 (en) 2010-05-04 2013-03-13 Pfizer Inc. Heterocyclic derivatives as alk inhibitors
JP5623996B2 (ja) 2010-09-21 2014-11-12 株式会社半導体エネルギー研究所 カルバゾール誘導体
JP5842630B2 (ja) 2011-03-16 2016-01-13 株式会社リコー カルバゾール誘導体、及び半導体ナノ結晶
TW201302973A (zh) * 2011-05-03 2013-01-16 羅門哈斯電子材料韓國公司 新穎有機電場發光化合物及使用該化合物之有機電場發光裝置
UA115576C2 (uk) * 2012-12-06 2017-11-27 Байєр Фарма Акцієнгезелльшафт Похідні бензимідазолу як антагоністи ер4

Also Published As

Publication number Publication date
WO2014134232A1 (en) 2014-09-04
EA027345B1 (ru) 2017-07-31
US9492460B2 (en) 2016-11-15
JP2016515098A (ja) 2016-05-26
EP2961748B1 (en) 2018-03-28
CA2902737A1 (en) 2014-09-04
US20140256700A1 (en) 2014-09-11
EP2961748A1 (en) 2016-01-06
BR112015020389A2 (pt) 2017-07-18
ES2669189T3 (es) 2018-05-24
EA201591591A1 (ru) 2015-12-30
CN105008352B (zh) 2018-12-07
BR112015020389A8 (pt) 2019-11-12
CN105008352A (zh) 2015-10-28
MX2015010921A (es) 2016-01-12

Similar Documents

Publication Publication Date Title
JP6395731B2 (ja) ブロモドメイン阻害剤として有用なカルバゾール化合物
JP6404838B2 (ja) ブロモドメイン阻害剤として有用なカルバゾール化合物
US10112941B2 (en) Tricyclic compounds as anticancer agents
JP6675501B2 (ja) 抗がん剤としての三環式化合物
JP6843767B2 (ja) 抗がん剤としての三環式化合物
MD3269370T2 (ro) Compus pirimidinic condensat nou sau sare a acestuia
ES2770349T3 (es) Compuestos de 5H-pirido[3,2-b]indol como agentes antineoplásicos
US10683290B2 (en) Tricyclic compounds as anticancer agents
TW202214634A (zh) 雜環化合物及其衍生物
TW201444828A (zh) 可作爲溴區結構域蛋白抑制劑之咔唑化合物

Legal Events

Date Code Title Description
RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20160219

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170224

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20170224

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20180118

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180130

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20180427

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180515

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20180807

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20180828

R150 Certificate of patent or registration of utility model

Ref document number: 6395731

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250