CN105008352B - 用作溴区结构域抑制剂的咔唑化合物 - Google Patents

用作溴区结构域抑制剂的咔唑化合物 Download PDF

Info

Publication number
CN105008352B
CN105008352B CN201480010613.1A CN201480010613A CN105008352B CN 105008352 B CN105008352 B CN 105008352B CN 201480010613 A CN201480010613 A CN 201480010613A CN 105008352 B CN105008352 B CN 105008352B
Authority
CN
China
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
CN201480010613.1A
Other languages
English (en)
Chinese (zh)
Other versions
CN105008352A (zh
Inventor
M·A·波斯
D·R·托尔托拉尼
D·S·多德
C·P·穆萨里
J·S·托卡尔斯基
A·V·加瓦伊
赵玉芬
G·V·德卢卡
D·奥马利
D·J·诺里斯
P·吉尔
C·A·魁斯内尔
韩文景
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 CN105008352A publication Critical patent/CN105008352A/zh
Application granted granted Critical
Publication of CN105008352B publication Critical patent/CN105008352B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/55Heterocyclic 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
    • 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
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41921,2,3-Triazoles
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic 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
    • A61K31/435Heterocyclic 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic 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
    • A61K31/535Heterocyclic 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
    • 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
    • A61K31/54Heterocyclic 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
    • 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
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • 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

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)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (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)
CN201480010613.1A 2013-02-27 2014-02-27 用作溴区结构域抑制剂的咔唑化合物 Active CN105008352B (zh)

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 (2)

Publication Number Publication Date
CN105008352A CN105008352A (zh) 2015-10-28
CN105008352B true CN105008352B (zh) 2018-12-07

Family

ID=50382555

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480010613.1A Active CN105008352B (zh) 2013-02-27 2014-02-27 用作溴区结构域抑制剂的咔唑化合物

Country Status (10)

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

Families Citing this family (45)

* 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
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
CA2895905A1 (en) 2012-12-21 2014-06-26 Zenith Epigenetics Corp. Novel heterocyclic compounds as bromodomain inhibitors
US10053454B2 (en) 2013-02-27 2018-08-21 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
AU2014249192B2 (en) 2013-03-11 2017-12-21 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.
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
PL3010503T3 (pl) 2013-06-21 2020-08-24 Zenith Epigenetics Ltd. Nowe bicykliczne inhibitory bromodomen
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
EP3027604B1 (en) 2013-07-31 2019-02-20 Zenith Epigenetics Ltd. Novel quinazolinones as bromodomain inhibitors
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
SMT201800643T1 (it) * 2013-12-24 2019-01-11 Bristol Myers Squibb Co Composti triciclici come agenti anticancro
US9458156B2 (en) 2014-12-23 2016-10-04 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
CA2940554A1 (en) 2014-02-28 2015-09-03 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
KR102702503B1 (ko) 2014-04-23 2024-09-05 인사이트 홀딩스 코포레이션 BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온
MX2016014574A (es) * 2014-05-08 2017-02-23 Oncoethix Gmbh El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo.
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
KR20170055549A (ko) * 2014-10-02 2017-05-19 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 화합물
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
CN107207474B (zh) 2014-12-11 2021-05-07 恒翼生物医药科技(上海)有限公司 被取代的杂环作为溴结构域抑制剂
US10231953B2 (en) 2014-12-17 2019-03-19 Zenith Epigenetics Ltd. Inhibitors of bromodomains
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
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
US10174024B2 (en) 2015-05-12 2019-01-08 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
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
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
ES3037659T3 (en) 2016-03-30 2025-10-03 Wisconsin Alumni Res Found Methods and compositions for modulating frataxin expression
PH12021551886A1 (en) 2016-06-20 2023-07-17 Incyte Corp Crystalline solid forms of a bet inhibitor
CA3050309A1 (en) 2017-01-31 2018-08-09 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2018183679A1 (en) 2017-03-29 2018-10-04 Wisconsin Alumni Research Foundation Methods and compositions for modulating gene expression
EP3743066A4 (en) 2018-01-26 2021-09-08 Yale University IMIDE-BASED PROTEOLYSIS MODULATORS AND RELATED METHODS OF USE
CR20220353A (es) 2019-12-19 2022-10-20 Arvinas Operations Inc Compuestos y métodos para la degradación dirigida del receptor de andrógenos
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002079154A1 (en) * 2001-03-28 2002-10-10 Eli Lilly And Company Substituted carbazoles as inhibitors of spla2
CN102325752A (zh) * 2008-12-19 2012-01-18 百时美施贵宝公司 咔唑和咔啉激酶抑制剂
CN102762569A (zh) * 2009-11-05 2012-10-31 葛兰素史克有限责任公司 苯并二氮杂*溴区结构域抑制剂
US20130026426A1 (en) * 2011-07-29 2013-01-31 Shigeyuki Harada Carbazole derivative and semiconductor nanocrystal

Family Cites Families (10)

* 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
EP1300159B1 (en) * 2000-06-29 2007-10-10 Anthera Pharmaceuticals, Inc. Remedies for cancer
US6602619B2 (en) 2001-10-19 2003-08-05 Lightronik Technology Inc. Organic EL device
EP1677786A1 (en) 2003-10-18 2006-07-12 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
US8916593B2 (en) 2010-05-04 2014-12-23 Pfizer Inc. Alkoxy-substituted 2-aminopyridines 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
EP2694619A4 (en) * 2011-05-03 2014-10-22 Rohm & Haas Elect Mat NEW ORGANIC ELECTROLUMINESCENSE COMPOUNDS AND ORGANIC ELECTROLUMINESCENCE DEVICE THEREWITH
UA115576C2 (uk) * 2012-12-06 2017-11-27 Байєр Фарма Акцієнгезелльшафт Похідні бензимідазолу як антагоністи ер4

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002079154A1 (en) * 2001-03-28 2002-10-10 Eli Lilly And Company Substituted carbazoles as inhibitors of spla2
CN102325752A (zh) * 2008-12-19 2012-01-18 百时美施贵宝公司 咔唑和咔啉激酶抑制剂
CN102762569A (zh) * 2009-11-05 2012-10-31 葛兰素史克有限责任公司 苯并二氮杂*溴区结构域抑制剂
US20130026426A1 (en) * 2011-07-29 2013-01-31 Shigeyuki Harada Carbazole derivative and semiconductor nanocrystal

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Synthesis of Carbazoles from N-(N,N-Diarylamino)phthalimides with Aluminum Chloride via Diarylnitrenium Ions;Yasuo Kikugawa,等;《J. Org. Chem.》;20011115;第66卷(第25期);第8614页 *
Youai Qiu,等.Carbazoles via AuCl3‑Catalyzed Cyclization of 1‑(Indol-2-yl)-3-alkyn-1-ols.《ORGANIC LETTERS》.2012,第14卷(第24期),第6200页. *

Also Published As

Publication number Publication date
JP2016515098A (ja) 2016-05-26
CN105008352A (zh) 2015-10-28
WO2014134232A1 (en) 2014-09-04
BR112015020389A8 (pt) 2019-11-12
ES2669189T3 (es) 2018-05-24
US9492460B2 (en) 2016-11-15
CA2902737A1 (en) 2014-09-04
MX2015010921A (es) 2016-01-12
EA201591591A1 (ru) 2015-12-30
US20140256700A1 (en) 2014-09-11
BR112015020389A2 (pt) 2017-07-18
EP2961748A1 (en) 2016-01-06
EA027345B1 (ru) 2017-07-31
JP6395731B2 (ja) 2018-09-26
EP2961748B1 (en) 2018-03-28

Similar Documents

Publication Publication Date Title
CN105008352B (zh) 用作溴区结构域抑制剂的咔唑化合物
CN105189488B (zh) 用作溴区结构域抑制剂的咔唑化合物
CN106029663B (zh) 作为抗癌剂的新颖三环化合物
CN105209443B (zh) 吲哚胺2,3-双加氧酶(ido)抑制剂
TWI429640B (zh) 作為激酶抑制劑之雜雙環甲醯胺
CN107709322B (zh) 作为抗癌剂的三环化合物
TW201629026A (zh) 作為hdac抑制劑的3-烷基雙環[4,5,0]異羥肟酸
TW201014855A (en) Compounds for the treatment of hepatitis C
CN110167935A (zh) 作为αV整合素抑制剂的3-经取代的丙酸
US10683290B2 (en) Tricyclic compounds as anticancer agents
CN114014844B (zh) 氨基吡啶衍生物及其作为选择性alk-2抑制剂的用途
CN107922353A (zh) Ido抑制剂
WO2016183115A1 (en) 5h-pyrido[3,2-b]indole compounds as anticancer agents
CN109071548A (zh) 可用于治疗尤其是癌症的吡咯并咪唑衍生物或其类似物
WO2023246837A1 (zh) 一类具有嘧啶并六元环结构的化合物、包含其的药物组合物及其应用
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
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant