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PE20181086A1 - Acetamida tienotrizolodiazepinas y usos de las mismas - Google Patents

Acetamida tienotrizolodiazepinas y usos de las mismas

Info

Publication number
PE20181086A1
PE20181086A1 PE2018000377A PE2018000377A PE20181086A1 PE 20181086 A1 PE20181086 A1 PE 20181086A1 PE 2018000377 A PE2018000377 A PE 2018000377A PE 2018000377 A PE2018000377 A PE 2018000377A PE 20181086 A1 PE20181086 A1 PE 20181086A1
Authority
PE
Peru
Prior art keywords
halogen
optionally substituted
diseases
bromodomain
proteins
Prior art date
Application number
PE2018000377A
Other languages
English (en)
Inventor
James E Bradner
Jun Qi
Minoru Tanaka
Original Assignee
Dana Farber Cancer Inst Inc
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 Dana Farber Cancer Inst Inc filed Critical Dana Farber Cancer Inst Inc
Publication of PE20181086A1 publication Critical patent/PE20181086A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biotechnology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invencion se refiere a derivados de trienotriazolodiazepinas de formula (I) o una sal, estereoisomero o tautomero farmaceuticamente aceptable de los mismos, en donde: Y es como se indica a continuacion; RA1 es H, halogeno, alquilo opcionalmente sustituido, entre otros; RA2 es carbociclilo opcionalmente sustituido, halogeno, entre otros; Rc es halogeno, alquenilo opcionalmente sustituido, entre otros; RB es H, halogeno, alquilo opcionalmente sustituido, entre otros; R2 es H, halogeno, alquilo opcionalmente sustituido, entre otros; X1 es N o CR5; c es 0, 1, 2, 3 o 4; n es 0, 1, 2, 3 o 4; y el anillo C es arilo o heteroarilo. Los compuestos de Formula (I) son moleculas de union de bromodominios y/o proteinas que contienen bromodominios (por ejemplo, proteinas de bromodominio y extra terminal (BET)). Tambien se proporcionan metodos, usos y kits que usan los compuestos y las composiciones farmaceuticas para inhibir la actividad (por ejemplo, la actividad aumentada) de los bromodominios y/o las proteinas que contienen bromodominio y para tratar y/o prevenir en un sujeto enfermedades asociadas con los bromodominios o las proteinas que contienen bromodominio (por ejemplo, enfermedades proliferativas, enfermedades cardiovasculares, infecciones viricas , enfermedades fibroticas, enfermedades metabolicas, enfermedades endocrinas y envenenamiento por radiacion). Los compuestos, las composiciones farmaceuticas y los kits tambien son utiles para la contracepcion masculina
PE2018000377A 2015-09-11 2016-09-09 Acetamida tienotrizolodiazepinas y usos de las mismas PE20181086A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562217544P 2015-09-11 2015-09-11

Publications (1)

Publication Number Publication Date
PE20181086A1 true PE20181086A1 (es) 2018-07-05

Family

ID=58240133

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2018000377A PE20181086A1 (es) 2015-09-11 2016-09-09 Acetamida tienotrizolodiazepinas y usos de las mismas

Country Status (21)

Country Link
US (2) US10881668B2 (es)
EP (1) EP3347020A4 (es)
JP (1) JP2018526424A (es)
KR (1) KR20180051576A (es)
CN (1) CN108472299A (es)
AU (2) AU2016319785C1 (es)
BR (1) BR112018004617A2 (es)
CA (1) CA2996977A1 (es)
CL (1) CL2018000622A1 (es)
CO (1) CO2018002568A2 (es)
CR (1) CR20180199A (es)
HK (1) HK1256419A1 (es)
IL (1) IL257593A (es)
MX (1) MX2018003030A (es)
PE (1) PE20181086A1 (es)
PH (1) PH12018550026A1 (es)
RU (1) RU2018112953A (es)
SG (1) SG10202007099TA (es)
UA (1) UA123946C2 (es)
WO (1) WO2017044792A1 (es)
ZA (1) ZA201801549B (es)

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MX2017001756A (es) 2014-08-08 2017-05-30 Dana Farber Cancer Inst Inc Derivados de diazepano y sus usos.
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
PE20181086A1 (es) * 2015-09-11 2018-07-05 Dana Farber Cancer Inst Inc Acetamida tienotrizolodiazepinas y usos de las mismas
CN108472300A (zh) 2015-09-11 2018-08-31 达纳-法伯癌症研究所股份有限公司 氰基噻吩并三唑并二氮杂环庚三烯及其用途
AU2016361478B2 (en) 2015-11-25 2020-09-10 Dana-Farber Cancer Institute, Inc. Bivalent bromodomain inhibitors and uses thereof
CN107629057B (zh) * 2016-07-19 2020-03-27 上海勋和医药科技有限公司 Bet蛋白抑制剂及其应用
KR20200058483A (ko) * 2017-09-22 2020-05-27 씨에스피씨 종콰이 팔마씨우티컬 테크놀로지 (스자좡) 컴퍼니 리미티드 티에노디아제핀 유도체 및 그의 적용
WO2020177762A1 (zh) * 2019-03-07 2020-09-10 南京明德新药研发有限公司 同时具有BET Bromodomain蛋白抑制和PD-L1基因调控作用的化合物
WO2021175432A1 (en) 2020-03-04 2021-09-10 Boehringer Ingelheim International Gmbh Method for administration of an anti cancer agent
CN112444582B (zh) * 2021-02-01 2021-06-04 宁波大学 基于液滴萃取的质谱分析方法
CN113816970B (zh) * 2021-09-18 2022-08-09 济宁医学院附属医院 一种选择性铜离子螯合剂、其制备方法及其在肺纤维化中的应用

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