UA122130C2 - Інгібітори бромодомену - Google Patents

Інгібітори бромодомену Download PDF

Info

Publication number
UA122130C2
UA122130C2 UAA201704436A UAA201704436A UA122130C2 UA 122130 C2 UA122130 C2 UA 122130C2 UA A201704436 A UAA201704436 A UA A201704436A UA A201704436 A UAA201704436 A UA A201704436A UA 122130 C2 UA122130 C2 UA 122130C2
Authority
UA
Ukraine
Prior art keywords
compound
alkyl
copy
pharmaceutically acceptable
acceptable salt
Prior art date
Application number
UAA201704436A
Other languages
English (en)
Ukrainian (uk)
Inventor
Стівен Б. Ландау
Стивен Б. ЛАНДАУ
Майкл Кегі
Майкл Кэги
Original Assignee
Тенша Терапеутікс, Інк.
Тенша Терапеутикс, Инк.
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 Тенша Терапеутікс, Інк., Тенша Терапеутикс, Инк. filed Critical Тенша Терапеутікс, Інк.
Publication of UA122130C2 publication Critical patent/UA122130C2/uk

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
    • A61K31/551Heterocyclic 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
    • 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
    • A61K31/551Heterocyclic 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
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • 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
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D255/00Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C07D255/04Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic 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
    • C07D495/14Ortho-condensed systems
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
UAA201704436A 2014-10-27 2015-10-27 Інгібітори бромодомену UA122130C2 (uk)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462068983P 2014-10-27 2014-10-27
PCT/US2015/057538 WO2016069578A1 (en) 2014-10-27 2015-10-27 Bromodomain inhibitors

Publications (1)

Publication Number Publication Date
UA122130C2 true UA122130C2 (uk) 2020-09-25

Family

ID=54478264

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201704436A UA122130C2 (uk) 2014-10-27 2015-10-27 Інгібітори бромодомену

Country Status (19)

Country Link
US (1) US10124009B2 (enExample)
EP (1) EP3212654B1 (enExample)
JP (1) JP6715243B2 (enExample)
KR (1) KR20170068597A (enExample)
CN (1) CN107635979A (enExample)
AU (1) AU2015339511B2 (enExample)
BR (1) BR112017008714A2 (enExample)
CA (1) CA2965330A1 (enExample)
CL (1) CL2017001046A1 (enExample)
CO (1) CO2017004898A2 (enExample)
CR (1) CR20170219A (enExample)
EA (1) EA033325B1 (enExample)
IL (1) IL251784A0 (enExample)
MX (1) MX376748B (enExample)
PE (1) PE20171042A1 (enExample)
PH (1) PH12017500745A1 (enExample)
SG (1) SG11201703414VA (enExample)
UA (1) UA122130C2 (enExample)
WO (1) WO2016069578A1 (enExample)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
PL2571503T3 (pl) 2010-05-14 2015-06-30 Dana Farber Cancer Inst Inc Kompozycje i sposoby leczenia nowotworu, choroby zapalnej i innych zaburzeń
WO2013106643A2 (en) 2012-01-12 2013-07-18 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
HRP20221389T1 (hr) 2013-10-18 2023-01-06 Celgene Quanticel Research, Inc. Inhibitori bromodomena
WO2015070020A2 (en) 2013-11-08 2015-05-14 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors
CN106456653A (zh) 2014-02-28 2017-02-22 腾沙治疗公司 高胰岛素血症相关病症的治疗
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
MX376748B (es) 2014-10-27 2025-03-07 Tensha Therapeutics Inc Inhibidores del bromodominio.
KR102616762B1 (ko) 2015-03-18 2023-12-20 아비나스 오퍼레이션스, 인코포레이티드 타겟화된 단백질들의 향상된 분해를 위한 화합물들 및 방법들
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
WO2018075908A1 (en) * 2016-10-21 2018-04-26 University Of Miami Materials and methods for treating ophthalmic inflammation
BR112019015484A2 (pt) 2017-01-31 2020-04-28 Arvinas Operations Inc ligantes de cereblon e compostos bifuncionais compreendendo os mesmos
CN109503618A (zh) * 2017-09-14 2019-03-22 成都海创药业有限公司 一种brd4抑制剂
JP2021512153A (ja) 2018-01-26 2021-05-13 イエール ユニバーシティ タンパク質分解のイミド系モジュレーターおよび使用方法
MX2020010571A (es) 2018-04-13 2021-01-08 Arvinas Operations Inc Ligandos de cereblon y compuestos bifuncionales que los comprenden.
KR20210020889A (ko) 2018-06-13 2021-02-24 디블라이 아게 응축된 트리아제핀 유도체의 제조 및 이의 bet 억제제로서 용도
TWI888359B (zh) * 2018-09-11 2025-07-01 瑞士商赫孚孟拉羅股份公司 噻吩并-三唑并-二氮呯醋酸酯
WO2021127443A1 (en) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
WO2024123929A1 (en) * 2022-12-06 2024-06-13 Bioventures, Llc Development of potent dual hdac/brd4 inhibitors
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
WO2025053994A1 (en) * 2023-09-08 2025-03-13 The Regents Of The University Of California Small molecule enhancers of secreted clusterin (sclu)

Family Cites Families (132)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2951540A (en) 1956-11-05 1960-09-06 Gen Motors Corp Propeller brake
US3709898A (en) 1971-02-09 1973-01-09 Upjohn Co Process for the production of triazolobenzodiazepines and intermediates
US3681343A (en) 1971-05-11 1972-08-01 Upjohn Co 6-phenyl-s-triazolo{8 4,3-a{9 {8 1,4{9 {0 benzodiazepines
US3812259A (en) 1971-08-09 1974-05-21 Upjohn Co Animal feed and process
CH622019A5 (en) 1975-10-23 1981-03-13 Upjohn Co Process for the preparation of aminotriazolobenzodiazepines
FR2329668A1 (fr) 1975-10-27 1977-05-27 Upjohn Co Procede de preparation d'aminotriazolobenzodiazepines
EP0087850A1 (en) 1982-01-04 1983-09-07 The Upjohn Company Benzodiazepines for anti-hypertensive use
DE3435973A1 (de) 1984-10-01 1986-04-10 Boehringer Ingelheim KG, 6507 Ingelheim Diazepine enthaltende pharmazeutische zusammensetzungen mit paf-antagonistischer wirkung
DE3724164A1 (de) 1986-07-25 1988-01-28 Boehringer Ingelheim Kg Neue 1,4-benzodiazepine, ihre herstellung und verwendung
ATE86256T1 (de) 1987-05-28 1993-03-15 Yoshitomi Pharmaceutical Thieno(triazolo)diazepinverbindungen, und medizinische verwendung derselben.
JPH0676326B2 (ja) 1988-05-24 1994-09-28 吉富製薬株式会社 循環器系疾患治療薬
EP0368175A1 (de) 1988-11-06 1990-05-16 Boehringer Ingelheim Kg 3S,7S-3-(Morpholinocarbonyl)-5-(2-chlorphenyl)-7,10-dimethyl-3,4-dihydro-2H,7H-cyclopenta[4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin.
EP0387613A1 (de) 1989-03-03 1990-09-19 Boehringer Ingelheim Kg Neue Thienodiazepine
CA2020806A1 (en) 1989-07-12 1991-01-13 Karl-Heinz Weber Thienodiazepine derivatives
DE4010528A1 (de) 1990-04-02 1991-10-17 Boehringer Ingelheim Kg Praeparativ chromatographisches trennverfahren zur herstellung enantiomerenreiner hetrazepine
US5593988A (en) 1991-10-11 1997-01-14 Yoshitomi Pharmaceutical Industries, Ltd. Therapeutic agent for osteoporosis and diazepine compound
EP0661284A1 (en) 1992-09-18 1995-07-05 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
WO1994022872A1 (fr) 1993-03-30 1994-10-13 Yoshitomi Pharmaceutical Industries, Ltd. Inhibiteur d'adhesion cellulaire et compose a base de thienotriazolodiazepine
CN1149874A (zh) 1994-04-01 1997-05-14 迈克罗赛药品公司 头孢菌素类抗菌素
WO1995032963A1 (en) 1994-06-01 1995-12-07 Yoshitomi Pharmaceutical Industries, Ltd. Thienylazole compound and thienotriazolodiazepine compound
PT801651E (pt) 1995-01-06 2001-12-28 Hoffmann La Roche Hidroximetil-imidazodiazepinas e seus esteres
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
AU725249B2 (en) 1995-09-09 2000-10-12 F. Hoffmann-La Roche Ag Use of a thienotriazolodiazepine to increase apolipoprotein A-I levels
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
IL127516A0 (en) 1996-06-12 1999-10-28 Japan Tobacco Inc A cytokine production inhibitor
US5693641A (en) 1996-08-16 1997-12-02 Berlex Laboratories Inc. Bicyclic pyrimidine derivatives and their use as anti-coagulants
AU716490B2 (en) 1996-09-13 2000-02-24 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compounds and pharmaceutical use thereof
US6444664B1 (en) 1997-04-18 2002-09-03 Nederlandse Organisatie Voor Toegepast - Natuurweten Schappelijk Onderzoek (Tno) Method for controlling the plasma level of lipoproteins to treat alzheimeris disease
JPH11228576A (ja) 1997-12-10 1999-08-24 Japan Tobacco Inc アポトーシス抑制剤
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
FR2779652B1 (fr) 1998-06-15 2001-06-08 Sod Conseils Rech Applic Utilisation de diazepines pour la preparation de medicaments destines a traiter les etats pathologiques ou les maladies dans lesquels un des recepteurs de la somatostatine est implique
KR20000016732A (en) 1998-12-12 2000-03-25 Japan Tobacco Inc Cytokine production inhibitors, triazepine compounds, and intermediates thereof
US6312215B1 (en) 2000-02-15 2001-11-06 United Technologies Corporation Turbine engine windmilling brake
US7589167B2 (en) 2000-02-22 2009-09-15 J. David Gladstone Institutes ZA loops of bromodomains
CA2412776C (en) 2000-06-16 2011-03-15 Mitsubishi Pharma Corporation Compositions controlling release ph range and/or speed
AU2001270297A1 (en) 2000-06-30 2002-01-14 Neurogen Corporation 2-phenylimidazo(1,2-a)pyridine derivatives: a new class of gaba brain receptor ligands
US20060142257A1 (en) 2001-01-19 2006-06-29 Eberhard Nieschlag Male contraceptive formulation comprising norethisterone
US6979682B2 (en) 2001-02-23 2005-12-27 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Platelet-activating factor antagonist inhibition of angiogenesis and tumor growth induced by basic fibroblast
US20030216758A1 (en) 2001-12-28 2003-11-20 Angiotech Pharmaceuticals, Inc. Coated surgical patches
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
US6861422B2 (en) 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
PL378116A1 (pl) 2003-02-27 2006-03-06 Abbott Laboratories Heterocykliczne inhibitory kinazy
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
WO2005002526A2 (en) 2003-07-01 2005-01-13 President And Fellows Of Harvard College Method and compositions for treatment of viral infections
EP1663992A1 (en) 2003-09-18 2006-06-07 Novartis AG 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
EP1528056A1 (en) 2003-10-29 2005-05-04 Academisch Ziekenhuis bij de Universiteit van Amsterdam Deoxynojirimycin analogues and their uses as glucosylceramidase inhibitors
US7759485B2 (en) 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
US20060035903A1 (en) 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
US20060074088A1 (en) 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
CN1759834B (zh) 2004-09-17 2010-06-23 中国医学科学院医药生物技术研究所 黄连素或其与辛伐他汀联合在制备用于预防或治疗与血脂有关疾病或症状的产品中用途
EP1887008B1 (en) * 2005-05-30 2021-04-21 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and a medicinal use thereof
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
MX391408B (es) 2005-11-01 2025-03-21 Impact Biomedicines Inc Inhibidores de biaril meta-pirimidina de cinasas.
PE20071042A1 (es) 2005-11-04 2007-10-12 Wyeth Corp Producto farmaceutico que comprende temsirolimus y malato de sunitinib
CA2634787C (en) 2005-12-23 2014-10-21 Smithkline Beecham Corporation Azaindole inhibitors of aurora kinases
AU2007207053B2 (en) 2006-01-17 2012-05-24 F. Hoffmann-La Roche Ag Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine useful for the treatment of Alzheimer's disease via GABA receptors
DE602007008837D1 (de) 2006-02-14 2010-10-14 Vertex Pharma Als protein-kinase-inhibitoren nutzbare dyhydrodiazepine
US20070218135A1 (en) 2006-03-14 2007-09-20 Glenmark Pharmaceuticals Limited Sustained release matrix pharmaceutical composition
AU2007248112A1 (en) 2006-05-03 2007-11-15 Novartis Ag Use of organic compounds
US7621117B2 (en) 2006-06-19 2009-11-24 Pratt & Whitney Canada Corp. Apparatus and method for controlling engine windmilling
EP2457913B1 (en) 2006-10-19 2017-04-19 Signal Pharmaceuticals, LLC Heteroaryl compounds, compositions thereof, and methods of treatment therewith
US7624617B2 (en) 2006-11-21 2009-12-01 Asml Netherlands B.V. Gas analyzing system, lithographic apparatus and method of improving a sensitivity of a gas analyzing system
WO2008066887A2 (en) 2006-11-30 2008-06-05 Albert Einstein College Of Medicine Of Yeshiva University Small molecule inhibitors of bcl6
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Brd2ブロモドメイン結合剤
WO2008137081A1 (en) 2007-05-02 2008-11-13 The Trustees Of Columbia University In The City Of New York Substituted ( 5, 6 ) -dihydronaphraalenyl compounds as reversible male contraceptives
KR20080107050A (ko) 2007-06-05 2008-12-10 울산대학교 산학협력단 항-cd137 단일클론 항체를 포함하는 만성이식편대숙주 질환의 예방 또는 치료용 약학적 조성물
CA2710118A1 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
CA2710740C (en) 2007-12-28 2016-07-19 Shinji Miyoshi Thienotriazolodiazepine compound as antitumor agent
EP2276747A1 (en) 2008-03-11 2011-01-26 Cellzome Limited Sulfonamides as zap-70 inhibitors
USPP20436P2 (en) 2008-04-10 2009-10-20 Driscoll Strawberry Associates, Inc. Blueberry plant named ‘DrisBlueThree’
WO2010015340A1 (en) 2008-08-06 2010-02-11 Bayer Schering Pharma Aktiengesellschaft Daa-pyridine as peripheral benzodiazepine receptor ligand for diagnostic imaging and pharmaceutical treatment
KR101633742B1 (ko) 2008-10-30 2016-06-27 써코메드 엘엘씨 아포 a에 활성인 티에노트리아졸로디아제핀 유도체
EP2379559B1 (en) 2009-01-06 2017-10-25 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
MY152386A (en) 2009-01-23 2014-09-15 Takeda Pharmaceutical Substituted 6a,7,8,9-tetrahydropyrido[3,2-e] pyrrolo[1,2-a]pyrazin-6(5h)-ones
EP2488548A1 (en) 2009-10-14 2012-08-22 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung A low density lipoprotein-related protein 1 splice variant as cancer marker
ME02360B (me) 2009-11-05 2016-06-20 Glaxosmithkline Llc Inhibitor bromodomena benzodiazepina
BR112012010705A2 (pt) 2009-11-05 2016-03-29 Glaxosmithkline Llc composto, composição farmacêutica, produto farmacêutico combinado, uso de um composto, e, métodos para tratar uma doença ou condição, e para inibir um bromodomínio
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
DE102009046518A1 (de) 2009-11-09 2011-05-12 Robert Bosch Gmbh Speicheranordnung
JP5841548B2 (ja) 2010-02-17 2016-01-13 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ジヒドロプテリジノン、その製造方法及び使用
US9624870B2 (en) 2010-03-26 2017-04-18 Rolls-Royce North American Technologies, Inc. Adaptive fan system for a variable cycle turbofan engine
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
EP2571875A4 (en) * 2010-05-14 2013-10-30 Dana Farber Cancer Inst Inc CONTRACEPTIVE COMPOSITIONS FOR MEN AND METHODS OF USE THEREOF
US20130252331A1 (en) 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
PL2571503T3 (pl) 2010-05-14 2015-06-30 Dana Farber Cancer Inst Inc Kompozycje i sposoby leczenia nowotworu, choroby zapalnej i innych zaburzeń
US9085582B2 (en) 2010-06-22 2015-07-21 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
CN103260637B (zh) 2010-06-25 2016-04-06 夏尔人类遗传性治疗公司 乙酰肝素n-硫酸酯酶cns递送的方法和组合物
US20120014979A1 (en) 2010-07-16 2012-01-19 Alexander Dent Use of bcl6 inhibitors for treating autoimmune diseases
TWI549955B (zh) 2010-08-04 2016-09-21 達納 法柏癌症學院有限公司 治療腫瘤形成、發炎疾病及其他病症之組成物及方法
CN107050456B (zh) 2010-09-28 2022-08-12 加利福尼亚大学董事会 治疗代谢综合征相关疾病的gaba激动剂和治疗或预防i型糖尿病的gaba组合
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012116170A1 (en) 2011-02-23 2012-08-30 Ming-Ming Zhou Inhibitors of bromodomains as modulators of gene expression
AU2012223448B2 (en) 2011-02-28 2017-03-16 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
AU2012290261A1 (en) 2011-07-29 2014-02-20 The Children's Hospital Of Philadelphia Compositions and methods for the treatment of HIV
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
FI20110279A7 (fi) 2011-08-29 2013-03-01 Outotec Oyj Menetelmä metallien talteenottamiseksi niitä sisältävästä materiaalista
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013033420A1 (en) 2011-08-30 2013-03-07 Whitehead Institute For Biomedical Research Methods of downregulating translocated oncogene expression using bromodomain inhibitors
DE102011082013A1 (de) * 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
ES2970401T3 (es) 2012-02-17 2024-05-28 Ansun Biopharma Inc Compuestos y composiciones para uso en un método de tratamiento del virus de parainfluenza
US20150133434A1 (en) 2012-03-28 2015-05-14 The J. David Gladstone Institutes Compositions and Methods for Reactivating Latent Immunodeficiency Virus
WO2013192274A2 (en) 2012-06-19 2013-12-27 The Broad Institute, Inc. Diagnostic and treatment methods in subjects having or at risk of developing resistance to cancer therapy
HK1210434A1 (en) * 2012-09-28 2016-04-22 翁科埃斯克斯有限公司 Pharmaceutical formulation containing thienotriazolodiazepine compounds
US9567301B2 (en) 2012-11-02 2017-02-14 Dana-Farber Cancer Institute, Inc. Pyrrol-1-yl benzoic acid derivatives useful as myc inhibitors
EP2958922A1 (de) 2013-02-22 2015-12-30 Bayer Pharma Aktiengesellschaft Pyrrolo- und pyrazolo-triazolodiazepine als bet-proteininhibitoren zur behandlung von hyper-proliferativen erkrankungen
US20150376196A1 (en) 2013-02-22 2015-12-31 Bayer Pharma Aktiengesellschaft 4-substituted pyrrolo- and pyrazolo-diazepines
AU2014223990A1 (en) * 2013-02-28 2015-09-10 Washington University Methods of treatment of human cytomegalovirus infection and diseases with bromodomain inhibitors
US9714946B2 (en) 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
HK1211471A1 (en) 2013-03-15 2016-05-27 基因泰克公司 Treating th2-mediated diseases by inhibition of bromodomain-comprising proteins brd7 and brd9
JP2016520130A (ja) 2013-05-28 2016-07-11 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 心臓疾患における新規治療戦略としてのbet阻害
WO2015013635A2 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
WO2015018522A1 (en) 2013-08-06 2015-02-12 Oncoethix Sa Bet-bromodomain inhibitor shows synergism with several anti-cancer agents in pre-clinical models of diffuse large b-cell lymphoma (dlbcl)
CN105899212A (zh) 2013-08-06 2016-08-24 翁科埃斯克斯有限公司 利用β溴结构域抑制剂治疗弥漫性大B细胞淋巴瘤(DLBCL)的方法
US20160201063A1 (en) 2013-08-16 2016-07-14 Rana Therapeutics, Inc. Epigenetic regulators of frataxin
WO2015042249A1 (en) 2013-09-19 2015-03-26 Dana-Farber Cancer Institute, Inc. Methods of bh3 profiling
CN105979958A (zh) 2013-10-11 2016-09-28 基因泰克公司 Cbp/ep300布罗莫结构域抑制剂用于癌症免疫疗法的用途
WO2015070020A2 (en) 2013-11-08 2015-05-14 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors
WO2015081284A1 (en) 2013-11-26 2015-06-04 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
KR20160115953A (ko) 2014-01-31 2016-10-06 다나-파버 캔서 인스티튜트 인크. 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도
MX2016009976A (es) 2014-01-31 2016-11-15 Dana Farber Cancer Inst Inc Derivados de diazepam y sus usos.
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
CN106456653A (zh) 2014-02-28 2017-02-22 腾沙治疗公司 高胰岛素血症相关病症的治疗
MX376748B (es) 2014-10-27 2025-03-07 Tensha Therapeutics Inc Inhibidores del bromodominio.
BR112017011780A2 (pt) 2014-12-05 2017-12-26 Dana Farber Cancer Inst Inc inibidor de bromodomínio como composto auxiliar na imunoterapia para câncer
JP2018520124A (ja) 2015-06-26 2018-07-26 テンシャ セラピューティクス,インコーポレイテッド Nut正中線癌の治療
CA2999523A1 (en) 2015-10-02 2017-04-06 Dana-Farber Cancer Institute, Inc. Combination therapy of bromodomain inhibitors and checkpoint blockade

Also Published As

Publication number Publication date
BR112017008714A2 (pt) 2017-12-19
US10124009B2 (en) 2018-11-13
CN107635979A (zh) 2018-01-26
PE20171042A1 (es) 2017-07-19
HK1243415A1 (en) 2018-07-13
IL251784A0 (en) 2017-06-29
AU2015339511B2 (en) 2020-05-14
JP2017531688A (ja) 2017-10-26
CL2017001046A1 (es) 2018-01-26
EP3212654A1 (en) 2017-09-06
PH12017500745A1 (en) 2017-10-30
JP6715243B2 (ja) 2020-07-01
AU2015339511A1 (en) 2017-05-18
EA201790922A1 (ru) 2017-08-31
CO2017004898A2 (es) 2017-10-31
CR20170219A (es) 2017-08-14
US20170333444A1 (en) 2017-11-23
KR20170068597A (ko) 2017-06-19
MX2017005555A (es) 2018-02-09
MX376748B (es) 2025-03-07
EP3212654B1 (en) 2020-04-08
CA2965330A1 (en) 2016-05-06
EA033325B1 (ru) 2019-09-30
WO2016069578A1 (en) 2016-05-06
SG11201703414VA (en) 2017-05-30

Similar Documents

Publication Publication Date Title
UA122130C2 (uk) Інгібітори бромодомену
KR20230079085A (ko) 항종양 화합물 및 그의 제조 방법 및 용도
US7888355B2 (en) Compositions and methods for inhibiting growth and metastasis of melanoma
JP2021107425A (ja) 自己免疫障害および炎症性障害の処置において有用な置換型1,2,3,4−テトラヒドロシクロペンタ[b]インドル−3−イル)酢酸誘導体
RU2722179C2 (ru) Лечение состояний, ассоциированных с гиперинсулинемией
CN111548343B (zh) 一种高活性csf1r抑制剂化合物的制备方法
AU2013308504A1 (en) Tetracycline compounds
WO2019109415A1 (zh) 一种靶向降解hmgcr的化合物及其应用
CN114835596B (zh) Kakeromycin及其衍生物的制造方法
US20190330142A1 (en) Inhibitors of mtor-deptor interactions and methods of use thereof
WO2017195138A1 (en) Small molecule n-(alpha-peroxy) carbazole compounds and methods of use
US20220242815A1 (en) Compositions and methods related to di-substituted bicyclo[2.2.1] heptanamine-containing compounds
WO2013114040A1 (fr) Nouveaux composes et compositions utilises comme anticancereux
AU2017380492A1 (en) Sulfonyl amidine as indoleamine-2,3-dioxygenase inhibitor, and preparation method therefor and use thereof
EP3455208A1 (en) Small molecule n-(alpha-peroxy) indole compounds and methods of use
CN104093703B (zh) Mglu 2/3激动剂
HK1243415B (en) Bromodomain inhibitors
RU2833354C1 (ru) Трициклическое соединение и его фармацевтическое применение
Class et al. Patent application title: INHIBITORS OF MTOR-DEPTOR INTERACTIONS AND METHODS OF USE THEREOF
TW202327576A (zh) 吡咯烷類化合物的鹽、晶型及其製備方法
CN118221642A (zh) 一种磺酰胺衍生物及其在医药上的应用
EA042123B1 (ru) Тетрациклиновые соединения для лечения острого миелоидного лейкоза