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MX2017001756A - Derivados de diazepano y sus usos. - Google Patents

Derivados de diazepano y sus usos.

Info

Publication number
MX2017001756A
MX2017001756A MX2017001756A MX2017001756A MX2017001756A MX 2017001756 A MX2017001756 A MX 2017001756A MX 2017001756 A MX2017001756 A MX 2017001756A MX 2017001756 A MX2017001756 A MX 2017001756A MX 2017001756 A MX2017001756 A MX 2017001756A
Authority
MX
Mexico
Prior art keywords
diseases
compounds
bromodomain
bromodomains
containing proteins
Prior art date
Application number
MX2017001756A
Other languages
English (en)
Inventor
Buckley Dennis
E Bradner James
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 MX2017001756A publication Critical patent/MX2017001756A/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/16Central respiratory analeptics
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • 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
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes
    • 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
    • A61P5/00Drugs for disorders of the endocrine 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Biotechnology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Toxicology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Emergency Medicine (AREA)
  • AIDS & HIV (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)

Abstract

La presente descripción proporciona compuestos de fórmula (I), y composiciones farmacéuticas de los mismos; se ha descubierto que los compuestos de fórmula (I) se unen a bromodromanos y/o proteínas que contienen bromodominio (por ejemplo, proteínas bromo y extra terminales (BET)); también se proporcionan métodos, usos y kits de los compuestos y composiciones farmacéuticas para inhibir la actividad (por ejemplo, actividad incrementada) de bromodománidos y/o proteínas que contienen bromodominio y para tratar y/o prevenir en un sujeto enfermedades asociadas con bromodominios o proteínas que contienen bromodominios (por ejemplo, enfermedades proliferativas, enfermedades cardiovasculares, infecciones virales, enfermedades fibróticas, enfermedades neurológicas, enfermedades metabólicas, enfermedades endocrinas y envenenamiento por radiación); los compuestos, las composiciones farmacéuticas y los kits también son útiles para la anticoncepción para hombres; (ver Fórmula).
MX2017001756A 2014-08-08 2015-08-07 Derivados de diazepano y sus usos. MX2017001756A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462034949P 2014-08-08 2014-08-08
PCT/US2015/044180 WO2016022902A1 (en) 2014-08-08 2015-08-07 Diazepane derivatives and uses thereof

Publications (1)

Publication Number Publication Date
MX2017001756A true MX2017001756A (es) 2017-05-30

Family

ID=55264621

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2017001756A MX2017001756A (es) 2014-08-08 2015-08-07 Derivados de diazepano y sus usos.

Country Status (10)

Country Link
US (1) US10308653B2 (es)
EP (1) EP3177626A4 (es)
JP (1) JP2017526741A (es)
KR (1) KR20170032473A (es)
CN (1) CN106715437A (es)
BR (1) BR112017002369A2 (es)
CA (1) CA2955074A1 (es)
MX (1) MX2017001756A (es)
RU (1) RU2017104897A (es)
WO (1) WO2016022902A1 (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016531113A (ja) 2013-07-25 2016-10-06 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 転写因子の阻害剤およびその使用
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
MX2016009974A (es) 2014-01-31 2016-10-31 Dana Farber Cancer Inst Inc Derivados de diaminopirimidina bencensulfona y sus usos.
WO2015164213A1 (en) * 2014-04-23 2015-10-29 The Research Foundation For The State University Of New York A rapid and efficient bioorthogonal ligation reaction and boron-containing heterocycles useful in conjuction therewith
EP3177626A4 (en) 2014-08-08 2017-12-27 Dana Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
KR20170032474A (ko) 2014-08-08 2017-03-22 다나-파버 캔서 인스티튜트 인크. 디히드로프테리디논 유도체 및 그의 용도
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
CA2996977A1 (en) 2015-09-11 2017-03-16 Dana-Farber Cancer Institute, Inc. Acetamide thienotriazolodiazepines and uses thereof
KR20180049058A (ko) 2015-09-11 2018-05-10 다나-파버 캔서 인스티튜트 인크. 시아노 티에노트리아졸로디아제핀 및 그의 용도
SG10201913450PA (en) 2015-11-25 2020-03-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
US11028089B2 (en) * 2016-10-18 2021-06-08 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating DCLK1/2-mediated disorders
EP3645530A2 (en) 2017-06-30 2020-05-06 Massachusetts Institute of Technology Branched multi-functional macromonomers and related polymers and uses thereof
US12414997B2 (en) 2018-04-13 2025-09-16 Massachusetts Institute Of Technology Brush prodrugs and uses thereof
WO2021076821A2 (en) 2019-10-16 2021-04-22 Massachusetts Institute Of Technology Brush prodrugs and uses thereof
DE102020110573A1 (de) * 2020-04-17 2021-10-21 Eberhard Karls Universität Tübingen Medizinische Fakultät Wirkstoffe gegen Coronavirus-Infektionen und dadurch verursachte Erkrankungen
CN117603212B (zh) * 2023-10-20 2025-12-12 中国人民解放军海军军医大学 一种dclk1荧光探针及其应用
CN118908950B (zh) * 2024-07-19 2025-09-19 慈溪市人民医院医疗健康集团(慈溪市人民医院) 一种用于治疗心血管疾病的药物及其制备方法

Family Cites Families (125)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
DE3878833T2 (de) 1987-05-28 1993-06-09 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
EP0407955A1 (de) 1989-07-12 1991-01-16 Boehringer Ingelheim Kg Neue Hetrazepine mit PAF-antagonistischer Wirkung, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
DE4010528A1 (de) 1990-04-02 1991-10-17 Boehringer Ingelheim Kg Praeparativ chromatographisches trennverfahren zur herstellung enantiomerenreiner hetrazepine
EP0638560A4 (en) 1991-10-11 1995-03-29 Yoshitomi Pharmaceutical MEDICINE FOR OSTEOPOROSIS AND DIAZEPINE COMPOUND *.
WO1994006802A1 (fr) 1992-09-18 1994-03-31 Yoshitomi Pharmaceutical Industries, Ltd. Compose de thienodiazepine et son utilisation medicinale
WO1994022872A1 (fr) 1993-03-30 1994-10-13 Yoshitomi Pharmaceutical Industries, Ltd. Inhibiteur d'adhesion cellulaire et compose a base de thienotriazolodiazepine
WO1995032963A1 (en) 1994-06-01 1995-12-07 Yoshitomi Pharmaceutical Industries, Ltd. Thienylazole compound and thienotriazolodiazepine compound
CA2209424A1 (en) 1995-01-06 1996-07-11 F. Hoffmann-La Roche Ag Hydroxymethylimidazodiazepines and their esters
AU725249B2 (en) 1995-09-09 2000-10-12 F. Hoffmann-La Roche Ag Use of a thienotriazolodiazepine to increase apolipoprotein A-I levels
AU3106197A (en) 1996-06-12 1998-01-07 Japan Tobacco Inc. Cytokine production inhibitors, triazepine compounds, and intermediates there of
US5693641A (en) 1996-08-16 1997-12-02 Berlex Laboratories Inc. Bicyclic pyrimidine derivatives and their use as anti-coagulants
EA001732B1 (ru) 1996-09-13 2001-08-27 Велфайд Корпорейшн Тиенотриазолодиазепиновые соединения и лекарственное средство
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
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
US7589167B2 (en) 2000-02-22 2009-09-15 J. David Gladstone Institutes ZA loops of bromodomains
WO2001095912A1 (fr) 2000-06-16 2001-12-20 Mitsubishi Pharma Corporation Compositions permettant de reguler la plage et/ou la vitesse de liberation du ph
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
CA2458699C (en) 2001-09-04 2010-10-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Novel dihydropteridinones, method for producing the same and the use thereof as medicaments
US6806272B2 (en) 2001-09-04 2004-10-19 Boehringer Ingelheim Pharma Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
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
RS52386B (sr) 2003-02-26 2013-02-28 Boehringer Ingelheim Pharma Gmbh & Co.Kg. Dihidropteridinoni, postupak za njihovo pripremanje i njihova primena kao leka
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
WO2005026130A1 (en) 2003-09-18 2005-03-24 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
US7728134B2 (en) 2004-08-14 2010-06-01 Boehringer Ingelheim International Gmbh Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament
US20060074088A1 (en) 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
US7759485B2 (en) 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US20060035903A1 (en) 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
JP2008510771A (ja) 2004-08-27 2008-04-10 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、その製造方法および医薬薬剤としてのその使用
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
WO2006129623A1 (ja) 2005-05-30 2006-12-07 Mitsubishi Tanabe Pharma Corporation チエノトリアゾロジアゼピン化合物及びその医薬としての用途
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
SG137989A1 (en) 2005-06-08 2008-01-28 Rigel Pharmaceuticals Inc Compositions and methods for inhibition of the JAK pathway
WO2007014838A1 (en) 2005-08-03 2007-02-08 Boehringer Ingelheim International Gmbh Dihydropteridinones in the treatment of respiratory diseases
HUE028987T2 (en) 2005-11-01 2017-01-30 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
ES2408318T3 (es) 2005-12-23 2013-06-20 Glaxosmithkline Llc Inhibidores de azaindol de las cinasas Aurora
BRPI0706560A2 (pt) 2006-01-17 2011-03-29 Hoffmann La Roche derivados de aril-isoxazol-4-il-imidazo [1,2-a] piridina úteis para o tratamento de doença de alzheimer por intermédio de receptores gaba
ES2351367T3 (es) 2006-02-14 2011-02-03 Vertex Pharmaceuticals Incorporated Dihidrodiazepinas útiles como inhibidores de proteína quinasas.
RU2475488C2 (ru) 2006-02-14 2013-02-20 Вертекс Фармасьютикалз Инкорпорейтед Дигидродиазепины, которые можно использовать в качестве ингибиторов протеинкиназ
US20070218135A1 (en) 2006-03-14 2007-09-20 Glenmark Pharmaceuticals Limited Sustained release matrix pharmaceutical composition
MX2008014008A (es) 2006-05-03 2009-03-25 Novartis Ag Uso de compuestos organicos.
WO2008009909A1 (en) 2006-07-17 2008-01-24 Astrazeneca Ab Pteridimones as modulators of polo-like kinase
RU2478635C2 (ru) 2006-10-19 2013-04-10 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Гетероарильные соединения, содержащие их композиции и способы лечения с применением этих соединений
US8338464B2 (en) 2006-11-30 2012-12-25 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
EP2474523B1 (en) 2006-12-26 2020-04-08 Lantheus Medical Imaging, Inc. Ligands for imaging cardiac innervation
JP5087640B2 (ja) 2007-03-22 2012-12-05 武田薬品工業株式会社 Plk1阻害剤として有用な置換ピリミドジアゼピン
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
AU2008287339A1 (en) 2007-08-15 2009-02-19 Vertex Pharmaceuticals Incorporated 4-(9-(3, 3-difluorocyclopentyl) -5, 7, 7-trimethyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido [4, 5-b][1, 4] diazepin-2-ylamino)-3-methoxybenzamide Derivatives as Inhibitors of the Human Protein Kinases PLK1 to PLK4 for the Treatment of Proliferative Diseases
ES2488966T3 (es) 2007-09-25 2014-09-01 Takeda Pharmaceutical Company Limited Inhibidores de cinasa de tipo Polo
EP2205603B1 (en) 2007-09-28 2014-01-15 Cyclacel Limited Pyrimidine derivatives as protein kinase inhibitors
WO2009067547A1 (en) 2007-11-19 2009-05-28 Takeda Pharmaceutical Company Limited Polo-like kinase inhibitors
CA2710118A1 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
JP5478262B2 (ja) 2007-12-28 2014-04-23 田辺三菱製薬株式会社 抗癌剤
DK2283024T3 (da) 2008-03-10 2013-08-05 Janssen Pharmaceutica Nv 4-aryl-2-anilinpyrimidiner som PLK-kinaseinhibitorer
WO2009112490A1 (en) 2008-03-11 2009-09-17 Cellzome Limited Sulfonamides as zap-70 inhibitors
EP2112152A1 (en) 2008-04-22 2009-10-28 GPC Biotech AG Dihydropteridinones as Plk Inhibitors
WO2009153197A1 (en) 2008-06-18 2009-12-23 F. Hoffmann-La Roche Ag Halo-substituted pyrimidodiazepines as plkl inhibitors
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
EA018620B1 (ru) 2008-10-30 2013-09-30 Сёркомед Ллк ПРОИЗВОДНЫЕ ТИЕНОТРИАЗОЛОДИАЗЕПИНА, АКТИВНЫЕ В ОТНОШЕНИИ Apo A1
WO2010080712A2 (en) 2009-01-06 2010-07-15 Dana Farber Cancer Institute Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
EP2389379A1 (en) 2009-01-23 2011-11-30 Takeda Pharmaceutical Company Limited Poly (ADP-Ribose) Polymerase (PARP) Inhibitors
CN102020643A (zh) 2009-09-22 2011-04-20 上海恒瑞医药有限公司 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用
WO2011036566A1 (en) 2009-09-25 2011-03-31 Vertex Pharmaceuticals Incorporated Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
KR101424989B1 (ko) 2009-11-05 2014-07-31 글락소스미스클라인 엘엘씨 벤조디아제핀 브로모도메인 억제제
ES2564318T3 (es) 2009-11-05 2016-03-21 Glaxosmithkline Llc Inhibidor de bromodominio de benzodiazepina
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US20120329803A1 (en) * 2010-02-17 2012-12-27 Boehringer Ingelheim International Gmbh Dihydropteridinones, method for production and use thereof
CA2799420C (en) 2010-05-14 2018-10-02 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating neoplasia, inflammatory disease and other disorders
US9301962B2 (en) 2010-05-14 2016-04-05 Baylor College Of Medicine Male contraceptive compositions and methods of use
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
CA2799373A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
WO2011161031A1 (en) 2010-06-22 2011-12-29 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
US20120014979A1 (en) 2010-07-16 2012-01-19 Alexander Dent Use of bcl6 inhibitors for treating autoimmune diseases
US9358233B2 (en) 2010-11-29 2016-06-07 Boehringer Ingelheim International Gmbh Method for treating acute myeloid leukemia
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
CN103547152A (zh) 2011-02-23 2014-01-29 西奈山伊坎医学院 溴结构域蛋白的抑制剂作为基因表达的调节剂
EP2681216B1 (en) 2011-02-28 2017-09-27 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
CN103619873A (zh) 2011-03-07 2014-03-05 泰莱托恩基金会 Tfeb变体及其应用
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
WO2013123521A1 (en) 2012-02-17 2013-08-22 Nexbio, Inc. Methods, Compounds and Compositions for Treatment of Parainfluenza Virus in Immunocompromised Patients
EP2830629A4 (en) 2012-03-28 2016-01-20 Icahn School Of Medicine Mount Sinai COMPOSITIONS AND METHOD FOR THE REACTIVATION OF LATENT IMMUNE FIZIENZVIRUS
EP2917203B1 (en) * 2012-11-02 2019-04-03 Dana-Farber Cancer Institute, Inc. Method for identifying myc inhibitors
CA2895404A1 (en) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydropyridopyrazinones
AR095266A1 (es) 2013-03-12 2015-09-30 Abbvie Inc Inhibidores de bromodominios tetraciclicos
US9714946B2 (en) 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
JP2016531113A (ja) 2013-07-25 2016-10-06 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 転写因子の阻害剤およびその使用
WO2015042249A1 (en) 2013-09-19 2015-03-26 Dana-Farber Cancer Institute, Inc. Methods of bh3 profiling
WO2015081284A1 (en) 2013-11-26 2015-06-04 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
MX2016009974A (es) 2014-01-31 2016-10-31 Dana Farber Cancer Inst Inc Derivados de diaminopirimidina bencensulfona y sus usos.
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
RU2016134941A (ru) 2014-01-31 2018-03-01 Дана-Фарбер Кансер Институт, Инк. Производные диазепана и их применения
CA2936871A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
EP3177626A4 (en) 2014-08-08 2017-12-27 Dana Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
KR20170032474A (ko) 2014-08-08 2017-03-22 다나-파버 캔서 인스티튜트 인크. 디히드로프테리디논 유도체 및 그의 용도
CA2996977A1 (en) 2015-09-11 2017-03-16 Dana-Farber Cancer Institute, Inc. Acetamide thienotriazolodiazepines and uses thereof

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