JP6022442B2 - 男性用避妊組成物および使用方法 - Google Patents

男性用避妊組成物および使用方法 Download PDF

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Publication number
JP6022442B2
JP6022442B2 JP2013510361A JP2013510361A JP6022442B2 JP 6022442 B2 JP6022442 B2 JP 6022442B2 JP 2013510361 A JP2013510361 A JP 2013510361A JP 2013510361 A JP2013510361 A JP 2013510361A JP 6022442 B2 JP6022442 B2 JP 6022442B2
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compound
pharmaceutical composition
salt
brdt
sperm
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Japanese (ja)
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JP2013528600A (ja
JP2013528600A5 (enExample
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ブラドナー,ジェームズ,エリオット
マツック,マーティン
チー,チュン
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Baylor College of Medicine
Dana Farber Cancer Institute Inc
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Baylor College of Medicine
Dana Farber Cancer Institute Inc
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    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
JP2013510361A 2010-05-14 2011-05-16 男性用避妊組成物および使用方法 Active JP6022442B2 (ja)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US33499110P 2010-05-14 2010-05-14
US61/334,991 2010-05-14
US37074510P 2010-08-04 2010-08-04
US61/370,745 2010-08-04
US37586310P 2010-08-22 2010-08-22
US61/375,863 2010-08-22
US201161467299P 2011-03-24 2011-03-24
US201161467376P 2011-03-24 2011-03-24
US61/467,299 2011-03-24
US61/467,376 2011-03-24
PCT/US2011/036667 WO2011143657A1 (en) 2010-05-14 2011-05-16 Male contraceptive compositions and methods of use

Publications (3)

Publication Number Publication Date
JP2013528600A JP2013528600A (ja) 2013-07-11
JP2013528600A5 JP2013528600A5 (enExample) 2014-07-03
JP6022442B2 true JP6022442B2 (ja) 2016-11-09

Family

ID=44914744

Family Applications (1)

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JP2013510361A Active JP6022442B2 (ja) 2010-05-14 2011-05-16 男性用避妊組成物および使用方法

Country Status (6)

Country Link
US (2) US9301962B2 (enExample)
EP (1) EP2571875A4 (enExample)
JP (1) JP6022442B2 (enExample)
CN (1) CN103180318B (enExample)
CA (1) CA2799381A1 (enExample)
WO (1) WO2011143657A1 (enExample)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130252331A1 (en) * 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
CN103180318B (zh) 2010-05-14 2017-05-10 达那-法伯癌症研究所 雄性避孕组合物以及使用方法
EP2902030B1 (en) 2010-05-14 2016-09-14 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
WO2011143660A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
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
WO2012151512A2 (en) 2011-05-04 2012-11-08 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012174487A2 (en) 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
WO2014159392A1 (en) * 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
CA2901083A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
CA2918910A1 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
CN103694253A (zh) * 2013-11-04 2014-04-02 湖南华腾制药有限公司 一种噻吩并三唑并[4,3-a][1,4]二氮杂卓类化合物的制备方法
EP3066101B1 (en) 2013-11-08 2020-07-29 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein 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
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
KR20160115953A (ko) 2014-01-31 2016-10-06 다나-파버 캔서 인스티튜트 인크. 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도
JP2017504651A (ja) 2014-01-31 2017-02-09 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 ジアゼパン誘導体の使用
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
ES2827253T3 (es) 2014-04-14 2021-05-20 Hayashibara Co Preparación cutánea externa antienvejecimiento
SI3674302T1 (sl) 2014-04-23 2023-07-31 Incyte Holdings Corporation 1h-pirolo(2,3-c)piridin-7(6h)-oni in pirazolo(3,4-c)piridin-7(6h)-oni kot zaviralci proteinov bet
PT3157928T (pt) 2014-06-20 2019-05-30 Constellation Pharmaceuticals Inc Formas cristalinas de 2-((4s)-6-(4-clorofenil)-1-metil-4h-benzo[c] isoxazolo[4,5-e]azepin-4-il)acetamida
CN106793775B (zh) 2014-08-08 2020-06-02 达纳-法伯癌症研究所股份有限公司 二氢碟啶酮衍生物及其用途
JP2017526741A (ja) 2014-08-08 2017-09-14 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 ジアゼパン誘導体およびその使用
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
SG11201703414VA (en) * 2014-10-27 2017-05-30 Tensha Therapeutics Inc Bromodomain inhibitors
US20180163180A1 (en) * 2015-05-01 2018-06-14 The UAB Research Foundation Inc. Method of enhancing somatic cell reprogramming with the acetyllysine reader brd3r
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
HK1256419A1 (zh) * 2015-09-11 2019-09-20 达纳-法伯癌症研究所股份有限公司 乙酰胺噻吩並三唑並二氮雜環庚三烯及其用途
PE20181287A1 (es) 2015-09-11 2018-08-07 Dana Farber Cancer Inst Inc Ciano tienotriazolpirazinas y usos de las mismas
PE20181068A1 (es) * 2015-10-02 2018-07-04 Dana Farber Cancer Inst Inc Terapia de combinacion de inhibidores de bromodominios y bloqueo de puntos de control
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
SG10201913450PA (en) 2015-11-25 2020-03-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
CA3019342A1 (en) 2016-03-30 2017-10-05 Wisconsin Alumni Research Foundation Methods and compositions for modulating frataxin expression
CR20190027A (es) 2016-06-20 2019-05-16 Incyte Corp Formas sólidas cristalinas de un inhibidor de bet
KR20190092429A (ko) * 2016-12-16 2019-08-07 에프. 호프만-라 로슈 아게 다이아제핀 유도체의 제조 방법
US11759533B2 (en) 2017-03-29 2023-09-19 Wisconsin Alumni Research Foundation Methods and compositions for modulating gene expression
JP7515175B2 (ja) 2018-07-31 2024-07-12 ファイメクス株式会社 複素環化合物
WO2020123855A1 (en) 2018-12-12 2020-06-18 University Of Washington Inhibitor compounds for male contraception
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (111)

* 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
US4210644A (en) 1978-02-23 1980-07-01 The Johns Hopkins University Male contraception
US4379454A (en) 1981-02-17 1983-04-12 Alza Corporation Dosage for coadministering drug and percutaneous absorption enhancer
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
US4743249A (en) 1986-02-14 1988-05-10 Ciba-Geigy Corp. Dermal and transdermal patches having a discontinuous pattern adhesive layer
DE3724164A1 (de) 1986-07-25 1988-01-28 Boehringer Ingelheim Kg Neue 1,4-benzodiazepine, ihre herstellung und verwendung
US4906169A (en) 1986-12-29 1990-03-06 Rutgers, The State University Of New Jersey Transdermal estrogen/progestin dosage unit, system and process
US5023084A (en) 1986-12-29 1991-06-11 Rutgers, The State University Of New Jersey Transdermal estrogen/progestin dosage unit, system and process
US4960770A (en) * 1987-05-28 1990-10-02 Yoshitomi Pharmaceutical Industries, Ltd. 2-alkyl thieno(triazolo)diazepine compounds and pharmaceutical uses thereof
US4816540A (en) 1987-06-12 1989-03-28 Yasuhiko Onishi Cationic graft-copolymer
US5422119A (en) 1987-09-24 1995-06-06 Jencap Research Ltd. Transdermal hormone replacement therapy
US5035891A (en) 1987-10-05 1991-07-30 Syntex (U.S.A.) Inc. Controlled release subcutaneous implant
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
US5223409A (en) 1988-09-02 1993-06-29 Protein Engineering Corp. Directed evolution of novel binding proteins
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
US4973468A (en) 1989-03-22 1990-11-27 Cygnus Research Corporation Skin permeation enhancer compositions
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
US5198223A (en) 1990-10-29 1993-03-30 Alza Corporation Transdermal formulations, methods and devices
KR100255493B1 (ko) 1991-10-11 2000-08-01 가마쿠라 아키오 골조송증 치료제
EP0661284A1 (en) * 1992-09-18 1995-07-05 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
EP0692483A1 (en) 1993-03-30 1996-01-17 Yoshitomi Pharmaceutical Industries, Ltd. Cell adhesion inhibitor and thienotriazolodiazepine compound
WO1995032963A1 (en) 1994-06-01 1995-12-07 Yoshitomi Pharmaceutical Industries, Ltd. Thienylazole compound and thienotriazolodiazepine compound
WO1996020941A1 (de) * 1995-01-06 1996-07-11 F. Hoffmann-La Roche Ag Hydroxymethyl-imidazodiazepine und deren ester
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
BR9610390A (pt) 1995-09-09 1999-07-06 Hoffmann La Roche O uso de uma tienotriazolodiazepina para aumentar os níveis da apoliproteína a-i
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
CA2258053A1 (en) 1996-06-12 1997-12-18 Yoshihisa Yamamoto Cytokine production inhibitors, triazepine compounds, and intermediates thereof
US5693641A (en) 1996-08-16 1997-12-02 Berlex Laboratories Inc. Bicyclic pyrimidine derivatives and their use as anti-coagulants
DE69717160T2 (de) 1996-09-13 2003-05-08 Mitsubishi Pharma Corp., Osaka Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen
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
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
WO2002002557A2 (en) 2000-06-30 2002-01-10 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
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
CA2538413A1 (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
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
JP5159305B2 (ja) * 2005-05-30 2013-03-06 田辺三菱製薬株式会社 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
EP1915155A1 (en) 2005-08-03 2008-04-30 Boehringer Ingelheim International GmbH Dihydropteridinones in the treatment of respiratory diseases
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
DK1951684T3 (en) 2005-11-01 2016-10-24 Targegen Inc BIARYLMETAPYRIMIDIN kinase inhibitors
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
KR20080083680A (ko) 2005-12-23 2008-09-18 스미스클라인 비참 코포레이션 오로라 키나제의 아자인돌 억제제
KR101062583B1 (ko) 2006-01-17 2011-09-06 에프. 호프만-라 로슈 아게 Gaba 수용체에 의해 알츠하이머병의 치료에 유용한아릴-아이속사졸-4-일-이미다조[1,2-a]피리딘
KR20080095902A (ko) 2006-02-14 2008-10-29 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로서 유용한 디하이드로디아제핀
US20070218135A1 (en) 2006-03-14 2007-09-20 Glenmark Pharmaceuticals Limited Sustained release matrix pharmaceutical composition
DE602007008553D1 (de) 2006-05-03 2010-09-30 Novartis Ag Verwendung von organischen verbindungen
MX2009004077A (es) 2006-10-19 2009-05-05 Signal Pharm Llc Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas.
US8338464B2 (en) 2006-11-30 2012-12-25 Albert Einstein College Of Medicine Of Yeshiva University Small molecule inhibitors of BCL6
PT2114873E (pt) 2006-12-26 2013-05-06 Lantheus Medical Imaging Inc Ligandos para imagiologia de inervação cardíaca
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
US7935964B2 (en) 2007-06-19 2011-05-03 Samsung Electronics Co., Ltd. Oxide semiconductors and thin film transistors comprising the same
WO2009080638A2 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
KR101600634B1 (ko) 2007-12-28 2016-03-07 미쓰비시 타나베 파마 코퍼레이션 항암제
EP2276747A1 (en) 2008-03-11 2011-01-26 Cellzome Limited Sulfonamides as zap-70 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
AU2009309691B2 (en) * 2008-10-30 2015-04-02 Circomed Llc Thienotriazolodiazepine derivatives active on apo A
EP2379559B1 (en) 2009-01-06 2017-10-25 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
CN102341394B (zh) 2009-01-23 2015-04-15 武田药品工业株式会社 聚(adp-核糖)聚合酶(parp)抑制剂
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ES2652304T3 (es) 2009-11-05 2018-02-01 Glaxosmithkline Llc Compuesto de benzodiacepina novedoso
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US9102677B2 (en) 2009-11-05 2015-08-11 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
WO2011101369A1 (en) 2010-02-17 2011-08-25 Boehringer Ingelheim International Gmbh Dihydropteridinones, method for production and use thereof
US20130252331A1 (en) 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
CN103180318B (zh) 2010-05-14 2017-05-10 达那-法伯癌症研究所 雄性避孕组合物以及使用方法
WO2011143660A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
EP2902030B1 (en) 2010-05-14 2016-09-14 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
JP5844358B2 (ja) 2010-06-22 2016-01-13 グラクソスミスクライン エルエルシー ベンゾトリアゾロジアゼピン化合物を含むブロモドメイン阻害剤
US20120014979A1 (en) 2010-07-16 2012-01-19 Alexander Dent Use of bcl6 inhibitors for treating autoimmune diseases
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
AU2012220620A1 (en) 2011-02-23 2013-10-03 Icahn School Of Medicine At Mount Sinai Inhibitors of bromodomains as modulators of gene expression
EP3323820B1 (en) 2011-02-28 2023-05-10 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
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
AU2013221230A1 (en) 2012-02-17 2014-10-02 Ansun Biopharma, Inc. Methods, compounds and compositions for treatment of parainfluenza virus in immunocompromised patients
US20150133434A1 (en) 2012-03-28 2015-05-14 The J. David Gladstone Institutes Compositions and Methods for Reactivating Latent Immunodeficiency Virus
EP2917203B1 (en) 2012-11-02 2019-04-03 Dana-Farber Cancer Institute, Inc. Method for identifying myc inhibitors
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
CA2918910A1 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
US10739333B2 (en) 2013-09-19 2020-08-11 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
JP2017504650A (ja) 2014-01-31 2017-02-09 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 ジアゼパン誘導体およびその使用
JP2017504651A (ja) 2014-01-31 2017-02-09 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 ジアゼパン誘導体の使用
KR20160115953A (ko) 2014-01-31 2016-10-06 다나-파버 캔서 인스티튜트 인크. 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도

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