ZA201408720B - Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof - Google Patents

Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof

Info

Publication number
ZA201408720B
ZA201408720B ZA2014/08720A ZA201408720A ZA201408720B ZA 201408720 B ZA201408720 B ZA 201408720B ZA 2014/08720 A ZA2014/08720 A ZA 2014/08720A ZA 201408720 A ZA201408720 A ZA 201408720A ZA 201408720 B ZA201408720 B ZA 201408720B
Authority
ZA
South Africa
Prior art keywords
benzo
bromodomain inhibitors
isoxazoloazepine
isoxazoloazepine bromodomain
inhibitors
Prior art date
Application number
ZA2014/08720A
Other languages
English (en)
Inventor
Rishi G Vaswani
Michael Charles Hewitt
Victor S Gehling
Brian K Albrecht
Original Assignee
Constellation Pharmaceuticals 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 Constellation Pharmaceuticals Inc filed Critical Constellation Pharmaceuticals Inc
Publication of ZA201408720B publication Critical patent/ZA201408720B/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/424Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
ZA2014/08720A 2012-06-06 2014-11-26 Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof ZA201408720B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261656205P 2012-06-06 2012-06-06
PCT/US2013/044444 WO2013184876A1 (en) 2012-06-06 2013-06-06 Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
ZA201408720B true ZA201408720B (en) 2018-05-30

Family

ID=48626693

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2014/08720A ZA201408720B (en) 2012-06-06 2014-11-26 Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof

Country Status (19)

Country Link
US (2) US9493483B2 (enExample)
EP (1) EP2859000B1 (enExample)
JP (1) JP6154004B2 (enExample)
KR (1) KR20150023562A (enExample)
CN (1) CN104428304B (enExample)
AR (1) AR091285A1 (enExample)
AU (1) AU2013271569B2 (enExample)
BR (1) BR112014030165A2 (enExample)
CA (1) CA2874774C (enExample)
EA (1) EA026894B1 (enExample)
ES (1) ES2632774T3 (enExample)
IL (1) IL235844A (enExample)
IN (1) IN2014DN10386A (enExample)
MX (1) MX360598B (enExample)
NZ (1) NZ702458A (enExample)
SG (1) SG11201407900WA (enExample)
TW (1) TWI602820B (enExample)
WO (1) WO2013184876A1 (enExample)
ZA (1) ZA201408720B (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR084070A1 (es) * 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
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
SG11201505979UA (en) 2013-02-19 2015-09-29 Bayer Pharma AG Bicyclo 2,3-benzodiazepines and spirocyclically substituted 2,3-benzodiazepines
CN105189514A (zh) 2013-02-22 2015-12-23 拜耳医药股份有限公司 作为bet-蛋白抑制剂用于治疗过度增殖性疾病的吡咯并-和吡唑并-三唑并二氮杂卓
JP2016513118A (ja) 2013-02-22 2016-05-12 バイエル ファーマ アクチエンゲゼルシャフト 4−置換されたピロロ−およびピラゾロジアゼピン類
EA038494B1 (ru) 2013-03-15 2021-09-07 Инсайт Холдингс Корпорейшн Трициклические гетероциклы как ингибиторы белков бэт
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EP3125896A2 (en) * 2014-04-04 2017-02-08 Constellation Pharmaceuticals, Inc. EXPRESSION LEVELS OF BCL-xL, BCL2, BCL-w, AND BAD AND CANCER THERAPIES
HRP20200564T1 (hr) 2014-04-23 2020-06-26 Incyte Corporation 1h-pirolo[2,3-c]piridin-7(6h)-oni i pirazolo[3,4-c]piridin-7(6h)-oni kao inhibitori bet proteina
WO2015195863A1 (en) * 2014-06-20 2015-12-23 Constellation Pharmaceuticals, Inc. Hydrated 2-((4s)-6-(4-chlorophenyl)-1 -methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
BR112017028178A2 (pt) 2015-06-26 2018-08-28 Tensha Therapeutics Inc tratamento de carcinoma de linha média nut
DK3347356T3 (da) 2015-09-09 2021-04-26 Jubilant Biosys Ltd Tricyclic forbundet pyridin-2-one-derivater og deres anvendelse som brd4-hæmmere
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
WO2017114843A1 (en) 2015-12-29 2017-07-06 INSERM (Institut National de la Santé et de la Recherche Médicale) Xanthine derivative inhibitors of bet proteins
KR102460046B1 (ko) 2016-06-20 2022-10-31 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
CN109963570A (zh) 2017-01-21 2019-07-02 宁波知明生物科技有限公司 芍药苷-6’-o-苯磺酸酯在治疗干燥综合征的应用
CA3081753A1 (en) 2017-11-06 2019-05-09 Centre National De La Recherche Scientifique Xanthine derivatives and uses thereof as inhibitors of bromodomains of bet proteins
KR102026243B1 (ko) * 2018-01-19 2019-09-27 연세대학교 산학협력단 백혈병 치료용 약학적 조성물
SG11202009088VA (en) 2018-03-30 2020-10-29 Kyowa Kirin Co Ltd Compound with anticancer activity
CN111518045A (zh) * 2019-02-02 2020-08-11 博诺康源(北京)药业科技有限公司 一种具有苯并七元环结构的化合物、其制备方法及用途
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (144)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3523939A (en) 1967-07-03 1970-08-11 Hoffmann La Roche 5-(2,6-disubstituted phenyl)-1,4-benzodiazepines and methods for their preparation
CH498846A (de) 1967-08-09 1970-11-15 Hoffmann La Roche Verfahren zur Herstellung von Benzodiazepin-Derivaten
US3781289A (en) 1971-02-09 1973-12-25 Upjohn Co 7-chloro-1-methyl-5-phenyl-s-triazolo (4,3-a)quinolines
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
US3903103A (en) 1971-09-15 1975-09-02 Upjohn Co 4-Amino-s-triazolo-{8 4,3-a{9 {8 1,4{9 benzodiazepine
DE2242918A1 (de) 1971-09-15 1973-03-22 Upjohn Co Neue 4-amino-s-triazolo eckige klammer auf 4,3-a eckige klammer zu eckige klammer auf 1,4 eckige klammer zu benzodiazepine
US3886141A (en) 1971-10-07 1975-05-27 Hoffmann La Roche Preparation of 5-pyridyl benzodiazepine utilizing hexamethylenetetramine
BE795790A (fr) 1972-02-22 1973-08-22 Upjohn Co Dibenzo-triazolo-azepine
US4155904A (en) 1973-02-08 1979-05-22 Schering Corporation Process for the preparation of 1,4-benzo-diazepines and 1,4-benzodiazepinones
FR2220257A1 (en) 1973-03-09 1974-10-04 Lipha 5,6-Dihydro-(4H)-s-triazolo-(4,3-a) (1,5)benzodiazepines - as antiinflam-matory and analgesic agents without tranquillising effects
IE38931B1 (en) 1973-03-09 1978-07-05 Lipha Triazolobenzodiazepines
US3966736A (en) 1975-04-07 1976-06-29 The Upjohn Company 2,9-Dihydro-3H-pyrido[3,2-c]-s-triazolo[4,3-a][1,5]-benzodiazepin-3-ones
AT350056B (de) 1975-11-04 1979-05-10 Degussa Verfahren zur herstellung von neuen pyrido- (2,3-f)-(1,4)-diazepinen, deren optischen isomeren und salzen
DE2640599A1 (de) 1976-09-09 1978-03-16 Scherico Ltd Verfahren zur herstellung von 1,4- benzodiazepinen
CA1152066A (en) 1980-02-08 1983-08-16 Hoffmann-La Roche Limited Benzodiazepine derivatives
CA1157855A (en) 1980-07-31 1983-11-29 Albert E. Fischli Benzodiazepine derivatives
CA1163266A (en) 1980-07-31 1984-03-06 Albert E. Fischli Benzodiazepine derivatives
US4455307A (en) 1982-01-04 1984-06-19 The Upjohn Company Antihypertensive use of triazolobenzodiazepines
US4663321A (en) 1984-06-26 1987-05-05 Merck & Co., Inc. Triazolobenzodiazepines and pharmaceutical use
US5004741A (en) 1984-06-26 1991-04-02 Merck & Co., Inc. Methods of antagonizing CCK or gastrin with benzodiazepine analogs
US4820834A (en) 1984-06-26 1989-04-11 Merck & Co., Inc. Benzodiazepine analogs
EP0315698B1 (en) 1987-05-28 1993-03-03 Yoshitomi Pharmaceutical Industries, Ltd. Thieno(triazolo)diazepine compounds and medicinal application of the same
US4959361A (en) 1987-12-18 1990-09-25 Hoffmann-La Roche Inc. Triazolo(4,3-A)(1,4)benzodiazepines and thieno (3,2-F)(1,2,4)triazolo(4,3-A)(1,4)diazepine compounds which have useful activity as platelet activating factor (PAF) antagonists
MC1999A1 (fr) 1987-12-18 1990-01-26 Hoffmann La Roche Composes tricycliques
US4992437A (en) 1987-12-22 1991-02-12 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compounds and their pharmaceutical use
CA1324863C (en) 1988-01-30 1993-11-30 Minoru Moriwaki Thienotriazolodiazepine compounds and pharmaceutical uses thereof
CA1322367C (en) 1988-05-17 1993-09-21 Yoshitomi Pharmaceutical Industries Ltd. Thienotriazolodiazepine compounds and pharmaceutical uses thereof
FI95708C (fi) 1988-10-31 1996-03-11 Eisai Co Ltd Analogiamenetelmä 1,4-diatsepiinijohdannaisen ja sen farmaseuttisesti sopivan suolan valmistamiseksi
US5382579A (en) 1988-10-31 1995-01-17 Eisai Co., Ltd. Triazolo-1,4-diazepine derivatives and their use in pharmaceuticals
US5221671A (en) 1988-10-31 1993-06-22 Eisai Co., Ltd. Triazolo-1,4-diazepine derivatives and their use in pharmaceuticals
DE3936828A1 (de) 1988-11-06 1990-05-10 Boehringer Ingelheim Kg Neue hetrazepine
DE4006471A1 (de) 1989-03-03 1990-09-06 Boehringer Ingelheim Kg Neue thienodiazepine
CA2020806A1 (en) 1989-07-12 1991-01-13 Karl-Heinz Weber Thienodiazepine derivatives
EP0727215A3 (en) 1989-08-04 1996-11-06 Merck Sharp & Dohme Central cholecystokinin antagonists for the treatment of psychiatric disorders
US5175159A (en) 1989-10-05 1992-12-29 Merck & Co., Inc. 3-substituted-1,4-benzodiazepines as oxytocin antagonists
IE904560A1 (en) 1989-12-18 1991-06-19 Merck & Co Inc New benzodiazepine analogs
IL96613A0 (en) 1989-12-18 1991-09-16 Merck & Co Inc Pharmaceutical compositions containing benzodiazepine analogs
JP2959591B2 (ja) 1990-05-23 1999-10-06 吉富製薬株式会社 チエノトリアゾロジアゼピン化合物
WO1994006801A1 (fr) 1990-05-23 1994-03-31 Yoshitomi Pharmaceutical Industries, Ltd. Compose de thienodiazepine et son utilisation comme medicament
DE4027470A1 (de) 1990-08-30 1992-03-05 Boehringer Ingelheim Kg Neue hetrazepinoide amide
JP2959598B2 (ja) 1990-10-12 1999-10-06 吉富製薬株式会社 光学活性なチエノトリアゾロジアゼピン化合物
US5206234A (en) 1990-10-22 1993-04-27 Merck & Co., Inc. Benzolactam analogs as antagonists of cck
CA2056809A1 (en) 1990-12-07 1992-06-08 Mark G. Bock Benzodiazepine analogs
DE4101146A1 (de) 1991-01-16 1992-07-23 Boehringer Ingelheim Kg Neue in 6-position substituierte diazepine, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
DE4107521A1 (de) 1991-03-08 1992-09-10 Boehringer Ingelheim Kg Neue acylaminosubstituierte hetrazepine
US5683998A (en) 1991-04-23 1997-11-04 Toray Industries, Inc. Tricyclic triazolo derivatives, processes for producing the same and the uses of the same
US5185331A (en) 1991-05-14 1993-02-09 Merck & Co., Inc. Triazolobenzodiazepines
CA2071092A1 (en) 1991-06-14 1992-12-15 Roger M. Freidinger 1,4-benzodiazepines with 5-membered heterocyclic rings
GB9117852D0 (en) 1991-08-19 1991-10-09 Merck Sharp & Dohme Therapeutic agents
US5153191A (en) 1991-08-20 1992-10-06 Warner-Lambert Company Cholecystokinin antagonists useful for treating depression
DE4128581A1 (de) 1991-08-28 1993-03-04 Boehringer Ingelheim Kg Verwendung von paf-antagonisten hetrazepinoider struktur zur behandlung der allergischen rhinitis
DE69131907T2 (de) 1991-09-30 2000-06-15 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepinverbindungen und ihre verwendung
WO1993007129A1 (fr) 1991-10-11 1993-04-15 Yoshitomi Pharmaceutical Industries, Ltd. Medicament utilise pour traiter l'osteoporose et compose de diazepine
ES2143993T3 (es) 1991-12-11 2000-06-01 Yoshitomi Pharmaceutical Farmaco para tratar una enfermedad autoinmune.
EP0617621A4 (en) 1991-12-20 1995-04-05 Merck Sharp & Dohme CENTRAL CHOLECYSTOKININE ANTAGONISTS WITH PHARMACEUTICAL EFFECTIVENESS.
DE4200610A1 (de) 1992-01-13 1993-07-15 Boehringer Ingelheim Kg Verwendung von paf-antagonisten zur behandlung der dysmenorrhea
CA2130196A1 (en) 1992-03-24 1993-09-30 Jose Luis Castro Pineiro Benzodiazepine derivatives
DE4219659A1 (de) 1992-06-16 1993-12-23 Boehringer Ingelheim Kg Die Verwendung von PAF-Antagonisten in Kombination mit Anticholinergika
WO1994006802A1 (fr) 1992-09-18 1994-03-31 Yoshitomi Pharmaceutical Industries, Ltd. Compose de thienodiazepine et son utilisation medicinale
JP3223290B2 (ja) 1992-11-10 2001-10-29 日本電信電話株式会社 マイクロ回転体およびその製造方法
US5302590A (en) 1992-12-18 1994-04-12 Hoffmann-La Roche Inc. Compounds useful as dual antagonists of platelet activating factor and leukotriene D4
CA2159344A1 (en) 1993-03-30 1994-10-13 Minoru Moriwaki Cell adhesion inhibitor and thienotriazolodiazepine compound
EP0698015A1 (en) 1993-05-14 1996-02-28 Genentech, Inc. Preparation of n-cyanodithioimino-carbonates and 3-mercapto-5-amino-1h-1,2,4-triazole
US5869483A (en) 1993-07-29 1999-02-09 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
US5516774A (en) 1993-07-29 1996-05-14 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
US5733905A (en) 1993-07-29 1998-03-31 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
US5760031A (en) 1993-07-29 1998-06-02 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
JP3633008B2 (ja) 1993-11-15 2005-03-30 三菱ウェルファーマ株式会社 チエノトリアゾロジアゼピン化合物
WO1995014694A1 (en) 1993-11-22 1995-06-01 Merck & Co., Inc. Benzodiazepines
WO1995018130A1 (en) 1993-12-28 1995-07-06 Meiji Seika Kabushiki Kaisha Tricyclic benzazepine and benzothiazepine derivatives
US5739129A (en) 1994-04-14 1998-04-14 Glaxo Wellcome Inc. CCK or gastrin modulating 5-heterocyclic-1, 5 benzodiazepines
JPH09511998A (ja) 1994-04-15 1997-12-02 グラクソ、ウェルカム、インコーポレーテッド 1,4 − ベンゾジアゼピン化合物を用いたコレシストキニンアゴニスト活性の誘導方法
JP3264588B2 (ja) 1994-08-23 2002-03-11 松下電器産業株式会社 電子地図データの生成装置
JP3264589B2 (ja) 1994-09-07 2002-03-11 東芝機械株式会社 研磨装置
KR100484294B1 (ko) 1995-09-21 2005-09-09 가부시키가이샤 이야쿠 분지 셋케이 겐쿠쇼 레티노이드작용증강성화합물
CA2258053A1 (en) 1996-06-12 1997-12-18 Yoshihisa Yamamoto Cytokine production inhibitors, triazepine compounds, and intermediates thereof
EA001732B1 (ru) 1996-09-13 2001-08-27 Велфайд Корпорейшн Тиенотриазолодиазепиновые соединения и лекарственное средство
IL129820A0 (en) 1996-12-23 2000-02-29 Elan Pharm Inc Cycloalkyl lactam lactone and related compounds as beta-amyloid peptide release inhibitors
US6433167B1 (en) 1997-06-25 2002-08-13 Nikken Chemicals Co., Ltd. Triazolo-1,4-diazepine compounds and medicinal composition containing the same
JP4204657B2 (ja) 1997-12-05 2009-01-07 有限会社ケムフィズ 糖尿病の予防・治療剤
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
PE20000944A1 (es) 1998-07-31 2000-09-20 Lilly Co Eli Derivados de sulfonamida
CA2335102A1 (en) 1998-09-01 2000-03-09 Innogenetics N.V. Benzodiazepines and benzothiazepines derivatives and hbsag peptides binding to annexins, their compositions and use
AU2939000A (en) 1999-03-12 2000-10-04 Welfide Corporation Preventive or therapeutic agents for inflammatory dermatoses
FR2791980B1 (fr) 1999-04-09 2001-07-06 Sod Conseils Rech Applic Pyrido-thieno-diazepines, leur procede de preparation, et les compositions pharmaceutiques les contenant
GB9911152D0 (en) 1999-05-14 1999-07-14 Glaxo Group Ltd Short-acting benzodiazepines
US7160880B1 (en) 1999-05-14 2007-01-09 Cenes Limited Short-acting benzodiazepines
DE60015392D1 (de) 1999-12-29 2004-12-02 Glaxo Group Ltd Verwendung von annexin-modulatoren zur herstellung eines medikaments zur behandlung und/oder vorbeugung von arthritis und arthritischen erkrankungen
CA2412776C (en) 2000-06-16 2011-03-15 Mitsubishi Pharma Corporation Compositions controlling release ph range and/or speed
US7250410B2 (en) 2001-06-07 2007-07-31 Via Pharmaceuticals, Inc. Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses thereof
US20050096322A1 (en) 2002-03-01 2005-05-05 Susumu Igarashi Nitrogen-containing heterocyclic compound
CA2503716A1 (fr) 2002-10-30 2004-05-21 Jean-Jacques Bourguignon Utilisation d'inhibiteurs des phosphodiesterases des nucleotides cycliques, ayant une structure benzodiazepinique en therapie
DE10251927A1 (de) 2002-11-08 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
US7482337B2 (en) 2002-11-08 2009-01-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
KR100562489B1 (ko) 2002-11-11 2006-03-21 삼성전자주식회사 셔터 타이밍 조절 가능한 로우 디코더를 갖는 이미지 센서
MXPA05006478A (es) 2002-12-18 2005-09-08 Vertex Pharma Triazolopiridazinas como inhibidores de proteinas cinasas.
US7119088B2 (en) 2003-02-19 2006-10-10 Pfizer Inc. Triazole compounds useful in therapy
EP1640010A1 (en) 2003-07-01 2006-03-29 Astellas Pharma Inc. Agent inducing increase in bone mass
WO2005099759A1 (ja) 2004-04-16 2005-10-27 Institute Of Medicinal Molecular Design. Inc. 動脈硬化症の予防及び/又は治療のための医薬
EP1806070A1 (en) 2004-10-05 2007-07-11 Pioneer Corporation Audio rack
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
CA2615463A1 (en) 2005-07-29 2007-02-08 Merck & Co., Inc. Heterocyclic benzodiazepine cgrp receptor antagonists
US20070105844A1 (en) 2005-10-26 2007-05-10 Regents Of The University Of Michigan Therapeutic compositions and methods
AU2006306347A1 (en) 2005-10-26 2007-05-03 The Regents Of The University Of Michigan Therapeutic compositions and methods
DE102005061840A1 (de) 2005-12-23 2007-06-28 Merck Patent Gmbh Triazolderivate
KR20090055001A (ko) 2006-08-25 2009-06-01 닛뽕 케미파 가부시키가이샤 P2x4 수용체 길항제
WO2008109856A2 (en) 2007-03-07 2008-09-12 Xenon Pharmaceuticals Inc. Methods of using diazepinone compounds in treating sodium channel-mediated diseases or conditions
US20090111780A1 (en) 2007-10-31 2009-04-30 Everett Laboratories, Inc. Compositions and methods for treatment of ear canal infection and inflammation
ITFI20070288A1 (it) 2007-12-21 2009-06-22 A I L Firenze Sezione Autonoma Inibitori delle deacetilasi istoniche
CA2710740C (en) 2007-12-28 2016-07-19 Shinji Miyoshi Thienotriazolodiazepine compound as antitumor agent
CN102123706B (zh) 2008-06-17 2013-08-14 米纳斯吉拉斯联合大学 血小板活化因子受体在治疗黄病毒科病毒引起的感染中的用途
KR20110033239A (ko) 2008-06-23 2011-03-30 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제
KR101633742B1 (ko) 2008-10-30 2016-06-27 써코메드 엘엘씨 아포 a에 활성인 티에노트리아졸로디아제핀 유도체
EP2417138B1 (en) 2009-04-09 2019-11-27 Merck Sharp & Dohme Corp. Pyrazolo[1, 5-a]pyrimidine derivatives as mtor inhibitors
WO2010121164A2 (en) 2009-04-17 2010-10-21 The Regents Of The University Of Michigan 1,4-benzodiazepinone compounds and their use in treating cancer
EP2427451B1 (en) 2009-05-07 2019-03-20 PRISM BioLab Co., Ltd. Alpha helix mimetics and methods relating thereto
WO2011037128A1 (ja) 2009-09-28 2011-03-31 日本曹達株式会社 含窒素ヘテロ環化合物およびその塩ならびに農園芸用殺菌剤
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919426D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
WO2011054851A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Novel process
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
SI2496582T1 (sl) 2009-11-05 2016-04-29 Glaxosmithkline Llc Corporation Service Company Benzodiazepinski inhibitor bromodomene
ME02360B (me) 2009-11-05 2016-06-20 Glaxosmithkline Llc Inhibitor bromodomena benzodiazepina
US8765920B2 (en) 2009-12-23 2014-07-01 The Scripps Research Institute Tyrosine bioconjugation through aqueous Ene-like reactions
TW201201813A (en) 2010-03-31 2012-01-16 Arqule Inc Substituted benzo-pyrido-triazolo-diazepine compounds
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
WO2011143657A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Male contraceptive compositions and methods of use
DK2571503T3 (en) 2010-05-14 2015-04-20 Dana Farber Cancer Inst Inc COMPOSITIONS AND THEIR USE IN THE TREATMENT OF NEOPLASIA, INFLAMMATORY DISEASE AND OTHER DISORDERS
WO2011143660A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
ES2526671T3 (es) * 2010-06-22 2015-01-14 Glaxosmithkline Llc Compuestos de benzotriazoldiazepina inhibidores de bromodominios
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (es) * 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
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
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof

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US20170079984A1 (en) 2017-03-23
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AU2013271569A1 (en) 2014-12-18
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NZ702458A (en) 2016-11-25
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