JP6154004B2 - ブロモドメイン阻害剤のベンゾ［ｃ］イソオキサゾロアゼピン及びその使用 - Google Patents

ブロモドメイン阻害剤のベンゾ［ｃ］イソオキサゾロアゼピン及びその使用 Download PDF

Info

Publication number
JP6154004B2
JP6154004B2 JP2015516192A JP2015516192A JP6154004B2 JP 6154004 B2 JP6154004 B2 JP 6154004B2 JP 2015516192 A JP2015516192 A JP 2015516192A JP 2015516192 A JP2015516192 A JP 2015516192A JP 6154004 B2 JP6154004 B2 JP 6154004B2
Authority
JP
Japan
Prior art keywords
cancer
alkyl
compound
methyl
pharmaceutically acceptable
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2015516192A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015518899A5 (2
JP2015518899A (ja
Inventor
アルブレヒト，ブライアン・ケイ
ヒューイット，マイケル・チャールズ
ゲーリング，ヴィクター・エス
ヴァスワニ，リシ・ジー
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Constellation Pharmaceuticals Inc
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 JP2015518899A publication Critical patent/JP2015518899A/ja
Publication of JP2015518899A5 publication Critical patent/JP2015518899A5/ja
Application granted granted Critical
Publication of JP6154004B2 publication Critical patent/JP6154004B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2015516192A 2012-06-06 2013-06-06 ブロモドメイン阻害剤のベンゾ［ｃ］イソオキサゾロアゼピン及びその使用 Active JP6154004B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261656205P 2012-06-06 2012-06-06
US61/656,205 2012-06-06
PCT/US2013/044444 WO2013184876A1 (en) 2012-06-06 2013-06-06 Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof

Publications (3)

Publication Number Publication Date
JP2015518899A JP2015518899A (ja) 2015-07-06
JP2015518899A5 JP2015518899A5 (2) 2016-06-30
JP6154004B2 true JP6154004B2 (ja) 2017-06-28

Family

ID=48626693

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015516192A Active JP6154004B2 (ja) 2012-06-06 2013-06-06 ブロモドメイン阻害剤のベンゾ［ｃ］イソオキサゾロアゼピン及びその使用

Country Status (19)

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

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
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
HK1214819A1 (zh) 2013-02-19 2016-08-05 Bayer Pharma Aktiengesellschaft 二环2，3-苯并二氮杂䓬和螺环取代的2，3-苯并二氮杂䓬
HK1212972A1 (zh) 2013-02-22 2016-06-24 Bayer Pharma Aktiengesellschaft 作爲bet-蛋白抑制剂用於治疗过度增殖性疾病的吡咯并-和吡唑并-三唑并二氮杂卓
EP2958923A1 (de) 2013-02-22 2015-12-30 Bayer Pharma Aktiengesellschaft 4-substituierte pyrrolo- und pyrazolo-diazepine
CA2903881C (en) 2013-03-15 2021-05-18 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 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
US20170027955A1 (en) * 2014-04-04 2017-02-02 Constellation Pharmaceuticals, Inc. Expression levels of bcl-xl, bcl2, bcl-w, and bad and cancer therapies
SG10201809353TA (en) 2014-04-23 2018-11-29 Incyte Corp 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
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
TWI712603B (zh) 2014-09-15 2020-12-11 美商英塞特公司 作為ｂｅｔ蛋白抑制劑之三環雜環
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
EP3314005A1 (en) 2015-06-26 2018-05-02 Tensha Therapeutics, Inc. Treatment of nut midline carcinoma
RU2734959C2 (ru) 2015-09-09 2020-10-26 Джубилант Байосис Лимитед Трициклические конденсированные производные пиридин-2-она и их применение в качестве ингибиторов brd4
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
EP3397640B1 (en) 2015-12-29 2021-08-04 INSERM - Institut National de la Santé et de la Recherche Médicale Xanthine derivative inhibitors of bet proteins
WO2017222977A1 (en) 2016-06-20 2017-12-28 Incyte Corporation Crystalline solid forms of a bet inhibitor
JP6827113B2 (ja) 2017-01-21 2021-02-10 広州白雲山漢方現代薬業有限公司Ｇｕａｎｇｚｈｏｕ Ｈａｎｆａｎｇ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｃｏ．，Ｌｔｄ． シェーグレン症候群の治療におけるペオニフロリン−６’−ｏ−ベンゼンスルホン酸の使用
WO2019086712A1 (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
MX2020009967A (es) 2018-03-30 2021-01-08 Kyowa Kirin Co Ltd Compuesto con actividad anticancerigena.
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
US3709898A (en) 1971-02-09 1973-01-09 Upjohn Co Process for the production of triazolobenzodiazepines and intermediates
US3781289A (en) 1971-02-09 1973-12-25 Upjohn Co 7-chloro-1-methyl-5-phenyl-s-triazolo (4,3-a)quinolines
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
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
US3903103A (en) 1971-09-15 1975-09-02 Upjohn Co 4-Amino-s-triazolo-{8 4,3-a{9 {8 1,4{9 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
IE38931B1 (en) 1973-03-09 1978-07-05 Lipha Triazolobenzodiazepines
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
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
CA1163266A (en) 1980-07-31 1984-03-06 Albert E. Fischli Benzodiazepine derivatives
CA1157855A (en) 1980-07-31 1983-11-29 Albert E. Fischli Benzodiazepine derivatives
US4455307A (en) 1982-01-04 1984-06-19 The Upjohn Company Antihypertensive use of triazolobenzodiazepines
US4820834A (en) 1984-06-26 1989-04-11 Merck & Co., Inc. Benzodiazepine analogs
US5004741A (en) 1984-06-26 1991-04-02 Merck & Co., Inc. Methods of antagonizing CCK or gastrin with benzodiazepine analogs
US4663321A (en) 1984-06-26 1987-05-05 Merck & Co., Inc. Triazolobenzodiazepines and pharmaceutical use
DE3878833T2 (de) 1987-05-28 1993-06-09 Yoshitomi Pharmaceutical Thieno(triazolo)diazepinverbindungen, und medizinische verwendung derselben.
MC1999A1 (fr) 1987-12-18 1990-01-26 Hoffmann La Roche Composes tricycliques
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
EP0348523A4 (en) 1987-12-22 1991-10-09 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compounds and their medicinal use
CA1324863C (en) 1988-01-30 1993-11-30 Welfide Corporation Thienotriazolodiazepine compounds and pharmaceutical uses thereof
CA1322367C (en) 1988-05-17 1993-09-21 Yoshitomi Pharmaceutical Industries Ltd. Thienotriazolodiazepine compounds and pharmaceutical uses thereof
US5221671A (en) 1988-10-31 1993-06-22 Eisai Co., Ltd. Triazolo-1,4-diazepine derivatives and their use in pharmaceuticals
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
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
DE69017302T3 (de) 1989-08-04 1999-08-05 Merck Sharp & Dohme Ltd., Hoddesdon, Hertfordshire Zentrale Cholecystokinin-Antagonisten zur Behandlung von psychiatrischen Krankheiten.
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
WO1994006801A1 (fr) 1990-05-23 1994-03-31 Yoshitomi Pharmaceutical Industries, Ltd. Compose de thienodiazepine et son utilisation comme medicament
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
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
WO1993007152A1 (en) 1991-09-30 1993-04-15 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and its use
EP0638560A4 (en) 1991-10-11 1995-03-29 Yoshitomi Pharmaceutical MEDICINE FOR OSTEOPOROSIS AND DIAZEPINE COMPOUND *.
US5686479A (en) 1991-12-11 1997-11-11 Yoshitomi Pharmaceutical Industries, Ltd. Immunosuppressive drug
JPH07507993A (ja) 1991-12-20 1995-09-07 メルク　シヤープ　エンド　ドーム　リミテツド 医薬活性を有する中枢神経系コレシストキニンアンタゴニスト
DE4200610A1 (de) 1992-01-13 1993-07-15 Boehringer Ingelheim Kg Verwendung von paf-antagonisten zur behandlung der dysmenorrhea
AU670431B2 (en) 1992-03-24 1996-07-18 Merck Sharp & Dohme Limited 3-ureido substituted benzodiazepin-2-ones having cholecystokinin and/or gastrin antagonistic activity and their use in therapy
DE4219659A1 (de) 1992-06-16 1993-12-23 Boehringer Ingelheim Kg Die Verwendung von PAF-Antagonisten in Kombination mit Anticholinergika
EP0661284A1 (en) 1992-09-18 1995-07-05 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
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
WO1994026723A2 (en) 1993-05-14 1994-11-24 Genentech, Inc. ras FARNESYL TRANSFERASE INHIBITORS
US5733905A (en) 1993-07-29 1998-03-31 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
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
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
EP0730596A4 (en) 1993-11-22 1997-07-30 Merck & Co Inc BENZODIAZEPINE
DE69427023T2 (de) 1993-12-28 2001-10-31 Meiji Seika K.K., Tokio/Tokyo Tricyclische benzazepin-und benzothiazepin derivate
US5739129A (en) 1994-04-14 1998-04-14 Glaxo Wellcome Inc. CCK or gastrin modulating 5-heterocyclic-1, 5 benzodiazepines
AU2446295A (en) 1994-04-15 1995-11-10 Glaxo Inc. A method of inducing cholecystokinin agonist activity using 1,4-benzodiazepine compounds
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
ATE214055T1 (de) 1995-09-21 2002-03-15 Inst Med Molecular Design Inc Retinoid-potenzierende verbindungen
CN1227555A (zh) 1996-06-12 1999-09-01 日本烟草产业株式会社 细胞因子生成抑制剂、三氮䓬化合物及其中间体
ATE227727T1 (de) 1996-09-13 2002-11-15 Mitsubishi Pharma Corp Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen
EA002100B1 (ru) 1996-12-23 2001-12-24 Элан Фармасьютикалз, Инк. ЦИКЛОАЛКИЛЬНЫЕ СОЕДИНЕНИЯ, ЛАКТАМЫ, ЛАКТОНЫ И РОДСТВЕННЫЕ СОЕДИНЕНИЯ, СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И СПОСОБЫ ИНГИБИРОВАНИЯ ВЫСВОБОЖДЕНИЯ И/ИЛИ СИНТЕЗА β-АМИЛОИДНОГО ПЕПТИДА С ПОМОЩЬЮ УКАЗАННЫХ СОЕДИНЕНИЙ
CA2294139A1 (en) 1997-06-25 1998-12-30 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
BR9913226A (pt) 1998-09-01 2001-05-22 Innogenetics Nv Benzodiazepinas e derivados de benzotiazepinas e peptìdios de hbsag ligados a anexinas, suas composições e uso
WO2000054778A1 (fr) 1999-03-12 2000-09-21 Welfide Corporation Agents preventifs ou therapeutiques des dermatoses inflammatoires
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
US7160880B1 (en) 1999-05-14 2007-01-09 Cenes Limited Short-acting benzodiazepines
GB9911152D0 (en) 1999-05-14 1999-07-14 Glaxo Group Ltd Short-acting benzodiazepines
WO2001047510A2 (en) 1999-12-29 2001-07-05 Glaxo Group Limited Methods and compositions related to modulators of annexin and cartilage homeostasis
EP1297836A4 (en) 2000-06-16 2007-06-13 Mitsubishi Pharma Corp COMPOSITIONS FOR CHECKING RELEASE, PH AREA AND / OR SPEED
AU2002317910B2 (en) 2001-06-07 2008-06-19 Via Pharmaceuticals, Inc. Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses thereof
CN1281606C (zh) 2002-03-01 2006-10-25 安斯泰来制药有限公司 含氮杂环化合物
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
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
DE10251927A1 (de) 2002-11-08 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
KR100562489B1 (ko) 2002-11-11 2006-03-21 삼성전자주식회사 셔터 타이밍 조절 가능한 로우 디코더를 갖는 이미지 센서
ATE473980T1 (de) 2002-12-18 2010-07-15 Vertex Pharma Triazolopyridazine als proteinkinase-inhibitoren
US20060173009A1 (en) 2003-01-07 2006-08-03 Hiroyuki Kanoh Agent inducing increase in bone mass
US7119088B2 (en) 2003-02-19 2006-10-10 Pfizer Inc. Triazole compounds useful in therapy
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
JP4494414B2 (ja) 2004-10-05 2010-06-30 パイオニア株式会社 オーディオラック
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
WO2007016087A2 (en) 2005-07-29 2007-02-08 Merck & Co., Inc. Heterocyclic benzodiazepine cgrp receptor antagonists
JP2009513644A (ja) 2005-10-26 2009-04-02 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 治療組成物および方法
US20070105844A1 (en) 2005-10-26 2007-05-10 Regents Of The University Of Michigan Therapeutic compositions and methods
DE102005061840A1 (de) 2005-12-23 2007-06-28 Merck Patent Gmbh Triazolderivate
EP2058304A4 (en) 2006-08-25 2012-10-10 Nippon Chemiphar Co P2X4 RECEPTOR ANTAGONIST
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
KR101600634B1 (ko) 2007-12-28 2016-03-07 미쓰비시 타나베 파마 코퍼레이션 항암제
EP2349257B1 (en) 2008-06-17 2013-11-27 Universidade Federal de Minas Gerais-UFMG Use of paf receptor for treating infections caused by flaviviridae
MX2011000021A (es) 2008-06-23 2011-02-24 Vertex Pharma Inhibidores de proteina cinasas.
JP5490811B2 (ja) 2008-10-30 2014-05-14 スルコメッド エルエルシー アポａに対して活性なチエノトリアゾロジアゼピン誘導体
WO2010118207A1 (en) 2009-04-09 2010-10-14 Schering Corporation Pyrazolo [1, 5-a] pyrimidine derivatives as mtor inhibitors
US8604023B2 (en) 2009-04-17 2013-12-10 The Regents Of The University Of Michigan 1,4-benzodiazepinone compounds and their use in treating cancer
WO2010128685A1 (en) 2009-05-07 2010-11-11 Prism Biolab Corporation Alpha helix mimetics and methods relating thereto
EP2484672B1 (en) 2009-09-28 2015-07-15 Nippon Soda Co., Ltd. Nitrogen-containing heterocyclic compound and salt thereof, and herbicide for agricultural and horticultural use
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919426D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (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
ES2564318T3 (es) 2009-11-05 2016-03-21 Glaxosmithkline Llc Inhibidor de bromodominio de benzodiazepina
EP2496945B1 (en) 2009-11-05 2015-04-01 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
WO2011079315A1 (en) 2009-12-23 2011-06-30 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
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
US9301962B2 (en) 2010-05-14 2016-04-05 Baylor College Of Medicine Male contraceptive compositions and methods of use
US20130252331A1 (en) 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
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
US9085582B2 (en) * 2010-06-22 2015-07-21 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
AR084070A1 (es) * 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
WO2012151512A2 (en) 2011-05-04 2012-11-08 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel 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
US10071129B2 (en) 2011-08-30 2018-09-11 Whitehead Institute For Biomedical Research Dana-Farber Cancer Institute, Inc. Method for identifying 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
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof

Also Published As

Publication number Publication date
WO2013184876A8 (en) 2014-11-27
EA026894B1 (ru) 2017-05-31
US9925197B2 (en) 2018-03-27
IL235844A (en) 2017-04-30
MX360598B (es) 2018-11-08
WO2013184876A1 (en) 2013-12-12
EP2859000B1 (en) 2017-04-26
US9493483B2 (en) 2016-11-15
AU2013271569A1 (en) 2014-12-18
KR20150023562A (ko) 2015-03-05
ES2632774T3 (es) 2017-09-15
ZA201408720B (en) 2018-05-30
US20150148337A1 (en) 2015-05-28
EP2859000A1 (en) 2015-04-15
IN2014DN10386A (2) 2015-08-14
TW201402580A (zh) 2014-01-16
HK1207372A1 (en) 2016-01-29
BR112014030165A2 (pt) 2017-06-27
CA2874774C (en) 2022-10-04
US20170079984A1 (en) 2017-03-23
IL235844A0 (en) 2015-02-01
SG11201407900WA (en) 2014-12-30
JP2015518899A (ja) 2015-07-06
AU2013271569B2 (en) 2017-09-14
CN104428304A (zh) 2015-03-18
AR091285A1 (es) 2015-01-21
CA2874774A1 (en) 2013-12-12
TWI602820B (zh) 2017-10-21
MX2014015004A (es) 2015-03-05
NZ702458A (en) 2016-11-25
CN104428304B (zh) 2016-09-21
EA201492216A1 (ru) 2015-03-31

Similar Documents

Publication Publication Date Title
JP6154004B2 (ja) ブロモドメイン阻害剤のベンゾ［ｃ］イソオキサゾロアゼピン及びその使用
EP2864336B1 (en) Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
WO2014152029A2 (en) Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
KR20130125378A (ko) 브로모도메인 억제제 및 이의 용도
US10501459B2 (en) Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
IL257340B1 (en) Converted benzaimidazoles, methods for their preparation and use as pharmaceuticals
EP3334717B1 (en) Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
WO2017024406A1 (en) N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
HK1207372B (en) Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof
HK1256752B (en) Substituted benzimidazoles, their preparation and their use as pharmaceuticals

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160509

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20160509

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20161226

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20161227

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20170324

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170403

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20170502

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20170531

R150 Certificate of patent or registration of utility model

Ref document number: 6154004

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250