PE20150729A1 - 2,3-benzodiazepines - Google Patents

2,3-benzodiazepines

Info

Publication number
PE20150729A1
PE20150729A1 PE2015000185A PE2015000185A PE20150729A1 PE 20150729 A1 PE20150729 A1 PE 20150729A1 PE 2015000185 A PE2015000185 A PE 2015000185A PE 2015000185 A PE2015000185 A PE 2015000185A PE 20150729 A1 PE20150729 A1 PE 20150729A1
Authority
PE
Peru
Prior art keywords
disorders
inhibitors
compounds according
atherosclerotic
benzodiazepines
Prior art date
Application number
PE2015000185A
Other languages
English (en)
Inventor
Stephan Siegel
Stefan Baurle
Arwed Cleve
Bernard Haendler
Amaury Ernesto Fernandez-Montalvan
Ursula Monning
Sabine Krause
Pascale Germaine Sylviane Lejeune
Norbert Schmees
Matthias Busemann
Simon Holton
Joachim Kuhnke
Original Assignee
Bayer Pharma AG
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48979774&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20150729(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of PE20150729A1 publication Critical patent/PE20150729A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • A61K31/551—Heterocyclic 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
    • 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
    • A61K31/551—Heterocyclic 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/02—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La invencion describe 2,3-benzodiacepinas inhibidoras de proteinas BET, en particular inhibidoras de BRD4 de formula general (I) en las que R1a, R1b, R1c, R2, R3, R4, R5, A y X tienen los significados dados en la descripcion, los intermedios para preparar los compuestos de acuerdo con la invencion, composiciones farmaceuticas que comprenden a los compuestos de acuerdo con la invencion y su uso profilactico y terapeutico para trastornos hiperproliferativos, en particular, para trastornos tumorales. Tambien se describe el uso de inhibidores de proteina BET para hiperplasias benignas, trastornos ateroescleroticos, septicemia, trastornos autoinmunes, trastornos vasculares, infecciones virales, para trastornos neurodegenerativos, para trastornos inflamatorios, para trastornos ateroescleroticos y para el control de la fertilidad masculina
PE2015000185A 2012-08-16 2013-08-13 2,3-benzodiazepines PE20150729A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102012214602 2012-08-16
DE102013202104 2013-02-08

Publications (1)

Publication Number Publication Date
PE20150729A1 true PE20150729A1 (es) 2015-06-14

Family

ID=48979774

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015000185A PE20150729A1 (es) 2012-08-16 2013-08-13 2,3-benzodiazepines

Country Status (23)

Country Link
US (1) US9890147B2 (es)
EP (1) EP2885286B1 (es)
JP (1) JP6333251B2 (es)
KR (1) KR20150041787A (es)
CN (1) CN104755473B (es)
AR (1) AR092129A1 (es)
AU (1) AU2013304146A1 (es)
CA (1) CA2881996A1 (es)
CL (1) CL2015000337A1 (es)
CR (1) CR20150066A (es)
DO (1) DOP2015000022A (es)
EA (1) EA201590356A1 (es)
EC (1) ECSP15005376A (es)
ES (1) ES2628005T3 (es)
HK (1) HK1208443A1 (es)
IL (1) IL236898A0 (es)
MX (1) MX2015001880A (es)
PE (1) PE20150729A1 (es)
PH (1) PH12015500323A1 (es)
TN (1) TN2015000051A1 (es)
TW (1) TW201408651A (es)
UY (1) UY34977A (es)
WO (1) WO2014026997A1 (es)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI568722B (zh) 2012-06-15 2017-02-01 葛蘭馬克製藥公司 作爲ｍＰＧＥＳ－１抑制劑之三唑酮化合物
EP2958909A1 (de) * 2013-02-19 2015-12-30 Bayer Pharma Aktiengesellschaft Bicyclo- und spirocyclisch substituierte 2,3-benzodiazepine
KR102355670B1 (ko) 2013-03-15 2022-02-08 인사이트 홀딩스 코포레이션 Bet 단백질 저해제로서의 삼환식 복소환
CA2917319A1 (en) 2013-07-08 2015-01-15 Incyte Holdings Corporation Tricyclic 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
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
WO2015121226A1 (de) * 2014-02-13 2015-08-20 Bayer Pharma Aktiengesellschaft 6-substituierte 2,3-benzodiazepine
UA119870C2 (uk) 2014-04-23 2019-08-27 Інсайт Корпорейшн 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
JP6930913B2 (ja) 2014-10-14 2021-09-01 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアＴｈｅ Ｒｅｇｅｎｔｓ Ｏｆ Ｔｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｃａｌｉｆｏｒｎｉａ 炎症を阻害するためのｃｄｋ９及びｂｒｄ４阻害剤の使用法
WO2016062688A1 (de) * 2014-10-23 2016-04-28 Bayer Pharma Aktiengesellschaft 1-phenyl-4,5-dihydro-3h-2,3-benzodiazepine derivatives
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
WO2017005711A1 (de) * 2015-07-09 2017-01-12 Bayer Pharma Aktiengesellschaft Phosphor- und schwefel-substituierte benzodiazepin-derivate
WO2017063959A1 (de) * 2015-10-15 2017-04-20 Bayer Pharma Aktiengesellschaft N-sulfoximinophenyl-substituierte benzodiazepin-derivate als bet-proteininhibitoren
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
US10167293B2 (en) * 2016-05-26 2019-01-01 Bayer Pharma Aktiengesellschaft [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanones
DE102017005089A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
DK3472157T3 (da) 2016-06-20 2023-05-01 Incyte Corp Krystallinske faste former af en bet-inhibitor
CN109563438B (zh) * 2016-08-15 2022-11-04 奇华顿股份有限公司 有机化合物
CN109406685B (zh) * 2018-12-27 2021-05-25 湖南泰新医药科技有限公司 一种分离卡非佐米和其异构体的高效液相色谱方法
US20220079952A1 (en) * 2019-05-24 2022-03-17 Emory University Uses of Radiation and Benzodiazepine Derivatives in Cancer Therapies
WO2021152113A1 (en) 2020-01-31 2021-08-05 Bayer Aktiengesellschaft Substituted 2,3-benzodiazepines derivatives
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN114920727B (zh) * 2022-05-26 2023-07-25 重庆华邦制药有限公司 一种卢帕他定的制备方法
WO2023229535A1 (en) 2022-05-27 2023-11-30 Engine Biosciences Pte. Ltd. Bet polypeptide therapeutic agents for generating synthetic lethality in tumors

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3483186A (en) * 1966-11-22 1969-12-09 Mcneilab Inc 2-benzazepine derivatives
HU208429B (en) 1991-05-03 1993-10-28 Gyogyszerkutato Intezet Process for producing 1-/3-chloro-phenyl/-4-methyl-7,8-dimethoxy-5h-2,3-benzodiazepine of high purity
JP3239364B2 (ja) 1991-10-11 2001-12-17 ウェルファイド株式会社 骨粗鬆症治療薬およびジアゼピン化合物
EP0661284A1 (en) 1992-09-18 1995-07-05 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
EP0703222A1 (en) 1993-05-13 1996-03-27 Yoshitomi Pharmaceutical Industries, Ltd. 3-aminoazepine compound and pharmaceutical use thereof
DE19604920A1 (de) * 1996-02-01 1997-08-07 Schering Ag Neue 2,3-Benzodiazepinderivate, deren Herstellung und Verwendung als Arzneimittel
US5891871A (en) 1996-03-21 1999-04-06 Cocensys, Inc. Substituted 2,3-benzodiazepin-4-ones and the use thereof
HU9600871D0 (en) * 1996-04-04 1996-05-28 Gyogyszerkutato Intezet New 2,3-benzodiazepine derivatives
BR9710453A (pt) 1996-06-12 1999-08-17 Japan Tobacco Inc Inhibidor de produ-Æo de citocina composto de triazepina e intermedi rio para o mesmo
AU716490B2 (en) 1996-09-13 2000-02-24 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compounds and pharmaceutical use thereof
WO2001098280A2 (en) 2000-06-16 2001-12-27 Annovis, Inc. 5h-2,3-benzodiazepine antagonists of excitatory amino acid receptors
HU225100B1 (hu) * 2000-12-21 2006-06-28 Egyt Gyogyszervegyeszeti Gyar 2,3-Benzodiazepinszármazékok, ilyen hatóanyagot tartalmazó gyógyászati készítmények és alkalmazásuk
WO2003087061A1 (en) 2002-04-12 2003-10-23 Pfizer Japan Inc. Pyrazole compounds as anti-inflammatory and analgesic agents
US6858605B2 (en) * 2003-02-04 2005-02-22 Ivax Drug Research Institute, Ltd. Substituted 2,3-benzodiazepine derivatives
GB0425196D0 (en) 2004-11-15 2004-12-15 Black James Foundation Gastrin and cholecystokinin receptor ligands
GB0503962D0 (en) 2005-02-25 2005-04-06 Kudos Pharm Ltd Compounds
US8044042B2 (en) 2005-05-30 2011-10-25 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and medicinal use thereof
EA016087B1 (ru) * 2005-12-30 2012-02-28 Эгиш Дьёдьсердьяр Ньильваношан Мюкёдё Ресвеньтаршашаг Оптические изомеры дигидро-2,3-бензодиазепинов и их стереоселективный синтез
DE102006042439A1 (de) 2006-09-09 2008-03-27 Saltigo Gmbh Verfahren zur katalytischen Herstellung von aromatischen oder heteroaromatischen Nitrilen
TW200902024A (en) * 2007-04-02 2009-01-16 Teva Pharma Novel 2,3-benzodiazepine derivatives and their use as antipsychotic agents
JP2008308491A (ja) * 2007-05-11 2008-12-25 Gunma Univ がん治療用の遊走阻害剤
US8476260B2 (en) 2007-12-28 2013-07-02 Mitsubishi Tanabe Pharma Corporation Antitumor agent
KR101435729B1 (ko) * 2009-09-28 2014-09-01 닛뽕소다 가부시키가이샤 함질소 헤테로 고리 화합물 및 그의 염, 그리고 농원예용 살균제
PE20121181A1 (es) 2009-11-05 2012-09-13 Glaxosmithkline Llc Inhibidor de bromodominio de benzodiazepina
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ES2564318T3 (es) 2009-11-05 2016-03-21 Glaxosmithkline Llc Inhibidor de bromodominio de benzodiazepina
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
HUE031073T2 (en) * 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
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

Also Published As

Publication number Publication date
TW201408651A (zh) 2014-03-01
ECSP15005376A (es) 2015-12-31
US20150203483A1 (en) 2015-07-23
CL2015000337A1 (es) 2015-05-04
CA2881996A1 (en) 2014-02-20
IL236898A0 (en) 2015-03-31
DOP2015000022A (es) 2015-09-15
ES2628005T3 (es) 2017-08-01
PH12015500323A1 (en) 2015-03-30
EA201590356A1 (ru) 2015-07-30
AU2013304146A1 (en) 2015-02-26
WO2014026997A1 (de) 2014-02-20
CR20150066A (es) 2015-04-17
EP2885286B1 (de) 2017-03-22
CN104755473A (zh) 2015-07-01
CN104755473B (zh) 2017-03-08
JP2015529192A (ja) 2015-10-05
AR092129A1 (es) 2015-03-25
MX2015001880A (es) 2015-05-11
EP2885286A1 (de) 2015-06-24
KR20150041787A (ko) 2015-04-17
HK1208443A1 (en) 2016-03-04
US9890147B2 (en) 2018-02-13
UY34977A (es) 2014-03-31
JP6333251B2 (ja) 2018-05-30
TN2015000051A1 (en) 2016-06-29

Similar Documents

Publication Publication Date Title
PE20150729A1 (es) 2,3-benzodiazepines
UY35205A (es) Dihidropiridopirazinonas inhibidoras de la proteína bet
CY1120517T1 (el) Διαρυλικες ενωσεις χρησιμες για την αγωγη ανθρωπινων νοσων στην ογκολογια, νευρολογια και ανοσολογια
CY1124436T1 (el) Δικυκλικες ετεροκυκλικες ενωσεις και χρησεις αυτων στη θεραπεια
CY1121850T1 (el) Διαρυλο μακροκυκλοι ως ρυθμιστες των πρωτεϊνικων kinασων
CY1120734T1 (el) Στερεες μορφες ενος εκλεκτικου αναστολεα cdk4/6
CU20190018A7 (es) Compuestos inhibidores de los receptores endosomales tipo peaje
ECSP15043696A (es) Compuestos de heteroarilo y sus usos
CL2012001821A1 (es) Compuestos derivados de 5-alquinil-pirimidinas, inhibidores de quinasas; composiciones farmaceuticas que los contienen; y su uso para el tratamiento y/o prevencion de cancer, infecciones, enfermedades inflamatorias y autoinmunitarias.
CL2018002924A1 (es) Inhibidores de bromodominios
CY1119576T1 (el) Ν-ακυλ-(3-υποκατεστημενες)-(8-υποκατεστημενες)-5,6-διϋδρο-[1,2,4]τριαζολο[4,3-α]πυραζινες ως επιλεκτικοι ανταγωνιστες του υποδοχεα νκ-3, φαρμακευτικη συνθεση, μεθοδοι για χρηση σε διαμεσολαβουμενες απο τον υποδοχεα νκ-3 διαταραχες
NZ712453A (en) Tricyclic heterocycles as bet protein inhibitors
CR20150426A (es) 2,3-benzodiazepinas biciclo y espirocíclico sustituidas
CL2016000925A1 (es) Inhibidores de bromodominio
EA201500926A1 (ru) Фумараты как пролекарства и их применение при лечении различных заболеваний
PE20151501A1 (es) Inhibidores de prmt5 y sus usos
PE20151070A1 (es) Inhibidores de la tirosina - quinasa de bruton
NI201500119A (es) Compuestos de heteroarilo y sus usos
EA201591420A1 (ru) Гетероарильные соединения и их применение
CL2014001547A1 (es) Compuestos derivados de benzotienilo-pirrolotriazina, como inhibidores de la proteina tirosina quinasa; procedimiento de preparacion de dichos compuestos; composicion farmaceutica que los comprende; y su uso para el tratamiento y/o la prevencion de cancer y enfermedades tumorales.
CL2011000691A1 (es) Compuestos derivados de nicotinamida sustituida; composicion farmaceutica que los comprende; uso para el tratamiento y/o prevencion de cancer, infecciones, enfermedades inflamatorias y autoinmunitarias.
EA201492216A1 (ru) Ингибиторы бромодомена и их применение
CR8929A (es) Polimorfo ii de rapamicina y usos del mismo
ECSP077316A (es) Compuestos imidazo-3-il-amina bicíclicos sustituidos
UY33616A (es) Compuestos con estructura de imidazotriazinona

Legal Events

Date Code Title Description
FD Application declared void or lapsed