UY35205A - Dihidropiridopirazinonas inhibidoras de la proteína bet - Google Patents

Dihidropiridopirazinonas inhibidoras de la proteína bet

Info

Publication number
UY35205A
UY35205A UY0001035205A UY35205A UY35205A UY 35205 A UY35205 A UY 35205A UY 0001035205 A UY0001035205 A UY 0001035205A UY 35205 A UY35205 A UY 35205A UY 35205 A UY35205 A UY 35205A
Authority
UY
Uruguay
Prior art keywords
inhibitors
bet protein
disorders
dihydropiridopirazinonas
compounds according
Prior art date
Application number
UY0001035205A
Other languages
English (en)
Inventor
Haendler Dr Bernard
Lejeune Dr Pascale
Schmees Dr Norbert
Bader Dr Benjamin
Stöckigt Dr Detlef
Fernandez-Montalvan Dr Amaury Ernesto
Stellfeld Dr Timo
Gallenkamp Dr Daniel
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
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of UY35205A publication Critical patent/UY35205A/es

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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/12—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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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 two hetero rings
    • C07D495/10—Spiro-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La presente invención se refiere a dihidropiridopirazinonas inhibidoras de la proteína BET, especialmente inhibidoras de BRD4, de fórmula general (I) en la que A, X, R1, R2, R3, R4, R4, R6, R7 y n tienen los significados dados en la descripción, a intermedios para la preparación de los compuestos de acuerdo con la invención, a composiciones farmacéuticas que comprenden los compuestos de acuerdo con la invención y al uso profiláctico y terapéutic o de los mismos en el caso de trastornos hiperproliferativos, especialmente en el caso de trastornos neoplásicos. Esta invención también se refiere al uso de inhibidores de la proteína BET en infecciones virales, en trastornos neurodegenerativos, en enfermedades inflamatorias, en trastornos ateroscleróticos y en el control de la fertilidad masculina
UY0001035205A 2012-12-20 2013-12-19 Dihidropiridopirazinonas inhibidoras de la proteína bet UY35205A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12198623 2012-12-20
EP13182252 2013-08-29
EP13191933 2013-11-07

Publications (1)

Publication Number Publication Date
UY35205A true UY35205A (es) 2014-07-31

Family

ID=49779903

Family Applications (1)

Application Number Title Priority Date Filing Date
UY0001035205A UY35205A (es) 2012-12-20 2013-12-19 Dihidropiridopirazinonas inhibidoras de la proteína bet

Country Status (10)

Country Link
US (1) US20160193206A1 (es)
EP (1) EP2935260A1 (es)
JP (1) JP2016504990A (es)
CN (1) CN105229002A (es)
AR (1) AR094148A1 (es)
CA (1) CA2895404A1 (es)
HK (1) HK1213899A1 (es)
TW (1) TW201427981A (es)
UY (1) UY35205A (es)
WO (1) WO2014095774A1 (es)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2935260A1 (de) * 2012-12-20 2015-10-28 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydropyridopyrazinone
KR102216288B1 (ko) 2013-03-15 2021-02-18 인사이트 홀딩스 코포레이션 Bet 단백질 저해제로서의 삼환식 복소환
AR096837A1 (es) 2013-07-08 2016-02-03 Incyte Corp Heterociclos tricíclicos como inhibidores de proteínas bet
JP2016523941A (ja) * 2013-07-09 2016-08-12 バイエル ファーマ アクチエンゲゼルシャフト 改変されたｂｅｔタンパク質阻害性ジヒドロキノキサリノンおよびジヒドロピリドピラジノン
KR20160034379A (ko) 2013-07-25 2016-03-29 다나-파버 캔서 인스티튜트 인크. 전사 인자의 억제제 및 그의 용도
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
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
US10150756B2 (en) 2014-01-31 2018-12-11 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
KR20160111520A (ko) * 2014-01-31 2016-09-26 다나-파버 캔서 인스티튜트 인크. 디히드로프테리디논 유도체 및 그의 용도
US9540368B2 (en) 2014-04-23 2017-01-10 Incyte Corporation 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins
CA2952526A1 (en) * 2014-06-18 2015-12-23 Bayer Pharma Aktiengesellschaft Bet-protein inhibiting 3,4-dihydropyrido[2,3-b]pyrazinones with meta-substituted aromatic amino- or ether groups
WO2015193217A1 (de) * 2014-06-18 2015-12-23 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydropyrido[2,3-b]pyrazinon-derivate mit para-substituierter aromatischer amino- oder ethergruppe
KR102633122B1 (ko) 2014-08-01 2024-02-05 누에볼루션 에이/에스 브로모도메인에 대하여 활성을 갖는 화합물
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
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
CA3000633C (en) 2014-10-14 2023-10-03 The Regents Of The University Of California Use of cdk9 and brd4 inhibitors to inhibit inflammation
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. ASSOCIATION THERAPY USING TRANSCRIPTION INHIBITORS AND KINASE INHIBITORS
WO2017024406A1 (en) * 2015-08-11 2017-02-16 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
US10501438B2 (en) 2015-08-11 2019-12-10 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
EP3334719B1 (en) 2015-08-12 2021-09-15 Neomed Institute Substituted benzimidazoles, their preparation and their use as pharmaceuticals
CA2996974A1 (en) 2015-09-11 2017-03-16 Dana-Farber Cancer Institute, Inc. Cyano thienotriazolodiazepines and uses thereof
CR20180199A (es) 2015-09-11 2018-05-25 Dana Farber Cancer Inst Inc Acetamida tienotriazolodiazepinas y usos de las mismas
US10501459B2 (en) 2015-10-21 2019-12-10 Neomed Institute Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
CR20180336A (es) 2015-11-25 2018-08-06 Dana Farber Cancer Inst Inc Inhibidores de bromodominio bivalentes y usos de los mismos
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
HUE062234T2 (hu) 2016-06-20 2023-10-28 Incyte Corp Egy BET inhibitor kristályos szilárd halmazállapotú formái
CN109350616B (zh) 2018-12-18 2020-04-21 南华大学 I-brd9或其衍生物在制备抗癫痫药物中的应用
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN113717080A (zh) * 2021-10-09 2021-11-30 西安瑞联新材料股份有限公司 一种4-氯-2-氰基苯磺酰氯的合成方法
WO2023205251A1 (en) 2022-04-19 2023-10-26 Nuevolution A/S Compounds active towards bromodomains

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19506742A1 (de) * 1995-02-27 1996-08-29 Bayer Ag Verwendung von Chinoxalinen in Kombination mit Protease-Inhibitoren als Arzneimittel zur Behandlung von AIDS und/oder HIV-Infektionen
US7351709B2 (en) * 2004-06-09 2008-04-01 Wyeth Estrogen receptor ligands
ZA200902382B (en) * 2006-10-19 2010-08-25 Signal Pharm Llc Heteroaryl compounds, compositions thereof, and their use as protein kinase inhibitors
JP2012197231A (ja) * 2009-08-06 2012-10-18 Oncotherapy Science Ltd Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体
JP5913292B2 (ja) * 2010-05-14 2016-04-27 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 代謝を調節する組成物および方法
EP2935260A1 (de) * 2012-12-20 2015-10-28 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydropyridopyrazinone

Also Published As

Publication number Publication date
CA2895404A1 (en) 2014-06-26
TW201427981A (zh) 2014-07-16
HK1213899A1 (zh) 2016-07-15
WO2014095774A1 (de) 2014-06-26
US20160193206A1 (en) 2016-07-07
CN105229002A (zh) 2016-01-06
AR094148A1 (es) 2015-07-15
EP2935260A1 (de) 2015-10-28
JP2016504990A (ja) 2016-02-18

Similar Documents

Publication Publication Date Title
UY35205A (es) Dihidropiridopirazinonas inhibidoras de la proteína bet
PE20150729A1 (es) 2,3-benzodiazepines
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.
DOP2015000274A (es) Compuestos químicos
CL2015002301A1 (es) Acido 2-aza-biciclo[2.2.1]heptano-3-carboxílico (bencil-ciano-metil)-amidas sustituidas inhibidores de catepsina c.
CL2015000295A1 (es) Compuestos derivados de alquilpirimidina; composicion farmaceutica que los comprende; uso para el tratamiento de infecciones víricas y otras enfermedades.
BR112015022643A2 (pt) inibidores diidro-pirrolpiridinona
PE20151501A1 (es) Inhibidores de prmt5 y sus usos
EA201500926A1 (ru) Фумараты как пролекарства и их применение при лечении различных заболеваний
BR112015011456A2 (pt) compostos de aminopirimidina como inibidores de egfr mutantes contendo t790m
CR20160033A (es) Inhibidores de autotaxina que comprenden un nucleo ciclico de anillo heteroaromático-bencil-amida
CR20120283A (es) Inhibidor de bromodominio de benzodiazepina
BR112015011036A2 (pt) derivados de 2-amino-quinazolina substituídos heterocíclicos para o tratamento de infecções virais
BR112015032693A2 (pt) inibidores de bromodomínio
BR112015020118A2 (pt) derivados de 2-aminopirimidina para o tratamento de infecções virais
BR112013019011A2 (pt) inibição de il17 e ifn-gama para o tratamento de inflamação autoimune
BR112015000399A2 (pt) derivados de pirazolil pirimidina
PE20151979A1 (es) Compuestos quimicos
BR112015007366A2 (pt) derivados de acilaminopirimidina para o tratamento de infecções virais e outras doenças
CL2015000408A1 (es) Compuestos derivados de pirazolo[4,3-d]pirimidina y sus sales; composicion farmaceutica que los comprende, util para el tratamiento de enfermedades alergicas, inflamatorias, infecciosas o cancer.
CO2018002211A2 (es) Piridinona dicarboxamida para su uso como inhibidores de bromodominio
UY35654A (es) Dihidroquinoxalinonas y dihidropiridopirazinonas modificadas como inhibidores de la proteína bet
CR20150426A (es) 2,3-benzodiazepinas biciclo y espirocíclico sustituidas
EA201300863A1 (ru) Ингибирование il17 и ifn-гамма для лечения аутоиммунного воспаления
NI201200168A (es) Formulaciones farmacéuticas

Legal Events

Date Code Title Description
109 Application deemed to be withdrawn

Effective date: 20210715