CU20150163A7 - DERIVADOS DE 5-HETEROARIL-4-FENIL-4,5-DIHIDROPIRROLO(3,4-c)PIRAZOL-6-ONA ACTIVOS COMO INHIBIDORES DE BET - Google Patents

DERIVADOS DE 5-HETEROARIL-4-FENIL-4,5-DIHIDROPIRROLO(3,4-c)PIRAZOL-6-ONA ACTIVOS COMO INHIBIDORES DE BET

Info

Publication number
CU20150163A7
CU20150163A7 CUP2015000163A CU20150163A CU20150163A7 CU 20150163 A7 CU20150163 A7 CU 20150163A7 CU P2015000163 A CUP2015000163 A CU P2015000163A CU 20150163 A CU20150163 A CU 20150163A CU 20150163 A7 CU20150163 A7 CU 20150163A7
Authority
CU
Cuba
Prior art keywords
derivatives
active
dihidropirrolo
heteroaril
fenil
Prior art date
Application number
CUP2015000163A
Other languages
English (en)
Other versions
CU24350B1 (es
Inventor
Jutta Blank
Vincent Bordas
Simona Cotesta
Vito Guagnano
Heinrich Rueeger
Andrea Vaupel
Original Assignee
Novartis 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 Novartis Ag filed Critical Novartis Ag
Publication of CU20150163A7 publication Critical patent/CU20150163A7/es
Publication of CU24350B1 publication Critical patent/CU24350B1/es

Links

Classifications

    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/41921,2,3-Triazoles
    • 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
    • A61K31/423Oxazoles condensed with carbocyclic rings
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención proporciona un compuesto de la fórmula (I) (ESPACIO PARA LA FÓRMULA) o una sal farmacéuticamente aceptable del mismo, que corresponde con derivados de 5 heteroaril-4-fenil-4,5-dihidropirrolo (3,4-c)pirazol-6-ona activos como inhibidores de BET, que tienen potencial terapéutico en varias condiciones o enfermedades humanas como cáncer; composiciones farmacéuticas de los mismos y combinaciones con agentes farmacológicamente activos.
CUP2015000163A 2013-05-27 2014-05-26 DERIVADOS DE 5-HETEROARIL-4-FENIL-4,5-DIHIDROPIRROLO(3,4-c)PIRAZOL-6-ONA ACTIVOS COMO INHIBIDORES DE BET CU24350B1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13169364 2013-05-27
EP13177673 2013-07-23
PCT/IB2014/061717 WO2014191896A1 (en) 2013-05-27 2014-05-26 Pyrazolopyrrolidine derivatives and their use in the treatment of disease

Publications (2)

Publication Number Publication Date
CU20150163A7 true CU20150163A7 (es) 2016-05-30
CU24350B1 CU24350B1 (es) 2018-06-05

Family

ID=50979827

Family Applications (1)

Application Number Title Priority Date Filing Date
CUP2015000163A CU24350B1 (es) 2013-05-27 2014-05-26 DERIVADOS DE 5-HETEROARIL-4-FENIL-4,5-DIHIDROPIRROLO(3,4-c)PIRAZOL-6-ONA ACTIVOS COMO INHIBIDORES DE BET

Country Status (36)

Country Link
US (2) US8975417B2 (es)
EP (1) EP3004110B1 (es)
JP (1) JP6181862B2 (es)
KR (1) KR20160012196A (es)
CN (1) CN105408335B (es)
AU (1) AU2014272776C1 (es)
BR (1) BR112015029512A8 (es)
CA (1) CA2913223A1 (es)
CL (1) CL2015003395A1 (es)
CR (1) CR20150628A (es)
CU (1) CU24350B1 (es)
CY (1) CY1119490T1 (es)
DK (1) DK3004110T3 (es)
EA (1) EA029515B1 (es)
EC (1) ECSP15053445A (es)
ES (1) ES2651843T3 (es)
HR (1) HRP20171613T1 (es)
HU (1) HUE036674T2 (es)
IL (1) IL242610A0 (es)
LT (1) LT3004110T (es)
ME (1) ME02906B (es)
MX (1) MX364205B (es)
NO (1) NO3004110T3 (es)
PE (1) PE20160005A1 (es)
PH (2) PH12015502628B1 (es)
PL (1) PL3004110T3 (es)
PT (1) PT3004110T (es)
RS (1) RS56522B1 (es)
SG (1) SG11201509474SA (es)
SI (1) SI3004110T1 (es)
SV (1) SV2015005115A (es)
TN (1) TN2015000505A1 (es)
UA (1) UA116017C2 (es)
UY (1) UY35586A (es)
WO (1) WO2014191896A1 (es)
ZA (1) ZA201508259B (es)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104321325B (zh) 2012-05-24 2016-11-16 诺华股份有限公司 吡咯并吡咯烷酮化合物
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
WO2014096965A2 (en) 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2014115080A1 (en) 2013-01-22 2014-07-31 Novartis Ag Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction
MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
ES2656471T3 (es) * 2013-05-28 2018-02-27 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona como inhibidores de BET y su uso en el tratamiento de enfermedades
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
SG11201510409QA (en) 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
AU2014337064B2 (en) 2013-10-18 2019-03-14 Celgene Quanticel Research, Inc. Bromodomain 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
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
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
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
JP2017537946A (ja) 2014-12-11 2017-12-21 ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. ブロモドメイン阻害剤としての置換複素環
HK1245247A1 (zh) 2014-12-17 2018-08-24 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
JP2018527340A (ja) 2015-08-11 2018-09-20 ネオメド インスティテュートNeomed Institute アリール置換ジヒドロキノリノン、その調製及び医薬品としてのその使用
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
CA2994478C (en) 2015-08-12 2023-10-03 Neomed Institute Substituted benzimidazoles, their preparation and their use as pharmaceuticals
US10501459B2 (en) 2015-10-21 2019-12-10 Neomed Institute Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
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
CN109153647A (zh) 2016-02-15 2019-01-04 分子医学研究中心责任有限公司 用于治疗癌症的taf1抑制剂
CN118436801A (zh) 2016-05-20 2024-08-06 豪夫迈·罗氏有限公司 Protac抗体缀合物及其使用方法
TW201803594A (zh) * 2016-06-09 2018-02-01 達納-法伯癌症協會 Hdac抑制劑與bet抑制劑之使用方法及醫藥組合
AU2017281286B2 (en) 2016-06-20 2021-05-20 Incyte Corporation Crystalline solid forms of a bet inhibitor
HUE057289T2 (hu) 2016-08-31 2022-05-28 Jiangsu Hengrui Medicine Co Oxopikolinamid-származék, annak elõállítási módszere és gyógyszerészeti felhasználása
CN110225755A (zh) 2016-11-14 2019-09-10 分子医学研究中心责任有限公司 Brd4抑制剂和抗叶酸剂的组合用于治疗癌症
CN109232301B (zh) * 2018-10-15 2021-01-01 天津希恩思生化科技有限公司 一种四异丙基肼的制备方法
JP2022053557A (ja) * 2019-02-08 2022-04-06 マルホ株式会社 ピリドン誘導体
MX2022000521A (es) * 2019-07-12 2022-06-14 Scenic Immunology B V Compuestos n-sustituidos-3,4-(5-anillo fusionado)-5-fenil-pirrolid in-2-ona como inhibidores de la enzima isoqc y/o qc.
WO2021065980A1 (ja) 2019-09-30 2021-04-08 協和キリン株式会社 Bet分解剤
CN112625036A (zh) * 2019-10-08 2021-04-09 上海海和药物研究开发股份有限公司 一类具有brd4抑制活性的化合物、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
WO2022155859A1 (en) * 2021-01-21 2022-07-28 Beijing Tiantan Hospital Modulators of fpr1 and methods of using the same
US12527741B2 (en) 2021-06-17 2026-01-20 Wisconsin Alumni Research Foundation Modular dendron micelles for treatment of pulmonary diseases related to fibrosis and viral infection including COVID-19
JP2024528175A (ja) 2021-08-02 2024-07-26 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 殺微生物ピラゾール誘導体
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same
EP4447682A1 (en) 2021-12-17 2024-10-23 Syngenta Crop Protection AG Microbiocidal pyrazole derivatives
EP4532495A1 (en) 2022-05-30 2025-04-09 Adorx therapeutics Limited Cd73 inhibitor compounds
TW202430514A (zh) 2022-09-30 2024-08-01 瑞士商先正達農作物保護股份公司 殺微生物之吡唑衍生物
PY2403614A (es) 2023-01-27 2025-09-11 Syngenta Crop Prot Ag Derivados de pirazol microbiocidas
PY2404467A (es) 2023-02-01 2025-03-31 Syngenta Crop Prot Ag Composiciones fungicidas
WO2024240858A1 (en) 2023-05-23 2024-11-28 Valerio Therapeutics Protac molecules directed against dna damage repair system and uses thereof
PY2447478A (es) 2023-06-14 2025-03-18 Syngenta Crop Prot Ag Composiciones fungicidas
WO2025114167A1 (en) 2023-11-28 2025-06-05 Syngenta Crop Protection Ag Microbiocidal pyrazole derivatives
WO2025163143A1 (en) 2024-02-02 2025-08-07 Syngenta Crop Protection Ag Microbiocidal pyrazole derivatives
WO2025191053A1 (en) 2024-03-14 2025-09-18 Syngenta Crop Protection Ag Microbiocidal pyrazole derivatives
WO2026022173A1 (en) 2024-07-26 2026-01-29 Syngenta Crop Protection Ag Microbiocidal pyrazole compounds

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5508300A (en) 1994-01-14 1996-04-16 Pfizer Inc. Dihydro pyrazolopyrroles, compositions and use
KR100904157B1 (ko) 2000-08-10 2009-06-23 파마시아 이탈리아 에스.피.에이. 키나제 억제제로서 활성인 비사이클로-피라졸, 이의제조방법 및 이를 포함하는 약제학적 조성물
SK287857B6 (sk) * 2001-05-24 2012-01-04 Eli Lilly And Company Novel pyrrole derivatives as pharmaceutical agents
DE60225719T2 (de) 2001-12-18 2009-04-23 F. Hoffmann-La Roche Ag Cis-2,4,5- triphenyl-imidazoline und ihre verwendung bei der behandlung von tumoren
US20060189511A1 (en) 2002-05-13 2006-08-24 Koblish Holly K Method for cytoprotection through mdm2 and hdm2 inhibition
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
MXPA06013246A (es) 2004-05-18 2007-02-08 Hoffmann La Roche Nuevas imidazolinas cis.
US20060069085A1 (en) 2004-09-28 2006-03-30 Rulin Zhao Preparation of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
EP1833807A1 (en) 2005-01-05 2007-09-19 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
JP5222731B2 (ja) 2005-12-12 2013-06-26 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害薬として活性な置換ピロロ−ピラゾール誘導体
WO2007096334A1 (en) 2006-02-24 2007-08-30 Pfizer Italia Srl Pyrrolopyrrolones active as kinase inhibitors
US8367699B2 (en) 2006-09-15 2013-02-05 Nexuspharma, Inc. Tetrahydro-isoquinolines
TW200843739A (en) 2007-03-30 2008-11-16 Shionogi & Co Novel pyrrolinone derivative and composition containing the same
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
UY31982A (es) 2008-07-16 2010-02-26 Boehringer Ingelheim Int Derivados de 1,2-dihidropiridin-3-carboxamidas n-sustituidas
WO2010035727A1 (ja) 2008-09-25 2010-04-01 塩野義製薬株式会社 新規ピロリノン誘導体およびそれを含有する医薬組成物
US20120208204A1 (en) 2009-06-03 2012-08-16 The Brigham And Women's Hospital, Inc. Compositions and Methods for Inhibiting Tumor Growth
GB0919423D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
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
US9085582B2 (en) 2010-06-22 2015-07-21 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
US20120065210A1 (en) 2010-09-15 2012-03-15 Xin-Jie Chu Substituted hexahydropyrrolo[1,2-c]imidazolones
GB201016880D0 (en) 2010-10-07 2010-11-17 Riotech Pharmaceuticals Ltd Phosphodiesterase inhibitors
AR084070A1 (es) * 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012151512A2 (en) 2011-05-04 2012-11-08 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
US9328117B2 (en) 2011-06-17 2016-05-03 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012175487A1 (en) 2011-06-20 2012-12-27 Novartis Ag Cyclohexyl isoquinolinone compounds
US8859535B2 (en) 2011-06-20 2014-10-14 Novartis Ag Hydroxy substituted isoquinolinone derivatives
GB2492950A (en) 2011-07-11 2013-01-23 Cambridge Consultants Measuring a luminescent property of a sample using a dual-modulated excitation beam
WO2013033270A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same
WO2013080141A1 (en) 2011-11-29 2013-06-06 Novartis Ag Pyrazolopyrrolidine compounds
US8815926B2 (en) 2012-01-26 2014-08-26 Novartis Ag Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases
CN104321325B (zh) 2012-05-24 2016-11-16 诺华股份有限公司 吡咯并吡咯烷酮化合物

Also Published As

Publication number Publication date
JP6181862B2 (ja) 2017-08-16
PH12015502628A1 (en) 2016-03-07
HRP20171613T1 (hr) 2017-12-01
NO3004110T3 (es) 2017-12-23
ECSP15053445A (es) 2017-10-31
HK1216251A1 (en) 2016-10-28
CN105408335B (zh) 2017-11-17
TN2015000505A1 (en) 2017-04-06
CU24350B1 (es) 2018-06-05
BR112015029512A8 (pt) 2019-12-17
PE20160005A1 (es) 2016-01-21
LT3004110T (lt) 2017-11-10
CL2015003395A1 (es) 2016-05-20
WO2014191896A1 (en) 2014-12-04
ES2651843T3 (es) 2018-01-30
AU2014272776B2 (en) 2016-11-10
EA201592250A1 (ru) 2016-05-31
US20140349990A1 (en) 2014-11-27
MX364205B (es) 2019-04-16
RS56522B1 (sr) 2018-02-28
ME02906B (me) 2018-04-20
UA116017C2 (uk) 2018-01-25
UY35586A (es) 2014-12-31
SV2015005115A (es) 2018-04-04
SG11201509474SA (en) 2015-12-30
CY1119490T1 (el) 2018-03-07
EA029515B1 (ru) 2018-04-30
BR112015029512A2 (pt) 2017-07-25
PL3004110T3 (pl) 2017-12-29
DK3004110T3 (da) 2017-11-06
CR20150628A (es) 2016-01-29
AU2014272776A1 (en) 2015-12-03
SI3004110T1 (sl) 2017-11-30
PH12015502628B1 (en) 2016-03-07
US8975417B2 (en) 2015-03-10
PH12018501807A1 (en) 2019-03-25
EP3004110A1 (en) 2016-04-13
PT3004110T (pt) 2017-11-08
CN105408335A (zh) 2016-03-16
EP3004110B1 (en) 2017-07-26
AU2014272776C1 (en) 2017-06-01
IL242610A0 (en) 2016-02-01
HUE036674T2 (hu) 2018-07-30
MX2015016416A (es) 2016-03-03
JP2016520117A (ja) 2016-07-11
KR20160012196A (ko) 2016-02-02
CA2913223A1 (en) 2014-12-04
US20160095843A1 (en) 2016-04-07
ZA201508259B (en) 2017-01-25

Similar Documents

Publication Publication Date Title
CU20150163A7 (es) DERIVADOS DE 5-HETEROARIL-4-FENIL-4,5-DIHIDROPIRROLO(3,4-c)PIRAZOL-6-ONA ACTIVOS COMO INHIBIDORES DE BET
CL2018000318A1 (es) Compuestos derivados de piridinona, inhibidores de bromodominio; composición farmacéutica que los comprende; y su uso en el tratamiento de enfermedades del cáncer. (solicitud divisional 201600925)
MX383686B (es) Derivados de piridazina 1,4-disustituida, y su uso para el tratamiento de afecciones relacionadas con la deficiencia de smn.
CU20160087A7 (es) Indazolcarboxamidas, procedimientos para su preparación, preparaciones farmacéuticas que las contienen
NI201300041A (es) Antagonistas de mdm2 de espiro-oxindol
PH12016500024A1 (en) Bromodomain inhibitor
BR112015020389A8 (pt) compostos carbazol úteis como inibidores de bromodomínio, seu uso, bem como composição e produto farmacêuticos compreendendo os mesmos
CU20150014A7 (es) Análogos de piridazina 1,4-disustituida y métodos para el tratamiento de condiciones relacionadas con la deficiencia de smn
MX2020001550A (es) Terapia de combinacion que incluye un inhibidor mdm2 y uno o mas agentes farmaceuticamente activos adicionales para el tratamiento de canceres.
DOP2016000071A (es) Inhibidores de tirosina cinasa de bruton
GT201200147A (es) Antagonistas de espiro-oxindol de mdm2
UY35353A (es) Un inhibidor de mdm2 derivado de ácido benzoico para el tratamiento del cáncer
MX391858B (es) Compuestos terapeuticamente activos y sus metodos de uso
MX2016008201A (es) Tratamiento del cancer usando combinaciones de inhibidores de erk y raf.
BR112016002287A2 (pt) compostos terapeuticamente ativos e seus métodos de uso
MX2015016421A (es) Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades.
MX2015016425A (es) Derivados de pirazolo-pirrolidin-4-ona y su uso en el tratamiento de enfermedades.
CL2017000845A1 (es) Inhibidores de gingipaina de lisina
CL2015002466A1 (es) Formulaciones de compuestos orgánicos
UY35209A (es) Compuestos tricíclicos
MX2019004484A (es) Derivados de naftiridinona y su uso en el tratamiento de la arritmia.
BR112015029894A2 (pt) forma de dosagem farmacêutica sólida
MX2015012153A (es) Inhibidores de la quinasa pirrolopirimidina cdk9.
BR112014030288A8 (pt) composição farmacêutica, uso da mesma, e, uso de metanossulfonilacetonitrila
NI201200196A (es) Agentes terapéuticos 976