[go: up one dir, main page]

SG11201608843TA - 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS - Google Patents

1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS

Info

Publication number
SG11201608843TA
SG11201608843TA SG11201608843TA SG11201608843TA SG11201608843TA SG 11201608843T A SG11201608843T A SG 11201608843TA SG 11201608843T A SG11201608843T A SG 11201608843TA SG 11201608843T A SG11201608843T A SG 11201608843TA SG 11201608843T A SG11201608843T A SG 11201608843TA
Authority
SG
Singapore
Prior art keywords
pyridin
ones
pyrazolo
pyrrolo
inhibitors
Prior art date
Application number
SG11201608843TA
Inventor
Andrew P Combs
Thomas P Maduskuie Jr
Nikoo Falahatpisheh
Original Assignee
Incyte Corp
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=53055117&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG11201608843T(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of SG11201608843TA publication Critical patent/SG11201608843TA/en

Links

Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biotechnology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Otolaryngology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
SG11201608843TA 2014-04-23 2015-04-22 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS SG11201608843TA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461983289P 2014-04-23 2014-04-23
PCT/US2015/027047 WO2015164480A1 (en) 2014-04-23 2015-04-22 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS

Publications (1)

Publication Number Publication Date
SG11201608843TA true SG11201608843TA (en) 2016-11-29

Family

ID=53055117

Family Applications (2)

Application Number Title Priority Date Filing Date
SG10201809353TA SG10201809353TA (en) 2014-04-23 2015-04-22 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
SG11201608843TA SG11201608843TA (en) 2014-04-23 2015-04-22 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS

Family Applications Before (1)

Application Number Title Priority Date Filing Date
SG10201809353TA SG10201809353TA (en) 2014-04-23 2015-04-22 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS

Country Status (38)

Country Link
US (8) US9540368B2 (en)
EP (3) EP3674302B1 (en)
JP (2) JP6572237B2 (en)
KR (3) KR102702503B1 (en)
CN (1) CN106414442B (en)
AR (1) AR100160A1 (en)
AU (3) AU2015249810B2 (en)
BR (1) BR112016024626B1 (en)
CA (1) CA2946731C (en)
CL (1) CL2016002681A1 (en)
CR (2) CR20200231A (en)
CY (2) CY1122948T1 (en)
DK (2) DK3134403T3 (en)
EA (2) EA039678B1 (en)
EC (1) ECSP16088983A (en)
ES (2) ES2942723T3 (en)
FI (1) FI3674302T3 (en)
HR (2) HRP20230340T1 (en)
HU (2) HUE061770T2 (en)
IL (3) IL248415B (en)
LT (2) LT3134403T (en)
MA (1) MA39985B1 (en)
ME (1) ME03763B (en)
MX (2) MX376174B (en)
MY (3) MY180775A (en)
NZ (3) NZ763737A (en)
PE (1) PE20170144A1 (en)
PH (1) PH12016502115B1 (en)
PL (2) PL3134403T3 (en)
PT (2) PT3134403T (en)
RS (2) RS64231B1 (en)
SG (2) SG10201809353TA (en)
SI (2) SI3134403T1 (en)
SM (2) SMT202000133T1 (en)
TW (2) TWI672301B (en)
UA (1) UA119870C2 (en)
WO (1) WO2015164480A1 (en)
ZA (1) ZA202101718B (en)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX366703B (en) 2013-03-15 2019-07-22 Incyte Holdings Corp Tricyclic heterocycles as bet protein inhibitors.
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 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
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
KR102702503B1 (en) 2014-04-23 2024-09-05 인사이트 홀딩스 코포레이션 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
MA40940A (en) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc SUBSTITUTED PYRROLOPYRIDINES USED AS BROMODOMA INHIBITORS
MA40943A (en) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc SUBSTITUTED PYRROLOPYRIDINES USED AS BROMODOMA INHIBITORS
WO2016077375A1 (en) 2014-11-10 2016-05-19 Genentech, Inc. Bromodomain inhibitors and uses thereof
CN107531692B (en) 2015-01-29 2020-12-25 基因泰克公司 Therapeutic compounds and uses thereof
AR104259A1 (en) * 2015-04-15 2017-07-05 Celgene Quanticel Res Inc BROMODOMINUM INHIBITORS
AU2016305513A1 (en) 2015-08-11 2018-03-08 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
WO2017024406A1 (en) * 2015-08-11 2017-02-16 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
JP6912039B2 (en) 2015-08-12 2021-07-28 ネオメド インスティテュート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
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
US10519151B2 (en) 2016-01-28 2019-12-31 Neomed Institute Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals
CA3018802A1 (en) 2016-04-15 2017-10-19 Abbvie Inc. Bromodomain inhibitors
PH12021551886A1 (en) 2016-06-20 2023-07-17 Incyte Corp Crystalline solid forms of a bet inhibitor
EP3539960A4 (en) 2016-11-10 2020-03-18 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Nitrogenous macrocyclic compound, preparation method therefor, pharmaceutical composition and application thereof
TW201825490A (en) * 2017-01-11 2018-07-16 大陸商江蘇豪森藥業集團有限公司 Pyrrolo[2,3-c]pyridine derivatives, preparation methods and pharmaceutical uses thereof
MX2020000690A (en) 2017-07-18 2020-07-29 Nuvation Bio Inc Heterocyclic compounds as adenosine antagonists.
BR112020000962A2 (en) 2017-07-18 2020-07-14 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
US11180510B2 (en) 2017-11-06 2021-11-23 Centre National De La Recherche Scientifique Xanthine derivatives and uses thereof as inhibitors of bromodomains of BET proteins
MX2020006612A (en) * 2017-12-20 2020-11-09 Betta Pharmaceuticals Co Ltd Compound functioning as bromodomain protein inhibitor, and composition.
EP3728207B1 (en) 2017-12-21 2023-02-01 Ribon Therapeutics Inc. Quinazolinones as parp14 inhibitors
CA3090439A1 (en) * 2018-02-06 2019-08-15 Shanghai Haihe Pharmaceutical Co., Ltd. Compound having bet inhibitory activity and preparation method and use therefor
CN110776508B (en) 2018-07-27 2021-07-16 海创药业股份有限公司 BRD4 inhibitor and preparation method and application thereof
CN109580433B (en) * 2018-10-26 2021-05-28 中国辐射防护研究院 Source term estimation method for diffusion of conventional explosive radioactive aerosol
AU2019372121A1 (en) 2018-10-30 2021-05-27 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
CN109432093A (en) * 2018-12-23 2019-03-08 黄泳华 The synergy system for the acetylcholinesterase inhibitor being made of Pyrazolopyridine ketone compounds
EP3911323A4 (en) 2019-01-18 2022-11-16 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS AS ADENOSIN ANTAGONISTS
CA3126931A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
BR112021018372A2 (en) * 2019-03-17 2021-11-23 Shanghai Ringene Biopharma Co Ltd Acylaminopyrrolo-pyridone compound, method for preparing said compound, pharmaceutical composition and use thereof
GB201905721D0 (en) 2019-04-24 2019-06-05 Univ Dundee Compounds
CN110003204B (en) * 2019-04-30 2020-08-11 上海勋和医药科技有限公司 A kind of BET protein inhibitor, its preparation method and use
CN112094266B (en) * 2019-06-17 2023-03-21 中国科学院上海药物研究所 Pyrrolopyridinone compound, preparation method, composition and application thereof
CN114206853A (en) * 2019-06-19 2022-03-18 里邦医疗公司 Targeted protein degradation of PARP14 for therapy
KR102677015B1 (en) 2019-07-02 2024-06-19 누베이션 바이오 인크. Heterocyclic Compounds as BET Inhibitors
CN112625036A (en) * 2019-10-08 2021-04-09 上海海和药物研究开发股份有限公司 Compound with BRD4 inhibitory activity, preparation method and application thereof
PE20221283A1 (en) 2019-12-27 2022-09-05 Lupin Ltd SUBSTITUTED TRICYCLIC COMPOUNDS
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CA3184633A1 (en) * 2020-06-03 2021-12-09 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022116968A1 (en) 2020-12-01 2022-06-09 成都苑东生物制药股份有限公司 Novel n-heterocyclic bet bromodomain inhibitor, and preparation method therefor and medical use thereof
WO2022132049A1 (en) * 2020-12-17 2022-06-23 National University Of Singapore Treating cancers using bet inhibitors
US20240366608A1 (en) 2021-01-19 2024-11-07 Lupin Limited Pharmaceutical combinations of sos1 inhibitors for treating and/or preventing cancer
GB2641636A (en) * 2022-12-23 2025-12-10 Tay Therapeutics Ltd Selective BET inhibitors and uses thereof

Family Cites Families (169)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2404E (en) 1899-12-05 1904-03-26 Louis Olivier Victor Parmentie Letter copy machine
JPS59170313A (en) 1983-03-14 1984-09-26 Kurimoto Iron Works Ltd Screen gate
JPS6053449A (en) 1983-09-01 1985-03-27 M K Seikou Kk Car washer
JPS6085739U (en) 1983-11-18 1985-06-13 クラリオン株式会社 Pinch roller device in tape recorder
JPS6243003U (en) 1985-09-05 1987-03-14
JPH0314566A (en) 1989-06-09 1991-01-23 Sankyo Co Ltd Benzimidazole derivative
US5244912A (en) 1991-03-28 1993-09-14 Eli Lilly And Company 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz(cd)indoles and pharmaceutical use thereof
FR2710915B1 (en) 1993-10-04 1995-11-24 Synthelabo Piperidine derivatives, their preparation and their therapeutic use.
GB9410469D0 (en) 1994-05-25 1994-07-13 Erba Farmitalia Imidazolylalkyl derivatives of imidazo (5,1-c) (1,4) benzoxazin-1-one and process for their preparation
FR2731708B1 (en) 1995-03-13 1997-04-30 Synthelabo PIPERIDINE DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR THERAPEUTIC APPLICATION
FR2747678B1 (en) 1996-04-22 1998-05-22 Synthelabo COMPOUNDS DERIVED FROM IMIDAZOBENZOXAZINE, PROCESSES FOR THEIR PREPARATION AND THERAPEUTIC USES
US6287693B1 (en) 1998-02-25 2001-09-11 John Claude Savoir Stable shaped particles of crystalline organic compounds
CA2405565A1 (en) 2000-04-21 2001-11-01 Pharmacia & Upjohn Company Compounds for treating fibromyalgia and chronic fatigue syndrome
JP4188078B2 (en) 2000-06-28 2008-11-26 スミスクライン ビーチャム ピー エル シー Wet grinding method
CZ294493B6 (en) 2000-08-08 2005-01-12 Sanofi-Synthelabo Benzimidazole derivatives, process of their preparation and medicinal compositions in which the derivatives are comprised
FR2816619B1 (en) 2000-11-15 2003-01-31 Sanofi Synthelabo BENZIMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
US6919334B2 (en) 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
RU2342388C2 (en) 2002-11-22 2008-12-27 Джапан Тобакко Инк. Condensing dicyclic nitrogen containing heterocycles, which have dgat inhibiting action
EP1462103A1 (en) 2003-03-25 2004-09-29 Faust Pharmaceuticals NO donors, combination products and uses as modulators of neurotransmitter release
AU2005214258A1 (en) 2004-02-23 2005-09-01 Dainippon Sumitomo Pharma Co., Ltd. Novel heterocyclic compound
JP4790703B2 (en) 2004-04-07 2011-10-12 武田薬品工業株式会社 Cyclic compounds
US7713954B2 (en) 2004-09-30 2010-05-11 Roche Palo Alto Llc Compositions and methods for treating cognitive disorders
DE102005011058A1 (en) 2005-03-10 2006-09-14 Merck Patent Gmbh Substituted tetrahydro-pyrrolo-quinoline derivatives
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
WO2006129623A1 (en) 2005-05-30 2006-12-07 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and a medicinal use thereof
US20080318999A1 (en) 2005-08-05 2008-12-25 Methvin Isaac Tricyclic Benzimidazoles and Their Use as Metabotropic Glutamate Receptor Modulators
US8975259B2 (en) 2007-04-27 2015-03-10 University Of Rochester Compositions and methods for inhibiting G protein signaling
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
WO2009020559A2 (en) 2007-08-03 2009-02-12 The J. David Gladstone Institutes Agents that inhibit p-tefb interactions and methods of use thereof
JP5478262B2 (en) 2007-12-28 2014-04-23 田辺三菱製薬株式会社 Anticancer drug
DE102008052618A1 (en) 2008-10-21 2010-04-22 Henkel Ag & Co. Kgaa Tricyclic aldehydes and C, H-acidic compounds
WO2010111626A2 (en) 2009-03-27 2010-09-30 Takeda Pharmaceutical Company Limited Poly (adp-ribose) polymerase (parp) inhibitors
TW201103941A (en) 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
TW201105681A (en) 2009-06-10 2011-02-16 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
WO2011024987A1 (en) 2009-08-31 2011-03-03 塩野義製薬株式会社 Aromatic fused heterocyclic derivative and pharmaceutical composition containing same
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
WO2011054851A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Novel process
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
HUE026967T2 (en) 2009-11-05 2016-07-28 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
DK2722334T3 (en) 2009-11-05 2016-03-07 Glaxosmithkline Llc benzodiazepine bromdomæneinhibitor
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
BR112012026641A2 (en) 2010-04-23 2016-07-12 Kineta Inc antiviral compounds
JP5913292B2 (en) 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 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
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
ES2526671T3 (en) 2010-06-22 2015-01-14 Glaxosmithkline Llc Compounds of benzotriazoldiazepine bromodomain inhibitors
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (en) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc BROMODOMINIUM INHIBITORS AND USES OF THE SAME
BR112013020329A2 (en) 2011-02-09 2016-08-02 Hoffmann La Roche heterocyclic compounds as pi3 kinase inhibitors
CA2828212A1 (en) 2011-02-23 2012-08-30 Shiraz Mujtaba Inhibitors of bromodomains as modulators of gene expression
CA2825966A1 (en) 2011-03-21 2012-09-27 F. Hoffmann-La Roche Ag Benzoxazepin compounds selective for pi3k p110 delta and methods of use
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2706852B1 (en) 2011-05-10 2018-08-22 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
WO2012174487A2 (en) 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012178208A2 (en) 2011-06-24 2012-12-27 The Trustees Of The Stevens Institute Of Technology Selective inhibitors of histone deacetylase isoform 6 and methods thereof
JP2013010719A (en) 2011-06-30 2013-01-17 Dainippon Sumitomo Pharma Co Ltd Benzimidazolone and oxindole derivative, and pharmaceutical application of them
CA2843643A1 (en) 2011-07-29 2013-02-07 The Children's Hospital Of Philadelphia Compositions and methods for the treatment of hiv
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033270A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
SI2751083T1 (en) 2011-08-31 2018-04-30 Otsuka Pharmaceutical Co., Ltd. Quinolone compound
DE102011082013A1 (en) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-thieno [3,2-f] [1,2,4] triazolo [4,3-a] [1,4] diazepines
ES2632443T3 (en) 2011-09-22 2017-09-13 Viiv Healthcare Uk Limited Pyrrolopyridinone compounds and HIV treatment procedures
CN103857391B (en) 2011-09-30 2016-06-08 沈阳蓝桑医药生物技术研发有限公司 Pharmaceutical composition containing religactone and its application
WO2013060636A1 (en) 2011-10-25 2013-05-02 Sanofi 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
AU2012330885B2 (en) 2011-11-01 2016-10-06 Resverlogix Corp. Oral immediate release formulations for substituted quinazolinones
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
WO2013148197A1 (en) 2012-03-28 2013-10-03 The J. David Gladstone Institutes Compositions and methods for reactivating latent immunodeficiency virus
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281396A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
WO2013155695A1 (en) 2012-04-20 2013-10-24 Abbott Laboratories Isoindolone derivatives
TWI602820B (en) 2012-06-06 2017-10-21 星宿藥物公司 Bromodomain inhibitors and uses thereof
US9624244B2 (en) 2012-06-06 2017-04-18 Constellation Pharmaceuticals, Inc. Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof
SG11201408324QA (en) 2012-06-12 2015-01-29 Abbvie Inc Pyridinone and pyridazinone derivatives
BR112014032105A2 (en) 2012-06-25 2017-08-01 Oncoethix Sa method for cancer treatment
US9610332B2 (en) 2012-07-18 2017-04-04 Massachusetts Institute Of Technology Compositions and methods for modulating BRD4 bioactivity
CA2880578A1 (en) 2012-08-16 2014-02-20 Glaxosmithkline Llc Benzodiazepines for treating small cell lung cancer
WO2014026997A1 (en) 2012-08-16 2014-02-20 Bayer Pharma Aktiengesellschaft 2,3-benzodiazepines
HK1208448A1 (en) 2012-09-28 2016-03-04 Bayer Pharma Aktiengesellschaft Bet protein-inhibiting 5-aryl triazole azepines
KR20150100613A (en) 2012-09-28 2015-09-02 온코에틱스 게엠베하 Pharmaceutical formulation containing thienotriazolodiazepine compounds
WO2014074775A1 (en) 2012-11-09 2014-05-15 Jacobus Pharmaceutical Company, Inc. Heteroaryl derivatives and uses thereof
US9422290B2 (en) 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
ES2625945T3 (en) 2012-11-14 2017-07-21 Glaxosmithkline Llc Thieno [3,2-c] pyridin-4 (5H) -ones as bet inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014095775A1 (en) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydroquinoxalinones
EP2935260A1 (en) 2012-12-20 2015-10-28 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydropyridopyrazinones
CA2895905A1 (en) 2012-12-21 2014-06-26 Zenith Epigenetics Corp. Novel heterocyclic compounds as bromodomain inhibitors
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
US10053454B2 (en) 2013-02-27 2018-08-21 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
AU2014249192B2 (en) 2013-03-11 2017-12-21 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
JP2016512524A (en) 2013-03-11 2016-04-28 アッヴィ・インコーポレイテッド Bromodomain inhibitor
US8980879B2 (en) 2013-03-11 2015-03-17 Abbvie Inc. Bromodomain inhibitors
AU2014248663A1 (en) 2013-03-12 2015-09-24 Abbvie Inc. Dihydro-pyrrolopyridinone bromodomain inhibitors
JP6419735B2 (en) 2013-03-12 2018-11-07 アッヴィ・インコーポレイテッド Tetracyclic bromodomain inhibitors
CA2905426A1 (en) 2013-03-12 2014-10-09 Abbvie Inc. Pyrrole amide inhibitors
US9695179B2 (en) 2013-03-14 2017-07-04 Convergene Llc Methods and compositions for inhibition of bromodomain-containing proteins
KR20150128842A (en) 2013-03-14 2015-11-18 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 Furopyridines as bromodomain inhibitors
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
SMT201900009T1 (en) 2013-03-14 2019-02-28 Glaxosmithkline Ip No 2 Ltd 2,3-disubstituted 1-acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
KR102244719B1 (en) 2013-03-15 2021-04-26 플렉시콘 인코퍼레이티드 Heterocyclic compounds and uses thereof
MX366703B (en) 2013-03-15 2019-07-22 Incyte Holdings Corp Tricyclic heterocycles as bet protein inhibitors.
WO2014152029A2 (en) 2013-03-15 2014-09-25 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
US9199988B2 (en) 2013-03-27 2015-12-01 Boehringer Ingelheim International Gmbh Dihydroquinazolinone analogues
EP2978757B1 (en) 2013-03-27 2017-02-08 Boehringer Ingelheim International GmbH Indolinone analogues as brd4 inhibitors
TWI530499B (en) 2013-03-28 2016-04-21 吉李德科學股份有限公司 Benzimidazolone derivatives as bromodomain inhibitors
EP2996689A1 (en) 2013-04-17 2016-03-23 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
HK1217484A1 (en) 2013-04-26 2017-01-13 百济神州有限公司 Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
TWI527811B (en) 2013-05-09 2016-04-01 吉李德科學股份有限公司 Benzimidazole derivatives as bromodomain inhibitors
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
EA029312B1 (en) 2013-05-27 2018-03-30 Новартис Аг Imidazopyrrolidinone derivatives and their use in the treatment of diseases
KR20160012197A (en) 2013-05-28 2016-02-02 노파르티스 아게 Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease
MX2015016421A (en) 2013-05-28 2016-03-03 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease.
CA2915419A1 (en) 2013-06-17 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted phenyl-2,3-benzodiazepines
ITMI20130991A1 (en) 2013-06-17 2014-12-18 Industrie De Nora Spa CURRENT MEASUREMENT SYSTEM PRESENT IN ELECTRODES IN INTERCONNECTED ELECTROLYTIC CELLS.
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
PL3010503T3 (en) 2013-06-21 2020-08-24 Zenith Epigenetics Ltd. Novel bicyclic bromodomain inhibitors
AR096758A1 (en) 2013-06-28 2016-02-03 Abbvie Inc BROMODOMINIUM CRYSTAL INHIBITORS
JP2016525503A (en) 2013-06-28 2016-08-25 アッヴィ・インコーポレイテッド Bromodomain inhibitor
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
PL3022191T3 (en) 2013-07-16 2017-08-31 Basf Se Herbicidal azines
CA2918910A1 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
KR101672096B1 (en) 2013-09-30 2016-11-02 주식회사 엘지화학 Heterocyclic compound and organic light emitting device comprising the same
HRP20200341T1 (en) 2013-10-18 2020-06-12 Celgene Quanticel Research, Inc. BROMODOMENE (BET) 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
US20150148372A1 (en) 2013-11-26 2015-05-28 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9428514B2 (en) 2013-12-09 2016-08-30 Abbvie Inc. Bromodomain inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
US9822107B2 (en) 2013-12-20 2017-11-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
SG11201604916YA (en) 2014-01-09 2016-07-28 Orion Corp Bicyclic heterocyclic derivatives as bromodomain inhibitors
CA2940554A1 (en) 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
KR102702503B1 (en) 2014-04-23 2024-09-05 인사이트 홀딩스 코포레이션 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
CR20160545A (en) 2014-04-23 2017-03-31 Basf Se DIAMINOTRIAZINE COMPOUNDS AS HERBICIDES
KR102349237B1 (en) 2014-04-23 2022-01-07 다케다 야쿠힌 고교 가부시키가이샤 Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease
JP2017514909A (en) 2014-05-02 2017-06-08 オンコエシックス ゲーエムベーハー Method for treating acute myeloid leukemia and / or acute lymphoblastic leukemia using thienotriazolodiazepine compound
WO2015168555A1 (en) 2014-05-02 2015-11-05 Oncoethix Sa Method of treating resistant non-hodgkin lymphoma, medulloblastoma, and/or alk+non-small cell lung cancer using thienotriazolodiazepine compounds
WO2015169953A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating glioma using thienotriazolodiazepine compounds
MX2016014574A (en) 2014-05-08 2017-02-23 Oncoethix Gmbh Method of treating triple-negative breast cancer using thienotriazolodiazepine compounds.
WO2015184257A2 (en) 2014-05-30 2015-12-03 Icahn School Of Medicine At Mount Sinai Small molecule transcription modulators of bromodomains
LT3157928T (en) 2014-06-20 2019-05-27 Constellation Pharmaceuticals, Inc. Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
CN110511209B (en) 2014-10-24 2022-07-05 百时美施贵宝公司 Indole carboxamide compounds useful as kinase inhibitors
MA40943A (en) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc SUBSTITUTED PYRROLOPYRIDINES USED AS BROMODOMA INHIBITORS
WO2016123709A1 (en) 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins
WO2016186453A1 (en) 2015-05-20 2016-11-24 Kainos Medicine, Inc. Quinoline derivatives as bromodomain inhibitors
MA43120A (en) 2015-05-29 2018-09-05 Shionogi & Co NITROGEN CONTAINING TRICYCLIC DERIVATIVE WITH HIV REPLICATION INHIBITOR ACTIVITY
CN105039258B (en) 2015-07-03 2018-04-17 北京大学 Method and composition by non-neuronal cell reprogramming for neuron cell
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN105254635A (en) 2015-10-30 2016-01-20 中国药科大学 Imidazo pyrazine compound, medicine composition of imidazo pyrazine compound and purpose of imidazo pyrazine compound
US20170127985A1 (en) 2015-11-11 2017-05-11 Medtronic Minimed, Inc. Sensor set
WO2017103670A1 (en) 2015-12-14 2017-06-22 Zenith Epigenetics Lid. 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors
US10519151B2 (en) 2016-01-28 2019-12-31 Neomed Institute Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals
WO2017133681A1 (en) 2016-02-05 2017-08-10 正大天晴药业集团股份有限公司 Tricyclic compound for bromodomain-containing protein inhibitor and preparation, pharmaceutical composition, and application thereof
PH12021551886A1 (en) 2016-06-20 2023-07-17 Incyte Corp Crystalline solid forms of a bet inhibitor
CN108069958A (en) 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 A kind of nitrogen-containing hetero cyclics, its preparation method, pharmaceutical composition and application

Also Published As

Publication number Publication date
EP4218766A1 (en) 2023-08-02
NZ763740A (en) 2023-06-30
CR20160542A (en) 2017-04-25
US20180312506A1 (en) 2018-11-01
US10472358B2 (en) 2019-11-12
US11702416B2 (en) 2023-07-18
RS60139B1 (en) 2020-05-29
AU2021200450A1 (en) 2021-02-25
PT3134403T (en) 2020-05-18
EA034972B1 (en) 2020-04-13
EP3134403A1 (en) 2017-03-01
PH12016502115B1 (en) 2020-07-01
US20200377502A1 (en) 2020-12-03
US9540368B2 (en) 2017-01-10
KR20160145796A (en) 2016-12-20
NZ725930A (en) 2023-04-28
AU2015249810A1 (en) 2015-10-29
WO2015164480A1 (en) 2015-10-29
AU2015249810B2 (en) 2019-04-18
US20200048251A1 (en) 2020-02-13
CN106414442A (en) 2017-02-15
DK3674302T3 (en) 2023-04-03
US12227502B2 (en) 2025-02-18
ES2942723T3 (en) 2023-06-06
SI3134403T1 (en) 2020-07-31
EP3134403B1 (en) 2020-02-12
PH12016502115A1 (en) 2017-01-16
EA202090371A1 (en) 2020-06-30
FI3674302T3 (en) 2023-04-27
AR100160A1 (en) 2016-09-14
HUE049627T2 (en) 2020-09-28
IL273049B (en) 2021-03-25
JP6745390B2 (en) 2020-08-26
IL248415A0 (en) 2016-11-30
TW201938559A (en) 2019-10-01
LT3674302T (en) 2023-06-12
PL3674302T3 (en) 2023-07-24
NZ763737A (en) 2023-04-28
UA119870C2 (en) 2019-08-27
US9957268B2 (en) 2018-05-01
KR20240134245A (en) 2024-09-06
SI3674302T1 (en) 2023-07-31
AU2015249810A8 (en) 2016-11-24
KR20220113552A (en) 2022-08-12
US10781209B2 (en) 2020-09-22
LT3134403T (en) 2020-05-11
TWI672301B (en) 2019-09-21
MA39985B1 (en) 2020-03-31
AU2021200450B2 (en) 2022-08-04
CA2946731A1 (en) 2015-10-29
TW201625607A (en) 2016-07-16
CY1122948T1 (en) 2021-10-29
US11059821B2 (en) 2021-07-13
PE20170144A1 (en) 2017-03-16
AU2019205984A1 (en) 2019-08-01
PL3134403T3 (en) 2020-07-13
EA039678B1 (en) 2022-02-24
MX2016013851A (en) 2017-07-14
US20250145621A1 (en) 2025-05-08
US20210300925A1 (en) 2021-09-30
MY207899A (en) 2025-03-27
KR102702503B1 (en) 2024-09-05
ES2784846T3 (en) 2020-10-01
HUE061770T2 (en) 2023-08-28
ME03763B (en) 2021-04-20
EP3674302B1 (en) 2023-03-01
SG10201809353TA (en) 2018-11-29
ECSP16088983A (en) 2017-05-31
AU2019205984B2 (en) 2020-10-29
EA201692134A1 (en) 2017-02-28
BR112016024626B1 (en) 2023-03-21
SMT202000133T1 (en) 2020-05-08
US20240002381A1 (en) 2024-01-04
PT3674302T (en) 2023-05-10
EP3674302A1 (en) 2020-07-01
IL273049A (en) 2020-04-30
JP6572237B2 (en) 2019-09-04
DK3134403T3 (en) 2020-03-09
KR102430144B1 (en) 2022-08-08
JP2019206584A (en) 2019-12-05
MY198727A (en) 2023-09-20
BR112016024626A2 (en) 2017-08-15
RS64231B1 (en) 2023-06-30
CA2946731C (en) 2022-06-07
SMT202300154T1 (en) 2023-07-20
TWI735002B (en) 2021-08-01
CN106414442B (en) 2019-03-15
ZA202101718B (en) 2025-12-17
CL2016002681A1 (en) 2017-02-03
CY1126052T1 (en) 2023-11-15
MX2020011035A (en) 2020-10-28
US20170158689A1 (en) 2017-06-08
CR20200231A (en) 2020-09-11
MX376174B (en) 2025-03-07
MY180775A (en) 2020-12-09
HRP20230340T1 (en) 2023-06-09
IL248415B (en) 2020-03-31
JP2017513879A (en) 2017-06-01
HRP20200564T1 (en) 2020-06-26
BR112016024626A8 (en) 2021-07-20
IL281263A (en) 2021-04-29
US20150307493A1 (en) 2015-10-29
IL281263B (en) 2021-09-30

Similar Documents

Publication Publication Date Title
IL281263B (en) H-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
ZA201802976B (en) N-sulfonylated pyrazolo[3,4-b]pyridin-6-carboxamides and method of use
IL240010B (en) Sulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide compounds for the treatment of cancer and autoimmune diseases
IL252578B (en) Derivatives of 1h-pyrazolo[4,3-c][1,5]naphthyridin-4(5h)-one and pharmaceutical compositions comprising them
PL2970260T3 (en) Imidazo[4,5-c]pyridine and pyrrolo[2,3-c]pyridine derivatives as ssao inhibitors
IL262257B (en) 1,5-dihydro-4h-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4h-pyrazolo[4,3-c]pyridin-4-ones as pde1 inhibitors
GB201802644D0 (en) Monocyclic,thieno, pyrido and pyrrolo pyrimidine compounds and methods of use and manufacture of the same
IL249307A0 (en) Derivatives of 2h-pyrazolo[4,3-c]quinolin-3(5h)-one and use thereof