MA39985B1 - 1h-pyrrolo [2,3-c]pyridine -7(6h)-ones et pyrazolo[3,4-c]pyridine-7(6h)-ones en tant qu'inhibiteurs de protéines bet - Google Patents

1h-pyrrolo [2,3-c]pyridine -7(6h)-ones et pyrazolo[3,4-c]pyridine-7(6h)-ones en tant qu'inhibiteurs de protéines bet

Info

Publication number
MA39985B1
MA39985B1 MA39985A MA39985A MA39985B1 MA 39985 B1 MA39985 B1 MA 39985B1 MA 39985 A MA39985 A MA 39985A MA 39985 A MA39985 A MA 39985A MA 39985 B1 MA39985 B1 MA 39985B1
Authority
MA
Morocco
Prior art keywords
pyridine
ones
pyrazolo
pyrrolo
inhibitors
Prior art date
Application number
MA39985A
Other languages
English (en)
French (fr)
Inventor
Andrew Combs
Thomas Maduskuie
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=MA39985(B1) "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 MA39985B1 publication Critical patent/MA39985B1/fr

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)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Biotechnology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • AIDS & HIV (AREA)
MA39985A 2014-04-23 2015-04-22 1h-pyrrolo [2,3-c]pyridine -7(6h)-ones et pyrazolo[3,4-c]pyridine-7(6h)-ones en tant qu'inhibiteurs de protéines bet MA39985B1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461983289P 2014-04-23 2014-04-23
EP15721085.7A EP3134403B1 (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
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
MA39985B1 true MA39985B1 (fr) 2020-03-31

Family

ID=53055117

Family Applications (1)

Application Number Title Priority Date Filing Date
MA39985A MA39985B1 (fr) 2014-04-23 2015-04-22 1h-pyrrolo [2,3-c]pyridine -7(6h)-ones et pyrazolo[3,4-c]pyridine-7(6h)-ones en tant qu'inhibiteurs de protéines bet

Country Status (37)

Country Link
US (8) US9540368B2 (enExample)
EP (3) EP4218766A1 (enExample)
JP (2) JP6572237B2 (enExample)
KR (3) KR102702503B1 (enExample)
CN (1) CN106414442B (enExample)
AR (1) AR100160A1 (enExample)
AU (3) AU2015249810B2 (enExample)
BR (1) BR112016024626B1 (enExample)
CA (1) CA2946731C (enExample)
CL (1) CL2016002681A1 (enExample)
CR (2) CR20160542A (enExample)
CY (2) CY1122948T1 (enExample)
DK (2) DK3134403T3 (enExample)
EA (2) EA039678B1 (enExample)
EC (1) ECSP16088983A (enExample)
ES (2) ES2784846T3 (enExample)
FI (1) FI3674302T3 (enExample)
HR (2) HRP20200564T1 (enExample)
HU (2) HUE061770T2 (enExample)
IL (3) IL248415B (enExample)
LT (2) LT3674302T (enExample)
MA (1) MA39985B1 (enExample)
ME (1) ME03763B (enExample)
MX (2) MX376174B (enExample)
MY (3) MY198727A (enExample)
NZ (3) NZ725930A (enExample)
PE (1) PE20170144A1 (enExample)
PH (1) PH12016502115B1 (enExample)
PL (2) PL3674302T3 (enExample)
PT (2) PT3674302T (enExample)
RS (2) RS64231B1 (enExample)
SG (2) SG10201809353TA (enExample)
SI (2) SI3674302T1 (enExample)
SM (2) SMT202300154T1 (enExample)
TW (2) TWI672301B (enExample)
UA (1) UA119870C2 (enExample)
WO (1) WO2015164480A1 (enExample)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
SI3674302T1 (sl) 2014-04-23 2023-07-31 Incyte Holdings Corporation 1h-pirolo(2,3-c)piridin-7(6h)-oni in pirazolo(3,4-c)piridin-7(6h)-oni kot zaviralci proteinov bet
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
MA40940A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
JP6639497B2 (ja) 2014-11-10 2020-02-05 ジェネンテック， インコーポレイテッド ブロモドメインインヒビターおよびその使用
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
CN107531692B (zh) 2015-01-29 2020-12-25 基因泰克公司 治疗化合物及其用途
AR104259A1 (es) 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
US10836742B2 (en) 2015-08-11 2020-11-17 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
CN114605387A (zh) 2015-08-12 2022-06-10 埃皮吉纳提克斯股份有限公司 取代的苯并咪唑、它们的制备和它们作为药物的用途
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
SG11201808003RA (en) 2016-04-15 2018-10-30 Abbvie Inc Bromodomain inhibitors
CR20190027A (es) 2016-06-20 2019-05-16 Incyte Corp Formas sólidas cristalinas de un inhibidor de bet
WO2018086605A1 (zh) 2016-11-10 2018-05-17 山东罗欣药业集团股份有限公司 一种含氮大环类化合物、其制备方法、药物组合物及应用
WO2018130174A1 (zh) * 2017-01-11 2018-07-19 江苏豪森药业集团有限公司 吡咯并[2,3-c]吡啶类衍生物、其制备方法及其在医药上的应用
JP2020527588A (ja) 2017-07-18 2020-09-10 ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． アデノシンアンタゴニストとしてのヘテロ環式化合物
BR112020000962A2 (pt) 2017-07-18 2020-07-14 Nuvation Bio Inc. compostos de 1,8-naftiridinona e usos dos mesmos
WO2019086712A1 (en) * 2017-11-06 2019-05-09 Centre National De La Recherche Scientifique Xanthine derivatives and uses thereof as inhibitors of bromodomains of bet proteins
US11466034B2 (en) * 2017-12-20 2022-10-11 Betta Pharmaceuticals Co., Ltd. Compound functioning as bromodomain protein inhibitor, and composition
BR112020012197A2 (pt) 2017-12-21 2020-11-24 Ribon Therapeutics Inc. quinazolinonas como inibidores de parp14
EP3750885A4 (en) * 2018-02-06 2021-10-27 Shanghai Haihe Pharmaceutical Co., Ltd. COMPOUND PRESENTING AN INHIBITORING ACTIVITY OF BET, ITS PREPARATION PROCESS AND ITS USE
CN110776508B (zh) 2018-07-27 2021-07-16 海创药业股份有限公司 一种brd4抑制剂及其制备方法和用途
CN109580433B (zh) * 2018-10-26 2021-05-28 中国辐射防护研究院 一种常规爆炸放射性气溶胶扩散的源项估算方法
EP3873474A4 (en) 2018-10-30 2022-07-13 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS USED AS BET INHIBITORS
CN109432093A (zh) * 2018-12-23 2019-03-08 黄泳华 由吡唑并吡啶酮类化合物构成的乙酰胆碱酯酶抑制剂的增效体系
CA3126931A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
AU2020208644A1 (en) 2019-01-18 2021-08-26 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
US12459939B2 (en) 2019-03-17 2025-11-04 Shanghai Ringene Biopharma Co., Ltd. Acylaminopyrrolo-pyridone compound, preparation method therefor and use thereof
GB201905721D0 (en) 2019-04-24 2019-06-05 Univ Dundee Compounds
CN110003204B (zh) * 2019-04-30 2020-08-11 上海勋和医药科技有限公司 一种bet蛋白抑制剂、其制备方法及用途
WO2020253711A1 (zh) * 2019-06-17 2020-12-24 中国科学院上海药物研究所 一种吡咯并吡啶酮类化合物、其制备方法、其组合物和用途
KR20220024098A (ko) * 2019-06-19 2022-03-03 리본 테라퓨틱스 인코포레이티드 요법에 사용하기 위한 parp14의 표적화된 단백질 분해
CA3145827A1 (en) 2019-07-02 2021-01-07 Nuvation Bio Inc. Heterocyclic compounds as bet inhibitors
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
US20230119316A1 (en) 2019-12-27 2023-04-20 Lupin Limited Substituted Tricyclic Compounds
WO2021247064A1 (en) * 2020-06-03 2021-12-09 Incyte Corporation Combination of ruxolitinib with incb057643 for treatment of myeloproliferative neoplasms
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN115427407B (zh) * 2020-12-01 2024-02-27 成都苑东生物制药股份有限公司 一种新型n-杂环bet溴结构域抑制剂、其制备方法及医药用途
WO2022132049A1 (en) * 2020-12-17 2022-06-23 National University Of Singapore Treating cancers using bet inhibitors
GEP20257811B (en) 2021-01-19 2025-10-27 Lupin Ltd Pharmaceutical combinations of sos1 inhibitors
WO2024138201A2 (en) * 2022-12-23 2024-06-27 Tay Therapeutics Limited 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 (fr) 1899-12-05 1904-03-26 Louis Olivier Victor Parmentie Machine à copier les lettres
JPS59170313A (ja) 1983-03-14 1984-09-26 Kurimoto Iron Works Ltd スクリ−ンゲ−ト
JPS6053449A (ja) 1983-09-01 1985-03-27 M K Seikou Kk 洗車機
JPS6085739U (ja) 1983-11-18 1985-06-13 クラリオン株式会社 テ−プレコ−ダにおけるピンチロ−ラ装置
JPS6243003U (enExample) 1985-09-05 1987-03-14
JPH0314566A (ja) 1989-06-09 1991-01-23 Sankyo Co Ltd ベンズイミダゾール誘導体
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 (fr) 1993-10-04 1995-11-24 Synthelabo Dérivés de pipéridine, leur préparation et leur utilisation en thérapeutique.
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 (fr) 1995-03-13 1997-04-30 Synthelabo Derives de piperidine, leur procede de preparation et leur application en therapeutique
FR2747678B1 (fr) 1996-04-22 1998-05-22 Synthelabo Composes derives d'imidazobenzoxazine, leurs procedes de preparation et leurs utilisations en therapeutique
US6287693B1 (en) 1998-02-25 2001-09-11 John Claude Savoir Stable shaped particles of crystalline organic compounds
ES2253370T3 (es) 2000-04-21 2006-06-01 PHARMACIA & UPJOHN COMPANY LLC Cabergolina para el tratamiento del sindrome de fibromialgia y de fatiga cronica.
PL202623B1 (pl) 2000-06-28 2009-07-31 Smithkline Beecham Plc Sposób wytwarzania drobno zmielonego preparatu substancji leczniczej, drobno zmielona substancja lecznicza wytworzona tym sposobem i zawierająca ją kompozycja farmaceutyczna
EA005950B1 (ru) 2000-08-08 2005-08-25 Санофи-Авентис Производные бензимидазола, их получение и терапевтическое применение
FR2816619B1 (fr) 2000-11-15 2003-01-31 Sanofi Synthelabo Derives de benzimidazole, leur preparation et leur application en therapeutique
US6919334B2 (en) 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
AU2003293006A1 (en) 2002-11-22 2004-06-18 Japan Tobacco Inc. Fused bicyclic nitrogen-containing heterocycles
EP1462103A1 (en) 2003-03-25 2004-09-29 Faust Pharmaceuticals NO donors, combination products and uses as modulators of neurotransmitter release
JPWO2005080334A1 (ja) 2004-02-23 2007-08-02 大日本住友製薬株式会社 新規ヘテロ環化合物
EP1732541A4 (en) 2004-04-07 2008-03-05 Takeda Pharmaceutical CYCLIC COMPOUNDS
US7713954B2 (en) 2004-09-30 2010-05-11 Roche Palo Alto Llc Compositions and methods for treating cognitive disorders
DE102005011058A1 (de) 2005-03-10 2006-09-14 Merck Patent Gmbh Substituierte Tetrahydro-pyrrolo-chinolinderivate
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
JP5159305B2 (ja) 2005-05-30 2013-03-06 田辺三菱製薬株式会社 チエノトリアゾロジアゼピン化合物及びその医薬としての用途
CA2616020A1 (en) 2005-08-05 2007-02-15 Astrazeneca Ab Tricyclic benzimidazoles and their use as metabotropic glutamate receptor modulators
WO2009020677A2 (en) 2007-04-27 2009-02-12 University Of Rochester Compositions and methods for inhibiting g protein signaling
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
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
WO2009020559A2 (en) 2007-08-03 2009-02-12 The J. David Gladstone Institutes Agents that inhibit p-tefb interactions and methods of use thereof
KR101600634B1 (ko) 2007-12-28 2016-03-07 미쓰비시 타나베 파마 코퍼레이션 항암제
DE102008052618A1 (de) 2008-10-21 2010-04-22 Henkel Ag & Co. Kgaa Tricyclische Aldehyde und C,H-acide Verbindungen
EP2415767B1 (en) 2009-03-27 2014-09-03 Takeda Pharmaceutical Company Limited Poly (ADP-ribose) Polymerase (PARP) Inhibitors
TW201105681A (en) 2009-06-10 2011-02-16 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
TW201103941A (en) 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
WO2011024987A1 (ja) 2009-08-31 2011-03-03 塩野義製薬株式会社 芳香族縮合へテロ環誘導体およびそれらを含有する医薬組成物
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
ES2652304T3 (es) 2009-11-05 2018-02-01 Glaxosmithkline Llc Compuesto de benzodiacepina novedoso
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US9102677B2 (en) 2009-11-05 2015-08-11 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US9360482B2 (en) 2009-11-05 2016-06-07 Glaxosmithkline Llc Process for the identification of a compound which inhibits the binding of the second bromodomain of each of human BRD-2, BRD-3, and BRD-4
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US8927561B2 (en) 2010-04-23 2015-01-06 Kineta, Inc. Pyrimidinedione anti-viral compounds
EP2902030B1 (en) 2010-05-14 2016-09-14 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
WO2011143660A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
CN103180318B (zh) 2010-05-14 2017-05-10 达那-法伯癌症研究所 雄性避孕组合物以及使用方法
US20130252331A1 (en) 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
JP5844358B2 (ja) 2010-06-22 2016-01-13 グラクソスミスクライン エルエルシー ベンゾトリアゾロジアゼピン化合物を含むブロモドメイン阻害剤
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012107465A1 (en) 2011-02-09 2012-08-16 F. Hoffmann-La Roche Ag Heterocyclic compounds as pi3 kinase inhibitors
AU2012220620A1 (en) 2011-02-23 2013-10-03 Icahn School Of Medicine At Mount Sinai Inhibitors of bromodomains as modulators of gene expression
RU2013143747A (ru) 2011-03-21 2015-04-27 Ф. Хоффманн-Ля Рош Аг Соединения бензоксазепина, селективные в отношении pi3k p110 дельта и способы их применения
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106799D0 (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
WO2012151512A2 (en) 2011-05-04 2012-11-08 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
US9145391B2 (en) 2011-05-10 2015-09-29 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 (ja) 2011-06-30 2013-01-17 Dainippon Sumitomo Pharma Co Ltd ベンズイミダゾロンおよびオキシインドール誘導体ならびにそれらの医薬用途
WO2013019710A1 (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
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
JP6106174B2 (ja) 2011-08-31 2017-03-29 大塚製薬株式会社 キノロン化合物
DE102011082013A1 (de) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
ES2632443T3 (es) 2011-09-22 2017-09-13 Viiv Healthcare Uk Limited Compuestos de pirrolopiridinona y procedimientos de tratamiento del VIH
CN103857391B (zh) 2011-09-30 2016-06-08 沈阳蓝桑医药生物技术研发有限公司 含有瑞利格内酯的药物组合物及其应用
EP2771340B1 (en) 2011-10-25 2016-04-13 Sanofi 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
LT2773354T (lt) 2011-11-01 2019-08-12 Resverlogix Corp. Geriamosios greitai atsipalaiduojančios pakeistų chinozolinų vaisto formos
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20150133434A1 (en) 2012-03-28 2015-05-14 The J. David Gladstone Institutes Compositions and Methods for Reactivating Latent Immunodeficiency Virus
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
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
CA2870931A1 (en) 2012-04-20 2013-10-24 Abbvie Inc. Isoindolone derivatives
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
EP2858982A4 (en) 2012-06-12 2015-11-11 Abbvie Inc PYRIDINONE AND PYRIDAZINONE DERIVATIVES
MX2014015986A (es) 2012-06-25 2016-02-11 Oncoethix Gmbh Metodo para tratar linfoma utilizando compuestos de tienotriazolodiazepina.
WO2014015175A1 (en) 2012-07-18 2014-01-23 Massachusetts Institute Of Technology Compositions and methods for modulating brd4 bioactivity
US20150238507A1 (en) 2012-08-16 2015-08-27 Glaxosmithkline Llc Benzodiazepines for treating small cell lung cancer
KR20150041787A (ko) 2012-08-16 2015-04-17 바이엘 파마 악티엔게젤샤프트 2,3-벤조디아제핀
EP2900221B1 (en) 2012-09-28 2019-03-06 Oncoethix GmbH Pharmaceutical formulation containing thienotriazolodiazepine compounds
US9663523B2 (en) 2012-09-28 2017-05-30 Bayer Pharma Aktiengesellschaft BET protein-inhibiting 5-aryltriazoleazepines
EP2917181B1 (en) 2012-11-09 2019-09-25 Jacobus Pharmaceutical Company, Inc. Heteroaryl derivatives and uses thereof
US9422290B2 (en) 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
ES2625945T3 (es) 2012-11-14 2017-07-21 Glaxosmithkline Llc Tieno[3,2-c]piridin-4(5H)-onas como inhibidores de bet
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
HK1213899A1 (zh) 2012-12-20 2016-07-15 Bayer Pharma Aktiengesellschaft 抑制bet蛋白的二氢吡啶并吡嗪酮
EP2935261A1 (de) 2012-12-20 2015-10-28 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydrochinoxalinone
MX2015007921A (es) 2012-12-21 2016-03-03 Zenith Epigenetics Corp Compuestos heterociclicos novedosos como inhibidores de bromodominio.
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2961747B1 (en) 2013-02-27 2017-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2970285B1 (en) 2013-03-11 2019-04-17 AbbVie Inc. Fused tetracyclic bromodomain inhibitors
CN105377851B (zh) 2013-03-11 2018-07-20 密执安州立大学董事会 Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法
JP2016512524A (ja) 2013-03-11 2016-04-28 アッヴィ・インコーポレイテッド ブロモドメイン阻害剤
CN105164113B (zh) 2013-03-12 2018-03-02 艾伯维公司 吡咯酰胺抑制剂
CN105026403B (zh) 2013-03-12 2018-05-18 艾伯维公司 四环布罗莫结构域抑制剂
HK1218909A1 (zh) 2013-03-12 2017-03-17 Abbvie Inc. 二氢-吡咯并吡啶酮布罗莫结构域抑制剂
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
EP2968360B1 (en) 2013-03-14 2021-01-20 ConverGene LLC Quinolinone derivatives for the inhibition of bromodomain-containing proteins
WO2014140077A1 (en) 2013-03-14 2014-09-18 Glaxosmithkline Intellectual Property (No.2) Limited Furopyridines as bromodomain inhibitors
ES2704048T3 (es) 2013-03-14 2019-03-14 Glaxosmithkline Ip No 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina-2,3-disustituida y su uso como inhibidores de bromodominio
US20160039842A1 (en) 2013-03-15 2016-02-11 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
NZ630875A (en) 2013-03-15 2017-12-22 Plexxikon Inc Heterocyclic compounds and uses thereof
US9102684B2 (en) 2013-03-27 2015-08-11 Boehringer Ingelheim International Gmbh Indolinone analogues
EP2978758B1 (en) 2013-03-27 2017-02-08 Boehringer Ingelheim International GmbH Dihydroquinazolinone analogues as brd4 inhibitors
TWI530499B (zh) 2013-03-28 2016-04-21 吉李德科學股份有限公司 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類
WO2014170350A1 (en) 2013-04-17 2014-10-23 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
CA2901083A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
TWI527811B (zh) 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
EP3004109A1 (en) 2013-05-27 2016-04-13 Novartis AG Imidazopyrrolidinone derivatives and their use in the treatment of disease
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
MX2015016421A (es) 2013-05-28 2016-03-03 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades.
EA028035B1 (ru) 2013-05-28 2017-09-29 Новартис Аг Производные пиразолопирролидин-4-она и их применение при лечении заболевания
ITMI20130991A1 (it) 2013-06-17 2014-12-18 Industrie De Nora Spa Sistema per la misurazione di correnti presenti sugli elettrodi in celle elettrolitiche interconnesse.
CA2915419A1 (en) 2013-06-17 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted phenyl-2,3-benzodiazepines
WO2015004534A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
CN105407888B (zh) 2013-06-21 2019-05-21 齐尼思表观遗传学有限公司 新双环溴结构域抑制剂
MX2015017963A (es) 2013-06-28 2016-11-10 Abbvie Inc Inhibidores de bromodominio.
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
JP6441334B2 (ja) 2013-07-16 2018-12-19 ビーエーエスエフ ソシエタス・ヨーロピアＢａｓｆ Ｓｅ 除草性アジン
CA2918910A1 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
KR101672096B1 (ko) 2013-09-30 2016-11-02 주식회사 엘지화학 헤테로환 화합물 및 이를 포함하는 유기 발광 소자
EA035727B1 (ru) 2013-10-18 2020-07-31 Селджен Квонтисел Рисёрч, Инк. Ингибиторы бромодомена
WO2015081246A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic 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
CN105939996A (zh) 2013-12-09 2016-09-14 艾伯维公司 用作布罗莫结构域抑制剂的二氢吡啶酮和二氢哒嗪酮衍生物
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
WO2015095445A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
LT3092227T (lt) 2014-01-09 2018-08-10 Orion Corporation Bicikliniai heterocikliniai dariniai kaip bromodomeno inhibitoriai
WO2015131005A1 (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
BR112016022782B1 (pt) 2014-04-23 2020-01-28 Basf Se composto de diaminotriazina, composição agroquímica e uso de um composto
EA030373B1 (ru) 2014-04-23 2018-07-31 Такеда Фармасьютикал Компани Лимитед Изоиндолин-1-оновые производные в качестве положительных аллостерических модуляторов холинергического мускаринового m1 рецептора для лечения болезни альцгеймера
SI3674302T1 (sl) 2014-04-23 2023-07-31 Incyte Holdings Corporation 1h-pirolo(2,3-c)piridin-7(6h)-oni in pirazolo(3,4-c)piridin-7(6h)-oni kot zaviralci proteinov bet
RU2016146099A (ru) 2014-05-02 2018-06-05 Онкоэтикс Гмбх Способ лечения острого миелоидного лейкоза и/или острого лимфобластного лейкоза с помощью тиенотриазолодиазепиновых соединений
JP2017514907A (ja) 2014-05-02 2017-06-08 オンコエシックス ゲーエムベーハー チエノトリアゾロジアゼピン化合物を用いる耐性非ホジキンリンパ腫、髄芽腫及び／又はａｌｋ＋非小細胞肺癌の治療方法
WO2015169953A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating glioma using thienotriazolodiazepine compounds
MX2016014574A (es) 2014-05-08 2017-02-23 Oncoethix Gmbh El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo.
EP3148543B1 (en) 2014-05-30 2020-04-08 Icahn School of Medicine at Mount Sinai Small molecule transcription modulators of bromodomains
PT3157928T (pt) 2014-06-20 2019-05-30 Constellation Pharmaceuticals Inc Formas cristalinas de 2-((4s)-6-(4-clorofenil)-1-metil-4h-benzo[c] isoxazolo[4,5-e]azepin-4-il)acetamida
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
PE20190710A1 (es) 2014-10-24 2019-05-17 Bristol Myers Squibb Co Compuestos de indol carboxamida utiles como inhibidores de cinasas
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
EP3253756B1 (en) 2015-02-03 2021-09-22 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
CA2987384A1 (en) 2015-05-29 2016-12-08 Shionogi & Co., Ltd. Nitrogen-containing tricyclic derivative having hiv replication inhibitory activity
CN105039258B (zh) 2015-07-03 2018-04-17 北京大学 将非神经元细胞重编程为神经元样细胞的方法和组合物
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN105254635A (zh) 2015-10-30 2016-01-20 中国药科大学 一类咪唑并吡嗪类化合物及其药物组合物和用途
US20170127985A1 (en) 2015-11-11 2017-05-11 Medtronic Minimed, Inc. Sensor set
CA3007168A1 (en) 2015-12-14 2017-06-22 Zenith Epigenetics Ltd. 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
US20190040063A1 (en) 2016-02-05 2019-02-07 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Tricyclic compound for bromodomain-containing protein inhibitor and preparation pharmaceutical composition, and application thereof
CR20190027A (es) 2016-06-20 2019-05-16 Incyte Corp Formas sólidas cristalinas de un inhibidor de bet
CN108069958A (zh) 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 一种含氮杂环类化合物、其制备方法、药物组合物及应用

Also Published As

Publication number Publication date
KR102430144B1 (ko) 2022-08-08
MX2020011035A (es) 2020-10-28
US20170158689A1 (en) 2017-06-08
DK3134403T3 (en) 2020-03-09
US20150307493A1 (en) 2015-10-29
US9540368B2 (en) 2017-01-10
UA119870C2 (uk) 2019-08-27
JP6572237B2 (ja) 2019-09-04
MY207899A (en) 2025-03-27
TWI672301B (zh) 2019-09-21
CN106414442A (zh) 2017-02-15
US20250145621A1 (en) 2025-05-08
DK3674302T3 (da) 2023-04-03
AU2021200450A1 (en) 2021-02-25
US11059821B2 (en) 2021-07-13
ES2942723T3 (es) 2023-06-06
CA2946731A1 (en) 2015-10-29
US9957268B2 (en) 2018-05-01
LT3134403T (lt) 2020-05-11
KR20160145796A (ko) 2016-12-20
MY198727A (en) 2023-09-20
AR100160A1 (es) 2016-09-14
AU2015249810A1 (en) 2015-10-29
IL281263B (en) 2021-09-30
NZ763737A (en) 2023-04-28
US20200048251A1 (en) 2020-02-13
BR112016024626B1 (pt) 2023-03-21
PH12016502115B1 (en) 2020-07-01
EP3134403B1 (en) 2020-02-12
CR20200231A (es) 2020-09-11
SG10201809353TA (en) 2018-11-29
CY1122948T1 (el) 2021-10-29
CL2016002681A1 (es) 2017-02-03
US20180312506A1 (en) 2018-11-01
PE20170144A1 (es) 2017-03-16
PT3674302T (pt) 2023-05-10
US12227502B2 (en) 2025-02-18
IL248415B (en) 2020-03-31
US20240002381A1 (en) 2024-01-04
EA034972B1 (ru) 2020-04-13
US10472358B2 (en) 2019-11-12
CR20160542A (es) 2017-04-25
US20210300925A1 (en) 2021-09-30
AU2015249810B2 (en) 2019-04-18
JP2017513879A (ja) 2017-06-01
WO2015164480A1 (en) 2015-10-29
SMT202000133T1 (it) 2020-05-08
EA039678B1 (ru) 2022-02-24
RS64231B1 (sr) 2023-06-30
IL273049A (en) 2020-04-30
TWI735002B (zh) 2021-08-01
PL3134403T3 (pl) 2020-07-13
FI3674302T3 (fi) 2023-04-27
BR112016024626A8 (pt) 2021-07-20
US20200377502A1 (en) 2020-12-03
IL281263A (en) 2021-04-29
LT3674302T (lt) 2023-06-12
JP2019206584A (ja) 2019-12-05
NZ725930A (en) 2023-04-28
RS60139B1 (sr) 2020-05-29
US10781209B2 (en) 2020-09-22
ME03763B (me) 2021-04-20
SG11201608843TA (en) 2016-11-29
EP3674302A1 (en) 2020-07-01
JP6745390B2 (ja) 2020-08-26
MX2016013851A (es) 2017-07-14
IL248415A0 (en) 2016-11-30
IL273049B (en) 2021-03-25
SI3134403T1 (sl) 2020-07-31
TW201938559A (zh) 2019-10-01
PT3134403T (pt) 2020-05-18
SMT202300154T1 (it) 2023-07-20
BR112016024626A2 (pt) 2017-08-15
MY180775A (en) 2020-12-09
HUE049627T2 (hu) 2020-09-28
ES2784846T3 (es) 2020-10-01
AU2015249810A8 (en) 2016-11-24
EP3674302B1 (en) 2023-03-01
ECSP16088983A (es) 2017-05-31
KR20240134245A (ko) 2024-09-06
HRP20200564T1 (hr) 2020-06-26
KR102702503B1 (ko) 2024-09-05
EA202090371A1 (ru) 2020-06-30
NZ763740A (en) 2023-06-30
AU2019205984B2 (en) 2020-10-29
AU2021200450B2 (en) 2022-08-04
HUE061770T2 (hu) 2023-08-28
PH12016502115A1 (en) 2017-01-16
HRP20230340T1 (hr) 2023-06-09
KR20220113552A (ko) 2022-08-12
CA2946731C (en) 2022-06-07
PL3674302T3 (pl) 2023-07-24
AU2019205984A1 (en) 2019-08-01
CN106414442B (zh) 2019-03-15
TW201625607A (zh) 2016-07-16
US11702416B2 (en) 2023-07-18
SI3674302T1 (sl) 2023-07-31
EP4218766A1 (en) 2023-08-02
EP3134403A1 (en) 2017-03-01
EA201692134A1 (ru) 2017-02-28
MX376174B (es) 2025-03-07
CY1126052T1 (el) 2023-11-15

Similar Documents

Publication Publication Date Title
MA39985B1 (fr) 1h-pyrrolo [2,3-c]pyridine -7(6h)-ones et pyrazolo[3,4-c]pyridine-7(6h)-ones en tant qu'inhibiteurs de protéines bet
JOP20190041B1 (ar) مركبات وتركيبات كمثبطات لمستقبلات شبيهة بالتول إندوسومية
MX382331B (es) Derivados de 6,7,8,9-tetrahidro-3h-pirazolo[4,3f] isoquinolina útiles en el tratamiento del cáncer.
MA40886B1 (fr) Nouveau triterpénone en c-3 avec des dérivés d'amide inverse en c-28 en tant qu'inhibiteurs du vih
EA201890852A1 (ru) Соли валбеназина и их полиморфы
EA202090258A2 (ru) ПРОИЗВОДНЫЕ ПИРРОЛО[3,2-d]ПИРИМИДИНА ДЛЯ ЛЕЧЕНИЯ ВИРУСНЫХ ИНФЕКЦИЙ И ДРУГИХ ЗАБОЛЕВАНИЙ
UA115558C2 (uk) Алкілпіримідинові похідні для лікування вірусних інфекцій та подальших захворювань
EA201590663A1 (ru) ПРОИЗВОДНЫЕ ПИРРОЛО[3,2-d]ПИРИМИДИНА ДЛЯ ЛЕЧЕНИЯ ВИРУСНЫХ ИНФЕКЦИЙ И ДРУГИХ ЗАБОЛЕВАНИЙ
MA40706A1 (fr) Pyrrolopyrimidines et pyrazolopyrimidines utilisées en tant qu'inhibiteurs de la protéase spécifique de l'ubiquitine 7
UY36112A (es) Compuestos de imidazo[4,5-c]quinolin-2-ona y su uso para tratar cáncer
MX2021001096A (es) 7-bencil-4-(2-metilbencilo)-2,4,6,7,8,9-hexahidroimidazo [1,2-a]pirido[3,4-e]pirimidin-5(1h)-ona, analogos y sales del mismo y su uso en terapia.
EA201492016A1 (ru) C-17 бициклические амины тритерпеноидов с ингибиторной активностью созревания вич
BR112017001726A2 (pt) compostos de 6,7-di-hidropirazolo [1,5-a]pirazin-4(5h)-ona e seus usos como moduladores alostéricos negativos de receptores mglur2
EA201692544A1 (ru) 6,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-4(5H)-ОНОВЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ОТРИЦАТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ MGLUR2
MY199668A (en) C-3 and c-17 modified triterpenoids as hiv-1 inhibitors
JO3601B1 (ar) مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
EA201790179A1 (ru) [1,2,4]триазоло[4,3-b]пиридазины для применения в лечении пролиферативных заболеваний
EA201890922A1 (ru) Циклические простоэфирные производные пиразоло[1,5-а]пиримидин-3-карбоксамида
CL2016001024A1 (es) Compuestos derivados de pirido[4,3-b]pirazin-2-carboxamidas; procedimiento de preparacion; composicion farmaceutica y uso para el tratamiento de trastornos neurodegenerativos, esquizofrenia, depresion, entre otras enfermedades.
MX384987B (es) Derivados del ácido acético azaindol y su uso como moduladores de receptor de prostaglandina d2.
UA110245C2 (xx) ПОХІДНІ 7-(ГЕТЕРОАРИЛАМІНО)-6,7,8,9-ТЕТРАГІДРОПІРИДО$1,2-а]ІНДОЛ-ОЦТОВОЇ КИСЛОТИ ТА ЇХ ЗАСТОСУВАННЯ ЯК МОДУЛЯТОРІВ РЕЦЕПТОРА ПРОСТАГЛАНДИНУ D2
EA202091139A1 (ru) Производные имидазопиридина и их применение в качестве лекарственного средства
MX2016011900A (es) Derivados de acido azaindol-acetico y su uso como moduladores del receptor de prostaglandina d2.
EA201790795A1 (ru) СОЕДИНЕНИЯ 4Н-ПИРИДО[1,2-a]ПИРИМИДИН-4-ОНА
PH12018501640A1 (en) C-3 and c-17 modified triterpenoids as hiv-1 inhibitors