[go: up one dir, main page]

PE20170144A1 - 1h-pirrolo[2,3-c] piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h)-onas como inhibidores de proteinas bet - Google Patents

1h-pirrolo[2,3-c] piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h)-onas como inhibidores de proteinas bet

Info

Publication number
PE20170144A1
PE20170144A1 PE2016002116A PE2016002116A PE20170144A1 PE 20170144 A1 PE20170144 A1 PE 20170144A1 PE 2016002116 A PE2016002116 A PE 2016002116A PE 2016002116 A PE2016002116 A PE 2016002116A PE 20170144 A1 PE20170144 A1 PE 20170144A1
Authority
PE
Peru
Prior art keywords
pyridin
alkyl
ones
halo
inhibitors
Prior art date
Application number
PE2016002116A
Other languages
English (en)
Inventor
Andrew P Combs
Thomas P 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=PE20170144(A1) "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 PE20170144A1 publication Critical patent/PE20170144A1/es

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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Biotechnology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)

Abstract

Se refiere a un compuesto de la formula I, donde: X es C=O o CR8R9; Y es O, S, o NR10; Z es CH o N; R1 y R2 son independientemente H, halo, alquilo C1-C6, alquenilo C2-C6, entre otros, o R1 y R2 junto con el atomo de carbono al que estan unidos forman un cicloalquilo C3-C10 o heterocicloalquilo de 4-10 miembros, cada uno opcionalmente sustituido; R3 es H o alquilo C1-C6 opcionalmente sustituido; R4 es H, halo, alquilo C1-C4, entre otros; R5 es H, halo, alquilo C1-C6, entre otros; R6 es H, halo, alquilo C1-C4, entre otros; R7 y R10 son H o alquilo C1-C4; R8 y R9 son H, halo, alquilo C1-C4 o haloalquilo C1-C4. Son compuestos preferidos: 8-(6-metil-7-oxo-6,7-dihidro-1H-pirrolo[2,3-c]piridin-4-il)-2-fenil-2H-1,4-benzoxazin-3(4H)-ona; 2-isopropil-8-(6-metil-7-oxo-6,7-dihidro-1H-pirrolo[2,3-c]piridin-4-il)-2H-1,4-benzoxazin-3(4H)-ona; entre otros. Tambien se refiere a una composicion farmaceutica y a un metodo de tratamiento. Dichos compuestos son inhibidores de proteinas BET siendo utiles en el tratamiento de cancer, alergia, EPOC, entre otros.
PE2016002116A 2014-04-23 2015-04-22 1h-pirrolo[2,3-c] piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h)-onas como inhibidores de proteinas bet PE20170144A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201461983289P 2014-04-23 2014-04-23

Publications (1)

Publication Number Publication Date
PE20170144A1 true PE20170144A1 (es) 2017-03-16

Family

ID=53055117

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016002116A PE20170144A1 (es) 2014-04-23 2015-04-22 1h-pirrolo[2,3-c] piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h)-onas como inhibidores de proteinas bet

Country Status (37)

Country Link
US (8) US9540368B2 (es)
EP (3) EP3674302B1 (es)
JP (2) JP6572237B2 (es)
KR (3) KR20240134245A (es)
CN (1) CN106414442B (es)
AR (1) AR100160A1 (es)
AU (3) AU2015249810B2 (es)
BR (1) BR112016024626B1 (es)
CA (1) CA2946731C (es)
CL (1) CL2016002681A1 (es)
CR (2) CR20200231A (es)
CY (2) CY1122948T1 (es)
DK (2) DK3134403T3 (es)
EA (2) EA039678B1 (es)
EC (1) ECSP16088983A (es)
ES (2) ES2942723T3 (es)
FI (1) FI3674302T3 (es)
HR (2) HRP20200564T1 (es)
HU (2) HUE049627T2 (es)
IL (3) IL248415B (es)
LT (2) LT3134403T (es)
MA (1) MA39985B1 (es)
ME (1) ME03763B (es)
MX (2) MX376174B (es)
MY (3) MY198727A (es)
NZ (3) NZ763737A (es)
PE (1) PE20170144A1 (es)
PH (1) PH12016502115B1 (es)
PL (2) PL3674302T3 (es)
PT (2) PT3674302T (es)
RS (2) RS64231B1 (es)
SG (2) SG11201608843TA (es)
SI (2) SI3134403T1 (es)
SM (2) SMT202000133T1 (es)
TW (2) TWI735002B (es)
UA (1) UA119870C2 (es)
WO (1) WO2015164480A1 (es)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2755827T3 (es) 2013-03-15 2020-04-23 Incyte Holdings Corp Heterciclos tricíclicos como inhibidores de proteína BET
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EP3674302B1 (en) 2014-04-23 2023-03-01 Incyte Holdings Corporation 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
MA40940A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
EP3218376B1 (en) 2014-11-10 2019-12-25 Genentech, Inc. Bromodomain inhibitors and uses thereof
EP3250571B1 (en) 2015-01-29 2022-11-30 Genentech, Inc. Therapeutic compounds and uses thereof
AR104259A1 (es) * 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
HK1256753A1 (zh) 2015-08-11 2019-10-04 Neomed Institute 芳基-取代的二氢喹诺酮、它们的制备和它们作为药物的用途
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
WO2017024412A1 (en) 2015-08-12 2017-02-16 Neomed Institute Substituted benzimidazoles, their preparation and their use as pharmaceuticals
WO2017066876A1 (en) 2015-10-21 2017-04-27 Neomed Institute Substituted imidazopyridines, their preparation and their use as pharmaceuticals
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
EP3442972B1 (en) 2016-04-15 2020-03-04 AbbVie Inc. Bromodomain inhibitors
CN114366748A (zh) * 2016-06-20 2022-04-19 因赛特公司 Bet抑制剂的结晶固体形式
JP2019534306A (ja) 2016-11-10 2019-11-28 羅欣薬業（上海）有限公司Ｌｕｏｘｉｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ（Ｓｈａｎｇｈａｉ） Ｃｏ．， Ｌｔｄ． 窒素含有大員環系化合物、その製造方法、薬物組成物および使用
TW201825490A (zh) * 2017-01-11 2018-07-16 大陸商江蘇豪森藥業集團有限公司 吡咯並［２，３－ｃ］吡啶類衍生物、其製備方法及其在醫藥上的應用
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
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
IL275478B2 (en) * 2017-12-20 2024-06-01 Betta Pharmaceuticals Co Ltd A preparation that functions as a bromodomain protein inhibitor, and the composition
BR112020012197A2 (pt) 2017-12-21 2020-11-24 Ribon Therapeutics Inc. quinazolinonas como inibidores de parp14
US20210261539A1 (en) * 2018-02-06 2021-08-26 Shanghai Haihe Pharmaceutical Co., Ltd. Compound having bet inhibitory activity and preparation method and use therefor
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
CN113226322A (zh) 2018-10-30 2021-08-06 诺维逊生物股份有限公司 作为bet抑制剂的杂环化合物
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
WO2020150676A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
SG11202107810WA (en) 2019-01-18 2021-08-30 Nuvation Bio Inc Heterocyclic compounds as adenosine antagonists
SG11202110099YA (en) * 2019-03-17 2021-10-28 Shanghai Ringene Biopharma Co Ltd Pyrrole amidopyridone 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
MA56513A (fr) * 2019-06-19 2022-04-27 Ribon Therapeutics Inc Dégradation de protéine ciblée de parp14 pour une utilisation en thérapie
MX2022000050A (es) 2019-07-02 2022-05-24 Nuvation Bio Inc Compuestos heterocíclicos como inhibidores de bromodominio extraterminal (bet).
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
WO2021130731A1 (en) 2019-12-27 2021-07-01 Lupin Limited Substituted tricyclic compounds
CA3184633A1 (en) * 2020-06-03 2021-12-09 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022116968A1 (zh) 2020-12-01 2022-06-09 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
PE20241625A1 (es) 2021-01-19 2024-08-07 Lupin Ltd Combinaciones farmaceuticas de inhibidores de sos1 para tratar o prevenir cancer
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 (es) 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
NZ531172A (en) 2000-04-21 2005-07-29 Upjohn Co Heterocyclic amine-type compounds for treating fibromyalgia and chronic fatigue syndrome
EP1294358B1 (en) 2000-06-28 2004-08-18 Smithkline Beecham Plc Wet milling process
PL365080A1 (en) 2000-08-08 2004-12-27 Sanofi-Aventis Benzimidazole derivatives, preparation and therapeutic use thereof
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
CA2514473C (en) 2002-11-22 2008-05-27 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
WO2005080334A1 (ja) 2004-02-23 2005-09-01 Dainippon Sumitomo Pharma Co., Ltd. 新規へテロ環化合物
JP4790703B2 (ja) 2004-04-07 2011-10-12 武田薬品工業株式会社 環式化合物
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
TWI447120B (zh) 2005-05-30 2014-08-01 Mitsubishi Tanabe Pharma Corp 噻吩并三唑并苯二氮呯化合物、其醫藥上之用途
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
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
US9603848B2 (en) 2007-06-08 2017-03-28 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
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 (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
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EA023441B1 (ru) 2009-11-05 2016-06-30 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Бензодиазепиновый ингибитор бромодомена
MX2012005295A (es) 2009-11-05 2012-06-19 Glaxosmithkline Llc Inhibidor de bromodominio de benzodiazepina.
EP2955524A3 (en) 2009-11-05 2016-03-23 GlaxoSmithKline LLC Novel process
US8927561B2 (en) 2010-04-23 2015-01-06 Kineta, Inc. Pyrimidinedione anti-viral compounds
JP6022442B2 (ja) 2010-05-14 2016-11-09 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 男性用避妊組成物および使用方法
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
MX354217B (es) 2010-05-14 2018-02-19 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
EP2569429A4 (en) 2010-05-14 2013-09-25 Dana Farber Cancer Inst Inc COMPOSITIONS AND METHODS FOR MODULATING METABOLISM
US9085582B2 (en) 2010-06-22 2015-07-21 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
CA2825028A1 (en) 2011-02-09 2012-08-16 F. Hoffman-La Roche Ag Heterocyclic compounds as pi3 kinase inhibitors
WO2012116170A1 (en) 2011-02-23 2012-08-30 Ming-Ming Zhou Inhibitors of bromodomains as modulators of gene expression
US9090628B2 (en) 2011-03-21 2015-07-28 Genentech, Inc. Benzoxazepin compounds selective for PI3K P110 delta and methods of use
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
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
CA2840380A1 (en) 2011-06-24 2012-12-27 Dana-Farber Cancer Institute, Inc. 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
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, 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
WO2013029548A1 (en) 2011-08-31 2013-03-07 Otsuka Pharmaceutical Co., Ltd. Quinolone compound
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
WO2013043553A1 (en) 2011-09-22 2013-03-28 Glaxosmithkline Llc Pyrrolopyridinone compounds and methods for treating hiv
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
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
SI2773354T1 (sl) 2011-11-01 2019-08-30 Resverlogix Corp. Peroralne formulacije s takojšnjim sproščanjem za substituirane kinazolinone
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
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
HK1206744A1 (en) 2012-04-20 2016-01-15 Abbvie Inc. Isoindolone derivatives
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
EP2858982A4 (en) 2012-06-12 2015-11-11 Abbvie Inc PYRIDINONE AND PYRIDAZINONE DERIVATIVES
WO2014001356A1 (en) 2012-06-25 2014-01-03 Oncoethix Sa Method of treating lymphoma using thienotriazolodiazepine compounds
US9610332B2 (en) 2012-07-18 2017-04-04 Massachusetts Institute Of Technology Compositions and methods for modulating BRD4 bioactivity
EA201590356A1 (ru) 2012-08-16 2015-07-30 Байер Фарма Акциенгезельшафт 2,3-бензодиазепины
ES2653990T3 (es) 2012-08-16 2018-02-09 Glaxosmithkline Llc Benzodiazepinas para tratamiento del cáncer de pulmón de células pequeñas
ES2625959T3 (es) 2012-09-28 2017-07-21 Bayer Pharma Aktiengesellschaft 5-Aril-triazolo-azepinas inhibidoras de la proteína BET
KR20150100613A (ko) 2012-09-28 2015-09-02 온코에틱스 게엠베하 티에노트리아졸로디아제핀 화합물을 함유하는 약제학적 제제
ES2763601T3 (es) 2012-11-09 2020-05-29 Medicines For Malaria Venture Mmv Derivados de heteroarilo y sus usos
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
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
WO2014095774A1 (de) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydropyridopyrazinone
WO2014095775A1 (de) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydrochinoxalinone
KR20150096794A (ko) 2012-12-21 2015-08-25 제니쓰 에피제네틱스 코포레이션 브로모도메인 저해제로서의 신규한 헤테로사이클릭 화합물
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
CN105189488B (zh) 2013-02-27 2018-07-24 百时美施贵宝公司 用作溴区结构域抑制剂的咔唑化合物
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
MX2015012005A (es) 2013-03-11 2016-04-04 Abbvie Inc Inhibidores de bromodominio.
US9675697B2 (en) 2013-03-11 2017-06-13 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
MX2015012158A (es) 2013-03-11 2015-12-01 Abbvie Inc Inhibidores de bomodominio tetraciclicos fusionados.
CN105026403B (zh) 2013-03-12 2018-05-18 艾伯维公司 四环布罗莫结构域抑制剂
US9493411B2 (en) 2013-03-12 2016-11-15 Abbvie Inc. Pyrrole-3-carboxamide bromodomain inhibitors
KR20150126696A (ko) 2013-03-12 2015-11-12 애브비 인코포레이티드 디하이드로-피롤로피리디논 브로모도메인 억제제
RU2655727C9 (ru) 2013-03-14 2018-07-06 ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед Фуропиридины в качестве ингибиторов бромодоменов
MX367420B (es) 2013-03-14 2019-08-21 Convergene Llc Metodos y composiciones para inhibicion de proteinas que contienen bromodominio.
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
HRP20182179T1 (hr) 2013-03-14 2019-02-22 Glaxosmithkline Intellectual Property (No. 2) Limited 2,3-disupstituirani 1-acil-4-amino-1,2,3,4-tetrahidrokonolin derivati i njihova uporaba kao inhibitora bromodomena
SG11201506687RA (en) 2013-03-15 2015-09-29 Plexxikon Inc Heterocyclic compounds and uses thereof
AU2014236606A1 (en) 2013-03-15 2015-09-24 Epigenetix, Inc. Oxazolo(5,4-c)quinolin-2-one compounds as bromodomain inhibitors
ES2755827T3 (es) 2013-03-15 2020-04-23 Incyte Holdings Corp Heterciclos tricíclicos como inhibidores de proteína BET
US9102684B2 (en) 2013-03-27 2015-08-11 Boehringer Ingelheim International Gmbh Indolinone analogues
WO2014154762A1 (en) 2013-03-27 2014-10-02 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
EP2996689A1 (en) 2013-04-17 2016-03-23 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
EP2989096B1 (en) 2013-04-26 2019-04-10 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
WO2014191894A1 (en) 2013-05-27 2014-12-04 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
KR20160012197A (ko) 2013-05-28 2016-02-02 노파르티스 아게 피라졸로-피롤리딘-4-온 유도체 및 질환의 치료에서의 그의 용도
US9624247B2 (en) 2013-05-28 2017-04-18 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease
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.
CN105492436A (zh) 2013-06-17 2016-04-13 拜耳制药股份公司 取代的苯基-2,3-苯并二氮杂环庚三烯
WO2015004534A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
SG11201510409QA (en) 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
AU2014303193A1 (en) 2013-06-28 2016-01-28 Abbvie Inc. Bromodomain inhibitors
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
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
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
KR101672096B1 (ko) 2013-09-30 2016-11-02 주식회사 엘지화학 헤테로환 화합물 및 이를 포함하는 유기 발광 소자
DK3290407T3 (da) 2013-10-18 2020-03-23 Celgene Quanticel Res Inc Bromodomæneinhibitorer
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015081246A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
MX2016007346A (es) 2013-12-09 2016-09-13 Abbvie Inc Derivados de dihidropiridinona y dihidropiridazinona utiles como inhibidores de bromodominio.
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
PE20161021A1 (es) 2014-01-09 2016-11-09 Orion Corp Derivados heterociclicos biciclicos como inhibidores de bromodominio
AU2015222887B2 (en) 2014-02-28 2019-06-27 The Regents Of The University Of Michigan 9H-pyrimido[4,5-b]indoles and related analogs as BET bromodomain inhibitors
CR20160544A (es) 2014-04-23 2017-01-13 Takeda Pharmaceuticals Co Compuesto heterocíclico que contiene nitrógeno
EP3674302B1 (en) * 2014-04-23 2023-03-01 Incyte Holdings Corporation 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
US9822105B2 (en) 2014-04-23 2017-11-21 Basf Se Diaminotriazine compounds as herbicides
AU2015252940A1 (en) 2014-05-02 2016-11-17 Kay NOEL Method of treating resistant non-Hodgkin lymphoma, medulloblastoma, and/or ALK+non-small cell lung cancer using thienotriazolodiazepine compounds
WO2015168621A1 (en) 2014-05-02 2015-11-05 Oncoethix Sa Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds
KR20170002610A (ko) 2014-05-08 2017-01-06 온코에틱스 게엠베하 티에노트리아졸로디아제핀 화합물을 사용한 삼중 음성 유방암의 치료 방법
WO2015169953A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating glioma using thienotriazolodiazepine compounds
US10065951B2 (en) 2014-05-30 2018-09-04 Icahn School Of Medicine At Mount Sinai Small molecule transcription modulators of bromodomains
TR201906788T4 (tr) 2014-06-20 2019-05-21 Constellation Pharmaceuticals Inc 2-((4s)-6-(4-klorofenil)-1-metil-4h-benzo[c]izoksazolo[4,5-e]azepın-4-il)asetamidin kristal formları.
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
PE20170695A1 (es) 2014-10-24 2017-05-26 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
US10259809B2 (en) 2015-02-03 2019-04-16 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
HK1253539A1 (en) 2015-05-29 2019-06-21 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
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
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
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
CN108770356A (zh) 2016-02-05 2018-11-06 正大天晴药业集团股份有限公司 溴区结构域蛋白抑制剂的三环类化合物及其制备、药物组合物和用途
CN114366748A (zh) 2016-06-20 2022-04-19 因赛特公司 Bet抑制剂的结晶固体形式
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
KR102702503B1 (ko) 2024-09-05
IL248415B (en) 2020-03-31
TW201938559A (zh) 2019-10-01
HRP20230340T1 (hr) 2023-06-09
CA2946731C (en) 2022-06-07
NZ725930A (en) 2023-04-28
MX2016013851A (es) 2017-07-14
SG10201809353TA (en) 2018-11-29
CY1122948T1 (el) 2021-10-29
HUE049627T2 (hu) 2020-09-28
US20240002381A1 (en) 2024-01-04
IL273049B (en) 2021-03-25
MY180775A (en) 2020-12-09
IL281263B (en) 2021-09-30
SG11201608843TA (en) 2016-11-29
KR20160145796A (ko) 2016-12-20
EA201692134A1 (ru) 2017-02-28
TW201625607A (zh) 2016-07-16
NZ763740A (en) 2023-06-30
CN106414442B (zh) 2019-03-15
JP2017513879A (ja) 2017-06-01
TWI735002B (zh) 2021-08-01
US9957268B2 (en) 2018-05-01
ECSP16088983A (es) 2017-05-31
US11059821B2 (en) 2021-07-13
CR20160542A (es) 2017-04-25
MA39985B1 (fr) 2020-03-31
MY198727A (en) 2023-09-20
DK3134403T3 (en) 2020-03-09
EA034972B1 (ru) 2020-04-13
EP3134403B1 (en) 2020-02-12
LT3674302T (lt) 2023-06-12
CR20200231A (es) 2020-09-11
US10472358B2 (en) 2019-11-12
US20180312506A1 (en) 2018-11-01
HUE061770T2 (hu) 2023-08-28
US20210300925A1 (en) 2021-09-30
IL248415A0 (en) 2016-11-30
AU2015249810A1 (en) 2015-10-29
US20150307493A1 (en) 2015-10-29
AR100160A1 (es) 2016-09-14
AU2021200450A1 (en) 2021-02-25
KR20220113552A (ko) 2022-08-12
BR112016024626B1 (pt) 2023-03-21
PL3134403T3 (pl) 2020-07-13
CN106414442A (zh) 2017-02-15
LT3134403T (lt) 2020-05-11
US10781209B2 (en) 2020-09-22
BR112016024626A8 (pt) 2021-07-20
UA119870C2 (uk) 2019-08-27
PL3674302T3 (pl) 2023-07-24
EA202090371A1 (ru) 2020-06-30
ME03763B (me) 2021-04-20
DK3674302T3 (da) 2023-04-03
US20200377502A1 (en) 2020-12-03
US20250145621A1 (en) 2025-05-08
SI3674302T1 (sl) 2023-07-31
AU2019205984B2 (en) 2020-10-29
KR20240134245A (ko) 2024-09-06
EP4218766A1 (en) 2023-08-02
IL273049A (en) 2020-04-30
US11702416B2 (en) 2023-07-18
CY1126052T1 (el) 2023-11-15
SI3134403T1 (sl) 2020-07-31
FI3674302T3 (fi) 2023-04-27
SMT202300154T1 (it) 2023-07-20
PT3134403T (pt) 2020-05-18
RS64231B1 (sr) 2023-06-30
JP2019206584A (ja) 2019-12-05
EP3134403A1 (en) 2017-03-01
KR102430144B1 (ko) 2022-08-08
MX2020011035A (es) 2020-10-28
US20170158689A1 (en) 2017-06-08
ES2784846T3 (es) 2020-10-01
AU2021200450B2 (en) 2022-08-04
HRP20200564T1 (hr) 2020-06-26
MX376174B (es) 2025-03-07
US9540368B2 (en) 2017-01-10
BR112016024626A2 (pt) 2017-08-15
MY207899A (en) 2025-03-27
PH12016502115A1 (en) 2017-01-16
JP6572237B2 (ja) 2019-09-04
EP3674302B1 (en) 2023-03-01
PH12016502115B1 (en) 2020-07-01
PT3674302T (pt) 2023-05-10
US20200048251A1 (en) 2020-02-13
AU2015249810A8 (en) 2016-11-24
CL2016002681A1 (es) 2017-02-03
CA2946731A1 (en) 2015-10-29
AU2019205984A1 (en) 2019-08-01
WO2015164480A1 (en) 2015-10-29
IL281263A (en) 2021-04-29
SMT202000133T1 (it) 2020-05-08
TWI672301B (zh) 2019-09-21
EP3674302A1 (en) 2020-07-01
US12227502B2 (en) 2025-02-18
RS60139B1 (sr) 2020-05-29
AU2015249810B2 (en) 2019-04-18
JP6745390B2 (ja) 2020-08-26
NZ763737A (en) 2023-04-28
EA039678B1 (ru) 2022-02-24
ES2942723T3 (es) 2023-06-06

Similar Documents

Publication Publication Date Title
PE20170144A1 (es) 1h-pirrolo[2,3-c] piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h)-onas como inhibidores de proteinas bet
CO2017003132A2 (es) Inhibidores de la aldosterona sintasa derivados de la 2,6-diazaspiro[3.3]heptán-6-il]-3-piridil]isoindolín-1-ona o 2,7-diazaspiro[3.5]nonán-2-il]-3-piridil]isoindolín-1-ona
PE20191245A1 (es) Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim
PE20171240A1 (es) Derivados de 4h-pirrol[3,2-c]piridin-4-ona
AR088449A1 (es) Benzilindazoles sustituidos
MX2021007665A (es) Metodos novedosos.
CR20160337A (es) Nuevas heteroarildihidropirimidinas 6-fusionadas para el tratamiento y la profilaxis de la infección por virus de la hepatitis b
PE20130376A1 (es) [1,8]naftiridinas sustituidas por 2,4-diarilo como inhibidores de quinasas para uso contra el cancer
PH12015501934A1 (en) New octahydro - pyrrolo [3,4-c] - pyrrole derivatives and analogs thereof as autotaxin inhibitors
CR20140091A (es) Nuevos derivados dihidroquinolina-2-ona
PE20130306A1 (es) Morfolinopirimidinas y su uso en terapia
AR097431A1 (es) Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim
ES2600636T3 (es) Spiro-[1,3]-oxazinas y spiro-[1,4]-oxazepinas como inhibidores de BACE1 y/o BACE2
CR20140089A (es) Nuevos derivados bicíclicos de dihidroquinolina-2-ona
UY35377A (es) Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y métodos de uso
AR088029A1 (es) Compuestos de pirimidina sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del dolor, accidentes cerebrovasculares, epilepsia y otras enfermedades del sistema nervioso central
PH12016500643B1 (en) NEW OCTAHYDRO-CYCLOBUTA [1,2-c;3,4-c'] DIPYRROL-2-YL
PE20141352A1 (es) Fenil-3-aza-biciclo[3,1,0]hex-3-il-metanonas y su uso como medicamento
CR20150378A (es) Compuestos tetracíclicos sustituidos con heterociclo y métodos de uso de los mismos para el tratamiento de enfermedades víricas
PE20180478A1 (es) Compuestos triciclicos y su uso como inhibidores de la fosfodiesterasa
PE20190339A1 (es) 1h-pirazolo[4,3-b] piridinas como inhibidores de pde1
PE20170501A1 (es) Un procedimiento que comprende compuestos que administran a un sujeto infectado con neisseria gonorrhoeae
PE20160934A1 (es) (aza) piridopirazolopirimidinonas e indazolopirimidinonas como inhibidores de fibrinolisis
PE20160201A1 (es) Bencil-1h-pirazol[3,4-b]piridinas y su uso
CO2017000980A2 (es) Compuestos derivados de imidazo[1,2-b]piridazin-2-carboxamida e imidazo[1,2- b]piridazin-2-ilmetanona activos como inhibidores selectivos de la fosfodiesterasa 4a (pde4a)

Legal Events

Date Code Title Description
FG Grant, registration