BR112015021983B1 - Compostos heterocíclicos, composições farmacêuticas que os compreendem e usos dos mesmos - Google Patents

Compostos heterocíclicos, composições farmacêuticas que os compreendem e usos dos mesmos Download PDF

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Publication number
BR112015021983B1
BR112015021983B1 BR112015021983-7A BR112015021983A BR112015021983B1 BR 112015021983 B1 BR112015021983 B1 BR 112015021983B1 BR 112015021983 A BR112015021983 A BR 112015021983A BR 112015021983 B1 BR112015021983 B1 BR 112015021983B1
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BR
Brazil
Prior art keywords
cancer
optionally substituted
cell
substituents
tumor
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BR112015021983-7A
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English (en)
Portuguese (pt)
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BR112015021983A2 (pt
BR112015021983A8 (pt
Inventor
Jiazhong Zhang
John Buell
Katrina Chan
Prabha N. Ibrahim
Jack Lin
Phuongly Pham
Songyuan Shi
Wayne Spevak
Guoxian Wu
Jeffrey Wu
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Plexxikon, Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50439534&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112015021983(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Plexxikon, Inc filed Critical Plexxikon, Inc
Publication of BR112015021983A2 publication Critical patent/BR112015021983A2/pt
Publication of BR112015021983A8 publication Critical patent/BR112015021983A8/pt
Publication of BR112015021983B1 publication Critical patent/BR112015021983B1/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61K31/695—Silicon compounds
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biochemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
BR112015021983-7A 2013-03-15 2014-03-14 Compostos heterocíclicos, composições farmacêuticas que os compreendem e usos dos mesmos BR112015021983B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361798856P 2013-03-15 2013-03-15
US61/798,856 2013-03-15
US201361872347P 2013-08-30 2013-08-30
US61/872,347 2013-08-30
PCT/US2014/029701 WO2014145051A1 (en) 2013-03-15 2014-03-14 Heterocyclic compounds and uses thereof

Publications (3)

Publication Number Publication Date
BR112015021983A2 BR112015021983A2 (pt) 2017-07-18
BR112015021983A8 BR112015021983A8 (pt) 2019-12-03
BR112015021983B1 true BR112015021983B1 (pt) 2022-03-03

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ID=50439534

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BR112015021983-7A BR112015021983B1 (pt) 2013-03-15 2014-03-14 Compostos heterocíclicos, composições farmacêuticas que os compreendem e usos dos mesmos

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US (2) US9718847B2 (enExample)
EP (1) EP2970265B1 (enExample)
JP (1) JP6325078B2 (enExample)
KR (1) KR102244719B1 (enExample)
CN (1) CN105073747B (enExample)
AU (1) AU2014233437B2 (enExample)
BR (1) BR112015021983B1 (enExample)
CA (1) CA2903293C (enExample)
CL (1) CL2015002565A1 (enExample)
CY (1) CY1120703T1 (enExample)
DK (1) DK2970265T3 (enExample)
ES (1) ES2688575T3 (enExample)
HR (1) HRP20181392T1 (enExample)
HU (1) HUE039380T2 (enExample)
IL (1) IL240836B (enExample)
LT (1) LT2970265T (enExample)
MX (1) MX376271B (enExample)
NZ (1) NZ630875A (enExample)
PE (1) PE20151997A1 (enExample)
PH (1) PH12015501996B1 (enExample)
PL (1) PL2970265T3 (enExample)
PT (1) PT2970265T (enExample)
RS (1) RS57733B1 (enExample)
RU (1) RU2680100C9 (enExample)
SG (1) SG11201506687RA (enExample)
SI (1) SI2970265T1 (enExample)
SM (1) SMT201800650T1 (enExample)
TW (1) TWI634111B (enExample)
UY (1) UY35485A (enExample)
WO (1) WO2014145051A1 (enExample)
ZA (1) ZA201506434B (enExample)

Families Citing this family (106)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
BRPI0814423B1 (pt) 2007-07-17 2022-04-19 Plexxikon, Inc Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
MX2012005827A (es) 2009-11-18 2012-06-19 Plexxikon Inc Compuestos y metodos para la modulacion de cinasas, e indicaciones para ello.
WO2011079133A2 (en) 2009-12-23 2011-06-30 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
CN103517710B (zh) 2011-02-07 2017-05-31 普莱希科公司 用于激酶调节的化合物
SG194847A1 (en) 2011-05-17 2013-12-30 Plexxikon Inc Kinase modulation and indications therefor
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
CN104981247A (zh) 2012-09-06 2015-10-14 普莱希科公司 用于激酶调节的化合物和方法及其适应症
US9676748B2 (en) 2012-12-21 2017-06-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
ES2649156T3 (es) 2013-01-14 2018-01-10 Incyte Holdings Corporation Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim
CA2897333C (en) 2013-01-15 2021-07-06 Incyte Corporation Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors
DK2970265T3 (en) 2013-03-15 2018-10-01 Plexxikon Inc HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
ES2909778T3 (es) 2013-03-15 2022-05-10 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de proteína BET para su uso en el tratamiento de una enfermedad proliferativa en combinación con un inhibidor de Janus quinasas
RU2015149937A (ru) 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
CN104230922B (zh) * 2013-06-19 2016-12-28 中国科学院上海药物研究所 一类五元杂环并吡啶类化合物及其制备方法和用途
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
WO2015002754A2 (en) * 2013-06-21 2015-01-08 Zenith Epigenetics Corp. Novel bicyclic bromodomain inhibitors
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
CR20160135A (es) 2013-08-23 2016-08-05 Incyte Corp Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de cinasas pim
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
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
SG10201809353TA (en) 2014-04-23 2018-11-29 Incyte Corp 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
ES2774177T3 (es) 2014-09-15 2020-07-17 Plexxikon Inc Compuestos heterocíclicos y usos de estos
GB201419015D0 (en) * 2014-10-24 2014-12-10 Orca Pharmaceuticals Ltd Compounds
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
WO2016087942A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridines as bromodomain inhibitors
US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
US10231953B2 (en) 2014-12-17 2019-03-19 Zenith Epigenetics Ltd. Inhibitors of bromodomains
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
GB201504689D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Chemical compounds
WO2016164641A1 (en) 2015-04-08 2016-10-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
AR104259A1 (es) * 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
EP3581573B1 (en) 2015-05-06 2022-07-06 Plexxikon Inc. Synthesis of a compound that modulates kinases
SG10201912355TA (en) 2015-05-06 2020-02-27 Plexxikon Inc Solid forms of a compound modulating kinases
WO2016191295A1 (en) 2015-05-22 2016-12-01 Plexxikon Inc. Solid forms of a compound for modulating kinases
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
AU2016291158B2 (en) * 2015-07-09 2020-04-30 Janssen Pharmaceutica Nv Substituted 4-azaindoles and their use as GluN2B receptor modulators
WO2017019804A2 (en) 2015-07-28 2017-02-02 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN108290856A (zh) 2015-08-11 2018-07-17 尼奥迈德研究所 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
WO2017024406A1 (en) 2015-08-11 2017-02-16 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
AU2016305515A1 (en) 2015-08-12 2018-03-08 Neomed Institute Substituted benzimidazoles, their preparation and their use as pharmaceuticals
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Ｐｉｍ激酶抑制劑之鹽
CN108137585B (zh) * 2015-09-21 2021-10-22 普莱希科公司 杂环化合物及其应用
TW201718546A (zh) 2015-10-02 2017-06-01 英塞特公司 適用作pim激酶抑制劑之雜環化合物
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
SG11201804711RA (en) 2015-12-07 2018-07-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
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
AU2017232610B2 (en) 2016-03-16 2021-07-22 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
TWI830533B (zh) 2016-06-20 2024-01-21 美商英塞特公司 Ｂｅｔ抑制劑之結晶固體形式
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症
TW201819376A (zh) 2016-10-06 2018-06-01 比利時商健生藥品公司 經取代之１Ｈ－咪唑並［４，５－ｂ］吡啶－２（３Ｈ）－酮及其作為ＧＬＵＮ２Ｂ受體調節劑之用途
MA47099A (fr) 2016-12-22 2021-05-12 Incyte Corp Composés hétéroaromatiques bicycliques utilisés en tant qu'immunomodulateurs
BR112019012993A2 (pt) * 2016-12-22 2019-12-03 Incyte Corporation derivados de benzo-oxazol como imunomoduladores
WO2018136202A2 (en) 2016-12-23 2018-07-26 Plexxikon Inc. Compounds and methods for cdk8 modulation and indications therefor
CN108314680A (zh) * 2017-01-16 2018-07-24 凯惠科技发展(上海)有限公司 一种含芳环化合物、其制备方法、药物组合物及应用
WO2018175311A1 (en) * 2017-03-20 2018-09-27 Plexxikon Inc. Crystalline forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1h- pyrrolo[3,2-b]pyridin-3-yl)benzoic acid that inhibits bromodomain
WO2018226846A1 (en) 2017-06-07 2018-12-13 Plexxikon Inc. Compounds and methods for kinase modulation
CN109111427B (zh) * 2017-06-22 2023-06-02 中国科学院广州生物医药与健康研究院 一种吲哚类化合物及其应用
CA3070505C (en) 2017-07-25 2023-09-26 Plexxikon Inc. Formulations of a compound modulating kinases
EP3694855A1 (en) * 2017-10-13 2020-08-19 Plexxikon Inc. Solid forms of a compound for modulating kinases
CN112165958A (zh) 2017-10-27 2021-01-01 普莱希科公司 调制激酶的化合物的制剂
CN111542318A (zh) * 2017-11-10 2020-08-14 密歇根大学董事会 Ash1l降解剂及用其进行治疗的方法
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
EP3305786A3 (de) 2018-01-22 2018-07-25 Bayer CropScience Aktiengesellschaft Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel
EP3768666A1 (en) 2018-03-20 2021-01-27 Plexxikon Inc. Compounds and methods for ido and tdo modulation, and indications therefor
HRP20230090T1 (hr) 2018-03-30 2023-03-17 Incyte Corporation Heterociklički spojevi kao imunomodulatori
HUE061503T2 (hu) 2018-05-11 2023-07-28 Incyte Corp Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok
WO2020015744A1 (zh) * 2018-07-19 2020-01-23 南京明德新药研发有限公司 氮杂吲哚衍生物及其作为FGFR和C-Met抑制剂的应用
AU2020206884A1 (en) * 2019-01-09 2021-08-05 Beth Israel Deaconess Medical Center, Inc. Modulators of Pin1 activity and uses thereof
TW202104221A (zh) * 2019-04-09 2021-02-01 美商普雷辛肯公司 用於ep300或cbp調節及其適應症之化合物及方法
CN110015985B (zh) * 2019-05-16 2022-05-13 河南师范大学 2-(α-氘-α-羟基-α-芳基/烷基)氮杂芳烃类化合物及其制备方法和应用
US11618750B2 (en) 2019-06-14 2023-04-04 Janssen Pharmaceutica Nv Substituted pyrazolo-pyridine amides and their use as GluN2B receptor modulators
AU2020291188A1 (en) 2019-06-14 2022-01-20 Janssen Pharmaceutica Nv Substituted heteroaromatic Pyrazolo-pyridines and their use as GluN2B receptor modulators
BR112021025132A2 (pt) 2019-06-14 2022-01-25 Janssen Pharmaceutica Nv Carbamatos de piridina e seu uso como moduladores do receptor glun2b
PH12021552839A1 (en) 2019-06-14 2022-10-03 Janssen Pharmaceutica Nv Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators
CN113993583A (zh) 2019-06-14 2022-01-28 詹森药业有限公司 取代的吡唑并[4,3-b]吡啶及其作为GLUN2B受体调节剂的用途
US11459336B2 (en) 2019-06-14 2022-10-04 Janssen Pharmaceutica Nv Pyrazine carbamates and their use as GluN2B receptor modulators
BR112021024117A2 (pt) 2019-06-14 2022-03-22 Janssen Pharmaceutica Nv Pirazolo-pirazinas substituídas e seu uso como moduladores do receptor de glun2b
CN112174945B (zh) * 2019-07-02 2022-06-07 四川大学 具有抗癌作用的吲唑类化合物及其制备方法和用途
PH12022550754A1 (en) 2019-09-30 2023-08-23 Incyte Corp Pyrido[3,2-d]pyrimidine compounds as immunomodulators
KR102270026B1 (ko) * 2020-01-31 2021-06-28 현대약품 주식회사 (3s)-3-(4-(3-(1,4-다이옥사스파이로[4,5]데스-7-엔-8-일)벤질옥시)페닐)헥스-4-이노익산의 품질 평가 방법
AU2021261383A1 (en) 2020-04-23 2022-11-17 Opna Bio SA Compounds and methods for CD73 modulation and indications therefor
CN115605460A (zh) 2020-04-29 2023-01-13 普莱希科公司（Us） 杂环化合物的合成
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
EP4178982A1 (en) 2020-07-13 2023-05-17 Precirix N.V. Antibody fragment against folr1
AU2021327375A1 (en) 2020-08-21 2023-03-16 Opna Bio SA Combinational drug anticancer therapies
MX2023005362A (es) 2020-11-06 2023-06-22 Incyte Corp Proceso para hacer un inhibidor de proteina de muerte programada 1 (pd-1)/ligando de muerte programada 1 (pd-l1) y sales y formas cristalinas del mismo.
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
CN113402515B (zh) * 2021-05-12 2022-05-27 四川大学华西医院 一种吲哚类化合物及其制备方法和用途
CA3218462A1 (en) * 2021-05-14 2022-11-17 Liang Wang Acid addition salt of rock inhibitor, and crystal form, composition and pharmaceutical use thereof
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
CN114773174B (zh) * 2022-04-29 2024-05-28 常州大学 α-氘代羰基类化合物的合成方法
JP2025517625A (ja) 2022-05-02 2025-06-10 プレシリックス・ナームローゼ・ベンノートシヤープ プレターゲティング
CN114984011A (zh) * 2022-07-11 2022-09-02 中南大学湘雅二医院 吡咯并吡啶类化合物在制备治疗狼疮药物中的应用
CN116925018B (zh) * 2023-07-19 2025-02-07 宁夏大学 大黄酸-哌嗪-呋喃酮杂化物及其制备方法和应用
CN119219631B (zh) * 2024-12-04 2025-04-18 山东大学 一种bet蛋白溴结构域bd1选择性共价抑制剂及其制备方法与应用

Family Cites Families (113)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5317103A (en) * 1991-01-15 1994-05-31 Merck Sharp & Dohme Limited Indole-substituted five-membered heteroaromatic compounds as 5-HT1 agonists
US5998438A (en) * 1996-11-26 1999-12-07 Allelix Biopharmaceuticals, Inc. 5-cyclo indole compounds
RU2219178C2 (ru) 1997-10-20 2003-12-20 Ф.Хоффманн-Ля Рош Аг Бициклические производные, фармацевтическая композиция на их основе и промежуточные соединения
US6358992B1 (en) * 1998-11-25 2002-03-19 Cell Pathways, Inc. Method of inhibiting neoplastic cells with indole derivatives
US6281356B1 (en) 1999-12-22 2001-08-28 Hoffmann-La Roche Inc. Substituted pyrroles
CN100379734C (zh) * 1999-12-24 2008-04-09 阿文蒂斯药物有限公司 氮杂吲哚类化合物
GB0031315D0 (en) * 2000-12-21 2001-02-07 Glaxo Group Ltd Indole derivatives
US20040110785A1 (en) * 2001-02-02 2004-06-10 Tao Wang Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
US20040171062A1 (en) 2002-02-28 2004-09-02 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
KR20050013534A (ko) * 2002-03-28 2005-02-04 에자이 가부시키가이샤 ｃ─Ｊｕｎ Ｎ─말단 키나아제 억제용 아자인돌
WO2004014851A2 (en) * 2002-08-09 2004-02-19 Merck & Co., Inc. Tyrosine kinase inhibitors
BR122012021252B8 (pt) 2002-09-06 2021-05-25 Cerulean Pharma Inc polímeros à base de ciclodextrina para o fornecimento de agentes terapêuticos ligados a eles por covalência
US20040142864A1 (en) 2002-09-16 2004-07-22 Plexxikon, Inc. Crystal structure of PIM-1 kinase
US20050048573A1 (en) 2003-02-03 2005-03-03 Plexxikon, Inc. PDE5A crystal structure and uses
US20040167188A1 (en) 2003-02-14 2004-08-26 Zhili Xin Protein-tyrosine phosphatase inhibitors and uses thereof
US20050170431A1 (en) 2003-02-28 2005-08-04 Plexxikon, Inc. PYK2 crystal structure and uses
US7432375B2 (en) 2003-03-06 2008-10-07 Eisai R & D Management Co., Ltd. JNK inhibitors
SE0301569D0 (sv) * 2003-05-27 2003-05-27 Astrazeneca Ab Novel compounds
US20050079548A1 (en) 2003-07-07 2005-04-14 Plexxikon, Inc. Ligand development using PDE4B crystal structures
AU2004259738B2 (en) 2003-07-17 2011-11-17 Plexxikon, Inc. PPAR active compounds
US7348338B2 (en) 2003-07-17 2008-03-25 Plexxikon, Inc. PPAR active compounds
US20050164300A1 (en) 2003-09-15 2005-07-28 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
PT1696920E (pt) 2003-12-19 2015-01-14 Plexxikon Inc Compostos e métodos para o desenvolvimento de moduladores de ret
US20070066641A1 (en) 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
US7517970B2 (en) 2003-12-19 2009-04-14 Plexxikon, Inc. Nucleic acids encoding kinase and phosphatase enzymes, expression vectors and cells containing same
EP1742627A4 (en) 2004-05-06 2009-08-26 Plexxikon Inc PDE4B HEMMER AND ITS USE
WO2006009755A2 (en) 2004-06-17 2006-01-26 Plexxikon, Inc. Azaindoles modulating c-kit activity and uses therefor
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
MX2007001127A (es) 2004-07-27 2007-07-11 Sgx Pharmaceuticals Inc Moduladores de pirrolo-piridina cinasa.
CA2583428A1 (en) 2004-09-03 2006-03-09 Plexxikon, Inc. Bicyclic heteroaryl pde4b inhibitors
JP2008521831A (ja) 2004-11-30 2008-06-26 プレキシコン，インコーポレーテッド Ｐｐａｒ活性化合物
JP2008521829A (ja) 2004-11-30 2008-06-26 プレキシコン，インコーポレーテッド Ｐｐａｒ活性化合物
US20060160135A1 (en) 2004-12-08 2006-07-20 Weiru Wang SF-1 and LRH-1 modulator development
US20060183758A1 (en) * 2005-02-17 2006-08-17 Cb Research And Development, Inc. Method for synthesis of AZA-annelated pyrroles, thiophenes, and furans
KR20080027775A (ko) 2005-05-17 2008-03-28 플렉시콘, 인코퍼레이티드 피롤(２,３-ｂ)피리딘 유도체 단백질 키나제 억제제
PL1893612T3 (pl) 2005-06-22 2012-01-31 Plexxikon Inc Pochodne pirolo-[2,3-b]pirydyny jako inhibitory kinazy białkowej
JP5072594B2 (ja) * 2005-07-22 2012-11-14 塩野義製薬株式会社 Ｐｇｄ２受容体アンタゴニスト活性を有するインドール誘導体
BRPI0615948A2 (pt) 2005-09-07 2011-05-31 Plexxikon Inc composto ativo de ppar, sua composição, seu kit e seu uso
NZ567162A (en) 2005-09-07 2011-06-30 Plexxikon Inc 1, 3-disubstituted indole derivatives for use as PPAR modulators
AU2006287528A1 (en) 2005-09-07 2007-03-15 Plexxikon, Inc. 1 , 4 and 1 , 5-disubstituted indole derivatives for use as PPAR active compounds
US7696229B2 (en) 2006-02-17 2010-04-13 Memory Pharmaceuticals Corporation Compounds having 5-HT6 receptor affinity
ES2393132T3 (es) 2006-10-23 2012-12-18 Sgx Pharmaceuticals, Inc. Moduoladores de proteína quinasa de triazolopiridazina
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
JP2010514695A (ja) 2006-12-21 2010-05-06 プレキシコン，インコーポレーテッド キナーゼ調節のための化合物および方法およびそのための適応症
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
US8524917B2 (en) * 2007-01-11 2013-09-03 Allergan, Inc. 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
WO2008087933A1 (ja) * 2007-01-15 2008-07-24 Santen Pharmaceutical Co., Ltd. ＩκＢキナーゼβ阻害活性を有する新規インドール誘導体
MX2009008439A (es) * 2007-02-12 2009-08-13 Intermune Inc Nuevos inhibidores de la replicacion del virus de hepatitis c.
MX2009009290A (es) 2007-03-08 2009-09-10 Plexxikon Inc Compuestos activos en ppar.
PE20090159A1 (es) 2007-03-08 2009-02-21 Plexxikon Inc COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs
WO2008110508A1 (en) * 2007-03-09 2008-09-18 Glaxo Group Limited Pyrrolo-pyridine derivatives for the treatment of disorders associated with inappropriate ikk1 activity
DE102007028515A1 (de) * 2007-06-21 2008-12-24 Merck Patent Gmbh 6-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
BRPI0814423B1 (pt) 2007-07-17 2022-04-19 Plexxikon, Inc Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos
EA201000113A1 (ru) * 2007-08-01 2010-08-30 Пфайзер Инк. Пиразольные соединения
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
WO2009155052A1 (en) 2008-05-28 2009-12-23 Wyeth 3-substituted-1h-pyrrolo[2,3-b]pyridine and 3-substituted-1h-pyrrolo[3,2-b]pyridine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
EP2313411A1 (en) 2008-06-10 2011-04-27 Plexxikon, Inc. 5h-pyrr0l0 [2,3-b]pyrazine derivatives for kinase modulation, and indications therefor
US8110576B2 (en) 2008-06-10 2012-02-07 Plexxikon Inc. Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications
AR072008A1 (es) 2008-06-13 2010-07-28 Merck & Co Inc Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38
US8012992B2 (en) * 2008-06-30 2011-09-06 Allergan, Inc. Aza-indoles and related compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
DE102008031517A1 (de) * 2008-07-03 2010-01-07 Merck Patent Gmbh Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
WO2010068292A1 (en) 2008-12-12 2010-06-17 Ariad Pharmaceuticals, Inc. Azaindole derivatives as kinase inhibitors
WO2010104945A1 (en) 2009-03-11 2010-09-16 Plexxikon, Inc. Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of raf kinases
US8129404B2 (en) 2009-03-11 2012-03-06 Plexxikon Inc. Compounds and uses thereof
WO2010111527A1 (en) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
MY160737A (en) 2009-04-03 2017-03-15 Hoffmann La Roche Propane-i-sulfonic acid {3- [5-(4-chloro-phenyl) -1h -pyrrolo [2, 3-b] pyridine-3-carbonyl] -2,4 difluoro-phenyl} - amide compositions and uses thereof
SG175877A1 (en) 2009-05-04 2011-12-29 Plexxikon Inc Compounds and methods for inhibition of renin, and indications therefor
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
KR101256018B1 (ko) * 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
SG10201407129SA (en) 2009-11-06 2014-12-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
MX2012005827A (es) 2009-11-18 2012-06-19 Plexxikon Inc Compuestos y metodos para la modulacion de cinasas, e indicaciones para ello.
WO2011079133A2 (en) 2009-12-23 2011-06-30 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
AR081039A1 (es) * 2010-05-14 2012-05-30 Osi Pharmaceuticals Llc Inhibidores biciclicos fusionados de quinasa
US8642606B2 (en) 2010-09-29 2014-02-04 Plexxikon Inc. ZAP-70 active compounds
AU2011333472A1 (en) 2010-11-26 2013-06-06 Lupin Limited Bicyclic GPR119 modulators
DE102011009961A1 (de) * 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
CN103517710B (zh) 2011-02-07 2017-05-31 普莱希科公司 用于激酶调节的化合物
TWI558702B (zh) 2011-02-21 2016-11-21 普雷辛肯公司 醫藥活性物質的固態形式
SG194847A1 (en) 2011-05-17 2013-12-30 Plexxikon Inc Kinase modulation and indications therefor
BR112014009108A2 (pt) 2011-10-25 2017-04-18 Shionogi & Co derivado heterocíclico tendo atividade antagonista de receptor de pgd2
WO2013078254A1 (en) 2011-11-22 2013-05-30 Array Biopharma Inc. Bicyclic heteroaryl derivatives as kinase inhibitors
FR2984325A1 (fr) 2011-12-14 2013-06-21 Sanofi Sa Derives de pyrazolopyridine, leur procede de preparation et leur application en therapeutique
US20130158066A1 (en) 2011-12-20 2013-06-20 Hoffmann-La Roche Inc. 4-azaindole inhibitors of crac
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
CN104981247A (zh) 2012-09-06 2015-10-14 普莱希科公司 用于激酶调节的化合物和方法及其适应症
US9676748B2 (en) 2012-12-21 2017-06-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
SG11201507383WA (en) * 2013-03-12 2015-10-29 Abbvie Inc Dihydro-pyrrolopyridinone bromodomain inhibitors
DK2970265T3 (en) 2013-03-15 2018-10-01 Plexxikon Inc HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
RU2015149937A (ru) 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
WO2015002754A2 (en) 2013-06-21 2015-01-08 Zenith Epigenetics Corp. Novel bicyclic bromodomain inhibitors
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
ES2774177T3 (es) 2014-09-15 2020-07-17 Plexxikon Inc Compuestos heterocíclicos y usos de estos
WO2016164641A1 (en) 2015-04-08 2016-10-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
SG10201912355TA (en) 2015-05-06 2020-02-27 Plexxikon Inc Solid forms of a compound modulating kinases
EP3581573B1 (en) 2015-05-06 2022-07-06 Plexxikon Inc. Synthesis of a compound that modulates kinases
WO2016191295A1 (en) 2015-05-22 2016-12-01 Plexxikon Inc. Solid forms of a compound for modulating kinases
CN113893253A (zh) 2015-05-22 2022-01-07 普莱希科公司 用于治疗braf-v600相关的疾病的plx-8394或plx-7904
WO2017019804A2 (en) 2015-07-28 2017-02-02 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN108137585B (zh) 2015-09-21 2021-10-22 普莱希科公司 杂环化合物及其应用
SG11201804711RA (en) 2015-12-07 2018-07-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
AU2017232610B2 (en) 2016-03-16 2021-07-22 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症
WO2018136202A2 (en) 2016-12-23 2018-07-26 Plexxikon Inc. Compounds and methods for cdk8 modulation and indications therefor
WO2018175311A1 (en) 2017-03-20 2018-09-27 Plexxikon Inc. Crystalline forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1h- pyrrolo[3,2-b]pyridin-3-yl)benzoic acid that inhibits bromodomain
EP3694855A1 (en) 2017-10-13 2020-08-19 Plexxikon Inc. Solid forms of a compound for modulating kinases
CN112165958A (zh) 2017-10-27 2021-01-01 普莱希科公司 调制激酶的化合物的制剂

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