MA34284B1 - Indoles - Google Patents

Indoles

Info

Publication number
MA34284B1
MA34284B1 MA35415A MA35415A MA34284B1 MA 34284 B1 MA34284 B1 MA 34284B1 MA 35415 A MA35415 A MA 35415A MA 35415 A MA35415 A MA 35415A MA 34284 B1 MA34284 B1 MA 34284B1
Authority
MA
Morocco
Prior art keywords
indoles
useful
formula
relates
present
Prior art date
Application number
MA35415A
Other languages
English (en)
Inventor
James Brackley
Joelle Lorraine Burgess
Seth Grant
Neil Johnson
Steven D Knight
Louis Lafrance
William H Miller
Kenneth Newlander
Stuart Romeril
Meagan B Rouse
Xinrong Tian
Sharad Kumar Verma
Original Assignee
Glaxosmithkline Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Publication of MA34284B1 publication Critical patent/MA34284B1/fr

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La présente invention concerne des indoles de formule (I) dont les divers groupes sont définis dans la présente et qui sont utiles pour traiter les cancers.
MA35415A 2010-05-07 2011-05-05 Indoles MA34284B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33230910P 2010-05-07 2010-05-07
PCT/US2011/035336 WO2011140324A1 (fr) 2010-05-07 2011-05-05 Indoles

Publications (1)

Publication Number Publication Date
MA34284B1 true MA34284B1 (fr) 2013-06-01

Family

ID=44904072

Family Applications (1)

Application Number Title Priority Date Filing Date
MA35415A MA34284B1 (fr) 2010-05-07 2011-05-05 Indoles

Country Status (33)

Country Link
US (5) US8536179B2 (fr)
EP (2) EP2566327B1 (fr)
JP (1) JP5864545B2 (fr)
KR (1) KR20130062290A (fr)
CN (1) CN102970869B (fr)
AU (1) AU2011248068B2 (fr)
BR (1) BR112012028556A2 (fr)
CA (1) CA2798622C (fr)
CL (1) CL2012003110A1 (fr)
CR (1) CR20120565A (fr)
CY (1) CY1119006T1 (fr)
DK (1) DK2566327T3 (fr)
DO (1) DOP2012000282A (fr)
EA (1) EA023788B1 (fr)
ES (1) ES2627085T3 (fr)
HR (1) HRP20170736T1 (fr)
HU (1) HUE034787T2 (fr)
IL (1) IL222878A (fr)
LT (1) LT2566327T (fr)
MA (1) MA34284B1 (fr)
ME (1) ME02757B (fr)
MX (1) MX2012012966A (fr)
MY (1) MY184101A (fr)
NZ (1) NZ603454A (fr)
PE (1) PE20130647A1 (fr)
PL (1) PL2566327T3 (fr)
PT (1) PT2566327T (fr)
RS (1) RS55874B1 (fr)
SG (1) SG185431A1 (fr)
SI (1) SI2566327T1 (fr)
UA (1) UA110112C2 (fr)
WO (1) WO2011140324A1 (fr)
ZA (1) ZA201208447B (fr)

Families Citing this family (117)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2534804T3 (es) 2010-05-07 2015-04-28 Glaxosmithkline Llc Indazoles
US20130102477A1 (en) 2010-06-23 2013-04-25 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
RU2765155C2 (ru) * 2010-09-10 2022-01-26 Эпизайм, Инк. Ингибиторы ezh2 человека и способы их применения
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
JP5908493B2 (ja) * 2010-12-01 2016-04-26 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーGlaxoSmithKline LLC インドール
WO2012118812A2 (fr) * 2011-02-28 2012-09-07 Epizyme, Inc. Composés hétéroaryles bicycliques substitués condensés en 6,5
AU2013203641B2 (en) * 2011-04-13 2014-08-21 Epizyme, Inc. Aryl-or heteroaryl-substituted benzene compounds
TW201733984A (zh) 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
JO3438B1 (ar) * 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
KR20140082742A (ko) * 2011-09-30 2014-07-02 글락소스미스클라인 엘엘씨 암을 치료하는 방법
EP2773754B1 (fr) 2011-11-04 2016-08-03 Glaxosmithkline Intellectual Property (No. 2) Limited Composés pour le traitement des maladies à mediation par cellule T
EP2780013A4 (fr) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc Modulateurs d'enzymes de modification par méthylation, compositions et utilisations associées
US9206128B2 (en) 2011-11-18 2015-12-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EA037918B1 (ru) 2011-12-21 2021-06-07 Новира Терапьютикс, Инк. Противовирусные агенты против гепатита в
US9085583B2 (en) * 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
ES2718900T3 (es) 2012-03-12 2019-07-05 Epizyme Inc Inhibidores de EZH2 humana y métodos de uso de los mismos
EP2828250B1 (fr) 2012-03-19 2021-03-10 Imperial College Innovations Limited Composes de quinazoline et leur application therapeutque
ES2745016T3 (es) * 2012-04-13 2020-02-27 Epizyme Inc Bromhidrato de N-((4,6-dimetil-2-oxo-L,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2H-piran-4-il)amino)-4-metil-4'-(morfolinometil)-[L,1'-bifenil]-3-carboxamida para su uso en el tratamiento de un trastorno proliferativo celular del sistema hematológico
WO2013173441A2 (fr) * 2012-05-16 2013-11-21 Glaxosmithkline Llc Inhibiteurs d'homologue d'activateur de zeste 2
EP2861988B1 (fr) 2012-06-14 2019-05-22 The Whitehead Institute for Biomedical Research Procédé à l'échelle du génome d'évaluation d'interactions entre des entités chimiques et leurs molécules cibles
UA123256C2 (uk) 2012-08-28 2021-03-10 ЯНССЕН САЙЄНСІЗ АЙРЛЕНД ЮСі Сульфамоїлариламіди та їх застосування як лікарських препаратів для лікування гепатиту b
EP2900653A1 (fr) 2012-09-28 2015-08-05 Pfizer Inc. Composés de benzamide et hétérobenzamide
PT2908823T (pt) 2012-10-15 2019-11-04 Epizyme Inc Métodos para tratamento do cancro
BR112015008487B1 (pt) 2012-10-15 2022-05-31 Epizyme, Inc Compostos de benzeno substituído, composição farmacêutica compreendendo os ditos compostos e uso terapêutico dos mesmos para tratar um distúrbio mediado por ezh2
CA2894657A1 (fr) * 2012-12-13 2014-07-10 Glaxosmithkline Llc Activateur d'inhibiteurs de l'homologue 2 de zeste
EP2934531A4 (fr) * 2012-12-19 2016-06-15 Glaxosmithkline Llc Combinaison
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
WO2014100665A1 (fr) * 2012-12-21 2014-06-26 Epizyme, Inc. Composés hétéroaryles bicycliques 1,4-pyridone
TWI629273B (zh) * 2013-02-11 2018-07-11 美商星宿藥物公司 甲基修飾酵素之調節劑、其組成物及用途
HUE034820T2 (en) 2013-02-28 2018-02-28 Janssen Sciences Ireland Uc Sulphamoyl arylamides and their use as medicaments for the treatment of hepatitis B
WO2014165128A2 (fr) * 2013-03-12 2014-10-09 Novira Therapeutics, Inc. Agents antiviraux contre l'hépatite b
EP2970134B1 (fr) 2013-03-14 2018-02-28 Epizyme, Inc. Derives de pyrazole comme inhibiteurs de prmt1 et leur utilisation
US9045455B2 (en) 2013-03-14 2015-06-02 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014144659A1 (fr) 2013-03-14 2014-09-18 Epizyme, Inc. Dérivés de pyrazole à titre d'inhibiteurs de prmt1 et leurs utilisations
EP2970137A1 (fr) 2013-03-14 2016-01-20 Epizyme, Inc. Inhibiteurs de l'arginine méthyltransférase et utilisations de ceux-ci
EP2970220A2 (fr) 2013-03-14 2016-01-20 Epizyme, Inc. Inhibiteurs de l'arginine méthyltransférase et utilisations de ceux-ci
RU2015139054A (ru) 2013-03-14 2017-04-19 Дженентек, Инк. Способы лечения рака и профилактики лекарственной резистентности рака
EP2970133B1 (fr) 2013-03-14 2018-10-24 Epizyme, Inc. Dérivés de pyrazole en tant qu'inhibiteurs de prmt1 et leurs utilisations
EP3363434A1 (fr) 2013-03-14 2018-08-22 Epizyme Inc Inhibiteurs de méthyltransférase d'arginine et leurs utilisations
WO2014153214A1 (fr) 2013-03-14 2014-09-25 Epizyme, Inc. Inhibteurs de l'arginine méthyltransférase et utilisations de ceux-ci
BR112015022785A2 (pt) 2013-03-14 2017-07-18 Epizyme Inc composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt
WO2014151142A1 (fr) * 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulateurs d'enzymes de modification du méthyle, compositions et utilisations associées
WO2014155301A1 (fr) * 2013-03-26 2014-10-02 Piramal Enterprises Limited Composés bicycliques substitués utilisés comme inhibiteurs d'ezh2
ES2640063T3 (es) 2013-04-03 2017-10-31 Janssen Sciences Ireland Uc Derivados de n-fenil-carboxamida y su uso como medicamentos para el tratamiento de la hepatitis B
EP2991980B1 (fr) 2013-04-30 2019-01-02 Glaxosmithkline Intellectual Property (No. 2) Limited Activateur d'inhibiteurs de l'homologue 2 de zeste
JO3603B1 (ar) 2013-05-17 2020-07-05 Janssen Sciences Ireland Uc مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي
AU2014267235B2 (en) 2013-05-17 2017-10-05 Janssen Sciences Ireland Uc Sulphamoylthiophenamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
CN105452246A (zh) * 2013-06-06 2016-03-30 葛兰素史密斯克莱知识产权(第2号)有限公司 Zeste增强子同源物2的抑制剂
WO2015004618A1 (fr) * 2013-07-10 2015-01-15 Glaxosmithkline Intellectual Property (No.2) Limited Inhibiteurs de l'amplificateur de l'homologue 2 de zeste
JP6348978B2 (ja) 2013-07-25 2018-06-27 ヤンセン・サイエンシズ・アイルランド・ユーシー グリオキサミド置換ピロールアミド誘導体およびb型肝炎を処置するための医薬品としてのその使用
US9969716B2 (en) 2013-08-15 2018-05-15 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
HUE063984T2 (hu) 2013-10-16 2024-02-28 Epizyme Inc Hidroklorid só forma az EZH2 gátlásához
ES2655518T3 (es) 2013-10-23 2018-02-20 Janssen Sciences Ireland Uc Derivados de carboxamida y su uso como medicamentos para el tratamiento de la hepatitis B
WO2015077194A1 (fr) * 2013-11-22 2015-05-28 Bristol-Myers Squibb Company Inhibiteurs de la lysine méthyltransférase
US9169212B2 (en) 2014-01-16 2015-10-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
US10392349B2 (en) 2014-01-16 2019-08-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
KR20160128305A (ko) 2014-02-05 2016-11-07 노비라 테라퓨틱스, 인코포레이티드 Hbv 감염의 치료를 위한 병용 요법
CN110483484A (zh) 2014-02-06 2019-11-22 爱尔兰詹森科学公司 氨磺酰基吡咯酰胺衍生物及其作为药物用于治疗乙型肝炎的用途
US20160340674A1 (en) * 2014-02-10 2016-11-24 University Of Rochester Compositions and Methods to Inhibit EZH2 for the Treatment of Cardiovascular Diseases
EP3111222A1 (fr) 2014-02-26 2017-01-04 Glaxosmithkline Intellectual Property (No. 2) Limited Méthodes de traitement de patients atteints de cancer réagissant à l'inhibiteur d'ezh2 gsk126
US20170105997A1 (en) * 2014-03-21 2017-04-20 Northwestern University Methods of treating cancer
CN105037360B (zh) * 2014-04-28 2016-08-17 四川大学 吡啶酮衍生物及其制备方法和用途
CN105017221B (zh) * 2014-04-30 2019-05-28 中国医学科学院药物研究所 苯并咪唑衍生物及其制法和药物组合物与用途
PL3157915T3 (pl) 2014-06-17 2019-07-31 Pfizer Inc. Podstawione związki dihydroizochinolinonowe
US20170217941A1 (en) * 2014-06-25 2017-08-03 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
KR20170068603A (ko) * 2014-10-28 2017-06-19 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 제스트 인핸서 상동체 2 억제제
BR112017009671A2 (pt) 2014-11-06 2017-12-26 Dana Farber Cancer Inst Inc inibidores de ezh2 e usos destes
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ezh2抑制劑
WO2016102493A1 (fr) * 2014-12-22 2016-06-30 Bayer Pharma Aktiengesellschaft Inhibiteurs d'ezh2 de type imidazopyridine
WO2016101956A2 (fr) 2014-12-23 2016-06-30 University Of Copenhagen Traitement du cancer par inhibition de l'activité de l'ezh2
SI3237418T1 (sl) * 2014-12-23 2019-06-28 Novartis Ag Spojine triazolopirimidina in njihove uporabe
US9884831B2 (en) 2015-03-19 2018-02-06 Novira Therapeutics, Inc. Azocane and azonane derivatives and methods of treating hepatitis B infections
US10961532B2 (en) 2015-04-07 2021-03-30 The General Hospital Corporation Methods for reactivating genes on the inactive X chromosome
WO2016201328A1 (fr) * 2015-06-10 2016-12-15 Epizyme, Inc. Inhibiteurs d'ezh2 pour traiter le lymphome
US10875876B2 (en) 2015-07-02 2020-12-29 Janssen Sciences Ireland Uc Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
WO2017035234A1 (fr) 2015-08-24 2017-03-02 Epizyme, Inc. Méthode de traitement du cancer
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ezh2抑制劑
WO2017040190A1 (fr) 2015-08-28 2017-03-09 Constellation Pharmaceuticals, Inc. Formes cristallines de (r)-n-((4-méthoxy-6-méthyl-2-oxo-1,2-dihydropyridin-3-yl)méthyl)-2-méthyl-1-(1-(1-(2,2,2-trifluoroéthyl)pipéridin-4-yl)éthyl)-1h-indole-3-carboxamide
EP3356328A1 (fr) 2015-09-29 2018-08-08 Novira Therapeutics, Inc. Formes cristallines d'un agent antiviral de l'hépatite b
CN108699046A (zh) 2015-10-06 2018-10-23 Epizyme股份有限公司 用ezh2抑制剂治疗成神经管细胞瘤的方法
WO2017079738A1 (fr) 2015-11-05 2017-05-11 Epizyme, Inc. Cytométrie de flux permettant de surveiller l'état de la méthylation d'une histone h3
BR112018007876B1 (pt) * 2015-11-19 2023-10-17 Shanghai Hengrui Pharmaceutical Co., Ltd. Derivado de benzofurano, seus usos e seu processo de preparação, e composição farmacêutica
AU2017211331A1 (en) 2016-01-29 2018-06-07 Epizyme, Inc. Combination therapy for treating cancer
AU2017217688B2 (en) 2016-02-10 2023-01-19 Wake Forest University Health Sciences Model system of liver fibrosis and method of making and using the same
IL261721B (en) 2016-03-15 2022-07-01 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
KR20180129943A (ko) 2016-04-15 2018-12-05 노비라 테라퓨틱스, 인코포레이티드 캡시드 조립 억제제를 포함하는 배합물 및 방법
EP3445365A4 (fr) 2016-04-22 2019-10-16 Dana-Farber Cancer Institute, Inc. Inhibiteurs d'ezh2 et leurs utilisations
CN105777718B (zh) * 2016-04-27 2019-03-19 上海应用技术学院 潜在ezh2小分子抑制剂及其合成方法
US10987353B2 (en) 2016-05-04 2021-04-27 The Wistar Institute Of Anatomy And Biology Methods of treating cancers overexpressing CARM1 with EZH2 inhibitors and platinum-based antineoplastic drugs
EP3471830A4 (fr) 2016-06-17 2020-02-26 Epizyme Inc Inhibiteurs d'ezh2 pour traiter le cancer
EP3472161B1 (fr) * 2016-06-20 2020-03-25 Novartis AG Composés de triazolopyridine et leurs utilisations
CN107573327B (zh) * 2016-07-05 2020-03-31 四川大学 吲唑-甲酰胺-吡啶酮衍生物及其制备方法和用途
CN107573336B (zh) * 2016-07-05 2021-01-19 四川大学 苯并杂环-甲酰胺-吡啶酮衍生物及其制备方法和用途
WO2018075598A1 (fr) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthèse d'inhibiteurs d'ezh2
US20200262813A1 (en) * 2016-11-11 2020-08-20 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. 1,5,7-trisubstituted isoquinoline derivatives, preparation thereof, and use thereof in medicines
US10793549B2 (en) 2016-11-11 2020-10-06 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. Sulfuryl-substituted benzoheterocyclic derivative, preparation method and medical use thereof
US20200078362A1 (en) 2016-12-02 2020-03-12 Epizyme, Inc. Combination therapy for treating cancer
JP7125353B2 (ja) * 2017-01-19 2022-08-24 第一三共株式会社 Htlv-1関連脊髄症を治療することに用いるための医薬組成物
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
WO2018183885A1 (fr) 2017-03-31 2018-10-04 Epizyme, Inc. Multithérapie pour le traitement du cancer
WO2018231973A1 (fr) 2017-06-13 2018-12-20 Epizyme, Inc. Inhibiteurs de ezh2 et leurs méthodes d'utilisation
KR20200088386A (ko) 2017-11-14 2020-07-22 화이자 인코포레이티드 Ezh2 억제제 병용 요법
DK4043466T3 (da) 2018-01-31 2024-09-30 Mirati Therapeutics Inc PRC2-inhibitorer
CN110229151B (zh) * 2018-03-06 2021-09-10 上海海和药物研究开发股份有限公司 吲嗪类化合物、其制备方法及用途
CA3090125A1 (fr) 2018-03-14 2019-09-19 Janssen Sciences Ireland Unlimited Company Schema posologique de modulateur d'assemblage de capside
WO2020011607A1 (fr) 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition de sous-unités de prc2 permettant de traiter des troubles oculaires
WO2020020374A1 (fr) 2018-07-27 2020-01-30 苏州信诺维医药科技有限公司 Composé de benzène polysubstitué et son procédé de préparation et son utilisation
CN113454077A (zh) 2019-02-22 2021-09-28 爱尔兰詹森科学公司 用于治疗hbv感染或hbv诱发的疾病的酰胺衍生物
CN113773304B (zh) * 2019-02-25 2023-03-10 江苏豪森药业集团有限公司 抗耐药抗肿瘤egfr抑制剂的制备方法
BR112021021454A2 (pt) 2019-05-06 2021-12-21 Janssen Sciences Ireland Unlimited Co Derivados de amida úteis no tratamento da infecção por hbv ou doenças induzidas por hbv
JP2022545467A (ja) 2019-08-22 2022-10-27 ジュノー セラピューティクス インコーポレイテッド T細胞療法とzesteホモログ2エンハンサー(EZH2)阻害剤との併用療法および関連方法
US12006232B2 (en) 2020-06-09 2024-06-11 Rapid Water Technology LLC Water processing apparatus
CN113307765A (zh) * 2021-05-24 2021-08-27 上海泰坦科技股份有限公司 吡啶甲胺类化合物及其制备方法
WO2023025856A1 (fr) 2021-08-25 2023-03-02 INSERM (Institut National de la Santé et de la Recherche Médicale) Utilisation d'inhibiteurs d'ezh2 pour le traitement de la sténose aortique
WO2023111810A1 (fr) 2021-12-14 2023-06-22 Pfizer Inc. Polythérapies et leurs utilisations pour le traitement du cancer
AU2023262308A1 (en) 2022-04-27 2024-10-03 Astrazeneca Uk Limited Combination of antibody-drug conjugate with ezh1 and/or ezh2 inhibitor

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2584713B1 (fr) * 1985-07-11 1988-09-09 Roussel Uclaf Nouveaux derives de l'indole carboxamide, leurs sels, procede et intermediaires de preparation, application a titre de medicaments et compositions les renfermant
DE10022925A1 (de) * 2000-05-11 2001-11-15 Basf Ag Substituierte Indole als PARP-Inhibitoren
JP4869068B2 (ja) * 2003-06-19 2012-02-01 スミスクライン ビーチャム コーポレーション 化合物
PE20060748A1 (es) 2004-09-21 2006-10-01 Smithkline Beecham Corp Derivados de indolcarboxamida como inhibidores de quinasa ikk2
ES2400293T3 (es) * 2007-02-26 2013-04-08 Merck Canada Inc. Derivados de indol e indolina ciclopropilamida como antagonistas de receptores EP4
PE20081889A1 (es) 2007-03-23 2009-03-05 Smithkline Beecham Corp Indol carboxamidas como inhibidores de ikk2
US20090012031A1 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan EZH2 Cancer Markers
AR070398A1 (es) * 2008-02-22 2010-03-31 Gruenenthal Chemie Derivados sustituidos de indol
EP2331543A4 (fr) 2008-09-26 2013-06-19 Agency Science Tech & Res Dérivés 3-désazanéplanocine
WO2012005805A1 (fr) * 2010-05-07 2012-01-12 Glaxosmithkline Llc Aza-indazoles
ES2534804T3 (es) * 2010-05-07 2015-04-28 Glaxosmithkline Llc Indazoles
WO2012118812A2 (fr) 2011-02-28 2012-09-07 Epizyme, Inc. Composés hétéroaryles bicycliques substitués condensés en 6,5

Also Published As

Publication number Publication date
LT2566327T (lt) 2017-05-25
MX2012012966A (es) 2013-01-22
CN102970869B (zh) 2014-07-16
HUE034787T2 (en) 2018-02-28
US20150313887A1 (en) 2015-11-05
US9402836B2 (en) 2016-08-02
PT2566327T (pt) 2017-05-26
EP3246027A1 (fr) 2017-11-22
PL2566327T3 (pl) 2017-09-29
US9649307B2 (en) 2017-05-16
JP5864545B2 (ja) 2016-02-17
SI2566327T1 (sl) 2017-07-31
US8536179B2 (en) 2013-09-17
IL222878A (en) 2016-11-30
ME02757B (fr) 2018-01-20
DOP2012000282A (es) 2013-02-28
AU2011248068B2 (en) 2014-09-11
UA110112C2 (uk) 2015-11-25
US20150141436A1 (en) 2015-05-21
CR20120565A (es) 2013-02-20
SG185431A1 (en) 2012-12-28
AU2011248068A1 (en) 2012-12-20
RS55874B1 (sr) 2017-08-31
CL2012003110A1 (es) 2013-03-08
US8975291B2 (en) 2015-03-10
EP2566327A1 (fr) 2013-03-13
BR112012028556A2 (pt) 2014-04-01
CA2798622C (fr) 2016-11-15
KR20130062290A (ko) 2013-06-12
MY184101A (en) 2021-03-18
IL222878A0 (en) 2012-12-31
EA023788B1 (ru) 2016-07-29
US20130345200A1 (en) 2013-12-26
ZA201208447B (en) 2013-07-31
EP2566327A4 (fr) 2013-12-11
PE20130647A1 (es) 2013-06-26
ES2627085T3 (es) 2017-07-26
CA2798622A1 (fr) 2011-11-10
HRP20170736T1 (hr) 2017-07-28
US9114141B2 (en) 2015-08-25
US20130053397A1 (en) 2013-02-28
EP2566327B1 (fr) 2017-03-29
US20160296518A1 (en) 2016-10-13
WO2011140324A1 (fr) 2011-11-10
CY1119006T1 (el) 2018-01-10
DK2566327T3 (en) 2017-05-08
EA201291194A1 (ru) 2013-04-30
CN102970869A (zh) 2013-03-13
JP2013525498A (ja) 2013-06-20
NZ603454A (en) 2014-06-27

Similar Documents

Publication Publication Date Title
MA34284B1 (fr) Indoles
EA201270149A1 (ru) Ингибиторы bace
EA201270257A1 (ru) Производные n1-сульфонил-5-фторпиримидинона
EA201171367A1 (ru) Винилиндазолильные соединения
EA201490132A1 (ru) Противовирусные соединения
MA39172A1 (fr) Dérivés bicycliques hétérocycliques comme inhibiteurs de bromodomaines
EA201691327A1 (ru) Полиморфные формы (s)-2-(1-(9h-пурин-6-иламино)пропил)-5-фтор-3-фенилхиназолин-4(3h)-она
EA201200999A1 (ru) Способы лечения рака молочной железы
EA201890333A1 (ru) Противовирусные соединения
EA201590171A1 (ru) ИММУНОКОНЪЮГАТЫ, СОДЕРЖАЩИЕ АНТИТЕЛА К CD79b
EA201490853A1 (ru) Противовирусные соединения
EA200971068A1 (ru) Триазолиламинопиримидиновые соединения
EA201201000A1 (ru) Способы лечения колоректального рака
JO2788B1 (en) Amido phenoxyendazole compounds beneficial as C-MET inhibitors
EA201070256A1 (ru) Способ и промежуточные соединения для получения ингибиторов интегразы
EA201200323A1 (ru) Соединения и композиции, как ингибиторы протеинкиназы
EA201490474A1 (ru) Аминохиназолины в качестве ингибиторов киназ
EA201170288A1 (ru) Оксабициклогептаны и оксабициклогептены, их получение и применение
EA201101241A1 (ru) Лечение лейкозов и хронических миелопролиферативных болезней антителами к ерна3
EA201290642A1 (ru) Соединения и способы
EA201170831A1 (ru) Аминопиразольное соединение
EA201170699A1 (ru) Тетразамещенные пиридазины в качестве антагонистов пути hedgehog
EA201270256A1 (ru) Производные т1-замещенного 5-фтор-2-оксопиримидинон-1 (2h) -карбоксамида
EA201270253A1 (ru) Производные n1-ацил-5-фторпиримидинона
EA201290744A1 (ru) Имидазо[1,2-b][1,2,4]триазины в качестве c-met ингибиторов