[go: up one dir, main page]

MA33614B1 - Composés de benzoxépine inhibiteurs de pi3k et leurs procédés d'utilisation - Google Patents

Composés de benzoxépine inhibiteurs de pi3k et leurs procédés d'utilisation

Info

Publication number
MA33614B1
MA33614B1 MA34727A MA34727A MA33614B1 MA 33614 B1 MA33614 B1 MA 33614B1 MA 34727 A MA34727 A MA 34727A MA 34727 A MA34727 A MA 34727A MA 33614 B1 MA33614 B1 MA 33614B1
Authority
MA
Morocco
Prior art keywords
methods
formula
benzoxin
combinations
pi3k inhibitors
Prior art date
Application number
MA34727A
Other languages
Arabic (ar)
English (en)
Inventor
Nicole Blaquiere
Steven Do
Danette Dudley
Adrian J Folkes
Richard A Goldsmith
Robert Heald
Tim Heffron
Aleksandr Kolesnikov
Chudi Ndubaku
Alan G Olivero
Stephen Price
Steven Staben
Binqing Wei
Original Assignee
Hoffmann La Roche
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=43125543&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA33614(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MA33614B1 publication Critical patent/MA33614B1/fr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed 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
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/41Heterocyclic 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
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4365Heterocyclic 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 having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/496Non-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
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines 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
    • A61K31/495Heterocyclic 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
    • A61K31/54Heterocyclic 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/14Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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

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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Biochemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

L'INVENTION PORTE SUR DES COMPOSÉS DE BENZOXÉPINE DE FORMULE I, Y COMPRIS LES STÉRÉOISOMÈRES, ISOMÈRES GÉOMÉTRIQUES, TAUTOMÈRES, SOLVATES, MÉTABOLITES ET SELS PHARMACEUTIQUEMENT ACCEPTABLES DE CEUX-CI, DANS LAQUELLE FORMULE : Z1 REPRÉSENTE CR1 OU N; Z2 REPRÉSENTE CR2 OU N; Z3 REPRÉSENTE CR3 OU N; Z4 REPRÉSENTE CR4 OU N; ET DANS LAQUELLE (I) X1 REPRÉSENTE N ET X2 REPRÉSENTE S, (II) X1 REPRÉSENTE S ET X2 REPRÉSENTE N, (III) X1 REPRÉSENTE CR7 ET X2 REPRÉSENTE S, (IV) X1 REPRÉSENTE S ET X2 REPRÉSENTE CR7; (V) X1 REPRÉSENTE NR8 ET X2 REPRÉSENTE N, (VI) X1 REPRÉSENTE N ET X2 REPRÉSENTE NR8, (VII) X1 REPRÉSENTE CR7 ET X2 REPRÉSENTE O, (VIII) X1 REPRÉSENTE O ET X2 REPRÉSENTE CR7, (IX) X1 REPRÉSENTE CR7 ET X2 REPRÉSENTE C(R7)2, (X) X1 REPRÉSENTE C(R7)2 ET X2 REPRÉSENTE CR7; (XI) X1 REPRÉSENTE N ET X2 REPRÉSENTE O OU (XII) X1 REPRÉSENTE O ET X2 REPRÉSENTE N, LESQUELS SONT UTILES POUR L'INHIBITION DE LIPIDE-KINASES, DONT LA P110-ALPHA ET D'AUTRES ISOFORMES DE PI3K, ET POUR LE TRAITEMENT DE TROUBLES TELS QU'UN CANCER À MÉDIATION PAR DES LIPIDE-KINASES. L'INVENTION PORTE ÉGALEMENT SUR DES PROCÉDÉS D'UTILISATION DE COMPOSÉS DE FORMULE I POUR LE DIAGNOSTIC IN VITRO, IN SITU ET IN VIVO, LA PRÉVENTION OU LE TRAITEMENT DE TELS TROUBLES DANS DES CELLULES DE MAMMIFÈRE, OU D'ÉTATS PATHOLOGIQUES ASSOCIÉS.
MA34727A 2009-09-28 2012-03-28 Composés de benzoxépine inhibiteurs de pi3k et leurs procédés d'utilisation MA33614B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24638609P 2009-09-28 2009-09-28
PCT/EP2010/064222 WO2011036284A1 (fr) 2009-09-28 2010-09-27 Composés de benzoxépine inhibiteurs de pi3k et leurs procédés d'utilisation

Publications (1)

Publication Number Publication Date
MA33614B1 true MA33614B1 (fr) 2012-09-01

Family

ID=43125543

Family Applications (1)

Application Number Title Priority Date Filing Date
MA34727A MA33614B1 (fr) 2009-09-28 2012-03-28 Composés de benzoxépine inhibiteurs de pi3k et leurs procédés d'utilisation

Country Status (25)

Country Link
US (4) US8263633B2 (fr)
EP (2) EP2483277B1 (fr)
JP (2) JP5546636B2 (fr)
KR (2) KR20140034948A (fr)
CN (2) CN104987345A (fr)
AU (1) AU2010299820A1 (fr)
BR (1) BR112012006802A2 (fr)
CA (1) CA2774807C (fr)
CL (1) CL2012000755A1 (fr)
CO (1) CO6620072A2 (fr)
CR (1) CR20120130A (fr)
EC (1) ECSP12011752A (fr)
ES (1) ES2558742T3 (fr)
HK (1) HK1216529A1 (fr)
IL (1) IL218800A0 (fr)
MA (1) MA33614B1 (fr)
MX (1) MX2012003641A (fr)
NZ (1) NZ599090A (fr)
PE (2) PE20121559A1 (fr)
PH (1) PH12012500608A1 (fr)
RU (2) RU2557658C2 (fr)
SG (1) SG10201407781SA (fr)
UA (1) UA108863C2 (fr)
WO (1) WO2011036284A1 (fr)
ZA (1) ZA201404552B (fr)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2483278T1 (sl) * 2009-09-28 2014-03-31 F. Hoffmann-La Roche Ag Inhibitorske spojine benzoksazepina pi3k in njihova uporaba pri zdravljenju raka
SG10201407781SA (en) * 2009-09-28 2015-01-29 Hoffmann La Roche Benzoxepin PI3K Inhibitor Compounds And Methods Of Use
WO2012126901A1 (fr) 2011-03-21 2012-09-27 F. Hoffmann-La Roche Ag Composés de benzoxazépine sélectifs pour pi3k p110 delta et leurs méthodes d'utilisation
WO2013030750A1 (fr) 2011-09-01 2013-03-07 Lupin Limited Composés antiviraux
BR112014019209A2 (pt) 2012-02-17 2017-07-04 Hoffmann La Roche compostos tricíclicos e métodos de uso para os mesmos
JP5829556B2 (ja) * 2012-03-15 2015-12-09 日本特殊陶業株式会社 微粒子検知システム
CN104350144B (zh) 2012-05-23 2017-08-04 弗·哈夫曼-拉罗切有限公司 获得和使用内胚层和肝细胞的组合物和方法
MX2014014831A (es) 2012-06-08 2015-02-12 Hoffmann La Roche Selectividad de mutante y combinaciones de un compuesto inhibidor de fosfoinositida 3 cinasa y agentes quimioterapeuticos para el tratamiento de cancer.
KR102281288B1 (ko) 2012-09-26 2021-07-26 에프. 호프만-라 로슈 아게 환형 에터 피라졸-4-일-헤테로사이클릴-카복사마이드 화합물 및 이의 사용 방법
EP2970329A1 (fr) 2013-03-13 2016-01-20 F. Hoffmann-La Roche AG Procédé de fabrication de composés benzoazépines
MX364895B (es) 2013-03-13 2019-05-10 Forma Therapeutics Inc Nuevos compuestos y composiciones para la inhibicion de fasn.
CN103274963B (zh) * 2013-06-28 2015-12-23 江苏倍达医药科技有限公司 一种合成1,1,1-三氟异丙基肼盐酸盐的方法
EP3125920B1 (fr) 2014-04-04 2020-12-23 Del Mar Pharmaceuticals Dianhydrogalactitol, diacetyldianhydrogalactitol ou dibromodulcitol dans le traitement du carcinome non à petites cellules des poumons et du cancer des ovaires
NO2714752T3 (fr) * 2014-05-08 2018-04-21
AU2016215432B2 (en) 2015-02-02 2020-07-30 Valo Early Discovery, Inc. 3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors
WO2016126726A1 (fr) 2015-02-02 2016-08-11 Forma Therapeutics, Inc. Acides hydroxamiques bicycliques [4,6,0] en tant qu'inhibiteurs hdac6
RU2571094C1 (ru) * 2015-02-11 2015-12-20 Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Омский государственный университет им. Ф.М. Достоевского" СПОСОБ ПОЛУЧЕНИЯ 4-АЛКОКСИ-4Н-ТИЕНО[3,2-с]ХРОМЕН-2-КАРБАЛЬДЕГИДОВ, ОБЛАДАЮЩИХ ПРОТИВОЯЗВЕННОЙ АКТИВНОСТЬЮ
EP3266455B1 (fr) 2015-03-06 2020-12-30 Korea Advanced Institute of Science and Technology Composition pour la prévention ou le traitement de l'épilepsie réfractaire comprenant un inhibiteur mtor
CN111848643A (zh) * 2015-07-02 2020-10-30 豪夫迈·罗氏有限公司 苯并氧氮杂*噁唑烷酮化合物及其使用方法
EP4585597A1 (fr) * 2015-07-02 2025-07-16 F. Hoffmann-La Roche AG Composés de benzoxazepine oxazolidinone et procédés d'utilisation
WO2017042182A1 (fr) * 2015-09-08 2017-03-16 F. Hoffmann-La Roche Ag Composés tricycliques inhibiteurs de pi3k et procédés d'utilisation
HRP20210581T1 (hr) 2015-09-09 2021-05-28 Jubilant Biosys Limited Triciklički kondenzirani derivati piridin-2-ona i njihova upotreba kao inhibitora brd4
US10241701B2 (en) * 2015-09-16 2019-03-26 Samsung Electronics Co., Ltd. Solid state memory system with power management mechanism and method of operation thereof
GB201516504D0 (en) 2015-09-17 2015-11-04 Astrazeneca Ab Imadazo(4,5-c)quinolin-2-one Compounds and their use in treating cancer
US10555935B2 (en) 2016-06-17 2020-02-11 Forma Therapeutics, Inc. 2-spiro-5- and 6-hydroxamic acid indanes as HDAC inhibitors
CN106317050B (zh) * 2016-08-24 2018-11-23 烟台大学 一种苯基噻唑衍生物及其制备方法与应用
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
EP3873214A4 (fr) 2018-10-29 2022-07-13 Forma Therapeutics, Inc. Formes solides de (4-(2-fluoro-4-(1-méthyl-1h-benzo[d]imidazol-5-yl)benzoyl)pipérazin-1-yl)(1-hydroxycyclopropyl)méthanone
CA3178415A1 (fr) * 2020-05-11 2021-11-18 Mark R. Bray Formes salines et cristallines de 4-amino-5-(6-(4-methylpiperazin-1-yl)-1h-benzo[d]imidazol-2-yl)thieno[2,3-b]pyridin-6(7h)-one

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
GB8504702D0 (en) * 1985-02-23 1985-03-27 Zyma Sa Tricyclic compounds
US5583024A (en) 1985-12-02 1996-12-10 The Regents Of The University Of California Recombinant expression of Coleoptera luciferase
FR2677356B1 (fr) * 1991-06-05 1995-03-17 Sanofi Sa Derives heterocycliques d'acylamino-2 thiazoles-5 substitues, leur preparation et compositions pharmaceutiques en contenant.
US6274327B1 (en) 1992-04-13 2001-08-14 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
GB9208135D0 (en) 1992-04-13 1992-05-27 Ludwig Inst Cancer Res Polypeptides having kinase activity,their preparation and use
US5846824A (en) 1994-02-07 1998-12-08 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
DK0638071T3 (da) * 1992-12-28 1997-10-27 Eisai Co Ltd Heterocykliske carboxylsyrederivater, der bindes til retenoidreceptorer (RAR)
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
JPH08176070A (ja) 1994-12-19 1996-07-09 Mitsubishi Chem Corp ジデプシド誘導体及びpi3キナーゼ阻害剤
JPH08175990A (ja) 1994-12-19 1996-07-09 Mitsubishi Chem Corp Pi3キナーゼ阻害剤とその製造法
JPH08336393A (ja) 1995-04-13 1996-12-24 Mitsubishi Chem Corp 光学活性なγ−置換−β−ヒドロキシ酪酸エステルの製造法
GB9521987D0 (en) 1995-10-26 1996-01-03 Ludwig Inst Cancer Res Phosphoinositide 3-kinase modulators
WO1997019087A1 (fr) * 1995-11-17 1997-05-29 E.I. Du Pont De Nemours And Company Heterocycles herbicides tricycliques
US6602677B1 (en) 1997-09-19 2003-08-05 Promega Corporation Thermostable luciferases and methods of production
DE19908535A1 (de) * 1999-02-26 2000-08-31 Aventis Pharma Gmbh Verwendung von polycyclischen Thiazol-Systemen zur Herstellung von Medikamenten zur Prophylaxe oder Behandlung von Obesitas
DE19908533A1 (de) * 1999-02-26 2000-08-31 Aventis Pharma Gmbh Polycyclische Thiazol-Systeme, Verfahren zu ihrer Herstellung und Arzneimittel enthaltend diese Verbindungen
DE19908538A1 (de) * 1999-02-26 2000-08-31 Aventis Pharma Gmbh Polycyclische 2-Amino-Thiazol Systeme, Verfahren zu ihrer Herstellung und Arzneimittel enthaltend diese Verbindungen
DE19908537A1 (de) * 1999-02-26 2000-08-31 Aventis Pharma Gmbh Verwendung von polycyclischen 2-Amino-Thiazol Systemen zur Herstellung von Medikamenten zur Prophylaxe oder Behandlung von Obesitas
US7273880B2 (en) * 1999-06-30 2007-09-25 H. Lunbeck A/S Selective NPY (Y5) antagonists
ATE245636T1 (de) 1999-07-29 2003-08-15 Lilly Co Eli Benzofurylpiperazine: 5-ht2c serotoninrezeptor agonisten
WO2001064675A1 (fr) * 2000-03-03 2001-09-07 Novartis Ag Thiazolamines condensees et leur utilisation comme antagonistes du neuropeptide y5
JP2001247477A (ja) 2000-03-03 2001-09-11 Teikoku Hormone Mfg Co Ltd 抗腫瘍剤
US6608053B2 (en) 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
US6403588B1 (en) 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
EP1353693B1 (fr) 2001-01-16 2005-03-16 Glaxo Group Limited Combinaison pharmaceutique contenant de l'amino-4 quinazoline et paclitaxel, carboplatin or vinorelbine pour le traitement du cancer
WO2002098863A1 (fr) * 2001-06-05 2002-12-12 Fujisawa Pharmaceutical Co., Ltd. Derive d'imidazole fondu
WO2003018057A1 (fr) 2001-07-26 2003-03-06 Santen Pharmaceutical Co., Ltd. Remede contre le glaucome contenant en tant qu'ingredient actif un compose presentant un effet inhibiteur de la kinase pi3
US6703414B2 (en) 2001-09-14 2004-03-09 Arizona Board Of Regents On Behalf Of The University Of Arizona Device and method for treating restenosis
AU2002349912A1 (en) 2001-10-24 2003-05-06 Iconix Pharmaceuticals, Inc. Modulators of phosphoinositide 3-kinase
AU2002357667A1 (en) 2001-10-24 2003-05-06 Iconix Pharmaceuticals, Inc. Modulators of phosphoinositide 3-kinase
WO2003037886A2 (fr) 2001-10-30 2003-05-08 Pharmacia Corporation Derives de carboxamide heteroaromatique destines au traitement des inflammations
AU2003255529B2 (en) 2002-07-10 2008-11-20 Laboratoires Serono Sa Use of compounds for increasing spermatozoa motility
US20040092561A1 (en) 2002-11-07 2004-05-13 Thomas Ruckle Azolidinone-vinyl fused -benzene derivatives
EA011807B1 (ru) 2002-07-10 2009-06-30 Лаборатуар Сероно Са Азолидинонвинильные производные конденсированного бензола
US20040082602A1 (en) * 2002-07-19 2004-04-29 Hagen Timothy J. Substituted thiophene carboxamide compounds for the treatment of inflammation
WO2004017950A2 (fr) 2002-08-22 2004-03-04 Piramed Limited Inhibiteurs de phosphatidylinositol 3,5-biphosphate en tant qu'agents antiviraux
CA2514241A1 (fr) * 2003-02-07 2004-08-19 Warner-Lambert Company Llc Derives d'oxazolidinones n-substitues par un noyau tricyclique, destines a etre utilises en tant qu'agents antibacteriens
EP1449844A1 (fr) * 2003-02-14 2004-08-25 Ferring B.V. derives de benzamide agonistes de l'ocytocine et antagonistes de la vasopressine
US20050239767A1 (en) * 2003-10-28 2005-10-27 Chan Michael K Intermolecular SNAr of the heterocycle-activated nitro and fluoro groups-application in the synthesis of polyazamacrocyclic ligands
RU2403258C2 (ru) * 2004-10-07 2010-11-10 Бёрингер Ингельхайм Интернациональ Гмбх Тиазолилдигидроиндазолы
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
NZ567140A (en) 2005-10-07 2011-09-30 Exelixis Inc Azetidines as MEK inhibitors for the treatment of proliferative diseases
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
CL2007001166A1 (es) 2006-04-26 2008-01-25 Piramed Ltd Compuestos derivados de pirimidina condensada, inhibidores de pi3-quinasa; procesos para preparar los compuestos; composicion farmaceutica que los comprende; uso de los compuestos en la preparacion de medicamentos; proceso para preparar la composicion farmaceutica; y kit que incluye a la composicion farmaceutica
CL2007001165A1 (es) 2006-04-26 2008-01-25 Hoffmann La Roche 2-(1h-indazol-4-il)-6-(4-metanosulfonil-piperazin-1-ilmetil)-4-morfolin-4-il-tieno[3,2-d]pirimidina; procedimiento de preparacion; composicion farmaceutica; proceso de preparacion de dicha composicion; kit farmaceutico; y uso para tratar enfermedades tales como cancer, desordenes inmunes y enfermedades cardiovasculares.
AU2007281911B2 (en) 2006-08-04 2014-02-06 Beth Israel Deaconess Medical Center Inhibitors of pyruvate kinase and methods of treating disease
US7649007B2 (en) 2006-08-15 2010-01-19 Wyeth Llc Oxazolidine derivatives as PR modulators
US8779154B2 (en) * 2006-09-26 2014-07-15 Qinglin Che Fused ring compounds for inflammation and immune-related uses
AR064155A1 (es) 2006-12-07 2009-03-18 Piramed Ltd Compuestos de inhibidores de fosfoinositido-3 quinasa y metodos de uso
BRPI0717907A2 (pt) 2006-12-07 2013-11-05 Genentech Inc "composto, composição farmacêutica, métodos para tratar um câncer, para inbir ou modular a atividade da lipídeo quinase, processo para a produçãoo de uma composição farmacêutica, uso de um composto e kit"
EP2276767B1 (fr) * 2008-03-31 2014-05-07 Genentech, Inc. Composés inhibiteurs de pi3k du type benzopyrane et benzoxépine et leurs procédés d'utilisation
SG10201407781SA (en) * 2009-09-28 2015-01-29 Hoffmann La Roche Benzoxepin PI3K Inhibitor Compounds And Methods Of Use
SI2483278T1 (sl) * 2009-09-28 2014-03-31 F. Hoffmann-La Roche Ag Inhibitorske spojine benzoksazepina pi3k in njihova uporaba pri zdravljenju raka

Also Published As

Publication number Publication date
ZA201404552B (en) 2015-06-24
AU2010299820A1 (en) 2012-04-19
BR112012006802A2 (pt) 2020-08-18
US8263633B2 (en) 2012-09-11
JP2014139222A (ja) 2014-07-31
IL218800A0 (en) 2012-06-28
KR20120065430A (ko) 2012-06-20
CO6620072A2 (es) 2013-02-15
NZ599090A (en) 2014-02-28
CR20120130A (es) 2012-06-01
US20140135308A1 (en) 2014-05-15
ES2558742T3 (es) 2016-02-08
EP2483277A1 (fr) 2012-08-08
CA2774807A1 (fr) 2011-03-31
RU2012117394A (ru) 2013-11-10
PE20140918A1 (es) 2014-08-06
US20110076291A1 (en) 2011-03-31
CN102762574A (zh) 2012-10-31
US9175009B2 (en) 2015-11-03
JP5546636B2 (ja) 2014-07-09
WO2011036284A1 (fr) 2011-03-31
KR20140034948A (ko) 2014-03-20
PE20121559A1 (es) 2012-12-05
US20150094347A1 (en) 2015-04-02
CL2012000755A1 (es) 2012-09-07
UA108863C2 (ru) 2015-06-25
MX2012003641A (es) 2012-04-30
CA2774807C (fr) 2018-04-03
RU2557658C2 (ru) 2015-07-27
HK1175180A1 (zh) 2013-06-28
US8673952B2 (en) 2014-03-18
KR101449217B1 (ko) 2014-10-08
PH12012500608A1 (en) 2017-08-09
RU2015104301A (ru) 2015-11-10
CN104987345A (zh) 2015-10-21
US8952043B2 (en) 2015-02-10
EP2483277B1 (fr) 2015-12-02
EP2784078A1 (fr) 2014-10-01
CN102762574B (zh) 2015-12-02
ECSP12011752A (es) 2012-10-30
SG10201407781SA (en) 2015-01-29
US20130012488A1 (en) 2013-01-10
HK1216529A1 (zh) 2016-11-18
JP2013505920A (ja) 2013-02-21

Similar Documents

Publication Publication Date Title
MA33614B1 (fr) Composés de benzoxépine inhibiteurs de pi3k et leurs procédés d'utilisation
TW200801012A (en) Phosphoinositide 3-kinase inhibitor compounds and methods of use
MA34234B1 (fr) Composes pyrazol-4-yl-heterocyclyle-carboxamide et leurs procedes d'utilisation
PH12013501779A1 (en) Pyrrolopyridines as kinase inhibitors
MA32271B1 (fr) Composes inhibiteurs de kinases raf et procedes d'utilisation
TW200800996A (en) Heterobicyclic pyrazole compounds and methods of use
WO2007127175A3 (fr) Composés pharmaceutiques
MA31146B1 (fr) Composes inhibant la phosphoinositide 3 kinase et procedes d'utilisation
MX338504B (es) Combinaciones de compuestos inhibidores de fosfoinosituro 3-cinasa y agentes quimioterapeuticos, y metodos de uso.
MX2021012122A (es) Inhibidores de la proteina tirosina fosfatasa.
MX2021004410A (es) Inhibidores de la proteina tirosina fosfatasa.
SG178899A1 (en) Raf inhibitor compounds and methods of use thereof
MA32135B1 (fr) Inhibiteurs de pim kinase et leurs procedes d'utilisation
MX2009005925A (es) Compuestos inhibidores de fosfoinositida 3-quinasa y los metodos de uso.
SG178900A1 (en) Raf inhibitor compounds and methods of use thereof
MX2010010659A (es) Compuestos de benzopirano y benzoxepina, inhibidores de fosfoinoinositida 3-cinasas y metodos para utilizarlos.
MA33531B1 (fr) Composés de benzoxazépine inhibiteurs de pi3k et leurs procédés d'utilisation
MA40225A (fr) Composés dihydroisoquinolinone substitués
MA31419B1 (fr) Derives de pyridine
MA31178B1 (fr) Dérivés de 3-amino-pyrrolo[3,4-c]pyrazole-5-(1h,4h, 6h) carbaldéhyde servant d'inhibiteurs de pkc
MA33533B1 (fr) Compositions pharmaceutiques pour le traitement du cancer et d'autres maladies ou troubles
UA98946C2 (en) Phosphoinositide 3-kinase inhibitor compounds and methods of use
JP2011509982A (ja) 上皮起源からのガン転移を防ぎ又は処置する為のアミノペプチダーゼインヒビター又はアザインドール化合物の使用
MA34431B1 (fr) Composés de pyridone et d'aza-pyridone et leurs procédés d'utilisation
MA38206B1 (fr) Pyridyl-hydrazones pour le traitement de la tuberculose et de maladies associées