WO2018057808A8 - Benzimidazole derivatives and their use as phosphatidylinositol 3-kinase inhibitors - Google Patents

Benzimidazole derivatives and their use as phosphatidylinositol 3-kinase inhibitors Download PDF

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Publication number
WO2018057808A8
WO2018057808A8 PCT/US2017/052817 US2017052817W WO2018057808A8 WO 2018057808 A8 WO2018057808 A8 WO 2018057808A8 US 2017052817 W US2017052817 W US 2017052817W WO 2018057808 A8 WO2018057808 A8 WO 2018057808A8
Authority
WO
WIPO (PCT)
Prior art keywords
phosphatidylinositol
kinase inhibitors
benzimidazole derivatives
compounds
formula
Prior art date
Application number
PCT/US2017/052817
Other languages
French (fr)
Other versions
WO2018057808A1 (en
Inventor
Jayaraman Chandrasekhar
Julian Andrew CODELLI
Devan Naduthambi
Leena Patel
Stephane Perreault
Gary Phillips
Kassandra F. SEDILLO
Jennifer Anne TREIBERG
Joshua Van Veldhuizen
William J. Watkins
Original Assignee
Gilead Sciences, Inc.
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 Gilead Sciences, Inc. filed Critical Gilead Sciences, Inc.
Publication of WO2018057808A1 publication Critical patent/WO2018057808A1/en
Publication of WO2018057808A8 publication Critical patent/WO2018057808A8/en

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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

Abstract

The present application provides the compounds of formula I or IA or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein s, t, m, n, R1, R2, R3, R4, R5, R6 and R7are as described herein. The compounds of formula I or IA selectively inhibit the activities of PI3K isoforms and are therefore useful in therapeutic treatments, in particular in the treatment of cancer and inflammatory conditions.
PCT/US2017/052817 2016-09-23 2017-09-21 Benzimidazole derivatives and their use as phosphatidylinositol 3-kinase inhibitors WO2018057808A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662398744P 2016-09-23 2016-09-23
US62/398,744 2016-09-23

Publications (2)

Publication Number Publication Date
WO2018057808A1 WO2018057808A1 (en) 2018-03-29
WO2018057808A8 true WO2018057808A8 (en) 2018-06-14

Family

ID=61690017

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2017/052817 WO2018057808A1 (en) 2016-09-23 2017-09-21 Benzimidazole derivatives and their use as phosphatidylinositol 3-kinase inhibitors

Country Status (1)

Country Link
WO (1) WO2018057808A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201825465A (en) * 2016-09-23 2018-07-16 美商基利科學股份有限公司 Phosphatidylinositol 3-kinase inhibitors

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US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5059714A (en) 1988-02-25 1991-10-22 Merrell Dow Pharmaceuticals Inc. Inhibitors of lysyl oxidase
US5021456A (en) 1988-02-25 1991-06-04 Merrell Dow Pharmaceuticals Inc. Inhibitors of lysyl oxidase
US4943593A (en) 1988-02-25 1990-07-24 Merrell Dow Pharmaceuticals Inc. Inhibitors of lysyl oxidase
US4965288A (en) 1988-02-25 1990-10-23 Merrell Dow Pharmaceuticals Inc. Inhibitors of lysyl oxidase
US5252608A (en) 1988-02-25 1993-10-12 Merrell Dow Pharmaceuticals Inc. Inhibitors of lysyl oxidase
US5182297A (en) 1988-02-25 1993-01-26 Merrell Dow Pharmaceuticals Inc. Inhibitors of lysyl oxidase
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
US5120764A (en) 1988-11-01 1992-06-09 Merrell Dow Pharmaceuticals Inc. Inhibitors of lysyl oxidase
US4997854A (en) 1989-08-25 1991-03-05 Trustees Of Boston University Anti-fibrotic agents and methods for inhibiting the activity of lysyl oxidase in-situ using adjacently positioned diamine analogue substrates
UA75055C2 (en) * 1999-11-30 2006-03-15 Пфайзер Продактс Інк. Benzoimidazole derivatives being used as antiproliferative agent, pharmaceutical composition based thereon
SI2223922T1 (en) 2000-04-25 2016-04-29 Icos Corporation Inhibitors of human phosphatidyl-inositol 3-kinase delta
FR2828206B1 (en) 2001-08-03 2004-09-24 Centre Nat Rech Scient USE OF LYSYL OXIDASE INHIBITORS FOR CELL CULTURE AND TISSUE ENGINEERING
BRPI0808888B8 (en) 2007-03-12 2021-05-25 Cytopia Res Pty Ltd phenyl amino pyrimidine compound for use in the treatment of a kinase-associated disease, process for preparing the compound, pharmaceutical composition, and implant
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
US8399460B2 (en) 2009-10-27 2013-03-19 Astrazeneca Ab Chromenone derivatives
MX2012013622A (en) 2010-05-31 2013-02-01 Ono Pharmaceutical Co Purinone derivative.
ES2714384T3 (en) 2010-10-06 2019-05-28 Glaxosmithkline Llc Benzimidazole derivatives as PI3 kinase inhibitors
LT2658844T (en) 2010-12-28 2017-02-10 Sanofi Novel pyrimidine derivatives, preparation thereof, and pharmaceutical use thereof as akt(pkb) phosphorylation inhibitors

Also Published As

Publication number Publication date
WO2018057808A1 (en) 2018-03-29

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