WO2012065057A3 - Phosphatidylinositol 3-kinase inhibitors and methods of their use - Google Patents

Phosphatidylinositol 3-kinase inhibitors and methods of their use Download PDF

Info

Publication number
WO2012065057A3
WO2012065057A3 PCT/US2011/060361 US2011060361W WO2012065057A3 WO 2012065057 A3 WO2012065057 A3 WO 2012065057A3 US 2011060361 W US2011060361 W US 2011060361W WO 2012065057 A3 WO2012065057 A3 WO 2012065057A3
Authority
WO
WIPO (PCT)
Prior art keywords
methods
phosphatidylinositol
kinase inhibitors
compound
formulations
Prior art date
Application number
PCT/US2011/060361
Other languages
French (fr)
Other versions
WO2012065057A2 (en
Inventor
Dana T. Aftab
Arthur Decillis
Original Assignee
Exelixis, 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 Exelixis, Inc. filed Critical Exelixis, Inc.
Publication of WO2012065057A2 publication Critical patent/WO2012065057A2/en
Publication of WO2012065057A3 publication Critical patent/WO2012065057A3/en

Links

Classifications

    • 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
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09B—ORGANIC DYES OR CLOSELY-RELATED COMPOUNDS FOR PRODUCING DYES, e.g. PIGMENTS; MORDANTS; LAKES
    • C09B57/00—Other synthetic dyes of known constitution
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

The invention relates to methods, combinations, and formulations of a compound of Formula I, particularly Compound A.
PCT/US2011/060361 2010-11-12 2011-11-11 Phosphatidylinositol 3-kinase inhibitors and methods of their use WO2012065057A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US41334510P 2010-11-12 2010-11-12
US61/413,345 2010-11-12

Publications (2)

Publication Number Publication Date
WO2012065057A2 WO2012065057A2 (en) 2012-05-18
WO2012065057A3 true WO2012065057A3 (en) 2012-11-22

Family

ID=45044732

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/060361 WO2012065057A2 (en) 2010-11-12 2011-11-11 Phosphatidylinositol 3-kinase inhibitors and methods of their use

Country Status (1)

Country Link
WO (1) WO2012065057A2 (en)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2755654A1 (en) * 2011-09-14 2014-07-23 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of cancer
CN107375289A (en) 2011-11-01 2017-11-24 埃克塞利希斯股份有限公司 For treating the compound as the kinase inhibitor of phosphatidylinositols 3 of lymphoproliferative malignant tumour
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
AR092501A1 (en) * 2012-09-13 2015-04-22 Sanofi Sa CRYSTAL COMPOUNDS
FR3008620A1 (en) * 2013-07-22 2015-01-23 Sanofi Sa COMPRESSOR FORMULATION OF A PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR
CA2925944C (en) 2013-10-04 2023-01-10 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
EP4066834A1 (en) 2014-03-19 2022-10-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN108349985A (en) 2015-09-14 2018-07-31 无限药品股份有限公司 Solid form, preparation method, the composition and its application method comprising it of isoquinolines
HUE054726T2 (en) 2016-03-02 2021-09-28 Eisai R&D Man Co Ltd Eribulin-based antibody-drug conjugates and methods of use
US10759806B2 (en) 2016-03-17 2020-09-01 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US20200223839A1 (en) * 2017-07-09 2020-07-16 Jiangsu Yingkebeita Yiyaokeji Co. Ltd Fluoro-containing compounds, use and preparation thereof
SG11202004019SA (en) 2017-11-17 2020-05-28 Cellix Bio Private Ltd Compositions and methods for the treatment of eye disorders
WO2021041749A1 (en) * 2019-08-27 2021-03-04 The Regents Of The University Of California Brown Adipose Tissue Myosin II Activators for Metabolic Therapy
CN115989030A (en) * 2020-05-29 2023-04-18 康涅狄格大学 Inhibitors of porcine reproductive and respiratory syndrome virus

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008021389A2 (en) * 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4107288A (en) 1974-09-18 1978-08-15 Pharmaceutical Society Of Victoria Injectable compositions, nanoparticles useful therein, and process of manufacturing same
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
JP5270353B2 (en) 2005-10-07 2013-08-21 エクセリクシス， インク． Phosphatidylinositol 3-kinase inhibitor and method of use thereof
WO2008127594A2 (en) 2007-04-11 2008-10-23 Exelixis, Inc. Combination therapies comprising quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008021389A2 (en) * 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
DATABASE BIOSIS, [Online] 20 November 2009 (2009-11-20), WALSH KATHERINE J ET AL: "PI3K Inhibitors Inhibit Lymphoma Growth by Downregulation of MYC-Dependent Proliferation", XP002666170, retrieved from BIOSIS Database accession no. PREV201000352691 *
FDA: "Summary of Color Additives for Use in the United States in Foods, Drugs, Cosmetics, and Medical Devices", 22 March 2007 (2007-03-22), XP002675594, Retrieved from the Internet <URL:http://www.fda.gov/ForIndustry/ColorAdditives/ColorAdditiveInventories/ucm115641.htm> [retrieved on 20120302] *
HAN L ET AL: "Inactivation of PI3K/AKT signaling inhibits glioma cell growth through modulation of beta-catenin-mediated transcription", BRAIN RESEARCH, ELSEVIER, AMSTERDAM, NL, vol. 1366, 1 October 2010 (2010-10-01), pages 9 - 17, XP027527870, ISSN: 0006-8993, [retrieved on 20101001] *
PIXU LIU ET AL: "Targeting the phosphoinositide 3-kinase pathway in cancer", NATURE REVIEWS DRUG DISCOVERY, vol. 8, no. 8, 1 August 2009 (2009-08-01), pages 627 - 644, XP055020926, ISSN: 1474-1776, DOI: 10.1038/nrd2926 *
T. W. MILLER ET AL: "Inhibition of Mammalian Target of Rapamycin Is Required for Optimal Antitumor Effect of HER2 Inhibitors against HER2-Overexpressing Cancer Cells", CLINICAL CANCER RESEARCH, vol. 15, no. 23, 1 December 2009 (2009-12-01), pages 7266 - 7276, XP055020913, ISSN: 1078-0432, DOI: 10.1158/1078-0432.CCR-09-1665 *
Y. WU ET AL: "FOXO1A Is a Target for HER2-Overexpressing Breast Tumors", CANCER RESEARCH, vol. 70, no. 13, 15 June 2010 (2010-06-15), pages 5475 - 5485, XP055020903, ISSN: 0008-5472, DOI: 10.1158/0008-5472.CAN-10-0176 *

Also Published As

Publication number Publication date
WO2012065057A2 (en) 2012-05-18

Similar Documents

Publication Publication Date Title
WO2012065057A3 (en) Phosphatidylinositol 3-kinase inhibitors and methods of their use
WO2012065019A3 (en) Combination comprising pyridopyrimidinone inhibitors of pi3k alpha
WO2011153157A3 (en) Benzoquinolone inhibitors of vmat2
IL222484A0 (en) Arginase inhibitor compounds, compositions comprising the same and uses thereof
PH12014501273A1 (en) Intranasal dexmedetomidine compositions and methods of use thereof
WO2013003298A3 (en) Inhibitors of pde10
UA108101C2 (en) N3-substituted N1-sulfonyl-5-fluoropyrimidinone derivatives
WO2012042371A3 (en) Pharmaceutical composition
WO2011077043A3 (en) Phenol derivatives and pharmaceutical or cosmetic use thereof
WO2012122011A3 (en) Amino-quinolines as kinase inhibitors
PL2563485T3 (en) Azeotropic compositions of e-1,1,1,4,4,4-hexafluoro-2-butene
WO2012122383A3 (en) Pi3 kinase inhibitors and uses thereof
EP2582664A4 (en) Phenylthioacetate compounds, compositions and methods of use
WO2012071509A3 (en) Benzoxazepines as inhibitors of p13k/mtor and methods of their use and manufacture
CA2873723A1 (en) Pyrrolopyrimidone and pyrrolopyridone inhibitors of tankyrase
WO2011143772A9 (en) Inhibitors of hiv replication
IL223865A0 (en) Calcium salts of dihydrooroorotate dehydrogenase inhibitors, compositions comprising the same and uses thereof
WO2010147830A3 (en) Aminothiazole modulators of beta-3-adrenoreceptor
WO2012037562A3 (en) Pharmaceutical and nutraceutical compositions of abscisic acid
WO2011143503A3 (en) Tetracycline compositions
WO2013055687A3 (en) R(+)-n-formyl-propargyl-aminoindan
EP2605648B8 (en) Herbicidal compositions
IT1403156B1 (en) PHOSPHATIDYLINOSITOL 3-CHINASE INHIBITORS, RELATED COMPOSITIONS AND USES.
WO2012054695A8 (en) Antimicrobial amphiphiles and methods for their use
WO2011123524A3 (en) Macrolide inhibitors of mtor

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 11788289

Country of ref document: EP

Kind code of ref document: A2

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 11788289

Country of ref document: EP

Kind code of ref document: A2