AU2008239668B2 - Combination therapies comprising quinoxaline inhibitors of PI3K-alpha for use in the treatment of cancer - Google Patents

Combination therapies comprising quinoxaline inhibitors of PI3K-alpha for use in the treatment of cancer Download PDF

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Publication number
AU2008239668B2
AU2008239668B2 AU2008239668A AU2008239668A AU2008239668B2 AU 2008239668 B2 AU2008239668 B2 AU 2008239668B2 AU 2008239668 A AU2008239668 A AU 2008239668A AU 2008239668 A AU2008239668 A AU 2008239668A AU 2008239668 B2 AU2008239668 B2 AU 2008239668B2
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AU
Australia
Prior art keywords
nhc
compound
amino
cancer
quinoxalin
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Ceased
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AU2008239668A
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English (en)
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AU2008239668A1 (en
Inventor
Peter Lamb
David Matthews
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Exelixis Inc
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Exelixis Inc
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Publication of AU2008239668A1 publication Critical patent/AU2008239668A1/en
Application granted granted Critical
Publication of AU2008239668B2 publication Critical patent/AU2008239668B2/en
Ceased legal-status Critical Current
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    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2008239668A 2007-04-11 2008-04-08 Combination therapies comprising quinoxaline inhibitors of PI3K-alpha for use in the treatment of cancer Ceased AU2008239668B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US92316407P 2007-04-11 2007-04-11
US60/923,164 2007-04-11
PCT/US2008/004570 WO2008127594A2 (en) 2007-04-11 2008-04-08 Combination therapies comprising quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer

Publications (2)

Publication Number Publication Date
AU2008239668A1 AU2008239668A1 (en) 2008-10-23
AU2008239668B2 true AU2008239668B2 (en) 2013-11-07

Family

ID=39864581

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2008239668A Ceased AU2008239668B2 (en) 2007-04-11 2008-04-08 Combination therapies comprising quinoxaline inhibitors of PI3K-alpha for use in the treatment of cancer

Country Status (33)

Country Link
US (1) US8481001B2 (Direct)
EP (1) EP2139483B9 (Direct)
JP (2) JP5726515B2 (Direct)
KR (1) KR101586774B1 (Direct)
CN (2) CN101959516B (Direct)
AU (1) AU2008239668B2 (Direct)
BR (1) BRPI0810208A2 (Direct)
CA (1) CA2684056A1 (Direct)
CO (1) CO6140024A2 (Direct)
CR (1) CR11099A (Direct)
CY (1) CY1114608T1 (Direct)
DK (1) DK2139483T3 (Direct)
EA (1) EA019064B1 (Direct)
EC (1) ECSP099723A (Direct)
ES (1) ES2438998T3 (Direct)
GT (1) GT200900263A (Direct)
HR (1) HRP20131081T1 (Direct)
IL (1) IL201211A (Direct)
MA (1) MA31335B1 (Direct)
ME (1) ME00937B (Direct)
MX (1) MX2009010929A (Direct)
MY (1) MY150797A (Direct)
NI (1) NI200900184A (Direct)
NZ (1) NZ580009A (Direct)
PL (1) PL2139483T3 (Direct)
PT (1) PT2139483E (Direct)
RS (1) RS53020B (Direct)
SI (1) SI2139483T1 (Direct)
SV (1) SV2009003390A (Direct)
TN (1) TN2009000399A1 (Direct)
UA (1) UA98141C2 (Direct)
WO (1) WO2008127594A2 (Direct)
ZA (1) ZA200906765B (Direct)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ594630A (en) * 2005-10-07 2013-04-26 Exelixis Inc N-(3-amino-quinoxalin-2-yl)-sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
GEP20115304B (en) * 2005-10-07 2011-10-10 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
WO2008021389A2 (en) 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
HRP20130688T1 (en) * 2007-04-10 2013-09-30 Exelixis Inc. Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k alpha
PL2374802T3 (pl) * 2008-11-10 2014-09-30 Kyowa Hakko Kirin Co Ltd Inhibitor wytwarzania kinureniny
DE102009049679A1 (de) 2009-10-19 2011-04-21 Merck Patent Gmbh Pyrazolopyrimidinderivate
TW201139436A (en) 2010-02-09 2011-11-16 Exelixis Inc Methods of treating cancer using pyridopyrimidinone inhibitors of PI3K and mTOR in combination with autophagy inhibitors
TW201244719A (en) 2010-07-09 2012-11-16 Exelixis Inc Combinations of kinase inhibitors for the treatment of cancer
CA2812089C (en) 2010-09-14 2020-02-18 Exelixis Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
DE102010048800A1 (de) 2010-10-20 2012-05-10 Merck Patent Gmbh Chinoxalinderivate
AU2011317675A1 (en) 2010-10-20 2013-05-02 Merck Serono S.A. Geneva Method for preparing substituted N-(3-amino-quinoxalin-2-yl)-sulfonamides and their intermediates N-(3-chloro-quinoxalin-2-yl)sulfonamides
DE102010049595A1 (de) 2010-10-26 2012-04-26 Merck Patent Gmbh Chinazolinderivate
WO2012065057A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
CA2848724A1 (en) * 2011-09-14 2013-03-21 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of cancer
AU2012318580A1 (en) * 2011-10-04 2014-05-22 Gilead Calistoga Llc Novel quinoxaline inhibitors of PI3K
WO2013056067A1 (en) 2011-10-13 2013-04-18 Exelixis, Inc. Compounds for use in the treatment of basal cell carcinoma
RU2014120792A (ru) * 2011-10-28 2015-12-10 Новартис Аг Способ лечения стромальных опухолей желудочно-кишечного тракта
PE20141794A1 (es) * 2011-11-01 2014-12-17 Exelixis Inc N-(3-{[(3-{[2-cloro-5-(metoxi)fenil]amino}quinoxalin-2-il)amino]sulfonil}fenil)-2-metilalaninamida como inhibidor de fosfatidilinositol 3-quinasa para el tratamiento de neoplasias linfoproliferativas
WO2013067306A1 (en) * 2011-11-02 2013-05-10 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers
CA2860051A1 (en) 2011-12-27 2013-07-04 Kadmon Corporation, Llc Methods for treatment of breast cancer nonresponsive to trastuzumab
JP6077642B2 (ja) 2012-04-10 2017-02-08 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合ピリミジン化合物、その調製法、中間体、組成物、及び使用
WO2014028479A1 (en) 2012-08-13 2014-02-20 Envoy Therapeutics, Inc. Quinoxaline derivatives as gpr6 modulators
WO2015043398A1 (zh) 2013-09-30 2015-04-02 上海璎黎药业有限公司 稠合嘧啶类化合物、中间体、其制备方法、组合物和应用
MX381304B (es) 2013-10-16 2025-03-12 Shanghai Yingli Pharm Co Ltd Compuesto heterocíclico fusionado, método de preparación del mismo, composición farmacéutica, y usos del mismo.
US10179783B2 (en) 2014-02-14 2019-01-15 Taketa Pharmaceutical Company Limited Tetrahydropyridopyrazines as modulators of GPR6
US9950194B2 (en) 2014-09-09 2018-04-24 Mevion Medical Systems, Inc. Patient positioning system
WO2019119206A1 (en) * 2017-12-18 2019-06-27 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007023186A1 (en) * 2005-08-26 2007-03-01 Laboratoires Serono S.A. Pyrazine derivatives and use as pi3k inhibitors
WO2007044729A2 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors

Family Cites Families (6)

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Publication number Priority date Publication date Assignee Title
JP2006515885A (ja) * 2003-01-17 2006-06-08 スレッシュオールド ファーマシューティカルズ， インコーポレイテッド 癌の処置のための併用療法
GEP20115304B (en) * 2005-10-07 2011-10-10 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
WO2008021389A2 (en) 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
ZA200904857B (en) * 2007-02-22 2010-09-29 Merck Serono Sa Quinoxaline compounds and use thereof
HRP20130688T1 (en) * 2007-04-10 2013-09-30 Exelixis Inc. Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k alpha
JP4623164B2 (ja) * 2008-08-21 2011-02-02 セイコーエプソン株式会社 プロジェクタ

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007023186A1 (en) * 2005-08-26 2007-03-01 Laboratoires Serono S.A. Pyrazine derivatives and use as pi3k inhibitors
WO2007044729A2 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors

Also Published As

Publication number Publication date
US8481001B2 (en) 2013-07-09
CR11099A (es) 2010-01-19
KR101586774B1 (ko) 2016-01-19
IL201211A (en) 2015-09-24
WO2008127594A3 (en) 2009-04-30
HRP20131081T1 (hr) 2013-12-20
PT2139483E (pt) 2013-12-27
ZA200906765B (en) 2010-05-26
NZ580009A (en) 2012-06-29
AU2008239668A1 (en) 2008-10-23
CA2684056A1 (en) 2008-10-23
PL2139483T3 (pl) 2014-02-28
RS53020B (sr) 2014-04-30
EA019064B1 (ru) 2013-12-30
CY1114608T1 (el) 2016-10-05
CN101959516A (zh) 2011-01-26
EA200970935A1 (ru) 2010-04-30
MY150797A (en) 2014-02-28
ECSP099723A (es) 2010-03-31
SI2139483T1 (sl) 2013-11-29
IL201211A0 (en) 2010-05-31
UA98141C2 (ru) 2012-04-25
MX2009010929A (es) 2010-01-20
BRPI0810208A2 (pt) 2014-10-21
EP2139483B9 (en) 2014-05-21
WO2008127594A2 (en) 2008-10-23
ME00937B (me) 2012-06-20
MA31335B1 (fr) 2010-04-01
JP5726515B2 (ja) 2015-06-03
JP2010523669A (ja) 2010-07-15
HK1140141A1 (en) 2010-10-08
GT200900263A (es) 2014-01-15
NI200900184A (es) 2011-09-08
ES2438998T3 (es) 2014-01-21
JP2014074031A (ja) 2014-04-24
CN101959516B (zh) 2013-05-08
TN2009000399A1 (fr) 2010-12-31
EP2139483B1 (en) 2013-09-18
KR20100019436A (ko) 2010-02-18
US20110123434A1 (en) 2011-05-26
CN103202842A (zh) 2013-07-17
CO6140024A2 (es) 2010-03-19
SV2009003390A (es) 2010-05-21
EP2139483A2 (en) 2010-01-06
DK2139483T3 (da) 2014-01-13

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