EA019064B1 - Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа - Google Patents

Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа Download PDF

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Publication number
EA019064B1
EA019064B1 EA200970935A EA200970935A EA019064B1 EA 019064 B1 EA019064 B1 EA 019064B1 EA 200970935 A EA200970935 A EA 200970935A EA 200970935 A EA200970935 A EA 200970935A EA 019064 B1 EA019064 B1 EA 019064B1
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EA
Eurasian Patent Office
Prior art keywords
amino
phenyl
quinoxaline
sulfonyl
methoxy
Prior art date
Application number
EA200970935A
Other languages
English (en)
Russian (ru)
Other versions
EA200970935A1 (ru
Inventor
Питер Лэмб
Дэвид Мэттьюз
Original Assignee
Экселиксис, Инк.
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 Экселиксис, Инк. filed Critical Экселиксис, Инк.
Publication of EA200970935A1 publication Critical patent/EA200970935A1/ru
Publication of EA019064B1 publication Critical patent/EA019064B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/436Heterocyclic 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
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/555Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • 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
    • 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

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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)
EA200970935A 2007-04-11 2008-04-08 Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа EA019064B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US92316407P 2007-04-11 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
EA200970935A1 EA200970935A1 (ru) 2010-04-30
EA019064B1 true EA019064B1 (ru) 2013-12-30

Family

ID=39864581

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200970935A EA019064B1 (ru) 2007-04-11 2008-04-08 Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа

Country Status (33)

Country Link
US (1) US8481001B2 (enExample)
EP (1) EP2139483B9 (enExample)
JP (2) JP5726515B2 (enExample)
KR (1) KR101586774B1 (enExample)
CN (2) CN103202842A (enExample)
AU (1) AU2008239668B2 (enExample)
BR (1) BRPI0810208A2 (enExample)
CA (1) CA2684056A1 (enExample)
CO (1) CO6140024A2 (enExample)
CR (1) CR11099A (enExample)
CY (1) CY1114608T1 (enExample)
DK (1) DK2139483T3 (enExample)
EA (1) EA019064B1 (enExample)
EC (1) ECSP099723A (enExample)
ES (1) ES2438998T3 (enExample)
GT (1) GT200900263A (enExample)
HR (1) HRP20131081T1 (enExample)
IL (1) IL201211A (enExample)
MA (1) MA31335B1 (enExample)
ME (1) ME00937B (enExample)
MX (1) MX2009010929A (enExample)
MY (1) MY150797A (enExample)
NI (1) NI200900184A (enExample)
NZ (1) NZ580009A (enExample)
PL (1) PL2139483T3 (enExample)
PT (1) PT2139483E (enExample)
RS (1) RS53020B (enExample)
SI (1) SI2139483T1 (enExample)
SV (1) SV2009003390A (enExample)
TN (1) TN2009000399A1 (enExample)
UA (1) UA98141C2 (enExample)
WO (1) WO2008127594A2 (enExample)
ZA (1) ZA200906765B (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
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GEP20115304B (en) * 2005-10-07 2011-10-10 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
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
ATE539752T1 (de) 2006-08-16 2012-01-15 Exelixis Inc Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung
JP2010523670A (ja) * 2007-04-10 2010-07-15 エクセリクシス, インク. Pi3kアルファのピリドピリミジノン阻害剤を使用した治療方法
US8673908B2 (en) 2008-11-10 2014-03-18 Kyowa Hakko Kirin Co., Ltd. Kynurenine production inhibitor
DE102009049679A1 (de) 2009-10-19 2011-04-21 Merck Patent Gmbh Pyrazolopyrimidinderivate
WO2011100319A1 (en) 2010-02-09 2011-08-18 Exelixis, Inc. Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k and mtor in combination with autophagy inhibitors
AR084469A1 (es) 2010-07-09 2013-05-22 Exelixis Inc Combinaciones de inhibidores de quinasas para el tratamiento del cancer
AU2011302196B2 (en) 2010-09-14 2016-04-28 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
AU2012308414A1 (en) * 2011-09-14 2014-05-01 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of cancer
CA2850763A1 (en) * 2011-10-04 2013-04-11 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
CA2853095A1 (en) * 2011-10-28 2013-05-02 Novartis Ag Method of treating gastrointestinal stromal tumors
SG11201401961UA (en) * 2011-11-01 2014-05-29 Exelixis Inc N- (3- { [ (3- { [2-chloro-5- (methoxy) phenyl] amino} quinoxalin- 2 -yl) amino] sulfonyl} phe nyl) - 2 -methylalaninamide as phosphatidylinositol 3 - kinase inhibitor for the treatment of lymphoproliferative malignancies
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
EP2860181B1 (en) 2012-04-10 2019-02-13 Shanghai Yingli Pharmaceutical Co. Ltd. Fused pyrimidine compound, and preparation method, intermediate, composition and uses thereof
JP6193374B2 (ja) 2012-08-13 2017-09-06 武田薬品工業株式会社 Gpr6モジュレーターとしてのキノキサリン誘導体
CN104513254B (zh) 2013-09-30 2019-07-26 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
RU2663999C2 (ru) 2013-10-16 2018-08-14 Шанхай Инли Фармасьютикал Ко., Лтд Конденсированное гетероциклическое соединение, способ его получения, его фармацевтическая композиция и применения
JP6526034B2 (ja) 2014-02-14 2019-06-05 武田薬品工業株式会社 Gpr6のピリドピラジンモジュレーター
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 (4)

* 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
WO2008021389A2 (en) * 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
WO2008101979A1 (en) * 2007-02-22 2008-08-28 Merck Serono S.A. Quinoxaline compounds and use thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004064734A2 (en) * 2003-01-17 2004-08-05 Threshold Pharmaceuticals, Inc. Combination therapies for the treatment of cancer
GEP20115304B (en) * 2005-10-07 2011-10-10 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
JP2010523670A (ja) * 2007-04-10 2010-07-15 エクセリクシス, インク. Pi3kアルファのピリドピリミジノン阻害剤を使用した治療方法
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 (4)

* 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
WO2008021389A2 (en) * 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
WO2008101979A1 (en) * 2007-02-22 2008-08-28 Merck Serono S.A. Quinoxaline compounds and use thereof

Also Published As

Publication number Publication date
PL2139483T3 (pl) 2014-02-28
CA2684056A1 (en) 2008-10-23
RS53020B (sr) 2014-04-30
HK1140141A1 (en) 2010-10-08
GT200900263A (es) 2014-01-15
CR11099A (es) 2010-01-19
JP2010523669A (ja) 2010-07-15
MX2009010929A (es) 2010-01-20
AU2008239668A1 (en) 2008-10-23
IL201211A (en) 2015-09-24
MY150797A (en) 2014-02-28
NI200900184A (es) 2011-09-08
EP2139483B1 (en) 2013-09-18
CN101959516B (zh) 2013-05-08
SV2009003390A (es) 2010-05-21
EP2139483A2 (en) 2010-01-06
KR101586774B1 (ko) 2016-01-19
MA31335B1 (fr) 2010-04-01
AU2008239668B2 (en) 2013-11-07
CY1114608T1 (el) 2016-10-05
TN2009000399A1 (fr) 2010-12-31
CN101959516A (zh) 2011-01-26
KR20100019436A (ko) 2010-02-18
CN103202842A (zh) 2013-07-17
WO2008127594A2 (en) 2008-10-23
EA200970935A1 (ru) 2010-04-30
UA98141C2 (ru) 2012-04-25
ES2438998T3 (es) 2014-01-21
DK2139483T3 (da) 2014-01-13
CO6140024A2 (es) 2010-03-19
BRPI0810208A2 (pt) 2014-10-21
WO2008127594A3 (en) 2009-04-30
EP2139483B9 (en) 2014-05-21
HRP20131081T1 (hr) 2013-12-20
NZ580009A (en) 2012-06-29
ZA200906765B (en) 2010-05-26
JP2014074031A (ja) 2014-04-24
ECSP099723A (es) 2010-03-31
US8481001B2 (en) 2013-07-09
IL201211A0 (en) 2010-05-31
JP5726515B2 (ja) 2015-06-03
ME00937B (me) 2012-06-20
PT2139483E (pt) 2013-12-27
US20110123434A1 (en) 2011-05-26
SI2139483T1 (sl) 2013-11-29

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU