JP5726515B2 - Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法 - Google Patents

Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法 Download PDF

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JP5726515B2
JP5726515B2 JP2010503043A JP2010503043A JP5726515B2 JP 5726515 B2 JP5726515 B2 JP 5726515B2 JP 2010503043 A JP2010503043 A JP 2010503043A JP 2010503043 A JP2010503043 A JP 2010503043A JP 5726515 B2 JP5726515 B2 JP 5726515B2
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nhc
cancer
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formula
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JP2010523669A5 (OSRAM
JP2010523669A (ja
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ピーター ラム，
ピーター ラム，
デイヴィッド マシューズ，
デイヴィッド マシューズ，
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エクセリクシス， インク．
エクセリクシス， インク．
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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)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (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)
JP2010503043A 2007-04-11 2008-04-08 Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法 Active JP5726515B2 (ja)

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

Related Child Applications (1)

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JP2013228684A Division JP2014074031A (ja) 2007-04-11 2013-11-01 Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法

Publications (3)

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JP2010523669A JP2010523669A (ja) 2010-07-15
JP2010523669A5 JP2010523669A5 (OSRAM) 2013-05-16
JP5726515B2 true JP5726515B2 (ja) 2015-06-03

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JP2010503043A Active JP5726515B2 (ja) 2007-04-11 2008-04-08 Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法
JP2013228684A Pending JP2014074031A (ja) 2007-04-11 2013-11-01 Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法

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Country Status (33)

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

Families Citing this family (27)

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CN101282948A (zh) * 2005-10-07 2008-10-08 埃克塞里艾克西斯公司 N-(3-氨基-喹喔啉-2-基)-磺酰胺衍生物及其作为磷脂酰肌醇3-激酶抑制剂的用途
JP5461012B2 (ja) * 2005-10-07 2014-04-02 エクセリクシス， インク． ＰＩ３Ｋαのピリドピリミジノン型阻害剤
WO2008021389A2 (en) 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
DK2139484T3 (da) * 2007-04-10 2013-10-21 Exelixis Inc Fremgangsmåder til behandling af cancer ved brug af pyridopyrimidinon-inhibitorer af PI3K-alfa
PT2374802E (pt) * 2008-11-10 2014-07-10 Kyowa Hakko Kirin Co Ltd Inibidor de produção de quinurenina
DE102009049679A1 (de) 2009-10-19 2011-04-21 Merck Patent Gmbh Pyrazolopyrimidinderivate
AR080151A1 (es) 2010-02-09 2012-03-14 Exelixis Inc Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia
AR084469A1 (es) 2010-07-09 2013-05-22 Exelixis Inc Combinaciones de inhibidores de quinasas para el tratamiento del cancer
TWI642670B (zh) 2010-09-14 2018-12-01 伊塞利克斯公司 Ｐｉ３ｋ-德爾塔抑制劑以及其應用和生產方法
CA2815107A1 (en) 2010-10-20 2012-04-26 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
DE102010048800A1 (de) 2010-10-20 2012-05-10 Merck Patent Gmbh Chinoxalinderivate
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
TW201325592A (zh) * 2011-09-14 2013-07-01 Exelixis Inc 用於治療癌症之磷脂醯肌醇－３激酶抑制劑
EP2763994A4 (en) * 2011-10-04 2015-08-26 Gilead Calistoga Llc NEW QUINOXALINE INHIBITORS OF THE PI3K PATH
WO2013056067A1 (en) 2011-10-13 2013-04-18 Exelixis, Inc. Compounds for use in the treatment of basal cell carcinoma
EP2770999A1 (en) * 2011-10-28 2014-09-03 Novartis AG Method of treating gastrointestinal stromal tumors
CN104302294A (zh) * 2011-11-01 2015-01-21 埃克塞利希斯股份有限公司 用于治疗淋巴组织增生性恶性肿瘤的作为磷脂酰肌醇3-激酶抑制剂的n-(3-{[(3-{[2-氯-5-(甲氧基)苯基]氨基}喹喔啉-2-基)氨基]磺酰基}苯基)-2-甲基丙氨酰胺
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
CN103467482B (zh) 2012-04-10 2017-05-10 上海璎黎药业有限公司 稠合嘧啶类化合物，其制备方法，中间体，组合物和应用
EP2882722B1 (en) 2012-08-13 2016-07-27 Takeda Pharmaceutical Company Limited Quinoxaline derivatives as gpr6 modulators
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
AU2014336775B2 (en) 2013-10-16 2018-04-05 Shanghai Yingli Pharmaceutical Co., Ltd Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof
EP3105230B1 (en) 2014-02-14 2021-04-07 Takeda Pharmaceutical Company Limited Pyridopyrazines 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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
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
MX2008002723A (es) * 2005-08-26 2008-03-26 Serono Lab Derivados de pirazina y uso como inhibidores de p13k.
JP5461012B2 (ja) * 2005-10-07 2014-04-02 エクセリクシス， インク． ＰＩ３Ｋαのピリドピリミジノン型阻害剤
CN101282948A (zh) * 2005-10-07 2008-10-08 埃克塞里艾克西斯公司 N-(3-氨基-喹喔啉-2-基)-磺酰胺衍生物及其作为磷脂酰肌醇3-激酶抑制剂的用途
WO2008021389A2 (en) 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
NZ578229A (en) 2007-02-22 2012-02-24 Merck Serono Sa Quinoxaline compounds and use thereof
DK2139484T3 (da) * 2007-04-10 2013-10-21 Exelixis Inc Fremgangsmåder til behandling af cancer ved brug af pyridopyrimidinon-inhibitorer af PI3K-alfa
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

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Publication number Publication date
HRP20131081T1 (hr) 2013-12-20
MY150797A (en) 2014-02-28
SV2009003390A (es) 2010-05-21
EA200970935A1 (ru) 2010-04-30
CR11099A (es) 2010-01-19
MX2009010929A (es) 2010-01-20
HK1140141A1 (en) 2010-10-08
UA98141C2 (ru) 2012-04-25
CA2684056A1 (en) 2008-10-23
WO2008127594A2 (en) 2008-10-23
AU2008239668B2 (en) 2013-11-07
EA019064B1 (ru) 2013-12-30
WO2008127594A3 (en) 2009-04-30
MA31335B1 (fr) 2010-04-01
EP2139483A2 (en) 2010-01-06
JP2010523669A (ja) 2010-07-15
CN101959516B (zh) 2013-05-08
ECSP099723A (es) 2010-03-31
GT200900263A (es) 2014-01-15
JP2014074031A (ja) 2014-04-24
NI200900184A (es) 2011-09-08
TN2009000399A1 (fr) 2010-12-31
CO6140024A2 (es) 2010-03-19
PL2139483T3 (pl) 2014-02-28
NZ580009A (en) 2012-06-29
ME00937B (me) 2012-06-20
DK2139483T3 (da) 2014-01-13
KR20100019436A (ko) 2010-02-18
CN103202842A (zh) 2013-07-17
US8481001B2 (en) 2013-07-09
RS53020B (sr) 2014-04-30
CY1114608T1 (el) 2016-10-05
ZA200906765B (en) 2010-05-26
EP2139483B9 (en) 2014-05-21
PT2139483E (pt) 2013-12-27
US20110123434A1 (en) 2011-05-26
BRPI0810208A2 (pt) 2014-10-21
AU2008239668A1 (en) 2008-10-23
CN101959516A (zh) 2011-01-26
EP2139483B1 (en) 2013-09-18
SI2139483T1 (sl) 2013-11-29
IL201211A (en) 2015-09-24
KR101586774B1 (ko) 2016-01-19
ES2438998T3 (es) 2014-01-21
IL201211A0 (en) 2010-05-31

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