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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JP2010523669A (ja
JP2010523669A5 (enExample
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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)

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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

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

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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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US (1) US8481001B2 (enExample)
EP (1) EP2139483B9 (enExample)
JP (2) JP5726515B2 (enExample)
KR (1) KR101586774B1 (enExample)
CN (2) CN101959516B (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)

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NZ594628A (en) * 2005-10-07 2013-04-26 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka
RS53627B1 (sr) * 2005-10-07 2015-04-30 Exelixis Inc. Derivati n-(3-amino-hinoksalin-2-il)-sulfonamida i njihova upotreba kao inhibitora fosfatidilinozitol3-kinaze
WO2008021389A2 (en) 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
RS52939B (sr) * 2007-04-10 2014-02-28 Exelixis Inc. Postupci za lečenje kancera upotrebom piridopirimidinonskih inhibitora pi3k alfa
EP2374802B1 (en) 2008-11-10 2014-04-23 Kyowa Hakko Kirin Co., Ltd. Kynurenine production inhibitor
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
CA2803900A1 (en) 2010-07-09 2012-01-12 Exelixis, Inc. Combinations of kinase inhibitors for the treatment of cancer
JP5792819B2 (ja) 2010-09-14 2015-10-14 エクセリクシス， インク． Ｐｉ３ｋ−デルタの阻害剤ならびにそれらの使用法および製造法
DE102010048800A1 (de) * 2010-10-20 2012-05-10 Merck Patent Gmbh Chinoxalinderivate
JP2013540141A (ja) 2010-10-20 2013-10-31 メルク セローノ ソシエテ アノニム ジュネーブ 置換ｎ−（３−アミノ−キノキサリン−２−イル）−スルホンアミドおよびそれらの中間体ｎ−（３−クロロ−キノキサリン−２−イル）スルホンアミドを調製する方法
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
US20140235643A1 (en) * 2011-10-04 2014-08-21 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
EA201490905A1 (ru) * 2011-11-01 2014-11-28 Экселиксис, Инк. N-(3-{[(3-{[2-хлор-5-(метокси)фенил]амино}хиноксалин-2-ил)амино]сульфонил}фенил)-2-метилаланинамид как ингибитор фосфатидилинозитол-3-киназы для лечения лимфопролиферативных злокачественных заболеваний
WO2013067306A1 (en) * 2011-11-02 2013-05-10 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers
JP2015503568A (ja) * 2011-12-27 2015-02-02 カドモン コーポレイション，リミティド ライアビリティ カンパニー トラスツズマブに不応性の乳癌の治療方法
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
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
EP3053926B1 (en) 2013-09-30 2018-08-08 Shanghai Yingli Pharmaceutical Co. Ltd. Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereof
JP6139789B2 (ja) 2013-10-16 2017-05-31 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 縮合複素環化合物、その調製方法、医薬組成物及びその使用
WO2015123505A1 (en) 2014-02-14 2015-08-20 Takeda Pharmaceutical Company Limited Pyridopyrazines modulators of gpr6
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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
EA015937B1 (ru) * 2005-08-26 2011-12-30 Мерк Сероно С.А. Производные пиразина и их применение в качестве ингибиторов pi3k
NZ594628A (en) 2005-10-07 2013-04-26 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka
RS53627B1 (sr) 2005-10-07 2015-04-30 Exelixis Inc. Derivati n-(3-amino-hinoksalin-2-il)-sulfonamida i njihova upotreba kao inhibitora fosfatidilinozitol3-kinaze
WO2008021389A2 (en) * 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
EP2118076B1 (en) * 2007-02-22 2019-09-04 Merck Serono S.A. Quinoxaline compounds and use thereof
RS52939B (sr) 2007-04-10 2014-02-28 Exelixis Inc. Postupci za lečenje kancera upotrebom piridopirimidinonskih inhibitora 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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AU2008239668A1 (en) 2008-10-23
KR20100019436A (ko) 2010-02-18
ZA200906765B (en) 2010-05-26
RS53020B (sr) 2014-04-30
TN2009000399A1 (fr) 2010-12-31
CN101959516A (zh) 2011-01-26
MA31335B1 (fr) 2010-04-01
CA2684056A1 (en) 2008-10-23
MX2009010929A (es) 2010-01-20
ME00937B (me) 2012-06-20
BRPI0810208A2 (pt) 2014-10-21
EA200970935A1 (ru) 2010-04-30
KR101586774B1 (ko) 2016-01-19
AU2008239668B2 (en) 2013-11-07
IL201211A (en) 2015-09-24
ECSP099723A (es) 2010-03-31
DK2139483T3 (da) 2014-01-13
MY150797A (en) 2014-02-28
GT200900263A (es) 2014-01-15
EP2139483A2 (en) 2010-01-06
WO2008127594A3 (en) 2009-04-30
ES2438998T3 (es) 2014-01-21
US8481001B2 (en) 2013-07-09
EA019064B1 (ru) 2013-12-30
NZ580009A (en) 2012-06-29
JP2010523669A (ja) 2010-07-15
HRP20131081T1 (hr) 2013-12-20
PT2139483E (pt) 2013-12-27
SI2139483T1 (sl) 2013-11-29
US20110123434A1 (en) 2011-05-26
EP2139483B1 (en) 2013-09-18
CN101959516B (zh) 2013-05-08
CO6140024A2 (es) 2010-03-19
UA98141C2 (ru) 2012-04-25
CN103202842A (zh) 2013-07-17
PL2139483T3 (pl) 2014-02-28
CR11099A (es) 2010-01-19
NI200900184A (es) 2011-09-08
HK1140141A1 (en) 2010-10-08
WO2008127594A2 (en) 2008-10-23
IL201211A0 (en) 2010-05-31
CY1114608T1 (el) 2016-10-05
JP2014074031A (ja) 2014-04-24
EP2139483B9 (en) 2014-05-21
SV2009003390A (es) 2010-05-21

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