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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JP2010523669A5 (enExample
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)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (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)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (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) 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 (28)

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US7989622B2 (en) * 2005-10-07 2011-08-02 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
EA016945B1 (ru) * 2005-10-07 2012-08-30 Экселиксис, Инк. ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα
CN101528231A (zh) 2006-08-16 2009-09-09 埃克塞利希斯股份有限公司 在癌症的治疗中使用pi3k和mek调控剂
MY150697A (en) * 2007-04-10 2014-02-28 Exelixis Inc Methods of treating cancer using pyridopyrimdinone inhibitors of p13k alpha
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
UY33221A (es) 2010-02-09 2011-09-30 Univ California MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA
PH12013500064A1 (en) 2010-07-09 2013-03-11 Exelixis Inc Combinations of kinase inhibitors for the treatment of cancer
EP2616442B8 (en) 2010-09-14 2018-10-17 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
KR20130141528A (ko) 2010-10-20 2013-12-26 메르크 세로노 에스에이 제네바 치환 ｎ-(3-아미노-퀴녹살린-2-일)-술폰아미드 및 이들의 중간체인 ｎ-(3-클로로-퀴녹살린-2-일)술폰아미드의 제조 방법
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
BR112014005858A2 (pt) * 2011-09-14 2017-06-13 Exelixis Inc inibidores de fosfatidilinositol 3-quinase para tratamento de câncer
HK1201065A1 (en) * 2011-10-04 2015-08-21 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
RU2014120792A (ru) * 2011-10-28 2015-12-10 Новартис Аг Способ лечения стромальных опухолей желудочно-кишечного тракта
CN107375289A (zh) * 2011-11-01 2017-11-24 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‑激酶抑制剂的化合物
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
US9499561B2 (en) 2012-04-10 2016-11-22 Shanghai Yingli Pharmaceutical Co., Ltd. Fused pyrimidine compound, and preparation method, intermediate, composition, and uses thereof
EP2882722B1 (en) 2012-08-13 2016-07-27 Takeda Pharmaceutical Company Limited Quinoxaline derivatives as gpr6 modulators
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
CN104557872B (zh) 2013-10-16 2017-05-24 上海璎黎药业有限公司 稠合杂环化合物、其制备方法、药物组合物和用途
WO2015123505A1 (en) 2014-02-14 2015-08-20 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
WO2023220131A2 (en) * 2022-05-10 2023-11-16 Relay Therapeutics, Inc. PI3Kα INHIBITORS AND METHODS OF USE THEREOF

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1599196A4 (en) * 2003-01-17 2006-05-31 Threshold Pharmaceuticals Inc COMBINATION THERAPIES FOR CANCER TREATMENT
US8071597B2 (en) * 2005-08-26 2011-12-06 Merck Serono Sa Pyrazine compounds and uses as PI3K inhibitors
US7989622B2 (en) 2005-10-07 2011-08-02 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
EA016945B1 (ru) 2005-10-07 2012-08-30 Экселиксис, Инк. ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα
CN101528231A (zh) * 2006-08-16 2009-09-09 埃克塞利希斯股份有限公司 在癌症的治疗中使用pi3k和mek调控剂
JP5508027B2 (ja) 2007-02-22 2014-05-28 メルク セローノ ソシエテ アノニム キノキサリン化合物及びその使用
MY150697A (en) 2007-04-10 2014-02-28 Exelixis Inc Methods of treating cancer using pyridopyrimdinone inhibitors of p13k 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

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

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