KR101586774B1 - 암의 치료에 사용하기 위한 ｐｉ３ｋ­알파의 퀴녹살린 억제제를 포함하는 병용 요법 - Google Patents

암의 치료에 사용하기 위한 ｐｉ３ｋ­알파의 퀴녹살린 억제제를 포함하는 병용 요법 Download PDF

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KR101586774B1
KR101586774B1 KR1020097023536A KR20097023536A KR101586774B1 KR 101586774 B1 KR101586774 B1 KR 101586774B1 KR 1020097023536 A KR1020097023536 A KR 1020097023536A KR 20097023536 A KR20097023536 A KR 20097023536A KR 101586774 B1 KR101586774 B1 KR 101586774B1
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nhc
alkyl
cancer
compound
formula
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KR20100019436A (ko
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피터 램
데이비드 매튜즈
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엑셀리시스, 인코포레이티드
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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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  • 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)
KR1020097023536A 2007-04-11 2008-04-08 암의 치료에 사용하기 위한 ｐｉ３ｋ­알파의 퀴녹살린 억제제를 포함하는 병용 요법 Expired - Fee Related KR101586774B1 (ko)

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US92316407P 2007-04-11 2007-04-11
US60/923,164 2007-04-11

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KR20100019436A KR20100019436A (ko) 2010-02-18
KR101586774B1 true KR101586774B1 (ko) 2016-01-19

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KR1020097023536A Expired - Fee Related KR101586774B1 (ko) 2007-04-11 2008-04-08 암의 치료에 사용하기 위한 ｐｉ３ｋ­알파의 퀴녹살린 억제제를 포함하는 병용 요법

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

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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

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WO2007023186A1 (en) * 2005-08-26 2007-03-01 Laboratoires Serono S.A. Pyrazine derivatives and use as pi3k inhibitors
WO2008101979A1 (en) 2007-02-22 2008-08-28 Merck Serono S.A. Quinoxaline compounds and use thereof

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EP1599196A4 (en) * 2003-01-17 2006-05-31 Threshold Pharmaceuticals Inc COMBINATION THERAPIES FOR CANCER TREATMENT
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
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)

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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
WO2008101979A1 (en) 2007-02-22 2008-08-28 Merck Serono S.A. Quinoxaline compounds and use thereof

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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
JP5726515B2 (ja) 2015-06-03
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

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