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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  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (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)

Applications Claiming Priority (2)

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

Publications (2)

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

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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)
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CA (1) CA2684056A1 (enExample)
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ES (1) ES2438998T3 (enExample)
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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)
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UA (1) UA98141C2 (enExample)
WO (1) WO2008127594A2 (enExample)
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EP2364974A1 (en) * 2005-10-07 2011-09-14 Exelixis, Inc. N-(3-Phenylamino-quinoxalin-2-yl)-benzenesulfonamide derivatives as phosphatidylinositol 3-kinase inhibitors
HRP20130902T1 (hr) * 2005-10-07 2013-11-08 Exelixis Inc. PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa
JP2010500994A (ja) 2006-08-16 2010-01-14 エグゼリクシス， インコーポレイテッド Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
ES2430614T3 (es) * 2007-04-10 2013-11-21 Exelixis, Inc. Métodos de tratamiento del cáncer usando inhibidores de piridopirimidinona de PI3K alfa
WO2010053182A1 (ja) * 2008-11-10 2010-05-14 協和発酵キリン株式会社 キヌレニン産生抑制剤
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
SG186889A1 (en) 2010-07-09 2013-02-28 Exelixis Inc Combinations of kinase inhibitors for the treatment of cancer
AR082985A1 (es) 2010-09-14 2013-01-23 Exelixis Inc INHIBIDORES DE PI3K-d Y METODOS DE SU USO Y PREPARACION
US20130211076A1 (en) 2010-10-20 2013-08-15 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
CA2848724A1 (en) * 2011-09-14 2013-03-21 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of cancer
JP2014528451A (ja) * 2011-10-04 2014-10-27 ギリアード カリストガ エルエルシー Ｐｉ３ｋの新規キノキサリン阻害剤
WO2013056067A1 (en) 2011-10-13 2013-04-18 Exelixis, Inc. Compounds for use in the treatment of basal cell carcinoma
US20140288073A1 (en) * 2011-10-28 2014-09-25 Novartis Ag Method of Treating Gastrointestinal Stromal Tumors
MX2014005249A (es) * 2011-11-01 2015-03-05 Exelixis Inc N-(3-{[(3-{[2-cloro-5-(metoxi)fenil]amino}quinoxalin-2-il)amino]s ulfonil}fenil)-2-metilalaninamida como inhibidor de fosfatidilinositol 3-cinasa para el tratamiento de neoplasias malignas linfoproliferativas.
WO2013067306A1 (en) * 2011-11-02 2013-05-10 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers
EP2797628A4 (en) 2011-12-27 2015-07-29 Kadmon Corp Llc METHOD FOR THE TREATMENT OF BREAST CANCER NOT RELATED TO TRASTUZUMAB
WO2013152717A1 (zh) 2012-04-10 2013-10-17 上海昀怡健康管理咨询有限公司 稠合嘧啶类化合物，其制备方法，中间体，组合物和应用
WO2014028479A1 (en) 2012-08-13 2014-02-20 Envoy Therapeutics, Inc. 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
KR101982912B1 (ko) 2013-10-16 2019-09-10 상하이 잉리 파마슈티컬 컴퍼니 리미티드 융합된 헤테로사이클릭 화합물, 이의 제조 방법, 약학적 조성물, 및 그 용도
US10179783B2 (en) 2014-02-14 2019-01-15 Taketa Pharmaceutical Company Limited Tetrahydropyridopyrazines as 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

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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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US20060276527A1 (en) * 2003-01-17 2006-12-07 Thresold Pharmaceuticals, Inc. Combination therapies for the treatment of cancer
HRP20130902T1 (hr) 2005-10-07 2013-11-08 Exelixis Inc. PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa
EP2364974A1 (en) 2005-10-07 2011-09-14 Exelixis, Inc. N-(3-Phenylamino-quinoxalin-2-yl)-benzenesulfonamide derivatives as phosphatidylinositol 3-kinase inhibitors
JP2010500994A (ja) 2006-08-16 2010-01-14 エグゼリクシス， インコーポレイテッド Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
ES2430614T3 (es) 2007-04-10 2013-11-21 Exelixis, Inc. Métodos de tratamiento del cáncer usando inhibidores de piridopirimidinona de 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

Patent Citations (2)

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

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KR20100019436A (ko) 2010-02-18
EP2139483B1 (en) 2013-09-18
BRPI0810208A2 (pt) 2014-10-21
CR11099A (es) 2010-01-19
EP2139483B9 (en) 2014-05-21
JP2014074031A (ja) 2014-04-24
IL201211A (en) 2015-09-24
EA200970935A1 (ru) 2010-04-30
MY150797A (en) 2014-02-28
RS53020B (sr) 2014-04-30
NZ580009A (en) 2012-06-29
SI2139483T1 (sl) 2013-11-29
CN103202842A (zh) 2013-07-17
ZA200906765B (en) 2010-05-26
GT200900263A (es) 2014-01-15
ECSP099723A (es) 2010-03-31
WO2008127594A2 (en) 2008-10-23
CY1114608T1 (el) 2016-10-05
WO2008127594A3 (en) 2009-04-30
CN101959516A (zh) 2011-01-26
JP2010523669A (ja) 2010-07-15
MA31335B1 (fr) 2010-04-01
HRP20131081T1 (hr) 2013-12-20
IL201211A0 (en) 2010-05-31
ES2438998T3 (es) 2014-01-21
CN101959516B (zh) 2013-05-08
DK2139483T3 (da) 2014-01-13
US8481001B2 (en) 2013-07-09
NI200900184A (es) 2011-09-08
JP5726515B2 (ja) 2015-06-03
AU2008239668B2 (en) 2013-11-07
AU2008239668A1 (en) 2008-10-23
CO6140024A2 (es) 2010-03-19
EP2139483A2 (en) 2010-01-06
SV2009003390A (es) 2010-05-21
CA2684056A1 (en) 2008-10-23
US20110123434A1 (en) 2011-05-26
UA98141C2 (ru) 2012-04-25
ME00937B (me) 2012-06-20
MX2009010929A (es) 2010-01-20
TN2009000399A1 (fr) 2010-12-31
HK1140141A1 (en) 2010-10-08
EA019064B1 (ru) 2013-12-30
PL2139483T3 (pl) 2014-02-28
PT2139483E (pt) 2013-12-27

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