CN101959516B - 用以治疗癌症的包含喹喔啉PI3Kα抑制剂的组合治疗 - Google Patents

用以治疗癌症的包含喹喔啉PI3Kα抑制剂的组合治疗 Download PDF

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CN101959516B
CN101959516B CN2008800173944A CN200880017394A CN101959516B CN 101959516 B CN101959516 B CN 101959516B CN 2008800173944 A CN2008800173944 A CN 2008800173944A CN 200880017394 A CN200880017394 A CN 200880017394A CN 101959516 B CN101959516 B CN 101959516B
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CN101959516A (zh
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P·兰布
D·马修斯
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Exelixis Inc
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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)
CN2008800173944A 2007-04-11 2008-04-08 用以治疗癌症的包含喹喔啉PI3Kα抑制剂的组合治疗 Expired - Fee Related CN101959516B (zh)

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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CN2013101161222A Division CN103202842A (zh) 2007-04-11 2008-04-08 通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法

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CN101959516A CN101959516A (zh) 2011-01-26
CN101959516B true CN101959516B (zh) 2013-05-08

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CN2013101161222A Pending CN103202842A (zh) 2007-04-11 2008-04-08 通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法

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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)

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
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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
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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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Non-Patent Citations (1)

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孙小平等.喹喔啉双氮氧化物衍生物QN-2013的乏氧细胞毒性和放射增敏作用.《北京大学学报(医学版)》.2001,第33卷(第2期),140-143. *

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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
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
JP5726515B2 (ja) 2015-06-03
ES2438998T3 (es) 2014-01-21
IL201211A0 (en) 2010-05-31

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