CN103202842A - 通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法 - Google Patents

通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法 Download PDF

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Publication number
CN103202842A
CN103202842A CN2013101161222A CN201310116122A CN103202842A CN 103202842 A CN103202842 A CN 103202842A CN 2013101161222 A CN2013101161222 A CN 2013101161222A CN 201310116122 A CN201310116122 A CN 201310116122A CN 103202842 A CN103202842 A CN 103202842A
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alkyl
hydrogen
chemotherapeutics
nhc
amino
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Chinese (zh)
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P.兰布
D.马修斯
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Exelixis Inc
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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)
  • 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)
CN2013101161222A 2007-04-11 2008-04-08 通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法 Pending CN103202842A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US92316407P 2007-04-11 2007-04-11
US60/923,164 2007-04-11

Related Parent Applications (1)

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CN2008800173944A Division CN101959516B (zh) 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

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Publication Number Publication Date
CN103202842A true CN103202842A (zh) 2013-07-17

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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
CN2008800173944A Expired - Fee Related CN101959516B (zh) 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

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Country Link
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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ES2513165T3 (es) * 2005-10-07 2014-10-24 Exelixis, Inc. Derivados de N-(3-amino-quinoxalin-2-il)-sulfonamida y su uso como inhibidores de la fosfatidilinositol-3-quinasa
US8044062B2 (en) * 2005-10-07 2011-10-25 Exelixis, Inc. Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha
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
UA100979C2 (ru) * 2007-04-10 2013-02-25 Экселиксис, Инк. Применение пиридопиримидиноновых ингибиторов pi3k альфа для лечения рака
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
BR112013000651A2 (pt) 2010-07-09 2016-05-31 Exelixis Inc combinações de inibidores de cinase para o tratamento de câncer.
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
DE102010048800A1 (de) * 2010-10-20 2012-05-10 Merck Patent Gmbh Chinoxalinderivate
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
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
CN104024257A (zh) * 2011-10-04 2014-09-03 吉利德卡利斯托加有限责任公司 Pi3k的新的喹喔啉抑制剂
WO2013056067A1 (en) 2011-10-13 2013-04-18 Exelixis, Inc. Compounds for use in the treatment of basal cell carcinoma
CN103889422A (zh) * 2011-10-28 2014-06-25 诺华股份有限公司 治疗胃肠道间质瘤的方法
PE20141794A1 (es) 2011-11-01 2014-12-17 Exelixis Inc N-(3-{[(3-{[2-cloro-5-(metoxi)fenil]amino}quinoxalin-2-il)amino]sulfonil}fenil)-2-metilalaninamida como inhibidor de fosfatidilinositol 3-quinasa para el tratamiento de neoplasias 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
US9499561B2 (en) 2012-04-10 2016-11-22 Shanghai Yingli Pharmaceutical Co., Ltd. Fused pyrimidine compound, and preparation method, intermediate, composition, and uses thereof
WO2014028479A1 (en) 2012-08-13 2014-02-20 Envoy Therapeutics, Inc. Quinoxaline derivatives as gpr6 modulators
WO2015043398A1 (zh) 2013-09-30 2015-04-02 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
CA2926596C (en) 2013-10-16 2020-07-14 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
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WO2019119206A1 (en) * 2017-12-18 2019-06-27 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
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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
WO2007023186A1 (en) * 2005-08-26 2007-03-01 Laboratoires Serono S.A. Pyrazine derivatives and use as pi3k inhibitors
ES2513165T3 (es) * 2005-10-07 2014-10-24 Exelixis, Inc. Derivados de N-(3-amino-quinoxalin-2-il)-sulfonamida y su uso como inhibidores de la fosfatidilinositol-3-quinasa
US8044062B2 (en) * 2005-10-07 2011-10-25 Exelixis, Inc. Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha
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
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
UA100979C2 (ru) * 2007-04-10 2013-02-25 Экселиксис, Инк. Применение пиридопиримидиноновых ингибиторов pi3k альфа для лечения рака
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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Publication number Publication date
MY150797A (en) 2014-02-28
IL201211A0 (en) 2010-05-31
NI200900184A (es) 2011-09-08
ECSP099723A (es) 2010-03-31
EP2139483B9 (en) 2014-05-21
MA31335B1 (fr) 2010-04-01
JP2010523669A (ja) 2010-07-15
CN101959516A (zh) 2011-01-26
WO2008127594A2 (en) 2008-10-23
HK1140141A1 (en) 2010-10-08
RS53020B (sr) 2014-04-30
EP2139483B1 (en) 2013-09-18
CY1114608T1 (el) 2016-10-05
SI2139483T1 (sl) 2013-11-29
MX2009010929A (es) 2010-01-20
EP2139483A2 (en) 2010-01-06
EA019064B1 (ru) 2013-12-30
GT200900263A (es) 2014-01-15
KR101586774B1 (ko) 2016-01-19
HRP20131081T1 (hr) 2013-12-20
AU2008239668B2 (en) 2013-11-07
PL2139483T3 (pl) 2014-02-28
CR11099A (es) 2010-01-19
KR20100019436A (ko) 2010-02-18
JP2014074031A (ja) 2014-04-24
IL201211A (en) 2015-09-24
JP5726515B2 (ja) 2015-06-03
AU2008239668A1 (en) 2008-10-23
ME00937B (me) 2012-06-20
WO2008127594A3 (en) 2009-04-30
US8481001B2 (en) 2013-07-09
EA200970935A1 (ru) 2010-04-30
SV2009003390A (es) 2010-05-21
NZ580009A (en) 2012-06-29
PT2139483E (pt) 2013-12-27
CO6140024A2 (es) 2010-03-19
UA98141C2 (ru) 2012-04-25
US20110123434A1 (en) 2011-05-26
ZA200906765B (en) 2010-05-26
CN101959516B (zh) 2013-05-08
TN2009000399A1 (fr) 2010-12-31
ES2438998T3 (es) 2014-01-21
CA2684056A1 (en) 2008-10-23
DK2139483T3 (da) 2014-01-13
BRPI0810208A2 (pt) 2014-10-21

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Application publication date: 20130717