EA019064B1 - Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа - Google Patents

Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа Download PDF

Info

Publication number
EA019064B1
EA019064B1 EA200970935A EA200970935A EA019064B1 EA 019064 B1 EA019064 B1 EA 019064B1 EA 200970935 A EA200970935 A EA 200970935A EA 200970935 A EA200970935 A EA 200970935A EA 019064 B1 EA019064 B1 EA 019064B1
Authority
EA
Eurasian Patent Office
Prior art keywords
amino
phenyl
quinoxaline
sulfonyl
methoxy
Prior art date
Application number
EA200970935A
Other languages
English (en)
Russian (ru)
Other versions
EA200970935A1 (ru
Inventor
Питер Лэмб
Дэвид Мэттьюз
Original Assignee
Экселиксис, Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Экселиксис, Инк. filed Critical Экселиксис, Инк.
Publication of EA200970935A1 publication Critical patent/EA200970935A1/ru
Publication of EA019064B1 publication Critical patent/EA019064B1/ru

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/436Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/555Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • 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)
EA200970935A 2007-04-11 2008-04-08 Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа EA019064B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US92316407P 2007-04-11 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

Publications (2)

Publication Number Publication Date
EA200970935A1 EA200970935A1 (ru) 2010-04-30
EA019064B1 true EA019064B1 (ru) 2013-12-30

Family

ID=39864581

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200970935A EA019064B1 (ru) 2007-04-11 2008-04-08 Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа

Country Status (33)

Country Link
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=)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0617162B8 (pt) * 2005-10-07 2021-05-25 Exelixis Inc compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos
CN101395155A (zh) * 2005-10-07 2009-03-25 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
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
JP2010523670A (ja) * 2007-04-10 2010-07-15 エクセリクシス, インク. Pi3kアルファのピリドピリミジノン阻害剤を使用した治療方法
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
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
EP2590654B1 (en) 2010-07-09 2016-12-21 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
BR112013009643A2 (pt) 2010-10-20 2016-07-19 Merck Serono S A Geneva método para preparar n-(3-amino-quinoxalin-2-il)-sulfonamidas substituídas e seus intermediários n-(3-cloo-quinoxalin-2-il)-sulfonamidas
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
KR20140077911A (ko) * 2011-09-14 2014-06-24 엑셀리시스, 인코포레이티드 암의 치료를 위한 포스파티딜이노시톨 3-키나아제 저해제
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
KR20140096035A (ko) * 2011-10-28 2014-08-04 노파르티스 아게 위장 기질 종양을 치료하는 방법
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
WO2014028479A1 (en) 2012-08-13 2014-02-20 Envoy Therapeutics, Inc. Quinoxaline derivatives as gpr6 modulators
US9745321B2 (en) 2013-09-30 2017-08-29 Shanghai Yingli Pharmaceutical Co., Ltd Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereof
NZ718487A (en) 2013-10-16 2020-01-31 Shanghai Yingli Pharm Co Ltd Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof
JP6526034B2 (ja) 2014-02-14 2019-06-05 武田薬品工業株式会社 Gpr6のピリドピラジンモジュレーター
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

Citations (4)

* 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
WO2007044729A2 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
WO2008021389A2 (en) * 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
WO2008101979A1 (en) * 2007-02-22 2008-08-28 Merck Serono S.A. Quinoxaline compounds and use thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004064734A2 (en) * 2003-01-17 2004-08-05 Threshold Pharmaceuticals, Inc. Combination therapies for the treatment of cancer
CN101395155A (zh) 2005-10-07 2009-03-25 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
JP2010523670A (ja) 2007-04-10 2010-07-15 エクセリクシス, インク. Pi3kアルファのピリドピリミジノン阻害剤を使用した治療方法
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 (4)

* 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
WO2007044729A2 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
WO2008021389A2 (en) * 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
WO2008101979A1 (en) * 2007-02-22 2008-08-28 Merck Serono S.A. Quinoxaline compounds and use thereof

Also Published As

Publication number Publication date
EP2139483A2 (en) 2010-01-06
EP2139483B1 (en) 2013-09-18
CA2684056A1 (en) 2008-10-23
RS53020B (sr) 2014-04-30
CY1114608T1 (el) 2016-10-05
CN103202842A (zh) 2013-07-17
NI200900184A (es) 2011-09-08
PL2139483T3 (pl) 2014-02-28
TN2009000399A1 (fr) 2010-12-31
CR11099A (es) 2010-01-19
GT200900263A (es) 2014-01-15
AU2008239668B2 (en) 2013-11-07
MX2009010929A (es) 2010-01-20
ECSP099723A (es) 2010-03-31
ME00937B (me) 2012-06-20
JP2010523669A (ja) 2010-07-15
PT2139483E (pt) 2013-12-27
ZA200906765B (en) 2010-05-26
EA200970935A1 (ru) 2010-04-30
IL201211A0 (en) 2010-05-31
CO6140024A2 (es) 2010-03-19
UA98141C2 (ru) 2012-04-25
SV2009003390A (es) 2010-05-21
JP5726515B2 (ja) 2015-06-03
MY150797A (en) 2014-02-28
CN101959516A (zh) 2011-01-26
IL201211A (en) 2015-09-24
KR101586774B1 (ko) 2016-01-19
KR20100019436A (ko) 2010-02-18
JP2014074031A (ja) 2014-04-24
DK2139483T3 (da) 2014-01-13
US20110123434A1 (en) 2011-05-26
WO2008127594A3 (en) 2009-04-30
NZ580009A (en) 2012-06-29
HK1140141A1 (en) 2010-10-08
CN101959516B (zh) 2013-05-08
EP2139483B9 (en) 2014-05-21
AU2008239668A1 (en) 2008-10-23
BRPI0810208A2 (pt) 2014-10-21
SI2139483T1 (sl) 2013-11-29
US8481001B2 (en) 2013-07-09
WO2008127594A2 (en) 2008-10-23
MA31335B1 (fr) 2010-04-01
ES2438998T3 (es) 2014-01-21
HRP20131081T1 (hr) 2013-12-20

Similar Documents

Publication Publication Date Title
EA019064B1 (ru) Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа
EA020022B1 (ru) Способы лечения с применением пиридопиримидиноновых ингибиторов pi3k-альфа
US20230151014A1 (en) Compounds, pharmaceutical compositions, and methods of preparing compounds and of their use
US7999006B2 (en) Methods of using MEK inhibitors
CN1976906B (zh) 用作parp抑制剂的取代2-烷基喹唑啉酮衍生物
CA3173955A1 (en) Methods of using myt1 inhibitors
US20250026748A1 (en) N-(5-substituted-[(1,3,4-thiadiazolyl) or (thiazolyl)])(substituted)carboxamide compounds and use thereof for inhibiting human polymerase theta
US20260022114A1 (en) N-(5-substituted-[(1,3,4-thiadiazolyl) or (1,3-thiazolyl)](substituted)carboxamide compounds, pharmaceutical compositions, and methods of preparing the amide compounds and of their use
CN1426310A (zh) 促进排便的药物组合物
JP2019070012A (ja) Torキナーゼ阻害剤組み合わせ療法を使用して癌を治療する方法
KR20160004272A (ko) 전립선암 치료를 위한 디하이드로피라지노-피라진 화합물 및 안드로겐 수용체 길항제를 포함하는 조합요법
TW202313016A (zh) 使用bcl-2抑制劑治療b細胞惡性腫瘤之方法
EP3195865A1 (de) Kombinationen von irak4 inhibitoren und btk inhibitoren
CA3268868A1 (en) Compounds, pharmaceutical compositions, and methods of preparing compounds and of their use
JP2023513016A (ja) Nek2阻害剤としてのアミノピリミジニルアミノベンゾニトリル誘導体
HK1140141B (en) Combination therapies comprising a quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer
AU2013204026A1 (en) Methods of using MEK inhibitors

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU