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)
  • 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)
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 (OSRAM)
EP (1) EP2139483B9 (OSRAM)
JP (2) JP5726515B2 (OSRAM)
KR (1) KR101586774B1 (OSRAM)
CN (2) CN101959516B (OSRAM)
AU (1) AU2008239668B2 (OSRAM)
BR (1) BRPI0810208A2 (OSRAM)
CA (1) CA2684056A1 (OSRAM)
CO (1) CO6140024A2 (OSRAM)
CR (1) CR11099A (OSRAM)
CY (1) CY1114608T1 (OSRAM)
DK (1) DK2139483T3 (OSRAM)
EA (1) EA019064B1 (OSRAM)
EC (1) ECSP099723A (OSRAM)
ES (1) ES2438998T3 (OSRAM)
GT (1) GT200900263A (OSRAM)
HR (1) HRP20131081T1 (OSRAM)
IL (1) IL201211A (OSRAM)
MA (1) MA31335B1 (OSRAM)
ME (1) ME00937B (OSRAM)
MX (1) MX2009010929A (OSRAM)
MY (1) MY150797A (OSRAM)
NI (1) NI200900184A (OSRAM)
NZ (1) NZ580009A (OSRAM)
PL (1) PL2139483T3 (OSRAM)
PT (1) PT2139483E (OSRAM)
RS (1) RS53020B (OSRAM)
SI (1) SI2139483T1 (OSRAM)
SV (1) SV2009003390A (OSRAM)
TN (1) TN2009000399A1 (OSRAM)
UA (1) UA98141C2 (OSRAM)
WO (1) WO2008127594A2 (OSRAM)
ZA (1) ZA200906765B (OSRAM)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2019119206A1 (en) 2017-12-18 2019-06-27 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta

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
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
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
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

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
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
WO2008127594A3 (en) 2009-04-30
MA31335B1 (fr) 2010-04-01
EP2139483A2 (en) 2010-01-06
JP2010523669A (ja) 2010-07-15
CN101959516B (zh) 2013-05-08
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

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
TW202019900A (zh) Ptpn11抑制劑
US20250026748A1 (en) N-(5-substituted-[(1,3,4-thiadiazolyl) or (thiazolyl)])(substituted)carboxamide compounds and use thereof for inhibiting human polymerase theta
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
WO2024197401A1 (en) 1,3,4-thiadiazol-2-yl carboxamide and 1,3-thiazol-2-yl carboxamide compounds and uses thereof as inhibitors of human polymerase theta
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