EA200970935A1 - Способы лечения с применением хинаксолиновых ингибиторов pi3k-альфа - Google Patents

Способы лечения с применением хинаксолиновых ингибиторов pi3k-альфа

Info

Publication number
EA200970935A1
EA200970935A1 EA200970935A EA200970935A EA200970935A1 EA 200970935 A1 EA200970935 A1 EA 200970935A1 EA 200970935 A EA200970935 A EA 200970935A EA 200970935 A EA200970935 A EA 200970935A EA 200970935 A1 EA200970935 A1 EA 200970935A1
Authority
EA
Eurasian Patent Office
Prior art keywords
hynaxoline
pi3k
inhibitors
alpha
application
Prior art date
Application number
EA200970935A
Other languages
English (en)
Other versions
EA019064B1 (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

    • 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

Abstract

Настоящее изобретение обеспечивает способы лечения рака путем введения соединения формулы I, возможно в виде фармацевтически приемлемой соли, сольвата и/или гидрата указанного соединения, в сочетании с другими способами лечения рака.
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 true EA200970935A1 (ru) 2010-04-30
EA019064B1 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 (34)

Country Link
US (1) US8481001B2 (ru)
EP (1) EP2139483B9 (ru)
JP (2) JP5726515B2 (ru)
KR (1) KR101586774B1 (ru)
CN (2) CN101959516B (ru)
AU (1) AU2008239668B2 (ru)
BR (1) BRPI0810208A2 (ru)
CA (1) CA2684056A1 (ru)
CO (1) CO6140024A2 (ru)
CR (1) CR11099A (ru)
CY (1) CY1114608T1 (ru)
DK (1) DK2139483T3 (ru)
EA (1) EA019064B1 (ru)
EC (1) ECSP099723A (ru)
ES (1) ES2438998T3 (ru)
GT (1) GT200900263A (ru)
HK (1) HK1140141A1 (ru)
HR (1) HRP20131081T1 (ru)
IL (1) IL201211A (ru)
MA (1) MA31335B1 (ru)
ME (1) ME00937B (ru)
MX (1) MX2009010929A (ru)
MY (1) MY150797A (ru)
NI (1) NI200900184A (ru)
NZ (1) NZ580009A (ru)
PL (1) PL2139483T3 (ru)
PT (1) PT2139483E (ru)
RS (1) RS53020B (ru)
SI (1) SI2139483T1 (ru)
SV (1) SV2009003390A (ru)
TN (1) TN2009000399A1 (ru)
UA (1) UA98141C2 (ru)
WO (1) WO2008127594A2 (ru)
ZA (1) ZA200906765B (ru)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ594628A (en) * 2005-10-07 2013-04-26 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka
EA019255B1 (ru) * 2005-10-07 2014-02-28 Экселиксис, Инк. Ингибиторы фосфатидилинозит-3-киназы и содержащие их фармацевтические композиции
CA2658725A1 (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
ES2463676T3 (es) * 2008-11-10 2014-05-28 Kyowa Hakko Kirin Co., Ltd. Inhibidor de la producción de quinurenina
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
WO2012006552A1 (en) 2010-07-09 2012-01-12 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
DE102010048800A1 (de) 2010-10-20 2012-05-10 Merck Patent Gmbh Chinoxalinderivate
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
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
CA2853095A1 (en) * 2011-10-28 2013-05-02 Novartis Ag Method of treating gastrointestinal stromal tumors
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
WO2013101964A1 (en) * 2011-12-27 2013-07-04 Kadmon Corporation, Llc Methods for treatment of breast cancer nonresponsive 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
EP2882722B1 (en) 2012-08-13 2016-07-27 Takeda Pharmaceutical Company Limited Quinoxaline derivatives as gpr6 modulators
EP3053926B1 (en) 2013-09-30 2018-08-08 Shanghai Yingli Pharmaceutical Co. Ltd. Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereof
CA2926596C (en) 2013-10-16 2020-07-14 Shanghai Yingli Pharmaceutical Co., Ltd Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof
WO2015123505A1 (en) 2014-02-14 2015-08-20 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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060276527A1 (en) * 2003-01-17 2006-12-07 Thresold Pharmaceuticals, Inc. Combination therapies for the treatment of cancer
MX2008002723A (es) * 2005-08-26 2008-03-26 Serono Lab Derivados de pirazina y uso como inhibidores de p13k.
EA019255B1 (ru) * 2005-10-07 2014-02-28 Экселиксис, Инк. Ингибиторы фосфатидилинозит-3-киназы и содержащие их фармацевтические композиции
NZ594628A (en) * 2005-10-07 2013-04-26 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka
CA2658725A1 (en) 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
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
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

Also Published As

Publication number Publication date
NI200900184A (es) 2011-09-08
EA019064B1 (ru) 2013-12-30
MX2009010929A (es) 2010-01-20
AU2008239668A1 (en) 2008-10-23
JP2014074031A (ja) 2014-04-24
EP2139483B1 (en) 2013-09-18
ES2438998T3 (es) 2014-01-21
WO2008127594A2 (en) 2008-10-23
PL2139483T3 (pl) 2014-02-28
CO6140024A2 (es) 2010-03-19
EP2139483B9 (en) 2014-05-21
GT200900263A (es) 2014-01-15
CN101959516B (zh) 2013-05-08
CN101959516A (zh) 2011-01-26
ZA200906765B (en) 2010-05-26
CN103202842A (zh) 2013-07-17
ME00937B (me) 2012-06-20
ECSP099723A (es) 2010-03-31
MY150797A (en) 2014-02-28
CR11099A (es) 2010-01-19
TN2009000399A1 (fr) 2010-12-31
NZ580009A (en) 2012-06-29
UA98141C2 (ru) 2012-04-25
IL201211A0 (en) 2010-05-31
BRPI0810208A2 (pt) 2014-10-21
IL201211A (en) 2015-09-24
MA31335B1 (fr) 2010-04-01
EP2139483A2 (en) 2010-01-06
KR101586774B1 (ko) 2016-01-19
WO2008127594A3 (en) 2009-04-30
AU2008239668B2 (en) 2013-11-07
US20110123434A1 (en) 2011-05-26
HRP20131081T1 (hr) 2013-12-20
CA2684056A1 (en) 2008-10-23
US8481001B2 (en) 2013-07-09
JP2010523669A (ja) 2010-07-15
CY1114608T1 (el) 2016-10-05
SI2139483T1 (sl) 2013-11-29
SV2009003390A (es) 2010-05-21
KR20100019436A (ko) 2010-02-18
DK2139483T3 (da) 2014-01-13
HK1140141A1 (en) 2010-10-08
RS53020B (en) 2014-04-30
PT2139483E (pt) 2013-12-27
JP5726515B2 (ja) 2015-06-03

Similar Documents

Publication Publication Date Title
EA200970935A1 (ru) Способы лечения с применением хинаксолиновых ингибиторов pi3k-альфа
EA200970932A1 (ru) Способы лечения с применением пиридопиримидиноновых ингибиторов pi3k альфа
EA201390085A1 (ru) Композиции ингибиторов киназ для лечения рака
TR201900306T4 (tr) Mek inhibitörlerini kullanma yöntemleri.
EA200970856A1 (ru) Ингибиторы пути хеджхога
EA201270247A1 (ru) Способы применения с-мет-модуляторов
TW200738725A (en) Unsaturated mTOR inhibitors
TN2011000293A1 (en) Protein kinase inhibitors
EA201391486A1 (ru) Способы и композиции для лечения болезни паркинсона
TN2011000298A1 (en) Compounds useful for inhibiting chk1
EA201391485A1 (ru) Способы и композиции для лечения нейродегенеративных заболеваний
TW200740776A (en) N-phenylbenzotriazolyl c-kit inhibitors
EA201001196A1 (ru) Соединения 4-пиридинона и их применение для лечения рака
TW201613577A (en) Pharmaceutical combinations
MX2010004967A (es) Uso de inhibidor de cfms para el tratamiento y la prevención del cancer de hueso, así como la perdida osea y el dolor de hueso asociados con el cancer de hueso.
EA201390499A1 (ru) Соединения, подходящие для ингибирования снк1
CY1114609T1 (el) Μεθοδοι θεραπειας καρκινου χρησιμοποιωντας αναστολεις p13k αλφα με βαση πυριδοπυριμιδινονη
UA110834C2 (uk) Сполука-інгібітор сигнального шляху notch
UA99612C2 (en) Inhibitors of the hedgehog pathway

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