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

Info

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
Authority
CN
China
Prior art keywords
alkyl
hydrogen
chemotherapeutics
nhc
amino
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN2013101161222A
Other languages
English (en)
Chinese (zh)
Inventor
P.兰布
D.马修斯
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Exelixis Inc
Original Assignee
Exelixis Inc
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 Exelixis Inc filed Critical Exelixis Inc
Publication of CN103202842A publication Critical patent/CN103202842A/zh
Pending legal-status Critical Current

Links

Images

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

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)
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)

Application Number Title Priority Date Filing Date
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

Publications (1)

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

Family

ID=39864581

Family Applications (2)

Application Number Title Priority Date Filing Date
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

Family Applications After (1)

Application Number Title Priority Date Filing Date
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

Country Status (33)

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 (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1940839B1 (en) * 2005-10-07 2013-07-31 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kalpha
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
ATE539752T1 (de) 2006-08-16 2012-01-15 Exelixis Inc Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung
ES2430614T3 (es) * 2007-04-10 2013-11-21 Exelixis, Inc. Métodos de tratamiento del cáncer usando inhibidores de piridopirimidinona de PI3K alfa
JP5687903B2 (ja) * 2008-11-10 2015-03-25 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
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
UY33498A (es) 2010-07-09 2013-01-03 Sanofi Aventis Combinaciones de inhibidores de quinasas para el tratamiento de cancer
AU2011302196B2 (en) 2010-09-14 2016-04-28 Exelixis, Inc. Inhibitors of PI3K-delta and methods of their use and manufacture
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
IN2014CN02671A (enExample) * 2011-09-14 2015-07-03 Exelixis Inc
CA2850763A1 (en) * 2011-10-04 2013-04-11 Gilead Calistoga Llc Novel quinoxaline inhibitors of pi3k
WO2013056067A1 (en) 2011-10-13 2013-04-18 Exelixis, Inc. Compounds for use in the treatment of basal cell carcinoma
JP2014532647A (ja) * 2011-10-28 2014-12-08 ノバルティス アーゲー 消化管間質腫瘍を治療する方法
AU2012332486A1 (en) * 2011-11-01 2014-06-19 Arthur Decillis N- (3- { [ (3- { [2-chloro-5- (methoxy) phenyl] amino} quinoxalin- 2 -yl) amino] sulfonyl} phe nyl) - 2 -methylalaninamide as phosphatidylinositol 3 - kinase inhibitor for the treatment of lymphoproliferative malignancies
WO2013067306A1 (en) * 2011-11-02 2013-05-10 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers
US20150010545A1 (en) * 2011-12-27 2015-01-08 Kadmon Corporation, Llc Methods for treatment of breast cancer nonresponsive to trastuzumab
WO2013152717A1 (zh) 2012-04-10 2013-10-17 上海昀怡健康管理咨询有限公司 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
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
CN104557872B (zh) 2013-10-16 2017-05-24 上海璎黎药业有限公司 稠合杂环化合物、其制备方法、药物组合物和用途
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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1599196A4 (en) * 2003-01-17 2006-05-31 Threshold Pharmaceuticals Inc COMBINATION THERAPIES FOR CANCER TREATMENT
JP5226513B2 (ja) * 2005-08-26 2013-07-03 メルク セローノ ソシエテ アノニム ピラジン誘導体及びその使用
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
EP1940839B1 (en) 2005-10-07 2013-07-31 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kalpha
ATE539752T1 (de) 2006-08-16 2012-01-15 Exelixis Inc Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung
ZA200904857B (en) 2007-02-22 2010-09-29 Merck Serono Sa Quinoxaline compounds and use thereof
ES2430614T3 (es) 2007-04-10 2013-11-21 Exelixis, Inc. Métodos de tratamiento del cáncer usando inhibidores de piridopirimidinona de 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
EA019064B1 (ru) 2013-12-30
WO2008127594A2 (en) 2008-10-23
EP2139483B1 (en) 2013-09-18
GT200900263A (es) 2014-01-15
PT2139483E (pt) 2013-12-27
CN101959516A (zh) 2011-01-26
DK2139483T3 (da) 2014-01-13
MA31335B1 (fr) 2010-04-01
BRPI0810208A2 (pt) 2014-10-21
EP2139483B9 (en) 2014-05-21
CR11099A (es) 2010-01-19
AU2008239668B2 (en) 2013-11-07
UA98141C2 (ru) 2012-04-25
NZ580009A (en) 2012-06-29
SV2009003390A (es) 2010-05-21
CN101959516B (zh) 2013-05-08
HRP20131081T1 (hr) 2013-12-20
JP2014074031A (ja) 2014-04-24
JP5726515B2 (ja) 2015-06-03
ECSP099723A (es) 2010-03-31
IL201211A (en) 2015-09-24
EP2139483A2 (en) 2010-01-06
IL201211A0 (en) 2010-05-31
CY1114608T1 (el) 2016-10-05
MX2009010929A (es) 2010-01-20
MY150797A (en) 2014-02-28
WO2008127594A3 (en) 2009-04-30
US8481001B2 (en) 2013-07-09
HK1140141A1 (en) 2010-10-08
ES2438998T3 (es) 2014-01-21
NI200900184A (es) 2011-09-08
AU2008239668A1 (en) 2008-10-23
US20110123434A1 (en) 2011-05-26
CA2684056A1 (en) 2008-10-23
PL2139483T3 (pl) 2014-02-28
EA200970935A1 (ru) 2010-04-30
ZA200906765B (en) 2010-05-26
SI2139483T1 (sl) 2013-11-29
KR101586774B1 (ko) 2016-01-19
CO6140024A2 (es) 2010-03-19
RS53020B (sr) 2014-04-30
TN2009000399A1 (fr) 2010-12-31
KR20100019436A (ko) 2010-02-18
ME00937B (me) 2012-06-20
JP2010523669A (ja) 2010-07-15

Similar Documents

Publication Publication Date Title
CN103202842A (zh) 通过用喹喔啉PI3Kα抑制剂抑制来治疗的方法
CN102727498B (zh) 使用吡啶并嘧啶酮PI3Kα抑制剂的治疗方法
EP2056829B9 (en) Using pi3k and mek modulators in treatments of cancer
CN1976906B (zh) 用作parp抑制剂的取代2-烷基喹唑啉酮衍生物
EP1931645B1 (en) N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
EP2142543B1 (en) Pyrido [2, 3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
WO2012065057A2 (en) Phosphatidylinositol 3-kinase inhibitors and methods of their use
HK1140141B (en) Combination therapies comprising a quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer
AU2013201011B2 (en) N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
WO2013067306A1 (en) Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers
CN103748095A (zh) 二环杂芳族化合物
HK1139948B (en) Pyrido [2, 3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
HK1162170A (en) N-(3-phenylamino-quinoxalin-2-yl)-benzenesulfonamide derivatives as phosphatidylinositol 3-kinase inhibitors
HK1119697B (en) N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
HK1130438B (en) Using pi3k and mek modulators in treatments of cancer

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20130717