CN104302295B - 用tor 激酶抑制剂治疗癌症 - Google Patents

用tor 激酶抑制剂治疗癌症 Download PDF

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Publication number
CN104302295B
CN104302295B CN201380025102.2A CN201380025102A CN104302295B CN 104302295 B CN104302295 B CN 104302295B CN 201380025102 A CN201380025102 A CN 201380025102A CN 104302295 B CN104302295 B CN 104302295B
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substituted
pyrazin
unsubstituted
methyl
triazol
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Chinese (zh)
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CN104302295A (zh
Inventor
徐水蟾
克里斯汀·梅·海格
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Signal Pharmaceuticals LLC
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Signal Pharmaceuticals LLC
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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
    • A61K31/395—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
    • A61K31/435—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
    • A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57557—Immunoassay; Biospecific binding assay; Materials therefor for cancer of other specific parts of the body, e.g. brain

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Biotechnology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
CN201380025102.2A 2012-03-15 2013-03-14 用tor 激酶抑制剂治疗癌症 Active CN104302295B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201710422322.9A CN107137402A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261611370P 2012-03-15 2012-03-15
US61/611,370 2012-03-15
US201261715329P 2012-10-18 2012-10-18
US61/715,329 2012-10-18
PCT/US2013/031202 WO2013138556A1 (en) 2012-03-15 2013-03-14 Treatment of cancer with tor kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201710422322.9A Division CN107137402A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症

Publications (2)

Publication Number Publication Date
CN104302295A CN104302295A (zh) 2015-01-21
CN104302295B true CN104302295B (zh) 2017-06-20

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CN201380025102.2A Active CN104302295B (zh) 2012-03-15 2013-03-14 用tor 激酶抑制剂治疗癌症
CN201710422322.9A Pending CN107137402A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症

Family Applications After (1)

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CN201710422322.9A Pending CN107137402A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症

Country Status (20)

Country Link
US (1) US20130245029A1 (enExample)
EP (1) EP2825168B1 (enExample)
JP (2) JP2015516375A (enExample)
KR (3) KR102057358B1 (enExample)
CN (2) CN104302295B (enExample)
AU (1) AU2013203156C1 (enExample)
BR (1) BR112014022697A2 (enExample)
CA (1) CA2867349A1 (enExample)
EA (1) EA028434B1 (enExample)
ES (1) ES2677908T3 (enExample)
IL (2) IL234640B (enExample)
MX (1) MX360877B (enExample)
MY (1) MY182650A (enExample)
NI (1) NI201400109A (enExample)
NZ (1) NZ628421A (enExample)
PH (2) PH12014502048B1 (enExample)
SG (1) SG11201405706TA (enExample)
TW (2) TWI664968B (enExample)
WO (1) WO2013138556A1 (enExample)
ZA (1) ZA201406709B (enExample)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
SG11201505446WA (en) 2013-01-16 2015-08-28 Signal Pharm Llc Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
CA2908742C (en) 2013-04-17 2021-06-01 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
MY189663A (en) 2013-04-17 2022-02-23 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
HK1221168A1 (zh) 2013-04-17 2017-05-26 西格诺药品有限公司 用於治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯醯胺的组合疗法
WO2014172425A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
EP3549940A1 (en) 2013-04-17 2019-10-09 Signal Pharmaceuticals, LLC Pharmaceutical formulations, of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl) pyridin-3-yl) -3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one
WO2014172436A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
JP6382946B2 (ja) 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ，エルエルシー ジヒドロピラジノ−ピラジンによる癌治療
CN107474051B (zh) 2013-05-29 2020-10-30 西格诺药品有限公司 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
WO2015160880A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
EP3131552B1 (en) 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
US9718824B2 (en) 2014-04-16 2017-08-01 Signal Pharmaceuticals, Llc Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof
NZ629796A (en) 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
WO2016010886A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
DK3558997T3 (da) * 2016-12-20 2021-04-19 Astrazeneca Ab Aminotriazolopyridinforbindelser og deres anvendelse til behandling af cancer
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection
BR202019004173Y1 (pt) 2018-03-01 2024-02-20 Essilor International Dispositivo óptico
KR102822755B1 (ko) 2018-03-01 2025-06-19 에씰로 앙터나시오날 렌즈 요소
CN113493471B (zh) * 2020-04-03 2024-06-11 山东轩竹医药科技有限公司 杂芳环类激酶抑制剂

Citations (4)

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WO2008051494A1 (en) * 2006-10-19 2008-05-02 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and use thereof as protein kinase inhibitors
WO2008051493A2 (en) * 2006-10-19 2008-05-02 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and their use as protein kinase inhibitors
WO2010062571A1 (en) * 2008-10-27 2010-06-03 Signal Pharmaceuticals, Llc Mtor kinase inhibitors for oncology indications and diseases associated with the mtor/p13k/akt pathway
WO2011133668A2 (en) * 2010-04-20 2011-10-27 President And Fellows Of Harvard College Methods and compositions for the treatment of cancer

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Patent Citations (4)

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WO2008051494A1 (en) * 2006-10-19 2008-05-02 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and use thereof as protein kinase inhibitors
WO2008051493A2 (en) * 2006-10-19 2008-05-02 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and their use as protein kinase inhibitors
WO2010062571A1 (en) * 2008-10-27 2010-06-03 Signal Pharmaceuticals, Llc Mtor kinase inhibitors for oncology indications and diseases associated with the mtor/p13k/akt pathway
WO2011133668A2 (en) * 2010-04-20 2011-10-27 President And Fellows Of Harvard College Methods and compositions for the treatment of cancer

Also Published As

Publication number Publication date
TWI664968B (zh) 2019-07-11
IL274318A (en) 2020-06-30
EP2825168B1 (en) 2018-05-09
KR20200034818A (ko) 2020-03-31
NZ628421A (en) 2016-04-29
SG11201405706TA (en) 2014-10-30
US20130245029A1 (en) 2013-09-19
MX2014011117A (es) 2015-04-08
PH12018502234B1 (en) 2021-07-23
AU2013203156B2 (en) 2015-12-10
TW201343167A (zh) 2013-11-01
HK1201755A1 (en) 2015-09-11
AU2013203156C1 (en) 2016-02-18
ES2677908T3 (es) 2018-08-07
TW201733586A (zh) 2017-10-01
PH12014502048A1 (en) 2014-12-10
EA201491694A1 (ru) 2015-06-30
NI201400109A (es) 2015-01-15
CN107137402A (zh) 2017-09-08
KR20140138929A (ko) 2014-12-04
AU2013203156A1 (en) 2013-10-03
ZA201406709B (en) 2016-07-27
PH12018502234A1 (en) 2019-08-14
JP2015516375A (ja) 2015-06-11
CN104302295A (zh) 2015-01-21
TWI600428B (zh) 2017-10-01
IL234640A0 (en) 2014-11-30
KR20190058673A (ko) 2019-05-29
MY182650A (en) 2021-01-27
EA028434B1 (ru) 2017-11-30
PH12014502048B1 (en) 2020-10-28
BR112014022697A2 (pt) 2020-06-30
KR102057358B1 (ko) 2019-12-18
CA2867349A1 (en) 2013-09-19
MX360877B (es) 2018-11-21
JP2018065820A (ja) 2018-04-26
JP6470821B2 (ja) 2019-02-13
IL234640B (en) 2020-05-31
WO2013138556A1 (en) 2013-09-19
EP2825168A1 (en) 2015-01-21

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