CN107137402A - 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
CN107137402A
CN107137402A CN201710422322.9A CN201710422322A CN107137402A CN 107137402 A CN107137402 A CN 107137402A CN 201710422322 A CN201710422322 A CN 201710422322A CN 107137402 A CN107137402 A CN 107137402A
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CN
China
Prior art keywords
bases
pyrazine
substituted
unsubstituted
kinase inhibitors
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Pending
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CN201710422322.9A
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English (en)
Chinese (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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Publication of CN107137402A publication Critical patent/CN107137402A/zh
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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57407Specifically defined cancers

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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)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Cell Biology (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Hospice & Palliative Care (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)
CN201710422322.9A 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症 Pending CN107137402A (zh)

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

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201380025102.2A Division CN104302295B (zh) 2012-03-15 2013-03-14 用tor 激酶抑制剂治疗癌症

Publications (1)

Publication Number Publication Date
CN107137402A true CN107137402A (zh) 2017-09-08

Family

ID=47998542

Family Applications (2)

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

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201380025102.2A Active CN104302295B (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) KR20200034818A (enExample)
CN (2) CN107137402A (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) TWI600428B (enExample)
WO (1) WO2013138556A1 (enExample)
ZA (1) ZA201406709B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111095082A (zh) * 2018-03-01 2020-05-01 依视路国际公司 镜片元件

Families Citing this family (19)

* 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
EP2945636B1 (en) 2013-01-16 2017-06-28 Signal Pharmaceuticals, LLC Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
BR112015026257B1 (pt) 2013-04-17 2022-12-20 Signal Pharmaceuticals, Llc Uso de um composto dihidropirazino-pirazina e enzalutamida, composição farmacêutica que os compreende, e kit
SG11201508527VA (en) 2013-04-17 2015-11-27 Signal Pharm Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 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
ES2944478T3 (es) 2013-04-17 2023-06-21 Signal Pharm Llc 1-etil-7-(2-metil-6-(1H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-ona para tratar el glioblastoma multiforme
NZ629411A (en) 2013-04-17 2017-06-30 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
AU2014254057A1 (en) 2013-04-17 2015-11-05 Signal Pharmaceuticals, Llc Combination therapy comprising a TOR kinase inhibitor and N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer
MX368286B (es) 2013-04-17 2019-09-27 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer.
KR102242505B1 (ko) 2013-04-17 2021-04-20 시그날 파마소티칼 엘엘씨 암 치료용 tor 키나제 억제제 및 시티딘 유사체를 포함하는 병용 요법
JP6401250B2 (ja) 2013-05-29 2018-10-10 シグナル ファーマシューティカルズ,エルエルシー 7−(6−(2−ヒドロキシプロパン−2−イル)ピリジン−3−イル)−1−((trans)−4−メトキシシクロヘキシル)−3,4−ジヒドロピラジノ[2,3−b]ピラジン−2(1H)−オン、その固体形態の医薬組成物、及びその使用方法
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
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
US9737535B2 (en) 2014-04-16 2017-08-22 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy comprising administering substituted pyrazino[2,3-b]pyrazines
US9512129B2 (en) 2014-04-16 2016-12-06 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
AU2015289929A1 (en) 2014-07-14 2017-03-02 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions 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
HUE054548T2 (hu) * 2016-12-20 2021-09-28 Astrazeneca Ab Amino-triazolopiridin vegyületek és azok alkalmazása rák kezelésében
EP3641772B1 (en) 2017-06-22 2023-08-02 Celgene Corporation Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
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

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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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JP2013508456A (ja) 2009-10-26 2013-03-07 シグナル ファーマシューティカルズ, エルエルシー ヘテロアリール化合物の合成方法および精製方法

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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
CN102245611A (zh) * 2008-10-27 2011-11-16 西格诺药品有限公司 用于与 mTOR/PI3K/AKT/途径相关的肿瘤适应症和疾病的 mTOR激酶抑制剂
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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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111095082A (zh) * 2018-03-01 2020-05-01 依视路国际公司 镜片元件
US11067832B2 (en) 2018-03-01 2021-07-20 Essilor International Lens element
CN111095082B (zh) * 2018-03-01 2021-11-30 依视路国际公司 镜片元件
US12158637B2 (en) 2018-03-01 2024-12-03 Essilor International Lens element

Also Published As

Publication number Publication date
CA2867349A1 (en) 2013-09-19
TWI664968B (zh) 2019-07-11
KR102057358B1 (ko) 2019-12-18
BR112014022697A2 (pt) 2020-06-30
EA028434B1 (ru) 2017-11-30
WO2013138556A1 (en) 2013-09-19
EA201491694A1 (ru) 2015-06-30
KR20140138929A (ko) 2014-12-04
HK1201755A1 (en) 2015-09-11
TW201343167A (zh) 2013-11-01
AU2013203156C1 (en) 2016-02-18
IL234640B (en) 2020-05-31
TW201733586A (zh) 2017-10-01
IL234640A0 (en) 2014-11-30
PH12014502048A1 (en) 2014-12-10
ES2677908T3 (es) 2018-08-07
JP2015516375A (ja) 2015-06-11
TWI600428B (zh) 2017-10-01
JP6470821B2 (ja) 2019-02-13
JP2018065820A (ja) 2018-04-26
NZ628421A (en) 2016-04-29
KR20200034818A (ko) 2020-03-31
AU2013203156A1 (en) 2013-10-03
AU2013203156B2 (en) 2015-12-10
MY182650A (en) 2021-01-27
MX2014011117A (es) 2015-04-08
IL274318A (en) 2020-06-30
EP2825168B1 (en) 2018-05-09
SG11201405706TA (en) 2014-10-30
EP2825168A1 (en) 2015-01-21
ZA201406709B (en) 2016-07-27
US20130245029A1 (en) 2013-09-19
MX360877B (es) 2018-11-21
CN104302295A (zh) 2015-01-21
NI201400109A (es) 2015-01-15
CN104302295B (zh) 2017-06-20
KR20190058673A (ko) 2019-05-29
PH12018502234A1 (en) 2019-08-14
PH12014502048B1 (en) 2020-10-28
PH12018502234B1 (en) 2021-07-23

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