CN104519887B - 包含B‑Raf抑制剂、EGFR抑制剂和任选PI3Kα抑制剂的药物组合 - Google Patents

包含B‑Raf抑制剂、EGFR抑制剂和任选PI3Kα抑制剂的药物组合 Download PDF

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Publication number
CN104519887B
CN104519887B CN201380042229.5A CN201380042229A CN104519887B CN 104519887 B CN104519887 B CN 104519887B CN 201380042229 A CN201380042229 A CN 201380042229A CN 104519887 B CN104519887 B CN 104519887B
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compound
inhibitor
combination
raf
cetuximab
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Chinese (zh)
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CN104519887A (zh
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G·卡波尼格罗
D·斯图尔特
帕斯瓦 L·穆图-德
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Array Biopharma Inc
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Novartis AG
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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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201380042229.5A 2012-08-07 2013-08-05 包含B‑Raf抑制剂、EGFR抑制剂和任选PI3Kα抑制剂的药物组合 Active CN104519887B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261680473P 2012-08-07 2012-08-07
US61/680,473 2012-08-07
PCT/US2013/053619 WO2014025688A1 (en) 2012-08-07 2013-08-05 Pharmaceutical combinations comprising a b-raf inhibitor, an egfr inhibitor and optionally a pi3k-alpha inhibitor

Publications (2)

Publication Number Publication Date
CN104519887A CN104519887A (zh) 2015-04-15
CN104519887B true CN104519887B (zh) 2017-06-27

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CN201380042229.5A Active CN104519887B (zh) 2012-08-07 2013-08-05 包含B‑Raf抑制剂、EGFR抑制剂和任选PI3Kα抑制剂的药物组合

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Country Link
US (1) US9474754B2 (enExample)
EP (2) EP3574904A1 (enExample)
JP (3) JP6342396B2 (enExample)
KR (1) KR102112885B1 (enExample)
CN (1) CN104519887B (enExample)
AR (1) AR092045A1 (enExample)
AU (1) AU2013299841B8 (enExample)
CA (1) CA2879548C (enExample)
CL (1) CL2015000294A1 (enExample)
CO (1) CO7200273A2 (enExample)
CY (1) CY1122143T1 (enExample)
DK (1) DK2882440T3 (enExample)
EA (1) EA028420B1 (enExample)
EC (1) ECSP15008695A (enExample)
ES (1) ES2717911T3 (enExample)
GT (1) GT201500025A (enExample)
HK (1) HK1211831A1 (enExample)
HR (1) HRP20190537T1 (enExample)
HU (1) HUE042877T2 (enExample)
IL (1) IL236934B (enExample)
IN (1) IN2015DN00450A (enExample)
JO (1) JOP20130236B1 (enExample)
LT (1) LT2882440T (enExample)
MA (1) MA37829A1 (enExample)
MX (1) MX359403B (enExample)
MY (1) MY176031A (enExample)
NZ (1) NZ703940A (enExample)
PE (2) PE20191655A1 (enExample)
PH (1) PH12015500246A1 (enExample)
PL (1) PL2882440T3 (enExample)
PT (1) PT2882440T (enExample)
RS (1) RS58734B1 (enExample)
SG (1) SG11201500321YA (enExample)
SI (1) SI2882440T1 (enExample)
TN (1) TN2015000027A1 (enExample)
TR (1) TR201904980T4 (enExample)
TW (1) TWI607754B (enExample)
UA (1) UA115786C2 (enExample)
WO (1) WO2014025688A1 (enExample)

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* Cited by examiner, † Cited by third party
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SG11201500321YA (en) * 2012-08-07 2015-04-29 Novartis Ag Pharmaceutical combinations comprising a b-raf inhibitor, an egfr inhibitor and optionally a pi3k-alpha inhibitor
EP2976106B1 (en) 2013-03-21 2021-04-14 Array BioPharma Inc. Combination therapy comprising a b-raf inhibitor and a second inhibitor
WO2015145388A2 (en) * 2014-03-27 2015-10-01 Novartis Ag Methods of treating colorectal cancers harboring upstream wnt pathway mutations
EA201790019A1 (ru) * 2014-06-16 2017-06-30 Уорлдуайд Иновейтив Нетуорк Способ выбора персонализированной трехкомпонентной терапии для лечения рака
WO2016193955A1 (en) * 2015-06-04 2016-12-08 Giorgio Stassi Combinations of kinase inhibitors for treating colorectal cancer
CN107921026A (zh) * 2015-08-28 2018-04-17 诺华股份有限公司 药物组合物包含(a)α‑同种型特异性PI3K抑制剂alpelisib(BYL719)和(b)AKT抑制剂,优选MK‑2206,afuresertib或uprosertib及其在治疗/预防癌症中的应用
EP3355886A1 (en) * 2015-08-28 2018-08-08 Novartis AG Pharmaceutical combination comprising the pi3k inhibitor alpelisib and the b-raf inhibitor dabrafenib; the use of such combination in the treatment or prevention of cancer
WO2017066664A1 (en) * 2015-10-16 2017-04-20 Millennium Pharmaceuticals, Inc. Combination therapy including a raf inhibitor for the treatment of colorectal cancer
BR112018074941A2 (pt) 2016-06-03 2019-03-12 Caponigro Giordano combinações farmacêuticas
KR102341660B1 (ko) * 2016-09-19 2021-12-23 노파르티스 아게 Raf 억제제 및 erk 억제제를 포함하는 치료적 조합
CN110494166B (zh) 2017-05-02 2022-11-08 诺华股份有限公司 组合疗法
JOP20200014A1 (ar) * 2017-08-03 2022-10-30 Novartis Ag توليفة علاجية لمثبط كيناز تيروزين egfr من الجيل الثالث ومثبط raf
TWI833819B (zh) 2018-10-05 2024-03-01 美商安尼波那生物公司 用於治療與apj受體活性相關的病狀的化合物及組成物
TWI849043B (zh) * 2019-01-25 2024-07-21 英屬開曼群島商百濟神州有限公司 B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途
WO2020164997A1 (en) * 2019-02-12 2020-08-20 Bayer Aktiengesellschaft Combination of pi3k-inhibitors
BR112021022335A2 (pt) 2019-05-13 2021-12-28 Novartis Ag Formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinopiridin-4-il)-4-metilfenil)-2 (trifluorome-til)isonicotinamida como inibidores raf para o tratamento de câncer
US20250108051A1 (en) * 2022-01-27 2025-04-03 Tohoku University Therapeutic agent for cancer
WO2023230554A1 (en) 2022-05-25 2023-11-30 Pfizer Inc. Combination of a braf inhibitor, an egfr inhibitor, and a pd-1 antagonist for the treatment of braf v600e-mutant, msi-h/dmmr colorectal cancer
TW202421133A (zh) * 2022-09-26 2024-06-01 美商馬布可爾公司 用於治療癌症的b-raf抑制劑和抗egfr抗體之組合
WO2025003956A1 (en) 2023-06-30 2025-01-02 Pfizer Inc. High drug loading formulations of encorafenib

Citations (4)

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WO2010029082A1 (en) * 2008-09-10 2010-03-18 Novartis Ag Organic compounds
WO2011025927A1 (en) * 2009-08-28 2011-03-03 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2011028540A1 (en) * 2009-08-24 2011-03-10 Genentech, Inc. Determining sensitivity of cells to b-raf inhibitor treatment by detecting kras mutation and rtk expression levels
WO2011046894A1 (en) * 2009-10-12 2011-04-21 Glaxosmithkline Llc Combination

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AU4128089A (en) 1988-09-15 1990-03-22 Rorer International (Overseas) Inc. Monoclonal antibodies specific to human epidermal growth factor receptor and therapeutic methods employing same
US6235883B1 (en) 1997-05-05 2001-05-22 Abgenix, Inc. Human monoclonal antibodies to epidermal growth factor receptor
KR101626435B1 (ko) 2007-04-10 2016-06-01 엑셀리시스, 인코포레이티드 Pi3k 알파의 피리도피리미디논 억제제를 이용한 암 치료 방법
US20120045433A1 (en) 2010-08-17 2012-02-23 Kapil Dhingra Combination therapy
AU2011328227B2 (en) * 2010-11-08 2015-04-09 Novartis Ag Use of 2-carboxamide cycloamino urea derivatives in the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members
WO2013070998A1 (en) 2011-11-10 2013-05-16 Memorial Sloan-Kettering Cancer Center TREATMENT OF OVARIAN CANCER WITH 2-AMINO-4H-NAPHTHO[1,2-b]PYRAN-3-CARBONITRILES
BR112014011223A8 (pt) * 2011-11-11 2023-01-31 Novartis Ag Método de tratar uma doença proliferativa
SG11201500321YA (en) * 2012-08-07 2015-04-29 Novartis Ag Pharmaceutical combinations comprising a b-raf inhibitor, an egfr inhibitor and optionally a pi3k-alpha inhibitor

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010029082A1 (en) * 2008-09-10 2010-03-18 Novartis Ag Organic compounds
WO2011028540A1 (en) * 2009-08-24 2011-03-10 Genentech, Inc. Determining sensitivity of cells to b-raf inhibitor treatment by detecting kras mutation and rtk expression levels
WO2011025927A1 (en) * 2009-08-28 2011-03-03 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2011046894A1 (en) * 2009-10-12 2011-04-21 Glaxosmithkline Llc Combination

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HK1211831A1 (zh) 2016-06-03
CA2879548C (en) 2020-07-21
GT201500025A (es) 2017-09-28
ES2717911T3 (es) 2019-06-26
TN2015000027A1 (en) 2016-06-29
MA37829A1 (fr) 2017-01-31
TWI607754B (zh) 2017-12-11
UA115786C2 (uk) 2017-12-26
HK1204976A1 (en) 2015-12-11
PH12015500246B1 (en) 2015-03-30
US9474754B2 (en) 2016-10-25
JP2018109022A (ja) 2018-07-12
KR102112885B1 (ko) 2020-05-19
MY176031A (en) 2020-07-22
EP2882440B1 (en) 2019-02-27
CY1122143T1 (el) 2020-11-25
ECSP15008695A (es) 2019-03-29
AU2013299841A1 (en) 2015-02-12
PL2882440T3 (pl) 2019-07-31
JP6595024B2 (ja) 2019-10-23
LT2882440T (lt) 2019-04-25
IL236934B (en) 2018-11-29
NZ703940A (en) 2018-04-27
KR20150040905A (ko) 2015-04-15
TW201410247A (zh) 2014-03-16
CN104519887A (zh) 2015-04-15
JP2015524472A (ja) 2015-08-24
MX2015001732A (es) 2015-06-03
BR112015002384A8 (pt) 2023-01-31
WO2014025688A1 (en) 2014-02-13
SG11201500321YA (en) 2015-04-29
PE20191655A1 (es) 2019-11-07
TR201904980T4 (tr) 2019-05-21
JP2020019780A (ja) 2020-02-06
PH12015500246A1 (en) 2015-03-30
RS58734B1 (sr) 2019-06-28
HUE042877T2 (hu) 2019-07-29
CL2015000294A1 (es) 2015-05-08
EA028420B1 (ru) 2017-11-30
CO7200273A2 (es) 2015-02-27
PE20150673A1 (es) 2015-05-20
DK2882440T3 (da) 2019-05-06
SI2882440T1 (sl) 2019-05-31
EP2882440A1 (en) 2015-06-17
US20150265616A1 (en) 2015-09-24
AU2013299841B2 (en) 2016-11-24
AU2013299841A8 (en) 2017-01-05
CA2879548A1 (en) 2014-02-13
EP3574904A1 (en) 2019-12-04
BR112015002384A2 (pt) 2017-07-04
HRP20190537T1 (hr) 2019-06-28
JP6974669B2 (ja) 2021-12-01
PT2882440T (pt) 2019-04-23
IN2015DN00450A (enExample) 2015-06-26
AR092045A1 (es) 2015-03-18
AU2013299841B8 (en) 2017-01-05
MX359403B (es) 2018-09-26
JP6342396B2 (ja) 2018-06-13
EA201590332A1 (ru) 2015-06-30
JOP20130236B1 (ar) 2021-08-17

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