CN107921026A - 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 - Google Patents

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 Download PDF

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Publication number
CN107921026A
CN107921026A CN201680050275.3A CN201680050275A CN107921026A CN 107921026 A CN107921026 A CN 107921026A CN 201680050275 A CN201680050275 A CN 201680050275A CN 107921026 A CN107921026 A CN 107921026A
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China
Prior art keywords
cancer
compound
formula
compounds
pharmaceutically acceptable
Prior art date
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Pending
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CN201680050275.3A
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English (en)
Chinese (zh)
Inventor
G·卡波尼格罗
T·霍恩-斯皮隆
J·莱哈尔
S·希拉瓦特
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Novartis AG
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Novartis AG
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Publication date
Application filed by Novartis AG filed Critical Novartis AG
Publication of CN107921026A publication Critical patent/CN107921026A/zh
Pending legal-status Critical Current

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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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and 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
    • A61K31/435—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
    • A61K31/4375—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 nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201680050275.3A 2015-08-28 2016-08-24 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 Pending CN107921026A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562211014P 2015-08-28 2015-08-28
US62/211,014 2015-08-28
PCT/IB2016/055049 WO2017037578A2 (en) 2015-08-28 2016-08-24 Combination therapy

Publications (1)

Publication Number Publication Date
CN107921026A true CN107921026A (zh) 2018-04-17

Family

ID=56896741

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680050275.3A Pending CN107921026A (zh) 2015-08-28 2016-08-24 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

Country Status (5)

Country Link
US (1) US20180256557A1 (enExample)
EP (1) EP3380097A2 (enExample)
JP (1) JP2018526375A (enExample)
CN (1) CN107921026A (enExample)
WO (1) WO2017037578A2 (enExample)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102149711B (zh) * 2008-09-10 2014-09-10 诺华股份有限公司 有机化合物

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
WO2011146710A1 (en) * 2010-05-21 2011-11-24 Glaxosmithkline Llc Combination
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
KR102182488B1 (ko) * 2013-02-25 2020-11-24 제넨테크, 인크. 약물 내성 akt 돌연변이체의 검출 및 치료를 위한 방법 및 조성물

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102149711B (zh) * 2008-09-10 2014-09-10 诺华股份有限公司 有机化合物

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
SADHNA R. VORA等: "CDK 4/6 Inhibitors Sensitize PIK3CA Mutant Breast Cancer to PI3K Inhibitors", 《CANCER CELL》 *
SAMUEL W. BRADY等: "Enhanced PI3K p110a Signaling Confers Acquired Lapatinib Resistance That Can Be Effectively Reversed by a p110a-Selective PI3K Inhibitor", 《MOL CANCER THER》 *
SARA M.JOHNSON MD等: "Novel Expression Patterns of PI3K/Akt/mTOR Signaling Pathway Components in Colorectal Cancer", 《JOURNAL OF THE AMERICAN COLLEGE OF SURGEONS》 *

Also Published As

Publication number Publication date
US20180256557A1 (en) 2018-09-13
WO2017037578A3 (en) 2017-04-20
WO2017037578A2 (en) 2017-03-09
JP2018526375A (ja) 2018-09-13
EP3380097A2 (en) 2018-10-03

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Application publication date: 20180417