CN103841976A - Akt和mek抑制剂化合物的组合及其使用方法 - Google Patents

Akt和mek抑制剂化合物的组合及其使用方法 Download PDF

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Publication number
CN103841976A
CN103841976A CN201280027030.0A CN201280027030A CN103841976A CN 103841976 A CN103841976 A CN 103841976A CN 201280027030 A CN201280027030 A CN 201280027030A CN 103841976 A CN103841976 A CN 103841976A
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China
Prior art keywords
combination
gdc
compound
cancer
pharmaceutical salts
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CN201280027030.0A
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English (en)
Chinese (zh)
Inventor
B.李
K.林
M.南尼尼
E.彭努斯
D.桑帕思
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Genentech Inc
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Genentech Inc
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Priority to CN201910098566.5A priority Critical patent/CN110433165A/zh
Publication of CN103841976A publication Critical patent/CN103841976A/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
    • A61K31/495—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
    • A61K31/505—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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth 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)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201280027030.0A 2011-04-01 2012-03-30 Akt和mek抑制剂化合物的组合及其使用方法 Pending CN103841976A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201910098566.5A CN110433165A (zh) 2011-04-01 2012-03-30 Akt和mek抑制剂化合物的组合及其使用方法

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161471038P 2011-04-01 2011-04-01
US61/471,038 2011-04-01
PCT/US2012/031716 WO2012135779A1 (en) 2011-04-01 2012-03-30 Combinations of akt and mek inhibitor compounds, and methods of use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201910098566.5A Division CN110433165A (zh) 2011-04-01 2012-03-30 Akt和mek抑制剂化合物的组合及其使用方法

Publications (1)

Publication Number Publication Date
CN103841976A true CN103841976A (zh) 2014-06-04

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Family Applications (2)

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CN201280027030.0A Pending CN103841976A (zh) 2011-04-01 2012-03-30 Akt和mek抑制剂化合物的组合及其使用方法
CN201910098566.5A Pending CN110433165A (zh) 2011-04-01 2012-03-30 Akt和mek抑制剂化合物的组合及其使用方法

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Country Status (16)

Country Link
US (1) US9682082B2 (2)
EP (1) EP2694073B1 (2)
JP (1) JP6147246B2 (2)
KR (1) KR20140022053A (2)
CN (2) CN103841976A (2)
AU (1) AU2012236164A1 (2)
BR (1) BR112013025397A2 (2)
CA (1) CA2831932A1 (2)
ES (1) ES2688809T3 (2)
IL (1) IL228643A0 (2)
MX (1) MX2013011333A (2)
PL (1) PL2694073T3 (2)
RU (1) RU2013148817A (2)
SG (1) SG194047A1 (2)
TR (1) TR201815685T4 (2)
WO (1) WO2012135779A1 (2)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116194095A (zh) * 2020-04-03 2023-05-30 百济神州有限公司 用于治疗癌症的米达替尼与利非芬尼的共同施用

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JP2016502974A (ja) * 2012-12-07 2016-02-01 ザ ジェネラル ホスピタル コーポレイション Ｐｉ３ｋ／ａｋｔ阻害剤化合物とｈｅｒ３／ｅｇｆｒ阻害剤化合物との組み合わせ及び高増殖性疾患の治療におけるその使用
EP2959014B1 (en) * 2013-02-25 2019-11-13 Genentech, Inc. Methods and compositions for detecting and treating drug resistant akt mutant
WO2015035146A2 (en) * 2013-09-05 2015-03-12 Memorial Sloan-Kettering Cancer Center Ddx43 as a biomarker of resistance to mek1/2 inhibitors
TWI719765B (zh) 2018-12-19 2021-02-21 美商建南德克公司 使用包含akt抑制劑、紫杉烷及pd-l1抑制劑之組合療法之乳癌治療
US11066358B1 (en) * 2021-02-17 2021-07-20 Warner-Lambert Company Llc Compositions of essentially pure form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide and uses thereof
US11084780B1 (en) * 2021-02-17 2021-08-10 Springworks Therapeutics, Inc. Crystalline solids of MEK inhibitor N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide and uses thereof
WO2024255830A1 (zh) * 2023-06-14 2024-12-19 南京正大天晴制药有限公司 Akt抑制剂在制备预防或治疗卵巢癌药物中的用途

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CN101605540A (zh) * 2006-12-14 2009-12-16 埃克塞利希斯股份有限公司 使用mek抑制剂的方法
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