CN103402518A - 包含pi3k抑制剂和mek抑制剂的组合物及其在治疗癌症中的用途 - Google Patents

包含pi3k抑制剂和mek抑制剂的组合物及其在治疗癌症中的用途 Download PDF

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Publication number
CN103402518A
CN103402518A CN2011800671706A CN201180067170A CN103402518A CN 103402518 A CN103402518 A CN 103402518A CN 2011800671706 A CN2011800671706 A CN 2011800671706A CN 201180067170 A CN201180067170 A CN 201180067170A CN 103402518 A CN103402518 A CN 103402518A
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Prior art keywords
compound
cancer
tumor
formula
treatment
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Pending
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CN2011800671706A
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Chinese (zh)
Inventor
L.德巴斯切
C.加西亚-埃希弗里亚
马建国
S.麦克米兰
J.A.M.奥格登
L.文森特
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Merck Patent GmbH
Sanofi Aventis France
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Merck Patent GmbH
Sanofi Aventis France
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45464841&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN103402518(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Patent GmbH, Sanofi Aventis France filed Critical Merck Patent GmbH
Publication of CN103402518A publication Critical patent/CN103402518A/zh
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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
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/495—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN2011800671706A 2010-12-09 2011-12-08 包含pi3k抑制剂和mek抑制剂的组合物及其在治疗癌症中的用途 Pending CN103402518A (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US42146510P 2010-12-09 2010-12-09
US61/421,465 2010-12-09
US201161436258P 2011-01-26 2011-01-26
US61/436,258 2011-01-26
US201161467485P 2011-03-25 2011-03-25
US61/467,485 2011-03-25
FR1159940 2011-11-03
FR1159940 2011-11-03
PCT/US2011/063871 WO2012078832A1 (en) 2010-12-09 2011-12-08 Compositions comprising a pi3k inhibitor and a mek inhibitor and their use for treating cancer

Publications (1)

Publication Number Publication Date
CN103402518A true CN103402518A (zh) 2013-11-20

Family

ID=45464841

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CN2011800671706A Pending CN103402518A (zh) 2010-12-09 2011-12-08 包含pi3k抑制剂和mek抑制剂的组合物及其在治疗癌症中的用途

Country Status (23)

Country Link
US (1) US20140024653A1 (enExample)
EP (1) EP2648729A1 (enExample)
JP (1) JP2013544892A (enExample)
KR (1) KR20140011311A (enExample)
CN (1) CN103402518A (enExample)
AR (1) AR084216A1 (enExample)
AU (1) AU2011338354A1 (enExample)
BR (1) BR112013014198A2 (enExample)
CA (1) CA2820748A1 (enExample)
CL (1) CL2013001643A1 (enExample)
CR (1) CR20130246A (enExample)
DO (1) DOP2013000131A (enExample)
MA (1) MA34815B1 (enExample)
MX (1) MX2013006319A (enExample)
NZ (1) NZ611581A (enExample)
PE (1) PE20140702A1 (enExample)
PH (1) PH12013501163A1 (enExample)
RU (1) RU2013131241A (enExample)
SG (1) SG190368A1 (enExample)
TW (1) TW201306837A (enExample)
UY (1) UY33790A (enExample)
WO (1) WO2012078832A1 (enExample)
ZA (1) ZA201303687B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104334192A (zh) * 2012-04-06 2015-02-04 赛诺菲 使用pi3k抑制剂和mek抑制剂治疗癌症的方法

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150297594A1 (en) * 2012-10-11 2015-10-22 Merck Patent Gmbh Combination of a 6-oxo-1,6-dihydro-pyridazine derivative having anti-cancer activity with a MEK inhibitor
ES2945387T3 (es) * 2014-02-07 2023-06-30 Verastem Inc Procedimientos y composiciones para tratar el crecimiento celular anormal
WO2016014390A1 (en) * 2014-07-25 2016-01-28 Merck Patent Gmbh Compositions and methods for mek inhibitor combination therapy in the treatment of cancer
MA51309A (fr) * 2017-12-22 2021-03-31 Adienne S A Procédé cellulaire quantitatif pour déterminer l'activité biologique d'un ligand anti-cd26
WO2021047783A1 (en) 2019-09-13 2021-03-18 The Institute Of Cancer Research: Royal Cancer Hospital Vs-6063 in combination with ch5126766 for the treatment of cancer
CA3195656A1 (en) * 2020-10-16 2022-04-21 Xuejun Jiang Induction of ferroptosis for cancer therapy
US11873296B2 (en) 2022-06-07 2024-01-16 Verastem, Inc. Solid forms of a dual RAF/MEK inhibitor

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
GEORGIOS GIAMAS ET AL.: "Kinases as targets in the treatment of solid tumors", 《CELLULAR SIGNALLING》 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104334192A (zh) * 2012-04-06 2015-02-04 赛诺菲 使用pi3k抑制剂和mek抑制剂治疗癌症的方法

Also Published As

Publication number Publication date
WO2012078832A1 (en) 2012-06-14
BR112013014198A2 (pt) 2016-09-13
NZ611581A (en) 2015-02-27
AU2011338354A1 (en) 2013-06-27
RU2013131241A (ru) 2015-01-20
US20140024653A1 (en) 2014-01-23
EP2648729A1 (en) 2013-10-16
MX2013006319A (es) 2013-07-03
PE20140702A1 (es) 2014-06-26
CA2820748A1 (en) 2012-06-14
JP2013544892A (ja) 2013-12-19
KR20140011311A (ko) 2014-01-28
DOP2013000131A (es) 2013-11-15
UY33790A (es) 2012-07-31
AR084216A1 (es) 2013-05-02
ZA201303687B (en) 2014-01-29
CL2013001643A1 (es) 2014-03-28
PH12013501163A1 (en) 2013-07-29
SG190368A1 (en) 2013-06-28
MA34815B1 (fr) 2014-01-02
CR20130246A (es) 2013-09-03
TW201306837A (zh) 2013-02-16

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Application publication date: 20131120