CN102958518A - 磷脂酰肌醇3-激酶抑制剂和抗糖尿病化合物的组合 - Google Patents

磷脂酰肌醇3-激酶抑制剂和抗糖尿病化合物的组合 Download PDF

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Publication number
CN102958518A
CN102958518A CN2010800199053A CN201080019905A CN102958518A CN 102958518 A CN102958518 A CN 102958518A CN 2010800199053 A CN2010800199053 A CN 2010800199053A CN 201080019905 A CN201080019905 A CN 201080019905A CN 102958518 A CN102958518 A CN 102958518A
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compound
combination
cancer
metformin
proliferative disease
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Chinese (zh)
Inventor
J·巴塞尔加
S·蒂科西摩
C·加西亚-埃切维里亚
W·哈克尔
S-M·马伊拉
M·鲁西洛
V·塞拉埃利萨尔德
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Novartis AG
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Novartis AG
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles 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
    • A61K31/4353Heterocyclic 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
    • A61K31/435Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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

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  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (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)
CN2010800199053A 2009-05-15 2010-05-12 磷脂酰肌醇3-激酶抑制剂和抗糖尿病化合物的组合 Pending CN102958518A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09160440.5 2009-05-15
EP09160440 2009-05-15
PCT/EP2010/056538 WO2010130779A2 (en) 2009-05-15 2010-05-12 COMBINATION OF A PBOSPBOINOSITKLE 3-KSπASE INHIBITOR AND AN ANTIDIABETIC COMPOUND

Publications (1)

Publication Number Publication Date
CN102958518A true CN102958518A (zh) 2013-03-06

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CN2010800199053A Pending CN102958518A (zh) 2009-05-15 2010-05-12 磷脂酰肌醇3-激酶抑制剂和抗糖尿病化合物的组合

Country Status (11)

Country Link
US (1) US20120059005A1 (https=)
EP (1) EP2429516A2 (https=)
JP (1) JP2012526772A (https=)
KR (1) KR20120096869A (https=)
CN (1) CN102958518A (https=)
AU (1) AU2010247397B2 (https=)
BR (1) BRPI1010979A2 (https=)
CA (1) CA2760179A1 (https=)
MX (1) MX2011012201A (https=)
RU (1) RU2011150619A (https=)
WO (1) WO2010130779A2 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109789210A (zh) * 2016-08-03 2019-05-21 瑞美德生物医药科技有限公司 用于治疗癌症的胰高血糖素受体拮抗剂和pi3k途径抑制剂的组合
CN112533596A (zh) * 2018-07-23 2021-03-19 豪夫迈·罗氏有限公司 用pi3k抑制剂gdc-0077治疗癌症的方法
CN120361228A (zh) * 2025-04-08 2025-07-25 复旦大学附属妇产科医院 一种葡萄糖激酶激活剂与pi3k抑制剂的组合物

Families Citing this family (6)

* Cited by examiner, † Cited by third party
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AR081060A1 (es) 2010-04-15 2012-06-06 Bayer Schering Pharma Ag Procedimiento para preparar 4-{4-[({[4-cloro-3-(trifluorometil)fenil]amino}carbonil)amino]-3-fluorofenoxi}-n-metilpiridin-2-carboxamida
EP2621908A2 (en) * 2010-10-01 2013-08-07 Novartis AG Manufacturing process for pyrimidine derivatives
AU2014250795B2 (en) * 2013-04-12 2019-07-18 Ned Biosystems, Inc. Cancer therapy
CN113194752A (zh) * 2018-06-01 2021-07-30 康奈尔大学 Pi3k相关疾病或病症的组合疗法
EP3863618A1 (en) * 2018-10-08 2021-08-18 F. Hoffmann-La Roche AG Methods of treating cancer with pi3k alpha inhibitors and metformin
BR112022012280A2 (pt) * 2019-12-20 2022-08-30 Recurium Ip Holdings Llc Combinações

Citations (2)

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WO2006122806A2 (en) * 2005-05-20 2006-11-23 Novartis Ag 1,3-dihydro-imidazo [4,5-c] quinolin-2-ones as lipid kinase inhibitors
CN101389622A (zh) * 2006-01-20 2009-03-18 诺瓦提斯公司 用作pi-3激酶抑制剂的嘧啶衍生物

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WO2004066929A2 (en) * 2003-01-24 2004-08-12 Bristol-Myers Squibb Company Cycloalkyl containing anilide ligands for the thyroid receptor
AU2005333515B2 (en) * 2004-07-09 2012-05-10 Arizona Board Of Regents, Acting On Behalf Of The University Of Arizona Wortmannin analogs and methods of using same in combination with chemotherapeutic agents
US7714005B2 (en) * 2004-12-22 2010-05-11 The Ohio State University Research Foundation Small molecule Bcl-xL/Bcl-2 binding inhibitors
TW200824678A (en) * 2006-08-11 2008-06-16 Combinatorx Inc Methods and compositions for the treatment of neurodegenerative disorders
EP2120909A2 (en) * 2006-12-15 2009-11-25 Ordway Research Institute Treatments of therapy-resistant diseases comprising drug combinations
CA2708149A1 (en) * 2007-12-13 2009-06-18 Novartis Ag Combinations of therapeutic agents for treating cancer
WO2009155659A1 (en) * 2008-06-27 2009-12-30 The University Of Queensland Combination therapy
KR20110028651A (ko) * 2008-07-11 2011-03-21 노파르티스 아게 (a) 포스포이노시타이드 3-키나제 억제제 및 (b) ras/raf/mek 경로의 조절제의 조합물

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006122806A2 (en) * 2005-05-20 2006-11-23 Novartis Ag 1,3-dihydro-imidazo [4,5-c] quinolin-2-ones as lipid kinase inhibitors
CN101389622A (zh) * 2006-01-20 2009-03-18 诺瓦提斯公司 用作pi-3激酶抑制剂的嘧啶衍生物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
NATHAN T. IHLE ET AL.: "Peroxisome proliferator-activated receptor ; agonist pioglitazone prevents the hyperglycemia caused by phosphatidylinositol 3-kinase pathway inhibition byPX-866 without affecting antitumor activity", 《MOLECULAR CANCER THERAPEUTICS》 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109789210A (zh) * 2016-08-03 2019-05-21 瑞美德生物医药科技有限公司 用于治疗癌症的胰高血糖素受体拮抗剂和pi3k途径抑制剂的组合
CN112533596A (zh) * 2018-07-23 2021-03-19 豪夫迈·罗氏有限公司 用pi3k抑制剂gdc-0077治疗癌症的方法
CN117281814A (zh) * 2018-07-23 2023-12-26 豪夫迈·罗氏有限公司 用pi3k抑制剂gdc-0077治疗癌症的方法
CN120361228A (zh) * 2025-04-08 2025-07-25 复旦大学附属妇产科医院 一种葡萄糖激酶激活剂与pi3k抑制剂的组合物
CN120361228B (zh) * 2025-04-08 2025-11-21 复旦大学附属妇产科医院 一种葡萄糖激酶激活剂与pi3k抑制剂的组合物

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Publication number Publication date
CA2760179A1 (en) 2010-11-18
RU2011150619A (ru) 2013-06-20
MX2011012201A (es) 2011-12-08
US20120059005A1 (en) 2012-03-08
WO2010130779A2 (en) 2010-11-18
JP2012526772A (ja) 2012-11-01
EP2429516A2 (en) 2012-03-21
KR20120096869A (ko) 2012-08-31
AU2010247397A1 (en) 2011-11-03
WO2010130779A3 (en) 2013-03-28
AU2010247397B2 (en) 2012-07-12
BRPI1010979A2 (pt) 2018-03-06

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Application publication date: 20130306