CN111821306A - Mdm2抑制剂和其组合 - Google Patents

Mdm2抑制剂和其组合 Download PDF

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Publication number
CN111821306A
CN111821306A CN202010783071.9A CN202010783071A CN111821306A CN 111821306 A CN111821306 A CN 111821306A CN 202010783071 A CN202010783071 A CN 202010783071A CN 111821306 A CN111821306 A CN 111821306A
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China
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pharmaceutical combination
inhibitor
cancer
compound
combination
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CN202010783071.9A
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English (en)
Chinese (zh)
Inventor
E·哈利罗维克
G·卡波尼格罗
T·霍恩-斯皮隆
J·莱哈尔
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Novartis AG
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Novartis AG
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Publication of CN111821306A publication Critical patent/CN111821306A/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
    • A61K31/495—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not 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
    • A61K31/495—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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • 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)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (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)
CN202010783071.9A 2015-08-28 2016-08-24 Mdm2抑制剂和其组合 Withdrawn CN111821306A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201562211080P 2015-08-28 2015-08-28
US62/211,080 2015-08-28
US201562243337P 2015-10-19 2015-10-19
US62/243,337 2015-10-19
US201562250574P 2015-11-04 2015-11-04
US62/250,574 2015-11-04
CN201680062336.8A CN108348520A (zh) 2015-08-28 2016-08-24 Mdm2抑制剂和其组合

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201680062336.8A Division CN108348520A (zh) 2015-08-28 2016-08-24 Mdm2抑制剂和其组合

Publications (1)

Publication Number Publication Date
CN111821306A true CN111821306A (zh) 2020-10-27

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CN202010783071.9A Withdrawn CN111821306A (zh) 2015-08-28 2016-08-24 Mdm2抑制剂和其组合
CN201680062336.8A Pending CN108348520A (zh) 2015-08-28 2016-08-24 Mdm2抑制剂和其组合

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Country Status (11)

Country Link
US (3) US20190060309A1 (https=)
EP (2) EP4241850A3 (https=)
JP (2) JP2018528206A (https=)
KR (1) KR20180041677A (https=)
CN (2) CN111821306A (https=)
AU (2) AU2016314082B2 (https=)
CA (1) CA2992221C (https=)
ES (1) ES2962460T3 (https=)
IL (2) IL257015B (https=)
RU (2) RU2740091C2 (https=)
WO (1) WO2017037579A1 (https=)

Cited By (1)

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CN117562907A (zh) * 2023-11-17 2024-02-20 广州医科大学 一种提升抗癌效果的可口服吉非替尼复合物及其制备方法与应用

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TW201613576A (en) 2014-06-26 2016-04-16 Novartis Ag Intermittent dosing of MDM2 inhibitor
US11672801B2 (en) 2016-10-19 2023-06-13 United States Government As Represented By The Department Of Veterans Affairs Compositions and methods for treating cancer
ES2928773T3 (es) 2017-01-17 2022-11-22 Heparegenix Gmbh Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos
WO2018183762A1 (en) * 2017-03-29 2018-10-04 United States Government As Represented By The Department Of Veterans Affairs Methods and compositions for treating cancer
JP6617208B2 (ja) * 2017-03-31 2019-12-11 ノバルティス アーゲー 血液腫瘍におけるｈｄｍ２−ｐ５３相互作用阻害剤の用量およびレジメン
WO2019040511A1 (en) * 2017-08-22 2019-02-28 University Of Maryland Batimore DOUBLE INHIBITORS OF BCL-2 AND HDM2 FAMILIES BY CO-MIMETTISM OF ALPHA BH3 AND P53 PROPELLERS
CN111868039A (zh) * 2017-09-26 2020-10-30 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
EP3694518A1 (en) * 2017-10-12 2020-08-19 Novartis AG Combinations of mdm2 inhibitors with inhibitors of erk for treating cancers
SG11202006304SA (en) * 2017-12-31 2020-07-29 Evergreen Biosciences Compositions for cryopreservation and methods of use thereof
EP3766883B1 (en) 2018-03-12 2022-09-28 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Imidaxopyrolone compound and application thereof
TWI791794B (zh) * 2018-03-20 2023-02-11 瑞士商諾華公司 藥物組合
CA3095699A1 (en) 2018-07-31 2020-02-06 Ascentage Pharma (Suzhou) Co., Ltd. Combination product of bcl-2 inhibitor and chemotherapeutic agent and use thereof in the prevention and/or treatment of diseases
US11554127B2 (en) 2018-07-31 2023-01-17 Ascentage Pharma (Suzhou) Co., Ltd. Synergistic antitumor effect of Bcl-2 inhibitor combined with rituximab and/or bendamustine or Bcl-2 inhibitor combined with CHOP
BR112020018978A2 (pt) * 2018-07-31 2021-03-02 Ascentage Pharma (Suzhou) Co., Ltd. produto de combinação que compreende um inibidor de bcl-2 e um inibidor de mdm2 e uso dos ditos inibidores na prevenção e/ou tratamento de câncer
CN114522167A (zh) 2018-07-31 2022-05-24 苏州亚盛药业有限公司 Bcl-2抑制剂或Bcl-2/Bcl-xL抑制剂与BTK抑制剂的组合产品及其用途
EP3897648B1 (en) 2018-12-20 2023-08-23 Novartis AG Extended low dose regimens for mdm2 inhibitors
US12194024B2 (en) 2019-07-26 2025-01-14 Ascentage Pharma (Suzhou) Co., Ltd. Pharmaceutical composition of MDM2 inhibitor and use thereof for preventing and/or treating disease
CN119097631A (zh) * 2019-12-03 2024-12-10 苏州亚盛药业有限公司 作为bcl-2抑制剂的n-(苯基磺酰基)苯甲酰胺及相关化合物
CA3178927A1 (en) * 2020-05-26 2021-12-02 Hanmi Pharm. Co., Ltd. Belvarafenib for use in cancer treatment
CN115124533A (zh) * 2021-03-26 2022-09-30 浙江海正药业股份有限公司 四环类衍生物、其制备方法和其医药上的用途
JP2024157057A (ja) * 2021-06-29 2024-11-07 国立大学法人 東京大学 バレット食道の治療用組成物

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Cited By (2)

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Publication number Priority date Publication date Assignee Title
CN117562907A (zh) * 2023-11-17 2024-02-20 广州医科大学 一种提升抗癌效果的可口服吉非替尼复合物及其制备方法与应用
CN117562907B (zh) * 2023-11-17 2025-08-22 广州医科大学 一种提升抗癌效果的可口服吉非替尼复合物及其制备方法与应用

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RU2018110770A3 (https=) 2020-01-15
CA2992221C (en) 2023-06-27
RU2018110770A (ru) 2019-09-30
CA2992221A1 (en) 2017-03-09
IL277239A (en) 2020-10-29
IL277239B (en) 2022-04-01
EP3340989A1 (en) 2018-07-04
RU2020142739A (ru) 2021-01-15
RU2740091C2 (ru) 2021-01-11
US20190060309A1 (en) 2019-02-28
EP4241850A3 (en) 2023-11-08
AU2016314082B2 (en) 2019-07-25
ES2962460T3 (es) 2024-03-19
AU2019204938B2 (en) 2020-07-16
EP4241850A2 (en) 2023-09-13
US20230398115A1 (en) 2023-12-14
JP2018528206A (ja) 2018-09-27
WO2017037579A1 (en) 2017-03-09
IL257015B (en) 2022-02-01
KR20180041677A (ko) 2018-04-24
CN108348520A (zh) 2018-07-31
EP3340989B1 (en) 2023-08-16
JP2021042222A (ja) 2021-03-18
RU2020142739A3 (https=) 2021-05-20
AU2016314082A1 (en) 2018-02-08
US20210260059A1 (en) 2021-08-26
IL257015A (en) 2018-03-29
AU2019204938A1 (en) 2019-07-25

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Application publication date: 20201027