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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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)

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CN201680062336.8A Division CN108348520A (zh) 2015-08-28 2016-08-24 Mdm2抑制剂和其组合

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CN111821306A true CN111821306A (zh) 2020-10-27

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CN202010783071.9A Withdrawn CN111821306A (zh) 2015-08-28 2016-08-24 Mdm2抑制剂和其组合

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US (3) US20190060309A1 (enExample)
EP (2) EP4241850A3 (enExample)
JP (2) JP2018528206A (enExample)
KR (1) KR20180041677A (enExample)
CN (2) CN108348520A (enExample)
AU (2) AU2016314082B2 (enExample)
CA (1) CA2992221C (enExample)
ES (1) ES2962460T3 (enExample)
IL (2) IL257015B (enExample)
RU (2) RU2020142739A (enExample)
WO (1) WO2017037579A1 (enExample)

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
WO2018075823A1 (en) 2016-10-19 2018-04-26 United States Government As Represented By The Department Of Veterans Affairs Compositions and methods for treating cancer
JP7300394B2 (ja) 2017-01-17 2023-06-29 ヘパリジェニックス ゲーエムベーハー 肝再生の促進又は肝細胞死の低減もしくは予防のためのプロテインキナーゼ阻害
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
AU2018242612B2 (en) * 2017-03-31 2020-05-21 Novartis Ag Dose and regimen for an HDM2-p53 interaction inhibitor in hematological tumors
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
CN118459413A (zh) * 2017-09-26 2024-08-09 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
CN111655258B (zh) * 2017-12-31 2025-03-21 常青树生物科学公司 用于冷冻保存的组合物和其使用方法
WO2019174576A1 (zh) * 2018-03-12 2019-09-19 罗欣药业(上海)有限公司 咪唑并吡咯酮化合物及其应用
MX2020009614A (es) * 2018-03-20 2020-10-07 Novartis Ag Combinaciones farmaceuticas.
AU2019314624B2 (en) * 2018-07-31 2022-03-03 Ascentage Pharma (Suzhou) Co., Ltd. Combination product of Bcl-2 inhibitor and MDM2 inhibitor and use thereof in the prevention and/or treatment of diseases
CN110772521A (zh) 2018-07-31 2020-02-11 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
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
MX2020009759A (es) 2018-07-31 2020-10-08 Ascentage Pharma Suzhou Co Ltd Efecto antitumoral sinergico de un inhibidor de bcl-2 combinado con rituximab y/o bendamustina o un inhibidor de bcl-2 combinado con chop.
JP2022514280A (ja) * 2018-12-20 2022-02-10 ノバルティス アーゲー Ｍｄｍ２阻害剤のための延長低用量レジメン
EP4003332A4 (en) * 2019-07-26 2023-05-10 Ascentage Pharma (Suzhou) Co., Ltd. PHARMACEUTICAL COMPOSITION OF AN MDM2 INHIBITOR AND ITS USE TO PREVENT AND/OR TREAT DISEASES
WO2021110097A1 (en) * 2019-12-03 2021-06-10 Ascentage Pharma (Suzhou) Co., Ltd. N-(phenylsulfonyl)benzamides and related compounds as bcl-2 inhibitors
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)

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

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Application publication date: 20201027