CN115003306A - 用bet溴结构域抑制剂和二肽基肽酶4抑制剂的组合治疗和/或预防主要不良心血管事件(mace)的方法 - Google Patents

用bet溴结构域抑制剂和二肽基肽酶4抑制剂的组合治疗和/或预防主要不良心血管事件(mace)的方法 Download PDF

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CN115003306A
CN115003306A CN202180008640.5A CN202180008640A CN115003306A CN 115003306 A CN115003306 A CN 115003306A CN 202180008640 A CN202180008640 A CN 202180008640A CN 115003306 A CN115003306 A CN 115003306A
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dpp
alkyl
alkoxy
inhibitor
hydrogen
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Chinese (zh)
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K·E·莱贝达
C·R·A·哈利迪
A·N·卡恩
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Resverlogix Corp
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Resverlogix Corp
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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/4985—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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • 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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  • Pharmacology & Pharmacy (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Cardiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Cosmetics (AREA)
  • Detergent Compositions (AREA)
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CN202180008640.5A 2020-01-08 2021-01-07 用bet溴结构域抑制剂和二肽基肽酶4抑制剂的组合治疗和/或预防主要不良心血管事件(mace)的方法 Pending CN115003306A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202062958474P 2020-01-08 2020-01-08
US62/958,474 2020-01-08
PCT/IB2021/000006 WO2021140418A1 (en) 2020-01-08 2021-01-07 Methods of treatment and/or prevention of major adverse cardiovascular events (mace) with a combination of a bet bromodomain inhibitor and a dipeptidyl peptidase 4 inhibitor

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Publication Number Publication Date
CN115003306A true CN115003306A (zh) 2022-09-02

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CN202180008640.5A Pending CN115003306A (zh) 2020-01-08 2021-01-07 用bet溴结构域抑制剂和二肽基肽酶4抑制剂的组合治疗和/或预防主要不良心血管事件(mace)的方法

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US (1) US20230241064A1 (https=)
EP (1) EP4087575A4 (https=)
JP (1) JP7763761B2 (https=)
KR (1) KR20220124736A (https=)
CN (1) CN115003306A (https=)
CA (1) CA3164933A1 (https=)
IL (1) IL294344B1 (https=)
TW (1) TWI882058B (https=)
WO (1) WO2021140418A1 (https=)

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Publication number Priority date Publication date Assignee Title
CN114650824A (zh) 2019-11-05 2022-06-21 雷斯韦洛吉克斯公司 用bet溴结构域抑制剂和钠依赖性葡萄糖转运蛋白2抑制剂的组合治疗和/或预防主要不良心血管事件(mace)的方法

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102448456A (zh) * 2009-03-27 2012-05-09 百时美施贵宝公司 用dpp-iv抑制剂预防重度有害心血管事件的方法
CN105473144A (zh) * 2013-08-21 2016-04-06 雷斯韦洛吉克斯公司 用于加速斑块消退的组合物和治疗方法
CN105473145A (zh) * 2013-08-21 2016-04-06 雷斯韦洛吉克斯公司 用于加速斑块消退的组合物和治疗方法
CN106109469A (zh) * 2010-11-15 2016-11-16 贝林格尔·英格海姆国际有限公司 保护血管及保护心脏的抗糖尿病性治疗
CN106687119A (zh) * 2014-07-17 2017-05-17 杰罗米.申塔格 用于器官再生的内源性回肠制动激素途径的激活和相关的组合物、治疗方法、诊断学、和调控系统
US20190031774A1 (en) * 2017-06-09 2019-01-31 Sanofi Biotechnology Methods for treating hyperlipidemia in diabetic patients by administering a pcsk9 inhibitor
CN109824608A (zh) * 2019-03-15 2019-05-31 深圳晶泰科技有限公司 一种Apabetalone晶型及其制备方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2118074E (pt) * 2007-02-01 2014-03-20 Resverlogix Corp Compostos para a prevenção e tratamento de doenças cardiovasculares

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102448456A (zh) * 2009-03-27 2012-05-09 百时美施贵宝公司 用dpp-iv抑制剂预防重度有害心血管事件的方法
CN106109469A (zh) * 2010-11-15 2016-11-16 贝林格尔·英格海姆国际有限公司 保护血管及保护心脏的抗糖尿病性治疗
CN105473144A (zh) * 2013-08-21 2016-04-06 雷斯韦洛吉克斯公司 用于加速斑块消退的组合物和治疗方法
CN105473145A (zh) * 2013-08-21 2016-04-06 雷斯韦洛吉克斯公司 用于加速斑块消退的组合物和治疗方法
CN106687119A (zh) * 2014-07-17 2017-05-17 杰罗米.申塔格 用于器官再生的内源性回肠制动激素途径的激活和相关的组合物、治疗方法、诊断学、和调控系统
US20190031774A1 (en) * 2017-06-09 2019-01-31 Sanofi Biotechnology Methods for treating hyperlipidemia in diabetic patients by administering a pcsk9 inhibitor
CN109824608A (zh) * 2019-03-15 2019-05-31 深圳晶泰科技有限公司 一种Apabetalone晶型及其制备方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KAUSIK K. RAY等: "Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial", 《AMERICAN HEART JOURNAL》, vol. 217, pages 72 - 83, XP085907309, DOI: 10.1016/j.ahj.2019.08.001 *

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WO2021140418A1 (en) 2021-07-15
JP7763761B2 (ja) 2025-11-04
CA3164933A1 (en) 2021-07-15
EP4087575A4 (en) 2024-02-28
JP2023509186A (ja) 2023-03-07
KR20220124736A (ko) 2022-09-14
IL294344A (en) 2022-08-01
US20230241064A1 (en) 2023-08-03
TW202140019A (zh) 2021-11-01
TWI882058B (zh) 2025-05-01
EP4087575A1 (en) 2022-11-16
IL294344B1 (en) 2026-03-01

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