KR20220124736A - Bet 브로모도메인 억제제 및 디펩티딜 펩티다아제 4 억제제의 조합을 이용해 주요 심혈관 이상 반응(mace)을 치료 및/또는 예방하는 방법 - Google Patents

Bet 브로모도메인 억제제 및 디펩티딜 펩티다아제 4 억제제의 조합을 이용해 주요 심혈관 이상 반응(mace)을 치료 및/또는 예방하는 방법 Download PDF

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KR20220124736A
KR20220124736A KR1020227026575A KR20227026575A KR20220124736A KR 20220124736 A KR20220124736 A KR 20220124736A KR 1020227026575 A KR1020227026575 A KR 1020227026575A KR 20227026575 A KR20227026575 A KR 20227026575A KR 20220124736 A KR20220124736 A KR 20220124736A
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inhibitor
dpp
alkyl
alkoxy
hydrogen
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케네쓰 유진 레비오다
크리스토퍼 로스 암스트롱 할리데이
아지즈 나엠 칸
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리스버로직스 코퍼레이션
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    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/40Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • C07D239/91Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • 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)
  • Paper (AREA)
KR1020227026575A 2020-01-08 2021-01-07 Bet 브로모도메인 억제제 및 디펩티딜 펩티다아제 4 억제제의 조합을 이용해 주요 심혈관 이상 반응(mace)을 치료 및/또는 예방하는 방법 Pending KR20220124736A (ko)

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

Publications (1)

Publication Number Publication Date
KR20220124736A true KR20220124736A (ko) 2022-09-14

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KR1020227026575A Pending KR20220124736A (ko) 2020-01-08 2021-01-07 Bet 브로모도메인 억제제 및 디펩티딜 펩티다아제 4 억제제의 조합을 이용해 주요 심혈관 이상 반응(mace)을 치료 및/또는 예방하는 방법

Country Status (9)

Country Link
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=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
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

Family Cites Families (8)

* 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
MX2011009852A (es) * 2009-03-27 2011-09-29 Bristol Myers Squibb Co Metodos para prevenir episodios cardiovasculares adversos mayores con inhibidores de dipeptidil peptidasa iv.
AR083878A1 (es) * 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
HK1219434A1 (zh) * 2013-08-21 2017-04-07 Resverlogix Corp. 用於加速斑块消退的组合物和治疗方法
AU2014310371A1 (en) * 2013-08-21 2016-03-10 Resverlogix Corp. Compositions and therapeutic methods for accelerated plaque regression
WO2016011335A1 (en) * 2014-07-17 2016-01-21 Jerome Schentag Activation of the endogenous ileal brake hormone pathway for organ regeneration and related compositions, methods of treatment, diagnostics, and regulatory systems
US20190031774A1 (en) * 2017-06-09 2019-01-31 Sanofi Biotechnology Methods for treating hyperlipidemia in diabetic patients by administering a pcsk9 inhibitor
CN109824608B (zh) * 2019-03-15 2022-06-21 深圳晶泰科技有限公司 一种Apabetalone晶型及其制备方法

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WO2021140418A1 (en) 2021-07-15
JP7763761B2 (ja) 2025-11-04
CA3164933A1 (en) 2021-07-15
EP4087575A4 (en) 2024-02-28
CN115003306A (zh) 2022-09-02
JP2023509186A (ja) 2023-03-07
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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