JP2017535561A - 可溶性グアニル酸シクラーゼ活性化剤として有用なトリアゾロ−ピラジニル誘導体 - Google Patents

可溶性グアニル酸シクラーゼ活性化剤として有用なトリアゾロ−ピラジニル誘導体 Download PDF

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Publication number
JP2017535561A
JP2017535561A JP2017526957A JP2017526957A JP2017535561A JP 2017535561 A JP2017535561 A JP 2017535561A JP 2017526957 A JP2017526957 A JP 2017526957A JP 2017526957 A JP2017526957 A JP 2017526957A JP 2017535561 A JP2017535561 A JP 2017535561A
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JP
Japan
Prior art keywords
triazolo
pyrrolo
pyrimidin
pyrazin
methyl
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JP2017526957A
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Japanese (ja)
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JP2017535561A5 (OSRAM
Inventor
ベルジェ，ラファエル
ドン，グイジェン
ラガワン，サブハレカ
ヤン，チーチャン
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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Publication of JP2017535561A publication Critical patent/JP2017535561A/ja
Publication of JP2017535561A5 publication Critical patent/JP2017535561A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/519—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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2017526957A 2014-11-21 2015-11-19 可溶性グアニル酸シクラーゼ活性化剤として有用なトリアゾロ−ピラジニル誘導体 Withdrawn JP2017535561A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462082686P 2014-11-21 2014-11-21
US62/082,686 2014-11-21
US201562144697P 2015-04-08 2015-04-08
US62/144,697 2015-04-08
PCT/US2015/061442 WO2016081668A1 (en) 2014-11-21 2015-11-19 Triazolo-pyrazinyl derivatives useful as soluble guanylate cyclase activators

Publications (2)

Publication Number Publication Date
JP2017535561A true JP2017535561A (ja) 2017-11-30
JP2017535561A5 JP2017535561A5 (OSRAM) 2019-01-10

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JP2017526957A Withdrawn JP2017535561A (ja) 2014-11-21 2015-11-19 可溶性グアニル酸シクラーゼ活性化剤として有用なトリアゾロ−ピラジニル誘導体

Country Status (12)

Country Link
US (1) US9822130B2 (OSRAM)
EP (1) EP3221319B1 (OSRAM)
JP (1) JP2017535561A (OSRAM)
KR (1) KR20170084299A (OSRAM)
CN (1) CN107001389A (OSRAM)
AU (1) AU2015349888A1 (OSRAM)
BR (1) BR112017010551A2 (OSRAM)
CA (1) CA2967965A1 (OSRAM)
MX (1) MX2017006649A (OSRAM)
RU (1) RU2017121278A (OSRAM)
TW (1) TW201625635A (OSRAM)
WO (1) WO2016081668A1 (OSRAM)

Cited By (3)

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KR20200100696A (ko) * 2017-12-19 2020-08-26 사이클리온 테라퓨틱스, 인크. sGC 자극제
JP2023523830A (ja) * 2020-04-30 2023-06-07 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド ピリミジン系三環式化合物及びその使用
JP2024515119A (ja) * 2021-04-20 2024-04-04 ティセント セラピューティクス インコーポレーテッド ｓＧＣ刺激剤

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US9783552B2 (en) 2013-12-11 2017-10-10 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
US9611278B2 (en) 2013-12-11 2017-04-04 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
EP3152214B1 (en) 2014-06-04 2020-01-29 Merck Sharp & Dohme Corp. Imidazo-pyrazine derivatives useful as soluble guanylate cyclase activators
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EP3303342B1 (en) 2015-05-27 2021-03-17 Merck Sharp & Dohme Corp. Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators
US10213429B2 (en) 2015-05-28 2019-02-26 Merck Sharp & Dohme Corp. Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators
WO2017107052A1 (en) 2015-12-22 2017-06-29 Merck Sharp & Dohme Corp. Soluble guanylate cyclase stimulators
WO2017197555A1 (en) * 2016-05-16 2017-11-23 Merck Sharp & Dohme Corp. Fused pyrazine derivatives useful as soluble guanylate cyclase stimulators
EP3458063A4 (en) * 2016-05-18 2020-02-26 Merck Sharp & Dohme Corp. METHOD FOR USE OF TRIAZOLO-PYRAZINYL-SOLUBLE GUANYLATE CYCLASE ACTIVATORS IN FIBROTIC DISEASES
CN105968055B (zh) * 2016-07-26 2018-08-28 中国科学院长春应用化学研究所 一种芳基嘧啶及其衍生物的制备方法
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CN113330030A (zh) 2019-01-17 2021-08-31 拜耳公司 确定受试者是否适于用可溶性鸟苷酸环化酶(sGC)的激动剂治疗的方法
TW202308634A (zh) 2021-04-20 2023-03-01 美商賽克瑞恩醫療公司 使用sGC刺激劑之CNS疾病治療
CN120112293A (zh) 2022-10-18 2025-06-06 帝善多制药公司 使用sGC刺激剂治疗线粒体疾病
CN116768868B (zh) * 2023-08-15 2023-12-08 云南省药物研究所 一种哒嗪酮硫代衍生物及其制备方法和应用

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Cited By (7)

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JP2021508326A (ja) * 2017-12-19 2021-03-04 サイクレリオン・セラピューティクス，インコーポレーテッド ｓＧＣ刺激薬
JP7337067B2 (ja) 2017-12-19 2023-09-01 サイクレリオン・セラピューティクス，インコーポレーテッド ｓＧＣ刺激薬
KR102745228B1 (ko) 2017-12-19 2024-12-19 사이클리온 테라퓨틱스, 인크. sGC 자극제
JP2023523830A (ja) * 2020-04-30 2023-06-07 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド ピリミジン系三環式化合物及びその使用
JP7663605B2 (ja) 2020-04-30 2025-04-16 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド ピリミジン系三環式化合物及びその使用
JP2024515119A (ja) * 2021-04-20 2024-04-04 ティセント セラピューティクス インコーポレーテッド ｓＧＣ刺激剤

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TW201625635A (zh) 2016-07-16
US20170073355A2 (en) 2017-03-16
AU2015349888A1 (en) 2017-05-18
CA2967965A1 (en) 2016-05-26
WO2016081668A1 (en) 2016-05-26
US20160145272A1 (en) 2016-05-26
RU2017121278A (ru) 2018-12-21
EP3221319A1 (en) 2017-09-27
BR112017010551A2 (pt) 2018-02-27
CN107001389A (zh) 2017-08-01
EP3221319B1 (en) 2019-10-30

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