CA2959757A1 - Pyrazole derivatives as sgc stimulators - Google Patents

Pyrazole derivatives as sgc stimulators Download PDF

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Publication number
CA2959757A1
CA2959757A1 CA2959757A CA2959757A CA2959757A1 CA 2959757 A1 CA2959757 A1 CA 2959757A1 CA 2959757 A CA2959757 A CA 2959757A CA 2959757 A CA2959757 A CA 2959757A CA 2959757 A1 CA2959757 A1 CA 2959757A1
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Canada
Prior art keywords
disease
pulmonary
fibrosis
diseases
disorder
Prior art date
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Abandoned
Application number
CA2959757A
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English (en)
French (fr)
Inventor
Timothy Claude Barden
James Edward SHEPPECK
Glen Robert RENNIE
Paul Allan Renhowe
Nicholas Perl
Takashi Nakai
Ara Mermerian
Thomas Wai-Ho Lee
Joon Jung
James Jia
Karthik Iyer
Rajesh R. Iyengar
G-Yoon Jamie Im
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cyclerion Therapeutics Inc
Original Assignee
Ironwood Pharmaceuticals Inc
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Filing date
Publication date
Application filed by Ironwood Pharmaceuticals Inc filed Critical Ironwood Pharmaceuticals Inc
Publication of CA2959757A1 publication Critical patent/CA2959757A1/en
Abandoned legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
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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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Reproductive Health (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2959757A 2014-09-17 2015-09-16 Pyrazole derivatives as sgc stimulators Abandoned CA2959757A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462051557P 2014-09-17 2014-09-17
US62/051,557 2014-09-17
US201562204710P 2015-08-13 2015-08-13
US62/204,710 2015-08-13
PCT/US2015/050468 WO2016044447A1 (en) 2014-09-17 2015-09-16 Pyrazole derivatives as sgc stimulators

Publications (1)

Publication Number Publication Date
CA2959757A1 true CA2959757A1 (en) 2016-03-24

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ID=54200121

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Application Number Title Priority Date Filing Date
CA2959757A Abandoned CA2959757A1 (en) 2014-09-17 2015-09-16 Pyrazole derivatives as sgc stimulators

Country Status (8)

Country Link
US (4) US20170291889A1 (OSRAM)
EP (1) EP3194382B1 (OSRAM)
JP (1) JP6624616B2 (OSRAM)
CN (1) CN107406422B (OSRAM)
AU (2) AU2015317824A1 (OSRAM)
CA (1) CA2959757A1 (OSRAM)
MX (1) MX2017003516A (OSRAM)
WO (1) WO2016044447A1 (OSRAM)

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US10844064B2 (en) * 2014-09-17 2020-11-24 Cyclerion Therapeutics, Inc. sGC stimulators
WO2017106175A2 (en) 2015-12-14 2017-06-22 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF GASTROINTESTINAL SPHINCTER DYSFUNCTION
CN105859726B (zh) * 2016-05-18 2018-07-13 南京富润凯德生物医药有限公司 一种嘧啶并环中选择性脱卤素的方法
CA3029375A1 (en) 2016-07-07 2018-01-11 Ironwood Pharmaceuticals, Inc. Novel processes for preparation of soluble guanylate cyclase stimulators
SG10202100168XA (en) * 2016-07-07 2021-02-25 Cyclerion Therapeutics Inc Novel processes for preparation of soluble guanylate cyclase stimulators
KR102803160B1 (ko) * 2016-07-07 2025-04-30 사이클리온 테라퓨틱스, 인크. sGC 자극제의 고체 형태
CN110022871A (zh) 2016-10-11 2019-07-16 拜耳制药股份公司 包含sGC刺激物和盐皮质激素受体拮抗剂的组合产品
EP3525778A1 (de) 2016-10-11 2019-08-21 Bayer Pharma Aktiengesellschaft Kombination enthaltend sgc aktivatoren und mineralocorticoid-rezeptor-antagonisten
EP3554488A2 (en) 2016-12-13 2019-10-23 Cyclerion Therapeutics, Inc. Use of sgc stimulators for the treatment of esophageal motility disorders
WO2019081456A1 (en) 2017-10-24 2019-05-02 Bayer Aktiengesellschaft USE OF SGC ACTIVATORS AND STIMULATORS COMPRISING A BETA2 SUBUNIT
EP3498298A1 (en) 2017-12-15 2019-06-19 Bayer AG The use of sgc stimulators and sgc activators alone or in combination with pde5 inhibitors for the treatment of bone disorders including osteogenesis imperfecta (oi)
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
EP3737679B1 (en) * 2018-01-10 2023-09-06 Cyclerion Therapeutics, Inc. Novel processes and intermediates for the preparation of soluble guanylate cyclase stimulators
WO2019161534A1 (en) * 2018-02-22 2019-08-29 Ironwood Pharmaceuticals, Inc. Novel processes and intermediates for preparation of soluble guanylate cyclase stimulators
EP3787610A1 (en) 2018-04-30 2021-03-10 Bayer Aktiengesellschaft The use of sgc activators and sgc stimulators for the treatment of cognitive impairment
CN112384213A (zh) 2018-05-15 2021-02-19 拜耳公司 用于治疗与神经纤维敏化有关的疾病的1,3-噻唑-2-基取代的苯甲酰胺
US11508483B2 (en) 2018-05-30 2022-11-22 Adverio Pharma Gmbh Method of identifying a subgroup of patients suffering from dcSSc which benefits from a treatment with sGC stimulators and sGC activators in a higher degree than a control group
CA3103676A1 (en) 2018-07-11 2020-01-16 Cyclerion Therapeutics, Inc. Use of sgc stimulators for the treatment of mitochonrial disorders
US20220128561A1 (en) 2019-01-17 2022-04-28 Bayer Aktiengesellschaft Methods to determine whether a subject is suitable of being treated with an agonist of soluble gyanylyl cyclase (sgc)
CN110498740A (zh) * 2019-09-18 2019-11-26 重庆医药高等专科学校 一种生产3-羟基丙酸的方法
CN110577467A (zh) * 2019-09-18 2019-12-17 重庆医药高等专科学校 一种3-羟基丙酸的合成方法
JP7487953B2 (ja) * 2019-12-18 2024-05-21 株式会社 バイオラジカル研究所 血管拡張剤およびその用途
CN112007027B (zh) * 2020-09-14 2022-07-15 长春金赛药业有限责任公司 含酯基芳香丙酰胺类化合物及其代谢产物在制备治疗心衰药物中的应用
CN112169717B (zh) * 2020-09-30 2022-06-03 深圳大学 一种微胶囊化氯化血红素及其制备方法与应用
WO2022093722A1 (en) * 2020-10-27 2022-05-05 Pts Consulting, Llc A liquid injectable composition of donepezil
WO2023009710A1 (en) * 2021-07-28 2023-02-02 Cyclerion Therapeutics, Inc. Treatment of hfpef in post-menopausal women with an sgc stimulator
WO2025106494A1 (en) * 2023-11-15 2025-05-22 Yanping Kong Compositions and methods for treating erectile dysfunction and male hypogonadism
WO2025189097A1 (en) * 2024-03-07 2025-09-12 Yale University Artificial intelligence-guided screening of under-recognized cardiomyopathies adapted for point-of-care cardiac ultrasound
DE202024103267U1 (de) 2024-06-18 2024-07-09 Ashutosh Aggarwal Ein System zur Herstellung einer antihypertensiven Formulierung mit verlängerter Freisetzung
CN119185590B (zh) * 2024-11-28 2025-02-25 华润双鹤利民药业(济南)有限公司 羟丙基-β-环糊精在制备维立西呱固体制剂中的应用、固体制剂及制备方法
CN119909007B (zh) * 2025-04-02 2025-06-03 四川大学 一种具有氧化还原活性和电活性的可注射水凝胶及其制备方法与应用

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US20170291889A1 (en) 2017-10-12
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EP3194382B1 (en) 2021-09-08
JP2017528494A (ja) 2017-09-28
US20190031641A1 (en) 2019-01-31
US20210221793A1 (en) 2021-07-22
MX2017003516A (es) 2017-07-28
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EP3194382A1 (en) 2017-07-26
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