IL280078B2 - Thrombin inhibitors, formulations, and uses thereof - Google Patents

Thrombin inhibitors, formulations, and uses thereof

Info

Publication number
IL280078B2
IL280078B2 IL280078A IL28007821A IL280078B2 IL 280078 B2 IL280078 B2 IL 280078B2 IL 280078 A IL280078 A IL 280078A IL 28007821 A IL28007821 A IL 28007821A IL 280078 B2 IL280078 B2 IL 280078B2
Authority
IL
Israel
Prior art keywords
compound
methyl
amino
dihydropyridin
pyrazol
Prior art date
Application number
IL280078A
Other languages
English (en)
Hebrew (he)
Other versions
IL280078B1 (en
IL280078A (en
Original Assignee
Verseon Int Corporation
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Verseon Int Corporation filed Critical Verseon Int Corporation
Publication of IL280078A publication Critical patent/IL280078A/en
Publication of IL280078B1 publication Critical patent/IL280078B1/en
Publication of IL280078B2 publication Critical patent/IL280078B2/en

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846—Poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2893—Tablet coating processes
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
IL280078A 2018-07-13 2019-07-12 Thrombin inhibitors, formulations, and uses thereof IL280078B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862697817P 2018-07-13 2018-07-13
PCT/US2019/041699 WO2020014669A1 (en) 2018-07-13 2019-07-12 Thrombin inhibitors, formulations, and uses thereof

Publications (3)

Publication Number Publication Date
IL280078A IL280078A (en) 2021-03-01
IL280078B1 IL280078B1 (en) 2023-12-01
IL280078B2 true IL280078B2 (en) 2024-04-01

Family

ID=67470750

Family Applications (1)

Application Number Title Priority Date Filing Date
IL280078A IL280078B2 (en) 2018-07-13 2019-07-12 Thrombin inhibitors, formulations, and uses thereof

Country Status (13)

Country Link
US (1) US11865110B2 (enExample)
EP (1) EP3820564A1 (enExample)
JP (2) JP2021531338A (enExample)
KR (1) KR20210080347A (enExample)
CN (1) CN113164765B (enExample)
AU (1) AU2019300161B2 (enExample)
BR (1) BR112021000515A2 (enExample)
CA (1) CA3106359A1 (enExample)
IL (1) IL280078B2 (enExample)
MX (1) MX2021000472A (enExample)
SG (1) SG11202100247WA (enExample)
WO (1) WO2020014669A1 (enExample)
ZA (1) ZA202100955B (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116735514B (zh) * 2023-08-11 2023-11-03 昆明理工大学 纳米酶结合液液微萃取快速检测天麻硫熏标志物的方法
WO2025184627A1 (en) * 2024-03-01 2025-09-04 Cadrenal Therapeutics, Inc. Method for preventing coagulation in patients with implanted cardiac devices

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014145986A1 (en) * 2013-03-15 2014-09-18 Verseon, Inc. Multisubstituted aromatic compounds as serine protease inhibitors
WO2016044662A1 (en) * 2014-09-17 2016-03-24 Verseon Corporation Pyrazolyl-substituted pyridone compounds as serine protease inhibitors

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5579843A (en) 1994-08-16 1996-12-03 Loitherstein; Joel S. Resilient spider for well installation
SE9900070D0 (sv) 1999-01-13 1999-01-13 Astra Ab New use
SI21097A (sl) 2001-12-04 2003-06-30 Univerza V Ljubljani Inhibitorji trombina
SE0200198D0 (sv) 2002-01-23 2002-01-23 Astrazeneca Ab New use
AR061996A1 (es) 2006-07-17 2008-08-10 Boehringer Ingelheim Int Indicaciones para los inhibidores directos de la trombina en el campo cardiovascular
EA201100358A1 (ru) 2008-08-19 2011-10-31 Бёрингер Ингельхайм Интернациональ Гмбх Дабигатран для чрескожной хирургической катетеризации сердца
US20110190352A1 (en) 2008-08-19 2011-08-04 Boehringer Ingelheim International Gmbh Use of dabigatranetexilate for treating patients with pulmonary hypertension
WO2010020601A1 (en) 2008-08-19 2010-02-25 Boehringer Ingelheim International Gmbh Dabigatran in tumour therapy

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014145986A1 (en) * 2013-03-15 2014-09-18 Verseon, Inc. Multisubstituted aromatic compounds as serine protease inhibitors
WO2016044662A1 (en) * 2014-09-17 2016-03-24 Verseon Corporation Pyrazolyl-substituted pyridone compounds as serine protease inhibitors

Also Published As

Publication number Publication date
CA3106359A1 (en) 2020-01-16
JP2025098029A (ja) 2025-07-01
US20210315877A1 (en) 2021-10-14
CN113164765B (zh) 2026-03-20
US11865110B2 (en) 2024-01-09
JP2021531338A (ja) 2021-11-18
AU2019300161B2 (en) 2025-05-22
IL280078B1 (en) 2023-12-01
IL280078A (en) 2021-03-01
WO2020014669A1 (en) 2020-01-16
BR112021000515A2 (pt) 2021-04-06
KR20210080347A (ko) 2021-06-30
AU2019300161A1 (en) 2021-02-25
EP3820564A1 (en) 2021-05-19
CN113164765A (zh) 2021-07-23
MX2021000472A (es) 2021-06-23
ZA202100955B (en) 2023-10-25
SG11202100247WA (en) 2021-02-25

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