CN113164765B - 凝血酶抑制剂、制剂及其用途 - Google Patents

凝血酶抑制剂、制剂及其用途

Info

Publication number
CN113164765B
CN113164765B CN201980059868.XA CN201980059868A CN113164765B CN 113164765 B CN113164765 B CN 113164765B CN 201980059868 A CN201980059868 A CN 201980059868A CN 113164765 B CN113164765 B CN 113164765B
Authority
CN
China
Prior art keywords
tablet
compound
disease
thrombosis
acid
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201980059868.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN113164765A (zh
Inventor
K·M·肖特
M·D·L·A·埃斯绨阿特-马缇内斯
D·B·奇塔
N·S·西里索玛
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.)
Vison International Inc
Original Assignee
Vison International Inc
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 Vison International Inc filed Critical Vison International Inc
Publication of CN113164765A publication Critical patent/CN113164765A/zh
Application granted granted Critical
Publication of CN113164765B publication Critical patent/CN113164765B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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
    • 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
    • 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)
CN201980059868.XA 2018-07-13 2019-07-12 凝血酶抑制剂、制剂及其用途 Active CN113164765B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862697817P 2018-07-13 2018-07-13
US62/697,817 2018-07-13
PCT/US2019/041699 WO2020014669A1 (en) 2018-07-13 2019-07-12 Thrombin inhibitors, formulations, and uses thereof

Publications (2)

Publication Number Publication Date
CN113164765A CN113164765A (zh) 2021-07-23
CN113164765B true CN113164765B (zh) 2026-03-20

Family

ID=67470750

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980059868.XA Active CN113164765B (zh) 2018-07-13 2019-07-12 凝血酶抑制剂、制剂及其用途

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
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
IL280078B2 (en) 2024-04-01
SG11202100247WA (en) 2021-02-25

Similar Documents

Publication Publication Date Title
JP6694458B2 (ja) セリンプロテアーゼ阻害剤としての多置換芳香族化合物
JP2020143112A (ja) セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物
KR102113960B1 (ko) 트롬빈 억제제로서의 다중치환된 방향족 화합물
EP1389194A2 (en) Inhibitors of bace
JP2018506563A (ja) セリンプロテアーゼ阻害剤としての置換ピラゾール化合物
JP2025098029A (ja) トロンビン阻害薬、製剤、及びそれらの使用
US9951025B2 (en) Halogenopyrazoles as inhibitors of thrombin
HK1214142B (en) Multisubstituted aromatic compounds as serine protease inhibitors

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant