CA3106359A1 - Thrombin inhibitors, formulations, and uses thereof - Google Patents

Thrombin inhibitors, formulations, and uses thereof Download PDF

Info

Publication number
CA3106359A1
CA3106359A1 CA3106359A CA3106359A CA3106359A1 CA 3106359 A1 CA3106359 A1 CA 3106359A1 CA 3106359 A CA3106359 A CA 3106359A CA 3106359 A CA3106359 A CA 3106359A CA 3106359 A1 CA3106359 A1 CA 3106359A1
Authority
CA
Canada
Prior art keywords
compound
methyl
amino
tablet
pyrazol
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.)
Pending
Application number
CA3106359A
Other languages
English (en)
French (fr)
Inventor
Kevin Michael Short
Maria De Los Angeles Estiarte-Martinez
David Ben Kita
Nilantha Sudath Sirisoma
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.)
Verseon International Corp
Original Assignee
Verseon International Corp
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 International Corp filed Critical Verseon International Corp
Publication of CA3106359A1 publication Critical patent/CA3106359A1/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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)
CA3106359A 2018-07-13 2019-07-12 Thrombin inhibitors, formulations, and uses thereof Pending CA3106359A1 (en)

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 (1)

Publication Number Publication Date
CA3106359A1 true CA3106359A1 (en) 2020-01-16

Family

ID=67470750

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3106359A Pending CA3106359A1 (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

Family Cites Families (10)

* 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
WO2014145986A1 (en) * 2013-03-15 2014-09-18 Verseon, Inc. Multisubstituted aromatic compounds as serine protease inhibitors
KR20170048410A (ko) * 2014-09-17 2017-05-08 베르선 코포레이션 세린 프로테아제 저해제로서의 피라졸릴-치환된 피리돈 화합물

Also Published As

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

Similar Documents

Publication Publication Date Title
AU2017225000B2 (en) Multisubstituted aromatic compounds as serine protease inhibitors
KR102269492B1 (ko) 낭포성 섬유증 막관통 전도성 조절인자의 조절제, 약제학적 조성물, 치료 방법, 및 상기 조절제를 제조하는 방법
JP6236445B2 (ja) 組織トランスグルタミナーゼ阻害剤としてのピリジノン誘導体
EP3788039B1 (en) Factor xiia inhibitors
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
JP2025098029A (ja) トロンビン阻害薬、製剤、及びそれらの使用
KR20130053404A (ko) 트롬빈 억제제로서의 다중치환된 방향족 화합물
KR20190026904A (ko) 비시클릭 헤테로아릴 치환된 화합물
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
KR20050100655A (ko) 티에노〔2,3-ｃ〕피리딘 유도체를 함유하는 약제학적조성물 및 그의 용도
FR2974576A1 (fr) Derives de n-[(1h-pyrazol-1-yl)aryl]-1h-indole ou 1h- indazole-3-carboxamide, leur preparation et leurs applications en therapeutique
EP1369419B1 (en) N-phenylarylsulfonamide compound, drug containing the compound as active ingredient, intermediate for the compound, and processes for producing the same
KR20190026905A (ko) 모노시클릭 헤테로아릴 치환된 화합물
JP2009501187A (ja) 新規なヘテロアリール縮合環式アミン
WO2007121662A1 (en) Diphenyl urea derivatives as kinase inhibitors, compositions and uses thereof
CN101486701B (zh) 色满酮类化合物及其类似物和医药用途
CA3203896A1 (en) Plasmin inhibitor, and preparation method therefor and application thereof
EP4011880A1 (en) Jak kinase inhibitor and use thereof
TW202412778A (zh) 一種脯氨醯羥化酶抑制劑及其用途
CA2889538A1 (en) 1h-indole-3-carboxamide derivatives, and use thereof as p2y12 antagonists
CN110194769A (zh) 一类hdac、cdk双靶点抑制剂及其制备方法与应用
CN102924442B (zh) 含有噻唑环的色满类化合物及其类似物和医药用途
CN104684559A (zh) 针对Uba6的吲哚取代的吡咯并嘧啶基抑制剂
TW202304932A (zh) Abhd6拮抗劑

Legal Events

Date Code Title Description
D11 Substantive examination requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D11-D117 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST FOR EXAMINATION RECEIVED

Effective date: 20240711

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P11-P101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - VOLUNTARY AMENDMENT

Effective date: 20240711

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20241119

D00 Search and/or examination requested or commenced

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D00-D118 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST FOR EXAMINATION REQUIREMENTS DETERMINED COMPLIANT

Effective date: 20241120

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20241120

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20241120

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20241120

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20250411

D11 Substantive examination requested

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D11-D155 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: ALL REQUIREMENTS FOR EXAMINATION DETERMINED COMPLIANT

Effective date: 20250429

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 6TH ANNIV.) - STANDARD

Year of fee payment: 6

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250707

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20250707

D15 Examination report completed

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D15-D126 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S REPORT

Effective date: 20250812

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - RESPONSE TO EXAMINER'S REQUISITION

Effective date: 20251210

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20260119

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20260119

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20260119

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - VOLUNTARY AMENDMENT

Effective date: 20260120