CA3132530A1 - Enhanced performance of amorphous solid and solubilized formulations for achieving therapeutic plasma concentrations - Google Patents

Enhanced performance of amorphous solid and solubilized formulations for achieving therapeutic plasma concentrations Download PDF

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Publication number
CA3132530A1
CA3132530A1 CA3132530A CA3132530A CA3132530A1 CA 3132530 A1 CA3132530 A1 CA 3132530A1 CA 3132530 A CA3132530 A CA 3132530A CA 3132530 A CA3132530 A CA 3132530A CA 3132530 A1 CA3132530 A1 CA 3132530A1
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CA
Canada
Prior art keywords
compound
polymer
amorphous
dispersion
formulation
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
CA3132530A
Other languages
English (en)
French (fr)
Inventor
Robert J. GARMISE
Jaquan Kalani Levons
Jay Poorna REDDY
Kevin J. Stefanski
Vrushali M. WAKNIS
Theresa M. ZIEMBA
Ajay Saxena
Srikanth Koravady SRIDHAR
Gajendra Singh CHOWAN
Sharmistha Pal
Shabeerali PATTASSERI
Roopa NARASIMHAMURTHY
Narayan Swamy PANDURANGA
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.)
Bristol Myers Squibb Co
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA3132530A1 publication Critical patent/CA3132530A1/en
Pending legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/18—Bridged 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
CA3132530A 2019-04-11 2020-04-10 Enhanced performance of amorphous solid and solubilized formulations for achieving therapeutic plasma concentrations Pending CA3132530A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962832606P 2019-04-11 2019-04-11
US62/832,606 2019-04-11
PCT/US2020/027677 WO2020210629A1 (en) 2019-04-11 2020-04-10 Enhanced performance of amorphous solid and solubilized formulations for achieving therapeutic plasma concentrations

Publications (1)

Publication Number Publication Date
CA3132530A1 true CA3132530A1 (en) 2020-10-15

Family

ID=70465560

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3132530A Pending CA3132530A1 (en) 2019-04-11 2020-04-10 Enhanced performance of amorphous solid and solubilized formulations for achieving therapeutic plasma concentrations

Country Status (18)

Country Link
US (2) US12509461B2 (https=)
EP (1) EP3953355A1 (https=)
JP (2) JP2022526656A (https=)
KR (1) KR20210151183A (https=)
CN (1) CN113924300A (https=)
AR (1) AR118650A1 (https=)
AU (2) AU2020271103B2 (https=)
BR (1) BR112021020257A2 (https=)
CA (1) CA3132530A1 (https=)
CL (1) CL2021002627A1 (https=)
CO (1) CO2021015054A2 (https=)
EA (1) EA202192753A1 (https=)
IL (1) IL287103A (https=)
MX (2) MX2021012288A (https=)
PE (1) PE20212367A1 (https=)
SG (1) SG11202111131VA (https=)
TW (1) TW202104228A (https=)
WO (1) WO2020210629A1 (https=)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2023010629A (es) 2021-03-09 2023-09-19 Bayer Ag Formas de dosificacion farmaceuticas que comprenden (4s)-24-cloro-4-etil-7?-fluoro-35-metoxi-3?,5-dioxo-14-(trifluoro metil)-3?h-6-aza-3(4,1)-piridina-1(1)-[1,2,3]triazola-2(1,2),7(1) -dibencenaheptafano-74-carboxamida.
TW202327607A (zh) 2021-09-17 2023-07-16 美商必治妥美雅史谷比公司 用於預防及治療血管栓塞病症之米爾維仙(milvexian)
UY40381A (es) 2022-08-01 2024-01-31 Janssen Pharmaceutica Nv Uso de milvexian para el tratamiento o la prevención del accidente cerebrovascular isquémico
CN120712076A (zh) 2023-02-06 2025-09-26 百时美施贵宝公司 米尔维仙药物组合物
WO2025099743A1 (en) * 2023-11-07 2025-05-15 Dr. Reddy’S Laboratories Limited Process for preparation of milvexian and solid-state forms thereof
WO2025126240A1 (en) * 2023-12-12 2025-06-19 Dr. Reddy's Laboratories Limited Pharmaceutical compositions and use thereof
WO2025220042A1 (en) * 2024-04-18 2025-10-23 Dr. Reddy's Laboratories Limited Pharmaceutical compositions comprising asundexian and use thereof
WO2025224678A1 (en) 2024-04-25 2025-10-30 Assia Chemical Industries Ltd. Solid state forms of milvexian and process for preparation thereof

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK569786A (da) 1985-11-27 1987-05-28 Syntex Inc Benzimidazolderivater
ATE364374T1 (de) * 1997-08-11 2007-07-15 Pfizer Prod Inc Feste pharmazeutische dispersionen mit erhöhter bioverfügbarkeit
GEP20053427B (en) * 1999-12-23 2005-01-25 Pfizer Prod Inc Pharmaceutical Compositions Providing Enhanced Drug Concentrations
ES2598178T5 (es) * 2008-10-07 2023-12-26 Kudos Pharm Ltd Formulación farmacéutica 514
WO2010102245A1 (en) 2009-03-05 2010-09-10 Upsher-Smith Laboratories, Inc. Solid dispersion comprising resveratrol
KR101739994B1 (ko) * 2009-04-03 2017-05-25 에프. 호프만-라 로슈 아게 프로판-１-술폰산 ｛３-［５-（４-클로로-페닐）-１Ｈ-피롤로［２，３-ｂ］피리딘-３-카르보닐］-２，４-디플루오로-페닐｝-아미드 조성물 및 그의 용도
CN116987080A (zh) * 2014-01-31 2023-11-03 百时美施贵宝公司 作为因子xia抑制剂的具有杂环p2′基团的大环化合物
PT107568B (pt) 2014-03-31 2018-11-05 Hovione Farm S A Processo de secagem por atomização para a produção de pós com propriedades melhoradas.
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
NO2721243T3 (https=) * 2014-10-01 2018-10-20
JP6203702B2 (ja) 2014-11-18 2017-09-27 信越化学工業株式会社 ヒプロメロース酢酸エステルコハク酸エステルを用いたスプレードライ用溶液及び固体分散体の製造方法
PT3445767T (pt) 2016-04-22 2020-05-13 Astrazeneca Ab Inibidores de mcl-1 macrocíclicos para o tratamento de cancro

Also Published As

Publication number Publication date
AU2020271103A1 (en) 2021-12-02
IL287103A (en) 2021-12-01
US20220144835A1 (en) 2022-05-12
US20260042761A1 (en) 2026-02-12
AU2020271103B2 (en) 2026-01-08
WO2020210629A1 (en) 2020-10-15
AU2025279715A1 (en) 2026-01-15
AR118650A1 (es) 2021-10-20
PE20212367A1 (es) 2021-12-21
TW202104228A (zh) 2021-02-01
MX2025011559A (es) 2025-11-03
SG11202111131VA (en) 2021-11-29
JP2022526656A (ja) 2022-05-25
US12509461B2 (en) 2025-12-30
JP2025131625A (ja) 2025-09-09
EP3953355A1 (en) 2022-02-16
EA202192753A1 (ru) 2022-01-11
CO2021015054A2 (es) 2021-11-19
MX2021012288A (es) 2021-11-12
CL2021002627A1 (es) 2022-05-06
BR112021020257A2 (pt) 2021-12-07
KR20210151183A (ko) 2021-12-13
CN113924300A (zh) 2022-01-11

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