CN113924300A - 用于达到治疗血浆浓度的增加效能的非晶形固体及经溶解调配物 - Google Patents

用于达到治疗血浆浓度的增加效能的非晶形固体及经溶解调配物 Download PDF

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Publication number
CN113924300A
CN113924300A CN202080041944.7A CN202080041944A CN113924300A CN 113924300 A CN113924300 A CN 113924300A CN 202080041944 A CN202080041944 A CN 202080041944A CN 113924300 A CN113924300 A CN 113924300A
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CN
China
Prior art keywords
compound
amorphous
polymer
dispersion
amorphous form
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Pending
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CN202080041944.7A
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English (en)
Chinese (zh)
Inventor
R·J·加米斯
J·K·莱翁
J·P·雷迪
K·J·斯特凡斯基
V·M·瓦克尼斯
T·M·齐姆巴
A·萨塞纳
S·K·斯里达尔
G·S·乔万
S·帕
S·帕塔塞里
R·纳拉希姆姆希
N·S·宾童龙
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CN113924300A publication Critical patent/CN113924300A/zh
Pending legal-status Critical Current

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    • 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

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  • 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)
CN202080041944.7A 2019-04-11 2020-04-10 用于达到治疗血浆浓度的增加效能的非晶形固体及经溶解调配物 Pending CN113924300A (zh)

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
CN113924300A true CN113924300A (zh) 2022-01-11

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Family Applications (1)

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CN202080041944.7A Pending CN113924300A (zh) 2019-04-11 2020-04-10 用于达到治疗血浆浓度的增加效能的非晶形固体及经溶解调配物

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

Citations (2)

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CN105980384A (zh) * 2014-01-31 2016-09-28 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
CN106795161A (zh) * 2014-10-01 2017-05-31 百时美施贵宝公司 作为因子xia抑制剂的嘧啶酮

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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
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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105980384A (zh) * 2014-01-31 2016-09-28 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
CN106795161A (zh) * 2014-10-01 2017-05-31 百时美施贵宝公司 作为因子xia抑制剂的嘧啶酮

Non-Patent Citations (1)

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GUY VAN DEN MOOTER等: "The use of amorphous solid dispersions: A formulation strategy to overcome poor solubility and dissolution rate", 《DRUG DISCOVERY TODAY:TECHNOLOGIES》, vol. 9, no. 2, pages 79 *

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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
CA3132530A1 (en) 2020-10-15
CL2021002627A1 (es) 2022-05-06
BR112021020257A2 (pt) 2021-12-07
KR20210151183A (ko) 2021-12-13

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