TW202019402A - 可口服之修飾釋放藥物劑型 - Google Patents

可口服之修飾釋放藥物劑型 Download PDF

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Publication number
TW202019402A
TW202019402A TW108125542A TW108125542A TW202019402A TW 202019402 A TW202019402 A TW 202019402A TW 108125542 A TW108125542 A TW 108125542A TW 108125542 A TW108125542 A TW 108125542A TW 202019402 A TW202019402 A TW 202019402A
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TW
Taiwan
Prior art keywords
compound
formula
disorders
osmotic
present
Prior art date
Application number
TW108125542A
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English (en)
Chinese (zh)
Inventor
卡門 羅北克
彼得 山諾
安科 斯特勒耶
凱 拉維斯
飛利浦 魯賓包爾
漢寇 希爾莫
達尼亞 格羅斯巴赫
提亞 雅各布斯
布利塔 歐力尼克
茱麗亞 庫塞爾
唐納 比爾瑞
Original Assignee
德商拜耳廠股份有限公司
德商拜耳製藥股份有限公司
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
Priority claimed from US16/043,567 external-priority patent/US10905667B2/en
Application filed by 德商拜耳廠股份有限公司, 德商拜耳製藥股份有限公司 filed Critical 德商拜耳廠股份有限公司
Publication of TW202019402A publication Critical patent/TW202019402A/zh

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0002Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0004Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/2853Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/53Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/55Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW108125542A 2018-07-24 2019-07-19 可口服之修飾釋放藥物劑型 TW202019402A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP18185127 2018-07-24
US16/043,567 US10905667B2 (en) 2018-07-24 2018-07-24 Orally administrable modified-release pharmaceutical dosage form
US16/043,567 2018-07-24
EP18185127.0 2018-07-24

Publications (1)

Publication Number Publication Date
TW202019402A true TW202019402A (zh) 2020-06-01

Family

ID=67314781

Family Applications (1)

Application Number Title Priority Date Filing Date
TW108125542A TW202019402A (zh) 2018-07-24 2019-07-19 可口服之修飾釋放藥物劑型

Country Status (22)

Country Link
EP (1) EP3826627B1 (https=)
JP (1) JP2021532113A (https=)
KR (1) KR20210035235A (https=)
CN (1) CN112469402B (https=)
AU (1) AU2019311234A1 (https=)
BR (1) BR112020026644A2 (https=)
CA (1) CA3107169A1 (https=)
CL (1) CL2021000160A1 (https=)
CO (1) CO2021000450A2 (https=)
CR (1) CR20210043A (https=)
DO (1) DOP2021000015A (https=)
EC (1) ECSP21003707A (https=)
IL (1) IL280083A (https=)
JO (1) JOP20210019A1 (https=)
MA (1) MA53368A (https=)
MX (1) MX2021000904A (https=)
PE (1) PE20210415A1 (https=)
PH (1) PH12021550170A1 (https=)
SG (1) SG11202100369WA (https=)
TW (1) TW202019402A (https=)
UY (1) UY38308A (https=)
WO (1) WO2020020789A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020245342A1 (en) 2019-06-07 2020-12-10 Bayer Aktiengesellschaft The use of sgc activators for the treatment of ophthalmologic diseases
CN112557533A (zh) * 2020-11-29 2021-03-26 北京康立生医药技术开发有限公司 一种恩格列净的分析方法
US20240317696A1 (en) * 2021-05-14 2024-09-26 Medshine Discovery Inc. Alkyl carboxylic acid compounds and application thereof
EP4536205A1 (en) 2022-06-09 2025-04-16 Bayer Aktiengesellschaft Soluble guanylate cyclase activators for use in the treatment of heart failure with preserved ejection fraction in women
CN117982443B (zh) * 2022-10-31 2026-03-06 优辉药业(北京)有限公司 一种达格列净二甲双胍缓释片剂

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US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
GB1478759A (en) 1974-11-18 1977-07-06 Alza Corp Process for forming outlet passageways in pills using a laser
US4063064A (en) 1976-02-23 1977-12-13 Coherent Radiation Apparatus for tracking moving workpiece by a laser beam
US4111202A (en) * 1976-11-22 1978-09-05 Alza Corporation Osmotic system for the controlled and delivery of agent over time
US4327725A (en) 1980-11-25 1982-05-04 Alza Corporation Osmotic device with hydrogel driving member
NZ206600A (en) 1983-05-11 1987-01-23 Alza Corp Osmotic drug delivery device
US4765989A (en) 1983-05-11 1988-08-23 Alza Corporation Osmotic device for administering certain drugs
ES2039287T3 (es) 1987-01-14 1993-09-16 Ciba-Geigy Ag Procedimiento para la obtencion de un sistema terapeutico peroral para productos activos dificilmente solubles.
DE19747261A1 (de) 1997-10-25 1999-04-29 Bayer Ag Osmotisches Arzneimittelfreisetzungssystem
DE19834044A1 (de) 1998-07-29 2000-02-03 Bayer Ag Neue substituierte Pyrazolderivate
DE19834047A1 (de) 1998-07-29 2000-02-03 Bayer Ag Substituierte Pyrazolderivate
ATE433318T1 (de) * 1999-02-10 2009-06-15 Pfizer Prod Inc Osmotisches system zur verabreichung von wirkstoffen, die feste amorphe dispersionen enthalten
AR031176A1 (es) 2000-11-22 2003-09-10 Bayer Ag Nuevos derivados de pirazolpiridina sustituidos con piridina
US20030161882A1 (en) 2002-02-01 2003-08-28 Waterman Kenneth C. Osmotic delivery system
DE10220570A1 (de) 2002-05-08 2003-11-20 Bayer Ag Carbamat-substituierte Pyrazolopyridine
DE102004062475A1 (de) 2004-12-24 2006-07-06 Bayer Healthcare Ag Feste, oral applizierbare pharmazeutische Darreichungsformen mit modifizierter Freisetzung
DE102008059206A1 (de) 2008-11-27 2010-06-10 Bayer Schering Pharma Aktiengesellschaft Pharmazeutische Darreichungsform enthaltend Nifedipin oder Nisoldipin und einen Angiotensin-II Antagonisten und/oder ein Diuretikum
DE102010021637A1 (de) 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
PE20130779A1 (es) 2010-07-09 2013-06-21 Bayer Ip Gmbh Pirimidinas y triazinas condensadas y su uso
DE102010040233A1 (de) 2010-09-03 2012-03-08 Bayer Schering Pharma Aktiengesellschaft Bicyclische Aza-Heterocyclen und ihre Verwendung
DE102010043379A1 (de) 2010-11-04 2012-05-10 Bayer Schering Pharma Aktiengesellschaft Substituierte 6-Fluor-1H-Pyrazolo[4,3-b]pyridine und ihre Verwendung
DE102011007272A1 (de) * 2011-04-13 2012-10-18 Bayer Pharma Aktiengesellschaft Verzweigte 3-Phenylpropionsäure-Derivate und ihre Verwendung
UY34856A (es) * 2012-07-03 2013-12-31 Bayer Pharma AG Formas de presentación farmacéuticas que contienen 5-cloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4- morfolinil)-fenil]-1,3-oxazolidin-5-il}-metil)-2-tiofencarboxamida
WO2019105881A1 (de) 2017-12-01 2019-06-06 Bayer Pharma Aktiengesellschaft Verfahren zur herstellung von (3s)-3-(4-chlor-3-{[(2s,3r)-2-(4-chlorphenyl)-4,4,4-trifluor-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropansäure und dessen kristalline form für die verwendung als pharmazeutischer wirkstoff

Also Published As

Publication number Publication date
JOP20210019A1 (ar) 2021-01-24
CN112469402A (zh) 2021-03-09
UY38308A (es) 2020-02-28
ECSP21003707A (es) 2021-02-26
MX2021000904A (es) 2021-03-31
KR20210035235A (ko) 2021-03-31
BR112020026644A2 (pt) 2021-03-23
CR20210043A (es) 2021-03-09
CN112469402B (zh) 2024-05-14
MA53368A (fr) 2021-06-02
CO2021000450A2 (es) 2021-01-29
PH12021550170A1 (en) 2021-09-13
EP3826627C0 (de) 2023-10-18
CL2021000160A1 (es) 2021-06-04
IL280083A (en) 2021-03-01
SG11202100369WA (en) 2021-02-25
AU2019311234A1 (en) 2021-02-04
WO2020020789A1 (de) 2020-01-30
EP3826627A1 (de) 2021-06-02
PE20210415A1 (es) 2021-03-04
DOP2021000015A (es) 2021-02-15
EP3826627B1 (de) 2023-10-18
CA3107169A1 (en) 2020-01-30
JP2021532113A (ja) 2021-11-25

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