KR101188333B1 - 안정성이 우수하고 경피제로 유용한 톨테로딘 결정성산부가염 - Google Patents

안정성이 우수하고 경피제로 유용한 톨테로딘 결정성산부가염 Download PDF

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Publication number
KR101188333B1
KR101188333B1 KR1020080015336A KR20080015336A KR101188333B1 KR 101188333 B1 KR101188333 B1 KR 101188333B1 KR 1020080015336 A KR1020080015336 A KR 1020080015336A KR 20080015336 A KR20080015336 A KR 20080015336A KR 101188333 B1 KR101188333 B1 KR 101188333B1
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KR
South Korea
Prior art keywords
tolterodine
acid addition
salt
acid
acetone
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Expired - Fee Related
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KR1020080015336A
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English (en)
Korean (ko)
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KR20090090078A (ko
Inventor
김남호
황용연
김용한
최원재
Original Assignee
에스케이케미칼주식회사
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Priority to KR1020080015336A priority Critical patent/KR101188333B1/ko
Application filed by 에스케이케미칼주식회사 filed Critical 에스케이케미칼주식회사
Priority to EP09711813.7A priority patent/EP2247569B1/en
Priority to CN200980111347.0A priority patent/CN101980999B/zh
Priority to JP2010547565A priority patent/JP5543377B2/ja
Priority to PCT/KR2009/000814 priority patent/WO2009104920A1/en
Priority to US12/918,753 priority patent/US8367726B2/en
Priority to ES09711813.7T priority patent/ES2516704T3/es
Publication of KR20090090078A publication Critical patent/KR20090090078A/ko
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/48Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups
    • C07C215/54Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/64Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings 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
    • C07C233/82Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings 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 an acyclic carbon atom
    • C07C233/83Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings 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 an acyclic carbon atom of an acyclic saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C07C309/31Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups by alkyl groups containing at least three carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/33Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems
    • C07C309/34Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems formed by two rings
    • C07C309/35Naphthalene sulfonic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/14Adipic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/03Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring
    • C07C65/05Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring o-Hydroxy carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • C07D207/2732-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C07D207/277Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D207/282-Pyrrolidone-5- carboxylic acids; Functional derivatives thereof, e.g. esters, nitriles

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
KR1020080015336A 2008-02-20 2008-02-20 안정성이 우수하고 경피제로 유용한 톨테로딘 결정성산부가염 Expired - Fee Related KR101188333B1 (ko)

Priority Applications (7)

Application Number Priority Date Filing Date Title
KR1020080015336A KR101188333B1 (ko) 2008-02-20 2008-02-20 안정성이 우수하고 경피제로 유용한 톨테로딘 결정성산부가염
CN200980111347.0A CN101980999B (zh) 2008-02-20 2009-02-20 用于经皮药物递送系统的具有有效稳定性的托特罗定酸式盐
JP2010547565A JP5543377B2 (ja) 2008-02-20 2009-02-20 経皮ドラッグデリバリーシステムとして効果的な安定性を有するトルテロジン酸付加塩
PCT/KR2009/000814 WO2009104920A1 (en) 2008-02-20 2009-02-20 Acid salt of tolterodine having effective stability for transdermal drug delivery system
EP09711813.7A EP2247569B1 (en) 2008-02-20 2009-02-20 Acid salt of tolterodine having effective stability for transdermal drug delivery system
US12/918,753 US8367726B2 (en) 2008-02-20 2009-02-20 Acid salt of tolterodine having effective stability for transdermal drug delivery system
ES09711813.7T ES2516704T3 (es) 2008-02-20 2009-02-20 Sal ácida de tolterodina con una estabilidad eficaz para un sistema de administración transdérmica de fármacos

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1020080015336A KR101188333B1 (ko) 2008-02-20 2008-02-20 안정성이 우수하고 경피제로 유용한 톨테로딘 결정성산부가염

Publications (2)

Publication Number Publication Date
KR20090090078A KR20090090078A (ko) 2009-08-25
KR101188333B1 true KR101188333B1 (ko) 2012-10-09

Family

ID=40985718

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020080015336A Expired - Fee Related KR101188333B1 (ko) 2008-02-20 2008-02-20 안정성이 우수하고 경피제로 유용한 톨테로딘 결정성산부가염

Country Status (7)

Country Link
US (1) US8367726B2 (enExample)
EP (1) EP2247569B1 (enExample)
JP (1) JP5543377B2 (enExample)
KR (1) KR101188333B1 (enExample)
CN (1) CN101980999B (enExample)
ES (1) ES2516704T3 (enExample)
WO (1) WO2009104920A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012051875A (ja) * 2010-08-03 2012-03-15 Hisamitsu Pharmaceut Co Inc 経皮・経粘膜吸収製剤の保存方法及び経皮・経粘膜吸収製剤包装体
EP2799066B1 (en) 2011-12-27 2021-01-20 Teikoku Seiyaku Co., Ltd. Tolterodine-containing adhesive patch
TWI852364B (zh) * 2022-02-22 2024-08-11 大陸商上海雲晟研新生物科技有限公司 卡利拉嗪藥用鹽及其晶型、藥物組合物、製備方法和用途
CN117384073A (zh) * 2022-07-11 2024-01-12 南京毓浠医药技术有限公司 一种维a酸醇胺类复合物及其制备方法和应用
CN118121574A (zh) * 2022-12-02 2024-06-04 南京毓浠医药技术有限公司 一种含维a酸组合物及其制备方法和用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998003067A1 (en) * 1996-07-19 1998-01-29 Gunnar Aberg S(-)-tolterodine in the treatment of urinary and gastrointestinal disorders
US20030199582A1 (en) * 2002-04-23 2003-10-23 Michael Hawley Tolterodine salts

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5382600A (en) * 1988-01-22 1995-01-17 Pharmacia Aktiebolag 3,3-diphenylpropylamines and pharmaceutical compositions thereof
SE9203318D0 (sv) * 1992-11-06 1992-11-06 Kabi Pharmacia Ab Novel 3,3-diphenylpropylamines, their use and preparation
KR20000057548A (ko) 1996-12-13 2000-09-25 알프레드 엘. 미첼슨 광학적 전송물질 및 결합재
SE9802864D0 (sv) * 1998-08-27 1998-08-27 Pharmacia & Upjohn Ab Transdermally administered tolterodine as antimuscarinic agent for the treatment of overactive bladder
PE20020547A1 (es) 2000-10-24 2002-06-12 Upjohn Co Uso de la tolterodina en tratamientos del asma

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998003067A1 (en) * 1996-07-19 1998-01-29 Gunnar Aberg S(-)-tolterodine in the treatment of urinary and gastrointestinal disorders
US20030199582A1 (en) * 2002-04-23 2003-10-23 Michael Hawley Tolterodine salts

Also Published As

Publication number Publication date
US8367726B2 (en) 2013-02-05
JP2011512405A (ja) 2011-04-21
CN101980999B (zh) 2014-11-12
KR20090090078A (ko) 2009-08-25
JP5543377B2 (ja) 2014-07-09
CN101980999A (zh) 2011-02-23
WO2009104920A1 (en) 2009-08-27
US20100331552A1 (en) 2010-12-30
EP2247569A4 (en) 2011-02-23
EP2247569A1 (en) 2010-11-10
EP2247569B1 (en) 2014-08-13
ES2516704T3 (es) 2014-10-31

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