CN101980999B - 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 - Google Patents

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 Download PDF

Info

Publication number
CN101980999B
CN101980999B CN200980111347.0A CN200980111347A CN101980999B CN 101980999 B CN101980999 B CN 101980999B CN 200980111347 A CN200980111347 A CN 200980111347A CN 101980999 B CN101980999 B CN 101980999B
Authority
CN
China
Prior art keywords
tolterodine
acid
acetone
room temperature
acid salt
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.)
Expired - Fee Related
Application number
CN200980111347.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN101980999A (zh
Inventor
黄用渊
金南镐
崔源宰
金容汉
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.)
SK Chemicals Co Ltd
Original Assignee
SK Chemicals Co Ltd
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 SK Chemicals Co Ltd filed Critical SK Chemicals Co Ltd
Publication of CN101980999A publication Critical patent/CN101980999A/zh
Application granted granted Critical
Publication of CN101980999B publication Critical patent/CN101980999B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds 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
    • C07C215/48—Compounds 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
    • C07C215/54—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds 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
    • C07C215/64—Compounds 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81—Carboxylic 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
    • C07C233/82—Carboxylic 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
    • C07C233/83—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic 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
    • C07C309/31—Sulfonic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/33—Sulfonic 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
    • C07C309/34—Sulfonic 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
    • C07C309/35—Naphthalene sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/14—Adipic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds 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
    • C07C65/01—Compounds 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
    • C07C65/03—Compounds 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
    • C07C65/05—Compounds 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/18—Heterocyclic 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
    • C07D207/22—Heterocyclic 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-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
    • C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D207/28—2-Pyrrolidone-5- carboxylic acids; Functional derivatives thereof, e.g. esters, nitriles

Landscapes

  • 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)
CN200980111347.0A 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 Expired - Fee Related CN101980999B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
KR10-2008-0015336 2008-02-20
KR1020080015336A KR101188333B1 (ko) 2008-02-20 2008-02-20 안정성이 우수하고 경피제로 유용한 톨테로딘 결정성산부가염
PCT/KR2009/000814 WO2009104920A1 (en) 2008-02-20 2009-02-20 Acid salt of tolterodine having effective stability for transdermal drug delivery system

Publications (2)

Publication Number Publication Date
CN101980999A CN101980999A (zh) 2011-02-23
CN101980999B true CN101980999B (zh) 2014-11-12

Family

ID=40985718

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980111347.0A Expired - Fee Related 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

Country Status (7)

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

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
CA2868334C (en) 2011-12-27 2020-03-10 Teikoku Seiyaku Co., Ltd. Tolterodine-containing adhesive patch
WO2023160583A1 (zh) * 2022-02-22 2023-08-31 上海云晟研新生物科技有限公司 卡利拉嗪药用盐及其晶型、药物组合物、制备方法和用途
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1238768A (zh) * 1996-12-31 1999-12-15 法玛西雅厄普约翰美国公司 制备托特瑞定的方法
WO2000012070A1 (en) * 1998-08-27 2000-03-09 Pharmacia & Upjohn Ab Transdermally administered tolterodine as anti-muscarinic agent for the treatment of overactive bladder
CN1646110A (zh) * 2002-04-23 2005-07-27 法玛西亚普强责任有限公司 托特罗定的盐

Family Cites Families (4)

* 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
WO1998003067A1 (en) * 1996-07-19 1998-01-29 Gunnar Aberg S(-)-tolterodine in the treatment of urinary and gastrointestinal disorders
PE20020547A1 (es) 2000-10-24 2002-06-12 Upjohn Co Uso de la tolterodina en tratamientos del asma

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1238768A (zh) * 1996-12-31 1999-12-15 法玛西雅厄普约翰美国公司 制备托特瑞定的方法
WO2000012070A1 (en) * 1998-08-27 2000-03-09 Pharmacia & Upjohn Ab Transdermally administered tolterodine as anti-muscarinic agent for the treatment of overactive bladder
CN1646110A (zh) * 2002-04-23 2005-07-27 法玛西亚普强责任有限公司 托特罗定的盐

Also Published As

Publication number Publication date
WO2009104920A1 (en) 2009-08-27
KR20090090078A (ko) 2009-08-25
JP5543377B2 (ja) 2014-07-09
CN101980999A (zh) 2011-02-23
EP2247569B1 (en) 2014-08-13
US20100331552A1 (en) 2010-12-30
ES2516704T3 (es) 2014-10-31
US8367726B2 (en) 2013-02-05
KR101188333B1 (ko) 2012-10-09
JP2011512405A (ja) 2011-04-21
EP2247569A4 (en) 2011-02-23
EP2247569A1 (en) 2010-11-10

Similar Documents

Publication Publication Date Title
KR101779214B1 (ko) １―［２―（２，４―디메틸페닐술파닐）페닐］피페라진 염의 액체 제형
CN101980999B (zh) 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
US20260116853A1 (en) New n,n-dimethyltryptamine salts and crystalline salt forms
CN101528211A (zh) 眼用经皮吸收型制剂
JPH09507219A (ja) α−２−アドレノセプター作動剤として有用な７−（２−イミダゾリニルアミノ）キノリン化合物
NZ550809A (en) Phenoxyalkycarboxylic acid derivatives in the treatment of inflammatory diseases
CA2804797C (en) Therapeutic compositions for diabetic symmetrical polyneuropathy and/or tactile allodynia
CN101712658A (zh) 1-丁基-2-羟基芳烷哌嗪衍生物及作为抗抑郁剂应用
CN110327336A (zh) 昔萘酸甲哌卡因及其长效缓释制剂
TWI886312B (zh) 磷脂肌醇3-激酶抑制劑的調配物
SK69699A3 (en) 2-imidazolinylaminoindazole compounds useful as alpha-2 adrenoceptor agonists
CN1107333A (zh) 那布扶林镇痛剂的长效前体药物及其制备方法
KR20150100902A (ko) 옥시부티닌의 투여를 위한 방법 및 조성물
JP2012532096A (ja) 保管安定性が向上したトルテロジンを含有する経皮投与組成物
CN113440483B (zh) 一种犬用盐酸特比萘芬喷剂及其制备方法
WO2024125645A1 (zh) 一种κ阿片受体激动剂药物组合物及其制备方法和用途
WO2025077888A1 (zh) 一种适合外用的化合物及药物组合物
US20200276146A1 (en) Methods for the treatment of sialorrhea
KR20110094858A (ko) 피부 자극이 감소한 톨테로딘의 경피 투여용 조성물
CN1161651A (zh) 透皮给药制剂
HK1168553A (en) Liquid formulations of salts of 1-[2-(2,4-dimethylphenylsulfanyl)pheny]piperazine
JPWO2000029021A1 (ja) 脳機能賦活薬を含有する経皮適応製剤

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20141112

Termination date: 20150220

EXPY Termination of patent right or utility model