JPS6452742A - Omega-quaternary ammonium alkyl ester and thioester of acidic non-steroidal antiinflammatory - Google Patents

Omega-quaternary ammonium alkyl ester and thioester of acidic non-steroidal antiinflammatory

Info

Publication number
JPS6452742A
JPS6452742A JP63101531A JP10153188A JPS6452742A JP S6452742 A JPS6452742 A JP S6452742A JP 63101531 A JP63101531 A JP 63101531A JP 10153188 A JP10153188 A JP 10153188A JP S6452742 A JPS6452742 A JP S6452742A
Authority
JP
Japan
Prior art keywords
thioester
omega
quaternary ammonium
alkyl ester
steroidal antiinflammatory
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
JP63101531A
Other languages
English (en)
Inventor
Shii Benutsutei Maikuru
Emu Yangu Jiyon
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.)
Syntex Pharmaceuticals International Ltd
Original Assignee
Syntex Pharmaceuticals International 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 Syntex Pharmaceuticals International Ltd filed Critical Syntex Pharmaceuticals International Ltd
Publication of JPS6452742A publication Critical patent/JPS6452742A/ja
Pending legal-status Critical Current

Links

Classifications

    • 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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/337—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/26—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an acyl radical attached to the ring nitrogen atom
    • C07D209/28—1-(4-Chlorobenzoyl)-2-methyl-indolyl-3-acetic acid, substituted in position 5 by an oxygen or nitrogen atom; Esters thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D263/57—Aryl or substituted aryl radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP63101531A 1987-04-27 1988-04-26 Omega-quaternary ammonium alkyl ester and thioester of acidic non-steroidal antiinflammatory Pending JPS6452742A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US4307287A 1987-04-27 1987-04-27

Publications (1)

Publication Number Publication Date
JPS6452742A true JPS6452742A (en) 1989-02-28

Family

ID=21925341

Family Applications (1)

Application Number Title Priority Date Filing Date
JP63101531A Pending JPS6452742A (en) 1987-04-27 1988-04-26 Omega-quaternary ammonium alkyl ester and thioester of acidic non-steroidal antiinflammatory

Country Status (4)

Country Link
EP (1) EP0289262A3 (ja)
JP (1) JPS6452742A (ja)
AU (1) AU1508988A (ja)
ZA (1) ZA882957B (ja)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009543857A (ja) * 2006-07-18 2009-12-10 テックフィールズ バイオケム カンパニー リミテッド イブプロフェンの正荷電水溶性プロドラッグ
JP2009544685A (ja) * 2006-07-25 2009-12-17 テックフィールズ バイオケム カンパニー リミテッド 非常に速い皮膚透過率を有するジクロフェナクの正荷電水溶性プロドラッグ
JP2010500989A (ja) * 2006-08-15 2010-01-14 テックフィールズ バイオケム カンパニー リミテッド 非常に速い皮膚透過率を有するアリール−及びヘテロアリールプロピオン酸の正荷電水溶性プロドラッグ
JP2010529101A (ja) * 2007-06-04 2010-08-26 テックフィールズ インコーポレイテッド 非常に速い皮膚及び膜浸透速度を有するｎｓａｉａプロドラッグ及びその新規医薬使用
JP2013014631A (ja) * 2012-10-23 2013-01-24 Techfields Biochem Co Ltd 非常に速い皮膚透過率を有するアリール−及びヘテロアリールプロピオン酸の正荷電水溶性プロドラッグ
JP2013224292A (ja) * 2012-04-20 2013-10-31 Rohm & Haas Co ジベンジルアミン疎水性物質
JP2014043450A (ja) * 2013-10-08 2014-03-13 Techfields Biochem Co Ltd 非常に速い皮膚透過率を有するアリール−及びヘテロアリールプロピオン酸の正荷電水溶性プロドラッグ
JP2016130241A (ja) * 2016-02-05 2016-07-21 テックフィールズ バイオケム カンパニー リミテッド 非常に速い皮膚透過率を有するアリール−及びヘテロアリールプロピオン酸の正荷電水溶性プロドラッグ

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JPH0662521B2 (ja) * 1988-02-24 1994-08-17 日東紡績株式会社 新規コリン誘導体及びそれを用いた血清コリンエステラーゼ活性測定法
IL89848A (en) * 1988-04-07 1997-08-14 Sepracor Chiral ester derivatives
EP0647133A4 (en) * 1992-06-12 1997-10-29 Affymax Tech Nv COMPOSITIONS AND METHODS FOR IMPROVED DRUG DELIVERY.
DE4300697C1 (de) * 1993-01-13 1994-05-19 Roemmers Sa Keterolac-Derivat mit wesentlich geringerer gastrointestinaler Reizung und Ulzeration
US7151100B1 (en) 1999-07-23 2006-12-19 The Regents Of The University Of California Indole compounds useful for the treatment of cancer
US7361680B2 (en) 1999-07-23 2008-04-22 The Regents Of The University Of California Indole compounds useful for the treatment of cancer
US6545034B1 (en) 1999-07-23 2003-04-08 The Regents Of The University Of California Use of etodolac for the treatment of chronic lymphocytic leukemia
US7105560B1 (en) 1999-07-23 2006-09-12 The Regents Of The University Of California Use of etodolac in the treatment of multiple myeloma
US7129262B2 (en) 1999-07-23 2006-10-31 The Regents Of The University Of California Indole compounds useful for the treatment of cancer
AU8322401A (en) * 2000-08-09 2002-02-18 Univ California Indole compounds useful for the treatment of cancer
US7601846B2 (en) 2001-06-26 2009-10-13 The Regents Of The University Of California Compounds having activity as inhibitors of apoptosis
US7211599B2 (en) 2002-09-19 2007-05-01 The Regents Of The University Of California Use of etodolac to treat hyperplasia
US20090238763A1 (en) 2006-07-09 2009-09-24 Chongxi Yu High penetration compositions and uses thereof
US20090221703A1 (en) 2006-07-09 2009-09-03 Chongxi Yu High penetration composition and uses thereof
AU2013231152B2 (en) * 2006-07-18 2016-06-09 Techfields Biochem Co. Ltd Positively charged water-soluble pro-drugs of ibuprofen
CN104610077B (zh) * 2006-07-27 2020-04-14 于崇曦 具有快速皮肤穿透速度的带正电荷的水溶性酮洛芬及相关化合物的前药
CN104622858B (zh) * 2006-07-27 2019-08-30 于崇曦 具有快速皮肤穿透速度的带正电荷的水溶性酮洛芬及相关化合物的前药
CN108250090B (zh) * 2006-07-27 2021-08-20 于崇曦 具有快速皮肤穿透速度的带正电荷的水溶性酮洛芬及相关化合物的前药
CN103705496B (zh) * 2006-08-15 2017-03-01 于崇曦 具有快速皮肤穿透速度的带正电荷的水溶性的芳基和杂芳基丙酸类前药
AU2013206218B2 (en) * 2006-08-15 2016-06-30 Techfields Biochem Co. Ltd Positively charged water-soluble prodrugs of aryl- and heteroarylpropionic acids with very fast skin penetration rate
CN104706630B (zh) * 2006-09-03 2020-01-10 于崇曦 具有快速皮肤穿透速度的带正电荷的水溶性的芳基邻氨基苯甲酸的前药
EP2084132B1 (en) * 2006-09-03 2018-08-08 Techfields Biochem Co. Ltd Positively charged water-soluble prodrugs of n-arylanthranilic acids with very fast skin penetration rate
CN105669531B (zh) * 2007-06-04 2019-05-07 于崇曦 具有快速皮肤和生物膜穿透速度的非甾体抗炎药的前药及其新的医药用途
US11731991B2 (en) 2008-11-03 2023-08-22 Lehigh University Augmenting moieties for anti-inflammatory compounds
WO2010051044A1 (en) 2008-11-03 2010-05-06 University Of Medicine And Dentistry Unique dual-action therapeutics
US20170044096A1 (en) 2013-03-15 2017-02-16 Rutgers, The State University Of New Jersey Augmenting Moieties for Anti-Inflammatory Compounds
KR101946297B1 (ko) 2008-12-04 2019-02-11 충시 위 고투과력을 가진 조성물 및 이의 적용
CN101434567B (zh) * 2008-12-19 2012-10-24 李扬 一种二乙氨基乙硫醇的制备方法
AU2013262320B2 (en) 2012-01-18 2018-02-22 Techfields Pharma Co., Ltd. High penetration prodrug compositions and pharmaceutical composition thereof for treatment of pulmonary conditions
CN104876848B (zh) * 2015-05-15 2017-05-17 南开大学 一种1‑酰基‑3‑吲哚硫酯化合物及其制备方法

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2390555A (en) * 1943-08-03 1945-12-11 Poythress William P & Co Antispasmodic agents
FR1052419A (fr) * 1951-03-17 1954-01-25 Sterling Drug Inc Procédé perfectionné de préparation de composés organiques nouveaux
FR3354M (fr) * 1962-12-15 1965-06-08 Lemoine Jean Philippe Nouveaux agents antispasmodiques et parasympatholytiques.
IL42472A (en) * 1972-06-27 1977-01-31 Syntex Corp Dialkylaminoalkyl esters of 6-methoxy-2-naphthylpropionic acid and salts thereof and their preparation
AR206620A1 (es) * 1974-02-07 1976-08-06 Hexachimie Procedimiento para preparar acidos 5-indanilaceticos
EP0180416A3 (en) * 1984-10-30 1986-11-20 Takeda Chemical Industries, Ltd. Benzoic acid analogues and their production
IT1208736B (it) * 1986-03-04 1989-07-10 Sigma Tau Ind Farmaceuti Alogenuri dell'estere del 2-n,n,n,dimetil-alchil-amminoetanolo con acido acetico variamente sostituito e composizioni farmaceutiche che licontengono ad attivita' antiinfiammatoria e antisettica

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009543857A (ja) * 2006-07-18 2009-12-10 テックフィールズ バイオケム カンパニー リミテッド イブプロフェンの正荷電水溶性プロドラッグ
JP2009544685A (ja) * 2006-07-25 2009-12-17 テックフィールズ バイオケム カンパニー リミテッド 非常に速い皮膚透過率を有するジクロフェナクの正荷電水溶性プロドラッグ
JP2010500989A (ja) * 2006-08-15 2010-01-14 テックフィールズ バイオケム カンパニー リミテッド 非常に速い皮膚透過率を有するアリール−及びヘテロアリールプロピオン酸の正荷電水溶性プロドラッグ
JP2010529101A (ja) * 2007-06-04 2010-08-26 テックフィールズ インコーポレイテッド 非常に速い皮膚及び膜浸透速度を有するｎｓａｉａプロドラッグ及びその新規医薬使用
JP2013224292A (ja) * 2012-04-20 2013-10-31 Rohm & Haas Co ジベンジルアミン疎水性物質
JP2013014631A (ja) * 2012-10-23 2013-01-24 Techfields Biochem Co Ltd 非常に速い皮膚透過率を有するアリール−及びヘテロアリールプロピオン酸の正荷電水溶性プロドラッグ
JP2014043450A (ja) * 2013-10-08 2014-03-13 Techfields Biochem Co Ltd 非常に速い皮膚透過率を有するアリール−及びヘテロアリールプロピオン酸の正荷電水溶性プロドラッグ
JP2016130241A (ja) * 2016-02-05 2016-07-21 テックフィールズ バイオケム カンパニー リミテッド 非常に速い皮膚透過率を有するアリール−及びヘテロアリールプロピオン酸の正荷電水溶性プロドラッグ

Also Published As

Publication number Publication date
EP0289262A2 (en) 1988-11-02
ZA882957B (en) 1989-12-27
EP0289262A3 (en) 1989-05-31
AU1508988A (en) 1988-10-27

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