CN101506168A - 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 - Google Patents
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 Download PDFInfo
- Publication number
- CN101506168A CN101506168A CNA2006800557447A CN200680055744A CN101506168A CN 101506168 A CN101506168 A CN 101506168A CN A2006800557447 A CNA2006800557447 A CN A2006800557447A CN 200680055744 A CN200680055744 A CN 200680055744A CN 101506168 A CN101506168 A CN 101506168A
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- China
- Prior art keywords
- acid
- carbon atom
- structural formula
- compound
- general formula
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
- C07D213/80—Acids; Esters in position 3
-
- 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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
- C07C237/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C327/00—Thiocarboxylic acids
- C07C327/20—Esters of monothiocarboxylic acids
- C07C327/30—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pain & Pain Management (AREA)
- Pharmacology & Pharmacy (AREA)
- Rheumatology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyridine Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
组别 | 剂量(mg/kg) | 扭体次数 | 抑制率(%) |
A | 0 | 35.0 | |
B | 100 | 15.6 | 55 |
C | 100 | 14.2 | 59 |
D | 100 | 16.1 | 54 |
E | 100 | 15.2 | 57 |
F | 100 | 15.7 | 55 |
化合物 | t=0min. | t=90min. | t=180min. | t=270min. |
A(对照组) | 37.34±0.05 | 37.36±0.07 | 37.37±0.05 | 37.44±0.08 |
B(100mg/kg) | 37.35±0.06 | 36.71±0.05 | 36.60±0.08 | 36.59±0.07 |
C(100mg/kg) | 37.28±0.06 | 36.68±0.05 | 36.62±0.08 | 36.58±0.07 |
D(100mg/kg) | 37.27±0.06 | 36.76±0.05 | 36.65±0.08 | 36.49±0.07 |
E(100mg/kg) | 37.25±0.07 | 36.82±0.06 | 36.70±0.05 | 36.50±0.08 |
F(100mg/kg) | 37.23±0.06 | 36.69±0.06 | 36.52±0.08 | 36.40±0.07 |
Claims (11)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201510019131.9A CN104706630B (zh) | 2006-09-03 | 2006-09-03 | 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 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IB2006/053090 WO2008029199A1 (en) | 2006-09-03 | 2006-09-03 | Positively charged water-soluble prodrugs of n-arylanthranilic acids with very fast skin penetration rate |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201510019131.9A Division CN104706630B (zh) | 2006-09-03 | 2006-09-03 | 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 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101506168A true CN101506168A (zh) | 2009-08-12 |
CN101506168B CN101506168B (zh) | 2014-12-10 |
Family
ID=39156867
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN200680055744.7A Active CN101506168B (zh) | 2006-09-03 | 2006-09-03 | 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 |
Country Status (6)
Country | Link |
---|---|
EP (2) | EP2623495B1 (zh) |
CN (1) | CN101506168B (zh) |
ES (2) | ES2694685T3 (zh) |
HK (1) | HK1137426A1 (zh) |
PL (2) | PL2623495T3 (zh) |
WO (1) | WO2008029199A1 (zh) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101687792A (zh) * | 2007-06-04 | 2010-03-31 | 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 |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7632866B2 (en) | 2002-10-21 | 2009-12-15 | Ramot At Tel Aviv University | Derivatives of N-phenylanthranilic acid and 2-benzimidazolone as potassium channel and/or neuron activity modulators |
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 |
JP5378219B2 (ja) | 2006-10-02 | 2013-12-25 | テックフィールズ バイオケム カンパニー リミテッド | 非常に高い皮膚浸透率を有するプロスタグランジン及び関連化合物の正荷電水溶性プロドラッグ |
JP5424887B2 (ja) | 2006-11-08 | 2014-02-26 | チョンシー ユー | ペプチド及び関連化合物の経皮送達システム |
CA2671938C (en) | 2006-12-10 | 2017-10-17 | Chongxi Yu | Transdermal delivery systems of beta-lactam antibiotics |
CN101605754B (zh) | 2007-01-15 | 2015-09-16 | 于崇曦 | 具有快速皮肤穿透速度的带正电荷的水溶性的维生素a酸类和类维生素a酸化合物的前药 |
ES2607901T3 (es) | 2007-01-31 | 2017-04-04 | Chongxi Yu | Profármacos hidrosolubles cargados positivamente de 1H-imidazo[4,5-c]quinolin-4-aminas y compuestos relacionados con ratas de penetración de piel muy altas |
EP2203411B1 (en) | 2007-09-20 | 2016-01-06 | Ramot at Tel-Aviv University Ltd. | N-phenyl anthranilic acid derivatives and uses thereof |
WO2009037705A2 (en) * | 2007-09-20 | 2009-03-26 | Ramot At Tel Aviv University Ltd. | Esters of n-phenylanthranilic acid for use in the treatment of cancer and inflammation |
KR20210123406A (ko) * | 2008-12-04 | 2021-10-13 | 충시 위 | 고투과력을 가진 조성물 및 이의 적용 |
ES2845612T3 (es) | 2009-05-08 | 2021-07-27 | Techfields Biochem Co Ltd | Composiciones de profármaco de alta penetración de péptidos y compuestos relacionados con péptidos |
US9969751B2 (en) | 2009-06-10 | 2018-05-15 | Techfields Pharma Co., Ltd. | High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds |
US20120022116A1 (en) * | 2010-07-20 | 2012-01-26 | Huayun Deng | Compositions and methods for the treatment of pathological condition(s) related to gpr35 and/or gpr35-herg complex |
PL2849738T3 (pl) | 2012-01-18 | 2024-05-13 | Techfields Pharma Co., Ltd. | Kompozycje proleków o dużej szybkości przenikania i ich kompozycje farmaceutyczne do leczenia chorób płuc |
CA2917145C (en) | 2013-03-15 | 2023-10-24 | Techfields Pharma Co., Ltd. | Novel high penetration drugs and their compositions thereof for treatment of parkinson diseases |
US9862698B2 (en) | 2014-12-16 | 2018-01-09 | Adt Pharmaceuticals, Inc. | Indenyl compounds, pharmaceutical compositions, and medical uses thereof |
US20160168108A1 (en) | 2014-12-16 | 2016-06-16 | Adt Pharmaceuticals, Inc. | Method of treating or preventing ras-mediated diseases |
EP3784228A1 (en) | 2018-04-26 | 2021-03-03 | ADT Pharmaceuticals, LLC | Anticancer indenes, indanes, azaindenes, azaindanes, pharmaceutical compositions and uses |
WO2020070557A1 (en) * | 2018-10-02 | 2020-04-09 | Q Biomed Inc. | Modified therapeutic agent analogs of mefenamic acid |
US20220267270A1 (en) * | 2019-08-30 | 2022-08-25 | University Of South Florida | Sting modulators, compositions, and methods of use |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
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GB100208A (en) * | 1915-03-24 | 1917-03-01 | Isidore Swientoslawsk Morrison | Improvements in Watch Movements. |
US2671805A (en) * | 1952-07-02 | 1954-03-09 | Searle & Co | Basically substituted o-arylamino-benzamides |
GB984471A (en) * | 1961-01-12 | 1965-02-24 | Parke Davis & Co | Anthranilic acid esters and methods for producing the same |
BE630053A (zh) * | 1962-03-27 | |||
US3420871A (en) * | 1964-09-01 | 1969-01-07 | Parke Davis & Co | Anthranilic acid esters |
DK121236B (da) * | 1967-07-03 | 1971-09-27 | Gea As | Analogifremgangsmåde til fremstilling af terapeutisk aktive, basisk substituerede amider af N-substituerede antranilsyrer, eller syreadditionssalte deraf. |
GB1187259A (en) * | 1967-10-23 | 1970-04-08 | Hexachimie | New Aminoalkyl Esters of 2-Anilino-Nicotinic Acids and process for their manufacture |
US3814811A (en) * | 1972-06-07 | 1974-06-04 | Andreu Sa Dr | Method of eliminating or alleviating local pain with diethylaminoethyl flufenamate |
JPS57183738A (en) * | 1981-05-06 | 1982-11-12 | Yamanouchi Pharmaceut Co Ltd | Aromatic carboxylic acid derivative |
JPS6452742A (en) * | 1987-04-27 | 1989-02-28 | Syntex Pharma Int | Omega-quaternary ammonium alkyl ester and thioester of acidic non-steroidal antiinflammatory |
US5654337A (en) | 1995-03-24 | 1997-08-05 | II William Scott Snyder | Topical formulation for local delivery of a pharmaceutically active agent |
AUPN531195A0 (en) | 1995-09-11 | 1995-10-05 | J.W. Broadbent Nominees Pty. Ltd. | Lipid extract having anti-inflamatory activity |
KR100213465B1 (ko) | 1996-11-01 | 1999-08-02 | 최좌진 | 케토프로펜 패취 조성물 |
US5885597A (en) | 1997-10-01 | 1999-03-23 | Medical Research Industries,Inc. | Topical composition for the relief of pain |
MXPA00012844A (es) | 1998-07-07 | 2004-05-21 | Transdermal Technologies Inc | Composiciones para la liberacion transdermica rapida y sin irritacion de agentes farmaceuticamente activos y metodos para formular tales composiciones y liberar los mismos. |
US6416772B1 (en) | 2001-01-12 | 2002-07-09 | H. Wayne Van Engelen | Topical dermal anaesthetic |
US6528040B1 (en) | 2001-01-18 | 2003-03-04 | Maurine Pearson | EMU oil-based formulations for use as an analgesic, anesthetic and antipruritic |
US7052715B2 (en) | 2003-04-11 | 2006-05-30 | All Natural Fmg, Inc. | Alcohol-free transdermal analgesic composition and processes for manufacture and use thereof |
-
2006
- 2006-09-03 ES ES06795893.4T patent/ES2694685T3/es active Active
- 2006-09-03 WO PCT/IB2006/053090 patent/WO2008029199A1/en active Application Filing
- 2006-09-03 PL PL13153470T patent/PL2623495T3/pl unknown
- 2006-09-03 PL PL06795893T patent/PL2084132T3/pl unknown
- 2006-09-03 EP EP13153470.3A patent/EP2623495B1/en active Active
- 2006-09-03 CN CN200680055744.7A patent/CN101506168B/zh active Active
- 2006-09-03 EP EP06795893.4A patent/EP2084132B1/en not_active Not-in-force
- 2006-09-03 ES ES13153470T patent/ES2735287T3/es active Active
-
2010
- 2010-01-28 HK HK10100929.4A patent/HK1137426A1/zh unknown
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101687792A (zh) * | 2007-06-04 | 2010-03-31 | 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 |
CN101687792B (zh) * | 2007-06-04 | 2016-03-02 | 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医药用途 |
Also Published As
Publication number | Publication date |
---|---|
EP2623495B1 (en) | 2019-05-01 |
ES2694685T3 (es) | 2018-12-26 |
HK1137426A1 (zh) | 2010-07-30 |
WO2008029199A1 (en) | 2008-03-13 |
EP2084132A4 (en) | 2010-05-26 |
EP2084132A1 (en) | 2009-08-05 |
CN101506168B (zh) | 2014-12-10 |
PL2084132T3 (pl) | 2019-03-29 |
EP2084132B1 (en) | 2018-08-08 |
EP2623495A1 (en) | 2013-08-07 |
PL2623495T3 (pl) | 2019-11-29 |
ES2735287T3 (es) | 2019-12-17 |
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