CN101500983B - 具有快速皮肤穿透速度的带正电荷的水溶性二氟尼柳及相关化合物的前药 - Google Patents
具有快速皮肤穿透速度的带正电荷的水溶性二氟尼柳及相关化合物的前药 Download PDFInfo
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- CN101500983B CN101500983B CN200680055458.0A CN200680055458A CN101500983B CN 101500983 B CN101500983 B CN 101500983B CN 200680055458 A CN200680055458 A CN 200680055458A CN 101500983 B CN101500983 B CN 101500983B
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- carbon atom
- diflunisal
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- acid
- structural formula
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C219/02—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C219/04—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C219/14—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the hydroxy groups esterified by a carboxylic acid having the esterifying carboxyl group bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
- C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
- C07C229/12—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of acyclic carbon skeletons
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/58—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/60—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
- C07C53/08—Acetic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/235—Saturated compounds containing more than one carboxyl group
- C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
- C07C59/265—Citric acid
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
组别 | A | B1 | B2 | C1 | C2 | D1 | D2 | E1 | E2 |
剂量(mg/kg) | 0 | 50 | 100 | 50 | 100 | 50 | 100 | 50 | 100 |
扭体次数 | 35.0 | 18.1 | 13.2 | 13.2 | 10.2 | 14.2 | 12.0 | 14.0 | 11.9 |
百分比(%) | - | 48 | 62 | 62 | 71 | 59 | 65 | 60 | 66 |
化合物 | t=0min. | t=90min. | t=180min. | t=270min. |
A,对照组 | 37.33±0.05 | 37.26±0.07 | 37.32±0.05 | 37.34±0.08 |
B1(100mg/kg) | 37.25±0.06 | 36.81±0.05 | 36.82±0.08 | 36.78±0.07 |
B2(150mg/kg) | 37.35±0.09 | 36.61±0.07 | 36.56±0.06 | 36.57±0.05 |
C1(100mg/kg) | 37.22±0.07 | 36.42±0.06 | 36.40±0.05 | 36.47±0.08 |
C2(150mg/kg) | 37.26±0.08 | 36.20±0.05 | 36.30±0.07 | 36.31±0.08 |
D1(100mg/kg) | 37.28±0.06 | 36.75±0.06 | 36.78±0.08 | 36.80±0.07 |
D2(150mg/kg) | 37.26±0.05 | 36.45±0.05 | 36.40±0.07 | 36.50±0.05 |
E1(100mg/kg) | 37.28±0.06 | 36.85±0.06 | 36.88±0.08 | 36.86±0.07 |
E2(150mg/kg) | 37.26±0.05 | 36.55±0.05 | 36.60±0.07 | 36.65±0.05 |
Claims (18)
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201510594436.2A CN105439877B (zh) | 2006-07-26 | 2006-07-26 | 带正电荷的水溶性二氟尼柳及相关化合物的前药 |
HK16105026.9A HK1217015A1 (zh) | 2006-07-26 | 2016-05-03 | 帶正電荷的水溶性二氟尼柳及相關化合物的前藥 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IB2006/052563 WO2008012603A1 (en) | 2006-07-26 | 2006-07-26 | Positively charged water-soluble prodrugs of diflunisal and related compounds with very fast skin penetration rate |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201510594436.2A Division CN105439877B (zh) | 2006-07-26 | 2006-07-26 | 带正电荷的水溶性二氟尼柳及相关化合物的前药 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101500983A CN101500983A (zh) | 2009-08-05 |
CN101500983B true CN101500983B (zh) | 2015-09-16 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN200680055458.0A Active CN101500983B (zh) | 2006-07-26 | 2006-07-26 | 具有快速皮肤穿透速度的带正电荷的水溶性二氟尼柳及相关化合物的前药 |
Country Status (3)
Country | Link |
---|---|
CN (1) | CN101500983B (zh) |
HK (2) | HK1136814A1 (zh) |
WO (1) | WO2008012603A1 (zh) |
Families Citing this family (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20090221703A1 (en) | 2006-07-09 | 2009-09-03 | Chongxi Yu | High penetration composition and uses thereof |
US20090238763A1 (en) | 2006-07-09 | 2009-09-24 | Chongxi Yu | High penetration compositions and uses thereof |
EP2084124B9 (en) | 2006-10-02 | 2015-07-01 | Techfields Biochem Co. Ltd | Positively charged water-soluble prodrugs of prostaglandins and related compounds with very high skin penetration rates |
CN101541743A (zh) | 2006-11-08 | 2009-09-23 | 于崇曦 | 多肽及相关化合物的透皮给药系统 |
JP5324463B2 (ja) | 2006-12-10 | 2013-10-23 | チョンシー ユー | β−ラクタム抗生物質の経皮送達システム |
EP2125697B1 (en) | 2007-01-15 | 2016-09-28 | Chongxi Yu | Positively charged water-soluble prodrugs of retinoids and retinoid-like compounds with very high skin penetration rates |
JP5389668B2 (ja) | 2007-01-31 | 2014-01-15 | チョンシー ユー | 皮膚浸透率の非常に高い1H−イミダゾ[4,5−c]キノリン−4−アミン及び関連化合物の正に荷電した水溶性プロドラッグ |
CN105820107B (zh) | 2007-06-04 | 2022-09-09 | 泰飞尔公司 | 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 |
KR20200022525A (ko) * | 2008-12-04 | 2020-03-03 | 충시 위 | 고투과력을 가진 조성물 및 이의 적용 |
CA2755069A1 (en) * | 2009-03-16 | 2010-09-23 | Genmedica Therapeutics Sl | Anti-inflammatory and antioxidant conjugates useful for treating metabolic disorders |
CN108084246A (zh) | 2009-05-08 | 2018-05-29 | 上海泰飞尔生化技术有限公司 | 多肽和多肽相关化合物的高穿透力前药组合物 |
US9969751B2 (en) | 2009-06-10 | 2018-05-15 | Techfields Pharma Co., Ltd. | High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds |
US8466197B2 (en) | 2010-12-14 | 2013-06-18 | Genmedica Therapeutics Sl | Thiocarbonates as anti-inflammatory and antioxidant compounds useful for treating metabolic disorders |
IN2014KN02583A (zh) | 2012-05-16 | 2015-05-08 | Techfields Pharma Co Ltd | |
JP2016516018A (ja) * | 2013-03-15 | 2016-06-02 | テックフィールズ ファーマ カンパニー リミテッド | パ−キンソン病治療用の新規高透過薬物及びその組成物 |
US20160168108A1 (en) | 2014-12-16 | 2016-06-16 | Adt Pharmaceuticals, Inc. | Method of treating or preventing ras-mediated diseases |
US9862698B2 (en) | 2014-12-16 | 2018-01-09 | Adt Pharmaceuticals, Inc. | Indenyl compounds, pharmaceutical compositions, and medical uses thereof |
CN106924272B (zh) * | 2015-12-31 | 2021-04-13 | 中国医学科学院药物研究所 | 水杨酸甲酯糖苷在制备预防和/或治疗系统性红斑狼疮及其并发症药物中的用途 |
US11186596B2 (en) | 2018-04-26 | 2021-11-30 | Adt Pharmaceuticals, Llc | Anticancer indenes, indanes, azaindenes, azaindanes, pharmaceutical compositions and uses |
CN113999126B (zh) * | 2021-12-03 | 2024-05-24 | 浙江东亚药业股份有限公司 | 一种曲美布汀的制备方法 |
WO2023134732A1 (en) * | 2022-01-17 | 2023-07-20 | Techfields Pharma Co., Ltd. | Prevention or treatment of cardiovascular diseases with high penetration prodrugs of aspirin and other nsaids |
CN117776940A (zh) * | 2022-09-28 | 2024-03-29 | 浙江越甲药业有限公司 | 苯甲酸酯的衍生物 |
Citations (2)
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US3476791A (en) * | 1966-05-04 | 1969-11-04 | Trustees Of Ohio State Univ Th | O-thiocarbamoyl benzoic acid esters |
US3488380A (en) * | 1966-03-30 | 1970-01-06 | Bristol Myers Co | Carbamate esters and their method of preparation |
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AU2004201178A1 (en) * | 1999-02-26 | 2004-04-22 | Emisphere Technologies, Inc. | Compounds and compositions for delivering active agents |
US7985422B2 (en) * | 2002-08-05 | 2011-07-26 | Torrent Pharmaceuticals Limited | Dosage form |
US20050272108A1 (en) * | 2004-05-21 | 2005-12-08 | Bhanu Kalra | Stabilized two component system for chemiluminescent assay in immunodiagnostics |
-
2006
- 2006-07-26 CN CN200680055458.0A patent/CN101500983B/zh active Active
- 2006-07-26 WO PCT/IB2006/052563 patent/WO2008012603A1/en active Application Filing
-
2010
- 2010-01-18 HK HK10100503.8A patent/HK1136814A1/zh unknown
-
2016
- 2016-05-03 HK HK16105026.9A patent/HK1217015A1/zh unknown
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3488380A (en) * | 1966-03-30 | 1970-01-06 | Bristol Myers Co | Carbamate esters and their method of preparation |
US3476791A (en) * | 1966-05-04 | 1969-11-04 | Trustees Of Ohio State Univ Th | O-thiocarbamoyl benzoic acid esters |
Non-Patent Citations (3)
Title |
---|
A. Gringauz.Certain Disubstituted o-Aminoacetoxy- and Propoxybenzoic and Cinnamic Acids and their tert-Butyl Esters.《Journal of Pharmaceutical Sciences》.1970,第59卷(第3期),422-425. * |
G. E.Cwalina et al..Synthesis and Stability Studies of Certain Disubstituted Aminoacetoxybenzoic Acids.《 Journal of Organic Chemistry》.1961,第26卷3344-3346. * |
W. Adam et al..A convenient synthesis of nickel(II) and cobalt(II) complexes of unsymmetrical salen-type ligands and their application as catalysts for the oxidation of 2,6-dimethylphenol and 1,5-dihydroxynaphthalene by molecular oxygen.《Indian Journal of Chemistry》.2004,第43A卷56-62. * |
Also Published As
Publication number | Publication date |
---|---|
WO2008012603A1 (en) | 2008-01-31 |
HK1217015A1 (zh) | 2016-12-16 |
CN101500983A (zh) | 2009-08-05 |
HK1136814A1 (zh) | 2010-07-09 |
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Address after: Illinois, America Patentee after: Yu Chongxi Patentee after: Taifeier biomedical (Suzhou) Co.,Ltd. Address before: Illinois, America Patentee before: Yu Chongxi Patentee before: Shanghai Taifeier Biochemical Technology Co.,Ltd. |
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Effective date of registration: 20220519 Address after: 215129 Room 401, building 9, No. 168, Majian Road, high tech Zone, Suzhou, Jiangsu Province Patentee after: Taifeier biomedical (Suzhou) Co.,Ltd. Address before: Illinois, America Patentee before: Yu Chongxi Patentee before: Taifeier biomedical (Suzhou) Co.,Ltd. |