CN101500983A - 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
- Publication number
- CN101500983A CN101500983A CNA2006800554580A CN200680055458A CN101500983A CN 101500983 A CN101500983 A CN 101500983A CN A2006800554580 A CNA2006800554580 A CN A2006800554580A CN 200680055458 A CN200680055458 A CN 200680055458A CN 101500983 A CN101500983 A CN 101500983A
- Authority
- CN
- China
- Prior art keywords
- carbon atom
- general formula
- structural formula
- diflunisal
- ointment
- 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.)
- Granted
Links
Images
Classifications
-
- 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
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 (10)
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 true CN101500983A (zh) | 2009-08-05 |
CN101500983B CN101500983B (zh) | 2015-09-16 |
Family
ID=38981173
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) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN115448905A (zh) * | 2022-09-28 | 2022-12-09 | 浙江越甲药业有限公司 | 苯甲酸酯的衍生物 |
Families Citing this family (21)
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 |
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 |
AU2006350707A1 (en) | 2006-11-08 | 2008-05-15 | Chongxi Yu | Transdermal delivery systems of peptides and related compounds |
PL2121593T3 (pl) | 2006-12-10 | 2015-11-30 | Chongxi Yu | Przezskórne systemy dostarczania antybiotyków beta-laktamowych |
HUE031712T2 (en) | 2007-01-15 | 2017-08-28 | Chongxi Yu | Retinoids and retinoid-like compounds with positively charged water-soluble prodrugs having very high skin penetration rates |
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 |
BRPI0721709B1 (pt) | 2007-06-04 | 2024-03-12 | Techfields Inc. | PRÓ-FÁRMACOS DE NSAIAs, PROCESSO PARA PREPARAÇÃO DOS MESMOS, SEU USO, SISTEMAS TERAPÊUTICOS DE APLICAÇÃO TRANSDÉRMICA E COMPOSIÇÃO QUE OS COMPREENDE |
RU2630577C2 (ru) | 2008-12-04 | 2017-09-11 | Чунси ЮЙ | Композиции интенсивного проникновения и их применение |
US8575217B2 (en) | 2009-03-16 | 2013-11-05 | Genmedica Therapeutics Sl | Anti-inflammatory and antioxidant conjugates useful for treating metabolic disorders |
JP6352587B2 (ja) | 2009-05-08 | 2018-07-11 | テックフィールズ バイオケム カンパニー リミテッド | ペプチド及びペプチド関連化合物の高浸透性プロドラッグ組成物 |
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 |
MX2014013910A (es) | 2012-05-16 | 2015-06-04 | Techfields Pharma Co Ltd | Composiciones de profarmacos de alta penetracion y composiciones farmaceuticas de los mismos para el tratamiento de afecciones pulmonares. |
BR112015022896B1 (pt) | 2013-03-15 | 2022-08-23 | Chongxi Yu | Composto de fármacos de alta penetração, composição farmacêutica e seus usos para o tratamento de doenças de parkinson |
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 |
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 |
CA3096700C (en) | 2018-04-26 | 2023-08-22 | Adt Pharmaceuticals, Llc | Anticancer indenes, indanes, azaindenes, azaindanes, pharmaceutical compositions and uses |
CN113999126A (zh) * | 2021-12-03 | 2022-02-01 | 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 |
Family Cites Families (5)
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 |
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
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN115448905A (zh) * | 2022-09-28 | 2022-12-09 | 浙江越甲药业有限公司 | 苯甲酸酯的衍生物 |
Also Published As
Publication number | Publication date |
---|---|
CN101500983B (zh) | 2015-09-16 |
HK1136814A1 (zh) | 2010-07-09 |
WO2008012603A1 (en) | 2008-01-31 |
HK1217015A1 (zh) | 2016-12-16 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CN101500983B (zh) | 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 | |
CN101489985B (zh) | 具有快速皮肤穿透率的带正电荷的水溶性布洛芬前药 | |
CN101506168B (zh) | 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 | |
CN101506161B (zh) | 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 | |
JP5466006B2 (ja) | 非常に速い皮膚浸透率を有するアセトアミノフェン及び関連化合物の正荷電水溶性プロドラッグ | |
CN101484415B (zh) | 带有正电荷的水溶性阿司匹林前药 | |
CN101500982A (zh) | 具有快速皮肤穿透速度的带正电荷的水溶性双氯芬酸前药 | |
CN101506160A (zh) | 具有快速皮肤穿透速度的带正电荷的芳基和杂芳基乙酸类前药 | |
CN101522692A (zh) | 具有快速皮肤穿透速度的带正电荷的水溶性的昔康及其相关化合物的前药 | |
CN101500984A (zh) | 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 | |
AU2013231152B2 (en) | Positively charged water-soluble pro-drugs of ibuprofen | |
CN104622858B (zh) | 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 | |
CN105439877B (zh) | 带正电荷的水溶性二氟尼柳及相关化合物的前药 | |
CN104974058A (zh) | 具有快速皮肤穿透速度的带正电荷的水溶性双氯芬酸前药 | |
CN104610077A (zh) | 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 | |
CN103948571A (zh) | 具有快速皮肤穿透率的带正电荷的水溶性布洛芬前药 | |
AU2006347925B2 (en) | Positively charged water-soluble prodrugs of acetaminophen and related compounds with very fast skin penetration rate | |
JP2013173777A (ja) | 非常に速い皮膚浸透率を有するアセトアミノフェン及び関連化合物の正荷電水溶性プロドラッグ | |
CN104706630B (zh) | 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 | |
CN103772259B (zh) | 具有快速皮肤穿透速度的带正电荷的芳基和杂芳基乙酸类前药 | |
CN103705496A (zh) | 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 | |
JP2016006124A (ja) | 非常に速い皮膚浸透率を有するアセトアミノフェン及び関連化合物の正荷電水溶性プロドラッグ | |
CN103772258A (zh) | 具有快速皮肤穿透速度的带正电荷的芳基和杂芳基乙酸类前药 | |
CN103980228A (zh) | 具有快速皮肤穿透速度的带正电荷的水溶性的昔康及其相关化合物的前药 | |
CN103922946A (zh) | 带有正电荷的水溶性阿司匹林前药 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
C06 | Publication | ||
PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 1136814 Country of ref document: HK |
|
C14 | Grant of patent or utility model | ||
GR01 | Patent grant | ||
REG | Reference to a national code |
Ref country code: HK Ref legal event code: GR Ref document number: 1136814 Country of ref document: HK |
|
CP01 | Change in the name or title of a patent holder | ||
CP01 | Change in the name or title of a patent holder |
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. |
|
TR01 | Transfer of patent right | ||
TR01 | Transfer of patent right |
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. |