CN101511774B - 具有快速皮肤穿透速度的带正电荷的水溶性的芥子气类化合物及其相关化合物的前药 - Google Patents
具有快速皮肤穿透速度的带正电荷的水溶性的芥子气类化合物及其相关化合物的前药 Download PDFInfo
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- CN101511774B CN101511774B CN200680056000.7A CN200680056000A CN101511774B CN 101511774 B CN101511774 B CN 101511774B CN 200680056000 A CN200680056000 A CN 200680056000A CN 101511774 B CN101511774 B CN 101511774B
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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
- C07C233/46—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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
- C07C233/47—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms 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 having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07C229/40—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/42—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/22—Amides of acids of phosphorus
- C07F9/24—Esteramides
- C07F9/2404—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/242—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic of hydroxyaryl compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/22—Amides of acids of phosphorus
- C07F9/24—Esteramides
- C07F9/2404—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/2429—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic of arylalkanols
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/22—Amides of acids of phosphorus
- C07F9/24—Esteramides
- C07F9/2454—Esteramides the amide moiety containing a substituent or a structure which is considered as characteristic
- C07F9/2458—Esteramides the amide moiety containing a substituent or a structure which is considered as characteristic of aliphatic amines
Abstract
Description
化合物 | 每天用量(mg/kg) | 小鼠只数 | 存活时间(天) | 生命延长率(%) | 无病率 | 体重减轻率(%) |
空白组(A) | - | 7 | 45.5±1.6 | 100 | 0/7 | 1% |
B1 | 1.5 | 7 | 55.7±1.3 | 122 | 0/7 | 10% |
B2 | 3.0 | 7 | 88.5±1.8 | 195 | 2/7 | 18% |
C1 | 1.5 | 7 | 57.8±1.5 | 127 | 0/7 | 9% |
C2 | 3.0 | 7 | 90.2±1.9 | 198 | 3/7 | 17% |
D1 | 1.5 | 7 | 128.5±1.3 | 282 | 4/7 | 5% |
D2 | 3.0 | 7 | 115.2±2.1 | 253 | 4/7 | 10% |
E1 | 1.5 | 7 | 130.5±1.6 | 287 | 4/7 | 4% |
E2 | 3.0 | 7 | 121.2±1.8 | 266 | 3/7 | 9% |
F1 | 1.5 | 7 | 122.5±1.7 | 269 | 4/7 | 6% |
F2 | 3.0 | 7 | 111.2±1.9 | 244 | 3/7 | 11% |
Claims (12)
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201510276230.5A CN104987296B (zh) | 2006-10-03 | 2006-10-03 | 具有快速皮肤穿透速度的带正电荷的水溶性的芥子类化合物及其相关化合物的前药 |
HK16104109.2A HK1216096A1 (zh) | 2006-10-03 | 2016-04-11 | 具有快速皮膚穿透速度的帶正電荷的水溶性的芥子類化合物及其相關化合物的前藥 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IB2006/053619 WO2008041059A1 (en) | 2006-10-03 | 2006-10-03 | Positively charged water-soluble prodrugs of mustards and related compounds with very high skin penetration rates |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201510276230.5A Division CN104987296B (zh) | 2006-10-03 | 2006-10-03 | 具有快速皮肤穿透速度的带正电荷的水溶性的芥子类化合物及其相关化合物的前药 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101511774A CN101511774A (zh) | 2009-08-19 |
CN101511774B true CN101511774B (zh) | 2015-05-13 |
Family
ID=39268129
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN200680056000.7A Active CN101511774B (zh) | 2006-10-03 | 2006-10-03 | 具有快速皮肤穿透速度的带正电荷的水溶性的芥子气类化合物及其相关化合物的前药 |
Country Status (5)
Country | Link |
---|---|
US (3) | US10189774B2 (zh) |
EP (2) | EP2077991B1 (zh) |
CN (1) | CN101511774B (zh) |
HK (3) | HK1137415A1 (zh) |
WO (1) | WO2008041059A1 (zh) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
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 |
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 |
CN108627380B (zh) * | 2017-03-15 | 2020-10-20 | 中国人民解放军军事医学科学院毒物药物研究所 | 去除或减少有毒物质的方法以及检测有毒物质的方法 |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1370161A (zh) * | 1999-06-23 | 2002-09-18 | 瑟维尔实验室 | 新的季铵化合物,其制备方法和其药物用途 |
US6638528B1 (en) * | 2000-01-20 | 2003-10-28 | Noven Pharmaceuticals, Inc. | Compositions and methods to effect the release profile in the transdermal administration of active agents |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5091552A (en) | 1986-06-30 | 1992-02-25 | Board Of Regents, The University Of Texas System | Novel antitumor aldophosphamide analogs |
US5773435A (en) | 1987-08-04 | 1998-06-30 | Bristol-Myers Squibb Company | Prodrugs for β-lactamase and uses thereof |
ATE101342T1 (de) | 1988-09-06 | 1994-02-15 | Kabi Pharmacia Ab | Prostaglandinderivate zur behandlung des gruenen stars oder einer okularen hypertension. |
WO1994027954A1 (en) | 1993-05-25 | 1994-12-08 | Auckland Uniservices Limited | Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective cytotoxic agents |
ES2181805T3 (es) * | 1994-12-23 | 2003-03-01 | Astrazeneca Ab | Compuestos quimicos. |
GB9501052D0 (en) | 1995-01-19 | 1995-03-08 | Cancer Res Campaign Tech | Improvements relating to prodrugs |
US5659061A (en) | 1995-04-20 | 1997-08-19 | Drug Innovation & Design, Inc. | Tumor protease activated prodrugs of phosphoramide mustard analogs with toxification and detoxification functionalities |
DE19636889A1 (de) * | 1996-09-11 | 1998-03-12 | Felix Dr Kratz | Antineoplastisch wirkende Transferrin- und Albuminkonjugate zytostatischer Verbindungen aus der Gruppe der Anthrazykline, Alkylantien, Antimetabolite und Cisplatin-Analoga und diese enthaltende Arzneimittel |
US6137003A (en) * | 1998-10-28 | 2000-10-24 | Shionogi Bioresearch | Bis (haloethyl) aminobenzene derivatives |
GB9907414D0 (en) | 1999-03-31 | 1999-05-26 | Cancer Res Campaign Tech | Improvements relating to prodrugs |
GB0102239D0 (en) | 2001-01-29 | 2001-03-14 | Cancer Res Ventures Ltd | Methods of chemical synthisis |
-
2006
- 2006-10-03 WO PCT/IB2006/053619 patent/WO2008041059A1/en active Search and Examination
- 2006-10-03 EP EP06809490.3A patent/EP2077991B1/en not_active Not-in-force
- 2006-10-03 CN CN200680056000.7A patent/CN101511774B/zh active Active
- 2006-10-03 EP EP20140156554 patent/EP2792670A1/en active Pending
-
2009
- 2009-04-03 US US12/418,564 patent/US10189774B2/en not_active Expired - Fee Related
-
2010
- 2010-01-28 HK HK10100931.0A patent/HK1137415A1/zh unknown
-
2015
- 2015-04-15 HK HK15103662.4A patent/HK1203188A1/zh unknown
-
2016
- 2016-04-11 HK HK16104109.2A patent/HK1216096A1/zh unknown
-
2018
- 2018-12-04 US US16/209,744 patent/US11479527B2/en active Active
-
2022
- 2022-10-24 US US18/049,041 patent/US20230097823A1/en active Pending
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1370161A (zh) * | 1999-06-23 | 2002-09-18 | 瑟维尔实验室 | 新的季铵化合物,其制备方法和其药物用途 |
US6638528B1 (en) * | 2000-01-20 | 2003-10-28 | Noven Pharmaceuticals, Inc. | Compositions and methods to effect the release profile in the transdermal administration of active agents |
Non-Patent Citations (1)
Title |
---|
Wolf M et al.Alkylating benzamides with melanoma cytotoxicity.《Melanoma Rearch》.2004,第14卷(第5期),第353页、表1. * |
Also Published As
Publication number | Publication date |
---|---|
HK1203188A1 (zh) | 2015-10-23 |
US20100069336A1 (en) | 2010-03-18 |
US20230097823A1 (en) | 2023-03-30 |
HK1216096A1 (zh) | 2016-10-14 |
EP2077991A1 (en) | 2009-07-15 |
US10189774B2 (en) | 2019-01-29 |
EP2077991A4 (en) | 2011-11-16 |
US11479527B2 (en) | 2022-10-25 |
WO2008041059A1 (en) | 2008-04-10 |
EP2077991B1 (en) | 2014-02-26 |
CN101511774A (zh) | 2009-08-19 |
US20190233367A1 (en) | 2019-08-01 |
HK1137415A1 (zh) | 2010-07-30 |
EP2792670A1 (en) | 2014-10-22 |
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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: 20220525 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. |