POLYMER-CARBOHYDRATE CONJUGATES FOR DRUG DELIVERY TECHNOLOGY
申请人:Wu Nian
公开号:US20150157721A1
公开(公告)日:2015-06-11
The invention comprises compounds, methods of making, and methods of using. The compounds may have a linear or cylic backbone and three or four appended functional groups: one or two lipohilic compounds including sterols or “fat soluble” vitamins, one or two hydrophilic polymer, and one or two carbohydrate. A group of polymer-carbohydrate conjugates having a central backbone and three appended functional groups are disclosed wherein one lipophilic compound is void of both steroid acids. The conjugate may have fatty acids as the primary lipophilic carrier, one hydrophilic polymer, and one carbohydrate. Specific functional groups may be selected for specific applications in formulating pharmaceuticals, cosmetics, nutriceuticals, and the like. Typical coupling reaction of the conjugates may involve one or more or combinations or in series of alkylation including N-alkylation or O-alkylation, etherification, esterification and amidation chemical processes. A variety of linkers between the backbone and functional groups may also be selected to modify the carriers or center backbones for the coupling reactions and optimize performance of the conjugates.
[EN] IMPROVED SYNTHESIS OF LYSINE ACETYLSALICYLATE · GLYCINE PARTICLES<br/>[FR] SYNTHÈSE AMÉLIORÉE DE PARTICULES D'ACÉTYLSALICYLATE DE LYSINE · GLYCINE
申请人:VENTALEON GMBH
公开号:WO2018115434A1
公开(公告)日:2018-06-28
The invention relates to a method for the production of acetylsalicylic acid lysinate, optionally lysine acetylsalicylate · glycine, comprising the following steps: a) providing a solution of acetylsalicylic acid in ethanol; b) providing an aqueous solution of lysine; c) combining the solutions of step a) and b) to form a mixture; d) optionally stirring the mixture; e) adding acetone to the mixture; f) incubating the mixture, to allow the formation of a acetylsalicylic acid lysinate product; g) isolating the acetylsalicylic acid lysinate product; wherein acetylsalicylic acid is used in excess compared to lysine and wherein no seed crystals are added to the mixture; and optionally the following further steps: h) providing a recrystallized glycine; wherein the glycine has been recrystallized with the following steps: h1) dissolving glycine in water; h2) adding acetone to the glycine solution; h3) stirring the mixture until a precipitate is obtained; i) combining the recrystallized glycine of step h) with the acetylsalicylic acid lysinate product of step g) to obtain lysine acetylsalicylate · glycine (LASAG) particles.
Prodrugs of piperazine and substituted piperidine antiviral agents
申请人:Ueda Yasutsugu
公开号:US20050209246A1
公开(公告)日:2005-09-22
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection.
wherein:
X is C or N with the proviso that when X is N, R
1
does not exist;
W is C or N with the proviso that when W is N, R
2
does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and
Y is selected from the group consisting of
Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I.
wherein:
L and M are independently selected from the group consisting of C
1
-C
6
alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
[EN] CRYSTALLIZATION METHOD AND BIOAVAILABILITY<br/>[FR] PROCÉDÉ DE CRISTALLISATION ET BIODISPONIBILITÉ
申请人:THAR PHARMACEUTICALS INC
公开号:WO2017049294A1
公开(公告)日:2017-03-23
Preparation and in vitro and in vivo characterization of novel forms of active pharmaceutical ingredients, suitable for pharmaceutical compositions in drug delivery systems for humans.
准备并进行体外和体内特性评价,研究新型活性药物成分的形式,适用于人体药物输送系统中的药物组合。
[EN] POLYBIOTIN COMPOUNDS FOR MAGNETIC RESONANCE IMAGINING AND DRUG DELIVERY<br/>[FR] COMPOSES DE POLYBIOTINE POUR IRM ET ADMINISTRATION DE MEDICAMENTS
申请人:GEN HOSPITAL CORP
公开号:WO2005032598A1
公开(公告)日:2005-04-14
The invention relates generally to biotin-containing compounds that are useful as imaging agents and drug-delivery agents. Another aspect of the invention relates to the aforementioned compounds chelated to a metal atom. In a preferred embodiment, the metal atom is a gadolinium. Another aspect of the invention relates to a compound comprising three biotin moieties and a pharmaceutical agent covalently bound to a heterocyclic core. In certain embodiments, the pharmaceutical agent is an antibiotic, antiviral, or radionuclide. Another aspect of the present invention relates to a method of treating disease involving administering the compounds of the invention to a mammal. Another aspect of the present invention relates to a method of acquiring a magnetic resonance image using the compounds of the invention.