Abstract: The present invention relates to new anionic glycodendrimers having new biological activity, processes for preparing them and their use in medicine including veterinary medicine.

Abstract: Degradable polyacetal polymers and functionalized degradable polyacetal polymers have properties favorable for use in pharmaceutical and biomedical applications. The degradable polyacetal polymers are relatively stable at physiological pH with favorable biodistribution profiles, and degrade readily in low pH conditions. Conjugates of the polymers with drugs, especially anticancer drugs, and methods of treatment of cancer.

Abstract: Antineoplastic dendritic polymer conjugates which are useful drug delivery systems for carrying antineoplastic agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to an antineoplastic agent capable of interacting with the functional groups, and contacting the dendritic polymer with the antineoplastic agent. The preferred platin-based analogues of the antineoplastic agents conjugated to the dendritic polymer may be administered intravenously, orally, parentally, subcutaneously, intramuscularly, intraarterially or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The antineoplastic dendritic polymer conjugates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.

Abstract: Antineoplastic dendritic polymer conjugates which are useful drug delivery systems for carrying antineoplastic agents to malignant tumors are prepared. The antineoplastic agent is encapsulated within the dendritic polymer using an ionic charge shunt mechanism, whereby, the antineoplastic agent interacts with the anionic functional groups on the surface of the dendritic polymer allowing the antineoplastic agent to be uptaken by the dendritic polymer through an association with the functional groups of the interior of the dendritic polymer. The antineoplastic dendritic polymer conjugates may be administered intravenously, orally, parentally, subcutaneously, intraarterially or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The antineoplastic dendritic polymer conjugates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, and reduced toxicity.

Abstract: The present invention relates to new anionic glycodendrimers having new biological activity, processes for preparing them and their use in medicine including veterinary medicine.

Abstract: The present disclosure concerns biologically active materials, particularly materials that comprise a biodegradeable polymer linked to a biologically active agent. The disclosure further concerns materials known as polymer-drug conjugates that typically contain a therapeutic agent, for instance a bioactive cytotoxic drug linked to a polymer backbone. The linkage typically is a convalent linkage. However, in some embodiments the disclosure concerns other polymer conjugates including those where the biologically active agent is an imaging agent, such as a tyrosinamide, a diagnostic agent, or a targeting agent, such as biotin.

Abstract: Dendritic polymer conjugates which are useful drug delivery systems for carrying platinum containing anti-tumor agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to a platinum containing compound capable of interacting with the functional groups, contacting the dendritic polymer with the platinum containing compound, and reacting the dendritic polymer with the platinum containing compound. The dendritic polymer platinates may be administered intravenously, orally, parentally, subcutaneously or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The dendritic polymer platinates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.

Abstract: The present invention describes the use of polysaccharides, surfactants, and dendrimers as bioavailability enhancers for oral pharmaceutical compositions. These substances exhert an inhibitory action of the gastrointestinal pump efflux proteins, such as the P-glycoprotein and the MDR protein, responsible for poor drug bioavailability and multidrug resistance. The formulations herein described comprise a medicinally active substance in association with said polysaccharides, surfactants, and dendrimers. They are well tolerated, are not absorbed by the gastrointestinal tract, and increase the bioavailability and the activity of orally administered medicaments, like, e.g. antineoplastic, antiviral, antibiotic, or antidepressant medicaments.

Abstract: Dendritic polymer conjugates which are useful drug delivery systems for carrying platinum containing anti-tumor agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to a platinum containing compound capable of interacting with the functional groups, contacting the dendritic polymer with the platinum containing compound, and reacting the dendritic polymer with the platinum containing compound. The dendritic polymer platinates may be administered intravenously, orally, parentally, subcutaneously or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The dendritic polymer platinates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.

Abstract: Dendritic polymer conjugates which are useful drug delivery systems for carrying platinum containing anti-tumor agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to a platinum containing compound capable of interacting with the functional groups, contacting the dendritic polymer with the platinum containing compound, and reacting the dendritic polymer with the platinum containing compound. The dendritic polymer platinates may be administered intravenously, orally, parentally, subcutaneously or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The dendritic polymer platinates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.

Abstract: Antineoplastic dendritic polymer conjugates which are useful drug delivery systems for carrying antineoplastic agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to an antineoplastic agent capable of interacting with the functional groups, and contacting the dendritic polymer with the antineoplastic agent. The preferred platin-based analogues of the antineoplastic agents conjugated to the dendritic polymer may be administered intravenously, orally, parentally, subcutaneously, intramuscularly, intraarterially or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The antineoplastic dendritic polymer conjugates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.

Abstract: Degradable polyacetal polymers and functionalized degradable polyacetal polymers have properties favorable for use in pharmaceutical and biomedical applications. The degradable polyacetal polymers are relatively stable at physiological pH with favorable biodistribution profiles, and degrade readily in low pH conditions. Conjugates of the polymers with drugs, especially anticancer drugs, and methods of treatment of cancer.

Abstract: Dendritic polymer conjugates which are useful drug delivery systems for carrying platinum containing anti-tumor agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to a platinum containing compound capable of interacting with the functional groups, contacting the dendritic polymer with the platinum containing compound, and reacting the dendritic polymer with the platinum containing compound. The dendritic polymer platinates may be administered intravenously, orally, parentally, subcutaneously or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The dendritic polymer platinates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.

Abstract: Prodrugs which can be activated by enzymes, are formulated for sequential administration, with enzyme conjugates. Either or each component comprises a polymeric carrier which allows it to be directed preferentially to the target tissue. A new polymer-prodrug conjugate is cleavable by cathepsin-B or othe invention is of particular utility for targeting solid tumours.

Abstract: A polymer-drug conjugate, in which the polymer is the polysaccharide dextrin, linked directly or indirectly to the drug, is effective to deliver the drug to a target site and is biodegradable. The conjugate may be prepared by succinoylating dextrin followed by reaction with the drug or a derivative thereof.

Abstract: A polymer-platinum compound for use in tumor treatment is described. The compound is composed of a biodegradable diamido-diamine polymer linked to a platinum species. The platinum species is released from the polymer to yield a platinum species having anti-tumor activity.

Abstract: A polymer-platinum compound for use in tumor treatment is described. The compound is composed of a polymer backbone having platinum-containing side chains spaced along the polymer backbone. The side chains are composed of an oligopeptide attached at one end to the backbone and at the other end to the platinum compound.

Abstract: A conjugate of a carrier polymer and aziridine ring containing mitomycin (MMC) drug molecules is prepared by coupling the MMC molecules via their aziridine imino groups to spacer groups that terminate in protected amino groups, deprotecting said amino groups, recovering and purifying the spacer-MMC derivatives, and then coupling these derivatives via said deprotected amino groups to the carrier polymer. Alternatively, the MMC may first be treated with an activating agent, e.g. carbodiimidazole, to form an activated MMC derivative which is then coupled directly to spacer groups linked to the carrier polymer.

Abstract: The invention is an alginate-bioactive agent conjugate connected via an acid labile biodegradable spacer linkage. The conjugate is effective for delivering bioactive agents to targets existing in low-pH environments, either at the target surface or in the target interior.

Abstract: A polymeric drug comprising an inert synthetic polymeric carrier combined through aminoacid or peptide spacers with a bioactive molecule, a targeting moiety, and an optional cross-linkage, comprises:(a) 5.0 to 99.7 mol % of units derived from N-(2-hydroxypropyl)methacrylamide,(b) 0.2 to 20.0 mol % of units derived from an N-methylacrylcylated peptide, the peptide groups being bound to a bioactive moiety,(c) 0.1 to 94.8 mol % of units derived from N-methacrylamide, N-methacrylic acid or an N-methacrylolated aminoacid or peptide, to which are bound a determinant capable of interacting with specific receptors on cell surfaces,(d) optionally, 0 to 5 mol % of units derived from an N-methacryloylated peptide, the peptide groups being bound to a linking group which is similarly to a similar peptide group attached to another polymer chain, and(e) optionally, as a bioassay label, 0 to 2 mol % units derived from N-methyacryloylated tyrosinamide.