摘要:
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.
摘要:
The present invention relates to novel therapeutic and diagnostic arrays. More particularly, the present invention is directed to dendrimer based multifunctional compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems generally comprise two or more separate components for targeting, imaging, sensing, and/or triggering release of a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
摘要:
A novel process for preparing poly(2-isopropenyl-2-oxazoline or oxazine) and its methyl methacrylate copolymer, which are useful as water borne curing agents, particularly in the non-stick coating industry. The process converts commercially available poly(methyl methacrylate) into poly(2-isopropenyl-2-oxazoline or oxazine) polymers or copolymers with methyl methacrylate, while circumventing the use of the highly toxic monomer, 2-isopropenyl-2-oxazoline or oxazine. The process involves converting a poly(methacrylic ester) to the corresponding poly(.beta.-hydroxy-N-ethyl or propyl methacrylamide) and activating the ring-forming .beta.-hydroxy-N-ethyl or propyl methacrylamide moiety to form an oxazoline or oxazine ring.
摘要:
Cyclic peptides, such as 1,4,8,11-tetraazacyclotetradecane-5,12-dione, that are useful chelation agents for metals are prepared by contacting an acrylic acid ester and a 1,2-alkylenediamine.
摘要:
Dense star polymers having terminal group densities greater than conventional star polymers exhibit greater and more uniform reactivity than their corresponding conventional star polymers. For example, a third generation, amine-terminated polyamidoamine dense star polymer prepared from ammonia, methyl acrylate and ethylenediamine has 1.24.times.10.sup.-4 amine moieties per unit volume (cubic Angstrom units) in contrast to the 1.58.times.10.sup.-6 amine moieties per unit volume contained by a conventional star polymer. Such dense star polymers are useful as demulsifiers for oil/water emulsions, wet strength agents in the manufacture of paper, and agents for modifying viscosity in aqueous formulations such as paints.
摘要:
The level of residual 2-isopropenyl-2-oxazoline monomer in polymers prepared therefrom can be reduced by reaction of the protonated salt of the monomer with a variety of nucleophiles. The products of the reaction with the monomer are much less toxic than the 2-isopropenyl-2-oxazoline and the utility of the polymer is thereby enhanced. The reaction product of 2-isopropenyl-2-oxazoline and H.sub.2 SO.sub.3 is itself novel and useful.
摘要翻译:由其制备的聚合物中残留的2-异丙烯基-2-恶唑啉单体的水平可以通过单体的质子化盐与各种亲核试剂的反应来降低。 与单体的反应产物的毒性远低于2-异丙烯基-2-恶唑啉,从而提高了聚合物的用途。 2-异丙烯基-2-恶唑啉和H 2 SO 3的反应产物本身是新颖的和有用的。
摘要:
Compounds represented by the formula: ##STR1## and addition polymers thereof where m is an integer from 2 to about 10, X-- is chlorine, hydroxy, carboxy or:--AC--R).dbd.CH.sub.2--R is hydrogen or methyl, --R--' is an ethylene or propylene group and--AC--R).dbd.CH.sub.2is one of: ##STR2## These compounds and their addition polymers form complexes with alkali metal or alkaline earth metal salts and permit the concentration of aqueous solutions of said salts. For example, a compound of the formula: ##STR3## is polymerized with an azobis (isobutyronitrile) catalyst to form addition polymers of the repeating unit ##STR4## When cross-linked, rendering it water-insoluble, such an addition polymer concentrates an aqueous solution of sodium chloride when contacted with same at about 0.degree. C.
摘要:
N-(haloalkyl)sulfonamides represented by the formula ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.20 aryl, alkaryl, aralkyl or alkyl group; R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen or methyl groups; n is the integer 0 or 1 and X is a chloro, bromo or iodo group, are prepared by reacting an N-(haloalkyl)sulfonyl imide with a C.sub.1 -C.sub.6 alkanol.
摘要:
Poly(ester-acrylate) and poly(ester/epoxide) dendrimers. These materials can be synthesized by utilizing the so-called “sterically induced stoichiometric” principles. The preparation of the dendrimers is carried out by reacting precursor amino/polyamino-functional core materials with various branch cell reagents. The branch cell reagents are dimensionally large, relative to the amino/polyamino-initiator core and when reacted, produce generation=1 dendrimers directly in one step. There is also a method by which the dendrimers can be stabilized and that method is the reaction of the dendrimers with surface reactive molecules to pacify the reactive groups on the dendrimers.