Abstract: Epimers and isomers of tetrazole-containing rapamycin analogs and a pharmaceutically acceptable salt or prodrug thereof, are immunomodulatory agents and are useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosis, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such isomers and epimers of tetrazole containing rapamycin and 42-Epi rapamycin analogs is in medicated devices and local vascular delivery wherein the stability and lipid solubility and subsequently diffusion through tissue and cell membranes are essential to the success of rapamycin containing combination devices.

Abstract: A rapamycin analog with an antioxidant moiety or a pharmaceutically acceptable salt or prodrug thereof, is an immunomodulatory agent and is useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed Are cancer-, fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such antioxidant moiety containing rapamycin analog is in medicated devices wherein the stability and resistance to oxidative processes are essential to the success of rapamycin containing combination devices.

Abstract: Isomers and 42-epimers of rapamycin alkyl ether analogs and pharmaceutically acceptable salts or prodrugs thereof, are immunomodulatory agents and are useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosis, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such isomers and 42-epimers of rapamycin alkyl ether analogs is in medicated devices and local vascular delivery wherein the stability and lipid solubility and subsequently diffusion through tissue and cell membranes are essential to the success of rapamycin containing combination devices.

Abstract: 15-C isomers of rapamycin and of 42-C Epi rapamycin, and pharmaceutically acceptable salts or prodrugs thereof are disclosed. These compounds are potential immunomodulatory and anti-inflammatory agents, and may be useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions comprising the invented isomers, and methods of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of these novel rapamycin derivatives are in implantable medicated devices wherein the prolonged presence of these compound locally are essential to the success of drug containing combination devices.

Abstract: Epimers and isomers of tetrazole-containing rapamycin analogs are immunomodulatory agents and are useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosis, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. It is preferred to use a combination of native rapamycin and its tetrazole containing isomers and epimers. One particular preferred application of such a combination of rapamycin and its tetrazole containing isomers and epimers is in medicated devices and local vascular delivery wherein the stability and lipid solubility and subsequently diffusion through tissue and cell membranes of the tetrazole isomers and epimers are essential to the success of the combined rapamycin formulation.

Abstract: Isomers and 42-epimers of rapamycin ester analogs and pharmaceutically acceptable salts or prodrugs thereof, are immunomodulatory agents and are useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosis, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such isomers and 42-epimers of rapamycin ester analogs is in medicated devices and local vascular delivery wherein the stability and lipid solubility and subsequently diffusion through tissue and cell membranes are essential to the success of rapamycin containing combination devices.

Abstract: The present invention discloses a block copolymer having a hydrophobic block, a hydrophilic block, and a biologically active block. The biologically active block is directly adjacent to the hydrophilic block. Preferably, the block copolymer is prepared through reversible addition fragmentation transfer (RAFT) polymerization. The present invention also discloses a coating composition comprising the inventive block copolymer. The coating composition may be used for applying on at least a portion of one surface of an article. Moreover, the present invention discloses an article having the inventive coating composition thereon. Preferably, the article is a medical device or a component of a medical device.

Abstract: The present invention discloses a tri-branched copolymer comprising a hydrophobic domain, a hydrophilic domain, a biologically active moiety, and an alkyl core of 2 to 10 carbon atoms. The hydrophobic domain, the hydrophilic domain, and the biologically active moiety are separately linked to the alkyl core of 2 to 10 carbon atoms through three functional groups, wherein said three functional groups are independently the same or different. Preferably, the tri-branched copolymer is prepared through reversible addition fragmentation transfer (RAFT) polymerization and conjugation reactions. The present invention also discloses a coating composition for applying on at least a portion of one surface of an article. The coating composition comprises the inventive tri-branched copolymer. In another aspect, the present invention discloses an article having the inventive coating composition thereon. Preferably, the article is a medical device or a component of a medical device.

Abstract: The present invention discloses a biocompatible coating composition that can be photo crosslinked when exposed to long wavelength ultraviolet light. The biocompatible coating composition comprises at least one biocompatible polymer having a photoactive moiety covalently attached thereto, and a biologically active molecule having a photoactive moiety covalently attached thereto. The photoactive moiety covalently attached to the biologically active molecule and the photoactive moiety covalently attached to the at least one biocompatible polymer are the same or different, and absorb and respond to ultraviolet light having a wavelength band of about 300 nm or above. Preferably, the photoactive moiety is a chemical moiety derived from thioxanthone. The inventive biocompatible coating composition can be applied on at least a portion of one surface of an article.

Abstract: The present invention relates to drug-eluting articles with multiple polymeric coatings arranged and constructed to provide improved drug release profiles. Specifically, the present invention relates to drug-eluting articles that each comprises a substrate, a first polymeric layer over said substrate, and a second polymeric layer over said first polymeric layer. The first polymeric layer comprises at least a first biocompatible polymer and at least a first pharmacologically active compound that is encapsulated in the first biocompatible polymer. The second polymeric layer comprises at least a second biocompatible polymer having a degradability that is higher than that of the first biocompatible polymer.

Abstract: The present invention discloses a radiographic contrasting agent containing multiple aromatic groups, each of which is substituted with at least three halogen atoms. The radiographic contrasting agent can initiate a polymerization process. The present invention also discloses a radio-opaque polymeric material that comprises a biodegradable polymer having at least one radiographic contrasting moiety covalently attached thereto. The radio-opaque polymeric material provides enhanced contrasting intensity in radiographic imaging. The radio-opaque polymeric material can be applied on at least a portion of one surface of a medical device. The radio-opaque polymeric material can also be used to construct a medical device, a component thereof, or a portion of a component thereof.

Abstract: A biocompatible metallic material may be configured into any number of implantable medical devices, including intraluminal stents. The biocompatible metallic material may comprise a magnesium alloy. The magnesium alloy implantable medical device may be designed to degrade over a given period of time. In order to control the degradation time, the device may be coated or otherwise have affixed thereto one or more coatings, one of which comprises a material for controlling the degradation time and maintain a pH neutral environment proximate the device. Additionally, therapeutic agents may be incorporated into one or more of the coatings on the implantable medical device.

Abstract: The present invention discloses an organic radiographic contrasting agent containing an aliphatic or alicyclic backbone and multiple halogen-substituted aromatic groups. Each of the halogen-substituted aromatic groups in the radiographic contrasting agent is substituted with at least three halogen atoms and is covalently attached to the aliphatic or alicyclic backbone. The present invention also discloses a radio-opaque polymeric material comprising the radiographic contrasting agent and at least one polymer. The radiographic contrasting agent is physically admixed with the at least one polymer or physically embedded or dispersed in the at least one polymer. The radio-opaque polymeric material provides enhanced contrasting intensity in radiographic imaging. The radio-opaque polymeric material can be applied on at least a portion of one surface of a medical device. The radio-opaque polymeric material can also be used to construct a medical device, a component thereof, or a portion of a component thereof.

Abstract: The present invention relates to nano- and/or micro-particulate formulations that can be locally injected into arterial walls at or near target sites to achieve a prolonged and sufficiently high local concentration of at least one pharmacologically active agent for treatment of vascular diseases, such as, for example, restenosis, vulnerable plaque, aneurysm, and stroke. Specifically, each formulation comprises biocompatible and biodegradable nano-particles and/or micro-particles loaded with the pharmacologically active agent and d-alpha-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS). The formulations can be formed by a solvent evaporation/extraction process or a supercritical CO2 extraction process that uses vitamin E TPGS as an emulsifier. Further, vitamin E TPGS can be used as a stabilizer for the pharmacologically active agent in the final drug formulation, as well as a release modulation to control release of the pharmacologically active agent.

Abstract: The present invention provides an amphiphilic coating material for applying on at least a portion of one surface of an article. The amphiphilic coating material comprises a polymer having a hydrophobic backbone derived from a vinyl moiety and hydrophilic pendent chains derived from a polyethylene oxide moiety. The present invention also provides an article having an amphiphilic coating thereon. The hydrophobic backbone derived from a vinyl moiety adheres to at least one surface of an article. The hydrophilic pendent chains derived from a polyethylene oxide moiety extend from the hydrophobic backbone and form a three-dimensional network.

Abstract: The present invention provides an amphiphilic coating material for applying on at least a portion of one surface of an article. The amphiphilic coating material comprises a copolymer containing one or more alkyl methacrylate or alkyl acrylate co-monomer units; one or more vinyl acetate co-monomer units; and up to 40% mole of polyethylene oxide substituted methacrylate co-monomer units. Optionally, one or more biologically active molecules may be covalently bonded to the polyethylene oxide substituted methacrylate co-monomer units. The present invention also provides an article having the inventive amphiphilic coating thereon.

Abstract: Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the prevention of thrombosis. The drugs, agents, and/or compounds may also be utilized to treat specific disorders, including vulnerable plaque. Therapeutic agents may also be delivered to the region of a disease site.

Abstract: Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic drugs, agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the formation of blood clots. The drugs, agents, and/or compounds may also be utilized to treat specific diseases, including vulnerable plaque. Therapeutic agents may also be delivered to the region of a disease site.

Abstract: An intralumen medical device comprising anti-inflamatory and anti-thrombotic or anti-coagulant drugs, agents or compounds may be utilized in the treatment of vascular disease. The intralumen medical device is selectively coated with the drugs, agents or compounds for local delivery, thereby increasing their effectiveness and reducing potential toxicity associated with systemic use. The selective coating is utilized to ensure that the specific drugs, agents or compounds come into contact with or are delivered to the appropriate tissues and/or fluids for maximum effectiveness.

Abstract: Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic drugs, agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the formation of blood clots. Various materials and coating methodologies may be utilized to maintain the drugs, agents or compounds on the medical device until delivered and positioned.