专利号:US-8734846-B2 优先权日:2008-06-16 标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles 发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS 权利人:BIND BIOSCIENCES INC 摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.
专利号:US-2008051323-A1 优先权日:2004-08-21 标 题 :Chloroquine drug compositions and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:US-2007203079-A1 优先权日:2005-11-21 标题:Methods of using small molecule compounds for neuroprotection 发明人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG 权利人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG 摘要:Methods are provided for preventing neurodegeneration and neuronal loss by administering compositions comprising small molecule compounds with the effect of preventing neurodegeneration and neuronal loss. In one aspect of the invention, the methods and compositions are also useful for treating neurodegenerative diseases. Small molecule compounds provide an important treatment option because of their stability, ease of use in both manufacture and formulation, ease of administration, and patient compliance. The small molecule compound compositions of the present invention may include topoisomerase II inhibitors, bacterial transpeptidase inhibitors, calcium channel antagonists, cyclooxygenase inhibitors, folic acid synthesis inhibitors, or sodium channel blockers and functional analogues thereof that have an effect on neurodegeneration. The compositions of the present invention may be administered prophylactically before the onset of clinical symptoms or after clinical symptoms of a neurodegenerative disease have manifested.
专利号:US-2007060499-A1 优先权日:2005-09-15 标 题 :Chloroquine combination drugs and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
专利号:US-2006040879-A1 优先权日:2004-08-21 标 题:Chloroquine coupled nucleic acids and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions and methods for preparing chloroquine-coupled nucleic acid compositions. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the nucleic acid needs to be released, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a nucleic acid directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing nucleic acids for therapeutic or other medical uses. The invention also discloses nucleic acid carrier compositions that are coupled to targeting molecules for targeting the delivery of nucleic acids to their site of action.