CAS: 908-54-3; 4,4'-(Triaz-1-Ene-1,3-Diyl)Dibenzimidamide Bis(2-Acetamidoacetate)

专利信息

专利号:US-2012129939-A1
优先权日:2009-02-26
标题:Polyamine inhibitors for the treatment and prevention of parkinson's disease
发明人：SMALL SCOTT A; LEWANDOWSKI NICOLE; LANDRY DONALD W; DENG SHI-XIANG
权利人:SMALL SCOTT A; LEWANDOWSKI NICOLE; LANDRY DONALD W; DENG SHI-XIANG
摘要:Disclosed herein are methods for treating a disease involving α-synucleic aggregation using (1) a compound which reduces the amount of polyamines in an amount effective to reduce α-synucleic aggregation; (2) a compound which inhibits polyamine synthesis in an amount effective to reduce α-synucleic aggregation; or (3) a compound which inhibits α-synucleic aggregation in an amount effective to reduce α-synucleic aggregation. Also disclosed are methods for reducing the amount of α-synucleic aggregation in a brain cell using (1) a compound which reduces the amount of polyamines in an amount effective to reduce α-synucleic aggregation; (2) a compound which inhibits polyamine synthesis in an amount effective to reduce α-synucleic aggregation; or (3) a compound which inhibits α-synucleic aggregation in an amount effective to reduce α-synucleic aggregation. Disclosed herein are also compounds which can be used in the above described methods.

专利号:WO-2023175036-A1
优先权日:2022-03-16
标 题 :Process for synthesizing poly(spermine acrylamide) and/or poly(spermine acrylamide-co-n-alkylacrylamide) and their application
发明人：MERKEL OLIVIA; ZIMMERMANN CHRISTOPH; ADAMS FRIEDERIKE; BALDASSI DOMIZIA
权利人:UNIV MUENCHEN LUDWIG MAXIMILIANS
摘要:The present invention relates to a process for the synthesis of poly(spermine acrylamide) and/or poly(spermine acrylamide-co-N- alkylacrylamide), the process comprising the following steps: a) Reacting a mixture of N-acryloxysuccinimide with N-alkylacrylamide, and b) Obtaining poly(N-acryloxysuccinimde) polymers, poly(N- alkylacrylamide) polymers and/or copolymers with varying ratios of N- acryloxysuccinimide and N-alkylacrylamide, and c) Treating the obtained polymers and/or copolymers of step b) with at least 0.1 equivalent of tri-boc spermine per N-acryloxysuccinimide- repeating unit and obtaining poly(spermine acrylamide) and/or poly(spermine acrylamide-co-N-alkylacrylamide) polymers.

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-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.

专利号:US-11279734-B2
优先权日:2017-12-01
标 题:Solution-phase affinity selection of inhibitors from combinatorial peptide libraries
发明人：PENTELUTE BRADLEY L; TOUTI FAYCAL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present invention provides novel peptides (e.g., peptides, macrocyclic peptides, mini-proteins) that modulate protein-protein interactions or salts thereof, and methods of making and using the inventive peptides. In some embodiments, the peptides are high affinity inhibitors (e.g., K D of at most 100 nM, at most 10 nM, at most 1 nM) of a protein-protein interaction. In certain embodiments, these peptides interfere with p53-MDM2 binding interactions (e.g., by binding to MDM2 (GenBank® Gene ID: 4193)). In some embodiments, the peptides interfere with the dimerization of the C-terminal domain of the human immunodeficiency virus (HIV) capsid protein (C-CA), comprising residues 146-231 of the HIV capsid protein (e.g., by binding to the C-terminal domain of the HIV capsid protein (C-CA), thereby inhibiting the dimeric interface of HIV capsid protein, thereby inhibiting viral assembly). These inventive peptides were rapidly generated and identified using novel methods described herein comprising combinatorial peptide synthesis and/or solution affinity selection.

专利号:US-2005153913-A1
优先权日:2001-04-10
标 题 :Nucleic acid carrier compositions and methods for their synthesis
发明人：KOSAK KENNETH M
摘要:This invention discloses compositions and methods for preparing pharmaceutical nucleic acid carriers. The compositions comprise a carrier substance coupled to a nucleic acid intercalator whereby the intercalator is coupled by intercalation to the nucleic acid. 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.