专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-6015808-A 优先权日:1993-08-20 标 题 :Synthesis of pharmaceutical compositions with lactams and β-lactams/oxo thia azabicyclo compounds 发明人:THIRUMALACHAR MANDAYAM JEERSAN; NARASIMHAN JR MANDAYAM JEERSAN 摘要:Pharmaceutical compositions with heretofore unknown and enhanced physical, chemical, and biological properties are prepared by combining known biologically active parent compounds with oxo thia azabicyclo compounds, such as lactam and beta -lactam compounds, capable of rapidly transporting the parent compounds in undegraded form to their target sites of action. A process for combining the parent compound with beta -lactam compounds consists of dissolving the parent compound in a polar solvent, adding a beta -lactam compound, incubating the resulting mixture, followed by drying, and subjecting the remaining solid material to solvent washing or extraction to further purify the new pharmaceutical composition. The new pharmaceutical composition possesses the biological and therapeutic activity of the parent compound and the barrier penetrating characteristics of the beta -lactam compound, which results in improved pharmacodynamics, including bioavailability, and an improved chemotherapeutic index, such that lower amounts of the parent may be used to avoid the toxic effects of the parent compound. Some of the new pharmaceutical compounds provide for the first time parent compounds in an orally administerable form.
专利号:US-5656743-A 优先权日:1992-02-19 标 题 :Oligonucleotide modulation of cell growth 发明人:BUSCH HARRIS; BENNETT CLARENCE FRANK; PERLAKY LASZLO; SAIJO YASUO; BUSCH ROSE K 权利人:BAYLOR COLLEGE MEDICINE; ISIS PHARMACEUTICALS INC 摘要:Oligonucleotides capable of inhibiting the production of proliferation-associated proteins are provided. Oligonucleotides designed to be hybridizable with nucleic acids encoding nucleolar proteins are believed to be therapeutically useful. Certain of such oligonucleotides, hybridizable to portions of the gene coding for p120, especially the 3' untranslated region, were made and found to inhibit the synthesis of p120. The oligonucleotides of the invention are useful for the treatment of diseases characterized by hyperproliferation of cells such as malignancies, inflammatory and cardiovascular diseases. Treatment of human breast cell carcinoma, human epitheloid cervix carcinoma, human amelanotic melanoma, human renal cell carcinoma and other tumors are indicated.
专利号:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:US-2007160574-A1 优先权日:2000-04-12 标题 :Design of CXC chemokine analogs for the treatment of human diseases 发明人:MERZOUK AHMED; SALARI HASSAN 权利人:MERZOUK AHMED; SALARI HASSAN 摘要:The present invention generally relates to the design, preparation, derivation, and use of mimetics of CXC chemokines (CXCL1-CXCL17) in the prevention, treatment, and ameliorization of a wide variety of diseases and disorders. Generally speaking, this invention is directed to the design, synthesis, and use of chemokine analogs which bind to CXC chemokine receptors CXCR1-CXCR7, such that the analogs can be designed to affect the activity of the receptor, either as an agonist or an antagonist. The analogs can be useful for treating a wide variety of diseases and disorders, and can also serve as an adjunct to the treatment of a variety of diseases and disorders.
专利号:WO-2025058418-A1 优先权日:2023-09-15 标 题:Magnetic rna nanoparticles for mrna delivery for expression of therapeutic protein 发明人:CHO HYEON-YEOL; YUN YEOCHAN 权利人:UNIV KOOKMIN IND ACAD COOP FOUND 摘要:The present invention relates to magnetic RNA nanoparticles for mRNA delivery for the expression of therapeutic proteins in cells. The features and advantages of the present invention are summarized as follows: (a) The present invention provides magnetic RNA nanoparticles for mRNA delivery for the expression of a therapeutic protein, and a method for synthesizing same. (b) The magnetic RNA nanoparticles for delivering mRNA for the expression of therapeutic proteins according to the present invention can express a therapeutic protein by delivering mRNA produced in vitro into cells. (c) According to the present invention, it is possible to obtain magnetic nanoparticles for mRNA delivery, which are uniformly dispersed and homogenous in size, avoiding aggregation during synthesis. (d) Compared to RNA nanoparticles without a magnetic nanoparticle core, the magnetic RNA nanoparticles for mRNA delivery according to the present invention exhibit remarkably high RNA delivery efficiency. (e) The magnetic nanoparticles for mRNA delivery according to the present invention have a remarkably high intracellular protein expression rate compared to lipofectamine.
参考文献:10.1093/jmedent/12.5.573 摘要:Van Peenen PF, Joseph PL, Atmosoedjono S, Irsiana R, Saroso JS. Isolation of Japanese encephalitis virus from mosquitoes near Bogor, West Java, Indonesia. J Med Entomol. 1975 Dec 30;12(5):573–4. doi: 10.1093/jmedent/12.5.573.