专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-2024336559-A1 优先权日:2021-10-06 标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids 发明人:OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.
专利号:US-12102615-B2 优先权日:2018-04-05 标 题:Synthesis of novel xylose free occidiofungin analogues and methods of using them 发明人:SMITH JAMES L; GENG MENGXIN; RAVICHANDRAN AKSHAYA; ORUGUNTY RAVI 权利人:TEXAS A & M UNIV SYS; SANO CHEMICALS 摘要:The subject invention pertains to methods for producing novel occidiofungin analogues lacking xylose (OF-Δxyl analogue). OF-Δxyl analogues can contain aldehyde, amine, triazole, or hydrazones. The aldehyde, amine, triazole or hydrazone containing analogues of OF-Δxyl can be further modified by substitution with additional functional groups. Various OF-Δxyl analogues described herein have reduced inflammation and toxicity and superior pharmacological properties compared to the natural occidiofungins. Accordingly, certain embodiments of the invention provide methods of treating or preventing fungal infections by administering to the subjects in need thereof the OF-Δxyl analogues described herein.
专利号:US-2023288116-A1 优先权日:2022-03-14 标 题:Large scale synthesis of pharmaceutical and biologic formulations using thin film freezing 发明人:OWENS III DONALD E; KOLENG JR JOHN J 权利人:TFF PHARMACEUTICALS INC 摘要:The invention encompasses methods for the large-scale (preferably under cGMP or cGLP standards) preparation of micron-sized or submicron-sized particles including pharmaceutical or biologic active agents. The systems and methods include a cryogenic cooling system including a novel shroud that enhances the cooling effects thereby reducing product loss and increasing product yields.
专利号:US-9382288-B2 优先权日:2010-10-06 标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action 发明人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO 权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG 摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).
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