专利号:US-2022098170-A1 优先权日:2019-01-16 标 题 :Process for the synthesis of gepirone 发明人:COLOMBANO GIAMPIERO; BARBERO MAURO; GIOVENZANA GIOVANNI BATTISTA; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of gepirone of formula (I) from 8-(pyrimidin-2-yl)-5,8-diazaspiro[4,5]decan-5-ium bromide. The process according to the invention is economically efficient and easily industrially scalable.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
专利号:US-9458100-B2 优先权日:2012-10-12 标 题:Synthesis and growth regulatory activity of a prototype member of a new family of aminothiol radioprotectors 发明人:FAHL WILLIAM E 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methyl-amino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective aminothiol molecule.
专利号:US-6956131-B2 优先权日:2000-04-13 标 题 :2-amino-3, 4 heptenoic compounds useful as nitric oxide synthase inhibitors 发明人:PITZELE BARNETT S; SIKORSKI JAMES A; WEBBER RONALD KEITH 权利人:PHARMACIA CORP 摘要:The present invention is directed to a compound of formula I: n n nor a pharmaceutically acceptable salt thereof, wherein:n R 2 is selected from the group consisting of H and methyl; and R 2 is selected from the group consisting of H and methyl.n nThe compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.
专利号:US-7320993-B1 优先权日:1997-12-17 标题 :Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents 发明人:BIEDERMANN ELFI; HASMANN MAX; LOESER ROLAND; RATTEL BENNO; REITER FRIEDEMANN; SCHEIN BARBARA; SEIBEL KLAUS; VOGT KLAUS; WOSIKOWSKI KATJA; SCHEMAINDA ISABEL 权利人:ASTELLAS DEUTSCHLAND GMBH 摘要:The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.