专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-12384803-B2 优先权日:2020-02-24 标 题:Non-cryogenic synthesis of heteroatom-bridge precursors of metal-ligand complex catalysts 发明人:DO HIEN Q; FONTAINE PHILIP P; KRASOVSKIY ARKADY L; SPENCER LIAM P; OGAWA KELLI A; LESNIEWSKI DANIEL K; ANDERSON RUSSELL W 权利人:DOW GLOBAL TECHNOLOGIES LLC 摘要:Embodiments are directed to a metal-ligand complex catalyst precursor, (L1)(L2)X(R1)(R2), and methods for producing the same from a compound of formula Q2X(R1)(R2). L1 and L2 are independently —R3—Z1 or —R4—Z1. R1 and R2 are independently selected from a hydrogen atom, (C1-C40)hydrocarbyl and, optionally, R1 and R2 are connected to form a ring having from 3 to 50 atoms in the ring, excluding hydrogen atoms. X is Si, Ge, Sn, or Pb. Each Q is independently Ar1—Y1R3— or Ar2—Y2—R4—. R3 and R4 are independently selected from —(CRC2)m—, where m is 1 or 2, and where each RC is independently selected from the group consisting of (C1-C40)hydrocarbyl, (C1-C40)heterohydrocarbyl, and —H. Y1 and Y2 are independently S, Se, or Te. Ar1 and Ar2 are independently (C6-C50)aryl. Ar1—Y1—R3— and Ar2—Y2—R4— are not identical. Each Z1 is independently selected from Cl, Br, and I.
专利号:US-9090922-B2 优先权日:2010-11-30 标题:Process for the preparation of nebivolol 发明人:MAURO SANDRO; FATTORI DANIELA; D ANDREA PIERO; CIPOLLONE AMALIA; D ANDREA ENZO; ERCOLANO CARMELA 权利人:MAURO SANDRO; FATTORI DANIELA; D ANDREA PIERO; CIPOLLONE AMALIA; D ANDREA ENZO; ERCOLANO CARMELA; MENARINI INT OPERATIONS LU SA 摘要:The present invention relates to a novel process for the synthesis of the Nebivolol product depicted in Scheme 1, comprised of a reduced number of high-yield steps, and characterized by the enzymatic resolution of the chroman ester precursor.
专利号:US-2009099200-A1 优先权日:2005-06-09 标题 :Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS 权利人:LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS 摘要:Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
专利号:US-7405310-B2 优先权日:2001-03-05 标 题:Non-nucleoside reverse transcriptase inhibitors 发明人:LINDSTROM STEFAN; SAHLBERG CHRISTER; WALLBERG HANS; KALYANOV GENAIDY; ODEN LOURDES SALVADOR; NAESLUND LOTTA 权利人:MEDIVIR AB 摘要:This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.
专利号:EP-4110787-B1 优先权日:2020-02-24 标 题:Non-cryogenic synthesis of heteroatom-bridge precursors of metal-ligand complex catalysts