专利号:US-2009253913-A1 优先权日:2008-03-06 标题:Process for the preparation of sorafenib and salts thereof 发明人:ROSSETTO PIERLUIGI; MACDONALD PETER LINDSAY; CANAVESI AUGUSTO 权利人:ROSSETTO PIERLUIGI; MACDONALD PETER LINDSAY; CANAVESI AUGUSTO 摘要:Methods for the synthesis of the N-carbamoyl imidazole (I) and its 1:1 adduct with imidazole are provided. Methods for the preparation of these crystalline intermediates in a high state of purity are also provided. These intermediates react cleanly under mild conditions to produce sorafenib in high yield and purity, without generating difficult-to-remove impurities.
专利号:US-8735391-B2 优先权日:2008-09-26 标 题 :Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods 发明人:AUBE JEFFREY; ROTH BRYAN L; GHOSH PARTHA; FRANKOWSKI KEVIN J 权利人:AUBE JEFFREY; ROTH BRYAN L; GHOSH PARTHA; FRANKOWSKI KEVIN J; UNIV KANSAS 摘要:A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.
专利号:WO-2024168196-A1 优先权日:2023-02-08 标 题:Systems and methods for enzymatic synthesis of polynucleotides containing non-standard nucleotide basepairs 发明人:MARCHAND JORGE; KAWABE HINAKO 权利人:UNIV WASHINGTON 摘要:Systems and methods for generating defined base pairs in a sequence-defined library format that include at least one non-standard nucleotide in a base pair. Non-standard base pairs can be created using a nucleic acid polymerase ( e.g. , DNA polymerase, RNA polymerase, terminal deoxynucleotide polymerase) for blunt-end tailing addition of the non-standard base, which then can be ligated to another nucleotide end. The nucleotide sequences containing non-standard base pairs can be used to generate libraries for basecalling models of the non-standard base with next-generation sequencing (NGS) platforms and sequencing non-standard nucleotide sequences, including xenonucleotide (XNAs).
专利号:US-6849650-B2 优先权日:1998-02-27 标 题:Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THORSETT EUGENE D; PORTER WARREN J; NISSEN JEFFREY S; LATIMER LEE H; AUDIA JAMES E; DROSTE JAMES 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6399628-B1 优先权日:1996-11-22 标 题 :N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting alpha- amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; REEL JON K; THORSETT EUGENE D; WHITESITT CELIA A 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:EP-0951466-B1 优先权日:1996-12-23 标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:WU JING; TUNG JAY S; THORSETT EUGENE D; PLEISS MICHAEL A; NISSEN JEFFREY S; NEITZ JEFFREY; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; DROSTE JAMES J; HENRY STEVEN S; MCDANIEL STACEY L; SCOTT WILLIAM L; STUCKY RUSSELL D 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds for Formula (I) wherein the substituents are as defined in the claims which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.