专利号:US-4381301-A 优先权日:1980-05-07 标题 :Substituted tricyclic thieno compounds, their synthesis, their use, their compositions and their medicaments 发明人:RAINER GEORG 权利人:BYK GULDEN LOMBERG CHEM FAB 摘要:Substituted thienobenzodiazepinones of the general formula I (I) [wherein R1 denotes a hydrogen atom (-H) or an alkyl radical with 1 to 4 carbon atoms; R2 represents a halogen atom (halo) or has one of the meanings of R1; R3 denotes a halogen atom (halo) or the group -N(R4)R5; R4 denotes an alkyl radical with 1 to 4 carbon atoms or an alkenyl radical with 3 to 5 carbon atoms; R5 has one of the meanings of R4 or represents the group -(CH2)m-N(R6)R7; or R4 and R5, together with the nitrogen atom to which both are bonded, denote a morpholino group, a pyrrolidino group, a piperidino group, a hexahydroazepin-1-yl group, a piperazin-1-yl group (which is optionally substituted in the 4-position by a methyl, ethyl or benzyl group), a 2,4-dimethylpiperazin-1-yl group, or a hexahydro-1H-1,4-diazepin-1-yl group (which is substituted in the 4-position by a methyl or ethyl group); R6 denotes an alkyl group with 1 to 4 carbon atoms; R7 denotes an alkyl group with 1 to 4 carbon atoms; A denotes a straight-chain or branched alkylene group with 1 to 5 carbon atoms; and m denotes 2 or 3] and their acid-addition salts are new compounds. They either have a protective action on the stomach and intestine and are suitable for treating illnesses based on disorders of the stomach or intestine, or they are intermediates for preparing products having protective action. Processes for the preparation of the new pharmacologically-active compounds and of the intermediate products are presented.
专利号:US-2023271983-A1 优先权日:2020-07-29 标题 :Functionalized isonitriles and products, preparation and uses thereof 发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA 权利人:UNIV SANTIAGO COMPOSTELA 摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.
专利号:US-8933207-B2 优先权日:2010-07-28 标 题 :Drug-ligand conjugates, synthesis thereof, and intermediates thereto 发明人:CHEN ZHIYU; LANCASTER THOMAS M; ZION TODD C 权利人:CHEN ZHIYU; LANCASTER THOMAS M; ZION TODD C; SMARTCELLS INC 摘要:The present invention relates to methods for synthesizing compounds of formula I or pharmaceutically acceptable salts thereof: I wherein each of X, Alk 1 , Alk 2 , and W are as defined and described herein.
专利号:JP-2007520493-A 优先权日:2004-02-03 标 题 :Synthesis of cyanoiminobenzimidazole
专利号:US-6025177-A 优先权日:1998-03-30 标题 :Asymmetric grignard synthesis with cyclic 1,2 aminoalcohols 发明人:SENANAYAKE CHRIS HUGH; BAKALE ROGER P; FANG QUN KEVIN; GROVER PAUL TIMOTHY; HEEFNER DONALD L; ROSSI RICHARD F; WALD STEPHEN ALAN 权利人:SEPRACOR INC 摘要:Processes for preparing a single enantiomer of an alpha , alpha -disubstituted- alpha -hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. Intermediates useful in the process are also disclosed.
专利号:US-2013131310-A1 优先权日:2010-07-28 标题 :Drug-ligand conjugates, synthesis thereof, and intermediates thereto 发明人:KANE JOHN; LANCASTER THOMAS M; ZION TODD C 权利人:KANE JOHN; LANCASTER THOMAS M; ZION TODD C 摘要:The present invention relates to methods for synthesizing compounds of formula I or pharmaceutically acceptable salts thereof: (I) wherein each of X, Alk, and W are as defined and described herein.
1: Klaphajone J, Kitisomprayoonkul W, Sriplakit S. Botulinum toxin type A injections for treating neurogenic detrusor overactivity combined with low-compliance bladder in patients with spinal cord lesions. Arch Phys Med Rehabil. 2005 Nov;86(11):2114-8. Swedish.
合成参考文献
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 参考文献:10.1007/bf00482998 摘要:Fujimoto K, Ogawa KS, Ogawa K. Gastric K+-stimulated p-nitrophenylphosphatase cytochemistry. Histochemistry and Cell Biology. 1986 Jul;84(4-6):600–8. doi: 10.1007/bf00482998.