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-4363816-A 优先权日:1981-02-02 标 题 :Tricyclic pyrroles, their compositions and their use 发明人:SENN-BILFINGER JOERG 权利人:BYK GULDEN LOMBERG CHEM FAB 摘要:1,4,9,10-tetrahydropyrrolo[3,2-b][1,5]benzodiazepin-10-ones have been found to provide excellent protection for the stomach and intestines of warm-blooded animals. They are useful for the treatment and prophylaxis of such maladies as gastritis, acute and chronic ulcus ventriculi and hyperacid gastric irritation. The compounds are administered enterally or parenterally, usually in a standard dosage form. The disclosure includes key intermediates, methods of synthesis, compositions and use.
专利号:US-4317823-A 优先权日:1979-08-03 标题 :Pyrazolobenzodiazepinones, their intermediates, their compositions and their use 发明人:RAINER GEORG 权利人:BYK GULDEN LOMBERG CHEM FAB 摘要:1-(Lower)alkyl-4-(substituted)aminoalkylcarbonyl-1,4,9,10-tetrahydropy razolo[4,3-b][1,5]benzodiazepin-10-ones are useful, e.g., to protect warm blooded animals against the formation of gastric ulcers. They are active ingredients in otherwise conventional medicament compositions administered enterally or parenterally in standard dosage forms. Their synthesis, their novel intermediates and their acid-addition salts are described.
1: Sarbhjit K, S K B, Parmjit K, Surinder B. To compare the effect of camylofin dihydrochloride (anafortin) with combination of valethamate bromide (epidosin) and hyoscine butyl-N-bormide (buscopan) on cervical dilation. J Clin Diagn Res. 2013 Sep;7(9):1897-9. doi: 10.7860/JCDR/2013/6231.3345. Epub 2013 Jul 22. 2: Rohwer AC, Khondowe O, Young T. Antispasmodics for labour. Cochrane Database Syst Rev. 2013 Jun 5;(6):CD009243. doi: 10.1002/14651858.CD009243.pub3. Review. doi: 10.1002/14651858.CD009243.pub2. Review. doi: 10.3109/10611860903572933. German. German. German. French. German. German. German. German.
合成参考文献
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