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专利信息

专利号:US-3595883-A
优先权日:1969-06-16
标 题 :Process for the preparation of 14beta-hydroxy - 17 -keto - 15 - androstenes and novel intermediates produced thereby
发明人：AFONSO ADRIANO
权利人:SCHERING CORP
摘要:14B-HYDROPEROXY-15-ANDROSTEN-17-ONES, PREPARED BY THE ACTION OF OXYGEN ON 14-ANDROSTEN-17-ONES, UPON TREATMENT WITH A MILD REDUCING AGENT YEILDS 14B-HYDROXY-15ANDROSTEN-17-ONES, USEFUL INTERMEDIATES IN THE SYNTHESIS OF STERODIAL CARDENOLIDES. PREFERRED SPECIES ARE 14 B-HYDROPEROXY-5A-15 ANDROSTEN3B-OL-17-ONE 3-ACETATE AND THE 5B-EPIMER THEREOF (PREPARED BY THE ACTION OF OXYGEN OR 5A-14-ANDROSTEN-3B-OL17-ONE 3-ACETATE AND THE 5B-EPIMER THEREOF, RESPECTIVELY) EACH OF WHICH, UPON MILD REDUCTION, PREFERABLY WITH TRIETHYL PHOSPHITE, YEILDS 14B-HYDROXY-5A-15-ANDROSTEN-3BOL-17-ONE 3-ACETATE AND THE 5B-EPIMER THEROF, RESPECTIVELY, WHICH ARE USEFUL INTERMEDIATES IN THE SYNTHESIS OF UZARIGENIN AND DIGITOXIGENIN, RESPECTIVELY.

专利号:US-9493461-B2
优先权日:2013-02-07
标 题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
发明人：DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; LAI ZHONG; NARGUND RAVI; MARCANTONIO KAREN; XIAO DONG; BROCKUNIER LINDA L; ZORN NICOLAS; DANG QUN; PENG XUANJIA; LI PENG
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-4743619-A
优先权日:1985-08-29
标 题 :Method of treating hepatitis
发明人：HUNG PAUL P
权利人:AMERICAN HOME PROD
摘要:The invention disclosed herein provides a method of treating an animal infected by hepatitis B virus comprising administering to such infected animal an amount of a rifamycin derivative selected from a group consisting of (a) 3-amino-4-deoxo-4-imino-rifamycin S, (b) 3-amino-4-deoxo-4-[(4-aminophenyl)sulfonyl]amino-rifamycin SV, (c) 4-O-(n-butylsulfonyl)-3-[(1-piperidinylimino)methyl]-rifamycin SV, (d) 4-O-(n-butylsulfonyl)-3-[(4-morpholinylimino)methyl]-rifamycin SV, (e) 3-[(dimethylhydrazono)methyl]-4-O-[(3-phenylpropyl)sulfonyl]-rifamycin SV, and (f) 4-deoxo-N,3-ethylidenimino-4-(methylsulfonyl)amino-rifamycin SV, said amount being effective to alleviate the effects of said hepatitis B virus. Also disclosed is a method of inhibiting the viral polymerase of hepatitis B virus by subjecting said polymerase to an amount of one of the rifamycin derivatives (a)-(f) above, said amount being effective to prevent the synthesis of hepatitis B virus by said viral polymerase. Compounds (b)-(f) described above are novel compounds.

专利号:US-6627744-B2
优先权日:1999-07-02
标 题 :Synthesis of glycodendrimer reagents
发明人：DAVIS BENJAMIN G; JONES JOHN BRYAN; BOTT RICHARD R
权利人:GENENCOR INT
摘要:The present invention relates to a chemically modified mutant protein including a cysteine residue substituted for a residue other than cysteine n a precursor protein, the substituted cysteine residue being subsequently modified by reacting the cysteine residue with a glycosylated thiosulfonate. Also a method of producing the chemically modified mutant protein is provided. The present invention also relates to a glycosylated methanethiosulfonate. Another aspect of the present invention is a method of modifying the functional characteristics of a protein including providing a protein and reacting the protein with a glycosylated methanethiosulfonate reagent under conditions effective to produce a glycoprotein with altered functional characteristics as compared to the protein. In addition, the present invention relates to methods of determining the structure-function relationships of chemically modified mutant proteins. The present invention also relates to synthetic methods for producing thio-glycoses, the thio-glycoses so produced, and to methods for producing glycodendrimer reagents.

专利号:US-5300649-A
优先权日:1991-09-12
标 题 :Process for the production of lactams
发明人：GRIFFITHS GARETH DR; PREVIDOLI FELIX DR
权利人:LONZA AG
摘要:β,γ-unsaturated δ-lactams, especially 2-azabicyclo[2.2.1]hept-5-en-3-one, are produced by Diels-Alder reaction of 1,3-dienes with sulfonyl cyanides and subsequent hydrolysis. The sulfonyl cyanides were formed in situ from cyanogen chloride and the corresponding sulfinates. By the renewed reaction of the sulfinate formed in the hydrolysis of the Diels-Alder adducts with cyanogen chloride, the sulfonyl cyanides are regenerated and a catalytic cyclic process results. The 2-azabicyclo[2.2.1]hept-5-en-3-one is a starting compound in the synthesis of antiviral nucleoside analogs.

专利号:WO-2025077857-A1
优先权日:2023-10-13
标题:Use of prmt5 inhibitor in treatment of tumors or cancers
发明人：YAO BING; GU XIAOHUI; MAO WEIFENG; ASWAD FRED JULLIEN; JOSEPH JAMES DAVID; LI MINGXI
权利人:SHANGHAI APEIRON THERAPEUTICS COMPANY LTD
摘要:The present disclosure describes a novel molecule having protein arginine methyltransferase 5 inhibitory activity, and methods for synthesis and use of a compound. Specifically, the present disclosure describes a compound of formula (I) or a pharmaceutically acceptable salt, hydrate or solvate thereof, and methods for synthesis and use of the compound.