专利号:US-12162849-B2 优先权日:2018-12-21 标题 :Synthesis of 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or of the methyl-d3 deuterated form thereof 发明人:HOVEYDA HAMID; DUTHEUIL GUILLAUME 权利人:OGEDA SA 摘要:The present invention relates to a method of synthesis of compound (I), wherein R1 represents methyl or methyl-d3, thus corresponding to 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or to the methyl-d3 deuterated form thereof. These compounds are useful as key intermediates in the synthesis of pharmaceutical compounds, especially fezolinetant and deuterated fezolinetant.
专利号:US-7910623-B2 优先权日:2005-07-22 标 题 :Synthesis of scabronines and analogues thereof 发明人:DANISHEFSKY SAMUEL J; WATERS STEPHEN P 权利人:SLOAN KETTERING INST CANCER 摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-10745354-B2 优先权日:2017-11-01 标题 :Methods for enantioselective allylic alkylation of esters, lactones, and lactams with unactivated allylic alcohols 发明人:STOLTZ BRIAN M; NGAMNITHIPORN AURAPAT; JETTE CARINA I; BACHMAN SHOSHANA; VIRGIL SCOTT C; LACKNER SEBASTIAN 权利人:CALIFORNIA INST OF TECHN 摘要:The present disclosure provides methods for enantioselective synthesis of cyclic and acyclic α-quaternary carboxylic acid derivatives via nickel-catalyzed allylic alkylation.
专利号:US-9475814-B2 优先权日:2011-10-03 标题:Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof 发明人:HOVEYDA HAMID R; DUTHEUIL GUILLAUME; FRASER GRAEME L; ROY MARIE-ODILE; EL BOUSMAQUI MOHAMED; BATT FREDERIC 权利人:EUROSCREEN SA 摘要:The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
专利号:US-2008281094-A1 优先权日:2004-05-10 标题 :Regioselective Functionalisation and Protection of Spirolactams 发明人:NOHEDA MARIN PEDRO; PAJARES MANUEL BERNABE; QUINTANA SERGIO MAROTO; CANTERO NURIA TABARES; ARENAS RAUL BENITO 权利人:ESTEVE LABOR DR 摘要:The invention provides highly functionalised spiro-fused lactams of en formula (I) having a cyclohexane moiety with the desired number of protected or un-protected functional groups or carbonated structures, which are introduced with high stereo and regioselectivity, as well as processes for their obtention. These compounds are useful for the synthesis of abroad range of bioactive molecules, such as condoritols and aminoinositols and their analogues.
专利号:US-7288671-B2 优先权日:1999-05-14 标题:Interleukin-1 and tumor necrosis factor-α modulators, synthesis of said modulators and their enantiomers and methods of using said modulators 发明人:PALLADINO MICHAEL; THEODORAKIS EMMANUEL A 权利人:UNIV CALIFORNIA 摘要:Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-α modulators, and thus are useful in the treatment of various diseases. n nwherein the R groups are defined as follows: if any R 3 -R 5 , R 7 , R 8 , R 11 -R 13 is not hydrogen, R 2 or R 6 or R 9 is not methyl, or R 10 is not CH 2 , then R 1 is selected from the group consisting of hydrogen, a halogen, COOH, C 1 -C 12 carboxylic acids, C 1 -C 12 acyl halides, C 1 -C 12 acyl residues, C 1 -C 12 esters, C 1 -C 12 secondary amides, (C 1 -C 12 )(C 1 -C 12 ) tertiary amides, (C 1 -C 12 )(C 1 -C 12 ) cyclic amides, (C 1 -C 12 ) amines, C 1 -C 12 alcohols, (C 1 -C 12 )(C 1 -C 12 ) ethers, C 1 -C 12 alkyls, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyls, C 2 -C 12 substituted alkenyls, and C 5 -C 12 aryls. If all R 3 -R 5 , R 7 , R 8 , R 11 -R 13 are hydrogen, R 2 , R 6 , and R 9 are each methyl, and R 10 is CH 2 , then R 1 is selected from hydrogen, a halogen, C 1 -C 12 carboxylic acids, C 1 -C 12 acyl halides, C 1 -C 12 acyl residues, C 2 -C 12 esters, C 2 -C 12 secondary amides, (C 1 -C 12 )(C 1 -C 12 ) tertiary amides, C 2 -C 12 alcohols, (C 1 -C 12 )(C 1 -C 12 ) ethers other than methyl-acetyl ether, C 2 -C 12 alkyls, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyls, C 2 -C 12 substituted alkenyls, and C 2 -C 12 aryls. R 2 and R 9 are each separately selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, C 2 -C 12 alkynyl, C 1 -C 12 acyl, C 1 -C 12 alcohol, and C 5 -C 12 aryl. R 3 -R 5 , R 7 , R 8 , and R 11 -R 13 are each separately selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, C 2 -C 12 alkynyl, and C 5 -C 12 aryl. R 6 is selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, and C 2 -C 12 alkynyl. R 10 is selected from hydrogen, a halogen, CH 2 , C 1 -C 6 alkyl, C 1 -C 6 substituted alkyl, C 2 -C 6 alkenyl, C 2 -C 6 substituted alkenyl, C 1 -C 12 alcohol, and C 5 -C 12 aryl. Pharmaceutical compositions comprising, and uses of, therapeutically effective amounts of the aove compounds and their prodrug esters, and a pharmaceutically acceptable carrier, are also disclosed, and are useful as, for example, anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making these compounds and their analogs, are also disclosed.
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