专利号:US-6448413-B1 优先权日:1999-06-10 标题:Process for the synthesis of a-nor-seco compounds with sterane skeleton 发明人:SANTA CSABA; TUBA ZOLTAN; MAHO SANDOR; SZELES JANOS; BALOGH GABOR; BRLIK JANOS; TRISCHLER FERENC; SZILAGYI GABRIELLA; BAKCSI ERIKA 权利人:RICHTER GEDEON VEGYESZET 摘要:The invention relates to a new process for the synthesis of 17β-hydroxy-17α-methyl-1,3-seco-2-nor-5α-androstane-3-acid derivatives of formula (I) n wherein the meaning of Z is carboxyl or formyl group and n to the new secoindoxylidene carboxylic acid derivatives of formula (II) n wherein R 1 and R 2 independently are C 1 -C 4 alkyl or alkoxy group, hydrogen or halogen atom—which are intermediates for preparing the compounds of formula (I). n The 17β-hydroxy-17α-methyl-1,3-seco-2-nor-5α-androstane-3-acid derivatives of formula (I) are intermediates in the synthesis of oxandrolon (17β-hydroxy-17α-methyl-2-oxa-5α-androstane-3-one), which is used as anabolic in therapy.
专利号:US-12247037-B2 优先权日:2018-12-12 标题:1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-A][1,4]diazepine derivatives and related compounds as vasopressin antagonists for the treatment of neuro-psychological disorders 发明人:BRANDT GARY 权利人:NEUMORA THERAPEUTICS INC 摘要:The present invention relates to 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives and related compounds of Formula (I): wherein A, B, G, R1, R1b, RiC, R2 and X are as defined herein. The present compounds are vasopressin receptor antagonists (in particular of the Via receptor) for the treatment of neuro-psychological disorders, such as e.g. autism, anxiety, stress-related disorders, depression, schizophrenia or bipolar disorder. The present description discloses the synthesis of exemplary compounds, as well as pharmacological data thereof (e.g. pages 71 to 246; examples 1 to 49; tables 1 to 5). An exemplary compound is e.g. 8-chloro-1-(2-(5-fluoropyridin-2-yl)-2,6-diazaspiro[3.3]heptan-6-yl)-5-methyl-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine (example 1, compound no. 1).
专利号:US-11040977-B2 优先权日:2013-12-05 标题 :Synthesis of trans-8-chloro-5-methyl-1-[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10B-tetraaza-benzo[e]azulene and crytalline forms thereof 发明人:ROTHENHAEUSLER BENNO; TRUSSARDI RENE; HOFFMANN-EMERY FABIENNE; SCHWITTER URS; ADAM JEAN-MICHEL; GRASSMANN OLAF; HARTUNG THOMAS; RAN FREDERIC; DIODONE RALPH; PFLEGER CHRISTOPHE; BARTELS BJORN 权利人:HOFFMANN LA ROCHE 摘要:The invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
专利号:US-7301049-B2 优先权日:2001-06-21 标 题:Photolabile esters and their uses 发明人:SERAFINOWSKI PAWEL JERZY; GARLAND PETER BRYAN 权利人:CANCER RES INST 摘要:Compounds which are capable of generating acid on photolysis are disclosed, and the uses of these compounds, especially for deprotecting the termini of nucleic acid molecules or peptides during synthesis of arrays. The compounds described herein may be employed in the detritylation of 5′-O-dimethoxytrityl (DMT) protected nucleotides by photolysing the compounds to generate an acid capable of removing the DMT group allowing oligonucleotide arrays to be synthesised using readily available 5′-O-DMT-nucleoside-3′-O-phosphoramidite monomers conventionally used in solid phase nucleic acid synthesis. A method of avoiding the effects of stray light in projection lithography techniques is also disclosed.
专利号:US-11040939-B1 优先权日:2020-06-23 标 题 :N-transfer reagent and method for preparing the same and its application 发明人:CHOU HO-HSUAN; LU GUAN-HAN; HSUEH HSIAO-CHIN; HUANG TZU-CHIA 权利人:UNIV NAT CHENG KUNG 摘要:Provided are a novel N-transfer reagent and a method for preparing the same and its application. The N-transfer reagent is represented by the following Formula (I): n n n n n n n n n n The various novel N-transfer reagents of the present invention can be quickly prepared by employing different nitrobenzene precursors. The N-transfer reagents can directly convert a variety of amino compounds into diazo compounds under mild conditions. Particularly, the N-transfer reagents can facilitate the synthesis of the diazo compounds. The application of synthesizing diazo compounds of the present invention can greatly decrease the difficulty in operation, increase the safety during experiments, reduce the cost of production and the environmental pollution, and enhance the industrial value of diazo compounds.
专利号:US-2019194210-A1 优先权日:2013-12-05 标 题 :Synthesis of trans-8-chloro-5-methyl-1 -[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4h-2,3,5,10b-tetraaza-benzo[e]azulene and crytalline forms thereof
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 349. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 351. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 353. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 394. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 340.