专利号:US-10829792-B2 优先权日:2017-03-21 标 题 :Biocatalytic synthesis of strained carbocycles 发明人:CHEN KAI; HUANG XIONGYI; KAN S B JENNIFER 权利人:CALIFORNIA INST OF TECHN 摘要:Provided herein are methods for producing products containing strained carbocycles, such as cyclopropene moieties and/or bicyclobutane moieties. The methods include combining an alkyne and a carbene precursor in the presence of a heme protein, e.g., a cytochrome P450, under conditions sufficient to form the strained carbocycle. Reaction mixtures for producing strained carbocycles are also described, as well as whole-cell catalysts comprising heme proteins and variants thereof for forming cyclopropenes, bicyclobutanes, and related products.
专利号:US-7473797-B2 优先权日:2004-04-27 标 题 :Methods of 1,3-enyne preparation using copper (I) catalysts 发明人:VENKATARAMAN DHANDAPANI; BATES CRAIG G; SAEJUENG PRANORM 权利人:UNIV MASSACHUSETTS 摘要:A copper(I) bi-dentate ligand complex-catalyzed procedure for synthesis of 1,3-enynes. The methods and/or systems of this invention afford a variety of enynes, tolerate a variety of sensitive functional groups, and can be employed without resort to expensive palladium reagents.
专利号:US-11130764-B2 优先权日:2017-02-17 标题 :Analogs of vincamine and uses thereof 发明人:HUIGENS III ROBERT WILLIAM; NORWOOD IV VERRILL M; LUESCH HENDRIK 权利人:UNIV FLORIDA 摘要:The present disclosure provides compounds of any one of Formulae (I′), (I), (IA), (II′), (II), (IIA), (IIIA), (III″), (III′), (III), (IIIA), (IV), (V′), (V), (VI), (VII), (VIII′), (VIII), (IX′), (IX), and (X). The compounds described herein may be useful in treating and/or preventing a broad range of diseases (e.g., proliferative disease (e.g., cancers (e.g., non-small cell lung cancer, or glioma), inflammatory diseases, autoimmune diseases), CNS disorder (e.g., drug addiction), metabolic disorder (e.g., diabetes), or infectious disease (e.g., bacterial infection or parasitic infection (e.g., malaria))). Also provided in the present disclosure are pharmaceutical compositions, methods of synthesis of a compound described herein, kits, methods, and uses including or using a compound described herein.
专利号:US-2022048879-A1 优先权日:2020-08-13 标 题:Synthesis of small molecules inspired by Phomoxanthone A 发明人:ALI RAMEEZ; MATTSON ANITA 权利人:WORCESTER POLYTECH INST 摘要:Methods, compositions, and kits are provided for synthesizing bioactive chromane, the method including: constructing a tertiary ether stereocenter enantioselectively by catalyzed alkynylation of a substituted chromenone to obtain a chromanone; reducing alkyne and ketone in the chromanone to obtain a chroman; and converting ester to methyl group thereby obtaining chromane.
专利号:US-7479575-B2 优先权日:2003-10-13 标 题:Method for preparing para-phenyl alkynyl benzaldehydes 发明人:SWINNEN DOMINIQUE; POHIN DANIG 权利人:SERONO LAB 摘要:The present invention is related to a new synthesis for preparing para-phenyl alkynyl benzaldehyde of general formula (I). The compounds of formula (I) are useful building blocks, in particular in the synthesis of electrically conducting polymers. R is selected from the group consisting of C 1 -C 12 -alkyl, C 1 -C 12 -alkyl aryl, C 1 -C 12 -alkyl heteroaryl, C 2 -C 12 -alkenyl, C 2 C 12 -alkenyl aryl, C 2 -C 12 -alkenyl heteroaryl, C 2 -C 12 -alkynyl, C 2 -C 12 -alkynyl aryl, C 2 -C 12 -alkynyl heteroaryl, C 3 -C 8 -cycloalkylC 1 -C 12 -alkyl-C 3 -C 8 -cycloalkyl, C 1 -C 12 -alkoxy, aryl, heteroaryl, halides.
专利号:EP-1551403-B1 优先权日:2002-10-10 标 题 :5-substituted 2h-pyrazone-3-carboxylic acid derivatives as antilipolytic agents for the treatment of metabolic-related disorders such as dyslipidemia 发明人:SEMPLE GRAEME; AVERBUJ CLAUDIA; SKINNER PHILIP; GHARBAOUI TAWFIK; SHIN YOUNG-JUN 权利人:ARENA PHARM INC 摘要:The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R2 is H, halogen, C1-12 alkyl or C1-12 haloalkyl; and R3 is C3-6 cycloalkyl, C1-12 alkyl, C1-12 haloalkyl, C3-6 cycloalkyl-C1-4-alkylene, aryl-C1-4-alkylene or heteroaryl-C1-4-alkylene, wherein said aryl-C1-4-alkylene and heteroaryl-C1-4-alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of alpha-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.
摘要:Trofimova, A.; Sirvinskas, M.; Yudin, A. K., Science of Synthesis Knowledge Updates, (2021) 2, 73. 摘要:Weibel, J.-M.; Blanc, A.; Pale, P., Science of Synthesis Knowledge Updates, (2018) 1, 39. 摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 218. 摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 68. 摘要:Dong, X.; Liu , H., Science of Synthesis Knowledge Updates, (2019) 3, .