专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-2009156465-A1 优先权日:2005-12-30 标题:Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors 发明人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 权利人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 摘要:The present invention relates to β-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
专利号:US-2008300251-A1 优先权日:2005-09-05 标 题 :Derivatives of 3-Azabicyclo[3.1.0] Hexane as Dipeptidyl Peptidase-IV Inhibitors 发明人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND 权利人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND 摘要:The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
专利号:US-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
专利号:US-2025223262-A1 优先权日:2022-03-31 标 题 :Synthesis of morphinans with reduced herg activity and mop binding 发明人:LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA 权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG 摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.
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