专利号:US-2014371464-A1 优先权日:2012-02-03 标 题:Process for the preparation of chiral isoxazoline azetidine derivatives as antiparasitic agents 发明人:BILLEN DENIS; GREENWOOD SEAN DAVID WILLIAM; STUK TIMOTHY LEE 权利人:ZOETIS LLC 摘要:The invention recites a chiral process for the synthesis of isoxazoline azetidine phenyl substituted derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, processes for making, and their use as a parasiticide in an animal. The variables *, R 1a , R 1b , R 1c , R 2 , and R 3 are as described herein
专利号:US-2022363662-A1 优先权日:2021-04-20 标题 :Compounds as lxr agonists 发明人:PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V 权利人:INTEGRAL BIOSCIENCES PRIVATED LTD 摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.
专利号:US-2009170828-A1 优先权日:2006-06-12 标题:Azetidine Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase 发明人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL 权利人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL 摘要:Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (I)
专利号:US-2011183958-A1 优先权日:2008-10-17 标 题 :Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:POWELL DAVID; TRANMER GEOFFREY K 权利人:MERCK FROSST CANADA LTD 摘要:Azetidine derivatives of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer; liver steatosis; and non-alcoholic steatohepatitis.
专利号:WO-2023086799-A1 优先权日:2021-11-09 标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-7582633-B2 优先权日:2007-01-26 标题:Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:LEBLANC YVES; POWELL DAVID; RAMTOHUL YEEMAN K; LEGER SERGE 权利人:MERCK FROSST CANADA L L C 摘要:Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
[参考文献]: Beck A, Et Al. Strategies And Challenges For The Next Generation Of Antibody-Drug Conjugates. Nat Rev Drug Discov. 2017;16(5):315-337. [参考文献]: Nalawansha Da, Et Al. Protacs: An Emerging Therapeutic Modality In Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
合成参考文献
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