Design and Synthesis of the First Generation of Dithiolane Thiazolidinedione- and Phenylacetic Acid-Based PPARγ Agonists
摘要:
A series of novel derivatives of potent antioxidant vitamin, alpha-lipoic acid, and related analogues were designed, synthesized, and evaluated for their PPAR gamma agonist activities. Compounds 9a and the water soluble analogue 11e were found to be potent PPAR gamma agonists. Compound 9a appeared to have a significant role in improving insulin sensitivity and reducing triglyceride levels in fa/fa rats as well as inhibited proliferation of a variety of normal and neoplastic cultured human cell types. These novel compounds may prove efficacious not only in the treatment of Type 2 diabetes, but also atherosclerosis, prevention of vascular restenosis, and inflammatory skin diseases.
[EN] 2-PHENYL-3H-IMIDAZO[4,5-B]PYRIDINE DERIVATES USEFUL AS INHIBITORS OF MAMMALIAN TYROSINE KINASE ROR1 ACTIVITY<br/>[FR] DÉRIVÉS DE 2-PHÉNYL-3H-IMIDAZO[4,5-B]PYRIDINE UTILISÉS COMME INHIBITEURS DE L'ACTIVITÉ DE LA TYROSINE KINASE DE MAMMIFÈRE ROR1
申请人:KANCERA AB
公开号:WO2016124553A1
公开(公告)日:2016-08-11
A compound of formula (I´) or (I´´) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of mammalian kinase enzyme activity, including ROR1 tyrosine kinase activity and may be used in the treatment of disorders associated with such activity.
[EN] INHIBITORS OF THE NOTCH TRANSCRIPTIONAL ACTIVATION COMPLEX AND METHODS FOR USE OF THE SAME<br/>[FR] INHIBITEURS DU COMPLEXE D'ACTIVATION DE TRANSCRIPTION DU RÉCEPTEUR NOTCH ET PROCÉDÉS D'UTILISATION DE CES DERNIERS
申请人:UNIV MIAMI
公开号:WO2016154255A1
公开(公告)日:2016-09-29
Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.
[EN] BENZOTHIAZOLE AMPHIPHILES<br/>[FR] AMPHOPHILES DE BENZOTHIAZOLE
申请人:UNIV CALIFORNIA
公开号:WO2017120198A1
公开(公告)日:2017-07-13
Disclosed herein, inter alia, are compounds and methods for increasing spine density in a neuron, and for treatment of neuronal diseases and cancer.
本文披露了用于增加神经元中脊柱密度的化合物和方法,以及用于治疗神经疾病和癌症的方法。
[EN] USE OF BENZOTHIAZOLE AMPHIPHILES FOR TREATING TRAUMATIC BRAIN INJURY<br/>[FR] UTILISATION D'AMPHIPHILES DE BENZOTHIAZOLE POUR TRAITER UNE LÉSION CÉRÉBRALE TRAUMATIQUE
申请人:SPINOGENIX INC
公开号:WO2019005682A1
公开(公告)日:2019-01-03
The present invention is directed to methods of reducing symptoms of traumatic brain injury in patients by administering a therapeutically effective amount of a benzothiazole amphiphile compound to a patient suffering from a traumatic brain injury within 0 to 72 hours of incurring the injury.
Raf inhibitor compounds and methods of use thereof
申请人:Laird Ellen
公开号:US20060281751A1
公开(公告)日:2006-12-14
Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.