36016-40-7Relevant articles and documents
Komplexchemie perhalogenierter Cyclopentadiene und Alkine. V. Darstellung weiterer funktioneller Derivate von (C5Cl4R)Mn(CO)3 und (C5Cl4R)Rh(COD). Kristallstruktur von (C5Cl4CONH2)Mn(CO)3
Suenkel, Karlheinz,Steiner, Doris
, p. 67 - 76 (1989)
Starting from (C5Cl4Li)Mn(CO)3, generated in situ, the functional derivatives (C5Cl4R)Mn(CO)3 with R = SnMe3, PPh2, SePh, (SCl5Cl4)Mn(CO)3, CHO, COCl, CONH2, CN, NCO, and NH2 can be obtained.A series of compounds (C5Cl4R)Rh(1,5-COD) with R = H, Me, SiMe3, SiMe2H and SnMe3 can be prepared from (C5Cl5)Rh(1,5-COD) via the lithio derivative.The crystal structure of (C5Cl4CONH2)Mn(CO)3 has been determined.
HYDROPYRAZINO[1,2-D][1,4]DIAZEPINE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
-
Page/Page column 21-22, (2021/05/07)
The present invention relates to compounds of formula (I), wherein R1 to R3 and n are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer
Lücking, Ulrich,Kosemund, Dirk,B?hnke, Niels,Lienau, Philip,Siemeister, Gerhard,Denner, Karsten,Bohlmann, Rolf,Briem, Hans,Terebesi, Ildiko,B?mer, Ulf,Sch?fer, Martina,Ince, Stuart,Mumberg, Dominik,Scholz, Arne,Izumi, Raquel,Hwang, Stuart,Von Nussbaum, Franz
, p. 11651 - 11674 (2021/07/31)
Selective inhibition of exclusively transcription-regulating positive transcription elongation factor b/CDK9 is a promising new approach in cancer therapy. Starting from atuveciclib, the first selective CDK9 inhibitor to enter clinical development, lead optimization efforts aimed at identifying intravenously (iv) applicable CDK9 inhibitors with an improved therapeutic index led to the discovery of the highly potent and selective clinical candidate VIP152. The evaluation of various scaffold hops was instrumental in the identification of VIP152, which is characterized by the underexplored benzyl sulfoximine group. VIP152 exhibited the best preclinical overall profile in vitro and in vivo, including high efficacy and good tolerability in xenograft models in mice and rats upon once weekly iv administration. VIP152 has entered clinical trials for the treatment of cancer with promising longterm, durable monotherapy activity in double-hit diffuse large B-cell lymphoma patients.
N-(4-FLUOROPHENYL)-5-PHENYL-[1,2,4] TRIAZOLO [1,5-A] PYRIDINE-2-CARBOXAMIDE DERIVATIVES AND THEIR SYNTHESIS THEREOF
-
, (2021/08/20)
The present invention relates to the development of novel N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for their different pharmacological activities. It particularly relates to the development of N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives as antiviral, anticancer, antifungal, hypoglycemic, anti-tubercular, sedative, anti-type 2 diabetes activity. It specifically relates to the N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for treatment of H37Rv and multidrug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB). The present invention also relates to the process for synthesis of N-(4-fluorophenyl)- 5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives. The invention further relates to method for treatment of method for treatment of diseases such as tuberculosis, type 2 diabetes, bacterial, viral and fungal infections. Invention addresses the challenges in working with chemical processes and products by inventing novel reaction methodology that can maximize the desired products and minimize by-products, designing new synthetic schemes that can simplify operations in chemical productions and seeking nontoxic reagent that are inherently environmentally and ecologically benign. Synthesis of novel N-(4- fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives is being employed to develop a novel synthetic methodology and their pharmacological applications. Novel series of N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[l,5-a]pyridine-2-carboxamide derivatives were designed synthesized evaluated for their in vitro anti-mycobacterial activity against H37Rv and multi-drug-resistant (MDR) strains of mycobacterium tuberculosis (MTB). All the synthesized compounds were characterized by spectroscopic methods like Mass, NMR and elemental analysis.