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
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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.
Pyrimidine-4 (3H)-ketone heterocyclic compound, preparation method thereof and application of pyrimidine-4 (3H)-ketone heterocyclic compound in medicine
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Paragraph 0280-0282; 0288-0291, (2021/07/21)
The invention relates to pyrimidine-4 (3H)-ketone heterocyclic compounds suitable for inhibiting or regulating SHP2, a preparation method of the pyrimidine-4 (3H)-ketone heterocyclic compounds and application of the pyrimidine-4 (3H)-ketone heterocyclic compounds in medicine. Specifically, the invention relates to a compound as shown in a general formula (I) and a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof, a method for treating and/or preventing related diseases mediated by SHP2, especially cancers by using the compound or the pharmaceutically acceptable salt thereof, and a preparation method of the compound or the pharmaceutically acceptable salt thereof. The invention also relates to application of the compound or the pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof in preparation of drugs for treating and/or preventing SHP2-mediated related diseases. Wherein each substituent in the general formula (I) is as defined in the specification.