676560-15-9Relevant academic research and scientific papers
Unsymmetrical α,ω-end-functionalized oligo(cyclohexylidenes): efficient synthesis and conformational analysis
Zeinyeh, Wa?l,Radix, Sylvie,Terreux, Rapha?l,Chemelle, Julie-Anne,Walchshofer, Nadia
, p. 4032 - 4038 (2016)
The title compounds were efficiently synthesized by decarboxylative dehydration of β-hydroxy acids. This iterative process allowed to obtain bis- and ter-cyclohexylidenes with good yield. The conformations of trans and cis isomers of an unsymmetrical α,ω-
Bcl-2 INHIBITORS
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Paragraph 0577; 0578; 0579, (2019/11/19)
Disclosed herein is a compound of Formula (I) for inhibiting Bcl-2 and treating disease associated with undesirable bcl-2 activity (Bcl-2 related diseases), a method of using the compounds disclosed herein for treating dysregulated apoptotic diseases including cancers and treating autoimmune disease, and a pharmaceutical composition comprising the same.
TRICYCLIC COMPOUND SERVING AS IMMUNOMODULATOR
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Paragraph 0809-0810, (2019/01/04)
Provided are compounds of formula I and formula II or pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The compounds of formula I and formula II or the pharmaceutically acceptable salts of the compounds provide indole 2,3-dioxygenase (IDO) inhibitory activity and are capable of treating IDO-mediated immunosuppressive diseases, such as infectious diseases or cancer.
AMIDO-SUBSTITUTED AZASPIRO DERIVATIVES AS TANKYRASE INHIBITORS
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Page/Page column 115, (2018/05/24)
The present invention relates to amido-substituted cyclohexane compounds of general formula (I) : in which A, R4, R6, R7, R8, R9, R10 and R11 are as defined herein, to methods of
AMIDO-SUBSTITUTED CYCLOHEXANE DERIVATIVES
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Page/Page column 118; 119, (2018/05/24)
The present invention relates to amido-substituted cyclohexane compounds of general formula (I) : in which m, A, R4, R6, R7, R8, R9, R10 and R11 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
COMPOUNDS FOR THE INHIBITION OF INDOLEAMINE-2,3-DIOXYGENASE
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Paragraph 0219-0220, (2016/04/09)
The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of IDO, and for the treatment of IDO-related disorders.
AMIDO-SUBSTITUTED CYCLOHEXANE DERIVATIVES
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Page/Page column 223; 224, (2016/11/21)
The present invention relates to amido-substituted cyclohexane compounds of general formula (I), in which A, R4, R6, R7, R8, R9, R10 and R11 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredient.
AROMATIC HETEROCYCLIC COMPOUND
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Paragraph 0693; 0694, (2015/05/05)
The compound represented by the general formula: wherein ring A is benzene which may be substituted and the like; ring B is benzene which may be substituted and the like; X is a single bond and the like; Y is alkyl which may be substituted and the like; Z is CR1 or nitrogen atom; R1 is hydrogen and the like; R2 is alkyl which may be substituted and the like or a pharmaceutically acceptable salt thereof is useful as a prevention/treatment agent of obesity, diabetes, and the like.
The synthesis and biological testing of bacilysin analogues
Robertson, Keith,Murphy, Cormac D.,Paradisi, Francesca
, p. 1157 - 1168 (2013/11/06)
A series of compounds based on the structure of bacilysin were synthesised and tested for antibacterial activity. The key steps in the syntheses are the coupling of an iodide to a diketopiperazine (DKP) and mono-lactim ether scaffold, respectively. The diastereoselectivity of the coupling reactions was dependant on the scaffold, with selectivity for DKP of about 4:1 and mono-lactim ether exceeding 98:2. Subsequent elaboration of the compounds to give open chain dipeptides and DKPs that mimic the structure of bacilysin but substitute the epoxy ketone for a saturated or unsaturated ketone is described. Overall yield from coupling to final product was between 5 and 21 %, with the yield of the saturated products notably higher. The open chain dipeptides demonstrated moderate antibacterial and antifungal activity.
Discovery of small molecule Mer kinase inhibitors for the treatment of pediatric acute lymphoblastic leukemia
Liu, Jing,Yang, Chao,Simpson, Catherine,Deryckere, Deborah,Van Deusen, Amy,Miley, Michael J.,Kireev, Dmitri,Norris-Drouin, Jacqueline,Sather, Susan,Hunter, Debra,Korboukh, Victoria K.,Patel, Hari S.,Janzen, William P.,MacHius, Mischa,Johnson, Gary L.,Earp, H. Shelton,Graham, Douglas K.,Frye, Stephen V.,Wang, Xiaodong
supporting information; experimental part, p. 129 - 134 (2012/04/04)
Ectopic Mer expression promotes pro-survival signaling and contributes to leukemogenesis and chemoresistance in childhood acute lymphoblastic leukemia (ALL). Consequently, Mer kinase inhibitors may promote leukemic cell death and further act as chemosensitizers increasing efficacy and reducing toxicities of current ALL regimens. We have applied a structure-based design approach to discover novel small molecule Mer kinase inhibitors. Several pyrazolopyrimidine derivatives effectively inhibit Mer kinase activity at subnanomolar concentrations. Furthermore, the lead compound shows a promising selectivity profile against a panel of 72 kinases and has excellent pharmacokinetic properties. We also describe the crystal structure of the complex between the lead compound and Mer, opening new opportunities for further optimization and new template design.
