104685-76-9Relevant articles and documents
Mild and efficient addition of carbon nucleophiles to condensed pyridines: influence of structure and limits of applicability
Starosotnikov, Alexey M.,Ilkov, Kirill V.,Bastrakov, Maxim A.,Fedyanin, Ivan V.,Kokorekin, Vladimir A.
, p. 92 - 100 (2020/02/28)
[Figure not available: see fulltext.] A number of azolo- and azinopyridines with varying substituents and annulated heterocycles were synthesized and examined in dearomatization reactions with carbon nucleophiles. Depending on the structure, the resulting covalent σ-adducts were formed either under basefree conditions or in Et3N-promoted process to give functionalized condensed dihydropyridines. Quantum-chemical calculations of the global electrophilicity index derived from FMO energies of azolopyridine series were performed to explain reactivity toward neutral and anionic C-nucleophiles. These values may be useful for qualitative prediction of particular reactivity pattern.
BICYCLIC HYDROXAMIC ACIDS USEFUL AS INHIBITORS OF MAMMALIAN HISTONE DEACETYLASE ACTIVITY
-
Page/Page column 97; 98, (2017/07/14)
A compound of formula (Ia) or (Ib) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of a histone deacetylase, and as such is useful in terepy, e.g. in the treatment of autoimmune disorders, mental disorders, neurodegenerative disorders, and hyperproliferative disorders.
HETEROCYCLIC COMPOUNDS AND USE THEREOF AS MODULATORS OF TYPE III RECEPTOR TYROSINE KINASES
-
Paragraph 0584, (2016/08/03)
Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFRβ kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
FUSED TRIAZOLE DERIVATIVES AS PHOSPHODIESTERASE 10A INHIBITORS
-
Page/Page column 30; 31, (2015/12/08)
Compounds of the general formula (I), wherein one of X1 and X2 represents N, and the other one of X1 and X2 represents -C(CH3), A represents unsubstituted or substituted 5-, 6-or 10-membered aryl or h
IMIDAZOPYRIDINE, IMIDAZOPYRIMIDINE AND IMIDAZOPYRAZINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS
-
Page/Page column 100, (2012/02/01)
Disclosed is a compound of Formula I or a salt thereof, in which X, X1, X2, R1, R2, and R3 are described herein. Also disclosed are pharmaceutical compositions and methods of using the compounds of Formula I to treat disorders mediated by melanocortin-4 r
Novel indanyl-substituted imidazo[1,2-a]pyridines as potent reversible inhibitors of the gastric H+/K+-ATPase
Zimmermann, Peter Jan,Buhr, Wilm,Brehm, Christof,Palmer, Andreas Marc,Feth, Martin Philipp,Senn-Bilfinger, Joerg,Simon, Wolfgang-Alexander
, p. 5374 - 5378 (2008/09/21)
A series of novel 8-indanylamino- and 8-indanyloxy-substituted imidazo[1,2-a]pyridines with reduced lipophilicity was synthesized from easily accessible starting compounds. The anti-secretory activity of these compounds has been assessed in a competitive
Phenyl-aza-benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
-
, (2008/06/13)
The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to phenyl-aza-benzimidazole molecules that are cellular proliferation inhibitors and thus are useful as anticancer agents. This invention further relates to small molecules which suppress cytokines and leukocytes.
Substituted triazolopyridine compounds
-
, (2008/06/13)
A compound of formula wherein R1 is —NR′R″, wherein R′ and R″ are independently selected from the group consisting of lower alkyl, —(CH2)n—C(O)NRaRb, —(CH2)n-heteroaryl, —(CH2)n-aryl, —(CH2)n—CN, —(CH2)n—O-lower alkyl or —(CH2)n-cycloalkyl, or R′ and R″ form together with the N-atom a five or six-membered non- aromatic ring, containing no or one additional heteroatom selected from the group consiting of O and S, and said ring being unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, —C(O)NRaRb and —(CH2)n—O-lower alkyl, and RaRb are independently from each other hydrogen or lower alkyl; R2 is aryl or heteroaryl, unsubstituted or substituted by lower alkyl or halogen; and n is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof. Compounds of formula I are useful in the treatment of disease associated with the adenosine A2 receptor.
Thrombin inhibitors
-
, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2or N; d is CY3or N; e is CY4or N; f is CY5or N; g is CY6or N; Y4, Y5, and Y6are independently hydrogen, C1-4alkyl, or halogen; Y1and Y2are independently hydrogen, C1-4alkyl, C3-7cycloalkyl, halogen, NH2, OH or C1-4alkoxy, and Y3is hydrogen, C1-4alkyl, C3-7cycloalkyl, halogen, —CN, NH2, OH or C1-4alkoxy; A is and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.
Thrombin inhibitors
-
, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.