Patent classifications
C07D235/04
Benzimidazol derivatives for treating filovirus infection
The present invention relates to compounds comprising a benzimidazole scaffold, and the use of such compounds for the treatment of viral diseases. The invention also relates to pharmaceutical compositions comprising said compounds as an active ingredient. In particular the compounds of the invention comprising a benzimidazole scaffold are used for the treatment of filoviruses or retroviruses, and preferably for the treatment of Ebola virus or HIV virus.
METHOD FOR INHIBITING REDUCTION IN CONCENTRATION OF OXIDIZING AGENT IN SULFURIC ACID SOLUTION CONTAINING PERSULFURIC ACID COMPONENT
A heterocyclic compound having a structure in which a benzene ring and a nitrogen-containing heterocycle are condensed is added to a sulfuric acid solution that contains a persulfuric acid component such as peroxomonosulfuric acid, peroxomonosulfate, peroxodisulfuric acid, or peroxodisulfate as an oxidant and in which impurities that promote the reduction in the oxidant concentration are present. Here, the heterocyclic compound having a structure in which a benzene ring and a nitrogen-containing heterocycle are condensed is preferably a benzotriazole-based compound. The impurities that promote a reduction in the oxidant concentration are suitably one or more selected from copper ions, iron ions, nitrate ions, and nitrite ions. The method of the present invention of inhibiting a reduction in the oxidant concentration in a sulfuric acid solution containing a persulfuric acid component can inhibit the reduction in the oxidant concentration to a minimum even when impurities that cause a reduction in the oxidant concentration are mixed.
ELECTROCHEMICAL DEVICE
An electrochemical device capable of more sufficiently preventing swelling due to generation of a gas such as carbon dioxide and decomposition of a lithium salt while having a simple structure. The electrochemical device includes a non-aqueous electrolytic solution, wherein the non-aqueous electrolytic solution contains a metal-organic framework containing: an azole-based organic molecule optionally having a hydrophobic group, and a metal atom.
Unsymmeirical salts, CCC-NHC pincer metal complexes, and methods of making the same
Provided herein are unsymmetrical bis(azolium) salts, unsymmetrical CCC-NHC metal complexes, and methods of forming the same. The unsymmetrical bis(azolium) salts include a central aryl ring that is substituted with two heterocyclic rings in an ortho, meta, or para fashion. The unsymmetrical CCC-NHC metal complexes include metalated unsymmetrical bis(azolium) salts. The method of forming the unsymmetrical CCC-NHC metal complexes includes reacting a dihalogenated benzene with a first azole to form a mono(azole)benzene, reacting the mono(azole)benzene with a second azole to form an unsymmetrical bis(azole)benzene, alkylating the unsymmetrical bis(azole)benzene to form an unsymmetrical bis(azolium) salt, and metalating the unsymmetrical bis(azolium) salt to form the unsymmetrical CCC-NHC metal complex. Also provided are a bis-ligated CCC-NHC metal complex and an unsymmetrical bimetallic complex.
COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE
This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with Abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor.
COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE
This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with Abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor.
Method of identifying potential inhibitors of APO TNFα trimers
A new, stable trimeric TNFα structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNFα/TNFR1 interaction. Membrane-bound TNFα is not affected in its ability to signal through TNFR2, and thus the new structure of TNFα may be used in therapies which do not significantly raise the risk of infection or malignancy.
Method of identifying potential inhibitors of APO TNFα trimers
A new, stable trimeric TNFα structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNFα/TNFR1 interaction. Membrane-bound TNFα is not affected in its ability to signal through TNFR2, and thus the new structure of TNFα may be used in therapies which do not significantly raise the risk of infection or malignancy.
BTK INHIBITOR
- Xuehai Wang ,
- Chengde Wu ,
- Yong XU ,
- Chunli Shen ,
- Li'e Li ,
- Guoping Hu ,
- Yang Yue ,
- Jian Li ,
- Diliang Guo ,
- Nengyang Shi ,
- Lu Huang ,
- Shuhui Chen ,
- Ronghua Tu ,
- Zhongwen Yang ,
- Xuwen Zhang ,
- Qiang Xiao ,
- Hua Tian ,
- Yanping Yu ,
- Hailiang Chen ,
- Wenjie Sun ,
- Zhenyu He ,
- Jie Shen ,
- Jing Yang ,
- Jing Tang ,
- Wen Zhou ,
- Jing Yu ,
- Yi Zhang ,
- Quan Liu
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).
##STR00001##
Benzo five-membered nitrogen heterocyclic piperidine or piperazine derivatives and preparation methods and pharmaceutical compositions thereof
Compounds of formula (I) and its pharmaceutically acceptable salts are described ##STR00001##
wherein R.sub.1, R.sub.2, X, Y, A, B are as defined in the specification. Also disclosed are methods for preparing the compounds of formula (I) or pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the compounds of formula (I) or pharmaceutically acceptable salts thereof.