Patent classifications
C07D473/00
sGC STIMULATORS
The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP), or both, or an upregulation of the NO pathway is desirable. The compounds are of Formula I:
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sGC STIMULATORS
The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP), or both, or an upregulation of the NO pathway is desirable. The compounds are of Formula I:
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CD73 INHIBITORS AND USES THEREOF
Compounds that modulate CD73 activity, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with CD73 activity are described herein.
PRMT5 INHIBITORS
The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
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COMPOUNDS FOR USE IN THE TREATMENT OF FASCIOLIASIS
The present invention relates to compounds and pharmaceutically acceptable salts or solvates thereof for use in the treatment or prevention of fascioliasis. Some of these compounds are novel per se and also have activity as inhibitors of Schistosoma growth. The invention also relates to pharmaceutical compositions comprising such novel compounds, salts or solvates and to the use of such novel compounds as medicaments, in particular in the treatment or prevention of schistosomiasis, also known as bilharzia.
COMPOUNDS FOR USE IN THE TREATMENT OF FASCIOLIASIS
The present invention relates to compounds and pharmaceutically acceptable salts or solvates thereof for use in the treatment or prevention of fascioliasis. Some of these compounds are novel per se and also have activity as inhibitors of Schistosoma growth. The invention also relates to pharmaceutical compositions comprising such novel compounds, salts or solvates and to the use of such novel compounds as medicaments, in particular in the treatment or prevention of schistosomiasis, also known as bilharzia.
SUBSTITUTED INDOLE COMPOUNDS
- Alaric J. Dyckman ,
- Dharmpal S. Dodd ,
- Christopher P. Mussari ,
- Trevor C. Sherwood ,
- John L. Gilmore ,
- Tasir Shamsul Haque ,
- Brian K. Whiteley ,
- David R. Tortolani ,
- Shoshana L. Posy ,
- John E. Macor ,
- Louis J. Lombardo ,
- Ramesh Kumar Sistla ,
- Anupama Kandhi Ramachandra Reddy ,
- Subramanya Hegde ,
- Laxman Pasunoori ,
- Sreekantha Ratna Kumar
Disclosed are compounds of Formula (I) or salts thereof, wherein Ring Het, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
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Aminopyrimidine five-membered heterocyclic compound, and intermediate, preparation method, pharmaceutical composition and application thereof
Disclosed in the present invention is an aminopyrimidine five-membered heterocyclic compound, and an intermediate, preparation method, pharmaceutical composition and application thereof. The aminopyrimidine five-membered heterocyclic compound provided by the present invention has a significant antagonistic effect on adenosine A2A receptors, and may be used as an antagonist for adenosine A2A receptors to effectively relieve or treat immune tolerance, diseases of the central nervous system, inflammatory diseases and like related diseases, while the preparation method is simple. ##STR00001##
Aminopyrimidine five-membered heterocyclic compound, and intermediate, preparation method, pharmaceutical composition and application thereof
Disclosed in the present invention is an aminopyrimidine five-membered heterocyclic compound, and an intermediate, preparation method, pharmaceutical composition and application thereof. The aminopyrimidine five-membered heterocyclic compound provided by the present invention has a significant antagonistic effect on adenosine A2A receptors, and may be used as an antagonist for adenosine A2A receptors to effectively relieve or treat immune tolerance, diseases of the central nervous system, inflammatory diseases and like related diseases, while the preparation method is simple. ##STR00001##
Catalyst-free and redox-neutral innate trifluoromethylation and alkylation of (hetero)aromatics enabled by light
The present disclosure relates to reagents and method for performing trifluoromethylation, difluoromethylation or alkylation of aromatic or heteroaromatic rings in a redox-neutral manner without any catalyst which are enabled by light. In addition, there are methods for synthesizing the starting reagents used in the trifluoromethylation, difluoromethylation or alkylation reactions.