- 2-AMINO-N-(AMINO-OXO-ARYL-LAMBDA6-SULFANYLIDENE)ACETAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
-
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(amino-oxo-aryl-λ6- sulfanylidene)acetamide compounds (referred to herein as ANASIA compounds) that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-tRNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
- -
-
Page/Page column 227
(2021/06/26)
-
- QUINOLINE DERIVATIVES AND THEIR USE FOR TREATING ENDOPLASMIC RETICULUM STRESS-RELATED DISEASES AND DISORDERS
-
Provided herein are quinolines, e.g., a compound of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of an endoplasmic reticulum stress-caused disease. Also provided herein are methods of their use for reducing endoplasmic reticulum stress and modulating the activity of a sarcoplasmic/endoplasmic reticulum Ca2+ ATPase.
- -
-
Paragraph 0935; 0936; 0937
(2017/07/01)
-
- HEPATITIS B ANTIVIRAL AGENTS
-
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: [in-line-formulae]X-A-Y-Z-L-R1??(I)[/in-line-formulae] which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
- -
-
Paragraph 0208
(2016/12/12)
-
- THIOPHENE-SULFONIC ACID PICOLYL AMIDES
-
The present invention relates to thiophene-sulfonic acid picolyl amides of the Formula (I), where R1 to R7 and n are as defined in the claims and to the N-oxides, the agriculturally acceptable salts and the veterinarily acceptable sa
- -
-
Page/Page column 60-61
(2008/06/13)
-
- N-aryl thienyl-, furyl-, and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
-
Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
- -
-
Page column 100
(2010/01/30)
-
- Thiophenesulfonamides as endothelin receptor antagonists
-
The synthesis and in vitro binding affinities of a series of thiophenesulfonamides as ET(A) selective endothelin receptor antagonists is described. The most potent inhibitor displayed an IC50 of 43 nM and 3 μM to ET(A) and ET(B) receptors, respectively.
- Raju,Wu, Chengde,Kois, Adam,Verner, Erik,Okun, Ilya,Stavros, Fiona,Chan, Ming Fai
-
p. 2651 - 2656
(2007/10/03)
-