- ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I' PATHWAY AND METHODS OF USE THEREOF
-
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
- -
-
-
- ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I" PATHWAY AND METHODS OF USE THEREOF
-
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
- -
-
-
- Method for synthesizing benzothiazole by microwave radiation of benzothioamide compound in aqueous phase
-
The invention discloses a method for synthesizing benzothiazole by microwave radiation of a benzothioamide compound in an aqueous phase. The method includes the steps: adding the benzothioamide compound into the aqueous phase under microwave conditions; performing cyclization under alkaline conditions to generate the benzothiazole. The method for preparing the benzothiazole is environmentally friendly, simple and convenient in operation, safe, cheap and efficient. Compared with the prior art, the method is applicable to a lot of functional groups, high in yield, few in by-products, simple in operation, safe, low in cost and environmentally friendly.
- -
-
Paragraph 0013; 0096
(2019/02/13)
-
- Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis
-
A previous publication from this lab (Patrick, et al. Bioorg. Med. Chem. 2016, 24, 2451-2465) explored the antitrypanosomal activities of novel derivatives of 2-(2-benzamido)ethyl-4-phenylthiazole (1), which had been identified as a hit against Trypanosoma brucei, the causative agent of human African trypanosomiasis. While a number of these compounds, particularly the urea analogues, were quite potent, these molecules as a whole exhibited poor metabolic stability. The present work describes the synthesis of 65 new analogues arising from medicinal chemistry optimization at different sites on the molecule. The most promising compounds were the urea derivatives of 2-aryl-benzothiazol-5-amines. One such analogue, (S)-2-(3,4-difluorophenyl)-5-(3-fluoro-N-pyrrolidylamido)benzothiazole (57) was chosen for in vivo efficacy studies based upon in vitro activity, metabolic stability, and brain penetration. This compound attained 5/5 cures in murine models of both early and late stage human African trypanosomiasis, representing a new lead for the development of drugs to combat this neglected disease.
- Patrick, Donald A.,Gillespie, J. Robert,McQueen, Joshua,Hulverson, Matthew A.,Ranade, Ranae M.,Creason, Sharon A.,Herbst, Zackary M.,Gelb, Michael H.,Buckner, Frederick S.,Tidwell, Richard R.
-
p. 957 - 971
(2017/02/19)
-
- Structure-activity relationships of N-phenyl-N′-benzothiazol-6-ylurea synthetic derivatives: Cytokinin-like activity and adventitious rooting enhancement
-
Some years ago we demonstrated the cytokinin-like activity of the synthetic N-phenyl-N′-benzothiazol-6-ylurea (PBU) and a relevant adventitious rooting adjuvant activity of symmetric urea derivatives devoid of any cytokinin- or auxin-like activity per se. Here we report the synthesis and the biological activity evaluation of nine symmetric or asymmetric ureas/thioureas, structurally related to PBU. None of them show cytokinin-like activity, while we demonstrate for the first time that PBU interacts with Arabidopsis cytokinin receptor CRE1/AHK4 in a heterologous bioassay system. Among the PBU derivatives, all the symmetric ureas/thioureas show an adventitious rooting adjuvant activity in various bioassays, confirming that this activity is strictly dependent on their chemical structure.
- Rolli, Enrico,Incerti, Matteo,Brunoni, Federica,Vicini, Paola,Ricci, Ada
-
experimental part
p. 159 - 165
(2012/03/27)
-
- COMPOUNDS AND METHODS OF USE
-
Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
- -
-
Page/Page column 112
(2010/11/27)
-
- HETEROAROMATIC UREAS WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1)
-
Compounds of formula (I): are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
- -
-
Page/Page column 27-28
(2010/02/11)
-
- Guanidinyl heterocycle compounds useful as alpha-2 adrenoceptor agonists
-
This invention involves compounds having the following structure: as described in the Claims; and enantiomers, optical isomers, stereoisomers, diastereomers, tautomers, addition salts, biohydrolyzable amides and esters thereof, as well as pharmaceutical compositions comprising such novel compounds. The invention also relates to the use of such compounds for preventing or treating disorders modulated by alpha-2 adrenoceptors.
- -
-
-
- 5- AND 6-(2-IMIDAZOLIN-2-YLAMINO) AND -(2-THIAZOLIN-2-YLAMINO)-BENZOTHIAZOLES AS ALPHA-2 ADRENERGIC LIGANDS
-
This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
- -
-
-