Patent classifications
C07C255/00
METHODS FOR MODULATING RNA SPLICING
In one aspect, described herein is an intronic recognition element for splicing modifier (iREMS) that can be recognized by a compound provided herein. In another aspect, described herein are methods for modulating the amount of a product of a gene, wherein a precursor RNA transcript transcribed from the gene contains an intronic REMS, and the methods utilizing a compound described herein. More particularly, described herein are methods for modulating the amount of an RNA transcript or protein product encoded by a gene, wherein a precursor RNA transcript transcribed from the gene comprises an intronic REMS, and the methods utilizing a compound described herein. In another aspect, provided herein are artificial gene constructs comprising an intronic REMS, and uses of those artificial gene constructs to modulate protein production. In another aspect, provided herein are methods for altering endogenous genes to comprise an intronic REMS, and the use of a compound described herein to modulate protein produced from such altered endogenous genes.
Triarylmethane compounds
The present invention relates to triarylmethane compounds of the formula (I), which suitable as monomers for preparing thermoplastic resins having beneficial optical properties and which can be used for producing optical devices. R.sup.1, R.sup.2 are e.g. hydrogen; Y is an alkylene group having 2, 3 or 4 carbon atoms, Ar is selected from mono- or polycyclic aryl and mono- or polycyclic hetaryl; X.sup.1, X.sup.2, X.sup.3, X.sup.4 are CH, C—R.sup.x or N, provided that in each ring at most two of X.sup.1, X.sup.2, X.sup.3, X.sup.4 are N; R.sup.x is e.g. halogen, CN or CH═CH.sub.2. The invention also relates to thermoplastic resins comprising a polymerized unit of the compound of formula (I). ##STR00001##
Efficient process for the preparation of sitagliptin
Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine. ##STR00001##
Inhibitors of RNA guided nucleases and uses thereof
Compositions and methods are provided for the inhibition of the function of RNA guided endonucleases, including the identification and use of such inhibitors.
Inhibitors of RNA guided nucleases and uses thereof
Compositions and methods are provided for the inhibition of the function of RNA guided endonucleases, including the identification and use of such inhibitors.
CANNABINOID DERIVATIVES
This disclosure relates generally to cannabinoid derivatives having the structural formula (I), pharmaceutical compositions comprising them, and methods of using the cannabinoid derivatives. In some embodiments, R.sup.1 is —CH.sub.2CH═C(CH.sub.3).sub.2, R.sup.2 is methyl, R.sup.3 is CsHn, R.sup.4 is —C(O)N(R.sup.4a)(R.sup.4b), R.sup.5 is H, R.sup.6 is OH, and R.sup.7 is H. Compounds of the present disclosure were tested in agonist and antagonist mode for both the CB1 and CB2 receptors. The tested compounds were generally found to exhibit activity in antagonist mode at the CB1 and CB2 receptor.
CANNABINOID DERIVATIVES
This disclosure relates generally to cannabinoid derivatives having the structural formula (I), pharmaceutical compositions comprising them, and methods of using the cannabinoid derivatives. In some embodiments, R.sup.1 is —CH.sub.2CH═C(CH.sub.3).sub.2, R.sup.2 is methyl, R.sup.3 is CsHn, R.sup.4 is —C(O)N(R.sup.4a)(R.sup.4b), R.sup.5 is H, R.sup.6 is OH, and R.sup.7 is H. Compounds of the present disclosure were tested in agonist and antagonist mode for both the CB1 and CB2 receptors. The tested compounds were generally found to exhibit activity in antagonist mode at the CB1 and CB2 receptor.
Compositions for the treatment of pulmonary fibrosis
The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.
Compositions for the treatment of pulmonary fibrosis
The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.
Method for producing ϵ-caprolactam
A method produces ε-caprolactam through adipamide as an intermediate, and characteristically includes a lactamization step of reacting adipamide, formed from a material compound, with hydrogen and ammonia in the presence of a catalyst containing: a metal oxide mainly containing an oxide(s) of one or more metallic elements selected from the group consisting of metallic elements of group 5 and groups 7 to 14 in the 4th to 6th periods of the periodic table; and a metal and/or a metal compound having a hydrogenation ability.