摘要:
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
摘要:
The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C1-C6)alkyl or a CN; R1b represents H, an halogen or a (C1-C6)alkyl; R1c represents H or a (C1-C6)alkyl; R2 represents H, an halogen, an OH, an O—(C1-C6)alkyl or (C1-C6)alkyl; R3 represents H, an halogen, a (C1-C6)alkyl, an OH, an O—(C1-C6)alkyl, a CONH2 or CN; R4 represents H, an halogen or a (C1-C6)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C1-C6)alkyl, or one of its enantiomers.
摘要翻译:本发明涉及式(I)的苯胺衍生物,其制备及其治疗应用,例如治疗青光眼:式(I),R 1a表示H,卤素,(C 1 -C 6)烷基或CN ; R 1b表示H,卤素或(C 1 -C 6)烷基; R1c表示H或(C1-C6)烷基; R 2表示H,卤素,OH,O-(C 1 -C 6)烷基或(C 1 -C 6)烷基; R 3表示H,卤素,(C 1 -C 6)烷基,OH,O-(C 1 -C 6)烷基,CONH 2或CN; R 4表示H,卤素或(C 1 -C 6)烷基; R5表示H或F:R7表示H或F; R8表示H或F; R9表示H或(C1-C6)烷基或其一种对映异构体。
摘要:
The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.
摘要:
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
摘要:
Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.
摘要翻译:游离或盐或溶剂合物形式的化合物,其中Ar是式Y基团是碳或氮,R 1,R 2,R 3, R 4,R 5,R 6,R 7,R 8, R 0,R 9,R 10,X,n,p,q和r如说明书中所定义,它们的制备及其作为药物的用途,特别是 治疗阻塞性或炎症性气道疾病。
摘要:
A process for preparing a 3-(N,N-disubstituted amino)phenol is herein disclosed which comprises reacting resorcin with a primary amine represented by formula (2): R.sup.1 NH.sub.2 (2) wherein R.sup.1 is an alkyl group, a cycloalkyl group, an alkenyl group, an alkoxyalkyl group, an aryl group or an aralkyl group, terminating the reaction when the conversion of resorcin is 50 mol % or more and when the amount of an N,N'-disubstituted-m-phenylenediamine as a by-product is 2 mol % or less of the amount of used resorcin, adding an alkyl halide represented by formula (3): R.sup.2 X (3) wherein R.sup.2 is an alkyl group or a cycloalkyl group; and X is a halogen atom, to the obtained reaction mixture, adding an aqueous alkaline solution to the resultant reaction mixture to dissolve unreacted resorcin in the aqueous phase, extracting the 3-(N,N-disubstituted amino)phenol with an organic solvent, and then recovering unreacted resorcin from the aqueous phase. According to this process, the high-purity 3-(N,N-disubstituted amino)phenol can be prepared from resorcin in a substantially high yield, the production of by-products being inhibited.
摘要:
p-Amino-phenols are advantageously prepared by catalytic hydrogenation of the aromatic nitro compounds on which they are based in a reaction medium of aqueous sulphuric acid in the sense of a Bamberger rearrangement at elevated temperature by a procedure in which the reaction medium additionally contains a water-miscible organic solvent.
摘要:
Novel compounds which are 2,6-di-t-butylphenols substituted on the 4 position by an anilino group, which anilino group is substituted by a carboxyl substituent, a tetrazolyl substituent or an N-methyltetrazolyl substituent, are useful antiallergic agents. Pharmaceutical compositions containing and pharmacological methods of using such compounds are also disclosed, as are synthetic intermediates for preparing such compounds. Certain of the synthetic intermediates also exhibit useful antiallergic activity.
摘要:
A process for preparing carbocyclic m-aminohydroxyaromatics comprises reacting the corresponding o-- or m-halohydroxyaromatics or metal salts thereof with primary or secondary amines in the presence of a base and in the presence or absence of a diluent.