摘要:
New thyroid receptor ligands are provided which have the general formula (I) in which X is -O-, -S-, -CH2-, -CO-, or -NH-; Y is -(CH2)n- where n is an integer from 1 to 5, or cis- or trans-ethylene; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R2 and R3 being other than hydrogen; R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; R6 is carboxylic acid, or esters or prodrugs; R7 is hydrogen or an alkanoyl or an aroyl. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
wherein R 1 is an eicosapentaenoyl or docosahexaenoyl; R 2 and R 3 are each independently an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; R 4 is a hydrogen atom, an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; and A is a single bond, -C(=O)NH-(CH 2 ) n -NH- wherein n is 2 or 3, or a bivalent group of the following formula
wherein m and p are each independently 0 or 1. The aniline derivative of the present invention has high inhibitory activity against and high selectivity for ACAT derived from macrophage and is useful as an agent for the prophylaxis and treatment of arteriosclerosis.
摘要:
Die Erfindung betrifft ein strahlungsempfindliches Gemisch, das ein polymeres Bindemittel mit säurespaltbaren Seitengruppen und eine bei Bestrahlung eine starke Säure bildende Verbindung enthält sowie neue Amide von α,β-ungesättigten Carbonsäuren, mit denen die als Bindemittel verwendeten Polymere aufgebaut werden. Außerdem betrifft die Erfindung ein positiv bzw. negativ arbeitendes strahlungsempfindliches Aufzeichnungsmaterial mit einem Träger und einer darauf befindlichen positiv oder negativ arbeitenden Schicht, die das erfindungsgemäße strahlungsempfindliche Gemisch enthält.
摘要:
Provided in the present invention are a class of alkylphenol compounds and a preparation method therefor. Specifically provided in the present invention are a new alkyl polyphenol compound as represented by chemical formula I, and a preparation method therefor and the use thereof in the treatment of metabolic syndrome.
摘要:
The invention relates to compounds of general formula (1): in which R1, R2, R3, R4, R5, A, B, D and E are as defined in Claim 1, and also to the preparation process therefor and the therapeutic use thereof. These compounds can be used in the treatment of pathologies associated with hyperglycaemia.
dans laquelle: R représnte un groupement alkyle supérieur, 1-(alkyle supérieur) cycloalk-1-yle inférieur, alcényle supérieur comportant une plusieurs doubles liaisons, et soit R 3 représente un hydroxy, R 1 et R 2 , différents, répresentent un hydrogéne ou un alkyle inférieur, R 4 et R 5 indentiques ou différents, représentent un alkyle ou un alkoxy inférieur, soit R 1 et R 4 représentent un groupement hydroxy et R 2 , R 3 , R 5 , indentiques ou différents représentent un alkyle ou un alkoxy inférieur, leurs isoméres ainsi que leurs sels. Les dérivés, sont doués d'une part d'une activité inhibitrice de l'acyl CoA-cholestérol-acyltransférase (ACAT) et d'autre part d'une capacité à protéger les lipoprotéines humaines de faible densité assurant le transport du cholestérol (LDL) vis-à-vis des modifications oxydatives induites par le cuivre. Les copositions pharmaceutiques sour utiles pour le traitement des dyslipidémies et de l'athérosclérose.
摘要:
There are disclosed a 4-aminophenol derivative of the formula: (wherein R¹ and R² each represent a lower alkyl group, Y represents a single bonding arm, a lower alkylene group or a lower alkenylene group, R³ represents a thienyl group or pyrrolyl group which may be also substituted with a lower alkyl group; benzothienyl group, indolyl group; or a phenyl group which is substituted with 1 to 2 groups selected from a lower alkoxy group and a lower alkanoyloxy group; or Y-R³ represents integrally an alkyl group with 6 to 9 carbon atoms; or a hydrocarbon group with 5 to 14 carbon atoms having 2 or 3 double bonds) or a pharmacologically acceptable salt thereof, and processes for preparing the same.
摘要翻译:公开了下式的4-氨基苯酚衍生物:其中R 1和R 2各自表示低级烷基,Y表示单键结合臂,低级亚烷基或低级亚烯基, R 3表示也可以被低级烷基取代的噻吩基或吡咯基;苯并噻吩基,吲哚基或被1〜2个选自低级烷氧基和低级烷酰氧基取代的苯基 基团或YR 3整体表示碳原子数6〜9的烷基或具有2或3个双键的碳原子数5〜14的烃基)或其药理学上可接受的盐,及其制备方法。