摘要:
The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to Farnesoid-X-receptors (FXR) and can be used to treat diseases which are modulated by FXR agonists such as diabetes and dyslipidemia.
摘要:
The present invention relates to novel α-substituted heteroarylalkylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.
摘要:
A method of increasing the quantity of circulating high density lipoproteins and clearing cholesterol from certain tissues, comprising administering to a human an effective amount of a compound of the formula ##STR1## where X is H, OH, ##STR2## or NH.sub.2 ; R and R' identical or different are H, CH.sub.3 or C.sub.2 H.sub.5 ; m is zero or 1; and A is selected from the group comprising (CH.sub.3).sub.3 C--, Y--C.sub.6 H.sub.4 --, Y--C.sub.6 H.sub.4 --O--C(CH.sub.3).sub.2 --, Y--C.sub.6 H.sub.4 --C(CH.sub.3).sub.2 --, Y--C.sub.6 H.sub.4 --C(O)--C.sub.6 H.sub.4 --, Y--C.sub.6 H.sub.4 --(CH.sub.2).sub.n -- and Y--C.sub.6 H.sub.4 --O--(CH.sub.2).sub.n --, where n is an integer from 1 to 6 and Y is H, CH.sub.3, OCH.sub.3 or Cl.The present invention is a division of our copending application Ser. No. 114,423, filed Jan. 22, 1980, now U.S. Pat. No. 4,309,364.
摘要:
The present invention relates to novel aminophosphonate derivatives substituted in .alpha. position by phenol groups, of formula (I): ##STR1## in which: X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2, A, B, Z and n are defined in claim 1, as well as their preparations and the pharmaceutical compositions comprising them.
摘要:
The invention relates to new gem-diphosphonates derivatives substituted by phenol groups of formula (I): ##STR1## as well as the process for their preparation and the pharmaceutical compositions containing them.
摘要:
The present invention relates to a pharmaceutical composition for increasing the relative quantity of circulating high density lipoproteins favorable augmentating the alpha/beta lipoprotein cholesterol ratios and clearing cholesterol and lipids from certain tissues and inducing hypotensive activity comprising administering to a human an effective amount of a compound of the formula: ##STR1## where X is H, OH, or ##STR2## R and R' identical or different are H, CH.sub.3 or C.sub.2 H.sub.5 ; m is zero or 1; and A is selected from the group comprising (CH.sub.3).sub.3 C--, Y--C.sub.6 H.sub.4 --, Y--C.sub.6 H.sub.4 --O--C(CH.sub.3).sub.2 --, Y--C.sub.6 H.sub.4 --C(CH.sub.3).sub.2 --, Y--C.sub.6 H.sub.4 --C(O)--C.sub.6 H.sub.4 --, Y--C.sub.6 H.sub.4 --(CH.sub.2).sub.n -- and Y--C.sub.6 H.sub.4 --O--(CH.sub.2).sub.n --, where n is an integer from 1 to 6 and Y is H, CH.sub.3, OCH.sub.3, a halogen, and a pharmaceutically acceptable excipient.
摘要翻译:本发明涉及用于增加循环高密度脂蛋白的相对量的药物组合物,其有利地增加了α/β脂蛋白胆固醇比例,并且从某些组织中清除胆固醇和脂质并诱导降血压活性,包括向人施用有效量的化合物 其中X是H,OH或R 1和R 3相同或不同的是H,CH 3或C 2 H 5; m为零或1; 并且A选自(CH 3)3C-,Y-C 6 H 4 - ,Y-C 6 H 4 -OC(CH 3)2 + 13,Y-C 6 H 4 -C(CH 3)2 - ,Y-C 6 H 4 -C(O) -C 6 H 4 - ,Y-C 6 H 4 - (CH 2)n - 和Y-C 6 H 4 -O-(CH 2)n - ,其中n是1至6的整数,Y是H,CH 3,OCH 3,卤素和药学上 可接受的赋形剂。
摘要:
The present invention relates to novel α-substituted-β-aminoethylphosphonate and α-substituted-β-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.