摘要:
The invention relates to the use of cyclopentane heptan(ene)oic acid, 2-heteroarylalk(en)yl derivatives as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: wherein the hatched segments represent &agr; bonds, the solid triangle represents a &bgr; bond, wavy line attachments indicate either the alpha (&agr;) or beta (&bgr;) configuration; dashed bonds represent a double bond or a single bond, R is a substituted hetero aryl radical having at least two pendant substituents selected from the group consisting of C1 to C6 alkyl; halogen; trifluoromethyl; COR1; COCF3; SO2NR1; NO2 and CN or at least one cyano group; R1 is hydrogen or a lower alkyl radical having up to six carbon atoms; X is selected from the group consisting of —OR1 and —N(R1)2; Y is ═O or represents 2 hydrogen radicals, and the 9, 11, or 15 alkyl esters thereof; provided, however, when said heteroaryl radical is a dichlorothienyl radical, said compound is not a 1-carboxylic acid or amide thereof.
摘要:
This invention relates to an agent for decreasing ocular tension comprising as an effective ingredient a 4,8-inter-m-phenylene PGI.sub.2 derivative represented by the formula: ##STR1## or a pharmaceutically acceptable salt thereof. The agent for decreasing ocular tension according to the present invention is useful as a therapeutic agent for treating various high ocular tension states such as glaucoma, ocular hypertension and high ocular tension which occurs after surgery.
摘要:
The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate a configuration; the solid triangle is used to indicate .beta. configuration; dashed bonds represent a double bond, or a single bond; R is a substituted heteroaryl radical having at least two pendant substituents selected from the group consisting of C.sub.1 to C.sub.6 alkyl; halogen; trifluoromethyl; COR.sup.1 ; COCF.sub.3 ; SO.sub.2 NR.sup.1 ; NO.sub.2 and CN or at least one cyano group; R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2 ; Y is .dbd.O or represents 2 hydrogen radicals and the 9, 11 or 15 lower alkyl esters thereof; provided, however, when said heteroaryl radical is a dichlorothienyl radical, the compound is not a 1-carboxylic add or amide thereof. Certain of the compounds represented by Formula I are novel and comprise another aspect of the present invention.
摘要:
The present invention provides cyclopentane heptanoic acid, 2 heteroaryl alkyl or alkenyl derivatives which may be substituted in the 1-position with hydroxyl, alkyloxy, amino and amido groups, e.g. 1-OH cyclopentane heptanoic acid, 2 heteroarylalkenyl derivatives. In particular, these derivatives are 7-[5-hydroxy-2-(heteroatom-substituted hydroxyhydrocarbyl)-3-hydroxycyclopentyl] heptanoic or heptenoic acids and amine, amide, ether, ester and alchohol derivatives of said acids wherein one or more of said hydroxy groups are replaced with an ether group. These compounds are potent ocular hypotensive and are particularly suited for the management of glaucoma. Moreover, the compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; with additional application in gastrointestinal disease, reproduction, fertility, incontinence, shock, inflammation, immune regulation, disorder of bone metabolism, renal dysfunction, cancer and other hypoproliferative diseases.
摘要:
The invention relates to 7-�5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)! heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.
摘要:
The invention relates to a dermal application form of prostacyclin derivatives of Formula I ##STR1## wherein R.sub.1 means hydrogen or alkyl of 1-10 carbon atoms,A is a --CH.sub.2 --CH.sub.2 --, trans-CH.dbd.CH-- or --C.ident.C-group,W represents a hydroxymethyl group which is free or functionally modified at the hydroxy group, the OH-group being in the .alpha.- or .beta.-position,X is a CH.sub.2 -group or an oxygen atom,Z is hydrogen or a cyano group,D means a straight-chain or branched, saturated alkylene group of 1-5 carbon atoms,E is a --C.ident.C-linkage or a direct bond,R.sub.2 is a straight- or branched-chain, saturated alkyl group of 1-7 carbon atoms,R.sub.3 is a free or functionally modified hydroxy group,and, if R.sub.1 means a hydrogen atom, containing the salts thereof with physiologically compatible bases, for the treatment of ulcerations caused by arterial occlusive diseases, and other skin disorders.
摘要:
The current application is directed to a method for treating pulmonary arterial hypertension (PAH), comprising: providing isolated endothelial progenitor cells (EPCs); treating the EPCs with prostacyclin, wherein the treated EPCs exhibit a hyperproliferative phenotype with enhanced angiogenic property; and administering a composition comprising the treated EPCs into a subject suffering from PAH.
摘要:
Use of prostacyclin or an analogue thereof for treatment of a new medical indication in acute critically ill patients, in particular acute critically ill patients with systemic endothelial damage, a biomarker for identifying individuals that have a new medical indication, and a method for identifying a new medical indication.
摘要:
The invention relates to the use of a pharmaceutical medication comprising an aromatase inhibitor, preferably a steroidal aromatase inactivator and an antioxidant as effective ingredients for the treatment of sex hormone-dependent diseases. Furthermore, the invention relates to a composition comprising an aromatase inhibitor/—inactivator and α-lipoic acid and/or extract of green tea containing polyphenols. The combination of an aromatase inhibitor and—inactivator and α-lipoic acid and/or extract of green tea containing polyphenols is particularly suitable for the treatment of sex hormone-dependent diseases as well as for the treatment of benign tumors such as e.g. lipomatoses as occurring in Madelung's disease.