摘要:
The present invention relates to sustained release compositions of prostacyclin, as well as uses thereof, in particular for the prevention and/or treatment of pulmonary arterial hypertension.
摘要:
There is provided a method for treating pulmonary hypertension in a subject, comprising: administering to the subject in need thereof a daily dose of ambrisentan from 1 mg to about 15 mg, wherein the method is carried out without drug labeling instruction to monitor liver aminotransferase levels during ambrisentan treatment.
摘要:
The compounds of Formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.
摘要:
This invention relates to novel prostacyclin derivatives and acceptable salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors.
摘要:
Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and a prostacyclin. Pharmaceutical formulations are also disclosed.
摘要:
Disclosed is a method for treatment of external secretion disorders, which comprises administering a fatty 5 acid derivative to a subject in need of said treatment. The method of the present invention is useful for treatment of at least one condition selected from hypolacrimation including disorder of basal tear secretion, dry-eye syndrome, hyposalivation and dry-mouth syndrome.
摘要:
According to the present invention, the gene for IL-13, an anti-inflammatory cytokine, was shown to be a target of prostacyclin (PGI2)-activated Peroxisome proliferator-activated receptor (PPAR) δ. Furthermore, the PGI2-PPARδ signaling pathway was revealed to regulate the expression of IL-13 gene in human vascular endothelial cells, and controls inflammatory responses induced by proinflammatory cytokines through the production of IL-13 in an autocrine or paracrine manner. Thus, the present invention provides a method for treating or preventing inflammatory disorders, which comprises administering a therapeutically effective amount of PPARδ agonist into a subject. Furthermore, the present invention provides a method for treating or preventing inflammatory disorders, which comprises administering a prostacyclin synthase gene or a protein encoded by the gene into a subject.
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 .alpha. 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 acid or amide thereof. Certain of the compounds represented by Formula I are novel and comprise another aspect of the present invention.
摘要:
A method is described for treating bacterially induced meningitis, comprising administering a prostane derivative of formula I or Ia ##STR1## wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described below, and the --O--R.sup.3 -- group is in the .alpha.- or .beta.-configuration. The prostane derivative can optionally comprise or serve as an adjuvant, and it can be administered in combination with an antiobiotic.
摘要:
The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives 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; dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, 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. Certain of the compounds represented by Formula I comprise another aspect of the present invention.