Abstract:
To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.Since the compound of the invention has an S1P1 agonist activity, it is useful as an active ingredient for a treating or preventing agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or a tissue, a graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, a nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, ischemia-reperfusion injury, or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer and leukemia.
Abstract:
To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity. Since the compound of the invention has an S1P1 agonist activity, it is useful as an active ingredient for a treating or preventing agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or a tissue, a graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, a nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, ischemia-reperfusion injury, or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer and leukemia.
Abstract:
The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-α mediated diseases.
Abstract:
The present invention relates to a sulfonamide compound of the formula (I): wherein each symbol is as defined in the specification, a salt thereof, and a pharmaceutical composition containing same. This compound can be an effective agent for the prophylaxis and treatment of the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy suppressing action.
Abstract:
This invention relates to a compound of the formula: wherein A1 is lower alkylene, R1 is substituted quinolyl, etc., R2 is hydrogen, halogen or lower alkyl, R3 is halogen or lower alkyl, and R4 is a group of the formula: —Q—A2—R5, etc., in which R5 is amino, acylamino, etc., A2 is lower alkylene or a single bond, and Q is a group of the formula: and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
Abstract:
The invention relates to a pharmaceutical composition for ophthalmic administration comprising a compound of the formula: wherein X1, X2, X3, R1, R2, R3, R4, R5, Q and A are as defined in the disclosure. This invention also relates to methods of using the pharmaceutical composition in the prevention and/or treatment of bradykinin or its analogues mediated diseases in the eye, such as allergy, inflammation and pain of the eye.
Abstract:
A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.2 is hydrogen, lower alkyl or a heterocyclic group,R.sup.3 is hydrogen, lower alkyl or halogen,R.sup.4 is lower alkyl or halogen,R.sup.5 is nitro or amino substituted with substituent(s) selected from the group consisting of lower alkyl and acyl, andA is lower alkylene.
Abstract:
This invention relates to a compound of formula (I) wherein A.sup.1 is lower alkylene, R.sup.1 is substituted quinolyl, etc., R.sup.2 is hydrogen, halogen or lower alkyl, R.sup.3 is halogen or lower alkyl, and R.sup.4 is a group of the formula: -Q-A.sup.2 -R.sup.5, etc., in which R.sup.5 is amino, acylamino, etc., A.sup.2 is lower alkylene or a single bond, and Q is a group of formula (a), and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals. ##STR1##
Abstract:
A compound of the formula: ##STR1## wherein --X.sup.3 .dbd.X.sup.2 --X.sup.1 .dbd.N-- is a group of the formula: ##STR2## R.sup.1 is hydrogen or halogen, R.sup.2 is halogen,R.sup.3 is hydrogen, nitro, amino optionally having at least one substituent or a heterocyclic group optionally having at least one substituent,R.sup.4 and R.sup.5 are each hydrogen, or halogen,R.sup.6 and R.sup.8 are each hydrogen, halogen, lower alkyl, hydroxy, lower alkylthio, amino optionally substituted with lower alkyl, or lower alkoxy optionally substituted with a substituent selected from the group consisting of hydroxy, lower alkoxy, amino, lower alkylamino and aryl optionally substituted with lower alkoxy,R.sup.7 is hydrogen or lower alkyl,A is lower alkylene, andQ is O or N--R.sup.9 is hydrogen or acyl,provided that R.sup.3 is not hydrogen when X.sup.1 is C--R.sup.6, in which R.sup.6 is hydrogen, andpharmaceutically acceptable salts thereof.
Abstract:
Disclosed is an image synthesizer including an image frames memory which memorizes a plurality of image frames which are produced by continuously taking pictures of a subject, an image synthesizer which synthesizes a plurality of image frames to a summation image, an image brightness adjuster which adjusts brightness of the summation image by synthesizing the image frames with the image synthesizer, and a display which displays the summation image which is being synthesized by the image synthesizing means in the image brightness adjusting processing.