摘要:
An ophthalmic preparation which comprises a fumagillol derivative represented by the general formula(I): ##STR1## wherein R.sup.1 is hydrogen; R.sup.2 is a halogen, N(O).sub.m R.sup.5 R.sup.6, N.sup.+ R.sup.5 R.sup.6 R.sup.7 .multidot.X.sup.-, S(O).sub.n R.sup.5 or S.sup.+ R.sup.5 R.sup.6 .multidot.X.sup.-, wherein R.sup.5, R.sup.6 and R.sup.7 represent independently a substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted heterocyclic group; X.sup.- represents a counter anion; m represents 0 or 1; n represents an integer from 0 to 2; or R.sup.5 and R.sup.6 together with the adjacent nitrogen or sulfur atom may form a substituted or unsubstituted nitrogen- or sulfur-containing heterocyclic group which may form a condensed ring; or R.sup.1 and R.sup.2 are combined to represent a chemical bond; R.sup.3 is a substituted or unsubstituted 2-methyl-l-propenyl group or a substituted or unsubstituted isobutyl group; A is oxygen or NR.sup.8, wherein R.sup.8 represents hydrogen, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted aryl group; and R.sup.4 is hydrogen, a substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted acyl group and a salt thereof is useful for inhibiting corneal opacification occurring after ophthalmic surgery.
摘要:
Dextran sulfate, .beta.-1,3-glucan sulfate, and the salts thereof are angiostatic and useful for treatment and prevention of various diseases caused by abnormally accelerated angiogenesis. Combination of such a compound with a steroidal or non-steroidal substance increases the angiostatic activity of each compound to induce the combined effect.
摘要:
A preventive and/or therapeutic agent which improves an abnormal bowel function such as an abdominal pain, a diarrhea, or a constipation and is effective for preventing or treating a functional gastrointestinal disorder is provided.A preventive and/or therapeutic agent for a functional gastrointestinal disorder contains refaximin as an effective ingredient. The functional gastrointestinal disorder includes a functional esophageal disorder, a functional gastroduodenal disorder (e.g., a functional dyspepsia), a functional bowel disorder (e.g., a functional bloating, a functional diarrhea), a functional abdominal pain syndrome, a functional gallbladder and Sphincter of Oddi disorder, a functional anorectal disorder (e.g., a functional fecal incontinence, a functional anorectal pain, a functional defecation disorder), a functional disorder in neonates and toddlers (e.g., an infant functional diarrhea), a functional disorder in children and adolescents (e.g., a childhood functional abdominal pain, a childhood nonretentive fecal incontinence), and other diseases.
摘要:
A complex of a fumagillin derivative represented by the general formula: ##STR1## wherein R.sup.1 is hydrogen; R.sup.2 is halogen, N(O)mR.sup.5 R.sup.6, N.sup.+ R.sup.5 R.sup.6 R.sup.7.X.sup.-, S(O)nR.sup.5 or S.sup.+ R.sup.5 R.sup.6.X.sup.- (wherein R.sup.5, R.sup.6 and R.sup.7 are independently an optionally substituted hydrocarbon or heterocyclic group; X.sup.- is a counter anion; m is an integer of 0 or 1; n is an integer from 0 to 2; and R.sup.5 and R.sup.6 together with the adjacent nitrogen or sulfur atom may form a nitrogen- or sulfur-containing heterocyclic group which may be substituted and form a condensed ring); or R.sup.1 and R.sup.2 together represent a bond; R.sup.3 is 2-methyl-1-propenyl group or isobutyl group; A is O or NR.sup.8 (wherein R.sup.8 is hydrogen or an optionally substituted lower alkyl or aryl group); R.sup.4 is hydrogen, an optionally substituted hydrocarbon group or an optionally substituted acyl group); or a salt thereof, with an optionally etherified cyclodextrin is disclosed. The present invention also provides an antineoplastic agent containing the complex.
摘要:
A method for preventing and/or treating a functional gastrointestinal disorder, comprising administering, to a subject with the functional gastrointestinal disorder, rifaximin as an effective ingredient. The functional gastroinstestinal disorder includes a functional esophageal disorder, a functional gastroduodenal disorder (e.g., a functional dyspepsia), a functional bowel disorder (e.g., a functional bloating, a functional diarrhea), a functional abdominal pain syndrome, a functional gallbladder and Sphincter of Oddi disorder, a functional anorectal disorder (e.g., a functional fecal incontinence, a functional anorectal pain, a functional defecation disorder), a functional disorder in neonates and toddlers (e.g., an infant functional diarrhea), a functional disorder in children and adolescents (e.g., a childhood functional abdominal pain, a childhood nonretentive fecal incontinence), and other diseases.
摘要:
At least one hyperlipidemic agent selected from the group consisting of a fibrate compound (e.g., fenofibrate, bezafibrate, or a salt thereof) and an HMG-CoA reductase inhibitor (e.g., a statin compound, for example, pravastatin, atorvastatin, or salts thereof) is, as active ingredients, combined with an α-glucosidase inhibitor (e.g., voglibose, and acarbose) in the pharmaceutical composition of the present invention. The proportion of the α-glucosidase inhibitor may be about 0.001 to 50 parts by weight relative to 100 parts by weight of the hyperlipidemic agent. The present invention provides a pharmaceutical composition which is excellent in prophylactic and/or therapeutic effect on metabolic syndrome, hyperlipemia, diabetes, diabetes complications, etc, and has few side effects.
摘要:
The present invention relates to a pharmaceutical composition for oral administration in which a fumagillol derivative is stabilized and exhibits remarkable antiangiogenesis activity in oral administration.
摘要:
The present invention relates to a composition with enhanced angiogenic activity which contains a compound of the formula:R--Awherein R stands for a higher aliphatic hydrocarbon residue, and A stands for hydrogen atom, carboxyl group, hydroxyl group, carbamoyl group which may be substituted or amino group which may be substituted or quaternized.The composition of the present invention has been found to enhance blood vessel formation, which is useful for the treatment of various ischemic diseases, trauma, thermal burns, alopecia, etc.