Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.
Abstract: An eye drop containing (i) a peptide having an amino acid sequence which is represented by Ser-Ser-Ser-Arg (“SSSR”), or a pharmaceutically acceptable salt thereof and (ii) a peptide having an amino acid sequence represented by Phe-Gly-Leu-Met-NH2 (“FGLM”), or a pharmaceutically acceptable salt thereof. The concentration ratio of the SSSR or a pharmaceutically acceptable salt thereof and the FGLM or a pharmaceutically acceptable salt thereof is 1/15 and 1/50. The concentration of the SSSR or a pharmaceutically acceptable salt thereof is 0.001% to 0.3% (w/v), and the concentration of the FGLM or a pharmaceutically acceptable salt thereof is 0.015% to 1.5% (w/v). The pH of the eye drop is 2.5 to 6.5. The eye drop serves to minimize the occurrence of side effects and serves to improve its storage stability.
Abstract: Provided is a pharmaceutical composition including an 11-deoxy-prostaglandin compound represented by formula (I): and a fatty acid ester. By mixing the compound of formula (I) and a fatty acid ester, the compound of formula (I) will be stabilized.
Abstract: A method for manufacturing a fatty acid derivative represented by formula (I) is provided: wherein Z1 is wherein R3 is a protecting group for a hydroxy group; which includes the step of reacting a compound of formula (II): wherein Z2 is the same as Z1 except for when Z1 is Z2 is with a co-oxidizer under the presence of an azaadamantane-N-oxyl derivative.
Abstract: A method for manufacturing a fatty acid derivative represented by formula (I) is provided: wherein Z1 is wherein R3 and R4 are hydrogen atom, halogen atom, lower alkyl or lower alkoxy; when R3 and R4 are lower alkoxy, R3 and R4 may be linked together to form a ring structure; which includes the step of reacting a compound of formula (II): wherein Z2 is the same as Z1; with a co-oxidizer under the presence of an azaadamantane-N-oxyl derivative.
Abstract: The present invention provides a method for screening an agent being useful for the treatment of dry eye and/or corneal and conjunctival lesion of dry eye severity level 3 or more according to the report of the International Dry Eye WorkShop (DEWS Report) (2007) and a pharmaceutical composition comprising the agent. The present invention further provides a method for the treatment of dry eye and/or corneal and conjunctival lesion of dry eye severity level 3 or more according to DEWS Report (2007) using the agent.
Abstract: Provided is a pharmaceutical composition including an 11-deoxy-prostaglandin compound represented by formula (I): and a fatty acid ester. By mixing the compound of formula (I) and a fatty acid ester, the compound of formula (I) will be stabilized.
Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.
Abstract: Provided is a pharmaceutical composition comprising a 11-deoxy-prostaglandin compound represented by formula (I): and a fatty acid ester. By mixing the compound of formula (I) and a fatty acid ester, the compound of formula (I) will be stabilized.
Abstract: The present invention provides a method for screening an agent being useful for the treatment of dry eye and/or corneal and conjunctival lesion of dry eye severity level 3 or more according to the report of the International Dry Eye WorkShop (DEWS Report) (2007) and a pharmaceutical composition comprising the agent. The present invention further provides a method for the treatment of dry eye and/or corneal and conjunctival lesion of dry eye severity level 3 or more according to DEWS Report (2007) using the agent.
Abstract: The present invention provides a method for screening an agent being useful for the treatment of dry eye and/or corneal and conjunctival lesion of dry eye severity level 3 or more according to the report of the International Dry Eye WorkShop (DEWS Report) (2007) and a pharmaceutical composition comprising the agent. The present invention further provides a method for the treatment of dry eye and/or corneal and conjunctival lesion of dry eye severity level 3 or more according to DEWS Report (2007) using the agent.
Abstract: The present invention discloses a soft gelatin capsule formulation of a 15-keto-prostaglandin compound, which comprises: a soft gelatin capsule shell comprising gelatin and sugar alcohol as a plasticizer, and a mixture comprising a 15-keto-prostaglandin compound and a pharmaceutically acceptable vehicle which is filled in the shell. By encapsulating the 15-keto-prostaglandin compound in the specified soft gelatin capsule shell, stability of the compound is significantly improved.
Abstract: The present invention relates to methods and pharmaceutical compositions for immunosuppression by using the fatty acid derivative represented by formula (I). The present invention further relates to methods and pharmaceutical compositions for treating inflammatory diseases, allergic diseases and autoimmune diseases by using said fatty acid derivative.
Abstract: The present invention discloses a soft gelatin capsule formulation of a 15-keto-prostaglandin compound, which comprises: a soft gelatin capsule shell comprising gelatin and sugar alcohol as a plasticizer, and a mixture comprising a 15-keto-prostaglandin compound and a pharmaceutically acceptable vehicle which is filled in the shell. By encapsulating the 15-keto-prostaglandin compound in the specified soft gelatin capsule shell, stability of the compound is significantly improved.
Abstract: Provided is a composition for scalp and hair treatment, including a menthol derivative and a prostaglandin compound having two hetero atoms at the 15 position. The composition of the present invention is effective not only for preventing dandruff and itchy scalp but also for preventing or treating hair loss, baldness, or hair thinness.
Abstract: The present invention provides a method and composition for promoting hair growth in a mammal which comprises a prostaglandin compound having two hetero atoms at the 15 position as an active ingredient thereof.
Abstract: The present invention provides a method and composition for promoting hair growth in a mammal which comprises a prostaglandin compound having two hetero atoms at the 15 position as an active ingredient thereof.
Abstract: Disclosed is a method for stabilizing a pharmaceutically active bi-cyclic compound of formula (I): comprising the step of: admixing the same with a polyol and/or a fatty acid ester other than glyceride and a composition obtained by the method. In addition a soft gelatin capsule formulation of the compound of formula (I) obtained by incorporating the compound in a soft gelatin capsule shell comprising gelatin and a polyol plasticizer.
Abstract: The present invention provides an applicator, which holds an intended quantity of liquid medicament and applies the same to skin or mucous membrane without wasting. The applicator comprises a grip portion 10 for grasping; a neck portion 12, which can be elastically deflected, continuous from the grip portion 10; and a head portion 13, having a slit 14 for holding the liquid medicament supplied, continuous from the neck portion 12. When the head portion 13 is pressed against the skin or the mucous membrane, the liquid medicament is applied there while the neck portion 12 is elastically deflected.
Abstract: The invention provides a thiazole derivative useful as a VAP-1 inhibitor, as well as a pharmaceutical agent for the prophylaxis or treatment of VAP-1 associated diseases and the like, a method of inhibiting VAP-1 in a subject, and a method for the prophylaxis or treatment of VAP-1 associated disease in a subject. The thiazole derivative is a compound represented by the formula (I): R1—NH—X—Y—Z wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.