Abstract: A compound having the following formula wherein A is —O—; B is alkylene or alkenylene optionally containing —O—, —S—, —(NR7)—, —CO— or —N?; R1 and R2 are alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl is unsubstituted or substituted by halogen, cycloalkyl, aryl, adamantyl or amino; R3 is a substituted or unsubstituted pyridine ring; R5 and R6 are hydrogen or alkyl; R7 is hydrogen or alkyl; X is O or S; and each hydrogen of the said amino is unsubstituted or substituted by alkyl, alkoxycarbonyl, cycloalkyloxycarbonyl, arylalkoxycarbonyl or halogenoalkyloxycarbonyl. The compound is a TNF-? production inhibitor that is useful for treating autoimmune diseases such as rheumatoid arthritis.

Abstract: A compound having the following formula wherein A is —O—; B is alkylene or alkenylene optionally containing —O—, —S—, —(NR7)—, —CO— or —N?; R1 and R2 are alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl is unsubstituted or substituted by halogen, cycloalkyl, aryl, adamantyl or amino; R3 is a substituted or unsubstituted pyridine ring; R5 and R6 are hydrogen or alkyl; R7 is hydrogen or alkyl; X is O or S; and each hydrogen of the said amino is unsubstituted or substituted by alkyl, alkoxycarbonyl, cycloalkyloxycarbonyl, arylalkoxycarbonyl or halogenoalkyloxycarbonyl. The compound is a TNF-? production inhibitor that is useful for treating autoimmune diseases such as rheumatoid arthritis.

Abstract: A purpose of the present invention is to provide TNF-? production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-? production inhibitory activities, wherein “A” is —(NR4)—, —(CR5R6)— or —O—, “B” is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and “X” is oxygen or sulfer respectively.

Abstract: An object of the present invention is to prepare substances which are excellent in delivery and enable drugs to be retained in a body effectively over a long period and to construct a drug delivery system using the substances. When the delivering substance which is obtained by reacting polyalkylene glycol or a reactive derivative thereof, a phospholipid and a drug with each other to form covalent bonds is administered systemically or topically, the substance is retained at a target site in a body for a long period, thereby making it possible to sustain drug efficacy over a long period by a single administration.

Abstract: A purpose of the present invention is to provide TNF-? production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-? production inhibitory activities, wherein A is —(NR4)—, —(CR5R6)— or —O—, B is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and X is oxygen or sulfer respectively.

Abstract: A purpose of the present invention is to provide TNF-? production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-? production inhibitory activities, wherein A is —(NR4)—, —(CR5R6)— or —O—, B is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and X is oxygen or sulfer respectively.

Abstract: A purpose of the present invention is to provide TNF-? production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-? production inhibitory activities, wherein A is —(NR4)—, —(CR5R6)— or —O—, B is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and X is oxygen or sulfer respectively.

Abstract: A purpose of the present invention is to provide TNF-? production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-? production inhibitory activities, wherein “A” is —(NR4)—, —(CR5R6)— or —O—, “B” is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and “X” is oxygen or sulfer respectively.

Abstract: A purpose of the present invention is to provide TNF-? production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-? production inhibitory activities, wherein “A” is —(NR4)—, —(CR5R6)— or —O—, “B” is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and “X” is oxygen or sulfer respectively.

Abstract: Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects. The present invention provides compounds represented by the following formula [I] wherein R1 is H, alkyl, aromatic, RA—CO—, RC—S— or the formula [II]; R2, R3 and R4 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 can together form a nonaromatic heterocyclic ring; R7 is H, alkyl, cycloalkyl, hydroxy, mercapto, phenyl, RB—O—, RC—S—, RD—COS—, RE—OCO—, RF—N(RG)— or —CONHOH; and A1 and A2 are alkylene.

Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.

Abstract: An object of the present invention is to prepare substances which are excellent in delivery and enable drugs to be retained in a body effectively over a long period and to construct a drug delivery system using the substances. When the delivering substance which is obtained by reacting polyalkylene glycol or a reactive derivative thereof, a phospholipid and a drug with each other to form covalent bonds is administered systemically or topically, the substance is retained at a target site in a body for a long period, thereby making it possible to sustain drug efficacy over a long period by a single administration.

Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.

Abstract: A purpose of the present invention is to provide TNF-&agr; production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis.

Abstract: Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects.

Abstract: Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects. The present invention provides compounds represented by the following formula [I] wherein R1 is H, alkyl, aromatic, RA—CO—, RC—S—or the formula [II]; R2, R3 and R4 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 can together form a nonaromatic heterocyclic ring; R7 is H, alkyl, cycloalkyl, hydroxy, mercapto, phenyl, RB—O—, RC—S—, RD—COS—, RE—OCO—, RF—N(RG)— or —CONHOH; and A1 and A2 are alkylene.

Abstract: An object of the present invention is to provide novel urea derivatives which have TNF-&agr; production inhibitory effects and are useful as therapeutic agents for various diseases, particularly as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. The urea derivatives according to the present invention are compounds represented by the formula [I] and salts thereof. In the formula, R1 is H, alkyl, phenyl or a group of the formula [`I]; R2 is H, alkyl, carboxyl or ester thereof or the like; R3 and R4 are each H, alkyl, cycloalkyl or the like; R5 is H, alkyl, hydroxy or the like; R6 is a nitrogen aromatic heterocycle; and A1 and A2 are alkylene.

Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.

Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.

Abstract: The present invention provides compounds represented by the following formula [I] or salts thereof which lower intraocular pressure by causing morphological change in trabecular meshwork cells. In the formula, R1 is H, lower alkyl, hydroxy, lower alkoxy or halogen, R2, R3 and R4 are H or lower alkyl, and . . . is a single bond or a double bond. When R3 and/or R4 is hydrogen, the amino can be protected by a protecting group.