NKT cell-activating agents containing α-glycosylceramides
AssigneeKirin Beer Kabushiki Kaisha
InventorsMasaru Taniguchi, Tetsu Kawano, Yasuhiko Koezuka
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Abstract
An objective of the present invention is to provide NKT cell-activating agents, therapeutic agents for autoimmune diseases (for example, systemic lupus erythematosus, systemic sclerosis, ulcerative colitis, encephalomyelitis, multiple sclerosis and human type I diabetes), and abortifacients. The medicinal compositions according to the present invention comprise α-glycosylceramides of the following formula (I), or a salt or a solvate thereof as an active ingredient.
Claims30
A method for treating an autoimmune disease comprising the step of administering a compound of formula (I) or a salt or a solvate thereof to a mammal including a human in need thereof:
- wherein R1 to R9 and X are as defined wherein
- R1 represents H or OH,
- X represents an integer between 7 and 27,
- R2 represents a substituent selected from the group consisting of the following (a) to (e), wherein Y represents an integer between 5 and 17:
- (a) —CH2(CH2)yCH3
- (b) —CH(OH)(CH2)yCH3
- (c) —CH(OH)(CH2)yCH(CH3)2
- (d) —CH═CH(CH2)yCH3
- (e)—CH(OH)(CH2)yCH(CH3)CH2CH3, and
- R3 to R9 represent substituents as defined in any one of the following (i) to (ii):
- (i) when R3, R6 and R8 represent H,
- R4 represents H, OH, NH2, NHCOCH3, or a substituent selected from the group consisting of the following groups (A) to (D):
- R5 represents OH or a substituent selected from the group consisting of the following groups (E) and (F):
- R7 represents OH or a substituent selected from the group consisting of the following groups (A) to (D):
- R9 represents H, CH3, CH2OH or a substituent selected from the group consisting of the following groups (A) to (D):
- (ii) when R3, R6 and R7 represent H, R4 represents H, OH, NH2, NHCOCH3, or a substituent selected from the group consisting of the following groups (A) to (D):
- R5 represents OH or a substituent selected from the group consisting of groups (E) and (F):
- R8 represents OH or a substituent selected from the group consisting of the following groups (A) to (D):
- and
- R9 represents H, CH3, CH2OH or a substituent selected from the group consisting of the following groups (A) to (D):
A method for inducing abortion which comprises the step of administrating a compound of formula (I) or a salt or a solvate thereof to a mammal including a human in need thereof:
- wherein R1 to R9 and X are as defined wherein
- R1 represents H or OH,
- X represents an integer between 7 and 27,
- R2 represents a substituent selected from the group consisting of the following (a) to (e), wherein Y represents an integer between 5 and 17:
- (a) —CH2(CH2)yCH3
- (b) —CH(OH)(CH2)yCH3
- (c) —CH(OH)(CH2)yCH(CH3)2
- (d) —CH═CH(CH2)yCH3
- (e)—CH(OH)(CH2)yCH(CH3)CH2CH3, and
- R3 to R9 represent substituents as defined in any one of the following (i) to (ii):
- (i) when R3, R6 and R8 represent H,
- R4 represents H, OH, NH2, NHCOCH3, or a substituent selected from the group consisting of the following groups (A) to (D):
- R5 represents OH or a substituent selected from the group consisting of the following groups (B) and (F):
- R7 represents OH or a substituent selected from the group consisting of the following groups (A) to (D):
- R9 represents H, CH3, CH2OH or a substituent selected from the group consisting of the following groups (A) to (D):
- (ii) when R3, R6 and R7 represent H, R4 represents H, OH, NH2, NHCOCH3, or a substituent selected from the group consisting of the following groups (A) to (D):
- R5 represents OH or a substituent selected from the group consisting of groups (E) and (F):
- R8 represents OH or a substituent selected from the group consisting of the following groups (A) to (D):
- and
- R9 represents H, CH3, CH2OH or a substituent selected from the group consisting of the following groups (A) to (D):
Dependencies are inferred from the claim text.