摘要:
Provided are a novel compound having an antagonistic activity for the P2X 7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X 7 receptor. A compound represented by Formula (I):
wherein Z 1 is C(R 4 ) or the like; R 4 is a hydrogen atom or the like; Z 2 is C(R 5a )(R 5a' ) or the like; the dashed line represents the presence or absence of a bond; when the dashed line represents the presence of a bond, then R 5a' is absent; R 5a and R 5a' are each independently a hydrogen atom or the like; Ring Q is a substituted or unsubstituted 5-membered non-aromatic heterocycle or the like; Y 1 is O or the like; R 2a is a group represented by the formula: -(C(R 2a' )(R 2b' )) n -R 1 ; R 2b is a hydrogen atom or the like; R 2a' and R 2b' is each independently a hydrogen atom or the like; R 1 is substituted or unsubstituted aromatic carbocyclyl or the like; X is N(R 7a ) or the like; R 7a is a hydrogen atom or the like; R 3 is substituted or unsubstituted aromatic carbocyclyl or the like; n is an integer from 0 to 4; and m is an integer from 0 to 4, or a pharmaceutically acceptable salt thereof.
摘要:
The present invention provides useful compounds for HIV protease inhibitor. A compound represented by formula or its pharmaceutically acceptable salt Formula:
wherein ring A is
R 4 is -Y-Z, hydrogen atom, halogen, hydroxy and the like, R 5 is hydrogen atom, halogen, hydroxy and the like, R 6 is each independently halogen, hydroxy, carboxy and the like, ring A may be substituted with said R 6 at any substitutable position(s), a is an integer of 0 to 7, ring B is substituted or unsubstituted aromatic carbocyclyl, or substituted or unsubstituted aromatic heterocyclyl, ring C is substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, or substituted or unsubstituted non-aromatic heterocyclyl, R 1 is -Y-Z, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl and the like, R 2 and R 3 are each independently -Y-Z or hydrogen atom, provided that at least one of R 1 , R 2 , R 3 and R 4 is a group represented by formula: -Y-Z, Y is a bond, or a spacer of any combination selected from the group consisting of -O-, -S-, -NR 7 -, -C(=O)-, -SO-, -SO 2 -, -NR 7 -C(=O)-, -C(=O)-NR 7 -, -NR 7 -C(=O)-NR 7 -, -NR 7 -C(=O)-O-, -SO 2 -NR 7 -, -NR 7 -SO 2 -, substituted or unsubstituted alkylene, substituted or unsubstituted alkenylene, substituted or unsubstituted alkynylene, substituted or unsubstituted aromatic carbocyclediyl, substituted or unsubstituted non-aromatic carbocyclediyl, substituted or unsubstituted aromatic heterocyclediyl and substituted or unsubstituted non-aromatic heterocyclediyl, R 7 are each independently hydrogen atom, hydroxy, carboxy and the like, and Z is substituted aromatic carbocyclyl, substituted non-aromatic carbocyclyl, substituted aromatic heterocyclyl or substituted non-aromatic heterocyclyl.
摘要翻译:本发明提供了用于HIV蛋白酶抑制剂的有用化合物。 由式或其药学上可接受的盐表示的化合物或其药学上可接受的盐式:其中环A为R 4为-YZ,氢原子,卤素,羟基等,R 5为氢原子,卤素,羟基等,R 6各自独立地为卤素,羟基 ,羧基等,环A可以在任何可取代的位置被所述R6取代,a是0-7的整数,环B是取代或未取代的芳族碳环基或取代或未取代的芳族杂环基,环C是 取代或未取代的芳族碳环基,取代或未取代的非芳族碳环基,取代或未取代的芳族杂环基或取代或未取代的非芳族杂环基,R1是-YZ,取代或未取代的烷基,取代或未取代的烯基, 例如,R2和R3各自独立地是-YZ或氢原子,条件是R1,R2,R3和R4中的至少一个是由式-YZ表示的基团, Y是键,或选自-O - , - S - , - NR 7 - , - C(= O) - , - SO - , - SO 2 - , - NR 7 -C (= O)-NR 7 - , - NR 7 -C(= O)-NR 7 - , - NR 7 -C(= O)-O - , - SO 2 -NR 7 - ,取代或未取代的亚烷基,取代或未取代的亚烯基,取代或未取代的亚炔基,取代或未取代的芳族碳环基,取代或未取代的非芳族碳环基,取代或未取代的芳族杂环二基和取代或未取代的非芳族杂环二基, ,羟基,羧基等,Z是取代的芳族碳环基,取代的非芳族碳环基,取代的芳族杂环基或取代的非芳族杂环基。
摘要:
Disclosed is a compound which is useful as an endothelial lipase inhibitor. A compound represented by the formula:
its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is aromatic carbocycle or aromatic heterocycle, Z is -NR 5 -, -O- or -S-, R 5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl or the like, R 1 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R 2 and R 3 are each independently hydrogen, halogen, hydroxy or the like, R 4 is a group represented by the formula: -(CR 6 R 7 )n-R 8 , wherein R 6 and R 7 are each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, R 8 is carboxy, cyano, substituted or unsubstituted alkyl or the like, R x is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, m is an integer of 0 to 3.
摘要:
Disclosed is a compound useful as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1. A compound represented by the formula:
a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is a group of the formula: -C(=O)NR 4 R 5 , (wherein R 4 and R 5 are each independently, hydrogen, optionally substituted alkyl or the like) or a group of the formula: -NR 6 C(=O)R 7 , (wherein R 6 and R 7 are each independently, hydrogen, optionally substituted alkyl or the like), X and Y are each independently -0- or the like, Z is a bond or the like, R 2 is optionally substituted alkyl, optionally substituted alkenyl or the like, R 3 is optionally substituted alkyl, optionally substituted alkenyl or the like.
摘要:
Novel compounds having D3 receptor antagonistic activity are provided. A compound represented by formula (I):
wherein ring A is a heterocycle, X 1 is each independently CR 4a R 4b , X 2 is each independently CR 4c R 4d , Y 1 and Y 2 are each independently a carbon atom or a nitrogen atom, L is -N(R 6 )-C(=O)- or the like, W is cyclyl or the like, R 2 and R 3 are each independently substituted or unsubstituted alkyl or the like, R 1a , R 1b , R 4a to R 4d , and R 6 are each independently hydrogen atoms or the like, p is 1 or 2, q is an integer of 1 to 3, n is an integer of 1 to 4, s is an integer of 0 to 4, or a pharmaceutically acceptable salt thereof.
摘要:
Disclosed is a compound useful as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1. A compound represented by the formula:
a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is a group of the formula: -C(=O)NR 4 R 5 , (wherein R 4 and R 5 are each independently, hydrogen, optionally substituted alkyl or the like) or a group of the formula: -NR 6 C(=O)R 7 , (wherein R 6 and R 7 are each independently, hydrogen, optionally substituted alkyl or the like), X and Y are each independently -0- or the like, Z is a bond or the like, R 2 is optionally substituted alkyl, optionally substituted alkenyl or the like, R 3 is optionally substituted alkyl, optionally substituted alkenyl or the like.
摘要:
Disclosed is a compound useful as a type I 11βhydroxysteroid dehydrogenase inhibitor. A compound represented by the formula:
a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is optionally substituted alkyl or the like, one of R 2 and R 4 is a group of formula: -Y-R 5 , wherein Y is -O- or the like, R 5 is substituted alkyl (the substituent is optionally substituted cycloalkyl or the like), optionally substituted branched alkyl or the like, the other of R 2 and R 4 is hydrogen or optionally substituted alkyl, R 3 is a group of formula: -C(=O)-Z-R 6 , wherein Z is -NR 7 - or -NR 7 -W-, R 6 is optionally substituted cycloalkyl or the like, R 7 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, X is =N- or the like, with the proviso that compounds wherein R 2 is 2-(morphorino)ethoxy, R 3 is N-(1-adamantyl)carbamoyl and R 1 is benzyl are excluded.
摘要:
Disclosed is an adamantanamine derivative which is useful as a significant intermediate of an 11βHSD-1 inhibitor. Disclosed is a compound represented by the formula (II):
wherein R 10 is a group represented by the formula: -(CR 13 R 14 )m-NR 12 -R 11 or the like.