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US 8,299,296 B2Granted
Spiro compounds and pharmaceutical use thereof
AssigneeJapan Tobacco Inc.
InventorsTakashi Shimada, Hiroshi Ueno, Kazuhiro Tsutsumi, Kouichi Aoyagi, Tomoyuki Manabe, Shin-Ya Sasaki, Susumu Katoh
Life of this patent
Estimating the term…
Abstract
The spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereof
Claims44
A spiro compound of the following general formula [Ia]:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is
- (1) a hydrogen atom,
- (2) a C1-C6 alkyl group,
- (3) a C2-C6 alkenyl group,
- (4) a C2-C6 alkynyl group,
- (5) a C1-C6 alkoxy group,
- (6) a hydroxy C1-C6 alkyl group,
- (7) a C1-C6 alkoxy(C1-C6)alkyl group,
- (8) —CONR11R12 in which R11 and R12 are the same or different and each represents a hydrogen atom or a C1-C6 alkyl group,
- (9) a phenyl group or
- (10) a five-membered heteroaryl group which has at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, and which is optionally substituted by a C1-C6 alkyl group;
- R2 is
- (1) a halogen atom,
- (2) a C1-C6 alkyl group,
- (3) a hydroxy group or
- (4) a C1-C6 alkoxy group;
- p is 0, 1, 2 or 3;
- X is a carbon atom or a nitrogen atom;
- m1 is 0, 1 or 2;
- m2 is 0 or 1;
- spiro-ring AB is optionally substituted by 1 to 5 same or different substituent(s) selected from the group consisting of
- (1) a hydroxy group,
- (2) a C1-C6 alkyl group,
- (3) a C1-C6 alkoxy group and
- (4) an oxo group;
- n1 is 0, 1, 2, 3 or 4;
- n2 is 1, 2, 3 or 4;
- n3 is 0, 1 or 2 with the proviso that n2+n3 is 2, 3 or 4;
- and
- a bond represented by the symbol:
- means a single bond or a double bond with the proviso that three contiguous carbon atoms do not constitute an allene bond represented by the formula:
- C═C═C.
30 more elements
A spiro compound of the following general formula [I]:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is
- (1) a hydrogen atom,
- (2) a C1-C4 alkyl group,
- (3) a C2-C4 alkenyl group,
- (4) a C2-C4 alkynyl group,
- (5) a C1-C4 alkoxy group,
- (6) a hydroxy C1-C4 alkyl group,
- (7) a C1-C4 alkoxy(C1-C4)alkyl group,
- (8) —CONR11R12 in which R11 and R12 are the same or different and each represents a hydrogen atom or a C1-C4 alkyl group,
- (9) a phenyl group or
- (10) a five-membered heteroaryl group which has at least one heteroatom selected from a nitrogen atom, an oxygen atom and a sulfur atom, and which is optionally substituted by a C1-C4 alkyl group;
- m1 is 0, 1 or 2;
- m2 is 0 or 1;
- spiro-ring AB is optionally substituted by 1 to 5 same or different substituent(s) selected from
- (1) a hydroxy group and
- (2) a C1-C4 alkyl group;
- n1 is 2, 3 or 4;
- n2 is 1, 2 or 3;
- n3 is 0, 1 or 2 with the proviso that n2+n3 is 2 or 3;
- and
- a bond represented by the symbol:
- means a single bond or a double bond with the proviso that three contiguous carbon atoms do not constitute an allene bond represented by the formula:
- C═C═C.
21 more elements
Dependencies are inferred from the claim text.