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US 6,610,694 B1Granted
Condensed pyridazine compounds, their production and use
AssigneeTakeda Chemical Industries, Ltd.
InventorsYasuhiko Kawano, Hideaki Nagaya, Michiyo Gyoten
Life of this patent
Estimating the term…
Abstract
A condensed pyridazine derivative which exhibits anti-allergic activity, anti-histaminic activity and/or eosinophil chemotaxis-inhibiting activity, anti-inflammatory activity, anti-PAF (platelet-activating factor) activity, and the like, and is useful as an agent for preventing or treating asthma, allergic conjunctivitis, allergic rhinitis, urticaria, atopic dermatitis, and the like.
Claims28
A compound represented by the formula:
- wherein Ring A is a ring represented by the formula:
- wherein R1a is a hydrogen atom, a halogen atom, an alkyl group optionally having a substituent, an alkenyl group optionally having a substituent, an alkynyl group optionally having a substituent, a cycloalkyl group optionally having a substituent, an aryl group optionally having a substituent, an aralkyl group optionally having a substituent, an acyl group or a hydroxy group having a substituent;
- R1b is a hydrogen atom, a halogen atom, an alkyl group optionally having a substituent, an alkenyl group optionally having a substituent, an alkynyl group optionally having a substituent, a cycloalkyl group optionally having a substituent, an aryl group optionally having a substituent, an aralkyl group optionally having a substituent, an acyl group or a hydroxy group optionally having a substituent;
- Ar1 and Ar2 are independently a phenyl group optionally having a substituent;
- Ring B is a ring represented by the formula:
- wherein Z is a nitrogen atom or a methine group,
- Z1 and Z2 are each independently a linear C1-4 alkylene group optionally having a substituent;
- X and Y, whether identical or not, are
- (i) a bond,
- (ii) an oxygen atom,
- (iii) S(O)p
- wherein p is an integer from 0 to 2,
- (iv) NR4
- wherein R4 is a hydrogen atom or a lower alkyl group, or
- (v) a divalent linear lower hydrocarbon group which may have a substituent, and
- which may contain 1 to 3 hetero atoms;
- R2 and R3, whether identical or not, are a hydrogen atom, a halogen atom, an alkyl group optionally having a substituent, an alkenyl group optionally having a substituent, an alkynyl group optionally having a substituent, a cycloalkyl group optionally having a substituent, an aryl group optionally having a substituent, an aralkyl group optionally having a substituent, an acyl group or a hydroxy group optionally having a substituent;
- R7 is a hydrogen atom, a hydroxy group which may be substituted by lower alkyl or a carboxyl group;
- or a salt thereof
- or a pro-drug thereof.
17 more elements
A compound represented by the formula:
- wherein Ring A is a ring represented by the formula:
- wherein R1b is (1) a hydrogen atom, or
- (2) a C1-6 alkyl group which may be substituted by a group selected from the group consisting of
- (i) carboxyl,
- (ii) C1-6 alkoxy-carbonyl,
- (iii) C1-6 alkyl-carbonyloxy and
- (iv) C1-6 alkyl-carbonyloxy-C1-6 alkoxy-carbonyl;
- Ar1 and Ar2 are independently a phenyl group optionally having a substituent;
- Ring B is a ring represented by the formula:
- wherein Z is a nitrogen atom or a methine group,
- Z1 and Z2 are each independently a linear C1-4 alkylene group optionally having a substituent;
- X and Y, whether identical or not, are
- (i) a bond,
- (ii) an oxygen atom,
- (iii) S(O)p
- wherein p is an integer from 0 to 2,
- (iv) NR4
- wherein R4 is a hydrogen atom or a lower alkyl group, or
- (v) a divalent linear lower hydrocarbon group which may have a substituent, and which may contain 1 to 3 hetero atoms;
- R2 and R3, whether identical or not, are a hydrogen atom, a halogen atom, an alkyl group optionally having a substituent, an alkenyl group optionally having a substituent, an alkynyl group optionally having a substituent, a cycloalkyl group optionally having a substituent, an aryl group optionally having a substituent, an aralkyl group optionally having a substituent, an acyl group or a hydroxy group optionally having a substituent;
- R7 is a hydrogen atom, a hydroxy group which may be substituted by lower alkyl or a carboxyl group;
- or a salt thereof
- or a pro-drug thereof.
20 more elements
{circle around (1)} 6-[6-[4-(diphenylmethoxy)piperidino]hexyloxy][1,2,4]triazolo[4,3-b]pyridazine,
- {circle around (2)} 6-[6-[4-(diphenylmethoxy)piperidino]hexylamino][1,2,4]triazolo[4,3-b]pyridazine,
- {circle around (3)} 3-tert-butyl-6-[3-[4-(diphenylmethoxy)piperidino]propoxy][1,2,4]triazolo[4,3-b]pyridazine,
- {circle around (4)} 6-[3-[4-(diphenylmethoxy)piperidino]propylamino][1,2,4]triazolo[4,3-b]pyridazine-3-carboxylic acid, or a salt thereof.
{circle around (1)} 6-[3-[4-(diphenylmethoxy)piperidino]propylamino][1,2,4]triazolo[4,3-b]pyridazin-3(2H)-one,
- {circle around (2)} ethyl 2-[6-[3-[4-(diphenylmethoxy)piperidino]propylamino]-3-oxo[1,2,4]triazolo[4,3-b]pyridazin-2(3H)-yl]-2-methylpropionate,
- {circle around (3)} 2-[6-[3-[4-(diphenylmethoxy)piperidino]propylamino]-3-oxo[1,2,4]triazolo[4,3-b]pyridazin-2(3H)-yl]-2-methylpropionic acid,
- {circle around (4)} pivaloyloxymethyl 2-[6-[3-[4-(diphenylmethoxy)piperidino]propylamino]-3-oxo[1,2,4]triazolo[4,3-b]pyridazin-2(3H)-yl]-2-methylpropionate,
- {circle around (5)} pivaloyloxymethyl 2-[6-[3-[4-(diphenylmethoxy)piperidino]propoxy]-3-oxo[1,2,4]triazolo[4,3-b]pyridazin-2(3H)-yl]-2-methylpropionate, or a salt thereof.
1 more element
Dependencies are inferred from the claim text.