摘要:
The present invention provides a novel N-hydroxyurea compound of chemical formula (I) wherein R.sup.1 and R.sup.2 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl; Ar is phenyl or mono-, di- or trisubstituted phenyl; A is a valence bond or a C.sub.1 -C.sub.6 alkylene chain, optionally having one double bond or one triple bond in the chain, and optionally having one or more C.sub.1 -C.sub.4 alkyl groups attached to the chain: X is oxygen or sulfur, n is an integer of 3 to 6; M is hydrogen, pharmaceutically acceptable cation or a metabolically cleavable group: and X and A may be attached at any available position on the ring. These compounds are useful for treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
摘要:
Certain novel hydroxamic acid derivatives having the structure inhibit the enzyme lipoxygenase. These compounds, and the pharmaceutically acceptable salts thereof, are useful in the treatment or alleviation of inflammatory diseases, allergic conditions and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
摘要:
Compounds of formula I ##STR1## or salts thereof, where R is alkyl, phenyl, phenoxy or substituted phenyl and phenoxy; X is S or O; n is an integer of 1 or 2; A is --CH.sub.2 -- or --CH(CH.sub.3)--; and B is hydrogen or methyl, useful as antiallergy and antiinflammatory agents.
摘要:
Certain 6-aryl- or 6-heteroaryl- alkylaminobenzoxazolones, and their pharmaceutically-acceptable salts, are dual inhibitors of lipoxygenase and cyclooxygenase enzymes, and so are useful as antiallergy and antiinflammatory agents.
摘要:
This invention relates to certain benzoxazolinones which inhibit lipoxygenase and/or cyclooxygenase enzymes. Such compounds are useful in inhibiting such enzymes, per se, and are useful in treating allergic and inflammatory conditions in a mammal. This invention also relates to methods of inhibiting lipoxygenase and/or cyclooxygenase in a mammal with such benzoxazolinones; methods of treating an allergic condition in a mammal with such compounds; methods of treating an inflammatory condition in a mammal with such compounds; and pharmaceutical compositions comprising the benzoxazolinones hereof.
摘要:
This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof, wherein Ar is heteroaryl; X1 and X2 are independently selected from halo, C1-C4 alkyl, hydroxy, C1-C4 alkoxy, amino, C1-C4 alkanoyl, carboxy, carbamoyl, cyano, nitro, mercapto, (C1-C4 alkyl)thio, (C1-C4 alkyl)sulfinyl, (C1-C4 alkyl)sulfonyl, aminosulfonyl, or the like; R1 is selected from hydrogen, straight or branched C1-C4 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, phenyl, heteroaryl and the like; R2 and R3 are independently selected from hydrogen, halo, C1-C4 alkyl, phenyl and the like; or R1 and R2 can form, together with the carbon atom to which they are attached, a C5-C7 cycloalkyl ring; and m and n are independently 0, 1, 2 or 3. These compounds and pharmaceutical compositions containing such compounds are useful as analgesics and anti-inflammatory agents.
摘要:
This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof, wherein Ar is heteroaryl; X1 and X2 are independently selected from halo, C1-C4 alkyl, hydroxy, C1-C4 alkoxy, amino, C1-C4 alkanoyl, carboxy, carbamoyl, cyano, nitro, mercapto, (C1-C4 alkyl)thio, (C1-C4 alkyl)sulfinyl, (C1-C4 alkyl)sulfonyl, aminosulfonyl, or the like; R1 is selected from hydrogen, straight or branched C1-C4 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, phenyl , heteroaryl and the like; R2 and R3 are independently selected from hydrogen, halo, C1-C4 alkyl, phenyl and the like; or R1 and R2 can form, together with the carbon atom to which they are attached, a C5-C7 cycloalkyl ring; and m and n are independently 0, 1, 2 or 3. These compounds and pharmaceutical compositions containing such compounds are useful as analgesics and anti-inflammatory agents.
摘要:
Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.1-4 alkyl, or together they form a group of formula --D.sup.1 --Z--D.sup.2 -- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D.sup.1 and D.sup.2 are C.sub.1-4 alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D.sup.1 and D.sup.2 may be substituted by C.sub.1-3 alkyl; and Y is CONR.sup.3 R.sup.4, CN, C(R.sup.3).dbd.N--OR.sup.4, COOR.sup.3, COR.sup.3 or CSNR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are each H or C.sub.1-4 alkyl. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
摘要翻译:具有抑制5-脂肪氧合酶并具有下式I的能力的新型化合物:其中Ar1是选自咪唑基,吡咯基,吡唑基,1,2,3或3位的杂环部分 三唑基,1,2,4-三唑基,吲哚基,吲唑基和苯并咪唑基,其通过环氮原子与X1键合,并且其可任选被一个或两个选自卤素,羟基,氰基,氨基和 C 1-4烷基; X1是直接键或C1-4亚烷基; Ar 2是任选被卤素,羟基,氰基取代的亚苯基,氨基X2是-A-X-或-X-A-,其中A是直接键或C 1-4亚烷基,X是氧基,硫代,亚磺酰基或磺酰基; Ar 3是任选被一个或两个选自卤素,羟基,氰基,氨基和C 1-4烷基的取代基取代的亚苯基,亚吡啶基,亚噻吩基,呋喃基,恶唑基或噻唑基; R1和R2各自为C1-4烷基,或者它们一起形成式-D1-Z-D2-的基团,与其所连接的碳原子一起形成具有3至8个原子的环,其中D1和D2是 C 1-4亚烷基,Z是直接键或氧基,硫基,亚磺酰基,磺酰基或亚乙烯基,D1和D2可以被C 1-3烷基取代; 并且Y是CONR 3 R 4,CN,C(R 3)= N-OR 4,COOR 3,COR 3或CSNR 3 R 4,其中R 3和R 4各自为H或C 1-4烷基。 这些化合物可用于治疗或缓解哺乳动物的炎性疾病,变态反应和心血管疾病,并用作治疗这些病症的药物组合物中的活性成分。
摘要:
Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; R.sup.1 and R.sup.2 are each C.sub.1-4 alkyl, or together they form a group of formula --D.sup.1 --Z--D.sup.2 -- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D.sup.1 and D.sup.2 are C.sub.1-4 alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D.sup.1 and D.sup.2 may be substituted by C.sub.1-3 alkyl; and Y is CONR.sup.3 R.sup.4, CN, C(R.sup.3).dbd.N--OR.sup.4, COOR.sup.3, COR.sup.3 or CSNR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are each H or C.sub.1-4 alkyl. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
摘要翻译:具有抑制5-脂肪氧合酶并具有下式I的能力的新型化合物及其药学上可接受的盐,其中Ar1是选自咪唑基,吡咯基,吡唑基,1,2,3-三唑基, ,2,4-三唑基,吲哚基,吲唑基和苯并咪唑基,其通过环氮原子与X1连接,并且其可任选被一个或两个选自卤素,羟基,氰基,氨基,C 1-4烷基的取代基取代, 类似; X1是直接键或C1-4亚烷基; Ar 2是任选被卤素,羟基,氰基,氨基等取代的亚苯基; X2是-A-X或-X-A-,其中A是直接键或C 1-4亚烷基,X是氧基,硫代,亚磺酰基或磺酰基; Ar 3是任选被一个或两个选自卤素,羟基,氰基,氨基,C 1-4烷基等的取代基取代的亚苯基,亚吡啶基,亚噻吩基,呋喃基,恶唑基或噻唑基; R1和R2各自为C1-4烷基,或者它们一起形成式-D1-Z-D2-的基团,与其所连接的碳原子一起形成具有3至8个原子的环,其中D1和D2是 C 1-4亚烷基,Z是直接键或氧基,硫基,亚磺酰基,磺酰基或亚乙烯基,D1和D2可以被C 1-3烷基取代; 并且Y是CONR 3 R 4,CN,C(R 3)= N-OR 4,COOR 3,COR 3或CSNR 3 R 4,其中R 3和R 4各自为H或C 1-4烷基。 这些化合物可用于治疗或缓解哺乳动物的炎性疾病,变态反应和心血管疾病,并用作治疗这些病症的药物组合物中的活性成分。
摘要:
Compounds of the formula ##STR1## wherein A is C1 to C3 alkylene, Ar is phenyl or styryl, R is halosubstituted C1 to C3 alkyl, NHR' or ##STR2## R' is hydrogen or C2 to C8 alkytthioalkyl, n is an integer of from 1 to 4 and p is an integer of from 2 to 5, with the proviso that when R' is hydrogen then Ar is styryl, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.