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1. 发明授权

EP0625140B1 CYCLOPROPYL N-HYDROXYUREA AND N-HYDROXYACETAMIDES WHICH INHIBIT LIPOXYGENASE 失效
标题翻译：环丙基-N-羟基硫代氨基甲酸
公开(公告)号：EP0625140B1
公开(公告)日：1996-12-11
申请号：EP92922190.1
申请日：1992-10-27
申请人： PFIZER INC.
发明人： IKEDA, Takafumi , KAWAI, Akiyoshi , MANO, Takashi , OKUMURA, Yoshiyuki , STEVENS, Rodney W.
IPC分类号： C07C275/64 , A61K31/17 , C07C323/44 , C07C259/06 , C07D295/15 , A61K31/16 , A61K31/40
CPC分类号： C07D295/15 , C07C259/06 , C07C275/64 , C07C323/44 , C07C2601/02
摘要： Compounds of formula (I) wherein A is C1 to C3 alkylene, Ar is phenyl or styryl, R is halosubstituted C1 to C3 alkyl, NHR' or (II), R' is hydrogen or C2 to C8 alkylthioalkyl, 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.
摘要翻译：式（I）的化合物，其中A为C1至C3亚烷基，Ar为苯基或苯乙烯基，R为卤素取代的C1至C3烷基，NHR'或（II），R'为氢或C2至C8烷硫基烷基，n为 1至4，p为2至5的整数，条件是当R'为氢时，Ar为苯乙烯基，其药学上可接受的盐抑制酶脂氧合酶，可用于治疗过敏和炎症和心血管已经涉及脂氧合酶作用的条件。这些化合物在用于治疗这些病症的药物组合物中形成活性成分。

2. 发明公开

EP0693054A1 CYCLOALKYLHYDROXYUREAS AND THEIR USE AS LIPOXYGENASE INHIBITORS 失效
标题翻译：环丙基甲基氧基羰基氧化物
公开(公告)号：EP0693054A1
公开(公告)日：1996-01-24
申请号：EP94910604.0
申请日：1994-04-05
申请人： PFIZER INC.
发明人： STEVENS, Rodney, W. , MANO, Takashi , OKUMURA, Yoshiyuki , NAKANE, Masami
IPC分类号： A61K31 , A61P29 , A61P37 , A61P43 , C07C273 , C07C275 , C07C323
CPC分类号： C07C275/64 , C07C323/47 , C07C2601/04 , C07C2601/08
摘要： The present invention provides a novel N-hydroxyurea compound of chemical formula (I) wherein R?1 and R2¿ are each independently hydrogen or C¿1?-C4 alkyl; Ar is phenyl or mono-, di- or trisubstituted phenyl; A is a valence bond or a C1-C6 alkylene chain, optionally having one double bond or one triple bond in the chain, and optionally having one or more C1-C4 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.
摘要翻译： PCT No.PCT / JP94 / 00567 Sec。 371日期1995年10月3日 102（e）日期1995年10月3日PCT 1994年4月5日PCT PCT。第WO94 / 22814号公报日期：1994年10月13日本发明提供了化学式（I）的新型N-羟基脲化合物，其中R 1和R 2各自独立地为氢或C 1 -C 4烷基; Ar是苯基或单，二或三取代的苯基; A是价键或C 1 -C 6亚烷基链，任选在链中具有一个双键或一个三键，并且任选地具有连接到链上的一个或多个C 1 -C 4烷基：X是氧或硫，n是 3〜6的整数; M是氢，药学上可接受的阳离子或代谢可切割基团：X和A可以连接在环上的任何可用位置。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，并用作用于治疗这些病症的药物组合物中的活性成分。

3. 发明授权

EP0693054B1 CYCLOALKYLHYDROXYUREAS AND THEIR USE AS LIPOXYGENASE INHIBITORS 失效
标题翻译： CYCLOALKYLHYDROXYHARNSTOFFE及其作为LIPOXY脱氢酶抑制剂
公开(公告)号：EP0693054B1
公开(公告)日：1998-06-10
申请号：EP94910604.1
申请日：1994-04-05
申请人： PFIZER INC.
发明人： STEVENS, Rodney, W. , MANO, Takashi , OKUMURA, Yoshiyuki , NAKANE, Masami
IPC分类号： C07C275/64 , A61K31/17
CPC分类号： C07C275/64 , C07C323/47 , C07C2601/04 , C07C2601/08
摘要： The present invention provides a novel N-hydroxyurea compound of chemical formula (I) wherein R and R are each independently hydrogen or C1-C4 alkyl; Ar is phenyl or mono-, di- or trisubstituted phenyl; A is a valence bond or a C1-C6 alkylene chain, optionally having one double bond or one triple bond in the chain, and optionally having one or more C1-C4 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.

4. 发明授权

EP0703913B1 IMIDAZOLES AS LIPOXYGENASE INHIBITORS 失效
标题翻译： AS的咪唑脂氧合酶抑制剂
公开(公告)号：EP0703913B1
公开(公告)日：1997-06-11
申请号：EP94916398.4
申请日：1994-05-25
申请人： PFIZER INC.
发明人： STEVENS, Rodney, W. , MANO, Takashi , ANDO, Kazuo
IPC分类号： C07D405/12 , C07D405/14 , C07D233/60 , C07D401/04
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/12 , C07D405/14
摘要： Certain novel imidazole derivatives having the ability to inhibit the lipoxygenase enzyme and having formula (I), wherein Y is hydrogen, C1-C8 alkyl, halosubstituted C1-C4 alkyl, phenyl, substituted phenyl, C7-C14 phenylalkyl, C7-C14 (substituted phenyl)alkyl, pyridyl, substituted pyridyl, C6-C13 pyridylalkyl or C6-C13 (substituted pyridyl)alkyl, wherein each substituent is independently halo, nitro, cyano, C1-C4 alkyl, C1-C4 alkoxy, halosubstituted C1-C4 alkyl, halosubstituted C1-C4 alkoxy, NR4R5, CO2R4 or CONR4R5, wherein R?4 and R5¿ are each, independently, hydrogen or C¿1?-C6 alkyl; Ar?1 and Ar2¿ are each, independently, phenylene, mono-substituted phenylene or di-substituted phenylene, wherein the substituents are, independently, halo, C¿1?-C4 alkyl, C1-C4 alkoxy, halo-substituted C1-C4 alkyl or halo-substituted C1-C4 alkoxy; X and X?1¿ are each, independently, O, S, SO or SO¿2; R?1 is hydrogen or C¿1?-C4 alkyl; and R?2 and R3¿ are each, independently, methylene, ethylene or propylene. These compounds are useful for the treatment of disease states such as bronchial asthma, skin disorders and arthritis in mammals, and as the active ingredient in pharmaceutical compositions for treating such conditions.

5. 发明授权

EP0559743B1 NOVEL HYDROXAMIC ACID AND N-HYDROXYUREA DERIVATIVES AND THEIR USE 失效转让
标题翻译：异羟肟和N-羟基脲及其用途的衍生物。
公开(公告)号：EP0559743B1
公开(公告)日：1995-03-08
申请号：EP92900454.7
申请日：1991-11-13
申请人： PFIZER INC.
发明人： IKEDA, Takafumi , KAWAI, Akiyoshi , MANO, Takashi , OKUMURA, Yoshiyuki 362, Giro, Okuda , STEVENS, Rodney, William
IPC分类号： C07C273/18 , C07C275/64 , A61K31/17
CPC分类号： C07D271/07 , C07C275/64 , C07C311/59 , C07C323/47 , C07C335/40 , C07C2601/04 , C07C2601/08 , C07D307/52
摘要： Certain novel hydroxamic acid derivatives having structure (I), 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.

6. 发明公开

EP0787127A1 5-LIPOXYGENASE INHIBITORS 失效
标题翻译： 5脂氧合酶抑制剂
公开(公告)号：EP0787127A1
公开(公告)日：1997-08-06
申请号：EP95918121.0
申请日：1995-05-29
申请人： PFIZER INC.
发明人： STEVENS, Rodney, W. , MANO, Takashi , NAKAO, Kazunari , OKUMURA, Yoshiyuki
IPC分类号： A61K31 , A61P9 , A61P29 , A61P37 , A61P43 , C07D233 , C07D309 , C07D405 , C07D521
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D309/08
摘要： Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having formula (I) and the pharmaceutically acceptable salts thereof, wherein Ar1 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 X1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C¿1-4? alkyl and the like; X?1¿ is a direct bond or C¿1-4? alkylene; Ar?2¿ is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X2 is -A-X- or -X-A- wherein A is a direct bond or C¿1-4? alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar?3¿ is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C¿1-4? alkyl and the like; R?1 and R2¿ are each C¿1-4? alkyl, or together they form a group of formula -D?1-Z-D2¿- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D?1 and D2¿ are C¿1-4? alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D?1 and D2¿ may be substituted by C¿1-3? alkyl; and Y is CONR?3R4¿, CN, C(R?3)=N-OR4, COOR3, COR3¿ or CSNR3R4, wherein R?3 and R4¿ are each H or C¿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.

7. 发明公开

EP0703913A1 IMIDAZOLE LIPOXYGENASE INHIBITORS 失效
标题翻译：咪唑脂氧合酶抑制剂
公开(公告)号：EP0703913A1
公开(公告)日：1996-04-03
申请号：EP94916398.0
申请日：1994-05-25
申请人： PFIZER INC.
发明人： STEVENS, Rodney, W. , MANO, Takashi , ANDO, Kazuo
IPC分类号： A61K31 , A61P9 , A61P11 , A61P17 , A61P19 , A61P25 , A61P29 , A61P37 , A61P43 , C07D233 , C07D305 , C07D309 , C07D405 , C07D521
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/12 , C07D405/14

8. 发明公开

EP0625140A1 CYCLOPROPYL N-HYDROXYUREA AND N-HYDROXYACETAMIDES WHICH INHIBIT LIPOXYGENASE 失效
标题翻译：环丙氧基-N-羟基硫代氨基甲酰胆碱酯酶。
公开(公告)号：EP0625140A1
公开(公告)日：1994-11-23
申请号：EP92922190.0
申请日：1992-10-27
申请人： PFIZER INC.
发明人： IKEDA, Takafumi , KAWAI, Akiyoshi , MANO, Takashi , OKUMURA, Yoshiyuki , STEVENS, Rodney W.
IPC分类号： A61K38 , C07C259 , C07C275 , C07C323 , C07D295
CPC分类号： C07D295/15 , C07C259/06 , C07C275/64 , C07C323/44 , C07C2601/02
摘要： Composés de la formule (I) dans laquelle A représente alkylène C1 à C3, Ar représente phényle ou styryle, R représente alkyle C1 à C3 à substitution par halogène, NHR' ou (II), R' représente hydrogène ou alkylthioalkyle C2 à C8, n représente un entier compris entre 1 et 4, et p représente un entier compris entre 2 et 5, à condition que, lorsque R' représente hydrogène, Ar représente styryle. Ces composés, ainsi que leurs sels phramaceutiquement acceptables, inhibent la lipoxygénase et servent à traiter des allergies et des effections inflammatoires et cardiovasculaires impliquant l'activité de la lipoxygénase. Ces composés constituent le principe actif dans des compositions pharmaceutiques servant à traiter de telles affections.
摘要翻译：式（I）的化合物，其中A为C1至C3亚烷基，Ar为苯基或苯乙烯基，R为卤素取代的C1至C3烷基，NHR'或（II），R'为氢或C2至C8烷硫基烷基，n为 1至4，p为2至5的整数，条件是当R'为氢时，Ar为苯乙烯基，其药学上可接受的盐抑制酶脂氧合酶，可用于治疗过敏和炎症和心血管已经涉及脂氧合酶作用的条件。这些化合物在用于治疗这些病症的药物组合物中形成活性成分。

9. 发明授权

EP0787127B1 5-LIPOXYGENASE INHIBITORS 失效
标题翻译： 5脂氧合酶抑制剂
公开(公告)号：EP0787127B1
公开(公告)日：2001-01-03
申请号：EP95918121.5
申请日：1995-05-29
申请人： PFIZER INC.
发明人： STEVENS, Rodney, W. , MANO, Takashi , NAKAO, Kazunari , OKUMURA, Yoshiyuki
IPC分类号： C07D233/60 , C07D405/12 , A61K31/415
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D309/08
摘要： Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having formula (I) and the pharmaceutically acceptable salts thereof, wherein Ar1 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 X1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C¿1-4? alkyl and the like; X?1¿ is a direct bond or C¿1-4? alkylene; Ar?2¿ is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X2 is -A-X- or -X-A- wherein A is a direct bond or C¿1-4? alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar?3¿ is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C¿1-4? alkyl and the like; R?1 and R2¿ are each C¿1-4? alkyl, or together they form a group of formula -D?1-Z-D2¿- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D?1 and D2¿ are C¿1-4? alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D?1 and D2¿ may be substituted by C¿1-3? alkyl; and Y is CONR?3R4¿, CN, C(R?3)=N-OR4, COOR3, COR3¿ or CSNR3R4, wherein R?3 and R4¿ are each H or C¿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.

10. 发明授权

EP0863905B1 IMIDAZOLE LIPOXYGENASE INHIBITORS 失效转让
标题翻译：咪唑脂氧合酶抑制剂
公开(公告)号：EP0863905B1
公开(公告)日：2000-11-29
申请号：EP96923010.1
申请日：1996-07-24
申请人： PFIZER INC.
发明人： MANO, Takashi , STEVENS, Rodney, W.
IPC分类号： C07D493/08 , A61K31/35
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The present invention provides a compound of formula (I) and a pharmaceutically acceptable salt thereof, wherein Ar is phenylene optionally substituted with halo, hydroxy, cyano, amino, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 halo-substituted alkyl or C1-C4 halo-substituted alkoxy; X is -A-X?1- or -X1¿-A-, wherein A is a direct bond or C¿1?-C4 alkylene, and X?1¿ is oxy, thio, sulfinyl or sulfonyl; Ar1 is phenylene, pyridylene or thienylene optionally substituted with halo, hydroxy, cyano, nitro, amino, C¿1?-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 halo-substituted alkyl, C1-C4 halo-substituted alkoxy, C1-C4 alkylamino or di(C1-C4)alkylamino; Y is CN or CONR?1R2¿ wherein R?1 and R2¿ are independently hydrogen or C¿1?-C4 alkyl; and R is hydrogen or C1-C6 alkyl; W is C2-C3 alkylene, one carbon atom of which may be replaced by an oxygen atom. Further the invention provides a pharmaceutical composition for treating an inflammatory disease, allergy or cardiovascular diseases or the like in a mammalian subject which comprises a compound of formula (I) and a pharmaceutically acceptable carrier.

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