公开(公告)号：US06949536B2

公开(公告)日：2005-09-27

申请号：US10771861

申请日：2004-02-03

申请人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

发明人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

IPC分类号： A61K31/33 ,  A61K31/4025 ,  A61K31/422 ,  A61K31/425 ,  A61K31/427 ,  A61K31/454 ,  C07D233/00 ,  C07D277/00 ,  C07D333/00

CPC分类号： A61K31/422 ,  A61K31/427 ,  A61K31/454 ,  C07C311/39 ,  C07C317/36 ,  C07D207/325 ,  C07D207/333 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

摘要： This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl; halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring. R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐，其中A是部分不饱和或不饱和的五元杂环或部分不饱和或不饱和的五元碳环，其中4-（磺酰基）苯基和4-取代的苯基 在式（I）中，与环A相邻的环原子相连; R 1是任选取代的芳基或杂芳基，条件是当A是吡唑时，R 1是杂芳基; R 2是C 1-4烷基; 卤素取代的C 1-4烷基，C 1-4烷基氨基，C 1-4烷基氨基或氨基; R 4，R 4和R 5独立地是氢，卤素，C 1-4烷基，卤代 - 取代的C 1-4烷基等; 或者R 3，R 4和R 5中的两个与它们所连接的原子一起形成4-7元环 。 R 6和R 7独立地是氢，卤素，C 1-4烷基，卤素取代的C 1-4烷基， C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-4烷基氨基或N，N-二C < 烷基氨基; m和n分别为1,2,3或4.本发明还提供了一种药物组合物，其用于治疗前列腺素涉及病原体的医疗状况。

公开(公告)号：US06294558B1

公开(公告)日：2001-09-25

申请号：US09446049

申请日：1999-12-15

申请人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

发明人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

IPC分类号： A61K3144

CPC分类号： C07D207/335 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

摘要： This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐，其中A是部分不饱和或不饱和的五元杂环或部分不饱和或不饱和的五元碳环，其中4-（磺酰基）苯基和4-取代的苯基 在式（I）中，与环A相邻的环原子相连; R1是任选取代的芳基或杂芳基，条件是当A是吡唑时，R 1是杂芳基; R 2是C 1-4烷基，卤素取代的C 1-4烷基，C 1-4烷基氨基，C 1-4二烷基氨基或氨基; R 3，R 4和R 5独立地为氢，卤素，C 1-4烷基，卤素取代的C 1-4烷基等; 或者R 3，R 4和R 5中的两个与它们所连接的原子一起形成4-7元环; R 6和R 7独立地是氢，卤素，C 1-4烷基，卤素取代的C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-4烷基氨基或N，N-二C 1-4烷基氨基; m和n分别为1,2,3或4.本发明还提供了一种药物组合物，其用于治疗前列腺素涉及病原体的医疗状况。

公开(公告)号：US06727238B2

公开(公告)日：2004-04-27

申请号：US10465767

申请日：2003-06-18

申请人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

发明人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

IPC分类号： A61K3133

CPC分类号： A61K31/422 ,  A61K31/427 ,  A61K31/454 ,  C07C311/39 ,  C07C317/36 ,  C07D207/325 ,  C07D207/333 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

摘要： This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo,, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐，其中A是部分不饱和或不饱和的五元杂环或部分不饱和或不饱和的五元碳环，其中4-（磺酰基）苯基和4-取代的苯基 在式（I）中，与环A相邻的环原子相连; R 1是任选取代的芳基或杂芳基，条件是当A是吡唑时，R 1是杂芳基; R 2是C 1-4烷基，卤素取代的C 1-4烷基，C 1-4烷基氨基，C 1-4二烷基氨基或氨基; R 3，R 4和R 5独立地是氢，卤素，C 1-4烷基，卤素取代的C 1-4烷基等; 或R 3，R 4和R 5中的两个与它们所连接的原子一起形成4-7元环; R 6和R 7独立地是氢，卤素，C 1-4烷基，卤素取代的C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-4烷基氨基或N，N-二C1- 4烷基氨基; 并且m和n独立地为1,2,3或4.本发明还提供了可用于治疗前列腺素作为病原体的医学病症的药物组合物。

公开(公告)号：US06608095B2

公开(公告)日：2003-08-19

申请号：US09841348

申请日：2001-04-24

申请人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

发明人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

IPC分类号： A61K3141

CPC分类号： C07D207/335 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

摘要： This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐，其中A是部分不饱和或不饱和的五元杂环或部分不饱和或不饱和的五元碳环，其中4-（磺酰基）苯基和4-取代的苯基 在式（I）中，与环A相邻的环原子相连; R1是任选取代的芳基或杂芳基，条件是当A是吡唑时，R 1是杂芳基; R2是C1-4烷基，卤素取代的C1-4烷基，C1-4烷基氨基，C1-4二烷基氨基或氨基; R 3，R 4和R 5独立地为氢，卤素，C 1-4烷基，卤素取代的C 1-4烷基等; 或者R 3，R 4和R 5中的两个与它们所连接的原子一起形成4-7元环; R 6和R 7独立地是氢，卤素，C 1-4烷基，卤素取代的C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-4烷基氨基或N，N-二C 1-4烷基氨基; 并且m和n独立地为1,2,3或4.本发明还提供了可用于治疗前列腺素作为病原体的医学病症的药物组合物。