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    Optically active azole compounds and their production
    3.
    发明授权
    Optically active azole compounds and their production 失效
    光活性唑化合物及其生产

    公开(公告)号：US5495024A

    公开(公告)日：1996-02-27

    申请号：US302411

    申请日：1994-09-08

    申请人： Katsumi Itoh ,  Kenji Okonogi ,  Norikazu Tamura

    发明人： Katsumi Itoh ,  Kenji Okonogi ,  Norikazu Tamura

    IPC分类号： C07D249/08 ,  C07D521/00 ,  C07D405/06

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： An optically active azole compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom, a halogen atom, a haloalkyl group, a haloalkoxy group or an optionally substituted nitrogen-containing heterocyclic group; R.sup.3 is a hydrogen atom or an acyl group; Q is CH or N; ##STR2## is a nitrogen-containing aromatic five-membered heterocyclic group having at least two adjacent nitrogen atoms as the ring-constituting atoms which may be substituted, or an aromatic condensed heterocyclic group having two or more nitrogen atoms as the ring-constituting atoms which may be substituted; and (R) shows that the carbon atom marked with (R) has R-configuration; provided that either of R.sup.1 and R.sup.2 is an optionally substituted nitrogen-containing heterocyclic group when ##STR3## is an 1H-1,2,4-triazol-1-yl group, or a salt thereof, which is useful as an antifungal agent.

    摘要翻译： 式（I）的光学活性唑化合物：其中R 1和R 2独立地为氢原子，卤素原子，卤代烷基，卤代烷氧基或任选取代的含氮杂环基; R3是氢原子或酰基; Q是CH或N; 具有至少两个相邻氮原子的含氮芳香族五元杂环基作为可被取代的构成环的原子，或具有2个以上氮原子的芳香族稠合杂环基作为构成环的原子 可以替代; 和（R）表示具有（R）标记的碳原子具有R-构型; 条件是当＆lt; IMAGE＆gt;是可用作抗真菌剂的1H-1,2,4-三唑-1-基或其盐时，R 1和R 2中的任一个为任选取代的含氮杂环基。

    Azole compounds, their production and use
    4.
    发明授权
    Azole compounds, their production and use 失效
    唑类化合物，其生产和使用

    公开(公告)号：US06034248A

    公开(公告)日：2000-03-07

    申请号：US624649

    申请日：1996-10-17

    申请人： Katsumi Itoh ,  Kenji Okonogi ,  Akihiro Tasaka

    发明人： Katsumi Itoh ,  Kenji Okonogi ,  Akihiro Tasaka

    IPC分类号： C07D403/06 ,  A01N43/653 ,  C07D521/00 ,  C07D403/14

    CPC分类号： C07D231/12 ,  A01N43/653 ,  C07D233/56 ,  C07D249/08

    摘要： The present invention provides an azole compound represented by the formula (I): ##STR1## wherein Ar is an optionally substituted phenyl group; R.sup.1 and R.sup.2, the same or different, are a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 may combine together to form a lower alkylene group; R.sup.3 is a hydrogen atom or an acyl group; X is a nitrogen atom or a methine group; A is Y.dbd.Z (Y and Z, the same or different, are a nitrogen atom or a methine group optionally substituted with a lower alkyl group) or an ethylene group optionally substituted with a lower alkyl group; n is an integer from 0 to 2; and Az is an optionally substituted azolyl group, or its salt, which is useful for a prevention and therapy of a fungal infection of a mammal as a antifungal agent.

    摘要翻译： PCT No.PCT / JP96 / 00325 Sec。 371日期1996年10月17日第 102（e）日期1996年10月17日PCT 1996年2月15日PCT PCT。 公开号WO96 / 25410 PCT 日期：1980年8月20日本发明提供由式（I）表示的唑化合物：其中Ar为任选取代的苯基; R1和R2相同或不同，为氢原子或低级烷基，或者R1和R2可以结合在一起形成低级亚烷基; R3是氢原子或酰基; X是氮原子或次甲基; A是Y = Z（Y和Z相同或不同，是任选被低级烷基取代的氮原子或次甲基）或任选被低级烷基取代的亚乙基; n为0〜2的整数; 并且Az是任选取代的唑基或其盐，其可用于预防和治疗作为抗真菌剂的哺乳动物的真菌感染。

    Azole compounds, their production and their use
    7.
    发明授权
    Azole compounds, their production and their use 失效
    唑类化合物，其生产及其用途

    公开(公告)号：US06407129B1

    公开(公告)日：2002-06-18

    申请号：US09381479

    申请日：1999-09-20

    申请人： Katsumi Itoh ,  Tomoyuki Kitazaki ,  Kenji Okonogi

    发明人： Katsumi Itoh ,  Tomoyuki Kitazaki ,  Kenji Okonogi

    IPC分类号： A61K3141

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： A quaternized nitrogen-containing imidazol-1-yl or 1,2,4-triazol-1-yl compound wherein one of the nitrogen atoms constituting an azole ring is quaternized with a substituent capable of being eliminated in vivo and the substituent can be eliminated in vivo to be converted into an antifungal azole compound, has an improved solubility in water, can advantageously be applied to injection, has an improved internal absorption and can be expected to have a good effect for the treatment or prevention of disease.

    摘要翻译： 构成唑环的氮原子之一的季铵化的含氮咪唑-1-基或1,2,4-三唑-1-基化合物被能够在体内消除的取代基季铵化，并且可以消除取代基 在体内被转化为抗真菌唑化合物，在水中的溶解度提高，可有利地应用于注射，具有改善的内部吸收，并且可以预期对于治疗或预防疾病具有良好的效果。

    Azole compounds, their production and use
    8.
    发明授权
    Azole compounds, their production and use 失效
    唑类化合物，其生产和使用

    公开(公告)号：US06362206B1

    公开(公告)日：2002-03-26

    申请号：US09413876

    申请日：1999-10-07

    申请人： Katsumi Itoh ,  Kenji Okonogi ,  Akihiro Tasaka

    发明人： Katsumi Itoh ,  Kenji Okonogi ,  Akihiro Tasaka

    IPC分类号： A61K314192

    CPC分类号： C07D231/12 ,  A01N43/653 ,  C07D233/56 ,  C07D249/08

    摘要： The present invention provides an azole compound represented by the formula (I): wherein Ar is an optionally substituted phenyl group; R1 and R2, the same or different, are a hydrogen atom or a lower alkyl group, or R1 and R2 may combine together to form a lower alkylene group; R is a hydrogen atom or an acyl group; X is a nitrogen atom or a methine group; A is Y═Z (Y and Z, the same or different, are a nitrogen atom or a methine group optionally substituted with a lower alkyl group) or an ethylene group optionally substituted with a lower alkyl group; n is an integer from 0 to 2; and Az is an optionally substituted azolyl group, or its salt, which is useful for a prevention and therapy of a fungal infection of a mammal as a antifungal agent.

    摘要翻译： 本发明提供由式（I）表示的唑化合物：其中Ar为任选取代的苯基; R1和R2相同或不同，为氢原子或低级烷基，或者R1和R2可以结合在一起形成低级亚烷基; R是氢原子或酰基; X是氮原子或次甲基; A是Y = Z（Y和Z相同或不同，是任选被低级烷基取代的氮原子或次甲基）或任选被低级烷基取代的亚乙基; n为0〜2的整数; 并且Az是任选取代的唑基或其盐，其可用于预防和治疗作为抗真菌剂的哺乳动物的真菌感染。

    Azole compounds, their production and use
    9.
    发明授权
    Azole compounds, their production and use 失效
    唑类化合物，其生产和使用

    公开(公告)号：US5792780A

    公开(公告)日：1998-08-11

    申请号：US640717

    申请日：1996-05-01

    申请人： Katsumi Itoh ,  Kenji Okonogi ,  Akihiro Tasaka

    发明人： Katsumi Itoh ,  Kenji Okonogi ,  Akihiro Tasaka

    IPC分类号： C07D233/58 ,  A61K31/4196 ,  A61P31/10 ,  C07D249/08 ,  C07D521/00 ,  A61K31/41 ,  A61K31/415

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The present invention provides an azole compound represented by the formula (I): ##STR1## , wherein Ar is an optionally-substituted phenyl group; R.sup.1 and R.sup.2 are, the same or different, a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 may combine together to form a lower alkylene group; R.sup.3 is a hydrogen atom or an acyl group; Y is a nitrogen atom or a methine group; and A is an optionally-substituted saturated cyclic amide group bonded through a first nitrogen atom, or a salt thereof, which is useful for prevention and therapy of fungal infections of mammals as antifungal agent.

    摘要翻译： 本发明提供由式（I）表示的唑类化合物：其中Ar为任选取代的苯基; R 1和R 2可以相同或不同，为氢原子或低级烷基，或者R 1和R 2可以结合在一起形成低级亚烷基; R3是氢原子或酰基; Y是氮原子或次甲基; A是通过第一氮原子或其盐键合的任选取代的饱和环酰胺基，其可用于预防和治疗作为抗真菌剂的哺乳动物的真菌感染。

    Triazole and imidazole compounds and their use as antifungal therapeutic agents
    10.
    发明授权
    Triazole and imidazole compounds and their use as antifungal therapeutic agents 失效
    三唑和咪唑化合物及其作为抗真菌剂的用途

    公开(公告)号：US5545652A

    公开(公告)日：1996-08-13

    申请号：US310995

    申请日：1994-09-23

    申请人： Katsumi Itoh ,  Kenji Okonogi ,  Akihiro Tasaka

    发明人： Katsumi Itoh ,  Kenji Okonogi ,  Akihiro Tasaka

    IPC分类号： C07D233/58 ,  A61K31/4196 ,  A61P31/10 ,  C07D249/08 ,  C07D521/00 ,  A61K31/41 ,  A61K31/415 ,  C07D403/10

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The present invention provides an azole compound represented by the formula (I): ##STR1## wherein Ar is an optionally-substituted phenyl group; R.sup.1 and R.sup.2 are, the same or different, a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 may combine together to form a lower alkylene group; R.sup.3 is a hydrogen atom or an acyl group; Y is a nitrogen atom or a methine group; and A is an optionally-substituted saturated cyclic amide group bonded through a first nitrogen atom, or a salt thereof, which is useful for prevention and therapy of fungal infections of mammals as antifungal agent.

    摘要翻译： 本发明提供由式（I）表示的唑化合物：其中Ar是任选取代的苯基; R 1和R 2可以相同或不同，为氢原子或低级烷基，或者R 1和R 2可以结合在一起形成低级亚烷基; R3是氢原子或酰基; Y是氮原子或次甲基; A是通过第一氮原子或其盐键合的任选取代的饱和环酰胺基，其可用于预防和治疗作为抗真菌剂的哺乳动物的真菌感染。