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13 条记录 (耗时 0.032 秒)

    Optically active azole compounds and their production
    1.
    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。

    Optically active tetrazole compounds, and fungicidal compositions thereof
    3.
    发明授权
    Optically active tetrazole compounds, and fungicidal compositions thereof 失效
    光活性四唑化合物及其杀真菌组合物

    公开(公告)号：US5371100A

    公开(公告)日：1994-12-06

    申请号：US981850

    申请日：1992-11-24

    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 ,  A01N43/713 ,  C07D403/06

    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; --NA 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 --NA 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; -NA是具有至少两个相邻氮原子的含氮芳族五元杂环基，作为可被取代的构成环的原子，或具有两个以上氮原子的芳香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-NA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。

    2-piperazinone-1-acetic acid derivatives and their use
    5.
    发明授权
    2-piperazinone-1-acetic acid derivatives and their use 失效
    2-哌嗪酮-1-乙酸衍生物及其用途

    公开(公告)号：US06242600B1

    公开(公告)日：2001-06-05

    申请号：US09355499

    申请日：1999-07-28

    申请人： Norikazu Tamura ,  Zen-ichi Terashita

    发明人： Norikazu Tamura ,  Zen-ichi Terashita

    IPC分类号： C07D41314

    CPC分类号： C07D401/12 ,  C07D401/14

    摘要： The present invention provides compounds and medicines effective for prophylaxis and therapy of various diseases by controlling or inhibiting cell-adhesion. Especially, the compounds of this invention inhibit platelet aggregation action without remarkable elongation of hemorrhagic period and can be used as a safe and long-acting antithrombotic drug as compared with known substances showing the same activity. Compounds of this invention are piperazinones of the formula: wherein the ring A is a basic heterocyclic group; the ring B is a nitrogen containing heterocyclic group or a cyclic hydrocarbon group; Y is CH2; R1 is H, OH, NH2 or an hydrocarbon group which may be bound through CO, S, SO or SO2; R2 is H or a hydrocarbon group; R3 is an optionally esterified or amidated carboxyl group; and D is a lower alkyl group substituted with an optionally esterified carboxyl group; or a salt thereof.

    摘要翻译： 本发明提供通过控制或抑制细胞粘附而有效预防和治疗各种疾病的化合物和药物。 特别是本发明的化合物抑制血小板聚集作用而没有显着的出血期延长，与已知的具有相同活性的物质相比，可以作为安全且长效的抗血栓形成药物使用。本发明的化合物是下式的哌嗪酮： 其中环A是碱性杂环基; 环B是含氮杂环基或环状烃基; Y是CH2; R1是H，OH，NH2或可以通过CO，S，SO或SO 2结合的烃基; R2是H或烃基; R3是任选酯化或酰胺化的羧基; D是被任意酯化的羧基取代的低级烷基; 或其盐。

    Pharmaceutical composition
    8.
    发明授权
    Pharmaceutical composition 失效
    药物组成

    公开(公告)号：US06432996B1

    公开(公告)日：2002-08-13

    申请号：US09551546

    申请日：2000-04-18

    申请人： Norikazu Tamura ,  Takashi Sohda ,  Hitoshi Ikeda

    发明人： Norikazu Tamura ,  Takashi Sohda ,  Hitoshi Ikeda

    IPC分类号： A01N4378

    CPC分类号： A61K45/06 ,  A61K31/222 ,  A61K31/4184 ,  A61K31/425 ,  A61K31/44 ,  A61K31/415 ,  A61K2300/00

    摘要： To provide a pharmaceutical composition which performs a remarkable effect with a relatively decreased dosage, and, with less side effects, a pharmaceutical composition formulated by combination of an angiotensin II-mediated compound or a salt thereof with at least one species of a compound having the activity of increasing insulin-sensitivity, a compound having the activity of improving postprandial hyperglycemia in diabetes mellitus, an indane derivative having the activity of inhibiting angiotensin converting enzyme, a pyridine derivative having the activity of inhibiting HMG-Co A reductase or salts thereof are advantageously employed.

    摘要翻译： 本发明提供一种药物组合物，其以相对减少的剂量进行显着效果，并且具有较少的副作用，通过将血管紧张素II介导的化合物或其盐与至少一种具有 增加胰岛素敏感性的活性，具有改善糖尿病餐后高血糖活性的化合物，具有抑制血管紧张素转换酶活性的二氢吲哚衍生物，具有抑制HMG-CoA还原酶活性的吡啶衍生物或其盐有利地 雇用。

    Carbapenems, their production and use
    9.
    发明授权
    Carbapenems, their production and use 失效
    碳水化合物，其生产和使用

    公开(公告)号：US4698339A

    公开(公告)日：1987-10-06

    申请号：US655454

    申请日：1984-09-28

    申请人： Koichi Yoshioka ,  Norikazu Tamura ,  Hideaki Natsugari

    发明人： Koichi Yoshioka ,  Norikazu Tamura ,  Hideaki Natsugari

    IPC分类号： C07D205/08 ,  C07D409/04 ,  C07D477/20 ,  C07D498/04 ,  C07F7/10 ,  C07D487/04 ,  A61K31/40

    CPC分类号： C07D409/04 ,  C07D205/08 ,  C07D477/20 ,  C07F7/10

    摘要： A compound of the general formula: ##STR1## wherein X is a lower alkylene group which may optionally be substituted by a hydroxyl group, or a lower alkenylene group, Y is (1) a lower alkyl group, (2) a cycloalkyl group containing 3 to 8 carbon atoms, (3) a lower alkenyl group, (4) an aryl group, (5) an aralkyl group or (6) a 3- to 8-membered heterocyclic group, or the partial structural formula Y--SO.sub.2 --X--, with X and Y being combined with each other, represents a group of the formula: ##STR2## wherein l is an integer of 0 to 3, and m and n each is an integer of 0 to 6, provided that the sum of m and n is in the range of 2 to 6, and R is a hydrocarbon group which may optionally be substituted or a 3- to 8-membered heterocyclic group, or a pharmaceutically acceptable salt thereof a method of production thereof and use thereof. The compound (I) has antimicrobial and .beta.-lactamase inhibitory activities.

    摘要翻译： 下式的化合物：其中X是可以被羟基或低级亚烯基取代的低级亚烷基，Y是（1）低级烷基，（2）a 含有3〜8个碳原子的环烷基，（3）低级烯基，（4）芳基，（5）芳烷基或（6）3-8元杂环基，或部分结构式Y -SO 2 -X-，其中X和Y彼此结合，表示下式的基团：其中l为0〜3的整数，m和n各自为0〜 6，条件是m和n的总和在2至6的范围内，并且R是可任选取代的烃基或3至8元杂环基，或其药学上可接受的盐，其方法为 其生产和使用。 化合物（I）具有抗微生物和β-内酰胺酶抑制活性。

    Substituted aromatic-ring compounds, process for producing the same, and use
    10.
    发明授权
    Substituted aromatic-ring compounds, process for producing the same, and use 失效

    公开(公告)号：US07078540B1

    公开(公告)日：2006-07-18

    申请号：US10048938

    申请日：2000-08-03

    申请人： Norikazu Tamura ,  Takashi Ichikawa ,  Masayuki Ii

    发明人： Norikazu Tamura ,  Takashi Ichikawa ,  Masayuki Ii

    IPC分类号： C07D315/00 ,  C07D321/00

    CPC分类号： C07C317/44 ,  C07C2601/10

    摘要： A compound of the formula: wherein R1 is an aliphatic hydrocarbon group optionally having substituent(s), an aromatic hydrocarbon group optionally having substituent(s), a heterocyclic group optionally having substituent(s), a group of the formula: OR1a wherein R1a is a hydrogen atom or an aliphatic hydrocarbon group optionally having substituent(s), or a group of the formula: wherein R1b and R1c are the same or different and each is a hydrogen atom or an aliphatic hydrocarbon group optionally having substituent(s), X is a methylene group, a nitrogen atom, a sulfur atom or an oxygen atom, Y is an optionally substituted methylene group or an optionally substituted nitrogen atom, ring A is a 5 to 8-membered ring optionally substituted further by 1 to 4 substituent(s) selected from (1) an aliphatic hydrocarbon group optionally having substituent(s), (2) an aromatic hydrocarbon group optionally having substituent(s), (3) a group of the formula: OR2 wherein R2 is a hydrogen atom, or an aliphatic hydrocarbon group optionally having substituent(s) and (4) a halogen atom, Ar is an aromatic hydrocarbon group optionally having substituent(s), a group of the formula: is a group of the formula: or the formula: m is an integer of 0 to 2, n is an integer of 1 to 3, and the sum of m and n is not more than 4, provided that when X is a methylene group, Y is an optionally substituted methylene group, and a salt thereof have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases, such as cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, septic shock and the like.