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119 条记录 (耗时 0.047 秒)

    Aminomethylpyrrolidine derivatives having aromatic substituents
    21.
    发明授权
    Aminomethylpyrrolidine derivatives having aromatic substituents 失效

    公开(公告)号：US07186843B2

    公开(公告)日：2007-03-06

    申请号：US10834079

    申请日：2004-04-29

    申请人： Makoto Takemura ,  Hisashi Takahashi ,  Katsuhiro Kawakami ,  Toshiyuki Takeda ,  Rie Miyauchi

    发明人： Makoto Takemura ,  Hisashi Takahashi ,  Katsuhiro Kawakami ,  Toshiyuki Takeda ,  Rie Miyauchi

    IPC分类号： C07D207/09 ,  C07D401/12 ,  C07D403/12

    CPC分类号： C07D401/04 ,  C07D405/14

    摘要： This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both. In the formula, R2, R3: hydrogen atom, an alkyl group; R4, R5, R6: hydrogen atom, hydroxyl group, a halogen atom, carbamoyl group, an alkyl group, an alkoxyl group, an alkylthio group; R7, R8: hydrogen atom, an alkyl group; R9: an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, an aryl group, a heteroaryl group, an alkoxyl group having from 1 to 6 carbon atoms, an alkylamino group; R10:hydrogen atom, an alkylthio group; R11: hydrogen atom, amino group, hydroxyl group, thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; X1: halogen atom, a hydrogen atom; A1: nitrogen atom, C—X2; X2: hydrogen atom, amino group, a halogen atom, cyano group, an halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; A2, A3:>C═C (—A1═)—N(—R9)—, >N—C (—A1>)═C(—R9)—; R10 and R9 or R9 and X2 may be integrated to form a ring structure; and Y: hydrogen atom, ester forming group.

    Aminomethylpyrrolidine derivatives having aromatic substituents
    23.
    发明授权
    Aminomethylpyrrolidine derivatives having aromatic substituents 失效
    具有芳香取代基的氨基甲基吡咯烷衍生物

    公开(公告)号：US06762181B1

    公开(公告)日：2004-07-13

    申请号：US09936050

    申请日：2001-09-07

    申请人： Makoto Takemura ,  Hisashi Takahashi ,  Katsuhiro Kawakami ,  Toshiyuki Takeda ,  Rie Miyauchi

    发明人： Makoto Takemura ,  Hisashi Takahashi ,  Katsuhiro Kawakami ,  Toshiyuki Takeda ,  Rie Miyauchi

    IPC分类号： A61K314375

    CPC分类号： C07D401/04 ,  C07D405/14

    摘要： This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both. In the formula, R2, R3: hydrogen atom, an alkyl group; R4, R5, R6: hydrogen atoms, hydroxyl group, a halogen atom, carbamoyl group, an alkyl group, an alkoxyl group, an alkylthio group; R7, R8: hydrogen atom, an alkyl group; R9: an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, an aryl group, a heteroaryl group, an alkoxyl group having from 1 to 6 carbon atoms, an alkylamino group; R10: hydrogen atom, an alkylthio group; R11: hydrogen atom, amino group, hydroxyl group, thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; X1: halogen atom, a hydrogen atom; A1: nitrogen atom, C—X2; X2: hydrogen atom, amino group, a halogen atom, cyano group, an halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; A2, A3: >C═C(—A1═)—N(—R9)—, >N—C(—A1═)═C(—R9)—; R10 and R9 or R9 and X2 may be integrated to form a ring structure; and Y: hydrogen atom, ester forming group.

    摘要翻译： 本发明提供了一种喹诺酮衍生物，其具有对各种细菌的抗菌活性，包括耐药菌株，其为下式的化合物，其中R 1为任选取代的芳族基团，其两者的盐或两者的水合物。 式R 2，R 3：氢原子，烷基; R 4，R 5，R 6：氢原子，羟基，卤素原子，氨基甲酰基，烷基，烷氧基，烷硫基; R 7，R 8：氢原子，烷基; R 9：烷基，烯基，卤代烷基，环状烷基，芳基，杂芳基，碳原子数1〜6的烷氧基，烷基氨基， R 10：氢原子，烷硫基; R 11：氢原子，氨基，羟基，硫醇基，卤代甲基，烷基，烯基，炔基，烷氧基; X 1：卤素原子，氢原子; A 1：氮原子，C-X 2; X 2：氢原子，氨基，卤原子，氰基，卤代甲基，卤代甲氧基，烷基，烯基，炔基，烷氧基; A 2，A 3：C = C（-A 1 =）-N（-R 9） - ，> NC（-A 1）= C（-R 9） >） - ; R 10和R 9或R 9和X 2可以一体形成环结构; 和Y：氢原子，酯形成基团。

    8-Cyanoquinolonecarboxylic Acid Derivative
    24.
    发明申请
    8-Cyanoquinolonecarboxylic Acid Derivative 有权
    8-氰基喹诺酮羧酸衍生物

    公开(公告)号：US20080255190A1

    公开(公告)日：2008-10-16

    申请号：US10572742

    申请日：2004-09-29

    申请人： Hisashi Takahashi ,  Rie Miyauchi ,  Makoto Takemura

    发明人： Hisashi Takahashi ,  Rie Miyauchi ,  Makoto Takemura

    IPC分类号： A61K31/47 ,  C07D215/00 ,  A61P31/04

    CPC分类号： C07D215/233 ,  A61K31/4709 ,  Y02A50/475

    摘要： To provide a quinolone antibacterial drug and a therapeutic agent for infectious diseases, which exhibit potent antibacterial activity on Gram-positive and Gram-negative bacteria and which is highly safe.A compound represented by the following formula (1): (wherein R1 represents a C3-C6 cycloalkyl group which may have a substituent or the like; R2 represents a hydrogen atom or the like; R3 and R4 each independently represent a hydrogen atom or a C1-C6 alkyl group, or a substituted carboxyl group derived from an amino acid, a dipeptide, or a tripeptide, and, in the case where each of R3 and R4 represents a C1-C6 alkyl group, the alkyl group may be substituted by one or more atoms or groups selected from among a hydroxyl group, a halogen atom, a C1-C6 alkylthio group, and a C1-C6 alkoxy group; and n denotes an integer of 1 to 3), a salt thereof, and a hydrate of the compound or the salt. Also, antibacterial drugs and therapeutic agents for infectious diseases are prepared.

    摘要翻译： 提供喹诺酮抗菌药物和用于感染性疾病的治疗剂，其对革兰氏阳性和革兰氏阴性细菌具有强力的抗菌活性，并且是高度安全的。 由下式（1）表示的化合物：其中R 1表示可以具有取代基的C 3 -C 6环烷基等; R 2表示氢 原子等; R 3和R 4各自独立地表示氢原子或C 1 -C 6烷基或衍生自氨基酸的取代羧基， 二肽或三肽，并且在R 3和R 4各自表示C 1 -C 6烷基的情况下，该烷基可以被一个或多个 更多选自羟基，卤素原子，C1-C6烷硫基和C1-C6烷氧基的原子或基团，n表示1〜3的整数），其盐，和 化合物或盐。 此外，还制备了用于感染性疾病的抗菌药物和治疗剂。

    Substituted cyclobutylamine derivatives
    27.
    发明授权
    Substituted cyclobutylamine derivatives 失效
    取代的环丁胺衍生物

    公开(公告)号：US06448266B1

    公开(公告)日：2002-09-10

    申请号：US09424780

    申请日：1999-11-30

    申请人： Makoto Takemura ,  Hisashi Takahashi ,  Kazuyuki Sugita ,  Rie Miyauchi

    发明人： Makoto Takemura ,  Hisashi Takahashi ,  Kazuyuki Sugita ,  Rie Miyauchi

    IPC分类号： A61K3147

    CPC分类号： C07D401/04

    摘要： Substituted cyclobutylamine derivativesb with a novel structure represented by the following formula (I), wherein R1 to R4 and Q each represents a specific substituent and, in particular, Q represents a quinolone derivative having a specific structure. These derivatives are useful as antibacterial compounds which have excellent antibacterial activity against a wide scope of bacteria including Gram-negative and Gram-positive bacteria, exert potent antibacterial activity particularly against methicillin-resistant Staphylococcus aureus (MRSA) strains, penicillin-resistant pneumococcus strains and quinolone-resistant bacteria, and are also possessed of both excellent pharmacokinetics and high safety.

    摘要翻译： 具有由下式（I）表示的新结构的取代的环丁基胺衍生物b，其中R 1至R 4和Q各自表示特定取代基，特别是Q表示具有特定结构的喹诺酮衍生物。 这些衍生物可用作对广泛范围的细菌（包括革兰氏阴性和革兰氏阳性细菌）具有优异的抗菌活性的抗菌化合物，特别是耐甲氧西林金黄色葡萄球菌（MRSA）菌株，青霉素耐药性肺炎球菌菌株和 喹诺酮抗性细菌，也具有优异的药代动力学和高安全性。