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    Aminomethylpyrrolidine derivatives having aromatic substituents
    1.
    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。

    Medicines for the prevention and treatment of neurodegenerative diseases
    2.
    发明授权
    Medicines for the prevention and treatment of neurodegenerative diseases 失效
    用于预防和治疗神经退行性疾病的药物

    公开(公告)号：US06743803B2

    公开(公告)日：2004-06-01

    申请号：US10311932

    申请日：2002-12-20

    申请人： Kiyoshi Furukawa ,  Satoshi Kurumiya ,  Kazuo Okimoto ,  Kazunori Ohno

    发明人： Kiyoshi Furukawa ,  Satoshi Kurumiya ,  Kazuo Okimoto ,  Kazunori Ohno

    IPC分类号： A61K314375

    CPC分类号： C07D471/04 ,  A61K31/4375 ,  A61K31/444

    摘要： Medicines for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease and schizophrenia of mammals (including human beings) through the retardation or inhibition of neurodegeneration due to hypofunction of glutamic acid receptor and which contain as an active ingredient 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivatives of the formula (I): wherein Het is oxadiazolyl; R1 is hydrogen, lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, etc.; and R2 is hydrogen, lower alkyl, cyclo-lower alkyl, substituted or unsubstituted aryl, etc., or physiologically acceptable acid addition salts thereof.

    摘要翻译： 通过延迟或抑制谷氨酸受体功能低下的神经退行性疾病，预防和治疗神经变性疾病如阿尔茨海默病和哺乳动物（包括人类）的精神分裂症的药物，其含有作为活性成分的5-取代-3-恶二唑基 （I）的-1,6-萘啶-2（1H） - 酮衍生物：其中Het是恶二唑基; R 1是氢，低级烷基，环低级烷基，低级烯基，低级烷氧基，取代或未取代的芳基，取代或未取代的杂芳基等。 R 2为氢，低级烷基，环低级烷基，取代或未取代的芳基等，或其生理上可接受的酸加成盐。

    Imidazonaphthyridines
    4.
    发明授权
    Imidazonaphthyridines 失效
    脲取代的咪唑并（1,5）萘啶

    公开(公告)号：US06638944B2

    公开(公告)日：2003-10-28

    申请号：US10184304

    申请日：2002-06-27

    申请人： John W. Mickelson

    发明人： John W. Mickelson

    IPC分类号： A61K314375

    CPC分类号： C07D471/04 ,  A61K31/4745 ,  A61K45/06 ,  C07D471/14 ,  A61K2300/00

    摘要： Imidazonaphthyridine compounds that have a urea containing substituent at the 1-position induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

    摘要翻译： 在1位具有含有取代基的脲的咪唑并吡啶化合物诱导细胞因子如干扰素和肿瘤坏死因子的生物合成。 该化合物显示抗病毒和抗肿瘤性质。 还公开了制备可用于制备化合物的化合物和中间体的方法。

    Treating sleep disorders using desloratadine
    8.
    发明授权
    Treating sleep disorders using desloratadine 失效
    使用地氯雷他定治疗睡眠障碍

    公开(公告)号：US06265414B1

    公开(公告)日：2001-07-24

    申请号：US09563553

    申请日：2000-05-03

    申请人： Alan G. Harris ,  Domenic G. Iezzoni

    发明人： Alan G. Harris ,  Domenic G. Iezzoni

    IPC分类号： A61K314375

    CPC分类号： A61K31/445 ,  A61K31/4545 ,  A61K45/06 ,  A61K2300/00

    摘要： Methods of treating and/or preventing sleep disorders in a human afflicted with upper airway passage allergic inflammation and/or congestion associated with allergic rhinitis, including seasonal allergic rhinitis or perennial allergic rhinitis, by administering a therapeutically effective amount of desloratadine, alone or in combination with other active such as a decongestant, e.g., pseudoephedrine are disclosed.

    摘要翻译： 通过施用治疗有效量的去氯雷他定来治疗和/或预防患有上呼吸道通路过敏性炎症和/或与过敏性鼻炎有关的充血的人的睡眠障碍的方法，包括季节性过敏性鼻炎或常年性变应性鼻炎，单独或组合 与其他活性物质如减充血剂，例如假麻黄碱被公开。

    Agent for improving learning or memory
    10.
    发明授权
    Agent for improving learning or memory 失效
    改善学习或记忆的代理

    公开(公告)号：US06803366B2

    公开(公告)日：2004-10-12

    申请号：US10148489

    申请日：2002-05-30

    申请人： Kuniaki Kawamura ,  Hiroshi Nagase ,  Noriyuki Hirano ,  Junzo Kamei

    发明人： Kuniaki Kawamura ,  Hiroshi Nagase ,  Noriyuki Hirano ,  Junzo Kamei

    IPC分类号： A61K314375

    CPC分类号： C07D471/04 ,  A61K31/4738 ,  A61K31/4745 ,  A61K31/498

    摘要： Disclosed is an agent for improving learning and/or memory, which is useful for therapy of dementia accompanying disorder of memory due to a cerebrovascular disease, neurodegenerative disease such as Alzheimer's disease, endocrine disease, nutritional or metabolic disorder, infectious disease, drug addiction or the like. The agent for improving learning and/or memory according to the present invention comprises as an effective ingredient an isoquinoline derivative having a specific structure, such as (4aR, 12aR)-2-methyl-4a-(3-hydroxyphenyl)-1,2,3,4,4a,5,12,12a-octahydro-quinoline[2,3-g]isoquinoline or a pharmaceutically acceptable salt thereof.

    摘要翻译： 公开了一种用于改善学习和/或记忆的药剂，其用于治疗由于脑血管疾病，神经变性疾病如阿尔茨海默病，内分泌疾病，营养或代谢障碍，感染性疾病，药物成瘾引起的记忆障碍的痴呆症 类似。 根据本发明的用于改善学习和/或记忆的药剂包括作为有效成分的具有特定结构的异喹啉衍生物，例如（4aR，12aR）-2-甲基-4a-（3-羟基苯基）-1,2 ，3,4,4a，5,12,12a-八氢 - 喹啉[2,3-g]异喹啉或其药学上可接受的盐。