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1. 发明授权

US06407116B1 Nitrogenous fused-ring compounds, process for the preparation of the same, and drugs 失效
标题翻译：含氮稠环化合物，其制备方法和药物
公开(公告)号：US06407116B1
公开(公告)日：2002-06-18
申请号：US09486646
申请日：2000-02-25
申请人： Masahiro Kajino , Shinji Morimoto , Atsuhiro Inaba , Hideaki Nagaya
发明人： Masahiro Kajino , Shinji Morimoto , Atsuhiro Inaba , Hideaki Nagaya
IPC分类号： C07D23996
CPC分类号： C07D401/06 , C07D239/96 , C07D401/14 , C07D471/04 , C07D475/02 , C07D495/04
摘要： A compound represented by the formula: [wherein ring A represents a homocycle optionally having substituents or a nitrogen-containing heterocycle optionally having substituents; D and E are O or S; one of R1 and R2 represents a group represented by the formula: (wherein Ar1 and Ar2 represent an aromatic group optionally having substituents; Ar1 and Ar2 may form a condensed cyclic group optionally having substituents together with an adjacent carbon atom; ring B represents a nitrogen-containing heterocycle optionally having substituents; X and Y are a bond, O, S(O)p (p is an integer of 0 to 2), NR4 (R4 is H or a lower alkyl group) or a bivalent straight-chained lower hydrocarbon group, which may contain 1 to 3 hetero atoms, optionally having substituents; and R3 represents H, a hydroxy group optionally having substituents or an optionally esterified carboxyl group); and the other is a hydrogen atom, a cyano group or a hydrocarbon group optionally having substituents], or a salt thereof, has an anti-histaminic action, an anti-inflammatory action, eosinophil chemotaxis-inhibiting action, and is useful for preventing or treating asthma, allergic conjunctivitis, allergic rhinitis, urticaria, atopic dermatitis and so on.
摘要翻译：由下式表示的化合物：其中环A表示任选具有取代基的均质环或任选具有取代基的含氮杂环; D和E为O或S; R1和R2中的一个表示由下式表示的基团：其中Ar1和Ar2表示任选具有取代基的芳族基团; Ar1和Ar2可以与相邻碳原子一起形成任选具有取代基的稠合环状基团;环B表示氮任选具有取代基的杂环; X和Y是键，O，S（O）p（p是0-2的整数），NR4（R4是H或低级烷基）或二价直链低级可以含有1〜3个杂原子的烃基，任选具有取代基; R 3表示H，任选具有取代基的羟基或任选被酯化的羧基）; 另一个是氢原子，氰基或任选具有取代基的烃基]或其盐具有抗组胺作用，抗炎作用，嗜酸性粒细胞趋化性抑制作用，并且可用于预防或治疗哮喘，过敏性结膜炎，过敏性鼻炎，荨麻疹，特应性皮炎等。

2. 发明授权

US06506744B1 Benzazepinone-derivatives 失效
标题翻译：苯并氮杂酮衍生物
公开(公告)号：US06506744B1
公开(公告)日：2003-01-14
申请号：US09611700
申请日：2000-07-07
申请人： Leo Alig , Alexander Chucholowski , Thomas Weller
发明人： Leo Alig , Alexander Chucholowski , Thomas Weller
IPC分类号： C07D23996
CPC分类号： C07D413/12 , C07D239/96 , C07D243/14 , C07D267/14
摘要： Compounds of formula I as well as pharmaceutically usable salts and esters thereof, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations for the treatment or prevention of neoplasms, tumor metastasis, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure as well as infection caused by viruses, bacteria or fungi.
摘要翻译：式I的化合物以及其药学上可用的盐和酯抑制粘合蛋白与不同类型细胞表面的结合，并因此影响细胞和细胞与细胞 - 基质相互作用。它们可以以药物制剂的形式用于治疗或预防肿瘤，肿瘤转移，肿瘤生长，骨质疏松症，佩吉特氏病，糖尿病性视网膜病变，黄斑变性，血管干预后的再狭窄，牛皮癣，关节炎，纤维化，肾衰竭以及作为病毒，细菌或真菌引起的感染。

3. 发明授权

US06825199B2 7-Substituted quinazolin-2,4-diones useful as antibacterial agents 失效
标题翻译： 7-取代喹唑啉-2,4-二酮可用作抗菌剂
公开(公告)号：US06825199B2
公开(公告)日：2004-11-30
申请号：US09971343
申请日：2001-10-04
申请人： John Michael Domagala , Edmund Lee Ellsworth , Liren Huang , Thomas Eric Renau , Rajeshwar Singh , Michael Andrew Stier
发明人： John Michael Domagala , Edmund Lee Ellsworth , Liren Huang , Thomas Eric Renau , Rajeshwar Singh , Michael Andrew Stier
IPC分类号： C07D23996
CPC分类号： C07D403/04 , C07D239/96 , C07D471/04 , C07D471/06
摘要： The invention is a series of 7-substituted quinazolin-2,4-diones useful as antibacterial agents, processes for the preparation of the compounds, and a pharmaceutical composition containing one or more of the compounds.
摘要翻译：本发明是用作抗菌剂的一系列7-取代喹唑啉-2,4-二酮，用于制备化合物的方法和含有一种或多种化合物的药物组合物。

4. 发明授权

US06344559B1 Process for producing quinazoline derivatives 失效
标题翻译：喹唑啉衍生物的制备方法
公开(公告)号：US06344559B1
公开(公告)日：2002-02-05
申请号：US09380609
申请日：1999-10-13
申请人： Hiroki Omori , Shunsuke Goto , Hiroyuki Tsuboi , Masayasu Fukagawa , Kooji Kagara
发明人： Hiroki Omori , Shunsuke Goto , Hiroyuki Tsuboi , Masayasu Fukagawa , Kooji Kagara
IPC分类号： C07D23996
CPC分类号： C07D239/96
摘要： This invention provides an industrially useful process for producing a quinazoline derivative (I) of the general formula: [wherein R1 is hydrogen or halogen; R2 is carboxy or protected carboxy; A is lower alkylene] or its salt on a commercial scale which comprises reacting a compound of the general formula: [wherein R1 is hydrogen or halogen] or its salt with a silylating agent and then with a compound of the general formula: Cl—A—R2 (III) [wherein R2 is carboxy or protected carboxy; A is lower alkylene] or its salt, optionally followed by desilylation.
摘要翻译：本发明提供了一种工业上有用的制备具有以下通式的喹唑啉衍生物（I）的方法：其中R 1是氢或卤素; R2是羧基或被保护的羧基; A是低级亚烷基]或其盐，其包括使通式为[其中R 1为氢或卤素]的化合物或其盐与甲硅烷基化试剂反应，然后与下列通式的化合物反应：其中R 2 是羧基或被保护的羧基; A是低级亚烷基]或其盐，任选地随后脱甲硅烷基化。

5. 发明授权

US06331538B1 7-substituted quinazolin-2,4-diones useful as antibacterial agents 失效
标题翻译：可用作抗菌剂的7-取代喹唑啉-2,4-二酮
公开(公告)号：US06331538B1
公开(公告)日：2001-12-18
申请号：US09508796
申请日：2000-03-15
申请人： John Michael Domagala , Edmund Lee Ellsworth , Liren Huang , Thomas Eric Renau , Rajeshwar Singh , Michael Andrew Stier
发明人： John Michael Domagala , Edmund Lee Ellsworth , Liren Huang , Thomas Eric Renau , Rajeshwar Singh , Michael Andrew Stier
IPC分类号： C07D23996
CPC分类号： C07D403/04 , C07D239/96 , C07D471/04 , C07D471/06
摘要： The invention is a series of 7-substituted quinazolin-2,4-diones useful as antibacterial agents, processes for the preparation of the compounds, and a pharmaceutical composition containing one or more of the compounds.
摘要翻译：本发明是用作抗菌剂的一系列7-取代喹唑啉-2,4-二酮，用于制备化合物的方法和含有一种或多种化合物的药物组合物。

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