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1. 发明授权

US06686502B1 Compounds and methods for treatment of asthma, allergy and inflammatory disorders 失效
公开(公告)号：US06686502B1
公开(公告)日：2004-02-03
申请号：US10386226
申请日：2003-03-11
申请人： Xiong Cai , Timothy Lewis
发明人： Xiong Cai , Timothy Lewis
IPC分类号： C07C25904
CPC分类号： C07D295/096 , C07D295/084 , C07D295/088 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/15 , C07D307/52
摘要： The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted,4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.

2. 发明授权

US06235753B1 Inhibitors of the production of S-CD23 and the secretion of TNF 失效
标题翻译：产生S-CD23的抑制剂和TNF的分泌
公开(公告)号：US06235753B1
公开(公告)日：2001-05-22
申请号：US09180547
申请日：1999-01-21
申请人： Stuart Bailey , Andrew Faller , David Glynn Smith , Derek Richard Buckle
发明人： Stuart Bailey , Andrew Faller , David Glynn Smith , Derek Richard Buckle
IPC分类号： C07C25904
CPC分类号： C07D333/54 , C07C259/06 , C07D277/64 , C07D307/80 , C07D333/60
摘要： Inhibitors of the Production of s-CD23 and the secretion of TNF are provided.
摘要翻译：提供了s-CD23的产生抑制剂和TNF的分泌

3. 发明授权

US06552223B1 N-hydroxacylamino compounds, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译： N-羟酰基氨基化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US06552223B1
公开(公告)日：2003-04-22
申请号：US09763598
申请日：2001-02-26
申请人： Rebecca J Cartwright , Robert I Dowell
发明人： Rebecca J Cartwright , Robert I Dowell
IPC分类号： C07C25904
CPC分类号： C07C259/06
摘要： A compound of the formula (I): R1—CO—N(OH)—CR2R3—CR4R5—CONH—CR6R7—CONR8R9 (I) wherein: R1 is C1-6alkyl, aryl or arylC1-6alkyl; R2 is hydrogen, C1-6alkyl, C3-8cycloalkyl, aryl or arylC1-6alkyl; R3 is hydrogen, C1-6alkyl or arylC1-6alkyl; or R2 and R3, together with the carbon atom to which they are joined, form a C3-8cycloalkyl ring; R4 is benzyl, phenethyl, phenylpropyl, phenylbutyl or flurophenylbutyl; R5 is hydrogen, C1-6alkyl or arylC1-6alkyl; R6 is hydrogen, C1-6alkyl, C2-6alkenyl, C3-8cycloalkylC1-6alkyl, arylC1-6alkyl, heteroarylC1-6alkyl or the side-chain of a naturally occurring amino acid; R7 is hydrogen or C1-6alkyl; R8 is hydrogen, C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or heterocyclylC1-6alkyl; R9 is hydrogen or C1-6alkyl; or R8 and R9, together with the nitrogen atom to which they are joined, form a heterocyclic ring; wherein any group or ring in R1-R9 is optionally substituted; or a pharmaceutically-acceptable salt or in vivo hydrolysable precursor thereof.
摘要翻译：式（I）的化合物：其中：R 1是C 1-6烷基，芳基或芳基C 1-6烷基; R 2是氢，C 1-6烷基，C 3-8环烷基，芳基或芳基C 1-6烷基; R 3是氢，C 1-6烷基或芳基C 1 -6-烷基; 或R 2和R 3与它们连接的碳原子一起形成C 3-8环烷基环; R 4是苄基，苯乙基，苯基丙基，苯基丁基或氟代苯基丁基; R 5是氢，C 1-6烷基或芳基C 1-6烷基; R 6是氢 C 1-6烷基，C 2-6烯基，C 3-8环烷基C 1-6烷基，芳基C 1-6烷基，杂芳基C 1-6烷基或天然氨基酸的侧链; R 7是氢或C 1-6烷基; R 8是氢，C 1-6烷基， C 3-8环烷基，C 3-8环烯基，芳基C 1-6烷基，杂芳基C 1-6烷基或杂环基C 1-6烷基; R 9是氢或C 1-6烷基;或者R 8和R 9与它们连接的氮原子一起形成杂环; R1-R9中的任何基团或环可任选被取代;或其药学上可接受的盐或体内可水解的前体。

4. 发明授权

US06329373B1 Metalloproteinase inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US06329373B1
公开(公告)日：2001-12-11
申请号：US09479588
申请日：2000-01-07
申请人： Fionna Mitchell Martin , Christopher Norman Lewis , Mark Whittaker
发明人： Fionna Mitchell Martin , Christopher Norman Lewis , Mark Whittaker
IPC分类号： C07C25904
CPC分类号： C07D213/75 , C07C237/22 , C07C259/06 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D211/34 , C07D277/46 , C07D333/24
摘要： A compound of formula (I) wherein X is a —CONHOH group and the R groups are defined in the claims. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation and inhibitors of the release of tumour necrosis factor from cells.
摘要翻译：式（I）的化合物，其中X是-CONHOH基团，R基团在权利要求中定义。这些化合物是参与组织降解的基质金属蛋白酶的抑制剂和从细胞释放肿瘤坏死因子的抑制剂。

5. 发明授权

US06673965B1 Hydroxamic acid derivative as inhibitor of the formation of soluble human CD23 失效
标题翻译：羟肟酸衍生物作为可溶性人CD23形成的抑制剂
公开(公告)号：US06673965B1
公开(公告)日：2004-01-06
申请号：US10111209
申请日：2002-07-16
申请人： John Gerard Ward , Andrew Faller
发明人： John Gerard Ward , Andrew Faller
IPC分类号： C07C25904
CPC分类号： C07C259/06 , A61K31/165 , C07C237/22
摘要： A compound of formula (I) wherein: R isopropyl; n is 0; R1 is naphthylmethyl; R2 is t-butyl; and R3 is methyl; is useful in the treatment of disorders mediated by s-CD23.
摘要翻译：式（I）的化合物，其中：R异丙基; n为0; R 1为萘基甲基; R 2为叔丁基; 和R 3是甲基;可用于治疗由s-CD23介导的病症。

6. 发明授权

US06605742B2 Cyclo azaphospha hydrocarbons 失效
标题翻译：环阿氮磷碳氢化合物
公开(公告)号：US06605742B2
公开(公告)日：2003-08-12
申请号：US10119769
申请日：2002-04-11
申请人： Thomas Høyer , Morten Dahl Sørensen
发明人： Thomas Høyer , Morten Dahl Sørensen
IPC分类号： C07C25904
CPC分类号： C07F9/6584
摘要： Novel cyclo azaphospha hydrocarbons according to formula I are provided. The compounds are useful as metalloprotease inhibitors.
摘要翻译：提供了根据式Iare的新型环氮杂磷杂环烃。该化合物可用作金属蛋白酶抑制剂。

7. 发明授权

US06500983B2 Hydroxamic acid derivatives 失效
标题翻译：羟肟酸衍生物
公开(公告)号：US06500983B2
公开(公告)日：2002-12-31
申请号：US09973255
申请日：2001-10-09
申请人： Georg Kottirsch , Ulf Neumann
发明人： Georg Kottirsch , Ulf Neumann
IPC分类号： C07C25904
CPC分类号： C07C259/06
摘要： Novel hydroxamic acid compounds, e.g., of formula I, wherein R1, R2, R3 and R4 are as defined, are found to be useful as pharmaceuticals, e.g., for the suppression of TNF release and the treatment of autoimmune and inflammatory diseases, e.g., multiple sclerosis and rheumatoid arthritis. Methods of making the compounds, novel intermediates, and pharmaceutical compositions comprising the compounds are provided.
摘要翻译：发现新的异羟肟酸化合物，例如其中R 1，R 2，R 3和R 4如所定义的式I的异羟肟酸化合物可用作药物，例如用于抑制TNF释放和治疗自身免疫性和炎性疾病，多发性硬化症和类风湿性关节炎。提供了制备化合物的方法，新型中间体和包含该化合物的药物组合物。

8. 发明授权

US06350907B1 Matrix metalloprotease inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：US06350907B1
公开(公告)日：2002-02-26
申请号：US09546756
申请日：2000-04-11
申请人： Michael Jonathan Fray , Roger Peter Dickinson , Kevin Neil Dack
发明人： Michael Jonathan Fray , Roger Peter Dickinson , Kevin Neil Dack
IPC分类号： C07C25904
CPC分类号： C07D213/75 , C07B2200/07 , C07C237/22 , C07C259/06 , C07C259/18 , C07C2602/08 , C07D317/34 , Y02P20/55
摘要： Compounds of formula (I): or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitors
摘要翻译：其中取代基具有本文所述的值的式（I）化合物或其药学上可接受的盐或任一实体的溶剂合物可用作基质金属蛋白酶（MMP）抑制剂

9. 发明授权

US06291709B1 Solid supported synthesis of hydroxamic acids 失效
标题翻译：固体支持的异羟肟酸合成
公开(公告)号：US06291709B1
公开(公告)日：2001-09-18
申请号：US09582975
申请日：2000-07-07
申请人： Adam Golebiowski , Sean Rees Klopfenstein
发明人： Adam Golebiowski , Sean Rees Klopfenstein
IPC分类号： C07C25904
CPC分类号： C07C259/04 , C07B2200/11 , C40B40/00
摘要： The subject invention involves processes for making hydroxamic acid compounds using a solid-support resin having an oxime moiety as the linking moiety of the resin, comprising the steps of (a) treating the resin with a carboxylic acid compound, such that it is attached to the resin by a condensation reaction between the oxime and carboxyl moieties; (b) optionally modifying the side chain; (c) cleaving a product from the resin by treating with O-tert-butyldimethylsilylhydroxylamine; (d) optionally modifying the side chain; and (e) optionally treating the resulting O-TBS-protected material with acid to produce an unprotected hydroxamic acid compound.
摘要翻译：本发明涉及使用具有肟部分的固体支持树脂作为树脂的连接部分制备异羟肟酸化合物的方法，包括以下步骤：（a）用羧酸化合物处理树脂，使其与该树脂通过肟和羧基部分之间的缩合反应; （b）任选改性侧链; （c）用O-叔丁基二甲基甲硅烷基羟胺处理从树脂中切割产物; （d）任选地改性侧链; 和（e）任选地用酸处理得到的O-TBS保护的材料以产生未保护的异羟肟酸化合物。

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