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公开(公告)号:US06620848B2
公开(公告)日:2003-09-16
申请号:US09930605
申请日:2001-08-15
申请人: Richard Mansfield Beams , Martin James Drysdale , Karl Witold Franzmann , Anthony Joseph Frend , Harold Francis Hodson , Richard Graham Knowles , Daryl David Rees , David Alan Sawyer
发明人: Richard Mansfield Beams , Martin James Drysdale , Karl Witold Franzmann , Anthony Joseph Frend , Harold Francis Hodson , Richard Graham Knowles , Daryl David Rees , David Alan Sawyer
IPC分类号: A61K31195
CPC分类号: C07C323/58
摘要: The present invention relates to novel amidino compound of formula (I): to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.
摘要翻译: 本发明涉及式(I)的新型脒基化合物:其制备方法,含有它们的药物组合物及其在治疗中的用途,特别是其作为诱导型一氧化氮合酶选择性抑制剂的用途。
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公开(公告)号:US06369272B1
公开(公告)日:2002-04-09
申请号:US09341220
申请日:1999-08-24
申请人: Richard Mansfield Beams , Martin James Drysdale , Karl Witold Franzmann , Anthony Joseph Frend , Harold Francis Hodson , Richard Graham Knowles , Daryl David Rees , David Alan Sawyer
发明人: Richard Mansfield Beams , Martin James Drysdale , Karl Witold Franzmann , Anthony Joseph Frend , Harold Francis Hodson , Richard Graham Knowles , Daryl David Rees , David Alan Sawyer
IPC分类号: A61K31195
CPC分类号: C07C323/58 , C07C323/59
摘要: The present invention relates to novel amidino compound of formula (I). to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.
摘要翻译: 本发明涉及式(I)的新的脒基化合物,其制备方法,含有它们的药物组合物及其在治疗中的用途,特别是其作为诱导型一氧化氮合酶选择性抑制剂的用途。
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公开(公告)号:US07589123B2
公开(公告)日:2009-09-15
申请号:US11773952
申请日:2007-07-05
申请人: Daryl David Rees , Phillip James Gunning , Antonia Orsi , Patrick A. Howson , Paul Barraclough , Noelle Callizot
发明人: Daryl David Rees , Phillip James Gunning , Antonia Orsi , Patrick A. Howson , Paul Barraclough , Noelle Callizot
CPC分类号: A61K31/12 , C07C45/455 , C07C45/62 , C07C45/673 , C07C45/68 , C07C45/74 , C07C49/255 , C07C49/577 , C07C49/84 , C07C69/738 , C07C217/22 , C07C255/56 , C07C2601/02 , C07C2601/10 , C07C2601/14 , C07F7/1804 , Y02P20/582
摘要: Compounds of general formula I: wherein: R1 and R2 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, optionally substituted —CO—(C1-10alkyl), optionally substituted C3-10cycloalkyl, optionally substituted —CO—(C3-10cycloalkyl), optionally substituted C2-10alkenyl, optionally substituted —CO—(C2-10alkenyl), optionally substituted aryl, and optionally substituted —CO-aryl, or R1 and R2 together represent an optionally substituted saturated or unsaturated C1-10alkylidene group, or an optionally substituted saturated or unsaturated C3-10cycloalkylidene group, or R1 and R2 together with the carbon atom to which they are attached represent an optionally substituted saturated or unsaturated organic ring containing 3, 4, 5, 6, 7 or 8 ring carbon atoms and optionally 1, 2 or 3 ring heteroatoms selected from O, N and S; R3, which may be the same as, or different from, either of R1 and R2, is selected from optionally substituted C1-10alkyl, optionally substituted C3-10cycloalkyl, optionally substituted C2-10alkenyl, and optionally substituted aryl; R4, R5 and R6 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, OH, optionally substituted C1-10 alkoxy, halo, optionally substituted aryloxy, optionally substituted (C1-10alkyl)-S(O)n— where n=0, 1 or 2, optionally substituted aryl-S(O)n— where n=0, 1 or 2, or R4 is hydrogen and R5 and R6 together represent an optionally substituted saturated or unsaturated organic chain containing 1, 2, 3, 4, 5, 6 or 7 chain carbon atoms and optionally 1, 2 or 3 chain heteroatoms selected from O, N and S, provided that the chain is at least 3 atoms long; with the proviso that, when R1═R2=hydrogen, then any optionally substituted C1-10alkyl or optionally substituted C2-10alkenyl for R3 must have a branch point at one or more of the α and β positions counted from the carbonyl group (or tautomeric form thereof) to which R3 is attached; or a physiologically acceptable salt, complex or prodrug thereof; are disclosed per se and for use in the treatment or prophylaxis of hypersensitivity, smooth muscle disorders, spasmodic conditions, allergic conditions, inflammatory conditions and/or pain.
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