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1. 发明授权

US06740655B2 Pyrimidine carboxamides useful as inhibitors of PDE4 isozymes 失效
标题翻译：可用作PDE4同功酶抑制剂的嘧啶甲酰胺
公开(公告)号：US06740655B2
公开(公告)日：2004-05-25
申请号：US10181417
申请日：2002-07-24
申请人： Thomas Victor Magee , Anthony Marfat , Robert James Chambers
发明人： Thomas Victor Magee , Anthony Marfat , Robert James Chambers
IPC分类号： A61K3138
CPC分类号： C07D239/34 , A61K45/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/14
摘要： This invention is directed to compounds of the formula: wherein j is 0 or 1; k is 0 or 1; m is 0 or 1; n is 0 or 1; W is —O—; —S(═O)t—, where t is 0, 1, or 2; or —N(R3)—; where R3 is —H, —(C1-C3) alkyl, —OR12, phenyl, or benzyl; RC and RD have the same meaning as RA and RB, except that at least one of RC and RD must be —H; and the other variables are defined as set forth in the specification. The invention is also directed to pharmaceutical compositions comprising the above compounds and to methods of treating a subject suffering from a disease, disorder or condition mediated by the PDE4 isozyme, the method comprising administering a therapeutically effective amount of a compound as described above. The invention is particularly directed to methods of treating inflammatory, respiratory and allergic diseases and conditions, especially asthma; chronic obstructive pulmonary disease (COPD) including chronic bronchitis, emphysema, and bronchiectasis; chronic rhinitis; and chronic sinusitis.
摘要翻译：本发明涉及下式的化合物：其中j是0或1; k为0或1; m为0或1; n为0或1; W是-O-; -S（= O）t-，其中t为0,1或2; 或-N（R 3） - ; 其中R 3是-H， - （C 1 -C 3）烷基，-OR 12，苯基或苄基; R C和R D具有与R A和R B相同的含义，除了R C和R D中的至少一个必须为-H; 并且其他变量被定义为说明书中阐述的。本发明还涉及包含上述化合物的药物组合物和治疗患有由PDE4同功酶介导的疾病，病症或病况的受试者的方法，所述方法包括施用治疗有效量的如上所述的化合物。本发明特别涉及治疗炎性，呼吸和过敏性疾病和病症，特别是哮喘的方法; 慢性阻塞性肺疾病（COPD），包括慢性支气管炎，肺气肿和支气管扩张; 慢性鼻炎和慢性鼻窦炎。

2. 发明授权

US6096901A Processes and intermediates for preparing 2-fluorothiophene derivatives 失效
标题翻译：制备2-氟噻吩衍生物的方法和中间体
公开(公告)号：US6096901A
公开(公告)日：2000-08-01
申请号：US450976
申请日：1999-11-30
申请人： Anthony Marfat , Robert James Chambers
发明人： Anthony Marfat , Robert James Chambers
IPC分类号： C07D333/38
CPC分类号： C07D333/38
摘要： A process for the preparation of the compound of the formula: ##STR1## wherein R.sup.1 is OH, which comprises the steps of a) treating the compound of the formula: ##STR2## with an inorganic fluoride, of the formula M.sup.2 F wherein M.sup.2 is an alkali metal cation, at an elevated temperature in the presence of a compound of the formula R.sup.4 P.sup.+ Z.sup.- and a compound of the formula R.sup.5 vic (COW).sub.2 wherein R.sup.4 and R.sup.5 are each selected from optionally substituted (C.sub.6 -C.sub.10) aryl and optionally substituted (C.sub.1 -C.sub.6) alkyl, and W is halo; to form the compound of the formula: ##STR3## and b) I) treating the compound of the formula IV with an aqueous solution of a base, of the formula MOH, wherein M is an alkali metal cation, andii) treating the product of step i) with a mineral acid. A compound of the formula: ##STR4## wherein R.sup.1 is selected from the group consisting of, halo, R.sup.7 O, R.sup.7 COO and N(R.sup.8).sub.2 wherein R.sup.7 is (C.sub.1 -C.sub.6)alkyl or (C.sub.6 -C.sub.10)aryl and each R.sup.8 is selected from hydrogen and R.sup.7 with the proviso that R.sup.7 is not methyl when R.sup.1 is R.sup.7 O.
摘要翻译：一种制备下式化合物的方法，其中R1是OH，其包括以下步骤：a）用式M2F的无机氟化物处理其中M2为碱金属阳离子的式在式R4P + Z-的化合物和式的化合物R5vic（COW）2的存在下升高温度，其中R 4和R 5各自选自任选取代的（C 6 -C 10）芳基和任选取代的（C 1 -C 6）烷基，W是卤素; 形成下式的化合物：和b）I）用式MOH的碱的水溶液处理式IV的化合物，其中M是碱金属阳离子，和ii）处理步骤i的产物）与无机酸。下式的化合物：其中R 1选自卤素，R 7 O，R 7 COO和N（R 8）2，其中R 7是（C 1 -C 6）烷基或（C 6 -C 10）芳基，并且每个R 8选自氢和R 7，条件是当R 1是R 7 O时，R 7不是甲基。

3. 发明授权

US07354941B2 Nicotinamide benzofused-heterocyclyl derivatives useful as selective inhibitors of PDE4 isozymes 失效
标题翻译：可用作PDE4同功酶选择性抑制剂的烟酰胺苯并吲哚杂环基衍生物
公开(公告)号：US07354941B2
公开(公告)日：2008-04-08
申请号：US10181416
申请日：2001-01-30
申请人： Anthony Marfat , Robert James Chambers
发明人： Anthony Marfat , Robert James Chambers
IPC分类号： A61K31/465
CPC分类号： C07D401/12 , A61K45/06 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of Formula (1.0.0): wherein R5 and R6 are taken together to form a moiety of partial Formulas (1.1.1) through (1.1.5): or a pharmaceutically acceptable salt thereof.
摘要翻译：可用作PDE4抑制剂的化合物用于治疗由式（1.0.0）的嗜酸性粒细胞，特别是哮喘，慢性支气管炎和慢性阻塞性肺病的活化和脱颗粒调节的疾病：其中R 5，和R 6彼此一起形成部分式（1.1.1）至（1.1.5）的部分：或其药学上可接受的盐。

4. 发明授权

US6043379A Processes and intermediates for preparing 2-fluorothiophene derivatives 失效
标题翻译：制备2-氟噻吩衍生物的方法和中间体
公开(公告)号：US6043379A
公开(公告)日：2000-03-28
申请号：US355265
申请日：1999-07-26
申请人： Anthony Marfat , Robert James Chambers
发明人： Anthony Marfat , Robert James Chambers
IPC分类号： C07D333/38
CPC分类号： C07D333/38
摘要： A process for the preparation of the compound of the formula ##STR1## wherein R.sup.1 is OH, which comprises the steps of a) treating the compound of the formula ##STR2## with an inorganic fluoride, of the formula M.sup.2 F wherein M.sup.2 is an alkali metal cation, at an elevated temperature in the presence of a compound of the formula R.sup.4 P.sup.+ Z.sup.- and a compound of the formula R.sup.5 vic (COW).sub.2 wherein R.sup.4 and R.sup.5 are each selected from optionally substituted (C.sub.6 -C.sub.10)aryl and optionally substituted (C.sub.1 -C.sub.6)alkyl, and W is halo; to form the compound of the formula; ##STR3## and b) i) treating the compound of the formula IV with an aqueous solution of a base, of the formula MOH, wherein M is an alkali metal cation, andii) treating the product of step i) with a mineral acid. A compound of the formula ##STR4## wherein R.sup.1 is selected from the group consisting of, halo, R.sup.7 O, R.sup.7 COO and N(R.sup.8).sub.2 wherein R.sup.7 is (C.sub.1 -C.sub.6)alkyl or (C.sub.6 -C.sub.10)aryl and each R.sup.8 is selected from hydrogen and R.sup.7 with the proviso that R.sup.7 is not methyl when R.sup.1 is R.sup.7 O.
摘要翻译： PCT No.PCT / IB98 / 00304 Sec。 371日期：1999年7月26日 102（e）1999年7月26日PCT 1998年3月9日PCT PCT。出版物WO98 / 45282 日期1998年10月15日制备下式化合物的方法其中R1是OH，其包括以下步骤：a）用式M2F的无机氟化物处理式的化合物，其中M2是碱金属阳离子在式R4P + Z-的化合物和式R 5 vic（COW）2的化合物的存在下，在升高的温度下，其中R 4和R 5各自选自任选取代的（C 6 -C 10）芳基和任选取代的（C 1 -C 10） -C 6）烷基，W是卤素; 形成式的化合物; 和b）i）用式MOH的碱的水溶液处理式IV的化合物，其中M是碱金属阳离子，和ii）用无机酸处理步骤i）的产物。下式的化合物其中R 1选自卤素，R 7 O，R 7 COO和N（R 8）2，其中R 7是（C 1 -C 6）烷基或（C 6 -C 10）芳基，并且每个R 8选自氢和 R7，条件是当R1为R7O时，R7不是甲基。

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