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21. 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。

22. 发明申请

US20080009474A1 PENEM PRODRUGS 有权
公开(公告)号：US20080009474A1
公开(公告)日：2008-01-10
申请号：US11769849
申请日：2007-06-28
申请人： Katherine E. BRIGHTY , Anthony Marfat , Dale G. McLeod , John P. O'Donnell
发明人： Katherine E. BRIGHTY , Anthony Marfat , Dale G. McLeod , John P. O'Donnell
IPC分类号： A61K31/43 , C07D501/14
CPC分类号： C07D499/887
摘要： Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.
摘要翻译：口服生物可利用的磺脲类前体药物，例如及其溶剂化物和水合物，其制备，其制剂，以及治疗和预防哺乳动物如人类感染的用途。该摘要不限于本发明。

23. 发明授权

US07091197B2 Beta-lactamase inhibitor prodrug 失效
标题翻译： β-内酰胺酶抑制剂前药
公开(公告)号：US07091197B2
公开(公告)日：2006-08-15
申请号：US10648408
申请日：2003-08-25
申请人： Anthony Marfat , Dale G. McLeod
发明人： Anthony Marfat , Dale G. McLeod
IPC分类号： C07D499/861 , A61K31/43 , A61P31/04
CPC分类号： C07D499/00
摘要： Prodrugs of 6-β-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention or a solvate thereof, an optional beta-lactam antibiotic and a pharmaceutically acceptable excipient. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a beta-lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof.Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.
摘要翻译：公开了具有其中R为H或甲基的结构及其溶剂合物的6-β-羟甲基青霉烷酸砜的前药。还公开了包含本发明的前药或其溶剂合物，任选的β-内酰胺抗生素和药学上可接受的赋形剂的药物组合物。进一步公开的是通过施用有效量的β-内酰胺抗生素和增加有效量的本发明的前药或其溶剂化物来增加哺乳动物中β-内酰胺抗生素的治疗有效性的方法。另外公开了通过向有需要的哺乳动物施用治疗有效量的本发明药物组合物来治疗哺乳动物细菌感染的方法。

24. 发明授权

US06828333B2 Ether derivatives useful as inhibitors of PDE4 isozymes 失效
标题翻译：醚衍生物可用作PDE4同功酶的抑制剂
公开(公告)号：US06828333B2
公开(公告)日：2004-12-07
申请号：US10066503
申请日：2002-01-31
申请人： Anthony Marfat , Robert J. Chambers , Thomas V. Magee
发明人： Anthony Marfat , Robert J. Chambers , Thomas V. Magee
IPC分类号： A61K3144
CPC分类号： C07D213/82 , C07D277/56 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12
摘要： This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(═O)t—, where t is 0, 1, or 2; Y is ═C(R1a)—, where R1a is a member selected from the group consisting of H; F; Cl; CN; NO2; —(C1-C4) alkyl; —(C2-C4) alkynyl; fluorinated-(C1-C3) alkyl; fluorinated-(C1-C3) alkoxy; —OR16; and —C(═O)NR22aR22b; R22a and R22b are defined as set forth in the specification; —RA and RB are each a member independently selected from the group consisting of H; F; CF3; —(C1-C4) alkyl; —(C3-C7) cycloalkyl; phenyl; and benzyl; wherein said cycloalkyl, phenyl, and benzyl moieties are each independently substituted with 0 to 3 substituents R10, which is defined as set forth in the specification; R16 and R17 are defined as set forth in the specification; —RC and RD have the same meaning as defined above for RA and RB except that one of them must be —H, and they are selected independently of each other and of RA and RB; R1 and R2 are each a member independently selected from the group consisting of H; F; Cl; CN; NO2; —(C1-C4) alkyl; —(C2-C4) alkynyl; fluorinated-(C1-C3)alkyl; OR16; and —C(═O)NR22aR22b; —R3 is H; —(C1-C3)alkyl; phenyl; benzyl; or OR16; R4, R5 and R6 are defined as set forth in the specification; J1 and J2 are each independently a moiety comprising a saturated or unsaturated six-membered monocyclic carbon ring; and D is a member independently selected from the group consisting of partial Formulas (1.1.1) through (1.1.5) as set forth in the specification; a pharmaceutically acceptable salt thereof; which are useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinaphils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease.
摘要翻译：本申请针对的是化合物，其中j为1; k为0或1; m为1,2或3; n为1或2; W 1和W 2独立地是-O-或-S（= O）t - ，其中t是0,1或2; Y是= C（R a a a） - ，其中R a是选自H的成员; F; Cl; CN; NO2; - （C 1 -C 4）烷基; - （C 2 -C 4）炔基; 氟化 - （C 1 -C 3）烷基; 氟化 - （C1-C3）烷氧基; -OR <16>; 和-C（= O）NR 22 aR 22 b; R 22a和R 22b定义如说明书中所述; -R A和R B各自独立地选自H; F; CF3; - （C 1 -C 4）烷基; - （C 3 -C 7）环烷基; 苯基; 和苄基; 其中所述环烷基，苯基和苄基部分各自独立地被0至3个如本说明书所述定义的取代基R 10取代; R 16和R 17定义如说明书所述; -R＆lt; C＆gt;和R D具有与上述R A和R B相同的含义，不同之处在于它们之一必须是-H，并且它们彼此独立地选自和R 和R B; R 1和R 2各自独立地选自H; F; Cl; CN; NO2; - （C 1 -C 4）烷基; - （C 2 -C 4）炔基; 氟化 - （C 1 -C 3）烷基; OR <16>; 和-C（= O）NR 22 aR 22 b; -R 3为H; - （C 1 -C 3）烷基; 苯基; 苄基; 或OR 16; R 4，R 5和R 6是取代的

25. 发明授权

US06262040B1 Indazole derivatives and their use as inhibitors of phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF) 失效
标题翻译：吲唑衍生物及其作为IV型磷酸二酯酶（PDE）抑制剂和肿瘤坏死因子（TNF）的产生的用途，
公开(公告)号：US06262040B1
公开(公告)日：2001-07-17
申请号：US09254346
申请日：1999-03-04
申请人： Anthony Marfat
发明人： Anthony Marfat
IPC分类号： A61K31655
CPC分类号： C07D403/12 , C07D231/56 , C07D401/12 , C07D409/04
摘要： The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R1, and R2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of using, the compounds of formula (I), or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal. The invention also relates to intermediates that are useful in the preparation of the compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其中R，R 1和R 2如本文所定义。本发明进一步涉及药物组合物，其含有式（I）化合物或其可接受的盐用于抑制哺乳动物中IV型磷酸二酯酶（PDE）或肿瘤坏死因子（TNF）的产生的方法和使用方法。本发明还涉及可用于制备式（I）化合物的中间体。

26. 发明授权

US6166031A Substituted tetralins, chromans and related compounds in the treatment of asthma 失效
标题翻译：哮喘治疗中取代的四氢化萘，色满和相关化合物
公开(公告)号：US6166031A
公开(公告)日：2000-12-26
申请号：US474734
申请日：1990-04-11
申请人： James F. Eggler , Anthony Marfat , Lawrence S. Melvin, Jr.
发明人： James F. Eggler , Anthony Marfat , Lawrence S. Melvin, Jr.
IPC分类号： A61K31/4402 , A61K31/47 , A61K31/4709 , A61P1/14 , A61P11/06 , A61P17/06
CPC分类号： A61K31/4709 , A61K31/4402 , A61K31/47
摘要： Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals; pharmaceutical compositions comprising said compounds; a method of treatment with said compounds; and intermediates useful in the synthesis of said compounds.
摘要翻译： PCT No.PCT / US87 / 02734 Sec。 371日期1990年04月11日 102（e）日期1990年04月11日PCT 1987年10月19日提交了通过抑制5-脂氧合酶和/或阻断白三烯受体的取代的四氢化萘，色原和相关化合物可用于预防或治疗哮喘，关节炎，牛皮癣，溃疡，心肌梗塞和哺乳动物中的相关疾病状态; 包含所述化合物的药物组合物; 用所述化合物处理的方法; 以及可用于合成所述化合物的中间体。

27. 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。

28. 发明授权

US5965745A Indole carbamates as leukotriene antagonists 失效
标题翻译：吲哚氨基甲酸酯作为白三烯拮抗剂
公开(公告)号：US5965745A
公开(公告)日：1999-10-12
申请号：US51364
申请日：1998-07-01
申请人： Matthew F. Brown , Anthony Marfat
发明人： Matthew F. Brown , Anthony Marfat
IPC分类号： C07D401/12 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/495 , A61K31/535 , A61P11/00 , A61P11/08 , A61P27/16 , A61P29/00 , A61P37/08 , A61P43/00 , C07D209/10 , C07D209/18 , C07D401/06 , C07D403/06 , C07D413/06
CPC分类号： C07D209/18
摘要： Compounds of the formula ##STR1## wherein R.sup.1 AND R.sup.2 are as defined, useful in the treatment of asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways diseases, psoriasis, allergic rhinitis, atopic dermatitis, shock, and other inflammatory diseases and for blocking the leucotriene D4 receptor, pharmaceutical compositions containing such compounds and methods of blocking leucotriene D4 receptors using such compositions.
摘要翻译： PCT No.PCT / IB96 / 00832 Sec。 371日期：1998年7月1日 102（e）1998年7月1日PCT PCT 1996年8月26日PCT公布。公开号WO97 / 13751 日期1997年04月17日其中R1和R2如上所定义的化合物，其可用于治疗哮喘，类风湿性关节炎，骨关节炎，支气管炎，慢性阻塞性气道疾病，牛皮癣，过敏性鼻炎，特应性皮炎，休克和其他炎性疾病并且用于封闭白三烯D4受体，含有这些化合物的药物组合物和使用这种组合物阻断白三烯D4受体的方法。

29. 发明授权

US5952326A Tetralin and chroman derivatives useful in the treatment of asthma, arthritis and related diseases 失效
标题翻译：用于治疗哮喘，关节炎和相关疾病的四氢萘酮和苯并二氢吡喃衍生物
公开(公告)号：US5952326A
公开(公告)日：1999-09-14
申请号：US999064
申请日：1997-12-10
申请人： James F. Eggler , Anthony Marfat , Lawrence S. Melvin, Jr.
发明人： James F. Eggler , Anthony Marfat , Lawrence S. Melvin, Jr.
IPC分类号： C07D405/12 , C07D405/14 , C07D417/14 , A61K31/47 , C07D215/227
CPC分类号： C07D405/12 , C07D405/14 , C07D417/14
摘要： Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or �(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.
摘要翻译：下式的化合物其中R是任选取代的杂芳基如2-苯并二氢吡喃基，2-吡啶基或5-氟-2-苯并噻唑基; X是O，S或（CH 2）m; R 1是苯基或吡啶基，任选地被一个或多个（C 1 -C 3）烷基，（C 1 -C 3）烷氧基，羧基或[（C 1 -C 3）烷氧基]羰基取代; n为0,1或2; m为1或2; Y和Y1一起是氧，或Y和Y1分别取代，Y是氢，Y1是羟基或体内可水解的酰氧基; Z是CH 2，NR 2，O或S; 并且R 2是氢或（C 1 -C 3）烷基; 可用于治疗由白三烯介导的哮喘，关节炎和相关疾病。

30. 发明授权

US5698550A Tetralin and chroman derivatives useful in the treatment of asthma, arthritis and related diseases 失效
标题翻译：用于治疗哮喘，关节炎和相关疾病的四氢萘酮和苯并二氢吡喃衍生物
公开(公告)号：US5698550A
公开(公告)日：1997-12-16
申请号：US920291
申请日：1993-06-14
申请人： James F. Eggler , Anthony Marfat , Lawrence S. Melvin, Jr.
发明人： James F. Eggler , Anthony Marfat , Lawrence S. Melvin, Jr.
IPC分类号： C07D215/22 , C07D215/227 , C07D215/233 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/14 , A61K31/55 , A61K31/47
CPC分类号： C07D215/227 , C07D215/233 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/14
摘要： Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl; X is O, S or (CH.sub.2).sub.m ; R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or �(C.sub.1 -C.sub.3)alkoxy!carbonyl groups; n is 0, 1 or 2; m is 1 or 2; Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group; Z is CH.sub.2, NR.sup.2, O or S; and R.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl; are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.
摘要翻译：式（I）的化合物其中R是任选取代的杂芳基如2-苯并二氢吡喃基，2-吡啶基或5-氟-2-苯并噻唑基; X是O，S或（CH 2）m; R 1是苯基或吡啶基，任选地被一个或多个（C 1 -C 3）烷基，（C 1 -C 3）烷氧基，羧基或[（C 1 -C 3）烷氧基]羰基取代; n为0,1或2; m为1或2; Y和Y1一起是氧，或Y和Y1分别取代，Y是氢，Y1是羟基或体内可水解的酰氧基; Z是CH 2，NR 2，O或S; 并且R 2是氢或（C 1 -C 3）烷基; 可用于治疗由白三烯介导的哮喘，关节炎和相关疾病。

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