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1. 发明申请

US20060014780A1 Nicotinamide derivatives useful as PDE4 inhibitors 审中-公开
公开(公告)号：US20060014780A1
公开(公告)日：2006-01-19
申请号：US11229395
申请日：2005-09-16
申请人： Simon Bailey , Elisabeth Gautier , Alan Henderson , Thomas Magee , Anthony Marfat , John Mathias , Dale McLeod , Sandra Monaghan , Blanda Stammen
发明人： Simon Bailey , Elisabeth Gautier , Alan Henderson , Thomas Magee , Anthony Marfat , John Mathias , Dale McLeod , Sandra Monaghan , Blanda Stammen
IPC分类号： A61K31/46 , A61K31/4545 , A61K31/4433 , A61K31/4415 , C07D405/02 , C07D401/02 , C07D453/02
CPC分类号： C07D213/82 , A61K31/4433 , A61K31/455 , A61K31/46 , A61K31/537 , A61K45/06 , C07D401/12 , C07D405/12 , C07D451/04 , C07D451/10 , Y02A50/411 , A61K2300/00
摘要： The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.

2. 发明申请

US20050004093A1 Beta-lactamase inhibitor prodrug 审中-公开
标题翻译： β-内酰胺酶抑制剂前药
公开(公告)号：US20050004093A1
公开(公告)日：2005-01-06
申请号：US10862200
申请日：2004-06-07
申请人： Anthony Marfat , Dale McLeod , John O'Donnell
发明人： Anthony Marfat , Dale McLeod , John O'Donnell
IPC分类号： A61K31/351 , A61K31/357 , A61K31/397 , A61K31/43 , A61P31/04 , C07D309/12 , C07D319/12 , C07D499/00 , C07D499/48 , C07D499/86 , C07D499/861
CPC分类号： C07D499/861 , C07D309/12 , C07D319/12
摘要： Prodrugs of 6-β-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, each X is methylene, and Y is O, or wherein R is H, each X is O and Y is methylene, 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 at least one pharmaceutically acceptable carrier. 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：具有以下结构的6-β-羟甲基青霉烷酸砜的前药，其中R为H或甲基，X为亚甲基，Y为O，或其中R为H，每个X为O，Y为亚甲基，其溶剂化物为其公开的。还公开了包含本发明的前药或其溶剂合物，任选的β-内酰胺抗生素和至少一种药学上可接受的载体的药物组合物。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。

3. 发明授权

US06949573B2 Nicotinamide derivatives useful as PDE4 inhibitors 失效
标题翻译：可用作PDE4抑制剂的烟酰胺衍生物
公开(公告)号：US06949573B2
公开(公告)日：2005-09-27
申请号：US10361062
申请日：2003-02-06
申请人： Simon Bailey , Elisabeth C. L. Gautier , Alan J. Henderson , Thomas V. Magee , Anthony Marfat , John P. Mathias , Dale G. McLeod , Sandra M. Monaghan , Blanda L. C. Stammen
发明人： Simon Bailey , Elisabeth C. L. Gautier , Alan J. Henderson , Thomas V. Magee , Anthony Marfat , John P. Mathias , Dale G. McLeod , Sandra M. Monaghan , Blanda L. C. Stammen
IPC分类号： A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4545 , A61K31/455 , A61K31/46 , A61K31/537 , A61K45/06 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/06 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P31/16 , A61P31/22 , A61P35/00 , A61P37/00 , A61P37/02 , A61P43/00 , C07D213/82 , C07D401/12 , C07D405/12 , C07D451/04 , C07D451/10 , C07D213/643
CPC分类号： C07D213/82 , A61K31/4433 , A61K31/455 , A61K31/46 , A61K31/537 , A61K45/06 , C07D401/12 , C07D405/12 , C07D451/04 , C07D451/10 , Y02A50/411 , A61K2300/00
摘要： The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.
摘要翻译：本发明涉及烟酰胺衍生物以及制备用于制备含有这些衍生物的组合物和用途的中间体的方法。根据本发明的烟酰胺衍生物可用于许多疾病，病症和病症，特别是炎性，过敏性，呼吸道疾病，病症和病症以及伤口。

4. 发明申请

US20050049258A1 Ether derivatives useful as inhibitors of PDE4 isozymes 失效
标题翻译：醚类衍生物可用作PDE4同功酶的抑制剂
公开(公告)号：US20050049258A1
公开(公告)日：2005-03-03
申请号：US10918820
申请日：2004-08-13
申请人： Anthony Marfat , Robert Chambers , Thomas Magee
发明人： Anthony Marfat , Robert Chambers , Thomas Magee
IPC分类号： A61K31/44 , A61K31/443 , A61K31/4439 , A61P1/00 , A61P3/00 , A61P3/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P35/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D213/82 , C07D277/56 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , A61K31/497 , C07D213/62 , C07D213/78 , C07D239/02
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 eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease.
摘要翻译：本申请涉及下式的化合物其中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）

5. 发明授权

US07060717B2 Nicotinamide derivatives useful as PDE4 inhibitors 失效
公开(公告)号：US07060717B2
公开(公告)日：2006-06-13
申请号：US10865263
申请日：2004-06-09
申请人： Simon Bailey , Elisabeth C. L. Gautier , Alan J. Henderson , Thomas V. Magee , Anthony Marfat , John P. Mathias , Dale G. McLeod , Sandra M. Monaghan , Blanda L. C. Stammen
发明人： Simon Bailey , Elisabeth C. L. Gautier , Alan J. Henderson , Thomas V. Magee , Anthony Marfat , John P. Mathias , Dale G. McLeod , Sandra M. Monaghan , Blanda L. C. Stammen
IPC分类号： A61K31/445 , C07D211/72
CPC分类号： C07D213/82 , A61K31/4433 , A61K31/455 , A61K31/46 , A61K31/537 , A61K45/06 , C07D401/12 , C07D405/12 , C07D451/04 , C07D451/10 , Y02A50/411 , A61K2300/00
摘要： The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.

6. 发明申请

US20070161681A1 ETHER DERIVATIVES USEFUL AS INHIBITORS OF PDE4 ISOZYMES 审中-公开
标题翻译：其他衍生物作为PDE4 ISOZYMES的抑制剂有用
公开(公告)号：US20070161681A1
公开(公告)日：2007-07-12
申请号：US11668915
申请日：2007-01-30
申请人： Anthony Marfat , Robert Chambers , Thomas Magee
发明人： Anthony Marfat , Robert Chambers , Thomas Magee
IPC分类号： A61K31/4439 , C07D417/02 , C07D413/02
CPC分类号： C07D213/82 , C07D277/56 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12
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 the formula: wherein the substituents are as defined in the specification.
摘要翻译：可用作PDE4抑制剂的化合物，用于治疗受下列通式的嗜酸性粒细胞，特别是哮喘，慢性支气管炎和慢性阻塞性肺疾病的活化和脱颗粒调节的疾病，其中取代基如本说明书中所定义。

7. 发明申请

US20080125408A1 PENEM PRODRUG 审中-公开
公开(公告)号：US20080125408A1
公开(公告)日：2008-05-29
申请号：US11938942
申请日：2007-11-13
申请人： Katherine Elizabeth Brighty , Anthony Marfat , Dale Gordon McLeod , John P. O'Donnell , Stephen R. Anderson
发明人： Katherine Elizabeth Brighty , Anthony Marfat , Dale Gordon McLeod , John P. O'Donnell , Stephen R. Anderson
IPC分类号： A61K31/431 , C07D499/897 , A61P31/04
CPC分类号： C07D499/887
摘要： The invention relates to prodrugs of sulopenem of formula (I): wherein R1 is —(C2-C8)alkyl, or a solvate or hydrate thereof. The invention also relates to the preparation, formulation, and use of the prodrugs of sulopenem to treat a disorder such as an infection in a patient in need thereof.
摘要翻译：本发明涉及式（I）的磺脲的前药：其中R 1是 - （C 2 -C 8 -C 8）烷基，或溶剂化物或水合物。本发明还涉及用于治疗有需要的患者中的疾病如感染的疾病的前体药物的制备，制剂和用途。

8. 发明授权

US07250518B2 Nicotinamide acids, amides, and their mimetics active as inhibitors of PDE4 isozymes 失效
标题翻译：烟酰胺酸，酰胺及其作为PDE4同功酶抑制剂活性的模拟物
公开(公告)号：US07250518B2
公开(公告)日：2007-07-31
申请号：US10781062
申请日：2004-02-17
申请人： Thomas V. Magee , Anthony Marfat , Robert J. Chambers
发明人： Thomas V. Magee , Anthony Marfat , Robert J. Chambers
IPC分类号： C07D405/12 , C07D213/64
CPC分类号： C07D213/82 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/12
摘要： Compounds of the formula: useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils.
摘要翻译：式的化合物：可用作PDE4的抑制剂，用于治疗由嗜酸性粒细胞的活化和脱颗粒调节的疾病。

9. 发明授权

US06559168B2 Thiazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes 失效
标题翻译：可用作PDE4同功酶抑制剂的噻唑基酰胺衍生物
公开(公告)号：US06559168B2
公开(公告)日：2003-05-06
申请号：US10062145
申请日：2002-01-31
申请人： Anthony Marfat , Michael William McKechney
发明人： Anthony Marfat , Michael William McKechney
IPC分类号： C07D41710
CPC分类号： C07D417/12 , C07D277/56
摘要： This application is directed to 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 obstructuive pulmonary disease, of the formula: where Y is ═C(R1a)— or —[N□(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recited, optionally one carbon atom of said carbon ring system may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; E is selected from: and all other substituents shown above are as defined in the specification.
摘要翻译：本申请涉及可用作PDE4抑制剂的化合物，用于治疗由下列通式的嗜酸性粒细胞，特别是哮喘，慢性支气管炎和慢性阻塞性肺疾病的活化和脱颗粒调节的疾病，其中Y = C（R 1a） - 或 - [Nsquare（O）k] - 其中k是0或1; G 1是饱和或不饱和的碳环体系，其是3-至7-元单环，或者是7-12元稠合多环 ; 条件是G1不是如G2定义的不连续或限制性的联芳基部分; 其中任选地一个碳原子可以被选自N，O和S的杂原子取代; 其中任选地，其第二个碳原子和其另外任选的第三个碳原子可以被N取代; -G2是饱和或不饱和的碳环体系，其为3-至7-元单环; 或者是7-12元稠合的多环; 或者是7至18元不连续或限制性的联芳基部分; 其中对于所述碳环体系中的每一个，所述碳环体系的任选一个碳原子可被选自N，O和S的杂原子代替; 其中任选地，其第二个碳原子和其另外任选的第三个碳原子可以被N取代; E选自：和上述所有其它取代基如说明书中所定义。

10. 发明授权

US06391872B1 Indazole bioisostere replacement of catechol in therapeutically active compounds 失效
标题翻译：吲唑生物电子替代治疗活性化合物中的儿茶酚
公开(公告)号：US06391872B1
公开(公告)日：2002-05-21
申请号：US09381425
申请日：1999-09-20
申请人： Anthony Marfat
发明人： Anthony Marfat
IPC分类号： A61K314155
CPC分类号： C07D231/56
摘要： Therapeutically active compositions of matter and member species thereof are described which comprise indazole-containing compounds, said compounds and their therapeutic activity resulting directly from an indazole-for-catechol bioisostere replacement of a catechol-containing compound having the same therapeutic activity, where non-catechol substituents are the same or homologous before and after said replacement, and wherein said compositions of matter comprise a compound of Formula (I1) or (I2): or a pharmaceutically acceptable salt thereof, wherein in a preferred embodiment RC is hydrogen; RA is cyclohexyl; and RB is ethyl. Ra and Rb are each individually and independently hydrogen or non-catechol substituents of said compounds resulting directly from an indazole-for-catechol bioisostere replacement of said catechol-containing compound having said therapeutic activity, where said non-catechol substituents are the same or homologous before and after said replacement, provided that both of Ra and Rb cannot be hydrogen at the same time. The therapeutic activity involved may comprise cholinesterase inhibitory activity, adrenergic &agr;1-antagonist and &bgr;1-agonist activity, calcium channel inhibitory activity, antineoplastic activity, and phosphodiesterase type IV inhibitory activity.
摘要翻译：描述了物质及其成员物质的治疗活性组合物，其包含含吲唑的化合物，所述化合物及其直接由具有相同治疗活性的含儿茶酚的化合物的吲唑类邻苯二酚生物电子替代产生的治疗活性，邻苯二酚取代基在所述置换之前和之后是相同或同源的，并且其中所述物质组合物包含式（I 1）或（I 2）的化合物或其药学上可接受的盐，其中在优选的实施方案中，RC为氢; RA为环己基; 而RB是乙基。 R a和R b各自独立地和独立地是所述化合物的氢或非邻苯二酚取代基，其直接由具有所述治疗活性的所述含儿茶酚的化合物的吲唑 - 邻苯二酚生物电子替代物取代，其中所述非邻苯二酚取代基相同或同源在所述替换之前和之后，条件是Ra和Rb两者不能同时为氢。所涉及的治疗活性可包括胆碱酯酶抑制活性，肾上腺素能α1-拮抗剂和β1-激动剂活性，钙通道抑制活性，抗肿瘤活性和磷酸二酯酶IV抑制活性。

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