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1. 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.

2. 发明授权

US07462600B2 Macrolides 失效
标题翻译：大环内酯类
公开(公告)号：US07462600B2
公开(公告)日：2008-12-09
申请号：US11313523
申请日：2005-12-21
申请人： Louis S. Chupak , Mark E. Flanagan , Takushi Kaneko , Thomas V. Magee , Mark C. Noe , Usa Reilly
发明人： Louis S. Chupak , Mark E. Flanagan , Takushi Kaneko , Thomas V. Magee , Mark C. Noe , Usa Reilly
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/08
摘要： Macrolide compounds per se, as shown below and defined herein, and their use, e.g., as antibacterial and antiprotozoal agents in animals, including humans: Also disclosed are methods of preparing the compounds, intermediates, and pharmaceutical compositions thereof, and methods of treating or preventing disease by administering the compounds to subjects in need. This abstract is only an excerpt and is not limiting of the invention.
摘要翻译：大环内酯类化合物本身，如下文所示和定义，以及它们在动物（包括人）中作为抗细菌剂和抗原虫药的用途：还公开了制备化合物，中间体及其药物组合物的方法，以及治疗或通过将化合物给予需要的受试者来预防疾病。该摘要仅是摘录而不是本发明的限制。

3. 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。

4. 发明授权

US07183293B2 Ether derivatives useful as inhibitors of PDE4 isozymes 失效
公开(公告)号：US07183293B2
公开(公告)日：2007-02-27
申请号：US10918820
申请日：2004-08-13
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： C07D405/12 , A61K31/44
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.

5. 发明授权

US06953810B2 Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes 失效
公开(公告)号：US06953810B2
公开(公告)日：2005-10-11
申请号：US10613988
申请日：2003-07-02
申请人： Robert J. Chambers , Anthony Marfat , Thomas V. Magee
发明人： Robert J. Chambers , Anthony Marfat , Thomas V. Magee
IPC分类号： A61K20060101 , A61K31/155 , A61K31/17 , A61K31/343 , A61K31/353 , A61K31/381 , A61K31/4045 , A61K31/415 , A61K31/44 , A61K31/4433 , A61K31/4439 , A61K31/455 , A61K31/47 , A61K31/4704 , A61K31/4709 , A61K31/5415 , A61P20060101 , A61P1/16 , A61P3/10 , A61P7/06 , A61P7/10 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/08 , A61P13/00 , A61P13/02 , A61P13/08 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/06 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/16 , A61P31/18 , A61P31/20 , A61P31/22 , A61P33/06 , A61P35/02 , A61P37/02 , A61P37/08 , C07D20060101 , C07D213/82 , C07D213/89 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D413/12 , C07D417/12 , A61K31/4412 , C07D417/02
CPC分类号： C07D213/82 , C07D405/12
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 obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; W1 is —O—; or —S(═O)t—, where t is 0, 1, or 2; or —N(R3)—; W2 is —O—CRARB— or is absent; Y is ═C(R1a)— or —[N→(O)k]— where k is 0 or 1; RA and RB are —H; —F; —CF3; —(C1-C4)alkyl; —(C3-C7) cycloalkyl; phenyl; or benzyl substituted with 0 to 3 substituents R10; or RA and RB are taken together, but only in the case where m is 1, to form a spiro moiety; RC and RD have the same meaning as RA and RB except that one of them must be —H, R1 and R2 are —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 in addition to other meanings may be taken together to form, e.g., Q1 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 Q1 is not a discontinuous or restricted biaryl moiety as defined under Q2; 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; Q2 is a discontinuous or restricted biaryl moiety consisting of 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; 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; Z is selected from:

6. 发明授权

US06649633B2 Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes 失效
标题翻译：可用作PDE4同功酶抑制剂的烟酰胺联芳衍生物
公开(公告)号：US06649633B2
公开(公告)日：2003-11-18
申请号：US10062813
申请日：2002-01-31
申请人： Robert J. Chambers , Anthony Marfat , Thomas V. Magee
发明人： Robert J. Chambers , Anthony Marfat , Thomas V. Magee
IPC分类号： A61K3144
CPC分类号： C07D213/82 , C07D405/12
摘要： This application is directed to compounds useful as inhibitors at 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 j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; W1 is —O—; or —S(═O)t—, where t is 0, 1, or 2; Y is —C(R1a); Q1 is phenyl or substituted phenyl; Q2 is biphenyl or substituted biphenyl; and the remaining variables are defined as set forth in the specification. This application is also directed to pharmaceutical compositions comprising those compounds and to methods of treating diseases regulated by the activation and degranulation of eosinophils, in particular asthma, chronic bronchitis and chronic obstructive pulmonary disease.
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j为0或1，条件是当j 为0，n必须为2; k为0或1; m为0,1或2; n为1或2; W 1是-O-; 或-S（= O）t - ，其中t为0,1或2; Y是-C（R 1a）; Q 1是苯基或取代的苯基; Q 2是联苯基或取代的联苯基; 并且其余变量被定义为说明书中所阐述的。本申请还涉及包含那些化合物的药物组合物和治疗由嗜酸性粒细胞，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的方法。

7. 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

8. 发明授权

US5488116A Total synthesis of taxol and analogues thereof 失效
标题翻译：紫杉醇及其类似物的总合成
公开(公告)号：US5488116A
公开(公告)日：1996-01-30
申请号：US146704
申请日：1993-11-02
申请人： Samuel J. Danishefsky , William G. Bornmann , Yves Queneau , Thomas V. Magee , Walter J. Krol , John J. Masters , David K. Jung
发明人： Samuel J. Danishefsky , William G. Bornmann , Yves Queneau , Thomas V. Magee , Walter J. Krol , John J. Masters , David K. Jung
IPC分类号： A61K31/335 , C07C13/28 , C07C45/29 , C07C45/59 , C07C49/603 , C07C49/613 , C07C49/687 , C07C49/713 , C07C49/723 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/757 , C07C255/31 , C07C255/45 , C07C255/46 , C07D305/14 , C07D317/72 , C07D339/08 , C07D493/04 , C07F7/18 , C07D317/70
CPC分类号： C07F7/1856 , C07C255/31 , C07C255/46 , C07C403/08 , C07C403/14 , C07C403/16 , C07C403/20 , C07C45/29 , C07C45/59 , C07C49/613 , C07C49/687 , C07C49/713 , C07C49/723 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/757 , C07D305/14 , C07D317/72 , C07F7/1852 , C07C2101/14 , C07C2101/16
摘要： The present invention provides three basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.
摘要翻译：本发明提供了具有以下结构的紫杉醇的总合成的三种基本途径：本发明还提供了上述方法中制备的中间体，合成这些中间体的方法以及紫杉醇和北美多酚的类似物。

9. 发明申请

US20080293646A1 MACROLIDES 审中-公开
公开(公告)号：US20080293646A1
公开(公告)日：2008-11-27
申请号：US12047154
申请日：2008-03-12
申请人： Thomas V. Magee , Usa Reilly , Mark Carl Noe , Mark E. Flanagan , Zhengong Bryan Li , Richard Allen Buzon , Daniel William Widlicka
发明人： Thomas V. Magee , Usa Reilly , Mark Carl Noe , Mark E. Flanagan , Zhengong Bryan Li , Richard Allen Buzon , Daniel William Widlicka
IPC分类号： A61K31/7048 , C07H17/08 , C07D471/02 , A61P31/04
CPC分类号： C07H17/08
摘要： The invention relates to compounds of Formula (I): wherein R1, R2 and X are as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of Formula (I).
摘要翻译：本发明涉及式（I）的化合物：其中R1，R2和X如本文所定义。本发明还涉及使用式（I）的化合物治疗细菌感染的药物组合物和方法。

10. 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。

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