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1. 发明授权

US06255326B1 Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic-or heteroatom-containing linking group 失效
标题翻译：含有通过含脂肪族或含杂原子的连接基与芳基或杂芳基连接的苯基的化合物
公开(公告)号：US06255326B1
公开(公告)日：2001-07-03
申请号：US09239075
申请日：1999-01-27
申请人： Michael John Ashton , David Charles Cook , Garry Fenton , Susan Jacqueline Hills , Ian Michael McFarlane , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Nigel Vicker
发明人： Michael John Ashton , David Charles Cook , Garry Fenton , Susan Jacqueline Hills , Ian Michael McFarlane , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Nigel Vicker
IPC分类号： C07D21172
CPC分类号： C07C43/225 , C07C45/004 , C07C45/292 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/57 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D213/50 , C07D213/75 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07D409/12
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
摘要翻译：本发明涉及通过各种连接与芳基部分连接的用于抑制肿瘤坏死因子的苯基化合物的药物用途。本发明还涉及含有这些化合物的化合物及其制备方法和药物组合物。此外，本发明涉及化合物抑制环AMP磷酸二酯酶的药物用途。

2. 发明授权

US6096768A Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic- or heteroatom-containing linking group 有权
标题翻译：含有通过含脂肪族或含杂原子的连接基与芳基或杂芳基连接的苯基的化合物
公开(公告)号：US6096768A
公开(公告)日：2000-08-01
申请号：US301877
申请日：1999-04-29
申请人： Michael John Ashton , David Charles Cook , Garry Fenton , Susan Jacqueline Hills , Ian Michael McFarlane , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Nigel Vicker
发明人： Michael John Ashton , David Charles Cook , Garry Fenton , Susan Jacqueline Hills , Ian Michael McFarlane , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Nigel Vicker
IPC分类号： C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07C235/56 , C07C255/60 , C07C311/46 , C07C323/42 , C07D213/75 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/02 , C07D275/03 , A61K31/435 , A61K31/165 , A61K31/44 , A61K31/4523 , C07D211/72
CPC分类号： C07D213/75 , C07C235/56 , C07C255/60 , C07C311/46 , C07C323/42 , C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07C2101/08 , C07C2101/14 , C07C2102/42
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
摘要翻译：本发明涉及通过各种连接与芳基部分连接的用于抑制肿瘤坏死因子的苯基化合物的药物用途。本发明还涉及含有这些化合物的化合物及其制备方法和药物组合物。此外，本发明涉及化合物抑制环AMP磷酸二酯酶的药物用途。

3. 发明授权

US5935978A Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic- or heteroatom-containing linking group 失效
公开(公告)号：US5935978A
公开(公告)日：1999-08-10
申请号：US98178
申请日：1993-07-28
申请人： Garry Fenton , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Michael John Ashton , David Charles Cook , Susan Jacqueline Hills , Ian Michael McFarlane , Nigel Vicker
发明人： Garry Fenton , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Michael John Ashton , David Charles Cook , Susan Jacqueline Hills , Ian Michael McFarlane , Nigel Vicker
IPC分类号： C07C43/225 , C07C45/00 , C07C45/29 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/42 , C07C69/76 , C07C69/92 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/57 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07D213/50 , C07D213/75 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/02 , C07D275/03 , C07D409/12 , A61K31/44
CPC分类号： C07D213/75 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/57 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07C43/225 , C07C45/004 , C07C45/292 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/42 , C07C69/76 , C07C69/92 , C07D213/50 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07D409/12 , C07C2101/08 , C07C2101/14 , C07C2102/42
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

4. 发明授权

US5840724A Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic- o r 失效
公开(公告)号：US5840724A
公开(公告)日：1998-11-24
申请号：US881888
申请日：1997-06-24
申请人： Garry Fenton , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Keith Alfred James Stuttle , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher
发明人： Garry Fenton , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Keith Alfred James Stuttle , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher
IPC分类号： C07C43/225 , C07C45/00 , C07C45/29 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07D213/50 , C07D213/75 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/02 , C07D275/03 , C07D409/12 , C07D213/02 , A61K31/44
CPC分类号： C07C43/225 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07C45/004 , C07C45/292 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07D213/50 , C07D213/75 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07D409/12 , C07C2101/08 , C07C2101/14 , C07C2102/42
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

5. 发明授权

US5679696A Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic-or heteroatom-containing linking group 失效
标题翻译：含有通过含脂肪族或含杂原子的连接基与芳基或杂芳基连接的苯基的化合物
公开(公告)号：US5679696A
公开(公告)日：1997-10-21
申请号：US484805
申请日：1995-06-07
申请人： Garry Fenton , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Keith Alfred James Stuttle , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher
发明人： Garry Fenton , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Keith Alfred James Stuttle , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher
IPC分类号： C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07C235/56 , C07C255/60 , C07C311/46 , C07C323/42 , C07D213/75 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/02 , C07D275/03 , A61K31/44 , C07D213/02
CPC分类号： C07D213/75 , C07C235/56 , C07C255/60 , C07C311/46 , C07C323/42 , C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07C2101/08 , C07C2101/14 , C07C2102/42
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
摘要翻译：本发明涉及通过各种连接与芳基部分连接的用于抑制肿瘤坏死因子的苯基化合物的药物用途。本发明还涉及含有这些化合物的化合物及其制备方法和药物组合物。此外，本发明涉及化合物抑制环AMP磷酸二酯酶的药物用途。

6. 发明授权

US06472412B1 Compounds as PDE IV and TNF inhibitors 失效
标题翻译：化合物作为PDE IV和TNF抑制剂
公开(公告)号：US06472412B1
公开(公告)日：2002-10-29
申请号：US08592817
申请日：1996-01-26
申请人： Garry Fenton , Tahir Nadeem Majid , Malcolm Norman Palfreyman
发明人： Garry Fenton , Tahir Nadeem Majid , Malcolm Norman Palfreyman
IPC分类号： A61K3144
CPC分类号： C07D213/70 , C07C43/247 , C07C217/58 , C07C235/56 , C07C237/30 , C07C255/60 , C07C327/48 , C07C2601/08 , C07C2603/64 , C07C2603/66 , C07D213/65 , C07D213/69 , C07D213/75 , C07D213/79 , C07D213/81 , C07D213/82 , C07D213/89 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.
摘要翻译：本发明涉及[二（醚或硫醚）杂芳基或氟取代的芳基]化合物或其N-氧化物或其药学上可接受的盐，其可用于抑制TNF在治疗中的产生或生理作用患有与生理上有害的肿瘤坏死因子（TNF）过量相关的疾病状态的患者。本发明范围内的化合物还抑制环AMP磷酸二酯酶，并且可用于治疗与由下列疾病调节的病理状况相关的疾病状态：抑制环AMP磷酸二酯酶，这种疾病状态包括炎性和自身免疫疾病，特别是IV型环AMP磷酸二酯酶。因此，本发明涉及其用于抑制TNF和/或环AMP磷酸二酯酶的药理学用途，包含该化合物的药物组合物及其制备方法。

7. 发明授权

US07045660B2 Compounds as PDE IV and TNF-inhibitors 有权
公开(公告)号：US07045660B2
公开(公告)日：2006-05-16
申请号：US10792579
申请日：2004-03-03
申请人： Garry Fenton , Tahir Nadeem Majid , Malcolm Norman Palfreyman
发明人： Garry Fenton , Tahir Nadeem Majid , Malcolm Norman Palfreyman
IPC分类号： C07C233/64 , A61K31/165
CPC分类号： C07D213/70 , C07C43/247 , C07C217/58 , C07C235/56 , C07C237/30 , C07C255/60 , C07C327/48 , C07C2601/08 , C07C2603/64 , C07C2603/66 , C07D213/65 , C07D213/69 , C07D213/75 , C07D213/79 , C07D213/81 , C07D213/82 , C07D213/89 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF).Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.

8. 发明授权

US07652144B2 Compounds as PDE IV and TNF inhibitors 失效
标题翻译：化合物作为PDE IV和TNF抑制剂
公开(公告)号：US07652144B2
公开(公告)日：2010-01-26
申请号：US11764317
申请日：2007-06-18
申请人： Garry Fenton , Tahir Nadeem Majid , Malcolm Norman Palfreyman
发明人： Garry Fenton , Tahir Nadeem Majid , Malcolm Norman Palfreyman
IPC分类号： C07D213/02
CPC分类号： C07D213/70 , C07C43/247 , C07C217/58 , C07C235/56 , C07C237/30 , C07C255/60 , C07C327/48 , C07C2601/08 , C07C2603/64 , C07C2603/66 , C07D213/65 , C07D213/69 , C07D213/75 , C07D213/79 , C07D213/81 , C07D213/82 , C07D213/89 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： A compound of formula XIX wherein R1, R2, Z1, Z2, Q1, Q2 and Q3 as defined in the specification.
摘要翻译：式XIX的化合物，其中R1，R2，Z1，Z2，Q1，Q2和Q3如说明书中所定义。

9. 发明授权

US08129537B2 Compounds as PDE IV and TNF inhibitors 失效
标题翻译：化合物作为PDE IV和TNF抑制剂
公开(公告)号：US08129537B2
公开(公告)日：2012-03-06
申请号：US12693791
申请日：2010-01-26
申请人： Garry Fenton , Tahir Nadeem Majid , Malcolm Norman Palfreyman
发明人： Garry Fenton , Tahir Nadeem Majid , Malcolm Norman Palfreyman
IPC分类号： C07D211/72 , A61K31/44
CPC分类号： C07D213/70 , C07C43/247 , C07C217/58 , C07C235/56 , C07C237/30 , C07C255/60 , C07C327/48 , C07C2601/08 , C07C2603/64 , C07C2603/66 , C07D213/65 , C07D213/69 , C07D213/75 , C07D213/79 , C07D213/81 , C07D213/82 , C07D213/89 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF).Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.
摘要翻译：本发明涉及[二（醚或硫醚）杂芳基或氟取代的芳基]化合物或其N-氧化物或其药学上可接受的盐，其可用于抑制TNF在治疗中的产生或生理作用患有与生理上有害的肿瘤坏死因子（TNF）过量相关的疾病状态的患者。本发明范围内的化合物还抑制环AMP磷酸二酯酶，并且可用于治疗与通过抑制环AMP磷酸二酯酶调节的病理状况相关的疾病状态，所述疾病状态包括炎性和自身免疫性疾病，特别是IV型环AMP 磷酸二酯酶。因此，本发明涉及其用于抑制TNF和/或环AMP磷酸二酯酶的药理学用途，包含该化合物的药物组合物及其制备方法。

10. 发明授权

US06762199B2 Indane derivatives 有权
标题翻译：茚满衍生物
公开(公告)号：US06762199B2
公开(公告)日：2004-07-13
申请号：US10229592
申请日：2002-08-28
申请人： Garry Fenton , Clive McCarthy , Robert Edward MacKenzie , Andrew David Morley
发明人： Garry Fenton , Clive McCarthy , Robert Edward MacKenzie , Andrew David Morley
IPC分类号： A61K31423
CPC分类号： C07D263/58 , C07D235/30
摘要： The invention is directed to physiologically active compounds of general formula (I): wherein: R1 represents aryl, heteroaryl or a group R3—L2—Ar1—L3—; R2 represents hydrogen or lower alkyl; R3 represents aryl or heteroaryl; and Ar1 represents an optionally substituted saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring system containing at least one heteroatom selected from O, S or N; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).
摘要翻译：本发明涉及通式（I）的生理活性化合物：其中：R 1表示芳基，杂芳基或基团R 3 -L 2 -Ar 1 -L 3 - ; R R 2表示氢或低级烷基; R 3表示芳基或杂芳基; 并且Ar 1表示任选取代的饱和，部分饱和或完全不饱和的8至10元双环体系，其含有至少一个选自O，S或N的杂原子; Y是羧基或酸式生物电子等排体;及其相应的N-氧化物或这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力，。

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