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1. 发明授权

US06479519B1 Substituted anilides 有权
标题翻译：取代的酰苯胺
公开(公告)号：US06479519B1
公开(公告)日：2002-11-12
申请号：US09558812
申请日：2000-04-26
申请人： Peter Charles Astles , David Edward Clark , Alan John Collis , Paul Joseph Cox , Paul Robert Eastwood , Neil Victor Harris , Justine Yeun Quai Lai , Andrew David Morley , Barry Porter
发明人： Peter Charles Astles , David Edward Clark , Alan John Collis , Paul Joseph Cox , Paul Robert Eastwood , Neil Victor Harris , Justine Yeun Quai Lai , Andrew David Morley , Barry Porter
IPC分类号： C07C27538
CPC分类号： C07D213/75 , C07C275/42 , C07D211/62 , C07D213/71 , C07D213/81 , C07D213/82 , C07D213/89 , C07D233/84 , C07D237/24 , C07D261/18 , C07D309/06 , C07D333/38
摘要： The invention is directed to physiologically active compounds of formula (I): wherein: R1 is hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR10; and one of X3, X4 and X5 represents CR11 and the others independently represents N or CR10; where R10 is hydrogen, amino, halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, nitro or trifluoromethyl; and R11 represents a group —L1—Ar1—L2—Y; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and 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：本发明涉及式（I）的生理活性化合物：其中：R 1是氢，卤素，羟基，低级烷基或低级烷氧基; X 1，X 2和X 6独立地表示N或CR 10; X 3，X 4和X 5的一方表示CR 11，其余独立地表示N或CR 10;其中R 10为氢，氨基，卤素，羟基，低级烷基，低级烷氧基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，硝基或三氟甲基; R11表示基团-L1-Ar1-L2-Y; 和相应的N-氧化物及其前药; 和这些化合物及其N-氧化物和前药的药学上可接受的盐和溶剂化物。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。

2. 发明授权

US07227020B2 Azaindoles 有权
公开(公告)号：US07227020B2
公开(公告)日：2007-06-05
申请号：US10827978
申请日：2004-04-20
申请人： Paul Joseph Cox , Tahir Nadeem Majid , Shelley Amendola , Stephanie Daniele Deprets , Christoper David Edlin , Justine Yeun Quai Lai , Andrew David Morley
发明人： Paul Joseph Cox , Tahir Nadeem Majid , Shelley Amendola , Stephanie Daniele Deprets , Christoper David Edlin , Justine Yeun Quai Lai , Andrew David Morley
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： A61K31/4985 , A61K31/437 , C07D471/04 , C07D487/04
摘要： Chemical compositions containing physiologically active compounds of general formula (I): wherein R1 is aryl or heteroaryl; R2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z1R8, —C(═O)—NY3Y4, —CO2R8, —NY3Y4, —N(R6)—C(═O)—R7, —N(R6)—C(═O)—NY3Y4, —N(R6)—C(═O)—OR7, —N(R6)—SO2—R7, —N(R6)—SO2—NY3Y4 and one or more halogen atoms; R3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, —C(═O)—OR5 or —C(═O)—NY3Y; and X1 represents N, CH, C-halo, C—CN, C—R7, C—NY3Y4, C—OH, C-Z2R7, C—C(═O)—OR5, C—C(═O)—NY3Y4, C—N(R8)—C(═O)—R7, C—SO2—NY3Y4, C—N(R8)—SO2—R7, C-alkenyl, C-alkynyl or C—NO2; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

3. 发明授权

US06593354B2 Substituted benzoxazole compounds 有权
标题翻译：取代苯并恶唑化合物
公开(公告)号：US06593354B2
公开(公告)日：2003-07-15
申请号：US09925110
申请日：2001-08-09
申请人： David Edward Clark , Paul Robert Eastwood , Neil Victor Harris , Clive McCarthy , Andrew David Morley , Stephen Dennis Pickett
发明人： David Edward Clark , Paul Robert Eastwood , Neil Victor Harris , Clive McCarthy , Andrew David Morley , Stephen Dennis Pickett
IPC分类号： A61K31423
CPC分类号： C07D263/58 , C07D235/30
摘要： The invention is directed to physiologically active compounds of formula (Ia): wherein R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is alkylene, alkenylene or alkynylene; R5 is hydrogen or lower alkyl; L2 is optionally substituted alkylene or alkenylene; Y is carboxy; and Z1 is NR5; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and 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：本发明涉及式（Ia）的生理活性化合物：其中R 1是任选取代的芳基或任选取代的杂芳基; R2是氢，卤素，低级烷基或低级烷氧基; R3是亚烷基，亚烯基或亚炔基; R5是氢或低级烷基; L2是任选取代的亚烷基或亚烯基; Y是羧基; Z1为NR5; 和相应的N-氧化物及其前药; 和这些化合物的药学上可接受的盐和溶剂合物（例如水合物）及其N-氧化物和前药。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。

4. 发明授权

US06706738B2 Substituted bicyclic heteroaryl compounds and their use as integrin antagonists 有权
标题翻译：取代的双环杂芳基化合物及其作为整联蛋白拮抗剂的用途
公开(公告)号：US06706738B2
公开(公告)日：2004-03-16
申请号：US09975721
申请日：2001-10-11
申请人： David Edward Clark , Paul Robert Eastwood , Neil Victor Harris , Clive McCarthy , Andrew David Morley , Stephen Dennis Pickett
发明人： David Edward Clark , Paul Robert Eastwood , Neil Victor Harris , Clive McCarthy , Andrew David Morley , Stephen Dennis Pickett
IPC分类号： A61K31443
CPC分类号： C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14
摘要： The invention is directed to physiologically active compounds of general formula (I): R1Z1—Het—L1—Ar1—L2—Y (I) wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring containing at least one heteroatom selected from O, S or N; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; Z1 represents a direct bond, an alkylene chain, NR4, O or S(O)n; L1 is an a —R5—R6— linkage where R5 is alkylene, alkenylene or alkynylene and R6 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, —C(═Z3)—NR4—, —NR4—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR4)—, —NR4—, —NR4—C(═Z3)—NR4—, —SO2—NR4—, —NR4—SO2—, —O—C(═O)—, —C(═O)—O—, —NR4—C(═O)—O— or —O—C(═O)—NR4—; L2 is a direct bond; an optionally substituted alkylene, alkenylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or arylene linkage; a —[C(═O)—N(R9)—C(R4)(R10)]p— linkage; a —Z4—R11— linkage; a —C(═O)—CH2—C(═O)— linkage; a —R11—Z4—R11— linkage; or a —L3—L4—L5— linkage; and Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and 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Het是任选取代的，饱和的，部分饱和的或完全不饱和的8至10元双环，其含有至少一个选自O，S或N的杂原子; R 1是任选取代的芳基，杂芳基，烷基，烯基，炔基，环烷基或杂环烷基; Z 1表示直接键，亚烷基链，NR 4，O或S（O）n; L 1是-R 5 -R 6 - 键，其中R 5是亚烷基，亚烯基或亚炔基，R 6是直接键，亚环烷基，亚杂环亚烷基，亚芳基，杂芳基二基，-C （= Z 3）-NR 4 - ， - NR 4 -C（= Z 3） - ， - Z 3 - ， - C（= O） - ， - -NR 4 - ， - NR 4 -C（= Z 3）-NR 4 - ， - SO 2 -NR 4 - ， - NR 4 -SO 2 - ， - OC（= O） - ， - C（= O）-O-，-NR 4 -C（= O）-O-或-OC（= O）-NR 4 - L 2是直接键; 亚烯基，亚炔基，亚环烯基，亚环烷基，杂芳基二基，杂环亚烷基或亚芳基键; a - [C（= O）-N（R 9）-C（R 4）（R 10）] p - 键; a -Z 4 -R 11 - 键; -C（= O）-CH 2 -C（= O） - 键; -R 11 -Z 4 -R 11 - 键; 或-L 3 -L 4 -L 5 - 键; Y为羧基或酸式生物电子等排体; 和相应的N-氧化物及其前药; 和这些化合物的药学上可接受的盐和溶剂合物（例如水合物）及其N-氧化物和前药。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。

5. 发明授权

US06562851B2 Substituted bicyclic compounds 有权
标题翻译：取代的双环化合物
公开(公告)号：US06562851B2
公开(公告)日：2003-05-13
申请号：US10002041
申请日：2001-11-02
申请人： David Edward Clark , Paul Robert Eastwood , Neil Victor Harris , Clive McCarthy , Andrew David Morley , Stephen Dennis Pickett
发明人： David Edward Clark , Paul Robert Eastwood , Neil Victor Harris , Clive McCarthy , Andrew David Morley , Stephen Dennis Pickett
IPC分类号： A61K31423
CPC分类号： C07D263/58 , C07D235/30 , C07D413/12 , C07D413/14
摘要： The invention is directed to physiologically active compounds of general formula (I): wherein Het is 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; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; Z1 is NR5; L1 is a —R6—R7— linkage (where R6 is alkylene, alkenylene or alkynylene and R7 is a direct bond, cycloalkylene, heterocycloalkylene, aryldiyl, heteroaryldiyl, —C(═Z3)—NR5—, —NR5—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR5)—, —NR5—, —NR5—C(═Z3)—NR5—, —SO2—NR5—, —NR5—SO2—, —O—C(═O)—, —C(═O)—O—, —NR5—C(═O)—O— or —O—C(═O)—NR5—); L2 is an alkylene chain substituted by hydroxy, oxo, —OR4, —O—C(═O)—R4, —N(R8)—C(═O)—R9, —N(R8)—C(═O)—OR9, —N(R8)—SO2—R9, or —NY3Y4; and Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and 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Het是含有至少一个选自O，S或N的杂原子的任选取代的，饱和的，部分饱和的或完全不饱和的8至10元双环体系; R 1是任选取代的芳基，杂芳基，烷基，烯基，炔基，环烷基或杂环烷基; R2是氢，卤素，低级烷基或低级烷氧基; Z1是NR5; L1是-R6-R7-键（其中R6是亚烷基，亚烯基或亚炔基，R7是直接键，亚环烷基，亚杂烷基亚烷基，芳基二基，杂芳基二基，-C（= Z3）-NR5-，-NR5-C（= Z3 ） - ， - Z3 - ， - （= O） - ， - （= NOR5） - ， - NR5-，-NR5-C（= Z3）-NR5-，-SO2-NR5-，-NR5-SO2- ，-OC（= O） - ， - C（= O）-O-，-NR 5 -C（= O）-O-或-OC（= O）-NR 5 - ）; L2是被羟基，氧代，-OR4，-OC（= O）-R4，-N（R8）-C（= O）-R9，-N（R8）-C（= O）-OR9取代的亚烷基链，-N（R 8）-SO 2 -R 9或-NY 3 Y 4; Y为羧基或酸式生物电子等排体; 和相应的N-氧化物及其前药; 和这些化合物及其N-氧化物和前药的药学上可接受的盐和溶剂化物。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。

6. 发明授权

US06352977B1 Substituted &bgr;-alanines 有权
标题翻译：取代的β-丙氨酸
公开(公告)号：US06352977B1
公开(公告)日：2002-03-05
申请号：US09589825
申请日：2000-06-08
申请人： Peter Charles Astles , Neil Victor Harris , Andrew David Morley
发明人： Peter Charles Astles , Neil Victor Harris , Andrew David Morley
IPC分类号： C07C27542
CPC分类号： C07D207/27 , C07C275/42
摘要： The invention is directed to physiologically active compounds of general formula (I): wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR2; and one of X3, X4 and X5 represents CR3 and the others independently represents N or CR2 where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group —L1—(CH2)n—C(═O)—N(R4)—CH2—CH2—Y; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their 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是氢，卤素，低级烷基或低级烷氧基; X1，X2和X6独立地表示N或CR2; X 3，X 4和X 5中的一个表示CR 3，其余的独立地表示N或CR 2，其中R 2为氢，卤素，低级烷基或低级烷氧基; 并且R 3表示基团-L 1 - （CH 2）n -C（= O）-N（R 4）-CH 2 -CH 2 -Y; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物。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。

7. 发明授权

US07276517B2 Heterocyclic amide derivatives as inhibitors of glycogen phosphorylase 失效
标题翻译：杂环酰胺衍生物作为糖原磷酸化酶的抑制剂
公开(公告)号：US07276517B2
公开(公告)日：2007-10-02
申请号：US11463144
申请日：2006-08-08
申请人： Alan Martin Birch , Andrew David Morley , Andrew Stocker , Paul Robert Owen Whittamore
发明人： Alan Martin Birch , Andrew David Morley , Andrew Stocker , Paul Robert Owen Whittamore
IPC分类号： A61K31/4375 , C07D471/04
CPC分类号： C07D495/04
摘要： Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof, possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的杂环酰胺其中：X是N或CH; R 4和R 5一起是-SC（R 6）-C（R 7） - 或 -C（R 7）C（R 6）-S-; R 6和R 7独立地选自，例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代）组）; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10）），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR ^{9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前药具有糖原磷酸化酶抑制活性，因此在治疗与增加的糖原磷酸化酶活性相关的疾病状态方面具有价值。描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。}

8. 发明授权

US07572826B2 Thiophene-carboxamide derivatives and their use as inhibitors of the enzyme IKK-2 失效
标题翻译：噻吩 - 甲酰胺衍生物及其作为IKK-2酶抑制剂的用途
公开(公告)号：US07572826B2
公开(公告)日：2009-08-11
申请号：US10542326
申请日：2004-01-13
申请人： Alan Wellington Faull , Craig Johnstone , Andrew David Morley , Jeffrey Philip Poyser
发明人： Alan Wellington Faull , Craig Johnstone , Andrew David Morley , Jeffrey Philip Poyser
IPC分类号： A61K31/381 , C07D333/36
CPC分类号： C07D409/12 , C07D333/38 , C07D333/44 , C07D413/12
摘要： The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明涉及式（I）的噻吩甲酰胺，其中A，R 1，R 2，R 3，R 4，R 5和X如说明书中所定义，其制备中使用的方法和中间体，含有它们的药物组合物及其在治疗中的用途。

9. 发明授权

US07169927B2 Indole-amide derivatives and their use as glycogen phosphorylase inhibitors 失效
标题翻译：吲哚酰胺衍生物及其作为糖原磷酸化酶抑制剂的用途
公开(公告)号：US07169927B2
公开(公告)日：2007-01-30
申请号：US10506748
申请日：2003-03-04
申请人： Alan Martin Birch , Andrew David Morley
发明人： Alan Martin Birch , Andrew David Morley
IPC分类号： C07D215/38 , C07D217/02
CPC分类号： C07D401/12 , C07D401/14 , C07D417/14
摘要： Heterocyclic amides of formula (1) wherein: is a single or double bond; A is phenylene or heteroarylene; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的杂环酰胺其中：是单键或双键; A是亚苯基或亚杂芳基; m为0,1或2; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代）组）; R 4独立地选自例如氢，卤素，硝基，氰基，羟基，C 1-4烷基和C 1-4烷基。烷酰基; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10）），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR ^{9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。}

10. 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。

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