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1. 发明公开

EP0196184A3 New aryl derivatives 失效
标题翻译：新的ARYL DERIVATIVES
公开(公告)号：EP0196184A3
公开(公告)日：1988-04-20
申请号：EP86301895
申请日：1986-03-14
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： Kneen, Geoffrey , Jackson, William Paul , Islip, Peter John , Wates, Peter John
IPC分类号： C07C83/10 , C07C127/00 , C07C125/065 , C07D521/00 , A61K31/16 , A61K31/33
CPC分类号： C07D213/30 , A01N3/00 , A01N3/02 , C07C275/64 , C07D207/46 , C07D213/42 , C07D213/64 , C07D213/643 , C07D233/38 , C07D279/12 , C07D333/20 , C07D333/32 , C07D333/38 , C07D401/04 , C07D401/06
摘要： Novel compounds of formula (I)
wherein:-
k,p and q are independently 0 or 1, provided that when k is 1 then p must also be 1; Ar represents either:
(i) naphthyl, tetrahydronaphthyl or pyridyl, any of which is optionally substituted by one or more substituents independently selected from C 1-4 alkyl (which may itself optionally be substituted by one or more halogen atoms); C 1-4 alkoxy, halo, nitro, amino, carboxy, C 1-4 alkoxycarbonyl and hydroxy, or (ii) phenyl optionally substituted by one or more substituents independently selected from phenyl (optionally substituted by one or more substituents independently selected from those specified as optional substituents in (i) above) and said optional substituents specified in (i) above; L is selected from -(CH 2 ) r -(where r is 1-4), -0-, -CH 2 0-, -CH2S-, -OCH2-, -CONH-, -NHCO-, -CO-and -CH 2 NH-, and, Ar' represents phenylene, thienylene or pyridylene, any of which may be optionally substituted by one or more substituents independently selected from those specified as optional substituents in definition (i) of Ar; X represents oxygen, sulphur or carbonyl, provided that at least one atom separates said carbonyl group from any carbonyl group in Q as defined below; Y is C 1-10 alkylene or C 1-10 alkenylene; Q represents a non-cyclic moiety selected from groups of formula in which one of m and n is 0 and the other is 1, and when n is 1 and m is 0, R 1 and R 2 are independently selected from hydrogen and C 1-4 alkyl, with the possibility that R 2 can also be G 5-7 cycloalkyl, or when n is 0 and m is 1, R 1 is independently selected from hydrogen, C 1-4 alkyl, groups as defined for Ar above and groups of formula -COR 3 in which R 3 is selected from C 1-4 alkyl (optionally substituted by a carboxy or C 1-4 atkoxycarbonyl group) and groups of formula -N(R 4 )R 5 in which R 4 is hydrogen or C 1 - 4 alkyl and R 5 represents hydrogen C 1-4 alkyl or phenyl optionally substituted by one or more substituents independently selected from those specified as optional substituents in the definition (i) of Ar, and R 2 is selected from hydrogen, C 1-4 alkyl, amino, C 1-4 alkylamino, di-C 1-4 alkylamino, C 5-7 cycloalkylamino, C 5-7 cycloalkyl (C 1-4 alkyl) amino, anilino, N-C 1-4 alkylanilino and groups as defined for Ar above; or Q represents a cyclic moiety selected from 1-hydroxy-1,3-dihydro-imidazol-2-one and groups of formula
in which Z represents a C 2 . 5 alkylene chain in which one of the carbon atoms may be replaced by a hetero atom; and salts thereof; with the proviso that- when q is 0, k is 0 or 1 and p is 1, Ar is phenyl or naphthyl, either being optionally substituted by one or more substituents as specified in definition (i) of Ar, and X is oxygen or sulphur (in the case when k is 1) Y is C 1-10 alkylene and Q represents said non-cyclic moiety as hereinbefore defined in which one of R' and R 2 is hydrogen or C 1 -4 alkyl; then the other of R' and R 2 is neither hydrogen nor C 1-4 alkyl. Also described are their preparation, compositions containing them and their use.

2. 发明授权

EP0370740B1 Anti-atherosclerotic diaryl compounds 失效
标题翻译：抗神经毒素二元化合物
公开(公告)号：EP0370740B1
公开(公告)日：1992-07-29
申请号：EP89312025.3
申请日：1989-11-20
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： Jackson, William Paul , Harris, Clifford John , Arrowsmith, Richard James , Dann, John Gordon , O'Connor, Kevin Julian , Booth, Robert Frederick Geoffrey
IPC分类号： C07C275/28 , C07C233/07 , C07C327/44 , C07C271/44 , C07C279/28 , A61K31/17 , A61K31/27 , A61K31/165 , A61K31/155
CPC分类号： C07C275/24 , C07C233/07 , C07C233/11 , C07C271/44 , C07C275/28 , C07C275/30 , C07C279/28 , C07C327/44 , C07C2601/14

3. 发明授权

EP0299761B1 Anti-inflammatory aryl derivatives 失效
标题翻译：抗炎ARYL衍生物
公开(公告)号：EP0299761B1
公开(公告)日：1991-12-18
申请号：EP88306446.1
申请日：1988-07-14
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： Salmon, John Anthony , Jackson, William Paul
IPC分类号： C07C259/06 , A61K31/16 , A01N3/00 , A01N37/28
CPC分类号： A61K31/185 , A01N37/28

4. 发明公开

EP0370740A1 Anti-atherosclerotic diaryl compounds 失效
标题翻译：二芳基化合物作为抗动脉粥样硬化剂。
公开(公告)号：EP0370740A1
公开(公告)日：1990-05-30
申请号：EP89312025.3
申请日：1989-11-20
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： Jackson, William Paul , Harris, Clifford John , Arrowsmith, Richard James , Dann, John Gordon , O'Connor, Kevin Julian , Booth, Robert Frederick Geoffrey
IPC分类号： C07C275/28 , C07C233/07 , C07C327/44 , C07C271/44 , C07C279/28 , A61K31/17 , A61K31/27 , A61K31/165 , A61K31/155
CPC分类号： C07C275/24 , C07C233/07 , C07C233/11 , C07C271/44 , C07C275/28 , C07C275/30 , C07C279/28 , C07C327/44 , C07C2601/14
摘要： The present invention is concerned with compounds of formula (I)
wherein

m is 0 or 1;
W is hydrogen, a C 1-16 straight, branched, or cyclic alkyl group, or a C 2 -16 straight, branched, or cyclic alkenyl or alkynyl group, or
Ph(CH 2 ) n - where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C 1 - 4 alkoxy and C 1 - 4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, or
R 1 NHCO- where R 1 is hydrogen or a C 1-6 alkyl group, or
R 2 CONH- where R 2 is hydrogen or a C 1-6 alkyl group;
X is -(CH 2 ) P NHCO H,
where p is an integer of from 0 to 2, -NHCONH H 2 ,
-CO H, -NHCO H 2 , -NHCO ,
-CS H, -NHCS H, -NHC(:NH) H,
-NHC(:NCN) H, -NHC(:CHCN) H,
-NHC(:CHN0 2 ) H, or -CH(A)CO H
where A is halogen;
Y is -(CH 2 ) q , where q is an integer of from 1 to 3, or -CH = CH- (E or Z);
Z is a C 1 - 6 alkyl group optionally substituted by one or more independently selected polar groups; and ring A is optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C 1 -4 alkoxy and C 1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen;
provided said compound of formula (I) is not N-{2-[(4-methylphenyl)methyl]phenyl}acetamide or α-(p-tolyl)-o-cresol carbanilate;
and salts, solvates and physiologically functional derivatives thereof, processes for the preparation of these compounds, pharmaceutical formulations containing them and their use in medicine.

5. 发明授权

EP0450660B1 Anti-atherosclerotic diaryl compound 失效
标题翻译：二芳基化合物作为抗动脉粥样硬化剂。
公开(公告)号：EP0450660B1
公开(公告)日：1994-03-09
申请号：EP91107475.5
申请日：1989-11-20
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： Jackson, William Paul , Harris, Clifford John , Arrowsmith, Richard James , Dann, John Gordon , O'Connor, Kevin Julian , Booth, Robert Frederick Geoffrey
IPC分类号： C07C275/30 , A61K31/17
CPC分类号： C07C275/24 , C07C233/07 , C07C233/11 , C07C271/44 , C07C275/28 , C07C275/30 , C07C279/28 , C07C327/44 , C07C2601/14

6. 发明授权

EP0384594B1 Anti-inflammatory aryl derivatives 失效
标题翻译：抗炎芳基衍生物。
公开(公告)号：EP0384594B1
公开(公告)日：1993-10-27
申请号：EP90301090.8
申请日：1990-02-02
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： Jackson, William Paul , Salmon, John Anthony
IPC分类号： C07C275/64 , A61K31/17
CPC分类号： C07C275/64

7. 发明公开

EP0450660A1 Anti-atherosclerotic diaryl compound 失效
标题翻译： Diarylverbindungen als antiatherosklerotische Mittel。
公开(公告)号：EP0450660A1
公开(公告)日：1991-10-09
申请号：EP91107475.5
申请日：1989-11-20
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： Jackson, William Paul , Harris, Clifford John , Arrowsmith, Richard James , Dann, John Gordon , O'Connor, Kevin Julian , Booth, Robert Frederick Geoffrey
IPC分类号： C07C275/30 , A61K31/17
CPC分类号： C07C275/24 , C07C233/07 , C07C233/11 , C07C271/44 , C07C275/28 , C07C275/30 , C07C279/28 , C07C327/44 , C07C2601/14
摘要： The present invention is concerned with the compound of formula (I)

and salts, solvates and physiologically functional derivatives thereof, processes for the preparation of this compound, pharmaceutical formulations containing it and their use in medicine.
摘要翻译：本发明涉及式（I）化合物，其中m为0或1; W是氢，C1-16直链，支链或环状烷基或C2-16直链，支链或环状烯基或炔基或Ph（CH2）n-，其中Ph是苯基，n是整数 0至2，苯基任选被一个或多个独立地选自卤素，羟基，硝基，C 1-4烷氧基和C 1-4烷基的一个或多个原子或基团取代，其中所述烷基中的一个或多个氢原子是任选的被卤素取代，或R 1 NHCO-，其中R 1是氢或C 1-6烷基，或R 2 CONH-，其中R 2是氢或C 1-6烷基; X是 - （CH 2）p NHCO @ H，其中p是0-2的整数，-NHCONH 2 H 2，-CO 2 H，-NHCO 2 H 2，-NHCO 2，-CS 2 H，-NHCS H， -NHC（：NH）@ H，-NHC（：NCN）@H，-NHC（：CHCN）@H，-NHC（：CHNO 2）@H或-CH（A）CO 2 H，其中A是卤素; Y是 - （CH 2）q，其中q是1至3的整数，或-CH = CH-（E或Z）; Z是任选被一个或多个独立选择的极性基团取代的C 1-6烷基; 环A任选被一个或多个独立地选自卤素，羟基，硝基，C 1-4烷氧基和C 1-4烷基的原子或基团取代，其中所述烷基中的一个或多个氢原子任选被卤素取代; 所述式（I）化合物不是N- {2 - [（4-甲基苯基）甲基]苯基}乙酰胺或α-（对甲苯基） - 邻甲酚氨基苯甲酸酯; 及其盐，溶剂合物及其生理功能衍生物，制备这些化合物的方法，含有它们的药物制剂及其在药物中的用途。

8. 发明公开

EP0351214A1 Anti-inflammatory aryl derivatives 失效
标题翻译：抗炎芳基衍生物
公开(公告)号：EP0351214A1
公开(公告)日：1990-01-17
申请号：EP89307096.1
申请日：1989-07-13
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： Jackson, William Paul , Salmon, John Anthony
IPC分类号： C07C259/06 , A61K31/16
CPC分类号： C07C259/06
摘要： The present invention is concerned with (E)-N-{1(S)-methyl-3-[3-(4-fluorophenoxy)phenyl]prop-2-en-1-yl}acetohydroxamic acid and salts thereof, pharmaceutical formulations containing them, processes for their preparation, and uses for them in medicine and other applications.
摘要翻译：本发明涉及（E）-N- {1（S） - 甲基-3- [3-（4-氟苯氧基）苯基]丙-2-烯-1-基}乙氧肟酸及其盐，药物制剂含有它们，它们的制备过程，以及它们在医学和其他应用中的用途。

9. 发明授权

EP0196184B1 Aryl derivatives 失效
标题翻译： ARYL衍生物
公开(公告)号：EP0196184B1
公开(公告)日：1992-09-16
申请号：EP86301895.8
申请日：1986-03-14
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： Kneen, Geoffrey , Jackson, William Paul , Islip, Peter John , Wates, Peter John
IPC分类号： C07C271/02 , C07C271/06 , C07D213/00 , A61K31/16 , A61K31/33
CPC分类号： C07D213/30 , A01N3/00 , A01N3/02 , C07C275/64 , C07D207/46 , C07D213/42 , C07D213/64 , C07D213/643 , C07D233/38 , C07D279/12 , C07D333/20 , C07D333/32 , C07D333/38 , C07D401/04 , C07D401/06

10. 发明公开

EP0384594A1 Anti-inflammatory aryl derivatives 失效
标题翻译： EntzündungshemmendeArylderivate。
公开(公告)号：EP0384594A1
公开(公告)日：1990-08-29
申请号：EP90301090.8
申请日：1990-02-02
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： Jackson, William Paul , Salmon, John Anthony
IPC分类号： C07C275/64 , A61K31/17
CPC分类号： C07C275/64
摘要： The present inventions concerned with compounds of formula (I)
wherein
Ar is 4-halophenyl;
Ar′ is 1,3- or 1,4-phenylene;
Y is (E)-CH=CH-; and
R¹ and R² are independently selected from hydrogen and C 1-4 alkyl;
and base salts and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and, optionally, one or more other pharmacologically active ingredients and the use of these compounds in medicine.
摘要翻译：本发明涉及式（I）化合物，其中Ar是4-卤代苯基; Ar min为1,3-或1,4-亚苯基; Y为（E）-CH = CH-; R 1和R 2独立地选自氢和C 1-4烷基; 其碱盐和生理功能衍生物，其制备方法，含有它们的药物制剂和任选的一种或多种其它药理学活性成分以及这些化合物在医药中的用途。

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