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1. 发明申请

WO1996013479A1 NITRO-BENZAMIDES USEFUL AS ANTI-ARRHYTHMIC AGENTS 审中-公开
标题翻译：硝基苯甲酮有效用作抗神经药物
公开(公告)号：WO1996013479A1
公开(公告)日：1996-05-09
申请号：PCT/EP1995004203
申请日：1995-10-24
申请人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES , NADLER, Guy, Marguerite, Marie, Gérard , MARTIN, Michel, Jean, Roger
发明人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES
IPC分类号： C07C233/78
CPC分类号： C07C233/78
摘要： A compound of formula (I), or a salt thereof, or a solvate thereof, wherein Ar represents substituted or unsubstituted aryl, wherein the optional substituents are selected from alkyl, hydroxy or alkoxy or, if attached to adjacent carbon atoms any two substituents together with the carbon atoms to which they are attached may form a fused heterocyclic ring of five to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; A represents a C1-4n-alkylene group wherein each carbon is optionally substituted by 1 or 2 C1-6alkyl groups; R1 represents hydrogen, alkyl, alkenyl or cycloalkyl; one or two of the group of R2, R3 and R4 represents nitro the remaining members of the group of R2, R3 and R4 represent hydrogen; X represents a -CO-NH- moiety; and Z represents C2-4n-alkylene group wherein each carbon is optionally substituted 1 or 2 C1-6alkyl groups; a process for preparing such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其盐或其溶剂合物，其中Ar表示取代或未取代的芳基，其中任选的取代基选自烷基，羟基或烷氧基，或者如果连接到相邻的碳原子上，则任意两个取代基在一起与它们所连接的碳原子可以形成五至六个原子的稠合杂环，其中一个，两个或三个所述原子是氧或氮; A表示C 1-4亚烷基，其中每个碳任选被1或2个C 1-6烷基取代; R1代表氢，烷基，烯基或环烷基; R 2，R 3和R 4中的一个或两个表示硝基，R 2，R 3和R 4中的剩余成员表示氢; X表示-CO-NH-部分; Z表示C2-4n亚烷基，其中每个碳任选被1或2个C 1-6烷基取代; 制备这种化合物的方法，包含这些化合物的药物组合物和这些化合物在医药中的用途。

2. 发明申请

WO1995007884A1 ALKANEDIAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF ARRHYTHMIC AND ISCHAEMIC RHYTHM DISORDERS 审中-公开
标题翻译：阿卡蜜胺衍生物及其在治疗ARHHTHTHMIC和ISCHEMY RHYTHM病症中的应用
公开(公告)号：WO1995007884A1
公开(公告)日：1995-03-23
申请号：PCT/EP1994002959
申请日：1994-09-05
申请人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES , NADLER, Guy, Marguerite, Marie, Gérard , MARTIN, Michel, Jean, Roger
发明人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES
IPC分类号： C07C311/08
CPC分类号： C07D231/12 , C07C217/84 , C07C237/42 , C07C311/08 , C07C311/44 , C07D233/56 , C07D249/08
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein A and B each independently represents a C1-4 n-alkylene group wherein each carbon is optionally substituted by a C1-6 alkyl group; D represents CO, SO2, NH-CO or CH2CO; T represents hydrogen, alkyl, alkenyl or cycloalkyl; Z represents a bond, CH2, (CH2)2 or X-CH2-CH2 wherein X represents O or S; R1, R2 and R3 each independently represents H, alkyl, OH or alkoxy or, if attached to adjacent carbon atoms, any two of R1, R2 and R3 together with the carbon atoms to which they are attached may form a fused heterocyclic ring of five to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; R4 represents alkylsulphonamido, alkylamido or imidazo; and Ar represents substituted or unsubstituted aryl, wherein the optional substituents are the above defined R1, R2 and R3; a composition containing such a compound, a process for the preparation of such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物或其盐或其溶剂化物，其中A和B各自独立地表示碳原子数为1〜6的亚烷基，其中各碳任选被C 1-6烷基取代; D表示CO，SO 2，NH-CO或CH 2 CO; T代表氢，烷基，烯基或环烷基; Z表示键，CH 2，（CH 2）2或X-CH 2 -CH 2，其中X表示O或S; R 1，R 2和R 3各自独立地表示H，烷基，OH或烷氧基，或者如果连接到相邻的碳原子上，R 1，R 2和R 3中的任何两个与它们所连接的碳原子一起可以形成五个稠合杂环至六个原子，其中一个，两个或三个所述原子是氧或氮; R4代表烷基磺酰氨基，烷基酰氨基或咪唑; 并且Ar表示取代或未取代的芳基，其中任选的取代基是上述定义的R 1，R 2和R 3; 含有这种化合物的组合物，制备这种化合物的方法和这种化合物在医药中的用途。

3. 发明申请

WO1998001436A1 HETEROAROMATIC PENTADIENOIC ACID DERIVATIVES USEFUL AS INHIBITORS OF BONE RESORPTION 审中-公开
标题翻译：作为骨骼受体抑制剂的异氟醚酸衍生物
公开(公告)号：WO1998001436A1
公开(公告)日：1998-01-15
申请号：PCT/EP1997003709
申请日：1997-07-07
申请人： SMITHKLINE BEECHAM S.P.A. , SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES , FARINA, Carlo , GAGLIARDI, Stefania , NADLER, Guy, Marguerite, Marie, Gerard , MARTIN, Michel, Jean, Roger
发明人： SMITHKLINE BEECHAM S.P.A. , SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES
IPC分类号： C07D307/80
CPC分类号： C07D405/06 , C07D215/12 , C07D307/80 , C07D333/60 , C07D409/06
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein: R1 represents an alkyl group or a substituted or unsubstituted aryl group; R2, R3 and R4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R5 and R6 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R5 and R6 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; X represents a hydroxy or an alkoxy group wherein the alkyl group may be substituted or unsubstituted or X represents a group NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclic group; and Y represents O or S and Z represents CH, CH=CH or N; or Y represents NR7 wherein R7 represents hydrogen, hydroxy, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or aminosulphonyl and Z represents CH=CH or N; a pharmaceutical composition containing such a compound, a process for preparing such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物或其盐或其溶剂合物，其中：R1表示烷基或取代或未取代的芳基; R2，R3和R4各自独立地表示氢，烷基，芳基或取代的芳基; R5和R6各自独立地表示氢，羟基，氨基，烷氧基，任选取代的芳氧基，任选取代的苄氧基，烷基氨基，二烷基氨基，卤素，三氟甲基，三氟甲氧基，硝基，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基或R5和R6一起代表亚甲二氧基，羰基二氧基或羰基二氨基; X表示羟基或烷氧基，其中烷基可以是取代或未取代的或X表示基团NRsRt，其中R 5和R 5各自独立地表示氢，烷基，取代的烷基，任选取代的烯基，任选取代的芳基，任选取代的芳基烷基，任选取代的杂环基或任选取代的杂环基烷基，或R 5和R 5与它们所连接的氮一起形成杂环基; Y表示O或S，Z表示CH，CH = CH或N; 或Y表示NR7，其中R7表示氢，羟基，烷酰基，烷基，氨基烷基，羟基烷基，羧基烷基，碳烷氧基烷基，氨基甲酰基或氨基磺酰基，Z表示CH = CH或N; 含有这种化合物的药物组合物，这种化合物的制备方法和这种化合物在医药中的应用。

4. 发明申请

WO1994027971A1 ANTI-ARRHYTHMIC N-SUBSTITUTED 3-BENZAZEPINES OR ISOQUINOLINES 审中-公开
标题翻译：抗坏血酸N-取代的3-苯并嗪或异喹啉
公开(公告)号：WO1994027971A1
公开(公告)日：1994-12-08
申请号：PCT/EP1994001705
申请日：1994-05-24
申请人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES , NADLER, Guy, Marguerite, Marie, Gérard , MARTIN, Michel, Jean, Roger
发明人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , C07D217/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07F9/6558
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein A represents CH2, (CH2)2, CO, COCH2, CH2CO, CSCH2 or CH=CH; B represents CH2 or CO; Z represents a bond, CH2, (CH2)2 or X-CH2-CH2 wherein X represents O or S; D represents CO, SO2, NH-CO, NH-SO2, CH=CH or P(O)OR6 wherein R6 is C1-6 alkyl; Q represents aryl, aralkyl, aralkenyl or aralkynyl, wherein the aryl moiety may be substituted or unsubstituted with 1 to 5 substituents selected from the list consisting of nitro, halogen, alkylsulfonamide, amino, 1-imidazo, alkyl or haloalkyl, or Q represents substituted or unsubstituted: furanyl, pyranyl, thienyl, thiazolyl, imidazolyl, triazolyl or the benzo fused equivalents of furanyl, pyranyl, thienyl, thiazolyl, imidazolyl or triazolyl, indolyl, oxoindolyl, indenyl, isoindenyl, indazolyl, indolizinyl or pyridinyl or cycloalkyl optionally fused to an aryl group; R1, R2, R3, R4 and R5 each independently represent H, alkyl, OH or alkoxy or, if attached to adjacent carbon atoms, any two of R1, R2, R3, R4 and R5 together with the carbon atoms to which they are attached may form a fused heterocyclic ring of four to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; and E represents C2-4 n-alkylene group wherein each carbon is optionally substituted by R6; a process for preparing such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其盐或其溶剂化物，其中A表示CH 2，（CH 2）2，CO，COCH 2，CH 2 CO，CSCH 2或CH = CH; B表示CH 2或CO; Z表示键，CH 2，（CH 2）2或X-CH 2 -CH 2，其中X表示O或S; D表示CO，SO 2，NH-CO，NH-SO 2，CH = CH或P（O）OR 6，其中R 6是C 1-6烷基; Q表示芳基，芳烷基，芳烯基或芳炔基，其中芳基部分可以被1至5个选自硝基，卤素，烷基磺酰胺，氨基，1-咪唑基，烷基或卤代烷基的取代基取代或未取代，或Q表示取代的或未取代的：呋喃基，吡喃基，噻吩基，噻唑基，咪唑基，三唑基或呋喃基，吡喃基，噻吩基，噻唑基，咪唑基或三唑基的苯并稠合当量，吲哚基，氧代吲哚基，茚基，异茚基，吲唑基，中氮茚基或吡啶基或环烷基，芳基; R 1，R 2，R 3，R 4和R 5各自独立地表示H，烷基，OH或烷氧基，或者如果连接到相邻碳原子上，则R 1，R 2，R 3，R 4和R 5中的任何两个与它们所连接的碳原子一起可以形成四至六个原子的稠合杂环，其中一个，两个或三个所述原子是氧或氮; 并且E表示其中每个碳任选被R 6取代的C 2-4的亚烷基; 制备这种化合物的方法，包含这些化合物的药物组合物和这些化合物在医药中的用途。

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