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1. 发明申请

WO1998022480A1 PHOSPHORUS CONTAINING ARYLOXY OR ARYLTHIO PROPANOLAMINE DERIVATIVES 审中-公开
标题翻译：含有ARYLOXY或ARYLTHIO丙酰胺衍生物的磷
公开(公告)号：WO1998022480A1
公开(公告)日：1998-05-28
申请号：PCT/GB1997003131
申请日：1997-11-13
申请人： SMITHKLINE BEECHAM PLC , BEELEY, Lee, James , BERGE, John, Michael , DEAN, David, Kenneth , RAMI, Harshad, Kantilal
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07F09/30
CPC分类号： C07F9/657181 , C07F9/301 , C07F9/3211 , C07F9/4006
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein, R represents an aryl group optionally substituted with one, two or three substituents selected from the list consisting of: hydroxy, hydroxymethyl, nitro, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, formamido, halogen, alkoxy and allyl; X represents O or S; R and R each independently represents hydrogen or an alkyl group or R together with R and the carbon atom to which they are attached represent a cycloalkyl group; R represents a moiety of formula (a), wherein R represents hydrogen, alkyl, hydroxyalkyl, arylalkyl, aryloxyalkyl, aralkyloxyalkyl or cycloalkyl and R represents hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, aryloxyalkyloxy, arylalkoxyalkyloxy or cycloalkyloxy or R represents hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, aryloxyalkyl, arylalkyloxyalkyl or R together with OR represents O(CH2)nO wherein n is 2, 3 or 4; and R and R each independently represents halogen, hydrogen, alkyl or alkoxy; a process for the preparation of such compounds, a pharmaceutical composition comprising such compounds and the use of such a compound or composition in medicine.
摘要翻译：式（I）化合物或其盐或其溶剂合物，其中R 0表示任选被一个，两个或三个选自以下的取代基取代的芳基：羟基，羟甲基，硝基，氨基，烷基氨基，二烷基氨基，烷基磺酰氨基，芳基磺酰氨基，甲酰氨基，卤素，烷氧基和烯丙基; X表示O或S; R 1和R 1a各自独立地表示氢或烷基或R 1与R 1a一起，并且它们所连接的碳原子表示环烷基; R 2表示式（a）的部分，其中R 4表示氢，烷基，羟烷基，芳烷基，芳氧基烷基，芳烷氧基烷基或环烷基，R 5表示羟基，烷氧基，芳基烷氧基，羟基烷氧基，烷氧基烷氧基，芳氧基烷氧基，芳基烷氧基或环烷氧基或R 5表示氢，烷基，取代的烷基，环烷基，芳基，芳基烷基，芳氧基烷基，芳基烷氧基烷基或芳基烷氧基烷基或R 5与OR 4一起代表O（CH 2）n O，其中n为2,3或4 ; R 3和R 3a各自独立地表示卤素，氢，烷基或烷氧基; 制备这些化合物的方法，包含这些化合物的药物组合物和这种化合物或组合物在医药中的用途。

2. 发明申请

WO1996004233A1 ARYLOXY AND ARYLTHIOPROPANOLAMINE DERIVATIVES USEFUL AS BETA 3-ADRENORECEPTOR AGONISTS AND ANTAGONISTS OF THE BETA 1 AND BETA 2-ADRENORECEPTORS AND PHARMACEUTICAL COMPOSITION THEREOF 审中-公开
标题翻译：有利于ARALOXY和ARYLROPOPOLOLOLINE衍生物作为β-3受体激动剂和β1和β-2-肾上腺素受体拮抗剂及其药物组合物
公开(公告)号：WO1996004233A1
公开(公告)日：1996-02-15
申请号：PCT/EP1995003037
申请日：1995-07-27
申请人： SMITHKLINE BEECHAM PLC , BEELEY, Lee, James , THOMPSON, Mervyn , DEAN, David, Kenneth , KOTECHA, Nikesh, Rasiklal , BERGE, John, Michael , WARD, Robert, William
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07C217/60
CPC分类号： C07F9/3211 , C07C217/34 , C07C2601/14 , C07D317/46 , C07F9/301 , C07F9/303 , C07F9/3223 , C07F9/4006
摘要： A compound formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein R represents an aryl group optionally substituted with one, two or three substituents selected from the list consisting of: hydroxy, hydroxymethyl, nitro, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, formamido, halogen, alkoxy and allyl; X represents O or S; R and R each independently represents hydrogen or an alkyl group; R represents OCH2CO2H, or an ester or amide thereof, or R represents a moiety of formula (b), wherein R represents hydrogen, alkyl, hydroxyalkyl, arylalkyl, aryloxyalkyl, aralkyloxyalkyl or cycloalkyl and R represents hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, aryloxyalkyloxy, arylalkoxyalkyloxy or cycloalkyloxy or R represents hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, aryloxyalkyl, arylalkyloxyalkyl or R together with OR represents O(CH2)nO, wherein n is 2, 3 or 4; and R represents hydrogen, halogen, alkyl or alkoxy or R together with R represents a moiety of formula (c) or an ester or amide thereof; providing that 4-[2-[2-hydroxy-3-(4-hydroxyphenoxy)propylamino]propyl]phenoxyacetic acid and salts and esters thereof and the compounds of examples 1 to 36 disclosed in EP0328251 are excluded from the scope of formula (I); a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物或其药学上可接受的盐或其药学上可接受的溶剂合物，其中R 0表示任选被1,2或3个选自羟基，羟甲基，硝基的取代基取代的芳基，氨基，烷基氨基，二烷基氨基，烷基磺酰氨基，芳基磺酰氨基，甲酰氨基，卤素，烷氧基和烯丙基; X表示O或S; R 1和R 1a各自独立地表示氢或烷基; R 2表示OCH 2 CO 2 H或其酯或酰胺，或R 2表示式（b）的部分，其中R 4表示氢，烷基，羟烷基，芳烷基，芳氧基烷基，芳烷氧基烷基或环烷基， R 5代表羟基，烷氧基，芳基烷氧基，羟基烷氧基，烷氧基烷氧基，芳氧基烷氧基，芳基烷氧基氧基或环烷氧基或R 5表示氢，烷基，取代烷基，环烷基，芳基，芳基烷基，芳氧基烷基，芳基烷氧基烷基或R 5与OR 4 >表示O（CH 2）n O，其中n为2,3或4; 和R 3代表氢，卤素，烷基或烷氧基或R 3与R 2一起代表式（c）的部分或其酯或酰胺; 提供4- [2- [2-羟基-3-（4-羟基苯氧基）丙基氨基]丙基]苯氧基乙酸及其盐和酯以及EP0328251中公开的实施例1至36的化合物不包括在式（I ）; 含有这种化合物的药物组合物，制备这种化合物的方法以及这种化合物在医药中的用途。

3. 发明申请

WO1996004234A1 ARYLOXY ANDARYCTHIO PROPANOLAMINE DERIVATIVES USEFUL AS B3-ADRENORECEPTOR AGONISTS AND ANTAGONS OF THE B1 AND B2 ADRENORECEPTORS AND PHARMACEUTICAL COMPOSITION THEREOF 审中-公开
标题翻译：用于B3和ADBENORECEPTOR激动剂的ARYLOXY ANDARYCTHIO丙酰胺衍生物和B1和B2受体的拮抗剂及其药物组合物
公开(公告)号：WO1996004234A1
公开(公告)日：1996-02-15
申请号：PCT/GB1995001325
申请日：1995-06-07
申请人： SMITHKLINE BEECHAM PLC , BEELEY, Lee, James , THOMPSON, Mervyn , DEAN, David, Kenneth , KOTECHA, Nikesh, Rasiklal , BERGE, John, Michael , WARD, Robert, William
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07C217/60
CPC分类号： C07F9/3211 , C07C217/34 , C07C2601/14 , C07D317/46 , C07F9/301 , C07F9/303 , C07F9/3223 , C07F9/4006
摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein, R represents an aryl group optionally substituted with one, two or three substituents selected from the list consisting of: hydroxy, hydroxymethyl, nitro, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, formamido, halogen, alkoxy and allyl; X represents O or S; R and R each independently represents hydrogen or an alkyl group; R represents OCH2CO2H, or an ester or amide thereof, or R represents a moiety of formula (b) wherein R represents hydrogen, alkyl, hydroxyalkyl, arylalkyl, aralkyloxyalkyl or cycloalkyl and R represents hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, arylalkoxyalkyloxy or cycloalkyloxy or R represents hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, arylalkyloxyalkyl or R together with OR represents O(CH2)nO wherein n is 2, 3 or 4; and R represents hydrogen, halogen, alkyl or alkoxy or R together with R represents a moiety of formula (c) or an ester or amide thereof; providing that 4-[2-[2-hydroxy-3-(4-hydroxyphenoxy)propylamino]propyl] phenoxyacetic acid and salts and esters thereof and the examples disclosed in EP0328251 are excluded from the scope of formula (I); a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物或其药学上可接受的盐或其药学上可接受的溶剂合物，其中R 0表示任选被一个，两个或三个选自以下的取代基取代的芳基：羟基，羟甲基，硝基，氨基，烷基氨基，二烷基氨基，烷基磺酰氨基，芳基磺酰氨基，甲酰氨基，卤素，烷氧基和烯丙基; X表示O或S; R 1和R 1a各自独立地表示氢或烷基; R 2表示OCH 2 CO 2 H或其酯或酰胺，或R 2表示式（b）的部分，其中R 4表示氢，烷基，羟烷基，芳烷基，芳烷氧基烷基或环烷基，R 5表示羟基，烷氧基，芳基烷氧基，羟烷基氧基，烷氧基烷氧基，芳基烷氧基氧基或环烷氧基或R 5表示氢，烷基，取代的烷基，环烷基，芳基，芳基烷基，芳基烷氧基烷基或R 5与OR 4一起代表O（CH 2）n O 其中n为2,3或4; 和R 3代表氢，卤素，烷基或烷氧基或R 3与R 2一起代表式（c）的部分或其酯或酰胺; 提供4- [2- [2-羟基-3-（4-羟基苯氧基）丙基氨基]丙基]苯氧基乙酸及其盐和酯，并且EP0328251中公开的实施例不包括在式（I）的范围内。含有这种化合物的药物组合物，制备这种化合物的方法以及这种化合物在医药中的用途。

4. 发明申请

WO1995007284A1 PHOSPHINIC ACID DERIVATIVES WITH ANTI-HYPER GLYCEMIC AND/OR ANTI-OBESITY ACTIVITY 审中-公开
标题翻译：具有抗高血糖和/或抗脂肪活性的磷酸衍生物
公开(公告)号：WO1995007284A1
公开(公告)日：1995-03-16
申请号：PCT/EP1994002886
申请日：1994-08-29
申请人： SMITHKLINE BEECHAM PLC , BEELEY, Lee, James , BERGE, John, Michael
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07F09/30
CPC分类号： C07F9/301 , C07F9/3211
摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein, R represents a substituted or unsubstituted aryl group; R represents hydrogen or an alkyl group; R represents a moiety of formula (a) wherein R and R each independently represent hydrogen, alkyl, phenyl, hydroxyalkyl or cycloalkyl and R represents hydrogen, halogen, alkyl or alkoxy; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物或其药学上可接受的盐或其药学上可接受的溶剂合物，其中R 0表示取代或未取代的芳基; R 1表示氢或烷基; R 2表示式（a）的部分，其中R 4和R 5各自独立地表示氢，烷基，苯基，羟基烷基或环烷基，R 3表示氢，卤素，烷基或烷氧基; 制备这种化合物的方法，含有这种化合物的药物组合物和这种化合物在医药中的用途。

5. 发明申请

WO1994002493A1 PHOSPHONATED ARYLETHANOLAMINE COMPOUNDS WITH ANTI-HYPERGLYCEMIC AND/OR ANTI-OBESITY ACTIVITY 审中-公开
标题翻译：具有抗高血压和/或抗脂肪活性的磷酸化芳香胺化合物
公开(公告)号：WO1994002493A1
公开(公告)日：1994-02-03
申请号：PCT/GB1993001554
申请日：1993-07-22
申请人： SMITHKLINE BEECHAM PLC , BEELEY, Lee, James , BERGE, John, Michael , JARVEST, Richard, Lewis
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07F09/38
CPC分类号： C07F9/65515 , C07F9/3808 , C07F9/4006
摘要： A compound of formula (I) or a pharmaceutically acceptable salt, ester or amide thereof, or a pharmaceutically acceptable solvate thereof, wherein R0 represents a substituted or unsubstituted aryl group; R1 represents hydrogen or an alkyl group; R2 represents a moiety of formula (a) wherein R4 and R5 each independently represent hydrogen, alkyl, hydroxyalkyl, cycloalkyl or R4 together with R5 represents (CH2)n wherein n is 2, 3 or 4; T represents hydrogen, nitrile or a group -CO.Rs wherein Rs represents hydroxy, alkoxy or a group -NRtRu wherein Rt and Ru independently represent hydrogen, alkyl or Rt and Ru together with the nitrogen to which they are attached represent a saturated heterocyclic group; and R3 represents hydrogen, halogen, alkyl or alkoxy; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物或其药学上可接受的盐，酯或酰胺或其药学上可接受的溶剂合物，其中R 0表示取代或未取代的芳基; R1表示氢或烷基; R 2表示式（a）的部分，其中R 4和R 5各自独立地表示氢，烷基，羟烷基，环烷基或R 4以及R 5表示（CH 2）n，其中n为2,3或4; T表示氢，腈或基团-CO.Rs，其中R 5表示羟基，烷氧基或基团-NR t R u，其中R t和R u独立地表示氢，烷基或R t和R u与它们所连接的氮一起表示饱和杂环基 ; 并且R 3表示氢，卤素，烷基或烷氧基; 制备这种化合物的方法，包含这种化合物的药物组合物和这种化合物在医药中的用途。

6. 发明申请

WO1995004047A1 2-BENZOHETEROCYCLYLOXY OR THIOPROPANOLAMINE DERIVATIVES WITH ADRENO RECEPTOR AGONIST ACTIVITY 审中-公开
标题翻译：具有ADRENO受体激动剂活性的2-苯并二氧杂环戊烯或噻喃酚胺衍生物
公开(公告)号：WO1995004047A1
公开(公告)日：1995-02-09
申请号：PCT/EP1994002434
申请日：1994-07-22
申请人： SMITHKLINE BEECHAM PLC , BEELEY, Lee, James , BERGE, John, Michael
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D235/26
CPC分类号： C07F9/65068 , C07C217/84 , C07D235/26 , C07F9/4006
摘要： 2-Benzoheterocyclyloxy or thiopropanolamine derivatives of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein, R represents a moiety of formula (a), wherein one of X or X represents NH and the other of X or X represents NH, O or S and T represents hydrogen or one, two or three substituents selected from the list consisting of: hydroxy, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, amidoformyl, halogen and alkoxy; X represents O or S; R and R each independently represents hydrogen or an alkyl group; R represents OCH2CO2H, or an ester or amide thereof, or R represents a moiety of formula (b), wherein R represents hydrogen, alkyl, hydroxyalkyl or cycloalkyl and R represents hydroxy, alkoxy, hydroxyalkyloxy or cycloalkyloxy or R represents hydrogen, alkyl, substituted alkyl, cycloalkyl or aryl or R together with OR represents O(CH2)nO wherein n is 2, 3 or 4; and R represents hydrogen, halogen, alkyl or alkoxy or R together with R represents a moiety of formula (c), or an ester or amide thereof; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound in medicine. The claimed compounds are adreno receptor agonists.
摘要翻译：式（I）的2-苯并杂环氧基或硫代丙醇胺衍生物或其药学上可接受的盐，或其药学上可接受的溶剂合物，其中R 0表示式（a）的部分，其中X 1或X' 2>表示NH，X 1或X 2中的另一个表示NH，O或S，T表示氢或选自以下的一个，两个或三个取代基：羟基，氨基，烷基氨基，二烷基氨基，烷基磺酰氨基，芳基磺酰氨基，酰氨基甲酰基，卤素和烷氧基; X表示O或S; R 1和R 1a各自独立地表示氢或烷基; R 2表示OCH 2 CO 2 H或其酯或酰胺，或R 2表示式（b）的部分，其中R 4表示氢，烷基，羟烷基或环烷基，R 5表示羟基，烷氧基，羟基烷氧基或环烷氧基或R 5表示氢，烷基，取代的烷基，环烷基或芳基或R 5与OR 4一起代表O（CH 2）n O，其中n为2,3或4; 和R 3代表氢，卤素，烷基或烷氧基或R 3与R 2一起代表式（c）的部分，或其酯或酰胺; 制备这种化合物的方法，包含这种化合物的药物组合物和这种化合物在医药中的用途。要求保护的化合物是肾上腺素受体激动剂。

7. 发明申请

WO1994024090A1 ARYLETHANOLAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF OBESITY AND HYPERGLYCAEMIA 审中-公开
标题翻译：芳香胺衍生物及其在治疗肥胖和高血压中的应用
公开(公告)号：WO1994024090A1
公开(公告)日：1994-10-27
申请号：PCT/GB1994000829
申请日：1994-04-19
申请人： SMITHKLINE BEECHAM PLC , BEELEY, Lee, James , BERGE, John, Michael , SMITH, Richard, Anthony, Godwin
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07C217/60
CPC分类号： C07C69/712 , C07C205/32 , C07C217/60
摘要： A compound of formula (I) or a salt, ester or amide thereof, or a solvate thereof, wherein, R represents a substituted or unsubstituted aryl group; R represents hydrogen or an alkyl group; R represents a moiety of formula (a), wherein R represents a moiety (CH2)nCO2H wherein n is zero or an integer in the range of from 1 to 3 and R represents a moiety (CH2)pCO2H, (CH2)pOH, (CH2)pCN, (CH2)pCOCH3 or (CH2)pNH2 wherein p is zero or an integer in the range of from 1 to 3; and R represents hydrogen, halogen, alkyl or alkoxy; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound in medicine.
摘要翻译：式（I）的化合物或其盐，酯或酰胺或其溶剂合物，其中R 0表示取代或未取代的芳基; R 1表示氢或烷基; R 2表示式（a）的部分，其中R 4表示部分（CH 2）n CO 2 H，其中n为0或1至3的整数，R 5表示部分（CH 2 ）pCO 2 H，（CH 2）p OH，（CH 2）p CN，（CH 2）p COCH 3或（CH 2）p NH 2，其中p为0或1至3的整数; R 3表示氢，卤素，烷基或烷氧基; 制备这种化合物的方法，包含这种化合物的药物组合物和这种化合物在医药中的用途。

8. 发明申请

WO1993009113A1 2-((IMIDAZOL-2-YL)METHYL)-ISOINDOLE DERIVATIVES AS ALPHA-2-ADRENOCEPTOR ANTAGONISTS 审中-公开
标题翻译： 2 - （（咪唑烷-2-基）甲基） - 衍生物作为ALPHA-2-ADRENOCEPTOR ANTAGONISTS
公开(公告)号：WO1993009113A1
公开(公告)日：1993-05-13
申请号：PCT/GB1992002047
申请日：1992-11-05
申请人： SMITHKLINE BEECHAM PLC , BERGE, John, Michael , BEELEY, Lee, James , CAWTHORNE, Michael, Anthony
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein R and R may each represent hydrogen or C1-6alkyl, providing that at least one of R or R represents C1-6alkyl; and R and R each represent hydrogen or R together with R represents a bond; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound, and the use of such a composition and compound in medicine.
摘要翻译：式（I）化合物或其药学上可接受的盐，或其药学上可接受的溶剂合物，其中R 1和R 2各自可以表示氢或C 1-6烷基，条件是R 1，或R 2表示C 1-6烷基; R 3和R 4各自代表氢或R 3与R 4一起代表键; 制备这种化合物的方法，包含这种化合物的药物组合物，以及这种组合物和化合物在医药中的用途。

9. 发明申请

WO1994013650A1 HETEROCYCLIC DERIVATIVES AND THEIR USE IN PHARMACEUTICALS 审中-公开
标题翻译：杂环衍生物及其在药物中的应用
公开(公告)号：WO1994013650A1
公开(公告)日：1994-06-23
申请号：PCT/EP1993003269
申请日：1993-11-22
申请人： SMITHKLINE BEECHAM PLC , HAIGH, David , RAMI, Harshad, Kantilal
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D263/58
CPC分类号： C07D213/74 , C07D263/58
摘要： A compound of formula (I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein: A represents a substituted or unsubstituted aromatic heterocyclyl group; A represents a benzene ring having three optional substituents; R and R each independently represents hydrogen or R together with R represents a bond; R and R each independently represents a nitrile group or a group of formula: -COR wherein R represents hydroxy, alkoxy, alkyl, aryl or a group of formula: -NR R wherein R and R each independently represents hydrogen or alkyl or R and R together with the nitrogen atom to which they are attached form a heterocyclic ring; X represents NR wherein R represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; and n represents an integer in the range of from 2 to 6; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound and composition in medicine.
摘要翻译：式（I）化合物或其互变异构形式和/或其药学上可接受的盐，和/或其药学上可接受的溶剂合物，其中：A 1表示取代或未取代的芳族杂环基; A 2表示具有三个任选取代基的苯环; R 1和R 2各自独立地表示氢或R 1与R 2一起表示键; R 3和R 4各自独立地表示腈基或式-COR 5的基团，其中R 5表示羟基，烷氧基，烷基，芳基或式-NR 6的基团，其中R 6和R 7各自独立地表示氢或烷基或R 6和R 7与它们所连接的氮原子一起形成杂环; X表示NR，其中R表示氢原子，烷基，酰基，芳基部分可以被取代或未取代的芳烷基，或取代或未取代的芳基; n表示2〜6的整数，制备这种化合物的方法，包含这种化合物的药物组合物和在药物中使用这种化合物和组合物。

10. 发明申请

WO1996004260A1 BENZOXAZOLES AND PYRIDINE DERIVATIVES USEFUL IN THE TREATMENT OF THE TYPE II DIABETES 审中-公开
标题翻译：用于治疗II型糖尿病的苯并唑和吡啶衍生物
公开(公告)号：WO1996004260A1
公开(公告)日：1996-02-15
申请号：PCT/EP1995003038
申请日：1995-07-28
申请人： SMITHKLINE BEECHAM PLC , HAIGH, David , RAMI, Harshad, Kantilal
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D263/58
CPC分类号： C07D213/74 , C07D263/58
摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein R represents 2-benzoxazolyl or 2-pyridyl and R represents CH2OCH3 or CF3; a process for the preparation of such compounds, a pharmaceutical composition containing such compounds and the use of such compounds and compositions in medicine.
摘要翻译：式（I）化合物或其药学上可接受的盐，和/或其药学上可接受的溶剂合物，其中R 0表示2-苯并恶唑基或2-吡啶基，R 1表示CH 2 OCH 3或CF 3; 制备这种化合物的方法，含有这些化合物的药物组合物以及这些化合物和组合物在医药中的用途。

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