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1. 发明申请

WO1994021637A1 PROCESS FOR THE PREPARATION OF CONDENSED CARBAPENEME DERIVATIVES 审中-公开
标题翻译：制备冷凝型碳水化合物衍生物的方法
公开(公告)号：WO1994021637A1
公开(公告)日：1994-09-29
申请号：PCT/EP1994000838
申请日：1994-03-17
申请人： GLAXO SPA , ARALDI, Gian, Luca
发明人： GLAXO SPA
IPC分类号： C07D477/00
CPC分类号： C07D477/00 , Y02P20/55
摘要： A process for the preparation of the antibacterial compound of formula (I) or a salt thereof which comprises the thermal cyclisation of a compound of formula (II), wherein R is a carboxyl protecting group, followed by removal of the said carboxyl protecting group R and if necessary or desired conversion of the resultant carboxylic acid into a salt thereof.
摘要翻译：一种制备式（I）的抗菌化合物或其盐的方法，其包括式（II）化合物的热环化，其中R是羧基保护基，然后除去所述羧基保护基R 并且如果需要或期望将所得羧酸转化成其盐。

2. 发明申请

WO1995003284A1 1,5-BENZODIAZEPINE DERIVATIVES USEFUL AS CCK OR GASTRIN ANTAGONISTS 审中-公开
标题翻译： 1,5-苯二酮衍生物作为CCK或GASTRIN ANTAGONISTS有用
公开(公告)号：WO1995003284A1
公开(公告)日：1995-02-02
申请号：PCT/EP1994002352
申请日：1994-07-18
申请人： GLAXO SPA , CUROTTO, Giovanni , PELLEGATTI, Mario , POLINELLI, Stefano
发明人： GLAXO SPA
IPC分类号： C07D243/12
CPC分类号： C07D243/12
摘要： Compounds of formula (I) wherein R represents a phenyl, C3-7cycloalkyl, C7-11 bridgedcycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C7-11 bridgedcycloalkyl group; R represents phenyl substituted by a group (CH2)nNR R , O(CH2)pR , or (CH2)nCO2R ; R represents phenyl optionally substituted by one or 2 halogen atoms; R represents hydrogen or C1-4alkyl; R represents acyl, or C2-4alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R and R together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C1-4alkyl or hydroxy groups. R represents hydroxy, C1-4alkoxy, CO2R or NR R ; R represents hydrogen or C1-4alkyl or a metabolically labile ester group; R represents hydrogen, C1-4alkyl, acyl or C2-6alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R and R together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C1-4alkyl or hydroxy groups; R represents hydrogen or a halogen atom; R represents a metabolically labile ester group; m is zero, 1 or 2; n is zero or 1; p is an integer from 1 to 4; X represents oxygen or NH and pharmaceutically acceptable salts thereof are antagonists of gastrin and CCK.
摘要翻译：式（I）的化合物，其中R 1表示苯基，C 3-7环烷基，C 7-11桥环的环烷基或C 1-6烷基，该烷基可被羟基，苯基，C 1-6烷氧基羰基，C 3-7环烷基或C 7 -11桥连环烷基; R 2表示被基团（CH 2）n NR 4 R 5，O（CH 2）p R 6或（CH 2）n CO 2 R 11取代的苯基; R 3表示任选被一个或两个卤素原子取代的苯基; R 4表示氢或C 1-4烷基; 或被一个或多个羟基，羧基和/或氨基取代的C 2-4烷基或R 4和R 5与它们所连接的氮原子一起形成5-7饱和的杂环，其含有选自氧，硫或氮的另外的杂原子和/或可以被1或2个C 1-4烷基或羟基取代。 R 6表示羟基，C 1-4烷氧基，CO 2 R 7或NR 8 R 9; R 7表示氢或C 1-4烷基或代谢不稳定的酯基; R 8表示氢，C 1-4烷基，酰基或被一个或多个羟基，羧基和/或氨基取代的C 2-6烷基或R 8和R 9与它们所连接的氮原子一起形成 5-7饱和杂环，其含有选自氧，硫或氮的另外的杂原子和/或可被1或2个C 1-4烷基或羟基取代; R 10表示氢或卤素原子; R 11表示代谢不稳定的酯基; m为零，1或2; n为零或1; p是1至4的整数; X表示氧或NH，其药学上可接受的盐是胃泌素和CCK的拮抗剂。

3. 发明申请

WO1994025444A1 3-PHENYLUREIDO-1,5-BENZODIAZEPINE-DIONES USEFUL AS GASTRIN OR CCK ANTAGONISTS 审中-公开
标题翻译： 3-苯并呋喃并-1,5-苯并二氢吡喃酮可用作胃肠素或CCK拮抗剂
公开(公告)号：WO1994025444A1
公开(公告)日：1994-11-10
申请号：PCT/EP1994001252
申请日：1994-04-22
申请人： GLAXO SPA , FINCH, Harry , TRIST, David, Gordon , FERIANI, Aldo , TARZIA, Giorgio , SHAH, Pritom
发明人： GLAXO SPA
IPC分类号： C07D243/12
CPC分类号： C07D403/12 , C07D243/12
摘要： Compounds of formula (I), wherein R represents a phenyl, C3-7cycloalkyl, C7-11 bridged cycloalkyl or C1-6alkyl group which alkyl group may be susbtituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl or C7-11 bridged cycloalkyl group; R represents NR SO2CF3, SO2NR COR , CONR SO2R , or a tetrazole, carboxamidotetrazole, or 3-trifluoromethyl-1,2,4-triazole group, which groups may be substituted on one of the nitrogen atoms by a C1-4alkyl group; R is phenyl optionally substituted by one or two halogen atoms; R represents hydrogen or a C1-4alkyl group; R represents a C1-4alkyl group; R represents hydrogen or a halogen atom; m is zero, 1 or 2; n is zero or 1; and pharmaceutically acceptable salts and solvates thereof, and their use as gastrin/CCK-B antagonists.
摘要翻译：式（I）化合物，其中R 1表示苯基，C 3-7环烷基，C 7-11桥环烷基或C 1-6烷基，该烷基可以被羟基，苯基，C 1-6烷氧基羰基，C 3-7环烷基或 C7-11桥连环烷基; R 2表示NR 4 SO 2 CF 3，SO 2 NR 4 COR 5，CONR 4 SO 2 R 5，或四唑，羧酰胺基四唑或3-三氟甲基-1,2,4-三唑基，其中基团可以在一个氮原子上被C 1-4烷基取代; R 3是任选被一个或两个卤素原子取代的苯基; R 4表示氢或C 1-4烷基; R 5表示C 1-4烷基; R 6表示氢或卤素原子; m为零，1或2; n为零或1; 及其药学上可接受的盐和溶剂合物，以及它们作为胃泌素/ CCK-B拮抗剂的用途。

4. 发明申请

WO1995003285A1 1,5-BENZODIAZEPINE DERIVATIVES USEFUL AS CCK OR GASTRIN ANTAGONISTS 审中-公开
标题翻译： 1,5-苯二酮衍生物作为CCK或GASTRIN ANTAGONISTS有用
公开(公告)号：WO1995003285A1
公开(公告)日：1995-02-02
申请号：PCT/EP1994002353
申请日：1994-07-18
申请人： GLAXO SPA , DONATI, Daniele , URSINI, Antonella , CORSI, Mauro
发明人： GLAXO SPA
IPC分类号： C07D243/12
CPC分类号： C07D243/12 , Y02P20/582
摘要： Compounds of formula (I) wherein R represents a phenyl, C3-7cycloalkyl, c7-11 bridgedcycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C7-11 bridgedcycloalkyl group; R represents a phenyl group optionally substituted by 1 or 2 substituents selected from halogen, C1-4alkyl, C1-4alkylthio, cyano, nitro, trifluoromethyl, trifluoromethoxy, (CH2)nR or O(CH2)pR wherein R represents hydroxy, C1-4alkoxy, CO2R or NR R ; n is zero or 1; p is an integer from 1 to 4; R represents the group AlkNR R ; R represents hydrogen or C1-4alkyl; R represents hydrogen or C1-4alkyl; R represents hydrogen, C1-4alkyl, acyl, or C2-6alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R and R together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C1-4alkyl or hydroxy groups. R and R independently represent hydrogen, C1-4alkyl or C2-6alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R or R together with the nitrogen atom which they are attached represent a 5-7 saturated heterocyclic ring which may contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C1-4alkyl or hydroxy groups; Alk represents a straight or branched C2-6alkylene chain optionally substituted by a hydroxyl group; R represents hydrogen or a halogen atom; m is zero, 1 or 2; X is oxygen or NH; and pharmaceutically acceptable salts and or metabolically labile esters thereof are antagonists of gastrin and CCK.
摘要翻译：式（I）的化合物，其中R 1表示苯基，C 3-7环烷基，C 7-11桥环的环烷基或C 1-6烷基，该烷基可以被羟基，苯基，C 1-6烷氧基羰基，C 3-7环烷基或C 7 -11桥连环烷基; R 2表示任选被1或2个选自卤素，C 1-4烷基，C 1-4烷硫基，氰基，硝基，三氟甲基，三氟甲氧基，（CH 2）nR 4或O（CH 2）p R 4的取代基取代的苯基其中R 4表示羟基，C 1-4烷氧基，CO 2 R 5或NR 6 R 7; n为零或1; p是1至4的整数; R 3表示基团AlkNR 8 R 9; R 5表示氢或C 1-4烷基; R 6表示氢或C 1-4烷基; R 7表示氢，C 1-4烷基，酰基或被一个或多个羟基，羧基和/或氨基取代的C 2-6烷基或R 6和R 7与它们所连接的氮原子一起形成5-7饱和杂环，其含有选自氧，硫或氮的另外的杂原子和/或可被1或2个C 1-4烷基或羟基取代。 R 8和R 9独立地表示氢，被一个或多个羟基，羧基和/或氨基取代的C 1-4烷基或C 2-6烷基，或者R 8或R 9与氮原子一起被取代连接表示5-7饱和杂环，其可以含有选自氧，硫或氮的另外的杂原子和/或可以被1或2个C 1-4烷基或羟基取代; Alk表示任选被羟基取代的直链或支链C 2-6亚烷基链; R 10表示氢或卤素原子; m为零，1或2; X是氧或NH; 和其药学上可接受的盐和/或代谢不稳定的酯是胃泌素和CCK的拮抗剂。

5. 发明申请

WO1994021638A1 PROCESS FOR THE PREPARATION OF CONDENSED CARBAPENEME DERIVATIVES 审中-公开
标题翻译：制备冷凝型碳水化合物衍生物的方法
公开(公告)号：WO1994021638A1
公开(公告)日：1994-09-29
申请号：PCT/EP1994000839
申请日：1994-03-17
申请人： GLAXO SPA , TUGHAN, Garfield, Cecil
发明人： GLAXO SPA
IPC分类号： C07D477/00
CPC分类号： C07D477/00
摘要： A process for the preparation of antibacterial compound (I) or a salt thereof which comprises hydrogenolysis of the novel compound of formula (II) and if necessary or desired isolating the resultant carboxylic acid as a salt thereof.
摘要翻译：一种制备抗菌化合物（I）或其盐的方法，其包括使新型式（II）化合物氢解，如果需要或需要，将其作为其盐分离所得羧酸。

6. 发明申请

WO1993014075A1 CARBAMATE DERIVATIVES AND THEIR USE IN MEDICINE 审中-公开
标题翻译：氨基甲酸酯类衍生物及其在医学
公开(公告)号：WO1993014075A1
公开(公告)日：1993-07-22
申请号：PCT/EP1993000099
申请日：1993-01-15
申请人： GLAXO SPA , TRIST, David , PENTASSUGLIA, Giorgio , TRANQUILLINI, Maria, Elvira , URSINI, Antonella
发明人： GLAXO SPA
IPC分类号： C07D243/12
CPC分类号： C07D243/12
摘要： Compounds of general formula (I), wherein R represents a phenyl, C3-7cycloalkyl, bridged C7-11cycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl or bridged C7-11cycloalkyl group or R represents the group XYR wherein X is a C1-3 straight or branched alkylene chain, Y is C=O, C(OR )2 or C(SR )2 and R is a C1-6alkyl, optionally substituted phenyl, C3-7cycloalkyl or bridged C7-11cycloalkyl. R represents a substituted or unsubstituted phenyl (wherein the substituents may be 1 or 2 of halo, C1-4alkyl, nitro, cyano, trifluoromethyl, trifluoromethoxy C1-4alkylthio or (CH2)nR wherein R is hydroxy, C1-4alkoxy, CO2R or NR R . R represents phenyl optionally substituted by one or two halogen atoms; R represents hydrogen or a C1-4alkyl group; R and R independently represent hydrogen or a C1-4alkyl group. R represents hydrogen or a halogen atom; m is 0, 1 or 2; n is 0 or 1; are antagonists of gastrin and CCK-B receptors.
摘要翻译：通式（I）的化合物，其中R 1表示苯基，C 3-7环烷基，桥连的C 7-11环烷基或C 1-6烷基，该烷基可以被羟基，苯基，C 1-6烷氧基羰基，C 3-7环烷基或桥连基团C7-11cycloalkyl或R <1>代表基团XYR <4>其中X是C 1-3直链或支链亚烷基链，Y是C = O，C（OR <5>）2或C（SR <5 >）2和R <4>是一个C 1-6烷基，任选取代的苯基，C 3-7环烷基或桥接C7-11cycloalkyl。 R 2表示取代或未取代的苯基（其中取代基可以是卤素，C 1-4烷基，硝基，氰基，三氟甲基，三氟甲氧基C 1-4烷硫基或（CH 2）n R 6的1或2，其中R 6为羟基，C 1-4烷氧基，CO 2 R 7或NR 8 R 9，R 3表示任选被一个或两个卤素原子取代的苯基; R 7表示氢或C 1-4烷基; 8>和R 9独立地表示氢或C 1-4烷基，R 10表示氢或卤素原子; m为0,1或2; n为0或1;为胃泌素和CCK-B的拮抗剂受体。

7. 发明申请

WO1995026333A1 PROCESS FOR THE PREPARATION OF CYCLOHEXYL-AZETIDINONES 审中-公开
标题翻译：制备环己基氨基甲酸酯的方法
公开(公告)号：WO1995026333A1
公开(公告)日：1995-10-05
申请号：PCT/EP1995001114
申请日：1995-03-23
申请人： GLAXO SPA , ROSSI, Tino , ZARANTONELLO, Paola , THOMAS, John, Russel
发明人： GLAXO SPA
IPC分类号： C07D205/08
CPC分类号： C07D205/08 , C07F7/1804 , Y02P20/55
摘要： A process for the preparation of compounds of formula (I) wherein R>1
摘要翻译：一种制备式（I）化合物的方法，其中R 1是羟基保护基，其包括使氮杂环丁酮（II）与同时合成的（2S）-2-甲氧基环己烷（III）或其与一个氯化锡分子。

8. 发明申请

WO1995010517A1 INDOLE DERIVATIVES AS NMDA ANTAGONISTS 审中-公开
标题翻译：将衍生物作为NMDA拮抗剂
公开(公告)号：WO1995010517A1
公开(公告)日：1995-04-20
申请号：PCT/EP1994003359
申请日：1994-10-12
申请人： GLAXO SPA , CUGOLA, Alfredo , Di FABIO, Romano , PENTASSUGLIA, Giorgio
发明人： GLAXO SPA
IPC分类号： C07D403/06
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D413/06 , Y02P20/55
摘要： This invention relates to compounds of formula (I) or a salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO2R2 or COR2 wherein R2 represents hydroxy, methoxy, amino, alkylamino, or dialkylamino; m is zero or an integer 1 or 2; R1 represents a cycloalkyl, bridged cycloalkyl, heteroaryl, bridged heterocyclic or optionally substituted phenyl or fused bicyclic carbocyclic group; A represents a C1-4 alkylene chain or the chain (CH2)pY(CH2)q wherein Y is O, S(O)n or NR3 and which chains may be substituted by one or two groups selected from C1-6 alkyl optionally substituted by hydroxy, amino, alkylamino or dialkylamino, or which chains may be substituted by the group = O; R3 represents hydrogen, alkyl or a nitrogen protecting group; n is zero or an integer from 1 to 2; p is zero or an integer from 1 to 3; q is zero or an integer from 1 to 3 with the proviso that the sum of p + q is 1, 2 or 3, which are antagonists of excitatory amino acids, to processes for the preparation and to other use in medicine.
摘要翻译：本发明涉及式（I）化合物或其盐或其代谢不稳定的酯，其中R表示选自卤素，烷基，烷氧基，氨基，烷基氨基，二烷基氨基，羟基，三氟甲基，三氟甲氧基，硝基，氰基，SO 2 R 2或 COR2其中R2表示羟基，甲氧基，氨基，烷基氨基或二烷基氨基; m为零或整数1或2; R 1表示环烷基，桥连环烷基，杂芳基，桥连杂环或任选取代的苯基或稠合双环碳环基团; A表示C1-4亚烷基链或链（CH2）pY（CH2）q，其中Y是O，S（O）n或NR3，哪些链可以被一个或两个选自任选取代的C 1-6烷基的基团取代羟基，氨基，烷基氨基或二烷基氨基，或哪些链可以被基团= O取代; R3表示氢，烷基或氮保护基; n为0或1至2的整数; p为0或1至3的整数; q为0或1至3的整数，条件是p + q的和为1,2或3，它们是兴奋性氨基酸的拮抗剂，用于制备和在医药中的其它用途。

9. 发明申请

WO1993014074A1 1,5-BENZODIAZEPINE DERIVATIVES AND THEIR USE IN MEDICINE 审中-公开
公开(公告)号：WO1993014074A1
公开(公告)日：1993-07-22
申请号：PCT/EP1993000098
申请日：1993-01-19
申请人： GLAXO SPA , FINCH, Harry , TRIST, David, Gordon , TARZIA, Giorgio , FERIANI, Aldo
发明人： GLAXO SPA
IPC分类号： C07D243/12
CPC分类号： C07D243/12
摘要： Compounds of general formula (I), wherein R represents a phenyl, C3-7cycloalkyl, C7-11 bridged cycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C7-11 bridged cycloalkyl group; R represents a substituted or unsubstituted phenyl group (wherein the substituents may be 1 or 2 of halo, C1-4alkyl, nitro, cyano trifluoromethyl, trifluoromethoxy, C1-4alkylthio or (CH2)nR wherein R is hydroxy, C1-4alkoxy, CO2R or NR R . R is phenyl optionally substituted by one or two halogen atoms; R represents hydrogen or a C1-4alkyl group; R and R independently represent hydrogen or a C1-4alkyl group. R represents hydrogen or a halogen atom; m is 0, 1 or 2; n is 0 or 1; are antagonists of gastrin and CCK-B receptors.
摘要翻译：通式（I）的化合物，其中R 1表示苯基，C 3-7环烷基，C 7-11桥环烷基或C 1-6烷基，该烷基可被羟基，苯基，C 1-6烷氧基羰基，C 3-7环烷基或C7-11桥连环烷基; R 2表示取代或未取代的苯基（其中取代基可以是卤素，C 1-4烷基，硝基，氰基三氟甲基，三氟甲氧基，C 1-4烷硫基或（CH 2）n R 4的1或2，其中R 4， R 3是任选被一个或两个卤素原子取代的苯基; R 5代表氢或C 1-4烷基; R 3是氢，C 1-4烷氧基， R 8和R 7独立地表示氢或C 1-4烷基，R 8表示氢或卤原子; m为0,1或2; n为0或1;为胃泌素和CCK- B受体。

10. 发明申请

WO1992014460A1 USE OF LACIDIPINE FOR THE TREATMENT OF ARTERIOSCLEROSIS 审中-公开
标题翻译：拉西替丁治疗肠梗塞的用途
公开(公告)号：WO1992014460A1
公开(公告)日：1992-09-03
申请号：PCT/EP1992000276
申请日：1992-02-08
申请人： GLAXO SPA , GAVIRAGHI, Giovanni
发明人： GLAXO SPA
IPC分类号： A61K31/44
CPC分类号： A61K31/44
摘要： The use of (E)-4-[2-[3-(1,1-dimethylethoxy)-3-oxo-1-propenyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid diethyl ester (lacidipine) for the treatment and/or prevention of arteriosclerosis.

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