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81. 发明申请

WO1995033723A1 PHENOXYALKYL SUBSTITUTED PIPERIDINES, PYRROLIDINES, MORPHOLINES AND THIOMORPHOLINES AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：苯氧基取代的哌啶，吡咯烷酮，吗啉和三羟基磷酰胺作为钙通道拮抗剂
公开(公告)号：WO1995033723A1
公开(公告)日：1995-12-14
申请号：PCT/EP1995002003
申请日：1995-05-24
申请人： SMITHKLINE BEECHAM PLC , BROWN, Thomas, Henry , COPPER, David, Gwyn
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D211/22
CPC分类号： C07D211/22
摘要： Compounds of formula (I), in which W is -(CH2)4, (CH2)5, -(CH2)2O(CH2)2 or -(CH2)2S(CH2)2 n is 0 to 6; m is 0 to 3; A is a bond, -CH=CH-, -CC-, oxygen, sulphur or NR ; R is hydrogen, C1-8alkyl or phenyl C1-4alkyl; and Ar is a group (a) where X is a bond, O, CH2, CO or OCH2 and Hal is fluoro or chloro; and salts thereof are calcium channel antagonists with activity in neurons and are useful in the treatment of conditions such as ischaemic stroke.
摘要翻译：其中W为 - （CH 2）4，（CH 2）5， - （CH 2）2 O（CH 2）2或 - （CH 2）2 S（CH 2）2 n的式（I）化合物为0至6; m为0〜3; A是键，-CH = CH-，-CC-，氧，硫或NR 1; R 1是氢，C 1-8烷基或苯基C 1-4烷基; 并且Ar是其中X是键的基团（a），O，CH 2，CO或OCH 2，Hal是氟或氯; 其盐是在神经元中具有活性的钙通道拮抗剂，可用于治疗缺血性中风等病症。

82. 发明申请

WO1995032199A1 PROCESS FOR PREPARING BENZOPYRAN COMPOUNDS 审中-公开
标题翻译：制备苯并噻唑化合物的方法
公开(公告)号：WO1995032199A1
公开(公告)日：1995-11-30
申请号：PCT/EP1995001915
申请日：1995-05-18
申请人： SMITHKLINE BEECHAM PLC , HAYLER, John, David , GRINTER, Trevor, John , NOVAK, Vance , LEWIS, Norman, John
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D405/04
CPC分类号： C07D257/04 , C07D405/04
摘要： A process for preparing certain substituted benzopyran compounds is disclosed.
摘要翻译：公开了制备某些取代的苯并吡喃化合物的方法。

83. 发明申请

WO1995028402A2 PREPARATION OF PURINES 审中-公开
标题翻译：产品的制备
公开(公告)号：WO1995028402A2
公开(公告)日：1995-10-26
申请号：PCT/EP1995001840
申请日：1995-04-19
申请人： SMITHKLINE BEECHAM PLC , DALES, John, Robert, Mansfield
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D473/00
CPC分类号： C07D473/00
摘要： A process for the preparation of a compound of formula (A) wherein: X is hydrogen, hydroxy, chloro, C1-6 alkoxy or phenyl C1-6 alkoxy; and Ra and Rb are hydrogen, or acyl or phosphate derivatives thereof, which process comprises: (i) the preparation of a compound of formula (I) wherein R1 is C1-6 alkyl, or phenyl C1-6 alkyl in which the phenyl group is optionally substituted; R2 is hydrogen, hydroxy, chlorine, C1-6 alkoxy, phenyl C1-6 alkoxy or amino; and R3 is halogen, C1-6 alkylthio, C1-6 alkylsulphonyl, azido, an amino group or a protected amino group, which preparation comprises the reaction of a compound of formula (II), wherein R2 and R3 are as defined for formula (I) with a compound of formula (V) wherein L is a leaving group and R1 is as defined for formula (I), to give a compound of formula (VI), and thereafter converting the intermediate compound of formula (VI) to a compound of formula (I) via decarboxylation, and, as necessary or desired, interconverting variables R1, R2 and R3 to further values of R1, R2 and R3; (ii) the conversion of the resulting compound of formula (I) to a compound of formula (A) by converting variable R3, when other than amino, to amino, reducing the ester groups CO2R1 to CH2OH and optionally forming acyl or phosphate derivatives thereof, and as necessary or desired converting variable R2 in the compound of formula (I) to variable X in the compound of formula (A); characterised in that R2 is chloro in formula (I).
摘要翻译：一种制备式（A）化合物的方法，其中：X是氢，羟基，氯，C 1-6烷氧基或苯基C 1-6烷氧基; 并且R a和R b是氢或其酰基或磷酸酯衍生物，该方法包括：（i）制备其中R 1为C 1-6烷基的式（I）化合物或苯基C 1-6烷基，其中苯基任选地被取代; R2是氢，羟基，氯，C1-6烷氧基，苯基C1-6烷氧基或氨基; 并且R 3是卤素，C 1-6烷硫基，C 1-6烷基磺酰基，叠氮基，氨基或被保护的氨基，其制备包括式（II）化合物的反应，其中R 2和R 3如式 I）与式（V）化合物反应，其中L是离去基团，R 1如式（I）所定义，得到式（VI）化合物，然后将式（VI）的中间体化合物转化为将式（I）化合物通过脱羧反应，并且根据需要或需要将相互转化的变量R1，R2和R3转化为R1，R2和R3的进一步的值; （ii）将所得的式（I）化合物转化成式（A）化合物时，通过将可变的R 3（当除氨基以外）转化为氨基时，将酯基CO 2 R 1至CH 2 OH还原并任选地形成其酰基或磷酸酯衍生物，并且根据需要或需要将式（I）化合物中的变量R2转化为式（A）化合物中的可变的X; 其特征在于式（I）中的R 2为氯。

84. 发明申请

WO1995024832A1 STABLE, OPTICALLY CLEAR COMPOSITIONS 审中-公开
标题翻译：稳定，光学清晰的组合物
公开(公告)号：WO1995024832A1
公开(公告)日：1995-09-21
申请号：PCT/EP1995000899
申请日：1995-03-09
申请人： SMITHKLINE BEECHAM PLC , FORD, Michael, Anthony
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： A23L01/035
CPC分类号： A61K9/0095 , A23L2/42 , A23L2/52 , A61K9/1075
摘要： Stable aqueous compositions of biologically active oils for the preparation of optically clear products for use in human or animal healthcare, for example beverages, are prepared by a process comprising: (a) mixing 0.001-2.0 % w/w of a biologically active oil or 0.1-2.0 % w/w of a biologically active oil as a 20-30 % dispersion in a suitable oil with 0.1-1.0 % of an antioxidant or antioxidant mixture, (b) dispersing the mixture from (a) in 2-20 % of an emulsifier or an emulsifier mixture having an HLB (hydrophilic-lipophilic balance) value of 10 to 18 and heating to 50 to 150 DEG C so as to yield a transparent mixture, (c) raising the temperature of the mixture from (b) as appropriate whilst maintaining stirring to maintain a transparent mixture, and (d) combining the mixture from (c) with water having a minimum temperature of 95 DEG C while continuously stirring to provide a transparent composition.
摘要翻译：用于制备用于人或动物保健（例如饮料）的光学透明产品的生物活性油的稳定水性组合物通过以下方法制备，所述方法包括：（a）将0.001-2.0％w / w的生物活性油或 0.1-2.0％w / w的生物活性油作为20-30％的分散体在合适的油中，含有0.1-1.0％的抗氧化剂或抗氧化剂混合物，（b）将来自（a）的混合物分散在2-20％的乳化剂或乳化剂混合物，其HLB（亲水 - 亲油平衡）值为10至18，加热至50至150℃，以产生透明混合物，（c）将混合物的温度从（b）同时保持搅拌以保持透明混合物，和（d）将来自（c）的混合物与最低温度为95℃的水混合，同时连续搅拌以提供透明组合物。

85. 发明申请

WO1995017190A1 PHARMACEUTICALS 审中-公开
标题翻译：制药
公开(公告)号：WO1995017190A1
公开(公告)日：1995-06-29
申请号：PCT/EP1994004163
申请日：1994-12-14
申请人： SMITHKLINE BEECHAM PLC , BOON, Ronald, James , GRIFFIN, David, Ronald, John
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： A61K31/52
CPC分类号： C07D473/00 , A61K31/52
摘要： A method for the treatment (including prophylaxis) of ZAP in mammals, including humans, which method comprises administering to the mammal in need of such treatment, an effective amount of a compound of formula (A) or a bioprecursor, or a pharmaceutically acceptable salt, phosphate ester and/or acyl derivative of either of the foregoing and the use of a compound of formula (A): or a bioprecursor, or a pharmaceutically acceptable salt, phosphate ester and/or acyl derivative of either of the foregoing in the manufacture of a medicament for use in the treatment (including prophylaxis) of ZAP.
摘要翻译：一种用于哺乳动物（包括人）中ZAP治疗（包括预防）的方法，该方法包括向需要这种治疗的哺乳动物施用有效量的式（A）化合物或生物前体或其药学上可接受的盐，前述的任何一种的磷酸酯和/或酰基衍生物以及式（A）化合物或其制备方法中使用的任何一种的生物前体或生物前体或其药学上可接受的盐，磷酸酯和/或酰基衍生物的用途的用于治疗（包括预防）ZAP的药物。

86. 发明申请

WO1995016686A1 HETEROARYL MUPIROCIN DERIVATIVES USEFUL AS ANTIBACTERIAL, ANTIFUNGAL OR HERBICIDAL AGENTS 审中-公开
标题翻译：异丙肾上腺素衍生物作为抗生素，抗真菌药物或除草剂
公开(公告)号：WO1995016686A1
公开(公告)日：1995-06-22
申请号：PCT/EP1994004136
申请日：1994-12-13
申请人： SMITHKLINE BEECHAM PLC , BROWN, Pamela , O'HANLON, Peter, John
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D413/14
CPC分类号： C07D405/14 , A01N43/647 , A01N43/713 , A01N43/74 , A01N43/80 , A01N43/82 , C07D413/14 , C07D417/14 , Y02P20/55
摘要： Compounds of formula (I), in which A represents a 5-membered heteroaryl ring; R DEG is an optionally substituted aryl or a heteroaryl ring; and Z1, Z2 and Z3 are the same or different and each is hydrogen or a hydroxyl protecting group, have antibacterial, antimycoplasmal, antifungal and herbicical activity.
摘要翻译：式（I）化合物，其中A表示5元杂芳基环; R DEG是任选取代的芳基或杂芳基环; Z1，Z2和Z3相同或不同，各自为氢或羟基保护基，具有抗菌，抗支原体，抗真菌和除草活性。

87. 发明申请

WO1995016674A1 AMINOSULPHONYL-PHENYL-1H-PYRROLE DERIVATIVES, METHOD OF THEIR PREPARATION AND THEIR USE 审中-公开
标题翻译：氨基苯基 - 苯基-1H-吡咯衍生物，其制备方法及其用途
公开(公告)号：WO1995016674A1
公开(公告)日：1995-06-22
申请号：PCT/EP1994004175
申请日：1994-12-16
申请人： SMITHKLINE BEECHAM PLC , MARKWELL, Roger, Edward , STEMP, Geoffrey , WADSWORTH, Harry, John , WATTS, Eric, Alfred
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D207/335
CPC分类号： C07D207/333 , C07D207/335 , C07D401/14 , C07D403/06 , C07D405/12 , C07D405/14
摘要： Compounds of formula (I) wherein R represents C1-4alkyl; one of R , R , R and R represents a sulphonamido group R R NSO2-, wherein either: R represents hydrogen, C1-6alkyl, or C1-4alkoxyC1-4alkyl; and R represents a group (R )p-(Ar)-(CH2)j- wherein Ar represents phenyl, naphthyl, a 5- or 6-membered heterocyclic aryl group, or a 5- or 6-membered heterocyclic aryl group fused to a phenyl ring; j represents zero or an integer from 1-4; R represents a substituent selected from halogen, C1-4alkyl, C1-4alkoxy, C1-4alkoxyC1-4alkyl, nitro, cyano, trifluoromethyl, trifluoromethoxy, hydroxy, hydroxyC1-4alkyl, C1-4alkanoyl, C1-4alkoxycarbonyl, amino, mono- or -di-C1-4alkylamino, C1-4alkylthio, C1-4alkylsulphinyl, C1-4alkylsulphonyl and phenylC1-4alkoxy; and p represents zero or an integer from 1-4; or R R N- represents a 5-7 membered heterocyclic ring which is fused to or substituted by a phenyl group, or substituted by a 5- or 6-membered heterocyclic aryl group, said phenyl or heteroaryl group being optionally substituted by a group (R )p, wherein R and p are as defined hereinabove; and Y represents a group selected from (a) - (e); and salts thereof, have activity at dopamine receptors and are potentially useful in the treatment of psychoses such as schizophrenia.
摘要翻译：其中R 1表示C 1-4烷基的式（I）化合物; R 2，R 3，R 4和R 5之一表示磺酰氨基R 6 R 7 NSO 2 - ，其中R 6表示氢，C 1-6烷基，或C 1-4烷氧基C 1-4烷基; 并且R 7表示基团（R a）p-（Ar） - （CH 2）j - ，其中Ar表示苯基，萘基，5-或6-元杂环芳基或5-或6-元杂环芳基，稠合到苯环的多元杂环芳基; j表示0或1-4的整数; R a表示选自卤素，C 1-4烷基，C 1-4烷氧基，C 1-4烷氧基C 1-4烷基，硝基，氰基，三氟甲基，三氟甲氧基，羟基，羟基C 1-4烷基，C 1-4烷酰基，C 1-4烷氧基羰基，氨基，单 - 或 - 二-C 1-4烷基氨基，C 1-4烷硫基，C 1-4烷基亚磺酰基，C 1-4烷基磺酰基和苯基C 1-4烷氧基; p表示0或1-4的整数; 或R 6 R 7表示与5-位或者5-元杂环芳基取代的苯基稠合或取代的5-7元杂环，所述苯基或杂芳基为任选地被基团（R a）p取代，其中R a和p如上所定义; Y表示选自（a） - （e）的基团。其盐在多巴胺受体中具有活性，并且可用于治疗精神病如精神分裂症。

88. 发明申请

WO1995016448A1 PAROXETINE TABLETS AND PROCESS TO PREPARE THEM 审中-公开
标题翻译： PAROXETINE片剂及其制备方法
公开(公告)号：WO1995016448A1
公开(公告)日：1995-06-22
申请号：PCT/EP1994004164
申请日：1994-12-14
申请人： SMITHKLINE BEECHAM PLC , PATHAK, Ram, Dutta , DOUGHTY, David, George
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： A61K31/445
CPC分类号： A61K9/2095 , A61K31/445
摘要： Paroxetine which is formulated into tablets using a formulation process in which water is absent.
摘要翻译：使用其中不存在水的制剂方法将帕曲西汀制成片剂。

89. 发明申请

WO1995004729A1 AMIDE DERIVATIVES AS 5HT1D RECEPTOR ANTAGONISTS 审中-公开
标题翻译： AMT衍生物作为5HT1D受体拮抗剂
公开(公告)号：WO1995004729A1
公开(公告)日：1995-02-16
申请号：PCT/EP1994002492
申请日：1994-07-26
申请人： SMITHKLINE BEECHAM PLC , DUCKWORTH, David, Malcolm , JENKINS, Sarah, Margaret , JENNINGS, Andrew, John
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D295/14
CPC分类号： C07D213/82 , C07C2601/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/135 , C07D295/185 , C07D295/205 , C07D333/24 , C07D405/04 , C07D409/04
摘要： Novel amide derivatives, processes for their preparation, and pharmaceutical compositions containing them.
摘要翻译：新型酰胺衍生物，其制备方法和含有它们的药物组合物。

90. 发明申请

WO1995004037A1 2-(2-HYDROXYPHENYL)-5-(N-PHENYLMETHYL-AMINOMETHYL)-PYRROLES AS ANTIPSYCHOTIC AGENTS 审中-公开
标题翻译： 2-（2-羟基苯基）-5-（N-苯基甲基 - 氨基甲基） - 吡咯烷作为抗菌剂
公开(公告)号：WO1995004037A1
公开(公告)日：1995-02-09
申请号：PCT/EP1994002411
申请日：1994-07-21
申请人： SMITHKLINE BEECHAM PLC , STEMP, Geoffrey , JOHNSON, Christopher, Norbert
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D207/32
CPC分类号： C07D207/335
摘要： Phenylpyrrole derivatives of formula (I) with antipsychotic activity.
摘要翻译：具有抗精神病活性的式（I）的苯基吡咯衍生物。

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