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91. 发明申请

WO1996031201A1 RATE-CONTROLLED TRANSDERMAL ADMINISTRATION OF RISPERIDONE 审中-公开
标题翻译：雷帕酮的速率控制转导管理
公开(公告)号：WO1996031201A1
公开(公告)日：1996-10-10
申请号：PCT/EP1996001421
申请日：1996-03-29
申请人： JANSSEN PHARMACEUTICA N.V. , MESENS, Jean, Louis
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： A61K09/70
CPC分类号： A61K9/7061 , A61K31/519
摘要： Medical patches for the rate-controlled transdermal administration of risperidone through intact skin for an extended period of time which comprise: (a) a drug reservoir (1) comprising risperidone (I) and a skin permeation enhancer (II) for risperidone in amounts sufficient to deliver (I) at a therapeutically effective rate for said extended period of time, and (b) a drug-impermeable backing (2); methods of treating patients with such patches; process of manufacturing such patches.
摘要翻译：用于通过完整皮肤进行速率控制的透皮给药利培酮的药物补片，其包括：（a）包含利培酮（I）的药物储存器（1）和用于利培酮的皮肤渗透增强剂（II），其量足够以治疗有效率递送（I）所述延长的时间段，和（b）药物不可渗透的背衬（2）; 治疗患有这种斑块的患者的方法; 制造这种贴片的过程。

92. 发明申请

WO1996020200A1 6-[TRIAZOLYL[3-(TRIFLUOROMETHYL)PHENYL]METHYL]-2-QUINOLINONES AND -QUINOLINETHIONES 审中-公开
标题翻译： 6- [三唑并[3-（三氟甲基）苯基]甲基] -2-喹啉酮和二氢化茚
公开(公告)号：WO1996020200A1
公开(公告)日：1996-07-04
申请号：PCT/EP1995005173
申请日：1995-12-21
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston , MABIRE, Dominique, Jean-Pierre , SANZ, Gérard, Charles
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： This invention is concerned with the compounds of formula (I), the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R is hydrogen, amino or C1-4alkyl; R is hydrogen, halo or C1-4alkyl; R is hydrogen, halo or C1-4alkyl; Y is O or S, and -X = X - is a bivalent radical having the formula: -N = CH- (a-1) or -CH = N- (a-2); compositions containing the same, and processes of preparing these compounds. It further relates to their use as a medicine, in particular their use as a medicine to treat keratinization disorders.
摘要翻译：本发明涉及式（I）化合物，其药学上可接受的酸加成盐及其立体化学异构形式，其中R 1是氢，氨基或C 1-4烷基; R 2是氢，卤素或C 1-4烷基; R 3是氢，卤素或C 1-4烷基; Y是O或S，-X 1 = X 2 - 是具有下式的二价基团：-N = CH-（a-1）或-CH = N-（a-2）; 含有它们的组合物，以及制备这些化合物的方法。它还涉及它们作为药物的用途，特别是它们作为治疗角质化障碍的药物的用途。

93. 发明申请

WO1996017787A1 SAFETY SCREW CAP FOR BOTTLE WITH DISPENSER 审中-公开
标题翻译：带分配器的瓶子安全螺帽
公开(公告)号：WO1996017787A1
公开(公告)日：1996-06-13
申请号：PCT/EP1995004817
申请日：1995-11-30
申请人： JANSSEN PHARMACEUTICA N.V. , WOUTERS, Alfons, Jeanne
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： B65D50/04
CPC分类号： B65D41/3438 , B01L3/0282 , B65D50/043
摘要： The present invention relates to a safety screw cap for bottleneck type containers associated with a dispensing device, and to an arrangement of bottle, dispenser and cap. The upper portion (4) of the cap proper has a smaller diameter than the lower portion (5), thus causing an external flange (14) extending radially from the dispensing device (13) to be tightly fitted on the rim of the bottleneck (3). The arrangement of bottle, dispenser and cap comprises a central stopper (17) the lower part of which fits in the bottleneck, the upper part (18) of which constitutes an annular flange jutting outwardly over the rim of the bottleneck and which is centrally perforated in order to accommodate the dispensing device (13), and assures that the flange (18) of the stopper and the flange (14) of the dispensing device are aligned coaxially, thus allowing the safety screw cap to be screwed onto the bottleneck without effort.
摘要翻译：本发明涉及一种用于与分配装置相关联的瓶颈式容器的安全螺帽，以及瓶，分配器和帽的布置。盖本体的上部（4）具有比下部（5）更小的直径，从而使从分配装置（13）径向延伸的外部凸缘（14）紧紧地装配在瓶颈的边缘上 3）。瓶子，分配器和盖子的布置包括一个中心塞子（17），其下部装配在瓶颈中，其上部（18）构成一个环形凸缘，该环形凸缘向外凸出在瓶颈的边缘上，为了容纳分配装置（13），并且确保止动件的凸缘（18）和分配装置的凸缘（14）同轴对准，从而允许将安全螺帽拧紧到瓶颈上，而不用费力。

94. 发明申请

WO1996015790A1 LUBELUZOLE INTRAVENOUS SOLUTIONS 审中-公开
公开(公告)号：WO1996015790A1
公开(公告)日：1996-05-30
申请号：PCT/EP1995004520
申请日：1995-11-16
申请人： JANSSEN PHARMACEUTICA N.V. , FRANÇOIS, Marc, Karel, Jozef , PEETERS, Jozef , HEYNS, Christiane, Grabiëlla, Gerardus, Maria
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： A61K31/445
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/02 , A61K47/26
摘要： A solution for intravenous administration containing lubeluzole or a pharmaceutically acceptable addition salt thereof, an isotonizing agent, water and acid and base substances to adjust the pH of the solution in the range from 2.5 to 3.6; processes of preparing the same.
摘要翻译：用于静脉内施用的溶液，其含有卢溴唑或其药学上可接受的加成盐，等渗剂，水和酸和碱物质，以将溶液的pH调节在2.5至3.6的范围内; 制备方法

95. 发明申请

WO1996010026A1 PHENYL-OXO-ALKYL-(4-PIPERIDINYL)BENZOATE DERIVATIVES 审中-公开
标题翻译：苯基 - 邻 - 烷基 - （4-哌啶基）苯甲酸酯衍生物
公开(公告)号：WO1996010026A1
公开(公告)日：1996-04-04
申请号：PCT/EP1995003690
申请日：1995-09-19
申请人： JANSSEN PHARMACEUTICA N.V. , HENDRICKX, Marie-Louis +hf , VAN DAELE, Kurt, Godfreid, Cornelius, Emile +hm , VAN DAELE, Peter, Jules, Victor +hm , VAN DAELE, Glenn, Kurt, Ludo +hm , BOSMANS, Jean-Paul, René, Marie, André , VERDONCK, Marc, Gustaaf, Celine
发明人： JANSSEN PHARMACEUTICA N.V. , HENDRICKX, Marie-Louis +hf , VAN DAELE, Kurt, Godfreid, Cornelius, Emile +hm , VAN DAELE, Peter, Jules, Victor +hm , VAN DAELE, Glenn, Kurt, Ludo +hm , VAN DAELE, Georges, Henri, Paul +di
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , C07D211/46 , C07D405/14
摘要： The present invention is concerned with novel benzoate derivatives having formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R is halo or C1-6alkylsulfonylamino; either R is hydrogen and R is C1-6alkyl, C2-6alkenyl or C2-6alkynyl; or R and R taken together form a bivalent radical of formula -CH=CH- (a), -(CH2)2- (b), or -(CH2)3- (c); in the bivalent radicals of formula (a), (b) or (c) one or two hydrogen atoms may be replaced by C1-6alkyl; Alk is C1-6alkanediyl; R is hydrogen or C1-6alkyloxy; R , R and R each independently are hydrogen, halo, C1-6alkyl, C1-6alkyloxy; or R and R taken together may also form a bivalent radical of formula: -NR C(O)NR -, -NH-C(NHR )=N-, -O-(CH2)m-O-; R and R each independently are hydrogen or C1-6alkyl; R is hydrogen, C1-6alkycarbonyl, C1-6alkyloxycarbonyl; m is 1 or 2. Pharmaceutical compositions comprising said compounds, processes for preparing compounds and compositions as well as the use as a medicine, in particular for the treatment of intestinal disorders involving a decreased colon motility are described.
摘要翻译：本发明涉及具有式（I）的新型苯甲酸酯衍生物，N-氧化物形式，其药学上可接受的酸加成盐及其立体化学异构形式，其中R 1为卤素或C 1-6烷基磺酰基氨基; R 2是氢，R 3是C 1-6烷基，C 2-6烯基或C 2-6炔基; 或R 2和R 3一起形成式-CH = CH-（a）， - （CH 2）2 - （b）或 - （CH 2）3 - （c）的二价基团; 在式（a），（b）或（c）的二价基团中，一个或两个氢原子可被C 1-6烷基取代; Alk是C1-6烷二基; R 4是氢或C 1-6烷氧基; R 5，R 6和R 7各自独立地为氢，卤素，C 1-6烷基，C 1-6烷氧基; 或R 5和R 6一起也可以形成下式的二价基团：-NR 8 C（O）NR 9 - ， - NH-C（NHR 10）= N-， -O-（CH2）MO-; R 8和R 9各自独立地为氢或C 1-6烷基; R 10是氢，C 1-6烷羰基，C 1-6烷氧基羰基; 描述了包含所述化合物的药物组合物，制备化合物和组合物的方法以及用作药物的用途，特别是用于治疗涉及降低结肠运动的肠道疾病。

96. 发明申请

WO1995005381A1 VASOCONSTRICTIVE SUBSTITUTED DIHYDROPYRANOPYRIDINES 审中-公开
标题翻译：血管内取代二氢吡啶类药物
公开(公告)号：WO1995005381A1
公开(公告)日：1995-02-23
申请号：PCT/EP1994002700
申请日：1994-08-12
申请人： JANSSEN PHARMACEUTICA N.V. , VAN LOMMEN, Guy, Rosalia, Eugène , FERNANDEZ-GADEA, Francisco Javier , ANDRES-GIL, José Ignacio , MATESANZ-BALLESTEROS, Maria Encarnacion
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D491/04
CPC分类号： C07D491/04
摘要： The present invention is concerned with compounds of formula (I), the pharmaceutically acceptable acid addition salts thereof, the N &cir& _-oxides thereof and the stereochemically isomeric forms thereof, wherein =a1-a2=a3-a4= is a bivalent radical of formula: =N-CH=CH-CH= (a); =CH-N=CH-CH= (b); =CH-CH=N-CH= (c); =CH-CH=CH-N= (d), wherein in said bivalent radicals one or two hydrogen atoms can be substituted by halo, hydroxy, C1-6 alkyl or C1-6 alkyloxy; R is hydrogen or C1-6 alkyl; R is hydrogen or C1-6 alkyl; R is hydrogen or C1-6 alkyl; Alk is C1-5 alkanediyl; Alk is C2-15 alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula (aa), wherein R is hydrogen, cyano, aminocarbonyl or C1-6 alkyl; R is hydrogen, C1-6 alkyl, C3-6 alkenyl or C3-6 alkynyl; R is hydrogen or C1-6 alkyl; or R and R taken together may form a bivalent radical of formula -(CH2)4- or -(CH2)5-. Pharmaceutical compositions, preparations and use as medicine are described.
摘要翻译：本发明涉及式（I）化合物，其药学上可接受的酸加成盐，其N-氧化物及其立体化学异构形式，其中= a1-a2 = a3-a4 =是式：= N-CH = CH-CH =（a）; = CH-N = CH-CH =（b）; = CH-CH = N-CH =（c）; = CH-CH = CH-N =（d），其中在所述二价基团中，一个或两个氢原子可以被卤素，羟基，C 1-6烷基或C 1-6烷氧基取代; R 1是氢或C 1-6烷基; R 2是氢或C 1-6烷基; R 3是氢或C 1-6烷基; Alk 1是C 1-5烷二基; Alk 2是C 2-15烷二基; Q是含有至少一个氮原子或式（aa）基团的五元或六元杂环，其中R 4是氢，氰基，氨基羰基或C 1-6烷基; R 5是氢，C 1-6烷基，C 3-6烯基或C 3-6炔基; R 6是氢或C 1-6烷基; 或R 5和R 6一起可以形成式 - （CH 2）4 - 或 - （CH 2）5 - 的二价基团。描述了作为药物的药物组合物，制剂和用途。

97. 发明申请

WO1995001924A1 CHILDPROOF DOSING DEVICE 审中-公开
标题翻译： CHILDPROOF剂量设备
公开(公告)号：WO1995001924A1
公开(公告)日：1995-01-19
申请号：PCT/EP1994002149
申请日：1994-06-30
申请人： JANSSEN PHARMACEUTICA N.V. , PUTTEMAN, Peter , WOUTERS, Alfons, Jeanne
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： B65D83/00
CPC分类号： A61J1/2096 , A61J1/2065 , G01F11/027
摘要： A childproof device (1) for holding and dispensing liquids, in particular medicines, that provides precise dosages of liquid, comprising a bottle (2), a cap (5) which is irremovable from the bottleneck (4), said cap being associated with a hollow cylinder (6) extending axially to near the bottle bottom (3) and a reciprocating dispenser comprising a barrel (8) and a plunger (9). The dispenser provides the only means of getting medicine out of the bottle since the cylinder associated with the cap prevents the contents of the bottle from being poured or shaken out. The device is easily assembled and can be stored, sold and used as supplied by the manufacturer.
摘要翻译：一种用于容纳和分配提供精确剂量的液体的液体的儿童防护装置（1），包括瓶（2），不能从瓶颈（4）排出的帽（5），所述帽与轴向延伸到瓶底（3）附近的中空圆筒（6）和包括筒（8）和柱塞（9）的往复式分配器。分配器提供将药物从瓶中取出的唯一方法，因为与帽相关联的圆筒防止瓶子的内容物倒出或摇动。该设备易于组装，可以由制造商提供存储，出售和使用。

98. 发明申请

WO1994029305A1 N-[[1-[4-(4-FLUOROPHENOXY)BUTYL]-4-PIPERIDINYL]-N-METHYLAMINO]-2-BENZOTHIAZOLOLS AS CLASS III ANTIARRHYTHMIC AGENTS 审中-公开
标题翻译： N-ÄÄ1-Ä4-（4-氟异戊氧基）丁基-4-哌啶基-L- N-甲基氨基-2-苯并噻唑醇作为III类抗生素
公开(公告)号：WO1994029305A1
公开(公告)日：1994-12-22
申请号：PCT/EP1994001849
申请日：1994-06-06
申请人： JANSSEN PHARMACEUTICA N.V. , HEYKANTS, Jozef, Jan, Pieter , BORGERS, Marcel, Jan, Maria , WILHELM, Doris
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： 2-[[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]methylamino]-benzothiaz ololes of formula (I), wherein R or R is hydroxy, the other variable always being hydrogen, and the pharmaceutically acceptable acid addition salts thereof. Novel compounds, pharmaceutical compositions, as well as their use as a class III antiarrhythmicum is disclosed.
摘要翻译：式（I）的2- [2- [4-（4-氟苯氧基）丁基] -4-哌啶基]甲基氨基] - 苯并噻唑，其中R 1或R 2是羟基，另一个变量总是氢及其药学上可接受的酸加成盐。公开了新型化合物，药物组合物及其作为III类抗心律失常药物的用途。

99. 发明申请

WO1994016710A1 TOPICAL KETOCONAZOLE COMPOSITIONS 审中-公开
标题翻译：局部酮康唑组合物
公开(公告)号：WO1994016710A1
公开(公告)日：1994-08-04
申请号：PCT/EP1994000092
申请日：1994-01-12
申请人： JANSSEN PHARMACEUTICA N.V. , FRANÇOIS, Marc, Karel, Josef , WOUTERS, Alfons, Jeanne , CAUWENBERGH, Gerard, Frans, Maria, Jan
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： A61K31/57
CPC分类号： A61K31/57 , Y10S514/887 , A61K31/495 , A61K2300/00
摘要： The present invention relates to a topical composition comprising ketoconazole, an acetonide glucocorticosteroid and a dermatologically acceptable carrier, characterized by a pH above 2.5 and below 6, and a method of preparing said composition.
摘要翻译：本发明涉及包含酮康唑，丙酮糖苷类糖皮质激素和皮肤病学上可接受的载体的局部组合物，其特征在于pH在2.5以上且低于6，以及制备所述组合物的方法。

100. 发明申请

WO1994010164A1 4-QUINOLINYL DERIVATIVES WITH ANTI-HELICOBACTER ACTIVITY 审中-公开
标题翻译：具有抗真菌活性的4-喹啉衍生物
公开(公告)号：WO1994010164A1
公开(公告)日：1994-05-11
申请号：PCT/EP1993002884
申请日：1993-10-19
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston , GUILLEMONT, Jérôme, Emiles, Georges , VERNIER, Daniel, Franck, Jean , ODDS, Franck, Christopher
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/06
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D401/06
摘要： The present invention is concerned with novel quinoline derivatives having anti-Helicobacter activity of formula (I), the pharmaceutically acceptable acid addition salts therof, the stereochemically isomeric forms thereof, the quaternized forms thereof and the N &cir& _-oxides thereof, wherein -A- represents a bivalent radical of formula: (a) -N=CH-CH=CH-, (b) -CH=N-CH=CH-, (c) -N=N-CH=CH-, (d) -N=CH-N=CH-, (e) -N=CH-CH=N-, (f) -CH=N-N=CH-, (g) -N=N-N=CH-, (h) -N=N-CH=N-, or (i) -CH=CH-CH=CH-; R , R , R , R , R , R and R each independently represent hydrogen, halo, hydroxy, C1-4alkyloxy, C1-4alkyl, trifluromethyl, amino, mono- or di(C1-4alkyl)- amio or nitro, provided that when one substituent on a phenyl group is a nitro then the other substituents on said phenyl group are other than nitro; novel compositions comprising said compunds, processes of preparing said compounds and compositions and methods for treating subjects suffering from disorders or afflictions associated with Helicobacter infection.
摘要翻译：本发明涉及具有式（I）的抗幽门螺杆菌活性的新型喹啉衍生物，其药学上可接受的酸加成盐，其立体化学异构形式，其季铵化形式及其N-氧化物，其中-A - 表示式（a）-N = CH-CH = CH-，（b）-CH = N-CH = CH-，（c）-N = N-CH = CH-的二价基团，（d） -N = CH-N = CH-，（e）-N = CH-CH = N-，（f）-CH = NN = CH-，（g）-N = NN = CH-，（h）-N = N-CH = N-，或（i）-CH = CH-CH = CH-; R 1，R 2，R 3，R 4，R 5，R 6和R 7各自独立地表示氢，卤素，羟基，C 1-4烷氧基，C 1-4烷基，三氟甲基，氨基，单 - 或二（C 1-4烷基） - 氨基或硝基，条件是当苯基上的一个取代基为硝基时，所述苯基上的其它取代基不是硝基; 包含所述组合物的新型组合物，制备所述化合物的方法和组合物以及治疗患有与幽门螺杆菌感染相关的病症或苦难的受试者的方法。

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