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1. 发明申请

WO1995005358A1 USE OF PHENOLS AND PHENOL DERIVATES AS MEDICAMENTS WITH FIBRINOGEN-REDUCING EFFECT 审中-公开
标题翻译：使用酚，苯酚衍生物与影响FIBRINOGENSENKENDER药物
公开(公告)号：WO1995005358A1
公开(公告)日：1995-02-23
申请号：PCT/EP1994002709
申请日：1994-08-13
申请人： BOEHRINGER MANNHEIM GMBH , WITTE, Ernst-Christian , STEGMEIER, Karlheinz , DOERGE, Liesel
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07C233/73
CPC分类号： C07C271/58 , C07C39/15 , C07C43/23 , C07C59/68 , C07C59/88 , C07C217/58 , C07C217/60 , C07C217/84 , C07C233/73 , C07C235/38 , C07C235/46 , C07C235/56 , C07C255/13 , C07C255/54 , C07C255/56 , C07C259/06 , C07C271/10 , C07C271/44 , C07F9/3808
摘要： Phenols and phenol derivatives having the general structural formula (I) are used to produce medicaments with fibrinogen-reducing effect. Also disclosed are new phenols and phenol derivatives, a process for producing the same and medicaments containing these compounds. In the formula, R stands for hydrogen or one to three substituents selected independently from each other from the halogen, C1-C4-alkyl, C1-C4-alkoxy, hydroxy, cyano oder trifluoromethyl series; B stands for a saturated or unsaturated alkylene chain with up to 6 C atoms substituted or not by one or two methyl groups in any desired position. One of the saturated C atoms may be substituted by an oxygen atom or by one of the groups >NH, >C=O oder >CH-OH, and two adjacent saturated C atoms may also be substituted together by a group -CONH- or -NHCO-. X is in a meta- or para-position in relation to B and stands for the following groups: a hydroxy group or a C1-C4-alkylurethane or substituted or non-substituted phenylurethane group derived from the hydroxy group; an unbranched or a C1-C6-alkyloxy, omega-hydroxy-C2-C6-alkyloxy, omega-halogen-C2-C6-alkyloxy or omega-cyano-C1-C6-alkyloxy group substituted by one or two methyl groups in any desired position; a C1-C4-alkyl urethane, a substituted or non-substituted phenyl urethane, phosphoric acid ester, aliphatic carboxylic acid ester grouping or a possibly substituted benzoic acid ester grouping derived from the omega-hydroxy-C2-C6-alkoxy group; an aminocarbonyl-C1-C6-alkoxy or a N-hydroxy-aminocarbonyl-C1-C6-alkoxy group; carboxymethoxy, 1-carboxy-ethoxy, 1-carboxy-propyloxy or 3-carboxy-propyloxy; the residue -O-C-(CH3)2-CH2-O-CO-(CH2)2-COOH; the possibly substituted benzoyloxy residue.
摘要翻译：本发明涉及使用用于制备药物的用效果fibrinogensenkender结构通式（I）的酚和酚衍生物。本发明还提供了新的酚和酚衍生物，它们的制备方法和药物组合物含有该化合物中，R是氢或1至三个卤素独立地选择的取代基，C1-C4烷基，C1-C4烷氧基，羟基，氰基或三氟甲基; B是具有至多六个碳原子，其中所述饱和碳原子中的一个可被氧原子取代或由以下基团之一为未取代的或任选被一个或两个甲基在取代的任何位置象征的，饱和或不饱和的亚烷基链> NH，> C = O或> CH-OH，并且两个相邻的饱和碳原子，也可以通过共同的基团代替-CONH-或-NHCO-; 且X是相对于间位或对位B和以下基团：羟基或从C1-C4-Alkylurethan-衍生或取代或未取代Phenylurethangruppe的基团; 无支链的或在任意位置C1-C6 Alkyloxyomega羟基C2-C6烷氧基被一个或两个甲基取代，ω-卤代 - C2-C6烷氧基或ω-氰基C1-C6烷氧基; ω-羟基C2-C6烷氧基衍生的C1-C4 Alkylurethan-之一，取代或未取代Phenylurethan-，磷酸酯，脂族羧酸酯，或任选被取代的，Benzoesäureestergruppierung; 氨基羰基-C 1 -C 6 - 烷氧基 - ，或N-羟基氨基羰基-C 1 -C 6 - 烷氧基; 羧基甲氧基，1-羧基乙氧基，1-羧基丙氧基或3-羧基丙氧基; 自由基-O-C（CH3）2-CH2-O-CO-（CH2）2-COOH; 其是任选取代的苯甲酰氧基。

2. 发明申请

WO1992011234A1 NOVEL AMINES, PROCESS FOR PRODUCING THEM AND MEDICAMENTS CONTAINING SAID COMPOUNDS 审中-公开
标题翻译：新陈代谢，生产其含有化合物的药物和方法
公开(公告)号：WO1992011234A1
公开(公告)日：1992-07-09
申请号：PCT/EP1991002456
申请日：1991-12-19
申请人： BOEHRINGER MANNHEIM GMBH , WITTE, Ernst-Christian , BECKH, Hansjörg , STEGMEIER, Karlheinz , DOERGE, Liesel
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07C311/00
CPC分类号： C07D295/185 , C07C311/17 , C07C311/18 , C07C2601/14
摘要： Compounds of formula (I), in which: R1 is an aryl, aralkyl or an aralkenyl group, the aryl radical of which may be singly or multiply substituted by halogen, cyanogen, alkyl, trifluoromethyl, alkoxy, alkylthio, trifluoromethoxy, hydroxy or carboxy; m is a whole number from 1 to 3; n is an integer from 1 to 5; R2 is hydrogen, an alkyl, aralkyl or acyl group; Q is a bond or an aoxygen atom; R3 is hydrogen or a low alkyl group which may be substituted in the terminal position by carboxyl or a hydroxy group; and R4 is hydrogen, a low alkyl group with 1 to 4 C atoms, which may be substituted in the terminal position by carboxyl or hydroxyl, a possibly substituted phenyl, heteroaryl, cycloalkyl or acyl group or a (a) group; in which R5 is a straight or branched alkyl chain with 1 to 4 C atoms, which may be substituted in the terminal position by carboxyl, alkoxycarbonyl, aminocarbonyl, hydroxy, mercapto, alkylthio or imidazolyl; and Y is a carboxy, alkoxycarbonyl, aminocarbonyl or cyano, formyl, hydroxymethyl, aminomethyl or orthoester group; whereby R3 and R4 may be a component of a 5 or 6-member saturated or unsaturated, possibly substituted heterocycle with 1 to 4 hetero atoms, which may be annulated with further annular compounds via one or more bonds; and their salts, esters and amides, process for producing them and medicaments with counterthromboxane effect containing these compounds.

3. 发明申请

WO1997036899A1 NOVEL OXAZOLIDINE DERIVATIVES, PROCESS FOR THEIR PRODUCTION AND MEDICAMENTS CONTAINING THEM 审中-公开
标题翻译：新恶唑烷，方法为生产和药物含有它们的
公开(公告)号：WO1997036899A1
公开(公告)日：1997-10-09
申请号：PCT/EP1997001542
申请日：1997-03-26
申请人： BOEHRINGER MANNHEIM GMBH , TSAKLAKIDIS, Christos , DOERGE, Liesel
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： The present invention relates to novel oxazolidine derivatives, a process for their production and medicaments containing said substances. The object of the present invention are compounds of the general formula (I) in which the symbols have the meanings given in the claims.
摘要翻译：本发明涉及新的恶唑烷衍生物，它们的制备方法和含有这些物质的药物组合物。本发明涉及通式（I），其中，所述符号具有如在权利要求中所列的含义的化合物。

4. 发明专利

CA2032570A1 PHENOXYALKYLCARBOXYLIC ACID AMIDES, PROCESSES FOR THE PREPA RATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：CA2032570A1
公开(公告)日：1991-06-24
申请号：CA2032570
申请日：1990-12-18
申请人： WITTE ERNST CHRISTIAN , STEGMEIER KARLHEINZ , DOERGE LIESEL
发明人： WITTE ERNST-CHRISTIAN , STEGMEIER KARLHEINZ , DOERGE LIESEL
IPC分类号： C07D233/64 , A61K31/195 , A61K31/225 , A61P7/02 , A61P43/00 , C07C311/17 , C07C323/59 , C07D207/16 , C07C311/19 , A61K31/395 , C07C311/51 , C07C323/67
摘要： The present invention provides compounds of the general formula : (I) in which the sulphonylaminoalkyl radical is in the ortho-, meta- or para-position to the phenoxyalkylcarbonamide radical and in which R1 is an aryl, aralkyl or aralkenyl radical, the aryl moiety of which can, in each case, be substituted one or more times by halogen, cyano, alkyl, trifluoromethyl or alkoxy, R2 is a hydrogen atom or an alkyl or acyl radical, R3 and R4, which can be the same or different, are hydrogen atoms or lower alkyl radicals, n is 1, 2 or 3, R6 is a hydrogen atom or an alkyl radical containing 1 to 4 carbon atoms which is optionally terminally substituted by carboxyl, aminocarbonyl or alkoxycarbonyl, by alkylthio, hydroxyl, phenyl or by imidazol-4-yl and R5 is a hydrogen atom or, together with R6, forms an alkylene chain containing 3-or 4 carbon atoms, as well as the physiologically acceptable salts, esters, amides and optical isomers thereof; the compounds may be used in the treatment of heart and circulatory diseases.

5. 发明申请

WO2008052718A1 VERFAHREN UND VORRICHTUNGEN ZUR ELEKTROCHEMISCHEN BESTIMMUNG VON FAKTOR XA-INHIBITOREN IN BLUTPROBEN 审中-公开
标题翻译：方法和设备电化学测定Xa因子抑制剂在血液样本
公开(公告)号：WO2008052718A1
公开(公告)日：2008-05-08
申请号：PCT/EP2007/009347
申请日：2007-10-27
申请人： ROCHE DIAGNOSTICS GMBH , F. HOFFMANN-LA ROCHE AG , HORN, Carina , DOERGE, Liesel , KRZYSIUK, Margarete
发明人： HORN, Carina , DOERGE, Liesel , KRZYSIUK, Margarete
IPC分类号： C12Q1/56 , G01N33/86
CPC分类号： G01N27/26 , C12Q1/005 , C12Q1/56 , G01N33/86
摘要： Die Erfindung betrifft Verfahren und Vorrichtungen zur Bestimmung von Faktor Xa-Inhibitoren, insbesondere von Heparinen und fraktionierten oder niedermolekularen Heparinen sowie direkten FXa-Inhibitoren, in Blutproben, welche dadurch gekennzeichnet sind, dass in einem ersten Schritt die Blutprobe mit einem Nachweisreagenz, welches zumindest ein Thrombinsubstrat, welches aus einem durch Thrombin abspaltbaren Peptidrest besteht, der über das Carboxylende amidisch an eine elektrogene Substanz gebunden ist, enthält, und mit einer bekannten Menge von Faktor X-Reagenz und einem Aktivator-Reagenz, welche die Umwandlung von Faktor X in Faktor Xa hervorruft, in Kontakt gebracht wird, anschließend in einem zweiten Schritt die Menge oder Aktivität der elektrogenen Substanz, welche durch die Faktor Xa- vermittelte Thrombinaktivierung vom Thrombinsubstrat abgespalten wird, und/oder deren zeitlicher Verlauf als Messsignal mit elektrochemischen Methoden bestimmt wird, und schließlich in einem dritten Schritt anhand dieses Messsignals die Menge des Faktor Xa-Inhibitors in der Probe des zu untersuchenden Blutes oder eine damit korrelierende Messgröße, insbesondere eine damit korrelierende Gerinnungszeit, ermittelt wird.
摘要翻译：本发明特别涉及的肝素和分级分离的或低分子量肝素和血液样品，其中所述血液样品的特征在于在第一步骤中与检测试剂包含至少一个直接的FXa抑制剂为因子Xa抑制剂的测定方法和装置，包含凝血酶，其通过经由羧基末端amidically键合到电的物质，并与因子X试剂的已知量和活化剂的试剂，因子X转化为因子Xa凝血酶肽残基包括一个可切割的原因被带入接触，然后在第二步骤中的量或通过因子Xa介导的凝血酶物质生电的活性是通过凝血酶裂解，和/或它的时间过程被确定为与电化学方法的测定信号，最后在一个博士基于该测量信号伊顿步骤，因子Xa抑制剂的血液样品中的量要测试或测量的变量与其相关联，特别是与其相关凝血时间被确定。

6. 发明申请

WO9624581A2 NEW DERIVATIVES OF PYRIDIL PIPERAZINE OR PYRIDAZINYL PIPERAZYL, PROCESS FOR PRODUCTION THEREOF AND MEDICAMENTS CONTAINING THESE COMPOUNDS 审中-公开
标题翻译：新的吡啶基或哒嗪基，哌嗪衍生物，其制造方法相同，并且含药物
公开(公告)号：WO9624581A2
公开(公告)日：1996-08-15
申请号：PCT/EP9600524
申请日：1996-02-08
申请人： BOEHRINGER MANNHEIM GMBH , TSAKLAKIDIS CHRISTOS , MERTENS ALFRED , ZIMMERMANN GERD , SCHAEFER WOLFGANG , DOERGE LIESEL
发明人： TSAKLAKIDIS CHRISTOS , MERTENS ALFRED , ZIMMERMANN GERD , SCHAEFER WOLFGANG , DOERGE LIESEL
IPC分类号： C07D237/20 , A61K31/495 , A61K31/50 , A61P7/02 , C07D213/74 , C07D , A61K
CPC分类号： C07D213/74
摘要： Compounds of formula (I), in which R stands for hydrogen, lower alkyl, lower alkenyl, cycloalkyl, cycloalkenyl, a possibly substituted mono-or bi-cyclic aryl, a possibly substituted hetaryl, a possibly substituted aryl alkyl or one of the groups -OR , -NR R , W stands for nitrogen or -CR , X, Z independently of each other stands for nitrogen or -CH, and where W stands for a nitrogen atom, X must be the group -CH, A stands for a valency bond or the carbonyl group, B stands for a valency bond or a C1-C6 alkyl chain possibly substituted once or several times by lower alkyl or an OR group, D stands for a valency bond, and, where X is a nitrogen atom, can also be the carbonyl group, A, B and D being unable to represent the valency bond simultaneously, R stands for hydrogen, lower alkyl or aryl alkyl, R , R independently of each other stand for hydrogen or lower alkyl, or form a five- or six-membered heterocyclic ring together with the nitrogen atom to which they are linked, R stands for hydrogen or a group OR . The invention also relates to a process for the production of these compounds, and medicaments containing them for the treatment of diseases which are attributable to thromboembolic conditions.
摘要翻译：式（I），其中R <1>是氢，低级烷基，低级烯基，环烷基，环烯基的化合物，任选取代的单环或双环芳基，任选取代的杂芳基，任选取代的芳基烷基或以下基团之一-OR < 2>，-NR <3> [R <4>中，W为氮或-CR <5>，X，Z独立地为氮或-CH，以及用于其中W代表氮原子的情况下，X为基团 - 一个必须是CH，表示价键或羰基，B代表被低级烷基或一个或或多取代C1-C6亚烷基链价键或任选的单 - <2>基，D表示化合价键，并且在壳体在于X是氮原子，也可以是羰基，其中A，B和D不能同时意味着价键，R <2>是氢，低级烷基或芳烷基，R <3>，R <4>独立地是氢，或妮 ederes烷基，或与氮原子一起形成它们所连接形成五至六元杂环，R <5>是氢或基团或<2>，它们的制备方法和含有这些化合物的药物组合物用于治疗疾病的那是由于血栓栓塞事件。

7. 发明申请

WO1994002128A1 USE OF 'alpha',w DICARBOXYLIC ACIDS AS FIBRINOGEN REDUCERS 审中-公开
标题翻译：阿尔法运用，瓦特 - 二羧酸如FIBRINOGENSENKER
公开(公告)号：WO1994002128A1
公开(公告)日：1994-02-03
申请号：PCT/EP1993001894
申请日：1993-07-17
申请人： BOEHRINGER MANNHEIM GMBH , PILL, Johannes , DOERGE, Liesel , STEGMEIER, Karlheinz
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： A61K31/20
CPC分类号： A61K31/20
摘要： Compounds of (alpha),w dicarboxylic acids of formula (I) in which X and Y, which may be the same or different, are hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, hydroxy, cyano, carboxyl, C1-C6-alkoxycarbonyl or carbamoyl, R1 and R2, which may the same or different, are hydrogen or C1-C6-alkyl, and Q is a linear saturated or unsaturated alkylene chain with 2-14 C atoms in which one or more C atoms may be replaced by cyclohexyl rings, phenyl or heterocycles, and their (in vivo) hydrolysable carboxylic acid derivatives for the production of medicaments with a fibrinogen reducing effect.

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