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1. 发明申请

WO03031447A3 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：与PDE-V锁效果嘧啶衍生物
公开(公告)号：WO03031447A3
公开(公告)日：2003-08-28
申请号：PCT/EP0209935
申请日：2002-09-05
申请人： MERCK PATENT GMBH , EGGENWEILER HANS-MICHAEL , BAUMGARTH MANFRED , SCHELLING PIERRE , BEIER NORBERT , CHRISTADLER MARIA
发明人： EGGENWEILER HANS-MICHAEL , BAUMGARTH MANFRED , SCHELLING PIERRE , BEIER NORBERT , CHRISTADLER MARIA
IPC分类号： A61K31/519 , A61P1/00 , A61P1/04 , A61P1/14 , A61P1/16 , A61P7/00 , A61P7/04 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/08 , A61P13/12 , A61P15/12 , A61P19/10 , A61P27/06 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D487/04 , C07D491/04 , C07D491/048 , A61K31/505 , C07D495/04
CPC分类号： C07D487/04 , C07D491/04
摘要： Pyrimidine derivatives of formula (I) and the physiologically acceptable salts thereof, where R , R , R , R , W, X, Y and Z have the meanings given in claim 1, display a phosphodiesterase V inhibition and can be used for treatment of diseases of the coronary circulatory system and for treatment and/or therapy of potency disorders.
摘要翻译：式（I）的嘧啶衍生物和它们生理上可接受的盐，其中R1，R2，R3，R4，W，X，Y和Z具有权利要求1中，显示出磷酸二酯酶V抑制中给出的含义，并且可以用于治疗的心脏疾病 -Kreislaufsystems和用于治疗和/或效力病症的治疗。

2. 发明申请

WO1997023476A1 HETEROCYCLYL-CONDENSED BENZOYLGUANIDINES, THEIR PRODUCTION AND USE AS INHIBITORS OF THE CELLULAR Na+/H+-ANTIPORTER 审中-公开
标题翻译： HETEROCYCLYLKONDENSIERTE benzoylguanidines，生产及其作为细胞Na + / H +反向转运蛋白的抑制剂
公开(公告)号：WO1997023476A1
公开(公告)日：1997-07-03
申请号：PCT/EP1996005645
申请日：1996-12-16
申请人： MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG , BAUMGARTH, Manfred , GERICKE, Rolf , MINCK, Klaus-Otto , BEIER, Norbert
发明人： MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
IPC分类号： C07D333/64
CPC分类号： C07D333/54 , C07D333/62 , C07D333/64 , C07D333/66 , C07D333/68
摘要： Cyclic sulphones of formula (I) are disclosed, in which: R and R each independently of one another stand for H, A, CF3, CH2F, CHF2, C2F5, Hal, OH, OA, NH2, NHA, NA2, NO2 or CN; X stands for CR R , C=Z, O, S, NH, NA or NR ; Y stands for CR R , C=Z, O, NH, NA, or NR ; Z stands for O, S, NH, NA, NOH, NOA, CH2, CHA or CA2; R , R , R and R each independently of one another stand for H, A, R , Hal, OH, OA, SH, SA, NH2, NHA or NA2, or alternatively, R and R or R and R can together represent a bond, only one such bond being present in each molecule; R and R together can also stand for O-(CH2)2-O or O-(CH2)3-O; R and R each independently of one another stand for H or A; A stands for alkyl with 1-6 C atoms; Hal stands for F, Cl, Br or I; and R stands for phenyl or benzyl which is unsubstituted or single-, double- or triple-substituted by A, OA, NH2, NHA, NA2, F, Cl, Br and/or CF3; and n is 0 or 1. Also disclosed are the physiologically tolerable salts of these compounds. These compounds and their salts have anti-arrhythmic properties and act as inhibitors of the cellular Na+/H+-antiporter.
摘要翻译：式（I）其中，R <1>和R <2>各自独立地是H，A，CF 3，CH 2 F，CHF 2，C 2 F 5，哈尔，OH，OA，NH 2，NHA，NA2，NO 2或CN，X的环状砜 CR <4> - [R <5>，C = Z，O，S，NH，NA或NR <3>中，Y为CR <6> - [R <7>，C = Z，O，NH，NA或NR <3> 中，Z是O，S，NH，NA，NOH，NOA，CH 2，CHA或CA2，R <4>，R <5> - [R <6>和R <7>各自独立地是H，A，R <3>，哈尔，OH，OA，SH，SA，NH 2，NHA或NA2或者R <5>和R <6>或R <7>和R <8>在每一种情况下一起键，在每个分子中，最多只有一个这样的结合可以发生，R <4>和R <5>一起是可替代地-O-（CH 2）2 O或O-（CH2）3-O-，R <8>和R <9>各自独立为H或A，A 碳原子数1〜6的烷基中，Hal是F，Cl，Br或I和R <3>是未取代的或单 - ，二 - 或A，OA，NH 2，NHA，NA2，F，氯，溴三取代的和/或 CF 3 - 取代的苯基或苄基，n是0或1，以及它们的生理学可接受的盐表现出抗心率失常特性，并作为细胞的抑制剂 ARY的Na + / H +反向转运蛋白。

3. 发明申请

WO0030624A3 USE OF BENZOYLGUANIDINES FOR THE TREATMENT OF NON-INSULIN-DEPENDENT DIABETES MELLITUS 审中-公开
标题翻译：苯甲酰胍对治疗非胰岛素依赖性糖尿病的作用
公开(公告)号：WO0030624A3
公开(公告)日：2000-10-05
申请号：PCT/EP9908795
申请日：1999-11-16
申请人： MERCK PATENT GMBH , GERICKE ROLF , BAUMGARTH MANFRED , MINCK KLAUS , MESANGEAU DIDIER , DOARE LILIANE , KERGOAT MICHELINE
发明人： GERICKE ROLF , BAUMGARTH MANFRED , MINCK KLAUS , MESANGEAU DIDIER , DOARE LILIANE , KERGOAT MICHELINE
IPC分类号： C07D207/327 , A61K31/155 , A61K31/166 , A61K31/40 , A61K31/402 , A61P3/10 , A61P5/48 , C07C279/22
CPC分类号： A61K31/402 , A61K31/155
摘要： (57) Abstract The invention relates to the use of benzoylguanidines of formula (I) wherein R is A; R is Het, CnFmH2n+1-mOp, R , OR , OH, benzyl, CN, Hal, SOq-R , Ph, O-Ph, O-Het, NH-Het, NH2, NHA, NA2 or NH-Ph; R is SO2A'; R is a straight-chain or branched alkyl radical having 1 to 8 C atoms or cycloalkyl having 3 to 8 C atoms which can be unsubstituted or mono-, di- or trisubstituted by A; R is A or Ph; A, A' in each case independently of one another are alkyl having 1 to 6 C atoms, and/or their physiologically acceptable salts and solvates for the production of a medicament for the treatment of non-insulin-dependent diabetes mellitus.
摘要翻译：（57）摘要本发明涉及式（I）的苯甲酰基胍：其中R 1是A; R 2是Het，CnFmH 2n + 1-mOp，R 4，OR 4，OH，苄基，CN，Hal，SOq-R 5，Ph，O-Ph，O-Het，NH- Het，NH 2，NHA，NA 2或NH-Ph; R 3是SO 2 A'; R 4是具有1至8个C原子的直链或支链烷基或具有3至8个C原子的环烷基，其可以是未取代的或者被A单取代，二取代或三取代; R 5是A或Ph; A，A'在每种情况下彼此独立地为具有1至6个C原子的烷基，和/或其生理学上可接受的盐和溶剂合物用于制备用于治疗非胰岛素依赖性糖尿病的药物。

4. 发明申请

WO2005005389A2 MALONAMIDE DERIVATIVES 审中-公开
标题翻译：马来酰胺衍生物
公开(公告)号：WO2005005389A2
公开(公告)日：2005-01-20
申请号：PCT/EP2004/006573
申请日：2004-06-18
申请人： MERCK PATENT GMBH , BRUGE, David , BUCHSTALLER, Hans-Peter , WIESNER, Matthias , FINSINGER, Dirk , BAUMGARTH, Manfred , SIRRENBERG, Christian , ZENKE, Frank , AMENDT, Christiane , GRELL, Matthias
发明人： BRUGE, David , BUCHSTALLER, Hans-Peter , WIESNER, Matthias , FINSINGER, Dirk , BAUMGARTH, Manfred , SIRRENBERG, Christian , ZENKE, Frank , AMENDT, Christiane , GRELL, Matthias
IPC分类号： C07D213/00
CPC分类号： C07D213/66 , C07C233/15 , C07D213/38 , C07D213/68 , C07D213/75 , C07D213/79 , C07D213/81 , C07D261/14 , C07D413/12
摘要： The present invention relates to malonamide derivatives of formula (I): A-D-B, the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
摘要翻译：本发明涉及式（I）的丙二酰胺衍生物：ADB，式（I）化合物作为raf-激酶抑制剂的用途，式（I）化合物用于制备药物组合物和一种治疗方法，包括将所述药物组合物施用于患者。

5. 发明申请

WO2003031447A2 PYRIMIDINDERIVATE 审中-公开
标题翻译：嘧啶衍生物
公开(公告)号：WO2003031447A2
公开(公告)日：2003-04-17
申请号：PCT/EP2002/009935
申请日：2002-09-05
申请人： MERCK PATENT GMBH , EGGENWEILER, Hans-Michael , BAUMGARTH, Manfred , SCHELLING, Pierre , BEIER, Norbert , CHRISTADLER, Maria
发明人： EGGENWEILER, Hans-Michael , BAUMGARTH, Manfred , SCHELLING, Pierre , BEIER, Norbert , CHRISTADLER, Maria
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D491/04
摘要： Pyrimidinderivate der Formel (I) sowie deren physiologisch unbedenklichen Salze, worin R 1 , R 2 , R 3 , R 4 , W, X, Y und Z die in Anspruch 1 angegebenen Bedeutungen haben, zeigen eine Phosphodiesterase V-Hemmung und können zur Behandlung von Erkrankungen des Herz-Kreislaufsystems und zur Behandlung und/oder Therapie von Potenzstörungen eingesetzt werden.
摘要翻译：式（I）的嘧啶衍生物和它们生理上可接受的盐，其中，R <1>，R <2>，R <3>，R <4>中，W，X，Y和Z具有权利要求1中给出的含义，显示出磷酸二酯酶V抑制，并且可以用于治疗心血管系统的以及用于治疗和/或效力病症的治疗的疾病。

6. 发明专利

SK279095B6 CHROMAN DERIVATIVES FOR DISEASES TREATMENT, THE METHOD OF THEIR PRODUCTION, THEIR USE FOR PRODUCING THE MEDICAMENTS AND PHARMACEUTICAL COMPOSITIONS ON THEIR BASE 未知
公开(公告)号：SK279095B6
公开(公告)日：1998-06-03
申请号：SK367491
申请日：1991-12-04
申请人： GERICKE ROLF , BAUMGARTH MANFRED , LUES INGEBORG , HARTING JURGEN , BERGMANN ROLF
发明人： GERICKE ROLF , BAUMGARTH MANFRED , LUES INGEBORG , HARTING JURGEN , BERGMANN ROLF
IPC分类号： A61K31/35 , A61K31/395 , A61K31/435 , A61K31/443 , A61K31/4433 , A61K31/495 , A61K31/50 , A61K31/501 , A61K31/505 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/08 , A61P13/02 , A61P15/00 , C07D405/12
摘要： Chroman derivatives of common formula (I), where Rl and R2 always represent residue A; R3 stands for OH or OAc; R4 and R7 always stands for H; R3 and R4 altogether, as well, represents a bond; R8 and R9 always stands for H or A; R5 is oxodihydropyridyl or oxodihydropyridazinyl, which might be monosubstituted by residue A, R6 stands for cyano; A stands for alkyl with 1-6 C; Ac stands for acetyl, as well as their salts, whereas when Rl and R2 stands for methyl, R3 stands for OH, R4, R7, R8 and R9 is always H and R6 stands for 6-cyano, then R5 does not represent 3-oxo-2,3-dihydro-2-pyridyl, on their own and for diseases treatment, the method of their production, their use for producing the medicaments, and on their base derived pharmaceutical components. These derivatives effect the cardiovascular system and might be used in its medical treatment or prophylaxis of hearth insufficiency, angina pectoris, hypertension, incontinence and allopathy. They are prepared as follows: chroman of common formula (II), where X-Y are residuals of common formula (B) or -CHE-CR3R8- and E represents chlorine, bromine, iodine or reactive esterificated hydroxygroup and Rl, R2, R3, R6, R7 and R8 has the above stated meaning, reacts with the compound of common formula R5-NH-R9, where R5 and R9 have the above stated meaning, or by their reactive derivative and/or the compound of common formula (I) in which R3 stands for OH and R4 stands for H, is dehydrated and/or in the compound of common formula (I) i s, at least, one residue R3 and/or R5 tranformed to other residue R3 and/or R5, and/or basic compound of common formula (I) transforms to its additive salt with acid during the acid reaction.

7. 发明申请

WO2005005389A3 MALONAMIDE DERIVATIVES 审中-公开
标题翻译：马来酰胺衍生物
公开(公告)号：WO2005005389A3
公开(公告)日：2005-03-24
申请号：PCT/EP2004006573
申请日：2004-06-18
申请人： MERCK PATENT GMBH , BRUGE DAVID , BUCHSTALLER HANS-PETER , WIESNER MATTHIAS , FINSINGER DIRK , BAUMGARTH MANFRED , SIRRENBERG CHRISTIAN , ZENKE FRANK , AMENDT CHRISTIANE , GRELL MATTHIAS
发明人： BRUGE DAVID , BUCHSTALLER HANS-PETER , WIESNER MATTHIAS , FINSINGER DIRK , BAUMGARTH MANFRED , SIRRENBERG CHRISTIAN , ZENKE FRANK , AMENDT CHRISTIANE , GRELL MATTHIAS
IPC分类号： A61P35/00 , C07C233/15 , C07D213/38 , C07D213/66 , C07D213/68 , C07D213/75 , C07D213/79 , C07D213/81 , C07D261/14 , C07D413/12 , A61K31/44
CPC分类号： C07D213/66 , C07C233/15 , C07D213/38 , C07D213/68 , C07D213/75 , C07D213/79 , C07D213/81 , C07D261/14 , C07D413/12
摘要： The present invention relates to malonamide derivatives of formula A-D-B-1, as inhibitors of raf-kinase and the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition.
摘要翻译：本发明涉及作为raf-激酶抑制剂的式A-D-B-1的丙二酰胺衍生物和式（I）化合物在制备药物组合物中的应用。

8. 发明申请

WO2003097600A1 VERFAHREN ZUR HERSTELLUNG VON CYCLISCHEN IMIDEN IN GEGENWART VON POLYPHOSPHORSÄURE 审中-公开
标题翻译：用于在多存在下生产环酰亚胺
公开(公告)号：WO2003097600A1
公开(公告)日：2003-11-27
申请号：PCT/EP2003/003584
申请日：2003-04-07
申请人： MERCK PATENT GMBH , MEDERSKI, Werner , BAUMGARTH, Manfred , GERMANN, Martina , KUX, Dieter , WEITZEL, Thomas
发明人： MEDERSKI, Werner , BAUMGARTH, Manfred , GERMANN, Martina , KUX, Dieter , WEITZEL, Thomas
IPC分类号： C07D211/88
CPC分类号： C07D207/404 , C07D207/452 , C07D211/88
摘要： Die vorliegende Erfindung betrifft ein neues Verfahren zur Herstellung von N-substituierten cyclischen Imiden. N-substituierte cyclische Imide sind wertvolle Zwischenprodukte, die beispielweise zur Synthese pharmakologisch wertvoller Verbindungen eingesetzt werden können.
摘要翻译：本发明涉及一种用于制备N-取代的环状酰亚胺的新方法。 N-取代的环状酰亚胺是可用于药理学的有价值的化合物的合成中，例如有用的中间体。

9. 发明申请

WO2000066552A1 METHOD FOR PRODUCING A BENZOYLGUANIDINE DERIVATIVE 审中-公开
标题翻译：用于生产BENZOYLGUANIDINDERIVATES
公开(公告)号：WO2000066552A1
公开(公告)日：2000-11-09
申请号：PCT/EP2000003455
申请日：2000-04-17
申请人： MERCK PATENT GMBH , BAUMGARTH, Manfred , GERICKE, Rolf
发明人： MERCK PATENT GMBH
IPC分类号： C07D207/32
CPC分类号： C07D207/325 , C07C317/14
摘要： The invention relates to a method for producing the benzoylgaunidine derivative N- (diaminomethylene)- 2-methyl-5- (methyl-sulfonyl)-4- (pyrrol-1-yl)- benzamide of formula (I). This substance is an HHE-1 selective Na+¿/H+¿ antiport inhibitor.
摘要翻译：本发明涉及一种方法，用于生产Benzoylgaunidinderivates N-（二氨基亚甲基）-2-甲基-5-（甲磺酰基）-4-（吡咯-1-基） - （I）结构的苯甲酰胺。这种物质是一种NHE-1选择性的Na <+> / H <+> - 反向转运蛋白抑制剂。

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