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1. 发明专利

ES2355045T3 PROCEDIMIENTO MEJORADO PARA LA PREPARACION DE LAS SALES DE 4-(BENCIMIDAZOLILMETILAMINO)-BENZAMIDAS. 未知
公开(公告)号：ES2355045T3
公开(公告)日：2011-03-22
申请号：ES06830756
申请日：2006-12-20
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA
发明人： HAUSHERR ARNDT , HAMM RAINER , SCHMITT HEINZ-PETER , WEYELL BJORN , SCHLARB KERSTIN , KOCH GUNTER , ZERBAN GEORG
IPC分类号： C07D235/14
摘要： Procedimiento para la preparación de una sal de una 4-(bencimidazol-2-ilmetilamino)-benzamidina opcionalmente sustituida, caracterizado porque (a) se condensa un diaminobenceno opcionalmente sustituido de manera correspondiente con ácido 2-[4-(1,2,4-oxadiazol-5-on-3-il)-fenilamino]-acético y (b) i) se hidrogena el producto, así obtenido, ii) opcionalmente se carbonila el grupo amidino, sin aislar previamente el producto intermedio de la hidrogenación, y iii) sin aislamiento previo del producto intermedio de la carbonilación se aísla la sal deseada.

2. 发明专利

AU2006326980B2 Improved process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides 未知
公开(公告)号：AU2006326980B2
公开(公告)日：2012-07-05
申请号：AU2006326980
申请日：2006-12-20
申请人： BOEHRINGER INGELHEIM INT
发明人： SCHLARB KERSTIN , HAUSHERR ARNDT , KOCH GUNTER , SCHMITT HEINZ-PETER , ZERBAN GEORG , HAMM RAINER , WEYELL BJORN
IPC分类号： C07D235/14
摘要： The invention relates to a process for preparing a salt of an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterised in that (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, b) i) the product thus obtained is hydrogenated, ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand and iii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

3. 发明专利

AU2005256424A1 Method for producing 4-(benzimidazolylmethylamino)-benzamidines 未知
公开(公告)号：AU2005256424A1
公开(公告)日：2006-01-05
申请号：AU2005256424
申请日：2005-06-18
申请人： BOEHRINGER INGELHEIM INT
发明人： KOCH GUNTER , SCHMITT HEINZ-PETER , ZERBAN GEORG , WEYELL BJORN , SCHLARB KERSTIN , HAMM RAINER , HAUSHERR ARNDT
IPC分类号： C07D271/07 , C07D271/06 , C07D401/12 , C07D413/14
摘要： Production of optionally substituted 4-(benzimidazol-2-ylmethylamino)-benzamidines (I) involves: (a) condensing an optionally substituted diaminobenzene (II) with 2-(4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino)-acetic acid (III); (b) hydrogenating the product (IV); and (c) optionally carbonylating the amidino group. The intermediates (III), 2-(4-(1,2,4-oxadiazol-5-on-3-yl)-aniline (V) and benzimidazole derivatives (IV') are new compounds. Independent claims are included for the following new intermediates: 2-(4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino)-acetic acid of formula (III), 2-(4-(1,2,4-oxadiazol-5-on-3-yl)-phenylaminomethyl)-benzimidazoles of formula (IV') and 2-(4-(1,2,4-oxadiazol-5-on-3-yl)-aniline of formula (V). R 1> : alkyl or cycloalkyl; R 2> : alkyl (optionally substituted (os) by cycloalkyl-(1-3C) alkyl, where the 1-3C alkyl is os by COOH or a group convertible in vivo to COOH); or NR 21>R 22>; R 21> : alkyl (os by COOH, alkoxycarbonyl, COOCH 2Ph, CONHSO 2T, CONHSO 2Ph, 'trifluorosulfonylamino' (sic), trifluorosulfonylaminocarbonyl' (sic), or 1H-tetrazolyl); 2-4C alkyl substituted (but not on the alpha -C adjacent to the N) by OH, -O-T-Ph, -NH-T-COOH, -NH-T-COOT, -N(T)-T-COOH or -N(T)-T-COOT; or piperidinyl (os by T); R 22> : H; alkyl; cycloalkyl (os by T); 3-6C alkenyl or 3-6C alkynyl (both with the unsaturated part not bonded directly to N); phenyl (os by F, Cl, Br, T or OT); or benzyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, thienyl or imidazolyl (all os by T); or NR 21>R 22> : 5-7 membered cycloalkyleneimino (os by COOH or (1-4C) alkoxycarbonyl and optionally fused with a benzene ring); T : 1-3C alkyl; alkyl groups have 1-6C and cycloalkyl groups 3-7C unless specified otherwise. [Image] ACTIVITY : Anticoagulant. MECHANISM OF ACTION : Thrombin inhibitor.

4. 发明专利

AU2006326979B2 Improved process for the preparation of 4-(benzimidazolylmethylamino)-benzamides and the salts thereof 未知
公开(公告)号：AU2006326979B2
公开(公告)日：2013-03-28
申请号：AU2006326979
申请日：2006-12-20
申请人： BOEHRINGER INGELHEIM INT
发明人： HAUSHERR ARNDT , KOCH GUNTER , ZERBAN GEORG , SCHMITT HEINZ-PETER , WEYELL BJORN , HAMM RAINER , SCHLARB KERSTIN
IPC分类号： C07D271/06 , C07D401/12 , C07D413/14
摘要： The invention relates to a process for preparing an optionally substituted 4-benzimidazol- 2-ylmethylamino)-benzamidine, characterised in that (a) an optionally correspondingly substituted diaminobenzene is condensed with 2 [4- (1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, (b) i) the product thus obtained is hydrogenated and ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand; as well as a process for preparing a salt of an optionally substituted 4(benzimidazol-2-ylmethylamino)-benzamidine, wherein (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, (b) the product thus obtained is hydrogenated, and (c) i) optionally the amidino group is carbonylated and ii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

5. 发明专利

AU2006326980A1 Improved process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides 未知
公开(公告)号：AU2006326980A1
公开(公告)日：2007-06-28
申请号：AU2006326980
申请日：2006-12-20
申请人： BOEHRINGER INGELHEIM INT
发明人： KOCH GUNTER , HAMM RAINER , HAUSHERR ARNDT , WEYELL BJORN , ZERBAN GEORG , SCHMITT HEINZ-PETER , SCHLARB KERSTIN
IPC分类号： C07D235/14
摘要： The invention relates to a process for preparing a salt of an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterised in that (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, b) i) the product thus obtained is hydrogenated, ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand and iii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

6. 发明专利

ZA200804030B IMPROVED PROCESS FOR THE PREPARATION OF 4-(BENZIMIDAZOLYLMETHYLAMINO)BENZAMIDES AND THE SALTS THEREOF 未知
公开(公告)号：ZA200804030B
公开(公告)日：2009-02-25
申请号：ZA200804030
申请日：2008-05-12
申请人： BOEHRINGER INGELHEIM INT
发明人： ZERBAN GEORG , HAUSHERR ARNDT , HAMM RAINER , KOCH GUNTER , SCHLARB KERSTIN , SCHMITT HEINZ-PETER , WEYELL BJORN
IPC分类号： C07D20060101
摘要： The invention relates to a process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterized in that (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, (b) i) the product thus obtained is hydrogenated and ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand; as well as a process for preparing a salt of an optionally substituted 4-(benzimidazol-2-ylmethylamino)-benzamidine, wherein (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, (b) the product thus obtained is hydrogenated, and (c) i) optionally the amidino group is carbonylated and ii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

7. 发明专利

AU2006326979A1 Improved process for the preparation of 4-(benzimidazolylmethylamino)-benzamides and the salts thereof 未知
公开(公告)号：AU2006326979A1
公开(公告)日：2007-06-28
申请号：AU2006326979
申请日：2006-12-20
申请人： BOEHRINGER INGELHEIM INT
发明人： SCHMITT HEINZ-PETER , HAUSHERR ARNDT , HAMM RAINER , ZERBAN GEORG , KOCH GUNTER , SCHLARB KERSTIN , WEYELL BJORN
IPC分类号： C07D271/06 , C07D401/12 , C07D413/14
摘要： The invention relates to a process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterized in that (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, (b) i) the product thus obtained is hydrogenated and ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand; as well as a process for preparing a salt of an optionally substituted 4-(benzimidazol-2-ylmethylamino)-benzamidine, wherein (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, (b) the product thus obtained is hydrogenated, and (c) i) optionally the amidino group is carbonylated and ii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

8. 发明专利

NZ569851A Improved process for the preparation of 4-(benzimidazolymethylamino)-benzamides and the salts thereof 未知
公开(公告)号：NZ569851A
公开(公告)日：2011-10-28
申请号：NZ56985106
申请日：2006-12-20
申请人： BOEHRINGER INGELHEIM INT
发明人： ZERBAN GEORG , HAUSHERR ARNDT , HAMM RAINER , KOCH GUNTER , SCHLARB KERSTIN , SCHMITT HEINZ-PETER , WEYELL BJORN
IPC分类号： C07D271/06 , C07D401/12 , C07D413/14
摘要： Disclosed is a process for preparing a salt of a 4-(benzimidazol-2-ylmethylamino)-benzamidine, wherein (a) a diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-5 acetic acid, (b) the product thus obtained is hydrogenated and isolated, and (c) i) the amidino group is carbonylated and ii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

9. 发明专利

SI1968949T1 IzboljĹˇani postopek za pripravo soli 4-(benzimidazolilmetilamino)-benzamidov 未知
公开(公告)号：SI1968949T1
公开(公告)日：2011-02-28
申请号：SI200630879
申请日：2006-12-20
申请人： BOEHRINGER INGELHEIM INT
发明人： ZERBAN GEORG , HAUSHERR ARNDT , HAMM RAINER , KOCH GUNTER , SCHLARB KERSTIN , SCHMITT HEINZ-PETER , WEYELL BJORN
IPC分类号： C07D235/00

10. 发明专利

MXPA06015210A METODO PARA LA PREPARACION DE 4-(BENCIMIDAZOLILMETILAMINO)-BENZAMIDINAS. 未知
公开(公告)号：MXPA06015210A
公开(公告)日：2007-03-15
申请号：MXPA06015210
申请日：2005-06-18
申请人： BOEHRINGER INGELHEIM INT
发明人： ZERBAN GEORG , HAUSSHERR ARNDT , SCHLARB KERSTIN , SCHMITT HEINZ-PETER , WEYELL BJORN , KOCH GUNTER , HAMM RAINER
IPC分类号： A61K31/4184 , A61P7/02 , C07D271/06 , C07D271/07 , C07D401/12 , C07D413/14
摘要： La invencion se relaciona con un metodo para la preparacion de una 4-benzimidazol-2-ilmetilamino)-benzamidina eventualmente sustituida, caracterizado porque (a) un diaminobenceno eventualmente sustituido de forma correspondiente se condensa con acido 2-[4-(1,2,4-oxadiazol-5-on-3-il)-fenilamino]-acetico, (b) el producto asi obtenido se hidrogena y (c) el grupo amidino eventualmente se carbonila.

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