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1.发明授权NON-IMIDAZOLE ALKYLAMINES AS HISTAMINE H 3?-RECEPTOR LIGANDS AND THEIR THERAPEUTIC APPLICATIONS 有权治疗用途组胺H3受体配体烷基胺中不含咪唑
公开(公告)号：EP1100503B1
公开(公告)日：2004-09-22
申请号：EP99941543.3
申请日：1999-07-29
发明人： SCHWARTZ, Jean-Charles , ARRANG, Jean-Michel , GARBARG, Monique , LECOMTE, Jeanne-Marie , LIGNEAU, Xavier , SCHUNACK, Walter, G. , STARK, Holger , GANELLIN, Charon, Robin , LEURQUIN, Fabien , SIGURD, Elz
IPC分类号： A61K31/4453 , A61K31/40 , A61K31/445 , A61K31/138
CPC分类号： C07D213/74 , A61K31/396 , A61K31/397 , A61K31/40 , A61K31/445 , A61K31/55 , C07B2200/07 , C07C217/16 , C07C217/20 , C07C217/22 , C07C251/48 , C07C255/54 , C07C2602/10 , C07D207/20 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/70 , C07D215/38 , C07D215/46 , C07D239/42 , C07D271/06 , C07D277/82 , C07D295/03 , C07D295/088 , C07D295/096 , C07D295/13 , C07D295/185
摘要： Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R?1 and R2¿ may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H¿3?-receptors of histamine.
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2.发明公开
公开(公告)号：EP0597088A1
公开(公告)日：1994-05-18
申请号：EP93914482.0
申请日：1993-01-08
发明人： SCHWARTZ, Jean-Charles , ARRANG, Jean-Michel, 160, av. du Général-Leclerc , GARBARG, Monique , LECOMTE, Jeanne-Marie , GANELLIN, Charon, Robin , TERTIUK, Wasyl 81 The Commons , SCHUNACK, Walter , LIPP, Ralph , STARK, Holger , PURAND, Katja
CPC分类号： C07D233/64 , C07D233/84 , C07D401/12 , C07D403/12 , C07D417/12
摘要： L'invention concerne des dérivés de l'imidazole répondant à la formule générale (IA) ou (IB). Procédés pour la préparation de ces composés et composition pharmaceutique les incorporant.
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3.发明公开
公开(公告)号：EP0482183A1
公开(公告)日：1992-04-29
申请号：EP91910312.0
申请日：1991-05-10
发明人： GARBARG, Monique , ARRANG, Jean-Michel 160 avenue du Général-Leclerc , SCHUNACK, Walter , LIPP, Ralph , STARK, Holger , LECOMTE, Jeanne-Marie , SCHWARTZ, Jean-Charles
CPC分类号： C07D233/64
摘要： Les composés proviennent d'une amine R-NH2 ayant une forte affinité pour le récepteur H3 de l'histamine et à la fonction amine primaire de laquelle est lié un groupe déterminant une liaison lentement hydrolysable en milieu neutre. Les compositions pharmaceutiques comprennent ces composés et un véhicule ou excipient pharmaceutiquement acceptable. Ces composés sont utilisés pour la réalisation d'un médicament inhibiteur de la synthèse et de la libération d'histamine, notamment à effets sédatifs, régulateur du sommeil, anticonvulsivant, antidépresseur, antiallergique, anti-inflammatoire, antisécrétoire ou antiulcéreux.
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4.发明公开NON-IMIDAZOLE ALKYLAMINES AS HISTAMINE H 3?-RECEPTOR LIGANDS AND THEIR THERAPEUTIC APPLICATIONS 有权治疗用途组胺H3受体配体烷基胺中不含咪唑
公开(公告)号：EP1100503A2
公开(公告)日：2001-05-23
申请号：EP99941543.3
申请日：1999-07-29
发明人： SCHWARTZ, Jean-Charles , ARRANG, Jean-Michel , GARBARG, Monique , LECOMTE, Jeanne-Marie , LIGNEAU, Xavier , SCHUNACK, Walter, G. , STARK, Holger , GANELLIN, Charon, Robin , LEURQUIN, Fabien , SIGURD, Elz
IPC分类号： A61K31/4453 , A61K31/40 , A61K31/445 , A61K31/138
CPC分类号： C07D213/74 , A61K31/396 , A61K31/397 , A61K31/40 , A61K31/445 , A61K31/55 , C07B2200/07 , C07C217/16 , C07C217/20 , C07C217/22 , C07C251/48 , C07C255/54 , C07C2602/10 , C07D207/20 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/70 , C07D215/38 , C07D215/46 , C07D239/42 , C07D271/06 , C07D277/82 , C07D295/03 , C07D295/088 , C07D295/096 , C07D295/13 , C07D295/185
摘要： Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R?1 and R2¿ may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H¿3?-receptors of histamine.
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公开(公告)号：EP0760811B1
公开(公告)日：2009-11-18
申请号：EP96908172.8
申请日：1996-03-21
发明人： SCHWARTZ, Jean-Charles , ARRANG, Jean-Michel , GARBARG, Monique , QUEMENER, Agnès , LECOMTE, Jeanne-Marie , LIGNEAU, Xavier , SCHUNACK, Walter, G. , STARK, Holger , PURAND, Katja , HÜLS, Annette , REIDEMEISTER, Sybille , ATHMANI, Salah , GANELLIN, Charon, Robin , PELLOUX-LEON, Nadia , TERTIUX, Wasyl , KRAUSE, Michael, C., O. , BASSEM, Sadek
IPC分类号： C07D233/64 , C07D409/12 , C07D401/12 , C07D405/12 , C07D411/12 , C07D413/12 , A61K31/415
CPC分类号： C07D233/56 , C07D233/64 , C07D405/12 , C07D409/12 , C07D411/12 , C07D413/12 , G01N33/567 , G01N33/74 , G01N2333/726
摘要： Novel imidazole derivatives as histamine receptor H3 antagonists and/or agonists, preparation thereof and therapeutical uses thereof. Chemical compounds for use as histamine receptor H3 agonists, partial agonists or antagonists, having general formula (Ia) or (Ib), the use thereof for making drugs, and methods for revealing the agonist, partial agonist or antagonist activity of such compounds in vivo, are disclosed.
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6.发明授权PROCEDE DE SYNTHESE ASYMETRIQUE DES DERIVES S-ACYLES DE L'ACIDE 2-MERCAPTOMETHYL 3-PHENYL PROPANOIQUE, APPLICATION A LA SYNTHESE DE DERIVES N-(MERCAPTOACYL) AMINO-ACIDES 失效程序对2-巯基-3-苯基及其用于合成N- mercaptoacyl氨基衍生物的S-酰化衍生物的不对称合成
公开(公告)号：EP0820439B1
公开(公告)日：2000-05-03
申请号：EP97904485.6
申请日：1997-02-04
发明人： DANVY, Denis , MONTEIL, Thierry , DUHAMEL, Pierre , DUHAMEL, Lucette , LECOMTE, Jeanne-Marie , SCHWARTZ, Jean-Charles , NOEL-LEFEBRVRE, Nadine , GROS, Claude , PLAQUEVENT, Jean-Christophe
IPC分类号： C07C327/32 , C07B53/00
CPC分类号： C07C29/149 , C07C59/48 , C07C327/32 , C07C33/26
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公开(公告)号：EP0760811A1
公开(公告)日：1997-03-12
申请号：EP96908172.0
申请日：1996-03-21
发明人： SCHWARTZ, Jean-Charles , ARRANG, Jean-Michel , GARBARG, Monique , QUEMENER, Agnès , LECOMTE, Jeanne-Marie , LIGNEAU, Xavier , SCHUNACK, Walter, G. , STARK, Holger , PURAND, Katja , HÜLS, Annette , REIDEMEISTER, Sybille , ATHMANI, Salah , GANELLIN, Charon, Robin , PELLOUX-LEON, Nadia , TERTIUX, Wasyl , KRAUSE, Michael, C., O. , BASSEM, Sadek
IPC分类号： G01N33 , A61K31 , A61P1 , A61P7 , A61P9 , A61P11 , A61P13 , A61P15 , A61P17 , A61P25 , A61P27 , A61P29 , A61P37 , A61P43 , C07D233 , C07D401 , C07D405 , C07D409 , C07D411 , C07D413
CPC分类号： C07D233/56 , C07D233/64 , C07D405/12 , C07D409/12 , C07D411/12 , C07D413/12 , G01N33/567 , G01N33/74 , G01N2333/726
摘要： Novel imidazole derivatives as histamine receptor H3 antagonists and/or agonists, preparation thereof and therapeutical uses thereof. Chemical compounds for use as histamine receptor H3 agonists, partial agonists or antagonists, having general formula (Ia) or (Ib), the use thereof for making drugs, and methods for revealing the agonist, partial agonist or antagonist activity of such compounds in vivo, are disclosed.
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8.发明公开PROCEDE DE SYNTHESE ASYMETRIQUE DES DERIVES S-ACYLES DE L'ACIDE 2-MERCAPTOMETHYL 3-PHENYL PROPANOIQUE, APPLICATION A LA SYNTHESE DE DERIVES N-(MERCAPTOACYL) AMINO-ACIDES 失效程序对2-巯基-3-苯基及其用于合成N- mercaptoacyl氨基衍生物的S-酰化衍生物的不对称合成
公开(公告)号：EP0820439A1
公开(公告)日：1998-01-28
申请号：EP97904485.0
申请日：1997-02-04
发明人： DANVY, Denis , MONTEIL, Thierry , DUHAMEL, Pierre , DUHAMEL, Lucette , LECOMTE, Jeanne-Marie , SCHWARTZ, Jean-Charles , NOEL-LEFEBRVRE, Nadine , GROS, Claude , PLAQUEVENT, Jean-Christophe
CPC分类号： C07C29/149 , C07C59/48 , C07C327/32 , C07C33/26
摘要： A method for the asymmetrical synthesis of S-acylated derivatives of 2-mercaptomethyl 3-phenyl propanoic acid of formula (I) is disclosed. The method comprises the steps of (a) preparing diol (VI) by reducing a malonic ester (V) in the presence of a hydride; (b) preparing respective monoacetates (VII R) or (VII S); (c) oxidising the monoacetates to give acids (IX S) or (IX R); (d) saponifying compounds (IX S) or (IX R) to form hydroxyacids (X S) or (X R); and (e) thioacylating hydroxyacids (X S) or (X R) with a mercaptoacid R1SH (XI) using a Mitsunobu reaction to give the desired acids (I R) or (I S), respectively. The method is useful for synthesising N-(mercaptoacyl) amino acids of formula (II).
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9.发明授权
公开(公告)号：EP0597088B1
公开(公告)日：2000-12-06
申请号：EP93914482.0
申请日：1993-01-08
发明人： SCHWARTZ, Jean-Charles , ARRANG, Jean-Michel, 160, av. du Général-Leclerc , GARBARG, Monique , LECOMTE, Jeanne-Marie , GANELLIN, Charon, Robin , FKYERAT, Abdellatif , TERTIUK, Wasyl 81 The Commons , SCHUNACK, Walter , LIPP, Ralph , STARK, Holger , PURAND, Katja
IPC分类号： C07D233/64 , C07D233/84 , C07D403/12 , C07D401/12 , C07D417/12 , A61K31/415
CPC分类号： C07D233/64 , C07D233/84 , C07D401/12 , C07D403/12 , C07D417/12
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10.发明授权COMPOSES AGONISTES DU RECEPTEUR H3 DE L'HISTAMINE A USAGE THERAPEUTIQUE, COMPOSITIONS PHARMACEUTIQUES AGISSANT COMME AGONISTES DUDIT RECEPTEUR ET PROCEDE DE PREPARATION 失效组胺H3受体激动剂对于治疗用途，药物制剂H3受体激动性的工作，他们介绍联合国的方法
公开(公告)号：EP0482183B1
公开(公告)日：1997-07-30
申请号：EP91910312.7
申请日：1991-05-10
发明人： GARBARG, Monique , ARRANG, Jean-Michel 160 avenue du Général-Leclerc , SCHUNACK, Walter , LIPP, Ralph , STARK, Holger , LECOMTE, Jeanne-Marie , SCHWARTZ, Jean-Charles
IPC分类号： C07D233/54 , A61K31/415
CPC分类号： C07D233/64
摘要： The compounds are derived from an R-NH2 amine with a strong affinity for the histamine H3-receptor and to the primary amine function of which is bonded a group forming a bond which can hydrolyze slowly in a neutral medium. The pharmaceutical compositions consist of these compounds and a pharmaceutically acceptable excipient. The compounds are used to produce a drug inhibiting histamine synthesis and release, and having, in particular, sedative, sleep regulating, anti-convulsive, anti-depressive, anti-allergic anti-inflammatory, anti-secretory or anti-ulcerous effects.
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