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1.发明公开COMPOSES TRICYCLIQUES, LEUR PROCEDE DE PREPARATION ET LES INTERMEDIAIRES DE CE PROCEDE, LEUR APPLICATION A TITRE DE MEDICAMENTS ET LES COMPOSITIONS PHARMACEUTIQUES LES RENFERMANT 有权DREIRINGIGE化合物的方法，为自己的产品，这个过程之间，其应用药物和你的药物组合物含
公开(公告)号：EP1017680A1
公开(公告)日：2000-07-12
申请号：EP98945362.6
申请日：1998-09-23
发明人： CARNIATO, Denis , GADEK, Thomas, R. , GOURVEST, Jean-François , KNOLLE, Jochen , McDOWELL, Robert , PEYMAN, Anuschirwan
IPC分类号： C07D233/52 , C07D233/50 , C07D239/18 , C07D239/14 , C07D401/12 , C07D407/12 , C07C69/76 , C07C69/003 , C07C65/40 , C07C235/84 , C07C271/22 , A61K31/415 , A61K31/505
CPC分类号： C07D239/42 , C07D233/52 , C07D401/12 , C07D405/12
摘要： The invention concerns products of formula (I) in which R1 represents -CONH - [A] - [B] -COR6, [A], [B]; R2, R3, R4, R5 and G are as defined in the description, and their salt additives with acids, bases and esters, the method for preparing them and the intermediates of said method, their application as medicines and the pharmaceutical compositions containing them.
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2.发明公开DERIVES D'HYDRAZONO-BENZAZULENE, COMPOSITIONS PHARMACEUTIQUES ET INTERMEDIAIRES 有权肼基benzazulene衍生物，药物组合物和中间产品
公开(公告)号：EP1017681A1
公开(公告)日：2000-07-12
申请号：EP98945363.4
申请日：1998-09-23
发明人： CARNIATO, Denis , GADEK, Thomas, R. , GOUBET, François , GOURVEST, Jean-François , KNOLLE, Jochen , MCDOWELL, Robert , SCHEUNEMANN, Karl-Heinz
IPC分类号： C07D233/52 , A61K31/415 , C07C49/747 , C07C333/04 , C07C323/22
CPC分类号： C07C333/04 , C07C49/747 , C07C323/22 , C07D233/52
摘要： The invention concerns products of formula (I) in which R1 represents S(O)X-[A]-[B]-COR6, x being equal to 0, 1 or 2; [A]- representing a bivalent radical derived from an aliphatic hydrocarbon, linear or branched, saturated or unsaturated, comprising 1 to 12 carbon atoms; [B] representing a phenyl radical, a CH(Z) radical or a single bond; G represents, either a radical of formula (G1) in which (Het') is a heterocycle of general formula (a), in which (H) forms, with the structural unit N=C-NH-, the residue of an aromatic or non-aromatic heterocycle, monocyclic or bicyclic, saturated or unsaturated, comprising 1 to 9 carbon atoms and 2 to 5 heteroatoms selected among oxygen, nitrogen or sulphur atoms, or a NRaRb radical (radical G2), or a (Het) radical (radical G3), or a -NRh-C(=X)-NHRc radical (radical G4), in which X is a sulphur, oxygen or NH atom, or a -NRh-SO2Rc radical (radical G5), and their additive salts with acids, bases and esters, the method for preparing them and the intermediates of said method, their application as medicines and the pharmaceutical compositions containing them.
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3.发明公开COMPOSES TRICYCLIQUES AYANT UNE ACTIVITE VIS-A-VIS DES INTEGRINES NOTAMMENT VIS-A-VIS DE L'INTEGRINE ALPHA vBETA3, LEUR PROCEDE DE PREPARATION ET LES INTERMEDIAIRES DE CE PROCEDE, LEUR APPLICATION A TITRE DE MEDICAMENTS ET LES COMPOSITIONS PHARMACEUTIQUES LES RENFERMANT 失效WITH EFFECT含有TRIZYCLISCHE TIES ON整特别是在素αVβ3整联蛋白，制备方法以及诉讼的中间产品，它们的使用药物和YOU药物组合物
公开(公告)号：EP0888292A1
公开(公告)日：1999-01-07
申请号：EP97915519.0
申请日：1997-03-20
发明人： BERNARD, Serge , CARNIATO, Denis , GOURVEST, Jean-François , TEUTSCH, Jean-Georges , KNOLLE, Jochen , STILZ, Hans-Ulrich , WEHNER, Volkmar , BODARY, Sarah, C. , GADEK, Thomas, R. , MCDOWELL, Robert, S. , PITTI, Robert, M.
CPC分类号： C07D239/18 , C07C45/516 , C07C45/63 , C07C45/673 , C07C45/71 , C07C49/747 , C07C49/755 , C07C281/12 , C07C281/18 , C07C331/04 , C07C331/10 , C07C331/12 , C07C331/14 , C07C337/08 , C07C2603/30 , C07D233/52 , Y02P20/55 , C07C49/753
摘要： Compounds of formula (I), wherein R1, R2, R3, R4, R5 and G are as defined in the description and the dotted lines indicate an optional second bond, as well as the acid, base and ester addition salts thereof, a method for preparing said compounds, intermediates therefor, the use of said compounds as drugs, and pharmaceutical compositions containing same, are disclosed.
摘要翻译： 本发明的主题是式（I）的产品：其中被作为在说明书中定义R1，R2，R3，R4，R5和G中，虚线表示在可选的第二个键，以及与所述的加成盐 酸和碱及酯，其制备过程，这个过程的中间体，它们作为药物和包含它们的药物组合物。
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公开(公告)号：EP0865446A1
公开(公告)日：1998-09-23
申请号：EP96942315.0
申请日：1996-12-06
发明人： KITAMURA, Kazuyuki , KOMIYAMA, Osamu , INAZU, Mizuho , BARON, Roland , GADEK, Thomas , KNOLLE, Jochen , STILZ, Han-Ulrich , WEHNER, Volkmar , MCDOWELL, Robert, S.
CPC分类号： C07K5/0821 , A61K38/04 , A61K38/05 , A61K38/07 , A61K38/12 , A61K38/1703 , A61K38/39 , C07C271/22 , C07C279/08 , C07C279/20 , C07K5/0202 , C07K5/0817 , C07K5/1019 , C07K5/1024 , C07K14/46 , C07K14/745 , C07K14/78
摘要： The object is to provide a promoting agent for bone formation, a therapeutic method for bone formation and a process for preparing a promoting agent for bone formation. A promoting agent for bone formation which comprises at least one of kistrin, echstatin, a peptide or polypeptide containing the amino acid sequence ArgGlyAsp in the molecule such as a peptide represented by Gly-Arg-Gly-Asp-Ser or a compound represented by general formula (IX) and so on, as well as a biologically acceptable salt thereof, wherein R16 represents -N(R20)2 (R20 represents a hydrogen atom or a C1-C4 alkyl group), R17 represents a hydrogen atom or a C1-C4 alkyl group, R18 represents a hydrogen atom, a C1-C4 alkyl group and so on, R19 represents OH, NH2 and so on, Y represents -NH-, -O- or a direct bond, a represents 1-3, b represents 1 or 2, c represents 0 or 1 and d represents 0 or 1.
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5.发明授权NOVEL ACYLGUANIDINE DERIVATIVES AS INHIBITORS OF BONE RESORPTION AND AS VITRONECTIN RECEPTOR ANTAGONISTS 有权酰基胍衍生物作为抑制剂骨吸收和ALS玻受体拮抗剂
公开(公告)号：EP1042301B1
公开(公告)日：2002-11-20
申请号：EP98966287.9
申请日：1998-12-10
发明人： PEYMAN, Anuschirwan , KNOLLE, Jochen , BREIPOHL, Gerhard , SCHEUNEMANN, Karl-Heinz , CARNIATO, Denis , GOURVEST, Jean-François , GADEK, Thomas , MCDOWELL, Robert , BODARY, Sarah, Catherine , CUTHBERTSON, Robert, Andrew , FERRARA, Napoleane
IPC分类号： C07D239/16 , C07C279/20 , A61K31/505
CPC分类号： C07C279/20 , C07D239/16
摘要： The present invention relates to acylguanidine derivatives of formula (I) in which R?1, R2, R4, R5, R6¿, A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmaceutical active ingredients. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts and are suitable, for example, for the therapy or prophylaxis of diseases which are caused at least partially by an undesired extend of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical preparations comprising them.
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6.发明授权COMPOSES TRICYCLIQUES AYANT UNE ACTIVITE VIS-A-VIS DES INTEGRINES NOTAMMENT VIS-A-VIS DE L'INTEGRINE ALPHA vBETA3, LEUR PROCEDE DE PREPARATION ET LES INTERMEDIAIRES DE CE PROCEDE, LEUR APPLICATION A TITRE DE MEDICAMENTS ET LES COMPOSITIONS PHARMACEUTIQUES LES RENFERMANT 失效WITH对整TRIZYCLISCHE TIES，特别是在素αVβ3整联蛋白，生产和诉讼的中间产品的方法，它们作为包含新药与YOU药物组合物
公开(公告)号：EP0888292B1
公开(公告)日：2001-10-31
申请号：EP97915519.9
申请日：1997-03-20
发明人： BERNARD, Serge , CARNIATO, Denis , GOURVEST, Jean-François , TEUTSCH, Jean-Georges , KNOLLE, Jochen , STILZ, Hans-Ulrich , WEHNER, Volkmar , BODARY, Sarah, C. , GADEK, Thomas, R. , MCDOWELL, Robert, S. , PITTI, Robert, M.
IPC分类号： C07C281/12 , C07D233/52 , C07C337/08 , C07D239/18 , C07D317/70 , A61K31/19 , A61K31/415 , A61K31/505 , A61K31/36
CPC分类号： C07D239/18 , C07C45/516 , C07C45/63 , C07C45/673 , C07C45/71 , C07C49/747 , C07C49/755 , C07C281/12 , C07C281/18 , C07C331/04 , C07C331/10 , C07C331/12 , C07C331/14 , C07C337/08 , C07C2603/30 , C07D233/52 , Y02P20/55 , C07C49/753
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7.发明公开DERIVES D'IMINOGUANIDINES, LEUR PROCEDE DE PREPARATION, LEUR APPLICATION COMME MEDICAMENTS 有权IMINOGUANIDINE衍生物，生产与应用，药物
公开(公告)号：EP1133476A1
公开(公告)日：2001-09-19
申请号：EP99956122.8
申请日：1999-11-23
发明人： CARNIATO, Denis,Résidence Le Samoa Entrée B , GADEK, Thomas, R. , GOURVEST, Jean-François , KNOLLE, Jochen , PEYMAN, Anurschirwan , RUXER, Jean-Marie , BODARY, Sarah, C.
IPC分类号： C07D233/52 , C07C281/18 , A61K31/4168 , A61K31/155 , A61P19/10
CPC分类号： C07C281/18 , C07D233/52
摘要： The invention concerns compounds of formula (I) wherein: m = 1, 2 or 3; n = 1, 2 or 3; R5 represents a group selected among COR6, CO2R6, SO2R6, SO2NHR6, SO2NHCOR6, SO2NHCO2R6, CONH2, CONHR6; R1, R2, R4, R6, R7 R8 and R12 are as defined in the description, in all their possible isomeric forms, their physiologically acceptable salts, their prodrugs. The invention also concerns the method for preparing them, their use as medicines in particular for treating osteoporosis and the pharmaceutical compositions containing them.
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8.发明授权
公开(公告)号：EP1133478B1
公开(公告)日：2016-01-06
申请号：EP99956120.2
申请日：1999-11-23
发明人： CARNIATO, Denis , GADEK, Thomas, R. , GOURVEST, Jean-François , KNOLLE, Jochen , PEYMAN, Anurschirwan , RUXER, Jean-Marie , BODARY, Sarah, C.
IPC分类号： C07D239/16 , C07C279/22 , C07C311/06 , A61K31/505
CPC分类号： C07D239/16 , C07C279/22 , C07C311/06
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公开(公告)号：EP1313737A1
公开(公告)日：2003-05-28
申请号：EP01956555.5
申请日：2001-07-23
发明人： PEYMAN, Anushirwan , WILL, David , GADEK, Thomas, R. , McDOWELL, Robert , GOURVEST, Jean-François , RUXER, Jean-Marie , KNOLLE, Jochen
IPC分类号： C07D473/34 , C07D487/04 , A61K31/52 , A61P19/10
CPC分类号： C07D473/00 , C07D487/04
摘要： The present invention relates to acylguanidino derivatives of formula (I), in which R?1, R2, R3¿, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical compositions comprising them.
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10.发明授权
公开(公告)号：EP1133491B1
公开(公告)日：2003-02-19
申请号：EP99956121.0
申请日：1999-11-23
发明人： CARNIATO, Denis , GADEK, Thomas, R. , GOURVEST, Jean-François , KNOLLE, Jochen , PEYMAN, Anurschirwan , BODARY, Sarah, C.
IPC分类号： C07D405/12 , A61K31/495
CPC分类号： C07D405/12
摘要： The invention concerns compounds of formula (I) wherein: m = 1, 2 or 3; n = 1, 2 or 3; R5 represents a group selected among COR6, CO2R6, SO2R6, SO2NHR6, SO2NHCOR6, SO2NHCO2R6, CONH2 and CONHR6; R1, R2, R4, R5, R6 and R7 are as defined in the description, in all their possible isomeric forms, their physiologically acceptable salts, their prodrugs. The invention also concerns the method for preparing them, their use as medicines in particular for treating osteoporosis and pharmaceutical compositions containing them.
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