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1. 发明授权

US06602878B1 Acylquanidine derivatives, method for preparing same, application as medicines and pharmaceutical compositions containing them 有权
标题翻译：酰基胍衍生物，其制备方法，作为药物的应用和含有它们的药物组合物
公开(公告)号：US06602878B1
公开(公告)日：2003-08-05
申请号：US09856351
申请日：2001-06-27
申请人： Denis Carniato , Thomas R. Gadek , Jean-Francois Gourvest , Jochen Knolle , Anurschirwan Peyman , Jean-Marie Ruxer , Sarah C. Bodary
发明人： Denis Carniato , Thomas R. Gadek , Jean-Francois Gourvest , Jochen Knolle , Anurschirwan Peyman , Jean-Marie Ruxer , Sarah C. Bodary
IPC分类号： C07D23916
CPC分类号： C07D239/16 , C07C279/22 , C07C311/06
摘要： Acylquanidines of the formula wherein the substituents are defined as in the specification which are antagonists of the vitronectin receptor and inhibitors of cell adhesion and bone resorption mediated by the osteoclasts.
摘要翻译：在说明书中定义了取代基的甲酰基喹啉，其是玻连蛋白受体的拮抗剂和由破骨细胞介导的细胞粘附和骨吸收的抑制剂。

2. 发明授权

US06391904B1 Iminoguanidine derivatives, preparation method, use as medicines 有权
标题翻译：咪喹啉衍生物，制备方法，用作药物
公开(公告)号：US06391904B1
公开(公告)日：2002-05-21
申请号：US09856693
申请日：2001-06-29
申请人： Denis Carniato , Jean-Francois Gourvest , Jean-Marie Ruxer , Jochen Knolle , Anurschirwan Peyman , Sarah C. Bodary , Thomas R. Gadek
发明人： Denis Carniato , Jean-Francois Gourvest , Jean-Marie Ruxer , Jochen Knolle , Anurschirwan Peyman , Sarah C. Bodary , Thomas R. Gadek
IPC分类号： A61K314168
CPC分类号： C07C281/18 , C07D233/52
摘要： A compound of the formula where the substituents are defined in the specification and its pharmaceutically acceptable salts and prodrugs thereof useful as antagonists of vitronectin receptors.
摘要翻译：在说明书中定义取代基的化合物及其药学上可接受的盐和前药，其可用作玻连蛋白受体的拮抗剂。

3. 发明授权

US06586442B2 Benzofurane derivatives, their preparation process, their use as medicaments and the pharmaceutical compositions containing them 失效
标题翻译：苯并呋喃衍生物，其制备方法，它们作为药物的用途以及含有它们的药物组合物
公开(公告)号：US06586442B2
公开(公告)日：2003-07-01
申请号：US10180253
申请日：2002-06-26
申请人： Denis Carniato , Jean-Francois Gourvest , Jochen Knolle , Anurschirwan Peyman , Sarah C. Bodary , Thomas R. Gadek
发明人： Denis Carniato , Jean-Francois Gourvest , Jochen Knolle , Anurschirwan Peyman , Sarah C. Bodary , Thomas R. Gadek
IPC分类号： A61K31505
CPC分类号： C07D405/12
摘要： A compound of the formula wherein the substituents are as defined in the specification and its pharmaceutically acceptable salts and it prodrug useful for treating osteoporosis.
摘要翻译：取代基中的取代基的化合物如说明书及其药学上可接受的盐所定义，并且其用于治疗骨质疏松症的前药。

4. 发明授权

US06458801B1 Benzofurane derivatives, preparation method, use as medicines and pharmaceutical compositions containing same 有权
标题翻译：苯并呋喃衍生物，制备方法，用作药物和含有它们的药物组合物
公开(公告)号：US06458801B1
公开(公告)日：2002-10-01
申请号：US09856542
申请日：2001-06-29
申请人： Denis Carniato , Thomas R. Gadek , Jean-Francois Gourvest , Jochen Knolle , Anurschirwan Peyman , Sarah C. Bodary
发明人： Denis Carniato , Thomas R. Gadek , Jean-Francois Gourvest , Jochen Knolle , Anurschirwan Peyman , Sarah C. Bodary
IPC分类号： A61K31505
CPC分类号： C07D405/12
摘要： A compound of the formula wherein the substituents are as defined in the specification and its pharmaceutically acceptable salts and its prodrug useful for treating osteoporosis.
摘要翻译：取代基中的取代基的化合物如说明书及其药学上可接受的盐及其用于治疗骨质疏松症的前药所定义。

5. 发明授权

US06500815B1 Substituted 11.beta steroid derivatives, method for preparing same and intermediates of said method, use as medicine and compositions containing them 有权
标题翻译：取代的11.β类固醇衍生物，其制备方法和所述方法的中间体，用作药物和含有它们的组合物
公开(公告)号：US06500815B1
公开(公告)日：2002-12-31
申请号：US09914025
申请日：2001-12-17
申请人： Denis Carniato , Thomas R. Gadek , Jochen Knolle , Jean-Francois Gourvest , Anurschirwan Peyman , Sarah C. Bodary
发明人： Denis Carniato , Thomas R. Gadek , Jochen Knolle , Jean-Francois Gourvest , Anurschirwan Peyman , Sarah C. Bodary
IPC分类号： A61K3156
CPC分类号： C07J41/0005
摘要： The invention concerns compounds of formula (I) wherein: X, Y, R1, R2, Z, G are as defined in the description, the methods for preparing them and the intermediates in said method, their use as medicine and the pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）的化合物，其中：X，Y，R 1，R 2，Z，G如说明书中所定义，其制备方法和所述方法中的中间体，其用作药物和含有他们。

6. 发明授权

US06459001B1 Tricyclic compounds, their preparation process and the intermediates of this process, their use as medicaments and the pharmaceutical compositions containing them 有权
标题翻译：三环化合物，其制备方法和该方法的中间体，它们作为药物的用途和含有它们的药物组合物
公开(公告)号：US06459001B1
公开(公告)日：2002-10-01
申请号：US09769018
申请日：2001-01-25
申请人： Serge Bernard , Denis Carniato , Jean-Francois Gourvest , Jean-Georges Teutsch , Jochen Knolle , Hans-Ulrich Stilz , Volkmar Wehner , Sarah C. Bodary , Thomas R. Gadek , Robert S. McDowell , Robert M. Pitti
发明人： Serge Bernard , Denis Carniato , Jean-Francois Gourvest , Jean-Georges Teutsch , Jochen Knolle , Hans-Ulrich Stilz , Volkmar Wehner , Sarah C. Bodary , Thomas R. Gadek , Robert S. McDowell , Robert M. Pitti
IPC分类号： C07C25182
CPC分类号： C07D239/18 , C07C45/516 , C07C45/63 , C07C45/673 , C07C45/71 , C07C49/747 , C07C49/755 , C07C281/12 , C07C281/18 , C07C337/08 , C07C2603/30 , C07D233/52 , C07C49/753
摘要： The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.
摘要翻译：本发明的主题是式（I）的产物：其中R1，R2，R3，R4，R5和G如说明书中所定义，虚线代表任选的第二键，以及与酸和碱和酯，它们的制备方法和该方法的中间体，它们作为药物的用途和含有它们的药物组合物。

7. 发明授权

US06339082B1 Tricyclic compounds, preparation method and said method intermediates, application as medicines and pharmaceutical compositions containing same 有权
标题翻译：三环化合物，制备方法和所述方法中间体，作为药物和含有其的药物组合物的应用
公开(公告)号：US06339082B1
公开(公告)日：2002-01-15
申请号：US09509327
申请日：2000-06-29
申请人： Denis Carniato , Thomas R. Gadek , Jean-Francois Gourvest , Jochen Knolle , Robert S. McDowell , Anurschirwan Peyman
发明人： Denis Carniato , Thomas R. Gadek , Jean-Francois Gourvest , Jochen Knolle , Robert S. McDowell , Anurschirwan Peyman
IPC分类号： C07D23352
CPC分类号： C07D239/42 , C07D233/52 , C07D401/12 , C07D405/12
摘要： A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as set forth in the specification and its salts with non-toxic pharmaceutically acceptable acids and bases useful for treating loss of bone matrix.
摘要翻译：选自由取代基中的烷基脲的化合物组成的组中的化合物定义如说明书中所述，并且其盐与无毒的药学上可接受的酸和碱可用于治疗骨基质的丧失。

8. 发明授权

US06221907B1 Tricyclic compounds having activity specific for integrins, particularly alphanubeta3 integrins, method for preparing same, intermediates therefor, use of said compounds as drugs, and pharmaceutical compositions containing same 有权
标题翻译：具有对整联蛋白特异性的活性的三环化合物，特别是α2β3整联蛋白，其制备方法，其中间体，所述化合物作为药物的使用，以及含有该化合物的药物组合物
公开(公告)号：US06221907B1
公开(公告)日：2001-04-24
申请号：US09155063
申请日：1999-02-02
申请人： Serge Bernard , Denis Carniato , Jean-Francois Gourvest , Jean-Georges Teutsch , Jochen Knolle , Hans-Ulrich Stilz , Volkmar Wehner , Sarah C. Bodary , Thomas R. Gadek , Robert S. McDowell , Robert M. Pitti
发明人： Serge Bernard , Denis Carniato , Jean-Francois Gourvest , Jean-Georges Teutsch , Jochen Knolle , Hans-Ulrich Stilz , Volkmar Wehner , Sarah C. Bodary , Thomas R. Gadek , Robert S. McDowell , Robert M. Pitti
IPC分类号： A61K3115
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： The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.
摘要翻译：本发明的主题是式（I）的产物：其中R1，R2，R3，R4，R5和G如说明书中所定义，虚线代表任选的第二键，以及与酸和碱和酯，它们的制备方法和该方法的中间体，它们作为药物的用途和含有它们的药物组合物。

9. 发明授权

US06747016B1 Substituted purine derivatives as inhibitors of cell adhesion 失效
标题翻译：取代嘌呤衍生物作为细胞粘附的抑制剂
公开(公告)号：US06747016B1
公开(公告)日：2004-06-08
申请号：US10030290
申请日：2002-03-06
申请人： Anuschirwan Peyman , Jochen Knolle , Thomas R Gadek , Jean-Francois Gourvest , Jean-Marie Ruxer
发明人： Anuschirwan Peyman , Jochen Knolle , Thomas R Gadek , Jean-Francois Gourvest , Jean-Marie Ruxer
IPC分类号： C07D47334
CPC分类号： C07D473/34
摘要： The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R1, R2 and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonist and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses 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 inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or prolifertion of cells of the vascular smooth musculature. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）化合物，其中B，D，E，G，X，Y，Z，R 1，R 2和s具有权利要求书中所示的含义，盐及其前药。式（I）化合物是有价值的药理活性化合物。它们是玻连蛋白受体拮抗剂和细胞粘附抑制剂，并且适用于治疗和预防基于玻连蛋白受体及其配体在细胞 - 细胞或细胞 - 基质相互作用过程中的相互作用的疾病，或可被预防，缓解或通过影响这种相互作用来治愈。例如，它们可以用于抑制破骨细胞的骨吸收，从而用于治疗和预防骨质疏松症，或用于抑制血管平滑肌肉细胞的不期望的血管生成或增殖。本发明还涉及制备式（I）化合物，其用途，特别是作为药物中的活性成分的方法，以及包含它们的药物组合物。

10. 发明授权

US06340679B1 Guanidine derivatives as inhibitors of cell adhesion 有权
标题翻译：胍衍生物作为细胞粘附抑制剂
公开(公告)号：US06340679B1
公开(公告)日：2002-01-22
申请号：US09502577
申请日：2000-02-11
申请人： Anuschirwan Peyman , Jochen Knolle , Karl-Heinz Scheunemann , David William Will , Denis Carniato , Jean-Francois Gourvest , Thomas R. Gadek , Sarah Catherine Bodary
发明人： Anuschirwan Peyman , Jochen Knolle , Karl-Heinz Scheunemann , David William Will , Denis Carniato , Jean-Francois Gourvest , Thomas R. Gadek , Sarah Catherine Bodary
IPC分类号： C07D23916
CPC分类号： C07D409/12 , C07D239/16
摘要： The present invention relates to acylguanidine derivatives of the formula I in which R1, R2, R4, Ar, X and n have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the formula I are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion. They inhibit, for example, bone resorption by osteoclasts and are suitable for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example osteoporosis. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceutical preparations, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式Iin的酰基胍衍生物，其中R 1，R 2，R 4，Ar，X和n具有权利要求中所示的含义，其生理上可耐受的盐及其前药。式I的化合物是有价值的药理活性化合物。它们是玻连蛋白受体拮抗剂和细胞粘附抑制剂。它们抑制例如破骨细胞的骨吸收，并且适用于治疗和预防至少部分由不期望的骨吸收程度引起的疾病，例如骨质疏松症。本发明还涉及制备式I化合物的方法，其用途，特别是作为药物制剂中的活性成分，以及包含它们的药物制剂。

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