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1. 发明授权

US06872735B2 LFA-1 antagonist compounds 失效
标题翻译： LFA-1拮抗剂化合物
公开(公告)号：US06872735B2
公开(公告)日：2005-03-29
申请号：US10618178
申请日：2003-07-11
申请人： Daniel J. Burdick , Mark S. Stanley , David Oare , Mark E. Reynolds , Thomas R. Gadek , James C. Marsters
发明人： Daniel J. Burdick , Mark S. Stanley , David Oare , Mark E. Reynolds , Thomas R. Gadek , James C. Marsters
IPC分类号： C07D277/06 , A61K31/197 , A61K31/198 , A61K31/341 , A61K31/351 , A61K31/385 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/445 , A61K31/4458 , A61K31/4462 , A61K31/4465 , A61K31/4525 , A61P1/04 , A61P11/06 , A61P17/06 , A61P19/02 , A61P29/00 , A61P37/06 , C07C233/83 , C07D207/16 , C07D211/60 , C07D211/62 , C07D307/54 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
CPC分类号： C07D405/12 , A61K31/198 , A61K31/40 , A61K31/44 , C07D207/16 , C07D277/06 , C07D307/54 , C07D417/12
摘要： The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.
摘要翻译：本发明涉及具有式（I）的新化合物，其中Cy，X，Y，L和R1-6如本文所定义。这些化合物结合CD11 / CD18粘附受体如淋巴细胞功能相关抗原-1（LFA-1），因此可用于治疗由LFA-1介导的疾病如炎症和自身免疫性疾病。

2. 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。

3. 发明授权

US06313119B1 Sulfonamide derivatives as inhibitors of bone resorption and as inhibitors of cell adhesion 失效
标题翻译：磺酰胺衍生物作为骨吸收抑制剂和细胞粘附抑制剂
公开(公告)号：US06313119B1
公开(公告)日：2001-11-06
申请号：US09564988
申请日：2000-05-05
申请人： Anuschirwan Peyman , David William Will , Jochen Knolle , Karlheinz Scheunemann , Denis Carniato , Jean-Francois Gourvest , Thomas R. Gadek , Robert McDowell , Sarah Catherine Bodary , Robert Andrew Cuthbertson
发明人： Anuschirwan Peyman , David William Will , Jochen Knolle , Karlheinz Scheunemann , Denis Carniato , Jean-Francois Gourvest , Thomas R. Gadek , Robert McDowell , Sarah Catherine Bodary , Robert Andrew Cuthbertson
IPC分类号： A61K31192
CPC分类号： C07D409/12 , C07D239/16
摘要： Sulfonamide derivatives, their physiologically tolerable salts and their prodrugs according to the present invention are vitronectin receptor antagonists and inhibitors of cell adhesion, as well as inhibit bone resorption by osteoclasts. These derivatives, salts and prodrugs are pharmaceutically active compounds useful in the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. Processes for the preparation of the sulfonamide derivatives according to the present invention, the use of these derivatives as pharmaceutically active ingredients, and pharmaceutical preparations comprising these derivatives also are disclosed.
摘要翻译：根据本发明的磺酰胺衍生物，其生理上可耐受的盐及其前药是玻连蛋白受体拮抗剂和细胞粘附抑制剂，以及抑制破骨细胞的骨吸收。这些衍生物，盐和前药是用于治疗和预防由至少部分由不期望的骨吸收程度引起的疾病的药物活性化合物，例如骨质疏松症。本发明的磺酰胺衍生物的制备方法，这些衍生物作为药物活性成分的用途，以及包含这些衍生物的药物制剂也被公开。

4. 发明授权

US06194380B1 Agents for promoting bone formation 有权
标题翻译：促进骨形成的药剂
公开(公告)号：US06194380B1
公开(公告)日：2001-02-27
申请号：US09077714
申请日：1999-04-20
申请人： Kazuyuki Kitamura , Osamu Komiyama , Mizuho Inazu , Roland Baron , Thomas R. Gadek , Hans-Ulrich Stilz , Volkmar Wehner , Jochen Knolle , Robert S. McDowell
发明人： Kazuyuki Kitamura , Osamu Komiyama , Mizuho Inazu , Roland Baron , Thomas R. Gadek , Hans-Ulrich Stilz , Volkmar Wehner , Jochen Knolle , Robert S. McDowell
IPC分类号： A01N3718
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 the following 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.
摘要翻译：本发明的目的是提供骨形成促进剂，骨形成用治疗剂和骨形成促进剂的制备方法.1，一种骨形成促进剂，其特征在于，含有丝ist药，e嗪，肽或多肽中的至少一种包含分子中的氨基酸序列ArgGlyAsp，例如由Gly-Arg-Gly-Asp-Ser表示的肽或由以下通式（IX）表示的化合物等，以及其生物可接受的盐，其中R 16表示 -N（R 20）2（R 20表示氢原子或C 1 -C 4烷基），R 17表示氢原子或C 1〜C 4烷基，R 18表示氢原子，C 1〜C 4烷基等， R 19表示OH，NH 2等，Y表示-NH-，-O-或直接键，a表示1-3，b表示1或2，c表示0或1，d表示0或1。

5. 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。

6. 发明授权

US06667318B2 LFA-1 antagonist compounds 失效
标题翻译： LFA-1拮抗剂化合物
公开(公告)号：US06667318B2
公开(公告)日：2003-12-23
申请号：US09994546
申请日：2001-11-26
申请人： Daniel J. Burdick , Mark S. Stanley , David Oare , Mark E. Reynolds , Thomas R. Gadek , James C. Marsters
发明人： Daniel J. Burdick , Mark S. Stanley , David Oare , Mark E. Reynolds , Thomas R. Gadek , James C. Marsters
IPC分类号： A61K314525
CPC分类号： C07D405/12 , A61K31/198 , A61K31/40 , A61K31/44 , C07D207/16 , C07D277/06 , C07D307/54 , C07D417/12
摘要： The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.
摘要翻译：本发明涉及具有式（I）的新化合物，其中Cy，X，Y，L和R1-6如本文所定义。这些化合物结合CD11 / CD18粘附受体如淋巴细胞功能相关抗原-1（LFA-1），因此可用于治疗由LFA-1介导的疾病如炎症和自身免疫性疾病。

7. 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。

8. 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。

9. 发明授权

US06387395B1 N-[1, (1-1) -dialkyloxy] - and N- [1, (1-1) -dialkenyloxy]- alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor 失效
标题翻译： N- [1，（1-1） - 二烷氧基] - 和N- [1,1-（1,1-） - 二烯氧基] - 烷-1-基-N，N，N-四取代的铵脂质及其用途
公开(公告)号：US06387395B1
公开(公告)日：2002-05-14
申请号：US08348635
申请日：1994-12-02
申请人： Deborah A. Eppstein , Philip L. Felgner , Thomas R. Gadek , Gordon H. Jones , Richard B. Roman
发明人： Deborah A. Eppstein , Philip L. Felgner , Thomas R. Gadek , Gordon H. Jones , Richard B. Roman
IPC分类号： A61K9127
CPC分类号： C07D453/02 , A61K9/0014 , A61K9/0019 , A61K9/1272 , A61K47/186 , C12N15/88 , Y10S435/829
摘要： This invention relates to compounds of the formula or an optical isomer thereof wherein R1 and R2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R3, R4 and R5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R3, R4, and R5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
摘要翻译：本发明涉及式的化合物或其光学异构体，其中R 1和R 2相同或不同，为6至24个碳原子的烷基或烯基; R3，R4和R5相同或不同，为碳原子数为1〜8的烷基，芳基，碳原子数为7〜11的芳烷基，或者当R3，R4，R5中的2个或3个相同时，可以形成奎宁二基，哌啶子基，吡咯烷子基或吗啉代; n为1至8; X是药学上可接受的阴离子。

10. 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。

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