公开(公告)号：US06660728B2

公开(公告)日：2003-12-09

申请号：US10368771

申请日：2002-11-14

申请人： Karl-Heinz Scheunemann ,  Jochen Knolle ,  Amuschirwan Peyman ,  David William Will ,  Denis Carniato ,  Jean-Francois Gourvest ,  Thomas Gadek ,  Robert McDowell ,  Sarah Catherine Bodary ,  Robert Andrew Cuthbertson

发明人： Karl-Heinz Scheunemann ,  Jochen Knolle ,  Amuschirwan Peyman ,  David William Will ,  Denis Carniato ,  Jean-Francois Gourvest ,  Thomas Gadek ,  Robert McDowell ,  Sarah Catherine Bodary ,  Robert Andrew Cuthbertson

IPC分类号： A61K3133

CPC分类号： C07D409/12 ,  C07D333/24 ,  C07D409/14

摘要： The present invention relates to thienyl substituted acylguanidine derivatives, such as compounds of formula (I) in which R1, R2, R4, R6, A, B and D have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the present invention are valuable pharmaceutical active compounds. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts. They are suitable, for example, for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of thienyl substituted acylguanidines, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

摘要翻译： 本发明涉及噻吩基取代的酰基胍衍生物，例如式（I）的化合物，其中R 1，R 2，R 4，R 6，A，B和D具有如 权利要求书，其生理上可耐受的盐及其前药。 本发明的化合物是有价值的药物活性化合物。 它们是玻连蛋白受体拮抗剂和破骨细胞骨吸收抑制剂。 例如，它们适合用于治疗和预防至少部分地由不期望的骨吸收程度引起的疾病，例如骨质疏松症。 本发明还涉及噻吩基取代的酰基胍的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

公开(公告)号：US06566366B1

公开(公告)日：2003-05-20

申请号：US09700655

申请日：2001-03-06

申请人： Karl-Heinz Scheunemann ,  Jochen Knolle ,  Amuschirwan Peyman ,  David William Will ,  Denis Carniato ,  Jean-Francois Gourvest ,  Thomas Gadek ,  Robert McDowell ,  Sarah Catherine Bodary ,  Robert Andrew Cuthbertson

发明人： Karl-Heinz Scheunemann ,  Jochen Knolle ,  Amuschirwan Peyman ,  David William Will ,  Denis Carniato ,  Jean-Francois Gourvest ,  Thomas Gadek ,  Robert McDowell ,  Sarah Catherine Bodary ,  Robert Andrew Cuthbertson

IPC分类号： A61K31505

CPC分类号： C07D409/12 ,  C07D333/24 ,  C07D409/14

摘要： Compounds of the formula and salts thereof wherein the substituents are defined as in accordance with the specification useful for the treatment of tumor growth, osteoporosis, inflammation and cardiovascular disorders.

摘要翻译： 式及其盐的化合物，其中取代基根据可用于治疗肿瘤生长，骨质疏松症，炎症和心血管疾病的说明书定义。

公开(公告)号：US06492356B1

公开(公告)日：2002-12-10

申请号：US09581915

申请日：2000-11-02

申请人： Anuschirwan Peyman ,  Jochen Knolle ,  Gerhard Breipohl ,  Karl-Heinz Scheunemann ,  Denis Carniato ,  Jean-Francois Gourvest ,  Thomas Gadek ,  Robert McDowell ,  Sarah Catherine Bodary ,  Robert Andrew Cuthbertson ,  Napoleane Ferrara

发明人： Anuschirwan Peyman ,  Jochen Knolle ,  Gerhard Breipohl ,  Karl-Heinz Scheunemann ,  Denis Carniato ,  Jean-Francois Gourvest ,  Thomas Gadek ,  Robert McDowell ,  Sarah Catherine Bodary ,  Robert Andrew Cuthbertson ,  Napoleane Ferrara

IPC分类号： A61K3155

CPC分类号： C07C279/20 ,  C07D239/16

摘要： The present invention relates to acylguanidine derivatives of formula (I) in which R1, 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.

摘要翻译： 本发明涉及式（I）的酰基胍衍生物，其中R 1，R 2，R 4，R 5，R 6，A，m和n具有专利权利要求中指出的含义，其生理上可耐受的盐及其前药。 式（I）化合物是有价值的药物活性成分。 它们是玻连蛋白受体拮抗剂和破骨细胞骨吸收的抑制剂，并且适合于例如治疗或预防由至少部分由不期望的骨吸收扩展（例如骨质疏松症）引起的疾病。 本发明还涉及式（I）化合物的制备方法，其用途，特别是作为药物活性成分，以及包含它们的药物制剂。

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。

公开(公告)号：US06747148B2

公开(公告)日：2004-06-08

申请号：US09972190

申请日：2001-10-09

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： C07C211119

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。

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。

公开(公告)号：US06399620B1

公开(公告)日：2002-06-04

申请号：US09606080

申请日：2000-06-29

申请人： Volkmar Wehner ,  Jochen Knolle ,  Hans Ulrich Stilz ,  Jean-Francois Gourvest ,  Denis Carniato ,  Thomas Richard Gadek ,  Robert McDowell ,  Robert Maurice Pitti ,  Sarah Catherine Bodary

发明人： Volkmar Wehner ,  Jochen Knolle ,  Hans Ulrich Stilz ,  Jean-Francois Gourvest ,  Denis Carniato ,  Thomas Richard Gadek ,  Robert McDowell ,  Robert Maurice Pitti ,  Sarah Catherine Bodary

IPC分类号： A61K31505

CPC分类号： C07C277/08 ,  C07C279/20 ,  C07C2603/74 ,  C07D233/48 ,  C07D239/16 ,  C07C279/22

摘要： There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G  (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.

摘要翻译： 描述了式（I）的环烷基衍生物，其中R 1，Y，A，B，D，E，F和G具有本文所指的含义，它们的制备及其作为药物的用途。 根据本发明的化合物可用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

公开(公告)号：US6005117A

公开(公告)日：1999-12-21

申请号：US899887

申请日：1997-07-24

申请人： Volkmar Wehner ,  Jochen Knolle ,  Hans Ulrich Stilz ,  Jean-Francois Gourvest ,  Denis Carniato ,  Thomas Richard Gadek ,  Robert McDowell ,  Robert Maurice Pitti ,  Sarah Catherine Bodary

发明人： Volkmar Wehner ,  Jochen Knolle ,  Hans Ulrich Stilz ,  Jean-Francois Gourvest ,  Denis Carniato ,  Thomas Richard Gadek ,  Robert McDowell ,  Robert Maurice Pitti ,  Sarah Catherine Bodary

IPC分类号： C07C229/04 ,  A61K31/19 ,  A61K31/197 ,  A61K31/415 ,  A61K31/445 ,  A61P3/00 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P19/08 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C251/02 ,  C07D211/18 ,  C07D233/52 ,  C07D233/54 ,  C07D233/66 ,  C07D257/04 ,  C07D233/44

CPC分类号： C07D233/52

摘要： There are described imino derivatives of formula (I)R.sup.1 --Y--A--B--D--E--F--G (I)their preparation and their use as medicaments. The compounds according to the invention may be used as vitronectin receptor antagonists and as inhibitors of bone resorption.

摘要翻译： 描述了式（I）R1-Y-A-B-D-E-F-G（I）的亚氨基衍生物及其作为药物的用途。 根据本发明的化合物可用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

公开(公告)号：US07348333B2

公开(公告)日：2008-03-25

申请号：US10141986

申请日：2002-05-10

申请人： Volkmar Wehner ,  Jochen Knolle ,  Hans Ulrich Stilz ,  Jean-Francois Gourvest ,  Denis Carniato ,  Thomas Richard Gadek ,  Robert McDowell ,  Robert Maurice Pitti ,  Sarah Catherine Bodary

发明人： Volkmar Wehner ,  Jochen Knolle ,  Hans Ulrich Stilz ,  Jean-Francois Gourvest ,  Denis Carniato ,  Thomas Richard Gadek ,  Robert McDowell ,  Robert Maurice Pitti ,  Sarah Catherine Bodary

IPC分类号： A61P9/00 ,  A61K31/517 ,  A61K31/44 ,  C07D403/00 ,  C07D257/00

CPC分类号： C07C277/08 ,  C07C279/20 ,  C07C2603/74 ,  C07D233/48 ,  C07D239/16 ,  C07C279/22

摘要： There are described cycloalkyl derivatives of the formula (I) R1—Y-A-B-D-E-F-G  (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.

摘要翻译： 描述式（I）的环烷基衍生物<？in-line-formula description =“In-line Formulas”end =“lead”？> R 1 -YABDEFG（I）<αin 其中R 1，Y，A，B，D，E，F和G具有本文所示的含义，-line-formula description =“In-line Formulas”end =“tail”？> 他们的准备和用作药物。 根据本发明的化合物可以用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

公开(公告)号：US20080021055A1

公开(公告)日：2008-01-24

申请号：US11892235

申请日：2007-08-21

申请人： Volkmar Wehner ,  Jochen Knolle ,  Hans Stilz ,  Jean-Francois Gourvest ,  Denis Carniato ,  Thomas Gadek ,  Robert McDowell ,  Robert Pitti ,  Sarah Bodary

发明人： Volkmar Wehner ,  Jochen Knolle ,  Hans Stilz ,  Jean-Francois Gourvest ,  Denis Carniato ,  Thomas Gadek ,  Robert McDowell ,  Robert Pitti ,  Sarah Bodary

IPC分类号： A61K31/505 ,  A61K31/27 ,  A61P9/10 ,  C07D233/00 ,  C07D239/02 ,  C07C269/00 ,  A61K31/4164

CPC分类号： C07C277/08 ,  C07C279/20 ,  C07C2603/74 ,  C07D233/48 ,  C07D239/16 ,  C07C279/22

摘要： There are described cycloalkyl derivatives of the formula (I) R1—Y-A-B-D-E-F-G   (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.

摘要翻译： 描述式（I）的环烷基衍生物<？in-line-formula description =“In-line Formulas”end =“lead”？> R 1 -YABDEFG（I）<αin 其中R 1，Y，A，B，D，E，F和G具有本文所示的含义，-line-formula description =“In-line Formulas”end =“tail”？> 他们的准备和用作药物。 根据本发明的化合物可用作玻连蛋白受体拮抗剂和骨吸收抑制剂。