公开(公告)号：WO0193840A3

公开(公告)日：2002-08-08

申请号：PCT/EP0106397

申请日：2001-06-06

Applicant: BASF AG ,  GENESTE HERVE ,  KLING ANDREAS ,  LANGE UDO ,  SEITZ WERNER ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HORNBERGER WILFRIED ,  LAUTERBACH ARNULF

Inventor： GENESTE HERVE ,  KLING ANDREAS ,  LANGE UDO ,  SEITZ WERNER ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HORNBERGER WILFRIED ,  LAUTERBACH ARNULF

IPC: C07D223/10 ,  A61K31/55 ,  A61K31/5513 ,  A61K45/00 ,  A61K45/06 ,  A61P3/10 ,  A61P5/18 ,  A61P7/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P43/00 ,  C07D263/48 ,  C07D277/08 ,  C07D307/68 ,  C07D333/38 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07K5/023

CPC classification number: A61K45/06

Abstract: The invention relates to the use of cyclic compounds as ligands of integrin receptors, in particular as ligands of the alpha vss3 integrin receptor. The invention also relates to the novel compounds, to the use thereof and to pharmaceutical preparations which contain said compounds. Examples of said compounds include benzazepines, benzodiazepines and thieno[3,2-b]azepines, used for treating arteriosclerosis, rheumatoid arthritis, restenosis after vessel damage or stent implantation, angioplasty, acute kidney failure, microangiopathy associated with angiogenesis, diabetic angiopathy, thrombocyte-mediated vascular occlusion, arterial thrombosis, congestive heart-failure, myocardial infarct, apoplexy, cancer, osteoporosis, hypertension, psoriasis or viral, parasitic or bacterial diseases, inflammation, wound healing, hyperparathyroidism, Paget's bone disease, malignant hypercalcemia, or metastatic osteolytic lesions.

Abstract translation: 本发明涉及使用包含化合物作为整合素受体，特别是作为avB3整联的配体，该新颖化合物本身，它们的用途，以及药物制剂，这些化合物的配位体环状的。 作为例子苯并吖庚因，苯并二氮杂类和噻吩并[3,2-B]氮杂列出用于治疗动脉粥样硬化的，类风湿性关节炎，再狭窄血管损伤或支架植入术，血管成形术，急性肾功能衰竭，血管成形术，血管生成相关性微血管病，糖尿病性血管病，Blutplättchenvermitteltem血管闭合后 ，动脉血栓形成，充血性心脏衰竭，心肌梗死，中风，癌症，骨质疏松症，高血压，牛皮癣或病毒，寄生虫或细菌性疾病，炎症，疼痛肺，Hyperparathyroismus，佩吉特病，恶性高钙血症或转移性溶骨性病变。

公开(公告)号：WO0061551A3

公开(公告)日：2000-12-28

申请号：PCT/EP0002746

申请日：2000-03-29

Applicant: BASF AG ,  ZECHEL JOHANN CHRISTIAN ,  KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  SADOWSKI JENS ,  HORNBERGER WILFRIED

Inventor： ZECHEL JOHANN-CHRISTIAN ,  KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  SADOWSKI JENS ,  HORNBERGER WILFRIED

IPC: C07D239/36 ,  A61K31/505 ,  A61K45/00 ,  A61K45/06 ,  A61P3/14 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  C07D239/34 ,  C07D239/60 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D239/46 ,  C07D403/04

CPC classification number: C07D405/14 ,  A61K45/06 ,  C07D239/34 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

Abstract: The invention relates to novel compounds that bind to integrin receptor ligands. The invention also relates to the production thereof, to their use as integrin receptor ligands and to their use for treating diseases, to pharmaceutical preparations that contain said compounds and to pharmaceutical preparations that contain at least one additional active compound.

Abstract translation: 本发明涉及一种结合于整联蛋白受体的新的化合物，它们的制备，它们作为整联的使用和用于治疗疾病的，含有这些化合物和含有至少一种其他活性化合物的药物制剂的药物制剂。

公开(公告)号：WO0110847A8

公开(公告)日：2001-12-06

申请号：PCT/EP0007440

申请日：2000-08-01

Applicant: BASF AG ,  KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HOLZENKAMP UTA ,  MACK HELMUT ,  SADOWSKI JENS ,  HORNBERGER WILFRIED ,  LAUX VOLKER

Inventor： KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HOLZENKAMP UTA ,  MACK HELMUT ,  SADOWSKI JENS ,  HORNBERGER WILFRIED ,  LAUX VOLKER

IPC: A61K31/4402 ,  A61K31/55 ,  A61K31/5513 ,  A61P3/14 ,  A61P5/18 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D213/74 ,  C07D223/20 ,  C07D243/38 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14 ,  C07D213/73 ,  C07D491/04

CPC classification number: C07D401/06 ,  C07D223/20 ,  C07D243/38 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14

Abstract: The invention relates to novel compounds of formula (I) which bind to integrin receptors, wherein G and L have the following meaning: L is a structural element of formula IL, wherein T represents a COOH group or a radical that can be hydrolyzed to obtain COOH and U- represents (XL)a-(CRL RL )b-, -CRL =CRL -, ethylene or =CRL -, wherein a is 0 or 1; b is 0, 1 or 2; XL represents CRL RL , NRL , oxygen or sulfur and G is a structural element of formula IG, wherein the insertion of structural element G can occur in both orientations and XO represents nitrogen or CRG . The invention also relates to the production of said compounds and to their use as medicaments.

Abstract translation: 本发明涉及式（I）的化合物BGL（I）其中G和L具有以下含义：L式IL -UT（IL），其中T是基团COOH或水解性与COOH和-U-自由基的结构元件 - （XL ）α-（CRL <1> RL <2>）b -CRL <1> CRL <1> CRL <2> - ，亚乙炔基或= CRL <1> - 表示，其中a是0或1，b 0,1或2 XL CRL <3> RL <4> NRL <5>，氧或硫，G是式LG（IG）的结构元件的结构元件G能够以两个方向和XG进行的，其中，所述安装是氮或CRG < 1与整联蛋白受体结合，它们的产生和它们作为药物的用途。

公开(公告)号：WO0110847A3

公开(公告)日：2001-11-01

申请号：PCT/EP0007440

申请日：2000-08-01

Applicant: BASF AG ,  KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HOLZENKAMP UTA ,  MACK HELMUT ,  SADOWSKI JENS ,  HORNBERGER WILFRIED ,  LAUX VOLKER

Inventor： KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HOLZENKAMP UTA ,  MACK HELMUT ,  SADOWSKI JENS ,  HORNBERGER WILFRIED ,  LAUX VOLKER

IPC: A61K31/4402 ,  A61K31/55 ,  A61K31/5513 ,  A61P3/14 ,  A61P5/18 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D213/74 ,  C07D223/20 ,  C07D243/38 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14 ,  C07D213/73 ,  C07D491/04

CPC classification number: C07D401/06 ,  C07D223/20 ,  C07D243/38 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14

Abstract: The invention relates to novel compounds of formula (I) which bind to integrin receptors, wherein G and L have the following meaning: L is a structural element of formula IL, wherein T represents a COOH group or a radical that can be hydrolyzed to obtain COOH and U- represents (XL)a-(CRL RL )b-, -CRL =CRL -, ethylene or =CRL -, wherein a is 0 or 1; b is 0, 1 or 2; XL represents CRL RL , NRL , oxygen or sulfur and G is a structural element of formula IG, wherein the insertion of structural element G can occur in both orientations and XO represents nitrogen or CRG . The invention also relates to the production of said compounds and to their use as medicaments.

Abstract translation: 本发明涉及式（I）的化合物BGL（I）其中G和L具有以下含义：L式IL -UT（IL），其中T是基团COOH或水解性与COOH和-U-自由基的结构元件 - （XL ）α-（CRL <1> RL <2>）b -CRL <1> CRL <1> CRL <2> - ，亚乙炔基或= CRL <1> - 表示，其中a是0或1，b 0,1或2 XL CRL <3> RL <4> NRL <5>，氧或硫，G是式LG（IG）的结构元件的结构元件G能够以两个方向和XG进行的，其中，所述安装是氮或CRG < 1>结合至整联蛋白受体，它们的制备和它们作为药物的用途。

公开(公告)号：CZ20013678A3

公开(公告)日：2002-07-17

申请号：CZ20013678

申请日：2000-03-29

Applicant: BASF AG

Inventor： ZECHEL JOHANN-CHRISTIAN ,  KLING ANDREAS ,  GENESTE HERVE ,  LANGE UDO ,  LAUTERBACH AMULF ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  SADOWSKI JENS ,  HORNBERGER WILFRIED

IPC: C07D239/36 ,  A61K31/505 ,  A61K45/00 ,  A61K45/06 ,  A61P3/14 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  C07D239/34 ,  C07D239/60 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D239/32 ,  C07D239/70 ,  C07D239/46 ,  A61K31/506 ,  A61K31/541 ,  A61K31/517 ,  A61P9/00 ,  A61P7/00 ,  A61P19/00 ,  A61P31/00

Abstract: The invention relates to novel compounds which bind to integrin receptors, to their preparation, to their use as integrin receptor ligands and for treating diseases, to pharmaceutical preparations comprising these compounds, and to pharmaceutical preparations comprising at least one other active compound.

公开(公告)号：BG106040A

公开(公告)日：2002-05-31

申请号：BG10604001

申请日：2001-10-23

Applicant: BASF AG

Inventor： KLING ANDREAS ,  LANGE UDO ,  LAUTERBACH ARNULF ,  GENESTE HERVE ,  SUBKOWSKI THOMAS ,  ZECHEL JOHANN-CHRISTIA ,  GRAEF CLAUDIA I ,  HORNBERGER WILFRIED

IPC: C12N9/99 ,  A61K31/27 ,  A61K31/381 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4406 ,  A61K31/443 ,  A61K31/4439 ,  A61K38/00 ,  A61K45/00 ,  A61K45/06 ,  A61P3/10 ,  A61P3/14 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P43/00 ,  C07C275/42 ,  C07D207/34 ,  C07D213/56 ,  C07D249/14 ,  C07D263/34 ,  C07D263/48 ,  C07D277/20 ,  C07D277/48 ,  C07D277/56 ,  C07D307/68 ,  C07D333/38 ,  C07D333/40 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07K5/02 ,  C07K5/023 ,  A61K38/04 ,  A61K31/33

Abstract: The invention relates to new compounds which bind to integrin receptors, as well as to their production, their use as integrin receptor antagonists and for the treatment of diseases, pharmaceutical preparations containing said compounds and pharmaceutical preparations containing at least one other active compound. 28 claims

公开(公告)号：DE10028575A1

公开(公告)日：2002-03-14

申请号：DE10028575

申请日：2000-06-14

Applicant: BASF AG

Inventor： GENESTE HERVE ,  KLING ANDREAS ,  LANGE UDO ,  LAUTERBACH ARNULF ,  SEITZ WERNER ,  GRAEF CLAUDIA ISABELLA ,  SUBKOWSKI THOMAS ,  HORNBERGER WILFRIED

IPC: A61K45/06 ,  A61P9/00 ,  C07D403/04 ,  C07D401/04 ,  C07D409/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  A61K31/55

Abstract: The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the αv&bgr;3 integrin receptor, and pharmaceutical preparations comprising these compounds.

公开(公告)号：CA2379977A1

公开(公告)日：2001-02-15

申请号：CA2379977

申请日：2000-08-01

Applicant: BASF AG

Inventor： HORNBERGER WILFRIED ,  LANGE UDO ,  GENESTE HERVE ,  KLING ANDREAS ,  SUBKOWSKI THOMAS ,  HOLZENKAMP UTA ,  MACK HELMUT ,  GRAEF CLAUDIA ISABELLA ,  LAUTERBACH ARNULF ,  LAUX VOLKER ,  SADOWSKI JENS

IPC: A61K31/4402 ,  A61K31/55 ,  A61K31/5513 ,  A61P3/14 ,  A61P5/18 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D213/74 ,  C07D223/20 ,  C07D243/38 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14 ,  C07D221/00 ,  C07D223/00 ,  C07D233/00 ,  C07D333/00 ,  C07D491/04 ,  C07D213/73

Abstract: The invention relates to novel compounds of formula (I) which bind to integr in receptors, wherein G and L have the following meaning: L is a structural element of formula IL, wherein T represents a COOH group or a radical that c an be hydrolyzed to obtain COOH and U- represents (XL)a-(CRL1RL2)b-, -CRL1=CRL2 -, ethylene or =CRL1-, wherein a is 0 or 1; b is 0, 1 or 2; XL represents CRL3RL4, NRL5, oxygen or sulfur and G is a structural element of formula IG, wherein the insertion of structural element G can occur in both orientations and XO represents nitrogen or CRG1. The invention also relates to the production of said compounds and to their use as medicaments.

公开(公告)号：ES2151741T3

公开(公告)日：2001-01-01

申请号：ES97934552

申请日：1997-07-29

Applicant: BASF AG

Inventor： BAUCKE DORIT ,  LANGE UDO ,  MACK HELMUT ,  PFEIFFER THOMAS ,  SEITZ WERNER ,  ZIERKE THOMAS

IPC: A61K31/40 ,  A61K31/44 ,  A61K38/00 ,  A61K38/05 ,  A61P1/18 ,  A61P7/02 ,  A61P11/02 ,  A61P11/06 ,  A61P17/00 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D207/22 ,  C07D211/78 ,  C07K5/00 ,  C07K5/02 ,  C07K5/083

Abstract: Compounds of the formula Iwhere R, R1, R2, R3, R4, R5 and R6, and l, m and n have the meanings stated in the description, and their preparation are described. The novel compounds are suitable for controlling diseases.

公开(公告)号：CA2371604A1

公开(公告)日：2000-11-09

申请号：CA2371604

申请日：2000-04-17

Applicant: BASF AG

Inventor： GENESTE HERVE ,  LANGE UDO ,  KLING ANDREAS ,  LAUTERBACH ARNULF ,  GRAEF CLAUDIA ISABELLA ,  HORNBERGER WILFRIED ,  ZECHEL JOHANN-CHRISTIAN ,  SUBKOWSKI THOMAS

IPC: C12N9/99 ,  A61K31/27 ,  A61K31/381 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4406 ,  A61K31/443 ,  A61K31/4439 ,  A61K38/00 ,  A61K45/00 ,  A61K45/06 ,  A61P3/10 ,  A61P3/14 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P43/00 ,  C07C275/42 ,  C07D207/34 ,  C07D213/56 ,  C07D249/14 ,  C07D263/34 ,  C07D263/48 ,  C07D277/20 ,  C07D277/48 ,  C07D277/56 ,  C07D307/68 ,  C07D333/38 ,  C07D333/40 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07K5/02 ,  C07K5/023 ,  A61K38/04 ,  A61K31/33

Abstract: The invention relates to new compounds which bind to integrin receptors, as well as to their production, their use as integrin receptor antagonists and for the treatment of diseases, pharmaceutical preparations containing said compounds and pharmaceutical preparations containing at least one other acti ve compound.