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11. 发明授权

US06677360B2 Biphenyl and biphenyl-analogous compounds as integrin antagonists 失效
标题翻译：联苯和联苯类似物作为整联蛋白拮抗剂
公开(公告)号：US06677360B2
公开(公告)日：2004-01-13
申请号：US09828514
申请日：2001-04-06
申请人： Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Härter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jörg Keldenich , Ulf Brueggemeier , Klemens Lustig
发明人： Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Härter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jörg Keldenich , Ulf Brueggemeier , Klemens Lustig
IPC分类号： C07C31119
CPC分类号： C07D213/40 , C07C237/36 , C07C271/22 , C07C275/42 , C07C311/06 , C07C311/09 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/19 , C07C311/29 , C07C311/43 , C07C311/47 , C07C317/14 , C07C323/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D207/34 , C07D213/38 , C07D213/55 , C07D213/74 , C07D213/75 , C07D213/82 , C07D231/18 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/30 , C07D235/32 , C07D261/10 , C07D263/58 , C07D277/42 , C07D277/54 , C07D277/82 , C07D285/10 , C07D285/135 , C07D285/14 , C07D295/096 , C07D295/13 , C07D295/15 , C07D295/215 , C07D307/52 , C07D333/34 , C07D333/48 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
摘要翻译：本发明涉及联苯和联苯类似物，其作为药物组合物的制备和用途，作为整联蛋白拮抗剂，特别涉及用于治疗和预防癌症，动脉硬化，再狭窄，溶骨性疾病如骨质疏松和眼科疾病根据本发明的化合物具有式（1）其中R 1，R 2，U，V，A，B，W，R 3，C和R 4具有如声称。

12. 发明授权

US06420396B1 Biphenyl and biphenyl-analogous compounds as integrin antagonists 失效
标题翻译： 2-甲磺酰基氨基-3-ä'（吡啶基氨基）甲基] -1,1'-联苯-4-基]丙酸及其处理方法
公开(公告)号：US06420396B1
公开(公告)日：2002-07-16
申请号：US09464237
申请日：1999-12-15
申请人： Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Härter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jörg Keldenich , Ulf Brueggemeier , Klemens Lustig
发明人： Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Härter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jörg Keldenich , Ulf Brueggemeier , Klemens Lustig
IPC分类号： C07D21374
CPC分类号： C07D213/40 , C07C237/36 , C07C271/22 , C07C275/42 , C07C311/06 , C07C311/09 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/19 , C07C311/29 , C07C311/43 , C07C311/47 , C07C317/14 , C07C323/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D207/34 , C07D213/38 , C07D213/55 , C07D213/74 , C07D213/75 , C07D213/82 , C07D231/18 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/30 , C07D235/32 , C07D261/10 , C07D263/58 , C07D277/42 , C07D277/54 , C07D277/82 , C07D285/10 , C07D285/135 , C07D285/14 , C07D295/096 , C07D295/13 , C07D295/15 , C07D295/215 , C07D307/52 , C07D333/34 , C07D333/48 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to 2-Mesitylsulfonylamino-3-{3′[(pyridinylamino)methyl][1,1-biphenyl]-4-yl}propanoic acid, pharmaceutical compositions thereof, their preparation, their use in the treatment of cancer, arteriosclerosis, restenosis, osteolytic disorders, ophthalmic disorders, and their use as integrin antagonists. The compounds according to the invention have the formula (I):
摘要翻译：本发明涉及2-间三甲苯磺酰氨基-3- {3'[（吡啶基氨基）甲基] [1,1-联苯] -4-基}丙酸，其药物组合物，其制备方法，其用于治疗癌症，动脉硬化，再狭窄，溶骨性疾病，眼科疾病及其作为整合素拮抗剂的用途。根据本发明的化合物具有式（I）：

13. 发明申请

US20050222247A1 Chroman derivatives 审中-公开
标题翻译：色原衍生物
公开(公告)号：US20050222247A1
公开(公告)日：2005-10-06
申请号：US10996230
申请日：2004-11-23
申请人： Stephen Boyer , Kentaro Hashimoto , Thomas Rolle , Peter Sandner , Beatrix Stelte-Ludwig , Hanna Tinel , Kerstin Henninger , Arnel Concepcion , Osamu Sakurai , Kanako Hirai , Tadashi Inoue , Yuki Mochizuki , Noriko Nunami , Masaomi Tajimi , Noriyuki Yamamoto , Yasuhiro Tsukimi
发明人： Stephen Boyer , Kentaro Hashimoto , Thomas Rolle , Peter Sandner , Beatrix Stelte-Ludwig , Hanna Tinel , Kerstin Henninger , Arnel Concepcion , Osamu Sakurai , Kanako Hirai , Tadashi Inoue , Yuki Mochizuki , Noriko Nunami , Masaomi Tajimi , Noriyuki Yamamoto , Yasuhiro Tsukimi
IPC分类号： A61K31/353 , A61K31/403 , A61K31/4192 , C07D311/58 , C07D405/12 , C07D311/74
CPC分类号： C07D311/58 , C07D405/12
摘要： This invention relates to chroman derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The chroman derivatives of the present invention have an excellent activity as BETA 3 antagonists and are useful for the prophylaxis and treatment of diseases associated with BETA 3 activity, in particular for the treatment of urological disorder or disease, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; and inflammatory disorders, such as asthma and COPD.
摘要翻译：本发明涉及可用作药物制剂的活性成分的苯并二氢吡喃衍生物及其盐。本发明的苯并二氢吡喃衍生物作为BETA 3拮抗剂具有优异的活性，可用于预防和治疗与BETA 3活性相关的疾病，特别是用于治疗泌尿系统疾病或疾病，如逼尿肌过度活动（膀胱过度活动症），尿失禁，神经源性逼尿肌反应性（逼尿肌hyperflexia），特发性逼尿肌过度活动（逼尿肌不稳定），良性前列腺增生和下尿路症状; 和炎症性疾病，如哮喘和COPD。

14. 发明授权

US06495545B1 1,4-benzodiazepinone derivatives and their use as integrin antagonists 失效
标题翻译： 1,4-苯并二氮杂酮衍生物及其作为整合素拮抗剂的用途
公开(公告)号：US06495545B1
公开(公告)日：2002-12-17
申请号：US09857981
申请日：2001-06-12
申请人： Klaus Urbahns , Delf Schmidt , Ulf Brüggemeier , Christoph Gerdes , Beatrix Stelte-Ludwig , Jörg Keldenich , Elke Stahl
发明人： Klaus Urbahns , Delf Schmidt , Ulf Brüggemeier , Christoph Gerdes , Beatrix Stelte-Ludwig , Jörg Keldenich , Elke Stahl
IPC分类号： C07D41314
CPC分类号： C07D413/14 , C07D417/14
摘要： The present invention relates to compounds of general formula (I) and their preparation and use for the production of pharmaceuticals, and pharmaceuticals comprising these compounds.
摘要翻译：本发明涉及通式（I）的化合物及其制备和制备药物的用途，以及包含这些化合物的药物。

15. 发明授权

US06589972B2 &bgr;-phenylalanine derivatives as integrin antagonists 失效
标题翻译： β-苯丙氨酸衍生物作为整联蛋白拮抗剂
公开(公告)号：US06589972B2
公开(公告)日：2003-07-08
申请号：US09867835
申请日：2001-05-30
申请人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
发明人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
IPC分类号： A01N4350
CPC分类号： C07C311/19 , C07C311/47
摘要： The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4′, —COOR4″, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.
摘要翻译：本发明涉及通式（1）的化合物，其中R 4是-SO 2 R 4'，-COOR 4“，-COR 4'， - CONR 4'2或-CSNR 4'2; R 4'是氢，取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4“是取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选被一个或两个亚甲基延伸的磺酰胺，酰胺，醚，酯，酮，脲，硫醚，亚砜或砜单元; X为N，O或S; 及其生理上可接受的盐和立体异构体。本发明还涉及制备式（1）化合物的方法，含有这些化合物中的至少一种的药物组合物，以及式（1）化合物在制备药物组合物中的用途具有整合素拮抗作用，特别是用于治疗和预防癌症，溶骨性疾病如骨质疏松症，动脉硬化，再狭窄和眼科疾病。

16. 发明授权

US06339083B1 Multiheterocyclic pharmAceuticals 失效
标题翻译：多杂环药物治疗
公开(公告)号：US06339083B1
公开(公告)日：2002-01-15
申请号：US09211274
申请日：1998-12-14
申请人： Klaus Urbahns , Delf Schmidt , Ulf Brueggemeier , Christoph Gerdes , Beatrix Stelte-Ludwig , Jörg Keldenich , Elke Stahl
发明人： Klaus Urbahns , Delf Schmidt , Ulf Brueggemeier , Christoph Gerdes , Beatrix Stelte-Ludwig , Jörg Keldenich , Elke Stahl
IPC分类号： A61K315513
CPC分类号： C07D413/14 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I): and their preparation and use for the production of pharmaceuticals, and pharmaceuticals comprising these compounds.
摘要翻译：本发明涉及通式（I）的化合物及其药物制备和用途以及包含这些化合物的药物。

17. 发明授权

US06291503B1 &bgr;-phenylalanine derivatives as integrin antagonists 失效
标题翻译： β-苯丙氨酸衍生物作为整联蛋白拮抗剂
公开(公告)号：US06291503B1
公开(公告)日：2001-09-18
申请号：US09232738
申请日：1999-01-15
申请人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
发明人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
IPC分类号： A01N4356
CPC分类号： C07C311/19 , C07C311/47
摘要： The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4, —COOR4′, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.
摘要翻译：本发明涉及通式（1）的化合物，其中R4是-SO2R4，-COOR4'，-COR4'，-CONR4'2或-CSNR4'2; R 4'是氢，取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4“是取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选被一个或两个亚甲基延伸的磺酰胺，酰胺，醚，酯，酮，脲，硫醚，亚砜或砜单元; X为N，O或S; 及其生理上可接受的盐和立体异构体。本发明还涉及制备式（1）化合物的方法，含有这些化合物中的至少一种的药物组合物，以及式（1）化合物在制备药物组合物中的用途具有整合素拮抗作用，特别是用于治疗和预防癌症，溶骨性疾病如骨质疏松症，动脉硬化，再狭窄和眼科疾病。

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