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1. 发明授权

US6034115A Indolyl-substituted phenylacetic acid derivatives 失效
公开(公告)号：US6034115A
公开(公告)日：2000-03-07
申请号：US761922
申请日：1996-12-09
申请人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Stefan Lohmer , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
发明人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Stefan Lohmer , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/435 , A61P3/06 , A61P9/00 , A61P9/10 , C07D209/08 , C07D209/42 , C07D235/16 , C07D471/04 , C07D235/08 , C07D235/10 , C07D235/18
CPC分类号： C07D471/04 , C07D209/08 , C07D209/42 , C07D235/16
摘要： The indolyl-substituted phenylacetic acid derivatives are prepared by reacting the corresponding phenylacetic acids with the required amines. The indolyl-substituted phenylacetic acid derivatives are suitable as active compounds in medicaments, in particular in antiarteriosclerotic medicaments.

2. 发明授权

US5811429A Bicyclic heterocyclic compounds 失效
公开(公告)号：US5811429A
公开(公告)日：1998-09-22
申请号：US761921
申请日：1996-12-09
申请人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Stefan Lohmer , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
发明人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Stefan Lohmer , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
IPC分类号： C07D237/06 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/517 , A61K31/535 , A61K31/5355 , A61K31/54 , A61K31/541 , A61K31/5415 , A61P3/06 , A61P9/10 , C07D209/48 , C07D235/08 , C07D235/10 , C07D235/28 , C07D237/32 , C07D239/91 , C07D263/58 , C07D265/36 , C07D275/06 , C07D277/20 , C07D277/56 , C07D279/16 , C07D401/04 , C07D409/04 , C07D417/04 , C07D471/04 , C07D498/04 , C07D239/72 , C07D413/00
CPC分类号： C07D209/48 , C07D235/08 , C07D235/10 , C07D235/28 , C07D237/32 , C07D239/91 , C07D263/58 , C07D275/06 , C07D279/16 , C07D401/04 , C07D409/04 , C07D417/04
摘要： The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.

3. 发明授权

US6025378A Bicyclic heterocyclic compounds 失效
标题翻译：双环杂环化合物
公开(公告)号：US6025378A
公开(公告)日：2000-02-15
申请号：US99557
申请日：1998-06-18
申请人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Stefan Lohmer , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
发明人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Stefan Lohmer , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
IPC分类号： C07D237/06 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/517 , A61K31/535 , A61K31/5355 , A61K31/54 , A61K31/541 , A61K31/5415 , A61P3/06 , A61P9/10 , C07D209/48 , C07D235/08 , C07D235/10 , C07D235/28 , C07D237/32 , C07D239/91 , C07D263/58 , C07D265/36 , C07D275/06 , C07D277/20 , C07D277/56 , C07D279/16 , C07D401/04 , C07D409/04 , C07D417/04 , C07D471/04 , C07D498/04 , A61K31/42 , A61K31/47 , C07D215/00 , C07D263/04 , C07D263/30 , C07D403/02 , C07D413/00
CPC分类号： C07D209/48 , C07D235/08 , C07D235/10 , C07D235/28 , C07D237/32 , C07D239/91 , C07D263/58 , C07D275/06 , C07D279/16 , C07D401/04 , C07D409/04 , C07D417/04
摘要： The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.
摘要翻译：双环杂环化合物通过相应地取代的羧酸与胺，特别是苯基甘氨酚的反应来制备。根据本发明的双环杂环化合物适合作为药物中的活性化合物，特别是具有抗动脉粥样硬化作用的药物。

4. 发明授权

US5714494A Xanthines in the 7th position with a benzyl acetic acid moiety 失效
标题翻译：第七位的黄嘌呤与苄基乙酸部分
公开(公告)号：US5714494A
公开(公告)日：1998-02-03
申请号：US710503
申请日：1996-09-18
申请人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Stefan Lohmer , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
发明人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Stefan Lohmer , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
IPC分类号： A61K31/52 , A61K31/522 , A61P9/00 , A61P9/10 , C07D473/06 , C07D473/08 , C07D473/22
CPC分类号： C07D473/06 , C07D473/08
摘要： Substituted xanthines of formula ##STR1## in which A represents a radical of the formula ##STR2## in which R.sup.3, R.sup.4, R.sup.6 and R.sup.7 denote hydrogen, cycloalkyl, aryl having 6 to 10 carbon atoms, or denote straight-chain of branched alkyl or alkenyl, each of which is optionally substituted; T, V, X and Y are identical or different and denote an oxygen or sulphur atom; R.sup.5 and R.sup.8 are identical or different and denote hydrogen, halogen, cycloalkyl having 3 to 8 carbon atoms or straight-chain or branched alkyl or alkenyl in each case having up to 8 carbon atoms, optionally substituted or R.sup.5 and R.sup.8 denote aryl having 6 to 10 carbon atoms or a 5- to 7-membered aromatic, optionally benzo-fused heterocycle having up to 3 heteroatoms S, N and/or O, each of which is optionally substituted; L represents an oxygen or sulphur atom; R.sup.2 represents mercapto, hydroxyl, straight-chain or branched alkoxy having up to 8 carbon atoms or the group of the formula ##STR3## in which R.sup.13 denotes hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms; R.sup.14 denotes hydrogen, phenyl or a 5- to 6-membered aromatic heterocycle having up to 3 heteroatoms S, N and/or O; and R.sup.15 denotes hydrogen or straight-chain or branched alkyl having up to 8 carbon atom, optionally substituted by hydroxyl, and their salts are prepared by reaction of the suitable unsubstituted xanthines with halogenomethylphenylacetic acids and subsequent reaction of the carboxylic esters or acids with phenylglycinolamine. The substituted xanthines are suitable as active compounds in medicaments, in particular in antiatherosclerotic medicaments.
摘要翻译：式（I）的取代黄嘌呤其中A表示式为“IMAGE”的基团，其中R 3，R 4，R 6和R 7表示氢，环烷基，具有6至10个碳原子的芳基，或表示直链支链烷基或烯基，其各自任选被取代; T，V，X和Y相同或不同，表示氧或硫原子; R5和R8相同或不同，表示氢，卤素，具有3-8个碳原子的环烷基或具有至多8个碳原子的直链或支链烷基或链烯基，任选取代或R 5和R 8表示具有6至 10个碳原子或5至7元芳族，任选苯并稠合的杂环，其具有至多3个杂原子S，N和/或O，每个杂原子任选被取代; L表示氧或硫原子; R 2表示具有至多8个碳原子的巯基，羟基，直链或支链烷氧基或式“IMAGE”的基团，其中R13表示氢或具有至多4个碳原子的直链或支链烷基; R14表示氢，苯基或具有至多3个S，N和/或O的杂原子的5至6元芳族杂环; 并且R 15表示氢或具有至多8个碳原子的直链或支链烷基，任选被羟基取代，并且它们的盐通过合适的未取代黄嘌呤与卤代甲基苯基乙酸的反应制备，随后羧酸酯或酸与苯基甘氨酚的反应来制备。取代黄嘌呤在药物，特别是抗动脉粥样硬化药物中适合作为活性化合物。

5. 发明授权

US5747505A Heterocyclic aryl-, alkyl- and cycloalkylacetamides 失效
标题翻译：杂环芳基，烷基和环烷基乙酰胺
公开(公告)号：US5747505A
公开(公告)日：1998-05-05
申请号：US717027
申请日：1996-09-20
申请人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Martin Beuck , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
发明人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Martin Beuck , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61P3/06 , A61P9/08 , A61P9/10 , C07C69/732 , C07C69/734 , C07D213/65 , C07D215/14 , C07D401/12 , C07D409/12 , C07D215/12 , C07D217/12
CPC分类号： C07D401/12 , C07C69/732 , C07C69/734 , C07D213/65 , C07D215/14 , C07D409/12
摘要： The heterocyclic aryl-, alkyl- and cycloalklacetamides are prepared by reacting the appropriately substituted acetic acids with amines, if appropriate in complexed form. The heterocyclic aryl-, alkyl- and cycloalkylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.
摘要翻译：杂环芳基 - ，烷基 - 和环烷基乙酰胺通过使适当取代的乙酸与胺反应制备，如果合适的话，可以配合形式。杂环芳基 - ，烷基 - 和环烷基乙酰胺可用作药物中的活性化合物，特别是抗动脉粥样硬化药物。

6. 发明授权

US5849751A Amides and sulphonamides of benzylamines having heterocyclic substituents 失效
标题翻译：具有杂环取代基的苄胺的酰胺和磺酰胺
公开(公告)号：US5849751A
公开(公告)日：1998-12-15
申请号：US675668
申请日：1996-07-03
申请人： Ulrich Muller , Richard Connell , Hilmar Bischoff , Dirk Denzer , Stefan Lohmer , Stefan Wohlfeil , Rudi Grutzmann
发明人： Ulrich Muller , Richard Connell , Hilmar Bischoff , Dirk Denzer , Stefan Lohmer , Stefan Wohlfeil , Rudi Grutzmann
IPC分类号： A61K31/435 , A61P3/06 , A61P9/00 , A61P9/10 , C07D471/04 , A61K31/44
CPC分类号： C07D471/04
摘要： Amides and sulphonamides of benzylamines having heterocyclic substituents are prepared by first converting the corresponding carboxylic acids into the corresponding amines and then substituting these on the amine nitrogen in a corresponding manner. The new amides and sulphonamides of benzylamines having heterocyclic substituents can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.
摘要翻译：通过首先将相应的羧酸转化为相应的胺，然后以相应的方式将其替换在胺氮上来制备具有杂环取代基的苄胺的酰胺和磺酰胺。具有杂环取代基的苄胺的新酰胺和磺酰胺可用作药物中的活性化合物，特别是抗动脉粥样硬化药物。

7. 发明授权

US5684014A Cycloalkano-indole and -azaindole derivatives 失效
标题翻译：环烷基 - 吲哚和-azaindole衍生物
公开(公告)号：US5684014A
公开(公告)日：1997-11-04
申请号：US535698
申请日：1995-09-28
申请人： Ulrich Muller , Richard Connell , Siegfried Goldmann , Rudi Grutzmann , Martin Beuck , Hilmar Bischoff , Dirk Denzer , Anke Domdey-Bette , Stefan Wohlfeil
发明人： Ulrich Muller , Richard Connell , Siegfried Goldmann , Rudi Grutzmann , Martin Beuck , Hilmar Bischoff , Dirk Denzer , Anke Domdey-Bette , Stefan Wohlfeil
IPC分类号： C07D209/86 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/435 , A61K31/4353 , A61K31/44 , A61P1/00 , A61P3/04 , A61P3/06 , A61P9/08 , A61P9/10 , C07D20060101 , C07D209/00 , C07D209/82 , C07D209/94 , C07D219/02 , C07D221/00 , C07D471/04 , C07D471/02
CPC分类号： C07D471/04 , C07D219/02
摘要： Cycloalkano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.
摘要翻译：通过适当取代的羧酸与胺的反应制备环烷基 - 吲哚和吖啶衍生物。环烷基 - 吲哚和吖啶衍生物适合用作药物，优选抗动脉粥样硬化药物的活性化合物。

8. 发明授权

US5925646A Heterocyclic aryl-, alkyl- and cycloalkylacetamides 失效
标题翻译：杂环芳基，烷基和环烷基乙酰胺
公开(公告)号：US5925646A
公开(公告)日：1999-07-20
申请号：US8709
申请日：1998-01-16
申请人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Martin Beuck , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
发明人： Richard Connell , Siegfried Goldmann , Ulrich Muller , Martin Beuck , Hilmar Bischoff , Dirk Denzer , Rudi Grutzmann , Stefan Wohlfeil
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61P3/06 , A61P9/08 , A61P9/10 , C07C69/732 , C07C69/734 , C07D213/65 , C07D215/14 , C07D401/12 , C07D409/12 , A61K31/445 , C07C233/11 , C07D213/51
CPC分类号： C07D401/12 , C07C69/732 , C07C69/734 , C07D213/65 , C07D215/14 , C07D409/12
摘要： The heterocyclic aryl-, alkyl- and cycloalkylacetamides are prepared by reacting the appropriately substituted acetic acids with amines, if appropriate in complexed form. The heterocyclic aryl-, alkyl- and cycloalkylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.
摘要翻译：杂环芳基 - ，烷基 - 和环烷基乙酰胺通过使适当取代的乙酸与胺反应制备，如果合适的话可以配合形式。杂环芳基 - ，烷基 - 和环烷基乙酰胺可用作药物中的活性化合物，特别是抗动脉粥样硬化药物。

9. 发明授权

US5693650A 4-(Quinolin-2-yl-methoxy)-phenyl-acetic acid derivatives 失效
标题翻译： 4-（喹啉-2-基 - 甲氧基） - 苯基 - 乙酸衍生物
公开(公告)号：US5693650A
公开(公告)日：1997-12-02
申请号：US567764
申请日：1995-12-05
申请人： Ulrich Muller , Richard Connell , Siegfried Goldmann , Klaus-Helmut Mohrs , Rolf Angerbauer , Matthias Muller-Gliemann , Ulrich Niewohner , Rudi Grutzmann , Martin Beuck , Stefan Wohlfeil , Hilmar Bischoff , Dirk Denzer
发明人： Ulrich Muller , Richard Connell , Siegfried Goldmann , Klaus-Helmut Mohrs , Rolf Angerbauer , Matthias Muller-Gliemann , Ulrich Niewohner , Rudi Grutzmann , Martin Beuck , Stefan Wohlfeil , Hilmar Bischoff , Dirk Denzer
IPC分类号： A61K31/47 , A61K31/495 , A61K31/535 , A61P9/08 , A61P9/10 , C07D215/14 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07H13/04 , C07D215/12
CPC分类号： C07D401/12 , C07D215/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07H13/04
摘要： 4-(Quinolin-2-yl-methoxy)-phenyl-acetic acid derivatives are prepared by reacting quinoline-methoxy-phenyl-acetic acids with the corresponding glycinol derivatives, if appropriate with activation of the carboxylic acid function. The new compounds are suitable as active compounds in medicaments, in particular in antiatherosclerotic medicaments.
摘要翻译： 4-（喹啉-2-基 - 甲氧基） - 苯基 - 乙酸衍生物是通过使喹啉 - 甲氧基 - 苯基 - 乙酸与相应的甘油醇衍生物反应制备的，如果合适的话，羧酸官能团的活化。新化合物适合作为药物中的活性化合物，特别是抗动脉粥样硬化药物。

10. 发明授权

US5691337A Oxy-phenyl-(phenyl)glycinolamides with heterocyclic substituents 失效
标题翻译：具有杂环取代基的氧 - 苯基 - （苯基）甘氨酰胺
公开(公告)号：US5691337A
公开(公告)日：1997-11-25
申请号：US785146
申请日：1997-01-13
申请人： Ulrich Muller , Richard Connell , Siegfried Goldmann , Klaus-Helmut Mohrs , Siegfried Raddatz , Michael Matzke , Rudi Grutzmann , Martin Beuck , Stefan Wohlfeil , Hilmar Bischoff , Dirk Denzer
发明人： Ulrich Muller , Richard Connell , Siegfried Goldmann , Klaus-Helmut Mohrs , Siegfried Raddatz , Michael Matzke , Rudi Grutzmann , Martin Beuck , Stefan Wohlfeil , Hilmar Bischoff , Dirk Denzer
IPC分类号： A61K31/165 , A61K31/38 , A61K31/381 , A61K31/47 , A61K31/472 , A61K31/495 , A61P9/08 , A61P9/10 , C07C231/02 , C07C235/34 , C07D215/14 , C07D215/18 , C07D215/26 , C07D217/16 , C07D241/42 , C07D333/56 , C07D401/12 , C07D405/12 , C07F7/10 , C07D217/00
CPC分类号： C07D401/12 , C07C235/34 , C07D215/14 , C07D215/18 , C07D215/26 , C07D241/42 , C07D333/56 , C07D405/12
摘要： Oxy-phenyl-(phenyl)glycinolamides with heterocyclic substituents are prepared by reaction of the corresponding oxyphenylcarboxylic acids with heterocyclic substituents with phenylglycinol. The new substances are suitable as active compounds in medicaments, in particular in agents having an antiatherosclerotic action.
摘要翻译：具有杂环取代基的羟基 - 苯基 - （苯基）甘氨酰胺通过相应的氧基苯基羧酸与杂环取代基与苯基甘氨醇的反应来制备。这些新物质适合作为药物中的活性化合物，特别是具有抗动脉粥样硬化作用的药物。

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