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1. 发明授权

US06887864B2 Azepane derivatives 失效
标题翻译： Azepane衍生物
公开(公告)号：US06887864B2
公开(公告)日：2005-05-03
申请号：US10383111
申请日：2003-03-06
申请人： Walter-Gunar Friebe , Birgit Masjost , Ralf Schumacher
发明人： Walter-Gunar Friebe , Birgit Masjost , Ralf Schumacher
IPC分类号： A61K31/55 , A61P35/00 , A61P43/00 , C07D223/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号： C07D401/12 , C07D223/12 , C07D401/14 , C07D403/12 , C07D405/14
摘要： This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.
摘要翻译：本发明提供了根据通式（I）的新型氮杂环庚烷衍生物或其药学上可接受的盐，其中符号在说明书中定义，以及其制备方法。根据本发明的化合物具有抗细胞增殖活性并显示出增加的血浆稳定性。

2. 发明授权

US07432291B2 Ether derivatives 失效
标题翻译：醚衍生物
公开(公告)号：US07432291B2
公开(公告)日：2008-10-07
申请号：US11083176
申请日：2005-03-17
申请人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Ulrike Reiff , Edgar Voss
发明人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Ulrike Reiff , Edgar Voss
IPC分类号： A61K31/41 , C07D249/04
CPC分类号： C07D417/12 , C07D413/12 , C07D413/14
摘要： The present invention provides the compounds of formula (I) their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明提供式（I）化合物的药学上可接受的盐或酯，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的组合物及其制备方法，以及上述用途，提及的化合物在控制或预防诸如癌症的疾病中。

3. 发明授权

US07247649B2 Oxazoles, their manufacture and use as pharmaceutical agents 失效
标题翻译：恶唑，其制造和用作药剂
公开(公告)号：US07247649B2
公开(公告)日：2007-07-24
申请号：US10910765
申请日：2004-08-03
申请人： Birgit Bossenmaier , Walter-Gunar Friebe , Ulrike Reiff , Matthias Rueth , Edgar Voss
发明人： Birgit Bossenmaier , Walter-Gunar Friebe , Ulrike Reiff , Matthias Rueth , Edgar Voss
IPC分类号： A61K31/422 , C07D263/30 , C07D413/12
CPC分类号： C07D413/12
摘要： The present invention relates to novel oxazoles of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明涉及式（I）的新颖恶唑，其药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备，以及上述用途控制或预防疾病如癌症的化合物。

4. 发明授权

US07097854B2 Amino alcohol derivatives, process for their production and pharmaceutical preparations and reagents containing these compounds 失效
标题翻译：氨基醇衍生物，其制备方法和药物制剂以及含有这些化合物的试剂
公开(公告)号：US07097854B2
公开(公告)日：2006-08-29
申请号：US10059207
申请日：2002-01-31
申请人： Walter-Gunar Friebe , Nikolaos Dimoudis , Uwe Michaelis , Bernhard Knipp
发明人： Walter-Gunar Friebe , Nikolaos Dimoudis , Uwe Michaelis , Bernhard Knipp
IPC分类号： A61K9/127 , A61K38/00 , A01N43/04
CPC分类号： C07D295/13 , A61K48/00 , C07C219/06 , C07D211/26
摘要： The present invention relates to new amino alcohol derivatives, process for the production thereof and medicaments and reagents containing these compounds.
摘要翻译：本发明涉及新的氨基醇衍生物，其制备方法以及含有这些化合物的药物和试剂。

5. 发明申请

US20050267178A1 Novel benzylether derivatives 失效
标题翻译：新型苄基醚衍生物
公开(公告)号：US20050267178A1
公开(公告)日：2005-12-01
申请号：US11131576
申请日：2005-05-18
申请人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Christian Geletneky , Guy Georges , Irene Kolm , Edgar Voss
发明人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Christian Geletneky , Guy Georges , Irene Kolm , Edgar Voss
IPC分类号： C07D413/12 , C07D521/00 , A61K31/422 , C07D413/02
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D413/12
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）化合物的药学上可接受的盐或酯，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物组合物及其制备方法，以及使用上述化合物控制或预防诸如癌症等疾病。

6. 发明申请

US20050203064A1 Novel oxidized thioether derivatives 失效
标题翻译：新型氧化型硫醚衍生物
公开(公告)号：US20050203064A1
公开(公告)日：2005-09-15
申请号：US11073065
申请日：2005-03-04
申请人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Lothar Kling , Matthias Rueth , Edgar Voss
发明人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Lothar Kling , Matthias Rueth , Edgar Voss
IPC分类号： C07D413/12 , C07D417/12 , A61K31/675 , A61K31/4164 , A61K31/421 , A61K31/426 , C07D263/30 , C07D277/22
CPC分类号： C07D417/12 , C07D413/12
摘要： The present invention provides the compounds of formula I their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明提供式I化合物的药学上可接受的盐或酯，对映异构体形式，非对映异构体和外消旋物，上述化合物的制备，含有它们的药物组合物及其制备方法以及使用上述控制或预防疾病如癌症的化合物。

7. 发明授权

US4904666A Pyrazolo(3,4-d)pyrimidine compounds, compositions and method of use 失效
标题翻译：吡唑并（3,4-d）嘧啶化合物，组合物和使用方法
公开(公告)号：US4904666A
公开(公告)日：1990-02-27
申请号：US181729
申请日：1988-04-14
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Otto-Henning Wilhelms
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Otto-Henning Wilhelms
IPC分类号： A61K31/505 , A61K31/519 , A61P11/08 , A61P11/16 , A61P29/00 , A61P37/08 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides pyrazolo[3,4-d]-pyrimidines of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 to C.sub.6 -alkyl radical, a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aryl radical, R.sub.2 is a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aralkyl or hetaralkyl radical with 1 to 6 carbon atoms in the alkyl moiety and substituted, if desired, one or more times by halogen, C.sub.1 to C.sub.6 -alkyl, hydroxyl, C.sub.1 to C.sub.6 -alkoxy, C.sub.1 to C.sub.3 -haloalkyl, C.sub.3 to C.sub.7 -alkoxy carbonyl, aminocarbonyl, C.sub.2 to C.sub.7 -alkylaminocarbonyl, C.sub.3 to C.sub.13 -dialkylaminocarbonyl, cyano or C.sub.1 to C.sub.6 -alkylthio and R.sub.3 is a hydrogen atom or a C.sub.2 to C.sub.6 -alkyl radical substituted, if desired, one or more times by hydroxyl or is a tetrahydrofuranyl or tetrahydropyranyl radical, with the proviso that R.sub.2 cannot be an unsubstituted benzyl radical when R.sub.1 is a methyl radical, and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要翻译：本发明提供通式如下的吡唑并[3,4-d] - 嘧啶：其中R 1为C 1至C 6 - 烷基，C 2至C 6链烯基，C 3至C 7环烷基基团或芳基，R 2是C 2至C 6 - 烯基，C 3至C 7 - 环烷基或在烷基部分具有1至6个碳原子的芳烷基或杂烷基，如果需要，卤素，C1至C6烷基，羟基，C1至C6烷氧基，C1至C3-卤代烷基，C3至C7-烷氧基羰基，氨基羰基，C2至C7-烷基氨基羰基，C3至C13-二烷基氨基羰基，氰基或C1至C6-烷硫基并且R 3是氢原子或C 2至C 6烷基如果需要，被羟基取代一次或多次，或者是四氢呋喃基或四氢吡喃基，条件是当R 1是甲基时，R 2不能是未被取代的苄基，以及其与无机和有机酸的生理上可接受的盐。本发明还提供了制备这些化合物的方法和含有它们的药物组合物。

8. 发明授权

US4853386A N.sup.6 -disubstituted purine derivatives, and pharmaceutical compositions containing them, useful for treating allergic diseases, bronchospastic and bronchoconstrictory conditions 失效
标题翻译： N6-二取代嘌呤衍生物和含有它们的药物组合物，其可用于治疗过敏性疾病，支气管痉挛和支气管收缩条件
公开(公告)号：US4853386A
公开(公告)日：1989-08-01
申请号：US897109
申请日：1986-08-15
申请人： Walter-Gunar Friebe , Otto-Henning Wilhelms
发明人： Walter-Gunar Friebe , Otto-Henning Wilhelms
IPC分类号： A61K31/52 , A61P11/08 , A61P37/08 , C07D473/00 , C07D473/16 , C07D473/34 , C07D473/40
CPC分类号： C07D473/00 , C07D473/16 , C07D473/34
摘要： The present invention provides N.sup.6 -disubstituted purine derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.4 are the same or different and each represents a hydrogen or halogen atom or an --NR.sub.6 R.sub.7 group, R.sub.2 and R.sub.3 are the same or different and each represents a C.sub.1 -C.sub.6 alkyl radical, a C.sub.2 -C.sub.6 alkenyl radical, a C.sub.3 -C.sub.7 cycloalkyl radical, a phenalkyl radical containing up to 4 carbon atoms in the alkyl moiety, which can be straight-chained or branched, the phenyl moiety of which can be substituted one or more times by halogen, hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio or trifluoromethyl; a furylmethyl or furylethyl radical, a thiophenemethyl or thiopheneethyl radical, a pyridylmethyl or pyridylethyl radical optionally substituted by a C.sub.1 -C.sub.4 alkyl radical, an indanyl radical or a tetrahydronaphthyl radical, R.sub.5 is a hydrogen atom, a tetrahydrofuranyl or tetrahydropyranyl radical or a C.sub.1 -C.sub.10 radical which is optionally substituted one or more times by hydroxyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.2 -C.sub.6 carboxyalkanoyloxy, C.sub.2 -C.sub.6 hydroxyalkoxy, C.sub.3 -c.sub.6 dihydroxyalkoxy, carboxyl, cyano or 1H-tetrazol-5-yl radical, R.sub.6 and R.sub.7 are the same or different and each represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical or together represent a C.sub.2 -C.sub.5 alkylene radical optionally interrupted by oxygen, sulphur or an NR.sub.8 group and R.sub.8 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical; as well as the pharmacologically acceptable salts thereof.
摘要翻译：本发明提供以下通式的N6-二取代的嘌呤衍生物：其中R 1和R 4相同或不同，并且各自表示氢或卤素原子或-NR 6 R 7基团，R 2和R 3相同或不同，各自表示C1-C6烷基，C2-C6链烯基，C3-C7环烷基，在烷基部分含有至多4个碳原子的苯烷基，其可以是直链或支链的，苯基其部分可以被卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6烷硫基或三氟甲基取代一次或多次; 呋喃基甲基或呋喃乙基，噻吩甲基或噻吩乙基，任选被C 1 -C 4烷基，茚满基或四氢萘基取代的吡啶基甲基或吡啶基，R5是氢原子，四氢呋喃基或四氢吡喃基或C1- C 1 -C 6烷氧基，C 1 -C 6烷氧基羰基，C 2 -C 6羧基烷酰氧基，C 2 -C 6羟基烷氧基，C 3 -C 6二羟基烷氧基，羧基，氰基或1H-四唑-5-基，R6和R7相同或不同，各自表示氢原子或C1-C6烷基，或一起代表任选被氧，硫或NR8基中断的C2-C5亚烷基，R8是氢原子或C1 -C6烷基; 以及其药理学上可接受的盐。

9. 发明授权

US4721717A .alpha.-(aminoalkylaminomethyl)phenylmethanols, composition containing them, and use thereof to treat certain heart and circulatory diseases 失效
标题翻译： α-（氨基烷基氨基甲基）苯基甲醇，含有它们的组合物及其用于治疗某些心脏和循环系统疾病的用途
公开(公告)号：US4721717A
公开(公告)日：1988-01-26
申请号：US760128
申请日：1985-07-29
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Erwin Bohm , Klaus Strein
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Erwin Bohm , Klaus Strein
IPC分类号： A61K31/135 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P9/00 , C07C67/00 , C07C213/00 , C07C213/04 , C07C215/30 , C07C215/60 , C07C301/00 , C07C303/40 , C07C311/08 , C07C313/00 , C07C315/04 , C07C317/32 , C07C317/36 , C07C317/48 , C07D209/30 , C07D231/38 , C07D231/56 , C07D235/04 , C07D239/54 , C07D235/30 , C07D239/10
CPC分类号： C07D231/38 , C07D231/56
摘要： The present invention provides aminoalcohols of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be same or different, are hydrogen atoms, hydroxyl groups, C.sub.1 -C.sub.4 -alkoxy, benzyloxy, C.sub.1 -C.sub.4 -alkoxycarbonyl, C.sub.1 -C.sub.4 -alkanesulphonylamino, C.sub.1 -C.sub.4 -alkanesulphinyl or C.sub.1 -C.sub.4 -alkanesulphonyl radicals, m is 2, 3 or 4, X and Y, which can be the same or different, are hydrogen atoms or benzyl radicals and R.sub.3 is a phenyl radical substituted twice by C.sub.1 -C.sub.6 -alkyl radicals, a nitrophenyl radical, an aminophenyl radical, a 1,3,5-tri-C.sub.1 -C.sub.6 -alkyl-2,4-dioxo-1H,3H-pyrimidin-6-yl radical, an indolyl radical, an indazolyl radical, a benzimidazolyl radical, a 1,4-di-C.sub.1 -C.sub.6 -alkylpyrazol-5-yl radical or a radical of the general formula: ##STR2## wherein R.sub.4 and R.sub.5, which can be the same or different, are C.sub.1 -C.sub.4 -alkyl radicals and R.sub.6 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, phenyl or benzyl radical; and the pharmacologically acceptable salts there, as well as methods for making and using these compounds and compositions containing them. There are useful as cardiovascular medicaments.
摘要翻译：本发明提供以下通式的氨基醇：其中R 1和R 2可以相同或不同，为氢原子，羟基，C 1 -C 4 - 烷氧基，苄氧基，C 1 -C 4 - 烷氧基羰基，C 1 C 1-4烷基磺酰基氨基，C 1 -C 4烷基亚磺酰基或C 1 -C 4烷基磺酰基，m为2,3或4，X和Y可相同或不同，为氢原子或苄基，R 3为苯基由C 1 -C 6烷基取代两次，硝基苯基，氨基苯基，1,3,5-三-C1- C6-烷基-2,4-二氧代-1H，3H-嘧啶-6-基，吲哚基，吲唑基，苯并咪唑基，1,4-二-C1- C6烷基吡唑-5-基或通式如下的基团：其中R4和R5可以是 C 1 -C 4 - 烷基，R 6是C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，苯基或苄基; 和其中的药理学上可接受的盐，以及制备和使用这些化合物和含有它们的组合物的方法。有用的心血管药物。

10. 发明授权

US4382943A Anti-allergic aryl ether derivatives 失效
标题翻译：抗过敏芳基醚衍生物
公开(公告)号：US4382943A
公开(公告)日：1983-05-10
申请号：US280434
申请日：1981-07-06
申请人： Werner Winter , Walter-Gunar Friebe , Androniki Roesch , Otto-Henning Wilhelms
发明人： Werner Winter , Walter-Gunar Friebe , Androniki Roesch , Otto-Henning Wilhelms
IPC分类号： C07D409/14 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P37/08 , C07D401/12 , C07D405/12 , C07D405/14 , C07D405/06
CPC分类号： C07D401/12
摘要： An aryl ether derivative of the formula ##STR1## in which A is an oxygen atom or an >N--R.sub.1 grouping,R.sub.1 is a hydrogen atom or a lower alkyl radical,B is an alkylene radical containing 2 to 4 carbon atoms,R.sub.2 and R.sub.3 each independently is a hydrogen or halogen atom, hydroxyl group or lower alkyl, lower alkoxy or lower alkanoyl radical,R.sub.4 is a hydrogen atom or an acyl radical, andn is an integer from 1 to 5,or a pharmacologically acceptable salt thereof, which possesses anti-allergic activity.
摘要翻译：其中A是氧原子或> N-R 1基团的式“IMAGE”的芳基醚衍生物，R 1是氢原子或低级烷基，B是含有2至4个碳原子的亚烷基，R 2和 R3各自独立地为氢或卤原子，羟基或低级烷基，低级烷氧基或低级烷酰基，R4为氢原子或酰基，n为1至5的整数，或其药理学上可接受的盐，其具有抗过敏活性。

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