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31.发明授权Heterocyclic substituted alkylsulphonamides pharmaceutical compositions containing them, and arterial disease treatment therewith 失效杂环取代的烷基磺酰胺含有它们的药物组合物和用其进行动脉疾病治疗
公开(公告)号：US4931462A
公开(公告)日：1990-06-05
申请号：US287888
申请日：1988-12-21
IPC分类号： A61K31/34 , A61K31/343 , A61P7/02 , A61P9/00 , A61P11/08 , A61P11/14 , C07D209/42 , C07D307/85 , C07D333/70
CPC分类号： C07D307/85 , C07D209/42 , C07D333/70
摘要： New Sulphonamides of the formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are hydrogen or halogen atoms, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulphinyl, C.sub.1 -C.sub.6 -alkylsulphonyl or trifluoromethyl radicals or hydroxyl or cyano groups, R.sub.3 and R.sub.8, which can be the same or different, are hydrogen atoms, C.sub.1 -C.sub.6 -alkyl, benzyl or C.sub.1 -C.sub.6 -alkanoyl radicals, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or C.sub.1 -C.sub.6 -alkyl radicals, R.sub.6 and R.sub.7 are both hydrogen atoms or together form a valency bind, X is an oxygen or sulphur atom or an .dbd.NOH or .dbd.NR.sub.8 group and n is a whole number of from 1 to 4; and the physiologically acceptable salts thereof with inorganic and organic bases. These compounds are useful for example in the treatment of asthma or cardiovascular disease, thrombosis prevention and treatment, and to combat broncoconstriction.
摘要翻译： 新的具有下式的磺酰胺：其中R 1和R 2可以相同或不同，为氢或卤原子，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷硫基，C 1 C 1-6 - 烷基亚磺酰基，C 1 -C 6 - 烷基磺酰基或三氟甲基或羟基或氰基，可以相同或不同的R 3和R 8为氢原子，C 1 -C 6 - 烷基，苄基或C 1 -C 6 - 烷酰基， R4和R5可以相同或不同，是氢原子或C1-C6-烷基，R6和R7都是氢原子或一起形成价键，X是氧或硫原子或= NOH或= NR8组，n为1〜4的整数; 以及其与无机和有机碱的生理上可接受的盐。 这些化合物可用于例如治疗哮喘或心血管疾病，预防和预防血栓以及治疗支气管收缩。
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32.发明授权Hydroxamic acids and pharmaceutical compositions containing them, and anti-allergic use thereof 失效羟肟酸和含有它们的药物组合物及其抗过敏应用
公开(公告)号：US4906666A
公开(公告)日：1990-03-06
申请号：US11096
申请日：1987-02-05
IPC分类号： A61K31/10 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/235 , A61K31/26 , A61K31/275 , A61K31/41 , A61P11/00 , A61P29/00 , A61P37/08 , C07C67/00 , C07C313/00 , C07C315/02 , C07C317/18 , C07C317/44 , C07C323/12 , C07C323/14 , C07C323/20 , C07C323/52 , C07C323/54 , C07C323/60 , C07C325/00 , C07C331/04 , C07D257/04 , C07D257/06
CPC分类号： C07D257/04 , A61K31/10 , A61K31/26 , A61K31/275 , C07C323/12 , C07C323/52 , C07C323/60 , C07C331/04 , C07D257/06
摘要： The present invention provides compounds of the general formula: ##STR1## wherein Ar is a phenyl radical optionally substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen, A is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 aliphatic hydrocarbon radical which is optionally substituted by a hydroxyl group, n is 0, 1 or 2, B is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 -aliphatic hydrocarbon radical and R is 5-(1H)-tetrazolyl, --CO--NH-tetrazolyl, ##STR2## CN, SCN, OH, halogen, 5-(1H)-tetrazolylthio, ##STR3## or CO--O--NH--R.sub.1, wherein R.sub.1 is a hydrogen atom, an alkyl radical optionally substituted by cycloalkyl or an alkenyl, cycloalkyl, aralkyl or aryl radical, wherein the aromatic moiety can be substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen; and the pharmacologically acceptable salts thereof. The present invention also provides processes for preparing these compounds and pharmaceutical compositions containing them for combating allergic diseases.
摘要翻译： 本发明提供以下通式的化合物：其中Ar是任选被烷基，烯基，烷氧基，烷硫基，烷酰基，羟基，羟基烷基，羧基，烷氧基羰基，氨基甲酰基，硝基，氨基或卤素取代的苯基 A是直链或支链，饱和或不饱和的C1-C8脂族烃基，其任选被羟基取代，n是0,1或2，B是直链或支链的饱和或不饱和的C1- C8-脂族烃基，R是5-（1H） - 四唑基，-CO-NH-四唑基，CN，SCN，OH，卤素，5-（1H） - 四唑基硫代， NH-R1，其中R1是氢原子，任选被环烷基或烯基，环烷基，芳烷基或芳基取代的烷基，其中芳族部分可以被烷基，烯基，烷氧基，烷硫基，烷酰基，羟基，羟烷基 ，羧基，烷氧基羰基，氨基甲酰基，硝基，氨基或卤素; 及其药理学上可接受的盐。 本发明还提供了制备这些化合物的方法和含有它们的用于防治过敏性疾病的药物组合物。
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33.发明授权Coumarins connected via an oxyalkyl group with a piperidine ring having anti-allergic action 失效通过氧烷基连接的香豆素与具有抗过敏作用的哌啶环
公开(公告)号：US4330549A
公开(公告)日：1982-05-18
申请号：US104205
申请日：1979-12-17
IPC分类号： C07D409/14 , A61K31/085 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4468 , A61K31/4709 , A61P9/12 , A61P37/00 , A61P37/08 , C07D215/02 , C07D233/60 , C07D311/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/14 , A61K31/445 , C07D311/16
CPC分类号： C07D401/12 , Y10S514/826
摘要： The present invention provides aryl ether derivatives of the general formula: ##STR1## wherein A is an oxygen atom or the group >N--R.sub.1, R.sub.1 being a hydrogen atom or a lower alkyl radical, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.4 is a hydrogen atom or a hydroxyl group, R.sub.5 is a hydrogen atom or an acyl radical, R.sub.7 is a hydrogen atom, a lower alkyl radical or a lower alkanoyl radical and R.sub.8 is a hydrogen atom, a lower alkyl radical, a lower alkoxy radical or a hydroxyl group; and the pharmacologically acceptable salts thereof.The present invention also provides a process for the preparation of these compounds and pharmaceutical compositions containing them. It is also concerned with the use of these compounds for combating allergic diseases.
摘要翻译： 本发明提供以下通式的芳醚衍生物：其中A为氧原子或基团> N-R 1，R 1为氢原子或低级烷基，R 2和R 3可以相同或为 不同的是氢原子或低级烷基，R4是氢原子或羟基，R5是氢原子或酰基，R7是氢原子，低级烷基或低级烷酰基，R8是氢 原子，低级烷基，低级烷氧基或羟基; 及其药理学上可接受的盐。 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。 还关注这些化合物用于防治过敏性疾病。
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公开(公告)号：US4243807A
公开(公告)日：1981-01-06
申请号：US737518
申请日：1976-11-01
IPC分类号： C07D211/18 , C07D211/22 , C07D213/26 , C07D213/30
CPC分类号： C07D211/22 , C07D211/18
摘要： 4-Phenoxymethyl-piperidines of the formula ##STR1## wherein R is hydrogen, halogen, nitro, lower alkyl or lower alkoxy, in the form of the free base or an acid addition salt, are provided and they are useful as intermediates in the production of anti-hypertensive agents through condensation with (a) propyl chloride and then with an adenine, or (b) a propyl indole.
摘要翻译： 其中R为氢，卤素，硝基，低级烷基或低级烷氧基的式为“IMAGE”的4-苯氧基甲基 - 哌啶，以游离碱或酸加成盐的形式提供，它们可用作生产中的中间体 的抗高血压药通过与（a）丙基氯然后与腺嘌呤缩合，或（b）丙基吲哚。
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35.发明授权Pharmaceutically active derivatives of 9-[3-(4-amino-piperidino)-propyl]-adenines 失效9- [3-（4-氨基 - 哌啶子基） - 丙基] - 腺苷的药物活性衍生物
公开(公告)号：US4212866A
公开(公告)日：1980-07-15
申请号：US006050
申请日：1979-01-24
申请人： Walter-Gunar Friebe , Max Thiel , Androniki Roesch , Otto-Henning Wilhelms , Wolfgang Schaumann
发明人： Walter-Gunar Friebe , Max Thiel , Androniki Roesch , Otto-Henning Wilhelms , Wolfgang Schaumann
IPC分类号： A61K31/52 , A61P29/00 , A61P37/08 , C07D211/58 , C07D473/34 , C07D473/00
CPC分类号： C07D473/34 , C07D211/58 , Y10S514/826
摘要： Novel 9-[3-(4-amino-piperidino)-propyl]-adenine derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom, an aryl radical, a lower alkyl radical, a hydroxy lower alkyl radical, or together with R.sub.1 and the nitrogen atom to which they are attached form a heterocyclic ring, andR.sub.3 is a hydrogen atom or an acyl radical,or salts thereof with pharmacologically acceptable acids, characterized by anti-allergic, anti-inflammatory and anti-oedematous activity.
摘要翻译： 新颖的式[IMAGE]的9- [3-（4-氨基 - 哌啶子基） - 丙基] - 腺嘌呤衍生物，其中R1是氢原子或低级烷基，R2是氢原子，芳基，低级烷基 基团，羟基低级烷基或与R 1和它们所连接的氮原子一起形成杂环，并且R 3是氢原子或酰基，或其与药理学上可接受的酸的盐，其特征在于抗过敏 ，抗炎和抗水肿活性。
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36.发明授权Blood pressure lowering and adrenergic .beta.-receptor inhibiting 3-(4-phenoxymethylpiperidino)-propyl-phenyl ethers 失效血压降低和ADRENERGIC“ - 抑制3-（4-苯甲酰氨基哌啶）丙基苯基醚
公开(公告)号：US4146630A
公开(公告)日：1979-03-27
申请号：US846057
申请日：1977-10-27
申请人： Wolfgang Kampe , Walter-Gunar Friebe , Fritz Wiedemann , Gisbert Sponer , Wolfgang Bartsch , Karl Dietmann
发明人： Wolfgang Kampe , Walter-Gunar Friebe , Fritz Wiedemann , Gisbert Sponer , Wolfgang Bartsch , Karl Dietmann
IPC分类号： C07D401/12 , A61K31/403 , A61K31/4184 , A61K31/44 , A61K31/4427 , A61K31/445 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D209/90 , C07D211/22 , C07D231/56
CPC分类号： C07D211/22 , C07D231/56
摘要： A 3-(4-phenoxymethylpiperidino)-propyl-phenyl-ether of the formula ##STR1## wherein R.sub.1 and R.sub.2 each independently is hydrogen, lower alkyl, hydroxyalkyl, lower alkanoyloxyalkyl or --CO--Z,Z is hydroxy, lower alkyloxy or ##STR2## R.sub.6 and R.sub.7 each independently is hydrogen, lower alkyl or hydroxyalkyl,R.sub.3 is hydrogen or --O--R.sub.8,R.sub.8 is hydrogen, lower alkanoyl or aroyl optionally substituted by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, hydroxyl, alkylthio, nitrile, nitro or trifluoromethyl,R.sub.4 and R.sub.5 each independently is hydrogen, halogen, hydroxy, benzyloxy, lower alkyl, lower alkoxy, lower alkylthio, carboxy, benzyloxycarbonyl or lower alkoxycarbonyl,X and Y each independently is nitrogen or ##STR3## R.sub.9 is hydrogen, lower allkyl optionally substituted by --O--R.sub.8, or --CO--Z,or a pharmacologically acceptable salt thereof. The compounds lower blood pressure and inhibit adrenergic .beta.-receptors.
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公开(公告)号：US07205326B2
公开(公告)日：2007-04-17
申请号：US10833721
申请日：2004-04-28
IPC分类号： A61K31/422 , C07D263/30 , C07D413/02
CPC分类号： C07D413/12 , C07D413/14
摘要： Compounds of formula (I) are useful in the therapy and/or prevention of illnesses with known over-expression of receptor tyrosine kinases of the HER-family like HER-2 and EGFR (HER-1). Accordingly, these compounds are useful for the treatment of diseases such as cancer in humans or animals.
摘要翻译： 式（I）化合物
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公开(公告)号：US20060211750A1
公开(公告)日：2006-09-21
申请号：US11226677
申请日：2005-09-14
IPC分类号： A61K31/422 , C07D413/02
CPC分类号： C07D413/12
摘要： The present invention relates to 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 such compounds and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.
摘要翻译： 本发明涉及式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物，上述化合物的制备，含有这些化合物的组合物及其制备方法以及这些化合物在 控制或预防癌症等疾病。
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公开(公告)号：US20050267179A1
公开(公告)日：2005-12-01
申请号：US11132082
申请日：2005-05-18
申请人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Lothar Kling , Ulrike Reiff , Edgar Voss
发明人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Lothar Kling , Ulrike Reiff , Edgar Voss
IPC分类号： A61K31/422 , A61P35/00 , C07D413/02 , C07D413/12
CPC分类号： C07D413/12
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above 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，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，以及上述化合物在 控制或预防癌症等疾病。
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40.发明申请Novel arylazole derivatives, their manufacture and use as pharmaceutical agents 失效新型芳基唑衍生物，其制造和用作药剂公开(公告)号：US20050124670A1
公开(公告)日：2005-06-09
申请号：US10965996
申请日：2004-10-15
IPC分类号： A61K31/4155 , A61K31/4192 , A61K31/422 , A61K31/426 , C07D413/14 , C07D417/14 , C07D277/38 , A61K31/427 , C07D413/02 , C07D417/02
CPC分类号： C07D417/14 , C07D413/14
摘要： There are presented compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms thereof, 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： 提供式（I）化合物的药学上可接受的盐，其对映体形式，非对映异构体和外消旋物，上述化合物的制备，含有它们的药物及其制备，以及上述化合物在 控制或预防癌症等疾病。
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