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1. 发明授权

US4353904A Phenylpiperazine derivatives of 1,3,4-oxadiazolylphenols, and therapeutic agents containing these compounds 失效
标题翻译： 1,3,4-恶二唑基苯酚的苯基哌嗪衍生物和含有这些化合物的治疗剂
公开(公告)号：US4353904A
公开(公告)日：1982-10-12
申请号：US228370
申请日：1981-01-26
申请人： Peter C. Thieme , Albrecht Franke , Dieter Lenke , Hans D. Lehmann , Josef Gries
发明人： Peter C. Thieme , Albrecht Franke , Dieter Lenke , Hans D. Lehmann , Josef Gries
IPC分类号： C07D413/12 , A61K31/495 , A61K31/496 , A61P9/12 , C07D271/10
CPC分类号： C07D271/10
摘要： Novel phenylpiperazinylpropanols of 1,3,4-oxadiazolylphenols and their physiologically tolerated addition salts with acids, processes for their preparation, and pharmaceutical formulations which contain these compounds and are useful in the treatment of hypertonia.
摘要翻译： 1,3,4-恶二唑基酚的新型苯基哌嗪基丙醇及其与酸的生理学耐受加成盐，其制备方法和含有这些化合物并可用于治疗高渗的药物制剂。

2. 发明授权

US4305951A Novel amino derivatives of 5-(2-hydroxystyryl)-isoxazole, their preparation and therapeutic formulations containing these compounds 失效
标题翻译： 5-（2-羟基苯乙烯基） - 异恶唑的新型氨基衍生物，其制备方法和含有这些化合物的治疗制剂
公开(公告)号：US4305951A
公开(公告)日：1981-12-15
申请号：US199835
申请日：1980-10-23
申请人： Fritz-Frieder Frickel , Peter C. Thieme , Albrecht Franke , Hans Theobald , Dieter Lenke , Josef Gries
发明人： Fritz-Frieder Frickel , Peter C. Thieme , Albrecht Franke , Hans Theobald , Dieter Lenke , Josef Gries
IPC分类号： A61K31/42 , A61P9/00 , A61P9/12 , A61P25/02 , C07C43/12 , C07C45/61 , C07C45/64 , C07C45/70 , C07D261/08 , C07F9/653
CPC分类号： C07F9/653 , C07C43/12 , C07C45/61 , C07C45/64 , C07C45/70 , C07D261/08
摘要： Novel aminopropanol derivatives of 5-(2-hydroxystyryl)-isoxazole and their addition salts with acids, their preparation, pharmaceutical formulations containing these compounds, and their use in the treatment of hypertonia, coronary heart disease and cardiac arrhythmias.
摘要翻译： 5-（2-羟基苯乙烯基） - 异恶唑的新型氨基丙醇衍生物及其与酸的加成盐，其制备方法，含有这些化合物的药物制剂及其在治疗高血压，冠心病和心律失常中的应用。

3. 发明授权

US4428950A (Hetarylphenoxy)-(phenylpiperazinyl)-propanols, their preparation and drugs containing these compounds 失效
标题翻译：（丁基苯氧基） - （苯基哌嗪基） - 丙醇，它们的制备方法和含有这些化合物的药物
公开(公告)号：US4428950A
公开(公告)日：1984-01-31
申请号：US339508
申请日：1982-01-15
申请人： Albrecht Franke , Gerd Steiner , Peter C. Thieme , Dieter Lenke , Josef Gries , Hans-Juergen Teschendorf
发明人： Albrecht Franke , Gerd Steiner , Peter C. Thieme , Dieter Lenke , Josef Gries , Hans-Juergen Teschendorf
IPC分类号： C07D249/08 , A61K31/495 , A61K31/496 , A61K31/505 , A61P9/02 , A61P11/08 , A61P25/08 , A61P25/20 , C07D231/12 , C07D231/38 , C07D233/60 , C07D239/42 , C07D261/08 , C07D295/06 , C07D295/092 , C07D521/00 , C07D403/00
CPC分类号： C07D231/12 , C07D233/56 , C07D239/42 , C07D249/08 , C07D261/08 , C07D295/088 , Y10S514/923
摘要： Novel (hetarylphenoxy)-(phenylpiperazinyl)-propanols of the formula ##STR1## where R.sup.1 is hydrogen, amino or alkyl of 1 to 4 carbon atoms, R.sup.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy where alkyl is of 1 to 3 carbon atoms, the phenyl ring can be monosubstituted or disubstituted by R.sup.2, and the heterocyclic structure Het. is pyrimidinyl, triazol-1-yl, imidazol-1-yl, pyrazol-3-yl or isoxazol-3-yl, and their physiologically tolerated addition salts with acids, processes for their preparation, and pharmaceutical formulations which contain these compounds and exhibit predominantly hypotensive, sedative, neuroleptic and broncholytic properties.
摘要翻译：式（Ⅰ）的新型（杂芳基苯氧基） - （苯基哌嗪基） - 丙醇，其中R 1是氢，氨基或1-4个碳原子的烷基，R 2是氢，卤素，1-4个碳原子的烷基或烷氧基， 1至3个碳原子，苯环可以被R2单取代或二取代，并且杂环结构Het。是嘧啶基，三唑-1-基，咪唑-1-基，吡唑-3-基或异恶唑-3-基，以及它们与酸的生理耐受加成盐，其制备方法和含有这些化合物的药物制剂和展示主要是降血压，镇静，精神安定和支气管扩张性质。

4. 发明授权

US4251539A Amino derivatives of 3-alkyl-5-(2-hydroxystyryl)-isoxazoles 失效
标题翻译： 3-烷基-5-（2-羟基苯乙烯基） - 异恶唑的氨基衍生物
公开(公告)号：US4251539A
公开(公告)日：1981-02-17
申请号：US30927
申请日：1979-04-17
申请人： Peter C. Thieme , Fritz-Frieder Frickel , Hans Theobald , Albrecht Franke , Dieter Lenke , Josef Gries
发明人： Peter C. Thieme , Fritz-Frieder Frickel , Hans Theobald , Albrecht Franke , Dieter Lenke , Josef Gries
IPC分类号： A61K31/42 , A61P9/00 , A61P9/06 , A61P9/12 , A61P25/02 , C07D261/08
CPC分类号： C07D261/08
摘要： Alkylamino-propanol derivatives of 3-alkyl-5-(2-hydroxystyryl)-isoxazole, of the general formula ##STR1## where R is hydrogen, alkyl of 1 to 8 carbon atoms, which is unsubstituted or substituted by hydroxyl, alkoxy of 1 to 3 carbon atoms or cycloalkyl with 3 to 8 carbon atoms in the ring, alkenyl or alkynyl of 2 to 8 carbon atoms, or cycloalkyl with 3 to 8 carbon atoms in the ring, the cycloalkyl rings being unsubstituted or mono- or di-substituted by alkyl of 1 to 3 carbon atoms, and R' is alkyl of 1 to 4 carbon atoms, and their addition salts with physiologically acceptable acids, their preparation, and pharmaceutical formulations which contain these compounds and which can be used as valuable drugs in the treatment of hypertonia, coronary diseases of the heart and cardiac arrhythmias.
摘要翻译： 3-烷基-5-（2-羟基苯乙烯基） - 异恶唑的通式为：其中R为氢的烷基氨基丙醇衍生物，未取代或被羟基取代的碳原子数为1至8的烷基，烷氧基为1 至3个碳原子或环中具有3至8个碳原子的环烷基，2至8个碳原子的链烯基或炔基或环中具有3至8个碳原子的环烷基，环烷基环为未取代的或单或二取代的具有1至3个碳原子的烷基，R'是1至4个碳原子的烷基，以及它们与生理上可接受的酸的加成盐，它们的制备方法和含有这些化合物的药物制剂，并且可以在治疗高血压，心脏冠状动脉疾病和心律失常。

5. 发明授权

US4353917A Amino derivatives of 2-methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole, their preparation, and formulations containing these compounds 失效
标题翻译： 2-甲基-5-（2-羟基苯乙烯基）-1,3,4-噻二唑的氨基衍生物及其制备方法和含有这些化合物的制剂
公开(公告)号：US4353917A
公开(公告)日：1982-10-12
申请号：US199834
申请日：1980-10-23
申请人： Fritz-Frieder Frickel , Peter C. Thieme , Albrecht Franke , Helmut Hagen , Dieter Lenke , Josef Gries
发明人： Fritz-Frieder Frickel , Peter C. Thieme , Albrecht Franke , Helmut Hagen , Dieter Lenke , Josef Gries
IPC分类号： A61K31/41 , A61K31/433 , A61P9/00 , A61P9/12 , A61P25/02 , C07D285/12 , A61K31/425
CPC分类号： C07D285/12 , Y10S514/823
摘要： Novel aminopropanol derivatives of 2-methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole and their addition salts with acids, their preparation, pharmaceutical formulations containing these compounds, and their use as drugs in the treatment of coronary heart disease, hypertonia and cardiac arrhythmias.
摘要翻译： 2-甲基-5-（2-羟基苯乙烯基）-1,3,4-噻二唑的新型氨基丙醇衍生物及其与酸的加成盐，其制备方法，含有这些化合物的药物制剂及其在治疗冠心病中的用途疾病，高血压和心律失常。

6. 发明授权

US4305950A Pharmaceutical agent containing amino derivatives of 2-methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole 失效
标题翻译：含有2-甲基-5-（2-羟基苯乙烯基）-1,3,4-噻二唑的氨基衍生物的药剂
公开(公告)号：US4305950A
公开(公告)日：1981-12-15
申请号：US124218
申请日：1980-02-25
申请人： Peter C. Thieme , Fritz-Frieder Frickel , Helmut Hagen , Albrecht Franke , Dieter Lenke , Josef Gries
发明人： Peter C. Thieme , Fritz-Frieder Frickel , Helmut Hagen , Albrecht Franke , Dieter Lenke , Josef Gries
IPC分类号： A61K31/41 , A61K31/433 , A61P9/00 , A61P9/06 , A61P9/12 , C07D285/12 , A61K31/425
CPC分类号： C07D285/12 , Y10S514/821
摘要： Alkylaminopropanol derivatives of 2-methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole and their addition salts with acids, their preparation, and pharmaceutical formulations, containing these compounds, which may be used for the treatment of coronary diseases of the heart, of hypertonia and of cardiac arrhythmias.
摘要翻译： 2-甲基-5-（2-羟基苯乙烯基）-1,3,4-噻二唑的烷基氨基丙醇衍生物及其与酸的加成盐，其制备物和含有这些化合物的药物制剂，其可用于治疗冠状动脉疾病的心脏，高血压和心律失常。

7. 发明授权

US4237278A Amino derivatives of 2-methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole 失效
标题翻译： 2-甲基-5-（2-羟基苯乙烯基）-1,3,4-噻二唑的氨基衍生物
公开(公告)号：US4237278A
公开(公告)日：1980-12-02
申请号：US30842
申请日：1979-04-17
申请人： Peter C. Thieme , Fritz-Frieder Frickel , Helmut Hagen , Albrecht Franke , Dieter Lenke , Josef Gries
发明人： Peter C. Thieme , Fritz-Frieder Frickel , Helmut Hagen , Albrecht Franke , Dieter Lenke , Josef Gries
IPC分类号： A61K31/41 , A61K31/433 , A61P9/00 , A61P9/06 , A61P9/12 , C07D285/12 , A61K31/425 , C07D23/00
CPC分类号： C07D285/12 , Y10S514/821
摘要： Novel alkylaminopropanol derivatives of 2-methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole and their addition salts with acids, their preparation, and pharmaceutical formulations, containing these compounds, which may be used for the treatment of coronary diseases of the heart, of hypertonia and of cardiac arrhythmias.
摘要翻译： 2-甲基-5-（2-羟基苯乙烯基）-1,3,4-噻二唑的新型烷基氨基丙醇衍生物及其与酸的加成盐，其制备方法和含有这些化合物的药物制剂，其可用于治疗冠状动脉心脏疾病，高血压和心律失常。

8. 发明授权

US4619929A Phenylpiperazine derivatives of hetarylphenols and hetarylanilines, their preparation, and therapeutic agents containing these compounds 失效
标题翻译：苯二甲基苯酚和杂芳基苯胺的苯基哌嗪衍生物，它们的制备和含有这些化合物的治疗剂
公开(公告)号：US4619929A
公开(公告)日：1986-10-28
申请号：US590746
申请日：1984-03-19
申请人： Peter C. Thieme , Gerd Steiner , Wolfgang Rohr , Dieter Lenke , Josef Gries , Harald Weifenbach , Hans-Juergen Teschendorf , Hans P. Hofmann , Horst Kreiskott
发明人： Peter C. Thieme , Gerd Steiner , Wolfgang Rohr , Dieter Lenke , Josef Gries , Harald Weifenbach , Hans-Juergen Teschendorf , Hans P. Hofmann , Horst Kreiskott
IPC分类号： C07D249/08 , A61K31/495 , A61K31/496 , A61P9/02 , A61P11/00 , A61P25/20 , C07D231/12 , C07D233/60 , C07D233/61 , C07D271/10 , C07D295/06 , C07D295/067 , C07D295/096 , C07D521/00 , C07D413/12 , C07D403/12 , C07D417/12
CPC分类号： C07D271/10 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/067 , C07D295/096
摘要： Novel phenylpiperazinylpropane and -butane derivatives of hetarylphenols and hetarylanilines of the formula ##STR1## where R.sup.1 is hydrogen or alkyl of 1 to 4 carbon atoms, R.sup.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy where alkyl is of 1 to 3 carbon atoms, the phenyl ring can be monosubstituted or disubstituted by R.sup.2, X is oxygen or an NH group, and the heterocyclic structure Het. is 1,3,4-oxadiazolyl, triazolyl, imidazolyl or pyrazolyl, and their physiologically tolerated addition salts with acids, processes for their preparation, and pharmaceutical formulations which contain these compounds and exhibit predominantly sedative, neuroleptic and hypotensive properties.
摘要翻译：式（I）的芳基苯酚和杂芳基苯胺的新型苯基哌嗪基丙烷和丁烷衍生物，其中R 1为氢或1至4个碳原子的烷基，R 2为氢，卤素，1至4个碳原子的烷基或烷氧基，其中烷基为1〜 3个碳原子，苯环可以被R2单取代或二取代，X是氧或NH基，杂环结构Het。是1,3,4-恶二唑基，三唑基，咪唑基或吡唑基，以及它们与酸的生理学上可耐受的加成盐，其制备方法和含有这些化合物并且主要表现出镇静，抗精神病药和降血压性质的药物制剂。

9. 发明授权

US4618622A Sulfonates of hydroxycoumarins 失效
标题翻译：羟基香豆素磺酸盐
公开(公告)号：US4618622A
公开(公告)日：1986-10-21
申请号：US552787
申请日：1983-11-17
申请人： Rainer Schlecker , Peter Schmidt , Peter C. Thieme , Dieter Lenke , Hans-Jurgen Teschendorf , Martin Traut , Claus D. Mueller , Hans P. Hofmann , Horst Kreiskott
发明人： Rainer Schlecker , Peter Schmidt , Peter C. Thieme , Dieter Lenke , Hans-Jurgen Teschendorf , Martin Traut , Claus D. Mueller , Hans P. Hofmann , Horst Kreiskott
IPC分类号： A61K31/35 , A61K31/352 , A61K31/365 , A61P25/18 , A61P25/24 , A61P25/26 , A61P37/08 , A61P43/00 , C07D311/08 , C07D311/16 , C07D311/80 , A61K31/37
CPC分类号： C07D311/80 , C07D311/16
摘要： Sulfonates of hydroxycoumarins of the formula I ##STR1## where R.sup.1 and R.sup.2 are identical or different and are each hydrogen, halogen or alkyl of 1 to 5 carbon atoms which can be substituted by --NR.sup.4 R.sup.5, --OR.sup.4 or --OC(O)R.sup.4, where R.sup.4 and R.sup.5 are identical or different and are each hydrogen or alkyl of 1 to 4 carbon atoms, or R.sup.1 and R.sup.2 are each a carboxylic acid group --OC(O)R.sup.4 or a carboxamido radical, with the proviso that R.sup.1 is not methyl when R.sup.2 is hydrogen, or R.sup.1 and R.sup.2 together form a --(CH.sub.2).sub.n -- chain where n is 3-5, and R.sup.3 is a straight-chain or branched alkyl radical of 1 to 8 carbon atoms or cycloalkyl of 3 to 8 carbon atoms, each of which can be substituted by halogen, --OR.sup.4, --NR.sup.4 R.sup.5, --CN or phenyl, or R.sup.3 is a straight-chain or branched alkenyl radical of 3 to 8 carbon atoms, an amino group -- NR.sup.4 R.sup.5, or phenyl or naphthyl, each of which is unsubstituted or monosubstituted or polysubstituted by --OR.sup.4, --NR.sup.4 R.sup.5, --NO.sub.2, halogen, --SR.sup.4, --S(O)R.sup.4, --OS(O)R.sup.4, --SCF.sub.3, --OS(O)CF.sub.3, --CN, --C(O)R.sup.4, --OC(O)R.sup.4, --NHC(O)R.sup.4, --CF.sub.3, C.sub.1 -C.sub.4 -alkyl or a combination of these substituents, a process for their preparation, drugs containing these compounds, and compounds of the formula I, in which R.sup.1 is methyl and R.sup.2 is hydrogen, for use as drugs.
摘要翻译：式I的羟基香豆素的磺酸盐其中R 1和R 2相同或不同，各自为氢，卤素或可被-NR 4 R 5，-OR 4或-OC（O）取代的1至5个碳原子的烷基）R 4，其中R 4和R 5相同或不同并且各自为氢或1至4个碳原子的烷基，或者R 1和R 2各自为羧酸基-OC（O）R 4或甲酰胺基，条件是R 1 当R 2为氢时，R 1和R 2一起形成 - （CH 2）n - 链，其中n为3-5，R 3为1至8个碳原子的直链或支链烷基或3个环烷基至8个碳原子，每个可以被卤素，-OR4，-NR4R5，-CN或苯基取代，或R3是3-8个碳原子的直链或支链烯基，氨基-NR4R5或苯基或萘基，它们各自被-OR4，-NR4R5，-NO2，卤素，-SR4，-S（O）R4，-OS（O）R4，-SCF3，-OS（O）未取代或单取代或多取代， CF 3，-CN，-C（O）R 4，-OC（O）R 4， -NHC（O）R 4，-CF 3，C 1 -C 4烷基或这些取代基的组合，其制备方法，含有这些化合物的药物和式I化合物，其中R 1是甲基，R 2是氢，用作药物。

10. 发明授权

US4263430A 2-Methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole 失效
标题翻译： 2-甲基-5-（2-羟基苯乙烯基）-1,3,4-噻二唑
公开(公告)号：US4263430A
公开(公告)日：1981-04-21
申请号：US30886
申请日：1979-04-17
申请人： Helmut Hagen , Peter C. Thieme , Albrecht Franke
发明人： Helmut Hagen , Peter C. Thieme , Albrecht Franke
IPC分类号： C07D285/12 , C07F9/6539
CPC分类号： C07D285/12 , C07F9/65395
摘要： 2-Methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole of the formula ##STR1## and processes for its preparation by condensing salicylaldehyde with 2,5-dimethyl-1,3,4-thiadiazole or 2-methyl-5-(triphenylphosphine-methylene)-1,3,4-thiadiazole. 2-Methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole is a valuable intermediate for the preparation of pharmacologically active compounds; for example the alkylamino-hydroxypropyl ethers can, because of their .beta.-sympatholytic action, be used as drugs for the treatment of coronary diseases of the heart, cardiac arrhythmias and hypertonia.
摘要翻译：式（1）的2-甲基-5-（2-羟基苯乙烯基）-1,3,4-噻二唑及其制备方法是将水杨醛与2,5-二甲基-1,3,4-噻二唑或2-甲基-5-（三苯基膦 - 亚甲基）-1,3,4-噻二唑。 2-甲基-5-（2-羟基苯乙烯基）-1,3,4-噻二唑是制备药理活性化合物的有价值的中间体; 例如，烷基氨基 - 羟丙基醚可以由于其β - 溶血性作用而被用作治疗心脏冠状动脉疾病，心律失常和高渗性的药物。

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