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1. 发明授权

US4119710A Bronchospasmolytic 1-(p-amino-phenyl)-2-amino-ethanols-(1) and salts 失效
标题翻译：支气管解痉剂1-（对氨基 - 苯基）-2-氨基 - 乙醇 - （1）和盐
公开(公告)号：US4119710A
公开(公告)日：1978-10-10
申请号：US754981
申请日：1976-12-28
申请人： Gunther Engelhardt , Johannes Keck , Gerd Kruger , Klaus-Reinhold Noll , Helmut Pieper
发明人： Gunther Engelhardt , Johannes Keck , Gerd Kruger , Klaus-Reinhold Noll , Helmut Pieper
IPC分类号： C07D263/04 , C07D317/58 , A61K31/04 , A61K31/135 , A61K31/275 , A61K31/36
CPC分类号： C07D263/04 , C07D317/58
摘要： Racemic and optically active compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, iodine or cyano,R.sub.2 is fluorine, trifluoromethyl, nitro or cyano, andR.sub.3 is alkyl of 3 to 5 carbon atoms, hydroxy(alkyl of 3 to 5 carbon atoms), cycloalkyl of 3 to 5 carbon atoms, 1-(3,4-methylenedioxy-phenyl)-2-propyl or 1-(p-hydroxy-phenyl)-2-propyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as analgesics, uterospasmolytics, bronchospasmolytics and antispastics for the skeletal musculature, and especially as .beta..sub.2 -receptor mimetics and .beta..sub.1 -receptor blockers.
摘要翻译：其中R 1为氢，氟，氯，溴，碘或氰基的外消旋和旋光活性化合物，R 2为氟，三氟甲基，硝基或氰基，R 3为3至5个碳原子的烷基，羟基（烷基 3至5个碳原子的环烷基，3至5个碳原子的环烷基，1-（3,4-亚甲二氧基 - 苯基）-2-丙基或1-（对羟基 - 苯基）-2-丙基，和非毒性其药理学可接受的酸添加剂; 这些化合物作为其作为骨质疏松症，骨质疏松症，骨质疏松症和骨质疏松症的抗生素有用的化合物，特别适用于β2受体的MIME和β受体阻断剂。

2. 发明授权

US4244967A Antiphlogistic pharmaceutical compositions containing a phenylethanolamine and methods of use 失效
标题翻译：含有苯乙醇胺的消炎药物组合物及其使用方法
公开(公告)号：US4244967A
公开(公告)日：1981-01-13
申请号：US72553
申请日：1979-09-04
申请人： Gunther Engelhardt , Johannes Keck , Gerd Kruger , Klaus Noll , Helmut Pieper , Rainer Zimmermann
发明人： Gunther Engelhardt , Johannes Keck , Gerd Kruger , Klaus Noll , Helmut Pieper , Rainer Zimmermann
IPC分类号： A61K31/135 , A61K31/17 , A61K31/275 , A61K31/325 , A61P29/00 , A61P43/00 , A61K31/27
CPC分类号： A61K31/135 , A61K31/17 , A61K31/275 , A61K31/325
摘要： The method of using compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, iodine or cyano,R.sub.2 is fluorine, cyano, trifluoromethyl, nitro or alkyl of 1 to 4 carbon atoms,R.sub.3 is cycloalkyl or alkyl, each of 3 to 5 carbon atoms, andR.sub.4 is hydrogen or --CO--R.sub.5, whereR.sub.5 is alkoxy of 1 to 5 carbon atoms, alkenyloxy of 2 to 5 carbon atoms, aryloxy of 6 to 10 carbon atoms, aralkoxy of 7 to 11 carbon atoms, or amino which may be mono- or di-substituted by alkyl of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms, aryl of 6 to 10 carbon atoms and/or aralkyl of 7 to 11 carbon atoms,and non-toxic, pharmacologically acceptable acid addition salts thereof as antirheumatics and antiphlogistics.
摘要翻译：使用下式化合物的方法其中R1是氢，氟，氯，溴，碘或氰基，R2是氟，氰基，三氟甲基，硝基或1-4个碳原子的烷基，R3是环烷基或烷基， 3〜5个碳原子，R4为氢或-CO-R5，R5为1〜5个碳原子的烷氧基，2〜5个碳原子的烯氧基，6〜10个碳原子的芳氧基，7〜11个芳氧基碳原子或可以被1至5个碳原子的烷基，2至5个碳原子的烯基，6至10个碳原子的芳基和/或7至11个碳原子的芳烷基单取代或二取代的氨基，以及无毒，药理学上可接受的酸加成盐作为抗风湿剂和消炎药。

3. 发明授权

US4362738A Esters and amides containing the 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetyl moiety 失效
标题翻译：含有1-（4-氯苯甲酰基）-5-甲氧基-2-甲基-1H-吲哚-3-乙酰基部分的酯和酰胺
公开(公告)号：US4362738A
公开(公告)日：1982-12-07
申请号：US158587
申请日：1980-06-11
申请人： Johannes Keck , Gerd Kruger , Helmut Pieper , Klaus Noll , Gunther Engelhardt , Norbert Promberger , Rainer Zimmermann
发明人： Johannes Keck , Gerd Kruger , Helmut Pieper , Klaus Noll , Gunther Engelhardt , Norbert Promberger , Rainer Zimmermann
IPC分类号： C07D209/08 , A61K31/495 , A61P29/00 , C07C67/00 , C07C227/00 , C07C227/16 , C07C227/18 , C07C229/54 , C07C237/32 , C07C237/38 , C07C313/00 , C07C323/12 , C07C323/65 , C07D209/28 , C07D213/74 , C07D295/088 , C07D295/155 , C07D401/12 , C07H13/08 , C07D279/18 , A61K27/00
CPC分类号： C07D213/74 , C07D209/28 , C07D295/088 , C07D295/155
摘要： Compounds of the formula ##STR1## wherein each X, which may be identical or different from the other X, is oxygen or imino;R.sub.1 is hydrogen, fluorine, chlorine or bromine;R.sub.2 and R.sub.3, which may be identical or different from each other, are each hydrogen; unsubstituted or mono-substituted alkyl of 1 to 6 carbon atoms, where the substituent is phenyl or dialkylamino with 1 to 3 carbon atoms in each alkyl moiety; pyridyl; or cycloalkyl of 5 to 7 carbon atoms;R.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, are pyrrolidino, piperidino, hexamethyleneimino, morpholino, N-aryl-piperazino or N-(alkyl of 1 to 3 carbon atoms)-piperazino;A is cycloalkylene of 5 to 7 carbon atoms; unsubstituted or substituted alkylene of 2 to 10 carbon atoms, where the substituents are one to two alkyls of 1 to 3 carbon atoms each, one to two carbalkoxys of 2 to 4 carbon atoms each, one to two phenyls, one to four hydroxyls, one halomethyl, one hydroxymethyl, one alkanoyloxy of 1 to 18 carbon atoms, one alkanoyloxymethyl of 1 to 18 carbon atoms in the alkanoyl moiety or one ##STR2## where R.sub.1, R.sub.2 and R.sub.3 have the meanings previously defined; or alkylene of 2 to 10 carbon atoms interrupted by oxygen, sulfur, sulfoxide, sulfonyl, phenyl, cyclohexyl, pyridyl, piperazino or unsubstituted or substituted imino, where the substituent on the imino group is alkyl of 1 to 6 carbon atoms, phenyl or phenylalkyl of 1 to 3 carbon atoms in the alkyl moiety;B is the acyl residue of an antiphlogistic carboxylic acid;and their non-toxic, pharmacologically acceptable acid addition salts. The compounds as well as their salts are useful as anti-inflammatories.
摘要翻译：其中每个X可以相同或不同于另一个X的式“IMAGE”的化合物是氧或亚氨基; R1是氢，氟，氯或溴; R2和R3可以相同或不同，分别为氢; 未取代或单取代的1至6个碳原子的烷基，其中取代基为苯基或每个烷基部分具有1至3个碳原子的二烷基氨基; 吡啶基或5至7个碳原子的环烷基; 吡咯烷基，哌啶子基，六亚甲基亚氨基，吗啉代，N-芳基 - 哌嗪子基或N-（1至3个碳原子的烷基） - 哌嗪基; R 2和R 3彼此连接并连接的氮原子。 A是5至7个碳原子的亚环烷基; 2至10个碳原子的未取代或取代的亚烷基，其中取代基为1至2个碳原子数为1至2个的烷基，每个为2至4个碳原子的1至2个碳烷氧基，1至2个苯基，1至4个羟基，1至2个卤代甲基，一个羟甲基，一个1至18个碳原子的烷酰氧基，一个在烷酰基部分中具有1至18个碳原子的烷酰氧基甲基或一个，其中R1，R2和R3具有以前定义的含义; 或由氧，硫，亚砜，磺酰基，苯基，环己基，吡啶基，哌嗪子基或未取代或取代的亚氨基所取代的2至10个碳原子的亚烷基，其中亚氨基上的取代基是1至6个碳原子的烷基，苯基或苯基烷基在烷基部分中具有1至3个碳原子; B是消炎性羧酸的酰基残基; 及其无毒，药理学上可接受的酸加成盐。化合物及其盐可用作抗炎剂。

4. 发明授权

US4214001A 1-(4-Acylamino-phenyl)-2-amino-ethanols and salts thereof 失效
标题翻译： 1-（4-酰基氨基 - 苯基）-2-氨基 - 乙醇及其盐
公开(公告)号：US4214001A
公开(公告)日：1980-07-22
申请号：US883814
申请日：1978-03-06
申请人： Gunther Engelhardt , Johannes Keck , Kruger , Klaus Noll , Helmut Pieper
发明人： Gunther Engelhardt , Johannes Keck , Kruger , Klaus Noll , Helmut Pieper
IPC分类号： A61K31/17 , A61K31/167 , A61K31/27 , A61P25/04 , A61P25/08 , C07C67/00 , C07C215/52 , C07C239/00 , C07C269/00 , C07C271/28 , C07C271/58 , C07C275/28 , C07C275/40 , A61K31/275 , C07C121/80 , C07C125/06
CPC分类号： C07C275/40
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or cyano;R.sub.2 is fluorine, cyano, trifluoromethyl, nitro or alkyl of 1 to 4 carbon atoms;R.sub.3 is alkoxy of 1 to 5 carbon atoms, alkenyloxy of 2 to 5 carbon atoms, aryloxy of 6 to 10 carbon atoms, aralkoxy of 7 to 11 carbon atoms, or --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are each hydrogen, alkyl of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms, aryl of 6 to 10 carbon atoms or aralkyl of 7 to 11 carbon atoms; andR.sub.4 is cycloalkyl of 3 to 5 carbon atoms or alkyl of 3 to 5 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salt thereof. The compounds as well as the salts are useful as analgesics, uterospasmolytics and antiasthmatics.
摘要翻译：其中R1是氢，卤素或氰基的式“IMAGE”的化合物; R2是氟，氰基，三氟甲基，硝基或1-4个碳原子的烷基; R3为1〜5个碳原子的烷氧基，2〜5个碳原子的烯氧基，6〜10个碳原子的芳氧基，7〜11个碳原子的芳烷氧基或-NR5R6，其中R5和R6分别为氢， 2至5个碳原子的烯基，6至10个碳原子的芳基或7至11个碳原子的芳烷基; R4为3〜5个碳原子的环烷基或3〜5个碳原子的烷基; 和无毒的，药学上可接受的酸加成盐。化合物以及盐可用作镇痛药，子宫内膜溶解药和止喘药。

5. 发明授权

US5393774A Phenylethanolamines, pharmaceutical compositions containing these compounds and process for preparing them 失效
标题翻译：苯乙醇胺，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US5393774A
公开(公告)日：1995-02-28
申请号：US187671
申请日：1994-01-27
申请人： Helmut Pieper , Gunther Engelhardt
发明人： Helmut Pieper , Gunther Engelhardt
IPC分类号： A23K1/16 , A61K31/275 , A61K31/277 , A61K31/36 , A61P3/06 , A61P11/00 , A61P11/08 , A61P13/02 , A61P15/00 , A61P21/02 , A61P25/02 , A61P25/04 , A61P29/00 , A61P43/00 , C07C255/59 , C07C271/28 , C07C255/50 , C07D317/54 , C07C28/58
CPC分类号： C07C255/59 , A23K20/111 , A61K31/275 , A61K31/36 , C07C271/28
摘要： The invention relates to phenylethanolamines of general formula ##STR1## wherein R.sub.1 and R.sub.2 are defined as in claim 1, the enantiomers and the acid addition salts thereof, which have valuable pharmacological properties, not only analgesic, antiphlogistic, broncholytic, uterus-spasmolytic, lipolytic effects and an antispastic effect on the cross-striped muscle, but also .beta..sub.2 -mimetic and/or .beta..sub.1 -blocking effects, the use thereof as pharmaceuticals and as performance enhancers and processes for preparing them.
摘要翻译：本发明涉及通式为“IMAGE”的苯乙醇胺，其中R 1和R 2如权利要求1所定义，其对映体及其酸加成盐具有有价值的药理学性质，不仅止痛，消炎，支气管分解，子宫解痉，脂肪分解效应和抗交叉效应，而且还具有β2-模拟和/或β1-阻断作用，其作为药物的用途以及用于制备它们的性能增强剂和方法。

6. 发明授权

US5061098A Printer station with output discharging device for individual sheets 失效
标题翻译：带单张纸的出纸装置的打印机
公开(公告)号：US5061098A
公开(公告)日：1991-10-29
申请号：US384736
申请日：1989-07-21
申请人： Gunther Engelhardt , Gerhard Lohrmann , Helmut Riesenegger
发明人： Gunther Engelhardt , Gerhard Lohrmann , Helmut Riesenegger
IPC分类号： B41J13/10
CPC分类号： B41J13/106
摘要： A printer station (1) with output discharging device (3) for individual sheets (6) is in particular used for laser page printers. An outwardly directed output discharging device (3) follows to output roller pairs (5), as seen in transport direction (7) of the printed individual sheets (6). In order to dispose the output discharging device (3) in a space-saving fashion, and in order to create the possibility for the operator to adjust the output discharging device (3) to the local special situation, the output discharging device (3) is tiltably supported at the printer frame (4) of the printer station (1), where the output discharging device (3) is furnished with drivable friction roller pairs (13), disposed behind the output roller pairs (5), as seen in transport direction (7). The shafts (14, 15) of the friction roller pairs (13) are in each case rotatably supported at the side walls (8,9) of the tiltable output discharging device (3).
摘要翻译：具有用于单张纸（6）的输出排出装置（3）的打印机站（1）特别用于激光打印机。如印刷的单张纸（6）的输送方向（7）所见，输出辊对（5）的向外指示的输出排出装置（3）。为了以节省空间的方式配置输出排出装置（3），为了使操作者将输出排出装置（3）调整到本地特殊情况的可能性，输出排出装置（3）被可倾斜地支撑在打印机站（1）的打印机框架（4）处，其中输出排放装置（3）配备有设置在输出辊对（5）后面的可驱动的摩擦辊对（13），如运输方向（7）。摩擦辊对（13）的轴（14,15）各自可旋转地支撑在可倾斜输出排放装置（3）的侧壁（8,9）处。

7. 发明授权

US4137313A 2,5-Dihydro-1,2-thiazino(5,6-b)indole-3-carboxamide-1,1-dioxides and salts thereof 失效
标题翻译： 2,5-二氢-1,2-噻嗪（5,6-b）吲哚-3-甲酰胺-1,1-二氧化物及其盐
公开(公告)号：US4137313A
公开(公告)日：1979-01-30
申请号：US872889
申请日：1978-01-27
申请人： Gunter Trummlitz , Wolfhard Engel , Ernst Seeger , Walter Haarmann , Gunther Engelhardt
发明人： Gunter Trummlitz , Wolfhard Engel , Ernst Seeger , Walter Haarmann , Gunther Engelhardt
IPC分类号： A61K31/54 , A61P7/02 , A61P29/00 , C07D209/42 , C07D513/04 , C07D513/14 , A61K31/38
CPC分类号： C07D513/04 , C07D209/42 , C07D513/14 , Y10S514/822
摘要： Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen, methyl or ethyl;R.sub.2 is methyl or ethyl;Y is hydrogen, fluorine, chlorine, bromine, methoxy, methyl, ethyl or trifluoromethyl; andAr is 2-thiazolyl which may have one or two methyl or ethyl substituents attached thereto; 5,6-dihydro-4H-cyclopentathiazol-2-yl; 4,5,6,7-tetrahydro-2-benzothiazolyl; 2-benzothiazolyl; 3-isothiazolyl which may have a methyl substituent attached thereto; 2-pyridyl which may have a methyl or hydroxyl substituent attached thereto; 3-pyridyl; 4-pyridyl; 4-pyrimidinyl; pyrazinyl; 2-benzimidazolyl; 2-oxazolyl which may have a methyl substituent attached thereto; 2-benzoxazolyl; or phenyl which may have a fluoro, chloro, bromo, methyl, ethyl, trifluoromethyl or methoxy substituent attached thereto; and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antiphlogistics and blood platelet aggregation inhibitors.
摘要翻译：式中的化合物，其中R1是氢，甲基或乙基; R2是甲基或乙基; Y是氢，氟，氯，溴，甲氧基，甲基，乙基或三氟甲基; 并且Ar是可以具有一个或两个连接到其上的甲基或乙基取代基的2-噻唑基; 5,6-二氢-4H-环戊基噻唑-2-基; 4,5,6,7-四氢-2-苯并噻唑基; 2-苯并噻唑基可具有与其连接的甲基取代基的3-异噻唑基; 可以具有连接到其上的甲基或羟基取代基的2-吡啶基; 3-吡啶基; 4-吡啶基; 4-嘧啶基; 吡嗪基 2-苯并咪唑基; 可具有与其连接的甲基取代基的2-恶唑基; 2-苯并恶唑基; 或可具有与其连接的氟，氯，溴，甲基，乙基，三氟甲基或甲氧基取代基的苯基; 和与无机或有机碱形成的无毒的，药学上可接受的盐。化合物及其盐可用作消炎剂和血小板聚集抑制剂。

8. 发明授权

US5648386A Separation of enantiomers of cimaterol, (-)-cimaterol and the use thereof in pharmaceutical compositions and animal feeds 失效
标题翻译：西马特罗，（ - ） - 西马特罗的对映异构体的分离及其在药物组合物和动物饲料中的用途
公开(公告)号：US5648386A
公开(公告)日：1997-07-15
申请号：US346105
申请日：1994-11-29
申请人： Wolfgang Resemann , Adolf Durr , Gunther Engelhardt , John Frances Quirke
发明人： Wolfgang Resemann , Adolf Durr , Gunther Engelhardt , John Frances Quirke
IPC分类号： C07C255/59 , A23K1/16 , A23K1/18 , A61K31/00 , A61K31/275 , A61K31/277 , A61P3/00 , A61P3/04 , A61P11/00 , A61P11/06 , A61P13/02 , A61P15/00 , A61P21/02 , A61P25/04 , A61P29/00 , A61P37/08 , C07B57/00 , C07C253/34 , C07C255/49 , C07C255/00
CPC分类号： A61K31/275 , A23K20/111 , A23K50/30 , A61K31/277 , C07C255/59 , Y10S514/826 , Y10S514/888 , Y10S514/909
摘要： The invention relates to the separation of enantiomers of cimaterol, (-)-cimaterol, the addition salts thereof and processes for preparing them and their use in pharmaceutical compositions and animal feeds.
摘要翻译：本发明涉及分离西马特罗，（ - ） - 西马特罗的对映异构体，其加成盐及其制备方法及其在药物组合物和动物饲料中的应用。

9. 发明授权

US5292753A Separation of enantiomers of cimaterol, (-)-cimaterol and the use thereof in pharmaceutical compositions and animal feeds 失效
标题翻译：西马特罗，（ - ） - 西马特罗的对映异构体的分离及其在药物组合物和动物饲料中的用途
公开(公告)号：US5292753A
公开(公告)日：1994-03-08
申请号：US81996
申请日：1993-06-23
申请人： Wolfgang Resemann , Adolf Durr , Gunther Engelhardt , John F. Quirke
发明人： Wolfgang Resemann , Adolf Durr , Gunther Engelhardt , John F. Quirke
IPC分类号： C07C255/59 , A23K1/16 , A23K1/18 , A61K31/00 , A61K31/275 , A61K31/277 , A61P3/00 , A61P3/04 , A61P11/00 , A61P11/06 , A61P13/02 , A61P15/00 , A61P21/02 , A61P25/04 , A61P29/00 , A61P37/08 , C07B57/00 , C07C253/34 , C07C255/49 , A01N37/34
CPC分类号： A61K31/275 , A23K20/111 , A23K50/30 , A61K31/277 , C07C255/59 , Y10S514/826 , Y10S514/888 , Y10S514/909
摘要： The invention relates to the separation of enantiomers of cimaterol, (-)-cimaterol, the addition salts thereof and processes for preparing them and their use in pharmaceutical compositions and animal feeds.
摘要翻译：本发明涉及分离西马特罗，（ - ） - 西马特罗的对映异构体，其加成盐及其制备方法及其在药物组合物和动物饲料中的应用。

10. 发明授权

US4292319A Antiphlogistic pharmaceutical compositions and method of use 失效
标题翻译：消炎药组合物及其使用方法
公开(公告)号：US4292319A
公开(公告)日：1981-09-29
申请号：US168608
申请日：1980-07-14
申请人： Oswald Tauber , Gunther Engelhardt , Matyas Leitold , Gunther Schmidt
发明人： Oswald Tauber , Gunther Engelhardt , Matyas Leitold , Gunther Schmidt
IPC分类号： A61K31/045 , A61K31/19 , A61K31/195 , A61K31/22 , A61K31/405 , A61K31/415 , A61K31/55 , A61K45/00 , A61P29/00 , C07D471/04 , A61K31/40 , A61K31/445 , A61K31/495
CPC分类号： A61K31/55 , A61K31/60 , Y10S514/825 , Y10S514/974
摘要： Pharmaceutical compositions containing a non-steroidal anti-inflammatory compound and 5,11-dihydro-11-[(4-methyl-1-piperazinyl)-acetyl]-6H-pyrido[2,3-b]-[1,4]benzodiazepin-6-one or a non-toxic acid addition salt thereof, and a method of using the same as antiphlogistics; the pyridobenzodiazepinone ingredient effectively suppresses the gastro-intestinal side-effects of the anti-inflammatory ingredient.
摘要翻译：含有非甾体抗炎化合物和5,11-二氢-11 - [（4-甲基-1-哌嗪基） - 乙酰基] -6H-吡啶并[2,3-b] - [1,4] 苯并二氮杂-6-酮或其无毒酸加成盐，以及其用作消炎剂的方法; 吡啶并苯并二氮杂酮成分有效地抑制了抗炎成分的胃肠副作用。

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