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1. 发明授权

US4600721A Pharmaceutical preparation 失效
标题翻译：药物制剂
公开(公告)号：US4600721A
公开(公告)日：1986-07-15
申请号：US716408
申请日：1985-03-27
申请人： Peter Morsdorf , Helmut Schickaneder , Heidrun Engler , Istvan Szelenyi , Kurt H. Ahrens , Kay Brune
发明人： Peter Morsdorf , Helmut Schickaneder , Heidrun Engler , Istvan Szelenyi , Kurt H. Ahrens , Kay Brune
IPC分类号： A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61P11/00 , A61P17/00 , A61P27/02 , A61P27/14 , A61P29/00 , A61P37/08 , A61P43/00 , C07D263/58 , C07D277/82
CPC分类号： C07D263/58 , A61K31/42 , A61K31/425 , C07D277/82
摘要： Pharmaceutical preparations having an antiphlogistic action are described. The preparations contain, as active ingredient, a benzazole derivative corresponding to the general tautomeric formulae I ##STR1## wherein X represents a sulphur or oxygen atom and R.sup.1 represents a hydrogen atom and R.sup.2 a hydroxymethyl, formyl, lower carbalkoxy or lower acyl group or R.sup.1 and R.sup.2 together represent the group ##STR2## wherein R.sup.3 and R.sup.4 denote, independently of one another, a hydrogen atom or a C.sub.1 -C.sub.6 -alkyl group, or they contain a physiologically acceptable salt thereof. These pharmaceutical preparations are suitable in particular for the treatment of inflammatory conditions and for inhibiting the lipoxygenase and/or cyclooxygenase route of arachidonic acid metabolism.
摘要翻译：描述具有消炎作用的药物制剂。该制剂含有作为活性成分的对应于一般互变异构体I（I）的苯并唑衍生物，其中X表示硫或氧原子，R1表示氢原子，R2表示羟甲基，甲酰基，低级烷氧羰基或低级酰基基团或R 1和R 2一起表示基团，其中R 3和R 4彼此独立地表示氢原子或C 1 -C 6烷基，或它们含有其生理上可接受的盐。这些药物制剂特别适用于治疗炎性病症和抑制花生四烯酸代谢的脂氧合酶和/或环氧合酶途径。

2. 发明授权

US4732986A Benzothiazole derivatives, processes for their preparation and pharmaceutical compositions containing these compounds 失效
标题翻译：苯并噻唑衍生物，其制备方法和含有这些化合物的药物组合物
公开(公告)号：US4732986A
公开(公告)日：1988-03-22
申请号：US51214
申请日：1987-05-12
申请人： Kay Brune , Heidrun Engler , Istvan Szelenyi , Peter Morsdorf , Helmut Schickaneder , Kurt H. Ahrens
发明人： Kay Brune , Heidrun Engler , Istvan Szelenyi , Peter Morsdorf , Helmut Schickaneder , Kurt H. Ahrens
IPC分类号： A61K31/425 , A61K31/428 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D277/82 , C12N9/99
CPC分类号： C07D277/82
摘要： Benzothiazole derivatives corresponding to the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent, independently of one another, a hydrogen atom, a halogen atom, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group, R.sup.5 represents a hydrogen atom or a linear C.sub.1 -C.sub.3 -alkyl group, R.sup.6 represents a hydrogen atom, and R.sup.7 represents a formyl group, a carbalkoxy group of the formula ##STR2## wherein R.sup.8 denotes a linear or branch chained C.sub.1 -C.sub.4 -alkyl group, or it represents an acyl group of the formula ##STR3## wherein R.sup.9 denotes a linear C.sub.1 -C.sub.3 -alkyl group, or R.sup.6 and R.sup.7 together represent the group ##STR4## wherein R.sup.10 and R.sup.11 represent, independently of one another, a hydrogen atom or a linear C.sub.1 -C.sub.6 -alkyl group or R.sup.6 and R.sup.7 represent the group ##STR5## wherein R.sup.12 and R.sup.13 represent, independently of one another, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group or R.sup.6 and R.sup.7 represent the group ##STR6## wherein R.sup.14 denotes a linear C.sub.1 -C.sub.3 -alkyl group, as well as the physiologically acceptable salts thereof, a process for the preparation of these compounds, and a pharmaceutical preparation containing them, are described.
摘要翻译：对应于通式I（I）的苯并噻唑衍生物，其中R 1，R 2，R 3和R 4彼此独立地表示氢原子，卤素原子，直链C 1 -C 3 - 烷基或直链C 1 -C 3 - C 3 - 烷氧基，R 5表示氢原子或直链C 1 -C 3 - 烷基，R 6表示氢原子，R 7表示甲酰基，式◎的烷氧基，其中，R 8表示直链或支链或者它表示下式的酰基，其中R 9表示直链C 1 -C 3 - 烷基，或者R 6和R 7一起表示基团，其中R 10和R 11独立地表示另一方面，氢原子或直链C 1 -C 6 - 烷基或R 6和R 7表示基团，其中R 12和R 13彼此独立地表示直链C 1 -C 3 - 烷基或直链C 1 -C 3 - 烷氧基或R6和R7表示基团，其中R14表示直链C1-C3-烷基，以及生理记录描述了其可接受的盐，制备这些化合物的方法和含有它们的药物制剂。

3. 发明授权

US4659721A Alkanol derivatives, and pharmaceutical preparation containing these compounds 失效
标题翻译：烷醇衍生物和含有这些化合物的药物制剂
公开(公告)号：US4659721A
公开(公告)日：1987-04-21
申请号：US693204
申请日：1985-01-22
申请人： Helmut Schickaneder , Stefan Postius , Istvan Szelenyi , Peter Morsdorf , Rolf Herter , Kurt H. Ahrens
发明人： Helmut Schickaneder , Stefan Postius , Istvan Szelenyi , Peter Morsdorf , Rolf Herter , Kurt H. Ahrens
IPC分类号： A61K31/41 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/445 , A61P1/04 , C07C67/00 , C07C213/00 , C07C215/28 , C07C217/48 , C07C239/00 , C07C279/28 , C07C313/00 , C07C323/29 , C07D209/48 , C07D249/14 , C07D275/02 , C07D275/03 , C07D277/20 , C07D277/26 , C07D277/48 , C07D285/10 , C07D295/08 , C07D295/096 , C07D303/36 , C07D307/52 , C07D333/00 , C07D333/20 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D209/48 , C07D249/14 , C07D275/03 , C07D285/10 , C07D295/096 , C07D303/36 , C07D333/20 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Alkanol derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--CH.sub.2 X--CH.sub.2 --Y--(CH.sub.2).sub.n --NHR.sup.3 (I)which have a highly selective action on histamine-H.sub.2 receptors are described. Due to this action, these compounds may advantageously be used for treatment of diseases caused by raised gastric secretion.
摘要翻译：描述对应于对组胺-H 2受体具有高度选择性作用的通式I R1R2N-（CH2）m-Q-CH2X-CH2-Y-（CH2）n-NHR3（I）的烷醇衍生物。由于这种作用，这些化合物可有利地用于治疗由升高的胃分泌引起的疾病。

4. 发明授权

US4559344A Pyridine-pyrimidinone derivatives, a process for their production and H.sub. -antagonist medicament containing these compounds 失效
标题翻译：吡啶 - 嘧啶酮衍生物，其制备方法和含有这些化合物的H 2拮抗剂药物
公开(公告)号：US4559344A
公开(公告)日：1985-12-17
申请号：US574077
申请日：1984-01-26
申请人： Helmut Schickaneder , Peter Morsdorf , Stefan Postius , Istvan Szelenyi , Rolf Herter , Herbert Hansen , Kurt H. Ahrens
发明人： Helmut Schickaneder , Peter Morsdorf , Stefan Postius , Istvan Szelenyi , Rolf Herter , Herbert Hansen , Kurt H. Ahrens
IPC分类号： C07D295/08 , C07D213/55 , C07D307/38 , C07D401/06 , C07D405/14 , C07D409/14 , C07D417/14 , A61K31/505 , C07D239/02
CPC分类号： C07D401/06
摘要： The invention relates to new pyridine-pyrimidinone derivatives corresponding to the following general formula ##STR1## wherein R.sup.1 represents linear C.sub.1-6 alkyl or cycloalkyl and R.sup.2 represents linear C.sub.1-6 alkyl or R.sup.1 and R.sup.2 together with the nitrogen atom form a pyrrolidine or piperidine ring;Alk represents a linear alkylene chain C.sub.1-6 ;Q represents a benzene ring, furan ring, thiophene ring or thiazole ring;X represents oxygen, Y is a single bond and m is 2, 3 or 4 when Q represents benzene;X represents methylene, Y represents sulfur and m is 2 or 3 when Q is furan, thiophene or thiazole; andR.sup.3 represents a hydrogen atom or a lower alkyl group.These compounds show improved H.sub.2 -antagonistic activity.
摘要翻译：本发明涉及对应于以下通式的新的吡啶 - 嘧啶酮衍生物，其中R 1表示直链C 1-6烷基或环烷基，R 2表示直链C 1-6烷基或R 1和R 2与氮原子一起形成吡咯烷或哌啶环; Alk表示直链亚烷基链C 1-6; Q表示苯环，呋喃环，噻吩环或噻唑环; X表示氧，Y为单键，当Q表示苯时m为2,3或4; X表示亚甲基，Y表示硫，当Q为呋喃，噻吩或噻唑时，m为2或3; 并且R 3表示氢原子或低级烷基。这些化合物显示出改善的H2拮抗活性。

5. 发明授权

US4656180A Diamine derivatives and pharmaceutical preparations containing these compounds 失效
标题翻译：含有这些化合物的二胺衍生物和药物制剂
公开(公告)号：US4656180A
公开(公告)日：1987-04-07
申请号：US708239
申请日：1985-03-05
申请人： Stefan Postius , Rolf Herter , Peter Morsdorf , Helmut Schickaneder , Istvan Szelenyi , Kurt H. Ahrens
发明人： Stefan Postius , Rolf Herter , Peter Morsdorf , Helmut Schickaneder , Istvan Szelenyi , Kurt H. Ahrens
IPC分类号： C07D295/08 , A61K31/135 , A61K31/34 , A61K31/341 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/445 , A61P43/00 , C07C67/00 , C07C213/00 , C07C217/48 , C07C217/58 , C07C217/76 , C07C217/84 , C07C313/00 , C07C323/29 , C07C323/32 , C07D209/48 , C07D277/28 , C07D285/10 , C07D295/096 , C07D295/135 , C07D295/155 , C07D303/36 , C07D307/52 , C07D333/20 , C07D409/12 , C07D401/14
CPC分类号： C07D209/48 , C07D285/10 , C07D295/096 , C07D295/135 , C07D295/155 , C07D303/36 , C07D307/52 , C07D333/20 , C07D409/12
摘要： Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.
摘要翻译：对应于通式I R1R2N-（CH2）mQA-NH-R-NH-B-Q' - （CH2）nNR3R4（I）的二胺衍生物，其对组胺-H 2受体具有高选择性作用，因此适用于作为抗溃疡剂。还描述了制备这些化合物的方法和含有这些化合物的药物制剂。

6. 发明授权

US4666921A Pyrazole derivatives, processes for their preparation and pharmaceutical preparations containing these compounds 失效
标题翻译：吡唑衍生物，其制备方法和含有这些化合物的药物制剂
公开(公告)号：US4666921A
公开(公告)日：1987-05-19
申请号：US787114
申请日：1985-10-15
申请人： Rolf Herter , Helmut Schickaneder , Peter Morsdorf , Stefan Postius , Istvan Szelenyi , Kurt H. Ahrens
发明人： Rolf Herter , Helmut Schickaneder , Peter Morsdorf , Stefan Postius , Istvan Szelenyi , Kurt H. Ahrens
IPC分类号： C07D231/52 , A61K31/445 , A61K31/415 , C07D401/12 , C07D403/12
CPC分类号： C07D231/52
摘要： Special pyrazole derivatives corresponding to the general formula I which have a highly selective action on histamine-H.sub.2 receptors are described. Compared with other drugs known to be effective in their action on histamine-H.sub.2 receptors, these compounds have improved pharmacological properties. A method of preparation of these compounds is also described.
摘要翻译：描述对应于对组胺-H 2受体具有高度选择性作用的通式I的特殊的吡唑衍生物。与已知对其组胺-H 2受体的作用有效的其它药物相比，这些化合物具有改善的药理学性质。还描述了这些化合物的制备方法。

7. 发明授权

US4599346A Propan-2-ol derivatives, a process for their production and medicaments containing these compounds 失效
标题翻译：丙-2-醇衍生物，其生产方法和含有这些化合物的药物
公开(公告)号：US4599346A
公开(公告)日：1986-07-08
申请号：US630963
申请日：1984-07-16
申请人： Helmut Schickaneder , Stefan Postius , Rolf Herter , Peter Morsdorf , Istvan Szelenyi , Kurt H. Ahrens
发明人： Helmut Schickaneder , Stefan Postius , Rolf Herter , Peter Morsdorf , Istvan Szelenyi , Kurt H. Ahrens
IPC分类号： C07D295/08 , A61K31/435 , A61K31/445 , A61P1/04 , A61P43/00 , C07D209/48 , C07D285/10 , C07D295/096 , C07D405/06 , A61K31/41 , C07D211/06 , C07D417/12
CPC分类号： C07D209/48 , C07D285/10 , C07D295/096 , C07D405/06
摘要： The invention relates to new propan-2-ol derivatives corresponding to the following general formula ##STR1## in which R represents ##STR2## and to salts thereof with pharmacologically acceptable acids. These compounds have a selective effect on histamine-H.sub.2 -receptors.
摘要翻译：本发明涉及对应于下列通式（I）的新的丙-2-醇衍生物，其中R代表“IMAGE”，以及其与药理学上可接受的酸的盐。这些化合物对组胺-H 2受体具有选择性作用。

8. 发明授权

US4866066A Thiomethylpyridine derivatives and their use for eliciting a bronchosecretolytic or mucolytic response 失效
标题翻译：硫代甲基吡啶衍生物及其用于引发支气管解吸或溶血反应的用途
公开(公告)号：US4866066A
公开(公告)日：1989-09-12
申请号：US015007
申请日：1987-02-17
申请人： Helmut Schickaneder , Heidrun Engler , Istvan Szelenyi
发明人： Helmut Schickaneder , Heidrun Engler , Istvan Szelenyi
IPC分类号： A61K31/325 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/505 , A61P11/10 , C07D213/32 , C07D213/61 , C07D213/70 , C07D401/12 , C07D413/12 , C07D487/04 , C07D498/04
CPC分类号： C07D213/70 , C07D213/32 , C07D401/12 , C07D487/04
摘要： Thiomethylpyridine derivatives having bronchosecretolytic and mucolytic activity according to the formula: ##STR1## wherein R is a group attached in the 2-, 3- or 4-position of the pyridine ring which corresponds to the following general formula:Q--S--CH.sub.2 -- (II)wherein Q is a substituted or unsubstituted aryl group or a 5- or 6-membered heterocyclic group which may optionally contain one or more substituents and/or which may be condensed with an optionally substituted phenyl group or with an optionally substituted heterocycle; R' is a lower alkyl group, a halogen atom or an aminoalkyl group; and n is 0 or an integer of from 1 to 4; and the therapeutically-acceptable acid addition salts thereof.The new compounds are distinguished by surprising activity compared with known compounds, such as "Ambroxol".
摘要翻译：具有下列通式的其中R是连接在吡啶环的2-，3-或4-位的基团的具有支气管解吸和溶血活性的硫代甲基吡啶衍生物，其对应于下列通式：QS-CH2 - （II）其中Q是取代或未取代的芳基或可以任选地含有一个或多个取代基和/或可以与任选取代的苯基或任选取代的杂环稠合的5-或6-元杂环基 ; R'是低级烷基，卤素原子或氨基烷基; n为0或1〜4的整数，及其治疗上可接受的酸加成盐。与已知化合物（例如“Ambroxol”）相比，新化合物的特征在于惊人的活性。

9. 发明授权

US4810715A Imidazoyl-substituted thiomethylpyridine derivatives, method of administration thereof and medicaments containing them 失效
标题翻译：咪唑酰基取代的硫代甲基吡啶衍生物，其施用方法和含有它们的药物
公开(公告)号：US4810715A
公开(公告)日：1989-03-07
申请号：US26189
申请日：1987-03-16
申请人： Helmut Schickaneder , Heidrun Engler , Istvan Szelenyi
发明人： Helmut Schickaneder , Heidrun Engler , Istvan Szelenyi
IPC分类号： A61K31/325 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/505 , A61P11/10 , C07D213/32 , C07D213/61 , C07D213/70 , C07D401/12 , C07D413/12 , C07D487/04 , C07D498/04
CPC分类号： C07D213/70 , C07D213/32 , C07D401/12 , C07D487/04
摘要： Thiomethylpyridine derivatives having bronchosecretolytic and mucolytic activity according to the formula: ##STR1## wherein R is a group attached in the 2-, 3- or 4-position of the pyridine ring which corresponds to the following general formula:Q--S--CH.sub.2 -- (II) wherein Q is a substituted or unsubstituted aryl group or a 5- or 6-membered heterocyclic group which may optionally contain one or more substituents and/or which may be condensed with an optionally substituted phenyl group or with an optionally substituted heterocycle;R' is a lower alkyl group, a halogen atom or an aminoalkyl group; andn is 0 or an integer of from 1 to 4;and the therapeutically-acceptable acid addition salts thereof.The new compounds are distinguished by surprising activity compared with known compounds, such as "Ambroxol".
摘要翻译：具有下列通式的其中R是连接在吡啶环的2-，3-或4-位的基团的具有支气管解吸和溶血活性的硫代甲基吡啶衍生物，其对应于下列通式：QS-CH2 - （II）其中Q是取代或未取代的芳基或可以任选地含有一个或多个取代基和/或可以与任选取代的苯基或任选取代的杂环稠合的5-或6-元杂环基 ; R'是低级烷基，卤素原子或氨基烷基; n为0或1〜4的整数，及其治疗上可接受的酸加成盐。与已知化合物如“Ambroxol”相比，新化合物的特征在于惊人的活性。

10. 发明授权

US5021431A Imidazolyl alkyl guanidine derivatives, processes for their preparation and pharmaceutical preparations containing these compounds 失效
标题翻译：咪唑基烷基胍衍生物，其制备方法和含有这些化合物的药物制剂
公开(公告)号：US5021431A
公开(公告)日：1991-06-04
申请号：US318467
申请日：1989-02-28
申请人： Armin Buschauer , Helmut Schickaneder , Walter Schunack , Sigurd Elz , Istvan Szelenyi , Gert Baumann , Kurt H. Ahrens
发明人： Armin Buschauer , Helmut Schickaneder , Walter Schunack , Sigurd Elz , Istvan Szelenyi , Gert Baumann , Kurt H. Ahrens
IPC分类号： C07D233/54 , C07D233/64 , C07D401/12 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14
CPC分类号： C07D233/64 , C07D401/12 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14
摘要： New imidazolylalkyl-guanidine derivatives are described, which by virtue of their agonistic action on histamine-H.sub.2 receptors and in part also due to their additional H.sub.1 -antagonistic receptor activity can be used in the treatment of cardiac diseases, certain forms of hypertension and diseases of arterial occlusion.These imidazolylalkyl-guanidine derivatives correspond to the general formula I: ##STR1##
摘要翻译：描述了新的咪唑基烷基胍衍生物，其由于其对组胺-H 2受体的激动作用，并且部分还由于其另外的H1拮抗受体活性而可用于治疗心脏疾病，某些形式的高血压和疾病动脉闭塞。这些咪唑烷基 - 胍衍生物对应于通式I：

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