公开(公告)号：US5039675A

公开(公告)日：1991-08-13

申请号：US497223

申请日：1990-03-22

申请人： Peter Morsdorf ,  Helmut Schickaneder ,  Rolf Herter ,  Volker Pfanhlert ,  Geidrun Engler ,  Kurt H. Ahrens

发明人： Peter Morsdorf ,  Helmut Schickaneder ,  Rolf Herter ,  Volker Pfanhlert ,  Geidrun Engler ,  Kurt H. Ahrens

IPC分类号： A61K31/505 ,  A61P9/06 ,  C07D403/04 ,  C07D403/14

CPC分类号： C07D403/04

摘要： New benzimidazoles correponding to the general formula I ##STR1## are described, in which the pyridazinone ring is attached in the 5- or 6- position of the benzimidazole ring and R.sup.1 denotes a hydrogen atom or a straight chained or branched C.sub.1 to C.sub.4 alkyl group, R.sup.2 denotes a hydrogen atom, a straight chained or branched C.sub.1 to C.sub.4 alkyl group, a C.sub.1 to C.sub.4 alkoxy group, a hydroxy group, a halogen atom, an amino group or a nitro group, A denotes a hydrogen atom, a group of the formula ##STR2## wherein R.sup.3 denotes a hydrogen atom, an optionally substituted C.sub.1 to C.sub.4 alkyl group or a C.sub.1 to C.sub.4 alkoxy group and B denotes a cyano group, a benzoyl group or a phenylsulphonyl group, or A denotes a group of the formula ##STR3## in which m has the value 2 or 3 and n represents an integer from 1 to 6, and the physiologically acceptable salts thereof as well as processes for their preparation and pharmaceutical preparations. containing these compounds These compounds are new, effective, positive inotropic substances which do not act by the mechanism of phosphodiesterase inhibition.

公开(公告)号：US4921856A

公开(公告)日：1990-05-01

申请号：US176689

申请日：1988-04-01

申请人： Helmut Schickaneder ,  Peter Morsdorf ,  Volker Pfahlert ,  Heidrun Engler ,  Kurt H. Ahrens

发明人： Helmut Schickaneder ,  Peter Morsdorf ,  Volker Pfahlert ,  Heidrun Engler ,  Kurt H. Ahrens

IPC分类号： A61K31/50 ,  A61P9/04 ,  C07D237/04 ,  C07D403/10 ,  C07D403/12

CPC分类号： C07D403/10 ,  C07D237/04 ,  C07D403/12

摘要： New dihydropryidazinone derivatives corresponding to the following formula ##STR1## and a process for their preparation and pharmaceutical preparations containing these compounds are described. These compounds are effective positively inotropic substances with an improved therapeutic profile.

摘要翻译： 描述了对应于下式（I）的新的二氢哒嗪酮衍生物及其制备方法和含有这些化合物的药物制剂。 这些化合物是具有改善的治疗特征的有效的正性肌力物质。

公开(公告)号：US6133269A

公开(公告)日：2000-10-17

申请号：US992474

申请日：1997-12-17

申请人： Johann Peter Morsdorf ,  Ingomar Grafe

发明人： Johann Peter Morsdorf ,  Ingomar Grafe

IPC分类号： A61K31/505 ,  A61P13/02 ,  A61P15/00 ,  C07D405/12 ,  C07D407/14 ,  A61K31/517

CPC分类号： C07D405/12

摘要： A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 10.68.degree., 14.45.degree., 17.37.degree., 23.45.degree., 23.82.degree. and 24.30 .degree.. Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and pharmaceutical compositions comprising the new form of doxazosin mesylate are also described.

摘要翻译： 描述了新的结晶和无水形式的甲磺酸多沙唑嗪。 新型结晶和无水，其特征在于X射线谱由高和中强度的以下反射位置：10.68°，14.45°，17.37°，23.45°，23.82°和24.30°。 由于其结晶性质，根据本发明的新形式的甲磺酸多沙唑嗪在其合成和药物加工成固体剂型方面具有惊人的优点。 还描述了制备新形式的甲磺酸多沙唑嗪和包含新形式的甲磺酸多沙唑嗪的药物组合物的方法。

公开(公告)号：US06130218A

公开(公告)日：2000-10-10

申请号：US992252

申请日：1997-12-17

申请人： Johann Peter Morsdorf ,  Ingomar Grafe

发明人： Johann Peter Morsdorf ,  Ingomar Grafe

IPC分类号： A61K31/505 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  C07D405/12 ,  C07D407/14 ,  A61K31/517

CPC分类号： C07D405/12

摘要： A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 15.40.degree., 16.85.degree., 18.06.degree., 24.15.degree. and 25.81.degree.. Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and pharmaceutical compositions comprising the new form of doxazosin mesylate are also described.

摘要翻译： 描述了新的结晶和无水形式的甲磺酸多沙唑嗪。 新型结晶无水，其特征在于其X射线光谱由高，中强度的以下反射位置：15.40°，16.85°，18.06°，24.15°和25.81°。 由于其结晶性质，根据本发明的新形式的甲磺酸多沙唑嗪在其合成和药物加工成固体剂型方面具有惊人的优点。 还描述了制备新形式的甲磺酸多沙唑嗪和包含新形式的甲磺酸多沙唑嗪的药物组合物的方法。

公开(公告)号：US4912119A

公开(公告)日：1990-03-27

申请号：US95892

申请日：1987-09-14

申请人： Armin Buschauer ,  Helmut Schickaneder ,  Peter Morsdorf ,  Walter Schunack ,  Gert Baumann ,  Kurt-Henning Ahrens

发明人： Armin Buschauer ,  Helmut Schickaneder ,  Peter Morsdorf ,  Walter Schunack ,  Gert Baumann ,  Kurt-Henning Ahrens

IPC分类号： A61K31/415 ,  A61K31/38 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61P7/02 ,  A61P9/00 ,  A61P9/12 ,  C07D233/54 ,  C07D233/64 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

CPC分类号： C07D233/64 ,  C07D401/12 ,  C07D409/14

摘要： New imidazolyl guanidine derivatives corresponding to the following general formula ##STR1## are described. These compounds may be used in cardiac diseases, certain forms of hypertension and in diseases of arterial occlusion on account of their agonistic action on histamine-H.sub.2 receptors and in part their additional H.sub.1 -antagonistic receptor activity.

摘要翻译： 描述了对应于以下通式的新的咪唑基胍衍生物。 这些化合物可能用于心脏疾病，某些形式的高血压和由于其对组胺-H 2受体的激动作用以及部分其额外的H1拮抗受体活性而在动脉闭塞的疾病中。

公开(公告)号：US4757080A

公开(公告)日：1988-07-12

申请号：US51300

申请日：1987-05-19

申请人： Helmut Schickaneder ,  Peter Morsdorf ,  Armin Buschauer ,  Walter Schunack ,  Heidrun Engler ,  Hartmut Vergin ,  Kurt H. Ahrens

发明人： Helmut Schickaneder ,  Peter Morsdorf ,  Armin Buschauer ,  Walter Schunack ,  Heidrun Engler ,  Hartmut Vergin ,  Kurt H. Ahrens

IPC分类号： A61K31/4427 ,  A61K31/455 ,  A61P9/10 ,  A61P9/12 ,  C07D211/90 ,  C07D401/12 ,  C07D413/14 ,  A61K31/44

CPC分类号： C07D401/12 ,  C07D211/90 ,  C07D413/14

摘要： New compounds which act on the cardiac circulation and correspond to the general formula ##STR1## and may be used for the treatment of cardiac diseases, in certain forms of hypertension and in diseases of arterial occlusion are described.Methods of preparation for these compounds and medicaments containing these compounds are also described.

摘要翻译： 描述了作用于心脏循环并对应于通式并可用于治疗某些形式的高血压和动脉闭塞疾病的心脏疾病的新化合物。 还描述了这些化合物的制备方法和含有这些化合物的药物。

公开(公告)号：US6140334A

公开(公告)日：2000-10-31

申请号：US992251

申请日：1997-12-17

申请人： Johann Peter Morsdorf ,  Ingomar Grafe

发明人： Johann Peter Morsdorf ,  Ingomar Grafe

IPC分类号： A61K31/505 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  C07D405/12 ,  C07D403/14 ,  A61K31/517

CPC分类号： C07D405/12

摘要： A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 8.49.degree., 11.72.degree., 16.03.degree., 18.29.degree., 21.03.degree., 22.87.degree. and 25.02.degree.. Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and pharmaceutical compositions comprising the new form of doxazosin mesylate are also described.

摘要翻译： 描述了新的结晶和无水形式的甲磺酸多沙唑嗪。 新型结晶无水，其特征在于X射线光谱中高强度的以下反射位置：8.49°，11.72°，16.03°，18.29°，21.03°，22.87°和25.02°。 由于其结晶性质，根据本发明的新形式的甲磺酸多沙唑嗪在其合成和药物加工成固体剂型方面具有惊人的优点。 还描述了制备新形式的甲磺酸多沙唑嗪和包含新形式的甲磺酸多沙唑嗪的药物组合物的方法。

公开(公告)号：US06017921A

公开(公告)日：2000-01-25

申请号：US18515

申请日：1998-02-04

申请人： Paul Kennedy ,  Ingomar Grafe ,  Johann Peter Morsdorf ,  Kurt-Henning Ahrens

发明人： Paul Kennedy ,  Ingomar Grafe ,  Johann Peter Morsdorf ,  Kurt-Henning Ahrens

IPC分类号： A61K31/505 ,  A61K31/517 ,  C07D239/95

CPC分类号： C07D239/95

摘要： The present invention provides for a crystalline form of trimetrexate either as a glucuronate, acetate, hydrochloride, methanosulfonate or lactate salt, which can be processed galenically as a stable, well-defined solid substance and processes for producing the crystalline forms. Such crystalline forms allow for prolonged stability in storage and for oral and intravenous administration of the drug.

摘要翻译： 本发明提供了作为葡萄糖醛酸盐，乙酸盐，盐酸盐，甲磺酸盐或乳酸盐的三甲氧
磷酸盐的结晶形式，其可以作为稳定的，明确定义的固体物质进行加成以及制备结晶形式的方法。 这种结晶形式允许在储存和口服和静脉内施用药物时延长稳定性。

公开(公告)号：US5182294A

公开(公告)日：1993-01-26

申请号：US639511

申请日：1991-01-10

申请人： Peter Morsdorf ,  Heidrun Engler ,  Helmut Schickaneder ,  Kurt-Henning Ahrens

发明人： Peter Morsdorf ,  Heidrun Engler ,  Helmut Schickaneder ,  Kurt-Henning Ahrens

IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61P9/00 ,  A61P9/04 ,  C07D401/12

CPC分类号： C07D401/12

摘要： A new imidazolyl propyl guanidine derivative corresponding to formula I ##STR1## is described, which is distinguished by a combination of particularly advantageous properties for the treatment of diseases of the heart and circulation.

摘要翻译： 描述了对应于式I的新的咪唑基丙基胍衍生物（I），其特征在于用于治疗心脏和循环疾病的特别有利的性质的组合。

公开(公告)号：US4954501A

公开(公告)日：1990-09-04

申请号：US247868

申请日：1988-09-21

申请人： Rolf Herter ,  Peter Morsdorf ,  Volker Pfahlert ,  Heidrun Engler ,  Helmut Schickaneder ,  Kurt-Henning Ahrens

发明人： Rolf Herter ,  Peter Morsdorf ,  Volker Pfahlert ,  Heidrun Engler ,  Helmut Schickaneder ,  Kurt-Henning Ahrens

IPC分类号： A61K31/50 ,  A61K31/505 ,  A61P9/04 ,  A61P9/12 ,  C07D237/04 ,  C07D401/10 ,  C07D403/12 ,  C07D417/12

CPC分类号： C07D401/10 ,  C07D237/04 ,  C07D403/12 ,  C07D417/12

摘要： New 6-phenyldihydro-3(2H)-pyridazinones corresponding to the following general formula ##STR1## are described. These compounds are readily prepared in a form suitable for oral administration and are distinguished by a high positive inotropic action and have only a slight effect on blood pressure and cardiac frequency. A process for their preparation and pharmaceutical preparations containing these compounds are also described.

摘要翻译： 描述对应于以下通式的新的6-苯基二氢-3（2H） - 哒嗪酮。 这些化合物容易地以适于口服给药的形式制备，并且通过高的正性肌力作用区分，并且对血压和心脏频率仅具有轻微的影响。 还描述了其制备方法和含有这些化合物的药物制剂。