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31. 发明授权

US5204374A Cycloalkano(b)dihydroindoles and -indolesulphonamides substituted by heterocycles 失效
标题翻译：环己烷（B）二异氰酸酯和异烟肼取代的二羟基苯甲酸酯
公开(公告)号：US5204374A
公开(公告)日：1993-04-20
申请号：US679710
申请日：1991-04-03
申请人： Ulrich E. Muller , Ulrich Rosentreter , Ulrich Niewohner , Elisabeth Perzborn , Erwin Bischoff , Hans-Georg Dellweg , Peter Norman , Nigel J. Cuthbert , Hilary P. Francis
发明人： Ulrich E. Muller , Ulrich Rosentreter , Ulrich Niewohner , Elisabeth Perzborn , Erwin Bischoff , Hans-Georg Dellweg , Peter Norman , Nigel J. Cuthbert , Hilary P. Francis
IPC分类号： A61K31/40 , A61K31/403 , A61P7/02 , A61P11/00 , A61P37/08 , C07D209/86 , C07D209/94 , C07D401/12 , C07D409/12 , C07D417/12
CPC分类号： C07D401/12 , C07D409/12 , C07D417/12
摘要： New cycloalkano[b]dihydroindoles and -indolesulphonamides, substituted by heterocycles, of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different andrepresent hydrogen, nitro, cyano, halogen, trifluoromethyl, carboxyl, hydroxyl or trifluoromethoxy, orrepresent a group of the formula --S(O).sub.w R.sup.5, in whichR.sup.5 denotes alkyl or optionally substituted aryl,w denotes the number 0, 1 or 2, orrepresents alkoxy or alkoxycarbonyl, or benzyloxy, orrepresents a group of the formula --NR.sup.6 R.sup.7, in whichR.sup.6 and R.sup.7 are identical or different anddenote hydrogen, alkyl or acyl ordenote aryl, ordenote a group of the formula --S(O).sub.w R.sup.5, in which R.sup.5 and w have the abovementioned meaning,represent cycloalkyl orrepresent optionally substituted alkyl or alkenyl,m represents the number 1, 2, 3 or 4,n represents the number 0, 1 or 2,z represents the number 1, 2, 3 or 4,A represents a bond or the --NH group,X represents an optionally substituted heterocycle,Y represents hydroxyl, alkoxy, phenoxy or a group of the formula --NR.sup.6 R.sup.7, in whichR.sup.6 and R.sup.7 have the abovementioned meaning, an isomeric form thereof or salts thereof are useful to treat thromboembolisms, ischaemias, asthma and allergies. Processes of making and chemical intermediates are also disclosed.

32. 发明授权

US5155121A Phenylsulphonamide substituted pyridinealkene- and aminooxyalkanecarboxylic acid derivatives 失效
标题翻译：苯基膦酰胺取代的吡嗪基和氨基氧基甲酰氧基酸衍生物
公开(公告)号：US5155121A
公开(公告)日：1992-10-13
申请号：US739747
申请日：1991-08-02
申请人： Ulrich Niewohner , Ulrich E. Muller , Elisabeth Perzborn , Erwin Bischoff , Hans-Georg Dellweg
发明人： Ulrich Niewohner , Ulrich E. Muller , Elisabeth Perzborn , Erwin Bischoff , Hans-Georg Dellweg
IPC分类号： A61K31/44 , A61K31/4406 , A61K31/4418 , A61P7/02 , A61P43/00 , C07D213/44 , C07D213/50 , C07D213/53 , C07D213/55 , C07D213/71 , C12N9/99
CPC分类号： C07D213/53 , C07D213/55 , C07D213/71
摘要： The compounds according to the invention can be prepared by reaction of the corresponding amines with sulphonic acid derivatives, or in the case of the aminooxy compounds by reaction of ketones with aminooxy compounds or alkylation of hydroxylamines, or in the case of the alkene compounds by reaction of ketones with phosphorusylides. The phenylsulphonamide substituted pyridinealkene- and -aminooxyalkenecarboxylic acid derivatives can be used for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, allergies and asthma.
摘要翻译：根据本发明的化合物可以通过相应的胺与磺酸衍生物的反应或在氨基氧化合物的情况下通过酮与氨基氧化合物的反应或羟胺的烷基化反应来制备，或者在烯烃化合物的情况下通过反应的含有二酰亚胺的酮。苯基磺酰胺取代的吡啶亚烷基 - 和 - 氨基氧代羧酸衍生物可用于治疗血栓栓塞障碍，局部缺血，动脉硬化，过敏和哮喘。

33. 发明授权

US5374647A Antithrombotic substituted cycloalkano (B) dihydroindole sulphonamides 失效
标题翻译：抗血栓代用环烷基（B）二氢吲哚磺酰胺
公开(公告)号：US5374647A
公开(公告)日：1994-12-20
申请号：US42857
申请日：1993-04-05
申请人： Horst Bohagen , Ulrich Muller , Ulrich Rosentreter , Erwin Bischoff , Volker-Bernd Fiedler , Elisabeth Perzborn , Joachim Hutter , Peter Norman , Nigel J. Cuthbert , Hilary P. Francis , Marie G. McKenniff
发明人： Horst Bohagen , Ulrich Muller , Ulrich Rosentreter , Erwin Bischoff , Volker-Bernd Fiedler , Elisabeth Perzborn , Joachim Hutter , Peter Norman , Nigel J. Cuthbert , Hilary P. Francis , Marie G. McKenniff
IPC分类号： C07D209/86 , A61K31/40 , A61K31/403 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P37/08 , C07D209/88 , C07D209/94
CPC分类号： C07D209/88
摘要： Substituted antithrombotic substituted cycloalkano[b]dihydroindole- and -indole-sulphonamides for treatment of thromboses, thromboembolisms, ischaemias, asthma and allergies, of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen or other radicals,X is aryl, alkyl or CF.sub.3,m and Z each is 1,2,3 or 4,n is 0,1 or 2,A is a bond or --NH--, andY is OH, alkoxy, aryloxy, amino or sulphonylamine,with the proviso, that in all cases, two of the substituents R.sup.1 -R.sup.4 are other than hydrogen in the event that m represents the number 2 and Y represents the hydroxyl group, or a salt thereof.
摘要翻译：取代的抗血栓形成取代的环烷基[b]二氢吲哚 - 和吲哚磺酰胺，用于治疗其他基团的血栓形成，血栓栓塞，局部缺血，哮喘和过敏，X是芳基，烷基或CF 3，m和Z各自为1 ，2,3或4，n为0,1或2，A为键或-NH-，Y为OH，烷氧基，芳氧基，氨基或磺酰胺，条件是在所有情况下，两个取代基在m表示数2，Y表示羟基的情况下，R 1 -R 4不是氢，或其盐。

34. 发明授权

US5185348A Phenylsulphonamide substituted pyridinealkene- and -aminooxyalkanecarboxylic acid derivatives 失效
标题翻译：苯磺酰胺取代的吡啶烯基 - 和 - 氨基氧烷基羧酸衍生物
公开(公告)号：US5185348A
公开(公告)日：1993-02-09
申请号：US887208
申请日：1992-05-21
申请人： Ulrich Niewohner , Ulrich E. Muller , Elisabeth Perzborn , Erwin Bischoff , Hans-Georg Dellweg
发明人： Ulrich Niewohner , Ulrich E. Muller , Elisabeth Perzborn , Erwin Bischoff , Hans-Georg Dellweg
IPC分类号： C07D213/53 , C07D213/55 , C07D213/71
CPC分类号： C07D213/53 , C07D213/55 , C07D213/71
摘要： The compounds according to the invention can be prepared by reaction of the corresponding amines with sulphonic acid derivatives, or in the case of the aminooxy compounds by reacton of ketones with aminooxy compounds or alkylation of hydroxylamines, or in the case of the alkene compounds by reaction of ketones with phosphorusylides. The phenylsulphonamide substituted pyridinealkene- and -aminooxyalkencarboxylic acid derivatives can be used for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, allergies and asthma.
摘要翻译：根据本发明的化合物可以通过相应的胺与磺酸衍生物反应来制备，或者在氨基氧化合物的情况下通过酮与氨氧基化合物的反应或羟胺的烷基化反应，或在烯烃化合物的情况下通过反应的含有二酰亚胺的酮。苯基磺酰胺取代的吡啶基烯基 - 和 - 氨基氧代羧酸衍生物可用于治疗血栓栓塞性疾病，局部缺血，动脉硬化，过敏和哮喘。

35. 发明授权

US5721238A 2,8-disubstituted quinazolinones 失效
标题翻译： 2,8-二取代喹唑啉酮
公开(公告)号：US5721238A
公开(公告)日：1998-02-24
申请号：US584865
申请日：1996-01-11
申请人： Fred Robert Heiker , Ulrich Niewohner , Wolfgang Hartwig , Helmuth Schutz , Erwin Bischoff , Elisabeth Perzborn , Matthias Schramm
发明人： Fred Robert Heiker , Ulrich Niewohner , Wolfgang Hartwig , Helmuth Schutz , Erwin Bischoff , Elisabeth Perzborn , Matthias Schramm
IPC分类号： A61K31/505 , A61K31/517 , A61K31/535 , A61K31/655 , A61P7/02 , A61P9/06 , A61P9/08 , A61P9/10 , A61P13/08 , A61P29/00 , A61P43/00 , C07D239/91 , C07D405/04 , C07D413/12 , C07D413/14 , C07D239/80
CPC分类号： C07D405/04 , C07D239/91
摘要： 2,8-Disubstituted quinazolinones are prepared by first subjecting the quinazolinone basic skeleton to condensation by customary reactions and then introducing the desired substituents into the 8-position. The compounds are suitable as active compounds in medicaments, in particular for the treatment of inflammations, thromboembolic diseases and cardiovascular diseases.
摘要翻译：通过首先使喹唑啉酮碱性骨架通过常规反应冷凝，然后将所需的取代基引入8-位来制备2,8-二取代喹唑啉酮。该化合物适合作为药物中的活性化合物，特别是用于治疗炎症，血栓栓塞性疾病和心血管疾病。

36. 发明授权

US5039670A Antithrombotic substituted cycloalkano(B)dihydroindole- and -indole-sulphonamides and use 失效
标题翻译：抗血栓取代环烷（B）二氢吲哚 - 和吲哚磺酰胺和用途
公开(公告)号：US5039670A
公开(公告)日：1991-08-13
申请号：US599321
申请日：1990-10-17
申请人： Horst Boshagen , Ulrich Muller , Ulrich Rosentreter , Erwin Bischoff , Volker-Bernd Fiedler , Elisabeth Perzborn , Joachim Hutter , Peter Norman , Nigel J. Cuthbert , Hilary P. Francis , Marie G. McKenniff
发明人： Horst Boshagen , Ulrich Muller , Ulrich Rosentreter , Erwin Bischoff , Volker-Bernd Fiedler , Elisabeth Perzborn , Joachim Hutter , Peter Norman , Nigel J. Cuthbert , Hilary P. Francis , Marie G. McKenniff
IPC分类号： C07D209/86 , A61K31/40 , A61K31/403 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P37/08 , C07D209/88 , C07D209/94
CPC分类号： C07D209/88
摘要： Substituted antithrombotic substituted cycloalkano[b]-dihydroindole- and -indole-sulphonamides for treatment of thromboses, thromboembolisms, ischemias, asthma and allergies, of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen or other radicals,X is aryl, alkyl or CF.sub.3,m and Z each is 1,2,3 or 4,n is 0, 1 or 2,A is a bond or --NH--, andY is OH, alkoxy, aryloxy, amino or sulphonylamine, with the proviso that, in all cases, two of the substituents R.sup.1 -R.sup.4 are other than hydrogen in the event that m represents the number 2 and Y represents the hydroxyl group,or a salt thereof.
摘要翻译：用于治疗式（I）的血栓形成，血栓栓塞，缺血，哮喘和过敏的取代的抗血栓形成取代的环烷基[b] - 二氢吲哚和吲哚磺酰胺，其中R 1，R 2，R 3和R 4是氢或其它基团，X是芳基，烷基或CF 3，m和Z各自为1,2,3或4，n为0,1或2，A为键或-NH-，Y为OH，烷氧基，芳氧基，氨基或磺酰胺，条件是在所有情况下，在m表示数2且Y表示羟基的情况下，两个取代基R 1 -R 4不同于氢，或其盐。

37. 发明申请

US20080085897A1 Use of 2-alkoxyphenyl-substituted imidazotriazinones 审中-公开
标题翻译：使用2-烷氧基苯基取代的咪唑并三嗪酮
公开(公告)号：US20080085897A1
公开(公告)日：2008-04-10
申请号：US11906382
申请日：2007-10-01
申请人： Ulrich Niewohner , Maria Niewohner , Erwin Bischoff , Helmut Haning , Afssaneh Rahbar , Tiemo-Joerg Bandel , Wolfgang Barth
发明人： Ulrich Niewohner , Maria Niewohner , Erwin Bischoff , Helmut Haning , Afssaneh Rahbar , Tiemo-Joerg Bandel , Wolfgang Barth
IPC分类号： A61K31/53 , A61K31/5377 , A61P13/08 , A61P13/10 , A61P35/00 , A61P9/00
CPC分类号： A61K31/53 , A61K31/5377
摘要： The present invention relates to the use of known 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position and cGMP PDE-inhibitory properties for the treatment of cardiac insufficiency, cancer, bladder disorders, or prostate hyperplasia.
摘要翻译：本发明涉及在9位具有短的无支链烷基的已知2-苯基取代的咪唑并三嗪酮和cGMP PDE抑制性质用于治疗心功能不全，癌症，膀胱病或前列腺增生的用途。

38. 发明申请

US20050234022A1 Use of 2-alkoxyphenyl-substituted imidazotriazinones 失效
标题翻译：使用2-烷氧基苯基取代的咪唑并三嗪酮
公开(公告)号：US20050234022A1
公开(公告)日：2005-10-20
申请号：US11156082
申请日：2005-06-17
申请人： Ulrich Niewohner , Maria Niewohner , Erwin Bischoff , Helmut Haning , Afssaneh Rahbar , Tiemo-Joerg Bandel , Wolfgang Barth
发明人： Ulrich Niewohner , Maria Niewohner , Erwin Bischoff , Helmut Haning , Afssaneh Rahbar , Tiemo-Joerg Bandel , Wolfgang Barth
IPC分类号： C07D487/04 , A61K31/00 , A61K31/53 , A61K31/5377 , A61K31/675 , A61P1/00 , A61P3/10 , A61P9/04 , A61P9/12 , A61P11/00 , A61P11/12 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P15/06 , A61P15/08 , A61P17/06 , A61P17/14 , A61P23/00 , A61P25/04 , A61P25/16 , A61P27/06 , A61P27/16 , A61P35/00 , C07D519/00 , A61K31/541
CPC分类号： A61K31/53 , A61K31/5377
摘要： The present invention relates to the use of known 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position and cGMP PDE-inhibitory properties for the production of medicaments for the treatment of cardiac insufficiency, psoriasis, female infertility, cancer, diabetes, ophthalmic disorders such as glaucoma, disorders of gastric motility, cystic fibrosis, premature labour, pulmonary hypertension, bladder disorders, prostate hyperplasia, nitrate-induced tolerance, pre-eclampsia, alopecia, Parkinson's disease, pain, tinnitus or the renal syndrome.
摘要翻译：本发明涉及在9位具有短的无支链烷基的已知2-苯基取代的咪唑并三氮嗪酮和cGMP PDE抑制性质用于生产用于治疗心功能不全的药物，牛皮癣，女性不育症，癌症糖尿病，眼科疾病如青光眼，胃动力障碍，囊性纤维化，早产，肺动脉高压，膀胱疾病，前列腺增生，硝酸盐诱导的耐受，先兆子痫，脱发，帕金森病，疼痛，耳鸣或肾综合征。

39. 发明申请

US20060148802A1 Use of compounds that stimulate cgmp 审中-公开
标题翻译：使用刺激cgmp的化合物
公开(公告)号：US20060148802A1
公开(公告)日：2006-07-06
申请号：US10516778
申请日：2003-05-30
申请人： Helmut Haning , Erwin Bischoff , UIrich Niewohner , Maria Niewohner
发明人： Helmut Haning , Erwin Bischoff , UIrich Niewohner , Maria Niewohner
IPC分类号： A61K31/53
CPC分类号： A61K31/53
摘要： The invention relates to the use of compounds that stimulate cGMP, in particular imidazo[1,3,5]triazinones, for producing a medicament for the treatment and/or prophylaxis of diseases, in which the clinical picture can be improved and/or cured by the improvement of the micro-circulation of tissue containing a phosphodiesterase that metabolises cGMP.
摘要翻译：本发明涉及刺激cGMP，特别是咪唑并[1,3,5]三嗪酮的化合物在制备用于治疗和/或预防疾病的药物中的用途，其中可以改善和/或治愈临床症状通过改善含有代谢cGMP的磷酸二酯酶的组织的微循环。

40. 发明申请

US20080096880A1 Novel use of imidazotriazinones 审中-公开
标题翻译：新型使用咪唑并三嗪酮
公开(公告)号：US20080096880A1
公开(公告)日：2008-04-24
申请号：US10519129
申请日：2003-06-24
申请人： Helmut Haning , Erwin Bischoff , Ulrich Niewohner , Maria Niewohner
发明人： Helmut Haning , Erwin Bischoff , Ulrich Niewohner , Maria Niewohner
IPC分类号： A61K31/5377 , A61K31/53 , A61P25/00 , A61P3/00 , A61P9/00 , C07D413/14 , C07D487/04
CPC分类号： A61K31/53
摘要： The invention relates to novel uses of imidazo[1,2,4]triazinones for producing a medicament for the treatment and/or prophylaxis of coronary cardiopathy, heart failure, pulmonary hypertension, bladder complaints, prostatic hyperplasia, nitrate-induced tolerance, or diseases of the eye, such as glaucoma, for the treatment or prophylaxis of central, retinal or posterior ciliary artery occlusion, central retinal vein occlusion, optical neuropathy, such as anterior ischaemic optical neuropathy and glaucomatous optical neuropathy, in addition to macular degeneration, diabetes, in particular diabetic gastroparesis, for the treatment of dysperistalsis of the stomach and oesophagus, female infertility, premature contractions, pre-eclampsia, alopecia, psoriasis associated with renal syndrome, cystic fibrosis, cancer and for improving cognition, powers of concentration, learning skills or hypermnesia, in particular if the disorder is a symptom of dementia.
摘要翻译：本发明涉及咪唑并[1,2,4]三嗪酮在制备用于治疗和/或预防冠状动脉心脏病，心力衰竭，肺动脉高压，膀胱反应，前列腺增生，硝酸盐诱导的耐受或疾病的药物中的新用途的眼睛，如青光眼，用于治疗或预防中枢，视网膜或后睫状动脉闭塞，视网膜中央静脉阻塞，光学神经病变，如前部缺血性视神经病变和青光眼性视神经病变，以及黄斑变性，糖尿病，特别是糖尿病性胃轻瘫，用于治疗胃和食道的dysperistalsis，女性不孕症，早产，先兆子痫，脱发，与肾综合征相关的牛皮癣，囊性纤维化，癌症和改善认知，集中力，学习技能或特别是如果该疾病是痴呆的症状。

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