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1. 发明授权

US4457938A Antimycotic agent, in the form of sticks, with a high release of active compound 失效
标题翻译：具有高释放活性化合物的棒状形式的抗真菌剂
公开(公告)号：US4457938A
公开(公告)日：1984-07-03
申请号：US346479
申请日：1982-02-05
申请人： Miklos von Bittera , Karl H. Buchel , Manfred Plempel , Erik Regel
发明人： Miklos von Bittera , Karl H. Buchel , Manfred Plempel , Erik Regel
IPC分类号： A61K9/00 , A61K9/06 , A61K31/415 , A61K47/10 , A61K47/12 , A61K47/14 , A61P31/04 , A61P31/10
CPC分类号： A61K47/10 , A61K31/415 , A61K47/12 , A61K47/14 , A61K9/0014 , Y10S424/05
摘要： The invention relates to stick formulations of antimycotic azole derivatives containing, in addition to the antimycotic azole derivatives, 3 to 5% by weight relative to the formulation, of benzyl alcohol, 2.5 to 10% by weight, relative to the formulation of spreading agent and one or more auxiliaries.
摘要翻译：本发明涉及抗真菌唑衍生物的粘性制剂，除了抗真菌唑衍生物之外，相对于制剂，除了抗真菌唑类衍生物之外，相对于铺展剂的制剂，苄基醇为2.5〜10重量％一种或多种助剂。

2. 发明授权

US4582717A Process for production of vaginal tampons containing pharmaceutical active compound 失效
标题翻译：生产含有药物活性化合物的阴道棉塞的方法
公开(公告)号：US4582717A
公开(公告)日：1986-04-15
申请号：US634941
申请日：1984-07-27
申请人： Miklos von Bittera , Karl H. Buchel , Manfred Plempel , Erik Regel
发明人： Miklos von Bittera , Karl H. Buchel , Manfred Plempel , Erik Regel
IPC分类号： C07D233/58 , A61K9/00 , A61K9/02 , A61L15/20 , A61L15/46 , C07D233/62 , A01N1/02 , A61F13/16 , A61F13/18 , A61F13/20
CPC分类号： A61L15/46 , A61K9/0036 , A61L15/20 , A61L2300/202 , A61L2300/408 , Y10S604/904
摘要： The invention relates to a process for production of tampons containing novel formulations of antimycotic azole derivatives which provide a higher release of active compounds and make short-term therapy possible. The tampon formulations of the invention contain active antimycotic azole derivatives in impregnated form, only melting at body temperature, or dissolved form, such as, for example, in suppository bases or their combinations with emulsifiers and/or spreading agents and/or solubilisers.
摘要翻译：本发明涉及一种生产含有抗真菌唑衍生物的新制剂的棉塞的方法，其提供较高释放的活性化合物并使短期治疗成为可能。本发明的棉条制剂含有浸渍形式的活性抗真菌唑衍生物，其仅在体温下熔化或溶解形式，例如栓剂基质或其与乳化剂和/或铺展剂和/或增溶剂的组合。

3. 发明授权

US4627852A Active compound release systems 失效
标题翻译：活性化合物释放系统
公开(公告)号：US4627852A
公开(公告)日：1986-12-09
申请号：US681977
申请日：1984-12-14
申请人： Miklos von Bittera , Rolf-Volker Meyer
发明人： Miklos von Bittera , Rolf-Volker Meyer
IPC分类号： A61K9/70 , A61F7/02
CPC分类号： A61K9/7053 , A61K9/7076
摘要： In a therapeutic system such as a plaster for administration of an active compound through the skin and comprising a covering layer which is essentially impermeable to the active compound, an active coupound reservoir layer and a protective layer which can be pulled off and which is essentially impermeable to the active compound, the improvement wherein the reservoir layer contains about 1-30% of active compound in an elastomer mixture comprising a diene rubber which can optionally be copolymerized with an .alpha.-olefin, mixed with from 0 up to about 70% by weight of a polyisobutylene, polybutadiene oil and/or paraffin oil, and a tackifying resin. Thereby the active compound can be released in regulated relatively large quantity over a prolonged period of time.
摘要翻译：在诸如用于通过皮肤施用活性化合物的石膏的治疗系统中，包括基本上不可渗透活性化合物的覆盖层，活性偶合储库层和可以被拉出并且基本上不渗透的保护层对活性化合物的改进，其中储层在弹性体混合物中含有约1-30％的活性化合物，其包含二烯橡胶，其可以任选地与α-烯烃共聚，与0至约70重量％的聚异丁烯，聚丁二烯油和/或石蜡油，以及增粘树脂。因此，活性化合物可以在更长的时间内以相对大的量调节释放。

4. 发明授权

US5104879A Antimycotically active substituted 2-aminothiazoles 失效
标题翻译：抗微生物活性取代的2-氨基丁酸
公开(公告)号：US5104879A
公开(公告)日：1992-04-14
申请号：US596626
申请日：1990-10-11
申请人： Joachim Ippen , Bernd Baasner , Klaus Schaller , Miklos von Bittera
发明人： Joachim Ippen , Bernd Baasner , Klaus Schaller , Miklos von Bittera
IPC分类号： A61K31/505 , A61P31/04 , C07C45/00 , C07C45/63 , C07C49/80 , C07C49/84 , C07D417/12 , C07D417/14
CPC分类号： C07D417/12 , C07C45/004 , C07C45/63 , C07C49/80 , C07C49/84 , C07D417/14
摘要： Antimicotically active 2-aminothiazoles have been found having the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl andR.sup.2 represents optionally substituted cyclohexyl or phenyl which is substituted by halogen, alkyl, halogenoalkyl, halogenoalkoxy, dioxyhalogenoalkyl or halogenoalkylthio,and their physiologically tolerable acid addition salts,with the exception of the compounds 4-(4-chlorophenyl)-2-[2-(1,4,5,6-tetrahydropyrimidinyl)-amino]thiazole and 4-(2,4-dichlorophenyl)-2-[2-(1,4,5,6-tetrahydropyrimidinyl)-amino]-thiazole and 4-(4-chloro-2-methylphenyl)-2-[2-(1,4,5,6-tetrahydropyrimidinyl)-amino]-thiazole and with the exception of the physiologically tolerable acid addition salts of these compoundshave been found.
摘要翻译：已经发现具有式“IMAGE”的反活性2-氨基噻唑，其中R1代表氢或烷基，R2代表任选取代的环己基或被卤素，烷基，卤代烷基，卤代烷氧基，二卤基烷基或卤代烷硫基取代的苯基，以及它们的生理可耐受酸加成盐，除4-（4-氯苯基）-2- [2-（1,4,5,6-四氢嘧啶基） - 氨基]噻唑和4-（2,4-二氯苯基）-2- [2-（1,4,5,6-四氢嘧啶基） - 氨基] - 噻唑和4-（4-氯-2-甲基苯基）-2- [2-（1,4,5,6-四氢嘧啶基） - 氨基] - 噻唑，除了这些化合物的生理可耐受酸加成盐之外。

5. 发明授权

US4661099A Self-adhesive sheet-like structures, process for their preparation and their use 失效
标题翻译：自粘片状结构，其制备方法及其用途
公开(公告)号：US4661099A
公开(公告)日：1987-04-28
申请号：US669402
申请日：1984-11-08
申请人： Miklos von Bittera , Dietmar Schapel , Ulrich von Gizycki , Roland Rupp
发明人： Miklos von Bittera , Dietmar Schapel , Ulrich von Gizycki , Roland Rupp
IPC分类号： A61L15/20 , A61L15/58 , C08G18/08 , C09J7/02 , C09J175/04 , A61F13/02 , A61L15/06 , C08K5/06 , C08L75/04
CPC分类号： A61F13/063 , A61L15/20 , A61L15/58 , C08G18/08 , C09J175/04 , C09J7/0207 , C08G2220/00 , Y10T428/263 , Y10T428/2852 , Y10T428/2857 , Y10T428/2874 , Y10T428/2878 , Y10T428/2896 , Y10T442/2738
摘要： The present disclosure is concerned with self-adhesive sheet-like structures made by adhering an adhesive polyurethane gel material to a supporting substrate and the utilization of such structures in the medical field to adhere materials such as plasters, wound dressings and appliances to the human body, and in other fields to connect articles, such as the parts of a fractured or cracked object, to one another by means of an adhesive bond. The gel is formed by immobilizing a high molecular weight polymeric polyol in the matrix of a covalently crosslinked polyurethane which is prepared by reacting polyisocyanates having an isocyanate functionality of at least 2 with higher molecular weight polyhydroxyl compounds having a hydroxyl functionality of at least 3. These reactants are selected in accordance with the following formula which relates the isocyanate number, K, (isocyanate to hydroxyl equivalents ratio times 100) to the average functionalities of the polyisocyanates (F.sub.I) and of the polyhydroxyl compounds (F.sub.P) as follows: ##EQU1## wherein X is less than or equal to 120. These reactants are also selected to give a weight ratio of matrix to immobilized polymeric polyol of between about 15:85 and 62:38.
摘要翻译：本公开涉及通过将粘性聚氨酯凝胶材料粘附到支撑基底而制成的自粘片状结构，并且在医疗领域中利用这种结构将诸如膏药，伤口敷料和器具等材料粘附到人体上，并且在其他领域中，通过粘合剂粘合将诸如断裂或裂纹物体的部分的物品彼此连接。凝胶通过将高分子量聚合物多元醇固定在共价交联的聚氨酯的基质中而形成，该聚合物多羟基化合物通过使具有至少2个异氰酸酯官能度的多异氰酸酯与具有至少3个羟基官能度的较高分子量多羟基化合物反应而制备。根据以下公式选择反应物：将异氰酸酯数K（异氰酸酯与羟基当量比100倍）相对于多异氰酸酯（FI）和多羟基化合物（FP）的平均官能度如下所述：其中X小于或等于120.这些反应物也被选择为使基质与固定的聚合多元醇的重量比在约15:85和62:38之间。

6. 发明授权

US4738670A Medicinal plasters 失效
标题翻译：药膏
公开(公告)号：US4738670A
公开(公告)日：1988-04-19
申请号：US72063
申请日：1987-07-10
申请人： Miklos von Bittera
发明人： Miklos von Bittera
IPC分类号： A61K9/70 , A61L15/44 , A61L15/06
CPC分类号： A61K9/7053 , A61K9/7076 , A61L15/44 , A61L2300/41
摘要： A medicinal plaster comprising a covering layer, a reservior layer for an active compound and a detachable protective layer is disclosed. The covering is a substantially impermeable material comprising a textile sheet-like structure which is longitudinally and transversely elastic and is impregnated or coated with a polymer. Disposed on such a covering layer is a reservior layer comprising 1 to 30% by weight of active compound is an elastomeric mixture comprising a polyisobutylene polymer, a carrier such as a polybutadiene oil or liquid paraffin and a resin such as a polybutadiene oil or liquid paraffin and a resin such as a adhesion-conferring resin. Methods for the formation of such medicinal plaster and the use of such medicinal plaster, especially to apply large dosages of antiinflammatory materials are disclosed.
摘要翻译：公开了一种药膏，其包含覆盖层，活性化合物的储液层和可拆卸保护层。覆盖物是基本上不可渗透的材料，其包括纵向和横向弹性并被聚合物浸渍或涂覆的织物片状结构。在这样的覆盖层上设置的是含有1〜30重量％的活性化合物的储液层，是包含聚异丁烯聚合物，载体如聚丁二烯油或液体石蜡和树脂如聚丁二烯油或液体石蜡的弹性体混合物以及树脂如粘合赋予树脂。公开了形成这种药膏的方法和使用这种药膏，特别是应用大剂量的抗炎材料。

7. 发明授权

US4661104A Active compound release systems 失效
标题翻译：活性化合物释放系统
公开(公告)号：US4661104A
公开(公告)日：1987-04-28
申请号：US681976
申请日：1984-12-14
申请人： Miklos von Bittera , Rolf-Volker Meyer , Rolf Dhein
发明人： Miklos von Bittera , Rolf-Volker Meyer , Rolf Dhein
IPC分类号： A61K9/70 , A61F7/02 , A61F13/02 , A61L15/03 , A61L15/06
CPC分类号： A61K9/7053 , A61K9/7076 , Y10T428/24479
摘要： In a therapeutic system such as a plaster for administration of an active compound through the skin and comprising a covering layer which is essentially impermeable to the active compound, an active compound reservoir layer and a protective layer which can be pulled off and which is essentially impermeable to the active compound, the improvement wherein the reservoir layer contain about 1-30% of active compound in an elastomer mixture comprising a predominantly amorphous olefinic (co)polymer with a glass transition temperature of
摘要翻译：在诸如用于通过皮肤施用活性化合物的石膏的治疗系统中，包括基本上不可渗透活性化合物的覆盖层，活性化合物储存层和可以被拉出并且基本上不渗透的保护层对活性化合物的改进，其中储层在含有玻璃化转变温度<20℃的主要是无定形烯烃（共）聚合物的弹性体混合物中含有约1-30％的活性化合物，与0混合至约50重量％的聚异丁烯，聚丁二烯油和/或石蜡油，以及增粘树脂。因此，活性化合物可以在更长的时间内以相对大的量调节释放。

8. 发明授权

US4283400A Medicated animal feed based on liver meal 失效
标题翻译：基于肝粉的药用动物饲料
公开(公告)号：US4283400A
公开(公告)日：1981-08-11
申请号：US73990
申请日：1979-09-10
申请人： Miklos von Bittera , Herbert Voege , Reinwalt Bauditz
发明人： Miklos von Bittera , Herbert Voege , Reinwalt Bauditz
IPC分类号： A23K1/16 , A23K1/10 , A61K9/20 , A61K31/495 , A61P33/00 , A61K31/43 , A61K31/325 , A61K31/65
CPC分类号： A61K9/2068 , A23K10/20 , Y10S514/974
摘要： The invention relates to the provision of medicated animal feeds comprising one or more pharmaceutically active compounds and liver meal as a formulation auxiliary. Also included in the invention are methods for the use of said animal feeds of the invention.
摘要翻译：本发明涉及提供包含一种或多种药物活性化合物和肝粉作为制剂助剂的药用动物饲料。本发明还包括使用本发明所述动物饲料的方法。

9. 发明授权

US4225578A Animal collars having ectoparasiticidal activity 失效
标题翻译：动物圈具有外寄生虫活性
公开(公告)号：US4225578A
公开(公告)日：1980-09-30
申请号：US25427
申请日：1979-03-30
申请人： Miklos von Bittera , Hans U. Sieveking , Wilhelm Stendel , Herbert Voege
发明人： Miklos von Bittera , Hans U. Sieveking , Wilhelm Stendel , Herbert Voege
IPC分类号： A01K13/00 , A01K27/00 , A01N25/34 , A01N47/22 , A01K29/00 , A01N17/00
CPC分类号： A01K27/007 , A01N25/34
摘要： The instant invention relates to new ectoparasiticidally (especially insecticidally and acaricidally) active animal collars, which are prepared by impregnating suitable carriers with certain ectoparasiticides, and to a process for their preparation.
摘要翻译：本发明涉及通过用某些外寄生物杀螨剂浸渍合适的载体制备的新的外寄生（特别是杀虫和杀螨剂）活性动物领，以及其制备方法。

10. 发明授权

US4956370A Antimycotically active substituted 2-aminothiazoles 失效
标题翻译：抗真菌活性取代的2-氨基噻唑
公开(公告)号：US4956370A
公开(公告)日：1990-09-11
申请号：US419981
申请日：1989-10-11
申请人： Joachim Ippen , Bernd Baasner , Albrecht Marhold , Ernst Kysela , Klaus Schaller , Miklos von Bittera
发明人： Joachim Ippen , Bernd Baasner , Albrecht Marhold , Ernst Kysela , Klaus Schaller , Miklos von Bittera
IPC分类号： A61K31/505 , A61P31/04 , C07C45/00 , C07C45/46 , C07C45/63 , C07C45/71 , C07C49/84 , C07C205/37 , C07C205/38 , C07D417/12
CPC分类号： C07D417/12 , C07C205/37 , C07C205/38 , C07C45/00 , C07C45/004 , C07C45/46 , C07C45/63 , C07C45/71 , C07C49/84
摘要： A 2-aminothiazole of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl andR.sup.2 represents a radical of the formula ##STR2## where R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another in each case represent hydrogen, halogen, nitro, alkyl, alkoxy, alkoxycarbonyl, dialkylamino, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, halogenoalkylsulphinyl or halogenoalkylsulphonyl,X represents oxygen, sulphur, sulphinyl or sulphonyl andAr represents an unsubstituted aryl or a substituted aryl radical,and their physiologically tolerable acid addition salts.
摘要翻译：其中R 1表示氢或烷基，R 2表示下式的基团，其中R 3，R 4，R 5和R 6在各种情况下彼此独立地表示氢，卤素，硝基，烷基，烷氧基，烷氧基羰基，二烷基氨基，烷硫基，烷基亚磺酰基，烷基磺酰基，卤代烷基，卤代烷氧基，卤代烷硫基，卤代烷基亚磺酰基或卤代烷基磺酰基，X表示氧，硫，亚磺酰基或磺酰基，Ar表示未取代的芳基或取代的芳基，及其生理上可耐受的酸加成盐。

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