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1. 发明授权

US4614741A Depot antiinflammatory agents 失效
标题翻译：仓库抗炎剂
公开(公告)号：US4614741A
公开(公告)日：1986-09-30
申请号：US622423
申请日：1984-06-20
申请人： Hans-Dieter Dell , Bernhard Pelster , Reinhold Kraus , Detlef Schierstedt
发明人： Hans-Dieter Dell , Bernhard Pelster , Reinhold Kraus , Detlef Schierstedt
IPC分类号： A61K9/107 , A61K9/00 , A61K31/19 , A61K47/14 , A61K47/44 , A61K31/40 , A61K31/195 , A61K31/54
CPC分类号： A61K31/19 , A61K47/14 , A61K47/44 , A61K9/0019
摘要： The invention relates to depot formulations containing, as an active antiinflammatory and/or analgesic agent a compound of Formula I, infra together with a suspension medium. Typical suspension agents are glycerides and/or esters of mono- or poly-hydric alcohols as well as selected ethers, alcohols and amides.
摘要翻译：本发明涉及含有作为活性抗炎和/或止痛剂的式I化合物与含有悬浮介质的式I化合物的贮库制剂。典型的悬浮剂是甘油酯和/或单醇或多元醇的酯，以及选择的醚，醇和酰胺。

2. 发明授权

US4539402A Quinazolinone derivatives 失效
标题翻译：喹唑啉酮衍生物
公开(公告)号：US4539402A
公开(公告)日：1985-09-03
申请号：US492775
申请日：1983-05-09
申请人： Wolfgang Opitz , Haireddin Jacobi , Bernhard Pelster
发明人： Wolfgang Opitz , Haireddin Jacobi , Bernhard Pelster
IPC分类号： A61K31/505 , A61P25/04 , A61P25/20 , A61P29/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to quinazolinone derivatives and of formula (I) as defined herein and processes for the production of said derivatives. Also included in the invention are pharmaceutical compositions containing a compound of said formula (I) as active ingredient and the use of said compounds and compositions as anti-inflammatory agents.
摘要翻译：本发明涉及喹唑啉酮衍生物和本文所定义的式（I）和用于制备所述衍生物的方法。本发明还包括含有所述式（I）化合物作为活性成分的药物组合物和所述化合物和组合物作为抗炎剂的用途。

3. 发明授权

US4628062A 1,4-naphthoquinone derivatives having anti-inflammatory action 失效
标题翻译：具有抗炎作用的1,4-萘醌衍生物
公开(公告)号：US4628062A
公开(公告)日：1986-12-09
申请号：US682408
申请日：1984-12-17
申请人： Wolfgang Opitz , Bernhard Pelster , Romanis Fruchtmann , Udo Krupka , Walter Gauss , Hartmut Kiehne , Hermann Oediger
发明人： Wolfgang Opitz , Bernhard Pelster , Romanis Fruchtmann , Udo Krupka , Walter Gauss , Hartmut Kiehne , Hermann Oediger
IPC分类号： A61K31/12 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/18 , A61K31/19 , A61P29/00 , C07C45/00 , C07C50/24 , C07C50/32 , C07C50/38 , C07C67/00 , C07C213/00 , C07C225/30 , C07C233/32 , C07C301/00 , C07C311/00 , C07C313/00 , C07C323/38 , C07C50/14 , C07C97/22
CPC分类号： C07C50/24 , A61K31/12 , A61K31/135 , A61K31/16 , C07C50/32 , C07C50/38
摘要： New compounds of the formula ##STR1## in which R.sub.1 is an allylamino, acetylamino or propionylamino radical,R.sub.2 is hydrogen or a 2-methoxyethoxy or ethoxy radical,R.sub.3 is hydrogen or a sulphamoyl radical, andR.sub.4 is hydrogen,and of the formula ##STR2## in which R.sub.1 is a halogen atom or a free or substituted hydroxyl, sulphhydryl or amino group,R.sub.2 is a hydrogen atom, an alkyl radical, a halogen atom, or a free or substituted hydroxyl, sulphhydryl or amino group,R.sub.3 and R.sub.4 each independently is hydrogen, alkyl, hydroxyl, alkoxy, sulphonamido or halogen, with the proviso that R.sub.2, R.sub.3 and R.sub.4 are hydrogen when R.sub.1 is hydroxyl,exhibit anti-inflammatory activity.
摘要翻译：式中，R1是烯丙基氨基，乙酰氨基或丙酰基氨基，R2是氢或2-甲氧基乙氧基或乙氧基的新化合物，其中R 3是氢或氨磺酰基，R 4是氢， IMAGE>其中R1是卤素原子或游离或取代的羟基，巯基或氨基，R2是氢原子，烷基，卤素原子或游离或取代的羟基，巯基或氨基，R3和R4 每个独立地是氢，烷基，羟基，烷氧基，磺酰胺基或卤素，条件是当R 1是羟基时，R 2，R 3和R 4是氢，表现出抗炎活性。

4. 发明授权

US4861878A 1H-pyrido-(2,3-b) (1,4)-thiazines 失效
标题翻译： 1H-吡啶并（2,3-b）（1,4） - 噻嗪
公开(公告)号：US4861878A
公开(公告)日：1989-08-29
申请号：US927909
申请日：1986-11-06
申请人： Gerd Fengler , Alexander Klausener , Hans-Josef Buysch , Mithat Mardin , Bernhard Pelster
发明人： Gerd Fengler , Alexander Klausener , Hans-Josef Buysch , Mithat Mardin , Bernhard Pelster
IPC分类号： A61K31/54 , A61P11/00 , A61P29/00 , A61P37/08 , C07D513/04
CPC分类号： C07D513/04
摘要： New potent lipoxygenase inhibitors which are 1H-pyrido-[2,3-b][1,4] thiazines are disclosed. The new thiazines are of the formula ##STR1## in which R.sup.1 denotes hydrogen, halogen, optionally substituted alkyl or alkoxy or the group ##STR2## in which R.sup.5 and R.sup.6 are identical or different and denote hydrogen, optionally substituted alkyl or aryl, or can be linked to form a 5- or 6-membered heterocyclic ring,R.sup.2 and R.sup.3 are identical or different and denote hydrogen or optionally substituted alkyl or alkoxy andR.sup.4 denotes hydroxyl, the group ##STR3## in which R.sup.5 and R.sup.6 have the abovementioned meaning, or, in the case where R.sup.3 denotes hydrogen or optionally substituted alkoxy, also denotes optionally substituted alkoxy.
摘要翻译：公开了新的有效的脂氧合酶抑制剂，它们是1H-吡啶并[2,3-b] [1,4]噻嗪。新的噻嗪类具有式“IMAGE”，其中R 1表示氢，卤素，任选取代的烷基或烷氧基或其中R 5和R 6相同或不同并表示氢，任选取代的烷基或芳基或可以连接形成5-或6-元杂环，R2和R3相同或不同，表示氢或任选取代的烷基或烷氧基，R4表示羟基，其中R5和R6具有上述含义的基团或者在R3表示氢或任选取代的烷氧基的情况下，也表示任选取代的烷氧基。

5. 发明授权

US4710491A N-glycosylated carboxylic acid derivatives as agents for combating rheumatic diseases 失效
标题翻译： N-糖基化羧酸衍生物作为抗风湿病的药剂
公开(公告)号：US4710491A
公开(公告)日：1987-12-01
申请号：US681965
申请日：1984-12-14
申请人： Oswald Lockhoff , Peter Stadler , Hans-Georg Opitz , Harald Horstmann , Bodo Junge , Bernhard Pelster
发明人： Oswald Lockhoff , Peter Stadler , Hans-Georg Opitz , Harald Horstmann , Bodo Junge , Bernhard Pelster
IPC分类号： A61K31/70 , A61K31/7008 , A61K31/7024 , A61K31/7028 , A61P29/00 , C07H5/06 , C07H13/04 , C07H13/06 , C07H15/04 , C07H15/12 , C07H15/18
CPC分类号： C07H13/04 , C07H13/06 , C07H15/04 , C07H15/18
摘要： A method of combating rheumatic diseases which comprises administering to a patient afflicted therewith an amount effective to combat such disease of a compound of the formula ##STR1## in which Z is a glycosyl radical bonded via the anomeric carbon atom,R.sub.1 is hydrogen or an optionally substituted hydrocarbon radical with up to 30 C atoms, which hydrocarbon radical is optionally interrupted by O, N or S, andR.sub.2 is hydrogen or an alkyl or aralkyl radical with up to 30 C atoms, which is optionally interrupted by O, N or S or substituted by an oxygen-containing group or halogen,with the proviso that COR.sub.1 is not an acyl group with 1-5 C atoms if R.sub.2 is alkyl with 10-20 C atoms.
摘要翻译：一种抗风湿性疾病的方法，其包括对患有其有效抗击下列化合物的疾病的患者施用：其中Z是通过端基异构体碳原子键合的糖基，R1是氢或任选的具有多达30个C原子的取代的烃基，该烃基任选地被O，N或S间隔，并且R 2是氢或具有至多30个C原子的烷基或芳烷基，其任选地被O，N或S 或被含氧基团或卤素取代，条件是如果R2是具有10-20个C原子的烷基，则COR1不是具有1-5个C原子的酰基。

6. 发明授权

US4698344A 1-Heteroaryl-4-aryl-pyrazolin-5-ones for use as medicaments 失效
标题翻译： 1-杂芳基-4-芳基 - 吡唑啉-5-酮，用作药物
公开(公告)号：US4698344A
公开(公告)日：1987-10-06
申请号：US800485
申请日：1985-11-21
申请人： Klaus Sasse , Michael Hammond , Friedel Seuter , Elisabeth Perzborn , Bernhard Pelster , Graham Sturton , Trevor Abram
发明人： Klaus Sasse , Michael Hammond , Friedel Seuter , Elisabeth Perzborn , Bernhard Pelster , Graham Sturton , Trevor Abram
IPC分类号： C07D213/77 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4412 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/505 , A61P7/02 , A61P29/00 , A61P37/08 , C07D231/22 , C07D251/46 , C07D317/00 , C07D401/04 , C07D403/04 , C07D405/14 , C12N9/99
CPC分类号： C07D401/04 , C07D403/04 , C07D405/14
摘要： The invention relates to 1-heteroaryl-4-aryl-pyrazolin-5-ones, a preparation process and the use in combating diseases, in particular for use as lipoxygenase inhibitors.
摘要翻译：本发明涉及1-杂芳基-4-芳基 - 吡唑啉-5-酮，其制备方法以及抗疾病特别用作脂氧合酶抑制剂的用途。

7. 发明授权

US4594357A Depot antiinflammatory agents 失效
公开(公告)号：US4594357A
公开(公告)日：1986-06-10
申请号：US622425
申请日：1984-06-20
申请人： Hans-Dieter Dell , Bernhard Pelster , Reinhold Kraus , Detlef Schierstedt
发明人： Hans-Dieter Dell , Bernhard Pelster , Reinhold Kraus , Detlef Schierstedt
IPC分类号： C07D213/80 , A61K9/00 , A61K9/08 , A61K9/10 , A61K9/107 , A61K31/195 , A61K31/245 , A61K31/44 , A61K31/455 , A61K47/14 , A61K47/44 , A61K31/19 , A61K31/24
CPC分类号： A61K47/44 , A61K31/195 , A61K31/455 , A61K47/14 , A61K9/0019
摘要： The invention relates to depot formulations containing, as an active antiinflammatory and/or analgesic agent a compound of Formula I, infra together with a suspension medium. Typical suspension agents are glycerides and/or esters of mono- or poly-hydric alcohols as well as selected ethers, alcohols and amides.

8. 发明授权

US4784997A 1-H-pyrido-[3,2-b][1,4]-thiazine 失效
标题翻译： 1-H-吡啶并[3,2-b] [1,4] - 噻嗪
公开(公告)号：US4784997A
公开(公告)日：1988-11-15
申请号：US942468
申请日：1986-12-16
申请人： Alexander Klausener , Gerd Fengler , Hans-Josef Buysch , Bernhard Pelster
发明人： Alexander Klausener , Gerd Fengler , Hans-Josef Buysch , Bernhard Pelster
IPC分类号： A61K31/54 , A61P9/10 , A61P29/00 , A61P37/08 , C07D513/04 , C07D513/12
CPC分类号： C07D513/04
摘要： 1-H-pyrido-[3,2-b][1,4]-thiazines of the formula ##STR1## are prepared by the reaction of 2-halogenocarbonyl compounds an 2-amino-3-pyridinethiols. These compounds are useful as medicaments especially as inhibitors of lipoxygenase.
摘要翻译：通过2-卤代羰基化合物与2-氨基-3-吡啶硫醇的反应来制备式“IMAGE”的1-H-吡啶并[3,2-b] [1,4] - 噻嗪。这些化合物可用作特别是脂氧合酶抑制剂的药物。

9. 发明授权

US4771062A Diaryl sulphide derivatives 失效
标题翻译：二芳基硫化物衍生物
公开(公告)号：US4771062A
公开(公告)日：1988-09-13
申请号：US18091
申请日：1987-02-20
申请人： Siegfried Raddatz , Hans Plumpe , Romanis Fruchtmann , Christian Kohlsdorfer , Bernhard Pelster
发明人： Siegfried Raddatz , Hans Plumpe , Romanis Fruchtmann , Christian Kohlsdorfer , Bernhard Pelster
IPC分类号： C07D277/18 , C07D277/38 , C07D277/42 , C07D279/06 , A61K31/425
CPC分类号： C07D279/06 , C07D277/18 , C07D277/42
摘要： A diaryl sulphide derivative of the formula ##STR1## in which R.sup.1 represents a thiazolamino radical of the formulae ##STR2## wherein R.sup.5 represents hydrogen, alkyl, aralkyl or acyl,R.sup.6 and R.sup.6 ' are identical or different and represent hydrogen, alkyl, aralkyl or aryl,R.sup.7 represents alkyl, cycloalkyl, aralkyl, acyl or aryl andn represents the number 1 or 2,R.sup.2 and R.sup.3 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, aryl, aralkyl, aryloxy, aralkoxy, aralkylthio, acyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, nitro, cyano or halogen, or represent a group of the formula ##STR3## wherein R.sup.8 and R.sup.9 are identical or different and represent hydrogen, alkyl, aryl, aralkyl, acyl, trifluoroacetyl, alkylsulphonyl, arylsulphonyl, trifluoromethylphenylsulphonyl or tolylsulphonyl andR.sup.4 has one of the abovementioned meanings or R.sup.1, or represents hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, aryl, aralkyl, aryloxy, aralkoxy, aralkylthio, acyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, nitro, cyano or halogen, or represents a group of the formula ##STR4## wherein R.sup.8 and R.sup.9 have the abovementioned meanings, and salts thereof. Such diaryl sulphide derivatives being useful as active compounds in the treatment and prevention of diseases of the respiratory tract and cardiovascular diseases.
摘要翻译：式（I）的二芳基硫化物衍生物，其中R 1表示下式的噻唑烷基：其中R 5表示氢，烷基，芳烷基或酰基，R 6和R 6'相同或不同代表氢，烷基，芳烷基或芳基，R7代表烷基，环烷基，芳烷基，酰基或芳基，n代表数字1或2，R2和R3相同或不同，代表氢，烷基，烯基，环烷基，烷氧基，烷硫基，卤代烷基，卤代烷氧基，卤代烷硫基，芳基，芳烷基，芳氧基，芳烷氧基，芳烷硫基，酰基，羧基，烷氧基羰基，羧基烷基，烷氧基羰基烷基，硝基，氰基或卤素，或表示下式的基团：其中R8和R9相同或代表氢，烷基，芳基，芳烷基，酰基，三氟乙酰基，烷基磺酰基，芳基磺酰基，三氟甲基苯磺酰基或甲苯磺酰基，R4具有上述含义之一或R 1，或表示氢，烷基，烯基，C 烷氧基，烷硫基，卤代烷基，卤代烷氧基，卤代烷硫基，芳基，芳烷基，芳氧基，芳烷氧基，芳烷硫基，酰基，羧基，烷氧基羰基，羧基烷基，烷氧基羰基烷基，硝基，氰基或卤素，或表示下式的基团其中R8 和R9具有上述含义及其盐。这种二芳基硫化物衍生物可用作活性化合物，用于治疗和预防呼吸道疾病和心血管疾病。

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