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1. 发明授权

US4603204A Theophylline derivatives 失效
标题翻译：茶碱衍生物
公开(公告)号：US4603204A
公开(公告)日：1986-07-29
申请号：US474230
申请日：1983-03-11
申请人： Kurt Thiele , Felix Geissmann , Ludwig Zirngibl , Ulrich Jahn
发明人： Kurt Thiele , Felix Geissmann , Ludwig Zirngibl , Ulrich Jahn
IPC分类号： A61K31/52 , A61K31/522 , A61P25/02 , A61P29/00 , A61P37/08 , A61P43/00 , C07D295/22 , C07D307/02 , C07D473/08
CPC分类号： C07D473/08
摘要： New derivatives of theophylline having the formula ##STR1## in which R denotes hydrogen or OH, n the numbers 0 or 1, X either >CH-- or >N--, Y either --O-- or --CO-- and R a five membered or six membered aryl ring or hetero-aryl ring, that is substituted in given cases with halogen, short chain alkyl groups, alkoxy groups or halogen-alkyl, and exhibit in addition to other properties, histamine-, serotinine- bradykynine- antagonistic, anti-anaphylactic and -adrenergic stimulating effects.
摘要翻译：具有式（I）的茶碱的新衍生物，其中R表示氢或OH，n为数字0或1，X或> CH-或> N-，Y为-O-或-CO-，R a 在给定的情况下被卤素，短链烷基，烷氧基或卤素 - 烷基取代的五元或六元芳基环或杂芳基环，并且除了其它性质外，还表现出组胺，血清素 - 卡那霉素拮抗剂，抗过敏和肾上腺素能刺激作用。

2. 发明授权

US4668786A P-fluorobenzoyl-piperidino alkyl theophylline derivatives 失效
标题翻译：对氟苯甲酰 - 哌啶子基烷基茶碱衍生物
公开(公告)号：US4668786A
公开(公告)日：1987-05-26
申请号：US813439
申请日：1985-12-26
申请人： Kurt Thiele , Felix Geissmann , Ludwig Zirngibl , Ulrich Jahn
发明人： Kurt Thiele , Felix Geissmann , Ludwig Zirngibl , Ulrich Jahn
IPC分类号： A61K31/52 , A61K31/522 , A61P25/02 , A61P29/00 , A61P37/08 , A61P43/00 , C07D295/22 , C07D307/02 , C07D473/08
CPC分类号： C07D473/08
摘要： New derivatives of theophylline having the formula ##STR1## wherein R is hydrogen or a hydroxy group, and n is an integer of 0.ltoreq.n.ltoreq.3 and/or the pharmaceutically acceptable, acid addition salts thereof, exhibit in addition to other properties, histamine-serotinine- bradykynine- antagonistic, anti-anaphylactic and .beta.-adrenergic stimulating effects.

3. 发明授权

US4526898A Antihypertensive 4-(2-imidazolin-2-yl-amino)-2-methyl-indazole 失效
标题翻译：抗高血压4-（2-咪唑啉-2-基 - 氨基）-2-甲基 - 吲唑
公开(公告)号：US4526898A
公开(公告)日：1985-07-02
申请号：US530145
申请日：1983-09-07
申请人： Istvan Molnar , Kurt Thiele , Felix Geissmann , Ulrich Jahn
发明人： Istvan Molnar , Kurt Thiele , Felix Geissmann , Ulrich Jahn
IPC分类号： C07D403/12 , A61K31/415
CPC分类号： C07D403/12
摘要： 4-(2-Imidazolin-2-yl-amino)-2-methyl-indazole is a highly selective and effective .alpha..sub.2 -antagonist, .alpha..sub.1 -partial agonist and .alpha..sub.1s -agonist and displays anti-hypertensive activity and antagonistic activity on adrenaline and noradrenaline. It is useful as an .alpha.-adrenoceptor influencing and as an anti-hypertensively active drug.
摘要翻译： 4-（2-咪唑啉-2-基 - 氨基）-2-甲基 - 吲唑是一种高选择性和有效的α2拮抗剂，α1-部分激动剂和α1s激动剂，并且对抗高血压活性和拮抗活性肾上腺素和去甲肾上腺素。作为α肾上腺素能受体影响作为抗高血压活性药物是有用的。

4. 发明授权

US4436913A 1H- and 2H- indazole derivatives 失效
标题翻译： 1H-和2H-吲唑衍生物
公开(公告)号：US4436913A
公开(公告)日：1984-03-13
申请号：US375116
申请日：1982-04-28
申请人： Istvan Molnar , Kurt Thiele , Felix Geissmann , Ulrich Jahn
发明人： Istvan Molnar , Kurt Thiele , Felix Geissmann , Ulrich Jahn
IPC分类号： C07D231/56 , C07D231/16 , C07D403/00 , C07D403/12
CPC分类号： C07D403/12
摘要： 1H- and 2H- indazole derivatives and pharmaceuticals containing these blood-pressure lowering 1H- and 2H- indazole derivatives of the formula ##STR1## and their acid addition salts, wherein R1 may be in position 1 or position 2 on the nitrogen atoms in formula I. The groups R1, R2 and R3 represent hydrogen or the usual lower molecular groups. The R group is a 2-imidazolinylamino group or a 3,4,5,6-tetryhydropyrimidinylamino group, wherein these groups may also be present in their tautomeric forms. These groups may also be in an aryl group in the R1 group, in which case the R group may also be a halogen atom. R may only represent one of the heterocyclic secondary or tertiary amino groups in the 4 or 7 position for the 1H- indazole derivatives when the R1 group is simultaneously an aryl or an aralkyl group.
摘要翻译： PCT No.PCT / EP80 / 00094 Sec。 371日期1982年4月28日 102（e）日期1982年4月28日PCT提交1980年9月5日PCT公布。出版物WO82 / 0082400 日期：1982年3月18日1 H-和2H-吲唑衍生物和含有这些降血压的1H-和2H-吲唑衍生物及其酸加成盐的药物，其中R1可位于1位或位置2在式I中的氮原子上。基团R 1，R 2和R 3表示氢或通常的较低分子基团。 R基团是2-咪唑啉基氨基或3,4,5,6-四氢嘧啶基氨基，其中这些基团也可以它们的互变异构形式存在。这些基团也可以是R 1基团中的芳基，在这种情况下，R基团也可以是卤素原子。当R1基团同时为芳基或芳烷基时，R可以仅代表1H-吲唑衍生物的4或7位杂环仲或叔氨基之一。

5. 发明授权

US4204998A N-Amino indole derivatives having pharmacological activity 失效
标题翻译：具有药理活性的N-氨基吲哚衍生物
公开(公告)号：US4204998A
公开(公告)日：1980-05-27
申请号：US903128
申请日：1978-05-05
申请人： Franz Schatz , Christian Stammbach , Kurt Thiele , Theodor W. Wagner-Jauregg , Ludwig Zirngibl , Johanna Fischer , Ulrich Jahn
发明人： Franz Schatz , Christian Stammbach , Kurt Thiele , Theodor W. Wagner-Jauregg , Ludwig Zirngibl , Johanna Fischer , Ulrich Jahn
IPC分类号： C07D209/08 , C07D209/10 , C07D209/12 , C07D209/44 , C07D231/56 , C07D235/22 , C07D249/18
CPC分类号： C07D249/18 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/44 , C07D231/56 , C07D235/22
摘要： Novel hydrazines are disclosed in which one of the nitrogen atoms forms a ring member of the five membered ring of a [4.3.0] heterobicyclic compound which may be substituted elsewhere in the ring system. Characteristic ring systems described include indole and benztriazole ring systems. The compounds possess anti-depressant properties as well as anti-microbial, in particular fungistatic and bacteriostatic, properties.
摘要翻译：公开了新的肼，其中一个氮原子形成[4.3.0]杂双环化合物的五元环的环成员，其可以在环系中的别处取代。描述的特征环体系包括吲哚和苯并三唑环体系。该化合物具有抗抑郁特性以及抗微生物，特别是抑菌和抑菌性质。

6. 发明授权

US4554356A Method for production of imidazolyl vinyl ethers 失效
标题翻译：咪唑基乙烯基醚的制备方法
公开(公告)号：US4554356A
公开(公告)日：1985-11-19
申请号：US692324
申请日：1985-01-16
申请人： Ludwig Zirngibl , Kurt Thiele
发明人： Ludwig Zirngibl , Kurt Thiele
IPC分类号： C07D233/00 , B01J31/02 , C07B61/00 , C07D233/60 , C07D233/68 , C07D233/70 , C07D233/91 , C07D333/00 , C07D401/00 , C07D409/00 , C07D521/00
CPC分类号： C07D231/12 , C07D249/08
摘要： A process for the manufacture of imidazolylvinyl ethers of the formula ##STR1## wherein Im represents the substituted or unsubstituted 1-H-imidazol-1-yl group and An, R and Y are defined hereinbelow by condensation of a corresponding ketone of the formulaAr--CO--CHR--Im (II)with the splitting-off of a Z group, with a condensable substance of the formulaZ--Y (III)in the aqueous solution of a strong inorganic base, preferably in concentrated aqueous soda lye. The reaction may also be carried out in the presence of a second liquid organic phase, preferably benzene or toluene, especially in the presence of a phase transfer catalyst in this case. Through careful crystallization of the product manufactured according to this method, it is possible to manufacture approximately pure E-isomers of the imidazolylvinyl ether of formula (I), without the requirement of chromatographic separation.
摘要翻译： PCT No.PCT / EP82 / 00010 Sec。 371日期1982年5月24日 102（e）日期1982年5月24日PCT提交1982年1月21日PCT公布。出版物WO82 / 02552 日本1982年8月5日。一种制备式（I）的咪唑基乙烯基醚的方法，其中Im表示取代或未取代的1-H-咪唑-1-基，An，R和Y定义如下通过将式Ar-CO-CHR-Im（II）的相应的酮与Z基团的分离与式ZY（III）的可冷凝物质在强无机碱的水溶液中缩合，优选在浓缩的苏打碱液中。反应也可以在第二液体有机相存在下进行，优选苯或甲苯，特别是在这种情况下在相转移催化剂存在下。通过根据该方法制造的产品的仔细结晶，可以制备式（I）的咪唑基乙烯基醚的近似纯的E-异构体，而不需要色谱分离。

7. 发明授权

US4330545A Heterocyclic imidazolyl vinyl ethers and use of same as fungicides or bactericides 失效
标题翻译：杂环咪唑基乙烯基醚，用作杀真菌剂或杀菌剂
公开(公告)号：US4330545A
公开(公告)日：1982-05-18
申请号：US150964
申请日：1980-05-19
申请人： Ludwig Zirngibl , Johanna Fischer , Kurt Thiele
发明人： Ludwig Zirngibl , Johanna Fischer , Kurt Thiele
IPC分类号： A01N43/50 , C07C43/225 , A01N43/54 , A01N43/56 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12
CPC分类号： C07C43/225 , A01N43/50
摘要： Aryl-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar in the formula represents a substituted or unsubstituted aryl or heterocyclic radical; R represents hydrogen or a C.sub.1 -C.sub.12 alkyl or cycloalkyl (saturated or unsaturated) or Ar as above; Im represents a 1-H-imidazol-1-yl group (unsubstituted or substituted); and Y represents a saturated or unsaturated C.sub.1 -C.sub.12 alkyl or a group --Z--Ar in which Ar has the above meaning and --Z-- is a saturated or unsaturated C.sub.1 -C.sub.12 alkylene wherein each of the alkyl and the alkylene may have a carbon chain once or twice interrupted by or, in the case of the alkylene, terminated on its Ar-end by oxy, thio, sulfinyl or sulfonyl bridges, always with the proviso that at least one of Ar and Y is a heterocyclic radical. These compounds are wide-spectrum fungicides and bactericides, and the preferred compounds among them are hydrophilic.
摘要翻译：公开了芳基 - 咪唑-1-基乙烯基醚及其酸加成盐，其中咪唑基乙烯基醚具有下式：下式中的Ar表示取代或未取代的芳基或杂环基; R代表氢或C1-C12烷基或环烷基（饱和或不饱和）或如上所述的Ar; Im表示1-H-咪唑-1-基（未取代或取代的）; 并且Y表示饱和或不饱和的C 1 -C 12烷基或基团-Z-Ar，其中Ar具有上述含义，-Z-是饱和或不饱和的C 1 -C 12亚烷基，其中烷基和亚烷基中的每一个可以具有碳链中断一次或两次，或者在亚烷基的情况下，通过氧基，硫基，亚磺酰基或磺酰基桥接在其Ar末端上，条件是Ar和Y中的至少一个是杂环基。这些化合物是广谱杀菌剂和杀菌剂，其中优选的化合物是亲水的。

8. 发明授权

US4210657A Aryl imidazolyl vinyl ethers and processes for using same 失效
标题翻译：芳基咪唑基乙烯基醚及其使用方法
公开(公告)号：US4210657A
公开(公告)日：1980-07-01
申请号：US970330
申请日：1978-12-18
申请人： Ludwig Zirngibl , Johanna Fischer , Kurt Thiele
发明人： Ludwig Zirngibl , Johanna Fischer , Kurt Thiele
IPC分类号： A01N43/50 , A61K31/415 , A61P31/04 , C07C43/225 , C07D233/60 , C07D233/68 , C07D233/91 , C07D521/00
CPC分类号： C07D231/12 , A01N43/50 , C07C43/225 , C07D233/56 , C07D249/08
摘要： Aryl-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar in the formula represents a substituted or unsubstituted aryl or heterocyclic radical; R represents hydrogen or a C.sub.1 -C.sub.12 alkyl or cycloalkyl (saturated or unsaturated) or Ar as above; Im represents a 1-H-imidazol-1-yl group (unsubstituted or substituted); and Y represents a saturated or unsaturated, acyclic or cyclic C.sub.1 -C.sub.12 alkyl, or aryl or aralkyl, or an alkyl or alkylene residue directly bound to the ether oxygen and having a chain once or twice interrupted by --O--, --S--, --SO-- or --SO.sub.2 -- bridges. These compounds are effective wide spectrum fungicides and bactericides.
摘要翻译：公开了芳基 - 咪唑-1-基乙烯基醚及其酸加成盐，其中咪唑基乙烯基醚具有下式：式中的Ar表示取代或未取代的芳基或杂环基; R代表氢或C1-C12烷基或环烷基（饱和或不饱和）或如上所述的Ar; Im表示1-H-咪唑-1-基（未取代或取代的）; 并且Y表示饱和或不饱和的无环或环状C 1 -C 12烷基或芳基或芳烷基，或直接键合到醚氧上并具有一个或两个被-O - ， - S - 间隔的链的烷基或亚烷基， -SO-或-SO 2 - 桥。这些化合物是有效的广谱杀菌剂和杀菌剂。

9. 发明授权

US4131608A Thioethers 失效
标题翻译：硫醚
公开(公告)号：US4131608A
公开(公告)日：1978-12-26
申请号：US795224
申请日：1977-05-09
申请人： Ludwig Zirngibl , Johanna Fischer , Kurt Thiele
发明人： Ludwig Zirngibl , Johanna Fischer , Kurt Thiele
IPC分类号： C07D413/12 , A61K31/415 , A61P31/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D521/00 , C07D263/58
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： This invention relates to novel thioethers as well as to the addition salts thereof with inorganic or organic acids. The novel compounds and their addition salts have valuable anti-mycotic and fungicidal properties. Further the invention relates to a process for preparing the novel compounds and their addition salts, and to anti-mycotic and fungicidal compositions containing the novel thioethers, or addition salts thereof, as the active constituent.
摘要翻译：本发明涉及新型硫醚以及其与无机或有机酸的加成盐。新化合物及其加成盐具有有价值的抗真菌和杀真菌性能。此外，本发明涉及一种制备新化合物及其加成盐的方法，以及含有新型硫醚或其加成盐作为活性成分的抗霉菌和杀真菌组合物。

10. 发明授权

US4210656A Imidazolyl vinyl ethers and process for preparing same 失效
标题翻译：咪唑基乙烯基醚及其制备方法
公开(公告)号：US4210656A
公开(公告)日：1980-07-01
申请号：US970312
申请日：1978-12-18
申请人： Ludwig Zirngibl , Johanna Fischer , Kurt Thiele
发明人： Ludwig Zirngibl , Johanna Fischer , Kurt Thiele
IPC分类号： A01N43/50 , A61K31/415 , A61P31/04 , C07D233/60 , C07D233/92 , C07D521/00
CPC分类号： C07D231/12 , A01N43/50 , C07D233/56 , C07D249/08
摘要： .alpha.-Aryl-.beta.-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar represents a substituted or unsubstituted aryl group, R an alkyl, aryl or aralkyl group, X an oxygen atom, a sulfur atom, a sulfinyl or a sulfonyl group and R1 a lower alkyl group or a nitro group. These compounds are effective wide spectrum fungicides and bactericides. To prepare these vinyl ethers, a corresponding 1-arylacylimidazole is o-alkylated in presence of NaH with a corresponding .alpha.-halogen ether, .alpha.-halogen thioether, .alpha.-halogen sulfinyl compound or a corresponding .alpha.-halogen sulfonyl compound.
摘要翻译：公开了α-氨基-β-咪唑-1-基乙烯基醚及其酸加成盐，其中咪唑基乙烯基醚具有下式：Ar表示取代或未取代的芳基，R是烷基，芳基或芳烷基 X为氧原子，硫原子，亚磺酰基或磺酰基，R 1为低级烷基或硝基。这些化合物是有效的广谱杀菌剂和杀菌剂。为了制备这些乙烯基醚，相应的1-芳基酰基咪唑在NaH存在下与相应的α-卤代醚，α-卤代硫醚，α-卤代亚磺酰基化合物或相应的α-卤代磺酰化合物进行邻烷基化。

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