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1. 发明授权

US4374990A Cyclic diamine derivatives 失效
标题翻译：环二胺衍生物
公开(公告)号：US4374990A
公开(公告)日：1983-02-22
申请号：US88338
申请日：1979-10-26
申请人： Rolf-Ortwin Weber , Alfons Soder , Istvan Boksay
发明人： Rolf-Ortwin Weber , Alfons Soder , Istvan Boksay
IPC分类号： C07D209/42 , A61K31/495 , A61K31/55 , A61P9/08 , A61P25/04 , A61P25/18 , A61P25/24 , A61P25/26 , A61P29/00 , A61P31/04 , C07D209/50 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/04 , C07D215/12 , C07D307/54 , C07D307/68 , C07D307/81 , C07D307/82 , C07D307/85 , C07D309/08 , C07D309/28 , C07D311/04 , C07D311/22 , C07D311/58 , C07D333/20 , C07D333/38 , C07D403/06 , C07D405/06 , C07D405/12 , C07D407/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D405/02
CPC分类号： C07D405/06 , A61K31/495 , C07D409/14 , Y10S514/906
摘要： A compound having the general formula or an acid addition salt thereof ##STR1## in which formula R.sub.1 is selected from the group consisting of(A) an at least mononuclear heterocyclic group having 4 to 10 carbon atoms in the ring system bound to the group ##STR2## through a carbon atom and containing at least one oxygen, nitrogen or sulphur atom,(B) substitution products of (A) containing at least one substituent selected from the group consisting of halogen, trifluoromethyl, hydroxy, alkoxy of 1 to 3 carbon atoms, unsubstituted amino, amino substituted by up to two alkyl groups each having 1 to 3 carbon atoms and alkyl groups having 1 to 6 carbon atoms,X is oxygen, sulphur or an NH-group,Y is an alkylene group having 1 to 3 carbon atoms in the chain, or an alkylene group having 1 to 3 carbon atoms in the chain substituted by (a) up to 3 alkyl groups each having up to 3 carbon atoms and a total of not more than 8 carbon atoms, or (b) substituted by one or two phenyl groups,R.sub.2 is selected from the group consisting of(c) an at least mononuclear carbocyclic or heterocyclic group having 4 to 10 carbon atoms in the ring system, containing but one heteroatom in a ring,(D) substitution products of (C) containing at least one substituent selected from the group consisting of nitro, halogen, trifluoromethyl, alkyl having 1 to 6 carbon atoms, hydroxy, alkoxy having 1 to 3 carbon atoms, unsubstituted amino groups and amino groups substituted by up to two alkyl groups each having 1 to 3 carbon atoms,R.sub.3 is hydrogen or up to two substituents selected from alkyl groups having up to 2 carbon atoms and phenyl groups. n is 2 or 3; a process for its preparation and a pharmaceutical composition containing said compound (I).
摘要翻译：具有通式的化合物或其酸加成盐，其中式R 1选自（A）环系中具有4至10个碳原子的至少单核杂环基，其结合到通过碳原子并含有至少一个氧，氮或硫原子的基团，（B）含有至少一个选自卤素，三氟甲基，羟基，烷氧基的取代基的（A）的取代产物1 至3个碳原子，未取代的氨基，被至多两个各自具有1至3个碳原子的烷基和具有1至6个碳原子的烷基取代的氨基，X是氧，硫或NH-基，Y是具有链中有1至3个碳原子，或链中具有1至3个碳原子的亚烷基被（a）最多3个具有多达3个碳原子的烷基和总共不超过8个碳原子的烷基取代，或（b）被一个或两个苯基取代，R 2是se 由（c）环系中具有4至10个碳原子的至少单核碳环或杂环基团组成的基团，其在环中含有一个杂原子;（D）含有至少一个取代基的（C）取代产物选自硝基，卤素，三氟甲基，具有1至6个碳原子的烷基，羟基，具有1至3个碳原子的烷氧基，未取代的氨基和被至多两个各自具有1至3个碳原子的烷基取代的氨基。，R 3是氢或至多两个选自具有至多2个碳原子的烷基和苯基的取代基。

2. 发明授权

US4312861A Pharmaceutical compositions containing N-alkyl-N-(nuclearly-substituted) benzylamines having vasotonia-regulating activity 失效
标题翻译：含有N-烷基-N-（核取代的）苄胺的药物组合物具有调节血管的活性
公开(公告)号：US4312861A
公开(公告)日：1982-01-26
申请号：US806272
申请日：1977-06-13
申请人： Istvan Boksay , Alfons Soder , Volkher Bollmann , Rolf-Ortwin Weber
发明人： Istvan Boksay , Alfons Soder , Volkher Bollmann , Rolf-Ortwin Weber
IPC分类号： A61K31/13 , A61K31/135 , A61K31/66 , A61P9/00 , A61P9/06 , A61P9/08 , C07C67/00 , C07C209/00 , C07C209/08 , C07C209/26 , C07C209/50 , C07C211/27 , C07C211/29 , C07C213/00 , C07C213/02 , C07C215/08 , C07C217/08 , C07C301/00 , C07C307/02 , C07F9/32 , C07F9/53 , A01N33/02 , A01N57/00
CPC分类号： C07F9/5304
摘要： Aralkylamines of the formula:R.sup.1 --CH.sub.2 --N(R.sup.3)--R.sup.2whereinR.sup.1 is a phenyl substituted by one of:(I) alkyls,(II) halo and(III) nitro;R.sup.2 is(IV) alkyl having from 4 to 10 carbon atoms, four of which are in one chain,(V) alkyl interrupted by an oxygen atom, i.e. an alkoxyalkyl or ether radical, or(VI) hydroxyalkyl wherein the alkyl is either (IV) or (V) and the hydroxy is the sole substituent;R.sup.3 is a hydrogen atom, alkyl having from 1 to 4 carbon atoms or such alkyl substituted by a dialkylphosphinyl group;a physiologically-compatible acid-addition salt thereof and a pharmaceutical composition containing such compound(s) as active ingredient(s) are valuable in view of the physiological activity, e.g. vasotonic, capillary sealing and antiarrhythmic, of the aralkylamines and their physiologically-compatible acid-addition salts.
摘要翻译：下式的芳烷基胺：R1-CH2-N（R3）-R2其中R1是被下列之一取代的苯基：（I）烷基，（Ⅱ）卤素和（Ⅲ）硝基; R2是具有4至10个碳原子的（IV）烷基，其中4个是一个链，（V）被氧原子间隔的烷基，即烷氧基烷基或醚基，或（Ⅵ）羟烷基，其中烷基是（ IV）或（V），羟基是唯一的取代基; R3是氢原子，具有1至4个碳原子的烷基或被二烷基氧膦基取代的烷基; 考虑到生理活性，其生理学相容的酸加成盐和含有作为活性成分的化合物的药物组合物是有价值的。血管紧张素，毛细血管密封和抗心律不齐的芳烷基胺及其生理相容的酸加成盐。

3. 发明授权

US4152440A Novel derivatives of imidazole, and pharmaceutical compositions containing them 失效
标题翻译：咪唑的新型衍生物和含有它们的药物组合物
公开(公告)号：US4152440A
公开(公告)日：1979-05-01
申请号：US741418
申请日：1976-11-12
申请人： Ulrich Gebert , Josef Musil , Rolf-Ortwin Weber
发明人： Ulrich Gebert , Josef Musil , Rolf-Ortwin Weber
IPC分类号： C07D401/14 , A61K31/41 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P7/10 , A61P13/02 , A61P15/00 , A61P19/06 , A61P25/04 , A61P29/00 , C07D403/04 , C07D403/06 , C07D409/14 , C07D257/04
CPC分类号： C07D403/04 , A61K31/41 , A61K31/415 , C07D403/06
摘要： A compound of one of formulae (I) and (II) (of formula sheet) whereinR.sup.1 represents a radical selected from the group consisting of hydrogen alkyl containing up to 6 carbon atoms and being unsubstituted or substituted by at least one of the groups alkoxy and phenylalkoxy containing up to 4 carbon atoms in the alkoxy moiety; aryl or aralkyl each containing from 1 to 4 carbon atoms in the alkyl moiety and being unsubstituted or substituted by at least one substituent selected from the group consisting of alkyl, alkoxy and haloalkyl containing up to 4 carbon atoms, halogen and nitro; a 5- or 6-membered heteroaromatic ring containing up to 2 hetero atoms chosen from O,N and S, at most one of which is different from nitrogen; an alkyl group containing from 1 to 4 carbon atoms substituted by such a heteroaromatic ring;R.sup.2 and R.sup.3, which are the same or different, each represents a hydrogen atom or, alkyl containing up to 4 carbon atoms and being unsubstituted or substituted by at least one substituent selected from the group consisting of alkyl, alkoxy and haloalkyl containing up to 4 carbon atoms, halogen and nitro; taken together R.sup.2 and R.sup.3 alternatively represent a --CH.dbd.CH--CH.dbd.CH-- group which is unsubstituted or substituted by a substituent selected from the group consisting of alkyl, alkoxy and haloalkyl, each containing up to 4 carbon atoms, halogen and nitro;R.sup.4 is selected from the group consisting of hydrogen alkyl, aryl and aralkyl containing up to 4 carbon atoms in each alkyl moiety; andA represents a single bond or alkylene containing from 1 to 6 carbon atoms; with the proviso that R.sup.1 is other than a hydrogen atom or methyl group when A represents a single bond and R.sup.2 and R.sup.3 taken together represent an unsubstituted --CH.dbd.CH--CH.dbd.CH-- group; physiologically acceptable salts thereof, a synthesis therefor and a pharmaceutical composition containing it.
摘要翻译：式（I）和（II）之一（式）的化合物，其中R 1表示选自含有至多6个碳原子的烷基的基团，并且是未被取代的或被至少一个烷氧基取代的基团烷氧基和在烷氧基部分含有至多4个碳原子的苯基烷氧基; 在烷基部分中各自含有1至4个碳原子的芳基或芳烷基，未被取代或被至少一个选自烷基，烷氧基和含有最多4个碳原子的卤代烷基取代的取代基，卤素和硝基; 含有至多2个选自O，N和S的杂原子的5或6元杂芳环，其中最多一个不同于氮; 由这样的杂芳环取代的含有1至4个碳原子的烷基; R 2和R 3相同或不同，各自表示氢原子或含有至多4个碳原子的烷基，未被取代或被至少一个选自烷基，烷氧基和含有至多4个碳原子，卤素和硝基; 一起取代R2和R3代表-CH = CH-CH = CH-基团，其未被取代或被选自烷基，烷氧基和卤代烷基的取代基取代，每个含有最多4个碳原子的卤素和硝基; R 4选自在每个烷基部分含有至多4个碳原子的烷基，芳基和芳烷基; A表示单键或含有1至6个碳原子的亚烷基; 条件是当A表示单键时，R1不是氢原子或甲基，R2和R3一起代表未取代的-CH = CH-CH = CH-基团; 其生理上可接受的盐，其合成物和含有它的药物组合物。

4. 发明授权

US4221793A N,N'-Disubstituted piperazine derivative 失效
标题翻译： N，N'-二取代哌嗪衍生物
公开(公告)号：US4221793A
公开(公告)日：1980-09-09
申请号：US972068
申请日：1978-12-21
申请人： Rolf-Ortwin Weber , Klaus Perrey , Wolfrad von Rechenberg
发明人： Rolf-Ortwin Weber , Klaus Perrey , Wolfrad von Rechenberg
IPC分类号： A61K31/34 , A61K31/343 , A61P25/24 , A61P25/26 , C07D307/85 , A61K31/495 , C07D405/06
CPC分类号： C07D307/85
摘要： A compound of the formula ##STR1## or its acid addition salt with a physiologically compatible acid, a process for its preparation by a reaction selected from the group consisting of(a) reacting N-benzyl-piperazine and 5-methoxycumarilic acid(a1) at an elevated temperature in the absence of a condensation agent,(a2) at a temperature of at least 15.degree. C. in the presence of a condensation agent;(b) reacting N-benzyl-piperazine with an activated derivative of 5-methoxy-cumarilic acid;(c) N-(5-methoxycumaroyl)-piperazine with a benzyl compound selected from the group consisting of benzyl halide, benzylalkyl sulfonate and benzyl-aryl sulfonate and a pharmaceutical composition containing said compounds.
摘要翻译：式（Ia）化合物或其酸加成盐与生理上相容的酸，其制备方法为选自（a）N-苄基哌嗪与5-甲氧基肉桂酸（a1）的反应，在不存在缩合剂的情况下在升高的温度下，（a2）在冷凝剂存在下在至少15℃的温度下进行; （b）使N-苄基 - 哌嗪与5-甲氧基 - 间歇二酸的活化衍生物反应; （c）N-（5-甲氧基枯烯酰基） - 哌嗪与选自苄基卤，苄基烷基磺酸酯和苄基 - 芳基磺酸酯的苄基化合物和含有所述化合物的药物组合物。

5. 发明授权

US4213986A Novel derivatives of imidazole and pharmaceutical compositions containing them and method of use 失效
标题翻译：咪唑的新型衍生物和含有它们的药物组合物和使用方法
公开(公告)号：US4213986A
公开(公告)日：1980-07-22
申请号：US949018
申请日：1978-10-06
申请人： Ulrich Gebert , Josef Musil , Rolf-Ortwin Weber
发明人： Ulrich Gebert , Josef Musil , Rolf-Ortwin Weber
IPC分类号： A61K31/415 , C07D401/14 , C07D409/14 , A61K31/44 , A61K31/495 , A61K31/505
CPC分类号： C07D401/14 , A61K31/415 , C07D409/14
摘要： A physiologically-acceptable compound of one of the formulae ##STR1## wherein R.sup.1 is a member selected from the group consisting of (a) a 6-membered heteroaromatic ring with up to two ring hetero atoms selected from the group consisting of O, N and S, at most one of which is different from nitrogen, and (b) an alkyl group containing from 1 to 4 carbon atoms and substituted by such a heteroaromatic ring;each of R.sup.2 and R.sup.3 is, independently, a hydrogen atom, alkyl having up to 4 carbon atoms, substituted or unsubstituted aryl or, together with the other of R.sup.2 and R.sup.3, unsubstituted --CH.dbd.CH--CH.dbd.CH-- or --CH.dbd.CH--CH.dbd.CH-- substituted by a member selected from the group consisting of alkyl having up to 4 carbon atoms, alkoxy having up to 4 carbon atoms, haloalkyl having up to 4 carbon atoms, halo and nitro;R.sup.4 is a member selected from the group consisting of a hydrogen atom, alkyl having up to 4 carbon atoms, aryl and aralkyl having up to 4 carbon atoms in the alkyl moiety; andA is a single bond or alkylene having from 1 to 6 carbon atoms;any substituent of substituted aryl being a member selected from the group consisting of alkyl having up to 4 carbon atoms, alkoxy having up to 4 carbon atoms, haloalkyl having up to 4 carbon atoms, halo or nitro;or a physiologically-acceptable salt thereof and a composition containing said compounds.
摘要翻译：其中R 1是选自（a）选自具有至多2个环杂原子的6元杂芳环的成员的成员的生理学上可接受的化合物从由O，N和S组成的组中，最多一个不同于氮，和（b）含有1至4个碳原子并被这样的杂芳环取代的烷基; R 2和R 3各自独立地为氢原子，具有至多4个碳原子的烷基，取代或未取代的芳基，或者与另一个R 2和R 3一起未取代的-CH = CH-CH = CH-或-CH = CH-CH = CH-被选自具有至多4个碳原子的烷基，具有至多4个碳原子的烷氧基，至多4个碳原子的卤代烷基，卤素和硝基组成的组中的一个取代基; R4是选自氢原子，具有至多4个碳原子的烷基，芳基和烷基中具有至多4个碳原子的芳烷基的成员; 且A为单键或具有1至6个碳原子的亚烷基; 取代芳基的任何取代基是选自具有至多4个碳原子的烷基，具有至多4个碳原子的烷氧基，具有至多4个碳原子的卤代烷基，卤素或硝基的成员; 或其生理上可接受的盐和含有所述化合物的组合物。

6. 发明授权

US4115569A Cyclic diamine derivatives 失效
标题翻译：环二胺衍生物
公开(公告)号：US4115569A
公开(公告)日：1978-09-19
申请号：US606488
申请日：1975-08-21
申请人： Rolf-Ortwin Weber , Alfons Soder , Istvan Boksay
发明人： Rolf-Ortwin Weber , Alfons Soder , Istvan Boksay
IPC分类号： A61K31/495 , C07D405/06 , C07D409/14 , C07D295/10
CPC分类号： C07D409/14 , A61K31/495 , C07D405/06
摘要： A compound having the general formula or an acid addition salt thereof ##STR1## in which formula R.sub.1 is selected from the group consisting ofA. an at least mononuclear heterocyclic group having 4 to 10 carbon atoms in the ring system bound to the group ##STR2## through a carbon atom and containing at least one oxygen, nitrogen or sulphur atom,B. substitution products of (A) containing at least one substituent selected from the group consisting of halogen, trifluoromethyl, hydroxy, alkoxy of 1 to 3 carbon atoms, unsubstituted amino, amino substituted by up to two alkyl groups each having 1 to 3 carbon atoms and alkyl groups having 1 to 6 carbon atoms,X is oxygen, sulphur or an NH-group,Y is an alkylene group having 1 to 3 carbon atoms in the chain, or an alkylene group having 1 to 3 carbon atoms in the chain substituted by (a) up to 3 alkyl groups each having up to 3 carbon atoms and a total of not more than 8 carbon atoms, or (b) substituted by one or two phenyl groups,R.sub.2 is selected from the group consisting ofC. an at least mononuclear carbocyclic or heterocyclic group having 4 to 10 carbon atoms in the ring system, containing but one heteroatom in a ring,D. substitution products of (C) containing at least one substituent selected from the group consisting of nitro, halogen, trifluoromethyl, alkyl having 1 to 6 carbon atoms, hydroxy, alkoxy having 1 to 3 carbon atoms, unsubstituted amino groups and amino groups substituted by up to two alkyl groups each having 1 to 3 carbon atoms,R.sub.3 is hydrogen or up to two substituents selected from alkyl groups having up to 2 carbon atoms and phenyl groups.n is 2 or 3;A process for its preparation and a pharmaceutical composition containing said compound (I).
摘要翻译：具有通式的化合物或其酸加成盐，其中式R1选自A.在环系中结合有至少单个的具有4至10个碳原子的单核杂环基含有至少一个氧原子，氮原子或硫原子的基团“IMAGE”，B.含有至少一个选自卤素，三氟甲基，羟基，1〜3的烷氧基的取代基的（A）碳原子，未取代的氨基，被至多两个各自具有1至3个碳原子的烷基和具有1至6个碳原子的烷基取代的氨基，X是氧，硫或NH-基，Y是具有1至该链中的3个碳原子或链中具有1至3个碳原子的亚烷基被（a）至多3个各自具有至多3个碳原子和总共不超过8个碳原子的烷基取代，或（ b）被一个或两个苯基取代，R2是sele 在环系中具有4-10个碳原子的至少单核碳环或杂环基团，在环中含有一个杂原子，D.含有至少一个选自以下的取代基的取代产物：（C）由硝基，卤素，三氟甲基，具有1至6个碳原子的烷基，羟基，具有1至3个碳原子的烷氧基，未取代的氨基和被至多两个各自具有1至3个碳原子的烷基取代的氨基，R3，是氢或至多两个选自具有至多2个碳原子的烷基和苯基的取代基。

7. 发明授权

US4216216A Aromatic piperazinyl substituted dihydrouracils 失效
标题翻译：芳香哌嗪基取代的二氢尿嘧啶
公开(公告)号：US4216216A
公开(公告)日：1980-08-05
申请号：US915899
申请日：1978-06-15
申请人： Rolf-Ortwin Weber , Hiristo Anagnostopulos , Ulrich Gebert
发明人： Rolf-Ortwin Weber , Hiristo Anagnostopulos , Ulrich Gebert
IPC分类号： A61K31/495 , A61K31/505 , A61P25/04 , A61P43/00 , C07D239/22 , C07D239/54 , C07D239/56 , C07D295/13 , C07D401/06 , C07D403/06
CPC分类号： C07D239/22 , C07D295/13
摘要： Compounds of general formula ##STR1## are disclosed wherein appropriate substituents for R.sup.1, R.sup.2 to R.sup.5, R.sup.6, A, Q, X, and Z are defined for these novel hexahydropyrimidines. Procedures for the preparation of these compounds are also given. Because of the highly effective serotonin antagonistic activity in combination with a strong inhibiting effect on thrombocyte aggregation and good compatibility these compounds are effective in treating migraine. Additionally, the compounds also exhibit an anti-histamine activity, cause an increase in erythrocyte fluidity, a psychotropic activity, a weak bradykinin antagonism and hypotensive effects.
摘要翻译：公开了通式“IMAGE”的化合物，其中适用于R1，R2至R5，R6，A，Q，X和Z的取代基用于这些新的六氢嘧啶。还给出了这些化合物的制备方法。由于高度有效的5-羟色胺拮抗活性与对血栓细胞聚集的强抑制作用以及良好的相容性，这些化合物在治疗偏头痛方面是有效的。此外，化合物还表现出抗组胺活性，导致红细胞流动性增加，精神活性，弱缓激肽拮抗作用和降血压作用。

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