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1. 发明授权

US4536402A Vinylogous carboxamides 失效
标题翻译： Vinylogous甲酰胺
公开(公告)号：US4536402A
公开(公告)日：1985-08-20
申请号：US676067
申请日：1984-11-29
申请人： Wolfhard Engel , Eckhart Bauer , Gunter Trummlitz , Peter Danneberg , Joachim Kahling
发明人： Wolfhard Engel , Eckhart Bauer , Gunter Trummlitz , Peter Danneberg , Joachim Kahling
IPC分类号： A61K31/38 , A61K31/381 , A61P25/00 , A61P25/08 , C07D333/64 , C07D409/06 , A61K31/44 , C07D333/52
CPC分类号： C07D409/06 , C07D333/64
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is phenyl, halo- and/or methyl-substituted phenyl or pyridinyl;R.sub.2 is hydrogen, straight or branched alkyl of 1 to 4 carbon atoms, 2- or 3-hydroxy-(alkyl of 2 to 3 carbon atoms) or 2- or 3-dimethylamino-(alkyl of 2 to 3 carbon atoms);R.sub.3 is hydrogen or alkyl of 1 to 3 carbon atoms; andR.sub.4 is hydrogen, chlorine or methyl.The compounds are useful as anticonvulsants.
摘要翻译：其中R 1是苯基，卤代和/或甲基取代的苯基或吡啶基; R2是氢，1至4个碳原子的直链或支链烷基，2-或3-羟基 - （2-3个碳原子的烷基）或2-或3-二甲基氨基 - （2-3个碳原子的烷基）; R3是氢或1至3个碳原子的烷基; R4为氢，氯或甲基。该化合物可用作抗惊厥药。

2. 发明授权

US4735959A Carboxylic acid amides and pharmaceutical compositions containing them 失效
标题翻译：羧酸酰胺和含有它们的药物组合物
公开(公告)号：US4735959A
公开(公告)日：1988-04-05
申请号：US734252
申请日：1985-05-14
申请人： Wolfgang Grell , Gerhart Griss , Robert Sauter , Rudolf Hurnaus , Eckhard Rupprecht , Nikolaus Kaubisch , Joachim Kahling , Bernhard Eisele
发明人： Wolfgang Grell , Gerhart Griss , Robert Sauter , Rudolf Hurnaus , Eckhard Rupprecht , Nikolaus Kaubisch , Joachim Kahling , Bernhard Eisele
IPC分类号： C07D207/26 , C07D207/27 , C07D209/44 , C07D211/22 , C07D211/46 , C07D211/70 , C07D211/74 , C07D213/40 , C07D213/80 , C07D217/04 , C07D223/04 , C07D225/02 , C07D295/073 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/192 , C07D317/22 , C07D473/08 , C07D491/10 , A61K31/445 , A61K31/165 , C07C103/82 , C07D295/14
CPC分类号： C07D207/27 , C07D209/44 , C07D211/22 , C07D211/46 , C07D211/70 , C07D211/74 , C07D213/40 , C07D213/80 , C07D217/04 , C07D223/04 , C07D225/02 , C07D295/073 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/192 , C07D317/22 , C07D473/08 , C07D491/10 , Y10S514/866
摘要： There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.
摘要翻译：描述了式（I）的新型羧酸衍生物和式（Ia）的衍生物及其加成盐，其对中间代谢具有影响。此外，式Ia化合物以及式I化合物具有降血糖特性。

3. 发明授权

US4288437A 2-[(Amino)-aryl-methylene]-benzo[b]thiophen-3(2H)-ones 失效
标题翻译： 2 - [（氨基） - 芳基 - 亚甲基] - 苯并[b]噻吩-3（2H） - 酮
公开(公告)号：US4288437A
公开(公告)日：1981-09-08
申请号：US173173
申请日：1980-07-28
申请人： Wolfhard Engel , Gunter Trummlitz , Ernst Seeger , Joachim Kahling
发明人： Wolfhard Engel , Gunter Trummlitz , Ernst Seeger , Joachim Kahling
IPC分类号： A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4433 , A61K31/445 , A61K31/495 , A61K31/535 , A61P25/08 , C07D333/62 , C07D333/64 , C07D409/06
CPC分类号： C07D333/62 , C07D333/64
摘要： Compounds of the formula ##STR1## wherein Ar is phenyl; mono- or di-substituted phenyl, where the substituents are one to two halogens, one to two alkyls of 1 to 3 carbon atoms, or one amino, nitro, cyano or trifluoromethyl; or pyridinyl;R is hydrogen, chlorine, methyl or methoxy;R.sub.1 is hydrogen or methyl;R.sub.2 is hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, methyl-(cycloalkyl of 3 to 8 carbon atoms) or --A--R.sub.4,where A is alkylene of 2 to 3 carbon atoms, and R.sub.4 is hydroxyl, methylamino, dimethylamino, N-methyl-ethylamino, diethylamino, pyrrolidino, piperidino, hexamethyleneimino, morpholino or 4-methyl-1-piperazinyl; orR.sub.1 and R.sub.2, together with each other and the nitrogen atom to which they are attached, form a 4- to 7-membered, saturated or mono-unsaturated, unsubstituted or substituted heterocycle which may contain nitrogen, oxygen, sulfur, sulfinyl or sulfonyl as additional ring members, where the substituents are alkyls of 1 to 3 carbon atoms.The compounds are useful as anticonvulsants.
摘要翻译：其中Ar是苯基的式IMAMA的化合物; 单取代或二取代的苯基，其中取代基是一至两个卤素，一至二个碳原子数为1至2个的烷基，或一个氨基，硝基，氰基或三氟甲基; 或吡啶基; R是氢，氯，甲基或甲氧基; R1是氢或甲基; R2是氢，1至6个碳原子的烷基，2至6个碳原子的烯基，2至6个碳原子的炔基，3至8个碳原子的环烷基，甲基 - 3至8个碳原子的环烷基或-A -R4，其中A为2至3个碳原子的亚烷基，R4为羟基，甲基氨基，二甲基氨基，N-甲基 - 乙基氨基，二乙基氨基，吡咯烷子基，哌啶子基，六亚甲基亚氨基，吗啉代或4-甲基-1-哌嗪基; 或R 1和R 2彼此连接并与它们相连的氮原子形成可含有氮，氧，硫，亚磺酰基或磺酰基的4-至7-元饱和或单不饱和的未被取代或取代的杂环作为另外的环成员，其中取代基是1至3个碳原子的烷基。该化合物可用作抗惊厥药。

4. 发明授权

US4343811A 2[3-(4-Chlorophenyl)-1,2-dimethyl-1H-indol-5-yloxy]-2-methyl propanoic acid and hyperlipidemic or atheosclerotic use thereof 失效
标题翻译： 2 [3-（4-氯苯基）-1,2-二甲基-1H-吲哚-5-基氧基] -2-甲基丙酸和其高脂血症或动脉粥样硬化用途
公开(公告)号：US4343811A
公开(公告)日：1982-08-10
申请号：US126006
申请日：1980-02-29
申请人： Rudolf Hurnaus , Gerhart Griss , Wolfgang Grell , Robert Sauter , Bernhard Eisele , Nikolaus Kaubisch , Eckhard Rupprecht , Joachim Kahling
发明人： Rudolf Hurnaus , Gerhart Griss , Wolfgang Grell , Robert Sauter , Bernhard Eisele , Nikolaus Kaubisch , Eckhard Rupprecht , Joachim Kahling
IPC分类号： C07D401/04 , A61K31/40 , A61K31/403 , A61K31/44 , A61K31/4427 , A61P3/06 , A61P9/10 , C07D209/04 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D209/43 , C07D401/06 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D487/04 , Y10S514/824
摘要： This invention relates to novel indole derivatives of formula ##STR1## and the non-toxic, pharmacologically acceptable salts thereof. These compounds exhibit desirable pharmacological properties, especially lipid-level lowering and anti-atherosclerotic activity. The compounds of the invention may be prepared by, for example, alkylation of a corresponding hydroxy indole.
摘要翻译：本发明涉及式IMA的新型吲哚衍生物及其无毒的药理学上可接受的盐。这些化合物显示出所需的药理学性质，特别是脂质降低和抗动脉粥样硬化活性。本发明的化合物可以通过例如相应的羟基吲哚的烷基化来制备。

5. 发明授权

US3992536A Pharmaceutical compositions containing a 1-phenyl-2,2,4,4-C.sub.1 -C.sub.2 alkyl-3-[4-phenyl of pyridyl)-piperazino]-cyclobutanol-(1) and method of use 失效
标题翻译：含有1-苯基-2,2,4,4-C（HD 1 {B -C {HD 2 {B烷基-3- {8-吡啶基]苯基） - 哌嗪基{9-环丁醇 - （1 ）和使用方法
公开(公告)号：US3992536A
公开(公告)日：1976-11-16
申请号：US641337
申请日：1975-12-16
申请人： Manfred Kleemann , Joachim Kahling , Gerhart Griss , Rudolf Hurnaus
发明人： Manfred Kleemann , Joachim Kahling , Gerhart Griss , Rudolf Hurnaus
IPC分类号： A61K31/495
CPC分类号： A61K31/495 , Y10S514/906
摘要： Pharmaceutical dosage unit compositions containing as an active ingredient a compound of the formula ##SPC1##WhereinR.sub.1 to R.sub.3, which may be the same or different, represent hydrogen atoms, halogen atoms, hydroxy, trifluoromethyl, benzyloxy, acyloxy groups, alkyl groups with 1 to 6 carbon atoms, alkoxy groups with 1 to 3 carbon atoms, phenyl, cyclohexyl, or 2 of the radicals R.sub.1 to R.sub.3 together represents a methylenedioxy group,R.sub.4 represents a hydrogen atom or an alkyl group with 1 or 2 carbon atoms,R.sub.5 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms andR.sub.6 represents a phenyl group, which may be mono- or disubstituted by halogen atoms, trifluoromethyl, hydroxy, nitro, amino, benzyloxy, acyloxy groups, alkyl groups with 1 to 3 carbon atoms, alkoxy groups with 1 to 3 carbon atoms or alkylthio groups with 1 to 3 carbon atoms; or a pyridyl group, optionally substituted by a halogen atom, a hydroxy, nitro, amino, benzyloxy, acyloxy, carboxy group, a carbaloxy group with 1 to 3 carbon atoms in the alkoxy, an alkyl group with 1 to 3 carbon atoms or an alkoxy group with 1 to 3 carbon atoms,Or a salt thereof with a physiologically compatible inorganic or organic acid or base; and a method of using the same as sedatives and muscle relaxants.
摘要翻译：含有式+ q，10的化合物作为活性成分的药物剂量单位组合物可以相同或不同，表示氢原子，卤素原子，羟基，三氟甲基，苄氧基，酰氧基，烷基与 1至6个碳原子，具有1至3个碳原子的烷氧基，基团R 1至R 3的苯基，环己基或2一起表示亚甲二氧基，R 4表示氢原子或具有1或2个碳原子的烷基，R 5 表示氢原子或具有1至3个碳原子的烷基，R 6表示可被卤素原子，三氟甲基，羟基，硝基，氨基，苄氧基，酰氧基单 - 或二取代的苯基， 3个碳原子，1〜3个碳原子的烷氧基或1〜3个碳原子的烷硫基; 或任选被卤素原子取代的吡啶基，羟基，硝基，氨基，苄氧基，酰氧基，羧基，烷氧基中具有1至3个碳原子的碳酰氧基，具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基，或其与生理上相容的无机或有机酸或碱的盐; 以及将其用作SEDATIVES和MUSCLE RELAXANTS的方法。

6. 发明授权

US4179508A Sulfur-containing derivatives of 4,4-dimethyl-2H,4H-isoquinoline-1,3-dione, and anticonvulsant and antihyperlipidemic compositions thereof 失效
标题翻译： 4,4-二甲基-2H，4H-异喹啉-1,3-二酮的含硫衍生物及其抗惊厥和抗高脂血症组合物
公开(公告)号：US4179508A
公开(公告)日：1979-12-18
申请号：US925877
申请日：1978-07-18
申请人： Volkhard Austel , Eberhard Kutter , Wolfgang Eberlein , Joachim Heider , Joachim Kahling
发明人： Volkhard Austel , Eberhard Kutter , Wolfgang Eberlein , Joachim Heider , Joachim Kahling
IPC分类号： A61K31/47 , A61K31/472 , A61P3/06 , A61P25/08 , C07D217/24
CPC分类号： C07D217/24
摘要： Compounds of the formula ##STR1## wherein A is lower alkylene,R is lower alkyl, andn is 0, 1 or 2;the compounds are useful as anti-hyperlipidemics and anti-convulsants.
摘要翻译：其中A为低级亚烷基，R为低级烷基，n为0,1或2的式IMA化合物; 该化合物可用作抗高脂血症和抗惊厥药。

7. 发明授权

US4093734A Amino-benzoic acid amides 失效
标题翻译：氨基 - 苯甲酸酰胺
公开(公告)号：US4093734A
公开(公告)日：1978-06-06
申请号：US734818
申请日：1976-10-22
申请人： Gerd Kruger , Johannes Keck , Klaus Reinhold Noll , Helmut Pieper , Harald Ziegler , Helmut Ballhause , Joachim Kahling
发明人： Gerd Kruger , Johannes Keck , Klaus Reinhold Noll , Helmut Pieper , Harald Ziegler , Helmut Ballhause , Joachim Kahling
IPC分类号： C07D295/12 , A61K31/165 , A61K31/40 , A61K31/415 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P1/04 , A61P1/08 , A61P25/24 , A61P25/26 , C07C237/30 , C07D207/09 , C07D211/26 , C07D211/56 , C07D211/58 , C07D213/40 , C07D213/75 , C07D233/30 , C07D295/13 , C07D453/02 , C07D207/44
CPC分类号： C07D213/40 , C07D207/09 , C07D211/26 , C07D211/56 , C07D233/30 , C07D295/13 , C07D453/02
摘要： Compounds of the formula ##STR1## wherein (A) WHEN THE AMINO-SUBSTITUENT IS IN THE P-POSITION WITH RESPECT TO THE CARBONYL GROUP,R.sub.1 is chlorine in the o-position with respect to the carbonyl group,R.sub.2 is hydrogen, andR.sub.3 is ethylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, N-methyl-cyclohexylamino, benzylamino or 1-ethyl-pyrrolidyl-(2)-aminomethyl, or(b) when the amino-substituent is in the o--, m-- or p-position with respect to the carbonyl group,R.sub.1 is hydrogen, chlorine or bromine,R.sub.2 is trifluoromethyl, nitro or, when R.sub.4 is 1-(alkyl of 1 to 3 carbon atoms)-pyrrolidyl or 1-(alkyl of 1 to 3 carbon atoms)-piperidyl, also fluorine, chlorine, bromine or methyl,R.sub.3 is (alkyl of 1 to 5 carbon atoms)-amino, (cycloalkyl of 3 to 7 carbon atoms)-amino, benzylamino, quinuclidinyl-amino or --NH--(CH.sub.2).sub.n --R.sub.4where R.sub.4 is pyridyl, 1-(alkyl of 1 to 3 carbon atoms)-pyrrolidyl, 1-(alkyl of 1 to 3 carbon atoms)-piperidyl or, when n is 2 or 3, also imidazolonyl, pyrrolidino, piperidino or morpholino, andn is 0, 1, 2 or 3,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anxiolytics, anticonvulsives, antiemetics and antiulcerogenics.
摘要翻译：式（A）的化合物其中（A）当氨基取代基位于与碳组相对位置时，R 1为相对于羰基的o位置的氯，R 2为氢，R 3为是乙基氨基，环戊基氨基，环己基氨基，环庚基氨基，N-甲基 - 环己基氨基，苄基氨基或1-乙基 - 吡咯烷基 - （2） - 氨基甲基，或（B）当氨基取代基位于O-，对于羰基，R1是氢，氯或溴，R2是三氟甲基，硝基，或当R4是1-（1至3个碳原子的烷基） - 吡咯烷基或1-（1至3个碳原子的烷基）时， - 哌啶基，氟，氯，溴或甲基，R3是（碳原子数1〜5的烷基） - 氨基，（3〜7个碳原子的环烷基） - 氨基，苄基氨基，奎宁环基 - 氨基或-NH-（CH2） n-R4，其中R4是吡啶基，1-（1至3个碳原子的烷基） - 吡咯烷基，1-（1至3个碳原子的烷基） - 哌啶基，或当n是2或3时，也是咪唑啉基，吡咯烷子基，哌啶子基或mor pholino和N IS 0,1,2或3，以及非毒性，药理学上可接受的酸添加量; 化合物作为它们的有效的有用的ANXIOLYTICS，ANTICONVULSIVES，抗原和抗生素。

8. 发明授权

US3931185A 1-Phenyl-2,2,4,4-C.sub.1 -C.sub.2 alkyl-3-[4-(phenyl or pyridyl)-piperazino]-cyclobutanols-(1) 失效
标题翻译： 1-苯基-2,2,4,4-C（HD 1 {B -C {HD 2 {B烷基-3- {8 4-（苯基或吡啶基） - 哌嗪基{9-环丁烷醇 - （1）
公开(公告)号：US3931185A
公开(公告)日：1976-01-06
申请号：US413233
申请日：1973-11-06
申请人： Manfred Kleemann , Joachim Kahling , Gerhart Griss , Rudolf Hurnaus
发明人： Manfred Kleemann , Joachim Kahling , Gerhart Griss , Rudolf Hurnaus
IPC分类号： C07D295/08 , A61K31/495 , A61K31/496 , C07D213/74 , C07D213/79 , C07D295/00 , C07D295/04 , C07D295/096 , C07D295/135 , C07D405/08 , C07D295/12
CPC分类号： C07D295/096 , A61K31/495 , C07D295/135 , Y10S514/906
摘要： This invention relates to cyclobutane derivatives having the formula ##SPC1##Wherein R.sub.1 to R.sub.3, which may be the same or different, represent hydrogen atoms, halogen atoms, hydroxy, trifluoromethyl, benzyloxy, acyloxy groups, alkyl groups with 1 to 6 carbon atoms, alkoxy groups with 1 to 3 carbon atoms, phenyl, cyclohexyl, or 2 of the radicals R.sub.1 to R.sub.3 together represents a methylenedioxy group,R.sub.4 represents a hydrogen atom or an alkyl group with 1 or 2 carbon atoms,R.sub.5 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms andR.sub.6 represents a phenyl group, which may be mono- or disubstituted by halogen atoms, trifluoromethyl, hydroxy, nitro, amino, benzyloxy, acyloxy groups, alkyl groups with 1 to 3 carbon atoms, alkoxy groups with 1 to 3 carbon atoms or alkylthio groups with 1 to 3 carbon atoms; or a pyridyl group, optionally substituted by a halogen atom, a hydroxy, nitro, amino, benzyloxy, acyloxy, carboxy group, a carbalkoxy group with 1 to 3 carbon atoms in the alkoxy, an alkyl group with 1 to 3 carbon atoms or an alkoxy group with 1 to 3 carbon atoms;To salts thereof with physiologically compatible inorganic or organic acids or bases as well as to processes for their preparation.The cyclobutane compounds of the above general formula show valuable pharmacological properties, especially a sedative and muscle relaxing activity.
摘要翻译：本发明涉及具有式WHEREIN R 1至R 3的环丁烷衍生物，其可以相同或不同，表示氢原子，卤素原子，羟基，三氟甲基，苄氧基，酰氧基，具有1-6个碳原子的烷基， 1至3个碳原子，基团R 1至R 3的苯基，环己基或2一起表示亚甲二氧基，R 4表示氢原子或具有1或2个碳原子的烷基，R 5表示氢原子或 1至3个碳原子，R 6表示可被卤素原子，三氟甲基，羟基，硝基，氨基，苄氧基，酰氧基，具有1至3个碳原子的烷基，1至3个碳原子的烷基， 3个碳原子或1〜3个碳原子的烷硫基; 或任选被卤素原子取代的吡啶基，羟基，硝基，氨基，苄氧基，酰氧基，羧基，烷氧基中具有1至3个碳原子的烷氧基，具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基; 与生理学兼容的有机酸或有机酸或基础同样适用于其制备方法。

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