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1. 发明授权

US4328235A Suppressing pain with benzothiazol-2(3H)-ones 失效
标题翻译：用苯并噻唑-2（3H）酮抑制疼痛
公开(公告)号：US4328235A
公开(公告)日：1982-05-04
申请号：US163965
申请日：1980-06-30
申请人： Gunter Trummlitz , Wolfhard Engel , Gunther Schmidt , Wolfgang Eberlein , Ernst Seeger , Gunther Engelhardt , Rainer Zimmermann
发明人： Gunter Trummlitz , Wolfhard Engel , Gunther Schmidt , Wolfgang Eberlein , Ernst Seeger , Gunther Engelhardt , Rainer Zimmermann
IPC分类号： A61K31/425 , A61K31/428 , A61P25/04 , A61P29/00 , C07D277/68
CPC分类号： C07D277/68 , A61K31/425
摘要： There are described pharmaceutical compositions containing as active substances benzothiazol-2(3H)-ones of the general formula ##STR1## wherein R represents a hydrogen atom or a methyl, methoxy, or ethoxy group. The pharmaceutical compositions serve as analgesics and antipyretics and possess little or no methemoglobin-forming activity.
摘要翻译：描述了含有作为活性物质的通式为“IMAGE”的苯并噻唑-2（3H） - 酮的药物组合物，其中R表示氢原子或甲基，甲氧基或乙氧基。药物组合物用作止痛剂和解热药，并且几乎没有或没有高铁血红蛋白形成活性。

2. 发明授权

US4381303A 1,4,9,10-Tetrahydro-pyrazolo [4,3-]pyrido[-3,2-b][1,4]diazepin-10-ones 失效
标题翻译： 1,4,9,10-四氢 - 吡唑并[4,3]吡啶并[-3,2-b] [1,4]二氮杂-10-酮
公开(公告)号：US4381303A
公开(公告)日：1983-04-26
申请号：US377911
申请日：1982-05-13
申请人： Gunther Schmidt , Wolfhard Engel , Wolfgang Eberlein , Gunter Trummlitz , Gunther Engelhardt
发明人： Gunther Schmidt , Wolfhard Engel , Wolfgang Eberlein , Gunter Trummlitz , Gunther Engelhardt
IPC分类号： A61K31/55 , A61K31/5517 , A61P25/04 , A61P29/00 , C07D231/16 , C07D471/14
CPC分类号： C07D471/14 , C07D231/16
摘要： This invention is directed to the compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or an alkyl of from 1 to 6 carbon atoms;R.sub.2 is an alkyl of from 1 to 3 carbon atoms;R.sub.3 is hydrogen or an alkyl of from 1 to 3 carbon atoms; andR.sub.4 is hydrogen or an alkyl of from 1 to 4 carbon atoms.These compounds are useful in pharmaceutical compositions which serve as analgesics, antiphlogistics and antipyretics.
摘要翻译：本发明涉及式（I）的化合物，其中R 1是氢或1至6个碳原子的烷基; R2是1至3个碳原子的烷基; R3是氢或1至3个碳原子的烷基; 且R 4为氢或1至4个碳原子的烷基。这些化合物可用作用作镇痛药，消炎药和解热药的药物组合物。

3. 发明授权

US4353919A Analgesic and antipyretic pharmaceutical compositions containing a benzothiazol-2(3H)-one 失效
标题翻译：含有苯并噻唑-2（3H） - 酮的镇痛药和解热药物组合物
公开(公告)号：US4353919A
公开(公告)日：1982-10-12
申请号：US254539
申请日：1981-04-15
申请人： Wolfhard Engel , Gunter Trummlitz , Wolfgang Eberlein , Gunther Schmidt , Gunther Engelhardt , Rainer Zimmermann
发明人： Wolfhard Engel , Gunter Trummlitz , Wolfgang Eberlein , Gunther Schmidt , Gunther Engelhardt , Rainer Zimmermann
IPC分类号： A61K31/425 , C07D277/68
CPC分类号： C07D277/68 , A61K31/425 , Y10S514/916
摘要： Analgesic and antipyretic pharmaceutical dosage unit compositions containing as an active ingredient a compound of the formula ##STR1## wherein R.sub.5 is methyl or methoxy, and R.sub.4, R.sub.6 and R.sub.7 are hydrogen; orR.sub.6 is fluorine or chlorine, and R.sub.4, R.sub.5 and R.sub.7 are hydrogen; orR.sub.7 is chlorine, and R.sub.4, R.sub.5 and R.sub.6 are hydrogen; orR.sub.5 and R.sub.6 are methoxy, and R.sub.4 and R.sub.7 are hydrogen; orR.sub.4 is methyl or chlorine, and R.sub.5, R.sub.6 and R.sub.7 are hydrogen;and methods of using said compounds as analgesics and antipyretics.
摘要翻译：镇痛药和解热药物单位组合物，其含有下式的化合物作为活性成分：其中R5是甲基或甲氧基，R4，R6和R7是氢; 或R6是氟或氯，R4，R5和R7是氢; 或R 7为氯，R 4，R 5和R 6为氢; 或R5和R6是甲氧基，R4和R7是氢; 或R4是甲基或氯，R5，R6和R7是氢; 以及使用所述化合物作为止痛剂和解热剂的方法。

4. 发明授权

US4404230A 4-Hydroxy-1,2-Benzisothiazol-3(2H)-one-1,1-dioxides and salts thereof 失效
标题翻译： 4-羟基-1,2-苯并异噻唑-3（2H） - 酮-1,1-二氧化物及其盐
公开(公告)号：US4404230A
公开(公告)日：1983-09-13
申请号：US254546
申请日：1981-04-15
申请人： Gunter Trummlitz , Wolfgang Eberlein , Wolfhard Engel , Gunther Schmidt
发明人： Gunter Trummlitz , Wolfgang Eberlein , Wolfhard Engel , Gunther Schmidt
IPC分类号： A23L27/20 , A23L27/30 , C07C205/58 , C07D275/04 , C07D275/06 , A23L1/236
CPC分类号： C07D275/06 , A23L27/2056 , A23L27/30 , C07C205/58 , C07C255/00 , C07C309/00
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxyl, and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as sweetening agents.
摘要翻译：其中R1是氢或羟基的式“IMAGE”的化合物，以及与无机或有机碱形成的无毒的药学上可接受的盐。化合物及其盐可用作甜味剂。

5. 发明授权

US4550107A Condensed diazepinones, their compositions and methods of use as pharmaceuticals 失效
标题翻译：浓缩二氮杂酮，其组合物和用作药物的方法
公开(公告)号：US4550107A
公开(公告)日：1985-10-29
申请号：US711913
申请日：1985-03-14
申请人： Wolfhard Engel , Gunter Trummlitz , Wolfgang Eberlein , Gerhard Mihm , Gunther Schmidt , Rudolf Hammer , Antonio Giachetti
发明人： Wolfhard Engel , Gunter Trummlitz , Wolfgang Eberlein , Gerhard Mihm , Gunther Schmidt , Rudolf Hammer , Antonio Giachetti
IPC分类号： A61K31/00 , A61K31/55 , A61P9/06 , A61P25/02 , C07D207/09 , C07D207/16 , C07D207/34 , C07D211/26 , C07D213/38 , C07D223/04 , C07D223/08 , C07D223/12 , C07D243/00 , C07D243/14 , C07D243/38 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/06 , C07D413/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D495/14 , C07D521/00
CPC分类号： C07D401/06 , C07C255/00 , C07D207/16 , C07D207/34 , C07D211/26 , C07D223/04 , C07D223/08 , C07D403/06 , C07D413/06 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Disclosed are novel condensed diazepinones of formula I ##STR1## wherein B is a fused ring selected from ##STR2## X is --CH-- or, when B is ortho-phenylene, X can also be nitrogen; A.sub.1 is C.sub.1 -C.sub.2 alkylene; A.sub.2 is C.sub.1 -C.sub.2 when it is in the 2-position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3- or 4-position; R.sub.1 is C.sub.1 -C.sub.3 alkyl; R.sub.2 is C.sub.1 -C.sub.7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C.sub.3 -C.sub.7 cycloalkyl, optionally hydroxy substituted, or C.sub.3 -C.sub.7 cycloalkylmethyl; or R.sub.1 and R.sub.2 can, together with the nitrogen therebetween, be a 4- to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N--CH.sub.3 ; R.sub.3 is hydrogen, chlorine, or methyl; R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 is hydrogen, chlorine or C.sub.1 -C.sub.4 alkyl; and Z is a single bond, oxygen, methylene or 1,2-ethylene; and NR.sub.1 R.sub.2 --N oxides and nontoxic, pharmaceutically acceptable addition salts thereof. Also disclosed are pyrrolobenzodiazepinone intermediates, pharmaceutical compositions containing the condensed diazepinones and methods of using them to treat cardiovascular disorders, particularly bradycardia and bradyarrhythmia.
摘要翻译：公开了式I的新型稠合二氮杂酮，其中B是选自下列的稠环，X是-CH-，或当B是邻 - 亚苯基时，X也可以是氮; A1是C1-C2亚烷基; 当A2位于3-或4-位时相对于饱和杂环氮或单键或亚甲基为2-位，则为C1-C2; R1是C1-C3烷基; R2是任选在其第二至第七碳中的至少一个上被羟基取代的C 1 -C 7烷基，或任选被羟基取代的C 3 -C 7环烷基或C 3 -C 7环烷基甲基; 或者R 1和R 2可以与它们之间的氮一起是可以任选地包括氧或N-CH 3的4-至7-元饱和单环杂环; R3是氢，氯或甲基; R4是氢或C1-C4烷基，R5是氢，氯或C1-C4烷基; Z为单键，氧，亚甲基或1,2-亚乙基; 和NR 1 R 2 -N氧化物和无毒的药学上可接受的加成盐。还公开了吡咯并苯并二氮杂酮中间体，含有缩合二氮嗪酮的药物组合物及其用于治疗心血管疾病，特别是心动过缓和缓慢性心律失常的方法。

6. 发明授权

US4443452A Dibenzodiazepinones, pharmaceutical compositions thereof and method of use thereof 失效
标题翻译：二苯并二氮杂酮，其药物组合物及其使用方法
公开(公告)号：US4443452A
公开(公告)日：1984-04-17
申请号：US462378
申请日：1983-01-31
申请人： Wolfhard Engel , Gunter Trummlitz , Gunther Schmidt , Wolfgang Eberlein , Rudolf Hammer , Piero del Soldato
发明人： Wolfhard Engel , Gunter Trummlitz , Gunther Schmidt , Wolfgang Eberlein , Rudolf Hammer , Piero del Soldato
IPC分类号： A61K31/55 , A61P1/04 , C07D243/38 , C07D401/12 , C07D451/02 , C07D451/04 , C07D451/06 , C07D403/12 , C07D403/14
CPC分类号： C07D451/04 , C07D243/38 , C07D401/12 , C07D451/06 , Y10S514/926 , Y10S514/927
摘要： This invention relates to compounds of the formula ##STR1## wherein X is oxygen, --NH--, or--NCH.sub.3 --andR is 1-methyl-4-piperidinyl, 4-methyl-1-piperazinyl, endo-8-methyl-8-azabicyclo[3.2.1]oct-3-yl, or exo-8-methyl-8-acabicyclo[3.2.1]oct-3-yl, each of which may optionally have an additional methyl substitutent,a diastereomer or enantiomer thereof, or a non-toxic, pharmacologically acceptable acid addition salt thereof with an inorganic or organic acid.
摘要翻译：本发明涉及下式化合物，其中X为氧，-NH-或-NCH 3 - ，R为1-甲基-4-哌啶基，4-甲基-1-哌嗪基，内-8-甲基-8 - 氮杂双环[3.2.1]辛-3-基或外-8-甲基-8-氮杂双环[3.2.1]辛-3-基，其各自可以任选地具有另外的甲基取代基，非对映异构体或对映体，或其与无机或有机酸的无毒，药理学上可接受的酸加成盐。

7. 发明授权

US4567178A Substituted 5,11-dihydro-6H-dibenz[b,e]azepin-6-ones and pharmaceutical compositions containing same 失效
标题翻译：取代的5,11-二氢-6H-二苯并[b，e]氮杂-6-酮和含有它们的药物组合物
公开(公告)号：US4567178A
公开(公告)日：1986-01-28
申请号：US689325
申请日：1985-01-07
申请人： Wolfgang Eberlein , Gunter Trummlitz , Wolfhard Engel , Gunther Schmidt , Rudolf Hammer , Antonio Giachetti
发明人： Wolfgang Eberlein , Gunter Trummlitz , Wolfhard Engel , Gunther Schmidt , Rudolf Hammer , Antonio Giachetti
IPC分类号： A61K31/00 , A61K31/55 , A61P1/04 , A61P25/02 , C07D223/20 , C07D401/06 , C07D401/12 , C07D403/12 , C07D403/14
CPC分类号： C07D401/06 , C07D223/20 , C07D401/12
摘要： The invention relates to novel substituted 5,11-dihydro-6H-dibenz[b,e]azepin-6-one of the formula ##STR1## wherein A represents a (1-methyl-4-piperidinyl)-acetyl, (4-methyl-1-piperazinyl)-acetyl, or [(1-methyl-4-piperidinyl)-amino]-carbonyl group,and the acid addition salts thereof, which have valuable pharmacological properties, particularly an ulcer-inhibiting and secretion-inhibiting activity. The compounds of Formula I may be prepared using methods conventionally used for analogous compounds.
摘要翻译：本发明涉及式（I）的新的取代的5,11-二氢-6H-二苯并[b，e]氮杂-6-酮，其中A表示（1-甲基-4-哌啶基） - 乙酰基，（4-甲基-1-哌嗪基） - 乙酰基或[（1-甲基-4-哌啶基） - 氨基] - 羰基及其酸加成盐，其具有有价值的药理学特性，特别是溃疡抑制和分泌抑制活性。式I的化合物可以使用常规用于类似化合物的方法制备。

8. 发明授权

US4447434A Substituted dibenzodiazepinones 失效
标题翻译：取代的二苯并二氮杂酮
公开(公告)号：US4447434A
公开(公告)日：1984-05-08
申请号：US462149
申请日：1983-01-31
申请人： Gunter Trummlitz , Wolfhard Engel , Wolfgang Eberlein , Gunther Schmidt , Rudolf Hammer , Piero del Soldato
发明人： Gunter Trummlitz , Wolfhard Engel , Wolfgang Eberlein , Gunther Schmidt , Rudolf Hammer , Piero del Soldato
IPC分类号： C07D243/26 , A61K31/00 , A61K31/55 , A61K31/5513 , A61P1/04 , C07D243/38 , C07D401/04 , C07D401/06 , C07D403/06 , C07D451/02 , C07F9/645
CPC分类号： C07D451/02 , C07D243/38 , C07D401/06 , C07F9/645
摘要： The specification describes new substituted dibenzodiazepinones of formula ##STR1## wherein R.sub.1 is hydrogen or chlorine atom and R is (1-methyl-4-piperidinyl)methyl, (1-methyl-1,2,5,6-tetrahydro-4-pyridinyl)methyl,1-methyl-1,2,5,6-tetrahydro-4-pyridinyl, (1-methyl-4-piperidinylidene)methyl,(2,3-dehydro-8-methyl-8-aza-bicyclo[3,2,1]oct-3-yl)-methyl, (8-methyl-8-aza-bicyclo[3,2,1]oct-3-ylidene)-methyl or an endo-or exo-(8-methyl-8-azabicyclo[3,2,1]oct-3-yl)methyl each being optionally substituted by one or two methyls on the heterocyclic ring, and the nontoxic, pharmaceutically acceptable acid addition salts thereof, processes for preparing them and pharmaceutical compositions containing these compounds.The compounds of formula I have an antiulcerative effect and an inhibitory effect on the secretion of gastric substances having anticholinergic activity, such as dryness of the mouth and mydriasis.
摘要翻译：该说明书描述了式（Ⅰ）的新的取代二苯并二氮杂酮，其中R 1是氢或氯原子，R是（1-甲基-4-哌啶基）甲基，（1-甲基-1,2,5,6-四氢 - 4-吡啶基）甲基，1-甲基-1,2,5,6-四氢-4-吡啶基，（1-甲基-4-亚哌啶基）甲基，（2,3-脱氢-8-甲基-8-氮杂 - 双环[3,2,1]辛-3-基） - 甲基，（8-甲基-8-氮杂 - 双环[3,2,1]辛-3-基） - 甲基或内 - 或外 - - （8-甲基-8-氮杂双环[3,2,1]辛-3-基）甲基，其各自任选被杂环上的一个或两个甲基取代，及其无毒的药学上可接受的酸加成盐，用于制备它们和含有这些化合物的药物组合物。式I化合物具有抗溃疡作用和对具有抗胆碱能活性的胃物质分泌的抑制作用，例如口干和散瞳。

9. 发明授权

US4410527A Substituted thienobenzodiazepinones and salts thereof 失效
标题翻译：取代的噻吩并二氮杂酮及其盐
公开(公告)号：US4410527A
公开(公告)日：1983-10-18
申请号：US462182
申请日：1983-01-31
申请人： Wolfhard Engel , Gunther Schmidt , Wolfgang Eberlein , Gunter Trummlitz , Rudolf Hammer , Piero Del Soldato
发明人： Wolfhard Engel , Gunther Schmidt , Wolfgang Eberlein , Gunter Trummlitz , Rudolf Hammer , Piero Del Soldato
IPC分类号： A61K31/55 , A61P1/04 , C07D495/04 , C07D519/00 , C07D417/06
CPC分类号： C07D495/04 , Y10S514/926 , Y10S514/927
摘要： Compounds of the formula ##STR1## wherein R is 1-methyl-4-piperididinyl, 4-methyl-1-piperazinyl, or 3 - or 3 -tropanyl, each of which may optionally have another methyl substituent attached to the heterocyclic ring;R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.2 is hydrogen, halogen or alkyl of 1 to 4 carbon atoms; andX is oxygen, --NH-- or --N(CH.sub.3)--;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
摘要翻译：其中R是1-甲基-4-哌啶基，4-甲基-1-哌嗪基或3-或3-支链基，其各自可以任选地具有连接到杂环上的另一个甲基取代基; R1是氢或1-4个碳原子的烷基; R2是氢，卤素或1-4个碳原子的烷基; X是氧，-NH-或-N（CH 3） - ; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作抗溃疡发生剂。

10. 发明授权

US4137313A 2,5-Dihydro-1,2-thiazino(5,6-b)indole-3-carboxamide-1,1-dioxides and salts thereof 失效
标题翻译： 2,5-二氢-1,2-噻嗪（5,6-b）吲哚-3-甲酰胺-1,1-二氧化物及其盐
公开(公告)号：US4137313A
公开(公告)日：1979-01-30
申请号：US872889
申请日：1978-01-27
申请人： Gunter Trummlitz , Wolfhard Engel , Ernst Seeger , Walter Haarmann , Gunther Engelhardt
发明人： Gunter Trummlitz , Wolfhard Engel , Ernst Seeger , Walter Haarmann , Gunther Engelhardt
IPC分类号： A61K31/54 , A61P7/02 , A61P29/00 , C07D209/42 , C07D513/04 , C07D513/14 , A61K31/38
CPC分类号： C07D513/04 , C07D209/42 , C07D513/14 , Y10S514/822
摘要： Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen, methyl or ethyl;R.sub.2 is methyl or ethyl;Y is hydrogen, fluorine, chlorine, bromine, methoxy, methyl, ethyl or trifluoromethyl; andAr is 2-thiazolyl which may have one or two methyl or ethyl substituents attached thereto; 5,6-dihydro-4H-cyclopentathiazol-2-yl; 4,5,6,7-tetrahydro-2-benzothiazolyl; 2-benzothiazolyl; 3-isothiazolyl which may have a methyl substituent attached thereto; 2-pyridyl which may have a methyl or hydroxyl substituent attached thereto; 3-pyridyl; 4-pyridyl; 4-pyrimidinyl; pyrazinyl; 2-benzimidazolyl; 2-oxazolyl which may have a methyl substituent attached thereto; 2-benzoxazolyl; or phenyl which may have a fluoro, chloro, bromo, methyl, ethyl, trifluoromethyl or methoxy substituent attached thereto; and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antiphlogistics and blood platelet aggregation inhibitors.
摘要翻译：式中的化合物，其中R1是氢，甲基或乙基; R2是甲基或乙基; Y是氢，氟，氯，溴，甲氧基，甲基，乙基或三氟甲基; 并且Ar是可以具有一个或两个连接到其上的甲基或乙基取代基的2-噻唑基; 5,6-二氢-4H-环戊基噻唑-2-基; 4,5,6,7-四氢-2-苯并噻唑基; 2-苯并噻唑基可具有与其连接的甲基取代基的3-异噻唑基; 可以具有连接到其上的甲基或羟基取代基的2-吡啶基; 3-吡啶基; 4-吡啶基; 4-嘧啶基; 吡嗪基 2-苯并咪唑基; 可具有与其连接的甲基取代基的2-恶唑基; 2-苯并恶唑基; 或可具有与其连接的氟，氯，溴，甲基，乙基，三氟甲基或甲氧基取代基的苯基; 和与无机或有机碱形成的无毒的，药学上可接受的盐。化合物及其盐可用作消炎剂和血小板聚集抑制剂。

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