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41. 发明授权

US4424226A Pyridobenzodiazepinones, pharmaceutical compositions thereof and method of use thereof 失效
标题翻译：吡啶并二氮杂酮，其药物组合物及其使用方法
公开(公告)号：US4424226A
公开(公告)日：1984-01-03
申请号：US462377
申请日：1983-01-31
申请人： Wolfgang Eberlein , Gu/ nter Trummlitz , Gu/ nther Schmidt , Wolfhard Engel , Rudolf Hammer , Piero Del Soldato
发明人： Wolfgang Eberlein , Gu/ nter Trummlitz , Gu/ nther Schmidt , Wolfhard Engel , Rudolf Hammer , Piero Del Soldato
IPC分类号： A61K31/00 , A61K31/55 , A61P1/00 , A61P1/04 , A61P25/02 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , Y10S514/926 , Y10S514/927
摘要： This invention relates to compounds of the formula ##STR1## wherein 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-azabicyclo�3.2.1!oct-3-yl methyl, endo-8-methyl-8-azabicyclo�3.2.1!oct-3-yl-methyl, or exo-8-methyl-8-azabicyclo�3.2.1!oct-3-yl-methyl, each of which may optionally have one or two methyl substituents on the six-membered heterocyclic ring, 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：本发明涉及式（I）的化合物，其中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] 内-8-甲基-8-氮杂双环[3.2.1]辛-3-基 - 甲基或外-8-甲基-8-氮杂双环[3.2.1]辛-3-基 - 甲基，各自其可以任选地在六元杂环上具有一个或两个甲基取代基，以及其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。

42. 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。

43. 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。

44. 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。

45. 发明授权

US5571806A Dibenz[b,f][1,4]oxazepin(and thiazepin)-11(10H)-ones and-thiones and their use in the prevention or treatment of HIV infection 失效
标题翻译：二苯并[b，f] [1,4]氧氮杂（和硫氮杂）-11（10H）酮和硫堇及其在预防或治疗艾滋病毒感染中的应用
公开(公告)号：US5571806A
公开(公告)日：1996-11-05
申请号：US271350
申请日：1994-07-06
申请人： Karl D. Hargrave , Gunther Schmidt, deceased , Wolfhard Engel , Kurt Schromm
发明人： Karl D. Hargrave , Gunther Schmidt, deceased , Wolfhard Engel , Kurt Schromm
IPC分类号： A61K31/00 , A61K31/55 , A61K31/554 , A61P31/12 , A61P31/18 , A61P37/04 , C07D267/20 , C07D281/16 , C07D413/04 , C07D417/04
CPC分类号： C07D281/16 , A61K31/55 , C07D267/20
摘要： Disclosed is the use of dibenz[b,f][1,4]oxazepin (or thiazepin)-11(10H)-ones and -thiones in the prevention and treatment of AIDS, ARC and related disorders associated with HIV infection.
摘要翻译：公开了二苯并[b，f] [1,4]氧氮杂（或硫氮杂）-11（10H） - 硫代乙酸酯在预防和治疗艾滋病，ARC和与HIV感染相关的相关疾病中的用途。

46. 发明授权

US5087625A Pyridodiazepines and their use in the prevention or treatment of HIV infection 失效
标题翻译：吡喹二氮卓类及其在预防或治疗艾滋病毒感染中的应用
公开(公告)号：US5087625A
公开(公告)日：1992-02-11
申请号：US650141
申请日：1991-02-04
申请人： Karl D. Hargrave , Gunther Schmidt, deceased , Wolfhard Engel , Vokhard Austel
发明人： Karl D. Hargrave , Gunther Schmidt, deceased , Wolfhard Engel , Vokhard Austel
IPC分类号： C07D471/04 , C07D495/14
CPC分类号： C07D471/04 , C07D495/14
摘要： Disclosed are novel pyridodiazepines. These compounds, as well as certain known 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-ones are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.
摘要翻译：公开的是新的吡啶并二氮杂。这些化合物以及某些已知的5,11-二氢-6H-吡啶并[2,3-b] [1,4]苯并二氮杂-6可用于治疗艾滋病，ARC和与HIV感染有关的相关疾病。

47. 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。

48. 发明授权

US3969418A (4-Biphenylyl)-butenols 失效
标题翻译：（4-联苯基） - 丁烯醇
公开(公告)号：US3969418A
公开(公告)日：1976-07-13
申请号：US485574
申请日：1974-07-03
申请人： Helmut Teufel , Wolfhard Engel , Ernst Seeger
发明人： Helmut Teufel , Wolfhard Engel , Ernst Seeger
IPC分类号： C07C31/34 , C07C31/14
摘要： Compounds of the formula ##SPC1##Wherein A is ##EQU1## or WHERE Z is hydrogen or methyl, andR.sub.1 is halogen or, when A is ##EQU2## also hydrogen, THE COMPOUNDS ARE USEFUL AS ANTIPHLOGISTICS.
摘要翻译：式WHEREIN A的化合物是Z CH 3 | | C = CH-CH 2 - 或-C = CH-或者其中Z是氢或甲基，并且R 1是卤素，或者当A是Z | -C = CH-CH 2 - ，也是氢，化合物作为抗肿瘤药物有用。

49. 发明授权

US4259336A 4-Hydroxy-2H-[1]-benzothieno [2,3-e]-1,2-thiazine-3-carboxamide-1,1-dioxides and salts thereof 失效
标题翻译： 4-羟基-2H- [1] - 苯并噻吩并[2,3-e] -1,2-噻嗪-3-甲酰胺-1,1-二氧化物及其盐
公开(公告)号：US4259336A
公开(公告)日：1981-03-31
申请号：US86743
申请日：1979-10-22
申请人： Wolfhard Engel , Gunter Trummlitz , Ernst Seeger , Walter Haarmann , Gunther Engelhardt , Rainer Zimmermann
发明人： Wolfhard Engel , Gunter Trummlitz , Ernst Seeger , Walter Haarmann , Gunther Engelhardt , Rainer Zimmermann
IPC分类号： A61K31/54 , A61P9/08 , A61P9/10 , A61P29/00 , C07D333/70 , C07D513/04 , A61K31/38
CPC分类号： C07D513/04 , C07D333/70 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or alkyl of 1 to 3 carbon atoms; R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms; andR.sub.3 is aromatic hydrocarbyl of 6 to 10 carbon atoms or an aromatic heterocycle of 2 to 9 carbon atoms and 1 to 2 nitrogen atoms and/or an oxygen or a sulfur atom, where each of said aromatic substituents may in turn be substituted with one or two alkyls of 1 to 6 carbon atoms, halogen, hydroxyl, trifluoromethyl, halophenyl or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases; the compounds as well as their salts are useful as analgesics, antipyretics, antithrombotic and antiphlogistics.
摘要翻译：其中R 1是氢，卤素或1至3个碳原子的烷基; R2是氢或1至3个碳原子的烷基; 并且R 3是6至10个碳原子的芳族烃基或2至9个碳原子和1至2个氮原子和/或氧或硫原子的芳族杂环，其中每个所述芳族取代基可以依次被一个或两个1至6个碳原子的烷基，卤素，羟基，三氟甲基，卤代苯基或具有1至3个碳原子的烷氧基; 和与无机或有机碱形成的无毒的，药理学上可接受的盐; 化合物及其盐可用作镇痛药，解热药，抗血栓和消炎药。

50. 发明授权

US4233299A 4-Hydroxy-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxides and salts thereof 失效
标题翻译： 4-羟基-2H-1,2-苯并噻嗪-3-甲酰胺-1,1-二氧化物及其盐
公开(公告)号：US4233299A
公开(公告)日：1980-11-11
申请号：US966963
申请日：1978-12-06
申请人： Gunter Trummlitz , Wolfhard Engel , Ernst Seeger , Gunther Engelhardt
发明人： Gunter Trummlitz , Wolfhard Engel , Ernst Seeger , Gunther Engelhardt
IPC分类号： A61K31/427 , A61K31/54 , A61K31/5415 , A61P29/00 , C07D275/06 , C07D279/02 , C07D417/12 , C07D513/14 , A61K31/38
CPC分类号： C07D275/06 , C07D279/02 , C07D417/12 , C07D513/14
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, methyl or ethyl;R.sub.2 is methyl, ethyl or n-propyl; andY is hydrogen, methyl, methoxy, fluorine or chlorine;and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as antiphlogistics.
摘要翻译：其中R 1是氢，甲基或乙基; R2是甲基，乙基或正丙基; Y为氢，甲基，甲氧基，氟或氯; 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。

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