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1. 发明授权

US4313931A Fused dibenzo imidazolo compounds, compositions and use 失效
标题翻译：稠合二苯并咪唑化合物，组合物和用途
公开(公告)号：US4313931A
公开(公告)日：1982-02-02
申请号：US236818
申请日：1981-02-23
申请人： Gerhard Walther , Claus S. Schneider , Karl-Heinz Weber , Armin Fugner
发明人： Gerhard Walther , Claus S. Schneider , Karl-Heinz Weber , Armin Fugner
IPC分类号： A61K31/5365 , A61K31/542 , A61K31/55 , A61P7/02 , A61P11/06 , A61P17/00 , A61P27/02 , A61P31/16 , A61P37/08 , A61P43/00 , C07D223/20 , C07D267/20 , C07D281/16 , C07D487/04 , C07D498/04 , C07D513/04 , A61K31/535 , A61K31/415
CPC分类号： C07D487/04 , C07D223/20 , C07D267/20 , C07D281/16 , C07D513/04 , Y10S514/826 , Y10S514/849 , Y10S514/912
摘要： This invention relates to a compound of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4, which may be the same or different, each represent a hydrogen or halogen atom or an alkyl or alkoxy group of from 1 to 6 carbon atoms;R.sub.5 and R.sub.6, which may be the same or different, each represent a hydrogen atom, an alkyl group of from 1 to 6 carbon atoms, or an alkenyl group of from 3 to 6 carbon atoms, or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached represent a pyrrolidino, piperidino, or morpholino group; andX represents oxygen, sulfur, or a methylene group,or a non-toxic, pharmacologically acceptable acid addition salt thereof, or a racemate, enantiomer, or mixture of enantiomers thereof. The compounds of Formula I are useful in pharmaceutical compositions for treating bronchial asthma and allergic bronchitis.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，R 3和R 4可以相同或不同，分别表示氢或卤素原子或烷基或烷氧基， 6个碳原子; R 5和R 6可以相同或不同，分别表示氢原子，1〜6个碳原子的烷基或3〜6个碳原子的链烯基，或者R5和R6与氮原子一起它们所连接的表示吡咯烷基，哌啶子基或吗啉基; X表示氧，硫或亚甲基，或其无毒的药学上可接受的酸加成盐，或其外消旋物，对映异构体或其对映异构体的混合物。式I的化合物可用于治疗支气管哮喘和过敏性支气管炎的药物组合物。

2. 发明授权

US4686219A 11-(Piperazin- or homopiperazin-1-yl)-5H-imidazo-(2,1-C)(1,4)benzodiazepines useful as anti-allergics 失效
标题翻译：可用作抗过敏剂的11-（哌嗪或高哌嗪-1-基）-5H-咪唑并 - （2,1-C）（1,4）苯并二氮杂
公开(公告)号：US4686219A
公开(公告)日：1987-08-11
申请号：US827849
申请日：1986-02-07
申请人： Gerhard Walther , Claus Schneider , Karl-Heinz Weber , Armin Fugner
发明人： Gerhard Walther , Claus Schneider , Karl-Heinz Weber , Armin Fugner
IPC分类号： A61K31/55 , A61P25/02 , A61P25/04 , A61P25/20 , A61P37/08 , A61P43/00 , C07D233/90 , C07D487/04 , A61K31/33 , C07D487/14
CPC分类号： C07D487/04 , C07D233/90
摘要： Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, trifluoromethyl, hydroxyl, nitro, amino, cyano, methylsulfonamido, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 3 carbon atoms, (alkyl of 1 to 3 carbon atoms)thio or (alkanoyl of 2 to 4 carbon atoms)amino;R.sub.3 is hydrogen, fluorine, chlorine, bromine or alkyl of 1 to 3 carbon atoms;R.sub.4 is hydrogen, alkyl of 1 to 4 carbon atoms, hydroxy(alkyl of 2 to 4 carbon atoms), (alkoxy of 1 to 2 carbon atoms)-(alkyl of 2 to 4 carbon atoms), alkenyl of 3 to 6 carbon atoms, alkynyl of 3 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, (cycloalkyl of 3 to 7 carbon atoms)-(alkyl of 1 to 3 carbon atoms) or (unsubstituted or substituted phenyl)-(alkyl of 1 to 3 carbon atoms) where the substituent is fluorine, chlorine, bromine, methyl, methoxy, hydroxyl or trifluoromethyl; andn is 1 or 2;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiallergic.
摘要翻译：其中R 1和R 2可以相同或不同，各自为氢，氟，氯，溴，三氟甲基，羟基，硝基，氨基，氰基，甲基亚磺酰氨基，1至4的烷基碳原子，1至3个碳原子的烷氧基，（1至3个碳原子的烷基）硫代或（2至4个碳原子的烷酰基）氨基; R3是氢，氟，氯，溴或1至3个碳原子的烷基; R4为氢，1至4个碳原子的烷基，羟基（2至4个碳原子的烷基），（1至2个碳原子的烷氧基） - （2至4个碳原子的烷基），3至6个碳原子的链烯基 3〜6个碳原子的炔基，3〜7个碳原子的环烷基，3〜7个碳原子的环烷基，1〜3个碳原子的烷基或（未取代或取代的苯基） - （1〜3的烷基）碳原子），其中取代基是氟，氯，溴，甲基，甲氧基，羟基或三氟甲基; n为1或2; 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过敏药。

3. 发明授权

US5688802A Bornyl xanthine derivatives with adenosine-antagonistic activity 失效
标题翻译：具有腺苷拮抗作用的牛磺酸黄嘌呤衍生物
公开(公告)号：US5688802A
公开(公告)日：1997-11-18
申请号：US663417
申请日：1996-06-14
申请人： Ulrike Kufner-Muhl , Karl-Heinz Weber , Gerhard Walther , Werner Stransky , Helmut Ensinger , Gunter Schingnitz , Franz Josef Kuhn , Erich Lehr
发明人： Ulrike Kufner-Muhl , Karl-Heinz Weber , Gerhard Walther , Werner Stransky , Helmut Ensinger , Gunter Schingnitz , Franz Josef Kuhn , Erich Lehr
IPC分类号： C07D473/06 , A61K31/495 , A61K31/52 , A61K31/522 , A61P9/00 , A61P11/08 , A61P25/00 , A61P25/02 , C07D473/08 , C07D519/00 , C07H19/04
CPC分类号： C07D473/08 , C07D473/06
摘要： The invention relates to new xanthine derivatives of general formula I, processes for preparing them and their use as pharmaceutical compositions.
摘要翻译：本发明涉及通式I的新型黄嘌呤衍生物，其制备方法及其作为药物组合物的用途。

4. 发明授权

US4732900A 1,2,4-triazolo-carbamates 失效
标题翻译： 1,2,4-三唑并 - 氨基甲酸酯
公开(公告)号：US4732900A
公开(公告)日：1988-03-22
申请号：US791184
申请日：1985-10-25
申请人： Karl-Heinz Weber , Dieter Hinzen , Franz-Josef Kuhn , Erich Lehr , Wilhelm Frolke , Wolfgang Troger , Helmut Ensinger , Gerhard Walther , Albrecht Harreus
发明人： Karl-Heinz Weber , Dieter Hinzen , Franz-Josef Kuhn , Erich Lehr , Wilhelm Frolke , Wolfgang Troger , Helmut Ensinger , Gerhard Walther , Albrecht Harreus
IPC分类号： A61K31/41 , A61K31/4196 , A61K31/44 , A61K31/4427 , A61K31/445 , A61P21/00 , A61P25/02 , A61P25/20 , A61P25/26 , A61P25/28 , C07D213/74 , C07D249/12 , C07D401/04 , C07D401/14 , C07D401/12
CPC分类号： C07D213/74 , C07D249/12 , C07D401/04
摘要： New 1,2,4-triazolo-carbamates of general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings given in the specification, are acetylcholinesterase inhibitors and may be used as drugs for the treatment of senile dementia.
摘要翻译：通式为“IMAGE”I的新的1,2,4-三唑并 - 氨基甲酸酯其中R1，R2，R3和R4具有说明书中给出的含义，是乙酰胆碱酯酶抑制剂，可用作治疗老年痴呆的药物。

5. 发明授权

US4670456A 4-Aminocarbonylaminomethyl-1-benzylpyrrolidin-2-ones as nootropic agents and as agents for treating cerebral insufficiency 失效
标题翻译： 4-氨基羰基氨基甲基-1-苄基吡咯烷-2-酮作为助推剂和作为治疗脑功能不全的药物
公开(公告)号：US4670456A
公开(公告)日：1987-06-02
申请号：US738152
申请日：1985-05-24
申请人： Karl-Heinz Weber , Claus Schneider , Gerhard Walther , Dieter Hinzen , Franz J. Kuhn , Erich Lehr , Helmut Ensinger , Wolfgang Troger
发明人： Karl-Heinz Weber , Claus Schneider , Gerhard Walther , Dieter Hinzen , Franz J. Kuhn , Erich Lehr , Helmut Ensinger , Wolfgang Troger
IPC分类号： A61K31/40 , A61K31/4015 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61P25/00 , A61P25/28 , C07D207/26 , C07D401/12 , C07D413/12 , C07D451/02 , C07D487/08 , C07D207/12
CPC分类号： C07D207/26 , C07D401/12 , C07D413/12 , C07D451/02
摘要： The invention relates to new substituted pyrrolidinones of general formula ##STR1## wherein R.sub.1 represents a phenyl group which may be mono- or di-substituted by methyl, methoxy, fluorine, chlorine, bromine or trifluoromethyl, or a pyridyl group;R.sub.2 represents hydrogen or a straight-chained or branched alkyl group with 1-4 carbon atoms;R.sub.3 represents a straight-chained or branched alkyl group with 1-3 carbon atoms, a hydroxyalkyl group with 2-3 carbon atoms, a phenyl group which can be mono- or di-substituted by chlorine, bromine, methyl or methoxy, a cyclohexyl group or a dialkylamino alkyl group, where in each alkyl group can contain from 1-3 carbon atoms;R.sub.4 represents hydrogen or a straight-chained or branched alkyl group with 1-3 carbon atoms; orR.sub.3 and R.sub.4 together with the nitrogen atom represent a piperidine, morpholine or piperazine ring, while the ring may be substituted by 1 or 2 methyl groups and the piperazine ring at the nitrogen atom in 4-position may also carry a phenyl, chlorophenyl or benzyl group, or they may represent the nortropanyl group, processes for preparing them and pharmaceutical compositions.The new compounds have proved effective in animal trials in alleviating or remedying conditions or restricted cerebral performance.
摘要翻译：本发明涉及通式为（I）的新的取代的吡咯烷酮，其中R 1表示可被甲基，甲氧基，氟，氯，溴或三氟甲基或吡啶基单取代或二取代的苯基; R 2表示氢或具有1-4个碳原子的直链或支链烷基; R3表示具有1-3个碳原子的直链或支链烷基，具有2-3个碳原子的羟烷基，可被氯，溴，甲基或甲氧基单取代或二取代的苯基，环己基基团或二烷基氨基烷基，其中在每个烷基中可以含有1-3个碳原子; R4表示氢或具有1-3个碳原子的直链或支链烷基; 或者R3和R4与氮原子一起代表哌啶，吗啉或哌嗪环，而环可以被1或2个甲基取代，4-位氮原子上的哌嗪环也可以带有苯基，氯苯基或或它们可以代表异丙基丙基，其制备方法和药物组合物。新化合物已被证明在动物试验中有效减轻或补救病症或限制脑部表现。

6. 发明授权

US4623646A PAF-antagonistic diazepines, methods of use 失效
标题翻译： PAF拮抗二氮杂，使用方法
公开(公告)号：US4623646A
公开(公告)日：1986-11-18
申请号：US782648
申请日：1985-10-01
申请人： Jorge Casals-Stenzel , Karl-Heinz Weber , Gerhard Walther , Albrecht Harreus , Gojko Muacevic
发明人： Jorge Casals-Stenzel , Karl-Heinz Weber , Gerhard Walther , Albrecht Harreus , Gojko Muacevic
IPC分类号： C07D495/04 , A61K31/55 , A61P7/02 , A61P11/08 , A61P43/00 , C07D243/12 , C07D471/04 , C07D487/04 , C07D495/14 , C07D513/04
CPC分类号： A61K31/55
摘要： The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I. ##STR1## wherein A is an anellated and optionally substituted benzene or 5- or 6- membered heterocyclic ring; R.sub.5 and Z are each independently hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, alkenyl or alkynyl; R.sub.6 is an optionally substituted phenyl, or is thienyl or .alpha.-pyridyl; Y is ##STR2## and nontoxic, pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明公开了一种通过用式I化合物处理个体来治疗患有对PAF-拮抗剂活性有反应作用的病症的个体的方法。其中A是一种有一定义的任选取代的苯或5-或6-元杂环 ; R 5和Z各自独立地为氢或任选取代的C 1 -C 8烷基，烯基或炔基; R6是任选取代的苯基，或是噻吩基或α-吡啶基; Y是及其无毒的药学上可接受的酸加成盐。

7. 发明授权

US4621083A PAF-antagonistic diazepines 失效
标题翻译： PAF拮抗二氮杂
公开(公告)号：US4621083A
公开(公告)日：1986-11-04
申请号：US782632
申请日：1985-10-01
申请人： Jorge Casals-Stenzel , Karl-Heinz Weber , Gerhard Walther , Albrecht Harreus , Gojko Muacevic
发明人： Jorge Casals-Stenzel , Karl-Heinz Weber , Gerhard Walther , Albrecht Harreus , Gojko Muacevic
IPC分类号： C07D495/04 , A61K31/55 , A61P7/02 , A61P11/00 , A61P11/08 , A61P37/08 , A61P43/00 , C07D487/04 , C07D487/14 , C07D495/14 , C07D495/22 , C07D513/14 , A61K31/65
CPC分类号： A61K31/55
摘要： The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I or II: ##STR1## wherein A is an annealed and optionally substituted benzene or 5- or 6-membered heterocyclic ring; B is an optionally substituted 5-membered heterocyclic ring; R.sub.5 and R.sub.7 are each independently hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, alkenyl or alkynyl; R.sub.6 is an optionally substituted phenyl, or is thienyl or .alpha.-pyridyl; and non-toxic, pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明公开了通过用式I或II化合物处理个体来治疗患有对PAF-拮抗剂活性有反应作用的病症的个体的方法：其中A是退火和任选取代的苯或5-或6-元杂环 B是任选取代的5元杂环; R 5和R 7各自独立地为氢或任选取代的C 1 -C 8烷基，烯基或炔基; R6是任选取代的苯基，或是噻吩基或α-吡啶基; 及其无毒的药学上可接受的酸加成盐。

8. 发明授权

US4550106A 4-Phenyl-4,5,6,7-tetrahydro-thieno[2,3-c]pyridines and salts thereof, compositions and use 失效
标题翻译： 4-苯基-4,5,6,7-四氢 - 噻吩并[2,3-c]吡啶及其盐，组合物和用途
公开(公告)号：US4550106A
公开(公告)日：1985-10-29
申请号：US630376
申请日：1984-07-23
申请人： Claus Schneider , Gerhard Walther , Karl-Heinz Weber , Wolf D. Bechtel , Karin Boke-Kuhn
发明人： Claus Schneider , Gerhard Walther , Karl-Heinz Weber , Wolf D. Bechtel , Karin Boke-Kuhn
IPC分类号： A61K31/435 , A61P25/24 , A61P25/26 , C07D495/04 , A61K31/44 , A61K31/535
CPC分类号： C07D495/04
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is amino, acetylamino, hydroxymethyl, methoxymethyl or ##STR2## R.sub.2 and R.sub.3, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, trifluoromethyl, hydroxyl, methoxy, methyl or ethyl;R.sub.4 is straight or branched alkyl of 1 to 3 carbon atoms; andR.sub.5 and R.sub.6, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms or, together with each other and the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic ring where, in the case of a 6-membered ring, a --CH.sub.2 -group in the ring may be replaced by an oxygen atom,and non-toxic, pharmacologically acceptable salts thereof. The compounds as well as their salts are useful as antidepressants.
摘要翻译：其中R 1是氨基，乙酰氨基，羟甲基，甲氧基甲基或者R 2可以相同或不同的式（I）化合物分别是氢，氟，氯，溴，三氟甲基，羟基，甲氧基，甲基或乙基; R4是1〜3个碳原子的直链或支链烷基; 和可以相同或不同的R 5和R 6各自为氢或1至4个碳原子的烷基，或彼此连接并与它们相连的氮原子形成5-，6- 或7-元杂环，其中在6元环的情况下，环中的-CH 2 - 基可被氧原子取代，及其无毒的药学上可接受的盐。化合物及其盐可用作抗抑郁药。

9. 发明授权

US5155103A Methods of using new thieno-triazole-1,4-diazepino-2-carboxylic acid amides 失效
标题翻译：使用新的噻吩并三唑-1,4-二氮杂-2-羧酸酰胺的方法
公开(公告)号：US5155103A
公开(公告)日：1992-10-13
申请号：US774683
申请日：1991-10-11
申请人： Karl-Heinz Weber , Albrecht Harreus , Jorge Casals-Stenzel , Gojko Muacevic , Wolfgang Troger , Gerhard Walther
发明人： Karl-Heinz Weber , Albrecht Harreus , Jorge Casals-Stenzel , Gojko Muacevic , Wolfgang Troger , Gerhard Walther
IPC分类号： A61K31/55 , A61K31/5517 , A61P7/02 , A61P9/02 , A61P11/08 , A61P29/00 , A61P37/00 , A61P37/08 , C07C235/40 , C07D243/00 , C07D249/08 , C07D333/00 , C07D333/36 , C07D495/00 , C07D495/04 , C07D495/14
CPC分类号： C07D495/04 , C07D333/36 , C07D495/14
摘要： The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably Cl or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R.sub.2 and R.sub.3, each independently, represent hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or the two groups R.sub.2 and R.sub.3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C.sub.1 -C.sub.4 alkyl, preferably a methyl group;R.sub.4 represents alpha-pyridyl or a phenyl in which the phenyl ring can be substituted preferably in the 2-position, by methyl, halogen, preferably chlorine or bromine, nitro or trifluoromethyl;n represents one of the numbers 0, 1, 2, 3, 4, 5, 6, 7 or 8; and novel intermediates therefor.The compounds of formula I are useful in the treatment of pathological conditions and diseases in which platelet activating factor is implicated.
摘要翻译：本发明涉及式I的新的噻吩并三唑并-1,4-二氮杂-2-羧酸酰胺其中R 1表示氢，可以任意被C 1 -C 4直链或支链烷基取代的C 1 -C 4直链或支链烷基卤素，优选Cl或Br，或羟基，环丙基，C 1 -C 3烷氧基，优选甲氧基或卤素，优选氯或溴; R2和R3各自独立地代表氢，C1-C4直链或支链烷基，C1-C4羟基烷基或两个R2和R3与氮原子一起表示5-，6-或7-元环，其中任选地含有氮，氧或硫原子作为另外的杂原子，第二氮原子任选被C 1 -C 4烷基，优选甲基取代; R4表示α-吡啶基或苯基，其中苯环优选在2-位上被甲基，卤素，优选氯或溴，硝基或三氟甲基取代; n表示数字0,1,2,3,4,5,6,7或8中的一个; 及其新型中间体。式I化合物可用于治疗涉及血小板活化因子的病理状况和疾病。

10. 发明授权

US5149808A N-heterocyclic substituted -pyrrolidin-2-ones 失效
标题翻译： N-杂环取代的吡咯烷-2-酮
公开(公告)号：US5149808A
公开(公告)日：1992-09-22
申请号：US755039
申请日：1991-09-04
申请人： Karl-Heinz Weber , Gerhard Walther , Claus Schneider , Dieter Hinzen , Franz J. Kuhn , Erich Lehr
发明人： Karl-Heinz Weber , Gerhard Walther , Claus Schneider , Dieter Hinzen , Franz J. Kuhn , Erich Lehr
IPC分类号： C07D207/26 , C07D401/06 , C07D521/00
CPC分类号： C07D207/26 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms; R.sub.2 is 2-, 3- or 4-pyridyl, phenyl or mono- or di-substituted phenyl, where the substituents are each individually alkoxy of 1 to 2 carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, alkyl or 1 to 4 carbon atoms, hydroxyl or nitro; andR.sub.3 and R.sub.4 are each independently hydrogen or alkyl of 1 to 4 carbon atoms; orR.sub.3 and R.sub.4, together with each other and the nitrogen atom to which they are attached, form an unsubstituted or methyl-substituted, saturated 5- or 6-membered heterocycle which may contain an additional oxygen or nitrogen heteroatom, or form an imidazole ring;where the aminomethyl substituent is attached to the 4- or 5-position or the pyrrolidine ring, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as nootropics and antihypoxics.
摘要翻译：其中R 1为氢或1至4个碳原子的烷基的式IMA化合物; R2是2-，3-或4-吡啶基，苯基或单取代或二取代的苯基，其中取代基各自为1至2个碳原子的烷氧基，氟，氯，溴，三氟甲基，烷基或1至4个碳原子，羟基或硝基; 并且R 3和R 4各自独立地为氢或1至4个碳原子的烷基; 或R 3和R 4彼此连接并与它们所连接的氮原子形成未取代的或甲基取代的饱和的5-或6-元杂环，其可以含有另外的氧或氮杂原子，或形成咪唑环 ; 其中氨基甲基取代基连接到4-或5-位或吡咯烷环上，以及无毒的药学上可接受的酸加成盐。这些化合物以及盐类可用作神经递质和抗缺氧剂。

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