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41. 发明授权

US3966916A N(6)-disubstituted adenoisine compounds and therapeutic compositions 失效
标题翻译： N（6） - 二取代腺苷化合物和治疗组合物
公开(公告)号：US3966916A
公开(公告)日：1976-06-29
申请号：US525795
申请日：1974-11-21
申请人： Wolfgang Kampe , Erich Fauland , Kurt Stach , Harald Stork , Felix Helmut Schmidt
发明人： Wolfgang Kampe , Erich Fauland , Kurt Stach , Harald Stork , Felix Helmut Schmidt
IPC分类号： C07H19/16 , A61K31/70
CPC分类号： C07H19/16
摘要： New N(6)-disubstituted adenosine compound of the formula ##SPC1##WhereinR.sub.1 is lower alkyl substituted by at least one of hydroxyl, alkoxy or acyloxy; or is cycloalkyl or straight-chained or branched lower alkenyl;R.sub.2 and R.sub.3 are hydrogen, halogen, or nitro or lower alkyl, alkoxy or alkylthio andR.sub.4 is hydrogen or acyl; when R.sub.4 is acyl, R.sub.1 can also be lower alkyl;And the pharmacologicaly compatible salts thereof; exhibits shown anti-lipolytic, anti-hyperlipaemic and anti-hypercholesterolaemic action.
摘要翻译：新的N（6） - 二取代的腺苷化合物，式WHERE R1是被羟基，烷氧基或酰氧基中的至少一个取代的低级烷基; 或是环烷基或直链或支链低级链烯基; R2和R3是氢，卤素或硝基或低级烷基，烷氧基或烷硫基，R4是氢或酰基; 当R 4是酰基时，R 1也可以是低级烷基; 及其药理学兼容性; 展示了抗脂肪，抗高血压和抗高血脂药物作用。

42. 发明授权

US5399575A Pyridine compounds which have useful pharmaceutical activity 失效
标题翻译：具有有用药物活性的吡啶化合物
公开(公告)号：US5399575A
公开(公告)日：1995-03-21
申请号：US66058
申请日：1993-06-14
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Marcel Linssen , Otto-Henning Wilhelms
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Marcel Linssen , Otto-Henning Wilhelms
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61P37/08 , C07D213/30 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/89 , C07D401/04 , C07D401/10 , C07D401/12 , C07D213/54
CPC分类号： C07D213/30 , C07D213/55 , C07D213/56 , C07D213/57 , C07D401/12
摘要： Compounds of the formula I ##STR1## in which A signifies an alkylene radical with 1 to 3 carbon atoms or a group --CH.dbd.CH--, B an oxygen atom or a valency bond, m a whole number from 0 to 5, n the number 0 or 1, X a valency bond, an oxygen atom or a sulphur atom, Y a valency bond or a phenylene radical substituted, if desired, one or more times by C.sub.1 - to C.sub.6 -alkyl, C.sub.1 - to C.sub.6 -alkoxy, halogen, hydroxyl or aminocarbonyl, Z hydrogen, halogen, C.sub.1 - to C.sub.6 -alkyl or cyano and R a group CN, COOH, COOC.sub.1 - to C.sub.6 -alkyl, CONH-tetrazolyl, CON(OH)(C.sub.1 -C.sub.6 -alkyl) or 5-(1H)-tetrazolyl, as well as, for the case that Y represents a phenylene radical, also hydrogen, with the exception of the compound 4-[2-(4)-pyridinovinyl]-carboxymethoxybenzene, their physiologically compatible salts and processes for their preparation, as well as medicaments containing these compounds for the treatment of allergic diseases.
摘要翻译： PCT No.PCT / EP91 / 02249 Sec。 371日期：1993年6月14日 102（e）日期1993年6月14日PCT 1991年11月28日PCT PCT。第WO92 / 09598号公报日期：1992年6月11日。式I的化合物（I）其中A表示具有1至3个碳原子的亚烷基或基团-CH = CH-，B为氧原子或价键， 0至5的整数，n为0或1，X为价键，氧原子或硫原子，Y为化合键或亚苯基，如果需要，可以被C 1 -C 6 - 烷基，C 1至C 6 - 烷氧基，卤素，羟基或氨基羰基，Z氢，卤素，C 1至C 6 - 烷基或氰基，R a基团CN，COOH，COOC 1 -C 6烷基，CONH-四唑基，CON ）（C 1 -C 6 - 烷基）或5-（1H） - 四唑基，以及对于Y代表亚苯基的情况，也是氢，除了化合物4- [2-（4） - 吡啶基乙烯基 ] - 羧甲氧基苯，它们的生理上相容的盐及其制备方法，以及含有这些化合物用于治疗过敏性疾病的药物。

43. 发明授权

US5025028A Tetrazolyl substituted thioethers, pharmaceutical compositions and anti-allergic use thereof 失效
标题翻译：四唑基取代的硫醚，药物组合物和抗过敏应用
公开(公告)号：US5025028A
公开(公告)日：1991-06-18
申请号：US466197
申请日：1990-01-17
申请人： Erhard Reinholz , Walter-Gunar Friebe , Wolfgang Kampe , Jurgen Mertin , Otto-Henning Wilhelms
发明人： Erhard Reinholz , Walter-Gunar Friebe , Wolfgang Kampe , Jurgen Mertin , Otto-Henning Wilhelms
IPC分类号： A61K31/10 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/235 , A61K31/26 , A61K31/275 , A61K31/41 , A61P11/00 , A61P29/00 , A61P37/08 , C07C67/00 , C07C313/00 , C07C315/02 , C07C317/18 , C07C317/44 , C07C323/12 , C07C323/14 , C07C323/20 , C07C323/52 , C07C323/54 , C07C323/60 , C07C325/00 , C07C331/04 , C07D257/04 , C07D257/06
CPC分类号： C07D257/04 , A61K31/10 , A61K31/26 , A61K31/275 , C07C323/12 , C07C323/52 , C07C323/60 , C07C331/04 , C07D257/06
摘要： The present invention provides compounds of the general formula: ##STR1## wherein Ar is a phenyl radical optionally substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen, A is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 aliphatic hydrocarbon radical which is optionally substituted by a hydroxyl group, n is 0, 1 or 2, B is a straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.8 -aliphatic hydrocarbon radical and R is 5-(1H)-tetrazolyl, --CO--NH-tetrazolyl, ##STR2## Cn, SCN, OH, halogen, 5-(1H)-tetrazolylthio, ##STR3## or CO--O--NH--R.sub.1, wherein R.sub.1 is a hydrogen atom, an alkyl radical optionally substituted by cycloalkyl or an alkenyl, cycloalkyl, aralkyl or aryl radical, wherein the aromatic moiety can be substituted by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen; and the pharmacologically acceptable salts thereof. The present invention also provides processes for preparing these compounds and pharmaceutical compositions containing them for combating allergic diseases.

44. 发明授权

US4621098A Thioethers and pharmaceutical compositions containing them 失效
标题翻译：硫醚和含有它们的药物组合物
公开(公告)号：US4621098A
公开(公告)日：1986-11-04
申请号：US626690
申请日：1984-07-02
申请人： Robert Umminger , Walter-Gunar Friebe , Wolfgang Kampe , Androniki Roesch , Otto-Henning Wilhelms
发明人： Robert Umminger , Walter-Gunar Friebe , Wolfgang Kampe , Androniki Roesch , Otto-Henning Wilhelms
IPC分类号： C07D295/12 , A61K31/04 , A61K31/10 , A61K31/12 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/22 , A61K31/535 , A61K31/5375 , A61P37/08 , C07C67/00 , C07C313/00 , C07C315/02 , C07C317/00 , C07C317/04 , C07C317/18 , C07C319/14 , C07C321/28 , C07C323/07 , C07C323/12 , C07C323/14 , C07C323/20 , C07C323/22 , C07C323/25 , C07C323/36 , C07C323/52 , C07C323/58 , C07C323/62 , C07C323/65 , C07D295/18 , C07D295/185 , C07C147/107
CPC分类号： C07D295/185 , C07C317/00 , C07C321/00 , C07C323/00 , C07C323/25
摘要： The present invention provides thioethers of the general formula: ##STR1## wherein Ar is a phenyl radical which is optionally substituted one, two or three times by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen, Q is an oxygen or sulphur atom or an NH group, A is a straight-chained or branched C.sub.2 -C.sub.8 alkylene radical which is optionally substituted by a hydroxyl group or can be interrupted by an ethenylene or ethynylene group, n is 0, 1 or 2, and R is a hydrogen atom or a straight-chained or branched alkyl radical which is optionally substituted one or more times by the same or different radicals selected from alkoxycarbonyl, alkoxy, hydroxyl, carboxyl or optionally substituted carbamoyl or amino; as well as the pharmacologically acceptable salts thereof, with the proviso that A cannot be ethylene when Ar is a phenyl radical, Q is an oxygen atom and R is the group --CH.sub.2 COOH.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要翻译：本发明提供以下通式的硫醚：其中Ar是任选被烷基，烯基，烷氧基，烷硫基，烷酰基，羟基，羟基烷基，羧基，烷氧基羰基任选取代一至两次的苯基，氨基甲酰基，硝基，氨基或卤素，Q是氧或硫原子或NH基团，A是任选被羟基取代的直链或支链C 2 -C 8亚烷基，或可被亚乙烯或亚乙炔基，n为0,1或2，R为氢原子或直链或支链烷基，其任选被相同或不同的选自烷氧基羰基，烷氧基，羟基，羧基或基团的基团取代一次或多次任选取代的氨基甲酰基或氨基; 以及其药理学上可接受的盐，条件是当Ar为苯基时A不能为乙烯，Q为氧原子，R为基团-CH 2 COOH。本发明还提供了制备这些化合物的方法和含有它们的药物组合物。

45. 发明授权

US4397848A N-Substituted aziridine-2-carboxylic acid immunostimulant derivatives 失效
标题翻译： N-取代的氮丙啶-2-羧酸免疫刺激剂衍生物
公开(公告)号：US4397848A
公开(公告)日：1983-08-09
申请号：US236375
申请日：1981-02-20
申请人： Elmar Bosies , Wolfgang Kampe , Max Thiel , Uwe Bicker , Dietmar Boerner
发明人： Elmar Bosies , Wolfgang Kampe , Max Thiel , Uwe Bicker , Dietmar Boerner
IPC分类号： A61K31/395 , A61K31/396 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/505 , A61P35/00 , A61P37/00 , A61P37/06 , C07D203/22 , C07D401/12 , C07D403/12 , C07D405/12
CPC分类号： C07D203/22 , Y10S514/885
摘要： The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, or an optionally substituted aliphatic hydrocarbon radical or cycloalkyl or cycloalkenyl radical, and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.
摘要翻译：本发明提供含有下列通式的N-取代的氮丙啶-2-羧酸衍生物的药物组合物：其中X是羧基，氰基，烷氧基羰基或任选取代的氨基甲酰基，R是氢原子或任选取代的脂族烃基或环烷基或环烯基，R 1为氢原子或烷基或苯基; 和其药学上可接受的盐，与药物稀释剂或载体混合。本发明还提供了作为新化合物的通式（I'）的N-取代的氮丙啶-2-羧酸衍生物，但条件是当X是氨基甲酰基或烷氧基羰基并且R 1是氢原子时，R不是甲基，乙基，异丙基或苄基; 及其药理学上可接受的盐，也提供制备这些新化合物的方法。此外，本发明涉及通式（I'）的化合物及其药理学上可接受的盐在与免疫系统的弱化相关的疾病中的用途。

46. 发明授权

US4370323A 2-Cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methanes 失效
标题翻译： 2-氰基氮丙啶基 - （1）-2-取代的吖丙啶基 - （1） - 甲烷
公开(公告)号：US4370323A
公开(公告)日：1983-01-25
申请号：US776068
申请日：1977-03-09
申请人： Wolfgang Kampe , Max Thiel , Erich Fauland , Uwe Bicker , Gottfried Hebold
发明人： Wolfgang Kampe , Max Thiel , Erich Fauland , Uwe Bicker , Gottfried Hebold
IPC分类号： C07D203/06 , A61K31/395 , A61K31/396 , A61K31/435 , A61P35/00 , A61P37/04 , C07D203/08 , C07D203/12 , C07D203/14 , C07D333/00 , C07D335/00 , C07D403/14 , C07D405/14 , C07D409/14 , C07D451/14 , C07D403/06 , C07D401/14
CPC分类号： C07D203/08 , C07D451/14 , Y10S514/885
摘要： A 2-cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methane ##STR1## wherein R is a nitrile or carbamoyl group, andR.sub.1 and R.sub.2 each independently is a hydrogen atom, an aliphatic hydrocarbon radical containing up to 10 carbon atoms optionally substituted by hydroxyl, alkoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, cyano, 1, 2 or 3 halogens, cycloalkyl, phenyl or phenoxy; nitrile, carboxyl, alkoxycarbonyl or optionally hydrogenated monocyclic heteroaryl or phenyl optionally substituted by alkyl, alkoxy, hydroxy, alkoxcarbonyl, dialkylamino, alkylthio, trifluoromethyl, nitro, carbamoyl, nitrile, sulphonamido, hydroxyalkyl, methylenedioxy, or halogen; or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a ring containing up to 8 ring members of which at least one may be oxygen, sulphur, SO, SO.sub.2 NH, N-alkyl, N-acyl or N-alkoxycarbonylalkyl, and which can be substituted by alkyl, alkoxy, hydroxyl, alkylenedioxy, alkoxycarbonyl, hydroxyalkyl, alkoxycarbonylalkyl, dialkylamino, oxo or 2-cyanoaziridino groups, or can be fused to 1 or 2 benzene rings or can be bridged by alkylene radicals containing up to 3 carbon atoms.The compounds are characterized by cytostatic and immune response-stimulating activity.
摘要翻译： 2-氰基氮丙啶基 - （1）-2-取代的吖丙啶基 - （1） - 甲烷，其中R是腈或氨基甲酰基，R 1和R 2各自独立地为氢原子，含有至多任选被羟基，烷氧基，氨基，烷基氨基，二烷基氨基，烷氧基羰基，氰基，1,2或3卤素，环烷基，苯基或苯氧基取代的10个碳原子; 腈，羧基，烷氧基羰基或任选氢化的单环杂芳基或任选被烷基，烷氧基，羟基，烷氧基羰基，二烷基氨基，烷硫基，三氟甲基，硝基，氨基甲酰基，腈，磺酰胺基，羟烷基，亚甲二氧基或卤素取代的苯基。或R 1和R 2与它们所连接的碳原子一起形成含有至多8个环成员的环，其中至少一个可以是氧，硫，SO，SO 2 + L，NH，N-烷基，酰基或N-烷氧基羰基烷基，其可以被烷基，烷氧基，羟基，亚烷基二氧基，烷氧基羰基，羟基烷基，烷氧基羰基烷基，二烷基氨基，氧代或2-氰基氮丙啶基取代，或者可以与1或2个苯环稠合，或可以被含有至多3个碳原子的亚烷基。该化合物的特征在于细胞抑制和免疫应答刺激活性。

47. 发明授权

US4367235A 2-Benzimidazolinone compounds and therapeutic compositions 失效
标题翻译： 2-苯并咪唑啉酮化合物和治疗组合物
公开(公告)号：US4367235A
公开(公告)日：1983-01-04
申请号：US171940
申请日：1980-07-18
申请人： Carl H. Ross , Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Egon Roesch
发明人： Carl H. Ross , Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Egon Roesch
IPC分类号： A61K31/415 , A61K31/4184 , A61P9/00 , A61P25/02 , C07D235/02 , C07D235/26
CPC分类号： A61K31/415 , C07D235/02 , C07D235/26
摘要： 2-benzimidazolinone compounds of the formula ##STR1## wherein R is lower alkyl,R.sub.1 and R.sub.2, which can be the same or different, are lower straight-chained or branched alkyl and one of R.sub.1 and R.sub.2 can also be hydrogen orR.sub.1 and R.sub.2 together represent an alkylene radical and R.sub.3 is hydrogen or acyl, i.e., alkanoyl or aromatic carboxylic acid moieties;and the pharmacologically acceptable salts thereof; have marked .beta.-receptor blocking action and are outstandingly useful in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：其中R是低级烷基，可以相同或不同的R 1和R 2的低级直链或支链烷基，R 1和R 2之一也可以是氢或R 1和R 2 一起代表亚烷基，R3是氢或酰基，即烷酰基或芳族羧酸部分; 及其药理学上可接受的盐; 具有明显的β-受体阻断作用，并且在治疗或预防心脏和循环系统疾病方面非常有用。

48. 发明授权

US4284633A Derivatives of xanthine 失效
标题翻译：黄嘌呤衍生物
公开(公告)号：US4284633A
公开(公告)日：1981-08-18
申请号：US148870
申请日：1980-05-12
申请人： Walter-Gunar Friebe , Max Thiel , Wolfgang Kampe , Otto-Henning Wilhelms , Androniki Roesch
发明人： Walter-Gunar Friebe , Max Thiel , Wolfgang Kampe , Otto-Henning Wilhelms , Androniki Roesch
IPC分类号： A61K31/52 , A61K31/522 , A61P11/08 , A61P37/08 , C07D473/08 , C07D473/10 , C07D473/06
CPC分类号： C07D473/08 , C07D473/10 , Y10S514/826
摘要： The present invention provides xanthine derivatives of the general formula: ##STR1## wherein one of the symbols R.sub.1 and R.sub.2 stands for a methyl radical and the other for a radical of the general formula: ##STR2## wherein R.sub.3 is a hydrogen atom or an acyl radical; and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them and is also concerned with the use thereof for the preparation of pharmaceutical compositions for the treatment of allergies.
摘要翻译：本发明提供了以下通式的黄嘌呤衍生物：其中符号R1和R2之一代表甲基，另一个代表下列通式的基团：其中R3是氢原子或酰基激进; 及其药理学上可接受的盐。本发明还提供了制备这些化合物和含有它们的药物组合物的方法，并且还涉及其用于制备用于治疗过敏症的药物组合物的用途。

49. 发明授权

US4282212A Immune-stimulating 1-(N-acylcarbamoyl)-2-cyanoaziridines 失效
标题翻译：免疫刺激1-（N-酰基氨基甲酰基）-2-氰基氮丙啶
公开(公告)号：US4282212A
公开(公告)日：1981-08-04
申请号：US838426
申请日：1977-09-30
申请人： Herbert Berger , Rudi Gall , Wolfgang Kampe , Uwe Bicker , Gottfried Hebold
发明人： Herbert Berger , Rudi Gall , Wolfgang Kampe , Uwe Bicker , Gottfried Hebold
IPC分类号： C07D203/12 , C07D203/06 , C07D203/08 , C07D203/18 , C07D203/20 , C07D203/24 , C07D237/24 , C07D317/68 , C07D333/38 , C07D409/12 , C07D417/12 , C07F9/22 , C07F9/24 , C07F9/564 , A61K31/395
CPC分类号： C07C265/16 , C07D203/06 , C07D203/20 , C07D203/24 , C07D237/24 , C07D317/68 , C07D333/38 , C07F9/564
摘要： 1-(N-Acyl-carbamoyl)-2-cyanoaziridines of the formula ##STR1## wherein X is oxygen or sulphur,Z is hydrogen or an organic radical, andY is a carbonyl, sulphonyl, sulphinyl, sulphenyl, phosphoryl or phosphonyl radical,and salts thereof, exhibit immune-stimulating and cancerostatic activities.
摘要翻译：其中X是氧或硫，Z是氢或有机基团，Y是羰基，磺酰基，亚磺酰基，磺酰基，磷酰基或膦酰基的1-（N-酰基 - 氨基甲酰基）-2-氰基氮丙啶及其盐具有免疫刺激和癌症活性。

50. 发明授权

US4215134A 4-Hydroxy-2-benzimidazoline-thione compounds and pharmaceutical compositions containing them 失效
标题翻译： 4-羟基-2-苯并咪唑啉 - 硫酮化合物和含有它们的药物组合物
公开(公告)号：US4215134A
公开(公告)日：1980-07-29
申请号：US2129
申请日：1979-01-09
申请人： Carl H. Ross , Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Egon Roesch
发明人： Carl H. Ross , Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Egon Roesch
IPC分类号： A61K31/415 , A61K31/4184 , A61P9/00 , C07D235/02 , C07D235/28 , C07D303/22
CPC分类号： C07D235/02 , C07D235/28 , C07D303/22
摘要： Novel 4-hydroxy-2-benzimidazoline-thione compound of the formula: ##STR1## wherein R is lower alkyl;R.sub.1 and R.sub.2, which can be the same or different, are hydrogen or lower straight-chained or branched alkyl orR.sub.1 and R.sub.2 together represent alkylene; andR.sub.3 is a hydrogen atom or an acyl radical;and the pharmacologically acceptable salts thereof; have marked .beta.-receptor blocking action and are outstandingly useful in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：下式的新型4-羟基-2-苯并咪唑啉 - 硫酮化合物：其中R是低级烷基; R 1和R 2可以相同或不同，为氢或低级直链或支链烷基或R 1和R 2一起表示亚烷基; 并且R 3是氢原子或酰基; 及其药理学上可接受的盐; 具有明显的β-受体阻断作用，并且在治疗或预防心脏和循环系统疾病方面非常有用。

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