公开(公告)号：US4457927A

公开(公告)日：1984-07-03

申请号：US452009

申请日：1982-12-22

申请人： Helmut Biere ,  Joachim-Friedrich Kapp ,  Irmgard Bottcher

发明人： Helmut Biere ,  Joachim-Friedrich Kapp ,  Irmgard Bottcher

IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P25/04 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D209/38 ,  C07D213/61 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D209/38 ,  C07D213/61

摘要： Pyrido[2,1-b]quinazolinones of the formula ##STR1## wherein X is cyano, hydroxyamidocarbonyl, carbamoyl, 5-tetrazolyl, carboxy, carboxy in the form of a salt thereof with a physiologically compatible base, carboxy esterified with a physiologically acceptable alcohol or carboxy amidated with a physiologically acceptable amine;R.sub.1 is hydrogen or methyl; andR.sub.2 through R.sub.5 are independently each hydrogen, halogen, alkyl of 1-4 carbon atoms, trifluoromethyl, carboxy, thiocyano, methylthio, methylsulfinyl, methylsulfonyl, methylsulfonimidoyl or methylsulfonamido with the proviso that two or three of the groups R.sub.2 through R.sub.5 are hydrogen; or a salt thereof with a physiologically acceptable acid or base;possess valuable pharmacological properties.

摘要翻译： 其中X是氰基的吡啶并[2,1-b]喹唑啉酮，其中X是氰基，羟基酰氨基羰基，氨基甲酰基，5-四唑基，羧基，其盐与生理上相容的碱形式的羧基， 醇或羧基与生理学上可接受的胺酰胺化; R1是氢或甲基; R 2至R 5各自独立地为氢，卤素，1-4个碳原子的烷基，三氟甲基，羧基，硫氰基，甲硫基，甲基亚磺酰基，甲基磺酰基，甲基亚氨基亚氨基或甲基亚磺酰氨基，条件是R2至R5中的两个或三个为氢; 或其盐与生理上可接受的酸或碱反应; 具有宝贵的药理性质。

公开(公告)号：US4244960A

公开(公告)日：1981-01-13

申请号：US61779

申请日：1979-07-27

申请人： Eberhard Schroder ,  Clemens Rufer ,  Irmgard Bottcher ,  Joachim-Friedrich Kapp

发明人： Eberhard Schroder ,  Clemens Rufer ,  Irmgard Bottcher ,  Joachim-Friedrich Kapp

IPC分类号： C07C205/38 ,  C07C205/45 ,  C07D213/65 ,  C07D213/70 ,  A61K31/44 ,  A61K31/18 ,  C07D213/63

CPC分类号： C07D213/70 ,  C07C205/38 ,  C07C205/45 ,  C07D213/65

摘要： Indanyl derivatives of the formula ##STR1## wherein AR is phenyl, pyridyl, or phenyl or pyridyl substituted by halogen, alkyl of 1-4 carbon atoms or trifluoromethyl; X is oxygen or a sulfur; R.sub.1 is alkyl of 1-4 carbon atoms or alkyl of 1-4 carbon atoms substituted by fluorine or chlorine; A is ##STR2## Y is oxo, oximino, C.sub.1-4 -alkoximino of 1-4 carbon atoms, phenylhydrazono or p-toluenesulfonylhydrazono; n is 0, 1 or 2; R.sub.2 is alkyl of 1-4 carbon atoms, phenyl or phenyl substituted by halogen, alkyl of 1-4 carbon atoms, nitro or carboxy; Z is hydroxy, acyloxy of 1 to 6 carbon atoms, R.sub.1 SO.sub.3 -- amino, acylamino of 1 to 6 carbon atoms, R.sub.1 SO.sub.2 NH-- or cyano, and V is hydrogen, acyl of 1 to 6 carbon atoms or R.sub.1 SO.sub.2 --, and the salts thereof with physiologically acceptable bases or acids have valuable pharmacological and herbicidal activity.

摘要翻译： 其中AR为苯基，吡啶基或苯基或被卤素取代的吡啶基，1-4个碳原子的烷基或三氟甲基; X是氧或硫; R1是1-4个碳原子的烷基或被氟或氯取代的1-4个碳原子的烷基; A是CH 2 CH 2 CH 2，CHCHCH 2，Y，Y是氧代，肟基，1-4个碳原子的C1-4-肟基，苯基亚肼基或对甲苯磺酰肼; n为0,1或2; R2是1-4个碳原子的烷基，苯基或被卤素取代的苯基，1-4个碳原子的烷基，硝基或羧基; Z是羟基，1至6个碳原子的酰氧基，R1SO3-氨基，1至6个碳原子的酰氨基，R1SO2NH-或氰基，V是氢，1至6个碳原子的酰基或R1SO2-，其盐与 生理上可接受的碱或酸具有有价值的药理学和除草活性。

公开(公告)号：US4528298A

公开(公告)日：1985-07-09

申请号：US516395

申请日：1983-07-22

申请人： Ulrich Niedballa ,  Irmgard Bottcher

发明人： Ulrich Niedballa ,  Irmgard Bottcher

IPC分类号： A61K31/415 ,  A61K31/505 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C381/00 ,  C07D233/54 ,  C07D233/84 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D409/12 ,  C07D417/12

CPC分类号： C07D233/64 ,  C07C381/00 ,  C07D233/84

摘要： Imidazole derivatives of the formula ##STR1## wherein AR.sub.1 and AR.sub.2 each independently is phenyl, optionally substituted by halogen atoms, alkyl residues, alkoxy residues; or dialkylamino residues; pyridyl, furyl; or thienyl;R.sub.1 is hydrogen; alkyl of 1-6 carbon atoms optionally; substituted by hydroxy groups, alkoxy groups, or acyloxy groups; benzyl; tetrahydropyran-2-yl; or tetrahydrofuran-2-yln is 0, 1 or 2; andZ is phenyl optionally substituted by halogen atoms, alkyl groups, alkoxy groups, nitro groups, amino, acylamino groups or trifluoromethyl groups; pyridyl; N-oxypyridyl; pyrimidinyl; thiazolyl; or thienyl, and the physiologically acceptable salts thereof with acids,have valuable pharmacological activity, e.g., antiinflammatory activity.

摘要翻译： 其中AR1和AR2各自独立地是苯基，任选地被卤素原子，烷基残基，烷氧基残基取代的式（I）的咪唑衍生物; 或二烷基氨基残基; 吡啶基，呋喃基 或噻吩基; R1是氢; 1-6个碳原子的烷基; 被羟基，烷氧基或酰氧基取代; 苄基; 四氢吡喃-2-基; 或四氢呋喃-2-基n为0,1或2; Z为任选被卤素原子，烷基，烷氧基，硝基，氨基，酰氨基或三氟甲基取代的苯基; 吡啶基 N-氧吡啶基 嘧啶基; 噻唑基 或噻吩基及其与酸的生理上可接受的盐具有有价值的药理活性，例如抗炎活性。

公开(公告)号：US4269847A

公开(公告)日：1981-05-26

申请号：US41367

申请日：1979-05-22

申请人： Ulrich Niedballa ,  Irmgard Bottcher

发明人： Ulrich Niedballa ,  Irmgard Bottcher

IPC分类号： A61K31/415 ,  A61P29/00 ,  C07D233/84 ,  C07D233/88 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

CPC分类号： C07D233/84 ,  C07D233/88 ,  Y10S514/825 ,  Y10S514/826 ,  Y10S514/926 ,  Y10S514/927

摘要： Imidazole derivatives of the formula ##STR1## wherein Ar.sub.1 and Ar.sub.2 are each phenyl; phenyl substituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.2-6 dialkylamino; pyridyl; furyl; or thienyl; with the proviso that Ar.sub.1 and Ar.sub.2 are not both unsubstituted phenyl;R.sub.1 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted by hydroxy, C.sub.1-4 alkoxy or C.sub.1-6 alkanoyloxy;n is 0, 1 or 2; andZ is a C.sub.2-6 -alkyl or -alkenyl residue substituted by one or two of hydroxy, C.sub.1-4 alkoxy, C.sub.2-8 alkylenedioxy, C.sub.1-6 alkanoyloxy or benzoyloxy, or by one alkoxycarbonyl group;and the salts thereof with physiologically acceptable acids, possess valuable pharmacological properties.

摘要翻译： 其中Ar1和Ar2各自为苯基的式“IMAGE”的咪唑衍生物; 被卤素，C 1-4烷基，C 1-4烷氧基或C 2-6二烷基氨基取代的苯基; 吡啶基 呋喃 或噻吩基; 条件是Ar 1和Ar 2不是未被取代的苯基; R1是氢，C1-4烷基或被羟基，C1-4烷氧基或C1-6烷酰氧基取代的C1-4烷基; n为0,1或2; Z为被羟基，C 1-4烷氧基，C 2-8亚烷基二氧基，C 1-6烷酰氧基或苯甲酰氧基或一个烷氧基羰基中的一个或两个取代的C 2-6 - 烷基或链烯基; 其盐与生理上可接受的酸具有有价值的药理学性质。

公开(公告)号：US4440776A

公开(公告)日：1984-04-03

申请号：US361225

申请日：1982-03-24

申请人： Ulrich Niedballa ,  Irmgard Bottcher

发明人： Ulrich Niedballa ,  Irmgard Bottcher

IPC分类号： A61K31/415 ,  A61P29/00 ,  C07D233/84 ,  C07D233/88 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

CPC分类号： C07D233/84 ,  C07D233/88 ,  Y10S514/825 ,  Y10S514/826 ,  Y10S514/926 ,  Y10S514/927

摘要： Imidazole derivatives of the formula ##STR1## wherein Ar.sub.1 and Ar.sub.2 are each phenyl; phenyl substituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.2-6 dialkylamino; pyridyl; furyl; or thienyl; with the proviso that Ar.sub.1 and Ar.sub.2 are not both unsubstituted phenyl;R.sub.1 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted by hydroxy, C.sub.1-4 alkoxy or C.sub.1-6 alkanoyloxy;n is 0, 1 or 2; andZ is a C.sub.2-6 -alkyl or -alkenyl residue substituted by one or two of hydroxy, C.sub.1-4 alkoxy, C.sub.2-8 alkylenedioxy, C.sub.1-6 alkanoyloxy or benzoyloxy, or by one alkoxycarbonyl group;and the salts thereof with physiologically acceptable acids, possess valuable pharmacological properties.

摘要翻译： 其中Ar1和Ar2各自为苯基的式“IMAGE”的咪唑衍生物; 被卤素，C 1-4烷基，C 1-4烷氧基或C 2-6二烷基氨基取代的苯基; 吡啶基 呋喃 或噻吩基; 条件是Ar 1和Ar 2不是未被取代的苯基; R1是氢，C1-4烷基或被羟基，C1-4烷氧基或C1-6烷酰氧基取代的C1-4烷基; n为0,1或2; Z为被羟基，C 1-4烷氧基，C 2-8亚烷基二氧基，C 1-6烷酰氧基或苯甲酰氧基或一个烷氧基羰基中的一个或两个取代的C 2-6 - 烷基或链烯基; 其盐与生理上可接受的酸具有有价值的药理学性质。

公开(公告)号：US4402960A

公开(公告)日：1983-09-06

申请号：US280163

申请日：1981-07-02

申请人： Ulrich Niedballa ,  Irmgard Bottcher

发明人： Ulrich Niedballa ,  Irmgard Bottcher

IPC分类号： A61K31/415 ,  A61K31/505 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C381/00 ,  C07D233/54 ,  C07D233/84 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D409/12 ,  C07D417/12

CPC分类号： C07D233/64 ,  C07C381/00 ,  C07D233/84

摘要： Imidazole derivatives of the formula ##STR1## wherein AR.sub.1 and AR.sub.2 each independently is phenyl, optionally substituted by halogen atoms, alkyl residues, alkoxy residues; or dialkylamino residues; pyridyl, furyl; or thienyl;R.sub.1 is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy groups, alkoxy groups, or acyloxy groups; benzyl; tetrahydropyran-2-yl; or tetrahydrofuran-2-yl;n is 0, 1 or 2; andZ is phenyl optionally substituted by halogen atoms, alkyl groups, alkoxy groups, nitro groups, amino, acylamino groups or trifluoromethyl groups; pyridyl; N-oxypyridyl; pyrimidinyl; thiazolyl; or thienyl, and the physiologically acceptable salts thereof with acids,have valuable pharmacological activity, e.g., antiinflammatory activity.

摘要翻译： 其中AR1和AR2各自独立地是苯基，任选地被卤素原子，烷基残基，烷氧基残基取代的式（I）的咪唑衍生物; 或二烷基氨基残基; 吡啶基，呋喃基; 或噻吩基; R1是氢; 任选被羟基，烷氧基或酰氧基取代的1-6个碳原子的烷基; 苄基; 四氢吡喃-2-基; 或四氢呋喃-2-基; n为0,1或2; Z为任选被卤素原子，烷基，烷氧基，硝基，氨基，酰氨基或三氟甲基取代的苯基; 吡啶基 N-氧吡啶基 嘧啶基; 噻唑基 或噻吩基及其与酸的生理上可接受的盐具有有价值的药理活性，例如抗炎活性。

公开(公告)号：US4355039A

公开(公告)日：1982-10-19

申请号：US190309

申请日：1980-09-24

申请人： Ulrich Niedballa ,  Irmgard Bottcher

发明人： Ulrich Niedballa ,  Irmgard Bottcher

IPC分类号： A61K31/415 ,  A61P29/00 ,  C07D233/84 ,  C07D233/88 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

CPC分类号： C07D233/84 ,  C07D233/88 ,  Y10S514/825 ,  Y10S514/826 ,  Y10S514/926 ,  Y10S514/927

摘要： Imidazole derivatives of the formula ##STR1## wherein Ar.sub.1 and Ar.sub.2 are each phenyl; phenyl substituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.2-6 dialkylamino; pyridyl; furyl; or thienyl; with the proviso that Ar.sub.1 and Ar.sub.2 are not both unsubstituted phenyl;R.sub.1 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted by hydroxy, C.sub.1-4 alkoxy or C.sub.1-6 alkanoyloxy;n is 0, 1 or 2; andZ is a C.sub.2-6 -alkyl or -alkenyl residue substituted by one or two of hydroxy, C.sub.1-4 alkoxy, C.sub.2-8 alkylenedioxy, C.sub.1-6 alkanoyloxy or benzoyloxy, or by one alkoxycarbonyl group;and the salts thereof with physiologically acceptable acids, possess valuable pharmacological properties.

摘要翻译： 其中Ar1和Ar2各自为苯基的式“IMAGE”的咪唑衍生物; 被卤素，C 1-4烷基，C 1-4烷氧基或C 2-6二烷基氨基取代的苯基; 吡啶基 呋喃 或噻吩基; 条件是Ar 1和Ar 2不是未被取代的苯基; R1是氢，C1-4烷基或被羟基，C1-4烷氧基或C1-6烷酰氧基取代的C1-4烷基; n为0,1或2; Z为被羟基，C 1-4烷氧基，C 2-8亚烷基二氧基，C 1-6烷酰氧基或苯甲酰氧基或一个烷氧基羰基中的一个或两个取代的C 2-6 - 烷基或链烯基; 其盐与生理上可接受的酸具有有价值的药理学性质。

公开(公告)号：US4272543A

公开(公告)日：1981-06-09

申请号：US107802

申请日：1979-12-27

申请人： Ulrich Niedballa ,  Irmgard Bottcher

发明人： Ulrich Niedballa ,  Irmgard Bottcher

IPC分类号： A61K31/415 ,  A61P29/00 ,  A61P37/08 ,  C07D233/84 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04

CPC分类号： C07D233/84

摘要： Imidazole derivatives of the formula ##STR1## wherein AR.sub.1 and AR.sub.2 are independently each phenyl; phenyl substituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.2-6 dialkylamino; pyridyl; furyl; or thienyl; with the proviso that AR.sub.1 and AR.sub.2 are not both unsubstituted phenyl;R.sub.1 is hydrogen, alkyl of 1-4 carbon atoms or alkyl of 1-4 carbon atoms substituted by hydroxy, C.sub.1-4 alkoxy or C.sub.1-6 alkanoyloxy;n is 0, 1 or 2; andZ is cyano; alkynyl of 2-6 carbon atoms; cycloalkyl of 3-8 carbon atoms; cycloalkyl of 3-8 carbon atoms substituted by hydroxy, acyloxy, hydroxymethyl or acyloxymethyl, "acyl" in both cases being the acyl group of a hydrocarbon, aliphatic C.sub.1-6 carboxylic acid or of benzoic acid; or alkyl of 1-4 carbon atoms substituted by cyano, phenyl or cycloalkyl of 3-6 carbon atoms;or physiologically acceptable salts thereof with an acid, have valuable pharmacological properties.

摘要翻译： 其中AR1和AR2各自独立地为苯基的式[IMAGE]的咪唑衍生物; 被卤素，C 1-4烷基，C 1-4烷氧基或C 2-6二烷基氨基取代的苯基; 吡啶基 呋喃 或噻吩基; 条件是AR1和AR2不是未取代的苯基; R1是氢，1-4个碳原子的烷基或1-4个碳原子被羟基，C1-4烷氧基或C1-6烷酰氧基取代的烷基; n为0,1或2; Z为氰基; 2-6个碳原子的炔基; 3-8个碳原子的环烷基; 由羟基，酰氧基，羟甲基或酰氧基甲基取代的3-8个碳原子的环烷基，两种情况下均为烃，脂族C 1-6羧酸或苯甲酸的酰基; 或被3-6个碳原子的氰基，苯基或环烷基取代的1-4个碳原子的烷基; 或其生理上可接受的盐与酸具有有价值的药理学性质。

公开(公告)号：US4975466A

公开(公告)日：1990-12-04

申请号：US282928

申请日：1988-12-07

申请人： Irmgard Bottcher ,  Werner Pignat

发明人： Irmgard Bottcher ,  Werner Pignat

IPC分类号： A61K9/00 ,  A61K31/165 ,  A61P11/08 ,  A61P17/00 ,  A61P25/02 ,  A61P29/00

CPC分类号： A61K31/165 ,  Y10S514/863 ,  Y10S514/887

摘要： Pharmaceutical preparations for topical, i.e. dermal, application that contain as active ingredient a compound of the formula I ##STR1## especially 2-hydroxy-5-[(RS)-1-hydroxy-2-[[(RS)-1-(p-methoxyphenyl)-prop-2-yl]-amino]-ethyl]-formanilide (formoterol), or one of its pharmaceutically acceptable salts, especially its semifumarate, are proposed for the treatment of inflammatory skin diseases.

摘要翻译： 含有作为活性成分的式I化合物（I）特别是2-羟基-5 - [（RS）-1-羟基-2 - [[（RS） - 1-（对甲氧基苯基） - 丙-2-基] - 酰胺] - 乙基] - 甲酰苯胺（福莫特罗）或其药学上可接受的盐，特别是其半富马酸盐之一被提出用于治疗炎性皮肤疾病。

公开(公告)号：US4289777A

公开(公告)日：1981-09-15

申请号：US107676

申请日：1979-12-27

申请人： Rudolf Albrecht ,  Eberhard Schroder ,  Irmgard Bottcher

发明人： Rudolf Albrecht ,  Eberhard Schroder ,  Irmgard Bottcher

IPC分类号： A61K31/47 ,  A61P29/00 ,  A61P31/04 ,  A61P37/08 ,  C07D215/56 ,  C07D401/12

CPC分类号： C07D215/56

摘要： Quinolonecarboxylic acid derivatives of the formula ##STR1## wherein the grouping ##STR2## is independently in the 6-, 7- or 8-position of each of the quinolone residues;m and n independently are each 1-4;R.sub.1 is hydrogen or alkyl of 1-6 carbon atoms;R.sub.2 is hyrogen, alkanoyl of 1-8 carbon atoms or benzoyl; andX is hydrogen, alkyl of 1-6 carbon atoms or the cation of a base which produces a physiologically acceptable salt with the quinolonecarboxylic acid,have valuable pharmacological properties.

摘要翻译： 喹诺酮羧酸衍生物，其分子式“IMAGE”独立地在每个喹诺酮残基的6-，7-或8-位; m和n各自独立地为1-4; R1是氢或1-6个碳原子的烷基; R2为氢，1-8个碳原子的烷酰基或苯甲酰基; X为氢，1-6个碳原子的烷基或与喹诺酮羧酸产生生理上可接受的盐的碱的阳离子，具有有价值的药理学性质。