公开(公告)号：US4148806A

公开(公告)日：1979-04-10

申请号：US860504

申请日：1977-12-14

申请人： Richard E. Brown ,  Paul C. Unangst ,  Frank Fontsere ,  Arthur C. Fabian

发明人： Richard E. Brown ,  Paul C. Unangst ,  Frank Fontsere ,  Arthur C. Fabian

IPC分类号： C07D209/36 ,  C07D491/04 ,  C07D491/052

CPC分类号： C07D491/04 ,  C07D209/36

摘要： This invention relates to a novel process for preparing a group of novel substituted indolopyrones.

摘要翻译： 本发明涉及制备一组新型取代的吲哚吡酮的新方法。

公开(公告)号：US4013671A

公开(公告)日：1977-03-22

申请号：US666829

申请日：1976-03-15

申请人： Richard E. Brown ,  John Shavel, Jr.

发明人： Richard E. Brown ,  John Shavel, Jr.

IPC分类号： A61K31/535 ,  C07D491/052 ,  C07D311/06 ,  C07D311/76

CPC分类号： C07D491/052 ,  A61K31/535

摘要： Substituted benzopyrano[3,4-c]pyridines having the following structural formula are disclosed: ##STR1## In the above formula, R.sub.1 R.sub.2 are hydrogen, a hydroxyl group or a lower alkoxyl group of from 1 to 6 carbon atoms; R.sub.3 is hydrogen or a lower alkyl group of from 1 to 6 carbon atoms and X is an oxygen atom, a sulfur atom, a methylene group or a nitrogen atom substituted by hydrogen, a lower alkyl group of from 1 to 6 carbon atoms or a lower alkanoyl group of from 1 to 6 carbon atoms. The compounds of this invention are prepared by reacting an R.sub.1, R.sub.2 -substituted phenol with a 3-carbethoxy-4-piperidone in the presence of an acid catalyst to give an intermediate R.sub.1, R.sub.2 -substituted benzopyrano[3,4-c] pyridine. N-aminoalkylbenzopyrano[3,4-c]pyridines are obtained by treating the benzopyrano[3,4-c]pyridine with an appropriately substituted alkyl halide. The compounds of this invention are useful as bronchodilators for the treatment of bronchial asthma.

公开(公告)号：US3984546A

公开(公告)日：1976-10-05

申请号：US622547

申请日：1975-10-15

申请人： Richard E. Brown ,  John Shavel, Jr.

发明人： Richard E. Brown ,  John Shavel, Jr.

IPC分类号： A61K31/535 ,  A61K31/54 ,  A61K31/44 ,  A61K31/445

CPC分类号： C07D491/052 ,  A61K31/535 ,  A61K31/54 ,  Y10S514/826

摘要： Substituted benzopyrano[3,4-c]pyridines having the following structural formula are disclosed: ##SPC1##In the above formula, R.sub.1 and R.sub.2 are hydrogen, a hydroxyl group or a lower alkoxyl group of from 1 to 6 carbon atoms; and X is an oxygen atom, a sulfur atom, a methylene group or a nitrogen atom substituted by hydrogen, a lower alkyl group of from 1 to 6 carbon atoms or a lower alkanoyl group of from 1 to 6 carbon atoms. The compounds of this invention are prepared by reacting an R.sub.1, R.sub.2 -substituted phenol with a 3-carbethoxy-4-piperidone in the presence of an acid catalyst to give an intermediate R.sub.1, R.sub.2 -substituted benzopyrano[3,4-c]pyridine. N-aminoalkylbenzopyrano[3,4-c]pyridines are obtained by treating the benzopyrano[3,4-c]pyridine with an appropriately substituted alkyl halide. The compounds of this invention are useful as bronchodilators for the treatment of bronchial asthma.

摘要翻译： 公开了具有以下结构式的取代的苯并吡喃并[3,4-c]吡啶：在上式中，R 1和R 2是氢，羟基或具有1至6个碳原子的低级烷氧基; X为氧原子，硫原子，亚甲基或被氢取代的氮原子，1〜6个碳原子的低级烷基或1〜6个碳原子的低级烷酰基。 本发明化合物是通过在酸催化剂存在下使R1，R2取代的苯酚与3-乙酯基-4-哌啶酮反应得到中间体R1，R2取代的苯并吡喃并[3,4-c]吡啶 。 通过用适当取代的烷基卤处理苯并吡喃并[3,4-c]吡啶得到N-氨基烷基苯并吡喃并[3,4-c]吡啶。 本发明的化合物可用作治疗支气管哮喘的支气管扩张剂。

公开(公告)号：US3961057A

公开(公告)日：1976-06-01

申请号：US538424

申请日：1975-01-03

申请人： Richard E. Brown ,  John Shavel, Jr.

发明人： Richard E. Brown ,  John Shavel, Jr.

IPC分类号： A61K31/535

CPC分类号： C07D491/052 ,  A61K31/535 ,  Y10S514/826

摘要： Substituted benzopyrano[3,4-c]pyridines having the following structural formula are disclosed: ##SPC1##In the above formula, R.sub.1 and R.sub.2 are hydrogen, a hydroxyl group or a lower alkoxyl group of from 1 to 6 carbon atoms; R.sub.3 is hydrogen or a lower alkyl group of from 1 to 6 carbon atoms and X is an oxygen atom, a sulfur atom, a methylene group or a nitrogen atom substituted by hydrogen, a lower alkyl group of from 1 to 6 carbon atoms or a lower alkanoyl group of from 1 to 6 carbon atoms. The compounds of this invention are prepared by reacting an R.sub.1, R.sub.2 -substituted phenol with a 3-carbethoxy-4-piperidone in the presence of an acid catalyst to give an intermediate R.sub.1, R.sub.2 -substituted benzopyrano[3,4-c]pyridine. N-aminoalkylbenzopyrano[3,4-c]pyridines are obtained by treating the benzopyrano[3,4-c]pyridine with an appropriately substituted alkyl halide. The compounds of this invention are useful as bronchodilators for the treatment of bronchial asthma.

摘要翻译： 公开了具有以下结构式的取代的苯并吡喃并[3,4-c]吡啶：在上式中，R 1和R 2是氢，羟基或具有1至6个碳原子的低级烷氧基; R3是氢或1〜6个碳原子的低级烷基，X是氧原子，硫原子，亚甲基或被氢取代的氮原子，1〜6个碳原子的低级烷基或 1至6个碳原子的低级烷酰基。 本发明化合物是通过在酸催化剂存在下使R1，R2取代的苯酚与3-乙酯基-4-哌啶酮反应得到中间体R1，R2取代的苯并吡喃并[3,4-c]吡啶 。 通过用适当取代的烷基卤处理苯并吡喃并[3,4-c]吡啶得到N-氨基烷基苯并吡喃并[3,4-c]吡啶。 本发明的化合物可用作治疗支气管哮喘的支气管扩张剂。

公开(公告)号：US3932466A

公开(公告)日：1976-01-13

申请号：US532417

申请日：1974-12-13

申请人： Richard E. Brown ,  David M. Lustgarten

发明人： Richard E. Brown ,  David M. Lustgarten

IPC分类号： C07D311/22 ,  C07D7/34

CPC分类号： C07D311/22 ,  Y10S514/826

摘要： This invention relates to substituted 2-amino chromones of the general structure I: ##SPC1##wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 may be hydrogen, hydroxy, lower alkyl or lower alkoxy of 1-6 carbon atoms, halogen such as chloro or bromo, or aryl such as phenyl, and X may be cyano or carboxamido. Two novel procedures for preparing substituted 2-amino chromones having the Formula I, starting with salicylic acid or substituted salicylic acid, are described. The compounds of this invention are active in the prevention of allergic and asthmatic reactions in mammals.

摘要翻译： 本发明涉及通用结构I的取代的2-氨基色酮：

公开(公告)号：US07272516B2

公开(公告)日：2007-09-18

申请号：US10745122

申请日：2003-12-23

申请人： Zhenyuan Wang ,  Jiuping Pan ,  David Lubkeman ,  Richard E. Brown

发明人： Zhenyuan Wang ,  Jiuping Pan ,  David Lubkeman ,  Richard E. Brown

IPC分类号： G01R21/00

CPC分类号： H02J3/00 ,  H02J2003/007 ,  Y02E60/76 ,  Y04S40/22

摘要： Methodologies adjust a component failure rate for electric power network reliability analysis. A component may include subcomponents and the failure of each subcomponent may be feature dependent. Features are measurable or observable inputs, which can affect the life of one or more subcomponents. The failure rate of a particular component may be obtained according to its real conditions. The methodologies can be used to do condition-based reliability analysis for electric power networks, in order to obtain a maintenance/replacement/operation strategy.

摘要翻译： 方法调整电力网可靠性分析的组件故障率。 组件可以包括子组件，并且每个子组件的故障可以是特征相关的。 特征是可测量的或可观测的输入，可以影响一个或多个子部件的寿命。 特定部件的故障率可以根据实际情况获得。 这些方法可以用于对电力网络进行基于条件的可靠性分析，以获得维护/更换/操作策略。

公开(公告)号：US4698346A

公开(公告)日：1987-10-06

申请号：US889021

申请日：1986-07-24

申请人： John H. Musser ,  Richard E. Brown

发明人： John H. Musser ,  Richard E. Brown

IPC分类号： C07D215/28 ,  C07D498/04 ,  A61K31/425 ,  C07D513/04

CPC分类号： C07D215/28

摘要： New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.

摘要翻译： 新喹啉化合物及相应的1,2-; 1,3- 和1,4-苯并二嗪，喹啉化合物具有下式：其中R1和R2独立地是氢，低级烷基，卤素，三氟甲基，氨基，低级烷基氨基，低级酰氨基，氰基，芳基 ，芳基/低级亚烷基，硝基，低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷酰基，羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y为氧，硫，氮或R 3 N，其中R 3为氢 低级烷基，烯基，炔基，芳基，芳烷基，酰基，氨基烷基或羧基烷基，Z是氧，硫或氮，X是氰基，烷氧羰基，羧基，甲酰肟基，四唑基，烷氧基烷基或羧基烷基，m是0或1， 可用作药物，特别是用于治疗哮喘，和/或作为制备用于治疗哮喘的化合物的中间体。

公开(公告)号：US4440929A

公开(公告)日：1984-04-03

申请号：US362713

申请日：1982-03-29

申请人： Thomas D. Lee ,  Richard E. Brown

发明人： Thomas D. Lee ,  Richard E. Brown

IPC分类号： C07D233/90 ,  C07D487/04 ,  A61K31/495 ,  C07D405/10

CPC分类号： C07D487/04 ,  C07D233/90

摘要： Provided are imidazoquinoxalines of the structures: ##STR1## wherein R.sub.1, R.sub.5, R.sub.6 and R.sub.7 are independently H, alkyl, aryl, alkenyl, alkynyl, hydroxy, hydroxyalkyl, alkoxy, mercapto, mercaptoalkyl, alkylthio, amino, alkylamino, aminoalkyl, carboxaldehyde, carboxylic acid and salts thereof, carbalkoxy, alkanoyl, cyano, nitro, halo, trifluoromethyl, alkylsulfonyl, sulfonamido, or R.sub.1, R.sub.5, R.sub.6 and R.sub.7 may be taken together with the adjacent group to form a methylenedioxy group.R.sub.4 is H, alkyl, alkenyl, alkynyl, aryl, aralkyl, hydroxy or alkanoyl.R.sub.3 is H, cyano, tetrazolo, carboxaldehyde, hydroxyalkyl, carboxylic acid and salts thereof or derivatives thereof such as esters or amides in which the substituent on the ester oxygen or amide nitrogen is alkyl, aryl, hydroxyalkyl, alkoxyalkyl or amino alkyl.R.sub.2 and R.sub.8 are independently H, alkyl, aryl, halo, amino, alkylamino, arylamino, hydroxyamino, hydroxy, alkoxy, mercapto or alkylthio, andX is oxygen, sulfur, imino, and hydroxyimino.

摘要翻译： 提供以下结构的咪唑并喹啉：其中R1，R5，R6和R7独立地为H，烷基，芳基，烯基，炔基，羟基，羟基烷基，烷氧基，巯基，巯基烷基，烷硫基，氨基， 烷基氨基，氨基烷基，甲醛，羧酸及其盐，烷氧基，烷酰基，氰基，硝基，卤素，三氟甲基，烷基磺酰基，亚磺酰氨基或R 1，R 5，R 6和R 7可与相邻基团一起形成亚甲二氧基。 R4是H，烷基，烯基，炔基，芳基，芳烷基，羟基或烷酰基。 R 3是H，氰基，四唑，羧醛，羟烷基，羧酸及其盐或其衍生物，例如酯或酰胺，其中酯氧或酰胺氮的取代基是烷基，芳基，羟基烷基，烷氧基烷基或氨基烷基。 R 2和R 8独立地是H，烷基，芳基，卤素，氨基，烷基氨基，芳基氨基，羟基氨基，羟基，烷氧基，巯基或烷硫基，X是氧，硫，亚氨基和羟基亚氨基。

公开(公告)号：US4298742A

公开(公告)日：1981-11-03

申请号：US149079

申请日：1980-05-12

申请人： Richard E. Brown ,  Vasil St. Georgiev ,  Bernard Loev

发明人： Richard E. Brown ,  Vasil St. Georgiev ,  Bernard Loev

IPC分类号： A61K31/42 ,  A61K31/423 ,  A61K31/425 ,  A61K31/428 ,  A61P37/08 ,  C07D263/58 ,  C07D265/36 ,  C07D277/68 ,  C07D413/12 ,  C07D263/34

CPC分类号： C07D263/58 ,  C07D265/36 ,  C07D277/68

摘要： New benzoxazole-2-carboxylic acid esters are described. These compounds are useful as anti-allergic reagents.

摘要翻译： 描述了新的苯并恶唑-2-羧酸酯。 这些化合物可用作抗过敏试剂。

公开(公告)号：US4092328A

公开(公告)日：1978-05-30

申请号：US685039

申请日：1976-05-10

申请人： Richard E. Brown

发明人： Richard E. Brown

IPC分类号： C07D209/30 ,  C07D495/04 ,  C07D513/04 ,  A61K31/40

CPC分类号： C07D495/04 ,  C07D209/30

摘要： This invention relates to novel indolothiopyrones having the formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or aryl; R.sub.2 is hydrogen or halogen; and R.sub.7 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, nitro-substituted-aryl, or .omega.-substituted lower alkyl wherein the substituent is: ##STR2## wherein R.sub.4 and R.sub.5 each represent hydrogen, lower alkyl, or together with the nitrogen atom, form a heterocyclic ring; and R.sub.6 is lower alkoxy or amino, and novel intermediates used in their preparation. The indolothiopyrones are prepared by reacting a 3-mercaptoindole with sodium propiolate or a substituted sodium propiolate followed by acidification to obtain an intermediate acid; the intermediate acid cyclizes in the presence of an acid catalyst to obtain the indolothiopyrone structure which may be additionally subjected to halogenation, alkylation or hydrolysis to obtain derivatives having the various substituent groups disclosed. The compounds of this invention are useful in the treatment of angina pectoris and conditions benefiting from the depression of the central nervous system.

摘要翻译： 本发明涉及具有下式的新的吲哚硫噻酮：其中R 1是氢，低级烷基或芳基; R2是氢或卤素; 并且R 7是氢，低级烷基，低级烯基，低级炔基，硝基取代的芳基或ω-取代的低级烷基，其中取代基是：其中R 4和R 5各自代表氢，低级烷基或与氮一起 原子，形成杂环; 并且R6是低级烷氧基或氨基，并且其制备中使用的新型中间体。 吲哚硫代吡喃是通过使3-巯基吲哚与丙炔酸钠或取代的丙酸炔丙酯反应，然后酸化得到中间体酸制备的; 中酸在酸催化剂的存在下环化，得到吲哚硫酮吡喃酮结构，其可另外进行卤化，烷基化或水解，得到具有所公开的各种取代基的衍生物。 本发明的化合物可用于治疗心绞痛和受益于中枢神经系统抑制的病症。