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1. 发明授权

US4159273A Tricyclic mono-chromone-2-carboxylic acids 失效
标题翻译：三环单色酮-2-羧酸
公开(公告)号：US4159273A
公开(公告)日：1979-06-26
申请号：US869654
申请日：1978-01-16
申请人： Roger C. Brown , Richard Hazard , John Mann
发明人： Roger C. Brown , Richard Hazard , John Mann
IPC分类号： C07D311/58 , C07D311/74 , C07D311/78 , C07D311/92 , C07D493/04 , C07D311/22 , A61K31/35
CPC分类号： C07D493/04 , C07C45/513 , C07C45/54 , C07C45/62 , C07C45/63 , C07C45/64 , C07C45/67 , C07C45/71 , C07C45/75 , C07D311/58 , C07D311/74 , C07D311/78 , C07D311/92 , Y10S514/826
摘要： There are described compounds of formula I, ##STR1## in which R.sub.3 represents hydrogen, or alkyl C 1 to 6, R.sub.5 represents hydrogen, hydroxy, alkoxy C 1 to 6, alkanoyloxy C 2 to 6, alkenyloxy C 2 to 6, nitro, -NR.sub.1 R.sub.2, halogen, alkyl C 1 to 6, hydroxy-alkyl C 1 to 6, or hydroxy-alkoxy C 1 to 6,An adjacent pair of X, Y and Z form a --(CH.sub.2).sub.4 --, --CH.dbd.CH--CH.dbd.CH--or --O(CH.sub.2).sub.3 --chain, each of the chains optionally being substituted by one or two C 1 to 6 alkyl groups, and the remaining substituent X or Z represents alkenyl C2 to 6 optionally substituted by phenyl; halogen; or alkyl C 1 to 9 optionally substituted by one or more of the groups hydroxy, halogen, carbonyl oxygen, phenyl, or alkoxy C 1 to 6,Or, when an adjacent pair of X, Y and Z form a chain substituted by one or two C 1 to 6 alkyl groups, the remaining substituent X or Z may be hydrogen, andR.sub.1 and R.sub.2, which may be the same or different, are each hydrogen or alkyl C 1 to 6,And pharmaceutically acceptable derivatives thereof.Processes for making the compounds and pharmaceutical, e.g. anti-allergic, compositions containing the compounds are also described.
摘要翻译：描述了式I的化合物，其中R 3表示氢，或C 1至6的烷基，R 5表示氢，羟基，烷氧基C 1-6，烷酰氧基C 2-6，烯氧基C 2-6，硝基，-NR1R2，卤素，C1-6烷基，羟基 - 烷基C1至6，或羟基 - 烷氧基C1至6，X，Y和Z的相邻对形成 - （CH 2）4 - ， - CH = CH-CH = CH-或-O（CH 2）3 - 链，每个链任选被一个或两个C 1-6烷基取代，其余取代基X或Z表示任选被苯基 ; 卤素; 或任选被一个或多个羟基，卤素，羰基氧，苯基或烷氧基C 1-6取代的烷基C 1至9，当X，Y和Z的相邻对形成被一个或多个两个C 1-6烷基，剩余的取代基X或Z可以是氢，R 1和R 2可以相同或不同，分别为氢或C 1-6烷基，以及其药学上可接受的衍生物。

2. 发明授权

US4238606A Tricyclic mono-chromone-2-carboxylic acids 失效
标题翻译：三环单色酮-2-羧酸
公开(公告)号：US4238606A
公开(公告)日：1980-12-09
申请号：US35739
申请日：1979-05-03
申请人： Roger C. Brown , Richard Hazard , John Mann
发明人： Roger C. Brown , Richard Hazard , John Mann
IPC分类号： C07D311/24 , C07C45/54 , C07C45/62 , C07C45/63 , C07C45/64 , C07C45/67 , C07C45/71 , C07C49/83 , C07C49/86 , C07D20060101 , C07D311/58 , C07D311/74 , C07D311/78 , C07D311/92 , C07D493/04 , C07D311/22
CPC分类号： C07D493/04 , C07C45/54 , C07C45/62 , C07C45/63 , C07C45/64 , C07C45/67 , C07C45/673 , C07C45/71 , C07D311/58 , C07D311/74 , C07D311/78 , C07D311/92
摘要： There are described compounds of formula I, ##STR1## in which R.sub.3 represents hydrogen, or alkyl C 1 to 6,R.sub.S represents hydrogen, hydroxy, alkoxy C 1 to 6, alkanoyloxy C 2 to 6, alkenyloxy C 2 to 6, nitro, --NR.sub.1 R.sub.2, halogen, alkyl C 1 to 6, hydroxy-alkyl C 1 to 6, or hydroxy-alkoxy C 1 to 6,an adjacent pair of X, Y and Z form a --(CH.sub.2).sub.4 --, --CH.dbd.CH--CH.dbd.CH-- or --O(CH.sub.2).sub.3 -- chain, each of the chains optionally being substituted by one or two C 1 to 6 alkyl groups, and the remaining substituent X or Z represents alkenyl C 2 to 6 optionally substituted by phenyl; halogen; or alkyl C 1 to 9 optionally substituted by one or more of the groups hydroxy, halogen, carbonyl oxygen, phenyl, or alkoxy C 1 to 6,or, when an adjacent pair of X, Y and Z form a chain substituted by one or two C 1 to 6 alkyl groups, the remaining substituent X or Z may be hydrogen, andR.sub.1 and R.sub.2, which may be the same or different, are each hydrogen or alkyl C 1 to 6,and pharmaceutically acceptable derivatives thereof.Processes for making the compounds and pharmaceutical, e.g. anti-allergic, compositions containing the compounds are also described.
摘要翻译：描述了式I的化合物，其中R 3表示氢，或C 1至6的烷基，RS表示氢，羟基，烷氧基C 1-6，烷酰氧基C 2-6，烯氧基C 2-6，硝基，-NR1R2，卤素，C1-6烷基，羟基 - 烷基C1至6，或羟基 - 烷氧基C1至6，相邻的一对X，Y和Z形成 - （CH 2）4 - ， - CH = CH-CH = CH-或-O（CH 2）3 - 链，每个链任选被一个或两个C 1-6烷基取代，其余的取代基X或Z表示任选被苯基; 卤素; 或任选被一个或多个羟基，卤素，羰基氧，苯基或烷氧基C 1-6取代的C 1至9烷基，或者当相邻的一对X，Y和Z形成被一个或多个两个C 1至6个烷基，其余的取代基X或Z可以是氢，R 1和R 2可以相同或不同，分别为氢或C 1-6烷基，及其药学上可接受的衍生物。制备化合物和药物的方法，例如还描述了抗过敏剂，含有这些化合物的组合物。

3. 发明授权

US5648370A 7-(2-aminoethyl) benzothiazolones 失效
标题翻译： 7-（2-氨基乙基）苯并噻唑酮
公开(公告)号：US5648370A
公开(公告)日：1997-07-15
申请号：US348154
申请日：1994-11-28
申请人： Roger V. Bonnert , Roger C. Brown , David R. Cheshire , Francis Ince , John Dixon
发明人： Roger V. Bonnert , Roger C. Brown , David R. Cheshire , Francis Ince , John Dixon
IPC分类号： C07C233/43 , C07D209/34 , C07D235/26 , C07D277/68 , C07D417/12 , A61K31/425
CPC分类号： C07D277/68 , C07C233/43 , C07D209/34 , C07D235/26 , C07D417/12
摘要： There are disclosed compounds of formula I,Ar--CH.sub.2 CH.sub.2 --NH--CR.sup.1 R.sup.2 --X--Y Iin whichAr represents a group, ##STR1## X represents a C.sub.1-12 alkylene chain optionally interrupted or terminated by one or more groups selected from --S(O).sub.n --, --O--, --C(Z)--, CR.sup.6 R.sup.7, phenylmethyne, --NR.sup.8 --, --CONH--, --NHCO-- and --NHCONH--,Y represents an optionally substituted aryl or cycloalkyl group,Z represents O or S,R.sup.1, R.sup.2, R.sup.5 and R.sup.9 each independently represent hydrogen or alkyl C.sub.1-6,R.sup.3 and R.sup.4 represent hydrogen, or R.sup.3 and R.sup.4 together form a group --S--, --NR.sup.9 -- or --CH.sub.2 --,R.sup.6 and R.sup.7 independently represent hydrogen, alkyl C.sub.1-6, fluoro, cyano, or CF.sub.3, provided that at least one of R.sup.6 and R.sup.7 is other than hydrogen,R.sup.8 represents hydrogen or alkyl C.sub.1-6, or when X is interrupted or terminated by more than one --NR.sup.8 -- group may together with another R.sup.8 group form the chain --CH.sub.2 --CH.sub.2 --, andn represents 0, 1 or 2,and pharmaceutically acceptable derivatives thereof.Processes for their production and pharmaceutical compositions and methods of treatment involving their use are also described.
摘要翻译：公开了式I的化合物，Ar-CH2CH2-NH-CR1R2-X-Yinin，其中Ar表示一个基团，X表示C1-12亚烷基链，任选地被一个或多个选自-S（ O）n - ， - C（Z） - ，CR 6 R 7，苯基甲炔基，-NR 8 - ， - CONH - ， - NHCO-和-NHCONH-，Y表示任选取代的芳基或环烷基，Z表示O或 S，R 1，R 2，R 5和R 9各自独立地表示氢或烷基C 1-6，R 3和R 4表示氢，或者R 3和R 4一起形成基团-S - ， - NR 9 - 或-CH 2 - ，R 6和R 7独立地表示氢，烷基C 1-6，氟，氰基或CF 3，条件是R 6和R 7中的至少一个不是氢，R 8表示氢或C 1-6烷基，或者当X被多于一个-NR 8中断或终止时 - 基团可以与另一个R8基团一起形成链-CH2-CH2-，n代表0,1或2及其药学上可接受的衍生物。还描述了其生产方法和药物组合物及其使用方法。

4. 发明授权

US5566700A Walking stick 失效
标题翻译：拐杖
公开(公告)号：US5566700A
公开(公告)日：1996-10-22
申请号：US567114
申请日：1995-12-04
申请人： Roger C. Brown
发明人： Roger C. Brown
IPC分类号： A45B9/02 , A45B9/04 , A61H3/02
CPC分类号： A45B9/02 , A45B9/04 , A61H2003/0211 , A61H2003/0216 , A61H2003/0272
摘要： A walking stick for aiding support of a walking individual. The inventive device includes a stanchion assembly having a handgrip assembly secured to an upper end thereof. A ground engaging assembly is secured to a lower end of the stanchion assembly for rollingly engaging a ground surface during walking and for supporting the walking stick in an upright orientation during periods of non-use thereof.
摘要翻译：用于协助支持步行个人的手杖。本发明的装置包括具有固定到其上端的手柄组件的支柱组件。地面接合组件被固定到支柱组件的下端，用于在行走期间滚动地接合地面，并且用于在不使用它的时段期间以直立的方向支撑手杖。

5. 发明授权

US4328230A N-Substituted-quinolin-4-one-2-carboxic acid derivatives 失效
标题翻译： N-取代的喹啉-4-酮-2-羧酸衍生物
公开(公告)号：US4328230A
公开(公告)日：1982-05-04
申请号：US17612
申请日：1979-03-05
申请人： Roger C. Brown , Hugh Cairns , Anthony R. Payne
发明人： Roger C. Brown , Hugh Cairns , Anthony R. Payne
IPC分类号： C07D215/26 , C07D215/28 , C07D215/32 , C07D215/48 , C07D221/08 , C07D221/10 , C07D471/04 , A61K31/47 , C07D215/58
CPC分类号： C07D471/04 , C07D215/48 , C07D221/08 , C07D221/10
摘要： There are described compounds of formula I, ##STR1## in which R.sub.5 to R.sub.8 may be a variety of substituents, or an adjacent pair of R.sub.5, R.sub.6, R.sub.7 and R.sub.8 form a chain--COCH.dbd.C(COOH)NRh--,or one of R.sub.5, R.sub.6, R.sub.7 and R.sub.8 form a group of formula II, ##STR2## in which Ra, Rb and Rc have the same significances as R.sub.5, R.sub.6, R.sub.7 and R.sub.8,X is an optionally interrupted or substituted hydrocarbon chain,Rg and Rh, which may be the same or different are each alkyl, alkenyl, phenyl-alkyl, alkanoyl, benzoyl or phenylalkanoyl,or Rg and R.sub.8 and/or Rh and Rc in formula II, together form a chain --(CH.sub.2).sub.n --, and n is 2, 3 or 4.There are also described processes for making the compounds and pharmaceutical, e.g. anti-allergic, compositions containing the compounds.
摘要翻译：描述了式I，其中R 5至R 8可以是多种取代基的式I化合物，或相邻的一对R 5，R 6，R 7和R 8形成链-COCH = C（COOH）NRh-，或 R 5，R 6，R 7和R 8中的一个形成式II，其中R a，R b和R c与R 5，R 6，R 7和R 8具有相同的含义，X是任选中断或取代的烃链， Rg和Rh可以相同或不同，分别为烷基，烯基，苯基 - 烷基，烷酰基，苯甲酰基或苯基烷酰基，或式II中的R g和R 8和/或Rh和R c一起形成链 - （CH 2）n - 和n为2,3或4.还描述了制备化合物和药物的方法，例如抗过敏剂，含有这些化合物的组合物。

6. 发明授权

US4156726A 4-Oxo-2-carboxyl quinoline derivatives used as antiallergic compounds 失效
标题翻译：用作抗过敏化合物的4-氧代-2-羧基喹啉衍生物
公开(公告)号：US4156726A
公开(公告)日：1979-05-29
申请号：US635615
申请日：1975-11-26
申请人： Roger C. Brown , Hugh Cairns , Anthony R. Payne
发明人： Roger C. Brown , Hugh Cairns , Anthony R. Payne
IPC分类号： C07D215/26 , C07D215/28 , C07D215/32 , C07D215/48 , C07D221/08 , C07D221/10 , C07D471/04 , A61K31/47
CPC分类号： C07D471/04 , C07D215/48 , C07D221/08 , C07D221/10
摘要： There are described compounds of formula I, ##STR1## in which R.sub.5 to R.sub.8 may be a variety of substituents, OR AN ADJACENT PAIR OF R.sub.5, R.sub.6, R.sub.7 and R.sub.8 form a chain --COCH.dbd.C(COOH)NRh--,Or one of R.sub.5, R.sub.6, R.sub.7 and R.sub.8 form a group of formula II, ##STR2## in which Ra, Rb and Rc have the same significances as R.sub.5, R.sub.6, R.sub.7 and R.sub.8,X is an optionally interrupted or substituted hydrocarbon chain,Rg and Rh, which may be the same or different are each alkyl, alkenyl, phenyl-alkyl, alkanoyl, benzoyl or phenylalkanoyl,Or Rg and R.sub.8 and/or Rh and Rc in formula II, together form a chain --(CH.sub.2).sub.n --, and n is 2, 3 or 4.There are also described processes for making the compounds and pharmaceutical, e.g. anti-allergic, compositions containing the compounds.
摘要翻译：描述式I的化合物，其中R 5至R 8可以是多种取代基，或者R 5，R 6，R 7和R 8的相邻对形成链-COCH = C（COOH）NR h - ，OR R 5，R 6，R 7和R 8中的一个形成式II，其中R a，R b和R c具有与R 5，R 6，R 7和R 8相同的含义的基团，X是任选中断或取代的烃链， Rg和Rh可以相同或不同，分别为烷基，烯基，苯基 - 烷基，烷酰基，苯甲酰基或苯基烷酰基，OR Rg和R 8和/或式II中的Rh和R c一起形成链 - （CH 2）n - ，n为2,3或4。

7. 发明授权

US5763465A 7-(2-aminoethyl) benzothiazolones 失效
标题翻译： 7-（2-氨基乙基）苯并噻唑酮
公开(公告)号：US5763465A
公开(公告)日：1998-06-09
申请号：US740622
申请日：1996-10-31
申请人： Roger V. Bonnert , Roger C. Brown , David R. Cheshire , Francis Ince , John Dixon
发明人： Roger V. Bonnert , Roger C. Brown , David R. Cheshire , Francis Ince , John Dixon
IPC分类号： C07C233/43 , C07D209/34 , C07D235/26 , C07D277/68 , C07D417/12 , A61K31/425 , A61K31/16 , C07C233/02 , C07D277/62
CPC分类号： C07D277/68 , C07C233/43 , C07D209/34 , C07D235/26 , C07D417/12
摘要： There are disclosed compounds of formula I, Ar--CH.sub.2 CH.sub.2 --NH--CR.sup.1 R.sup.2 --X--Y I in which Ar represents a group, ##STR1## X represents a C.sub.1-12 alkylene chain optionally interrupted or terminated by one or more groups selected from --S(O).sub.n --, --O--, --C(Z)--, CR.sup.6 R.sup.7, phenylmethyne, --NR.sup.8 --, --CONH--, --NHCO-- and --NHCONH--, Y represents an optionally substituted aryl or cycloalkyl group, Z represents O or S, R.sup.1, R.sup.2, R.sup.5 and R.sup.9 each independently represent hydrogen or alkyl C.sub.1-6, R.sup.3 and R.sup.4 represent hydrogen, or R.sup.3 and R.sup.4 together form a group --S--, --NR.sup.9 -- or --CH.sub.2 --, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl C.sub.1-6, fluoro, cyano, or CF.sub.3, provided that at least one of R.sup.6 and R.sup.7 is other than hydrogen, R.sup.8 represents hydrogen or alkyl C.sub.1-6, or when X is interrupted or terminated by more than one --NR.sup.8 -- group may together with another R.sup.8 group form the chain --CH.sub.2 --CH.sub.2 --, and n represents 0, 1 or 2, and pharmaceutically acceptable derivatives thereof. Processes for their production and pharmaceutical compositions and methods of treatment involving their use are also described.
摘要翻译：公开了式I，Ar-CH 2 CH 2 -NH-CR 1 R 2 I-XY I的化合物，其中Ar表示被一个或多个选自-S（O）n - ， - O - ， - C （Z） - ，CR6R7，苯基甲炔，-NR8-，-CONH-，-NHCO-和-NHCONH-，Y表示任选取代的芳基或环烷基，Z表示O或S，R1，R2，R5和R9各自独立地代表氢或烷基C1-6，R3和R4代表氢，或R3和R4一起形成基团-S-，-NR9-或-CH2-，R6和R7独立地表示氢，烷基C1-6，氟，氰基，或CF 3，条件是R 6和R 7中的至少一个不是氢，R 8表示氢或C 1-6烷基，或当X被多于一个-NR 8 - 基团中断或终止时，可以与另一个R8基团形成链 -CH 2 -CH 2 - ，n表示0,1或2，及其药学上可接受的衍生物。还描述了其生产方法和药物组合物及其使用方法。

8. 发明授权

US4927822A 1,3,4-thiadiazoles 失效
标题翻译： 1,3,4-噻二唑
公开(公告)号：US4927822A
公开(公告)日：1990-05-22
申请号：US901048
申请日：1986-08-27
申请人： Roger C. Brown , John Dixon , David H. Robinson
发明人： Roger C. Brown , John Dixon , David H. Robinson
IPC分类号： A61K31/41 , A61K31/4245 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/54 , A61K38/00 , A61P9/12 , A61P43/00 , C07D249/12 , C07D253/06 , C07D271/10 , C07D285/12 , C07D285/125 , C07D285/135 , C07D285/16 , C07D401/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07K5/02 , C07K5/068 , C12N9/99
CPC分类号： C07D253/06 , C07D271/10 , C07D285/12 , C07D285/135 , C07D285/16 , C07D417/04 , C07K5/0222 , C07K5/06086 , A61K38/00
摘要： There are described compounds of formula I, ##STR1## in which Y is S, O or NR.sub.9,n is 0 or 1,R.sub.9 is hydrogen or alkyl C 1 to 10,R.sub.3 is hydrogen, alkyl C 1 to 10, cycloalkyl C3 to 10, CF.sub.3, SR.sub.10, a 5 or 6 membered heterocyclic group containing one or more S, O or N atoms, NR.sub.4 R.sub.5, phenyl or phenylalkyl C7 to 12, the phenyl, phenylalkyl and heterocyclic groups optionally being fused to a further phenyl group, the heterocyclic group and any phenyl group optionally being substituted by alkyl C 1 to 6, halogen, alkoxy C 1 to 6, nitro, nitrile, CF.sub.3, SR.sub.6, NR.sub.7 R.sub.11 or hydroxy,R.sub.6, R.sub.7 and R.sub.11, which may be the same or different, are each hydrogen or alkyl C 1 to 10,R.sub.4 and R.sub.5, which may be the same or different, are each hydrogen, alkyl C 1 to 10 or phenyl,R.sub.10 is alkyl C 1 to 10,X.sub.1 is S or O, andA is a chain comprising from 2-16 atoms, which chain carries an O or S containing substitutent at a position 2-6 atoms away from the group C=X.sub.1,and pharmaceutically acceptable salts, esters and amides thereof, p1 there are also described method of making the compounds and pharmaceutical formulations, e.g. for the treatment of hypertension, containing them.
摘要翻译：描述了式I的化合物，其中Y是S，O或NR9，n是0或1，R9是氢或烷基C1至10，R3是氢，烷基C1至10，环烷基C3 至10，CF 3，SR 10，含有一个或多个S，O或N原子的5或6元杂环基，NR 4 R 5，苯基或苯基烷基C 7至12，任选地与另外的苯基稠合的苯基，苯基烷基和杂环基，杂环基和任选被烷基C 1-6取代的任何苯基，卤素，烷氧基C 1至6，硝基，腈，CF 3，SR 6，NR 7 R 11或羟基，R 6，R 7和R 11可以相同或不同各自为氢或烷基C 1至10，R 4和R 5可以相同或不同，各自为氢，烷基C 1至10或苯基，R 10为烷基C 1至10，X 1为S或O，以及 A是包含2-16个原子的链，该链在距离基团C = X1的2-6个原子的位置上携带含有O或S的取代基，以及药学上可接受的盐，酯和酰胺除此之外，还描述了制备化合物和药物制剂的方法，例如，用于治疗高血压，包含它们。

9. 发明授权

US4299832A Substituted theophylline compounds 失效
标题翻译：取代茶碱化合物
公开(公告)号：US4299832A
公开(公告)日：1981-11-10
申请号：US89286
申请日：1979-10-30
申请人： Roger C. Brown , Rodney A. Brown , Stephen E. O'Connor
发明人： Roger C. Brown , Rodney A. Brown , Stephen E. O'Connor
IPC分类号： C07D473/08
CPC分类号： C07D473/08
摘要： The substituted theophyllines of the formula: ##STR1## (wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each represent alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or phenylalkyl of 7 to 10 carbon atoms, each of which may be unsubstituted or substituted by one or more hydroxy groups, alkoxy or alkylthio groups of 1 to 4 carbon atoms, halogen atoms, cyano groups, nitro groups, carboxy groups, alkoxycarbonyl groups of 2 to 5 carbon atoms, amino groups, alkylamino groups of 1 to 4 carbon atoms or dialkylamino groups of 2 to 8 carbon atoms, or when the group is phenyl or phenylalkyl, by one or more alkyl groups of 1 to 4 carbon atoms;or R.sup.2 and R.sup.3 together represent a hydrocarbon chain of 3 to 6 carbon atoms optionally interrupted by a heteroatom;and n represents an integer of from 1 to 6)and the acid additional salts thereof, are novel compounds which are useful in the treatment of cardiac disorders. Processes for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：下式的取代茶碱：其中R 1，R 2和R 3可相同或不同，各自表示1至6个碳原子的烷基，3至7个碳原子的环烷基，苯基或苯基烷基每个可以是未取代的或被一个或多个羟基，1-4个碳原子的烷氧基或烷硫基，卤原子，氰基，硝基，羧基，烷氧基羰基取代为2〜具有1至4个碳原子的烷基氨基或2至8个碳原子的二烷基氨基，或当该基团为苯基或苯基烷基时，通过一个或多个含有1至4个碳原子的烷基;或R 2和 R3一起表示3〜6个碳原子的烃链，任选被杂原子中断; n表示1〜6的整数）及其酸的附加盐，可用于治疗心脏病。还描述了其制备方法和含有它们的药物组合物。

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