公开(公告)号：EP0125803A3

公开(公告)日：1987-01-21

申请号：EP84302566

申请日：1984-04-16

申请人： FISONS plc

发明人： Baxter, Andrew John Gilby ,  Dixon, John ,  Gould, Kenneth John ,  McInally, Thomas ,  Tinker, Alan Charles

IPC分类号： C07D211/90 ,  C07D211/78 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D401/06 ,  A61K31/445

CPC分类号： C07D231/12 ,  C07C17/093 ,  C07C45/00 ,  C07C47/55 ,  C07C205/56 ,  C07D205/04 ,  C07D211/78 ,  C07D211/90 ,  C07D233/56 ,  C07D249/08 ,  C07D305/08 ,  C07D309/12 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07C25/13

摘要： There are described compounds of formula I,
in which R 1 represents benzofurazanyl, pyridyl or phenyl, the pyridyl or phenyl being substituted, -COOR 2 and -COOR 3 are various ester groups, Yand Ztogetherform a bond, and additionally, when R. is an electron withdrawing group Y may be hydrogen and Z may be hydroxy, one of R 7 and R. represents alkyl Cl to 6 and the other represents -CONR 10 R 11 ; -CSNH 2 ; -C(=NN)SR 9 ; -S(O) m R 9 ; phenyl optionally substituted by one or more of alkyl Cl to 6, halogen, alkoxy CI to 6 or nitro; alkyl Cl to 6 substituted by halogen; or furanyl, or R 7 and R. may be the same or different and each represents phenyl optionally substituted by one or more of alkyl CI to 6, halogen, alkoxy Cl to 6 or nitro; amino; alkyl CI to 6 substituted by halogen; -CN; -CH 2 OH; -CHO or-CH(OR 9 ) 2 , m is 0 or 1 R 9 is alkyl CI to 6, and R 10 and R 11 each independently represent hydrogen or alkyl Cl to 6, or together with the nitrogen atom to which they are attached form a 5 or 6 membered heterocyclic ring. There are also described processes for making the compounds, and pharmaceutical, eg calcium antagonist, formulations containing them.

公开(公告)号：EP0169009A3

公开(公告)日：1988-08-31

申请号：EP85304728

申请日：1985-07-02

申请人： FISONS plc

发明人： Baxter, Andrew John ,  Dixon, John ,  Gould, Kenneth John

IPC分类号： C07D211/90 ,  A61K31/44

CPC分类号： C07D211/90

摘要： There are described compounds of formula I,
in which R 1 represents phenyl optionally substituted by ne or more of the groups, halogen, nitro, -CN, or alkyl C1 to optionally substituted by halogen, R 2 and R 3 , which may be the same or different, each present alkyl C1 to 6 or cycloalkyl C3 to 8, R 4 represents alkyl C1 to 6 substituted by halogen, and R 5 represants alkyl! to 6. There are also described methods of making the com- ounds, and their formulation and use as pharmaceuticals.

摘要翻译： 描述了式I的化合物，其中R 1表示任选被一个或多个下列基团取代的苯基：卤素，硝基，-CN或任选被卤素，R 2和R 3取代的C 1至C 6烷基，其可以是 相同或不同，各自表示烷基C1至6或环烷基C3至8，R4表示被卤素取代的C1至6烷基，R5表示C1至6的烷基。还描述了制备该化合物及其制剂和用途的方法 作为药物。

公开(公告)号：EP0174131A2

公开(公告)日：1986-03-12

申请号：EP85305930.1

申请日：1985-08-21

申请人： FISONS plc

发明人： Baxter, Andrew John Gilby ,  Dixon, John ,  Gould, Kenneth John ,  Tinker, Alan Charles

IPC分类号： C07D211/90 ,  C07D405/12 ,  C07D409/12 ,  C07D401/12 ,  C07D401/04 ,  C07D409/14 ,  C07D417/12 ,  C07D401/06 ,  A61K31/44

CPC分类号： C07D209/48 ,  C07C45/00 ,  C07C47/55 ,  C07C47/575 ,  C07C205/44 ,  C07D231/12 ,  C07D231/20 ,  C07D233/56 ,  C07D249/08 ,  C07D305/08 ,  C07D331/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

摘要： There are described compounds of formula 1,

in which R,, R 2 , R 3 , R s and R 6 are as defined in the specification and R 4 is a phenyl group carrying 3 or 4 substituents or is an unsaturated 5 membered heterocyclic group containing a single hetero-atom selected from oxygen, sulphur or nitrogen, R 4 being substituted by CF 3 , XR 22 , nitro, halogen, CN, alkyl C1 to 6, formyl dioxalanyl, -N(R 23 )COR 24 -CONR 25 R 26 , or amino which is optionally substituted by phenylsulphonyl or by trifluoroacetyl, and R 4 carries a substituent on the atom adjacent to the atom through which R 4 is connected to the remainder of the molecule,

R 22 is phenyl or alkyl C1 to 6 optionally substituted by halogen,
X is 0 or S(O) n ,
n is 0, 1 or 2, and
R 23 , R 24 , R 25 and R 26 , which may be the same or different, are each hydrogen or alkyl C1 to 6.

There are also described methods for making the compounds, and their formulation and use as pharmaceuticals, eg for the treatment of cardiovascular conditions.
There are further described compounds R 4 CHO which are useful in making compounds of formula I.

摘要翻译： 中描述了式I的化合物，其中R1，R2，R3，R5和R6如说明书中所定义和R 4是承载3个或4个取代基的苯基或是包含单一的不饱和5元杂环基团 选自氧，硫或氮，R 4由CF 3，XR22，硝基，卤素，CN，烷基C1〜6，二氧戊环基甲酰基是substituiertem的杂原子，-N（R23）COR24 -CONR25R26，或氨基其是由苯磺酰OPTIONALLY substituiertem 或三氟乙酰基，和R 4进行的原子毗邻通过其中R 4被连接到分子的其余部分的原子的取代基，R 22是苯基或烷基C1至由卤素6 OPTIONALLY substituiertem，X是O或S（O）N 中，n为0，1或2，且R23，R24，R25和R26，其可以是相同或不同，各自为氢或烷基C1〜6有这样描述了用于制备该化合物的方法以及它们的配制和使用 作为药品，例如用于心血管疾病的治疗。 有进一步描述化合物中，R 4 CHO它们在制备式I化合物的有用

公开(公告)号：EP0150966A2

公开(公告)日：1985-08-07

申请号：EP85300381.2

申请日：1985-01-21

申请人： FISONS plc

发明人： Dicker, Ian Douglas ,  Gould, Kenneth John ,  Suschitzky, John Louis

IPC分类号： C07D493/04 ,  C07D491/04 ,  C07D495/04 ,  C07D311/92 ,  C07D311/94 ,  A61K31/335 ,  A61K31/47

CPC分类号： C07D491/04 ,  C07D311/92 ,  C07D311/94 ,  C07D493/04 ,  C07D495/04

摘要： There are provided benzopyrans of formula I,
wherein an adjacent pair of R 5 , Re, R 7 and R 8 represent the chain -X-CR 12 R 13 -CR 14 R 15 -Y- in which the chain is substituted by -A 1 E 1 ,

X represents CR 10 R 11 or a single bond,
Y represents 0, S, NR 20 or CR 16 R 17 , and

(a) R 14 and R 20 together form a single bond and optionally R 10 and R 12 together form a single bond, or
(b) R 12 and R 14 together form a single bond, or
(c) Rio, R 12 and R 14 each represent hydrogen; and

the remainder of Rio, R 11 , R 12 , R 13 , R 14 , R 15 , R 16 and R 17 , which may be the same or different, independently represent hydrogen, alkyl, NR 21 COR 22 , CN or C n H x F (2+1-x) ; in addition, a a geminal pair of Rio, R 11 , R 12 , R 13 , R 14 , R 15 , R 16 and R 17 together with the carbon atoms to which they are attached, may represent C=O or C=N-OR 23 ; also a vicinal pair of R 11 , R 13 , R 15 and R 17 , may form the chain -CH =CH-CH=CH- which is substituted by A 1 E 1 ;
A and A 1 , which may be the same or different, represent a single bond, (CH 2 ) m or arylene,
n represents an integer from 1 to 10 inclusive,
x represents 0 or an integer from 1 to 2n inclusive,
m represents an integer from 1 to 10 inclusive, when R 20 does not form a single bond with R 14 , R 20 may represent hydrogen, alkyl, aryl or alkyl substituted by aryl,
R 21 , R 22 and R 23 , which may be the same or different, independently represent hydrogen, alkyl or aryl;
the remainder of R 5 , R 6 , R 7 and R 8 , which may be the same or different, each independently represent hydrogen, hydroxy, alkoxy, amino, halogen, nitro, cyano, alkyl, aryl or alkyl substituted by aryl,
E and E 1 , which may be the same or different, independently represent -COOH, or 5H-tetrazolyl,
with certain provisos defined herein,
and pharmaceutically acceptable derivatives thereof.
There are also decribed processes to the compounds of formula I and pharmaceutical, e.g. anti-asthma, compositions containing them.

摘要翻译： 提供式I的苯并吡喃，其中相邻的一对R 5，R 6，R 7和R 8表示链-X-CR 12 R 13 -CR 14 R 15 -Y-，其中链被-A 1 E 1取代，X表示CR 10 R 11或 单键，Y表示O，S，NR 20或CR 16 R 17，和（a）R 14和R 20一起形成单键，并且任选地R 10和R 12一起形成单键，或（b）R 12和R 14一起形成单键或（ c）R 10，R 12和R 14各自表示氢; R 10，R 11，R 12，R 13，R 14，R 15，R 16和R 17的其余部分可以相同或不同，独立地表示氢，烷基，NR 21 COR 22，CN或C n H x F（2 + 1-x）。 此外，R 10，R 11，R 12，R 13，R 14，R 15，R 16和R 17的偕对与它们所连接的碳原子一起可表示C = O或C = N-OR 23; 也可以是R11，R13，R15和R17的连位对，可以形成被A1E1取代的链-CH = CH-CH = CH-; A和A1可以相同或不同，表示单键，（CH2）m或亚芳基，n表示1〜10的整数，x表示0或1〜2n的整数，m表示整数 当R 20不与R 14形成单键时，R 20可以表示氢，烷基，芳基或芳基取代的烷基，R 21，R 22和R 23可以相同或不同，独立地表示氢，烷基 或芳基; R 5，R 6，R 7和R 8的其余部分可以相同或不同，各自独立地表示氢，羟基，烷氧基，氨基，卤素，硝基，氰基，烷基，芳基或被芳基，E和E1取代的烷基， 可以相同或不同，独立地表示-COOH或5H-四唑基，具有本文定义的某些条件及其药学上可接受的衍生物。 还有对式I化合物和药物，例如， 抗哮喘，含有它们的组合物。

公开(公告)号：EP0174131A3

公开(公告)日：1989-06-07

申请号：EP85305930.1

申请日：1985-08-21

申请人： FISONS plc

发明人： Baxter, Andrew John Gilby ,  Dixon, John ,  Gould, Kenneth John ,  Tinker, Alan Charles

IPC分类号： C07D211/90 ,  C07D405/12 ,  C07D409/12 ,  C07D401/12 ,  C07D401/04 ,  C07D409/14 ,  C07D417/12 ,  C07D401/06 ,  A61K31/44

CPC分类号： C07D209/48 ,  C07C45/00 ,  C07C47/55 ,  C07C47/575 ,  C07C205/44 ,  C07D231/12 ,  C07D231/20 ,  C07D233/56 ,  C07D249/08 ,  C07D305/08 ,  C07D331/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

摘要： There are described compounds of formula 1,

in which R,, R 2 , R 3 , R s and R 6 are as defined in the specification and R 4 is a phenyl group carrying 3 or 4 substituents or is an unsaturated 5 membered heterocyclic group containing a single hetero-atom selected from oxygen, sulphur or nitrogen, R 4 being substituted by CF 3 , XR 22 , nitro, halogen, CN, alkyl C1 to 6, formyl dioxalanyl, -N(R 23 )COR 24 -CONR 25 R 26 , or amino which is optionally substituted by phenylsulphonyl or by trifluoroacetyl, and R 4 carries a substituent on the atom adjacent to the atom through which R 4 is connected to the remainder of the molecule,
R 22 is phenyl or alkyl C1 to 6 optionally substituted by halogen, X is 0 or S(O) n , n is 0, 1 or 2, and R 23 , R 24 , R 25 and R 26 , which may be the same or different, are each hydrogen or alkyl C1 to 6. There are also described methods for making the compounds, and their formulation and use as pharmaceuticals, eg for the treatment of cardiovascular conditions. There are further described compounds R 4 CHO which are useful in making compounds of formula I.

摘要翻译： 描述了式I，其中R 1，R 2，R 3，R 5和R 6如本说明书中所定义的式I化合物，其中R 4为含3或4个取代基的苯基，或为含有单个取代基的不饱和5元杂环基 选自氧，硫或氮的杂原子，R 4被CF 3，XR 22，硝基，卤素，CN，C 1-6烷基，二甲基丙烯酰基，-N（R 23）COR 24 -CONR 25 R 26或任选被苯基磺酰基取代的氨基取代的 或者是三氟乙酰基，R 4在与R 4连接到该分子的其余部分的原子相邻的原子上携带取代基，R22是任选被卤素取代的苯基或C 1-6烷基，X是O或S（O）n ，n为0,1或2，R 23，R 24，R 25和R 26可以相同或不同，分别为氢或C1至6的烷基。还描述了制备化合物的方法及其制备和用途 作为药物，例如用于治疗心血管疾病。 进一步描述可用于制备式I化合物的化合物R4CHO。

公开(公告)号：EP0150966A3

公开(公告)日：1986-06-25

申请号：EP85300381

申请日：1985-01-21

申请人： FISONS plc

发明人： Gould, Kenneth John ,  Suschitzky, John Louis ,  Dicker, Ian Douglas

IPC分类号： C07D493/04 ,  C07D491/04 ,  C07D495/04 ,  C07D311/92 ,  C07D311/94 ,  A61K31/335 ,  A61K31/47

CPC分类号： C07D491/04 ,  C07D311/92 ,  C07D311/94 ,  C07D493/04 ,  C07D495/04

摘要： There are provided benzopyrans of formula I,
wherein an adjacent pair of R 5 , Re, R 7 and R 8 represent the chain -X-CR 12 R 13 -CR 14 R 15 -Y- in which the chain is substituted by -A 1 E 1 ,
X represents CR 10 R 11 or a single bond, Y represents 0, S, NR 20 or CR 16 R 17 , and
(a) R 14 and R 20 together form a single bond and optionally R 10 and R 12 together form a single bond, or (b) R 12 and R 14 together form a single bond, or (c) Rio, R 12 and R 14 each represent hydrogen; and the remainder of Rio, R 11 , R 12 , R 13 , R 14 , R 15 , R 16 and R 17 , which may be the same or different, independently represent hydrogen, alkyl, NR 21 COR 22 , CN or C n H x F (2+1-x) ; in addition, a a geminal pair of Rio, R 11 , R 12 , R 13 , R 14 , R 15 , R 16 and R 17 together with the carbon atoms to which they are attached, may represent C=O or C=N-OR 23 ; also a vicinal pair of R 11 , R 13 , R 15 and R 17 , may form the chain -CH =CH-CH=CH- which is substituted by A 1 E 1 ; A and A 1 , which may be the same or different, represent a single bond, (CH 2 ) m or arylene, n represents an integer from 1 to 10 inclusive, x represents 0 or an integer from 1 to 2n inclusive, m represents an integer from 1 to 10 inclusive, when R 20 does not form a single bond with R 14 , R 20 may represent hydrogen, alkyl, aryl or alkyl substituted by aryl, R 21 , R 22 and R 23 , which may be the same or different, independently represent hydrogen, alkyl or aryl; the remainder of R 5 , R 6 , R 7 and R 8 , which may be the same or different, each independently represent hydrogen, hydroxy, alkoxy, amino, halogen, nitro, cyano, alkyl, aryl or alkyl substituted by aryl, E and E 1 , which may be the same or different, independently represent -COOH, or 5H-tetrazolyl, with certain provisos defined herein, and pharmaceutically acceptable derivatives thereof. There are also decribed processes to the compounds of formula I and pharmaceutical, e.g. anti-asthma, compositions containing them.

公开(公告)号：EP0174071A2

公开(公告)日：1986-03-12

申请号：EP85304805.6

申请日：1985-07-05

申请人： FISONS plc

发明人： Baxter, Andrew John Gilby ,  Dixon, John ,  Gould, Kenneth John ,  Fuher, John

IPC分类号： C07D211/90 ,  A61K31/44

CPC分类号： C07D211/90

摘要： There are described compounds of formula I,
in which R 2 and R 3 , which may be the same or different, each represent alkyl C1 to 6 or cycloalkyl C3 to 8,

R 7 and R 8 , which may be the same or different, each represent alkyl C1 to 6 optionally substituted by halogen, and
X, Y and Z, which may be the same or different, are each hydrogen, halogen, nitro or alkyl C1 to 6 optionally substituted by halogen, or Z is as defined above and X and Y, together with the carbon atoms to which they are attached, form a C5 to 8 carbocyclic ring, other than a benzene ring,
provided that when R 2 , R 3 , R 7 and R 8 are all methyl and X and Z are hydrogen; or when R 2 and R 3 are both ethyl, R 7 and R 8 are both methyl and X and Z are hydrogen; then Y is other I than methyl.

There are also described methods for making the compounds and their formulation and use as pharmaceuticals, e.g. for the treatment of cardiovascular conditions.

摘要翻译： 描述了式I，的化合物，其中可以相同或不同的R 2和R 3各自代表烷基C1至6或环烷基C3至8，R7和R8各自可相同或不同 表示任选被卤素取代的C 1-6的烷基，X，Y和Z可以相同或不同，各自为氢，卤素，硝基或任选被卤素取代的C 1-6的烷基，或Z如上所定义，X为 并且Y与它们所连接的碳原子一起形成除苯环之外的C5至8碳环，条件是当R 2，R 3，R 7和R 8全部为甲基且X和Z为氢时; 或当R 2和R 3均为乙基时，R 7和R 8均为乙基，X和Z为氢; 那么Y不是甲基。 还描述了制备化合物及其制剂和用作药物的方法，例如， 用于治疗心血管疾病。

公开(公告)号：EP0125803A2

公开(公告)日：1984-11-21

申请号：EP84302566.9

申请日：1984-04-16

申请人： FISONS plc

发明人： Baxter, Andrew John Gilby ,  Dixon, John ,  Gould, Kenneth John ,  McInally, Thomas ,  Tinker, Alan Charles

IPC分类号： C07D211/90 ,  C07D211/78 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D401/06 ,  A61K31/445

CPC分类号： C07D231/12 ,  C07C17/093 ,  C07C45/00 ,  C07C47/55 ,  C07C205/56 ,  C07D205/04 ,  C07D211/78 ,  C07D211/90 ,  C07D233/56 ,  C07D249/08 ,  C07D305/08 ,  C07D309/12 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07C25/13

摘要： There are described compounds of formula I,

in which R 1 represents benzofurazanyl, pyridyl or phenyl, the pyridyl or phenyl being substituted,
-COOR 2 and -COOR 3 are various ester groups,
Yand Ztogetherform a bond, and additionally, when R. is an electron withdrawing group Y may be hydrogen and Z may be hydroxy,
one of R 7 and R. represents alkyl Cl to 6 and the other represents -CONR 10 R 11 ; -CSNH 2 ; -C(=NN)SR 9 ; -S(O) m R 9 ; phenyl optionally substituted by one or more of alkyl Cl to 6, halogen, alkoxy CI to 6 or nitro; alkyl Cl to 6 substituted by halogen; or furanyl,
or R 7 and R. may be the same or different and each represents phenyl optionally substituted by one or more of alkyl CI to 6, halogen, alkoxy Cl to 6 or nitro; amino; alkyl CI to 6 substituted by halogen; -CN; -CH 2 OH; -CHO or-CH(OR 9 ) 2 ,
m is 0 or 1
R 9 is alkyl CI to 6, and
R 10 and R 11 each independently represent hydrogen or alkyl Cl to 6, or together with the nitrogen atom to which they are attached form a 5 or 6 membered heterocyclic ring.
There are also described processes for making the compounds, and pharmaceutical, eg calcium antagonist, formulations containing them.

摘要翻译： 描述了式I的化合物，其中R 1表示苯并呋咱基，吡啶基或苯基，被取代的吡啶基或苯基，-COOR2和-COOR3是各种酯基，Y和Z一起形成键，此外，当 R8是吸电子基团Y可以是氢，Z可以是羟基，R 7和R 8之一表示烷基C 1-6，另一个代表-CON​​R 10 R 11; -CSNH2; -C（= NH）SR9; -S（O）MR9; 任选被一个或多个烷基C1至6，卤素，烷氧基C1至6或硝基取代的苯基; 被卤素取代的C1〜6烷基; 或呋喃基，或者R 7和R 8可以相同或不同，并且各自表示任选被一个或多个C 1-6烷基，卤素，烷氧基C 1-6或硝基取代的苯基; 氨基; 被卤素取代的C1〜6烷基; -CN; -CH2OH; -CHO或-CH（OR 9）2，m为0或1 R 9为C 1-6烷基，R 10和R 11各自独立地表示氢或烷基C 1-6，或与它们相连的氮原子一起形成5 或6元杂环。 还描述了制备化合物的方法和药物，例如钙拮抗剂，其含有它们的制剂。

公开(公告)号：EP0150966B1

公开(公告)日：1989-07-12

申请号：EP85300381.2

申请日：1985-01-21

申请人： FISONS plc

发明人： Dicker, Ian Douglas ,  Gould, Kenneth John ,  Suschitzky, John Louis

IPC分类号： C07D493/04 ,  C07D491/04 ,  C07D495/04 ,  C07D311/92 ,  C07D311/94 ,  A61K31/335 ,  A61K31/47

CPC分类号： C07D491/04 ,  C07D311/92 ,  C07D311/94 ,  C07D493/04 ,  C07D495/04

公开(公告)号：EP0312189A1

公开(公告)日：1989-04-19

申请号：EP88305220.1

申请日：1988-06-08

申请人： FISONS plc

发明人： Gould, Kenneth John

IPC分类号： C07D493/04 ,  A61K31/35

CPC分类号： C07D493/04

摘要： There is described the calcium salt of 10-propyl-­2,8-bis(1H-tetrazol-5-yl)-4H,6H-benzo(1,2-b;5,4-b′)dipyran-­4,6-dione and processes for its preparation.
Also described are pharmaceutical compositions containing the calcium salt and methods of treatment involving its use.

摘要翻译： 描述了10-丙基-2,8-双（1H-四唑-5-基）-4H，6H-苯并（1,2-b; 5,4-b min）二吡喃-4,6 并进行其制备。 还描述了含有钙盐的药物组合物和涉及其用途的治疗方法。