公开(公告)号：US4390541A

公开(公告)日：1983-06-28

申请号：US327146

申请日：1981-12-03

申请人： John Goldsworthy ,  William J. Ross ,  John P. Verge

发明人： John Goldsworthy ,  William J. Ross ,  John P. Verge

IPC分类号： C07D215/22 ,  A61K31/47 ,  A61P37/08 ,  C07D215/233 ,  C07D215/26 ,  C07D215/36 ,  C07D215/56

CPC分类号： C07D215/233 ,  C07C255/00 ,  C07D215/26 ,  C07D215/36 ,  C07D215/56

摘要： Compounds of the following formula are described: ##STR1## in which n is 0, 1 or 2, R.sup.1 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, trifluoromethyl, halo or nitro, and R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1-4 alkyl, and salts thereof. The compounds are useful in the treatment of immediate hypersensitivity conditions and are prepared by reaction of the appropriate formylquinolone with malonic acid, ylid or phosphonate.

摘要翻译： 描述了下式的化合物：其中n为0,1或2，R1为C1-4烷基，C1-4烷氧基，C1-4烷硫基，C1-4烷基磺酰基，三氟甲基，卤素或 硝基，R 2和R 3各自独立地为氢或C 1-4烷基，及其盐。 该化合物可用于治疗立即超敏反应病症，并通过适当的甲酰喹诺酮与丙二酸，内里膦酸或膦酸酯的反应来制备。

公开(公告)号：US4595540A

公开(公告)日：1986-06-17

申请号：US543196

申请日：1983-10-19

申请人： John Goldsworthy ,  Winston S. Marshall ,  John P. Verge

发明人： John Goldsworthy ,  Winston S. Marshall ,  John P. Verge

IPC分类号： A61K31/41 ,  A61P11/00 ,  A61P37/08 ,  C07C67/00 ,  C07C313/00 ,  C07C315/02 ,  C07C317/24 ,  C07C317/44 ,  C07C323/22 ,  C07C323/56 ,  C07C323/62 ,  C07C323/65 ,  C07C325/00 ,  C07C331/10 ,  C07D257/04 ,  C07C121/76 ,  C07C161/02

CPC分类号： C07D257/04

摘要： There are described compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl, X and Y are each oxygen, sulphur, sulphinyl or sulphonyl, n is 2 to 6 and Z is 1H-tetrazol-5-yl, 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl, cyano or thiocyano, provided that when both X and Y are oxygen Z is 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl or thiocyano; and salts thereof. The compounds in which Z is other than cyano or thiocyano have pharmaceutical activity and inhibit leukotriene action or formation. '

摘要翻译： 描述了式（I）的化合物，其中R 1是氢或C 1-6烷基，R 2是氢，C 1-6烷基或C 3-6烯基，X和Y各自是氧，硫，亚磺酰基或磺酰基，n是 2〜6，Z为1H-四唑-5-基，1H-四唑-5-基硫基，1H-四唑-5-基亚磺酰基，1H-四唑-5-基磺酰基，氰基或硫氰基，条件是当X和Y均为 氧Z是1H-四唑-5-基硫基，1H-四唑-5-基亚磺酰基，1H-四唑-5-基磺酰基或硫氰基; 及其盐。 其中Z不同于氰基或硫氰酸的化合物具有药物活性并抑制白三烯作用或形成。

公开(公告)号：US4740514A

公开(公告)日：1988-04-26

申请号：US866663

申请日：1986-05-27

申请人： John Goldsworthy ,  Winston S. Marshall ,  John P. Verge

发明人： John Goldsworthy ,  Winston S. Marshall ,  John P. Verge

IPC分类号： A61K31/41 ,  A61P11/00 ,  A61P37/08 ,  C07C67/00 ,  C07C313/00 ,  C07C315/02 ,  C07C317/24 ,  C07C317/44 ,  C07C323/22 ,  C07C323/56 ,  C07C323/62 ,  C07C323/65 ,  C07C325/00 ,  C07C331/10 ,  C07D257/04

CPC分类号： C07D257/04

摘要： There are described compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl, X and Y are each oxygen, sulphur, sulphinyl or sulphonyl, n is 2 to 6 and Z is 1H-tetrazol-5-yl, 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl, cyano or thiocyano, provided that when both X and Y are oxygen Z is 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl or thiocyano; and salts thereof. The compounds in which Z is other than cyano or thiocyano have pharmaceutical activity and inhibit leukotriene action or formation.

公开(公告)号：US4968711A

公开(公告)日：1990-11-06

申请号：US182648

申请日：1988-04-18

申请人： Stephen R. Baker ,  John Goldsworthy ,  William J. Ross

发明人： Stephen R. Baker ,  John Goldsworthy ,  William J. Ross

IPC分类号： C07D233/76 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4166 ,  A61P37/08 ,  C07C67/00 ,  C07C313/00 ,  C07C323/56 ,  C07C323/60 ,  C07D257/04 ,  C07D403/12 ,  C07D405/10

CPC分类号： C07D257/04 ,  C07D403/12 ,  Y02P20/55

摘要： There is disclosed a pharmaceutical compound of the formula ##STR1## in which R.sup.1 is C.sub.7-20 alkyl, C.sub.7-20 alkenyl, or C.sub.7-20 alkynyl, the alkyl, alkenyl or alkynyl group being optionally substituted by phenyl or substituted phenyl, R.sup.2 is --CN, --COOR.sup.3 or ##STR2## wherein R.sup.3 is hydrogen or a protecting group, X is alkylene containing 1 to 6 carbon atoms and Y is a nitrogen-containing group selected from ##STR3## where each R.sup.4 independently is hydrogen or C.sub.1-4 alkyl; and salts thereof.

公开(公告)号：US5863947A

公开(公告)日：1999-01-26

申请号：US853285

申请日：1997-05-09

申请人： Stephen Richard Baker ,  Barry Peter Clark ,  John Goldsworthy ,  John Richard Harris

发明人： Stephen Richard Baker ,  Barry Peter Clark ,  John Goldsworthy ,  John Richard Harris

IPC分类号： C07D295/14 ,  A61K31/195 ,  A61K31/245 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61P1/08 ,  A61P25/04 ,  A61P25/18 ,  C07C229/36 ,  C07C229/38 ,  C07C259/10 ,  C07C305/24 ,  C07C309/58 ,  C07C313/02 ,  C07D257/04 ,  C07D295/155 ,  C07D307/54 ,  C07D333/24 ,  C07D521/00 ,  C07F9/09 ,  C07F9/40 ,  C07C321/28

CPC分类号： C07D295/155 ,  C07C229/36 ,  C07C229/38 ,  C07D307/54 ,  C07D333/24

摘要： A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sup.2 is hydrogen, carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or aryl C.sub.1-6 alkyl,R.sup.3 is hydrogen, hydroxy or C.sub.1-4 alkoxy, andR.sup.4 is fluoro, trifluoromethyl, nitro, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkylthio, heteroaryl, optionally substituted aryl, optionally substituted aryl C.sub.1-6 alkyl, optionally substituted aryl C.sub.2-6 alkenyl, optionally substituted aryl C.sub.2-6 alkynyl, optionally substituted aryloxy, optionally substituted aryl C.sub.1-6 alkoxy, optionally substituted arylthio, optionally substituted aryl C.sub.1-6 alkylthio or --CONR"R'", --SO.sub.2 NR"R"", --NR"R'", --OCONR"R"' or --SONR"R'" where R" and R'" are each hydrogen, C.sub.1-6 alkyl or aryl C.sub.1-6 alkyl, or R" and R'" together form a C.sub.3-7 alkylene ring;provided that (i) R.sup.1, R.sup.2 and R.sup.3 are not all hydrogen,and (ii) when R.sup.2 and R.sup.3 are hydrogen and R.sup.1 is hydroxy, R.sup.4 is not fluoro;or a salt or ester thereof.

摘要翻译： 下式的药物化合物：其中R 1是氢，羟基或C 1-6烷氧基，R 2是氢，羧基，四唑基，-SO 2 H，-SO 3 H，-OSO 3 H，-CONHOH或-P（ OH）OR'，-PO（OH）OR'，-OP（OH）OR'或-OPO（OH）OR'，其中R'是氢，C 1-6烷基，C 2-6烯基或芳基C 1-6烷基， R3是氢，羟基或C1-4烷氧基，R4是氟，三氟甲基，硝基，C1-6烷基，C3-7环烷基，C2-6烯基，C2-6炔基，C1-6烷硫基，杂芳基，任选取代的芳基 ，任选取代的芳基C 1-6烷基，任选取代的芳基C 2-6烯基，任选取代的芳基C 2-6炔基，任选取代的芳氧基，任选取代的芳基C 1-6烷氧基，任选取代的芳硫基，任选取代的芳基C 1-6烷硫基或 - CONR''R“'，-SO2NR''R”'，-NR''R“'，-OCONR''R”'或-SONR''R“'，其中R”和R“ “各自为氢，C 1-6烷基或芳基C 1-6烷基，或R”和R“”一起形成C 3-7亚烷基环; 条件是（i）R 1，R 2和R 3不全部为氢，和（ii）当R 2和R 3为氢且R 1为羟基时，R 4不为氟; 或其盐或酯。

公开(公告)号：US5906985A

公开(公告)日：1999-05-25

申请号：US916028

申请日：1997-08-21

申请人： Stephen Richard Baker ,  Almudena Rubio Esteban ,  John Goldsworthy ,  Concepcion Pedregal Tercero

发明人： Stephen Richard Baker ,  Almudena Rubio Esteban ,  John Goldsworthy ,  Concepcion Pedregal Tercero

IPC分类号： A61K31/195 ,  A61P25/00 ,  A61P25/04 ,  C07C229/30 ,  C07C229/36 ,  C07C229/48 ,  A61K31/66

CPC分类号： C07C229/30 ,  Y02P20/55

摘要： Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and m is 1 or 2, R.sup.1 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, phenyl, naphthyl, C.sub.1-10 alkyl-phenyl, C.sub.2-10 alkenyl-phenyl or C.sub.2-10 alkynyl-phenyl, said phenyl and naphthyl groups being optionally substituted, R.sup.2 is hydrogen or a protecting group, and Q is an acidic group; or a salt or ester thereof.

摘要翻译： 下式的药物化合物，其中n为0,1或2，m为1或2，R1为氢，C1-10烷基，C2-10烯基，C2-10炔基，苯基，萘基，C1-10烷基 - 苯基 ，C 2-10烯基 - 苯基或C 2-10炔基 - 苯基，所述苯基和萘基任选被取代，R 2是氢或保护基，Q是酸性基团; 或其盐或酯。