公开(公告)号：US5374647A

公开(公告)日：1994-12-20

申请号：US42857

申请日：1993-04-05

申请人： Horst Bohagen ,  Ulrich Muller ,  Ulrich Rosentreter ,  Erwin Bischoff ,  Volker-Bernd Fiedler ,  Elisabeth Perzborn ,  Joachim Hutter ,  Peter Norman ,  Nigel J. Cuthbert ,  Hilary P. Francis ,  Marie G. McKenniff

发明人： Horst Bohagen ,  Ulrich Muller ,  Ulrich Rosentreter ,  Erwin Bischoff ,  Volker-Bernd Fiedler ,  Elisabeth Perzborn ,  Joachim Hutter ,  Peter Norman ,  Nigel J. Cuthbert ,  Hilary P. Francis ,  Marie G. McKenniff

IPC分类号： C07D209/86 ,  A61K31/40 ,  A61K31/403 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P37/08 ,  C07D209/88 ,  C07D209/94

CPC分类号： C07D209/88

摘要： Substituted antithrombotic substituted cycloalkano[b]dihydroindole- and -indole-sulphonamides for treatment of thromboses, thromboembolisms, ischaemias, asthma and allergies, of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen or other radicals,X is aryl, alkyl or CF.sub.3,m and Z each is 1,2,3 or 4,n is 0,1 or 2,A is a bond or --NH--, andY is OH, alkoxy, aryloxy, amino or sulphonylamine,with the proviso, that in all cases, two of the substituents R.sup.1 -R.sup.4 are other than hydrogen in the event that m represents the number 2 and Y represents the hydroxyl group, or a salt thereof.

摘要翻译： 取代的抗血栓形成取代的环烷基[b]二氢吲哚 - 和吲哚磺酰胺，用于治疗其他基团的血栓形成，血栓栓塞，局部缺血，哮喘和过敏，X是芳基，烷基或CF 3，m和Z各自为1 ，2,3或4，n为0,1或2，A为键或-NH-，Y为OH，烷氧基，芳氧基，氨基或磺酰胺，条件是在所有情况下，两个取代基 在m表示数2，Y表示羟基的情况下，R 1 -R 4不是氢，或其盐。

公开(公告)号：US5039670A

公开(公告)日：1991-08-13

申请号：US599321

申请日：1990-10-17

申请人： Horst Boshagen ,  Ulrich Muller ,  Ulrich Rosentreter ,  Erwin Bischoff ,  Volker-Bernd Fiedler ,  Elisabeth Perzborn ,  Joachim Hutter ,  Peter Norman ,  Nigel J. Cuthbert ,  Hilary P. Francis ,  Marie G. McKenniff

发明人： Horst Boshagen ,  Ulrich Muller ,  Ulrich Rosentreter ,  Erwin Bischoff ,  Volker-Bernd Fiedler ,  Elisabeth Perzborn ,  Joachim Hutter ,  Peter Norman ,  Nigel J. Cuthbert ,  Hilary P. Francis ,  Marie G. McKenniff

IPC分类号： C07D209/86 ,  A61K31/40 ,  A61K31/403 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P37/08 ,  C07D209/88 ,  C07D209/94

CPC分类号： C07D209/88

摘要： Substituted antithrombotic substituted cycloalkano[b]-dihydroindole- and -indole-sulphonamides for treatment of thromboses, thromboembolisms, ischemias, asthma and allergies, of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen or other radicals,X is aryl, alkyl or CF.sub.3,m and Z each is 1,2,3 or 4,n is 0, 1 or 2,A is a bond or --NH--, andY is OH, alkoxy, aryloxy, amino or sulphonylamine, with the proviso that, in all cases, two of the substituents R.sup.1 -R.sup.4 are other than hydrogen in the event that m represents the number 2 and Y represents the hydroxyl group,or a salt thereof.

摘要翻译： 用于治疗式（I）的血栓形成，血栓栓塞，缺血，哮喘和过敏的取代的抗血栓形成取代的环烷基[b] - 二氢吲哚和吲哚磺酰胺，其中R 1，R 2，R 3和R 4是氢或其它 基团，X是芳基，烷基或CF 3，m和Z各自为1,2,3或4，n为0,1或2，A为键或-NH-，Y为OH，烷氧基，芳氧基，氨基 或磺酰胺，条件是在所有情况下，在m表示数2且Y表示羟基的情况下，两个取代基R 1 -R 4不同于氢，或其盐。

公开(公告)号：US5096897A

公开(公告)日：1992-03-17

申请号：US678563

申请日：1991-03-28

申请人： Horst Boshagen ,  Ulrich Muller ,  Ulrich Rosentreter ,  Erwin Bischoff ,  Volker-Bernd Fiedler ,  Elisabeth Perzborn ,  Joachim Hutter ,  Peter Norman ,  Nigel J. Cuthbert ,  Hilary P. Francis ,  Marie G. McKenniff

发明人： Horst Boshagen ,  Ulrich Muller ,  Ulrich Rosentreter ,  Erwin Bischoff ,  Volker-Bernd Fiedler ,  Elisabeth Perzborn ,  Joachim Hutter ,  Peter Norman ,  Nigel J. Cuthbert ,  Hilary P. Francis ,  Marie G. McKenniff

IPC分类号： C07D209/86 ,  A61K31/40 ,  A61K31/403 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P37/08 ,  C07D209/88 ,  C07D209/94

CPC分类号： C07D209/88

摘要： Substituted antithrombotic substituted cycloalkano[b]-dihydroindole- and -indole-sulphonamides for treatment of thromboses, thromboembolisms, ischaemias, asthma and allergies, of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen or other radicals,X is aryl, alkyl or CF.sub.3,m and Z each is 1, 2, 3 or 4,n is 0, 1 or 2,A is a bond or --NH--, andY is OH, alkoxy, aryloxy, amino or sulphonylamine, with the proviso that, in all cases, two of the substituents R.sup.1 -R.sup.4 are other than hydrogen in the event that m represents the number 2 and Y represents the hydroxyl group,or a salt thereof.

公开(公告)号：US5204374A

公开(公告)日：1993-04-20

申请号：US679710

申请日：1991-04-03

申请人： Ulrich E. Muller ,  Ulrich Rosentreter ,  Ulrich Niewohner ,  Elisabeth Perzborn ,  Erwin Bischoff ,  Hans-Georg Dellweg ,  Peter Norman ,  Nigel J. Cuthbert ,  Hilary P. Francis

发明人： Ulrich E. Muller ,  Ulrich Rosentreter ,  Ulrich Niewohner ,  Elisabeth Perzborn ,  Erwin Bischoff ,  Hans-Georg Dellweg ,  Peter Norman ,  Nigel J. Cuthbert ,  Hilary P. Francis

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61P7/02 ,  A61P11/00 ,  A61P37/08 ,  C07D209/86 ,  C07D209/94 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12

CPC分类号： C07D401/12 ,  C07D409/12 ,  C07D417/12

摘要： New cycloalkano[b]dihydroindoles and -indolesulphonamides, substituted by heterocycles, of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different andrepresent hydrogen, nitro, cyano, halogen, trifluoromethyl, carboxyl, hydroxyl or trifluoromethoxy, orrepresent a group of the formula --S(O).sub.w R.sup.5, in whichR.sup.5 denotes alkyl or optionally substituted aryl,w denotes the number 0, 1 or 2, orrepresents alkoxy or alkoxycarbonyl, or benzyloxy, orrepresents a group of the formula --NR.sup.6 R.sup.7, in whichR.sup.6 and R.sup.7 are identical or different anddenote hydrogen, alkyl or acyl ordenote aryl, ordenote a group of the formula --S(O).sub.w R.sup.5, in which R.sup.5 and w have the abovementioned meaning,represent cycloalkyl orrepresent optionally substituted alkyl or alkenyl,m represents the number 1, 2, 3 or 4,n represents the number 0, 1 or 2,z represents the number 1, 2, 3 or 4,A represents a bond or the --NH group,X represents an optionally substituted heterocycle,Y represents hydroxyl, alkoxy, phenoxy or a group of the formula --NR.sup.6 R.sup.7, in whichR.sup.6 and R.sup.7 have the abovementioned meaning, an isomeric form thereof or salts thereof are useful to treat thromboembolisms, ischaemias, asthma and allergies. Processes of making and chemical intermediates are also disclosed.

公开(公告)号：US5264458A

公开(公告)日：1993-11-23

申请号：US913513

申请日：1992-07-14

申请人： Ulrich Niewohner ,  Franz-Peter Hoever ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler ,  Peter Norman ,  Hilary P. Francis ,  Marie G. McKenniff

发明人： Ulrich Niewohner ,  Franz-Peter Hoever ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler ,  Peter Norman ,  Hilary P. Francis ,  Marie G. McKenniff

IPC分类号： C07C237/06 ,  C07C311/17 ,  C07C311/29 ,  C07D311/92 ,  C07D311/94 ,  C07D493/04 ,  A61K31/24 ,  A61K31/18 ,  A61K31/19

CPC分类号： C07D493/04 ,  C07C237/06 ,  C07C311/17 ,  C07C311/29 ,  C07D311/92 ,  C07D311/94 ,  C07C2102/08 ,  C07C2102/10 ,  C07C2103/24 ,  C07C2103/26

摘要： Iso- and heterocyclic phenylsulphonamides can be prepared by reaction of corresponding iso- and heterocyclic amines with phenylsulphonic acid derivatives. The iso- and heterocyclic phenylsulphonamides have thrombocyte aggregation-inhibiting and thromboxane A.sub.2 antagonist action and can be used in medicaments.

摘要翻译： 异构和杂环苯基磺酰胺可以通过相应的异杂环胺和苯基磺酸衍生物的反应来制备。 异硫醚和杂环苯基磺酰胺具有血小板聚集抑制和血栓素A2拮抗作用，可用于药物。

公开(公告)号：US5246966A

公开(公告)日：1993-09-21

申请号：US816162

申请日：1991-12-30

申请人： Heinrich Meier ,  John E. B. Ransohoff ,  Trevor S. Abram ,  Peter Norman ,  Tudhope Stephen R. ,  Phillip J. Gardiner ,  Nigel J. Cuthbert ,  Hilary P. Francis

发明人： Heinrich Meier ,  John E. B. Ransohoff ,  Trevor S. Abram ,  Peter Norman ,  Tudhope Stephen R. ,  Phillip J. Gardiner ,  Nigel J. Cuthbert ,  Hilary P. Francis

IPC分类号： C07C323/62 ,  A61K31/19 ,  A61K31/194 ,  A61K31/235 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C20060101 ,  C07C69/734 ,  C07C319/20

CPC分类号： C07C69/734 ,  C07C323/62

摘要： The new substituted alkenoic acid derivatives can be prepared by reacting the appropriate aldehyde with a phosphonium compound. The compounds have leukotriene antagonistic properties and can be incorporated into pharmaceutical compositions.

公开(公告)号：US5221760A

公开(公告)日：1993-06-22

申请号：US891629

申请日：1992-06-01

申请人： Ulrich Rosentreter ,  Harold C. Kluender ,  Trevor S. Abram ,  Peter Norman ,  Steven R. Tudhope

发明人： Ulrich Rosentreter ,  Harold C. Kluender ,  Trevor S. Abram ,  Peter Norman ,  Steven R. Tudhope

IPC分类号： C07C43/225 ,  C07C43/23 ,  C07C63/14 ,  C07C65/24 ,  C07C309/73 ,  C07C323/56 ,  C07F7/18 ,  C07F9/54

CPC分类号： C07F9/5456 ,  C07C309/73 ,  C07C323/56 ,  C07C43/225 ,  C07C43/23 ,  C07C63/14 ,  C07C65/24 ,  C07F7/1852 ,  C07F9/5407

摘要： An alkenoic acid derivative of the formula ##STR1## in which X and Y are identical or different and represent sulfur, sulfoxide, sulfone, an alkylene chain, --SCH.sub.2 --, or oxygen or a direct bond,W represents --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --,o represents a number 1 to 5,A and B are identical or different and represent carboxyl, carboxymethylene, tetrazolyl or tetrazolylmethylene, or --CO.sub.2 R.sup.9 or --CH.sub.2 CO.sub.2 R.sup.9 or --CONR.sup.10 R.sup.11 or nitrilen represents a number 1 to 10,m represents a number 0 to 7,T and Z are identical or different and represent oxygen or a direct bond andR.sup.2, R.sup.3, R.sup.8 are identical or different and represent hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano or nitro andR.sup.9 is lower alkyl and R.sup.10 and R.sup.11 are hydrogen, lower alkyl, alkylsulfonyl or arylsulfonyl or together are an alkylene chain to form a ringand pharmaceutically acceptable salts thereof. Such alkenoic acid derivatives are useful as leucotriene disease antagonists.

摘要翻译： 其中X和Y相同或不同并表示硫，亚砜，砜，亚烷基链，-SCH 2 - 或氧或直接键的式（I）的链烯酸衍生物，W表示-CH = CH-或-CH 2 -CH 2 - ，o表示数1至5，A和B相同或不同，表示羧基，羧基亚甲基，四唑基或四唑基亚甲基，或-CO 2 R 9或-CH 2 CO 2 R 9或-CONR 10 R 11或腈n表示1 至10，m表示0至7的数，T和Z相同或不同，表示氧或直接键，R2，R3，R8相同或不同，表示氢，烷基，烷氧基，卤素，三氟甲基，三氟甲氧基，氰基 或硝基，R 9为低级烷基，R 10和R 11为氢，低级烷基，烷基磺酰基或芳基磺酰基，或一起为形成环的亚烷基链及其药学上可接受的盐。 这样的链烯酸衍生物可用作白三烯类疾病拮抗剂。

公开(公告)号：US5159097A

公开(公告)日：1992-10-27

申请号：US618184

申请日：1990-11-26

申请人： Ulrich Rosentreter ,  Harold C. Kluender ,  Trevor S. Abram ,  Peter Norman ,  Steven R. Tudhope

发明人： Ulrich Rosentreter ,  Harold C. Kluender ,  Trevor S. Abram ,  Peter Norman ,  Steven R. Tudhope

IPC分类号： A61K31/19 ,  A61K31/215 ,  A61K31/235 ,  A61K31/275 ,  A61K31/41 ,  A61P11/08 ,  A61P43/00 ,  C07C43/225 ,  C07C43/23 ,  C07C51/353 ,  C07C63/14 ,  C07C63/66 ,  C07C65/24 ,  C07C65/28 ,  C07C67/343 ,  C07C69/76 ,  C07C69/94 ,  C07C309/73 ,  C07C317/44 ,  C07C317/46 ,  C07C319/20 ,  C07C323/52 ,  C07C323/56 ,  C07C323/62 ,  C07C323/65 ,  C07D257/06 ,  C07F7/18 ,  C07F9/54

CPC分类号： C07F9/5456 ,  C07C309/73 ,  C07C323/56 ,  C07C43/225 ,  C07C43/23 ,  C07C63/14 ,  C07C65/24 ,  C07F7/1852 ,  C07F9/5407

摘要： An alkenoic acid derivative of the formula ##STR1## in which X and Y are identical or different and represent sulfur, sulfoxide, sulfone, an alkylene chain, --SCH.sub.2 --, or oxygen or a direct bond,W represents --CH.dbd.CH--or --CH.sub.2 --CH.sub.2 --,o represents a number 1 to 5,A and B are identical or different and represent carboxyl, carboxymethylene, tetrazolyl or tetrazolylmethylene, or --CO.sub.2 R.sup.9 or --CH.sub.2 CO.sub.2 R.sup.9 or --CONR.sup.10 R.sup.11 or nitrilen represents a number 1 to 10,m represents a number 0 to 7,T and Z are identical or different and represent oxygen or a direct bond andR.sup.2, R.sup.3, R.sup.8 are identical or different and represent hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano or nitro andR.sup.9 is lower alkyl and R.sup.10 and R.sup.11 are hydrogen, lower alkyl, alkylsulfonyl or arylsulfonyl or together are an alkylene chain to form a ringand pharmaceutically acceptable salts thereof. Such alkenoic acid derivatives are useful as leucotriene disease antagonists.

摘要翻译： 其中X和Y相同或不同并表示硫，亚砜，砜，亚烷基链，-SCH 2 - 或氧或直接键的式（I）的链烯酸衍生物，W表示-CH = CH-或-CH 2 -CH 2 - ，o表示数1至5，A和B相同或不同，表示羧基，羧基亚甲基，四唑基或四唑基亚甲基，或-CO 2 R 9或-CH 2 CO 2 R 9或-CONR 10 R 11或腈n表示1 至10，m表示0至7的数，T和Z相同或不同，表示氧或直接键，R2，R3，R8相同或不同，表示氢，烷基，烷氧基，卤素，三氟甲基，三氟甲氧基，氰基 或硝基，R 9为低级烷基，R 10和R 11为氢，低级烷基，烷基磺酰基或芳基磺酰基，或一起为形成环的亚烷基链及其药学上可接受的盐。 这样的链烯酸衍生物可用作白三烯类疾病拮抗剂。

公开(公告)号：US5266713A

公开(公告)日：1993-11-30

申请号：US928693

申请日：1992-08-12

申请人： Trevor S. Abram ,  Peter Norman ,  Stephen R. Tudhope ,  Harold C. Kluender ,  Robert N. Schut ,  Heinrich Meier ,  Ulrich Rosentreter

发明人： Trevor S. Abram ,  Peter Norman ,  Stephen R. Tudhope ,  Harold C. Kluender ,  Robert N. Schut ,  Heinrich Meier ,  Ulrich Rosentreter

IPC分类号： C07C323/56 ,  C07C323/60 ,  C07C323/62 ,  C07C235/00

CPC分类号： C07C323/56 ,  C07C323/60 ,  C07C323/62

摘要： Aryl alkenoic acid derivatives, and physiologically acceptable salts thereof, are provided which are potent leukotriene antagonists and may be used for the treatment of circulatory diseases and preferably for respiratory diseases such as asthma. The derivatives have a general formula I ##STR1## in which X is --S--,W is CH.dbd.CH;o is 1 to 4;n is 2 to 6;m is 0 to 2;T and Z, same or different, represent oxygen or a direct bond;R.sup.2 and R.sup.3, represent hydrogen, or fluorine;A represents carboxyl, CO.sub.2 R.sub.4.sup.4, wherein R.sup.4 is lower alkylR is ##STR2## wherein Y represents carboxyl, CO.sub.2 R.sup.4, wherein R.sup.4 is lower alkylR.sup.7 and R.sup.8, same or different, represent H or lower alkyl;R.sup.9 represents --OH, --O-alkyl, NH.sub.2 or a NHCH.sub.2 CO.sub.2 H group; andR.sup.10 R3 is H.

摘要翻译： 提供了芳基链烯酸衍生物及其生理上可接受的盐，它们是有效的白三烯拮抗剂，可用于治疗循环系统疾病，优选用于呼吸系统疾病如哮喘。 衍生物具有通式I（I）其中X是-S-，W是CH = CH; o是1到4; n为2〜6; m为0〜2; T和Z相同或不同，代表氧或直接键; R2和R3代表氢或氟; A表示羧基，CO 2 R 44，其中R 4是低级烷基R 3是其中Y表示羧基，CO 2 R 4，其中R 4是低级烷基，R 7和R 8相同或不同，表示H或低级烷基; R9表示-OH，-O-烷基，NH2或NHCH2CO2H基团; R10 R3为H.

公开(公告)号：US5041638A

公开(公告)日：1991-08-20

申请号：US349371

申请日：1989-05-09

申请人： Ulrich Rosentreter ,  Harold C. Kluender ,  Trevor S. Abram ,  Peter Norman ,  Steven R. Tudhope

发明人： Ulrich Rosentreter ,  Harold C. Kluender ,  Trevor S. Abram ,  Peter Norman ,  Steven R. Tudhope

IPC分类号： A61K31/19 ,  A61K31/215 ,  A61K31/235 ,  A61K31/275 ,  A61K31/41 ,  A61P11/08 ,  A61P43/00 ,  C07C43/225 ,  C07C43/23 ,  C07C51/353 ,  C07C63/14 ,  C07C63/66 ,  C07C65/24 ,  C07C65/28 ,  C07C67/343 ,  C07C69/76 ,  C07C69/94 ,  C07C309/73 ,  C07C317/44 ,  C07C317/46 ,  C07C319/20 ,  C07C323/52 ,  C07C323/56 ,  C07C323/62 ,  C07C323/65 ,  C07D257/06 ,  C07F7/18 ,  C07F9/54

CPC分类号： C07F9/5456 ,  C07C309/73 ,  C07C323/56 ,  C07C43/225 ,  C07C43/23 ,  C07C63/14 ,  C07C65/24 ,  C07F7/1852 ,  C07F9/5407

摘要： An alkenoic acid derivative of the formula ##STR1## in which X and Y are identical or different and represent sulfur, sulfoxide, sulfone, an alkylene chain, --SCH.sub.2 --, or oxygen or a direct bond,W represents --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --,o represents a number 1 to 5,A and B are identical or different and represent carboxyl, carboxymethylene, tetrazolyl or tetrazolylmethylene, or --CO.sub.2 R.sup.9 or --CH.sub.2 CO.sub.2 R.sup.9 or --CONR.sup.10 R.sup.11 or nitrilen represents a number 1 to 10,m represents a number 0 to 7,T and Z are identical or different and represent oxygen or a direct bond andR.sup.2, R.sup.3, R.sup.8 are identical or different and represent hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano or nitro andR.sup.9 is lower alkyl and R.sup.10 and R.sup.11 are hydrogen, lower alkyl, alkylsulfonyl or arylsulfonyl or together are an alkylene chain to form a ringand pharmaceutically acceptable salts thereof. Such alkenoic acid derivatives are useful as leucotriene disease antagonists.