公开(公告)号：US07087605B2

公开(公告)日：2006-08-08

申请号：US10480947

申请日：2002-05-21

Applicant: Cristina Alonso-Alija ,  Heike Gielen ,  Martin Hendrix ,  Maria Theresia Niewohner, legal representative ,  Dagmar Schauss ,  Hilmar Bischoff ,  Nils Burkhardt ,  Volker Geiss ,  Karl-Heinz Schlemmer ,  Nigel J. Cuthbert ,  Mary F. Fitzgerald ,  Richard Graham Sturton ,  Martin Michels

Inventor： Ulrich Niewohner, deceased

IPC: C07D487/04 ,  A61K31/53 ,  A61P11/06 ,  A61P11/08

CPC classification number: C07D253/07 ,  C07D405/12 ,  C07D487/04

Abstract: The invention relates to novel 5-Ethyl-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.

Abstract translation: 本发明涉及新的5-乙基咪唑并三嗪酮，其制备方法及其在药物中的应用， 用于治疗和/或预防炎症过程和/或免疫疾病。

公开(公告)号：US5332755A

公开(公告)日：1994-07-26

申请号：US820109

申请日：1992-01-13

Applicant: John E. Butler ,  Nigel J. Cuthbert

Inventor： John E. Butler ,  Nigel J. Cuthbert

IPC: C07D209/08 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D209/12 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  A61K31/41

CPC classification number: C07D403/04 ,  C07D209/12

Abstract: Indole derivative for leucotriene antagonism of the formula ##STR1## wherein groups A, B, D, E, F and G are as described in the specification.

Abstract translation: 其中基团A，B，D，E，F和G如说明书中所述的式“IMAGE”的白三烯拮抗剂的吲哚衍生物。

公开(公告)号：US5204374A

公开(公告)日：1993-04-20

申请号：US679710

申请日：1991-04-03

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

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

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

CPC classification number: C07D401/12 ,  C07D409/12 ,  C07D417/12

Abstract: 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：US5118700A

公开(公告)日：1992-06-02

申请号：US547560

申请日：1990-07-02

Applicant: John E. Butler ,  Nigel J. Cuthbert

Inventor： John E. Butler ,  Nigel J. Cuthbert

IPC: C07D209/08 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D209/12 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D403/04 ,  C07D209/12

Abstract: Indole derivative for leukotriene antagonists of the formula ##STR1## wherein groups A, B, D, E, F & G are as described in the specification.

Abstract translation: 其中组A，B，D，E，F和G如说明书中所述的式IIIA的白三烯拮抗剂的吲哚衍生物。

公开(公告)号：US5096897A

公开(公告)日：1992-03-17

申请号：US678563

申请日：1991-03-28

Applicant: 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

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

CPC classification number: C07D209/88

Abstract: 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：US5374647A

公开(公告)日：1994-12-20

申请号：US42857

申请日：1993-04-05

Applicant: 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

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

CPC classification number: C07D209/88

Abstract: 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.

Abstract translation: 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：US07115602B2

公开(公告)日：2006-10-03

申请号：US10160352

申请日：2002-05-30

Applicant: Cristina Alonso-Alija ,  Heike Gielen ,  Martin Hendrix ,  Maria Niewöhner ,  Dagmar Schauss ,  Hilmar Bischoff ,  Nils Burkhardt ,  Volker Geiss ,  Karl-Heinz Schlemmer ,  Nigel J. Cuthbert ,  Mary F. Fitzgerald ,  Graham Sturton

Inventor： Ulrich Niewöhner

IPC: A01N43/64 ,  A61K31/53 ,  C07D487/00

CPC classification number: C07D253/07 ,  C07D487/04

Abstract: The invention relates to 7-(4-tert butyl-cyclohexyl)-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.

Abstract translation: 本发明涉及7-（4-叔丁基 - 环己基） - 咪唑并三嗪酮，其制备方法及其在药物中的应用， 用于治疗和/或预防炎症过程和/或免疫疾病。

公开(公告)号：US5039670A

公开(公告)日：1991-08-13

申请号：US599321

申请日：1990-10-17

Applicant: 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

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

CPC classification number: C07D209/88

Abstract: 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.

Abstract translation: 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：US5246966A

公开(公告)日：1993-09-21

申请号：US816162

申请日：1991-12-30

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

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

IPC: 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 classification number: C07C69/734 ,  C07C323/62

Abstract: 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.