公开(公告)号：AT122659T

公开(公告)日：1995-06-15

申请号：AT93102220

申请日：1993-02-12

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  MANIA DIETER DR ,  WETTLAUFER DAVID DR ,  KLAUS ERIK DR

IPC: A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4425 ,  A61P9/00 ,  A61P21/00 ,  C07D213/64 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D213/89 ,  C07D401/12 ,  A61K31/455 ,  C07D213/82 ,  A61K31/495 ,  A61K31/47

Abstract: Arylcarbonylaminoalkyl-dihydro-oxo-pyridines of Formula I are disclosed wherein aryl is an aromatic or heteroaromatic system, n is zero through 5; R and R(1), are hydrogen, or loweralkyl; W is hydrogen, (hetero)-(aryl)-loweralkyl; Z is hydrogen, CH2OR(2), CHO, (CO)OR(2), (CO)NR(2)2. Processes for the preparation of compound I are also disclosed. Compounds I are suitable for the treatment of disorders of the cardiovascular system, for example of hypertension, of cardiac insufficiency or of disturbances of blood flow in the coronary systems such as, for example, angina. Disturbances of cerebral and peripheral blood flow are likewise influenced beneficially. Furthermore, compounds I are able to influence smooth-muscle organs such as uterus, bronchi, intestines and biliary system, the urinary tract (ureter, bladder and urethra) in the sense of spasmolysis. They are therefore also suitable for the treatment of diseases associated with spasms of these organs, for example for the treatment of premature labor in pregnancy, of ureteral or biliary colic, of obstructive airway diseases such as asthma, of disturbances of intestinal motility such as, for example, of irritable colon or of bladder incontinence. Additionally, compounds of formula I can serve as anti-convulsants in the treatment of epilepsy and as hair growth inducers in the treatment of baldness.

公开(公告)号：AT248829T

公开(公告)日：2003-09-15

申请号：AT96101096

申请日：1996-01-26

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  HARTUNG JENS DR ,  CRAUSE PETER DR ,  MANIA DIETER DR ,  GOEGELEIN HEINZ DR ,  KAISER JOACHIM DR

IPC: A61K31/38 ,  A61K31/381 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P43/00 ,  C07C335/00 ,  C07D333/34

Abstract: N-((2-Benzamidoethyl)- thiophene-sulphonyl)-urea or-thiourea derivs. of formula (I) are new. R1 = H, halogen, Me, Et, OMe, OEt, SMe, SEt, 1-2C fluoroalkyl or 1-2C fluoroalkoxy; X = O or S; R2 = H, Me or CF3; Y, Z = H, F, Cl, Br, I, Me, Et, OMe or OEt.

公开(公告)号：DK0726250T3

公开(公告)日：2001-01-08

申请号：DK96101585

申请日：1996-02-05

Applicant: HOECHST AG

Inventor： GOEGELEIN HEINZ DR ,  KAISER JOACHIM DR ,  CRAUSE PETER DR ,  ENGLERT HEINRICH DR ,  GERLACH UWE DR ,  MANIA DIETER DR

IPC: C07D333/20 ,  A61K31/18 ,  A61K31/34 ,  A61K31/35 ,  A61K31/38 ,  A61K31/381 ,  A61K31/395 ,  A61K31/40 ,  A61K31/425 ,  A61K31/426 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  C07C233/00 ,  C07C303/40 ,  C07C311/58 ,  C07C327/40 ,  C07C335/42 ,  C07D207/32 ,  C07D207/335 ,  C07D213/40 ,  C07D277/28 ,  C07D307/52

Abstract: Substd. benzenesulphonylurea or -thiourea cpds. of formula (I) are new: R1 = H, 1-6C alkyl, or 3-6C cycloalkyl; R2 = 1-6C alkyl, 1-6C alkoxy, 1-6C mercaptoalkyl, 3-6C cycloalkyl, or a 1-8C chain in which 1-3C may be replaced by O, NH or S; R3, R4 = H or 1-6C alkyl; or R3 + R4 = (CH2)p; p = 2-5; E, X = O or S; Y = ÄC(R5)2Üm; R5 = H, Me or Et; m = 1 or 2; Ar = phenyl, thienyl, furyl, pyrrolyl, thiazolyl, naphthyl or pyridyl (all opt. substd. by 1-3 Me, Et, MeO, EtO, Cl, Br or F).

公开(公告)号：ES2149234T3

公开(公告)日：2000-11-01

申请号：ES94120773

申请日：1994-12-27

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  MANIA DIETER DR ,  HARTUNG JENS DR ,  GOGELEIN HEINZ DR ,  KAISER JOACHIM DR ,  GERLACH UWE DR

IPC: C07D217/24 ,  A61K31/40 ,  A61K31/64 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  A61P43/00 ,  C07C303/36 ,  C07C311/58 ,  C07C335/42 ,  C07D207/38 ,  C07D521/00

Abstract: There are described substituted benzenesulphonylureas and -thioureas of the formula I where R(1) is H, (cyclo)(CH2)a(fluoro)alk(en)yl, R(2) is H, Hal, (fluoro)(mercapto)(CH2)e(cyclo)alk(oxy)(yl), NR(4)R(5) where R(4) and R(5) together are a (CH2)2-7 chain, or R(4), R(5), R(6) are H, (alkyl)(cyclo)(fluoro)alk(en)yl, E is O, S; Y is -[CR(7)2]n-R(3) B is (C3-C6)-alkenyl, or R(3) is X is H, Hal, alkyl; Z is Hal, (cyclo)alk(yl)(oxy). Compounds I are used for the treatment of cardiac arrhythmias and for the prevention of sudden heart death caused by arrhythmia and can therefore be used as antiarrhythmics. They are particularly suitable in those cases in which arrhythmias are the result of constriction of a coronary vessel, such as in angina pectoris or in acute cardiac infarct.

公开(公告)号：DK0657423T3

公开(公告)日：1999-07-19

申请号：DK94118931

申请日：1994-12-01

Applicant: HOECHST AG

Inventor： GOEGELEIN HEINZ DR ,  KAISER JOACHIM DR ,  ENGLERT HEINRICH DR ,  MANIA DIETER DR ,  HARTUNG JENS DR

IPC: A61K31/64 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C303/36 ,  C07C311/57 ,  C07C311/58 ,  C07C335/42 ,  C07D295/135

Abstract: Amino-substituted benzenesulphonylureas and -thioureas of the formula I are described. The compounds I are used for treating cardiac dysrhythmias and for preventing sudden heart death due to arrhythmias and can therefore be used as antiarrhythmics. They are particularly suitable for cases in which arrhythmias are the consequence of a constriction of a coronary vessel, such as in angina pectoris or acute myocardial infarct.

公开(公告)号：AU701278B2

公开(公告)日：1999-01-21

申请号：AU4560096

申请日：1996-02-19

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  GERLACH UWE DR ,  MANIA DIETER DR ,  GOGELEIN HEINZ DR ,  KAISER JOACHIM DR

IPC: C07D331/02 ,  A61K31/18 ,  A61K31/38 ,  A61K31/64 ,  A61P9/00 ,  A61P9/02 ,  A61P9/06 ,  A61P9/10 ,  C07C233/00 ,  C07C303/40 ,  C07C311/58 ,  C07C327/46 ,  C07C335/42 ,  C07D203/08 ,  C07D295/00 ,  C07D303/48 ,  A61K31/17

Abstract: N-(3-substd. benzensulphonyl)-urea or -thiourea derivs. of formula (I) and their salts are new. R1 = H, 1-7C alkyl or 3-7C cycloalkyl; R2 = H, F, Cl, 1-6C alkyl, 1-6C alkoxy, 1-6C mercaptoalkyl, 3-6C cycloalkyl or CbH2b+1, in which one or more C can be replaced by Het; Het = heteroatoms, e.g. O, NH or S; b = 1-8; 1-8C alkyl in which 1-4C may be replaced by O, N or S; R3 = H, 1-12C alkyl, 3-10C cycloalkyl, 1-6C fluoroalkyl, 3-6C fluorocycloalkyl or CaH2a+1 in which 1-4C are replaced by Het; a = 1-10; R4 = aryl or as R3; or R3+R4 = CbH2b, in which one or more CH2 can be replaced by Het; R5 = as R4; R6 = as R4 but not 3-10C cycloalkyl; Q, X = O or S; Y = -(C(R7)2)c, O, S or NH; c = 1-4; R7 = H, 1-4C alkyl, F, Cl or Br.

公开(公告)号：ES2114874T3

公开(公告)日：1998-06-16

申请号：ES91122406

申请日：1992-01-01

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT DR ,  ENGLERT HEINRICH DR ,  KLEEMANN HEINZ-WERNER DR ,  GERHARDS HERMANN DR ,  SCHOLKENS BERNWARD PROF DR ,  BECKER REINHARD DR

IPC: A61K31/40 ,  A61K31/415 ,  A61K31/425 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/64 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D207/34 ,  C07D207/36 ,  C07D233/54 ,  C07D233/66 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D233/90 ,  C07D249/02 ,  C07D255/02 ,  C07D257/02 ,  C07D257/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D453/02 ,  C07D521/00

Abstract: Azole derivative of the general formula (I) in which A, L, O, R , X, Y, Z and q have the meanings given, a process for their preparation, pharmaceutical preparations and the use of the compounds are described. Azole derivatives of the formula I where the symbols have, for example, the following meanings: R = (C2-C10)-alkyl Z = nitrogen X and Y = independently of one another CR L = -CH2- q = zero or 1 A = biphenyl radical which is substituted, for example, by R R = halogen or hydrogen R = SO2-NH-CO-OR and R = phenyl, are highly active antagonists of angiotensin II receptors.

公开(公告)号：CZ28096A3

公开(公告)日：1998-04-15

申请号：CZ28096

申请日：1996-01-30

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  HARTUNG JENS DR ,  CRAUSE PETER DR ,  MANIA DIETER DR ,  GOGELEIN HEINZ DR ,  KAISER JOACHIM DR

IPC: A61K31/38 ,  A61K31/381 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P43/00 ,  C07C335/00 ,  C07D333/34

Abstract: N-((2-Benzamidoethyl)- thiophene-sulphonyl)-urea or-thiourea derivs. of formula (I) are new. R1 = H, halogen, Me, Et, OMe, OEt, SMe, SEt, 1-2C fluoroalkyl or 1-2C fluoroalkoxy; X = O or S; R2 = H, Me or CF3; Y, Z = H, F, Cl, Br, I, Me, Et, OMe or OEt.

公开(公告)号：GR3024731T3

公开(公告)日：1997-12-31

申请号：GR970402375

申请日：1997-09-16

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  MANIA DIETER DR ,  LANG HANS-JOCHEN DR ,  SCHOLZ WOLFGANG DR ,  LINZ WOLFGANG DR ,  ALBUS UDO DR

IPC: A61K31/155 ,  A61K31/165 ,  A61K31/445 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C279/22 ,  C07D213/65 ,  C07D295/14 ,  C07D295/155

Abstract: There are described benzoylguanidines of the formula I in which R(1) or R(2) is an amino group -NR(3)R(4), where R(3) and R(4) are equal to H, (cyclo)alkyl or R(3) is equal to phenyl-(CH2)p- where p = 0, 1, 2, 3 or 4, or phenyl, or R(3) and R(4) together can also be a methylene chain, and in which the other substituent R(1) or R(2) in each case is H, F, Cl, alkyl, alkoxy, CF3, CmF2m+1-CH2-, benzyl or phenoxy, and their pharmaceutically tolerable salts. The compounds according to the invention have very good antiarrhythmic properties, such as they show, for example, in the case of oxygen deficiency symptoms. The compounds are used as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they preventively inhibit or strongly decrease the pathophysiological processes during the formation of ischaemically induced damage, in particular during the induction of ischaemically induced cardiac arrhythmias.

公开(公告)号：PH30954A

公开(公告)日：1997-12-23

申请号：PH43726

申请日：1992-01-02

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT DR ,  ENGLERT HEINRICH DR ,  KLEEMANN HEINZ-WERNER DR ,  GERHARDS HERMANN DR ,  SCHOLKENS BERNWARD PROF DR ,  BECKER REINHARD DR ,  LINZ WOLFGANG DR ,  JEAN-PAUL VEVERT ,  JOHN-CLAUDE CAILLE

IPC: A61K31/415 ,  A61K31/425 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/40 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/64 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D207/34 ,  C07D207/36 ,  C07D233/54 ,  C07D233/66 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D233/90 ,  C07D249/02 ,  C07D255/02 ,  C07D257/02 ,  C07D257/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D453/02 ,  C07D521/00 ,  A61K31/41

Abstract: Azole derivative of the general formula (I) in which A, L, O, R , X, Y, Z and q have the meanings given, a process for their preparation, pharmaceutical preparations and the use of the compounds are described. Azole derivatives of the formula I where the symbols have, for example, the following meanings: R = (C2-C10)-alkyl Z = nitrogen X and Y = independently of one another CR L = -CH2- q = zero or 1 A = biphenyl radical which is substituted, for example, by R R = halogen or hydrogen R = SO2-NH-CO-OR and R = phenyl, are highly active antagonists of angiotensin II receptors.