公开(公告)号：JPH10287641A

公开(公告)日：1998-10-27

申请号：JP4365298

申请日：1998-02-25

Applicant: HOECHST AG

Inventor： BRENDEL JOACHIM ,  LANG HANS JOCHEN DR ,  GERLACH UWE DR

IPC: C07D239/24 ,  A61K31/18 ,  A61K31/335 ,  A61K31/38 ,  A61K31/39 ,  A61K31/495 ,  A61P1/00 ,  A61P9/00 ,  C07C311/07 ,  C07D239/70 ,  C07D313/08 ,  C07D321/02 ,  C07D321/06

Abstract: PROBLEM TO BE SOLVED: To provide a new pharmaceutically active compound giving influence to a potassium channel and IKS channel opening by cyclic adenosine monophosphate and useful for the prevention and treatment of cardiovascular diseases and the treatment of the ulcer of gastrointestinal region, etc. SOLUTION: This compound is expressed by formula I X1 is O, S or CR(1)R(2) [R(1) and R(2) are each H, CF3 , etc.]; X2 is CR(1)R(2), etc.; X3 is CR(1)R(2), etc.; X4 is CR(1)R(2) or NR(6) [R(6) is same as X1]; Y1 to Y4 are each CR(12) [R(12) is H, F, etc.] or N; R(3) is phenyl, etc.; R(4) is Cr H2r -R(20) [the CH2 groups of Cr H2r may be substituted with O, S, etc.; (r) is 0-20; R(20) is H, methyl, etc.]; R(5) is H, etc.}, e.g. 3-fluoro-5-(N-ethylsulfonylamino)-6,7,8,9- tetrahydro-5H-benzocycloheptene. The compound of the formula I can be produced by reacting a compound of formula II with a compound of formula III (M is H, Li, etc.).

公开(公告)号：JPH10231293A

公开(公告)日：1998-09-02

申请号：JP3711698

申请日：1998-02-19

Applicant: HOECHST AG

Inventor： LANG HANS JOCHEN DR ,  BRENDEL JOACHIM ,  GERLACH UWE DR ,  WEIDMANN KLAUS DR

IPC: C07D311/60 ,  A61K31/35 ,  A61K31/352 ,  A61P1/00 ,  A61P9/00 ,  C07D311/68 ,  C07D311/70

Abstract: PROBLEM TO BE SOLVED: To obtain the subject new compound consisting of a specific sulfonamide-substituted chromane, exhibiting K channel blocking and gastric- acid secretion inhibiting effects, and useful for, e.g. prevention or treatment of gastric ulcer, enterelcosis, esophagitis regurgitica, diarrhea, allorhythmia and ventricular fibrillation. SOLUTION: This compound is a new chromane derivative shown by formula I R(1) and R(2) are each H, CF3 , C2 F5 , a 1-6C alkyl, (substituted)phenyl or the like; R(A) is O, H, a 1-6C alkanoyloxyl or the like; R(B) is H, forms a bond together with R(A) or the like; R(3) is shown by formula II (R(9) is H or a 3-8C cycloalkyl; (n) is 0 to 10; (m) is 0 or 1; R(11) is H, a 1-6C alkyl or the like; R(4) is an R(12)-Cr H2r [R(12) is H, a 3-8C cycloalkyl, piperidyl, 1- pyrrolidyl or the like]; R(5) to R(8) are each H, a halogen, a 1-6C alkyl, a 3-8C cycloalkyl, CN, CF3 , N3 or the like}, and useful, e.g. as a K channel blocking agent, gastric-acid secretion inhibitor, and for treatment of duodenal ulcer, esophagitis regurgitica, diarrhea, for prevention of treatment of allorhythmia and for prevention of ventricular fibrillation.

公开(公告)号：JPH10218855A

公开(公告)日：1998-08-18

申请号：JP2863598

申请日：1998-02-10

Applicant: HOECHST AG

Inventor： GERLACH UWE DR ,  BRENDEL JOACHIM ,  LANG HANS JOCHEN DR ,  WEIDMANN KLAUS DR

IPC: C07D335/02 ,  A61K31/015 ,  A61K31/18 ,  A61K31/215 ,  A61K31/38 ,  A61K31/382 ,  A61K31/435 ,  A61K31/47 ,  A61P9/00 ,  C07C13/20 ,  C07C311/07 ,  C07C403/04 ,  C07D211/72 ,  C07D215/42 ,  C07D335/06

Abstract: PROBLEM TO BE SOLVED: To obtain the subject new compound useful for treating gastrointestinal ulcer such as duodenal ulcer and treating/preventing arrhythmia through its potent and specific blocking effect on K channel different from K (ATP) channel. SOLUTION: This new compound is expressed by formula I X is S(O)q ((q) is 0-2), etc.; R(1) and R(2) are each H, CF3 , etc.; R(3) is R(12)-Ca H2a [NR(13)]m ; R(12) is H, a 3-8C cycloalkyl, etc.; (a) is 0-10; (m) is 0 or 1; R(13) is H, etc.; R(4) is R(14)-Cr H2r ; (r) is 1-20; R(14) is H, etc.; R(5) and R(6) are each CR(15)=CR(16)-CR(17)-CR(18), etc.; R(15) to R(18) are each H, F, etc.; R(7) is H, etc.; R(8) is H, etc.}, e.g. N-methyl-N-(7-nitro-1,2,3,4- tetrahydronaphthalen-1-yl)-methanesulfonamide. There are various synthetic methods for this compound; one of them being as follows: a compound of formula II (L is a nucleofugic eliminable group) is reacted with a compound of formula III (M is Li, K, etc.) in the presence of a base such as NaOH in a polar organic solvent at -10 to 140 deg.C.

公开(公告)号：JPH1067772A

公开(公告)日：1998-03-10

申请号：JP13798497

申请日：1997-05-14

Applicant: HOECHST AG

Inventor： LANG HANS JOCHEN DR ,  GERLACH UWE DR ,  BRENDEL JOACHIM DR ,  ENGLERT HEINRICH CHRISTIAN DR ,  GOEGELEIN HEINZ DR ,  HROPOT MAX DR ,  BOHN HELMUT DR ,  HERLING ANDREAS DR ,  BUSCH ANDREAS PROF DR ,  GREGER RAINER PROF DR

IPC: A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61K31/44 ,  A61K31/443 ,  A61P1/00 ,  A61P1/04 ,  A61P9/00 ,  A61P9/06 ,  C07D311/68 ,  C07D311/70 ,  C07D311/72 ,  C07D311/96 ,  C07D405/12

Abstract: PROBLEM TO BE SOLVED: To obtain the subject new compound opened by cyclic adenosine- phosphoric acid (CAMP), exhibiting strong and specific blocking action in K channel different from K (ATP) channel and useful as an agent, etc., for treating tumor of stomach and intestinal canal. SOLUTION: This chroman is represented by formula I R(1) or R(2) are each independently H, a 1-6C alkyl, etc.; R(3) is a group of R(9)-Cn H2n [NR(11)] [R(9) is H or a 3-8C cycloalkyl; (n) is an integer of 0-10; R(11) and R(9) together form a 1-8C alkylene]; R(4) is a group of R(12)-Cr H2r [R(12) is H, a 3-8C cycloalkyl, etc.; (r) is an integer of 1-20]; R(5) to R(8) are each independently H, F, Cl, Br, I, a 1-4C alkyl, etc.} or its physiologically permissible salt, e.g. a compound of formula II. The compound of the formula is obtained by alkylation, etc., of sulfonamide by a chroman derivative having alkylation action.

公开(公告)号：HU226462B1

公开(公告)日：2008-12-29

申请号：HU9503877

申请日：1995-12-28

Applicant: HOECHST AG

Inventor： KAISER JOACHIM DR ,  ENGLERT HEINRICH DR ,  GOEGELEIN HEINZ DR ,  MANRIA DIETER DR ,  GERLACH UWE DR

IPC: A61K31/18 ,  C07C311/51 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  C07C233/00 ,  C07C303/36 ,  C07C303/40 ,  C07C311/57 ,  C07C311/58 ,  C07C311/59 ,  C07C327/40 ,  C07C335/00 ,  C07C335/42

Abstract: Substd. benzene sulphonyl urea and thiourea cpds. of formula (I) and their salts are new. R1 = H, 1-7C alkyl or 3-7C cycloalkyl; R2 = H, 1-6C alkyl, 1-6C alkoxy, 1-6C mercaptoalkyl, 3-6C cycloalkyl, or 1-8C chain (in which 1-4C atoms are replaced by Het), F or Cl; R3, R4 = H, 1-12C alkyl, 3-10C cycloalkyl, 1-6C fluoroalkyl, 3-6C fluorocycloalkyl, or 1-10C chain in which 1-4C atoms are replaced by Het; or R3+R4 = (CH2)p, opt. with 1 or more CH2 replaced by heteroatoms; p = 2-8; Q, X = O or S; Y = (CR5R6)m; R5; R6 = H, Me or Et (opt. different in different CR5R6 gps.); Het = heteroatom such as O, N or S, m = 1-4.

公开(公告)号：HU226108B1

公开(公告)日：2008-04-28

申请号：HU9701984

申请日：1997-11-12

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH CHRISTIAN DR ,  GERLACH UWE DR ,  GOEGELEIN HEINZ DR ,  KLAUS ERIK DR ,  LINZ WOLFGANG DR ,  MANIA DIETER DR

IPC: C07D311/04 ,  C07D311/58 ,  A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61K31/355 ,  A61K31/40 ,  A61K31/4025 ,  A61P9/00 ,  A61P9/06 ,  C07D207/26 ,  C07D209/34 ,  C07D211/76 ,  C07D217/24 ,  C07D227/02 ,  C07D311/16 ,  C07D311/18 ,  C07D311/42 ,  C07D311/70 ,  C07D405/12

Abstract: 3-Amido-chromanylsulphonyl-urea or -thiourea derivatives of formula (I), in all stereoisomer (or mixture) forms, and their salts are new. R1 = H, alkyl, alkoxy, alkoxyalkoxy, alkylthio, F, Cl, Br, I or CF3; R2 = H, Me or Et; R3 = H or alkyl; Z = O or S; A = phenyl (optionally substituted by 1-3 halo, Me, Et, OMe or OEt), lactam residue of formula (i), 1-oxo-1,2,3,4-tetrahydroisoquinolin-2-yl, 1-oxo-perhydroisoquinolin-2-yl, 1-oxo-2,3-isoindolin-2-yl or 1-oxo-perhydroisoindolin-2-yl; B = 3-6C alkylene or 3-6C alkenylene (both optionally substituted by 1-3 alkyl); all alkyl moieties have 1-4C.

公开(公告)号：CY2220B1

公开(公告)日：2003-04-18

申请号：CY0100006

申请日：2001-05-03

Applicant: HOECHST AG

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

IPC: A61K31/18 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  C07C233/00 ,  C07C303/40 ,  C07C311/58 ,  C07C311/59 ,  C07C327/40 ,  C07C335/42

Abstract: Substd. benzene sulphonyl urea and thiourea derivs. of formula (I) and their salts are new. R1 = H, Me or CF3; R2 = 4-10C alkoxy with 1-6C replaced by O, S or NH; Q = O or S; Y = ÄC(R3)2Üm; R3 = H, Me or Et; R' = H, halo or 1-6C alkyl; R" = halo, 1-4C alkoxy or 1-4C alkyl; and m = 1-4.

公开(公告)号：CZ291271B6

公开(公告)日：2003-01-15

申请号：CZ43696

申请日：1996-02-14

Applicant: HOECHST AG

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

IPC: A61K31/18 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  C07C233/00 ,  C07C303/40 ,  C07C311/58 ,  C07C311/59 ,  C07C327/40 ,  C07C335/42

Abstract: In the present invention there are disclosed benzenesulfonyl ureas and thioureas of the general formula I, in which R(1) represents hydrogen, methyl or trifluoromethyl, R(2) denotes alkoxy having 4 to 10 carbon atoms, where 1 to 6 carbon atoms are replaced by oxygen, sulfur or NH hetero atoms, E represents oxygen or sulfur, Y denotes -[CR(3)i2 ]i(1-4), R(3) represents hydrogen or alkyl having 1 or 2 carbon atoms, X denotes hydrogen, halogen or alkyl having 1 to 6 carbon atoms, Z represents a nitro group, a halogen, an alkoxy group having 1 to 4 carbon atoms or an alkyl group having 1 to 4 carbon atoms, as well as their pharmaceutically acceptable salts. These compounds exhibit effects on the cardiovascular system. In the invention there is further described a process for preparing these compounds as well as a medicament in which they are comprised.

公开(公告)号：GR3034886T3

公开(公告)日：2001-02-28

申请号：GR20000402575

申请日：2000-11-22

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH DR ,  GERLACH UWE DR ,  CRAUSE PETER DR ,  MANIA DIETER DR ,  GOEGELEIN HEINZ DR ,  KAISER JOACHIM 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：DK0661264T3

公开(公告)日：2000-10-23

申请号：DK94120773

申请日：1994-12-27

Applicant: HOECHST AG

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