公开(公告)号：JPH10279568A

公开(公告)日：1998-10-20

申请号：JP6266598

申请日：1998-03-13

Applicant: HOECHST AG

Inventor： FALK EUGEN ,  ENHSEN ALFONS ,  STENGELIN SIEGFRIED ,  GLOMBIK HEINER

IPC: C12N15/09 ,  A61K31/55 ,  A61K31/554 ,  A61K31/675 ,  A61K31/70 ,  A61K48/00 ,  A61P1/16 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P35/00 ,  C07D281/00 ,  C07D281/10 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07F9/6558 ,  C07H17/00 ,  C12N5/00 ,  C12N5/10 ,  C12N9/12 ,  C12N15/06 ,  C12N15/10 ,  C12N15/11 ,  C12N15/54 ,  C12N15/85 ,  C12P21/02 ,  C12R1/91

Abstract: PROBLEM TO BE SOLVED: To obtain a new compound capable of reducing the concentration of an (ultra) low density lipoprotein cholesterol in plasma or serum and useful for treating and preventing hyperlipemia such as atherosclerosis. SOLUTION: This compound is represented by formula I R and R are each a straight-chain 1-6C alkyl; R is H or OR [R is H or a (substituted) 1-6C alkyl]; R is pyridyl or a (substituted) phenyl; R , R and R are each H, a halogen, cyano, etc.; R is represented by formula II (R is COOH, CH2 OH, etc.), etc.; X is NH or O; R and R are each H or 1-6C alkyl}. The objective compound is prepared by acylating or alkylating a compound represented by formula III at the group X-H according to the standard method or glycosylating or glucuronidating the compound represented by formula III at the group X-H and then eliminating the protecting group, especially hydroxyl group and amino functional group.

公开(公告)号：WO9746226A3

公开(公告)日：1998-03-05

申请号：PCT/EP9702548

申请日：1997-05-20

Applicant: HOECHST AG ,  LANG HANS JOCHEN ,  JANSEN HANS WILLI ,  SCHWARK JAN ROBERT ,  KLEEMANN HEINZ WERNER ,  JUNG OLIVER ,  SCHAEFER HANS LUDWIG ,  LINZ WOLFGANG ,  KRAMER WERNER ,  SCHOELKENS BERNWARD ,  FALK EUGEN

Inventor： LANG HANS JOCHEN ,  JANSEN HANS-WILLI ,  SCHWARK JAN-ROBERT ,  KLEEMANN HEINZ-WERNER ,  JUNG OLIVER ,  SCHAEFER HANS-LUDWIG ,  LINZ WOLFGANG ,  KRAMER WERNER ,  SCHOELKENS BERNWARD ,  FALK EUGEN

IPC: A61K31/155 ,  A61K31/00 ,  A61K31/166 ,  A61K31/22 ,  A61K31/255 ,  A61K31/365 ,  A61K31/41 ,  A61K31/455 ,  A61K45/00 ,  A61K45/06 ,  A61P3/00 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00

CPC classification number: A61K31/166 ,  A61K31/00 ,  A61K31/155 ,  A61K31/22 ,  A61K31/365 ,  A61K31/165 ,  A61K2300/00

Abstract: The active substances identified as inhibitors of the cellular Na+/H+ exchanger (NHE) are used to prepare a medicament for normalizing serum lipids. They are used in the preparation of a medicament which reduces lipid levels in the blood and can be administered for treating diseases caused by lipid levels which are too high, and for alleviating the endothelial dysfunctional syndrome and for treating diseases caused thereby.

Abstract translation: 被鉴定为细胞Na + / H +交换剂（NHE）的抑制剂的活性物质用于制备用于使血清脂质正常化的药物。 它们用于制备降低血液中脂质水平并且可以用于治疗由过高的脂质水平引起的疾病以及用于缓解内皮功能障碍综合征和用于治疗由此引起的疾病的药物的药物。

公开(公告)号：NZ333095A

公开(公告)日：2000-08-25

申请号：NZ33309597

申请日：1997-05-20

Applicant: HOECHST AG

Inventor： LANG HANS JOCHEN ,  JANSEN HANS-WILLI ,  SCHWARK JAN-ROBERT ,  KLEEMANN HEINZ-WERNER ,  JUNG OLIVER ,  SCHAEFER HANS-LUDWIG ,  LINZ WOLFGANG ,  KRAMER WERNER ,  SCHOELKENS BERNWARD ,  FALK EUGEN

IPC: A61K31/155 ,  A61K31/00 ,  A61K31/166 ,  A61K31/22 ,  A61K31/255 ,  A61K31/365 ,  A61K31/41 ,  A61K31/455 ,  A61K45/00 ,  A61K45/06 ,  A61P3/00 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00

Abstract: Use of Na+/H+ exchange inhibitors benzoylguanidines of the formula 1 where: R(1) or R(2) is R(6)-S(O)n- or R(7)R(8)N-02S-; and the other substituent R(1) or R(2) in each case are H, F, Cl, Br, (C1-C4)-alkyl, (C1-C4)-alkoxy or phenoxy, is unsubstituted or substituted by 1 - 3 substituents selected from F, Cl, methyl and methoxy; or the other substituent R(1) or R(2) is: R(6)-S(O)n or R(7)R(8)N-; n is 0, 1 or 2; R(6) is (C1-C6)-alkyl, (C5-C7)-cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, which is unsubstituted or substituted by 1 - 3 substituents selected from F, Cl, methyl and methoxy R(7) and R(8) are H or (C1-C6)-alkyl; or R(7) is phenyl-(CH2)m; m is 1-4; or R(7) is phenyl, which is unsubstituted or substituted by 1 - 2 substituents selected from F, Cl, methyl and methoxy or R(7) and R(8) together are straight chain or branched (C4-C7) chain, where the chain can additionally be interrupted by O, S or NR9; R(9) is H, Methyl; or R(7) and R(8) together with the nitrogen atom to which they are bonded are a dihydroindole tetrahydroquinoline or tetrahydroisoquinoline system; R(3), R(4} and R(5) independently are H or C1-2 alkyl or R4 and R5 are C4-7 alkylene chain

公开(公告)号：DE19622222A1

公开(公告)日：1997-12-04

申请号：DE19622222

申请日：1996-06-03

Applicant: HOECHST AG

Inventor： LANG HANS JOCHEN ,  JANSEN HANS-WILLI ,  SCHWARK JAN-ROBERT ,  KLEEMANN HEINZ-WERNER ,  JUNG OLIVER ,  SCHAEFER HANS-LUDWIG ,  LINZ WOLFGANG ,  KRAMER WERNER ,  SCHOELKENS BERNWARD ,  FALK EUGEN

IPC: A61K31/155 ,  A61K31/00 ,  A61K31/166 ,  A61K31/22 ,  A61K31/255 ,  A61K31/365 ,  A61K31/41 ,  A61K31/455 ,  A61K45/00 ,  A61K45/06 ,  A61P3/00 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00

Abstract: Use of a Na /H exchange (NHE) inhibitor (I) for preparing a medicament for treating raised blood fat levels is new. Also claimed is the use of (I) for preparing medicaments for treating atherosclerosis, hypercholesterinic diseases of the coronary circulation system, endothelial dysfunction syndromes, cardiac hypertrophy and cardiomyopathy, coronary vessel spasm, myocardial infarction, thromboses, high blood pressure and peripheral vessel disease caused by atherosclerosis, raised blood lipid levels and endothelial dysfunction.

公开(公告)号：CA2231971C

公开(公告)日：2008-05-20

申请号：CA2231971

申请日：1998-03-12

Applicant: HOECHST AG

Inventor： ENHSEN ALFONS ,  FALK EUGEN ,  STENGELIN SIEGFRIED ,  GLOMBIK HEINER

IPC: C07H15/26 ,  C12N15/09 ,  A61K31/55 ,  A61K31/554 ,  A61K31/675 ,  A61K31/70 ,  A61K48/00 ,  A61P1/16 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P35/00 ,  C07D281/00 ,  C07D281/10 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07F9/6536 ,  C07F9/6558 ,  C07H17/00 ,  C12N5/00 ,  C12N5/10 ,  C12N9/12 ,  C12N15/06 ,  C12N15/10 ,  C12N15/11 ,  C12N15/54 ,  C12N15/85 ,  C12P21/02 ,  C12R1/91

Abstract: Hypolipidernic 1,4-benzothiazepine-1,1-dioxides The present invention is concerned with new hypolipidemic compounds, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis. Compounds of the formula (I): (I) wherein R1 to R10 and X are a defined.

公开(公告)号：PL189950B1

公开(公告)日：2005-10-31

申请号：PL33041297

申请日：1997-05-20

Applicant: HOECHST AG

Inventor： LANG HANS JOHEN ,  JANSEN HANS-WILLI ,  SCHWARK JAN-ROBERT ,  KLEEMANN HEINZ-WERNER ,  JUNG OLIVER ,  SCHAEFER HANS-LUDWIG ,  LINZ WOLFGANG ,  KRAMER WERNER ,  SCHOELKENS BERNWARD ,  FALK EUGEN

IPC: A61K31/155 ,  A61K31/00 ,  A61K31/166 ,  A61K31/22 ,  A61K31/255 ,  A61K31/365 ,  A61K31/41 ,  A61K31/455 ,  A61K45/00 ,  A61K45/06 ,  A61P3/00 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00

Abstract: The active substances identified as inhibitors of the cellular Na /H exchanger (NHE) are used to prepare a medicament for normalizing serum lipids. They are used in the preparation of a medicament which reduces lipid levels in the blood and can be administered for treating diseases caused by lipid levels which are too high, and for alleviating the endothelial dysfunctional syndrome and for treating diseases caused thereby.

公开(公告)号：HU9800541A2

公开(公告)日：1999-06-28

申请号：HU9800541

申请日：1998-03-12

Applicant: HOECHST AG

Inventor： ENHSEN ALFONS ,  FALK EUGEN ,  GLOMBIK HEINER ,  STENGELIN SIEGFRIED

IPC: A61K31/55 ,  A61K31/554 ,  A61K31/675 ,  A61K31/70 ,  A61K48/00 ,  C12N15/09 ,  A61P1/16 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P35/00 ,  C07D281/00 ,  C07D281/10 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07F9/6558 ,  C07H17/00 ,  C12N5/00 ,  C12N5/10 ,  C12N9/12 ,  C12N15/06 ,  C12N15/10 ,  C12N15/11 ,  C12N15/54 ,  C12N15/85 ,  C12P21/02 ,  C12R1/91

Abstract: The present invention is concerned with new hypolipidemic compounds (I) and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis. Compounds of the formula (I): wherein X is -NH- or -O-; and R is a group of the formula wherein the hydroxyl groups may be substituted by acetyl or benzyl, or -(C1-C6)-alkyl-R wherein the alkyl group may be substituted with one or more hydroxyl groups; R is -COOH or -CH2-OH; R is H, -OH, -NH2, -COOH or COOR ; R is (C1-C4)-alkyl or -NH-(C1-C4)-alkyl.

公开(公告)号：TR199802505T2

公开(公告)日：1999-04-21

申请号：TR9802505

申请日：1997-05-20

Applicant: HOECHST AG

Inventor： LANG JOCHEN HANS ,  JANSEN HANS-WILLI ,  SCHWARK JAN-ROBERT ,  KLEEMANN HEINZ-WERNER ,  JUNG OLIVER ,  FER HANS-LUDWIG SCH ,  LINZ WOLFGANG ,  KRAMER WERNER ,  SCHOELKENS BERNWARD ,  FALK EUGEN

IPC: A61K31/155 ,  A61K31/00 ,  A61K31/166 ,  A61K31/22 ,  A61K31/255 ,  A61K31/365 ,  A61K31/41 ,  A61K31/455 ,  A61K45/00 ,  A61K45/06 ,  A61P3/00 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00

Abstract: The active substances identified as inhibitors of the cellular Na /H exchanger (NHE) are used to prepare a medicament for normalizing serum lipids. They are used in the preparation of a medicament which reduces lipid levels in the blood and can be administered for treating diseases caused by lipid levels which are too high, and for alleviating the endothelial dysfunctional syndrome and for treating diseases caused thereby.

公开(公告)号：NO985480L

公开(公告)日：1999-01-28

申请号：NO985480

申请日：1998-11-24

Applicant: HOECHST AG

Inventor： LANG HANS JOCHEN ,  JANSEN HANS-WILLI ,  SCHWARK JAN-ROBERT ,  KLEEMANN HEINZ-WERNER ,  JUNG OLIVER ,  SCHOFER HANS-LUDWIG ,  LINZ WOLFGANG ,  KRAMER WERNER ,  SCH LKENS BERNWARD ,  FALK EUGEN

IPC: A61K31/155 ,  A61K31/00 ,  A61K31/166 ,  A61K31/22 ,  A61K31/255 ,  A61K31/365 ,  A61K31/41 ,  A61K31/455 ,  A61K45/00 ,  A61K45/06 ,  A61P3/00 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00

Abstract: The active substances identified as inhibitors of the cellular Na /H exchanger (NHE) are used to prepare a medicament for normalizing serum lipids. They are used in the preparation of a medicament which reduces lipid levels in the blood and can be administered for treating diseases caused by lipid levels which are too high, and for alleviating the endothelial dysfunctional syndrome and for treating diseases caused thereby.

公开(公告)号：ZA974828B

公开(公告)日：1997-12-03

申请号：ZA974828

申请日：1997-06-02

Applicant: HOECHST AG

Inventor： LANG HANS JOCHEN ,  JANSEN HANS-WILLI ,  SCHWARK JAN-ROBERT ,  KLEEMANN HEINZ-WERNER ,  JUNG OLIVER ,  SCHAEFER HANS-LUDWIG ,  LINZ WOLFGANG ,  KRAMER WERNER ,  SCHOELKENS BERNWARD ,  FALK EUGEN

IPC: A61K31/155 ,  A61K31/00 ,  A61K31/166 ,  A61K31/22 ,  A61K31/255 ,  A61K31/365 ,  A61K31/41 ,  A61K31/455 ,  A61K45/00 ,  A61K45/06 ,  A61P3/00 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  A61K

Abstract: The active substances identified as inhibitors of the cellular Na /H exchanger (NHE) are used to prepare a medicament for normalizing serum lipids. They are used in the preparation of a medicament which reduces lipid levels in the blood and can be administered for treating diseases caused by lipid levels which are too high, and for alleviating the endothelial dysfunctional syndrome and for treating diseases caused thereby.