公开(公告)号：CZ9204033A3

公开(公告)日：1993-12-15

申请号：CS403392

申请日：1992-12-31

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 ,  C07C279/20 ,  A61K31/40 ,  C07C277/08

CPC classification number: C07D295/155 ,  C07C279/22 ,  C07D213/65

公开(公告)号：CZ403592A3

公开(公告)日：1993-12-15

申请号：CS403592

申请日：1992-12-31

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

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：DE4010488A1

公开(公告)日：1991-10-02

申请号：DE4010488

申请日：1990-03-31

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH-CHRISTIAN DR ,  MANIA DIETER DR ,  LINZ WOLFGANG DR

IPC: A61K31/535 ,  A61P9/00 ,  A61P9/06 ,  A61P9/12 ,  A61P11/08 ,  A61P17/00 ,  C07D265/20 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: Benzoxazine derivatives of the formula I where R(1) and R(2) equal H, OH, alkoxy, Hal or a multiplicity of other substituents, R(3) equals alkyl or alkanoyl; R(4) equals H, alkyl or alkanoyl, and R(5) equals pyrid(azin)yloxy, pyrimidinyloxy, pyridazinyloxy and other heterocycles and their salts are useful medicaments for the treatment of disorders of the cardiovascular system, asthma, smooth muscle disorders, high blood pressure, cardiac arrhythmias and circulatory disorders of the brain; they are also used for topical application to control hair loss.

公开(公告)号：DE3911549A1

公开(公告)日：1990-10-31

申请号：DE3911549

申请日：1989-04-08

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH CHRISTIAN DR ,  LANG HANS-JOCHEN DR ,  MANIA DIETER DR ,  MERKEL WULF DR ,  ELLORY CLIVE PROF

IPC: A61K31/245 ,  A61K31/18 ,  A61K31/357 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61P7/06 ,  C07C311/39 ,  C07C317/48 ,  C07C323/67 ,  C07D317/62 ,  C07D333/24 ,  C07D333/30

公开(公告)号：DE3827532A1

公开(公告)日：1990-03-01

申请号：DE3827532

申请日：1988-08-13

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH-CHRISTIAN DR ,  MANIA DIETER DR ,  UTZ ROLAND DR ,  SCHOELKENS BERNWARD DR

IPC: C07D311/68 ,  A61K31/40 ,  A61K31/443 ,  A61K31/445 ,  A61K31/455 ,  A61K31/495 ,  A61P1/00 ,  A61P7/10 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/08 ,  A61P25/00 ,  A61P25/08 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04

公开(公告)号：DE3811017A1

公开(公告)日：1989-10-19

申请号：DE3811017

申请日：1988-03-31

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH CHRISTIAN DR ,  MANIA DIETER DR ,  SCHOELKENS BERNWARD DR ,  UTZ ROLAND DR

IPC: C07D405/00 ,  A61K31/40 ,  A61K31/44 ,  A61K31/443 ,  A61K31/455 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P21/02 ,  A61P25/04 ,  C07C277/00 ,  C07C279/28 ,  C07C317/42 ,  C07C323/35 ,  C07C323/65 ,  C07D217/24 ,  C07D295/18 ,  C07D405/04

Abstract: Compounds I I where R1 is H, alkyl, alkoxy, CO alkyl, COOH, carboxyalkyl, CONR2, CN, NO2, alkylsulfi(o)nyl, arylsulfi(i)-nyl; R2 is H, OH, alkoxy, alkyl or alkylcarbonyl, R3/R4 are alkyl, m is zero or one and X is -CR6=CR7-(-CR8=CR9) (R6 R9 are H or alkyl), where n is zero or 1, are described. They are active antihypertensives and spasmolytics for the bladder, intestine, gall bladder, uterus, trachea and ureter.

公开(公告)号：DE3366181D1

公开(公告)日：1986-10-23

申请号：DE3366181

申请日：1983-03-02

Applicant: HOECHST AG

Inventor： ENGLERT HEINRICH CHRISTIAN DR ,  MANIA DIETER DR ,  MUSCHAWECK ROMAN DR ,  HROPOT MAX DR

IPC: A61K31/18 ,  A61K31/40 ,  A61P3/00 ,  A61P7/10 ,  A61P9/12 ,  C07C67/00 ,  C07C301/00 ,  C07C303/02 ,  C07C303/38 ,  C07C303/40 ,  C07C311/15 ,  C07C311/37 ,  C07D295/22 ,  C07D295/26 ,  C07C143/78

Abstract: The invention relates to 2-aminomethylphenols of the formula I in which R1 and R2 represent hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or benzyl which is optionally substituted by alkyl, alkoxy or halogen, R3 and R5 denote hydrogen, halogen, alkyl or alkoxy, R4 denotes halogen, alkyl or cycloalkyl and R6 and R7 represent hydrogen or alkyl, it being possible for the radicals R1 and R2, R6 R7 and/or two of the radicals R3, R4 and R5 to form an alkylene chain which is optionally substituted by methyl groups and which, in the case of the radicals R1, R2, R6 and R7, can also be interrupted by oxygen atoms, sulfur atoms and/or imino groups, and to physiologically acceptable salts thereof, a process for their preparation, and their use and to pharmaceutical formulations based on these compounds.

公开(公告)号：CH639371A5

公开(公告)日：1983-11-15

申请号：CH593882

申请日：1982-10-08

Applicant: HOECHST AG

Inventor： MERKEL WULF DR ,  BORMANN DIETER DR ,  MANIA DIETER DR ,  MUSCHAWECK ROMAN DR

IPC: C07D207/32 ,  C07D207/327 ,  C07D295/155 ,  C07D317/64 ,  A61K31/40

公开(公告)号：CH637379A5

公开(公告)日：1983-07-29

申请号：CH109978

申请日：1978-02-01

Applicant: HOECHST AG

Inventor： MERKEL WULF DR ,  BORMANN DIETER DR ,  MANIA DIETER DR ,  MUSCHAWECK ROMAN DR

IPC: C07D207/32 ,  C07D207/327 ,  C07D295/155 ,  C07D317/64

公开(公告)号：CH621776A5

公开(公告)日：1981-02-27

申请号：CH1059479

申请日：1979-11-28

Applicant: HOECHST AG

Inventor： BORMANN DIETER DR ,  MERKEL WULF DR ,  MUSCHAWECK ROMAN DR ,  MANIA DIETER DR

IPC: C07D207/00 ,  A61K31/395 ,  A61K31/40 ,  A61K31/445 ,  C07D207/06 ,  C07D207/10 ,  C07D207/20 ,  C07D207/32 ,  C07D207/327 ,  C07D207/40 ,  C07D207/404 ,  C07D207/44 ,  C07D207/452 ,  C07D209/14 ,  C07D209/44 ,  C07D209/48 ,  C07D209/52 ,  C07D211/14 ,  C07D211/30 ,  C07D211/34 ,  C07D211/88 ,  C07D265/32 ,  C07D265/33 ,  C07D295/00 ,  C07D295/155 ,  C07D295/18 ,  C07D207/04 ,  C07D207/18 ,  C07D211/06 ,  C07D227/00

Abstract: Novel heterocyclically substituted 5-sulphamoylbenzoic acid derivatives of the accompanying formula I, in which the symbols R , R , X and A have the meaning given in Patent Claim 1, are prepared by introducing the radical X into appropriate 3-nitro-5-sulphamoylbenzoic acids or their esters, which carry a halogen atom in the 4-position and whose 5-sulphamoyl group is protected, reducing the reaction product to the corresponding 3-amino compound, reacting this with dicarboxylic acid derivatives, reducing the 3-imido or 3-amido compounds thus obtained and hydrolysing the reaction product thus obtained to remove the protective group B and the ester group R . The alkyl radicals R can then be introduced by alkylation. Starting from the compounds of the formula I prepared according to the invention, in which X denotes a -SR group, the corresponding compounds in which X denotes a -SOR or -SO2R group are obtained by oxidation. The novel compounds are highly active saluretics and diuretics. They are used mainly for the treatment of oedematous diseases of various origins.