公开(公告)号：DE3542197A1

公开(公告)日：1987-06-04

申请号：DE3542197

申请日：1985-11-29

Applicant: BASF AG

Inventor： MAY HANS-JOACHIM DR ,  TRAUT MARTIN DR ,  WEIFENBACH HARALD DR ,  BALDINGER VERENA DR ,  GRIES JOSEF DR MED ,  TESCHENDORF HANS-JUERGEN DR ME

IPC: A61K31/50 ,  A61P25/00 ,  A61P25/24 ,  A61P25/26 ,  C07D237/20

公开(公告)号：DE3532880A1

公开(公告)日：1987-03-26

申请号：DE3532880

申请日：1985-09-14

Applicant: BASF AG

Inventor： OSTERSEHLT BERND DR ,  RIEBER NORBERT DR ,  GRIES JOSEF DR MED

IPC: A61K31/415 ,  A61K31/505 ,  A61P1/04 ,  A61P43/00 ,  C07D231/12 ,  C07D317/00 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  C07D401/06 ,  A61K31/445 ,  C07D403/14 ,  C07D413/14 ,  A61K31/535

Abstract: 1,4-disubstituted pyrazole derivatives of the formula I I where R1 and R2 independently of one another are each hydrogen, lower alkyl or benzyl, or R1 and R2, together with the nitrogen atom to which they are bonded, may be a pyrrolidino, piperidino or morpholino radical, n is an integer from 2 to 5 and Z is a radical of the formula or QNR1R2 where R1 and R2 have the same meanings as above, Q is A is CHR3 or NR3 in which R3 is CN, NO2, SO2-aryl or SO2-lower alkyl and m may be 0 or 1, and their pharmaceutically tolerated salts, processes for their preparation, pharmaceutical compositions containing the compounds of formula I, the use of such compositions and an intermediate of the formula III III where R1, R2 and n have the same meanings as above, in the preparation of the compounds of the formula I. The compounds are useful to block histamine H2- receptors.

公开(公告)号：DE3243370A1

公开(公告)日：1984-05-24

申请号：DE3243370

申请日：1982-11-24

Applicant: BASF AG

Inventor： KUBINYI HUGO DR ,  TRAUT MARTIN DR ,  GRIES JOSEF DR MED

IPC: A61K31/16 ,  A61K31/21 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07C327/20 ,  C07D205/04 ,  C07D207/10 ,  C07D207/16 ,  C07D209/20 ,  C07D211/60 ,  C07D217/26 ,  C07D277/06 ,  C07K5/04 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/078 ,  C07K5/083 ,  C07K14/81 ,  C07C153/09 ,  C07C103/52 ,  A61K31/195 ,  A61K31/40

Abstract: Benzoylthio compounds of the formula I I CO(NR3CHR4CO)mOH where R1 and R3 are identical or different and are each hydrogen or C1-C4-alkyl, R2 and R4 are identical or different and are each hydrogen or C1-C6-alkyl which is unsubstituted or substituted by hydroxyl, mercapto, C1-C4-alkylthio, a carboxylic ester group, carboxamido or acylamino or are each an aryl, hetaryl, arylalkylene or hetarylalkylene radical which is unsubstituted or substituted in the aryl moiety by hydroxyl, C1-C4-alkoxy, arylalkoxy or halogen, R1 and R2 and/or R3 and R4 together may furthermore be a radical -(CH2)p- (p=2, 3, 4), -CH2-S-CH2- or -CH2-C6H4-CH2-(ortho), X is NH or sulfur, m and n are identical or different and are each 0 or 1, and q is 0 or 1 where X is S, and is 0 where X is NH, and their salts with physiologically tolerated bases, their preparation, drugs containing these compounds and the use of these drugs in treating disorders.

公开(公告)号：DE3209158A1

公开(公告)日：1983-09-15

申请号：DE3209158

申请日：1982-03-13

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  THYES MARCO DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  KOENIG HORST PROF DIPL CHEM DR ,  GRIES JOSEF DR MED ,  LEHMANN HANS DIETER DR MED ,  LENKE DIETER PROF DR

IPC: C07D237/04 ,  C07D237/14 ,  A61K31/50

Abstract: Compounds of the general formula in which R denotes a hydrogen atom or the methyl, ethyl or propyl radical and R , if R denotes a hydrogen atom, denotes an alkenyl radical having 3 to 8 C atoms, which is optionally substituted by 1 to 3 halogen atoms, excluding the 1-methylvinyl radical, or, if R denotes the methyl, ethyl or propyl group, denotes an alkenyl radical having 2 to 8 C atoms, which is optionally substituted by 1 to 3 halogen atoms, and therapeutic compositions which contain these compounds.

公开(公告)号：DE3135617A1

公开(公告)日：1983-03-17

申请号：DE3135617

申请日：1981-09-09

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  THYES MARCO DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  KOENIG HORST PROF DIPL CHEM DR ,  GRIES JOSEF DR MED ,  LEHMANN HANS-DIETER DR MED ,  LENKE DIETER PROF DR

IPC: C07D237/26 ,  A61K31/50

Abstract: The present invention relates to diazabicyclo[4.2.0]octenones of the formula I, in which Y has the meaning given in the description, to their preparation and to their use as medicaments in the treatment of high blood pressure and for the therapy of thromboembolic disorders.

公开(公告)号：DE3044566A1

公开(公告)日：1982-07-15

申请号：DE3044566

申请日：1980-11-26

Applicant: BASF AG

Inventor： FRICKEL FRITZ-FRIEDER DIPL CHE ,  OSTERSEHLT BERND DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  THYES MARCO DIPL CHEM DR ,  FRIEDRICH LUDWIG DR ,  GRIES JOSEF DR MED ,  LENKE DIETER PROF DR ,  WEIFENBACH HARALD DR

IPC: C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  A61K31/415

Abstract: N-substd. imidazole derivs. of formula (I) and their salts with physiologically acceptable acids are new. (R1,R2 and R3 are each H, 1-8C alkyl or opt. substd. aralkyl; Alk is 2-8C alkylene opt. substd. with 1-3C alkyl gps.; R4 is O,S, =NR6, =CHNO2, or =CHR7R8; R5 is 2-((4-methyl-5-imidazolyl) methyl-thio) ethylamino; R6 is H, NO2, CN, carboxamido, 1-4C alkyl, aryl or arylsulphonyl; R7 and R8 are each nitrile or carboalkoxy). 12 cpds. (I) are specifically claimed, including N-cyano- N'-(2-((5-methyl- 1H-imidazol-4-yl)- methylthio)-ethyl)-N"-(3-(2-methylimidazol-1-yl) propyl) guanidine. (I) are selective Histamine-H2- antagonists and can be used in the treatment of illnesses associated with increased stomach acid production, e.g. stomach and duodenal ulcers. Suitable daily doses are 0.5-20 mg/kg p.o. and 0.05-10.0 mg/kg i.v.

公开(公告)号：DE3026331A1

公开(公告)日：1982-02-18

申请号：DE3026331

申请日：1980-07-11

Applicant: BASF AG

Inventor： FRANKE ALBRECHT DIPL CHEM DR ,  LENKE DIETER PROF DR ,  GRIES JOSEF DR MED ,  WEIFENBACH HARALD DR ,  KREISKOTT HORST DR ,  HOFMANN HANS PETER DR

IPC: C07D295/08 ,  A61K31/495 ,  A61P9/12 ,  A61P25/20 ,  C07C45/70 ,  C07D295/092 ,  C07D303/22 ,  C07D295/04

公开(公告)号：DE3005287A1

公开(公告)日：1981-08-20

申请号：DE3005287

申请日：1980-02-13

Applicant: BASF AG

Inventor： THIEME PETER C DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  DENKE DIETER PROF DR ,  LEHMANN HANS DIETER DR MED ,  GRIES JOSEF DR MED

IPC: C07D413/12 ,  A61K31/495 ,  A61K31/496 ,  A61P9/12 ,  C07D271/10 ,  C07D405/12 ,  A61K31/41

Abstract: Novel phenylpiperazinylpropanols of 1,3,4-oxadiazolylphenols and their physiologically tolerated addition salts with acids, processes for their preparation, and pharmaceutical formulations which contain these compounds and are useful in the treatment of hypertonia.

公开(公告)号：DE2720613A1

公开(公告)日：1978-11-16

申请号：DE2720613

申请日：1977-05-07

Applicant: BASF AG

Inventor： FRICKEL FRITZ-FRIEDER DIPL CHE ,  LENKE DIETER PROF DR ,  GRIES JOSEF DR MED

IPC: C07D333/38 ,  A61K31/38

Abstract: 1-Amino-3-thienyloxy-2-propanol derivs. of formula (I) and their acid addn. salts are new. In (I), R1 = H, 1-6C alkyl, 7-10C aralkyl, phenyl, or phenyl mono-or poly-substd. by halogen, 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio, CF3, methylenedioxy, COOH, OH and/or amino; and R2 = H, 2-8C alkenyl, 2-8C alkynyl, 3-8C cycloalkyl, 1-8C alkyl, or 1-8C alkyl substd. by OH, 1-3C alkoxy or 1-3C alkylthio. (I) can be used in the treatment and prophylaxis of cardiovascular disorders, esp. coronary heart disease, heart rhythm disorders and hypertension. Specific cpds. (I) include 2-cyano-3-(2-hydroxy-3-tert.-butylaminopropoxy)thiophene. In an example, this is prepd. in 72% yield by reacting 18 g. 1-(2-cyano-3-thienyloxy)-2,3-epoxypropane with 40 ml. tert.-butylamine in 100 ml. ethanol at room temp. for 10 hrs. The prod. is isolated in the form of it shydrochloride.

公开(公告)号：DE2711382A1

公开(公告)日：1978-09-21

申请号：DE2711382

申请日：1977-03-16

Applicant: BASF AG

Inventor： FRICKEL FRITZ-FRIEDER DIPL CHE ,  LENKE DIETER PROF DR ,  GRIES JOSEF DR MED

IPC: C07D261/20 ,  C07D261/12 ,  A61K31/42

Abstract: Benzisoxazole derivs. of formula (I) and their pharmaceutically tolerable salts are new: (R1=1-8C alkyl(opt. substd. by OH, 1-3C alkoxy or alkylthio, di(1-5C)alkylamino or 5-7 ring-membered cyclic amino), 2-8C alkenyl or alkynyl, 3-8C cycloalkyl or cycloalkenyl, 5-8C bicycloalkyl, the cycloalkyl rings opt. being substd. by 1-3C alkyl). Pref. cpds. have R1 = 3-6C alkyl. They are prepd. e.g. by reacting H2NR1 with 3-methyl-4-(2,3-epoxypropoxy)-1,3-benzisoazole. (I) have beta-sympatholytic activity and are esp. useful for treating coronary heart disorders, cardiac arrythmia and hypertension. The cpds. with R1=tert. butyl has a separation between its negative inotropic activity and beta1-sympatholytic activity 100 times greater than propanolol (A), and its LD50 (intraperitoneal in rats) in 197 mg/kg compared with 108 mg/kg for (A).