公开(公告)号：DE3022176A1

公开(公告)日：1982-01-07

申请号：DE3022176

申请日：1980-06-13

Applicant: BASF AG

Inventor： THYES MARCO DIPL CHEM DR ,  KOENIG HORST DIPL CHEM DR ,  LENKE DIETER PROF DR ,  LEHMANN HANS DIETER DR ,  GRIES JOSEF DR

IPC: A61K31/50 ,  A61P7/02 ,  A61P9/12 ,  C07D237/04

Abstract: Novel 6-(p-acylaminophenyl)-4,5-dihydro-3(2H)-pyridazinones, whose acyl radical is derived from a cycloalkylcarboxylic acid, processes for their preparation, pharmaceutical formulations containing these compounds, and their use as drugs in thrombo-embolic disorders and as anti-hypertensives.

公开(公告)号：DE3011327A1

公开(公告)日：1981-10-01

申请号：DE3011327

申请日：1980-03-24

Applicant: BASF AG

Inventor： MAY HANS-JOACHIM DIPL CHEM DR ,  LENKE DIETER PROF DR ,  GRIES JOSEF DR ,  TESCHENDORF HANS-JUERGEN DR ,  WORSTMANN WOLFGANG DR

IPC: C07D409/06 ,  A61K31/33 ,  A61K31/415 ,  A61K31/465 ,  A61K31/47 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D233/54 ,  C07D233/64 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  C07D233/50 ,  C07D401/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  A61K31/435 ,  A61K31/42 ,  A61K31/425

Abstract: 1-Aroyl-2-phenylamino-2-imidazolines of the general formula where R1 and R2 are identical or different and each is chlorine, bromine, fluorine, methyl, ethyl, methoxy, trifluoromethyl or cyano, R3 has the meanings given for R1 and R2 or is hydrogen and Ar is an unsubstituted or substituted monocyclic or bicyclic heteroaromatic radical containing 1, 2 or 3 nitrogen and/or oxygen and/or sulfur atoms, their salts with physiologically tolerated acids, their preparation, and drugs containing these compounds. The compounds have, inter alia, a blood pressure-reducing action.

公开(公告)号：DE2914615A1

公开(公告)日：1980-10-30

申请号：DE2914615

申请日：1979-04-11

Applicant: BASF AG

Inventor： LENKE DIETER PROF DR ,  MUELLER CLAUS D DR MED ,  GEISS KARL-HEINZ DIPL CHEM DR ,  BLIESENER JENS-UWE DIPL CHEM D

IPC: C07D207/48 ,  C07D307/68 ,  C07D333/28 ,  C07D333/38 ,  C07D409/12 ,  A61K31/40 ,  C07D207/32

Abstract: Pyrrole derivs. of formula (I) and their therapeutically useful ammonium, alkali metal and acid addition salts are new: (R1 = satd., opt. substd. 1-8C aliphatic gp.; 2-8C unsatd. alkyl, 3-7C cycloalkyl, or 1-4C alkyl substd. by phenyl or 5-6 membered aromatic heterocycle with N, O or S atom (these rings are opt. substd. at least once); R2 = H; or R1 + R2 together complete a 4-6 membered satd. heterocycle; R3 = H or 1-5C alkyl; R4 and R5 = H or 1-5C alkyl; X is O, S, SO or NH; Ar = phenyl, opt. substd. 1-3 times). (I) are diuretics useful in treatment of oedema and hypertension. They are given orally at 0.1-100 mg/kg/day or intravenously at 0.05-10 mg/kg/day.

公开(公告)号：DE2734882A1

公开(公告)日：1979-02-22

申请号：DE2734882

申请日：1977-08-03

Applicant: BASF AG

Inventor： HAGEN HELMUT DIPL ING DR ,  LENKE DIETER PROF DR ,  PHILIPSBORN GERDA VON DR MED

IPC: A61K31/425 ,  A61K31/505 ,  C07D275/04 ,  C07D417/10

Abstract: 3-[4-(1,3-Diazacyclo-2-yl)]-1,2-benzisothiazoles, their addition salts with acids, their manufacture, and pharmaceutical formulations which contain these compounds as active ingredients and which may be used for the pharmacotherapy of cardiac arrhythmias.

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).

公开(公告)号：DE2528285A1

公开(公告)日：1977-01-20

申请号：DE2528285

申请日：1975-06-25

Applicant: BASF AG

Inventor： WEITZ HANS-MARTIN DIPL CHEM DR ,  FISCHER ROLF DIPL CHEM DR ,  LENKE DIETER PROF DR

IPC: C07D253/10 ,  C07D253/08

Abstract: 1,2,4-Dihydrotriazine-4-oxide-spiro-(3,1')-[oximino-(2')-cycloalkanes] are manufactured by reaction of oximinocycloalk-1-enes, substituted in the 1-position, with hydrazine. The products, especially the triazine derivative described in Example 1, possess antiphlogistic properties and are starting materials for the manufacture of dyes and pharmaceuticals.