公开(公告)号：DE2944222A1

公开(公告)日：1981-05-14

申请号：DE2944222

申请日：1979-11-02

Applicant: BASF AG

Inventor： FRICKEL FRITZ-FRIEDER DIPL CHE ,  FRANKE ALBRECHT DIPL CHEM DR ,  HAGEN HELMUT DIPL ING DR ,  LENKE DIETER PROF DR ,  GRIES JOSEF DR MED

IPC: C07D275/04 ,  A61K31/425

Abstract: Novel amino-derivs. of 1,2-benzisothiazole are of formula (I). n is 2 or 3; R1 and R2 are H or opt. branched 1-5C alkyl; R3 is Ph, opt. mono-, di- or tri-substd. by halogen, alkyl, alkoxy, alkylthio, haloalkyl or haloalkoxy (these 2 gps. contg. 1-3 halogen), hydroxyalkyl or alkoxyalkyl (all alkyl gps. contg. 1-5C), 2-6C alkenyl, alkinyl or alkinyloxy, 3-8 ring C cycloalkoxy, methylene dioxy, amino, 1-5C alkylamino or di(1-5C)alkylamino. R3 may also be indanyl or tetrabydropaphthyl). The physiologically acceptable acid addn.-salts of (I) are also new. (I) are pharmaceuticals and can be used in heart and circulatory disorders. As a result of their beta-sympatholytic action, (I) are esp. suitable for the treatment of coronary heart disease, hypertonia and disturbances of cardiac rhythm. Suitable unit doese for humans are 1-100 (sp. 3-50) mg. (I) are strong beta-sympatholytics of low toxicity and have a therapeutic breadth 3-12 times greater than that of the known beta-sympatholitic propandol.

公开(公告)号：DE2704794A1

公开(公告)日：1978-08-17

申请号：DE2704794

申请日：1977-02-05

Applicant: BASF AG

Inventor： FRICKEL FRITZ-FRIEDER DIPL CHE ,  HAGEN HELMUT DIPL ING DR ,  OHNSORGE ULRICH DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  LENKE DIETER PROF DR ,  GRIES JOSEF DR MED ,  LEHMANN HANS DIETER DR MED

IPC: A61K31/428 ,  C07D275/04 ,  A61K31/425

Abstract: New aminopropanol derivatives of 4-hydroxy-1,2-benzisothiazole and their addition salts with acids, their preparation, and pharmaceutical formulations which contain the said compounds and may be used for the treatment and prophylaxis of cardiac and circulatory disorders.

公开(公告)号：DE3531504A1

公开(公告)日：1987-03-12

申请号：DE3531504

申请日：1985-09-04

Applicant: BASF AG

Inventor： GEISS KARL-HEINZ DR ,  HIMMELE WALTER DR ,  DEGNER DIETER DR ,  SIEGEL HARDO DR ,  GRIES JOSEF DR MED ,  LENKE DIETER PROF DR

IPC: A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/41 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61P1/04 ,  A61P43/00 ,  C07D207/32 ,  C07D207/335 ,  C07D209/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D409/06 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D513/04

公开(公告)号：DE3302442A1

公开(公告)日：1984-07-26

申请号：DE3302442

申请日：1983-01-26

Applicant: BASF AG

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

IPC: A61K31/50 ,  A61P1/04 ,  A61P7/02 ,  A61P9/12 ,  C07D237/14

公开(公告)号：DE3033702A1

公开(公告)日：1982-04-22

申请号：DE3033702

申请日：1980-09-08

Applicant: BASF AG

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

IPC: C07D237/04 ,  A61K31/50

Abstract: -pyridazinone derivs. (I) are new. X is O or S; R1 is H or 1-3C alkyl; and R2 is 1-8C alkyl (opt. substd. by 1-4 halogen atoms, 1-4C alkoxy (sepd. from X by at least 2 C-atoms), 3-8C cycloalkyl (opt. carrying 1 or 2 1-3C alkyl gps.) or phenyl (opt. in turn carrying 1-3 substits. from 1-3C alkyl, 1-3C alkoxy, halogen, CF3 or NO2), 3-8C cycloalkyl (opt. mono- to tetra substd. by 1-4C alkyl), 3-8C alkenyl, 3-8C alkynyl or phenyl (opt. carrying 1-3 substits. from 1-4C alkyl, 1-4C alkoxy, halogen, CF3, CN and NO2). (I) have thrombocyte aggregation inhibiting and hypotensive properties. They can be used as antihypertensive agents and for the prophylaxis and treatment of thrombo-embolid diseases. Results of tests for pharmacological activity are given in the spec.

公开(公告)号：DE3006351A1

公开(公告)日：1981-09-17

申请号：DE3006351

申请日：1980-02-20

Applicant: BASF AG

Inventor： SCHLECKER RAINER DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  THIEME PETER C DIPL CHEM DR ,  FRICKEL FRITZ-FRIEDER DIPL CHE ,  LENKE DIETER PROF DR ,  GRIES JOSEF DR MED

IPC: C07D213/30 ,  C07D271/06 ,  C07D271/10 ,  C07D275/02 ,  C07D277/24 ,  C07D307/42 ,  C07D333/16 ,  C07F9/58 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/655 ,  C07F9/6553 ,  C07D271/02 ,  A61K31/34 ,  A61K31/38 ,  A61K31/42 ,  A61K31/425 ,  A61K31/44 ,  C07D213/24 ,  C07D283/00

Abstract: 2-((3-amimo-2-hydroxypropoxy)-styryl) derivs. of formula (I) and their physiologically acceptable salts are new. (where Het is 2-furyl, 2- or 3-thienyl, 2- or 4-pyridyl, 4-thiazolyl, 4-isothiazolyl, 5-(1,2,4-oxadiazolyl) or 5-(1,3,4-oxadiazolyl), all these gps. opt. substd. by 1-4C alkyl or Ph which is itself opt. mono or disubstd by 1-3C alkyl; R is H, 1-8C alkyl (opt. substd. by OH, 1-3C alkoxy or 1-3C alkyl or 3-8 ring C cycloalkyl), 3-8 ring C cycloalkyl, opt. mono or disubstd. on the ring with 1-3C alkyl). (I) are pharmaceuticals for the treatment of hypertonia, coronary heart disease or cardiac arhythm. (I) are beta-sympatholytics which can be used in doses 15-23 times smaller than doses necessary if a similar effect is to be achieved using propranolol. (I) are of low toxicity. LD50 are 6,800-121,000 times greater than the ED50. (I) therefore have a wider therapeutic index than propranol has (only 1,030). Suitable unit doses of (I) are 1-100 (pref. 3-50) mg for humans.

公开(公告)号：DE2943405A1

公开(公告)日：1981-05-07

申请号：DE2943405

申请日：1979-10-26

Applicant: BASF AG

Inventor： FRICKER FRITZ-FRIEDER DIPL CHE ,  THIEME PETER C DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  THEOBALD HANS DIPL CHEM DR ,  LENKE DIETER PROF DR ,  GRIES JOSEF DR MED

IPC: A61K31/42 ,  A61P9/00 ,  A61P9/12 ,  A61P25/02 ,  C07C43/12 ,  C07C45/61 ,  C07C45/64 ,  C07C45/70 ,  C07D261/08 ,  C07F9/653

Abstract: Novel aminopropanol derivatives of 5-(2-hydroxystyryl)-isoxazole and their addition salts with acids, their preparation, pharmaceutical formulations containing these compounds, and their use in the treatment of hypertonia, coronary heart disease and cardiac arrhythmias.

公开(公告)号：DE2835438A1

公开(公告)日：1980-03-06

申请号：DE2835438

申请日：1978-08-12

Applicant: BASF AG

Inventor： FRICKEL FRITZ-FRIEDER DIPL CHE ,  FRANKE ALBRECHT DIPL CHEM DR ,  KOENIG HORST DIPL CHEM DR ,  LENKE DIETER PROF DR ,  GRIES JOSEF DR MED

IPC: A61K31/40 ,  A61P9/00 ,  C07D207/32 ,  C07D207/333 ,  C07D405/12

Abstract: Alkylaminopropanol derivatives of 2-(o-hydroxyphenyl)-pyrrole of the formula (I) (I) where R is hydrogen or is alkyl of 1 to 8 carbon atoms which is unsubstituted or substituted by hydroxyl, alkoxy of 1 to 3 carbons atoms or cycloalkyl of 3 to 8 carbon atoms in the ring, or is alkenyl or alkynyl of 2 to 8 carbon atoms or is cycloalkyl or cycloalkenyl of 3 to 8 carbon atoms in the ring, the cycloalkyl rings being unsubstituted or monosubstituted or disubstituted by alkyl or 1 to 3 carbon atoms, and their physiologically acceptable acid addition salts, processes for their preparation, and pharmaceutical formulations which contain the said compounds and may be used in the treatment of cardiac and circulatory disorders.

公开(公告)号：DE2727481A1

公开(公告)日：1979-01-11

申请号：DE2727481

申请日：1977-06-18

Applicant: BASF AG

Inventor： LEBKUECHER ROLF ,  THYES MARCO DIPL CHEM DR ,  KOENIG HORST DIPL CHEM DR ,  LEHMANN HANS DIETER DR MED ,  GRIES JOSEF DR MED ,  LENKE DIETER PROF DR ,  KUNZE JOHANNES DR MED

IPC: C07D237/00 ,  A61K31/50 ,  A61P7/02 ,  A61P9/12 ,  C07D237/04

Abstract: 6-(p-Acylaminophenyl)-4,5-dihydropyridaz-3-ones of the formula I I where R1 is hydrogen or alkyl of 1 to 3 carbon atoms and R2, if R1 is hydrogen, is halogen-substituted alkyl of 3 to 6 carbon atoms or beta -haloethyl or, if R1 is alkyl of 1 to 3 carbon atoms, is halogen-substituted alkyl of 1 to 6 carbon atoms, their manufacture, and therapeutic agents which contain, as the active ingredient, a compound of the formula I, where R2 may also be halomethyl or alpha -haloethyl if R1 is hydrogen. These compounds may be used as anti-hypertensive agents and for the prophylaxis and therapy of thromboembolic disorders.

公开(公告)号：DE3542994A1

公开(公告)日：1987-06-11

申请号：DE3542994

申请日：1985-12-05

Applicant: BASF AG

Inventor： SEITZ WERNER DR ,  BALDINGER VERENA DR ,  GRIES JOSEF DR MED ,  LENKE DIETER PROF DR ,  RASCHACK MANFRED DR ,  RUEBSAMEN KLAUS DR

IPC: A61K31/135 ,  A61P1/04 ,  A61P9/00 ,  A61P9/12 ,  C07C223/02 ,  C07D317/58 ,  C07D319/18 ,  C07D325/00 ,  C07C95/08