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US 5,395,828 AGranted
Inositol phosphate analogues as calcium-antagonistic substances
AssigneeHoechst Aktiengesellschaft
InventorsWerner Schiebler, Elke Deckert, Erik Dreef, Gijs V. D. Marel, Jacques V. Boom
Life of this patent
Estimating the term…
Abstract
A compound of the formula (I) ##STR1## in which R.sub.1 is e.g. phosphate, R.sub.2 is e.g. phosphate or OH, and R.sub.4 is e.g. ##STR2## are suitable Calcium antagonists and useful e.g. for the treatment of cardio-vascular diseases.
Claims6
A compound of the formula (I) ##STR18## in which R.sup.1 is
- 1) phosphate
- 2) 1,2 diacyl-sn-glycer-3-yl phosphate, wherein acyl is a fatty acid with 2 to 20 C-atoms and 0 to 4 C--C-double bonds, or
- 3) 1,2 dialkyl-sn-glycer-3-yl phosphate, wherein alkyl is a hydrocarbon having 2 to 20 carbon atoms and 0 to 4 C--C double bonds
- R.sup.2 is
- 1) OH, or
- 2) phosphate
- R.sup.3 is
- 1) phosphate, or
- 2) OH
- 3) a radical of formula (II) ##STR19## wherein a) Y=Z.dbd.O and X=(C.sub.1 -C.sub.8)-alkyl
- b) Y=Z.dbd.O and X=(C.sub.1 -C.sub.18)-aryl
- c) Y=S and Z=O and X=(C.sub.1 -C.sub.8)-alkyl
- d) Y=S and Z=O and X=(C.sub.6 -C.sub.18)-aryl
- e) Y=O and Z=X.dbd.(C.sub.1 -C.sub.8)-alkyl
- f) Y=O and Z=X.dbd.(C.sub.6 -C.sub.8)-aryl
- g) Y=S and Z=X.dbd.(C.sub.1 -C.sub.8)-alkyl
- h) Y=S and Z=X.dbd.(C.sub.6 -C.sub.18)-aryl
- i) Y=Z.dbd.O and X=CF.sub.2 H
- j) Y=O and Z=X.dbd.F
- k) Y=Z.dbd.O and X=O--(C.sub.1 -C.sub.8)-alkyl
- l) Y=Z.dbd.O and X=O--(C.sub.6 -C.sub.18)-aryl
- m) Y=S and Z=O and X=O--(C.sub.1 -C.sub.8)-alkyl
- n) Y=S and Z=O and X=O--(C.sub.6 -C.sub.18)-aryl
- o) Y=O and Z=X.dbd.O--(C.sub.1 -C.sub.8)-alkyl
- p) Y=O and Z=X.dbd.O--(C.sub.6 -C.sub.18)-aryl
- q) Y=S and Z=X.dbd.O--(C.sub.1 -C.sub.8)-alkyl
- r) Y=S and Z=X.dbd.O--(C.sub.6 -C.sub.18)-aryl
- 4) a radical of formula (III ) ##STR20## where a) X=OR where R is H, (C.sub.1 -C.sub.8) -alkyl, or (C.sub.6 -C.sub.18) -aryl
- b) X=(C.sub.1 -C.sub.8)-alkyl
- c) X=(C.sub.6 -C.sub.18)-aryl
- d) X=NH--(C.sub.1 -C.sub.8)-alkyl
- e) X=NH--(C.sub.6 -C.sub.18)-aryl
- 5) a radical of formula (IV) ##STR21## where a) X=OR where R is (C.sub.1 -C.sub.8)-alkyl or (C.sub.6 -C.sub.18)-aryl
- b) X=(C.sub.1 -C.sub.8)-alkyl
- c) X=(C.sub.6 -C.sub.18)-aryl
- d) X=NH--(C.sub.1 -C.sub.8)-alkyl
- e) X=NH--(C.sub.6 -C.sub.18)-aryl
- wherein when R.sup.2 is OH, R.sup.3 is not OH
- R.sup.4 is
- 1) a radical of formula (V) ##STR22## where a) Y=Z.dbd.O and X=(C.sub.1 -C.sub.8)-alkyl
- b) Y=Z.dbd.O and X=(C.sub.1 -C.sub.18)-aryl
- c) Y=S and Z=O and X=(C.sub.1 -C.sub.8)-alkyl
- d) Y=S and Z=O and X=(C.sub.6 -C.sub.18)-aryl
- e) Y=O and Z=X.dbd.(C.sub.1 -C.sub.8)-alkyl
- f) Y=O and Z=X.dbd.(C.sub.6 -C.sub.18)-aryl
- g) Y=S and Z=X.dbd.(C.sub.1 -C.sub.8)-alkyl
- h) Y=S and Z=X.dbd.(C.sub.1 -C.sub.18)-aryl
- i) Y=Z.dbd.O and X=CF.sub.2 H
- j) Y=O and Z=X.dbd.F
- k) Y=Z.dbd.O and X=O--(C.sub.1 -C.sub.8)-alkyl
- l) Y=Z.dbd.O and X=O--(C.sub.6 -C.sub.18)-aryl
- m) Y=S and Z=O and X=O--(C.sub.1 -C.sub.8)-alkyl
- n) Y=S and Z=O and X=O--(C.sub.6 -C.sub.18)-aryl
- o) Y=O and Z=X.dbd.O--(C.sub.1 -C.sub.8)-alkyl
- p) Y=O and Z=X.dbd.O--(C.sub.6 -C.sub.18)-aryl
- q) Y=S and Z=X.dbd.O--(C.sub.1 -C.sub.8)-alkyl
- r) Y=S and Z=X.dbd.O--(C.sub.6 -C.sub.18)-aryl
- 2) a radical of formula (VI) ##STR23## wherein a) X=OR where R is H, (C.sub.1 -C.sub.8)-alkyl, or (C.sub.6 -C.sub.18)-aryl
- b) X=(C.sub.1 -C.sub.8)-alkyl
- c) X=(C.sub.6 -C.sub.18)-aryl
- d) X=NH--(C.sub.1 -C.sub.8)-alkyl
- e) X=NH--(C.sub.6 -C.sub.18)-aryl
- 3) a radical of formula (VII) ##STR24## wherein a) X=OR where R is (C.sub.1 -C.sub.8)-alkyl or (C.sub.6 -C.sub.18)-aryl
- b) X=(C.sub.1 -C.sub.8)-alkyl
- c) X=(C.sub.6 -C.sub.18)-aryl
- d) X=NH--(C.sub.1 -C.sub.8)-alkyl
- e) X=NH--(C.sub.6 -C.sub.18)-aryl
- and the physiologically tolerated salts thereof.
65 more elements
Dependencies are inferred from the claim text.