Hoffmann-la Roche Inc.

Actelion Pharmaceuticals Ltd

Peter Loeliger

Michael J Klaus

Peter Mohr

Ekkehard Weiss

Milos Suchy

Albert Pfiffner

Ulrich Schwieter

Madhukar Subraya Chodnekar

Rene Zurfluh

Harald Weiser

Rene Zurflun

Difficulties in preparing a stable pharmaceutical composition containing 5-Isopropyl-pyridine-2-sulfonic acid 6-(2-hydroxy-ethoxy)-5(2-methoxy-phenoxy)2-(2-1H-tetrazol-5-yl-pyridin-4yl)-pyrimidin-4-ylamide in form of the water soluble disodium salt, a buffer and preferably a metal complex forming agent, have been encountered. It was unexpectedly found that these difficulties can be overcome by adjusting the pH of the solution with an acid to over and above 8,2, preferably to 9,0, but not higher than 10.

Aqueous pharmaceutical composition

Novel Styryl-tetrahydromaphthalene and indane derivatives useful for treating neoplasms and dermatoses.

Novel tetrahydronaphthalene and indane derivatives

The present invention is concerned with novel tetrahydronaphthalene and indane derivatives of the formula ##STR1## useful as for combatting dermatoses as well as neoplasmas.

Novel styryl-tetrahydronaphthalene and indane derivatives useful for treating neoplasms and dermatoses.

Novel styryl-tetrahydromaphthalene and indane derivatives useful for treating neoplasms and dermatoses.

Novel tetrahydronaphthalene & indane derivatives

Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--; R.sup.1 is the group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl; and R.sup.4 is hydrogen, hydroxy, amino, lower-alkyl amino, di-(lower alkyl)amino or lower alkyl; with at least one ring of the molecule being heterocyclic, as well as salts of such compounds are useful in rodenticidal compositions containing a bait to eliminate rodents.

Heterocyclic rodenticidal compounds, compositions containing the

Novel styryl-tetrahydromaphythalene and indane derivatives useful for treating neoplasms and dermatoses.

Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--, --O-- or --S--; R.sup.1 is a group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl and R.sup.4 is hydrogen, hydroxy, amino, lower alkylamino, di-(lower alkyl)amino or lower-alkyl; at least one ring of the molecule being heterocyclic, salts thereof, processes for their preparation, rodenticidal compositions containing these compounds as the active ingredient and methods of use of the rodenticidal compositions are disclosed.

Novel p-[2(4,4-dimethyl-6-heterophenyl)substituted phenyl derivatives and salts thereof which are useful for combatting neoplasms and dermatoses including oral and topical compositions containing said derivatives which are suitable for such uses.

Benzopyranyl and benzothiopyranyl compounds and uses

Heterocyclic compounds

Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--, --O--or --S--; R.sup.1 is a group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl and R.sup.4 is hydrogen, hydroxy, amino, lower alkylamino, di-(lower alkyl)amino or lower-alkyl; at least one ring of the molecule being heterocyclic, salts thereof, processes for their preparation, rodenticidal compositions containing these compounds as the active ingredient and methods of use of the rodenticidal compositions are disclosed.

Benzofuranyl (thienyl) propenyl derivatives useful as rodenticides

Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--, --O-- or --S--; R.sup.1 is a group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is a group--CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl and R.sup.4 is hydrogen, hydroxy, amino, lower alkylamino, di-(lower alkyl)amino or lower-alkyl; at least one ring of the molecule being heterocyclic, salts thereof, processes for their preparation, rodenticidal compositions containing these compounds as the active ingredient and methods of use of the rodenticidal compositions are disclosed.

4,5,6,7-Tetrahydro-4,4,7,7-tetramethylbenzo[b]thien-2-yl or furan-2-yl

This invention is directed to 5,6,7,8-tetrahydro-naphthyl or indanyl stilbene derivatives which are useful as tumor inhibiting agents, in the treatment of neoplasms, dermatological conditions and rheumatic illnesses.

Growing community of inventors

Muttenz, Switzerland

Peter Loeliger