Abstract: The object of the invention are novel halogen substituted methylenebisphosphonic acid anhydrides, ester anhydrides, amide anhydrides, and ester amide anhydrides, processes for the preparation of these novel compounds, as well as pharmaceutical preparations comprising these novel compounds.

Abstract: The present invention is directed to an ophthalmic composition in the form of a topical aqueous solution consisting essentially ofan ophthalmologically active agent containing basic groups,an ion sensitive, hydrophilic polymer containing acidic groups in an amount of 0.004 to 1.5% by weight,at least one salt selected from the group of inorganic salts and buffers in a total amount of from 0.01 to 2.0% by weight,and optionally a wetting agent and a preservative, the ratio between salt and polymer being such that the solution exhibits a viscosity of less than 1000 mpas, and the pH of the solution is 4.0 to 8.0. The composition contains a sufficient amount of polymer to provide for a controlled absorption of the drug into the eye, its viscosity having been reduced to provide for better handling characteristics.

Abstract: The object of the invention is a process for preparing a clodronate preparation. The process is characterized in that clodronate is crystallized as disodium clodronate tetrahydrate from an aqueous solution of disodium clodronate; the resulting disodium clodronate tetrahydrate is dry granulated by compressing in such a way that the crystal structure of the disodium clodronate tetrahydrate is preserved and by crumbling and screening the mass to granules of a sutiable size, the dry granulated disodium clodronate tetrahydrate is optionally mixed with suitable excipients, such as filling agents and gliding agents and, if necessary, disintegrants.

Abstract: The invention relates to novel methylenebisphosphonic acid ester amide derivatives of general formula (I), in which formula W.sup.1, W.sup.2, W.sup.3 and W.sup.4 are independently the group OR.sup.1 or the group NR.sup.2 R.sup.3 wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen or straight or branched, optionally unsaturated C.sub.1 -C.sub.22 -alkyl, optionally substituted, optionally unsaturated C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl or silyl SiR.sub.3, or the groups R.sup.2 and R.sup.3 form together with the adjacent nitrogen atom a 3 to 10-membered saturated, partly saturated or aromatic heterocyclic ring, wherein in addition to the nitrogen atom, there may be one or two heteroatoms from the group N, O and S, provided that in formula (I) at least one of the groups W.sup.1, W.sup.2, W.sup.3 and W.sup.4 is hydroxy and at least one of the groups W.sup.1, W.sup.2, W.sup.3 and W.sup.4 is amino group NR.sup.2 R.sup.3, Q.sup.1 and Q.sup.

Abstract: Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently are straight or branched, optionally unsaturated C.sub.1 -C.sub.10 -alkyl, optionally unsaturated C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl, silyl SiR.sub.3 or hydrogen, whereby in formula (I) at least one of the groups R.sup.1, R.sup.2, R.sup.3 or R.sup.4 is hydrogen and at least one of the groups is different from hydrogen, Q.sup.1 is hydrogen, hydroxyl, halogen, amino NH.sub.2, or OR', wherein R' is C.sub.1 -C.sub.4 -lower alkyl or acyl, Q.sup.2 is straight or branched, optionally unsaturated C.sub.1 -C.sub.10 -alkyl, -hydroxyalkyl or -aminoalkyl, whereby the oxygen may, as a substituent, contain one group or the nitrogen as a substituent may contain one or two groups, which are C.sub.1 -C.sub.4 -lower alkyl or acyl, or the two substituents of the nitrogen form together with the nitrogen atom a saturated, partly saturated or an aromatic heterocyclic ring, or Q.sup.

Abstract: The object of the invention are bispilocarpates useful in the treatment of glaucoma and having the formula ##STR1## wherein A) Y is hydrogen or the acyl group ##STR2## and W is the group --O--A--O--Z--Y', wherein Y' is hydrogen or the acyl group ##STR3## the groups R and R' having different meanings and may be the same or different and A is an aliphatic, aromatic or heterocyclic bridging group, and --Z--Y' is ##STR4## or B) W is OR, wherein R has the same meaning as above, Y is ##STR5## where R' has the same meaning as above, B means the same as A and Z'--OR' is ##STR6## or C) W and Y together mean ##STR7## where the symbols have the same meanings as above.

Abstract: Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R.sup.1 -R.sup.4 independently are C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl, silyl SiR.sub.3 or hydrogen, whereby in formula (I) at least one of the groups R.sup.1 -R.sup.4 is hydrogen and at least one of the groups R.sup.1 -R.sup.4 is different from hydrogen, Q.sup.1 is hydrogen, hydroxyl, halogen, amino NH.sub.2, or OR'.sub.1, wherein R'.sub.1 is C.sub.1 -C.sub.4 -alkyl or acyl, Q.sup.2 is the group (.alpha.) wherein Y is a six-membered heterocyclic group, or a carbocyclic aromatic group, X is a bond, O, S or NR'", wherein R'" is hydrogen, lower alkyl, or acyl, n is the integer 0 to 6, and R' and R" are hydrogen or lower alkyl provided that as a ring atom of the ring Y and/or a chain atom of the group X, there is always at least one heteroatom from the group O, N and S, including the steroisomers and the salts of the compounds.

Abstract: Novel pharmaceutically active bisphosphonic acid derivatives of formula (I), in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently are C.sub.1 -C.sub.22 -alkyl, C.sub.2 -C.sub.22 -alkenyl, C.sub.2 -C.sub.22 -alkynyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.3 -C.sub.10 -cycloalkenyl, aryl, aralkyl, silyl and hydrogen, and R.sup.4 is different from hydrogen, Q.sup.1 is hydrogen, fluorine, chlorine, bromine or iodine, and Q.sup.2 is chlorine, bromine or iodine, including the stereoisomers, such as the geometrical isomers and optically active isomers, of the compounds, as well as the pharmaceutically acceptable salts of the compounds.