Abstract: This invention provides novel Sn compounds, i.e. di-n.butyltindihydroxybenzoates, which exhibit excellent activities against varies tumors. This invention also provides pharmaceutical compositions which contain said novel Sn compounds in combination with a suitable carrier, in particular aqueous solutions which are suitable for injection.
Type:
Grant
Filed:
April 12, 1995
Date of Patent:
December 10, 1996
Assignee:
Pharmachemie B.V.
Inventors:
Marcel Gielen, Rudolph Willem, Abdeslam Bouhdid, Dick de Vos
Abstract: The invention relates to novel aromatic fluorine-containing organotin compounds of the formula {(F.sub.5 C.sub.6 RCO.sub.2 SnBu.sub.2).sub.2 O}.sub.2 and {(F.sub.5 C.sub.6 RCO.sub.2).sub.2 SnBu.sub.2 } wherein R is CH.sub.2, CH.dbd.CH or a single bond between the phenyl ring and the CO.sub.2 group, and Bu is a butyl group; as well as to anti-tumour compositions containing as an active ingredient one or more of these compounds.
Type:
Grant
Filed:
August 24, 1995
Date of Patent:
September 24, 1996
Assignee:
Pharmachemie B.V.
Inventors:
Marcel Gielen, Rudolph Willem, Abdeslam Bouhdid, Dick de Vos
Abstract: The invention relates to anti-tumor compositions containing as an active ingredient one or more compounds of the formulaAr.sub.3 Sn--O--C(O)--C.sub.6 H.sub.2 XYZwherein X and Y are each H, OH, halogen or alkyl; and Z is halogen, amino, alkoxy, acyloxy, sulphonic acid or alkyl. A number of these compounds are novel compounds.
Type:
Grant
Filed:
October 1, 1992
Date of Patent:
January 17, 1995
Assignee:
Pharmachemie B.V.
Inventors:
Mohammad Boualam, Marcel Gielen, Abdelaziz El Khloufi, Dirk De Vos, Rudolph Willem
Abstract: The invention relates to a device for use with the inhalation of powdered materials contained in rod-shaped capsules, having two parts (2, 3) which may be pivoted one relative to the other, and provided with a mixing chamber (7) having substantially tangentially directed air inlet openings, said mixing chamber having one end in communication with a mouth piece (6) and the other end in communication with a capsule receiving cavity (26), the latter being formed in conformity with the longitudinal sectional shape of a capsule and having at at least one longitudinal end a passage opening (27) for a transversely (=in the longitudinal direction of the capsule receiving cavity) reciprocating piercing needle, and wherein the part (2) of the device comprising the mouth piece (6) is mounted to pivot relative to the capsule receiving cavity comprising part (3) of the device between a closed ready for use-position and an opened position permitting the insertion of a capsule.
Type:
Grant
Filed:
September 23, 1992
Date of Patent:
June 14, 1994
Assignee:
Pharmachemie B.V.
Inventors:
Alfred J. Nijkerk, Jarig E. Schram, Sander J. Sinot
Abstract: This invention provides novel anti-tumour compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or together form an alkyl-, alkoxy- or OH-substituted aromatic group, which optionally contains an N atom as a hetero-atom; R is --COCH.sub.3 or --C.tbd.C--R.sub.4 and R.sub.4 is H or trimethylsilyl; and R.sub.3 is H or --COCF.sub.3 ; and acid addition salts thereof; as well as compositions containing these compounds.
Type:
Grant
Filed:
May 6, 1992
Date of Patent:
March 15, 1994
Assignee:
Pharmachemie B.V.
Inventors:
Johan W. Scheeren, Joannes F. M. de Bie, Dirk de Vos
Abstract: The invention provides novel cyclic triketone compounds of the formulae ##STR1## wherein S is H, alkyl or alkoxy and R* is a group of the formule ##STR2## wherein R.sup.1 is methyl and R.sub.2 is an alkyl group containing at least 2 carbon atoms or R.sup.1 is an alkyl group having 1-4 carbon atoms and R.sup.2 is an aryl group, a hetero aryl group, a --CH.sub.2 OR' group, a --CH.sub.2 N<group, a --CH.sub.2 SR" group or a --CH.sub.2 CH.dbd.CH.sub.2 group, wherein R' and R" are alkyl groups having 1-4 carbon atoms.These compounds can be used for preparing daunomycinone and derivatives thereof. Daunomycinone is used for preparing daunomycin and adriamycin.By introducing chirality at C-1 of ring A in the preparation of said novel compounds by using a novel diene of formula (1) in a Diels-Alder reaction for said preparation, the chirality of C-3 is established in the subsequent reaction with LiC.tbd.CSi(CH.sub.3).sub.3 in the synthesis of daunomycinone and deriviatives thereof.
Type:
Grant
Filed:
December 20, 1991
Date of Patent:
February 2, 1993
Assignee:
Pharmachemie B.V.
Inventors:
Johan W. Scheeren, Joannes F. Martinus De Bie, Dirk De Vos
Abstract: A carboplatin composition is provided in the form of an aqueous solution of carboplatin buffered at a pH of 2-6.5. Such a ready to use solution possesses a remarkable stability.
Type:
Grant
Filed:
May 29, 1990
Date of Patent:
April 14, 1992
Assignee:
Pharmachemie B.V.
Inventors:
Alfred J. Nijkerk, Johanna M. P. Vermeer
Abstract: The invention provides novel cyclic triketone compounds of the formulae ##STR1## wherein S is H, alkyl or alkoxy and R* is a group of the formule ##STR2## wherein R.sup.1 is methyl and R.sub.2 is an alkyl group containing at least 2 carbon atoms or R.sup.1 is an alkyl group having 1-4 carbon atoms and R.sup.2 is an aryl group, a hetero aryl group, a --CH.sub.2 OR' group, a --CH.sub.2 N< group, a --CH.sub.2 SR" group or a --CH.sub.2 CH.dbd.CH.sub.2 group, wherein R' and R" are alkyl groups having 1-4 carbon atoms.These compounds can be used for preparing daunomycinone and derivatives thereof. Daunomycinone is used for preparing daunomycin and adriamycin.by introducing chirality at C-1 of ring A in the preparation of said novel compounds by using a novel diene of formula (1) in a Diels-Alder reaction for said preparation, the chirality of C-3 is established in the subsequent reaction with LiC.tbd.CSi(CH.sub.3).sub.3 in the synthesis of daunomycinone and derivatives thereof.
Type:
Grant
Filed:
February 1, 1990
Date of Patent:
March 17, 1992
Assignee:
Pharmachemie B.V.
Inventors:
Johan W. Scheeren, Joannes F. M. DeBie, Dirk DeVos
Abstract: The invention relates to novel compounds of the formulae ##STR1## wherein S is H, alkyl or alkoxy and R is a good leaving group, and to the preparation of these compounds in a stereospecific manner to obtain a configuration wherein OH at C-3 and OR at C-1 are in the cis-position, which compounds can be used for the synthesis of daunomycinone and derivatives thereof.Daunomycinone can be used for the preparation of daunomycin and adriamycin.
Type:
Grant
Filed:
February 1, 1990
Date of Patent:
January 7, 1992
Assignee:
Pharmachemie B.V.
Inventors:
Johan W. Scheeren, Joannes F. M. De Bie, Dirk De Vos