Patents by Inventor Johan W. Scheeren

Johan W. Scheeren has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 6344571
    Abstract: The invention relates to water soluble antitumor analogs of paclitaxel of formula (I) wherein R1=C(O)CH2CH(OH)COOX, R2=H, C(O)CH2CH(OH)COOX, X=H, Li, Na or any other pharmaceutically acceptable counterion, as well as to a pharmaceutical composition comprising an antineoplastically effective amount of such analogs as an active ingredient.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: February 5, 2002
    Assignee: Pharmachemie B.V.
    Inventors: Peter H. G. Wiegerinck, Duncan Sperling, Lesly Braamer, Eric W. P. Damen, Johan W. Scheeren, Dick de Vos
  • Publication number: 20010018531
    Abstract: The invention relates to water soluble antitumor analogs of paclitaxel of formula (I) wherein R1═C(O)CH2CH(OH)COOX, R2═H, C(O)CH2CH(OH)COOX, X═H, Li, Naa or any other pharmaceutically acceptable counterion, as well as to a pharmaceutical composition comprising an antineoplastically effective amount of such analogs as an active ingredient.
    Type: Application
    Filed: February 21, 2001
    Publication date: August 30, 2001
    Inventors: Peter H.G. Wiegerinck, Duncan Sperling, Lesly Braamer, Eric W.P. Damen, Johan W. Scheeren, Dick de Vos
  • Patent number: 5760072
    Abstract: A paclitaxel prodrug has a paclitaxel portion coupled to a cleavable N-(aliphatic or aromatic)-O-glycosyl carbamate spacer group, and can be administered orally, topically or by injection to provide an anti-tumor effect, the prodrug being activated by a hydrolizing enzyme, an endogeneous enzyme or an exogeneous enzyme.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: June 2, 1998
    Assignee: Pharmachemie B.V.
    Inventors: Hendricus B. A. de Bont, Ruben G. G. Leenders, Johan W. Scheeren, Hidde J. Haisma, Dick de Vos
  • Patent number: 5348949
    Abstract: The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## by an intramolecular ringclosure reaction of compounds of formula 2. ##STR2## wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a function during the ringclosure reaction.The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumour activity.
    Type: Grant
    Filed: February 12, 1993
    Date of Patent: September 20, 1994
    Assignee: Duphar International Research B.V.
    Inventors: Peter H. H. Hermkens, Jan H. Van Maarseveen, Johan W. Scheeren, Cornelis G. Kruse
  • Patent number: 5294701
    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
  • Patent number: 5183913
    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
  • Patent number: 5106840
    Abstract: The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## wherein R.sub.1 is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino.n has the value 0, 1 or 2,R.sub.2 is hydrogen, lower alkyl or acyl,R.sub.3 is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R.sub.
    Type: Grant
    Filed: June 5, 1990
    Date of Patent: April 21, 1992
    Assignee: Duphar International Research B.V.
    Inventors: Peter H. H. Hermkens, Jan H. Van Maarseveen, Johan W. Scheeren, Cornelis G. Kruse
  • Patent number: 5097051
    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
  • Patent number: 5079349
    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