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Attorney: Muthard; David A., Daniel; Mark R.


Number of patents: 83
Last date: April 22, 2003

1      
NumberTitleIssue Date
6552166Process for the preparation of conjugates useful in the treatment of prostate cancer
The present invention is directed to the improved synthesis of compounds of formula I: ##STR1## which may be useful in the treatment of prostate cancer. Such compounds are synthesized in the presence of a carboxyl activating agent, an additive and a ...
04/22/2003
6500841Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
12/31/2002
6413964Inhibitors of prenyl-protein transferase
The present invention is directed to peptidomimetic macrocyclic compounds of the formula A: ##STR1## wherein W is a heterocycle, V is a heterocycle or aryl moiety and Z1 is a suitably substituted aryl or heterocycle moiety. The instant com...
07/02/2002
6410534Inhibitors of prenyl-protein transferase
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds...
06/25/2002
6391305Conjugates useful in the treatment of prostate cancer
Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking groups and known cytotoxic agents are disclosed. Such con...
05/21/2002
6380228Inhibitors of prenyl-protein transferase
The present invention is directed to peptidomimetic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this inv...
04/30/2002
6376496Inhibitors of prenyl-protein transferase
The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of canc...
04/23/2002
6358956Inhibitors of prenyl-protein transferase
The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including-farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of canc...
03/19/2002
6358985Inhibitors of prenyl-protein transferase
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds...
03/19/2002
6355643Inhibitors of prenyl-protein transferase
The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, ##STR1## which inhibit prenyl-protein transferases. In parti...
03/12/2002
6355611Salt form of a conjugate useful in the treatment of prostate cancer
The present invention is directed to the sodium salt of formula 5: ##STR1## which may be useful in the treatment of prostate cancer and benign prostatic hyperplasia. Also described are lyophilized formulations that comprise the sodium salt 5 or the corres...
03/12/2002
6350755Inhibitors of prenyl-protein transferase
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds...
02/26/2002
6335343Inhibitors of prenyl-protein transferase
The present invention comprises piperazine/piperazinone-containing compounds having multicyclic ring system substituents on one of the piperazine/piperazinone nitrogens, which inhibit prenyl-protein transferases, including farnesyl-protein transferase and...
01/01/2002
6333335Phenyl-protein transferase inhibitors
The present invention is directed to tetrahydro-imidazopyridinyl compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compound...
12/25/2001
6329376Inhibitors of prenyl-protein transferase
The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit a prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compo...
12/11/2001
6207798Modified PE40 toxin fusion proteins
We have modified PE40 toxin by removing at least two of its four cysteine amino acid residues and have formed hybrid molecules containing modified PE40 linked to a cell recognition protein that can be an antibody, a growth factor, a ...
03/27/2001
6177404Conjugates useful in the treatment of benign prostatic hyperplasia
Novel pharmaceutical compositions useful for the treatment of benign prostatic hyperplasia which comprises novel oligopeptides, which are selectively cleaved by enzymatically active PSA, in conjugation with a cytotoxic agent are described. Methods of trea...
01/23/2001
6160015Compounds useful in the treatment of neurofibromatosis
The present invention relates to compositions useful in the treatment of benign proliferative disorder neurofibromatosis comprising a farnesyl protein transferase inhibitor. Further contained in this invention are methods of treating benign proliferative ...
12/12/2000
6130204Peptides
Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease a...
10/10/2000
6127333Conjugates useful in the treatment of prostate cancer
Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. The conjugates of the invention are characterized ...
10/03/2000
6127390Inhibitors of prenyl-protein transferase
The present invention is directed to compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention ...
10/03/2000
6103487Method of treating cancer
The instant invention provides for a method of inhibiting prenyl-protein transferases and treating cancer which comprises administering to a mammal a prenyl-protein transferase inhibitor which is efficacious in vivo as an inhibitor of geranylgeranyl-prote...
08/15/2000
6093737Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
07/25/2000
6077853Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
06/20/2000
5998362Conjugates useful in the treatment of prostate cancer
Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking groups and known cytotoxic agents are disclosed. Such con...
12/07/1999
5972942Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
10/26/1999
5948750Conjugates useful in the treatment of prostate cancer
Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of pro...
09/07/1999
5939439Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
08/17/1999
5919785Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
07/06/1999
5912322Modified pseudomonas exotoxin PE40
Psuedomonas exotoxin 40 is modified by deleting or substituting one or more cysteine residues. Such a modified protein may be incorporated into a fusion protein with TGF଱. The resulting fusion protein exhibits altered biological activities from unmo...
06/15/1999
5891889Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
04/06/1999
5885995Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
03/23/1999
5883105Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
03/16/1999
5880140Biheteroaryl inhibitors of farnesyl-protein transferase
The present invention is directed to compounds of the formula A which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras: ##STR1## The invention is further directed to chemotherapeutic compositions con...
03/09/1999
5874452Biheteroaryl inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
02/23/1999
5872136Arylheteroaryl inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
02/16/1999
5869682Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
02/09/1999
5866679Peptides
Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease a...
02/02/1999
5859012Inhibitors of farnesyl-protein transferase
The present invention is directed to piperazine-2,3-dione compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the com...
01/12/1999
5859015N-heterocyclic piperazinyl and H-heterocyclic piperazinonyl inhibitors of farnesyl-protein transferase
The present invention is directed to compounds of the formula A which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras: ##STR1## The invention is further directed to chemotherapeutic compositions con...
01/12/1999
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