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| Number | Title | Issue Date |
| 6552166 | Process 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 |
| 6500841 | 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... | 12/31/2002 |
| 6413964 | Inhibitors 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 |
| 6410534 | Inhibitors 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 |
| 6391305 | Conjugates 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 |
| 6380228 | Inhibitors 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 |
| 6376496 | Inhibitors 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 |
| 6358956 | Inhibitors 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 |
| 6358985 | Inhibitors 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 |
| 6355643 | Inhibitors 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 |
| 6355611 | Salt 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 |
| 6350755 | Inhibitors 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 |
| 6335343 | Inhibitors 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 |
| 6333335 | Phenyl-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 |
| 6329376 | Inhibitors 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 |
| 6207798 | Modified 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 |
| 6177404 | Conjugates 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 |
| 6160015 | Compounds 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 |
| 6130204 | Peptides 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 |
| 6127333 | Conjugates 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 |
| 6127390 | Inhibitors 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 |
| 6103487 | Method 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 |
| 6093737 | 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... | 07/25/2000 |
| 6077853 | 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... | 06/20/2000 |
| 5998362 | Conjugates 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 |
| 5972942 | 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... | 10/26/1999 |
| 5948750 | Conjugates 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 |
| 5939439 | 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... | 08/17/1999 |
| 5919785 | 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... | 07/06/1999 |
| 5912322 | Modified 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 |
| 5891889 | 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... | 04/06/1999 |
| 5885995 | 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... | 03/23/1999 |
| 5883105 | 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... | 03/16/1999 |
| 5880140 | Biheteroaryl 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 |
| 5874452 | Biheteroaryl 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 |
| 5872136 | Arylheteroaryl 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 |
| 5869682 | 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... | 02/09/1999 |
| 5866679 | Peptides 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 |
| 5859012 | Inhibitors 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 |
| 5859015 | N-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 |