Patents by Inventor S. Jane deSolms
S. Jane deSolms 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).
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Patent number: 5817678Abstract: 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 invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: November 15, 1996Date of Patent: October 6, 1998Assignee: Merck & Co., Inc.Inventors: Byeong M. Kim, Anthony W. Shaw, Samuel L. Graham, S. Jane deSolms, Terrence M. Ciccarone
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Patent number: 5703241Abstract: The present invention comprises an analog of the CA.sub.1 A.sub.2 X motif of the protein Ras that is modified by farnesylation in vivo. This CA.sub.1 A.sub.2 X analog inhibits the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, this CA.sub.1 A.sub.2 X analog differs from most compounds previously described as inhibitors of farnesyl-protein transferase in that it does not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. The compound of the instant invention also incorporates a cyclic amine moiety in the A.sup.1 position of the motif. Further contained in this invention are chemotherapeutic compositions containing this farnesyl transferase inhibitor and methods for its production.Type: GrantFiled: October 10, 1996Date of Patent: December 30, 1997Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Samuel L. Graham
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Patent number: 5686472Abstract: 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 invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: October 27, 1993Date of Patent: November 11, 1997Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, S. Jane deSolms, Ta Jyh Lee, deceased
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Patent number: 5661161Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl-protein transferase. Furthermore, these CAAX analogues differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid antoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 14, 1995Date of Patent: August 26, 1997Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Terrence M. Ciccarone, S. Jane deSolms, Samuel L. Graham, Gerald E. Stokker, Catherine M. Wiscount
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Patent number: 5652257Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 21, 1995Date of Patent: July 29, 1997Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, S. Jane deSolms, Robert P. Gomez, Samuel L. Graham, John H. Hutchinson, Gerald E. Stokker
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Patent number: 5627202Abstract: The present invention comprises analogs of the CA.sup.1 A.sup.2 X motif of the protein Ras that is modified by farnesylation in vivo. These CA.sup.1 A.sup.2 X analogs inhibit the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, these CA.sup.1 A.sup.2 X analogs differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. The compounds of the instant invention also incorporate a cyclic amine moiety in the A.sup.2 position of the motif. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: February 13, 1996Date of Patent: May 6, 1997Assignee: Merck & Co., Inc.Inventor: S. Jane deSolms
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Patent number: 5624936Abstract: The present invention comprises analogs of the CA.sup.1 A.sup.2 X motif of the protein Ras that is modified by farnesylation in vivo. These CA.sup.1 A.sup.2 X analogs inhibit the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, these CA.sup.1 A.sup.2 X analogs differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. The compounds of the instant invention also incorporate a cyclic amine moiety in the A.sup.2 position of the motif. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: February 13, 1996Date of Patent: April 29, 1997Assignee: Merck & Co., Inc.Inventor: S. Jane deSolms
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Patent number: 5576293Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 29, 1994Date of Patent: November 19, 1996Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Victor M. Garsky, Elizabeth A. Giuliani, Robert P. Gomez, Samuel L. Graham, Gerald E. Stokker, Catherine M. Wiscount
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Patent number: 5571835Abstract: The present invention comprises analogs of the CA.sub.1 A.sub.2 X motif of the protein Ras that is modified by farnesylation in vivo. These CA.sub.1 A.sub.2 X analogs inhibit the farnesylation of Ras. Furthermore, these CA.sub.1 A.sub.2 X analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they have a prolyl like moiety in the A.sub.1 position. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 29, 1994Date of Patent: November 5, 1996Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, S. Jane deSolms, Samuel L. Graham
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Patent number: 5536750Abstract: 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 invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: November 30, 1994Date of Patent: July 16, 1996Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Samuel L. Graham
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Patent number: 5504115Abstract: 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 invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: June 28, 1994Date of Patent: April 2, 1996Assignee: Merck & Co., Inc.Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
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Patent number: 5491164Abstract: The present invention comprises dipeptide analogs that inhibit the farnesylation of Ras. These farnesyl-protein transferase inhibitors are characterized by the inclusion of a cyclic amine in the backbone of the dipeptide. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 29, 1994Date of Patent: February 13, 1996Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Samuel J. Graham
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Patent number: 5480893Abstract: 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 invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: May 13, 1994Date of Patent: January 2, 1996Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, S. Jane deSolms
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Patent number: 5468733Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 30, 1993Date of Patent: November 21, 1995Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Elizabeth A. Giuliani, Samuel L. Graham
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Patent number: 5439918Abstract: 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 invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.Type: GrantFiled: March 14, 1994Date of Patent: August 8, 1995Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Samuel L. Graham
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Patent number: 5352705Abstract: 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 invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: June 26, 1992Date of Patent: October 4, 1994Assignee: Merck & Co., Inc.Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
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Patent number: 5340828Abstract: 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 invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: September 30, 1991Date of Patent: August 23, 1994Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, S. Jane deSolms
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Patent number: 5238922Abstract: 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 invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: September 30, 1991Date of Patent: August 24, 1993Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, S. Jane deSolms, Victor M. Garsky
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Patent number: 4755612Abstract: This invention relates to novel intermediate compounds resulting from a method for forming a dihydrogen-phosphate inositol from a protected or unprotected inositol that comprises at least two vicinal trans hydroxy groups that are unprotected. This method results in each of the unprotected hydroxy groups of the inositol, which can contain from two to six unprotected hydroxy groups, being converted to a dihydrogen-phosphate group and each protected group being converted to a free hydroxy group. The method permits one to make such compounds in very few steps and in very high yields.Type: GrantFiled: July 20, 1987Date of Patent: July 5, 1988Assignee: Merck & Co., Inc.Inventors: Joseph P. Vacca, S. Jane deSolms
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Patent number: 4272537Abstract: This invention relates to 3-amino-5-substituted-6-halo-N-(4,4-disubstituted-6-substituted-1,3,5-tria zin-2-yl)-2-pyrazinecarboxamides and processes for preparing same. The compounds are eukalemic/saluretic agents useful in the treatment of edema and hypertension.Type: GrantFiled: July 2, 1980Date of Patent: June 9, 1981Assignee: Merck & Co., Inc.Inventors: Otto W. Woltersdorf, Jr., S. Jane deSolms, Robert L. Smith