Patents by Inventor Roland Ellwood Dolle, III

Roland Ellwood Dolle, III 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: 7037916
    Abstract: Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, —O—alkyl or —S-alkyl.
    Type: Grant
    Filed: January 10, 2003
    Date of Patent: May 2, 2006
    Assignee: Pharmacopeia Drug Discovery, Inc.
    Inventors: Shawn David Erickson, John J. Baldwin, Roland Ellwood Dolle, III, James Inglese, Michael H. J. Ohlmeyer, Koc-Kan Ho, Adolph C Bohnstedt, Steven G. Kultgen, Paolo Giovanni Martino Conti, Dirk Leysen, Jaap van der Louw
  • Patent number: 6887865
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: May 3, 2005
    Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6864368
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: March 8, 2005
    Assignees: Berlax Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6864263
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: March 8, 2005
    Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6849739
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: February 1, 2005
    Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6846829
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: January 25, 2005
    Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6841673
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: January 11, 2005
    Assignees: Berlex Laboratories, Inc., Pharmacopeia, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6841674
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: January 11, 2005
    Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6747031
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: June 8, 2004
    Assignees: Berlex Laboratories, Inc., Pharmacopeia, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6670473
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: December 30, 2003
    Assignees: Berlex Laboratories, Inc., Pharmacopeia, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6432947
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: August 26, 1999
    Date of Patent: August 13, 2002
    Assignees: Berlex Laboratories, Inc., Pharmacopeia, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6432933
    Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or &agr;-hydroxyamide group and Z is an acyl or &agr;-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.
    Type: Grant
    Filed: June 20, 2000
    Date of Patent: August 13, 2002
    Assignee: Pharmacopeia, Inc.
    Inventors: Carolyn DiIanni Carroll, Roland Ellwood Dolle, III, Yvonne Class Shimshock, Timothee Felix Herpin
  • Patent number: 6326393
    Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or &agr;-hydroxyamide group and Z is an acyl or &agr;-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.
    Type: Grant
    Filed: June 20, 2000
    Date of Patent: December 4, 2001
    Assignee: Pharmacopeia, Inc.
    Inventors: Carolyn DiIanni Carroll, Roland Ellwood Dolle, III, Yvonne Class Shimshock, Timothee Felix Herpin
  • Patent number: 6265228
    Abstract: Combinatorial chemical libraries of the Formula [S]—C(O)—L′—Z containing dihyroxy amides and hydroxyphosphonate amides are disclosed, in which [S] represents a solid support and —L′—Z is a linker/ligand residue. In these libraries, Z is and Y is —P(O)(OR6)(OR7), —CH(OH)—COR8, —CH,CH═CH2—CH2CH(OH)CH2OH, —CH2CHO, —CH2CH2OH, —CH2CH2OC(O)NHR26, —CH2CH2NR27R28, or The combinatorial libraries are optionally encoded with tags. The use of these libraries in assays to discover biologically active compounds is also disclosed.
    Type: Grant
    Filed: June 18, 1999
    Date of Patent: July 24, 2001
    Assignee: Pharmacopeia, Inc.
    Inventors: Roland Ellwood Dolle, III, Timothee Felix Herpin, Yvonne Class Shimshock, Cullen Lee Cavallaro
  • Patent number: 6255120
    Abstract: A combinatorial chemical library comprising a plurality of members of the Formula [S]—C(O)—L′-Z containing hydroxyamides is disclosed, in which [S] represents a solid support and L′-Z is a linker/compound residue. In this library, Z is and Y is —NR3R4 or —OR9. R3 and R4 are independently selected from the group consisting of H, alkyl, aralkyl, heteroarylalkyl, heterocycloalkyl, —CH(R5)CH(R6)OH, —CH(R5)C(O)NHR6 and —CH(R5)C(O)NHCH(R6)C(O)NHR7. R3 and R4 together are wherein X=O or NR8 and R9 is aryl, aralkyl or R7CH═CH(CH2){overscore (n)}. The combinatorial library can be optionally encoded with identifiers T′-L, which are covalently attached to the solid support. The methods of synthesizing such a library are described. The use of such library in assays to discover biologically active compounds is also disclosed.
    Type: Grant
    Filed: May 15, 1998
    Date of Patent: July 3, 2001
    Assignee: Pharmacopeia, Inc.
    Inventors: Roland Ellwood Dolle, III, Cullen Lee Cavallaro, Timothee Felix Herpin
  • Patent number: 6218551
    Abstract: Combination chemical libraries of Formula I and methods for preparation are disclosed. The libraries allow one to screen large numbers of compounds for a desired biological activity with relative ease. The libraries may be tagged or untagged. In preferred libraries, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or substituted piperazinealkanoic acid. The use of the libraries to discover biologically active compounds is also disclosed.
    Type: Grant
    Filed: June 21, 1999
    Date of Patent: April 17, 2001
    Assignee: Pharmacopeia, Inc.
    Inventors: Roland Ellwood Dolle, III, Tao Guo, Theodore Otto Johnson, Jr., Hitesh K. Patel, Shiwei Tao, Zhen Min He
  • Patent number: 6191277
    Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathsepsin D. The compounds are useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is a heterocycle, amide, sulfonamide or carbamate and Z is an acyl or a functionalized acyl. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid phase support, are also disclosed.
    Type: Grant
    Filed: September 29, 1999
    Date of Patent: February 20, 2001
    Assignee: Pharmacopeia, Inc.
    Inventors: Roland Ellwood Dolle, III, Cullen Lee Cavallaro, Timothee Felix Herpin
  • Patent number: 6175020
    Abstract: Azaspirononanes of formula I and their synthesis are disclosed. The compounds are useful as templates for constructing synthetic receptors and as intermediates in the synthesis of enzyme inhibitors. They are prepared by an intramolecular ylide cycloaddition of a 6-hydrazone of 2,10-undecadienoic acid ester.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: January 16, 2001
    Assignee: Pharmacopeia, Inc.
    Inventors: Roland Ellwood Dolle, III, Michael C. Barden
  • Patent number: 6150344
    Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or .alpha.-hydroxyamide group and Z is an acyl or .alpha.-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.
    Type: Grant
    Filed: May 26, 1999
    Date of Patent: November 21, 2000
    Assignee: Pharmacopeia, Inc.
    Inventors: Carolyn DiIanni Carroll, Roland Ellwood Dolle, III, Yvonne Class Shimshock, Timothee Felix Herpin
  • Patent number: 5986102
    Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathsepsin D. The compounds are useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is a heterocycle, amide, sulfonamide or carbamate and Z is an acyl or a functionalized acyl. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid phase support, are also disclosed.
    Type: Grant
    Filed: April 29, 1998
    Date of Patent: November 16, 1999
    Assignee: Pharmacopeia, Inc.
    Inventors: Roland Ellwood Dolle, III, Cullen Lee Cavallaro, Timothee Felix Herpin