Patents by Inventor Robert DeSimone

Robert DeSimone 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).

  • Publication number: 20150320560
    Abstract: Cranial implants, kits including cranial implants, and methods of making cranial implants are described. The cranial implants may be radiolucent. The cranial implants may have contact surfaces complementary in shape to measured portions of a surface of a specific cranium. The radiolucent cranial implants may include carbon-PEEK.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 12, 2015
    Inventors: Grant Haverstock Mulliken, Narcisse Pascal Bichot, Robert Desimone
  • Patent number: 7348326
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: March 25, 2008
    Assignee: Neurogen Corporation
    Inventors: Robert DeSimone, Alan Hutchison, Kenneth Shaw, Daniel Rosewater
  • Publication number: 20060229298
    Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
    Type: Application
    Filed: May 17, 2006
    Publication date: October 12, 2006
    Inventors: Alan Hutchison, Linda Gustavson, John Peterson, Dario Dollar, Timothy Caldwell, Taeyoung Yoon, Wallace Pringle, Rajagopal Bakthavatchalam, Yiping Shen, Cheryl Steenstra, Helen Yin, Robert DeSimone, Xiao-shu He
  • Publication number: 20060211738
    Abstract: Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma.
    Type: Application
    Filed: January 13, 2006
    Publication date: September 21, 2006
    Inventors: Scott Mitchell, Mihaela Danca, Peter Blomgren, Robert DeSimone, Douglas Pippin
  • Publication number: 20060199846
    Abstract: Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma.
    Type: Application
    Filed: January 13, 2006
    Publication date: September 7, 2006
    Inventors: Scott Mitchell, Mihaela Danca, Peter Blomgren, Robert DeSimone, Douglas Pippin, David Brittelli
  • Publication number: 20060183746
    Abstract: Certain compounds, such as at least one chemical entity choen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, may in certain embodiments be used to treat patients suffering from one or more diseases responsive to inhibition of tyrosine kinase activity. The diseases may, for instance, be responsive to inhibition of Btk activity and/or B-cell proliferation. Example diseases include cancer, an autoimmune and/or inflammatory disease, and an acute inflammatory reaction.
    Type: Application
    Filed: December 2, 2005
    Publication date: August 17, 2006
    Inventors: Kevin Currie, Robert Desimone, Scott Mitchell, Douglas Pippin, James Darrow, Xiaobing Qian, Mark Velleca, Dapeng Qian
  • Publication number: 20060178367
    Abstract: Chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are described herein. Pharmaceutical compositions comprising at least one chemical entity of Formula 1, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell proliferation are described. Methods for determining the presence of Btk in a sample are described.
    Type: Application
    Filed: November 10, 2005
    Publication date: August 10, 2006
    Inventors: Kevin Currie, Jeffrey Kropf, James Darrow, Robert Desimone
  • Publication number: 20060160842
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
    Type: Application
    Filed: December 6, 2005
    Publication date: July 20, 2006
    Applicant: Neurogen Corporation
    Inventors: Robert DeSimone, Alan Hutchison, Kenneth Shaw, Daniel Rosewater
  • Publication number: 20050288295
    Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable pharmaceutically acceptable salts, hydrates, solvates, crystal forms, diastereomers, and prodrugs thereof. Methods of treating or preventing disorders in which aberrant kinase activity is implicated, pharmaceutically compositions, and methods for detecting the presence kinases in cells or biological preparations and for identifying kinases of therapeutic interest.
    Type: Application
    Filed: November 10, 2004
    Publication date: December 29, 2005
    Inventors: Kevin Currie, Robert DeSimone, Douglas Pippin, James Darrow, Scott Mitchell
  • Publication number: 20050101604
    Abstract: Compounds of Formula I and all pharmaceutically acceptable forms thereof, are described herein. The variables R1, R2, R3, Z2, and Q, shown in Formula I are defined herein. Pharmaceutical compositions containing one or more compounds of Formula I, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Methods of treating patients suffering from certain diseases responsive to inhibition of tyrosine kinase activity are also given. In certain embodiments the diseases are responsive to inhibition of Btk activity and/or B-cell proliferation. Such methods comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These diseases include cancer, an autoimmune and/or inflammatory disease, or an acute inflammatory reaction.
    Type: Application
    Filed: June 30, 2004
    Publication date: May 12, 2005
    Inventors: Kevin Currie, Robert DeSimone, Scott Mitchell, Douglas Pippin
  • Publication number: 20050090499
    Abstract: Compounds of Formula I-a and all pharmaceutically-acceptable forms thereof, are described herein. The variables R1, R2, R3, Z1, Q, and A shown in Formula I-a are defined herein. Pharmaceutical compositions containing one or more compounds of Formula I-a, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Methods of treating patients suffering from certain diseases responsive to inhibition of tyrosine kinase activity are also given. In certain embodiments the diseases are responsive to inhibition of Btk activity and/or B-cell proliferation. Such methods comprise administering to such patients an amount of a compound of Formula I-a effective to reduce signs or symptoms of the disease. These diseases include cancer, an autoimmune and/or inflammatory disease, or an acute inflammatory reaction.
    Type: Application
    Filed: June 4, 2004
    Publication date: April 28, 2005
    Inventors: Kevin Currie, Robert DeSimone, Scott Mitchell, Douglas Pippin, James Darrow, Xiaobing Qian, Mark Velleca, Dapeng Qian
  • Publication number: 20050085484
    Abstract: Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically-acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound of the invention to decrease the symptoms or slow the progression of these diseases or disorders.
    Type: Application
    Filed: August 11, 2004
    Publication date: April 21, 2005
    Inventors: Scott Mitchell, Robert DeSimone, James Darrow, Douglas Pippin, M. Danca
  • Publication number: 20050054648
    Abstract: This invention pertains to compounds of Formula I: and all pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including of breast neoplasma, endometrial cancer, colon cancer, and neck squamous cell carcinoma.
    Type: Application
    Filed: February 10, 2004
    Publication date: March 10, 2005
    Inventors: Scott Mitchell, Kevin Currie, Robert DeSimone, Douglas Pippin
  • Publication number: 20050054649
    Abstract: This invention pertains to compounds of Formula I: and the pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to Hsp90 complex modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including chronic myeloid leukemia, melanoma, breast, ovarian, brain, thyroid, colorectal, prostate, and bladder cancer, heart disease, stroke, autoimmune/inflammatory diseases, and neurodegenerative diseases.
    Type: Application
    Filed: February 10, 2004
    Publication date: March 10, 2005
    Inventors: Kevin Currie, Robert DeSimone, Douglas Pippin, James Darrow, Scott Mitchell
  • Publication number: 20030229076
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: September 16, 2002
    Publication date: December 11, 2003
    Inventors: Stanislaw Rachwal, Alan Hutchison, Kenneth Shaw, George D. Maynard, Xiao-Shu He, Robert DeSimone, Kevin Hodgetts
  • Patent number: 6509366
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein Y, R1, R2, R3, R4, R5, R6, R7 R7′ are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are therefore useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis, and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
    Type: Grant
    Filed: January 17, 2001
    Date of Patent: January 21, 2003
    Assignee: Neurogen Corporation
    Inventors: Stanislaw Rachwal, Alan Hutchison, Kenneth Shaw, George D. Maynard, Xiao-shu He, Robert DeSimone, Kevin Hodgetts
  • Patent number: 6482844
    Abstract: Provided are compounds (and pharmaceutically acceptable non-toxic salt of such compounds) of the formula: in which A and B are C1-C3 alkylene; R1 is C1-C6 alkyl; R2 and R3 are hydrogen or C1-C6 alkyl; U and V are C1-C6 alkyl or halogen; X, Y and Z are hydrogen, C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, trifluoromethoxy, halogen, or cyano; and W represents up to three substituents which are C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, trifluoromethoxy, halogen, hydroxy, amino, or cyano. These compounds act as modulators of blood glucose levels and are useful for the treatment of diabetes, eating disorders, and obesity. Pharmaceutical compositions and methods of use of the compounds as pharmaceutical agents are also provided.
    Type: Grant
    Filed: April 6, 2001
    Date of Patent: November 19, 2002
    Assignee: Neurogen Corporation
    Inventors: Xiao-Shu He, Xiaoyan Zhang, He Zhao, Robert DeSimone, Andrew Thurkauf
  • Publication number: 20020115693
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: January 17, 2001
    Publication date: August 22, 2002
    Inventors: Stanislaw Rachwal, Alan Hutchison, Kenneth Shaw, George D. Maynard, Xiao-shu He, Robert DeSimone, Kevin J. Hodgetts
  • Patent number: 6316617
    Abstract: This invention encompasses compounds of the formula where X1, X2, and X3, independently represent substituents of formula  and the pharmaceutically acceptable salts thereof wherein the remaining variables are as defined herein and wherein said compounds are useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: November 13, 2001
    Assignee: Neurogen Corporation
    Inventors: Charles A. Blum, Robert DeSimone, Alan Hutchison, John M. Peterson
  • Patent number: 6133265
    Abstract: Amido, amino and sulfonamide substituted benzylamine derivatives useful in treating eating disorders have the formula ##STR1## where X.sub.1, X.sub.2, and X.sub.3, independently represent substituents of formula ##STR2## D=H, lower straight or branched chain alkyl having 1-6 carbon atoms, a methylene unit incorporated into a ring connected with G as in the cases of pyrrolidine, pyrrolidone, piperidine, and piperidone;E=O or H.sub.2 ;O=0 or 1;G=straight or branched chain lower alkyl having 1-6 carbon atoms, aryl, aryl substituted with halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, heteroaryl--selected from the group consisting of 2-, 3-, or 4-pyridyl, 2-pyrazyl, 2-, or 3-thienyl, 2-pyrazinyl, 2-, 3-, or 4-quinolyl, 1-, 3-, or 4-isoquinolyl, 2-quinoxalyl, 3-, or 4-cinnolyl, said heteroaryl substituted with halogen, hydroxy, straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms;and A, T and R.sub.1 -R.sub.
    Type: Grant
    Filed: July 18, 1997
    Date of Patent: October 17, 2000
    Assignee: Neurogen Corporation
    Inventors: Charles A. Blum, Robert DeSimone, Alan Hutchison, John M. Peterson