Patents by Inventor John J. Piwinski

John J. Piwinski 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: 6436928
    Abstract: A compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —SO0-2—, —NR12—, —NCOR12— or —NR12SO2R15;  is X2 is —O—, —S— or optionally substituted nitrogen; Y is ═O, ═S or ═NR11; Y1 is H, alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6-heterocycloalkyl, -alkyl-NH—C(O)O-alkyl or —NHC(O)R15; R1, R2, R3 and R7 are H, alkyl, OH-alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2 form an alkylene ring; or R1 and R2 together are ═O; R6 is H, alkyl, —OR13 or —SR12; and the remaining variables are as defined in the specification, is disclosed, as well as a pharmaceutical compositions comprising said compound, methods of
    Type: Grant
    Filed: December 14, 2000
    Date of Patent: August 20, 2002
    Assignee: Schering Corporation
    Inventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
  • Publication number: 20020103235
    Abstract: The present invention discloses novel substituted imidazole compounds which have either or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.
    Type: Application
    Filed: September 18, 2001
    Publication date: August 1, 2002
    Inventors: Robert G. Aslanian, Stuart B. Rosenblum, Mwangi Wa Mutahi, Neng-Yang Shih, John J. Piwinski
  • Publication number: 20020086859
    Abstract: The present invention discloses novel substituted imidazole compounds which have dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.
    Type: Application
    Filed: September 18, 2001
    Publication date: July 4, 2002
    Inventors: Neng-Yang Shih, Daniel M. Solomon, John J. Piwinski, Andrew T. Lupo, Michael J. Green
  • Publication number: 20020082278
    Abstract: The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, nasal congestion, inflammatory and CNS-related diseases and others.
    Type: Application
    Filed: September 18, 2001
    Publication date: June 27, 2002
    Inventors: Neng-Yang Shih, Robert G. Aslanian, Daniel M. Solomon, Stuart B. Rosenblum, Mwangi Wa Mutahi, Wing C. Tom, Kevin D. Mc Cormick, John J. Piwinski, Ronald Wolin
  • Publication number: 20020082272
    Abstract: The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist activity or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, congestion, inflammatory and CNS-related diseases and others.
    Type: Application
    Filed: September 18, 2001
    Publication date: June 27, 2002
    Inventors: Neng-Yang Shih, Robert G. Aslanian, John J. Piwinski, Andrew T. Lupo, Adriano Afonso
  • Publication number: 20020068742
    Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.
    Type: Application
    Filed: April 9, 2001
    Publication date: June 6, 2002
    Inventors: W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
  • Patent number: 6365588
    Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of the formulas 5.0, 5.1 and 5.2, wherein R is —C(R20)(R21)(R46), and 5.3, 5.3A and 5.3B, wherein R is —N(R25)(R48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.
    Type: Grant
    Filed: July 9, 1999
    Date of Patent: April 2, 2002
    Assignee: Schering Corporation
    Inventors: Robert W. Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
  • Patent number: 6300338
    Abstract: A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 Also disclosed are novel compounds of the formulas: Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3. Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
    Type: Grant
    Filed: July 7, 1999
    Date of Patent: October 9, 2001
    Assignee: Schering Corporation
    Inventors: W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
  • Patent number: 6242458
    Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of the formulas 5.1 and 5.2 are disclosed.
    Type: Grant
    Filed: September 21, 1999
    Date of Patent: June 5, 2001
    Assignee: Schering Corporation
    Inventors: W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
  • Patent number: 6211182
    Abstract: This invention discloses novel imidazoles substituted with a six or seven membered heterocyclic ring which contains two nitrogen atoms as part of the heterocyclic ring structure. These compounds have excellent histamine-H3 receptor antagonist activity. Also disclosed are methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)—i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypomotility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimer's Disease, schizophrenia, and migraine).
    Type: Grant
    Filed: March 8, 1999
    Date of Patent: April 3, 2001
    Assignee: Schering Corporation
    Inventors: Wayne Vaccaro, John J. Piwinski, Wing C. Tom, Daniel M. Solomon, Robert G. Aslanian
  • Patent number: 6103735
    Abstract: The present invention is directed towards a pharmaceutical composition useful for the treatment of allergic rhinitis, asthma and related disorders. In one embodiment, the composition comprises, in combination, a therapeutically effective amount of at least one neurokinin antagonist, a therapeutically effective amount of at least one H.sub.3 antagonist and a therapeutically effective amount of at least one H.sub.1 antagonist.
    Type: Grant
    Filed: October 6, 1999
    Date of Patent: August 15, 2000
    Assignee: Schering Corporation
    Inventors: Robert G. Aslanian, John J. Piwinski
  • Patent number: 6100279
    Abstract: Disclosed are compounds of Formula I ##STR1## or pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula I. Further disclosed is a method of treating allergy (for example asthma), inflammation, hypotension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimer's, schizophrenia, obesity and migraine) comprising administering an effective amount of a compound of Formula I to a patient in need of such treatment.
    Type: Grant
    Filed: November 5, 1998
    Date of Patent: August 8, 2000
    Assignee: Schering Corporation
    Inventors: Wayne D. Vaccaro, Ronald L. Wolin, Daniel M. Solomon, Robert G. Aslanian, John J. Piwinski, Stuart B. Rosenblum
  • Patent number: 6075025
    Abstract: A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 ##STR1## Also disclosed are novel compounds of the formulas: ##STR2## Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3.Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
    Type: Grant
    Filed: March 11, 1998
    Date of Patent: June 13, 2000
    Assignee: Schering Corporation
    Inventors: W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
  • Patent number: 6051575
    Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, R.sub.c, y, m, u, Ar.sub.2, n, X, R.sub.c', I and Ar.sub.2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
    Type: Grant
    Filed: May 17, 1999
    Date of Patent: April 18, 2000
    Assignee: Schering Corporation
    Inventors: David J. Blythin, Xiao Chen, Richard J. Friary, Kevin D. McCormick, John J. Piwinski, Neng-Yang Shih, Ho-Jane Shue
  • Patent number: 6034251
    Abstract: Disclosed are novel phenyl-alkyl-imidazoles of the formula ##STR1## wherein R.sup.1, R.sup.7, m, n, p, q, X, Y, Z, R and R.sup.15 are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Further disclosed are methods of treating allergy, inflammation, hypotension, glaucoma, sleeping disorders, states of hyper and hypo motility of the gastrointestinal tract, hypo and hyperactivity of the central nervous system, Alzheimer's, schizophrenia, obesity and migraines by administering compounds of formula I.Also disclosed are methods for treatment of upper airway allergic responses comprising administering a compound, or salt or solvate thereof, of formula I in combination or admixture with a histamine H.sub.1 receptor antagonist.
    Type: Grant
    Filed: November 5, 1998
    Date of Patent: March 7, 2000
    Assignee: Schering Corporation
    Inventors: Robert G. Aslanian, Kevin D. McCormick, John J. Piwinski
  • Patent number: 5981520
    Abstract: The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
    Type: Grant
    Filed: June 17, 1998
    Date of Patent: November 9, 1999
    Assignee: Schering Corporation
    Inventors: Ho-Jane Shue, Neng-Yang Shih, David J. Blythin, Xiao Chen, Wing C. Tom, John J. Piwinski, Kevin D. McCormick
  • Patent number: 5977128
    Abstract: A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 ##STR1## Also disclosed are novel compounds of the formulas: ##STR2## Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3.Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
    Type: Grant
    Filed: November 14, 1997
    Date of Patent: November 2, 1999
    Assignee: Schering Corporation
    Inventors: Robert W. Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
  • Patent number: 5968929
    Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, R.sub.c, y, m, u, Ar.sub.2, n, X, R.sub.c', l and Ar.sub.2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: October 19, 1999
    Assignee: Schering Corporation
    Inventors: David J. Blythin, Xiao Chen, Richard J. Friary, Kevin D. McCormick, John J. Piwinski, Neng-Yang Shih, Ho-Jane Shue
  • Patent number: 5892039
    Abstract: The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
    Type: Grant
    Filed: August 30, 1996
    Date of Patent: April 6, 1999
    Assignee: Schering Corporation
    Inventors: Ho-Jane Shue, Neng-Yang Shih, David J. Blythin, Xiao Chen, John J. Piwinski, Kevin D. McCormick
  • Patent number: 5869488
    Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, R.sub.c, y, m, u, Ar.sub.2, n, X, R.sub.c', I and Ar.sub.2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
    Type: Grant
    Filed: August 29, 1996
    Date of Patent: February 9, 1999
    Assignee: Schering Corporation
    Inventors: Ho-Jane Shue, Neng-Yang Shih, David J. Blythin, Xiao Chen, John J. Piwinski, Kevin D. McCormick