Abstract: Disclosed are compounds of formula III and a process to prepare a compound of formula III wherein R1, R2, R3 and R6 are defined herein, using a zinc chloride/optionally substituted oxazole adduct and an compound of formula I. Further disclosed are methods of using compounds of formula III to prepare compounds useful in the treatment of Alzheimer's disease and related conditions.
Abstract: Disclosed is a non-sustained release pharmaceutical tablet composition which comprises a rapidly precipitating drug in an amount from about 5 to about 60% and at least one member selected from the group consisting of a binder in an amount of from about 2 to about 25% and a superdisintegrant in an amount from about 6 to about 40% where the rapidly precipitating drug, “binder” and superdisintegrant are mixed and compressed into a tablet without heating, solvent or grinding.
Type:
Grant
Filed:
September 6, 2000
Date of Patent:
September 19, 2006
Assignee:
Pharmacia & Upjohn Company
Inventors:
Alice C. Martino, Ashley H. Bates, Walter Morozowich, E. John Lee
Abstract: A pharmaceutical composition in a form of an orally deliverable liquid comprises water having in solution therein a pharmaceutically acceptable water-soluble salt of a tolterodine related compound at a therapeutically effective concentration in the composition. The composition has a pH of about 2 to about 6 and further comprises a sweetening agent and an antimicrobial agent at a concentration that is antimicrobially effective at the pH of the composition. The composition is useful for treating a muscarinic receptor mediated disorder, more particularly overactive bladder, in a subject by orally administering to the subject a therapeutically effective amount of the composition.
Type:
Grant
Filed:
August 25, 2003
Date of Patent:
September 5, 2006
Assignee:
Pharmacia & UpJohn Company
Inventors:
Joseph P. Reo, Kathryn M. Kienle, Jennifer K. Fredrickson
Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein Y is —S(?O)n—, —S(?NR8)—, or —S(?NR8)(?O)—; Z is —NHC(?O)R1, —NHC(?S)R1, —NH-het1, —O-het1, —S-het1, or -het2. The compounds of formula I are useful as antibacterial agents.
Type:
Grant
Filed:
February 22, 2005
Date of Patent:
September 5, 2006
Assignee:
Pharmacia and Upjohn Company
Inventors:
Mikhail F. Gordeev, Adam Renslo, Gary W. Luehr, Stuart Lam, Neil E. Westlund, Dinesh Vinoobhai Patel
Abstract: The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
Type:
Application
Filed:
September 10, 2003
Publication date:
August 31, 2006
Applicant:
Pharmacia & Upjohn Company LLC
Inventors:
James Beck, Matthew Drowns, Martha Warpehoski
Abstract: Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: and pharmaceutically acceptable salts thereof wherein R1 and R2 are independently hydrogen, C1-6 alkyl or R1 and R2 are joined to form pyrrolidine, piperidine, morpholine or imidazole. X is OCH3, SO2R3, SO2CF3 or CN where R3 is C1-6 alkyl or an Aryl; and Y is hydrogen, Cl, Br, F, CN, CONR1R2, CF3, OCH3, SO2NR1R2. These new compounds are suitable for treating anxiolytic disorder, schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure or treating migraine headaches in patients in need of such treatment.
Abstract: Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula (I), wherein Ar, W, Z, Q, R1, U, and L, are as herein defined.
Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.
Type:
Application
Filed:
February 7, 2006
Publication date:
June 29, 2006
Applicant:
PHARMACIA & UPJOHN COMPANY
Inventors:
Erik Wong, Saeeduddin Ahmed, Robert Marshall, Robert McArthur, Duncan Taylor
Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
Type:
Grant
Filed:
July 10, 2002
Date of Patent:
June 27, 2006
Assignee:
Pharmacia & Upjohn Company
Inventors:
Heinrich Josef Schostarez, Robert A. Chrusciel
Abstract: The present invention provides novel ion channel polypeptides and polynucleotides that identify and encode them. In addition, the invention provides expression vectors, host cells and methods for their production. The invention also provides methods for the identification of ion channel agonists/antagonists, useful for the treatment of human diseases and conditions.
Type:
Grant
Filed:
July 5, 2001
Date of Patent:
June 27, 2006
Assignee:
Pharmacia & Upjohn Company
Inventors:
Christopher W. Benjamin, Steven L. Roberds, Alla M. Karnovsky, Cara L. Ruble
Abstract: The present invention is macrocycles of the formula (X): for treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme for the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
Type:
Grant
Filed:
June 13, 2002
Date of Patent:
June 27, 2006
Assignee:
Pharmacia & Upjohn Company
Inventors:
Shon R. Pulley, James P. Beck, Ruth E. TenBrink, Jon S. Jacobs
Abstract: Methods and compositions for treating humans suffering from or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.
Type:
Application
Filed:
February 7, 2006
Publication date:
June 22, 2006
Applicant:
PHARMACIA & UPJOHN COMPANY
Inventors:
Erik Wong, Saeeduddin Ahmed, Robert Marshall, Robert McArthur, Duncan Taylor
Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.
Type:
Application
Filed:
February 7, 2006
Publication date:
June 22, 2006
Applicant:
PHARMACIA & UPJOHN COMPANY
Inventors:
Erik Wong, Saeeduddin Ahmed, Robert Marshall, Robert McArthur, Duncan Taylor
Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.
Type:
Application
Filed:
February 7, 2006
Publication date:
June 15, 2006
Applicant:
PHARMACIA & UPJOHN COMPANY
Inventors:
Erik Wong, Saeeduddin Ahmed, Robert Marshall, Robert McArthur, Duncan Taylor
Abstract: The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Type:
Grant
Filed:
December 24, 2003
Date of Patent:
May 30, 2006
Assignees:
Sugen, Inc., Pharmacia & Upjohn Company LLC
Inventors:
Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Peng Cho Tang
Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
Type:
Grant
Filed:
July 10, 2002
Date of Patent:
May 30, 2006
Assignee:
Pharmacia & Upjohn Company
Inventors:
Heinrich Josef Schostarez, Robert Alan Chrusciel