Abstract: This invention provides ethers of 7-desmethylrapamycin which are useful in inducing immunosuppression and in the treatment of transplantation rejection, autoimmune diseases, solid tumors, fungal infections, and vascular disease.
Abstract: This invention provides 1-oxorapamycins, which are useful in inducing immunosuppression, as a neurotrophic agent, and in the treatment of transplantation rejection, autoimmune diseases, solid tumors, fungal infections, and vascular disease.
Abstract: This invention provides a method of providing contraception which comprises administering to a female of child bearing age a combination of a non-uterotrophic anti-estrogen and a progestin for 28 days per 28-day menstrual cycle.
Abstract: Compounds of the Formulae (I) and (II):
wherein R1, R2, R3, X, Y and Z are as defined in the specification which compounds are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel modulation.
Type:
Grant
Filed:
June 25, 2001
Date of Patent:
May 21, 2002
Assignee:
American Home Products Corporation
Inventors:
Schuyler A. Antane, John A. Butera, Joseph R. Lennox
Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure:
wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.
Type:
Grant
Filed:
April 19, 2000
Date of Patent:
May 21, 2002
Assignees:
American Home Products Corporation, Ligand Pharmaceuticals, Inc.
Inventors:
Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
Abstract: This invention provides substituted compounds of the general formulae:
wherein B and E are C or N; D, G and W are O, S, or N; or salt forms thereof, and methods and pharmaceutical compositions for their use in treating disorders related to insulin resistance or hyperglycemia.
Type:
Grant
Filed:
March 2, 2001
Date of Patent:
May 21, 2002
Assignee:
American Home Products Corporation
Inventors:
Michael S. Malamas, Robert E. McDevitt, Folake O. Adebayo
Abstract: Novel proteins which bind human &bgr;-amyloid peptide, polynucleotides which encode these proteins, and methods for producing these proteins are provided. Diagnostic, therapeutic, and screening methods employing the polynucleotides and polypeptides of the present invention are also provided. Transgenic animals and knockout animals are also provided.
Type:
Application
Filed:
May 9, 2001
Publication date:
May 16, 2002
Applicant:
American Home Products Corporation
Inventors:
Bradley A. Ozenberger, Jonathan A. Bard, Eileen M. Kajkowski, Jack S. Jacobsen, Stephen G. Walker, Heidi Sofia, David Howland
Abstract: The present invention provides processes for the preparation of 1, 2, 3, 4, 8, 9, 10, 10a-octahydro-7bH-cyclopenta[b][1, 4]diazepino[6, 7, 1-hi]indole derivatives of the general formula: 1
Abstract: This invention provide pegylated hydroxyesters of rapamycin which are useful in inducing immunosuppression and in the treatment of transplantation rejection, autoimmune diseases, solid tumors, fungal infections, and vascular disease.
Abstract: This invention provides a process for preparing compounds of formula 1:
wherein:
X is phenyl optionally substituted with one or more substituents selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, amino, and alkanoylamino of 1-6 carbon atoms;
R and R1 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, or trifluoromethyl;
R2 is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, trifluoromethyl;
R3 is independently hydrogen, alkyl of 1-6 carbon atoms, carboxy, carboalkoxy of 1-6 carbon atoms, phenyl, or carboalkyl of 2-7 carbon atoms;
n=2-4;
or a pharmaceutically acceptable salt thereof, with the proviso that each R3 of Y may be the same or different.
Abstract: The present invention relates to novel substituted pyridine compounds of Formula (I)
wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.
Type:
Grant
Filed:
November 1, 2000
Date of Patent:
May 7, 2002
Assignee:
American Home Products Corporation
Inventors:
Chingfan Chiu, Zhilian Tang, John W. Ellingboe
Abstract: The present invention relates to novel substituted pyridine compounds of Formula (I)
wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.
Type:
Grant
Filed:
November 1, 2000
Date of Patent:
May 7, 2002
Assignee:
American Home Products Corporation
Inventors:
Chingfan Chiu, Zhilian Tang, John W. Ellingboe
Abstract: Composition comprising lamellar vesicles that comprise a local anesthetic and a nucleic acid molecule are disclosed. Methods of making such compositions are disclosed. Method of delivering proteins to cells of individuals are disclosed. Methods of inducing immune responses in individuals are disclosed. Methods of delivering nucleic acid molecules to cells of individuals are disclosed.
Type:
Grant
Filed:
April 4, 2000
Date of Patent:
May 7, 2002
Assignee:
American Home Products Corporation
Inventors:
Richard B. Ciccarelli, C. Satishchandran, Catherine J. Pachuk
Abstract: The present invention relates to novel substituted pyridine compounds of Formula (I)
wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.
Type:
Grant
Filed:
November 1, 2000
Date of Patent:
May 7, 2002
Assignee:
American Home Products Corporation
Inventors:
Chingfan Chiu, Zhilian Tang, John W. Ellingboe
Abstract: This invention provides tissue selective estrogens of formula I having the structure
wherein:
R1 and R2 are independently, hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, benzoyl,
X is hydrogen, alkyl of 1-6 carbon atoms, CN, halogen, trifluoromethyl, or thioalkyl of 1-6 carbon atoms;
n=1-3;
with the proviso that at least one of R1 or R2 are not hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, or benzoyl;
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
September 11, 2000
Date of Patent:
April 30, 2002
Assignee:
American Home Products Corporation
Inventors:
Chris P. Miller, Michael D. Collini, Bach D. Tran, Anita Wai-Yin Chan, Arkadiy Z. Rubezhov