Abstract: The present invention relates to methods and compositions for the identification of species-specific material in pharmaceutical products. In particular, the present invention relates to methods for the identification of species-specific DNA in a population of a different species or following contact (e.g., growth) with cells of a different species.
Abstract: The invention provides isolated AGS nucleic acid molecules, recombinant expression vectors containing a nucleic acid molecule of the invention, including AGS specific promoters, host cells into which the expression vectors have been introduced, and a process of transcribing or expressing a heterologous sequence by culturing the host cells under appropriate conditions.
Abstract: The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and to methods of treating hyperproliferative disorders, such as cancer, by administering N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.
Type:
Application
Filed:
November 17, 2003
Publication date:
May 27, 2004
Applicant:
OSI Pharmaceuticals, Inc.
Inventors:
Douglas John Meldrum Allen, Timothy Norris, Jeffrey William Raggon, Dinos Paul Santafianos, Ravi Mysore Shanker
Abstract: Liposomal encapsulated camptothecin formulations are provided. The liposomes have improved pharmacokinetics, enhanced efficacy as anti-tumor agents and provide an increased therapeutic index as compared to the free drug and topotecan. The formulations include liposomes comprising at least one phospholipid and a camptothecin or analog thereof.
Type:
Grant
Filed:
February 24, 2000
Date of Patent:
May 25, 2004
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Karen Lewis Moynihan, David Lloyd Emerson, Su-Ming Chiang, Ning Hu
Abstract: A screening assay in yeast is disclosed wherein G-protein coupled-receptor independent activators and inhibitors of the pheromone pathway can be identified using a mammalian cDNA library. Novel Activator of G protein Signaling (“AGS”) proteins, which are Ras-related proteins that stimulate G protein activity in a receptor-independent manner, are disclosed, as well as nucleic acid molecules encoding AGS proteins. In addition to isolated AGS proteins, the invention further provides isolated AGS fusion proteins, antigenic peptides and anti-AGS antibodies. The invention also provides isolated AGS nucleic acid molecules, recombinant expression vectors containing a nucleic acid molecule of the invention, host cells into which the expression vectors have been introduced and non-human transgenic animals in which an AGS gene has been introduced or disrupted. Diagnostic, screening and therapeutic methods utilizing compositions of the invention are also provided.
Abstract: This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
Type:
Application
Filed:
November 20, 2003
Publication date:
April 29, 2004
Applicant:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
Type:
Application
Filed:
November 20, 2003
Publication date:
April 29, 2004
Applicant:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: The present invention relates to compositions and methods for treating the epithelial toxicity caused by administering to a human cancer patient an epidermal growth factor receptor (EGFR) inhibitor. The pharmaceutical composition preferably comprises an EGFR inhibitor and a keratinocyte growth factor (KGF) in a pharmaceutically-acceptable carrier. The method of treatment comprises co-administering to the patient a therapeutically effective amount of KGF with the EGFR inhibitor.
Type:
Application
Filed:
June 10, 2003
Publication date:
April 15, 2004
Applicants:
PFIZER PRODUCTS INC., OSI PHARMACEUTICALS, INC.
Inventors:
Penelope Elizabeth Miller, James Dale Moyer
Abstract: The present invention relates to a process for preparing camptothecin and camptothecin analogs of Formula (I) from compounds of Formula (II) and to novel intermediates useful in their preparation,
wherein R1 to R6 represent various substituents.
Abstract: Liposomal encapsulated benzoquinazoline thymidylate synthase inhibitor formulations are provided. The liposomes have improved pharmacokinetics and enhanced efficacy as anti-tumor agents compared to the free drug. The formulations include liposomes comprising at least one phosphatidylcholine, a cholesterol, and a benzoquinazoline thymidylate synthase inhibitor.
Type:
Application
Filed:
July 1, 2003
Publication date:
March 25, 2004
Applicant:
OSI Pharmaceuticals, Inc.
Inventors:
Claudine S. Ashvar, Su-Ming Chiang, David L. Emerson, Ning Hu, Gerard M. Jensen
Abstract: The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and to methods of treating hyperproliferative disorders, such as cancer, by administering N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.
Type:
Grant
Filed:
July 29, 1999
Date of Patent:
March 16, 2004
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Douglas John Meldrum Allen, Timothy Norris, Jeffrey William Raggon, Dinos Paul Santafianos, Ravi Mysore Shanker
Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of inflammatory bowel disease.
Abstract: Liposomal encapsulated benzoquinazoline thymidylate synthase inhibitor formulations are provided. The liposomes have improved pharmacokinetics and enhanced efficacy as anti-tumor agents compared to the free drug. The formulations include liposomes comprising at least one phosphatidylcholine, a cholesterol, and a benzoquinazoline thymidylate synthase inhibitor.
Type:
Grant
Filed:
June 6, 2001
Date of Patent:
February 10, 2004
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Claudine S. Ashvar, Su-Ming Chiang, David L. Emerson, Ning Hu, Gerard M. Jensen
Abstract: This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
Type:
Grant
Filed:
December 2, 1999
Date of Patent:
February 3, 2004
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
Type:
Grant
Filed:
December 1, 2000
Date of Patent:
January 20, 2004
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
Type:
Grant
Filed:
November 30, 2001
Date of Patent:
January 20, 2004
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: The subject invention provides a compound having the structure:
or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A3 adenosine receptor by administering a therapeutically effective amount of the compound.
Type:
Grant
Filed:
November 30, 2001
Date of Patent:
January 6, 2004
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: This invention pertains to compounds having the structure:
wherein NR1R2 is a substituted or unsubstituted 4-8 membered ring; wherein R3 is a substituted or unsubstituted four to six membered ring; wherein R5 is H, alkyl, substituted alkyl, aryl, arylalkyl, amino, substituted aryl; wherein R6 is H, alkyl, substituted alkyl, or cycloalkyl; with the proviso that NR1R2 is not 3-acetamido piperadino, 3-hydroxy pyrrolidino, 3-methyloxy carbonylmethyl pyrolidino, or 3-aminocarbonylmethyl pyrrolidino; with the proviso that NR1R2 is 3-hydroxymethyl piperadino only when R3 is 4-pyridyl; which specifically inhibit the adenosine A2a receptor and the use of these compounds to treat a disease associated with A2a adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
Type:
Grant
Filed:
December 1, 2000
Date of Patent:
December 16, 2003
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo L. Castelhano, Bryan McKibben, David J. Witter
Abstract: The present invention relates to a method for the preparation for camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I′) known by the chemical name “7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin”, which comprises cyclising the compound of formula (II′), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I′) is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer; and/or if desired, converting the resulting compound of formula (I′) or a salt thereof into a physiologically acceptable salt or solvate thereof.
Type:
Application
Filed:
March 24, 2003
Publication date:
October 30, 2003
Applicant:
OSI Pharmaceuticals, Inc.
Inventors:
Francis Gerard Fang, Edward McDonald Huie, Shiping Xie, Daniel L. Comins
Abstract: Spirolactam compounds useful as inhibitors of protein-protein interactions modulated by SH3 domains are disclosed. Compounds of the invention are also useful as &bgr;-turn mimetics. Also disclosed are libraries of compounds of the invention, pharmaceutical compositions of the compounds of the invention, and methods for using the compounds of the invention to inhibit growth of a cell or to inhibit protein-protein interactions modulated by SH3 domains.