Patents Represented by Attorney, Agent or Law Firm Scott K. Larsen
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Patent number: 7018999Abstract: Novel methods for the treatment and/or prevention of pain are presented. The methods may comprise administering to a subject in need thereof an effective amount of a stress-activated protein kinase inhibitor. Preferred compounds for use in the methods include fused pyrrolocarbazole compounds.Type: GrantFiled: May 15, 2002Date of Patent: March 28, 2006Assignee: Cephalon, Inc.Inventors: Lisa D. Aimone, Robert L. Hudkins, Matthew S. Miller
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Patent number: 6831075Abstract: The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.Type: GrantFiled: August 22, 2002Date of Patent: December 14, 2004Assignee: Cephalon, Inc.Inventors: Jasbir Singh, Rabindranath Tripathy
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Patent number: 6825208Abstract: This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; pharmaceutical compositions containing the same; and methods of using the same as anticoagulant agents for modulation of the coagulation cascade.Type: GrantFiled: August 20, 2002Date of Patent: November 30, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jinglan Zhou, Leslie Robinson, Nikolaus M. Gubernator, Eddine Saiah, Xu Bai, Xin Gu
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Patent number: 6774212Abstract: The present invention relates to ketoamide and ketoester compounds of Formula (I): wherein W is —NH— or —O—, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: December 1, 2000Date of Patent: August 10, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Wei Han
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Patent number: 6699855Abstract: The present invention relates to compounds of Formula (I): wherein A1 is methylene, ethylene or propylene group and A2 is N or CR5, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: February 28, 2001Date of Patent: March 2, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Zhang, Wei Han
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Patent number: 6653295Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): that are useful as serine protease inhibitors, and more particularly as Hepatitis C virus NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.Type: GrantFiled: December 12, 2001Date of Patent: November 25, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Peter William Glunz, Brent Dale Douty, Wei Han
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Patent number: 6635669Abstract: The present invention is directed to novel fused pyrrolocarbazoles and isoindolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.Type: GrantFiled: February 1, 2002Date of Patent: October 21, 2003Assignee: Cephalon, Inc.Inventor: Robert L. Hudkins
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Patent number: 6552017Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: June 15, 2000Date of Patent: April 22, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. Mc Clung, Emilie J. B. Calvello, David M. Zawrotny
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Patent number: 6548493Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: June 15, 2000Date of Patent: April 15, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Wenting Chen, Christopher D. McClung, Emilie J. B. Calvello, David M. Zawrotny
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Patent number: 6525044Abstract: This invention relates to novel carbocycles and heterocycles having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: February 16, 2001Date of Patent: February 25, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Richard E Olson, Thomas P Maduskuie, Lorin Andrew Thompson, Andrew J Tebben, Nenghui Wang, Wei Deng, Hong Liu
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Patent number: 6489333Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: April 9, 2001Date of Patent: December 3, 2002Assignee: Bristol - Meyers Squibb Pharma CompanyInventors: William J. Pitts, Prabhakar K. Jadhav
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Patent number: 6486173Abstract: The present invention relates to compounds having pharmacological activity toward the 5-HT7 receptor. Pharmaceutical compositions and methods for their use in the treatment of CNS disorders are described.Type: GrantFiled: March 7, 2001Date of Patent: November 26, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Gary Avonn Cain, John Francis McElroy
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Patent number: 6476226Abstract: This invention relates to novel isoxazolines and isoxazoles of formula (I): or a pharmaceutically acceptable salt or prodrug form thereof. The invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: July 13, 2001Date of Patent: November 5, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Joanne M. Smallheer, Shuaige Wang, Prabhakar Kondaji Jadhav
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Patent number: 6452000Abstract: The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric cyclic ureas. In the process, a diamine of formula (I-a) is selectively monoacylated to give an asymmetric monoacylated diamine which can be converted into asymmetric intermediates. The asymmetric intermediates can be further alkylated, cyclized, and/or modified to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection. The invention allows for scalable preparation of a wide variety of asymmetrical cyclic ureas.Type: GrantFiled: March 7, 2001Date of Patent: September 17, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Benjamin R. P. Stone, Luigi Anzalone, Joseph M. Fortunak, Gregory D. Harris, Ioannis I. Valvis, Robert E. Waltermire
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Patent number: 6358976Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the &agr;v&bgr;3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: February 22, 2000Date of Patent: March 19, 2002Inventors: John Wityak, Aleksandra Ewa Tobin
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Patent number: 6303609Abstract: This invention relates to novel isoxazolines and isoxazoles of formula (I): or a pharmaceutically acceptable salt or prodrug form thereof. The invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 18, 1999Date of Patent: October 16, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Joanne M. Smallheer, Shuaige Wang, Prabhakar Kondaji Jadhav
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Patent number: 6159980Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I) ##STR1## and their use in treating psychiatric disorders and neurological diseases including major depression, anxiety-related disorders, post-traumatic stress disorders, supranuclear palsy and eating disorders.Type: GrantFiled: September 15, 1997Date of Patent: December 12, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Argyrios Georgios Arvanitis, Richard E. Olson, Charles R. Arnold, III, William E. Frietze
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Patent number: 6147210Abstract: The present invention describes novel methods for the synthesis of benzoxazinone compounds which are useful as human immunodeficiency virus (HIV) reverse transcriptase inhibitors. The benzoxazinone of the formula: is particularly effective in the treatment of HIV.Type: GrantFiled: June 25, 1999Date of Patent: November 14, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Michael Ernest Pierce, Lilian Alicia Radesca
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Patent number: 6049019Abstract: The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In the process, cyclopropane carboxaldehyde is condensed with malonic acid to form 3-cyclopropylacrylic acid; 3-cyclopropylacrylic acid is halogenated to form (E,Z)-1-halo-2-cyclopropylethylene; and (E,Z)-1-halo-2-cyclopropylethylene is dehydrohalogenated to form cyclopropyl acetylene. This improvement provides for high conversion of inexpensive, readily available starting materials into cyclopropylacetylene, high overall yields and can be conducted on an industrial scale.Type: GrantFiled: July 30, 1998Date of Patent: April 11, 2000Assignee: DuPont PharmaceuticalsInventors: Joseph M. Fortunak, Zhe Wang, Jianguo Yin
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Patent number: 5998614Abstract: The present invention describes a method for the preparation of asymmetric N,N'-disubstituted cyclic ureas through the selective monodebenzylation of symmetric N,N'-disubstituted cyclic ureas using a dissolving metal reduction. The intermediates can be alkylated to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection.Type: GrantFiled: July 6, 1998Date of Patent: December 7, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Thomas E Smyser, Pasquale N. Confalone