Patents Assigned to Dupont Pharmaceuticals
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Publication number: 20060122169Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-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 ?-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: ApplicationFiled: January 13, 2006Publication date: June 8, 2006Applicant: Dupont PharmaceuticalsInventor: Richard Olson
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Publication number: 20060025407Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-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 ?-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: ApplicationFiled: September 19, 2005Publication date: February 2, 2006Applicant: Dupont PharmaceuticalsInventor: Richard Olson
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Patent number: 6713476Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their 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: April 3, 2001Date of Patent: March 30, 2004Assignee: Dupont Pharmaceuticals CompanyInventors: Michael G Yang, Hong Liu
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Patent number: 6635430Abstract: This invention is directed to filtrate-holder and reversible-well collection plates composed of polypropylene and Teflon®, and to their use, in connection with compatible filter units, in high-throughput screening assays for assessing the binding of small molecules to proteins.Type: GrantFiled: March 31, 2000Date of Patent: October 21, 2003Assignee: DuPont Pharmaceuticals CompanyInventor: Micky D. Tortorella
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Patent number: 6632812Abstract: This invention relates to novel lactams of Formula (I): 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: April 11, 2001Date of Patent: October 14, 2003Assignee: Dupont Pharmaceuticals CompanyInventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
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6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
Patent number: 6559152Abstract: The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: February 27, 2001Date of Patent: May 6, 2003Assignee: DuPont Pharmaceuticals CompanyInventors: Jay A. Markwalder, Steven P. Seitz, Susan R. Sherk -
Patent number: 6544417Abstract: This invention is directed to filtrate-holder and reversible-well collection plates composed of polypropylene and Teflon® resin, and to their use, in connection with compatible filter units, in high-throughput screening assays for assessing the binding of small molecules to proteins.Type: GrantFiled: July 14, 2000Date of Patent: April 8, 2003Assignee: DuPont Pharmaceuticals, Inc.Inventor: Micky Daniel Tortorella
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Patent number: 6531477Abstract: The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: October 12, 1999Date of Patent: March 11, 2003Assignee: DuPont Pharmaceuticals CompanyInventors: Jay A. Markwalder, Steven P. Seitz, Susan R. Sherk
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Patent number: 6451842Abstract: A compound represented by the general formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C1-C6 alkyl addition salt thereof, and their medical applications. These compounds inhibit the action of chemokines such as MIP-1&agr; and/or MCP-1 on target cells, and are useful as therapeutic and/or preventative drugs in diseases, such as atherosclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissues.Type: GrantFiled: May 16, 2000Date of Patent: September 17, 2002Assignees: Dupont Pharmaceuticals Company, Teijin LimitedInventors: Tatsuki Shiota, Ken-ichiro Kataoka, Minoru Imai, Takaharu Tsutsumi, Masaki Sudoh, Ryo Sogawa, Takuya Morita, Takahiko Hada, Yumiko Muroga, Osami Takenouchi, Minoru Furuya, Noriaki Endo, Christine M. Tarby, Wilna Moree, Steven Teig
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Patent number: 6362177Abstract: A compound represented by the general formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C1-C6 alkyl addition salt thereof, and their medical applications. These compounds inhibit the action of chemokines such as MIP-1&agr; and/or MCP-1 on target cells, and are useful as therapeutic and/or preventative drugs in diseases, such as atheroclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissues.Type: GrantFiled: July 16, 2001Date of Patent: March 26, 2002Assignees: Teijin Limited, Dupont Pharmaceuticals Research LaboratoriesInventors: Tatsuki Shiota, Ken-ichiro Kataoka, Minoru Imai, Takaharu Tsutsumi, Masaki Sudoh, Ryo Sogawa, Takuya Morita, Takahiko Hada, Yumiko Muroga, Osami Takenouchi, Minoru Furuya, Noriaki Endo, Christine M. Tarby, Wilna Moree, Steven Teig
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Patent number: 6342503Abstract: The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer'disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R4, R5, Z, Y, V, X, X′, J, K, L, and M are as defined herein.Type: GrantFiled: January 7, 1998Date of Patent: January 29, 2002Assignee: DuPont Pharmaceuticals CompanyInventors: Paul Edward Aldrich, Argyrios Georgios Arvanitis, Robert Scott Cheeseman, Robert John Chorvat, Thomas Eugene Christos, Paul Joseph Gilligan, Dimitri Emil Grigoriadis, Carl Nicholas Hodge, Paul John Krenitsky, Everett Latham Scholfield, Sang William Tam, Zelda Rakowitz Wasserman
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Patent number: 6339099Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D—E represent guanidine mimics, which are useful as inhibitors of factor Xa.Type: GrantFiled: June 18, 1998Date of Patent: January 15, 2002Assignee: DuPont Pharmaceuticals CompanyInventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
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Patent number: 6326368Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.Type: GrantFiled: March 13, 1997Date of Patent: December 4, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Robert John Chorvat, Parthasarathi Rajagopalan
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Patent number: 6322770Abstract: The present invention d ribs novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.Type: GrantFiled: March 30, 1999Date of Patent: November 27, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Milind Rajopadhye, Thomas David Harris
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Patent number: 6319937Abstract: This invention relates to novel isoxazolines of formula (I): or a pharmaceutically acceptable salt form thereof. This invention also relates to novel isoxazolines of formula (I) 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 17, 1999Date of Patent: November 20, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: John Wityak, Prabhakar K. Jadhav
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Patent number: 6313110Abstract: The present invention relates to a compound of Formula (I): or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as inhibitors of HIV 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: June 1, 2000Date of Patent: November 6, 2001Assignee: Dupont Pharmaceuticals CompanyInventor: George V. DeLucca
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Patent number: 6313124Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: January 28, 1998Date of Patent: November 6, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Georgios Arvanitis
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Patent number: 6306886Abstract: The potent platelet glycoprotein IIb/IIIa antagonist, roxifiban, is produced in crystalline form. Crystalline roxifiban exists in two polymorphic forms, designated Form 1 and Form 2. These polymorphic forms are characterized by x-ray powder diffraction and solid-state carbon NMR. Pharmaceutical compositions and methods for the treatment or prevention of diseases mediated by platelet aggregation are described.Type: GrantFiled: June 15, 1998Date of Patent: October 23, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Michael Blaise Maurin, Philip Ma, David John Meloni, Jaan A. Pesti, Lucius Thomas Rossano, Randall K. Ward, Jianguo Yin, Lin Hua Zhang, Goss S. Kauffman
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Patent number: 6307044Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a): or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.Type: GrantFiled: June 10, 1999Date of Patent: October 23, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Roberta L. Dorow, Silvio Campagna, Pasquale N. Confalone, Fuqiang Jin, Zhe Wang
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Patent number: RE37781Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.Type: GrantFiled: March 10, 1999Date of Patent: July 2, 2002Assignee: DuPont Pharmaceuticals CompanyInventors: Patrick Y. Lam, Prabhakar K. Jadhav, Charles J. Eyermann, Carl N. Hodge, George V. De Lucca, James D. Rodgers