Chalcogen Or Nitrogen Bonded Indirectly To The Imidazole Ring By Nonionic Bonding Patents (Class 514/399)
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Patent number: 6989399Abstract: A series of N-alkanol-N-phenyl benzenesulfonamide and related derivatives of the Formula I are disclosed, wherein R1, R2, R3, X, and Y are defined herein. The compounds are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions characterized by aberrant extracellular deposition of amyloid. Pharmaceutical compositions and methods of treatment are also disclosed.Type: GrantFiled: July 24, 2003Date of Patent: January 24, 2006Assignee: Bristol-Myers Squibb CompanyInventors: David W. Smith, Michael F. Parker
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Patent number: 6989402Abstract: New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR?R?) or an acylsulphonamide (CONHSO2R?) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR?R?). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H).Type: GrantFiled: December 23, 1999Date of Patent: January 24, 2006Assignee: Karo Bio ABInventors: Jon Hangeland, Minsheng Zhang, Yolanda Caringal, Denis Ryono, Yi-Lin Li, Johan Malm, Ye Liu, Neeraj Garg, Chris Litten, Ana Maria Garcia Collazo, Konrad Koehler
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Patent number: 6979696Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein m, A, X, Y, R1, R2, R3, R4 and R5 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: May 7, 2004Date of Patent: December 27, 2005Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Clara Jeou Jen Lin, Amy Geraldine Moore, Counde O'Yang, Yansheng Zhai
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Patent number: 6969512Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.Type: GrantFiled: October 10, 2002Date of Patent: November 29, 2005Assignee: The University of Florida Research Foundation, Inc.Inventors: Philip Frederick Brode, III, Garry Steven Garrett, Leo Timothy Laughlin, Randall Stryker Matthews
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Patent number: 6960600Abstract: The invention concerns novel azole or triazole derivatives of formula (I), wherein: X, Ar1, Ar3, A, R1, R5, R6, R7 and B are such as defined in the description, their preparation method and their use as antifungal medicines.Type: GrantFiled: May 2, 2002Date of Patent: November 1, 2005Assignee: Aventis Pharma S.A.Inventors: Didier Babin, John Bernard Weston
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Patent number: 6949578Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.Type: GrantFiled: July 14, 2004Date of Patent: September 27, 2005Assignee: Pharmacia CorporationInventors: Ish Kumar Khanna, Michael Clare, Alan F. Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu
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Patent number: 6946460Abstract: The invention concerns novel azole or triazole derivatives of formula (I), wherein X, Ar1, Ar2, Ar3, A, B, and R1 are as defined herein, their preparation method and their use as fungicides.Type: GrantFiled: May 2, 2002Date of Patent: September 20, 2005Assignee: Aventis Pharma S.A.Inventors: Didier Babin, John Bernard Weston
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Patent number: 6943183Abstract: The present invention provides novel 5-substituted tetralones of Formulas I, II, III, and IV and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis.Type: GrantFiled: April 16, 2001Date of Patent: September 13, 2005Assignee: Pfizer IncInventors: William Alexander Denny, Richard H. Hutchings, Douglas S. Johnson, James Stanley Kaltenbronn, Ho Huat Lee, Daniele Marie Leonard, Jared Bruce John Milbank, Joseph Thomas Repine, Gordon William Rewcastle, Andrew David White
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Patent number: 6927227Abstract: aP2 inhibiting compounds are provided having the formula wherein R1, R2, R3, R4, X—Z and are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.Type: GrantFiled: December 17, 2002Date of Patent: August 9, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, David R. Magnin
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Patent number: 6927232Abstract: This invention relates to the treatment of mGluR5 receptor mediated disorders, which comprises administering to a person in need of treatment a compound having the formula wherein R1, R2, R3, R4 and R5 are as defined in the description, A signifies —CH?CH— or —C?C—; and B signifies wherein R6 to R26, X and Y are as defined herein.Type: GrantFiled: April 4, 2003Date of Patent: August 9, 2005Assignee: Hoffman-La Roche Inc.Inventors: Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
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Patent number: 6916813Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, are useful for modulating mitochondrial F1F0 ATPase activity and treating ischemic conditions including myocardial infarction, congestive heart failure, and cardiac arrhythmias.Type: GrantFiled: December 10, 2002Date of Patent: July 12, 2005Assignee: Bristol-Myers Squibb Co.Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrnce G. Hamann, David Green, Francis N. Ferrara
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Patent number: 6916837Abstract: Amidino derivatives represented by the following general formula (I): {where X is a group represented by R1SO2NR2— (wherein R1 represents optionally substituted C6-14 aryl, etc. and R2 represents hydrogen atom, etc.), etc., Ar1 represents 2,6-naphthylene, etc., R3 represents hydrogen atom, etc. and Y represents carboxyphenyl, etc.} and their pharmacologically acceptable salts or solvates.Type: GrantFiled: November 14, 2002Date of Patent: July 12, 2005Assignee: Eisai Co., Ltd.Inventors: Takashi Satoh, Yasushi Okamoto, Osamu Asano, Nobuhisa Watanabe, Tadashi Nagakura, Takao Saeki, Atsushi Inoue, Masahiro Sakurai
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Patent number: 6906053Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: May 12, 2004Date of Patent: June 14, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
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Patent number: 6906075Abstract: Melanin concentrating hormone receptor ligands (especially substituted benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: January 9, 2003Date of Patent: June 14, 2005Assignee: Neurogen Corp.Inventors: Robert W. DeSimone, Cheryl Steenstra, Linda Gustavson, Rajagopal Bakthavatchalam, Alan Hutchison
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Patent number: 6890915Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: May 23, 2002Date of Patent: May 10, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
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Patent number: 6884821Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.Type: GrantFiled: September 29, 2000Date of Patent: April 26, 2005Assignee: Eisai Co., Ltd.Inventors: Masanobu Shinoda, Eita Emori, Fumiyoshi Matsuura, Toshihiko Kaneko, Norihito Ohi, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Sadakazu Miyashita, Taro Hibara, Takashi Seiki, Richard Clark, Hitoshi Harada
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Patent number: 6884809Abstract: The invention provides a method for reducing cardiac dysfunctions in a human. The method comprises administration to the human of an effective amount of a selective histamine H3 Receptor agonist. In one embodiment, the method comprises limiting the accumulation of intracellular sodium (Nai) by inhibiting the Na+/H+ exchanger activity in the human having a cardiac dysfunction, or a predisposition to a cardiac dysfunction. In another embodiment the method comprises inhibiting the N-type Ca2+ channel to modulate the concentration of intracellular calcium. The invention also provides a pharmaceutical composition that includes a selective histamine H3 Receptor agonist with a pharmaceutical carrier.Type: GrantFiled: February 13, 2002Date of Patent: April 26, 2005Assignee: Cornell Research Foundation, Inc.Inventors: Roberto Levi, Randi B. Silver
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Patent number: 6884801Abstract: Compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed. Such compounds are useful in the treatment of Alpha-1A mediated diseases or conditions such as urinary incontinence.Type: GrantFiled: April 28, 2000Date of Patent: April 26, 2005Assignee: SmithKline Beecham CorporationInventors: Eric Cleveland Bigham, Michael Joseph Bishop, David Harold Drewry, Deanna Trojan Garrison, Stephen Joseph Hodson, Frank Navas, III, Jason D. Speake
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Patent number: 6872741Abstract: The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).Type: GrantFiled: September 11, 2003Date of Patent: March 29, 2005Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul R. Fatheree, David C. Green, Daniel Marquess
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Patent number: 6867229Abstract: Composition which is useful in particular for the treatment and protection of domestic animals which are infested with parasites or are likely to be infested with them, these compositions comprising, in the form of a ready-to-use solution: a) an insecticidal active substance of formula (I), b) a crystallization inhibitor, c) an organic solvent having a dielectric constant of between 10 and 35, preferably of between 20 and 30, d) an organic co-solvent having a boiling point below 100° C., preferably below 80° C., and a dielectric constant of between 10 and 40, preferably of between 20 and 30.Type: GrantFiled: April 8, 2002Date of Patent: March 15, 2005Assignee: MerialInventor: Jean Pierre Etchegaray
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Patent number: 6863906Abstract: This invention provides therapeutic compositions and combinations for the protection, treatment and repair of liver tissue. The invention relates to novel compositions and combinations comprising two or more compounds selected from the group consisting of S-adenosylmethionine, L-ergothioneine, and a substance selected from the group consisting of constituents of Milk thistle (Silybum marianum), silymarin and active components of silymarin, whether naturally, synthetically, or semi-synthetically derived, and to methods of preventing and treating liver disease and of repairing damaged liver tissue. The invention also provides a method of administering these compositions and combinations to humans or animals in need thereof.Type: GrantFiled: May 24, 2002Date of Patent: March 8, 2005Assignee: Nutramax Laboratories, Inc.Inventors: Todd R. Henderson, Barbara E. Corson
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Patent number: 6849634Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: December 7, 2001Date of Patent: February 1, 2005Assignee: ICAgenInventors: Serge Beaudoin, Aimee D. Reed, Michael F. Gross
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Patent number: 6846837Abstract: Methods and topical pharmaceutical formulations are provided for the treatment of nail fungus (onychomycosis). The invention involves a pharmacologically active antifungal agent, plus a pharmaceutically acceptable base in a formulation having a pH of 7.5 to about 13.0, preferably about 8.0 to 11.5, and most preferably about 8.5 to 10.5. These basic formulations permeate the nail and are effective in treating fungal infections of the nail and surrounding tissues.Type: GrantFiled: June 21, 2002Date of Patent: January 25, 2005Inventors: Howard I. Maibach, Eric C. Luo, Tsung-Min Hsu
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Patent number: 6838476Abstract: Compounds of formula I wherein: one of X or Y represents N and the other represents C; R1 represents hydrogen, methyl, halogen, cyano, nitro, —CHO, —COCH3 or —COOR4; PR2 represents optionally-substituted aryl or heteroaryl; R3 represents C1-8 alkyl, C1-8 haloalkyl or —NR4R6; R4 represents hydrogen, C1-8 alkyl or arylC0-8 alkyl; R6 represents hydrogen, C1-8 alkyl, arylC1-8 alkyl, —COR8 or —COOR8; R8 represents C1-8 alkyl or C1-8 haloalkyl; aryl in the above definitions represents phenyl or naphthyl; and heteroaryl in the above definitions represents pyridine, pyrazine, pyrimidine or pyridazine, which can be optionally fused to a benzene ring. These compounds are useful as cyclooxygenase-2 inhibitors.Type: GrantFiled: October 15, 1999Date of Patent: January 4, 2005Assignee: J. Uriach & Cia, SAInventors: Carmen Almansa, Concepción Gonzalez, Ma Carmen Torres
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Patent number: 6833381Abstract: TNF-&agr; inhibitors containing a heterocyclic compound having angiotensin II antagonistic activity which are useful as preventives/remedies for inflammatory diseases, etc.Type: GrantFiled: August 14, 2002Date of Patent: December 21, 2004Assignee: Takeda Chemical Industries, Ltd.Inventors: Kazuaki Ikeya, Takahito Kitayoshi
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Patent number: 6821965Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno(1-6C)alkyl, hydroxy-(1-6C)alkyl, di-[(1-6C)alklyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino-2(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseaseType: GrantFiled: February 2, 2001Date of Patent: November 23, 2004Assignee: AsterZeneca ABInventors: Dearg S Brown, George R Brown
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Patent number: 6821997Abstract: A method for the treatment and prophylaxis of conditions of aging in humans, such conditions of aging associated with a decreased presence of cell-specific carbonic anhydrase enzymes in the brain, such as conditions associated with chronic neurodegenerative conditions including dementia such as Alzheimer's disease, which method includes the administering over an extended period of time, ranging from 6 months to 5 years, of a pharmaceutically effective, non-toxic amount of a compound that increases the presence of cell-specific carbonic anhydrase enzymes in the brain. That compound may be the cell-specific carbonic anhydrase enzyme, a compound that when absorbed by the body reacts or dissociates to form the cell-specific carbonic anhydrase enzyme, or a compound that promotes the natural generation of the cell-specific carbonic anhydrase enzyme within the body.Type: GrantFiled: February 15, 2002Date of Patent: November 23, 2004Inventor: Victorio C. Rodriguez
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Patent number: 6803367Abstract: A substance for inducing apoptosis represented by specific formulae. A pharmaceutical composition which can be used for an anticancer agent containing said substance.Type: GrantFiled: October 1, 2002Date of Patent: October 12, 2004Assignee: Takara Shuzo Co., Ltd.Inventors: Tatsuji Enoki, Nobuto Koyama, Katsushige Ikai, Ikunoshin Kato
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Patent number: 6797725Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: April 9, 2002Date of Patent: September 28, 2004Assignee: Sugen, Inc.Inventors: Connie Li Sun, Chung Chen Wei, Peng Cho Tang, Marcel Koenig, Yong Zhou, Tomas Vojkovsky, Asaad S. Nematalla
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Patent number: 6784183Abstract: Compounds of formula (I): and medicinal products containing the same which are useful as dual &agr;2/5-HT2c antagonists.Type: GrantFiled: June 29, 2001Date of Patent: August 31, 2004Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
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Publication number: 20040167129Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: December 22, 2003Publication date: August 26, 2004Inventors: Alexander Mayweg, Hans Peter Marty, Werner Mueller, Robert Narquizian, Werner Neidhart, Philippe Pflieger, Stephan Roever
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Publication number: 20040152745Abstract: The present invention provides the inhibitors of dipeptidyl peptidase IV based upon or including proline or similar moieties. The inhibitors are useful for treating various disorders, including those of the central nervous system and the prostate. Many of the inhibitors can be reversible, and can cross the blood-brain barrier. Methods of making and using the inhibitors and treatment methods also are provided.Type: ApplicationFiled: November 25, 2003Publication date: August 5, 2004Applicant: Guilford Pharmaceuticals, Inc.Inventors: Paul Jackson, Joseph Steiner
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Patent number: 6770306Abstract: The present invention relates to a pharmaceutical composition for reducing vaginal acidity, treating abnormal enhancement of vaginal acidity, and high acidity vaginitis associated with abnormal enhancement of vaginal acidity, especially for the treatment of fungal vaginitis, comprising of one or more ingredients defined as follows: amino acids, physiologically acceptable salts of amino acids, oligopeptides and polypeptides. Also, the present invention relates to the use of the said amino acids, physiologically acceptable salts of amino acids, oligopeptides and polypeptides, as active ingredients or auxiliaries in preparing drugs for reducing vaginal acidity, the treatment of abnormal enhancement of vaginal acidity, and high acidity vaginitis especially to their use in preparing drugs for the treatment of fungal vaginitis and the use thereof as nutrients for vaginal mucous membranes in preparing drugs that are locally applied in the vagina.Type: GrantFiled: January 3, 2001Date of Patent: August 3, 2004Inventor: Zhongming Zeng
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Patent number: 6770667Abstract: The present invention is a compound and pharmaceutical composition comprising a compound of formula (I): wherein R1 is a 4-(lower) alkyl-imidazol-1-yl or a 4,5-di(lower) alkyl-imidazol-1-yl group, R2 is a hydrogen atom or a lower alkyl group, and R3 is a fluorenyl group. The compound of formula (I) includes pharmaceutically acceptable salts: The compound of formula (I) and salts thereof have 5-HT antagonism activity.Type: GrantFiled: March 21, 2002Date of Patent: August 3, 2004Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyotaka Ito, Glen W. Spears, Fumie Takahashi, Akira Yamada, Masaki Tomishima, Hiroshi Miyake
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Publication number: 20040142930Abstract: 1.Type: ApplicationFiled: November 4, 2003Publication date: July 22, 2004Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
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Publication number: 20040142989Abstract: The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases.Type: ApplicationFiled: June 30, 2003Publication date: July 22, 2004Inventors: Barry Craig Finzel, Lee A. Funk, Robert Charles Kelly, Matthew T. Reding, Nancy Anne Wicnienski
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Publication number: 20040138244Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: ApplicationFiled: October 14, 2003Publication date: July 15, 2004Inventors: James T. Dalton, Duane D. Miller
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Patent number: 6759387Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length (SEQ ID NO:50).Type: GrantFiled: July 30, 2002Date of Patent: July 6, 2004Assignee: Cellgate, Inc.Inventors: Jonathan B. Rothbard, Paul A. Wender, P. Leo McGrane, Lalitha V. S. Sista, Thorsten A. Kirschberg
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Publication number: 20040110804Abstract: The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds.Type: ApplicationFiled: July 9, 2003Publication date: June 10, 2004Inventors: Michael A. Walker, Zhuping Ma, B. Narasimhulu Naidu, Margaret E. Sorenson, Annapurna Pendri, Jacques Banville, Serge Plamondon, Roger Remillard
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Patent number: 6740659Abstract: The invention relates to the use of compounds which inhibit selectively mu opioid receptor activity, or activation, for the treatment of dyskinesia (which, for example, may arise as a side effect of L-DOPA therapy). The compounds used are preferably mu opioid receptor antagonists such as cyprodime.Type: GrantFiled: August 2, 2002Date of Patent: May 25, 2004Assignee: Motac Neuroscience LimitedInventor: Jonathan Brotchie
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Publication number: 20040097571Abstract: Imidazole compounds having adenosine deaminase inhibitory activity represented by the formula (I) wherein R1 is aryloxy, or aryl which is optionally substituted with suitable substituent(s); R2 is lower alkyl; R3 is hydroxy or protected hydroxy; and -A- is lower alkylene, its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.Type: ApplicationFiled: October 22, 2002Publication date: May 20, 2004Inventors: Kiyoshi Tsuji, Tadashi Terasaka, Katsuya Nakamura
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Patent number: 6737434Abstract: Imidazole derivatives of the formula (1) or salts thereof, pharmaceuticals containing the derivatives or the salts, and intermediates for the synthesis of the derivatives or the salts (wherein R1 is lower alkyl; R2 is alkyl or aralkyl; and X1 is halogeno). These compounds exhibit G-CSF-like activities and can be substituted for G-CSF preparations.Type: GrantFiled: March 19, 2003Date of Patent: May 18, 2004Assignee: SSP Co., Ltd.Inventors: Minoru Tokizawa, Sunao Takeda, Yasushi Kaneko, Koji Kusano, Hiromichi Eto, Koichi Tachibana, Susumu Sato, Tadayoshi Taniyama
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Patent number: 6737418Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: April 30, 2002Date of Patent: May 18, 2004Assignee: Euro-Celtique S.A.Inventors: Derk Hogenkamp, Ravindra Upasani, Phong Nguyen
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Patent number: 6734202Abstract: The invention relates to a novel fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent together with, and synergistically effective amounts of (a) at least one benzophenone of formula I wherein R1, R2, R3, R4, R5, R6, R7, m and n have the meaning given; at least one fungicidal active ingredient selected from the following groups (A), (B), (C), (D) and (E): (A) an ergosterol biosynthesis inhibitor; (B) a strobilurine derivative, (C) a melanin biosynthesis inhibitor; (D) a compound selected from the group consisting of acibenzolar, benomyl, captan, carboxin, chlorothalonil, copper, cyprodinil, dinocap, dithianon, dimethomorph, dodine, ethirimol, famoxadone, fenpiclonil, fluazinam, mancozeb, metalaxyl, pyrifenox, sulfur, vinclozolin and (E) an azolopyrimidine of formula II in which R8, R9, R10, R11, A, L and p have the meaning given; and to a method of controlling the growth of phytopathogenic fungi at a locus which comprises aType: GrantFiled: January 16, 2002Date of Patent: May 11, 2004Assignee: BASF AktiengesellschaftInventors: Henry Van Tuyl Cotter, Gunther Reichert, Ewald Sieverding, Petrus Martinus Franciscus Emanuel Jegerings
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Publication number: 20040077639Abstract: Therapeutic methods for the prevention and treatment of respiratory diseases or conditions are described, the methods including administering to a subject in need thereof a respiratory disease or condition effective amount of a selective inhibitor of inducible nitric oxide synthase.Type: ApplicationFiled: May 16, 2003Publication date: April 22, 2004Inventor: Pamela T. Manning
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Patent number: 6723753Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.Type: GrantFiled: February 7, 2002Date of Patent: April 20, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6720452Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: June 10, 2002Date of Patent: April 13, 2004Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber, Timothy Luker, Michael Mortimore, Philip Thorne
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Patent number: 6716421Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.Type: GrantFiled: March 5, 2001Date of Patent: April 6, 2004Assignee: University of Florida Research Foundation, Inc.Inventors: Philip Frederick Brode, III, Garry Steven Garrett, Leo Timothy Laughlin, Randall Stryker Matthews, Dale Edwin Barker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
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Publication number: 20040063772Abstract: The present application describes intermediates for nitrogen containing heteroaromatics and derivatives thereof of formula I: 1Type: ApplicationFiled: June 24, 2003Publication date: April 1, 2004Inventors: Mimi L. Quan, Renhua Li
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Patent number: 6713501Abstract: Use of a tablet diet supplement for administration to a dialysis patient comprising a mixture of L-histidine, L-isoleucine, L-leucine, L-lysine, L-methionine, L-phenylalanine, L-threonine, L-tryptophan, L-tyrosine and L-valine, for preventing and/or correcting hypoalbuminemia in a patient on dialysis.Type: GrantFiled: August 21, 2000Date of Patent: March 30, 2004Assignee: The Johns Hopkins UniversityInventor: Mackenzie Walser