Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 514/329)
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Patent number: 6727241Abstract: The present invention is directed to pharmaceutical compositions containing active compounds, which inhibit the activity of the chemokines, MIP-1&agr; and RANTES. It also is directed to methods of treating inflammatory and immunoregulatory disorders and diseases using these pharmaceutical compositions.Type: GrantFiled: June 12, 2002Date of Patent: April 27, 2004Assignee: ChemocentryxInventor: Brian McMaster
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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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Patent number: 6713492Abstract: Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.Type: GrantFiled: May 24, 2001Date of Patent: March 30, 2004Assignees: Daiichi Radioisotope Laboratories, Ltd., Yamagata Public Corporation for the Development of IndustryInventors: Osamu Itoh, Heitaro Obara, Hidekatsu Yokoyama, Masaaki Aoyama
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Patent number: 6710179Abstract: Compounds of general formula (I) wherein m is 0 or 1, and n is 1 or 2; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: April 15, 2002Date of Patent: March 23, 2004Assignee: AstraZeneca Canada Inc.Inventors: Benjamin Pelcman, Edward Roberts
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Patent number: 6710061Abstract: The present invention is directed to compounds useful as selective serine protease or dual-serine protease inhibitors, compositions thereof and methods for treating serine protease or dual-serine protease mediated disorders.Type: GrantFiled: November 25, 2002Date of Patent: March 23, 2004Assignee: Ortho-McNeil Pharamceutical, Inc.Inventors: Michael N. Greco, Bruce E. Maryanoff, Michael J. Hawkins, Robert E. Boyd
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Publication number: 20040039025Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.Type: ApplicationFiled: August 28, 2003Publication date: February 26, 2004Inventors: Syed M. Ali, Kurt R. Brunden, Dario Doller, Brian Herbert, Jack B. Jiang, Amy Jordan
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Patent number: 6680071Abstract: This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as active ingredient, an opioid (&mgr;receptor) agonist, such as fentanyl, or a salt thereof, characterized in that the composition is in the form of a fast-dispersing dosage form designed to release the active ingredient rapidly in the oral cavity. A process for preparing such a composition and the use of such a composition as an analgesic, for the treatment of chronic pain and/or breakthrough pain, as an anesthetic premedication, for the induction of anesthesia, as a sedative and/or for the treatment of anxiety are also provided.Type: GrantFiled: January 14, 2002Date of Patent: January 20, 2004Assignee: R. P. Scherer Technologies, Inc.Inventors: Edward Stewart Johnson, Jon Lacy
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Publication number: 20040006089Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula 1Type: ApplicationFiled: May 23, 2002Publication date: January 8, 2004Inventors: Christophe Thurieau, Jerome Gonzalez, Christhope Moinet
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Patent number: 6673829Abstract: Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.Type: GrantFiled: September 12, 2002Date of Patent: January 6, 2004Assignee: Novo Nordisk A/SInventors: Florencio Zaragoza Dorwald, Rolf Hohlweg
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Patent number: 6667319Abstract: The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: July 24, 2002Date of Patent: December 23, 2003Assignee: Schering-Plough CorporationInventors: Andrew W. Stamford, Ying Huang, Guoqing Li
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Patent number: 6667309Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: GrantFiled: March 12, 2002Date of Patent: December 23, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert H. Chen, Min A. Xiang
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Patent number: 6664237Abstract: The invention provides single-dose oral formulations for controlling an ectoparasite infestation on a companion animal for a prolonged time, said formulations comprising a spinosyn component, or a physiologically acceptable derivative or salt thereof, and a carrier in oral dosage form. It also provides methods for controlling such infestations comprising orally administering a single dose of these formulations to the animal.Type: GrantFiled: January 24, 2002Date of Patent: December 16, 2003Assignee: Eli Lilly and CompanyInventor: Daniel Earl Snyder
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Patent number: 6664273Abstract: The present invention discloses compounds, which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: November 25, 2002Date of Patent: December 16, 2003Assignee: Schering CorporationInventors: Duane A. Burnett, Wen-Lian Wu
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Patent number: 6664248Abstract: Compounds of formula wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group R1 is hydrogen or C1-C3alkyl; R2 is hydrogen or C1-C3alkyl; R3 is hydrogen an unsubstituted or substituted C1-C6alkyl, C3-C6cycloalkyl, C2-C6alkenyl or C2-C6alkynyl group, or C(═O)—R5, R5 is C1-C4alkyl, C1-C4alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R6)2, each R6, independently of the other, is hydrogen, C1-C4alkyl or unsubstituted or substituted phenyl, X is CH—NO2, N—CN or N—NO2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per seType: GrantFiled: January 13, 2003Date of Patent: December 16, 2003Assignee: Syngenta Investment Corp.Inventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
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Patent number: 6649614Abstract: The present invention relates to the treatment of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or anti-anxiety agent.Type: GrantFiled: October 16, 2001Date of Patent: November 18, 2003Assignee: Merck Sharp & Dohme Ltd.Inventors: Emma Joanne Carlson, Nadia Melanie Rupniak
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Publication number: 20030212049Abstract: Compounds of the formula: 1Type: ApplicationFiled: February 27, 2003Publication date: November 13, 2003Applicant: WyethInventors: Jeremy I. Levin, James Ming Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
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Patent number: 6645980Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: GrantFiled: November 20, 2000Date of Patent: November 11, 2003Assignee: Sepracor Inc.Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
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Patent number: 6638950Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 20, 2001Date of Patent: October 28, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng
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Patent number: 6638951Abstract: A novel benzamide derivative represented by the following general formula: wherein R represents an alkyl group having 3 to 6 carbon atoms or a salt thereof, and a medicament comprising said derivative as an active ingredient. The medicament has excellent enhancing action on gastrointestinal tract motility, and is orally available with reduced side effects. Therefore, the medicament is extremely useful as an agent for therapeutic treatment of digestive diseases, an agent for improving function of gastrointestinal tract motility and the like.Type: GrantFiled: November 8, 2001Date of Patent: October 28, 2003Assignee: Hokuriku Seiyaku Co., Ltd.Inventors: Hideo Kato, Noriyuki Kado, Jun Sakaguchi
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Patent number: 6635764Abstract: This invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.Type: GrantFiled: December 7, 2000Date of Patent: October 21, 2003Assignee: Theravance, Inc.Inventors: Mathai Mammen, David Oare
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Publication number: 20030195212Abstract: The present invention relates to novel aromatic amines of general formula (I) and to the use of these amines for the treatment of obesity, anorexia, inflammation, mental disorders an other diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.Type: ApplicationFiled: November 20, 2002Publication date: October 16, 2003Inventors: Torbjorn Lundstedt, Anna Skottner, Elisabeth Seifert, Igor Starchenkov, Peteris Trapencieris, Valerjans Kauss, Ivars Kalvins, Arne Boman
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Publication number: 20030166635Abstract: Compounds of formula 1Type: ApplicationFiled: January 13, 2003Publication date: September 4, 2003Inventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
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Publication number: 20030166668Abstract: Disclosed are substituted heteroarylalkanoic acids acids of the following formula D-A-C(O)R′, where D, A, and R′ are defined herein. These compounds are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: ApplicationFiled: November 14, 2002Publication date: September 4, 2003Applicant: The Institutes for Pharmaceutical Discovery, Inc. A Corporation of the State of DelawareInventors: Michael C. Van Zandt, Leo Geraci
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Patent number: 6610709Abstract: This invention relates to (2R,3S,4R,5R)-2-amino-5-methylpiperidine-3,4-diol or a (2S,3S,4R,5R)-2-N-substituted-2-amino-5-methylpiperidine-3,4-diol represented by the general formula (I): wherein R1 and R2 each are a hydrogen atom, or R1 is a hydrogen atom and R2 is a lower alkanoyl group or a lower &ohgr;-trihaloalkanoyl group, or R1 and R2 together denote phthaloyl group, and a pharmaceutically acceptable salt thereof. Said compound can be prepared from a (2S,3S,4R)-5-N-protected-2,3,4-O-tri-protected-5-aminopentane-1,2,3,4-tetraol by multi-steps of reactions.Type: GrantFiled: August 1, 2001Date of Patent: August 26, 2003Assignees: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Meiji Seika Kaisha, Ltd.Inventors: Yoshio Nishimura, Eiki Shitara, Tomio Takeuchi
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Publication number: 20030158186Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: December 20, 2002Publication date: August 21, 2003Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Bradley Paul Morgan, Han-Jie Zhou, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans,
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Patent number: 6608227Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.Type: GrantFiled: October 13, 2000Date of Patent: August 19, 2003Assignee: Bristol-Myers Squibb PharmaInventors: Dean A Wacker, John V Duncia, Joseph B Santella, III, Daniel S Gardner
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Patent number: 6605620Abstract: A cyclic amine compound by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.Type: GrantFiled: March 28, 2002Date of Patent: August 12, 2003Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Shunji Takemura, Takeshi Doi, Yoshinori Kyotani, Masao Ohkuchi
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Publication number: 20030139388Abstract: The present application describes novel cyclic hydroxamic acids of formula I: 1Type: ApplicationFiled: September 16, 2002Publication date: July 24, 2003Inventors: Gregory R. Ott, Xiao-Tao Chen, Jingwu Duan, Zhonghui Lu
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Patent number: 6593346Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.Type: GrantFiled: February 14, 2002Date of Patent: July 15, 2003Assignee: Merck & Co. Inc.Inventors: Paul E. Finke, Kerry A. Hilfiker, Malcolm MacCoss, Kevin T. Chapman, Jennifer L. Loebach, Sander G. Mills, Ravi N. Guthikonda, Shrenik K. Shah, Dooseop Kim, Dong-Ming Shen, Bryan Oates
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Patent number: 6586441Abstract: The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to adenosine receptor modulators, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses, hypoxia, ischaemia, seizure, substance abuse, sedation and they may be active as muscle relaxants, antipsychotics, anti epileptics, anticonvulsants and cardiaprotective agents.Type: GrantFiled: February 20, 2001Date of Patent: July 1, 2003Assignee: Hoffman-La Roche Inc.Inventors: Edilio Maurizio Borroni, Gerda Huber-Trottmann, Gavin John Kilpatrick, Roger David Norcross
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Patent number: 6573281Abstract: The present invention relates to the use of saredutant and of its pharmaceutically acceptable salts for the treatment or prevention of adaptation disorders, bipolar disorders, and dysthymic disorders.Type: GrantFiled: October 9, 2001Date of Patent: June 3, 2003Assignee: Sanofi-SynthelaboInventors: Xavier Emonds-Alt, Philippe Soubrie, Régis Steinberg
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Patent number: 6569872Abstract: Use of an antagonist selected from the group consisting of: (a) antagonists of neurokinin-1 (NK1), neurokinin-2 (NK2) and neurokinin-3 (NK3) receptors, (b) antagonists of NK1 and NK2 receptors, (c) antagonists of NK2 and NK3 receptors, (d) antagonists of NK1 and NK3 receptors, (e) antagonists of NK1 receptors, and (f) antagonists of NK2 to treat symptoms and disorders associated with a production and/or secretion of androgen. One aspect of the invention relates to the use of antagonists to suppress production/secretion of androgens in mammals suffering from an androgen-dependent disease, such as benign prostatic hyperplasia and prostatic carcinoma.Type: GrantFiled: May 7, 2002Date of Patent: May 27, 2003Assignee: Schering CorporationInventors: Michael W. Leach, Mark R. Berardi, Elmer J. Mirro, Dineshwar Sinha, Jonathan A. Pachter, Mark E. Cartwright, Gregory A. Reichard
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Publication number: 20030092694Abstract: The invention relates to compounds of the general formula (I): 1Type: ApplicationFiled: October 11, 2002Publication date: May 15, 2003Applicant: Biovitrum, AB, a Stockholm, Sweden corporationInventors: Bjorn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jonsson
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Patent number: 6555552Abstract: The present invention relates compounds of the formula (I): wherein X represents hydrogen or a C1-4alkyl group optionally substituted by a hydroxy group; Y represents hydrogen, C1-6alkyl or C3-7cycloalkyl; Z is —CR9R10CH2— or —CH2CR9R10—; R represents hydrogen, fluorine, hydroxy, C1-6alkyl or C1-6alkoxy; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: April 1, 2002Date of Patent: April 29, 2003Assignee: Merck Sharp & Dohme Ltd.Inventors: Janusz Jozef Kulagowski, Piotr Antoni Raubo, Christopher George Thomson
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Patent number: 6552046Abstract: The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate.Type: GrantFiled: June 7, 2001Date of Patent: April 22, 2003Assignee: Aryx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner, Jürg Pfister, Cyrus Becker
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Publication number: 20030069225Abstract: Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound.Type: ApplicationFiled: July 10, 2002Publication date: April 10, 2003Applicant: Shionogi BioResearch Corp.Inventors: Shoujun Chen, Lijun Sun, Zhi-Qiang Xia, Keizo Koya, Mitsunori Ono
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Publication number: 20030055045Abstract: Compounds of general formula (I) 1Type: ApplicationFiled: April 15, 2002Publication date: March 20, 2003Applicant: Astra Pharma Inc.Inventors: Benjamin Pelcman, Edward Roberts
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Patent number: 6525069Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 21, 2000Date of Patent: February 25, 2003Assignee: Bristol-Myers Squibb Pharma Co.Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
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Publication number: 20030027813Abstract: The present invention provides a composition comprising synergistic amounts of a compound of the formula (I) 1Type: ApplicationFiled: June 3, 2002Publication date: February 6, 2003Inventors: Stefan Dutzmann, Christoph Erdelen, Wolfram Andersch, Heinz-Wilhelm Dehne, Jurgen Hartwig, Klaus Stenzel, Wolfgang Kramer
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Patent number: 6514992Abstract: The present invention is to novel compounds of Formula (I), their pharmaceutical compositions, and to the novel inhibition of Caspases for use in the treatment of apoptosis, and disease states caused by excessive or inappropriate cell death.Type: GrantFiled: December 14, 2000Date of Patent: February 4, 2003Assignee: SmithKline Beecham CorporationInventors: Dennis Lee, Scott A. Long
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Patent number: 6511995Abstract: A pyridine derivative represented by formula (1) wherein all the variables have been defined in the specification. The compounds are used for inhibiting collagen production and are useful for preventing or treating fibrosis.Type: GrantFiled: September 25, 2000Date of Patent: January 28, 2003Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Kouji Edamatsu, Takao Nagahama, Satoshi Hayakawa, Yutaka Kojima, Makoto Sakamoto, Koichi Yasumura
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Patent number: 6509358Abstract: This invention provides compounds of Formula I having the structure and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.Type: GrantFiled: July 12, 2001Date of Patent: January 21, 2003Assignee: WyethInventors: William Floyd Fobare, Jill Freymuller
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Patent number: 6506775Abstract: The invention provides a compound of formula (I): and its pharmaceutically acceptable salts, wherein R is halo C2-C8 alkenyl or halo C2-C8 alkynyl; R1 is hydrogen, halo or C1-C6 alkoxy; or R and R1, together with the two carbon atoms to which they are attached, form a C4-C6 cycloalkyl or a C4-C6 oxacycloalkyl ring wherein said ring may be optionally substituted by one or more substituents selected from the group consisting of halo, C1-C6 alkyl and halo C1-C6 alkyl; X is C1-C6 alkoxy, halo C1-C6 alkoxy, phenoxy or halo; and Ar is phenyl optionally substituted by halo. These compounds are useful in the treatment of a gastrointestinal disorder; a central nervous system (CNS) disorder; an inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by Heliobacter pylori; or angiogenesis especially CNS disorders in a mammalian subject, especially humans.Type: GrantFiled: May 1, 2000Date of Patent: January 14, 2003Assignee: Pfizer INCInventors: Kunio Satake, Yuji Shishido, Hiroaki Wakabayashi
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Patent number: 6506777Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.Type: GrantFiled: June 8, 2000Date of Patent: January 14, 2003Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Jennifer L. Loebach, Malcolm Maccoss, Sander G. Mills
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Publication number: 20030004151Abstract: The present application describes modulators of MCP-1 of formula (I): 1Type: ApplicationFiled: December 20, 2001Publication date: January 2, 2003Inventor: Robert Cherney
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Patent number: 6498170Abstract: This invention provides compounds of Formula I having the structure wherein R1, R2, R3, W, X, and Z are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: July 12, 2001Date of Patent: December 24, 2002Assignee: WyethInventors: Fuk-Wah Sum, Baihua Hu
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Patent number: 6498169Abstract: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 an W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 each independently represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroalkyl group; and l, m and n each represents a number of 0 to 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.Type: GrantFiled: October 26, 2001Date of Patent: December 24, 2002Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Shunji Takemura, Takeshi Doi, Yoshinori Kyotani, Masao Ohkuchi
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Publication number: 20020177609Abstract: The invention provides conjugates of fatty alcohols and pharmaceutical agents useful in treating cancer, viruses, psychiatric disorders. Compositions, pharmaceutical preparations, and methods of preparation of the fatty alcohols-pharmaceutical agent conjugates are provided.Type: ApplicationFiled: March 25, 2002Publication date: November 28, 2002Inventors: Charles S. Swindell, Glenn J. Fegley
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Publication number: 20020172658Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies.Type: ApplicationFiled: March 5, 2001Publication date: November 21, 2002Inventors: Philip Frederick Brode, 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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Patent number: RE38407Abstract: Liposome-encapsulated opioid analgesic agents delivered by the pulmonary route provide local, or systemic analgesia superior to that produced by the solution form of these agents administered by parentral (intravenous, intramuscular, or subcutaneous injection) or oral routes.Type: GrantFiled: June 14, 2001Date of Patent: January 27, 2004Assignee: Delex Therapeutics Inc.Inventors: Michael Mezel, Orlando Hung