Benzene Ring Bonded Directly To Ring Carbon Of The Seven-membered Hetero Ring Patents (Class 514/217.02)
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Patent number: 11261205Abstract: The present invention relates to the use of oxazolidinone-quinolone hybrids for the parenteral (especially intravenous) treatment or prophylaxis of bacterial diseases. The present invention relates moreover to improved methods of administering oxazolidinone-quinolone hybrid antibacterials.Type: GrantFiled: June 22, 2020Date of Patent: March 1, 2022Assignee: Morphochem GmbHInventors: Thomas Kapsner, Axel Dalhoff, Thomas Gramatte
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Patent number: 10723746Abstract: The present invention relates to the use of oxazolidinone-quinolone hybrids for the parenteral (especially intravenous) treatment or prophylaxis of bacterial diseases. The present invention relates moreover to improved methods of administering oxazolidinone-quinolone hybrid antibacterials.Type: GrantFiled: May 9, 2014Date of Patent: July 28, 2020Assignee: Morphochem Aktiengesellschaft Für Kombinatorische ChemieInventors: Thomas Kapsner, Axel Dalhoff, Thomas Gramatte
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Publication number: 20150065489Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.Type: ApplicationFiled: October 30, 2014Publication date: March 5, 2015Inventors: Matthias HOFFMANN, Daniel BISCHOFF, Georg DAHMANN, Jasna KLICIC, Gerhard SCHAENZLE, Stefan Ludwig Michael WOLLIN, Serge Gaston CONVERS-REIGNIER, Stephen Peter EAST, Frederic Jacques MARLIN, Clive McCARTHY, John SCOTT
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Publication number: 20140249136Abstract: This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.Type: ApplicationFiled: May 7, 2014Publication date: September 4, 2014Applicant: VEROSCIENCE, LLCInventor: Anthony H. Cincotta
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Patent number: 8754073Abstract: Piperidinodihydrothienopyrimidines of formula 1 wherein X is SO or SO2 (preferably SO), and R1, R2, R3, and R4 may have the meanings given in the disclosure and claims, pharmacologically acceptable salts thereof, and pharmaceutical compositions containing these compounds. These piperidinodihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system, or cancers.Type: GrantFiled: October 16, 2008Date of Patent: June 17, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
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Patent number: 8741890Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: GrantFiled: November 14, 2008Date of Patent: June 3, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Kai Gerlach, Herbert Nar, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
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Publication number: 20140107104Abstract: The present invention provides a combination medicine for treatment of depression, comprising a combination of (A1) an antidepressant and either (B1) a dopamine D1 receptor agonist or (C1) a dopamine D1 receptor antagonist; and a method for screening for an antidepressant that in combination with a dopamine D1 receptor agonist provides an improvement in treatment of depression, the method comprising the steps of: administering, to a mammal, (A2) a compound having an antidepressant action and (B1) a dopamine D1 receptor agonist, and detecting a greater increase in depression-related gene expression, dopamine D1 receptor expression and/or dopamine D1 receptor signaling in comparison with the case where (A2) the compound having an antidepressant action or (B1) the dopamine D1 receptor agonist is administered.Type: ApplicationFiled: March 22, 2012Publication date: April 17, 2014Inventors: Akinori Nishi, Katsunori Kobayashi, Tsuyoshi Miyakawa, Paul Greengard
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Publication number: 20140051685Abstract: The present invention is directed to a method for treating a patient suffering from a metabolic disorder such as the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, and the metabolic sequale of these diseases including cardiovascular, cerebrovascular, renal and hepatic diseases, comprising the step of: administering to a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes a pharmaceutical composition comprising (1) at least one compound that stimulates an increase in central dopaminergic neuronal activity level in the subject, and (2) at least one compound that stimulates a decrease in central noradrenergic neuronal activity level in the subject.Type: ApplicationFiled: November 21, 2011Publication date: February 20, 2014Inventor: Anthony H. Cincotta
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Patent number: 8633184Abstract: The invention is directed to compounds of Formula (I) useful as PPAR agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, diabetes, nephropathy, neuropathy, retinopathy, polycystic ovary syndrome, hypertension, ischemia, stroke, irritable bowel disorder, inflammation, cataract, cardiovascular diseases, Metabolic X Syndrome, hyper-LDL-cholesterolemia, dyslipidemia (including hypertriglyceridemia, hypercholesterolemia, mixed hyperlipidemia, and hypo-HDL-cholesterolemia), atherosclerosis, obesity, and other disorders related to lipid metabolism and energy homeostasis complications thereof, using compounds of the invention are also described.Type: GrantFiled: January 19, 2010Date of Patent: January 21, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Gee-Hong Kuo, Yan Zhang, Lan Shen, Songfeng Lu, Keith T. Demarest, Patricia Pelton
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Publication number: 20130338145Abstract: Provided is a method of treating or preventing age-related macular degeneration (AMD) or Stargardt's disease in a patient subject to, or symptomatic of the disease, whereby normal lysosomal pH (pHL) of compromised retinal pigment epithelium (RPE) cells of the eye is restored, or abnormally elevated pHL is reacidified, thus decreasing or preventing damaging accumulations of lipofuscin debris or photoreceptor waste products. Further provided is a method for restoring photoreceptors to the eye of a patient subject to, or symptomatic of reduced photoreceptor activity or lipofuscin accumulation in RPE cells. By these methods D5 dopamine receptor (D5DR) agonists are administered to stimulate D5DR activity of compromised RPE cells, thereby regulating and reacidifying lysosomal pH (pHL) by a D5 dopamine receptor-(D5DR)-mediated pathway, without altering baseline maintenance.Type: ApplicationFiled: March 15, 2013Publication date: December 19, 2013Inventors: Claire H. Mitchell, Alan M. Laties
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Publication number: 20130239234Abstract: The present invention provides methods and compositions for modulating the activity of phosphodiesterase 1B (PDE1B) in intracellular signaling pathways, including but not limited to, dopamine D1 intracellular signaling pathways. The invention also provides methods and compositions for modulating the activities of intracellular signaling molecules, including, but not limited to, DARPP-32 and GluR1 AMPA receptor, via modulation of PDE1B. The invention also provides pharmaceutical compositions and methods of screening for compounds that modulate PDE1B activity. The invention also provides methods of treating or ameliorating the symptoms of a disorder, including but not limited to a PDE1B-related disorder or a dopamine D1 receptor intracellular signaling pathway disorder, by administering a modulator of PDE1B, preferably, but not limited to, an inhibitor of PDE1B or an agent that decreases the production of PDE1B.Type: ApplicationFiled: November 22, 2010Publication date: September 12, 2013Inventors: Paul Greengard, David Repaske, Gretchen Snyder
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Publication number: 20130090307Abstract: The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid ? toxicity. More specifically, the present invention relates to novel combinatorial therapies of Multiple Sclerosis, Alzheimer's disease, Alzheimer's disease related disorder, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on Baclofen and Acamprosate combination.Type: ApplicationFiled: December 6, 2012Publication date: April 11, 2013Applicant: PHARNEXTInventor: PHARNEXT
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Publication number: 20130078284Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Inventors: Tzuchi R. Ju, Claudia M. Davila, Yi Gao, Linda E. Gustavson, David LeBlond, Tong Zhu
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Publication number: 20120264698Abstract: Dopamine reuptake inhibitors, and their analogs, are disclosed for treating and delaying the progression of autoimmune diseases.Type: ApplicationFiled: October 5, 2011Publication date: October 18, 2012Inventors: Hao Chen, Alexel Miagkov, Lisa Leary, Ming Liu, Qi Su
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Publication number: 20120171262Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.Type: ApplicationFiled: March 15, 2012Publication date: July 5, 2012Inventors: Tzuchi R. Ju, Claudia M. Davila, Yi Gao, Linda E. Gustavson, David LeBlond, Tong Zhu
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Publication number: 20120164139Abstract: Provided herein are methods of treating gastrointestinal motility disorders by targeting the dopamine 3 receptor (D3R). A D3R agonist is administered to a subject to decrease gastrointestinal motility to treat the disorder. A D3R antagonist is administered to a subject to decrease gastrointestinal motility to treat the disorder.Type: ApplicationFiled: March 6, 2012Publication date: June 28, 2012Applicant: The Board of Regents of the University of Texas SystemInventors: Pankaj Jay Pasricha, Maria-Adelaide Micci
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Publication number: 20120058992Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate angiogenesis for treating said disease.Type: ApplicationFiled: October 29, 2010Publication date: March 8, 2012Applicant: PHARNEXTInventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Oxana Guerassimenko, Esther Graudens
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Publication number: 20120046242Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: December 21, 2009Publication date: February 23, 2012Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Travis L. BIechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Publication number: 20110218158Abstract: Cytosine deaminase inhibitors and methods for identifying inhibitors of the anti-retroviral activity of APOBEC3G are described.Type: ApplicationFiled: September 22, 2009Publication date: September 8, 2011Inventors: Reuben S. Harris, Ming Li
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Publication number: 20100316731Abstract: Methods and compounds are disclosed for treating dry age-related macular degeneration, and preventing or delaying the onset of wet age-related macular degeneration.Type: ApplicationFiled: May 30, 2008Publication date: December 16, 2010Inventors: Joseph Weinstock, Sarah Jane Paikowsky
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Publication number: 20100311728Abstract: Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol/inositol phosphate after treatment to a basal ratio in a subject.Type: ApplicationFiled: July 23, 2010Publication date: December 9, 2010Inventor: Ashiwel S. Undieh
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Publication number: 20100286124Abstract: The present invention relates to new prop-2-yn-1-amine inhibitors of monoamine oxidase type B activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 9, 2010Publication date: November 11, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100172916Abstract: The present invention relates to new substituted hydroxyphenylamine based modulators of hormone and/or pigment levels, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 9, 2009Publication date: July 8, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Craig Hodulik, Soon Woo
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Publication number: 20100075926Abstract: The invention provides methods and compounds for the treatment of neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (Amyotrophic Lateral Sclerosis), traumatic brain injury, ischemic brain injury or a stroke. In one aspect the compounds are HDAC1 activators. Exemplary HDAC1 activators include metal chelators, iron chelators, deferoxamin, flavonoids, compounds comprising a catechol moity, ginkgetin K, Chembridge 5104434, sciadopilysin, tetrahydrogamboic acid, TAM-11, LY 235959, CGS 19755, SK&F 97541, etidronic acid, levonordefrin, methyldopa, ampicillin trihydrate, D-aspartic acid, gamma-D-glutamylaminomethylsulfonic acid, phenazopyridine to hydrochloride, oxalamine citrate salt, podophyllotoxin, SK&F 97541, (+-)-4-amino-3-(5-chloro-2-thienyl)-butanoic acid, (RS)-(tetrazol-5-yl) glycine, R(+)-SKF-81297, gambogic acid, and derivatives thereof.Type: ApplicationFiled: July 23, 2009Publication date: March 25, 2010Inventors: Li-Huei Tsai, Stephen J. Haggarty, Dohoon Kim
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Patent number: 7678786Abstract: The invention is directed to compounds of Formula (I) useful as PPAR agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, diabetes, nephropathy, neuropathy, retinopathy, polycystic ovary syndrome, hypertension, ischemia, stroke, irritable bowel disorder, inflammation, cataract, cardiovascular diseases, Metabolic X Syndrome, hyper-LDL-cholesterolemia, dyslipidemia (including hypertriglyceridemia, hypercholesterolemia, mixed hyperlipidemia, and hypo-HDL-cholesterolemia), atherosclerosis, obesity, and other disorders related to lipid metabolism and energy homeostasis complications thereof, using compounds of the invention are also described.Type: GrantFiled: April 17, 2007Date of Patent: March 16, 2010Assignee: Janssen Pharmaceutica NVInventors: Gee-Hong Kuo, Yan Zhang, Lan Shen, Songfeng Lu, Keith T. Demarest, Patricia Pelton
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Publication number: 20090156581Abstract: Pharmaceutical compositions and method using aminergic compounds and complement compounds. Compositions are provided comprising: (a) a subefficacious amount of a non-adrenergic aminergic compound or of an adrenergic antagonist; and (b) a safe and effective amount of a complement compound. Methods are also provided comprising the administration of: (a) a low dose of a non-adrenergic aminergic compound or of any adrenergic antagonist; and (b) a safe and effective amount of a complement compound. Non-adrenergic aminergic compounds can comprise a histaminergic, dopaminergic, muscarinergic, serotoninergic, octopaminergic, or trace aminergic compound. Complement compounds include ascorbates, opioids, polycarboxylic acid chelators, resveratrols, cysteines, substituted derivatives and analogs thereof, and mixtures thereof. Preferred complements include ascorbates, particularly ascorbic acid.Type: ApplicationFiled: April 14, 2006Publication date: June 18, 2009Applicant: BOARD OF TRUSTREES OF MICHIGAN STATE UNIVERSITYInventors: Patrick F. Dillon, Robert S. Root-Bernstein
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Patent number: 7504391Abstract: The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: May 20, 2004Date of Patent: March 17, 2009Assignee: Schering CorporationInventors: Duane A. Burnett, William J. Greenlee, Brian McKittrick, Jing Su, Zhaoning Zhu, Thavalakulamgara K. Sasikumar, Robert Mazzola, Li Qiang, Yuanzan Ye
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Publication number: 20080306019Abstract: Provided herein is a method of protecting a neuron from dysfunction induced by an HIV neurotoxin, comprising contacting the cell with a therapeutically effective dose of a dopamine D1 receptor agonist. Also provided is a method of treating or preventing HIV-1 associated dementia (HAD) in a subject in need of such treatment or prevention, comprising administering to the subject a therapeutically effective dose of a dopamine D1 receptor agonist and estrogenic compound.Type: ApplicationFiled: May 3, 2006Publication date: December 11, 2008Inventors: Rosemarie M. Booze, Charles Mactutus
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Publication number: 20080200453Abstract: The present invention is directed to a method of simultaneously treating hypertension, hypertriglyceridemia, a pro-inflammatory state, a pro-coagulative state, and insulin resistance (with or without treating obesity or endothelial dysfunction), associated with or independent from Metabolic Syndrome, as well as vascular disease such as cardiovascular, cerebrovascular, or peripheral vascular disease comprising the step of administering to a patient suffering from such disorders a therapeutically effective amount of a central acting dopamine agonist. In one embodiment, the central acting dopamine agonist is bromocriptine, optionally combined with a pharmaceutically acceptable carrier.Type: ApplicationFiled: March 20, 2008Publication date: August 21, 2008Inventor: Anthony H. Cincotta
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Publication number: 20080166298Abstract: The present invention relates to radiolabelled compounds of formula (I), which are useful for the labelling and diagnostic imaging of histamine H3 receptor functionality.Type: ApplicationFiled: January 5, 2006Publication date: July 10, 2008Inventor: Christophe Plisson
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Publication number: 20080027040Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: December 20, 2004Publication date: January 31, 2008Applicant: Morphochem Aktiengesellschaft Fur KombinatorischeInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Muller, Michael W. Cappi
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Publication number: 20070281920Abstract: Compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ar, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, methods of preparing the compounds, and method of using the compounds for treatment of monoamine reuptake inhibitor-mediated diseases.Type: ApplicationFiled: May 31, 2007Publication date: December 6, 2007Inventors: Ryan Craig Schoenfeld, Robert James Weikert
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Patent number: 7279468Abstract: The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the ?v?3 integrin receptor, their use, and pharmaceutical preparations comprising these compounds.Type: GrantFiled: June 15, 2001Date of Patent: October 9, 2007Assignee: Abbott GmbH & Co. KGInventors: Herve Geneste, Andreas Kling, Udo Lange, Werner Seitz, Claudia Isabella Graef, Thomas Subkoski, Wilfried Hornberger, Arnulf Lauterbach
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Patent number: 7202237Abstract: The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the central nervous system, pain, inflammatory diseases, diseases caused by smooth muscle contractions and as assistance in the cessation of chemical substance abuse.Type: GrantFiled: May 19, 2004Date of Patent: April 10, 2007Assignee: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet Østergaard Nielsen
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Publication number: 20040057987Abstract: Composition of matter for application to a body surface or membrane to administer fenoldopam by permeation through the body surface or membrane, the composition comprising fenoldopam to be administered, at a therapeutically effective rate, in combination with a permeation enhancer or mixture. Also disclosed are drug delivery devices and methods for the transdermal administration of fenoldopam for the treatment of hypertension, congestive heart failure, and chronic and acute renal failure.Type: ApplicationFiled: September 29, 2003Publication date: March 25, 2004Inventors: William W. van Osdol, Nieves M. Crisologo, Su Il Yum
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Patent number: 6677332Abstract: 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: May 25, 2000Date of Patent: January 13, 2004Assignee: 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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Publication number: 20030170741Abstract: Screening methods for identifying compounds that bind to or activate (D1 or D5 dopamine receptors individually or in combination) or regulate or potentially regulate skeletal muscle mass or function in vivo. Also disclosed are screening methods for identifying compounds that prolong or augment the activation of D1 or D5 dopamine receptors or of D1 or D5 dopamine receptor signal transduction pathways and increase D1 or D5 dopamine receptor expression. Pharmaceutical compositions comprising D1 or D5 dopamine receptor agonists, antibodies to D1 or D5 dopamine receptors and methods for increasing skeletal muscle mass or function or for the treatment of skeletal muscle atrophy using D1 or D5 dopamine receptors as the target for intervention and methods for treatment of muscular dystrophies are described.Type: ApplicationFiled: November 18, 2002Publication date: September 11, 2003Applicant: The Procter & Gamble CompanyInventors: Robert Joseph Isfort, Russell James Sheldon
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Publication number: 20030092701Abstract: The invention is directed to a pharmaceutical composition and a corresponding method for inducing analgesia or anesthesia in a mammalian subject, while simultaneously inhibiting respiratory depression in the subject. The composition contains in combination, an opiate or opioid analgesic or anesthetic and a D1-dopamine receptor agonist in an amount sufficient to inhibit respiratory depression caused by the opiate or opioid.Type: ApplicationFiled: November 9, 2001Publication date: May 15, 2003Inventor: Peter M. Lalley
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Patent number: 6534496Abstract: The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and high universality in usage. Another object of the present invention is to provide a pharmaceutical composition comprising a compound of the following formula: wherein Ar represents phenyl which may be substituted and/or condensed; n represents an integer of 1 to 10; R represents hydrogen or a hydrocarbon group which may be substituted, which may not be the same in its n occurrences; R may be bound to either Ar or a substituent for Ar; Y represents an amino group which may be subsituted or a nitrogen-containing saturated heterocyclic group which may be substituted, or a salt thereof, which can be used for a thermogenic agent, an antiobesity agent, a lipolytic agent, or a prophylactic and/or treating drug for obesity-associated diseases.Type: GrantFiled: October 7, 1999Date of Patent: March 18, 2003Assignee: Takeda Chemical Industries, Inc.Inventors: Yuji Ishihara, Yukio Fujisawa, Naoki Furuyama
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Patent number: 6495543Abstract: The invention relates to compounds of formula (I): wherein: G1 represents an alkylene chain as defined in the description, A represents R2 and R3 represent hydrogen, alkyl, alkoxy or hydroxy or together form oxo, R4 and R5 represent hydrogen or together form aryl, R1 is as defined in the description. and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.Type: GrantFiled: October 12, 2000Date of Patent: December 17, 2002Assignee: Les Laboratoires ServierInventors: Gérald Guillaumet, Marie-Claude Viaud, Hervé Van De Poel, Philippe Delagrange, Caroline Bennejean, Pierre Renard
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Patent number: 6489354Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f 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-3 and/or CCR-5.Type: GrantFiled: March 1, 2000Date of Patent: December 3, 2002Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht