Benzene Ring Bonded Directly Or Attached Indirectly By An Acyclic Carbon Or An Acyclic Carbon Chain To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 548/506)
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Publication number: 20150005346Abstract: The present invention relates to novel heterocyclic derivatives which are allosteric modulators of cannabinoid receptor 1 (CB1) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with endocannabinoid dysfunction and diseases in which the CB1 subtype of cannabinoid receptor is involved; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.Type: ApplicationFiled: July 3, 2014Publication date: January 1, 2015Inventors: Ganeshsingh A. THAKUR, Pushkar M. KULKARNI
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Publication number: 20140357634Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.Type: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Applicant: GRÜNENTHAL GMBHInventors: BERT NOLTE, WOLFGANG SCHRÖDER, KLAUS LINZ, WERNER ENGLBERGER, HANS SCHICK, HEINZ GRAUBAUM, BIRGIT ROLOFF, SIGRID OZEGOWSKI, JÓZSEF BÁLINT, HELMUT SONNENSCHEIN
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Publication number: 20140194472Abstract: Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.Type: ApplicationFiled: August 26, 2012Publication date: July 10, 2014Applicants: WOMEN AND INFANTS' HOSPITAL OF RHODE ISLAND, UWM RESEARCH FOUNDATION, INC.Inventors: Alexander E. Arnold, Preetpal Singh Sidhu, Premchendar Nandhikonda, Rakesh K. Singh
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Patent number: 8680134Abstract: The present invention provides for a composition comprising a tryptamine based drug that acts as a 5-hydroxytryptamine-1 inhibitor in an amount sufficient to reduce the effects of psoriasis and wherein the composition is formulated for topical or oral administration.Type: GrantFiled: October 22, 2010Date of Patent: March 25, 2014Inventor: Avi Dascalu
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Publication number: 20130296230Abstract: A method of the present invention for treating malaria includes the step of administering, to a human or an animal, a therapeutically effective amount of drug for suppressing calcium ion exit from an intracellular organelle of the malaria parasite to an outside of the intracellular organelle and/or calcium ion entry from an outside of a cell of the malaria parasite into the cell.Type: ApplicationFiled: October 27, 2011Publication date: November 7, 2013Applicant: RIKENInventors: Katsuhiko Mikoshiba, Masahiro Enomoto, Shin-Ichiro Kawazu
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Patent number: 8343964Abstract: The invention relates to the use of at least one compound of the formula (I), in which R and R3 are particularly a hydrogen atom, R1 is particularly a hydrogen atom or a methyl, ethyl or isobutyl mi group, R4, R5, R6 and R7 are independently a hydrogen atony, an alkoxyl group with 1 to 7 carbon atoms or a halogen atom, R2 is a hydrogen atom, an O? group or an OH group, B is an N-GP1 or NRc, group, GP1 being a Boc or Cbz group, and Rc is a hydrogen atom or a methyl or t-butyl group, for preparing a drug for treating conditions associated with bacterial infections, in particular for treating bacterial diseases.Type: GrantFiled: January 31, 2008Date of Patent: January 1, 2013Assignees: Universite Joseph Fourier, Centre National de la Recherche ScientifiqueInventors: Jean-Noel Marie Leon Denis, Xavier Jean Georges Marie Guinchard, Nicole Jeanne Moreau born Laffont, Luc Neuville, Yannick Vallee
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Publication number: 20120316171Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.Type: ApplicationFiled: November 4, 2010Publication date: December 13, 2012Inventor: Tamas Oravecz
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Publication number: 20120252863Abstract: The present invention provides for a composition comprising a tryptamine based drug that acts as a 5-hydroxytryptamine-1 inhibitor in an amount sufficient to reduce the effects of psoriasis and wherein the composition is formulated for topical or oral administration.Type: ApplicationFiled: October 22, 2010Publication date: October 4, 2012Inventor: Avi Dascalu
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Publication number: 20120202810Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.Type: ApplicationFiled: April 24, 2012Publication date: August 9, 2012Applicant: Grunenthal GmbHInventors: Bert NOLTE, Wolfgang SHRÖDER, Klaus LINZ, Werner ENGLBERGER, Hans SCHICK, Heinz GRAUBAUM, Birgit ROLOFF, Sigrid OZEGOWSKI, József BÁLINT, Helmut SONNENSCHEIN
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Publication number: 20120108617Abstract: Disclosed is bucindolol substantially free of its R-stereoisomer. Also disclosed are pharmaceutical compositions that include bucindolol substantially free of its R-stereoisomer or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. Also disclosed are methods of treating a patient that involve administering to the patient a therapeutically effective amount of a composition of the present invention. Formula (I).Type: ApplicationFiled: January 27, 2009Publication date: May 3, 2012Applicant: Arca Biopharma, Inc.Inventors: Michael R. Bristow, Jonathan D. Port
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Patent number: 8138219Abstract: Novel compounds of the structural formula (I) are antagonists of the 5-HT6 receptor and are useful in the treatment, prevention and suppression of diseases mediated by the 5-HT6 receptor. The compounds of the present invention are useful in the treatment of obesity, diabetes, metabolic disorder, cognitive disorders, age related cognitive disorder, depression, mania, bipolar disorders, schizophrenia, anxiety, generalized anxiety disorder, panic disorder, and obsessive compulsive disorder, epilepsy, convulsions, migraine, substance withdrawal from substances including but not limited to opiates, nicotine, tobacco products, alcohol, benzodiazepines, sedatives, and the like, sleep disorders, attention deficit/hyperactivity disorder, and Alzheimer's disease.Type: GrantFiled: November 25, 2008Date of Patent: March 20, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Alexander Pasternak, Michael J. Szymonifka
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Publication number: 20120010418Abstract: N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide and starting materials therefore are prepared by new synthetic methods.Type: ApplicationFiled: September 23, 2011Publication date: January 12, 2012Applicant: NOVARTIS AGInventors: Murat Acemoglu, Joginder S. Bajwa, David John Parker, Joel Slade
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Patent number: 8071786Abstract: Novel indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds.Type: GrantFiled: December 14, 2009Date of Patent: December 6, 2011Assignee: Galenea Corp.Inventors: Howard P. Sard, Louis Shuster, Bryan Roth, Cynthia Morency, Govindaraj Kumaran, Liang Xu
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Patent number: 8034960Abstract: The present invention provides a compound of formula 1: wherein R1 is CF3, R2 is H? R3 is H.Type: GrantFiled: November 11, 2010Date of Patent: October 11, 2011Assignee: Pfizer Inc.Inventors: Ronald S. Michalak, Mahmut Levent, Frederick J. Vyverberg, Ara R. Boyajian, Panolil Raveendranath, Michel Cantin, Alan Stockton, Michael W. Winkley, Mousumi Ghosh, Christoph Dehnhardt, Charles Guinosso
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Publication number: 20110054189Abstract: The present invention provides a compound of formula 1: wherein R1 is CF3, R2 is H, R3 is H, and R4 is H.Type: ApplicationFiled: November 11, 2010Publication date: March 3, 2011Inventors: Ronald S. Michalak, Mahmut Levent, Frederick J. Vyverberg, Ara R. Boyajian, Panolil Raveendranath, Michel Cantin, Alan Stockton, Michael W. Winkley, Mousumi Ghosh, Christoph Dehnhardt, Charles Guinosso
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Publication number: 20100144726Abstract: The invention relates to the use of at least one compound of the formula (I), in which R and R3 are particularly a hydrogen atom, R1 is particularly a hydrogen atom or a methyl, ethyl or isobutyl mi group, R4, R5, R6 and R7 are independently a hydrogen atony, an alkoxyl group with 1 to 7 carbon atoms or a halogen atom, R2 is a hydrogen atom, an O? group or an OH group, B is an N-GP1 or NRc, group, GP1 being a Boc or Cbz group, and Rc is a hydrogen atom or a methyl or t-butyl group, for preparing a drug for treating conditions associated with bacterial infections, in particular for treating bacterial diseases.Type: ApplicationFiled: January 31, 2008Publication date: June 10, 2010Applicants: UNIVERSITE JOSEPH FOURIER, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Jean-Noel Marie Leon Denis, Xavier Jean Georges Marie Guinchard, Nicole Jeanne Moreau nee Laffont, Yannick Vallee
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Patent number: 7709661Abstract: A process for the reductive alkylation at the C-3 position of an indole compound in which the indole is treated with an aldehyde in the presence of a Lewis acid and a silicon hydride reducing agent. The process is useful for alkylating the C-3 position of indoles that contain acid-sensitive substituents at the N-1 position.Type: GrantFiled: October 15, 2007Date of Patent: May 4, 2010Assignee: Wyeth LLCInventors: Ronald S. Michalak, Panolil Raveendranath
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Patent number: 7705022Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.Type: GrantFiled: October 27, 2006Date of Patent: April 27, 2010Assignee: Lankenau Institute for Medical ResearchInventors: George C. Prendergast, William P. Malachowski, Alexander J. Muller, James B. DuHadaway
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Publication number: 20100029598Abstract: The present invention relates to extended benzamide derivatives of the general formula I, to processes for preparation thereof and to use thereof for production of pharmaceutical compositions for treatment of disorders and indications associated with the EP2 receptor.Type: ApplicationFiled: July 24, 2009Publication date: February 4, 2010Applicant: Bayer Schering Pharma AGInventors: Marcus Kopitz, Bernhard Lindenthal, Antonius Ter Laak, Tim Wintermantel, Olaf Peters, Gernot Langer, Nico Braeuer, Bernd Buchmann
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Patent number: 7635662Abstract: A urea-urethane compound having one or more urea groups and one or more urethane groups in the molecular structure, the number of said urea groups (A) and the number of said urethane groups (B) satisfying the following numerical formula: 10?(A+B)?3 wherein each of A and B is an integer of 1 or more.Type: GrantFiled: March 2, 2001Date of Patent: December 22, 2009Assignee: Chemipro Kasei Kaisha, Ltd.Inventors: Kazuo Kabashima, Hiroshi Kobayashi, Tetsurou Iwaya
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Publication number: 20090305995Abstract: The invention relates to substituted F3-Phe-trp-F 3-Lys-beta-tri-peptides and derivatives thereof, a process for their preparation, pharmaceutical preparations which contain these compounds which are agonists/antagonists of somatostatin receptors, as active agents for the treatment of disorders which can be influenced by a modulation of somatostatin receptor activity, in particular somatostatin receptor sst4 activity, by the compounds of the invention.Type: ApplicationFiled: November 14, 2005Publication date: December 10, 2009Applicant: Novartis AGInventors: Karl Heinz Krawinkler, Peter Meier, Bernard Faller
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Publication number: 20090306405Abstract: N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide and starting materials therefor are prepared by new synthetic methods.Type: ApplicationFiled: June 7, 2007Publication date: December 10, 2009Applicant: NOVARTIS AGInventors: Murat Acemoglu, Joginder S. Bajwa, David John Parker, Joel Slade
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Publication number: 20090197936Abstract: Salts of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide are prepared and characterized.Type: ApplicationFiled: June 7, 2007Publication date: August 6, 2009Applicant: NOVARTIS AGInventors: Murat Acemoglu, Joginder S. Bajwa, Piotr Karpinski, Dimitris Papoutsakis, Joel Slade, Frank Stowasser
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Publication number: 20090110662Abstract: The present invention relates to the field of polymer chemistry and more particularly to click-functionalized targeting compounds and methods for using the same.Type: ApplicationFiled: April 30, 2008Publication date: April 30, 2009Applicant: Intezyne Technologies, Inc.Inventors: Kurt Breitenkamp, Jonathan Rios-Doria, Rebecca Breitenkamp, Kevin N. Sill, Habib Skaff
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Patent number: 7476690Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: GrantFiled: June 21, 2006Date of Patent: January 13, 2009Assignee: Cephalon FranceInventors: Brigitte Lesur, Christophe Yue, Sophie Chasset, Olivier Renault
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Publication number: 20080255117Abstract: The present invention relates to sulfonyltryptophanols of the general formula I, in which Q, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description. The compounds according to the invention are effective FSH receptor antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.Type: ApplicationFiled: February 29, 2008Publication date: October 16, 2008Inventors: Lars WORTMANN, Bernd Menzenbach, Marcus Koppitz, Dirk Kosemund, Hans Peter Muhn, Anna Schrey, Ronald Kuehne, Thomas Frenzel, Florian Peter Liesener
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Patent number: 7365061Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.Type: GrantFiled: November 14, 2005Date of Patent: April 29, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, Gang Wu, Wei Meng, Alexandra A. Nirschl, William N. Washburn, Terry Stouch
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Patent number: 7365091Abstract: The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula: useful as inhibitors of PHEX. These derivatives are useful for promoting generation of bone mass and treating or preventing diseases or conditions associated with a phosphate metabolism defect. Methods for preparation and intermediates are also disclosed.Type: GrantFiled: May 26, 2006Date of Patent: April 29, 2008Assignee: Enobia PharmaInventors: Denis Gravel, Elaref S. Ratemi, Mostafa Hatam, Guy Boileau, Philippe Crine, Isabelle Lemire
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Patent number: 7288553Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: April 1, 2005Date of Patent: October 30, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
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Patent number: 7276518Abstract: Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds.Type: GrantFiled: November 10, 2003Date of Patent: October 2, 2007Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Werner Englberger, Babette-Yvonne Koegel
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Patent number: 7226942Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.Type: GrantFiled: November 14, 2005Date of Patent: June 5, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, Alexandra A. Nirschl, Wei Meng, Wllliam N. Washburn
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Patent number: 7223786Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.Type: GrantFiled: November 14, 2005Date of Patent: May 29, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Wei Meng, Philip M. Sher, Bruce A. Ellsworth, William N. Washburn
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Patent number: 7214704Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.Type: GrantFiled: November 14, 2005Date of Patent: May 8, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Gang Wu, Philip M. Sher
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Patent number: 7166622Abstract: Compounds of Formula I, wherein R1–R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer's Disease and Down's syndrome are described.Type: GrantFiled: June 9, 2003Date of Patent: January 23, 2007Assignees: Wyeth, ArQule, Inc.Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin Roger Woller, Joseph Raymond Stock, Kristina Martha Kutterer, Dennis Martin Kubrak, Charles William Mann, William Jay Moore, David Scott Casebier
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Patent number: 7115753Abstract: Disclosed are triaryl cationic compounds that exhibit broad spectrum antibiotic and antifungal activity, pharmaceutical compositions containing the compounds, and methods of treating bacterial and fungal infections using the compounds. The compounds were initially isolated by screening a 25,000-member bacterial artificial chromosome (BAC) library of environmental (eDNA) from soil. At least one clone produced a dark brown melanin-like compound that was found to have antibiotic activity. The compounds were isolated and synthesized de novo. From within the positive clone, a single open reading frame that shares extensive sequence similarity with members of the 4-hydroxyphenylpyruvate family of enzymes was found to be necessary and sufficient to confer the production of at least one of the subject compounds on E. coli.Type: GrantFiled: August 8, 2003Date of Patent: October 3, 2006Assignee: Wisconsin Alumni Research FoundationInventors: Jo E. Handelsman, Robert M. Goodman, Doreen E. Gillespie, Alan D. Bettermann, Jon C. Clardy, Sean F. Brady
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Patent number: 7091220Abstract: The present invention relates to substituted indole Mannich bases, processes of preparing substituted indole Mannich base, a medicament containing the same, and a pharmaceutical composition containing the same.Type: GrantFiled: December 20, 2000Date of Patent: August 15, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul
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Patent number: 7001905Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: GrantFiled: March 12, 2001Date of Patent: February 21, 2006Assignee: Warner-Lambert CompanyInventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
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Patent number: 6891065Abstract: A process for making a compound of formula (I) in which process the compound HC?C—(CH2)n—NH2 is reacted with the compound R1—SO2Cl to produce an intermediate compound, which intermediate compound is then reacted with the compound of formula to produce the compound of formula (I), and compounds produced by the process of this invention. The terms R1, R2, R3, R4 and n have the definitions set forth in the specification.Type: GrantFiled: July 21, 2004Date of Patent: May 10, 2005Assignee: WyethInventors: Yanzhong Wu, Panolil Raveendranath
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Patent number: 6787550Abstract: A compound of formula (1) or a salt thereof, or a solvate thereof, wherein; R1 and R2 each independently represents C1-6alkoxy or halo; R3 and R4 each independently represents hydrogen, C1-6alkoxy, arylC1-6alkoxy, hydroxy, carboxyC1-6alkoxy, hydroxyC1-6alkoxy, dihydroxyC1-6alkoxy, mono- and di-(C1-6alkyl)aminoC1-6alkoxy or aminoC1-6alkoxy, and; R5 represents —NRsRt wherein Rs and Rt each independently represent hydrogen, unsubstituted or substituted C1-6alkyl, or unsubstituted or substituted heterocyclyl, a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of the compound or composition in medicine.Type: GrantFiled: December 12, 2001Date of Patent: September 7, 2004Assignee: Nikem Research S.r.l.Inventors: Carlo Farina, Stefania Gagliardi, Pietro A. Novella
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Publication number: 20040110824Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below: 1Type: ApplicationFiled: November 24, 2003Publication date: June 10, 2004Applicant: WyethInventors: Chris P. Miller, Michael D. Collini, Bach D. Tran, Arthur A. Santilli
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Patent number: 6743810Abstract: Indol-3-yl derivatives of the general formula I in which A, B, X, R1, R2, R3, R4, R5, n and m are as defined in patent claim 1, and their physiologically acceptable salts or solvates are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumours, osteoporosis, rheumatic arthritis, macular degenerative disease, diabetic retinopathy, infections and restenosis after angioplasty or in pathological processes maintained or propagated by angiogenesis.Type: GrantFiled: August 9, 2002Date of Patent: June 1, 2004Assignee: Merck Patent GmbHInventors: Matthias Wiesner, Simon Goodman, Rudolf Gottschlich
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Publication number: 20040058977Abstract: The present invention relates to sulfonyl-containing 2,3-diarylindole, especially to new compounds of general Formula, to a preparation method for their preparation, to pharmaceutical compositions containing said compound, and to the medical use thereof in the treatment of diseases relating to the inhibition of cyclooxygenase-2 (COX-2).Type: ApplicationFiled: September 16, 2002Publication date: March 25, 2004Inventors: Zongru Guo, Guifang Cheng, Fengming Chu
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Publication number: 20040053983Abstract: The present invention provides compounds of formula (I) wherein R, Z, Y, W, R5, V, and X are as defined in the description, and pharmaceutically acceptable salts thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of formula (I) and their pharmaceutically acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.Type: ApplicationFiled: February 21, 2003Publication date: March 18, 2004Inventors: Nicole Chantel Barvian, Patrick Michael O.Brien, William Chester Patt, Joseph Armand Picard, Drago Robert Sliskovic
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Patent number: 6552065Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.Type: GrantFiled: August 31, 2001Date of Patent: April 22, 2003Assignee: Novartis AGInventors: Stacy William Remiszewski, Kenneth Walter Bair, Richard William Versace, Lawrence Blas Perez, Michael Alan Green, Lidia Cristina Sambucetti, Sushil Sharma
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Patent number: 6486153Abstract: A class of tryptamine analogues bearing an optionally substituted phenyl nucleus at the 2-position are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse neurological conditions, including psychotic disorders such as schizophrenia.Type: GrantFiled: March 3, 2000Date of Patent: November 26, 2002Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Steven Michael Hutchins, Stephen John Lewis, Michael Rowley, Adrian Leonard Smith, Graeme Irvine Stevenson
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Patent number: 6458824Abstract: The present invention provides a solid preparation comprising a crystal of [3-[(2R)-[[(2R)-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1H-indol-7-yloxy]acetic acid (Compound A), especially a crystal of Compound A having a particle size of not larger than 100 &mgr;m at the cumulative weight distribution value of 50%, and not larger than 200 &mgr;m at the cumulative weight distribution value of 95%, preferably a solid preparation having the excellent stability and the content uniformity of Compound A, which is prepared by preparing granules of the crystal of Compound A with fillers, disintegrants and binders, and then followed by mixing said granules with external excipients.Type: GrantFiled: September 14, 2000Date of Patent: October 1, 2002Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Motokazu Iwata, Teruaki Kuriyama, Megumi Fujita, Keiichi Fujiwara, Shiro Kato, Hiroshi Harada, Akihito Fujii, Osamu Odai, Hitoshi Kawashima
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Publication number: 20020099054Abstract: Benzimidazole derivatives of Formula I or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection 1Type: ApplicationFiled: October 25, 2001Publication date: July 25, 2002Applicant: Warner-Lambert CompanyInventors: David Thomas Connor, Shelly Ann Glase, Terri Stoeber Purchase, Bruce David Roth, Bharat Kalidas Trivedi
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Patent number: 6403577Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.Type: GrantFiled: November 17, 1993Date of Patent: June 11, 2002Assignee: Eli Lilly and CompanyInventors: Sung Y. Cho, Thomas A. Crowell, Bruce D. Gitter, Philip A. Hipskind, J. Jeffry Howbert, Joseph H. Krushinski, Jr., Karen L. Lobb, Brian S. Muehl, James A. Nixon
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Patent number: 6358994Abstract: This invention provides compounds of the Formula I: which are useful as tachykinin receptor antagonists. This invention also provides methods employing these compounds, as well as pharmaceutical formulations comprising these compounds.Type: GrantFiled: January 27, 2000Date of Patent: March 19, 2002Assignee: Eli Lilly and CompanyInventors: James E Fritz, Philip A Hipskind, Stephen W Kaldor, Karen L Lobb, James A Nixon
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Patent number: 6358943Abstract: This invention provides compounds of the formula wherein R1, R2, R3, R4, R5, R6, R7, X, n and Y, are as defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods utilizing the compounds for treating or preventing disease states or syndromes which are caused or associated with an estrogen deficiency or an excess of estrogen utilizing these compounds.Type: GrantFiled: February 25, 2000Date of Patent: March 19, 2002Assignee: American Home Products CorporationInventor: John W. Ullrich