Carbocyclic Ring Containing Patents (Class 546/191)
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Publication number: 20090054451Abstract: The present invention is directed to novel piperidine derivatives and to the use of piperidine derivatives of formula I as agonists of chemokine receptor activity.Type: ApplicationFiled: August 4, 2008Publication date: February 26, 2009Applicant: Euroscreen S.A.Inventors: Jacques Huck, Frederic Ooms, Christian Tyrchan, Hamid R. Hoveyda
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Patent number: 7482363Abstract: The present invention provides a compound of formula (I), wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.Type: GrantFiled: March 17, 2003Date of Patent: January 27, 2009Assignee: AstraZeneca ABInventors: Hitesh Sanganee, Brian Springthorpe
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Publication number: 20080269250Abstract: The invention provides compounds of formula (I) wherein the substituents are as defined in the description, processes and intermediates for their preparation and their use as pharmaceuticals.Type: ApplicationFiled: February 20, 2006Publication date: October 30, 2008Inventors: Ralf Glatthar, Thomas J. Troxler, Thomas Zoller, Joachim Nozulak
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Publication number: 20080255345Abstract: The invention relates to iRNA agents that preferably include a modification that targets CC chemokine receptor 5 (CCR5). The invention also relates to methods of making and using such modified iRNA agents.Type: ApplicationFiled: November 21, 2007Publication date: October 16, 2008Inventors: Muthiah Manoharan, Kallanthottahil G. Rajeev
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Publication number: 20080249111Abstract: Disclosed are compounds of formula I: wherein R1, R2, R3 and X are as defined herein, in free or salt form, which are useful as CCR5 inhibitors, e.g. in the prevention or treatment of disorders mediated by interactions between chemokine receptors and their ligands.Type: ApplicationFiled: May 2, 2008Publication date: October 9, 2008Inventors: Rainer ALBERT, Nigel Graham Cooke, Gebhard Thoma, Christian Bruns, Francois Nuninger, Markus Streiff, Hans-Gunter Zerwes
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Patent number: 7368461Abstract: NK2R binding compounds in accord with structural diagram I useful for the treatment or prevention of OAB or UI in mammals, particularly humans are disclosed: wherein in said compounds D, A, R1, R3 and R4 are as defined in the specification. Pharmaceutically-advantageous salts of the compounds, methods of use of the compounds, either alone or in combination with other pharmacological agents, and pharmaceutical compositions useful in practicing the methods of the invention are also disclosed.Type: GrantFiled: November 1, 2002Date of Patent: May 6, 2008Assignee: AstraZeneca ABInventors: Russell Bialecki, Cathy Dantzman, Keith Herzog
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Patent number: 7361755Abstract: This invention pertains to a novel process for preparing sterically hindered N-substituted alkyloxyamines from alkenes by the transition-metal-catalyzed reaction of a intermediate alkylborane with a sterically hindered nitroxyl radical.Type: GrantFiled: December 12, 2002Date of Patent: April 22, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Stephen Daniel Pastor, Sai Ping Shum
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Patent number: 7238811Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.Type: GrantFiled: May 13, 2003Date of Patent: July 3, 2007Assignee: AstraZeneca ABInventors: Aaron Rigby, Hitesh Sanganee, Brian Springthorpe, Louise Lawrence
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Patent number: 7199243Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: GrantFiled: November 24, 2003Date of Patent: April 3, 2007Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Scott W. Bagley, Thomas A. Brandt, Robert W. Dugger, William A. Hada, Cheryl M. Hayward, Zhengyu Liu
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Patent number: 7186732Abstract: Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: August 6, 2001Date of Patent: March 6, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Richard Apodaca, Nicholas I. Carruthers, Curt A. Dvorak, Dale A. Rudolph, Chandravadan R. Shah, Wei Xiao
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Patent number: 7122675Abstract: Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.Type: GrantFiled: August 1, 2002Date of Patent: October 17, 2006Assignee: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Theodros Asberom, Dmitri A. Pissarnitski
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Patent number: 7005436Abstract: Novel heterocyclo compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.Type: GrantFiled: April 16, 2003Date of Patent: February 28, 2006Assignees: Bristol Myers Squibb Company, Icagen, Inc.Inventors: John Lloyd, Yoon T. Jeon, Heather Finlay, Lin Yan, Michael F. Gross, Serge Beaudoin
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Patent number: 6900326Abstract: A method of producing an N-alkoxycarbonylpiperidine derivative, comprising reacting an N-aralkylpiperidine derivative represented by the following general formula (1): wherein R1 represents an aralkyl group which may have a substituent, with a mesyl halide in the presence of a base, thereby obtaining a mesylated product represented by the following general formula (2): wherein R1 represents an aralkyl group which may have a substituent and Ms represents a mesyl group, and reacting the mesylated product with a dicarbonate represented by the following general formula (3): wherein R4 represents an alkyl group, in the presence of hydrogen and a catalyst containing palladium, thereby obtaining an N-alkoxycarbonylpiperidine derivative represented by the following general formula (4): wherein R4 represents an alkyl group and Ms represents a mesyl group.Type: GrantFiled: September 17, 2003Date of Patent: May 31, 2005Assignee: Yuki Gosei Kogyo Co., Ltd.Inventor: Kiyono Nakagawa
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Patent number: 6878723Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.Type: GrantFiled: April 6, 2000Date of Patent: April 12, 2005Assignees: Institut National de la Sante et de la rescherche Medicale (INSERM), BioprojetInventors: Denis Danvy, Thierry Monteil, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Nadine Noel, Claude Gros, Olivier Chamard, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Serge Piettre
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Patent number: 6841668Abstract: Sterically hindered N-substituted aryloxyamines are prepared by the Keggin polyoxometalate or the transition metal substituted polyoxometalate (TMS-POM) catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitoxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.Type: GrantFiled: April 4, 2003Date of Patent: January 11, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Deborah Judd, Sai P. Shum, Stephen D. Pastor
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Patent number: 6831089Abstract: The present invention discloses compounds, which are novel muscarinic receptor antagonists, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such muscarinic receptor antagonists as well as methods for using them to treat cognitive disorders such as Alzheimer's disease.Type: GrantFiled: October 8, 2002Date of Patent: December 14, 2004Assignee: Schering CorporationInventors: Yuguang Wang, Samuel Chackalamannil
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Patent number: 6780863Abstract: Compounds of which the following are exemplary: These have tryptase-inhibiting activity and are useful for the treatment of inflammatory and allergic disease conditions.Type: GrantFiled: October 30, 2000Date of Patent: August 24, 2004Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Ralf Anderskewitz, Christine Braun, Rainer Hamm, Bernd Disse, Hans Michael Jennewein, Georg Speck
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Patent number: 6743808Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7-membered ring; R8 is hydrogen or alkyl; hType: GrantFiled: April 14, 2000Date of Patent: June 1, 2004Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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Patent number: 6737527Abstract: The present invention relates to 4-formylamino-N-methylpiperidine derivatives of the formula (I) where the variables are as defined in the Description, to a process for preparing these piperidine derivatives, to the use of these piperidine derivatives of the invention, or prepared according to the invention, for stabilizing organic material, in particular for stabilizing plastics or coating materials, and also to the use of these piperidine derivatives of the invention, or prepared according to the invention, as light stabilizers or stabilizers for wood surfaces. The present invention further relates to stabilized organic material which comprises these piperidine derivatives of the invention or prepared according to the invention.Type: GrantFiled: September 27, 2002Date of Patent: May 18, 2004Assignee: BASF AktiengesellschaftInventors: Sylke Haremza, Jürgen Krockenberger, Manfred Appel, Hubert Trauth, Alexander Aumüller
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Patent number: 6723729Abstract: Novel compounds are provided having the formula and salt thereof, where R1 is hydrogen, an alkyl, aralkyl, hydroxymethyl, carboxymethyl acyloxymethyl or trialkylsilyl group, or a group —CH2NR3R4 where N is a linking nitrogen atom and where (a) R3 and R4 are independently selected from hydrogen and alkyl, alkenyl, hydroxyalkyl and alkoxyalkyl groups; (b) R3 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group, and R4 is —COR5 where R5 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group; or (c) R3 and R4 taken together with the linking nitrogen atom form a saturated 3- to 7-member heterocyclic group. These compounds are useful intermediates in a process to prepare camptothecin derivatives including the anti-cancer drug irinotecan.Type: GrantFiled: April 16, 2003Date of Patent: April 20, 2004Assignee: Pharmacia and Upjohn CompanyInventor: Kevin E. Henegar
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Patent number: 6693202Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.Type: GrantFiled: August 25, 2000Date of Patent: February 17, 2004Assignee: Theravance, Inc.Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
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Patent number: 6642228Abstract: There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R1 is hydrogen etc., B is bond, or B—N—R1 forms a ring structure and is piperidine etc., n is 0, 1, etc., A is trimethylene, butylene, etc., Q is piperidine, isoindoline, etc.], or pharmacologically acceptable acid addition salts thereof, and &agr;1B adrenoceptor antagonists composed of these substances. The invented compounds are antagonists having high affinity for &agr;1B adrenoceptor and are useful as pharmaceutical agents for use in prophylaxis/therapy of diseases (e.g., hypertension) in which &agr;1B adrenoceptor is involved or as pharmacological tools for elucidation of physiological activities mediated by &agr;1B adrenoceptor.Type: GrantFiled: April 13, 2001Date of Patent: November 4, 2003Assignee: Toray Industries, Inc.Inventors: Ryoji Hayashi, Eiji Ohmori, Masafumi Isogaya, Mitsuhiro Moriwaki, Hiroki Kumagai
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Patent number: 6627629Abstract: 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 29, 2001Date of Patent: September 30, 2003Assignee: Bristol-Myers Squibb PharmaInventors: Soo S. Ko, James R. Pruitt, Dean A. Wacker, Douglas G. Batt
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Patent number: 6613769Abstract: The invention relates to bifunctional tryptase inhibitors of formula (I) wherein H1 and H2 comprise a Q group and L is a linker of formula and the conformation of the H1, H2 and L groups is such that the groups are separated by a distance of from 20 to 45 Å. Pharmaceutical compositions and crystal forms of the compounds are described in addition to methods for producing and identifying such compounds, as well as the use of such compounds in methods of treating allergic and inflammatory diseases.Type: GrantFiled: January 22, 2001Date of Patent: September 2, 2003Assignees: Max-Planck-Gesellschaft zur Föderung der Wissenschaften. e.V., Altana Pharma AGInventors: Wolfram Bode, Luis Moroder, Pedro Jose Barbosa Pereira, Andreas Bergner, Robert Huber, Christian Sommerhoff, Norbert Schaschke, Thomas Bär, Thomas Martin, Josef Stadlwieser, Wolf-Rüdiger Ulrich, Andreas Dominik, Ulrich Thibaut, Daniela Bundschuh, Rolf Beume, Karl-Josef Goebel
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Patent number: 6605642Abstract: The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.Type: GrantFiled: March 8, 2001Date of Patent: August 12, 2003Assignee: City of HopeInventors: Samuel Rahbar, Iraj Lalezari
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Patent number: 6605635Abstract: N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)benzyl aromatic sulfonamides and N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)phenyl aromatic sulfonamides compounds in accordance with the animal test, are active in the prevention and the treatment of cardiac arrhythmia. These compounds are prepared as corresponding diamines by the condensation of optionally substituted aromatic sulfochlorides with p-hydroxybenzylamine, p-aminophenol, or the like, which followed by the Mannich reaction of the resulted corresponding aromatic sulfamides with formaldehyde and secondary amines; or directly obtained by the reaction of the aromatic sulfamides with 4-amino-2,6-bis-disubstituted aminomethylphenol. Subsequently, the diamines are reacted with various acids to provide their salts.Type: GrantFiled: June 7, 2002Date of Patent: August 12, 2003Assignee: Shanghai Institute of Materia Medica Chinese Academy of ScienceInventors: Donglu Bai, Weizhou Chen, Yunxin Bu, Yiping Wang, Yueli Dong, Aili Kang
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Patent number: 6602886Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.Type: GrantFiled: June 21, 2002Date of Patent: August 5, 2003Assignee: Warner-Lambert CompanyInventors: Michael Huai Gu Chen, Fu-Zon Chung, Helen Tsenwhei Lee
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Patent number: 6602885Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl for the treatment of HIV, solid organ transplant rejection, graft v.Type: GrantFiled: November 8, 2001Date of Patent: August 5, 2003Assignee: Schering CorporationInventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin
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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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Patent number: 6545156Abstract: Oligomeric compounds and methods of making the compounds having the formula: T&Parenopenst;M—F&Parenclosest;i&Parenopenst;M—F′&Parenclosest;jM (III) wherein i and j are integers from about 0 to 300 and the sum of i and j is greater than 2, wherein the units F, F′ and T are derived from one or more multi-functional carbonyl compounds of general structure DO—CO—CRaRb—(—CRcRd—)n—NH—(Y)m—CO—OD (IV) wherein n is an integer from 1 to 15, m is either 0 or 1; Ra, Rb, Rc, and Rd, are each a hydrogen or a hydrocarbyl group; Y is CO—(CReRf)p, wherein Re and Rf are each a hydrogen or hydrocarbyl group and p is zero or an integer from 1 to 20 or CO—C6H4—, D is a hydrocarbyl group, and M is a moiety derived from one or more diamino or dihydroxy compounds that contain a 4-aminopiperidine radical.Type: GrantFiled: November 3, 2000Date of Patent: April 8, 2003Assignee: Cytec Technology Corp.Inventors: Thomas Patrick Sassi, Ram Baboo Gupta
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Patent number: 6525070Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.Type: GrantFiled: April 6, 2001Date of Patent: February 25, 2003Assignee: AstraZeneca ABInventors: Aaron Rigby, Hitesh Sanganee, Brian Springthorpe, Louise Lawrence
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Patent number: 6518283Abstract: Squaric acid Derivatives of formula (1) are described: wherein R1 is an integrin binding group; R2 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic chain; R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune of inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.Type: GrantFiled: May 25, 2000Date of Patent: February 11, 2003Assignee: Celltech R&D LimitedInventors: Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
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Publication number: 20030027822Abstract: The invention provides sodium channel modulating compounds of formula I: 1Type: ApplicationFiled: August 30, 2001Publication date: February 6, 2003Inventors: Jason P. Chinn, Seok-Ki Choi, Paul R. Fatheree, Daniel Marquess, S. Derek Turner
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Patent number: 6511993Abstract: Compounds of formula (I) and pharmaceutically-acceptable derivatives thereof, are matrix metalloprotease inhibitors, useful in treatment of conditions mediated by matrix metalloproteases, such as chronic dermal ulcers.Type: GrantFiled: June 2, 2000Date of Patent: January 28, 2003Inventors: Kevin Neil Dack, Michael Jonathan Fray, Gavin Alistair Whitlock, Mark Llewellyn Lewis, Nicholas Murray Thomson
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Publication number: 20030013873Abstract: Secondary amines of the formula 1Type: ApplicationFiled: June 19, 2002Publication date: January 16, 2003Inventors: Peter Neumann, Johann-Peter Melder, Christoph Benisch, Arthur Hohn, Joachim Pfeffinger
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Patent number: 6495568Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: December 17, 2002Assignee: Warner-Lambert CompanyInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6455529Abstract: Compounds of the formula I in which R1, R2 and R3 have the stated meanings, and their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be used for the treatment of thromboses, osteoporoses, oncoses, stroke, myocardial infarct, ischemias, inflammations, arteriosclerosis and osteolytic disorders.Type: GrantFiled: May 3, 1996Date of Patent: September 24, 2002Assignee: Merck Patent Gesellschaft mit beschraenkter HaftungInventors: Joachim Gante, Hörst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 6444821Abstract: Monohydrate and trihydrate crystals of N-(2-(4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidino) ethyl)-1-formyl-4-piperidinecarboxamide hydrochloride having excellent stability.Type: GrantFiled: February 6, 2001Date of Patent: September 3, 2002Assignee: Ajinomoto Co., Inc.Inventors: Akiko Fujii, Mie Kubo, Tomoya Yamamoto, Jiro Shimada, Ryuichi Mihara, Hirokazu Naora, Koji Asai
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Patent number: 6441244Abstract: The invention relates to new compounds of the formula (I) in which R is phenyl, C1-4alkyl-, C1-4alkoxy- or halogen-substituted phenyl, naphthyl or an aromatic ring containing heteroatoms; X is O or S; R1 and R2 are each a methyl radical or R1 and R2 together are a C4-8alkylene radical; Y is hydroxyl, C1-12alkoxy, C1-4alkylamino, di-C1-4alkylamino or a piperidine or morpholine ring that is attached by its nitrogen atom; to a process for preparing them and to their use as photoinitiators and/or photosensitizers.Type: GrantFiled: July 12, 2001Date of Patent: August 27, 2002Assignee: Clariant Finance (BVI) LimitedInventors: Lajos Avar, René Bär, Victor Sanahuja
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Patent number: 6440440Abstract: This invention concerns compounds of formula. stereochemically isomeric forms thereof, acid or base addition salts thereof, N-oxides thereof, or quaternary ammonium derivatives thereof, wherein the dotted line is an optional bond; X is a direct bond when the dotted line represents a bond, or X is hydrogen or hydroxy, when the dotted line does not represent a bond; R1, R2, R5 and R6 are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, —SO3H, and the like; R3 and R4 are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, nitro, amino, cyano, trifluoromethyl, or trifluoromethoxy; L is a radical of formula wherein A1 is a direct bond or C1-6alkanediyl; A2 is C2-6alkanediyl; and R7 to R11 are hydrogen, C1-6alkyl, aminoC1-6alkyl and the like; having biocidal properties; their preparation, compositions containing them and their use as a biocide.Type: GrantFiled: September 22, 2000Date of Patent: August 27, 2002Inventors: Lieven Meerpoel, Mark Arthur Josepha Van der Flaas, Louis Jozef Elisabeth Van Der Veken, Jan Heeres
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Patent number: 6440996Abstract: The invention provides compounds of formula (I): X—L—X1 (I) wherein X and X1 are substituted piperidine, cyclohexane, or tetrahydropyran rings, and L is a linking group between X and X1; as well a pharmaceutical composition comprising a compound of formula I; intermediates and methods useful for preparing a compound of formula I; and therapeutic methods for treating drug addiction, Parkinson's disease, depression, or a disease wherein the administration of cocaine is indicated, comprising administering a compound of formula I or a pharmaceutically acceptable salt thereof to a mammal in need of such treatment.Type: GrantFiled: October 7, 1999Date of Patent: August 27, 2002Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Gian Luca Araldi, Amir P. Tamiz
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Patent number: 6433178Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.Type: GrantFiled: June 4, 2001Date of Patent: August 13, 2002Assignee: Warner-Lambert CompanyInventors: Michael Huai Gu Chen, Fu-Zon Chung, Helen Tsenwhei Lee
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Patent number: 6387930Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein X is —C(R13)2—, —C(R13)(R19)—, —C(O)—, —O—, —NH—, —N(alkyl)—, R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl for the treatment of HIV, solid organ transplant rejection, graft v.Type: GrantFiled: May 1, 2000Date of Patent: May 14, 2002Assignee: Schering CorporationInventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin
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Patent number: 6387931Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: May 14, 2002Assignee: Pfizer INCInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6376584Abstract: Hindered amines substituted on the N-atom with an hydroxy-substituted alkoxy moiety are particularly effective in stabilizing organic polymer compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not otherwise attainable.Type: GrantFiled: February 27, 2001Date of Patent: April 23, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: James Peter Galbo, Gerald A. Capocci, Nancy N. Cliff, Robert E. Detlefsen, Michael P. DiFazio, Ramanathan Ravichandran, Peter Solera, Christophe Bulliard
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Patent number: 6348597Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.Type: GrantFiled: April 4, 2001Date of Patent: February 19, 2002Assignee: Merrell Pharmaceuticals, Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Publication number: 20020010173Abstract: The invention relates to new compounds of general formula I 1Type: ApplicationFiled: July 2, 2001Publication date: January 24, 2002Inventor: Sven Luettke
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Patent number: 6331545Abstract: 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: December 17, 1999Date of Patent: December 18, 2001Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 6326369Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.Type: GrantFiled: July 6, 1999Date of Patent: December 4, 2001Assignee: Takeda Chemicals Industries, Ltd.Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
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Patent number: RE38257Abstract: A piperidine compound of the formula (I): wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH2)n, which may be substituted, in which n is 0 or an integer of 1 to 10, —CH≡CH—, —C≡C—, —O—, —S—, —NH—, —N(COCH3)—, —N(COOC2H5)—, —N(CHO)—, —N(CH3)—, —CO—, —SO—, or —SO2—; Y is —CH≡CH—, —CH2CH2—, —CH2CO—, —O—, —S—, —NH—, —OCH2—, —SCH2—, —NHCH2—, —CH(OH)CH2— or —CH(OH)CH(OH)—; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of tType: GrantFiled: February 10, 1999Date of Patent: September 23, 2003Assignee: Ajinomoto Co., Inc.Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura