Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/224)
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Publication number: 20080312237Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: July 18, 2008Publication date: December 18, 2008Inventors: Michael G. Kelly, Satyanarayana Janagani, Ravindra B. Upasani
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Publication number: 20080280951Abstract: The invention provides N-{2-[((2S)-3-{[1-(4-chlorobenzyl)piperidin-4-yl]amino}-2-hydroxy-2-methyl-propyl)oxy]-4-hydroxyphenyl}acetamide furoate or a solvate thereof, pharmaceutical compositions containing the salt or solvate and use of the salt or solvate in therapy.Type: ApplicationFiled: July 31, 2006Publication date: November 13, 2008Applicant: ASTRAZENECA ABInventors: Julien Giovannini, Bo-Goran Josefsson
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Publication number: 20080249132Abstract: The present invention relates to the compound of formula (I) or pharmaceutically acceptable salts or solvates thereof, process for their preparation, their use in the treatment of conditions mediated by tachykinins and pharmaceutical compositions containing them.Type: ApplicationFiled: July 14, 2006Publication date: October 9, 2008Inventor: Silvia Martinucci
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Publication number: 20080227817Abstract: The invention provides N-{2-[((2S)-3-{[1-(4-chlorobenzyl)piperidin-4-yl]amino}-2-hydroxy-2-methyl-propyl)oxy]-4-hydroxyphenyl}acetamide benzoate or a solvate thereof, pharmaceutical compositions containing the salt or solvate and use of the salt or solvate in therapy.Type: ApplicationFiled: July 31, 2006Publication date: September 18, 2008Applicant: ASTRAZENECA ABInventors: Julien Giovannini, Bo-Goran Josefsson
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Publication number: 20080221100Abstract: Disclosed are urea compounds, stereoisomer, or pharmaceutical acceptable salt thereof, and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.Type: ApplicationFiled: October 19, 2007Publication date: September 11, 2008Inventors: Richard D. Gless, Sampath Kumar Anandan, Bhaskar R. Aavula
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Process for the Preparation of N-(4-Piperidinyl)-N-Ethyl-Phenylacetamides from N-Boc-4-Oxopiperidine
Publication number: 20080214824Abstract: The present invention concerns a process for the preparation of an N-(4-piperidinyl)-N-ethyl-phenylacetamide of formula (I); wherein R1 and R2 are independently selected from the group comprising: hydrogen, halogen, C1-4 alkyl, C1-4alkoxy, cyano and S(O)2(C1-4 alkyl).Type: ApplicationFiled: December 14, 2005Publication date: September 4, 2008Inventors: Emma Anderson, John Pavey -
Publication number: 20080194632Abstract: The invention provides compounds of formula wherein m, R1, R2 and R3 are as defined in the specification, salts and polymorphic forms thereof, processes for the preparation of the compounds, salts and polymorphs, pharmaceutical compositions containing these compounds, salts and/or polymorphic forms and their use in therapy.Type: ApplicationFiled: July 31, 2006Publication date: August 14, 2008Applicant: ASTRAZENECA ABInventors: Julien Giovannini, Bo-Goran Josefsson, Marguerite Mensonides-Harsema, Hakan Schulz
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Patent number: 7405307Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: September 13, 2007Date of Patent: July 29, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
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Patent number: 7381721Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: March 17, 2003Date of Patent: June 3, 2008Assignee: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Patent number: 7381735Abstract: The subject invention concerns analogs of fentanyl opioids. The subject invention also concerns methods for synthesizing the compounds of the invention. The invention also concerns methods for treating pain in a patient by administering a compound of the invention to a person in need of such treatment.Type: GrantFiled: October 24, 2005Date of Patent: June 3, 2008Assignee: Aryx TherapeuticsInventor: Pascal Druzgala
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Patent number: 7368443Abstract: The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: which are used to treat diseases of the central nervous system, drug abuse, and withdrawal therefrom as well as treating eating disorders.Type: GrantFiled: March 31, 2004Date of Patent: May 6, 2008Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Linda Dwoskin, Marlon D. Jones, Dennis Keith Miller, Seth Davin Norholm, Guangrong Zheng, Sairam Krishamurthy
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Patent number: 7361666Abstract: 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: April 11, 2002Date of Patent: April 22, 2008Assignee: Sepracor, Inc.Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
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Patent number: 7358359Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: July 22, 2005Date of Patent: April 15, 2008Assignee: University of WashingtonInventors: Niels H. Andersen, Jason Bowman
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Patent number: 7320990Abstract: The invention provides a crystalline naphthalene-1,5-disulfonic acid salt of biphenyl-2-ylcarbamic acid 1-{9-[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydro-quinolin-5 -yl)ethylamino]nonyl}piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.Type: GrantFiled: February 11, 2005Date of Patent: January 22, 2008Assignee: Theravance, Inc.Inventors: Robert Chao, Miroslav Rapta, Pierre-Jean Colson, Junning Lee
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Patent number: 7282509Abstract: The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.Type: GrantFiled: March 23, 2005Date of Patent: October 16, 2007Assignee: Aryx TherapeuticsInventors: Ian Irwin, Monica Palme, Cyrus Becker, Courtney Rubens, Pascal Druzgala
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Patent number: 7223780Abstract: The present invention is directed to the compound of formula I which is useful for inhibiting the activity of blood clotting enzyme Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically treating a patient suffering from, or subject to, a disease state associated with a cardiovascular disorder.Type: GrantFiled: May 19, 2004Date of Patent: May 29, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volker Laux, Armin Bauer, Michael Wagner
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Patent number: 7208496Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.Type: GrantFiled: June 7, 2004Date of Patent: April 24, 2007Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih Elzein, Tim Marquart
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Patent number: 7199245Abstract: The present invention relates to selected 4-imino-N-alkoxy-polyalkyl-peperidine compounds preparation, a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 4-imino-N-alkoxy-polyalkyl-piperidine compound. Further aspects of the present invention are a process for polymerizing ethylenically unsaturated monomers, and the use of 4-imino-N-alkoxy-polyalkyl-piperidine compounds for controlled polymerization.Type: GrantFiled: June 4, 2002Date of Patent: April 3, 2007Assignee: Ciba Specialty Chemicals Corp.Inventors: Peter Nesvadba, Tobias Hintermann, Andreas Kramer, Marie-Odile Zink, Lucienne Bugnon
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Patent number: 7141671Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: February 13, 2004Date of Patent: November 28, 2006Assignee: Theravance, Inc.Inventors: Mathai Mammen, Sarah Dunham, Adam Hughes, Tae Weon Lee, Craig Husfeld, Eric Stangeland, Yan Chen
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Patent number: 7126010Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.Type: GrantFiled: January 21, 2005Date of Patent: October 24, 2006Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Dean A Wacker, John V Duncia, Joseph B Santella, III., Daniel S Gardner
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Patent number: 7067533Abstract: The present invention relates to an aminophenoxyacetamide derivative of the formula (I): wherein R1 to R4 are, independent from each other, a hydrogen atom or an optionally substituted alkyl group; E1 is —NR4—; and E2 is an oxygen atom or —NR10—; Q is the group —X—Y-Q?, wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and Y is selected from a group comprising C?O, NHC(?), and C(?O)NH, and Q? is a hydrogen atom or a phenyl or pyridyl group which may be substituted; and pharmaceutically acceptable salts thereof. The present invention further relates to compositions comprising compounds of the formula (I) and methods of using said compounds for treating cerebral functional disorders and cerebral organic disorders.Type: GrantFiled: April 13, 2001Date of Patent: June 27, 2006Assignee: Daiichi Asubio Pharma Co., Ltd.Inventors: Naohiro Takemoto, Hirokazu Annoura, Norihito Murayama
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Patent number: 7049326Abstract: A method for modifying at least one non-ester-containing parent compound, and the compounds produced using such method, which compounds are deployed to temporarily incapacitate at least one subject are disclosed. The modified compounds are rapidly metabolized to inactive and non-toxic metabolites when exposure to the modified compounds is halted.Type: GrantFiled: November 18, 2002Date of Patent: May 23, 2006Assignee: The University of ToledoInventor: Paul W. Erhardt
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Patent number: 7026510Abstract: (R)-Enantiomers of quaternary ammonium salts of general formula (I) are described: where R, R1, R2, R3, X and Z are as defined in the description. The process for their preparation and pharmaceutical preparations thereof are also described. The quaternary salts of the invention are useful in the inhibition of chemotaxis of neutrophils and monocytes induced by the fraction C5a of the complement and are used in the treatment of psoriasis, pemphigus and pemphigoid, rheumatoid arthritis, intestinal chronic inflammatory pathologies including ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, cystic fibrosis, chronic obstructive pulmonary disease and glomerulonephritis. The compounds of the invention are advantageously used in the prevention and the treatment of injury caused by ischemia and reperfusion.Type: GrantFiled: September 25, 2002Date of Patent: April 11, 2006Assignee: Dompé S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta
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Patent number: 7022716Abstract: This invention provides compounds of Formula I having the structure wherein, R1, R2, R3, R4, R5, T, T1, T2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.Type: GrantFiled: December 27, 2002Date of Patent: April 4, 2006Assignee: WyethInventors: Baihua Hu, Fuk-Wah Sum, Michael Sotirios Malamas
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Patent number: 7019007Abstract: The invention provides compounds of Formula (I): wherein: R1–R4, A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.Type: GrantFiled: November 27, 2002Date of Patent: March 28, 2006Assignee: Syntex (U.S.A.) LLCInventors: Daisy Joe Du Bois, Beihan Wang
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Patent number: 7015235Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 25, 2002Date of Patent: March 21, 2006Assignee: Merck & Co., Inc.Inventors: Mark T. Goulet, Ravi P. Nargund, Iyassu K. Sebhat, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner, Zhixiong Ye, Jonathan R. Young, Raman K. Bakshi
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Patent number: 7012084Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 25, 2002Date of Patent: March 14, 2006Assignee: Merck & Co., Inc.Inventors: Mark T. Goulet, Ravi P. Nargund, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner
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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: 7001915Abstract: The subject invention encompasses compounds of the formula: wherein R1, R2, and R3 are as defined herein. The subject invention also concerns methods for synthesizing the compounds of the invention. The invention also concerns compositions comprising the above compounds as well as methods for treating pain in a patient, where the method comprises administering a compound of the invention to a patient in need of such treatment.Type: GrantFiled: February 2, 2004Date of Patent: February 21, 2006Assignee: ARYx Therapeutics, Inc.Inventor: Pascal Druzgala
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Patent number: 6989402Abstract: New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR?R?) or an acylsulphonamide (CONHSO2R?) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR?R?). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H).Type: GrantFiled: December 23, 1999Date of Patent: January 24, 2006Assignee: Karo Bio ABInventors: Jon Hangeland, Minsheng Zhang, Yolanda Caringal, Denis Ryono, Yi-Lin Li, Johan Malm, Ye Liu, Neeraj Garg, Chris Litten, Ana Maria Garcia Collazo, Konrad Koehler
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Patent number: 6974825Abstract: Compounds of general formula (I) wherein m is 0 or 1, and n is 1 or 2; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: July 29, 2003Date of Patent: December 13, 2005Assignee: AstraZeneca Canada Inc.Inventors: Benjamin Pelcman, Edward Roberts
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Patent number: 6960602Abstract: The invention provides a compound of formula (I): wherein R1, R2, R3, R3a, R4, R4a, R5, and R6 are as defined; or a pharmaceutically acceptable salt thereof or a solvate thereof; compositions containing these compounds, processes for preparing them and their use as modulators of chemokine activity (especially CCR5 activity)Type: GrantFiled: March 19, 2002Date of Patent: November 1, 2005Assignee: AstraZeneca ABInventors: Jeremy Burrows, John Cumming
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Patent number: 6943177Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating disorders.Type: GrantFiled: August 30, 2002Date of Patent: September 13, 2005Assignee: University of Kentucky Research FoundationInventors: Linda P. Dwoskin, Peter A. Crooks, Marlon D. Jones
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Patent number: 6916929Abstract: The invention relates to a process for preparing a 4-alkoxycarbonylamino-1-benzyl-4-phenylpiperidine of formula (I) via hydrolysis of 1-benzyl-4-cyano-4-phenylpiperidine (II) in acidic medium and treatment of the 1-benzyl-4-phenyl-4-piperidinecarboxamide (III) thus obtained with bromine in the presence of an alkali metal alkoxide. The invention also relates to a process for preparing 4-methylamino-4-phenylpiperidine from compound (II).Type: GrantFiled: July 15, 2002Date of Patent: July 12, 2005Assignee: Sanofi-SynthelaboInventors: Gilles Anne-Archard, Patrick Gros-Claude
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Patent number: 6900228Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.Type: GrantFiled: March 9, 1999Date of Patent: May 31, 2005Assignee: Research Triangle InstituteInventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
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Patent number: 6878712Abstract: A compound of formula (I): wherein: Ring A is a nitrogen linked mono or bicyclic heterocyclic ring as defined within; R1 and R2 are independently C1-3alkyl optionally substituted by fluoro or chloro; or R1 and R2 together with the carbon atom to which they are attached, form a C3-5cycloalkyl ring optionally substituted by fluoro; R3 is defined within; and n is 0-5; wherein the values of R3 may be the same or different; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.Type: GrantFiled: August 30, 2000Date of Patent: April 12, 2005Assignee: AstraZeneca ABInventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows, David Stephen Clarke
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Patent number: 6875777Abstract: The present application is directed to compounds having the structure of Formula I: where R1 is phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl or trazolyl, each optionally substituted by a straight or branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, or iodo; where Ra and Rb are independently selected from hydrogen, a straight or branched C1-C6 alkyl, NO2, C1-C6 alkoxy, chloro, fluoro, bromo, or iodo; and where X is O or CH3. The compounds may be incorporated into pharmaceutical compositions and administered to patients as a treatment for pain, gastrointestinal disorders, spinal injury, or disorders of the sympathetic nervous system.Type: GrantFiled: December 15, 2000Date of Patent: April 5, 2005Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole
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Patent number: 6867221Abstract: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.Type: GrantFiled: July 10, 2002Date of Patent: March 15, 2005Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Shunji Takemura, Takeshi Doi, Yoshinori Kyotani, Masao Ohkuchi
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Patent number: 6864380Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.Type: GrantFiled: July 3, 2003Date of Patent: March 8, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Dean A Wacker, John V Duncia, Joseph B Santella, III, Daniel S Gardner
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Patent number: 6858628Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: December 3, 2002Date of Patent: February 22, 2005Assignee: The Proctor & Gamble CompanyInventors: Michael George Natchus, Biswanath De, Stanislaw Pikul, Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Menyan Cheng
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Publication number: 20040266823Abstract: Compounds of the invention, for example compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).Type: ApplicationFiled: May 13, 2004Publication date: December 30, 2004Inventors: John Cumming, Howard Tucker
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Patent number: 6835840Abstract: The present invention discloses a now and improved process for the preparation 1-substituted di-aryl-4-amino-piperidinyl compounds by a one-pot double arylation followed by optional deprotection step(s).Type: GrantFiled: June 4, 2003Date of Patent: December 28, 2004Assignee: AstraZeneca ABInventor: Andrew Griffin
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Publication number: 20040259913Abstract: Compounds of Formula (1), and their N-oxides and suitable slats, are disclosed which are useful as invertebrate pest control agents, wherein A and B are independently O or S; E is C or N; J is a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 4 R5; K is taken together with the two contiguous linking carbon atoms to form a 5- or 6-membered nanoaromatic carbocyclic or heterocyclic ring optionally including one or two ring members selected from the group consisting of C(═O), SO or S(O)2, each ring optionally substituted with 1 to 4 R4; and R1, R2, R3, R4 and R5 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling an invertebrate pests which involves contacting the pest or its environment with an effective amount of a compound of Formula (I).Type: ApplicationFiled: May 21, 2004Publication date: December 23, 2004Inventor: David Alan Clark
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Publication number: 20040235825Abstract: A carboxylic acid derivative of formula (I) 1Type: ApplicationFiled: June 10, 2004Publication date: November 25, 2004Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Kousuke Tani, Masaki Osada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
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Publication number: 20040181071Abstract: The invention relates to a process for preparing a 4-alkoxycarbonylamino-1-benzyl-4-phenylpiperidine of formula (I) 1Type: ApplicationFiled: January 12, 2004Publication date: September 16, 2004Inventors: Gilles Anne-Archard, Patrick Gros-Claude
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Publication number: 20040138201Abstract: This invention relates to novel lactams of Formula (I): 1Type: ApplicationFiled: October 14, 2003Publication date: July 15, 2004Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
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Patent number: 6759420Abstract: The present invention is directed to new compounds for the inhibition of blood clotting proteins and factor Xa activity, and more particularly, to arylalkanoyl derivatives of the formula (I): wherein R(1), R(2), R(3), R(4), R(5), R(6a), and R(6b) have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula (I) in the treatment and prophylaxis of diseases whcih can be treated or prevented by the inhibition of factor Xa activity, such as cardiovascular or thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases.Type: GrantFiled: December 28, 1999Date of Patent: July 6, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Elisabeth Defossa, Uwe Heinelt, Otmar Klingler, Gerhard Zoller, Hans Matter, Fahad A. Al-Obeidi, Armin Walser, Peter Wildgoose
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Publication number: 20040110952Abstract: The invention provides a compound of formula (1): wherein R1, R2, R3, R3a, R4, R4a, R5, and R6 are defined; or a pharmaceutically acceptable salt thereof or a solvate thereof; compositions containing these compounds, processes for preparing them and their use as modulators of chemokine activity (especially CCR5 activity).Type: ApplicationFiled: August 26, 2003Publication date: June 10, 2004Inventors: Jeremy Burrows, John Cumming, Howard Tucker
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Publication number: 20040110794Abstract: The invention provides a compound of formula (I): wherein R1, R2, R3, R3a, R4, R4a, R5, and R6 are as defined; or a pharmaceutically acceptable salt thereof or a solvate thereof; compositions containing these compounds, processes for preparing them and their use as modulators of chemokine activity (especially CCR5 activity).Type: ApplicationFiled: September 18, 2003Publication date: June 10, 2004Inventors: Jeremy Burrows, John Cumming