The Chalcogen, X, Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/335)
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Publication number: 20090062269Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: February 2, 2007Publication date: March 5, 2009Inventors: Subharekha Raghavan, Darby Rye Schmidt, Steven L. Colletti, Abigail Lee Smenton
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Patent number: 7495001Abstract: There are presented compounds of the formula wherein R6 and R7 is R4 and R5 or R5 and R6 together with the carbon atoms to which they are attached, form a ring as defined in the description and X1, X2, Y1 to Y4, R1 to R13 and n are as specified in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.Type: GrantFiled: October 29, 2004Date of Patent: February 24, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Matthew Blake Wright
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Publication number: 20090048255Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3 and R4 are as defined herein.Type: ApplicationFiled: July 17, 2008Publication date: February 19, 2009Inventors: Richard A. SCHUMACHER, Allen T. HOPPER, Ashok TEHIM, Hans-Jurgen Ernst HESS, Axel UNTERBECK, Erik KUESTER, William Frederick BRUBAKER, JR., Robert F. DUNN
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Publication number: 20090042772Abstract: Novel compounds, compositions comprising compounds, and methods for methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyl transferase activity.Type: ApplicationFiled: October 13, 2008Publication date: February 12, 2009Applicant: Transition Therapeutics Inc.Inventor: John Nestor
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Publication number: 20090036423Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.Type: ApplicationFiled: February 1, 2008Publication date: February 5, 2009Inventors: Shifeng Pan, Wenqi Gao, Nathanael S. Gray, Yuan Mi, Yi Fan
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Publication number: 20090036357Abstract: This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.Type: ApplicationFiled: June 12, 2008Publication date: February 5, 2009Applicant: CoNCERT Pharmaceuticals, Inc.Inventors: Scott L. Harbeson, Roger D. Tung
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Publication number: 20090023787Abstract: One aspect of the invention relates to novel complexes of technetium (Tc) with various heteroaromatic ligands, e.g., pyridyl and imidazolyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to novel pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium complexes are also described. Another aspect of the invention relates to novel pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.Type: ApplicationFiled: May 21, 2008Publication date: January 22, 2009Inventors: John W. Babich, Kevin P. Maresca
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Patent number: 7468383Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome activity.Type: GrantFiled: February 9, 2006Date of Patent: December 23, 2008Assignee: Cephalon, Inc.Inventors: Raffaella Bernardini, Alberto Bernareggi, Paolo G. Cassara, Germano D'Arasmo, Ernesto Menta, Ambrogio Oliva
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Patent number: 7465803Abstract: Use for the treatment of diseases having an inflammatory basis of compounds or salts thereof, having the following general formula (I): A-X1-L-(W)p—NO2 wherein A contains the radical of a drug, X1 and W are bivalent radicals, p is an integer equal to 1 or 0, and L is a covalent bond, CO, oxygen, sulphur, or NR1C where R1C is H or a C1-C5 linear or branched alkyl.Type: GrantFiled: October 9, 2001Date of Patent: December 16, 2008Assignee: Nicox S.A.Inventors: Piero Del Soldato, Francesca Benedini, Patrizia Antognazza
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Patent number: 7405230Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3 and R4 are as defined herein.Type: GrantFiled: July 21, 2003Date of Patent: July 29, 2008Assignee: Memory Pharmaceuticals CorporationInventors: Richard A. Schumacher, Allen T. Hopper, Ashok Tehim, Hans-Jurgen Ernst Hess, Axel Unterbeck, Erik Kuester, William Frederick Brubaker, Jr., Robert F. Dunn
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Patent number: 7388023Abstract: Certain ?-amino acids that bind to the alpha-2-delta (?2?) subunit of a calcium channel are disclosed. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders. Also disclosed are methods of making the ?-amino acids.Type: GrantFiled: December 7, 2006Date of Patent: June 17, 2008Assignee: Warner-Lambert Company LLCInventors: Peter Garth Blazecka, Joseph Richard Bozelak, Norman Lloyd Colbry, Timothy Thomas Curran, Annise Paige Goodman, Kevin E. Henegar, Garrett Hoge, Paul D. Johnson, Augustine Tobi Osuma, Mark Stephen Plummer, Jacob Bradley Schwarz, Derek Clinton Vrieze, Ji Zhang
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Publication number: 20080139630Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.Type: ApplicationFiled: June 3, 2005Publication date: June 12, 2008Inventors: Barbara Hanney, Yuntae Kim, Michael R. Krout, Robert S. Meissner, Helen J. Mitchell, Jeffrey Musselman, James J. Perkins, Jiabing Wang
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Publication number: 20080139455Abstract: Novel compounds, compositions comprising compounds, and methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, restenosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyltransferase activity.Type: ApplicationFiled: October 12, 2007Publication date: June 12, 2008Applicant: Forbes Medi-Tech (Research), Inc.Inventor: John J. Nestor
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Patent number: 7378446Abstract: The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV, its production method, an intermediate compound useful for its production and a pharmaceutical composition containing these compounds, and the present invention relates to a compound represented by the formula (I): (wherein A represents —(CH2)n—, etc.; B represents —(C?O)—, etc.; D represents —(CH2)m—R?, etc.; E represents a hydrogen atom, etc.; G represents —(CH2)p-J, etc.; bond Q represents a single bond or double bond; and R1, R2 and R3 may be the same or different and each represent a hydrogen atom, etc.), a prodrug thereof or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 9, 2004Date of Patent: May 27, 2008Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Masayuki Sudoh, Takuo Tsukuda, Miyako Masubuchi, Kenichi Kawasaki, Takeshi Murata, Fumio Watanabe, Hiroshi Fukuda, Susumu Komiyama, Tadakatsu Hayase
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Patent number: 7375231Abstract: The present invention relates to a novel compound of formula (IV) which is an intermediate that can be used for the preparation of pioglitazone. It also relates to a method of obtaining the novel compound (IV) starting from the natural product L-tyrosine, in which the amino group is protected in the form of aromatic imino group, and a method of obtaining pioglitazone from the said intermediate.Type: GrantFiled: May 4, 2004Date of Patent: May 20, 2008Assignee: Medichem S.A.Inventor: Ernesto Duran Lopez
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Publication number: 20080114175Abstract: The present invention is directed to a process for preparing certain cysteine protease inhibitors.Type: ApplicationFiled: September 16, 2005Publication date: May 15, 2008Inventor: Jiayao Li
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Publication number: 20080114036Abstract: Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hyper triglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.Type: ApplicationFiled: May 3, 2005Publication date: May 15, 2008Applicant: Novo Nordisk A/SInventors: Miroslav Havranek, Per Sauerberg, Ingrid Pettersson
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Publication number: 20080096892Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellu-lar activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Even more specifically, the invention provides compounds for modulating c-Kit kinase activity and methods of treating diseases mediated by c-Kit activity utilizing the compounds and pharmaceutical compositions thereof.Type: ApplicationFiled: August 27, 2004Publication date: April 24, 2008Applicant: Exelixis, Inc.Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew Tsuhako, John M. Nuss, Wei Xu, William Bajjalieh
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Patent number: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
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Patent number: 7342115Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Patent number: 7320983Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 25, 2006Date of Patent: January 22, 2008Assignee: G.D. Searle LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Patent number: 7320993Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.Type: GrantFiled: June 16, 2000Date of Patent: January 22, 2008Assignee: Astellas Deutschland GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
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Patent number: 7301031Abstract: A method for producing a hydroxy-amino ester, or derivative thereof, is provided. A substituted ?-ketodiester having a ketone group and two ester functional groups is contacted with a ketoreductase under conditions permitting the reduction of the ketone group to an alcohol. Only one of the ester functional groups is regioselectively hydrolyzed to the corresponding carboxylic acid, whereby a non-hydrolyzed ester functional group remains. The carboxylic acid is converted to an amine or a derivative thereof to produce a hydroxy-amino ester or derivative thereof. A number of novel hydroxy-amino esters are prepared by the method.Type: GrantFiled: December 16, 2004Date of Patent: November 27, 2007Assignee: BioCatalytics, Inc.Inventors: J. David Rozzell, Jr., Spiros Kambourakis
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Patent number: 7253171Abstract: Novel antagonists of ?4?1 integrin and/or ?4?7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4.Type: GrantFiled: January 15, 2002Date of Patent: August 7, 2007Assignee: Laboratorios Almirall, S.A.Inventors: Juan Miguel Jimenez Mayorga, Jordi Bach Tana, Jesus Maria Ontoria Ontoria, Eloisa Navarro Romero
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Patent number: 7232911Abstract: Process for the preparation of 2-aminomethylpyridine derivative of general formula (I), in which: n represents 0, 1, 2 or 3; X is halogen atom; Y may be the same or different and may be a halogen atom, a halogenoalkyl, a alkoxycarbonyl or a alkylsulphonylType: GrantFiled: November 18, 2003Date of Patent: June 19, 2007Assignee: Bayer Cropscience S.A.Inventors: Manuel Vangelisti, Mehul Amin, Robert Pannell
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Patent number: 7230003Abstract: Prodrugs of propofol, methods of making prodrugs of propofol, pharmaceutical compositions of prodrugs of propofol and methods of using prodrugs of propofol and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting are disclosed herein.Type: GrantFiled: September 9, 2004Date of Patent: June 12, 2007Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Feng Xu
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Patent number: 7199141Abstract: Nitro-oxyderivative compounds or salts thereof having the following general formula (I): A—(B)b0—(C)c0—NO2 wherein: c0 is an integer and is 0 or 1, b0 is an integer and is 0 or 1, A=R—T1—, wherein R is the radical of an analgesic drug for the chronic pain, in particular for the neuropathic pain; B is such that its precursor is selected from anminoacids, hydroxyacids, polyalcohols, compounds containing at least one acid function; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.Type: GrantFiled: May 10, 2002Date of Patent: April 3, 2007Assignee: Nicox S.A.Inventors: Piero Del Soldato, Ennio Ongini
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Patent number: 7166726Abstract: Disclosed herein are compounds of the formula wherein R1 is independently H or alkyl of 1 to 6 carbons; R2 is optional and is defined as lower alkyl of 1 to 6 carbons, F, Cl, Br, I, CF3, fluoro substituted alkyl of 1 to 6 carbons, OH, SH, alkoxy of 1 to 6 carbons, or alkylthio of 1 to 6 carbons; n is an integer of between 0 and 2; o is an integer between 0 and 3; R3 is hydrogen, lower alkyl of 1 to 6 carbons, F, Cl, Br or I; R4 is heteroaryl or (R5)p-heteroaryl where the heteroaryl group is 5-membered or 6-membered and has 1 to 3 heteroatoms selected from the group consisting of O, S, and N; p is an integer having the values of 0–5; R5 is F, Cl, Br, I, NO2, N(R8)2, N(R8)CORO8, N(R8)CON(R8)2, OH, OCOR8, OR8, CN, COOH, COOR8, C1-10 alkyl, fluoro substituted C1-10 alkyl, C2-10 alkenyl having 1 to 3 double bonds, C2-10 alkynyl having 1 to 3 triple bonds, or a (trialkyl)silyl or (trialkyl)silyloxy group where the alkyl groups independently have 1 to 6 carbons; A is (CH2)q where q is 0–5, C3-6 branched alkyl,Type: GrantFiled: January 2, 2003Date of Patent: January 23, 2007Assignee: Allergan, Inc.Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Roshantha A. Chandraratna
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Patent number: 7166746Abstract: The invention relates to N-bisaryl- and N-aryl-cycloalkylidenyl-a-hydroxy- and a-alkoxy acetic acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, C1–C12alkyl; C2–C12alkenyl; C2–C12alkynyl; C1–C12haloalkyl; R2 is hydrogen; optionally substituted alkyl; or optionally substituted alkynyl; R3 is optionally substituted aryl or optionally substituted heteroaryl; A is an optionally substituted saturated or unsaturated C3–C8-cycloalkylidene, optionally substituted phenylidene or optionally substituted saturated or unsaturated heterocyclylidene bridge, R4 and R5 are each independently hydrogen or an organic radical, and R6 is hydrogen; tri-C1–C4alkyl-silyl; di-C1–C4alkyl-phenylsilyl; C1–C4alkyl-diphenylsilyl; triphenylsilyl; optionally substituted alkyl; optionally substituted alkenyl or optionally substituted alkynyl.Type: GrantFiled: July 23, 2003Date of Patent: January 23, 2007Assignee: Syngenta Crop Protection, Inc.Inventors: Clemens Lamberth, Martin Zeller, Tibor Goegh
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Patent number: 7115618Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 30, 2004Date of Patent: October 3, 2006Assignee: G.D. Searle & Co.Inventors: Michael J. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Patent number: 7081535Abstract: Hydroxy-amino acids are provided and are prepared by contacting a substituted ?-ketodiester having a ketone group and two ester functional groups with a ketoreductase under conditions permitting the reduction of the keytone group to an alcohol. Only one of the ester functional groups is regioselectively hydrolyzed to the corresponding carboxylic acid, whereby a non-hydrolyzed ester functional group remains. The carboxylic acid is converted to an amine to produce a hydroxy-amino acid.Type: GrantFiled: December 16, 2004Date of Patent: July 25, 2006Assignee: BioCatalytics, Inc.Inventors: J. David Rozzell, Jr., Spiros Kambourakis
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Patent number: 6953792Abstract: The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R?17, R18, R19, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: May 16, 2001Date of Patent: October 11, 2005Assignees: Merck Sharp & Dohme Limited, Merck & Co., Inc.Inventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliot, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain, Lihu Yang
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Patent number: 6939967Abstract: Process for production of non-proteinogenic L-amino acids by direct fermentation of a microorganism strain known per se having a deregulated cysteine metabolism in a manner known per se, which comprises adding, during the fermentation, a nucleophilic compound to the fermentation batch in a manner such that this leads to the production of non-proteinogenic L-amino acids by the microorganism strain.Type: GrantFiled: April 28, 2004Date of Patent: September 6, 2005Assignee: Consortium für elektrochemische Industrie GmbHInventor: Thomas Maier
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Patent number: 6936719Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.Type: GrantFiled: December 18, 2003Date of Patent: August 30, 2005Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
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Patent number: 6884821Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.Type: GrantFiled: September 29, 2000Date of Patent: April 26, 2005Assignee: Eisai Co., Ltd.Inventors: Masanobu Shinoda, Eita Emori, Fumiyoshi Matsuura, Toshihiko Kaneko, Norihito Ohi, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Sadakazu Miyashita, Taro Hibara, Takashi Seiki, Richard Clark, Hitoshi Harada
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Patent number: 6849649Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: October 28, 2003Date of Patent: February 1, 2005Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
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Publication number: 20040266789Abstract: Disclosed are compounds and pharmaceutically acceptable salts of formula (I): 1Type: ApplicationFiled: April 30, 2004Publication date: December 30, 2004Inventors: Darren Whitehouse, Shaojing Hu, Michael C. Van Zandt, Garrett Parker, Thomas G. Meskill
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Publication number: 20040266788Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): 1Type: ApplicationFiled: April 14, 2004Publication date: December 30, 2004Applicant: The Institute for Pharmaceutical Discovery LLCInventors: Michael C. Van Zandt, Darren Whitehouse, Kerry Combs, Shaojing Hu
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Publication number: 20040266698Abstract: Compounds of the formula (I), wherein R1, R1-R7 and alk have meaning as defined, pharmaceutical compositions thereof, and use thereof for the treatment and/or prevention of cardiovascular disorders responsive to ACE and NEP inhibition and/or ECE inhibition.Type: ApplicationFiled: February 24, 2004Publication date: December 30, 2004Inventor: Cynthia Anne Fink
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Publication number: 20040254225Abstract: Novel compounds and compositions including those compounds, as well as methods of using and making the compounds are herein described. The compounds are useful in therapeutic applications, including modulation of disease or disease symptoms in a subject (e.g., mammal, human, dog, cat, horse). The compounds are useful as modulators of the mu opioid receptor (MOR) through their binding affinity with that receptor.Type: ApplicationFiled: October 10, 2003Publication date: December 16, 2004Inventors: Bryce A. Harrison, Tiffany M. Gierasch, Gregory L. Verdine, Zhangjie Shi
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Patent number: 6809207Abstract: The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. These derivatives may comprise such representative side groups as a phenyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, or thienyl group. The present invention further provides a method for synthesizing alpha-amino acids and derivatives thereof via a modified Ugi type reaction using an aldehyde, ammonium formate and a C1-C5 alkyl isocyanide. The compounds provided by this method are useful in the development of new pharmaceuticals for the treatment of human diseases.Type: GrantFiled: July 24, 2002Date of Patent: October 26, 2004Assignee: PharmaCore, Inc.Inventors: Sekar Alla, Seung-Yong Choi, Dale Dhanoa, Elso DiFranco, Galina Krokhina, Keqiang Li, Balasubramanian Thiagarajan, Wen-Chun Zhang
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Publication number: 20040210060Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiomers.Type: ApplicationFiled: May 7, 2004Publication date: October 21, 2004Applicant: SOLVAY S.A.Inventors: Thierry Delplanche, Roland Callens
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Patent number: 6803378Abstract: Novel diketoacid compounds of Formula I are provided which are useful as HIV integrase inhibitors and for the treatment of AIDS or ARC.Type: GrantFiled: September 25, 2002Date of Patent: October 12, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
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Publication number: 20040198777Abstract: Compounds which have utility in the treatment of conditions associated with altered mitochondrial function.Type: ApplicationFiled: December 19, 2003Publication date: October 7, 2004Applicant: MitoKor, Inc.Inventors: Soumitra S. Ghosh, Yazhong Pei, Xiao-Qing Tang
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Publication number: 20040198727Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.Type: ApplicationFiled: June 6, 2003Publication date: October 7, 2004Inventors: Takumi Kawabe, Hidetaka Kobayashi
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Publication number: 20040171656Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: March 10, 2004Publication date: September 2, 2004Inventors: Hartmuth C. Kolb, Gerard McGeehan, Zhi-Cai Shi, Laxma Reddy Kolla, Cullen Cavallaro
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Patent number: 6784311Abstract: Process for the preparation of 3-aminoalkanoic acid esters of the general formula: in which R is C1-6-alkyl and R1 is hydrogen, C1-6-alkyl or phenyl, or their salts, by catalytic hydrogenation of the corresponding 3-amino-2-alkenoic acid esters of the general formula: in which R and R1 have the above mentioned meanings. The hydrogenation is carried out in the presence of a strong acid and the salt of the 3-aminoalkanoic acid ester (I) and the strong acid formed is optionally converted into the free 3-aminoalkanoic acid ester (I) or into another salt in a manner known per se.Type: GrantFiled: August 21, 2002Date of Patent: August 31, 2004Assignee: Lonza AGInventor: Rudolf Fuchs
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Publication number: 20040147455Abstract: The present invention relates generally to prodrugs of fused GABA analogs, pharmaceutical compositions of prodrugs of fused GABA analogs, methods of making prodrugs of fused GABA analogs and methods of using prodrugs of fused GABA analogs and pharmaceutical compositions of prodrugs of fused GABA analogs to treat or prevent various diseases.Type: ApplicationFiled: December 11, 2003Publication date: July 29, 2004Inventor: Mark A. Gallop
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Publication number: 20040147454Abstract: The present invention provides compounds having the formula: 1Type: ApplicationFiled: December 10, 2003Publication date: July 29, 2004Inventor: Wenjin Yang
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Publication number: 20040142877Abstract: Novel biphenyl derivatives of the general formula I 1Type: ApplicationFiled: October 14, 2003Publication date: July 22, 2004Inventors: Oliver Schadt, Alfred Jonczyk, Wolfgang Staehle, Simon Goodman