Chalcogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 540/604)
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Patent number: 9809680Abstract: Thioaminal polymers are made from hexahydrotriazine precursors and dithiol precursors. The precursors are blended together and subjected to mild heating to make the polymers. An amine scavenger is used to remove amine byproducts from the reaction, thus promoting polymer growth to high molecular weight. The polymers have the general structure wherein each R1 is independently an organic or hetero-organic group, a plurality of R2 groups are substituents having molecular weight greater than about 120 Daltons, and n is an integer greater than or equal to 1. The polymers may be functionalized by adding a thiol-reactive group to either end or both ends.Type: GrantFiled: May 17, 2016Date of Patent: November 7, 2017Assignee: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Dylan J. Boday, Jeannette M. Garcia, James L. Hedrick, Robert J. Ono, Rudy J. Wojtecki
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Patent number: 9738606Abstract: A compound of Formula I, Formula IA, Formula IB, or Formula II, or an acid or base addition salt thereof, and use of these compounds as antioxidants. In one embodiment, a compound of Formula II, wherein each of X, Y, and Z are independently a carbon or nitrogen atom; R1 and R2 are each independently a hydrogen or an electron donating group, but are not both hydrogen, and wherein R1, and R2 are each bonded to a carbon atom in their own respective aryl ring.Type: GrantFiled: June 4, 2012Date of Patent: August 22, 2017Assignees: Queen's University at Kingston, Alma Mater Studiorum—Universita Di BolognaInventors: Derek A. Pratt, Jason J. Hanthorn, Luca Valgimigli
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Patent number: 9233362Abstract: The invention relates to metal complexes of general formula (I) and to a method for the production thereof, in which M, R1, R2, R3, X and Y in addition to Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh can have the meanings defined in the claims. Said metal complexes form air-stable compounds and are suitable as pre-catalysts in the olefin metathesis.Type: GrantFiled: February 23, 2012Date of Patent: January 12, 2016Assignee: Studiengesellschaft Kohle MBHInventors: Alois Furstner, Johannes Heppekausen
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Publication number: 20150133431Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.Type: ApplicationFiled: July 10, 2014Publication date: May 14, 2015Applicant: COYOTE PHARMACEUTICALS, INC.Inventor: Gary C. Look
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Publication number: 20150065554Abstract: Disclosed herein are methods of treating a patient at risk of developing or having a neurofibromatosis or a sporadic schwannoma. In exemplary embodiments, the method involves administering to a subject in need an effective amount of a modulator of a target related to neurofibromatosis. Also disclosed are screening assays involving the implementation of Merlin-null Schwann cells, and to compounds identified using same.Type: ApplicationFiled: March 13, 2013Publication date: March 5, 2015Applicant: University of Central Florida Research Foundation, Inc.Inventor: Cristina Fernandez-Valle
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Publication number: 20140336178Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.Type: ApplicationFiled: April 29, 2014Publication date: November 13, 2014Applicants: The General Hospital Corporation, Massachusetts Institute of TechnologyInventors: Aleksey G. Kazantsev, Anne B. Young, David E. Housman, Steven M. Hersch
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Publication number: 20140296516Abstract: The invention relates to metal complexes of general formula (I) and to a method for the production thereof, in which M, R1, R2, R3, X and Y in addition to Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh can have the meanings defined in the claims. Said metal complexes form air-stable compounds and are suitable as pre-catalysts in the olefin metathesis.Type: ApplicationFiled: February 23, 2012Publication date: October 2, 2014Applicant: STUDIENGESELLSCHAFT KOHLE MBHInventors: Alois Furstner, Johannes Heppekausen
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Publication number: 20140228354Abstract: Compounds of the general structure S-1, wherein X and R1-R5 are defined in the specification, are capable of abrogating the deubiquitinating (DUB) activity of the 19S RP DUBs and are useful in methods and compositions for treating cancer, in particular, cancer tumors refractory to treatment by state-of-the-art chemotherapy.Type: ApplicationFiled: April 18, 2014Publication date: August 14, 2014Applicant: Vivolux ABInventors: Stig Linder, Rolf Larsson
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Publication number: 20140179681Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.Type: ApplicationFiled: January 8, 2014Publication date: June 26, 2014Inventor: Joseph P. Errico
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Publication number: 20140155511Abstract: Sulfur chelated ruthenium compounds represented by the following formula: wherein M indicates the ruthenium metal bound to a benzylidene carbon; R represents C1-C7 alkyl group or optionally substituted aryl; X1 and X2 each independently represent halogen; Y1 and Y2 each independently denote unsubstituted or alkyl-substituted phenyl; and Z independently represents hydrogen, electron withdrawing or electron donating substituent, with m being an integer from 1 to 4, and processes and compositions related thereto.Type: ApplicationFiled: July 18, 2013Publication date: June 5, 2014Inventors: N. Gabriel LEMCOFF, Amos BEN-ASULY
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Publication number: 20140107323Abstract: The present disclosure is directed to a reactive ester agent for conjugating a click-reactive group to a carrier molecule or solid support. The reactive ester agent has the general formula IA, wherein the variables R1, R2, R3, Ra and L are described throughout the application.Type: ApplicationFiled: March 22, 2012Publication date: April 17, 2014Inventors: Kyle Gee, Aimei Chen, Hee Chol Kang
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Patent number: 8575148Abstract: This invention concerns spiro azepane-ox-azolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein R1, R2, (R3)n, and (R4)m have the meanings given in the specification.Type: GrantFiled: December 10, 2009Date of Patent: November 5, 2013Assignee: Abbott Healthcare Products B.V.Inventors: Pieter Smid, Michael Mlinaric, Konrad F. Koehler, Sara Nuñez Garcia, Elmar Wegener, Josephus H. M. Lange
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Patent number: 8563779Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.Type: GrantFiled: July 19, 2011Date of Patent: October 22, 2013Assignee: Bayer CropScience AGInventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
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Publication number: 20130261296Abstract: Catalytic complexes including a metal atom having anionic ligands, at least one nucleophilic carbene ligand, and an alkylidene, vinylidene, or allenylidene ligand. The complexes are highly stable to air, moisture and thermal degradation. The complexes are designed to efficiently carry out a variety of olefin metathesis reactions.Type: ApplicationFiled: January 25, 2013Publication date: October 3, 2013Inventors: Steven P. NOLAN, Jinkun HUANG
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Publication number: 20130203733Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.Type: ApplicationFiled: December 20, 2012Publication date: August 8, 2013Applicants: Massachusetts Institute of Technology, The General Hospital CorporationInventors: The General Hospital Corporation, Massachusetts Institute of Technology
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Publication number: 20130196978Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.Type: ApplicationFiled: March 14, 2013Publication date: August 1, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130190296Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: ApplicationFiled: November 20, 2012Publication date: July 25, 2013Applicant: Dendreon CorporationInventor: Dendreon Corporation
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Publication number: 20130165649Abstract: Cls ruthenium complexes that can be used as catalysts are described. The complexes are generally square pyramidal in nature, having two anionic ligands X adjacent to each other. The complexes can be used as catalysts, for example in olefin metathesis reactions. Corresponding trans ruthenium complexes are also described, together with cationic complexes where one or both of the anionic ligands X are replaced by a non-co-ordinating anionic ligand.Type: ApplicationFiled: March 21, 2011Publication date: June 27, 2013Inventor: Catherine Cazin
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Patent number: 8455646Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.Type: GrantFiled: December 22, 2009Date of Patent: June 4, 2013Assignee: Chiesi Farmaceutici S.p.A.Inventors: Antonio Caligiuri, Mauro Riccaboni, Gabriele Amari
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Publication number: 20120135968Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.Type: ApplicationFiled: May 7, 2010Publication date: May 31, 2012Inventors: Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus Rönn
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Patent number: 8163735Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.Type: GrantFiled: December 1, 2005Date of Patent: April 24, 2012Assignee: Virobay, Inc.Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
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Publication number: 20120046276Abstract: A method of preventing or treating diseases caused by Mycobacterium, comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.Type: ApplicationFiled: October 25, 2011Publication date: February 23, 2012Applicant: Nabriva Therapeutics AGInventors: Gerd Ascher, Heinz Berner, Rosemarie Mang
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Publication number: 20110195929Abstract: Described are various compounds and methods for the treatment of flaviviral infections. In particular, alkaloids and imino sugars in arabinose and/or lyxose stereochemical configuration with antiflaviviral activity are described.Type: ApplicationFiled: August 4, 2009Publication date: August 11, 2011Applicant: SUMMIT CORPORATION PLCInventors: Olivier De Moor, Graeme Horne, Penny Jane Middleton, Frank Schroer, Stephen Paul Wren, Maria Ines Passos Eleuterio, Renate Van Well, Colin Richard Dorgan, Francis Xavier Wilson, Robert Nash, Richard Storer, Graham Michael Wynne, Alan Geoffrey Roach, Akane Kawamura, Jonathon Mark Tinsley
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Publication number: 20110130562Abstract: In one embodiment, the present application discloses mixtures comprising (a) water in an amount of at least 1% wt/wt of the mixture; (b) a transition metal catalyst; and (c) one or more solubilizing agents; and methods for using such mixtures for performing transition metal mediated bond formation reactions.Type: ApplicationFiled: December 1, 2010Publication date: June 2, 2011Inventor: Volker Berl
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Publication number: 20110129542Abstract: In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.Type: ApplicationFiled: August 12, 2008Publication date: June 2, 2011Inventors: Santhosh Neelamkavil, Craig D. Boyle, Samuel Chackalamannil
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Publication number: 20110112076Abstract: The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).Type: ApplicationFiled: July 13, 2009Publication date: May 12, 2011Inventors: Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
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Publication number: 20110098281Abstract: The invention relates to pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, Z and m are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: April 8, 2008Publication date: April 28, 2011Applicant: Purdue Pharma L.P.Inventors: Donald J. Kyle, Jiangchao Yao
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Patent number: 7910729Abstract: The present invention provides azulenyl nitrones, such as those having the following general formula: (I) compositions comprising the same and methods of their use for the treatment or prevention of oxidative, ischemic, ischemia/reperfusion-related and chemokine-mediated conditions.Type: GrantFiled: September 22, 2005Date of Patent: March 22, 2011Assignee: The Florida International University Board of TrusteesInventors: David A. Becker, James J. Ley
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20110009621Abstract: The invention relates, in particular, to supported transition metal complexes based on a polystyrene matrix comprising structural units of the formula (Ia): or supported transition metal complexes based on a silica gel matrix comprising structural units of the formula (II): where the radicals and indices have the meanings given in the description. The invention also relates to the use of the supported transition metal complexes in catalysis and corresponding processes for the transition metal-catalyzed conversion of starting material(s) into product(s). In particular, the invention relates to the field of olefin metathesis.Type: ApplicationFiled: December 6, 2006Publication date: January 13, 2011Applicant: Raap Polymere GmbHInventors: Willi Bannwarth, Florian Michalek, Jurgen Ruhe
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Patent number: 7858613Abstract: The invention relates to substituted benzo-condensed cycloheptanone derivatives, to methods for producing them, to drugs containing said compounds and to the use of said compounds for producing drugs.Type: GrantFiled: May 17, 2006Date of Patent: December 28, 2010Assignee: Gruenenthal GmbHInventors: Claudia Hinze, Robert Frank, Ruth Jostock, Klaus Schiene, Michael Haurand, Hagen-Heinrich Hennies
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Publication number: 20100173880Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.Type: ApplicationFiled: December 22, 2009Publication date: July 8, 2010Applicant: Chiesi Farmaceutici S.p.A.Inventors: Antonio Caligiuri, Mauro Riccaboni, Gabriele Amari
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Publication number: 20100152125Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.Type: ApplicationFiled: March 20, 2008Publication date: June 17, 2010Applicant: Brandeis UniversityInventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R.P. Novak
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Publication number: 20100063030Abstract: The invention relates to pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, Z and m are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: April 8, 2008Publication date: March 11, 2010Applicant: Purdue Pharma L.P.Inventors: Donald J. Kyle, Jiangchao Yao
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Publication number: 20090233909Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.Type: ApplicationFiled: December 1, 2005Publication date: September 17, 2009Applicant: Virobay, Inc.Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
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Patent number: 7563784Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: GrantFiled: April 25, 2006Date of Patent: July 21, 2009Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
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Publication number: 20090137759Abstract: The invention relates to biochemical synthesis of 6-amino caproic acid from 6-aminohex-2-enoic acid compound or from 6-amino-2-hydroxyhexanoic acid, by treatment with an enzyme having ?,?-enoate reductase activity towards molecules containing an ?,?-enoate group and a primary amino group. The invention also relates to processes for obtaining suitable genetically engineered cells for being used in such biotransformation process, and to precursor fermentation of 6-amino caproic acid from intermediates leading to 6-amino caproic acid. Finally, the invention relates to certain novel biochemically produced compounds, namely 6-aminohex-2-enoic acid, 6-aminohexanoic acid, as well as to caprolactam produced therefrom and to nylon-6 and other derivatives produced from such biochemically produced compounds or caprolactam.Type: ApplicationFiled: January 8, 2009Publication date: May 28, 2009Applicant: DSM IP ASSETS B.V.Inventors: Petronella C. Raemakers-Franken, Petrus M.M. Nossin, Paul M. Brandts, Marcel G. Wubbolts, Wijnand P.H. Peeters, Sandra Ernste, Stefaan M.A. Wildeman De, Martin Schuermann
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Publication number: 20090075975Abstract: Arylsulfonamide compounds of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:Type: ApplicationFiled: November 24, 2008Publication date: March 19, 2009Inventors: Michael R. DeGraffenreid, JAY P. POWERS, Daqing Sun, Xuelei Yan
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 7456195Abstract: The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, Y, Z, R7, R8, R9, and R11 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: GrantFiled: June 22, 2006Date of Patent: November 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Zhang, Alexandra A. Nirschl, Yan Zou, Eldon Scott Priestley
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Patent number: 7449573Abstract: A compound which generates a sulfonic acid having one or more —SO3H groups and one or more —SO2— bonds upon irradiation with an actinic ray or a radiation; a photosensitive composition containing the compound; and a method of pattern formation with the photosensitive composition.Type: GrantFiled: February 14, 2005Date of Patent: November 11, 2008Assignee: FUJIFILM CorporationInventors: Kunihiko Kodama, Kenji Wada, Kaoru Iwato
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Publication number: 20080262224Abstract: This invention relates to a method of preparation of benzofuran-2-carboxylic acid {(S)-3-methyl-1-[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-sulfonyl)-azepan-4-ylcarbamoyl]-butyl}-amide.Type: ApplicationFiled: January 21, 2005Publication date: October 23, 2008Inventors: William M. Clark, Neil Francis Badham, Qunying Dai, Ann Marie Eldridge, Hayao Matsuhashi
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Patent number: 7405209Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: June 14, 2005Date of Patent: July 29, 2008Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: Robert Wells Marquis, Jr., Yu Ru, Daniel Frank Veber, Maxwell David Cummings, Scott Kevin Thompson, Dennis Shinji Yamashita
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Patent number: 7354771Abstract: The absolute configuration of a chiral compound is determined by (i) coordinating the chiral compound to a metalloporphyrin having a carbon chain-crosslinked porphyrin dimer structure in which one of the two porphyrin rings has at least one ethyl or substituent bulkier than ethyl at at least one of the second peripheral carbon atoms from the carbon atom at the carbon chain crosslink site, and (ii) analyzing the resultant coordination compound by circular dichroism spectrophotometry to determine the absolute configuration of the asymmetric carbon based on the sign of the Cotton effect. The chiral compound has an asymmetric carbon bonded to a basic group capable of coordinating to the metal of the other porphyrin ring of the metalloporphyrin dimer or an asymmetric carbon atom adjacent to the carbon atom bonded to the basic group.Type: GrantFiled: December 4, 2000Date of Patent: April 8, 2008Assignee: Japan Science and Technology CorporationInventors: Yoshihisa Inoue, Victor Borovkov, Juha Lintuluoto
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Patent number: 7256186Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.Type: GrantFiled: September 15, 2004Date of Patent: August 14, 2007Assignee: Schering CorporationInventors: Dimitri A. Pissarntiski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
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Patent number: 7208602Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.Type: GrantFiled: February 5, 2003Date of Patent: April 24, 2007Assignees: Schering Corporation, Pharacopeia Drug Discovery, Inc.Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
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Patent number: 7202237Abstract: The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the central nervous system, pain, inflammatory diseases, diseases caused by smooth muscle contractions and as assistance in the cessation of chemical substance abuse.Type: GrantFiled: May 19, 2004Date of Patent: April 10, 2007Assignee: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet Østergaard Nielsen
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Patent number: 7192953Abstract: Compounds of formula (I) have antibacterial activity; wherein Q represents a radical of formula —N(OH)CH(?O) or formula —C(?O)NH(OH); Y represents —C(?O)—, —C(?S)—, —S(?O)—, or —SO2—; R1 represents hydrogen, C1–C6 alkyl or C1–C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of formula —N(OH)CH(?O), a hydroxy, C1–C6 alkoxy, C1–C6 alkenyloxy, halogen, amino, C1–C6 alkylamino, or di-(C1–C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1–C6 alkyl, C1–C3 alkyl-O—C1–C3 alkyl, C1–C3 alkyl-S—C1–C3 alkyl, cycloalkyl(C1–C3 alkyl)-, aryl(C1–C3alkyl)-, heterocyclyl(C1–C3 alkyl)-, or R1R2N—C1–C3 alkyl group wherein R1 represents hydrogen or C1–C3 alkyl and R2 represents C1–C3 alkyl, or R1R2N-represents a cyclic amino group; R3 and R4 taken together with the nitrogen atoms to which they are respectively attached form a saturated heterocyclic ring of from 4 to 7 ring atoms, which may be fused to a second carbocyclic or heterocyclic ring, either of which rings may optionallType: GrantFiled: December 1, 2003Date of Patent: March 20, 2007Assignee: Vernalis (Oxford) LimitedInventor: Stephen Peter East
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Patent number: 7071184Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: GrantFiled: March 7, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
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Patent number: 6960574Abstract: Disclosed are compounds having the formula: where R1=H, C1-C6 alkyl, cycloalkyl, R2=H, C1-C6 alkyl, cycloalkyl W=CnH2n-m—NH (n=1-6, m=0, 2, or 4), X= R3= Y= Z=CONR8(CH2)n, CONR8(CH2)nCO, P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n, SO2(CH2)nCO, SO2NR8(CH2)n, SO2NR8(CH2)nCO, n=1-4 R4=H, (CH2)nOH, (CH2)nOCOR10, (CH2)nNR10R11, (CH2)nCONR10R11, n=0-4 R5=H, (CH2)nNR12R13, n=0-4 R6=H, (CH2)nNR14R15, n=0-4 R7=H, C1-C6 alkyl, cycloalkyl; R8=H, C1-C6 alkyl, cycloalkyl; R9=H, C1-C6 alkyl, cycloalkyl; R10=H, C1-C6 alkyl, cycloalkyl; R11=H, C1-C6 alkyl, cycloalkyl; R12=H, C1-C6 alkyl, cycloalkyl; R13=H, C1-C6 alkyl, cycloalkyl; R14=H, C1-C6 alkyl, cycloalkyl; R15=H, C1-C6 alkyl, cycloalkyl. Dashed lines: optional; conformational constraint by (CH2)n, n=1-3, R?=H or O(?) as well as pharmaceuticals compositions and methods for the treatment of opiate addiction, opiate dependence, opiate tolerance, opiate related abstinence syndrome, nicotine addition and obesity based thereon.Type: GrantFiled: March 17, 2004Date of Patent: November 1, 2005Assignee: University of FloridaInventor: Laszlo Prokai