Chalcogen Bonded Directly To Ring Carbon Of The Piperidine Ring Patents (Class 546/242)
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Patent number: 7589035Abstract: Disclosed are stabilized body care products, household products, textiles and fabrics which comprise certain sterically hindered amine salt compounds. Dyed products and articles are effectively stabilized against color degradation. The products are for example skin-care products, hair-care products, dentifrices, cosmetics, laundry detergents and fabric softeners, non-detergent based fabric care products, household cleaners and textile-care products.Type: GrantFiled: March 19, 2009Date of Patent: September 15, 2009Assignee: Ciba Specialty Chemicals CorporationInventors: Joseph A. Lupia, Joseph Suhadolnik, Mervin G. Wood, Wanda H. Martin
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Publication number: 20090209581Abstract: Pharmaceutical compositions are provided that are useful in treating immunological diseases. The compositions comprise a pharmaceutically acceptable carrier, and an effective therapeutic or prophylactic amount of a nitroxide antioxidant that alters the expression of a gene related to an immunological disease. Methods are also provided for the use of the pharmaceutical compositions in the treatment or prevention of immunological disease.Type: ApplicationFiled: February 2, 2006Publication date: August 20, 2009Inventors: Louis Habash, Clarence Jones
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Patent number: 7572869Abstract: The present invention relates to selected 1-alkoxy-2,2,6,6 tetramethyl piperidine, 1-alkoxy-2,2 diethyl-6,6 dimethyl piperidine and 1-alkoxy-2,6 diethyl-2,3,6 dimethyl piperidine derivatives which are substituted in the 4 position by two oxygen atoms forming an open chain or cyclic ketal structure, a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) said piperidine derivatives. Further aspects of the present invention are a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-2,2,6,6 tetramethyl piperidine, 1-alkoxy-2,2 diethyl-6,6 dimethyl piperidine and 1-alkoxy-2,6 diethyl-2,3,6 dimethyl piperidine derivatives which are substituted in the 4 position by two oxygen atoms forming an open chain or cyclic ketal structure for controlled polymerization.Type: GrantFiled: September 20, 2007Date of Patent: August 11, 2009Assignee: Ciba Specialty Chemicals Corp.Inventors: Peter Nesvadba, Marie-Odile Zink, Wiebke Wunderlich
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Publication number: 20090186862Abstract: The present invention discloses a therapeutic target for the treatment of cystic fibrosis. It was found that inhibition of non-lysosomal glucosylceramidase (GBA2) sufficiently restores chloride current in cells from CF patients carrying the common delF508-CFTR mutation. With the catalytic centre (4) of the enzyme positioned on top of the membrane bilayer face particularly potent inhibitors are found in deoxynojirimycin derivatives having a group that is capable of inserting in the membrane bilayer.Type: ApplicationFiled: April 24, 2007Publication date: July 23, 2009Applicant: ACADEMISCH MEDISCH CENTRUMInventors: Johannes Maria Franciscus Gerardus Aerts, Rolf Gabriel Boot
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Publication number: 20090176830Abstract: A novel tartaric acid salt of Isofagomine (Isofagomine tartrate) that can be used for the treatment of Gaucher disease is provided. The invention also provides a crystalline form of isofagomine tartrate, method for preparing the salt, a pharmaceutical composition containing the salt, and a method of treating Gaucher disease.Type: ApplicationFiled: February 23, 2009Publication date: July 9, 2009Applicant: AMICUS THERAPEUTICS, INC.Inventors: Benjamin Mugrage, Kamlesh A. Sheth, David Palling, Philip Rybczynski
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Patent number: 7550599Abstract: Sterically hindered alkoxyamine and hydroxy substituted alkoxyamine stabilizer compounds are made water compatible via certain backbones with affinity towards water. The sterically hindered amines are for example of the formula where for example E and E? are 2-hydroxycyclohexyloxy, 2-hydroxy-2-methylpropoxy, benzyloxy, methoxy, propoxy, hexyloxy, heptyloxy, octyloxy or cyclohexyloxy, Rx is for example —NH2+CH2CH2OH Cl?, —NH3+?OAc, ?NOH, —NHCH(CH3)COO?K+, —NHCH2CH2N(CH3)2+?OAc, —NHCH2CH2SO3?K+, —NHCH(COO?K+)CH2CH2SCH3, —NHCH2COO?K+, —OCH(CH3)COO?K+, —OCH2CH2N(CH3)2+?OAc, —OCH2CH2SO3?K+, —OCH(COO?K+)CH2CH2SCH3 or —OCH2COO31K+, and where R5 comprises repeating units of —(OCH2CH2)—, —(OCH2CH2(CH3))—, —(CH2CHCOOH)—, —(CH2C(CH3)COOH)—, —(CH2CHCOOCH3)—, —(NHCH2CH2)—, —(CH2CHOH)—, —(CH2CHCONH2)— or —(CH2CH(NHCOH))—. These compounds are particularly effective in stabilizing aqueous polymer systems against the deleterious effects of oxidative, thermal and actinic radiation.Type: GrantFiled: May 25, 2005Date of Patent: June 23, 2009Assignee: Ciba Specialty Chemicals CorporationInventors: Mervin G. Wood, Robert Detlefsen, James Galbo, Wanda Martin, Paul Kondracki, Michael P. DiFazio, Joseph E. Babiarz
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Publication number: 20090137810Abstract: The subject invention provides methods and/or processes for making 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: ApplicationFiled: April 25, 2008Publication date: May 28, 2009Applicant: ARYx Therapeutics, Inc.Inventors: Kolbot By, J. B. Yeh, Ponny Pang
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Patent number: 7531555Abstract: The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotinic acetylcholine receptors by administering 2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH), or a pharmaceutically acceptable salt thereof, to the patient. In another aspect, the present invention pertains to pharmaceutical compositions containing TMPH, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. In another aspect, the present invention pertains to methods for selectively inhibiting nicotinic acetylcholine receptors that lack an ?5, ?6, or ?3 subunit by contacting an effective amount of TMPH, or a pharmaceutically acceptable salt thereof, to the receptor. The method for selectively inhibiting nicotinic acethylcholine receptors that lack an ?5 subunit can be carried out in vivo or in vitro.Type: GrantFiled: September 30, 2004Date of Patent: May 12, 2009Assignee: University of Florida Research Foundation, Inc.Inventors: Roger L. Papke, Nicole A. Horenstein, Michael M. Francis, Kyung Il Choi
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Publication number: 20090111699Abstract: Hindered amines represented by the general formula (I): (wherein R is an alkyl or hydroxyalkyl group having 1 to 30 carbon atoms or alkenyl having 2 to 30 carbon atoms; n is an integer of 1 to 4; when n is 1, R1 is alkyl having 1 to 22 carbon atoms, alkenyl having 2 to 22 carbon atoms, or a group represented by the general formula (III): (R is as defined above), while when n is 2 to 4, R1 is an n-valent organic group having 2 to 20 carbon atoms). When added to synthetic resins or coating materials, the amines can impart long-period stabilizing effect to the resins or the materials and exhibit excellent resistance to extraction with acid rain or chemicals.Type: ApplicationFiled: February 28, 2005Publication date: April 30, 2009Applicant: ADEKA CORPORATIONInventors: Yoshinori Negishi, Takashi Ayabe, Etsuo Tobita
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Patent number: 7521558Abstract: The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]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: August 15, 2005Date of Patent: April 21, 2009Assignee: Theravance, Inc.Inventors: Robert S. Chao, Miroslav Rapta, Pierre-Jean Colson
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Publication number: 20090082399Abstract: The present invention relates to new compounds which are Carbamate derivatives of formula I wherein X, B, P, Q5W, R1 and R2 are defined in the description.Type: ApplicationFiled: May 17, 2006Publication date: March 26, 2009Applicant: Addex Pharma SAInventors: Piergiuliano Bugada, Stefania Gagliardi, Giovanni Palombi, Jean-Philippe Rocher
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Publication number: 20090069469Abstract: Scorch is inhibited during the free-radical crosslinking of a crosslinkable polymer, e.g., an EPDM, by incorporating into the polymer before melt processing and crosslinking a scorch inhibiting amount of a derivative, preferably an ether, ester or urethane derivative, of a TEMPO compound, e.g., 4-hydroxy-tetrahydrocarbylpiperidin-1-oxyl. The scorch inhibitors of this invention perform as well, if not better, than their 4-hydroxy-tetrahydrocarbylpiperidin-1-oxyl counterparts in similar polymer compositions and under similar conditions in terms of scorch inhibition and ultimate degree of crosslinking, but exhibit less volatility and less migration within the polymer composition.Type: ApplicationFiled: November 10, 2008Publication date: March 12, 2009Inventors: Mohamed Esseghir, Bharat I. Chaudhary, Jeffrey M. Cogen, John Klier, Jinder Jow, Robert F. Eaton, Suzanne M. Guerra
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Publication number: 20090069375Abstract: The present application describes deuterium-enriched miglustat, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 12, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7501439Abstract: A novel tartaric acid salt of Isofagomine (Isofagomine tartrate) that can be used for the treatment of Gaucher disease is provided. The invention also provides a crystalline form of isofagomine tartrate, method for preparing the salt, a pharmaceutical composition containing the salt, and a method of treating Gaucher disease.Type: GrantFiled: May 23, 2007Date of Patent: March 10, 2009Assignee: Amicus Therapeutics, Inc.Inventors: Benjamin Mugrage, Kamlesh A Sheth, David Palling, Philip Rybczynski
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Publication number: 20090062261Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: February 21, 2007Publication date: March 5, 2009Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Makoto Adachi, Hidenori Mikamiyama, Akira Matsumura, Naoki Tsuno
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Publication number: 20090062339Abstract: The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotinic acetylcholine receptors by administering 2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH), or a pharmaceutically acceptable salt thereof, to the patient. In another aspect, the present invention pertains to pharmaceutical compositions containing TMPH, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. In another aspect, the present invention pertains to methods for selectively inhibiting nicotinic acetylcholine receptors that lack an ?5, ?6, or ?3 subunit by contacting an effective amount of TMPH, or a pharmaceutically acceptable salt thereof, to the receptor. The method for selectively inhibiting nicotinic acethylcholine receptors that lack an ?5 subunit can be carried out in vivo or in vitro.Type: ApplicationFiled: November 4, 2008Publication date: March 5, 2009Inventors: Roger L. Papke, Nicole A. Horenstein, Michael M. Francis, Kyung Il Choi
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Publication number: 20090042942Abstract: The invention provides compounds of formula (I), wherein R1, R2, R3, R4, R5, n and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation.Type: ApplicationFiled: April 18, 2006Publication date: February 12, 2009Applicant: ASTRAZENECA ABInventors: Andrew Bailey, David Donald
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Publication number: 20080287407Abstract: The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.Type: ApplicationFiled: December 10, 2004Publication date: November 20, 2008Applicant: NitroMed, Inc.Inventors: David S. Garvey, Xinqin Fang, Subhash P. Khanapure, Ramani R. Ranatunga, Shiow-Jyi Wey
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Publication number: 20080269285Abstract: The invention concerns the use of a compound of general formula (I) wherein: R0 represents in particular a hydrogen atom or an alkyl group; R1 represents in particular a hydrogen atom or an alkyl group; R2, R3 and R4 represent in particular, independently of one another, a hydrogen atom, a hydroxyl group, an alkoxy group or an acyloxy group, for preparing a medicine for treating lysosomal diseases related to a dysfunction of at least one lysosomal glycosidase enzyme.Type: ApplicationFiled: June 22, 2006Publication date: October 30, 2008Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Olivier Richard Martin, Philippe Compain, Charlotte Boucheron, Naoki Asano
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Publication number: 20080221332Abstract: The present invention relates water-soluble hindered amine compounds of the general formula (I): wherein G1 and G2 are independently alkyl of 1 to 4 carbon atoms or are together pentamethylene; Z1 and Z2 are each methyl, or Z1 and Z2 together form an unsubstituted linking moiety or a linking moiety substituted by one or more groups selected from an ester, ether, hydroxy, oxo, cyanohydrin, amide, amino, carboxy or an urethane group; E is alkoxy of 1 to 18 carbon atoms, cycloalkoxy of 5 to 12 carbon atoms or aralkoxy of 7 to 15 carbon atoms, or E is —O-T-(OH)b; T is a straight or branched chain alkylene of 1 to 18 carbon atoms, cycloalkylene of 5 to 18 carbon atoms, cycloalkenylene of 5 to 18 carbon atoms, a straight or branched chain alkylene of 1 to 4 carbon atoms substituted by phenyl or by phenyl substituted by one or two alkyl groups of 1 to 4 carbon atoms; b is 1, 2 or 3 with the proviso that b cannot exceed the number of carbon atoms in T, and when b is 2 or 3, each hydroxyl group is attached to a diType: ApplicationFiled: April 29, 2008Publication date: September 11, 2008Inventors: Marvin G. Wood, Robert E. Detlefsen, Joseph Suhadolink, Walter Renz
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Publication number: 20080161354Abstract: The present invention relates to stable S-nitrosothiols derivatives of formula (I) having vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparation of medicaments for treatment of NO related diseases. The invention also relates to a process for the synthesis of the compounds of formula (I).Type: ApplicationFiled: March 1, 2007Publication date: July 3, 2008Applicant: LACER, S.A.Inventors: Jose Repolles Moliner, Francisco Pubill Coy, Marisabel Mourelle Mancini, Juan Carlos del Castillo Nieto, Lydia Cabeza Llorente, Juan Martinez Bonin, Ana Modolell Saladrigas
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Publication number: 20080132543Abstract: A compound comprising a prodrug of a prostaglandin EP4 agonist, wherein said prodrug is an ester, ether, or amide of a carbohydrate; or said prodrug is an ester, ether, or amide of an amino acid is disclosed herein. Maintenance of the colonic mucosal barrier by method comprising administering a therapeutically effective amount of a prostaglandin EP4 agonist to a colon of a mammal is also disclosed herein. Dosage forms, medicaments, and compositions, related thereto are also disclosed.Type: ApplicationFiled: October 24, 2005Publication date: June 5, 2008Inventors: Wha Bin Im, Yariv Donde, Mark Holoboski, David W. Old, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Robert M. Burk, Todd Gac
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Publication number: 20080085973Abstract: Scorch is inhibited during the free-radical crosslinking of a crosslinkable polymer, e.g., an EPDM, by incorporating into the polymer before melt processing and crosslinking a scorch inhibiting amount of a derivative, preferably an ether, ester or urethane derivative, of a TEMPO compound, e.g., 4-hydroxy-tetrahydrocarbylpiperidin-1-oxyl. The scorch inhibitors of this invention perform as well, if not better, than their 4-hydroxy-tetrahydrocarbylpiperidin-1-oxyl counterparts in similar polymer compositions and under similar conditions in terms of scorch inhibition and ultimate degree of crosslinking, but exhibit less volatility and less migration within the polymer composition.Type: ApplicationFiled: October 9, 2006Publication date: April 10, 2008Inventors: Mohamed Esseghir, Bharat I. Chaudhary, Jeffrey M. Cogen, John Klier, Jinder Jow, Robert F. Eaton, Suzanne M. Guerra
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Patent number: 7345175Abstract: 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: June 7, 2006Date of Patent: March 18, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yan Chen
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Patent number: 7288613Abstract: The present invention relates to selected 1-alkoxy-2,2,6,6 tetramethyl piperidine, 1-alkoxy-2,2 diethyl-6,6 dimethyl piperidine and 1-alkoxy-2,6 diethyl-2,3,6 dimethyl piperidine derivatives which are substituted in the 4 position by two oxygen atoms forming an open chain or cyclic ketal structure, a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) said piperidine derivatives. Further aspects of the present invention are a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-2,2,6,6 tetramethyl piperidine, 1-alkoxy-2,2 diethyl-6,6 dimethyl piperidine and 1-alkoxy-2,6 diethyl-2,3,6 dimethyl piperidine derivatives which are substituted in the 4 position by two oxygen atoms forming an open chain or cyclic ketal structure for controlled polymerization.Type: GrantFiled: February 28, 2006Date of Patent: October 30, 2007Assignee: Ciba Specialty Chemicals Corp.Inventors: Peter Nesvadba, Marie-Odile Zink, Wiebke Wunderlich
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Patent number: 7265227Abstract: The invention provides compounds of formula (I) wherein: T is C(O) or S(O)2; W is C(O) or S(O)2; X is CH2, O or NH; Y is CR11 or N; n is 0, 1 or 2; m is 1 or, when Y is CR11 m is 0; R1 is optionally substituted aryl or optionally substituted heterocyclyl; R2, R3, R,4, R5, R6, R7 and R8 are, independently, hydrogen or C?1-6#191 alkyl; R9 is hydrogen or C1-C6 alkyl; R10 is alkyl, optionally substituted aryl, optionally substituted aralkyl or optionally substituted heterocyclyl; and R11 is hydrogen or C1-C6 allkyl; that are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis.Type: GrantFiled: July 19, 2002Date of Patent: September 4, 2007Assignee: AstraZeneca ABInventors: Richard Evans, Matthew Perry, Brian Springthorpe
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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: 7196099Abstract: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: February 26, 2004Date of Patent: March 27, 2007Assignees: Aventis Pharmaceuticals Inc., Axys Pharmaceuticals Inc.Inventors: Michael Graupe, James T. Palmer, David John Aldous, Sukanthini Thurairatnam
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Patent number: 7144897Abstract: Disclosed are compounds of formula X, which are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising compounds of formula X and methods of preparing the compounds of formula X are also disclosed.Type: GrantFiled: May 31, 2002Date of Patent: December 5, 2006Assignees: Elan Oharmaceuticals, Inc., Pharmacia & Upjohn, Co.Inventors: John Freskos, David L. Brown, Yvette M. Fobian, Larry Fang, Arthur Glenn Romero, Varghese John
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Patent number: 7129238Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.Type: GrantFiled: November 21, 2003Date of Patent: October 31, 2006Assignee: Hoffmann-La Roche Inc.Inventors: David William Banner, Luca Claudio Gobbi, Katrin Groebke Zbinden, Ulrike Obst, Christoph Martin Stahl
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Patent number: 7129228Abstract: 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: January 7, 2004Date of Patent: October 31, 2006Assignee: Sepracor Inc.Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
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Patent number: 7122551Abstract: Compounds of the formula I useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: GrantFiled: February 26, 2004Date of Patent: October 17, 2006Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Robert Ian Dowell, Maurice Raymond Verschoyle Finlay, Nicholas John Newcombe, Howard Tucker, David Waterson
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Patent number: 7109217Abstract: Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: November 6, 2003Date of Patent: September 19, 2006Assignee: Merck & Co., Inc.Inventors: Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca
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Patent number: 7091355Abstract: A crystalline salt according to formula (1): or the opposite enantiomer thereof, wherein X+ is a cation.Type: GrantFiled: December 21, 2001Date of Patent: August 15, 2006Assignee: Dow Global Technologies Inc.Inventor: Richard Lloyd
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Patent number: 7087759Abstract: Disclosed are MC-3/MC-4 receptor ligands, the ligands having the following formula: wherein A is a conformationally restricted ring system selected from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; wherein said rings comprises from 5 to 8 atoms; and W is a unit which preferable comprises D-1-fluorophenyalanine, Y comprises a heteroatom, and Z comprises an aromatic carbocyclic ring. Also disclosed are pharmaceutical compositions comprising the ligands of the invention as well as methods of treating diseases mediated through MC-3/MC-4 receptors.Type: GrantFiled: May 28, 2004Date of Patent: August 8, 2006Assignee: The Procter & Gamble CompanyInventors: Wieslaw Adam Mazur, Xinrong Tian, Xiufeng Eric Hu, Frank Hallock Ebetino
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Patent number: 7074803Abstract: The present invention provides high-concentration formulations of opioids such as fentanyl or fentanyl congeners. The formulation of the invention comprises fentanyl or a fentanyl congener in concentrations significantly in excess of conventional formulations, e.g., on the order about 2-fold to about 10,000-fold greater than conventional formulations, e.g., currently commercially available formulations. These formulations are particularly useful for long-term delivery to a subject suffering from pain. The invention further provides drug delivery devices comprising the high-concentration opioid formulations, and further provides methods of alleviating pain in a subject, comprising administering the high-concentration formulations to a subject in need thereof.Type: GrantFiled: March 2, 2001Date of Patent: July 11, 2006Assignee: Durect CorporationInventors: Dana Litmanovitz, Barbara J. F. Laidlaw
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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: 6989449Abstract: Selected chlorohydrin and cationic compounds containing nitroxide or hydroxylamine moieties are effective in stabilizing pulp or paper, especially pulp or paper containing lignin, against yellowing and discoloration due to the adverse effects of light. These compounds are added at various points in the paper-making process, especially at the wet ends, making the need for water soluble or water dispersible materials having high affinity for pulp or paper essential. This performance is often further enhanced by the presence of one or more coadditives selected from the group consisting of the UV absorbers, the polymeric inhibitors, the nitrones, the fluorescent whitening agents and metal chelating agents. Combinations of hydroxylamines or their salts, benzotriazole or benzophenone UV absorbers and a metal chelating agent are particularly effective.Type: GrantFiled: September 11, 2000Date of Patent: January 24, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Glen T. Cunkle, David Devore, Thomas F. Thompson
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Patent number: 6977260Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification.Type: GrantFiled: January 22, 2004Date of Patent: December 20, 2005Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 6967252Abstract: Novel flame retarding compounds that comprise at least one sterically hindered nitroxyl, hydroxylamine or hydrocarbyloxyamine moiety and at least one conventional organohalogen or organophosphorus flame retardant moiety, represented by where HA is independently of each other a sterically hindered nitroxyl, sterically hindered hydroxylamine or sterically hindered hydrocarbyloxyamine moiety, L is independently of each other a direct bond or chemical linking group, FRM is independently of each other an organohalogen or an organophosphorus flame reatardant moiety, and x, y and z are each independently greater than or equal to 1, are especially effective towards providing flame retardancy to organic polymer substrates.Type: GrantFiled: December 16, 2002Date of Patent: November 22, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Malisa V. Troutman, Ramanathan Ravichandran, Redina Kote, Roswell E. King
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Patent number: 6875888Abstract: In a process for preparing an ester of an unsaturated carboxylic acid by reacting an ester of the unsaturated carboxylic acid and a C1-C4-alkanol with an alcohol R3OH, where R3 is a C4-C20-alkyl radical, a C5-C7-cycloalkyl radical, a phenyl-C1-C4-alkyl radical or a C2-C12-alkyl radical substituted by at least one NR5R5 group or by from 1 to 3 hydroxyl groups or C1-C4-alkoxyl groups or interrupted by one or more oxygen atoms, where the radicals R5 are, independently of one another, C1-C6-alkyl or together with the nitrogen atom form a 5- to 7-membered heterocyclic ring which may contain a further nitrogen or oxygen atom, in the presence of a transesterification catalyst, the transesterification catalyst used is at least one metal alkanolate containing at least one OR1 group, where R1 is a 2,2,6,6-tetraalkyl-1-oxylpiperidin-4-yl radical.Type: GrantFiled: May 28, 2001Date of Patent: April 5, 2005Assignee: BASF AktiengesellschaftInventors: Gerhard Nestler, Jürgen Schröder
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Patent number: 6872832Abstract: Hindered amines substituted on the N-atom with an —O-E-OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O-E moieties.Type: GrantFiled: July 31, 2002Date of Patent: March 29, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: James Peter Galbo, Robert E. Detlefsen
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Patent number: 6852735Abstract: A compound of the formula (I): and a compound of the formula (V): as well as a compound of the formula (X): which are each a novel siastatin B derivative having a potent inhibitory activity against a glycosidase, are now synthesized by new processes. The compound of the formula (I), the compound of the formula (V) and the compound of the formula (X) have a potent enzyme-inhibitory activity to a glycosidase, which is particularly N-acetyl-galactosaminidase, galactosidase, glucosidase and mannosidase.Type: GrantFiled: December 24, 1999Date of Patent: February 8, 2005Assignees: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Meiji Seika Kaisha, Ltd.Inventors: Yoshio Nishimura, Eiki Shitara, Tomio Takeuchi
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Publication number: 20040198772Abstract: Designed imminocyclitols have potent inhibition activity with respect to hexoaminidases and glycosidases.Type: ApplicationFiled: March 10, 2004Publication date: October 7, 2004Applicant: The Scripps Research InstituteInventors: Chi-Huey Wong, Jungie Liu
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Patent number: 6790845Abstract: This invention relates generally to a novel class of fused heterocyclic compounds of the Formula (I) or Formula (II): or pharmaceutically acceptable salt forms thereof, which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.Type: GrantFiled: April 8, 2002Date of Patent: September 14, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Irina C. Jacobson, Mimi L. Quan, Ruth R. Wexler
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Publication number: 20040176309Abstract: The invention relates to Siglec inhibitors that have an increased affinity for the receptor molecule. The Siglec inhibitors provided by the invention are preferably selective of a given Siglec molecule. The invention further relates to a method for producing Siglec inhibitors and to a method for increasing the binding selectivity for a given Siglec molecule. The invention also relates to pharmaceutical compositions that contain the Siglec inhibitors and to medical indications for the Siglec inhibitors.Type: ApplicationFiled: February 13, 2004Publication date: September 9, 2004Inventors: Sorge Kelm, Reinhard Brossmer
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Patent number: 6784193Abstract: A compound of formula (I) wherein R2 is arylene or heterocyclene; or R and R2 together with the nitrogen atom to which they are attached form non-aromatic heterocyclene; and the other residues have various meanings, useful as pharmaceuticals, e.g. antimicrobials.Type: GrantFiled: January 28, 2002Date of Patent: August 31, 2004Assignee: Sandoz GmbHInventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
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Patent number: 6759430Abstract: The present invention relates to chemical compounds comprising a nitric oxide (NO) donor and a superoxide ion (O2−) scavenger, their preparation and their use in the treatment of conditions associated with oxidative stress or endothelial dysfunction. In particular, the present invention relates to chemical compounds of Formula (I) wherein: R1 may be the same of different and are independently selected from hydrogen, alkoyl, carboxy, hydroxy, amino, amido, cyano, nitro, thio, sulphonyl, sulphoxide alkyl groups comprising an NO-donor, provided that at least one R1 is a group comprising an NO-donor; R2 may be the same or different and are independently selected from alkyl groups; n is an integer 1, 2, or 3; or a salt thereof.Type: GrantFiled: July 25, 2002Date of Patent: July 6, 2004Assignee: OxoN Medica Inc.Inventors: Erik Emil Anggard, Abdullah Ibrahim Haj-Yehia
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Patent number: 6755875Abstract: Hindered amine compounds which are substituted by a long hydrocarbon chain are useful in a number of applications where the solubility or compatibility afforded by said substitution is needed. This is seen particularly for example with white, dyed, dipped, unscented and/or scanted candle wax which is effectively stabilized against discoloration and fading by the incorporation therein of a long chain hindered amine alone or in combination with a UV absorber and/or an antioxidant.Type: GrantFiled: September 6, 2002Date of Patent: June 29, 2004Assignee: Ciba Specialty Chemicals CorporationInventors: Mervin G. Wood, Andrea R. Smith, James P. Galbo
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Publication number: 20040097551Abstract: Compounds of formula (I): 1Type: ApplicationFiled: July 11, 2003Publication date: May 20, 2004Inventors: Terence D. Butters, Raymond A. Dwek, George WJ Fleet, Michael Glen Orchard, Frances Mary Platt