Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/220)
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Patent number: 10266564Abstract: The present invention relates to the cationic lipid cordiaroimide hybrid compounds of formula I. The present invention provides a process for preparation of these compounds is also being elaborated. The compounds described provides anticancerous activity against cell lines including PC-3 (prostate cancer), HepG2 (liver cancer), MCF-7 (breast cancer) and NIH-1/3T3 (non cancer cells. The compound was also capable of inducing caspase-3 mediated apoptosis in HepG2 cells by arresting the cell cycle in the G1 phase. Furthermore, the compound exhibited DNA ligase I inhibition. The present class of cationic lipid cordiarimide hybrids is likely to find specific use in developing novel targeted therapies for liver and prostate cancers.Type: GrantFiled: June 10, 2015Date of Patent: April 23, 2019Assignee: Council of Scientific & Industrial ResearchInventors: Bathula Surendar Reddy, V.k.k. Durga Rao, Komal Sharma, M. Prathap Reddy, Dibyendu Banerjee, Deependra Kumar Singh
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Patent number: 9181279Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.Type: GrantFiled: July 4, 2011Date of Patent: November 10, 2015Assignee: ROTTAPHARM BIOTECH S.R.L.Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
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Patent number: 9066960Abstract: The present invention relates to an effective fraction of alkaloids and the effective fraction is prepared from mulberry twig and its active ingredients are a composition of alkaloids. Determined by HPLC, the percentage of the total alkaloids are 50% or more by weight in the effective fraction and the percentage of the compound 1-deoxynojirimycin is 30% or more by weight in the total alkaloids. The effective fraction of the invention is prepared as the following steps: the mulberry twig is extracted by solvents, and the extract is precipitated by alcohol precipitation or flocculation to remove the impurities, and then concentrated, purified by resin chromatography. The present invention also relates to a pharmaceutical composition containing the said effective fraction of alkaloids and to the use of the effective fraction of alkaloids according to claim 1-4 in preparing hypoglycemic agents.Type: GrantFiled: August 22, 2007Date of Patent: June 30, 2015Assignee: INSTITUTE OF MATARIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCESInventors: Yuling Liu, Zhufang Shen, Zhen Chen, Renyun Wang, Xuejun Xia, Yueteng Chen, Quan Liu, Sujuan Sun, Mingzhi Xie
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Publication number: 20150119366Abstract: Pharmaceutical compositions of the invention comprise alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include Viral hemorrhagic fevers, and any other diseases involving glucosidase activity.Type: ApplicationFiled: March 27, 2013Publication date: April 30, 2015Inventors: Yanming Du, Xiaodong Xu, Hong Ye, Jinhong Chang, Timothy M. Block
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Publication number: 20150031670Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.Type: ApplicationFiled: March 21, 2013Publication date: January 29, 2015Applicant: MERCK PATENT GmbHInventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
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Patent number: 8841324Abstract: Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumors.Type: GrantFiled: March 3, 2010Date of Patent: September 23, 2014Assignee: Merck Patent GmbHInventors: Wolfgang Staehle, Kai Schiemann, Melanie Schultz
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Patent number: 8822679Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.Type: GrantFiled: June 22, 2012Date of Patent: September 2, 2014Assignee: California Institute of TechnologyInventors: Brian M Stoltz, Scott C. Virgil, David E White, Taiga Yurino, Yiyang Liu, Douglas C Behenna, Douglas Duquette, Christian Eidamshaus
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Publication number: 20140024639Abstract: Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.Type: ApplicationFiled: July 19, 2013Publication date: January 23, 2014Inventors: Drew Adams, Mingji Dai, Stuart Schreiber, Mahmud Mustaqim Hussain, Zarko Boskovic
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Patent number: 8604206Abstract: The present invention provides novel compounds as well as compositions and methods using the same for preventing and/or treating degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Parkinson's disease.Type: GrantFiled: October 5, 2010Date of Patent: December 10, 2013Assignee: Amicus Therapeutics, Inc.Inventors: Robert Boyd, Gary Lee, Philip Rybczynski
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Patent number: 8501782Abstract: The present application describes modulators of MIP-1? of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.Type: GrantFiled: July 23, 2008Date of Patent: August 6, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Daniel S. Gardner, John V. Duncia, John Hynes, T.G. Murali Dhar, Percy H. Carter, Joseph B. Santella
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Publication number: 20130041106Abstract: Chemoselective isolation of hydroxyl group-containing and carboxyl group-containing compounds is accomplished via formation of polymeric silyl ethers and polymeric siloxyl esters, respectively. Preparation of chemoselective polymeric reagents for capture of hydroxyl group containing compounds and carboxyl group containing compounds is described.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Inventors: Erin E. Carlson, Darci Trader, Antoinette Odendaal
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Publication number: 20130040990Abstract: A convenient and scalable synthesis of DGJNAc ID from D-glucuronolactone in an overall yield of 20% is provided. DGJNAc is the first highly potent and specific competitive inhibitor of GalNAcases. DGJNAc ID is also a competitive inhibitor of -hexosaminidases. Synthesis and activity of L-DGJNAc IL is also shown. The use of DGJNAc as a potent and specific inhibitor of GalNAcases will allow useful investigation and treatment of a number of diseases, including Schindler Disease.Type: ApplicationFiled: January 28, 2011Publication date: February 14, 2013Inventors: George William John Fleet, Terry Douglas Butters
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Publication number: 20130012701Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.Type: ApplicationFiled: June 22, 2012Publication date: January 10, 2013Applicant: California Institute of TechnologyInventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
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Publication number: 20110190307Abstract: The present invention provides zebrafish based methods for the identification of compounds potentially useful in the treatment of motor neuron degenerative diseases (MNDDs), compounds identified by these methods and compositions, methods and medicaments for treating MNDDs.Type: ApplicationFiled: June 25, 2009Publication date: August 4, 2011Inventors: Catherina G. Becker, Thomas Becker
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Publication number: 20110124867Abstract: The present invention relates to novel processes for the preparation of the compound of the Formula A45: or a physiologically acceptable salt, solvate or prodrug thereof, which has utility, for example, as a pharmaceutically active compound with CXCR3 antagonist activity, and to novel intermediates useful in the synthesis thereof.Type: ApplicationFiled: December 16, 2008Publication date: May 26, 2011Applicant: Schering CorporationInventors: Frank Xing Chen, Timothy D. Cutarelli, Xiayong Fu, Xian Liang, Timothy L. McAllister, Robert K. Orr, Jianguo Yin, Kelvin H. Yong, Man Zhu
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Publication number: 20110092706Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially rennin inhibitors such as Aliskiren. The invention describes a preparation of enantiomerically pure 8-aryloctanoic acids of general formula I from readily available key intermediate, a novel bicyclic compound of formula IV.Type: ApplicationFiled: October 15, 2010Publication date: April 21, 2011Applicant: CarboDesign LLCInventor: Milan Soukup
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Patent number: 7846945Abstract: Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.Type: GrantFiled: March 4, 2008Date of Patent: December 7, 2010Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins
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Patent number: 7671059Abstract: Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases.Type: GrantFiled: September 28, 2006Date of Patent: March 2, 2010Assignee: Novartis AGInventors: Timothy D. Machajewski, Cynthia M. Shafer, Christopher McBride, William Antonios-McCrea, Brandon M. Doughan, Barry H. Levine, Yi Xia, Maureen McKenna, X. Michael Wang, Kris Mendenhall, Yasheen Zhou, Kristin Brinner, Zhenhai Gao, Daniel Poon, Paul Barsanti, Xiaodong Lin, Abran Costales, Alice Rico, Nathan Brammeier, Teresa Pick, Paul A. Renhowe
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Patent number: 7544682Abstract: The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.Type: GrantFiled: January 8, 2007Date of Patent: June 9, 2009Assignee: Sanofi-AventisInventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Pierre Perreaut
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Publication number: 20090143592Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.Type: ApplicationFiled: December 3, 2007Publication date: June 4, 2009Applicant: Novo Nordisk A/SInventors: Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Josef Vagner, Inge Thoger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thogersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Anker Steen Jogensen, Janos Tibor Kodra, Shenghua Shi
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Publication number: 20080260651Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic N-heterocyclic central moiety such as pyrrolidine or piperidine heterocycles allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging, in particular in X-ray imaging, and to contrast media containing such compounds.Type: ApplicationFiled: April 15, 2008Publication date: October 23, 2008Applicant: GE HEALTHCARE ASInventors: Veronique Morisson-Iveson, Joanna Marie Passmore
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Publication number: 20080221164Abstract: Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.Type: ApplicationFiled: March 4, 2008Publication date: September 11, 2008Inventors: Nicole C. Goodwin, Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins
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Patent number: 7402639Abstract: The present invention relates to 1-alkoxy-polyalkyl-peridine derivatives containing a structural element of formula (I) G1, G2, G3, G4 are independently C1-C6alkyl with the proviso that at least one is not methyl or G1 and G2 or G3 and G4, or G1 and G2 and G3 and G4 together form a C5-C12cycloalkyl group; G5, G6 independently are H, C1-C18alkyl, phenyl, naphthyl or a group COOC1-C18alkyl and X represents a group such that the free radical X• derived from X is capable of initiating polymerization of ethylenically unsaturated monomers, with the proviso that compounds A1 and A2 are excluded Further subjects of the invention are a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 1-alkoxy-polyalkyl-piperidine derivative, a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-polyalkyl-piperidine derivatives for controlled polymerization.Type: GrantFiled: January 14, 2005Date of Patent: July 22, 2008Assignee: Ciba Specialty Chemicals Corp.Inventors: Andreas Kramer, Peter Nesvadba
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Patent number: 7368443Abstract: The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: which are used to treat diseases of the central nervous system, drug abuse, and withdrawal therefrom as well as treating eating disorders.Type: GrantFiled: March 31, 2004Date of Patent: May 6, 2008Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Linda Dwoskin, Marlon D. Jones, Dennis Keith Miller, Seth Davin Norholm, Guangrong Zheng, Sairam Krishamurthy
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Patent number: 7223779Abstract: A novel azasugar derivative, and a drug containing the same as an active ingredient are disclosed. The drug is useful for treatment of keratinocyte-proliferative diseases.Type: GrantFiled: June 26, 2003Date of Patent: May 29, 2007Assignee: Carna Biosciences Inc.Inventors: Takahiro Tsukida, Hideki Moriyama, Koichi Yokota, Mariko Hatakeyama, Shinichiro Nishimura
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Patent number: 7189742Abstract: Novel bisulphate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4-dimethylpiperidin-2,6-diones and pharmacologically acceptable solvates thereof are devoid of the weight loss and hepatocyte changes in the rat which limited to marginally effective levels the permitted clinical doses of the corresponding hydrochlorides in the treatment or prophylaxis of stress-related affective disorders such as anxiety, depression, migraine and sleep apnea. The preferred bisulphate salts are 3(3,5-dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione bisulphate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione bisulphate.Type: GrantFiled: August 22, 2002Date of Patent: March 13, 2007Assignee: Prestwick Pharmaceuticals, Inc.Inventor: Maurice Ward Gittos
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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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: 6967196Abstract: In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid ? protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.Type: GrantFiled: February 22, 2000Date of Patent: November 22, 2005Assignees: Bristol-Myers Squibb Company, Merck & Co. Inc.Inventors: David W. Smith, Benito Munoz, Kumar Srinivasan, Carl P. Bergstrom, Prasad V. Chaturvedula, Milind S. Deshpande, Daniel J. Keavy, Wai Yu Lau, Michael F. Parker, Charles P. Sloan, Owen B. Wallace, Henry Hui Wang
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Patent number: 6956046Abstract: A compound represented by the following Formula (I): (wherein A represents oxygen atom or —NR3— (R3 represents hydrogen atom or lower alkyl group); R1 represents nitro group, lower alkoxycarbonyl group, carbamoyl group unsubstituted or mono- or di-substituted by lower alkyl group, unprotected or protected hydroxyl group, unprotected or protected carboxyl group, lower alkyl group substituted by unprotected or protected hydroxyl group, or tetrazolyl group; and R2 represents hydrogen atom, cyano group or lower alkylsulfonyl group, provided that when A is —NR3—, it is excluded that R1 represents unprotected or protected hydroxyl group or lower alkyl group substituted by unprotected or protected hydroxyl group) or its salt, and method for producing the compound, and a pharmaceutical composition containing the compound as active ingredient.Type: GrantFiled: May 17, 2002Date of Patent: October 18, 2005Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Ichiro Yamamoto, Kazuyuki Matsuura, Kazuhiro Suzuki, Kazuo Kato, Yasushige Akada, Hidenori Mochizuki, Akihito Shimoi
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Patent number: 6946269Abstract: The invention relates to lower-alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid derivatives, and to processes for preparing the same.Type: GrantFiled: December 4, 2003Date of Patent: September 20, 2005Assignee: Sanofi-AventisInventors: Bertrand Castro, Jean-Robert Dormoy, Alain Rabion
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Patent number: 6943177Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating disorders.Type: GrantFiled: August 30, 2002Date of Patent: September 13, 2005Assignee: University of Kentucky Research FoundationInventors: Linda P. Dwoskin, Peter A. Crooks, Marlon D. Jones
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Patent number: 6943179Abstract: Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumorsType: GrantFiled: February 27, 2002Date of Patent: September 13, 2005Assignee: Merck Patent GmbHInventors: Werner Mederski, Bertram Cezanne, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Patent number: 6927294Abstract: Functionalized nitrogen heterocyclic compounds, including benzodiazepines and azasugars, and synthetic methods for preparing such compounds. Nitrogen-containing heterocycles are prepared by reacting amino-carbonyl compounds that contain an amine moiety connected via a linker to a carbonyl moiety with an organoboron derivative.Type: GrantFiled: March 10, 2003Date of Patent: August 9, 2005Assignee: University of Southern CaliforniaInventors: Nicos A. Petasis, Xin Yao, Jeffrey C. Raber
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Patent number: 6750228Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: GrantFiled: May 12, 2000Date of Patent: June 15, 2004Assignee: Pharmacia CorporationInventors: Thomas E Barta, Daniel P Becker, Louis J Bedell, Terri L Boehm, Jeffrey N Carroll, Gary A DeCrescenzo, Yvette M Fobian, John N Freskos, Daniel P Getman, Joseph J McDonald, Madeleine H Li, Susan L Hockerman, Susan C Howard, Steve A Kolodziej, Deborah A Mischke, Joseph G Rico, Nathan W Stehle, Michael B Tollefson, William F Vernier, Clara I Villamil
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Publication number: 20040110796Abstract: The invention relates to lower-alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid derivatives, and to processes for preparing the same.Type: ApplicationFiled: December 4, 2003Publication date: June 10, 2004Inventors: Bertrand Castro, Jean-Robert Dormoy, Alain Rabion
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Patent number: 6689909Abstract: A compound of formula (I) wherein: n is 1 or 2; R1 is chloro, fluoro, bromo, methyl or methoxy; R2 is as defined within; R3 is as defined within; and R4 is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.Type: GrantFiled: June 17, 2002Date of Patent: February 10, 2004Assignee: AstraZeneca ABInventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows
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Patent number: 6670477Abstract: A process for making enantiomerically enriched 4-piperidinylglycine having the formula (I), said process comprising (a) combining N-protected glycine ester with 4-piperidone to form didehydroamino acid ester; (b) reducing the didehydroamino acid ester with hydrogen gas in the presence of a rhodium catalyst selected from the group consisting of (R,R)-BPE-Rh; (S,S)-BPE-Rh; (R,R)-DuPHOS-Rh; (S,S)-DuPHOS-Rh; and combinations thereof; whereby a protected compound is formed; and (c) removing the protecting groups from the protected compound, whereby the 4-piperidinylglyeine having the formula (I) is formed, wherein X− is an anion wherein X is independently a halogen; and “*” designates an asymmetric carbon having (R)- or (S)-configuration. The process of the invention yields an enantiomerically enriched (R)-4-piperidineglycine or (S)-4-piperidineglycine.Type: GrantFiled: March 4, 2002Date of Patent: December 30, 2003Assignee: Novartis AGInventors: Wen-Chung Shieh, Song Xue, Noela Marjory Reel, John Joseph Fitt
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Patent number: 6610851Abstract: A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is caType: GrantFiled: October 25, 2000Date of Patent: August 26, 2003Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Kiyoshi Sugi, Nobushige Itaya, Tadashi Katsura, Masami Igi, Shigeya Yamazaki, Taro Ishibashi, Teiji Yamaoka, Yoshihiro Kawada, Yayoi Tagami
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Patent number: 6590102Abstract: A process for producing a piperidinecarbinol represented by the general formula (2), which comprises reducing the trans isomer of a compound represented by the general formula (1): wherein R1 is a hydrogen atom, a lower alkyl group or an aralkyl group, R2 is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, and X is a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, a dialkylamino group, an alkylthio group, an arylthio group or CmF2m+1— wherein m is an integer of from 1 to 20.Type: GrantFiled: November 27, 2000Date of Patent: July 8, 2003Assignee: Asahi Glass Company Ltd.Inventors: Shu-zhong Wang, Takashi Okazoe, Yasushi Matsumura, Nobuaki Mori, Jiro Nishino, Kazuhiro Ookura
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Patent number: 6586598Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.Type: GrantFiled: May 8, 2002Date of Patent: July 1, 2003Assignee: Geneva Pharmaceuticals, Inc.Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
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Patent number: 6552225Abstract: A compound of formula (I) wherein: R1, R2, R3, R4, R5, R6 and R7 are as defined within; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.Type: GrantFiled: June 17, 2002Date of Patent: April 22, 2003Assignee: AstraZeneca ABInventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows
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Patent number: 6534536Abstract: Alkylsulfonamido heterocyclic thrombin inhibitors are provided which have the structure wherein G is wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; R is hydrogen, hydroxyalkyl, aminoalkyl, alkyl, cycloalkyl, amidoalkyl, arylalkyl, alkenyl, aryl, alkynyl, arylalkoxyalkyl, or an amino acid side chain; R1 and R2 are independently hydrogen, lower alkyl, cycloalkyl, aryl, hydroxy, alkoxy, oxo, thioketal, thioalkyl, thioaryl, amino or alkylamino; or R1 and R2 can be taken together with the carbons to which they are attached to form a cycloalkyl, aryl or heteroaryl ring.Type: GrantFiled: March 16, 1994Date of Patent: March 18, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau
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Patent number: 6472529Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: April 18, 2001Date of Patent: October 29, 2002Assignee: Abbott LaboratoriesInventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Patent number: 6469173Abstract: The invention relates to lower-alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid derivatives, and to processes for preparing the same.Type: GrantFiled: June 12, 2001Date of Patent: October 22, 2002Assignee: Sanofi-SynthelaboInventors: Bertrand Castro, Jean-Robert Dormoy, Alain Rabion
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Patent number: 6452012Abstract: This invention relates to 3-(3-phenyl-2,6-dioxopiperidin-3-yl) propionamide derivatives, and to processes for preparing the same.Type: GrantFiled: November 13, 2001Date of Patent: September 17, 2002Assignee: Sanofi-SynthelaboInventors: Bertrand Castro, Hélène Mattras, Aldo Previero
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Patent number: 6444190Abstract: Novel reduction compositions are prepared from an active hydride, an additive, and a Lewis base in a hydrocarbon solvent. Such compositions can provide a superior reducing system for organic substrates.Type: GrantFiled: March 4, 1999Date of Patent: September 3, 2002Assignee: FMC CorporationInventors: Anne Pautard-Cooper, Eric John Granger, Philip Franklin Sims, James Anthony Schwindeman, John Francis Engel, Terry Lee Rathman
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Publication number: 20020019534Abstract: A compound of the formula 1Type: ApplicationFiled: March 27, 2001Publication date: February 14, 2002Inventor: Mark C. Noe
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Patent number: 6342607Abstract: This invention relates to 3-(3-phenyl-2,6-dioxopiperidin-3-yl)propionamide derivatives, and to processes for preparing the same.Type: GrantFiled: June 12, 2001Date of Patent: January 29, 2002Assignee: Sanofi-SynthelaboInventors: Bertrand Castro, Hélène Mattras, Aldo Previero
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Patent number: RE39263Abstract: There is disclosed substituted thiocarboxamides of the general formula (I) useful as herbicides.Type: GrantFiled: December 12, 2003Date of Patent: September 5, 2006Assignee: Bayer AktiengesellschaftInventors: Karl-Heinz Linker, Kurt Findeisen, Roland Andree, Mark-Wilhelm Drewes, Andreas Lender, Otto Schallner, Wilhelm Haas, Hans-Joachim Santel, Markus Dollinger