Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/220)
  • Patent number: 10266564
    Abstract: 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: Grant
    Filed: June 10, 2015
    Date of Patent: April 23, 2019
    Assignee: Council of Scientific & Industrial Research
    Inventors: Bathula Surendar Reddy, V.k.k. Durga Rao, Komal Sharma, M. Prathap Reddy, Dibyendu Banerjee, Deependra Kumar Singh
  • Patent number: 9181279
    Abstract: 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: Grant
    Filed: July 4, 2011
    Date of Patent: November 10, 2015
    Assignee: ROTTAPHARM BIOTECH S.R.L.
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Patent number: 9066960
    Abstract: 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: Grant
    Filed: August 22, 2007
    Date of Patent: June 30, 2015
    Assignee: INSTITUTE OF MATARIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES
    Inventors: Yuling Liu, Zhufang Shen, Zhen Chen, Renyun Wang, Xuejun Xia, Yueteng Chen, Quan Liu, Sujuan Sun, Mingzhi Xie
  • Publication number: 20150119366
    Abstract: 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: Application
    Filed: March 27, 2013
    Publication date: April 30, 2015
    Inventors: Yanming Du, Xiaodong Xu, Hong Ye, Jinhong Chang, Timothy M. Block
  • Publication number: 20150031670
    Abstract: 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: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GmbH
    Inventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
  • Patent number: 8841324
    Abstract: 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: Grant
    Filed: March 3, 2010
    Date of Patent: September 23, 2014
    Assignee: Merck Patent GmbH
    Inventors: Wolfgang Staehle, Kai Schiemann, Melanie Schultz
  • Patent number: 8822679
    Abstract: 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: Grant
    Filed: June 22, 2012
    Date of Patent: September 2, 2014
    Assignee: California Institute of Technology
    Inventors: Brian M Stoltz, Scott C. Virgil, David E White, Taiga Yurino, Yiyang Liu, Douglas C Behenna, Douglas Duquette, Christian Eidamshaus
  • Publication number: 20140024639
    Abstract: 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: Application
    Filed: July 19, 2013
    Publication date: January 23, 2014
    Inventors: Drew Adams, Mingji Dai, Stuart Schreiber, Mahmud Mustaqim Hussain, Zarko Boskovic
  • Patent number: 8604206
    Abstract: 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: Grant
    Filed: October 5, 2010
    Date of Patent: December 10, 2013
    Assignee: Amicus Therapeutics, Inc.
    Inventors: Robert Boyd, Gary Lee, Philip Rybczynski
  • Patent number: 8501782
    Abstract: 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: Grant
    Filed: July 23, 2008
    Date of Patent: August 6, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Daniel S. Gardner, John V. Duncia, John Hynes, T.G. Murali Dhar, Percy H. Carter, Joseph B. Santella
  • Publication number: 20130041106
    Abstract: 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: Application
    Filed: August 10, 2012
    Publication date: February 14, 2013
    Inventors: Erin E. Carlson, Darci Trader, Antoinette Odendaal
  • Publication number: 20130040990
    Abstract: 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: Application
    Filed: January 28, 2011
    Publication date: February 14, 2013
    Inventors: George William John Fleet, Terry Douglas Butters
  • Publication number: 20130012701
    Abstract: 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: Application
    Filed: June 22, 2012
    Publication date: January 10, 2013
    Applicant: California Institute of Technology
    Inventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
  • Publication number: 20110190307
    Abstract: 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: Application
    Filed: June 25, 2009
    Publication date: August 4, 2011
    Inventors: Catherina G. Becker, Thomas Becker
  • Publication number: 20110124867
    Abstract: 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: Application
    Filed: December 16, 2008
    Publication date: May 26, 2011
    Applicant: Schering Corporation
    Inventors: Frank Xing Chen, Timothy D. Cutarelli, Xiayong Fu, Xian Liang, Timothy L. McAllister, Robert K. Orr, Jianguo Yin, Kelvin H. Yong, Man Zhu
  • Publication number: 20110092706
    Abstract: 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: Application
    Filed: October 15, 2010
    Publication date: April 21, 2011
    Applicant: CarboDesign LLC
    Inventor: Milan Soukup
  • Patent number: 7846945
    Abstract: 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: Grant
    Filed: March 4, 2008
    Date of Patent: December 7, 2010
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins
  • Patent number: 7671059
    Abstract: 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: Grant
    Filed: September 28, 2006
    Date of Patent: March 2, 2010
    Assignee: Novartis AG
    Inventors: 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
  • Patent number: 7544682
    Abstract: 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: Grant
    Filed: January 8, 2007
    Date of Patent: June 9, 2009
    Assignee: Sanofi-Aventis
    Inventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Pierre Perreaut
  • Publication number: 20090143592
    Abstract: 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: Application
    Filed: December 3, 2007
    Publication date: June 4, 2009
    Applicant: Novo Nordisk A/S
    Inventors: 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
  • Publication number: 20080260651
    Abstract: 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: Application
    Filed: April 15, 2008
    Publication date: October 23, 2008
    Applicant: GE HEALTHCARE AS
    Inventors: Veronique Morisson-Iveson, Joanna Marie Passmore
  • Publication number: 20080221164
    Abstract: 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: Application
    Filed: March 4, 2008
    Publication date: September 11, 2008
    Inventors: Nicole C. Goodwin, Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins
  • Patent number: 7402639
    Abstract: 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: Grant
    Filed: January 14, 2005
    Date of Patent: July 22, 2008
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Andreas Kramer, Peter Nesvadba
  • Patent number: 7368443
    Abstract: 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: Grant
    Filed: March 31, 2004
    Date of Patent: May 6, 2008
    Assignee: University of Kentucky Research Foundation
    Inventors: Peter A. Crooks, Linda Dwoskin, Marlon D. Jones, Dennis Keith Miller, Seth Davin Norholm, Guangrong Zheng, Sairam Krishamurthy
  • Patent number: 7223779
    Abstract: 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: Grant
    Filed: June 26, 2003
    Date of Patent: May 29, 2007
    Assignee: Carna Biosciences Inc.
    Inventors: Takahiro Tsukida, Hideki Moriyama, Koichi Yokota, Mariko Hatakeyama, Shinichiro Nishimura
  • Patent number: 7189742
    Abstract: 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: Grant
    Filed: August 22, 2002
    Date of Patent: March 13, 2007
    Assignee: Prestwick Pharmaceuticals, Inc.
    Inventor: Maurice Ward Gittos
  • Patent number: 7034015
    Abstract: 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: Grant
    Filed: August 28, 2002
    Date of Patent: April 25, 2006
    Assignee: Leo Pharma A/S
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
  • Patent number: 6989449
    Abstract: 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: Grant
    Filed: September 11, 2000
    Date of Patent: January 24, 2006
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Glen T. Cunkle, David Devore, Thomas F. Thompson
  • Patent number: 6967196
    Abstract: 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: Grant
    Filed: February 22, 2000
    Date of Patent: November 22, 2005
    Assignees: 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
  • Patent number: 6956046
    Abstract: 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: Grant
    Filed: May 17, 2002
    Date of Patent: October 18, 2005
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Ichiro Yamamoto, Kazuyuki Matsuura, Kazuhiro Suzuki, Kazuo Kato, Yasushige Akada, Hidenori Mochizuki, Akihito Shimoi
  • Patent number: 6946269
    Abstract: 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: Grant
    Filed: December 4, 2003
    Date of Patent: September 20, 2005
    Assignee: Sanofi-Aventis
    Inventors: Bertrand Castro, Jean-Robert Dormoy, Alain Rabion
  • Patent number: 6943179
    Abstract: 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 tumors
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: September 13, 2005
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Bertram Cezanne, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
  • Patent number: 6943177
    Abstract: 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: Grant
    Filed: August 30, 2002
    Date of Patent: September 13, 2005
    Assignee: University of Kentucky Research Foundation
    Inventors: Linda P. Dwoskin, Peter A. Crooks, Marlon D. Jones
  • Patent number: 6927294
    Abstract: 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: Grant
    Filed: March 10, 2003
    Date of Patent: August 9, 2005
    Assignee: University of Southern California
    Inventors: Nicos A. Petasis, Xin Yao, Jeffrey C. Raber
  • Patent number: 6750228
    Abstract: 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: Grant
    Filed: May 12, 2000
    Date of Patent: June 15, 2004
    Assignee: Pharmacia Corporation
    Inventors: 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
  • Publication number: 20040110796
    Abstract: 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: Application
    Filed: December 4, 2003
    Publication date: June 10, 2004
    Inventors: Bertrand Castro, Jean-Robert Dormoy, Alain Rabion
  • Patent number: 6689909
    Abstract: 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: Grant
    Filed: June 17, 2002
    Date of Patent: February 10, 2004
    Assignee: AstraZeneca AB
    Inventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows
  • Patent number: 6670477
    Abstract: 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: Grant
    Filed: March 4, 2002
    Date of Patent: December 30, 2003
    Assignee: Novartis AG
    Inventors: Wen-Chung Shieh, Song Xue, Noela Marjory Reel, John Joseph Fitt
  • Patent number: 6610851
    Abstract: 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 ca
    Type: Grant
    Filed: October 25, 2000
    Date of Patent: August 26, 2003
    Assignee: Sumika Fine Chemicals Co., Ltd.
    Inventors: Kiyoshi Sugi, Nobushige Itaya, Tadashi Katsura, Masami Igi, Shigeya Yamazaki, Taro Ishibashi, Teiji Yamaoka, Yoshihiro Kawada, Yayoi Tagami
  • Patent number: 6590102
    Abstract: 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: Grant
    Filed: November 27, 2000
    Date of Patent: July 8, 2003
    Assignee: Asahi Glass Company Ltd.
    Inventors: Shu-zhong Wang, Takashi Okazoe, Yasushi Matsumura, Nobuaki Mori, Jiro Nishino, Kazuhiro Ookura
  • Patent number: 6586598
    Abstract: 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: Grant
    Filed: May 8, 2002
    Date of Patent: July 1, 2003
    Assignee: Geneva Pharmaceuticals, Inc.
    Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
  • Patent number: 6552225
    Abstract: 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: Grant
    Filed: June 17, 2002
    Date of Patent: April 22, 2003
    Assignee: AstraZeneca AB
    Inventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows
  • Patent number: 6534536
    Abstract: 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: Grant
    Filed: March 16, 1994
    Date of Patent: March 18, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau
  • Patent number: 6472529
    Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Grant
    Filed: April 18, 2001
    Date of Patent: October 29, 2002
    Assignee: Abbott Laboratories
    Inventors: 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
  • Patent number: 6469173
    Abstract: 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: Grant
    Filed: June 12, 2001
    Date of Patent: October 22, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Bertrand Castro, Jean-Robert Dormoy, Alain Rabion
  • Patent number: 6452012
    Abstract: This invention relates to 3-(3-phenyl-2,6-dioxopiperidin-3-yl) propionamide derivatives, and to processes for preparing the same.
    Type: Grant
    Filed: November 13, 2001
    Date of Patent: September 17, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Bertrand Castro, Hélène Mattras, Aldo Previero
  • Patent number: 6444190
    Abstract: 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: Grant
    Filed: March 4, 1999
    Date of Patent: September 3, 2002
    Assignee: FMC Corporation
    Inventors: Anne Pautard-Cooper, Eric John Granger, Philip Franklin Sims, James Anthony Schwindeman, John Francis Engel, Terry Lee Rathman
  • Publication number: 20020019534
    Abstract: A compound of the formula 1
    Type: Application
    Filed: March 27, 2001
    Publication date: February 14, 2002
    Inventor: Mark C. Noe
  • Patent number: 6342607
    Abstract: This invention relates to 3-(3-phenyl-2,6-dioxopiperidin-3-yl)propionamide derivatives, and to processes for preparing the same.
    Type: Grant
    Filed: June 12, 2001
    Date of Patent: January 29, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Bertrand Castro, Hélène Mattras, Aldo Previero
  • Patent number: RE39263
    Abstract: There is disclosed substituted thiocarboxamides of the general formula (I) useful as herbicides.
    Type: Grant
    Filed: December 12, 2003
    Date of Patent: September 5, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karl-Heinz Linker, Kurt Findeisen, Roland Andree, Mark-Wilhelm Drewes, Andreas Lender, Otto Schallner, Wilhelm Haas, Hans-Joachim Santel, Markus Dollinger