At Least Three Chalcogens Bonded Directly To The Thiazole Ring Patents (Class 548/210)
  • Publication number: 20150119428
    Abstract: Mew tranilast complexes and new tranilast cocrystals are disclosed. These include all tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-amtnoben2oic acid complex, a 1:1 tranilast 4-am!nobers2oic acid cocrystal, a 1:1 tranilast 2,4-di?hydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystais as well as the pharmaceutical compositions are disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: April 30, 2015
    Inventors: Joanne Holland, Christopher Frampton
  • Publication number: 20150031685
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 29, 2015
    Applicant: Dr. Reeddy's Laboratories Ltd.
    Inventors: Pradip Kumar Sasmal, Chintakunta Vamseekrishna, Vijay Potluri, Ashok Tehim, Yonghua Gai, Hang Zhang
  • Publication number: 20130252953
    Abstract: The present invention relates to novel TMPK inhibitor compositions and their methods of use. In particular, it relates to novel TMPK inhibitor compositions and therapeutics that lead to dUTP-mediated DNA repair in tumor cells and acts as a novel chemosensitizer, which are useful in methods for treating or preventing cancers.
    Type: Application
    Filed: November 29, 2011
    Publication date: September 26, 2013
    Inventors: Zee-Fen Chang, Jim-Min Fang, Chun-Mei Hu, Ming-Tyng Yeh
  • Patent number: 8153658
    Abstract: To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: April 10, 2012
    Assignee: Astellas Pharma, Inc.
    Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
  • Patent number: 8093397
    Abstract: A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1?6-benzo[d]isothiazol-3-one, preferably in the presence of an organic base.
    Type: Grant
    Filed: October 6, 2008
    Date of Patent: January 10, 2012
    Assignee: Avecia Biotechnology, Inc.
    Inventors: Nanda Sinha, William Edward Zedalis, Gregory Keith Miranda
  • Publication number: 20110039874
    Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.
    Type: Application
    Filed: April 16, 2010
    Publication date: February 17, 2011
    Applicant: Northeastern University
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
  • Publication number: 20100173377
    Abstract: Compounds having two reactive functional groups are described that can be used to provide a connector group between a substrate and an amine-containing material. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonylaminocarbonyl group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a carbonylimino-containing connector group. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.
    Type: Application
    Filed: January 21, 2010
    Publication date: July 8, 2010
    Inventors: Karl E. Benson, Moses M. David, Cary A. Kipke, Brinda B. Lakshmi, Charles M. Leir, George G. Moore, Rahul Shah
  • Publication number: 20090318704
    Abstract: Provided are processes for the preparation of N-(2-Acetyl-4,6-dimethylphenyl)-3-{[(3,4-dimethyl-5-isoxazolyl)amino]sulfonyl}-2-thiophenecarboxamide, a compound useful for the treatment of endothelin-mediated disorders.
    Type: Application
    Filed: August 3, 2007
    Publication date: December 24, 2009
    Inventor: John F. Reichwein
  • Patent number: 7635772
    Abstract: A process for the synthesis of an oligonucleotide is provided in which an oligonucleotide is assembled on a swellable solid support using the phosphoramidite approach in the presence of an activator, wherein the activator is not tetrazole or a substituted tetrazole. Preferred activators are pyridinium, imidazolinium and benzimidazolinium salts; benzotriazole and derivatives thereof; and saccharin or a saccharin derivative. Preferred swellable solid supports comprise functionalised polystyrene, partially hydrolysed polyvinylacetate or poly(acrylamide).
    Type: Grant
    Filed: December 16, 2003
    Date of Patent: December 22, 2009
    Assignee: Avecia Biotechnology Inc.
    Inventor: Paul McCormac
  • Publication number: 20090085006
    Abstract: A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1?6-benzo[d]isothiazol-3-one, preferably in the presence of an organic base.
    Type: Application
    Filed: October 6, 2008
    Publication date: April 2, 2009
    Applicant: AVECIA BIOTECHNOLOGY, INC.
    Inventors: Nanda Sinha, William Edward Zedalis, Gregory Keith Miranda
  • Patent number: 7501505
    Abstract: A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1?6-benzo[d]isothiazol-3-one, preferably in the presence of an organic base.
    Type: Grant
    Filed: July 1, 2002
    Date of Patent: March 10, 2009
    Assignee: Avecia Biotechnology, Inc.
    Inventors: Nanda Sinha, William Edward Zedalis, Gregory Keith Miranda
  • Publication number: 20090062355
    Abstract: An agent for suppressing the production of various cytokines (IL-8 and the like) and inflammatory mediators, an agent for suppressing the expression of COX-II and the like, or an inhibitor of various phosphorylation enzymes (ATF2 and the like), which contains a TLR signaling inhibitory substance, preferably a compound represented by the formula (I) or the formula (II) wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
    Type: Application
    Filed: April 19, 2007
    Publication date: March 5, 2009
    Inventors: Yuji Iizawa, Masayuki Ii, Tomohiro Kawamoto
  • Publication number: 20080242710
    Abstract: 3a,4,5,6-Tetrahydro-pyrrolol,2-b]-isothiazoles wherein the sulphur is in the form of a dioxide and their use for the treatment or prevention of disorders mediated by interactions of LFA-1 with its ligands involved in cell adhesion, migration and activation.
    Type: Application
    Filed: October 4, 2006
    Publication date: October 2, 2008
    Inventor: Karl Baumann
  • Publication number: 20080146544
    Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.
    Type: Application
    Filed: February 25, 2008
    Publication date: June 19, 2008
    Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
  • Patent number: 7358254
    Abstract: A method is provided for treating atherosclerosis and related diseases, employing an aP2 inhibitor or a combination of an aP2 inhibitor and another antiatherosclerotic agent, for example, an HMG CoA reductase inhibitor such as pravastatin.
    Type: Grant
    Filed: June 21, 2004
    Date of Patent: April 15, 2008
    Assignees: Bristol-Myers Squibb Company, President & Fellows of Harvard College
    Inventors: Jeffrey A. Robl, Rex A. Parker, Scott A. Biller, Haris Jamil, Bruce L. Jacobson, Krishna Kodukula, Gokhan Hotamisligil
  • Patent number: 7345062
    Abstract: Imido and amido substituted acylhydroxamidic acids which reduce the levels of TNF? and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propandylamino)propanoate.
    Type: Grant
    Filed: February 25, 2004
    Date of Patent: March 18, 2008
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W Muller, Shaei Y Huang
  • Patent number: 7179923
    Abstract: Compounds having two reactive functional groups are described that can be used to provide a connector group between a substrate and an amine-containing material. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonylaminocarbonyl group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a carbonylimino-containing connector group. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.
    Type: Grant
    Filed: November 12, 2004
    Date of Patent: February 20, 2007
    Assignee: 3M Innovative Properties Company
    Inventors: Karl E. Benson, Moses M. David, Cary A. Kipke, Brinda B. Lakshmi, Charles M. Leir, George G. I. Moore, Rahul R. Shah
  • Patent number: 6838415
    Abstract: The invention relates to novel substituted benzoylisoxazoles of the general formula (I), in which n represents the number 0, 1, 2 or 3, A represents a single bond or represents alkanediyl (alkylene), R1 represents hydrogen or represents in each case optionally substituted alkyl, alkenyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, halogen, or represents in each case optionally substituted alkyl, alkylcarbonyl, alkoxy, alkoxycarbonyl or alkylthio, alkylsulphinyl or alkylsulphonyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, and Z represents an optionally substituted 4-
    Type: Grant
    Filed: April 20, 2000
    Date of Patent: January 4, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Hans-Georg Schwarz, Heinz-Jürgen Wroblowsky, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
  • Publication number: 20040259924
    Abstract: The present invention relates to chromans, to processes for their preparation and to their use in medicaments, in particular as agents for treating disorders of the central nervous system.
    Type: Application
    Filed: August 18, 2004
    Publication date: December 23, 2004
    Inventors: Dietrich Scherling, Wolfgang Karl, Dietrich Seidel, Corinna Weinz, Rudolf Schohe-Loop, Frank Mauler
  • Publication number: 20040259873
    Abstract: The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4.
    Type: Application
    Filed: March 12, 2004
    Publication date: December 23, 2004
    Inventors: Hon-Wah Man, George W. Muller
  • Publication number: 20040254214
    Abstract: The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders. Examples inlcude, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.
    Type: Application
    Filed: March 12, 2004
    Publication date: December 16, 2004
    Inventors: Hon-Wah Man, George W. Muller, Weihong Zhang
  • Publication number: 20040204448
    Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.
    Type: Application
    Filed: December 29, 2003
    Publication date: October 14, 2004
    Applicant: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man, Weihong Zhang
  • Publication number: 20040127500
    Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented.
    Type: Application
    Filed: December 12, 2003
    Publication date: July 1, 2004
    Applicant: Bayer Pharmaceuticals Corporation
    Inventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
  • Publication number: 20040116616
    Abstract: Initiators for atom transfer radical polymerizations are described. The initiators have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.
    Type: Application
    Filed: December 11, 2002
    Publication date: June 17, 2004
    Applicant: 3M Innovative Properties Company
    Inventors: Kevin M. Lewandowski, Duane D. Fansler, Babu N. Gaddam, Steven M. Heilmann, Larry R. Krepski, Stephen B. Roscoe, Michael S. Wendland
  • Patent number: 6699899
    Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.
    Type: Grant
    Filed: December 21, 1999
    Date of Patent: March 2, 2004
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W Muller, Shaei Y Huang
  • Patent number: 6605255
    Abstract: The invention relates to a kit comprising a pharmaceutical composition containing repinotan or a physiologically acceptable salt of repinotan, and a means for the determination of the concentration of repinotan or its metabolites in body fluids, and also new pharmaceutical compositions containing repinotan or a physiologically acceptable salt of repinotan, and processes for their preparation.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: August 12, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Werner Kroll, Ferdinand Rombout, Horst Weber, Maria-Luisa Rodriguez, Bernd Sennhenn, Rudolf Schohe-Loop
  • Patent number: 6518281
    Abstract: Novel amides and imides are inhibitors of tumor necrosis factor&agr; and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: February 11, 2003
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire
  • Patent number: 6498004
    Abstract: This invention provides a photographic element comprising at least one silver halide emulsion layer in which the silver halide is sensitized with a compound of the formula (a): &Dgr;−(t)m−XY′  (a) XY′−(t)m−&Dgr;  (b) &Dgr;−(t)m−XY′−(t)m−&Dgr;  (c) wherein &Dgr; is protective group that is eliminated during development of the photographic element, t is a timing group, m is an integer from 0 to 3, and XY′ is a fragmentable electron donor moiety in which X is an electron donor group and Y′ is a leaving proton H or a leaving group Y, with the proviso that if Y′ is a proton, a base, &bgr;−, is present in the emulsion or is covalently linked directly or indirectly to X, and wherein: 1) X—Y′ has an oxidation potential between 0 and about 1.
    Type: Grant
    Filed: December 28, 2000
    Date of Patent: December 24, 2002
    Assignee: Eastman Kodak Company
    Inventors: Jerome R. Lenhard, Annabel A. Muenter, Stephen A. Godleski, Paul A. Zielinski, Deepak Shukla, Donald R. Diehl
  • Patent number: 6410485
    Abstract: The present application relates to saccharin-5-carbonyl derivatives of the formula I in which the substituents have the following meanings: L is C1-C6-alkyl, C1-C6-alkoxy; Z is C1-C6-alkyl, C3-C8-cycloalkyl, C3-C6-alkenyl, C3-C5-alkynyl, phenyl-C1-C6-alkyl or phenyl, where the phenyl rings are in each case optionally mono- or polysubstituted by C1-C6-alkyl, C1-C6-alkoxy or halogen; M is hydrogen, C1-C6-alkyl, C1-C6-alkoxy, halogen, cyano, nitro or halo-C1-C6-alkyl; R1, R2, R3, R4, R5, R6, R7, R8 are hydrogen, C1-C6-alkyl; and agriculturally utilizable salts of the compound I.
    Type: Grant
    Filed: September 5, 2001
    Date of Patent: June 25, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulf Misslitz, Ernst Baumann, Wolfgang von Deyn, Steffen Kudis, Klaus Langemann, Guido Mayer, Ulf Neidlein, Matthias Witschel, Roland Götz, Michael Rack, Peter Plath, Martina Otten, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 6410580
    Abstract: Compounds of formula (I) wherein W is —OH or —NHOH; X is an optionally substituted heterocycle, NR1SO2R2, heterocyclylalkythio, CONR2R3 or NR1COR2; Y, Z, R1-R3 and n are as defined in the application. Compounds (I) are inhibitors of matrix-degrading metalloproteinases and are use for the treatment of related conditions.
    Type: Grant
    Filed: August 2, 2000
    Date of Patent: June 25, 2002
    Assignee: Novartis AG
    Inventors: Paivi Jaana Kukkola, Leslie Ann Robinson, Junichi Sakaki, Motowo Nakajima
  • Patent number: 6319932
    Abstract: Novel oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: November 20, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Jennie B. Nerenberg, Mark G. Bock, Harold G. Selnick, Linda Payne
  • Patent number: 6288063
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 27, 1998
    Date of Patent: September 11, 2001
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, David Ross Brittelli, William Riley Schoen, Sookhee Nicole Ha
  • Patent number: 6083880
    Abstract: Saccharin-5-carbonylcyclohexane-1,3,5-trione derivatives of the formula I ##STR1## where: L is C.sub.1 -C.sub.3 -alkyl or C.sub.1 -C.sub.3 -alkoxy;Z is C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.5 -alkynyl, benzyl or phenyl, the phenyl rings in each case being unsubstituted or mono- or polysubstituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.3 -alkoxy or halogen;M is hydrogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, fluorine, chlorine, cyano, nitro or trifluoromethyl;R.sup.1, R.sup.2, R.sup.3, R.sup.4 are each C.sub.1 -C.sub.4 -alkyl;and agriculturally useful salts of compound I.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: July 4, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Helmut Walter, Peter Plath, Uwe Kardorff, Matthias Witschel, Regina Luise Hill, Wolfgang von Deyn, Stefan Engel, Martina Otten, Ulf Misslitz, Karl-Otto Westphalen
  • Patent number: 6075041
    Abstract: Cyclic amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 3-phenyl-3-(1-oxoisoindolin-2-yl)propionamide.
    Type: Grant
    Filed: September 22, 1998
    Date of Patent: June 13, 2000
    Assignee: Celgene Corporation
    Inventor: George W. Muller
  • Patent number: 6057350
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
    Type: Grant
    Filed: June 17, 1998
    Date of Patent: May 2, 2000
    Assignees: Merck & Co., Inc., Synaptic Pharmaceutical Corp.
    Inventors: Michael A. Patane, Mark G. Bock, Dhanapalan Nagarathnam, Bharat Lagu, Wai C. Wong
  • Patent number: 6011050
    Abstract: Phenethylsulfones substituted in the position .alpha. to the phenyl group with a 1-oxoisoindoline or 1,3-dioxoisoindoline group reduce the levels of TNF.alpha. in a mammal. Typical embodiments are 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-aminoisoindoline- 1,3-dione and 2-[1-(3-cyclopentyloxy-4-methoxyphenyl)-2-methylsulfonylethyl]isoindoline- 1,3-dione.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: January 4, 2000
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man
  • Patent number: 5981758
    Abstract: A process for preparing saccharincarbonyl halides of the formula 1 ##STR1## where: X is halogen,R.sup.1, R.sup.2 are each hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy, optionally C.sub.1 -C.sub.4 -alkyl-, fluorine- or C.sub.1 -C.sub.4 -alkoxy-substituted benzyl or phenyl,R.sup.3 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl or phenyl or benzyl which is optionally mono- or polysubstituted by C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -haloalkyl or C.sub.1 -C.sub.4 -alkoxy,by reaction of an isophthalylsulfonamide 2 with an inorganic acid halide to give the saccharincarbonyl halide 1 ##STR2## is described.
    Type: Grant
    Filed: March 25, 1999
    Date of Patent: November 9, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Plath, Wolfgang von Deyn, Michael Rack, Ulf Misslitz
  • Patent number: 5945540
    Abstract: Disclosed is a process that provides steps for synthesizing intermediates useful for appending a N heterocyclic compound to the 3-position of a 4-H-pyrazolo-?1,5-a!benzimidazole compound and further steps that together provide a combined process that yields the target compounds in good yields while using readily available reagents and mild conditions.
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: August 31, 1999
    Assignee: Eastman Kodak Company
    Inventor: Barbara B. Lussier
  • Patent number: 5942529
    Abstract: The benzisothiazolyl-substituted aminomethylchromans are prepared either by substituting the corresponding unsubstituted aminomethylchromans on the amine nitrogen or reacting the corresponding benzisothiazolylalkylamines with appropriate activated methylchromans or reacting the amine nitrogen of aminomethylchroman first with an appropriately substituted alkine and then hydrogenating. The benzisothiazolyl-substituted aminomethylchromans can be used as active compounds in medicaments, in particular in medicaments for the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: June 13, 1996
    Date of Patent: August 24, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe-Loop, Hans-Georg Heine, Peter-Rudolf Seidel, Wolfgang Kanhai, Joachim Schuhmacher, Arno Friedl, Ervin Horvath, Thomas Glaser, Reinhard Jork
  • Patent number: 5925637
    Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## wherein r is 0-2, T is selected from ##STR2## and R.sup.40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, comeal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibularjoint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture.
    Type: Grant
    Filed: May 15, 1997
    Date of Patent: July 20, 1999
    Assignee: Bayer Corporation
    Inventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
  • Patent number: 5874432
    Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO-- or --SO.sub.2 --;m and n are each independently 0 or 1;R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl;R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; andR.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.
    Type: Grant
    Filed: February 20, 1997
    Date of Patent: February 23, 1999
    Assignee: Sanofi
    Inventors: Richard Paul Dunlap, Neil Warren Boaz, Albert Joseph Mura, Dennis John Hlasta, Ranjit Chimanlal Desai, Chakrapani Subramanyam, Lee Hamilton Latimer, Eric Piatt Lodge
  • Patent number: 5863864
    Abstract: Saccharincarboxylic acids and -carboxylic acid esters of the formula I ##STR1## where the substituents have the following meanings: L and M are hydrogen, alkyl, alkoxy, alkylthio, chlorine, cyano, alkylsulfonyl, nitro or trifluoromethyl;Z is hydrogen, alkyl, cycloalkyl, alkyl, aryl or aralkyl;R is H or C.sub.1 -C.sub.6 -alkyl,are prepared by reacting corresponding bromo- or iodo-substituted saccharin derivatives of the formula II ##STR2## where L, M and Z have the abovementioned meanings, or if Z.noteq.H, compounds of the formula III ##STR3## in the presence of a palladium, nickel, cobalt or rhodium transition metal catalyst and of a base with carbon monoxide and water or a C.sub.1 -C.sub.6 -alcohol under elevated pressure.
    Type: Grant
    Filed: February 3, 1997
    Date of Patent: January 26, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Plath, Harald Rang, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
  • Patent number: 5856349
    Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: January 5, 1999
    Assignee: Sanofi
    Inventors: Richard Paul Dunlap, Dennis John Hlasta, Ranjit Chimanlal Desai, Lee Hamilton Latimer, Chakrapani Subramanyam, John Joseph Court, Malcolm Rice Bell, Virendra Kumar
  • Patent number: 5830908
    Abstract: The invention relates to the crystalline form of the hydrochloride of the compound (R)-(-)-2-{N-?4-(1,1-dioxido-3-oxo-2,3-dihydro-benzisothiazol-2-yl)-butyl! -aminomethyl}-chroman, which is present as a stable form at room temperature. The crystalline modification V of the hydrochloride is suitable in particular for the preparation of solid medicaments, in particular of medicaments for the treatment of neuronal degenerations.
    Type: Grant
    Filed: November 19, 1996
    Date of Patent: November 3, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alfons Grunenberg, Oliver Brehm, Michael Conrad, Dietrich Seidel
  • Patent number: 5783589
    Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl and aryloxy acetates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an aryl or aryloxyacetic acid in the presence of an acid-acceptor.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: July 21, 1998
    Assignee: Sanofi
    Inventors: Lee Hamilton Latimer, Richard Paul Dunlap
  • Patent number: 5773456
    Abstract: Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2;L--R.sup.1 is a leaving group, H--L--R.sup.1 is the conjugate acid thereof and, when L is N, H--L--R.sup.1 has a pK.sub.a value less than or equal to 6, when L is O, H--L--R.sup.1 has a pK.sub.a value less than or equal to to 8, and when L is SO.sub.n, H--L--R.sup.1 has a pK.sub.a value less than or equal to 5;R.sup.2 is primary or secondary alkyl of two to four carbon atoms, primary alkylamino of one to three carbon atoms, primary alkylmethylamino of two to four carbon atoms, diethylamino or primary alkoxy of one to three carbon atoms; andR.sup.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: June 30, 1998
    Assignee: Sanofi
    Inventors: Richard Paul Dunlap, Albert Joseph Mura, Dennis John Hlasta, Ranjit Chimanlal Desai, Lee Hamilton Latimer
  • Patent number: 5750550
    Abstract: 2-(Pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
    Type: Grant
    Filed: September 15, 1995
    Date of Patent: May 12, 1998
    Assignee: Sanofi
    Inventors: Michael A. Eissenstat, Gee-Hong Kuo, Ranjit C. Desai, Dennis J. Hlasta, John J. Court
  • Patent number: 5744425
    Abstract: Saccharin derivatives of the formula I ##STR1## where the substituents have the following meanings: L and M are hydrogen, alkyl, alkoxy, alkylthio, chlorine, cyano, methylsulfonyl, nitro or trifluoromethyl;Z is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, acyl, or benzyl or phenyl which are unsubstituted or substituted by halogen or alkyl;J is a 2-linked, unsubstituted or substituted cyclohexane-1,3-dione ring,are described.
    Type: Grant
    Filed: February 3, 1997
    Date of Patent: April 28, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Plath, Uwe Kardorff, Wolfgang von Deyn, Stefan Engel, Jurgen Kast, Harald Rang, Hartmann Konig, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
  • Patent number: 5723415
    Abstract: 5-Hydroxypyrazol-4-ylcarbonyl-substituted saccharin derivatives of the formula I ##STR1## where the substituents have the following meanings: L and M are hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, chlorine, cyano, methylsulfonyl, nitro or trifluoromethyl;Z is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.5 -alkynyl, C.sub.1 -C.sub.4 -acyl, benzyl or phenyl, the phenyl rings in each case being unsubstituted or substituted by halogen or C.sub.1 -C.sub.4 -alkyl;Q is a radical CO--J,J is a 4-linked 5-hydroxypyrazole ring of the formula II ##STR2## where R .sup.1 is C.sub.1 -C.sub.4 -alkyl andR .sup.2 is hydrogen or methyl,and agriculturally customary salts of the compounds I are described.
    Type: Grant
    Filed: February 3, 1997
    Date of Patent: March 3, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Plath, Wolfgang von Deyn, Stefan Engel, Uwe Kardorff, Hartmann Konig, Harald Rang, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
  • Patent number: 5716906
    Abstract: Saccharin derivatives of the formula I ##STR1## where the substituents have the following meanings: L and M are hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, chlorine, cyano, methylsulfonyl, nitro or trifluoromethyl;Z is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.5 -alkynyl, C.sub.1 -C.sub.4 -acyl, benzyl or phenyl, the phenyl rings in each case being unsubstituted or substituted by halogen or C.sub.1 -C.sub.4 -alkyl;Q is a radical T-J, whereT is a carbonyl radical CO or the radical --CHY,J is a 4-linked isoxazole ring of the formula II ##STR2## where R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl andR.sup.2 is C.sub.1 -C.sub.4 -alkyl, cyclopropyl, 1-methylcyclopropyl or 1-methylthiocyclopropyl;Y is an OH group, a hydroxyl group which may be acylated by C.sub.2 -C.sub.4 -acyl or a chlorine atom;and agriculturally customary salts of the compounds I are described.
    Type: Grant
    Filed: February 10, 1997
    Date of Patent: February 10, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Plath, Wolfgang von Deyn, Stefan Engel, Uwe Kardorff, Hartmann Konig, Harald Rang, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen