At Least Three Chalcogens Bonded Directly To The Thiazole Ring Patents (Class 548/210)
-
Publication number: 20150119428Abstract: 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: ApplicationFiled: March 29, 2013Publication date: April 30, 2015Inventors: Joanne Holland, Christopher Frampton
-
Publication number: 20150031685Abstract: 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: ApplicationFiled: March 5, 2013Publication date: January 29, 2015Applicant: Dr. Reeddy's Laboratories Ltd.Inventors: Pradip Kumar Sasmal, Chintakunta Vamseekrishna, Vijay Potluri, Ashok Tehim, Yonghua Gai, Hang Zhang
-
Publication number: 20130252953Abstract: 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: ApplicationFiled: November 29, 2011Publication date: September 26, 2013Inventors: Zee-Fen Chang, Jim-Min Fang, Chun-Mei Hu, Ming-Tyng Yeh
-
Patent number: 8153658Abstract: 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: GrantFiled: November 14, 2007Date of Patent: April 10, 2012Assignee: Astellas Pharma, Inc.Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
-
Patent number: 8093397Abstract: 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: GrantFiled: October 6, 2008Date of Patent: January 10, 2012Assignee: Avecia Biotechnology, Inc.Inventors: Nanda Sinha, William Edward Zedalis, Gregory Keith Miranda
-
Publication number: 20110039874Abstract: 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: ApplicationFiled: April 16, 2010Publication date: February 17, 2011Applicant: Northeastern UniversityInventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
-
Publication number: 20100173377Abstract: 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: ApplicationFiled: January 21, 2010Publication date: July 8, 2010Inventors: Karl E. Benson, Moses M. David, Cary A. Kipke, Brinda B. Lakshmi, Charles M. Leir, George G. Moore, Rahul Shah
-
Publication number: 20090318704Abstract: 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: ApplicationFiled: August 3, 2007Publication date: December 24, 2009Inventor: John F. Reichwein
-
Patent number: 7635772Abstract: 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: GrantFiled: December 16, 2003Date of Patent: December 22, 2009Assignee: Avecia Biotechnology Inc.Inventor: Paul McCormac
-
Publication number: 20090085006Abstract: 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: ApplicationFiled: October 6, 2008Publication date: April 2, 2009Applicant: AVECIA BIOTECHNOLOGY, INC.Inventors: Nanda Sinha, William Edward Zedalis, Gregory Keith Miranda
-
Patent number: 7501505Abstract: 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: GrantFiled: July 1, 2002Date of Patent: March 10, 2009Assignee: Avecia Biotechnology, Inc.Inventors: Nanda Sinha, William Edward Zedalis, Gregory Keith Miranda
-
Publication number: 20090062355Abstract: 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: ApplicationFiled: April 19, 2007Publication date: March 5, 2009Inventors: Yuji Iizawa, Masayuki Ii, Tomohiro Kawamoto
-
Publication number: 20080242710Abstract: 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: ApplicationFiled: October 4, 2006Publication date: October 2, 2008Inventor: Karl Baumann
-
Publication number: 20080146544Abstract: 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: ApplicationFiled: February 25, 2008Publication date: June 19, 2008Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
-
Patent number: 7358254Abstract: 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: GrantFiled: June 21, 2004Date of Patent: April 15, 2008Assignees: Bristol-Myers Squibb Company, President & Fellows of Harvard CollegeInventors: Jeffrey A. Robl, Rex A. Parker, Scott A. Biller, Haris Jamil, Bruce L. Jacobson, Krishna Kodukula, Gokhan Hotamisligil
-
Patent number: 7345062Abstract: 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: GrantFiled: February 25, 2004Date of Patent: March 18, 2008Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
-
Patent number: 7179923Abstract: 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: GrantFiled: November 12, 2004Date of Patent: February 20, 2007Assignee: 3M Innovative Properties CompanyInventors: Karl E. Benson, Moses M. David, Cary A. Kipke, Brinda B. Lakshmi, Charles M. Leir, George G. I. Moore, Rahul R. Shah
-
Patent number: 6838415Abstract: 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: GrantFiled: April 20, 2000Date of Patent: January 4, 2005Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Hans-Georg Schwarz, Heinz-Jürgen Wroblowsky, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
-
Publication number: 20040259924Abstract: 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: ApplicationFiled: August 18, 2004Publication date: December 23, 2004Inventors: Dietrich Scherling, Wolfgang Karl, Dietrich Seidel, Corinna Weinz, Rudolf Schohe-Loop, Frank Mauler
-
Publication number: 20040259873Abstract: 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: ApplicationFiled: March 12, 2004Publication date: December 23, 2004Inventors: Hon-Wah Man, George W. Muller
-
Publication number: 20040254214Abstract: 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: ApplicationFiled: March 12, 2004Publication date: December 16, 2004Inventors: Hon-Wah Man, George W. Muller, Weihong Zhang
-
Publication number: 20040204448Abstract: 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: ApplicationFiled: December 29, 2003Publication date: October 14, 2004Applicant: Celgene CorporationInventors: George W. Muller, Hon-Wah Man, Weihong Zhang
-
Publication number: 20040127500Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented.Type: ApplicationFiled: December 12, 2003Publication date: July 1, 2004Applicant: Bayer Pharmaceuticals CorporationInventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
-
Publication number: 20040116616Abstract: Initiators for atom transfer radical polymerizations are described. The initiators have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.Type: ApplicationFiled: December 11, 2002Publication date: June 17, 2004Applicant: 3M Innovative Properties CompanyInventors: Kevin M. Lewandowski, Duane D. Fansler, Babu N. Gaddam, Steven M. Heilmann, Larry R. Krepski, Stephen B. Roscoe, Michael S. Wendland
-
Patent number: 6699899Abstract: 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: GrantFiled: December 21, 1999Date of Patent: March 2, 2004Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
-
Patent number: 6605255Abstract: 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: GrantFiled: November 16, 2001Date of Patent: August 12, 2003Assignee: Bayer AktiengesellschaftInventors: Werner Kroll, Ferdinand Rombout, Horst Weber, Maria-Luisa Rodriguez, Bernd Sennhenn, Rudolf Schohe-Loop
-
Patent number: 6518281Abstract: 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: GrantFiled: July 20, 2001Date of Patent: February 11, 2003Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
-
Patent number: 6498004Abstract: 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: GrantFiled: December 28, 2000Date of Patent: December 24, 2002Assignee: Eastman Kodak CompanyInventors: Jerome R. Lenhard, Annabel A. Muenter, Stephen A. Godleski, Paul A. Zielinski, Deepak Shukla, Donald R. Diehl
-
Patent number: 6410485Abstract: 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: GrantFiled: September 5, 2001Date of Patent: June 25, 2002Assignee: BASF AktiengesellschaftInventors: 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: 6410580Abstract: 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: GrantFiled: August 2, 2000Date of Patent: June 25, 2002Assignee: Novartis AGInventors: Paivi Jaana Kukkola, Leslie Ann Robinson, Junichi Sakaki, Motowo Nakajima
-
Patent number: 6319932Abstract: 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: GrantFiled: November 10, 1999Date of Patent: November 20, 2001Assignee: Merck & Co., Inc.Inventors: Jennie B. Nerenberg, Mark G. Bock, Harold G. Selnick, Linda Payne
-
Patent number: 6288063Abstract: 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: GrantFiled: May 27, 1998Date of Patent: September 11, 2001Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, David Ross Brittelli, William Riley Schoen, Sookhee Nicole Ha
-
Patent number: 6083880Abstract: 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: GrantFiled: September 1, 1999Date of Patent: July 4, 2000Assignee: BASF AktiengesellschaftInventors: 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: 6075041Abstract: 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: GrantFiled: September 22, 1998Date of Patent: June 13, 2000Assignee: Celgene CorporationInventor: George W. Muller
-
Patent number: 6057350Abstract: 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: GrantFiled: June 17, 1998Date of Patent: May 2, 2000Assignees: Merck & Co., Inc., Synaptic Pharmaceutical Corp.Inventors: Michael A. Patane, Mark G. Bock, Dhanapalan Nagarathnam, Bharat Lagu, Wai C. Wong
-
Patent number: 6011050Abstract: 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: GrantFiled: June 29, 1999Date of Patent: January 4, 2000Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
-
Patent number: 5981758Abstract: 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: GrantFiled: March 25, 1999Date of Patent: November 9, 1999Assignee: BASF AktiengesellschaftInventors: Peter Plath, Wolfgang von Deyn, Michael Rack, Ulf Misslitz
-
Patent number: 5945540Abstract: 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: GrantFiled: August 14, 1998Date of Patent: August 31, 1999Assignee: Eastman Kodak CompanyInventor: Barbara B. Lussier
-
Patent number: 5942529Abstract: 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: GrantFiled: June 13, 1996Date of Patent: August 24, 1999Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe-Loop, Hans-Georg Heine, Peter-Rudolf Seidel, Wolfgang Kanhai, Joachim Schuhmacher, Arno Friedl, Ervin Horvath, Thomas Glaser, Reinhard Jork
-
Patent number: 5925637Abstract: 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: GrantFiled: May 15, 1997Date of Patent: July 20, 1999Assignee: Bayer CorporationInventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
-
Patent number: 5874432Abstract: 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: GrantFiled: February 20, 1997Date of Patent: February 23, 1999Assignee: SanofiInventors: 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: 5863864Abstract: 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: GrantFiled: February 3, 1997Date of Patent: January 26, 1999Assignee: BASF AktiengesellschaftInventors: Peter Plath, Harald Rang, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
-
Patent number: 5856349Abstract: 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: GrantFiled: June 6, 1997Date of Patent: January 5, 1999Assignee: SanofiInventors: Richard Paul Dunlap, Dennis John Hlasta, Ranjit Chimanlal Desai, Lee Hamilton Latimer, Chakrapani Subramanyam, John Joseph Court, Malcolm Rice Bell, Virendra Kumar
-
Patent number: 5830908Abstract: 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: GrantFiled: November 19, 1996Date of Patent: November 3, 1998Assignee: Bayer AktiengesellschaftInventors: Alfons Grunenberg, Oliver Brehm, Michael Conrad, Dietrich Seidel
-
Patent number: 5783589Abstract: 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: GrantFiled: May 24, 1995Date of Patent: July 21, 1998Assignee: SanofiInventors: Lee Hamilton Latimer, Richard Paul Dunlap
-
Patent number: 5773456Abstract: 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: GrantFiled: September 25, 1996Date of Patent: June 30, 1998Assignee: SanofiInventors: Richard Paul Dunlap, Albert Joseph Mura, Dennis John Hlasta, Ranjit Chimanlal Desai, Lee Hamilton Latimer
-
Patent number: 5750550Abstract: 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: GrantFiled: September 15, 1995Date of Patent: May 12, 1998Assignee: SanofiInventors: Michael A. Eissenstat, Gee-Hong Kuo, Ranjit C. Desai, Dennis J. Hlasta, John J. Court
-
Patent number: 5744425Abstract: 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: GrantFiled: February 3, 1997Date of Patent: April 28, 1998Assignee: BASF AktiengesellschaftInventors: Peter Plath, Uwe Kardorff, Wolfgang von Deyn, Stefan Engel, Jurgen Kast, Harald Rang, Hartmann Konig, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
-
Patent number: 5723415Abstract: 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: GrantFiled: February 3, 1997Date of Patent: March 3, 1998Assignee: BASF AktiengesellschaftInventors: Peter Plath, Wolfgang von Deyn, Stefan Engel, Uwe Kardorff, Hartmann Konig, Harald Rang, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
-
Patent number: 5716906Abstract: 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: GrantFiled: February 10, 1997Date of Patent: February 10, 1998Assignee: BASF AktiengesellschaftInventors: Peter Plath, Wolfgang von Deyn, Stefan Engel, Uwe Kardorff, Hartmann Konig, Harald Rang, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen