Chalcogen Bonded Directly To The Oxazine Ring Patents (Class 544/92)
-
Publication number: 20090156588Abstract: The present invention relates 3,4-dihydro-benzo[e][1,3]oxazin-2-ones which are substituted at the nitrogen atom by unsubstituted or substituted (C1-8)alkyl, (C3-8)cycloalkyl, (C3-8)cycloalkyl(C1-4)alkyl, (C6-18)aryl or (C6-18)aryl(C1-4)alkyl and their use as pharmaceuticals.Type: ApplicationFiled: April 13, 2006Publication date: June 18, 2009Inventors: Andreas Billich, Hubert Gstach, Philipp Lehr
-
Publication number: 20090137577Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: June 30, 2008Publication date: May 28, 2009Inventors: Allen J. Duplantier, Ivan Efremov, Lei Zhang, Noha S. Maklad, Theresa O'Sullivan
-
Publication number: 20090105236Abstract: The present invention relates to the use of the compounds of general formula 1 wherein the groups R1, R2 and R3 may have the meanings specified in the claims and in the description, for preparing a pharmaceutical composition for the treatment of respiratory complaints, as well as new compounds of formula 1, processes for preparing them, and pharmaceutical formulations containing them.Type: ApplicationFiled: December 18, 2008Publication date: April 23, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ingo KONETZKI, Thierry BOUYSSOU, Philipp LUSTENBERGER, Andreas SCHNAPP
-
Patent number: 7514429Abstract: The present invention relates to Benzoxazinone-derived compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals.Type: GrantFiled: January 24, 2006Date of Patent: April 7, 2009Assignee: ESTEVE Laboratorios Dr. Esteve S.A.Inventors: Antoni Torrens Jover, Jose Aurelio Castrillo Perez, Jordi Frigola Constansa, Josep Mas Prió, Alberto Dordal Zueras, Maria Angeles Fisas Escasany
-
Publication number: 20090085344Abstract: The present disclosure provides Benzoxazinone compounds represented by the formula: wherein each R1, R2, R3, and R4 is independently selected from hydrogen, alkyl of 1-12 carbon atoms, substituted alkyl, aryl of 6-12 carbon atoms, substituted aryl, halo, and alkoxy; and R5 is selected from alkyl of 1-12 carbon atoms, substituted alkyl, aryl of 6-12 carbon atoms, substituted aryl, halo, and alkoxy; wherein each of the substituted alkyl and the substituted aryl groups have a substituent selected from alkyl, aryl, halo, and alkoxy. The present disclosure provides a mark having a benzoxazinone compound, and a method for applying the mark onto an article. Also provided is a process for preparing benzoxazinone compounds.Type: ApplicationFiled: October 1, 2007Publication date: April 2, 2009Inventors: Thomas Potrawa, Joachim Schulz
-
Publication number: 20090075991Abstract: The present application describes deuterium-enriched efavirenz, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicant: Protia, LLCInventor: Anthony W. Czarnik
-
Publication number: 20090068719Abstract: This invention provides compounds, methods, immunoassays, and kits relating to active, metabolically sensitive (“met-sensitive”) moieties of anti-HIV therapeutics, such as HIV protease inhibitors (PI) and HIV non-nucleoside reverse transcriptase inhibitors (NNRTI).Type: ApplicationFiled: January 11, 2008Publication date: March 12, 2009Inventor: Johnny Valdez
-
Patent number: 7488822Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 are independent substituents or are fused to form spirocyclic rings; R3, RC, and R4 are as defined herein; and R5 is a substituted benzene ring or a substituted five or six membered heterocyclic ring having in its backbone 1, 2, or 3 heteroatoms including O, S, SO, SO2 or NR6; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.Type: GrantFiled: January 29, 2004Date of Patent: February 10, 2009Assignee: WyethInventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
-
Publication number: 20090030119Abstract: The invention relates to a method for preparing a benzoxazinone comprising reacting an isatoic anhydride with an acylating compound in the presence of an N-alkyl imidazole, to a method for preparing a photo-stabilised composition, comprising adding a benzoxazinone and to the use of a benzoxazinone as a light-absorber or as a stabiliser for a light-sensitive compound.Type: ApplicationFiled: January 5, 2007Publication date: January 29, 2009Applicant: TEMSA INTERNATIONAL INC.Inventor: Asim Kumar Sarkar
-
Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
-
Patent number: 7476699Abstract: The present invention provides compounds having the formula: in which R is hydrogen, hydroxy, halogen, C1-C20-alkyl, C4-C12cycloalkyl, C2-C20alkenyl, C2-C20alkynyl, C1-C20-alkoxy, C4-C12cycloalkoxy, C2-C20alkenoxy, C2-C20alkynoxy or C7-C13aralkyl; R1 and R2, independently, are hydrogen, C1-C20alkyl, C4-C12cycloalkyl, C7-C13 aralkyl, —C(?O)—R4 (in which R4 is C1-C20alkyl, C2-C20alkyl interrupted by 1 to 6 oxygen atoms, hetero-substituted C1-C20alkyl, C4-C12cycloalkyl, C2-C20alkenyl, C2-C20alkynyl, C1-C20-alkoxy, C4-C12cycloalkoxy, C2-C20alkenoxy, C2-C20alkynoxy, C6-C12 aryl, C6-C12 aryloxy or C7-C13 aralkyl), or —C(?O)—NH—R1 in which R1 has its previous significance; and R3 is hydrogen, halogen, hydroxy, C1-C20alkyl, C4-C12cycloalkyl, C2-C20alkenyl, C2-C20alkynyl, C1-C20-alkoxy, C4-C12cycloalkoxy, C2-C20alkenoxy, C2-C20alkynoxy, phenyl, C7-C13 aralkyl or —N(R1)(R2) in which R1 and R2 have their previous significance, or R1 and R2 together form a C4-C12 membered ring.Type: GrantFiled: August 10, 2007Date of Patent: January 13, 2009Assignee: Ciba Specialty Chemicals Corp.Inventors: Dieter Reinehr, Georges Metzger, Peter Michaelis, Helmut Luther
-
Patent number: 7442696Abstract: This invention relates to compounds that bind to mineralocorticoid receptors and/or modulate activity of mineralocorticoid receptors, and to methods for making and using such compounds. Some embodiments relate to compounds of Formula I: or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, wherein R1 —R10 are as defined herein.Type: GrantFiled: January 12, 2007Date of Patent: October 28, 2008Assignee: Ligand Pharmaceuticals, Inc.Inventors: Robert I. Higuchi, Lin Zhi, Mark E. Adams, Yan Liu, Donald S. Karanewsky
-
Patent number: 7423146Abstract: A process for making a compound of formula 1 or a salt thereof, wherein: R1 and R2 are each independently H, halogen, or C1-4-alkyl, or R1 and R2 together are C1-6-alkylene; and R3 is H, halogen, OH, C1-4-alkyl, or O—C1-4-alkyl, the process comprising: (a) reacting a compound of formula 6 wherein R4 is benzyl, diphenylmethyl, or trityl, each optionally substituted at, if available, an aryl group or an aliphatic carbon atom, with a compound of formula 7 or a salt thereof, to obtain a compound of formula 5, or a salt thereof (b) reducing the nitro group of the compound of formula 5 to an amine group and mesylating this amine group and cleaving the protecting group during the reduction step or after the mesylation step to obtain the compound of formula 1.Type: GrantFiled: October 25, 2006Date of Patent: September 9, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Marco Santagostino, Werner Rall, Rainer Soyka
-
Patent number: 7408060Abstract: This invention relates to nonsteroidal progesterone receptor modulators of general formula I, a process for their production, the use of progesterone receptor modulators for the production of pharmaceutical agents as well as pharmaceutical compositions that contain these compounds. The compounds according to the invention are suitable for therapy and prophylaxis of gynecological diseases, such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhea, as well as for the therapy and prophylaxis of hormone-dependent tumors and for use for female birth control as well as for hormone replacement therapy.Type: GrantFiled: June 23, 2006Date of Patent: August 5, 2008Assignee: Schering AGInventors: Norbert Schmees, Ulrich Bothe, Wolfgang Schwede, Carsten Moeller, Ulrike Fuhrmann, Anja Schmidt
-
Publication number: 20080182750Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: ApplicationFiled: April 18, 2006Publication date: July 31, 2008Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andre Jeanguenat, Anthony O'Sullivan, Michel Muehlebach, Stephan Trah, Roger Graham Hall
-
Publication number: 20080167299Abstract: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.Type: ApplicationFiled: March 7, 2008Publication date: July 10, 2008Applicant: WyethInventor: Bogdan Kazimierz Wilk
-
Publication number: 20080161290Abstract: Provided herein are benzoxazinone compounds of formula I and compositions containing the compounds. The compounds and compositions are useful in the methods of inhibiting the action of serine hydrolase, including neutrophil elastase. In certain embodiments, the compounds and compositions are useful in the prevention, amelioration or treatment of serine hydrolase-mediated diseases.Type: ApplicationFiled: September 20, 2007Publication date: July 3, 2008Inventors: Kevin Shreder, Yi Hu, Allister Fraser, Yasushi Kohno, Akihiko Kojima, Junichi Ishiyama
-
Publication number: 20080161301Abstract: The use of a compound comprising formula (I): or a salt, ester, amide or prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality, e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I) A is a 6-membered aromatic or heteroaromatic ring; and R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups.Type: ApplicationFiled: March 7, 2008Publication date: July 3, 2008Applicant: Alizyme Therapeutics LimitedInventors: Harold Francis Hodson, Robert Downham, Timothy John Mitchell, Beverley Jane Carr, Christopher Robert Dunk, Richard Michael John Palmer
-
Publication number: 20080132499Abstract: Compounds are provided which are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.Type: ApplicationFiled: September 17, 2007Publication date: June 5, 2008Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Carroll Anna Crew Scarborough, Shawn M. Bauer, Anjali Pandey
-
Patent number: 7375104Abstract: A compound of formula 1? wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1? are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1? together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2?, R2?, and R?? are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, orType: GrantFiled: November 15, 2006Date of Patent: May 20, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Thierry Bouyssou, Ingo Konetzki, Philipp Lustenberger, Juergen Mack, Andreas Schnapp, Dieter Wiedenmayer, Christoph Hoenke, Klaus Rudolf
-
Patent number: 7358246Abstract: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.Type: GrantFiled: April 7, 2005Date of Patent: April 15, 2008Assignee: WyethInventor: Bogdan Kazimierz Wilk
-
Patent number: 7339057Abstract: A method for preparing a fused oxazinone is disclosed in which (1) a carboxylic acid is contacted with a sulfonyl chloride in the presence of an optionally substituted pyridine compound, the nominal mole ratio of sulfonyl chloride to carboxylic acid being from about 0.75 to 1.5; (2) the mixture prepared in (1) is contacted with an ortho-amino aromatic carboxylic acid in the presence of an optionally substituted pyridine compound, the nominal mole ratio of the ortho-amino aromatic carboxylic acid to carboxylic acid charged in (1) being from about 0.8 to 1.2; and (3) additional sulfonyl chloride is added to the mixture prepared in (2), the nominal mole ratio of additional sulfonyl chloride added in (3) to carboxylic acid charged in (1) being at least about 0.5.Type: GrantFiled: July 29, 2003Date of Patent: March 4, 2008Assignee: E.I. du Pont de Nemours and CompanyInventor: Eric Deguyon Taylor
-
Patent number: 7332105Abstract: A stabilizer composition comprising (A) a compound of the formula (I) wherein R is (CH2—CH2—O—)n, —R2; —CH2—CH(OH)—CH2—O—R2; or —CH(R3)—CO—O—R4; n is 0 or 1; R2 is C1-C13alkyl or C2C20alkenyl or C6-C12aryl or CO—C1-C18alkyl; R3 is H or C1-C8 alkyl; R4 is C1-C12alkyl or C2-C12alkenyl or C5C6cycloalkyl; and (B) one or more compounds selected from benzotriazoles of the formula (IIa), 2-hydroxybenzophenones of the formula (IIb), oxalanilides of the formula (IIc), 2-hydroxyphenyltriazines of formula (IId), cinnamates of formula (IIe), and benzoates of formula (IIf) as defined in claim 1, is especially effective towards stabilizing organic materials against degradation induced by light, heat or oxidation.Type: GrantFiled: September 23, 2003Date of Patent: February 19, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Adalbert Braig, David George Leppard, Frédérique Wendeborn
-
Patent number: 7314932Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrite groups, are provided.Type: GrantFiled: April 7, 2005Date of Patent: January 1, 2008Assignee: WyethInventor: Bogdan Kazimierz Wilk
-
Patent number: 7314883Abstract: The present invention relates to methods of treating neurogenic vasodilation, neurogenic inflammaton, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors using pharmaceutical compositions comprising compounds of Formula (I)Type: GrantFiled: January 5, 2007Date of Patent: January 1, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Ling Chen, Prasad V. Chaturvedula, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, George N. Karageorge, Guanglin Luo, John E. Macor, Graham S. Poindexter, George O. Tora
-
Patent number: 7312211Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: August 26, 2004Date of Patent: December 25, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
-
Patent number: 7276601Abstract: A method for preparing a fused oxazinone is disclosed in which a carboxylic acid is contacted with a sulfonyl chloride and an isatoic anhydride in the presence of a tertiary amine, the nominal mole ratio of said sulfonyl chloride to said carboxylic acid being from about 1.0 to 1.5 and the nominal mole ratio of said isatoic anhydride to said carboxylic acid is from about 0.8 to 1.2.Type: GrantFiled: June 10, 2004Date of Patent: October 2, 2007Assignee: E.I. du Pont de Nemours and CompanyInventor: Eric DeGuyon Taylor
-
Publication number: 20070213526Abstract: Processes are provided for purifying a compound of the structure: wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.Type: ApplicationFiled: March 5, 2007Publication date: September 13, 2007Applicant: WyethInventors: Mahmut Levent, Panolil Raveendranath, Bogdan Wilk, Donald Carl Boop, Marinus Cornelis Hofman
-
Patent number: 7247625Abstract: Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions.Type: GrantFiled: September 21, 2004Date of Patent: July 24, 2007Assignee: WyethInventors: Puwen Zhang, Jeffrey Kern
-
Patent number: 7220862Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: December 5, 2003Date of Patent: May 22, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Ling Chen, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, George N. Karageorge, Guanglin Luo, John E. Macor, Graham Poindexter, George Tora
-
Patent number: 7205402Abstract: The present invention provides novel methods for the synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (III) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.Type: GrantFiled: September 1, 2005Date of Patent: April 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Purushotham Vemishetti, Scott T. Chadwick, Carrie A. Costello, Sridhar Desikan, Emily A. Reiff
-
Patent number: 7205296Abstract: Substituted benzoxazin-4(3H)-ones are provided which are useful for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.Type: GrantFiled: September 26, 2005Date of Patent: April 17, 2007Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Meenakshi S. Venkatraman, Xiaoming Zhang, Anjali Pandey
-
Patent number: 7192471Abstract: Fluorescent pigment compounds comprising aryl-ureido benzoxazinone compounds of the general formula (I): wherein R1 is an substituted or unsubstituted aryl group, R2 and R3 are each independently selected from an H atom, an alkyl group, an alkoxy group, an alkylcarboxy group and a halogen atom, X is a carbon or sulfur atom and n is an integer of 1 or more. Many of the compounds of this class produce a yellow, generally deep yellow, emission at wavelengths of about 560 to about 585 nm when excited by an appropriate UV source. These compounds produce fluorescence making them useful as fluorescent pigments, those compounds providing emission wavelengths within the range of from about 560 to about 585 or higher when excited by a UV source are particularly useful. Those compounds having this emission spectra for the compounds makes these compounds particularly useful as pigments in security applications, particularly as pigments for use in security inks and fibers.Type: GrantFiled: September 24, 2004Date of Patent: March 20, 2007Assignee: Honeywell International Inc.Inventors: Thomas Potrawa, Joachim Schulz
-
Patent number: 7189713Abstract: The present invention relates to piperidine derivatives of formula (I): R represents halogen or C1-4 alkyl R1 represents C1-4 alkyl; R2 or R3 independently represent hydrogen or C1-4 alkyl; R4 represents trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy or halogen; R5 represents hydrogen, C1-4 alkyl or C3-7 cycloalkyl; R6 is hydrogen and R7 is a radical of formula (W): ?or R6 is a radical of formula (W) and R7 is hydrogen; X represents CH2, NR5 or O; Y represents Nitrogen and Z is CH or Y represents CH and Z is Nitrogen; A represents C(O) or S(O)q, provided that when Y is nitrogen and Z is CH, A is not S(O)q; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p and q are independently an integer from 1 to 2; and pharmaceutically acceptable salts and solvates thereof. The process for their preparation and their use in the treatment of a condition mediated by tachykinins.Type: GrantFiled: February 10, 2003Date of Patent: March 13, 2007Assignee: Glaxo Group LimitedInventors: Giuseppe Alvaro, Romano Di Fabio, Maria Elvira Tranquillini, Simone Spada
-
Patent number: 7173128Abstract: The present invention relates to novel ultraviolet light absorbers of the benzoxazinone, oxanilide, benzylidene malonate, quinazoline and benzotriazole classes. The invention also relates to polymer and photographic compositions stabilized against the deleterious effects of light induced degradation which comprise the novel ultraviolet light absorbers.Type: GrantFiled: August 5, 2002Date of Patent: February 6, 2007Assignee: Ciba Specialty Chemicals CorporationInventors: Ramanathan Ravichandran, Stephen Daniel Pastor, Deborah Judd, Joseph Edmund Babiarz, Andrew Brian Naughton, Mervin Gale Wood, Anthony David Debellis, Rong Xiong, Robert Edward Detlefsen, Joseph Suhadolnik
-
Patent number: 7169776Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.Type: GrantFiled: January 19, 2005Date of Patent: January 30, 2007Assignee: Emisphere Technologies, Inc.Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
-
Patent number: 7166592Abstract: Compounds of Formula 1 are useful in the treatment of inflammation.Type: GrantFiled: June 24, 2004Date of Patent: January 23, 2007Assignee: Schering AktiengesellschaftInventors: Stefan Jaroch, Manfred Lehmann, Norbert Schmees, Bernd Buchmann, Harmur Rehwinkel, Peter Droescher, Werner Skuballa, Konrad Krolikiewicz, Hartwig Hennekes, Heike Schaecke, Arndr Schottelius
-
Patent number: 7160882Abstract: The present invention relates to compounds of formula 1 wherein the groups X, Ra, Rb, R1, R1?, R2, R2?, R2?, R2??, V and n may have the meanings given in the claims and in the specification, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.Type: GrantFiled: January 5, 2005Date of Patent: January 9, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Thierry Bouyssou, Ingo Konetzki, Philipp Lustenberger, Juergen Mack, Andreas Schnapp, Dieter Wiedenmayer, Christoph Hoenke, Klaus Rudolf
-
Patent number: 7115736Abstract: A novel process for preparing imidazopyran derivatives of the formula: wherein R1 is halogen atom, hydrogen atom, C1 to C3 alkyl group, aryl group, or aryl group substituted by C1 to C3 alkyl group, by using dinitroimidazole and 2,3-epoxy-1-propanol as starting materials and being followed by five steps.Type: GrantFiled: September 16, 2005Date of Patent: October 3, 2006Assignee: Daiso Co., Ltd.Inventors: Junzo Otera, Akihiro Orita
-
Patent number: 7081457Abstract: Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1 and R2 are selected from the group of H, optionally substituted C1 to C6 alkyl, alkenyl, alkynyl, or alkynyl groups C3 to C8 cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or CORA or NRBCORA; or R1 and R2 are fused to form an optionally substituted ring structure as defined herein; RA and RB are as defined herein; R3 is H, OH, NH2, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; RC is as defined herein; Q1 is S, NR7, or CR8R9; R5 is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring.Type: GrantFiled: May 6, 2002Date of Patent: July 25, 2006Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley, Jay E. Wrobel, Mark A. Collins
-
Patent number: 7071177Abstract: This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: April 26, 2001Date of Patent: July 4, 2006Assignee: Syntex (U.S.A.) LLCInventors: Nancy Elisabeth Krauss, Taraneh Mirzadegan, David Bernard Smith, Keith Adrian Walker
-
Patent number: 7056915Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases.Type: GrantFiled: April 24, 2003Date of Patent: June 6, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Michel Jose Emmanuel, Eugene R. Hickey, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
-
Patent number: 7056914Abstract: The present invention relates to Benzoxazinone-derived compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals.Type: GrantFiled: April 4, 2003Date of Patent: June 6, 2006Assignee: ESTEVE Laboratorios Dr. Esteve S.A.Inventors: Antoni Torrens Jover, Jose Aurelio Castrillo Perez, Jordi Frigola Constansa, Josep Mas Prió, Alberto Dordal Zueras, Maria Angeles Fisas Escasany
-
Patent number: 7041665Abstract: The present invention relates to new compounds of general formula (I), as well as to their physiologically acceptable salts, the procedures for their preparation, the intermediate compounds for obtaining them, the application of the compounds of general formula (I) as medicaments in the prevention and treatment of disorders of the Central nervous System and to the pharmaceutical compositions containing them.Type: GrantFiled: April 8, 2003Date of Patent: May 9, 2006Assignee: Laboratories del Dr. Esteve, S.A.Inventors: Antonio Torrens-Jover, Jose Aurelio Castrillo-Perez, Jordi Frigola-Constansa
-
Patent number: 6982261Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1–5; p=1–4; q=1–4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 15, 2003Date of Patent: January 3, 2006Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
-
Patent number: 6967251Abstract: Novel fluorescent derivitization reagents are described that are suitable for coupling to biomolecules that contain aldehyde or ketone functional groups. In one embodiment is provided reagents that have the following formula: wherein Q is carbonyl, thiocarbonyl, or sulfonyl, and R5 is -L-Z; L is arylene, or a C1-6 perfluoroalkylene, or a single covalent bond; Z is a carbonyl hydrazide, hydrazide, sulfonyl hydrazide, or a thiocarbonyl hydrazide; R11-R14 are independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 perfluoroalkyl, C1-6 alklyamino, di(C2-12alkyl)amino, amino, carboxy, cyano, halogen, hydroxy, nitro, phenyl, or sulfo; and R21-R24 are independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 perfluoroalkyl, C1-6 alklyamino, di(C2-12-alkyl)amino, amino, carboxy, cyano, halogen, hydroxy, nitro, phenyl, sulfo, or -L-Z. The method of treating a sample with the derivativization reagents is described.Type: GrantFiled: October 2, 2001Date of Patent: November 22, 2005Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Thomas H. Steinberg, Wayne F. Patton, Zhenjun Diwu
-
Patent number: 6956034Abstract: Oxazin(ethi)one compounds of the formula I: in which the variables Z, R1, R2, R3 and n are as defined in claim 1 and A is a 5- or 6-membered carbocycle or a 5- or 6-membered heterocycle having 1, 2 or 3 heteroatoms selected from the group consisting of N, O and S, each of which cycles is attached via two carbon atoms to the oxazin(ethi)one ring, and the agriculturally useful salts of the oxazin(ethi)one compounds I are described. Moreover, the invention describes the use of compounds I and their salts for controlling phytopathogenic fungi, compositions which comprise the compounds I and/or their salts in a fungicidally effective amount and a method for controlling phytopathogenic fungi which comprises treating the fungi or the materials, plants, seeds or the soil threatened by fungal attack with a fungicidally effective amount of at least one compound of the formula I as claimed in claim 1 and/or a salt of I.Type: GrantFiled: May 17, 2002Date of Patent: October 18, 2005Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Andreas Gypser, Ingo Rose, Thomas Grote, Peter Schäfer, Frank Schieweck, Eberhard Ammermann, John-Bryan Speakman, Siegfried Strathmann, Gisela Lorenz
-
Patent number: 6939964Abstract: The instant invention describes a method for crystallizing (?)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one from a solvent and anti-solvent solvent system and producing the crystalline product. The desired final crystal form, Form I, can be produced when using methanol or ethanol. Form II is isolated from 2-propanol and can be converted to the desired crystal form at low drying temperatures, such as between about a temperature of 40° C. and 50° C.Type: GrantFiled: June 24, 2004Date of Patent: September 6, 2005Assignee: Merck & Co., Inc.Inventors: Louis S. Crocker, Joseph L. Kukura, II, Andrew S. Thompson, Christine Stelmach, Steven D. Young
-
Patent number: 6936602Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.Type: GrantFiled: June 15, 2000Date of Patent: August 30, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
-
Patent number: 6936606Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: September 27, 2002Date of Patent: August 30, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel