Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Nitrogen Patents (Class 548/267.6)
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Publication number: 20100099682Abstract: The invention provides compounds of formula (I) wherein R1 represents hydrogen or alkyl; R2 represents an unsubstituted or substituted heterocycle or R2 represents an unsubstituted or substituted aryl; R3 represents alkyl or halogen; X represents a single bond or an alkandiyl-group, optionally interrupted by one or more oxygen atoms or carbonyl groups or carbonyloxy groups in free base or acid addition salt form, processes for their preparation and their use as pharmaceuticals.Type: ApplicationFiled: September 17, 2009Publication date: April 22, 2010Inventors: Ralf GLATTHAR, Thomas J. Troxler, Thomas Zoller, Joachim Nozulak
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Publication number: 20100081826Abstract: A compound of Formula (I):Type: ApplicationFiled: November 24, 2009Publication date: April 1, 2010Applicant: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
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Publication number: 20100034813Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:Type: ApplicationFiled: November 8, 2007Publication date: February 11, 2010Inventors: Yi Xia, Kris G. Mendenhall, Paul A. Barsanti, Annette O. Walter, David Duhl, Paul A. Renhowe
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Patent number: 7511061Abstract: A prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(?O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; =Z1-Z2=Z3- represents a radical of formula ?N—N?CH— (a-1), ?N—CH?N— (a-2), ?CH—N?N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(?O), C(?S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hyType: GrantFiled: June 2, 2005Date of Patent: March 31, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Ashis Kumar Saha, David William End, Bart Lieven Daniel De Corte, Henry Joseph Breslin, Li Liu
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Publication number: 20090042854Abstract: The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: ApplicationFiled: January 19, 2007Publication date: February 12, 2009Inventors: Jianming Bao, Robert J. DeVita, Huagang Lu, Sander G. Mills, Gregori J. Morriello
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Publication number: 20090023228Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5.7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: April 23, 2008Publication date: January 22, 2009Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20080214622Abstract: The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).Type: ApplicationFiled: March 8, 2006Publication date: September 4, 2008Inventors: Alan Daniel Brown, David Ellis, Christophen Ronald Smith
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Publication number: 20080096892Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellu-lar activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Even more specifically, the invention provides compounds for modulating c-Kit kinase activity and methods of treating diseases mediated by c-Kit activity utilizing the compounds and pharmaceutical compositions thereof.Type: ApplicationFiled: August 27, 2004Publication date: April 24, 2008Applicant: Exelixis, Inc.Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew Tsuhako, John M. Nuss, Wei Xu, William Bajjalieh
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Patent number: 7361769Abstract: The present invention discloses compounds of formula I wherein m, n, p, R1, R2 and X, are herein defined, the compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: July 14, 2005Date of Patent: April 22, 2008Assignee: Schering CorporationInventors: Jing Su, Brian A. McKittrick, Haiqun Tang, Thavalakulamgara K. Sasikumar, Li Qiang
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Patent number: 7179825Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aType: GrantFiled: March 16, 2005Date of Patent: February 20, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Dominique Mabire, Christophe Denis Adelinet, Imré Christian Csoka, Marc Gaston Venet
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Patent number: 7049324Abstract: a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(?O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ?Z1—Z2?Z3— represents a radical of formula ?N—N?CH— (a-1), ?N—CH?N— (a-2), ?CH—N?N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(?O), C(?S), or a direct bond, R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyType: GrantFiled: November 15, 2000Date of Patent: May 23, 2006Inventors: Ashis Kumar Saha, David William End, Bart Lieven Daniel De Corte, Henry Joseph Breslin, Li Liu
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Patent number: 6939967Abstract: Process for production of non-proteinogenic L-amino acids by direct fermentation of a microorganism strain known per se having a deregulated cysteine metabolism in a manner known per se, which comprises adding, during the fermentation, a nucleophilic compound to the fermentation batch in a manner such that this leads to the production of non-proteinogenic L-amino acids by the microorganism strain.Type: GrantFiled: April 28, 2004Date of Patent: September 6, 2005Assignee: Consortium für elektrochemische Industrie GmbHInventor: Thomas Maier
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Patent number: 6849648Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.Type: GrantFiled: October 4, 2002Date of Patent: February 1, 2005Assignee: Warner-Lambert CompanyInventors: Amy Mae Bunker, William Glen Harter, James Lester Hicks, Patrick Michael O'Brien, Ly Pham, Joseph Armand Picard, William Howard Roark
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Patent number: 6803380Abstract: 5-aryl-1H-triazole compounds of the formula are potent and selective COX-2 inhibitors. The invention further relates to pharmaceutical compositions containing these compounds.Type: GrantFiled: May 17, 2002Date of Patent: October 12, 2004Assignee: Laboratoire TheramexInventors: Jean-Claude Pascal, Denis Carniato
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Patent number: 6759538Abstract: The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.Type: GrantFiled: November 1, 2002Date of Patent: July 6, 2004Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, Henry Lu, Sarkiz D. Issankani, Thomas Sun
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Patent number: 6723742Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.Type: GrantFiled: May 29, 2003Date of Patent: April 20, 2004Assignee: Novartis AG.Inventors: René Lattmann, Pierre Acklin
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Patent number: 6624309Abstract: Benzoic acid derivatives of the formula where X is oxygen, sulfur, —NH, —NR1, —N—CN, —N—OR1 or —N—NO2; Y is a single bond, —C═C—, or —NH; R1 is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocyclo, or (heterocyclo)alkyl; and R2 is aryl or heterocyclo. The compounds of formula I are useful in the treatment of arrhythmia.Type: GrantFiled: September 25, 2002Date of Patent: September 23, 2003Assignee: Bristol-Myers Squibb CompanyInventors: John Lloyd, George C. Rovnyak, Philip D. Stein, Saleem Ahmad, Karnail S. Atwal, Thomas J. Caulfield, Michael A. Poss
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Publication number: 20030130323Abstract: Polysubstituted indan-1-ol compounds of formula I, its physiologically acceptable salts and physiologically functional derivatives are disclosed 1Type: ApplicationFiled: August 29, 2002Publication date: July 10, 2003Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Patent number: 6566383Abstract: Sulphonyltriazoles of the formula wherein Hal, R1, R2 are as defined in the specification are provided along with a process for preparing these compounds and a process using these compounds to control the growth of microorganisms.Type: GrantFiled: March 5, 2002Date of Patent: May 20, 2003Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Stefan Hillebrand, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Patent number: 6518292Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably, and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.Type: GrantFiled: February 18, 2000Date of Patent: February 11, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, James J. Li, Jun Li, Stephen G. Swartz
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Patent number: 6465504Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.Type: GrantFiled: October 30, 2000Date of Patent: October 15, 2002Assignee: Novartis AGInventors: René Lattmann, Pierre Acklin
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Patent number: 6436980Abstract: Compounds are described which have efflux pump inhibitor activity. Also described are methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.Type: GrantFiled: November 28, 2000Date of Patent: August 20, 2002Assignee: Essential Therapeutics, Inc.Inventors: Roger Leger, Ving J. Lee, Miles She
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Publication number: 20020016471Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: March 16, 2001Publication date: February 7, 2002Inventors: Francesco Salituro, Guy Bemis, John Cochran
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Patent number: 6319939Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkType: GrantFiled: June 1, 2000Date of Patent: November 20, 2001Assignee: Janssen Pharmaceutica N.V.Inventors: Dominique Mabire, Christophe Denis Adelinet, Imré Christian Csoka, Marc Gaston Venet
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Patent number: 6306880Abstract: A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted; Ar2 represents a phenyl group which may be substituted; R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represnet a hydrogen atom or an unsubstituted or halo substituted alkyl; n represnets 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic, not including 1,3-dioxan-5-yl. The compound of the present invention exhibits an excellent antifungal activity.Type: GrantFiled: February 1, 1999Date of Patent: October 23, 2001Assignee: Sankyo Company, LimitedInventors: Sadao Oida, Teruo Tanaka, Yawara Tajima, Toshiyuki Konosu, Atsushi Somada, Takeo Miyaoka, Hiroshi Yasuda
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Patent number: 6265584Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.Type: GrantFiled: May 20, 1999Date of Patent: July 24, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
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Patent number: 6262099Abstract: 3-(Substituted phenyl)-5-(substituted cyclopropyl)-1,2,4-triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.Type: GrantFiled: October 22, 1999Date of Patent: July 17, 2001Assignee: Dow AgroSciences LLCInventors: Francis E. Tisdell, Joe R. Schoonover, Jr., James T. Pechacek, Perry V. Ripa, Leonard P. Dintenfass, Timothy P. Martin, Donald H. DeVries, Mary L. Ash, James M. Gifford, Maurice C. Yap
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Patent number: 6225288Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters and hydrates thereof are disclosed along with pharmaceutical compositions and methods of treatment. The compounds are useful as inhibitors of caspase-3, which is implicated in modulating apoptosis.Type: GrantFiled: March 16, 2000Date of Patent: May 1, 2001Assignee: Merk Frosst Canada & Co.Inventors: Yongxin Han, Andre Giroux, Erich Grimm, Renee Aspiotis, Sebastien Francoeur, Robert Zamboni, Petpiboon Prasit, Christopher Bayly, Dan McKay, Cameron Black
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Patent number: RE40183Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula wherein R, X, R5 and R6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.Type: GrantFiled: June 3, 2005Date of Patent: March 25, 2008Assignee: Wyeth Holdings CorporationInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross