Plural Nitrogens In The Six-membered Hetero Ring Patents (Class 544/66)
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Patent number: 7713965Abstract: A subject of the invention is the compounds of formula (I): in which either R1 represents H, OH, NH2, —(CH2)m—NRaRb(m=0.1 or 2), Ra and Rb represent H, linear, branched or cyclic (C1-C6) alkyl, (C3-C6) cycloalkyl-(C3-C6)— alkyl, Rc, S(O)2Rc, C(O)Rc, S(O)2Rd or C(O)Rd; or Ra and Rb with N form an Rc radical; Rc represents a saturated, unsaturated or 5- or 6-members aromatic ring, containing 1 to 4 heteroatoms chosen from N, O and S, optionally substituted; Rd represents a linear, branched or cyclic (C1-C6) alkyl, optionally substituted by 1 to 4 halogens; or R1 represents Rc or CHReRc or CHReRd; Re represents H, OH, NH2, NH—(C1-C6)-alk or N-(C1-C6)-alk2, or NH—(C1-C7)-acyl or NHRc; R2 represents H, (CH2)m—NRaRb, Rc, CHReRc or CHReRd, and R?2 represents H.Type: GrantFiled: February 27, 2009Date of Patent: May 11, 2010Assignee: Vetoquinol SAInventors: Paola Ciapetti, Florence Chery-Mozziconacci, Camille G. Wermuth, Françoise Leblanc, Marc Schneider, Sandrine Ropp, Christophe Morice, Bruno Giethlen
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Publication number: 20100063275Abstract: The present invention relates, inter alia, to a process for preparing a compound of formula (I): using a quinuclidine-based catalyst or an optionally 3-substituted N-methyl pryrrolidine-based catalyst.Type: ApplicationFiled: October 2, 2007Publication date: March 11, 2010Applicant: SYNGENTA LIMITEDInventors: Gillan Beveridge, Ewan Campbell Boyd, Jack Hugh Vass, Alan John Whitton
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Patent number: 7666863Abstract: The present invention relates to benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.Type: GrantFiled: May 24, 2007Date of Patent: February 23, 2010Assignees: ViroPharma Incorporated, WYETHInventors: Ashis K. Saha, Christopher J Burns, Alfred M. Del Vecchio, Thomas R. Bailey, Jason A. Reinhardt, Bheemashankar A. Kulkarni, Thomas H. Faitg, Hao Feng, Susan R. Rippin, Charles W. Blackledge, David J. Rys, Thomas A. Lessen, John Swestock, Yijun Deng, Theodore J. Nitz
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Publication number: 20100009979Abstract: The invention relates to the use of quaternary ammonium compounds for preventing precipitations of fluoroquinolones from their solutions and to stable, tolerated pharmaceuticals which are particularly suitable for parenteral use and which contain, in dissolved form, a fluoroquinolone and a quaternary ammonium compound.Type: ApplicationFiled: February 23, 2007Publication date: January 14, 2010Applicant: BAYER ANIMAL HEALTH GMBHInventors: Iris Heep, Kristine Fraatz, Hans-Juergen Hamann, Markus Edingloh
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Publication number: 20100009980Abstract: A subject of the invention is the compounds of formula (I): wherein R1, R2, R3, R?3, R4, R?4, R5, R6 and R7 are as described in the application, in the form of enantiomers or mixtures, as well as their salts with acids and bases, their preparation and their application as anti-bacterials, in both human and veterinary medicine.Type: ApplicationFiled: June 23, 2009Publication date: January 14, 2010Applicant: Vetoquinol SAInventors: Sandrine Ropp, Christophe Morice, Bruno Giethlen, Paola Ciapetti, Florence Chery-Mozziconacci, Camille G. Wermuth, Francoise Leblanc, Marc Schneider
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Publication number: 20090258868Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 10, 2008Publication date: October 15, 2009Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
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Publication number: 20090253690Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.Type: ApplicationFiled: June 18, 2009Publication date: October 8, 2009Applicant: CytRx CorporationInventors: Zita Jegesne Csakai, Ede Marvanyos, Laszlo Urogdi, Magdolna Bathone Torok, Laszlo Denes
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Publication number: 20090246134Abstract: The present invention is directed toward radiolabelled ASIC imaging agents, as well as metabolites of ASIC antagonists. These compounds are useful for the diagnosis and treatment of diseases and disorders related to the activity of gated ion channels.Type: ApplicationFiled: May 30, 2008Publication date: October 1, 2009Applicant: PainCeptor Pharma CorporationInventors: Rahul Vohra, Gilles Dube, Zhonghong Gan
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Publication number: 20090227572Abstract: The present invention provides methods of enhancing healing of wound associated with diabetes, comprising administering an effective amount of one or more of certain hydroxylamine derivatives to a subject in need thereof. In another aspect, the instant invention provides methods of treating or preventing peripheral nervous system neuropathies. Peripheral nervous system neuropathies may but need not be diabetic neuropathies, and may but need not be associated with a diabetic wound. The invention also provides pharmaceutical compositions comprising a certain hydroxylamine derivative or a pharmaceutically acceptable salt thereof, optionally in combination with one or more additional therapeutic agents. In certain compositions and methods, the additional therapeutic agent is a second hydroxylamine derivative or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 17, 2009Publication date: September 10, 2009Applicant: Cytrx CorporationInventors: Jack R. Barber, Shi Chung Ng
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Publication number: 20090221565Abstract: A subject of the invention is the compounds of formula (I): in which either R1 represents H, OH, NH2, —(CH2)m—NRaRb(m=0.Type: ApplicationFiled: February 27, 2009Publication date: September 3, 2009Applicant: Vetoquinol SAInventors: Sandrine Ropp, Christophe Morice, Bruno Giethlen, Paola Ciapetti, Florence Chery-Mozziconacci, Camille G. Wermuth, Francoise Leblanc, Marc Schneider
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Patent number: 7550457Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.Type: GrantFiled: October 30, 2007Date of Patent: June 23, 2009Assignee: CytRx CorporationInventors: Zita Jegesné Csákai, Ede Márványos, László Ürögdi, Magdolna Bathóné Török, László Dénes
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Publication number: 20090143228Abstract: Novel dioxazine- and oxdiazine-substituted arylamides of the formula (I) in which A1, A2, R1, R2, R3, R4 and R5 are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.Type: ApplicationFiled: September 5, 2006Publication date: June 4, 2009Applicant: BAYER CROPSCIENCE AGInventors: Bernd-Wieland Kruger, Achim Hense, Bernd Alig, Rudiger Fischer, Christian Funke, Ernst Rudolf Gesing, Olga Malsam, Mark Wilhelm Drewes, Christian Arnold, Peter Lummen, Erich Sanwald
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Patent number: 7511034Abstract: Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: GrantFiled: January 11, 2006Date of Patent: March 31, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
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Publication number: 20090012070Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)=C(R7)N(R8)-, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)=C(R12)C(R13)=C(R14) 112, -, where R, R, R6, R7, R8, R11, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: August 22, 2008Publication date: January 8, 2009Applicant: Bayer Cropscience AGInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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Publication number: 20080306259Abstract: The present invention pertains to a process for preparing a compound of Formula I that is achiral, racemic or enantiomerically enriched at the hydroxylation center indicated by * comprising contacting a compound of Formula II with an oxidant selected from oxygen, hydrogen peroxide, peracids or alkyl hydropetoxides in the presence of a zirconium complex, wherein R1, R2 and R3 are as defined in the disclosure. This invention also pertains to zirconium complexes useful in this procedure comprising zirconium and a ligand of Formula III or its enantiomer wherein J, R6 and n are as defined in the disclosure. This invention further pertains to a compound of Formula III or its enantiomer.Type: ApplicationFiled: June 24, 2008Publication date: December 11, 2008Inventor: ALBERT LOREN CASALNUOVO
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Publication number: 20080299076Abstract: The present invention relates to erastin analogs, particularly compounds of formulae I and II, including compounds 1-20, 22-24, 34, and 40. The invention also relates to pharmaceutical compositions containing such analogs and to methods of treating conditions in a mammal with such analogs and pharmaceutical compositions.Type: ApplicationFiled: February 28, 2008Publication date: December 4, 2008Inventor: Brent R. Stockwell
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Publication number: 20080188448Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula I, the use of the progesterone receptor modulators for the manufacture of medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.Type: ApplicationFiled: December 20, 2007Publication date: August 7, 2008Inventors: Wolfgang Schwede, Thomas Andrew Kirkland, Anja Schmidt, Ulrike Fuhrmann, Carsten Moeller, Andrea Rotgeri
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Patent number: 7384936Abstract: The invention relates to carboxamidine derivatives to pharmaceutical compositions containing the same and the use thereof in the preparation of pharmaceutical compositions for the treatment of vascular diseases.Type: GrantFiled: January 10, 2003Date of Patent: June 10, 2008Assignee: CytRx CorporationInventors: Zita Jegesné Csákai, Ede Márványos, László Ürögdi, Magdolna Bathóné Török, László Dénes
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Publication number: 20080051578Abstract: The present invention relates to compounds of general formula (I) wherein A, B, L, R1, R2, R3a and R3b are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: August 24, 2006Publication date: February 28, 2008Inventors: Georg Dahmann, Kai Gerlach, Roland Pfau, Henning Priepke, Wolfgang Wienen, Annette Schuler-Metz, Herbert Nar
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Patent number: 7229988Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: GrantFiled: June 5, 2003Date of Patent: June 12, 2007Assignee: Samsung Electronics Co., Ltd.Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
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Patent number: 7105661Abstract: The invention relates to the use of morpholino-nucleosides of formula: in which R1 represents a nucleic base and R2 represents a group corresponding to one of the following formulae: —(CH2)n—NH2 —(CH2)n—SH —(CH2)n—COOH —(CH2)n—OH —(CH2)n—NH—R3 —(CH2)n—SR3 —(CH2)n—CO—R3 —(CH2)n—OR3 in which n is an interger ranging from 1 to 12 and R3 is a group derived from a label, from a protein, from an enzyme, from a fatty acid or from a peptide, as chain terminators in a process of DNA or RNA sequencing by the Sanger method, or for the labelling of DNA or RNA fragments.Type: GrantFiled: December 9, 2003Date of Patent: September 12, 2006Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche ScientifiqueInventors: Florence Marciacq, Sylvie Sauvaigo, Jean-François Mouret, Jean-Paul Issartel, Didier Molko
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Patent number: 7087598Abstract: This invention provides compounds of Formula I, their N-oxides and agriculturally suitable salts wherein A and B are independently O or S; J is an optionally substituted 5- or 6-memebered nonaromatic heterocyclic ring; K is taken together with the two contiguous linking carbon atoms to form a phenyl ring or a 5- or 6-membered heteroaromatic ring, each ring optionally substituted; and R1, R2, and R3 are as defined in the disclosure. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I, an N-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein).Type: GrantFiled: May 21, 2002Date of Patent: August 8, 2006Assignee: E. I. du Pont de Nemours and CompanyInventor: David Alan Clark
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Patent number: 7081526Abstract: The invention relates to the use of morpholino-nucleosides of formula: in which R1 represents a nucleic base and R2 represents a group corresponding to one of the following formulae: —(CH2)n—NH2 —(CH2)n—SH —(CH2)n—COOH —(CH2)n—OH —(CH2)n—NH—R3 —(CH2)n—SR3 —(CH2)n—CO—R3 —(CH2)n—OR3 in which n is an interger ranging from 1 to 12 and R3 is a group derived from a label, from a protein, from an enzyme, from a fatty acid or from a peptide, as chain terminators in a process of DNA or RNA sequencing by the Sanger method, or for the labelling of DNA or RNA fragments.Type: GrantFiled: December 9, 2003Date of Patent: July 25, 2006Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche ScientifiqueInventors: Florence Marciacq, Sylvie Sauvaigo, Jean-François Mouret, Jean-Paul Issartel, Didier Molko
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Patent number: 6943158Abstract: Compounds of formula I are p38 inhibitors: or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen or alkyl; R2 alkyl, haloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkyl, cyanoalkyl, heterocyclyl, heterocyclylalkyl, or —Y1—C(O)—Y2—R11 (where Y1 and Y2 are independently either absent or an alkylene group and R11 is hydrogen, alkyl, haloalkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino); R3 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, heterosubstituted cycloalkyl, heterocyclyl, aryl, aralkyl, haloalkyl, heteroalkyl, cyanoalkyl, -alkylene-C(?O)—R4 (where R4 is hydrogen, alkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino), or acyl; Ar1 is aryl; X1 is O, NR5 or S, where R5 is hydrogen or alkyl; and X2 is a bond, O, NR6, S or CH2, where R6 is hydrogen or alkyl.Type: GrantFiled: November 18, 2003Date of Patent: September 13, 2005Assignees: Roche Palo Alto LLC, Hoffmann-La Roche Inc.Inventors: Jian Jeffrey Chen, Kin-Chun Thomas Luk
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Patent number: 6916933Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: September 24, 2003Date of Patent: July 12, 2005Assignee: Hoffman-La Roche Inc.Inventors: Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
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Patent number: 6867298Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.Type: GrantFiled: May 8, 2003Date of Patent: March 15, 2005Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Wolter, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
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Patent number: 6838560Abstract: The invention relates to the use of morpholino-nucleosides of formula: in which R1 represents a nucleic base and R2 represents a group corresponding to one of the following formulae: —(CH2)n—NH2 —(CH2)n—SH —(CH2)n—COOH —(CH2)n—OH —(CH2)n—NH—R3—(CH2)nS—R3 —(CH2)n—CO—R3 —(CH2)n—OR3 in which n is an integer ranging from 1 to 12 and R3 is a group derived from a label, from a protein, from an enzyme, from a fatty acid or from a peptide, as chain terminators in a process of DNA or RNA sequencing by the Sanger method, or for the labelling of DNA or RNA fragments.Type: GrantFiled: February 21, 2000Date of Patent: January 4, 2005Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche ScientifiqueInventors: Florence Marciacq, Sylvie Sauvaigo, Jean-François Mouret, Jean-Paul Issartel, Didier Molko
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Publication number: 20040259870Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 protease that comprise a compound comprising the formula: 1Type: ApplicationFiled: March 24, 2004Publication date: December 23, 2004Applicant: Syrrx, Inc.Inventors: Jun Feng, Stephen L. Gwaltney, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
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Patent number: 6790955Abstract: The invention relates to the preparation of compounds (I) in which A═H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)-Het, where Ar=phenyl, M═H or cation and Het=heterocycle from formula (I), to give compounds (I) (A═H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A═H), or c) reaction of (III) with cyanates and amines (VII) of the formula HNR3-Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A═H) and optional acylation if A is to be other than H.Type: GrantFiled: November 5, 2002Date of Patent: September 14, 2004Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Jan Vermehren, Lothar Willms
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Publication number: 20040097493Abstract: The present invention provides a compound of the formula: 1Type: ApplicationFiled: November 18, 2003Publication date: May 20, 2004Inventors: Jian Jeffrey Chen, Kin-Chun Thomas Luk
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Publication number: 20040097728Abstract: The present invention relates to a process for preparing fused tetrahydro-[1H]-triazoles of the formula I 1Type: ApplicationFiled: March 5, 2003Publication date: May 20, 2004Inventors: Gerhard Hamprecht, Olaf Menke, Robert Reinhard, Michael Puhl, Ingo Sagasser, Cyrill Zagar, Matthias Witschel, Helmut Walter
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Patent number: 6737525Abstract: N-fluorotriazinium salts, especially those of the following Formula I, are electrophilic fluorinating agents useful in fluorinating, preferably in a nitromethane solvent, carbanionic species and/or activated aromatic compounds: wherein three A moieties are independently CR, where each R is, independently, hydrogen, halogen, (primary, secondary or tertiary) amino, hydroxyl, amino, cyano, perfluorothio hydroxysulfonyl, halosulfonyl, hydrocarbyloxysulfonyl, or a carbon-containing substituent selected from the group consisting of optionally substituted hydrocarbyl, hydrocarbyloxy, hydrocarbyloxycarbonyl, and hydrocarbylthio groups; two A moieties are independently Z, where each Z is independently nitrogen or a quaternary nitrogen atom and Y is a counterion or group of counterions which are inert to chemical attack by fluorine, and oligomers or polymers thereof in which adjacent triazinium moieties are linked by a common R substituent.Type: GrantFiled: October 23, 2001Date of Patent: May 18, 2004Assignee: Air Products and Chemicals, Inc.Inventors: Ronald Eric Banks, Mohamed Khalifa Besheesh
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Patent number: 6734304Abstract: The invention relates to a novel process for preparing known asymmetrical 4,6-bis(aryloxy)pyrimidine derivatives.Type: GrantFiled: September 17, 2002Date of Patent: May 11, 2004Assignee: Bayer AktiengesellschaftInventors: Holger Weintritt, Uwe Stelzer, Herbert Gayer, Walter Hübsch
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Publication number: 20040039197Abstract: The invention relates to novel, substituted, fused indole and heteroindole derivatives of the general formula I 1Type: ApplicationFiled: August 30, 2002Publication date: February 26, 2004Inventors: Heinz Weinberger, Thomas Beckers, Mathias Schmidt, Silke Baasner, Bernd Nickel
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Patent number: 6683028Abstract: The invention relates to novel guanidine derivatives of the formula (I) in which A, R1, R2, R3 and Z are as defined in the description, to a process for their preparation and to their use for controlling animal pests.Type: GrantFiled: August 17, 2001Date of Patent: January 27, 2004Assignee: Bayer AktiengesellschaftInventors: Klaus Wagner, Christoph Erdelen, Andreas Turberg, Norbert Mencke, Olaf Hansen
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Publication number: 20040014747Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animal, such as stroke.Type: ApplicationFiled: February 3, 2003Publication date: January 22, 2004Applicant: Neurocrine Biosciences, Inc.Inventor: Mustapha Haddach
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Publication number: 20030232821Abstract: Compounds of the formula 1Type: ApplicationFiled: July 22, 2003Publication date: December 18, 2003Inventors: Peter Maienfisch, Laurenz Gsell
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Publication number: 20030207867Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: ApplicationFiled: January 15, 2003Publication date: November 6, 2003Inventors: Mark W. Orme, Jason Scott Sawyer, Lisa M Schultze
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Patent number: 6639070Abstract: N-substituted perhydro-2,3-diazines of the formula I in which the variables Z, R, m and RA are as defined in claim 1, a process for their preparation and the use of the compounds of the formula I as starting materials for preparing herbicides of the formula V in which R, RA, Z and m are as defined above, X is O or S and Q is a C6-C14-aromatic radical are described.Type: GrantFiled: December 17, 2001Date of Patent: October 28, 2003Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Michael Puhl, Olaf Menke, Robert Reinhard, Ingo Sagasser, Cyrill Zagar
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Patent number: 6635637Abstract: Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R1, R3-R6, R21-R26, L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formulae I and II. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: August 2, 2001Date of Patent: October 21, 2003Assignee: Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Tianbao Lu, Bruce Edward Tomczuk, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Publication number: 20030187091Abstract: The invention relates to iminooxadiazine dione derivatives with the formula (I) 1Type: ApplicationFiled: February 10, 2003Publication date: October 2, 2003Applicant: Ivoclar Vivadent AG.Inventors: Norbert Moszner, Thomas Volkel, Urs Karl Fischer, Volker Rheinberger
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Patent number: 6624159Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: June 22, 2001Date of Patent: September 23, 2003Assignee: Pharmacia & Upjohn CompanyInventors: David John Anderson, Gordon L. Bundy, Fred L. Ciske, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
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Publication number: 20030166741Abstract: The invention relates to dental materials which contain an iminooxadiazine dione derivative with at least two free isocyanate groups and a hydroxyl compound with at least two OH groups.Type: ApplicationFiled: February 10, 2003Publication date: September 4, 2003Applicant: Ivoclar Vivadent AG.Inventors: Martin Klare, Andreas Radl, Volker Rheinberger
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Publication number: 20030139397Abstract: Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful as arthropodicides wherein A is H; E is H or C1-C3 alkyl; or A and E can be taken together to form —CH2—, —CH2CH2—, —O—, —S—, —S(O)—, —S(O)2—, —NR8—, —OCH2—, —SCH2—, —N(R8)CH2—, substituted —CH2— and substituted —CH2CH2—, the substituents independently selected from 1-2 halogen and 1-2 methyl; W is N or CR4;X is CR5R6, O, S, NR7 or a direct bond, provided that when W is N, then X is other than a direct bond; Y is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C3 alkylsulfonyl, C3-C6 cycloalkyl, C3-C6 cycloalkylalkyl, NR9R10, N═CR11R12, OR7, COR13, CO2R14 or C1-C6 alkyl substituted by at least one group selected from halogen, C1-C3 alkoxy, CN, NO2, S(O)1R15, COR13, CO2R14 and optionally substituted phenyl; Z is O or S; and R2, R3, R4, R5, R6, R7, R8, R9Type: ApplicationFiled: August 28, 2002Publication date: July 24, 2003Inventor: David Walter Piotrowski
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Publication number: 20030125325Abstract: The invention relates to novel pyrazolyl benzyl thioethers, to two processes for their preparation and to their use for controlling harmful organisms.Type: ApplicationFiled: June 28, 2002Publication date: July 3, 2003Inventors: Ulrich Heinemann, Bernd-Wieland Kruger, Herbert Gayer, Fritz Maurer, Christiane Boie, Ronald Ebbert, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik
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Patent number: 6579982Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: August 9, 2000Date of Patent: June 17, 2003Assignee: Pfizer Inc.Inventor: Julian Blagg
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Patent number: 6552187Abstract: A process for the preparation of compounds of formula (I), which process comprises reacting a compound of formula (II), in an inert organic solvent, optionally in the presence of a base, with a compound of formula (IV), (IVa) or (IVb), and optionally converting the resulting compound of formula (I) wherein G is a metal ion equivalent or an ammonium cation, by salt conversion into the corresponding salt of formula (I) wherein G is a sulfonium or phosphonium cation, or by treatment with a Brönsted acid into the corresponding compound of formula (I) wherein G is hydrogen, and ‘in situ’ conversion of compounds of formula (I) with an electrophile of formula (XII) or (XIId) G0—L (XII) or R32—N═C═X3 (XIId), optionally in the presence of an acid-binding agent or a catalyst, to the compounds of formula (Ia).Type: GrantFiled: November 29, 2001Date of Patent: April 22, 2003Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Maetzke, René Mutti, Henry Szczepanski
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Patent number: 6541469Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein X is nitrogen or CR3; A is O, S, or NR4, and R, R1, R2are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.Type: GrantFiled: May 18, 2001Date of Patent: April 1, 2003Assignee: Neurocrine Biosciences, Inc.Inventor: Mustapha Haddach
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Patent number: 6518266Abstract: The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I: or a salt thereof, where R1 represents R5O, R5SO2, R5SO or R5S in which R5 is as defined herein; X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond; R2 is hydrogen, amino, chloro, bromo, iodo, cyano, C1-6 alkoxy, C1-6 alkyl or C6-10 aryl; and R3-R7 each represent hydrogen, halogen, straight- or branched-chain C1-4 alkyl or C1-4 alkoxy, either of which is unsubstituted or substituted by one or more halogen atoms, straight- or branched-chain C1-4 alkylthio or C1-4 alkylsulphinyl, either of which is substituted by one or more halogen atoms, nitro, cyano, or straight- or branched-chain C1-4 alkylsulphonyl group which is unsubstituted or substituted by one or more halogen atoms.Type: GrantFiled: July 21, 2000Date of Patent: February 11, 2003Assignees: 3-Dimensional Pharmaceuticals, Heska CorporationInventors: Daljit S. Dhanoa, Dario Doller, Sanath Meegalla, Richard M. Soll, Nancy Wisnewski, Gary Silver, Dan T. Stinchcomb, R. Lee Seward, Dimitris Agrafiotis, Deyou Sha
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Patent number: 6476016Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: July 17, 2001Date of Patent: November 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone