The Nitrogen Bonded Additionally Only To Hydrogen Patents (Class 546/311)
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Publication number: 20100298571Abstract: The invention relates to a method for preparing arylamines and, in particular, a method for preparing aniline and anilines substituted on the aromatic ring from ammonia, under easily-industrialised mild conditions with good selectivity and yields, in the presence of a catalytic system including a copper complex.Type: ApplicationFiled: September 24, 2008Publication date: November 25, 2010Inventors: Marc Taillefer, Ning Xia
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Patent number: 7820820Abstract: A method of preparing azaindole compounds for antiviral use having the formulaType: GrantFiled: August 24, 2009Date of Patent: October 26, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Wansheng Liu, Sunil S. Patel, Nicolas Cuniere, Yvonne Lear, Prashant P. Deshpande, Jeffrey N. Simon, Chiajen Lai, Annie J. Pullockaran, Nachimuthu Soundararajan, Jeffrey T. Bien
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Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
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Publication number: 20100240652Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.Type: ApplicationFiled: January 15, 2007Publication date: September 23, 2010Inventors: Karl Richard Gibson, Melanie Susanne Glossop
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Publication number: 20100234607Abstract: A process in which a 2-aminopyridine derivative of the general formula II is obtained from open-chain nitrile precursor I or III by reaction with a nitrogen compound in a cyclization reaction is described.Type: ApplicationFiled: March 11, 2010Publication date: September 16, 2010Inventors: Joerg JUNG, Sebastian Wuertz
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Publication number: 20100179172Abstract: A novel pesticide is provided. The present invention provides a pesticide containing, as an active ingredient, an N-phenyl-methanamine derivative represented by the formula (I) or its salt: wherein R1 is alkyl which may be substituted, etc.; each of R2, R3, R4 and R6 which are independent of one another, is hydrogen, halogen, alkyl which may be substituted, etc.; R5 is haloalkyl or halogen; each of R7 and R8 which are independent of each other, is hydrogen, cyano, alkyl, etc.; R9 is alkyl, cycloalkyl, etc.; m is from 0 to 1 and n is from 0 to 4.Type: ApplicationFiled: June 20, 2008Publication date: July 15, 2010Applicant: Ishihara Sangyo Kaisha , Ltd.Inventors: Masayuki Morita, Kazuhiro Yamamoto, Toshihiko Ueki, Kumiko Azuma, Taku Hamamoto
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Publication number: 20100121061Abstract: The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.Type: ApplicationFiled: December 8, 2009Publication date: May 13, 2010Applicant: Targacept, Inc.Inventors: William S. Caldwell, Gary M. Dull, Balwinder S. Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared M. Wagner, Peter A. Crooks, Patrick M. Lippiello, Merouane Bencherif
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Patent number: 7704995Abstract: This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.Type: GrantFiled: May 2, 2003Date of Patent: April 27, 2010Assignee: Exelixis, Inc.Inventors: Chris A. Buhr, Tae-Gon Baik, Sunghoon Ma, Zerom Tesfai, Longcheng Wang, Erick Wang Co, Sergey Epshteyn, Abigail R Kennedy, Baili Chen, Larisa Dubenko, Neel Kumar Anand, Tsze H. Tsang, John M. Nuss, Csaba J Peto, Kenneth D. Rice, Mohamed Abdulkader Ibrahim, Kevin Luke Schnepp, Xian Shi, James William Leahy, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Grace Mann, Larry Wayne Mann, Craig Stacy Takeuchi, Peter Lamb, David J. Matthews, Nicole Miller
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Patent number: 7662822Abstract: This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.Type: GrantFiled: April 23, 2005Date of Patent: February 16, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Tobias Wunberg, Judith Baumeister, Mario Jeske, Frank Süβmeier, Holger Zimmermann, Kerstin Henninger, Dieter Lang
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Patent number: 7645799Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: November 7, 2008Date of Patent: January 12, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
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Patent number: 7598380Abstract: A method of preparing azaindole compounds for antiviral use having the formulaType: GrantFiled: July 25, 2006Date of Patent: October 6, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Wansheng Liu, Sunil S. Patel, Nicolas Cuniere, Yvonne Lear, Prashant P. Deshpande, Jeffrey N. Simon, Chiajen Lai, Annie J. Pullockaran, Nachimuthu Soundararajan, Jeffrey T. Bien
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Publication number: 20090176989Abstract: The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1).Type: ApplicationFiled: December 4, 2008Publication date: July 9, 2009Inventor: David Siesel
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Patent number: 7446117Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.Type: GrantFiled: September 12, 2003Date of Patent: November 4, 2008Assignee: Glaxo Group LimitedInventors: Paul Beswick, Neil Pegg, Martin Swarbrick, John Skidmore, Sandeep Modi
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Publication number: 20080251754Abstract: The invention concerns novel ionic compounds with low melting point whereof the onium type cation having at least a heteroatom such as N, O, S or P bearing the positive charge and whereof the anion includes, wholly or partially, at least an ion imidide such as (FX1O)N?(OX2F) wherein X1 and X2 are identical or different and comprise SO or PF, and their use as solvent in electrochemical devices. Said composition comprises a salt wherein the anionic charge is delocalised, and can be used, inter alia, as electrolyte.Type: ApplicationFiled: March 28, 2008Publication date: October 16, 2008Applicants: ACEP INC., CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE MONTREALInventors: CHRISTOPHE MICHOT, Michel Armand, Michel Gauthier, Nathalie Ravet
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Patent number: 7435743Abstract: Pyrimidine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: September 30, 2005Date of Patent: October 14, 2008Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshiro, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuiyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Patent number: 7432227Abstract: 4-Aminopicolinic acids having alkyl or alkenyl substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: April 2, 2004Date of Patent: October 7, 2008Assignee: Dow AgroSciences LLCInventors: Terry William Balko, Ann Marie Buysse, Stephen Craig Fields, Nicholas Martin Irvine, William Chi-Leung Lo, Christian Thomas Lowe, John Sanders Richburg, Paul Richard Schmitzer
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Publication number: 20080207695Abstract: There is provided a compound of formula (I) wherein R1, R2a, R2b, R3a, R3b, R4, R5a, R5b, R6 to R8, A and G have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of thrombin is required or desired, and/or conditions where anticoagulant therapy is indicated).Type: ApplicationFiled: June 14, 2006Publication date: August 28, 2008Applicant: ASTRAZENECA ABInventors: Ingemar Nilsson, Magnus Polla
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Publication number: 20080182842Abstract: The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.Type: ApplicationFiled: January 29, 2008Publication date: July 31, 2008Applicant: ASTRAZENECA ABInventors: Jean-Claude Arnould, Benedicte Delouvrie, Christine Marie Paul Lambert-Van Der Brempt
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Publication number: 20080161363Abstract: The present invention is directed to 2-aminopyridine compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: October 25, 2005Publication date: July 3, 2008Inventors: Craig A. Coburn, M. Katharine Holloway, Shawn J. Stachel
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Publication number: 20080132539Abstract: To provide a novel compound which inhibits the generation of AGE and an AGE generation inhibitor containing the compound. A compound represented by the following formula or a pharmaceutically acceptable salt thereof, a medicinal composition containing the compound or such a salt thereof, and an additive composition containing the compound.Type: ApplicationFiled: December 27, 2004Publication date: June 5, 2008Inventors: Junji Kakuchi, Toru Yamazaki, Kazumi Obara, Hideyuki Yamato
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Patent number: 7342115Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Patent number: 7320985Abstract: A method for stabilizing an arylcarboxylic acid, which comprises adding a heterocyclic base to the arylcarboxylic acid or a pharmacologically acceptable salt thereof, a stabilizer thereof and an aqueous solution containing a stabilized arylcarboxylic acid. According to the stabilization method of the present invention, arylcarboxylic acid and pharmacologically acceptable salts thereof, particularly pranoprofen, can be stabilized at every temperature range, particularly at lower temperatures, thereby making the production of an aqueous solution to be used as an eye drop, nasal drop, ear drop and the like possible.Type: GrantFiled: July 23, 2003Date of Patent: January 22, 2008Assignee: Senju Pharmaceutical Co., Ltd.Inventor: Shirou Sawa
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Patent number: 7220863Abstract: A method for preparing 2-aminopyridine derivatives, which comprises substituting of fluorine for hydrazine moiety and reducing with hydrogen using 3-substituted-2,5,6-trifluoropyridine as a starting material, provides 2-aminopyridine derivatives having a purity over 98% under a mild reaction condition.Type: GrantFiled: August 23, 2005Date of Patent: May 22, 2007Assignee: Korea Research Institute of Chemical TechnologyInventors: Tae-Ho Park, Long-Xuan Zhao, Sang-Ho Lee
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Patent number: 7148229Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl substituted by halogen substituted phenyl; R2 is lower alkyl or lower alkyl substituted by lower cycloalkyl; and R3 is: Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: February 11, 2004Date of Patent: December 12, 2006Assignee: Hoffman-La Roche Inc.Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
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Patent number: 7129238Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.Type: GrantFiled: November 21, 2003Date of Patent: October 31, 2006Assignee: Hoffmann-La Roche Inc.Inventors: David William Banner, Luca Claudio Gobbi, Katrin Groebke Zbinden, Ulrike Obst, Christoph Martin Stahl
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Patent number: 7067541Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: June 3, 2004Date of Patent: June 27, 2006Assignee: Pfizer IncInventors: Alan Daniel Brown, Justin Stephen Bryans, Charlotte Alice Louise Lane, Simon John Mantell
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Patent number: 7056909Abstract: The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as ?v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and/or ?v?5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.Type: GrantFiled: July 20, 2001Date of Patent: June 6, 2006Assignee: Merck & Co., Inc.Inventor: Jiabing Wang
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Patent number: 7034044Abstract: The present invention relates to compounds of formulae The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and are used in the treatment of diseases related to this receptor.Type: GrantFiled: September 26, 2003Date of Patent: April 25, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, Rene Wyler
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Patent number: 7022718Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: January 18, 2005Date of Patent: April 4, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Matthias Steger, Peter Weiss
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Patent number: 7012078Abstract: The present invention relates to 2-aminopyridine derivatives of the formula wherein G, R1 and R2 are defined as in the specification, that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system and other disorders.Type: GrantFiled: December 6, 2002Date of Patent: March 14, 2006Assignee: Pfizer Inc.Inventor: John Adams Lowe, III
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Patent number: 6984649Abstract: Pyridine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents 1.2.3.6-tetrahydro-pyridine, or —CR31R32R33 wherein R31 represents H or C1-6 alkyl and R32 and R33 are joined to form a 5-8 membered saturated ring optionally containing up to three heteroatoms; R4 is carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: March 28, 2003Date of Patent: January 10, 2006Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshino, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Patent number: 6951875Abstract: The present invention relates to compounds of formulae The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and are used in the treatment of diseases related to this receptor.Type: GrantFiled: October 21, 2002Date of Patent: October 4, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, Rene Wyler
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Patent number: 6803470Abstract: The present invention relates to the compounds 6-[4-(N-methyl-3-azetidinoxy)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine, 6-[4-(N,N-dimethylaminomethyl)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine, 6-[4-(N-methylaminomethyl)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine and 6-[4-(3-azetidinoxy)-5-ethyl-2-methoxy-phenyl]-pyridin-2-ylamine, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds and to the use of such compounds in the treatment and prevention of central nervous system and other disorders.Type: GrantFiled: October 8, 2002Date of Patent: October 12, 2004Assignee: Pfizer IncInventors: John A. Lowe, III, Robert A. Volkmann
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Patent number: 6800784Abstract: The present invention concerns a process for preparing a polyaromatic compound comprising a concatenation of two aromatic cycles and carrying at least one amino group on one of the aromatic cycles. The process of the invention is characterized in that it consists of reacting an aromatic compound carrying at least one amino group and a leaving group with an arylboronic acid in an aqueous medium and in the presence of a palladium catalyst.Type: GrantFiled: September 3, 2002Date of Patent: October 5, 2004Assignee: Rhodia ChimieInventors: Thierry Schlama, Jean-Christophe Bigouraux
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Patent number: 6800650Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: February 11, 2003Date of Patent: October 5, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Claus Riemer, Peter Weiss
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Patent number: 6589967Abstract: The present invention relates to novel oxime O-ether compounds represented by a general formula [I]; wherein R1 represents C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, etc., m represents an integer of 1 to 4, R2 represents hydrogen atom, C1-6 alkyl, etc., R3 and R4 each independently represents hydrogen atom or C1-6 alkyl, etc., R5 represents hydrogen atom, C1-6 alkyl, etc., R6 represents C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, Halogen atom, etc. and n represents an integer of 1 to 4, and a fungicide for agricultural and horticultural use comprising the compound as the active ingredient.Type: GrantFiled: May 6, 2002Date of Patent: July 8, 2003Assignee: Nippon Soda Co. Ltd.Inventors: Hiroshi Sano, Tadashi Sugiura, Yuuki Nakagawa, Hiroshi Hamamura, Akira Mitani, Takahiro Ando
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Patent number: 6492515Abstract: The present invention relates to benzoxazinones of formula I: or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.Type: GrantFiled: July 31, 2001Date of Patent: December 10, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Joseph Marian Fortunak, Mona Patel
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Patent number: 6465491Abstract: The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.Type: GrantFiled: April 4, 2001Date of Patent: October 15, 2002Assignee: Pfizer Inc.Inventors: John A. Lowe, III, Peter J. Whittle
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Patent number: 6433214Abstract: A process for the preparation of 2-(4-methylphenyl)benzoic acid C1-6alkyl esters by reaction of a sulfonic derivative of formula wherein R is C1-6alkyl and R1 is optionally perfluorinated C1-6alkyl or optionally substituted C1-6aryl, with a 4-methylphenylzinc halide.Type: GrantFiled: April 3, 2000Date of Patent: August 13, 2002Assignee: Dipharma S.p.A.Inventors: Graziano Castaldi, Antonio Tarquini, Renzo Rossi
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Patent number: 6410737Abstract: Compounds of formula (I) are prepared by hydrogenolysis of a compound of formula (II): where R1 is haloalkyl, haloalkoxy or −SF5; W is N or CR3; and R2 and R3 are H or Cl. The compounds of formula (I) can be used as intermediates in the preparation of pesticidally active arylpyrazole compounds.Type: GrantFiled: January 4, 2002Date of Patent: June 25, 2002Assignee: Aventis CropScience, S.A.Inventors: Jean-Erick Ancel, Gilles Perrin-Janet, Manuel Vangelisti, Pierre Versproumy
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Patent number: 6399781Abstract: A method for making 3-amino-2-chloro-4-methylpyridine, as shown in Scheme 12, below.Type: GrantFiled: September 12, 2001Date of Patent: June 4, 2002Assignee: Boehringer Ingelheim Chemicals, Inc.Inventor: Bernard Franklin Gupton
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Patent number: 6372768Abstract: The present invention relates to 2-aminopyridine derivatives of the formula I: or pharmaceutically acceptable salts thereof, wherein A and B are each independently H, or together, A and B form a ring fused to the phenyl ring, said ring being saturated or unsaturated and containing from 5 to 7 ring member atoms, where said ring member atoms may optionally comprise from 1 to 2 heteroatoms selected independently from the group consisting of N, O or S, provided that no two adjacent ring members are heteroatoms; X is oxygen or a single bond; Y is (C1-C6)alkyl; R1 is hydrogen, (C1-C6)alkyl or a (C1-C6 alkyl) group substituted with —NR2R3 wherein R2 and R3 are either selected independently from the group consisting of H, alkyl, aryl, aralkyl or tetrahydronaphthalene, wherein said aryl group or said aryl moiety of said aralkyl group is phenyl or naphthyl, said alkyl group or said alkyl moiety of said aralkyl group contains from one to six carbon atoms and is straight-chained or branched,Type: GrantFiled: February 8, 2001Date of Patent: April 16, 2002Assignee: Pfizer INCInventor: John A. Lowe, III
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Publication number: 20010049379Abstract: The present invention relates to 2-aminopyridine derivatives of the formula 1Type: ApplicationFiled: December 20, 2000Publication date: December 6, 2001Inventor: John Adams Lowe
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Patent number: 6323366Abstract: The present invention provides a method for the preparation of a wide range of primary arylamines. The arylamines are prepared in two efficient, straightforward transformations: 1) an activated aryl group and an imine group are combined, in the presence of a transition metal catalyst, under conditions wherein the transition metal catalyst catalyzes the formation of a carbon-nitrogen bond between the activated carbon of the arene and the imine nitrogen; and 2) the resulting N-aryl imine is transformed, via any of a number of standard protocols, to the primary arylamine. The method of the invention may also be exploited in the preparation of vinylamines.Type: GrantFiled: July 24, 1998Date of Patent: November 27, 2001Assignee: Massachusetts Institute of TechnologyInventors: John P. Wolfe, Jens Ahman, Joseph P. Sadighi, Robert A. Singer, Stephen L. Buchwald
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Patent number: 6297197Abstract: 4-Aminopicolinic acids, having halogen, alkoxy, alkylthio, aryloxy, heteroaryloxy or trifluoromethyl substituents in the 3-, 5- and 6-positions, and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: January 12, 2001Date of Patent: October 2, 2001Assignee: Dow AgroSciences LLCInventors: Stephen Craig Fields, Anita Lenora Alexander, Terry William Balko, Leslie Anne Bjelk, Ann Marie Buysse, Renee Joan Keese, Karl Leopold Krumel, William Chi-Leung Lo, Christian Thomas Lowe, John Sanders Richburg, III, James Melvin Ruiz
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Publication number: 20010007873Abstract: This present invention relates to compounds of the formula 1Type: ApplicationFiled: July 31, 1998Publication date: July 12, 2001Inventors: ROBERT A. VOLKMANN, JOHN A. LOWE, JOLANTA NOWAKOWSKI
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Publication number: 20010003780Abstract: Retinoid antagonist compounds have been found to be useful in the prevention and/or minimization of surgical adhesion formation.Type: ApplicationFiled: December 8, 2000Publication date: June 14, 2001Inventors: Kenneth M. Tramposch, Xina Nair, Anne Marinier, Fred Christopher Zusi
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Patent number: 6211208Abstract: The present invention relates to 2-aminopyridine derivatives of the formula I: or pharmaceutically acceptable salts thereof, wherein A and B are each independently H, or together, A and B form a ring fused to the phenyl ring, said ring being saturated or unsaturated and containing from 5 to 7 ring member atoms, where said ring member atoms may optionally comprise from 1 to 2 heteroatoms selected independently from the group consisting of N, O or S, provided that no two adjacent ring members are heteroatoms; X is oxygen or a single bond; Y is (C1-C6)alkyl; R1 is hydrogen, (C1-C6)alkyl or a (C1-C6 alkyl) group substituted with —NR2R3 wherein R2 and R3 are either selected independently from the group consisting of H, alkyl, aryl, aralkyl or tetrahydronaphthalene, wherein said aryl group or said aryl moiety of said aralkyl group is phenyl or naphthyl, said alkyl group or said alkyl moiety of said aralkyl group contains from one to six carbon atoms and is straight-chained or branched,Type: GrantFiled: February 15, 2000Date of Patent: April 3, 2001Assignee: Pfizer IncInventor: John A. Lowe, III
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Patent number: 6194599Abstract: The present invention provides a process for preparing biaryl compounds comprising reacting an arylzinc reagent with an arylchloride in the presence of a nickel catalyst or a palladium catalyst. The present invention specifically provides a process for the preparation of 2-(4′-methylphenyl)benzonitrile comprising reacting a 4-methylphenylzinc reagent with 2-chlorobenzonitrile in the presence of a nickel catalyst or a palladium catalyst.Type: GrantFiled: April 8, 1997Date of Patent: February 27, 2001Assignee: Catalytica, Inc.Inventors: Joseph A. Miller, Robert P. Farrell