Chalcogen Or Halogen Containing Substituent Patents (Class 544/215)
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Patent number: 7642255Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, c-Raf, Csk, Fes, FGFR, Flt3, Ikk, IR, JNK, Lck, Mkk, PKC, PKD, Rsk, SAPK, Syk, Trk, BTK, Src, EGFR, IGF, Mek, Ros and Tie2 kinases.Type: GrantFiled: April 8, 2008Date of Patent: January 5, 2010Assignee: IRM LLCInventors: Taebo Sim, Hyun Soo Lee, Pingda Ren, Qiang Ding, Yi Liu, Bing Li, Lintong Li, Xia Wang, Tetsuo Uno, Guobao Zhang, Nathanael Schiander Gray, Shuli You
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Publication number: 20090286976Abstract: The present invention relates to a method for one-pot synthesis of ionic liquid with fluoroalkyl group, more particularly to a method for one-pot synthesis of ionic liquid with fluoroalkyl group represented by the following Chemical Formula 1 by adding and reacting a nitrogen-containing compound, a Brønsted acid of the formula YH and a fluoroolefin compound of the formula CFR1?CR2R3 in a single reactor: wherein represents a nitrogen-containing compound; Y? represents an anion of the Brønsted acid; and R1, R2 and R3, which may be same or different, represent hydrogen, fluorine, C1-C10 alkyl or C1-C10 fluoroalkyl having from 1 to 23 fluorine atoms.Type: ApplicationFiled: August 15, 2008Publication date: November 19, 2009Inventors: Hyun Joo Lee, Dong Jin Suh, Byoung Sung Ahn, Hong Gon Kim, Chang Soo Kim, Hoon Sik Kim
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Publication number: 20090270369Abstract: Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R1, R2 and R3 represent hydrogen, etc., X1 represents C1-6 alkylene, etc., X2 represents C1-6 alkylene, etc., A1 represents a 5- to 6-membered heterocyclic group, etc., and A2 represents C6-14 aryl, etc.Type: ApplicationFiled: February 9, 2009Publication date: October 29, 2009Applicant: Eisai R&D Management Co., Ltd.Inventors: Fumihiro Ozaki, Motohiro Soejima, Tasuku Ishida, Yoshihiko Norimine, Nobuyuki Kurusu, Eriko Doi, Toshihiko Kaneko, Daiju Hasegawa, Kiyoaki Kobayashi, Noburu Yamamoto
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Patent number: 7569526Abstract: Disclosed herein is a method for reducing the oxidative and biological degradation of a metalworking fluid comprising adding thereto at least one antioxidant and at least one biocide.Type: GrantFiled: March 12, 2004Date of Patent: August 4, 2009Assignee: Crompton CorporationInventors: Michael T. Costello, Igor Riff
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Patent number: 7550463Abstract: An object of the present invention provides a novel compound having the anti-viral activity, particularly, the HIV integrase inhibitory activity, and a drug containing the same, particularly, an anti-HIV drug.Type: GrantFiled: September 14, 2005Date of Patent: June 23, 2009Assignee: Shionogi & Co., Ltd.Inventor: Hiroshi Yoshida
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Patent number: 7507734Abstract: Disclosed are compounds according to the general formula (I), where the definitions of the substituents X, R1 and R2 are detailed in the description, as well as their physiologically acceptable salts and solvate, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).Type: GrantFiled: November 16, 2006Date of Patent: March 24, 2009Assignee: Aventis Pharma S.A.Inventors: Swen Hoelder, Gunter Muller, Karl Schoenafinger, David William Will, Hans Matter, Martin Bossart, Cecile Combeau, Christine Delaisi, Ingrid Sassoon, Anke Steinmetz, Didier Benard
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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
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Publication number: 20080275235Abstract: Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)- signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.Type: ApplicationFiled: July 23, 2008Publication date: November 6, 2008Applicants: PFIZER INC., PFIZER PRODUCTS INC.Inventors: Laura C. Blumberg, Michael J. Munchhof, Andrei Shavnya
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Patent number: 7405296Abstract: Compounds of formula wherein Rf is a (per)fluoropolyoxyalkylene chain having a number average molecular weight in the range 500-10,000; W1, W2, equal to or different from each other, are —F or —CF3; T1 is equal to —CHAa—Ba (CH2CH2O)na— wherein Aa=H, CF3; Ba=O, S, NH; na=0 or an integer between 1 and 6; T2 is equal to —F, —CF3, —C2 F5, —(C2 F4) Cl, or a group of formula: Q1, Q2 equal to or different from each other, are a chain of formula -T1-l -CFW1—O—Rf—CFW2-T?2, wherein: T?2 is equal to —F, —CF3, —C2 F5, —(C2F4) Cl; or is a group of formula: wherein B is equal to O, S, NH; R1, R2, R3, R4, R5 equal to or different from each other are selected from H, F, NO2, CN, C1-C8 perfluoroalkyl, carboxyl, phenyl (Ph), O- Ph, NH-Ph, S-Ph; wherein B is equal to O, S, NH; R1, R2, R3, R4, R5 equal to or different from each other are selected from H, F, NO2, CN, C1-C8 perfluoroalkyl, carboxyl, phenyl (Ph), O- Ph, NH-Ph, S-Ph; with the proviso that at least one of Q1 and Q2a is equal to:Type: GrantFiled: April 13, 2006Date of Patent: July 29, 2008Assignee: Solvay Solexis S.p.A.Inventors: Antonio Russo, Patrizia Maccone
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Publication number: 20080166593Abstract: The present invention relates to the use of certain organic compounds comprising fused aromatic compounds in organic electronic devices, in particular electroluminescent devices.Type: ApplicationFiled: March 20, 2006Publication date: July 10, 2008Inventors: Philipp Stoessel, Holger Heil, Horst Vestweber
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Patent number: 7354924Abstract: This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: GrantFiled: October 20, 2004Date of Patent: April 8, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Zhongxing Zhang, Nicholas A. Meanwell, John F. Kadow, Zhiwei Yin, Qiufen May Xue, Alicia Regueiro-Ren, John D. Matiskella, Yasutsugu Ueda
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Patent number: 7268228Abstract: This invention relates to compounds of Formula I having an aziridine-2-carboxylic group and a menthol group, a process for preparing such compounds, a method for obtaining optically active aziridine-2-carboxylate derivatives by optical resolution of such compounds, and optically active aziridine-2-carboxylate derivatives obtained by the same method: wherein R1 is hydrogen; alkyl; cycloalkyl; 4-chlorophenyl; 4-methoxyphenyl; s-triazinyl or pyridinyl acyl; benzyl; hydrocarbon residue which may be substituted with a substituent selected from the group consisting of hydroxy, alkoxy, dialkylamino, phenyl, 4-chlorophenyl and 4-methoxyphenyl; 2,4-dimethoxyphenyl; substituted phenyl including (1R)-phenylethyl or (1S)-phenylethyl. Preferences are given to (1R)-phenylethyl and (1S)-phenylethyl. Menthol is selected from the group consisting of (+)-menthol and (?)-menthol.Type: GrantFiled: August 10, 2001Date of Patent: September 11, 2007Assignee: Imagene Co., Ltd.Inventors: Won Koo Lee, Chan Sun Park, Yeon Hwa Lim, Hyun J on Ha
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Patent number: 7230098Abstract: Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided.Type: GrantFiled: February 26, 2004Date of Patent: June 12, 2007Assignee: Sugen, Inc.Inventors: Jingrong Jean Cui, Dilip Bhumralkar, Iriny Botrous, Ji Yu Chu, Lee A. Funk, Cathleen Elizabeth Hanau, G. Davis Harris, Lei Jia, Joanne Johnson, Stephen A. Kolodziej, Pei-Pei Kung, Xiaoyuan (Sharon) Li, Jason (Qishen) Lin, Jerry Jialun Meng, Mitchell David Nambu, Christopher G. Nelson, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube, Allison Walter, Fang-Jie Zhang, Jennifer Zhang
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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: 7214742Abstract: Compounds of the general formula I? in which R1 is H, C1–C12alkyl; C5–C12cycloalkyl; C2–C18alkyl which is interrupted by one or more O; SR4; OR5; or is a group of formula II or III R2, R21 and R3 independently of one another, are H or —Y—T as defined in claim 1, where T is a reactive group selected from OH, acryl- and methacryloxy and arylcarbonate groups, and further symbols are as defined in claim 1, are effective as crosslinking agents for polymeric networks, especially as in flexographic printing plates, coatings, and plastic containers or films. Further provided is a method of protecting the content of a clear or lightly colored plastic container or film against the deleterious effects of ultraviolet radiation, which method comprises permanently and covalently bonding one or more UV absorbing moieties of a durable s-triazine UV absorber via condensation to a suitable polymer component.Type: GrantFiled: November 21, 2002Date of Patent: May 8, 2007Assignee: Ciba Specialty Chemicals Corp.Inventors: Thomas Bolle, Andreas Valet, David George Leppard, Stephen Mark Andrews, Ramanathan Ravichandran, Markus Grob, Dirk Simon
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Patent number: 7135471Abstract: Aryl oxime derivatives of the formula (I), in which R1, R2, R3, X and B are as defined in claim 1, act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDSType: GrantFiled: May 16, 2003Date of Patent: November 14, 2006Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Norbert Beier, Pierre Schelling, Michael Wolf
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Patent number: 7129241Abstract: Pyridazine derivatives of the formula (I) act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDSType: GrantFiled: May 12, 2003Date of Patent: October 31, 2006Assignee: Merck Patent GesellschaftInventors: Hans-Michael Eggenweiler, Michael Wolf
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Patent number: 7122547Abstract: The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.Type: GrantFiled: November 9, 1999Date of Patent: October 17, 2006Assignees: Schering AG, Novartis AGInventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch, Guido Bold, Paul William Manley, Pascal Furet, Jeanette Marjorie Wood, Jürgen Mestan, Jose Brüggen, Stefano Ferrari, Martin Krüger, Eckhard Ottow, Andreas Menrad, Michael Schirner
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Patent number: 7064125Abstract: The invention relates to triazines and the use thereof to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity. The invention further relates to methods of treating cancer using said triazines. The invention also relates to methods for screening for LPAAT-? activity.Type: GrantFiled: November 13, 2003Date of Patent: June 20, 2006Assignee: Cell Therapeutics, Inc.Inventors: Baoqing Gong, John Tulinsky, Lynn Bonham, J. Peter Klein, Robert E. Finney, David M. Hollenback, Scott A. Shaffer, Norina M. Tang, Thayer H. White, David W. Leung
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Patent number: 7026307Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which R1, R2, R4 and Het are as defined in the description, with anhydrous hydrogen halide in the presence of a nitrile.Type: GrantFiled: April 24, 2002Date of Patent: April 11, 2006Assignee: Bayer CropScience AGInventors: Jörn Stölting, Kai van Laak, Wolfram Sirges, Armin Heyn, Torsten Taschner
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Patent number: 7026477Abstract: The invention relates to a preparation process for a compound (I) or a salt thereof, in which Q, X*, Y, Z, R, R1, R2 and R3 are as defined in claim 1, which comprises a) ammonolyzing a comp. (II) in which Hal=halogen atom to give (III), pref. (a1) carrying out the reaction in an organic solvent mixture (org. solv. mixture) comprising (1) opt. halogenated aromatic hydrocarbons and (2) polar aprotic solvents, in a weight ratio of solv. (1): solv. (2) of 20:1 to 1:1, (b) phosgenating the comp. (III) with phenylsulfonyl isocyanate of the formula (IV), pref. (b1) in the case X*=halogen, carrying out the reaction with phosgene in an org. solv. in the presence of isocyanates R?-NCO as catalyst, where R?=(subst.) hydrocarbon, with or without addition of an amine base, (c) reacting the resulting compound (IV) in org. solv. with the aminoheterocycle H2N-Het (Het=heterocycle as in (I)) to give the comp. (I) or a salt thereof, pref. (c1) carrying out the reaction in a solv. mixture of opt. halogenated arom.Type: GrantFiled: September 28, 2000Date of Patent: April 11, 2006Assignee: Aventis CropScience GmbHInventors: Jan Vermehren, Ernst Schmidt, Mark James Ford, Richard W. G. Foster, Ian A. Bourne
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Patent number: 6903097Abstract: 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: December 18, 2002Date of Patent: June 7, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Fred L. Ciske, John R. Palmer, Mark E. Schnute, Valerie A. Vaillancourt
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Patent number: 6867250Abstract: The invention relates generally to pyrimidines and triazines ultraviolet light absorbers containing a phenolic aromatic group(s) and a non-phenolic aromatic group(s) and the use thereof to protect against degradation by environmental forces, inclusive of ultraviolet light, actinic radiation, oxidation, moisture, atmospheric pollutants, and combinations thereof. The new class of pyrimidines and triazines includes two (one) non-phenolic aromatic groups with hydrocarbyl groups that are ortho to each other and one (two) resorcinol or substituted resorcinol group attached to a triazine or pyrimidine ring. The pyrimidines and triazines may be included in a polymeric structure. A method for stabilizing a material by incorporating the novel pyrimidines and triazines is also disclosed.Type: GrantFiled: October 30, 2000Date of Patent: March 15, 2005Assignee: Cytec Technology Corp.Inventors: Ram B. Gupta, Hargurpreet Singh, Russell C. Cappadona, Mark Paterna, Al Wagner
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Patent number: 6855269Abstract: This invention relates generally to phenyl ether substituted triazines compounds and compositions containing same and their use to protect against degradation by environmental forces. A method for stabilizing a material by incorporating such triazines is also disclosed.Type: GrantFiled: November 9, 2001Date of Patent: February 15, 2005Assignee: Cytec Technology Corp.Inventors: Ram Baboo Gupta, Hargurpreet Singh, Russell C. Cappadona
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Patent number: 6846818Abstract: The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I: pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The compounds of the invention are particularly useful in the treatment or alleviation of inflammation and inflammation associated disorders, such as, for example, rheumatoid arthritis and osteoarthritis, and in the relief of pain, such as, for example, pain associated with surgery or trauma, in mammals, preferably felines and canines.Type: GrantFiled: April 16, 2003Date of Patent: January 25, 2005Assignee: Pfizer Inc.Inventors: Kristin Lundy DeMello, Brian S. Bronk, Rhonda Marie Crosson
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Patent number: 6838415Abstract: The invention relates to novel substituted benzoylisoxazoles of the general formula (I), in which n represents the number 0, 1, 2 or 3, A represents a single bond or represents alkanediyl (alkylene), R1 represents hydrogen or represents in each case optionally substituted alkyl, alkenyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, halogen, or represents in each case optionally substituted alkyl, alkylcarbonyl, alkoxy, alkoxycarbonyl or alkylthio, alkylsulphinyl or alkylsulphonyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, and Z represents an optionally substituted 4-Type: GrantFiled: April 20, 2000Date of Patent: January 4, 2005Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Hans-Georg Schwarz, Heinz-Jürgen Wroblowsky, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
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Patent number: 6835329Abstract: The present invention provides compounds having the formula (1) in which each of the radicals R1, R2, R3 and R4, independently, represent hydrogen, hydroxy, halogen, C1-C20-alkyl, C1-C20-alkoxy, CN or COOR5, in which R5 is C1-C20-alkyl and Z represents a heterocyclic residue selected from the 2H-benzo[1,2-d]triazol-2-yl, 2H-naphtho[1,2-d]triazol-2-yl, benzimidazol-2-yl, benzoxazol-2-yl and benzofuran-2-yl moieties, optionally substituted by C1-C4-alkyl, C1-C4-alkoxy, halogen or NHCOC1-C4-alkyl, a process for their preparation, new intermediate benzoxazinones useful for their preparation and use of the compounds of formula (1) as UV-absorbers which have improved absorption spectrum characteristics, superior resistance to exposure to UV light and excellent thermal stability, relative to known triphenyltriazine compounds.Type: GrantFiled: March 31, 2003Date of Patent: December 28, 2004Assignee: Ciba Specialty Chemicals CorporationInventors: Dieter Reinehr, Hanspeter Sauter, Rudolf Zink
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Patent number: 6803349Abstract: A heterocyclic ring-containing compound represented by the following formula (1). In the formula, D represents a heterocyclic ring residue having a 5- to 7-membered ring structure and substituted with (m+n) of substituents, X represents a divalent linking group consisting of a single bond, NR3 group (R3 represents a hydrogen atom or an alkyl group having 1-30 carbon atoms), an oxygen atom, a sulfur atom, a carbonyl group, a sulfonyl group or a combination thereof, R1 represents an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, which may be substituted or unsubstituted, R2 represents a halogen atom, a hydroxy group, an unsubstituted amino group, a mercapto group, a cyano group, a sulfide group, a carboxy group or salt thereof, a sulfo group or salt thereof, a hydroxyamino group, a ureido group or a urethane group, m represents 1 or 2, and n represents an integer of 1 or larger.Type: GrantFiled: September 25, 2002Date of Patent: October 12, 2004Assignee: Fuji Photo Film Co., Ltd.Inventors: Masayuki Negoro, Kensuke Morita, Ken Kawata
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Publication number: 20040157843Abstract: The present invention relates to the use of 2-amino-thiazoline derivatives of formula (I): 1Type: ApplicationFiled: January 26, 2004Publication date: August 12, 2004Applicant: Aventis Pharma S.A.Inventors: Antony Bigot, Jean-Christophe Carry, Serge Mignani
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Patent number: 6773861Abstract: A UV absorbent represented by the following formula (1) [R1 represents an alkenyl group, all of R1 represent the same group, and R2, R3 and R4 independently represent a hydrogen atom, an alkyl group, an alkoxy group, or a halogen atom], a method of preparing the UV absorbent due to a reaction of a compound represented by the following formula (2) and an alkenylating agent represented by the following formula (3) in the presence of a base [R2, R3 and R4 independently represent a hydrogen atom, an alkyl group, an alkoxy group, or a halogen atom, and X represents a halogen atom, —OSO2R5 or —OSO2OR1, and R5represents an alkyl group or an aryl group], a composition containing therein the UV absorbent, and an image forming method using the composition:Type: GrantFiled: May 29, 2002Date of Patent: August 10, 2004Assignee: Fuji Photo Film Co., Ltd.Inventors: Masanobu Takashima, Hideaki Itou
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Patent number: 6759407Abstract: Novel pesticides of formula (I) wherein the substituents, R, R1, R2, R2′, T, U, X and Y are as defined in claim 1, are described. Also described are compositions suitable for use as parasiticides comprising those compounds as active ingredient and to methods of controlling parasites that are based on the administration of those compounds or compositions, and to the use of the said compounds and compositions in a method of controlling parasites and in the manufacture of pesticides for use against parasites. Also described are intermediates of formula (XX) wherein R1, R2, R2′, T, U, X and Y are as defined in claim 1; and Hal is halogen. The latter also exhibit parasiticidal activity and are suitable for the preparation of the compounds of formula (I).Type: GrantFiled: January 21, 2003Date of Patent: July 6, 2004Assignee: Novartis Animal Health US, Inc.Inventors: Thomas Goebel, Eliane Humbert-Droz, Maurizio Schwarzenbach
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Patent number: 6730785Abstract: It has been now surprisingly discovered after extensive research that 2-halo-4,6-bisaryl-1,3,5-triazine can be prepared with unprecedented selectivity, efficiency, mild conditions, and in high yield by the reaction of cyanuric halide with aromatics in the presence of at least one Lewis acid and at least one reaction promoter. This reaction is also unprecedently general as a variety of aromatics can be used to produce a wide selection of 2-halo-4,6-bisaryl-1,3,5-triazines. The novel approach includes the use of the reaction promoters in combination with at least one Lewis acid under certain reaction conditions to promote the formation of 2-halo-4,6-bisaryl-1,3,5-triazine compounds from cyanuric halide. Preferably, the Lewis acids and reaction promoters are combined to form a complex. 2-Halo-4,6-bisaryl-1,3,5-triazines are key intermediates for making 2-(2-oxyaryl)-4,6-bisaryl-1,3,5-triazine class of UV absorbers.Type: GrantFiled: February 9, 2001Date of Patent: May 4, 2004Assignee: Cytec Technology Corp.Inventors: Ram B. Gupta, Dennis J. Jakiela, Sampath Venimadhavan, Russell C. Cappadona, Venkatrao K. Pai
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Patent number: 6706743Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.Type: GrantFiled: March 5, 2003Date of Patent: March 16, 2004Assignee: Pfizer IncInventors: Robert F. Day, Jennifer A. Lafontaine
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6677353Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6664391Abstract: Novel N-fluorotriazinium electrophilic fluorinating agents have the Formula I: wherein three A moieties are independently CR, where each R is, independently, hydrogen, halogen, hydroxyl, (primary, secondary or tertiary) amino, 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, and at least one R is neither hydrogen nor halogen; 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, or adjacent triazinium moieties are linked by a common R substituent to provide an oligomer or polymer.Type: GrantFiled: October 23, 2001Date of Patent: December 16, 2003Assignee: Air Products and Chemicals, Inc.Inventors: Ronald Eric Banks, Mohamed Khalifa Besheesh
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Patent number: 6635760Abstract: Aromatic compounds having one or more electron-withdrawing substituents are fluorinated, preferably in a nitromethane solvent, by contact with tri(halo- or trifluoromethyl) substituted N-fluorotriazinium salts of the following Formula I: wherein three A moieties are independently CR, where each R is independently halogen or trifluoromethyl; 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. Preferably the cation of the salt is 2,4,6-trichloro-1,3,5-triazinium.Type: GrantFiled: October 23, 2001Date of Patent: October 21, 2003Assignee: Air Products and Chemicals, Inc.Inventors: Ronald Eric. Banks, Mohamed Khalifa Besheesh
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Publication number: 20030191242Abstract: The invention relates to metathesis polymers wherein an aromatic group that has UV-light absorbing properties is attached with a bridge group to the polymer. Also disclosed is a polymerisable composition comprising a catalytically effective amount of a penta- or hexavalent ruthenium or osmium carbene catalyst, the process for preparing the metathesis polymer by applying the reaction conditions of Ring Opening Metathesis Polymerisation (=ROMP) to the polymerisable composition; and various technical applications of the metathesis polymers.Type: ApplicationFiled: November 29, 2002Publication date: October 9, 2003Inventors: Alessandro Zedda, Dario Lazzari, Massimiliano Sala, Michela Bonora, Manuele Vitali, Paul Adriaan Van Der Schaaf
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Patent number: 6624166Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(═O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(═O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, sybstituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1&bgr; protease activity in a mammal utilizing the compounds and compositions.Type: GrantFiled: April 3, 1996Date of Patent: September 23, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roland E. Dolle, Denton W. Hoyer, Tina Morgan Ross, James M. Rinker, Stanley J. Schmidt, Mark A. Ator
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Patent number: 6617325Abstract: The present invention relates to biphenyl derivatives of general formula wherein Ra to Rg and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.Type: GrantFiled: May 15, 2002Date of Patent: September 9, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
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Patent number: 6573219Abstract: The invention relates to novel substituted heterocyclyl-2H-chromenes of the general formula (I) in which R1, R2, R3, R4, R5 Z are each as defined in the description, and to a process for their preparation and to their use as herbicides.Type: GrantFiled: February 5, 2002Date of Patent: June 3, 2003Assignee: Bayer AktiengesellschaftInventors: Karl-Heinz Linker, Roland Andree, Karl-Julius Reubke, Otto Schallner, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Publication number: 20030096993Abstract: Mixtures of compounds comprising a compound G2 and at least one further compound from the group G0, G1, G3, G4, G5, G6, the compounds G0-G6 each corresponding to formula (I) in which, in the compound G0, the radicals R1, R2, R3, R4, R5 and R6 are each hydrogen; G1, the radical R1 is Q and R2, R3, R4, R5 and R6 are each hydrogen; G2, the radicals R1 and R2 independently of one another are each Q and R3, R4, R5 and R6 are each hydrogen; G3 the radicals R1, R2 and R3 independently of one another are each Q and R4, R5 and R6 are each hydrogen; G4, the radicals R1, R2, R3 and R4 independently of one another are each Q and R5 and R6 are each hydrogen; G5, the radicals R1, R2, R3, R4 and R5 independently of one another are each Q and R6 is hydrogen; G6, the radicals R1, R2, R3, R4, R5 and R6 independently of one another are each Q; and Q and the other symbols are as defined in claim 1, are effective as stabilizers for organic material with respect to damaging exposure to light, oxygen and/or heat.Type: ApplicationFiled: June 19, 2002Publication date: May 22, 2003Inventor: Pascal Hayoz
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Patent number: 6559100Abstract: Substituted 2-benzoylcyclohexane-1,3-diones of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3, —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl or phenyl-C1-C6-alkyl; where the abovementioned alkyl radicals may be partially or fully halogenated and/or may carry one to three of the following groups: hydroxyl, mercapto, amino, cyano, R3, —OR3, —SR3, —N(R3)2, ═NOR3, —OCOR3, —SCOR3, —NR3COR3, —CO2R3, —COSR3, —CON(R3)2, C1-C4-alkyliminooxy, C1-C4-alkoxyamino, C1-C4-alkylcarbonyl, C1-C4-alkoxy-C2-C6-alkoxycarbonyl, C1-C4-alkylsulfonyl, heterocyclyl, heterocyclyloxy, phenyl, benzyl, hetaryl, phenoxy, benzyloxy and hetaryloxy, where the eight last mentioned radicType: GrantFiled: February 7, 2000Date of Patent: May 6, 2003Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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Publication number: 20030082464Abstract: A UV absorbent represented by the following formula (1) [R1 represents an alkenyl group, all of R1 represent the same group, and R2, R3 and R4 independently represent a hydrogen atom, an alkyl group, an alkoxy group, or a halogen atom], a method of preparing the UV absorbent due to a reaction of a compound represented by the following formula (2) and an alkenylating agent represented by the following formula (3) in the presence of a base [R2, R3 and R4 independently represent a hydrogen atom, an alkyl group, an alkoxy group, or a halogen atom, and X represents a halogen atom, —OSO2R5 or —OSO2OR1, and R5represents an alkyl group or an aryl group], a composition containing therein the UV absorbent, and an image forming method using the composition: 1Type: ApplicationFiled: May 29, 2002Publication date: May 1, 2003Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Masanobu Takashima, Hideaki Itou
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Patent number: 6555682Abstract: Provided are chromophores of the formula Q—(—L—Z)x, wherein x is 3 or 4, wherein Q is selected from the group consisting of wherein L is selected from the group consisting of wherein R is an alkyl group having 1 to 20 carbon atoms, and wherein Z is selected from the group consisting ofType: GrantFiled: June 13, 2002Date of Patent: April 29, 2003Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Ramamurthi Kannan, Loon-Seng Tan, Richard A. Vaia
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Publication number: 20030045444Abstract: Biphenyl-substituted triazines of the formulae 1Type: ApplicationFiled: July 31, 2002Publication date: March 6, 2003Inventors: Ian John Fletcher, Jurgen Kaschig, Georges Metzger, Dieter Reinehr, Pascal Hayoz
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Detecting reagent for double-stranded nucleic acid and double-stranded nucleic acid detecting method
Patent number: 6528648Abstract: The present invention provides a novel detecting reagent for double-stranded nucleic acid, and a method of using it to detect double-stranded nucleic acid formed by hybridization with a probe, with absolutely no labeling of the target nucleic acid. The detecting reagent for double-stranded nucleic acid of the invention is characterized by comprising, in the same molecule, a naphthalenediimide group which is intercalatable into double-stranded nucleic acid and a &bgr;-diketone group capable of forming a lanthanoid metal complex.Type: GrantFiled: December 5, 2001Date of Patent: March 4, 2003Assignee: Waseda University and RikenInventors: Kazuko Matsumoto, Takahiko Nojima, Hideo Tashiro, Yasumitsu Kondoh, Shigeori Takenaka -
Patent number: 6528455Abstract: Phenoxy- and thiophenoxyacrylic acid compounds of the formula I in which Het, R1, R2, R3, V, W and Z are as defined in claim 1 and processes for their preparation, intermediates for their preparation, herbicidally active compositions comprising the compounds of the formula I and a method for controlling harmful fungi are described.Type: GrantFiled: June 5, 2002Date of Patent: March 4, 2003Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Michael Puhl, Robert Reinhard, Ingo Sagasser, Cyrill Zagar, Karl-Otto Westphalen, Matthias Witschel, Helmut Walter
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Patent number: 6521609Abstract: A method for treating menopausal hot flushes using CGRP antagonists and/or CGRP release inhibitors and the corresponding pharmaceutical compositions containing as active substance one or more CGRP antagonists and/or CGRP release inhibitors, and the preparation thereof.Type: GrantFiled: July 12, 2000Date of Patent: February 18, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Henri Doods, Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel
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Publication number: 20030018190Abstract: This invention pertains generally to valency molecules, such as valency platform molecules which act as scaffolds to which one or more molecules may be covalently tethered to form a conjugate. More particularly, the present invention pertains to valency platform molecules which comprise a carbamate linkage (i.e., —O—C(═O)—N<). In one aspect, the present invention pertains to valency platforms comprising carbamate linkages, which molecules have the structure of any one of Formulae I, II, or III, shown in FIG. 1. In one aspect, the present invention pertains to valency platforms comprising carbamate linkages, which molecules have the structure of any one of Formulae IV, V, or VI, shown in FIG. 8. The present invention also pertains to methods of preparing such valency platform molecules, conjugates comprising such valency platform molecules, and methods of preparing such conjugates.Type: ApplicationFiled: August 13, 2002Publication date: January 23, 2003Inventor: David S. Jones