Chalcogen Attached Directly To The 1,2-diazole Ring By Nonionic Bonding Patents (Class 546/276.1)
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Publication number: 20110033417Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: February 10, 2011Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20110003851Abstract: The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders.Type: ApplicationFiled: May 6, 2010Publication date: January 6, 2011Applicant: Ligand Pharmaceuticals, Inc.Inventors: Lin Zhi, Andrew R. Hudson, Cornelis A. Van Oeveren, Steven L. Roach, Jason C. Pickens, Yixing Shen, Catalina Cuervo, Lino J. Valdez, Jillian Basinger, Virgina H. Grant
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Publication number: 20100305085Abstract: The invention relates to dihydropyrazolon-derivatives of formula (I), to methods for their production, to their use for treating and/or for preventing diseases and their use for producing medicaments for treating and/or for preventing diseases, in particular cardiovascular and haematological diseases, kidney diseases and for promoting the healing of wounds.Type: ApplicationFiled: October 12, 2007Publication date: December 2, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Jörg Keldenich, Metin Akbaba, Mario Jeske
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Publication number: 20100298141Abstract: Disclosed are compounds of Formula 1, including N-oxides, and salts thereof, wherein W is O or NR7, n is 0 or 1, and R1, R2, R3, R4, R5, R6, R7 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention. Also disclosed are mixtures and compositions comprising a herbicidally effective amount of a compound of Formula 1 and an effective amount of another herbicide or herbicide safener.Type: ApplicationFiled: February 8, 2008Publication date: November 25, 2010Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Thomas Paul Selby, Brenton Todd Smith, Thomas Martin Stevenson
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Patent number: 7834186Abstract: A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(R2b)C(O)Y (i.e. Formula II) wherein X and Y are leaving groups and L, R1, R2a and R2b are as defined in the disclosure, with a substituted hydrazine of the formula LNHNH2 (i.e. Formula III) in the presence of a suitable acid scavenger and solvent. Also disclosed is the preparation of compounds of Formula IV wherein X1, R6, R7, R8a, R8b, R9, and n are as defined in the disclosure. Also disclosed is a composition comprising on a weight basis about 20 to 99% of the compound of Formula II wherein R1, R2a, R2b, R3, R4 and R5 are as defined in the disclosure; X is Cl, Br or I; and Y is F, Cl, Br or I; provided that when R2a and R2b are each H, and X and Y are each Cl then R1 is other than benzyl and when R2a and R2b are each phenyl, and X and Y are each Cl, then R1 is other than methyl or ethyl.Type: GrantFiled: September 19, 2008Date of Patent: November 16, 2010Assignee: E.I. du Pont de Nemours and CompanyInventor: Gary David Annis
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Publication number: 20100280251Abstract: Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; Y is Br or Cl; X is NR13 or O; n is 0 or 1; and R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 2 wherein Y is Br and R1 is NHR3 comprising introducing a gas containing bromine into a liquid containing a compound of Formula 4, and further disclosed is a method for preparing a compound of Formula 5 wherein R14, R15, R16 and Z are as defined in the disclosure using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above.Type: ApplicationFiled: December 18, 2007Publication date: November 4, 2010Applicant: E.I. Du Pont De Nemours and CompanyInventors: Joerg Bruening, Gary David Annis, Martin James Currie, Donald J. Dumas, Rafael Shapiro
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Publication number: 20100273830Abstract: An insecticidal compound of formula (I) in which G1, G2, and G3 together with the two carbon atoms to which G1 and G3 are attached, form a non-aromatic 4- or 5-membered ring system; wherein G1 is sulfur, SO, SO2, oxygen, a direct bond, NRa or CR5aR5b; G2 is sulfur, SO, SO2, oxygen, a direct bond, NRb or CR5cR5d; G3 is sulfur, SO, SO2, oxygen, a direct bond, NRc or CR5eR5f; with the provisos that a) not more than 1 group G can be a direct bond, b) not more than 2 G groups can be oxygen, sulfur, SO or SO2 and c) when 2 G groups are oxygen, SO, SO2 and/or sulfur the two groups are separated by a carbon atom; each of Z1 and Z2, which may be the same or different, represents oxygen or sulfur; D is phenyl or a 5- or 6-membered heteroaromatic ring and R1a, R1b, R5a, R5b, R5c, R5d, R5e, R5f, Ra, Rb Rc, R2, R3 and R20 are specified organic groups and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.Type: ApplicationFiled: July 14, 2008Publication date: October 28, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Roger Graham Hall, Olivier Loiseleur, Jagadish Pabba, Sitaram Pal, Andre Jeanguenat, Andrew Edmunds, Andre Stoller
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Publication number: 20100256192Abstract: In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: December 29, 2009Publication date: October 7, 2010Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Publication number: 20100222592Abstract: A pyridone derivative represented by Formula [1] or an agriculturally acceptable salt thereof: wherein R1 is a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or the like; R2 and R3 are each independently a hydrogen atom, a nitro group, a cyano group, or the like; and A is a group represented by Formula A-1, Formula A-2, Formula A-3, Formula A-4, or Formula A-5: The compounds represented by general formula [1] control various weeds growing in upland fields, orchards, paddy fields, and non-crop lands while showing high safety to useful plants and crops.Type: ApplicationFiled: January 31, 2007Publication date: September 2, 2010Applicants: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Fumiaki Takabe, Shunichirou Fukumoto, Ryu Kajiki, Sohei Asakura, Ryohei Ueno, Masami Kobayashi, Satoru Takahashi, Norihisa Yonekura, Ryo Hanai, Takashi Mitsunari
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Patent number: 7759381Abstract: Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.Type: GrantFiled: July 3, 2007Date of Patent: July 20, 2010Assignee: Aventis AgricultureInventors: Hyoung Ik Lee, Loïc Patrick Le Hir de Fallois, Philip Reid Timmons, William Glenn Cawthorne, Jr., Adalberto Perez de Leon
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Publication number: 20100179161Abstract: Compounds of the formula (I) and pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, useful in the treatment of Mycobacterium tuberculosis (M.tb).Type: ApplicationFiled: August 16, 2006Publication date: July 15, 2010Applicant: ASTRAZENECA ABInventors: Balachandra Shankar Bandodkar, Stefan Schmitt
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Publication number: 20100152443Abstract: The present invention provides a pyrazole derivative of the general formula (1), which has an excellent efficacy as an active component for a herbicide, an intermediate for the production thereof, processes for the production thereof, and a herbicide containing the derivative as an active ingredient.Type: ApplicationFiled: February 26, 2010Publication date: June 17, 2010Applicants: SAGAMI CHEMICAL RESEARCH CENTER, KAKEN PHARMACEUTICAL CO., LTD.Inventors: Kenji Hirai, Atsushi Uchida, Atsuko Watanabe, Taeko Abe, Takuya Ueda, Hiroshi Sakurai
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Patent number: 7723363Abstract: A compound of general formula (I). A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: March 1, 2005Date of Patent: May 25, 2010Assignee: Bayer Cropscience SAInventors: Darren James Mansfield, Heiko Rieck, Pierre-Yves Coqueron, Philippe Desbordes, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier
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Publication number: 20100063063Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: ApplicationFiled: September 9, 2009Publication date: March 11, 2010Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Patent number: 7666882Abstract: This invention provides compounds of Formula I, N-oxides and suitable salts thereof wherein Y and V are each independently N or CR4a; W is N, CH or CR6; and R1 through R6, and n are as defined in the disclosure. This invention also pertains to a composition for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula I, an N-oxide thereof or an agronomic or nonagronomic suitable salt of the compound and at least one additional component selected from the group consisting of a surfactant, a solid diluent and a liquid diluent, and optionally further comprising an effective amount of at least one additional biologically active compound or agent. 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 an agronomic or nonagronomic suitable salt of the compound or with the composition described herein.Type: GrantFiled: November 12, 2003Date of Patent: February 23, 2010Assignee: E.I. du Pont de Nemours and CompanyInventor: George Philip Lahm
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Patent number: 7659288Abstract: The invention relates to 5-aminoalkylaminopyrazole derivatives of formula (I) or salts thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).Type: GrantFiled: September 22, 2006Date of Patent: February 9, 2010Assignee: Merial LimitedInventors: Stefan Schnatterer, David Teh-Wei Chou, Werner Knauf, Daniela Jans, Karl Seeger
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Publication number: 20100022503Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: January 4, 2008Publication date: January 28, 2010Inventors: Marco Dodier, Claude A. Quesnelle, Anne Marinier
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Patent number: 7638514Abstract: There are described compounds of formula (I) wherein X1 and X2 are each independently of the other fluorine, chlorine or bromine; A1 and A2 are, for example, a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge; R1 and R2 are, for example, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkyl-carbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C3-C6alkynyl; R,3 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R4 and R5 are, for example, H, halogen, cyano, nitro, C1-C6alkyl or C1-C3haloalkyl; m is 1 or 2; Y is, for example, O, S, SO or SO2; Q is, for example, O, S, SO or SO2; W is, for example, a bond, O, S, SO, S02, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; and E is aryl unsubstituted or substituted from one to five times or heterocyclyl unsubstituted or, depending upon the possibilities of substitution on the ring, substituted from one to four times; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtType: GrantFiled: August 25, 2004Date of Patent: December 29, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Werner Zambach, Stephan Trah, Roger Graham Hall, William Lutz
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Publication number: 20090253751Abstract: Compounds effective for preventing, treatment or improving diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1, R2, R3, L1, L2, X and Y are defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: November 7, 2006Publication date: October 8, 2009Applicant: Nissan Chemical Industries, Ltd.Inventors: Katsuaki Miyaji, Yukihiro Shigeta, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
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Publication number: 20090227592Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).Type: ApplicationFiled: February 2, 2009Publication date: September 10, 2009Applicant: AstraZeneca ABInventors: Scott BOYD, Peter William Rodney CAULKETT, Rodney Brian HARGREAVES, Suzanne Saxon BOWKER, Roger JAMES, Clifford David JONES, Darren McKERRECHER, Michael Howard BLOCK, Craig JOHNSTONE
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Patent number: 7576107Abstract: The invention relates to the use for the control of pests, of a compound which is a 5-substituted-alkylaminopyrazole derivative of formula (I) or a salt thereof: wherein the various symbols are as defined in the description, to novel 5-substituted-alkylaminopyrazole derivatives and pesticidal compositions thereof, and to processes for their preparation.Type: GrantFiled: February 27, 2003Date of Patent: August 18, 2009Assignee: Merial LimitedInventors: David Teh-Wei Chou, Henricus Maria Marinus Bastiaans, Anke Kuhlmann, Maria-Theresia Thönessen, Stefan Schnatterer, Uwe Döller, Jamin Huang, Karl Seeger, Andrew Scribner, Adalberto A. Perez De Leon
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Publication number: 20090131676Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: July 19, 2006Publication date: May 21, 2009Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Katsuaki Miyaji, Yutaka Hirokawa, Masato Horikawa, Norihisa Ishiwata
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Publication number: 20090099209Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; and R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treatiType: ApplicationFiled: December 12, 2008Publication date: April 16, 2009Inventors: Paul Anthony Bradley, Kevin Neil Dack, Ian Roger Marsh
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Patent number: 7514561Abstract: Substituted-acylaminopyrazole derivatives of formula (I): or salts thereof, wherein the various symbols are as defined in the description, processes for their preparation, compositions thereof and methods for their use for the control of pests, such as arthropods (e.g. insects and arachnids) and helminths (including nematodes).Type: GrantFiled: November 12, 2003Date of Patent: April 7, 2009Assignee: Merial LimitedInventors: Stefan Schnatterer, David William Hawkins, Daniela Jans, Michael Maier, Anke Kuhlmann, Erich Friedrich Sanwald, Maria-Theresia Thönessen, Karl Seeger
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Publication number: 20090074373Abstract: The present invention provides optical filters comprising a squarylium compound represented by General Formula (I): [wherein R1 and R2 may be the same or different and each represents a hydrogen atom, an alkyl group optionally having substituent(s) or the like, R3 represents a hydrogen atom or an alkyl group optionally having substituent(s), and Y represents a group represented by General Formula (A): (wherein R4 represents a hydrogen atom, an alkyl group optionally having substituent(s) or the like, R5 represents a hydrogen atom, a halogen atom or the like, and R6, R7, R8 and R9 may be the same or different and each represents a hydrogen atom, a halogen atom, an alkyl group optionally having substituent(s) or the like)] and the like.Type: ApplicationFiled: November 18, 2005Publication date: March 19, 2009Applicant: KYOWA HAKKO CHEMICAL CO., LTD.Inventors: Junzo Yamano, Katsumi Ukai, Motoharu Kinugasa
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Publication number: 20090048256Abstract: The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: —N(R7)—, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: —N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: —N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc.Type: ApplicationFiled: October 20, 2006Publication date: February 19, 2009Inventors: Yasunori Moritani, Ritsuo Imashiro, Atsushi Sato
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Patent number: 7488824Abstract: The present invention relates to a process for the preparation of compounds of formula (I) wherein the substituents are as defined in claim 1, by reaction of a compound of formula (II) wherein R3 is C1-C8alkyl or C3-C6cycloalkyl and R4 and R05 are as defined for formula (I), with a compound of formula (III) wherein R, R1, R2 and X1, are as defined for formula (I) in claim 1, in an inert solvent in the presence of a proton source.Type: GrantFiled: March 5, 2004Date of Patent: February 10, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: David Anthony Jackson, Martin Charles Bowden
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Patent number: 7452873Abstract: The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I. The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I.Type: GrantFiled: June 3, 2005Date of Patent: November 18, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Michael J. Arnost, Albert Pierce
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Patent number: 7452874Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.Type: GrantFiled: January 8, 2007Date of Patent: November 18, 2008Assignee: SmithKline Beecham Corp.Inventors: Kevin J. Duffy, Juan I. Luengo, Antony N. Shaw, Kenneth Wiggall
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Publication number: 20080275070Abstract: The invention relates to aryl ether compounds and its preparation method and use thereof. The aryl ether compounds of the invention having general formula (I): The groups are as defined as specification. The aryl ether compounds of present invention have wide spectrum fungicidal activity, and may be used to control diseases in all sorts of plants caused by oomycete, basidiomycete, ascomycete pathogens and deuteromycete. The some of the compounds have very good insecticidal and acaricidal activity, and may be used to control insects and mites.Type: ApplicationFiled: May 15, 2006Publication date: November 6, 2008Applicant: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRYInventors: Changling Liu, Miao Li, Zhinian Li, Liwen Geng, Hong Zhang, Defeng Zhou, Dongliang Cui, Yanmei Luo
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Publication number: 20080269293Abstract: This invention relates to novel compounds of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof wherein Y, R1 through R9, and X1 through X7 are as defined in the specification, pharmaceutical compositions containing said compounds useful as P2Y1 antagonists, and to methods of treating thromboembolic disorders.Type: ApplicationFiled: August 22, 2007Publication date: October 30, 2008Inventors: Liguo Chi, Chulho Choi, Andrew G. Geyer, Robert M. Kennedy, Jeffery A. Pfefferkorn, Roy T. Winters
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Publication number: 20080263787Abstract: The present application relates to cationic pyrazolone dyes of the general formula (I), and to coloring agents for keratin fibers comprising these dyes.Type: ApplicationFiled: May 18, 2005Publication date: October 30, 2008Inventors: Markus Speckbacher, Hans-Juergen Braun
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Patent number: 7442702Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: September 25, 2002Date of Patent: October 28, 2008Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Patent number: 7442799Abstract: A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I. The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(R2b)C(O)Y (i.e. Formula II)wherein X and Y are leaving groups and L, R1, R2a and R2b are as defined in the disclosure, with a substituted hydrazine of the formula LNHNH2 (i.e. Formula III) in the presence of a suitable acid scavenger and solvent. Also disclosed is the preparation of compounds of Formula IV wherein X1, R6, R7, R8a, R8b, R9, and n are as defined in the disclosure. Also disclosed is a composition comprising on a weight basis about 20 to 99% of the compound of Formula II wherein R1, R2a, R2b, R3, R4 and R5 are as defined in the disclosure; X is Cl, Br or I; and Y is F, Cl, Br or I; provided that when R2a and R2b are each H, and X and Y are each Cl then R1 is other than benzyl and when R2a and R2b are each phenyl, and X and Y are each Cl, then R1 is other than methyl or ethyl.Type: GrantFiled: March 25, 2004Date of Patent: October 28, 2008Assignee: E.I. du Pont de Nemours and CompanyInventor: Gary David Annis
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Publication number: 20080167322Abstract: Substituted pyrazole compounds such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.Type: ApplicationFiled: February 14, 2006Publication date: July 10, 2008Inventors: Anthony B. Pinkerton, Rowena Cube, John Hutchinson, Dehua Huang, Jean-Michel Vernier, Dong-Ming Shen
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Publication number: 20080090880Abstract: Novel phenylpyrazole derivatives of the formula (I), in which R1-R6, X and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a roleType: ApplicationFiled: September 14, 2005Publication date: April 17, 2008Inventors: Hans-Michael Eggenweiler, Michael Wolf
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Publication number: 20080064682Abstract: A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrType: ApplicationFiled: July 1, 2005Publication date: March 13, 2008Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Naoaki Kanaya, Takashi Ishiyama, Ryo Muto, Toshiyuki Watanabe, Yuichi Ochiai
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Patent number: 7335649Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.Type: GrantFiled: November 9, 2006Date of Patent: February 26, 2008Assignee: SmithKline Beecham CorporationInventors: Kevin J. Duffy, Connie Erickson-Miller, Julian Jenkins, Juan I. Luengo, Sophie Visonneau
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Patent number: 7253290Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R5, R6, R6a, R7, R8, A, B and M are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.Type: GrantFiled: August 19, 2003Date of Patent: August 7, 2007Assignee: AstraZeneca ABInventors: Thomas Geoffrey Bird, Mickael Louis Pierre Maudet
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Patent number: 7232836Abstract: This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.Type: GrantFiled: August 13, 2002Date of Patent: June 19, 2007Assignee: E. I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
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Patent number: 7223777Abstract: The invention discloses a new clause of a five membered heterocylic ring compounds of general formula I and its pharmaceutically or cosmetically acceptable salts, wherein R1, R2, R3, R4, R5, A, B, X and Y are as defined in the specification. The invention also discloses a process for preparation of these compound and their therapeutic and cosmetic applications particularly in the management of aging related and diabetic vascular complications. The compounds in question act by triple action of an AGE (Advanced Glycation Endproducts) breaker, AGE inhibitor and free radical scavenger which make them most suitable in different therapeutic and cosmetic applications. The invention also discloses pharmaceuticals and cosmetic compositions comprising these compounds and method of treatment of diseases caused by accumulation of AGE and/or free radicals in the body cells.Type: GrantFiled: April 5, 2002Date of Patent: May 29, 2007Assignee: Torrent Pharmaceuticals Ltd.Inventor: Alangudi Sankaranarayanan
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Patent number: 7214678Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: June 1, 2006Date of Patent: May 8, 2007Assignee: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
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Patent number: 7199246Abstract: A process for the preparation of a compound of general formula (I), wherein R1 is CN or CSNH2; R2 is hydrogen or chloride; and R3 is halogen or haloalkyl or haloalkoxy or SF5 which process comprises reacting a compound of formula (II), where R1, R2 and R3 are as defined above; with a proton source.Type: GrantFiled: June 7, 2001Date of Patent: April 3, 2007Assignee: Merial LimitedInventor: Jean-François Rousseau
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Patent number: 7199138Abstract: This invention provides compounds of Formula I, N-oxides and salts thereof wherein A, B, R1 through R5, R7 through R9, X and Y 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. Also disclosed are compositions for controlling an invertebrate pest comprising the compounds of Formula I.Type: GrantFiled: August 13, 2002Date of Patent: April 3, 2007Assignee: E. I. du Pont de Nemours and CompanyInventors: Bruce Lawrence Finkelstein, George Philip Lahm, Stephen Frederick McCann, Thomas Paul Selby, Ying Song, Thomas Martin Stevenson
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Patent number: 7183296Abstract: The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV infection.Type: GrantFiled: January 27, 2004Date of Patent: February 27, 2007Assignee: Roche Palo Alto LLCInventors: Brian William Dymock, Philip Stephen Jones, John Herbert Merrett, Martin John Parratt
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Patent number: 7179823Abstract: A compound of formula (I) F wherein R1 represents a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; x represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: —CO—, —CS—, —CR4(OR5)— or —NR6— wherein each of R4 and R6 represents a hydrogen atom or a hydrocarbon group which may be stubstituted, R5 represents a hydrogen atom or a protective group for a hydroxyl group; m represents an integer of 0 to 3; Y represents an oxygen atom, a sulfur atom, or a group of the formula: —SO—, —SO2—, —NR7—, —CONR7— or —NR7CO— wherein R7 represents a hydrogen atom or a hydrocarbon group which may be substituted; ring A represents an aromatic ring which may further have 1 to 3 substituents; n represents an integer of 1 to 8; ring B represents a nitrogen-containing 5-membered hetero ring which may further be substituted by an alkyl group.Type: GrantFiled: November 9, 2000Date of Patent: February 20, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Yu Momose, Tsuyoshi Maekawa, Hiroyuki Odaka, Hiroyuki Kimura
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Patent number: 7179824Abstract: This invention pertains to a compound of Formula I, its N-oxide or an agriculturally suitable salt of the compound (Formula I) wherein R1, R2, R3, R4, and R5 are as defined in the disclosure.Type: GrantFiled: September 6, 2002Date of Patent: February 20, 2007Assignee: E. I. du Pont de Nemours and CompanyInventor: William Thomas Zimmerman
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Patent number: 7132435Abstract: This invention relates to nicotinamide derivatives of general formula (I): in which R1, X, Y, Z and R2 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.Type: GrantFiled: July 20, 2004Date of Patent: November 7, 2006Assignee: Pfizer Inc.Inventors: Mya Coral Helen Smith, Christine Anne Louise Watson