Chalcogen Bonded Directly To Ring Carbon Of Pyridine Or Partially Hydrogenated Pyridine Ring Patents (Class 546/261)
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Publication number: 20090018145Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreating carcinomas) and mesotheliomas.Type: ApplicationFiled: October 18, 2005Publication date: January 15, 2009Applicant: Compass Pharmaceuticals LLCInventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
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Publication number: 20080306108Abstract: Compounds with antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related disease, are described. The methods are directed to administering pharmaceutical compositions comprising a pyridoxine analogue.Type: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: MEDICURE INTERNATIONAL INC.Inventors: Wasimul Haque, James Diakur, Vinh Pham, Wenlian Zhang
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Publication number: 20080293684Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: July 26, 2005Publication date: November 27, 2008Inventors: Anthony B Pinkerton, Jean-Michel Vernier, Rowena V. Cube, John H. Hutchinson, Dehua Huang, Celine Bonnefous, Steven P. Govak, Theodore Kamenecka
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Publication number: 20080280904Abstract: Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.Type: ApplicationFiled: October 4, 2006Publication date: November 13, 2008Inventors: Anne Bettina Eldrup, Fariba Soleymanzadeh, Steven John Taylor
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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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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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Patent number: 7399735Abstract: Compounds formed of (per)fluoropolyether chains and end groups having a pyridine structure, with structural formula: T1-CW1—O—Rf—CW2-T2??(I) wherein T1, T2, equal to or different from each other, have the following meanings: F, CF3, C2F5, (C2F4)Cl; CH2—B—Y, CH(CF3)O—Y, wherein: B?O, S; wherein R1, R2, R3, R4, equal to or different from each other, are H, F, C1-C8 linear or branched perfluoroalkyl, NO2, CN; with the proviso that at least one of the two end groups T1, T2 is CH2—B—Y or CH(CF3)O—Y as above defined; W1, W2, equal to or different from each other, are —F, —CF3; Rf is a (per)fluoropolyoxyalkylene chain having a number average molecular weight from 400 to 10,000.Type: GrantFiled: May 20, 2004Date of Patent: July 15, 2008Assignee: Solvay Solexis S.p.A.Inventors: Antonio Russo, Patrizia Maccone
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Publication number: 20080139557Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: September 11, 2007Publication date: June 12, 2008Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Tony Lee, James W. Darrow, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt
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Publication number: 20080132706Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: ApplicationFiled: June 18, 2007Publication date: June 5, 2008Applicant: AVENTIS PHARMA LIMITEDInventors: Garry FENTON, Tahir Nadeem MAJID, Malcolm Norman PALFREYMAN
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Publication number: 20080114033Abstract: The invention is directed to pyridinone compounds useful for modulating Met kinase, having the following structure: and is further directed to pharmaceutical compositions comprising the compound; and methods for treating proliferative diseases, such as cancer by the administration of this compound.Type: ApplicationFiled: November 8, 2007Publication date: May 15, 2008Inventors: Robert M. Borzilleri, Gretchen M. Schroeder, Zhen-Wei Cai
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Patent number: 7358397Abstract: The present invention relates to halogenated 4-aminophenols and to halogenated 4-(phenyidiazenyl)phenols, to a process for their preparation and to the use of the halogenated 4-hydroxyphenols for preparing active ingredients, especially in pharmaceuticals and agrochemicals.Type: GrantFiled: September 3, 2004Date of Patent: April 15, 2008Assignee: LANXESS Deutschland GmbHInventors: Karen Peilstöcker, Albrecht Marhold, Jens-Peter Joschek
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Patent number: 7291580Abstract: 4-Aminopicolinic acids having (1,1-difluoroalkyl) substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: August 4, 2004Date of Patent: November 6, 2007Assignee: Dow AgroSciences LLCInventors: Terry William Balko, Stephen Craig Fields, Nicholas Martin Irvine, Christian Thomas Lowe, Paul Richard Schmitzer
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Patent number: 7288541Abstract: The present invention includes ketone derivatives (I) and (II), which are useful as cathepsin K inhibitors.Type: GrantFiled: October 2, 2002Date of Patent: October 30, 2007Assignee: SmithKline Beecham CorporationInventors: David Norman Deaton, John George Catalano
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Patent number: 7262209Abstract: The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.Type: GrantFiled: October 2, 2002Date of Patent: August 28, 2007Assignee: Novartis Animal Health US, Inc.Inventors: Thomas Goebel, Pierre Ducray
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Patent number: 7157580Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided hereinType: GrantFiled: October 18, 2004Date of Patent: January 2, 2007Assignee: Roche Palo Alto LLCInventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
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Patent number: 7074742Abstract: Compounds of Formula (I), their N-oxides and agriculturally suitable salts are disclosed which are useful as fungicides formula (I), (II) wherein A is a substituted pyridinyl ring; B is a substituted pyridinyl ring; W is C=L or SOn is O or S; R1 and R2 are each independently H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, each optionally substituted; R3 is H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl or C3-C8 dialkylaminocarbonyl; R4 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, each optionally substituted; X is O or S; and n is 1 or 2; provided that when W is C?O and R1, R2 and R3 are H; then B is other than 4-trifluoromethyl-3-pyridinyl, 2-chloro-4-pyridinyl and 2,6-dihalo-4-pyridinyl.Type: GrantFiled: September 17, 2001Date of Patent: July 11, 2006Assignee: E. I. du Pont de Nemours and CompanyInventors: Timothy Donald Neubert, David Walter Piotrowski, Michael Paul Walker
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Patent number: 7045631Abstract: Compounds of the formula (I) a process for preparing them, and their use as medicaments are described.Type: GrantFiled: July 3, 2002Date of Patent: May 16, 2006Assignee: Bayer AktiengesellschaftInventors: Ulrich Rosentreter, Thomas Kramer, Mitsuyuki Shimada, Walter Hubsch, Nicole Diedrichs, Thomas Krahn, Kerstin Henninger, Johannes-Peter Stasch
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Patent number: 6977266Abstract: It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): ? wherein R1 is a group represented by the formula: —Y1—Y2—Y3—Ra wherein Y1 is single bond or the like; Y2 is —C(?O)—NH— or the like; Y3 is optionally substituted aryl or the like; R2 is hydrogen or the like; R3 is alkyl or the like; R4 is alkyl or the like; R5 is optionally substituted alkyl or the like; or R3 and R4 taken together with the adjacent atom form cyclic group or the like.Type: GrantFiled: December 26, 2001Date of Patent: December 20, 2005Assignee: Shionogi & Co., Ltd.Inventors: Yukio Tada, Yasuyoshi Iso, Kohji Hanasaki
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Patent number: 6953798Abstract: Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra?)R??(1) Ar1 is an optionally substituted aromatic or heteroarotic group; L1 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of ?4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: November 29, 1999Date of Patent: October 11, 2005Assignee: Celltech R&D LimitedInventors: John Robert Porter, John Clifford Head, Graham John Warrellow, Sarah Catherine Archibald
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Patent number: 6927225Abstract: The present invention relates to compounds of Formula I: wherein: represents a 6-membered heterocyclic aromatic ring in which X1 is N, and X2, X3 and X4 are CR?; wherein R? is independently H, halogen, cyano, hydroxy, C1-C3 alkyl, C1-C3 haloalkyl, cyclopropyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-C3 alkylthio, aryl, C1-C3 NHC(O)alkyl, NHC(O)H, C1-C3 haloalkylthio, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl or nitro wherein adjacent R? substituents may form a ring; b) Z is O, S or NORz in which Rz is H or C1-C3 alkyl; and c) A represents (i) C2-C14 alkenyl, or C2-C14 alkynyl, all of which may be branched or unbranched, unsubstituted or substituted with halogen, hydroxy, nitro, aroyl, aryloxy, C1-C8 acyloxy, C1-C6 alkylthio, arylthio, aryl, heteroaryl, heteroarylthio, heteroaryloxy, C1-C6 acyl, C1-C6 haloalkyl, C1-C6 alkoxy or C1-C6 haloalkoxy, and (ii) C3-C14 cycloalkyl, containing 0 heteroatoms and 0-2 unsaturations, substituted with aryloxy, heteroaryloxy, C1-C6 alkylthio, aType: GrantFiled: December 2, 2002Date of Patent: August 9, 2005Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, Richard B. Rogers, William H. Dent, III, Chenglin Yao, Bassam S. Nader, Gina M. Fitzpatrick, Noormohamed M. Niyaz, Robert P. Gajewski, John L. Miesel, Kevin G. Meyer, Irene M. Morrison
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Patent number: 6908923Abstract: Certain substituted benzamide derivatives of Formula I: selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: December 20, 2002Date of Patent: June 21, 2005Assignee: Cytokinetics, Inc.Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
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Patent number: 6906195Abstract: The present invention relates to pyridone dyes of formula (1), wherein R is a radical —(CR?H)n—W, R? is hydrogen, C1-C2alkyl or phenyl, Y is cyano, —CONH2 or —CH2SO3H, W is hydrogen, a radical —NR1R2 or a radical —OR3, R1 and R2 are each independently of the other hydrogen, unsubstituted or hydroxy- or phenyl-substituted C1-C6-alkyl, it being possible for the alkyl chain from C3 upwards to be interrupted by one or more oxygen atoms, or a radical of formula (3), (4) or (5), or R1 and R2 together with the nitrogen atom in —NR1R2 form a heterocyclic ring, R3 is hydrogen, unsubstituted or hydroxy-substituted C1-C6alkyl, phenyl or a radical of formula (6), R4 is alkyl or aryl, R5 and R6 are each independently of the other alkyl, aryl or heteroaryl, n is an integer from 2 to 6, and m is an integer from 1 to 6, a process for the preparation thereof and their use in the production of coloured plastics or polymeric colour particlesType: GrantFiled: April 30, 2002Date of Patent: June 14, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Athanassios Tzikas, Urs Lauk, Romeo Dreier, Antoine Clément
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Patent number: 6893650Abstract: The invention provides fungicidal compounds of formula (I) and salts thereof wherein: R1 is alkyl, alkenyl, alkynyl, carbocyclyl or heterocyclyl, each of which may be substituted, or hydrogen; R2 and R3, which may be the same or different, are any group defined for R1; cyano; acyl; —ORa or —SRa, where Ra is alkyl, alkenyl, alkynyl, carbocyclyl or heterocyclyl, each of which may be substituted; or R2 and R3, or R2 and R1, together with their interconnecting atoms may form a ring, which may be substituted; R4 is alkyl, alkenyl, alkynyl, carbocyclyl or heterocyclyl, each of which may be substituted; hydroxy; mercapto; azido; nitro; halogen; cyano; acyl; optionally substituted amino; cyanato; thiocyanato; —SF5; —ORa; —SRa or —Si(Ra)3; m is 0 to 3; when present R5, which may be the same or different to any other R5, is any group defined for R4; R6 is optionally substituted carbo- or heterocylclyl; and A is a defined linking group, or —A—R6 and R5 together with benzene ring M form an optionally substituted fused riType: GrantFiled: February 4, 2000Date of Patent: May 17, 2005Assignee: Bayer Cropscience GmbHInventors: Mark David Charles, Wilfried Franke, David Eric Green, Thomas Lawley Hough, Dale Robert Mitchell, Donald James Simpson, John Frederick Atherall
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Patent number: 6881846Abstract: This invention relates to certain dioxodihydropyridine derivatives and certain methacrylic acid and furan derivative precursors thereof, processes for their preparation, pharmaceutical compositions containing such compounds and their use as anti-proliferative agents, especially tumour growth inhibitors and anti-cancer agents, antibiotics and/or antiviral agents.Type: GrantFiled: September 15, 2003Date of Patent: April 19, 2005Assignee: EPX Research LimitedInventors: Washington Odur Ayuko, Michael John Tisdale, Eric Lattmann
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Patent number: 6881736Abstract: Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: wherein R1 is Het or Ar R2 is or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 7, 2000Date of Patent: April 19, 2005Assignee: SmithKline Beecham CorporationInventors: Peter J. Manley, William H. Miller, Irene N. Uzinskas
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Patent number: 6872690Abstract: The invention relates method of combating undesired plant growth at a locus, comprising application to the locus of an effective amount of at least one compound of formula (I): wherein R1, R3, A, X, Z and m have the meaning given in claim 1, and the agronomically acceptable salts or N-oxides thereof, and to novel compounds of formula I as well as to herbicidal compositions containing such compounds as active ingredients.Type: GrantFiled: March 1, 2002Date of Patent: March 29, 2005Assignee: WYETHInventor: Thomas Maier
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Patent number: 6844295Abstract: The present invention relates to benzoxazole compounds represented by the following formula (I): wherein R1 to R4 may be the same or different from each other, and each represent a hydrogen atom, alkyl group having 1 to 6 carbon atoms, alkoxy group having 1 to 4 carbon atoms, haloalkyl group having 1 to 4 carbon atoms, haloalkoxy group having 1 to 4 carbon atoms, halogen atom, nitro group, cyano group, R12S(O)n, alkoxycarbonyl group having 1 to 4 carbon atoms, amino group, —NHCOR11 or carbonyl group, where R11 and R12 each represent an alkyl group having 1 to 6 carbon atoms, and n is an integer of 0 to 2, A represents a single bond, CHR5—Y, CR5?CR6, CR5R7—CHR6 or CHR5, where R5 represents a hydrogen atom, hydroxyl group, halogen atom or alkyl group, R6 and R7 each represent a hydrogen atom, hydroxyl group, alkyl group, halogen atom or substituted sulfonyloxy group, Y represents O, S or NH, and W represents a substituted or unsubstituted benzene ring or hetero ring, and processes for preparing the same.Type: GrantFiled: July 4, 2001Date of Patent: January 18, 2005Assignee: Ube Industries, Ltd.Inventors: Shohei Fukuda, Akira Nakamura, Motohisa Shimizu, Tatsuo Okada, Satoshi Oohida, Takehiko Asahara
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Patent number: 6833378Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.Type: GrantFiled: January 17, 2001Date of Patent: December 21, 2004Assignee: Pfizer IncInventor: Yuhpyng L. Chen
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Publication number: 20040254378Abstract: The present invention relates to a novel bipyridinyl derivative having a structure of formula (1) and its pharmaceutically acceptable salts, optical isomer and method for preparing it as a highly selective cyclooxygenase-2 inhibitor, wherein R is defined in this specification.Type: ApplicationFiled: May 4, 2004Publication date: December 16, 2004Inventors: II-Hwan Cho, Jee-Woong Lim, Ji-Young Noh, Jong-Hoon Kim, Sang-Wook Park, Hyung-Chul Ryu, Je-Hak Kim, Jong-Ho Kim, So-Young Wang, Dal-Hyun Kim
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Patent number: 6825204Abstract: N-substituted 3-hydroxy-4-pyridinones and metal chelates, methods of preparing N-substituted 3-hydroxy-4-pyridinones and metal chelates, and pharmaceutical compositions containing new N-substituted 3-hydroxy-4-pyridinones and/or their metal chelates. Use of N-substituted 3-hydroxy-4-pyridinones and their metal chelates as pharmaceutical agents for the treatment of diseases, such as parasitic and viral infections, conditions associated with inflammation and infection, and conditions mediated by cell-proliferation or collagen formation.Type: GrantFiled: February 5, 2003Date of Patent: November 30, 2004Assignee: Bristol-Myers Squibb CompanyInventor: Shuang Liu
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Publication number: 20040235685Abstract: Compounds formed of (per)fluoropolyether chains and end groups having a pyridine structure, with structural formula:Type: ApplicationFiled: May 20, 2004Publication date: November 25, 2004Applicant: SOLVAY SOLEXIS S.p.A.Inventors: Antonio Russo, Patrizia Maccone
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Publication number: 20040209917Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) 1Type: ApplicationFiled: March 12, 2004Publication date: October 21, 2004Inventors: Richard A. Hartz, Argyrios G. Arvanitis
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Patent number: 6794336Abstract: The present invention relates to a compound of the formula (I) or salt thereof in which R1 is identical or different at each occurrence and is H, halogen, CN, nitro, SF5, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C1-C8)alkoxy, [(C1-C8)alkyl]-carbonyl or (C1-C8)alkylsulfonyl, each of the radicals being unsubstituted or substituted, or is S(O)p—R7, where p=0, 1 or 2 and R7 is (C1-C8)alkyl, (C1-C8)haloalkyl or NR8R9, where R8 and R9 independently of one another are identical or different and are H, (C1-C8)alkyl, (C2-C8)alkenyl, (C7-C10)arylalkyl, (C7-C10)alkylaryl or (C6-C10)aryl, each of the last-mentioned five radicals being unsubstituted or substituted, or is a group of the formula where R10 is (C1-C8)alkyl which is unsubstituted or substituted, and W=O or S, A is optionally substituted aryl or an optionally substituted heterocyclic radical, X is O or S, R2,R3,R4, and R5 are identical or different and are H, halType: GrantFiled: June 21, 2002Date of Patent: September 21, 2004Assignee: Aventis Crop Science GmbHInventors: Klaus Haaf, Lothar Willms, Thomas Auler, Hubert Menne, Hermann Bieringer
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Patent number: 6794398Abstract: The invention provides an agent for the prophylaxis and treatment of liver disease and an activation inhibitor of hepatic stellate cells, which contains a compound having a Rho kinase inhibitory activity. The compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)cyclohexane, is useful for the prophylaxis and treatment of liver diseases, such as hepatitis, hepatic fibrosis, hepatic cirrhosis, hepatic cancer and the like, because it has various actions, such as a superior inhibitory action on the activation of hepatic stellate cell, suppressive action on hepatic fibrogenesis in liver tissues and the like.Type: GrantFiled: March 6, 2002Date of Patent: September 21, 2004Assignee: Mitsubishi Pharma CorporationInventors: Makoto Nakamuta, Hajime Nawata, Masayoshi Uehata
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Publication number: 20040176605Abstract: The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.Type: ApplicationFiled: October 10, 2003Publication date: September 9, 2004Applicant: Klinge Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Loser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
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Patent number: 6780874Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in, which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.Type: GrantFiled: June 10, 2003Date of Patent: August 24, 2004Assignee: Celltech R & D LimitedInventors: Timothy John Norman, John Robert Porter, Brian Woodside Hutchinson, Andrew James Ratcliffe, John Clifford Head, Rikki Peter Alexander, Barry John Langham, Graham John Warrellow, Sarah Catherine Archibald, Janeen Marsha Linsley
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Patent number: 6765096Abstract: There are provided a compound represented by the formula (I): wherein X and X′ are —N(COOCR3R2OCOR1)—, —O— or the like, R1 is alkyl substituted with carbamoyl, lower alkylcarbamoyl, carbamoyloxy, lower alkylcarbamoyloxy, acetylamino or the like, R2 and R3 are hydrogen or the like, Y and Y′ are lower alkyl, lower alkenyl or the like, ring A, ring B and ring C are optionally substituted aromatic carbocycle or optionally substituted heterocycle, W1, W2 and/or W3 are a bond or the like, and V1 and V2 are a single bond or the like, or a pharmaceutically acceptable salt or a solvate thereof, as well as a pharmaceutical composition containing the present compound.Type: GrantFiled: December 3, 2001Date of Patent: July 20, 2004Assignee: Shionogi & Co., Ltd.Inventors: Katsutoshi Aono, Teruhisa Ichinashi, Akira Kugimiya
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Publication number: 20040097729Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as herbicides.Type: ApplicationFiled: December 6, 2002Publication date: May 20, 2004Inventors: Andrew Edmunds, Alain De Mesmaeker, Christoph Luthy, Jurgen Schaetzer
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Publication number: 20040067955Abstract: A pyridazinone or pyridone compound of the following formula (I).Type: ApplicationFiled: September 3, 2003Publication date: April 8, 2004Applicant: Fujisawa Pharmaceutical Co. Ltd.Inventors: Seiichiro Tabuchi, Hideo Tsutumi, Atsushi Akahane, Yoshinari Sato
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Patent number: 6683186Abstract: A compound of the formula (I) wherein A is O, S, CHR1 or NR2, R1 and R2 are H, lower alkyl, X1 and X2 are H, halogen, nitro, cyano, etc., Y1 is H, lower alkyl, Z1 and Z2 are H, halogen, cyano, hydroxy, lower alkyl, etc., and n is an integer of 2 to 4, a pharmaceutically acceptable salt thereof, a process for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and an intermediate therefor. The compounds (I) of the present invention show a potent PDE IV inhibitory activity as well as an excellent bronchodilating activity, and hence, they are widely useful as a PDE IV inhibitor in the treatment or prophylaxis of allergic inflammatory diseases or organ inflammatory diseases, especially in the treatment or prophylaxis of pulmonary diseases accompanied by airway obstruction such as asthma.Type: GrantFiled: March 10, 2003Date of Patent: January 27, 2004Assignee: Dainippon Pharmaceutical Company, LimitedInventors: Motoji Kawasaki, Tomohiro Nigo
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Patent number: 6673745Abstract: The invention relates to novel compounds of formula I: wherein R, A, B and X have the meaning given in claim 1; and the agronomically acceptable salts or N-oxides thereof, and to herbicidal compositions containing such compounds as active ingredients.Type: GrantFiled: January 12, 2001Date of Patent: January 6, 2004Assignee: BASF AktiengesellschaftInventors: Thomas Maier, Stefan Scheiblich, Helmut S. Baltruschat
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Patent number: 6670380Abstract: Compounds are provided having the formula: wherein A, Q, and X are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such compounds alone or in combination with other antidiabetic agents such as metformin, glyburide, troglitazone and/or insulin.Type: GrantFiled: November 20, 2001Date of Patent: December 30, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Richard Sulsky, Jeffrey A. Robl
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Publication number: 20030222243Abstract: Fluorinated indenes and 1,7-dihydroindacenes of the general formulae (I) and (II) of negative dielectric anisotropy (&Dgr;&egr;<0) 1Type: ApplicationFiled: April 4, 2003Publication date: December 4, 2003Applicant: Merck Patent GmbHInventors: Lars Lietzau, Melanie Klasen-Memmer, Matthias Bremer
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Patent number: 6656958Abstract: The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.Type: GrantFiled: February 1, 2001Date of Patent: December 2, 2003Assignee: Abbott LaboratoriesInventors: Nan-Horng Lin, Liming Dong
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Publication number: 20030216257Abstract: The use of 1-aryl-4-haloalkyl-2-[1H]-pyridones of the formula I 1Type: ApplicationFiled: January 14, 2003Publication date: November 20, 2003Inventors: Ingo Sagasser, Olaf Menke, Gerhard Hamprecht, Michael Puhl, Robert Reinhard, Matthias Witschel, Cyrill Zagar, Helmut Walter
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Publication number: 20030199554Abstract: A compound of the formula (I) 1Type: ApplicationFiled: March 10, 2003Publication date: October 23, 2003Inventors: Motoji Kawasaki, Tomohiro Nigo
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Publication number: 20030195232Abstract: A compound of the formula (I) 1Type: ApplicationFiled: March 10, 2003Publication date: October 16, 2003Inventors: Motoji Kawasaki, Tomohiro Nigo
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Publication number: 20030191317Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: ApplicationFiled: December 1, 2000Publication date: October 9, 2003Applicant: G. D. Searle & Co.,Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo, Clara I. Villamil
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Publication number: 20030186989Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of Formula (1.0.Type: ApplicationFiled: July 24, 2002Publication date: October 2, 2003Inventors: Anthony Marfat, Robert James Chambers
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Publication number: 20030181420Abstract: Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of nuclear receptors, including liver X receptor (LXR) and orphan nuclear receptors. In certain embodiments, the compounds are N-substituted pyridones.Type: ApplicationFiled: December 20, 2002Publication date: September 25, 2003Inventors: Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Ronald C. Griffith