Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/298)
  • Publication number: 20080135803
    Abstract: The invention relates to a high dielectric anisotropy liquid crystal compound which is a pyridyl derivative with substituents of electrons push-pull effect. Furthermore, the high dielectric anisotropy liquid crystal compounds are colorless and have high thermal and photo stability as well as high compatibility in a liquid crystal host. A liquid crystal composition containing the high dielectric anisotropy liquid crystal compound can reduce threshold voltage of cholesteric reflective displays, thus saving power and extending lifetime of driver ICs.
    Type: Application
    Filed: December 3, 2007
    Publication date: June 12, 2008
    Inventors: Kung-Lung Cheng, Shib-Hsien Liu, Ann-Cheng Chen, Peu-Jane Haung, Chih-Lung Chin
  • Patent number: 7368479
    Abstract: The invention relates to ?-sulfonylamino-acetonitrile derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein Ar1, and Ar2 independently of each other stand for an optionally substituted aryl or heteroaryl group, R1, and R2 stand independently of each other for hydrogen, optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R3 designates hydrogen, C3-C5alkenyl, C3-C5alkynyl or optionally substituted C1,-C5alkyl; R4 is optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R5 and R6 are independently of each other hydrogen or optionally substituted C1-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R7, and R8 are independently of each other hydrogen or optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally su
    Type: Grant
    Filed: June 18, 2003
    Date of Patent: May 6, 2008
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Martin Eberle, Daniel Stierli, Urs Müller
  • Patent number: 7361654
    Abstract: The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory- and immune-associated diseases, and have the structure including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein X is selected from N, O, and S; Y is N or CR6; Z is a ring; and where R, Ra, Rb, Rc, Rd, R1, R2, R3, R4, and R5 are as defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising such compounds.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: April 22, 2008
    Assignee: Bristol-Myers Squibb Co.
    Inventors: James Sheppeck, T. G. Murali Dhar, Lidia Doweyko, John Gilmore, David Weinstein, Hai-Yun Xiao, Bingwei V. Yang, Arthur M. Doweyko
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 7317016
    Abstract: This invention relates to methods of treatment of cardiovascular disorders, thromboembolic disorders, inflammation, and disorders of the central nervous system using pyrazol pyridine derivatives of formula (I) wherein R1 is a radical of the formula —O—SO2—R3 in which R3 is optionally substituted C1-6-alkyl, optionally substituted C3-8-cycloalkyl, or optionally substituted phenyl; R2 is H, optionally substituted C1-6-alkyl-CO— or optionally substituted C1-6-alkyl-SO2—; as well as salts, stereoisomers, tautomers, and hydrates thereof.
    Type: Grant
    Filed: July 5, 2005
    Date of Patent: January 8, 2008
    Assignee: Bayer Aktiengesellschaft
    Inventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elisabeth Perzborn
  • Patent number: 7291622
    Abstract: This invention relates to methods for treating sexual dysfunction, by administering a compound of the formula wherein R1 is H or a di-C1-6-alkylaminocarbonyl radical, and R2 is a radical of the formula —O—C(X)—NR3R4 wherein X is O or S. The compound may also be administered in combination with at least one organic nitrate or NO donor, or in combination with at least one compound which inhibits the breakdown of cyclic guanosine monophosphate (cGMP).
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: November 6, 2007
    Assignee: Bayer Aktiengesellschaft
    Inventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elizabeth Perzborn
  • Patent number: 7268145
    Abstract: The present invention is a thiobenzimidazole derivative represented by the following formula (1) or a medically acceptable salt thereof wherein said thiobenzimidazole derivative and a medically acceptable salt thereof have a potent activity of inhibiting human chymase. Thus, they are potential preventive and/or therapeutic agents clinically applicable to various diseases in which human chymase is involved.
    Type: Grant
    Filed: October 14, 2004
    Date of Patent: September 11, 2007
    Assignee: Teijin Pharma Limited
    Inventors: Yoshiyuki Matsumoto, Susumu Takeuchi, Naoki Hase
  • Patent number: 7244737
    Abstract: The present invention relates to a compound of the general formula: wherein R1 is a 4-pyrimidinyl ring substituted at the 6-position by halo, hydroxy, 2-cyanophenoxy, 2,6-difluorophenoxy, 2-nitrophenoxy or 2-thiocarboxamidophenoxy and wherein R2 is any group which can be transesterified to form a methyl ester. The present invention is also directed to a process of preparing said compound.
    Type: Grant
    Filed: June 20, 2006
    Date of Patent: July 17, 2007
    Assignee: Syngenta Limited
    Inventors: David Anthony Jackson, James Peter Muxworthy, Mark Robert Sykes
  • Patent number: 7232926
    Abstract: The present invention relates to a process for preparing sulfamoyl halides of primary or secondary amines, comprising the following steps: i) reacting a primary or secondary amine A1 with at least equimolar amounts of SO3 or an SO3 source in the presence of at least equimolar amounts of a tertiary amine A2, based in each case on the amine A1, and ii) reacting the reaction mixture obtained in step i) with at least the amount of a phosphorus halide required by the stoichiometry; The invention further relates to a process for preparing sulfonic diamides, comprising the preparation of sulfamoyl halides by means of carrying out steps i) and ii) and subsequently reacting the sulfamoyl halide obtained with ammonia. The invention further relates to the use of this process for preparing active herbicidal ingredients having a sulfuric diamide structure. The invention further relates to novel sulfamoyl chlorides.
    Type: Grant
    Filed: May 15, 2003
    Date of Patent: June 19, 2007
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Hamprecht, Michael Puhl, Robert Reinhard, Ingo Sagasser, Thomas Schmidt, Norbert Götz, Thomas Zierke
  • Patent number: 7230026
    Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
    Type: Grant
    Filed: February 8, 2006
    Date of Patent: June 12, 2007
    Assignee: Cephalon, Inc.
    Inventors: Diane E. Gingrich, Robert L. Hudkins
  • Patent number: 7205328
    Abstract: The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.
    Type: Grant
    Filed: October 21, 2003
    Date of Patent: April 17, 2007
    Assignee: IRM LLC
    Inventors: Yun He, Tao Jiang, Kelli L. Kuhen, David Archer Ellis, Baogen Wu, Tom Yao-Hsiang Wu, Badry Bursulaya
  • Patent number: 7205302
    Abstract: The present invention provides a compound which is useful as a PGI2 receptor agonist, and a pharmaceutical composition. The present invention is directed to a pharmaceutical composition comprising a compound represented by the following formula [1]: (R1 and R2 are the same or different and each represents optionally substituted aryl, Y represents N or CH, Z represents N or CH, A represents NH, NR5, O, S, or ethylene, R5 represents alkyl, D represents alkylene or alkenylene, E represents phenylene or single bond, G represents O, S, or CH2, R3 and R4 are the same or different and each represents hydrogen or alkyl, Q represents carboxy, alkoxycarbonyl, tetrazolyl, carbamoyl, or N-(alkylsulfonyl)carbamoyl), or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: April 25, 2002
    Date of Patent: April 17, 2007
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Tetsuo Asaki, Taisuke Hamamoto, Keiichi Kuwano
  • Patent number: 7195719
    Abstract: The invention relates to chiral nonracemic liquid crystal compounds having achiral tails comprising a perfluoroalkyl terminal portion which are useful as components in liquid crystal to impart high polarization to the mixture. The materials of this invention can be combined with known liquid crystal host materials to impart improved properties. Chiral nonracemic compounds of this invention can function as additives or dopants in host materials to impart chirality into an LC material.
    Type: Grant
    Filed: January 3, 2002
    Date of Patent: March 27, 2007
    Assignee: Displaytech, Inc.
    Inventors: Michael Wand, Xin Hua Chen, William N. Thurmes
  • Patent number: 7196089
    Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.
    Type: Grant
    Filed: January 29, 2004
    Date of Patent: March 27, 2007
    Assignee: Asterand UK Limited
    Inventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
  • Patent number: 7186732
    Abstract: Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
    Type: Grant
    Filed: August 6, 2001
    Date of Patent: March 6, 2007
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Richard Apodaca, Nicholas I. Carruthers, Curt A. Dvorak, Dale A. Rudolph, Chandravadan R. Shah, Wei Xiao
  • Patent number: 7176199
    Abstract: An aryl-substituted alicyclic compound of the formula (I): wherein U is 1,4,5,6-tetrahydropyrimidin-2-yl, etc., A is phenylene, etc., B is piperidine-1,4-diyl, etc., Z is —CONH—, etc., R3 is hydrogen, etc., R5 is hydrogen, aryl, etc., R6 is a mono-substituted amino (e,g., benzyloxycarbonylamino), R7 is hydrogen, etc., and a process for preparation thereof, and a pharmaceutical composition containing the same. The compound of the present invention has a high selectivity for ?v?3 integrin, and exhibits a potent inhibitory activity thereto, and hence, it is useful as a preventive or/and a therapeutic agent for a disease in which ?v?3 integrin is involved.
    Type: Grant
    Filed: March 14, 2002
    Date of Patent: February 13, 2007
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Toshiya Morie, Seiji Iwama, Mitsue Notake, Tomoko Kitano
  • Patent number: 7169325
    Abstract: To provide a liquid crystalline compound capable of exhibiting a biaxial liquid crystal phase, provide a trifunctional or greater functional polymerizable liquid crystalline compound having polymerizable groups, and also to provide a liquid crystalline composition and a retardation film which are using the liquid crystalline compound, a compound and a liquid crystalline compound each are represented by formula (I) defined in the specification; a liquid crystalline composition contains the compound; and a retardation film has an optically anisotropic layer formed from the compound.
    Type: Grant
    Filed: July 16, 2004
    Date of Patent: January 30, 2007
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hideyuki Nishikawa, Atsuhiro Ohkawa
  • Patent number: 7135569
    Abstract: The present invention relates to a process for preparing pyridinyl and pyrimidinyl mono-fluorinated beta keto esters of formula (I): wherein: R1 represents a pyridine ring or a pyrimidine ring, the rings being optionally substituted by a C3-6 cycloalkyl group, a C1-4 alkyl group, a C1-4 alkoxy group, a benzyl group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group or ahalogenatom; and R3 represents a C1-6 alkyl group; by reacting with fluorine a compound of formula (II) wherein R1, R2 and R3 have the same meaning as defined above.
    Type: Grant
    Filed: September 7, 2005
    Date of Patent: November 14, 2006
    Assignee: Sanof I-Aventis
    Inventor: Jonathan Frost
  • Patent number: 7125881
    Abstract: The present invention therefore provides use of a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S.
    Type: Grant
    Filed: June 23, 2003
    Date of Patent: October 24, 2006
    Assignee: AstraZeneca AB
    Inventors: Andrew Bailey, Garry Pairaudeau, Anil Patel, Stephen Thom
  • Patent number: 7115613
    Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
    Type: Grant
    Filed: March 26, 2003
    Date of Patent: October 3, 2006
    Assignee: Cephalon, Inc.
    Inventors: Diane E. Gingrich, Robert L. Hudkins
  • Patent number: 7112585
    Abstract: 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”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.
    Type: Grant
    Filed: March 12, 2004
    Date of Patent: September 26, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard A. Hartz, Argyrios G. Arvanitis
  • Patent number: 7112674
    Abstract: The invention relates to an organic electroluminescent device which contains 2,5-diaminoterephthalic acid derivatives of formula 1a as emitter substances in one or several emitter layers in a pure or doped manner. The ring A is a triple unsaturated benzene ring wherein R4? and R8? are zero or ring A is a double unsaturated ring respectively provided with a double bond in the 1,2 position and 4,5 position, and wherein R10 is a nitrile radical —CN or a radical C(?X1)—X2R1, R11 is a nitrile radical —CN or a radical —C(?X3)—X4R5, X1 and X3 are oxygen, sulfur or imino, X2 and X4 are oxygen, sulfur or optionally substituted amino, R1–R8, R4? and R8? are H, C1–20-alkyl, aryl, heteroaryl, R4 and R8 can be halogen, nitro, cyanogen or amino, R2–R4, R6–R8, R4? and R8? can be trifluoromethyl or pentafluorophenyl, and wherein certain radicals can form a saturated or unsaturated ring.
    Type: Grant
    Filed: August 21, 2002
    Date of Patent: September 26, 2006
    Assignee: Sensient Imaging Technologies GmbH
    Inventors: Andreas Richter, Jens Schoenewerk, Gerhard Diener
  • Patent number: 7109148
    Abstract: A stem/leaf desiccant for crop plants which comprises as an active ingredient, a compound of formula (I): wherein X represent CH or nitrogen; Z represents halogen; A represents oxygen, sulfur, or NH; R1 represents hydroxyl, C1–C7 alkoxy, C3–C7 alkenyloxy, C3–C7 alkynyloxy, C5–C7 cycloalkoxy, {(C1–C7 alkoxy)carbonyl} C1–C3 alkoxy, (C1–C7 alkylamino)oxy, {di(C1–C7 alkyl)amino}oxy, (C3–C7 alkylideneamino)oxy, C1–C7 alkylamino, di(C1–C7 alkyl)amino, C3–C7 alkenylamino, C3–C7 alkynylamino, C5–C7 cycloalkylamino, {(C1–C7 alkoxy)carbonyl} C1–C3 alkylamino, or (C1–C7 alkoxy)amino; R2 is hydrogen or methyl; and R3 is hydrogen, halogen, C1–C3 alkyl, or C1–C3 alkoxy; a method for desiccating a crop plant and a method for harvesting a crop by using the stem/leaf desiccant.
    Type: Grant
    Filed: May 31, 2001
    Date of Patent: September 19, 2006
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Nobuaki Mito
  • Patent number: 7105523
    Abstract: This invention relates to compounds of the formula wherein R1 is H or a di-C1-6-alkylaminocarbonyl raical, and R2 is a radical of the formula —O—C(X)—NR3R4 wherein X is O or S. A process for preparing such compounds, pharmaceutical compositions containing them, and methods for using them in treatment of hypertension are also disclosed and claimed.
    Type: Grant
    Filed: November 9, 2001
    Date of Patent: September 12, 2006
    Assignee: Bayer Aktiengeselischaft
    Inventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elisabeth Perzborn
  • Patent number: 7087768
    Abstract: The disclosure relates to a fumagillol compound which can be usefully used not only as an angiogenesis inhibiting agent showing a superior angeogenesis inhibitory effect with less toxicity, but also as a cancer metastasis inhibitor and a therapeutic agent against cancer and other various inflammatory diseases such as rheumatic disease, psoriasis, etc., and diabetic retinopathy related to angeogeneois, and also a method for preparing the same.
    Type: Grant
    Filed: June 11, 2002
    Date of Patent: August 8, 2006
    Assignee: Equispharm Co., Ltd.
    Inventors: Cheol-Kyu Han, Jeong-Hyeok Yoon, Seung-Moak Kim, Nam-Doo Kim, Byung-Ha Chang, Jee-Young Lee, Tae-Bo Sim
  • Patent number: 7067664
    Abstract: 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: Grant
    Filed: May 30, 2000
    Date of Patent: June 27, 2006
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventor: Yuhpyng L. Chen
  • Patent number: 7037880
    Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: May 2, 2006
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
  • Patent number: 7026270
    Abstract: This invention concerns new biocidal compounds of formula (I) wherein R is H or CH3. Of particular interest are two isomers that are named malayamycin A and desmethylmalayamycin A. These isomers, which may be prepared by growing under controlled conditions a previously unknown strain of micro-organism from the species Streptomyces malaysiensis, are characterised by nmr and mass spectroscopic data. They have biocidal activity, including anti-fungal, anti-viral and anti-cancer activity, and are of special interest for use in agriculture, horticulture, animal and human health.
    Type: Grant
    Filed: January 10, 2003
    Date of Patent: April 11, 2006
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Jill Patricia Benner, Bettina Gertrud Henriette Boehlendorf, Martin Richard Kipps, Nicolas Eugene Paul Lambert, Riet Luck, Louis-Pierre Molleyres, Snezana Neff, Traugott Christoph Schuez, Paul David Stanley
  • Patent number: 6936597
    Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.
    Type: Grant
    Filed: March 21, 2002
    Date of Patent: August 30, 2005
    Assignee: Enzon, Inc.
    Inventors: Richard B. Greenwald, Yun H. Choe
  • Patent number: 6930208
    Abstract: What is described are derivatives of benzoylcyclohexanediones of the formula (I) and their use as herbicides. In this formula (I), R1a, R1b, R1c, R2, R3, R4 and R5 denote various radicals, X1 is a bridging atom, X2 is a carbon chain and X3 is a chalcogen atom or an oximino radical.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: August 16, 2005
    Assignee: Bayer CropScience GmbH
    Inventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Monika H. Schmitt, Thomas Auler, Hermann Bieringer, Hubert Menne
  • Patent number: 6924251
    Abstract: The invention relates to novel substituted benzoylcyclohexanediones of the general formula (I), in which m, n, A, R1, R2, R3, R4 and Z are each as defined in the description, and also to processes for their preparation and to their use as herbicides.
    Type: Grant
    Filed: July 13, 1999
    Date of Patent: August 2, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Georg Schwarz, Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky, Heinz-Jürgen Wroblowsky
  • Patent number: 6921767
    Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: July 26, 2005
    Assignee: Pharmacia Corporation
    Inventors: Nagarajan R. Srinivasan, Ish Kumar Khanna, Michael Clare, Alan Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu, Yu Yi, Renee M. Huff, Bipinchandra N. Desai, Balekudru Devadas, Mihir D. Parikh, Thomas Penning
  • Patent number: 6919345
    Abstract: This invention relates to pyrazol pyridine derivatives of formula (I) wherein R1 is a radical of the formula ?O—SO2—R3 in which R3 is optionally substituted C1—6—alkyl, optionally substituted C3—8—cycloalkyl, or optionally substituted phenyl; R2 is H, optionally substituted C1—6—alkyl —CO—or optionally substituted C1—6—alkyl—SO2— ; as well as salts, stereoisomers, tautomers, and hydrates thereof. Pharmaceutical compositions containing these materials and methods of using them in medical treatment are also described and claimed.
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: July 19, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elisabeth Perzborn
  • Patent number: 6916820
    Abstract: The present invention relates to a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral nervous systems.
    Type: Grant
    Filed: April 6, 2000
    Date of Patent: July 12, 2005
    Assignee: Krenitsky Pharmaceuticals, Inc.
    Inventors: James L. Kelley, Thomas A. Krenitsky, Lilia M. Beauchamp
  • Patent number: 6906051
    Abstract: The present invention relates to a class of compounds represented by the Formula I: or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?V?3 and/or the ?V?5 integrin.
    Type: Grant
    Filed: November 19, 2003
    Date of Patent: June 14, 2005
    Assignee: Pharmacia Corporation
    Inventors: Peter Ruminiski, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Thomas Rogers, Jennifer VanCamp, Chester Yuan
  • Patent number: 6884804
    Abstract: The present invention provides compounds of formula I: wherein A is N or CR, and G, R1, R2 and R3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of Src mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: May 16, 2002
    Date of Patent: April 26, 2005
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: Young Choon-Moon
  • Patent number: 6867210
    Abstract: This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3, R1-R4, X and Y are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: March 15, 2005
    Assignee: Euro-Celtique S.A.
    Inventors: Derk J. Hogenkamp, Phong Nguyen, Bin Shao
  • Patent number: 6867298
    Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.
    Type: Grant
    Filed: May 8, 2003
    Date of Patent: March 15, 2005
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Wolter, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
  • Patent number: 6864368
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: March 8, 2005
    Assignees: Berlax Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6864263
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: March 8, 2005
    Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6864252
    Abstract: The present invention relates to hydrazinyl and nitrogen oxide pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, X, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.
    Type: Grant
    Filed: November 1, 2002
    Date of Patent: March 8, 2005
    Assignee: Pfizer, Inc.
    Inventors: Subas M. Sakya, Bryson Rast
  • Patent number: 6844351
    Abstract: 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: Grant
    Filed: May 31, 2000
    Date of Patent: January 18, 2005
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng L. Chen
  • Patent number: 6844295
    Abstract: 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: Grant
    Filed: July 4, 2001
    Date of Patent: January 18, 2005
    Assignee: Ube Industries, Ltd.
    Inventors: Shohei Fukuda, Akira Nakamura, Motohisa Shimizu, Tatsuo Okada, Satoshi Oohida, Takehiko Asahara
  • Patent number: 6835216
    Abstract: Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E and C), many of which are more reactive toward peroxyl radicals than the most potent form of Vitamin E. These compounds may exhibit many chemopreventive effects associated with conditions in which free radical-mediated cellular damage or disruption is implicated and Vitamins E and C are shown to have protective effects. Additionally, these compounds should be excellent oxidation inhibitors as additives to fuels, lubricants, rubber, polymers, chemicals, solvents and foodstuffs.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: December 28, 2004
    Assignee: Vanderbilt University
    Inventors: Derek A. Pratt, Luca Valgimigli, Gino A. DiLabio
  • Patent number: 6831081
    Abstract: The present invention provides a compound of formula as described herein, which are useful as antiviral agents, in particular, as agents against viruses of the herpes family.
    Type: Grant
    Filed: August 27, 2003
    Date of Patent: December 14, 2004
    Assignee: Pharmacia & Upjohn
    Inventors: Mark E. Schnute, Fred L. Ciske, Michael J. Genin, Joseph Walter Strohbach, Suvit Thaisrivongs
  • Patent number: 6825208
    Abstract: This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; pharmaceutical compositions containing the same; and methods of using the same as anticoagulant agents for modulation of the coagulation cascade.
    Type: Grant
    Filed: August 20, 2002
    Date of Patent: November 30, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Jinglan Zhou, Leslie Robinson, Nikolaus M. Gubernator, Eddine Saiah, Xu Bai, Xin Gu
  • Patent number: 6806230
    Abstract: Pyrimidine derivatives having excellent herbicidal activities for crop plants and selectivity between crop plants and weeds, are presented. Pyrimidine derivatives represented by the following formula (I): wherein R1 is a hydrogen atom, an alkyl group, a haloalkyl group or the like; R2 is an alkyl group, a phenyl group which may be substituted, or the like; R3 is a hydrogen atom, an alkyl group, an alkynyl group or the like; R7 is a hydrogen atom, a halogen atom, an alkyl group or the like; R8 is a hydrogen atom, an alkyl group or the like, W is a —C(═Q) Z— group or a —SO2— group; Q is O or S; Z is O, S, a —C(R4)R5—, a —NR6 group or the like; each of R4 and R5 is a hydrogen atom, an alkyl group, an alkoxy group or the like; R6 is a hydrogen atom or an alkyl group; and Ar is a phenyl group which may be substituted, a pyridyl group which may be substituted, or the like, and herbicides containing such pyrimidine derivatives as active ingredients.
    Type: Grant
    Filed: March 11, 2002
    Date of Patent: October 19, 2004
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Atsushi Yasuda, Fumiaki Takabe, Ikumi Urushibata, Mikio Yamaguchi, Yoshihiro Yamaji, Makoto Fujinami, Takeshige Miyazawa
  • Patent number: 6794379
    Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.
    Type: Grant
    Filed: June 6, 2002
    Date of Patent: September 21, 2004
    Assignee: Tularik Inc.
    Inventors: Julio C. Medina, Michael G. Johnson, An-Rong Li
  • Patent number: 6794336
    Abstract: 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, hal
    Type: Grant
    Filed: June 21, 2002
    Date of Patent: September 21, 2004
    Assignee: Aventis Crop Science GmbH
    Inventors: Klaus Haaf, Lothar Willms, Thomas Auler, Hubert Menne, Hermann Bieringer
  • Patent number: RE39266
    Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione derivatives of the general formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: September 5, 2006
    Assignee: Dr. Reddy's Laboratories, Limited
    Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti, Sarma K. S. Pakala