Thiocarbonyl Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/313)
  • Patent number: 8835467
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: September 16, 2014
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Patent number: 8796175
    Abstract: The invention relates to the use of at least one compound selected from the class of the sulphoximines for enhancing plants' intrinsic defenses and/or for improving plant growth and/or for enhancing the resistance of plants to plant diseases which are caused by fungi, bacteria, viruses, MLOs (mycoplasma-like organisms) and/or RLOs (rickettsia-like organisms), and/or for enhancing the resistance of plants to abiotic stress factors.
    Type: Grant
    Filed: August 17, 2009
    Date of Patent: August 5, 2014
    Assignee: Bayer CropScience AG
    Inventors: Peter Jeschke, Wolfgang Thielert, Heike Hungenberg
  • Patent number: 8680100
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: March 25, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • Publication number: 20130324737
    Abstract: The invention disclosed in this document is related to the field of processes to produce certain 2-(pyridine-3-yl)thiazoles as intermediates for the synthesis of pesticidal thiazole amides.
    Type: Application
    Filed: May 30, 2013
    Publication date: December 5, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Ronald Ross, JR., Carl DeAmicis, Yuanming Zhu, Noormohamed M. Niyaz, Kim E. Arndt, Scott P. West, Gary Roth
  • Publication number: 20130231351
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Application
    Filed: January 23, 2013
    Publication date: September 5, 2013
    Applicant: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Patent number: 8461346
    Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: June 11, 2013
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Markus Berger, Jan Dahmen, Hartmut Rehwinkel, Stefan Jaroch, Heike Schaecke
  • Publication number: 20130102774
    Abstract: A process for transforming a group >C?O (I) in a compound into a group >C?S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2 C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2 C5H5N.
    Type: Application
    Filed: February 3, 2012
    Publication date: April 25, 2013
    Applicant: VIRONOVA AB
    Inventors: Birgitta Pettersson, Vedran Hasimbegovic, Per H Svensson, Jan Bergman
  • Patent number: 8383653
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Grant
    Filed: June 30, 2004
    Date of Patent: February 26, 2013
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Publication number: 20120065206
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Application
    Filed: December 1, 2009
    Publication date: March 15, 2012
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • Publication number: 20110218220
    Abstract: The present invention relates to the use of isotopically labeled derivatives of isoniazid, ethionamide and related compounds as effective therapy for the treatment of mycobacterial diseases, including Mycobacterium tuberculosis.
    Type: Application
    Filed: August 20, 2008
    Publication date: September 8, 2011
    Applicants: STC.UNM, THE JOHN HOPKINS UNIVERSITY
    Inventors: Graham Timmins, Sharon Master, Vojo P. Deretic, William Bishai
  • Publication number: 20110178102
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Application
    Filed: June 30, 2004
    Publication date: July 21, 2011
    Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Vern L Schramm, Anthony A. Suave
  • Patent number: 7915253
    Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: March 29, 2011
    Assignee: Kalypsys, Inc
    Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen K. Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
  • Patent number: 7678920
    Abstract: N-Substituted sulfoximines are effective at controlling insects.
    Type: Grant
    Filed: April 8, 2005
    Date of Patent: March 16, 2010
    Assignee: Dow AgroSciences LLC
    Inventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang
  • Patent number: 7528274
    Abstract: Certain thiol and acylthiol compounds inhibit retrovirus growth by attacking the highly conserved zinc finger regions of essential viral proteins. These compounds, compositions containing them, and methods of using them to treat retroviral infections such as HIV are described. These compounds are also useful for preparation of vaccines comprised of inactivated retroviruses such as HIV, prevention of the transmission of such retroviruses, and detection of retroviral proteins.
    Type: Grant
    Filed: July 25, 2002
    Date of Patent: May 5, 2009
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: John K. Inman, Atul Goel, Ettore Appella, Jim Turpin, Marco Schito
  • Patent number: 7507828
    Abstract: One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
    Type: Grant
    Filed: May 11, 2004
    Date of Patent: March 24, 2009
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Bin Chen
  • Publication number: 20090029971
    Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
    Type: Application
    Filed: September 4, 2008
    Publication date: January 29, 2009
    Applicant: KALYPSYS, INC.
    Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
  • Patent number: 7241782
    Abstract: The invention relates to a novel polymorph V of torasemide, to a process for its preparation, to its use as a raw material for the preparation of crystalline modifications I and III of torasemide, to amorphous torasemide modifications and to pharmaceutically acceptable salts of torasemide, to pharmaceutical forms containing the said novel polymorph V of torasemide as the active ingredient as well as to its use.
    Type: Grant
    Filed: September 25, 2000
    Date of Patent: July 10, 2007
    Assignee: PLIVA, farmaceutska industrija, dionicko drustvo
    Inventors: Darko Filić, Miljenko Dumić, Bo{hacek over (z)}ena Klepić, Aleksandar Danilovski, Marijan Tudja
  • Patent number: 7105549
    Abstract: This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1–R4 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: September 6, 2002
    Date of Patent: September 12, 2006
    Assignee: Euro-Celtique S.A.
    Inventors: Bin Shao, R. Richard Goehring, Samuel F Victory, Qun Sun
  • 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: 6930130
    Abstract: The present invention relates to novel active compounds named Citrullimycines, which are obtainable by cultivation of Streptomyces sp. ST 101396 (DSM 13309), and to their pharmaceutically acceptable salts and derivatives. The present invention further relates to a process for the production of the Citrullimycines, to the microorganism Streptomycetes sp. ST 101396 (DSM 13309), to the use of the Citrullimycines and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, for example as inhibitors of the neurotensin receptor, and to pharmaceutical compositions comprising Citrullimycines or a pharmaceutically acceptable salt or derivative thereof.
    Type: Grant
    Filed: October 1, 2001
    Date of Patent: August 16, 2005
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Cordula Hopmann, Michael Kurz, Mark Brönstrup, Joachim Wink
  • Patent number: 6852863
    Abstract: The present invention relates to metabolites of (3-{[4-tert-butyl-benzyl)-(pyridine-3-sulfonyl)-amino]-methyl}-phenoxy)-acetic acid.
    Type: Grant
    Filed: January 29, 2003
    Date of Patent: February 8, 2005
    Assignee: Pfizer Inc.
    Inventors: Kimberly O. Cameron, Kim A. Johnson, Bruce A. Lefker, Chandra A. Prakash
  • Patent number: 6825221
    Abstract: 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: Grant
    Filed: August 29, 2002
    Date of Patent: November 30, 2004
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, Sophie Beauchemin
  • Publication number: 20040110802
    Abstract: The invention provides antimicrobial agents and methods of using the agents for sterilization, sanitation, antisepsis, disinfection, and treatment of infections in mammals.
    Type: Application
    Filed: August 20, 2003
    Publication date: June 10, 2004
    Inventors: Atli Thorarensen, J. Craig Ruble, Jed F. Fisher, Donna Lee Romero, Thomas J. Beauchamp, Jill M. Northuis
  • Patent number: 6747041
    Abstract: Heterocyclic dicarboxylic acid diamide derivative represented by the general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Het represents a 5- or 6-membered heterocycle; X and Y represent each halocyano, nitro, optionally halogenated C3-6, cycloalkyl, optionally substituted phenyl, an optionally substituted heterocycle, etc; n is from 0 to 3; m is from 1 to 5; Z1 and Z2 represent each O or S; and B1 to B4 represent each C or N. Agricultural/horticultural insecticides having an excellent controlling effect on pest insects such as diamond-back moth (Pluntella xylostella) and tobacco cutworm (Spodoptera litura).
    Type: Grant
    Filed: April 10, 2002
    Date of Patent: June 8, 2004
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Takeshi Katsuhira, Takashi Furuya, Makoto Gotoh, Masanori Tohnishi, Hideo Takaishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
  • Publication number: 20040034069
    Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.
    Type: Application
    Filed: August 8, 2003
    Publication date: February 19, 2004
    Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
  • Publication number: 20040018942
    Abstract: The compound of the formula 1
    Type: Application
    Filed: July 17, 2002
    Publication date: January 29, 2004
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Masamitsu Tsukamoto, Mark Read
  • Publication number: 20030195230
    Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: January 10, 2002
    Publication date: October 16, 2003
    Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
  • Publication number: 20030191113
    Abstract: The invention concerns compounds of general formula (1) wherein: n, G, Q1, Q2, X1, X2, Y and Z are as defied in the description, the method for preparing said compounds, fungicide compositions comprising said compounds and methods for treating plants using said compounds or compositions.
    Type: Application
    Filed: July 8, 2002
    Publication date: October 9, 2003
    Inventors: Francisco Nieto-Roman, Jean-Pierre Vors, Alain Villier, Helene Lachaise, Adeline Mousques, Benoit Hartmann, Pierre Hutin, Jose Lorenzo Molina, Benoit Muller
  • Publication number: 20030119883
    Abstract: The present invention relates to amlodipine free base in a crystalline form, to pharmaceutical formulations comprising such material, processes of manufacture and its use in therapy.
    Type: Application
    Filed: August 20, 2002
    Publication date: June 26, 2003
    Applicant: Pfizer Inc.
    Inventors: Alan Craig Bentham, Alan John Pettman, Keith Stephen Ruddock
  • Publication number: 20030119852
    Abstract: What is described are compounds of the formulae (I) and (II) 1
    Type: Application
    Filed: September 18, 2002
    Publication date: June 26, 2003
    Inventors: Marion Beckmann, Oswald Ort, Uwe Doller, Gerhard Krautstrunk, Wolfgang Schaper, Peter Lummen, Daniela Jans, Waltraud Hempel, Jutta Maria Waibel, Barbara Lorkens
  • Publication number: 20030083523
    Abstract: A compound represented by the following general formula (I): 1
    Type: Application
    Filed: June 18, 2002
    Publication date: May 1, 2003
    Applicant: Mitsubishi Chemical Corporation
    Inventors: Ryoichi Ando, Makoto Kawamura, Noriko Chiba, Kazutoshi Watanabe
  • Patent number: 6521626
    Abstract: Compounds of formula (1): wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a linker atom or group; r and s is each zero or an integer 1; R2 and R3, which may be the same or different, is each a hydrogen or halogen atom or a straight or branched alkyl, haloalkyl, alkoxy, haloalkoxy, hydroxyl or nitro group; Alk2 is a straight or branched alkylene chain; m is zero or an integer 1; R4 is a hydrogen atom or a methyl group; R5 is a hydrogen atom or a straight or branched alkyl group; R6 is a group —(CH2)tR7 in which t is zero or the integer 1 and R7 is an optionally substituted polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates and hydrates the
    Type: Grant
    Filed: March 23, 1999
    Date of Patent: February 18, 2003
    Assignee: Celltech R&D Limited
    Inventors: Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
  • Patent number: 6511993
    Abstract: Compounds of formula (I) and pharmaceutically-acceptable derivatives thereof, are matrix metalloprotease inhibitors, useful in treatment of conditions mediated by matrix metalloproteases, such as chronic dermal ulcers.
    Type: Grant
    Filed: June 2, 2000
    Date of Patent: January 28, 2003
    Inventors: Kevin Neil Dack, Michael Jonathan Fray, Gavin Alistair Whitlock, Mark Llewellyn Lewis, Nicholas Murray Thomson
  • Publication number: 20020173631
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: May 8, 2002
    Publication date: November 21, 2002
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 6465471
    Abstract: Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
    Type: Grant
    Filed: July 1, 1999
    Date of Patent: October 15, 2002
    Assignee: Celltech Therapeutics Limited
    Inventors: Graham John Warrellow, John Clifford Head, John Robert Porter, Sarah Catherine Archibald
  • Publication number: 20020143206
    Abstract: Process for the oxidation of aldehydes to the corresponding acids in which an aldehyde as substrate is oxidized to the corresponding acid in the presence of an equimolar amount, or a molar excess, of periodate, catalytic amounts of dichromate or CrO3, and in the presence of an acid in water, a water/solvent mixture or in a solvent at a temperature of −20° C. to +50° C.
    Type: Application
    Filed: March 28, 2002
    Publication date: October 3, 2002
    Inventors: Paul Alsters, Elisabeth Schmieder Van De Vondervoort
  • Patent number: 6339045
    Abstract: N-(substituted or unsubstituted)-4-substituted-6-(substituted or unsubstituted) phenoxy-2-pyridine carboxamide or thiocarboxamide represented by the general formula (I) and a process for producing the compound. A herbicide containing as an effective ingredient N-(substituted or unsubstituted)-4-substituted-6-(substituted or unsubstituted) phenoxy-2-pyridine carboxamide or thiocarboxamide represented by the general formula (I).
    Type: Grant
    Filed: August 12, 1998
    Date of Patent: January 15, 2002
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Hisashi Kanno, Yoshikazu Kubota, Tsutomu Sato, Koki Sato
  • Patent number: 6214835
    Abstract: The present invention provides dihalopropene compounds of the general formula: wherein R1 is C1-C10 alkyl or the like; L is C(═O)NH or the like; R2, R3 and R4 are independently halogen or the like; R5, R6 and R7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.
    Type: Grant
    Filed: June 2, 1999
    Date of Patent: April 10, 2001
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
  • Patent number: 6191280
    Abstract: A process for preparing thiopyridines of the formula I where the substituents are as defined in the description.
    Type: Grant
    Filed: November 17, 1999
    Date of Patent: February 20, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Hamprecht, Markus Menges, Olaf Menke, Robert Reinhard, Peter Schäfer, Cyrill Zagar
  • Patent number: 6121273
    Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: September 19, 2000
    Assignee: GPI NIL Holdings, Inc
    Inventors: Gregory S. Hamilton, Jai-He Li, Wei Huang
  • Patent number: 6110945
    Abstract: Aromatic amines of formula (1) are described: ##STR1## wherein Az is an optionally substituted monocyclic six-membered nitrogen-containing aromatic group;L.sup.1 is a linker atom or group;R is a carboxylic acid or a derivative thereof;and R.sup.5 is a group --L.sup.2 (CH.sub.2).sub.t R.sup.6 in which L.sup.2 is a --N(R.sup.7)CO-- or --N(R.sup.7)CS-- group.The compounds are able to inhibit the binding of .alpha..sub.4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
    Type: Grant
    Filed: June 2, 1999
    Date of Patent: August 29, 2000
    Assignee: Celltech Therapeutics Limited
    Inventors: John Clifford Head, Graham John Warrellow, John Robert Porter, Sarah Catherine Archibald
  • Patent number: 6005112
    Abstract: A process for producing N-substituted pyridine carboxamide or thiocarboxamide, comprising reacting a substituted or unsubstituted pyridine metal compound with substituted isocyanate or isothiocyanate to obtain an addition reaction product thereof, and then substituting the metal of said addition reaction product with a proton. The process according to the present invention can be applied even to compounds having an oxidation-susceptible substituent group and, therefore, industrially useful.
    Type: Grant
    Filed: August 12, 1998
    Date of Patent: December 21, 1999
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Hisashi Kanno, Yoshikazu Kubota
  • Patent number: 5919792
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
  • Patent number: 5834467
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 10, 1998
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Vincent J. Kalish, Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriquez
  • Patent number: 5705513
    Abstract: A compound, composition, and method for controlling Take-all disease of plants by applying to the seed prior to planting, a fungicide of the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring which is pyridine; R and n are defined herein; A is selected from the group consisting of --C(O)--SR.sub.3, --NH--C(X)R.sub.4, --C(.dbd.NR.sub.3)--XR.sub.7, and --C(X)-amine wherein the amine is substituted with with an alkylaminocarbonyl and a hydrogen or wherein the amine has a first and a second amine substituent defined herein; B is --W.sub.m --Q(R.sub.2).sub.3 or selected from 0-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ; Q is C, Si, Ge, or Sn; W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W may also be selected from --N(R.sub.3).sub.m H(.sub.1-m)--, --S(O)p--, and --O--; X is O or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R.sub.
    Type: Grant
    Filed: December 28, 1994
    Date of Patent: January 6, 1998
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
  • Patent number: 5597839
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: January 28, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5571897
    Abstract: Lanthanide chelates which contain three heterocyclic rings covalently coupled to each other (either one 2,6-pyridylene and two five-membered unsaturated heterocyclic ring moieties or two 2,6-pyridylene and one five-membered unsaturated heterocyclic ring moiety) and two chelating groups so seated that they together chelate the same lanthanide ion even in aqueous solutions. These lanthanide chelates can optionally contain a reactive group for coupling to biologically active molecules. The new chelates are suitable for classical lanthanide chelate applications and are also useful as probes in time-resolved fluorescence microscopy, cytometry, multilabelling techniques and in process controls in industry.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: November 5, 1996
    Assignee: Wallac Oy
    Inventors: Harri Takalo, Veli-Matti Mukkala
  • Patent number: 5439925
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: August 8, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
  • Patent number: 5389653
    Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
    Type: Grant
    Filed: April 16, 1993
    Date of Patent: February 14, 1995
    Assignee: Hoffman-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
  • Patent number: 5225545
    Abstract: The compounds of the formula (1) indicated in claim 1 are suitable for use as direct dyes for dyeing and printing a wide range of materials, in particular cellulose-containing fibre materials, producing dyeings and prints having good fastness properties.
    Type: Grant
    Filed: May 12, 1992
    Date of Patent: July 6, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Urs Lauk