Acyclic C-n=n-n Containing Patents (Class 514/151)
  • Publication number: 20020071875
    Abstract: Disclosed is both a method and composition for controlling deleterious organisms, such as insects, nematodes and weeds by applying a compound comprised of a liquid medium comprising an azide and an azide stabilizer. The azide can be selected from the group consisting of sodium azide and potassium azide or a combination of the two. The composition provides an effective pesticide, without causing significant harm to the environment. The composition may be applied to soil to control a population of a deleterious organism.
    Type: Application
    Filed: October 9, 2001
    Publication date: June 13, 2002
    Inventor: Rodrigo Rodriguez-Kabana
  • Publication number: 20020072529
    Abstract: The present invention relates to new aryl ether sulphonamides and analogues, processes for their preparation and their use for the treatment of neurodegenerative disorders, in particular for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy and craniocerebral trauma.
    Type: Application
    Filed: June 11, 2001
    Publication date: June 13, 2002
    Inventors: Joachim Mittendorf, Jurgen Dressel, Michael Matzke, Jorg Keldenich, Klaus-Helmut Mohrs, Siegfried Raddatz, Jurgen Franz, Peter Spreyer, Verena Vohringer, Joachim Schuhmacher, Michael-Harold Rock, Ervin Horvath, Arno Friedl, Frank Mauler, Jean Marie Viktor de Vry, Reinhard Jork
  • Publication number: 20020065269
    Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: June 22, 2001
    Publication date: May 30, 2002
    Applicant: Amgen Inc.
    Inventors: Kevin Koch, Andreas Termin, John A. Josey
  • Patent number: 6395719
    Abstract: The present invention is directed to increasing levels of acetylcholine by the administration of 2-aryl-3-aroylbenzo[b]thiophenes.
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: May 28, 2002
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Michele Annette Glinn, Steven Marc Paul, Xin Wu
  • Publication number: 20020058635
    Abstract: Novel purine L-nucleoside compounds are disclosed, in which both the purine rings and the sugar are either modified, functionalized, or both. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Th1 and Th2.
    Type: Application
    Filed: October 30, 2001
    Publication date: May 16, 2002
    Inventor: Devron R. Averett
  • Publication number: 20020049187
    Abstract: This invention provides methods and 2-(azetidin-2-on-1-yl) acetic acid derivatives of Formula I 1
    Type: Application
    Filed: December 8, 2000
    Publication date: April 25, 2002
    Inventors: Robert F. Bruns, Robin DG Cooper, Bruce A. Dressman, David C. Hunden, Stephen W. Kaldor, Gary A. Koppel, John R. Rizzo, Jeffrey J. Skelton, Mitchell I. Steinberg
  • Publication number: 20020049212
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: January 3, 2001
    Publication date: April 25, 2002
    Inventors: Fumitaka Ito, Hirohide Noguchi, Yoriko Ohashi, Hirohisa Shimokawa
  • Publication number: 20020037881
    Abstract: Omega chain modified 15-HETE derivatives and methods of their use for treating dry eye are disclosed.
    Type: Application
    Filed: September 20, 2001
    Publication date: March 28, 2002
    Inventor: David B. Belanger
  • Publication number: 20020035094
    Abstract: Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. 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 inflammation, pain, diabetes, 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: August 17, 2001
    Publication date: March 21, 2002
    Applicant: Amgen Inc.
    Inventors: Nathan B. Mantlo, Stephen T. Schlachter, John A. Josey
  • Publication number: 20020035095
    Abstract: Hydroxyeicosatetraenoic acid analogs and methods of their use in treating dry eye disorders are disclosed.
    Type: Application
    Filed: September 10, 2001
    Publication date: March 21, 2002
    Inventors: Peter G. Klimko, Mark R. Hellberg, John R. Falck, Raymond E. Conrow
  • Publication number: 20020032209
    Abstract: A method for inhibiting the growth of neoplastic cells by exposure to 2,9-disubstituted purin-6-ones.
    Type: Application
    Filed: July 30, 2001
    Publication date: March 14, 2002
    Inventors: Rifat Pamukcu, Gary A. Piazza
  • Publication number: 20020019382
    Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.
    Type: Application
    Filed: December 4, 2000
    Publication date: February 14, 2002
    Inventors: James P. Snyder, Matthew C. Davis, Brian Adams, Mamoru Shoji, Dennis C. Liotta, Eva M. Ferstl, Ustun B. Sunay
  • Publication number: 20020004514
    Abstract: The present invention relates to the compound (+)-6-[amino-(6-chloro-pyridin-3-yl)-(3-methyl-3H-imidazol-4-yl)-methyl ]-4-(3-chloro-phenyl)-1-cyclopropylmethyl-1H-quinolin-2-one, pharmaceutically acceptable salts and solvates thereof, prodrugs thereof, and to the use of said compound for inhibiting abnormal cell growth, including cancer, in mammals. The invention also relates to methods useful in synthesizing the aforementioned compound.
    Type: Application
    Filed: January 17, 2001
    Publication date: January 10, 2002
    Inventor: Bingwei V. Yang
  • Publication number: 20020002196
    Abstract: Heteroatom-interrupted HETE derivatives and methods of their use for treating dry eye are disclosed.
    Type: Application
    Filed: June 25, 2001
    Publication date: January 3, 2002
    Inventors: Raymond E. Conrow, Peter G. Klimko
  • Publication number: 20010056084
    Abstract: The invention provides the use of selective mGluR5 antagonists for the treatment of pain and anxiety, and the use of mGluR antagonists for the treatment of pain, whereby analgesic effect is achieved by interaction of said antagonists primarily or predominantly at peripheral mGluR receptors.
    Type: Application
    Filed: March 29, 2001
    Publication date: December 27, 2001
    Inventors: Hans Allgeier, Nicholas David Cosford, Peter Josef Flor, Fabrizio Gasparini, Conrad Gentsch, Stephen D. Hess, Edwin Carl Johnson, Rainer Kuhn, Mark Tricklebank, Laszlo Urban, Mark Andrew Varney, Gonul Velicelebi, Katharine Walker
  • Publication number: 20010051633
    Abstract: The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
    Type: Application
    Filed: February 7, 2001
    Publication date: December 13, 2001
    Inventors: Christopher F. Bigge, Gian Luca Araldi, Sui Xiong Cai, Anthony P. Guzikowski, Donald Lamunyon, Nancy C. Lan, Zhang-Lin Zhou, John F.W. Keana
  • Publication number: 20010051648
    Abstract: Heteroatom-interrupted HETE derivatives and methods of their use for treating dry eye are disclosed.
    Type: Application
    Filed: June 25, 2001
    Publication date: December 13, 2001
    Inventors: Raymond E. Conrow, Peter G. Klimko
  • Publication number: 20010049367
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: March 5, 2001
    Publication date: December 6, 2001
    Inventors: Youssef L. Bennani, Lawrence A. Black, Wesley J. Dwight, Ramin Faghih, Robert G. Gentles, Huaqing Liu, Kathleen M. Phelan, Anil Vasudevan, Henry Q. Zhang
  • Publication number: 20010044428
    Abstract: This invention relates to aminopyridines of Formula I: 1
    Type: Application
    Filed: March 29, 2001
    Publication date: November 22, 2001
    Applicant: CoCensys, Inc.
    Inventor: Derk J. Hogenkamp
  • Publication number: 20010031749
    Abstract: The compounds of the general formula I 1
    Type: Application
    Filed: January 25, 2001
    Publication date: October 18, 2001
    Inventor: Hans Rudolf Pfaendler
  • Publication number: 20010027209
    Abstract: Calanolides and analogues thereof that demonstrate potent mycobacterium activity are provided. Also provided is a method of using calanolides and analogues thereof for treating or preventing mycobacterium infections. The calanolides and analogues thereof provided are obtained via syntheses employing chromene 4 and chromanone 7 as key intermediates.
    Type: Application
    Filed: December 11, 2000
    Publication date: October 4, 2001
    Applicant: Sarawak Medichem Pharmaceuticals, Inc.
    Inventors: Ze-Qi Xu, Yuh Meei Lin, Michael T. Flavin
  • Publication number: 20010025045
    Abstract: This invention relates to substituted isoquinoline derivatives and their use as anticonvulsants.
    Type: Application
    Filed: April 22, 2001
    Publication date: September 27, 2001
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Peter David Edwards, John David Harling, Mervyn Thompson
  • Publication number: 20010021706
    Abstract: Compound of formula I: 1
    Type: Application
    Filed: November 29, 2000
    Publication date: September 13, 2001
    Applicant: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Akireddy Srinivasa Rao, Venkata Ramana Doppalapudi
  • Patent number: 6287601
    Abstract: Compositions and methods of the topical treatment of equine laminitis are disclosed. In particular, combinations of a fast acting nitric oxide (NO) donor, a sustained acting NO donor and an NSAID mixed in a lipid-based carrier are described. The application of such combinations to the affected areas, e.g., the hoofs and surrounding tissues, of an equine afflicted with laminitis provides relief from the debilitating effects of this painful, often life-threatening condition.
    Type: Grant
    Filed: June 16, 1999
    Date of Patent: September 11, 2001
    Inventor: Meri Charmyne Russell
  • Patent number: 6214813
    Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: April 10, 2001
    Assignee: Kinetek Pharmaceuticals, Inc.
    Inventors: Zaihui Zhang, Jun Yan, Danny Leung, Penelope C. Costello, Jasbinder Sanghera
  • Patent number: 6191124
    Abstract: The present invention relates to compounds of formula (I) which are imidazo[2,1-b]benzothiazole-3-methanol and imidazo[2,1-b]thiazole-5-methanol derivatives useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R1 is —H or —CH3; wherein R2 is —H or —CH3; or wherein R1 and R2 taken together are (a) formula (II), or (b) formula (III).
    Type: Grant
    Filed: April 7, 1997
    Date of Patent: February 20, 2001
    Assignee: Pharmacia & Upjohn Company
    Inventor: Herman W. Smith
  • Patent number: 6045827
    Abstract: Compositions and methods of the topical treatment of equine laminitis are disclosed. In particular, combinations of a fast acting nitric oxide (NO) donor, a sustained acting NO donor and an NSAID mixed in a lipid-based carrier are described. The application of such combinations to the affected areas, e.g., the hoofs and surrounding tissues, of an equine afflicted with laminitis provides relief from the debilitating effects of this painful, often life-threatening condition.
    Type: Grant
    Filed: August 19, 1997
    Date of Patent: April 4, 2000
    Assignee: Meri Charmyne Russell
    Inventor: Meri Charmyne Russell
  • Patent number: 6013814
    Abstract: The present invention relates to novel 1.alpha.-hydroxy vitamin D derivatives in which the 17-position side chain carries an azide or optionally substituted 1,2,3-triazole group, including compounds of general formula (I) where R.sup.1 represents a methyl group having .alpha.- or .beta.-configuration; W represents a valence bond or a C.sub.1-5 alkylene group; X represents azide or an optionally substituted triazole group; and A.dbd. represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-hydroxylated vitamin D or analogue thereof. Active compounds of the invention exhibit cell modulating activity while exhibiting a substantial lack of calcaemic effect.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: January 11, 2000
    Assignee: Research Institute for Medicine and Chemistry, Inc.
    Inventors: Robert Henry Hesse, Sundara Katugam Srinivasasetty Setty, Malathi Ramgopal, Gaddam Subba Reddy
  • Patent number: 6001824
    Abstract: The present invention provides a compound having the structure: ##STR1## wherein R.sub.1 is a saturated or unsaturated linear or branched chain alkyl group, or a cholestanyl group; wherein R.sub.2 is a 2-indolyl, 3-indolyl, 4-indolyl, 5-indolyl, 4-hydroxyphenyl, 4-(arylalkyloxy)phenyl, 3,4-dihalophenyl, 4-hydroxy-3,5-dihalophenyl, 4-azidophenyl or 4-halophenyl group; wherein R.sub.3 is H, a linear or branched chain alkyl or alkenyl group, or a phenyl, 2-azidophenyl, 3-azidophenyl, 4-azidophenyl group, or an a alkenylacyl, 3-amino-3-butylpropyl, N-[N-(N-{4-azidobenzoyl}aminopropyl) aminopropyl], cis- or trans-cinnamyl, 2-amino-2-[(4'-azidophenyl)acetyl, (trifluoromethyl)aminoacetyl or D- or L-arginyl group bonded through the .alpha.-carbonyl moiety thereof; R.sub.4 is H, or a linear or branched chain alkyl group; wherein R.sub.5, R.sub.6 and R.sub.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: December 14, 1999
    Assignee: The Trustees of Columbia University
    Inventors: Koji Nakanishi, Danwen Huang, Seok-Ki Choi, Aristotle Kalivretenos, Robert Goodnow
  • Patent number: 5808038
    Abstract: The present invention is directed to bistriazene compounds, pharmaceutical compositions containing effective anti-cancer amounts of these compounds, a method for treating cancer comprising administering to affected subjects an anti-cancer effective amount of a bistriazene compound, and the use of bistriazene compounds as crosslinking reagents applicable to the synthesis and manipulation of polymeric macromolecules.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: September 15, 1998
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventors: Christopher J. Michejda, Jeffrey J. Blumenstein
  • Patent number: 5731301
    Abstract: The present invention is directed to bistriazene compounds, pharmaceutical compositions containing effective anti-cancer amounts of these compounds, a method for treating cancer comprising administering to affected subjects an anti-cancer effective amount of a bistriazene compound, and the use of bistriazene compounds as crosslinking reagents applicable to the synthesis and manipulation of polymeric macromolecules.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: March 24, 1998
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Christopher J. Michejda, Jeffrey J. Blumenstein
  • Patent number: 5728687
    Abstract: Pharmaceutical compositions having therapeutic synergy comprising taxol or Taxotere or analogues thereof combined with at least one therapeutically useful substance for treating neoplastic diseases.
    Type: Grant
    Filed: May 9, 1995
    Date of Patent: March 17, 1998
    Assignee: Rhone-Poulenc Rorer, S.A.
    Inventor: Marie-Christine Bissery
  • Patent number: 5672593
    Abstract: The present invention is directed to bistriazene compounds, pharmaceutical compositions containing effective anti-cancer amounts of these compounds, a method for treating cancer comprising administering to affected subjects an anti-cancer effective amount of a bistriazene compound, and the use of bistriazene compounds as crosslinking reagents applicable to the synthesis and manipulation of polymeric macromolecules.
    Type: Grant
    Filed: June 28, 1993
    Date of Patent: September 30, 1997
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Christopher J. Michejda, Jeffrey J. Blumenstein
  • Patent number: 5232916
    Abstract: Compounds having the formula: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
    Type: Grant
    Filed: October 28, 1991
    Date of Patent: August 3, 1993
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert Zamboni, Petpiboon Prasit, Robert N. Young
  • Patent number: 5032572
    Abstract: Polymers from ethylenically unsaturated monomers, cross-linked by a substituted divinylazobenzene are useful as pharmaceutical compositions for the delivery of medicaments. The polymers are degraded by the enzymes of the upper gastrointestinal tract or are transferred intact past the upper gastrointestinal tract, to deliver the medicament to the large intestine. In particular, the polymers contain divinylazobenzene compounds of the formulae ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of H, (except that R.sub.1 and R.sub.2 are not both H), Cl, Br, I, NO.sub.2, NH.sub.2, RO, ArO, COOH or salts thereof, COOR, COOAr, CHO, COR, SO.sub.3 H or salts thereof, R or Ar and wherein R is alkyl of up to 18 carbon atoms and Ar is mono- or bicyclic aryl of up to 15 carbon atoms.
    Type: Grant
    Filed: August 12, 1988
    Date of Patent: July 16, 1991
    Assignees: Medical College of Ohio, Bowling Green State University
    Inventors: Murray Saffran, Douglas C. Neckers
  • Patent number: 4923970
    Abstract: A substituted 1-(2-chloroethyl)-3-acyl-3-alkyltriazene of the formula: ##STR1## in which R.sub.1 is 1-oxoalkyl containing from two to eight carbon atoms, fluorinated 1-oxoalkyls containing from two to eight carbon atoms and substituted with up to three fluorine atoms, benzoyl, phenylacetyl, carboalkoxy containing from two to eight carbon atoms, fluorinated carboalkyl containing from two to eight carbon atoms and up to three fluorine atoms, carbophenoxy, N-phenyl aminocarbonyl, N-alkyl aminocarbonyl containing from two to eight carbon atoms, thiocarbamoyl, N-alkylthiocarbamoyls with from two to eight carbon atoms, N-phenylthiocarbamoyl, dialkylphosphonates in which the alkyl groups can be the same or different and each contains from one to seven carbon atoms, phenylsulfonyl, and meta or para-substituted phenylsulfonyl in which the meta or para substituent is methyl, ethyl, methoxy, ethoxy, fluoro and chloro; and R.sub.
    Type: Grant
    Filed: March 28, 1988
    Date of Patent: May 8, 1990
    Assignee: Bionetics Research, Inc.
    Inventors: Christopher J. Michejda, Richard H. Smith, Jr.
  • Patent number: 4766142
    Abstract: Compound of the formula (I) ##STR1## wherein n is zero or an integer of 1 to 3;R is(a) --NHR.sub.3, wherein R.sub.3 is(a') --CON(NO)R.sub.4, in which R.sub.4 is C.sub.1 -C.sub.4 alkyl either unsubstituted or substituted by halogen; or(b') --CO(CH.sub.2).sub.m --R.sub.5, in which R.sub.5 is halogen, oxiranyl, methyloxiranyl, aziridinyl, a group ##STR2## or a group ##STR3## and m is zero or an integer of 1 to 4; or (b) ##STR4## wherein either R.sub.6 and R.sub.7 are the same and are each oxiranemethyl, aziridinemethyl, or C.sub.2 -C.sub.4 alkyl 2-substituted by halogen or by a group --OSO.sub.2 R.sub.8 wherein R.sub.8 is C.sub.1 -C.sub.4 alkyl or phenyl, or one of R.sub.6 and R.sub.7 is hydrogen and the other is as defined above;each group R.sub.1 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.2 is a C.sub.1 -C.sub.6 alkyl group terminating with (i) a basic moiety chosen from an amino group, a mono- or di- C.sub.1 -C.sub.
    Type: Grant
    Filed: October 3, 1985
    Date of Patent: August 23, 1988
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Federico Arcamone, Nicola Mongelli, Sergio Penco
  • Patent number: 4663308
    Abstract: Polymers from ethylenically unsaturated monomers, cross-linked by a substituted or unsubstituted divinylazobenzene are useful as carriers or capsules for medicaments, which are degraded by the enzymes of the upper gastrointestinal tract or which must be transferred intact past the upper gastrointestinal tract, to deliver the medicament to the large intestine.Polymers containing monomeric units of the formulaH.sub.2 C.dbd.CH--C.sub.6 H.sub.4 --N.dbd.N--M,wherein M is the residue of an amino-containing medicament, are useful as carriers for therapeutic agents or as therapeutic agents per se.
    Type: Grant
    Filed: July 18, 1984
    Date of Patent: May 5, 1987
    Assignees: Medical College of Ohio, Bowling Green State University
    Inventors: Murray Saffran, Douglas C. Neckers