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.
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
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
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.
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
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
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
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.
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
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
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
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
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.
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
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).
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.
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
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
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
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
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.
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
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
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
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.
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.
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