Abstract: Tertiary amines of the formula
wherein
A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.
Type:
Grant
Filed:
December 16, 1999
Date of Patent:
August 27, 2002
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synèse Jolidon, Hans Lengsfeld, Olivier Morand, Gérard Schmid, Yu-Hua Ji
Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
Abstract: It has been discovered that compounds of the formula:
and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).
Type:
Grant
Filed:
May 23, 2001
Date of Patent:
July 30, 2002
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Kenneth Gregory Hull, Achytharao Sidduri, Jefferson Wright Tilley
Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.
Type:
Application
Filed:
October 19, 2001
Publication date:
July 25, 2002
Applicant:
NPS Pharmaceuticals, Inc.
Inventors:
Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
Abstract: It has been discovered that compounds of the formula:
and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are usefull in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (IBD).
Type:
Grant
Filed:
May 23, 2001
Date of Patent:
July 23, 2002
Assignee:
Hoffman-La Roche Inc.
Inventors:
Kenneth Gregory Hull, Achytharao Sidduri, Jefferson Wright Tilley
Abstract: Certain 2,6-pyridinecarboxaldehydebis(imine) and 2,6-diacylpyridinebis(imine) compounds are provided, which are particularly suitable for use as tridentate ligands in iron and cobalt olefin polymerization catalysts.
Abstract: An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like and for inhibiting platelet aggregation.
Abstract: The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent.
Abstract: 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives
are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or disorders whose course involves increased connective tissue or cartilage degradation.
Abstract: The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
Type:
Grant
Filed:
June 24, 1999
Date of Patent:
April 30, 2002
Assignee:
G. D. Searle, L.L.C.
Inventors:
Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
Abstract: A production method of hydrazine derivative having a group of the formula (II)
which comprises subjecting a hydrazone derivative having a group of the formula (I)
to catalytic reduction and deactivating the reduction catalyst contained in the reaction mixture thereof.
Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
April 9, 2002
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Patrick Y. S. Lam, Charles G. Clark, Renhau Li, Donald J. P. Pinto
Abstract: The present invention provides a phthalic acid diamide derivative represented by the general formula (I)
(wherein R1, R2 and R3 are each H, C3-C6 cycloalkyl group, group of the formula —A1—Ql or the like; X may be the same or different and are each halogen atom, nitro group, phenyl group, group of the formula —A2—R7 or the like; n is 1 to 4; Y may be same or different and are each halogen atom, cyano group, phenyl group, group of the formula —A2—R7 or the like; m is 1 to 5; Z1 and Z2 are each 0 or S), fluorine-containing aniline compound represented by the general formula (ST-I) as starting material for said phthalic acid diamide derivative
(wherein Ra is halogen atom, C1-C6 alkyl group or the like and Rb, Rc and Rd is H or C2-C6 perfluoroalkyl group), and an agricultural and horticultural insecticide containing said phthaldiamide derivative, as well as to provide a method for use of said insecticide.
Abstract: Compounds of the formula:
useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
Type:
Grant
Filed:
January 27, 2000
Date of Patent:
March 19, 2002
Assignee:
American Cyanamid Company
Inventors:
Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
Abstract: The invention relates to new imides, to a plurality of processes for their preparation and to their use as fungicides.
Type:
Grant
Filed:
January 2, 2001
Date of Patent:
February 26, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Martin Vaupel, Astrid Mauler-Machnik, Gerd Hänssler, Klaus Stenzel, Martin Kugler, Thomas Jaetsch, Peter Wachtler
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved 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:
Application
Filed:
December 21, 2000
Publication date:
February 14, 2002
Inventors:
Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases.
Type:
Application
Filed:
April 6, 2001
Publication date:
February 7, 2002
Inventors:
Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Harter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jorg Keldenich, Ulf Brueggemeier, Klemens Lustig
Abstract: Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1&bgr; and TNF-&agr; and may therefore be useful in the therapy of inflammatory diseases and conditions.
Abstract: The invention relates to the use of a compound of formula (I):
for the preparation of pharmaceutical compositions for increasing the circulating, cellular and extracellular levels of TGF-&bgr;1.
Type:
Grant
Filed:
April 10, 2000
Date of Patent:
January 29, 2002
Assignee:
Sanofi-Synthelabo
Inventors:
Françoise Bono-Combie, Jacqueline Fournier, Jean Marc Herbert, Isabelle Lamarche, Umberto Guzzi
Abstract: The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
Type:
Application
Filed:
July 28, 2001
Publication date:
January 24, 2002
Inventors:
Ben C. Askew, Paul J. Coleman, Mark E. Duggan, Wasyl Halczenko, George D. Hartman, Cecilia A. Hunt, John H. Hutchinson, Robert S. Meissner, Michael A. Patane, Garry R. Smith, Jiabing Wang
Abstract: Monobenzenic ortho-phenylenediamines comprising at least one cationic group Z, Z being chosen from aliphatic chains, comprising at least one quaternized unsaturated ring, to their use for the oxidation dyeing of keratin fibers, to dye compositions containing them and to oxidation dyeing processes using them.
Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
Type:
Application
Filed:
December 21, 2000
Publication date:
January 17, 2002
Inventors:
Michael Gross, Serge Beaudoin, Aimee Reed
Abstract: The invention provides N-phenyltetrahydrophthalamic acid derivatives represented by the general formula [I], methods of producing the same, herbicides containing the same as the effective components, imidoylchloride derivatives as the intermediate products and methods of producing the same,
wherein X and Y each individually represent hydrogen atoms or halogen atoms, R1 represents a lower alkoxycarbonylalkylthio group, R2 represents a lower alkyl group, a halogenated lower alkyl group or a substituted or unsubstituted phenyl group, and R3 represents a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, or a lower alkoxyalkoxy group. The herbicides of the present invention, which are very useful, can be widely applied to upland, paddy field, orchard, turf, forest, non-crop land, etc., and are not harmful to crops.
Abstract: Novel compounds having the formula:
wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.
Abstract: Compounds of formula (I):
{wherein: R1 and R2 each represents a variety of organic groups; R3 and R4 each represents hydrogen or a variety of organic groups; A represents a group of formula (A-1):
[wherein: R5 represents hydrogen, hydroxy or alkyl, R6 represents hydroxy, alkoxy, alkylthio or an amine residue, X and Y each represents oxygen or sulfur, and Z represents a direct single bond between the nitrogen atom shown and the benzene ring shown in formula (I), or an alkylene group],
G represents a single bond, alkylene or substituted alkylene; the broken line represents a single or double bond; when the broken line represents a double bond, D represents a carbon atom; and E represents an ═N—O— group; when the broken line represents a single bond, D represents a CH group or a nitrogen atom, and E represents an oxygen atom, a sulfur atom, an —NH— group or a —CO— group}; and pharmaceutically acceptable salts, ester
Type:
Grant
Filed:
July 20, 2000
Date of Patent:
December 11, 2001
Assignee:
Sankyo Company, Limited
Inventors:
Hitoshi Kurata, Takafumi Kohama, Keita Kono, Ken Kitayama
Abstract: Described are compounds of the Formula VII:
wherein Het, R1, R7 and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
May 26, 2000
Date of Patent:
December 4, 2001
Assignee:
3-Dimensional Pharmaceuticals, Inc.
Inventors:
Aihua Wang, Tianbao Lu, Bruce E. Tomczuk, Richard M. Soll, John Spurlino, Roger Bone
Abstract: Certain cyclopropyl oxime ethers substituted by aryl and heterocyclic moieties possess broad spectrum fungicidal and insecticidal properties. These compounds are disclosed along with compositions containing these compounds and methods for controlling fungi and insects by the use of a fungitoxic or insecticidal amount of these compounds.
Type:
Grant
Filed:
February 17, 2000
Date of Patent:
November 6, 2001
Inventors:
Ronald Ross, Jr., Duyan Vuong Nguyen, Steve Howard Shaber
Abstract: The present invention relates to certain oxime ether compounds, compositions containing these compounds, and methods for controlling fungi by the use of a fungitoxic amount of the compounds or compositions.
Abstract: The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.
Type:
Application
Filed:
January 19, 2001
Publication date:
September 13, 2001
Applicant:
De Montfort University
Inventors:
Gerald Andrew Potter, Lawrence Hylton Patterson, Michael Danny Burke
Abstract: This invention relates to peptide-containing &agr;-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.
Type:
Grant
Filed:
March 16, 2000
Date of Patent:
September 11, 2001
Assignee:
Cephalon, Inc.
Inventors:
Sankar Chatterjee, John P. Mallamo, Ron Bihovsky, Gregory J. Wells
Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.
Type:
Grant
Filed:
December 10, 1998
Date of Patent:
September 11, 2001
Assignee:
Bayer Aktiengesellschaft
Inventors:
Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
Abstract: The invention relates to substituted N-Aliphatic-N-Aromatic tertiary - Heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis, dyslipidemia, and other coronary artery disease.
Type:
Application
Filed:
January 16, 2001
Publication date:
August 30, 2001
Applicant:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Deborah A. Mischke, Emily J. Reinhard, Barry L. Parnas, Melvin L. Rueppel
Abstract: This invention provides compounds of Formula I having the structure 1
Type:
Application
Filed:
January 26, 2001
Publication date:
August 30, 2001
Inventors:
John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa M. Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
Abstract: N-heterocyclicmethylpropylamine derivatives of formula (I):
and acid addition salts thereof;
wherein R1 represents hydrogen, halogen, alkyl, alkenyl, halogenated alkyl, alkoxy, halogenated alkoxy, hydroxyl, cyano, nitro, phenyl optionally having a substituent on a ring thereof or phenoxy; n represents an integer of 0-5; R2 represents a heterocycle containing at least one nitrogen atom as the hetero atom and optionally having a substituent on a ring thereof; and R3 represents hydrogen or C1-C5 alkyl.
Abstract: The present invention relates to a method for producing a compound of the formula:
wherein R1 is an optionally substituted hydrocarbon group; R2 is H or an optionally substituted hydrocarbon group; and Q is an optionally substituted heterocyclic group, or a salt thereof which comprises subjecting a compound of the formula:
wherein R1 has the same meaning as defined above, or a salt thereof to a nitration reaction (a), and further subjecting the resulting mixture without isolating/purifying the resulting compound of the formula:
wherein R1 has the same meaning as defined above, or a salt thereof to a reaction (b) with a compound of the formula:
Q—CH2—NH—R2 [III]
wherein each symbol has the same meaning as defined above, or a salt thereof.
Abstract: A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
Type:
Grant
Filed:
November 9, 2000
Date of Patent:
July 17, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Michael Palucki, David L. Hughes, Chunhua Yang, Nobuyoshi Yasuda
Abstract: Ortho-substituted benzoylguanidines of the formula I
in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction and for the treatment of angina pectoris. They also inhibit, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the triggering of ischemically induced cardiac arrhythmias.
Type:
Grant
Filed:
September 17, 1999
Date of Patent:
July 17, 2001
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Udo Albus, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Wolfgang Scholz, Jan-Robert Schwark, Andreas Weichert
Abstract: Compounds, or solvates or salts thereof, of formula (I):
selective delta opioid agonists and antagonists and may be of therapeutic utility as analgesics, immunosuppressants to prevent rejection in organ transplant and skin graft, anti-allergic and anti-inflammatory agents, brain cell protectants, agents for treating drug and alcohol abuse, gastritis, diarrhoea, cardiovascular and respiratory diseases, cough, mental illness, epilepsy and, in general, agents for the treatment of those pathological conditions which, customarily, can be treated with agonists and antagonists of the delta opioid receptor.
Abstract: A new class of N-linked Lewis and LacNAc analogs of are synthesized and shown to be effective inhibitors of human fucosyltransferases. In a high yielding reaction sequence the glucosamine derivative 1 was transformed to the 3-azido-2,3-dideoxy sugar 2e under excellent stereocontrol. The LacNAc analog 4d was synthesized as a single isomer in three steps starting from 2e. In a one pot procedure iminocyclitol 5 was transformed into aldehyde 6 and successfully used for reductive amination with 4c and 2f yielding trisaccharide 8a, and disaccharide 7a.