Sulfonamides (i.e., Q-(o=)s(=o)-n, Wherein Q Is A Substituent And Wherein Any Substituent Attached To The Nitrogen Will Be Referred To As E) Patents (Class 514/601)
Abstract: A composition in the form of an ultrafine oil-in-water emulsion in which the mean size of the oil globules ranges from 50 nm to 1000 nm containing a haloalkynyl derivative, preferably 3-iodo-2-propynyl butylcarbamate.
Abstract: The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
Type:
Grant
Filed:
January 23, 2001
Date of Patent:
February 25, 2003
Assignee:
Eli Lilly and Company
Inventors:
Macklin Brian Arnold, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
Abstract: This invention provides a method for treating or preventing arrhythmias in a human subject comprising the administration of an effective amount of a calcium/calmodulin-dependent protein kinase inhibitor. Also provided are pharmaceutical compositions comprising a calcium/calmodulin-dependent protein kinase inhibitor and a pharmaceutically acceptable carrier and methods for identifying agents useful for the treatment of arrhythmias.
Type:
Grant
Filed:
January 30, 1998
Date of Patent:
February 11, 2003
Assignee:
The Board of Trustees of the Leland Stanford Jr.
University
Inventors:
Mark E. Anderson, Andrew P. Braun, Howard Schulman, Ruey J. Sung
Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; 1
Abstract: The invention provides a COX-2 inhibitor or a pharmaceutically acceptable derivative thereof for use in the treatment of a disorder ameliorated by a gastroprokinetic.
Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
February 19, 2002
Publication date:
January 16, 2003
Applicant:
G.D. Searle & Co.
Inventors:
John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
Abstract: Compounds of the formula:
are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.
Type:
Grant
Filed:
March 15, 2000
Date of Patent:
January 14, 2003
Assignee:
Axys Pharmaceuticals, Inc.
Inventors:
Ann M. Buysse, Rohan V. Mendonca, James T. Palmer, Zong-Qiang Tian, Shankar Venkatraman
Abstract: Medical devices, compositions and methods for treating or preventing atherosclerotic plaque rupture are disclosed. Specifically, medical devices that deliver to a treatment site metalloproteinase inhibitors (MMPI) are disclosed. The medical devices include catheters, guide wires, vascular stents, micro-particles, electronic leads, probes, sensors, drug depots, transdermal patches, and vascular patches. Representative MMPIs included zinc chelators, urea derivatives, caprolactone-based inhibitors, phoshoinamides, piperazines, sulfonamides, tertiary amines, carbamate derivatives, mercaptoalcohols, mecaptoketones, antimicrobial tertracyclines, non-antimicrobial tetracyclines, and derivatives and combinations thereof. In one embodiment a self-expanding vascular stent is coated with at least one MMPI and deployed at a site within an artery where vulnerable plaque has been identified.
Abstract: The present invention relates to an anti-inflammatory eye drop comprising a drug selectively inhibiting COX-2, selected from the group consisting of etodolac, N-(2-(cyclohexyloxy)-4-nitrophenyl) methane-sulfonamide and meloxicam, which only slightly damages corneal epithelium and conjunctiva and which is excellent in the anti-inflammatory effect.
Abstract: Compounds of the general formula I are provided:
and pharmaceutically acceptable salts thereof, wherein,
Z is a chemical species or Ri capable of binding at a primary specificity site of a protease;
Y is a chemical species reactive to a specific class of protease;
each of R2, R3, R5 and R7 is independently selected from the group consisting hydrogen, alkyls, aryls, substituted aryls, alkylaryls and arylalkyls;
R4 and R6 are independently selected from the group consisting of:
(a) H, alkyl, aryl, arylalkyl, alkylaryl, substituted derivatives thereof, and Ri;
(b) —C(O)OH and derivatives thereof, said derivatives selected from the group consisting of —C(O)OQ, —C(O)NRYRZ, —C(O)[NHCHRi(q)C(O)]qOQ, and —C(O)[NHCHRi(q)C(O)]qNRYRZ; and
(c) —CHRiNH2 and derivatives thereof, said derivatives selected from the group consisting of —CHRiNHW, —CHRiNHC(O)OQ, —CHRiNHC(O)R, —CHRiNHC(O)NRYRZ, —CHRiNHC(O)[NHCHRi(q
Abstract: The present invention provides a compound represented by the formula:
wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula:
wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents,
and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating disease
Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives.
Type:
Application
Filed:
May 24, 2002
Publication date:
December 12, 2002
Inventors:
Robert M. Burk, Mark Holoboski, Mari F. Posner
Abstract: The invention relates to novel pesticidally active compounds of the general formula I
as well as possible isomers and mixtures of isomers thereof,
wherein
n is a number zero or one; and
R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene;
R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring;
R4, R5, R6 and R7 are identical or different and are ea
Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.
Type:
Application
Filed:
January 25, 2002
Publication date:
November 7, 2002
Inventors:
Yong-Qian Wu, Sergei Belyakov, Gregory S. Hamilton, David Limburg, Joseph P. Steiner, Mark Vaal, Ling Wei, Douglas Wilkinson
Abstract: The efficacy of amide- and ester-linked local anesthetics is increased by administering methanesulfonamide compounds (for example, ibutilide and sotalol) as adjuvants with the local anesthetics. The effectiveness of these compounds as adjuvants is further increased by the concomitant administration of epinephrine. Pharmaceutical compositions comprising an amide- and ester-linked local anesthetic and a methanesulfonamide compound, which may further include epinepherine, are also provided.
Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
Type:
Grant
Filed:
March 21, 2000
Date of Patent:
October 29, 2002
Assignee:
Genentech, Inc.
Inventors:
Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
Abstract: The present invention relates to compounds that are inhibitors of interleukin-1&bgr; converting enzyme that have the Formula (I). This invention also relates to a method of treatment of stroke, reperfusion injury, Alzheimer's disease, shigellosis, inflammatory diseases, and septic shock and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1&bgr; converting enzyme.
Type:
Application
Filed:
September 25, 2001
Publication date:
October 24, 2002
Applicant:
Warner-Lambert Company
Inventors:
Hans P. Albrecht, Hamish John Allen, Kenneth Dale Brady, William Glen Harter, Catherine Rose Kostlan, Bruce David Roth, Nigel Walker
Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
Type:
Grant
Filed:
March 15, 2000
Date of Patent:
September 24, 2002
Assignee:
AXYS Pharmaceuticals, Inc.
Inventors:
Clifford M. Bryant, Barry A. Bunin, Erica A. Kraynack, John W. Patterson
Abstract: A series of substituted sulfonamide derivatives have been prepared and may be used to treat antiviral infections, especially infections caused by orthopoxviruses.
Abstract: A pesticidal composition comprising the pesticidal ingredient, which is solid at room temperature and has a grain size of 30 &mgr;m or less in volume median diameter, and an organic foaming agent has a high vaporization rate and show a high pest-controlling effect.
Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I):
wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.
Abstract: The present invention relates to compositions and methods for treating equines, such as horses, afflicted with equine protozoal myeloencephalitis or EPM. The therapeutic compositions comprise a combination of pyrimethamine and a sulfonamide, preferably, sulfadiazine, in the absence of known therapeutic amounts of trimethoprim.
Abstract: The present invention relates to acetylenic aryl sulfonamide thiols which act as inhibitors of TNF-&agr; converting enzyme (TACE). The compounds of the present invention are useful in disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
Abstract: This invention relates to the use of EP2 receptor subtype selective prostaglandin E2 agonists to augment bone mass including the prevention and treatment of skeletal disorders in mammals, including humans.
Type:
Grant
Filed:
June 11, 1999
Date of Patent:
July 30, 2002
Assignee:
Pfizer Inc.
Inventors:
Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L Rosati, David D. Thompson
Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.
Type:
Application
Filed:
December 5, 2001
Publication date:
June 27, 2002
Inventors:
Prabha N. Ibrahim, Robert Jiang, Christopher Morrison, Kevin Shenk, Jeff A. Zablocki, Richard Lawn
Abstract: A palatable antimicrobial drug concentrate comprising: (a) a sulfonamide and/or sulfonamide salt in aqueous solution; (b) a 2,4-diaminopyrimidine in stable suspension within said solution; and (c) a suspending agent. The invention has a long room temperature shelf life and is sufficiently stable to be administered via the drinking water of animals.
Type:
Grant
Filed:
February 12, 2001
Date of Patent:
June 25, 2002
Assignee:
Pharmaceutical Solutions, Inc.
Inventors:
Michael A. Strobel, William A. Soderlund, Jr.
Abstract: The invention relates to a method of preventing or treating cartilage damage by administering a GABA analog such as, for example, a compound of Formula 1
Type:
Application
Filed:
September 14, 2001
Publication date:
June 13, 2002
Inventors:
Denis Schrier, Howard Glenn Welgus, David Juergen Wustrow
Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),4(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),ll(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.
Type:
Application
Filed:
December 14, 2001
Publication date:
June 13, 2002
Inventors:
Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),14(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.
Type:
Grant
Filed:
February 23, 1999
Date of Patent:
May 28, 2002
Assignee:
MCW Research Foundation
Inventors:
Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
March 5, 2001
Publication date:
May 2, 2002
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z), 8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),14(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.
Type:
Application
Filed:
December 14, 2001
Publication date:
April 25, 2002
Inventors:
Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
Abstract: The invention provides a method of inhibiting tumor growth in a mammal, by administering to the mammal composition containing methylol-containing compound. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death by apoptosis.
Type:
Application
Filed:
December 6, 2000
Publication date:
April 25, 2002
Inventors:
Paul Calabresi, James Darnowski, James Costin
Abstract: The present invention relates to an ant or yellow jacket bait that is particularly effective for controlling carpenter ants. The bait is comprised mostly of sugars in a viscous and fluid form that may be readily dispensed into an ant station at room temperatures, and provides a moist, sweet surface that is attractive to ants.
Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
Type:
Application
Filed:
June 29, 2001
Publication date:
February 7, 2002
Inventors:
Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compounds and the compositions and methods that utilize them can be used, either alone or in conjunction with a neurotrophic factor, such as nerve growth factor, to promote repair of neuronal damage caused by disease or physical trauma.
Type:
Application
Filed:
June 27, 2001
Publication date:
January 31, 2002
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Patricia McCaffrey, Perry M. Novak, Michael Mullican
Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of a disorder mediated by inhibiting plasma renin activity.
Abstract: A pharmaceutical composition for the prophylaxis and therapy of brain tissue impairment, which contains, as an active ingredient, a compound of the following formula (I)
wherein R1 represents an alkyl group having 1-4 carbon atoms or an aryl group having 6-10 carbon atoms which is optionally substituted; R2 and R3 may be the same or different and each represents hydrogen or an alkyl group having 1-4 carbon atoms or R2 and R3 may jointly form a ring having 3-7 carbon atoms; and R4 represents a lower alkyl group which is optionally substituted by aryl, cycloalkyl, or aromatic heterocyclic residue, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
September 19, 2000
Date of Patent:
January 29, 2002
Assignee:
Senju Pharmaceutical Co., Ltd.
Inventors:
Mitsuyoshi Azuma, Yukuo Yoshida, Yuji Sakamoto, Jun Inoue
Abstract: This invention provides a method for treating and preventing neurological disorder such as Alzheimer's disease, and for promoting wound healing comprising administering a compound characterized as being a matrix metalloproteinase inhibitor.
Type:
Grant
Filed:
March 19, 1999
Date of Patent:
January 22, 2002
Assignee:
Warner-Lambert Company
Inventors:
Thomas Michael Andrew Bocan, Peter Alan Boxer, Joseph Thomas Peterson, Jr., Denis Schrier, Andrew David White
Abstract: Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. Many other phenoxyisobutyric acid derivatives as well as certain other compounds as set out in this disclosure also have been found to inhibit the nonenzymatic glycation of proteins. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences.