Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof:
wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocylyl group.
Type:
Grant
Filed:
June 27, 2003
Date of Patent:
August 17, 2004
Assignee:
Syngenta Limited
Inventors:
John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
Type:
Application
Filed:
February 6, 2004
Publication date:
August 12, 2004
Inventors:
Macklin Brian Arnold, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
Abstract: The present invention provides new trans-9,10-dehydroepothilone C and trans-9,10-dehydroepothilone D based derivative compounds, compositions and methods of inhibiting cellular hyperproliferation and/or stabilizing microtubules in vitro and of treatment of hyperproliferative diseases in vivo. Also disclosed are methods of making the compounds.
Type:
Application
Filed:
November 7, 2003
Publication date:
August 5, 2004
Inventors:
Yong Li, Kurt Sundermann, Li Tang, David Myles
Abstract: The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.
Type:
Application
Filed:
August 6, 2003
Publication date:
June 17, 2004
Inventors:
Francine Feirong Li, Kenneth S. Rehder, Michael Gordon Campbell, Celeste Patrice Viscardi, Jon-Paul Strachan, Zhengming Guo
Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
Type:
Application
Filed:
November 19, 2002
Publication date:
June 3, 2004
Inventors:
Frederick Earl Boyer, John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Susan Elizabeth Hagen, Michael James Lovdahl, Elizabeth Ann Lunney, Larry James Markoski, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
Abstract: Provided is a method of treating or ameliorating certain fibrotic diseases or other indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I:
Type:
Application
Filed:
October 23, 2003
Publication date:
May 20, 2004
Inventors:
Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
Abstract: It comprises a compound having antifungal activity as active principle, an inert core and a coating including said active principle, and is characterized in that said inert core has a particle size comprised between 50 and 600 &mgr;m, and in that said coating comprises a single layer obtained by spraying, on said inert core, a solution comprising a compound having antifungal activity, a hydrophilic polymer and a non-ionic surfactant.
The method consists in carrying out a coating, comprising a single layer, of the inert cores having a size between 50 and 600 &mgr;m, by means of the spraying of a solution composed by the antifungal agent, the hydrophilic polymer and the non-ionic surfactant, at a constant coating speed throughout the whole process; and a single drying step of said coating in the same apparatus.
Type:
Grant
Filed:
March 22, 2001
Date of Patent:
May 18, 2004
Assignee:
Liconsa Liberacion Controlada de Sustancias Activas,
S.A.
Abstract: The invention concerns compounds of formula (I)
wherein each of G1, G2 and G3 is CH or N; m is 1 or 2; R1 includes hydrogen, halogeno and (1-4C)alkyl; M1 is a group of the formula: NR2—L1—T1R3 in which R2 and R3 together form a (1-4C)alkylene group, L1 includes (1-4C)alkylene, and T1 is CH or N; A may be a direct link; M2 is a group of the formula: (T2R4)r—L2—T3R5 in which r is 0 or 1, each of T2 and T3 is CH or N, each of R4 and R5 is hydrogen or (1-4C)alkyl, or R4 and R5 together form a (1-4C)alkylene group, and L2 includes (1-4C)alkylene; M3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocyclic moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.
Type:
Grant
Filed:
March 8, 2001
Date of Patent:
May 4, 2004
Assignee:
Zeneca Limited
Inventors:
Alan Wellington Faull, Andrew Stocker, Colette Marie Mayo, John Preston
Abstract: Disclosed is a pharmaceutical composition for modulating immunity, which comprises a benzimidazole, represented by the following general formula (I), a 3H tautomer, an optically active enantiomer or a pharmaceutically acceptable acid-addition salt thereof wherein, R represents an alkyl group having 1 to 5 carbon atoms, a hydroxyphenyl group or a methoxyphenyl group.
Abstract: The present invention relates to a biphenylamidine derivative of the general formula (1):
or a pharmaceutically acceptable salt thereof, which is a novel compound functioning as a clinically applicable FXa inhibitor.
Abstract: This invention provides a method of treating a disease state in mammals that is alleviated by treatment with a protein kinase inhibitor, especially an ERK inhibitor, which method comprises administering a compound having the pharmacophoric features Grp1, Grp2 and Grp3: 1
Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
Type:
Application
Filed:
May 21, 2003
Publication date:
February 26, 2004
Applicant:
Millennium Pharmaceuticals, Inc.
Inventors:
Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
Abstract: Benzoyl derivatives of formula (I)
and their physiologically acceptable salts and solvates, in which R1, R2, R3, R4, R5 and R6 have the meanings indicated,
inhibit phosphodiesterase IV and can be used for the treatment of allergic diseases, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin diseases, inflammatory diseases, auto-immune diseases such as rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumoral growth or tumoral metastases, septicemia, memory defects, atherosclerosis and AIDS.
Type:
Grant
Filed:
January 9, 2002
Date of Patent:
February 24, 2004
Assignee:
Merck Patent GmbH
Inventors:
Rochus Jonas, Michael Wolf, Norbert Beier
Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
Type:
Grant
Filed:
April 4, 2001
Date of Patent:
February 17, 2004
Assignee:
Pharmacia Corporation
Inventors:
Michael S. South, Chun C. Ma, Kevin J. Koeller, Hayat K. Rahman, William L. Neumann
Abstract: The present invention makes available methods and reagents for inducing activation of a hedgehog pathway in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as a small molecule, in a sufficient amount to achieve a therapeutic result. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
Type:
Grant
Filed:
November 28, 2000
Date of Patent:
January 27, 2004
Assignee:
Curis, Inc.
Inventors:
Anthony David Baxter, Edward Andrew Boyd, Oivin M. Guicherit, Jeffrey Porter, Stephen Price, Lee Rubin
Abstract: Methods for treating cardiovascular and related diseases such as hypertrophy, hypertension, congestive heart failure, ischemia, ischemia reperfusion injuries in various organs, arrhythmia, and myocardial infarction, are described. The methods are directed to concurrently administering a compound such as pyridoxal-5′-phosphate, pyridoxamine, pyridoxal, or a 3-acylated pyridoxal analogue with a therapeutic cardiovascular compound.
Abstract: &bgr;-lactamases are the most widespread resistance mechanism to &bgr;-lactam antibiotics, such as penicillins and cephalosporins. In response to these enzymes, inhibitors have been introduced. Unfortunately, these inhibitors are also &bgr;-lactams, and resistance to them has developed rapidly. Consequently, the present invention provides a novel structure-based approach to inhibitors of these enzymes.
Abstract: Thiazolidinedione (TZD) and its pharmacologically active derivatives can be used in combination with agonists of glucagon-like peptide-1 (GLP-1), to treat non-insulin dependent diabetes mellitus, optionally with other therapies, by improving glycemic control while minimizing side effects, such as heart hypertrophy and elevated fed-state plasma glucose, which are associated with both TZD and GLP-1 monotherapies. Thus, the co-administration of TZD and GLP-1 helps regulate glucose homeostasis in Type II diabetic patients.
Type:
Grant
Filed:
April 24, 2001
Date of Patent:
December 9, 2003
Assignee:
Eli Lilly and Company
Inventors:
Fatima Emitsel Yakubu-Madus, Lawrence Edward Stramm, William Terry Johnson, Vignati Louis
Abstract: An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I):
wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, —NH—Q—R3 (R3 is a substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or —NH—R4 (R4 is a substituted or unsubstituted cycloalkyl group); R2 is a substituted or unsubstituted aryl group; one of Y and Z is ═CH—, and the other is ═N—, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.
Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
Type:
Grant
Filed:
October 30, 2000
Date of Patent:
November 25, 2003
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jeffrey O. Saunders, Daniel Elbaum, Perry M. Novak, Douglas Naegele, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Catharine Frank, Dean P. Stamos, William Walters, David Pearlman
Abstract: Compounds having the structure shown below 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:
Application
Filed:
August 19, 2002
Publication date:
November 13, 2003
Applicant:
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
Inventors:
Qun Li, Keith W. Woods, Gui-Dong Zhu, John P. Fischer, Jianchun Gong, Tongmei Li, Virajkumar Gandhi, Sheela A. Thomas, Garrick K. Packard, Xiaohong Song, Jason N. Abrams, Robert B. Diebold, Jurgen Dinges, Charles W. Hutchins, Vincent S. Stoll, Saul H. Rosenberg, Vincent L. Giranda
Abstract: The invention relates to 2,5-diazabicyclo[2.2.1]heptane derivatives, to pharmaceutical compositions containing them, and to methods for the treatment or prevention of disorders associated with a dysfunction of the nicotinic receptors utilizing them.
Abstract: Amide compounds represented by the formula:
wherein:
R1 is a moiety represented by the formula
where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting of CH2, O, and S, provided that at least one of X and Y is CH2, or X and Y together with the bond there-between form a cyclopropyl; are described. These compounds and pharmaceutical compositions containing them modulate and/or inhibit the activity of certain protein kinases and are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation.
Type:
Grant
Filed:
January 19, 2001
Date of Patent:
October 21, 2003
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Steven Lee Bender, Dilip Bhumralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney
Abstract: The compounds of formula I in which Ar1, A, R6, R7, R8 and Ar2 have the meanings as given in the description are novel effective bronchial therapeutics.
Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof:
wherein
R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate;
R2 is COOR5, C(═O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(═O)N(R5)R6 or NH(CHR5)mOH;
R3 is H or alkyl;
R4 is H, sybstituted or unsubstituted aryl, heteroaryl or alkyl;
R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1&bgr; protease activity in a mammal utilizing the compounds and compositions.
Type:
Grant
Filed:
April 3, 1996
Date of Patent:
September 23, 2003
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Roland E. Dolle, Denton W. Hoyer, Tina Morgan Ross, James M. Rinker, Stanley J. Schmidt, Mark A. Ator
Abstract: There is provided novel cinnamide derivatives of Formula I 1
Type:
Application
Filed:
May 31, 2002
Publication date:
September 4, 2003
Inventors:
Yong-Jin Wu, Li-Quang Sun, Jie Chen, Huan He, Alexandre L'Heureux, Pierre Dextraze, Jean-Paul Daris, Gene G. Kinney, Steven I. Dworetzky, Piyasena Hewawasam
Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
Type:
Grant
Filed:
November 28, 2000
Date of Patent:
September 2, 2003
Assignee:
Curis, Inc.
Inventors:
Jeffrey Porter, Oivin M. Guicherit, Lee Rubin, Anthony David Baxter, Edward Andrew Boyd, Stephen Price
Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII:
wherein Z1 is N or C—R9, Z2 is N or CH, and Z3 is N or C—Rx, provided that one of Z1 and Z3 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and Rx, R1, R2, R2′, R3, and R9 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
Type:
Grant
Filed:
September 14, 2001
Date of Patent:
August 26, 2003
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Robert Davies, Pan Li, Julian M. C. Golec, Jean-Damien Charrier, Ronald Knegtel, David Bebbington
Abstract: The invention relates to a method of treating a diabetic condition by administering a therapeutically effective amount of a histamine-3 receptor antagonist, including benzofuran and benzopyran derivatives of formula (I), aminoalkoxybiphenylcarboxamide compounds of formula (III), and aminoetherbiphenyl compounds of formula (IV) as described herein.
Type:
Application
Filed:
December 23, 2002
Publication date:
August 14, 2003
Inventors:
Arthur A. Hancock, Eugene N. Bush, Marlon D. Cowart, Peer B. Jacobson, Terry J. Opgenorth, Youssef Bennani
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 4, 2001
Date of Patent:
August 5, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Patrick Y. S. Lam, Charles G. Clark, John M. Fevig, Robert A. Galemmo, Qi Han, Irina C. Jacobson, Renhau Li, Donald J. P. Pinto, Ruth R. Wexler
Abstract: Methods and compositions for inhibiting or preventing spermatogenesis in a male mammal. Also disclosed are compounds and formulations for use in such methods.
Type:
Application
Filed:
November 25, 2002
Publication date:
July 31, 2003
Applicant:
Allergan Sales, Inc.
Inventors:
Elliott S. Klein, Yang-Dar Yuan, Roshantha A. Chandraratna
Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.