Abstract: Aspects of the present invention are directed towards compounds of Formula I for the treatment of human erectile disorders including erectile dysfunction in men.
Abstract: Compounds of the formula (I), in which M, A1, A2, K1 and K2 have the meanings indicated in the description are novel active tryptase inhibitors.
Abstract: The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
Type:
Application
Filed:
September 3, 2002
Publication date:
March 13, 2003
Inventors:
Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, David Lee Varie
Abstract: Disclosed are novel compounds of the formula 1
Type:
Application
Filed:
October 15, 2001
Publication date:
March 6, 2003
Inventors:
Robert G. Aslanian, Neng-Yang Shih, Pauline C. Ting, Michael Y. Berlin, Stuart B. Rosenblum, Kevin D. McCormick, Wing C. Tom, Christopher W. Boyce, Pietro Mangiaracina, Mwangi W. Mutahi, John J. Piwinski
Abstract: The present invention relates to novel sulfoxide and bis-sulfoxide compounds, compositions comprising sulfoxide and bis-sulfoxide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
Type:
Application
Filed:
October 11, 2001
Publication date:
January 30, 2003
Inventors:
Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
Abstract: This invention relates to the preparation of N,N′-carbonyldiazoles in a particularly advantageous manner by reacting corresponding azolide salts with phosgene in an aromatic compound or an ether as solvent. The azolide salts are preferably prepared by a novel process from an azole that is reacted with a compound of the formula M′R7 or MgR8Z′ in the presence of a solvent.
Type:
Application
Filed:
August 15, 2002
Publication date:
January 16, 2003
Inventors:
Johannes Scherer, Alexander Klausener, Robert Sollner
Abstract: In one embodiment, the invention provides a polymer comprising imidazole ring units having nitrogen at the 1 and 3 positions of the ring; a carbon at each of the 2, 4 and 5 positions of the ring; and radical substituents G1 and G2 carried at the 4 and 5 positions. G1 and G2 are each independently selected from cyano, substituents derived from cyano, and substituents which replace cyano. The polymers formed by at least two of the cyclic imidazole units. In another embodiment, the invention provides new imidazole compounds usable as monomers to form the polymers. In still another embodiment, the invention provides a method for using the polymers as a coupling/activator for synthon synthesis.
Type:
Grant
Filed:
July 26, 2001
Date of Patent:
November 19, 2002
Assignee:
The Regents of the University of Michigan
Inventors:
Paul G. Rasmussen, Sarah E. Reybuck, David M. Johnson, Richard G. Lawton
Abstract: The invention encompasses improved polyamides for binding to specific nucleotide sequences in the minor groove of double stranded DNA. The 3-hydroxy-N-methylpyrrole/N-methylpyrrole carboxamide pair specifically recognizes the T·A base pair, while the N-methylpyrrole/3-hydroxy-N-methylpyrrole pair recognizes A·T nucleotide pairs. Similarly, an N-methylimidizole/N-methylpyrrole carboxamide pair specifically recognizes the G·C nucleotide pair, and the N-methylpyrrole/N-methylimidizole carboxamide pair recognizes the C·G nucleotide pair.
Abstract: Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
Type:
Application
Filed:
February 21, 2002
Publication date:
October 24, 2002
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
Abstract: Compounds of formula (I) which are optionally substituted 2-(&ohgr;,&ohgr;-diarylalkyl)-4,5-dihydro-1H-imidazoles and 2-(&ohgr;,&ohgr;-diarylalkyl)-1,4,5,6-tetrahydropyrimidines and salts thereof with inorganic and organic acids have interesting pharmacological properties. Thus, the compounds are useful in the treatment of type 2 diabetes.
Type:
Application
Filed:
November 9, 2001
Publication date:
September 19, 2002
Inventors:
Henrik Sune Andersen, Palle Jakobsen, Peter Madsen
Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
Type:
Grant
Filed:
July 28, 1998
Date of Patent:
September 10, 2002
Assignee:
G.D. Searle & Co.
Inventors:
Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
Abstract: The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two substituted histidine residues, or similar compounds, linked to a lipophilic moiety. The lipids form a complex when mixed with polyanions such as nucleic acids or peptides. The complexes permit efficient transfer of polyanions into cells, usually without significant toxicity to the cells.
Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor antagonists, and which are represented by Formula I: 1
Abstract: The invention relates to the use of heterocyclic quaternary polyammonium polymers as protective agent for keratin fibres, to cosmetic compositions using them and to method for treating hair with the aid of these polymers.
Abstract: A photo-induced phase transition organic material is composed of a diheteroarylethene-based compound within which the photo-chromic reaction occurs in the crystalline state. The diheteroarylethene-based compound of the present invention reversibly changes in color with light irradiation and also changes in phase from the open-ring form in the crystalline state to the closed-ring form in the crystalline state, or from the closed-ring form in the crystalline state to the open-ring form in the crystalline state via the liquid state, and can be applicable to optical recording media, display panels, sensors, optical switch devices and the like, by taking advantages of its variations in color with light irradiation and also its changes in physical property, such as the refractive index and the permeability, with its changes in phase.
Type:
Application
Filed:
August 13, 2001
Publication date:
January 17, 2002
Applicant:
JAPAN SCIENCE AND TECHNOLOGY CORPORATION
Abstract: The present application describes nitrogen containing heteroaromatics with ortho-substituted P1's and derivatives thereof of formula I:
or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D is substituted ortho to G on E and may be CH2NH2, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
December 21, 1998
Date of Patent:
August 7, 2001
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Robert A. Galemmo, Jr., Lori L. Bostrom, Donald J. P. Pinto, Karen A. Rossi
Abstract: The present invention relates to compounds, compositions, and methods which are useful for the prevention and treatment of adverse health, skin, hair, and oral conditions. The compounds, compositions, and methods are also widely applicable for use in health, skin, hair, oral, beauty, and personal care applications.
In particular, the present invention relates to compounds having the structure:
and the tautomers, acceptable salts, and biohydrolyzable amides, esters, and imides thereof, wherein A, Q, n, P, L1, L2, L3, L4, Z, X, B1, and B2 are defined herein.
Type:
Grant
Filed:
February 16, 2000
Date of Patent:
April 3, 2001
Assignee:
The Procter & Gamble Company
Inventors:
John McMillan McIver, Todd Laurence Underiner, Timothy Bates