Plural 1,3-diazoles Patents (Class 548/312.7)
  • Publication number: 20030092741
    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.
    Type: Application
    Filed: August 9, 2002
    Publication date: May 15, 2003
    Inventors: Duane D. Miller, Seoung-Soo Hong
  • Publication number: 20030083344
    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.
    Type: Application
    Filed: September 20, 2002
    Publication date: May 1, 2003
    Inventor: Thomas Martin
  • Publication number: 20030083352
    Abstract: The invention provides a method for synthesis of compounds of formula 1
    Type: Application
    Filed: July 25, 2002
    Publication date: May 1, 2003
    Applicant: Pfizer Inc.
    Inventor: Christopher J. Helal
  • Patent number: 6545162
    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.
    Type: Grant
    Filed: July 22, 1999
    Date of Patent: April 8, 2003
    Assignee: California Institute of Technology
    Inventors: Peter B. Dervan, Eldon E Baird
  • Publication number: 20030055086
    Abstract: Compounds of formula (I): 1
    Type: Application
    Filed: August 12, 2002
    Publication date: March 20, 2003
    Inventors: Bernard P. Roques, Marie-Claude Fournie-Zaluski, Nicolas Inguimbert, Herve Poras, Elizabeth Scalbert, Caroline Bennejean, Pierre Renard
  • Publication number: 20030050311
    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
  • Publication number: 20030045519
    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
  • Publication number: 20030022865
    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
  • Publication number: 20030013891
    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
  • Publication number: 20030013873
    Abstract: Secondary amines of the formula 1
    Type: Application
    Filed: June 19, 2002
    Publication date: January 16, 2003
    Inventors: Peter Neumann, Johann-Peter Melder, Christoph Benisch, Arthur Hohn, Joachim Pfeffinger
  • Publication number: 20020183374
    Abstract: The present invention relates to hydantoins of formula I, 1
    Type: Application
    Filed: March 8, 2002
    Publication date: December 5, 2002
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Klaus Burger, Alexander Golubev, Sergej Ossipov
  • Patent number: 6482954
    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
  • Patent number: 6472537
    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.
    Type: Grant
    Filed: August 11, 1999
    Date of Patent: October 29, 2002
    Assignee: California Institute of Technology
    Inventors: Eldon E. Baird, Peter B. Dervan
  • Publication number: 20020156082
    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
  • Publication number: 20020132812
    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
  • Patent number: 6448286
    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
  • Patent number: 6437121
    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.
    Type: Grant
    Filed: April 25, 2000
    Date of Patent: August 20, 2002
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventors: Kuei-Ying Lin, Mark D. Mattuecci
  • Publication number: 20020094453
    Abstract: A metal coordination compound suitable as an organic material for a luminescent device is represented by the following formula (1): 1
    Type: Application
    Filed: November 29, 2001
    Publication date: July 18, 2002
    Inventors: Takao Takiguchi, Shinjiro Okada, Akira Tsuboyama, Koji Noguchi, Takashi Moriyama, Jun Kamatani, Manabu Furugori
  • Publication number: 20020091147
    Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor antagonists, and which are represented by Formula I: 1
    Type: Application
    Filed: November 13, 2001
    Publication date: July 11, 2002
    Inventor: Alam Jahangir
  • Patent number: 6416770
    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.
    Type: Grant
    Filed: September 21, 2000
    Date of Patent: July 9, 2002
    Assignee: L'Oréal S.A.
    Inventors: Madeleine Leduc, Hervé Richard, Alain Lagrange
  • Publication number: 20020037896
    Abstract: Substituted N-substituted alkoxyphenyl compounds, compositions containing them, and methods of making and using them.
    Type: Application
    Filed: August 6, 2001
    Publication date: March 28, 2002
    Inventors: Michael Bogenstaetter, Wenying Chai, Annette K. Kwok
  • Publication number: 20020007072
    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
    Inventor: Masahiro Irie
  • Patent number: 6271237
    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
  • Patent number: 6211186
    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