Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.
Type:
Grant
Filed:
March 11, 1999
Date of Patent:
September 26, 2000
Assignee:
Eli Lilly and Company
Inventors:
Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
Abstract: The present invention relates to compositions useful as cosmetic or therapeutic agents, as well as methods of their use. The compositions herein are particularly useful as coatings for mammalian nails. More particularly, the present invention relates to compositions which, when applied to mammalian nails exhibit long wear properties including excellent adhesion to the nail.
Type:
Grant
Filed:
May 1, 1998
Date of Patent:
September 26, 2000
Assignee:
The Procter & Gamble Company
Inventors:
Peter Christopher Ellingson, Edward Dewey Smith, III
Abstract: A process for preparing substantially single enantiomer d-threo-methylphenidate, proceeds by means of a classical salt resolution using (-)-menthoxyacetic acid.
Abstract: The invention relates to a process for the preparation of a fluorescent conjugate between a carrier molecule possessing at least one amino, hydroxyl, carboxyl and/or sulfhydryl group and a fluorophoric reagent possessing at least one functional group capable of reacting with said amino, hydroxyl, carboxyl and/or sulfhydryl group(s), which consists in bringing said carrier molecule and said fluorophoric reagent into contact with an aqueous solution of a water-soluble macrocycle.The invention further relates to the conjugates obtained by this process and to their use.
Abstract: A clear stick composition is disclosed that includes a solvent, a gelling agent, a plasticizing/solubilizing agent and a clarity/stability agent. The clarity/stability enhancing agent is preferably polyoxypropylene (10) butanediol (PPG-10 butanediol).
Type:
Grant
Filed:
January 11, 1999
Date of Patent:
September 12, 2000
Assignee:
Avon Products, Inc.
Inventors:
Ronald Matesevac, Jeffrey S. Graf, Philip Franco
Abstract: This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
Type:
Grant
Filed:
November 25, 1997
Date of Patent:
September 5, 2000
Assignee:
Dupont Pharmaceuticals Company
Inventors:
John Wityak, Chu-Biao Xue, Thais Motria Sielecki-Dzurdz, Richard Eric Olson, William Frank Degrado, Gary Avonn Cain, Douglas Guy Batt, Donald Pinto, Munir Alwan Hussain, Shaker Ahmed Mousa
Abstract: The present invention provides a process to prepare a pyridine-2,3-dicarboxylate derivative via the reaction of a dialkyl alkoxy(or alkylthio)oxalacetate with an appropriately substituted acrolein compound in the presence of an ammonia source and a solvent. The present invention also provides useful intermediate compounds of formula IV.
Abstract: Compounds analogous to thalidomide from the class comprising piperidine-2,6-diones are described, as are a method of preparing them and their use in drugs.
Type:
Grant
Filed:
January 29, 1998
Date of Patent:
August 29, 2000
Assignee:
Gruenenthal GmbH
Inventors:
Oswald Zimmer, Werner Winter, Stephan Wnendt, Kai Zwingenberger, Kurt Eger, Uwe Teubert
Abstract: The present invention relates to a pigment composition comprising an effective amount of an aqueous extract of coffee and at least one organic pigment. The pigment compositions are useful in preparing cosmetic formulations in which a true black color in the final product is needed. In particular, the pigment composition is useful in the preparation of eyeliner, lash coloring, and hair dyes or rinses.
Abstract: A .beta.,.gamma.-dihydropolyprenyl alcohol derivative having the formula: ##STR1## wherein n is an integer of 5 to 7 and R is hydrogen, a lower alkyl group or an aliphatic or aromatic acyl group, is new and useful as a prophylactic therapeutic agent for human and animal immuno-deficiency deseases and phylactic agent against human and animal infectious deseases. Another disclosed polyprenyl compound is also useful as the same agent.
Abstract: The present invention teaches method for culturing nematode pesticidal compositions, to produce at a high yield, and generate biotic compositions that are effective as insecticides with high pesticidal activity and preventive effects.
Abstract: A process for the preparation of cyclic esters of the general formula: ##STR1## in which m is an integer from 6-14 and n is an integer from 2-6, which comprises heating a dicarboxylic acid bis(glycol) ester of the general formula:HO--(CH.sub.2).sub.n --O--CO--(CH.sub.2).sub.m --CO--O--(CH.sub.2).sub.n --OH, formula IIin which m and n are as defined above,(b) optionally, up to 100% by weight, based on the weight of ester II, of esters of the general formula:H[O--(CH.sub.2).sub.n --O--CO--(CH.sub.2).sub.m --CO--].sub.x --O--(CH.sub.2).sub.n --OH, formula IIIH[O--(CH.sub.2).sub.n --O--CO--(CH.sub.2).sub.m CO--]X--OH and/orformula IVHO--CO--(CH.sub.2).sub.m --CO--[--O--(CH.sub.2).sub.n O--CO--(CH.sub.2).sub.m --CO--].sub.x --OH, formula Vin which m and n are as defined previously and x is an integer >1, and(c) a glycol of the general formula:HO--(CH.sub.2).sub.n --OH, formula VIin which n has the same numerical value as in formula I-V,(d) an inert high-boiling reaction medium, and(e) a catalyst.
Type:
Grant
Filed:
March 3, 1999
Date of Patent:
August 22, 2000
Assignee:
Huels Aktiengesellschaft
Inventors:
Clemens Osterholt, Josef Metz, Guenther Koehler
Abstract: A topical barrier composition contains a, synthetic, polymeric, hydrophobic silicone material, a bentonite component, zinc oxide, water and an unctuous carrier base for the other ingredients of the composition. The composition provides a barrier function protecting mammalian epidermis against external insults such as hyperhydration and maceration from any cause with an intended use for protection against extended periods of exposure to urine and feces.
Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell--cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.
Type:
Grant
Filed:
December 22, 1998
Date of Patent:
August 8, 2000
Assignee:
Hoffman-La Roche Inc.
Inventors:
Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
Abstract: 2-Phenylpyridines I ##STR1## wherein X is a chemical bond, 1,2-ethynediyl or optionally substituted --(CH.sub.2).sub.1-3 --, --O--(CH.sub.2).sub.1-2 --, --s--(CH.sub.2).sub.1-2 --, --CH.sub.2 --O--CH.sub.2 --, --CH.sub.2 --S--CH.sub.2 -- or --CH.dbd.CH--;Y is oxygen or sulfur;Z.sup.1 is oxygen, sulfur or --N(R.sup.7)--;Z.sup.2 is oxygen, sulfur or --N(R.sup.8)--;R.sup.1, R.sup.2, R.sup.7 and R.sup.8 independently of one another are hydrogen, optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or heterocyclyl; orR.sup.1 and R.sup.2 or R.sup.7, or R.sup.2 and R.sup.8 together are optionally substituted --(CH.sub.2).sub.2-5 -- or --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --, orR.sup.1 and R.sup.2 together are optionally substituted 1,2-phenylene;R.sup.3 is cyano, halogen, alkyl, haloalkyl, alkoxy or haloalkoxy;R.sup.4 and R.sup.5 are hydrogen or halogen;R.sup.
Type:
Grant
Filed:
August 4, 1998
Date of Patent:
August 8, 2000
Assignee:
BASF Aktiengesellschaft
Inventors:
Cyrill Zagar, Peter Schafer, Gerhard Hamprecht, Elisabeth Heistracher, Markus Menges, Olaf Menke, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
Abstract: The invention provides compositions containing dermaphile oils and methods for their use. Preferred composition contain Purcellin Oil and are useful in treating a wide variety of adverse skin conditions, including disorders manifesting inflammatory and non-inflammatory symptoms and having a variety of etiologies. The compositions are especially useful in treating psoriasis, eczema, acne, surgical scars and sunburn, but are also useful in treating cuts, insect bites, pruritis, cold sores and dry skin. Methods for the use of these compositions are also provided.
Abstract: A compound of formula (I): ##STR1## wherein Ar is optionally substituted phenyl or optionally substituted 5-or 6-membered heterocyclic ring containing from 1 to 3 heteroatoms individually selected from nitrogen, oxygen and sulfur atoms, and at least one unsaturation (double bond) between adjacent atoms in the ring, said heterocyclic ring being optionally fused to a benzene ring; or an acid addition salt, quaternary ammonium salt or N-oxide derived therefrom, an insecticidal, acaricidal or nematicidal composition comprising a compound of formula (I) and a suitable carrier or diluent therefor, a method of combating and controlling insect, acarine or nematode pests at a locus which comprises treating the pests or the locus of the pests with an effective amount of a compound of formula (I) or a composition as hereinbefore described.
Type:
Grant
Filed:
November 13, 1997
Date of Patent:
July 25, 2000
Assignee:
Zeneca Limited
Inventors:
Christopher John Urch, Roger Salmon, Christopher Richard Ayles Godfrey
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved in 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:
Grant
Filed:
June 27, 1997
Date of Patent:
July 25, 2000
Assignee:
Vertex Pharmaceuticals, Inc.
Inventors:
Francesco Gerald Salituro, Guy W. Bemis, Jeremy Green, James L. Kofron
Abstract: The invention relates to novel racemic and optically active trans apovincaminic acid ester derivatives of formula (I), ##STR1## wherein R means hydrogen or a group (a), wherein Z stands for C.sub.1-4 alkyl, optionally substituted aryl, aralkyl, heteroaryl or 14-eburnameninyl group; and n is an integer of 2, 3 or 4, as well as therapeutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions, and in addition, to a method of treatment. The novel compounds of Formula (I) exhibit particularly antioxidant, antiischemic as well as antiamnesic effects and are useful for inhibiting lipid peroxidation and for protection from or treatment of ischemia and amnesia as well as for treating various degenerative neurological diseases, e.g. Alzheimer's disease.
Type:
Grant
Filed:
June 9, 1998
Date of Patent:
July 25, 2000
Assignee:
Richter Gedeon Vegyeszeti GmbH
Inventors:
Csaba Szantay, Istvan Moldvai, Andras Vedres, Maria Incze, Janos Kreidl, Laszlo Czibula, Maria Farkas Nee Kiriak, Ida Deutsch Nee Juhasz, Aniko Gere, Margit Pellionisz Nee Paroczai, Erzsebet Lapis, Andras Szekeres, Maria Zajer Nee Balazs, Adam Sarkadi, Ferenc Auth, Bela Kiss, Egon Karpati, Sandor Farkas
Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.
Type:
Grant
Filed:
March 11, 1999
Date of Patent:
July 18, 2000
Assignee:
Eli Lilly and Company
Inventors:
Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley