Patents Examined by Philip I. Datlow
  • Patent number: 5585374
    Abstract: Amide derivatives of formula (I) and their pharmaceutically acceptable salts (where a and b each represent 0, 1, 2 or 3 such that a+b=0, 1, 2 or 3, the dotted line represents an optional double bond, A is an optionally substituted C.sub.1-2 -alkylene chain, R is mono or bicyclic aryl or heteroaryl radical, R.sup.1 is hydrogen or lower alkyl, R.sup.2 is an aryl, aralkyl, heteroaryl or heteroarylalkyl and --CONR.sup.3 R.sup.4 represents a specified amide group) are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics.
    Type: Grant
    Filed: February 1, 1995
    Date of Patent: December 17, 1996
    Assignee: John Wyeth Brother, Limited
    Inventors: Ian A. Cliffe, Alan C. White
  • Patent number: 5585376
    Abstract: The present invention relates to compounds of general formula (I) ##STR1## and physiologically acceptable salts thereof wherein the group NR.sub.1 R.sub.2 represents a 5-7 membered saturated heterocyclic ring which may be substituted by one or two methyl groups; R.sub.3 is C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or phenyl optionally substituted by 1 or 2 halogen atoms; R.sub.4 is phenyl or phenyl substituted by one or two groups selected from the group consisting of halogen, C.sub.1-4 alkyl, trifluoromethyl, trifluoromethoxy or (CH.sub.2).sub.n R.sub.5 wherein n is zero or 1 and R.sub.5 represents C.sub.1-4 alkoxy, hydroxy, nitro, cyano, CO.sub.2 R.sub.6, S(O).sub.p CH.sub.3, NR.sub.7 R.sub.8, CONR.sub.7 R.sub.8, SO.sub.2 NR.sub.7 CO(C.sub.1-4)alkyl, tetrazolyl, carboxamidotetrazolyl, or a 3-trifluoromethyl 1,2,4-triazolyl; R.sub.6 is hydrogen, C.sub.1-4 alkyl or benzyl; R.sub.7 is hydrogen or C.sub.1-4 alkyl, R.sub.8 is hydrogen, C.sub.1-4 alkyl, SO.sub.2 CH.sub.3 or SO.sub.2 CF.sub.3, X represent hydrogen, C.
    Type: Grant
    Filed: October 30, 1995
    Date of Patent: December 17, 1996
    Assignee: Glaxo Wellcome Inc.
    Inventors: Harry Finch, Pritom Shah, Robin A. E. Carr
  • Patent number: 5585489
    Abstract: Triphendioxazine compounds corresponding to the formula (1) ##STR1## in which Z is a radical of the formula (2) ##STR2## in which Y.sup.1 and Y.sup.2 each vinyl .beta.-hydroxyethyl or an ethyl radical which contains a substituent which can be eliminated under alkaline conditions in the .beta.-position, and in which Y.sup.1 and Y.sup.2 are not simultaneously .beta.-hydroxyethyl, W.sup.1 and W.sup.2 are both allyene having 2 to 6 carbon atoms, A is a covalent bond of a group of the formula --B.sup.1 --N(R.sup.3)--, in which R.sup.3 has one of the meanings of R.sup.1 and B.sup.1 is an aliphatic or aromatic bridge member, and in which the group--N(R.sup.1) --B.sup.1 --N(R.sup.3)-- can also be in total a bivalent saturated heterocyclic radical, and Z.sup.0 is hydrogen or a group of the formula (4) ##STR3## in which A.sup.0 is a covalent bond or a radical or the formula --N(R.sup.4)--B.sup.2 -- having the meaning corresponding to the above formula --B.sup.1 (NR.sup.3)-- are described.
    Type: Grant
    Filed: May 4, 1995
    Date of Patent: December 17, 1996
    Assignee: Hoechst AG
    Inventors: Werner H. Russ, Christian Schumacher
  • Patent number: 5583131
    Abstract: Polyamine macrocyclic compounds, e.g. of 10 to 15 ring members and 3 to 6 ring amine nitrogens, linked through methylene groups to an aromatic moiety, show high selective activity against HIV.
    Type: Grant
    Filed: August 18, 1994
    Date of Patent: December 10, 1996
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Gary J. Bridger, Sreenivasan Padmanbhan, Renato T. Skerlj, David M. Thornton
  • Patent number: 5583133
    Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.
    Type: Grant
    Filed: August 4, 1995
    Date of Patent: December 10, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Paul Hadvary, Kurt Hilpert, Klaus M uller, Ludvik Labler, G erard Schmid, Thomas B. Tschopp, Hans P. Wessel, Beat Wirz
  • Patent number: 5583130
    Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such bezno-fused lactams as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: December 10, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Bochis, Michael H. Fisher, Robert J. Devita, William R. Schoen, Matthew J. Wyvratt
  • Patent number: 5583156
    Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle ribonic acid or a topically effective salt thereof, or ribonolactone.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 10, 1996
    Assignee: Tristrata Technology Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5580902
    Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle ethyl pyruvate.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Tristrata Technology, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5578644
    Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle isocitric acid or a topically effective salt thereof.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 26, 1996
    Assignee: Tristrata Technology, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5576315
    Abstract: The present invention provides dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: August 1, 1995
    Date of Patent: November 19, 1996
    Assignee: G.D. Searle & Co.
    Inventors: E. Ann Hallinan, Timothy J. Hagen, Robert K. Husa, Sofya Tsymbalov, Jean-Pierre Van Hoeck, Albert C. Lee
  • Patent number: 5574067
    Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle gluconic acid or a topically effective salt thereof or gluconolactone.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 12, 1996
    Assignee: Tristrata Technology, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5574031
    Abstract: Compounds of general formula (I) are useful for treating mental disorders, wherein R.sub.1 and R.sub.2 are the same or different and selected from hydrogen or lower alkyl; Ar are the same or different and selected from pyridyl and phenyl groups, n is 1 or 2, X is nitrogen or methine. When X is nitrogen, Y is methylene. When X is methine, Y is selected from nitrogen or oxygen. A is selected from carboxylic derivatives. The pharmacologically active salts of formula (I) are also embraced.
    Type: Grant
    Filed: January 31, 1995
    Date of Patent: November 12, 1996
    Assignee: Pharmacia Aktiebolag
    Inventors: Lisbeth Abramo, Torbj orn Lundstedt, Curt Nordvi, Knut G. Olsson, Martin Brodszki
  • Patent number: 5574035
    Abstract: A novel compound and method for making and using compositions containing S--(--)-3-morpholino-4-(3-tert-butylamino-2-hydroxypropoxy)-1,2,5 thiadiazole hemihydrate useful for administration to a subject particularly for topical administration as a pharmaceutical agent for treating known conditions and disorder.
    Type: Grant
    Filed: October 7, 1994
    Date of Patent: November 12, 1996
    Inventor: Markku Per alampi
  • Patent number: 5571837
    Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle saccharic acid or a topically effective salt thereof, or saccharolactone.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 5, 1996
    Assignee: Tristrata Technology Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5571908
    Abstract: The invention comprises new compositions of matter, which are iron, manganese, cobalt or ruthenium complexes of porphyrins having hydrogen, haloalkyl or haloaryl groups in meso positions, two of the opposed meso atoms or groups being hydrogen or haloaryl, and two of the opposed meso atoms or groups being hydrogen or haloalkyl, but not all four of the meso atoms or groups being hydrogen. The invention also comprises new compositions of matter in which all four of the meso positions are substituted with haloalkyl groups and the beta positions are substituted with halogen atoms. A new method of synthesizing porphyrinogens is also provided.The novel compositions and others made according to the process of the invention are useful as hydrocarbon conversion catalysts; for example, for the oxidation of alkanes and the decomposition of hydroperoxides.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: November 5, 1996
    Assignee: Sun Company, Inc. (R&M)
    Inventors: Tilak Wijesekera, James E. Lyons, Paul E. Ellis, Jr.
  • Patent number: 5571841
    Abstract: Composition and method for enhancing therapeutic effects of topically applied agents are disclosed. The cosmetic or therapeutic composition may include one or more of cosmetic or pharmaceutical agents present in a total amount of from 0.01 to 40 percent and one or more of hydroxycarboxylic acids or related compounds present in a total amount of from 0.01 to 99 percent by weight of the total composition. The cosmetic and pharmaceutical agents may include but not limited to age spots, wrinkles and keratoses removing agents; vitamins; aloes; sun screens; tanning, depigmenting and shampooing agents; antiyeasts; antifungal, antibacterial and antiviral agents; topical bronchial dilators and topical cardiovascular agents; hormonal agents; vasodilators; retinoids and other dermatological agents. The hydroxycarboxylic acids and related compounds include organic alpha and beta hydroxycarboxylic acids, alpha and beta ketocarboxylic acids and salts thereof.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 5, 1996
    Assignee: Tristrata Technology, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5565487
    Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle galactonic acid or a topically effective salt thereof, or galactonolactone.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 15, 1996
    Assignee: Tristrata, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5565562
    Abstract: Triaza macrocycles carrying a -CH.sub.2 COOH, -CH.sub.2 CONR.sup.6 R.sup.7, --CH.sub.2 P(R.sup.5)O.sub.2 H, or --CH.sub.2 PO.sub.3 H.sub.2 group on two of the three ring nitrogen atoms and a --CH(L--Z)COOH, --CH(L--Z)CONR.sup.6 R.sup.7, --CH(L--Z)P(R.sup.5)O.sub.2 H, or --CH(L--Z)PO.sub.3 H.sub.2 group on the third ring nitrogen atom, in which L is an organic linking radical and Z is any group capable of reacting with a thiol, amino, carboxy, hydroxyl, aldehyde, aromatic, or heteroaromatic group, and metal complexes thereof, are useful for imaging, diagnosis, and therapy. A typical embodiment is N-[5-carboxy-5-{4,7-bis-(carboxymethyl)-1,4,7-triazacyclonon-1-yl}pentyl] 3-maleimidopropionamide.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 15, 1996
    Assignee: Celltech Therapeutics Limited
    Inventors: David Parker, Nigel R. A. Beeley, Thomas A. Millican
  • Patent number: 5565563
    Abstract: Triphendioxazine compounds of formula I, ##STR1## in which R.sub.1 and R.sub.2 are either both hydrogen or form a single chain linking the 8,9-; 9,10- or 10,11-positions, the single chain having the formula --NR.sub.5 ---(CO).sub.m --NH--, --CR.sub.5 .dbd.CH--CO--NH--, --CO--CH.sub.2 --CO--NH--, --CO--CH.dbd.CR.sub.5 --NH--, --CO--NH--CO--NH--, --CO--NH--CR.sub.6 .dbd.N--, --CR.sub.6 .dbd.N--CO--NH--, --NR.sub.5--(CO).sub.m --O--or --NH--CR.sub.5 .dbd.N--whereR.sub.5 is hydrogen, C.sub.1-4 alkyl or phenyl, R.sub.6 is hydrogen, C.sub.1-4 alkyl or phenyl;m is 1 or 2 and R.sub.3 and R.sub.4 are either both hydrogen or form a single chain linking the 1,2-, 2,3- or 3,4-positions, the single chain having a formula selected from --NR.sub.5 --(CO).sub.m --NH--, --CR.sub.5 .dbd.CH--CO--NH--, --O--CH.sub.2 --CO--NH--, --CO--CH.dbd.CR.sub.5 --NH--, --CO--NH--CO--NH--, --CONH--CR.sub.6 .dbd.N--, --CR.sub.6 .dbd.N--CO--NH--, --NR.sub.5 --(CO).sub.m --O--or --NH--CR.sub.5 .dbd.N--where the symbols R.sub.5, R.sub.
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: October 15, 1996
    Assignee: Sandoz Ltd.
    Inventors: Bansi L. Kaul, Peter Kempter
  • Patent number: 5563133
    Abstract: This invention provides a novel series of substituted hexamethyleneimines which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.
    Type: Grant
    Filed: February 21, 1995
    Date of Patent: October 8, 1996
    Assignee: Eli Lilly and Company
    Inventor: Philip A. Hipskind