The Hetero Ring Has Exactly 15 Ring Carbons Patents (Class 514/30)
  • Patent number: 7674475
    Abstract: A homogenous, clear, veterinary gel composition which has a broad spectrum of efficacy against endoparasites over a prolonged period of time and which allows for higher concentrations of a mixture of parasiticidal agents in a single application. This composition is useful for treating and controlling endoparasiticidal infection and infestation in a homeothermic animal.
    Type: Grant
    Filed: December 24, 2004
    Date of Patent: March 9, 2010
    Assignee: Wyeth LLC
    Inventors: Shobhan S. Sabnis, Jon Hayes, Jack A. Zupan
  • Patent number: 7671034
    Abstract: The invention relates to a stabilized premix feed or feed-like formulation that has an extended shelf life due to a decrease of the degradates of the active ingredient by controlling the amount of an already existing stabilizer in the formulation. The feed premix is used in the treatment of parasites in mammals, in particular swine and horses. The invention further relates to a method to extend the shelf life of a stable premix feed or feed-like formulation for the treatment of parasite infestation in swine and horses comprising controlling the amount of an already existing antioxidant or stabilizer in the formulation to decrease or to prevent the formation of acid/base catalyzed decomposition of the active ingredient.
    Type: Grant
    Filed: March 1, 2004
    Date of Patent: March 2, 2010
    Assignee: Merial Limited
    Inventor: Keith Allan Freehauf
  • Publication number: 20100016248
    Abstract: The invention relates to a tablet formulated for administration to an animal to treat parasite infestation. The tablet includes at least one macrocyclic lactone compound with anthelmintic activity dissolved in at least one organic solvent and subsequently formulated into a tablet. The tablets produced have a high degree of stability when stored over time and also provide the animal with a dose of agent sufficient to be therapeutically effective.
    Type: Application
    Filed: December 18, 2007
    Publication date: January 21, 2010
    Applicant: BOMAC RESEARCH LIMITED
    Inventors: Karthigeyan Nanjan, Fadil Al Alawi, Wayne Frederick Leech, Man Yik Li, Steve Li
  • Patent number: 7648711
    Abstract: A sustained release formulation by using dimeticone as the dispersion medium, which includes active ingredient (e.g., drugs against parasites, insecticides, NSAIDs, antibiotics, sex hormone like agents or oily soluble vitamins) and dimeticone as the medium. Suitable stabilizer, antioxidant, local analgesics and material for sustained release may be added. The formulation is bio-compatible, stable and injectable.
    Type: Grant
    Filed: October 8, 2003
    Date of Patent: January 19, 2010
    Inventors: Yuwan Wang, Zhende Pan, Xiaoxi Dai
  • Patent number: 7645816
    Abstract: Water-soluble compositions comprising a lipophilic compound and a solubilizing agent of the general formula: {X—OOC—[(CH2)n—COO]m}p—Y??(I) wherein: X is a residue of a hydrophobic moiety, Y is a residue of a hydrophilic moiety, p is 1 or 2, m is 0 or 1, and n is an integer greater than or equal to 0 are disclosed. The lipophilic compound is preferably selected from the group consisting of water-insoluble ubiquinones, ubiquinols, vitamins, provitamins, polyene macrolide antibiotics, and mixtures thereof. The hydrophobic moiety is preferably a sterol or a tocopherol and the hydrophilic moiety is preferably a polyalkylene glycol. In some embodiments, the sterol is cholesterol or sitosterol, the tocopherol is ?-(+)-tocopherol, the polyalkylene glycol is a polyethylene glycol or its methyl monoether having an average molecular weight between 400 and 1000, p is equal to 1 or 2, m is equal to 0 or 1 and n is an integer between 2 and 18.
    Type: Grant
    Filed: August 27, 2003
    Date of Patent: January 12, 2010
    Assignee: National Research Council of Canada
    Inventors: Henryk Borowy-Borowski, Marianna Sikorska-Walker, P. Roy Walker
  • Patent number: 7638545
    Abstract: A formulation having triclabendazole in solution. In addition a further anthelmintic may be included. The formulation is made by mixing the abamectin and benzyl alcohol and mixing this with triclabendazole and butyl dioxitol. The mix is then heated to dissolve the active, and allowed to cool at which stage the solution is diluted to volume with PEG 4000.
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: December 29, 2009
    Assignee: Merial Limited
    Inventor: Colin Manson Harvey
  • Publication number: 20090318375
    Abstract: This invention provides a crystalline azithromycin L-malate monohydrate for treating various microbial infections, which has high thermostability, solubility and non-hygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.
    Type: Application
    Filed: June 6, 2003
    Publication date: December 24, 2009
    Applicant: Hanmi Pharm Co., Ltd
    Inventors: Bo Sung Kwon, Eun Sook Kim, Hee Cheol Kim, Sangmin Yun, Myoung-sil Ko, Tae Hun Song, Han Kyong Kim, Kwee Hyun Suh, Gwansun Lee
  • Patent number: 7632820
    Abstract: Disclosed are compounds of the formulain which n is 0 or 1; X—Y is —CH?CH— or —CH2—CH2—; Z is —C(?O)—, —C(?S)— or —SO2—; R1 is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; and R2 is R3-Z-, R3—O-Z-, R4 or -Z-N(R6)(R7); Q is O or —N—R5; R3 and R4 are for example H, C1C12alkyl, C2-C12alkenyl, C2-C12alkynyl, C3-C12zcycloalkyl, C5-C12cycloalkenyl, aryl or heterocyclyl; R5 is for example H, C1-C8alkyl, hydroxy-C1-C8alkyl, C3-C8cycloalkyl, C2-C8alkenyl, C2-C8alkynyl, phenyl or benzyl; R6 and R7 are for example, H, unsubstituted or mono- to pentasubstituted C1-C12alkyl, unsubstituted or mono- to pentasubstituted C2-C12alkenyl or, if appropriate, an E/Z isomer, E/Z isomer mixture and/or tautomer thereof, in each case in free form or in salt form, are useful as pesticides.
    Type: Grant
    Filed: January 30, 2004
    Date of Patent: December 15, 2009
    Assignee: Merial Limited
    Inventors: Thomas Pitterna, Peter Maienfisch, Fiona Murphy Kessabi, Jerome Cassayre, Laura Quaranta, Pierre Jung
  • Patent number: 7605134
    Abstract: A description is given of compounds of the formula which in the 4?-position has the (S)-configuration and wherein R1 is C1-C12alkyl, C3-C8cycloalkyl; or C2-C12alkenyl; R2 is hydrogen, optionally substituted C1-C12alkyl or optionally substituted C2-C12alkenyl; R3 is C1-C12alkyl, optionally substituted C1-C12alkyl, optionally substituted C1-C12alkoxy-C1-C12alkyl, optionally substituted C3-C12cycloalkyl, optionally substituted C2-C12alkenyl; optionally substituted C4-C12cycloalkenyl, optionally substituted C2-C12alkynyl; or R2 and R3 together are a three- to seven-membered alkylene or four- to seven-membered alkenylene bridge in each of which a CH2 group may have been replaced by O, S or NR4; X is O or S; R4 is C1-C8alkyl, C3-C8cycloalkyl, C2-C8alkenyl, C2-C8alkynyl, benzyl or C(?O)—R5; R5 is for example H, OH, SH, C1-C12alkyl, C2-C8alkenyl, C2-C8alkynylyl or C1-C12haloalkyl; and, where appropriate, E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form; to a pro
    Type: Grant
    Filed: August 20, 2002
    Date of Patent: October 20, 2009
    Assignee: Merial Limited
    Inventor: Hans Tobler
  • Publication number: 20090258065
    Abstract: Compositions and nanoemulsions containing lipid nanocapsules dispersed in a hydrophilic phase, such nanocapsules including at least one avermectin compound, are useful for the treatment of dermatological pathologies, e.g., rosacea.
    Type: Application
    Filed: April 10, 2009
    Publication date: October 15, 2009
    Applicant: GALDERMA S.A.
    Inventors: Lara Baudonnet, Claire Mallard
  • Publication number: 20090233877
    Abstract: Compounds of the natural avermectin family are formulated into pharmaceutical compositions useful for the treatment of dermatological conditions in humans, in particular rosacea.
    Type: Application
    Filed: March 20, 2009
    Publication date: September 17, 2009
    Applicant: GALDERMA S.A.
    Inventors: Alexandre KAOUKHOV, Cecile Cousin
  • Patent number: 7585887
    Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula ?in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (29) listed in the disclosure.
    Type: Grant
    Filed: October 29, 2001
    Date of Patent: September 8, 2009
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • Patent number: 7582612
    Abstract: The present invention provides a method for preparing a pharmaceutical formulation containing ivermectin and a method and composition that can contain ivermectin plus tetrahydropyrimidines. An examples of a tetrahydropyrimidine includes pyrantel. A pharmaceutical formulation is provided for use in the treatment of helminthiasis of mammals, and particularly tapeworm, hookworm, roundworm and heartworm of domestic animals and farm animals. The present invention also provides a method of treating helminthiasis in mammals, which method comprises administering to the mammal in need thereof an anthelmintically effective amount of a pharmaceutical formulation of the invention.
    Type: Grant
    Filed: August 3, 2004
    Date of Patent: September 1, 2009
    Assignees: Hartz Mountain Corporation, Virbac Corporation
    Inventors: Albert Ahn, Ian Cottrell
  • Patent number: 7563773
    Abstract: This invention provides for, inter alia, oral homogeneous veterinary pastes for the treating, controlling and preventing of endo- and ectoparasite infections in warm-blooded animals or birds, such as horses and household pets. This invention further provides for a process of preparing these veterinary pastes and for a method for increasing the bioavailability of the anthelmintic agents contained in the paste in the warm-blooded animal or bird. The inventive oral homogeneous anthelmintic pastes comprise a first anthelmintic agent, for example, prazequantel and/or pyrantel, and at least one marcrolide anthelmintic compound, a solvent, which dissolves both the first anthelmintic agent and second the macrolide anthelmintic compound, and a thickening agent.
    Type: Grant
    Filed: April 15, 2005
    Date of Patent: July 21, 2009
    Assignee: Merial Limited
    Inventors: Keith Freehauf, Maryam Moaddeb
  • Patent number: 7550440
    Abstract: Dermatological conditions/afflictions such as rosacea, common acne, seborrheic dermatitis, perioral dermatitis, acneform rashes, transient acantholytic dermatosis, and acne necrotica miliaris, most notably rosacea, are treated by topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical composition which comprises a thus effective amount of ivermectin.
    Type: Grant
    Filed: October 24, 2005
    Date of Patent: June 23, 2009
    Assignee: Galderma S.A.
    Inventors: Vincent Manetta, Gary R. Watkins
  • Patent number: 7521429
    Abstract: A compound of formula (I) wherein the bond between carbon atoms 22 and 23 may be a single or a double bond; R1 is C1-C12alkyl, C3-C8cycloalkyl, or C2-C12alkenyl; R2 and R3 are, for example, independently of each other hydrogen, C1-C12alkyl, C3-C12cycloalkyl, C2-C12alkenyl, C2-C12alkynyl, aryl or heteroaryl; and, where applicable, to E/Z isomers, mixtures of E/Z isomers, diastereomers and/or tautomers, in each case in free form or in salt form; pesticidal compositions in which the active ingredient has been selected from those compounds and their tautomers; and a method of controlling pests using those compositions are described.
    Type: Grant
    Filed: June 15, 2004
    Date of Patent: April 21, 2009
    Assignee: Merial Limited
    Inventors: Thomas Pitterna, Pierre Jung, Fiona Murphy Kessabi, Jerome Cassayre, Laura Quaranta, Ottmar Franz Hueter
  • Publication number: 20090093421
    Abstract: Administration of at least one compound of the family of the avermectins or of the family of the milbemycins, notably ivermectin, is useful for the treatment of ophthalmic pathologies, including ocular rosacea.
    Type: Application
    Filed: March 31, 2008
    Publication date: April 9, 2009
    Applicant: GALDERMA S.A.
    Inventors: Alexandre KAOUKHOV, Christophe VILLARD, Philippe BOUISSOU
  • Patent number: 7514094
    Abstract: A pesticidal composition comprising a pesticidally effective amount of at least one of a pyridic compound of the formula (I) or it salt and at least one of other pesticides: wherein Y is a haloalkyl group, m is 0 or 1, and Q is or a substituted or unsubstituted heterocyclic group, (wherein X is an oxygen atom or a sulfur atom, R1 and R2 are respectively independently a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted cycloalkyl group, and the like.
    Type: Grant
    Filed: February 1, 2007
    Date of Patent: April 7, 2009
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Masayuki Morita, Mitsugu Iwasa
  • Publication number: 20090075918
    Abstract: Veterinarian composition comprising an organic salt of levamisole in combination with at least one avermectine and/or milbemycine. A veterinarian formulation comprising of organics salts of levamisole, more specifically to the disophenolat salt of levamisole and the nitroxynil-salt of levamisole with avermectines and milbemycines and its use in treatment of helminthiasis in mammals, in particular in bovines, swines, caprines, equines, ovines, canines and felines.
    Type: Application
    Filed: December 18, 2006
    Publication date: March 19, 2009
    Inventors: Dolivar Coracci Neto, Nelson Henriques Fernandes Filho, Ricardo da Silva Sercheli
  • Publication number: 20090042815
    Abstract: This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.
    Type: Application
    Filed: July 26, 2007
    Publication date: February 12, 2009
    Applicant: Intervet International B.V.
    Inventors: Fritz Blatter, Meinrad Brenner, Monika Brink, Kerstin Fleischhauer, Guixian Hu, Hans Peter Niedermann, Timo Rager, Tanja Schweisel, Stephan Veit, Ralf Warrass, Heinz-Jorg Wennesheimer
  • Publication number: 20080248998
    Abstract: Composition intended for the oral administration of active principles with unacceptable taste, which comprises from about 15% to about 30% of organoleptically unpleasant active ingredient (principle) that is mixed with from about 60% to about 80% of an ester of glycerol or of a fatty acid, to which a wax is optionally added and to which a surfactant is added, and in that it is prepared by a spray-cooling process which can produce a particle size of less than 350 ?m.
    Type: Application
    Filed: June 16, 2008
    Publication date: October 9, 2008
    Applicant: AVENTIS PHARMA SA
    Inventors: Isabelle CHACORNAC, Patricia PROBECK
  • Publication number: 20080194498
    Abstract: Described is a compound of the formula (1) wherein the bond between carbon atoms 22 and 23 is a single or double bond; m is 0 or 1; R1, is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; and either (A) R2 is —N(R3)R4, and (1) X is 0, wherein R3 is, for instance, hydrogen, unsubstituted or mono- to pentasubstituted C1-C12alkyl, and R4 is, for instance, mono- to pentasubstituted C1-C12alkyl, unsubstituted or mono- to pentasubstituted C3-C12cycloalkyl; or (2) X is S, wherein R3 is, for instance, hydrogen, unsubstituted or mono- to pentasubstituted C1-C12alkyl, and R4 is, for instance, hydrogen, unsubstituted or mono- to pentasubstituted C1-C12alkyl; or (3) X is 0 or S, wherein R3 and R4 together are, for instance, a three- to seven membered alkylene or a four- to seven-membered alkenylene bridge; or (B) R2 is OR5, X is 0 or S, wherein R5 is, for instance, C1-C12alkyl, mono- to pentasubstituted C1-C12alkyl; or, if appropriate, an E/Z isomer, E/Z isomer mixture and/or tautomer thereof, in each case in free form or
    Type: Application
    Filed: August 27, 2004
    Publication date: August 14, 2008
    Inventors: Fiona Murphy Kessabi, Thomas Pitterna, Peter Maienfisch, Jerome Cassayre, Laura Quaranta, Pierre Jung, Ottmar Franz Hueter
  • Patent number: 7396820
    Abstract: The present invention provides a method for preparing a pharmaceutical formulation containing ivermectin and a method and composition that can contain ivermectin plus hexahydropyrazinoisoquinolines, tetrahydropyrimidines and benzimidazoles or febantel. Examples of hexahydropyrazinoisoquinolines, tetrahydropyrimidines and benzimidazoles include praziquantel, pyrantel pamoate and fenbendazole, respectively. A pharmaceutical formulation is provided for use in the treatment of helminthiasis of mammals, and particularly tapeworm, hookworm, roundworm, whipworm and heartworm of domestic animals and farm animals. The present invention also provides a method of treating helminthiasis in mammals, which method comprises administering to the mammal in need thereof an anthelmintically effective amount of a pharmaceutical formulation of the invention.
    Type: Grant
    Filed: March 12, 2004
    Date of Patent: July 8, 2008
    Assignees: Virbac Corporation, The Hartz Mountain Corporation
    Inventors: Ian Cottrell, Arima Das Nandy, Albert Ahn, Richard Fisher
  • Patent number: 7396819
    Abstract: The present invention provides a method for preparing a pharmaceutical formulation containing ivermectin and a method and composition that can contain ivermectin plus hexahydropyrazinoisoquinolines and tetrahydropyrimidines. Examples of these include praziquantel and pyrantel. A pharmaceutical formulation is provided for use in the treatment of helminthiasis of mammals, and particularly tapeworm, hookworm, roundworm and heartworm of domestic animals and farm animals. The present invention also provides a method of treating helminthiasis in mammals, which method comprises administering to the mammal in need thereof an anthelmintically effective amount of a pharmaceutical formulation of the invention.
    Type: Grant
    Filed: August 8, 2003
    Date of Patent: July 8, 2008
    Assignees: Virbac Corporation, The Hartz Mountain Corporation
    Inventors: Michael Burke, Vinay Tripathi, Albert Ahn, Ian Cottrell
  • Publication number: 20080161249
    Abstract: The present invention relates to the use of novel antibacterial compounds, and pharmaceutical compositions containing these compounds.
    Type: Application
    Filed: November 17, 2005
    Publication date: July 3, 2008
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventor: Jianzhong Huang
  • Patent number: 7378399
    Abstract: What is described are a compound of the formula (I) Wherein A-B is —CH?CH— or —CH2—CH2—; n is 0 or 1; R1, is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; R2 and R3 for instance are either, (i) independently from each other for instance -Q, —C(?Y)-Q, or —C(?Y)—O-Q; or (ii) together form with the nitrogen atom to which they are bound a three- to seven-membered ring, (iii) together are ?C(R4)R5; R4 and R5 are, independently from each other, for instance -Q, —C(?Y)-Q, or —C(?Y)—O-Q; Y is O or S; Q is for instance H or unsubstituted or mono- to pentasubstituted C1-C12alkyl; or, if appropriate, an E/Z isomer, E/Z isomer mixture and/or tautomer thereof; a process for preparing these compounds, their isomers and tautomers and the use of these compounds, their isomers and tautomers; pesticidal compositions whose active compound is selected from these compounds and their tautomers; intermediates for the preparation of the said compounds of the formula (I), methods for the preparation of the compounds of the formula (
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: May 27, 2008
    Assignee: Merial Limited
    Inventors: Jerome Cassayre, Hans Tobler, Thomas Pitterna, Peter Maienfisch, Fiona Murphy Kessabi, Laura Quaranta, Ottmar Franz Hueter
  • Patent number: 7368435
    Abstract: A topical formulation having significant parasiticidal activity effective against endoparasites and/or ectoparasites such as heartworms, mites, fleas, ticks, flies is provided, which can be safe to use and avoids the many common deleterious side effects of conventional topical formulations. The topical formulations comprise a combination of a macrocyclic lactone, a neo-nicotinoid and optionally, an insect growth regulator. The topical formulation can be packaged together or packaged so that the macrocyclic lactone and the neo-nicotinoid are stored separately prior to administering the topical insecticide formulation to the animal.
    Type: Grant
    Filed: September 7, 2005
    Date of Patent: May 6, 2008
    Assignee: Summit Vetpharm, LLC
    Inventors: Ian W. Cottrell, Albert Ahn, Richard Fisher
  • Patent number: 7282487
    Abstract: The invention relates to methods of treating a bacterial infection in a horse or a pig. The method involves administering to the horse or pig a composition comprising (i) a salt made from tilmicosin and a lipophilic acid and (ii) a pharmaceutically acceptable solvent combined together to form an injectable composition that precipitates when injected into water.
    Type: Grant
    Filed: October 28, 2004
    Date of Patent: October 16, 2007
    Assignee: Idexx Laboratories
    Inventor: Yerramilli V. S. N. Murthy
  • Patent number: 7250402
    Abstract: A compound represented by the general formula (I) or a salt thereof: wherein represents —CH?CH—, —CH2—CH2— or the like, between R1 and the carbon atom at 4?-position represents a single bond or a double bond, between R2 and the carbon atom at 5-position represents a single bond or a double bond, and for example, 1) when represents —CH?CH— or —CH2—CH2—, and between R1 and the carbon atom at 4?-position represents a double bond, R1 represents ?C(R11)(R12) (wherein R11 represents a lower alkyl group or the like and R12 represents a hydrogen atom or the like) or the like, and R2 represents a hydroxyl group or the like, or R2 may be combined together with the carbon atom at 5-position to form a carbonyl group, and 2) when represents —CH?CH— or —CH2—CH2—, and between R1 and the carbon atom at 4?-position represents a single bond, R1 represents —OCH(R1a)(R1b) (wherein R1a represents a lower alkyl or the like and R1b represents a hydrogen atom or the like) or the like, and R2 re
    Type: Grant
    Filed: November 29, 2004
    Date of Patent: July 31, 2007
    Assignee: The Kitasato Institute
    Inventors: Satoshi Omura, Kenichiro Nagai, Toshiaki Sunazuka
  • Patent number: 7247617
    Abstract: Sixteen membered macrolide anti-infective agents having a structure according to formula I where R1, R2, R3, R4, R5, and R6 are as defined herein, and related compounds are disclosed.
    Type: Grant
    Filed: June 15, 2005
    Date of Patent: July 24, 2007
    Assignee: Kosan Biosciences Incorporated
    Inventors: Hong Fu, Leonard Katz, David C. Myles
  • Patent number: 7195773
    Abstract: A pesticidal composition comprising a pesticidally effective amount of at least one of a pyridic compound of the formula (I) or it salt and at least one of other pesticides: wherein Y is a haloalkyl group, m is 0 or 1, and Q is or a substituted or unsubstituted heterocyclic group, (wherein X is an oxygen atom or a sulfur atom, R1 and R2 are respectively independently a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted cycloalkyl group, and the like.
    Type: Grant
    Filed: October 22, 2001
    Date of Patent: March 27, 2007
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Masayuki Morita, Mitsugu Iwasa
  • Patent number: 7144866
    Abstract: Provided is a compound represented by the general formula (I) or a salt thereof: wherein, —XY— represents —CH?CH— and the like, between R2 and the carbon atom at 5-position represents a single bond or a double bond, R1 represents a lower alkyl group, a formyl group, a carboxyl group, a lower alkoxycarbonyl group (wherein a lower alkyl moiety of said lower alkoxycarbonyl group may be substituted with a heterocyclic group) and the like, and R1a represents a hydrogen atom, provided when R1 represents a lower alkoxycarbonyl group and the like, R1a may further represents a lower alkoxycarbonyl group and the like, when between R2 and the carbon atom at 5-position is a single bond, R2 represents a hydroxyl group and the like, and when between R2 and the carbon atom at the 5-position is a double bound, R2 combines with the carbon atom at 5-position to form a hydroxime group (—C(?NOH)) and the like, and R3 represents a hydroxyl group or a tri(lower alkyl)silyloxy group.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: December 5, 2006
    Assignee: The Kitasato Institute
    Inventors: Satoshi Omura, Kenichiro Nagai, Toshiaki Sunazuka
  • Patent number: 7119076
    Abstract: A drug effective for prevention and therapy of endometriosis and hysteromyoma is disclosed. The drug for prevention and/or therapy of endometriosis and/or hysteromyoma according to the present invention comprises as an effective ingredient a macrolide antibiotic.
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: October 10, 2006
    Inventor: Masao Sugamata
  • Patent number: 7094431
    Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: August 22, 2006
    Inventor: Mickey L. Peshoff
  • Patent number: 7064108
    Abstract: A topical gel composition comprising between about 0.005 and 1.0% ivermectin, between about 30 and 40% of a pharmaceutically acceptable alcohol, between about 30 and 40% of a pharmaceutically acceptable glycol, and a pharmaceutically acceptable carrier, useful for treating Pediculosis capitis infestation in a human patient.
    Type: Grant
    Filed: February 4, 2003
    Date of Patent: June 20, 2006
    Assignees: Merck & Co., Inc., McNeil-PPC, Inc.
    Inventors: Cynthia A. Guzzo, Coleen M. Clineschmidt, George Schorn, James M. Reynolds
  • Patent number: 7037523
    Abstract: The present invention provides a controlled release pharmaceutical composition of an acid labile, poorly soluble drug having pH dependent solubility profile in aqueous environment. In a preferred embodiment the drug is combined with a practically water insoluble polymer an optimizing agent and optional additives to produce a controlled release of therapeutic agent when compositions is exposed to aqueous environment.
    Type: Grant
    Filed: November 1, 2002
    Date of Patent: May 2, 2006
    Assignee: Wockhardt Limited
    Inventors: Javed Hussain, Pankaj Khapra, Arun S. Gosavi
  • Patent number: 7001889
    Abstract: This invention provides for, inter alia, oral homogeneous veterinary pastes for the treating, controlling and preventing of endo- and ectoparasite infections in warm-blooded animals or birds, such as horses and household pets. This invention further provides for a process of preparing these veterinary pastes and for a method for increasing the bioavailability of the anthelmintic agent contained in the paste in the warm-blooded animal or bird. The inventive oral homogeneous anthelmintic pastes comprise a first anthelmintic agent, for example, prazequantel and/or pyrantel, and at least one marcrolide anthelmintic compound, a solvent, which dissolves both the first anthelmintic agent and second the macrolide anthelmintic compound, and a thickening agent.
    Type: Grant
    Filed: June 21, 2002
    Date of Patent: February 21, 2006
    Assignee: Merial Limited
    Inventors: Keith Freehauf, Maryam Moaddeb
  • Patent number: 6998131
    Abstract: In particular this invention provides for spot-on compositions for the treatment or prophylaxis of parasite infestations in mammals or birds which comprise: (1) a composition comprising (A) an effective amount of a 1-phenylpyrazole derivative; and (B) an effective amount of emamectin; (2) an acceptable liquid carrier vehicle; and (3) optionally, a crystallization inhibitor. The invention also provides for a method of treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal or bird an effective amount of a composition according to the present invention.
    Type: Grant
    Filed: October 24, 2002
    Date of Patent: February 14, 2006
    Assignee: Merial Limited
    Inventors: Mark D. Soll, Albert Boeckh
  • Patent number: 6991801
    Abstract: This invention provides for inter alia, topical anthelmintic formulations which comprise a pharmaceutically active combination consisting of at least one macrocyclic compound and at least one compound selected from the group consisting of praziquantel, morantel and pyrantel, which are dissolved in a non-aqueous solvent or solvent mixture and optionally a thickening agent.
    Type: Grant
    Filed: April 5, 2004
    Date of Patent: January 31, 2006
    Assignee: Merial Limited
    Inventors: Mark D. Soll, Krishan Kumar, Robert P. Waranis, Natalya Shub
  • Patent number: 6962713
    Abstract: In particular this invention provides for spot-on compositions for the treatment or prophylaxis of parasite infestations in mammals or birds which comprise: (1) a composition comprising (A) an effective amount of a 1-phenylpyrazole derivative; and/or (B) an effective amount of a macrocyclic lactone antihelmintic or antiparasitic agent; (2) an acceptable liquid carrier vehicle; and (3) optionally, a crystallization inhibitor. The invention also provides for a method of treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal or bird an effective amount of a composition according to the present invention.
    Type: Grant
    Filed: May 24, 2002
    Date of Patent: November 8, 2005
    Assignee: Merial
    Inventors: Anne-Marie Huet, Bruno Julia, Jean-Pierre Etchegaray, André Weil, Philippe Jeannin
  • Patent number: 6919317
    Abstract: Synergistic combinations of a squalene epoxidase inhibitor such as terbinafine and a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro, 33-desoxyascomycin are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin plays a role, such as atopic dermatitis and seborrhoeic dermatitis, and in situations of fungal resistance.
    Type: Grant
    Filed: February 16, 2001
    Date of Patent: July 19, 2005
    Assignee: Novartis AG
    Inventors: Neil Stewart Ryder, Friedrich Karl Mayer
  • Patent number: 6914051
    Abstract: A penetrating antibiotic gel for treating pain, inflammation and other pathological conditions affecting musculoskeletal tissues and other soft tissues of the body. The composition includes an antibiotic compound and a mobilizing agent in an amount sufficient to enable the antimicrobial compound to penetrate into the sub-dermal soft tissues. The antimicrobial compound may be a macrolide antibiotic compound such as azithromycin, erythromycin or roxithromycin, for example, and the mobilizing agent may be an organogel compound, such as pluronic lecithin liposomal organogel (PLO). The composition may further include a penetration enhancing adjuvant, such as d-limonene, for example. The composition may be applied topically so as to penetrate into the sub-dermal soft tissues, or may injected so as to be absorbed into the soft tissues locally.
    Type: Grant
    Filed: June 28, 2001
    Date of Patent: July 5, 2005
    Inventor: David M Allen
  • Patent number: 6903052
    Abstract: The invention concerns the use of certain compounds related to fatty acids to control nematodes that infest plants or the situs of plants. Nematodes that parasitize animals can also be controlled using the methods and composition of this invention. Certain of the useful compounds are fatty acid esters that are predicted inhibitors of nematode delta-12 fatty acid desaturases and can be, for example, from C16 to C20 in length.
    Type: Grant
    Filed: July 1, 2002
    Date of Patent: June 7, 2005
    Assignee: Divergence, Inc.
    Inventors: Deryck J. Williams, Andrew P. Kloek, Michelle Coutu Hresko
  • Patent number: 6893652
    Abstract: A homogenous, clear, veterinary gel composition which has a broad spectrum of efficacy against endoparasites over a prolonged period of time and which allows for higher concentrations of a mixture of parasiticidal agents in a single application. This composition is useful for treating and controlling endoparasiticidal infection and infestation in a homeothermic animal.
    Type: Grant
    Filed: July 24, 2002
    Date of Patent: May 17, 2005
    Assignee: Wyeth
    Inventors: Shobhan S. Sabnis, Jon Hayes, Jack A. Zupan
  • Patent number: 6872708
    Abstract: A local injection prescription that disperses a malignant tumor to decrease the size of the tumor or terminate the tumor. The local injection prescription is produced by dissolving an organic compound having a lactone nucleus in lower alcohol and water.
    Type: Grant
    Filed: April 7, 2003
    Date of Patent: March 29, 2005
    Inventors: Mitsukazu Matsumoto, Hisatake Ishikawa, Hirohiko Matsumoto
  • Patent number: 6764999
    Abstract: A method to treat an animal in need thereof with one or more parasiticides by administering those one or more parasiticides to the nasal pharynx of the animal. A method to increase an animal's blood levels of one or more avermectin compounds/milbemycin compounds such that the blood levels of those one or more avermectin compounds/milbemycin compounds reach a maximum concentration in about 24 hours, and such that those blood levels exceed about 2 ng/ml for at least 96 hours post administration.
    Type: Grant
    Filed: July 11, 2002
    Date of Patent: July 20, 2004
    Inventors: Stephen E. Bachman, Michael E. Hubbert
  • Patent number: 6756369
    Abstract: The present invention provides a unique approach for the diagnosis and management of infections by Chlamydia species, particularly C. pneumoniae. The invention is based, in part, upon the discovery that a combination of agents directed toward the various stages of the chlamydial life cycle is effective in substantially reducing infection. Products comprising combination of antichlamydial agents, novel compositions and pharmaceutical packs are also described.
    Type: Grant
    Filed: March 19, 2002
    Date of Patent: June 29, 2004
    Assignee: Vanderbilt University
    Inventors: William M. Mitchell, Charles W. Stratton
  • Patent number: 6746677
    Abstract: The invention relates to certain stable vaccine compositions comprising a macrocyclic lactone compound, a milbemycin compound, an avermectin compound or mixtures thereof; at least one antigen; a dispersing agent; an adjuvant; a water soluble organic solvent; and saline or water or mixtures thereof. The invention further relates to stable compositions as described above of a macrocyclic lactone compound, a milbemycin compound, an avermectin compound or mixtures thereof, but without an antigen. The invention also relates to a method for preventing or controlling helminthiasis, infection by acarids and arthropod endo-and ectoparasites and bacterial and viral disease in warm-blooded animals by the parenteral administration of compositions of the invention. The invention further relates to a process for the preparation of the invention compositions.
    Type: Grant
    Filed: October 8, 1999
    Date of Patent: June 8, 2004
    Assignee: American Cyanamid Company
    Inventors: Ramune Marija Cobb, Christopher Leigh Schwartzkoff
  • Patent number: 6710034
    Abstract: There are described novel 5-O-mycaminosyltylonide derivatives and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described are a method for treating bacterial infections by administering to an animal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: March 23, 2004
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Ly Tam Phan, Nha Vo, Yat Sun Or, Yao-Ling Qiu, Ying Hou
  • Patent number: 6680299
    Abstract: There are described novel 4′ substituted 16-membered macrolides and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described are a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.
    Type: Grant
    Filed: July 27, 2001
    Date of Patent: January 20, 2004
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Ly Tam Phan, Zhaolin Wang, Tianying Jian