Patents Represented by Attorney, Agent or Law Firm J. Eric Thies
  • Patent number: 5962485
    Abstract: The subject N-(2-benzyloxy-1-phenethyl)-N-(2'-methoxyethyl)amino-methane compounds of the formula: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and Het are defined herein) are tachykinin receptor antagonists which are useful in the treatment of pain, inflammation, migraine and emesis.
    Type: Grant
    Filed: September 16, 1997
    Date of Patent: October 5, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Andrew Pate Owens
  • Patent number: 5962462
    Abstract: The present invention is directed to spiro-substituted azacycles of the Formula 1: ##STR1## (wherein R.sub.1, l, m, Q, W, X, Y, and Z are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: October 5, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Sander G. Mills, Malcolm Maccoss, Martin S. Springer
  • Patent number: 5952315
    Abstract: The present invention provides methods for the treatment or prevention of bipolar disorder without concomitant therapy with other antidepressant or anti-anxiety agents which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.
    Type: Grant
    Filed: December 1, 1997
    Date of Patent: September 14, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Patent number: 5952330
    Abstract: The present invention provides methods for the treatment or prevention of mania or hypomania which comprises administration of a NK-1 receptor antagonist, optionally with an antipsychotic agent, and pharmaceutical compositions containing a NK-1 receptor antagonist.
    Type: Grant
    Filed: December 1, 1997
    Date of Patent: September 14, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Nadia Melanie Rupniak
  • Patent number: 5945445
    Abstract: There is disclosed a composition for preventing wilting of pines which comprises as an active ingredient a compound of the formula (I): whereinR.sub.1 is alkyl, cycloalkyl or alkenyl;R.sub.2 is hydrogen, alkyl, alkanoyl or alkylsilyl;R.sub.3 is hydrogen or optionally substituted hydroxyl;R.sub.4 is hydrogen, hydroxyl or alkoxyimino;the carbon-carbon bond X represents a single bond or double bond, provided that, when R.sub.4 is alkoxyimino, X represents a single bond, and when R.sub.1 is methyl or ethyl and R.sub.2, R.sub.3 and R.sub.4 are hydrogen, X represents a double bond; or a salt thereof, as well as a method of preventing the pine wilt using the same.Even if pine trees are infected with pine wilt nematodes, the pine wilt nematodes can be killed before the pine wilt nematodes start action in the trunks of the pine trees.
    Type: Grant
    Filed: July 2, 1998
    Date of Patent: August 31, 1999
    Assignee: Merck & Co., Inc.
    Inventors: George F. Barringer, Tetsuo Kumagai
  • Patent number: 5929243
    Abstract: The present invention is concerned with a novel process for the preparation of a compound of the formula: ##STR1## This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: April 2, 1998
    Date of Patent: July 27, 1999
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Peter Maligres, Michel Chartrain, Ralph Volante
  • Patent number: 5929094
    Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
    Type: Grant
    Filed: October 22, 1997
    Date of Patent: July 27, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Philippe Durette, Ihor Kopka, Malcolm MacCoss, Sander Mills
  • Patent number: 5929054
    Abstract: The present invention provides a method for the treatment or prevention of sexual dysfunctions which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such an NK-1 receptor antagonist.
    Type: Grant
    Filed: December 1, 1997
    Date of Patent: July 27, 1999
    Assignees: Merck Sharp, Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Patent number: 5925627
    Abstract: The present invention provides a method for the treatment or prevention of movement disorders using an orally active, long acting, CNS-penetrant NK-1 antagonist and pharmaceutical compositions comprising such an antagonist.
    Type: Grant
    Filed: December 1, 1997
    Date of Patent: July 20, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Patent number: 5922744
    Abstract: The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.
    Type: Grant
    Filed: January 12, 1998
    Date of Patent: July 13, 1999
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Timothy Harrison, Andrew Pate Owens
  • Patent number: 5922706
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: November 13, 1997
    Date of Patent: July 13, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Tamara Ladduwahetty
  • Patent number: 5919776
    Abstract: The present invention is directed to aminoquinolines of Formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: December 18, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: William K. Hagmann, Martin S. Springer
  • Patent number: 5919781
    Abstract: The present invention provides a method for the treatment or prevention of substance use disorders using an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.
    Type: Grant
    Filed: December 1, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Patent number: 5892082
    Abstract: The present invention is directed to a process for the preparation of the reagent dimethyl titanocene (Cp.sub.2 Ti(CH.sub.3).sub.2) from titanocene dichloride (Cp.sub.2 TiCl.sub.2) and a methyl magnesium halide, in particular, methyl magnesium chloride (CH.sub.3 MgCl). The instant process provides the desired reagent in a manner which is generally less hazardous and more economical than previous methods.
    Type: Grant
    Filed: March 7, 1997
    Date of Patent: April 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Dongwei Cai, Ian F. Cottrell, David L. Hughes, Joseph F. Payack
  • Patent number: 5880125
    Abstract: The present invention is directed to certain novel compounds identified as 4-spiroindoline piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5, R.sup.8, and A are as defined herein. These compounds 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 treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing these compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: March 18, 1997
    Date of Patent: March 9, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Ravi Nargund
  • Patent number: 5880123
    Abstract: The present invention relates to the use of a non-ionic surface-active agent or an emulsion for the reduction of the hemolytic effects of an amphiphilic compound. There is also provided a method for reducing the hemolytic effects of an amphiphilic compound which comprises formulating said compound with a non-ionic surface-active agent or in the form of an emulsion.
    Type: Grant
    Filed: June 20, 1997
    Date of Patent: March 9, 1999
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Timothy Harrison
  • Patent number: 5880132
    Abstract: This invention relates to methods and compositions for treating pain and nociception in a patient by administering a combination of a piperidine tachykinin antagonist and an opioid analgesic.
    Type: Grant
    Filed: June 20, 1997
    Date of Patent: March 9, 1999
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Raymond George Hill
  • Patent number: 5877316
    Abstract: The present invention relates to compounds of formula (I), wherein R.sup.1 and R.sup.4 represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, C.sub.1-6 alkoxy, C.sub.1-4 alkyl substituted by a hydroxy or C.sub.1-4 alkoxy group, OCF.sub.3, hydroxy, trifluoromethyl, trimethylsilyl, nitro, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, COR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are each independently hydrogen or C.sub.1-4 alkyl; R.sup.2, R.sup.3 and R.sup.5 represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy substituted by a C.sub.1-4 alkoxy group, or trifluoromethyl; R.sup.6 represents C.sub.1-6 alkyl, optionally substituted by oxo, substituted by a 5-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, oxadiazole and thiadiazole, wherein each heteroaromatic ring is substituted at the available carbon atom by a group of the formula: ZNR.sup.7 R.sup.8.
    Type: Grant
    Filed: September 16, 1997
    Date of Patent: March 2, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Karen Elizabeth Haworth, Simon Neil Owen, Eileen Mary Seward
  • Patent number: 5877214
    Abstract: The present invention is directed to the certain polyaryl-poly(ethylene glycol) compounds ("polyaryl-PEG" compounds) which are useful as soluble polyvalent supports in the preparation of combinatorial libraries of compounds. The resultant combinatorial libraries are useful in screening for biologically active moieties in the drug discovery process or in developing compounds with desired physical and chemical properties.
    Type: Grant
    Filed: September 4, 1997
    Date of Patent: March 2, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Ronald M. Kim
  • Patent number: 5877182
    Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.5, D,E, X, Y, n, x and y are as defined herein. These compounds 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 treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: September 9, 1997
    Date of Patent: March 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Ravi Nargund, Arthur A. Patchett, James Tata