Patents Represented by Attorney, Agent or Law Firm Philippe L. Durette
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Patent number: 6255305Abstract: Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the &agr;2 and/or &agr;3 subunits.Type: GrantFiled: November 10, 1998Date of Patent: July 3, 2001Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, William Robert Carling, Jose Luis Castro Pineiro, Alexander Richard Guiblin, Andrew Madin, Kevin William Moore, Michael Geoffrey Russell, Leslie Joseph Street
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Patent number: 6232308Abstract: The present invention relates to benzazepine derivatives and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.Type: GrantFiled: February 2, 2000Date of Patent: May 15, 2001Assignee: Merck & Co., Inc.Inventor: Ben C. Askew
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Patent number: 6211191Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;&ngr;&bgr;3, &agr;&ngr;&bgr;5, and/or &agr;&ngr;&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.Type: GrantFiled: December 15, 1998Date of Patent: April 3, 2001Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, James J. Perkins, Robert S. Meissner
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Patent number: 6211184Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are &agr;v&bgr;3 antagonists, &agr;v&bgr;5 antagonists or dual &agr;v&bgr;3/&agr;v&bgr;5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: June 14, 1999Date of Patent: April 3, 2001Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Robert S. Meissner, James J. Perkins, Ben C. Askew, Paul J. Coleman, John J. Hutchinson, Adel M. Naylor-Olsen
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Patent number: 6211219Abstract: A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D&agr; receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT1D&agr; receptor subtype relative to the 5-HT1D&bgr; subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.Type: GrantFiled: January 4, 1999Date of Patent: April 3, 2001Assignee: Merck Sharp & Dohme Ltd.Inventors: Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street
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Patent number: 6204273Abstract: Compounds of the Formula I are inhibitors of the 5&agr;-reductase 1 isozyme, and are useful alone, or in combination with a 5&agr;-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.Type: GrantFiled: January 29, 1999Date of Patent: March 20, 2001Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
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Patent number: 6191148Abstract: The present invention describes an improved process for the preparation, isolation, and purification of the anti-ulcer agent omeprazole whereby the sulfide precursor pyrmetazole is reacted subsurfacely with exactly one molar equivalent of meta-chloroperoxybenzoic acid in a chlorinated aliphatic hydrocarbon or aromatic hydrocarbon solvent, such as methylene chloride or toluene; residual organic solvent is removed from the aqueous layer by vacuum distillation; crude product is obtained by reactive crystallization with an alkyl formate or formic acid solution and seeding; and pure product is isolated by recrystallization in methanol-water containing aqueous NaOH by subsurface addition of aqueous acetic acid to pH 9.0, seeding, filtration, washing, and drying. Omeprazole and compositions of omeprazole containing no chromatographically detectable levels of residual non-alcoholic organic reaction solvent and diminished levels of alcoholic solvent are also described.Type: GrantFiled: December 15, 1999Date of Patent: February 20, 2001Assignee: Merck & Co., Inc.Inventors: James W. McManus, Nick Anousis, Benjamin Newton Banks, Hui Liu, Lingwen Zhou
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Patent number: 6166213Abstract: The present invention describes an improved process for the preparation, isolation, and purification of the anti-ulcer agent omeprazole whereby the sulfide precursor pyrmetazole is reacted subsurfacely with exactly one molar equivalent of meta-chloroperoxybenzoic acid in methylene chloride or toluene solution; residual organic solvent is removed from the aqueous layer by vacuum distillation; crude product is obtained by reactive crystallization with an alkyl formate and seeding; and pure product is isolated by recrystallization in methanol-water containing aqueous NaOH by subsurface addition of aqueous acetic acid to pH 9.0, seeding, filtration, washing, and drying. Compositions of omeprazole containing no chromatographically detectable levels of residual non-alcoholic organic reaction solvent are also described.Type: GrantFiled: October 9, 1998Date of Patent: December 26, 2000Assignee: Merck & Co., Inc.Inventors: Nick Anousis, James W. McManus, Benjamin Newton Banks, Lingwen Zhou, Hui Liu
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Patent number: 6147103Abstract: The present invention describes an improved process for the preparation, isolation, and purification of the anti-ulcer agent omeprazole whereby the sulfide precursor pyrmetazole is reacted subsurfacely with exactly one molar equivalent of meta-chloroperoxybenzoic acid in methylene chloride or toluene solution; residual organic solvent is removed from the aqueous layer by vacuum distillation; crude product is obtained by reactive crystallization with an alkyl formate and seeding; and pure product is isolated by recrystallization in methanol-water containing aqueous NaOH by subsurface addition of aqueous acetic acid to pH 9.0, seeding, filtration, washing, and drying. Compositions of omeprazole containing no chromatographically detectable levels of residual non-alcoholic organic reaction solvent are also described.Type: GrantFiled: September 1, 1999Date of Patent: November 14, 2000Assignee: Merck & Co., Inc.Inventors: Nick Anousis, James W. McManus, Benjamin Newton Banks, Lingwen Zhou
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Patent number: 6143773Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O).sub.p R.sup.1, OR.sup.1 or NR.sup.1 R.sup.12 ;B is optionally substituted 5- or 6-membered heteroaromatic ring or C(O)NR.sup.10 R.sup.11 ;R.sup.1 is hydrogen, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl, optionally substituted aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl or an optionally substituted 5- or 6-membered heteroaromatic ring;R.sup.2 and R.sup.3 are hydrogen or C.sub.1-6 alkyl;R.sup.4 is hydrogen, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, aryl or CH.sub.2 (CO).sub.m NR.sup.8 R.sup.9 ;R.sup.5 is NR.sup.6 R.sup.7, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;R.sup.6 is independently as defined for R.sup.4 ;R.sup.Type: GrantFiled: April 22, 1999Date of Patent: November 7, 2000Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, Mark Stuart Chambers
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Patent number: 6114132Abstract: Disclosed is a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfhydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfhydryl, --SH (or --S.sup.-), in the cysteine, which then adversely affects the binding ability of the enzyme.Type: GrantFiled: November 4, 1997Date of Patent: September 5, 2000Assignee: Merck Frosst Canada & Co.Inventors: Sylvie Desmarais, Michael Gresser, Richard Friesen, Brian Kennedy, Don Nicholson, Kathryn Skorey, Chidambaran Ramachandran, Anthony Ford-Hutchinson
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Patent number: 6090805Abstract: This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.Type: GrantFiled: June 10, 1998Date of Patent: July 18, 2000Assignee: Merck & Co., Inc.Inventors: Peter D. Williams, Michelle A. Sparks, Ian Bell, Debra S. Perlow, Kenneth Stauffer, Roger M. Freidinger
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Patent number: 6090944Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors .alpha.v.beta.3, .alpha.v.beta.5 and/or .alpha.v.beta.6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, and tumor growth and metastasis.Type: GrantFiled: August 10, 1999Date of Patent: July 18, 2000Assignee: Merck & Co., Inc.Inventor: John H. Hutchinson
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Patent number: 6066715Abstract: Disclosed are new ligands for use in a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfihydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfihydryl, --SH (or --S.sup.-), in the cysteine, which then adversely affects the binding ability of the enzyme.Type: GrantFiled: November 4, 1997Date of Patent: May 23, 2000Assignee: Merck Frosst Canada & Co.Inventors: Sylvie Desmarais, Richard Friesen, Robert Zamboni
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Patent number: 6066648Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the vitronectin receptors .alpha..nu..beta.3 and/or .alpha..nu..beta.5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, viral disease, and tumor growth.Type: GrantFiled: December 15, 1998Date of Patent: May 23, 2000Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Robert S. Meissner, James J. Perkins
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Patent number: 6063783Abstract: A class of substituted 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives as shown in Formula I, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABA.sub.A receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of pain.Type: GrantFiled: December 10, 1998Date of Patent: May 16, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Raymond George Hill
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Patent number: 6054469Abstract: Compounds having formula I, or salts or prodrugs thereof: ##STR1## are selective agonists of the 5-HT.sub.1D.alpha. receptor and are useful in the treatment of migraine and associated conditions.Type: GrantFiled: April 29, 1998Date of Patent: April 25, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Sylvie Bourrain, Angus Murray MacLeod, Graham Andrew Showell
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Patent number: 6054456Abstract: The present invention provides a compound of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein Z, E, Q, T, U, V and L are as defined herein; processes for its preparation and its use in the treatment of conditions for which the administration of an agonist selective for the 5-HT.sub.1D.alpha. receptor subtype is indicated, such as migraine.Type: GrantFiled: May 26, 1998Date of Patent: April 25, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Michael Rowley
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Patent number: 6048861Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors .alpha.v.beta.3, .alpha.v.beta.5, and/or .alpha.v.beta.6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.Type: GrantFiled: December 15, 1998Date of Patent: April 11, 2000Assignee: Merck & Co., Inc.Inventors: Ben C. Askew, Paul J. Coleman, Mark E. Duggan, Wasyl Halczenko, George D. Hartman, Cecilia A. Hunt, John H. Hutchinson, Robert S. Meissner, Michael A. Patane, Garry R. Smith, Jiabing Wang
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Patent number: 6048869Abstract: The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, ester, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase. The compounds of formula I are useful in the oral, systemic, parenteral or topical treatment of hyperandrogenic conditions. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis the treatment of sweat-related conditions such as apocrine gland sweating, hyperhidrosis, and hydradenitis suppurativa, the treatment of polycystic ovary syndrome, the prevention and treatment of bone loss and related diseases, and the prevention and treatment of premature labor are provided, as well as pharmaceutical compositions for the compounds of formula I.Type: GrantFiled: July 26, 1999Date of Patent: April 11, 2000Assignee: Merck & Co., Inc.Inventors: Derek Von Langen, Susan D. Aster, Donald W. Graham