Patents Represented by Attorney, Agent or Law Firm Carol S. Quagliato
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Patent number: 5468860Abstract: Disclosed is a new process for producing finasteride which involves reacting the magnesium halide salt of 17.beta.B-carboalkoxy-4-aza-5.alpha.-androst-1-en-3-one with t-butylamino magnesium halide, present in at least a 2:1 molar ratio to the ester, formed from t-butyl amine and an aliphatic/aryl magnesium halide at ambient temperature in an inert organic solvent under an inert atmosphere followed by heating and recovering said product finasteride.Also disclosed are two polymorphic crystalline Forms I and II of finasteride, and methods of their production.Type: GrantFiled: January 29, 1993Date of Patent: November 21, 1995Assignee: Merck & Co., Inc.Inventors: Ulf H. Dolling, James A. McCauley, Richard J. Varsolona
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Patent number: 5463067Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.Type: GrantFiled: January 26, 1994Date of Patent: October 31, 1995Assignee: Merck & Co., Inc.Inventors: David Askin, Kan K. Eng, Ralph P. Volante
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Patent number: 5447717Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferass and farnesylation of the oncogene protein Ras and thus useful in treating cancer.Type: GrantFiled: February 25, 1993Date of Patent: September 5, 1995Assignee: Merck & Co., Inc.Inventor: Tesfaye Biftu
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Patent number: 5438061Abstract: Compounds of the formula I ##STR1## wherein R.sub.1 hydrogen or methyl; R.sub.2 is methyl; R.sub.3 hydrogen, Alk-R.sub.4, X-Alk, C.sub.1-6 -X-Alk, XCO-Alk, CN, CO-Alk, CO-Ar, CO-O-Alk, CO-NH-Alk, CO-NH-Ar, CO-NH-Het and CO-N(Alk).sub.2 ; Alk is C.sub.1-12 straight or branched alkyl; Ar is phenyl, Het is piperidinyl, piperizinyl, pyrrolidinyl, pyrrolyl, furanyl or thienyl and X is O, N or S. Such compounds are useful in the treatment of pathologic conditions that benefit from blockade of isozymes of 5.alpha.-reductase.Type: GrantFiled: July 16, 1993Date of Patent: August 1, 1995Assignee: Merck & Co., Inc.Inventors: Jeffrey P. Bergman, Donald W. Graham, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
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Patent number: 5420024Abstract: An immobilized lipase is employed in an organic solvent to esterify diol lactone derivatives of HMG-CoA reductase inhibitors to form HMG-CoA reductase inhibitors of formula (I). ##STR1## This process allows for the efficient, one-step production of HMG-CoA reductase inhibitors of structural formula (I).Type: GrantFiled: May 11, 1993Date of Patent: May 30, 1995Assignees: Merck & Co., Inc., The University of Virginia Alumni Patents FoundationInventors: Giorgio Carta, Michael J. Conder, John L. Gainer, Robert W. Stieber, Victor A. Vinci, Timothy W. Weber
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Patent number: 5413999Abstract: Compounds of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, or R.sup.1 and R.sup.2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of treating infection by HIV are also described.Type: GrantFiled: May 7, 1993Date of Patent: May 9, 1995Assignee: Merck & Co., Inc.Inventors: Joseph P. Vacca, Bruce D. Dorsey, James P. Guare, M. Katharine Holloway, Randall W. Hungate, Rhonda B. Levin
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Patent number: 5326783Abstract: This invention is directed to compounds of formula (I) which are novel C3- or C5-acyl sulfonamide, carboxamic acid or tetrazolyl analogs of the Zaragozic acids. These compounds inhibit the enzyme squalene synthase and are useful as cholesterol lowering agents.Type: GrantFiled: January 19, 1993Date of Patent: July 5, 1994Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Chan-Hwa Kuo, Conrad Santini
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Patent number: 5314506Abstract: Impinging fluid jet streams are used in a continuous crystallization process to achieve high intensity micromixing of fluids so as to form a homogeneous composition prior to the start of nucleation. This process permits direct crystallization of high surface area particles of high purity and stability.Type: GrantFiled: November 18, 1991Date of Patent: May 24, 1994Assignee: Merck & Co., Inc.Inventors: Michael Midler, Jr., Edward L. Paul, Edwin F. Whittington, Mauricio Futran, Paul D. Liu, Jaanpyng Hsu, Shih-Hsie Pan
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Patent number: 5290689Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6969) ATCC No. 55280. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.Type: GrantFiled: September 28, 1992Date of Patent: March 1, 1994Assignee: Merck & Co., Inc.Inventors: George M. Garrity, Magda M. Gagliardi, Shieh-Shung T. Chen
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Patent number: 5288507Abstract: This invention relates to a pharmaceutical composition for use in the treatment of pain and inflammation and the treatment of acid indigestion, sour stomach, heartburn and symptoms of upset stomach associated with these conditions in a mammalian organism, said composition comprising:(i) an analgesically and anti-inflammatory effective amount of (S)-ibuprofen, or a salt thereof, substantially free of (R)-ibuprofen;(ii) an amount effective in the treatment of acid indigestion, sour stomach and/or heartburn of at least one of the antacids; and(iii) optionally, an amount effective in treating excess gas and flatulence of an anti-gas agent.Type: GrantFiled: July 29, 1992Date of Patent: February 22, 1994Assignees: Merck & Co., Inc., McNeill-PPC, Inc.Inventors: Robert T. Sims, Thomas N. Gates, William Slivka
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Patent number: 5283183Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6971) ATCC No. 55282. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.Type: GrantFiled: September 28, 1992Date of Patent: February 1, 1994Assignee: Merck & Co., Inc.Inventors: George M. Garrity, Shieh-Shung T. Chen
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Patent number: 5278159Abstract: Described are new 17.beta.-aryl ester carboxylates of 4-aza-5.alpha.-androstan-3-ones and related compounds and the use of such compounds as 5.alpha.-reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenetic related disorders.Type: GrantFiled: October 6, 1992Date of Patent: January 11, 1994Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Gool F. Patel, Gary H. Rasmusson
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Patent number: 5268282Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6970) ATCC No. 55281. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.Type: GrantFiled: September 28, 1992Date of Patent: December 7, 1993Assignee: Merck & Co., Inc.Inventors: George M. Garrity, Shieh-Shung T. Chen
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Patent number: 5268281Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6968) ATCC No. 55279. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.Type: GrantFiled: September 28, 1992Date of Patent: December 7, 1993Assignee: Merck & Co., Inc.Inventors: George M. Garrity, Magda M. Gagliardi, Shieh-Shung T. Chen
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Patent number: 5267650Abstract: A child resistant drug assemblage is disclosed comprising a container having rows of spaced drug cell cavities each of which receives a unit drug dose of medication. The container is provided with a lock means that enables it to be readily opened by an adult but difficult to be opened by a child. Each of the drug dose modules has a plurality of drug cell cavities each of which can hold unit daily doses of a drug.Type: GrantFiled: October 15, 1992Date of Patent: December 7, 1993Assignee: Merck & Co., Inc.Inventor: Kenneth J. Gilbilisco
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Patent number: 5260337Abstract: This invention relates to pharmaceutical compositions for use in the treatment of pain and inflammation and the treatment of muscle spasms and associated pain, soreness and tightness of muscles in mammalian organism, said composition comprising:(i) an analgesically and anti-inflammatory effective amount of (S)-ibuprofen, or a salt thereof, substantially free of (R)-ibuprofen; and(ii) an amount effective in the treatment of muscle spasms of at least one of the muscle relaxants, or a therapeutically active stereoisomer thereof, substantially free of its other stereoisomers.Type: GrantFiled: July 29, 1992Date of Patent: November 9, 1993Assignee: Merck & Co., Inc.Inventors: Robert T. Sims, Thomas N. Gates, William Slivka
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Patent number: 5258401Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.Type: GrantFiled: September 10, 1992Date of Patent: November 2, 1993Assignee: Merck & Co., Inc.Inventors: Gregory D. Berger, Robert W. Marquis, Jr., Albert J. Robichaud, Edward M. Scolnick
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Patent number: 5256689Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents and as inhibitors of squalene synthase.Type: GrantFiled: October 26, 1992Date of Patent: October 26, 1993Assignee: Merck & Co., Inc.Inventor: Yuan-Ching P. Chiang
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Patent number: 5252612Abstract: Described is a new immunosuppressant, L-683,756, a bisdemethylated, ring rearranged derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, Actinoplanacete sp. (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.Type: GrantFiled: June 24, 1992Date of Patent: October 12, 1993Assignee: Merck & Co., Inc.Inventors: Byron H. Arison, Edward S. Inamine, Shieh-Shung T. Chen, Linda S. Wicker
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Patent number: 5215900Abstract: Fermentation of the microorganism Streptomyces sp. (MA6804), ATTC No. 55095, in the presence of the HIV reverse transcriptase inhibitor ##STR1## yields a 5-(1-hydroxy)ethyl analog which is useful in the prevention or treatment of infection by HIV and the treatment of AIDS.Type: GrantFiled: June 7, 1991Date of Patent: June 1, 1993Assignee: Merck & Co., Inc.Inventors: Shieh-Shung T. Chen, George Doss