Abstract: A stable aqueous suspension of a mixture of magnesium hydroxide and copper oxychloride, together with a suspending agent, is used to reduce deposits in kilns or furnaces used to make iron ore agglomerates, known as pellets, during a calcination process in which iron ore fines mixed with fluxing materials having a phosphate content of less than 1% by weight of the total flux and iron ore weight, are heated to from about 900.degree. to about 1400.degree. C. in order to create the hardened iron ore pellets, called flux pellets, one of the chief raw materials in steel making.
Abstract: Compounds of the general formula ##STR1## and the pharmaceutically acceptable salts thereof whereinn is an integer of from 0 to 6;Y is CH.sub.2, O, SO.sub.2, --CONH--, --NHCO--, or ##STR2## R.sup.1 and R.sup.2 are independently hydrogen,C.sub.1-8 alkyl,heterocyclyl C.sub.0-4 alkyl,aryl C.sub.0-4 alkyl,amino C.sub.1-4 alkyl,C.sub.1-4 alkylamino C.sub.1-4 alkyl, orC.sub.3-8 cycloalkylwherein R.sup.1 and R.sup.2 may be unsubstituted or substituted with one or more groups chosen from R.sup.3, whereR.sup.3 ishydrogen,C.sub.1-6 alkyl,hydroxy C.sub.0-4 alkyl,carboxy C.sub.0-4 alkyl,C.sub.1-4 alkyloxy C.sub.0-4 alkyl,heterocyclyl C.sub.0-4 alkyl,aryl C.sub.0-4 alkyl,halogen, orCF.sub.3 ;R.sup.4 isC.sub.1-6 alkyl,heterocyclyl C.sub.0-4 alkyl, oraryl C.sub.0-4 alkyl;R.sup.5 ishydrogen,C.sub.1-6 alkyl,aryl C.sub.0-3 alkyl, orC.sub.1-6 alkylcarbonyloxymethylare used in a method of treating osteoporosis by inhibiting the bone resorption activity of osteoclasts.
Type:
Grant
Filed:
August 9, 1991
Date of Patent:
June 8, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Melissa S. Egbertson, Robert J. Gould, George D. Hartman
Abstract: The present invention is concerned with a novel biotransformation process for producing 17.beta.-N-monosubstituted carbamoyl-11-oxo-4-aza-5-.alpha.-androst-3-ones of the formula: ##STR1## These compounds are testosterone 5-.alpha. reductase inhibitors and are produced via a claimed novel biotransformation process using the green algae, Selenastrum capricornutum.
Type:
Grant
Filed:
February 25, 1992
Date of Patent:
June 1, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Byron H. Arison, Josephine R. Carlin, Edamanal S. Venkataramani
Abstract: 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.
Abstract: Novel fungicidal compositions comprising a pyranyl glycine ester compound and a .beta.-lactone compound and a method for controlling mycotic infections is disclosed.
Abstract: There is disclosed a medication container which is adapted to be side loaded with unit doses of medication during packaging operations. After being filled with the unit doses of medication, the container side is sealed. The medication doses can be removed by a user from the sealed container by means of a removable closure at one end of the container.
Abstract: There is disclosed an automated system for testing the sterility of products intended for human health administration or for human consumption. The system permits a plurality of samples of a product to be concurrently tested and is arranged so that multiple samples of a product to be tested can be mixed and then conveyed to test canisters along with appropriate growth media prior to determining that the product is sterile or is free from microbial contamination.
Abstract: Described is a new process for selectively acylating FK-506 type immunosuppressant macrolides, including immunomycin (FK-520), in the C-32 position, under novel conditions utilizing an immobilized lipase enzyme, an acyl donor, and a dry, non hydroxylic organic solvent. The enzyme is absorbed onto a solid support and the enzyme/support catalyzes the C-32 acylation. The enzyme/support complex can then be filtered from the reaction mixture and, recycled for use.
Type:
Grant
Filed:
June 25, 1990
Date of Patent:
May 11, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Brian R. Petuch, Shieh-shung T. Chen, Byron H. Arison
Abstract: Aminomacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by incorporation of a nitrogen substituent at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma.
Type:
Grant
Filed:
May 13, 1991
Date of Patent:
May 4, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Hyun O. Ok, Thomas R. Beattie, Michael H. Fisher, Matthew J. Wyvratt, Mark Goulet
Abstract: N-Heteroaryl, N-alkylheteroaryl, N-alkenylheteroaryl and N-alkynylheteroaryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by amination, alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma. Furthermore, these macrolides are useful as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis.
Type:
Grant
Filed:
September 9, 1991
Date of Patent:
May 4, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Hyun O. Ok, Joung Goulet, Peter J. Sinclair
Abstract: There is disclosed a child resistant cap and container assemblage comprising a container and a cap member that is secured to the container so that it can not be removed without either breaking the cap member or damaging the seal that joins the cap member to the container. The cap member is provided with a nozzle having an internal locking means so that the contents of the container can not be accessed when the container is in its normal upright position. To access the contents in the container, the assemblage is titled to disengage the locking means enabling the nozzle to be opened and permitting a user to access the contents of the container using only one hand.
Abstract: The invention is a highly efficient synthesis for making compounds of the formula: ##STR1## wherein: R.sup.1 is a six member saturated or unsaturated heterocyclic ring containing one or two heterocyclic atoms wherein the heteroatoms are N; or NR.sup.6, wherein R.sup.6 is H or C.sub.1-10 alkyl;m is an integer from two to six; andR.sup.4 is aryl, C.sub.1-10 alkyl, or C.sub.4-10 aralkyl.
Type:
Grant
Filed:
February 28, 1992
Date of Patent:
April 27, 1993
Assignee:
Merck & Co., Inc.
Inventors:
John Y. L. Chung, David L. Hughes, Dalian Zhao
Abstract: Compounds of the formula: ##STR1## where R.sup.1 is hydrogen or hydroxy and R.sup.2 is a substituted amino group, a substituted heterocyclic ring or a substituted alkyl. These compounds are oxytocin and vasopressin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery, timing of parturition, uterine hyperactivity, endometriosis, hypertension, congestive heart failure, hyponatremia and cognitive disorders. Also disclosed are pharmaceutical compositions containing these compounds, methods of their use and methods of their preparation.
Type:
Grant
Filed:
September 16, 1991
Date of Patent:
April 20, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Mark G. Bock, Ben E. Evans, Roger M. Freidinger, Kevin Gilbert, Doug W. Hobbs, James B. Hoffman, George F. Lundell, Douglas J. Pettibone
Abstract: Compounds of the general formula ##STR1## Y is an integer of from 0 to 6 is chosen from: O,SO.sub.2,--CONH--,--NHCO--,--CH2-- or ##STR2## R.sup.1 is substituted or unsubstituted mono- or polycyclic saturated hetero-cyclic ring system having 1, 2 or 3 heteroatoms where said heteroatoms are independently chosen from N, O and S and said substituents are chosen from the group comprising R.sup.2 ;R.sup.2 isC.sub.1-6 alkyl,aryl C.sub.0-6 alkyl,hydroxy C.sub.0-6 alkyl,C.sub.1-6 alkoxy C.sub.0-6 alkyl,carboxy C.sub.0-6 alkyloxo,halogen,CF.sub.3,C.sub.0-4 alkylamino-C.sub.0-6 alkyl orC.sub.0-4 dialkylamino-C.sub.0-6 alkyl;R.sup.3 isC.sub.1-8 alkyl or cycloalkyl,aryl C.sub.0-4 alkyl,hydroxy C.sub.0-4 alkylC.sub.1-4 alkyloxy C.sub.0-4 alkyl,carboxy C.sub.0-4 alkyl,halogen,CF.sub.3 orhydrogen;R.sup.4 ishydrogen,C.sub.1-6 alkyl,aryl C.sub.0-4 alkyl orC.sub.1-6 alkylcarbonyloxymethyl; andR.sup.5 isC.sub.1-6 alkyl,aryl C.sub.0-4 alkyl orheterocycly C.sub.
Type:
Grant
Filed:
August 9, 1991
Date of Patent:
April 20, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Melissa S. Egbertson, George D. Hartman, Robert J. Gould
Abstract: Described is a new microorganism, Actinoplanacete sp., (Merck Culture Collection MA 6559) ATCC No. 53771. The microorganism acts as a demethylating agent and can produce the new immunosuppressants, "demethomycin" (L-682,993) a C-31 demethylated analog of L-679,934, and "demethimmunomycin" (L-683,742) a C-31 demethylated analog of L-683,590, under novel fermentation conditions. These macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
Type:
Grant
Filed:
March 9, 1992
Date of Patent:
April 13, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Shieh-Shung T. Chen, Byron H. Arison, George M. Garrity, Edward S. Inamine, Sagrario Mochales, Linda S. Wicker
Abstract: Incubation of 3-[2-benzoxazol-2-yl)ethyl]-5-ethyl-6-methyl-2-(1H)-pyridinone ##STR1## with a preparation from mammalian organ yields as biotransformation product the 6-hydroxymethyl analog. This product is useful in the prevention or treatment of infection by HIV and the treatment of AIDS.
Abstract: Incubation of 3-[(4,7-dichlorobenzoxazol-2-yl)methyl]amino-5-ethyl-6-methyl-2-(1H)-pyrid inone ##STR1## with a preparation from mammalian organ yields as biotransformation products the 5-(1-hydroxy)ethyl and 6-hydroxymethyl analogs. These products are useful in the prevention or treatment of infection by HIV and the treatment of AIDS.
Type:
Grant
Filed:
March 10, 1992
Date of Patent:
April 6, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Suresh K. Balani, Anthony D. Theoharides, Laura R. Kauffman
Abstract: S(+)-ibuprofen-L-amino acids and S(+)-ibuprofen-D-amino acids, substantially free of other ibuprofen-amino acid stereoisomers, give an onset-hastened, enhanced analgesic response in humans.
Abstract: A method for inhibiting oxytocin activity by administering an oxytocin inhibiting amount of a penicillide compound having the formula ##STR1## and compositions for such use are described.
Abstract: Described is a process for producing a new immunosuppressant, a C-31 desmethyl, C-19/C-22 cyclic hemiketal biotransformation analog (Compound I) of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces, lavendulae ATCC No. 55209. Also disclosed is the C-31 methylated derivative (Compound II) of Compound I produced by enzymatic methylation using 31-O-desmethylimmunomycin O-methyl transferase, (DIMT), a methyl transferase enzyme. The macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
Type:
Grant
Filed:
August 28, 1991
Date of Patent:
March 30, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Magda M. Gagliardi, Shieh-Shung T. Chen, George M. Garrity