Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method and/or solution synthesis.
Abstract: This invention relates to a novel process for the preparation of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which contain a 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety, such as compactin and mevinolin, by utilizing an alkyl 5(S),6-epoxy-3(R)-(alkoxy)hexanoate as a chiral synthon for the stereospecific introduction of the 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety.
Type:
Grant
Filed:
November 19, 1984
Date of Patent:
September 9, 1986
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Yvan Guindon, Howard E. Morton, Christiane Yoakim
Abstract: A novel process for intermediates in the synthesis and hypercholesterolemic compounds of the HMG-CoA reductase type of the following general formula (1): ##STR1## involving an enantioselective aldol condensation is disclosed.
Type:
Grant
Filed:
July 5, 1985
Date of Patent:
September 9, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Joseph E. Lynch, Ichiro Shinkai, Ralph P. Volante
Abstract: Cyclic hexapeptide somatostatin analogs are prepared wherein a peptide surrogate replaces eight of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.
Abstract: This invention relates to a novel process for the preparation of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which contain a 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety, such as compactin and mevinolin, by utilizing an alkyl 4-cyano-3(R)-hydroxybutanoate as a chiral synthon for the stereospecific introduction of the 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety.
Type:
Grant
Filed:
January 31, 1985
Date of Patent:
September 9, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Ralph P. Volante, Thomas R. Verhoeven, Meyer Sletzinger, James M. McNamara, Thomas M. H. Liu, Edward G. Corley
Abstract: Novel substituted and bridged pyrimidine compounds useful as calcium channel blockers, pharmaceutical compositions thereof, and methods of treatment are disclosed.
Type:
Grant
Filed:
February 21, 1985
Date of Patent:
September 2, 1986
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, David A. Claremon, David E. McClure
Abstract: Indeno[2,1-c]pyridine compounds, particularly cyano substituted tetrahydroindeno[2,1-c]pyridine dicarboxylic acid ester compounds, their preparation and their use as calcium entry blockers are disclosed.
Abstract: The instant invention is directed to synergistic antimicrobial admixtures comprising 2-bromo-2-bromomethylglutaronitrile and 2,2-dibromo-3-nitrilopropionamide and its use in inhibiting microbial growth.
Abstract: The instant invention is directed to a process for inhibiting corrosion and the formation and deposition of scale in aqueous systems comprising adding to the system at least 0.1 ppm. of a water soluble polymer, having an intrinsic viscosity of 0.05 to 2.5 dl/g, prepared from:(A) 50 to 95%, by weight, of an unsaturated carboxylic acid, or its salt, and(B) 5 to 50%, by weight, of a betaine-containing monomer selected from the group consisting of: ##STR1## wherein R, which may be the same or different, is hydrogen, a straight or branched, alkyl or an aryl or alkylaryl group of from 1 to 20 carbon atoms;R.sup.
Abstract: This invention relates to a novel and improved process for preparing .alpha.-(trichloromethyl) benzyl alcohols, particularly, trichloromethyl-3-nitrobenzyl alcohol a key intermediate useful in the preparation of clorsulon (4-amino-6-(trichloroethenyl)-1,3-benzene-disulfonamide) via a base-catalyzed condensation reaction of benzaldehydes and chloroform.
Abstract: Compounds of the formula: ##STR1## wherein R.sup.2 is --(CH.sub.2).sub.k --X--(CH.sub.2).sub.j --NHR.sup.3 ; wherein k is 0 to 3, j is 1 or 2; X is F or OH; and, R.sup.3 is hydrogen; loweralkyl or loweraralkyl which may be substituted by hydroxy, carboxy, carbamoyl, or carbalkoxy; or, acyl; and, a pharmaceutically acceptable salt thereof; are inhibitors of angiotensin I converting enzyme useful as antihypertensive agents.
Abstract: Novel substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit cardioselective .beta.-adrenergic blocking activity, and are useful as antihypertensive agents, cardioprotective agents, antiarrythmic agents, antianginal agents with reduced side effects; e.g., they are devoid of intrinsic sympathomimetic activity.
Type:
Grant
Filed:
February 8, 1984
Date of Patent:
July 22, 1986
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
Abstract: Novel substituted and bridged pyridine compounds useful as calcium channel blockers, pharmaceutical compositions thereof, and methods of treatment are disclosed.
Abstract: The novel compounds of this invention and their pharmaceutically acceptable salts exhibit cardioselective .beta.-adrenergic blocking activity, with a direct relaxing effect on the .beta..sub.2 -adrenergic receptors and are useful as antihypertensive, cardioprotective, antiarrhythmic and, antianginal agents.
Abstract: The instant invention is directed to a method of settling fine calcium carbonate solids from a suspension comprising water and calcium carbonate, comprising adding to said suspension an effective amount of an admixture comprising: (a) an anionic polyelectrolyte; and (b) an anionic surfactant, wherein said polyelectrolyte/surfactant ratio ranges from 10:1 to 1:5, by weight.
Abstract: [(2-Hydroxy-5-alkoxyphenyl)methylthio]phenylmethanol and derivatives thereof were prepared from an appropriate 2-hydroxy-5-alkoxybenzaldehyde with a hydroxymethylthiophenol. These compounds were found to be potent anti-inflammatory agents.
Abstract: Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared.These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.
Type:
Grant
Filed:
June 4, 1984
Date of Patent:
June 17, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Tesfaye Biftu, Thomas W. Doebber, San-Bao Hwang, Thomas R. Beattie, Tsung-Ying Shen, Robert Stevenson
Abstract: The instant invention is directed to a method for suppressing dust comprising contacting the material being treated with an aqueous emulsion of a methacrylate polymer or a composition comprising a hydrophobic liquid and a methacrylate polymer. These emulsions and compositions may further comprise a wetting/penetrating surfactant.