Abstract: Valuable 9.alpha.-hydroxy steroids are prepared via microbial enzymatic oxidation (MEO) by conventional fermentation means, without the need for a .DELTA..sup.1 dehydrogenation inhibitor, utilizing novel microorganism Nocardia canicruria ATCC 31548. Also disclosed is a novel method using any .DELTA..sup.1 dehydrogenase producing organism and a novel bio-reactor technique means for preparing said steroids.
Type:
Grant
Filed:
June 12, 1981
Date of Patent:
August 9, 1983
Assignee:
G. D. Searle & Co.
Inventors:
William J. Marsheck, James Jiu, Ping T. Wang
Abstract: 1-Cycloalkyl phosphonium salts represented by the formula ##STR1## wherein: R is selected from the group consisting of lower alkyl, hydroxy lower alkyl, halo lower alkyl, amino lower alkyl, cyano lower alkyl, lower alkenyl with the limitation that the double bond is not on the carbon atom attached to the oxygen atom, benzyl, substituted benzyl and ##STR2## wherein q is O or 1 and R.sub.4 is selected from the group consisting of hydroxy, loweralkoxy, phenyl, substituted phenyl, and ##STR3## wherein R.sub.5 and R.sub.6 are the same or different members of the group consisting of hydrogen and loweralkyl or taken together form a 5 or 6 membered ring; m is 1, 2 or 3; n is 0 or 1; o is 0 or 1; p is 0 or 1; R.sub.1, R.sub.2 and R.sub.3 are the same or different members of the group consisting of hydrogen, lower alkyl, lower alkoxy and halo; and X is a pharmaceutically acceptable anion. The compounds are useful as analgesic agents.
Abstract: The invention relates to certain urea derivatives of the formula R.sub.1 CH.sub.2 S(CH.sub.2).sub.2 NHCONHR.sub.2 where R.sub.1 are certain furanyls, imidazoles and thiazolyls and R.sub.2 are certain imidazoles and thiazolyls. These compounds are H-2 histamine receptor inhibitors and therefore useful in the treatment of ulcers.
Type:
Grant
Filed:
August 25, 1981
Date of Patent:
May 31, 1983
Assignee:
G. D. Searle & Co.
Inventors:
Richard E. L. Henderson, Barnett S. Pitzele
Abstract: The present invention relates to novel compounds for the prophylaxis and treatment of Inflammatory Bowel disease (IBD) via the administration of an effective amount in a suitable pharmaceutical dosage of a polymeric agent for releasing 5,5'-azobis-salicylic acid which comprises a non-degradable anionic exchange resin and the dianionic form of 5,5'-azobis-salicylic acid. The 5,5'-azobis-salicylic acid undergoes bacterial cleavage in the mammalian lower bowel to release 5-aminosalicylic acid.
Abstract: A process for the production of a synthetic gene for an influenza haemagglutinin which comprises:(a) subjecting isolated vRNA to the action of reverse transcriptase to produce a double-stranded RNA/DNA hybrid;(b) digesting the RNA component of the hybrid;(c) treating the residual DNA component of the hybrid to produce a double-stranded DNA molecule having one "hairpin" end; and(d) treating the "hairpin" structure with a single-strand specific nuclease to produce a bimolecular double-stranded copy of the vRNA.
Abstract: 1-Piperidinylmethyl benzenamines represented by the formula: ##STR1## wherein X is S or --CH.sub.2 --CH.sub.2 --; R.sub.1 and R.sub.2 are the same different members of the group consisting of hydrogen or lower alkyl; and the pharmaceutically acceptable salts thereof. The compounds are useful as anti-allergic and antihypertensive agents.
Abstract: The invention provides certain substituted tryptophan derivatives of Formula I which are useful for alleviating or reducing angiotensin related hypertension in hypertensive mammals.
Abstract: Compounds corresponding to the following general formula: ##STR1## wherein Ar and Ar.sup.1, which may be the same or different, each represents an aromatic radical which may be substituted one or more times by halogen and/or nitro and/or lower alkyl and/or trihalomethyl and/or cyano and/or lower alkoxy and/or di-lower alkyl-amino, the alkyl groups optionally completing a ring optionally incorporating a further heteroatom, and/or lower alkyl sulphonyl;Alk.sup.1 and Alk.sup.2, which may be the same or different, each represents an alkylene group containing from one to eight carbon atoms which may be substituted one or more times by aryl and/or cycloalkyl and/or lower alkyl and if two such alkyl groups are present, they may complete a ring optionally containing a heteroatom and in which imidazole ring may be further substituted; and m represents 0 or 1; provided that not both Ar and Ar.sup.1 represent phenyl; and acid addition salts thereof.
Type:
Grant
Filed:
January 16, 1981
Date of Patent:
September 28, 1982
Assignee:
G.D. Searle & Co.
Inventors:
Peter J. Fellner, Brendan J. Hamill, Paul W. Manley
Abstract: 25-Substituted-5.alpha.-cholestane-3.beta.,22S-diols and esters thereof of Formula I which inhibit the activity of 3-hydroxy-3-methyl-glutaryl coenzyme A reductase and inhibit the formation of serum cholesterol are disclosed.
Abstract: Derivatives of .alpha.,.beta.-unsaturated ketones having anticonvulsant activity and methods of their preparation from heterocyclic phosphonium salts and acyclic phosphoranes are disclosed.
Abstract: Animal cells are grown in a vertically disposed cylindrical vessel containing a stack of parallel spaced-apart discs inclined at least 5.degree. from the horizontal and mounted to a rotatable axial shaft. The vessel is closed by a top plate having a plurality of inlets and a bottom plate with an outlet, and contains an external pumping loop for circulating contents of the vessel from the bottom to the top of the vessel. Growing of the cells is carried out by substantially filling the vessel with a mixture of animal cells and growth medium, allowing the cells to settle on the disc surfaces and then rotating the axial shaft at a speed of at least 5 rpm while continuously circulating the vessel contents from the bottom to the top of the vessel. This process and apparatus provides efficient mixing and ensures a homogeneous system within the vessel.
Type:
Grant
Filed:
August 21, 1980
Date of Patent:
August 10, 1982
Assignee:
G. D. Searle & Co.
Inventors:
John R. Birch, Terence Cartwright, John A. Ford
Abstract: The present invention provides a trans-dermal delivery pad for nitroglycerin administration, specifically a microsealed, trans-dermal nitroglycerin pad having a backing which is impervious to nitroglycerin absorption and transport and a silicon matrix affixed thereto, said silicone polymer matrix being of cross-linked silicone rubber having from about 10 to 200 micron microsealed compartments being formed by in situ cross-linking of the silicone rubber after it is mixed with a hydrophilic solvent system containing the nitroglycerin and a hydrophobic solvent which enhances nitroglycerin dispersion and transport.
Type:
Grant
Filed:
May 4, 1981
Date of Patent:
June 22, 1982
Assignee:
G. D. Searle & Co.
Inventors:
Dilip R. Sanvordeker, James G. Cooney, Ronald C. Wester
Abstract: A compound of the formula ##STR1## wherein R is hydrogen or lower alkyl having 1-7 carbon atoms; R', R", and R'" are each individually hydrogen or methyl; n is 0-3; and Ar is phenyl, halosubstituted phenyl, lower alkyl substituted phenyl wherein the lower alkyl contains 1-4 carbon atoms, lower alkoxy substituted phenyl wherein the lower alkoxy contains 1-4 carbon atoms, p-biphenyl, or trifluoromethyl substituted phenyl. Compounds of the present invention are useful as antifertility agents.
Abstract: An enkephalin derivative represented by the formula(.+-.) H-2,6-C-diMeTyr-(D)X-Gly-Phe-N(CH.sub.2).sub.m COORwherein: X is methionine, alanine or nor-leucine; m is 3 or 5; and R is selected from the group consisting of hydrogen, lower alkyl or -NR.sub.2 R.sub.3 wherein R.sub.2 and R.sub.3 are the same or different members of the group consisting of hydrogen and lower alkyl, wherein the (.+-.) refers to the compound shown, its mirror image or a mixture of racemates; or the pharmaceutically acceptable salts thereof. The compounds are useful as analgesic agents.