Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each individually are hydrogen or lower alkyl optionally substituted by aryl or C.sub.3-6 -cycloalkyl;R.sup.4 and R.sup.5 either both are hydrogen or both are halogen or one is hydrogen and the other is halogen, hydroxy, lower alkoxy, aryloxy or amino; andR.sup.3 is hydrogen or, where no primary or secondary amino group is present, alkanoyl;with the proviso that all the groups R.sup.1 through R.sup.5 cannot simultaneously be hydrogen; as well as pharmaceutically acceptable salts of compounds of formula I with acids have valuable pharmacodynamic properties as non-competitive NMDA antagonists and can accordingly be used as neuroprotectives.
Abstract: A compound of the formula ##STR1## its pharmaceutically acceptable salts, and its pharmaceutically acceptable hydrolyzable esters for reducing sebum secretion and combatting acne as well as oral and topical compositions for use thereof.
Type:
Grant
Filed:
January 6, 1993
Date of Patent:
November 29, 1994
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Thomas I. Doran, Michael Rosenberger, Stanley S. Shapiro
Abstract: Expression control sequences are provided for the expression of pro- and eukaryotic proteins. These control sequences are produced by combining promoter sequences having a low signal strength and a high in vivo promoter strength and operator/repressor systems having a high association rate. Expression vectors containing such expression control sequences, microorganisms transformed with such expression vectors and methods for producing pro- and eukaryotic proteins using the expression control sequences, expression vectors and transformed microorganisms are also provided.
Abstract: A process for the manufacture of aldehydes by the catalytic reduction of carboxylic acid halides with hydrogen in the presence of an alkylene oxide.
Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen. acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.5 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.
Type:
Grant
Filed:
August 18, 1992
Date of Patent:
April 5, 1994
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Michael Klaus, Peter Mohr, Ekkehard Weiss
Abstract: Analogs of Tyrosine Sulfate or Tyrosine Phosphate containing peptides, the novel intermediate compounds used in the preparation of these analogs, as well as a method for suppressing appetite in subjects by administering to the subject an effective amount of CCK analog wherein one or more of any Tyrosine Sulfate present is substituted with a radical of the invention.
Type:
Grant
Filed:
April 9, 1992
Date of Patent:
March 22, 1994
Assignee:
Hoffman-La Roche Inc.
Inventors:
Waleed Danho, Jefferson W. Tilley, Joseph Triscari, Rolf Wagner
Abstract: The invention is concerned with a process for the manufacture of beta-isophorone from alpha-isophorone by converting alpha-isophorone into beta-isophorone in the presence of a heterogeneous catalyst in the gas phase. The heterogenous catalyst used is especially an oxide or mixed oxide of the elements Mg, Al, Si and Ni.
Abstract: Vasoactive intestinal compound analogs containing substitutions of appropriately selected amino acids at specific positions of the VIP molecule.
Abstract: Compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen, halogen or OR.sup.5 ; R.sup.2 is hydrogen, lower-alkyl lower-alkoxy or halogen; R.sup.3 and R.sup.4 each independently are lower-alkyl or taken together are alkylene with 3-5 C atoms in a straight-chain; R.sup.5 is hydrogen, acyl, lower-alkoxycarbonyl, lower-alkyl, amino-lower-alkyl, mono-alkylamino-lower-alkyl di-alkylamino-lower-alkyl or a N-containing 5-8-membered saturated or unsaturated monocyclic heterocyclic ring which is attached via a N atom to lower alkyl; and M signifies --CONH-- or --NHCO--, which can be used as medicaments, e.g., for the treatment of neoplasms and dermatological indications of an inflammatory and allergic nature.
Abstract: Phosphonium salts of the formula ##STR1## wherein A signifies aryl and Y.sup.- signifies C.sub.1 -C.sub.6 -alkanoate or hydroxytrifluoroborate, as well as their manufacture from 3,7,11-trimethyldodeca-1,4,6,10-tetraen-3-ol with a triarylphosphine and with a C.sub.1 -C.sub.6 -alkanoic acid or a boron trifluoride etherate and, if desired after conversion into the phosphonium salt of a strong acid, further reaction to give lycopene.
Abstract: Analogs of Tyrosine Sulfate or Tyrosine Phosphate containing peptides, the novel intermediate compounds used in the preparation of these analogs, as well as a method for suppressing appetite in subjects by administering to the subject an effective amount of CCK analog wherein one or more of any Tyrosine Sulfate present is substituted with a radical of the invention.
Type:
Grant
Filed:
July 18, 1991
Date of Patent:
January 26, 1993
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Waleed Danho, Jefferson W. Tilley, Joseph Triscari, Rolf Wagner
Abstract: Phosphonium salts of the formula ##STR1## wherein A signifies aryl and Y.sup.- signifies C.sub.1 -C.sub.6 -alkanoate or hydroxytrifluoroborate, as well as their manufacture from 3,7,11-trimethyldodeca-1,4,6,10-tetraen-3-ol with a triarylphosphine and with a C.sub.1 -C.sub.6 -alkanoic acid or a boron trifluoride etherate and, if desired after conversion into the phosphonium salt of a strong acid, further reaction to give lycopene.
Abstract: Retinoids of the formula R.sup.1 --OCH(R.sup.2)OC(O)R.sup.3 wherein R.sup.1 signifies 13-cis-retinoyl, R.sup.2 signifies hydrogen or lower-alkyl and R.sup.3 signifies straight-chain lower-alkyl can be used as medicaments in the case of dermatological disorders.
Abstract: Vasoactive intestinal peptide analogs containing substitutions of appropriately selected amino acids at specific positions of the VIP molecule.
Abstract: The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the significance given in claim 1, in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency.
Type:
Grant
Filed:
March 29, 1990
Date of Patent:
August 18, 1992
Assignee:
Hoffmann-La Roche, Inc.
Inventors:
Quirico Branca, Hans P. Marki, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
Abstract: Compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen, halogen or OR.sup.5 ; R.sup.2 is hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.3 and R.sup.4 each independently are lower-alkyl or taken together are alkylene with 3-5 C atoms in a straight-chain; R.sup.5 is hydrogen, acyl, lower-alkoxycarbonyl, lower-alkyl, amino-lower-alkyl, mono-alkylamino-lower-alkyl, di-alkylamino-lower-alkyl or a N-containing 5-8-membered saturated or unsaturated monocyclic heterocyclic ring which is attached via a N atom to lower alkyl; and M signifies --CONH-- or --NHCO--, which can be used as medicaments, e.g., for the treatment of neoplasms and dermatological indications of an inflammatory and allergic nature.
Abstract: The invention is directed to novel CCK analogs wherein Tryptophan and/or Phenylalamine are substituted with a radical which provides enhanced appetite suppressant activity to the peptide.
Type:
Grant
Filed:
January 10, 1990
Date of Patent:
July 7, 1992
Assignee:
Hoffman-La Roche Inc.
Inventors:
Waleed Danho, David J. Nelson, Gary L. Olson, Shian-Jan Shiuey, Jefferson W. Tilley, Rolf Wagner
Abstract: A method for the liberation of polysaccharide antigens from bacteria or fungi in biological probes or in grown cultures of these probes is described. In the majority of cases such a liberation is necessary in order that subsequently the polysaccharide antigens can be determined immunologically in a manner known per se. This liberation is effected by treating the biological probe or the grown culture with an aqueous phenol solution. A 1-10% phenol solution is conveniently used, with a 2.5% phenol solution being preferred and a 2% phenol solution being especially preferred. The phenol solution is allowed to act on the probe or culture for 5-30%, preferably 15, minutes. No extraction is necessary for the subsequent immunological determination of the polysaccharides.
Abstract: A process of producing 2-keto-L-gulonic acid from sorbose via a recombinant bacteria including expression vectors and probes for producing said recombinant bacteria.