Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
Type:
Grant
Filed:
May 12, 1995
Date of Patent:
May 14, 1996
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
Abstract: A novel process for the asymmetric hydrogenation of compounds of the formula: ##STR1## wherein R represent aryl or heteroaryl, to compounds of the formula: ##STR2## wherein R has the above significance, is carried out using rhodium-diphosphine complexes.
Type:
Grant
Filed:
April 8, 1994
Date of Patent:
May 7, 1996
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Emil A. Broger, Werner Hofheinz, Arthur Meili
Abstract: Sulphonic acid esters of formula ##STR1## wherein R1 is lower-alkyl or phenyl, useful as intermediates in the production of .beta.-aminoalcohols.
Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, and X is H.sub.2 or .dbd.CH.sub.2 are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of cancer, such as, leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.
Type:
Grant
Filed:
April 11, 1995
Date of Patent:
April 30, 1996
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Enrico G. Baggiolini, deceased, Shian-Jan Shiuey, Milan R. Uskokovic
Abstract: Methods and reagents are provided for the amplification of DNA sequences longer than 10 kilobases by the polymerase chain reaction (PCR). The methods use compositions consisting of a primary thermostable DNA polymerase from Thermus thermophilus combined with a lesser amount of a secondary thermostable DNA polymerase possessing a 3'-to-5' exonuclease activity from Thermococcus litoralis, Pyrococcus species GB-D or Thermotoga maritima. The DNA polymerase compositions, when used with the disclosed reaction buffer, enable amplifications of DNA sequences up to at least 42.2 kilobases in length.
Abstract: An analyzer has a horizontally disposed baseplate on which primary containers and secondary containers are disposed, a pipetting needle, a transport device, and a control device. The pipetting needle is formed of an electrically conductive material and is connected to a metering device by a tubing, and is for transferring a predetermined volume of liquid each time from a primary container to a secondary container. The transport device is for the controlled transport of the pipetting needle in three directions at right angles to one another, two of the transport directions extending horizontally and the third transport direction extending vertically. The control device is for controlling the metering device and the transport device.
Type:
Grant
Filed:
April 11, 1995
Date of Patent:
April 30, 1996
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Guido Bonacina, Thomas Caratsch, Rolf Moser
Abstract: Compounds of the formula ##STR1## in which X is --S--, --SO-- or --SO.sub.2 --; R.sup.1 is C.sub.7-10 -alkyl or C.sub.7-10 -alkoxy; R.sup.2 is a residue of the formula ##STR2## R.sup.3 is carboxy or lower-alkoxycarbonyl; and n is an integer of 1, 2 or 3; and salts of carboxylic acids of formula I can be used for the treatment of autoimmune diseases and diseases having a strong immunological component, such as psoriasis.
Abstract: A process for the preparation of hypoallergenic moss oils, comprising reacting the starting moss oil, a concrete or preferably an absolute thereof, with an aldehyde reducing agent, in an organic solvent medium.
Abstract: There are described compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxycarbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formulaQ--X--Y-- (a)wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --;and in which R.sup.1 signifies hydrogen, halogen, carbamoyloxy, lower alkanoyloxy or a group of the formula --S--Het, wherein Het represents a 5- or 6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and R.sup.2 represents the sulpho group --SO.sub.3 H or R.sup.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
April 23, 1996
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Robert Charnas, Klaus Gubernator, Ingrid Heinze, Christian Hubschwerlen
Abstract: Novel odorant compositions which are characterized by a content of one or more compounds selected from the group consisting of tetrahydrofurans of structures 1 or 2, or tetrahydropyrans of structure 3. ##STR1## wherein R can be an acyclic, where acyclic refers to a chain of at least four carbon atoms substituted with at least three methyl groups in the chain, carbocyclic, where carbocyclic refers to a ring of 5-8 carbon atoms, and with at least two methyl groups on the ring, or bicyclic where bicyclic refers to two carbon rings, each ring having between 5-8 carbon atoms fused together, substituted with at least two methyl groups, and where R.sub.1 .dbd.CH.sub.3, or higher alkyl group, R.sub.2 .dbd.H, CH.sub.3, or higher alkyl group, R.sub.3 .dbd.H, or CH.sub.3, R.sub.4 and R.sub.5 .dbd.H, CH.sub.3, or higher alkyl group.
Abstract: Novel, racemic and optically active phosphorus compounds of the formula ##STR1## wherein R signifies lower alkyl, lower alkoxy, hydroxy or a protected hydroxy group, R.sup.1 and R.sup.2 are different from each other and represent lower alkyl, cycloalkyl, aryl, a five-membered heteroaromatic or a group of the formula ##STR2## are described. The compounds of formula I are useful in the form of complexes with a metal of Group VIII as catalysts for asymmetric hydrogenations and for enantioselective hydrogen displacements in prochiral allylic systems.
Abstract: The present invention provides methods and reagents for the detection and identification of four causative agents of genital ulcerations, herpes simplex virus (HSV) types 1 and 2, Treponema pallidum, and Haemophilus ducreyi. The methods use sequence-specific primers which enable the simultaneous polymeric chain reaction amplification of genomic nucleic acid sequences from HSV types 1 and 2, T. pallidum, and H. ducreyi. Following amplification, sequence-specific oligonucleotide probes are used to detect and distinguish HSV type 1 and 2, T. pallidum, and H. ducreyi nucleic acid.
Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
Type:
Grant
Filed:
May 12, 1995
Date of Patent:
April 16, 1996
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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:
December 17, 1993
Date of Patent:
April 16, 1996
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Waleed Danho, Jefferson W. Tilley, Joseph Triscari, Rolf Wagner
Abstract: This invention relates to a process for the amplification of nucleic acids in the form of DNA or RNA from blood samples by means of an enzymatic amplification method, characterized in that no preparation of the blood sample otherwise necessary to prepurify the nucleic acid to be amplified is performed and the proportion of the sample in the reaction mixture for the amplification process is greater than 5 volume % if a specific amount of salt is present in the reaction mixture. Depending on the proportion of blood sample and its salt contribution of monovalent and/or bivalent ions, the salt concentration in the reaction mixture in which the amplification is performed is, where applicable, adapted to the enzyme requirements by the use of an appropriately concentrated salt solution.
Abstract: The present invention provides a novel immunoassay for the detection of multiple analytes such as amphetamine and methamphetamine in a single assay of a biological fluid sample. In this assay, a single labelled binding partner is utilized capable of cross reacting at differing sensitivities to antibodies derived from conjugate derivatives of the different analytes such that the presence of the analytes at selected levels of concentration of the analytes singly or in combination can be detected.
Type:
Grant
Filed:
June 10, 1994
Date of Patent:
March 26, 1996
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Kathy P. Ordonez, Salvatore J. Salamone
Abstract: A process for the manufacture of 5-cyano-4-lower alkyl-oxazoles is described in which a 5-carbamoyl-4-lower alkyl-oxazole is dehydrated in an organic solvent under mild conditions with cyanuric chloride and an N,N-disubstituted-formamide.
Type:
Grant
Filed:
February 16, 1994
Date of Patent:
March 26, 1996
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Werner Bonrath, Reinhard Karge, Horst Pauling
Abstract: The invention relates to intermediate compounds which are useful in the preparation of N-tert-butyl-decahydro-2- 2 (R)-hydroxy-4-phenyl-3(S)-phthalimidobutyl!-(4aS, 8aS)-isoquinoline-3(S)-carboxamide. The final products are suitable for the treatment of vital infections, such as those caused by HIV and other retroviruses.
Abstract: Vitamin E acetate, C.sub.3 -linked triesters, glycerin, t-butanol, and transesterified oil/polyethylene glycol are effective dispersing agents for use with hydrofluoroalkanes. Effective amounts of the above are effective in suspending medicaments which are useful in inhalation aerosols, and especially meter-dose inhalers.
Type:
Grant
Filed:
March 8, 1994
Date of Patent:
March 26, 1996
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Suresh C. Dixit, David Goldman, John J. Hu, Krish Sethachutkul