Abstract: There is described a process for the preparation of a compound of formula I ##STR1## in which process: a) a compound of formula II ##STR2## is reacted with an organolithium compound of formula IIILi--R.sub.7 (III)b) the resulting lithium complex is reacted with a compound of formula IVY.sub.1 --CO--CO--Y.sub.1 IVto form a compound of formula V ##STR3## c) that compound is, in either order, c1) oximated with O-methylhydroxylamine; or oximated with hydroxylamine and then methylated or fluoromethylated or difluoromethylated;c2) reacted with a chloroformic acid ester.X, m, Y, R.sub.1 to R.sub.3 and R.sub.7 are as defined in the description.
Type:
Grant
Filed:
October 19, 1998
Date of Patent:
September 26, 2000
Assignee:
Novartis Finance Corporation
Inventors:
Jean-Marie Assercq, Hans-Dieter Schneider, Albert Pfiffner, Werner Pfaff
Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.
Type:
Grant
Filed:
July 1, 1998
Date of Patent:
August 29, 2000
Assignee:
Novartis Finance Corporation
Inventors:
Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
Abstract: A homogeneous blended additive useful as a processing stabilizer for polymers which is a blend of Component (a), a defined phosphite or phosphonite; and Component (b) which is micronized zinc oxide. Component (b) is preferably in an amount of 5 to 10% based on the weight of component (a). This additive composition improves the resistance of phosphites and phosphonites against hydrolysis in the presence of moisture, by providing Component (b) as a hydrolysis stabilizer for Component (a).
Type:
Grant
Filed:
October 3, 1997
Date of Patent:
August 15, 2000
Assignee:
Clariant Finance (BVI) Limited
Inventors:
Peter Staniek, Klaus Stoll, Rainer Wolf
Abstract: The invention provides a pharmaceutical composition comprising a somatostatin analogue, and its use in the treatment of breast cancer. The pharmaceutical composition preferably contains lactic acid in addition to the somatostatin analogue and is better tolerated when administered by injection.
Abstract: The invention relates to low-viscosity, aqueous coolant brines based on inhibited alkali metal acetates and/or formates having improved corrosion protection, wherein the coolant brines contain 0.2 to 5% by weight of alkali metal sulfites or pyrosulfites, in particular 1 to 2.5% by weight of these sulfites. The brines according to the invention furthermore contain 0.3 to 5% by weight of basic substances from the alkali metal carbonates, hydroxides, borates and phosphates group and also 0 to 0.3% by weight of alkali metal silicates and 0.02 to 0.2% by weight of stabilizers from the triazoles, benzimidazoles and/or mercaptothiazoles group. The novel coolant brines result in very low corrosion rates, in particular with steel and cast iron.
Abstract: The present invention relates to a folding process for the preparation of biologically active, dimeric TGF-.beta. (Tranforming Growth Factor type .beta.)-like protein.
Abstract: A method for treating a human having elevated tumor necrosis factor levels by administrating an effective amount of one of the amino acids glycine, alanine, or serine.
Abstract: The invention relates to a process for preparing alkali metal salts and/or alkaline earth metal salts of alkylphosphonous acids and dialkylphosphinic acids from elemental yellow phosphorus and alkyl halides, which comprises carrying out the reaction in the presence of aqueous alkali metal hydroxide or alkaline earth metal hydroxide or mixtures thereof. The invention likewise relates to the use of the compounds prepared by the process according to the invention for preparing flame retardants, extraction media and plant protection agents.
Abstract: The compounds of the s-triazine series of formula I ##STR1## wherein the symbols R.sub.1, R.sub.2, R.sub.3, X and n possess the significances given in claim 1, are eminently suitable, when applied to textile material, as UV-absorbers, as resist agents for anionic dyes, and as stain blockers.
Abstract: Ascospores of wood-penetrating, pitch-grading fungi of the class of Ascomycotina and Deuteromycotina, eg. Ophiostromas, may be screened to provide fungi combining the properties of good growth on non-sterile wood substrates and minimized or even enhanced brightness effects for use in pitch reduction of wood substrates, eg. logs and wood chips. A new and improved method of isolating such ascospores involving effective suspension in an oil consumable by the fungus, eg. a vegetable oil, and then treatment of the oil with a dispersing agent is also disclosed.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 7, 1999
Assignee:
Clariant Finance (BVI) Limited
Inventors:
Roberta L. Farrell, Yitzhak Hadar, Philip A. Wendler, Wendy Zimmerman
Abstract: The present invention relates to novel inhibitors of human tryptase, to their isolation from leeches, to nucleotide sequences encoding the novel inhibtor molecules or fragments thereof, to vectors containing the coding sequence thereof, to host cells transformed with such vectors, to the recombinant production of the inibitors, to pharmaceutical compositions containing the novel inhibitor molecules, and to their use in diagnosis and therapy.
Type:
Grant
Filed:
January 25, 1996
Date of Patent:
October 26, 1999
Assignees:
Novartis Corporation, UCP Gen-Pharma AG
Abstract: Dyeing of cellulosic substrates with reactive dyes in the presence of at least 20 g/l of sodium chloride, employing auxiliaries (E) of levelling activity, which are methylene-bridge-containing and sulpho-group-containing aromatic compounds, obtainable by condensation of defined sulphonation products with formaldehyde resp. formaldehyde-yielding compounds and optionally salt formation; (E)-contaning compositions that further contain at least one hydrotrope (H) and/or at least one sequestering agent (Q); and novel condensation products.
Abstract: The invention concerns recombinant antibodies directed to the extracellular domain of the human growth factor receptor c-erbB-2 comprising a light chain variable domain and a heavy chain variable domain of a monoclonal antibody, monoclonal antibodies directed to c-erbB-2 themselves, a method of manufacture of said recombinant antibodies and said monoclonal antibodies, hybridoma cells secreting said monoclonal antibodies, a method of manufacture of said hybridoma cells, DNA coding for the heavy chain variable domain, for the light chain variable domain and for the recombinant antibody, a method of manufacture of said DNA, hybrid vectors suitable for expression of said DNA, host cells transformed with said DNA, and the use of said recombinant antibodies and said monoclonal antibodies in the diagnosis and treatment of tumors.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
August 17, 1999
Assignee:
Novartis Corp.
Inventors:
Winfried Stephan Wels, Nancy E. Hynes, Ina-Maria Harwerth, Bernd Groner, Norman Hardman, Markus Zwickl
Abstract: A plant-microbicidal composition having synergistic action, comprising at least two active ingredient components, wherein component I is a compound selected from the group(IA) 1-?3-(2-chlorophenyl)-2-(4-fluorophenyl)oxiran-2-ylmethyl!-1H-1,2,4-triazo le ("epoxiconazol");(IB) 4-(4-chlorophenyl)-2-phenyl-2-(1,2,4-triazol-1-ylmethyl)-butyronitrile ("fenbuconazol");(IC) 5-(4-chlorobenzyl)-2,2-dimethyl-1-(1H-1,2,4-triazol-1-ylmethyl)-cyclopenta nol ("metconazol");(ID) 2-(2,4-dichlorophenyl)-3-(1H-1,2,4-triazol-1-yl)propyl-1,1,2,2-tetrafluoro ethyl ether ("tetraconazol");(IE) .alpha.-?2-(4-chlorophenyl)ethyl!-.alpha.
Abstract: This invention provides a polyester of a polyol, said polyol containing at least 3 hydroxyl groups and having a molecular weight of up to 20,000 at least 1 hydroxyl group in said polyol being in the form of an ester, with a poly- or co-poly-lactic acid residue, each having a molecular weight of at least 5,000. These are useful for parenteral depot formulations.
Abstract: This invention provides a polyester of a polyol, said polyol containing at least 3 hydroxyl groups and having a molecular weight of up to 20,000 at least 1 hydroxyl group in said polyol being in the form of an ester, with a poly- or co-poly-lactic acid residue, each having a molecular weight of at least from 5,000. These are useful for parenteral depot formulations.
Abstract: The invention relates to a process for the production of biologically active, dimeric TGF-.beta., to novel TGF-.beta.s and pharmaceutical compositions comprising it. TGF-.beta. produced by this process can be used in various therapeutic modalities.
Type:
Grant
Filed:
January 24, 1997
Date of Patent:
July 13, 1999
Assignee:
Novartis Corp.
Inventors:
Nico Cerletti, Gary Kent McMaster, David Cox, Albert Schmitz, Bernd Meyhack
Abstract: The invention relates to a process for the preparation of substituted 3-amninobenzonitriles, which comprises reacting the appropriate substituted 3-aminochlorobenzene with a cyano-donating reagent, and to the compounds thereby produced. The compounds are intermediates, which after further reaction, produce 1,2,3-benzothiadiazole-derivatives having plant immunizing properties.
Type:
Grant
Filed:
August 1, 1997
Date of Patent:
March 16, 1999
Assignee:
Novartis Finance Corporation
Inventors:
Richard Breitschuh, Benoit Pugin, Adriano Indolese, Verena Gisin
Abstract: The invention discloses microparticles comprising a polypeptide, preferably somatostatin or an analog or derivative thereof, more preferably octreotide, in a polymeric matrix, preferably poly(lactide-co-glycolide) glucose. The invention also discloses sustained release formulations containing said microparticles and the use of said formulations in treating acromegaly and breast cancer.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
March 2, 1999
Assignee:
Novartis AG
Inventors:
David Bodmer, Jones W. Fong, Thomas Kissel, Hawkins V. Maulding, Oskar Nagele, Jane E. Pearson
Abstract: Immunoglobulin preparations, particularly liquid preparations of immunogllin G for intravenous infusion, are stabilized against dimer formation by the addition of one or more amphiphilic stabilizers. Preferred amphiphilic stabilizers are nicotinic acid derivatives, particularly nicotinamide, and naturally-occurring .alpha.-amino acids having a lipophilic side chain, for example phenylalanine, proline, leucine and isoleucine.
Type:
Grant
Filed:
March 7, 1997
Date of Patent:
February 16, 1999
Assignee:
Red Cross Foundation Central Laboratory Blood Transfusion Service SRC
Inventors:
Rene Bruegger, Katharina Gennari, Gerhard Hodler, Bernard Wuest