Patents Assigned to Novartis Corporation
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Patent number: 6096749Abstract: The invention relates to the use of the compounds mentioned below in the therapeutic treatment of tumor diseases and other proliferative diseases, such as psoriasis, and to novel compounds of that type. The compounds are compounds of formula I ##STR1## wherein n is from 0 to 5 and, when n is not 0,R is one or more substituents selected from halogen, alkyl, trifluoromethyl and alkoxy; andR.sub.1 and R.sub.2 are each independently of the other alkyl, or phenyl that is unsubstituted or substituted by halogen, trifluoromethyl, alkyl or by alkoxy, it also being possible for one of the two radicals R.sub.1 and R.sub.2 to be hydrogen, or R.sub.1 and R.sub.2 together form an alkylene chain having from 2 to 5 carbon atoms that is unsubstituted or substituted by alkyl;or salts thereof. Compounds of formula I inhibit protein kinases, for example the tyrosine protein kinase of the receptor for the epidermal growth factor, EGF.Type: GrantFiled: April 1, 1998Date of Patent: August 1, 2000Assignee: Novartis CorporationInventors: Peter Traxler, Pascal Furet, Wolfgang K.-D. Brill
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Patent number: 6083881Abstract: Compounds of formula (I) ##STR1## in which the substituents W, R.sub.100, R.sub.101 and R.sub.102 are as defined 1; and the pyrazole N-oxides, salts, complexes and stereoisomer of the compounds of (I) have good pre- and post-emergence selective herbicidal properties. The preparation compounds and their use as herbicidal active compounds are described.Type: GrantFiled: January 6, 1997Date of Patent: July 4, 2000Assignee: Novartis CorporationInventors: Kurt Nebel, Hans-Georg Brunner, Georg Pissiotas
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Patent number: 6072035Abstract: The invention relates to reshaped human monoclonal antibodies directed against isotypic determinants of immunoglobulin E (IgE), direct equivalents and derivatives of said antibodies. The molecules of the invention are useful for diagnostics, prophylaxis and treatment of allergy.Type: GrantFiled: June 7, 1995Date of Patent: June 6, 2000Assignees: Novartis Corporation, Tanox Biosystems, Inc.Inventors: Norman Hardman, Frank Kolbinger, Jose Saldanha
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Patent number: 6068853Abstract: A delivery mechanism and device for the passive periodic release of a drug or an active ingredient which avoids the need for external power sources and/or electronic controllers. By taking advantage of oscillating chemical systems, one can change the state, i.e. the pH, of a solution, a drug, enhancer or solubilizer resulting in oscillating the ability of an active ingredient to be delivered transdermally. The pH of a solution can be oscillated over a range of pH values from 2 to 10 by the reduction and oxidation (redox) reactions of salts, such as permanganates, iodates, sulfates, chlorates, or bromates. Upon activation, the delivery system conditions begin to oscillate and with it, the delivery of the active agent oscillates.Type: GrantFiled: October 13, 1995Date of Patent: May 30, 2000Assignee: Novartis CorporationInventors: Steven Andrew Giannos, Steven Minh Dinh, Bret Berner
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Patent number: 6066447Abstract: Oligonucleotides of the formula: 5'(U).sub.n -3' in which U is an identical or different radical of a natural or a synthetic nucleoside and n is a number from 2 to 200 comprising at least one structural unit of two consecutive nucleosides wherein one of the nucleotides is substituted in the 2'-position or wherein the nucleotides are substituted differently in their 2'-position and wherein the backbone is modified.Type: GrantFiled: November 12, 1996Date of Patent: May 23, 2000Assignee: Novartis CorporationInventors: Alain De Mesmaeker, Adrian Waldner, Jacques Lebreton, Marc-Olivier Bevierre, Catherine Lesueur
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Patent number: 6066718Abstract: The invention relates to reshaped human monoclonal antibodies directed against isotypic determinants of immunoglobulin E (IgE), direct equivalents and derivatives of said antibodies. The molecules of the invention are useful for diagnostics, prophylaxis and treatment of allergy.Type: GrantFiled: September 27, 1993Date of Patent: May 23, 2000Assignees: Novartis Corporation, Tanox Biosystems, Inc.Inventors: Norman Hardman, Frank Kolbinger, Jose Saldanha
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Patent number: 6066596Abstract: A herbicidal synergistic composition, comprising, besides customary inert formulation auxiliaries, a compound of formula I ##STR1## and a synergistically active amount of at least one active ingredient selected from among the compounds of formula II ##STR2## and of formula III ##STR3## and of formula V ##STR4##Type: GrantFiled: October 11, 1996Date of Patent: May 23, 2000Assignee: Novartis CorporationInventors: Jean Louis Allard, Manfred Hudetz
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Patent number: 6057306Abstract: The invention relates to a method of treating the navicular disease in horses, which comprises treating the navicular disease in horses with an effective amount of at least one compound of formula (I), ##STR1## wherein R.sub.1 is hydrogen, hydroxy, amino or halogen, and R.sub.2 is hydrogen, halogen or a radical which is bound through C, N, S or O, or of a C.sub.1 -C.sub.4 tetraalkyl ester thereof, each in the free form or in the form of the salt and/or in the hydrate form; to a compound of formula (I) for use in a method of treating the navicular disease, to a composition for use in a method of treating the navicular disease, which comprises one or more than one compound of formula (I), as well as to the use of a compound of formula (I) for the preparation of a veterinary composition for treating the navicular disease.Type: GrantFiled: May 15, 1998Date of Patent: May 2, 2000Assignee: Novartis CorporationInventors: Alan Martin Wilson, Allen Edward Goodship, Jonathan Green
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Patent number: 6057430Abstract: The present invention relates to a folding process for the preparation of biologically active, dimeric TGF-.beta. (Tranforming Growth Factor type .beta.)-like protein.Type: GrantFiled: July 28, 1998Date of Patent: May 2, 2000Assignee: Novartis CorporationInventor: Nico Cerletti
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Patent number: 6054454Abstract: The present invention relates to the use of compounds of formula ##STR1## wherein A is an unsubstituted or mono- to tetrasubstituted, aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, where one to two of the substituents of A can be selected from the group consisting of halo-C.sub.1 -C.sub.3 alkyl, cyclopropyl, halocyclopropyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, halo-C.sub.2 -C.sub.3 alkenyl, halo-C.sub.2 -C.sub.3 alkynyl, halo-C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, halo-C.sub.1 -C.sub.3 alkylthio, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro, and one to four of the substituents of A can be selected from the group consisting of C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R is hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl; and X is N--NO.sub.Type: GrantFiled: May 18, 1998Date of Patent: April 25, 2000Assignee: Novartis CorporationInventors: Hariolf Schmid, Ernst Hess
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Patent number: 6047495Abstract: Spraying tubes (20 . . . ) through each of which a plurality of spraying holes are perforated along the longitudinal axis of each tube are placed in prescribed positions upper than feces boards (10 . . . ) of henhouses; and the spraying tubes (20 . . . ) are connected to agent-supplying means for supplying an agent such as a tank, a pump, etc. and airsupplying means for supplying compressed air such as a compressor, etc. The spraying holes make an angle not smaller than 5 degrees and not greater than 90 degrees as measured downward from the horizontal plane at the time of spraying an agent, in order to make it possible to spray the agent to feces boards (10 . . . ) and feces floor (12). The eggs of pests such as housefly and the like laid on the feces adhering to the feces boards and feces floor can efficiently and certainly be controlled.Type: GrantFiled: December 11, 1996Date of Patent: April 11, 2000Assignee: Novartis CorporationInventors: Syunji Matsumura, Isao Takada, Toshiaki Mima, Kazuo Fukui
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Patent number: 6048824Abstract: Compounds of formula (I), wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group ##STR2## R.sub.1 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.3 is hydrogen, an unsubstituted or substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group, or C(.dbd.O)--R.sub.5, R.sub.5 is C.sub.1 -C.sub.4 alkyl C.sub.1 -C.sub.4 alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R.sub.6).sub.2, each R.sub.6, independently of the other, is hydrogen, C.sub.1 -C.sub.4 alkyl or unsubstituted or substituted phenyl, X is CH--NO.sub.2, N--CN or N--NO.sub.2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: November 22, 1995Date of Patent: April 11, 2000Assignee: Novartis CorporationInventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
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Patent number: 6022871Abstract: Compounds of the formula ##STR1## in which A is an unsubstituted or mono- to tetrasubstituted, aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, where one to two of the substituents of A can be selected from the group consisting of halo-C.sub.1 -C.sub.3 alkyl, cyclopropyl, halocyclopropyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, halo-C.sub.2 -C.sub.3 alkenyl, halo-C.sub.2 -C.sub.3 alkynyl, halo-C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, halo-C.sub.1 -C.sub.3 alkylthio, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro, and one to four of the substituents of A can be selected from the group consisting of C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen;R is hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl; andX is N--NO.sub.Type: GrantFiled: February 18, 1999Date of Patent: February 8, 2000Assignee: Novartis CorporationInventors: Peter Maienfisch, Laurenz Gsell
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Patent number: 6002013Abstract: Compounds of the formula I ##STR1## and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III ##STR2## In the compounds of the formulae I and III: X is halogen,n is 0, 1, 2 or 3;Z is CN, CO--A or CS--A,A is hydrogen, halogen, OR.sub.1, SR.sub.2 and N(R.sub.3)R.sub.4 ;R.sub.1 to R.sub.4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R.sub.3 and R.sub.Type: GrantFiled: September 4, 1998Date of Patent: December 14, 1999Assignee: Novartis CorporationInventors: Walter Kunz, Beat Jau
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Patent number: 5985921Abstract: Compounds of the formula ##STR1## in which n, q, A, X, G, Y, Z, R, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.9 are as defined in claim 1, and, where appropriate, E/Z isomers, E/Z isomer mixtures and/or tautomers thereof, in each case in the free form or in an agrochemically suitable salt form, can be used as agrochemical active compounds and can be prepared in a manner known per se.Type: GrantFiled: December 6, 1996Date of Patent: November 16, 1999Assignee: Novartis CorporationInventors: Saleem Farooq, Stephen Trah, Hugo Ziegler, Rene Zurfluh, Alfons Pascual, Henry Szczepanski, Roger Graham Hall
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Patent number: 5981582Abstract: When used in admixture with mancozeb, chlorothalonil, a copper salt, folpet, fluazinam or cymoxanil (it being possible for the latter to be used also together with one of the other five components), metalaxyl having a high R-enantiomer content of more than 70% by weight, or pure R-metalaxyl, exhibits a markedly increased fungicidal action against plant diseases as compared with a similar mixture in which metalaxyl is used in the form of the racemate.Type: GrantFiled: September 9, 1998Date of Patent: November 9, 1999Assignee: Novartis CorporationInventors: Cosima Nuninger, John Edward Nicholas Goggin, Dino Sozzi
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Patent number: 5977332Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently of the other hydrogen or a protecting group, orR.sub.1 has those meanings andR.sub.2 is a radical forming a phosphorus-containing nucleotide bridge group;B is a purine or pyrimidine radical or an analogue thereof; andR.sub.3 is OH, or F, and oligonucleotides that comprise those nucleosides are described.Type: GrantFiled: February 20, 1998Date of Patent: November 2, 1999Assignee: Novartis CorporationInventor: Pierre Martin
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Patent number: 5972698Abstract: 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: GrantFiled: January 25, 1996Date of Patent: October 26, 1999Assignees: Novartis Corporation, UCP Gen-Pharma AGInventors: Hans Fritz, Christian Sommerhoff
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Patent number: 5969116Abstract: Compounds of the formula ##STR1## are described wherein R.sub.1 and R.sub.2 are each independently of the other hydrogen or a protecting group, orR.sub.1 has those definitions andR.sub.2 is a radical forming a phosphorus-containing nucleotide bridge group;B is a purine or pyrimidine radical or an analogue thereof; andR.sub.3 is a radical of formula Ia, Ib or Ic ##STR2## wherein R.sub.4 is hydrogen, C.sub.1 -C.sub.21 alkyl, C.sub.2 -C.sub.21 alkenyl, C.sub.2 -C.sub.21 alkynyl or --C(.dbd.O)-alkyl;R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, --CH.sub.2 --O--R.sub.6 or a radical of formula Ib;R.sub.6 is hydrogen, C.sub.1 -C.sub.22 alkyl, C.sub.3 -C.sub.21 alkenyl, or partially or completely fluorine-substituted C.sub.1 -C.sub.10 alkyl or --[(CH.sub.2).sub.2 --O].sub.m --R.sub.7 ;R.sub.7 is hydrogen or C.sub.1 -C.sub.21 alkyl;Z is --(CH.sub.2).sub.p -- or --(CH.sub.2 --CH.sub.2 --O).sub.q --CH.sub.2 CH.sub.2 --, it being possible for Z in the case of --CH.sub.Type: GrantFiled: June 2, 1995Date of Patent: October 19, 1999Assignee: Novartis CorporationInventor: Pierre Martin
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Patent number: 5965592Abstract: Compounds of the formula ##STR1## and their salts, in which R.sub.1, is a C.sub.1 -C.sub.7 aliphatic hydrocarbon radical; X.sub.1 is --CO; X.sub.2 is a divalent aliphatic hydrocarbon radical which comprises an ethyl group and an alkylene of 2 to 6 carbon atoms; R.sub.2 is hydroxy, carboxy or alkoxycarbonyl in which alkoxy is from 1 to 7 carbon atoms; X.sub.3 is a divalent aliphatic hydrocarbon; R.sub.3 is carboxyl or 5-tetrazolyl; and the rings A and B independently of one another are otherwise unsubstituted; can be prepared in a known manner and may be used as active ingredients for medicaments.Type: GrantFiled: July 29, 1998Date of Patent: October 12, 1999Assignee: Novartis CorporationInventors: Peter Buhlmayer, Franz Ostermayer, Tibur Schmidlin