Patents Represented by Attorney, Agent or Law Firm Robert A. Silverman
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Patent number: 5676960Abstract: A method of treating a population of social insects includes applying topically to the insect a composition comprising a carrier and an active ingredient. The composition provides a coating that adheres to the insect and is groomable and ingestible by other insects to distribute the active ingredient within the population. In accordance with a preferred embodiment, the composition includes sulfluramid as an active ingredient and an air dryable resin as a carrier. A trap for collection of insects controls temperature within the trap to promote recruitment and also drive the insects to a collection area where they may be treated.Type: GrantFiled: April 3, 1996Date of Patent: October 14, 1997Inventor: Timothy G. Myles
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Patent number: 5670640Abstract: A process for the manufacture of compounds of formula ##STR1##Type: GrantFiled: December 9, 1996Date of Patent: September 23, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Mark Rogers-Evans, Paul Spurr
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Patent number: 5667721Abstract: Liquid crystalline compounds having two dioxane rings, the dipole moments of which are unidirectional. These are compounds of the general formula ##STR1## wherein A and B each independently is cyclic or acyclic hydrophobic residues; andn is 0, 1 or 2.as well as liquid crystalline mixtures which contain such compounds and the use of such compounds and, respectively, mixtures for electro-optical display devices.Type: GrantFiled: February 21, 1996Date of Patent: September 16, 1997Assignee: Rolic AGInventors: Richard Buchecker, Guy Marck, Alois Villiger
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Patent number: 5665718Abstract: The invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. is one of the residues ##STR2## Q is one of the residues ##STR3## R.sup.1 and R.sup.2 each independently are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower hydroxyalkyl, lower alkoxy-lower alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl-lower alkyl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or aryl-lower alkyl or together with the nitrogen atom are a 5- to 8-membered membered heterocycle optionally containing a further hetero atom or a fused benzene ring,R.sup.3 is hydrogen and R.sup.4 is lower alkyl or R.sup.3 and R.sup.4 together are dimethylene or trimethylene andR.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, lower alkoxy or nitro,the compounds of formula I having the (S) configuration with reference to the carbon atom denoted by .gamma. when R.sup.3 and R.sup.Type: GrantFiled: January 16, 1996Date of Patent: September 9, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Thierry Godel, Walter Hunkeler, Heinz Stadler, Ulrich Widmer
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Patent number: 5646173Abstract: The invention relates to tricyclic pyrrole derivatives useful as 5-HT selective agents of the formula ##STR1## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower alkyl, phenyl, cycloalkyl or lower alkoxy and R.sup.2 additionally is lower alkoxycarbonyl, acyloxy or mesyloxy;R.sup.5 to R.sup.7 are, independently, hydrogen or lower alkyl;X is --CH.sub.2 CH(C.sub.6 H.sub.5)--, --CH.dbd.C(C.sub.6 H.sub.5)--, --YCH.sub.2 --, --CH.dbd.CH-- or --(CR.sup.11 R.sup.12).sub.n ;R.sup.11 and R.sup.12 are, independently, hydrogen, phenyl, lower alkyl or halogen;n is 1 to 3 andy is O or S,as well as pharmaceutically acceptable salts of basic compounds of formula I with pharmaceutically acceptable acids.Type: GrantFiled: February 21, 1996Date of Patent: July 8, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Jurgen Wichmann, Ulrich Widmer
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Patent number: 5641485Abstract: Physiologically active caledothricins A-I and their salts, which are useful for the treatment of mycotic diseases. Also strains belonging to the genus Pseudomonas capable of producing the caledothricins upon cultivation.Type: GrantFiled: August 11, 1995Date of Patent: June 24, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Masae Kikuchi, Hisao Shimada, Hitomi Tanaka
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Patent number: 5641886Abstract: The invention relates to a process for the preparation of N-tert.butyl-decahydro-2-[2(R)-hydroxy-4-phenyl-3(S)-phthalimidobutyl]-(4a S,8aS)-isoquinoline-3(S)-carboxamide of the formula ##STR1## as well as novel intermediates. The compound of formula I is a valuable intermediate for pharmacologically active compounds. The compound of formula I can be converted into pharmacologically active compounds which are suitable for the treatment of viral infections, such as those caused by HIV and other retroviruses.Type: GrantFiled: December 20, 1995Date of Patent: June 24, 1997Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 5637720Abstract: The invention relates to a process of making a compound of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 and n are as described herein, and, when R.sub.1 is different from R.sub.2, and/or when R.sub.3 is different from R.sub.4, enantiomers, diastereomers and racemates thereof, and salts thereof with pharmaceutically acceptable bases. The method comprises reacting a compound of the formula ##STR2## wherein R.sub.5 and n are as described herein with a compound of the formula ##STR3## to produce a compound of the formula ##STR4## wherein n is as described herein, and converting a compound of formula IV to a compound of formula I.Type: GrantFiled: May 28, 1996Date of Patent: June 10, 1997Assignee: Hoffmann-La Roche Inc.Inventor: Hubert Maehr
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Patent number: 5633371Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: September 15, 1995Date of Patent: May 27, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
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Patent number: 5614526Abstract: A method of treating or preventing illnesses caused by a disorder of the dopamine system. The method comprises administering to a host in need of such treatment or prevention an effective amount of a pharmaceutical composition comprising a compound of the formula ##STR1## wherein R.sup.1 and R.sup.3 each independently are hydrogen, aryl, carbamoyl, lower-alkyl-carbonyl, lower-alkyl, halogen, lower-alkyl-carbonyl-amino, lower-alkenyl-carbonyl-amino, amino, arylamino, aryloxy, nitro, aryl-acetyl, lower-alkanoyl-lower-alkyl, alkyl-sulphonyl-amino, ureido or furan-2-yl-carbonyl-amino andR.sup.2 is hydrogen, lower-alkyl, trifluoromethyl, halogen, lower-alkoxy, lower-alkyl-carbonyl or lower-alkyl-carbonyl-amino orR.sup.1 and R.sup.2 together are --OCH.sub.2 O--, --O(CH.sub.2).sub.2 O-- or --(CH.sub.2).sub.3 --,R.sup.4 is hydrogen, halogen, hydroxy, lower-alkyl, lower-alkoxy or nitro,R.sup.5 is hydrogen, halogen or lower-alkoxy,R.sup.Type: GrantFiled: April 29, 1996Date of Patent: March 25, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Thierry Godel, Deborah Hartman, Claus Riemer
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Patent number: 5593870Abstract: The present invention is directed to a process for producing frenolicin B. The process comprises fermenting a broth so as to produce frenolicin, said broth having a microorganism capable of producing frenolicin. The frenolicin is then converted in the broth under anaerobic conditions to deoxyfrenolicin. The deoxyfrenolicin is converted to frenolicin B.Type: GrantFiled: September 14, 1994Date of Patent: January 14, 1997Assignee: Hoffmann-La Roche Inc.Inventors: David E. Block, Theron E. Hermann, Jih-Han Hsieh, Nikhil S. Mehta, Vishva R. Rai
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Patent number: 5582767Abstract: The invention relates to liquid crystalline, multiply-substituted fluorinated tolane derivatives, their preparation, liquid crystalline mixtures which comprise such compounds and the use of these compounds and mixtures for electro-optical purposes.Type: GrantFiled: November 8, 1993Date of Patent: December 10, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Richard Buchecker, Martin Schadt
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Patent number: 5578594Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.Type: GrantFiled: December 21, 1994Date of Patent: November 26, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, G erard Schmid
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Patent number: 5578272Abstract: A reagent kit having at least one container holding a reagent, and an analytical apparatus in which the reagent kit can be used. For the purpose of fully automatic processing of the reagent kit in an analytical apparatus, the reagent kit is characterized in that it is substantially a cuboid casing having a bottom, side walls and a removable lid and containers disposed in the casing, the lid having openings through which the contents of the reagent containers are accessible for automatic pipetting operations, each reagent container being closed by a closure, said closure being apt to be perforated by the needle of the pipetting device of an analytical apparatus, said closure being also apt to reclose the perforation after removal of the pipetting needle.Type: GrantFiled: June 24, 1994Date of Patent: November 26, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Bruno Koch, Gottlieb Schacher
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Patent number: 5574055Abstract: The present invention relates to compounds of the formula: ##STR1## wherein R is H or alkyl;Y.sup.1 is --CH.dbd. or --N.dbd.; andY.sup.2 --CH.dbd., --C(OH).dbd., --C(NO.sub.2).dbd., --C(NH.sub.2).dbd., --C(Hal).dbd., --N.dbd.;X is cycloalkenyl; bicyclo[2.2.1]hept-2-yl, optionally substituted by phenyl-2-oxo-5 -methoxymethyl-oxazolidinyl; bicyclo[2.2.1]-hept-5 -en-2-yl; adamantyl; or cycloalkyl or piperidinyl, optionally substituted by amino, alkyl, --CN, oxo hydroxyimino, ethylenedioxyor by --OR.sup.1,R.sup.1 is --CH(C.sub.6 H.sub.5).sub.2, --(CH.sub.2).sub.n C.sub.6 H.sub.5, alkyl, H, --(CH.sub.2).sub.n NHCOCH.sub.3, --(CH.sub.2).sub.n NH.sub.2, --(CH.sub.2).sub.n CN, --(CH.sub.2).sub.n SCH.sub.3 --(CH.sub.2).sub.n SO.sub.2 CH.sub.3, --CO-lower-alkyl, --COC.sub.6 H.sub.5, optionally substituted by oxazolidine;or by .dbd.CR.sup.2 R.sup.3,R.sup.2 is alkylR.sup.3 is H, --CN, alkyl, phenyl or COO-alkyl;or by --(CH.sub.2).sub.n R.sup.4R.sup.4 is --CN, amino, --NHCOCH.sub.3, --COC.sub.6 H.sub.Type: GrantFiled: December 2, 1994Date of Patent: November 12, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Janos Borgulya, Hans Bruderer, Roland Jakob-Roetne, Stephan R over
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Patent number: 5540917Abstract: A pharmaceutical composition comprising at least one water insoluble crude fiber and at least one lipase inhibitor. The lipase inhibitor is present in an amount effective for treating adiposity. The lipase inhibitor is selected from lipstatin in pure form, a biomass comprising a lipase inhibitor, and tetrahydrolipstatin.Type: GrantFiled: May 19, 1995Date of Patent: July 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Dorothea Isler, Walter Rehm, Erich Widmer
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Patent number: 5541186Abstract: A compound of the formula ##STR1## wherein R.sup.1 to R, R.sup.a, R.sup.b X, Y, Z, m and n have the significance given in the description, can be used as medicaments, especially for the treatment and prophylaxix of conditions which are associated with endothelin activities.Type: GrantFiled: June 27, 1994Date of Patent: July 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael L offler, Marcel M uller, Werner Neidhart, Henri Ramuz
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Patent number: 5539074Abstract: The invention is concerned with linear and cyclic polymers or oligomers having a photoreactive ethene group. The polymers are of the formula ##STR1## wherein M.sub.a, M.sub.b, M.sub.c are monomer units for homo- or copolymers;x, y, z are mole fractions of the copolymers, whereby in each case 0<x.ltoreq.1; 0.ltoreq.y.ltoreq.1 and 0.ltoreq.z<1;S.sub.a, S.sub.b are spacer units;Z.sub.a, Z.sub.b are molecule units which can undergo photochemical isomerization/dimerization;n is a magnitude of 4-100 000 andm is 0 or 1,The compounds are used as an orientating layer for liquid crystals.Type: GrantFiled: February 4, 1994Date of Patent: July 23, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Rolf-Peter Herr, Stephen Kelly, Martin Schadt, Klaus Schmitt, Andreas Schuster
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Patent number: 5523310Abstract: The invention relates to a compound of the formula ##STR1## wherein the substituents are as defined herein; its tautomer wherein the hydrogen of the triazole ring occupies position 1 of the triazole ring, and a pharmaceutically acceptable salt of the compound of formula I wherein R.sup.3 is --OH or its tautomer wherein the hydrogen of the triazole ring occupies position 1 of the triazole ring. The compounds of formula I and their salts possess inflammation inhibiting properties and are therefore useful in the treatment of inflammations such as inflammatory joint disease, for example, arthritis. In another aspect, the invention relates to pharmaceutical compositions and methods of use comprising the compounds of formula I.Type: GrantFiled: December 5, 1994Date of Patent: June 4, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Hubert Maehr
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Patent number: D382346Type: GrantFiled: October 13, 1995Date of Patent: August 12, 1997Assignee: Roche Diagnostic Systems, Inc.Inventors: Jurg Buhler, Siegfried Muller