Patents Represented by Attorney, Agent or Law Firm Robert A. Silverman
-
Patent number: 5789607Abstract: A process for preparing 1,25-dihydroxy-16-ene-23-yne cholecalciferol.Type: GrantFiled: April 18, 1997Date of Patent: August 4, 1998Assignee: Hoffmann-La Roche Inc.Inventor: Masami Okabe
-
Patent number: 5763604Abstract: 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: June 4, 1997Date of Patent: June 9, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, Gerard Schmid
-
Patent number: 5753595Abstract: Herbicidal 3-(substituted benzoxazol-7-yl) and 3-(substituted benzothiazol-7-yl)-1 -substituted-6-trifluoromethyl-2,4-(1H,3H)pyrimidinediones, compositions containing them, and methods of using them to control undesired plant growth are disclosed, as are novel intermediates used in the preparation of these compounds. The herbicidal compounds of the present invention are defined by the following generic structure: ##STR1## in which R is selected from a variety of substituents, including halogen, alkyl, alkenyl, alkynyl, phenyl, phenylalkyl, alkylphenylalkyl, haloalkyl, hydroxy, alkoxy, hydroxyalkyl, halophenyl, halophenylalkyl, alkoxyphenyl, sulfhydryl, alkylthio, piperidinyl, alkylamino, alkoxyalkyl, phenoxy, amino, alkylsulfonylamino, phenylsulfonylamino, and carboxy; R.sup.1 is alkyl or amino; R.sup.Type: GrantFiled: July 31, 1996Date of Patent: May 19, 1998Assignee: FMC CorporationInventors: Scott D. Crawford, Lester L. Maravetz, George Theodoridis
-
Patent number: 5753638Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.Type: GrantFiled: June 2, 1995Date of Patent: May 19, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Enrico Giuseppe Baggiolini, deceased, Shian-Jan Shiuey, Milan Radoje Uskokovic
-
Patent number: 5750517Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.Type: GrantFiled: March 1, 1996Date of Patent: May 12, 1998Assignee: Hoffman-La Roche Inc.Inventors: Enrico Giuseppe Baggiolini, deceased, Shian-Jan Shiuey, Milan Radoje Uskokovic
-
Patent number: 5750690Abstract: A process for the asymmetric hydrogenation of a compound of the formula ##STR1## wherein each R, independently, is alkyl, arylmethyl, aryl, alkoxy, arylmethoxy or aryloxy or both R's, taken together, are methylene, ethylene or 1,2-phenylene and n is 1,2 or 3,or of a salt thereof to a compound of the formula ##STR2## in the form of an (S) or (R) enantiomer, wherein R and n have the significances given above, using an optically active ruthenium-diphosphine complex as catalyst, is described. The preparation of the compounds of formula II, as well as the compounds of formula II, which form a further object of the invention, are also described.Type: GrantFiled: July 26, 1996Date of Patent: May 12, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Emil Albin Broger, Yvo Crameri, Marquard Imfeld, Fran.cedilla.ois Montavon, Erich Widmer
-
Patent number: 5747479Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin, produced by photodamage, which disorders include wrinkling, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein R.sub.1 is hydrogen, hydroxy or fluorine, R.sub.2 is hydrogen or halogen and A is --C.vertline.C--, --C.dbd.C-- or --CH.sub.2 --CH.sub.2 --, provided that when A is --CH.sub.2 --CH.sub.2 --, R.sub.2 is hydrogen.Type: GrantFiled: December 11, 1996Date of Patent: May 5, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Graeme Findlay Bryce, Milan Radoje Uskokovic
-
Patent number: 5726191Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-6 -alkyl;R.sup.2 is C.sub.1-6 -alkyl or adamantyl;R.sup.3 is C.sub.1-6 -alkyl or hydroxy; orR.sup.2 and R.sup.3 taken together are --(CR.sup.6 R.sup.7).sub.n --;R.sup.4 is C.sub.2-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 -alkynyl, --OCH.sub.2 R.sup.5 or C.sub.2-8 -alkanoyl; and hydrogen when R.sup.3 is hydroxy;R.sup.5 is C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl;R.sup.6 and R.sup.7 are hydrogen or C.sub.1-6 -alkyl;Y is oxygen or sulphur; andn is 3, 4 or 5,and pharmaceutically usable salts of carboxylic acids of formula I act as selective ligands of retinoic acid .gamma.-receptors and are useful for the treatment of epithelial lesions.Type: GrantFiled: October 23, 1996Date of Patent: March 10, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
-
Patent number: 5721245Abstract: A compound of the formula ##STR1## wherein R is hydrogen or hydroxy, R.sup.1 and R.sup.2 taken together are a group of the formula --(CH.sub.2).sub.m -- and R.sup.7 is hydrogen or R.sup.1 and R.sup.7 taken together are a group of the formula --(CH.sub.2).sub.n -- and R.sup.2 is hydrogen; R.sup.3 is an aryl or aromatic heterocyclic group; R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halogen, alkyl, hydroxy, alkoxy, haloalkyl, nitro, amino, acylamino, alkylthio, alkylsulfinyl or alkylsulfonyl; R.sup.8 is a group of the formula --(CH.sub.2).sub.p --R.sup.9 or --(CH.sub.2).sub.q --R.sup.10 ; R.sup.9 is hydrogen, alkylcarbonyl, aminoalkylcarbonyl, cyano, amidino, alkoxycarbonyl, aryloxycarbonyl, alkylsulfonyl, aminocarbonyl or aminothiocarbonyl; R.sup.Type: GrantFiled: January 17, 1995Date of Patent: February 24, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Peter David Davis, Christopher Huw Hill, Geoffrey Lawton
-
Patent number: 5721230Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is lower alkyl, lower cycloalkyl, aryl or lower aralkyl; R.sup.2 is hydrogen, aryl or lower alkyl optionally substituted by hydroxy, acyloxy, amino, mono(lower alkyl)amino, di(lower alkyl)amino, carboxy, lower alkoxycarbonyl or aminocarbonyl; andm and n are, independently, the numerals 1 or 2, andpharmaceutically acceptable salts of acidic compounds of formula I with bases and of basic compounds of formula I with acids are useful in the control or prevention of illnesses, particularly, in the control or prevention of inflammatory, immunological, oncological, bronchopulmonary, dermatological and cardiovascular disorders, in the treatment of asthma, AIDS or diabetic complications or for the stimulation of hair growth.Type: GrantFiled: April 24, 1996Date of Patent: February 24, 1998Assignee: Hoffmann-La Roche Inc.Inventors: William Harris, Christopher Huw Hill, Geoffrey Lawton
-
Patent number: 5705703Abstract: 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: January 21, 1997Date of Patent: January 6, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
-
Patent number: 5698698Abstract: 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, specifically described in Example 1 of European Patent Publication 0,432,694, 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: March 11, 1997Date of Patent: December 16, 1997Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
-
Patent number: 5698565Abstract: A method of treating or preventing illnesses caused by a disorder of the dopamine system. The method comprises administering to a host requiring such treatment or prevention an effective amount of a pharmaceutical composition comprising a compound of the formula ##STR1## wherein R.sup.1 is hydrogen, lower-alkyl, halogen, lower-alkoxy or nitro;R.sub.2 is hydrogen, lower alkyl or trifluoromethyl; andR.sup.3 is hydrogen, lower alkyl, trifluoromethyl, benzyl, hydroxy-lower-alkyl, lower alkoxy, lower-alkyl-carbonyl-amino, carbonyl-lower-alkyl, benzyl, di-lower-alkyl-amino-carbonyl, carbonylamino or amino-carbonyl-amino; orR.sup.2 and R.sup.3 together optionally are a fused benzene ring andR.sup.4 is hydrogen or halogen,or a pharmaceutically acceptable salt of a compound of formula I, and a pharmaceutically inert carrier material.Type: GrantFiled: April 29, 1996Date of Patent: December 16, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Thierry Godel, Deborah Hartman, Claus Riemer
-
Patent number: 5695776Abstract: The invention provides a method and apparatus for controlling termites. The invention provides a more attractive and durable termite bait by providing a thin flat block of wood with grooves and impregnating the surface of the wood with a slow acting toxicant.Type: GrantFiled: March 12, 1996Date of Patent: December 9, 1997Assignee: FMC CorporationInventors: James Bruce Ballard, Sherman H. Trimm
-
Patent number: 5693331Abstract: The invention provides a method and apparatus dispensing a liquid bait in a refillable manner. The invention provides a transparent bait station in which is mounted to a structure. A liquid bait is injected into the bait station to initially fill and then refill the bait station. The bait is a slow acting toxicant and attractant. The bait station is formed to allow access by bugs, but not by larger animals. The bait station is also able to protect the bait from wind and rain.Type: GrantFiled: March 25, 1996Date of Patent: December 2, 1997Assignee: FMC CorporationInventor: James Bruce Ballard
-
Patent number: 5693795Abstract: A process for the manufacture of 4H-imidazo?1,5-a!?1,4!benzodiazepine derivatives of formula I ##STR1## wherein R.sup.1 is phenyl or mono- or disubstituted phenyl;R.sup.2 is hydrogen, halogen, nitro, cyano, trifluoromethyl or lower alkyl;R.sup.3 is hydrogen or lower alkyl; andR.sup.4 is hydrogen or lower alkyland of pharmaceutically usable salts of these compounds by decarboxylating a 4H-imidazo?1,5-a!?1,4!benzodiazepinecarboxylic acid of formula II ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the above significances, at elevated temperature and under elevated pressure in the presence of an organic solvent. The compounds of formula I and their pharmaceutically usable acid addition salts are known muscle relaxants, sedatives and anticonvulsants.Type: GrantFiled: October 2, 1996Date of Patent: December 2, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Karl-Heinz Bender, Manfred Breuninger, Manfred Froom, Siegfried Schmitt, Kurt Steiner
-
Patent number: 5688798Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each individually are lower-alkyl or amino,A is ##STR2## B is hydrogen in A.sup.4, A.sup.5 and A.sup.6 ; ##STR3## in A.sup.1 -A.sup.6 ; lower-alkoxy in A.sup.4 -A.sup.6 ;and lower-alkyl, styryl, phenylethynyl or benzoyloxy-lower-alkyl in A.sup.1 and A.sup.2 ;n is 0, 1 or 2;m, p are, independently 0, 1 andR.sup.3, R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halogen, lower-alkyl, trifluoromethyl, lower-alkoxy or nitro,and pharmaceutically acceptable acid addition salts thereof. These compounds are useful in the control or prevention of illnesses which are caused by disorders of the dopamine system, in particular psychotic illnesses such as schizophrenia.Type: GrantFiled: September 11, 1996Date of Patent: November 18, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Thierry Godel, Claus Riemer
-
Patent number: 5688803Abstract: Compounds of general formula (Ia), (Ib) and (II), wherein R.sup.1 and R.sup.2 each independently signify hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R.sup.3 R.sup.4 NS(O).sub.2 -- and R.sup.3 and R.sup.4 signify lower alkyl, and R.sup.2 can additionally signify morpholino or thiomorpholino, a 5- or 6-membered heterocycle with 1-3N atoms optionally substituted by lower alkyl, hydroxy, amino or the group --CH.sub.2 NHCH.sub.3, a bicyclic heterocycle with 1-3N atoms or a group --NR.sup.5 R.sup.6 or --OR.sup.5 in which R.sup.5 and R.sup.6 can be the same or different and signify hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl, and X in formula (II) signifies --CH.dbd.CH--, --CH.dbd.N--, --NH--, --CO-- or --O--, as well as pharmaceutically usable salts of compounds of general formula (Ia), (Ib) and (II).Type: GrantFiled: November 15, 1996Date of Patent: November 18, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buttelmann, Thierry Godel, Laurence Gross, Marie-Paule Heitz Neidhart, Claus Riemer, Rene Wyler
-
Patent number: 5681504Abstract: A chiral dopant of the formula ##STR1## wherein ring A is 1,4-phenylene which is optionally substituted with one or more fluorine atoms, chlorine atoms, bromine atoms, cyano groups, or methyl groups, and in which one or two CH groups can be replaced by nitrogen, or is trans-1,4-cyclohexylene;Z is a single covalent bond, --CH.sub.2 CH.sub.2 --, --CH.sub.2 O-- or --OCH.sub.2 --; X.sup.1,X.sup.2,X.sup.3,X.sup.4 each independently are hydrogen or fluorine;R.sup.1 is hydrogen, is alkyl with 1 to 12 carbon atoms which is optionally substituted with one or more fluorine or chlorine atoms and in which one or two non-adjacent CH.sub.2 groups can be replaced by --0--, is alkenyl with 2 to 12 carbon atoms, which is optionally substituted with one or more fluorine or chlorine atoms and in which one or two non-adjacent CH.sub.2 groups can be replaced by --O--, is a group of the formula ##STR2## and when R.sup.1 is bonded to an aromatic ring, can also be fluorine, chlorine, cyano, CF.sub.3, OCHF.sub.2 or --OCF.sub.3 ;R.Type: GrantFiled: December 5, 1995Date of Patent: October 28, 1997Assignee: Rolic AGInventors: Richard Buchecker, Guy Marck, Martin Schadt
-
Patent number: 5677448Abstract: 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: August 13, 1996Date of Patent: October 14, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, Gerard Schmid