Patents Represented by Attorney Lewis J. Kreisler
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Patent number: 6150373Abstract: Amino-substituted dihydropyrimido[4,5-d]pyrimidinones of the formula in which R.sup.1 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl or lower cycloalkyl-lower alkyl, R.sup.2 represents lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl or lower cycloalkyl-lower alkyl, and R.sup.3 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl, lower cycloalkenyl or lower cycloalkyl-lower alkyl, and pharmaceutically acceptable salts thereof are protein kinase inhibitors. They can be used in the treatment or prophylaxis of inflammatory, immunological, oncological, bronchopulmonary, dermatological and cardiovascular disorders, in the treatment of asthma, central nervous system disorders or diabetic complications or for the prevention of graft rejection following transplant surgery.Type: GrantFiled: October 21, 1999Date of Patent: November 21, 2000Assignee: Hoffmann-La Roche Inc.Inventors: William Harris, Christopher Huw Hill, Ian Edward David Smith
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Patent number: 6069245Abstract: A novel process for the manufacture of compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.Type: GrantFiled: November 19, 1998Date of Patent: May 30, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Peter Karl Matzinger, Michelangelo Scalone, Ulrich Zutter
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Patent number: 6066662Abstract: The invention provides hydroxylamine derivatives of formula (I) wherein A, R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, which are matrix metalloproteinase inhibitors and which also prevent TNF release. They are therefore useful for the control or prevention of degenerative joints diseases such as rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis. They can be manufactured according to generally known methods.Type: GrantFiled: November 20, 1996Date of Patent: May 23, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
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Patent number: 6057426Abstract: The present invention relates to the discovery of novel genes and proteins, which function in pathways involved in brain pathogenesis. In particular, the novel genes and proteins relate to inflammatory tissue responses caused by brain injuries such trauma, ischemia or autoimmune-inflammation or other diseases or processes related to neuroinflammation. The compounds disclosed in the present invention are useful as therapeutics, diagnostics and in screening assays.Type: GrantFiled: April 30, 1998Date of Patent: May 2, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Werner Lesslauer, Ulrike Utans-Schneitz
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Patent number: 6037479Abstract: Novel, chiral diarsine compounds, which are present in the (R)- or (S)- or (rac)-form, of the formula ##STR1## wherein R signifies an optionally substituted aryl from the group of phenyI, naphthyl, furyl and thienyl; C.sub.3-8 -cycloalkyl or C.sub.1-8 -alkyl;R.sup.1, R.sup.2, R.sup.3 each independently signify C.sub.1-8 -alkyl, C.sub.1-8 -alkoxy, aryloxy, F or Cl,R.sup.2 and R.sup.3 each independently also signify hydrogen orR.sup.1 and R.sup.2 together signify tetramethylene or a benzo or benzofuro system or dioxymethylene on the respective benzene ring; orR.sup.2 and R.sup.3 together signify dioxymethylene,and the manufacture of the diarsine compounds of formula I, as well as complexes of the compounds of formula I with Group VIII metal and their use for enantioselective reactions.Type: GrantFiled: June 26, 1998Date of Patent: March 14, 2000Assignee: Hoffman-La Roche Inc.Inventors: Emil Albin Broger, Marco Cereghetti, Frank Kienzle
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Patent number: 6030602Abstract: The invention relates to conjugates of lipids and basic, membrane disturbing peptides, particularly compounds of the formula(R--CONH).sub.n --R.sup.3 (I)and(R--S--S).sub.n --R.sup.3 (II)wherein R is the hydrocarbyl moiety of a straight-chain or branched-chain, saturated or unsaturated aliphatic carboxylic acid, or a phospholipid moiety having a free valence bond; R.sup.3 is a basic membrane disturbing peptide having a free valence bond at one or two carbon atom(s); and n is 1 or 2. These conjugates can be used as a vector for transfecting a cell with a polynucleotide or any other anionic macromolecule.Type: GrantFiled: January 14, 1997Date of Patent: February 29, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Jean-Yves Legendre, Andreas Supersaxo, Arnold Trzeciak
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Patent number: 6025325Abstract: Polyethylene and polypropylene protein conjugates which modulate body weight of animals and humans for the treatment, prevention and control of obesity and associated diseases or conditions, and the recombinant expression of these biologically active proteins in purified and homogeneous forms.Type: GrantFiled: May 15, 1996Date of Patent: February 15, 2000Assignee: Hoffman-La Roche Inc.Inventors: Arthur Campfield, Rene Devos, Yves Guisez
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Patent number: 6025324Abstract: Polyethylene and polypropylene protein conjugates which modulate body weight of ani is and humans for the treatment, prevention and control obesity and associated diseases or conditions, and the recombinant expression of these biologically active proteins in purified and homogeneous forms.Type: GrantFiled: May 15, 1996Date of Patent: February 15, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Pascal Sebastian Bailon, Arthur Campfield, Rene Devos, Yves Guisez
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Patent number: 6018020Abstract: The invention provides amino acid derivatives of the formula ##STR1## wherein E represents CHO or B(OH).sub.2 ;R.sup.1 represents lower alkyl (optionally substituted by halo, cyano, lower alkylthio, aryl-lower alkylthio, aryl or heteroaryl), lower alkenyl or lower alkynyl;R.sup.2 represents lower alkyl optionally substituted by hydroxy, carboxy, aryl, aminocarbonyl or lower cycloalkyl; andR.sup.3 represents hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together represent di- or trimethylene optionally substituted by hydroxy;R.sup.4 represents lower alkyl (optionally substituted by hydroxy, lower cycloalkyl, carboxy, aryl, lower alkylthio, cyano-lower alkylthio or aryl-lower alkylthio), lower alkenyl, aryl or lower cycloalkyl;R.sup.5 represents lower alkyl (optionally substituted by hydroxy, lower alkylthio, aryl, aryl-lower alkylthio or cyano-lower alkylthio) or lower cycloalkyl;R.sup.6 represents hydrogen or lower alkyl;R.sup.Type: GrantFiled: June 12, 1998Date of Patent: January 25, 2000Assignee: Hoffman-La Roche Inc.Inventors: Michael Richard Attwood, David Nigel Hurst, Philip Stephen Jones, Paul Brittain Kay, Tony Michael Raynham, Francis Xavier Wilson
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Patent number: 5986131Abstract: Novel nonatetraenoic acid derivatives which selectively bind to retinoic acid X-receptors (RXR) and which have anti-acne acitvity and which potentiate the activity of retinoids having RAR.alpha. activity are disclosed.Type: GrantFiled: October 17, 1997Date of Patent: November 16, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Allen John Lovey, Peter Mohr, Michael Rosenberger
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Patent number: 5969190Abstract: The compound, (E)-(1R,3R)-5-[(R)-11-hydroxy-7,11-dimethyl-dodec-2-enylidene]-cyclohexane -1,3-diol of the formula I: ##STR1## is useful in the treatment or prevention of hyperproliferative skin diseases, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis; or for reversing the conditions associated with photodamage.Type: GrantFiled: May 15, 1998Date of Patent: October 19, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Franz Bauer, Lawrence F. Courtney
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Patent number: 5968779Abstract: Proteins which modulate body weight of animals and humans for the treatment, prevention and control of obesity and associated diseases or conditions, and the recombinant expression of these biologically active proteins in purified and homogeneous forms.Type: GrantFiled: January 5, 1998Date of Patent: October 19, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Arthur Campfield, Rene Devos, Yves Guisez
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Patent number: 5938990Abstract: Multiple micro-encapsulations of a high concentration oleophilic substance using heat to set the primary particle renders the composition suitable for the production of free-flowing powders or beadlets. Microencapsulation involves forming an emulsion out of the oleophilic substance and a polymer, and then use heat setting and/or cross-linking the polymer encapsulates the oleophilic composition. This process is then repeated with a second polymer or third polymer, and with or without cross-linked via the same or different mechanism to further protect the oleophilic substance.Type: GrantFiled: May 24, 1995Date of Patent: August 17, 1999Assignee: Roche Vitamins Inc.Inventors: Stasia Boyle, Kuei-Tu Chang
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Patent number: 5919939Abstract: The invention is concerned with a new process for the preparation of compounds of formula ##STR1## wherein R.sup.1 is trityl, acetyl, tetrahydropyranyl or cyclopentyl;R.sup.2 is hydrogen, hydroxy, lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, lower alkynyl, aryl, aryloxy, aryl-lower alkyl, aryl-lower alkoxy or heterocyclyl or heterocyclyl-lower alkyl; the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl, aryloxy, aryl-lower alkoxy, the heterocyclyl moieties being unsubstituted or substituted with at least one group selected from carboxy, amino, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen, --CONR.sup.21 R.sup.22, --N(R.sup.22)COOR.sup.23, R.sup.22 CO--, R.sup.22 OCO-- or R.sup.22 COO--, wherein R.sup.21 is hydrogen, lower alkyl, or cycloalkyl; R.sup.22 is hydrogen or lower alkyl; R.sup.23 is lower alkyl, lower alkenyl or a carboxylic acid protecting group;Y is --S-- and Z is --CH.sub.2 -- orY is --CH.sub.Type: GrantFiled: May 20, 1998Date of Patent: July 6, 1999Assignee: Hoffmann-La Roche Inc.Inventor: Thomas Oberhauser
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Patent number: 5907038Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is phenyl or alpha- or beta-naphthyl, which groups can be substituted by hydroxy, lower-alkyl, lower-alkoxy, lower alkoxycarbonyl, phenoxy, acyloxy, hydroxyphenoxy-sulfonyl, halogen, nitro, amino, acylamino or N-lower-alkyl-acylamino;R.sup.2 is phenyl or phenyl substituted by hydroxy or acyloxy;Y is a carbon-carbon bond or is vinylene; andn is 1,2 or 3;and pharmaceutically acceptable acid addition salts thereof are protein kinase inhibitors and can be used for the treatment of disorders mediated by such enzymes, for example, inflammatory diseases.Type: GrantFiled: March 31, 1997Date of Patent: May 25, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Josef Stadlwieser, Sven Taylor
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Patent number: 5902882Abstract: A novel process for the manufacture of compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.Type: GrantFiled: April 3, 1997Date of Patent: May 11, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Peter Karl Matzinger, Michelangelo Scalone, Ulrich Zutter
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Patent number: 5883247Abstract: The invention is concerned with a new process for the preparation of compounds of formula ##STR1## wherein R.sup.1 is trityl, acetyl, tetrahydropyranyl or cyclopentyl;R.sup.2 is hydrogen, hydroxy, lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, lower alkynyl, aryl, aryloxy, aryl-lower alkyl, aryl-lower alkoxy or heterocyclyl or heterocyclyl-lower alkyl; the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl, aryloxy, aryl-lower alkoxy, the heterocyclyl moieties being unsubstituted or substituted with at least one group selected from carboxy, amino, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen, --CONR.sup.21 R.sup.22, --N(R.sup.22)COOR.sup.23, R.sup.22 CO--, R.sup.22 OCO-- or R.sup.22 COO--, wherein R.sup.21 is hydrogen, lower alkyl, or cycloalkyl; R.sup.22 is hydrogen or lower alkyl; R.sup.23 is lower alkyl, lower alkenyl or a carboxylic acid protecting group;Y is --S-- and Z is --CH.sub.2 -- orY is --CH.sub.Type: GrantFiled: May 14, 1997Date of Patent: March 16, 1999Assignee: Hoffmann-La Roche Inc.Inventor: Thomas Oberhauser
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Patent number: 5866684Abstract: The invention provides amino acid derivatives of the formula ##STR1## wherein E represents CHO or B(OH).sub.2 ;R.sup.1 represents lower alkyl (optionally substituted by halo, cyano, lower alkylthio, aryl-lower alkylthio, aryl or heteroaryl), lower alkenyl or lower alkynyl;R.sup.2 represents lower alkyl optionally substituted by hydroxy, carboxy, aryl, aminocarbonyl or lower cycloalkyl; andR.sup.3 represents hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together represent di- or trimethylene optionally substituted by hydroxy;R.sup.4 represents lower alkyl (optionally substituted by hydroxy, lower cycloalkyl, carboxy, aryl, lower alkylthio, cyano-lower alkylthio or aryl-lower alkylthio), lower alkenyl, aryl or lower cycloalkyl;R.sup.5 represents lower alkyl (optionally substituted by hydroxy, lower alkylthio, aryl, aryl-lower alkylthio or cyano-lower alkylthio) or lower cycloalkyl;R.sup.6 represents hydrogen or lower alkyl;R.sup.Type: GrantFiled: November 14, 1997Date of Patent: February 2, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Richard Attwood, David Nigel Hurst, Philip Stephen Jones, Paul Brittain Kay, Tony Michael Raynham, Francis Xavier Wilson
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Patent number: 5834594Abstract: The present invention is a physiologically active, substantially non-immunogenic water soluble polyethylene glycol protein conjugate having the same utility as the protein which forms the conjugate, without having the same properties of producing an immunogenic response possessed by the protein which forms this conjugate.Type: GrantFiled: June 1, 1995Date of Patent: November 10, 1998Assignee: Hoffman-La Roche Inc.Inventors: John Hakimi, Patricia Kilian, Perry Rosen
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Patent number: 5792834Abstract: The present invention is a physiologically active, substantially non-immunogenic water soluble polyethylene glycol protein conjugate having the same utility as the protein which forms the conjugate, without having the same properties of producing an immunogenic response possessed by the protein which forms this conjugate.Type: GrantFiled: June 1, 1995Date of Patent: August 11, 1998Assignee: Hoffmann-La Roche Inc.Inventors: John Hakimi, Patricia Kilian, Perry Rosen