Abstract: A novel crystal form of ,&agr;-dimethyl-4-{1-hydroxy-4-{4-(hydroxydiphenylmethyl)-1-piperidinyl}butyl}benzeneacetic acid hydrochloride, processes for its preparation and its pharmaceutical use are disclosed.
Abstract: Disclosed are compounds of the formula
in free or salt form, wherein X, R1, R2, R3, and R4 are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of inflammatory or obstructive airways disease.
Type:
Grant
Filed:
March 19, 2002
Date of Patent:
July 8, 2003
Assignee:
Novartis AG
Inventors:
Stephen Paul Collingwood, Judy Hayler, Darren Mark Le Grand, Henri Mattes, Keith Allan Menear, Clive Victor Walker, Xiao-Ling Cockcroft
Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.
Type:
Grant
Filed:
May 8, 2002
Date of Patent:
July 1, 2003
Assignee:
Geneva Pharmaceuticals, Inc.
Inventors:
Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
Abstract: An ophthalmic composition particularly in the form of eye-drops suitable for the treatment of diseases of the eye and surrounding areas. The composition contains a cyclosporin and a surfactant selected from polyoxyethylene fatty acid esters, polyoxyethylene alkylphenyl ethers and polyoxyethylene alkyl ethers, or mixtures thereof.
Abstract: A pharmaceutical composition containing macrolide, e.g. a rapamycin compound in an emulsion preconcentrate or microemulsion preconcentrate for oral administration. The carrier medium for the rapamycin compound includes a hydrophilic phase, a lipophilic phase and a surfactant. The composition is stable and provides high absorption efficiency.
Type:
Grant
Filed:
March 22, 2000
Date of Patent:
May 20, 2003
Assignee:
Novartis AG
Inventors:
Gerd Fricker, Barbara Haeberlin, Armin Meinzer, Jacky Vonderscher
Abstract: A compound of formula
wherein Ac, R1 and R2 have various meanings, a process for a preparation thereof and its use as a pharmaceutical, i.e. as antibacterial agent.
Abstract: The invention relates to formulations of cyclosporin with high bioavailability for oral administration, which contain about 1 part by weight of one or more cyclosporin(s), preferably cyclosporin A and/or cyclosporin G, 7.5 to 7.8 parts by weight of one or more polyethylene glycol esters of saturated C10-C22hydroxy fatty acids, 0.7 to 0.85 part by weight of a monohydric alcohol as co-solvent, and 0.7 to 0.8 part by weight of a polyhydric alcohol as co-solvent. The drug form is produced by initially dissolving the cyclosporin in ethanol and, while stirring, adding propylene glycol and SOLUTOL® HS 15 until a clear, viscous solution results, bottled as drinkable solution or packed into capsules.
Abstract: A process is presented for producing spherical particles containing microorganism cells having desired enzyme activity. The process comprises the steps of mixing the cells directly with a primary or secondary amine-containing polymer, combining the resulting mixture with an organic solvent to form a two-phase system, and then adding a bifunctional cross-linking agent to yield the spherical particles. The preferred enzyme activities are D-amino acid oxidase and glutarylacylase activities.
Type:
Grant
Filed:
April 3, 2000
Date of Patent:
October 15, 2002
Assignee:
Biochemie Gesellschaft m.b.H.
Inventors:
Arno Reichert, Waander Riethorst, Franz Knauseder, Norbert Palma
Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.
Type:
Grant
Filed:
July 12, 2000
Date of Patent:
October 1, 2002
Assignee:
Geneva Pharmaceuticals, Inc.
Inventors:
Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
Abstract: A synergistic combination of an IL-2 transcription inhibitor (e.g., cyclosporin A or FK506) and 40-O-(2-hydroxyethyl)-rapamycin is provided, which is useful in the treatment and prevention of transplant rejection and also certain autoimmune and inflammatory diseases, together with novel pharmaceutical compositions comprising an IL-2 transcription inhibitor in combination with a rapamycin, e.g., 40-O-(2-hydroxyethyl)-rapamycin.
Type:
Grant
Filed:
January 11, 2001
Date of Patent:
September 24, 2002
Assignee:
Novartis AG
Inventors:
Gerhard Zenke, Hendrik Schuurman, Barbara Haeberlin, Armin Meinzer
Abstract: Particles of a substantially water insoluble biologically active substance, such as Cyclosporin, are loaded with a charged glyceryl ester as an electrostatic stabilizer which imparts to the particles a zeta potential and having an active substance:stabilizer weight ratio of 1:1 to 400:1 and an average particle diameter of 1 nanometer to 10 micrometers. Compositions having such particles are found to be useful delivery systems.
Abstract: Novel derivatives of rapamycin, particularly 9-deoxo-rapamycins, 26-dihydro-rapamycins, and 40-O-substituted and 28,40-O,O-disubstituted rapamycins. are found to have pharmaceutical utility, particularly as immunosuppressants.
Abstract: A pharmaceutical composition in the form of an emulsion preconcentrate for oral administration and containing a cyclosporin. The pharmaceutical composition has a carrier medium for the cyclosporin that contains a hydrophilic organic solvent; a mixed mono-, di-, and tri-glyceride or a transesterified and polyethoxylated vegetable oil; and a polyoxyethylene-sorbitan-fatty acid ester surfactant. The pharmaceutical composition provides high bioavailability and low inter- and intra-subject variability.
Abstract: Polyamide conjugates comprising either (a) a xenoantigenic group; or (b) a biologically active group and a macromolecular, macro- or microscopic entity, bound to a polyamide backbone, processes for their preparation and the use of these conjugates in therapeutic compositions.
Type:
Grant
Filed:
October 14, 1999
Date of Patent:
June 4, 2002
Assignee:
Novartis AG
Inventors:
Rudolf Duthaler, Andreas Katopodis, Willy Kinzy, Reinhold Öhrlein, Gebhard Thoma
Abstract: A polyolefinic composition comprising as component a) one or more compounds of formula I to III
in which
each R1 independently is selected from linear or branched C1-30alkyl, C5-12cycloalkyl, C2-24alkenyl, C2-18alkoxyalkyl, C2-19methoxyalkanoyl, C7-30alkaryl, C7-30aralkyl, C4-24heteroaryl (where any one of the above substituents of R1 are unsubstituted or are substituted by 1 to 3 groups selected from C1-12alkyl, —OR4, —NR4R5, —COR4 and —COOR4); and C6-30aryl, unsubstituted or substituted by 1 to 5 groups R3 selected from C1-12alkyl, C1-8alkoxy, C5-6cycloalkyl, phenyl or phenoxy, —OR4, —NR4R5, —COR4 and —COOR4,
R4 and R5 independently are selected from hydrogen, C1-30alkyl (linear or branched), C5-12cycloalkyl, C6-24aryl, C7-30alkaryl or C7-30aralkyl;
A is a direct bond, a group —(P-R1)p— or an n-valent aliphatic or aromatic residue, (preferably C1-30alkylene (linear or branched), C5-12cycloalkylene, C7-30alkarylene, C7-30aralkyl
Abstract: A method is disclosed of treating transplant-associated arteriosclerosis in a mammal which comprises administering to a mammal, preferably man, in need of such treatment an effective amount of a VLA-4 antagonist of formula I and a VCAM-1 inhibitor of formula II.
Abstract: Novel oxazolidines finding utility as intermediates in the preparation of C-13 acyloxy sidechain-bearing taxanes such as paclitaxel and analogs thereof. The present invention also relates to novel methods of coupling the oxazolidines to form the aforementioned taxanes, and to methods of preparing the oxazolidines.
Type:
Grant
Filed:
May 20, 1999
Date of Patent:
April 2, 2002
Assignee:
Bristol Myers Squibb Comp.
Inventors:
John K. Thottathil, Ivan D. Trifunovich
Abstract: A process for the synthesis of a C-4 methyl carbonate paclitaxel analog from 10-deacetylbaccatin III by the selective reduction of the acetate at the C-4 position of 10-deacetylbaccatin using Red-Al.
Abstract: Novel &bgr;-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling &bgr;-lactams to form such sidechain-bearing taxanes, and to novel sidechain-bearing taxanes.
Type:
Grant
Filed:
May 12, 1995
Date of Patent:
February 26, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
John K. Thottathil, Ivan D. Trifunovich, David J. Kucera, Wen-Sen Li
Abstract: Novel &bgr;-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling &bgr;-lactams to form such sidechain-bearing taxanes, and to novel sidechain-bearing taxanes.
Type:
Grant
Filed:
May 12, 1995
Date of Patent:
February 26, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
John K. Thottathil, Ivan D. Trifunovich, David J. Kucera, Wen-Sen Li