Patents Represented by Attorney Thomas O. McGovern
  • Patent number: 5955468
    Abstract: Compounds of formula I ##STR1## wherein A, B, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description, are useful for the treatment of conditions where prevention or delay of progressive atrophy of the optic nerve is desirable.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 21, 1999
    Assignee: Sandoz Ltd.
    Inventor: Rudolf Markstein
  • Patent number: 5840885
    Abstract: A new process is described for the production of 6-alpha-amino-penicillins and 7-alpha-amino-desacetoxy-cephalosporins free from halogen-containing solvents by acylating 6-APA, 7-ADCA or a derivative thereof in a halogen-free solvent.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 24, 1998
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Jose Diago, Johannes Ludescher
  • Patent number: 5767069
    Abstract: Nonimmunosuppressant cyclosporin derivatives having cyclophilin-binding activity, for example, the compound, ?MeIle!.sup.4 -ciclosporin, are useful in inhibiting HIV-1 replication in treating AIDS and AIDS related disorders.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: June 16, 1998
    Assignee: Novartis AG
    Inventors: Soo Young Ko, Hans Kobel, Brigitte Besemer-Rosenwirth, Dieter Seebach, Rene P. Traber, Roland Wenger, Pietro Bollinger
  • Patent number: 5719276
    Abstract: A new process is described for the production of 6-alpha-amino-penicillins and 7-alpha-amino-desacetoxy-cephalosporins free from halogen-containing solvents by acylating 6-APA, 7-ADCA or a derivative thereof in a halogen-free solvent.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 17, 1998
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Jose Diago, Johannes Ludescher
  • Patent number: 5719123
    Abstract: Pulmonary administration of Ciclosporin in orthorhombic crystal form (designated "CY-A/X-III"), e.g. for the treatment of obstructive or inflammatory airways disease, e.g. asthma, as well as crystalline Ciclosporin, e.g. CY-A/X-III, in spheroidal particulate form, processes for its preparation and its pharmaceutical use, e.g. for pulmonary administration. Pharmaceutical compositions comprising CY-A/X-III and crystalline Ciclosporin, e.g. CY-A/X-III, in spheroidal particulate form as well as Ciclosporin in solution in aerosol propellants are also provided.
    Type: Grant
    Filed: June 6, 1994
    Date of Patent: February 17, 1998
    Assignee: Sandoz Ltd.
    Inventors: John Morley, Andreas Rummelt, Martin List
  • Patent number: 5686604
    Abstract: The invention relates to a new economical and simple process, using a new intermediate compound, for the production of 3'-substituted 7-amino-3-propenyl-4-cephem-carboxylic acid derivatives of formula ##STR1## wherein R is hydrogen, a negative charge or a silyl protecting group, R.sub.o is hydrogen or methoxy, R.sub.1 is hydrogen or a silyl protecting group and X is the radical of a nucleophile, and their acid addition salts.
    Type: Grant
    Filed: May 5, 1995
    Date of Patent: November 11, 1997
    Assignee: Biochemie Gesellschaft
    Inventors: Johannes Ludescher, Hubert Sturm, Josef Wieser
  • Patent number: 5665727
    Abstract: The compounds of formula I, ##STR1## have been found to have excellent topical activity. They are thus indicated for use in the topical treatment of inflammatory and hyperpoliferative skin diseases and of cutaneous manifestations of immunologically-induced illnesses, such as psoriasis.
    Type: Grant
    Filed: August 15, 1994
    Date of Patent: September 9, 1997
    Assignee: Sandoz Ltd.
    Inventors: Maximilian Grassberger, Josef Gottfried Meingassner, Anton Stutz, Peter Stutz
  • Patent number: 5665772
    Abstract: Novel derivatives of rapamycin, particularly 9-deoxorapamycins, 26-dihydro-rapamycins, and 40-0-substituted and 28,40-0,0-di-substituted rapamycins, are found to have pharmaceutical utility, particularly as an immunosuppressants.
    Type: Grant
    Filed: April 7, 1995
    Date of Patent: September 9, 1997
    Assignee: Sandoz Ltd.
    Inventors: Sylvain Cottens, Richard Sedrani
  • Patent number: 5659030
    Abstract: A p-toluenesulphonic acid salt of 7-[2-(2-aminothiazol-4-yl)-2-(Z)-hydroximino-acetamido]-3-N,N-dimethylcarb amoyloxymethyl-3-cephem-4-carboxylic acid (isopropoxycarbonyloxy)ethylester, e.g. of formula ##STR1## its use in the production of other salts and a pharmaceutical composition containing it.
    Type: Grant
    Filed: June 14, 1995
    Date of Patent: August 19, 1997
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Johannes Ludescher, Rainer Pucher, Siegfried Wolf
  • Patent number: 5656721
    Abstract: The present invention provides a sugar derivative of a biologically active peptide, which derivative has a prolonged duration of action when compared to the non-sugar modified peptide, and contains at least on one of the amino acid units a sugar residue which is attached to an amino group thereof by a coupling other than a direct N-glycosidic bond, and additionally, when it is a condensation product of a carboxyl group containing sugar and a peptide with less than 8 amino acid units, by a coupling other than a direct amide bond.
    Type: Grant
    Filed: July 7, 1994
    Date of Patent: August 12, 1997
    Assignee: Sandoz Ltd.
    Inventors: Rainer Albert, Wilfried Bauer, Francois Cardinaux, Monika Mergler, Janos Pless, Walter Prikoszovich
  • Patent number: 5650134
    Abstract: Somatostatin peptides bearing a chelating group selected from a bifunctional N.sub.4 -chelating group particularly suitable for Tc, Rh, Cu, Co or Re-labelling, and a bifunctional polyamino-polycarboxylic acid chelating group are complexed with a .alpha.-, .beta.-, .gamma.- or positron-emitting nuclide or a nuclide with Auger-e.sup.- -cascades and are useful as radiopharmaceuticals.
    Type: Grant
    Filed: July 12, 1995
    Date of Patent: July 22, 1997
    Assignee: Novartis AG (formerly Sandoz Ltd.)
    Inventors: Rainer Albert, Helmut Macke
  • Patent number: 5644052
    Abstract: The invention relates to a new economical and simple process, using a new intermediate compound, for the production of 3'-substituted 7-amino-3-propenyl-4-cephem-carboxylic acid derivatives of formula ##STR1## wherein R is hydrogen, a negative charge or a silyl protecting group, R.sub.o is hydrogen or methoxy, R.sub.1 is hydrogen or a silyl protecting group and X is the radical of a nucleophile, and their acid addition salts.
    Type: Grant
    Filed: May 5, 1995
    Date of Patent: July 1, 1997
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Johannes Ludescher, Hubert Sturm, Josef Wieser
  • Patent number: 5643869
    Abstract: Pipecolic acid-containing peptolides wherein the peptidic backbone is of at least 9 .alpha.-amino acid residues joined together by peptide bonds, particularly the compounds of formula I ##STR1## wherein the substituents have various significances, are disclosed. They can be prepared by isolation or derivation from an appropriate microorganism strain such as S 42508/F (NRRL 15761).They have interesting pharmacological, e.g. antifungal, chemotherapeutic drug resistance reversing and to some extent immunosuppressant and antiinflammatory properties.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: July 1, 1997
    Assignee: Sandoz Ltd.
    Inventors: Michael Morris Dreyfuss, Gerhard Emmer, Maximilian Grassberger, Klaus Ruedi, Hans Tscherter
  • Patent number: 5643870
    Abstract: A cyclosporin of the formula ##STR1## wherein A is a residue of the formula ##STR2## wherein R is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy or C.sub.1-3 alkylthio; halo-substituted-C.sub.1-3 alkyl, -C.sub.1-3 alkoxy or -C.sub.1-3 alkylthio; hydroxy-substituted-C.sub.1-3 alkyl, -C.sub.2-3 alkoxy or -C.sub.2-3 alkylthio; or amino or mono- or di-(C.sub.1-2 alkyl)-amino,X is oxygen or sulphur,--x--y-- is --CH.dbd.CH-- (trans) or --CH.sub.2 --CH.sub.2 --,B is -.alpha.Abu-, -Val-, -Thr- or -Nva- andQ is -(D)Ala-; -(D)Ser-; -[O-(2-hydroxyethyl)(D)Ser]-; or -[O-acyl(D)Ser]- or -[O-(2-acyloxy ethyl)(D)Ser]-in which the acyl residue is physiologically hydrolysable and acceptable, are useful in the topical treatment of asthma.
    Type: Grant
    Filed: February 26, 1993
    Date of Patent: July 1, 1997
    Assignee: Sandoz Ltd.
    Inventors: Johann Jakob Boelsterli, Marcel Karl Eberle, Reto Naef, Trevor Glyn Payne
  • Patent number: 5639877
    Abstract: Novel amidine salts of 7-Amino-3-hydroxymethyl-3-cephem-4-carboxylic acid (=HACA), particular guanidine and diaza-bicyclo-alkylene salts, are useful as intermediates in the synthesis of cephalosporins.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: June 17, 1997
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Johannes Ludescher, Ingolf Macher
  • Patent number: 5629310
    Abstract: This invention relates to a hard gelatin capsule containing no more than 5 to 10 milligrams of crystalline temazepam and its use in the treatment of transient insomnia.
    Type: Grant
    Filed: April 17, 1995
    Date of Patent: May 13, 1997
    Inventor: William R. Sterling
  • Patent number: 5622982
    Abstract: The invention concerns azole compounds of formula ##STR1## wherein the substituents have various significances, in free form or salt form.They can be prepared e.g. by acylation, or by aziridine or oxazole ring opening.The compounds can be used as pharmaceuticals, especially as selective inhibitors of the 25-hydroxyvitamin D3--hydroxylases in the treatment of disorders of proliferation and differentiation in vitamin D--responsive tissues.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: April 22, 1997
    Assignee: Sandoz Ltd.
    Inventors: Ingeborg Schuster, Helmut Egger
  • Patent number: 5616703
    Abstract: Process of depleting 7-amino-3-[(E)-2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acid in Z/E mixtures of 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acida) by subjecting an amine salt of a Z/E mixture of 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephen-4-carboxylic acid to crystallization and converting this amine salt into 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acid, orb) by subjecting the Z/E mixture to chromatography.
    Type: Grant
    Filed: November 16, 1994
    Date of Patent: April 1, 1997
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Johannes Ludescher, Harald Summer, Siegfried Wolf
  • Patent number: 5608055
    Abstract: A new process is described for the production of 7-alpha-aminoacyl-cephalosporin free from halogen-containing solvents by acylating 7-amino-ceph-3-em-4-carboxylic acid or a derivative thereof in a halogen-free solvent.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 4, 1997
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Jose Diago, Johannes Ludescher
  • Patent number: 5602176
    Abstract: The (S)-N-ethyl-3-[(1-dimethylamino)ethyl]-N-methyl-phenylncarbamate in free base or acid addition salt form is useful as pharmaceutical, particularly for systemic transdermal administration.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 11, 1997
    Assignee: Sandoz Ltd.
    Inventor: Albert Enz