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Attorney: Honor; Robert S., Kassenoff; Melvyn M., McGovern; Thomas O.


Number of patents: 47
Last date: September 21, 1999

1    
NumberTitleIssue Date
5955468Benzo›G!quinolines for use in prevention or delay of progressive atrophy of the optic nerve
Compounds of formula I ##STR1## wherein A, B, R1, R2, R3 and R4 are as defined in the description, are useful for the treatment of conditions where prevention or delay of progressive atrophy of the optic ne...
09/21/1999
5719123Ciclosporin form for pulmonary administration
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 particul...
02/17/1998
5665772O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants
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....
09/09/1997
5665727Use of 11,28-dioxa-4-azatricyclo[22.3.1.04,9 ]octacos-18-ene derivatives and pharmaceutical compositions containing them
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 immunologica...
09/09/1997
5656721Peptide derivatives
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 w...
08/12/1997
5650134Peptides
Somatostatin peptides bearing a chelating group selected from a bifunctional N4 -chelating group particularly suitable for Tc, Rh, Cu, Co or Re-labelling, and a bifunctional polyamino-polycarboxylic acid chelating group are complexed with a &#x...
07/22/1997
5644052Process for the production of cephalosporines and novel intermediates in this process
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...
07/01/1997
5643870O-acylated cyclosporins
A cyclosporin of the formula ##STR1## wherein A is a residue of the formula ##STR2## wherein R is hydrogen, C1-3 alkyl, C1-3 alkoxy or C1-3 alkylthio; halo-substituted-C1-3 alkyl, -C1-3 alko...
07/01/1997
5643869Pipecolic acid-containing peptolides, their preparation and pharmaceutical compositions containing them
Pipecolic acid-containing peptolides wherein the peptidic backbone is of at least 9 ଱-amino acid residues joined together by peptide bonds, particularly the compounds of formula I ##STR1## wherein the substituents have various significances, ar...
07/01/1997
5639877Intermediates in the synthesis of cephalosporins
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....
06/17/1997
5629310Low dose temazepam
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....
05/13/1997
5622982Acylated aminoalkanimidazoles and - triazoles
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 p...
04/22/1997
5616703Separation of cephalosporin isomers
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 acid a) by subjecting an amine salt of a Z/E mixture of 7-amino-3-[2-(4-m...
04/01/1997
5608055Beta lactam production
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....
03/04/1997
5602176Phenyl carbamate
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....
02/11/1997
5597914Process for the production of cephalosporins
A process for etherifying the hydroxymethyl group in position 3 of a cephalosporin by reaction of a 3-hydroxymethyl cephalosporin with an dioxycarbenium-tetrafluoroborate....
01/28/1997
5596094Process for preparing 2' -0- alkyl adenosine derivatives
A process for alkylating the 2'-OH of N6 -modified adenosine comprising the reacting of an unprotected N6 -alkyl adenosine with dimethyl sulfate and tetrabutylammonium hydrogen sulfate in a non-polar solvent, preferably dichlorometha...
01/21/1997
5585485Cephalosporin intermediate products
A cephalosporin intermediate of the formula ##STR1## where R3 is carboxyl, carboxylate, or a carboxylic acid ester group and, R8 and R9 are each independently hydrogen, halogen, (C1-4) alkyl, hydroxy, carboxamid...
12/17/1996
5580978Process for the production of 7-ACA derivatives
The invention provides an improved process for the production of 7-amino-3-alkoxymethlycephem-4-carboxyl acid derivatives....
12/03/1996
5578585Pleuromutilin derivative complexes
Complexes and pharmaceutical preparations containing complexes of the pleuromutilin derivative of formula I ##STR1## in free base or in acid addition or quaternary salt form and cyclodextrin are described. They can be prepared by complexing the above...
11/26/1996
5574155Process for the synthesis of the disodium salt hemiheptahydrate of ceftriaxone
The invention relates to a new process for the production of the disodium salt hemiheptahydrate of ceftriaxone by reacting 7-amino-3-{[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)thio] methyl}-3-cephem-4-carboxylic acid with 2-(2-aminothi...
11/12/1996
5561112Pseudopeptide isosteres of gly-asp and their use as antithrombic agents
Pseudopeptides of formula I in free or salt form ##STR1## wherein A, B, R1, X, Y and m are defined as in claim 1, and their use in the prophylactic and acute treatment of thrombosis....
10/01/1996
5545654Pleuromutilin derivatives
A compound of formula (I), in which each of R1 and R2 is independently hydrogen, alkyi or, together with the carbon atom to which it is bonded, a cycloalkyl; and each of R3 and R4 is independently hydrogen, alky...
08/13/1996
5541159Calcitonin derivatives
Peptide derivatives selected from (i) a calcitonin peptide and a LHRH antagonist peptide modified by at least one sugar residue and/or at least one short polyhydroxy compound or derivative, and (ii) a calcitonin peptide modified by at least one formyl and...
07/30/1996
55389972,4-diamino-3-hydroxycarboxylic acid derivatives
The invention relates to compounds of formula I ##STR1## wherein the substituents have various significances. They can be prepared by conventional methods, e.g. coupling, substitution, deprotection or protection reactions. They possess interesting ph...
07/23/1996
55345032'-O, N6 -disubstituted and 2'-O, N6, 2-trisubstituted adenosines and their medicinal uses
Adenosines derivatives of the formula ##STR1## wherein R1 is allyl, methallyl, straight or branched chain (C3-7)alkynyl, (C3-8)cycloalkyl, or phenyl mono- or independently of one another di-substituted by halogen havi...
07/09/1996
5525590Cyclosporins and their use as pharmaceuticals
Cyclosporins wherein the residue at the 1-position (typically -MeBmt- or -dihydro-MeBmt-) is 3'O-acylated or 3'-oxo or -C1-4 alkoxyimino substituted, or wherein the residue at the 2-position is ଲ-O-acyl or ଲ-oxo substituted, or wher...
06/11/1996
5516767Phosphinyloxy propanaminium inner salt derivatives
Compounds of the formula ##STR1## where X1 and X2 are independently O or S, and R1 is as defined in the description R2, R3, and R4 are each independently straight or branched chain (C1-4
05/14/1996
5514685Heteroatom-containing tricyclic compounds
The invention concerns the compounds of formulae ##STR1## wherein the substituents have various significances. They can be prepared by various methods, e.g. acylation, reduction, alkylation, etc. They are indicated for use as pharmaceuticals, in part...
05/07/1996
5493019Tetrahydropyran derivatives
The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances, in free form and, where such forms exist, in salt form. They can be prepared by various processes, e.g. by irradiation; oxidation; elimina...
02/20/1996
54849282-(2-aminothiazol-4-yl)-2-oxoacetic acid derivatives
Compound of formula IVe ##STR1## where Het is 2-pyridyl or 2-benzothiazolyl, are useful as acylating agents in preparing 7-[2-(2-amino-4-thiazol)-2-oxoacetyl]-cephalosporin intermediates....
01/16/1996
5409894Method of preventing balloon catheterization blood vessel damage
Somatostatin analogues and derivatives in free form or in pharmaceutically acceptable salt or complex form are useful for preventing or reducing neointimal proleferation following angioplasty....
04/25/1995
5401841Process for the production of cephalosporines
The invention relates to a new, economical and simple process for the production of 3-vinylcephalosporin compounds of formula ##STR1## wherein R1 and R2 may be the same or different and denote hydrogen or an organic radical....
03/28/1995
5378728Benzoic acid derivatives as antidiabetic agents
Compound of the formula ##STR1## where R is CH3 (CH2)m, A and B are hydrogen, a bond or --(CH2)n, X is ##STR2## m is 0, 1 , 2 or 3, n is 1 , 2, or 3, R1 is hydrogen or lower alkyl...
01/03/1995
5366971Use of 11,28-dioxa-4-azatricyclo[22.3.1.04,9 ]octacos-18-ene derivatives and pharmaceutical compositions containing them
New use of 11,28-dioxa-4-azatricyclo[22.3.1.04,9 ]octacos-18-ene derivatives and pharmaceutical compositions containing them The compounds of formula I, ##STR1## have been found to have excellent topical activity. They are thus indicated f...
11/22/1994
5352671Heteroatoms-containing tricyclic compounds
The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances. They are prepared by several processes including epimerizing replacement, treatment with cyanogen bromide or thiophosgene, treatment with ...
10/04/1994
5326758Low dose temazepam
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....
07/05/1994
5319123Process for preparing substituted N-oxy-imidic acid derivatives
N-oxy substituted imidic acid derivative of the formula ##STR1## where R1, R2 and R3 are alkyl and aryl substituents, which are useful as antidiabetic and hypolipidemic agents are prepared by the following procedure: ...
06/07/1994
5284967Pleuromutilins
Compounds of formula I ##STR1## wherein R1 and R2 are the same or different and each represent hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl are produced by a new environmentally acceptable process....
02/08/1994
52848260-hydroxyethyl and acyloxyethyl derivatives of [ser]8 cyclosporins
Hydroxy-substituted [(D)Ser]8 -Ciclosporin derivatives, particularly [O-(2-hydroxyethyl)(D)Ser]8 -Ciclosporin, have advantageous pharmacological properties and are useful as immunosuppressants, for example in the treatment of transpl...
02/08/1994
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