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| Number | Title | Issue Date |
| 5955468 | BenzoG!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 |
| 5719123 | Ciclosporin 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 |
| 5665772 | O-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 |
| 5665727 | 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 for use in the topical treatment of inflammatory and hyperpoliferative skin diseases and of cutaneous manifestations of immunologica... | 09/09/1997 |
| 5656721 | Peptide 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 |
| 5650134 | Peptides 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 ... | 07/22/1997 |
| 5644052 | Process 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 |
| 5643870 | O-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 |
| 5643869 | Pipecolic 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 |
| 5639877 | Intermediates 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 |
| 5629310 | Low 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 |
| 5622982 | Acylated 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 |
| 5616703 | Separation 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 |
| 5608055 | Beta 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 |
| 5602176 | Phenyl 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 |
| 5597914 | Process 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 |
| 5596094 | Process 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 |
| 5585485 | Cephalosporin 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 |
| 5580978 | Process 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 |
| 5578585 | Pleuromutilin 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 |
| 5574155 | Process 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 |
| 5561112 | Pseudopeptide 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 |
| 5545654 | Pleuromutilin 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 |
| 5541159 | Calcitonin 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 |
| 5538997 | 2,4-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 |
| 5534503 | 2'-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 |
| 5525590 | Cyclosporins 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 |
| 5516767 | Phosphinyloxy 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 |
| 5514685 | Heteroatom-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 |
| 5493019 | Tetrahydropyran 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 |
| 5484928 | 2-(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 |
| 5409894 | Method 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 |
| 5401841 | Process 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 |
| 5378728 | Benzoic 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 |
| 5366971 | Use 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 |
| 5352671 | Heteroatoms-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 |
| 5326758 | Low 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 |
| 5319123 | Process 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 |
| 5284967 | Pleuromutilins 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 |
| 5284826 | 0-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 |