Abstract: The invention relates to a nitrate of (6R,7R)-7-{[2-(2-amino-4-thiazolyl)]-2-oxoacetamido}-3-(1,2,3-thiadizol-5- yl)thiomethyl-3-cephem-4-carboxylic acid, a process for its production and its use.
Abstract: Cyclic peptolides having the structure of a cyclosporin in which one amide linkage is replaced by an ester linkage are obtained by fermentation of fungal strains of the genus Cylindrotrichum Bonorden, or by cyclization of a hydroxy-undecapeptide. The cyclic peptolides have immunosuppressive, anti-inflammatory and anti-parasitic properties.
Type:
Grant
Filed:
June 20, 1988
Date of Patent:
May 26, 1992
Assignee:
Sandoz Ltd.
Inventors:
Michael M. Dreyfuss, Max H. Schreier, Hans Tscherter
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 represents a group of formula ##STR2## and R.sub.2 represents hydrogen or lower alkyl, orR.sub.1 and R.sub.2 together with the carbon atom to which they are attached represent a group of formula IIg ##STR3## R.sub.4 and R.sub.5 represents independently hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl or halogenalkyl andR.sub.6 represents a group of formula ##STR4## R.sub.1 represents a group of formula IIa to IIf as defined above, R.sub.2 and R.sub.3 together form a --(CH.sub.2)--.sub.u group wherein u stands for a whole number from 1 to 8 and R.sub.4, R.sub.5 and R.sub.6 have the meanings given above,which compounds are indicated for use as pharmaceuticals and agrochemicals.
Abstract: .alpha.-[10-oxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-carboxyli c acids, or physiologically-hydrolysable and -acceptable esters or pharmaceutically acceptable salts thereof are useful for effecting monokine inhibition, in particular interleukin-1 release or secretion inhibition, as a therapeutic means other than anti-inflammatory or anti-pyretic means.
Type:
Grant
Filed:
August 2, 1990
Date of Patent:
March 17, 1992
Assignee:
Sandoz Ltd.
Inventors:
Pietro Bollinger, Hans U. Gubler, Jorg Schnyder
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl, R.sub.2 is hydrogen, chlorine, bromine or methyl, R.sub.3 is C.sub.1-5 alkyl or C.sub.3-5 alkenyl and R.sub.4 is C.sub.3-7 alkyl; C.sub.3-7 cycloalkyl; adamantyl; or optionally substituted phenyl, having valuable pharmaceutical, and in particular LH- and PRL-secretion inhibiting as well as neuroleptic activity.
Abstract: New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R.sub.3 to R.sub.5, R.sub.9, R.sub.10, m, X, Y and Z are given in claim 1 and their N-oxides and their salts and their use in the treatment of raised blood pressure in the treatment of vascular disorders and other disorders in which a reduction in tension of the smooth muscles is therapeutically useful, as well as in the treatment of hair loss and baldness. Further the compounds are useful in the treatment of asthma and obstructive disorders of the respiratory system as well as in the prophylactic treatment of obstructive or inflammatory airways disease, for example asthma, as well as novel pharmaceutical compositions comprising said K.sup.+ channel activators suitable for such use.
Type:
Grant
Filed:
July 10, 1990
Date of Patent:
December 10, 1991
Assignee:
Sandoz Ltd.
Inventors:
Stefan Blarer, John Morley, Ian D. Chapman
Abstract: A peptide optionally in isosteric form wherein a methylene group in the backbone chain is disubstituted, one or both substituents being fluorine and/or chlorine, in free form or in pharmaceutically acceptable salt form, such as a compound of formula I ##STR1## wherein the substituents have various significances, or an isosteric form thereof,is useful as an enzyme inhibitor. In particular, as a renin inhibitor, it is useful in the prophylaxis or treatment of hypertension and congestive heart failure.It is prepared by a process comprising the step of coupling two corresponding peptide residues optionally in isosteric form, or precursors thereof, and if required appropriately converting any resultant compound in precursor form.
Abstract: The invention provides crystallilne (6R, 7R)-7-[[2 ( 2-Amino-4-thiazolyl)-(Z)-2-(1-diphenylmethoxycarbonyl-1-methylethoxy)imino ]acetamido]-3-(1--pyridiniummethyl)-3-cephem-4-carboxylate and a process for its production.
Abstract: Hydrophilic renin inhibitors, especially of formula ##STR1## wherein R.sub.1, W, o, m, n, A, B, C and D possess the definitions given in claim 2, processes for their production and their use in the treatment of hypertension, cardiac insufficiency and the treatment of diseases caused by retroviruses.
Abstract: The invention relates to activated aminothiazolyl-oximinoacetic acid derivatives, their production and their use in the production of e.g. amides, in particular cephalosporin antibiotics.
Type:
Grant
Filed:
June 19, 1989
Date of Patent:
August 6, 1991
Assignee:
Gema S.A.
Inventors:
Jose Diago Meseguer, Asuncion Esteve Bianchini, Carlos E. Lenhardt Padro, Esteve Sans Pitarch
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.
Abstract: A new compound called N,N'-carbonyl-bis-(4-ethyl-2,3-dioxo)-piperazine of Formula I ##STR1## A process for the preparation thereof based on the reaction of 4-ethyl-2,3-dioxo-piperazine or a trimethylsilyl derivative thereof with carbonyl chloride or a derivative thereof.The use of the compound of Formula I as an intermediate in the preparation of compounds of Formula II ##STR2## where R is a radical, substituted in alpha position, of a molecule of an acid selected from the group formed by phenylacetic acid, p-hydroxy phenylacetic acid, a 6-(phenylacetamido)-penicillanic acid and a 7-(phenylacetamido)-cephalosporanic acid.
Type:
Grant
Filed:
November 15, 1989
Date of Patent:
May 14, 1991
Assignee:
Gema, S.A.
Inventors:
Juan Cabre Castellvi, Jose Diago Meseguer, Asuncion Esteve Bianchini, Carlos E. Lenhardt Padro, Esteve Sans Pitarch
Abstract: The compounds of formula I ##STR1## wherein eitherR.sub.1 is hydroxy,R.sub.2 is allyl or n-propyl andthere is a single bond between the carbon atoms numbered 14 and 15orR.sub.1 is missing,R.sub.2 is allyl andthere is a double bond between the carbon atoms numbered 14 and 15,have interesting immunosuppressant and anti-inflammatory properties.They are obtained by fermentation or synthesis, e.g. by hydrogenation or dehydration.
Abstract: Process for the production of known 2-oximinoacetamido-3-cephem-4-carboxylic derivatives comprising acylation of 7-amino-3-cephem-4-carboxylic acid derivatives with novel 2-oximinoacetic acid thio esters, as well as such thioesters and their production.
Abstract: Pilocarpine derivatives of formula I, ##STR1## wherein R.sub.1 to R.sub.5 are as defined in the description, are useful in the treatment of senile dementia, Alzheimer's disease, confusional conditions in the elderly, myasthenia gravis, schizophrenia, mania or glaucoma.
Type:
Grant
Filed:
April 11, 1989
Date of Patent:
December 11, 1990
Assignee:
Sandoz Ltd.
Inventors:
Rene Amstutz, Georg Bolliger, Gideon Shapiro
Abstract: .alpha.-[10-oxy-4H-benzo[4,5]cycloheptal[1,2-b]thiophen-4-ylidene]-carboxyl ic acids, or physiologically-hydrolysable and -acceptable esters or pharmaceutically acceptable salts thereof are useful for effecting monokine inhibition, in particular interleukin-1 release or secretion inhibition, as a therapeutic means other than anti-inflammatory or anti-pyretic means.
Type:
Grant
Filed:
October 25, 1988
Date of Patent:
September 11, 1990
Assignee:
Sandoz Ltd.
Inventors:
Pietro Bollinger, Hans U. Gubler, Jorg Schnyder
Abstract: New process for the production of the pentahydrate of ceftazidime of formula ##STR1## characterized in that the ester group of the compound of formula ##STR2## or an acid addition salt thereof, is cleaved by the sole use of aqueous hydrochloric acid, and the resulting ceftazidime is either crystallized directly from the reaction mixture as the pentahydrate by adding a base, or first of all the dihydrochloride of the ceftazidime is isolated by adding acetone and/or ethanol or another anti-solvent which is miscible with water, and this is converted into the pentahydrate by known methods.
Abstract: Compounds of the formula I ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl, R.sub.2 is hydrogen, chlorine, bromine or methyl, R.sub.3 is C.sub.1-5 alkyl or C.sub.3-5 alkenyl and R.sub.4 is C.sub.3-7 alkyl; C.sub.3-7 cycloalkyl; adamantyl; or optionally substituted phenyl, having valuable pharmaceutical, and in particular LH- and PRL-secretion inhibiting as well as neuroleptic activity.