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 represent 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: Selective dopamine D1 receptor agonists for use in the treatment of primary degenerative dementia, depression, anxiety, obesity or schizophrenia.
Abstract: 1'-desoxy-1'-(6-amino-9-purinyl)-.beta.-D-ribofuranuronic acid thioamides of formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 possess various definitions given in claim 2, are effective against raised blood pressure.
Abstract: The compounds of formula I, ##STR1## in free form or in salt form have cardiotonic and antiarrhythmic activity. They may be used as medicaments. They are obtained by means of appropriate 3-amino-2-hydroxy-propylation of purines.
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:
January 29, 1988
Date of Patent:
May 30, 1989
Assignee:
Sandoz Ltd.
Inventors:
Rene Amstutz, Georg Bolliger, Gideon Shapiro
Abstract: The invention provides crystalline (6R, 7R)-7-[[2-(2-Amino-4-thiazolyl)-(Z)-2-(1-diphenylmethoxycarbonyl-1-methyle thoxy)imino ]acetamido]-3-(1-pyridiniummethyl)-3-cephem-4-carboxylate and a process for its production.
Abstract: 9-thia ergot cyclic peptide alkaloids produced by fermentation or synthetic methods have interesting anti-parkinson and other pharmacological activities.
Type:
Grant
Filed:
May 5, 1987
Date of Patent:
February 14, 1989
Assignee:
Sandoz Ltd.
Inventors:
Hans Kobel, Jean-Jacques Sanglier, Hans Tscherter, Georg Bolliger
Abstract: 4,5,5a,6-tetrahydro-dibenz[cd,f]indole derivatives having at least one oxy substitutent in one or both of the fused benzene rings, for the prevention of alcohol abuse.
Abstract: The present invention provides N,N-Diethyl-N'-[(8.alpha.)-1-ethyl-6-methyl-ergolin-8-yl]-sulfamide, and N,N-Diethyl-N'-[(8.alpha.)-1-isopropyl-6-methyl-ergolin-8-yl)-sulfamide useful as prolactin secretion inhibiton, anti-parkinson agents and anti-depressant agents.
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.1-7 alkyl; C.sub.3-7 cycloalkyl; adamantyl; or optionally substituted phenyl, are useful as neuroleptic agents and PRL secretion inhibitors.
Abstract: Novel N-substituted ergoline- and 9,10-didehydro-8-carboxamide- and -8-aminomethyl-derivatives for the treatment of vascular headaches, especially migraine, and of orthostatic hypotension.
Abstract: [2-Halo-10-oxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]acetic acids, for example of formula I ##STR1## wherein R.sub.1 is H or C.sub.1-4 alkyl and R.sub.2 is halogen, their physiologically-hydrolysable and -acceptable esters, and salts thereof. Such compounds, esters and salts possess valuable pharmaceutical, in particular anti-inflammatory, antipyretic and analgesic, properties.
Abstract: Cylosporins e.g. of formula II ##STR1## in which X is -MeBmt- or -dihydro-MeBmt- andY is -.alpha.Abu-, -Thr-, -Val- or -Nva-,wherein the residue at the 3-position, i.e. the residue Z in formula II, is an optically active, .alpha.-N-methylated .alpha.-amino acid residue of the (D)-configuration, possess pharmaceutical, in particular immunosuppressive, anti-inflammatory and anti-parasitic activity, Intermediate cyclosporin poly-anions having a de-protonated sarcosyl residue at the 3-position, e.g. polyanions of cyclosporins of formula II above wherein X and Y have the meanings given above and Z is -Sar-, in which the said residue Z is de-protonated, are also novel and part of the invention.
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: A compound of formula I ##STR1## wherein R.sub.1 is n-propyl,R.sub.2 is hydrogen or alkyl(C.sub.1-3),R.sub.3 is alkyl(C.sub.1-3), andR.sub.4 is hydrogen or methylin free base form or in pharmaceutically acceptable acid addition salt form is useful as a prolactin secretion inhibitor, anti-parkinson and anti-depressant agent.
Abstract: Cyclosporins wherein the amino acid residue at the 8-position is a (D)-acyloxy-.alpha.-amino acid residue, typically of formula ##STR1## wherein X=--MeBmt-- or --dihydro--MeBmt--, Y=--.alpha.Abu--, --Ala--, --Thr--, --Val-- or --Nva--, Z=--Val-- or --Nva-- and Q=R.sub.1 --CO--O--CH(R.sub.2)--CH(CO--)--NH-- wherein R.sub.1 =H, C.sub.1-4 alkyl or phenyl and R.sub.2 =H or CH.sub.3, possess immunosuppressive, anti-inflammatory and anti-parasitic activity.
Abstract: The present invention provides a nasal pharmaceutical composition comprising as active agent a compound of formula I, ##STR1## wherein R.sub.1 is hydrogen or halogen,R.sub.2 is hydrogen or alkyl of 1 to 4 carbon atoms,either (i) R.sub.3 is isopropyl, sec-butyl, or isobutyl, R.sub.4 methyl, ethyl or isopropyl and R.sub.5 hydrogen and R.sub.6 is hydrogen or methoxy or R.sub.5 and R.sub.6 are together a single bond,or (ii) R.sub.3 is benzyl, R.sub.4 is methyl, R.sub.5 is hydrogen and R.sub.6 is hydrogen or methoxy,in association with a pharmaceutically acceptable carrier or diluent, adapted for nasal or pulmonary administration.
Type:
Grant
Filed:
June 9, 1986
Date of Patent:
July 19, 1988
Assignee:
First Fidelity Bank, National Association, New Jersey
Abstract: A compound of formula I ##STR1## wherein R is H or R'CO wherein R'CO is an acyl radical of a carboxylic acid,Y.sub.1 is the radical linked to an alpha carbon atom an .alpha.-amino acid,Y.sub.2 is the radical linked to an alpha carbon atom of an .alpha.-amino acid, ##STR2## --CH.sub.2 --S--S--CH.sub.2 --CH.sub.2 --COOH, --(CH.sub.2).sub.p --COOH or --CH.sub.2 --S--Y.sub.3,Y.sub.3 is (C.sub.1-4)alkyl or benzyl optionally substituted by methyl or methoxy,or CH.sub.3 CO--NH--CH.sub.2 --,n is 1 to 4,A.sub.6 is Thr or D-Thr,p is 3 to 5,A.sub.8 is the aminoacyl radical of a neutral, lipophilic L-.alpha.-aminoacid,A.sub.9 is the aminoacyl radical of a neutral, lipophilic L- or D-.alpha.-aminoacid,Z is a polypeptide radical corresponding to the polypeptide radical in positions 10 to 31 of a natural calcitonin or a derivative or analogue thereof having a hypocalcemic effect,wherein, when there is more than one Y.sub.1 radical, these are the same or different, and with the exception of radical A.sub.
Type:
Grant
Filed:
December 3, 1986
Date of Patent:
July 19, 1988
Assignee:
Sandoz Ltd.
Inventors:
Francois Cardinaux, Janos Pless, Robert H. Buck