Abstract: 3,7-disubstituted indole derivatives of formula I ##STR1## wherein R.sub.1, R.sub.2, n, X, Y and Z are as defined in the description, are useful for the treatment of psychiatric disorders.
Abstract: 6-hydroxy or 6-alkoxy-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoxalines bearing in position 4 an optionally substituted phenyl group may be used in the treatment of schizophrenia, drug abuse or self-injurious behavior.
Type:
Grant
Filed:
May 27, 1994
Date of Patent:
July 23, 1996
Assignee:
Sandoz Ltd.
Inventors:
Peter Gull, Rudolf Markstein, Robert Swoboda
Abstract: The invention discloses microparticles comprising a polypeptide, preferably somatostatin or an analog or derivative thereof, more preferably octreotide, in a polymeric matrix, preferably poly(lactide-co-glycolide) glucose. The invention also discloses sustained release formulations containing said microparticles and the use of said formulations in treating acromegaly and breast cancer.
Type:
Grant
Filed:
January 18, 1991
Date of Patent:
July 23, 1996
Assignee:
Sandoz Ltd.
Inventors:
David Bodmer, Jones W. Fong, Thomas Kissel, Hawkins V. Maulding, Jr., Oskar Nagele, Jane E. Pearson
Abstract: The invention provides use of a 5HT-3 antagonist in the manufacture of a medicament suitable for the prevention or reduction of dependence on a dependence-inducing agent.
Abstract: Compounds of formulaA--X--Y--NH--Bwherein A is derived from optionally substituted benzothiophene, indole, 4-aza-and 7-aza-benzothiophene or-indole, A bearing in position 5 hydrogen, halogen, optionally substituted alkyl, hydroxy, nitro, amino, alkylamino, acylamino, alkoxycarbonyl, sulfamoyl, cyano, trimethylsilyl, carboxy, carbamoyl, phosphate, oxycarbamoyl, heterocyclic radical or ether or ester group, X-Y is --CR.sub.8 .dbd.N-- or CH(R.sub.8)--NH-- wherein R.sub.8 is -H or alkyl and attached at position 3 of A, and B is a heterocyclic radical or a residue ##STR1## wherein R.sub.10 is H, optionally substituted alkyl, cycloalkyl, aryl, adamantyl, acyl or carbamoyl and X.sub.2 is alkylthio or NR.sub.3 R.sub.10 wherein R.sub.3 is H or alkyl or R.sub.3 and R.sub.10 together with the nitrogen atom to which they are attached form a heterocyclic radical, in free form or in salt form, have pharmacological activity, e.g. for treating gastrointestinal disorders.
Abstract: A process for preparing carboxylates of polyoxyalkylene siloxanes and -amines, alkylpolyoxyalkylenes, polyoxyalkylene block polymers, alkylamidepolyoxyalkylenes and alkylpolyglucosides comprising subjecting a primary hydroxyl group-containing polyoxyalkylene compound or alkylpolyglucoside to mild oxidiation. The invention also relates to the novel polyoxyalkylene amine and alkylamidepolyoxyalkylene carboxylates prepared by the process.
Type:
Grant
Filed:
June 30, 1994
Date of Patent:
April 2, 1996
Assignee:
Sandoz Ltd.
Inventors:
Parfait J. Likibi, Robert V. Casciani, Gregory L. McCraw
Abstract: 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. The compounds have potent antihyperproliferative/antiinflammatory and anticancer activity.
Abstract: Novel capsaicin derivatives of general formula I ##STR1## wherein R, R.sub.1 to R.sub.7 and X may be a variety of substituents, processes for the production thereof, pharmaceutical compositions containing them and use thereof as pharmaceuticals.
Type:
Grant
Filed:
February 14, 1994
Date of Patent:
April 4, 1995
Assignee:
Sandoz Ltd.
Inventors:
Derek J. Reid, Christopher S. J. Walpole, Roger Wrigglesworth
Abstract: A process for preparing the (R) stereoisomer of 2,2-bis(hydroxmethyl)-tetrahydrofuran monobutyrate comprising subjecting the dibutyric ester of the 2,2-bis(hydroxymethyl)-tetrahydrofuran to enzymatic hydrolysis. The invention also relates to the novel (R) stereoisomer prepared by the instant process and to its more stable forms. In addition, the invention relates to the use of the (R) stereoisomer in preparing stereoisomers of pharmacologically active compounds and to certain specific stereoisomers produced thereby.
Type:
Grant
Filed:
June 4, 1993
Date of Patent:
August 16, 1994
Assignee:
Sandoz Ltd.
Inventors:
Heinrich Estermann, Prasad K. Kapa, Russell L. Underwood, William J. Houlihan
Abstract: A process for preparing carboxylates of polyoxyalkylene siloxanes and -amines, alkylpolyoxyalkylenes, polyoxyalkylene block polymers, alkylamidepolyoxyalkylenes and alkylpolyglucosides comprising subjecting a primary hydroxyl group-containing polyoxyalkylene compound or alkylpolyglucoside to mild oxidiation. The invention also relates to the novel polyoxyalkylene amine and alkylamidepolyoxyalkylene carboxylates prepared by the process.
Type:
Grant
Filed:
March 26, 1991
Date of Patent:
August 2, 1994
Assignee:
Sandoz Ltd.
Inventors:
Parfait J. M. Likibi, Robert V. Casciani, Gregory L. McCraw
Abstract: The invention discloses certain substituted .alpha.-aminoacids having the formula ##STR1## where m and n are 1 or 2, and R, R.sub.1, R.sub.2, R.sub.3 and Y have various significances, which compounds are useful in treating epilepsy, disorders associated with excess GH or LH secretion, anxiety, schizophrenia, depression, CNS degenerative disorders, cerebral hypoxic conditions and stress-related psychiatric disorders.
Abstract: A screening method for detecting the vulnerability of patients on clozapine therapy to developing agranulocytosis which comprises establishing the concentration of N-desmethylclozapine in the blood or bone marrow of said patient. In addition, a method of determining patient sensitivity to N-desmethylclozapine is provided which comprises collecting heparinized blood and assaying it for stem cell sensitivity to N-desmethylclozapine.
Abstract: The invention discloses certain heterocyclic, thioether, keto-ester and alkyl phospholipids, e.g., heterocyclic phospholipids having the formula ##STR1## where R is n-C.sub.14 -C.sub.20 alkyl or O-n-C.sub.14 -C.sub.20 alkyl; each R.sub.1 is methyl or ethyl; n is 2-6; and X is --CH.sub.2 --m, where m is 2-4, CH.sub.2 CH.sub.2 O or CH.sub.2 CH.sub.2 S, or a corresponding hydrate thereof, which compounds are useful in treating multiple sclerosis.
Abstract: The invention provides use of a 5HT-3 antagonist in the manufacture of a medicament suitable for the prevention or reduction of dependence on a dependence-inducing agent.
Abstract: 3,7-disubstituted indole derivatives of formula I ##STR1## wherein R.sub.1, R.sub.2, n, X, Y and Z are as defined in the description are useful for the treatment of psychiatric disorders.
Abstract: Use of calcium antagonists of formula I ##STR1## wherein the substituents have various significances in the treatment of conditions related directly or indirectly to ionized calcium levels in the blood and combinations of calcium antagonists, e.g. of formula I, with calcitonins.
Abstract: A process for preparing the (R) stereoisomer of 2,2-bis(hydroxmethyl)-tetrahydrofuran monobutyrate comprising subjecting the dibutyric ester of the 2,2-bis(hydroxymethyl)-tetrahydrofuran to enzymatic hydrolysis. The invention also relates to the novel (R) stereoisomer prepared by the instant process and to its more stable forms. In addition, the invention relates to the use of the (R) stereoisomer in preparing stereoisomers of pharmacologically active compounds and to certain specific stereoisomers produced thereby.
Type:
Grant
Filed:
April 26, 1991
Date of Patent:
July 20, 1993
Assignee:
Sandoz Ltd.
Inventors:
Heinrich Estermann, Prasad K. Kapa, Russell L. Underwood, William J. Houlihan
Abstract: Certain patients undergoing clozapine drug therapy may be vulnerable to agranulocytosis. It has been found that agranulocytosis vulnerability is correlated with the presence of HLA antigens B38, DR4 and DQw3. Accordingly, a method is provided for detecting such patients, and an HLA kit is provided.
Type:
Grant
Filed:
March 19, 1991
Date of Patent:
June 29, 1993
Assignees:
Long Island Jewish Medical Center, Dana-Farber Cancer Institute