Abstract: 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula I ##STR1## wherein the symbols are as defined in claim 1, and intermediates for their manufacture are described.The compounds of formula I inhibit especially the tyrosine kinase activity of the receptor for epidermal growth factor and can be used, for example, in the case of epidermal hyperproliferation (psoriasis) and as anti-tumor agents.
Type:
Grant
Filed:
October 3, 1997
Date of Patent:
November 9, 1999
Assignee:
Novartis AG
Inventors:
Peter Traxler, Pascal Furet, Guido Bold, Jorg Frei, Marc Lang
Abstract: The invention relates to a process for the production of epothilones and intermediate products within the process.Epothilones A and B are natural substances, which can be produced by microorganisms, and the taxols have similar properties and are thus of particular interest in pharmaceutical chemistry.
Type:
Grant
Filed:
September 2, 1997
Date of Patent:
October 19, 1999
Assignee:
Novartis AG
Inventors:
Dieter Schinzer, Anja Limberg, Oliver M. Bohm, Armin Bauer, Martin Cordes
Abstract: The invention provides compounds of formula I ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.
Type:
Grant
Filed:
January 7, 1998
Date of Patent:
March 23, 1999
Assignee:
Novartis AG
Inventors:
Peter Neumann, Paul Pfaeffli, Max Peter Seiler, Robert Swoboda
Abstract: Compounds of formula I, ##STR1## wherein R.sub.1 to R.sub.4 possess the significances given in the description, may be used in the treatment of senile dementia, Alzheimer's disease and depression.
Abstract: Described are compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or hydroxy;R.sub.2, R.sub.2 ' and R.sub.2 " are each independently of the others hydrogen or a substituent other than hydrogen;eitherR.sub.3 is hydrogen or a substituent other than hydrogen andR.sub.4 is hydrogen or lower alkyl,orR.sub.3 and R.sub.4 together form a divalent radical of the formula --(CH.sub.2).sub.n -- wherein n is 2 or 3;R.sub.5 and R.sub.6 are each independently of the other hydrogen, alkyl or aryl; andeither R.sub.7 and R.sub.8 are each hydrogen, or R.sub.7 and R.sub.8 together form a bond; tautomers thereof, provided that at least one tautomerisable group is present; and salts thereof.The compounds inhibit the enzyme S-adenosylmethionine decarboxylase and are suitable, for example, for the treatment of tumours and protozoal infections.
Abstract: The invention relates to compounds of formula (I) ##STR1## wherein either R.sub.1 is hydrogen andR.sub.2 is lower alkyl lower alkenyl or lower alkynyl,m is 3 or 4 andn is 2 or 3;orR.sub.1 and R.sub.2 together are tetrainethylene,m is 3 or 4 andn is 2;or salts thereof.The compounds of formula (I) influence polyamine biosynthesis and have antiproliferative activity as well as an action against protozoans.
Abstract: The utility of known and novel staurosporin derivatives of formula I ##STR1## wherein R.sub.1 is formyl, an aliphatic hydrocarbon radical having up to 29 carbon atoms that is unsubstituted or substituted by aryl, or is an aryl radical,R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, benzoyl, lower alkanoyl or .alpha.-aminoacyl having a free or protected amino group, andR.sub.3 is hydrogen, hydroxy, lower alkoxy or oxo,or whereinR.sub.1 is methoxycarbonylmethyl,R.sub.2 is benzoyl, andR.sub.3 is hydrogen,for avoiding or removing multi-drug resistance to anti-tumour agents, such as vinblastine or adriamycin, is described.
Type:
Grant
Filed:
November 27, 1996
Date of Patent:
October 27, 1998
Assignee:
Novartis Corp.
Inventors:
Urs Regenass, Giorgio Caravatti, Oskar Wacker
Abstract: Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant binding affinity for somatostatin receptors, in free or salt form, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of somatostatin receptor positive tumors or for therapy.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
July 7, 1998
Assignee:
Novartis AG
Inventors:
Rainer Albert, Eric P. Krenning, Steven W. J. Lamberts, Janos Pless
Abstract: Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant binding affinity for somatostatin receptors, in free or salt form, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of somatostatin receptor positive tumors or for therapy.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
May 19, 1998
Assignee:
Novartis AG
Inventors:
Rainer Albert, Eric P. Krenning, Steven W. J. Lamberts, Janos Pless
Abstract: Compounds of formula I ##STR1## their physiologically-hydrolyzable and -acceptable esters and salts thereof. Said compounds, esters and pharmaceutically acceptable acid addition salts are useful as pharmaceuticals, e.g. for asthma therapy.
Abstract: A biologically active peptide selected from growth factors, peptide hormones, interferons and cytokines and analogues and derivatives thereof, and bearing at least one chelating group linked to an amino group of said peptide, the chelating group being capable of complexing a detectable element and such amino group having no significant binding affinity to target receptors, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of target tissues or for therapy.
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 6, 1995
Date of Patent:
September 23, 1997
Assignee:
Clariant Finance (BVI) Limited
Inventors:
Parfait J. M. Likibi, Robert V. Casciani, Gregory L. McCraw
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 7, 1996
Date of Patent:
September 16, 1997
Assignee:
Clariant Finance (BVI) Limited
Inventors:
Parfait J. M. Likibi, Robert V. Casciani, Gregory L. McCraw
Abstract: Compounds of formula I, ##STR1## wherein R.sub.1 to R.sub.4 possess the significances given in the description, may be used in the treatment of senile dementia, Alzheimer's disease and depression.
Abstract: 2,2-di(C.sub.1-5 alkyl)- and trans-2,2-di(C.sub.1-5 alkyl)-3,4-dihydro-3-hydroxy-6-(pyridin-4-yl)-2H-1-benzopyrans, e.g. of formula ##STR1## in which R.sub.1 and R.sub.2 =H, alkyl, hydroxyalkyl or alkoxyalkyl, at least one being other than H, R.sub.3 =typically a 2-piperidinone group, R.sub.4 =H and R.sub.5 =--OH or R.sub.4 +R.sub.5 =an additional bond, and R.sub.6, R.sub.7 are alkyl and R.sub.8 is H or alkyl, and N-oxides, esters and salts thereof, processes for their production and their uses as pharmaceuticals e.g. as K.sup.+ -channel openers, bronchodilators and asthma prophylactic agents.
Abstract: Use of a mono or bicyclic carbocyclic, or heterocyclic carboxylic, acid ester or amide or an imidazolyl carbazol in the manufaccure of a medicament suitable for the treatment of stress-related psychiatric disorders, for increasing vigilance, for the treatment of rhinitis or serotonin-induced disorders and/or coadministration with another active agent to increase the bioavailability thereof, or for nasal administration.
Type:
Grant
Filed:
March 14, 1995
Date of Patent:
October 1, 1996
Assignee:
Sandoz Ltd.
Inventors:
Moise Azria, Karl-Heinz Buchheit, Keith A. Dixon, G unther Engel, Rudolf K. A. Giger