Abstract: New use of 11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene derivatives and pharmaceutical compositions containing themThe 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 immunologically-induced illnesses, such as psoriasis.
Type:
Grant
Filed:
November 30, 1992
Date of Patent:
November 22, 1994
Assignee:
Sandoz Ltd.
Inventors:
Maximilian Grassberger, Josef G. Meingassner, Anton Stutz, Peter Stutz
Abstract: 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 an acid having a non-nucleophilic anion, treatment with dimethylsulfoxide and acetic anhydride, acylation, treatment with an oxalyl derivative and ammonia, methylation, oxidation, deprotection and protection.They possess interesting pharmacological activity as antiinflammatory, immunosuppressant, antiproliferative and chemotherapeutic drug resistance reversing agents.
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: N-oxy substituted imidic acid derivative of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are alkyl and aryl substituents, which are useful as antidiabetic and hypolipidemic agents are prepared by the following procedure: ##STR2## where X is chlorine, bromine, or iodine, and R.sub.1 ' is the same as R.sub.1 but with any hydroxy or carboxy groups present protected by a hydroxy or carboxy protecting group and, when R.sub.1 ' is a protected hydroxy or carboxy substituent, deprotecting the substituent.
Type:
Grant
Filed:
May 17, 1991
Date of Patent:
June 7, 1994
Assignee:
Sandoz Ltd.
Inventors:
George T. Lee, Ustun B. Sunay, Prasad K. Kapa
Abstract: Hydroxy-substituted [(D)Ser].sup.8 -Ciclosporin derivatives, particularly [O-(2-hydroxyethyl)(D)Ser].sup.8 -Ciclosporin, have advantageous pharmacological properties and are useful as immunosuppressants, for example in the treatment of transplant rejection and autoimmune diseases.
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represent hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl are produced by a new environmentally acceptable process.
Abstract: A compound of formula I ##STR1## wherein R.sub.1 is C.sub.1-4 alkyl, C.sub.3-4 alkenyl or (C.sub.3-5 cycloalkyl)-methyl, R.sub.2 is C.sub.1-4 alkyl, [hydroxy- or (C.sub.1-4 alkoxy)-substituted C.sub.1-3 alkyl]-methyl, (C.sub.3-5 cycloalkyl)-methyl, tetrahydrofuran 2-yl-methyl or 1,3-dioxolan-2-yl-methyl, R.sub.3 and R.sub.4 are each hydrogen, hydroxymethyl, methoxymethyl or N,N-dimethylcarbamoyloxymethyl, R.sub.5 is hydroxy or methoxy, R.sub.6 is hydrogen, hydroxy, methoxy or halogen and R.sub.7 is in the 2- or 3-position and is hydroxy, methoxy or halogen, or together with R.sub.5 is 3,4-methylendioxy, or together with R.sub.6 is 2,3-methylenedioxy and their physiologically-hydrolysable and -acceptable esters are useful in the treatment (symptomatic and prophylactic) of obstructive or inflammatory airways disease, in particular asthma, and disease characterised by or having an aetiology comprising morbid eosinophil accumulation or activation, e.g. hypereosinophilia.
Abstract: The invention relates to the compound of formula I ##STR1## in free base form or in acid addition salt form its preparation and use as a medicament for glaucoma, depression, Morbus Parkinsonism or cocaine abuse.
Abstract: The saccharides of formula I, ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently are optionally substituted acyl, are novel. They possess interesting pharmacological, especially immunostimulant, antiinflammatory and antitumor properties. They may be obtained by deprotection of a corresponding compound in protected form.
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: The 3-O-[N-acetylmuramyl-D-isoglutaminyl]-1,2-di-O-palmitoyl-sn-glycerol derivative of formula I ##STR1## wherein the carbon atom marked with an asterisk * has the R or, respectively, the S configuration, possesses interesting pharmacological, in particular immunomodulating properties. It is particularly useful as an immunomodulant, as an adjuvant in vaccines and as a suppressing agent for IgE formation in e.g. type I allergies and atopical dermatitises.It is obtained by deprotection of a corresponding compound having one or more hydroxy group(s) in protected form.
Type:
Grant
Filed:
June 27, 1990
Date of Patent:
May 11, 1993
Assignee:
Sandoz Ltd.
Inventors:
Louis Chedid, Peter Dukor, Pierre Lefrancier, Peter Stutz
Abstract: The compounds of formula I ##STR1## wherein the substituents have various significances, possess pharmacological, particularly antiinflammatory and immunosuppressant activity.They can be prepared by one or more of the following process variants: reduction, deprotection, acylation, reaction with N,N'-carbonyl- or N,N'-thiocarbonyldiimidazole, halogenation, splitting off of hydrogen halide, reaction with a hydrogen carbonate, radical deoxygenation, dehydration or reaction with diazomethane of -ethane, optionally under transient protection of reactive groups which it is not desired to react.
Type:
Grant
Filed:
June 13, 1991
Date of Patent:
April 6, 1993
Assignee:
Sandoz, Ltd.
Inventors:
Andrew J. F. Edmunds, Maximilian Grassberger
Abstract: Compounds of formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description, are useful for the treatment of conditions associated with cerebral ischaemia, e.g. stroke.
Type:
Grant
Filed:
December 12, 1990
Date of Patent:
March 2, 1993
Assignee:
Sandoz Ltd.
Inventors:
Joachim Nozulak, Andre Sauter, Jean-Marie Vigouret
Abstract: Halogenoalkylphenyl-alcohols, ketones and their hydrates of formula I, ##STR1## wherein R.sub.1 to R.sub.8 are as defined in the description, are useful as acetylcholinesterase inhibitors.
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represent hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl are produced by a new environmentally acceptable process.
Abstract: Somatostatin analogues and derivatives in free form or in pharmaceutically acceptable salt or complex form are useful for treating degenerative and inflammatory processes in bone or catilage, e.g. arthritic conditions or diseases.
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is alkyl, alkoxy, alkylthio, alkylamino, aryl, aryloxy, arylthio, arylamino, aralkyl, aralkoxy, aralkylthio or aralkylamino,R.sub.2 and R.sub.3 are each independently hydrogen, halogen, hydroxy, mercapto, nitro or amino or have the meanings given for R.sub.1, andX is --NH.sub.2, --NH--OH, --N(R.sub.4)OH, --NH--NH.sub.2 or --NH--N.dbd.C(R.sub.4)R.sub.5, whereinR.sub.4 and R.sub.5 are each alkyl,in free form or pharmaceutically acceptable salt form, have pharmaceutical utility, in particular in the treatment or prophylaxis of asthma, or in the treatment of inflammation or psoriasis.