Abstract: The invention relates to 6-substituted 10.beta.-alkynylestrene derivatives wherein the 6 substituent is amino, azido, halogen or an alkylidene group and to corresponding 6,7-dihalo analogs.The invention provides also a process for the preparation of the above compounds and pharmaceutical compositions containing same.The compounds of the invention are useful aromatase inhibitors and can be used, e.g., in the treatment of hormone-dependent tumors and prostatic hyperplasia.
Type:
Grant
Filed:
December 15, 1986
Date of Patent:
February 28, 1989
Assignee:
Farmitalia Carlo Erba S. R. L.
Inventors:
Franco Faustini, Enrico di Salle, Vittoria Villa, Paolo Lombardi
Abstract: The invention relates to 6-alkylidenandrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R.sub.2, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl, which are useful in therapy, in particular in the treatment of hormone-dependent cancers.
Type:
Grant
Filed:
July 7, 1986
Date of Patent:
February 28, 1989
Assignee:
Farmitalia Carlo Erba S.r.l.
Inventors:
Franco Buzzetti, Natale Barbugian, Paolo Lombardi, Enrico di Salle
Abstract: Compounds of the formula I: ##STR1## wherein R.sub.1 =H, CH.sub.3 ; m=0,1; R.sub.2 =R.sub.3 =H or R.sub.2, R.sub.3 =bond, R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon, n=1 or 2 and their pharmaceutically acceptable salts are antihypertensive agents. Their preparation and pharmaceutical compositions containing them are also described.
Abstract: The invention relates to cycloalkyl-substituted 4-pyridyl derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl;each of R.sub.1 and R.sub.2 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;n is an integer of 1 to 5; and either(a) A is >C.dbd.O and B is --O--, --NH-- or --CH.sub.2 --; or(b) A is --CH.sub.2 --and B is --O--, --NH--, --CH.sub.2 -- or >C.dbd.O; or(c) A is --O-- and B is >C.dbd.O or --CH.sub.2 --; or(d) A is --NH-- and B is >C.dbd.O or --CH.sub.2 --,and their pharmaceutically acceptable salts.The compounds of the invention show aromatase inhibiting activity and can be useful, e.g., in treating hormone-dependent tumors and prostatic hyperplasia.
Type:
Grant
Filed:
July 13, 1987
Date of Patent:
January 10, 1989
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Angelo Crugnola, Enrico di Salle, Paolo Lombardi
Abstract: A process of preparing taurine-containing peptides of formula (I): ##STR1## comprises reacting a protected aminoacid with cysteamine or cystamine in the presence of a condensing agent, oxidizing the resulting compound and deprotection.
Abstract: Device for easily and simply coupling to the free end of a small tube (7) mounted on a transfusion needle an apparatus of the type used for coupling a syringe to a drug holding bottle. The device comprises a hollow shaped body (1) that can be coupled to the small tube (7). An axial passageway (13) in the body (1) is closed by a plug (5). A collar (2) shaped as the mouth of a conventional drug bottle projects from the body (1). The collar (2) extends axially and a continuous annular recess (3) is formed therein. The recess (3) has a profile and arrangment sized and shaped to allow for the teeth projecting from the resilient lugs of the apparatus to which the device is to be coupled to be inserted and locked therein.
Abstract: The invention concerns a method and an equipment for the simulated distillation, by means of gas chromatography, of petroleum products, capable of characterizing also high boiling products, exceeding C55, over 600.degree. C. TBP. A chromatograph is used with a capillary column having a length less than or equal to 10 m, containing an immobilized non polar polydimethylsilicon gum stationary phase with a film thickness less than or equal to 0.2 .mu.m. The sample is introduced through a non vaporizing direct cold on-column injection and the eluted sample is detected by means of a FID detector. The column oven is operated in temperature programming conditions up to temperatures exceeding 400.degree. (up to 430.degree.-450.degree. C.).
Type:
Grant
Filed:
December 11, 1987
Date of Patent:
November 22, 1988
Assignee:
Carlo Erba Strumentazione S.p.A.
Inventors:
Sorin Trestianu, Fausto Munari, Carlo Saravalle
Abstract: A body is provided with members for coupling it to one end of a bottle or the like. The body has a seat for housing the free end of a syringe, with a hole for allowing for the syringe needle to pass through. The free end of a syringe may be housed and threaded in the seat. On the side opposite surfaces of the body seat and at the syringe end provided for insertion in the seat, there are formed radially projecting longitudinal teeth and slanted resilient fins which are deflected by the teeth as the syringe is threaded to the body. The teeth abut against the fins, thereby preventing the syringe from being screwed off the body.
Abstract: In order to withdraw pharmaceutical products from sterile vials by means of a syringe, apparatus is used on one end of which a syringe possibly containing a liquid solvent is mounted and at the other end of which a seat is provided for housing the mouth of a vial. The syringe needle can puncture the rubber or similar stopper by which the vial is sealed, while the needle itself remains enclosed and protected by said apparatus. The invention relates to a device which, when the vial has been removed, can itself be housed in said apparatus seat to enable the needle to puncture a rubber stopper provided on the device, which is connected to one end of a cannula having for example mounted on its other end a needle for transfusion purposes. In this manner, the liquid can be discharged from the syringe while the needle remains enclosed and protected by the said apparatus.
Abstract: Ergoline Esters having the formula (I) ##STR1## in which R.sub.1 =H or CH.sub.3 ; R.sub.2 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.3 =H or OCH.sub.3 ; R.sub.4 =H or halogen; R.sub.5 =C.sub.1 -C.sub.4 alkyl and their pharmaceutically acceptable salts are active at the central nervous system level. A process for their preparation is described.
Abstract: The invention relates to a chemiluminescent composition, i.e. one which emits light when its various constituent components are mixed together.The composition consists of at least two separate solutions of at least one oxalate, at least one fluorescent substance, hydrogen peroxide and at least one catalyst, in which those components which react together are kept separated. The characteristic of the 9,10-bis(phenylethynyl)anthracene is that the oxalate is a bis(dihalo-acylphenyl)oxalate. This compound is easily and economically produced and is easily soluble in the solvents used, to provide high-intensity light emission for long time periods. The 2,4- or 2,6-acyl substituted phenyloxalate also forms a subject matter of the invention.
Abstract: This invention concerns a chamber for chromatographic analyses, in which capillary columns, in particular columns of fused silica, are thermally conditioned. The chamber comprises a thermally insulated space which can be perfectly sealed towards the outside and which houses means for heating the air and at least a fan for air circulation inside said space. In order to make the air flow going to the column(s) within the chamber as homogeneous and stable as possible from the thermal viewpoint the heating means are positioned on the suction side of the fan or of each fan, so to cause a perfect mixing of cold and hot fluid flow threads or lines in correspondence with the fan itself, and thereby obtain a uniform and stable air current from the fan towards the column.
Type:
Grant
Filed:
February 9, 1983
Date of Patent:
September 20, 1988
Assignee:
Carlo Erba Strumentazione, S.p.A.
Inventors:
Giorgio Sisti, Bruno Tosi, Giovanni Ostan, Fausto Munari, Ermete Riva, Sorin Trestianu
Abstract: The invention relates to 6-substituted androsta-1,4-diene-3,17-dione derivatives wherein the 6 substituent is an azido, amino or substituted amino group.The invention provides also a process for preparing the said compounds and pharmaceutical compositions containing same.The compounds of the invention are useful aromatase inhibitors and can be used, e.g., in the treatment of hormone-dependent tumors.
Type:
Grant
Filed:
July 21, 1986
Date of Patent:
September 13, 1988
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Franco Faustini, Roberto D'Alessio, Vittoria Villa, Enrico di Salle, Paolo Lombardi
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 is each H, halo or an organic group, R.sub.3 is H or organic group, n=1 or 2, M is a heavy mono- or divalent metal, or M.sub.2 A wherein M.sub.2 is a heavy divalent metal and A is an organic or inorganic group, are prepared by treating a starting penicillin in a solvent with a salt of M.sub.1 or M.sub.2 A in the presence of a base at a temperature of from -70.degree. to 100.degree. C.
Type:
Grant
Filed:
January 13, 1986
Date of Patent:
September 13, 1988
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Marco Alpegiani, Angelo Bedeschi, Ettore Perrone
Abstract: The invention relates to cycloalkyl substituted 4-aminophenyl derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl:n is an integer of 1 to 5; and either(a) A is ##STR2## and B is --O--, --NH-- or --CH.sub.2 --; or (b) A is --CH.sub.2 -- and B is --O--, --NH--, --CH.sub.2 -- or ##STR3## or (c) A is --O-- and B is ##STR4## or --CH.sub.2 --; or (d) A is --NH-- and B is ##STR5## or --CH.sub.2 -- and their pharmaceutically acceptable salts.The scope of the invention includes also a process for preparing the said compounds of formula (I) and pharmaceutical compositions containing same.The compounds of the invention show aromatase inhibiting activity and can be useful, e.g., in treating hormone-dependent tumors and prostatic hypertrophy or hyperplasia.
Type:
Grant
Filed:
September 2, 1986
Date of Patent:
September 6, 1988
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Paolo Lombardi, Angelo Crugnola, Enrico di Salle
Abstract: Compound of the formula (I) ##STR1## wherein n is zero or an integer of 1 to 3;R is(a) --NHR.sub.3, wherein R.sub.3 is(a') --CON(NO)R.sub.4, in which R.sub.4 is C.sub.1 -C.sub.4 alkyl either unsubstituted or substituted by halogen; or(b') --CO(CH.sub.2).sub.m --R.sub.5, in which R.sub.5 is halogen, oxiranyl, methyloxiranyl, aziridinyl, a group ##STR2## or a group ##STR3## and m is zero or an integer of 1 to 4; or (b) ##STR4## wherein either R.sub.6 and R.sub.7 are the same and are each oxiranemethyl, aziridinemethyl, or C.sub.2 -C.sub.4 alkyl 2-substituted by halogen or by a group --OSO.sub.2 R.sub.8 wherein R.sub.8 is C.sub.1 -C.sub.4 alkyl or phenyl, or one of R.sub.6 and R.sub.7 is hydrogen and the other is as defined above;each group R.sub.1 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.2 is a C.sub.1 -C.sub.6 alkyl group terminating with (i) a basic moiety chosen from an amino group, a mono- or di- C.sub.1 -C.sub.
Abstract: The compounds of the invention have the following general formula (I) ##STR1## wherein each of the groups R, R.sub.1 and R.sub.2, which may be the same or different, represents a hydrogen atom, a C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl group, and R.sub.3 represents a straight or branched chain, saturated or unsaturated, C.sub.1 -C.sub.8 aliphatic hydrocarbon group. The compounds are useful as antilipolytic agents.
Type:
Grant
Filed:
December 5, 1986
Date of Patent:
August 23, 1988
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Paolo Cozzi, Antonio Pillan, Leone Bertone, Pier P. Lovisolo
Abstract: A device for heating sample containing vials, in a gas-chromatographic apparatus provided with an automatic sampler, which includes a shroud in which a depression is made by a fan which sucks external air and conveys it under pressure into a Venturi tube shaped duct. This depression causes more external air to be sucked through separate openings of the shroud and to follow a different path along the resistors, the sampler, the tray and the vials and to be eventually exhausted through the vent together with air coming from the fan duct.
Abstract: Described is a novel process for the preparation of penams and penems useful as antibacterial agents, which comprises the reaction of an appropriate f-substituted-azetidin-2-one with a base, followed by reaction of the thereby formed penam compound with an oxidating agent and an organic or inorganic base.Also described are novel pemam compounds useful as antibacterials which are prepared by the described process.