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.

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: 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: 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: 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 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.

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.

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.

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.

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.

Abstract: The invention discloses 4-substituted androstendione derivatives of the following formula (I) ##STR1## wherein R is amino or substituted amino or azido,one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, alkyl, alkenyl or alkynyl, and(x) and (y) are each, independently, a single bond or a double bond.The compounds of formula (I) are useful aromatase inhibitors.

Abstract: Anthracycline glycosides of the general formula (A'): ##STR1## wherein R.sub.1 represents a hydrogen atom, a hydroxy group or a methoxy group; one of R.sub.2 and R.sub.3 represents a hydroxy group and the other of R.sub.2 and R.sub.3 represents a nitro group; and R.sub.4 represents a hydrogen atom or a hydroxy group; and their pharmaceutically acceptable salts; have anti-tumor activity.

Abstract: A method is disclosed for purifying non-homogeneous systems, known as liposomic suspensions, from non-entrapped drugs wherein said suspensions are treated with liquid or solid polymers of synthetic and organic nature having chemical functionality, which are used as ion-exchangers. The liquid or solid polymers are based on styrene, divinylbenzene, acrylic acid, methacrylic acid, and the like, normally known as ion-exchange resins, and may include carboxylic, phosphonic or sulphonic functions of different matrices. The ion-exchange resins may also include salified quaternary ammonium, primary, secondary and tertiary amminic or phosphinic functions or other functions with different matrices, including phenolformaldehyde, styrene-divinylbenzene, acrylates, methacrylates, hydrocarbons and condensation-resins.

Abstract: Ergoline derivatives of the formula I ##STR1## wherein R.sub.1 =H,CH.sub.3 ; R.sub.2 =H, halogen, CH.sub.3, CN, C.sub.1 -C.sub.4 alkylthio or phenylthio; R.sub.3 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.4 =H, OCH.sub.3 ; R.sub.5 =H and R.sub.6 =--CH.dbd.CH--CONHR.sub.7 or R.sub.5 and R.sub.6 =.dbd.CH--CONHR.sub.7 ; R.sub.7 =2-thiazolyl, 3-pyridazinyl, 1,3,4-thiadiazol-2-yl or 4-pyrimidinyl group optionally substituted, and pharmaceutically acceptable salts thereof, display activity on the Central Nervous System and are useful as antiprolactinic agents. Their preparation and pharmaceutical compositions containing them are also described.

Abstract: Distamycin A derivatives of formula ##STR1## wherein 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; andeach group R.sub.1 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl, and the pharmaceutically acceptable salts thereof.The compounds are useful as antiviral or antitumor agents.

Abstract: The present invention relates to new 4-aza-17.beta.-substituted 5.alpha.-androstan-3-ones, to a process for their preparation, to pharmacological compostions containing them, and to the use of said compounds as inhibitors of androgen action by means of testosterone 5-reductase inhibition.

Abstract: Antibacterial compounds of formula (I) ##STR1## wherein, R.sub.1 ' is alkyl or hydroxyalkyl;R.sub.2 is hydrogen or a carboxy protecting group; andY' is a group-S-heterocyclic or pyridyl, which group may be substituted, and pharmaceutically or veterinarily acceptable salts thereof and pharmaceutical compositions containing the same.

Abstract: A process for preparing compounds of the formula I ##STR1## wherein either (i) each of R.sub.1 and R.sub.2 independently represents H or an organic group, or (ii) NR.sub.1 R.sub.2 is a heterocyclic ring or (iii) R.sub.2 is H and R.sub.1 is ##STR2## wherein each of R.sub.6 and R.sub.7 independently represents H or an organic group, m is 1 or 2, n is 0-3, X is O, S, NH, NR.sub.8, CHNO.sub.2 or CHSO.sub.2 R.sub.4 wherein R.sub.8 and R.sub.4 are organic groups and R.sub.3 represents an organic group is characterized by the following reaction sequence: ##STR3## There are also provided new compounds of the formula I wherein n is 0 and m is 2 and pharmaceutical compositions containing them. These compounds and their pharmaceutically acceptable acid addition salts are active as anti-ulcer agents.