Abstract: Compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, and are as defined herein, their use as antiinflammatory, immunosuppressive, and antiallergic agents, pharmaceutical compositions comprising them, and methods for their preparation comprising irradiating compounds of formula II ##STR2## under an inert atmosphere, in the presence or absence of a compound of formula R.sub.3 --S--S(O).sub.m --R.sub.8, where R.sub.7, R.sub.8, and m are as defined herein, and methods for their preparation comprising oxidizing, reducing, halogenating, or alkylating compounds of formula I are disclosed.

Abstract: An inhaler for powdered medicament in capsules has a swirling chamber which can be opened to allow access of a closed capsule into the swirling chamber for operation of capsule-opening means in the swirling chamber. Access to the swirling chamber is gained by a pivoting cover member (22) which is provided with interlock means associated with the capsule-opening means to ensure that the capsule opening means cannot be operated while the cover member is in its open position to allow access of the user's finger to the region (28) of the swirling chamber (26,28) where the capsule-opening pins (30) could damage the user's finger. A further embodiment of an inhaler has a removable capsule reservoir having a container portion (74) with a closure (76) removable to reveal the interior of said reservoir and closable to define one entire side face of said reservoir, the closure member (76) being hinged to the container portion at thin film hinge (78).

Abstract: This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.

Abstract: Compounds of formula (I): ##STR1## wherein R is a polyfluoroalkoxy or polyfluoroalkyl radical and R.sub.1 is a hydrogen atom and R.sub.2 is a hydroxyl radical, or R.sub.1 is a hydroxyl radical and R.sub.2 is a hydrogen atom, salts thereof, the preparation of said compounds, and drugs containing same.

Abstract: A transgenic rabbit expressing a protein capable of interfering with dyslipoproteinaemia-related diseases, a method of preparing the same, and its use as an animal model, are disclosed. Specifically, a transgenic rabbit expressing high levels of Apo-AI, is disclosed.

Abstract: A method for preparing streptogramins of the formula (I): ##STR1## wherein R.sub.1 is methyl or ethyl, R.sub.2 is H and X and Y together form an oxo radical, or R.sub.1 is ethyl, R.sub.2 and X are H and Y is H or OH, or else R.sub.1 is ethyl, R.sub.2 is OH and X and Y together form an oxo radical, by demethylation of a synergistin derivative of the formula (II): ##STR2## wherein R.sub.1, R.sub.2, X and Y are as defined above, by means of a treatment with a periodate in an acetic medium, followed by a treatment in an aqueous medium.

Abstract: A novel method for preparing vectors derived from adeno-associated viruses (AAV), cells used therefor, and the use of the resulting vectors, particularly in gene and/or cell therapy, are disclosed.

Abstract: The compounds of formula (I) ##STR1## wherein R, R.sub.1 and R.sub.2 are defined in the disclosure, and salts thereof.The compounds of formula (I) are non-competitive N-methyl-D-asparate (NMDA) receptor antagonists, particularly NMDA receptor glycine modulation site ligands, and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, this receptor is also known as the quisqualate receptor.

Abstract: Streptogramine derivatives of general formula (I) below, wherein the radical R.sub.1 is a methyl or ethyl radical, the radical R.sub.2 is a bromine or chlorine atom, or is an alkenyl radical with 3 to 5 carbon atoms when R.sub.3 and R.sub.4 are methyl, and one of R.sub.3 and R.sub.4 is a hydrogen atom or a methyl radical and the other is a methyl radical are disclosed. The streptogramine derivatives of general formula (I) have particularly useful antibacterial properties, and may be used in combination with a pristinamycin II derivative.

Abstract: Simplified methods to produce recombinant adeno-associated virus (rAAV) vectors are described. The methods involve the use of chimeric plasmids which incorporate the Epstein Barr nuclear antigen (EBNA) gene, the latent origin of replication of Epstein Barr virus (oriP), and a rAAV genome. The chimeric plasmids themselves are also a part of the present invention. These plasmids are maintained as multicopy extra-chromosomal elements in cells, such as human 293 cells. Permanent cell lines carrying these EBV/AAV plasmids are induced to produce large amounts of rAAV upon addition of wild-type, adeno-associated virus helper functions. Vectors produced in this manner are capable of transducing exogenous genes into other human cell lines and exhibit the attributes of viral elements produced by conventional methods.

Abstract: The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-?N-?N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl!-(L)-aspartyl!-(L)-.beta. -cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula ##STR1## wherein: A, B, Z, E.sup.1, E.sup.2, G, R, m, n, and p are as defined herein.

Abstract: The invention relates to a process for the preparation of intermediates useful in the preparation of (1R,2R)-2-(3-pyridyl)-N-alkyltetrahydro-2H-thiopyran-2-carbothioamide 1-oxides, which possess useful pharmaceutical properties, for example antihypertensive properties, and to intermediates and pharmaceutical products prepared using said process.

Abstract: This invention relates to taxoids of the formula (I): a method for preparing these taxoids, and pharmaceutical compositions containing them. In formula (I), R is alkyl radical (1-6 carbon atoms), alkenyl (2-6 carbon atoms), alkynyl (2-6 carbon atoms), cycloalkyl (3-6 carbon atoms), cycloalkenyl (4-6 carbon atoms), phenyl, unsaturated heterocyclyl containing from 5 to 6 links, Z is a hydrogen atom or a radical of formula (II): ##STR1## wherein R.sub.1 is an optionally substituted benzoyl radical, thenoyl radical, furoyl radical, or a radical R.sub.2 --O--CO-- in which R.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl, and R.sub.3 is an alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, naphthyl or aromatic heterocyclic radical. The taxoids of formula (I) in which Z is a radical of formula (II) have remarkable antitumoral and antileukemic properties.

Abstract: Compounds of formula (I): ##STR1## wherein R.sub.3 and R.sub.4, taken together with the carbon atom to which they are attached, form (a) a 2- or 3-pyrrolidine ring, a 2- or 4-piperidine ring or a 2-azacycloheptane ring, said rings being optionally substituted at the nitrogen atom by an alkyl, --CHO, --COOR.sub.11, --CO--alk--COOR.sub.6, --CO--alk--NR.sub.6 R.sub.12, --CO--alk--CONR.sub.6 R.sub.8, --CO--COOR.sub.6, --CO--CH.sub.2 --O--CH.sub.2 --COOR.sub.6, --CO--CH.sub.2 --S--CH.sub.2 --COOR.sub.6, --CO--CH.dbd.CH--COOR.sub.6, CO--alk, --CO--Ar", --CO--alk--Ar", --CO--NH--Ar", --CO--NH--alk--Ar", --CO--Het, --CO--alk--Het, --CO--NH--Het, --CO--NH--alk--Het, --CO--NH.sub.2, --CO--NH--alk, --CO--N(alk)alk', --CS--NH.sub.2, --CS--NH--alk, --CS--NH--Ar", --CS--NH--Het, --alk--Het, --alk--NR.sub.6 R.sub.8, --alk--COOR.sub.6, --alk--CO--NR.sub.6 R.sub.8, --alk--Ar", --SO.sub.2 --alk or --SO.sub.

Abstract: Nanoparticles are prepared by dissolving a poly(ethylene oxide) and/or poly(propylene oxide) polylactic copolymer in an organic solvent followed by formation of nanoparticles by mixing the solution containing the polymer with an aqueous solution and by precipitation, without using an additional colloidal protective agent or by microfluidization and solvent evaporation. Nanoparticles prepared by this method are disclosed.

Abstract: Compounds of formula (1) ##STR1## wherein either R is C.dbd.R.sub.3, C(R.sub.4)R.sub.5 or CH--R.sub.6, R.sub.1 and R.sub.2 are hydrogen, halogen, alkyl, alkoxy, amino, acylamino, --NH--CO--NH--Ar, --N.dbd.CH--N(alk)alk', nitro, cyano, phenyl, imidazolyl or SO.sub.3 H, R.sub.3 is oxygen, NOH, NO-alk-COOK or CH--R.sub.7, R.sub.4 is alkyl, -alk-Het or alk-Ar, R.sub.5 is alkyl, -alk-Het or -alk-Ar, or C(R.sub.4)R.sub.5 is cycloalkyl, R.sub.6 is hydroxy, alkyl, NR.sub.8 R.sub.9, -alk-OH, -alk-NR.sub.8 R.sub.9, -alk-Ar or -alk-Het, R.sub.7 is hydroxy, alkyl, phenyl, -alk-Ar, -alk-Het, NR.sub.10 R.sub.11 or a heterocyclic ring, R.sub.8 and R.sub.9 are alkyl, or R.sub.8 is hydrogen and R.sub.9 is hydrogen or alkyl, --COR.sub.12, --CSR.sub.30 or --SO.sub.2 R.sub.13, R.sub.10 and R.sub.11 are alkyl or cycloalkyl, R.sub.12 is alkyl, cycloalkyl, phenyl, --COO-alk, --CH.sub.2 --COOX, --CH.sub.2 NH.sub.2, --NH-alk, --NH--Ar, --NH.sub.2 or --NH-Het, R.sub.13 is alkyl or phenyl, R.sub.30 is --NH-alk, --NH--Ar, --NH.sub.

Abstract: The invention provides new compositions containing taxane derivatives, consisting of solutions of such derivatives in a solvent mixture composed of ethanol and polysorbate. These compositions are used to prepare perfusions.

Abstract: A process is described for the preparation of a compound of formula (I) or a stereoisomeric compound thereof, in which the 1,2-position is saturated or is a double bond; X.sup.1 and X.sup.2 are each independently hydrogen or halogen; R.sup.1 is hydrogen or acyl; R.sup.2 is hydroxyl, acyloxy or oxo; and R.sup.3 is alkyl, by reacting a compound of formula (II) with an aldehyde R.sup.3 CHO in either phosphoric acid or about 60% to about 75% w/w sulphuric acid. Compounds of formula (I) are either pharmacologically active steroids or are intermediates in the synthesis of pharmacologically active steroids.

Abstract: This invention relates to a process for the preparation of 7-hydroxy taxanes of general formula (I) from 7-trialkylsilyl taxanes of general formula (II), wherein R.sub.1 is hydrogen, alkoxy, acyloxy, or alkoxyacetoxy, and Z is a hydrogen atom or a radical of general formula (III), wherein R.sub.2 is an optionally substituted benzyl radical or an R'.sub.2 --O--CO-- radical wherein R'.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical, R.sub.3 is an aromatic alkyl, alkenyl, alkynyl, cycloalyl, phenyl, naphthyl or heterocyclyl radical and either R.sub.4 is a hydrogen atom and R.sub.5 is a hydroxyl function protecting group, or R.sub.4 and R.sub.5 together form a saturated 5- or 6-membered heterocylic ring. In general formula (II), each R, which are the same or different, is an alkyl radical optionally substituted by a phenyl radical.

Abstract: The invention is directed to a novel compound of formula ##STR1## in which R is a hydroxyl, alkyloxy, phenylalkyloxy or --NH--CH.sub.2 --COOH radical, R' and R" are identical and are each a hydroxy or methoxy radical and R'" represents a hydrogen, bromine, chlorine or iodine atom or a nitro radical. The invention is also directed to the salts of said compounds and their use.