Abstract: The invention relates to novel histidine derivatives corresponding to the general formula (I) below: in which: R denotes a linear or branched, saturated or unsaturated alkyl radical containing from 6 to 22 carbon atoms, n is an integer ranging from 1 to 16, Q+ represents H+ or an organic or inorganic cation, and the addition salts with an acid. The invention also relates to a process for preparing the compounds of formula (I), as well as to the use of these compounds in cosmetics and pharmacy.

Abstract: The present invention provides a method for preventing or treating a human immunodeficiency virus (HIV) infection, including a new or an asymptomatic infection as well as AIDS, comprising administering to a mammal in need thereof a HIV infection preventing or treating effective amount of a &ggr;-L-glutamnyl-L-cysteine ester compound of formula (I): wherein R is a straight chain, branched or cyclic hydrocarbon group having 1-10 carbon atoms, or a straight chain or branched hydrocarbon group having 1-5 carbon atoms substituted with an aromatic group; or the oxidized dimer obtained by dehydrogenation between two &ggr;-L-glutamyl-L-cysteine esters having formula (I).

Abstract: The present invention provides formulations that prevent loss and damage of PEG-interferon alpha conjugates during and following lyophilization. The formulations of the present invention protect PEG-interferon alpha conjugates from loss and degradation during the lyophilization process, as well as degradation during subsequent storage. The formulations of the present invention are suitable for protection of PEG-interferon alpha conjugates from various types of degradation, including, but not limited to loss of biological activity and changes in the degree and/or nature of conjugation. A preferred PEG-interferon alpha conjugate protectable in the formulations of the present invention is an interferon alpha-2b-polyethylene glycol (12,000) conjugate.

Abstract: This invention is directed to the (L)-tartaric acid salt of 2-amino-N-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-[3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo{4,3-c}pyridin-5-yl]-ethyl]-2-methyl-propionamide which is a growth hormone secretagogue and as such is useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compound. The (L)-tartaric acid salt of the compound of this invention is useful in the treatment and/or prevention of osteoporosis, insulin resistance and other conditions or diseases associated with growth hormone deficiency. The (L)-tartaric acid salt of the compound of the present invention is also useful in treating osteoporosis when used in combination with: a bisphosphonate compound; estrogen, Premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin.

Abstract: The present invention relates to the preparation of polyol/thickened oil suspensions containing a biologically active agent, for the sustained delivery of the biologically active agent. The described protein/glycerol/oil suspensions show sustained release of protein, e.g., G-CSF, of up to at least one week.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: The present invention provides compositions containing corticosteroid compounds as active agents for the treatment of ailments and diseases of the respiratory tract, particularly the lungs, by way of nasal and pulmonary administration. The corticosteroid compounds are present in a dissolved state in the compositions. The compositions can be formulated in a concentrated, essentially non-aqueous form for storage or in a diluted, aqueous-based form for ready delivery. In a preferred embodiment, the corticosteroid composition contains an ethoxylated derivative of vitamin E and/or a polyethylene glycol fatty acid ester as the high-HLB surfactant present in the formulation. The compositions are ideally suited for inhaled delivery with a nebulizer or for nasal delivery.

Abstract: Novel functional sodium chloride compositions containing sodium gluconate as a substitute for the conventionally employed sodium chloride and being efficacious in preventing hypertension and the onset of complications thereof in the brain, heart, kidney; etc. These compositions are prepared by adding 40 to 400 parts by weight of sodium gluconate to 100 parts by weight of compositions containing 40 to 60% by weight of sodium chloride and 60 to 40% by weight of potassium chloride. These compositions are usable as a table salt for seasoning foods or in imparting the required saltiness to foods such as crackers or snacks. They are particularly appropriate for those who should cut down on the amount of salt in the diet.

Abstract: A chewable calcium composition and its associated method of manufacturing are disclosed. The chewable composition includes a lipid base and a micronized calcium salt substantially uniformly mixed with the lipid base such that the lipid base forms a continuous phase. The composition provides for a relatively large dose of calcium in a easy to take chocolate like, chewable form. The composition of the present invention is manufactured by providing the lipid base including a melting temperature. The lipid base is then heated to a temperature of approximately 120° F. such that the lipid base melts. After the lipid base melts, the micronized calcium salt is mixed with the lipid base to form a melted mixture such that the micronized calcium salt is substantially uniformly distributed in the melted lipid base.

Abstract: The present invention discloses the use, in the manufacture of a preventive and therapeutic drug of a brain disease, of a compound represented by formula (1): CH2═CH—CH2—S(O)n—R  (1) [wherein R represents a hydrogen atom, an alkyl group, an alkenyl group, a substituted alkyl group, a substituted alkenyl group, an alkylthio group, an alkenylthio group, a phenyl group, a substituted phenyl group, a heterocyclic group, or a group derived from an amino acid or an oligopeptide by deletion of one hydrogen atom, and which group may have a protective group; and n is 0, 1, or 2], a glycoside thereof, or a salt of the compound or the glycoside. The drug of the present invention for ameliorating brain diseases, inhibiting reduction of brain neurons and promoting branching of neurites, is useful for the prevention and treatment of brain diseases such as dementia in association with degeneration and sloughing of brain neurons.

Abstract: The present invention comprises homeopathic preparations of purified growth hormone, as well as methods and systems for delivery of such preparations and treatment of disorders and conditions by administering such preparations.

Abstract: A liquid phase process for preparing GnRH peptide analogs of the formula: G-AA1-(A)D-Phe-AA3-AA4-(R2-AA5-AA6-AA7-AA8-Pro-AA10-NH2   Formula 1 which comprises: (a) reacting a peptide of the formula: T-(R2)AA5-AA6-X  where T is (P2) AA4 orP2 and X is AA7-OH or is —OH, with a peptide of the formula: X′-AA8-Pro-AA10-NH2  or acid-addition salt form thereof, where X′ is AA7 when X is absent and X′ is absent when X is AA7-OH;  in a liquid reaction medium in the presence of a peptide coupling reagent and a strong organic amine base to obtain a product of the formula: T-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2 (b) removing the P2 protecting group at the N-terminus, and (c) reacting the product of step (b) or an acid addition salt thereof, with a peptide of the formula: G-AA1-(R1)D-Phe-AA3-T′  or acid-addition salt form thereof, where T′ is AA4-OH when T is absent and is absent when T is P2-AA4, in a liquid reaction medium to obtain a GnRH pepti

Abstract: The present invention relates to the use of a TNF Receptor together with a steroid hormone to produce a pharmaceutical composition for the treatment of lethal bacterial and viral infections as well as autoimmune and inflammatory diseases. It also relates to said pharmaceutical compositions for the simultaneous, separate or sequential use of its active ingredients for the above specified treatment. In particular, it relates to the use of TBP-1 together with dehydroepiandrosterone (DHEA) or its metabolites to produce a pharmaceutical composition for the treatment of septic shock.

Abstract: The invention relates to peptide conjugates comprising a sequence of at least 3 amino acids derived from a thymic hormone selected amongst thymuline and thymopoietine, the amino acids being independently in the form D, L or DL, said sequence being chemically or physically conjugated with at least one compound selected amongst monocarboxylic acids having the general formula (I): HOOC—R, as well as alcohol, aldehyde or amide derivatives, the dicarboxylic acids having the general formula (II): HOOC—R1—COOH. The invention also relates to the use of such conjugates as medicaments, and pharmaceutical or cosmetological compositions containing them.

Abstract: A pharmaceutical and/or veterinary formulation comprising deslorelin and an excipient, the formulation being characterised in that, in vitro, it releases deslorelin into phosphate buffered saline, as hereinbefore described, at 37° C. at a rate of about 2-80 &mgr;g/day for at least 200 days. The formulation may be used for prevention of reproductive function, particularly in dogs and cats, and for the treatment, particularly in humans, of prostate and breast cancer and other diseases and conditions where suppression of testosterone or estradiol levels is beneficial.

Abstract: Modulating agents comprising cyclic peptides, and compositions comprising such modulating agents are provided. The cyclic peptides comprise a cadherin cell adhesion recognition sequence HAV. Methods for using such peptides and compositions for modulating and/or directing neurite outgrowth in a variety of contexts are also provided.

Abstract: A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (R)-trihexyphenidyl. The method comprises administering a therapeutically effective amount of enantiomerically enriched (R)-trihexyphenidyl, or a pharmaceutically acceptable salt thereof, substantially free of the (S)-trihexyphenidyl enantiomer. Pharmaceutical compositions for the treatment of urinary incontinence comprising enantiomerically enriched (R)-trihexyphenidyl, or a pharmaceutically acceptable salt thereof, and an acceptable carrier are also disclosed.

Abstract: A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (R, R)-glycopyrrolate. The method comprises administering a therapeutically effective amount of enantiomerically enriched (R, R)-glycopyrrolate, or a pharmaceutically acceptable salt thereof, substantially free of the (S, S)-glycopyrrolate enantiomer. Pharmaceutical compositions for the treament of urinary incontinence comprising enantiomerically enriched (R, R)-glycopyrrolate, or a pharmaceutically acceptable salt thereof, and an acceptable carrier are also disclosed.

Abstract: The present invention broadly relates to chemical modification of biologically active proteins or analogs thereof. More specifically, the present invention describes novel methods for site-specific chemical modification of various proteins, and resultant compositions having improved biocompatibility and bioactivity.

Abstract: The present invention relates to a relaxin analogs and derivatives, and uses thereof. The present invention further relates to compositions comprising a relaxin analogs and derivatives, and relaxin wherein such composition exhibits an additive or synergistic effect.