Abstract: There is disclosed a compound of Formula (I): and any pharmaceutically acceptable salt or zwitterion thereof; wherein: R is hydrogen, methyl or ethyl; R1 is hydrogen or C1-C2 alkoxy; R2 is methyl or a C2-C4 group which may be saturated or unsaturated, branched or linear; and R3, R4, R5 and R6 each are independently selected from hydrogen, hydroxyl, halogen, methyl optionally substituted with hydroxy, methoxy, ethoxy, and a saturated or unsaturated C2-C3 that may be optionally substituted with hydroxyl, with the provisos that: (i) at least two of R4, R5, R6 and R7 must be hydrogen, and (ii) R3, R4, R5 and R6 may be selected such that an adjacent pair thereof join to form a ring having at least 5 members. The compound of Formula (I) is believed useful in treating a disease or disorder in a subject which may be alleviated by a 5HT2A agonist (e.g.

Abstract: The present invention provides a tryptamine prodrug compound. A compound represented by the formula (I) where each symbol is as described in the specification, or a salt or zwitterion thereof, is converted to an active which has 5HT2A receptor agonist activity, and is useful as an agent for the treatment of depression.

Abstract: Methods and systems for preventing or reducing side effects of testosterone replacement therapy (TRT) by administering a testosterone formulation multiple times per day are disclosed. The methods of the present invention enable men who cannot tolerate previous TRT regimens, e.g. because they wish to attempt to conceive or are at risk of developing cardiovascular side effects, to receive TRT treatment.

Abstract: The present invention provides a tryptamine prodrug compound. A compound represented by the formula (I) where each symbol is as described in the specification, or a salt or zwitterion thereof, is converted to an active which has 5HT2A receptor agonist activity, and is useful as an agent for the treatment of depression.

Abstract: The present invention provides a tryptamine prodrug compound. A compound represented by the formula (I) where each symbol is as described in the specification, or a salt or zwitterion thereof, is converted to an active which has 5HT2A receptor agonist activity, and is useful as an agent for the treatment of depression.

Abstract: The present invention contemplates novel neurosteroid derivative compounds, such as derivatives of ganaxolone and allopregnanolone, having improved solubility and bioavailability. The novel neurosteroid derivative compounds are characterized by the following formulas: wherein R1 is methyl or hydrogen, R2 is an ester function (R—C(O)O—), R3 is hydrogen, R4 is alpha or beta hydrogen, R5 is R—CO— or any hydrocarbon structure (R—), and wherein R (in R2 or R5) is independently selected from any structure comprising 10 carbon atoms or fewer, which is linear or branched, saturated or unsaturated, may comprise cyclic or aromatic functions within the structure, and wherein R contains no more than 1 OH or NR2, or 2 ether or thioether functions.

Abstract: Compositions and methods are presently disclosed that provide improved efficiacy for the treatment of cancer. In particular, 3-O-ribose monoester derivatives of adenosine triphosphate are observed to have vastly superior efficiacy over a previously reported compound, 3,5 benzoylbenzoyl adenosine triphosphate. These novel compounds have been shown to increase calcium channel activation mediated by the P2X7 receptor thereby resulting in increase apoptosis of cancer cells, either malignant or benign.

Abstract: The present invention relates to new compounds and compositions comprising active ingredient derivatives of testosterone, and novel testosterone derivatives, novel testosterone methods, novel testosterone compositions, novel testosterone articles of manufacture of pharmaceutical preparations and novel testosterone therapeutic uses thereof.

Abstract: A nasally administered cannabinoid semi-solid or viscous liquid composition; nasal methods for administering the nasal pharmaceutical compositions; methods for manufacturing the nasal pharmaceutical compositions; and nasal methods of treating diseases treatable by the nasal pharmaceutical compositions formulated with a cannabinoid or mixtures thereof.

Abstract: The present invention contemplates novel neurosteroid derivative compounds, such as derivatives of ganaxolone and allopregnanolone, having improved solubility and bioavailability. The novel neurosteroid derivative compounds are characterized by the following formulas: wherein R1 is methyl or hydrogen, R2 is an ester function (R—C(O)O—), R3 is hydrogen, R4 is alpha or beta hydrogen, R5 is R—CO— or any hydrocarbon structure (R—), and wherein R (in R2 or R5) is independently selected from any structure comprising 10 carbon atoms or fewer, which is linear or branched, saturated or unsaturated, may comprise cyclic or aromatic functions within the structure, and wherein R contains no more than 1 OH or NR2, or 2 ether or thioether functions.

Abstract: Methods and systems for preventing or reducing side effects of testosterone replacement therapy (TRT) by administering a testosterone formulation multiple times per day are disclosed. The methods of the present invention enable men who cannot tolerate previous TRT regimens, e.g. because they wish to attempt to conceive or are at risk of developing cardiovascular side effects, to receive TRT treatment.

Abstract: A nasally administered cannabinoid semi-solid or viscous liquid composition; nasal methods for administering the nasal pharmaceutical compositions; methods for manufacturing the nasal pharmaceutical compositions; and nasal methods of treating diseases treatable by the nasal pharmaceutical compositions formulated with a cannabinoid or mixtures thereof.

Abstract: An aqueous suspension, stable in physiological medium, of nanoparticles for delivering active principles such as insulin. The delivery particles are based on a three-block copolymer: polyethylene glycol/hydrophilic polyaminoacid/hydrophobic polyaminoacid. These three-block copolymers can be associated with an active principle without denaturing it, and perform a controlled and long-term release of the active principle in vivo, and thus provide the active principle with a very prolonged release. Also disclosed is a powder form solid from which are derived the delivery particles, the preparation of the powder-form solid, a suspension of delivery particles based on the three-block copolymer, and pharmaceutical specialties obtainable from the delivery particles filled with active principle.

Abstract: The invention relates to injectable long-acting insulin formulations for the treatment of type I and II diabetes in humans and animals. The main objective of the invention is to provide a long-acting insulin formulation in the form of a colloidal suspension: which allows easy filling of a syringe through a small diameter needle (for example with the gauge 29 G, 30 G or 31 G) and/or which can be easily injected through a small diameter needle (for example with the gauge 29 G, 30 G or 31 G), without damaging the therapeutic efficacy of the insulin. To achieve this objective, the subject of the invention is an aqueous and stable colloidal formulation of nanoparticles of at least one poly(Leu-block-Glu), loaded with insulin, in which the pH is such that: 6.0?pH?7.

Abstract: The invention concerns a suspension of biocompatible particles for carrying active principles. Said carrier particles are based on a double-block hydrophilic neutral polyaminoacid/hydrophobic neutral polyaminoacid copolymer. Said hydrophilic neutral polyaminoacid/hydrophobic neutral polyaminoacid particles are capable of combining in colloidal suspension in non-dissolved state, at least an active principle and of releasing same, in particular in vivo, in prolonged and/or delayed delivery. The invention also concerns a powdery solid from which are derived the carrier particles and the preparation of said solid and of said suspension of active principle based on hydrophilic neutral polyaminoacids/hydrophobic neutral polyaminoacids. Said carrier particles form spontaneously and in the absence of surfactants or organic solvents, stable aqueous suspensions.

Abstract: A suspension of vector particles (PV) based on polyamino acids and have a mean hydrodynamic diameter between 30 and 120 nm, and an insulin load factor of from 5 to 25% of associated insulin volume relative to the polyamino acid volume forming the vector particles. The polyamino acids are double-block polymers containing hydrophilic and hydrophobic monomers. The suspension may be prepared by copolymerizing N-carboxy anhydrides of hydrophobic monomers and precursors of hydrophilic monomers, in the presence of N-methyl pyrrolidone and methanol. The copolymer is optionally neutralized, subjected to dialysis, concentrated and water is eliminated to produce a solid powder, which can be suspended in a liquid to produce the colloidal suspension. Active principles such as insulin or vaccines are associated with the carrier particles to prepare special pharmaceutical products.

Abstract: A suspension of biocompatible particles based on a double-block hydrophilic neutral polyminoacid/hydrophobic neutral polyaminoacid copolymer and suitable for carrying active principles. The carrier particles can combine in colloidal suspension in a non-dissolved state with an active principle and release same, particularly in vivo, in prolonged and/or delayed delivery. The carrier particles may be derived from a powdery solid, and spontaneously form stable aqueous suspensions in the absence of surfactants or organic solvents. The invention also concerns the carrier particles in dry form, the method of preparing them, and pharmaceutical compositions (in dry form or suspension) which include the carrier particles associated with an active principle.

Abstract: The present invention is directed to a suspension of particles for delivering active principles, in particular proteins. Said particles are based on a diblock copolymer consisting of a neutral hydrophobic alpha hydroxy carboxylic acid polymer block and a hydrophilic linear polyaminoacid block with peptide alpha chaining, at least partly ionized. Said alpha hydroxy carboxylic acid polymer/linear polyaminoacid delivery particles spontaneously obtainable in the absence of surfactant can be stable. Said delivery particles are capable of being associated undissolved in colloidal suspension with at least an active principle and of delayed or prolonged release thereof. The invention is also directed to a powdery solid from which are derived the delivery particles and the preparation of said solid and said delivery particle suspension.

Abstract: A suspension of vector particles (PV) based on polyamino acids and have a mean hydrodynamic diameter between 30 and 120 nm, and an insulin load factor of from 5 to 25% of associated insulin volume relative to the polyamino acid volume forming the vector particles. The polyamino acids are double-block polymers containing hydrophilic and hydrophobic monomers. The suspension may be prepared by copolymerizing N-carboxy anhydrides of hydrophobic monomers and precursors of hydrophilic monomers, in the presence of N-methyl pyrrolidone and methanol. The copolymer is optionally neutralized, subjected to dialysis, concentrated and water is eliminated to produce a solid powder, which can be suspended in a liquid to produce the colloidal suspension. Active principles such as insulin or vaccines are associated with the carrier particles to prepare special pharmaceutical products.

Abstract: The invention relates to novel collagen peptides that are modified by grafting free or substitued thiol functions carried by mercaptoamine radicals. The aim of the invention is to provide thiol collagens that can be cross-linked in a sufficient and controlled manner by forming S—S bridges and which are biocompatible. This is achieved by means of the inventive thiol collagens which are characterized in that the mercaptoamine radicals are identical to or different from each other and are exclusively grafted on the aspartic and glutamic acids of the collagen chain by amide bonds. The invention also relates to a method for the production of said thiol and cross-linkable collagens. The novel modified cross-linkable and/or cross-linked collagens can be used as biomaterials.