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Nanocells allow the sequential delivery of two different therapeutic agents with different modes of action or different pharmacokinetics. A nanocell is formed by encapsulating a nanocore with a first agent inside a lipid vesicle containing a second agent. The agent in the outer lipid compartment is released first and may exert its effect before the agent in the nanocore is released. The nanocell delivery system may be formulated in pharmaceutical composition for delivery to patients suffering from diseases such as cancer, inflammatory diseases such as asthma, autoimmune diseases such as rheumatoid arthritis, infectious diseases, and neurological diseases such as epilepsy. In treating cancer, a traditional antineoplastic agent is contained in the outer lipid vesicle of the nanocell, and an antiangiogenic agent is loaded into the nanocore. This arrangement allows the antineoplastic agent to be released first and delivered to the tumor before the tumor's blood supply is cut off by the antianiogenic agent.

Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, which is useful as an anti-HIV agent. The present invention relates to a compound represented by the following formula [I] or [II] or a pharmaceutically acceptable salt thereof:wherein each symbol is as defined in the specification.

[Summary][Problem] Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, which is useful as an anti-HIV agent.[Solving Means] The present invention relates to a compound represented by the following formula [I] or [II] or a pharmaceutically acceptable salt thereof:wherein each symbol is as defined in the specification.

Medical devices and methods are designed to bias stretch receptors in the stomach wall of a patient to treat obesity. Biasing of the stretch receptors by pre-stretching induces an early sensation of satiety, causing the patient to consume less food. Biasing of the stretch receptors can be achieved by the placement of bulking devices within the wall of the stomach, e.g., in the mucosa, submucosa or muscle layer. The bulking devices may be expandable and, in some embodiments, may take the form of a hydrogel prosthesis that expands following implantation in a wall of the stomach.

Nanocells allow the sequential delivery of two different therapeutic agents with different modes of action or different pharmacokinetics. A nanocell is formed by encapsulating a nanocore with a first agent inside a lipid vesicle containing a second agent. The agent in the outer lipid compartment is released first and may exert its effect before the agent in the nanocore is released. The nanocell delivery system may be formulated in pharmaceutical composition for delivery to patients suffering from diseases such as cancer, inflammatory diseases such as asthma, autoimmune diseases such as rheumatoid arthritis, infectious diseases, and neurological diseases such as epilepsy. In treating cancer, a traditional antineoplastic agent is contained in the outer lipid vesicle of the nanocell, and an antiangiogenic agent is loaded into the nanocore. This arrangement allows the antineoplastic agent to be released first and delivered to the tumor before the tumor's blood supply is cut off by the antianiogenic agent.

Provided are: a compound represented by formula (I):(wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocyclic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, in which when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt thereof; an N-oxide form thereof; a solvate thereof, a prodrug thereof; and a medicament which includes those. The compound represented by formula (I) is capable of binding S1P receptors (in particular, EDG-1 and / or EDG-6), and useful for preventing and / or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc.

The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I]wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an agent for the prophylaxis or treatment of AIDS, or as an anti-HIV agent. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Becuae it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.

The present invention relates to method of sustained-delivery of an active drug to a posterior part of an eye of a mammal to treat or prevent a disease or condition affecting said mammal, wherein said disease or condition can be treated or prevented by the action of said active drug upon said posterior part of the eye, comprising administering an effective amount of an ester prodrug of the active drug subconjunctivally or periocularly. Preferably, the active drug is more than about 10 times as active as the prodrug. Other aspects of this invention deal with the treatment of certain diseases by the periocular or subconjunctival delivery of an ester prodrug, and certain pharmaceutical products containing ester prodrugs for periocular or subconjunctival administration.

A treatment of sweat glands in a target region of skin includes generating electromagnetic radiation having a wavelength of about 1,064 nm to about 1,800 nm. To decrease sweat production in a plurality of sweat glands, the electromagnetic radiation is delivered to a dermal interface defined by a dermal region and a subcutaneous fat region in the target region of skin to cause thermal injury to at least one of the dermal region, the subcutaneous fat region or the dermal interface. An epidermal region of the skin can be cooled at least one of before, during or after delivering the electromagnetic radiation to the dermal interface in the target region of skin.

The present disclosure provides conjugate structures (e.g., polypeptide conjugates) and hydrazinyl-indole compounds used to produce these conjugates. The disclosure also provides methods of production of such conjugates, as well as methods of using the same.

A method of reducing wrinkles in skin includes irradiating the skin with laser pulses to ablate an array of spaced apart voids in the skin. A region of coagulated tissue surrounds each of the voids and there viable tissue between the coagulated regions. Tissue in the coagulated regions is in tension due to shrinkage of collagen by the heat generated during the ablation. This tension rapidly closes the voids, tightening the skin and reducing the wrinkles. A healing process replaces the coagulated tissue with new tissue after a period of about one-month. The method is also applicable to lightening abnormally pigmented skin, as the new tissue replacing the coagulated tissue is not abnromally pigmented.

The sustained-release preparation of the present invention, which contains a dipeptidyl peptidase IV inhibitor and a hydrophilic polymer, can appropriately inhibit the DPP-IV activity, and is superior in convenience or compliance.

A method of treating ocular disorders involving angiogenesis includes the steps of providing a trans-scleral drug delivery device comprising an insert stabilizer for attachment to a scleral surface and having an interlock opening and a replaceable implant having a reservoir adjacent the scleral surface and an interlock tab, wherein said insert stabilizer and said replaceable implant are removeably connectable by mating said interlock tab and said interlock opening; providing an anti-angiogenic factor; introducing said anti-angiogenic factor into said reservoir; and attaching said insert stabilizer to the scleral surface. The reservoir can be refilled by disengaging the implant from the stabilizer, inserting a new dosage of anti-angiogenic factor, and reconnecting the implant to the stabilizer or injecting a new dosage of anti-angiogenic factor into the reservoir through an injection port in the stabilizer.

The invention discloses a diesel oil hydrogenation pour point depressing method. A series flow of hydrofining and hydrogenation pour point depressing is adopted in the method, wherein a hydrogenation pour point depressing catalyst is modified by metal auxiliary agent and silicon, effectively regulates the acidity and orifice shape of the inner surface and the outer surface of a shape-selective cracking molecular sieve, is favorable for dispersing wax molecules in a diesel oil raw material into pore canals of the molecular sieve to perform shape-selective cracking reaction, and has high catalytic activity and selectivity of a target product; and because the acidity of the outer surface of the molecular sieve is weak, side reactions such as secondary cracking and the like are reduced, the pour point depressing effect of the diesel oil is good, and the fraction yield of the diesel oil is high.

The invention relates to an aqueous liquid composition of calcium acetate, sweetener, and taste masking agent. Also provided is a method for binding phosphorus within the gastrointestinal tract of an individual by administering to the individual an aqueous solution of at least calcium acetate.

For the purpose of providing a GSK-3β inhibitor containing an oxadiazole compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3β-related pathology or disease, the present invention provides a GSK-3β inhibitor containing a compound represented by the formula (I):wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

The present invention provides combination therapies for treating a disease, disorder, or condition, and methods thereof.

Novel, advantageous oral compositions formulated to affect any one or combination of the following: reduce physical and mental fatigue, enhance activity, improve recovery from activity, promote muscle performance, increase energy substrates, contribute to improved antioxidant defenses (i.e., reduce oxidative stress or lipid peroxidation, conserve anti-oxidants in the sera), enhance mood, assist in preventing primary and secondary diseases associated with fatigue and muscle atrophy associated with inactivity, improve nervous system (i.e., neuronal) and musculoskeletal (i.e., increase skeletal muscle protein synthesis, increase satellite cells) health, and contribute to improvements in overall health. The compositions of the subject invention are preferably used as a replacement for a snack or meal in cases of hunger or fatigue for individuals across the broad spectrum of human function from elite athletes to those individuals compromised by aging and certain disease states.

A cancer test having prognostic utility in predicting time to disease progression, overall survival, and response to therapy in patients with MBC based upon the presence and number of CTC's. The Cell Spotter® System is used to enumerate CTC's in blood. The system immunomagnetically concentrates epithelial cells, fluorescently labels the cells and identifies and quantifies CTC's. The absolute number of CTC's detected in the peripheral blood tumor load is, in part, a factor in prediction of survival, time to progression, and response to therapy. The mean time to survival of patients depended upon a threshold number of 5 CTC's per 7.5 ml of blood. Detection of CTC's in metastatic cancer represents a novel prognostic factor in patients with metastatic cancers, suggests a biological role for the presence of tumor cells in the blood, and indicates that the detection of CTC's could be considered an appropriate surrogate marker for prospective therapeutic clinical trials.

Compositions containing an optionally surface-functionalized mesoporous support and a biologically active agent, and pharmaceutical compositions of the same, are provided herein. Such compositions can be useful in the treatment of tumors, for example, by injection of the composition at a location near the site of the tumor.

The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

Provided are cells containing exogenous antigen and uses thereof.

A conjugate between a target-seeking moiety and a modified superantigen, characterized in that the superantigen is a wild-type superantigen (SA I) in which an amino acid residue in a superantigen region (region I) determining binding to TCR, preferably TCRVβ, and T cell activation have been replaced by another amino acid residue while retaining the ability to activate a subset of T cells.In preferred embodiment the modified superantigen is a chimer between at least two wild-type superantigens (SA I, SA II etc) characterized in that one or more amino acid residues in a region determining binding to TCR and T cell activation have been interchanged between various wild-type superantigens.A therapeutic method making use of modified / chimeric superantigens as defined in the preceding paragraphs.An antibody preparation in which the cysteine residues that provide for interchain disulfide bonds have been mutated so as to forbid interchain disulfide bridges, preferably to serine residues, for use as pharmaceutical.

A method for synergistically treating a joint of an animal, including introducing a cushioning agent into a joint; and introducing an enzyme or hormone adapted to stimulate cartilage production into the joint. The joint may be subjected to a compression regimen following injection of the cushioning agent and enzyme / hormone. Alternatively, the invention may include a composition for synergistically treating a joint of an animal, comprising a viscous cushioning material adapted to be introduced within a joint space to provide cushioning for the joint, and hormones dispersed through the cushioning material, the hormones operable to increase cartilage production.

The invention discloses a composite solid polymer electrolyte and a preparing method and application thereof. The composite solid polymer electrolyte is prepared from a gadoleic acid ester monomer, a porous supporting matrix, lithium salt, an additive and an initiator, wherein the mass ratio of the gadoleic acid ester monomer to the additive is (1-10):1, the lithium salt accounts for 5-30% of the total mass of the gadoleic acid ester monomer and the additive, and the mass ratio of the initiator to the gadoleic acid ester monomer is (1-10):100. The composite solid polymer electrolyte prepared with the method has the advantages of being large in ion conductivity, high in mechanical strength, easy to form, stable in interface contact, high in electrochemical stability and easy to prepare and can be used for forming solid lithium ion secondary batteries, and the prepared solid lithium ion secondary batteries are high in safety, energy density and production efficiency.

An improved Transdermal Delivery System (TDS) comprising a backing layer inert to the components of the matrix, a selfadhesive matrix containing an amine-functional drug and a protective foil or sheet to be removed prior to use, characterized in that the self-adhesive matrix consists of a solid or semi-solid semi-permeable polymer (1) wherein an amine functional drug in its free base form has been incorporated, (2) which is saturated with the amine functional drug and contains said drug as a multitude of microreservoirs within the matrix, (3) which is highly permeable for the free base of the amine functional drug, (4) which is impermeable for the protonated form of the amine functional drug, (5) wherein the maximum diameter of the microreservoirs is less than the thickness of the matrix. is provided. Said TDS provides for enhanced flux of the amine functional drug across the TDS / skin interface.

The invention discloses a biodegradable linear random copolyester, its preparation method and uses, wherein the copolyester has a structural unit of (1), wherein m is an integer of 2-10, n is an integer of 0-8, p is an integer of 2-10, m, n, p are identical or different, x is an integer of 1-10, y is an integer of 1-10, the average molecular weight Mw of the copolyester is 100,000-600,000g / mol, its molecular weight distribution is 1.2-3, which is measured through GPC method. The copolyester can be widely applied into section bar, film, fabric and coating.