Abstract: A liposome formulation for stably incorporating high content of hydrophobic substance is disclosed. The liposome includes two phospholipids with different phase transition temperatures such as saturated and unsaturated phosphatidyl cholines, hydrophobic substances, cholesterol, cholesterol derivatives, antioxidant and hydrophilic polymer-modified lipids such as MPEG-DSPE.

Abstract: A method and a composition for the treatment of an Inflammatory Bowel Disease (IBD) or intestine polyposes is described. The method includes the local administration to the colon of a therapeutically effective amount of at least one Selective Serotonin Reuptake Inhibitor (SSRI) or at least one tricyclic antidepressant (TCA).

Abstract: Disclosed are compounds having Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, A, and B are as defined herein, for use in methods for treating, preventing or ameliorating hyperproliferative disorders, such as cancer and other diseases and conditions. The invention also relates to pharmaceutical compositions and formulations comprising a compound having Formula I, and in combination with one or more other active agents and/or treatments.

Abstract: The invention relates to polymeric nanoparticles and nanogels, which can contain, deliver, and/or release one or more active agents, such as biologically active molecules or fragrance molecules, and methods of preparing the polymeric nanoparticles and nanogels. The nanoparticles are crosslinked utilizing radiation (g-radiation) as the catalyst for free radical polymerization (see FIG. 1) rather than by toxic chemical means. The nanoparticles and nanogels can be modified, without limitation, with hydrophobic, hydrophilic, or ionic groups or moieties. or with enzymes. Methods of preparing nanoparticles and nanogels containing or encapsulating a variety of molecules, including biologically active molecules and fragrance molecules, are provided.

Abstract: The invention relates to the field of biochemistry, molecular biology, structural biology and medicine. More in particular, the invention relates to cross-? structures and the biological role of these cross-? structures. In one embodiment, the invention discloses a method for modulating extracellular protein degradation and/or protein clearance comprising modulating cross-?(beta) structure formation (and/or cross-? structure-mediated activity) of the protein present in the circulation.

Abstract: The present disclosure provides amide-based, non-nucleoside compounds having an inhibitory activity against endogenous polymerases, such as polymerase alpha and polymerase gamma. This disclosure further provides uses of treating hyperproliferative diseases or disorders, such as benign or malignant neoplasms, and more specifically cancers that are sensitive to inhibition of polymerase alpha and polymerase gamma.

Abstract: The present invention relates to pharmaceutical compositions comprising an analgesic agent and providing controlled release of the agent for improved treatment and prevention of pain and pain-related conditions, such as pain-related sleep disturbance. The present invention is particularly concerned with self-administered compositions.

Abstract: The present invention provides the diaminophenyladamantane derivatives with antitumor activities and the preparation method therefore. The method includes a step of reacting an aromatic diol with at least one 5-halo-2-nitrophenol in the presence of at least one inorganic base in an organic solvent with a relatively high boiling point.

Abstract: Sex steroid potentiated disorders including, prostate cancer and breast cancer, in a patient in need of treatment thereof, are treated with an amount of nitric oxide donating compound and/or nitrosoglutathione reductase inhibitor and/or cysteine binder different from that provided by nitric oxide donating compound effective to inhibit activation of steroid receptor. Variations include using only nitric oxide donating agent as treating agent; using only nitrosoglutathione reductase inhibitors as treating agent, using nitric oxide donating agent plus nitrosoglutathione reductase inhibiting agent; for prostate cancer treatment using prostate cancer drug modified to contain nitric oxide donating moiety or FDA approved nitric oxide donating agent and FDA approved prostate cancer treating agent. Also disclosed is an assay for assessing mutagenic potential of prostate cancer in a patient.

Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.

Abstract: Glutamate causes migration and proliferation of retinal pigment epithelium and/or glial cells, and glutamate antagonists can prevent, treat or reduce retinal pigment epithelium and/or glial migration and the subsequent development of proliferative vitreoretinopathy. Avoidance or management of proliferative vitreoretinopathy can be achieved by administering to the patient a compound capable of reducing glutamate-induced retinal cell migration in a concentration effective to reduce such migration.

Abstract: The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.

Abstract: The invention relates to amine compounds as well as methods and materials involved in modulating neurotransmitter reuptake. Specifically, the invention provides amine compounds, methods for synthesizing amine compounds, and methods for inhibiting neurotransmitter reuptake.

Abstract: Aminomethyl-phenyl-cyclohexanone derivatives of formula I or Ia, their diastereomers, enantiomers and salts formed with a physiologically tolerated acid. Also disclosed are processes for preparing the same, pharmaceutical compositions comprising the same, and methods of using the same for the treatment of pain, inflammatory reaction, allergic reactions, depression, drug abuse, alcohol abuse, gastritis, cardiovascular disease, respiratory tract disease, coughing, mental illness, epilepsy, urinary incontinence, itching, and diarrhoea.

Abstract: 2-Aminotetralines, a process for their preparation, and pharmaceutical compositions, for the prevention and therapeutic treatment of inflammatory pathologies (particularly septic shock) and/or autoimmune pathologies in which the aetiopathogenic role of inflammatory cytokines has been ascertained.

Abstract: The present invention is based on the discovery that nitric oxide (NO) is an important growth regulator in an intact developing organism. In particular, the present invention relates to a method of increasing in a mammal a population of hematopoietic stem cells which are capable of undergoing normal hematopoiesis, differentiation and maturation in hematopoietic tissue, wherein the hematopoietic tissue is contacted with at least one inhibitor of NO, such as one or more inhibitors of nitric oxide synthase (NOS), thereby producing hematopoietic tissue having an increased population of hematopoietic stem cells which are capable of undergoing normal hematopoiesis, differentiation and maturation. The present invention also relates to a method of increasing a population of cells in S phase in a tissue of a mammal, comprising contacting the tissue with an inhibitor (one or more) of NO, such as an inhibitor of NOS.

Abstract: The present invention includes the use of pelorol, related compounds and pharmaceutical compositions thereof as modulators of SHIP 1 activity. This invention also provides novel terpene compounds capable of modulating SHIP 1 activity and methods of synthesis thereof.

Abstract: Disclosed are thermally-stable, anthraquinone colorant compounds (dyes) which contain one or more vinyl groups which render the compounds copolymerizable with reactive vinyl monomers to produce colored, polymeric compositions such as acrylate and methacrylate polymeric materials. The compounds possess good fastness (stability) to ultraviolet (UV) light, good solubility in vinyl monomers, good color strength and excellent thermal stability. Also disclosed are (1) coating composition comprising (i) one or more polymerizable vinyl compounds, (ii) one or more of the dye compounds described above, and (iii) a photoinitiator and (2) polymeric materials, i.e., polymers derived from one or more acrylic acid esters, one or more methacrylic acid esters, one or more other polymerizable vinyl compounds or mixtures of any two or more thereof, having copolymerized therein one or more of the anthraquinone colorant compounds.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant inventive are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynecomastia, autoimmune disease, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer of the lung, colon, breast, uterus, and prrostate.

Abstract: Disclosed are thermally-stable, anthraquinone colorant compounds (dyes) which contain one or more vinyl groups which render the compounds copolymerizable with reactive vinyl monomers to produce colored, polymeric compositions such as acrylate and methacrylate polymeric materials. The compounds possess good fastness (stability) to ultraviolet (UV) light, good solubility in vinyl monomers, good color strength and excellent thermal stability. Also disclosed are (1) coating composition comprising (i) one or more polymerizable vinyl compounds, (ii) one or more of the dye compounds described above, and (iii) a photoinitiator and (2) polymeric materials, i.e., polymers derived from one or more acrylic acid esters, one or more methacrylic acid esters, one or more other polymerizable vinyl compounds or mixtures of any two or more thereof, having copolymerized therein one or more of the anthraquinone colorant compounds.

Abstract: We have now discovered that certain 9,10-anthraquinone derivatives we developed possess potent activity against O. perornata while possessing a sufficiently high level of solubility in water to make their activity against O. perornata viable. These compounds possess a high level of activity against O. perornata yet are relatively non-toxic to green algae and fishes. The compounds also possess a relatively short half-life. The compounds represent a new means to providing compounds possessing a high degree of selective activity against blue-green algae while being physiologically tolerated by catfish and green algae. The compounds provide a means for controlling blue-green algae in managed bodies of water that are destined for public use or consumption.

Abstract: Disclosed are thermally-stable, anthraquinone colorant compounds (dyes) which contain one or more vinyl groups which render the compounds copolymerizable with reactive vinyl monomers to produce colored, polymeric compositions such as acrylate and methacrylate polymeric materials. The compounds possess good fastness (stability) to ultraviolet (TV) light, good solubility in vinyl monomers, good color strength and excellent thermal stability. Also disclosed are (1) coating composition comprising (i) one or more polymerizable vinyl compounds, (ii) one or more of the dye compounds described above, and (iii) a photoinitiator and (2) polymeric materials, i.e., polymers derived from one or more acrylic acid esters, one or more methacrylic acid esters, one or more other polymerizable vinyl compounds or mixtures of any two or more thereof, having copolymerized therein one or more of the anthraquinone colorant compounds.

Abstract: The present invention is compositions and methods containing at least one perylenequinone, wherein the activated perylenequinone modulates the immune response. The compositions and methods of the present invention may also be used in combination with other administered immunotherapies. For example, the present invention may be used with antibody, antigen, cytokine, and/or immunoadjuvant based immunotherapies. In this embodiment of the invention, the compositions and methods modulate the function or activity of the immunotherapy itself.

Abstract: The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.

Abstract: Disclosed are compounds having one of the following structures: 1

Abstract: Substituted phenanthrene-9,10-diones in accord with structural diagram I, 1

Abstract: Topical compositions and methods for treating pain. The invention provides oil-in-water emulsions comprising an antidepressant; an NMDA-receptor antagonists; a lipophilic component; water; and a surfactant. The compositions induce a local-anesthetic effect when topically administered to intact skin thereby treating or preventing pain, for example, neuropathic pain.

Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.

Abstract: A hair dye composition containing at least one of the following compounds: or analogues thereof; and a method for dyeing hair which comprises a step of applying to the hair the hair dye composition is used. The dye composition of the invention exhibits excellent spreadability, applicability, level-dyeing property and shampoo resistance.

Abstract: The invention provides a use of a metalloproteinase inhibitor for the preparation of a pharmaceutical composition for treating human pulmonary emphysema which comprises admixing the metalloproteinase inhibitor in an amount effective to treat human pulmonary emphysema and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition which comprises a metalloproteinase inhibitor in an amount effective to treat human pulmonary emphysema and a pharmaceutically acceptable carrier.

Abstract: Glutamate causes migration and proliferation of retinal pigment epithelium and/or glial cells, and glutamate antagonists can prevent, treat or reduce retinal pigment epithelium and/or glial migration and the subsequent development of proliferative vitreoretinopathy. Avoidance or management of proliferative vitreoretinopathy can be achieved by administering to the patient a compound capable of reducing glutamate-induced retinal cell migration in a concentration effective to reduce such migration.

Abstract: The present invention pertains to methods for reducing the platelet activation state in an individual comprising administering a selective serotonin reuptake inhibitor (SSRI). The platelet activation state is reduced upon administering a SSRI, as measured by one or more platelet activation markers. The invention also relates to methods for treating or preventing an individual at risk for a vascular event, disease or disorder by administering a SSRI.

Abstract: Methods and compositions of tricyclic antidepressants for inducing local long-lasting anesthesia and analgesia are provided. The methods and compositions are useful for alleviating acute and chronic pain, particularly useful for treating a localized pain.

Abstract: The present invention relates to methods and compositions comprising a very low dose of cyclobenzaprine or metabolite thereof for preventing and treating sleep disturbances and illnesses manifested with sleep dysfunction including fibromyalgia syndrome, chronic fatigue syndrome, sleep disorders, psychogenic pain disorders or chronic pain syndromes or symptoms thereof. The present invention further relates to methods and compositions for treating sleep disturbances, chronic pain or fatigue in humans suffering from fibromyalgia syndrome, chronic fatigue syndrome, sleep disorders, psychogenic pain disorders, chronic pain syndromes using a very low dose of cyclobenzaprine.

Abstract: This invention provides novel fullerene derivatives, particularly fullerene derivatives that are water-soluble, that modulate the activity of nitric oxide synthase (NOS) and/or calmodulin. The invention provides methods for modulating NOS activity and particularly provides methods for inhibiting NOS activity, by contacting one or more fullerene derivatives of this invention with cells or tissue that exhibit NOS activity. In a specific embodiment, the invention provides water-soluble fullerene derivatives that are selective inhibitors of neuronal NOS or iNOS. Preferred water soluble fullerenes have substituents that contain one or more amine groups, amine cationic groups.

Abstract: A method of decreasing atherosclerosis and its complications involving administering to a human or animal various combinations of medications with Finasteride, Bicalutamide, Flutamide and Nilutamide.

Abstract: The invention is perylenequinones that are both sonosensitizers and photosensitizers, and their therapeutic use.

Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.

Abstract: Indane dimer compounds of general formula 5 or 6 are pharmaceutically useful, particularly to achieve smooth muscle relaxing activity and/or mast cell stabilizing activity and/or inflammatory activity. In formula 5 R1, R2 and R3to R15 and in formula 6 R1, R2 and R4 to R15, are selected from one or more of the same of different of: H, halo, hydroxy, alkoxy, aryloxy, acetoxy, carboxy, alkyl carbonyl, hydro carbonyl, amino, amido, alkylamino, hydroxylamino, sulphonic acid groups, sulphoxide groups, sulphone groups, C1-C10 alkyl or C3-C8 cycloalkyl groups. In formulae 5 and 6, X is O or NR, and the R in NR may be hydrogen, acyl, alkyl or sulphonate groups. In formulae 5 and 6 any one or more of R1, 1R1; R1, 1R2; R9, 1R9; R10, 1R10 and R14, 1R10 may together represent oxo.

Abstract: A compound selected from those of formula (I): wherein: denotes single bond or double bond, n is integer from 1 to 6 inclusive, R1, and R2 represent a group selected from hydrogen, linear or branched (C1-C6)-alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, X represents a group selected from —CH═CH—, oxygen, S(O)m wherein m is integer from 0 to 2 inclusive, and NR3 wherein R3 represents a group as defined in the description, Y represents CH or CH2 depending on whether denotes single bond or double bond, or may have the additional meaning of oxygen when X represents oxygen, T represents monocyclic or polycyclic (C3-C10)cycloalkyl optionally containing within the ring system oxygen, selenium, S(O)p, NR3, or SiR4R5 wherein p, R3, R4, and R5 are as defined in the description, its isomers and addition salts thereof with a pharmaceutically-accep

Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.

Abstract: The invention encompasses a compound having the formula: 1

Abstract: Competitive progesterone antagonists, including two novel steroids, viz., 11&bgr;,19-[4-(cyanophenyl)-o-phenylene]-17&bgr;-hydroxy-17&agr;-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one and 11&bgr;,19-[4-(3-pyridinyl)-o-phenylene]-17&bgr;-hydroxy-17&agr;-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one, inhibit formation of endometrial glands at below their ovulation inhibiting dose and the abortive dose, and thus achieve oral contraception in females without adversely affecting the menstrual cycle and without risk of aborting a previous implanted fertilized egg or a fetus.

Abstract: Glutamate causes migration and proliferation of retinal pigment epithelium and/or glial cells, and glutamate antagonists can prevent, treat or reduce retinal pigment epithelium and/or glial migration and the subsequent development of proliferative vitreoretinopathy. Avoidance or management of proliferative vitreoretinopathy can be achieved by administering to the patient a compound capable of reducing glutamate-induced retinal cell migration in a concentration effective to reduce such migration.

Abstract: Methods are provided for inhibiting stenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective dosage of a therapeutic conjugate containing a vascular smooth muscle binding protein that associates in a specific manner with a cell surface of the vascular smooth muscle cell, coupled to a therapeutic agent dosage form that inhibits a cellular activity of the muscle cell. Methods are also provided for the direct and/or targeted delivery of therapeutic agents to vascular smooth muscle cells that cause a dilation and fixation of the vascular lumen by inhibiting smooth muscle cell contraction, thereby constituting a biological stent.

Abstract: The present invention relates to methods and compositions comprising a very low dose of cyclobenzaprine or metabolite thereof for preventing and treating Generalized Anxiety Disorder. The present invention further relates to methods and compositions for treating and preventing symptoms associated with Generalized Anxiety Disorder using a very low dose of cyclobenzaprine.

Abstract: The invention provides a composition suitable for topical application comprising: an effective amount of a prostaglandin, a polymer thickener, a lipophilic component, and a buffer system. In another embodiment, the invention provides a composition suitable for topical application comprising: an effective amount of a vasoactive agent, a polymer thickener, a lipophilic component, and a buffer system. The invention also provides methods of ameliorating female sexual dysfunction. Also provided are methods of increasing female sexual arousal and methods of enhancing female sexual response.

Abstract: Composition of matter for application to a body surface or membrane to administer asimadoline by permeation through the body surface or membrane, the composition comprising asimadoline to be administered, at a therapeutically effective rate, alone or in combination with a permeation enhancer or mixture. Also disclosed are drug delivery devices and methods for the transdermal administration of asimadoline.

Abstract: A topical therapeutic preparation includes capsaicin which is an extract of peppers or chiles and which is a potent local pain killer. The ointment also includes a norepinephrine inhibitor and preferably a vasodilator which act to promote blood circulation in the treatment area and thereby promote healing of tissues in the treatment area. The ointment also preferably includes a local pain killer to offset the irritating effects of the capsaicin and a promoter of transcutaneous absorption.

Abstract: This invention relates to novel compounds, pharmaceutical compositions comprising these compounds and their use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).