Abstract: The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGFR kinase inhibitor and an IGF1R inhibitor compound of Formula I combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an EGFR kinase inhibitor and IGF1R inhibitor compound of Formula I combination with a pharmaceutically acceptable carrier. The IGF1R inhibitor is represented by Formula I: wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein.

Abstract: A coating formed of a substituted polycaprolactone and method of making and using the same are disclosed.

Abstract: A waterless composition suitable for delivery of an active agent to a body surface or cavity includes a vehicle having about 70% to about 99% by weight of a hydrophilic polar solvent, said hydrophilic solvent selected from the group consisting of (i) a mixture of two or more different polyethylene glycols (PEGs), wherein at least one PEG is a high molecular weight PEG having a melting point greater than 25° C.; and (ii) propylene glycol (PG); about 0% to about 10% of at least one surface active agent; about 0% to about 5% of a polymeric agent; about 0% to about 30% of a secondary hydrophilic solvent; and about 0% to about 5% of a silicone oil; and about 3% to about 25% hydrophobic propellant. The composition is otherwise substantially free of a hydrophobic solvent and includes at least one of a surface active agent and a polymeric agent. The vehicle and the propellant are sufficiently miscible that the components may be homogeneously distributed with mild shaking.

Abstract: A drug delivery device for placement in the eye includes a drug core comprising a hydrophobic pharmaceutically active agent, and a holder that holds the drug core. The holder is made of a material impermeable to passage of the active agent and includes an opening for passage of the pharmaceutically agent therethrough to eye tissue. The device includes polyurethane-siloxane-containing copolymers crosslinked with hydrophilic monomers.

Abstract: Novel estrogenic compounds of Formula I are provided. wherein the bond represented by the wavy line may be a single or double bond such that when the wavy line is a single bond, R1 is selected from the group consisting of hydrogen, sulfate and glucoronate or other esters, and when the wavy line is a double bond, R1 does not exist; R2 is lower alkyl; R3 may be selected from the group consisting of hydrogen, sulfate, or glucuronide or other esters; and R4 through R13 may independently be selected from the group consisting of hydrogen, hydroxy, ketone, lower alkyl, lower alkoxy, halogen, and carbonyl groups and R14 is selected from the group consisting of hydrogen, sulfate and glucoronide and other esters. When R1 is hydroxy, the hydroxy or ester substituent may have either an ? or a ? orientation. Compositions of matter including compounds of the present invention are also provided as are methods of treating mammals in need of treatment using compounds of the present invention.

Abstract: Kits for treating or preventing chronic obstructive pulmonary disease (COPD) by using as active agent a non-glucorticoid steroid, analogue thereof, such as dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEA-S), or their salts, in an amount effective for preventing or treating COPD.

Abstract: Disclosed herein are methods of using metaxalone. In one embodiment, the method comprises determining that a patient in need metaxalone therapy is taking a substance that is a n inhibitor or an inducer of a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4, and adjusting administration to the patient of metaxalone or the substance to avoid an adverse event associated with metaxalone. In another embodiment, the method comprises informing a user that metaxalone ais metabolized by a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4. Also included are articles of manufacture comprising a container containing a dosage form of metaxalone, wherein the container is associated with published material informing that metaxalone affects activity of a cytochrome p450 isozyme. Also disclosed are a method of treatment and a method of manufacturing a metaxalone product.

Abstract: A hormone replacement therapy formulation and method comprising selective estrogenic compounds which preferentially stimulate the estrogen receptor alpha over the estrogen receptor beta.

Abstract: A method for treating or preventing chronic obstructive pulmonary disease (COPD) by using as active agent a non-glucorticoid steroid, analogue thereof, such as dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEA-S), or their salts, in an amount effective for preventing or treating COPD.

Abstract: The invention relates to a novel sustained release pharmaceutical formulation adapted for administration by injection containing the compound 7?-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17?-diol, more particularly to a formulation adapted for administration by injection containing the compound 7?-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17?-diol in solution in a ricinoleate vehicle which additionally comprises at least one alcohol and a non-aqueous ester solvent which is miscible in the ricinoleate vehicle.

Abstract: Methods for treating a vascular disease by delivering therapeutic compositions with enhanced endothelium targeting are disclosed.

Abstract: A scleral lens is provided with a drug that is retained in the reservoir of fluid between the scleral lens and the cornea. This system can be used to deliver drugs not currently used because of poor bioavailability, to increase bioavailability of drugs used in patients already wearing a scleral lens, and to improve bioavailability in patients who are not currently wearing the lens. Dosing can be provided less frequently, thus decreasing the risk of non-compliance.

Abstract: A scleral lens is provided with a drug that is retained in the reservoir of fluid between the scleral lens and the cornea. This system can be used to deliver drugs not currently used because of poor bioavailability, to increase bioavailability of drugs used in patients already wearing a scleral lens, and to improve bioavailability in patients who are not currently wearing the lens. Dosing can be provided less frequently, thus decreasing the risk of non-compliance.

Abstract: The present disclosure provides methods for preventing or treating illness, improving responsiveness to immunization, and improving the efficacy of gene therapy in a patient by disrupting sex steroid signalling in the patient, wherein the bone marrow and other immune cell functionality is improved without, prior to, or concurrently with, thymic regeneration. In some embodiments, sex steroid signalling is interrupted or ablated in the patient by the administration of LHRH agonists, LHRH antagonists, anti-LHRH receptor antibodies, anti-LHRH vaccines, anti-androgens, anti-estrogens, selective estrogen receptor modulators (SERMs), selective androgen receptor modulators (SARMs), selective progesterone response modulators (SPRMs), ERDs, aromatase inhibitors, or various combinations thereof.

Abstract: Provided are nanoparticles prepared by the aggregation of cucurbituril derivatives and having a particle size of 1 to 1,000 nm, a pharmaceutical composition in which a pharmaceutically active substance is loaded into the nanoparticles, and preparation methods thereof.

Abstract: A pharmaceutical or veterinary composition, comprises a first active agent selected from a dehydroepiandrosterone and/or dehydroepiandrosterone-sulfate, or a salt thereof, and a second active agent comprising an anticholinergic bronchodilator for the treatment of asthma, chronic obstructive pulmonary disease, or other respiratory diseases. The composition is provided in various formulations and in the form of a kit. The products of this patent are applied to the prophylaxis and treatment of asthma, chronic obstructive pulmonary disease, or other respiratory diseases.

Abstract: The present invention relates to methods and compositions that control, i.e., antagonize/inhibit or agonize/stimulate, de novo glucocorticoid production in the skin. Such methods and compositions can be used for the prevention and/or treatment of a variety of skin conditions, including inflammation, acute wounds, chronic non-healing wounds, keloid, fibrotic or hypertrophic scars, and epithelial-derived cancer.

Abstract: A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.

Abstract: A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.

Abstract: A method of improving cumulative embryo score may comprise administering an androgen to a human female for at least about four consecutive months followed by harvesting and fertilizing oocytes and forming embryos. A method of increasing the quantity of fertilized oocytes in one cycle of in vitro fertilization may comprise administering an androgen to a human female for at least about four consecutive months, harvesting and fertilizing the oocytes. A method of normalizing ovarian DHEA may include administering an androgen for at least about four consecutive months. A method of decreasing the time to pregnancy and increasing the rate of pregnancy by administering an androgen for at least about two months. A method of decreasing miscarriage rates may comprise administering an androgen for at least about two months to a female. Moreover, a method of decreasing aneuploidy rates in human embryos may comprise administering an androgen to a female for at least about two months.

Abstract: The present invention relates to the treatment of patients suffering from pulmonary diseases, in particular from chronic obstructive pulmonary disease (COPD), bronchial asthma, cystic fibrosis and chronic cough in particular as caused by ACE-Inhibitors using megestrol acetate.

Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of a selective cytokine inhibitory drug alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of a selective cytokine inhibitory drug. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: Disclosed herein are substituted cyclohexanone-based NMDA receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to compositions for treating prepubertal males of adolescent age with insufficient testosterone production using a hydroalcoholic testosterone gel formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of treating said adolescent males.

Abstract: Compositions and methods for reducing the body weight of a subject are disclosed. The invention is directed to methods for reducing the body weight in a subject comprising administering therapeutically effective amounts of a fatty acid ester of an estrogen or estrogen derivative in an oil. Furthermore the invention is directed to compositions for reducing the body weight in a subject comprising administering therapeutically effective amounts of a fatty acid ester of an estrogen or estrogen derivative in an oil.

Abstract: Compositions comprise a fluoroquinolone having Formulae I-VIII for treating, reducing, ameliorating, or preventing infections caused by some bacteria that are resistant to an antibacterial drug. Methods for treating, reducing, ameliorating, or preventing such infections use such compositions.

Abstract: The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17?-hydroxy steroid dehydro-genase type 1.

Abstract: The present invention is directed to compounds of formula (I): wherein R1 represents C4-C7 branched chain alkyl, C3-C8 cycloalkyl optionally substituted by one or more groups independently selected from C1-C3 alkyl and methoxy, C4-C6 cycloalkylmethyl wherein the methyl group is optionally substituted by a group selected from methyl or ethyl, or a bicycloalkyl group optionally substituted by one or more methyl groups; R2 represents hydrogen, a methyl group, which may be in either the a or D configuration, or a methylene group; R3 and R4 are the same or a different group and each independently represents hydrogen, halogen or a methyl group; and represents a single or a double bond; physiologically acceptable solvates thereof, pharmaceutical compositions thereof, methods of treatment using such compounds, and processes for preparing such compounds.

Abstract: Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.

Abstract: A method of producing microparticles having a median diameter up to 100 ?m and the microparticles so produced are described. The method includes the steps of providing a solvent having a bioactive dispersed or dissolved therein and a vehicle dissolved therein, carrying out an emulsification in a non-solvent phase to produce an emulsion containing the bioactive and the vehicle in a solvent phase, and evaporating the solvent to leave the microparticles, wherein a mixture of at least two surfactants is employed to stabilize the emulsion and wherein the mixture has a hydrophilic-lipophilic balance (HLB) of up to 8.

Abstract: The subject invention relates in part to the oral administration of ecdysteroids for controlling subterranean termites. Preferred ecdysteroids for use according to the subject invention are ecdysone, certain ecdysone analogs, and 20-hydroxyecdysone, for example. In some preferred embodiments, one or more of these compounds is used in a termite bait in combination with one or more chitin synthesis inhibitors (CSI), such as hexaflumuron and/or noviflumuron. The subject invention also relates to mixtures comprising these two active ingredients. The ecdysteroid analog or molt-accelerating compound (MAC) typically induces a preliminary molting event in termite workers, which then allows the CSI to further disrupt the molt and cause mortality. The combination of these active ingredients, causing accelerated molting together with inhibition of chitin synthesis, is surprisingly shown herein to enhance activity against termites, as compared to either group of compounds alone.

Abstract: The invention provides combination therapy, wherein one or more other therapeutic agents are administered with indibulin or a pharmaceutically acceptable salt thereof and the combination is synergistic. Another aspect of the invention relates to the treatment of cancer with indibulin as a single agent. Another aspect of the invention relates to dosing regimen for administration of oral dosage forms of indibulin.

Abstract: Methods for treating ocular conditions by inserting an implant comprising an active agent into an ocular site of a patient thereby obtaining an amelioration of a symptom of the ocular condition (i.e. a therapeutic effect) for an extended period of time during which a therapeutic amount or a detectable amount of the active agent is not present at the ocular site.

Abstract: Solid or semi-solid intraocular implant compositions are disclosed. The compositions contain a lipophilic compound but lack a polymeric ingredient.

Abstract: The compounds of the present invention can be used to inhibit formation of beta-amyloid protein. The present invention provides methods of preventing, delaying onset of, or treating diseases or conditions characterized or mediated by amyloidosis. In particular, the present invention is useful for preventing, delaying onset of, and treating Alzheimer's disease and related diseases causing dementia.

Abstract: Stabilized dispersions are provided for the delivery of a bioactive agent. The dispersions preferably comprise a plurality of perforated microstructures dispersed in a suspension medium that typically comprises a liquid fluorochemical. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as by settling or flocculation. In particularly preferred embodiments the stabilized dispersions may be directly administered to the lung of a patient using an endotracheal tube or bronchoscope.

Abstract: The present invention relates to the use of pregnanes in inducing analgesia, preferably without overt sedation, in a mammal in response to neuropathic pain, and compositions and kits therefore.

Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of cytopathic diseases. Cytopathic diseases may be caused by a variety means such as viral infections like HIV and AIDS, or the development of neoplasms in a mammalian subject. The methods and compositions of the invention are effective for inhibiting de novo HIV infections upregulating viral expression from latent provirus, inhibiting HIV-induced cytopathic effects, down regulating the HIV receptor, increasing Th1 cytokine expression, decreasing Th2 cytokine expression, increasing ERK phosphorylation, inducing apoptosis in malignant cells, inducing remission, maintaining remission, as chemotherapeutic agents, as well as for decreasing symptoms of cytopathic diseases and opportunistic infections that may accompany such diseases.

Abstract: The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21 and R22 are individually and independently selected from the group comprising H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, alkoxyl, substituted alkoxyl, aryloxy, substituted aryloxy, arylalkyloxy, substituted arylalkyloxy, acyloxy, substituted acyloxy, halogen, hydroxyl, nitro, cyano, acyl, substituted acyl, mercapto, alkylthio, substituted alkylthio, amino, substituted amino, alkylamino, substituted alkylamino, bisalkyl amino, substituted bisalkyl amino, cyclic amino, substituted cyclic amino, carbamoyl (—CONH2), substituted carbamoyl, carboxyl

Abstract: The invention relates to new steroids nitrooxyderivatives, to topical pharmaceutical formulations thereof, and their use for treating skin or mucosal membrane diseases or disorders. These new steroids nitrooxyderivatives have an improved pharmacological activity and enhanced local tolerability.

Abstract: The present invention pertains to a method for treating cancer, such as lung cancer, multiple myeloma, lymphoma, and epithelial ovarian cancer, comprising the administration to a patient in need thereof a first amount or dose of a histone deacetylase (HDAC) inhibitor, such as PXD-101, and a second amount or dose of another chemotherapeutic agent, such as dexamethasone or 5-fluorouracil, or an epidermal growth factor receptor (EGFR) inhibitor, such as TarcevaÚ, wherein the first and second amounts or doses together comprise a therapeutically effective amount.

Abstract: A system and compositions including zotarolimus and paclitaxel are disclosed, as well as methods of delivery, wherein the drugs have effects that complement each other. Medical devices are disclosed which include supporting structures that include at least one pharmaceutically acceptable carrier or excipient, which carrier or excipient can include one or more therapeutic agents or substances, with the carrier including at least one coating on the surface thereof, and the coating associated with the therapeutic substances, such as, for example, drugs. Supporting structures for the medical devices that are suitable for use in this invention include, but are not limited to, coronary stents, peripheral stents, catheters, arterio-venous grafts, by-pass grafts, and drug delivery balloons used in the vasculature.

Abstract: The pharmaceutical preparation for treating endometriosis contains at least 28, preferably 30, daily dose units, each of which contain dienogest, cyproterone acetate, or chlormadinone acetate at a daily dose that is at most twice that required to inhibit ovulation together with one or more pharmaceutical aids and/or carriers. The daily dose units are administered in a method of prophylaxis and/or therapy of endometriosis continuously during a time interval of at least 169 days or 25 weeks, preferably more than two years. The method effectively reduces endometriosis and associated pain, while undesirable side effects including bone density decrease are reduced or eliminated.

Abstract: The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of formula I as well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for prophylaxis and/or therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17?-hydroxy steroid dehydrogenase type 1.

Abstract: The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a P2X7 receptor antagonist, and a second active ingredient which is a corticosteroid, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.

Abstract: The present invention relates to a waterless composition and foam as a vehicle in which an active pharmaceutical or cosmetic agent, when added is stable or stabilized by or its destabilization is impeded by the presence of a modulating agent. The pharmaceutical or cosmetic composition and foam, includes: a waterless solvent, a modulating agent and one or more active pharmaceutical or cosmetic agents. The present invention also relates to a method of treatment administering the waterless composition and foam.

Abstract: This invention relates to the preparation and use of anti-cancer compounds/formulation containing cucurbitacins. Said formulation comprises active ingredients, particularly cucurbitacin B and cucurbitacin D, with the efficacy of anti-proliferation and inducing cellular apoptosis. Said formulation owns the anticancer activity. This invention also provides a method of isolating and purifying the active ingredients in lab-scale and in industrial-scale.

Abstract: An effective formulation for the treatment and prevention of pseudofolliculitis barbae, commonly called razor bumps, and the skin irritation associated with the condition. The treat formulation can be used as the last step in a multi-step shaving system consisting of a shaving gel, aftershave balm and the aforementioned treat. The treat can also be used as a standalone product and is formulated to treat and prevent shaving symptoms day and night.

Abstract: Methods of treating, preventing and/or managing myelodysplastic syndromes are disclosed. Specific methods encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active ingredient, and/or the transplantation of blood or cells. Specific second active ingredients are capable of affecting or blood cell production. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.