Abstract: Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.

Abstract: A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g.

Abstract: Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.

Abstract: A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g.

Abstract: The present invention provides compositions and methods for noninvasive delivery of therapeutic agents across an intact tympanic membrane. For example, the compositions include a penetration enhancer which increases the flux of a therapeutic agent (e.g., antibiotic) across the tympanic membrane. Such compositions are particularly useful in the treatment of otitis media. Additionally, the composition may include a sustained release agents that, in some embodiments form sustained release reservoirs, in situ, once administered to a patient.

Abstract: The present invention disclosed compound 2-methyl-5-imino-benzo[d][1,3]oxazin[5-b]pyrazole and preparation method and uses thereof. The compound 2-methyl-5-imino-benzo[d][1,3]oxazin[5-b]pyrazole of the present invention has the following structure of formula (II), wherein the compound or pharmaceutically acceptable salts thereof can be used for preparing the drugs for treatment or prevention of cardiovascular diseases.

Abstract: The present invention relates to a granular pharmaceutical composition comprising a drug having a disagreeable taste, a wax and a sugar alcohol; a method for preparing the same; and a pharmaceutical product for oral administration, comprising the granular composition. The product excellently masks a disagreeable taste possessed by a drug and provides good sensation upon oral administration, and therefore is easily ingested by even the elderly, children, and patients suffering dysphagia. Moreover, the product is suitable for administration using tube.

Abstract: The present invention is directed towards methods of inhibiting thermo- and chemo-sensing in insects and pests by inhibiting TRPA1 ion gated channel or family members. The present invention is also directed towards methods of insect control by modulating the TRPA1 ion gated channel or family members. The methods are applicable to a wide variety of insects and pests including agricultural and horticultural pests.

Abstract: The present invention disclosed compound 2-methyl-5-imino-benzo[d][1,3]oxazin[5-b]pyrazole and preparation method and uses thereof. The compound 2-methyl-5-imino-benzo[d][1,3]oxazin[5-b]pyrazole of the present invention has the following structure of formula (II), wherein the compound or pharmaceutically acceptable salts thereof can be used for preparing the drugs for treatment or prevention of cardiovascular diseases.

Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)-group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.

Abstract: The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens.

Abstract: A medicament for the treatment of the phantom phenomena of acute tinnitus and/or phantom pain, a method for the production of such a medicament, and a method for the treatment of such phantom phenomena

Abstract: Substituted fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) with a —CH(—R2)— group in the fused ring at the 2-position of the imidazo ring and a —CH(—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.

Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R is hydrogen or C1-4 alkyl; R1 is hydrogen, C1-4 alkyl, C(O)OH, C(O)NH2 or (C1-4 alkylene)R10; R2 and R3 are independently hydrogen, C1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C1-4 alkyl, C1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C1-4 alkylene) R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2 or C(O)OH; n is 0, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.

Abstract: The present invention provides mTOR inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods of making the compounds and intermediates thereof; and methods of using the compounds.

Abstract: The invention encompasses series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

Abstract: The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R0, R1, R2, R3, R4 and a are defined herein.

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R0, R1, R2, R3, R4 and a are defined herein.

Abstract: Compounds of a compound of compound of general formula (I) wherein X1, X2, A, R1R2, R3 and R4 are as defined herein; are useful as anti-mycobacterial agents, especially agents for the treatment of tuberculosis.

Abstract: Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.

Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.

Abstract: The present invention relates to new tricyclic triazolic compounds having a high affinity for sigma-1 receptor as well as to the process for the preparation thereof, to composition comprising them and to their use as medicaments according to compounds of formula (I), Wherein R1 and R2 are as defined in the description.

Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.

Abstract: The invention relates to modulators of peripheral 5-HT receptors, particularly 5-HT4 receptors, said modulators essentially selective for peripheral 5-HT receptors over receptors of the central nervous system. The invention allows for the treatment, amongst others, of gastrointestinal disorders, lower urinary tract disorders, and cardiovascular disorders without side effects related to CNS activity.

Abstract: The subject application provides small compounds that are able to suppress autophagy in various cells. These compounds are useful in augmenting the existing treatments of various cancers and microbial/parasitic infections. Thus, the subject application also provides methods of treating various types of cancers and microbial/parasitic infections. Also provided by the subject application are methods of suppressing the expansion of autophagosomes within cells or individuals and inhibiting the lipidation of autophagy-related protein 8 (Atg8).

Abstract: Compounds of formula (I): prodrug derivatives and/or pharmaceutically acceptable salt thereof, selectively inhibit the enzyme kynurenine aminotransferase, thereby reducing the synthesis of kynurenic acid. The compounds are used for the treatment of psychiatric and neurological diseases which benefit from an increase in glutamatergic and/or cholinergic neurotransmission, such as schizophrenia, depression, bipolar illness, anxiety and Alzheimer's disease. Furthermore, the compounds of the invention are useful for stimulating attention, memory and other cognitive processes in normal individuals of any age, including children, adolescents and the elderly. Additionally, the compounds of the invention are also useful for treatment of patients suffering from malaria by preventing parasite gametogenesis and fertility based on reduction of xanthurenic acid formation from its bioprecursor 3-hydroxy kynurenine.

Abstract: The invention relates to combinations of A) oxazolidinones of formula (I) and B) other active ingredients, to a method for producing said combinations and to the use thereof as medicaments, in particular for the treatment and/or prophylaxis of thrombo-embolic diseases.

Abstract: Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing or one or more diseases or disorders of the eye, and methods of making and using thereof, are described. The microsphere compositions release an effective amount of the one or more active agents for a period greater than 14 days in vivo, preferably greater than 60 days in vivo, more preferably up to 73 days in vivo, more preferably greater than 90 days in vivo, even more preferably over 100 days in vivo, and most preferably greater than 107 days in vivo. In a preferred embodiment, the microparticle compositions contain one or more active agents useful for managing elevated intraocular pressure (TOP) in the eye. In one embodiment, the microspheres are formed from polylactide-co-glycolide (“PLGA”); in another embodiment, the microspheres are formed from a blend PLGA and poly lactic acid (“PLA”).

Abstract: A composition for oral cavity and skin which contains an antibacterial agent and does not have adverse side effects due to steroids, is provided. The composition contains 0.01 to 4.5% by mass of at least one selected from the group consisting of an antibacterial agent, an antiviral agent, an anti-HIV agent, a non-nucleic acid-based reverse transcriptase inhibitor, an anticancer agent for external use and a disinfectant; 0.01 to 4.5% by mass of a non-steroidal anti-inflammatory agent; 0.001 to 4.5% by mass of a steroidal anti-inflammatory agent; and 0.001 to 10% by mass of a highly water-absorbent polymer or a cellulose derivative.

Abstract: This invention relates to a pesticidal compositions containing at least one pyrrolizidine alkaloid compound derived from a plant and endophyte combination, and applying the pesticidal compositions to another plant without pesticidal protection, where upon application of the composition, the plant confers pest protection. The pyrrolizidine alkaloid compound is of Formula wherein: R?H or CH3 and R??H, CH3, CHO, COCH3.

Abstract: Provided herein are aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK-3 inhibitors mediated diseases.

Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.

Abstract: An orthopedic implant suitable for insertion into the body of a subject, the implant comprising: a metal substrate having one or more surfaces operable to contact a bone tissue or soft tissue when implanted into the subject; a coating comprising a resorbable polymer impregnated with an admixture of a rifamycin antibiotic and a second antibiotic selected from the group consisting of tetracyclines, penicillin, ampicillin, cefazolin, clindamycin, erythromycin, levofloxacin, or vancomycin. The adhered coating layer present on the one or more surfaces is capable of releasing the rifamycin and second antibiotics in an antimicrobially effective amount. Method for making an antibiotic coated implant by mixing a resorbable polymer mixture with an antibiotic solution forming a coating solution, applying the coating solution to a surface of the implant and evaporating the solvent from the coated layer.

Abstract: A formulation is provided that includes a volume of an aqueous multivalent physiological ion solution compatible with cerebrospinal fluid containing at least one divalent cation of magnesium or calcium, and at least one anion of carbonate or phosphate, and having a pH between 6.5 and 8.0. A zwitterionic therapeutic agent other than baclofen is dissolved the solution to achieve higher concentration or ease of solution and/or storage relative to therapeutic saline solutions of the same agent. A process of delivering a zwitterionic therapeutic agent into a subject is provided that includes dissolving a therapeutic amount of the zwitterionic therapeutic agent in a volume of artificial cerebrospinal fluid to form a stable formulation. The solution is then administered to the subject using an intrathecal pump.

Abstract: A process for treating a patient with leukemia or an aplastic anemia having cells with inclusions that stain with anti-E. canis antibodies or antibodies to other Ehrlichia or Anaplasma is disclosed. That process comprises administering to the patient (i) an antibacterial amount of a rifamycin, (ii) an antibacterial amount of a quinolone, or a mixture of (i) and (ii).

Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: The invention relates to tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivative having the general Formula (I) wherein X is CH2, O or S; R represents 1-3 substituents independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy and halogen; R1 is (C5-8)cycloalkyl; R2 is H or (C1-4)alkyl; R3, R3?, R4? R4?, R5, R5? and R6? are independently hydrogen or (C1-4)-alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; R6 is hydrogen or (C1-4)alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; or R6 forms together with R7 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; R7 forms together with R6 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; or R7 is H, (C1-4)alkyl or (C3-5)cycloalkyl, the alkyl groups being optionally substituted with OH, halogen or (C1-4)alkyloxy; or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.

Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.

Abstract: The present invention provides an agent for preventing or treating a trastuzumab-resistant cancer, which contains one or more medicaments selected from a cofilin inhibitor, a PAK1 inhibitor, a LIMK inhibitor, a RHO inhibitor, a ROCK1 inhibitor and a ROCK2 inhibitor.

Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract: The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.

Abstract: The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.

Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.

Abstract: Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described.

Abstract: The present invention relates to the use of a Compound of formula I preferably 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid or a pharmaceutically acceptable salt thereof for the preparation of a medicament for use in the treatment of biofilm formation, e.g. of P. aeruginosa, e.g. in cystic fibrosis patients.

Abstract: The invention relates to the use of at least one compound of the formula (I), in which R and R3 are particularly a hydrogen atom, R1 is particularly a hydrogen atom or a methyl, ethyl or isobutyl mi group, R4, R5, R6 and R7 are independently a hydrogen atony, an alkoxyl group with 1 to 7 carbon atoms or a halogen atom, R2 is a hydrogen atom, an O? group or an OH group, B is an N-GP1 or NRc, group, GP1 being a Boc or Cbz group, and Rc is a hydrogen atom or a methyl or t-butyl group, for preparing a drug for treating conditions associated with bacterial infections, in particular for treating bacterial diseases.

Abstract: The invention relates to a transdermal therapeutic system which comprises a back layer that is impermeable to the active substance, and a peelable protective layer that is impermeable to the active substance and at least one matrix layer consisting of polysiloxanes and/or polysiloxane derivatives and containing micro-reservoirs. Said micro-reservoirs contain at least one ion pair from a pharmacologically active substance and an additive and either the active substance is nucleophilic and the additive is electrophilic or the active substance is electrophilic and the additive is nucleophilic.