Abstract: A series of tricyclic benzimidazole derivatives, in particular dihydro-1H-imidazo [1,2-a]benzimidazole, dihydro-1H-pyrrolo [1,2-a]benzimidazole, dihydro-1H-pyrazino[1,2-a]benzimidazole, dihydro-1H-[1,4]oxazino[4,3-a]benzimidazole and dihydrothiazolo[3,4-a]benzimidazolem, and analogs thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 -associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.

Abstract: The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Abstract: Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleanine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.

Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.

Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.

Abstract: The present invention is a photochromic material formed of a biimidazole compound represented by general formula (1-1): (where, R4 and R5 respectively and independently represent a halogen atom or alkyl group, R1 to R3 and R6 to R8 respectively and independently represent a hydrogen atom, halogen atom, alkyl group, fluoroalkyl group, hydroxyl group, alkoxyl group, amino group, alkylamino group, carbonyl group, alkylcarbonyl group, nitro group, cyano group or aryl group, Ar1 to Ar4 respectively and independently represent a substituted or unsubstituted aryl group, R4 may form a condensed, substituted or unsubstituted aryl ring with R3, and R5 may form a condensed, substituted or unsubstituted aryl ring with R6).

Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.

Abstract: A material for an organic electroluminescence device including at least one of compounds shown by the following formula (Ia), (Ib), (IIa), (IIb), (III), (IVa) or (IVb):

Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.

Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.

Abstract: The present invention relates to compounds of formula a process for their production and their use in electronic devices, especially electroluminescent devices. When used as host material for phosphorescent emitters in electroluminescent devices, the compounds of formula I may provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.

Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.

Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.

Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.

Abstract: Disclosed are novel rigidified compounds having a rhodanine-like residue and at least one aryl or heteroaryl residue linked to the rhodanine-like residue, whereby a core structure of these compounds, as defined in the specification, is characterized as having one or zero free-to-rotate bonds. Also disclosed are pharmaceutical compositions containing these rigidified compounds and uses thereof for modulating the activity of heparanase and hence in the treatment of heparanase-associated diseases and disorders, and uses thereof for modulating the activity of heparin-binding proteins and hence in the treatment of heparin-binding proteins-associated diseases and disorders as well as in the treatment of medical conditions that are at least partially treatable by rhodanine or a rhodanine analog.

Abstract: The compounds of formula (I) in which R1, R11 and A have the meanings as given in the description are novel effective iNOS inhibitors.

Abstract: A material for an organic electroluminescence device including at least one of compounds shown by the following formula (Ia), (Ib), (IIa), (IIb), (III), (IVa) or (IVb):

Abstract: Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H. alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl.

Abstract: An electron transport material based on fused aromatic electron-deficient compounds. The accumulation of aromatic rings with an electron deficiency allows free-radical anions to be stabilized very efficiently in these systems.

Abstract: The present disclosure relates to a novel dye composition for the dyeing and/or lightening of keratin materials, such dye comprising a hemicyanin styryl chromophore thiol or disulfide dye of formula (I) or (II): the organic or mineral acid salts thereof, optical isomers and geometric isomers thereof, and the solvates thereof such as hydrates. The present disclosure further relates to a dyeing process with a lightening effect on keratin materials, in particular keratin fibers, including human keratin fibers such as the hair, using said composition. This composition makes it possible to obtain a coloring with a lightening effect which is particularly resistant and visible on dark keratin fibers.

Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.

Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.

Abstract: The present disclosure relates to the process of dyeing human keratinous fibers, such as the hair, with at least one specific direct dye in cosmetic compositions. Also disclosed herein are the direct dyeing and lightening compositions comprising said compounds, and the corresponding dyeing kits.

Abstract: The present disclosure relates to a composition for dyeing human keratin fibers, such as the hair, comprising, in a medium suitable for dyeing, at least one direct dye and at least on dicationic compound. Also disclosed herein is a process for dyeing and lightening human keratin fibers, such as the hair, with the compositions disclosed, as well as a the corresponding dyeing kits.

Abstract: The present disclosure relates to a dyeing composition for human keratinous fibers, such as the hair, comprising, in a suitable dyeing medium, at least one oxidation dye, and at least one dicationic compound. The disclosure further relates to the dyeing methods and dyeing kit using the dye composition.

Abstract: Imido and Amido substituted alkanohydroxamic acids reduce the levels of TNFa and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.

Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is S.

Abstract: Yungamycin A has been demonstrated to have unexpected in vivo anticancer activity. New compounds Yungamycin B and C are also disclosed, and have been demonstrated to be specific for DT-diaphorase, as well as to have in vivo anticancer activity.

Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.

Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.

Abstract: Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.

Abstract: Compounds having the formula (I): and pharmaceutically-acceptable salts thereof, are useful for treating inflammatory or immune diseases, in which A is a four to seven membered heterocyclic or carbocyclic saturated ring; L and K are O or S; M is N or CH; Y is N or CH; Z is hydrogen, alkyl or substituted alkyl; and R1-R4 are as defined in the specification.

Abstract: This invention relates to compounds represented by the general formula [I] 1

Abstract: This invention relates to pharmaceuticals for neuropathic pains comprising an mGluR1 receptor antagonist for systemic administration. Drugs efficacious in treating various neuropathic pain can be provided by the invention.

Abstract: This invention relates to compounds represented by the general formula [I]   wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) 1

Abstract: Novel antimicrobial compositions and strategy to combat bacterial resistance in a variety of bacterial strains are disclosed. The antimicrobial compositions comprise a combination of mitomycin C, or other reductively activated compounds, and ABPI and/or imino-ABPI. The unique strategy involves exposing microorganisms to a first antimicrobial agent, such as mitomycin C, which can induce the expression of at least one protein which confers resistance to mitomycin C, i.e., inactivates mitomycin C. Simultaneously or soon thereafter, the microorganisms are exposed to a second antimicrobial agent, such as ABPI and/or imino-APBI, which is activated by the same protein which inactivates the first antimicrobial agent.

Abstract: Disclosed are 5,6-Dihydro-napth[1,2-d]-imidazoles, Naphth[1,2-d]imidazoles, and Chromane[3,4-d]imidazoles compounds having the formula: and the pharmaceutically acceptable salts thereof, wherein, A represents ethenylene, or A represents —X—CH2—; where X is CH2 or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring; R1, R2, R3 and R4 are inorganic or organic substituents; and R5 and R6 is are optionally substituted organic substituents; or NR5R6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various organic or inorganic groups. Such compounds are useful in the treatment of neuropsychological disorders.

Abstract: Bicyclic and tricyclic pyrrolidine derivatives are disclosed that are useful as antagonists of the GnRH receptor. Methods for using the novel compounds to treat GnRH-related disorders are also provided, as are pharmaceutical compositions and novel synthetic methods.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: Disclosed are compounds encompassed by general formula (I), wherein, A represents ethenylene, or A represents —X—CH2—; where X is CH2 or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring; R1, R2, R3 and R4 are inorganic or organic substituents; and R5 and R6 are optionally substituted organic substituents; or NR5R6 represents a carbocyclic or heterocyclic six-membered ring optionally substituted with various organic or inorganic groups, which compounds can be used in treatment of neuropsychological disorders.