Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.

Abstract: In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.

Abstract: The present invention provides methods for the use of visible and/or near-infrared spectroscopic methodology to monitor and control processes for the generation of particles, including processes that provide for a reduction in particle size and processes that result in an increase in particle size. One embodiment of the present invention employs visible and/or near-infrared diffuse reflectance spectroscopy to monitor particle size. The present invention is particularly useful for monitoring particle size of optically dense samples and is further useful for monitoring the endpoint of particle generation processes. In contrast to methods known in the art, the present invention is especially useful for on-line monitoring of particle size.

Abstract: Pyrrole compounds of Formula (I): and pharmaceutically acceptable salts thereof (where A, B, R11, R12, R13, W, X, Y and Z are as defined herein), which are substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases

Abstract: A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: Pyrrole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, circadian rhythm disorders, and other diseases.

Abstract: In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one carbon atom. The ring additionally includes three, four or five atoms independently selected from carbon, nitrogen, sulfur and oxygen atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon double bond, a carbon-carbon triple bond or an azo group. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system.

Abstract: The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.

Abstract: The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.

Abstract: A class of 8-fluoro-3-phenylimidazo[1,2-?]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a —NH— or —OCH2— linkage, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: Substituted carbocyclic sulphonamide derivatives of formula (I), in which n is 0 or 1 and the other variables are as defined in the claims, are selective 5-HT7 receptor antagonists and are thereby effective in the treatment of a variety of neurological conditions, including depression and sleep disorders.

Abstract: Two new crystalline monhydrates and two new crystalline anhydrates of gaboxadol are disclosed together with methods for preparing them.

Abstract: The present invention is directed to processes for the preparation of 3-chloromethyl-1,2,4-triazolin-5-one. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity. Also disclosed are novel semicarbazide salts and the preparation thereof, which are intermediates for the preparation of 3-chloromethyl-1,2,4-triazolin-5-one.

Abstract: A class of 8-fluoroimidazo[1,2-?]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: The present invention provides a compound of formula I: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, —CO2Ra, —CONRaRb or —CRa?NORb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions comprising this compound and methods of treating and/or preventing anxiety and convulsions using it.

Abstract: Novel splice variants of the human H3 histamine receptor are described. The splice variants have deletions of portions of the N-terminal of the wild type H3 receptor. The splice variants are useful in methods for identifying agonists, inverse agonists or antagonists of histamine action at the H3 receptor.

Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.

Abstract: A class of imidazo[1,2b][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: Novel splice variants of the human H4 histamine receptor are described. The splice variants have delections of portions of the N-terminal of the wild type H4 receptor. The splice variants are useful in methods for identifying agonists, inverse agonists or antagonists of histamnie action at the H4 receptor.

Abstract: The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.