Abstract: The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting.

Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.

Abstract: This present invention generally relates to xanthine derivatives as muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.

Abstract: It is intended to provide antipruritics (drugs to control itching, antiitch agents and drugs to stop itching). It is found out that a compound having an agonistic activity to the cannabinoid receptor shows an antipruritics effect.

Abstract: The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.

Abstract: The present invention is directed to compounds of formula (I): described as novel indolizine derivatives and to a method for their preparation along with pharmaceutical compositions thereof whose substituents are as described in the specification.

Abstract: This present invention generally relates to muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.

Abstract: The present disclosure concerns methods of administering and detecting a distinguishable agent in a sample from and assessing the condition of an organ in a subject. In a particular embodiment, the present invention concerns methods of detecting and comparing the cholate shunt, in a subject, preferably in a subject with chronic hepatitis C. In certain embodiments, the methods may comprise obtaining a sample from a subject such as a blood or saliva sample after administering an oral and intravenous dose of a distinguishable agent such as cholate and analyzing the sample clearance of the distinguishable agent from the subject and comparing the clearance levels in order to assess hepatic health. In another embodiment, the methods may comprise analyzing a sample from a subject for the presence of a distinguishable agent such as cholate and applying information obtained from analyzing the presence of the distinguishable agent to determine a treatment for a medical condition of the subject.

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, CSK, JNK1, JNK2, PDGF-R, p38, p70S6K, TGF?, SRC, EGFR, c-Kit, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6 and SAPK2? kinases.

Abstract: Herbal extracts composition suitable for weight management in mammals is disclosed. The composition comprises a mixture of Garcinia extract, Green tea extract, Green coffee extract and Banaba extract. The method of reducing weight, and treating diabetes in mammals involve oral administration of the composition. The invention further relates to a method of producing and standardizing the individual extract useful for human health.

Abstract: Compounds of formula I or salts thereof: in which R1 represents —OH, (C1-C5)alkoxy, carboxyl, (C2-C6)alkoxycarbonyl, —NR5R6, —NH—SO2-Alk, —NH—SO2-Ph, —NH—CO-Ph, —N(Alk)-CO-Ph, —NH—CO—NH-Ph, —NH—CO-Alk, —NH—CO2-Alk, —O—(CH2)n-cAlk, —O-Alk-COOR7, —O-Alk-O—R8, —O-Alk-OH, —O-Alk-C(NH2):NOH, —O-Alk-NR5R6, —O-Alk-CN, —O—(CH2)n-Ph, —O-Alk-CO—NR5R6, —CO—NH—(CH2)m—COOR7, —CO—NH-Alk R2 represents H, (C1-C5)alkyl, (C1-C5)alkyl halide, (C3-C6)cycloalkyl or phenyl which is optionally substituted, A represents —CO—, —SO— or —SO2—, R3 and R4 which are identical or different, each represent H, (C1-C5)alkoxy, amino, carboxyl, (C2-C6)alkoxycarbonyl, —OH, nitro, hydroxyamino, -Alk-COOR7, —NR5R6, —NH-Alk-COOR7, —NH—COO-Alk, —N(R11)—SO2-Alk-NR9R10, —N(R11)—SO2-Alk, —N(R11)-Alk-NR5R6, —N(R11)—CO-Alk-NR9R10, —N(R11)—CO-Alk, —N(R11)—CO—CF3, —NH-Alk-HetN, —O-Alk-NR9R10, —O-Alk-CO—NR5R6, —O-Alk-HetN, or R3 and R4 form together a 5- to 6-membered unsaturated heterocycle, are inhibitors of basic fibroblast growth factors.

Abstract: Compounds of the formula I or a pharmaceutically acceptable salt thereof: processes for their preparation, pharmaceutical compositions which contain them and their uses in therapy.

Abstract: A method for rapidly screening small molecules to identify small molecules that stimulate axon regeneration and outgrowth from adult sensory neurons. The method generally comprises preparing a purified individualized dorsal root ganglia cell suspension (DRG), coating well surfaces of a suitably prepared multi-well microplate with the DRG, then dispensing dosages of selected small molecules into selected wells. The microplates are incubated under sterile conditions at about 37° C. for at least 24 hours. The DRG suspension in each well is then morphometrically assessed to assess the extent of axon regeneration and outgrowth that occurred, and the effects of the selected small molecules are determined by comparison to control treatments. The method is suitable for screening chemically derived small molecules and biologically derived small molecules.

Abstract: The present invention provides a compound of formula (I) where X, R, Y, D, A and B are as defined herein.

Abstract: Carbamates of formula (I) or pharmaceutically acceptable salts thereof, including quaternary ammonium salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

Abstract: The invention relates to a composition containing, preferably in a physiologically acceptable medium, at least one xanthine base or a plant extract containing it, at least one polyurethane powder, and at least one non-ionic dimethicone copolyol. The invention also relates to a cosmetic method for combating cellulite and/or “orange-peel” skin and/or slimming the figure, comprising the application of the composition to the skin. The composition applied to the skin exhibits good cosmetic properties of softness and of non-tackiness.

Abstract: This invention relates to azacyclic derivatives according of formula (I) and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or. disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the? termination of abuse of chemical substances.

Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, and depression. This invention could also be used for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.

Abstract: The present invention provides compositions, methods and kits for treating, preventing or reducing the risk of developing a CNS disorder. In general, the invention involves utilizing caffeine for preventing or alleviating pathological symptoms of a CNS disorder, such as headache, epilepsy, pain, Parkinson's disease, psychiatric disorders such as anxiety, bipolar disorder, depression, and schizophrenia, ADD, and ADHD.

Abstract: The present invention relates to a cosmetic preparation containing an emulsifier combination of polyacrylic acid salts, acrylate/C10-30 alkyl acrylate crosspolymer and carrageenan and the use of the cosmetic preparation.

Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the ?7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission.

Abstract: This invention relates to novel enantiomers useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.

Abstract: Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.

Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.

Abstract: A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula (I): wherein X represents a single bond or a C1 to C6 alkylene group which may be substituted; A represents a C1 to C6 alkyl group which may be substituted, a C6 to C10 aryl group which may be substituted, or a 4 to 10-membered monocyclic or bicyclic and unsaturated, partly saturated, or completely saturated heterocyclic group which may be substituted, wherein said heterocyclic group comprises as ring-constituting atoms 1 to 4 hetero atoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom.

Abstract: The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R18, R19, R20, R21 and R22 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. 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 chemokine receptors are involved.

Abstract: Chronic pain is alleviated in a mammal suffering there from by administering to the mammal a chronic pain alleviating amount of a nontoxic N-methyl-D-aspartate receptor antagonist such as dextromethorphan, dextrorphan, ketamine or pharmaceutically acceptable salt thereof, in combination with a ?-opiate analgesic such as tramadol or an analogously acting molecular entity, and a methylxanthine such as caffeine, and optionally in sustained release dosage form.

Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

Abstract: The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula wherein: R1, R2, and R3 are as defined herein and pharmaceutically acceptable acid addition salts thereof. These compounds have high affinity and selectivity for GABA A ?5 receptor binding sites. The invention also relates to methods for enhancing cognition and treating cognitive disorders like Alzheimer's disease.

Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Abstract: The present invention provides compounds of the formula: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.

Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof, may be used in therapy, for example as antifungal agents: (I) wherein: R1, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. Certain compounds of formula (I) are also provided. Compounds of formula (T), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.

Abstract: The present invention relates to capsules for holding pharmaceutical preparations for powder inhalers with increased drug safety and capsules for pharmaceutical preparations for powder inhalers with improved adaptation to their use in powder inhalers. The capsules consist of water-insoluble hydrophobic synthetic materials which do not significantly affect the pharmaceutical quality of the contents themselves, but which improve the usability of the filled capsules with regard to their function, their longevity, and/or the geographic location of their use, and are advantageous at various stages from manufacture up to utilization.

Abstract: Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.

Abstract: The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs).

Abstract: The present invention relates to a new use for compounds having 5-HT3 (serotonin M) receptor antagonist activity, especially tropisetron, for the manufacture of a pharmaceutical composition for the treatment of a non-inflammatory local disease of the musculo-sceletal system, of a local irritation condition of a joint or tendon sheath, or for the local treatment a local manifestation at the locomotor apparatus of an inflammatory disease except for a crystal induced arthritis and a living pathogen induced inflammatory disease condition as long as the living pathogen is still present.

Abstract: The present invention relates to compounds of formula (I-VII) or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R6, R7 and R8 are defined herein. The present invention also relates to methods of treating pain using these compounds and pharmaceutical compositions including these compounds.

Abstract: Disclosed herein are substituted 8-azabicyclo[3.2.1]octane-based anti-infective agents of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Sulfonamides of the formula I where the substituents are as follows: R1 is hydrogen, alkyl, alkoxy, alkenyl or alkynyl; and R2, R3, R4, R5 are hydrogen, halogen, alkyl, alkoxy or halomethyl; R2 and R3 together may also form a phenyl, cyclopentyl or cyclohexyl ring, it being possible for these rings to carry two groups R2, and R3, R2, R3, are hydrogen, halogen, alkyl, alkoxy or halomethyl; in case a), if R2, R3, R4 and R5 are hydrogen: X is phenyl substituted by a group —C(R6)?NOR7, where R6 is alkyl and R7 is alkyl, benzyl, alkenyl, haloalkyl, haloalkenyl, alkynyl or haloalkynyl; and in case b), if at least one of the groups R2, R3, R4 and R5 is not hydrogen: X is phenyl, naphthyl or a five- or six-membered saturated, or partially unsaturated or aromatic heterocycle which is attached via a carbon atom and contains one to four heteroatoms from the group consisting of O, N and S, where X may be substituted according to the description; Processes for preparing these compounds, compositions comprisi

Abstract: The invention relates to novel cyclic peptidomimetic compounds containing the sequence RGD for the preparation of appropriately functionalised antagonists of ?v?3 and ?v?5 integrins, and intended, for example, for the treatment of altered angiogenic phenomena or for the preparation of diagnostically useful compounds.

Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: Compounds of formula I: wherein A and R1 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.

Abstract: The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.

Abstract: The present invention relates to methods of alleviating and inhibiting a lymphoproliferative disorder in a mammal, the method comprising administering one or more rapamycin derivatives (including rapamycin) to the mammal. Further, the invention provides a method for identifying agents which are useful for alleviating and inhibiting a lymphoproliferative disorders, as well as a method for identifying agents which are capable of inhibiting metastasis of lymphatic tumors in a mammal.

Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.