Abstract: The present invention relates to CGRP antagonists of general formula wherein A, U, V, W, X and R1 to R3 are defined as in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.

Abstract: The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions in mammals: wherein n is an integer, preferably n is 1; wherein R1 and R2 are independently selected from the group consisting of:

Abstract: Various non-limiting embodiments disclosed herein relate generally to photochromic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. Other non-limiting embodiments relate to photochromic-dichroic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. For example, one non-limiting embodiment provides a thermally reversible, photochromic compound adapted to have at least a first state and a second state, wherein the thermally reversible, photochromic compound has an average absorption ratio greater than 2.3 in at least one state as determined according to CELL METHOD.

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 relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to 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. The invention further relates to crystalline forms of a compound of formula (I).

Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease

Abstract: Processes and intermediates for preparing substituted 4-amino-1-(pyridylmethyl)-piperidine and related compounds in high yield and high purity are described. The substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds prepared by the described processes are useful as muscarinic receptor antagonists.

Abstract: Substituted 1,5-diaminopentan-3-ol compounds and methods of making the same. Pharmaceutical compositions containing these compounds and methods of treatment using these pharmaceutical compositions.

Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.

Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract: The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable acid addition salts, intermediates thereto, processes for the preparation thereof, and therapeutic application thereof.

Abstract: The present invention relates to the CGRP antagonists of general formula wherein A and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.

Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.

Abstract: The present invention relates to compounds of formula I wherein X, A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, m and n are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.

Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.

Abstract: Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes.

Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF—or combinations thereof.

Abstract: The present invention discloses novel compounds of Formula I: (I) having 11-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11-HSD type 1 activity.

Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.

Abstract: The present invention discloses novel compounds of Formula I: having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.

Abstract: The present invention discloses novel compounds of Formula I: having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.

Abstract: Compounds of Formula I, or pharmaceutically acceptable salts thereof: wherein R2, R3, X, m and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

Abstract: The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract: The present invention relates to compounds of formula (I): The variables recited in formula (I) are defined in the specification. The present invention also relates to processes of preparing compounds of formula (I) and uses of such compounds for treating a chemokine (e.g., CCR3) or H1 mediated disease state.

Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.

Abstract: The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.

Abstract: This invention relates to piperidine derivatives of formula I wherein R1, R2, R3 and R4 are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), rheumatoid arthritis, solid organ transplant reject (graft vs. host disease), asthma and COPR.

Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreating carcinomas) and mesotheliomas.

Abstract: The invention is concerned with novel imidazole derivatives of formula (I), wherein m, E, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.

Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.

Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: [Problem] To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. [Means for Solution] We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

Abstract: Peptide mimetic small molecule inhibitors of Sur-2 are provided having the general formula:

Abstract: The present invention relates to compounds comprising an oxazole or thiazole moiety of formula (I), processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, Formula (I), wherein, A1 is CH, C(alkyl), C-halogen or N; R1 is hydrogen, halogen, C1-6 alkyl or alkoxy; R2 is, Formula (II?), A3 is O or S; R3 is hydrogen, halogen, C1-6 alkyl or alkoxy; R4 is hydrogen, halogen, C1-6 alkyl, alkoxy or —O-L; R5 is hydrogen or —O-L, wherein L is an aminoalkyl group and at least one of R4 and R5 should be —O-L.

Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, (II) or (III) R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl;

Abstract: The present invention provides a novel fluorescent chemosensor including a naphthalene diimide-Zn(II) complex, which can efficiently recognize pyrophosphate (PPi) at pH 7.4. The fluorescent chemosensor exhibits a new kind of excimer fluorescence, which is selective for PPi in 100% aqueous solution. Further, since the naphthalene diimide-Zn(II) complex of the present invention does not couple with inorganic phosphate (Pi) or adenosine triphosphate (ATP) and has high selectivity for PPi, it can be usefully used to detect pyrophosphate (PPi), which serves to transfer signals and store energy in living organisms.

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytotoxic drugs in a targeted fashion.

Abstract: Substituted sulfonamide compounds with bradykinin receptor (B1R) modulating activity; processes for the preparation thereof, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or inhibit pain and/or other disorders and/or disease states.

Abstract: Disclosed are compounds of formula I: wherein R1, R2, R3 and X are as defined herein, in free or salt form, which are useful as CCR5 inhibitors, e.g. in the prevention or treatment of disorders mediated by interactions between chemokine receptors and their ligands.

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 present invention relates to compounds comprising an oxazoline or thiazoline moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, (I), wherein A1 is CH C(CH3) or N; R1 is hydrogen or halogen; R2 is (II); A2 is O or S; R3 is hydrogen, halogen, C1-4 alkyl or C1-4 alkoxy; R4 is hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or —O—(CH2)n-NR12aR each CH2 in —O—(CH2)n-NR12aR 12b being optionally substituted by one or two C1-4 alkyl; R5 is hydrogen or —O—(CH2)m—NR13aR13b, each CH2 in —O—(CH2)m—NR13aR13b being optionally substituted by one or two C1-4 alkyl, and at least one of R4 and R5 should be a —O—(CH2)n-NR12/13aR12/13b group.

Abstract: The invention is concerned with novel heteroarylacetamides of formula (I) R—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb) ??(I) wherein Ra to Re are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Abstract: The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.