Abstract: The invention relates to a series of thiazoline and oxazoline derivatives, compositions thereof, and methods of treating conditions and disorders using such compounds.

Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

Abstract: Aamantane dipyrromethane derivatives are obtained by reacting adamantane carbonyl derivatives with pyrrole or pyrrole derivative, in the presence of acid. Adamantane-dipyrromethanes are used to bind anions of the group consisting of: F—, Cl—, Br—, acetate, HSO4— NO3—, and H2PO4—, and particularly F—.

Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.

Abstract: The present invention relates to compounds of formula (I), which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.

Abstract: The present invention relates to novel inhibitors of prolyl endopeptidase of formula 1 W—KCONH—X—CON—Y—CO—Z??(1) wherein K, W, X, Y and Z are specified in the description. The compounds are useful for the treatment of diseases such as mild cognitive impairment (MCI), Alzheimer's disease, Down Syndrome, Parkinson disease and Chorea Huntington.

Abstract: A colorant contains a crystal of a compound represented by the following formula (1): the crystal having a crystal form showing main peaks at interplanar spacings d of 3.45±0.5 ?, 3.63±0.5 ?, 4.23±0.5 ?, 6.65±0.5 ?, and 7.84±0.5 ? in powder X-ray diffraction pattern with CuK? radiation.

Abstract: This invention relates to novel macromolecular compositions having oxidation inhibition characteristics that are exhibited when added to organic material normally susceptible to oxidative degradation in the presence of air or oxygen, such a petroleum products, synthetic polymers, and elastomeric substances.

Abstract: The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

Abstract: Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.

Abstract: Pharmaceutical compositions containing organic compounds or salts thereof that serve as modulators for the SDF-1 or I-TAC chemokines are disclosed. The compounds and compositions are useful in the treatment of cancer, especially in the inhibition of cancer proliferation, growth, and metastasis. Methods of interfering with SDF-1 and/or I-TAC binding to the CCXCKR2 receptor and treating cancer using the compounds and pharmaceutical compositions of the present invention are also disclosed.

Abstract: Compounds of formula (I): wherein A is a 5-membered heteroaryl ring are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38, such as rheumatoid arthritis.

Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist 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 them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.

Abstract: Disclosed are compounds having Formula (I) and the compositions and methods relating to these compounds, for treating or preventing a viral infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R2, m, R, V, W, T, Z, R1, Y, and p are disclosed herein.

Abstract: The present invention relates to a compound of the following formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.

Abstract: The invention provides novel indane compounds which are useful in the treatment of affective disorders, pain disorders, attention deficit hyperactivity disorder (ADHD), cognitive disorders, substance abuse, smoking cessation and stress urinary incontinence.

Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.

Abstract: A method of making a porphyrin (I) is carried out by condensing (i) a bis(imino)dipyrromethane of Formula II: with (ii) a dipyrromethaneto produce a reaction product; then (b) optionally oxidizing said reaction product with an oxidizing agent; and then (c) optionally demetallating said reaction product to produce the porphyrin. Methods of making compounds of Formula II are also described.

Abstract: The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

Abstract: The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.

Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L1, R1, R2, R3, R4, R5, R6, and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.

Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: Compounds having the formula are angiogenesis inhibitors. Also disclosed are compositions containing the compounds, methods of making the compounds, and methods of treatment using the compounds.

Abstract: There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally.

Abstract: Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I: or a salt thereof, in which R1, R2, R100, R200, A, A1, B, B1, BG, n, Q and Q1 are substituents described. Also disclosed is the use of compounds of Formula 1 to treat proliferative disorders.

Abstract: Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

Abstract: Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.

Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrile groups, and the products thereby are provided.

Abstract: A method of making a porphyrin is carried out by: (a) condensing (i) a 1,9-bis(N,N-)dialkylaminomethyl)dipyrromethane of Formula II: with (ii) a dipyrromethane to produce a reaction product; then (b) oxidizing the reaction product; and then (c) optionally demetallating said reaction product to produce the porphyrin. The reaction is particularly useful for making substituted porphyrins with a wide range of substituents at the A and/or B (the 5 and/or 15) positions.

Abstract: Disclosed herein is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I: or a prodrug, or a pharmaceutically acceptable salt, or labeled with a detectable label or an affinity tag thereof; wherein R1, R1a, R100, R100a, R2, R200, W, B, and W1 are defined herein. Also disclosed are methods of using compounds of Formula I to treat proliferative disorders such as cancer.

Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.

Abstract: Described are merocyanine derivatives of formula wherein R2 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; a cyano group; or R1 and R2 together with the nitrogen atom linking them form a —(CH2)m— ring which is optionally interrupted by —O— or by —NR7—; R4 is a cyano group; or -Q1-R5; Q1 is —COO—; —CONH—; —CO—; —SO2—; or —CONR6—; R5 is C1-C22alkyl; cyclo-C3-C8alkyl; or unsubstituted or C1-C6alkyl-substituted C6-C20aryl; R6 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; R7 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; the cyclohexene radical C is not substituted or substituted by one or more C1-C5alkyl; m is from 3 to 7; n is from 2 to 4; and o is from 2 to 4.

Abstract: The present application relates to mixed Mg/Li amides of the general formula R1R2N—Mg(NR3R4)mX,m zLiY (II) wherein R1, R2, R3, and R4 are, independently, selected from H, substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or silyl derivatives thereof; and R1 and R2 together, or R3 and R4 together can be part of a cyclic or polymeric structure; and wherein at least one of R1 and R2 and at least one of R3 and R is other than H; X and Y are, independently, selected from the group consisting of F; Cl; Br; I; CN; SCN; NCO; HalOn, wherein n=3 or 4 and Hal is selected from Cl, Br and I; NO3; BF4; PF6; H; a carboxylate of the general formula RXCO2; an alcoholate of the general formula ORX; a thiolate of the general formula SRX; RXP(O)O2; or SCORX; or SCSRX; OnSRx, wherein n=2 or 3; or NOn, wherein n=2 or 3; and a derivative thereof; wherein Rx is a substituted or unsubstituted aryl or heteroaryl containi

Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.

Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, R3, W, D and R2 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.

Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.

Abstract: The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.

Abstract: Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I: or a salt thereof, in which R1, R2, R100, R200, A, A1, B, B1, BG, n, Q and Q1 are substituents described. Also disclosed is the use of compounds of Formula 1 to treat proliferative disorders.

Abstract: A method of making a 5-formylporphyrin, comprises the steps of: condensing a 5-acetaldipyrromethane with a dipyrromethane-1,9-dicarbinol to produce a porphyrin having an acetal group substituted thereon at the 5 position; and then hydrolyzing said porphyrin to produce said 5-formylporphyrin. Products and intermediates useful in such methods, along with methods of making such intermediates, are also described.

Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.

Abstract: The invention provides compounds of general formula (D wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: A method of making a metalloporphyrin is carried out by reacting (i) a linear tetrapyrrole, said linear tetrapyrrole having a 19-acyl group and a 1-protecting group, with (ii) a metal salt under basic conditions to produce the metalloporphyrin. Products produced by such methods and intermediates useful for carrying out such methods are also described.

Abstract: A method of making a 5-formylporphyrin, comprises the steps of: condensing a 5-acetaldipyrromethane with a dipyrromethane-1,9-dicarbinol to produce a porphyrin having an acetal group substituted thereon at the 5 position; and then hydrolyzing said porphyrin to produce said 5-formylporphyrin. Products and intermediates useful in such methods, along with methods of making such intermediates, are also described.

Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.

Abstract: The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist 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 them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.