Abstract: Metallotriangle-based nanomolecules are formed by a one-step self-assembly of specifically chosen shaped poly-ligand monomers, the poly-ligand monomers coordinating with metal ions through coordinating ligands. The poly-ligand monomers are defined by vertex groups having arms extending therefrom and ending in coordinating ligands. Based on the desired metallotriangle-based nanomolecule structure to be assembled, specifically shaped poly-ligand monomers and metal ions are chosen and mixed in appropriate ratios so that coordinating ligands bind to metal ions and the poly-ligand monomers thus spontaneously self-assemble into the desired metallotriangle-based nanomolecule structure.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

Abstract: The present invention relates to the use of compounds of general Formula I and pharmaceutically acceptable enantiomers, salts or solvates thereof, for treating pulmonary hypertension in a subject.

Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.

Abstract: A method of preparing a lyophilized powder for injection, including: (1) weighing and mixing aloe powder and Panax pseudo-ginseng powder to yield an active pharmaceutical ingredient, and mixing the active pharmaceutical ingredient and distilled water to yield a mixed aqueous solution; (2) stiffing the mixed aqueous solution to enable the aloe power and the Panax pseudo-ginseng powder to be completely dissolved, and then allowing the mixed aqueous solution to stand; (3) collecting, filtering, and clarifying a supernate obtained in (2); (4) adding hydrochloric acid to a filtrate obtained in (3) to adjust the pH value of the filtrate, heating and sterilizing the filtrate, and then naturally cooling the filtrate, to yield a cooled liquid; (5) adding hydrochloric acid to the cooled liquid to adjust the pH value of the cooled liquid, filtering the cooled liquid and collecting a pharmaceutical solution; and (6) packaging and lyophilizing the pharmaceutical solution.

Abstract: The presently-disclosed subject matter includes azetidine-substituted fluorescent compounds, where the compounds may be used as probes, dyes, tags, and the like. The presently-disclosed subject matter also includes kits comprising the same as well as methods for using the same to detect a target substance.

Abstract: Universal linkers, their facile processes of manufacture and methods of using the same are provided.

Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.

Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.

Abstract: The present invention relates to polymorphs of the 3-pyrrole substituted 2-indolinone compound 5-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide.

Abstract: One aspect of the present invention relates to novel peptidomometic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize ? opioid receptors. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels and agonize or antagonize ?-opioid receptors.

Abstract: Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.

Abstract: The present invention relates to novel phosphate isosteres. The invention relates to compounds having a sulfhydantoin or a reverse sulfhydantoin moiety, uses thereof, and related methods. The present invention relates to compounds of formula I or II: or pharmaceutically acceptable salts thereof; wherein Q, T, m, and X are as described herein. These compounds are inhibitors of phosphatases, particularly inhibitors of SHP-2. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing these compounds and compositions in the treatment of various phosphatase-mediated diseases.

Abstract: Novel indole derivatives of the formula (I), in which X, Y, R1, R1?, m and n have the meanings indicated in Patent Claim 1, have a strong affinity to the 5-HT1A and in some cases to the 5-HT1D receptors.

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I

Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen

Abstract: The present invention relates to a process for the preparation of a mixture comprising at least two structurally different diketopyrrolopyrrole pigments of formula (1) wherein A1 and A2 are each independently of the other an aromatic or heteroaromatic radical, by reacting a succinic acid ester with at least one unsubstituted or substituted aromatic or heteroaromatic nitrile, which process comprises carrying out the reaction in the presence of at least one compound of formula (2) wherein A is an aromatic or heteroaromatic radical, R3 is hydrogen, halogen, methyl, methoxy, —CF3 or —CN, R4 is a linear or, from C3 upwards, optionally branched C1-C30alkyl, C6-C10aryl or C6-C24aralkyl radical, X is —S—, —O—, —CR5R5?—, —COO—, —CONR5—, —SO—, SO2—, —SO2NR5— or —NR5— and R5 and R5? are each independently of the other hydrogen or a linear or, from C3 upwards, optionally branched C1-C30alkyl, C6-C10aryl or C6-C24aralkyl radical, to the use of such a mixture in the coloring of organic material and in cosmetics, and also t

Abstract: Compounds of formula wherein A1, A2 and A3 are each independently of the others a bond or a C1-C6alkylene bridge; A4 is a C1-C6alkylene bridge; D is CH or N; W is, for example, O, NR7 or S; T is, for example, a bond, O, NH or NR7; Q is O, NR7, S, SO or SO2; Y is O, NR7, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylcarbonyl or C2-C6alkenyl; R4 is, for example, H, halogen, CN, nitro or C1-C6alkyl; R5 and R6 are, for example, H, CN, OH, C1-C6alkyl, C3-C8cycloalkyl, C3-C8cycloalkyl-C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; R7 is H, C1-C6alkyl, C1-C6alkoxyalkyl or C1-C6alkylcarbonyl; k, when D is nitrogen, is 1, 2 or 3; or, when D is CH, is 1, 2, 3 or 4; and m is 1 or 2; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form or in salt form, a process for the preparation of those compounds and

Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. Said compounds are ligands of the TRPV1 vanilloid receptor, and are therefore, useful for treating diseases associated with TRPV1 receptors, such as pain and inflammation.