Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.

Abstract: Disclosed are dihydroindolone compounds which can modulate the activity of protein tyrosine kinases, a method for preparing the same, and pharmaceutical compositions comprising the same. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.

Abstract: Indirubin derivatives of formula (I) wherein R represents -(A)n- R1 or —CO—N(R2,R3) with •A being C1-C5 alkylene group, optionally substituted by one or several A1 radical, A1 being an halogen Br, OH, OR4 or NH2, R4 being C1-C5 alkyl; —R1 being halogen, OH, N(R2, R3); R2 and R3, identical or different, being C1-C5 alkyl, optionally substituted by A1 such as above defined, or R2 and R3 are part of a cycle with 5 or 6 elements optionally comprising another heteroatom such as O or N; •n=1?5. It also relates to the biological application thereof.

Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

Abstract: The invention concerns a method for separating a racemic compound-forming chiral substance by a cyclic crystallization process which is conducted in at least one first crystallization unit (10) and in at least one second crystallization unit (18), wherein in a first process cycle an enantiomer is crystallized in the first crystallization unit (10) and a racemic compound is crystallized in the second crystallization unit (18), wherein in a second process cycle the enantiomer is crystallized in the second crystallization unit (18) and the racemic compound is crystallized in the first crystallization unit (10), wherein during each process cycle in at least one process sub-step (B?C, F?G) a mother liquor (12) being contained in the first crystallization unit (10) is mutually exchanged with a mother liquor (20) being contained in the second crystallization unit (18). An auto-seeding process sub-step is applied at the beginning of a process cycle.

Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.

Abstract: The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.

Abstract: An N-phenyl-diphenylisoindole derivative having the following formula (1): wherein each of R1 and R2 represents a hydrogen atom, a substituted or an unsubstituted alkyl group, a substituted or an unsubstituted alkoxy group, a substituted or an unsubstituted phenyl group, or a substituted or an unsubstituted phenoxy group; R3 represents a hydrogen atom, a substituted or an unsubstituted alkyl group, a substituted or an unsubstituted alkoxy group, a substituted or an unsubstituted phenyl group, a substituted or an unsubstituted phenoxy group, or has the following formula (2): wherein each of R4 and R5 represents a substituted or an unsubstituted alkyl group, or a substituted or an unsubstituted phenyl group; 1 represents an integer of from 1 to 4; and each of m and n represents an integer of from 1 to 5.

Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

Abstract: A family of three 8-alkyl boron dipyrromethenes 1, 2, and 3 has been prepared. These compounds are characterized by emission in the green region of the electromagnetic radiation spectrum and exhibit an almost double laser efficiency than other commercial dyes and much greater photostability. The 8-alkyl boron dipyrromethenes are prepared by catalytic hydrogenation (reduction) of the corresponding 8-alkenyl boron dipyrromethenes, which are obtained by Liebeskind-Srogl coupling of thiomethylboron dipyrromethene with an alkenyl boronic acid.

Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract: Aspects of the present application relate to a microcrystalline monoclinic form of asenapine maleate represented by structural Formula (I); processes for its preparation; and pharmaceutically acceptable dosage forms thereof.

Abstract: In one aspect, the invention relates to indole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The invention relates to streptospirole derivatives of the general formula (I), wherein R1, R2, R3, X1, X2, Y1 and Y2 are as defined herein, a process for the preparation of said compounds by fermenting the microorganism Streptomyces sp. ST 108140 (DSM 19369) and optionally derivatizing the compounds produced by said microorganism, a pharmaceutical composition comprising at least one compound of the formula (I), and the use of a compound of the formula (I) for the preparation of a medicament for the treatment and/or prophylaxis of bacterial infections.

Abstract: Compounds that can be used as openers or blockers of voltage-dependent potassium channels, and which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing or enhancing cortical and/or peripheral neuron activity, compositions containing same and methods utilizing same are disclosed. Also disclosed are modulators of voltage-dependent potassium channels, which exhibit blocking of a TRPV1 channel, and hence are useful in the treatment of TRPV1-related conditions.

Abstract: Provided are a novel nitrogen-containing aromatic heterocyclic compound and an organic electronic device using the compound. This nitrogen-containing aromatic compound is represented by the general formula (1). Further, the present invention relates to organic electronic devices such as a light-emitting device, a thin-film transistor, and a photovoltaic device each using the nitrogen-containing aromatic compound. (L represents an m+n-valent aromatic hydrocarbon group or aromatic heterocyclic group, or a group arising from a triarylamine or a diaryl sulfone; X represents N-A, O, S, or Se; A represents an alkyl group or the like; R represent hydrogen, an alkyl group, an aromatic group, or the like; and m+n is an integer of 2 to 4.

Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.

Abstract: Provided are a nitrogen-containing aromatic heterocyclic compound useful as an organic semiconductor material and an organic electronic device using this compound. The nitrogen-containing aromatic heterocyclic compound has a fused indole skeleton represented by the following formula (1), the organic semiconductor material contains the compound, and the organic electronic device uses the organic semiconductor material. In general formula (1), X is N-A?, O, S, or Se; A is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more; and R is a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more.

Abstract: Inhibitors of HCV replication of formula (I) wherein W is a heterocycle of formula and the remaining variables are as defined in the specification.