Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Importantly, these compounds can be administered orally.

Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.

Abstract: The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15-A16-A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —C(O)C1-C20alky or a di-aminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.

Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: The present invention is directed to therapeutic methods using IL-6 antagonists such as anti-IL-6 antibodies and fragments thereof having binding specificity for IL-6 to prevent or treat anemia (e.g., anemia associated with chemotherapy) including persons on a treatment regimen with a drug or chemotherapy and/or radiation for cancer (e.g., head and neck cancer) that is associated with increased risk of anemia.

Abstract: In one aspect, the present invention provides a method of treating lung cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor. In another aspect, the present invention provides a method of treating non-small cell lung cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor.

Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.

Abstract: The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is —N(R1b)—, G2 is —CO—, G3 is —C(R1c)(R1d)—, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.

Abstract: The present invention relates to antiviral compounds of formula (I), compositions containing these compounds, processes for their preparation, intermediates in their synthesis, and their use as therapeutics for prevention of organ transplantation rejection, the treatment of immune disorders and inflammation, and treatment of viral (particularly hepatitis C viral) infection.

Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.

Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein substituents A, B, X and Y are defined as in claim 1, medicaments containing said derivatives, and the use thereof in the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.

Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.

Abstract: The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonus spp., Acenetobacter spp., Mvraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotynebacterium, Bacillus spp., Enterobactericeae (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.

Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.

Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.

Abstract: A compound of the formula (I), (II), (III) or (IV) wherein Z, A, B, C, R, R1, R2, Q, and n are as described herein.

Abstract: Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines are disclosed. The compounds are useful, for example, in reducing the levels of TNF? in a mammal.

Abstract: Disclosed are new compounds of formula (1) exhibiting excellent activity for glucokinase, pharmaceutical compositions having the same as an active ingredient, and a method of using the same as an active ingredient for lowering blood glucose level: in which the substituents are as defined herein.

Abstract: Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same.

Abstract: Improved pharmacokinetic profiles for the iontophoretic delivery of sumatriptan are described.

Abstract: Provided are 4?-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

Abstract: One object of the present invention are novel substituted piperidyl-propane-thiols of the formula (1), wherein R1, R2, R3 and R4 are defined as below. Another object of the present invention is to provide agonists or antagonists of CCR-3, or pharmaceutically acceptable salts thereof, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.

Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.

Abstract: To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).

Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).

Abstract: Compounds useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.

Abstract: The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors.

Abstract: Disclosed are isoindolinone derivatives, represented by Chemical Formula 1, having inhibitory activity against T-type calcium channels, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient. wherein R1˜R6 are as defined in the specification.

Abstract: One object of the present invention are novel substituted piperidyl-propane-thiols of the formula (1), wherein R1, R2, R3 and D are defined as below. Another object of the present invention is to provide agonists or antagonists of CCR-3, or pharmaceutically acceptable salts thereof, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (I): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of -X1=X2-X3=X4- is a formula of —C(R1)?C(R2)—C(R3)?C(R4)— etc.; X5 is C(R5) or N; R1, R2, R3, R4 and R5 is independently a hydrogen atom, a halogen atom etc; R6 is a formula of -Z-R10 etc. wherein Z is alkylene etc., and R10 is carboxy etc.; R7 is optionally substituted alkyloxy etc.; R8 is independently a halogen atom etc.; R9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or a solvate thereof.

Abstract: Compounds which inhibit the activity of poly(ADP-ribose)polymerase, compositions containing the compounds and methods of treating diseases using the compounds is disclosed.

Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.

Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Importantly, these compounds can be administered orally.

Abstract: The present invention relates to improved processes for preparing 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (I) (lenalidomide) and its intermediate 3-(1-oxo-4-nitro-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to improved processes for preparing lenalidomide crystalline form A, use of said crystalline form A as an active pharmaceutical ingredient or as an intermediate in the preparation of further crystalline or amorphous forms of lenalidomide, compositions comprising lenalidomide crystalline form A and their use in the treatment of disease.

Abstract: A method for treating migraines is disclosed. The method utilizes a rapid drug delivery system which prevents deactivation or degradation of the active agent, including small molecules and peptides being administered to a patient in need of treatment. In particular, the drug delivery system is designed for inhalation for delivery of drugs to the pulmonary circulation in a rapid and therapeutically effective manner.

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: Provided herein are thalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.

Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.

Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.

Abstract: The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R1, R2 and R3 are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.

Abstract: The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The compounds have the formula I? wherein R1, R2, T, R3 and R4 are as defined in the specification.

Abstract: Provided herein are lenalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.

Abstract: Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.

Abstract: The invention relates to non-crystalline lenalidomide in the form of a storage-stable intermediate, i.e. preferably amorphous lenalidomide together with a surface stabiliser in the form of a stable intermediate or a storage-stable intermediate, containing lenalidomide and matrix material, wherein the lenalidomide is present in the form of a solid solution (i.e. molecularly disperse). The invention further relates to methods of producing stable amorphous or molecularly disperse lenalidomide and pharmaceutical formulations containing stable amorphous or molecularly disperse lenalidomide. In a second aspect, the invention advantageously relates to dry-processing methods for lenalidomide, especially amorphous and disperse lenalidomide.

Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.

Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.

Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.

Abstract: The present invention relates to a novel crystalline form of zofenopril calcium of formula (I), chemically known as (4S)-1-[(2S)-3-(benzoylthio)-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt. The present invention further relates to a process for the preparation of the new crystalline form of zofenopril calcium and its use in pharmaceutical preparations.

Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.