Abstract: New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.

Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.

Abstract: The present disclosure relates to the use of 5-fluorocytosine as a seed treatment to prevent or control plant diseases.

Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD.

Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.

Abstract: A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect.

Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.

Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. 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 metabotropic glutamate receptors are involved, such as schizophrenia.

Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The invention relates to a pharmaceutical dosage form comprising one or more antiretroviral active ingredients in the form of a solid dispersion or solid solution in a matrix, wherein said matrix comprises an amino(meth)acrylate copolymer, characterized in that the matrix does not contain any essential amounts of pharmaceutically acceptable surfactants with an HLB value from 12 to 18 and in that the matrix comprises a mono carboxylic acid or an alcohol with 12 to 22 carbon atoms or both.

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Abstract: The present invention provides organic arsenicals. Many of these compounds have potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia.

Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.

Abstract: Various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis can be treated with a compound selected from an incretin mimetic and a dipeptidyl peptidase IV inhibitor in combination with a Compound of Formula I or a pharmaceutically acceptable salt thereof Three of R1, R2, R3, R4 and R5 are hydrogen and the remainder are independently selected from the group consisting of hydrogen, halo, hydroxy, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, and perfluoromethoxy; and m is 0, 2 or 4. R6 is hydrogen, O or hydroxy, and X is —OR7, wherein R7 is hydrogen or alkyl having from 1 to 3 carbon atoms; or R6 is hydrogen, and X is —NR8R9, wherein R8 is hydrogen or hydroxy and R9 is hydrogen, methyl or ethyl. When X is —NR8R9, hydroxy none of R1, R2, R3, R4 and R5 is hydroxy.

Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.

Abstract: The present invention provides a composition for use as a harmful organism control agent comprising as an active ingredient one or more of compounds represented by formula (I) or salts thereof and an agriculturally or zootechnically acceptable carrier. wherein Het represents pyridyl; X represents an oxygen atom; R1, R2, R3, R7, R10a, R10b, R11, and R12 represent a hydrogen atom; R4, R5, and R6 represent a hydrogen atom, hydroxyl, optionally substituted C1-18 alkylcarbonyloxy, optionally substituted C1-18 alkylsulfonyloxy, optionally substituted arylcarbonyloxy, C1-6 alkyloxy-C1-6 alkyloxy, C1-6 alkyloxy-C1-6 alkyloxy-C1-6 alkyloxy; R8 represents a hydrogen atom; and R13a, R13b, and R13c represent methyl.

Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.

Abstract: The present invention encompasses a therapeutic method which employs treatment of a disease such as cancer with triiodothyronine (T3) together with an anti-thyroid treatment such as treatment with an anti-thyroid agent, treatment with radioiodine and surgical removal of all or part of the thyroid gland. A pharmaceutical composition comprising T3 and an anti-thyroid agent and a kit comprising the same are also encompassed by the invention.

Abstract: The present invention relates to the compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and X are defined as described hereinafter, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the medicaments containing the pharmacologically effective compounds, the preparation thereof and the use thereof.

Abstract: The present invention provides a novel cyclohexane solvate form of lopinavir, and a process for its preparation thereof. The present invention also provides a novel desolvated crystalline form of lopinavir, process for its preparation and to pharmaceutical composition containing it. Thus, for example, lopinavir cyclohexane solvate was heated at 100° C. for 10 hours to give lopinavir desolvated crystalline form H1.

Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of proliferative diseases, as well as to intermediate compounds useful in the preparation of said compounds.

Abstract: A novel network of tumorigenic prognostic factors is identified that plays a critical role in advanced pancreatic cancer (PC) pathogenesis. This interactome is interconnected through a central tumor suppressive microRNA, miR-198, which is able to both directly and indirectly modulate expression of the various members of this network to alter the molecular makeup of pancreatic tumors. When this tumor signature network is intact, miR-198 expression is reduced and patient survival is dismal; patients with higher miR-198 present an altered tumor signature network, better prognosis and increased survival. Further, MiR-198 replacement reverses tumorigenicity in vitro and in vivo. embodiment of the disclosure is a method of treating cancer in an individual, comprising the step of increasing the level of active microRNA-198 molecules in the pancreatic cancer tumor cells of the individual by an amount sufficient to cause an improvement in the pancreatic cancer in the individual.

Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.

Abstract: Compounds of formula (I): wherein R, R1, R2, R3, R4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.

Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.

Abstract: Provided herein are compounds useful for kinase inhibition.

Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.

Abstract: Medical implants are provided which release a fluoropyrimidine or an analog thereof, thereby inhibiting or reducing the incidence of infection associated with the implant.

Abstract: The present invention relates to novel cyclic N,N?-diarylureas and N,N?-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer.

Abstract: Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5, Ra and Rb are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.

Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to 5 compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

Abstract: The present invention is directed to a method of inhibiting aconitase activity of fungal cells in an individual, the method comprising administering an inhibitor of aconitase activity to the fungal cell in an amount effective to inhibit activity of aconitase by said fungal cells.

Abstract: This invention relates to novel fluorouracil derivatives of Formula I or pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a thymidylate synthase inhibitor.

Abstract: The invention is based on the surprising finding that treatment with a chemotherapeutic agent such as 5-fluorouracil (5-FU) and an autophagy inducer effectively inhibit the continued growth of, and prevent the recovery following drug withdrawal, of cancer cells. In vivo, drug resistance from a failure to adequately engage in apoptotic programmed cell death leads to a recurrence of cancer and tumours can remain dormant for periods of time before re-emerging as drug resistant metastases. It has been hypothesised that autophagy (Type II cell death) may help cancer cells survive in response to growth limiting conditions, such as nutrient depletion, hypoxia, absence of growth factor, or presence of cytotoxic drug. LiCl is a known autophagy inducer and accelerates cell survival to autophagic programmed cell death.

Abstract: Compounds of formula I: wherein: R2 is hydrogen or C1-C4alkyl; R3 and R4 are hydrogen, —C(?O)R5, or —C(?O)CHR6—NH2; or R3 is hydrogen and R4 is a monophosphate-, diphosphate-, or triphosphate ester; or R3 is hydrogen, —C(?O)CHR5, or —C(?O)CHR6—NH2 and R4 is each R5 is hydrogen, C1-C6alkyl, or C3-C7cycloalkyl; R6 is hydrogen or C1-C6alkyl; R7 is optionally substituted phenyl; naphthyl; or indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl; or R8 and R8? combined form C3-C7cycloalkyl; R9 is C1-C6alkyl, benzyl, or optionally substituted phenyl; provided that R2, R3 and R4 are not all hydrogen; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations with the compounds I; the use of compounds I, including the compounds of formula I wherein R2, R3 and R4 are all hydrogen, as HCV inhibitors.

Abstract: Provided are methods of treating fibrotic conditions in a subject and diagnostic methods for determining fibrosis and appropriate treatments for the fibrosis by the identification of specific subsets of fibrogenic myofibroblasts.

Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.

Abstract: The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), and an inhibitor of cytochrome P450 (e.g., ritonavir).

Abstract: The present invention relates to a method of treating pancreatic cancer in a subject in need thereof by administering an effective amount of a composition containing (A) tegafur and (B) gimeracil in conjunction with radiotherapy.

Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in modulating lyn kinase activity. In particular, the compounds or a pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder including cardiovascular disease, dyslipidemia, dyslipoproteinemia, a disorder of glucose metabolism, metabolic syndrome (i.e., Syndrome X), a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, type II diabetes, obesity, pancreatitis, hypertension, renal disease, inflammation, or impotence.

Abstract: A controlled release delivery composition comprising: a housing adapted for oral administration; and a plurality of discrete vehicles assembled within the housing, each of the vehicles are not compressed together, each of the vehicles being a bead, a pellet, a tablet, and/or granules compressed into a preselect shape, wherein each of the vehicles comprise a different combination and/or amount of an active agent, an amino acid, a buffer, and a polymer, such that each of the vehicles comprises a different active agent and/or release property from each other, wherein each of the vehicles releases the active agent independently of each other, and wherein each of the vehicles remains independent from each other and intact within the housing prior to oral administration of the delivery composition.

Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].