Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.

Abstract: The present invention relates to a veterinary or pharmaceutical composition comprising: (i) about 1-65% w/v of a pyrethroid, or a salt thereof, (ii) a macrocyclic lactone, or a salt thereof, (iii) at least one alkalizing agent, (iv) at least one non aqueous solvent, wherein the pH of the composition is comprised between about 6.5 and 8.5, when measured by adding 25% of water to an aliquot of said composition. The invention further relates to the use of such composition for preventing and/or treating parasites infestations.

Abstract: The disclosure provides compounds. In certain embodiments, compounds of the disclosure are capable of inhibiting a mammalian SHMT, such as human SMHT1 and/or SHMT2. Compounds of the disclosure have numerous uses.

Abstract: A method of controlling phytopathogenic diseases on useful plants or on propagation material thereof, which comprises applying to the useful plants, the locus thereof or propagation material thereof a combination of components (A) and (B) in a synergistically effective amount, wherein component (A) is a compound of formula I compound of formula I wherein R is hydrogen or methoxy; Q is R1 is hydrogen, halogen or C1-C6alkyl; R2 is hydrogen, halogen, C1-C6alkyl, C2-C6alkenyl, C3-C6alkinyl, C3-C6cycloalkyl-C3-C6alkinyl, halophenoxy, halophenyl-C3-C6alkinyl, C(C1-C4alkyl)=NO—C1-C4alkyl, C1-C6haloalkyl, C1-C6haloalkoxy, C2-C6haloalkenyl, or C2-C6haloalkenyloxy; R3 is hydrogen, halogen, C1-C6alkyl; R4, R5 and R6, independently from each other, are hydrogen, halogen or —?—R7; with the proviso that at least one of R4, R5 and R6 is different from hydrogen; R7 is hydrogen, C1-C6alkyl, C1-C6haloalkyl or C1-C4alkoxyalkyl; and R8 is hydrogen or methoxy; and agrochemically acceptable salts/isomers/structural is

Abstract: The present disclosure provides the compound having inhibitory property against TNIK having a specific chemical structure or its pharmaceutically acceptable salt. The present disclosure also provides a composition comprising the compound or its pharmaceutically acceptable salt. The present disclosure also provides a medical use of the compound, its salt or the composition comprising the compound or its pharmaceutically acceptable salt for treating or preventing cancer. The present disclosure also provides a method of treatment or prevention of cancer comprising administering the compound, its salt or the composition comprising the compound or its salt to a subject in need of such treatment or prevention.

Abstract: A pyrrolo(pyrazolo)pyrimidine compound of Formula 1, a pharmaceutically acceptable salt, a hydrate, a solvate, a prodrug, and an isomer, and pharmaceutical compositions containing the compound are disclosed. The compound of Formula 1 shows excellent LRRK2 inhibitory activity.

Abstract: The present disclosure relates to methods for treating a variety of diseases and/or ameliorating pain by administering to the ear canal of a subject a composition.

Abstract: An object of the present invention is to provide a methyllactam ring compound that has an SGLT1 inhibitory activity and is useful for a drug, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof. A compound of Formula [I]: or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof is provided.

Abstract: Pyrazole compounds substituted with heteroaryl or pharmaceutically acceptable salts thereof that have an SGLT1 inhibitory activity and are useful for a drug, pharmaceutical compositions comprising the same, and pharmaceutical use thereof are disclosed. Specifically, a compound of Formula [X]: wherein R1 is hydrogen or halogen, R2 is C1-6 alkyl or halo-C1-6 alkyl, Ring Het is substituted pyridyl or optionally substituted pyrazinyl, pyrimidinyl, or pyridazinyl, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof is provided.

Abstract: The present invention relates to an aqueous pesticide microemulsion formulation including (a) at least one organic pesticide compound P, which is sparingly soluble in water and which is present in the formulation in dissolved form; (b) at least one organic solvent LM1 selected from C1-C4-alkyl lactates; (c) at least one organic solvent LM2 selected from C5-C12-alkyl lactates; (d) at least one organic solvent LM3 selected from N—(C4-C12 alkyl)pyrrolidones; (e) at least one surfactant S selected from anionic surfactants and non-ionic surfactants and mixtures thereof; and (f) water.

Abstract: Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same.

Abstract: The present invention relates to a method for the treatment of cancer or an autoimmune disorder, comprising the administration of a serine hydroxymethyltransferase (SHMT) inhibitor, and in particular the administration of pyrazolopyran compounds of Formula (VI) as presently described, wherein the compounds are capable of inhibiting a mammalian SHMT, such as human SHMT1 and/or SHMT2. The treatment method further comprises the optional administration of an additional agent as a rescue therapy to reduce toxicity, wherein said agent may be chosen from formate, a formate salt, folinic acid, formate ester, or leucovorin.

Abstract: This invention is directed to a pharmaceutical composition for drinking water administration comprising isoxazoline compounds of formula (I) and a polysorbate surfactant and diethylene glycol monoethyl ether (transcutol); and the use of the composition to treat or prevent parasite infestations of animals.

Abstract: An indole derivative as expressed by Formula (I), a preparation method thereof, a pharmaceutical salt, and use thereof as a therapeutic agent, especially as a FGFR inhibitor. Each substituent in Formula (I) has identical definition as specified in the specification.

Abstract: Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same.

Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.

Abstract: The invention relates inter alia to halogen-substituted compounds of the general formula (I) in which the A1-A4, T, W, Q, R1 and Z1-Z3 radicals are as defined in the description. Also described are processes for preparing the compounds of the formula (I). The compounds according to the invention are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.

Abstract: Methods for treating a variety of diseases that comprises performing auricular anesthesia of various cranial nerves. A pharmaceutical composition is administered to an ear canal of a subject in need of such treatment, the composition including an analgesic and/or at least one anesthetic. Compositions useful in the taught methods are also provided.

Abstract: A fungicidal composition containing a fungicidally effective amount of a compound of Formula I: (3S,6S,7R,8R)-8-benzyl-3-(3-((isobutyryloxy)methoxy)-4-methoxypicolinamido)-6-methyl-4,9-dioxo-1,5-dioxonan-7-yl isobutyrate, and at least one fungicide selected from the group consisting of fluoxastrobin, trifloxystrobin, and picoxystrobin, provides synergistic control of selected fungi.

Abstract: The present invention relates to a novel crystalline modification of fipronil, to a process for the preparation of the same, to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification and to their use for combating pests and parasites.

Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.

Abstract: Disclosed herein are embodiments of a compound capable of treating HIV. In particular disclosed embodiments, the compound is capable of inhibiting Nef, such as by acting as antagonists of HIV Nef function. Also disclosed are embodiments of a method of making the compound, embodiments of a method of using the compound, and embodiments of a method of identifying HIV Nef antagonists. The disclosed compound may be used alone or in combination with other pharmacologically active agents in order to promote reducing drug resistance and/or cumulative toxicity.

Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.

Abstract: The present invention relates to composition comprising a pesticide and an alkoxylate of the formula (I) as defined below. The invention further relates to said alkoxylate. The invention further relates to a method of preparing said composition by bringing the alkoxylate and the pesticide into contact. Finally, the invention relates to a method of controlling phytopathogenic fungi and/or undesired plant growth and/or undesired insect or mite attack and/or for regulating the growth of plants, wherein said composition is allowed to act on the respective pests, their environment or the crop plants to be protected from the respective pest, on the soil and/or on undesired plants and/or on the crop plants and/or on their environment; and to seed containing said composition.

Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoro ethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.

Abstract: The subject matter disclosed herein is directed to stable, highly-effective topical formulations comprising permethrin, fipronil and a solvent system that is sufficient to solubilize these two active ingredients and limit degradation of fipronil to its sulfone, and their uses in topical applications on animals and the environment. Useful formulations comprise from about 30% to about 55% (w/w) permethrin and about 2 to 15% (w/w) fipronil and a solvent system that comprises N-methyl pyrrolidone and a glycol, glycol ether, glycol ester, fatty acid ester or neutral oil, wherein the N-methyl pyrrolidone and glycol, glycol ether, glycol ester, fatty acid ester or neutral oil are present in a weight:weight ratio of from about 1:2.0 to about 1:3.5, glycol, glycol ether, glycol ester, fatty acid ester or neutral oil to n-methyl pyrrolidone. These two actives when combined in the described amounts have been found to have unexpected enhanced repellent activity against stable fly.

Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoroethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.

Abstract: Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.

Abstract: Provided herein are compounds of the formula (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such pulmonary fibrosis.

Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) prothioconazole and (B) fluxapyroxad and optionally (C) a further fungicidally active compound. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops (e.g. cereals such as wheat, barley, rye, oats, millet and triticale; soya beans; rice; com/maize; oil seed rape including canola; beans, peas, peanuts; sugar beet, fodder beet, beetroot; potatoes; cotton), and to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.

Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I), in which the substituents are as defined in the specification; to compounds of formula (I) for use as androgen receptor modulators. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.

Abstract: The present invention relates to topical bioadhesive formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

Abstract: The present invention relates to pharmaceutical compositions comprising (a) a pharmaceutically effective amount of an mGluR5 positive allosteric modulator, derivative, prodrug or a pharmaceutically acceptable salt thereof; (b) a pharmaceutically effective amount of an agent selected from an NMDA partial agonist or a GlyT1 inhibitor, derivative, prodrug or a pharmaceutically acceptable salt thereof; and (c) a pharmaceutically acceptable carrier. The present invention also relates to methods for treating drug addiction and preventing a drug relapse in a patient.

Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

Abstract: A stable liquid pharmaceutical formulation contains an N-phenylpyrazole derivative, a crystallization inhibitor/viscolizer, and a solvent/co-solvent system including a glycol ether solvent and at least one mono alkyl ester co-solvent; an improved topical veterinary applicator system; and the use of the formulation for the prevention and treatment of infestations with fleas and ticks.

Abstract: Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.

Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.

Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.

Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.

Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.

Abstract: The invention provides saturated acyl guanidine compounds that inhibit F1F0-ATPase, and methods of using saturated acyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.

Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.

Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.

Abstract: A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.

Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.

Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).