Abstract: A pyrazolone derivative represented by formula (I) below: wherein R1 to R3 are the same as defined in claims; or an optical isomer, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof is provided. The novel pyrazolone derivative according to the present invention has a PAI-1 production inhibitory activity, a tissue fibrosis inhibitory activity, and a fibrolytic activity, and is effective for preventing and/or treating tissue fibrotic diseases (lung fibrosis, kidney fibrosis, etc.) and diseases of which a pathological thrombus becomes the cause, such as ischemic cardiac diseases (cardiac infarction and angina pectoris), atrial thrombus, lung embolism, deep thrombophlebitis, disseminated intravascular clotting, ischemic brain diseases (brain infarction, brain hemorrhage), and arterial sclerosis.

Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.

Abstract: The present invention relates to novel crystalline modifications of pyraclostrobin, to processes for their preparation and to the use of the novel modifications for preparing crop protection compositions.

Abstract: The present invention relates to compounds of formula (I); and pharmaceutically acceptable salts thereof and individual enantiomers and diastereomers thereof, as GIyT1 inhibitors for treating neurological and psychiatric disorders.

Abstract: To provide pesticides such as insecticides, miticides and nematicides, which are excellent in the safety, pesticidal effects, residual effectiveness, etc., which further have infiltration, and which can be applied by soil treatment. A pesticide comprising a 3-alkoxy-1-phenyl-pyrazole derivative represented by the formula [I] or an agriculturally acceptable salt thereof as an active ingredient: wherein, for example, R1 is a C1-C10 alkyl group or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or the like, and each of R4, R5, R6 and R8 which are independent of one another, is a hydrogen atom or the like, and R7 is a C2-C4 haloalkylthio group or the like.

Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.

Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3-pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO)—, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.

Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.

Abstract: The present invention provides a pyrazole derivative of the general formula (1), which has an excellent efficacy as an active component for a herbicide, an intermediate for the production thereof, processes for the production thereof, and a herbicide containing the derivative as an active ingredient.

Abstract: The invention relates to compounds of formula I having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.

Abstract: The present invention provides a pyrazole compound of formula (a): a noxious arthropod pests controlling composition containing the compound shown by the formula (a) as an active ingredient; and a method for controlling noxious arthropod pests comprising applying an effective amount of the compound shown by the formula (a).

Abstract: The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.

Abstract: The present invention is directed to a compound of formula (I): wherein Ar1, Ar2, Ar3, R1 and T are as defined herein, its preparation, pharmaceutical composition and uses as orexin 2 receptor antagonist.

Abstract: The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I. The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I.

Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

Abstract: The present invention relates to novel crystalline modifications of pyraclostrobin, to processes for their preparation and to the use of the novel modifications for preparing crop protection compositions.

Abstract: Substituted pyrazole compounds such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.

Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.

Abstract: The compounds of formula I: inhibit gamma secretase and hence are of utility in the treatment or prevention of Alzheimer's Disease.

Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R5, R6, R6a, R7, R8, A, B and M are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.

Abstract: This invention relates to novel pyrazole derivatives of formula I wherein R1 to R4 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I and pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient.

Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).

Abstract: The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV infection.

Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.

Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).

Abstract: This invention relates to a novel organophotoreceptor that includes: (a) a charge transport material comprising a fluorenone hydrazone having a) least two fluorenone alkylsulfonylphenylhydrazone groups, b) at least two fluorenone pyrrolylhydrazone groups, c) at least two fluorenone benzotriazolylhydrazone groups, d) at least two fluorenone sulfolanylhydrazone groups, e) at least two fluorenone pyrazolylhydrazone groups, f) at least two fluorenone naphthylhydrazone groups, g) at least two fluorenone tetrazolylhydrazone groups, h) at least two fluorenone stilbenylhydrazone groups, or i) at least two fluorenone (9H-fluoren-9-ylidene)benzylhydrazone groups. Some of these fluoreneones may be represented by the formula where n is an integer between 2 and 6, inclusive; R1 is hydrogen, alkyl, or aryl; R2 is alkylsulfonylphenyl or one of its derivatives; X is a linking group having the formula —(CH2)m—, branched or linear.

Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.

Abstract: Novel benzamidoxime derivatives, processes and intermediates for their preparation and their use as fungicides are described. In the context of the present invention, benzamidoxime derivatives are compounds of the formula I where: A is an aryl or hetaryl radical; Y is a straight-chain or branched C1-C4-alkylene group, where one carbon can be replaced by oxygen, nitrogen or sulfur or by a cyclopropyl group; Rn1 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy; R2 is unsubstituted or substituted phenyl-C1-C6-alkyl, thienyl-C1-C4-alkyl, or pyrazolyl-C1-C4-alkyl, Rp3 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy, C1-C6-alkylcarbonyl; n is 0-5; p is, depending on the number of free valencies, 0-4.

Abstract: Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.

Abstract: The present invention relates to 5-(alkylidene-cycloalkyl)-pyrazoles and 5-(alkylidene-heterocyclyl)-pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, ring G, R1 through R7 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

Abstract: An efficient synthesis of sulfonyl pyrazoles of formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, R1 through R9 are as defined in the specification, comprising reacting a compound of formula II: wherein the ring of the formula (R5)-A-(SOmR4), m R1 through R9 are as defined above and wherein R10 is halo, (C1-C6)alkyl-SO3—, (C6-C10)aryl-SO3—, (C1-C6)alkyl-SO2—, or (C6-C10)aryl-SO2—; wherein each of said (C1-C6)alkyl component of said (C1-C6)alkyl-SO3— and (C1-C6)alkyl-SO2— radicals may optionally be substituted on any carbon atom by one to six fluoro substituents per (C1-C6)alkyl component; with a compound of formula R3—H, wherein R3 is as defined above, in the presence of a fluoride containing salt and in the presence of a solvent.

Abstract: The compound of the formula: wherein Y, X, Z, T and Q are defined in the specification,

Abstract: Compounds of formula (I), particularly a compound of formula (Ia), are non-peptide TPO mimetics, useful in the treatment of thrombocytopenia.

Abstract: The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.

Abstract: The present invention relates to carbamates and urea derivatives of the formula I 1

Abstract: The invention relates to new substituted aromatic amino compounds of the general formula (I) in which R1, R2, R3, R4 and Z have the meanings given in the description, to a process for their preparation, and to their use as herbicides.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The present invention provides novel N-alkyl-N-phenylhydroxylamine derivatives containing metal chelating groups, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species (ROS) and/or excess Zn ions, in particular stroke, Parkinson's disease and Alzheimer's disease. The compounds of the invention possess similar or superior LPO inhibition activity to the reference compounds of Trolox and Ebselen. While showing lower toxicity, they also effectively inhibit the cerebral neuronal cell death caused by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.

Abstract: The present invention discloses novel sulfenate derivatives and their bioconjugates for phototherapy of tumors and other lesions. The sulfenates of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photofragmentation of the sulfenate moiety, with the tissue of interest.

Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.

Abstract: Compounds of the general formula I where the index and the substituents have the following meanings: n is 0 or 1 to 4; X is O or S; Y is a five-membered heteroaromatic ring; R1 is nitro; cyano; halogen; alkyl; haloalkyl; alkoxy; haloalkoxy; alkylthio; phenyl or phenoxy; R2 is hydrogen; alkyl, alkenyl or alkynyl; or a saturatedy,or unsaturated ring which, in addition to carbon atoms, can also contain hetero atoms as ring members are described.

Abstract: The invention relates to novel 1-arylpyrazole oxime derivatives, of general formula (I) or (I bis) 1

Abstract: The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa.

Abstract: Compounds characterized generally as imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension.

Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: The invention is concerned with novel pyrazole derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV mediated process.

Abstract: The invention provides metabolites of the compound 2-amino-N-[2-(3a(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo-[4,3-c]pyridin-5-yl)-1-(R)-benzyl-oxymethyl-2-oxo-ethyl]-isobutyramide, the racemic-diastereomeric mixtures and optical isomers thereof, the prodrugs thereof, and the pharmaceutically acceptable salts of the metabolites, racemic-diastereomeric mixtures, optical isomers, and prodrugs; to pharmaceutical compositions thereof; and to methods of using the metabolites and the compositions in the treatment of diseases associated with reduced levels of growth hormone.

Abstract: A “one-pot” process is described herein for the production of pyrazole compounds of general formula (II) comprising the steps of reacting a compound of general formula (III) with an acylating agent in the presence of a base and an optional activating agent followed by the addition of a hydrazine compound in situ.

Abstract: The invention relates to novel arylpyrazoles of the formula (I): wherein R1, R3, R7, R14, R15, R16, and R17 are as defined in the description, and to their use as pesticides.