Abstract: Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.

Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.

Abstract: The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.

Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

Abstract: The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds.

Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).

Abstract: The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

Abstract: Compounds which exhibit antiviral activity, particularly against influenza virus, and methods of making and using thereof are described herein. In one embodiment, the compounds are heterocyclic amides containing piperazine and isozazole rings and optionally substituted with one or more substituents. The compounds can be formulated with one or more pharmaceutically acceptable excipients to form compositions suitable for enteral or parenteral administration. The compounds are preferably used to treat or prevent Influenza A infections, such as H1N1, H2N2, H3N2, H5N1, H7N7, H1N2, H9N2, H7N2, H7N3, and H10N7.

Abstract: The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.

Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.

Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.

Abstract: Piperazine compounds of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the piperazines of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one piperazine compound of the formula I to act on plants, their seed and/or their habitat.

Abstract: The present invention relates to compounds of formula Ia or Ib below and their tautomers and/or pharmaceutically acceptable salts and compositions and methods of uses thereof.

Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

Abstract: Disclosed herein are a reaction method and a production method of an organic compound which are capable of achieving high reaction selectivity according to the purpose and a high production rate of a target substance. The methods include at least two fluids, wherein at least one kind of the fluids is a fluid containing at least one organic compound and at least one kind of the fluids other than the above fluid is a fluid containing at least one reactant in the form of a liquid or solution, and the respective fluids join together in a thin film fluid foamed between processing surfaces arranged to be opposite to each other so as to be able to approach to and separate from each other, at least one of which rotates relative to the other, whereby an organic reaction is performed in the thin film fluid.

Abstract: A pesticide, particularly an insecticide or an acaricide, including a substituted isoxazoline compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., L is —N(R2c)—, or —CH(R2a)N(R2c)—, etc., X is halogen atom, C1-C6 haloalkyl, etc., Y is halogen atom, C1-C6alkyl, etc., R1 is —C(O)R1a, —C(O)OR1a, —C(O)NHR1a, etc., R2 is hydrogen atom, C1-C6haloalkyl, —C1-C4alkoxy C1-C4alkyl, cyano C1-C6alkyl, C3-C6alkenyl, C3-C6alkynyl, —C(O)R15, —C(O)OR15, etc., R3 is C1-C6haloalkyl, etc., m is an integer of 0 to 5, n is an integer of 0 to 4. The pesticide containing these compounds.

Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.

Abstract: The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.

Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.

Abstract: The present invention relates to the use of compounds with a potentiating effect on the activity of antibiotics that are activatable via the EthA enzymatic pathway, for the preparation of a medicament for preventing and/or treating mycobacterial infections such as tuberculosis and leprosy, to pharmaceutical compositions comprising them in combination with an antibiotic that is activatable via the EthA pathway, to compounds having a potentiating effect on the activity of antibiotics that are activatable via the EthA enzymatic pathway, to pharmaceutical compositions comprising them and to their use as medicaments, especially medicaments for preventing and/or treating mycobacterial infections such as tuberculosis and leprosy.

Abstract: A compound of formula (I) P—W—C(?X)-L-Q??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.

Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq? is H or Rq and Rq? define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl-moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.

Abstract: The present invention relates to new 4-phenyl-1,3-azole derivatives having the general formula (I) wherein R1, R2, R3, R4, X, A, B, and n are variable, in a racemic form, an enantiomeric form or any combinations thereof. These compounds exhibit affinity for cannabinoid receptors and may therefore be used as drugs to treat or prevent pathological states and diseases in which one or more of these receptors are involved. The invention also relates to pharmaceutical compositions containing said products and to the use thereof to prepare a drug.

Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.

Abstract: The present invention aims at providing an isoxazoline derivative and a pharmaceutically acceptable salt thereof, both having an excellent herbicidal effect and an excellent selectivity between crop and weed. The isoxazoline derivative of the present invention is represented by the following general formula: wherein R1 is a haloalkyl group; R2 is a hydrogen atom, an alkyl group, or the like; R3, R4, R5 and R6 are each a hydrogen atom, or the like; Y is a pyrrolyl group, a pyrazolyl group, an isothiazolyl group, an oxazolyl group, an imidazolyl group, a pyridazinyl group, a pyrimidinyl group, a pyrazinyl group, a triazinyl group, a triazolyl group, an oxadiazolyl group, or the like; and n is an integer of 0 to 2.

Abstract: Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.

Abstract: Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Abstract: Compounds of formula (I), and salts and pro-drugs thereof: wherein for example R1 is optionally substituted aryl or heteroaryl; Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain; R2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described.

Abstract: There is provided a FAAH inhibitor and a prophylactic or therapeutic agent for cerebrovascular disorders or sleep disorders comprising it. The prophylactic or therapeutic agent comprises a compound of the formula (I0): wherein Z is oxygen or sulfur; R1 is aryl which may be substituted, or a heterocyclic group which may be substituted; R1a is a hydrogen atom, a hydrocarbon group which may be substituted, hydroxyl, etc.; R2 is piperidin-1,4-diyl which may be substituted, or piperazin-1,4-diyl which may be substituted; R3 is a group formed by eliminating two hydrogen atoms from a 5-membered aromatic heterocyclic group having 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur, which may be further substituted, —CO—, etc.; and R4 is a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; or a salt thereof.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: There is provided compounds having the formula of structure I: wherein the groups —C(R8)(CH2)vCH(R9)(CH2)y-Q and —C(R8)(CH2)vCH(R9)(CH2)y-J are the same, and R1a, R1b, R2a, R2b, R8, R9, J, Q, W, X, L2, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract: Compounds of Formula (I) wherein R1, R2, R3 R4 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.

Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.

Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.

Abstract: Compounds of Formula (I) wherein R1 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Abstract: A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group whic

Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

Abstract: Compounds of Formula I: wherein R1, R2, R3, R4 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.

Abstract: An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.

Abstract: The invention relates to thiazole and pyrazole derivatives of formula (I) wherein Q is S and X is C, or Q is CH and X is N; R1 is unsubstituted or substituted phenyl; and R2 is unsubstituted or substituted aryl or heteroaryl; or a salt of the said compounds, and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour disease, in particular such diseases which respond to an inhibition of the Flt-3 kinase.

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.