Abstract: The invention provides a compound of general formula (I) wherein the substituents are defined further in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.

Abstract: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in the application and which can be used in the form of pharmaceutical compositions.

Abstract: Novel compounds, compositions, and kits are provided. Methods of modulating A? levels, and methods of treating a disease associated with aberrant A? levels are also provided.

Abstract: The present invention relates to a compound of formula I and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase.

Abstract: This document discloses molecules having the following formula (“Formula I”):

Abstract: The present invention provides novel sulfone and sulfoxide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and methods of production are provided.

Abstract: The present invention relates to hydroximoyl-tetrazole derivatives, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.

Abstract: The present invention relates to 1-(azolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and to their salts which are useful for combating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a radical of formulae A.1 or A.

Abstract: It is intended to provide an adenosine A2A receptor antagonist containing as an active ingredient a thiazole derivative represented by the general formula (I) [in the formula, R1 represents a substituted or unsubstituted five-membered aromatic heterocyclic group containing at least one oxygen atom, R2 represents a substituted or unsubstituted heterocyclic group, —COR6 (in the formula, R6 represents a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group or the like) or the like, R3 represents the general formula (II), —NHCOR (in the formula, R7 represents —NR8R9 or the like) or the like], or a pharmacologically acceptable salt thereof, etc.

Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.

Abstract: The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

Abstract: 2-Acylaminothiazole-4-carboxamides of the formula (I) and application thereof as an insecticide. wherein R1 represents phenyl which may be optionally substituted, or a 5- or 6-membered heterocyclic group containing at least one hetero atom selected from a group consisting of N, O and S which may be optionally substituted, R2 represents halogen, C1-6 alkyl or C1-6 haloalkyl, R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl or C1-6 haloalkylsulfonyl, R4 represents halogen, C1-6 alkyl or C1-6 haloalkyl, and X represents hydrogen, halogen, C1-6 alkyl or C1-6 haloalkyl, and the use of the new compounds as insecticides.

Abstract: The present invention is concerned with a process for the preparation of 2n-butyl-4-spirocyclopentane-1-[(2?-(tetrazol-5-yl)biphenyl-4-yl)methyl]-2-imidazolin-5-one hydrochloride, irbesartan hydrochloride, novel hydrated and anhydrous crystalline forms thereof, amorphous irbesartan hydrochloride, formulations containing the same, therapeutic uses thereof and methods of treatment employing the same. The process of the present invention is a one-pot process which comprises reacting intermediate compounds 2n-butyl-1,3-diazaspiro[4,4]non-1-en-4-one and 5-(4?-bromomethyl-biphenyl-2-yl)-1-trityl-1H-tetrazole.

Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.

Abstract: The present invention aims to provide a pharmaceutical composition effective for the treatment of cataract. A pharmaceutical composition for the treatment of cataract, containing a VAP-1 inhibitor as an active ingredient, particularly a pharmaceutical composition for the treatment of cataract, containing a compound represented by the formula (I) and the like as an active ingredient: R1—NH—X—Y—Z??(I) wherein each symbol is as defined in the description.

Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and X have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

Abstract: The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).

Abstract: The present invention concerns a compound of formula (I), or a pharmaceutically acceptable salt, or solvate thereof, wherein the groups Ri-Rs are defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.

Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.

Abstract: [Problem] To provide a compound which is useful as a GK activator. [Means for Resolution] As a result of an extensive study on thiazole derivatives, the present inventors have found that a compound having an oxamoyl group, a glycol group or the like on a thiazole ring and a compound having an acetamide group substituted by a bicyclic heteroaryl group such as a quinolyl have a good GK activation effect, and thereby have accomplished the present invention. Since the compounds of the present invention have a good GK activation effect, these are useful as therapeutic agents for diabetes, particularly type II diabetes.

Abstract: The present invention concerns a compound of formula Ia wherein: Ra* is hydrogen or C1-4-alkyl; Rb* is —(C1-C4-alkylene)-Y—C1-4-haloalkyl or —(C1-C4-alkylene)-Y—C1-C4-hydroxyalkyl; Y represents —CONH— or a five membered heteroaryl group.

Abstract: A hair resiliency and body improver comprising as the active ingredient thereof one or more types of compounds selected from the group consisting of 2-aminothiazole derivatives represented by the following general formula (1) or 3-aminoisoxazole derivatives represented by the following general formula (2), and pharmaceutically acceptable salts thereof: (wherein, R1, R2, R3, R4, n and m are as defined in the description).

Abstract: This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.

Abstract: The present invention relates to compounds of formula I and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.

Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.

Abstract: This invention is directed to methods for screening and identification of compounds capable of selectively eliminating cancer cells with specific loss-of-function alterations, including but not limited to mutations, deletions, hypermethylations, and other types of gene silencing. This invention is also directed to novel compounds that selectively eliminate cancer cells with specific loss-of-function alterations. Furthermore, this invention is directed to methods for production and therapeutic use of compounds that selectively eliminate cancer cells with specific loss-of-function alterations.

Abstract: Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes.

Abstract: Disclosed are heterocylic or heteroaryl compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.

Abstract: [Problems] To provide an agent useful for the prevention or treatment of various diseases associated with the infection with acyclovir-resistant viruses of the family Herpesviridae, specifically various infectious caused by herpes viruses, such as varicella associated with varicella-zoster virus infection, herpes zoster associated with recurrent infection with latent varicella-zoster virus, and herpes labialis, herpes encephalitis and genital herpes associated with HSV-1 and HSV-2 infection, and the like. [Means for Solving Problems] An N-[2-[(4-substituted phenyl)amino]-2-oxoethyl]tetrahydro-2H-thiopyran-4-carboxamide derivative in which the phenyl group is substituted at position 4 by a specific 5- or 6-membered heteroaryl group. This derivative has an excellent anti-viral activity against acyclovir-resistant herpes viruses and, therefore, is effective for the treatment of the diseases as mentioned above.

Abstract: The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.

Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and X have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: This invention relates to dicycloalkylcarbamoyl ureas of formula (I), which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.

Abstract: A compound of formula (I), wherein substituents are as given above, useful in the treatment of a disease mediated by the action of CCR3, in particular inflammatory or obstructive airway diseases.

Abstract: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.

Abstract: Compounds of formula (I) wherein R1, R2, R3, and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.

Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.

Abstract: Substituted aryl aminomethyl thiazole ureas and analogues thereof that act as inhibitors of viral capsid formation, including HIV capsid formation, are provided here. Generally the virus capsid formation inhibitors described herein are compounds of Formula I wherein the variables A, R1, R2, R3, R4, X, Y, Z, A5, A6, A7, R8, R9, R12, and R13 are defined herein. Pharmaceutical compositions comprising such compounds and methods of treating animals infected with a virus having a capsid protein are provided herein. Methods of using such compounds to treat human patients infected with an HIV virus and reducing the mortality of AIDS are also provided herein.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: Novel aromatic and heterocyclic thiazolyl thiourea compounds, pharameutical compositions including such, and methods for their use are disclosed. The compounds are effective agents for the treatment of HIV infection, including non-nucleoside inhibitor-resistant, and multi-drug resistant strains of HIV.

Abstract: Disclosed are compounds of formula: and pharmaceutically acceptable salts and esters thereof, useful in treating and/or preventing Alzheimer's disease and other similar diseases, wherein RN, RC, R1, R2 and R20 are defined herein. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: Compounds which are 2-ureido-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group optionally further substituted, selected from: i) straight or branched C1-C6 alkyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R1 is an optionally substituted group selected from: i) straight or branched C1-C6 alkyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R2 is hydrogen, a straight or branched C1-C6 alkyl or C2-C4 alkenyl or alkynyl group; or, taken together with the nitrogen atom so which they are bonded, R1 and R2 form a substituted or unsubstituted group selected from: i) an optionally benzocondensed or bridged 5 to 7 membered heterocycle; or ii) a 9 to 11 membered spiro-heterocyclic compound; or a pharmaceutically acceptab

Abstract: The invention provides compounds of formula 1 wherein R1, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and those affected by dopamine neurotransmission are described.