Abstract: There are disclosed imidazolinopyrimidinone compounds that have activity to induce TRAIL gene expression in macrophages. There is further disclosed a method for treating various cancers comprising administering effective amounts of an imidazolinopyrimidinone having the structure of Formula I herein.

Abstract: Provided herein is a process and intermediates for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, using cyanamide in the reaction.

Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.

Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.

Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.

Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.

Abstract: This invention relates in one aspect to non-natural desamino alkyl amino acid compounds, methods of making these compounds, and peptides containing these compounds. In one embodiment, the peptide is neurotensin (8-13) in which the N-terminus is an alpha-desamino, alpha-methyl-N,N-dimethyl-homolysine residue of the invention.

Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.

Abstract: The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients.

Abstract: The invention relates to the use of creatine, creatinine and/or derivatives thereof and/or their salts in an agent for hardening, strengthening, restructuring or increasing the shine, volume or combability of keratin fibers, particularly of human hair.

Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.

Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, acute, neuropathic and chronic.

Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic.

Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic.

Abstract: Described herein are novel N-(2 and/or 3-substituted benzyl)-4,5-dihydro-1H-imidazol-2-amine derivatives processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals modulators of subtype ?2B and/or ?2C adrenergic receptors.

Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.

Abstract: A composition that includes aldimines of Formula (I). The composition can be a two-component polyurethane composition. The composition can have a long open time, but build up an early strength quickly, and in the cured state can have high tensile strength and a high modulus of elasticity. The composition can be odorless or at least low-odor before, during and after curing.

Abstract: A class of 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 obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): including a stereoisomer thereof, a tautomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.

Abstract: The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.

Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.

Abstract: The present invention relates to Indanyl- and Tetrahydronaphthyl-amino-azoline compounds of formula I wherein the variables R1 and R2 are as defined in description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites.

Abstract: Disclosed herein is a method of treating motor disorders comprising administering to a subject in need of such treatment an alpha-2 receptor agonist lacking significant alpha-2A receptor activity.

Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.

Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.

Abstract: Cyclocreatine phosphate can be prepared in large quantities from inexpensive starting materials to afford a stable product.

Abstract: Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g.

Abstract: The present invention relates to 1-(imidazolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and their agriculturally acceptable salts, wherein A is a radical of the formula A1 or A2. The invention relates also to agricultural compositions and to seed comprising at least one compound I and/or a salt thereof, as well as a method of combating animal pests, a method for protecting crops from attack or infestation by animal pests and a method for protecting non-living materials from attack or infestation by animal pests, a method for the protection of seeds from animal pests and of the seedlings' roots and shoots from animal pests by applying a pesticidally effective amount of at least one 1-(imidazolin-2-yl)amino-1,2-diphenylethane compound I and/or a salt thereof.

Abstract: The present invention relates to compounds of formula I, wherein X is —CH2— or —NH—; Y is —CH(lower alkoxy)-, —CH(lower alkyl)-, —O—, —S—, —S(O)—, —S(O)2— or —CH2—; and Ar is phenyl or naphthyl, which rings are optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkoxy, lower alkyl and lower alkyl substituted by halogen; or a pharmaceutically-acceptable acid-addition salt thereof; with the proviso that, when X is —NH—, Y is —CH(lower alkyl)- or —CH2—; and the further proviso that the compound is not 2-phenethyl-1H-imidazole hydrochloride, 2-(3,4-dichloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2-chloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2,3-dichloro-phenoxymethyl)-1H-imidazole, benzyl-(1H-imidazol-2-yl)-amine, (4-chloro-benzyl)-(1H-imidazol-2-yl)-amine, or (2-chloro-benzyl)-(1H-imidazol-2-yl)-amine.

Abstract: The invention relates to a method of synthesizing heterocyclic compounds. The invention is characterised in that it consists in opening a compound having formula (I), wherein: —X represents NH, O, S or a N-p group, p being a protective group, such as Boc or Troc; —Y represents N, O, S; —Z represents NH2 or NH-p; and —R1 represents a C1-C6 alkoxy radical, aryloxy, such as phenyloxy, or a pyrrolyl radical, said radicals being optionally substituted, or the salts thereof, and the isomers of the aforementioned compounds. Moreover, the above-mentioned opening step is performed in conditions such as to produce a heterocycle having formula (II), wherein: —X, Y and Z are as defined above; —R2 represents a —CH?CH—CH2—NH—COR1 or —CH?CH—CH2—NH—CO group; and R3 occupies one, two or three positions and represents a halogen. The invention can be used to synthesise natural products.

Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

Abstract: Certain substituted amino heterocyclic and heteroaryl derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein R, R1, R2, R3, R4, A, B and Q are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of an additional compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: Compounds of the formula I, II or III: or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.

Abstract: This invention relates to non-natural desamino amino acid compounds, methods of making, and peptides containing these compounds as their N-terminus moieties. A preferred example is neurotensin (8-13) in which the N terminus is an alpha desamino N,N dimethyl homolysine residue.

Abstract: A method for producing N-(2-amino-1,2-dicyanovinyl)imidates represented by the following formula (1-III) under low temperature conditions within a short period of time in high yield is provided. In addition, a method for producing N-(2-amino-1,2-dicyanovinyl)formamidine represented by the following formula (2-II) which is suitably applicable to a cyclization reaction for producing AICN, AICA or the like and which enhances yield of the cyclization reaction is provided. In addition, a method for producing aminoimidazole derivatives represented by the following formula (3-V) in high yield by using diaminomaleonitrile as a starting material is provided.

Abstract: The present invention generally relates to methods for the preparation of compounds that contain imidazole moieties. In some embodiments, the methods include the reaction of a diamine with a dichloroimmonium compound to produce the imidazole moiety. In some embodiments, the methods are employed to prepare compounds having the Formulas II, II or III below: I II III wherein the constituent variables are as described herein.

Abstract: The present invention provides compounds with activity as inhibitors of acyl glucosaminylinositol amidases with amidase activity against S-conjugate amides, particularly mycothiol-derived S-conjugate amides. Certain of the invention compounds are naturally occurring compounds obtained from marine sponges and other organisms. The invention further provides methods for using the compounds to inhibit virulence and reduce antibiotic resistance of mycothiol-producing bacteria.

Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein Ar, X, m, R1, R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of 5-HT6-mediated diseases.

Abstract: The present invention relates to compounds of formula I wherein X—Y, R1, and n are as defined herein and to their pharmaceutically active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

Abstract: Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT2B receptor.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: The present invention relates to Indanyl- and Tetrahydronaphthyl-amino-azoline compounds of formula I wherein the variables R1 and R2 are as defined in description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites.

Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.

Abstract: Novel substituted 2-aminoimidazoles of formula I, process for their preparation, their use as medicament or diagnostic aid, and medicament containing them.

Abstract: The present invention relates to a two-step process for the preparation of guanidinium salts of the formula (1), where the substituents R have a meaning indicated in Claim, and A? is a sulfonate, alkyl- or arylsulfate, hydrogensulfate, imide, methanide, carboxylate, phosphate, phosphinate, phosphonate, borate, thiocyanate, perchlorate, fluorosilicate or nitrate, and to intermediate compounds from this process.

Abstract: Novel compounds of the formula (I), in which R1, R2, R3, X and Y have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.

Abstract: The present invention relates to 1-(imidazolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and their agriculturally acceptable salts, wherein A is a radical of the formula A1 or A2. The invention relates also to agricultural compositions and to seed comprising at least one compound I and/or a salt thereof, as well as a method of combating animal pests, a method for protecting crops from attack or infestation by animal pests and a method for protecting non-living materials from attack or infestation by animal pests, a method for the protection of seeds from animal pests and of the seedlings' roots and shoots from animal pests by applying a pesticidally effective amount of at least one 1-(imidazolin-2-yl)amino-1,2-diphenylethane compound I and/or a salt thereof.