Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

Abstract: The present invention is directed to novel organometallic complexes as catalysts for the reaction of compounds with isocyanate and hydroxyl functional groups to form urethane and/or polyurethane and the process employing such catalysts. More particularly, the present invention is directed to novel complexes of zinc(II) with substituted amidines. These novel catalysts are useful for the production of urethanes and polyurethanes which are important in many industrial applications.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to 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: There is intended to provide the novel compounds which generate a base easily when irradiated with long wavelength light (active energy rays), a photobase generator containing the compounds and a photobase generation method, and the present invention relates to the compounds represented by the general formula [1], a photobase generator containing the compounds and a photobase generation method: (wherein, Ar represents any of groups with specific structures selected from the group consisting of an anthracenyl group, an anthraquinonyl group and a pyrenyl group; R1 and R2 each independently represent a hydrogen atom or a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, or represent ones which can form an alicyclic ring containing nitrogen atom(s) or an aromatic ring containing nitrogen atom(s) together with a nitrogen atom to which they are bound, which the rings having 3 to 8 carbon atoms which may have a substituent, R3 and R4 each independently represent a hydrogen atom, a linear, branc

Abstract: Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: and intermediates useful for the preparation of I.

Abstract: The invention suggests amphoteric lipids wherein one or more amphoteric groups having an isoelectric point between 4 and 9 are substituted on a membranous or membrane-forming amphiphilic substance, as well as liposomes containing such compounds.

Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.

Abstract: The present invention provides a method for producing a 1-biphenylmethylimidazole compound having superior angiotensin II receptor antagonistic activity, or an intermediate thereof. The present invention provides a method for producing a compound having the formula (5) (R1, Ra: H, an alkyl group) by oxidizing a compound having the formula (1) (Ra: H, an alkyl group) using an oxidizing agent in the presence of a radical initiation reagent, and then reacting with an ammonia-generating reagent and a compound having the formula R1CHO(R1: H, an alkyl group) or a compound having the formula R1C(ORb)3 (R1: H, an alkyl group; Rb: an alkyl group).

Abstract: A radiation-sensitive resin composition includes a compound, a resin and a radiation-sensitive acid generator. The compound has a structure in which a group represented by a following formula (1) is bound to a nitrogen atom. The resin has an acid-dissociative dissolution-controlling group and has a property such that alkali solubility of the resin increases by an action of an acid. In the formula (1), Y is a monovalent group having 5 to 20 carbon atoms, and “*” represents a bonding hand with the nitrogen atom. In the formula (i), R1, R2 and R3 each independently represent a linear or branched alkyl group having 1 to 4 carbon atoms or a monovalent alicyclic hydrocarbon group having 4 to 12 carbon atoms, or R1 and R2 are linked with each other to form a bivalent alicyclic hydrocarbon group, and “*” represents a bonding hand with the oxygen atom.

Abstract: The present invention discloses a process for obtaining 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazole-5-carboxylate by the reaction of 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole, or its hydrolysis product, or its ring-opening product, with alcohol under appropriate catalytic conditions. Furthermore, the present invention also provides a process for obtaining high purity 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole.

Abstract: The invention relates to compositions comprising substituted imidazoline compounds including prodrugs, and salts thereof. In some embodiments, the invention relates to the use of these compositions as therapeutic agents, preferably for the treatment of arthritis or cancer. In further embodiments, The invention relates to the pharmaceutical compositions with effective amounts of substituted imidazoline compounds disclosed herein that function as agonist or antagonists of the genetic expression or interactions with transcription factor NF-?B.

Abstract: Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.

Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

Abstract: The present invention refers to a process for the preparation of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular Midazolam, through an efficient and selective decarboxylation reaction of the derivative compound of the 5-aminomethyl-1-phenyl-1H-imidazole-4-carboxylic acid of formula (II) avoiding the formation of the 6H-imidazo[1,5-a][1,4]benzodiazepines by-products and the ensuing process for the isomerization of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.

Abstract: A new class of imidazolines as 4-position esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma, etc.), antibacterial agents, and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-?B as well as potent activity against the Gram (+) bacterium. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants.

Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.

Abstract: MDM2 and MDM4 proteins prevent apoptosis of cancer cells by negatively regulating the transcription factor p53. Compounds according to Formula I are selective antagonists of MDM2 and MDM4 proteins, disrupting the p53/MDM2 and p53/MDM4 complex. These compounds therefore are candidate therapeutics for treating cancer as well as other cell proliferative disease states.

Abstract: The use of a complex of the form Z—M—OR in the carboxylation of a substrate is described. The group Z is a two-electron donor ligand, M is a metal and OR is selected from the group consisting of OH, alkoxy and aryloxy. The substrate may be carboxylated at a C—H or N—H bond. The metal M may be copper, silver or gold. The two-electron donor ligand may be a phosphine, a carbene or a phosphite ligand. Also described are methods of manufacture of the complexes and methods for preparing isotopically labelled caboxylic acids and carboxylic acid derivatives.

Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.

Abstract: A method for treating Alzheimer's Disease (AD) or Autism Spectrum Disorder (ASD) by administering at least one alky ester of imidazolecarboxylc acid, preferably methyl 4-imidazolecarboxylate. It is hypothesized that the treatment counters AD/ASD by maintaining the intracellular/extracellular osmolyte gradient in the central nervous system (CNS) within a substantially normal range. The methyl 4-imidazolecarboxylate may be administered orally, by inhaler, by injection or by transdermal application. When administered by transdermal application, the dosage range may be from about 0.01 mcg per day to about 3.0 mcg per day, preferably from about 0.1 mcg per day to about 0.3 mcg per day.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to 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 relates to compositions comprising substituted imidazoline compounds including prodrugs, and salts thereof. In some embodiments, the invention relates to the use of these compositions as therapeutic agents, preferably for the treatment of arthritis or cancer. In further embodiments, The invention relates to the pharmaceutical compositions with effective amounts of substituted imidazoline compounds disclosed herein that function as agonist or antagonists of the genetic expression or interactions with transcription factor NF-?B.

Abstract: The present invention discloses a process for obtaining 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazole-5-carboxylate (formula I) by the reaction of 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole (formula II), or its hydrolysis product, or its ring-opening product, with alcohol under appropriate catalytic conditions. Furthermore, the present invention also provides a process for obtaining high purity 4,4-dimethyl-2-propyl-4,6-dihydrofuro[3,4-d]imidazole (formula II), therefore purified compound of formula I can be produced. Producing of olmesartan medoxomil at high purity is assured by said processes. R in formula I is selected from C1-C6 alkyl.

Abstract: The present invention is directed to novel organometallic complexes as catalysts for the reaction of compounds with isocyanate and hydroxyl functional groups to form urethane and/or polyurethane and the process employing such catalysts. More particularly, the present invention is directed to novel complexes of zinc(II) with substituted amidines. These novel catalysts are useful for the production of urethanes and polyurethanes which are important in many industrial applications.

Abstract: Radioactively labeled derivatives of (R)-3-(1-phenylethyl)-3H-imidazole-4-carboxylic acid esters and one-step methods for preparing these compounds are provided. The radioactively labelled compounds, and pharmaceutical acceptable salts and solvates are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET) for the diagnosis of adrenal cortical masses such as incidentaloma, adenoma, primary and metastatic cortical carcinoma. Associated kits and method for PET studies are also provided.

Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

Abstract: The present invention refers to a process for the preparation of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular Midazolam, through an efficient and selective decarboxylation reaction of the derivative compound of the 5-aminomethyl-1-phenyl-1H-imidazole-4-carboxylic acid of formula (II) avoiding the formation of the 6H-imidazo[1,5-a][1,4]benzodiazepines by-products and the ensuing process for the isomerisation of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.

Abstract: There is intended to provide the novel compounds which generate a base easily when irradiated with long wavelength light (active energy rays), a photobase generator containing the compounds and a photobase generation method, and the present invention relates to the compounds represented by the general formula [1], a photobase generator containing the compounds and a photobase generation method: (wherein, Ar represents any of groups with specific structures selected from the group consisting of an anthracenyl group, an anthraquinonyl group and a pyrenyl group; R1 and R2 each independently represent a hydrogen atom or a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, or represent ones which can form an alicyclic ring containing nitrogen atom(s) or an aromatic ring containing nitrogen atom(s) together with a nitrogen atom to which they are bound, which the rings having 3 to 8 carbon atoms which may have a substituent, R3 and R4 each independently represent a hydrogen atom, a linear, branc

Abstract: The invention relates to an innovative method for synthesis of cyclic amidines. The synthesis starts from a ?-, ?- or ?-lactone which is twofold brominated. After esterification of the carboxyl function, the bromine atoms are nucleophilically substituted and the corresponding diamino compound is obtained. The ring closure to the cyclic amidine is accomplished subsequently by reaction with orthoester, imidate or thioimidate. Owing to interposing additional steps for recovery of the diamino compound in enantiomerically pure form, the enantiomers of the cyclic amidines can be stereoselectively synthesized.

Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.

Abstract: The present invention provides a method for producing a 1-biphenylmethylimidazole compound having superior angiotensin II receptor antagonistic activity, or an intermediate thereof. The present invention provides a method for producing a compound having the formula (5) (R1, Ra: H, an alkyl group) by oxidizing a compound having the formula (1) (Ra: H, an alkyl group) using an oxidizing agent in the presence of a radical initiation reagent, and then reacting with an ammonia-generating reagent and a compound having the formula R1CHO(R1: H, an alkyl group) or a compound having the formula R1C(ORb)3 (R1: H, an alkyl group; Rb: an alkyl group).

Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

Abstract: A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-?B as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 ?m/mL.

Abstract: A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-?B as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 ?m/mL.

Abstract: The invention relates to dihydroimidazoles of formula rac-(I), wherein the radicals and symbols are as defined herein; their use as inhibitors of the interaction of the MDM2 protein with a p53-like peptide, new pharmaceutical formulations comprising said compounds, said compounds for use in the therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of proliferative diseases or for the manufacture of pharmaceutical formulations useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide, a pharmaceutical formulation e.g. useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide comprising said compound, methods of treatment comprising administration of said compounds to a warm-blooded animal, and/or processes for the manufacture of said compounds.

Abstract: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone. Finally, the present invention also provides a pharmaceutical composition.

Abstract: The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds, including taxane derivatives, and convergent processes for the preparation of these taxane derivatives and their intermediates.

Abstract: Radioactively labeled derivatives of (R)-3-(1-phenylethyl)-3H-imidazole-4-carboxylic acid esters and one-step methods for preparing these compounds are provided. The radioactively labelled compounds, and pharmaceutical acceptable salts and solvates are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET) for the diagnosis of adrenal cortical masses such as incidentaloma, adenoma, primary and metastatic cortical carcinoma. Associated kits and method for PET studies are also provided.

Abstract: The present invention relates to immunosuppressants, processes for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction. This application relates to compounds selected from Formula (Ia), (Ib), (Ic) and (Id).

Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.

Abstract: The invention relates to compositions comprising substituted imidazoline compounds including prodrugs, and salts thereof. In some embodiments, the invention relates to the use of these compositions as therapeutic agents, preferably for the treatment of arthritis or cancer. In further embodiments, The invention relates to the pharmaceutical compositions with effective amounts of substituted imidazoline compounds disclosed herein that function as agonist or antagonists of the genetic expression or interactions with transcription factor NF-?B.

Abstract: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds and compositions of this invention.

Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.

Abstract: A molten salt and process for preparing a molten salt or hydrogen peroxide uses ionic hydroquinones or hydroquinone derivatives as O2 reduction catalysts.

Abstract: The invention relates to radioactively labeled derivatives of (R)-1-(1-phenylethyl)-1H-imidazole-5-carboxylic acid esters, uses, and methods for preparing these compounds.

Abstract: Compounds derived from phenylethyl imidazole carboxylic acid esters have shown selective accumulation of radioactivity in the adrenal cortex, when labeled with a radioactive halogen. In particular, these compounds bind selectively to adrenocortical tissue facilitating the diagnosis of adrenal cortical masses such as incidentaloma, adenoma, primary and metastatic cortical carcinoma. Trace amounts are injected intravenously and accumulate rapidly in the adrenals, maintaining a high radioactivity plateau, which permits external imaging using computed SPECT (single photon emission) or PET (positron emission) techniques. Independent of the position and type of the radioactive label, the compounds according to the invention are potent inhibitors of steroid P450c11 hydroxylation and bind with high affinity on sites of cortisol secretion. In order to avoid saturation of receptor sites, high specific activity labeling is mandatory for application in patients.

Abstract: A diastereomers of imidazolines as 4-position acids are described. The imidazoline diastereomers potentiate the activity of antitumor drugs and are potent inhibitors of the transcription factor NF-?B.