Abstract: The present disclosure relates generally to a process for the synthesis of 1,4,7,10-tetraazacyclododecane ligands, chelates, and derivatives thereof. In particular, the present disclosure is directed to a process for the synthesis of 1,4,7,10-tetraaza-1,4,7,10-tetrakis(carboxymethyl)cyclododecane (DOTA) ligands, corresponding DOTA-metal chelates, and various derivatives thereof.

Abstract: The present disclosure relates generally to a process for the synthesis of 1,4,7,10 -tetraazacyclododecane ligands, chelates, and derivatives thereof. In particular, the present disclosure is directed to a process for the synthesis of 1,4,7,10-tetraaza-1,4,7,10-tetrakis(carboxymethyl)cyclododecane (DOTA) ligands, corresponding DOTA-metal chelates, and various derivatives thereof.

Abstract: The use of compounds of formula wherein R2, R3, R4, R5, R6 and R7 have several meanings, for the treatment of disorders mediated by protozoan organisms, novel compounds of the above formula and intermediates for the preparation of such compounds, pharmaceutical compositions comprising such novel compounds, a method of treating disorders mediated by protozoan organisms comprising administering such compounds, optionally together with a second drug substance, to a subject in need thereof and the use of such compounds, whenever comprising a photoaffinity label, for the identification of the molecular target(s) of arylamino alcohol antimalarials.

Abstract: Several different pyrrolysine analogs are disclosed in this application. Those analogs have distinct chemical and biophysical properties. Some analogs are useful in chemical ligation applications. Methods of making and using are also disclosed.

Abstract: The present invention relates to beta-O/S/N fatty acids and derivatives thereof, in particular the compounds of formula (I) as described and defined herein, and their pharmaceutical use, including their use in the treatment or prevention of bacterial as well as protozoan infections, in particular the treatment or prevention of infections with Gram-positive and/or Gram-negative bacteria and infectious diseases caused by and/or related to Gram-positive and/or Gram-negative bacteria. The invention further relates to the use of these compounds for preventing or eliminating biofilms.

Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.

Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.

Abstract: The present invention relates to compounds of formula (I) or (I?), use of these compounds to treat mental disorders, especially depressions of different etiology, and methods for their preparation. The compounds that are provided for the treatment of mental disorders can be presented by a general formula (I) as meso-form—S,2S,1?R,2?R-1-[?-(3,3-dialkyldiaziridin-1-yl)alkyl]-3,3-dialkyldiaziridines: wherein R, X and n are as defined in specification or pharmaceutically acceptable salts thereof, solvates thereof such as hydrates, and pharmaceutical compositions containing such compounds, with the proviso that the compound of Formula (I) is not meso-1S,2S,1?R,2?R-1-[2-(3,3-dimethyldiaziridin-1-yl)ethyl]-3,3-dimethyldiaziridine (R?Me, X?CH2, n=2) (Formula I?).

Abstract: Several different pyrrolysine analogs are disclosed in this application. Those analogs have distinct chemical and biophysical properties. Some analogs are useful in chemical ligation applications. Methods of making and using are also disclosed.

Abstract: The invention provides reagents, methods, and compositions for studying protein-protein interactions. The inventive system and methods allow the analysis of protein-protein interactions in vivo and in vitro. Advantages offered by various embodiments of the inventive system and methods compared to existing photocrosslinking approaches include, for example, (i) novel reversible crosslinking reagents that allow easy isolation, purification, and enrichment of the crosslinked products; (ii) trifluoromethyl phenyldiazirine- or perfluorinated phenylazide-based photocrosslinking reagents that provide high specific labeling, no side product, and higher photocrosslinking efficiency; (iii) versatile spacer groups that allow systematic contact site mapping; (iv) novel methods for isolating, purifying, and detecting crosslinked products based on the reversible-link chemistry; and (v) the ability to study the interaction sites in vitro, in situ, or in vivo.

Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula Ia, or more particularly Formula Ib, or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.

Abstract: The invention relates to compounds of the formula (I), in which X, -Q1-Q2- and RF have the meaning indicated in Claim 1, as ionic liquids, and to a process for the preparation thereof.

Abstract: Disclosed is a polyamine sheet which is usable for DNA chips or protein chips. Also disclosed are a photoreactive polyamine used for producing such a polyamine sheet, and a photoreactive compound which can be a raw material for such a photoreactive polyamine. Specifically disclosed are a photoreactive compound having a diazirine group as a photoreactive group, a photoreactive polyamine compound produced from such a photoreactive compound and a polyamine, a polyamine sheet using such a photoreactive polyamine compound, and a method for producing such a polyamine sheet.

Abstract: The invention provides a method of identifying a peptide or protein capable of binding a ligand which comprises: (i) providing a support, the support comprising a photoreactive group; (ii) reacting the photoreactive group with a ligand to attach the ligand to the support and produce a supported ligand; (iii) providing an expression library comprising a plurality of members, each member expressing a different peptide or protein; (iv) screening the expression library to identify one or more peptides or proteins which bind to the ligand; (v) isolating the member or each member of the library which expresses a peptide or protein which binds to the ligand; and (vi) identifying the peptide or protein which binds to the ligand. Supported photo-reactive compounds are disclosed comprising a photo-reactive group attached to a support via a spacer and a dendritic group, the dendritic group comprising attached thereto, optionally via a spacer, at least one further photo-reactive group and/or a second functional group.

Abstract: The present invention provides branched polyalkylene glycols useful as a chemically modifying agent for physiologically active polypeptides, wherein two single-chain polyalkylene glycols are linked to a group having a cyclic structure other than a plane structure, and wherein a group having reactivity with an amino acid side chain, an N-terminal amino group or a C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity is linked to the group having a structure other than a plane structure.

Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Abstract: Disclosed herein are a cosmetic composition comprising at least one diazirine active-agent compound comprising a diazirine covalently bonded to a cosmetic active agent, said at least one diazirine-active agent compound and the uses of the composition or of the compound, as well as cosmetic treatment processes using the composition or the compound.

Abstract: A sphingomyelin analog represented by the following formula wherein R1 is C1-20 alkyl group, R2 is C1-20 alkyl group, aryl group or C1-6 alkyl group substituted by aryl group, and Z is photoaffinity-labeled group, or its optically active compound.

Abstract: This invention offers a photoreactive labeling reagent consisting of a novel biotinylated phenyldiazirine compound; a photoaffinity labeling reagent consisting of a saccharide-linked biotinylated phenyldiazirine compound where a saccharide compound is introduced into the novel compound; and a novel diazirine compound for such a reagent. The invention covers a biotinylated phenyldiazirine compound of the following formula (II); a phenyldiazirine compound which is an intermediate for synthesizing the above; a saccharide-linked biotinylated phenyldiazirine compound derived from the compound of the formula (II) and a saccharide compound and a method for manufacturing the same; a photoreactive labeling reagent containing the compound of the formula (II); a photoaffinity labeling reagent containing the saccharide-linked biotinylated phenyldiazirine compound; and a method for labeling a saccharide receptor using the reagent.

Abstract: A compound having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R3 is H or OH; wherein R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety. Optically pure enantiomers and salts of the compound are also described. Also, the synthesis of the compound, and uses of the compound, such as in a method for detecting the localization of, or identifying, receptors, enzymes or other targets, whether in a cell or in a subject.

Abstract: The subject invention provides compounds having the structure: 1

Abstract: The present invention provides branched polyalkylene glycols useful as a chemically modifying agent for physiologically active polypeptides, wherein two single-chain polyalkylene glycols are linked to a group having a cyclic structure other than a plane structure, and wherein a group having reactivity with an amino acid side chain, an N-terminal amino group or a C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity is linked to the group having a structure other than a plane structure.

Abstract: A compound having the structure: 1

Abstract: A process for the production of 1,4,7,10-tetraazacyclododecane (cyclene) and its derivatives on an industrial scale comprises cyclotetramerizing of benzylaziridine that is produced in situ.

Abstract: A method for producing a cyclic alkyleneimine, which comprises reacting a cyclic ether with a compound of the formula NH.sub.2 R wherein R is a hydrogen atom or an alkyl group, in a vapor phase in the presence of a solid acid catalyst, wherein the reaction is conducted under a pressure of at least 0.5 kg/cm.sup.2 G as the total pressure of partial pressures of the reactants and the reaction product.

Abstract: Compounds of the formula ##STR1## in which Het represents an optionally substituted aromatic heterocycle having a sulphur or oxygen hetero atom and attached via a ring carbon atom, and X is halogen, alkyl, alkaryl, cyano, alkoxy, mono- or di-alkylamino, acyloxy or aryl, are useful intermediates to a range of cyclopropane derivatives. Processes for their preparation and their use in further synthetic processes are also described.

Abstract: Novel perfluorodiaziridiness having the formula: ##STR1## wherein: R.sup.1 and R.sub.2, alike or different from each other, represent a perfluoroalkyl group of from 1 to 10 carbon atoms, andR.sub.3 represents a fluorine atom, or a perfluoroalkyl group of from 1 to 9 carbon atoms.These perfluorodiaziridines are obtained by reacting perfluoroaminooxaziridines with a source of fluoride ions.

Abstract: Process for preparing N,N'-dialkyldiaziridines or bicyclic diaziridines of the general formula I or II: ##STR1## where R.sup.1 and R.sup.2 are each alkyl or aryl, A is a substituted or unsubstituted one-membered carbon bridge and B is a substituted or unsubstituted three-membered methylene bridge, by reacting a mixture of two moles of a monoamine or one mole of a 1,3-diamine with one mole of an aldehyde or ketone at 25.degree.-70.degree. C., preferably 40.degree.-50.degree. C., while thoroughly mixing with one mole of an aqueous solution of an alkali metal or alkaline earth metal salt of hypochlorous acid and extracting with an organic solvent, preferably chloroform, from the reaction mixture, as well as bicyclic diaziridines which have 1,3-diazabicyclo-[3.1.0]-hexane as basic structure and are prepared using 2,2-dimethyl-1,3-propylenediamine.