Abstract: Azidohalogenobenzyl derivatives of the formula (I) ##STR1## wherein A is a halogen atom, B is a halogen atom or a hydrogen atom, and X is a group reactive with a hydroxy group, methods of protecting hydroxy group(s) using said derivatives, and sugar compounds wherein a hydrogen atom of at least one hydroxy group is substituted by an azidohalogenobenzyl group. According to the present invention, there are provided novel derivatives capable of introducing a group into a compound having hydroxy group(s), which group is useful as a stable hydroxy-protecting group even in solid phase synthesis for the purpose of the extension of sugar chain under continuous acidic conditions and of being removed under mild conditions; sugar compounds protected by using said derivatives; and methods of protecting hydroxy group(s) using said derivatives.

Abstract: Reagents and methods for multi-step labeling of nucleic acids allow the addition of relatively insoluble or unstable labels to nucleic acid in the final step. Nucleic acids can be stored as a stable intermediate capable of reacting with a label conjugated to a thiol-reactive group.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: The subject invention, provides arylhydrazone compounds having the Formula 1: ##STR1## wherein A and B are independently aryl or heteroaryl and A and B independently are substituted with at least one group selected from alkyl, halogen, CN, COOR.sup.7, NR.sup.7 R.sup.8, CONR.sup.7 R.sup.8, NO.sub.2, SR.sup.7, SOR.sup.7, SO.sub.2 R.sup.7, NHCOR.sup.7, NHSO.sub.2 R.sup.7, OR.sup.7, hydroxyalkyl, and aminoalkyl. The compounds of this invention are useful for treating a wide variety of bacterial infections, including diseases of the skin, e.g., acne and skin ulcers, gastroenteritis, colitis, meningitis, keratinitis, conjunctivitis, diseases of the urinary and genital tracts, etc.

Abstract: Novel glutamate receptor antagonists represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof, whereinZ is an alicyclic fused ring having 5 to 7 carbon atoms;R.sup.1 is hydrogen, an alkyl or an arylalkyl; andA is O, CH.sub.2, NR.sup.4, CH.sub.2 NR.sup.4, CN, tetrazole or CO wherein R.sup.4 is hydrogen, alkyl, hydroxyalkyl, aminoalkyl or aralkyl, wherein(i) when A is O, CH.sub.2, NR.sup.4 or CH.sub.2 NR.sup.4 then B is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, hydroxyalkyl, alkoxy, aminoalkyl, heterocyclic, alkylheterocyclic, heterocyclic-methyl, heterocyclic-ethyl, alkylcarbonyl, cycloalkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclic-carbonyl, alkylheterocyclic-carbonyl, or when A is NR.sup.4 or CH.sub.2 NR.sup.4 then B is a naturally occurring .alpha.-amino acid moiety joined by an amide bond or B joins with R.sup.4 and the nitrogen to form a four to seven membered heterocyclic ring, provided that when Z is a fused cyclohexyl ring and R.sup.

Abstract: The invention is concerned with novel heterotrifunctional compounds which contain a chemically reactive group R, a photochemically reactive group Ar--N.sup.3 and a reductively cleavable S--S(X.sub.2)-group. The chemically reactive group and the photochemically reactive group are separated by a spacer group which contains a disulfide group. The water-solubilizing groups are carboxylic acids and sulfonic acids or derivatives thereof which are attached either to the aromatic ring or to the spacer group between the aromatic ring and the cleavable SS group. The compounds facilitate a novel photoaffinity method for the labelling of biomolecules, whereby the labelled biomolecule preserves its water solubility and the labelling molecule preferably projects free into the solution after anchorage to the surface of the biomolecule.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

Abstract: Anomeric 2,2-difluororibosyl azide and amine intermediates which are useful for the preparation of 2'-deoxynucleosides, and processes thereto, are provided. Processes for preparing 2'-deoxynucleosides also are provided.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Anomeric 2,2-difluororibosyl azide and amine intermediates which are useful for the preparation of 2'-deoxynucleosides, and processes thereto, are provided. Processes for preparing 2'-deoxynucleosides also are provided.

Abstract: This invention comprises novel compounds that are useful and effective as photoaffinity probes useful for the identification of the biochemical components that form K.sub.ATP channels in smooth muscle cells. The probes are described by the formula below, ##STR1## where R.sub.1 is H, C.sub.1-3 alkyl; R.sub.2 is H, C.sub.1-3 alkyl; orR.sub.1 and R.sub.2 may be joined together to form C.sub.3-6 cycloalkyl, or C.sub.3-6 cycloalkyl optionally substituted with C.sub.1-4 alkyl;R.sub.3 is C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with 1-3 Halogens; or suitable salts thereof.

Abstract: Novel O.sub.10eq -derivatives of ryanodine and dehydroryanodine characterized as binding strongly to ryanodine receptor, useful in affecting Ca.sup.++ efflux in tissue and also in isolating ryanodine receptor from sarcoplasmic reticulum. Also described are novel radio-iodinated alanine derivatives useful to radio label ryanodine and dehydroryanodine derivatives.

Abstract: The invention disclosed relates to a process for producing azide-substituted aromatic polymers such as polysulfones, and to certain novel azide-substituted polysulfones so produced. The process involves attaching azide groups onto the aromatic rings of the polymers by first activating the attachment site by direct lithiation or bromination, followed by lithiation. The lithiated intermediates are converted substantially qantitatively to azides by reacting with a suitable azide, preferably tosyl azide, under substantially anhydrous conditions. Novel azide-substituted polysulfones containing from one to about three azide groups per repeat polymer unit were obtained, the degree of azide substitution being determined by the degree of lithiation. The azides may also be converted to other functional derivatives such as primary amines and cross-linked membranes.

Abstract: A class of halogenated phenylacetonitrile alkylaminoalkylphenyl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula ##STR1## wherein m is a number selected from three to five, inclusive; wherein n one or two; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein each of R.sup.3 through R.sup.

Abstract: The invention concerns a process of preparation of the polyazido alcohols by reaction of a polysubstituted oxirane having in position .beta. a nucleofuge group with a metal nitride, characterized in that the reaction is performed in an aqueous medium.The oxirane formula is: ##STR1## in which X represents a nucleofuge substituent, R1 represents an atom of hydrogen, a lower alkyl group substituted or not by a halogen, an aryl group possibly substituted, R2 and R3 represent an atom of hydrogen, a lower alkyl radical possibly substituted, an aryl group possibly substituted, R4 represents an atom of hydrogen, a lower alkyl group possibly substituted, an aryl group possibly substituted by an alkoxy group. Application to the preparation of polyamino alcohols, ureas, polyazidothiols and binding compositions for propergols.

Abstract: A photosensitive resin having at least one group as shown below in Chemical Formula (1) in a molecule. ##STR1## wherein n represents an integer from 1 to 10. Since the photosensitive resin has an azido group in a molecule having an adsorption region higher than 300 nm, the resin is highly sensitive. Therefore, an emulsion coating photo mask or a soda glass photo mask, which allows light permeation within the abosorption region of the azido group and is cheap in industry, can be used as the photo mask for the photosensitive resin of the invention. The photosensitive resin is particularly useful as a photo resist.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: A process for the preparation of a substituted guanidine by reacting a substituted cyanamide with ammonia or a substituted amine in the presence of a Lewis acid catalyst. Also disclosed is a process for the preparation of a tri-substituted guanidine by reacting a mono-substituted cyanamide with a di-substituted amine.

Abstract: Azido-substituted aromatic amino acids represented by the following formula I are synthesized through the use of tyrosine phenol-lyase. The azido derivatives are suitable for use as photoaffinity labels and inhibitors; ##STR1## wherein R.sup.1 represents a lower alkyl, a lower alkoxy, or an hydroxy group; R.sup.2 and R.sup.3 each independently represent a hydrogen or a lower alkyl group; X represents a hydrogen, a lower alkyl, an alkali metal, or an ammonium group; n is an integer of 0 to 3.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: A radiation sensitive material suitable for the production of radiation sensitive plates for lithographic printing plate manufacture comprises a polymer having appendent azide-substituted aromatic ester groups and sulphonyl urethane groups. The radiation sensitive compound is produced by a process in which some hydroxyl and/or epoxide groups of a polymer are reacted with an azide substituted carboxylic acid or ester forming derivative thereof, and some hydroxyl groups are reacted with a sulphonyl isocyanate.

Abstract: A compound selected from the group consisting of all tautomeric forms of a cycloalky-propanamide of the formula ##STR1## wherein R.sub.1 is cycloalkyl of 3 to 6 carbon atoms, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, azido, --CN, alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, --(CH.sub.2).sub.m --CF.sub.3, --O--(CH.sub.2).sub.m --CF.sub.3, --S--(CH.sub.2).sub.m --CF.sub.3, m is an integer from 0 to 3, --CF.sub.2 --Hal, --OCF.sub.2 --Hal, ##STR2## n is an integer from 1 to 3, Hal, Hal.sub.1, Hal.sub.2 and Hal.sub.3 are individually halogen, and --COR', R' is --OH or alkyl or alkoxy of 1 to 3 carbon atoms or R.sub.4 and R.sub.5 together are --O--CH.sub.2 --O-- and their non-toxic, pharmaceutically acceptable basic salts having anti-inflammatory activity.

Abstract: The present invention provides bifunctional chelating agents comprising a unique substrate reactive moiety incorporated into a carboxymethyl arm of a polyaminopolycarboxylate chelating framework capable of forming stable complexes with metal ions.

Abstract: A photosensitive agent comprising an aromatic diazide compound represented by Formula (I) ##STR1## wherein X denotes ##STR2## Y denotes --CH.dbd.CH--, ##STR3## R.sub.1 is --CH.sub.2 CH.sub.2 --, R.sub.2 --CH.sub.2 CH.sub.3, R.sub.3 is hydrogen, m is 1, and n is 1,R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are individually hydrogen, alkyl, substituted alkyl, aryl, or two of R.sub.6 to R.sub.9 form alkylene groups, provided that R.sub.6 to R.sub.9 are not all hydrogen simultaneouslyand use of the photosensitive agent in a photosensitive composition and in a method forming forming an image.

Abstract: The present invention provides sulphonylphenylalkylamines of the general formula: ##STR1## wherein R.sub.1 is an alkyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3-7 carbon atoms or an aralkyl, aralkenyl or aryl radical, the aryl moiety, in each case, being optionally substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.16 acyl or azide, R.sub.2 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical or an aralkyl or aralkenyl radical, the aryl moiety, in each case, optionally being substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.

Abstract: wherein R.sub.5, R.sub.6, R.sub.7, R.sub.8 which may be the same or different are selected from the group consisting of H, alkyl of 1 to 5 carbon atoms and halogen; whereinn is an integer of 0 to 5m is an integer of 1 to 10p is an integer of 0 to 1a is an integer of 0 to 1b is an integer of 1 to 10,wherein if a is 1 then b is 1, andwherein the moiety ##STR2## includes at least 5 carbon atoms and wherein D is selected from the group consisting of ##STR3## The compounds may be used as intermediates in the preparation of non-radioactive biological probes.

Abstract: Process for the preparation of aryloxy-benzoic acids containing a sulphonamide group by the direct reaction of a phenoxy-benzoic acid with a sulphonamide, in the presence of a halogenating agent such as P(O)Cl.sub.3.

Abstract: 1-Phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.