Abstract: The present invention relates to the technical field of medicine, and specifically provides methods for preparing Icotinib, Icotinib hydrochloride, and intermediates thereof. These methods avoid the use of phosphorus oxychloride, thereby greatly reducing the emission of pollutants, which is of major benefits to the economy and environment.

Abstract: A crosslinkable, pre-adhesive composition is described comprising an acid-functional (meth)acrylate copolymer and an aziridine crosslinking agent, which when crosslinked provides a pressure-sensitive adhesive and pressure-sensitive adhesive articles.

Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.

Abstract: The invention features oligofluorinated cross-linked polymers and their use in the manufacture of articles and coating surfaces.

Abstract: The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is —O—, —S—, or —NR7—; A is —(CR8R9)—(CH2)m—Z—wherein Z is —(CHR10)—, —C(?O)—, —C(?O)—C(?O)—, —OC(?O)—, —N(R11)C(?O)—, —SO2—, or —N(R11)SO2—; B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 are taken together to form a double bond; R2, R3, and R5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2 and R3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6 is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10, R11 and R12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or subst

Abstract: This invention relates to compositions and methods for achieving the efficient aziridination of organic molecules, especially olefins. More specifically, the invention is directed to a mild, selective, and efficient aziridination protocol that involves catalysis by a mixed-valent dirhodium(II,III) catalyst (Rh25+). Especially preferred sources for forming such mixed-valent dirhodium(II,III) catalyst (Rh25+) are dirhodium(II) carboxamidates, such as dirhodium(II) caprolactamate, and their derivatives and analogues.

Abstract: The present invention relates generally to novel protein modification reagents for fractionation and quantitative (differential) profiling of proteins in a complex mixture. The reagents react with amino acids or other protein components or structures and function as mass tags. The present invention provides methods of making the protein modification reagents and methods of using the protein modification reagents for quantitative analysis of proteins.

Abstract: An isoflavone derivative is provided. The isoxazole derivative has following formula: wherein R1 and R2, independently, include C1-C12 alkyl optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy, and R3 includes hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis including an isoflavone derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Abstract: Described are new 1-aziridino-1-hydroxyiminomethyl derivatives with the general formula (I), wherein R is able to is a single bond or a linker moiety capable of covalently bonding two aziridine oxime groups, R1 and R2 independently of one another are selected from the group consisting of —H, —CH3, —C2H5, —CN, —COOH, —COOCH3, —COOC2H5, —CONH2, or —C6H5 group, and n is the whole number 2, provided that R1 and R2 are not both —H and provided that R1 is not —H if R2 is —CH3 and R1 is not —CH3 if R2 is —H The compounds of general formula (I) show antitumor activity.

Abstract: The present invention relates to a new aziridine derivative that is represented herein by general chemical formulae (Ia) or (Ib), and to their preparation method. In the said chemical formulae, R2 and R3 can be the same or different, and they are hydrogen, low-quality alkyl or cycloalkyl respectively; R4 can be selected among hydrogen, alkyl, aryl, or amino protective group; and amino protective group is, for example, (Ph)3C, and FMOC(9-fluorenylmethyloxycarbonyl), alkoxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl and R5CO, R5SO2 where R5 is alkyl, aryl or aralkyl.

Abstract: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.

Abstract: The invention relates to a process for reducing the monomeric aziridine content in a polyaziridine forming reaction mixture by adding to the polyaziridine forming reaction mixture an excess of a carbodiimide scavenger wherein the excess is based on the equivalent ratio of scavenger to monomeric aziridine, and to a product obtained by this process and to a coating composition containing the product obtained by the process.

Abstract: The merits of N-unsubstituted indoles and cyclopent[b]indoles as DNA-directed reductive alkylating agents are described. These systems represent a significant departure from N-substituted and pyrrolo[1,2-?] fused systems such as the mitomycins and mitosenes. The cyclopent[b]indole-based aziridinylquinone, when bearing an acetate leaving group, was found to be cytotoxic and displayed significant in vivo activity against syngeneic tumor implants. This particular analogue was unexpectedly superior to the others studied, both in terms of high specificity for the activating enzyme DT-diaphorase and in high % DNA alkylation. Alkylation by a quinone methide intermediate as well as by the aziridinyl group were examined for crosslinking. The possible metabolites of the most active indole species were prepared and found to retain cytotoxicity, strongly suggesting that in vivo activity could also be sustained.

Abstract: The present invention relates to a new aziridine derivative that is represented herein by general chemical formulae (Ia) or (Ib), and to their preparation method. In the said chemical formulae, R2 and R3 can be the same or different, and they are hydrogen, low-quality alkyl or cycloalkyl respectively; R4 can be selected among hydrogen, alkyl, aryl, or amino protective group; and amino protective group is, for example, (Ph)3C, and FMOC(9-fluorenylmethyloxycarbonyl), alkoxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl and R5CO, R5SO2 where R5 is alkyl, aryl or aralkyl.

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: The invention relates to a process for reducing the monomeric aziridine content in a polyaziridine forming reaction mixture by adding to the polyaziridine forming reaction mixture an excess of an isocyanate scavenger wherein the excess is based on the equivalent ratio of scavenger to monomeric aziridine, an to a product obtained by this process and to a coating composition containing the product obtained by the process.

Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.

Abstract: The invention provides a composition of greater than 90% pure ethyleneimine dimer and a method of synthesizing the same. This method of synthesis provides several advantages over previous methods: (1) The starting compounds are all relatively inexpensive; (2) the yield of product is greater than 20% of the theoretical yield; and (3) the steps of synthesis are easy, inexpensive and amenable to large-scale production. All of these advantages allow for less expensive production of ethyleneimine dimer.

Abstract: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula 1

Abstract: The invention relates to compounds of the formula 1 1

Abstract: The invention provides a method to synthesizing ethyleneimine dimer. This method of synthesis provides several advantages over previous methods: (1) The starting compounds are all relatively inexpensive; (2) the yield of product is greater than 20% of the theoretical yield; and (3) the steps of synthesis are easy, inexpensive and amenable to large-scale production. All of these advantages allow for less expensive production of ethyleneimine dimer.

Abstract: The present invention relates to the synthesis of chiral cis-aziridines (IIIa and IIIb) by reacting an imine (I) with a diazo compound (II) in the presence of a chiral vaulted biary-Lewis Acid complex as shown below:

Abstract: This invention provides a method for synthesizing ethyleneimine dimer which includes reacting 2-(2-aminoethylamino)ethanol with an aqueous HX solution to produce N-(2-haloethyl)-1,2-ethanediamine dihydrohalide; reacting this product with a base in a solvent to convert the N-(2-haloethyl)-1,2-ethanediamine dihydrohalide into ethyleneimine dimer; and purifying the dimer from the solvent. This method of synthesis provides several advantages over previous methods: (1) The starting compounds are all relatively inexpensive; (2) the yield of the product is greater than 20% of the theoretical yield; and (3) the steps of the synthesis are easy, inexpensive and amenable to large-scale production. All of these advantages allow for less expensive production of ethyleneimine dimer.

Abstract: The invention relates to compounds of the formula The compounds have agreat affinity for the neurotensin receptors.

Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, p, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.

Abstract: Methods for preparing thiophene and pyrrole-based heterocyclic compounds are disclosed. Also disclosed are libraries of thiophene and pyrrole-based heterocyclic compounds, methods for preparing the libraries of thiophene and pyrrole-based heterocyclic compounds, and methods for using the thiophene and pyrrole-based heterocyclic compounds and compound libraries of the invention. The compounds of the invention have biological activity including anti-cancer activity.

Abstract: Disclosed is a photochromic compound having a diaryl-3H-napthopyran structure, which has at the 8-position a nitrogen atom-linked hetercyclus, in which the heterocylcus can also have a HALS compound as a substituent or the heterocyclus itself can be formed as a HALS compound.Furthermore a photochromic compound is described having a diaryl-3H-naphtopyran structure which has at the 8-position an N-atom linked and an alkyl-bridge linked HALS compound.

Abstract: Compounds of formula I ##STR1## wherein R1.dbd.(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2.dbd.H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5.dbd.H, halo, alkyl, alkoxy, etc.; R6,R7.dbd.H, alkyl; R6R7.dbd.atoms to complete a ring; R8,R9.dbd.groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other.dbd.CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8--OH DPAT cue agonism test in rats.

Abstract: The invention relates to compounds of the formula: ##STR1## Compounds of the above formula have a great affinity for the neurotensin receptors.

Abstract: The invention relates to compounds of the formula: ##STR1## The compounds have great affinity for the neurotensin receptors.

Abstract: The present invention relates to novel N-substituted amino alcohols, amino acids and acid derivatives thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: Disclosed are triazole derivatives represented by the following formula, insecticides and acaricides containing the triazole derivatives as active ingredients, and a method of controlling insect pests and mites. ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a halogen atom, 1-pyrrolyl group, a group represented by the formula NR.sup.2 R.sup.3 ; R.sup.5 represents a methyl or ethyl group substituted with at least one halogen atom; n represents 0, 1 or 2; Y represents a nitrogen atom or a group represented by the formula CX.sup.2 ; and X.sup.1 and X.sup.2 are the same or different and each represent a halogen atom, a nitro group or a cyano group.

Abstract: Compounds having the general formula: ##STR1## wherein R.sub.1 is an alkyl or substituted alkyl; R.sub.2 is selected from the group consisting of H and C(O)R.sub.a ; R.sub.3 is selected from the group consisting of H, protecting groups, R.sub.b, and C(O)R.sub.b ; R.sub.4 is selected from the group consisting of H and C(O)R.sub.c, and wherein R.sub.a, R.sub.b, and R.sub.c are independently selected from the group consisting of alkyls, substituted alkyls, alkenyls, alkynyls, aryls, and substituted aryls; provided that R.sub.a is other than phenyl and 3-hydroxyphenyl.

Abstract: A method of manufacturing charge transporting materials which impart a charge transporting property to a polysiloxane resin, and which is soluble in the resin. The charge transporting material is an aromatic substituted tertiary amine with a plurality of aromatic groups, and a silyl group introduced via a hydrocarbon group, into at least one of the aromatic groups. The method is characterized by using an unsaturated aliphatic group bonded to an aromatic group which makes up the silicon-type charge transporting compound, or using a newly bonded unsaturated aliphatic group which is bonded to a silane in which the substituent for silicon is hydrogen or a hydrolyzable group. This is conducted in the presence of a platinum compound as catalyst by means of hydrosilylation. The silicon-type charge transporting material is then brought into contact with an adsorbent for the platinum compound, causing the platinum compound to be adsorbed onto the adsorbent.

Abstract: Diaziridinylpolyamines useful as anti-cancer agents; compositions containing the same, and methods of using the same for the treatment of cancer are described.

Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are compounds substituted at the 3 position of the pyran ring with (i) an aryl substituent and (ii) a phenyl substituent having a 5- or 6-member heterocyclic ring fused at the number 3 and 4 carbon atoms of the phenyl substituent, and at the 6 position of the naphthyl portion of the naphthopyran compound with a nitrogen-containing heterocyclic ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.

Abstract: Compounds of the formula ##STR1## in which R.sup.1, X and Y have the meanings defined herein, and their salts, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and tumors.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: The present invention relates to renin inhibiting compounds of the formula: ##STR1##

Abstract: 4-[3-(benz[b]pyran-4-ylidene)prop-1-enyl]benz[b]pyrylium, 4-[5-(4H-benz[b]pyran-4-ylidene)penta-1,3-dienyl]benz[b]pyrylium and 4-[7-(4H-benz[b]pyran-4-ylidene)hepta-1,3,5-trienyl]benz[b]pyrylium dyes, wherein at least one of the benzpyrylium nuclei carries at its 2-position a substituent in which a non-aromatic carbon atom is bonded directly to the benzpyrylium nucleus, subject to the proviso that if the or each 2-substituent contains an aromatic nucleus, this aromatic nucleus is not conjugated with the benzpyrylium nucleus, are useful as visible and near infra-red absorbers, having high extinction coefficients and a reduced tendency to develop absorptions at shorter wavelengths when dispersed in polymeric media.

Abstract: Avermectin derivatives are disclosed wherein the 4"-hydroxy group is replaced by a substituted alkylthio or acylthio group or an iodo group. These avermectin derivatives can be further derivatized at the 5- and 23-positions as ketoximes or O-substituted ketoximes. The 4"-substituted avermectin derivatives are prepared from the 4"- and 4'-trifluoromethanesulfonyl avermectin derivatives with halo- or sulfur-containing nucleophiles. The 4"- and 4'-.alpha.- and .beta.-trifluoromethane sulfonates are prepared selectively and converted into 4"- or 4'-alkyl- or acylsulfides, or iodides using the appropriate sulfur-containing or iodine nucleophile. Substituted sulfoxy and sulfonyl substituents at the 4"- and 4'-positions are prepared from oxidation of the corresponding substituted sulfides. The new compounds are potent anti-parasitic agents; in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: Substituted cyclohexanols are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.

Abstract: The present invention describes novel tritium labelled nitrogen mustard type compounds, and their aziridinium type analog, and a process for the production of same. The compounds are of value in medical research and development and also as active ingredients of pharmaceutical compositions. The compounds can be used to develop analogs of human disease states and can also be used to evaluate the mechanism of neurotransmitter regulation and function, both in vitro and in vivo.

Abstract: Aziridine and phenethanolamine derivatives of formulae I and II-1 ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower-alkyl; Z.sup.1 is phenyl or a phenyl group substituted in a defined manner; Z.sup.2 and Z.sup.21 are phenyl or thienyl substituted in a defined manner; and, n is an integer from 1-4. The disclosed compounds have catabolic activity and can be used for the treatment of obesity and/or of sugar illnesses. The compounds of formula I are obtained by dehydrating .beta.-aminoalcohols (e.g. those of formula II-1) which, in turn, can be prepared by adding amines to epoxides or by reducing corresponding iminoketones, iminoalcohols a-keto-.beta.-hydroxyamines or .beta.-ketoamines.

Abstract: Perfluoropolyether oligomers or block polymers, having a backbone with one or a plurality of perfluoropolyether segments each consisting essentially of (1) at least one perfluoroisopropyleneoxy unit, (2) a bis(perfluoromethyleneoxy-terminated) unit, and (3) a perfluoroethylidene unit terminating each segment, the backbone of the perfluoropolyether being terminated with COF and/or a functional or nonfunctional derivative thereof, said perfluoropolyethers being made by reacting a perfluoroaliphatic diacid fluoride with hexafluoropropylene epoxide to produce an acid fluoride-terminated perfluoropolyether adduct or oligomer which then can be photopolymerized to yield an acid fluoride-terminated perfluoropolyether block polymer. These oligomers and block polymers are useful as high temperature lubricants, hydraulic fluids, gaskets, adhesives and coatings as well as co-reactants wtih urethane in forming propellant binders.

Abstract: New compounds active in the treatment of ulcers and alergic skin symptoms are prepared by reacting 2-[[5-[(dimethylamino)methyl]furfuryl]thio]ethylmethylsulphide with a suitable compound of formula RH. Said compounds are particularly useful as active principles in pharmaceutical compositions for use in the treatment of affections which require the administration of antagonists for histamine H.sub.2 receptors.

Abstract: The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is —O—, —S—, or —NR7—; A is —(CR8R9)—(CH2)m—Z—wherein Z is —(CHR10)—, —C(?O)—, —C(?O)—C(?O)—, —OC(?O)—, —N(R11)C(?O)—, —O2—, or —N(R11)SO2—; B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 are taken together to form a double bond; R2, R3, and R5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2 and R3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6 is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10, R11 and R12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substi