Abstract: The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention is directed to several newly discovered ecteinascidin (Et) species, designated herein as Et 731, Et 815, Et 808, and Et 594. The physical properties of these compounds, their preparation and therapeutic properties are also reported.

Abstract: Disclosed is a novel compound useful as a constituent of an organic EL device. Also disclosed is a practical organic EL device using this compound. This organic EL device has low driving voltage, long life, and reduced leakage current. Specifically disclosed is a compound characterized by having at least one structure (1) shown below in a molecule.

Abstract: The present invention concerns an intermediate of the following formula (I) in which R1 and R2 represent independently of each other a C1-C12 alkyl group, a (C1-C12 alkoxy)carbonyl group, optionally substituted by one, two or three halogen atom, a (C2-C12 alkenyloxy)carbonyl group, an acyl group, a aryl(C1-C12)alkyl group, an arylalkoxy carbonyl group, a (C1-C12 alkyl)sulfonyl group or an arylsulfonyl group, R3 represents a O-protecting group, R4 and R5 represent independently of each other a hydrogen atom or a O-protecting group, R6 represent a O-protecting group and R7 represent a C1-C12 alkyl group or —OR6 and —OR7 form together a group —OCH2O—. The present invention concerns also a process of preparation of the intermediate and its use for the preparation of Ecteinascidin 743 and Ecteinascidin-770.

Abstract: Disclosed are amide compounds of formula (I): wherein Ar1, Q, Y and R3-R6 of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.

Abstract: The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The ?,?-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores.

Abstract: Methods are provided for preparing a compound with a fused ring structure of formula (XIV) which comprises one or more reactions starting from a 21-cyano compound of formula (XVI) where typically; R1 is an amidomethylene group or an acyloxymethylene group; R5 and R8 are independently chosen from —H, —OH or —OCOCH2OH, or R5 and R8 are both keto and the ring A is a p-benzoquinone ring; R14a and R14b are both —H ozone is —H and the other is —OH, —OCH3 or —OCH2CH3, or R14a and R14b together form a keto group; and R15 and R18 are independently chosen from —H or —OH, or R5 and R8 are both keto and the ring A is a p-benzoquinone ring. In modified starting materials, the 21-cyano group can be replaced by other groups introduced using nucleophilic reagents.

Abstract: Briefly described, embodiments of this disclosure include charge-transport materials, methods of forming charge-transport materials, and methods of using the charge-transport materials.

Abstract: An object of the present invention is to provide a battery which is high in capacity density and superior in stability. An electrode containing a compound having a diazine-N,N?-dioxide structure shown by a general formula (1) described below as an electrode active material is used, where x, y, x?, and y? independently shows integer numbers of 0 or more respectively, and the order of condensation of diazine rings and benzene rings may be alternate or random. One of substituents R1, R2, R3, R4, Ra, Rb, Rc, and Rd shows a part of main chain or side chain of oligomer or polymer, and the other independently shows hydrogen atom, halogen atom, or a specific group.

Abstract: A medicament having inhibitory activity against NF-?B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.

Abstract: The present invention relates to the preparation and pharmacological use of sinomenine derivatives of formula I. The approach disclosed herein is the modification of D ring by-substituting for R. Additional substitutions in the other rings are also provided herein. Several of the sinomenine derivatives have significantly greater anti-inflammation activity when compared with the parent compound.

Abstract: This invention relates to process for preparing fluorinated dyes selected from the group consisting of compounds of the general formulae (I) and (III) and mixtures thereof by reacting the corresponding compounds which do not have R12 or R30 as substituents with compounds of the general formula R12A or R30A where A is selected from the group consisting of I and Br, the compounds obtained from said process and the use of these fluorinated dyes in electrophoretic displays.

Abstract: The invention aims at providing a novel azaaromatic compound having an azafluoranthene skeleton which is useful as the constituent of organic EL devices and at realizing a long lifetime, high-efficiency and practical organic EL device by using the compound in at least one of the organic compound layers.

Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having a 10-membered ring structure which can be converted to a ring of other numbered members.

Abstract: A quinoxalinone derivative of the formula (I): or a pharmaceutically acceptable salt or ester thereof, wherein; X is NH, S or the like; Y is O or the like; the partial structure is, for example, the formula: B1, B2, . . . , Bn?1 and Bn, (in which n is 4, 5 or 6) are each independently CH, N or the like; B?1, B?2, . . . , B?n?1 and B?n (in which n is 4, 5 or 6) are each independently hydrogen or the like; and R is hydrogen, lower alkyl or the like.

Abstract: NLO chromophores of the form of Formula I and the commercially acceptable salts, solvates and hydrates thereof, wherein Z1-4, X1-4, ?1-2, D and A have the definitions provided herein.

Abstract: An objective is to provide an organic thin film transistor material exhibiting an excellent property as a transistor together with reduced aging degradation, and also to provide an organic thin film transistor, a field-effect transistor, a switching element, an organic semiconductor material and an organic semiconductor film employing the organic thin film transistor material. Disclosed is an organic thin film transistor material possessing a compound represented by the following Formula (1). where A composed of a condensed ring formed with a 6 membered aromatic cycle or a 6 membered aromatic heterocycle represents C—R, N or P; at least one of As is N or P; R represents a hydrogen atom, a halogen atom or a substituent; and R may be bonded with other Rs with each other to form a ring.

Abstract: A process for printing an image on a substrate comprising applying to the substrate an ink comprising a compound of Formula (1) or a salt thereof: wherein: R1 and R2 are each independently H or a substituent; each X and Y independently is a substituent; and a and b are each independently 0, 1, 2, 3 or 4. The compounds used in the process have particularly good ozone fastness and are suitable for preparing inks which can be ink jet printed.

Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, d

Abstract: Melanocortin receptor-specific bicyclic compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, R3 X and z are as described in the specification, which are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

Abstract: This invention relates to compounds of the formula: wherein: the substituent groups defined by R1, R2 are each independently selected of H, C(?O)R?, C1–C18 alkyl, C2–C18 alkenyl, C2–C18 alkynyl, or aryl; each of the R? groups is independently selected from the group consisting of H; OH; NO2; NH2; SH; CN; halogen; ?O; C(?O)H; C(?O)CH3; CO2H; or C1–C18 alkyl, C2–C18 alkenyl, C2–C18 alkynyl, or aryl, each of which, independently, may be substituted with one or more substituents selected from the group consisting of halogen, cyano, hydroxy, nitro, azido; alkanoyl, carboxamido, alkyl, alkenyl, alkynyl, aryloxy, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, aminoalkyl, carbocylic aryl having 6 or more carbons, and aralkyl; X2 is OX1 or N(X1)2 wherein each X1 is independently H, C(?O)R? where R? is as defined, C1–C18 alkyl, C2–C18 alkenyl, C2–C18 alkynyl, aryl, alkoxy, heterocyclyl, or two X1 groups together form a cyclic substituent on the nitrogen atom, or X1 is SO2CH3 when X2 is OX1, or N(X1)2 is NHCOalk

Abstract: The present invention provides novel compounds having antiviral activities and antiviral drugs containing the compounds as the active ingredient.

Abstract: An organic electroluminescent material of the formula: wherein M is at least one selected from the group consisting of —CH2—, —CH2CH2—, —CH2CH2CH2—, —CH2C(CH3)2CH2—, and —CH2YCH2—, X is at least one selected from the group consisting of oxygen, sulfur, nitrogen, carbon, alkyl, silicon, silyl, phosphorus, aryl, and polyaryl, and n is depending on the amount of free radicals of X. Y is at least one selected from the group consisting of oxygen, sulfur, nitrogen and SiR1R2. Wherein, R1 and R2 is at least one selected from the group consisting of substituted or unsubstituted alkyl having 1 to 10 carbon atoms, and substituted or unsubstituted aryl having 6 to 30 carbon atoms. This invention also discloses an organic electroluminescent element having the organic electroluminescent material.

Abstract: An electrode including a compound acting as an electrode active material and represented by a general formula (1) having a diazine N,N?-dioxide structure. A novel battery with the higher specific density and the excellent charge and discharge stability can be provided by incorporating the electrode having the compound represented by the general formula (1).

Abstract: Compounds of formula (I): wherein: W1 and W2, together with the carbon atoms to which they are bonded, represent a phenyl group or a pyridyl group, and at least one of the groups W1 or W2 represents a pyridyl group, R1 and R2 each represent a group of formula U-V as defined in the description, X and X1 each represent a hydrogen atom or a hydroxy, alkoxy, mercapto or alkylthio group, Y and Y1 each represent a hydrogen atom, or X and Y, X1 and Y1, together with the carbon atom carrying them, represent a carbonyl or thiocarbonyl group, R4 and R5 are as defined in the description, Q1, Q2 represent a hydrogen atom, or Q1 and Q2, together with the carbon atoms carrying them, form an aromatic bond. Medicaments.

Abstract: In a process for the hydroformylation of ethylenically unsaturated compounds, at least one complex of a metal of transition group VIII. with at least one phosphorus-, arsenic- or antimony-containing compound as ligand is used as hydroformylation catalyst, where the compound used as ligand in each case comprises two groups which comprise a P, As or Sb atom and at least two further hetero atoms and are bound to a xanthene-like molecular framework. New compounds of this type and catalysts which comprise at least one complex of a metal of transition group VIII. with at least one such compound as ligand are also provided.

Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.

Abstract: Disclosed are compounds of the formulas (I) & (II) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds. wherein G, X, A and Q are described herein.

Abstract: An efficient process is described for the synthesis of 5, a key intermediate for the synthesis of the potent antitumor agents ecteinascidin 743 (1) and phthalascidin (2) from the readily available building blocks 3b and 4.

Abstract: A p-type mixture for use in an electronic device including a host including a dihydrophenazine compound, and a dopant provided in the host.

Abstract: The present invention provides monocyclic, bicyclic and oligomeric amine compounds with at least two sites of diversity. These compounds are formed from monocyclic scaffolds which can be cyclized to form bicyclic amine scaffolds. These can then be reacted with building blocks to form the amine compounds of the invention. This invention further provides libraries or monocyclic, bicyclic and oligomeric amine compounds. Also provided are methods for preparing monocyclic, bicyclic and oligomeric amine compounds and libraries thereof. The present invention also provides pharmaceutical compositions of the monocyclic, bicyclic and oligomeric amine compounds.

Abstract: Electron transporting materials and organic light emitting devices utilizing the electron transporting materials, wherein the electron transporting materials are dibenzoquinoxaline compounds, and the devices utilize at least one layer incorporating a dibenzoquinoxaline compound. Dibenzoquinoxaline compounds include dipyridyl substituted dibenzoquinoxaline compounds, diphenyl substituted dibenzoquinoxaline compounds, naphthalene substituted dibenzoquinoxaline compounds, anthrene-dibeanzoquinoxaline compounds, bis(methoxy)phenyl substituted dibenzoquinoxaline compounds, dithiophen-dibenzoquinoxaline compounds, and dibenzoquinoxaline compounds.

Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is COCONH2 or the like; Q1 is a nitrogen atom or C—R4; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; R21 and R22 are hydrogen atoms or the like; X is —CR23R24— or the like wherein R23 and R24 are hydrogen atoms or the like; Y is —CR25R26— or the like wherein R25 and R26 are hydrogen atoms or the like; Z is CH2 or the like; a broken line ( - - - ) represents the presence or absence of a bond, its prodrug, their pharmaceutically acceptable salt, or solvate thereof.

Abstract: Nanotubes having synthetic receptors, and processes for their formation are described. In addition, nanotubes that form complexes with promoters, and processes for forming such complexes are described.

Abstract: Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed: wherein R1 and R4 is H, a C1 to C4 alkyl group, or an acyl group; wherein R2 is an ether, ester, amide, or a phthalimide group; wherein R3 is ═O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R5 is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R6 is ═O, OH, OCH3, CN, or an acyloxy group; wherein R7, is ═O, OH, halogen, an ether group, or an acyl group; wherein R8 and R9 are independently H, CH3, OCH3, OC2H5, CF3, halogen such as Br and F, or R8 and R9 are joined together as a methylenedioxy group, or other five or six membered ring; wherein R10 and R11 are independently CH3, OCH3, OC2H5, SCH3, or SC2H5; wherein R12 is H, a C1 to C4 alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.

Abstract: Antitumour compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from an optionally protected or derivatised aminomethylene group or an optionally protected or derivatised hydroxymethylene group.

Abstract: Compounds having a fused ecteinascidin five ring system with a 1,4 bridge having the structure of formula (VIa or VIb) and compounds in which the —NH2 or —OH of the 1,4 bridge is derivatised are disclosed. Such compounds are useful in the treatment of tumours.

Abstract: The present invention provides novel compounds exemplified by pyrrolic nitrogens used as anion and neutral species recognition elements with an aromatic core as a signal group. Described are methods for the synthesis of various pyrrole aryl compounds as well as various applications for these compounds. Methods of use include the binding and detection of specific analytes in a mixture and, in some examples, the separation of the analyte from the mixture. Additional methods of use include the transport of therapeutic agents and the sensing of components, degradants, and impurities in foodstuffs.

Abstract: Electron transporting materials and organic light emitting devices utilizing the electron transporting materials, wherein the electron transporting materials are dibenzoquinoxaline compounds, and the devices utilize at least one layer incorporating a dibenzoquinoxaline compound. Dibenzoquinoxaline compounds include dipyridyl substituted dibenzoquinoxaline compounds, diphenyl substituted dibenzoquinoxaline compounds, naphthalene substituted dibenzoquinoxaline compounds, anthrene-dibeanzoquinoxaline compounds, bis(methoxy)phenyl substituted dibenzoquinoxaline compounds, dithiophen-dibenzoquinoxaline compounds, and dibenzoquinoxaline compounds.

Abstract: A compound selected from those of formula (I): wherein: R1 and R2, which may be identical or different, represent a group of formula U-V wherein U represents single bond, or alkylene which is optionally substituted and/or unsaturated, and V is as defined in the description, G represents oxygen, or NR3 wherein R3 is as defined in the description, X represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y represents hydrogen, or X+Y represents carbonyl, X1 represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y1 represents hydrogen, or X1+Y1 represents carbonyl, R4, R5, and R6 are as defined in the description, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same are useful in the treatment of cancer.

Abstract: The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NH2, NO2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7 and R8 may be joined into a carbocyclic or heterocyclic ring system; and wherein X1 and X2

Abstract: Compounds of formula A(B)x,  (I) wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group, B is a group of formula  and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R1, R2, R3, R4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.

Abstract: A compound selected from those of formula (I): 1

Abstract: The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NH2, NO2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7 and R8 may be joined into a carbocyclic or heterocyclic ring system; and wherein X1 and X2

Abstract: This invention relates to novel isoxazolines and isoxazoles of formula (I): or a pharmaceutically acceptable salt or prodrug form thereof. The invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: The novel antitumor antibiotics designated stephacidin A and stephacidin B are produced by fermentation of Aspergillus ochraceus ATCC-74432. The antibiotics inhibit the growth of mammalian tumors, including particularly prostate carcinoma.

Abstract: Compounds of formula A(B)x,  (I), wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group, B is a group of formula and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R1, R2, R3, R4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract: A conductive organopolysiloxane composition is provided which includes (A) 100 parts by weight of an organopolysiloxane; and (B) 0.1 to 800 parts by weight of a conductive material obtained by subjecting a member selected from the group consisting of a conductive metal, a conductive metal compound, a filler surface-treated with a conductive metal and a filler surface-treated with a conductive metal compound, to surface treatment with a compound selected from the group consisting of a compound represented by the formula (1) and a compound represented by the formula (2). ##STR1## wherein R.sup.1 represents --O-- or --NH--, and R.sup.2 represents a hydrogen atom or a phenyl group. This composition is useful for the formation of a silicone rubber having a sufficient electrical conductivity and also stably retainable of electrical conductivity almost without undergoing a change in electrical conductivity even in a high-temperature environment.

Abstract: What is claimed is a process for preparing macropolycyclic polyamines of the formula ##STR1## where A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are as defined in the description. These compounds are prepared by a novel improved process by reacting a cyclic amine of the formula ##STR2## with a compound of the formula X--A.sup.2 --Y or X--A.sup.3 --Y where A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are as defined in the description and X and Y are a leaving group.