Abstract: The present invention relates, inter alia, to a process for preparing a compound of formula (I): using, as a catalyst 1,4-diazabicyclo[2.2.2]octane.

Abstract: The present invention relates, inter alia, to a process for preparing a compound of formula (I): using a quinuclidine-based catalyst or an optionally 3-substituted N-methyl pryrrolidine-based catalyst.

Abstract: The present invention relates, inter alia, to a process for preparing a compound of formula (I): which comprises either (a) reacting a compound of formula (II): with 2-cyanophenyl, or a salt thereof, in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane, or (b) reacting a compound of the formula (III): with a compound of the formula (IV): in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane; where W is the methyl (E)-2-(3-methoxy)acrylate group C(CO2CH3)?CHOCH3 or the methyl 2-(3,3-dimethoxy)propanoate group C(CO2CH3)CH(OCH3)2, or a mixture of the two groups. In addition, the present invention relates to a novel precursors of the compound of formula (I) and methods for making them.

Abstract: The present invention relates, inter alia, to a process for preparing a compound of formula (I): using a quinuclidine-based catalyst or an optionally 3-substituted N-methyl pryrrolidine-based catalyst.

Abstract: The present invention relates, inter alia, to a process for preparing a compound of formula (I): using, as a catalyst 1,4-diazabicyclo[2.2.2]octane.

Abstract: The present invention relates, inter alia, to a process for preparing a compound of formula (I): which comprises either (a) reacting a compound of formula (II): with 2-cyanophenyl, or a salt thereof, in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane, or (b) reacting a compound of the formula (III): with a compound of the formula (IV): in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane; where W is the methyl (E)-2-(3-methoxy)acrylate group C(CO2CH3)?CHOCH3 or the methyl 2-(3,3-dimethoxy)propanoate group C(CO2CH3)CH(OCH3)2, or a mixture of the two groups. In addition, the present invention relates to a novel precursors of the compound of formula (I) and methods for making them.

Abstract: The present invention is based on the discovery that when a tooth primordium is inserted into a mammalian jaw and tooth formation follows, new alveolar bone around the new tooth forms. The present invention is based on the idea of stimulating new tooth formation via the implantation of tooth primordia at selected places in the jaw (e.g. at four points in the molar regions) to result in the formation of bony protuberances which could facilitate denture retention. The teeth may then be removed from the jaw of the patient to leave the new alveolar bone.

Abstract: Compounds of general formula (1) are described: 1

Abstract: Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D):  wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12

Abstract: 4,6-Dichloropyrimidine is prepared by treating 4,6-dihydroxypyrimidine with a chlorinating agent of the formula R.sup.1 R.sup.2 R.sup.3 PCl.sub.2 wherein R.sup.1, R.sup.2 and R.sup.3 are independently alkyl or aryl, or one or more of the groups R.sup.1, R.sup.2 and R.sup.3 is linked to a polymer support. Conveniently, the chlorinating agent may be prepared in situ by reacting the corresponding phosphine oxide with phosgene. Thus, in a preferred process, 4,6-dichloropyrimidine is prepared by treating 4,6-dihydroxypyrimidine with phosgene in the presence of a phosphine oxide.

Abstract: Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.5)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.

Abstract: A process for preparing 4,6-dichloropyrimidine is described, comprising treating 4,6-dihydroxypyrimidine with phosphorus oxychloride in the presence of a saturated hindered amine, the hydrochloride salt of a saturated hindered amine, or an unsaturated 5-membered nitrogen containing ring or a mixture thereof, and, as a first step, directly extracting the 4,6-dichloropyrimidine so formed.

Abstract: Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is optionally substituted alkyl; X is --O--, --S-- or --N(R.sup.8)-, where R.sup.8 is hydrogen or alkyl; R.sup.2 is optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 is --(CH.sub.2).sub.n Ar, where Ar is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur and nitrogen atoms, wherein Ar is substituted by an optionally substituted C.sub.3-9 cycloaliphatic group optionally containing one or more heteroatoms selected from oxygen, sulphur or --N(R.sup.8)-, and n is zero or an integer 1, 2 or 3; R.sup.5 is --(CH.sub.2).sub.

Abstract: Compounds of general formula (1): ##STR1## wherein Y is a halogen atom or a group --OR.sup.1 where R.sup.1 is an optionally substituted alkyl group;X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is a hydrogen atom or an alkyl group;R.sup.2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group;R.sup.3 is a hydrogen or halogen atom or an --OR.sup.9 group, where R.sup.9 is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl group, or a formyl, carboxamido or thiocarboxamido group;R.sup.4 is a group --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1,2 or 3;R.sup.5 is a C.sub.3-9 carbocyclic ketone optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms;R.sup.6 is a hydrogen atom or an optionally substituted alkyl group;R.sup.

Abstract: Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.4)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.