C07F9/6553

Monophosphine compounds and palladium catalysts based thereon for the alkoxycarbonylation of ethylenically unsaturated compounds

The invention relates to compounds of formula (I) ##STR00001## where R.sup.1 is selected from (C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.12)-cycloalkyl, (C.sub.3-C.sub.12)-heterocycloalkyl; R.sup.2 is selected from (C.sub.3-C.sub.12)-heterocycloalkyl, (C.sub.6-C.sub.20)-aryl, (C.sub.3-C.sub.20)-heteroaryl; R.sup.3 is (C.sub.3-C.sub.20)-heteroaryl; and R.sup.1, R.sup.2 and R.sup.3 may each independently be substituted by one or more substituents selected from (C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.12)-cycloalkyl, (C.sub.3-C.sub.12)-heterocycloalkyl, O(C.sub.1-C.sub.12)-alkyl, O(C.sub.1-C.sub.12)-alkyl-(C.sub.6-C.sub.20)-aryl, O(C.sub.3-C.sub.12)-cycloalkyl, S(C.sub.1-C.sub.12)-alkyl, S(C.sub.3-C.sub.12)-cycloalkyl, COO(C.sub.1-C.sub.12)-alkyl, COO(C.sub.3-C.sub.12)-cycloalkyl, CONH(C.sub.1-C.sub.12)-alkyl, CONH(C.sub.3-C.sub.12)-cycloalkyl, CO(C.sub.1-C.sub.12)-alkyl, COO(C.sub.3-C.sub.12)-cycloalkyl, N[(C.sub.1-C.sub.12)-alkyl].sub.2, (C.sub.6-C.sub.20)-aryl, (C.sub.6-C.sub.20)-aryl-(C.sub.1-C.sub.12)-alkyl, (C.sub.6-C.sub.20)-aryl-O(C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.20)-heteroaryl, (C.sub.3-C.sub.20)-heteroaryl-(C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.20)-heteroaryl-O(C.sub.1-C.sub.12)-alkyl, COOH, OH, SO.sub.3H, NH.sub.2, halogen. The invention further relates to Pd complexes comprising the compound according to the invention and to the use thereof in alkoxycarbonylation.

Ferrocene-based compounds and palladium catalysts based thereon for the alkoxycarbonylation of ethylenically unsaturated compounds

The invention relates to a compound of formula (I) ##STR00001##
where R.sup.1 and R.sup.3 are each a heteroaryl radical having five ring atoms, R.sup.2 and R.sup.4 are each independently selected from (C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.12)-cycloalkyl, (C.sub.3-C.sub.12)-heterocycloalkyl, (C.sub.6-C.sub.20)-aryl; R.sup.1 and R.sup.3 may each independently be substituted by one or more substituents selected from (C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.12)-cycloalkyl, (C.sub.3-C.sub.12)-heterocycloalkyl, O(C.sub.1-C.sub.12)-alkyl, O(C.sub.1-C.sub.12)-alkyl-(C.sub.6-C.sub.20)-aryl, O(C.sub.3-C.sub.12)-cycloalkyl, S(C.sub.1-C.sub.12)-alkyl, S(C.sub.3-C.sub.12)-cycloalkyl, COO(C.sub.1-C.sub.12)-alkyl, COO(C.sub.3-C.sub.12)-cycloalkyl, CONH(C.sub.1-C.sub.12)-alkyl, CONH(C.sub.3-C.sub.12)-cycloalkyl, CO(C.sub.1-C.sub.12)-alkyl, CO(C.sub.3-C.sub.12)-cycloalkyl, N[(C.sub.1-C.sub.12)-alkyl].sub.2, (C.sub.6-C.sub.20)-aryl, (C.sub.6-C.sub.20)-aryl-(C.sub.1-C.sub.12)-alkyl, (C.sub.6-C.sub.20)-aryl-O(C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.20)-heteroaryl, (C.sub.3-C.sub.20)-heteroaryl-(C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.20)-heteroaryl-O(C.sub.1-C.sub.12)-alkyl, COOH, OH, SO.sub.3H, NH.sub.2, halogen; and R.sup.2 and R.sup.4, if they are (C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.12)-cycloalkyl, (C.sub.3-C.sub.12)-heterocycloalkyl or (C.sub.6-C.sub.20)-aryl, may each independently be substituted by one or more substituents selected from (C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.12)-cycloalkyl, (C.sub.3-C.sub.12)-heterocycloalkyl, O(C.sub.1-C.sub.12)-alkyl, O(C.sub.1-C.sub.12)-alkyl-(C.sub.6-C.sub.20)-aryl, O(C.sub.3-C.sub.12)-cycloalkyl, S(C.sub.1-C.sub.12)-alkyl, S(C.sub.3-C.sub.12)-cycloalkyl, COO(C.sub.1-C.sub.12)-alkyl, COO(C.sub.3-C.sub.12)-cycloalkyl, CONH(C.sub.1-C.sub.12)-alkyl, CONH(C.sub.3-C.sub.12)-cycloalkyl, CO(C.sub.1-C.sub.12)-alkyl, CO(C.sub.3-C.sub.12)-cycloalkyl, N[(C.sub.1-C.sub.12)-alkyl].sub.2, (C.sub.6-C.sub.20)-aryl, (C.sub.6-C.sub.20)-aryl-(C.sub.1-C.sub.12)-alkyl, (C.sub.6-C.sub.20)-aryl-O(C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.20)-heteroaryl, (C.sub.3-C.sub.20)-heteroaryl-(C.sub.1-C.sub.12)-alkyl, (C.sub.3-C.sub.20)-heteroaryl-O(C.sub.1-C.sub.12)-alkyl, COOH, OH, SO.sub.3H, NH.sub.2, halogen;
excluding the compounds of the formulae (1) and (2) ##STR00002## The invention further relates to precursors for preparation of the compound according to the invention, to Pd complexes comprising the compound according to the invention and to the use thereof in alkoxycarbonylation.

Dyes with phosphinic acid, phosphinate, phosphonate and phosphonamidate substituents as auxochromic groups and methods for preparing the same

Compounds of formula I are disclosed: ##STR00001##
wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4 are independently H, F, Cl, Br, I, CN, NO.sub.2, OR.sup.1, SR.sup.1, NR.sup.1R.sup.2, COR.sup.1, COOR.sup.1, CONR.sup.1R.sup.2, PO.sub.3R.sup.1R.sup.2, SO.sub.2R.sup.1, SO.sub.3R.sup.1 or R.sup.3; R.sup.1 and R.sup.2 are, e.g., H, alkyl or aryl or optionally a ring; R.sup.3 is, e.g., alkyl, alkenyl, alkynyl, aryl or cycloalkyl; Y is OR.sup.1, NR.sup.1R.sup.2, or NR.sup.1R.sup.3; Q is O, S, SO.sub.2, NR, C(R.sup.3).sub.2, Si(R.sup.3).sub.2, Ge(R.sup.3).sub.2, P(O)R.sup.3 or P(O)OR.sup.3; Q and X.sup.1 can optionally form part of a ring; L and M are independently OR.sup.1, SR.sup.1, NR.sup.1R.sup.2 and R.sup.3; L and M can optionally form part of a ring; Z is O, S, NR.sup.1, CR.sup.1R.sup.3 or aryl; and Z and X.sup.4 can optionally form part of a ring.

TC-PTP inhibitors as APC activators for immunotherapy

The invention encompasses the novel class of compounds represented by the Formula (I) below, which are inhibitors of the TC-PTP enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing TC-PTP mediated diseases, including cancer, via their use in the activation of antigen-presenting cells, like dendritic cells, for applications in the immunotherapeutic treatment of diseases. ##STR00001##

Aminophosphinic derivatives that can be used in the treatment of pain

The present invention relates to a compound of the following general formula (I): R.sub.1NHCH(R.sub.2)P(O)(OR.sub.3)CH.sub.2C(R.sub.4)(R.sub.5)CONHCH(R.sub.6)COOR.sub.7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R.sub.1 represents a C(O)OC(R.sup.8)(R.sup.9)OC(O)R.sup.10 group; R.sub.2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R.sub.3 represents a hydrogen atom or a C(R.sup.12)(R.sup.13)OC(O)R.sup.14 group; R.sub.4 and R.sub.5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R.sub.4 represents a hydrogen atom and R.sub.5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R.sub.6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R.sub.7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, CHMe-COOR.sup.18, CHR.sup.19OC(O)R.sup.20 and CHR.sup.19OC(O)OR.sup.20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more advantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.

PHOSPHINIC PEPTIDE DERIVATIVES FOR USE AS MMP-12 INHIBITORS

This invention relates to compounds that are selective inhibitors of Matrix Metalloprotease-12 (MMP-12), to cosmetic and pharmaceutical compositions containing them, and to their use in the prevention and/or treatment of ailments associated with MMP-12. Formula (I).

##STR00001##

TC-PTP INHIBITORS AS APC ACTIVATORS FOR IMMUNOTHERAPY

The invention encompasses the novel class of compounds represented by the Formula (I) below, which are inhibitors of the TC-PTP enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing TC-PTP mediated diseases, including cancer, via their use in the activation of antigen-presenting cells, like dendritic cells, for applications in the immunotherapeutic treatment of diseases.

##STR00001##

Phosphohistidine and phosphotyrosine analogues

The invention relates to phosphohistidine analogs. The invention also relates to antibodies that specifically bind to the analogs and methods of generating said antibodies. In one embodiment of the invention there is provided a phosphohistidine analog of Formula V: (V) wherein W is selected from H, CO.sub.2H or CONH.sub.2; and X is selected from CH or N. ##STR00001##

Compound having diazatriphenylene ring structure, and organic electroluminescent device

A compound that emits fluorescence and delayed fluorescence is provided as a material for an organic electroluminescent device of high efficiency, and an organic photoluminescent device and an organic electroluminescent device of high efficiency and high luminance are provided using this compound. The compound of a general formula (1) having a diazatriphenylene ring structure is used as a constituent material of at least one organic layer in the organic electroluminescent device that includes a pair of electrodes, and one or more organic layers sandwiched between the pair of electrodes. ##STR00001##

CYCLIC-DISULFIDE MODIFIED PHOSPHATE BASED OLIGONUCLEOTIDE PRODRUGS

This invention relates to a compound comprising a structure of formula (I): cyclic disulfide moiety-phosphorus coupling group (I). The cyclic disulfide moiety has the structure of (C-I), (C-II), or (C-III). This invention also relates to an oligonucleotide comprising one or more compounds that comprise the structure of formula (I), wherein at least one phosphorus coupling group contains a nucleoside or oligonucleotide. The invention also relates to a pharmaceutical composition comprising the oligonucleotide described herein and a method of reducing or inhibiting the expression of a target gene by administering to the subject a therapeutically effective amount of the oligonucleotide described herein.

##STR00001##