Abstract: Processes of forming Csp2—Csp3 bonds at the allylic carbon of a cyclic allylic compound starting material are disclosed, in which a racemic mixture of a cyclic allylic compound having a leaving group attached to the allylic carbon is reacted with a compound having a nucleophilic carbon atom in the presence of a Rh(I), Pd(II) or Cu(I) pre-catalyst and a chiral ligand. The reaction products containing the newly-formed Csp2—Csp3 bond are generated in high stereoisomeric excess, and may therefore serve as important organic building blocks in the preparation of new agrochemicals and pharmaceuticals.

Abstract: The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.

Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

Abstract: The present document describes a cancer mutation-selective chemosensitizer that comprise compounds for restoring association between mutated keap1 protein and Nrf2 protein, and inhibition of Nrf2 functions. The present document also describes composition of matter containing the compounds, as well as methods of medical treatment for treating diseases such as cancer with the compounds.

Abstract: An indicator composition for indicating that an article has undergone an ethylene oxide sterilization process is provided. The indicator composition includes at least one pyridine derivative that reacts with moist ethylene oxide to provide an irreversible color change of the composition.

Abstract: Asymmetric cyanine dyes of Formula I bind nucleic acid but not red blood cell membrane, and function as photosensitizers when rigidly bound but not when free in solution. Unbound dye thus causes minimal oxidative damage. The dyes do not substantially accumulate in red blood cells, thereby minimizing hemolysis due to oxidative damage. Biological fluids can be disinfected by mixing the fluid with these asymmetric cyanine dye that binds to nucleic acid, irradiating the mixture, and recovering clinically significant components from the biological fluid and/or assaying the fluid for pathogens.

Abstract: This invention relates to methods for treating age-related macular degeneration, blindness or glaucoma using an iron-chelator SIH.

Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.

Abstract: The present invention relates to novel antimycobacterial compounds and in particular to antimycobacterial compounds comprised of Schiff base, diacylhydrazine, sulfur-containing diacylhydrazine and oxadiazoline congeners of isonicotinic acid hydrazide. This invention further relates to processes for their preparation, to intermediates useful in their preparation, to their use as therapeutic agents and to pharmaceutical compositions containing them.

Abstract: The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is C1-7 alkyl or C3-7 cycloalkyl; R2 is hydrogen, hydroxy, C1-5 alkyl or —CH2CH2C(═O)NH2; R3 and R4 are independently hydrogen, C1-7 alkyl, —C(═X)—R5, or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one or two selected from a group consisting of halogen, C1-6 alkoxy, nitro, trifluoromethyl, C1-6 alkyl and carboxyl, or R3 and R4 are directly bonded by C3-4 containing oxygen, sulfur or nitrogen to form a heterocyclic ring, X is oxygen, sulfur or NH and R5 is C1-7 alkyl, —NHR6, CONH2 or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one selected from a group consisting of halogen, C1-6 alkoxy, nitrile, trifluoromethyl, C1-6 alkyl and carboxyl, and R6 is hydrogen, hydroxy, NH2, C1-5 alkoxy, C1-5 alkyl, pyridyl or phenyl.

Abstract: The invention relates to a new process for the preparation of chloromethylpyridines of the general formula (I) ##STR1## in which X.sup.1 represents hydrogen, halogen or alkyl,characterized in that pyridine derivatives of the general formula (II) ##STR2## in which R.sup.1 and X.sup.1 have the meaning given in the description,are reacted by means of a formamide derivative of the general formula (III) ##STR3## in which R.sup.2 and R.sup.3 are identical or different and represent alkyl or cycloalkyl or together represent alkanediyl,and with a chlorinating agent, if appropriate in the presence of a diluent, at temperatures between 20.degree. and 120.degree. C. The invention furthermore relates to new pyridine derivatives of the formula (II) and their preparation.

Abstract: A series of novel 1-(phenethyl) and 1-(2-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone.

Abstract: An optically active compound represented by formula (I): ##STR1## wherein R.sup.1 represents an alkyl group having from 6 to 18 carbon atoms or an alkoxy group having from 6 to 18 carbon atoms; A represents ##STR2## or ##STR3## wherein ring ##STR4## represents a nitrogen-containing hetero-aromatic ring; n and m each represents 0 or 1; R.sup.2 represents an alkyl group having from 1 to 12 carbon atoms; and C* is an asymmetric carbon atom. The compound of formula (I) exhibits excellent physicochemical stability, a low temperature range for the chiral smectic C phase when used either alone or in combination with other compounds, and a rapid response.

Abstract: Novel compounds are described which are substituted benzophenone hydrazones. They have pesticidal activity, especially against insects and acarids, and pesticidal compositions and methods are described. Methods of making the compounds, and novel intermediates, are also described.