Patent classifications
C07C65/26
THERAPY
The invention addresses radioresistance in cancer treatment involving radiotherapy and, in particular, limitations associated with the use of the drug sulfasalazine. Specifically, it provides a series of compounds for use as radiosensitizers in the treatment of cancers such as glioblastomas which are lethal and inherently resistant to radiotherapy. In one embodiment, the invention provides compounds of general formula (I), their stereoisomers and pharmaceutically acceptable salts for use as radiosensitizers in the treatment of cancer:
##STR00001##
wherein ring A is selected from optionally substituted phenyl, biphenyl and fluorenyl; each X is independently selected from: —C.sub.1-6 alkyl (preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), —O—C.sub.1-6 alkyl (preferably —O—C.sub.1-3 alkyl, e.g. —OCH.sub.3), —S—C.sub.1-6 alkyl (preferably —S—C.sub.1-3 alkyl, e.g. —SCH.sub.3), —OH, —SH, —CO.sub.2R.sup.1 (where R.sup.1 is H or C.sub.1-6 alkyl, preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), —SO.sub.2—C.sub.1-6 alkyl (preferably —SO.sub.2—C.sub.1-3 alkyl, e.g. —SO.sub.2—CH.sub.3), —SO.sub.2—NR.sup.2R.sup.3 (where R.sup.2 is H and R.sup.3 is optionally substituted phenyl), —NR.sup.4R.sup.5 (wherein R.sup.4 and R.sup.5 are independently selected from H, C.sub.1-6 alkyl (preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), and —CO—C.sub.1-6 alkyl (preferably —CO—C.sub.1-3 alkyl, e.g. —CO—CH.sub.3), halogen (e.g. F, Cl or Br), and optionally substituted tetrazolyl; n is an integer from 0 to 5, preferably 0 to 2, e.g. 1 or 2; and denotes an E or Z double bond.
METHOD OF MAKING PERFLUOROCYCLOBUTANE-CONTAINING MONOMER
The invention pertains to a multi-step process for making polyfunctional aromatic compounds comprising two phenyl rings bearing reactive groups susceptible of polycondensation reaction to provide polycondensed polymers, said method using economic raw materials, and possessing high selectivity and overall yield.
METHOD OF MAKING PERFLUOROCYCLOBUTANE-CONTAINING MONOMER
The invention pertains to a multi-step process for making polyfunctional aromatic compounds comprising two phenyl rings bearing reactive groups susceptible of polycondensation reaction to provide polycondensed polymers, said method using economic raw materials, and possessing high selectivity and overall yield.
SYNTHETIC RETINOIDS FOR USE IN RAR ACTIVATION
The present invention relates to compounds of formula I: in which A.sup.1-A.sup.7 and R.sup.1 to R.sup.5 are defined herein, for use in the treatment of a condition or disease which is alleviated by the activation of retinoic acid receptors (RAR). The invention also relates to pharmaceutical compounds comprising such compounds, and related methods of treatment. In an aspect, the invention relates to a method of screening compounds for therapeutic potential in the treatment of a condition or disease which is alleviated by the activation of retinoic acid receptors (RAR). Aspects of the invention relate to novel compounds of formula I in which at least one of A.sup.1 to A.sup.3 is or at least one of A.sup.4 is CR.sup.12 or A.sup.5 is CR.sup.13 in which R.sup.12/R.sup.13 is halogen.
SYNTHETIC RETINOIDS FOR USE IN RAR ACTIVATION
The present invention relates to compounds of formula I: in which A.sup.1-A.sup.7 and R.sup.1 to R.sup.5 are defined herein, for use in the treatment of a condition or disease which is alleviated by the activation of retinoic acid receptors (RAR). The invention also relates to pharmaceutical compounds comprising such compounds, and related methods of treatment. In an aspect, the invention relates to a method of screening compounds for therapeutic potential in the treatment of a condition or disease which is alleviated by the activation of retinoic acid receptors (RAR). Aspects of the invention relate to novel compounds of formula I in which at least one of A.sup.1 to A.sup.3 is or at least one of A.sup.4 is CR.sup.12 or A.sup.5 is CR.sup.13 in which R.sup.12/R.sup.13 is halogen.
Process for the preparation of polymorph form B of treprostinil diethanolamine salt
The invention relates to a robust and reproducible process for the preparation of polymorph form B of treprostinil diethanolamine salt, comprising the following steps: a. treprostinil is dissolved in methanol, b. to the solution of step a) diethanolamine or its methanol solution is added, c. the reaction mixture of step b) is agitated till dissolution, d. when salt formation is completed in step c), first portion of an aprotic solvent is added to the solution, e. the solution of step d) is filtered to remove insoluble impurities, f. the filtrate of step e) is seeded with polymorph form B of treprostinil diethanolamine salt, g. to the crystal suspension obtained in step f) a second portion of the aprotic solvent is added, h. the suspension of step g) is agitated until crystallisation is completed, i. the crystals are separated, washed and dried.
Process for the preparation of polymorph form B of treprostinil diethanolamine salt
The invention relates to a robust and reproducible process for the preparation of polymorph form B of treprostinil diethanolamine salt, comprising the following steps: a. treprostinil is dissolved in methanol, b. to the solution of step a) diethanolamine or its methanol solution is added, c. the reaction mixture of step b) is agitated till dissolution, d. when salt formation is completed in step c), first portion of an aprotic solvent is added to the solution, e. the solution of step d) is filtered to remove insoluble impurities, f. the filtrate of step e) is seeded with polymorph form B of treprostinil diethanolamine salt, g. to the crystal suspension obtained in step f) a second portion of the aprotic solvent is added, h. the suspension of step g) is agitated until crystallisation is completed, i. the crystals are separated, washed and dried.
COMPOUND AND LIGHT EMITTING ELEMENT USING SAME
A compound with which the luminance life of a light emitting device is excellent is represented by formula (1):
##STR00001##
n represents an integer of 2 or more and 20 or less, R.sup.1 and R.sup.2 each independently represent a hydrogen atom, an alkyl group, a cycloalkyl group, an alkoxy group, a cycloalkoxy group or a halogen atom. Ar.sup.1 represents a mono-cyclic or condensed-cyclic arylene group, a mono-cyclic or condensed-cyclic divalent heterocyclic group or a group represented by —N(R.sup.X1)—, and R.sup.X1 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or a monovalent heterocyclic group. At least two of Ar.sup.1 represent prescribed groups.
COMPOUND AND LIGHT EMITTING ELEMENT USING SAME
A compound with which the luminance life of a light emitting device is excellent is represented by formula (1):
##STR00001##
n represents an integer of 2 or more and 20 or less, R.sup.1 and R.sup.2 each independently represent a hydrogen atom, an alkyl group, a cycloalkyl group, an alkoxy group, a cycloalkoxy group or a halogen atom. Ar.sup.1 represents a mono-cyclic or condensed-cyclic arylene group, a mono-cyclic or condensed-cyclic divalent heterocyclic group or a group represented by —N(R.sup.X1)—, and R.sup.X1 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or a monovalent heterocyclic group. At least two of Ar.sup.1 represent prescribed groups.
METAL-ORGANIC STRUCTURAL BODY
An object of the present invention is to provide a metal-organic framework capable of adsorbing a gas such as a hydrogen molecule or carbon dioxide at a practical level. The metal-organic framework is used for adsorbing a gas such as hydrogen or carbon dioxide and comprises a multivalent metal ion and a carboxylate ion of formula [I] [wherein in formula [I], X.sup.1 to X.sup.3 each independently represent a functional group of formula [II] (wherein in formula [II], Z is a single bond or a multivalent linking group, k is an integer of 1 to 4, and * is the position at which a bond is formed with a benzene ring); and Y.sup.1 and Y.sup.2 each independently represent a hydrogen atom, a halogeno group, a C1-6 alkyl group or the like, provided that when the multivalent metal ion is a trivalent metal ion, Y.sup.1 and Y.sup.2 each independently represent a halogeno group, a C1-6 alkyl group or the like], wherein the carboxylate ion and the multivalent metal ion are bound to each other.
##STR00001##