Patent classifications
C07D295/22
Process for the synthesis of E1 activating enzyme inhibitors
The present invention provides processes and synthetic intermediate (Ia) for the synthesis of 4-substituted ((1S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates. These sulfamate compounds are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity. ##STR00001##
Process for the synthesis of E1 activating enzyme inhibitors
The present invention provides processes and synthetic intermediate (Ia) for the synthesis of 4-substituted ((1S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates. These sulfamate compounds are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity. ##STR00001##
Polymerizable compound, polymerizable composition, polymer, and optically anisotropic substance
The present invention relates to: a polymerizable compound represented by a formula (I); a polymerizable composition comprising the polymerizable compound and an initiator; a polymer obtained by polymerizing the polymerizable compound or the polymerizable composition; and an optically anisotropic article comprising the polymer [in the formula, Y.sup.1 to Y.sup.8 are a chemical single bond, O, OC(O), C(O)O, or the like; G.sup.1 and G.sup.2 are a divalent aliphatic group having 1 to 20 carbon atoms, or the like; Z.sup.1 and Z.sup.2 are an alkenyl group having 2 to 10 carbon atoms, or the like; A.sup.1 is a tetravalent aromatic group, or the like; A.sup.2 and A.sup.3 are a divalent alicyclic hydrocarbon group having 3 to 30 carbon atoms, or the like; A.sup.4 and A.sup.5 are a divalent aromatic group having 4 to 30 carbon atoms, or the like; A.sup.x1 and A.sup.x2 are an organic group having 2 to 30 carbon atoms that includes an aromatic ring, or the like; A.sup.y1 and A.sup.y2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; Q.sup.1 and Q.sup.2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; and m and n are 0 or 1]. According to the present invention, a polymerizable compound, a polymerizable composition, and a polymer that have a practical low melting point, exhibit excellent solubility in a general-purpose solvent, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and also provide an optically anisotropic article. ##STR00001##
Polymerizable compound, polymerizable composition, polymer, and optically anisotropic substance
The present invention relates to: a polymerizable compound represented by a formula (I); a polymerizable composition comprising the polymerizable compound and an initiator; a polymer obtained by polymerizing the polymerizable compound or the polymerizable composition; and an optically anisotropic article comprising the polymer [in the formula, Y.sup.1 to Y.sup.8 are a chemical single bond, O, OC(O), C(O)O, or the like; G.sup.1 and G.sup.2 are a divalent aliphatic group having 1 to 20 carbon atoms, or the like; Z.sup.1 and Z.sup.2 are an alkenyl group having 2 to 10 carbon atoms, or the like; A.sup.1 is a tetravalent aromatic group, or the like; A.sup.2 and A.sup.3 are a divalent alicyclic hydrocarbon group having 3 to 30 carbon atoms, or the like; A.sup.4 and A.sup.5 are a divalent aromatic group having 4 to 30 carbon atoms, or the like; A.sup.x1 and A.sup.x2 are an organic group having 2 to 30 carbon atoms that includes an aromatic ring, or the like; A.sup.y1 and A.sup.y2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; Q.sup.1 and Q.sup.2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; and m and n are 0 or 1]. According to the present invention, a polymerizable compound, a polymerizable composition, and a polymer that have a practical low melting point, exhibit excellent solubility in a general-purpose solvent, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and also provide an optically anisotropic article. ##STR00001##
6-SUBSTITUTED NAPHTHALENE-1,3-DISULFONIC ACID DERIVATIVES AS MODULATORS OF THE EXTRACELLULAR NICOTINAMIDE PHOSPHORIBOSYL TRANSFERASE (ENAMPT) FOR THE TREATMENT OF E.G. DIABETES
This invention relates to therapeutic 6-substituted naphthalene-1,3-disulfonic acid derivatives of formula (I) (Formula (I)). More specifically, the invention relates to compounds of formula (I) useful as modulators of extracellular nicotinamide phosphoribosyl transferase (eNAMPT) that stabilize the protein in its dimeric form. In addition the invention contemplates pharmaceutical compositions comprising the compounds, processes to prepare the compounds and the compounds for use in methods of medical treatment of e.g. (i) diabetes; (ii) cardiovascular disease; (iii) inflammatory bowel condition; (iv) cancer; (v) liver disease; (vi) inflammatory skin conditions; (vii) lung conditions; (viii) arthritis; (ix) kidney disease (e.g. chronic kidney disease); or (x) sepsis. An exemplary compound is e.g. 6-(2-fluoro-5-((3-(4-(piperidin-1-ylsulfonyl) phenyl) ureido)methyl)phenyl)-4-(trioxidaneylthio) naphthalene-2-sulfonic acid (example 1).
##STR00001##
PROCESS FOR THE SYNTHESIS OF E1 ACTIVATING ENZYME INHIBITORS
The present invention provides processes and synthetic intermediates for the synthesis of 4-substituted ((4S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates, which are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity.
PROCESS FOR THE SYNTHESIS OF E1 ACTIVATING ENZYME INHIBITORS
The present invention provides processes and synthetic intermediates for the synthesis of 4-substituted ((4S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates, which are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity.
POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, POLYMER, AND OPTICALLY ANISOTROPIC SUBSTANCE
The present invention relates to: a polymerizable compound represented by a formula (I); a polymerizable composition comprising the polymerizable compound and an initiator; a polymer obtained by polymerizing the polymerizable compound or the polymerizable composition; and an optically anisotropic article comprising the polymer [in the formula, Y.sup.1 to Y.sup.8 are a chemical single bond, O, OC(O), C(O)O, or the like; G.sup.1 and G.sup.2 are a divalent aliphatic group having 1 to 20 carbon atoms, or the like; Z.sup.1 and Z.sup.2 are an alkenyl group having 2 to 10 carbon atoms, or the like; A.sup.1 is a tetravalent aromatic group, or the like; A.sup.2 and A.sup.3 are a divalent alicyclic hydrocarbon group having 3 to 30 carbon atoms, or the like; A.sup.4 and A.sup.5 are a divalent aromatic group having 4 to 30 carbon atoms, or the like; A.sup.x1 and A.sup.x2 are an organic group having 2 to 30 carbon atoms that includes an aromatic ring, or the like; A.sup.y1 and A.sup.y2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; Q.sup.1 and Q.sup.2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; and m and n are 0 or 1]. According to the present invention, a polymerizable compound, a polymerizable composition, and a polymer that have a practical low melting point, exhibit excellent solubility in a general-purpose solvent, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and also provide an optically anisotropic article.
##STR00001##
POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, POLYMER, AND OPTICALLY ANISOTROPIC SUBSTANCE
The present invention relates to: a polymerizable compound represented by a formula (I); a polymerizable composition comprising the polymerizable compound and an initiator; a polymer obtained by polymerizing the polymerizable compound or the polymerizable composition; and an optically anisotropic article comprising the polymer [in the formula, Y.sup.1 to Y.sup.8 are a chemical single bond, O, OC(O), C(O)O, or the like; G.sup.1 and G.sup.2 are a divalent aliphatic group having 1 to 20 carbon atoms, or the like; Z.sup.1 and Z.sup.2 are an alkenyl group having 2 to 10 carbon atoms, or the like; A.sup.1 is a tetravalent aromatic group, or the like; A.sup.2 and A.sup.3 are a divalent alicyclic hydrocarbon group having 3 to 30 carbon atoms, or the like; A.sup.4 and A.sup.5 are a divalent aromatic group having 4 to 30 carbon atoms, or the like; A.sup.x1 and A.sup.x2 are an organic group having 2 to 30 carbon atoms that includes an aromatic ring, or the like; A.sup.y1 and A.sup.y2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; Q.sup.1 and Q.sup.2 are a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; and m and n are 0 or 1]. According to the present invention, a polymerizable compound, a polymerizable composition, and a polymer that have a practical low melting point, exhibit excellent solubility in a general-purpose solvent, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and also provide an optically anisotropic article.
##STR00001##