C07D417/02

Pharmacophores, compounds and methods having application in the treatment of cancer through inhibition of CYP17A1 and CYP19A1

The invention provides compounds for use as medicaments, which act by inhibiting CYP17A1 and CYP19A1 enzymes. The compounds have particular application in the treatment of cancer especially prostate cancer and breast cancer. The compounds have the formula: [Chem. 1] wherein: R is independently selected from the group consisting of optionally substituted arylamide; optionally substituted alkylarylamide; optionally substituted aryl carboxamide; optionally substituted cyanopiperidine; optionally substituted oxopiperidine; optionally substituted N-(pyridin-3-yl); optionally substituted pyridin-3-yl; optionally substituted pyrazole-4-carboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted 1H-pyrrol-2-ylcarboxamide; optionally substituted morpholin carboxamide; optionally substituted 1H-indazol-3-ylcarboxamide; optionally substituted 5-cyanopiperidin-3-ylcarboxamide; optionally substituted quinolin-7-yl; optionally substituted pyrazin-2-ylcarboxamide; optionally substituted 1H-1,3-benzodiazole-6-carboxamide; and optionally substituted 3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-ylcarboxamide; Each R1, R2, R3, R4, R5 is independently selected from the group consisting of H; OH; a halogen atom; OCH.sub.3; and NH.sub.2; and X is independently selected from the group consisting of O, H and OH. Some of the compounds are claimed per se and the invention also encompasses pharmaceutically acceptable salts, solvates, hydrates, primary metabolites and prodrugs thereof.

Pharmacophores, compounds and methods having application in the treatment of cancer through inhibition of CYP17A1 and CYP19A1

The invention provides compounds for use as medicaments, which act by inhibiting CYP17A1 and CYP19A1 enzymes. The compounds have particular application in the treatment of cancer especially prostate cancer and breast cancer. The compounds have the formula: [Chem. 1] wherein: R is independently selected from the group consisting of optionally substituted arylamide; optionally substituted alkylarylamide; optionally substituted aryl carboxamide; optionally substituted cyanopiperidine; optionally substituted oxopiperidine; optionally substituted N-(pyridin-3-yl); optionally substituted pyridin-3-yl; optionally substituted pyrazole-4-carboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted 1H-pyrrol-2-ylcarboxamide; optionally substituted morpholin carboxamide; optionally substituted 1H-indazol-3-ylcarboxamide; optionally substituted 5-cyanopiperidin-3-ylcarboxamide; optionally substituted quinolin-7-yl; optionally substituted pyrazin-2-ylcarboxamide; optionally substituted 1H-1,3-benzodiazole-6-carboxamide; and optionally substituted 3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-ylcarboxamide; Each R1, R2, R3, R4, R5 is independently selected from the group consisting of H; OH; a halogen atom; OCH.sub.3; and NH.sub.2; and X is independently selected from the group consisting of O, H and OH. Some of the compounds are claimed per se and the invention also encompasses pharmaceutically acceptable salts, solvates, hydrates, primary metabolites and prodrugs thereof.

INDAZOLE CARBOXAMIDES AS KINASE INHIBITORS

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

##STR00001##

Pesticidally active pyrazole derivatives

A compound of formula (II) or formula (III) ##STR00001##
As defined herein.

Substituted heterocycles as harmful arthropod controlling agents

The present invention provides a compound substituted with an excellent control effect against a harmful arthropod, which is represented by formula (I)
Het-Q  (I)
wherein Q represents a group represented by Q1, etc., Het represents a group represented by Het1, etc., R.sup.2 represents a C1-C6 alkyl group, etc., G.sup.1 represents a nitrogen atom or CR.sup.3a, G.sup.2 represents a nitrogen atom or CR.sup.3b, G.sup.3 represents a nitrogen atom or CR.sup.3c, G.sup.4 represents a nitrogen atom or CR.sup.3d, R.sup.3a, R.sup.3b, R.sup.3c, and R.sup.3d are identical to or different from each other and represent a C1-C6 chain hydrocarbon group, etc., n represents 0, 1, or 2, T represents a C1-C10 chain hydrocarbon group substituted with one or more halogen atoms, etc., A.sup.2 represents a nitrogen atom or CR.sup.4a, A.sup.3 represents a nitrogen atom or CR.sup.4b, R.sup.4a and R.sup.4b are identical to or different from each other and represent a C1-C6 chain hydrocarbon group, W.sup.1 represents an oxygen atom, etc., and R.sup.6 represents a C1-C6 chain hydrocarbon group, etc. ##STR00001##

Methods for modifying RNA splicing

Described herein is an intronic recognition element for splicing modifier (iREMS) that can be recognized by a small molecule splicing modifier compound of Formula (I) provided herein or a form thereof, wherein W, X, A and B are as defined herein. In one aspect, methods for modifying RNA splicing to modulate the amount of a product of a gene, wherein a precursor RNA transcript transcribed from the gene that contains an intronic REMS is modified utilizing a splicing modifier compound of Formula (I), are described herein. In another aspect, methods for modifying RNA splicing to modulate the amount of an RNA transcript or protein product encoded by a gene, wherein a precursor RNA transcript transcribed from the gene is modified to comprise an intronic REMS utilizing a splicing modifier compound of Formula (I), are described herein.

Methods for modifying RNA splicing

Described herein is an intronic recognition element for splicing modifier (iREMS) that can be recognized by a small molecule splicing modifier compound of Formula (I) provided herein or a form thereof, wherein W, X, A and B are as defined herein. In one aspect, methods for modifying RNA splicing to modulate the amount of a product of a gene, wherein a precursor RNA transcript transcribed from the gene that contains an intronic REMS is modified utilizing a splicing modifier compound of Formula (I), are described herein. In another aspect, methods for modifying RNA splicing to modulate the amount of an RNA transcript or protein product encoded by a gene, wherein a precursor RNA transcript transcribed from the gene is modified to comprise an intronic REMS utilizing a splicing modifier compound of Formula (I), are described herein.

Probe for a biological specimen and labelling method and screening method using the probe

Provided is a novel probe for a biological specimen for labelling by itself and clearly visualizing one of a specific cell and a specific cell organ in a living body, the probe having excellent spectral characteristics and exhibiting excellent storage stability. The probe for a biological specimen contains, as an active agent, at least one kind of compound represented by a general formula (I). ##STR00001##

DICHROIC DYE COMPOUND, POLARIZING FILM, AND USES THEREOF
20170226071 · 2017-08-10 ·

A compound having a maximum absorption in a wavelength range of 350 nm to 550 nm that functions as a dichroic dye is provided. In particular, a compound represented by formula (1) is provided. In the compound of formula (1), R.sup.1 represents an alkyl group having 1 to 20 carbon atoms or the like; R.sup.2 represents an acyl group having 1 to 20 carbon atoms or the like; R.sup.3 represents a hydrogen atom or the like; and Y represents a group of formula (Y1). In the formula (Y1), * represents a bonding site with N, or a group of formula (Y2). In the formula (Y2), * represents a bonding site with N; P.sup.1 and P.sup.2 each independently represent —S— or the like; and Q.sup.1 and Q.sup.2 each independently represent ═N— or the like.

##STR00001##

DICHROIC DYE COMPOUND, POLARIZING FILM, AND USES THEREOF
20170226071 · 2017-08-10 ·

A compound having a maximum absorption in a wavelength range of 350 nm to 550 nm that functions as a dichroic dye is provided. In particular, a compound represented by formula (1) is provided. In the compound of formula (1), R.sup.1 represents an alkyl group having 1 to 20 carbon atoms or the like; R.sup.2 represents an acyl group having 1 to 20 carbon atoms or the like; R.sup.3 represents a hydrogen atom or the like; and Y represents a group of formula (Y1). In the formula (Y1), * represents a bonding site with N, or a group of formula (Y2). In the formula (Y2), * represents a bonding site with N; P.sup.1 and P.sup.2 each independently represent —S— or the like; and Q.sup.1 and Q.sup.2 each independently represent ═N— or the like.

##STR00001##