Patent classifications
C07D311/00
COMPOUNDS FOR SELECTIVE BINDING TO ESTROGEN RECEPTORS ALPHA/BETA RELATIVE TO GPER/GPR30 AND METHODS OF TREATING DISEASE STATES AND CONDITIONS MEDIATED THROUGH THESE RECEPTORS
The current invention is in the field of molecular biology/pharmacology and provides novel 3-oxabicyclo[3.3.1]nonene compounds and derivatives that modulate the effects of the classical estrogen receptors alpha and beta (ERalpha and ERbeta) with little to no biological or physiological effects on the G protein-coupled estrogen receptor GPER (also known as GPR30). These compounds may function as agonists and/or antagonists of one or more of the disclosed classical estrogen receptors. Diseases that are mediated through one or more of these receptors include cancer (including but not limited to breast (particularly endocrine or anti-hormone resistant, and for the prevention/reduction of endocrine or anti-hormone resistance), reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometritis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disorders (such as Parkinson's disease and Alzheimer's disease), as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine, among numerous others as described herein. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.
Heavy metal ion-hematein-complexes useful as ex vivo contrast agent for a computed tomography scanning of a biological sample, ex vivo method for investigating a biological sample, and use of the complexes
The present invention relates to specific complexes comprising heavy metal ions having an atomic number of 23 or higher and 83 or lower (in particular Ag.sup.1+, Ba.sup.2+, Pb.sup.2+, Gd.sup.3+ and Bi.sup.3+) and one or more hematein ligand(s). In particular, the invention relates to the use of the complexes as ex vivo contrast agents for a computed tomography scanning of a biological sample. Moreover, the invention relates to specific ex vivo methods for investigating a biological sample by means of computed tomography scanning methods, wherein the method comprises staining the biological sample with a solution comprising one or more of the complex(es); or wherein the method comprises staining the biological sample with a staining solution comprising hematein, and separately contacting the biological sample with one or more staining solution(s) comprising one or more heavy metal ions having an atomic number of 23 or higher and 83 or lower (in particular Ag.sup.1+, Ba.sup.2+, Pb.sup.2+, Gd.sup.3+ and Bi.sup.3+).
Heavy metal ion-hematein-complexes useful as ex vivo contrast agent for a computed tomography scanning of a biological sample, ex vivo method for investigating a biological sample, and use of the complexes
The present invention relates to specific complexes comprising heavy metal ions having an atomic number of 23 or higher and 83 or lower (in particular Ag.sup.1+, Ba.sup.2+, Pb.sup.2+, Gd.sup.3+ and Bi.sup.3+) and one or more hematein ligand(s). In particular, the invention relates to the use of the complexes as ex vivo contrast agents for a computed tomography scanning of a biological sample. Moreover, the invention relates to specific ex vivo methods for investigating a biological sample by means of computed tomography scanning methods, wherein the method comprises staining the biological sample with a solution comprising one or more of the complex(es); or wherein the method comprises staining the biological sample with a staining solution comprising hematein, and separately contacting the biological sample with one or more staining solution(s) comprising one or more heavy metal ions having an atomic number of 23 or higher and 83 or lower (in particular Ag.sup.1+, Ba.sup.2+, Pb.sup.2+, Gd.sup.3+ and Bi.sup.3+).
RADIATION-SENSITIVE RESIN COMPOSITION AND METHOD FOR FORMING PATTERN
A radiation-sensitive resin composition includes a solvent and an onium salt compound having a structure represented by formula (1). R.sup.f1 and R.sup.f2 each independently represent a fluorine atom or a monovalent fluorinated hydrocarbon group having 1 to 20 carbon atoms. R.sup.1 represents a hydrogen atom, a monovalent hydrocarbon group having 1 to 20 carbon atoms, a fluorine atom, or a monovalent fluorinated hydrocarbon group having 1 to 20 carbon atoms. R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 each independently represent a hydrogen atom or a monovalent hydrocarbon group having 1 to 20 carbon atoms. n.sub.1+n.sub.2 is an integer of 2 to 8. n.sub.3 represents an integer of 0 to 5. X.sup.1 and X.sup.2 each independently represent an oxygen atom or a sulfur atom. Each * represents a bond with another structure. Z.sup.+ represents a monovalent radiation-sensitive onium cation.
##STR00001##
Synthetic process for preparation of macrocyclic C1-keto analogs of Halichondrin B and intermediates useful therein including intermediates containing-SO2-(p-tolyl) groups
Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.7′, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12 and R.sup.13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed. ##STR00001##
Compound, resist composition, and method for forming resist pattern using it
The resist composition of the present invention contains one or more selected from compounds represented by specific formulae and resins obtained using these as monomers.
Compound, resist composition, and method for forming resist pattern using it
The resist composition of the present invention contains one or more selected from compounds represented by specific formulae and resins obtained using these as monomers.
Formation of chiral 4-chromanones using chiral pyrrolidines in the presence of phenols or thiophenols
The present invention relates to a synthesis of chromanones or chromanes in a stereospecific matter in view of the 2-position in the chromanone or chromane ring. It has been found that this synthesis is particularly possible in the presence of a chiral compound of formula of a specific type and of at least one phenol or thiophenol.
Formation of chiral 4-chromanones using chiral pyrrolidines in the presence of ureas or thioureas
The present invention relates to a synthesis of chromanones or chromanes in a stereospecific matter in view of the 2-position in the chromanone or chromane ring. It has been found that this synthesis is particularly possible in the presence of a chiral compound of formula of a specific type and of at least one urea or thiourea.
NOVEL HEAVY METAL ION-LIGAND-COMPLEXES USEFUL AS EX VIVO CONTRAST AGENT FOR A COMPUTED TOMOGRAPHY SCANNING OF A BIOLOGICAL SAMPLE, EX VIVO METHOD FOR INVESTIGATING A BIOLOGICAL SAMPLE, AND USE OF THE COMPLEXES
The present invention relates to specific complexes comprising heavy metal ions having an atomic number of 29 or higher and 83 or lower (preferably 29 or higher and 81 or lower) and one or more ligand(s) selected from the group consisting of specific xanthene derivatives, preferably eosin Y and/or erythrosin B ligand(s). In particular, the invention relates to the use of the complexes as ex vivo contrast agents for a computed tomography scanning of a biological sample. Moreover, the invention relates to specific ex vivo methods for investigating a biological sample by means of computed tomography scanning methods, wherein the method comprises staining the biological sample with a solution comprising one or more of the complex(es); or wherein the method comprises staining the biological sample with a staining solution comprising one or more specific xanthenes derivatives (e.g. eosin Y and/or erythrosin B), and separately contacting the biological sample with one or more staining solution(s) comprising one or more heavy metal ions having an atomic number of 29 or higher and 83 or lower (preferably 29 or higher and 81 or lower).