Patent classifications
C07D311/94
Photochromic fluorenopyrans with defined dibenzo[B,D]pyrano fused attachment
The present invention relates to photochromic fluorenopyrans with defined dibenzo[b,d]pyrano fusion in accordance with general formulae (I) or (II) and to their use in plastics of all kinds, particularly for ophthalmic purposes. The photochromic compounds of the invention are distinguished by two pronounced absorption bands of the open form in the visible wavelength range, meaning that with dye molecules of this kind it is possible to replace two conventional photochromic dyes each having only one discrete absorption band. The compounds of the invention, moreover, have a very good lifetime with very high performance.
METHODS AND COMPOSITIONS FOR TERPENOID SYNTHESIS
In one aspect, the disclosure relates to methods for preparation of terpene and terpene-like molecules. In a further aspect, the disclosure relates to the products of the disclosed methods, i.e., terpene and terpene-like molecules prepared using the disclosed methods. Intermediates for the synthesis of a wide variety of terpenoids are -allyl Knoevenagel adducts or quasi -allyl Knoevenagel adducts are disclosed. In various aspects, methods of preparing terpenoids through these intermediates are disclosed. The methods can comprise -alkylation of an allylic electrophile followed by ring-closure metathesis to a polycyclic terpenoid structure. In a further aspect, the disclosure pertains to terpenoid frameworks, and compounds prepared via disclosed oxidation and substitution reactions on the disclosed terpenoid frameworks. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
METHODS AND COMPOSITIONS FOR TERPENOID SYNTHESIS
In one aspect, the disclosure relates to methods for preparation of terpene and terpene-like molecules. In a further aspect, the disclosure relates to the products of the disclosed methods, i.e., terpene and terpene-like molecules prepared using the disclosed methods. Intermediates for the synthesis of a wide variety of terpenoids are -allyl Knoevenagel adducts or quasi -allyl Knoevenagel adducts are disclosed. In various aspects, methods of preparing terpenoids through these intermediates are disclosed. The methods can comprise -alkylation of an allylic electrophile followed by ring-closure metathesis to a polycyclic terpenoid structure. In a further aspect, the disclosure pertains to terpenoid frameworks, and compounds prepared via disclosed oxidation and substitution reactions on the disclosed terpenoid frameworks. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
##STR00001##
ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
##STR00001##
Method for purifying compound or resin
The method according to the present invention is a method for purifying a compound represented by a specific formula (1) or a resin having a structure represented by a specific formula (2), the method including a step of bringing a solution (A) including an organic solvent optionally immiscible with water, and the compound or the resin into contact with an acidic aqueous solution.
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
Methods of making fused ring compounds
The present invention relates to methods of making fused ring compounds, such as indeno-fused naphthols, and fused ring indenopyran compounds, such as indeno-fused naphthopyrans, that each employ an unsaturated compound represented by the following Formula II. ##STR00001## Referring to the unsaturated compound of Formula II: Ring-A can be selected from optionally substituted aryl (e.g., phenyl); m can be, for example, from 0 to 4; R.sup.1 for each m can be selected from optionally substituted hydrocarbyl (e.g., C.sub.1-C.sub.6 alkyl) optionally interrupted with at least one linking group (e.g., O); and R.sup.3 and R.sup.16 can each be independently selected from, for example, hydrogen or optionally substituted hydrocarbyl, such as C.sub.1-C.sub.8 alkyl. When Ring-A is a phenyl group, the unsaturated compound represented by Formula II can be referred to as an unsaturated indanone acid/ester compound, or an indenone acid/ester compound (depending on whether R.sup.16 is hydrogen, or an optionally substituted hydrocarbyl group).
Methods of making fused ring compounds
The present invention relates to methods of making fused ring compounds, such as indeno-fused naphthols, and fused ring indenopyran compounds, such as indeno-fused naphthopyrans, that each employ an unsaturated compound represented by the following Formula II. ##STR00001## Referring to the unsaturated compound of Formula II: Ring-A can be selected from optionally substituted aryl (e.g., phenyl); m can be, for example, from 0 to 4; R.sup.1 for each m can be selected from optionally substituted hydrocarbyl (e.g., C.sub.1-C.sub.6 alkyl) optionally interrupted with at least one linking group (e.g., O); and R.sup.3 and R.sup.16 can each be independently selected from, for example, hydrogen or optionally substituted hydrocarbyl, such as C.sub.1-C.sub.8 alkyl. When Ring-A is a phenyl group, the unsaturated compound represented by Formula II can be referred to as an unsaturated indanone acid/ester compound, or an indenone acid/ester compound (depending on whether R.sup.16 is hydrogen, or an optionally substituted hydrocarbyl group).
IRE-1? inhibitors
Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.