Abstract: The disclosure provides crystalline forms for certain synthetic intermediates for making belzutifan, a HIF-2? inhibitor, useful for the treatment of cancer. The disclosure also provides processes for isolating the crystalline forms.

Abstract: Disclosed herein, inter alia, are prodrug compositions and methods of using the same for treatment and detection of disease. Specifically, disclosed herein is a compound of formula (I) having spiro-fused 1,2,4-trioxolane and piperidine rings, namely, 1,2,4-trioxa-8-azaspiro[4.5] decane. Also disclosed is a pharmaceutical composition containing the compound and a pharmaceutically acceptable carrier.

Abstract: A salt represented by the formula (I): wherein R1 and R2 each independently represent a fluorine atom or a C1-C6 perfluoroalkyl group, X1 represents a C1-C17 divalent saturated hydrocarbon group which can have one or more fluorine atoms and in which one or more —CH2— can be replaced by —O— or —CO—, R3 represents a group having a cyclic ether structure, and Z1+ represents an organic cation.

Abstract: The present invention relates to the synthesis of ent-progesterone and intermediates thereof.

Abstract: Disclosed is a method for producing a tetrahydropyran compound represented by general formula (5) shown in the scheme. Accordingly, a tetrahydropyran derivative is obtained in high yield and with high selectivity without using a highly toxic reagent, and an industrially useful method for producing a tetrahydropyran derivative and an intermediate thereof can be provided. In formulae (1) to (5), R1 and R2 each independently represent a hydrogen atom, a linear, branched, or cyclic alkyl group, or an aromatic group which may have a substituent, and R1 and R2 may be combined to form an alkylene group, thereby forming a ring; and R3 and R4 each independently represent a hydrogen atom or a linear, branched, or cyclic alkyl group, and R3 and R4 may be combined to form an alkylene group, thereby forming a ring.

Abstract: Intermediates and methods of their use in the synthesis of anslogs of halichondrin B are provided.

Abstract: Embodiments of the present disclosure provide compositions including ketamine analogues, salts, and disalts, pharmaceutical compositions including ketamine analogues, salts, or disalts, methods of treatment of a condition or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

Abstract: Disclosed is a method for producing a tetrahydropyran compound represented by general formula (5) shown in the scheme. Accordingly, a tetrahydropyran derivative is obtained in high yield and with high selectivity without using a highly toxic reagent, and an industrially useful method for producing a tetrahydropyran derivative and an intermediate thereof can be provided. In formulae (1) to (5), R1 and R2 each independently represent a hydrogen atom, a linear, branched, or cyclic alkyl group, or an aromatic group which may have a substituent, and R1 and R2may be combined to form an alkylene group, thereby forming a ring; and R3 and R4 each independently represent a hydrogen atom or a linear, branched, or cyclic alkyl group, and R3 and R4 may be combined to form an alkylene group, thereby forming a ring.

Abstract: This invention relates to an improved process for the preparation of compounds of Formula I, salts of the free base cis-adamantane-2-spiro-3?-8?-[[[(2?-amino-2?-methylpropyl)amino]carbonyl]methyl]-1?,2?,4?-trioxaspiro[4.5]decane, Formula (I) wherein X is an anion. The compounds of Formula (I) have antimalarial activity.

Abstract: The invention relates to substituted 5-(cyclohex-2-en-1-yl)penta-2,4-dienes and 5-(cyclohex-2-en-1-yl)pent-2-en-4-ines of the formula (I) and their salts where the radicals R1, R2, R3, R4, [X—Y] and Q are each as defined in the description, to processes for preparation thereof and to the use thereof for enhancing stress tolerance in plants with respect to abiotic stress, and/or for increasing plant yield.

Abstract: The invention relates to substituted vinyl- and alkynylcyclohexenols of the general formula (I) and salts thereof where the R1, R2, R3, R4, R5, [X—Y] and Q radicals are each as defined in the description, to processes for preparation thereof and to the use thereof for enhancing stress tolerance in plants with respect to abiotic stress, and/or for increasing plant yield.

Abstract: Ketal compounds of the structure I and a method of preparation of the compound from polyols and oxocarboxylates, as well as uses thereof.

Abstract: A method for delivering a nucleic acid to a cell can include exposing sample cells to a composition which includes charged lipids.

Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.

Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions.

Abstract: The present invention relates to a new process for the preparation of 6-hydroxy-5-arylbicyclo[2.2.2]octan-2-one compounds of the formula (II); which may subsequently be further transformed to compounds of the formula (I): The present invention further relates to novel compounds as such, which compounds are useful intermediates in the above process.

Abstract: The present invention primarily relates to the use of dioxolanes of the following Formula (I) as fragrance and/or flavoring substances, certain perfume and/or flavoring compositions comprising these dioxolanes and corresponding perfumed and/or flavored items. The present invention also relates to a method for producing the dioxolanes of Formula (I) and certain new dioxolanes according to Formula (I).

Abstract: Disclosed is a method for producing a tetrahydropyran compound represented by general formula (5) shown in the scheme. Accordingly, a tetrahydropyran derivative is obtained in high yield and with high selectivity without using a highly toxic reagent, and an industrially useful method for producing a tetrahydropyran derivative and an intermediate thereof can be provided. In formulae (1) to (5), R1 and R2 each independently represent a hydrogen atom, a linear, branched, or cyclic alkyl group, or an aromatic group which may have a substituent, and R1 and R2may be combined to form an alkylene group, thereby forming a ring; and R3 and R4 each independently represent a hydrogen atom or a linear, branched, or cyclic alkyl group, and R3 and R4 may be combined to form an alkylene group, thereby forming a ring.

Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).

Abstract: Infections caused by Mycobacterium tuberculosis kill more than 1.8 million people each year. While the persistence of this pathogenic bacterial species and the emergence of multidrug resistant strains have created an urgent need for new TB therapies, a new TB-specific drug has not been developed in over 40 years. The disclosure herein provides short and scalable syntheses of small molecules, and small molecules as new therapeutics for eradicating this life threatening pathogen.

Abstract: Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.

Abstract: The invention relates to novel spiroketal-substituted cyclic ketoenols of the formula (I) in which A, B, Q1, Q2, D, G, W, X, Y, and Z are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or microbicides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, spiroketal-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound.

Abstract: An embodiment of the composition contains any of compounds of the formula A-LG in which A represents any of residues of general formula (A-1) below and LG represents any of groups that are cleaved to generate acids of the formula A-H when acted on by an acid. The composition further contains at least one of a compound that generates an acid when exposed to actinic rays or radiation and a compound that generates an acid when heated.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.

Abstract: The present invention provides a heterocyclic compound represented by the following formula (I), which has a glucagon antagonistic action and is useful for the prophylaxis or treatment of diabetes and the like, a compound represented by wherein ring A is an optionally substituted benzene ring and the like; Y is a nitrogen atom and the like; X is —O— and the like; R4 is a hydrogen atom and the like; R5 and R6 are each independently a hydrogen atom and the like; R1 is an optionally substituted hydrocarbon group and the like; R2 is a hydrogen atom and the like; and R3 is —(CH2)3—COOH and the like, or a salt thereof.

Abstract: The invention relates to a novel process for preparing and isolating known substituted and unsubstituted 1,4-cyclohexanone monoketals.

Abstract: There is provided a halogen-containing organosulfur compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein, m represents 0, 1 or 2, n represents 0, 1 or 2, A represents optionally substituted C3-C7 cycloalkyl or optionally substituted C5-C7 cycloalkenyl group, Q represents a C1-C5 haloalkyl group containing at least one fluorine atom, or a fluorine atom, R1 and R3 independently represent optionally substituted C1-C4 chain hydrocarbon, halogen or hydrogen, R2 and R4 independently represent optionally substituted C1-C4 chain hydrocarbon, —C?C(=G)R5, cyano, halogen or hydrogen, G represents oxygen or sulfur, and R represents optionally substituted C1-C4 alkyl, hydroxyl, optionally substituted C1-C4 alkoxy, optionally substituted C3-C6 alkenyloxy, optionally substituted C3-C6 alkynyloxy, amino, optionally substituted C1-C4 alkylamino, optionally substituted di(C1-C4 alkyl)amino, C2-C5 cyclic amino or hydrogen.

Abstract: The present invention is directed to the fragrance compounds and their intermediates and a method of improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount wherein the dotted line represents a possible single or double bond; wherein R is equal to a C3-C7 hydrocarbon moieties R1 and R2 together can be selected from the group consisting of oxygen and may form a closed ring structure represented by

Abstract: Provided is a method for manufacturing fullerene 1,3-dioxolane conveniently at high yield. Fullerene 1,3-dioxolane is manufactured by reacting a fullerene oxide and a carbonyl compound in the presence of a catalyst.

Abstract: Substituted 5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-2-yl and 5,6,7,8-tetrahydro-quinazolin-2-yl compounds, corresponding to formula I processes for the production thereof, pharmaceutical preparations containing these compounds the use thereof for the production of pharmaceutical preparations and related method of treating or inhibiting certain disorders or conditions, including pain.

Abstract: The present invention a method of improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of the following compound: wherein m is 1 or 2; and if m is 1, which provides a five-membered dioxaspiro ring, n is an integer from 2 to 4, and the methyl group in the dioxaspiro ring is independently located in the 2 and/or 3 positions of the dioxaspiro ring; or if m is 2, which provides a six-membered dioxaspiro ring, n is an integer from 0 to 6, and the methyl group in the dioxaspiro ring is independently located in the 2, 3, and/or 4 positions of the dioxaspiro ring.

Abstract: The present invention a method of improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of the following compound: wherein m is 1 or 2; and if m is 1, which provides a five-membered dioxaspiro ring, n is an integer from 2 to 4, and the methyl group in the dioxaspiro ring is independently located in the 2 and/or 3 positions of the dioxaspiro ring; or if m is 2, which provides a six-membered dioxaspiro ring, n is an integer from 0 to 6, and the methyl group in the dioxaspiro ring is independently located in the 2, 3, and/or 4 positions of the dioxaspiro ring.

Abstract: The present invention a method of improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of the following compound: wherein m is 1 or 2; and if m is 1, which provides a five-membered dioxaspiro ring, n is an integer from 0 to 4, and the methyl group in the dioxaspiro ring is independently located in the 2 and/or 3 positions of the dioxaspiro ring; or if m is 2, which provides a six-membered dioxaspiro ring, n is an integer from 0 to 6, and the methyl group in the dioxaspiro ring is independently located in the 2, 3, and/or 4 positions of the dioxaspiro ring.

Abstract: The invention relates to novel spiroketal-substituted cyclic ketoenols of the formula (I) in which A, B, Q1, Q2, D, G, W, X, Y, and Z are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or microbicides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, spiroketal-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound.

Abstract: The present invention comprises novel substituted 2-aminoimidazoles of formula I, processes for their preparation, pharmaceutical compositions thereof, and methods for their use in the treatment of disorders of the central nervous system, cardiovascular disorders, stroke and pulmonary disorders, urinary disorders such as acute or chronic renal failure, disorders of biliary function, respiratory disorders such as snoring or sleep apnea. wherein the substitutents R1-R8 are further defined herein.

Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.

Abstract: Substituted 4-aminocyclohexanols, processes for their preparation, pharmaceutical compositions comprising these compounds and to the use of substituted 4-aminocyclohexanols in the preparation of pharmaceutical compositions for the treatment of various indications, especially pain as well as the treatment of these indications.

Abstract: Substituted 4-aminocyclohexanols, methods of producing the same, pharmaceuticals containing these compounds, the use of substituted 4-aminocyclohexanols for producing pharmaceutical compositions for the treatment of various indications, in particular pain, and for related treatment methods.

Abstract: NST 400 compounds consisting of a unit for partial coordination of Ca2+ ions (CPCU). The NST 400 compounds are optionally conjugated to another pharmaceutically active compound. The compounds and conjugates can be used for affinity filters and for binding negative charged phospholipids. The compounds and conjugates can also be used for treating diseases involving changes of cell membrane asymmetry.

Abstract: There is provided a process for preparation of a monoketal compound of the structure that includes reacting 1,4-cyclohexanedione of the structure with a diol of the structure in a halogenated organic solvent in the presence of an acid catalyst, wherein X is a substituted or unsubstituted ethylene or propylene. Various embodiments and variants are provided.

Abstract: A description is given of the use of at least one compound of the formula I where R1, R2, R3 and R4 independently of one another are H or C1-C6-alkyl; and the use of a compound of the formula I for medical use.

Abstract: The present application describes novel spiro-cyclic ?-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), and/or aggrecanase inhibitors.

Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

Abstract: A process is provided for preparing an enantiopure 1,3-dioxolan-4-one or 1,3-oxathiolan-5-one derivative, which includes bringing a mixture containing enantiomeric 1,3-dioxolan-4-one or 1,3-oxathiolan-5-one derivatives and an enzyme with hydrolytic activity into contact in the presence of a nucleophile. Cleaving a dioxolanone/oxathiolanone ring of one enantiomer occurs by the enzyme with hydrolytic activity and, after the cleavage of one enantiomer has taken place, the uncleaved enantiomer of the 1,3-dioxolan-4-one or 1,3-oxathiolan-5-one derivative is isolated.

Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

Abstract: Described are photochromic materials of indeno [2′,3′:3,4]naphtho[1,2-b]pyran structure, characterized in that they have a nitrogen or sulfur containing substituent at the 11-position ring atom, are substantially free of spiro-substituents at the 13-position and have been adapted to provide an increase in the sensitivity, visible lambda max or a combination thereof as measured in the Indenonaphthopyran Photochromic Performance Test. Optional substituents can be present at the other positions of the indeno [2′,3′:3,4]naphtho [1,2-b]pyran structure. Also described are naphthols used to produce the photochromic materials and photochromic articles that contain or that have coatings containing at least one of the novel photochromic materials or combinations thereof with other photochromic materials.

Abstract: The invention relates to substituted &ggr;-lactone compounds, to methods for the production thereof, to medicaments containing these compounds and to the use of these compounds for producing medicaments.

Abstract: A description is given of the use of at least one compound of the formula I 1

Abstract: The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.

Abstract: A compound of formula (I) Wherein X, Y, ring A, ring B, l, m, R1, R2, R4 and R5 are as defined herein, to supress intracellular signal transduction or cell activation induced by endotoxin and to suppress cell responses due to the intracellular signal transduction and cell activation such as an excess generation of inflammatory mediators such as TNF-?, pharmacologically acceptable salts therefor, a preparation method therefor, and a medicament containing the aforementioned substituted cycloalkene derivative as an active ingredient which is superior in prophylaxis and/or treatment of diseases such as sepsis (septic shock, disseminated intravascular coagulation, multiple organ failure and the like), that are associated with intracellular signal transduction or cell activation induced by endotoxin and to cell responses to the intracellular signal transduction and cell activation.