Patent classifications
C07C215/10
Solid Forms of 2-((4-((S)-2-(5-Chloropyridin-2-yl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((S)-oxetan-2-yl)methyl)-1H-benzo[d]imidazole-6-carboxylic acid, 1,3-Dihydroxy-2-(hydroxymethyl)propan-2-amine Salt
The invention provides solid forms of 2-((4-((S)-2-(5-chloropyridin-2-yl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((S)-oxetan-2-yl)methyl)-1H-benzo[d]imidazole-6-carboxylic acid, 1,3-dihydroxy-2-(hydroxymethyl)propan-2-amine salt for example, a hydrate (e.g. a monohydrate) crystalline form (e.g. Form 2 or Form 3) or an amorphous form; as well as pharmaceutical compositions, and the uses thereof in treating diseases, conditions or disorders modulated by GLP-1R in a mammal, such as a human.
SALTS OF PRODRUGS OF PIPERAZINE AND SUBSTITUTED PIPERIDINE ANTIVIRAL AGENTS
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection.
##STR00001## wherein: X is C or N with the proviso that when X is N, R.sup.1 does not exist; W is C or N with the proviso that when W is N, R.sup.2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of
##STR00002##
Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I.
##STR00003## wherein: L and M are independently selected from the group consisting of C.sub.1-C.sub.6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
STEREOSELECTIVE PROCESS FOR PREPARING SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVES
The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity. In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof;
##STR00001##
STEREOSELECTIVE PROCESS FOR PREPARING SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVES
The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity. In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof;
##STR00001##
COMPOSITION AND METHOD FOR PRODUCING SAME
Provided is a composition having moderate viscosity for coating properties and ejection properties, being applicable for firing at low temperatures, and leaving an extremely small amount of ash after firing. The composition of the present disclosure contains a miscible material of a compound represented by Formula (1) below and a compound (A) represented by Formula (A) below. In Formula (1) below, R.sup.1 represents a linear aliphatic hydrocarbon group having from 10 to 25 carbons; R.sup.2 and R.sup.3 are identical or different and represent an aliphatic hydrocarbon group having 2, 4, 6, or 8 carbons; R.sup.4 represents an aliphatic hydrocarbon group having from 1 to 8 carbons; R.sup.5 and R.sup.6 are identical or different and represent an aliphatic hydrocarbon group having from 1 to 3 carbons or a hydroxyalkyl ether group; and L.sup.1 to L.sup.3 represent an amide bond. In Formula (A) below, in the formula, R.sup.a and R.sup.c are identical or different and represent a hydrogen atom or an aliphatic hydrocarbon group that has from 1 to 12 carbons and may have a substituent; R.sup.b represents an aliphatic hydrocarbon group that has from 1 to 12 carbons and may have a substituent; and the substituents are each an amino group and/or a hydroxyl group.
COMPOSITION AND METHOD FOR PRODUCING SAME
Provided is a composition having moderate viscosity for coating properties and ejection properties, being applicable for firing at low temperatures, and leaving an extremely small amount of ash after firing. The composition of the present disclosure contains a miscible material of a compound represented by Formula (1) below and a compound (A) represented by Formula (A) below. In Formula (1) below, R.sup.1 represents a linear aliphatic hydrocarbon group having from 10 to 25 carbons; R.sup.2 and R.sup.3 are identical or different and represent an aliphatic hydrocarbon group having 2, 4, 6, or 8 carbons; R.sup.4 represents an aliphatic hydrocarbon group having from 1 to 8 carbons; R.sup.5 and R.sup.6 are identical or different and represent an aliphatic hydrocarbon group having from 1 to 3 carbons or a hydroxyalkyl ether group; and L.sup.1 to L.sup.3 represent an amide bond. In Formula (A) below, in the formula, R.sup.a and R.sup.c are identical or different and represent a hydrogen atom or an aliphatic hydrocarbon group that has from 1 to 12 carbons and may have a substituent; R.sup.b represents an aliphatic hydrocarbon group that has from 1 to 12 carbons and may have a substituent; and the substituents are each an amino group and/or a hydroxyl group.
Salts of R-ketorolac
Salts of R-ketorolac, including solid salts, such as crystalline salts of the meglumine and tromethamine salts R-ketorolac, are disclosed. Methods of preparing such salts, pharmaceutical compositions comprising salts, and methods of treating cancer with such salts are further provided.
LAUNDRY DETERGENT CONTAINING AMINE ADDITIVES
A laundry detergent composition comprising:
(a) 4 to 25 wt % of a linear alkyl benzene sulfonate; (b) 25 to 55 wt % nonionic surfactant, (c) 2 to 10 wt % of an amine having formula (I)
##STR00001##
wherein R.sup.1 is C.sub.1-C.sub.4 alkyl or C.sub.1-C.sub.4 hydroxyalkyl; or formula (II)
##STR00002##
wherein R.sup.2 is C.sub.1-C.sub.4 alkyl and R.sup.3 is C.sub.2-C.sub.8 alkyl; or a combination thereof; and (d) 10 to 35 wt % C.sub.3-C.sub.6 polyhydroxy compounds.
Biological Buffers with Wide Buffering Ranges
Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.
Compounds Which Have a Protective Activity with Respect to the Action of Toxins and of Viruses with an Intracellular Mode of Action
The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.