Patent classifications
C07D213/62
Process for preparing [(3-hydroxypyridine-2-carbonyl)amino]alkanoic acids, esters and amides
Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, {[(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibittors or for treating conditions wherein prolyl hydroxylase inhibition is desired.
Non-systemic TGR5 agonists
The present invention relates to sulfonamide compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present sulfonamide compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing sulfonamide compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs. ##STR00001##
PROCESS FOR MAKING AMINO DIARYL ETHERS AND AMINO DIARYL ETHERS HYDROCHLORIDE SALTS
The present invention relates to a process for making a compound of formula (I) as described herein Formula (I) comprising reducing a compound of formula (II) as described herein with hydrogen in the presence of a palladium catalyst and a solvent wherein the solvent is a polar, aprotic solvent or a C3-C10 alcohol Formula (II). The present invention further relates to a hydrochloride salt and a monohydrochloride salt of the compound of formula (I) as described herein and to a process for making the same Formula (I).
PROCESS FOR MAKING AMINO DIARYL ETHERS AND AMINO DIARYL ETHERS HYDROCHLORIDE SALTS
The present invention relates to a process for making a compound of formula (I) as described herein Formula (I) comprising reducing a compound of formula (II) as described herein with hydrogen in the presence of a palladium catalyst and a solvent wherein the solvent is a polar, aprotic solvent or a C3-C10 alcohol Formula (II). The present invention further relates to a hydrochloride salt and a monohydrochloride salt of the compound of formula (I) as described herein and to a process for making the same Formula (I).
##STR00001##
PROCESS FOR MAKING AMINO DIARYL ETHERS AND AMINO DIARYL ETHERS HYDROCHLORIDE SALTS
The present invention relates to a process for making a compound of formula (I) as described herein Formula (I) comprising reducing a compound of formula (II) as described herein with hydrogen in the presence of a palladium catalyst and a solvent wherein the solvent is a polar, aprotic solvent or a C3-C10 alcohol Formula (II). The present invention further relates to a hydrochloride salt and a monohydrochloride salt of the compound of formula (I) as described herein and to a process for making the same Formula (I).
##STR00001##
PROCESS OF MAKING CFTR MODULATORS
- Paul Angell ,
- John E. Cochran ,
- Benjamin J. Littler ,
- David Siesel ,
- Armando Urbina ,
- Corey Don ANDERSON ,
- Jeremy J. Clemens ,
- Thomas Cleveland ,
- Timothy Richard Coon ,
- Bryan Frieman ,
- Peter Grootenhuis ,
- Sara Sabina Hadida Ruah ,
- Jason McCartney ,
- Mark Thomas Miller ,
- Prasuna Paraselli ,
- Fabrice Pierre ,
- Sara E. Swift ,
- Jinglan Zhou
The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.
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Pyridone compounds and agricultural and horticultural fungicides containing the same as active ingredients
An object of the invention is to provide compounds of formula (1) or salts thereof which are effective as agricultural and horticultural fungicides. In the formula, R1 represents, for example, a hydroxy group or a cyano group, R2, R3 and R4 are independent of one another and each represent, for example, a hydrogen atom or a halogen atom, R5 represents, for example, a hydrogen atom or a halogen atom, X represents an oxygen atom or a sulfur atom, Y represents, for example, a phenyl group or a pyridyl group, and the bond including the broken line represents a double bond or a single bond.
Pyridone compounds and agricultural and horticultural fungicides containing the same as active ingredients
An object of the invention is to provide compounds of formula (1) or salts thereof which are effective as agricultural and horticultural fungicides. In the formula, R1 represents, for example, a hydroxy group or a cyano group, R2, R3 and R4 are independent of one another and each represent, for example, a hydrogen atom or a halogen atom, R5 represents, for example, a hydrogen atom or a halogen atom, X represents an oxygen atom or a sulfur atom, Y represents, for example, a phenyl group or a pyridyl group, and the bond including the broken line represents a double bond or a single bond.
SULFONAMIDE DERIVATES AS NLRP3 INHIBITORS
The present invention relates to compounds of formula (I): (I) wherein Q is selected from O or S; R.sup.1 is an optionally substituted hydrocarbyl group which may optionally include one or more heteroatoms N, O or S in its carbon skeleton, provided that the hydrocarbyl group includes at least one heteroatom N, O or S in its carbon skeleton or is substituted with a substituent comprising at least one heteroatom N, O or S, and provided that the atom of R.sup.1 which is attached to the sulfur atom of the remainder of the molecule is not a ring atom of a cyclic group; R.sup.2 is an ,-substituted cyclic group which may optionally be further substituted; R.sup.3 and R.sup.4 are each independently hydrogen, halogen, OH, NH.sub.2, CN, R.sup.5, OR.sup.5, NHRs or N(R.sup.5).sub.2; or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and R.sup.5 is independently optionally substituted C.sub.1-C.sub.4 alkyl. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3.
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CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS
Compounds of formula (I), wherein R.sub.1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.