C07D403/02

Hepatitis C virus inhibitors

The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Substituted imidazo[1,2-a]imidazoles as modulators of metabotropic glutamate receptor 4 activity

The present invention relates to compounds of formula I ##STR00001## wherein L is a bond, a triple bond, —C(O)NH— or —NHC(O)—; R.sup.1 is phenyl or a five or six-membered heteroaryl group, optionally substituted by lower alkyl, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; R.sup.2 is fluoro; R.sup.3 is fluoro or chloro; R.sup.4 is hydrogen, lower alkyl, halogen, lower alkyl substituted by hydroxy, S(O).sub.2CH.sub.3, or is a five or six-membered heteroaryl group or a heterocycloalkyl group, which are optionally substituted by lower alkyl, hydroxy or ═O; R.sup.5 and R.sup.6 are both methyl and the dotted line is a bond, or R.sup.5 and R.sup.6 are both methyl and the dotted line is nothing, or one of R.sup.5 and R.sup.6 is hydrogen and the other is methyl, and the dotted line is nothing; or to a pharmaceutically acceptable salt or acid addition salt, to all possible tautomeric forms, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.

Preparation of angiotensin receptor blockers or pharmaceutically acceptable salts thereof

The present invention relates to a process for the preparation of angiotensin receptor blockers or its pharmaceutically acceptable salts thereof containing less than 10 ppm of the azido impurities. More particularly, the present invention relates to process for the preparation of Losartan, Losartan potassium of Formula I or its other pharmaceutically acceptable salts thereof containing less than 10 ppm of each of the azido impurities, wherein the azido impurity is selected from the group comprising of 5-(4′-(azidomethyl)-[1,1′-biphenyl]-2-yl)-1H-tetrazole, 4′-(azidomethyl)-[1,1′-biphenyl]-2-carbonitrile, 4′-((5-(azidomethyl)-2-butyl-4-chloro-1H-imidazol-1-yl)methyl)-[1,1′-biphenyl]-2-carbonitrile, 5-(4′-((5-(azidomethyl)-2-butyl-4-chloro-1H-imidazol-1-yl)methyl)-[1,1′-biphenyl]-2-yl)-1H-tetrazole, 5-(azidomethyl)-2-butyl-4-chloro-1H-imidazole, 4′-((4-(azidomethyl)-2-butyl-5-chloro-1H-imidazol-1-yl)methyl)-[1,1′-biphenyl]-2-carbonitrile, 5-(4′-((4-(azidomethyl)-2-butyl-5-chloro-1H-imidazol-1-yl)methyl)-[1,1′-biphenyl]-2-yl)-1H-tetrazole and 1-((1-((2′-(1H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-butyl-4-chloro-1H-imidazol-5-yl)methyl)-5-(4′-((5-(azidomethyl)-2-butyl-4-chloro-1H-imidazol-1-yl)methyl)-[1,1′-biphenyl]-2-yl)-1H-tetrazole. More particularly, the present invention relates to a simple, economical and industrially efficient process for the preparation of Losartan potassium of Formula I. ##STR00001##

Compounds for central reactivation of organophosphorus-based compound-inhibited acetylcholinesterase and/or inactivation of organophosphorus-based acetylcholinesterase inhibitors and related compositions methods and systems for making and using them

Described herein are oxime compounds capable of inactivating OP-based AChE inhibitors, crossing the blood brain barrier (BBB), and/or reactivation of OP-inhibited acetylcholinesterase (AChE) and related methods, systems and compositions for inactivation of one or more OP-based AChE inhibitors, therapeutic and/or prophylactic treatment of an individual, and/or decomposition of OP-based AChE inhibitors for decontamination.

4-carboxamido-isoindolinone derivatives as selective PARP-1 inhibitors

There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-I with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

4-carboxamido-isoindolinone derivatives as selective PARP-1 inhibitors

There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-I with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

CYCLIC CYANOENONE DERIVATIVES AS MODULATORS OF KEAP1

The present invention relates to cyclic cyanoenone derivatives of Formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and m are as defined herein. The present invention also relates to pharmaceutical compositions comprising the cyclic cyanoenone derivatives of Formula (I) and to their use in therapy.

##STR00001##

METHOD OF CONTROLLING SOYBEAN RUST FUNGUS RESISTANT TO QOI FUNGICIDE

The present invention provides a method for controlling soybean rust fungus having an amino acid replacement of F129L in mitochondrial cytochrome b protein. A compound represented by formula (I) [wherein: Q represents a group represented by Q1 etc. (wherein “•” represents a position bonding to benzene ring); E represents C1-C6 chain hydrocarbon group, etc.; R.sup.1 represents C1-C3 chain hydrocarbon group, etc.; n is 0, 1, 2 or 3; when n is 2 or 3, two or more of R.sup.2 may be identical to or different from each other; and R.sup.2 represents C1-C3 chain hydrocarbon group, etc.] can be used for controlling soybean rust fungus having an amino acid replacement of F129L in mitochondrial cytochrome b protein.

##STR00001##

Tracers for petroleum reservoirs

The disclosure features methods of analyzing a fluid extracted from a reservoir, the methods including introducing a first composition featuring a first complexing agent into a reservoir at a first location, extracting a fluid from the reservoir at a second location different from the first location, combining the fluid with a second composition featuring a concentration of a lanthanide ion to form a third composition featuring a concentration of a complex formed by the first complexing agent and the lanthanide ion, exposing a quantity of the complex to electromagnetic radiation for a first time period ending at a time t.sub.0, detecting fluorescence emission from the quantity of the complex for a second time period starting at a time t.sub.1>t.sub.0, where t.sub.1−t.sub.0 is greater than 2 microseconds, and determining information about a fluid flow path between the first location and the second location.

4-carboxamido-isoindolinone derivatives as selective parp-1 inhibitors

There are provided substituted 4-carboxamido-isoindolinone derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-I with respect to poly (ADP-ribose) polymerase P ARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of in-flammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.