Patent classifications
C07D233/78
5-[(PIPERAZIN-1-YL)-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS
The present invention discloses compounds according to Formula I:
##STR00001##
Wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, and Cy are as defined herein.
The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a compound of the invention.
5-[(PIPERAZIN-1-YL)-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS
The present invention discloses compounds according to Formula I:
##STR00001##
Wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, and Cy are as defined herein.
The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a compound of the invention.
Compounds useful as modulators of TRPM8
The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formulae (Ia), (Ib) and (Ic), and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations. ##STR00001##
Compounds useful as modulators of TRPM8
The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formulae (Ia), (Ib) and (Ic), and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations. ##STR00001##
2-naphthimidamides, analogues thereof, and methods of treatment using same
The present invention relates in certain aspects to the discovery of novel 2-naphthimidamide compounds that are capable of binding Type II Transmembrane Serine Proteases (TTSPs). In certain embodiments, the compounds of the invention can be used to treat or prevent Influenza A viral infection in a mammal.
5-[(piperazin-1-yl)-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS inhibitors for the treatment of osteoarthritis
The present invention discloses compounds according to Formula I: ##STR00001## Wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, and Cy are as defined herein. The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a compound of the invention.
5-[(piperazin-1-yl)-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS inhibitors for the treatment of osteoarthritis
The present invention discloses compounds according to Formula I: ##STR00001## Wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, and Cy are as defined herein. The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a compound of the invention.
DOCK1-INHIBITING COMPOUND AND USE THEREOF
Provided is a compound that is usable as an active ingredient of an anticancer agent. Preferably provided is a compound that has DOCK1-inhibiting activity and exerts an anticancer effect based on the activity. A compound represented by the following formula (A) or a salt thereof:
##STR00001## wherein X represents a carbon atom or a nitrogen atom; Y represents an oxygen atom, a hydroxy group, or a hydrocarbon group; R.sup.1 and R.sup.2 are different, and each represents a hydrogen atom or a group represented by the following formula (A-1):
##STR00002## (wherein R.sup.6 represents a pyrrolidino group or a phenyl group, and n.sup.2 is 0 or 1); R.sup.3 represents —CO—R.sup.7 (wherein R.sup.7 is an alkoxy group, an alkyl group, or an alkylamino group), a 1,3-oxazole group, an alkylhydroxy group, a hydrogen atom, or an oxygen atom; R.sup.4 represents a hydrogen atom, an oxygen atom, or a hydrocarbon group in which one or more hydrogen atoms may be replaced by one or more substituents; R.sup.5 represents a halogen atom, a halogenated alkyl group, or a halogenated alkylthio group; and n.sup.1 is an integer of 0 to 5; and in the skeleton of the compound of formula (A), each single solid line represents a single bond; each double line consisting of a solid line and a dotted line represents a single bond or a double bond; and two dotted lines represent no bond or a double bond.
DOCK1-INHIBITING COMPOUND AND USE THEREOF
Provided is a compound that is usable as an active ingredient of an anticancer agent. Preferably provided is a compound that has DOCK1-inhibiting activity and exerts an anticancer effect based on the activity. A compound represented by the following formula (A) or a salt thereof:
##STR00001## wherein X represents a carbon atom or a nitrogen atom; Y represents an oxygen atom, a hydroxy group, or a hydrocarbon group; R.sup.1 and R.sup.2 are different, and each represents a hydrogen atom or a group represented by the following formula (A-1):
##STR00002## (wherein R.sup.6 represents a pyrrolidino group or a phenyl group, and n.sup.2 is 0 or 1); R.sup.3 represents —CO—R.sup.7 (wherein R.sup.7 is an alkoxy group, an alkyl group, or an alkylamino group), a 1,3-oxazole group, an alkylhydroxy group, a hydrogen atom, or an oxygen atom; R.sup.4 represents a hydrogen atom, an oxygen atom, or a hydrocarbon group in which one or more hydrogen atoms may be replaced by one or more substituents; R.sup.5 represents a halogen atom, a halogenated alkyl group, or a halogenated alkylthio group; and n.sup.1 is an integer of 0 to 5; and in the skeleton of the compound of formula (A), each single solid line represents a single bond; each double line consisting of a solid line and a dotted line represents a single bond or a double bond; and two dotted lines represent no bond or a double bond.
Open Time Additive
The present disclosure is generally directed to an open time additive composition that includes at least two, different open time additives having the structure of Compound I, a salt thereof, or both. Compound I having the following formula:
##STR00001##