Patent classifications
C07C275/42
Vinylarene derivative and application
The present invention relates to a vinylarene deriv. which modulates or inhibits the enzymic activity of indoleamine 2,3-dioxygenase 1 (IDO-1), and the use thereof, and further relates to a vinylarene deriv. and the use thereof. The vinylarene deriv. and its stereoisomer, cis- or trans-isomer, or tautomer thereof and pharmaceutically acceptable salt thereof, has an IDO-1 enzyme inhibitory activity, and is expected to provide brand new therapeutic methods and schemes for related diseases caused by IDO enzymes. ##STR00001##
Vinylarene derivative and application
The present invention relates to a vinylarene deriv. which modulates or inhibits the enzymic activity of indoleamine 2,3-dioxygenase 1 (IDO-1), and the use thereof, and further relates to a vinylarene deriv. and the use thereof. The vinylarene deriv. and its stereoisomer, cis- or trans-isomer, or tautomer thereof and pharmaceutically acceptable salt thereof, has an IDO-1 enzyme inhibitory activity, and is expected to provide brand new therapeutic methods and schemes for related diseases caused by IDO enzymes. ##STR00001##
hTRPV1 chemical agents
Novel diphenylurea and benzylbenzenesulfonamide compounds are disclosed along with methods of inhibiting the activity of TRPV1 and methods of treating pain associated with transient receptor potential vanilloid type 1 (TRPV1) using such compounds.
hTRPV1 chemical agents
Novel diphenylurea and benzylbenzenesulfonamide compounds are disclosed along with methods of inhibiting the activity of TRPV1 and methods of treating pain associated with transient receptor potential vanilloid type 1 (TRPV1) using such compounds.
Compositions and methods for treating cancer
The present invention relates to the field of anti-cancer compounds. More particularly, the invention relates to a family of benzothiazolyl urea or thiorurea compound useful as such agents. The present invention also relates to methods for treating cancers using these compounds.
UREA DERIVATIVE
An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof:
##STR00001##
wherein R.sup.1 and R.sup.2 are the same or different, and represent a C.sub.1-C.sub.6 alkyl group or the like, and Ar represents an optionally substituted phenyl group or an optionally substituted thienyl group.
UREA DERIVATIVE
An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof:
##STR00001##
wherein R.sup.1 and R.sup.2 are the same or different, and represent a C.sub.1-C.sub.6 alkyl group or the like, and Ar represents an optionally substituted phenyl group or an optionally substituted thienyl group.
NOVEL AMINO ACID DERIVATIVES
- Naoki OKADA ,
- Kyosuke UEDA ,
- Masatoshi TAKUWA ,
- Shunichi NAKANO ,
- Kotaro TOKUMOTO ,
- Tomoko ASHIZAWA ,
- Shuhei YAMAKOSHI ,
- Yutaka KOBAYASHI ,
- Katsuma MATSUI ,
- Ayumu MATSUDA ,
- Masatoshi MATSUMOTO ,
- Keiichi MASUYA ,
- Atsushi YOSHIZAWA ,
- Masahiko KINEBUCHI ,
- Takeru EHARA ,
- Masami YAMADA ,
- Kouki MORIMOTO ,
- Yoshihide MIZUKOSHI ,
- Haruaki KURASAKI ,
- Motoki MURAI ,
- Kentarou FUKUMOTO ,
- Douglas Robert CARY
A novel amino acid derivative is provided, wherein the amino acid derivative is expected to improve solubility of polypeptides comprising the derivative therein.
NOVEL AMINO ACID DERIVATIVES
- Naoki OKADA ,
- Kyosuke UEDA ,
- Masatoshi TAKUWA ,
- Shunichi NAKANO ,
- Kotaro TOKUMOTO ,
- Tomoko ASHIZAWA ,
- Shuhei YAMAKOSHI ,
- Yutaka KOBAYASHI ,
- Katsuma MATSUI ,
- Ayumu MATSUDA ,
- Masatoshi MATSUMOTO ,
- Keiichi MASUYA ,
- Atsushi YOSHIZAWA ,
- Masahiko KINEBUCHI ,
- Takeru EHARA ,
- Masami YAMADA ,
- Kouki MORIMOTO ,
- Yoshihide MIZUKOSHI ,
- Haruaki KURASAKI ,
- Motoki MURAI ,
- Kentarou FUKUMOTO ,
- Douglas Robert CARY
A novel amino acid derivative is provided, wherein the amino acid derivative is expected to improve solubility of polypeptides comprising the derivative therein.
2,5- OR 2,6-DISUBSTITUTED HYDROQUINONE DERIVATIVES WITH AT LEAST ONE CARBOXY, SULFO OR AMIDO GROUP USEFUL AS MEDICAMENTS
The present invention provides novel hydroquinone derivatives of formula (I), processes of preparation, as well as pharmaceutical compositions and methods of treating and/or preventing e.g. autoimmune, immunological, rheumatology, vascular disorders, ophthalmologic disorders, fibrotic disorders, metabolic and gastrointestinal disorders, neuroinflammatory and neurodegenerative diseases, neoplasms and cancer associated disorders, hormone related diseases and immunological disorders resulting from viral and bacterial infectious diseases and complications thereof. wherein R.sub.1 is COOR.sub.4, (CH.sub.2)nCOOR.sub.4, SO.sub.3H, (CH.sub.2)nSO.sub.3H or CONH—R.sub.10; one of R.sub.2 and R.sub.3 is H and the other is R.sub.5.
##STR00001##