公开(公告)号：CA2785679A1

公开(公告)日：2011-07-07

申请号：CA2785679

申请日：2010-12-28

Applicant: GEN INC ASS PHARMA VALLEY PROJECT SUPPORTING ORGANI ZATION ,  PHARMA DESIGN INC ,  SHIZUOKA PREFECTURE ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY ,  YAKULT HONSHA KK

Inventor： ASAI AKIRA ,  MATSUNO KENJI ,  OGO NAOHISA ,  TAKAHASHI OSAMU ,  MASUDA YOSHIAKI ,  MUROYA AYUMU ,  AKIYAMA YASUTO ,  ASHIZAWA TADASHI ,  OKAWARA TADASHI

IPC: C07D413/04 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/55 ,  A61P35/00 ,  A61P43/00 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: Disclosed is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Specifically disclosed is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof. (In the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and -X-Y represents a diaryl group such as a biphenyl group.)

公开(公告)号：EA021306B1

公开(公告)日：2015-05-29

申请号：EA201170176

申请日：2009-07-10

Applicant: PHARMA IP GENERAL INC ASS ,  PHARMA DESIGN INC ,  SHIZUOKA PREFECTURE ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY ,  YAKULT HONSHA KK

Inventor： ASAI AKIRA ,  MATSUNO KENJI ,  OGO NAOHISA ,  YOKOTAGAWA TAKANE ,  TAKAHASHI OSAMU ,  AKIYAMA YASUTO ,  ASHIZAWA TADASHI ,  OKAWARA TADASHI

IPC: C07D401/12 ,  A61K31/4709 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Настоящееизобретениепредставляетингибитор STAT3, содержащийв качествеактивногоингредиентахинолинкарбоксамидноепроизводное, представленноеформулой (I) (вформуле W представляетсобойсвязьилиалкиленовуюсвязь; X представляетсобойО, S или NR; иот Rдо Rи RкаждыйпредставляетсобойН, галоген, алкил, фенил, фурил, тиенилилиподобное), илиегофармакологическиприемлемуюсоль.

公开(公告)号：NZ602099A

公开(公告)日：2014-06-27

申请号：NZ60209909

申请日：2009-07-10

Applicant: PHARMA IP GENERAL INC ASS ,  PHARMA DESIGN INC ,  SHIZUOKA PREFECTURE ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY ,  YAKULT HONSHA KK

Inventor： ASAI AKIRA ,  MATSUNO KENJI ,  OGO NAOHISA ,  YOKOTAGAWA TAKANE ,  TAKAHASHI OSAMU ,  AKIYAMA YASUTO ,  ASHIZAWA TADASHI ,  OKAWARA TADASHI

IPC: C07D417/14 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4709 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D215/50 ,  C07D215/52 ,  C07D249/08 ,  C07D249/14 ,  C07D271/10 ,  C07D271/113 ,  C07D285/12 ,  C07D285/135 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: Disclosed is the use of N-[1,3,4-oxadiazol-2-yl]-2-phenyl-4-quinolinecarboxamide, N-[1,3,4-thiadiazol-2-yl]-2-phenyl-4-quinolinecarboxamide and N-[1,3,4-triazol-2-yl]-2-phenyl-4-quinolinecarboxamide derivatives as represented by the general formula (I) in the manufacture of a medicament for the treatment and/or prevention of cancer by inhibition of STAT3, wherein R2 is hydrogen or methyl; R3 is a substituted or unsubstituted aryl group; W is a single bond or an unsubstituted alkylene group; X represents an oxygen atom, a sulphur atom, or NR34; and wherein the remaining substituents are as defined herein. Representative compounds of formula (I) include N-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-2-phenyl-4-quinolinecarboxamide, N-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-6-chloro-2-thienyl-4-quinolinecarboxamide, N-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-2-(4-(tert-butoxycarbonyl)phenyl)-4-quinolinecarboxamide, N-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-2-(1,3-benzodioxol-5-yl)-4-quinolinecarboxamide and N-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-6-bromo-2-(phenyl)-4-quinolinecarboxamide.

公开(公告)号：AU2009269410A1

公开(公告)日：2010-01-14

申请号：AU2009269410

申请日：2009-07-10

Applicant: YAKULT HONSHA KK ,  PHARMA IP GENERAL INC ASS ,  PHARMA DESIGN INC ,  SHIZUOKA PREFECTURE ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY

Inventor： ASAI AKIRA ,  ASHIZAWA TADASHI ,  OKAWARA TADASHI ,  YOKOTAGAWA TAKANE ,  OGO NAOHISA ,  TAKAHASHI OSAMU ,  AKIYAMA YASUTO ,  MATSUNO KENJI

IPC: C07D401/12 ,  A61K31/4709 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention provides a STAT3 inhibitor containing as an active ingredient, a quinolinecarboxamide derivative represented by the formula (I) (in the formula, W represents a bond or an alkylene chain; X represents O, S, or NR 34 ; and R 1 to R 8 and R 34 each represent H, halogen, alkyl, phenyl, furyl, thienyl, or the like.), or a pharmacologically acceptable salt thereof.

公开(公告)号：NZ590355A

公开(公告)日：2013-01-25

申请号：NZ59035509

申请日：2009-07-10

Applicant: YAKULT HONSHA KK ,  PHARMA IP GENERAL INC ASS ,  PHARMA DESIGN INC ,  SHIZUOKA PREFECTURE ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY

Inventor： ASAI AKIRA ,  MATSUNO KENJI ,  OGO NAOHISA ,  YOKOTAGAWA TAKANE ,  TAKAHASHI OSAMU ,  AKIYAMA YASUTO ,  ASHIZAWA TADASHI ,  OKAWARA TADASHI

IPC: A61K31/4709 ,  C07D417/12 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: 590355 Disclosed are N-[1,3,4-oxadiazol-2-yl]-4-quinolinecarboxamide derivatives as represented by the general formula (I), wherein R4a represents a hydrogen atom; W represents a single bond or an unsubstituted alkylene group; X represents an oxygen atom, a sulfur atom, or NR34; and wherein the remaining substituents are as defined herein. Representative compounds include N-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-2-phenyl-4-quinolinecarboxamide, 2-phenyl-N-(5-phenyl-1,3,4-oxadiazol-2-yl)-4-quinolinecarboxamide, N-[5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl]-2-phenyl-4-quinolinecarboxamide, 2-phenyl-N-[5-(3-pyridyl)-1,3,4-oxadiazol-2-yl]-4-quinolinecarboxamide and N-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl]-4-quinolinecarboxamide. Further disclosed is a pharmaceutical composition, containing as an active ingredient, a quinolinecarboxamide derivative as defined above, or a pharmacologically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent excipient and/or adjuvant for the treatment of cancer.

公开(公告)号：AU2010339271A1

公开(公告)日：2012-07-19

申请号：AU2010339271

申请日：2010-12-28

Applicant: GEN INC ASS PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY ,  YAKULT HONSHA KK ,  PHARMA DESIGN INC ,  SHIZUOKA PREFECTURE

Inventor： ASAI AKIRA ,  MATSUNO KENJI ,  OGO NAOHISA ,  TAKAHASHI OSAMU ,  MASUDA YOSHIAKI ,  MUROYA AYUMU ,  AKIYAMA YASUTO ,  ASHIZAWA TADASHI ,  OKAWARA TADASHI

IPC: C07D413/04 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/55 ,  A61P35/00 ,  A61P43/00 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: Disclosed is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Specifically disclosed is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof. (In the formula, Ar represents a furyl group or the like; R represents a hydrogen atom or the like; and -X-Y represents a diaryl group such as a biphenyl group.)

公开(公告)号：CA2729988A1

公开(公告)日：2010-01-14

申请号：CA2729988

申请日：2009-07-10

Applicant: PHARMA IP GENERAL INC ASS ,  PHARMA DESIGN INC ,  SHIZUOKA PREFECTURE ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY ,  YAKULT HONSHA KK

Inventor： ASAI AKIRA ,  MATSUNO KENJI ,  OGO NAOHISA ,  YOKOTAGAWA TAKANE ,  TAKAHASHI OSAMU ,  AKIYAMA YASUTO ,  ASHIZAWA TADASHI ,  OKAWARA TADASHI

IPC: C07D413/14 ,  A61K31/4709 ,  A61P35/00 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: Disclosed is a STAT3 inhibitor which contains a quinolinecarboxamide derivative represented by formula (I) or a pharmacologically acceptable salt thereof as an active ingredient. (In the formula, W represents a bond or an alkylene chain; X represents O, S or NR34; and R1-R8 and R34 each represents H, a halogen, an alkyl, a phenyl, a furyl, a thienyl or the like.)

公开(公告)号：EA022458B1

公开(公告)日：2016-01-29

申请号：EA201290397

申请日：2010-12-28

Applicant: GEN INC ASS PHARMA VALLEY PROJECT SUPPORTING ORGANISATION ,  SHIZUOKA PREFECTURE ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY ,  YAKULT HONSHA KK

Inventor： ASAI AKIRA ,  MATSUNO KENJI ,  OGO NAOHISA ,  TAKAHASHI OSAMU ,  MASUDA YOSHIAKI ,  MUROYA AYUMU ,  AKIYAMA YASUTO ,  ASHIZAWA TADASHI ,  OKAWARA TADASHI

IPC: C07D413/04 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/55 ,  A61P35/00 ,  A61P43/00 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: Изобретениеотноситсяк 1,3,4-оксадиазол-2-карбоксамидномусоединению, представленномуформулой (Ia), (Ib) и (Ic), гдезначения R, Z, Z, Z, Z, Z, Z, Z, Y и n раскрытыв формулеизобретения, обладающемуингибирующейактивностьюв отношении STAT3 иприменимомув качествепротивораковогосредства.

公开(公告)号：NZ600837A

公开(公告)日：2014-01-31

申请号：NZ60083710

申请日：2010-12-28

Applicant: GEN INC ASS PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION ,  PHARMA DESIGN INC ,  SHIZUOKA PREFECTURE ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY ,  YAKULT HONSHA KK

Inventor： AKIYAMA YASUTO ,  OGO NAOHISA ,  OKAWARA TADASHI ,  TAKAHASHI OSAMU ,  ASAI AKIRA ,  MASUDA YOSHIAKI ,  ASHIZAWA TADASHI ,  MUROYA AYUMU ,  MATSUNO KENJI

IPC: C07D413/04 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/55 ,  A61P35/00 ,  A61P43/00 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: 600837 Disclosed is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Specifically disclosed is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof. (In the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and -X-Y represents a diaryl group such as a biphenyl group.) Specific embodiments of the compound include the following: N-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-3-biphenylcarboxamide; N-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-3-(1-methyl-5-indolinyl)benzenecarboxamide; 4’’-ethoxy-N-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-3-(p-terphenyl)carboxamide; and N-[5-(3-methyl-2-thienyl)-1,3,4-oxadiazol-2-yl]-5-phenyl-2-piperidino-7-thiazolo[4,5-b]pyridinecarboxamide.

公开(公告)号：CA2828934A1

公开(公告)日：2012-09-20

申请号：CA2828934

申请日：2012-03-15

Applicant: KYOWA MEDEX CO LTD ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY

Inventor： KATAYAMA YUKI ,  SUGIUCHI HIROYUKI ,  MATSUSHIMA KAZUMI

IPC: C12Q1/60 ,  C12Q1/26 ,  C12Q1/32 ,  C12Q1/44

Abstract: The present invention provides a simple and accurate method for measuring cholesterol in an HDL subfraction of a test specimen. More specifically, the invention provides a method for measuring cholesterol in the HDL3 subfraction of a test specimen, which is characterized in that the specimen and either (1) a combination of cholesterol ester hydrolase and cholesterol oxidase or (2) a combination of cholesterol ester hydrolase, an oxidized coenzyme, and cholesterol dehydrogenase are reacted in an aqueous medium containing (a) a bivalent metal salt, (b) an alkali metal salt selected from a group consisting of sulfates, nitrates, carbonates, acetates, and halogenates, and (c) dextran sulfate or a salt thereof, and substances that are produced or substances that are consumed are measured without separating and removing lipoproteins other than HDL3.