Ishihara Sangyo Kaisha, Ltd.

Shiga University of Medical Science

Hirohiko Kimura

Kazuhiro Yamamoto

Takahiro Haga

Itaru Shigehara

Fuminori Kato

Shinji Odawara

Hideo Sugi

Syuichi Yotsuya

Takashi Okada

Keizo Miyata

Masato Omatsu

Hiroyuki Ikegami

Toshihiko Ueki

Hiromi Takeo

Masayuki Morita

Hiroshi Okada

Tsuyoshi Ueda

Taku Hamamoto

Shuichi Yotsuya

Kazuhisa Kiriyama

Mitsuo Sano

Shigehiro Morikawa

Kotaro Yoshida

Shunji Yuki

Masanari Kato

Kiyoshi Tamai

Hitoshi Nakayama

Makoto Urushitani

Tadao Bamba

Nobuaki Shirai

Ryuji Miyamoto

Tomone Nagae

Daijiro Yanagisawa

Koichi Hirao

Hiroyasu Taguchi

Ikuo Tooyama

Kumiko Azuma

Rie Higuchi

Taki Takenami

Shinya Mori

Disclosed are a curcumin derivative or a salt thereof, which contains a fluorine atom, represented by formula (I): (wherein Rand Rare each independently a hydrogen atom, alkyl, acetyl, or methoxycarbonyl; Rs are each independently a fluorine atom, CHF&#x2014;, CF&#x2014;, CHFO&#x2014;, or CFO&#x2014;; Rs are each independently a hydrogen atom or a fluorine atom; A is alkyl, cyano, carboxyl, alkoxycarbonyl, or R&#x2014;(CH)&#x2014;; Ris hydroxy, carboxy, cyano, acetyloxy, alkoxycarbonyl, alkoxyalkoxy, hydroxyalkoxy, or CONRR; Rand Rare each independently a hydrogen atom or alkyl; and m is an integer from 1 to 5), and a diagnostic imaging agent for diagnosing a disease in which an amyloid &#x3b2; peptide aggregate accumulates, the diagnostic imaging agent containing a compound having a 1,3-dicarbonyl structure, wherein the compound exists in a keto form and an enol form, and the keto form and the enol form have different affinities, respectively, to the amyloid &#x3b2; peptide aggregate.

Imaging diagnostic agent and extracorporeal diagnostic agent for incurable neurological diseases

To provide a novel pesticide. The present invention provides a pesticide containing a pyridyl-triazolopyrimidine derivative represented by the formula (I) or its salt as an active ingredient: wherein Ris substitutable alkyl, substitutable cycloalkyl, substitutable alkenyl, substitutable alkynyl, halogen, cyano, aryl, a heterocyclic group which may be substituted by alkyl, OR, S(O)3? or NRR; Ris hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, acetyl or aryl; Ris alkyl or acetyl; Ris hydrogen or alkyl; Ris hydrogen, alkyl or the like; X is alkyl, alkenyl, alkynyl, halogen, haloalkyl, cyano, nitro or the like; m is an integer of from 1 to 4; and n is an integer of from 0 to 2. 

Pyridyl-triazolopyrimidine derivative or its salt, pesticide containing it and its production process

To provide cytokine production inhibitors useful as preventive or therapeutic medicines for diseases accompanied by hyperactivated immune functions. A cytokine production inhibitor containing, as an active ingredient, a thioamide compound represented by the formula (I) or a salt thereof: wherein A is N, NO, C&#x2014;NOor C&#x2014;CN; Hal is a halogen; Mis alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclyl, amino, O, S, SO or SO; Mis amino, O, S or a single bond; Ris a halogen, alkyl or the like; each of R, R, Rand Ris independently H, alkyl or the like; Ris a halogen, alkyl or the like; Cy is cycloalkyl, cycloalkenyl, aryl or heterocyclyl; each of k, p and q is independently an integer of from 0 to 3; and r is an integer of from 0 to 5.

Thioamides and salts thereof and cytokine production inhibitors containing both

The present invention provides a cytokine production inhibitor containing as an active ingredient an aniline derivative of the formula (I) or a salt thereof: [wherein A is CO or SO; Cy is an aryl group or a heterocyclic group; each of Rand Rwhich are independent of each other, is a halogen atom, a cyano group, a nitro group, an alkyl group which may be substituted, an alkenyl group which may be substituted, an alkynyl group which may be substituted, a cycloalkyl group which may be substituted, a cycloalkenyl group which may be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an amino group which may be substituted or a &#x2014;B-Q group; Ris a -M-M-Rgroup; Ris a hydrogen atom or an alkyl group which may be substituted; x is an integer of from 0 to 5; y is an integer of from 0 to 4; and z is an integer of from 0 to 1].

Aniline derivatives or salts thereof and cytokine production inhibitors containing the same

The present invention provides a preventive or therapeutic medicine for diabetes containing as an active ingredient a fused-heterocyclic compound of the formula (I') or its salt: [wherein G is CN, NO, COR, CHO, SONRRor CONRR; Ris a halogen atom, a &#x2014;O&#x2014;Rgroup or a &#x2014;S&#x2014;Rgroup; Ris a halogen atom, a &#x2014;O&#x2014;Rgroup (wherein Ris as defined above) or an amino group which may be substituted; and each of Rand Rwhich are independent of each other, is a hydrogen atom, a halogen atom or an alkyl group].

Preventive or therapeutic medicines for diabetes containing fused-heterocyclic compounds or their salts

Remedies or preventives for digestive diseases containing diaminotrifluoromethylpyridine derivatives

Medical composition containing nitroetheneamine Derivative or salt there of as active constituent

Medical composition containing nitroetheneamine derivative or salt thereof as active constituent

Pyridazinone derivatives or their salts, processes for their production,

A method of treating rheumatoid arthritis using a diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW.sup.1 R.sup.1, --COCOR.sup.2, --CW.sup.1 NHCOR.sup.2, --C(.dbd.W.sup.1)W.sup.2 R.sup.3 or --CW.sup.1 N(R.sup.4)R.sup.5, and Y is alkyl, --CW.sup.3 R.sup.6, --COCOR.sup.7, --NHCOR.sup.7, --C(.dbd.W.sup.3)W.sup.4 R.sup.8, --(NH).sub.m SO.sub.2 R.sup.9, --(NH).sub.m SO.sub.2 OR.sup.10 or --(NH).sub.m SO.sub.2 N(R.sup.11)R.sup.12, wherein each of R.sup.1, R.sup.6 and R.sup.9, which are independent from one another, is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted or a polycyclic heterocycle group which may be substituted as further defined herein.

Diaminotrifluoromethylpyridine derivatives, process for their production

A diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW.sup.1 R.sup.1, --COCOR.sup.2, --CW.sup.1 NHCOR.sup.2, --C(.dbd.W.sup.1)W.sup.2 R.sup.3 or --CW.sup.1 N(R.sup.4)R.sup.5, and Y is alkyl, --CW.sup.3 R.sup.6, --COCOR.sup.7, --NHCOR.sup.7, --C(.dbd.W.sup.3)W.sup.4 R.sup.8, --(NH).sub.m SO.sub.2 R.sup.9, --(NH).sub.m SO.sub.2 OR.sup.10 or --(NH).sub.m SO.sub.2 N(R.sup.11)R.sup.12, as defined herein.

A diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW.sup.1 R.sup.1, --COCOR.sup.2, --CW.sup.1 NHCOR.sup.2, --C(.dbd.W.sup.1)W.sup.2 R.sup.3 or --CW.sup.1 N(R.sup.4)R.sup.5, and Y is alkyl, --CW.sup.3 R.sup.6, --COCOR.sup.7, --NHCOR.sup.7, --C(.dbd.W.sup.3)W.sup.4 R.sup.8, --(NH).sub.m SO.sub.2 R.sup.9, --(NH).sub.m SO.sub.2 OR.sup.10 or --(NH).sub.m SO.sub.2 N(R.sup.11)R.sup.12, wherein each of R.sup.1, R.sup.6 and R.sup.9, which are independent from one another, is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted or a polycyclic heterocycle group which may be substituted, each of R.sup.2 and R.sup.7, which are independent from each other, is alkyl which may be substituted, alkoxy which may be substituted, phenyl which may be substituted or phenoxy which may be substituted, each of R.sup.3, R.sup.8 and R.sup.10, which are independent from one another, is alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, cycloalkyl which may be substituted, phenyl which may be substituted or benzyl which may be substituted, each of R.sup.4, R.sup.5, R.sup.11 and R.sup.12, which are independent from one another, is alkyl which may be substituted, each of W.sup.1, W.sup.2, W.sup.3 and W.sup.4, which are independent from one another, is an oxygen atom or a sulfur atom, and m is 0 or 1, provided that a combination wherein one of X and Y is --COCF.sub.2 X.sup.1 wherein X.sup.1 is a hydrogen atom, a halogen atom, alkyl or haloalkyl, and the other is --COCF.sub.2 X.sup.2 wherein X.sup.2 is a hydrogen atom, a halogen atom, alkyl, haloalkyl or alkylcarbonyl, or --COOX.sup.3 wherein X.sup.3 is alkyl which may be substituted or phenyl which may be substituted, is excluded.

Diaminotrifluoromethylpyridine compounds and phospholipase A.sub.2

A diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW.sup.1 R.sup.1, --COCOR.sup.2, --CW.sup.1 NHCOR.sup.2, --C(.dbd.W.sup.1 (W.sup.2 W.sup.3 or --CW.sup.1 N(R.sup.4)R.sup.5, and Y is alkyl, --CW.sup.3 R.sup.6, --COCOR.sup.7, --NHCOR.sup.7, --C(.dbd.W.sup.3)W.sup.4 R.sup.8, --(NH).sub.m SO.sub.2 R.sup.9, --(NH).sub.m SO.sub.2 OR.sup.10 or --(NH).sub.m SO.sub.2 N R.sup.11)R.sup.12, wherein each of R.sup.1, R.sup.6 and R.sup.9, which are independent from one another, is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted or a polycyclic heterocycle group which may be substituted, each of R.sup.2 and R.sup.7, which are independent from each other, is alkyl which may be substituted, alkoxy which may be substituted, phenyl which may be substituted or phenoxy which may be substituted, each of R.sup.3, R.sup.8 and R.sup.10, which are independent from one another, is alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, cycloalkyl which may be substituted, phenyl which may be substituted or benzyl which may be substituted, each of R.sup.4, R.sup.5, R.sup.11 and R.sup.12, which are independent from one another, is alkyl which may be substituted, each of W.sup.1, W.sup.2, W.sup.3 and W.sup.4, which are independent from one another, is an oxygen atom or a sulfur atom, and m is 0 or 1, provided that a combination wherein one of X and Y is --COCF.sub.2 X.sup.1 wherein X.sup.1 is a hydrogen atom, a halogen atom, alkyl or haloalkyl, and the other is --COCF.sub.2 X.sup.2 wherein X.sub.2 is a hydrogen atom, a halogen atom, alkyl, haloalkyl or alkylcarbonyl, or --COOX.sup.3 wherein X.sup.3 is alkyl which may be substituted or phenyl which may be substituted, is excluded.

Diaminotrifluoromethylpyridine derivatives and phospholipase A.sub.2

Growing community of inventors

Shiga, Japan

Hirohiko Kimura