Eisai R&d Management Co., Ltd.

Eiichi Yamamoto

Keigo Tanaka

Jun Niijima

Osamu Asano

Masayuki Matsukura

Naoki Asakawa

Kazutaka Nakamoto

Kazumasa Nara

Naoaki Watanabe

Kaoru Murata

Takuma Minamisono

Crystals, amorphous substances, salts, and hydrates of a salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid having PDE4 inhibitory action are provided. These compounds are useful for treating allergic diseases such as atopic dermatitis.

Crystals, amorphous substances or salts of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl) phenyl] terephthalamic acid

Anti-fungal agent having excellent anti-fungal action physicochemical properties including safety and water solubility. Compound represented by formula (I), or salt thereof: wherein Rrepresents hydrogen, halogen, amino, R&#x2014;NH&#x2014; wherein Rrepresents Calkyl, hydroxy Calkyl, Calkoxy Calkyl, or Calkoxycarbonyl Calkyl, R&#x2014;(CO)&#x2014;NH&#x2014; wherein Rrepresents Calkyl group or Calkoxy Calkyl, Calkyl, hydroxy Calkyl, cyano Calkyl, Calkoxy, or Calkoxy Calkyl or a phosphonoamino group; Rrepresents hydrogen, Calkyl, amino, or a di Calkylamino group or a phosphonoamino group; one of X and Y is nitrogen while the other is nitrogen or oxygen; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom or 1 or 2 Calkyl groups; Z represents a single bond, a methylene group, an ethylene group, oxygen, sulfur, &#x2014;CHO&#x2014;, &#x2014;OCH&#x2014;, &#x2014;NH&#x2014;, &#x2014;CHNH&#x2014;, &#x2014;NHCH&#x2014;, &#x2014;CHS&#x2014;, or &#x2014;SCH&#x2014;; Rrepresents hydrogen or halogen or Calkyl, Ccycloalkyl, Caryl, a 5- or 6-member heteroaryl group or a 5- or 6-member nonaromatic heterocyclic group which may have 1 or 2 substituents; and Rrepresents hydrogen or halogen; provided that either Ror Rrepresents a phosphonoamino group.

Pyridine derivatives substituted by heterocyclic ring and phosphonoamino group, and anti-fungal agent containing same

There is provided a heterocycle-substituted pyridine derivative's salt or a crystal thereof. The present invention provides an acid addition salt of 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-yl amine or a crystal thereof as well as process for producing the same.

Heterocycle-substituted pyridine derivative's salt or crystal thereof

Novel &#x3b2;-type crystal of N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide of the formula: characterized in, for example, that in powder X-ray diffractometry, it has a diffraction peak at a diffraction angle (2&#x3b8;&#xb1;0.2&#xb0;) of 18.4&#xb0;. This crystal has favorable properties, such as high solubility in buffer solutions and various organic solvents, and is suitable to an active ingredient of a pharmaceutical composition for use as an antitumor agent, an activated lymphocyte suppressor or an eating enhancer.

Crystal of two-ring heterocyclic sulfonamide compound

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Tsukuba, Japan

Eiichi Yamamoto