Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Naoki Yoneda

Makoto Kotake

Kazutoshi Miyake

Toshiyuki Matsuoka

Masayuki Matsukura

Tomohiro Matsushima

Nobuyuki Mori

Hiroki Ishihara

Masanori Mizuno

Mamoru Saito

Shinji Suda

Jean-Christophe P Harmange

Shigeru Souda

Norio Minami

Mark Spyvee

Shigeto Negi

Seiichi Kobayashi

Tetsuya Kawahara

Kenzo Muramoto

Hitoshi Oinuma

Satoshi Yamamoto

Sachiyuki Hamano

Atsushi Inoue

Yoshiyuki Kawakami

Hong Du

Hiroshi Shirota

Shinsuke Hirota

Kenichi Chiba

Yoshiharu Mizui

Isao Tanaka

Fabian Gusovsky

Masaki Goto

Hideki Sakurai

Masanori Fujita

Yoshikazu Kuboi

John (Yuan) Wang

Yoshihito Eguchi

Akifumi Kimura

Takatoshi Kawai

Takashi Musha

Masayuki Namiki

Takeshi Sudo

Yong-Chun Shen

Osamu Hiroshima

Megumi Kawada

Makoto Okita

Toshiaki Ogawa

Hideyuki Adachi

Roch Boivin

Yoshiharu Daiku

Yimin Jiang

Kenichi Nomoto

Yoshio Fukuda

Xiang-Yi Li

Makoto Kaino

Tadanobu Takamura

Jesse Chow

Charles-André Lemelin

Koichi Nose

Masayoshi Ohkuro

Naoya Kishi

Fusayo Yoshida

Keizoh Satoh

Mikio Tomimatsu

Mitsuaki Miyamoto

Richard S Clark

Motosuke Yamanaka

Kenji Hayashi

Ichiro Yoshida

Fumiyoshi Matsuura

Yasutaka Takase

Junichi Kamata

Tomonori Hoshiko

Yoshiaki Ohashi

Hiromitsu Yokohama

Shuichi Suzuki

Yoshinori Sakuma

Daisuke Iida

Manabu Shirato

Hidenori Seshimo

So Yasui

Mitsumasa Shino

Ray Wood

Yasuaki Kamada

Toshiyuki Ohfusa

Katsunobu Osada

Futoshi Miyazaki

Daiya Shimokubo

John (yuan) Wang

The disclosure provides pyrazolo[1,5-a]pyrimidine compounds, and pharmaceutically acceptable salts thereof, having protease-activated receptor 2 (PAR2) inhibitory action, pharmaceutical compositions containing the same, and methods of treatment using the same.

Pyrazolo[1,5-a]pyrimidine compound

The present invention provides methods for the use of compounds having formula (I) in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R-R, t, X, Y, Z, and n are as defined herein.

Macrocyclic compounds useful as pharmaceuticals

The present invention provides compositions comprising compounds having formula (I): 

Salts and crystals of 1-cyclopropylmethyl-4-[2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine have excellent cell adhesion inhibitory action and cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis.

Crystal and salt of 1-cyclopropylmethyl-4-[2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine

The present invention provides compounds having formula (I): 

In one aspect, the present invention provides compounds having formula (1) or (100), a salt thereof or a hydrate of the foregoing, which compounds exhibit excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome; rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis.  wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.

1,2-di(cyclic)substituted benzene compounds

A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. 

The present invention discloses compounds and compositions of formula (I): having inhibitory activity on activation of STAT6, wherein X represents quinoline, isoquinoline, quinazoline or imidazopyridine; Y represents phenyl, piperazine, pyridine, thiophene, thiazole, oxathiazole or oxathiadiazole; and variables Z, n, R, R, Rand Rare as defined in the claims.

Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof

The present invention relates to a substituted thiazolo[3,2-a] azepine derivative having inhibitory activity against angiotensin I converting enzyme and neutral endpeptidase and is represented by the following general formula (I): ##STR1##

Substituted thiazolo[3,2-a]azepine derivatives

Substituted thiazolo �3,2-a!azepine derivatives

The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity. This amino acid derivative is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or an acyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent;

Amino acid derivative

Propenoic acid derivatives of the formula: ##STR1## where R.sup.15 and R.sup.17 are aryl or heteroalkyl groups and R.sup.16 and R.sup.18 are hydrogen, a lower alkyl or the like are intermediates used to prepare pharmaceutically active diazole propenoic acid compounds.

Diazole-propenoic acid compounds

A novel propenoic acid derivative which exhibits adenosine A1 antagonism is defined by the general formula (I): ##STR1## (wherein A represents an aromatic ring; R.sup.1 represents aryl or the like; R.sup.2, R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like; and R.sup.7 and R.sup.8 each represent lower alkyl or the like) or a pharmacologically acceptable salt thereof.

Propenoic acid derivatives diazole propenoic acid compounds which have

The biphenylmethane derivative having the formula (I) is useful to prevent and treat hypertension and cardiac failure. ##STR1## in which R1 is hydrogen, an alkyl, a cycloalkyl, a halogenated alkyl, --S--R7, --SO2--R7, --C.tbd.C--R7 or --(CH2)p--OR7, R7 being hydrogen, an alkyl, a cycloalkyl or a halogenated alkyl, p being zero or 1, --A1=A2--A3=A4-- is --CH=CH--CH=CH--, --N=CH--CH=CH--, --CH=N--CH=CH--, --CH=CH--N=CH--, --CH=CH--CH=N-- or --CH=N--CH=N--, R2 and R3 are each hydrogen, a halogen, a lower alkyl, a lower alkoxy, a carbamoyl or cyano, R4 is hydrogen or a lower alkyl, R5 is 1H-tetrazol-5-yl, carboxyl (--COOH) or a carboxylic ester and R6 is hydrogen, a halogen, hydroxyl or a lower alkoxy, or a pharmacologically acceptable salt thereof.

Biphenylmethane derivative and pharmacological use

A pyrrolidine compound having the following formula and a pharmacologically acceptable salt thereof is disclosed. It is useful in the pharmaceutical field. ##STR1## in which X is hydrogen, a halogen, or a lower alkyl, Y is --(CH2)n--, n being zero, 1 or 2, --S(O)p--, p being zero, 1 or 2, --O--, or --NH-- and R is phenyl, a substituent-having phenyl, naphtyl, a substituent-having naphthyl, a heteroaryl or a substituent-having heteroaryl.

Pyrrolidine compound and pharmaceutical use

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Tsukuba, Japan

Naoki Yoneda