Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Hitoshi Oinuma

Norio Minami

Kazutoshi Miyake

Yoshiharu Daiku

Kenichi Nomoto

Motosuke Yamanaka

Takashi Hasegawa

Tadao Shoji

Tomonori Hoshiko

Kohei Sawada

Fumihiro Ozaki

Hideyuki Adachi

Toshiaki Ogawa

Yasuhiro Kabasawa

Keiji Ishibashi

Nobuyuki Mori

Shigeru Souda

Nobuaki Sato

Motohiro Soejima

Naoki Yoneda

Sachiyuki Hamano

Toshihiko Naito

Makoto Kotake

Takashi Doko

Taro Terauchi

Norihito Ohi

Toshiyuki Matsuoka

Mamoru Saito

Shinji Suda

Hiroshi Katoh

Kohtarou Kodama

Tadanobu Takamura

Hidenori Seshimo

Naohiro Kohmura

Masayuki Namiki

Takeshi Sudo

Hideto Ohara

Makoto Okita

Tomohiro Matsushima

Satoshi Katayama

Yoshio Fukuda

Masanori Mizuno

Katsuhiro Moriya

Manabu Shirato

Kenji Hayashi

Afzal Khan

Piotr Pawel Graczyk

Gurpreet Singh Bhatia

Darren Peter Medland

Vanessa Palmer

Hirotoshi Numata

The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.  Wherein Ris a C-Caromatic cyclic hydrocarbon group etc.; R, Rand Reach independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C-Calkylene group etc.; X is a single bond, or a group represented by &#x2014;CO&#x2014;NH&#x2014; or &#x2014;NH&#x2014;CO&#x2014;, etc.; and Y is a C-Ccycloalkyl group, a C-Caromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.

[object Object]

The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Ris a C-Caromatic cyclic hydrocarbon group etc.; R, Rand Reach independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C-Calkylene group etc.; X is a single bond, or a group represented by &#x2014;CO&#x2014;NH&#x2014; or &#x2014;NH&#x2014;CO&#x2014;, etc.; and Y is a C-Ccycloalkyl group, a C-Caromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.

1H-indazole compounds

The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.

Jun kinase inhibitors

The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.Wherein Ris a C-Caromatic cyclic hydrocarbon group etc.; R, Rand Reach independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C-Calkylene group etc.; X is a single bond, or a group represented by &#x2014;CO&#x2014;NH&#x2014; or &#x2014;NH&#x2014;CO&#x2014;, etc.; and Y is a C-Ccycloalkyl group, a C-Caromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.

1H-indazole compound

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

A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.

Benzenesulfonamide derivatives

To provide a novel cyclohexane derivative, a cyclohexane derivative is defined by the formula (I) or a pharmacologically acceptable salt thereof: ##STR1## (wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represents hydrogen or lower alkyl; R.sup.3 represents optionally substituted aryl or optionally substituted heteroaryl; X represents oxygen or sulfur; and Y represents a group represented by the formula: ##STR2## or the like). The compound of the present invention is useful as a preventive and therapeutic agent for diseases against which a potassium channel opening action is efficacious.

Cyclohexane derivatives

The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like];

Thioformamide derivatives

The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like]; Z represents --CH.sub.2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl or the like; and R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like.

To provide a cyclohexane derivative defined by the formula (I) or a pharmacologically acceptable salt thereof: ##STR1## (wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represents hydrogen or lower alkyl; R.sup.3 represents optionally substituted aryl or optionally substituted heteroaryl; X represents oxygen or sulfur; and Y represents a group represented by the formula: ##STR2## or the like). The compound of the present invention is useful as a preventive and therapeutic agent for diseases against which a potassium channel opening action is efficacious.

Thioformamide derivatives having hypotensive activity

Growing community of inventors

Ibaraki, Japan

Hitoshi Oinuma