Suntory Limited

Asubio Pharma Co. Ltd.

Daiichi Suntory Pharma Co., Ltd.

Japan As Represented by President of National Center of Neurology and Psychiatry

Daiichi Asubio Pharma Co., Ltd.

Hirokazu Annoura

Shigeki Tamura

Kyoko Nakanishi

Naohiro Takemoto

Atsuko Fukunaga

Toshio Tatsuoka

Hiroshi Uramoto

Mayumi Uesugi

Norio Inomata

Takashi Yamamura

Kenji Murata

Shinsuke Matsuki

Norihito Murayama

Yoshiko Horikawa

Toshio Tatasuoka

Novel glycolipid derivatives, where the substituent of the sphingosine base part is a short carbon chain alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group and efficient synthetic methods for practical mass production of the same and intermediates useful for the synthesis of these compounds. Glycolipids having the formula (I): where Rindicates a substituted or unsubstituted Cto Clinear alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group, or substituted or unsubstituted aralkyl group and Rindicates a substituted or unsubstituted Cto Calkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group are chemically synthesized.

Glycolipids and synthetic method thereof as well as their synthetic intermediates, and synthetic method thereof

Glycolipids and synthetic method thereof as well as their synthetic intermediates, and synthetic intermediates, and synthetic method thereof

A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein Rto Rindependently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, Rrepresents H, optionally substituted alkyl, aryl, or aralkyl group, Erepresents O, S, or &#x2014;NR, where Rrepresents H, an optionally substituted alkyl, aryl, or aralkyl group, Erepresents O, S, or &#x2014;NR, where Rrepresents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when Erepresents O or S, Edoes not represent O or S, which has an action of suppressing the cytotoxic Caoverload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.

Arylipiperdinopropanol and arylipiperazinopropanol derivatives and pharmaceuticals containing the same

A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Caoverload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I): wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or &#x2014;NHCO(CH)&#x2014; where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.

Arylpiperidinol and arylpiperidine derivatives and pharmaceuticals containing the same

There is provided an aminophenoxyacetic acid derivative of the following formula (I): wherein, R, R, Rand Rare, independent from each other, alkoxy group, alkyl group or aryl group, etc.; Eand Eare oxygen atom, sulfur atom, etc.; n is 0 to 5; X and Y are alkylene group, cycloalkylen group, or alkenylen group; Q is phenyl group which may be substituted or benzoyl group, etc, or a pharmaceutically acceptable salt thereof. These compounds have neuroprotective effects by inducing calbindin D28Kd, one of Ca-binding proteins.

Aminophenoxyacetic acid derivatives and pharmaceutical composition containing thereof

The present invention relates to an aminophenoxyacetamide derivative of the formula (I): wherein Rto Rare, independent from each other, a hydrogen atom or an optionally substituted alkyl group; Eis &#x2014;NR&#x2014;; and Eis an oxygen atom or &#x2014;NR&#x2014;; Q is the group &#x2014;X&#x2014;Y-Q', wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and Y is selected from a group comprising C&#x2550;O, NHC(&#x2550;), and C(&#x2550;O)NH, and Q&#x2032; is a hydrogen atom or a phenyl or pyridyl group which may be substituted; and pharmaceutically acceptable salts thereof. The present invention further relates to compositions comprising compounds of the formula (I) and methods of using said compounds for treating cerebral functional disorders and cerebral organic disorders.

Aminophenoxyacetamide derivatives and pharmaceutical composition containing thereof

There is provided an aminophenoxyacetic acid derivative of the following formula (I):wherein, R, R, Rand Rare, independent from each other, alkoxy group, alkyl group or aryl group, etc.; Eand Eare oxygen atom, sulfur atom, etc.; n is 0 to 5; X and Y are alkylene group, cycloalkylen group, or alkenylen group; Q is pheny group which may be substituted or benzoyl group, etc,or a pharmaceutically acceptable salt thereof. These compounds have neuroprotective effects by inducing calbindin D28Kd, one of Ca-binding proteins.

A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate:wherein Rto Rindependently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, Rrepresents H, optionally substituted alkyl, aryl, or aralkyl group, Erepresents O, S, or &#x2014;NR, where Rrepresents H, an optionally substituted alkyl, aryl, or aralkyl group, Erepresents O, S, or &#x2014;NR, where Rrepresents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when Erepresents O or S, Edoes not represent O or S, which has an action of suppressing the cytotoxic Caoverload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.

Arylpiperidinopropanol and arylpiprazinopropanol derivatives and pharmaceuticals containing the same

Aminophenoxyacetic acid derivatives as neuroprotectants

Arylpiperidinopropanol and arylpiperazinopropanol derivatives and pharmaceuticals containing the same

Medicament for the alleviation or treatment of symptom derived from the ischemic disease and compound useful thereof

Arylpiperidinol and arylpiperidine derivatives and drugs containing the same

Medicament for the alleviation or treatment of symptom derived from

Growing community of inventors

Nagaokakyo, Japan

Hirokazu Annoura