Daiichi Sankyo Company, Limited

Sankyo Company, Limited

Sanford Burnham Prebys Medical Discovery Institute

Shojiro Miyazaki

Takahide Nishi

Futoshi Nara

Takaichi Shimozato

Anthony B Pinkerton

Yuko Yamamoto

Masanori Izumi

Masaharu Inui

Kaori Soma

Keisuke Suzuki

Taeko Shinozaki

Yuji Nakamura

Yasuyuki Ogawa

Takahiro Nagayama

Toshiyasu Takemoto

Masamichi Kishida

Taro Tokui

Yasunobu Kurosaki

Takashi Izumi

The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof. 

Sulfonamide compounds

The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I): wherein Rrepresents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, Rand Rare the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, Rand Rare the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, Rrepresents a hydrogen atom or the like, each Rmay be the same or different and may each represent an optionally substituted C1-6 alkoxy group or the like, X represents &#x2014;CH&#x2550;, &#x2014;C(&#x2014;R)&#x2550;, or &#x2014;N&#x2550;, and m represents 1 to 4, or a pharmacologically acceptable salt thereof.

Pyridine compounds

The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I): wherein Rrepresents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, Rand Rare the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R4 and R5 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, Rrepresents a hydrogen atom or the like, each Rmay be the same or different and may each represent an optionally substituted C1-6 alkoxy group or the like, X represents &#x2014;CH&#x2550;, &#x2014;C(&#x2014;R)&#x2550;, or &#x2014;N&#x2550;, and m represents 1 to 4, or a pharmacologically acceptable salt thereof. 

The present invention provides an excellent antihypertensive medicament. The medicament of the present invention comprises a compound having the general formula (I) and the like: 

Cyclic amine compound

A method for treating an immunology-related disease. The method involves administering to a mammal in need thereof a pharmaceutically effective amount of an amino acid compound, a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof. The compound has the following formula: wherein Rand Rare each hydrogen; Ris hydrogen; Ris C-Calkyl; n is 2; X is &#x2550;N-D, wherein D is hydrogen, C-Calkyl or phenyl; Y is ethylene, ethynylene, &#x2014;CO&#x2014;CHor phenylene; Z is ethylene or trimethylene; Ris unsubstituted C-Ccycloalkyl, unsubstituted C-Caryl, or C-Ccycloalkyl or C-Caryl substituted with 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, halogeno lower alkyl and lower alkoxy; and Rand Rare each hydrogen.

Method for treating a immunology-related disease

A compound having a formula II(a): wherein Rand Rare hydrogen lower alkyl, lower aliphatic acyl, or lower alkoxycarbonyl; Ris C-Calkyl; n is 2 or 3; X is a formula &#x2550;N-D, wherein D is hydrogen, C-Calkyl or phenyl; Y is ethylene, ethynylene, &#x2014;CO&#x2014;CH&#x2014;, &#x2014;CH(OH)&#x2014;CH&#x2014; or phenylene; Z is C-Calkylene; Ris C-Ccycloalkyl or C-Caryl; Rand Rare hydrogen, lower alkyl, halogeno lower alkyl, lower alkoxy or lower alkylthio; and Rand Rare hydrogen or lower alkyl.

Amino alcohol compounds or phosphonic acid derivatives thereof

A method for suppressing the number of peripheral blood lymphocytes involving administering to a human in need thereof a pharmaceutically effective amount of a compound which is (2R) -2-amino-2-methyl-4-{1-methyl-5-[4-(4-methylphenyl)butanoyl]pyrrol-2-yl}butan-1-ol or a pharmacologically acceptable salt thereof, such as the hydrochloride salt.

Method for suppressing the number of peripheral blood lymphocytes using an amino alcohol compound

A method for the prevention or treatment of an immunology-related disease, which is not rheumatoid arthritis or psoriasis, in a mammal in need thereof which involves administering to the mammal a pharmaceutically effective amount of a compound, a pharmacologically acceptable salt of the compound or a pharmacologically acceptable ester of the compound, wherein the compound is a compound having a formula (Ia): wherein Rand Rare each a hydrogen, Ris hydrogen; Ris C-Calkyl; n is 2; X is &#x2550;N&#x2014;D, wherein D is hydrogen C-Calkyl or phenyl; Y is ethylene, ethynylene, &#x2014;CO&#x2014;CHor phenylene; Z is ethylene or trimethylene; Ris an unsubstituted C-Ccycloalkyl, an unsubstituted C-Caryl, or a C-Ccycloalkyl or a C-Caryl substituted with 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, halogeno lower alkyl and lower alkoxy; and Rand Rare each hydrogen.

Amino alcohol compounds and phosphonic acid compounds having excellent immunosuppressive activity, pharmacologically acceptable salts thereof and pharmacologically acceptable esters thereof, and pharmaceutical compositions comprising such compounds, the compounds having the following formula: wherein Rand Reach represent hydrogen, or a protecting group of the amino group; Rrepresents hydrogen, or a protecting group of the hydroxyl group; Rrepresents a lower alkyl group; n is 1 to 6; X represents oxygen or nitrogen, which is unsubstituted or substituted with a lower alkyl group; Y represents ethylene; Z represents a C&#x2013;Calkylene; Rrepresents an aryl group; and Rand Reach represents hydrogen; provided that when Rrepresents hydrogen, then Z represents a group other than a single bond or a straight chain C&#x2013;Calkylene group.

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Tokyo, Japan

Shojiro Miyazaki