Sankyo Company, Limited

Daiichi Sankyo Company, Limited

The University of Tokyo

Takaichi Shimozato

Takahide Nishi

Futoshi Nara

Shojiro Miyazaki

Toshiyasu Takemoto

Kensuke Nakamura

Takashi Isobe

Toshiyuki Shimizu

Kensuke Miyake

Takashi Kagari

Jun Ishiguro

Atsuo Kanno

Yuji Motoi

Yusuke Murakami

Atsushi Manno

Umeharu Ohto

Tsuyoshi Nakamura

Yukiko Sekiguchi

Takashi Izumi

Yumiko Mizuno

Hiromi Doi

The present invention provides a pharmaceutical composition comprising an antibody which binds specifically to human TLR7 or monkey TLR7 and does not bind to mouse TLR7 or rat TLR7, and has an activity of inhibiting a function of human TLR7 or monkey TLR7, and the like.

Anti-human TLR7 antibody

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 compound having immunosuppressive activity with low toxicity or a pharmacological salt thereof. The compound has a general formula (I) shown below or a pharmacologically acceptable salt thereof, or a pharmacologically acceptable prodrug thereof 

Heterocyclic 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.

Amino alcohol compounds

Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof, esters thereof or other derivatives:wherein Rand Rare a hydrogen atom, an amino protecting group; Ris a hydrogen atom, a hydroxy protecting group; Ris a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C-Calkylene group, a C-Calkylene group substituted with 1 to 3 substituents selected from substituent group a and b; Ris an aryl group; Rand Rare a hydrogen atom, a group selected from substituent group a; with the proviso when Ris a hydrogen atom, Y is not a single bond or a straight chain C-Calkylene group.

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Miura, Japan

Takaichi Shimozato