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ANTIPRURITIC AGENT

Foreign code F110006064
File No. S2010-0110
Posted date Dec 28, 2011
Country WIPO
International application number 2010JP068695
International publication number WO 2011049200
Date of international filing Oct 22, 2010
Date of international publication Apr 28, 2011
Priority data
  • P2009-244528 (Oct 23, 2009) JP
Title ANTIPRURITIC AGENT
Abstract Provided is a faster-acting antipruritic agent which has little side effects and is efficacious in treating strongly itchy skin diseases such as atopic dermatitis, characterized by comprising, as the active ingredient, a cholecystokinin 2 acceptor agonist such as a peptide having an amino acid sequence that is homologous with a partial amino acid sequence consisting of 7 or more amino acids from the C-terminal side of a peptide having the amino acid sequence represented by SEQ ID NO:1. Val-Ser-Gln-Arg-Thr-Asp-Gly-Glu-Ser-Arg-Ala-His-Leu-Gly-Ala-Leu-Leu-Ala-Arg-Tyr-Ile-Gln-Gln-Ala-Arg-Lys-Ala-Pro-Ser-Gly-Arg-Met-Ser-Ile-Val-Lys-Asn-Leu-Gln-Asn-Leu-Asp-Pro-Ser-His-Arg-Ile-Ser-Asp-Arg-Asp-Tyr(SO3H)-Met-Gly-Trp-Met-Asp-Phe-NH2 [SEQ ID NO:1]
Outline of related art and contending technology BACKGROUND ART
Atopic dermatitis, contact dermatitis, hives, itching the disorder of the skin such as prurigo (itching: skin scratching the unpleasant sensation of the skin as desired) are often accompanied by. Is itching, scratching it induces to increase due to the behaviors of the exacerbation of the lesions and itching as well as cause a vicious circle, the operation in the daily life and working efficiency is lowered, which results in reduced sleep also inhibit QOL. Therefore, the suppression of itching, skin with a suppression of the inflammatory response in skin is important in the treatment of a disease.
Treatment of skin diseases, various types of synthetic steroid agent has been widely used, with a marked therapeutic effect has been mentioned. However, for use in the steroid is, the effect of preventing the itching does not have to directly, indirectly by suppressing the inflammatory response is effective to suppress the irritation considered. Such as in atopic dermatitis is pruritus, allergic reaction type I derived from mast cells by the phenomenon that is caused by histamine had the thought, for suppression of pruritus, antihistamines and anti-allergy medication is administered as Pnnciples or for use in many cases.
In recent years, including tacrolimus immunosuppressive agent is to be used also for use in (for example, see non-patent document 1). Also tacrolimus, steroids for use in the same manner, the primary mechanism of action inflammation and suppress the reaction but, atopic dermatitis skin disease from the experiments using the mouse disease models, inhibition of scratching behavior by tacrolimus have been observed (for example, see non-patent document 2).
In addition, conventional treatment cannot control severe atopic dermatitis patient, recent exclusively as a steroid for use in the difficulty of using pharmaceuticals for, oral cyclosporine immunosuppressive agent has been studied (for example, see non-patent document 3) and, in regard to, under certain conditions, the use of severe atopic dermatitis is authorized to the patient.
Another approach, itching and skin inflammation reaction or a chemical method for modulating the genetic level has been studied. For example, in patent document 1, which is a kind of neuropeptide cholecystokinin or its analogs containing a, containing a protein of a particular cell regeneration, growth or differentiation-regulating agents and it can be administered, obesity, diabetes, immune system disorders, liver disease, a digestive system disease such as cosmetic surgery at the time of tissue damage or cell regeneration, proliferation or differentiation are methods for treating diseases involving the disclosed, as a specific example, immune system disorders such as atopic dermatitis or as therapeutic agents for the prevention and/of disclosed the use of cholecystokinin.
In addition, Patent Document 2 is, as the active ingredient at least one pharmaceutical agent 1, at least one 1 in order to increase the uptake of a pharmaceutical agent in vivo or in a mixture of a liquid and nanostructures, a pharmaceutical composition comprising a liquid and the disclosed invention, as one embodiment of the invention, using the agent for the treatment of itching neuropeptide disclosed.
Scope of claims (In Japanese)請求の範囲 [請求項1]
 コレシストキニン2受容体(CCK2R)アゴニストを有効成分として含有することを特徴とする掻痒抑制剤。

[請求項2]
 前記コレシストキニン2受容体アゴニストが、
(1)下記の配列番号1で表されるアミノ酸配列を有するペプチドのC末端側から7個以上の部分アミノ酸配列と相同なアミノ酸配列を有するペプチド、および
 Val-Ser-Gln-Arg-Thr-Asp-Gly-Glu-Ser-Arg-Ala-His-Leu-Gly-Ala-Leu-Leu-Ala-Arg-Tyr-Ile-Gln-Gln-Ala-Arg-Lys-Ala-Pro-Ser-Gly-Arg-Met-Ser-Ile-Val-Lys-Asn-Leu-Gln-Asn-Leu-Asp-Pro-Ser-His-Arg-Ile-Ser-Asp-Arg-Asp-Tyr(SO 3H)-Met-Gly-Trp-Met-Asp-Phe-NH 2 [配列番号1]
(なお、配列番号1で表されるアミノ酸配列において、Tyr(SO 3H)はO-硫酸化チロシンまたはその塩を表す。)
(2)上記(1)のアミノ酸配列において、1もしくは複数のアミノ酸が欠失、置換もしくは付加されたアミノ酸配列からなり、かつCCK2Rアゴニスト活性を有するペプチドからなる群より選択される1または複数であることを特徴とする請求項1記載の掻痒抑制剤。

[請求項3]
 前記コレシストキニン2受容体アゴニストが、下記の配列番号2で表されるアミノ酸配列からなるペプチドおよび/または下記の配列番号3で表されるアミノ酸配列からなるペプチドであることを特徴とする請求項2記載の掻痒抑制剤。
 Asp-Tyr(SO 3H)-Met-Gly-Trp-Met-Asp-Phe-NH 2 [配列番号2]
 Tyr(SO 3H)-Met-Gly-Trp-Met-Asp-Phe-NH 2   [配列番号3]

[請求項4]
 肥満細胞の脱顆粒を抑制することを特徴とする請求項1から3のいずれか1項記載の掻痒抑制剤。

[請求項5]
 注射剤、軟膏剤、クリーム剤、外用液剤、スプレー剤、貼付剤およびゲル剤のいずれかである請求項1から4のいずれか1項記載の掻痒抑制剤。

  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • UNIVERSITY OF OCCUPATIONAL AND ENVIRONMENTAL HEALTH, JAPAN
  • Inventor
  • TOKURA, Yoshiki
  • FUKAMACHI, Akiko
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IS JP KE KG KM KN KP KR KZ LA LC LK LR LS LT LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PE PG PH PL PT RO RS RU SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ MD RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

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