PHARMACEUTICAL COMPOSITION HAVING ANTI-CANCER IMMUNOSTIMULATING EFFECT AND/OR IMMUNE CHECKPOINT INHIBITION POTENTIATING EFFECT

WIPO Patent Application WO/2023/068376

A1

Provided is a pharmaceutical composition which is effective as an anti-cancer immunostimulating therapy. Said pharmaceutical composition has a compound set forth in general formula (I) or a salt thereof as an active ingredient {in the formula, one of X1 and X2 is a hydroxy group, a morpholino alkylcarbonyloxy group, an alkylcarbonyloxy group, a phosphate group, an alkoxy group, a di(alkyl)amino alkyl triazolyl group, an acetoxy group in which at least one hydrogen atom may be halogenated, an azide group, or a sulfate group, and the other is a hydrogen atom. Alternatively, X1 and X2 together represent an oxo group. Y represents a C1-6 alkyl group or a hydrogen atom. Z1 and Z2 are different and represent a group represented by formula (II), a hydroxy group, an ethynyl group, an alkylcarbonyloxy group, a hydrogen atom, or a heterocyclic ring group which may have a substituent. Alternatively, Z1 and Z2 together represent an oxo group. The double line formed from a solid line and a dotted line means a single bond or a double bond. The symbols in formula (II) are as follows: R1 is an alkyl group or a hydrogen atom; R2 is a hydroxy group, an alkyl group, an alkoxy group, a group represented by formula (III) [in formula (III), * means a bond with a carbon atom of the carbonyl group in formula (II)], or -N(R3)(R4) (R3 and R4 are the same or different, and are a hydrogen atom, an alkyl group, a phenyl alkyl group, or a group represented by formula (IV) (in formula (IV), p is an integer from 1-10 and * means a bond with a carbon atom of the carbonyl group in formula (II)). Alternatively, R3 and R4 together form a heterocyclic ring together with a nitrogen atom); n is an integer which is 0, 1, or 2; and m is an integer which is 1 or 0}.

FUKUI YOSHINORI (JP)
URUNO TAKEHITO (JP)
HONMA TERUKI (JP)
TAKAYA DAISUKE (JP)
KANAI MOTOMU (JP)
OISAKI KOUNOSUKE (JP)
TOGO TAKAYA (JP)
SUGIURA YUKI (JP)

PCT/JP2022/039416

April 27, 2023

October 21, 2022

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UNIV KYUSHU NAT UNIV CORP (JP)
RIKEN (JP)
UNIV TOKYO (JP)
UNIV KEIO (JP)

A61K31/575; A61K31/57; A61K31/58; A61K39/395; A61K45/00; A61P35/00; A61P37/02; A61P43/00; C07J9/00; C07K16/28; C12N15/13

WO2017086436A1

2017-05-26

CN108727453A	2018-11-02
JP2003342176A	2003-12-03
JP2002502423A	2002-01-22
JP2002514168A	2002-05-14

TATSUGUCHI TAKAAKI; URUNO TAKEHITO; SUGIURA YUKI; OISAKI KOUNOSUKE; TAKAYA DAISUKE; SAKATA DAIJI; IZUMI YOSHIHIRO; TOGO TAKAYA; HA: "Pharmacological intervention of cholesterol sulfate-mediated T cell exclusion promotes antitumor immunity", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, ELSEVIER, AMSTERDAM NL, vol. 609, 10 April 2022 (2022-04-10), Amsterdam NL , pages 183 - 188, XP087047434, ISSN: 0006-291X, DOI: 10.1016/j.bbrc.2022.04.035
TATSUGUCHI TAKAAKI, URUNO TAKEHITO, SUGIURA YUKI, SAKATA DAIJI, IZUMI YOSHIHIRO, SAKURAI TETSUYA, HATTORI YUKO, OKI EIJI, KUBOTA N: "Cancer-derived cholesterol sulfate is a key mediator to prevent tumor infiltration by effector T cells", INTERNATIONAL IMMUNOLOGY, vol. 34, no. 5, 20 April 2022 (2022-04-20), pages 277 - 289, XP093058024, DOI: 10.1093/intimm/dxac002
DATABASE Registry 13 May 2011 (2011-05-13), ANONYMOUS : "Pregn-5-en-20-one, 17-(a cetyloxy)-3-hydroxy -, (3β,17ξ)-(CA INDE X NAME) OTHER CA INDEX NAME S", XP093059944, retrieved from STN Database accession no. RN 1294502-87-6

SAEGUSA & PARTNERS (JP)

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