Title:
LITHOCHOLIC ACID DERIVATIVE HAVING VITAMIN D ACTIVITY
Document Type and Number:
WIPO Patent Application WO/2021/033766
Kind Code:
A1
Abstract:
The purpose of the present invention is to provide a novel lithocholic acid derivative having sufficient vitamin D3 activity. A compound represented in general formula (I), a salt thereof, or a prodrug thereof is provided. (R1 and R2 independently represent a hydrogen atom or an alkyl group with a carbon number of 1-8. n represents an integer 1-3. X represents -C(=O)NH-Z, or -CH(OH)-(Y)m-CH(OH)R3. Z represents a hydrogen atom, an alkyl group with carbon number 1-8, an alkoxyl group with carbon number 1-8, or a hydroxyl group, Y represents -C(R4)(R5)-, -C(=O)-, or -C(=CH2)-, and m represents an integer 0-3. R3, R4 and R5 independently represent a hydrogen atom or an alkyl group with carbon number 1-8. Alkyl groups with carbon number 1-8 represented by Z, R3, R4 and R5 may optionally have a substituent selected from a carboxylic group or a hydroxyl group.)
Inventors:
TANATANI AYA (JP)
YOSHIOKA CHISAKI (JP)
YOSHIHARA AYANA (JP)
KAGECHIKA HIROYUKI (JP)
MASUNO HIROYUKI (JP)
YOSHIOKA CHISAKI (JP)
YOSHIHARA AYANA (JP)
KAGECHIKA HIROYUKI (JP)
MASUNO HIROYUKI (JP)
Application Number:
PCT/JP2020/031642
Publication Date:
February 25, 2021
Filing Date:
August 21, 2020
Export Citation:
Assignee:
UNIV OCHANOMIZU (JP)
UNIV NAT CORP TOKYO MEDICAL & DENTAL (JP)
UNIV NAT CORP TOKYO MEDICAL & DENTAL (JP)
International Classes:
A61P3/02; A61K31/575; A61P43/00; C07J9/00
Domestic Patent References:
| WO2017131144A1 | 2017-08-03 |
Foreign References:
| JP2005507855A | 2005-03-24 | |||
| CN109364084A | 2019-02-22 |
Other References:
"Structure-activity relationship of a novel non-secosteroid type VDR ligand using lithocholic acid as a lead compound", LECTURE ABSTRACTS OF 29TH ACADEMIC CONFERENCE OF JAPANESE SOCIETY FOR RETIONOID RESEARCH, 9 February 2018 (2018-02-09), pages 31
"Fabrication of lithocholic acid amide derivatives with vitamin D activity", LECTURE ABSTRACT OF THE 139TH ANNUAL MEETING OF THE, 19 March 2019 (2019-03-19), Retrieved from the Internet
"Fabrication of lithocholic acid derivatives with diol groups in the side chains and vitamin D activity", LECTURE ABSTRACTS OF THE 37TH MEDICINAL CHEMISTRY SYMPOSIUM, 5 November 2019 (2019-11-05), pages 111
"Fabrication of lithocholic acid amide derivatives with vitamin D activity", LECTURE ABSTRACTS OF THE 37TH MEDICINAL CHEMISTRY SYMPOSIUM, 5 November 2019 (2019-11-05), pages 119
"Structure evolution of lithocholic acid derivatives with vitamin D activity", VITAMINS, vol. 93, no. 8, 25 August 2019 (2019-08-25), pages 370 - 371
ROMBUNNO, LECTURE ABSTRACT OF THE 140TH ANNUAL MEETING OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 31 March 2020 (2020-03-31)
"Fabrication of lithocholic acid side chain derivatives with high vitamin D activity", VITAMINS, vol. 94, no. 4, 25 April 2020 (2020-04-25), pages 287
ROMBUNNO: "Carborane-containing carboxylic acid derivative with vitamin D activity", LECTURE ABSTRACT OF THE 138TH ANNUAL MEETING OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 2018
"Development of novel Vitamin D Derivatives", CLINICAL CALCIUM, vol. 27, no. 11, 2017, pages 1579 - 1586
HOSHITA, NOBUHIKO, OKUDA, KYUICHIRO: "Partial Synthesis of Stero-bile Acids Related to Chenodeoxycholic Acid", JOURNAL OF BIOCHEMISTRY, vol. 62, no. 6, 1967, pages 655 - 657, XP055794764, DOI: 10.1093/ oxfordjournals.jbchem.a128721
"Fabrication of lithocholic acid amide derivatives with vitamin D activity", LECTURE ABSTRACT OF THE 139TH ANNUAL MEETING OF THE, 19 March 2019 (2019-03-19), Retrieved from the Internet
"Fabrication of lithocholic acid derivatives with diol groups in the side chains and vitamin D activity", LECTURE ABSTRACTS OF THE 37TH MEDICINAL CHEMISTRY SYMPOSIUM, 5 November 2019 (2019-11-05), pages 111
"Fabrication of lithocholic acid amide derivatives with vitamin D activity", LECTURE ABSTRACTS OF THE 37TH MEDICINAL CHEMISTRY SYMPOSIUM, 5 November 2019 (2019-11-05), pages 119
"Structure evolution of lithocholic acid derivatives with vitamin D activity", VITAMINS, vol. 93, no. 8, 25 August 2019 (2019-08-25), pages 370 - 371
ROMBUNNO, LECTURE ABSTRACT OF THE 140TH ANNUAL MEETING OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 31 March 2020 (2020-03-31)
"Fabrication of lithocholic acid side chain derivatives with high vitamin D activity", VITAMINS, vol. 94, no. 4, 25 April 2020 (2020-04-25), pages 287
ROMBUNNO: "Carborane-containing carboxylic acid derivative with vitamin D activity", LECTURE ABSTRACT OF THE 138TH ANNUAL MEETING OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 2018
"Development of novel Vitamin D Derivatives", CLINICAL CALCIUM, vol. 27, no. 11, 2017, pages 1579 - 1586
HOSHITA, NOBUHIKO, OKUDA, KYUICHIRO: "Partial Synthesis of Stero-bile Acids Related to Chenodeoxycholic Acid", JOURNAL OF BIOCHEMISTRY, vol. 62, no. 6, 1967, pages 655 - 657, XP055794764, DOI: 10.1093/ oxfordjournals.jbchem.a128721
Attorney, Agent or Firm:
SIKS & CO. (JP)
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