Title:
POLYHYDROXYPHTHALAZINONE COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/214736
Kind Code:
A1
Abstract:
Provided are a polyhydroxyphthalazinone compound, a preparation method therefor and the use thereof, wherein the general formula of the chemical structure of the polyhydroxyphthalazinone compound is as shown by formula (I). The polyhydroxyphthalazinone compound disclosed in the present invention has a good ER receptor agonistic effect, and is expected to be useful in developing a novel ER receptor agonist.
Inventors:
LIANG FAXIANG (CN)
DING YANLING (CN)
DING YANLING (CN)
Application Number:
PCT/CN2018/086244
Publication Date:
November 29, 2018
Filing Date:
May 10, 2018
Export Citation:
Assignee:
REJUVGEN PHARMACEUTICALS INC (CN)
International Classes:
A61K31/502; C07D237/32; A61P1/04; A61P13/08; A61P15/00; A61P19/02; A61P19/10; A61P25/16; A61P25/28; A61P27/02; A61P29/00; A61P35/00
Foreign References:
| CN107082764A | 2017-08-22 | |||
| JPH10139640A | 1998-05-26 | |||
| EP0475527A2 | 1992-03-18 | |||
| EP1953147A1 | 2008-08-06 | |||
| BE628255A |
Other References:
LIU, BIN ET AL.: "Access to phthalazinones via palladium-catalyzed three-component cycloamino-carbonylation of 2-formylaryl tosylates, hydrazines and CO", TETRAHEDRON, vol. 72, no. 50, 28 October 2016 (2016-10-28), pages 8282 - 8286, XP029810954
LAD, V. ET AL.: "Nano Ti02: a recyclable catalyst for one pot synthesis of 2-(substituted phenyl)phthalazin-1 (2H)-ones", JOURNAL OF CHEMICAL AND PHARMACEUTICAL RESEARCH, vol. 7, no. 4, 31 December 2015 (2015-12-31), pages 257 - 261, XP055556880
WANG, HUAMIN ET AL.: "Palladium-Catalyzed Phthalazinone Synthesis Using Paraformaldehyde as Carbon Source", ORG. LETT., vol. 16, no. 20, 29 September 2014 (2014-09-29), pages 5324 - 5327, XP055556883
SURESH, A.S. ET AL.: "Convenient method for the synthesis of phthalazinones via carbonylation of 2-bromobenzaldehyde using Co2(CO)8 as a CO source", TETRAHEDRON LETTERS, vol. 55, no. 24, 1 May 2014 (2014-05-01), pages 3482 - 3485, XP055556892
RAO, K.P. ET AL.: "Microwave assisted palladium-catalyzed synthesis of phthalazinones and pyridopyridazinones", TETRAHEDRON LETTERS, vol. 54, no. 28, 13 May 2013 (2013-05-13), pages 3694 - 3696, XP028561942
MENDOZA, R. ET AL.: "Cracking the molecular weight barrier: Fragment screening of an aminotransferase using an NMR-based functional assay", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 21, no. 18, 21 July 2011 (2011-07-21), pages 5248 - 5250, XP028267842
FINKELSTEIN, J. ET AL.: "2,8-Substituted 4-methyl-1 (2H)-phthalazinones", JOURNAL OF ORGANIC CHEMISTRY, vol. 11, no. 2, 31 March 1968 (1968-03-31), pages 398 - 399, XP055556900
BRODRICK, C.I. ET AL.: "A Reaction of Certain Diaxosulphonates derived from p -Naphthol- 1 -sulphonic Acid. PART XXV The Phthalaxine Reaction with Bases not containing a Nitro-group. Derivatives of 2’-Chlorobenxene-2- naphthol-l-diazosulphonate.", JOURNAL OF THE CHEMICAL SOCIETY, 1 January 1948 (1948-01-01), pages 1026 - 1029, XP055615124
ANONYMOUS: "STNext Registry", REGISTRY (RN 931044-64-3, 11 September 2009 (2009-09-11), XP009515919, Retrieved from the Internet
YEPURU, M. ET AL.: "Estrogen receptor-beta-selective ligands alleviate high-fat diet- and ovariectomy-induced obesity in mice", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 285, no. 41, 8 October 2010 (2010-10-08), pages 31292 - 31303, XP055031052
See also references of EP 3564215A4
LAD, V. ET AL.: "Nano Ti02: a recyclable catalyst for one pot synthesis of 2-(substituted phenyl)phthalazin-1 (2H)-ones", JOURNAL OF CHEMICAL AND PHARMACEUTICAL RESEARCH, vol. 7, no. 4, 31 December 2015 (2015-12-31), pages 257 - 261, XP055556880
WANG, HUAMIN ET AL.: "Palladium-Catalyzed Phthalazinone Synthesis Using Paraformaldehyde as Carbon Source", ORG. LETT., vol. 16, no. 20, 29 September 2014 (2014-09-29), pages 5324 - 5327, XP055556883
SURESH, A.S. ET AL.: "Convenient method for the synthesis of phthalazinones via carbonylation of 2-bromobenzaldehyde using Co2(CO)8 as a CO source", TETRAHEDRON LETTERS, vol. 55, no. 24, 1 May 2014 (2014-05-01), pages 3482 - 3485, XP055556892
RAO, K.P. ET AL.: "Microwave assisted palladium-catalyzed synthesis of phthalazinones and pyridopyridazinones", TETRAHEDRON LETTERS, vol. 54, no. 28, 13 May 2013 (2013-05-13), pages 3694 - 3696, XP028561942
MENDOZA, R. ET AL.: "Cracking the molecular weight barrier: Fragment screening of an aminotransferase using an NMR-based functional assay", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 21, no. 18, 21 July 2011 (2011-07-21), pages 5248 - 5250, XP028267842
FINKELSTEIN, J. ET AL.: "2,8-Substituted 4-methyl-1 (2H)-phthalazinones", JOURNAL OF ORGANIC CHEMISTRY, vol. 11, no. 2, 31 March 1968 (1968-03-31), pages 398 - 399, XP055556900
BRODRICK, C.I. ET AL.: "A Reaction of Certain Diaxosulphonates derived from p -Naphthol- 1 -sulphonic Acid. PART XXV The Phthalaxine Reaction with Bases not containing a Nitro-group. Derivatives of 2’-Chlorobenxene-2- naphthol-l-diazosulphonate.", JOURNAL OF THE CHEMICAL SOCIETY, 1 January 1948 (1948-01-01), pages 1026 - 1029, XP055615124
ANONYMOUS: "STNext Registry", REGISTRY (RN 931044-64-3, 11 September 2009 (2009-09-11), XP009515919, Retrieved from the Internet
YEPURU, M. ET AL.: "Estrogen receptor-beta-selective ligands alleviate high-fat diet- and ovariectomy-induced obesity in mice", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 285, no. 41, 8 October 2010 (2010-10-08), pages 31292 - 31303, XP055031052
See also references of EP 3564215A4
Attorney, Agent or Firm:
CHANGZHOU RIGHT NAVIGATION PATENT AGENCY CO., LTD. (CN)
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