Title:
CTLA-4 SMALL MOLECULE DEGRADATION AGENT AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/194248
Kind Code:
A1
Abstract:
A CTLA-4 small molecule degradation agent and an application thereof. The CTLA-4 small molecule degradation agent comprises a compound having the structure represented by formula I or a pharmaceutically acceptable salt, an ester, a deuterated product, an isomer, a solvate, a prodrug, or an isotopic label thereof: ![]()
a new class of small molecule compounds having high degradation activity on CTLA-4. The compounds show a good degradation activity on CTLA-4 at the nanomolar (nM) level in in vitro studies.
Inventors:
MEI DESHENG (CN)
HE BAOKUN (CN)
LV SHIMING (CN)
SUN GAORUI (CN)
WANG KUI (CN)
XIAO CHENG (CN)
LIANG MIN (CN)
LING XIN (CN)
LIU SHUAISHUAI (CN)
HE BAOKUN (CN)
LV SHIMING (CN)
SUN GAORUI (CN)
WANG KUI (CN)
XIAO CHENG (CN)
LIANG MIN (CN)
LING XIN (CN)
LIU SHUAISHUAI (CN)
Application Number:
PCT/CN2022/081458
Publication Date:
September 22, 2022
Filing Date:
March 17, 2022
Export Citation:
Assignee:
SUZHOU GUOKUANG PHARMTECH CO LTD (CN)
International Classes:
C07D401/14; A61K31/506; A61P35/00; C07D239/42; C07D401/04; C07D471/04; C07D487/04; C07D498/04
Domestic Patent References:
| WO2021155320A1 | 2021-08-05 | |||
| WO2003062234A1 | 2003-07-31 | |||
| WO2009026319A1 | 2009-02-26 | |||
| WO2014128223A1 | 2014-08-28 |
Foreign References:
| CN101389622A | 2009-03-18 | |||
| CN102625799A | 2012-08-01 |
Other References:
DATABASE REGISTRY CAS; ANONYMOUS : "Quinoline, 3-[6-(1-piperidinyl)-4-pyrimidinyl]-(CA INDEX NAME) ", XP055968534, retrieved from STN
DATABASE Registry CAS; ANONYMOUS : "- 2-Pyrimidinamine, 4-(4-methyl-1-piperazinyl)-6-(6-quinolinyl)- (CA INDEX NAME)", XP055968539, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "8-Quinolinol, 6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-(CA INDEX NAME) ", XP055968543, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "Quinoline, 6-[6-(1-piperazinyl)-2-pyridinyl]-(CA INDEX NAME) ", XP055968547, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "5-Quinoxalinecarboxamide, 3-[6-(1-piperazinyl)-2-pyridinyl]-(CA INDEX NAME)", XP055968551, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "5-Quinoxalinecarboxamide, 3-[4-(1-piperazinyl)-2-pyridinyl]-(CA INDEX NAME)", XP055968552, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "-5-Quinoxalinecarboxamide, 3-[2-(1-piperazinyl)-4-pyridinyl]-(CA INDEX NAME)", XP055968555, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "5-Quinoxalinecarboxamide, 3-[2-(4-hexyl-1-piperazinyl)-4-pyridinyl]-(CA INDEX NAME) ", XP055968557, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "Quinoline, 6-[6-(3-piperidinyl)-2-pyridinyl]-(CA INDEX NAME) ", XP055968565, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "1-Piperidinecarboxylic acid, 3-[6-(6-quinolinyl)-2-pyridinyl]-, 1,1-dimethylethyl ester (CA INDEX NAME) ", XP055968567, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "-Quinoline, 3-[6-(hexahydro-1H-1,4-diazepin-1-yl)-4-pyrimidinyl]-(CA INDEX NAME) ", XP055968569, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "Quinoline, 3-(6-bromo-2-cyclopropyl-4-pyrimidinyl)-(CA INDEX NAME) ", XP055968571, retrieved from STN
THRIVENI K S, PADMASHALI B, SIDDESH M B, SANDEEP C: "Synthesis of Pyrimidine Incorporated Piperazine Derivatives and their Antimicrobial Activity", INDIAN JOURNAL OF PHARMACEUTICAL SCIENCES, 1 July 2014 (2014-07-01), pages 332 - 338, XP055968574, Retrieved from the Internet [retrieved on 20221006]
ALLEN, L. V. JR. ET AL.: "Remington: The Science and Practice of Pharmacy", vol. 2, 2012, PHARMACEUTICAL PRESS
DATABASE Registry CAS; ANONYMOUS : "- 2-Pyrimidinamine, 4-(4-methyl-1-piperazinyl)-6-(6-quinolinyl)- (CA INDEX NAME)", XP055968539, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "8-Quinolinol, 6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-(CA INDEX NAME) ", XP055968543, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "Quinoline, 6-[6-(1-piperazinyl)-2-pyridinyl]-(CA INDEX NAME) ", XP055968547, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "5-Quinoxalinecarboxamide, 3-[6-(1-piperazinyl)-2-pyridinyl]-(CA INDEX NAME)", XP055968551, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "5-Quinoxalinecarboxamide, 3-[4-(1-piperazinyl)-2-pyridinyl]-(CA INDEX NAME)", XP055968552, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "-5-Quinoxalinecarboxamide, 3-[2-(1-piperazinyl)-4-pyridinyl]-(CA INDEX NAME)", XP055968555, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "5-Quinoxalinecarboxamide, 3-[2-(4-hexyl-1-piperazinyl)-4-pyridinyl]-(CA INDEX NAME) ", XP055968557, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "Quinoline, 6-[6-(3-piperidinyl)-2-pyridinyl]-(CA INDEX NAME) ", XP055968565, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "1-Piperidinecarboxylic acid, 3-[6-(6-quinolinyl)-2-pyridinyl]-, 1,1-dimethylethyl ester (CA INDEX NAME) ", XP055968567, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "-Quinoline, 3-[6-(hexahydro-1H-1,4-diazepin-1-yl)-4-pyrimidinyl]-(CA INDEX NAME) ", XP055968569, retrieved from STN
DATABASE REGISTRY CAS; ANONYMOUS : "Quinoline, 3-(6-bromo-2-cyclopropyl-4-pyrimidinyl)-(CA INDEX NAME) ", XP055968571, retrieved from STN
THRIVENI K S, PADMASHALI B, SIDDESH M B, SANDEEP C: "Synthesis of Pyrimidine Incorporated Piperazine Derivatives and their Antimicrobial Activity", INDIAN JOURNAL OF PHARMACEUTICAL SCIENCES, 1 July 2014 (2014-07-01), pages 332 - 338, XP055968574, Retrieved from the Internet
ALLEN, L. V. JR. ET AL.: "Remington: The Science and Practice of Pharmacy", vol. 2, 2012, PHARMACEUTICAL PRESS
Attorney, Agent or Firm:
SUZHOU JINSHANG INTELLECTUAL PROPERTY LAW FIRM (GENERAL PARTNERSHIP) (CN)
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