COMPOUNDS FOR TREATING PD-L1 DISEASES Russian patent published in 2025 - IPC C07D207/06 C07D213/64 C07D217/04 C07D295/12 C07D401/12 C07C25/02 C07C217/58 C07C229/16 C07C309/14 A61K31/03 A61K31/132 A61K31/137 A61K31/513 A61P37/02 

Abstract RU 2838028 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I), where R1a, R1b, R1c and R1d each is independently selected from H, F, Cl, C1-3 alkyl, C1-3 haloalkyl and C1-3 alkoxy groups; X1 represents C1-3 alkylene, optionally substituted with one or two C1-2 alkyls; R2a and R2b each is independently selected from H, C1-8 alkyl, -X2-C(O)2Ra, -X2-ORa, where each X2 represents C1-6 alkylene; or R2a and R2b are combined to form 4–8-membered ring having one cycle vertex selected from N; or R1a and R2a are combined to form 5–7-membered ring having one or two cycle vertices selected from O and N; or R1b and R2b are combined to form 5–7-membered ring having one or two cycle vertices selected from O and N; where rings formed when combining R2a and R2b, R1a and R2a or R1b and R2b, contain 0 or 1 substituent independently selected from -X3-C(O)2Ra and -X3-ORa, where X3 is a bond or C1-6 alkylene; R3 selected from F, Cl, C1-3 alkyl, C1-3 alkoxy groups, C1-3 haloalkyl, C2-3 alkenyl and CN; n is 0; each of R4, R6, R7 and R8 is independently selected from H, halogen, C1-6 alkyl and -X4-ORa, where each X4 is a bond; R5 is selected from H, halogen, C1-6 alkyl, -Y2, -X5-ORa, -X5-NRaRb, -O-X5-Y2 and -AZ, where each X5 is a bond or C1-6 alkylene and each Y2 selected from C4-8 heterocyclyl containing one N heteroatom, C7-9 spiroheterocyclyl containing one N heteroatom, and 5–6 membered heteroaryl containing one N heteroatom, each of which is optionally further substituted with 1–4 substitutes independently selected from halogen, OH and C1-4 alkyl; where A is selected from a bond, -O, and -N(Ra)-; Z is selected from: i) monocyclic 6-member heteroaryl ring containing one N heteroatom; and ii) 6-membered non-aromatic heterocyclic ring containing one N heteroatom; and two of R4, R5 and R6 adjacent carbon atoms are optionally combined to form 6-membered non-aromatic heterocyclic ring having one or two ring vertices selected from O and -N (Rb) -; where said non-aromatic heterocyclic ring is optionally substituted with an oxo group and optionally 1 substituent Rc; and at least one of R4, R5, R6, R7 and R8 differs from H; every Ra is independently selected from H and C1-6 alkyl; every Rb is independently selected from H; and each Rc is independently selected from H, CN, -Y4, -X6-C(O)2Ra and -X6-NRaRb, where each X6 is a bond or C1-6 alkylene and each Y4 selected from C4-8 heterocyclyl containing one or two N heteroatoms. Invention also relates to a pharmaceutical composition containing a compound of formula (I), a method of treating a disease or disorder associated with PD-1, using a compound of formula (I), using the compound of formula (I) for treating a disease or disorder associated with PD-1, and compound 1.006 specified in the claim.

EFFECT: compounds having PD-1 inhibitory activity for treating PD-1 mediated diseases.

19 cl, 1 tbl, 25 ex

Similar patents RU2838028C2

Title Year Author Number
PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF 2020
  • Bogdan, Endryu
  • Khalvorsen, Dzheff T.
  • Farni, Elliot P.
  • Frost, Dzhennifer M.
  • Kim, Filip R.
  • Matulenko, Mark A.
  • O`Konnor, Mettyu
  • Shirudi, Reza
  • Vojt, Erik
  • Syun, Chzhaomin
  • Chzhan, Tsinvej
  • Baumgartner, Kristina
  • Ebbott, Dzhejson
  • Ikonomu, Kristos
  • Fosu, Stejsi
RU2833220C2
HETEROARYL-BIPHENYL AMINES FOR TREATING PD-L1 DISEASES 2020
  • Fan, Pingchen
  • Lange, Christopher W.
  • Lui, Rebecca M.
  • Mcmurtrie, Darren J.
  • Scamp, Ryan J.
  • Yang, Ju
  • Zeng, Yibin
  • Zhang, Penglie
RU2837843C1
TRIARYL COMPOUNDS FOR TREATING PD-L1 DISEASES 2020
  • Fan, Pingchen
  • Lange, Christopher
  • Mali, Venkat Reddy
  • Mcmurtrie, Darren, J.
  • Malathong, Viengkham
  • Punna, Sreenivas
  • Singh, Rajinder
  • Yang, Ju
  • Zeng, Yibin
  • Zhang, Penglie
RU2840345C2
HETEROCYCLIC DERIVATIVES AND USE THEREOF 2014
  • Park Chan Khee
  • Li Sang Khvi
  • Im Dzunkhvan
  • Li Soon Ok
  • Kim Khoe Moon
  • Moon Sung Khyun
  • Kim Seungkhi
  • Kim Dzongmin
  • Ko Kvang Seok
  • Choi Bu Yang
  • Kim Byungkho
RU2681849C2
HPK1 INHIBITORS AND USE THEREOF 2020
  • Zhong, Wenge
  • Zhu, Xiaotian
  • Feng, Song
  • Wu, Lei
  • Huang, Wei
  • Liu, Hao
  • Liu, Rongqiang
  • Wen, Kate Xin
  • Zhou, Hua
RU2839132C2
SUBSTITUTED CARBONUCLEOSIDES DERIVATIVES USED AS ANTICANCER AGENTS 2017
  • Kumpf, Robert Arnold
  • Mcalpine, Indrawan James
  • Mctigue, Michele Ann
  • Patman, Ryan
  • Rui, Eugene Yuanjin
  • Tatlock, John Howard
  • Tran-Dube, Michelle Bich
  • Wythes, Martin James
RU2712944C1
BICYCLIC COMPOUNDS AS PD1/PD-L1 INTERACTION/ACTIVATION INHIBITORS 2019
  • Venkateshappa, Chandregowda
  • D A, Jeyaraj
  • Pendyala, Muralidhar
  • Sivanandhan, Dhanalakshmi
  • Rajagopal, Sridharan
RU2777980C2
MODULATORS OF ATP-BINDING TRANSPORTERS 2010
  • Shet Urvi
  • Fehnning Lev T. D.
  • Numa Mekhdi
  • Binch Khehjli
  • Kharli Dennis Dzhejms
  • Chzhou Tszinlan'
  • Adida Rua Sara S.
  • Khejzlvud Anna R.
  • Silina Alina
  • Vairagoundar Radzhendran
  • Van Gur Frederik F.
  • Grotenkhejs Peter Diderik Jan
  • Botfild Martin K.
RU2552353C2
PROTEIN-TYROSINPHOSPHATASE INHIBITORS AND METHODS OF THEIR USE 2019
  • Farni, Elliot
  • Shiroodi, Rookhollakh, Kazem
  • Syun, Chzhaomin
  • Chzhan, Tsinvej
  • O`Konnor, Mettyu
  • Khalvorsen, Dzheff
  • Chzhao, Khunyuj
  • Baumgartner, Kristina
  • Frost, Dzhennifer, M.
  • Kim, Fil
  • Ebbot, Dzhejson, R.
  • Bogdan, Endryu
  • Ikonomu, Kristos
  • Van, Syuetsin
RU2799446C2
ARYL-OR HETEROARYL-SUBSTITUTED BENZENE COMPOUNDS 2012
  • Kuntts Kevin Uejn
  • Chesuort Richard
  • Dunkan Kennet Uillyam
  • Kajlkhak Khajke
  • Varkholik Natali
  • Klaus Kristin
  • Seki Masasi
  • Sirotori Syudzi
  • Kavano Satosi
  • Vigl Timoti Dzhejms Nelson
RU2632193C2

RU 2 838 028 C2

Authors

Malathong, Viengkham

Fan, Pingchen

Lange, Christopher

Mali, Venkat Reddy

Mcmurtrie, Darren J.

Punna, Sreenivas

Roth, Howard S.

Singh, Rajinder

Yang, Ju

Zhang, Penglie

Dates

2025-04-08Published

2020-06-19Filed