NEW TETRAHYDROPYRIMIDINE CONNECTION OR ITS SALT Russian patent published in 2017 - IPC C07D471/04 A61K31/519 A61K31/553 A61P35/00 A61P5/28 A61P13/08 

Abstract RU 2636310 C1

FIELD: pharmacology.

SUBSTANCE: invention relates to a new tetrahydropyridopyrimidine compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The compounds possess an inhibitory activity against the androgen receptor (AR) and can be used to treat a tumour associated with activity (AR). In the general formula

,

X is a halogen atom or halogen-C1-3an alkyl group; R is a phenyl group which is substituted by R1 and can also be substituted by R2, or a 5- or 6-membered heteroaryl group which contains 1 to 3 heteroatoms selected from a nitrogen, oxygen or sulfur atom and which is substituted by R1 and can also be substituted by R2; R1 represents a hydrogen atom, a phenyl group, a hydroxy-C1-6alkyl group, hydroxy-C3-7cycloalkyl group,C1-6an alkoxy group which may be substituted by Ra, C3-7 a cycloalkylaminosulfonyl group, a (6-7) membered monocyclic heterocycloalkylsulfonyl group, with two nitrogen atoms or a nitrogen atom and an oxygen atom in the ring; halogen-C1-3alkoxycarbonylamino group, halogen-C1-3alkylcarbonylamino group, a (5-7)membered monocyclic heterocycloalkanecarbonyl group,containing a nitrogen atom in the ring, and substituted with hydroxy-C1-6alkyl group, or - (CH2)n-C(=O)-NHRf; R2 is a hydrogen atom, a halogen atom or a halogen-C1-3an alkyl group; Ra is C1-6alkylpyrazolyl group, a triazolyl group, a tetrazolyl group or a C1-6 alkylsulfonylpiperazinyl group; Rf is halogen-C1-3alkyl group, hydroxy-C1-6alkyl group, hydroxy-C3-7cycloalkyl group, hydroxy-C3-7cycloalkyl-C1-6alkyl group C1-6alkyl group, substituted by Rfa; Rfa is C a 1-6alkylpyrazolyl group, halogen-C1-3alkylthiazolyl group, an oxadiazolyl group or a halogen-C1-3alkyloxadiazolyl group; and n is an integer from 0 to 3.

EFFECT: obtaining of a new compound.

20 cl, 5 tbl, 63 ex

Similar patents RU2636310C1

Title Year Author Number
AZABICYCLOCOMPOUND AND ITS SALT 2010
  • Kitade Makoto
  • Okhkubo Suiti
  • Josimura Tikhoko
  • Jamasita Satosi
  • Osiumi Khiromi
  • Uno Takao
  • Kavai Juiti
RU2565078C2
NOVEL PYRIDOPYRIMIDINONE COMPOUNDS FOR MODULATION OF CATALYTIC ACTIVITY OF HISTONE LYSINE DEMETHYLASES (KDMS) 2015
  • Kim Myeong-Seop
  • Park Taesun
  • Yoon Taeyoung
  • Yang Seung Min
  • Kim Hae-Sun
  • Kim Jun Gyu
RU2684396C2
SULFONAMIDE DERIVATIVE AND MEDICINAL USE THEREOF 2013
  • Ueno Khirokadzu
  • Yamamoto Takasi
  • Takasita Ryuta
  • Jokoyama Rekhei
  • Sugiura Tosikhiko
  • Kageyama Sunsuke
  • Ando Ayatosi
  • Eda Khiroyuki
  • Eviryanti Agung
  • Miyadzava Tomoko
  • Kirikhara Aya
  • Tanabe Itsuya
  • Nakamura Tarou
  • Noguti Misato
  • Suto Manami
  • Sugiki Masayuki
  • Dokhi Midzuki
RU2607081C2
ANTIVIRAL REMEDIES FOR TREATMENT AND PREVENTION OF HIV INFECTION 2021
  • Kurkin Aleksandr Vitalevich
  • Manasova Ekaterina Vladimirovna
  • Kazyulkin Denis Nikolaevich
  • Ivanov Vladimir Nikolaevich
  • Shurygin Mikhail Gennadevich
RU2780103C1
NITROIMIDAZOLE DERIVATIVE AGAINST PULMONARY TUBERCULOSIS 2016
  • Luo, Wei
  • Ding, Charles Z.
  • Huang, Zhigang
  • Chen, Shuhui
RU2675622C1
ANTIVIRAL REMEDIES FOR TREATMENT AND PREVENTION OF HIV INFECTION 2020
  • Kurkin Aleksandr Vitalevich
  • Manasova Ekaterina Vladimirovna
  • Kazyulkin Denis Nikolaevich
  • Ivanov Vladimir Nikolaevich
  • Shurygin Mikhail Gennadevich
RU2780101C2
SUBSTITUTED 1,2-DIHYDRO-3H-PYRAZOLO[3,4-D]PYRIMIDIN-3-ONES 2019
  • Khuan, Piter, Tsinkhua
  • Banker, Kevin, Duejn
  • Boren, Brant, Klejton
  • Khegde, Saji, Gadzhanan
  • Lyu, Khuej
  • Unni, Aditya, Krishnan
  • Abrakham, Sanni
  • Khopkins, Chad, Deniel
  • Palival, Sunil
RU2812726C2
HETEROCYCLIC MAT2A INHIBITORS AND METHODS OF THEIR USE FOR CANCER TREATMENT 2019
  • Konteatis, Zenon, D.
  • Li, Mingzong
  • Reznik, Samuel, K.
  • Sui, Zhihua
RU2809987C2
PYRIDOXAZINONE DERIVATIVES AS TNAP INHIBITORS 2016
  • Shinozaki, Taeko
  • Soma, Kaori
  • Izumi, Masanori
  • Inui, Masaharu
  • Suzuki, Keisuke
  • Yamamoto, Yuko
  • Miyazaki, Shojiro
  • Pinkerton, Anthony
RU2715704C2
SUBSTITUTED PYRIDINE COMPOUND 2011
  • Nakamura Tsujosi
  • Namiki Khidenori
  • Terasaka Naoki
  • Sima Akiko
  • Khagikhara Masakhiko
  • Ivase Noriaki
  • Takata Katsunori
  • Kikuti Osamu
  • Tsuboike Kadzunari
  • Setoguti Khirojuki
  • Joneda Kendzi
  • Sunamoto Khidetosi
  • Ito Kodzi
RU2572606C2

RU 2 636 310 C1

Authors

Minamiguti, Kadzukhisa

Okadzima, Sigeo

Aoki, Siniti

Asai, Masanori

Asai, Takakhiro

Yamanaka, Khirojosi

Dokhi, Suguru

Dates

2017-11-22Published

2015-05-28Filed