SULFOXIMIN-SUBSTITUTED PYRIMIDINES AS CDK AND/OR VEGF INHIBITORS, THEIR OBTAINING AND APPLICATION AS MEDICATIONS Russian patent published in 2011 - IPC C07D239/48 C07D239/47 C07C381/10 C07C313/02 A61K31/505 A61P35/00 A61P17/06 A61P37/00 

Abstract RU 2410378 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel pyrimidine derivatives of general formula I, as well as to their diastereoisomers, enentiomers and/or pharmaceutically acceptable salts, which possess inhibiting action with respect to cyclin-dependent kinases and/or tyrosinekinases of VEGF receptor. In compound of general formula (I) Q stands for group where D, E, G, L, M and T in each case represent carbon, R1 represents hydrogen, halogen or CF3, R2 represents C1-C10-alkyl, which can optionally be disrupted with one group-C(O), C2-C10-alkinyl, C3-C10-cycloalkyl or phenyl, which is optionally substituted in one or more places in similar or different way by hydroxyl, halogen, C1-C6-alkoxy, C1-C6-alkyl, C3-C10-cycloalkyl, C1-C6-alkoxy-C1-C6-alkyl, C1-C6-alkoxy-C1-C6-alkoxy-C1-C6-alkyl or -COR8, X represents oxygen, sulphur or group -NH-, R3 represents hydroxy, halogen, CF3 or C1-C6-alkoxy, m represents 0-4, R4 represents hydrogen or group -COR8, NO2 or -SO2R7, or represents C1-C10-alkyl or C3-C10-cycloalkyl, R5 represents C1-C10-alkyl, which can be optionally substituted in one or more places, in similar or different way, by hydroxyl or C3-C10-cycloalkyl, or C3-C10-cycloalkyl, R7 represents C1-C10-alkyl, which is optionally substituted by group trimethylsilanyl (TMS), R8 represents C1-C6-alkyl, C1-C6-alkoxy. Invention also relates to intermediate compounds.

EFFECT: compounds can be applied for obtaining medication intended for treatment of cancer, selected from Kaposhi's sarcoma, Khodgkin's disease, leukemia or solid tumour, such as carcinoma of mammalian gland, kung, large intestine or prostate gland, autoimmune disease, such as psoriasis, and/or proliferative diseases, such as hemangioma or angiofibroma.

21 cl, 3 tbl, 5 ex

Similar patents RU2410378C2

Title Year Author Number
OBTAINING DIHYDROTHIENO[3,2-d]PYRIMIDINES AND INTERMEDIATE PRODUCTS, APPLIED FOR THEIR SYNTHESIS 2008
  • Rokhelio Frutos
  • Dkhilipkumar Krishnamerti
  • Dzhejson Alan Malder
  • Sonija Rodriges
  • Kris Kh'Ju Senanajake
  • Tomas G. Tampoun
RU2528340C2
DEUTERATED BENZYL BENZENE DERIVATES AND METHODS FOR USE 2009
  • Sid Brajan
  • Lv Bin'Khua
  • Roberzh Zhak J
  • Chehn' Juan'Vehj
  • Pehn Kun'
  • Dun Tszjatszja
  • Sjuj Bajkhua
  • Du Tszijan'
  • Chzhan Lili
  • Tan Sin'Sin
  • Sjuj Geh
  • Fehn Jan'
  • Sjuj Min'
RU2509773C2
PRODUCT COMPRISING AT LEAST ONE SUBSTANCE INHIBITING ACTIVITY OF NO-SYNTHASE IN COMBINATION WITH AT LEAST ONE SUBSTANCE INHIBITING ACTIVITY OF PHOSPHOLIPASE A 2000
  • Oge Mishel'
  • Shabrie De Lasson'Er P'Er-Eht'Enn
RU2256465C2
SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES AS Rho-KINASE INHIBITORS 2007
  • Plettenburg Oliver
  • Khofmajster Armin
  • Brendel' Joakhim
  • Len Mattias
RU2455302C2
CYCLOALKYLAMINE-SUBSTITUTED ISOQUINOLONE DERIVATIVES 2007
  • Plettenburg Oliver
  • Khofmajster Armin
  • Lorents Katrin
  • Brendel' Joakhim
  • Len Mattias
  • Veston Dzhon
RU2457203C2
CYCLOHEXYLAMINIZOQUINOLONE AS Rho-KINASE INHIBITORS 2006
  • Plettenburg Oliver
  • Khofmajster Armin
  • Kaderajt Diter
  • Brendel' Joakhim
  • Len Mattias
RU2440988C2
NOVEL DERIVATIVES OF IMIDAZOLIDINE, THEIR PREPARING AND USING AS VLA-4 ANTAGONIST 2002
  • Vener Fol'Kmar
  • Flor Shtefani
  • Blum Khorst
  • Rjutten Khartmut
  • Shtil'Ts Khans Ul'Rikh
RU2318815C2
PIPERADINYL-SUBSTITUTED ISOQUINOLONE DERIVATIVES AS Rho-KINASE INHIBITORS 2006
  • Plettenburg Oliver
  • Khofmajster Armin
  • Kaderajt Diter
  • Brendel' Joakhim
  • Len Mattias
RU2414467C2
TRIAZOLE COMPOUNDS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF 1995
  • Beate Khellendal'
  • Annegret Lanski
  • Rajner Munshauer
  • Zigfrid Bialojan
  • Liliane Unger
  • Khans-Jurgen Teshendorf
  • Karsten Vike
  • Karla Dresher
RU2167869C2
MEK INHIBITORS AND THEIR THERAPEUTIC USE 2021
  • Kholl, Brett Mettyu
  • Dekorte, Bart Liven
  • King, Piter Dzhon
  • Linders, Ruben
  • Vegert, Anita
  • Fouler, Kevin
  • Kolitts, Sara
  • Dudman, Robin
  • Polakker, Yarno
  • Folmer, Rutger Khenk Adrian
RU2812929C1

RU 2 410 378 C2

Authors

Ljukking Ul'Rikh

Krjuger Martin

Jautelat Rol'F

Zimajster Gerkhard

Dates

2011-01-27Published

2004-10-12Filed