INGENOL-3-ACYLATES III AND INGENOL-3-CARBAMATES Russian patent published in 2016 - IPC C07C271/34 C07D261/18 C07D277/32 C07D309/08 C07D333/38 C07D401/04 C07D295/21 A61K31/215 A61K31/216 A61K31/27 A61K31/381 A61K31/4192 A61K31/42 A61K31/426 A61P35/00 

Abstract RU 2572549 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound of general structural formula which can be used for prevention, treatment, relieving course or prevention of physiological disorders or diseases, associated with hyperplasia or neoplasia. In formula (I) R stands for 5-10-membered mono- or bicyclic heteroaryl, containing 1-3 heteroatoms, selected from O, N and S, which can be optionally substituted with one or more substituents, independently selected from R7, or R stands for 5-10-membered heterocycloalkyl, containing 1-2 heteroatoms, selected from O, N and S, or 5-10-membered heterocycloalkenyl, containing 1-2 heteroatoms, selected from O, N and S, where said 5-10-membered heterocycloalkyl or 5-10-membered heterocycloalkenyl are optionally substituted with one or more substituents, independently selected from R8; or R stands for X; R7 represents halogen; or R7 represents (C1-C4) alkyl, (C2-C4) alkenyl, (C3) cycloalkyl, 6-membered heterocycloalkyl, containing 1 heteroatom, selected from N, C6-aryl, C6-aryl (C1-C4) alkyl, 6-membered heterocycloalkyl (C1-C4) alkyl, containing 1 heteroatom, selected from O, or (C3) cycloalkyl (C1-C4) alkyl, where said (C1-C4) alkyl or C6-aryl are optionally substituted with one or more substituents, independently selected from R9; or R7 represents -ORa; Ra represents (C1-C4) alkyl; Rc represents (C1-C4) alkyl; X represents -NR11R12, Rf represents (C1-C4) alkyl. Values of radicals R8-R13, Rd are given in the invention formula.

EFFECT: invention relates to pharmaceutical composition, containing said compound, and to method of prevention, treatment, relief of course or prophylaxis of physiological disorders or diseases, associated with hyperplasia or neoplasia, responding to stimulation of neutrophil oxidative burst, stimulation of IL-8 release from keratinocytes and to necrosis induction.

36 cl, 2 tbl, 753 ex

Similar patents RU2572549C2

Title Year Author Number
INGENOL-3-ACYLATES I 2011
  • Grueh-Serensen Gunnar
  • Ljan Sifu
  • Kherberg Tomas
RU2575349C2
3-ACYLINGENOLES II 2011
  • Grueh-Serensen Gunnar
  • Ljan Sifu
  • Khegberg Tomas
  • Monsson Kristoffer
  • Vedse Per
RU2575350C2
METHOD OF PRODUCING INGENOL-3-ANGELATE 2011
  • Khegberg Tomas
  • Grue-Serensen Gunnar
  • Lyan Sifu
  • Khorneman Anne Mariya
  • Petersen Anders Klarskou
RU2586975C2
CONDENSED TRICYCLIC DERIVATIVES FOR TREATING PSYCHOTIC DISORDERS 2005
  • Bentli Dzhonatan
  • Bergauehr Markus
  • Bertani Barbara
  • B'Jadzhetti Matteo
  • Borriello Manuehla
  • Bromidzh Stiven Mark
  • Dzhanotti Massimo
  • Granchi Ehnrika
  • Lesli Kolin Filip
  • Paskarello Alessandra
  • Tsukkelli Valerija
RU2409582C2
QUINOLINE AND QUINAZOLINE DERIVATIVES WITH AFFINITY TO 5HT-RECEPTORS 2004
  • Bergauehr Markus
  • Bertani Barbara
  • B'Jadzhetti Matteo
  • Bromidzh Stiven Mark
  • Fal'Ki Alessandro
  • Lesli Kolin Filip
  • Merlo Dzhankarlo
  • Pitstsi Dominika Antonia
  • Rinaldi Marilisa
  • Stasi Luidzhi P'Ero
  • Tibasko Dzhessika
  • Vong Antonio Kuok Keong
  • Uord Sajmon Ehdvard
RU2402533C2
1,2,4-TRIAZOLE DERIVATIVES AS SIGMA RECEPTOR INHBITORS 2007
  • Zhazherovik Nadin
  • Kumela-Montanches Khose Marija
  • Gojja-Lasa Marija Pilar
  • Dordal Suehras Alberto
  • Kuberes-Altisent Marija Rosa
RU2451015C2
DERIVATIVES OF 2-SUBSTITUTED PHENYL-5,7-DIHYDROCARBYL-3,7-DIHYDROPYRROLO[2,3-d]PYRIMIDIN-4-ONES, THEIR PREPARING AND PHARMACEUTICAL USING 2004
  • Van Junfehn
  • Chzhao Kehtszjun'
RU2323220C2
ORALLY BIOAVAILABLE PRODRUGS OF (+)-3-HYDROXYMORPHINAN FOR PREVENTING OR TREATING PARKINSON'S DISEASE 2008
  • Li Dzinkhva
  • Kim Dzeongmin
  • Dzung Miung Ehun
  • Kim Dzong Jup
  • Song Kvang-Seop
  • Son Ehun Dzung
  • Li Suk Kho
  • Khan Kho Kiun
  • Kim Min Dzu
  • Li Minvoo
RU2430089C2
PESTICIDE COMPOSITIONS 2010
  • Krauz Gari
  • Sparks Tomas
  • Maklaud Kasandra
  • Braun Annett
  • Siddall Tomas
RU2534529C2
SUBSTITUTED DIHYDRO-3-HALOGEN-1H-PYRAZOL-5-CARBOXYLATES, THEIR PREPARING AND USING 2002
  • Frojdenberger Dzhon Gerbert
  • Lehm Dzhordzh Filip
  • Selbi Tomas Pol
  • Stivenson Tomas Martin
RU2317983C2

RU 2 572 549 C2

Authors

Grueh-Serensen Gunnar

Ljan Sifu

Khegbert Tomas

Monsson Kristoffer

Vedse Per

Vifian Tomas

Dates

2016-01-20Published

2011-12-22Filed