DERIVATIVES OF THIENO[2,3-D]PYRIMIDINE-2,4-(1H,3H)-DIANE, PHARMACEUTICAL COMPOSITION, METHOD FOR ITS PREPARING, METHOD FOR IMMUNOSUPPRESSION AND METHOD FOR TREATMENT OR REDUCING RISK OF RESPIRATORY WAY OBSTRUCTION Russian patent published in 2004 - IPC

Abstract RU 2225410 C2

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to new derivatives of then[2,3-d]- pyrimidine-2,4-(1H,3H)-done of the general formula (I) or their pharmaceutically acceptable salts eliciting immunosuppressive activity. Invention relates also to pharmaceutical composition, method for its preparing, method for immunosuppression and method for treatment or reducing risk of obstruction of respiratory ways. In compounds of the general formula (I) R represents -C(O)-Ar1, -C(R4)(R5)Ar1 or Ar2 wherein Ar1 represents naphthyl, quaintly, isoquinolyl or benzofuranyl; or Ar1 represents phenyl optionally substituted with one or some substituents taken among: C1-4-alkyl, C1-4-alkoxy-group, halogen atom, trifluoromethyl, amino-, nitro-, cyano-, trifluoromethoxy-, phenoxy-group, -CH2N(R6)2, -NHSO2CF3, C1-4-alkylsulfonylamino-group, -NHC(O)R6a, CO2R7 or -C(O)NR8R8a; R4 represents hydrogen atom; R5 represents hydrogen atom or OH; each R6 and R7 represents hydrogen atom or C1-4- alkyl; R6a represents hydrogen atom, C1-6-alkyl, aryl or aryl-C1-4-alkyl wherein alkyl group or aryl moiety in arylalkyl group represents phenyl or pyridyl being each of them can be substituted optionally with one or some substituents; R8 and R8a each represents independently hydrogen atom, C1-4-alkyl, phenyl or pyridyl; Ar2 represents acenaphthenyl, indanyl, iminodihydrobenzofuranyl or fluorenyl and each of them can be substituted optionally with one or some substituents; R1 and R2 represent independently C1-6-alkyl, C3-6-alkenyl, CH2C3-5-cycloalkyl or C3-6-cycloalkyl; R3 represents hydrogen atom, X-R9 or X-Ar3 wherein X represents S(O)n, C(O)NR10, C(O)O, NH(CO)NR10, NH(CO)O or SO2NR10; n = 0, 1 or 2; X, R9 and R10 are given in the invention claim; Ar3 represents phenyl, pyridyl or pyridine N-oxide and each of them can be substituted optionally with one or some substituents taken among: OH, NO2, NH2, NHSO2CF3, C1-4-alkoxy-group, bis-C1-4-alkanesulfonylamino-group, C1-4- alkylcarbonylamino-group or C1-4-alkoxycarbonylamino-group. EFFECT: improved preparing and treatment methods, valuable medicinal properties of compounds. 17 cl, 95 ex _

Similar patents RU2225410C2

Title Year Author Number
THIENOPYRIMIDINE DIONES AND THEIR USE IN MODULATION OF AUTOIMMUNE DISEASE 2004
  • Gajl Sajmon Dejvid
RU2331647C2
THIENOPYRIMIDNEDIONES, METHODS FOR THEIR PREPARING (VARIANTS) AND PHARMACEUTICAL COMPOSITION 2002
  • Rejnolds Rejchel Kh'Juluehn
  • Ingoll Ehtoni Khauard
  • Rehjsul Rakhsehjna Tehsnim
  • Gil Sajmon Dejvid
  • Kuper Martin Ehdvard
RU2294937C9
THIENOPYRIMIDINDIONS AND THEIR APPLICATION IN AUTOIMMUNE DISEASE MODULATION 2004
  • Gajl Sajmon Dejvid
  • Ingoll Ehntoni Khauard
RU2332420C2
THIENOPYRIMIDINE COMPOUNDS AND THEIR APPLICATION 2004
  • To Nobuo
  • Imada Takasi
  • Khitaka Takenori
  • Miva Kazukhiro
  • Kusaka Masami
  • Suzuki Nobukhiro
RU2331648C2
PYRAZOLOPYRIMIDONE OR PYRROLOTRIAZONE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL APPLICATIONS THEREOF 2014
  • Lyuj Khetszyun
  • Sun Pyaoyan
  • Guj Bin
  • Dun Tsin
RU2674977C2
PHARMACEUTICAL COMPOSITION, METHODS FOR ITS PREPARING AND APPLYING 2003
  • Ivashchenko A.V.
  • Kravchenko D.V.
  • Tkachenko S.E.
  • Okun' Il'Ja Matusovich
RU2248978C1
NOVEL SUBSTITUTED THIOPHENE PYRIMIDINONE DERIVATIVES AS 17β HYDROXYSTEROID DEHYDROGENASE INHIBITORS 2004
  • Khirvelja Lena
  • Khuzen Bettina
  • Kivinimi Ioganna
  • Koskimies Pasi
  • Lekhtovuori Pekka
  • Messinger Jozef
  • Pentikjainen Olli-Taneli
  • Pirkkala Lila
  • Sarenketo Pauli
  • Tole Genrikh-Khubert
  • Unkila Mikko
  • Van-Sten Bartolomeus Iokhannes
RU2409581C2
COMPOSITIONS CONTAINING BENZOPIPERAZINE AS BROMODOMAIN BET INHIBITORS 2014
  • Bair Kenneth W.
  • Herbertz Torsten
  • Kauffman Goss Stryker
  • Kayser-Bricker Katherine J.
  • Luke George P.
  • Martin Matthew W.
  • Millan David S.
  • Schiller Shawn E. R.
  • Talbot Adam C.
  • Tebbe Mark J.
RU2720237C2
BENZODIAZEPINE COMPOUND AND PHARMACEUTICAL COMPOSITION 2009
  • Osima Kunio
  • Osijama Takasi
  • Taira Siniti
  • Mendzo Jasukhiro
  • Jamabe Khokuto
  • Matsumura Suudzi
  • Ueda Masataka
  • Koga Jasuo
  • Tai Kuninori
  • Nakajama Sunao
  • Onogava Tosijuki
  • Tsudzimae Kendzi
RU2496775C2
NOVEL COMPOUNDS AND USE THEREOF IN THERAPY 2004
  • Khirvela Leena
  • Jokhansson Nina
  • Koskimies Pasi
  • Pentikajnen Olli Taneli
  • Nirenen Tommi
  • Salminen Tiina Annamarija
  • Jonson Mark Stuart
  • Lekhtovuori Pekka
RU2412190C2

RU 2 225 410 C2

Authors

Cheshir Dehvid

Kuk Ehndrju

Kuper Martin

Donal'D Dehvid

Ferber Mark

Perri Mehtt'Ju

Tourn Filip

Dates

2004-03-10Published

1998-05-18Filed