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公开(公告)号:RU2136678C1
公开(公告)日:1999-09-10
申请号:RU96114993
申请日:1994-11-26
Applicant: BASF AG
Inventor: GERD SHTAJNER , RAJNER MUNSHAUER , LILIANE UNGER , KHANS-JURGEN TESHENDORF , TOMAS KHEGER
IPC: C07D401/04 , A61K31/40 , A61K31/403 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/505 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/18 , A61P25/28 , A61P43/00 , C07D209/02 , C07D209/46 , C07D209/52 , C07D209/90 , C07D209/96 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/06
Abstract: FIELD: biologically-active compounds. SUBSTANCE: new N- substituted 3-azabicyclo[32.0] heptane derivatives with formula I (presented in description) are provided, where R is phenyl or thienyl optionally monosubstituted by nitro, amino, mono- or dimethylamino group; A is group of formula II wherein R is hydrogen, R hydrogen or R and R together form oxygen atom; R optionally fluoro- or chloro-substituted thienyl or naphthyl; R hydrogen or methyl; R phenyl disubstituted by fluorine or fluorine, monosubstituted by amino, C 1 -C 4 -alkylamino, or di-C 1 -C 4 -dialkylamino, or thienyl, naphthyl, benzofuryl, benzothienyl, indolyl, N-methylindolyl, N-methylindenyl, or C 3 -C 6 - cycloalkyl each optionally substituted by fluorine or chlorine atoms; R hydrogen, fluorine, chlorine, C 1 -C 4 -alkyl, or amino group; R hydrogen or methyl; R hydrogen or methyl, or R and R together with annular carbon atom form spiro-cyclopropane ring; R phenyl, benzyl, or cyano group; and n=1,2,3 or 4; and their salts with physiologically tolerable acids. Compounds I function as D 4 dopamine receptor antagonists and can be utilized as neuroleptics and brain-protection drugs. EFFECT: extended choice of neuroleptics. 2 cl, 56 ex
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公开(公告)号:RU2163604C2
公开(公告)日:2001-02-27
申请号:RU97103198
申请日:1995-07-21
Applicant: BASF AG
Inventor: GERD SHTAJNER , RAJNER MUNSHAUER , TOMAS KHEGER , LILIANE UNGER , KHANS-JURGEN TESHENDORF
IPC: C07D401/06 , A61K31/40 , A61K31/415 , A61K31/47 , A61K31/505 , A61P25/18 , A61P43/00 , C07D403/06 , C07D471/04 , C07D513/04
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公开(公告)号:RU2135503C1
公开(公告)日:1999-08-27
申请号:RU95105435
申请日:1993-06-08
Applicant: BASF AG
Inventor: GERD SHTAJNER , LILIANE UNGER , BERTOL D BEL , KHANS-JURGEN TESHENDORF , RAJNER MUNSHAUER
IPC: A61K20060101 , A61K31/33 , A61K31/395 , A61K31/40 , A61K31/4045 , A61K31/4184 , C07D513/04 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/54 , A61K31/542 , A61P25/00 , A61P25/20 , A61P25/22 , A61P25/24 , A61P43/00 , C07D20060101 , C07D207/00 , C07D209/02 , C07D209/52 , C07D221/00 , C07D239/00 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/00 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
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公开(公告)号:RU2160254C2
公开(公告)日:2000-12-10
申请号:RU97103533
申请日:1995-07-22
Applicant: BASF AG
Inventor: GERD SHTAJNER , RAJNER MUNSHAUER , TOMAS KHEGER , LILIANE UNGER , KHANS-JURGEN TESHENDORF
IPC: A61K31/40 , A61K31/403 , A61P25/18 , A61P43/00 , C07D409/12 , C07D209/44 , C07D209/52 , C07D209/90 , C07D209/92 , C07D403/06
Abstract: chemical industry. SUBSTANCE: described are new N-substituted 3-azabicyclo (3.2.0) heptane derivatives of formula I: wherein R is naphthyl or phenanthryl group which is mono-or disubstituted by halogen atoms; A is residue of formula or naphthyl group which are substituted by halogen, or salts thereof with physiologically acceptable acids. Said compounds are useful as neuroleptic agents. EFFECT: improved properties of the title compounds. 2 cl, 1 ex, 1 tbl
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公开(公告)号:RU2167869C2
公开(公告)日:2001-05-27
申请号:RU97102158
申请日:1995-07-14
Applicant: BASF AG
Inventor: BEATE KHELLENDAL , ANNEGRET LANSKI , RAJNER MUNSHAUER , ZIGFRID BIALOJAN , LILIANE UNGER , KHANS-JURGEN TESHENDORF , KARSTEN VIKE , KARLA DRESHER
IPC: C07D249/08 , A61K31/41 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/505 , A61K31/53 , A61P1/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D249/12 , C07D249/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
Abstract: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel compounds of triazole of the general formula (I) where A means linear or branched C1-C18-alkylene group that can include at least one group that is taken among O, S, CONH, COO, C3-C6-cycloalkylene or double or triple bond; B means radical of the formula (a) , (b) or (c) ; R1 means H, NH2, C3-C6-cycloalkyl or C1-C8-alkyl that can be free or substituted with O-C1-C8-alkyl; R2 means H, OH, C1-C8-alkyl, C3-6-cycloalkyl, CF3, CN, WR3R4,SR3 or CO2R3 where R3 means H or C1-C8-alkyl and R4 means H, C1-C8-alkyl or COR3 where R34 means C1-C8-alkyl; Ar means naphthyl, phenyl with 1-2 substituents taken among C1-C8-alkyl, CF3,CHF2,NO2,SR3,SO2R3 where R3 means C1-C8-alkyl and also pyridyl, pyrimidyl or triazinyl that have from 1 to 3 substituents taken among C1-C8-alkyl, C2-C6-alkenyl, C2-C6/ -alkynyl, halogen atom, CN, CF3,OR4 where R4 means hydrogen atom or C1-C8-alkyl, CO2R3 where R3 means C1-C8-alkyl, phenyl that can be substituted with halogen atom, alkoxy- or phenoxy-group, C3-C6-cycloalkyl that can be condensed, phenylalkylamine or 5-membered aromatic heterocycle with 1-2 nitrogen atoms that can be condensed with benzene ring. Compounds show high affinity to dophamine-D3-[sic] -receptors and therefore they can be used for treatment of patients with disorders giving responses for dophamine-D3-ligands. Invention describes also pharmaceutical composition based on compounds of the formula (I). EFFECT: new compounds, valuable pharmacological properties. 11 cl, 9 tbl
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6.
公开(公告)号:RU95105435A
公开(公告)日:1996-11-20
申请号:RU95105435
申请日:1993-06-08
Applicant: BASF AG
Inventor: GERD SHTAJNER , LILIANE UNGER , BERTOL D BEL , KHANS-JURGEN TESHENDORF , RAJNER MUNSHAUER
IPC: C07D513/04 , A61K20060101 , A61K31/33 , A61K31/395 , A61K31/40 , A61K31/4045 , A61K31/4184 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/54 , A61K31/542 , A61P25/00 , A61P25/20 , A61P25/22 , A61P25/24 , A61P43/00 , C07D20060101 , C07D207/00 , C07D209/02 , C07D209/52 , C07D221/00 , C07D239/00 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/00 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
Abstract: Описываютсясоединенияобщейформулы, приведеннойв описании, атакжеихполучение. Новыесоединенияпригодныдляборьбыс болезнями.
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