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

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

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

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.

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

公开(公告)号：RU2120439C1

公开(公告)日：1998-10-20

申请号：RU93054506

申请日：1993-12-09

Applicant: BASF AG

Inventor： GERD SHTAJNER ,  LILIAN UNGER ,  BERTOL D BEL ,  GANS-JURGEN TESHENDORF

IPC: C07D209/52 ,  A61K31/40 ,  A61K31/403 ,  A61P25/00 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04

Abstract: 2.0] HEPTANE DERIVATIVES AND PHYSIOLOGICALLY TOLERABLE ACID SALTS THEREOF. FIELD: medicine. SUBSTANCE: present invention describes 3- azabicyclo [3.2.0] heptane derivatives wherein R is phenyl substituted optionally by one or two halogen atoms, trifluoromethyl, hydroxy, alkoxy, amino, cyano or nitro; or thienyl; R is H or phenyl; n is integer of 1 to 4; A is hydrogen or -C(R 3 )(R 4 )-C 6 H 4 (R 5 ),, NR 6 -CO-C 6 H 4 (R 5 ) or -CH=CH 2 , R 3 -H,OH or phenyl optionally substituted by fluorine, chlorine or bromine; R is H; or R and R together are oxygen; R is hydrogen, chlorine, fluorine or bromine, hydroxy, alkyl or methoxy; R is hydrogen or methyl or salts thereof. Said salts have neuroleplic activity . EFFECT: improved properties of the title compounds. 2 cl, 64 ex, 1 tbll