公开(公告)号：HU0104007A2

公开(公告)日：2002-05-29

申请号：HU0104007

申请日：1999-08-07

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  HERGENROEDER STEFAN ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/22 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D251/52 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04

Abstract: The invention relates to new carboxylic acid derivatives of the formula (I), where the substituents have the meaning given in the description, their production and their use as endothelin-receptor antagonists.

公开(公告)号：SK9862001A3

公开(公告)日：2002-04-04

申请号：SK9862001

申请日：2000-01-12

Applicant: BASF AG

Inventor： STARCK DOROTHEA ,  TREIBER HANS-JORG ,  UNGER LILIANE ,  NEUMANN-SCHULTZ BARBARA ,  BLUMBACH KAI ,  SCHOBEL DIETMAR

IPC: A61K31/41 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/436 ,  A61K31/4439 ,  C07D249/14 ,  A61K31/4725 ,  A61K31/473 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/55 ,  A61P3/04 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P15/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P25/34 ,  A61P25/36 ,  A61P43/00 ,  C07D249/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D491/04 ,  C07D491/052 ,  A61P25/24 ,  C07D413/12

Abstract: Triazole compounds of the following formulawhere R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3 receptor and can therefore be used for treating diseases which respond to the influence of dopamine D3 ligands.

公开(公告)号：PL182810B1

公开(公告)日：2002-03-29

申请号：PL31845995

申请日：1995-07-22

Applicant: BASF AG

Inventor： STEINER GERD ,  MUNSCHAUER RAINER ,  HOEGER THOMAS ,  UNGER LILIANE ,  TESCHENDORF HANS-JUERGEN

IPC: A61K31/40 ,  A61K31/403 ,  A61P25/18 ,  A61P43/00 ,  C07D209/44 ,  C07D409/12 ,  C07D209/52 ,  C07D209/90 ,  C07D209/92 ,  C07D403/06 ,  A61P25/00

Abstract: PCT No. PCT/EP95/02912 Sec. 371 Date Feb. 3, 1997 Sec. 102(e) Date Feb. 3, 1997 PCT Filed Jul. 22, 1995 PCT Pub. No. WO96/04245 PCT Pub. Date Feb. 15, 1996A compound of the formula in which A, R1 and n have the meanings stated in the description are described. The novel compounds are suitable for controlling diseases.

公开(公告)号：UA44721C2

公开(公告)日：2002-03-15

申请号：UA96072631

申请日：1994-11-26

Applicant: BASF AG

Inventor： STEINER GERD ,  MUNSCHAUER RAINER ,  UNGER LILIANE ,  TESCHENDORF HANS-JUERGEN

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: Описаніновіпохідні N-заміщеного 3-азабіцикло [3.2.0] гептануформули I, де R1-фенілаботієніл, незаміщеіабомонозаміщенігалогеном, нітрогрупою, аміногрупою, монометиламіногрупою, диметиламіногрупою: А - групиформул II, де R2 - водень, R3 –водень, або R2 і R3 разомпозначаютькисень, R4 - тієнілабонафтил, незаміщеіабозаміщеніфторомчихлором, R5 - воденьабометил, R6 - феніл, дизаміщенийфтором, хлором, монозаміщенийаміногрупою, алкіламіногрупоюз 1-4 атомамивуглецю, діалкіламіногрупоюз 1-4 атомамивуглецюв кожнійалкільнійчастині, абонезаміщеніабозаміщеніфтором, хлором, нітрогрупоютієніл, нафтил, бензофурил, бензотієніл, індоліл, N-метиліндолілабоінденіл, циклоалкілз 3-6 атомамивуглецю, R7 - водень, фтор, хлор, алкілз 1-4 атомамивуглецю, аміно, R8 - водень, метил, R9 - водень, метил, або R8 і R9 разомз кільцевиматомомвуглецюявляютьсобоюспіроциклопропановекільце, R10 - фенілабобензил, ціаногрупа, n=1, 2, 3, 4, іїхнісоліз кислотами, щоє фізіологічностерпними. Похідні N-заміщеного 3-азабіцикло [3.2.0] гептануформули I, якіявляютьсобоюантагоністирецептора D4 допаміну. Їхможназастосовуватиякнейролептичнізасобиі засобидлязахистумозку.

公开(公告)号：ZA200101975B

公开(公告)日：2002-03-11

申请号：ZA200101975

申请日：2001-03-09

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/22 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D251/52 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04 ,  C07D ,  A61K

Abstract: The invention relates to new carboxylic acid derivatives of the formula (I), where the substituents have the meaning given in the description, their production and their use as endothelin-receptor antagonists.

公开(公告)号：NZ502319A

公开(公告)日：2002-03-01

申请号：NZ50231998

申请日：1998-06-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENRODER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/16 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61P7/02 ,  A61P9/02 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  A61P13/12 ,  A61P25/06 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07C247/12 ,  C07D213/68 ,  C07D237/14 ,  C07D237/16 ,  C07D239/34 ,  C07D239/52 ,  C07D239/56 ,  C07D239/60 ,  C07D239/70 ,  C07D239/80 ,  C07D239/95 ,  C07D241/18 ,  C07D251/22 ,  C07D251/34 ,  C07D251/52 ,  C07D253/06 ,  C07D403/12 ,  C07D491/048 ,  C07C235/12 ,  C07C233/63 ,  C07C229/22 ,  C07C233/47 ,  C07C235/34

Abstract: An b-amino or b-azido carboxylic acid derivative has the formula (I) wherein: R1 is tetrazole or -C(=O)-R; R is OR4, -O-(CH2)p-S(O)k-R5, a 5 membered heteroaromatic system linked via a nitrogen atom, -NH-SO2-R5; A is NR7R8 or azido; W and Z are independently nitrogen or methine provided that Q is nitrogen if W and Z are methine; X is nitrogen or CR9; Y is nitrogen or CR10; Q is nitrogen or CR11 provided that if X is CR9 and Y is CR10 if Q is nitrogen; R2 and R3 are independently optionally substituted phenyl or naphthyl or phenyl or naphthyl is linked together in ortho position by a direct linkage, methylene, ethylene or ethenylene, oxygen, sulphur, SO2, NH or N-alkyl; R4 is H, alkali metal cation, alkaline earth metal cation, or a physiologically tolerated organic ammonium ion, optionally substituted cycloalkyl, alkyl or -CH2-phenyl. k is 0 to 2 and p is 1 to 4; R5 is alkyl, cycloalkyl, alkenyl, alkynyl or optionally substituted phenyl and R7 to R11 are defined in the specification. A pharmaceutical composition thereof is useful as an endothelin receptor antagonist. A compound of formula (II) A-C(R2)(R3)-CH(R1)-OH wherein A and R1 to R3 are as defined above s useful as a starting material to prepare the compounds of formula (I).

公开(公告)号：HU0100957A2

公开(公告)日：2002-02-28

申请号：HU0100957

申请日：1999-02-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  HERGENROEDER STEFAN ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RASCHACK MANFRED ,  RIECHERS HARTMUT ,  UNGER LILIANE

IPC: A61K31/505 ,  A61K31/506 ,  A61P5/14 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/46 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the following meanings; R = tetrazole or a group (1); R = a radical OR (2), (3), a 5-membe red heteroaromatic bonded by a nitrogen atom such a pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R , R = hydrogen, hydroxy, NH2, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, C1-C4-halogen alkyl, C1-C4-alkoxy, C1-C4-halogen alkoxy or C1-C4-alkythio; X = halogen, C1-C4-halogen alkyl, hydroxy; R and R = phenyl or naphthyl, C3-C7-cycloalkyl, phenyl or naphthyl which are bonded in ortho position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulfur atom or an SO2-NH or an N-alkyl group or a 5-membered or 6-membered heteroaromatic; R = hydrogen, phenyl or naphthyl, a five or six-membered heteroaromatic, C1-C8-alkyl, C3-C6-alkenyl, C3-C6-alkinyl or C3-C8-cycloalkyl, whereby said radicals can be substituted once or many times, with the proviso that R can only stand for hydrogen if Z does not represent a single bond; Z = sulfur, oxygen or a single bond, in addition to the physiologically compatible salts and the enantiomeric-pure and diastereomeric-pure forms. The novel compounds are suitable for combating diseases, especially as endothelin antagonists.

公开(公告)号：BG105689A

公开(公告)日：2002-02-28

申请号：BG10568901

申请日：2001-07-10

Applicant: BASF AG

Inventor： STEINER GERD ,  SCHNELLHAAS KURT ,  LUBISCH WILFRIED ,  HOLZENKAMP UTA ,  STARCK DOROTHEA ,  KNOPP MONIKA ,  SZABO LASZLO ,  EMLING FRANZ ,  GARCIA-LADONA FRANCISCO J ,  HOFMANN HANS-PETER ,  UNGER LILIANE

IPC: C07D495/04 ,  A61K31/505 ,  A61K31/519 ,  A61P9/10 ,  C07D495/14 ,  A61K31/495 ,  A61K31/55

Abstract: The invention relates to the utilization of pyrimidine derivatives of formula wherein the substituents have the meaning cited in the description, and to the utilization of the physiologically compatible salts thereof for producing medicaments used for preventing and treating cerebral ischaemia and strokes. 1 claim

公开(公告)号：GR3036931T3

公开(公告)日：2002-01-31

申请号：GR20010401798

申请日：2001-10-18

Applicant: BASF AG

Inventor： RIECHERS HARTMUT ,  KLINGE DAGMAR ,  AMBERG WILHELM ,  KLING ANDREAS ,  MUELLER STEFAN ,  BAUMANN ERNST ,  RHEINHEIMER JOACHIM ,  VOGELBACHER UWE JOSEF ,  WERNET WOLFGANG ,  UNGER LILIANE ,  RASCHACK MANFRED

IPC: C07D251/30 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  C07D239/00 ,  C07D239/26 ,  C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/60 ,  C07D239/70 ,  C07D239/96 ,  C07D251/12 ,  C07D251/52 ,  C07D257/02 ,  C07D309/00 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048

Abstract: Heterocyclyl-substd. propanoic acids and their derivs., of formula (I), are new. R = formyl, tetrazolyl, nitrile, COOH or a gp. that can be hydrolysed to COOH; X = N or CR14; R2 = H, OH, NH2, alkylamino, dialkylamino, halo, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio; R14 = H or 1-5 C alkyl; R3 = R2 or alkoxyimino; or CR3 + CR14 = 5 or 6 membered alkylene or alkenyl ring (opt. substd. by 1-2 alkyl) in which a methylene can be replaced by O, S, NH or alkylamino; R4, R5 = phenyl or naphthyl (both opt. substd. by one or more halo, NO2, CN, OH, alkyl, haloalkyl, alkoxy, haloalkyloxy, phenoxy, alkylthio, NH2, alkylamine or dialkylamino) or 3-7 C cycloalkyl; or the phenyl or naphthyl gps. are opt. bonded at the O- position (by a bond, CH2, O, S, SO2, ethylene, ethenylene or opt. alkylated amino); R6 = H, 1-8 C alkyl, 2-6 C alkenyl, 3-6 C alkynyl, 3-8 C cycloalkyl (all opt. substd. by 1 or more halo, NO2, CN, alkoxy 3-6 C alkenyloxy, 3-6 C alkynyloxy, alkylthio, haloalkoxy, alkylcarbonyl, alkoxycarbonyl, 3-8 C alkylcarbonylalkyl, alkylamino, dialkylamino, phenyl, Ph or OPh), Ar or Het; Y = S, O or bond; Q = S, O, SO, SO2 or bond; Ph = substd. phenyl, where substits. are halo, NO2, CN, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio; Ar = phenyl or naphthyl (both opt. substd. by 1 or more halo, NO2, CN, OH, NH2, alkylamino, dialkylamino or OCH2CH2O); Het = 5 or 6 membered heteroaromatic with 1-3 N atoms and/or one S or O (opt. substd. by 1-4 halo and/or 1 or 2 alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, phenyl, phenoxy or phenyl carbonyl (where the phenyl is opt. substd. by 1-5 halo and/or 1-3 alkyl, haloalkyl, alkoxy, haloalkoxy and/or alkylthio)); alkyl and alkoxy have 1-4 C unless otherwise stated; provided that R6 is not H when Q = bond.

公开(公告)号：PL346003A1

公开(公告)日：2002-01-14

申请号：PL34600399

申请日：1999-07-20

Applicant: BASF AG

Inventor： STEINER GERD ,  HOEGER THOMAS ,  UNGER LILIANE ,  TESCHENDORF HANS-JUERGEN ,  JUCHELKA FRIEDER

IPC: A61K31/4184 ,  A61P25/20 ,  A61P25/24 ,  A61P25/30 ,  C07D403/06

Abstract: The invention relates to compounds of formula (1), wherein R , R and R have the meaning cited in the description. The novel substances are suitable for use in disease control.