公开(公告)号：DE10025728A1

公开(公告)日：2001-11-29

申请号：DE10025728

申请日：2000-05-25

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KETTSCHAU GEORG

IPC: C07D251/22 ,  A61K31/44 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61P1/18 ,  A61P7/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P15/10 ,  A61P43/00 ,  C07D213/69 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D241/18 ,  C07D401/12 ,  C07D403/12 ,  C07D491/048 ,  C07D495/04 ,  C07D239/24 ,  C07D247/00 ,  C07D251/12

Abstract: The invention relates to carbamate and carbamide derivatives of formula (I), wherein the substituents have the meaning cited in the description. The invention also relates to the production and use thereof as endothelin receptor antagonists.

公开(公告)号：DK0785926T3

公开(公告)日：2001-10-08

申请号：DK95935916

申请日：1995-10-07

Applicant: BASF AG

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

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：NO20013000L

公开(公告)日：2001-08-15

申请号：NO20013000

申请日：2001-06-15

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  RIECHERS HARTMUT ,  BAUMANN ERNST ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/24 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P15/10 ,  A61P35/00 ,  A61P43/00 ,  C07C229/34 ,  C07C233/87 ,  C07C235/52 ,  C07D239/34 ,  C07D251/22 ,  C07D401/12 ,  C07D491/048

Abstract: The invention relates to carboxylic acid derivatives of formula (I), in which the substituents have the following meanings: R is tetrazol or a group (a); W and Z, can be identical or different and are nitrogen or methine, provided that if W and Z are methine, then Q is nitrogen; X is nitrogen or CR ; Y is nitrogen or CR ; Q is nitrogen or CR , provided that if Q is nitrogen then X is CR and Y is CR ; R and R are identical or different and are possibly substituted phenyl or naphthyl or phenyl or naphthyl which are linked in an ortho position via a direct bond, a methlyene, ethylene or ethenylene group, an oxygen or sulfur atom or a SO2-, NH- or N-alkyl group or possibly substituted C5-C6-cycloalkyl; R is a rest (b) or (c); and R is hydrogen, C1-C4-alkyl. The invention further relates to their preparation and their use as endothelin receptor antagonists. The invention also relates to compounds of formula (II) and a structural fragment of formula (d) in which the rests R , R , R , R and R have the meanings given in claim no. 1 and to their use as structural elements in an endothelin receptor antagonist.

公开(公告)号：NO20013000A

公开(公告)日：2001-08-15

申请号：NO20013000

申请日：2001-06-15

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  RIECHERS HARTMUT ,  BAUMANN ERNST ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/24 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P15/10 ,  A61P35/00 ,  A61P43/00 ,  C07C229/34 ,  C07C233/87 ,  C07C235/52 ,  C07D239/34 ,  C07D251/22 ,  C07D401/12 ,  C07D491/048

CPC classification number: C07D251/22 ,  C07C229/34 ,  C07C235/52 ,  C07D239/34

公开(公告)号：NO310651B1

公开(公告)日：2001-08-06

申请号：NO981002

申请日：1998-03-06

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  RASCHACK MANFRED ,  HERGENROEDER STEFAN ,  ELGER BERND ,  SCHULT SABINE

IPC: A61K31/00 ,  A61K31/19 ,  C07D317/02 ,  A61K31/192 ,  A61K31/34 ,  A61K31/341 ,  A61K31/343 ,  A61K31/35 ,  A61K31/352 ,  A61K31/357 ,  A61K31/36 ,  A61K31/435 ,  A61K31/44 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  C07C53/134 ,  C07C57/30 ,  C07C57/32 ,  C07C57/38 ,  C07C59/64 ,  C07C69/616 ,  C07C69/734 ,  C07C255/00 ,  C07D213/55 ,  C07D213/64 ,  C07D221/04 ,  C07D239/26 ,  C07D239/34 ,  C07D239/52 ,  C07D239/70 ,  C07D257/04 ,  C07D307/79 ,  C07D317/50 ,  C07D317/60 ,  C07D319/02 ,  C07D319/18

Abstract: PCT No. PCT/EP96/03793 Sec. 371 Date Feb. 24, 1998 Sec. 102(e) Date Feb. 24, 1998 PCT Filed Aug. 29, 1996 PCT Pub. No. WO97/09294 PCT Pub. Date Mar. 13, 1997Carboxylic acid derivatives of the formula I here R1 is a tetrazole [sic], nitrile [sic], a group COOH or a radical which can be hydrolyzed to COOH, and the other substituents have the meaning explained in the description.

公开(公告)号：AU736414B2

公开(公告)日：2001-07-26

申请号：AU4552497

申请日：1997-09-02

Applicant: BASF AG

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

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61P9/04 ,  A61P9/08 ,  A61P9/12 ,  A61P43/00 ,  C07C59/66 ,  C07C69/734 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D491/04 ,  C07D491/048

Abstract: The invention relates to carboxylic acid derivatives of the formula Iwhere the radicals have the meanings stated in the description, and to their use as drugs.

公开(公告)号：CO5040228A1

公开(公告)日：2001-05-29

申请号：CO96047377

申请日：1996-09-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  DAGMAR KLINGE ,  RIECHERS HARTMUT ,  UNGER UNGER ,  MANFRED RASCHACK ,  HERGENRODER STEFAN ,  BERND ELGER ,  SCHULT SABINE

IPC: C07D317/02 ,  A61K31/00 ,  A61K31/185 ,  A61K31/19 ,  A61K31/192 ,  A61K31/34 ,  A61K31/341 ,  A61K31/343 ,  A61K31/35 ,  A61K31/352 ,  A61K31/357 ,  A61K31/36 ,  A61K31/435 ,  A61K31/44 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  C07C53/134 ,  C07C57/30 ,  C07C57/32 ,  C07C57/38 ,  C07C59/64 ,  C07C69/616 ,  C07C69/734 ,  C07C255/00 ,  C07D213/55 ,  C07D213/64 ,  C07D221/04 ,  C07D239/26 ,  C07D239/34 ,  C07D239/52 ,  C07D239/70 ,  C07D257/04 ,  C07D307/79 ,  C07D317/50 ,  C07D317/60 ,  C07D319/02 ,  C07D319/18

Abstract: Derivados del ácido carboxílico de la fórmula IEn la que R1 significa un tetrazol, nitrilo, un grupo COOH o un radical COOH hidrolizable, y los otros sustituyentes tienen los siguientes significados:R2 y R3 (que pueden ser idénticos o diferentes):Fenilo o naftilo, que puede estar sustituido por uno o varios de los siguientes radicales: Halógeno, ciano, NO2 , hidroxi, C1 -C4 -alquilo, C1 -C4 -halógenoalquilo, C1 -C4 -alcoxi, C1 -C4 - halógenoalcoxi, fenoxi, C1 -C4 -alquiltio, amino, benciloxi, C1 -C4 -dialquilamino; ó fenilo o naftilo que están unidos entre sí en posición orto por vía de un enlace directo, un grupo metileno, etileno o etinileno, un átomo de oxígeno o de azufre;R4 fenilo o naftilo, metilendioxifenilo, etilendioxifenilo, indanilo, indolilo, piridilo, benzopiranilo, furanilo, benzofuranilo, isooxazolilo, isotiazolilo, 1, 3, 4-tiadiazolilo, pirimidinilo, 2,3-dihidrobenzofuranilo, benzotienilo, quinolinilo, C3 -C7 -cicloalquilo, tienilo, oxazolilo, tiazolilo, que pueden estar sustituidos por uno o varios de los siguientes radicales: halógeno, ciano, hidroxi, NO2 , C1 -C4 alquilo, C1 -C4 -halógenoalquilo, C1 -C4 -alcoxi, C1 -C4 -halogenoalcoxi, fenoxi, C1 -C4 -alquiltio, amino, beciloxi, C1 -C4 - alquilamino o C1 -C4 -dialquilamino, pudiendo los radicales alquilo formar juntos un anillo;R5 C1 -C8 alquilo, C3 -C6 -alquenilo, C3 -C6 -alquinilo o C3 -C8 -cicloalquilo, cuyos radicales pueden estar mono o polisustituidos por: halógeno, C1 -C4 -alcoxi, C1 -C4 -alquiltio, C1 -C4 -alquilamino, di-C1 -C4 -alquilamino;fenilo, bencilo, 1-metilnaftilo, 2-metilnaftilo o naftilo, que puede estar sustituidos cada vez por uno o varios de los siguientes radicales: halógeno, ciano, hidroxi, amino, C1 -C4 -alquilo, C1 -C4 - alcoxi, fenoxi, C1 -C4 -alquiltio, dioximetileno o dioxoetileno;n 1 - 2.

公开(公告)号：AU7912600A

公开(公告)日：2001-05-10

申请号：AU7912600

申请日：2000-10-02

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  HORNBERGER WILFRIED

IPC: A61K38/00 ,  A61K45/00 ,  A61K45/06 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P37/06 ,  A61P43/00 ,  C07D239/34 ,  C07D263/34 ,  C07D277/48 ,  C07D307/68 ,  C07D333/38 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07K5/02

公开(公告)号：HU0000553A2

公开(公告)日：2001-04-28

申请号：HU0000553

申请日：1997-12-04

Applicant: BASF AG

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

IPC: C07D253/06 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  C07D237/14 ,  C07D237/16 ,  C07D241/18 ,  C07D253/07 ,  C07D253/075 ,  C07D253/10 ,  C07D403/12 ,  C07D491/04

Abstract: The present invention relates to carboxylic acid derivatives of the formula Iwhere the substituents have the meanings explained in the description, and to preparation and use as endothelin receptor antagonists.

公开(公告)号：AU731458B2

公开(公告)日：2001-03-29

申请号：AU1192597

申请日：1996-12-11

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  BARLOZZARI TERESA ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  HEGE HANS-GUENTHER ,  JANSSEN BERND ,  KLING ANDREAS ,  LIETZ HELMUT ,  RITTER KURT ,  ULLRICH MARTINA ,  WEYMANN JURGEN ,  ZIERKE THOMAS

IPC: A61K38/00 ,  A61K31/00 ,  A61K38/08 ,  A61P35/00 ,  A61P35/02 ,  C07K1/00 ,  C07K7/06

Abstract: Novel peptides of the formula R R N-CHX-CO-A-B-D-E-(G)s-K in which R , R , A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.