公开(公告)号：US6111100C1

公开(公告)日：2002-04-02

申请号：US47490699

申请日：1999-12-30

Applicant: BASF AG

Inventor： RIECHERS HARTMUT ,  SIMON JOACHIM ,  HENNE ANDREAS ,  HOEHN ARTHUR

IPC: C07D295/08 ,  B01J23/72 ,  C07D295/088 ,  C07D413/12

CPC classification number: C07D295/088

公开(公告)号：JP2000212175A

公开(公告)日：2000-08-02

申请号：JP37063599

申请日：1999-12-27

Applicant: BASF AG

Inventor： RIECHERS HARTMUT ,  SIMON JOACHIM DR ,  HENNE ANDREAS ,  HOEHN ARTHUR

IPC: C07D295/08 ,  B01J23/72 ,  C07D295/088

Abstract: PROBLEM TO BE SOLVED: To obtain 2,2'-morpholino diethyl ether by using a specific catalyst before reducing diethylene glycol and ammonia with hydrogen. SOLUTION: This compound is obtained by incorporating a catalyst whose catalytic component contains aluminum oxide, zirconium dioxide, titanium dioxide, and/or silicon dioxide at 20-85 wt.%, an oxygen-containing compound of Cu at 1-70 wt.% as calculated as CuO, oxygen-containing compound(s) of Mg, Cr, Zn, Ba, and/or Ca at 0-50 wt.% as calculated as MgO, Cr2O3, ZnO, BaO, and/or CaO, respectively, and an oxygen-containing compound of Ni as calculated as NiO at less than 20 wt.% per the oxygen-containing compound of Cu before reducing diethylene glycol and ammonia with hydrogen in the presence of the obtained hydrogenation catalyst at an elevated temperature and pressure.

公开(公告)号：JP2001064281A

公开(公告)日：2001-03-13

申请号：JP2000221322

申请日：2000-07-21

Applicant: BASF AG

Inventor： RIECHERS HARTMUT ,  HOEHN ARTHUR ,  SIMON JOACHIM ,  LANG ORTMUND ,  SCHOENMAKERS HARTMUT ,  RAULS MATTHIAS DR ,  CLAERBOUT KOEN

IPC: C07D471/08 ,  C07D487/08

Abstract: PROBLEM TO BE SOLVED: To provide an effective and economical method for producing pure triethylenediamine(TEDA) and its solution. SOLUTION: This method for producing pure triethylenediamine solution comprises evaporating triethylenediamine and introducing the gas state triethylenediamine into a liquid solvent. The gaseous triethylendiamine is obtained from the top of a column or its side discharging port. Further, the pure triethylenediamine solution is produced by following the above method and then crystallizing the triethylenediamine from the solution. The liquid solvent is selected from the group consisting of cyclic or non-cyclic hydrocarbons, chlorinated aliphatic hydrocarbons, aromatic hydrocarbons, alcohols, ketones, aliphatic carboxylic acid esters, aliphatic nitriles and ethers.

公开(公告)号：WO9809953A3

公开(公告)日：1998-10-29

申请号：PCT/EP9704688

申请日：1997-09-02

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

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENROEDER 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

CPC classification number: C07D239/70 ,  C07C59/66 ,  C07C69/734 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D491/04

Abstract: Carboxylic acid derivatives have the formula (I), in which R1 stands for tetrazole or a group (a); R2 stands for hydrogen, hydroxy, NH¿2?, NH(C1-c4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-halogenalkyl, C1-C4-alkoxy, C1-C4-halogenalkoxy or C1-C4-alkylthio, or CR?2¿ is linked with CR10, as indicated below, into a 5- or 6-membered ring; X stands for nitrogen or methine; Y stands for nitrogen or methine; Z stands for nitrogen or CR10, wherein R10 is hydrogen or C¿1?-C4-alkyl or CR?10¿ forms together with CR?2 or CR3¿ an optionally substituted 5- or 6-membered alkylene or alkenylene ring, and wherein one or more methylene groups can be substituted by oxygen, sulphur, -NH or -N(C¿1?-C4-alkyl); R?3¿ stands for hydrogen, hydroxy, NH¿2?, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-halogenalkyl, C1-C4-alkoxy, C1-C4-halogenalkoxy, C1-C4-alkylthio; or CR?3¿ is linked to CR10 as indicated above into a 5- or 6-membered ring, R?4 and R5¿ (which may be identical or different) stand for optionally substituted phenyl or naphthyl, or for phenyl or naphthyl which are linked to each other at the ortho-position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulphur atom or an SO¿2?, NH or N-alkyl group; optionally substituted C3-C8-cycloalkyl; R?6¿ stands for optionally substituted C¿3?-C8-cycloalkyl; optionally substituted phenyl or naphthyl, a 5- or 6-membered, optionally substituted heteroaromatic compound containing one to three nitrogen atoms and/or one sulphur or oxygen atom; W stands for sulphur or oxygen; Q is a spacer with a length that corresponds to a C2-C4 chain. Also disclosed are the physiologically tolerable salts of these compounds, as well as their pure enantiomer and diastereoisomer forms, their preparation and use as mixed ETA/ETB-receptor antagonists.

公开(公告)号：CA2362365C

公开(公告)日：2009-07-14

申请号：CA2362365

申请日：1999-05-10

Applicant: BASF AG

Inventor： SIEGEL WOLFGANG ,  NUBLING CHRISTOPH ,  HOHN ARTHUR ,  FUNKE FRANK ,  KRAMER ANDREAS ,  SIMON JOACHIM ,  RIECHERS HARTMUT

IPC: B01J23/755 ,  C07C209/88 ,  C07B55/00 ,  C07B57/00 ,  C07B61/00 ,  C07C209/68 ,  C07C211/03 ,  C07C213/02 ,  C07C213/08 ,  C07C213/10 ,  C07C217/08

Abstract: The invention relates to a method for producing racemic amines of formula (I ), in which R1 and R2 are not the same and R1, R2, R3 are alkyl-, cycloalkyl-, arylalkyl-, aryl-, heteroaryl rests and heterocyclic rests and R3 also represents hydrogen. Said rests can carry substituents selected from the group of alkyl, cycloalkyl, alkoxy, aryloxy, amino, alkylamino and dialkylamino. The method is characterized in that the corresponding optically active amine (I) and the secondary alcoh ol of formula (II) and/or the asymmetrical ketone of formula (III) and the amine of the formula R3NH2 are simultaneously reacted in situ in the presence of hydrogen and a hydrogenation or dehydrogenation catalyst at an elevated temperature.

公开(公告)号：DE19533023B4

公开(公告)日：2007-05-16

申请号：DE19533023

申请日：1995-09-07

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: C07D239/60 ,  C07D251/30 ,  A61K31/41 ,  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 ,  C07D239/70 ,  C07D239/96 ,  C07D251/12 ,  C07D251/52 ,  C07D257/02 ,  C07D309/00 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D495/04

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：SK8682001A3

公开(公告)日：2002-08-06

申请号：SK8682001

申请日：1999-12-09

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  RIECHERS HARTMUT ,  BAUMANN ERNST ,  HERGENRODER 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 ,  C07D239/60

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：HK1040704A1

公开(公告)日：2002-06-21

申请号：HK02102528

申请日：2002-04-04

Applicant: BASF AG

Inventor： BERNARD HARALD ,  RIECHERS HARTMUT

IPC: C07C51/43 ,  C07B57/00 ,  C07C51/487 ,  C07C59/11 ,  C07C59/48 ,  C07C59/64 ,  C07C ,  C07B

Abstract: A process for racemate resolution of 2-hydroxypropionic acids by reacting the racemic acid with an optically active base and subsequently separating off a diastereomeric salt of acid and base comprises using 1-(4-chlorophenyl)ethylamine as optically active base.

公开(公告)号：NO312674B1

公开(公告)日：2002-06-17

申请号：NO991079

申请日：1999-03-04

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENROEDER 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 ,  C07D237/34

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：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).