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公开(公告)号:PL340871A1
公开(公告)日:2001-03-12
申请号:PL34087198
申请日:1998-10-16
Applicant: BASF AG
Inventor: AMBERG WILHELM , JANSEN ROLF , HERGENROEDER STEFAN , RASCHACK MANFRED , UNGER LILIANE
IPC: A61K31/505 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5377 , A61P9/02 , A61P9/10 , A61P9/12 , A61P13/08 , A61P13/12 , A61P35/00 , A61P43/00 , C07D239/34 , C07D239/36 , C07D239/52 , C07D239/60 , C07D239/70 , C07D401/12 , C07D403/12 , C07D491/048 , A61P9/04
Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the meaning as commented in the description. It also relates to the production and use of same as endothelin receptor antagonists.
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公开(公告)号:ID26183A
公开(公告)日:2000-12-07
申请号:ID20001703
申请日:1999-02-25
Applicant: BASF AG
Inventor: AMBERG WILHELM , JANSEN ROLF , KLINGE DAGMAR , RIECHERS HARTMUT , GENRODER STEFAN , RASCHACK MANFRED , UNGER LILIANE
IPC: C07D251/22 , A61K31/192 , A61K31/216 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/53 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/08 , A61P13/12 , A61P35/00 , A61P43/00 , C07C59/66 , C07C59/68 , C07C69/734 , C07D213/63 , C07D239/34 , C07D239/52 , C07D239/60 , C07D405/12 , C07D491/048 , C07D403/12 , C07D213/64 , A61K
Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein R -R , Q, W, X, Y and Z have the meanings given in the description. The novel compounds are suitable for combating diseases.
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公开(公告)号:AT197448T
公开(公告)日:2000-11-11
申请号:AT96930125
申请日:1996-08-29
Applicant: BASF AG
Inventor: AMBERG WILHELM , KLING ANDREAS , KLINGE DAGMAR , RIECHERS HARTMUT , UNGER LILIANE , RASCHACK MANFRED , HERGENROEDER STEFAN , ELGER BERND , SCHULT SABINE
IPC: C07D317/02 , A61K31/00 , 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: 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.
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公开(公告)号:TR9802042T2
公开(公告)日:2000-09-21
申请号:TR9802042
申请日:1997-04-04
Applicant: BASF AG
Inventor: AMBERG WILHELM , KLING ANDREAS , KLINGE DAGMAR , RIECHERS HARTMUT , BAUMANN ERNST , UNGER LILIANE , RASCHACK MANFRED , HERGENROEDER STEFAN , SCHULT SABINE
IPC: A61K31/00 , A61K31/47 , A61K31/505 , A61P9/00 , A61P9/12 , A61P13/00 , A61P13/12 , C07D215/22 , C07D215/227 , C07D239/34 , C07D239/60 , C07D401/12 , C07D403/12
CPC classification number: C07D215/227 , C07D239/34 , C07D239/60
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公开(公告)号:PL337507A1
公开(公告)日:2000-08-28
申请号:PL33750798
申请日:1998-06-05
Applicant: BASF AG
Inventor: AMBERG WILHELM , KLING ANDREAS , KLINGE DAGMAR , REICHERS HARTMUT , HERGENROEDER 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
Abstract: The invention relates to carboxylic acid derivatives of formula (I) wherein the constituents have the meaning given in the description. The invention also relates to the production of said derivatives, and to their use as endothelin receptor antagonists.
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公开(公告)号:CO4930270A1
公开(公告)日:2000-06-27
申请号:CO97073662
申请日:1997-12-17
Applicant: BASF AG
Inventor: AMBERG WILHELM , JANSEN ROLF , KLING ANDREAS , KLINGE DAGMAR , RIECHERS HARTMUT , HERGENRODER STEFAN , RASCHACK MANFRED , 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: Derivados de ácido carbónico de la fórmula I: CARACTERIZADOS porque R1 representa tetrazol o a un grupo en el que R tiene el siguiente significado: a) un residuo OR6 , en donde R6 significa: hidrógeno, el catión de un metal alcalino, el catión de metal alcalinotérreo, o un ión amonio fisiológicamente compatible; C3 -C8 cicloalquilo, C1 -C8 alquilo, CH2 -fenilo, que puede ser sustituido, un grupo C3 -C6 -alquenilo o C3 -C6 - alquinilo, que puede ser sustituido o fenilo, en caso dado, sustituido.b) un heteroaromático de 5 eslabones ligado con un átomo de nitrógeno, c) un grupo en el que k puede tomar los valores 0,1 y 2, p los valores 1, 2, 3 y 4 y R7 representa d) un residuo - 2 -donde R8 significa : C1 -C4 -alquilo, C3 -C8 -alquenilo, C3 -C8 -alquinilo, C3 -C8 -cicloalquilo, donde estos residuos pueden tener un residuo C1 -C4 -alcoxi, C1 -C4 -alquiltio y/o un residuo fenilo C1 -C4 -halogenalquilo o fenilo, en caso de ser necesario, sustituido; X nitrógeno o metino, con la condición de que si X = nitrógeno, entonces Z=nitrógeno y si X = metino, entonces por lo menos uno de los eslabones Y o Z son nitrógeno; Y nitrógeno o CR9 ; Z nitrógeno o CR10 , R2 C1 -C4 -alquilo, C2 -C4 -alquenilo, C2 -C4 -alquinilo, pudiendo estar estos residuos sustituidos; hidrógeno, halógeno, C1 -C4 -alcoxi, C1 -C4 -halogenalcoxi, C3 -C6 -alqueniloxi, C3 -C6 -alquiniloxi, C1 -C4 -alquiltio, C1 -C4 -alquilcarbonilo, C1 -C4 -coxicarbonilo, NH(C1 -C4 -alquilo) N(C1 -C4 -alquilo)2 , hidroxi, carboxi, ciano, amino; o CR2 junto con CR9 o CR10 forma un anillo de alquileno de 5 ó 6 eslabones o de alquenilo, que puede ser sustituido por uno o dos grupos C1 -C4 -alquilo y en donde uno o más grupos metilenos pueden ser sustituidos por oxígeno, azufre -NH o N(C1 -C4 -alquilo)2 . R3 y R4 (que pueden ser iguales o distintos) son: fenilo o naftilo, que pueden ser sustituidos fenilo o naftilo, que pueden estar unidos en posición orto por una unión directa a un grupo metileno, etileno o etenileno, a un átomo de oxígeno o azufre o a un grupo SO2 , NH- o N-alquilo; C3 -C8 -cicloalquilo, que puede ser sustituido; R5 hidrógeno, C1 -C8 alquilo, C3 -C8 -alquenilo o C3 -C8 -alquinilo, pudiendo estar estos residuos sustituidos; fenilo o naftilo, que pueden ser sustituidos; un heteroaromático de cinco a seis eslabones conteniendo de uno a tres átomos de nitrógeno y/o un átomo de azufre u oxígeno, el cual puede ser sustituido C3 -C8 -cicloalquilo, que puede ser sustituido R9 y R10 (que pueden ser iguales o diferentes) son:hidrógeno, hidroxi, NH2 , NH(C1 AND#8209;C4 AND#8209;alquilo), N(C1 AND#8209;C4 AND#8209;alquilo)2 , halógeno, C1 AND#8209;C4 alcoxi, C1 AND#8209;C4 AND#8209;halogenalcoxi o C1 AND#8209;C4 AND#8209;alquiltio; C1 AND#8209;C4 AND#8209;alquilo, C2 AND#8209;C4 AND#8209;alquenilo, C2 AND#8209;C4 AND#8209;alquinilo, pudiendo estos residuos estar sustituidos; o bien CR9 o CR10 está unido con CR2 como en R2 para dar un anillo de 5 o 6 eslabones;W es azufre, oxígeno o una unión simple; Q es oxígeno o nitrógeno, con la condición que en caso que Q = N, entonces W es una unión simple. así como las sales fisiológicamente compatibles y las formas enantiómeras y diastereómeras.
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公开(公告)号:NZ331704A
公开(公告)日:2000-06-23
申请号:NZ33170497
申请日:1997-04-04
Applicant: BASF AG
Inventor: AMBERG WILHELM , KLING ANDREAS , KLINGE DAGMAR , RIECHERS HARTMUT , BAUMANN ERNST , UNGER LILIANE , RASCHACK MANFRED , HERGENRODER STEFAN , SCHULT SABINE
IPC: A61K31/00 , A61K31/47 , A61K31/505 , A61P9/00 , A61P9/12 , A61P13/00 , A61P13/12 , C07D215/22 , C07D215/227 , C07D239/34 , C07D239/60 , C07D401/12 , C07D403/12
Abstract: These carboxylic acid derivatives, which are useful as inhibitors of endothelin receptors, are of the formula I where R is tetrazole, nitrile, COOH, R2 is H, OH, NH2, NHalkyl, N(alkyl)2, halo, alkyl, haloalkyl,alkoxy, haloalkoxy, alkylthio or CR2 is linked to CR12 to form a 5-6 membered ring; X is N or CR6, Y is N or CH, R3 is R2 or CR3 is linked to CR12 to form a 5-6 membered ring; R4 and R5 are generally optionally substituted phenyl or naphthyl; Z is S or O and R6 is selected from a wide group of substituents.
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公开(公告)号:DE19858779A1
公开(公告)日:2000-06-21
申请号:DE19858779
申请日:1998-12-18
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 , C07D239/70 , C07D247/00 , C07D403/06
Abstract: 3-(Acylamino or sulfonylamino)-2-heteroaryloxy-propionic acid derivatives are new. The 3-(acylamino or sulfonylamino)-2-heteroaryloxy-propionic acid derivatives are compounds of formula (I) and their enantiomers, diastereoisomers and salts, excluding the compounds 2-(6-ethyl-2-methyl-pyrimidin-4-yloxy)-3-(4-methoxybenzoylamino)-3,3-d iphenylpropionic acid; 2-(2,6-dimethyl-pyrimidin-4-yloxy)-3-(4-methoxybenzoylamino)-3,3-diphe nylpropionic acid; 3-(4-methoxy-benzoylamino)-2-(6-methoxy-2-methyl-pyrimidin-4-yloxy)-3, 3-diphenylpropionic acid; 3-(4-methoxy-benzoylamino)-2-(6-methoxy-5-methyl-pyrazin-2-yloxy)--3,3 -diphenylpropionic acid; 3-(4-methoxy-benzoylamino)-2-(5-methoxy-6-methyl-(1,2,4)triazin-3-ylox y)-3,3-diphenylpropionic acid; 2-(4-ethyl-6-methyl-(1,3,5)triazin-2-yloxy)-3-(4-methoxy-benzoylamino) -3,3-diphenylpropionic acid; 3-(4-methoxy-benzoylamino)-2-(5-methoxy-6-methyl-pyridazin-3-yloxy)--3 ,3-diphenylpropionic acid; 2-(4,6-dimethyl-(1,3,5)triazin-2-yloxy)-3-(4-methoxy-benzoylamino)--3, 3-diphenylpropionic acid; 3-(4-methoxy-benzoyl amino)-2-(4-methoxy-6-methyl-(1,3,5)triazin-2-yloxy)-3,3-diphenylpropi onic acid; 3-(4-methoxy-benzoylamino)-2-(4-methoxy-6,7-dihydro-5H-cyclopentapyrim idin-2-yloxy)-3,3-diphenylpropionic acid; 3-(4-methoxy-benzoylamino)-2-(4-methoxy-5,6-dihydrofuro(2,3-d)pyrimidi n-2-yloxy)--3,3-diphenylpropionic acid; 2-(4,6-dimethoxy-pyrimidin-2-yloxy)-3-(4-methoxy-benzoylamino)-3,3-dip henylpropionic acid; 2-(4-ethyl-6-methyl-pyrimidin-2-yloxy)-3-(4-methoxy-benzoylamino)-3,3- diphenylpropionic acid; 2-(4,6-dimethyl-pyrimidin-2-yloxy)-3-(4-methoxy-benzoylamino)-3,3-diph enylpropionic acid; 3-(4-methoxy-benzoylamino)-2-(4-methoxy-6-methyl-pyrimidin-2-yloxy)-3, 3-diphenylpropionic acid; 2-(4,6-dimethyl-pyrimidin-2-yloxy)-3-(4-hydroxy-benzoylamino)--3,3-dip henylpropionic acid; 2-(4-methoxy-6-methyl-pyrimidin-2-yloxy)-3-(4-methylsulfanyl-benzoylam ino)--3,3-diphenylpropionic acid; 2-(4,6-dimethyl-pyrimidin-2-yloxy)-3-(4-nitro-benzoylamino)-3,3-diphen ylpropionic acid; 3-(4-chloro-benzoylamino)-2-(4-ethyl-6-methyl-pyrimidin-2-yloxy)-3,3-d iphenylpropionic acid; 3-(4-ethyl-benzoylamino)-2-(4-methoxy-6,7-dihydro-5H-cyclopentapyrimid in-2-yloxy)-3,3-diphenylpropionic acid; 3,3-bis(4-fluorophenyl)-3-(4-methoxy-benzoylamino)-2-(4-methoxy-5,6-di hydrofuro(2,3-d)pyrimidin-2-yloxy)-3,3-diphenylpropionic acid; 3-(4-chloro-benzoylamino)--2-(4,6-dimethyl-(1,3,5)triazin-2-yloxy)--3, 3-diphenylpropionic acid; 3-(3,4-dimethoxy-benzoylamino)-2-(4-methoxy-6-methyl-(1,3,5)triazin-2- yloxy)-3,3-diphenylpropionic acid; 3-(3,4-dimethoxy-benzoylamino)-2-(4-ethyl-6-methyl-(1,3,5)triazin-2-yl oxy)-3,3-diphenylpropionic acid; 3-(4-chloro-benzoylamino)-2-(5-methoxy-6-methyl-pyridazin-3-yloxy)-3,3 -diphenylpropionic acid; 3-(3,4-dichloro-benzoylamino)-2-(6-methoxy-5-methyl-pyrazin-2-yloxy)-3 ,3-diphenylpropionic acid; 3-(4-hydroxy-3-methoxy-benzoylamino)-2-(5-methoxy-6-methyl-(1,2,4)tria zin-3-yloxy)-3,3-diphenylpropionic acid; 3-(3-chloro-benzoylamino)-2-(2,6-dimethyl-pyrimidin-4-yloxy)-3,3-diphe nylpropionic acid; 3-(2-chloro-benzoylamino)-2-(6-methoxy-2-methyl-pyrimidin-4-yloxy)-3,3 -diphenylpropionic acid; and 2-(6-ethyl-2-methyl-pyrimidin-4-yloxy)-3-(4-nitro-benzoylamino)-3,3-di phenylpropionic acid. R1 = tetrazolyl, or C(O)R; R = OR6, N-bonded 5-membered heteroaryl; -O-(CH2)p-S(O)k-R7; or -NH-SO2-R8; R6 = H, or 3-8C cycloalkyl, 1-8C alkyl, benzyl, 3-8C alkenyl, 3-8C alkynyl, or phenyl (all optionally substituted); k = 0-2; p = 1-4; R7 = 1-4C alkyl; 3-8C cycloalkyl; 3-8C alkenyl; 3-8C alkynyl; or optionally substituted phenyl; R8 = 1-4C alkyl, 3-8C alkenyl, 3-8C alkynyl or 3-8C cycloalkyl (each optionally substituted with 1-4C alkoxy, 1-4C alkylthio and/or phenyl); 1-4C haloalkyl; or optionally substituted phenyl; X = N or CR9; Y = N or CR10; Q = N or CR11 (X = CR9 and Y = CR10 when Q = N); W and V = N or CH (Q = N when W = V = CH); R9 and R10 = H, halo, 1-4C alkoxy, 1-4C haloalkoxy, 3-6C alkenyloxy, 3-6C alkynyloxy, 1-4C alkylthio, 1-4C alkylcarbonyl, 1-4C alkoxycarbonyl, OH, NH2, NH(1-4C alkyl), N(1-4C alkyl)2, or 1-4C alkyl, 2-4C alkenyl or 2-4C alkynyl (each optionally substituted); or R9 or R10 together with R11 forms a 5-6 membered alkylene or alkenylene group in which 1 or more CH2 is replaced with O, S, NH or N(1-4 alkyl); R11 = H, halo, 1-4C alkoxy, 1-4C haloalkoxy, 3-6C alkenyloxy, 3-6C alkynyloxy, 1-4C alkylthio, 1-4C alkylcarbonyl, 1-4C alkoxycarbonyl, NH(1-4C alkyl), N(1-4C alkyl)2, OH, COOH, CN, NH2, SH, or 1-4C alkyl, 2-4C alkenyl or 2-4C alkynyl (each optionally substituted); R2 and R3 = phenyl or naphthyl (both optionally substituted or optionally bonded to one another via a bond, CH2, CH2CH2, CH=CH, O, S, SO2, NH or N-alkyl); or 5-6C cycloalkyl; R4 = C(O)R12 or SO2R13; R12 = phenyl, naphthyl or 5-6 membered heteroaryl containing 1-3 N and/or 1 O or S atom (each optionally substituted); R13 = 1-4C alkyl or 1-4C alkoxy (each optionally substituted with halo), 1-4C alkylthio, or phenyl or phenoxy (each optionally substituted); and R5 = H or 1-4C alkyl. Independent claims are also included for the following: (1) 3-(acylamino or sulfonamido)-2-hydroxy-propionic acid derivatives (II); (2) the use of (I) in combination with a renin angiotensin system inhibitor, e.g. renin inhibitor, angiotensin-II antagonist, especially an ACE inhibitor, mixed ACE/neutral endopeptidase (NEP) inhibitor or beta -blocker; and (3) a fragment of formula (A) as a structural element in an endothelial receptor antagonist.
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公开(公告)号:ZA989923B
公开(公告)日:2000-05-02
申请号:ZA989923
申请日:1998-10-30
Applicant: BASF AG
Inventor: AMBERG WILHELM , JANSEN ROLF , HERGENROEDER STEFAN , RASCHACK MANFRED , UNGER LILIANE
IPC: C07D239/36 , C07D239/52 , C07D239/60 , C07D401/12 , C07D , A61K , C07B
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公开(公告)号:ZA9809923B
公开(公告)日:2000-05-02
申请号:ZA9809923
申请日:1998-10-30
Applicant: BASF AG
Inventor: AMBERG WILHELM , JANSEN ROLF , HERGENROEDER STEFAN , RASCHACK MANFRED , UNGER LILIANE
IPC: C07D239/36 , C07D239/52 , C07D239/60 , C07D401/12 , C07D , A61K , C07B
CPC classification number: C07D239/36 , C07D239/52 , C07D239/60 , C07D401/12
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