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1. 发明申请

WO1997021701A1 FARNESYL PROTEIN TRANSFERASE INHIBITING (IMIDAZOL-5-YL)METHYL-2-QUINOLINONE DERIVATIVES 审中-公开
标题翻译：蛋氨酸转运酶抑制剂（咪咪唑-5-基）甲基-2-喹啉酮衍生物
公开(公告)号：WO1997021701A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996004515
申请日：1996-10-16
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston , ANGIBAUD, Patrick, René , MULLER, Philippe , SANZ, Gérard, Charles
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/14 , Y02P20/55
摘要： This invention comprises the novel compounds of formula (I), wherein the dotted line represents an optional bond; X is oxygen or sulfur; R is hydrogen, C1-12alkyl, Ar , Ar C1-6alkyl, quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula -Alk -C(=O)-R , -Alk -S(O)-R or -Alk -S(O)2-R ; R , R and R each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar , Ar C1-6alkyl, Ar oxy, Ar C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; R and R each independently are hydrogen, halo, Ar , C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1-6alkylS(O)2C1-6alkyl; R and R each independently are hydrogen, halo, cyano, C1-6alkyl, 4,4-dimethyl-oxazolyl, C1-6alkyloxy or Ar oxy; R is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl, cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, carboxyC1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, imidazolyl, haloC1-6alkyl, C1-6alkyloxyC1-6alkyl, aminocarbonylC1-6alkyl, or a radical of formula -O-R , -S-R , -N-R R ; R is hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxycarbonyl, Ar ; R is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R is hydrogen or C1-6alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中虚线表示任选的键; X是氧或硫; R 1是氢，C 1-12烷基，Ar 1，Ar 2 C 1-6烷基，喹啉基C 1-6烷基，吡啶基C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，单或二（C 1-6烷基）氨基C 1-6烷基，氨基C 1-6烷基或式-Ak 1 -C（= O）-R 9，-AlK 1 -S（O）-R 9或-Alk 1> -S（O）2-R <9>; R 2，R 3和R 16各自独立地是氢，羟基，卤素，氰基，C 1-6烷基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，氨基C 1-6烷氧基，单或二（C 1-6烷基）氨基C 1-6烷氧基，Ar 1，Ar 2 C 1-6烷基，Ar 2氧基，Ar 2 C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基，三卤甲基，三卤甲氧基，C 2-6烯基 ; R 4和R 5各自独立地为氢，卤素，Ar 1，C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基S（O）C 1-6烷基或C 1-6烷基S（O）2 C 1-6烷基; R 6和R 7各自独立地为氢，卤素，氰基，C 1-6烷基，4,4-二甲基 - 恶唑基，C 1-6烷氧基或Ar 2氧基; R 8是氢，C 1-6烷基，氰基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基C 1-6烷基，氰基C 1-6烷基，C 1-6烷氧基羰基C 1-6烷基，羧基C 1-6烷基，羟基C 1-6烷基，氨基C 1-6烷基，二（C 1-6烷基）氨基C 1-6烷基，咪唑基，卤代C 1-6烷基，C 1-6烷氧基C 1-6烷基，氨基羰基C 1-6烷基或式-OR 10，-SR 10，-NR 11 R 12>; R 17是氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基羰基，Ar 1; R 18是氢，C 1-6烷基，C 1-6烷氧基或卤素; R 19是氢或C 1-6烷基; 具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

2. 发明申请

WO1997016443A1 FARNESYL TRANSFERASE INHIBITING 2-QUINOLONE DERIVATIVES 审中-公开
标题翻译：呋喃酮转移抑制2-喹啉酮衍生物
公开(公告)号：WO1997016443A1
公开(公告)日：1997-05-09
申请号：PCT/EP1996004661
申请日：1996-10-25
申请人： JANSSEN PHARMACEUTICA N.V. , END, David, William , VENET, Marc, Gaston , ANGIBAUD, Patrick, René , SANZ, Gérard, Charles
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06
摘要： The present invention is concerned with compounds of formula (I), the stereoisomeric forms thereof and the pharmaceutically acceptable acid or base addition salts thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R is hydrogen, C1-12alkyl, Ar , Ar C1-6alkyl, quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)-aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula -Alk -C(=O)-R , -Alk -S(O)-R or -Alk -S(O)2-R ; R and R each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxy-C1-6alkyloxy, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar , Ar C1-6alkyl, Ar oxy, Ar C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; or when on adjacent positions R and R taken together may form a bivalent radical; R and R each independently are hydrogen, Ar , C1-6alkyl, C1-6alkyloxy-C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1-6alkylS(O)2-C1-6alkyl; R and R each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy or Ar oxy; R is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl, cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, hydroxycarbonyl-C1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, haloC1-6alkyl, C1-6alkyloxy-C1-6alkyl, aminocarbonylC1-6alkyl, Ar , Ar C1-6alkyloxyC1-6alkyl, C1-6alkylthioC1-6alkyl; R is hydrogen, C1-6alkyl or halo; R is hydrogen or C1-6alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及式（I）化合物，其立体异构形式及其药学上可接受的酸或碱加成盐，其中虚线表示任选的键; X是氧或硫; R 1是氢，C 1-12烷基，Ar 1，Ar 2 C 1-6烷基，喹啉基C 1-6烷基，吡啶基C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，单或二（C 1-6烷基） - 氨基C 1-6烷基，氨基C 1-6烷基或式-Ak 1 -C（= O）-R 9，-AlK 1 -S（O）-R 9或-Alk <1> -S（O）2-R <9>; R 2和R 3各自独立地是氢，羟基，卤素，氰基，C 1-6烷基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基-C 1-6烷氧基，氨基C 1-6烷氧基，一或二（C 1 1-6烷基）氨基C 1-6烷氧基，Ar 1，Ar 2 C 1-6烷基，Ar 2氧基，Ar 2 C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基，三卤甲基，三卤甲氧基，C 2-6烯基; 或者当相邻位置R 2和R 3一起形成二价基团时; R 4和R 5各自独立地为氢，Ar 1，C 1-6烷基，C 1-6烷氧基-C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基（O）C 1-6烷基或C 1-6烷基S（O）2 -C 1-6烷基; R 6和R 7各自独立地为氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基或Ar 2氧基; R 8是氢，C 1-6烷基，氰基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基C 1-6烷基，氰基C 1-6烷基，C 1-6烷氧基羰基C 1-6烷基，羟基羰基-C 1-6烷基，羟基C 1-6烷基，氨基C 1-6烷基，单 - 或二（C 1-6烷基）氨基C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基-C 1-6烷基，氨基羰基C 1-6烷基，Ar 1，Ar 2 C 1-6烷氧基C 1-6烷基，C 1-6烷硫基C 1-6烷基; R 10是氢，C 1-6烷基或卤素; R 11是氢或C 1-6烷基; 具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

3. 发明申请

WO1997049704A1 N-[4-(HETEROARYLMETHYL)PHENYL]-HETEROARYLAMINES 审中-公开
标题翻译： N- [4-（杂芳基）苯基] -HETEROARYLAMINES
公开(公告)号：WO1997049704A1
公开(公告)日：1997-12-31
申请号：PCT/EP1997003248
申请日：1997-06-19
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston , MABIRE, Dominique, Jean-Pierre , LACRAMPE, Jean, Fernand, Armand , SANZ, Gérard, Charles
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D417/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention is concerned with compounds of formula (I), the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R is hydrogen, hydroxy, C1-6alkyl or aryl; R is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; formula (1) is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.
摘要翻译：本发明涉及式（I）化合物，N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R 2是氢; 任选取代的C 1-12烷基; 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R 3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环; 式（1）是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

4. 发明申请

WO1996020200A1 6-[TRIAZOLYL[3-(TRIFLUOROMETHYL)PHENYL]METHYL]-2-QUINOLINONES AND -QUINOLINETHIONES 审中-公开
标题翻译： 6- [三唑并[3-（三氟甲基）苯基]甲基] -2-喹啉酮和二氢化茚
公开(公告)号：WO1996020200A1
公开(公告)日：1996-07-04
申请号：PCT/EP1995005173
申请日：1995-12-21
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston , MABIRE, Dominique, Jean-Pierre , SANZ, Gérard, Charles
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： This invention is concerned with the compounds of formula (I), the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R is hydrogen, amino or C1-4alkyl; R is hydrogen, halo or C1-4alkyl; R is hydrogen, halo or C1-4alkyl; Y is O or S, and -X = X - is a bivalent radical having the formula: -N = CH- (a-1) or -CH = N- (a-2); compositions containing the same, and processes of preparing these compounds. It further relates to their use as a medicine, in particular their use as a medicine to treat keratinization disorders.
摘要翻译：本发明涉及式（I）化合物，其药学上可接受的酸加成盐及其立体化学异构形式，其中R 1是氢，氨基或C 1-4烷基; R 2是氢，卤素或C 1-4烷基; R 3是氢，卤素或C 1-4烷基; Y是O或S，-X 1 = X 2 - 是具有下式的二价基团：-N = CH-（a-1）或-CH = N-（a-2）; 含有它们的组合物，以及制备这些化合物的方法。它还涉及它们作为药物的用途，特别是它们作为治疗角质化障碍的药物的用途。

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