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1. 发明申请

WO1993014088A1 ANTIHISTAMINIC PIPERAZINYL DERIVATIVES 审中-公开
标题翻译：抗生素哌嗪衍生物
公开(公告)号：WO1993014088A1
公开(公告)日：1993-07-22
申请号：PCT/EP1992003000
申请日：1992-12-29
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , LEENAERTS, Joseph, Elisabeth , DIELS, Gaston, Stanislas, Marcella , SOMMEN, François, Maria
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D405/06
CPC分类号： C07D405/04 , C07D405/06 , C07D405/14 , C07D413/06 , C07D413/14 , C07D471/04 , C07D513/04
摘要： Antihistaminic piperazinyl derivatives having formula (I) wherein R is (hydroxyC1-6alkyl)furanyl, (C1-6alkyl)oxazolyl or (hydroxyC1-6alkyl)oxazolyl; -A =A -A =A - is a bivalent radical having the formula -CH=CH-CH=CH- (a-1), -N=CH-CH=CH- (a-2), -CH=N-CH=CH- (a-3), -CH=CH-N=CH- (a-4), -CH=CH-CH=N- (a-5), -N=CH-N=CH- (a-6) or -CH=N-CH=N- (a-7); m is 1, 2, 3 or 4; L is hydrogen; C1-12alkyl; C3-6cycloalkyl; C3-6alkenyl optionally substituted with aryl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; arylcarbonyl; arylC1-6alkyloxycarbonyl; or a radical of formula: -Alk-R (b-1); -Alk-Y-R (b-2); -Alk-Z -C(=X)-Z -R (b-3); or -CH2-CHOH-CH2-O-R (b-4). Process for preparing the same, compositions containing said antihistaminic derivatives and a method of treating allergic diseases.
摘要翻译：式（I）的抗组胺哌嗪衍生物，其中R 1为（羟基C 1-6烷基）呋喃基，（C 1-6烷基）恶唑基或（羟基C 1-6烷基）恶唑基; -A 1 = A 2 -A 3 3 = A 4是具有式-CH = CH-CH = CH-（a-1），-N = CH-CH = CH-（a-2），-CH = N-CH = CH-（a-3），-CH = CH-N = CH-（a-4），-CH = CH-CH = 5），-N = CH-N = CH-（a-6）或-CH = N-CH = N-（a-7）; m为1,2,3或4; L是氢; C1-12烷基; 3-6环; 任选被芳基取代的C 3-6烯基; C1-6烷基; C1-6alkyloxycarbonyl; 基羰基; arylC1-6alkyloxycarbonyl; 或式-Alk-R 3（b-1）的基团; -Alk-Y-R 4（b-2）; -Alk-Z 1 -C（= X）-Z 2 -R 5（b-3）; 或-CH 2 -CHOH-CH 2 -O-R 6（b-4）。制备该组合物的方法，含有所述抗组胺衍生物的组合物和治疗过敏性疾病的方法。

2. 发明申请

WO1992006086A1 NOVEL 4-PIPERIDINYLCARBONYL DERIVATIVES 审中-公开
标题翻译：新型4-哌啶子基衍生物
公开(公告)号：WO1992006086A1
公开(公告)日：1992-04-16
申请号：PCT/EP1991001782
申请日：1991-09-17
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , DIELS, Gaston, Stanislas, Marcella , SOMMEN, François, Maria
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D473/08 , C07D513/04
摘要： 4-piperidinylcarbonyl derivatives having formula (I), wherein -A =A -A =A - is a bivalent radical having the formula -CH=CH-CH=CH- (a-1), -N=CH-CH=CH- (a-2), -CH=N-CH=CH- (a-3), -CH=CH-N=CH- (a-4), -CH=CH-CH=N- (a-5), -N=CH-N=CH- (a-6) or -CH=N-CH=N- (a-7); R is aryl or a radical of formula -D-R wherein D is O or S; R is C1-6alkyl optionally substituted with hydroxy, C1-6alkyloxy, carboxyl or C1-6alkyloxy-carbonyl; m is 1, 2, 3 or 4; n is 0, 1 or 2; L is hydrogen; C1-12alkyl; C3-6cycloalkyl; C3-6alkenyl optionally substituted with aryl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; arylcarbonyl; arylC1-6alkyloxycarbonyl; -Alk-R (b-1); -Alk-Y-R (b-2); -Alk-Z -C(=X)-Z -R (b-3); -CH2-CHOH-CH2-O-R (b-4) or -Alk-CHOH-R (b-5); wherein Alk is C1-6alkanediyl; R is cyano, aryl or Het; R and R are hydrogen, aryl, Het or C1-6alkyl optionally substituted with aryl or Het; R is aryl or naphthalenyl; R is aryl; Y is O, S, NR ; said R being hydrogen, C1-6alkyl or C1-6alkylcarbonyl; Z and Z independently are O, S, NR or a direct bond; R being hydrogen or C1-6alkyl; X is O, S or NR ; said R being hydrogen, C1-6alkyl or cyano; provided that when -A =A -A =A - is a radical of formula (a-1) and R is phenyl optionally substituted with C1-6alkyl, C1-6alkyloxy, halo or hydroxy; then L is other than hydrogen, C1-6alkyloxycarbonyl or other than a radical of formula -Alk-R (b-1), -Alk-O-R (b-2-a), -Alk-C(=O)-R (b-3-a) or -Alk-CHOH-R (b-5) wherein R , R , R and R are phenyl optionally substituted with halo, hydroxy, C1-6alkyl, C1-6alkyloxy, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof having antihistaminic properties, compositions containing the same and methods of treating warm-blooded animals suffering from allergic diseases.
摘要翻译：具有式（I）的4-哌啶基羰基衍生物，其中-A 1 = A 2 -A 3 = A 4 - 是式-CH = CH-CH = CH-的二价基团（a -1），-N = CH-CH = CH-（a-2），-CH = N-CH = CH-（a-3），-CH = CH-N = CH-（a-4） CH = CH-CH = N-（a-5），-N = CH-N = CH-（a-6）或-CH = N-CH = N-（a-7） R 1是芳基1或式-D-R 2的基团，其中D是O或S; R 2是任选被羟基，C 1-6烷氧基，羧基或C 1-6烷氧基 - 羰基取代的C 1-6烷基; m为1,2,3或4; n为0,1或2; L是氢; C1-12烷基; 3-6环; 任选被芳基取代的C 3-6烯基; C1-6烷基; C1-6alkyloxycarbonyl; 基羰基; arylC1-6alkyloxycarbonyl; -Alk-R 3（b-1）; -Alk-Y-R 4（b-2）; -Alk-Z 1 -C（= X）-Z 2 -R 5（b-3）; -CH 2 -CHOH -CH 2 -O-R 6（b-4）或-Alk-CHOH-R 14（b-5）; 其中Alk是C1-6烷二基; R 3是氰基，芳基或Het; R 4和R 5是氢，芳基，Het或任选被芳基或Het取代的C 1-6烷基; R 6是芳基或萘基; R 14是芳基; Y是O，S，NR 7; 所述R 7为氢，C 1-6烷基或C 1-6烷基羰基; Z 1和Z 2独立地是O，S，NR 8或直接键; R 8是氢或C 1-6烷基; X是O，S或NR 9; 所述R 9为氢，C 1-6烷基或氰基; 条件是当-A 1 = A 2 -A 3 3 = A 4 - 是式（a-1）的基团时，R 1是任选被C 1-6烷基取代的苯基，C 1〜 6-烷氧基，卤素或羟基; 那么L不是氢，C 1-6烷氧基羰基或不同于式-Alk-R 3（b-1），-Alk-OR 4（b-2-a），-Alk-C（ = O）-R 5（b-3-a）或-Alk-CHOH-R 14（b-5）其中R 3，R 4，R 5和R 14，任选被卤素，羟基，C 1-6烷基，C 1-6烷氧基，具有抗组氨酸性质的药学上可接受的酸加成盐和立体化学异构体形式，含有该组合物的组合物和治疗患有过敏性疾病的温血动物的方法的苯基。

3. 发明申请

WO1994013680A1 ANTIALLERGIC IMIDAZO[1,2-a](PYRROLO, THIENO OR FURANO)[2,3-d]AZEPINE DERIVATIVES 审中-公开
标题翻译： [1,2-a]（吡咯，三苯或呋喃）[2,3-d]亚胺衍生物
公开(公告)号：WO1994013680A1
公开(公告)日：1994-06-23
申请号：PCT/EP1993003321
申请日：1993-11-25
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , DIELS, Gaston, Stanislas, Marcella , LEENAERTS, Joseph, Elisabeth
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D495/14
CPC分类号： C07D495/14
摘要： Antiallergic imidazo[1,2-a](pyrrolo, thieno or furano)[2,3-d]azepines of formula (I), the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R represents hydrogen, C1-4alkyl, halo, ethenyle substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl, hydroxycarbonyl or hydroxycarbonylC1-4alkyl; R represents hydrogen, C1-4alkyl, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, C1-4alkyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl or hydroxycarbonyl; R represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl, phenyl or halo; X represents O, S or NR ; L represents hydrogen; C1-6alkyl; substituted C1-6alkyl; C3-6alkenyl; C3-6alkenyl substituted with aryl; or a radical of the formula: -Alk-Y-Het (a-1), -Alk-NH-CO-Het (a-2) or Alk-Het (a-3). Compositions comprising said compounds, processes of preparing the same and intermediates in the preparation thereof.
摘要翻译：式（I）的抗过敏咪唑并[1,2-a]（吡咯并噻吩并或呋喃）[2,3-d]吖庚因，其药学上可接受的加成盐和立体化学异构形式，其中每条虚线独立地表示可选债券; R 1表示氢，C 1-4烷基，卤素，被羟基羰基或C 1-4烷氧基羰基取代的亚乙烯基，羟基C 1-4烷基，甲酰基，羟基羰基或羟基羰基C 1-4烷基; R 2表示氢，C 1-4烷基，被羟基羰基或C 1-4烷氧基羰基取代的乙烯基，被羟基羰基或C 1-4烷氧基羰基取代的C 1-4烷基，羟基C 1-4烷基，甲酰基或羟基羰基; R 3表示氢，C 1-4烷基，羟基C 1-4烷基，苯基或卤素; X表示O，S或NR 4; L表示氢; C1-6烷基; 取代的C 1-6烷基; C3-6alkenyl; 被芳基取代的C 3-6烯基; 或下式的基团：-Alk-Y-Het 1（a-1），-Alk-NH-CO-Het 2（a-2）或Alk-Het 3（a-3）。包含所述化合物的组合物，其制备方法及其制备中的中间体。

4. 发明申请

WO1992022553A1 IMIDAZO[1,2-a](PYRROLO, THIENO OR FURANO)[3,2-d]AZEPINE DERIVATIVES, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：咪唑（1,2-A）（吡咯烷，三苯或呋喃）（3,2-D）亚胺衍生物，组合物和使用方法
公开(公告)号：WO1992022553A1
公开(公告)日：1992-12-23
申请号：PCT/EP1992001331
申请日：1992-06-09
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , DIELS, Gaston, Stanislas, Marcella , LEENAERTS, Joseph, Elisabeth , COOYMANS, Ludwig, Paul
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D487/14
CPC分类号： C07D487/14 , C07D491/14 , C07D495/14
摘要： The present invention is concerned with novel imidazo[1,2-a](pyrrolo, thieno or furano)[3,2-d]azepines of formula (I), the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R1 represents hydrogen, C¿1-4?alkyl, halo, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl, hydroxycarbonyl or hydroxycarbonylC1-4alkyl; R?2¿ represents hydrogen, C¿1-4?alkyl, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, C1-4alkyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl or hydroxycarbonyl; R?3¿ represents hydrogen, C¿1-4?alkyl, hydroxyC1-4alkyl, phenyl or halo; L represents hydrogen; C1-6alkyl; C1-6alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C1-4alkyloxy, hydroxycarbonyl, C1-4alkyloxycarbonyl, C1-4alkyloxycarbonylC1-4alkyloxy, hydroxycarbonylC1-4alkyloxy, C1-4alkyloxycarbonylamino, C1-4alkylaminocarbonyl, C1-4alkylaminocarbonylamino, C1-4alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C1-6alkyl substituted with both hydroxy and aryloxy; C3-6alkenyl; C3-6alkenyl substituted with aryl; L represents a radical of formula -Alk-Y-Het?1¿ (a-1), -Alk-NH-CO-Het2 (a-2) or -Alk-Het3 (a-3); which are useful antiallergic compounds. Compositions comprising said compounds, methods of using, and processes for preparing the same.

5. 发明申请

WO1992022551A1 IMIDAZO[2,1-b][3]BENZAZEPINE DERIVATIVES, COMPOSITIONS AND METHOD OF USE 审中-公开
标题翻译：咪唑（2,1-B）（3）苯并噻吩衍生物，组合物和使用方法
公开(公告)号：WO1992022551A1
公开(公告)日：1992-12-23
申请号：PCT/EP1992001330
申请日：1992-06-09
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , DIELS, Gaston, Stanislas, Marcella , LEENAERTS, Joseph, Elisabeth
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention is concerned with novel imidazo[2,1-b][3]benzazepines of formula (I), the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R1 represents hydrogen, halo, C¿1-4?alkyl or C1-4alkyloxy; R?2¿ represents hydrogen, halo, C¿1-4?alkyl or C1-4alkyloxy; R?3¿ represents hydrogen, C¿1-4?alkyl, ethenyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, C1-4alkyl substituted with hydroxycarbonyl or C1-4alkyloxycarbonyl, hydroxyC1-4alkyl, formyl or hydroxycarbonyl; R?4¿ represents hydrogen, C¿1-4?alkyl, hydroxyC1-4alkyl, phenyl or halo; R?5¿ represents hydrogen, C¿1-4?alkyl or halo; L represents hydrogen; C1-6alkyl; C1-6alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C1-4alkyloxy, hydroxycarbonyl, C1-4alkyloxycarbonyl, C1-4alkyloxycarbonyl-C1-4alkyloxy, hydroxycarbonylC1-4alkyloxy, C1-4alkyloxycarbonylamino, C1-4alkylaminocarbonyl, C1-4alkylaminocarbonylamino, C1-4alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C1-6alkyl substituted with both hydroxy and aryloxy; C3-6alkenyl; C3-6alkenyl substituted with aryl; or, L represents a radical of formula -Alk-Y-Het?1¿ (a-1), -Alk-NH-CO-Het2 (a-2) or -Alk-Het3 (a-3); provided that 6,11-dihydro-11-(4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine is excluded, which are useful antiallergic compounds. Compositions comprising said compounds, methods of using and processes for preparing the same.

6. 发明申请

WO1997034897A1 FUSED IMIDAZOLE DERIVATIVES AS MULTIDRUG RESISTANCE MODULATORS 审中-公开
标题翻译：作为多电阻电阻调节剂的熔融咪唑衍生物
公开(公告)号：WO1997034897A1
公开(公告)日：1997-09-25
申请号：PCT/EP1997001264
申请日：1997-03-11
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , LEENAERTS, Joseph, Elisabeth , SOMMEN, François, Maria , SURLERAUX, Dominique, Louis, Nestor, Ghislaine
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D487/04
CPC分类号： C07D487/14 , C07D471/04 , C07D487/04 , C07D495/14
摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula -X-COOR , -X-CONR R or -X-COR wherein -X- is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R and R each independently are hydrogen or C1-4alkyl; R is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R is hydrogen, C1-4alkyl or C1-4alkyloxy; R is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is -CH2-, -CH2-CH2-, -CH=CH-, -CHOH-CH2-, -O-CH2-, -C(=O)-CH2- or -C(=NOH)-CH2-; -A-B- is a bivalent radical; A is a direct bond, optionally substituted C1-6alkanediyl, C1-6alkanediyl-oxy-C1-6alkanediyl, carbonyl, C1-6alkanediylcarbonyl, optionally substituted C1-6alkanediyloxy; A is a direct bond or C1-6alkanediyl; and Q is aryl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for inhibiting or reversing the effects of multidrug resistance.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中虚线是任选的键; n为1或2; R 1是氢; 光环; 甲酰基; 任选被羟基，C 1-4烷氧基，C 1-4烷基羰基氧基，咪唑基，噻唑基或恶唑基取代的C 1-4烷基; 或式-X-COOR 5，-X-CONR 6 R 7或-X-COR 10基团，其中-X-是直接键，C 1-4烷二基或C 2-6亚烯基; R 5是氢，C 1-12烷基，Ar，Het，被C 1-4烷氧基，芳基或杂芳基取代的C 1-6烷基; R 6和R 7各自独立地为氢或C 1-4烷基; R 2是氢，卤素，C 1-4烷基，羟基C 1-4烷基，C 1-4烷氧基羰基，羧基，甲酰基或苯基; R 3是氢，C 1-4烷基或C 1-4烷氧基; R 4是氢，卤素，C 1-4烷基，C 1-4烷氧基或卤代C 1-4烷基; Z是-CH 2 - ， - CH 2 -CH 2 - ， - CH = CH-，-CHOH-CH 2 - ， - O-CH 2 - ， - C（= O）-CH 2 - 或-C（= NOH） -A-B-是二价基团; A 1是直接键，任选取代的C 1-6烷二基，C 1-6烷二基 - 氧基-C 1-6烷二基，羰基，C 1-6烷二基羰基，任选取代的C 1-6烷二基氧基; A 2是直接键或C 1-6烷二基; Q为芳基。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于抑制或逆转多药耐药性的作用。

7. 发明申请

WO1997024350A1 N-ACYL-2-SUBSTITUTED-4-(BENZIMIDAZOLYL- OR IMIDAZOPYRIDINYL-SUBSTITUTED RESIDUES)-PIPERIDINES AS TACHYKININ ANTAGONISTS 审中-公开
标题翻译： N-取代-2-取代的4-（苄基咪唑并 - 咪唑并噻吩并 - 取代的残基） - 哌啶作为TACHYKININ ANTAGONISTS
公开(公告)号：WO1997024350A1
公开(公告)日：1997-07-10
申请号：PCT/EP1996005877
申请日：1996-12-20
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , SURLERRAUX, Dominique, Louis, Nestor, Ghislaine , LEENAERTS, Joseph, Elisabeth
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/14
CPC分类号： C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; X is a covalent bond or a bivalent radical of formula -O-, -S-, -NR -; =Q is =O or =NR ; R is Ar , Ar C1-6alkyl or di(Ar )C1-6alkyl wherein the C1-6alkyl group is optionally substituted; R is Ar , Ar C1-6alkyl, Het or HetC1-6alkyl; L is a benzimidazole or imidazopyridine derivative of formula (A) or (B); Ar is optionally substituted phenyl; Ar is naphtalenyl or optionally substituted phenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; 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，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n为0,1或2; m为1或2，条件是如果m为2，则n为1; X是共价键或式-O-，-S-，-NR 3 - 的二价基团; = Q是= O或= NR 3; R 1是Ar 1，Ar 1 C 1-6烷基或其中C 1-6烷基任选被取代的二（Ar 1）C 1-6烷基; R 2是Ar 2，Ar 2 C 1-6烷基，Het或Het C 1-6烷基; L是式（A）或（B）的苯并咪唑或咪唑并吡啶衍生物; Ar 1是任选取代的苯基; Ar 2是萘基或任选取代的苯基; Het是任选取代的单环或双环杂环; 作为P物质拮抗剂; 其制剂，含有它们的组合物及其作为药物的用途。

8. 发明申请

WO1997016440A1 1-(1,2-DISUBSTITUTED PIPERIDINYL)-4-SUBSTITUTED PIPERAZINE DERIVATIVES 审中-公开
标题翻译： 1-（1,2-取代的哌啶子基）-4-取代的哌嗪衍生物
公开(公告)号：WO1997016440A1
公开(公告)日：1997-05-09
申请号：PCT/EP1996004660
申请日：1996-10-25
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , SURLERAUX, Dominique, Louis, Nestor, Ghislaine , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/04
CPC分类号： C07D401/12 , C07D211/58 , C07D405/12 , C07D413/14 , C07D417/12 , C07D471/04 , Y02P20/55
摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 1 or 2; =Q is =O or =NR ; X is a covalent bond or a bivalent radical of formula -O-, -S-, -NR -; R is Ar , Ar C1-6alkyl or di(Ar )C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent; R is Ar , Ar C1-6alkyl, Het or Het C1-6alkyl; R is hydrogen or C1-6alkyl; L is hydrogen; Ar ; C1-6alkyl; C1-6alkyl substituted with 1 or 2 substituents selected from hydroxy, C1-6alkyloxy, Ar , Ar C1-6alkyloxy and Het ; C3-6alkenyl; Ar C3-6alkenyl; di(Ar )C3-6alkenyl or a radical of formula (a-1), (a-2), (a-3), (a-4) or (a-5); Ar , Ar and Ar are each phenyl or substituted phenyl; Het and Het are each monocyclic or a bicyclic heterocycle; as substance-P antagonists; 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，N-氧化物形式，其药学上可接受的加成盐和立体异构形式，其中n为0,1或2; m为1或2，条件是如果m为2，则n为1; p为1或2; = Q是= O或= NR 3; X是共价键或式-O-，-S-，-NR 3 - 的二价基团; R 1是Ar 1，Ar 1 C 1-6烷基或二（Ar 1）C 1-6烷基，其中每个C 1-6烷基任选地被羟基，C 1-4烷氧基，氧代或缩酮化的氧代取代基; R 2是Ar 2，Ar 2 C 1-6烷基，Het 1或Het 1 C 1-6烷基; R 3为氢或C 1-6烷基; L是氢; 的Ar <3>; C1-6烷基; 被1或2个选自羟基，C 1-6烷氧基，Ar 3，Ar 3 C 1-6烷氧基和Het 2的取代基取代的C 1-6烷基; C3-6alkenyl; 的Ar <3> C3-6alkenyl; （a-1），（a-2），（a-3），（a-4）或（a-5）的基团。 Ar 1，Ar 2和Ar 3各自为苯基或取代的苯基; Het 1和Het 2均为单环或双环杂环; 作为物质-P拮抗剂; 其制剂，含有它们的组合物及其作为药物的用途。

9. 发明申请

WO1997024324A1 1-(1,2-DISUBSTITUTED PIPERIDINYL)-4-SUBSTITUTED PIPERIDINE DERIVATIVES AS TACHYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为TACHYKININ受体拮抗剂的1-（1,2-取代的哌啶子基）-4-取代的哌啶衍生物
公开(公告)号：WO1997024324A1
公开(公告)日：1997-07-10
申请号：PCT/EP1996005883
申请日：1996-12-20
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , SURLERAUX, Dominique, Louis, Nestor, Ghislaine , VAN ROOSBROECK, Yves, Emiel, Maria
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D211/44
CPC分类号： C07D401/06 , C07D211/44 , C07D211/46 , C07D211/52 , C07D211/58 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/10 , C07D491/10
摘要： The present invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 0, 1 or 2; =Q is =O or =NR ; X is a covalent bond or a bivalent radical of formula -O-, -S-, -NR -; R is Ar ; Ar C1-6alkyl or di(Ar )C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent of formula -O-CH2-CH2-O- or -O-CH2-CH2-CH2-O-; R is Ar ; Ar C1-6alkyl; Het or HetC1-6alkyl; R is hydrogen or C1-6alkyl; R is hydrogen; C1-4alkyl; C1-4alkyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4alkyloxycarbonyl or Ar ; R is hydrogen; hydroxy; Ar ; Ar C1-6alkyloxy; di(Ar )C1-6alkyloxy; Ar C1-6alkylthio; di(Ar )C1-6alkylthio; Ar C1-6alkylsulfoxy; di(Ar )C1-6alkylsulfoxy; Ar C1-6alkylsulfonyl; di(Ar )C1-6alkylsufonyl; -NR R ; C1-6alkyl substituted with -NR R ; or a radical of formula (a-1) or (a-2); R and R may also be taken together; R is hydrogen; hydroxy; C1-6alkyloxy; C1-6alkyl or Ar C1-6alkyl; Ar , Ar and Ar are phenyl or substituted phenyl; Ar is also naphthalenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medecine.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n为0,1或2; m为1或2，条件是如果m为2，则n为1; p为0,1或2; = Q是= O或= NR 3; X是共价键或式-O-，-S-，-NR 3 - 的二价基团; R 1是Ar 1; Ar 1 -C 1-6烷基或二（Ar 1）C 1-6烷基，其中每个C 1-6烷基任选被羟基，C 1-4烷氧基，氧代或式-O-CH 2 -CH 2 - O-或-O-CH 2 -CH 2 -CH 2 -O-; R 2是Ar 2; 的Ar <2> C 1-6烷基; Het或HetC 1-6烷基; R 3是氢或C 1-6烷基; R 4是氢; C 1-4烷基; C1-4alkyloxyC1-4alkyl; hydroxyC1-4alkyl; 羧基; C 1-4烷氧基羰基或Ar 3; R 5是氢; 羟基; 的Ar <3>; 的Ar <3> C 1-6烷氧基; 二（AR <3>）C 1-6烷氧基; 的Ar <3> C 1-6烷硫基; 二（AR <3>）C 1-6烷硫基; 的Ar <3> C1-6alkylsulfoxy; 二（AR <3>）C1-6alkylsulfoxy; 的Ar <3> C1-6alkylsulfonyl; 二（AR <3>）C1-6alkylsufonyl; -NR <7> - [R <8>; 被-NR 7 R 8取代的C 1-6烷基; 或式（a-1）或（a-2）的基团; R 4和R 5也可以一起使用; R 6是氢; 羟基; C1-6烷; C 1-6烷基或Ar 3 C 1-6烷基; Ar 1，Ar 2和Ar 3是苯基或取代的苯基; Ar 2也是萘基; Het是任选取代的单环或双环杂环; 作为P物质拮抗剂; 它们的制备，含有它们的组合物及其作为药物的用途。

10. 发明申请

WO1995002600A1 ANTIALLERGIC IMIDAZOAZEPINES 审中-公开
标题翻译： ANTIALLERIC IMIDAZOAZEPINES
公开(公告)号：WO1995002600A1
公开(公告)日：1995-01-26
申请号：PCT/EP1994002287
申请日：1994-07-06
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , LEENAERTS, Joseph, Elisabeth
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D487/04
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , C07D487/14 , C07D491/14 , C07D495/14 , C07D513/04
摘要： The present invention is concerned with novel imidazoazepines of formula (I), the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; -A-B- is a radical of formula -X-CH=CH- (a-1); -CH=CH-X- (a-2); or -CH=CH-CH=CH- (a-3); X represents O, S or NR ; R represents hydrogen or C1-6alkyl; - &cir& NOt - &cir& NOt - &cir& NOt - &cir& NOt Y is a radical of formula =O (b-1); -OH (b-2); or =N-OH (b-3); and L represents hydrogen, C1-4alkylcarbonyl, C1-4alkyloxycarbonyl, phenylcarbonyl, C1-6alkyl or C1-6alkyl substituted with C1-4alkyloxycarbonyl, hydroxycarbonyl, aryl, aryloxy or a radical of formula (c), wherein -D-Z- is -S-CH=CH-, -S-CH2-CH2-, -S-CH2-CH2-CH2-, -CH=CH-CH=CH- or -CH2-CH2-CH2-CH2-; and aryl is phenyl or phenyl substituted with halo, hydroxy or C1-4alkyloxy. Compositions comprising said compounds, processes for preparing the same and the use of these compounds for treating allergic diseases.
摘要翻译：本发明涉及式（I）的新型咪唑并吖庚因，其药学上可接受的加成盐和立体化学异构形式，其中每个虚线独立地表示任选的键; -A-B-是式-X-CH = CH-（a-1）的基团; -CH = CH-X-（a-2）; 或-CH = CH-CH = CH-（a-3）; X表示O，S或NR 1; R 1表示氢或C 1-6烷基; - ＆cir＆NOt - ＆cir＆NOt - ＆cir＆NOt - ＆cir＆NOt Y是公式= O（b-1）的基数; -OH（b-2）; 或= N-OH（b-3）; 并且L表示氢，C 1-4烷基羰基，C 1-4烷氧基羰基，苯基羰基，C 1-6烷基或被C 1-4烷氧基羰基，羟基羰基，芳基，芳氧基或式（c）的基团取代的C 1-6烷基，其中DZ-是-S- CH = CH-，-S-CH2-CH2-，-S-CH2-CH2-CH2-，-CH = CH-CH = CH-或-CH2-CH2-CH2-CH2-; 并且芳基是苯基或被卤素，羟基或C 1-4烷氧基取代的苯基。包含所述化合物的组合物，其制备方法以及这些化合物用于治疗过敏性疾病的用途。

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