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1. 发明申请

WO1997030050A1 HETEROCYCLYL-ERGOLINE DERIVATIVES AS 5-HT1A RECEPTOR LIGANDS 审中-公开
标题翻译：作为5-HT1A受体配体的间苯二酚衍生物
公开(公告)号：WO1997030050A1
公开(公告)日：1997-08-21
申请号：PCT/EP1997000582
申请日：1997-02-07
申请人： PHARMACIA & UPJOHN S.P.A. , MANTEGANI, Sergio , BANDIERA, Tiziano , MERONI, Maurizio , VARASI, Mario , CACCIA, Carla
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07D457/04
CPC分类号： C07D457/02 , C07D457/00
摘要： Ergoline derivative having formula (I) wherein R1 is hydrogen atom or C1-4 alkyl group; R2 is hydrogen, chlorine, or bromine atom, methyl or C1-4 alkylthio group; n is 0, 1 or 2; the substituent at position 8 is in alpha or beta configuration; Het represents an aromatic 5-membered heterocyclic ring, said ring having three heteroatoms which are the same or different and which are selected from the group consisting of sulfur, oxygen and nitrogen atom and X is hydrogen, chlorine or bromine or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof are active at the Central Nervous System level. A process for their preparation is also described, as are pharmaceutical compositions containing them.
摘要翻译：式（I）的衍生物，其中R 1是氢原子或C 1-4烷基; R2是氢，氯或溴原子，甲基或C1-4烷硫基; n为0,1或2; 位置8处的取代基是α或β构型; Het表示芳族5元杂环，所述环具有三个相同或不同的杂原子，选自硫，氧和氮原子，X是氢，氯或溴或氟原子，或其药学上可接受的酸加成盐在中枢神经系统水平上是有活性的。还描述了其制备方法，以及含有它们的药物组合物。

2. 发明申请

WO1998000424A1 ANTINEURODEGENERATIVE ERGOLINE DERIVATIVES 审中-公开
标题翻译：过氧化物衍生物衍生物
公开(公告)号：WO1998000424A1
公开(公告)日：1998-01-08
申请号：PCT/EP1997002955
申请日：1997-05-29
申请人： PHARMACIA & UPJOHN S.P.A. , MANTEGANI, Sergio , BRAMBILLA, Enzo , CARFAGNA, Nicola , VARASI, Mario
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07D457/02
CPC分类号： C07D457/10 , A61K31/48 , C07D457/02
摘要： The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) wherein R1 represents a hydrogen atom or a linear or branched C1-C5 alkyl or C2-C5 alkenyl group optionally substituted with a C3-C7 cycloalkyl, a hydroxy group or a R3-substituted phenyl group wherein R3 is a hydroxy or a hydroxymethyl group; R2 represents a hydrogen atom or a linear or branched C1-C5 alkyl or a C2-C5 alkenyl group optionally substituted with a hydroxy group, or a R3-substituted phenyl group wherein R3 is as above defined, or with a C1-C5 alkoxy group; the symbols -- at positions 2,3 and 8, 9 independently denote a single or double chemical bond and Z represents a group (CH2)nOH, wherein n is 0 or an integer from 1 to 3, or a group C(R4)2OH wherein R4 is a C1-C5 alkyl or a phenyl group, or a pharmaceutically acceptable salt thereof. Some compounds of formula (I) are novel. Processes for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：本发明提供了用于治疗神经变性疾病的新用途，其中式（I）的麦角灵衍生物，其中R 1表示氢原子或任选被C 3 -C 7环烷基取代的直链或支链C 1 -C 5烷基或C 2 -C 5烯基，羟基或R 3取代的苯基，其中R 3是羟基或羟甲基; R2表示氢原子或任选被羟基取代的直链或支链C 1 -C 5烷基或C 2 -C 5烯基，或其中R 3如上所定义的R 3取代苯基，或与C 1 -C 5烷氧基 ; 符号 - 位置2,3和8,9独立地表示单一或双重化学键，Z表示基团（CH 2）n OH，其中n为0或1至3的整数，或基团C（R 4）其中R 4是C 1 -C 5烷基或苯基，或其药学上可接受的盐。一些式（I）化合物是新的。还描述了其制备方法和含有它们的药物组合物。

3. 发明申请

WO1997049433A1 FLUORO LABELLED ANTHRACYCLINONE AND ANTHRACYCLINE DERIVATIVES 审中-公开
标题翻译：荧光标记的蒽醌和蒽醌衍生物
公开(公告)号：WO1997049433A1
公开(公告)日：1997-12-31
申请号：PCT/EP1997003234
申请日：1997-06-18
申请人： PHARMACIA & UPJOHN S.P.A. , BANDIERA, Tiziano , FANCELLI, Daniele , CARUSO, Michele , LANSEN, Jacqueline , SUARATO, Antonino
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： A61K49/00
CPC分类号： C07D295/185 , A61K49/06 , C07C225/24 , C07C2603/44 , C07D295/112 , C07D295/26 , C07H15/252
摘要： Compounds of formula (A), wherein R1, R2, R3, Y and Z are organic substituents, are useful in the diagnosis of amyloidosis; some of the compounds of formula (A) are novel. Processes for their preparation, and pharmaceutical compositions containing them are also described.
摘要翻译：其中R1，R2，R3，Y和Z为有机取代基的式（A）化合物可用于淀粉样变性的诊断; 一些式（A）的化合物是新的。还描述了它们的制备方法和含有它们的药物组合物。

4. 发明申请

WO1998009938A1 N-SUBSTITUTED-2-AMINO-4-PHENYL-4-OXO-BUTANOIC ACID DERIVATIVES WITH KYNURENINE-3-HYDROXYLASE INHIBITORY ACTIVITY 审中-公开
标题翻译： N-取代-2-氨基-4-苯基-4-氧代 - 丁酸衍生物与奎宁尼-3-羟基酶抑制活性
公开(公告)号：WO1998009938A1
公开(公告)日：1998-03-12
申请号：PCT/EP1997004271
申请日：1997-07-31
申请人： PHARMACIA & UPJOHN S.P.A. , VARASI, Mario , GIORDANI, Antonio , CINI, Massimo , SPECIALE, Carmela , BIANCHETTI, Alberto
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07C229/36
CPC分类号： C07C233/47 , C07C311/06
摘要： N-substituted-2-amino-4-phenyl-4-oxo-butanoic acid compound of formula (I), wherein each of the groups X and Y is, independently, hydrogen; halogen; nitro; C1-C6 alkyl; C2-C4 alkenyl; C2-C4 alkynyl; C1-C6 alkoxy; C1-C6 alkylthio; SOR2 or SO2R2 in which R2 is C1-C6 alkyl, phenyl or benzyl; or SO2N(R3)2 in which each of the groups R3 is, independently, hydrogen, C1-C6 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, phenyl or benzyl; R is hydroxy, -OR5 in which R5 is C1-C6 alkyl, C2-C4 alkenyl, C2-C4 alkynyl or benzyl; -N(R3)2 or -N(R3)OR3 in which each of R3 is as defined above; W is -COOR4, -COR4 or -SO2R4 in which R4 is C1-C6 alkyl, an optionally substituted C2-C4 alkenyl, an optionally substituted phenyl or benzyl; -CONHR5 or -CSNHR5 in which R5 is as defined above; trichloroacetyl; or trifluoroacetyl; or a pharmaceutically acceptable salts thereof, for use as a medicament, in particular as Kynurenine 3-hydroxylase inhibitor is disclosed.
摘要翻译：式（I）的N-取代-2-氨基-4-苯基-4-氧代 - 丁酸化合物，其中基团X和Y各自独立地为氢; 卤素; 硝基; C1-C6烷基; C 2 -C 4烯基; C2-C4炔基; C1-C6烷氧基; C1-C6烷硫基; SOR2或SO2R2，其中R2是C1-C6烷基，苯基或苄基; 或SO 2 N（R 3）2，其中基团R 3各自独立地为氢，C 1 -C 6烷基，C 2 -C 4烯基，C 2 -C 4炔基，苯基或苄基; R是羟基，-OR 5，其中R 5是C 1 -C 6烷基，C 2 -C 4烯基，C 2 -C 4炔基或苄基; -N（R3）2或-N（R3）OR3，其中R3各自如上所定义; W是-COOR 4，-COR 4或-SO 2 R 4，其中R 4是C 1 -C 6烷基，任选取代的C 2 -C 4烯基，任选取代的苯基或苄基; -CONHR 5或-CSNHR 5，其中R 5如上所定义; 三氯; 或三氟乙酰基; 或其药学上可接受的盐，用作药物，特别是Kynurenine 3-羟化酶抑制剂。

5. 发明申请

WO1998003469A1 BENZOYLPROPIONIC ACID ESTER DERIVATIVES 审中-公开
标题翻译：苯甲酰丙酸酯衍生物
公开(公告)号：WO1998003469A1
公开(公告)日：1998-01-29
申请号：PCT/EP1997003588
申请日：1997-07-03
申请人： PHARMACIA & UPJOHN S.P.A. , VARASI, Mario , GIORDANI, Antonio , CINI, Massimo , SPECIALE, Carmela , BIANCHETTI, Alberto
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07C229/36
CPC分类号： C07C229/36
摘要： Benzoylpropionic acid ester derivatives of formula (I) wherein R is C1-C4 alkyl or benzyl, and the pharmaceutically acceptable salts thereof, which act as kynurenine-3-hydroxylase enzyme inhibitors and are useful in the treatment of neurodegenerative diseases. A process for preparing compounds of formula (I) and pharmaceutical compositions comprising them are also described.
摘要翻译：其中R为C 1 -C 4烷基或苄基的式（I）的苯甲酰基丙酸酯衍生物及其药学上可接受的盐，其用作犬奈因宁-3-羟化酶抑制剂，可用于治疗神经变性疾病。还描述了制备式（I）化合物的方法和包含它们的药物组合物。

6. 发明申请

WO1997005111A1 N-(4-SUBSTITUTED-BENZYL)-2-AMINOLACTAM DERIVATIVES 审中-公开
标题翻译： N-（4-取代苄基）-2-氨基甲酰胺衍生物
公开(公告)号：WO1997005111A1
公开(公告)日：1997-02-13
申请号：PCT/EP1996002962
申请日：1996-07-05
申请人： PHARMACIA & UPJOHN S.P.A. , PEVARELLO, Paolo , AMICI, Raffaella , VARASI, Mario , MAJ, Roberto , SALVATI, Patricia
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07D211/74
CPC分类号： C07D207/273 , C07D205/085 , C07D211/76
摘要： Novel N-(4-substituted-benzyl)-2-aminolactams compounds, having antiepileptic, anti-Parkinson, neuroprotective, anti-depressant, antispastic and/or hypnotic activity, of general formula (I) wherein: m is zero, 1, 2 or 3; n is zero, 1, 2 or 3; X is -O-, -S-, -CH2- or -NH-; each of R and R1 independently is hydrogen, C1-C6 alkyl, halogen, hydroxy, C1-C4 alkoxy or trifluoromethyl; each of R2, R3 and R4 independently is hydrogen, C1-C6 alkyl optionally substituted by a hydroxy group, or C3-C7 cycloalkyl; and the pharmaceutically acceptable salts thereof, are disclosed.
摘要翻译：具有通式（I）的具有抗癫痫，抗帕金森综合征，神经保护作用，抗抑郁药，抗痉挛和/或催眠活性的新型N-（4-取代 - 苄基）-2-氨基内酰胺化合物，其中：m为0,1， 2或3; n为零，1,2或3; X是-O - ， - S - ， - CH 2 - 或-NH-; R和R 1各自独立地为氢，C 1 -C 6烷基，卤素，羟基，C 1 -C 4烷氧基或三氟甲基; R 2，R 3和R 4各自独立地为氢，任选被羟基取代的C 1 -C 6烷基或C 3 -C 7环烷基; 及其药学上可接受的盐。

7. 发明申请

WO1997017317A1 4-PHENYL-4-OXO-BUTANOIC ACID DERIVATIVES WITH KYNURENINE-3-HYDROXYLASE INHIBITING ACTIVITY 审中-公开
标题翻译：邻苯二酚-3-羟基酶抑制活性的4-苯基-4-氧代 - 丁酸衍生物
公开(公告)号：WO1997017317A1
公开(公告)日：1997-05-15
申请号：PCT/EP1996004518
申请日：1996-10-16
申请人： PHARMACIA & UPJOHN S.P.A. , GIORDANI, Antonio , PEVARELLO, Paolo , SPECIALE, Carmela , VARASI, Mario
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07C59/90
CPC分类号： C07C59/90 , C07C69/738 , C07C205/56
摘要： 4-phenyl-4-oxo-butanoic acid derivatives for use in the treatment of the human or animal body by therepy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enyzme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butanoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.
摘要翻译： 4-苯基-4-氧代 - 丁酸衍生物，用于通过该药物治疗人体或动物体; 特别是作为犬尿氨酸-3-羟化酶抑制剂，在预防和/或治疗需要抑制这种乙烯的神经变性疾病中。本发明还包括所选类别的上述4-苯基-4-氧代 - 丁酸衍生物，其药学上可接受的盐，其制备方法和含有它们的药物组合物。

8. 发明申请

WO1997017316A1 4-PHENYL-4-OXO-2-BUTENOIC ACID DERIVATIVES WITH KYNURENINE-3-HYDROXYLASE INHIBITING ACTIVITY 审中-公开
标题翻译： 4-苯基-4-氧代-2-丁酮酸衍生物与奎宁宁-3-羟基酶抑制活性
公开(公告)号：WO1997017316A1
公开(公告)日：1997-05-15
申请号：PCT/EP1996004517
申请日：1996-10-16
申请人： PHARMACIA & UPJOHN S.P.A. , GIORDANI, Antonio , PEVARELLO, Paolo , SPECIALE, Carmela , VARASI, Mario
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07C59/88
CPC分类号： C07C205/56 , C07C59/88 , C07C69/738
摘要： 4-Phenyl-4-oxo-butenoic acid derivatives for use in the treatment of the human or animal body by therapy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enzyme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butenoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.
摘要翻译： 4-苯基-4-氧代 - 丁烯酸衍生物，用于治疗人体或动物体; 特别是作为犬尿氨酸-3-羟化酶抑制剂，在预防和/或治疗需要抑制这种酶的神经变性疾病中。本发明还包括所选类别的上述4-苯基-4-氧代 - 丁烯酸衍生物，其药学上可接受的盐，其制备方法和含有它们的药物组合物。

9. 发明申请

WO1997015550A1 FLUORO-SUBSTITUTED BENZOYLPROPIONIC ACID DERIVATIVES 审中-公开
标题翻译：氟取代苯甲酰丙酸衍生物
公开(公告)号：WO1997015550A1
公开(公告)日：1997-05-01
申请号：PCT/EP1996004321
申请日：1996-10-04
申请人： PHARMACIA & UPJOHN S.P.A. , VARASI, Mario , GIORDANI, Antonio , SPECIALE, Carmela , CINI, Massimo , BIANCHETTI, Alberto
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07C229/36
CPC分类号： C07C259/06 , C07C229/36 , C07C237/20
摘要： A fluoro-substituted benzoyl propionic acid derivative of formula (I) either as single isomer or as mixture of isomers, wherein R is hydroxy, amino, hydroxylamine, -OR', -NHR', N(R')2 or -NHOR' in which R' is C1-C6 alkyl or benzyl, or a pharmaceutically acceptable salt thereof, which act as kynurenine-3-hydroxylase enzyme inhibitor and can be useful in the treatment of neurodegenerative diseases. A process for preparing compounds of formula (I) and pharmaceutical compositions comprising them are also described.
摘要翻译：式（I）的氟取代的苯甲酰基丙酸衍生物作为单一异构体或异构体混合物，其中R是羟基，氨基，羟胺，-OR'，-NHR'，N（R'）2或-NHOR' 其中R'为C1-C6烷基或苄基，或其药学上可接受的盐，其用作kynurenine-3-羟化酶抑制剂，并且可用于治疗神经变性疾病。还描述了制备式（I）化合物的方法和包含它们的药物组合物。

10. 发明申请

WO1997005102A1 2-(4-SUBSTITUTED)-BENZYLAMINO-2-METHYL-PROPANAMIDE DERIVATIVES 审中-公开
标题翻译： 2-（4-取代的） - 苯甲酰胺-2-甲基丙酰胺衍生物
公开(公告)号：WO1997005102A1
公开(公告)日：1997-02-13
申请号：PCT/EP1996002961
申请日：1996-07-05
申请人： PHARMACIA & UPJOHN S.P.A. , PEVARELLO, Paolo , AMICI, Raffaella , VARASI, Mario , BONSIGNORI, Alberto , SALVATI, Patricia
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07C237/06
CPC分类号： C07C237/06 , C07C323/36
摘要： Novel 2-(4-substituted)-benzylamino-2-methyl-propanamides compounds, having CNS activity, of general formula (I) wherein: n is zero, 1, 2 or 3; X is -O-, -S-, -CH2- or -NH-; each of R and R1 independently is hydrogen, C1-C6 alkyl, halogen, hydroxy, C1-C4 alkoxy or trifluoromethyl; each of R2, R3 and R4 independently is hydrogen, C1-C6 alkyl or C3-C7 cycloalkyl; and the pharmaceutically acceptable salts thereof, are disclosed.
摘要翻译：具有通式（I）的CNS活性的新的2-（4-取代） - 苄基氨基-2-甲基 - 丙酰胺化合物，其中：n为0,1,2或3; X是-O - ， - S - ， - CH 2 - 或-NH-; R和R 1各自独立地为氢，C 1 -C 6烷基，卤素，羟基，C 1 -C 4烷氧基或三氟甲基; R2，R3和R4各自独立地为氢，C1-C6烷基或C3-C7环烷基; 及其药学上可接受的盐。

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