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1. 发明申请

WO2010072352A1 1, 2, 4 -OXADIAZOLE DERIVATIVES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译： 1,2,4-吲唑衍生物及其治疗用途
公开(公告)号：WO2010072352A1
公开(公告)日：2010-07-01
申请号：PCT/EP2009/008968
申请日：2009-12-15
申请人： ALMIRALL S.A. , GIULIO MATASSA, Victor , AGUILAR IZQUIERDO, Nuria , MIR CEPEDA, Marta , CARRASCAL RIERA, Marta , FONQUERNA POU, Silvia , CARDUS FIGUERAS, Aranzazu , CASTRO PALOMINO LARIA, Julio, Cesar , ERRA SOLA, Montserrat
发明人： GIULIO MATASSA, Victor , AGUILAR IZQUIERDO, Nuria , MIR CEPEDA, Marta , CARRASCAL RIERA, Marta , FONQUERNA POU, Silvia , CARDUS FIGUERAS, Aranzazu , CASTRO PALOMINO LARIA, Julio, Cesar , ERRA SOLA, Montserrat
IPC分类号： C07D413/04 , C07D413/14 , C07D471/04 , A61K31/4245 , A61P35/00 , A61P29/00 , A61P25/00 , A61P31/00
CPC分类号： C07D413/04 , C07D413/14 , C07D471/04
摘要： New derivatives of general formula (I), or pharmaceutically acceptable salts or N- oxides thereof wherein,either (i) A is selected from the group consisting of -N-, -O- and -S-; B and C are independently selected from the group consisting of -N- and -O-, with the proviso that two of A, B and C are nitrogen atoms, or (ii) two of A, B and C are -N- and one of A, B and C is -NH-; G1 is selected from the group consisting of -CH 2 -, -NH- and -O-; G 2 is selected from the group consisting of -NR 4 - and -O-; R 1 represents: > a 8 to 10 membered bicyclic N-containing heteroaryl group optionally substituted with a C 1-4 carboxyalkyl group or a C 1-4 aminoalkyl group, > a pyridyl group optionally substituted with one or more substituents selected from hydroxy groups, C 1-4 alkyl groups, C 1-4 carboxyalkyl groups, C 1-4 haloalkyl groups, C 1-4 alkoxy groups, amino groups, C 1-4 aminoalkyl groups and C 1-4 aminoalkoxy groups, > a pyridone group substituted with one or more C 1-4 alkyl groups; C 1-4 haloalkyl groups or C 1-4 aminoalkyl groups, or > a group of formula:
摘要翻译：通式（I）的新衍生物或其药学上可接受的盐或N-氧化物，其中（i）A选自-N-，-O-和-S-; B和C独立地选自-N-和-O-，条件是A，B和C中的两个是氮原子，或（ii）A，B和C中的两个是-N和 A，B和C之一是-NH-; G1选自-CH2-，-NH-和-O-; G 2选自-NR 4 - 和-O-; R 1表示：>任选被C 1-4羧基烷基或C 1-4氨基烷基取代的8至10元双环的含N杂芳基，任选被一个或多个选自羟基的取代基取代的吡啶基，C1- 4个烷基，C 1-4羧基烷基，C 1-4卤代烷基，C 1-4烷氧基，氨基，C 1-4氨基烷基和C 1-4氨基烷氧基，>被一个或多个C 1-4烷基取代的吡啶酮基组; C 1-4卤代烷基或C 1-4氨基烷基，或>下式的基团：

2. 发明申请

WO2009021696A1 AZABIPHENYLAMINOBENZOIC ACID DERIVATIVES AS DHODH INHIBITORS 审中-公开
标题翻译：作为DHODH抑制剂的亚氨基苯甲酸苯甲酸衍生物
公开(公告)号：WO2009021696A1
公开(公告)日：2009-02-19
申请号：PCT/EP2008/006573
申请日：2008-08-08
申请人： LABORATORIOS ALMIRALL, S.A. , CASTRO PALOMINO LARIA, Julio, Cesar , TERRICABRAS BELART, Emma , ERRA SOLA, Montserrat , NAVARRO ROMERO, Eloisa , FONQUERNA POU, Silvia , CARDUS FIGUERAS, Aranzazu , LOZOYA TORIBIO, Maria, Estrella
发明人： CASTRO PALOMINO LARIA, Julio, Cesar , TERRICABRAS BELART, Emma , ERRA SOLA, Montserrat , NAVARRO ROMERO, Eloisa , FONQUERNA POU, Silvia , CARDUS FIGUERAS, Aranzazu , LOZOYA TORIBIO, Maria, Estrella
IPC分类号： C07D213/74 , C07D239/42 , C07D401/04 , C07D401/10 , A61K31/44 , A61K31/506 , A61P19/00 , A61P17/00 , A61P35/00 , A61P37/00 , A61P31/00 , C07D413/10
CPC分类号： C07D213/74 , A61K31/44 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D215/38 , C07D239/42 , C07D401/04 , C07D401/10 , C07D413/10
摘要： New azabiphenylaminobenzoic acid derivatives having the chemcial structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).
摘要翻译：公开了具有式（I）化学结构的新的氮杂二苯胺基苯甲酸衍生物; 以及其制备方法，包含它们的药物组合物及其在治疗中作为脱氢山梨醇二氢化酶（DHODH）抑制剂的用途。

3. 发明申请

WO2010081692A1 OXADIAZOLE DERIVATIVES AS SLPL RECEPTOR AGONISTS 审中-公开
标题翻译：作为SLPL受体激动剂的OXADIAZOLE衍生物
公开(公告)号：WO2010081692A1
公开(公告)日：2010-07-22
申请号：PCT/EP2010/000158
申请日：2010-01-14
申请人： ALMIRALL, S.A. , AGUILAR IZQUIERDO, Nuria , CARRASCAL RIERA, Marta , CASTRO PALOMINO LARIA, Julio, Cesar , ERRA SOLA, Montserrat
发明人： AGUILAR IZQUIERDO, Nuria , CARRASCAL RIERA, Marta , CASTRO PALOMINO LARIA, Julio, Cesar , ERRA SOLA, Montserrat
IPC分类号： C07D413/04 , C07D413/14 , A61K31/435 , A61P37/06
CPC分类号： C07D413/04 , C07D413/14
摘要： New compounds having the chemical structure of formula (I) or pharmaceutically acceptable salts or N-oxides thereof wherein A is selected from the group consisting of -N-, -O- and -S-; B and C independently are selected from the group consisting of -N- and -O-, with the proviso that at least two of A, B and C are nitrogen atoms; G 1 is selected from the group consisting of nitrogen atoms and -CR c - groups, wherein R c represents a hydrogen atom, a halogen atom, a C 1-4 alkyl group or a C 1-4 alkoxy group.
摘要翻译：具有式（I）化学结构或其药学上可接受的盐或N-氧化物的新化合物，其中A选自-N-，-O-和-S-; B和C独立地选自-N-和-O-，条件是A，B和C中的至少两个是氮原子; G1选自氮原子和-CRc-基团，其中Rc表示氢原子，卤素原子，C1-4烷基或C1-4烷氧基。

4. 发明申请

WO2011144338A1 PYRAZOLE DERIVATIVES AS S1P1 AGONISTS 审中-公开
标题翻译：作为S1P1激动剂的吡咯衍生物
公开(公告)号：WO2011144338A1
公开(公告)日：2011-11-24
申请号：PCT/EP2011/002487
申请日：2011-05-18
申请人： ALMIRALL, S.A. , ERRA SOLA, Montserrat , AGUILAR IZQUIERDO, Nuria , CARRASCAL RIERA, Marta , TABOADA MARTINEZ, Lorena , NAVARRO ROMERO, Eloisa , VIDAL JUAN, Bernat
发明人： ERRA SOLA, Montserrat , AGUILAR IZQUIERDO, Nuria , CARRASCAL RIERA, Marta , TABOADA MARTINEZ, Lorena , NAVARRO ROMERO, Eloisa , VIDAL JUAN, Bernat
IPC分类号： C07D413/04 , C07D417/04 , A61P37/06 , A61K31/4245 , A61K31/433
CPC分类号： C07D413/04 , C07D417/04
摘要： The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by sphingosine-1-phosphate receptors (S1P1) agonists.
摘要翻译：本发明涉及式（I）化合物，涉及制备这些化合物的方法及其用于治疗易受鞘氨醇-1-磷酸受体（S1P1）激动剂改善的病理状况或疾病。

5. 发明申请

WO2008077639A1 AMINO NICOTINIC AND ISONICOTINIC ACID DERIVATIVES AS DHODH INHIBITORS 审中-公开
标题翻译：氨基酸和异柠檬酸衍生物作为DHODH抑制剂
公开(公告)号：WO2008077639A1
公开(公告)日：2008-07-03
申请号：PCT/EP2007/011401
申请日：2007-12-21
申请人： LABORATORIOS ALMIRALL, S.A. , CASTRO PALOMINO LARIA, Julio Cesar , ERRA SOLA, Montserrat , LOZOYA TORIBIO, Maria Estrella , NAVARRO ROMERO, Eloisa
发明人： CASTRO PALOMINO LARIA, Julio Cesar , ERRA SOLA, Montserrat , LOZOYA TORIBIO, Maria Estrella , NAVARRO ROMERO, Eloisa
IPC分类号： C07D213/79 , C07D213/80 , A61K31/465 , A61P35/00
CPC分类号： C07D213/79 , C07D213/80
摘要： A compound of formula (I) wherein : - one of the groups G 1 represents a nitrogen atom or a group CR c and the other represents a group CR c ; - G 2 represents a nitrogen atom or a group CR d ; - R 1 represents a group selected from hydrogen atoms, halogen atoms, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 3-8 cycloalkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - R 2 represents a group selected from hydrogen atoms, halogen atoms, hydroxyl groups, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 3-8 cycloalkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - R a , R b and R c independently represent groups selected from hydrogen atoms, halogen atoms, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - R d represents a group selected from hydrogen atoms, halogen atoms, hydroxyl groups, C 1-4 alkyl groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, and C 3-8 cycloalkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; - one of the groups G 3 and G 4 is a nitrogen atom and the other is a CH group; - M is a hydrogen atom or an pharmaceutically acceptable cation with the proviso that, when at least one of the groups R a and R b represent a hydrogen atom and G 2 is a group CR d , then Rd represents a groups selected from C 1-4 alkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups, C 3-8 cycloalkoxy groups which may be optionally substituted by 1, 2 or 3 substituents selected from halogen atoms and hydroxy groups; and the pharmaceutically acceptable salts and N-oxides thereof.
摘要翻译：式（I）的化合物，其中：基团G 1中的一个表示氮原子或基团CR c，另一个表示基团CR ; G 2表示氮原子或基团CR 11; R 1表示选自氢原子，卤素原子，C 1-4烷基的基团，其可任选被1,2或3个选自卤素原子的取代基取代和羟基，以及可以被1,2或3个选自卤素原子和羟基的取代基任选取代的C 3-8环烷基; R 2表示选自氢原子，卤素原子，羟基，C 1-4烷基的基团，其可任选被1,2或3个选自以下的取代基取代可以任选被1,2或3个选自卤素原子和羟基的取代基取代的C 1-4烷氧基和C 3-8烷基，可以任选地被1,2或3个选自卤素原子和羟基的取代基取代的环烷基; R a，R b和R c独立地表示选自氢原子，卤素原子，C 1-4烷基的基团，可以任选被1,2或3个选自卤素原子和羟基的取代基取代的亚烷基，和可以被1,2或3个取代基任意取代的C 1-4烷氧基选自卤素原子和羟基; -R d表示选自氢原子，卤素原子，羟基，C 1-4烷基的基团，其可任选被1,2或3个选自下列的取代基取代：可以任选地被1,2或3个选自卤素原子和羟基的取代基取代的C 1-4烷氧基和C 3-8烷氧基，其可任选被1,2或3个选自卤素原子和羟基的取代基取代; G 3和G 4之一是氮原子，另一个是CH基团; - M是氢原子或药学上可接受的阳离子，条件是当基团R a和R b中的至少一个表示氢原子时，G ^{2 是基团CR d，则Rd表示选自C 1-4烷氧基的基团，其可任选被1,2或3个取代基选自卤素原子和羟基的取代基，可以任选被1,2或3个选自卤素原子和羟基的取代基取代的C 3-8环烷氧基; 及其药学上可接受的盐和N-氧化物。}

6. 发明申请

WO2012146666A1 PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：吡咯烷酮衍生物作为PI3K抑制剂
公开(公告)号：WO2012146666A1
公开(公告)日：2012-11-01
申请号：PCT/EP2012/057671
申请日：2012-04-26
申请人： ALMIRALL, S.A. , BERNAL ANCHUELA, Francisco Javier , CARRASCAL RIERA, Marta , CATURLA JAVALOYES, Juan Francisco , GRACIA FERRER, Jordi , MATASSA, Victor Giulio , TERRICABRAS BELART, Emma , TALTAVULL MOLL, Joan , ERRA SOLA, Montserrat
发明人： BERNAL ANCHUELA, Francisco Javier , CARRASCAL RIERA, Marta , CATURLA JAVALOYES, Juan Francisco , GRACIA FERRER, Jordi , MATASSA, Victor Giulio , TERRICABRAS BELART, Emma , TALTAVULL MOLL, Joan , ERRA SOLA, Montserrat
IPC分类号： C07D473/34 , C07D487/04 , A61K31/4985 , A61K31/437 , A61P35/00
CPC分类号： C07D487/04 , A61K31/53 , A61K45/06 , C07D473/34
摘要： New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
摘要翻译：公开了具有式（I）化学结构的新的吡咯并三酮衍生物; 以及它们的制备方法，包含它们的药物组合物及其在治疗中作为磷酸肌醇3-激酶（PI3K）的抑制剂的用途。

7. 发明申请

WO2012041476A1 PYRIDINE AND ISOQUINOLINE DERIVATIVES AS SYK- AND JAK-KINASE INHIBITORS 审中-公开
标题翻译：吡啶和异喹啉衍生物作为SYK-和JAK-激酶抑制剂
公开(公告)号：WO2012041476A1
公开(公告)日：2012-04-05
申请号：PCT/EP2011/004809
申请日：2011-09-26
申请人： ALMIRALL, S.A. , VIDAL JUAN, Bernat , FORNS BERENGUEL, Maria Pilar , CASTILLO MCQUADE, Marcos , ERRA SOLA, Montserrat , MIR CEPEDA, Marta
发明人： VIDAL JUAN, Bernat , FORNS BERENGUEL, Maria Pilar , CASTILLO MCQUADE, Marcos , ERRA SOLA, Montserrat , MIR CEPEDA, Marta
IPC分类号： C07D213/74 , C07D401/12 , C07D401/14 , C07D405/14 , C07D487/08 , A61K31/444 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/4995 , A61P29/00
CPC分类号： C07D213/74 , C07D401/12 , C07D401/14 , C07D405/14 , C07D487/08
摘要： The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by inhibition of Syk kinase and/or Janus kinases.
摘要翻译：本发明涉及式（I）化合物，涉及制备这些化合物的方法及其用于治疗通过抑制Syk激酶和/或Janus激酶易于改善的病理状况或疾病的用途。

8. 发明申请

WO2016202800A1 PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：吡咯烷酮衍生物作为PI3K抑制剂
公开(公告)号：WO2016202800A1
公开(公告)日：2016-12-22
申请号：PCT/EP2016/063635
申请日：2016-06-14
申请人： ALMIRALL, S.A.
发明人： TALTAVULL MOLL, Joan , MIR CEPEDA, Marta , FORNS BERENGUEL, Maria Pilar , ERRA SOLA, Montserrat
IPC分类号： C07D487/04 , C07D519/00 , A61K31/53 , A61P11/00 , A61P9/00 , A61P25/00 , A61P35/00 , A61P17/00 , A61P37/00
CPC分类号： C07D487/04 , C07D519/00
摘要： New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
摘要翻译：公开了具有式（I）化学结构的新的吡咯并三酮衍生物; 以及它们的制备方法，包含它们的药物组合物及其在治疗中作为磷酸肌醇3-激酶（PI3K）的抑制剂的用途。

9. 发明申请

WO2014060431A1 PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：吡咯烷酮衍生物作为PI3K抑制剂
公开(公告)号：WO2014060431A1
公开(公告)日：2014-04-24
申请号：PCT/EP2013/071550
申请日：2013-10-15
申请人： ALMIRALL, S.A.
发明人： GRACIA FERRER, Jordi , CARRASCAL RIERA, Marta , ERRA SOLA, Montserrat
IPC分类号： C07D519/00 , A61K31/53 , A61P11/00 , A61P9/00 , A61P25/00 , A61P31/12
CPC分类号： C07D519/00
摘要： New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
摘要翻译：公开了具有式（I）化学结构的新的吡咯并三酮衍生物; 以及它们的制备方法，包含它们的药物组合物及其在治疗中作为磷酸肌醇3-激酶（PI3K）的抑制剂的用途。

10. 发明申请

WO2014060432A1 PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：吡咯烷酮衍生物作为PI3K抑制剂
公开(公告)号：WO2014060432A1
公开(公告)日：2014-04-24
申请号：PCT/EP2013/071551
申请日：2013-10-15
申请人： ALMIRALL, S.A.
发明人： ERRA SOLA, Montserrat , CARRASCAL RIERA, Marta , TALTAVULL MOLL, Joan , CATURLA JAVALOYES, Juan Francisco , BERNAL ANCHUELA, Francisco Javier , PAGES SANTACANA, Lluis Miquel , MIR CEPEDA, Marta , CASALS COLL, Gaspar , HERNANDEZ OLASAGARRE, Maria Begoña
IPC分类号： C07D487/04 , C07D519/00 , A61K31/53 , A61P11/00 , A61P9/00 , A61P25/00 , A61P31/12
CPC分类号： C07D487/04 , A61K31/53 , A61K45/06 , C07D519/00
摘要： New pyrrolotriazinone derivatives having the chemical structure of formula (I), are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks)
摘要翻译：公开了具有式（I）化学结构的新的吡咯并三酮衍生物; 以及它们的制备方法，包含它们的药物组合物及其在治疗中作为磷酸肌醇3-激酶（PI3K）抑制剂的用途，

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