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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

WO2011141180A1 NEW CYCLOHEXYLAMINE DERIVATIVES HAVING ß2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES 审中-公开
标题翻译：具有β2ADRENERGIC AGONIST和M3 MUSCARINIC ANTAGONIST活动的新CYCLOHEXYLAMINE衍生物
公开(公告)号：WO2011141180A1
公开(公告)日：2011-11-17
申请号：PCT/EP2011002376
申请日：2011-05-13
申请人： ALMIRALL SA , PRAT QUINONES MARIA , FONQUERNA POU SILVIA , PUIG DURAN CARLOS , LUMERAS AMADOR WENCESLAO , AIGUADE BOSCH JOSE , CATURLA JAVALOYES JUAN FRANCISCO
发明人： PRAT QUINONES MARIA , FONQUERNA POU SILVIA , PUIG DURAN CARLOS , LUMERAS AMADOR WENCESLAO , AIGUADE BOSCH JOSE
IPC分类号： C07D409/14 , A61K31/4709 , A61P11/00
CPC分类号： C07D409/14 , A61K31/4709 , C07D215/26 , C07D405/12 , C07D409/12 , C07D413/14
摘要： The present invention relates to novel compounds having ß2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
摘要翻译：本发明涉及具有β2肾上腺素能激动剂和M3毒蕈碱拮抗剂双重活性的新化合物，含有它们的药物组合物，其制备方法及其在呼吸治疗中的用途。

3. 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。

4. 发明申请

WO03082867A8 AZAINDOLYLPIPERIDINE DERIVATIVES AS ANTIHISTAMINIC AND ANTIALLERGIC AGENTS 审中-公开
标题翻译：作为抗病毒和抗癌药物的阿魏酸哌啶衍生物
公开(公告)号：WO03082867A8
公开(公告)日：2004-11-04
申请号：PCT/EP0303377
申请日：2003-04-01
申请人： ALMIRALL PRODESFARMA SA , FONQUERNA POU SILVIA , PAGES SANTACANA LUIS MIGUEL , PUIG DURAN CARLOS , CARDUS FIGUERAS ARANZAZU
发明人： FONQUERNA POU SILVIA , PAGES SANTACANA LUIS MIGUEL , PUIG DURAN CARLOS , PRIETO SOTO JOSE MANUEL , CARDUS FIGUERAS ARANZAZU
IPC分类号： A61K31/4545 , A61P11/06 , A61P17/00 , A61P27/02 , A61P27/16 , A61P37/08 , C07D471/04 , A61K31/437 , A61K31/498 , A61K31/5025 , A61K31/519 , A61K31/53 , C07D487/04
CPC分类号： C07D471/04
摘要： This invention is directed to new potent and selective antagonists of H1 histamine receptors having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.

5. 发明申请

WO2011141180A8 NEW CYCLOHEXYLAMINE DERIVATIVES HAVING β2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES 审中-公开
公开(公告)号：WO2011141180A8
公开(公告)日：2011-11-17
申请号：PCT/EP2011/002376
申请日：2011-05-13
申请人： ALMIRALL, S.A. , PRAT QUINONES, Maria , FONQUERNA POU, Silvia , PUIG DURAN, Carlos , LUMERAS AMADOR, Wenceslao , AIGUADE BOSCH, Jose , CATURLA JAVALOYES, Juan Francisco
发明人： PRAT QUINONES, Maria , FONQUERNA POU, Silvia , PUIG DURAN, Carlos , LUMERAS AMADOR, Wenceslao , AIGUADE BOSCH, Jose , CATURLA JAVALOYES, Juan Francisco
IPC分类号： C07D409/14 , A61K31/4709 , A61P11/00
摘要： The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.

6. 发明申请

WO2011113578A1 NEW OXADIAZOLE DERIVATIVES 审中-公开
标题翻译：新的氧化氮衍生物
公开(公告)号：WO2011113578A1
公开(公告)日：2011-09-22
申请号：PCT/EP2011/001273
申请日：2011-03-15
申请人： ALMIRALL, S.A. , AGUILAR IZQUIERDO, Nuria , FONQUERNA POU, Silvia , TABOADA MARTINEZ, Lorena , VIDAL JUAN, Bernat , CARRASCAL RIERA, Marta , NAVARRO ROMERO, Eloisa
发明人： AGUILAR IZQUIERDO, Nuria , FONQUERNA POU, Silvia , TABOADA MARTINEZ, Lorena , VIDAL JUAN, Bernat , CARRASCAL RIERA, Marta , NAVARRO ROMERO, Eloisa
IPC分类号： C07D413/04 , A61K31/4245 , C07D413/14 , A61P25/00 , A61P29/00 , A61P31/00 , A61P35/00
CPC分类号： C07D413/04 , A61K45/06 , C07D413/14
摘要： The present invention relates to an oxadiazole derivative of formula (I)1 or a pharmaceutically acceptable salt or N-oxide thereof: wherein, R 1 represents a hydrogen atom, a C 1-2 alkyl group or a C 3-4 cycloalkyl-C 1-2 alkyl group, both R 2 and R 3 represent a C 1-2 alkyl group; R a represents a hydrogen atom or a C 1-2 alkyl group; R b represents a hydrogen atom, a C 1-2 alkyl group, a C 3-4 , cycloalkyl group, a carboxy group, a carbamoyl group or a -CF 3 group; R c represents a linear or branched C 2.5 alkyl group substituted with one substituent selected from a hydroxy group, a triazolyl group and a -P(O)(OH) 2 group; a -(CH 2 )( 1-2 )-C(O)OR' group; a -NR'R" group; a -(CH 2 )( 1-2 NR'R" group; a -(CH 2 )( 1-2 )-NHC(O)R" group; a -(CH 2 ) (2-4) NH-(CH 2 ) (1-3) -NR'R" group; or a -O-(CH 2 ) (2-3) NR'R" group, wherein: R' represents a hydrogen atom or a C 1-2 alkyl group, R" represents a hydrogen atom; a C 5-6 cycloalkyl group substituted with a carboxy group; a 5- to 6-membered saturated heterocyclic ring containing one nitrogen atom and substituted with a carboxy(C 1-2 alkyl) group; or a C 1-2 alkyl group optionally substituted by one or more substituents selected from halogen atoms, hydroxy groups, methyl groups, amino groups, carbamoyl groups and carboxy groups; or R' and R" together with the nitrogen atom to which they are attached form (a) a 4 to 6 membered saturated or unsaturated heterocyclic group, which contains, as heteroatom, one N atom and, optionally, one further N atom and which heterocyclic group is substituted with one or more substituents selected from a halogen atom, a hydroxy group, a methyl group, an oxy group and a carboxy group, or (b) a 5 membered heteroaryl group which contains, as heteroatom, one N atom and, optionally, one or more further N atoms and which heteroaryl group is optionally substituted with one substituent selected from an amino group and a carboxy group.
摘要翻译：本发明涉及式（I）1的恶二唑衍生物或其药学上可接受的盐或N-氧化物：其中，R1表示氢原子，C1-2烷基或C3-4环烷基-C1-2烷基基团，R2和R3均表示C1-2烷基; R a表示氢原子或C 1-2烷基; Rb表示氢原子，C1-2烷基，C3-4，环烷基，羧基，氨基甲酰基或-CF3基; Rc表示被选自羟基，三唑基和-P（O）（OH）2基团的一个取代基取代的直链或支链C 2-5烷基; a - （CH 2）（1-2）-C（O）OR'基团; （CH2）（1-2NR'R“基; - （CH2）（1-2）-NHC（O）R”基; a - （CH2））NH-（CH 2）（1-3）-NR'R“基;或-O-（CH 2）（2-3）NR'R”基，其中：R'表示氢原子或C1-2 烷基，R“表示氢原子，被羧基取代的C5-6环烷基，含有一个氮原子并被羧基（C1-2烷基）取代的5-至6-元饱和杂环;或任选被一个或多个选自卤素原子，羟基，甲基，氨基，氨基甲酰基和羧基的取代基取代的C 1-2烷基;或R'和R“与它们所连接的氮原子一起形成（ a）4至6元饱和或不饱和杂环基，其含有一个N原子和任选的另外一个N原子作为杂原子，哪个杂环基被一个或多个选自卤素原子，羟基的取代基，甲基，氧基和羧基，或（b ）5元杂芳基，其含有作为杂原子的一个N原子和任选的一个或多个另外的N原子，并且该杂芳基任选被一个选自氨基和羧基的取代基取代。

7. 发明申请

WO2007039297A1 IMIDAZOPYRIDINE DERIVATIVES AS A2B ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：咪唑吡啶衍生物作为A2B腺苷受体拮抗剂
公开(公告)号：WO2007039297A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/009620
申请日：2006-10-05
申请人： LABORATORIOS ALMIRALL, S.A. , VIDAL JUAN, Bernat , FONQUERNA POU, Silvia , EASTWOOD, Paul, Robert , AIGUADE BOSCH, Jose , CARDUS FIGUERAS, Aranzazu , CARRANCO MORUNO, Ines , GONZALEZ RODRIGUEZ, Jacob , PAREDES APARICIO, Sergio
发明人： VIDAL JUAN, Bernat , FONQUERNA POU, Silvia , EASTWOOD, Paul, Robert , AIGUADE BOSCH, Jose , CARDUS FIGUERAS, Aranzazu , CARRANCO MORUNO, Ines , GONZALEZ RODRIGUEZ, Jacob , PAREDES APARICIO, Sergio
IPC分类号： C07D471/04 , A61K31/437 , A61P37/00 , A61P9/00 , A61P3/10 , A61P11/00
CPC分类号： C07D471/04
摘要： New imidazopyrdidine derivatives of formula (I) are disclosed as antagonists of the A 28 adenosine receptor.
摘要翻译：公开了式（I）的新的咪唑并吡啶衍生物作为A 28 N腺苷受体的拮抗剂。

8. 发明申请

WO2003099807A1 NEW INDOLYLPIPERIDINE DERIVATIVES AS POTENT ANTIHISTAMINIC AND ANTIALLERGIC AGENTS 审中-公开
标题翻译：新的吲哚美辛衍生物作为抗病毒和抗癌药物
公开(公告)号：WO2003099807A1
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005222
申请日：2003-05-19
申请人： ALMIRALL PRODESFARMA S.A. , FONQUERNA POU, Silvia , PAGES SANTACANA, Luis Miguel
发明人： FONQUERNA POU, Silvia , PAGES SANTACANA, Luis Miguel
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： This invention is directed to new potent and selective antagonists of H 1 histamine receptors having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy as antiallergic agents.
摘要翻译：本发明涉及具有通式（I）的H> 1 <组胺受体的新的有效和选择性拮抗剂，用于其制备方法; 包含它们的药物组合物; 并将其用于治疗作为抗过敏剂。

9. 发明申请

WO2003082867A1 AZAINDOLYLPIPERIDINE DERIVATIVES AS ANTIHISTAMINIC AND ANTIALLERGIC AGENTS 审中-公开
标题翻译：作为抗病毒和抗癌药物的阿魏酸哌啶衍生物
公开(公告)号：WO2003082867A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003377
申请日：2003-04-01
申请人： ALMIRALL PRODESFARMA S.A. , FONQUERNA POU, Silvia , PAGES SANTACANA, Luis, Miguel , PUIG DURAN, Carlos , PRIETO SOTO, José Manuel , CARDUS FIGUERAS, Aranzazu
发明人： FONQUERNA POU, Silvia , PAGES SANTACANA, Luis, Miguel , PUIG DURAN, Carlos , PRIETO SOTO, José Manuel , CARDUS FIGUERAS, Aranzazu
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： This invention is directed to new potent and selective antagonists of H 1 histamine receptors having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
摘要翻译：本发明涉及具有通式（I）的H1组胺受体的新的有效和选择性拮抗剂，用于其制备方法; 包含它们的药物组合物; 并用于治疗。

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