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1. 发明申请

WO2012146667A1 IMIDAZOPYRIDINE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的咪唑吡啶衍生物
公开(公告)号：WO2012146667A1
公开(公告)日：2012-11-01
申请号：PCT/EP2012/057674
申请日：2012-04-26
申请人： ALMIRALL, S.A. , CARRASCAL RIERA, Marta , GRACIA FERRER, Jordi , MATASSA, Victor, Giulio , TERRICABRAS BELART, Emma , PAGES SANTACANA, Lluis, Miquel
发明人： CARRASCAL RIERA, Marta , GRACIA FERRER, Jordi , MATASSA, Victor, Giulio , TERRICABRAS BELART, Emma , PAGES SANTACANA, Lluis, Miquel
IPC分类号： C07D473/34 , C07D487/04 , A61K31/4985 , A61K31/437 , A61P35/00
CPC分类号： C07D473/34 , C07D487/04
摘要： New imidazopyridine 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）化学结构的新的咪唑并吡啶衍生物; 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。

2. 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。

3. 发明申请

WO2011035900A1 NEW THIADIAZOLE DERIVATIVES 审中-公开
标题翻译：新的噻唑烷衍生物
公开(公告)号：WO2011035900A1
公开(公告)日：2011-03-31
申请号：PCT/EP2010/005801
申请日：2010-09-22
申请人： ALMIRALL, S.A. , GRIMA POVEDA, Pedro Manuel , AGUILAR IZQUIERDO, Nuria , MIR CEPEDA, Marta , CARRASCAL RIERA, Marta , TERRICABRAS BELART, Emma , GRACIA FERRER, Jordi , CASALS COLL, Gaspar
发明人： GRIMA POVEDA, Pedro Manuel , AGUILAR IZQUIERDO, Nuria , MIR CEPEDA, Marta , CARRASCAL RIERA, Marta , TERRICABRAS BELART, Emma , GRACIA FERRER, Jordi , CASALS COLL, Gaspar
IPC分类号： C07D285/135 , A61K31/433 , A61P37/02
CPC分类号： C07D285/135 , C07D417/12 , C07D417/14
摘要： The present invention relates to thiadiazole derivatives of formula (I), to processes for their preparation and to pharmaceutical compositions containing them. These compounds are potent agonists of S1P1 receptors and thus, they are useful In the treatment, prevention or suppression of diseases and disorders known to be susceptible to improvement by sphingosine-1-phosphate receptors agonists (S1P1), such as autoimmune diseases, chronic immune and inflammatory diseases, transplant rejection, malignant neoplastic diseases, angiogenic-related disorders, pain, neurological diseases, viral and infectious diseases.
摘要翻译：本发明涉及式（I）的噻二唑衍生物，其制备方法和含有它们的药物组合物。这些化合物是S1P1受体的有效激动剂，因此它们可用于治疗，预防或抑制已知易于通过鞘氨醇-1-磷酸受体激动剂（S1P1）改善的疾病和病症，例如自身免疫性疾病，慢性免疫和炎症性疾病，移植排斥反应，恶性肿瘤性疾病，血管发生相关疾病，疼痛，神经系统疾病，病毒和感染性疾病。

4. 发明申请

WO2011069647A1 NEW 2-AMINOTHIADIAZOLE DERIVATIVES 审中-公开
标题翻译：新的2-氨基噻唑衍生物
公开(公告)号：WO2011069647A1
公开(公告)日：2011-06-16
申请号：PCT/EP2010/007467
申请日：2010-12-08
申请人： ALMIRALL, S.A. , GRIMA POVEDA1 Pedro Manuel , AGUILAR IZQUIERDO, Nuria , MIR CEPEDA Marta , CARRASCAL RIERA, Marta , TERRICABRAS BELART, Emma
发明人： GRIMA POVEDA1 Pedro Manuel , AGUILAR IZQUIERDO, Nuria , MIR CEPEDA Marta , CARRASCAL RIERA, Marta , TERRICABRAS BELART, Emma
IPC分类号： C07D285/12 , A61K31/433
CPC分类号： C07D285/12 , A61K31/433 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or N-oxide thereof: wherein:. L represents a direct bond or a -S(O) 2 - group, • n is an integer having a value from 0 to 2, • R 1 represents a pyridyl group or an imidazo[1,2-α]pyridinyl group, wherein the pyridyl group is substituted with one or more substituents selected from halogen atoms, a hydroxy group, a C 1-4 alkyl group and a C 1-4 alkoxy group, or • R 1 represents a group of formula: wherein:. R a and R b independently represent a hydrogen atom, halogen atom or a linear or branched C 1-4 , alkyl group,. R c represents a hydroxy group, a linear or branched C 1-4 alkyl group or C 1-4 alkoxy group wherein the alkyl and the alkoxy groups independently are optionally substituted with one or more substituents selected from hydroxy group, cyano group and-NR'R" groups and wherein R' represents a hydrogen atom or a linear or branched C 1-4 alkyl group, R" represents a hydrogen atom or a linear or branched C 1-4 alkyl group optionally substituted with a hydroxycarbonyl group; or R' and R" together with the nitrogen atom to which they are attached form a 4 to 6 membered, saturated heterocyclic ring optionally substituted with a hydroxycarbonyl group.. R 2 represents a pyridyl group, a C 3-6 cycloalkyl group or a phenyl group which is optionally substituted with one or more substituents selected from halogen atoms, cyano group, and C 1-4 alkoxy group; and. R 3 represents a C 3-6 cycloalkyl group, a C 3-6 cycloalkyl-C 1-2 alkyl group or a linear or branched C 2-4 alkyl group optionally substituted with one or more substituents selected from halogen atoms and C 1-2 alkoxy group.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或N-氧化物：其中： L表示直接键或-S（O）2 - 基，n表示0〜2的整数，R 1表示吡啶基或咪唑并[1,2-a]吡啶基，其中，吡啶基被一个或多个选自卤素原子，羟基，C 1-4烷基和C 1-4烷氧基的取代基取代，或者R 1表示下列基团：其中：。 R a和R b独立地表示氢原子，卤素原子或直链或支链C 1-4烷基。 Rc表示羟基，直链或支链C 1-4烷基或C 1-4烷氧基，其中烷基和烷氧基独立地被一个或多个选自羟基，氰基和-NR'R“ 基团，其中R'表示氢原子或直链或支链C 1-4烷基，R“表示氢原子或任选被羟基羰基取代的直链或支链C 1-4烷基; 或R'和R“与它们所连接的氮原子一起形成任选被羟基羰基取代的4至6元饱和杂环.R 2表示吡啶基，C 3-6环烷基或苯基其任选被一个或多个选自卤素原子，氰基和C 1-4烷氧基的取代基取代; R 3表示C 3-6环烷基，C 3-6环烷基-C 1-2烷基或直链或任选被一个或多个选自卤素原子和C 1-2烷氧基的取代基取代的支链C 2-4烷基。

5. 发明申请

WO2004058729A1 NEW PYRIDAZIN-3(2H)-ONE DERIVATIVES 审中-公开
标题翻译：新的吡啶-3（2H） - 酮衍生物
公开(公告)号：WO2004058729A1
公开(公告)日：2004-07-15
申请号：PCT/EP2003/014722
申请日：2003-12-22
申请人： ALMIRALL PRODESFARMA SA , DAL PIAZ, Vittorio , AGUILAR IZQUIERDO, Nuria , BUIL ALBERO, Maria Antonia , CARRASCAL RIERA, Marta , GRACIA FERRER, Jordi , GIOVANNONI, Maria, Paola , VERGELLI, Claudia
发明人： DAL PIAZ, Vittorio , AGUILAR IZQUIERDO, Nuria , BUIL ALBERO, Maria Antonia , CARRASCAL RIERA, Marta , GRACIA FERRER, Jordi , GIOVANNONI, Maria, Paola , VERGELLI, Claudia
IPC分类号： C07D237/24
CPC分类号： C07D401/04 , C07D237/24 , C07D401/12 , C07D403/04 , C07D409/12 , C07D413/04 , C07D417/04
摘要： Pyridazin-3(2H)-one derivatives of formula (I) are found to inhibit PDE-4:, wherein R 1 , R 2 and R 4 are organic radicals, R 3 is a cyclic group, and R 5 is an ester or an aryl or heteroaryl group.
摘要翻译：发现式（I）的哒嗪-3（2H） - 酮衍生物抑制PDE-4：其中R 1，R 2和R 4是有机基团，R 3是环状基团 R 5为酯或芳基或杂芳基。

6. 发明申请

WO2005123693A1 PYRIDAZIN-3(2H)-ONE DERIVATIVES AND THEIR USE AS PDE4 INHIBITORS 审中-公开
标题翻译：吡啶并-3（2H） - 酮衍生物及其作为PDE4抑制剂的用途
公开(公告)号：WO2005123693A1
公开(公告)日：2005-12-29
申请号：PCT/EP2005/006712
申请日：2005-06-21
申请人： ALMIRALL PRODESFARMA, S.A. , AGUILAR IZQUIERDO, Nuria , CARRASCAL RIERA, Marta , DAL PIAZ, Vittorio , GRACIA FERRER, Jordi , LUMERAS AMADOR, Wenceslao , MASDEU MARGALEF, Maria del Carmen , WARRELLOW, Graham
发明人： AGUILAR IZQUIERDO, Nuria , CARRASCAL RIERA, Marta , DAL PIAZ, Vittorio , GRACIA FERRER, Jordi , LUMERAS AMADOR, Wenceslao , MASDEU MARGALEF, Maria del Carmen , WARRELLOW, Graham
IPC分类号： C07D237/24
CPC分类号： C07D405/14 , C07D237/24 , C07D401/12 , C07D401/14 , C07D409/14 , C07D471/04 , C07D495/04
摘要： The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives, to processes for their preparation and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention and suppression of related pathological conditions, diseases and disorders, in particular asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, topic dermatitis, psoriasis or irritable bowel disease.
摘要翻译：本发明涉及新的治疗上有用的哒嗪-3（2H） - 酮衍生物，其制备方法和含有它们的药物组合物。这些化合物是磷酸二酯酶4（PDE4）的有效和选择性抑制剂，因此可用于治疗，预防和抑制相关病理状况，疾病和病症，特别是哮喘，慢性阻塞性肺病，类风湿性关节炎，主题皮炎，牛皮癣或肠易激综合征

7. 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。

8. 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。

9. 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。

10. 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：

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