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公开(公告)号：US20130216498A1
公开(公告)日：2013-08-22
申请号：US13518863
申请日：2010-12-23
申请人： Paul Robert Eastwood , Jacob Gonzales Rodriguez , Jordi Bach Taña , Lluis Miquel Pages Santacana , Joan Taltavull Moll , Juan Francisco Caturla Javaloyes , Victor Giulio Matassa
发明人： Paul Robert Eastwood , Jacob Gonzales Rodriguez , Jordi Bach Taña , Lluis Miquel Pages Santacana , Joan Taltavull Moll , Juan Francisco Caturla Javaloyes , Victor Giulio Matassa
IPC分类号： C07D471/04 , A61K31/517 , A61K31/497 , A61K31/513 , A61K31/5377 , A61K45/06 , A61K31/506 , A61K31/551
CPC分类号： C07D471/04 , A61K31/437 , A61K31/497 , A61K31/506 , A61K31/513 , A61K31/517 , A61K31/5377 , A61K31/551 , A61K45/06
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 Janus Kinases (JAK).
摘要翻译： 公开了具有式（I）化学结构的新咪唑并吡啶衍生物; 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Janus Kinases（JAK）抑制剂的用途。
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公开(公告)号：US20130209400A1
公开(公告)日：2013-08-15
申请号：US13579344
申请日：2011-02-18
申请人： Jordi Bach Taña , Lluis Miquel Pages Santacana , Joan Taltavull Moll , Paul Robert Eastwood , Jacob Gonzalez Rodrigues , Victor Giulio Matassa
发明人： Jordi Bach Taña , Lluis Miquel Pages Santacana , Joan Taltavull Moll , Paul Robert Eastwood , Jacob Gonzalez Rodrigues , Victor Giulio Matassa
IPC分类号： C07D471/04 , A61K45/06 , A61K31/4985 , A61K31/497 , A61K31/506 , C07D487/04
CPC分类号： C07D487/04 , A61K31/437 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K45/06 , C07D471/04
摘要： New pyrazole 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 Janus Kinases (JAK).
摘要翻译： 公开了具有式（I）化学结构的新的吡唑衍生物; 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Janus Kinases（JAK）抑制剂的用途。
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公开(公告)号：US20140086870A9
公开(公告)日：2014-03-27
申请号：US13579344
申请日：2011-02-18
申请人： Jordi Bach Taña , Lluis Miquel Pages Santacana , Joan Taltavull Moll , Paul Robert Eastwood , Jacob Gonzalez Rodrigues , Victor Giulio Matassa
发明人： Jordi Bach Taña , Lluis Miquel Pages Santacana , Joan Taltavull Moll , Paul Robert Eastwood , Jacob Gonzalez Rodrigues , Victor Giulio Matassa
IPC分类号： C07D471/04 , A61K45/06 , A61K31/4985 , A61K31/497 , A61K31/506 , C07D487/04
CPC分类号： C07D487/04 , A61K31/437 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K45/06 , C07D471/04
摘要： New pyrazole 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 Janus Kinases (JAK).
摘要翻译： 公开了具有式（I）化学结构的新的吡唑衍生物; 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Janus Kinases（JAK）抑制剂的用途。
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![Substituted pyrazolo[1,5-a]pyridines as JAK inhibitors](/abs-image/US/2015/12/08/US09206183B2/abs.jpg.150x150.jpg)
公开(公告)号：US09206183B2
公开(公告)日：2015-12-08
申请号：US13579344
申请日：2011-02-18
申请人： Jordi Bach Taña , Lluis Miquel Pages Santacana , Joan Taltavull Moll , Paul Robert Eastwood , Jacob Gonzalez Rodrigues , Victor Giulio Matassa
发明人： Jordi Bach Taña , Lluis Miquel Pages Santacana , Joan Taltavull Moll , Paul Robert Eastwood , Jacob Gonzalez Rodrigues , Victor Giulio Matassa
IPC分类号： A61K31/437 , C07D221/04 , C07D487/04 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K45/06 , C07D471/04
CPC分类号： C07D487/04 , A61K31/437 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K45/06 , C07D471/04
摘要： New pyrazole 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 Janus Kinases (JAK).
摘要翻译： 公开了具有式（I）化学结构的新的吡唑衍生物; 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Janus Kinases（JAK）抑制剂的用途。
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公开(公告)号：US09340547B2
公开(公告)日：2016-05-17
申请号：US14114541
申请日：2012-04-26
申请人： Francisco Javier Bernal Anchuela , Marta Carrascal Riera , Juan Francisco Caturla Javaloyes , Jordi Gracia Ferrer , Victor Giulio Matassa , Emma Terricabras Belart , Joan Taltavull Moll , Montserrat Erra Sola
发明人： Francisco Javier Bernal Anchuela , Marta Carrascal Riera , Juan Francisco Caturla Javaloyes , Jordi Gracia Ferrer , Victor Giulio Matassa , Emma Terricabras Belart , Joan Taltavull Moll , Montserrat Erra Sola
IPC分类号： C07D487/04 , A61K31/53 , A61P11/06 , A61P11/00 , C07D473/34 , A61K45/06
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。
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公开(公告)号：US20140163033A1
公开(公告)日：2014-06-12
申请号：US14114541
申请日：2012-04-26
申请人： Francisco Javier Bernal Anchuela , Marta Carrascal Riera , Juan Francisco Caturla Javaloyes , Jordi Gracia Ferrer , Victor Giulio Matassa , Emma Terricabras Belart , Joan Tal Tavul Moll , Montserat Eraa Sola
发明人： Francisco Javier Bernal Anchuela , Marta Carrascal Riera , Juan Francisco Caturla Javaloyes , Jordi Gracia Ferrer , Victor Giulio Matassa , Emma Terricabras Belart , Joan Tal Tavul Moll , Montserat Eraa Sola
IPC分类号： C07D487/04 , A61K45/06 , A61K31/53
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。
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公开(公告)号：US20150099752A9
公开(公告)日：2015-04-09
申请号：US14114541
申请日：2012-04-26
申请人： Francisco Javier Bernal Anchuela , Marta Carrascal Riera , Juan Francisco Caturla Javaloyes , Jordi Gracia Ferrer , Victor Giulio Matassa , Emma Terricabras Belart , Joan Tal Tavul Moll , Montserat Eraa Sola
发明人： Francisco Javier Bernal Anchuela , Marta Carrascal Riera , Juan Francisco Caturla Javaloyes , Jordi Gracia Ferrer , Victor Giulio Matassa , Emma Terricabras Belart , Joan Tal Tavul Moll , Montserat Eraa Sola
IPC分类号： C07D487/04 , A61K45/06 , A61K31/53
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。
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8.发明授权Substituted indolin-2-one derivatives and their use as P38 mitogen-activated kinase inhibitors 失效取代的二氢吲哚-2-酮衍生物及其作为P38丝裂原活化激酶抑制剂的用途公开(公告)号：US08450341B2
公开(公告)日：2013-05-28
申请号：US12989696
申请日：2009-04-16
IPC分类号： A01N43/42 , A01N43/82 , A01N43/38 , A61K31/44 , A61K31/41 , A61K31/40 , A61K31/405 , C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02 , C07D271/06 , C07D271/12 , C07D413/00 , C07D498/00 , C07D261/20 , C07D249/00 , C07D487/02 , C07D495/02 , C07D497/02 , C07D405/00 , C07D409/00 , C07D411/00 , C07D209/36
CPC分类号： C07D413/04 , C07D491/107 , C07D491/20
摘要： The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译： 本公开涉及具有通式（I）的p38丝裂原活化蛋白激酶的新抑制剂，其制备方法，其药物组合物及其使用方法。
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9.发明申请SUBSTITUTED INDOLIN-2-ONE DERIVATIVES AND THEIR USE AS P38 MITOGEN-ACTIVATED KINASE INHIBITORS 失效取代的吲哚啉-2-酮衍生物及其作为P38激活的激酶激酶抑制剂公开(公告)号：US20110046097A1
公开(公告)日：2011-02-24
申请号：US12989696
申请日：2009-04-16
IPC分类号： A61K31/423 , C07D413/04 , C07D491/107 , C07D491/20 , C07D471/04 , C07D413/14 , A61K31/437 , A61K31/5377 , A61K31/416 , A61K31/573 , A61K31/4985 , A61P35/00 , A61P29/00 , A61P9/10 , A61P9/00 , A61P11/00 , A61P1/00 , A61P19/10 , A61P25/28 , A61P17/06 , A61P19/02
CPC分类号： C07D413/04 , C07D491/107 , C07D491/20
摘要： The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译： 本公开涉及具有通式（I）的p38丝裂原活化蛋白激酶的新抑制剂，其制备方法，其药物组合物及其使用方法。
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10.发明授权Benzodiazepine derivatives and their use as antagonists of cholecystokinin and/or gastrin receptors 失效苯并二氮杂衍生物及其作为胆囊收缩素和/或胃泌素受体拮抗剂的用途
公开(公告)号：US5696110A
公开(公告)日：1997-12-09
申请号：US523661
申请日：1995-09-05
IPC分类号： C07D243/20 , C07D403/04 , A61K31/55 , C07D401/04 , C07D413/04
CPC分类号： C07D403/04 , C07D243/20
摘要： ##STR1## Compounds of formula (I), and salts and prodrugs thereof, wherein X is O,S,NR
4 or CH
2 ; R
1 represents H, certain optionally substituted C
1-6 alkyl, or C
3-7 cycloalkyl; R
2 represents phenyl having certain optional substituents; R
3 represents C
1-6 alkyl, halo or NR
6 R
7 ; m is 2,3 or 4; n is 1,2,3,4,5,6 7 or 8 when X is CH
2 or 2,3,4,5,6,7 or 8 when X is O, S or NR
4 ; and x is 0,1,2, or 3; are CCK and/or gastrin antagonists. They and compositions thereof are therefore useful in therapy.摘要翻译： 式（I）化合物及其盐和前体药物，其中X为O，S，NR4或CH2; R1表示H，某些任选取代的C 1-6烷基或C 3-7环烷基; R2表示具有某些任选取代基的苯基; R 3表示C 1-6烷基，卤代或NR 6 R 7; m是2,3或4; 当X为CH 2时，n为1,2,3,4,5,6,7或8，X为O，S或NR4时为2,3,4,5,6,7或8; x为0,1,2或3; 是CCK和/或胃泌素拮抗剂。 因此，它们及其组合物可用于治疗。
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