65880-18-4Relevant articles and documents
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties
Wang, Xiaojing,Barbosa, James,Blomgren, Peter,Bremer, Meire C.,Chen, Jacob,Crawford, James J.,Deng, Wei,Dong, Liming,Eigenbrot, Charles,Gallion, Steve,Hau, Jonathon,Hu, Huiyong,Johnson, Adam R.,Katewa, Arna,Kropf, Jeffrey E.,Lee, Seung H.,Liu, Lichuan,Lubach, Joseph W.,Macaluso, Jen,Maciejewski, Pat,Mitchell, Scott A.,Ortwine, Daniel F.,Dipaolo, Julie,Reif, Karin,Scheerens, Heleen,Schmitt, Aaron,Wong, Harvey,Xiong, Jin-Ming,Xu, Jianjun,Zhao, Zhongdong,Zhou, Fusheng,Currie, Kevin S.,Young, Wendy B.
supporting information, p. 608 - 613 (2017/06/13)
In our continued effort to discover and develop best-in-class Bruton's tyrosine kinase (Btk) inhibitors for the treatment of B-cell lymphomas, rheumatoid arthritis, and systemic lupus erythematosus, we devised a series of novel tricyclic compounds that improved upon the druglike properties of our previous chemical matter. Compounds exemplified by G-744 are highly potent, selective for Btk, metabolically stable, well tolerated, and efficacious in an animal model of arthritis.
HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY
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Paragraph 0737; 0738, (2015/11/16)
Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I foranddiagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
HETEROARYL PYRIDONE AND AZA-PYRIDONE AMIDE COMPOUNDS
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, (2015/01/16)
Heteroaryl pyridone and aza-pyridone amide compounds of Formula (I) are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
BICYCLIC PIPERAZINE COMPOUNDS
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Paragraph 0202; 0203, (2013/05/21)
Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
ALKYLATED PIPERAZINE COMPOUNDS
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Paragraph 0406; 0407, (2013/05/21)
Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
PHARMACEUTICAL COMPOSITION CONTAINING FUSED HETERO-RING DERIVATIVE
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, (2012/06/18)
The present invention provides a compound which indicates a histamine H4 receptor modulating activity.A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R1 is substituted or unsubstituted alkyl, etc., W is -O-, etc., n is an integer of 0 to 6; X is N(R7)- or -O-; R7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is-C(R8)= or -N=; R8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is =O, =S, etc.; B ring is a ring represented by the following formula wherein R10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R11, R12a and R12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.The present invention provides a compound which indicates a histamine H4 receptor modulating activity. A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R 1 is substituted or unsubstituted alkyl, etc., W is -O-, etc., n is an integer of 0 to 6; X is N(R 7 )- or -O-; R 7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is-C(R 8 )= or -N=; R 8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is =O, =S, etc.; B ring is a ring represented by the following formula wherein R 10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R 11 , R 12a and R 12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.
PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE
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, (2011/11/30)
Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Manganese(III)-catalyzed formal [3+2] annulation of vinyl azides and ?-keto acids for synthesis of pyrroles
Ng, Eileen Pei Jian,Wang, Yi-Feng,Chiba, Shunsuke
experimental part, p. 783 - 786 (2011/06/11)
Manganese(III)-catalyzed formal [3+2] annnulation of vinyl azides and -keto acids has been developed for the synthesis of substituted NH pyrroles with a wide range of substituents. Georg Thieme Verlag Stuttgart.
A new synthesis of pyrroles
Quiclet-Sire, Beatrice,Wendeborn, Frederique,Zard, Samir Z.
, p. 2214 - 2215 (2007/10/03)
The radical reaction between an N-ethylsulfonylenamide and an α-xanthyl ketone gives an intermediate γ-keto imine which spontaneously ring-closes to the pyrrole.
