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公开(公告)号:US20090270389A1
公开(公告)日:2009-10-29
申请号:US12387181
申请日:2009-04-29
申请人: Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
发明人: Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
IPC分类号: A61K31/5377 , C07D471/04 , A61K31/519 , A61P35/00
CPC分类号: C07D471/04
摘要: This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R1, R2, R3, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.
摘要翻译: 本申请公开了根据式I的新型嘧啶基吡啶酮衍生物,其中A,R1,R2,R3和m如本文所述限定,其抑制JNK。 本文公开的化合物可用于调节JNK的活性并治疗与过量JNK活性相关的疾病。 这些化合物可用于治疗自身免疫性,炎性,代谢和神经疾病以及癌症。 还公开了包含式I化合物和治疗方法的组合物,其包括向有需要的受试者施用治疗有效量的式I化合物。
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公开(公告)号:US08268840B2
公开(公告)日:2012-09-18
申请号:US12387181
申请日:2009-04-29
申请人: Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
发明人: Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
IPC分类号: A01N43/90 , A61K31/519 , C07D471/00
CPC分类号: C07D471/04
摘要: This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R1, R2, R3, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.
摘要翻译: 本申请公开了根据式I的新型嘧啶基吡啶酮衍生物,其中A,R1,R2,R3和m如本文所述限定,其抑制JNK。 本文公开的化合物可用于调节JNK的活性并治疗与过量JNK活性相关的疾病。 这些化合物可用于治疗自身免疫性,炎性,代谢和神经疾病以及癌症。 还公开了包含式I化合物和治疗方法的组合物,其包括向有需要的受试者施用治疗有效量的式I化合物。
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公开(公告)号:US07749994B2
公开(公告)日:2010-07-06
申请号:US11503405
申请日:2006-08-14
申请人: Thomas E. Rawson , Brian Safina , Jennafer Dotson , Aihe Zhou , Ignacio Aliagas-Martin , Jason Halladay , Jun Liang , Matthias Rueth , Bing-Yan Zhu , Frederick Brookfield , Michael Prime , Birong Zhang , Jun M. Li
发明人: Thomas E. Rawson , Brian Safina , Jennafer Dotson , Aihe Zhou , Ignacio Aliagas-Martin , Jason Halladay , Jun Liang , Matthias Rueth , Bing-Yan Zhu , Frederick Brookfield , Michael Prime , Birong Zhang , Jun M. Li
IPC分类号: A61K31/55 , A61K31/538 , A61K31/424 , A61K31/4188 , C07D498/22
CPC分类号: C07D487/04 , C07D491/04
摘要: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.
摘要翻译: 本发明提供新的激酶抑制剂,其可用作例如治疗恶性肿瘤的治疗剂,其中化合物具有通式I,其中A,X,Y,Z,R a,R b,R c,R 1,R 2,R 3和m定义 这里。
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公开(公告)号:US07226923B2
公开(公告)日:2007-06-05
申请号:US11233311
申请日:2005-09-23
申请人: Edward Boyd , Frederick Brookfield , Guy Georges , Bernhard Goller , Sabine Huensch , Petra Rueger , Matthias Rueth , Stefan Scheiblich , Christine Schuell , Wolfgang von der Saal , Justin Warne , Stefan Weigand
发明人: Edward Boyd , Frederick Brookfield , Guy Georges , Bernhard Goller , Sabine Huensch , Petra Rueger , Matthias Rueth , Stefan Scheiblich , Christine Schuell , Wolfgang von der Saal , Justin Warne , Stefan Weigand
IPC分类号: C07D403/12 , C07D403/14 , A61K31/502
CPC分类号: C07D403/12
摘要: Compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates are disclosed. Also disclosed are methods for the preparation of the above-mentioned compounds, pharmaceutical compositions containing them, as well as the use of the above-mentioned compounds in the treatment, control or prevention of illnesses such as cancer.
摘要翻译: 公开了式I化合物的药学上可接受的盐,对映体形式,非对映异构体和外消旋体。 还公开了制备上述化合物的方法,含有它们的药物组合物,以及上述化合物在治疗,控制或预防诸如癌症等疾病中的用途。
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公开(公告)号:US20060270874A1
公开(公告)日:2006-11-30
申请号:US11414042
申请日:2006-04-28
申请人: Edward Boyd , Frederick Brookfield , Jonathan Gridley , Matthias Koerner , Manfred Kubbies , Raymond Lau , Ulrike Reiff , Georg Tiefenthaler , Wolfgang von der Saal , Timothy Woodcock
发明人: Edward Boyd , Frederick Brookfield , Jonathan Gridley , Matthias Koerner , Manfred Kubbies , Raymond Lau , Ulrike Reiff , Georg Tiefenthaler , Wolfgang von der Saal , Timothy Woodcock
IPC分类号: C07C311/45
CPC分类号: C07C311/51
摘要: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.
摘要翻译: 本发明涉及式I化合物:其药学上可接受的盐或酯,对映体形式,非对映异构体和外消旋物,上述化合物的制备,含有它们的药物组合物及其制备,以及这些化合物在 控制或预防癌症等疾病。
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公开(公告)号:US20050256151A1
公开(公告)日:2005-11-17
申请号:US11020793
申请日:2004-12-23
申请人: Barbara Salom , Matteo D'Anello , Maria Brasca , Patrizia Giordano , Katia Martina , Francesco Angelucci , Frederick Brookfield , William Trigg , Edward Boyd , Jonathan Larard
发明人: Barbara Salom , Matteo D'Anello , Maria Brasca , Patrizia Giordano , Katia Martina , Francesco Angelucci , Frederick Brookfield , William Trigg , Edward Boyd , Jonathan Larard
IPC分类号: C07D471/04 , G01N33/53 , A61K31/4745 , C07D471/02
CPC分类号: C07D471/04
摘要: Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
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公开(公告)号:US08883785B2
公开(公告)日:2014-11-11
申请号:US13575019
申请日:2011-01-20
申请人: Celia Dominguez , Leticia M. Toledo-Sherman , Dirk Winkler , Frederick Brookfield , Paula C. De Aguiar Pena
发明人: Celia Dominguez , Leticia M. Toledo-Sherman , Dirk Winkler , Frederick Brookfield , Paula C. De Aguiar Pena
IPC分类号: C07D403/04 , C07D413/04 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4245 , C07D401/04 , C07D417/04
CPC分类号: C07D403/04 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4245 , C07D401/04 , C07D413/04 , C07D417/04
摘要: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
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公开(公告)号:US20130116216A1
公开(公告)日:2013-05-09
申请号:US13509783
申请日:2010-11-12
申请人: Celia Dominguez , John Wityak , Michael Prime , Stephen Martin Courtney , Christopher Yarnold , Frederick Brookfield , Richard Marston , Douglas Macdonald
发明人: Celia Dominguez , John Wityak , Michael Prime , Stephen Martin Courtney , Christopher Yarnold , Frederick Brookfield , Richard Marston , Douglas Macdonald
IPC分类号: A61K31/55 , A61K31/496 , C07D401/02 , A61K31/45 , C07D413/02 , C07D403/04 , A61K31/5377 , A61K31/495
CPC分类号: C07C311/46 , C07C2601/14 , C07D211/34 , C07D211/54 , C07D211/58 , C07D211/96 , C07D213/38 , C07D213/40 , C07D213/56 , C07D215/38 , C07D217/14 , C07D217/22 , C07D239/42 , C07D263/58 , C07D277/42 , C07D295/205 , C07D295/26 , C07D307/52 , C07D401/04 , C07D487/04 , C07D495/04
摘要: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
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公开(公告)号:US20100120840A1
公开(公告)日:2010-05-13
申请号:US11989272
申请日:2006-07-28
申请人: Edward Boyd , Frederick Brookfield , Jonathan Gridley , Konrad Honold , Raymond Lau , Stefan Scheiblich
发明人: Edward Boyd , Frederick Brookfield , Jonathan Gridley , Konrad Honold , Raymond Lau , Stefan Scheiblich
IPC分类号: A61K31/437 , C07D471/04 , A61P35/00 , A61P37/02
CPC分类号: C07D471/04
摘要: Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
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公开(公告)号:US20070232681A1
公开(公告)日:2007-10-04
申请号:US10573670
申请日:2004-10-13
申请人: David Middlemiss , Mark Ashton , Edward Boyd , Frederick Brookfield , Richard Armer , Eric Pettipher
发明人: David Middlemiss , Mark Ashton , Edward Boyd , Frederick Brookfield , Richard Armer , Eric Pettipher
IPC分类号: A61K31/40 , A61K31/405 , C07D209/04 , C07D209/34
CPC分类号: C04B35/632 , C07D209/30 , C07D401/12 , C07D403/12 , C07D417/12
摘要: Compounds of general formula (I): wherein R1, R2, R3 and R4 are independently hydrogen, halo, C1-C6 alkyl, —O(C1-C6 alkyl), —CON(R9)2, —SOR9, —SO2R9, —SO2N(R9)2, —N(R9)2, —NR9COR9, —CO2R9, —COR9, —SR9, —OH, —NO2 or —CN; each R9 is independently hydrogen or C1-C6 alkyl; R5 and R6 are each independently hydrogen, or C1-C6 alkyl or together with the carbon atom to which they are attached form a C3-C7 cycloalkyl group; R7 is hydrogen or C1-C6 alkyl n is 1 or 2; X is a bond or, when n is 2, X may also be a NR9 group; wherein R9 is as defined above; when X is a bond R8 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, biphenyl or a 9-14 membered bicyclic or tricyclic heteroaryl group; when X is a NR9 group R8 may additionally be phenyl, naphthyl or a 5-7 membered heteroaromatic ring; and the R8 group is optionally substituted with one or more substituents selected from halo, C1-C6 alkyl, —O(C1-C6)alkyl, aryl, —O-aryl, heteroaryl, —O-heteroaryl, —CON(R9)2, —SOR9, —SO2R9, SO2N(9)2, —N(9)2, —NR9COR9, —CO2R9, —COR9, —SR9, —OH, —NO2 or —CN; wherein R9 is as defined above; and their pharmaceutically acceptable salts, hydrates, solvates, complexes and prodrugs are useful in the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
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