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1.omega-Carboxy Aryl Substituted Diphenyl Ureas As p38 Kinase Inhibitors 有权
标题翻译: ω-羧基芳基取代的二苯脲作为p38激酶抑制剂公开(公告)号:US20080027061A1
公开(公告)日:2008-01-31
申请号:US11845597
申请日:2007-08-27
申请人: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , William Scott , Roger Smith , Jill Wood , Mary-Katherine Monahan , Reina Natero , Joel Renick , Robert Sibley
发明人: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , William Scott , Roger Smith , Jill Wood , Mary-Katherine Monahan , Reina Natero , Joel Renick , Robert Sibley
IPC分类号: A61K31/535 , A61K31/17 , A61P19/02 , A61K31/495
CPC分类号: A61K31/5377 , A61K31/17 , A61K31/18 , A61K31/24 , A61K31/341 , A61K31/40 , A61K31/4035 , A61K31/44 , A61K31/4439 , A61K31/4453 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5375 , Y02A50/401 , Y02A50/411 , Y02A50/414 , Y02A50/473
摘要: This invention relates to the use of a group of aryl ureas in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.
摘要翻译: 本发明涉及一组芳基脲在治疗p38介导的疾病中的用途,以及用于此类治疗的药物组合物。
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2.
公开(公告)号:US07351834B1
公开(公告)日:2008-04-01
申请号:US09889227
申请日:2000-01-12
申请人: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , William Scott , Roger A. Smith , Jill E. Wood , Mary-Katherine Monahan , Reina Natero , Joel Renick , Robert Sibley
发明人: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , William Scott , Roger A. Smith , Jill E. Wood , Mary-Katherine Monahan , Reina Natero , Joel Renick , Robert Sibley
IPC分类号: C07D213/30 , A61K31/44
CPC分类号: C07D209/48 , C07C251/48 , C07C275/28 , C07C275/30 , C07C275/32 , C07C275/36 , C07C275/40 , C07C311/29 , C07C317/22 , C07D207/09 , C07D209/46 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/81 , C07D213/82 , C07D295/12 , C07D295/13 , C07D295/135 , C07D295/18 , C07D295/192 , C07D307/14 , C07D401/12
摘要: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
摘要翻译: 本发明涉及一组芳基脲在治疗raf介导的疾病中的用途,以及用于此类治疗的药物组合物。
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3.Omega-Carboxyaryl Substituted Diphenyl Ureas As Raf Kinease Inhibitors 审中-公开
标题翻译: ω-羧酰基取代的二苯基脲作为Raf Kinease抑制剂公开(公告)号:US20080032979A1
公开(公告)日:2008-02-07
申请号:US11845595
申请日:2007-08-27
申请人: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , Scott William , Roger Smith , Jill Wood , Mary-Katherine Monahan , Reink Natero , Joel Renick , Robert Sibley
发明人: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , Scott William , Roger Smith , Jill Wood , Mary-Katherine Monahan , Reink Natero , Joel Renick , Robert Sibley
IPC分类号: A61K31/4035 , A61K31/17 , A61K31/44 , A61K31/5377 , A61P35/00 , C07C275/28 , C07D209/48 , C07D213/62 , C07D413/12
CPC分类号: C07C275/36 , A61K31/17 , A61K31/18 , A61K31/24 , A61K31/341 , A61K31/40 , A61K31/4035 , A61K31/44 , A61K31/4439 , A61K31/4453 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , C07C275/28 , C07C275/30 , C07C275/32 , C07C275/40 , C07C311/29 , C07C317/22 , C07D209/46 , C07D209/48 , C07D209/50 , C07D213/75 , C07D213/80 , C07D213/81 , C07D213/82 , C07D295/073 , C07D295/12 , C07D295/13 , C07D295/135 , C07D295/18 , C07D295/192 , C07D401/12 , C07D413/12 , C07F7/1804
摘要: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
摘要翻译: 本发明涉及一组芳基脲在治疗raf介导的疾病中的用途,以及用于此类治疗的药物组合物。
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4.
公开(公告)号:US20070244120A1
公开(公告)日:2007-10-18
申请号:US11768112
申请日:2007-06-25
申请人: Jacques Dumas , Uday Khire , Timothy Lowinger , Holger Paulsen , Bernd Riedl , William Scott , Roger Smith , Jill Wood , Holia Hatoum-Mokdad , Jeffrey Johnson , Wendy Lee , Aniko Redman , Robert Sibley , Joel Renick
发明人: Jacques Dumas , Uday Khire , Timothy Lowinger , Holger Paulsen , Bernd Riedl , William Scott , Roger Smith , Jill Wood , Holia Hatoum-Mokdad , Jeffrey Johnson , Wendy Lee , Aniko Redman , Robert Sibley , Joel Renick
IPC分类号: A61K31/5377 , A61K31/09 , A61K31/136 , A61K31/381 , A61K31/4164 , A61K31/4196 , A61K31/42 , A61K31/426 , C07D401/12 , C07D231/10 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/497
CPC分类号: C07D231/40 , C07D207/34 , C07D259/00 , C07D261/14 , C07D271/113 , C07D285/135 , C07D333/36 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
摘要翻译: 治疗由raf激酶介导的肿瘤与取代的脲化合物及其化合物本身的方法。
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5.Hydroxy, ω-carboxyaryl substituted diphenyl ureas and dirivatives thereof as raf kinase inhibitors 有权
标题翻译: 羟基,ω-羧基芳基取代的二苯基脲和其衍生物作为raf激酶抑制剂公开(公告)号:US07528255B2
公开(公告)日:2009-05-05
申请号:US10071248
申请日:2002-02-11
申请人: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , William Scott , Roger Smith , Jill Wood
发明人: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , William Scott , Roger Smith , Jill Wood
IPC分类号: C07D211/72 , C07D213/62 , C07D213/78
CPC分类号: C07D295/192 , A61K31/17 , A61K31/18 , A61K31/24 , A61K31/341 , A61K31/40 , A61K31/4035 , A61K31/44 , A61K31/4439 , A61K31/4453 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , C07C275/28 , C07C275/30 , C07C275/32 , C07C275/36 , C07C275/40 , C07C311/29 , C07C317/22 , C07D209/46 , C07D209/48 , C07D209/50 , C07D213/75 , C07D213/80 , C07D213/81 , C07D295/073 , C07D295/12 , C07D295/13 , C07D295/135 , C07D295/18 , C07D401/12 , C07F7/1804
摘要: The invention relates to the use of a group of aryl ureas in treating raf mediated diseases and pharmaceutical compositions for use in such therapy of the formula wherein, Y is NHR Hal is chlorine or bromine, R is H, CH3 or CH2OH, and X1 to X7 are each, independently, H, OH or —OC(O)C1-C4 alkyl, or a salt purified stereoisomer thereof, wherein at least one of X1 to X7 is OH or —OC(O)C1-C4 alkyl.
摘要翻译: 本发明涉及一组芳基脲在治疗raf介导的疾病中的用途以及用于下列治疗的药物组合物:其中Y是NHR Hal是氯或溴,R是H,CH3或CH2OH,X1至 X 7各自独立地为H,OH或-OC(O)C 1 -C 4烷基或其盐纯化的立体异构体,其中X 1至X 7中的至少一个为OH或-OC(O)C 1 -C 4烷基。
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6.INHIBITION OF RAF KINASE USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS 失效
标题翻译: 使用ARYL和HETEROARYL取代的杂环类URAAS对RAF激酶的抑制作用公开(公告)号:US20080009527A1
公开(公告)日:2008-01-10
申请号:US11768533
申请日:2007-06-26
申请人: Jacques Dumas , Uday Khire , Timothy Lowinger , Bernard Riedl , William Scott , Roger Smith , Jill Wood , Holia Hatoum-Mokdad , Jeffrey Johnson , Aniko Redman , Robert Sibley
发明人: Jacques Dumas , Uday Khire , Timothy Lowinger , Bernard Riedl , William Scott , Roger Smith , Jill Wood , Holia Hatoum-Mokdad , Jeffrey Johnson , Aniko Redman , Robert Sibley
IPC分类号: A61K31/4439 , A61K31/415 , A61P35/00 , C07D401/12 , C07D405/04 , C07D231/38 , A61K31/443
CPC分类号: C07D231/40 , C07D333/36 , C07D401/12 , C07D405/04
摘要: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se,
摘要翻译: 用raf激酶介导的肿瘤治疗方法,用取代的脲化合物和这些化合物本身,
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7.Optically active pyridine derivative and a medicament containing the same 审中-公开
标题翻译: 光学活性吡啶衍生物和含有其的药物公开(公告)号:US20090054424A1
公开(公告)日:2009-02-26
申请号:US12123405
申请日:2008-05-19
申请人: Toshiki Murata , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Yuji Koriyama , Noriko Nunami , Megumi Yamauchi , Keiko Fukushima , Rolf Grosser , Kinji Fuchikami , Kevin Bacon , Timothy Lowinger
发明人: Toshiki Murata , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Yuji Koriyama , Noriko Nunami , Megumi Yamauchi , Keiko Fukushima , Rolf Grosser , Kinji Fuchikami , Kevin Bacon , Timothy Lowinger
IPC分类号: A61K31/5365 , C12N9/99 , A61P35/00 , A61P37/06
CPC分类号: C07D498/04
摘要: An optically active (−)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido[2,3-d][1,3]oxazin-2-one of the formula: or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
摘要翻译: 光学活性( - ) - 7- [2-(环丙基甲氧基)-6-羟基苯基] -5 - [(3S)-3-哌啶基] -1,4-二氢-2H-吡啶并[2,3-d] 1,3]恶嗪-2-酮或其盐。 该化合物具有优异的抗炎活性和其他生物活性。
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公开(公告)号:US20060100246A1
公开(公告)日:2006-05-11
申请号:US11240728
申请日:2005-09-30
申请人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy Lowinger , Karl Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
发明人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy Lowinger , Karl Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
IPC分类号: A61K31/444 , A61K31/4436 , C07D409/02 , C07D401/02
CPC分类号: C07D213/08 , C07D213/10 , C07D213/73 , C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D513/04 , C07D515/04
摘要: This invention is to provide a process for producing 2-amino-4,6-disubstituted nicotinic acid ester analogs and salts thereof, comprising the reaction shown by the following scheme. The ester analogs can be prepared in one pot, and in good yield by using tertiary alkyl cyanoacetate. Furthermore, the method is useful for preparing derivatives of various analogs of the ester, e.g. alkyl substituted and aryl substituted analogs.
摘要翻译: 本发明提供一种制备2-氨基-4,6-二取代的烟酸酯类似物及其盐的方法,其包括如下方案所示的反应。 酯类似物可以在一锅中制备,并且通过使用氰基乙酸叔烷酯以良好的产率制备。 此外,该方法可用于制备酯的各种类似物的衍生物,例如。 烷基取代和芳基取代的类似物。
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公开(公告)号:US20070099929A1
公开(公告)日:2007-05-03
申请号:US11455253
申请日:2006-06-16
申请人: Kai Thede , Tobias Wunberg , Timothy Lowinger , Diana Koletzki , Andreas Urban , Judith Baumeister , Kerstin Henninger
发明人: Kai Thede , Tobias Wunberg , Timothy Lowinger , Diana Koletzki , Andreas Urban , Judith Baumeister , Kerstin Henninger
IPC分类号: A61K31/496 , A61K31/453 , A61K31/4436 , A61K31/4025 , A61K31/381 , C07D409/02
CPC分类号: C07D409/04 , C07D333/38 , C07D409/12 , C07D409/14 , C07D417/04
摘要: The invention relates to substituted thiophenes and processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular for hepatitis C viruses.
摘要翻译: 本发明涉及取代的噻吩及其制备方法,其用于治疗和/或预防疾病的用途及其用于生产用于治疗和/或预防疾病,特别是用作抗病毒剂的药物的用途 特别适用于丙型肝炎病毒。
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公开(公告)号:US20060205676A1
公开(公告)日:2006-09-14
申请号:US11240867
申请日:2005-09-30
申请人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy Lowinger , Karl Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
发明人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy Lowinger , Karl Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
IPC分类号: A61K31/7052 , A61K31/444 , A61K31/4436
CPC分类号: C07D213/08 , C07D213/10 , C07D213/73 , C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D513/04 , C07D515/04
摘要: Pyrimidine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
摘要翻译: 其中R 1表示其中R 11为氢,C 1-6烷基,卤素,羟基,C 1 -C 6烷基, 1-12烷氧基,硝基,氨基,C 1-6烷基磺酰基氨基,C 1-6烷氧基羰基,C 1-6烷基, (C 1-6烷基)氨基,C 1-6烷酰基氨基,苯基C 1-6烷基氨基,苯基磺酰基氨基,C 1 -C 6烷基氨基, ,或-O-(CH 2)n - n - R 111; R 2表示氢或卤素; R 3表示氢,-CR 31,32,32,33, R 4是氢,氨基甲酰基,CN,羧基等; R 5是氨基,C 1-6烷基氨基,C 1-6烷基氨基等,或其盐。 该化合物具有优异的抗炎活性和其他生物活性。
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