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1.Optically active pyridine derivative and a medicament containing the same 审中-公开
Title translation: 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
Applicant: Toshiki Murata , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Yuji Koriyama , Noriko Nunami , Megumi Yamauchi , Keiko Fukushima , Rolf Grosser , Kinji Fuchikami , Kevin Bacon , Timothy Lowinger
Inventor: 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: A61K31/5365 , C12N9/99 , A61P35/00 , A61P37/06
CPC classification number: C07D498/04
Abstract: 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.
Abstract translation: 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
Applicant: 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
Inventor: 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: A61K31/444 , A61K31/4436 , C07D409/02 , C07D401/02
CPC classification number: 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
Abstract: 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.
Abstract translation: 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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3.OMEGA-CARBOXYARL SUBSTITUTED DIPHENYL UREAS AS RAF KINASE INHIBITORS 审中-公开
Title translation: 作为RAF激酶抑制剂的OMEGA-CARBOXYARL替代二苯醚公开(公告)号:US20140329866A1
公开(公告)日:2014-11-06
申请号:US14333533
申请日:2014-07-17
Applicant: Bernd RIEDL , Jacques DUMAS , Uday KHIRE , Timothy LOWINGER , William J. SCOTT , Roger A. SMITH , Jill E. WOOD
Inventor: Bernd RIEDL , Jacques DUMAS , Uday KHIRE , Timothy LOWINGER , William J. SCOTT , Roger A. SMITH , Jill E. WOOD
IPC: C07C275/36 , C07D209/46 , C07D213/82 , C07D213/81 , C07D413/12 , C07D209/48 , C07D213/75
CPC classification number: C07C275/36 , C07C275/28 , C07C275/30 , C07C275/32 , C07C275/40 , C07C311/29 , C07C317/22 , C07D209/46 , C07D209/48 , C07D213/75 , C07D213/81 , C07D213/82 , C07D295/13 , C07D295/135 , C07D295/192 , C07D413/12
Abstract: 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.
Abstract translation: 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.Hydroxy, ω-carboxyaryl substituted diphenyl ureas and dirivatives thereof as raf kinase inhibitors 有权
Title translation: 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
Applicant: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , William Scott , Roger Smith , Jill Wood
Inventor: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , William Scott , Roger Smith , Jill Wood
IPC: C07D211/72 , C07D213/62 , C07D213/78
CPC classification number: 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
Abstract: 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.
Abstract translation: 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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5.Omega-Carboxyaryl Substituted Diphenyl Ureas As Raf Kinease Inhibitors 审中-公开
Title translation: 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
Applicant: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , Scott William , Roger Smith , Jill Wood , Mary-Katherine Monahan , Reink Natero , Joel Renick , Robert Sibley
Inventor: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , Scott William , Roger Smith , Jill Wood , Mary-Katherine Monahan , Reink Natero , Joel Renick , Robert Sibley
IPC: A61K31/4035 , A61K31/17 , A61K31/44 , A61K31/5377 , A61P35/00 , C07C275/28 , C07D209/48 , C07D213/62 , C07D413/12
CPC classification number: 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
Abstract: 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.
Abstract translation: 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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公开(公告)号:US20060205676A1
公开(公告)日:2006-09-14
申请号:US11240867
申请日:2005-09-30
Applicant: 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
Inventor: 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: A61K31/7052 , A61K31/444 , A61K31/4436
CPC classification number: 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
Abstract: 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.
Abstract translation: 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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7.Arylsulfonamide derivatives for use as ccr3 antagonists in the treatment of inflammatory and immunological disorders 失效
Title translation: 用作治疗炎症和免疫疾病的ccr3拮抗剂的芳基磺酰胺衍生物公开(公告)号:US20050070582A1
公开(公告)日:2005-03-31
申请号:US10489029
申请日:2002-09-04
Applicant: Yingfu Li , Akihiko Watanabe , Timothy Lowinger , Kevin Bacon , Norihiro Kawamura , Takuya Shintani , Tetsuo Kikuchi , Toshiya Moriwaki , Klaus Urbahns , Keiko Fukushima , Noriko Nunami , Takashi Yoshino , Toshiki Murata , Megumi Yamauchi , Hiroko Yoshino
Inventor: Yingfu Li , Akihiko Watanabe , Timothy Lowinger , Kevin Bacon , Norihiro Kawamura , Takuya Shintani , Tetsuo Kikuchi , Toshiya Moriwaki , Klaus Urbahns , Keiko Fukushima , Noriko Nunami , Takashi Yoshino , Toshiki Murata , Megumi Yamauchi , Hiroko Yoshino
IPC: A61K31/18 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/437 , A61K31/4375 , A61K31/4406 , A61K31/445 , A61K31/4453 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/4985 , A61K31/5375 , A61K31/551 , A61P5/16 , A61P9/10 , A61P11/02 , A61P11/06 , A61P25/28 , A61P27/16 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07C311/29 , C07C323/67 , C07D207/14 , C07D207/48 , C07D209/08 , C07D209/44 , C07D211/14 , C07D211/26 , C07D211/28 , C07D211/58 , C07D211/96 , C07D213/65 , C07D213/70 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D241/04 , C07D241/06 , C07D243/08 , C07D257/04 , C07D295/088 , C07D295/12 , C07D295/13 , C07D295/194 , C07D295/22 , C07D295/26 , C07D307/14 , C07D333/38 , C07D333/40 , C07D471/04 , C07D487/04 , C07D487/08 , A61K31/44 , C07D213/62
CPC classification number: C07D213/70 , C07C311/29 , C07C323/67 , C07D207/14 , C07D207/48 , C07D209/08 , C07D211/28 , C07D211/58 , C07D211/96 , C07D213/65 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D241/04 , C07D241/06 , C07D243/08 , C07D257/04 , C07D295/088 , C07D295/13 , C07D295/194 , C07D295/26 , C07D307/14 , C07D333/38 , C07D471/04 , C07D487/04 , C07D487/08
Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
Abstract translation: 本发明涉及可用作药物制剂活性成分的磺酰胺衍生物。 本发明的磺酰胺衍生物具有CCR3(CC型趋化因子受体)拮抗活性,可用于预防和治疗与CCR3活性有关的疾病,特别是用于治疗哮喘,特应性皮炎,过敏性鼻炎等炎症 /免疫学障碍。
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8.Optically active pyridine derivative and a medicament containing the same 失效
Title translation: 光学活性吡啶衍生物和含有其的药物公开(公告)号:US07375103B2
公开(公告)日:2008-05-20
申请号:US10508107
申请日:2003-03-03
Applicant: Toshiki Murata , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Yuji Koriyama , Noriko Nunami , Megumi Yamauchi , Keiko Fukushima , Rolf Grosser , Kinji Fuchikami , Kevin Bacon , Timothy Lowinger
Inventor: 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: C07D498/04 , A61K31/5365 , A61P29/00
CPC classification number: C07D498/04
Abstract: 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 (I) or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity
Abstract translation: 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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9.omega-Carboxy Aryl Substituted Diphenyl Ureas As p38 Kinase Inhibitors 有权
Title translation: 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
Applicant: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , William Scott , Roger Smith , Jill Wood , Mary-Katherine Monahan , Reina Natero , Joel Renick , Robert Sibley
Inventor: Bernd Riedl , Jacques Dumas , Uday Khire , Timothy Lowinger , William Scott , Roger Smith , Jill Wood , Mary-Katherine Monahan , Reina Natero , Joel Renick , Robert Sibley
IPC: A61K31/535 , A61K31/17 , A61P19/02 , A61K31/495
CPC classification number: 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
Abstract: 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.
Abstract translation: 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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10.INHIBITION OF RAF KINASE USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS 失效
Title translation: 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
Applicant: Jacques Dumas , Uday Khire , Timothy Lowinger , Bernard Riedl , William Scott , Roger Smith , Jill Wood , Holia Hatoum-Mokdad , Jeffrey Johnson , Aniko Redman , Robert Sibley
Inventor: Jacques Dumas , Uday Khire , Timothy Lowinger , Bernard Riedl , William Scott , Roger Smith , Jill Wood , Holia Hatoum-Mokdad , Jeffrey Johnson , Aniko Redman , Robert Sibley
IPC: A61K31/4439 , A61K31/415 , A61P35/00 , C07D401/12 , C07D405/04 , C07D231/38 , A61K31/443
CPC classification number: C07D231/40 , C07D333/36 , C07D401/12 , C07D405/04
Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se,
Abstract translation: 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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