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公开(公告)号:US20190099392A1
公开(公告)日:2019-04-04
申请号:US15963599
申请日:2018-04-26
IPC分类号: A61K31/18 , C07D471/08 , A61K51/10 , C07C311/29 , C07C311/42 , C07C311/46 , C07C323/60 , C07D207/48 , C07D211/60 , C07C309/14 , C07C259/06 , C07D211/96 , C07D213/42 , C07D213/74 , C07D213/89 , C07D215/36 , C07D223/06 , C07D277/06 , C07D277/80 , C07D279/12 , C07D295/13 , C07D309/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D453/06 , C07D487/08 , C07C311/19
CPC分类号: A61K31/18 , A61K51/1051 , C07C259/06 , C07C309/14 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C323/60 , C07C2601/04 , C07D207/48 , C07D211/60 , C07D211/96 , C07D213/42 , C07D213/74 , C07D213/89 , C07D215/36 , C07D223/06 , C07D277/06 , C07D277/80 , C07D279/12 , C07D295/13 , C07D309/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D453/06 , C07D471/08 , C07D487/08 , C07K17/06
摘要: The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.
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公开(公告)号:US09980930B2
公开(公告)日:2018-05-29
申请号:US15518333
申请日:2015-10-16
IPC分类号: A61K31/18 , C07C311/46 , C07D211/96 , C07D211/60 , C07D471/08 , C07D277/80 , C07D213/89 , C07C311/42 , C07D215/36 , C07D405/12 , C07C323/60 , C07D309/06 , C07D207/48 , C07D295/13 , C07D401/12 , C07D453/06 , C07D223/06 , C07C311/19 , C07D279/12 , C07D413/12 , C07D213/42 , C07D213/74 , C07C311/29 , C07D277/06 , C07D487/08 , C07C247/14 , C07C235/74
CPC分类号: A61K31/18 , A61K51/1051 , C07C259/06 , C07C309/14 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C323/60 , C07C2601/04 , C07D207/48 , C07D211/60 , C07D211/96 , C07D213/42 , C07D213/74 , C07D213/89 , C07D215/36 , C07D223/06 , C07D277/06 , C07D277/80 , C07D279/12 , C07D295/13 , C07D309/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D453/06 , C07D471/08 , C07D487/08
摘要: The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.
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公开(公告)号:US20150225355A1
公开(公告)日:2015-08-13
申请号:US14694147
申请日:2015-04-23
发明人: George D. Hartman
IPC分类号: C07D267/10 , A61K31/55 , A61K45/06 , C07D223/06 , C07D223/32 , A61K31/439 , A61K31/553 , C07D243/08 , A61K31/551 , C07D223/08 , C07D221/22
CPC分类号: C07D223/08 , A61K31/439 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , A61K38/21 , A61K45/06 , A61K47/60 , C07D221/22 , C07D223/06 , C07D223/32 , C07D243/08 , C07D267/10 , C07D283/00 , C07D295/26 , C07D403/12 , A61K2300/00
摘要: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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公开(公告)号:US07408067B2
公开(公告)日:2008-08-05
申请号:US10500517
申请日:2002-07-29
申请人: Peter Charles Astles , Stephen Richard Baker , Celine Bonnefous , Jean Michel Vernier , Martine Keenan , Adam Jan Sanderson
发明人: Peter Charles Astles , Stephen Richard Baker , Celine Bonnefous , Jean Michel Vernier , Martine Keenan , Adam Jan Sanderson
IPC分类号: C07D211/22 , C07D401/00
CPC分类号: C07D401/06 , C07D207/12 , C07D211/54 , C07D223/06 , C07D401/12 , C07D405/06 , C07D413/12 , C07D417/06
摘要: Compounds comprising an aza-cyclic portion and an aromatic portion linked via a sulphur atom are disclosed. The compounds disclosed are selective modulators of beta 4 subtype nicotinic acetylcholine receptors and are useful for the treatment of dysfunctions of the central and autonomic nervous systems.
摘要翻译: 公开了包含氮杂环状部分和通过硫原子连接的芳香族部分的化合物。 所公开的化合物是β4亚型烟碱乙酰胆碱受体的选择性调节剂,并且可用于治疗中枢神经系统和自主神经系统的功能障碍。
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公开(公告)号:US20080108820A1
公开(公告)日:2008-05-08
申请号:US10572871
申请日:2004-09-22
申请人: Silvio A. Campagna , Francis G. Fang , James J. Kowalczyk , Shawn Schiller , Boris M. Seletsky , Mark Spyvee , Hu Yang
发明人: Silvio A. Campagna , Francis G. Fang , James J. Kowalczyk , Shawn Schiller , Boris M. Seletsky , Mark Spyvee , Hu Yang
IPC分类号: C07D211/60 , C07D277/06
CPC分类号: C07D207/04 , C07D207/12 , C07D207/16 , C07D207/42 , C07D209/20 , C07D211/60 , C07D217/26 , C07D223/06 , C07D233/84 , C07D237/04 , C07D241/04 , C07D265/30 , C07D277/06 , C07D279/12 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/12 , C07D471/04 , C07K5/0205 , C07K5/0207 , C07K5/0821
摘要: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.
摘要翻译: 本发明提供具有式(I)的化合物:另外提供其合成方法及其用于治疗癌症的方法,其中R 1 -R 7 X 1,X 2,R 3,Q 3和n如本文所定义。
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公开(公告)号:US20060128752A1
公开(公告)日:2006-06-15
申请号:US10520143
申请日:2003-07-02
申请人: Giuseppe Alvaro , Francesca Cardullo , Romano Di Fabio , Riccardo Giovannini , Elisabeth Piga , Maria Tranquillini
发明人: Giuseppe Alvaro , Francesca Cardullo , Romano Di Fabio , Riccardo Giovannini , Elisabeth Piga , Maria Tranquillini
IPC分类号: A61K31/445 , C07D211/06
CPC分类号: C07D211/34 , C07D211/64 , C07D223/04 , C07D223/06
摘要: The present invention relates to cyclic amine derivatives of formula(l) wherein R represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; R1 represents hydrogen, halogen, C3-7cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy; R2 represents hydrogen or C1-4 alkyl; R3 and R4 independently represent hydrogen, cyano, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl; R5 represents trifluoromethyl, S(O)t C1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano; R6 represents hydrogen or (CH2)rR7; R7 represents hydrogen, C37 cycloalkyl, NH(C1-4alkylOC1-4alkoxy), NH(C1-4alkyl), N(C1-4alkyl)2, OC(O)NR9R8, NR8C(O)R9 or C(O)NR9R8; R9 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m represents zero or an integer from 1 to 4; n represents 1 or 2; p is zero or an integer from 1 to 3; q is an integer from 1 to 3; r is an integer from 1 to 4; t is 0, 1 or 2; provided that when m is 0, p is 2, q , r and n represent 1, R1, R2,R3, R4, R5 and R7 are hydrogen and R is chlorine, R5 is not iodine; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of serotonin reuptake transporter protein.
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公开(公告)号:US06713467B2
公开(公告)日:2004-03-30
申请号:US10035714
申请日:2001-11-07
IPC分类号: A61K3133
CPC分类号: C07D401/12 , A61K45/06 , C07B2200/07 , C07C257/18 , C07D207/16 , C07D211/60 , C07D223/06
摘要: Compounds of formula I and II, or pharmaceutically-acceptable salts thereof, are useful as inhibitors of Factor VIIa, Factor IXa, Factor Xa, Factor FXIa, tryptase, and urokinase, wherein ring B is phenyl or pyridyl, L is a linker, and R1-R27, W, Z1, and Z2 are as defined in the specification.
摘要翻译: 式I和II的化合物或其药学上可接受的盐可用作因子VIIa,因子IXa,因子Xa,因子FXIa,类胰蛋白酶和尿激酶的抑制剂,其中环B是苯基或吡啶基,L是连接体,和 R1-R27,W,Z1和Z2如说明书中所定义。
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公开(公告)号:US06685617B1
公开(公告)日:2004-02-03
申请号:US09720088
申请日:2001-03-09
申请人: James Blinn , Robert Chrusciel , Jed Fisher , Steven Tanis , Edward Thomas , Thomas Lobl , Bradley Teegarden
发明人: James Blinn , Robert Chrusciel , Jed Fisher , Steven Tanis , Edward Thomas , Thomas Lobl , Bradley Teegarden
IPC分类号: A61K31425
CPC分类号: C07D207/26 , C07D205/04 , C07D207/16 , C07D207/28 , C07D211/60 , C07D211/62 , C07D223/06 , C07D263/06 , C07D277/06 , C07D277/60 , C07D279/12 , C07D281/06 , C07D401/06 , C07D405/04 , C07D405/06 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12 , C07D513/04 , C07D513/10 , C07K5/06139
摘要: The present invention relates to compound of formula (I), that are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.
摘要翻译: 本发明涉及式(I)化合物,其是α4β1介导的对VCAM或CS-1的粘附的有效抑制剂,其可用于治疗炎性疾病。 具体地说,本发明的分子可用于治疗或预防哺乳动物(例如人)中α4β1粘附介导的病症。 该方法可以包括向哺乳动物或人类患者施用有效量的本说明书中所述的化合物或组合物。
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公开(公告)号:US20030186958A1
公开(公告)日:2003-10-02
申请号:US10361115
申请日:2003-02-06
发明人: Biswanath De , Stanislaw Pikul , Menyan Cheng , Neil Gregory Almstead , Randall Stryker Matthews , Michael George Natchus , Yetunde Olabisi Taiwo
IPC分类号: A61K031/553 , A61K031/554 , A61K031/55 , C07D267/02 , C07D281/02 , C07D243/08 , C07D223/04
CPC分类号: C07D265/30 , C07D223/06 , C07D241/04 , C07D241/08 , C07D279/12 , C07D281/00 , C07D281/06 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/12 , Y02P20/582
摘要: The invention provides compounds of formula 1 as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译: 本发明提供了权利要求中所述的式的化合物或其旋光异构体,非对映异构体或其对映异构体或其药学上可接受的盐或其可生物水解的酰胺,酯或酰亚胺可用作金属蛋白酶的抑制剂。 还公开了使用这些化合物或含有它们的药物组合物治疗以金属蛋白酶活性为特征的疾病,病症和病症的药物组合物和方法。
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公开(公告)号:US5438118A
公开(公告)日:1995-08-01
申请号:US66136
申请日:1993-07-26
IPC分类号: A61K31/55 , A61K38/00 , A61K38/55 , A61P9/12 , A61P31/12 , A61P43/00 , C07C69/757 , C07D223/04 , C07D223/06 , C07D223/08 , C07D223/10 , C07D233/54 , C07D243/06 , C07D243/08 , C07K1/113 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/097 , C07K7/02 , C07K14/81 , C12N9/99 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号: C07D233/64 , C07C69/757 , C07D223/04 , C07D223/06 , C07D243/08 , C07K5/06052 , C07K5/06139 , C07K5/0821 , C07K7/02 , A61K38/00
摘要: Peptide mimics, having a constrained peptide backbone conformation, are HIV protease inhibitors. A compound of this invention is, for example, 3-Benzyl-5(alaninyl-1-aminoethyl)-2,3,6,7-tetrahydro-N-azepinyl-2-propionyl-valinyl-valinyl methyl ester.
摘要翻译: PCT No.PCT / US91 / 08850 Sec。 371日期:1993年7月26日 102(e)日期1993年7月26日PCT 1991年11月25日PCT公布。 出版物WO92 / 09297 日期:1992年6月11日。具有约束肽骨架构象的肽模拟物是HIV蛋白酶抑制剂。 本发明的化合物是例如3-苄基-5(丙烯酰基-1-氨基乙基)-2,3,6,7-四氢-N-氮杂基-2-丙酰基 - 缬氨酰基 - 缬氨酰基甲基酯。
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