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1. 发明申请

US20120077863A1 GUANIDINO-SUBSTITUTED BI-AND POLYPHENYLS AS SMALL MOLECULE CARRIERS 审中-公开
标题翻译：作为小分子载体的甘氨酸取代的双 - 聚双环
公开(公告)号：US20120077863A1
公开(公告)日：2012-03-29
申请号：US13203667
申请日：2010-03-01
申请人： David Selwood , Roberta Worthington , Anne-Sophie Rebstock , Michela Simone , Matt Gooding , Henry Dube , Kai Stoeber , Slavica Tudzarova , Christoffer Boshoff , Gareth Williams , Sarah Kingsbury , Dimitrios Lagos , Juan Manuel Funes Quesada
发明人： David Selwood , Roberta Worthington , Anne-Sophie Rebstock , Michela Simone , Matt Gooding , Henry Dube , Kai Stoeber , Slavica Tudzarova , Christoffer Boshoff , Gareth Williams , Sarah Kingsbury , Dimitrios Lagos , Juan Manuel Funes Quesada
IPC分类号： A61K31/713 , C12N5/071 , A61K31/155 , C07C279/08 , C07H21/02
CPC分类号： C07D277/18 , C07C279/08 , C07C279/24 , C07C323/60 , Y02P20/55
摘要： A compound of formula I, or a pharmaceutically acceptable salt thereof, wherein —X1, X2 and X3 are each independently where Y is an alkylene, alkenylene or alkynylene group, each of which may be optionally substituted with one or more substituents selected from alkyl, halo, CF3, OH, alkoxy, NH2, CN, NO2 and COOH; W is absent or is O, S or NH; R1, R2, R3 and R4 are each independently selected from H, alkyl, aryl and a protecting group Pi; R7, R8 and R9 are each independently selected from H, alkyl, halo, CF3, OH, alkoxy, CN, NO2 and COOH; —q is 1, 2, 3 or 4; q′ is 0, 1, 2 or 3, where q+q′ equals 4; p and r are each independently 1, 2, 3, 4 or 5; p′ and r′ are each independently 0, 1, 2, 3 or 4, where p+p′ and r+r′ each equal 5; and —n is 0, 1, 2, 3, 4, 5 or 6.
摘要翻译：式I化合物或其药学上可接受的盐，其中-X1，X2和X3各自独立地为Y为亚烷基，亚烯基或亚炔基，其各自可以任选地被一个或多个选自烷基，卤素，CF 3，OH，烷氧基，NH 2，CN，NO 2和COOH; W不存在或是O，S或NH; R1，R2，R3和R4各自独立地选自H，烷基，芳基和保护基团Pi; R 7，R 8和R 9各自独立地选自H，烷基，卤素，CF 3，OH，烷氧基，CN，NO 2和COOH; -q为1,2,3或4; q'为0,1,2或3，其中q + q'等于4; p和r各自独立地为1,2,3,4或5; p'和r'各自独立地为0,1,2,3或4，其中p + p'和r + r'各自等于5; 和-n是0，1，2，3，4，5或6。

2. 发明申请

US20080260756A1 Peptide Inhibitors of iASPP 失效
标题翻译： iASPP的肽抑制剂
公开(公告)号：US20080260756A1
公开(公告)日：2008-10-23
申请号：US12043058
申请日：2008-03-05
申请人： Xin Lu , Patricia Kuwabara , David Selwood
发明人： Xin Lu , Patricia Kuwabara , David Selwood
IPC分类号： A61K38/16 , C07K14/00 , G01N33/68 , C07K7/06 , C07K7/08 , A61K38/08 , A61K38/10 , A61K39/395 , A61P35/00
CPC分类号： A61K38/1709 , A61K38/193 , A61K38/50 , C07K14/4747 , A61K2300/00
摘要： The invention relates to a polypeptide or part thereof which inhibits the apoptotic activity of the tumor suppressor protein p53, and includes screening methods to identify agents which interfere with the activity of the polypeptide.
摘要翻译：本发明涉及抑制肿瘤抑制蛋白p53的凋亡活性的多肽或其部分，并且包括鉴定干扰多肽活性的试剂的筛选方法。

3. 发明申请

US20130123356A1 MODULATOR 有权
标题翻译：调制器
公开(公告)号：US20130123356A1
公开(公告)日：2013-05-16
申请号：US13654942
申请日：2012-10-18
申请人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
发明人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
IPC分类号： C07C255/44 , C07C237/42 , C07C235/84 , C07C69/78 , C07C235/42 , C07C233/69
CPC分类号： C07C235/42 , A61K31/165 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof,
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，

4. 发明授权

US07790761B2 Blockade of voltage dependent sodium channels 失效
标题翻译：电压依赖性钠通道阻断
公开(公告)号：US07790761B2
公开(公告)日：2010-09-07
申请号：US11312569
申请日：2005-12-21
申请人： Giti Garthwaite , David Selwood , Marcel Kling , Grant Wishart
发明人： Giti Garthwaite , David Selwood , Marcel Kling , Grant Wishart
IPC分类号： A61K31/41 , A61K31/4196 , A61K31/4166
CPC分类号： C07D417/14 , A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/422 , A61K31/4439 , C07D231/14 , C07D401/12 , C07D405/04 , C07D409/04 , C07D413/12
摘要： Compounds of Formula I and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.
摘要翻译：式I化合物及其药学上可接受的盐能够阻断电压依赖性钠通道，特别可用于治疗青光眼和多发性硬化症。

5. 发明授权

US07696382B2 Modulator 有权
标题翻译：调制器
公开(公告)号：US07696382B2
公开(公告)日：2010-04-13
申请号：US10590064
申请日：2005-02-21
申请人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
发明人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
IPC分类号： C07C233/00 , C07C229/00 , C07C255/00 , A01N37/18
CPC分类号： C07C235/42 , A61K31/165 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C≡—C—(CH2)2CO2H, meta-C≡—C—(CH2)2OH, meta-C≡C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C≡C—(CH2)4OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中Z为OR 1或NR 1 R 2，其中R 1和R 2各自独立地为H或烃基; X是亚烷基，亚烯基或亚炔基，其各自可以任选地被一个或多个选自烷基，COOH，CO 2 - 烷基，烯基，CN，NH 2，羟基，卤素，烷氧基，CF 3和硝基的取代基取代; Y是选自OH，NO2，CN，COR3，COOR3，NR3R4，CONR3R4，SO3H，SO2-R3，SO2NR3R4和CF3的极性官能团，其中R3和R4各自独立地为H或烃基; A是芳基或杂芳基，其各自可以任选被取代; 和B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A是苯基时，n是0，Z是OH，X-Y不是间位-C≡-C-（CH 2）2 CO 2 H，间-C≡C-（CH 2）（CH 2）2 CO 2 Me，间 - （CH 2）4 CO 2 H，邻-CH 2 CO 2 H，邻 - （CH 2）2 CO 2 H和邻 - （CH 2）4 CO 2 H; 和（ii）当A是苯基时，n是0，Z是OMe，X-Y不是间位-C≡C-（CH 2）4 OH。本发明的其它方面涉及这样的化合物在制备用于治疗肌肉疾病，胃肠道疾病或用于控制痉挛或震颤的药物中的用途。

6. 发明申请

US20080114062A1 Modulator 有权
公开(公告)号：US20080114062A1
公开(公告)日：2008-05-15
申请号：US10590064
申请日：2005-02-21
申请人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
发明人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
IPC分类号： A61K31/166 , C07C233/68 , C07C255/40 , C07C233/66 , A61P21/00 , A61P43/00 , G01N33/566 , A61K31/235 , A61P1/00 , A61K31/216 , A61K31/192
CPC分类号： C07C235/42 , A61K31/165 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C≡—C—(CH2)2CO2H, meta-C≡—C—(CH2)2OH, meta-C≡C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C≡C—(CH2)4OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.

7. 发明授权

US07223835B2 VEGF peptides and their use for inhibiting angiogenesis 失效
标题翻译： VEGF肽及其用于抑制血管生成的用途
公开(公告)号：US07223835B2
公开(公告)日：2007-05-29
申请号：US10398616
申请日：2001-10-25
申请人： David Selwood , Ian Zachary , Haiyan Jia , Marianne Lohr , Dana Davis
发明人： David Selwood , Ian Zachary , Haiyan Jia , Marianne Lohr , Dana Davis
IPC分类号： A61K38/00 , A61K38/12 , A61K38/04 , A01N37/18 , C07K5/00
CPC分类号： C07K14/521 , A61K38/00
摘要： A peptide having part or all of the amino acid sequence QKRKRKKSRYKSWSVP (which is part of VEGF) has the ability to inhibit angiogenesis.
摘要翻译：具有部分或全部氨基酸序列QKRKRKKSRYKSWSVP（其是VEGF的一部分）的肽具有抑制血管发生的能力。

8. 发明授权

US07009056B2 Blockade of voltage dependent sodium channels 失效
标题翻译：电压依赖性钠通道阻断
公开(公告)号：US07009056B2
公开(公告)日：2006-03-07
申请号：US10203001
申请日：2001-02-05
申请人： Giti Garthwaite , David Selwood , Marcel Kling , Grant Wishart
发明人： Giti Garthwaite , David Selwood , Marcel Kling , Grant Wishart
IPC分类号： C07D401/14 , C07D231/12 , C07D231/10 , C07D249/12
CPC分类号： C07D417/14 , A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/422 , A61K31/4439 , C07D231/14 , C07D401/12 , C07D405/04 , C07D409/04 , C07D413/12
摘要： Compounds of formula (I), and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.
摘要翻译：式（I）化合物及其药学上可接受的盐能够阻断电压依赖性钠通道，并且特别可用于治疗青光眼和多发性硬化。

9. 发明授权

US08293796B2 Modulator 有权
标题翻译：调制器
公开(公告)号：US08293796B2
公开(公告)日：2012-10-23
申请号：US12707812
申请日：2010-02-18
申请人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
发明人： Masahiro Okuyama , David Selwood , Cristina Visintin , David Baker , Gareth Pryce
IPC分类号： A01N37/18
CPC分类号： C07C235/42 , A61K31/165 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C≡—C—(CH2)2CO2H, meta-C≡—C—(CH2)2OH, meta-C≡C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C≡C—(CH2)4OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中Z为OR 1或NR 1 R 2，其中R 1和R 2各自独立地为H或烃基; X是亚烷基，亚烯基或亚炔基，其各自可以任选地被一个或多个选自烷基，COOH，CO 2 - 烷基，烯基，CN，NH 2，羟基，卤素，烷氧基，CF 3和硝基的取代基取代; Y是选自OH，NO2，CN，COR3，COOR3，NR3R4，CONR3R4，SO3H，SO2-R3，SO2NR3R4和CF3的极性官能团，其中R3和R4各自独立地为H或烃基; A是芳基或杂芳基，其各自可以任选被取代; 和B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A是苯基时，n是0，Z是OH，X-Y不是间位-C≡-C-（CH 2）2 CO 2 H，间-C≡C-（CH 2）（CH 2）2 CO 2 Me，间 - （CH 2）4 CO 2 H，邻-CH 2 CO 2 H，邻 - （CH 2）2 CO 2 H和邻 - （CH 2）4 CO 2 H; 和（ii）当A是苯基时，n是0，Z是OMe，X-Y不是间位-C≡C-（CH 2）4 OH。本发明的其它方面涉及这样的化合物在制备用于治疗肌肉疾病，胃肠道疾病或用于控制痉挛或震颤的药物中的用途。

10. 发明申请

US20120157385A1 CYCLOSPORIN CONJUGATES 审中-公开
标题翻译：环孢素联合
公开(公告)号：US20120157385A1
公开(公告)日：2012-06-21
申请号：US13386317
申请日：2010-07-19
申请人： David Selwood , Martin Crompton
发明人： David Selwood , Martin Crompton
IPC分类号： A61K38/13 , C12Q1/02 , A61P9/10 , G01N33/53 , C07K7/64 , A61P25/28
CPC分类号： C07K7/64 , A61K47/54 , A61K47/545 , A61K47/55 , A61K47/64 , C09B11/24 , C09B69/001 , G01N33/9493 , G01N2410/08
摘要： A conjugate which comprises a cyclosporin moiety of formula (I) linked to one or more mitochondrial targeting groups, or a pharmaceutically acceptable salt thereof: wherein: A represents or, B represents methyl or ethyl, one Of R1 and R1 represents hydrogen and the other represents methyl, R2 represents ethyl or isopropyl, R3 represents hydrogen or methyl, and R4 represents —CH2CH(CH3)CH3, —CH2CH(CH3)CH2CH3, —CH(CH3)CH3 or —CH(CH3)CH2CH3.
摘要翻译：一种缀合物，其包含与一个或多个线粒体靶向基团连接的式（I）的环孢菌素部分或其药学上可接受的盐：其中：A表示或者，B表示甲基或乙基，R1和R1表示氢，另一个表示甲基，R 2表示乙基或异丙基，R 3表示氢或甲基，R 4表示-CH 2 CH（CH 3）CH 3，-CH 2 CH（CH 3）CH 2 CH 3，-CH（CH 3）CH 3或-CH（CH 3）CH 2 CH 3。

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