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1. 发明申请

WO2005080316A3 MODULATORS OF CANNABINOID RECEPTORS 审中-公开
标题翻译：大麻素受体的调节因子
公开(公告)号：WO2005080316A3
公开(公告)日：2005-11-03
申请号：PCT/GB2005000605
申请日：2005-02-21
申请人： UNIV LONDON , OKUYAMA MASAHIRO , SELWOOD DAVID , VISINTIN CRISTINA , BAKER DAVID , PRYCE GARETH
发明人： OKUYAMA MASAHIRO , SELWOOD DAVID , VISINTIN CRISTINA , BAKER DAVID , PRYCE GARETH
IPC分类号： C07C63/04 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/68 , C07C233/69 , C07C233/77 , C07C235/42 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , A61K31/167 , A61K31/192 , A61K31/216 , A61K31/235
CPC分类号： C07C235/42 , 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 OR or NR R wherein each of R and R 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, COR , COOR , NR R , CONR R , SO3H, SO2-R , SO2NR R and CF3, where each of R and R 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为亚烷基，亚烯基或亚炔基，其各自可任选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，NO 2，CN，COR 3，COOR 3，NR 3 R 4，CONR 3 R 4，SO 3 H，SO 2 -R 3的极性官能团， SO 2 NR 3 R 4和CF 3，其中R 3和R 4各自独立地为H或烃基; A是芳基或杂芳基，它们中的每一个可以任选被取代; 并且B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A为苯基，n为0且Z为OH时，XY不是间位C = -C-（CH 2）2 CO 2 H，间位C = -C-（CH 2）2 OH，（CH 2）2 CO 2 H，间 - （CH 2）4 CO 2 H，邻 - CH 2 CO 2 H，邻 - （CH 2）2 CO 2 H和邻 - 和（ii）当A是苯基时，n是0，并且Z是OMe，X-Y不同于间位C = C-（CH 2）4 OH。本发明的其他方面涉及这些化合物在制备用于治疗肌肉疾病，胃肠疾病或用于控制痉挛状态或震颤的药物中的用途。

2. 发明申请

WO2005080316A2 MODULATOR 审中-公开
标题翻译： CANNABINOID受体的调节剂
公开(公告)号：WO2005080316A2
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000605
申请日：2005-02-21
申请人： UNIVERSITY COLLEGE LONDON , OKUYAMA, Masahiro , SELWOOD, David , VISINTIN, Cristina , BAKER, David , PRYCE, Gareth
发明人： OKUYAMA, Masahiro , SELWOOD, David , VISINTIN, Cristina , BAKER, David , PRYCE, Gareth
IPC分类号： C07C233/68
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 OR 1 or NR 1 R 2 wherein each of R 1 and R 2 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, CO 2 -alkyl, alkenyl, CN, NH 2 , hydroxy, halo, alkoxy, CF 3 and nitro; Y is a polar functional group selected from OH, NO 2 , CN, COR 3 , COOR 3 , NR 3 R 4 , CONR 3 R 4 , SO 3 H, SO 2 -R 3 , SO 2 NR 3 R 4 and CF 3 , where each of R 3 and R 4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH 2 ) 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-(CH 2 ) 2 CO 2 H, meta -C≡-C-(CH 2 ) 2 OH, meta -C≡C-(CH 2 ) 2 CO 2 Me, meta -(CH 2 ) 4 CO 2 H, ortho -CH 2 CO 2 H, ortho -(CH 2 ) 2 CO 2 H and ortho -(CH 2 ) 4 CO 2 H; and (ii) when A is phenyl, n is 0, and Z is OMe, X-Y is other than meta -C≡C-(CH 2 ) 4 OH. 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，NO 2，CN，COR 3，COOR 3，NR 3 R 4，CONR 3 R 4，SO 3 H，SO 2 -R 3的极性官能团。，SO 2 NR 3 R 4和CF 3，其中R 3和R 4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，XY不是间位-C = -C-（CH 2）2 CO 2 H，间位C = -C-（CH 2）2 OH，间 - C（C-（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些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。

3. 发明申请

WO1997005133A1 PRODRUGS OF 4-[3-(TRANS-3-DIMETHYLAMINOCYCLOBUTYL)-1H-INDOL-5-YL-METHYL]-4(S)OXAZOLIDIN-2-ONE, THEIR PREPARATION AND THEIR USE AS 5HT1-LIKE RECEPTOR AGONISTS 审中-公开
标题翻译： 4- [3-（反式-3-二甲基氨基环己基）-1H-吲哚-5-基甲基] -4（S）氧杂环丁烷-2-酮的制备及其作为5HT1样受体激动剂的制备及其用途
公开(公告)号：WO1997005133A1
公开(公告)日：1997-02-13
申请号：PCT/EP1996003251
申请日：1996-07-24
申请人： GLAXO GROUP LIMITED , SELWOOD, David, Lawrence , BLADE, Robert, John
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： The present invention provides compounds of formula (I), wherein A is a C1-6alkyl, -O-C1-6alkyl, -O-phenyl or phenyl group and may optionally be substituted by one or more substituents selected from C1-3alkyl and halogen. These compounds act as prodrugs of 4-[3-( trans -5-dimethylaminocyclobutyl)-1H-indol-5-yl-methyl]-4(S)oxazolidin-2-one. The invention is also concerned with use of compounds of formula (I) in medicine, particularly as "5HT1-like" receptor agonists for prophylaxis and treatment of migraine, pharmaceutical compounds containing them and processes for their preparation.
摘要翻译：本发明提供式（I）化合物，其中A为C 1-6烷基，-O-C 1-6烷基，-O-苯基或苯基，并且可任选被一个或多个选自C 1-3烷基和卤素的取代基取代。这些化合物作为4- [3-（反式-5-二甲基氨基环丁基）-1H-吲哚-5-基 - 甲基] -4（S）恶唑烷-2-酮的前药。本发明还涉及式（I）化合物在药物中的用途，特别是用作预防和治疗偏头痛的“5HT1样”受体激动剂，含有它们的药物化合物及其制备方法。

4. 发明申请

WO2011010084A2 CYCLOSPORIN CONJUGATES 审中-公开
标题翻译：环孢素联合
公开(公告)号：WO2011010084A2
公开(公告)日：2011-01-27
申请号：PCT/GB2010/001369
申请日：2010-07-19
申请人： UCL BUSINES PLC , SELWOOD, David , CROMPTON, Martin
发明人： SELWOOD, David , CROMPTON, Martin
IPC分类号： A61K47/48
CPC分类号： C07K7/64 , A61K47/54 , A61K47/545 , A61K47/55 , A61K47/64 , 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 R 1 and R 1* represents hydrogen and the other represents methyl, R2 represents ethyl or isopropyl, R3 represents hydrogen or methyl, and R4 represents -CH 2 CH(CH 3 )CH 3 , -CH 2 CH(CH 3 )CH 2 CH 3 , -CH(CH 3 )CH 3 or -CH(CH 3 )CH 2 CH 3 .
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，其他代表甲基，R2代表乙基或异丙基，R3代表氢或甲基，R4代表-CH2CH（CH3）CH3，-CH2CH（CH3）CH2CH3，-CH（CH3）CH3或-CH（CH3）CH2CH3。

5. 发明申请

WO2010097604A2 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2010097604A2
公开(公告)日：2010-09-02
申请号：PCT/GB2010/000359
申请日：2010-03-01
申请人： UCL BUSINESS PLC , SELWOOD, David , WORTHINGTON, Roberta , REBSTOCK, Anne-Sophie , SIMONE, Michela , GOODING, Matt , DUBE, Henry , STOEBER, Kai , TUDZAROVA, Slavica , BOSHOFF, Christoffer , WILLIAMS, Gareth , KINGSBURY, Sarah , LAGOS, Dimitrios , MANUEL FUNES QUESADA, Juan
发明人： SELWOOD, David , WORTHINGTON, Roberta , REBSTOCK, Anne-Sophie , SIMONE, Michela , GOODING, Matt , DUBE, Henry , STOEBER, Kai , TUDZAROVA, Slavica , BOSHOFF, Christoffer , WILLIAMS, Gareth , KINGSBURY, Sarah , LAGOS, Dimitrios , MANUEL FUNES QUESADA, Juan
IPC分类号： C07C279/08
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 - X 1 , X 2 and X 3 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, CF 3 , OH, alkoxy, NH 2 , CN, NO 2 and COOH; W is absent or is O, S or NH; R 1 , R 2 , R 3 and R 4 are each independently selected from H, alkyl, aryl and a protecting group Pi; R 7 , R 8 and R 9 are each independently selected from H, alkyl, halo, CF 3 , OH, alkoxy, CN, NO 2 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-X 1，X 2和X 3各自独立地为Y为亚烷基，亚烯基或亚炔基，其各自可任选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是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。

6. 发明申请

WO2008009935A1 PHARMACEUTICAL COMPOSITIONS AND THEIR USE 审中-公开
标题翻译：药物组合物及其用途
公开(公告)号：WO2008009935A1
公开(公告)日：2008-01-24
申请号：PCT/GB2007/002722
申请日：2007-07-19
申请人： UCL BUSINESS PLC , SELWOOD, David , RIDDAL, Dieter , GRIFFITHS, Charmaine , KEYNES, Robert , BELLAMY, Tomas , GARTHWAITE, John
发明人： SELWOOD, David , RIDDAL, Dieter , GRIFFITHS, Charmaine , KEYNES, Robert , BELLAMY, Tomas , GARTHWAITE, John
IPC分类号： A61K31/5415 , A61P25/16 , A61P25/28 , A61P9/10 , A61P11/06
CPC分类号： A61K31/5415
摘要： The invention relates to use of a phenothiazine derivative which is (a) a compound of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for use in treating a disorder mediated by lipid peroxidation wherein R 1 , R 2 , R 3 , R 4 , R 5 , S’, m, n, p and q are as defined herein.
摘要翻译：本发明涉及吩噻嗪衍生物的用途，其为（a）式（I）化合物或其互变异构体，或（b）其药学上可接受的盐，用于制备用于治疗由脂质过氧化，其中R 1，R 2，R 3，R 4，R 5， SUP>，S'，m，n，p和q如本文所定义。

7. 发明申请

WO2003082918A1 VEGF PEPTIDES AND THEIR USE 审中-公开
标题翻译： VEGF PEPTIDES及其用途
公开(公告)号：WO2003082918A1
公开(公告)日：2003-10-09
申请号：PCT/GB2003/001375
申请日：2003-03-28
申请人： ARK THERAPEUTICS LTD. , SELWOOD, David , LÖHR, Marianne , ZACHARY, Ian
发明人： SELWOOD, David , LÖHR, Marianne , ZACHARY, Ian
IPC分类号： C07K14/475
CPC分类号： C07K14/52 , A61K38/00
摘要： A novel peptide having the amino acid sequence SCKNTDSRCKARQLELNERTCRCDKPRR or a fragment thereof that substantially retains NP-1 antagonist activity, in cyclic form, is proposed for use in therapy.
摘要翻译：提出了一种具有基本保持NP-1拮抗剂活性的氨基酸序列SCKNTDSRCKARQLELNERTCRCDKPRR或其片段的新型肽用于治疗。

8. 发明申请

WO1995032966A1 INDOLE DERIVATIVES AS PRODRUGS OF 5-HT1-LIKE RECEPTOR AGONISTS 审中-公开
标题翻译：作为5-HT1样受体激动剂的单克隆抗体衍生物
公开(公告)号：WO1995032966A1
公开(公告)日：1995-12-07
申请号：PCT/GB1995001249
申请日：1995-05-31
申请人： THE WELLCOME FOUNDATION LIMITED , BLADE, Robert, John , PANG, Yih, Sang , SELWOOD, David, Lawrence
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： A compound of formula (I), wherein A is C1-6alkyl, -O-C1-6alkyl, -O-phenyl or phenyl, optionally substituted by C1-3alkyl or halogen; n is an integer of from 0 to 3; W is a group of formula (i), (ii) or (iii) wherein R is hydrogen or C1-4alkyl, x is -O-, -S-, -NH-, or -CH2-, Y is oxygen or sulphur and the chiral centre * in formula (i) or (ii) is in its (S) or (R) form or is a mixture thereof in any proportions; and Z is a group of formula (iv) -CH2CH2NR R , (v) or (vi) wherein R and R are independently selected from hydrogen and C1-4alkyl and R is hydrogen or C1-4alkyl; and salts, solvates and physiologically functional derivatives thereof.
摘要翻译：式（I）的化合物，其中A为C1-6烷基，-O-C1-6烷基，-O-苯基或苯基，任选被C 1-3烷基或卤素取代; n为0〜3的整数， W是式（ⅰ），（ⅱ）或（ⅲ）的基团，其中R是氢或C 1-4烷基，x是-O - ， - S - ， - NH-或-CH 2 - ，Y是氧或硫式（i）或（ii）中的手性中心*为其（S）或（R）形式，或其为任何比例的混合物; 并且Z是式（ⅳ）-CH 2 CH 2 NR R 2，（ⅴ）或（vi）的基团，其中R 1和R 2独立地选自氢和C 1-4烷基，R 3 >是氢或C 1-4烷基; 及其盐，溶剂合物及其生理功能衍生物。

9. 发明申请

WO2010116116A1 PROCESS FOR PREPARING CARBOXYLIC ACID AMIDES USEFUL IN THE TREATMENT OF MUSCULAR DISORDERS 审中-公开
标题翻译：制备用于治疗肌肉疾病的羧酸的方法
公开(公告)号：WO2010116116A1
公开(公告)日：2010-10-14
申请号：PCT/GB2010/000386
申请日：2010-03-03
申请人： UCL BUSINESS PLC , SELWOOD, David
发明人： SELWOOD, David
IPC分类号： C07C233/68
CPC分类号： C07C231/02 , C07C231/12 , C07C233/69
摘要： The present invention relates to a process for preparing a compound of formula wherein: R 2 is cycloalkyl or alkyl, each of which may be optionally substituted; Y is -CONR 3 R 4 , -CN or CO 2 R 5 ; R 3 , R 4 and R 5 are each independently H or alkyl; n is 1 to 6; wherein said process comprising the steps of : (i) treating a compound of formula (IV), where R 1 is alkyl, with a compound of formula (V) and forming a compound of formula (IIIb); (ii) treating said compound of formula (IIIb) with a compound of formula (Il) to form a compound of formula (I).
摘要翻译：本发明涉及制备下式化合物的方法：其中：R 2是环烷基或烷基，其中每一个可以被任选取代; Y是-CONR 3 R 4，-CN或CO 2 R 5; R3，R4和R5各自独立地为H或烷基; n为1至6; 其中所述方法包括以下步骤：（i）将式（Ⅳ）化合物（其中R1为烷基）与式（Ⅴ）化合物反应并形成式（IIIb）化合物; （ii）用式（II）化合物处理式（IIIb）化合物以形成式（I）化合物。

10. 发明申请

WO2008040986A1 SHORT PEPTIDIC NEUROPILIN-1 ANTAGONISTS AND THEIR USE 审中-公开
标题翻译：短暂性神经营养因子-1拮抗剂及其使用
公开(公告)号：WO2008040986A1
公开(公告)日：2008-04-10
申请号：PCT/GB2007/003775
申请日：2007-10-04
申请人： ARK THERAPEUTICS LTD. , JIA, Haiyan , BAGHERZADEH, Azadeh , ZACHARY, Ian , TICKNER, Michelle , CHAPMAN, Chris , JARVIS, Ashley , SELWOOD, David
发明人： JIA, Haiyan , BAGHERZADEH, Azadeh , ZACHARY, Ian , TICKNER, Michelle , CHAPMAN, Chris , JARVIS, Ashley , SELWOOD, David
IPC分类号： C07K5/06 , C07K5/10 , C07K7/06 , A61P9/02
CPC分类号： C07K5/1019 , C07K5/06086 , C07K7/06
摘要： The present invention is a peptide having up to 7 amino acids and comprising the sequence K-X 1 -X 2 -R, wherein X 1 is P or A, and wherein X 2 is any amino acid or COCONH. The peptides of the invention may be useful in treating cancer, neurodegeneration, and for stimulating nerve repair.
摘要翻译：本发明是具有至多7个氨基酸并且包含序列KX 1 -X 2 -R 2的肽，其中X 1是P 或A，其中X 2是任何氨基酸或COCONH。本发明的肽可用于治疗癌症，神经变性和刺激神经修复。

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