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1. 发明授权

US07939630B2 Conjugated biological molecules and their preparation 有权
标题翻译：共轭生物分子及其制备
公开(公告)号：US07939630B2
公开(公告)日：2011-05-10
申请号：US12458931
申请日：2009-07-28
申请人： Stephen James Brocchini , Antony Robert Godwin , Elisa Pedone , Ji-Won Choi , Sunil Shaunak
发明人： Stephen James Brocchini , Antony Robert Godwin , Elisa Pedone , Ji-Won Choi , Sunil Shaunak
IPC分类号： C07K1/13
CPC分类号： A61K47/48215 , A61K47/60
摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W— together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.
摘要翻译：通式（I）的新型生物活性化合物，其中X和X'之一表示聚合物，另一个表示氢原子; 每个Q独立地表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; 或者如果X'代表聚合物，则X-Q-W一起可以代表吸电子基团; 此外，如果X表示聚合物，则X'和吸电子基团W与中间原子一起可以形成环; Z 1和Z 2各自独立地表示衍生自生物分子的基团，其各自经由亲核部分与A和B连接; 或Z 1和Z 2一起表示衍生自经由两个亲核部分与A和B连接的生物分子的单一基团; A是C 1-5亚烷基或亚烯基链; 和B是键或C 1-4亚烷基或亚烯基链; 通过将所述分子中的亲核基团，优选通过二硫桥将合适的聚合物与合适的生物活性分子缀合而形成。

2. 发明授权

US08816051B2 Conjugated biological molecules and their preparation 有权
标题翻译：共轭生物分子及其制备
公开(公告)号：US08816051B2
公开(公告)日：2014-08-26
申请号：US13077980
申请日：2011-03-31
申请人： Stephen James Brocchini , Antony Robert Godwin , Elisa Pedone , Ji-Won Choi , Sunil Shaunak
发明人： Stephen James Brocchini , Antony Robert Godwin , Elisa Pedone , Ji-Won Choi , Sunil Shaunak
IPC分类号： C07K1/13 , A61K47/48
CPC分类号： A61K47/48215 , A61K47/60
摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W— together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.
摘要翻译：通式（I）的新型生物活性化合物，其中X和X'之一表示聚合物，另一个表示氢原子; 每个Q独立地表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; 或者如果X'代表聚合物，则X-Q-W一起可以代表吸电子基团; 此外，如果X表示聚合物，则X'和吸电子基团W与中间原子一起可以形成环; Z 1和Z 2各自独立地表示衍生自生物分子的基团，其各自经由亲核部分与A和B连接; 或Z 1和Z 2一起表示衍生自经由两个亲核部分与A和B连接的生物分子的单一基团; A是C 1-5亚烷基或亚烯基链; 和B是键或C 1-4亚烷基或亚烯基链; 通过将所述分子中的亲核基团，优选通过二硫桥将合适的聚合物与合适的生物活性分子结合而形成。

3. 发明申请

US20090298154A1 Conjugated biological molecules and their preparation 有权
公开(公告)号：US20090298154A1
公开(公告)日：2009-12-03
申请号：US12458931
申请日：2009-07-28
申请人： Stephen James Brocchini , Antony Robert Godwin , Elisa Pedone , Ji-Won Choi , Sunil Shaunak
发明人： Stephen James Brocchini , Antony Robert Godwin , Elisa Pedone , Ji-Won Choi , Sunil Shaunak
IPC分类号： C12N9/96 , C07C321/24 , C07K17/00 , C07K1/00
CPC分类号： A61K47/48215 , A61K47/60
摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W— together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.

4. 发明授权

US07595292B2 Conjugated biological molecules and their preparation 有权
标题翻译：共轭生物分子及其制备
公开(公告)号：US07595292B2
公开(公告)日：2009-09-29
申请号：US10564340
申请日：2004-07-12
申请人： Stephen James Brocchini , Antony Robert Godwin , Elisa Pedone , Jin-Won Choi , Sunil Shaunak
发明人： Stephen James Brocchini , Antony Robert Godwin , Elisa Pedone , Jin-Won Choi , Sunil Shaunak
IPC分类号： A61K38/16 , A61K39/00
CPC分类号： A61K47/48215 , A61K47/60
摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W- together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.
摘要翻译：通式（I）的新型生物活性化合物，其中X和X'之一表示聚合物，另一个表示氢原子; 每个Q独立地表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; 或者如果X'代表聚合物，则X-Q-W一起可以代表吸电子基团; 此外，如果X表示聚合物，则X'和吸电子基团W与中间原子一起可以形成环; Z 1和Z 2各自独立地表示衍生自生物分子的基团，其各自经由亲核部分与A和B连接; 或Z 1和Z 2一起表示衍生自经由两个亲核部分与A和B连接的生物分子的单一基团; A是C 1-5亚烷基或亚烯基链; 和B是键或C 1-4亚烷基或亚烯基链; 通过将所述分子中的亲核基团，优选通过二硫桥将合适的聚合物与合适的生物活性分子缀合而形成。

5. 发明申请

US20100119484A1 DERIVATISATION OF BIOLOGICAL MOLECULES 有权
标题翻译：生物分子的衍生物
公开(公告)号：US20100119484A1
公开(公告)日：2010-05-13
申请号：US12527233
申请日：2008-02-12
申请人： Stephen James Brocchini , Antony Robert Godwin , Yiqing Tang , Andrew Lennard Lewis
发明人： Stephen James Brocchini , Antony Robert Godwin , Yiqing Tang , Andrew Lennard Lewis
IPC分类号： A61K38/21 , C07C69/63 , C08F2/00 , C08G75/00 , C08G69/48 , A61P37/00
CPC分类号： A61K47/48176 , A61K38/00 , A61K38/21 , A61K47/58 , A61K47/60 , C07C323/22 , C07K17/08 , C08F4/00 , C08F4/06 , C08F30/02 , C08F130/02
摘要： The present disclosure relates to a new polymerisation process in which ethylenically unsaturated monomers are polymerised by a living radical polymerisation process in the presence of an initiator and a catalyst. Polymers produced by this new process are also thought to be novel and may be used to derivatise biological molecules to improve their efficacy as therapeutic treatments. A preferred polymer is of formula The polymers are particularly suitable for derivatising proteins, such as interferon-α.
摘要翻译：本公开涉及一种新的聚合方法，其中烯属不饱和单体通过活性自由基聚合方法在引发剂和催化剂存在下聚合。通过这种新方法生产的聚合物也被认为是新的，可用于衍生生物分子以提高其作为治疗疗法的功效。优选的聚合物具有下式聚合物特别适用于衍生化蛋白质，如干扰素-α。

6. 发明授权

US09005598B2 Conjugated proteins and peptides 有权
标题翻译：共轭蛋白和肽
公开(公告)号：US09005598B2
公开(公告)日：2015-04-14
申请号：US13254003
申请日：2010-03-04
申请人： Antony Robert Godwin , Stephen James Brocchini
发明人： Antony Robert Godwin , Stephen James Brocchini
IPC分类号： A61K31/00 , A61K47/48
CPC分类号： A61K47/48215 , A61K38/212 , A61K39/395 , A61K47/60
摘要： Novel compounds of the general formula (I): in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; each of R1 and R2 independently represents a hydrogen atom or a C1-4alkyl group; and either Z1 represents a protein or a peptide linked to CR2 via a nucleophilic moiety, and Z2 represents a molecule linked to CR2 via a nucleophilic moiety, or Z1 and Z2 together represent a single group derived from a protein or peptide linked to CR via two nucleophilic moieties.
摘要翻译：新型通式（I）的化合物：其中X表示聚合物; Q表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; R 1和R 2各自独立地表示氢原子或C 1-4烷基; Z1表示通过亲核部分与CR2连接的蛋白质或肽，Z2表示通过亲核部分与CR2连接的分子，或者Z1和Z2一起代表通过两个连接至CR的蛋白质或肽衍生的单一组亲核部分。

7. 发明申请

US20120014905A1 CONUGATED PROTEINS AND PEPTIDES 有权
标题翻译：结合蛋白和肽
公开(公告)号：US20120014905A1
公开(公告)日：2012-01-19
申请号：US13254003
申请日：2010-03-04
申请人： Antony Robert Godwin , Stephen James Brocchini
发明人： Antony Robert Godwin , Stephen James Brocchini
IPC分类号： A61K31/795 , C07C323/41 , C08G65/48 , C07K1/107 , A61K38/21 , C07C235/76 , C07K14/56 , C07C233/20
CPC分类号： A61K47/48215 , A61K38/212 , A61K39/395 , A61K47/60
摘要： Novel compounds of the general formula (I): in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; each of R1 and R2 independently represents a hydrogen atom or a C1-4alkyl group; and either Z1 represents a protein or a peptide linked to CR2 via a nucleophilic moiety, and Z2 represents a molecule linked to CR2 via a nucleophilic moiety, or Z1 and Z2 together represent a single group derived from a protein or peptide linked to CR via two nucleophilic moieties.
摘要翻译：新型通式（I）的化合物：其中X表示聚合物; Q表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; R 1和R 2各自独立地表示氢原子或C 1-4烷基; Z1表示通过亲核部分与CR2连接的蛋白质或肽，Z2表示通过亲核部分与CR2连接的分子，或者Z1和Z2一起代表通过两个连接至CR的蛋白质或肽衍生的单一基团亲核部分。

8. 发明授权

US08575397B2 Derivatisation of biological molecules 有权
标题翻译：生物分子的衍生化
公开(公告)号：US08575397B2
公开(公告)日：2013-11-05
申请号：US12527233
申请日：2008-02-12
申请人： Stephen James Brocchini , Antony Robert Godwin , Yiqing Tang , Andrew Lennard Lewis
发明人： Stephen James Brocchini , Antony Robert Godwin , Yiqing Tang , Andrew Lennard Lewis
IPC分类号： C07C319/00
CPC分类号： A61K47/48176 , A61K38/00 , A61K38/21 , A61K47/58 , A61K47/60 , C07C323/22 , C07K17/08 , C08F4/00 , C08F4/06 , C08F30/02 , C08F130/02
摘要： The present disclosure relates to a new polymerization process in which ethylenically unsaturated monomers are polymerised by a living radical polymerization process in the presence of an initiator and a catalyst. Polymers produced by this new process are also thought to be novel and may be used to derivatise biological molecules to improve their efficacy as therapeutic treatments. A preferred polymer is of formula The polymers are particularly suitable for derivatising proteins, such as interferon-α.
摘要翻译：本公开涉及一种新的聚合方法，其中烯键式不饱和单体在引发剂和催化剂存在下通过活性自由基聚合方法聚合。通过这种新方法生产的聚合物也被认为是新的，可用于衍生生物分子以提高其作为治疗疗法的功效。优选的聚合物具有下式聚合物特别适用于衍生化蛋白质，例如干扰素-α。

9. 发明授权

US5902812A Pharmaceutical piperazine compounds 失效
标题翻译：药用哌嗪化合物
公开(公告)号：US5902812A
公开(公告)日：1999-05-11
申请号：US693173
申请日：1996-09-24
申请人： Stephen James Brocchini , Justin Stephen Bryans , Adrian John Folkes , Christopher John Latham , Julie Elizabeth Brumwell
发明人： Stephen James Brocchini , Justin Stephen Bryans , Adrian John Folkes , Christopher John Latham , Julie Elizabeth Brumwell
IPC分类号： C07D241/18 , A61K31/495 , A61P7/02 , C07D241/02 , C07D403/10 , C07D405/10
CPC分类号： C07D241/02
摘要： Diketopiperazines of formula (A): ##STR1## wherein each of R.sub.1 to R.sub.8 is H or an organic radical as described herein and the pharmaceutically acceptable salts thereof have activity as inhibitors of plasminogen activator inhibitor.
摘要翻译： PCT No.PCT / GB95 / 00299 Sec。 371日期：1996年9月24日 102（e）1996年9月24日PCT 1995年2月14日提交PCT公布。出版物WO95 / 21829 日期：1995年8月17日式（A）的二氢哌嗪：其中R 1至R 8各自为H或如本文所述的有机基团，其药学上可接受的盐具有作为纤溶酶原激活物抑制剂抑制剂的活性。

10. 发明授权

US5700804A Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US5700804A
公开(公告)日：1997-12-23
申请号：US381932
申请日：1995-04-11
申请人： Mark Anthony David Collins , Maria Ines Chicarelli-Robinson , Justin Stephen Bryans , Stephen James Brocchini , Christopher John Latham , John Richardson Shaw
发明人： Mark Anthony David Collins , Maria Ines Chicarelli-Robinson , Justin Stephen Bryans , Stephen James Brocchini , Christopher John Latham , John Richardson Shaw
IPC分类号： A61K31/495 , A61P7/02 , A61P35/00 , C07D241/02 , C07D241/08
CPC分类号： C07D241/02
摘要： Diketopiperazines of the formula: ##STR1## where each of R.sub.1 to R.sub.10, which may be the same or different, is independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by one or more halogen atoms, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, halogen, hydroxy, nitro, phenyl, -cyano, --CH.sub.2 OH, --CH.sub.2 COOH, --CO.sub.2 R.sup.11, --NHCOR.sup.11, --NHSO.sub.2 R.sup.13, --SO.sub.2 R.sup.13, --CON(R.sup.11 R.sup.12), --SOR.sup.13, --SO.sub.2 N(R.sup.11 R.sup.12), --N(R.sup.11 R.sup.12), and --O(CH.sub.2).sub.n N(R.sup.11 R.sup.12), --O(CH.sub.2).sub.n CO.sub.2 R.sup.11, --OCOR.sup.11, --CH.sub.2 OCOR.sup.11, --CH.sub.2 NHCOR.sup.11, --CH.sub.2 NHCOOR.sup.13, --CH.sub.2 SR.sup.11, --CH.sub.2 SCOR.sup.11, --CH.sub.2 S(O).sub.m R.sup.13 wherein m is 1 or 2, --CH.sub.2 NHCO(CH.sub.2).sub.n CO.sub.2 R.sup.11, --N(R.sup.11)COR.sup.12, --NHCOCF.sub.3, --NHCO(CH.sub.2).sub.n CO.sub.2 R.sup.11, --NHCO(CH.sub.2).sub.n OCOR.sup.11 and --NHCO(CH.sub.2).sub.n OR.sup.11 wherein n is 0 or is an integer of from 1 to 6, each of R.sup.11 and R.sup.12 is independently H or C.sub.1 -C.sub.6 alkyl and R.sup.13 is C.sub.1 -C.sub.6 alkyl; or any of R.sub.1 and R.sub.2, R.sub.2 and R.sub.3, R.sub.3 and R.sub.4 and R.sub.4 and R.sub.5, or R.sub.6 and R.sub.7, R.sub.7 and R.sub.8, R.sub.8 and R.sub.9 and R.sub.9 and R.sub.10, form together with the carbon atoms to which they are attached a benzene ring; and pharmaceutically acceptable salts and esters thereof are inhibitors of the plasminogen activator inhibitor.
摘要翻译： PCT No.PCT / GB93 / 01734 Sec。 371日期1995年04月11日 102（e）日期1995年4月11日PCT提交1993年8月16日PCT公布。第WO94 / 04512号公报日期：1994年3月3日具有下式的下式的哌嗪基：不同的，独立地选自氢，未被取代或被一个或多个卤素原子取代的C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6烷硫基卤素，羟基，硝基，苯基， - 氰基，-CH 2 OH，-CH 2 COOH，-CO 2 R 11，-NHCOR 11，-NHSO 2 R 13，-SO 2 R 13，-CON（R 11 R 12），-SOR 13，-SO 2 N（R 11 R 12）， - N（R 11 R 12），和-O（CH 2）n N（R 11 R 12），-O（CH 2）n CO 2 R 11，-OCOR 11，-CH 2 OCOR 11，-CH 2 NHCOR 11，-CH 2 NHCOOR 13，-CH 2 S R 11，-CH 2 SCOR 11，-CH 2 S（O）m R 13，其中m为1或2， -CH2NHCO（CH2）nCO2R11，-N（R11）COR12，-NHCOCF3，-NHCO（CH2）nCO2R11，-NHCO（CH2）nOCOR11和-NHCO（CH2）nOR11，其中n为0或为1至6的整数 R 11和R 12各自独立地为H或C 1 -C 6烷基，R 13为C 1 -C 6烷基; 或R 1和R 2中的任一个，R 2和R 3，R 3和R 4以及R 4和R 5或R 6，R 7，R 7和R 8，R 8和R 9以及R 9和R 10与它们所连接的碳原子一起形成苯环 ; 及其药学上可接受的盐和酯是纤溶酶原激活物抑制剂的抑制剂。

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