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公开(公告)号：US06828412B1
公开(公告)日：2004-12-07
申请号：US10069929
申请日：2002-07-19
IPC分类号： C08G6900
摘要： A polymer comprising: a polymeric backbone comprising at least one unit having the structure (I), wherein R-R4 comprise groups selected from the group consisting of H, C1-C12 alkyl, C6-C18 aryl, C7-C18 aralkyl, C6-C18 cycloalkyl or any of the group consisting of C1-C12 alkyl, C6-C18 aryl, C7-C18 aralkyl, C6-C18 cycloalkyl substituted, within the carbon chain or appended thereto, with one or more heteroatoms; R and R2 or R and R4 or R and R1 or R2 and R3 may be joined so that with the carbon atom(s) to which they are attached they together form a saturated, partially unsaturated or unsaturated ring system respectively, may have a pendent group which may incorporate a linker unit, (for example a peptide linkage) or a unit having the structure (I); A comprises a proton donating moiety selected from the group consisting of formula (1). B comprises a hydrolytically labile group and is selected from the group consisting of formula (2), wherein each R5 is individually selected from the group consisting of H, C1-C12 alkyl, C6-C18 aryl, C7-C18 aralkyl, C6-C18 cycloalkyl; wherein groups A and B are in a cis-configuration about bond Ca—Cb; m is an integer of 0 to 100, n, p and q are each an integer of 0 or 1; Q comprises 1 or more structures selected from the group consisting of formula (3) wherein R6-R11 are individually selected from the same group as defined for group R above and r is an integer between 1 and 5000, preferably 1 to 10, most preferably 1 to 6; methods for the production, and uses thereof.
摘要翻译： 一种聚合物，其包括：包含至少一个具有结构（I）的单元的聚合物主链，其中RR 4包含选自H，C 1 -C 12烷基，C 6 -C 18芳基，C 7 -C 18芳烷基，C 6 -C 18环烷基或由碳原子链或其附着的一个或多个杂原子取代的C 1 -C 12烷基，C 6 -C 18芳基，C 7 -C 18芳烷基，C 6 -C 18环烷基中的任何一种; R和R 2或R和R 4或R和R 1或R 2和R 3可以连接成与它们所连接的碳原子一起形成 饱和的，部分不饱和的或不饱和的环系统可以具有可以结合接头单元（例如肽键）或具有结构（I）的单元的侧基; A包含选自式（1）的质子供体部分。 B包含水解不稳定基团，并且选自式（2），其中每个R 5分别选自H，C 1 -C 12烷基，C 6 -C 18芳基，C 7 -C 18芳烷基， C6-C18环烷基; 其中基团A和B是关于键Ca-Cb的顺式构型; m为0〜100的整数，n，p和q各自为0或1的整数; Q包括选自式（3）的一种或多种结构，其中R 6 -R 11分别选自与上述R基团所定义相同的基团，r是1至5000之间的整数，优选 1〜10，最优选1〜6; 生产方法及其用途。
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公开(公告)号：US20100119484A1
公开(公告)日：2010-05-13
申请号：US12527233
申请日：2008-02-12
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。
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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。
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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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公开(公告)号：US09005598B2
公开(公告)日：2015-04-14
申请号：US13254003
申请日：2010-03-04
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。
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公开(公告)号：US07939630B2
公开(公告)日：2011-05-10
申请号：US12458931
申请日：2009-07-28
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。
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公开(公告)号：US07595292B2
公开(公告)日：2009-09-29
申请号：US10564340
申请日：2004-07-12
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。
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公开(公告)号：US20120014905A1
公开(公告)日：2012-01-19
申请号：US13254003
申请日：2010-03-04
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。
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公开(公告)号：US5891877A
公开(公告)日：1999-04-06
申请号：US693172
申请日：1996-09-25
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： C07D241/02 , C07D241/18 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D521/00 , A61K31/495 , A61K31/535 , C07D241/08
CPC分类号： C07D241/02 , C07D231/12 , C07D233/56 , C07D241/18 , C07D249/08 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06
摘要： Diketopiperazines of the formula ##STR1## where one or both of R.sub.1 and R.sub.2, which are different, are chosen from X and a phenyl group substituted by X, C(O)X, OC(O)CH.sub.2 X, OCH.sub.2 CH.sub.2 X, CH.sub.2 X, CONH(CH.sub.2).sub.n X, O(CH.sub.2).sub.n CH(OH)(CH.sub.2).sub.n X ##STR2## and, where appropriate, the other of R.sub.1 and R.sub.2 is a phenyl group optionally substituted by one or more groups selected from halogen, nitro, methoxy, NHC(O)R.sub.12, CO.sub.2 H, O(CH.sub.2).sub.n N(R.sub.12 R.sub.13), C.sub.1 -C.sub.4 alkyl and (CH.sub.2).sub.n C(O)OR.sub.12 ; X is a five- or six-membered heterocyclic ring selected from the group consisting of pyridyl, imidazolyl, furyl, pyrrolyl, pyrrolidinyl, thienyl, piperazinyl, piperidinyl, morpholinyl, quinolyl, isoquinotyl and indolyl, the heteroatom(s) of the said heterocyclic ring, when nitrogen, being optionally substituted by hydrogen, methyl, oxygen, tertiary-butyloxycarbonyl, or SO.sub.2 Me, the heterocyclic ring being optionally substituted by halogen �hydrogen!, methyl, MeS, phenyl, O(CH.sub.2).sub.n N(R.sub.12 R.sub.13) or optionally containing one or more carbonyl groups and being optionally fused to a benzene ring; Y is O or S; R.sub.12 and R.sub.13, which may be the same or different, are hydrogen or C.sub.1 -C.sub.6 alkyl; and n is 0 or an integer having the value 1, 2, 3 or 4; a pharmaceutically acceptable salts or esters having activity as inhibitors of plasminogen activator inhibitor.
摘要翻译： PCT No.PCT / GB95 / 00302 Sec。 371日期1996年9月25日 102（e）日期1996年9月25日PCT提交1995年2月14日PCT公布。 出版物WO95 / 21832 日期为1995年8月17日，由X，C（O）X，OC（O）CH 2 X，OCH 2 CH 2 X，CH 2 X，CONH（CH 2）n X，O（ CH 2）n CH（OH）（CH 2）n X
，并且在适当的情况下，R 1和R 2中的另一个是任选被一个或多个选自卤素，硝基，甲氧基，NHC（O）R 12，CO 2 H ，O（CH 2）n N（R 12 R 13），C 1 -C 4烷基和（CH 2）n C（O）OR 12; X是选自吡啶基，咪唑基，呋喃基，吡咯基，吡咯烷基，噻吩基，哌嗪基，哌啶基，吗啉基，喹啉基，异喹啉基和吲哚基的五元或六元杂环，所述杂环的杂原子 环，任选地被氢，甲基，氧，叔丁氧基羰基或SO 2 Me取代，杂环任选被卤素[氢]，甲基，MeS，苯基，O（CH 2）n N（R 12 R 13）或任选地被 含有一个或多个羰基并任选地与苯环稠合; Y为O或S; R 12和R 13可以相同或不同，是氢或C 1 -C 6烷基; 并且n为0或具有值1,2,3或4的整数; 具有作为纤溶酶原激活物抑制剂抑制剂活性的药学上可接受的盐或酯。 -
公开(公告)号：US5861400A
公开(公告)日：1999-01-19
申请号：US693169
申请日：1996-11-04
IPC分类号： C07D241/02 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , A61K31/495
CPC分类号： C07D241/02 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06
摘要： Piperazine derivatives of the formula ##STR1## their esters and salts are useful as modulators of multiple drug resistance.
摘要翻译： PCT No.PCT / GB95 / 00301 Sec。 371日期：1996年11月4日 102（e）日期1996年11月4日PCT提交1995年2月14日PCT公布。 公开号WO95 / 21831 日期1995年8月17日公式为“IMAGE”（Aa）的哌嗪衍生物，其酯和盐可用作多种耐药性的调节剂。
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