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1. 发明授权

US5173482A Immunosuppressive analogues and derivatives of succinylacetone 失效
标题翻译：琥珀酰丙酮的免疫抑制类似物和衍生物
公开(公告)号：US5173482A
公开(公告)日：1992-12-22
申请号：US624078
申请日：1990-12-06
申请人： Danute E. Nitecki , Margaret Moreland , Lois Aldwin , Corey H. Levenson , Irwin Braude , David F. Mark , Henry Rapoport
发明人： Danute E. Nitecki , Margaret Moreland , Lois Aldwin , Corey H. Levenson , Irwin Braude , David F. Mark , Henry Rapoport
IPC分类号： A61K31/12 , A61K31/16 , A61K31/19 , A61K31/22 , A61K31/23 , A61K31/41
CPC分类号： A61K31/22 , A61K31/12 , A61K31/16 , A61K31/19 , A61K31/23 , A61K31/41
摘要： Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.
摘要翻译：所示的琥珀酰丙酮衍生物或相关药物及其合成方法，其中药物由琥珀酰丙酰基 - 脯氨酸-PEG，琥珀酰乙酰基-NH- PEG或具有下式的化合物组成：其中n = 1-6。基于它们在细胞免疫测定中的活性和大鼠中的佐剂诱导的关节炎的活性，分别在体内和体外具有免疫抑制活性。

2. 发明授权

US5252603A Immunosuppressive analogues and derivatives of succinylacetone 失效
标题翻译：琥珀酰丙酮的免疫抑制类似物和衍生物
公开(公告)号：US5252603A
公开(公告)日：1993-10-12
申请号：US623096
申请日：1990-12-06
申请人： Danute E. Nitecki , Lois Aldwin , Corey H. Levenson , Margaret Moreland , Irwin Braude , David F. Mark , Henry Rapoport
发明人： Danute E. Nitecki , Lois Aldwin , Corey H. Levenson , Margaret Moreland , Irwin Braude , David F. Mark , Henry Rapoport
IPC分类号： A61K31/12 , A61K31/16 , A61K31/19 , A61K31/22 , A61K31/23 , A61K31/41 , A61K31/205
CPC分类号： A61K31/19 , A61K31/12 , A61K31/16 , A61K31/22 , A61K31/23 , A61K31/41
摘要： Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## wherein n=1-6R=CH.sub.3, CF.sub.3, --CO.sub.2 R.sup.IV, ##STR2## R.sup.I, R.sup.II =H, F, CH.sub.3, or ##STR3## R.sup.III =H, ##STR4## or tetrazolyl R.sup.IV =H, or alkyland that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.
摘要翻译：显示衍生的琥珀酰丙酮衍生的或相关的药物及其合成方法，其中药物由琥珀酰丙酰基 - 脯氨酸-PEG，琥珀酰乙酰基-NH- PEG或具有下式的化合物组成：其中n = 1-6R = CH 3 ，CF3，-CO2RIV，IMA，RI，RII = H，F，CH3或R IMA = H，IMAGE或四唑基RIV = H或烷基，并且在体内和体外均具有免疫抑制活性分别在细胞免疫学测定和佐剂诱导的大鼠关节炎中的活性。

3. 发明授权

US5216005A Immunosuppressive analogues and derivatives of succinylacetone 失效
标题翻译：琥珀酰丙酮的免疫抑制类似物和衍生物
公开(公告)号：US5216005A
公开(公告)日：1993-06-01
申请号：US623095
申请日：1990-12-06
申请人： Danute E. Nitecki , Lois Aldwin , Corey H. Levenson , Margaret Moreland , Irwin Braude , David F. Mark , Henry Rapoport
发明人： Danute E. Nitecki , Lois Aldwin , Corey H. Levenson , Margaret Moreland , Irwin Braude , David F. Mark , Henry Rapoport
IPC分类号： A61K31/12 , A61K31/16 , A61K31/19 , A61K31/22 , A61K31/23 , A61K31/41
CPC分类号： A61K31/16 , A61K31/12 , A61K31/19 , A61K31/22 , A61K31/23 , A61K31/41
摘要： Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.
摘要翻译：所示的琥珀酰丙酮衍生物或相关药物及其合成方法，其中药物由琥珀酰丙酰基 - 脯氨酸-PEG，琥珀酰乙酰基-NH- PEG或具有下式的化合物组成：其中n = 1-6。基于它们在细胞免疫测定中的活性和大鼠中的佐剂诱导的关节炎的活性，分别在体内和体外具有免疫抑制活性。

4. 发明授权

US4895872A Immunosupressive analogues and derivatives of succinylacetone 失效
标题翻译：琥珀酰丙酮的免疫抑制类似物和衍生物
公开(公告)号：US4895872A
公开(公告)日：1990-01-23
申请号：US324360
申请日：1989-03-15
申请人： Danute E. Nitecki , Margaret Moreland , Lois Aldwin , Corey H. Levenson , Irwin Braude , David F. Mark , Henry Rapaport
发明人： Danute E. Nitecki , Margaret Moreland , Lois Aldwin , Corey H. Levenson , Irwin Braude , David F. Mark , Henry Rapaport
IPC分类号： A61K31/12 , A61K31/16 , A61K31/19 , A61K31/22 , A61K31/23 , A61K31/41
CPC分类号： A61K31/41 , A61K31/12 , A61K31/16 , A61K31/19 , A61K31/22 , A61K31/23
摘要： Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.
摘要翻译：所示的琥珀酰丙酮衍生物或相关药物及其合成方法，其中药物由琥珀酰丙酰基 - 脯氨酸-PEG，琥珀酰乙酰基-NH- PEG或具有下式的化合物组成：其中n = 1-6。基于它们在细胞免疫测定中的活性和大鼠中的佐剂诱导的关节炎的活性，分别在体内和体外具有免疫抑制活性。

5. 发明授权

US5153265A Conjugation of polymer to colony stimulating factor-1 失效
标题翻译：聚合物与集落刺激因子-1的结合
公开(公告)号：US5153265A
公开(公告)日：1992-10-06
申请号：US576415
申请日：1990-08-30
申请人： Paula J. Shadle , Kirston E. Koths , Margaret Moreland , Nandini Katre , Walter J. Laird , Lois Aldwin , Danute E. Nitecki , John D. Young
发明人： Paula J. Shadle , Kirston E. Koths , Margaret Moreland , Nandini Katre , Walter J. Laird , Lois Aldwin , Danute E. Nitecki , John D. Young
IPC分类号： A61K38/00 , A61K47/48 , C07K14/53
CPC分类号： A61K47/48215 , A61K47/48176 , C07K14/53 , A61K38/00
摘要： A biologically active CSF-1 protein is selectively conjugated via certain amino acid residues or carbohydrate moieties to a water-soluble polymer selected from polyethylene glycol or polypropylene glycol homopolymers, polyoxyethylated polyols, or polyvinyl alcohol. The resulting conjugated CSF-1 is biologically active and has increased circulating half-life in mammals, compared to that of the unconjugated protein. The conjugated CSF-1 may be used to stimulate the immune response or to provide more cells to be stimulated.
摘要翻译： PCT No.PCT / US89 / 00270 Sec。 371日期1990年8月30日 102（e）1990年8月30日PCT PCT 1989年1月23日提交PCT生物活性CSF-1蛋白通过某些氨基酸残基或碳水化合物部分选择性地与选自聚乙二醇或聚丙二醇均聚物的水溶性聚合物，聚氧乙烯化多元醇或聚乙烯醇。与未缀合的蛋白质相比，得到的共轭CSF-1具有生物活性并且在哺乳动物中具有增加的循环半衰期。缀合的CSF-1可用于刺激免疫应答或提供更多待刺激的细胞。

6. 发明授权

US5034514A Novel cross-linking agents 失效
标题翻译：新型交联剂
公开(公告)号：US5034514A
公开(公告)日：1991-07-23
申请号：US256723
申请日：1988-10-12
申请人： Danute E. Nitecki , Margaret Moreland
发明人： Danute E. Nitecki , Margaret Moreland
IPC分类号： C07D213/71 , G01N33/543
CPC分类号： G01N33/54353 , C07D213/71
摘要： Bifunctional chemicals useful for linking aldehyde containing moieties to moieties containing functionalities which are or can be reactive with sulfhydryl are claimed and have the formula:L--S--(CH.sub.2).sub.n1 --CONH--SPACER--NH--XwhereinL is a leaving group selected from --H or --S--Ar, wherein Ar represents optionally substituted phenyl or pyridyl;n.sub.1 =2-4;X is selected from: --CO--Y--CONHNH.sub.2, a hydrazide; ##STR1## a hydrazine; ##STR2## a hydrazine; --CO--Y--NH--CONHNH.sub.2, a semicarbazide; and --CO--Z--NH--CSNHNH.sub.2, a thiosemicarbazide;wherein Y is alkylene or oxaalkylene and Z is alkylene or a polypeptide residue briding the N-terminal amino group and C-terminal carboxy group thereof;the SPACER is oxaalkylene or oxaalkylene substituted with hydroxyl and specifically includes residues having formulas selected froma) --(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 -- wherein each n2 is independently 2-4 andb) ##STR3## wherein n3 is 2-6. Also claimed are hydrazides, semicarbazides, and thiosemicarbazides of .omega.-mercaptocarboxylic acids which lack SPACER diamine.
摘要翻译：要求具有下式的LS-（CH2）n1-CONH-SPACER-NH-X，其中L是选自以下的离去基团 - H或-S-Ar，其中Ar表示任选取代的苯基或吡啶基; n1 = 2-4; X选自：-CO-Y-CONHNH 2，酰肼; 肼; 肼; -CO-Y-NH-CONHNH 2，氨基脲; 和-CO-Z-NH-CSNHNH 2，硫代氨基脲; 其中Y是亚烷基或氧杂亚烷基并且Z是亚烷基，或多肽残基支持其N-末端氨基和C-末端羧基; SPACER是被羟基取代的氧杂亚烷基或氧杂亚烷基，具体包括具有选自a） - （CH 2）n 2 -O-（CH 2）n 2 -O-（CH 2）n 2-的式的残基，其中每个n2独立地为2-4，和b）其中n3为2-6。还要求的是缺乏SPACER二胺的ω-巯基羧酸的酰肼，氨基脲和氨基硫脲。

7. 发明授权

US4797491A Compound 1-(3-(2-pyridyldithio)propionamido)-12-(5-hydrazidoglutaramido)-4,9-diox adodecane 失效
标题翻译：化合物1-（3-（2-吡啶基二硫代）丙酰胺基）-12-（5-酰氨基戊酰氨基）-4,9-二氧代十二烷
公开(公告)号：US4797491A
公开(公告)日：1989-01-10
申请号：US840604
申请日：1986-03-17
申请人： Danute E. Nitecki , Margaret Moreland
发明人： Danute E. Nitecki , Margaret Moreland
IPC分类号： C08G69/48 , C07C67/00 , C07C313/00 , C07C323/60 , C07C323/62 , C07D213/71 , C07K1/113 , C07K14/415 , C07K16/00 , C07K17/06 , G01N33/543 , G01N33/547
CPC分类号： C07D213/71 , G01N33/54353
摘要： Bifunctional chemicals useful for linking aldehyde containing moieties to moieties containing functionalities which are or can be reactive with sulfhydryl are claimed and have the formula:L--S--(CH.sub.2).sub.n1 --CONH--SPACER--NH--Xwherein L is a leaving group selected from --H or --S--Ar, wherein Ar represents optionally substituted phenyl or pyridyl;n.sub.1 =2-4;X is selected from:--CO--Y--CONHNH.sub.2, a hydrazide; ##STR1## a hydrazine; ##STR2## a hydrazine; --CO--Y--NH--CONHNH.sub.2, a semicarbazide; and--CO--Z--NH--CSNHNH.sub.2, a thiosemicarbazide;wherein Y is alkylene or oxaalkylene and Z is alkylene or a polypeptide residue bridging the N-terminal amino group and C-terminal carboxy group thereof;the SPACER is oxaalkylene or oxaalkylene substituted with hydroxyl and specifically includes residues having formulas selected from--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --(a)wherein each n2 is independently 2-4 and ##STR3## wherein n3 is 2-6. Also claimed are hydrazides, semicarbazides, and thiosemicarbazides of .omega.-mercaptocarboxylic acids which lack SPACER diamine.
摘要翻译：要求具有下式的LS-（CH2）n1-CONH-SPACER-NH-X，其中L是选自以下的离去基团 - H或-S-Ar，其中Ar表示任选取代的苯基或吡啶基; n1 = 2-4; X选自：-CO-Y-CONHNH 2，酰肼; 肼; 肼; -CO-Y-NH-CONHNH 2，氨基脲; 和-CO-Z-NH-CSNHNH 2，硫代氨基脲; 其中Y是亚烷基或氧杂亚烷基，Z是亚烷基或桥接其N末端氨基和C末端羧基的多肽残基; SPACER是被羟基取代的氧杂亚烷基或氧杂亚烷基，具体包括具有选自 - （CH 2）n 2 -O-（CH 2）n 2 -O-（CH 2）n 2-（a）的式的残基，其中每个n2独立地为2-4，（b）其中n3为2-6。还要求的是缺乏SPACER二胺的ω-巯基羧酸的酰肼，氨基脲和氨基硫脲。

8. 发明授权

US5276140A Cross-linking agents 失效
标题翻译：交联剂
公开(公告)号：US5276140A
公开(公告)日：1994-01-04
申请号：US639050
申请日：1991-01-09
申请人： Danute E. Nitecki , Margaret Moreland
发明人： Danute E. Nitecki , Margaret Moreland
IPC分类号： C07D213/71 , G01N33/543 , C07K17/06 , C07D213/16
CPC分类号： C07D213/71 , G01N33/54353
摘要： Bifunctional chemicals useful for linking aldehyde containing moieties to moieties containing functionalities which are or can be reactive with sulfhydryl are claimed and have the formula:L--S--(CH.sub.2).sub.n1 --CONH--SPACER--NH--XwhereinL is a leaving group selected from --H or --S--Ar, wherein Ar represents optionally substituted phenyl or pyridyl;n.sub.1 =2-4;X is selected from: ##STR1## wherein Y is alkylene or oxaalkylene and Z is alkylene or a polypeptide residue briding the N-terminal amino group and C-terminal carboxy group thereof;the SPACER is oxaalkylene or oxaalkylene substituted with hydroxyl and specifically includes residues having formulas selected from--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --a) wherein each n2 is independently 2-4 and ##STR2## wherein n3 is 2-6. Also claimed are hydrazides, semicarbazides, and thiosemicarbazides of .omega.-mercaptocarboxylic acids which lack SPACER diamine.
摘要翻译：要求具有下式的LS-（CH2）n1-CONH-SPACER-NH-X，其中L是选自以下的离去基团 - H或-S-Ar，其中Ar表示任选取代的苯基或吡啶基; n1 = 2-4; X选自：-CO-Y-CONHNH 2，酰肼; （*化学结构*）（*化学结构*）-CO-Y-NH-CONHNH 2，氨基脲; 和-CO-Z-NH-CSNHNH 2，硫代氨基脲; 其中Y是亚烷基或氧杂亚烷基并且Z是亚烷基，或多肽残基支持其N-末端氨基和C-末端羧基; SPACER是被羟基取代的氧杂亚烷基或氧杂亚烷基并且具体包括具有选自 - （CH 2）n 2 -O-（CH 2）n 2 -O-（CH 2）n 2-a）的式的残基，其中每个n2独立地为2-4和（* 化学结构*）b）其中n3为2-6。还要求的是不含SPACER二胺的（ω） - 巯基羧酸的酰肼，氨基脲和氨基硫脲。

9. 发明授权

US5241078A Coupling agents and sterically hindered disulfide linked conjugates prepared therefrom 失效
标题翻译：偶联剂和由其制备的空间位阻二硫键连接的共轭物
公开(公告)号：US5241078A
公开(公告)日：1993-08-31
申请号：US837678
申请日：1992-02-14
申请人： Margaret Moreland , I. Lawrence Greenfield , Danute E. Nitecki
发明人： Margaret Moreland , I. Lawrence Greenfield , Danute E. Nitecki
IPC分类号： C07C327/32 , C07D207/44 , C07D207/452 , C07D207/46 , G01N33/532
CPC分类号： C07D207/452 , C07C327/32 , C07D207/46 , G01N33/532
摘要： This invention discloses heterobifunctional coupling agents for making a wide array of molecular conjugates. The agents contain a sterically hindered thiol, linked through a spacer arm to a second group reactive toward nucleophiles such as 1.degree. and 2.degree. amines or reactive thiols that are present on biological and organic materials. The coupling agents are useful for making conjugates containing a sterically hindered linkage.
摘要翻译：本发明公开了用于制备广泛分子结合物的异双功能偶联剂。这些试剂含有空间位阻硫醇，其通过间隔臂连接到对亲核试剂反应的第二组，所述亲核试剂例如存在于生物和有机材料上的1℃和2℃的胺或反应性硫醇。偶联剂可用于制备含空间位阻键的缀合物。

10. 发明授权

US4745180A Solubilization of proteins for pharmaceutical compositions using heparin fragments 失效
标题翻译：使用肝素片段对药物组合物进行蛋白质的溶解
公开(公告)号：US4745180A
公开(公告)日：1988-05-17
申请号：US879456
申请日：1986-06-27
申请人： Margaret Moreland , Danute E. Nitecki
发明人： Margaret Moreland , Danute E. Nitecki
IPC分类号： A61K38/20 , A61K47/48 , C07K15/00 , A61K37/02 , A61K39/00 , A61K45/02
CPC分类号： A61K47/48215 , A61K38/2013 , A61K47/4823 , Y10S435/811
摘要： A pharmaceutical composition is prepared wherein a biologically active conjugated protein which is .beta.-interferon, interleukin-2, or an immunotoxin is dissolved in an aqueous carrier medium without the presence of a solubilizing agent. The unconjugated protein, which is poorly or not at all water-soluble at pH 6-8 without such solubilizing agent, is selectively conjugated to at least one heparin fragment having a terminal 2,5-anhydro-D-mannose residue which has an aldehyde not involved in intramolecular hemiacetal formation.
摘要翻译：制备药物组合物，其中将β-干扰素，白细胞介素-2或免疫毒素的生物活性缀合蛋白溶解在含水载体介质中而不存在增溶剂。选择性地将至少一种具有末端2,5-脱水-D-甘露糖残基的肝素片段与未加入这些增溶剂的pH6-8水溶性差的非结合蛋白质选择性缀合，不参与分子内半缩醛形成。

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