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1. 发明公开

EP0406512A1 Polysaccharide fraction with anti-HIV activity 失效
$Polysaccharide fraction with anti-HIV activity$
标题翻译：多糖类药物Wirkung gegen HIV。
公开(公告)号：EP0406512A1
公开(公告)日：1991-01-09
申请号：EP90100448.1
申请日：1990-01-10
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Cardin, Alan D. , Jackson, Richard L.
IPC分类号： A61K31/725 , C08B37/02 , C08B37/08 , C08B37/10
CPC分类号： A61K31/715 , B01D15/3809
摘要： Various peptides having affinity for sulfated polysaccharides such as heparin, dextran sulfate and pentosan polysulfate are bound to resins and used in affinity chromatography to prepare anti-HIV sulfated polysaccharides.
摘要翻译：对硫酸化多糖如肝素，硫酸葡聚糖和戊聚糖多硫酸盐具有亲和力的各种肽与树脂结合，并用于亲和层析以制备抗HIV硫酸化多糖。

2. 发明公开

EP0467185A3 Oligomers, their uses and formulations 失效
标题翻译：低分子，其使用和制剂
公开(公告)号：EP0467185A3
公开(公告)日：1992-09-09
申请号：EP91111315.7
申请日：1991-07-08
申请人： THE DOW CHEMICAL COMPANY , MERRELL DOW PHARMACEUTICALS INC.
发明人： Cardin, Alan D. , Jackson, Richard L. , Mullins, Michael J.
IPC分类号： C08G71/02 , C08G64/08 , C08G63/688 , C08G69/32 , C07C309/51 , C07C309/42 , A61K31/795 , A61K31/74
CPC分类号： A61K31/185 , A61K31/785 , A61K31/795 , C07C309/42 , C07C309/51 , C08G63/19 , C08G63/6884 , C08G63/6924 , C08G64/06 , C08G64/081 , C08G64/083 , C08G69/26 , C08G69/32 , C08G71/02 , Y10S514/885
摘要： The preferred oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a number average molecular weight of

3. 发明公开

EP0346894A2 Extraction and purification of an anticoagulant substance from the south american leech, haementeria ghilianii 失效
标题翻译： Extraktion和Reinigung einer Antigerinnungssubstanz aus densüdamerikanischenBlutegeln Haementeria ghilianii。
公开(公告)号：EP0346894A2
公开(公告)日：1989-12-20
申请号：EP89110877.1
申请日：1989-06-15
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Cardin, Alan D.
IPC分类号： C07K1/16 , C07K14/815 , A61K38/58
CPC分类号： C07K14/815 , A61K38/00 , Y10S435/815 , Y10S514/822 , Y10S530/855
摘要： Applicant has isolated a Factor X a inhibiting substance from the salivary gland extract of the leech H. ghilianii . The extract is subjected to separation using both DEAE-cellulose and heparin-agarose chromatography resins eluting with an increasing salt gradient. The extract is subjected to affinity chromatography using Factor X a bound to an Affi-Gel-15 resin eluting with HEPES containing benzamidine. Reverse phase chromatography yields several purified peptides or proteins having Factor X a inhibiting activity. The properties and clinical compositions of these FX a inhibitors are described.
摘要翻译：申请人从水蛭H.hilianii的唾液腺提取物中分离出一种因子Xa抑制物质。使用DEAE-纤维素和肝素 - 琼脂糖层析树脂进行分离，用逐渐增加的盐梯度洗脱。使用与使用含有苯甲脒的HEPES洗脱的Affi-Gel-15树脂的因子Xa进行亲和层析。反相色谱法产生几种纯化的肽或具有因子Xa抑制活性的蛋白质。描述了这些FXa抑制剂的性质和临床组成。

4. 发明公开

EP0543555A1 Phosphorylated flavanoids in the treatment of viral diseases 失效
标题翻译：磷酰胆碱（Flavonoide zur Behandlung von Viruserkrankungen）。
公开(公告)号：EP0543555A1
公开(公告)日：1993-05-26
申请号：EP92310277.6
申请日：1992-11-11
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Cardin, Alan D. , Tyms, A. Stanley
IPC分类号： A61K31/665
CPC分类号： A61K31/665
摘要： Certain phosphorylated flavanoids are disclosed to be effective in treating retroviral infections including HIV infections as well as infections of herpes simplex virus and cytomegalovirus.
摘要翻译：公开了某些磷酸化类黄酮在治疗包括HIV感染以及单纯疱疹病毒和巨细胞病毒感染的逆转录病毒感染方面是有效的。

5. 发明公开

EP0346894A3 Extraction and purification of an anticoagulant substance from the south american leech, haementeria ghilianii 失效
标题翻译：来自南美洲南美洲的抗血清物质的提取和纯化，HAEMENTERIA GHILIANII
公开(公告)号：EP0346894A3
公开(公告)日：1990-04-25
申请号：EP89110877.1
申请日：1989-06-15
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Cardin, Alan D.
IPC分类号： C07K1/16 , C07K14/815 , A61K38/58
CPC分类号： C07K14/815 , A61K38/00 , Y10S435/815 , Y10S514/822 , Y10S530/855
摘要： Applicant has isolated a Factor X a inhibiting substance from the salivary gland extract of the leech H. ghilianii . The extract is subjected to separation using both DEAE-cellulose and heparin-agarose chromatography resins eluting with an increasing salt gradient. The extract is subjected to affinity chromatography using Factor X a bound to an Affi-Gel-15 resin eluting with HEPES containing benzamidine. Reverse phase chromatography yields several purified peptides or proteins having Factor X a inhibiting activity. The properties and clinical compositions of these FX a inhibitors are described.

6. 发明公开

EP0297456A2 Immunosuppressant peptides 失效
标题翻译：免疫抑制肽。
公开(公告)号：EP0297456A2
公开(公告)日：1989-01-04
申请号：EP88110111.7
申请日：1988-06-24
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Cardin, Alan D. , Bowlin, Terry L. , Krstenansky, John L.
IPC分类号： C07K7/08 , C07K7/06 , A61K37/02 , C07K1/04
CPC分类号： C07K14/005 , A61K38/00 , C12N2740/10022
摘要： Novel peptides having a fragment containing 2 or 3 Arg or Lys residues and having a fragment containing 2 or 3 Gly, Leu, Ile, or Thr residues adjacent to the carboxy end of the first fragment and having amino and carboxy tails consisting of chains made up of any amino acids are immunosuppressant agents and can suppress the lymphocyte system by suppressing lymphocyte proliferation.
The formula is as follows:
Tn-A-B-C-D-Tc
wherein
Tn is an amino terminal residue selected from hydrogen, one or two alkyl groups of from 1 to 6 carbon atoms, one or two acyl groups of from 2 to 10 carbon atoms, carbobenzyloxy, and t -butyloxycarbonyl;
A is a peptide fragment containing from 3 to 12 residues of any amino acid;
B is a peptide fragment containing 2 or 3 amino acid residues selected from Arg and Lys;
C is a peptide fragment containing 2 or 3 amino acid residues selected from Gly, Leu, Ile, and Thr;
D is a peptide fragment containing from 1 to 12 residues of any amino acid; and
Tc is a carboxy terminal residue selected from OH, (C₁-C₆)alkoxy, amino, mono- or di-(C₁-C₄)alkyl substituted amino, and benzylamino.
摘要翻译：具有包含2或3个Arg或Lys残基的片段的新型肽，并且具有与第一片段的羧基末端相邻的2或3个Gly，Leu，Ile或Thr残基的片段，并具有由构成的链组成的氨基和羧基尾任何氨基酸都是免疫抑制剂，可通过抑制淋巴细胞增殖来抑制淋巴细胞系统。该公式如下：Tn-ABCD-Tc其中Tn是选自氢，一个或两个1-6个碳原子的一个或两个烷基，一个或两个2-10个碳原子的酰基的氨基末端残基，苄氧羰基，和叔丁氧基羰基; A是含有任何氨基酸的3-12个残基的肽片段; B是含有选自Arg和Lys的2或3个氨基酸残基的肽片段; C是含有选自Gly，Leu，Ile和Thr的2或3个氨基酸残基的肽片段; D是含有任何氨基酸的1至12个残基的肽片段; 并且Tc是选自OH，（C 1 -C 6）烷氧基，氨基，单 - 或二 - （C 1 -C 4）烷基取代的氨基和苄基氨基的羧基末端残基。

7. 发明公开

EP0498095A1 Sulfonic stilbene derivatives in the treatment of viral diseases 失效
标题翻译： Sulfonische Stilbenderivate zur Behandlung von Viruserkrankungen。
公开(公告)号：EP0498095A1
公开(公告)日：1992-08-12
申请号：EP91300914.8
申请日：1991-02-05
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Cardin, Alan D. , Tyms, Stanley A.
IPC分类号： C07C331/28 , C07C331/30 , C07C309/40 , C07C309/51 , A61K31/095 , A61K31/26 , A61K31/165 , A61K31/275 , A61K31/135
CPC分类号： C07C331/30 , A61K31/185 , A61K31/26 , A61K31/275 , C07C331/28
摘要： Sulfonic acid stilbenes block the infection of cells by HSV, HIV and CMV and these compounds can be used to prevent viral infection.
摘要翻译：磺酸二苯乙烯通过HSV，HIV和CMV阻断细胞的感染，这些化合物可用于预防病毒感染。

8. 发明公开

EP0467185A2 Oligomers, their uses and formulations 失效
标题翻译： Oligomere，我是Verwendungen sowie Formulierungen。
公开(公告)号：EP0467185A2
公开(公告)日：1992-01-22
申请号：EP91111315.7
申请日：1991-07-08
申请人： THE DOW CHEMICAL COMPANY , MERRELL DOW PHARMACEUTICALS INC.
发明人： Cardin, Alan D. , Jackson, Richard L. , Mullins, Michael J.
IPC分类号： C08G71/02 , C08G64/08 , C08G63/688 , C08G69/32 , C07C309/51 , C07C309/42 , A61K31/795 , A61K31/74
CPC分类号： A61K31/185 , A61K31/785 , A61K31/795 , C07C309/42 , C07C309/51 , C08G63/19 , C08G63/6884 , C08G63/6924 , C08G64/06 , C08G64/081 , C08G64/083 , C08G69/26 , C08G69/32 , C08G71/02 , Y10S514/885
摘要： The preferred oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a number average molecular weight of
摘要翻译：本发明优选的低聚物是数均分子量<10,000的聚脲，聚碳酸酯，聚酯或聚酰胺。这些低聚物是水溶性的，具有刚性主链，具有通过具有阴离子基团的羰基连接部分偶联的重复单元，主要显示出线性几何形式，使得阴离子基团之间的规则间隔存在于水性介质中，并且是药学上可接受的。低聚物可用于治疗和/或诊断AIDS和ARC。

9. 发明公开

EP0404055A1 Ghilanten: antimetastatic principle from the south american leech, haementeria ghilianii 失效
标题翻译： Ghilanten：antimetastatischer Wirkstoff aus demsüdamerikanischenBlutegel Haementeria Ghilianii。
公开(公告)号：EP0404055A1
公开(公告)日：1990-12-27
申请号：EP90111551.9
申请日：1990-06-19
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Cardin, Alan D. , Sunkara, Sai Prasad
IPC分类号： A61K37/02
CPC分类号： C07K14/815 , A61K38/00 , Y10S530/856 , Y10S530/858
摘要： A method for the inhibition of tumor metastases is described herein. The method makes use of the administration of an antimetastatic factor isolated from the leech Haementeria ghilianii .
摘要翻译：本文描述了抑制肿瘤转移的方法。该方法利用从水蛭Haementeria ghilianii分离的抗转移因子的施用。

10. 发明授权

EP0346894B1 Extraction and purification of an anticoagulant substance from the south american leech, haementeria ghilianii 失效
标题翻译：提取和纯化从南美水蛭Haementeria ghilianii的抗凝血物质。
公开(公告)号：EP0346894B1
公开(公告)日：1995-02-01
申请号：EP89110877.1
申请日：1989-06-15
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Cardin, Alan D.
IPC分类号： C07K1/16 , C07K14/815 , A61K38/58
CPC分类号： C07K14/815 , A61K38/00 , Y10S435/815 , Y10S514/822 , Y10S530/855

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