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1. 发明公开

EP0533226A3 Novel chromophore containing compounds 失效
标题翻译：含有新化合物的化合物
公开(公告)号：EP0533226A3
公开(公告)日：1993-08-18
申请号：EP92202449.2
申请日：1992-08-08
申请人： MERCK & CO. INC.
发明人： Chapman, Kevin T. , Maccoss, Malcolm , Mumford, Richard A. , Thornberry, Nancy A. , Weidner, Jeffrey R.
IPC分类号： C07K5/10 , C12Q1/37
CPC分类号： C07K5/1016 , C07K14/545
摘要： Disclosed are novel chromophore containing compounds of Formula II and their use in determining interleukin-1 β convertase (ICE) activity. ICE has been implicated in inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes.
摘要翻译：公开了含有式II化合物的新颖发色团及其在测定白细胞介素-1β转化酶（ICE）活性中的用途。 ICE已经涉及肺和气道的炎性或免疫性疾病; 中枢神经系统和周围膜; 眼睛和耳朵关节，骨骼和结缔组织; 心包系统包括心包; 胃肠道和泌尿生殖系统; 皮肤和粘膜。 v

2. 发明公开

EP0345906A2 Unique elastase induced fibrinogen cleavage site antigens 有权转让
标题翻译： Antigene der einzigen Spaltungsstelle von Fibrinogen durch Elastase。
公开(公告)号：EP0345906A2
公开(公告)日：1989-12-13
申请号：EP89201460.6
申请日：1989-06-07
申请人： Merck & Co., Inc.
发明人： Dahlgren, Mary E. , Mumford, Richard A. , Boger, Joshua S. , Davies, D.T. Philip
IPC分类号： C07K7/06 , C07K14/75 , A61K38/36 , G01N33/68
CPC分类号： G01N33/6878 , C07K14/75 , C07K16/36 , G01N33/86 , G01N2333/75
摘要： Novel peptides associated with the amino and carboxyl termini of human leukocyte elastase cleavage sites of human fibrinogen are disclosed. The peptides are used to raise antibodies which are specific for as few as five amino acids on either side of the enzymatic cleavage site. The unique peptides are also used in novel assays for the rapid determination of in vivo and in vitro elastase cleavage products.
摘要翻译：公开了与人纤维蛋白原的人白细胞弹性蛋白酶切割位点的氨基和羧基末端相关的新肽。肽用于产生在酶切割位点的任一侧上至少5个氨基酸特异的抗体。独特的肽也用于快速测定体内和体外弹性蛋白酶裂解产物的新型测定。

3. 发明公开

EP0528487A3 Novel chromophore containing compounds 失效
标题翻译：含有新化合物的化合物
公开(公告)号：EP0528487A3
公开(公告)日：1993-08-18
申请号：EP92202450.0
申请日：1992-08-08
申请人： MERCK & CO. INC.
发明人： Chapman, Kevin T. , Thornberry, Nancy A. , Maccoss, Malcolm , Weidner, Jeffrey R. , Mumford, Richard A. , Hagmann, William K.
IPC分类号： C07K5/10 , C12Q1/37
CPC分类号： C07K5/1016 , C07K14/545
摘要： Disclosed are novel chromophore containing compounds of Formula I and their use in determining interleukin-1β convertase (ICE) activity. ICE has been implicated in inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes.
摘要翻译：公开了含有式I化合物的新颖发色团及其在测定白细胞介素-1β转化酶（ICE）活性中的用途。 ICE已经涉及肺和气道的炎性或免疫性疾病; 中枢神经系统和周围膜; 眼睛和耳朵关节，骨骼和结缔组织; 心包系统包括心包; 胃肠道和泌尿生殖系统; 皮肤和粘膜。 v

4. 发明公开

EP0525973A2 Substituted azetidinones as anti-inflammatory and antidegenerative agents 失效
标题翻译：取代基Azetidinone als Antiphlogistika und antidegenerative Wirkstoffe。
公开(公告)号：EP0525973A2
公开(公告)日：1993-02-03
申请号：EP92305820.0
申请日：1992-06-24
申请人： MERCK & CO. INC.
发明人： Finke, Paul E. , Kissinger, Amy L. , Maccoss, Malcolm , Shah, Shrenik K. , Doherty, James B. , Hagmann, William K. , Davies, Philip , Humes, John L. , Luedke, Edward S. , Mumford, Richard A.
IPC分类号： C07D205/08 , C07D307/81 , C07D317/58 , C07D401/12 , C07D403/12 , A61K31/295
CPC分类号： C07D405/12 , C07D205/08
摘要： New substituted azetidinones of the general formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.
摘要翻译：描述了已经被发现是有效的弹性蛋白酶抑制剂，从而有用的抗炎和抗再生剂的通式（I）的新的取代的氮杂环丁酮。

5. 发明公开

EP0379342A2 New FK-506 cytosolic binding protein 失效转让
标题翻译：蛋白质蛋白酶Cytosol，das FK-506 binden kann。
公开(公告)号：EP0379342A2
公开(公告)日：1990-07-25
申请号：EP90300459.6
申请日：1990-01-17
申请人： Merck & Co., Inc.
发明人： Siekierka, John J. , Staruch, Marie J. , Sigal, Nolan H. , Mumford, Richard A. , Hung, Hsueh-Yun
IPC分类号： C07K15/12 , G01N33/68
CPC分类号： C12N9/90 , C12N15/90
摘要： A new homogeneous cytosolic binding (HCB) protein, having a specific binding activity of about 26 µg FK-506 per mg protein and a molecular weight of about 10-12 kilodaltons, reversibly binds the immunosuppressant FK-506 but not cyclosporine A (CSA). The protein is stable to heating at 56 degrees C. for 30 minutes retaining its FK-506 binding affinity, and has the (partial) amino terminal amino acid sequence: H₂N-Gly-Val-Gln-Val-Glu-Thr-Ile-Ser-Pro-Gly-Asp-Gly-Arg-Thr-Phe-Pro-Lys-Arg-Gly-Gln-Thr-X-Val-Val-His-Tyr-Thr-Gly-Met-Leu-Glu-Asp-Gly-Lys-Lys-Phe-Asp (wherein X is undefined). The HCB protein is isolated from the cytosol of mammalian tissues, preferably human neoplastic T-cell lines, e.g. Jurkat, and can be used in diagnostic and purification procedures involving FK-506 macrolide type immunosuppressants. The HCB protein also catalyses the cis-trans isomerization of proline-containing peptide bonds.
摘要翻译：具有约26μgFK-506 / mg蛋白质和约10-12千道尔顿分子量的特异性结合活性的新的均匀胞质结合（HCB）蛋白可逆地结合免疫抑制剂FK-506而不是环孢霉素A（CSA ）。蛋白质在56℃下加热稳定30分钟，保持其FK-506结合亲和力，并具有（部分）氨基末端氨基酸序列：H2N-Gly-Val-Gln-Val-Glu-Thr-Ile- Ser-Pro-Gly-Asp-Gly-Arg-Thr-Phe-Pro-Ly-Arg-Gly-Gln-Thr-X-Val-Val-His-Tyr-Thr-Gly-Met-Leu-Glu-Asp -Gly-Lys-Lys-Phe-Asp（其中X未定义）。 HCB蛋白从哺乳动物组织的细胞溶质中分离，优选人肿瘤T细胞系，例如， Jurkat，可用于涉及FK-506大环内酯型免疫抑制剂的诊断和纯化程序。 HCB蛋白还催化含脯氨酸肽键的顺式 - 反式异构化。

6. 发明授权

EP0379342B1 New FK-506 cytosolic binding protein 失效转让
标题翻译：从胞质溶胶蛋白时，FK-506可结合。
公开(公告)号：EP0379342B1
公开(公告)日：1994-10-05
申请号：EP90300459.6
申请日：1990-01-17
申请人： Merck & Co., Inc.
发明人： Siekierka, John J. , Staruch, Marie J. , Sigal, Nolan H. , Mumford, Richard A. , Hung, Hsueh-Yun
IPC分类号： C07K15/12 , G01N33/68
CPC分类号： C12N9/90 , C12N15/90

7. 发明公开

EP0525973A3 Substituted azetidinones as anti-inflammatory and antidegenerative agents 失效
标题翻译：取代的AZETIDINONES作为抗炎和抗感染药物
公开(公告)号：EP0525973A3
公开(公告)日：1993-03-03
申请号：EP92305820.0
申请日：1992-06-24
申请人： MERCK & CO. INC.
发明人： Finke, Paul E. , Kissinger, Amy L. , Maccoss, Malcolm , Shah, Shrenik K. , Doherty, James B. , Hagmann, William K. , Davies, Philip , Humes, John L. , Luedke, Edward S. , Mumford, Richard A.
IPC分类号： C07D205/08 , C07D307/81 , C07D317/58 , C07D401/12 , C07D403/12 , A61K31/295
CPC分类号： C07D405/12 , C07D205/08
摘要： New substituted azetidinones of the general formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.
摘要翻译：描述了已经被发现是有效的弹性蛋白酶抑制剂，从而有用的抗炎和抗再生剂的通式（I）的新的取代的氮杂环丁酮。

8. 发明公开

EP0379342A3 New FK-506 cytosolic binding protein 失效转让
标题翻译：新FK-506 CYTOSOLIC结合蛋白
公开(公告)号：EP0379342A3
公开(公告)日：1990-11-28
申请号：EP90300459.6
申请日：1990-01-17
申请人： Merck & Co., Inc.
发明人： Siekierka, John J. , Staruch, Marie J. , Sigal, Nolan H. , Mumford, Richard A. , Hung, Hsueh-Yun
IPC分类号： C07K15/12 , G01N33/68
CPC分类号： C12N9/90 , C12N15/90
摘要： A new homogeneous cytosolic binding (HCB) protein, having a specific binding activity of about 26 µg FK-506 per mg protein and a molecular weight of about 10-12 kilodaltons, reversibly binds the immunosuppressant FK-506 but not cyclosporine A (CSA). The protein is stable to heating at 56 degrees C. for 30 minutes retaining its FK-506 binding affinity, and has the (partial) amino terminal amino acid sequence: H₂N-Gly-Val-Gln-Val-Glu-Thr-Ile-Ser-Pro-Gly-Asp-Gly-Arg-Thr-Phe-Pro-Lys-Arg-Gly-Gln-Thr-X-Val-Val-His-Tyr-Thr-Gly-Met-Leu-Glu-Asp-Gly-Lys-Lys-Phe-Asp (wherein X is undefined). The HCB protein is isolated from the cytosol of mammalian tissues, preferably human neoplastic T-cell lines, e.g. Jurkat, and can be used in diagnostic and purification procedures involving FK-506 macrolide type immunosuppressants. The HCB protein also catalyses the cis-trans isomerization of proline-containing peptide bonds.

9. 发明授权

EP0345906B1 Unique elastase induced fibrinogen cleavage site antigens 有权转让
标题翻译：通过弹性蛋白酶纤维蛋白原的单裂解位点的抗原
公开(公告)号：EP0345906B1
公开(公告)日：1996-03-13
申请号：EP89201460.6
申请日：1989-06-07
申请人： MERCK & CO. INC.
发明人： Dahlgren, Mary E. , Mumford, Richard A. , Boger, Joshua S. , Davies, D.T. Philip
IPC分类号： C07K7/06 , C07K14/75 , A61K38/36 , G01N33/68
CPC分类号： G01N33/6878 , C07K14/75 , C07K16/36 , G01N33/86 , G01N2333/75

10. 发明公开

EP0533226A2 Novel chromophore containing compounds 失效
标题翻译：新型含发色团的化合物
公开(公告)号：EP0533226A2
公开(公告)日：1993-03-24
申请号：EP92202449.2
申请日：1992-08-08
申请人： MERCK & CO. INC.
发明人： Chapman, Kevin T. , Maccoss, Malcolm , Mumford, Richard A. , Thornberry, Nancy A. , Weidner, Jeffrey R.
IPC分类号： C07K5/10 , C12Q1/37
CPC分类号： C07K5/1016 , C07K14/545
摘要： Disclosed are novel chromophore containing compounds of Formula II and their use in determining interleukin-1 β convertase (ICE) activity. ICE has been implicated in inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes.
摘要翻译：公开了新颖的含发色团的式II化合物及其在测定白细胞介素-1β转化酶（ICE）活性中的用途。 ICE与肺和呼吸道的炎症或基于免疫的疾病有关; 中枢神经系统和周围的膜; 眼睛和耳朵; 关节，骨骼和结缔组织; 包括心包在内的心血管系统; 胃肠道和泌尿生殖系统; 皮肤和粘膜。

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