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1. 发明授权

US06559174B2 N-arylsulfonyl aryl aza-bicyclic derivatives as potent cell adhesion inhibitors 失效
公开(公告)号：US06559174B2
公开(公告)日：2003-05-06
申请号：US10097028
申请日：2002-03-13
申请人： Linus S. Lin , Shrenik K. Shah , Linda L. Chang , William K. Hagmann , Richard A. Mumford
发明人： Linus S. Lin , Shrenik K. Shah , Linda L. Chang , William K. Hagmann , Richard A. Mumford
IPC分类号： A61K3147
CPC分类号： C07D401/12 , A61K31/4709 , A61K31/4745 , C07D401/14 , C07D487/04
摘要： Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

2. 发明授权

US5420010A Assay for evaluating inhibition of polymorphonuclear leukocyte elastase by N-substituted azetidinones 失效
标题翻译：用N-取代的氮杂环丁酮评价多形核白细胞弹性蛋白酶的抑制作用
公开(公告)号：US5420010A
公开(公告)日：1995-05-30
申请号：US100532
申请日：1993-07-30
申请人： Paul E. Finke , William K. Hagmann , William A. Hanlon , John L. Humes , Wilson B. Knight , Malcolm MacCoss , Richard A. Mumford , Shrenik K. Shah
发明人： Paul E. Finke , William K. Hagmann , William A. Hanlon , John L. Humes , Wilson B. Knight , Malcolm MacCoss , Richard A. Mumford , Shrenik K. Shah
IPC分类号： C07D317/58 , C07D405/12 , G01N33/573 , C07D317/60 , C07K16/44
CPC分类号： C07D405/12 , C07D317/58 , Y10S436/822
摘要： N-substituted azetidinones are a class of inhibitors of human leukocytes elastase which are known to be useful in the treatment of a wide variety of antiinflammatory and antidegenerative diseases. In inhibiting elastase, the therapeutic agents are shown to form a characteristic stable complex with the enzyme. In the assay disclosed herein, the inhibitor-enzyme complex is advantageously hydrolyzed and specific product(s) of the hydrolysis are measured. The assays are useful in a clinical setting, for determining appropriate dosage and assessing the effectiveness of treatment.
摘要翻译： N-取代的氮杂环丁酮是人类白细胞弹性蛋白酶抑制剂的一类，其已知可用于治疗各种抗炎和抗生殖疾病。在抑制弹性蛋白酶时，治疗剂显示与酶形成特征稳定的复合物。在本文公开的测定中，抑制剂 - 酶复合物有利地水解，并测量水解的特定产物。该测定在临床环境中有用，用于确定适当的剂量和评估治疗的有效性。

3. 发明授权

US5276139A Haptens useful in evaluating inhibition of PNN elastase by N-substituted azetidinones 失效
标题翻译：用于评估N-取代的氮杂环丁酮对PMN弹性蛋白酶抑制作用的半抗原
公开(公告)号：US5276139A
公开(公告)日：1994-01-04
申请号：US750148
申请日：1991-08-26
申请人： Paul E. Finke , William K. Hagmann , Richard A. Mumford , Shrenik K. Shah
发明人： Paul E. Finke , William K. Hagmann , Richard A. Mumford , Shrenik K. Shah
IPC分类号： C07C275/28 , C07C275/40 , C07D307/79 , C07K16/44 , C12Q1/37 , G01N33/94 , C07K3/08 , C07C275/04 , G01N33/68
CPC分类号： C07D307/79 , C07C275/28 , C07C275/40 , C07K16/44 , C12Q1/37 , G01N33/94 , G01N2333/966 , G01N2800/52 , Y10S530/807
摘要： N-substituted azetidinones are a class of inhibitors of human leukocytes elastase which are known to be useful in the treatment of a wide variety of antiinflammatory and antidegenerative diseases. In inhibiting elastase, the therapeutic agents are shown to form a characteristic stable complex with the enzyme. In the radioimmune assay disclosed herein, the inhibitor-enzyme complex is advantageously hydrolyzed and specific product(s) of the hydrolysis are measured. The assays are useful in a clinical setting, for determining appropriate dosage and assessing the effectiveness of treatment.
摘要翻译： N-取代的氮杂环丁酮是人类白细胞弹性蛋白酶抑制剂的一类，其已知可用于治疗各种抗炎和抗生殖疾病。在抑制弹性蛋白酶时，治疗剂显示与酶形成特征稳定的复合物。在本文公开的放射免疫测定中，抑制剂 - 酶复合物有利地水解，并测量水解的特定产物。该测定在临床环境中有用，用于确定适当的剂量和评估治疗的有效性。

4. 发明授权

US5109112A FK-506 cytosolic binding protein 失效
标题翻译： FK-506胞质结合蛋白
公开(公告)号：US5109112A
公开(公告)日：1992-04-28
申请号：US548429
申请日：1990-07-05
申请人： John J. Siekierka , Hsuen-Yun Hung , Marie J. Staruch , Nolan H. Sigal , Richard A. Mumford
发明人： John J. Siekierka , Hsuen-Yun Hung , Marie J. Staruch , Nolan H. Sigal , Richard A. Mumford
IPC分类号： C12N9/90 , C12N15/90
CPC分类号： C12N15/90 , C12N9/90 , Y10S530/81 , Y10S530/827
摘要： A new homogeneous cytosolic binding (HCB) protein, having a specific binding activity of about 26 .mu.g 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: H.sub.2 N-Gly-Val-Gln-Val-Glu-Thr-Ile-Ser-Pro- Gly-Asp-Gly-Arg-Thr-Phe-Pro-Lys- Ar g-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 catalyzes the cis-trans isomerization of proline-containing peptide bonds.
摘要翻译：具有约26μgFK-506 / mg蛋白的特异性结合活性和约10-12千道尔顿分子量的新的均匀胞质结合（HCB）蛋白可逆地结合免疫抑制剂FK-506而不是环孢菌素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-Lys-Ar g-Gly-Gln-Thr-X-Val-Val-His-Tyr-Thr-Gly-Met-Leu-Glu-Asp -Gly-Lys-Lys-Ph e-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，优选人类肿瘤T细胞系，例如Jurkat，并且可用于涉及FK-506大环内酯型免疫抑制剂的诊断和纯化方法。 HCB蛋白还催化含脯氨酸的肽键的顺式 - 反式异构化。

5. 发明授权

US08283344B2 Method of treating inherited severe neutropenia 有权
标题翻译：治疗遗传性严重中性粒细胞减少症的方法
公开(公告)号：US08283344B2
公开(公告)日：2012-10-09
申请号：US12673588
申请日：2008-09-05
申请人： David C. Dale , Paul E. Finke , Richard A. Mumford , Andranik Andrew Aprikyan
发明人： David C. Dale , Paul E. Finke , Richard A. Mumford , Andranik Andrew Aprikyan
IPC分类号： A01N43/00 , A61K31/397 , A61K31/407
CPC分类号： A61K31/4965 , A61K31/36
摘要： The invention is directed to a method of treating severe neutropenia, and in particular, cyclic neutropenia (CN) or severe congenital neutropenia (SCN), in a patient in need of such treatment comprising: administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及在需要这种治疗的患者中治疗严重中性粒细胞减少症，特别是循环中性粒细胞减少症（CN）或严重先天性中性粒细胞减少症（SCN）的方法，其包括：施用治疗有效量的式 I）或其药学上可接受的盐。

6. 发明授权

US06855708B2 N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors 失效
标题翻译： N-芳基磺酰基氮杂双环衍生物作为有效的细胞粘附抑制剂
公开(公告)号：US06855708B2
公开(公告)日：2005-02-15
申请号：US10096607
申请日：2002-03-13
申请人： Linus S. Lin , George Doherty , Shrenik K. Shah , Linda L. Chang , William K. Hagmann , Richard A. Mumford
发明人： Linus S. Lin , George Doherty , Shrenik K. Shah , Linda L. Chang , William K. Hagmann , Richard A. Mumford
IPC分类号： C07D401/12 , C07D487/04 , C07D498/04 , A61K31/55 , A61K31/47
CPC分类号： C07D401/12 , C07D487/04
摘要： Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
摘要翻译：式I的化合物是VLA-4和/或α4/β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎，接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎症性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，视网膜炎，类风湿性关节炎，败血症关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

7. 发明授权

US06348570B1 Chromophore containing compounds and their use in determining interleukin-1&bgr; convertase activity 失效
标题翻译：含有发色团的化合物及其在确定白细胞介素-1β转化酶活性中的应用
公开(公告)号：US06348570B1
公开(公告)日：2002-02-19
申请号：US07808994
申请日：1991-12-17
申请人： Kevin T. Chapman , Malcolm Maccoss , Richard A. Mumford , Nancy A. Thornberry , Jeffrey R. Weidner , William K. Hagmann
发明人： Kevin T. Chapman , Malcolm Maccoss , Richard A. Mumford , Nancy A. Thornberry , Jeffrey R. Weidner , William K. Hagmann
IPC分类号： A61K3804
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-1&bgr; 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; 包括心包的心血管系统; 胃肠道和泌尿生殖系统; 皮肤和粘膜。

8. 发明授权

US5766909A DNA encoding inducible nitric oxide synthase 失效
标题翻译：编码诱导型一氧化氮合酶的DNA
公开(公告)号：US5766909A
公开(公告)日：1998-06-16
申请号：US147812
申请日：1993-11-05
申请人： Qiao-Wen Xie , Carl F. Nathan , Richard A. Mumford , Jimmy Ramos Calaycay
发明人： Qiao-Wen Xie , Carl F. Nathan , Richard A. Mumford , Jimmy Ramos Calaycay
IPC分类号： C12N1/21 , C12N9/02 , C12N5/10 , C12N15/53
CPC分类号： C12N9/0075
摘要： Complementary DNAs (cDNAs) encoding inducible nitric oxide synthase are isolated and purified from a cDNA library prepared from macrophage-like cells activated with interferon gamma and bacterial lipopolysaccharide. The full length cDNAs of at least two isoforms of the enzyme are identified and sequenced.
摘要翻译：从用干扰素γ和细菌脂多糖活化的巨噬细胞样细胞制备的cDNA文库中分离和纯化编码诱导型一氧化氮合酶的互补DNA（cDNA）。鉴定并测序该酶的至少两种同工型的全长cDNA。

9. 发明授权

US5274080A Monospecific antibodies useful in evaluating inhibition of polymorphonuclear leukocyte elastase by N-substituted azetidinones 失效
标题翻译：单特异性抗体可用于评估N-取代的氮杂环丁酮对多形核白细胞弹性蛋白酶的抑制
公开(公告)号：US5274080A
公开(公告)日：1993-12-28
申请号：US750139
申请日：1991-08-26
申请人： Malcolm MacCoss , Richard A. Mumford
发明人： Malcolm MacCoss , Richard A. Mumford
IPC分类号： C07C275/28 , C07C275/40 , C07D307/79 , C07K16/44 , C12Q1/37 , G01N33/94 , C07K15/00 , C07C273/02
CPC分类号： C07D307/79 , C07C275/28 , C07C275/40 , C07K16/44 , C12Q1/37 , G01N33/94 , G01N2333/966 , G01N2800/52 , Y10S530/807
摘要： Inhibitors of human leukocytes elastase are known to be useful in the treatment of a wide variety of antiinflammatory and antidegenerative diseases. In inhibiting elastase, the therapeutic agents are shown to form a characteristic stable complex with the enzyme. In the radioimmunoassay disclosed herein, the inhibitor-enzyme complex is advantageously hydrolyzed and specific product(s) of the hydrolysis are measured utilizing polyclonal antibodies capable of binding to one or more haptens of formula II ##STR1## wherein M is allyl or n-propyl,Z.sub.1 is(a) 5-benzofuranyl or(b) substituted phenyl wherein the substituent is methyl or ethyloxy.The assays utilizing these antibodies are useful in a clinical setting, for determining appropriate dosage and assessing the effectiveness of treatment.
摘要翻译：已知人白细胞弹性蛋白酶抑制剂可用于治疗各种抗炎和抗发生性疾病。在抑制弹性蛋白酶时，治疗剂显示与酶形成特征稳定的复合物。在本文公开的放射免疫测定中，抑制剂 - 酶复合物有利地水解，并且使用能够结合一种或多种式II的半抗原的多克隆抗体测量水解的特定产物，其中M是烯丙基或正丙基，丙基，Z 1是（a）5-苯并呋喃基或（b）取代的苯基，其中取代基是甲基或乙氧基。使用这些抗体的测定可用于临床环境，用于确定适当的剂量和评估治疗的有效性。

10. 发明授权

US06943180B2 Substituted N-arylsulfonyl-proline derivatives as potent cell adhesion inhibitors 失效
标题翻译：取代的N-芳基磺酰基 - 脯氨酸衍生物作为有效的细胞粘附抑制剂
公开(公告)号：US06943180B2
公开(公告)日：2005-09-13
申请号：US10472303
申请日：2002-03-15
申请人： George Doherty , Linus S Lin , William K. Hagmann , Ginger Xu-qiang Yang , Linda L. Chang , Shrenik K. Shah , Richard A. Mumford , Theodore Kamenecka
发明人： George Doherty , Linus S Lin , William K. Hagmann , Ginger Xu-qiang Yang , Linda L. Chang , Shrenik K. Shah , Richard A. Mumford , Theodore Kamenecka
IPC分类号： A61K38/00 , A61P1/04 , A61P11/02 , A61P11/06 , A61P25/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D401/12 , C07D401/14 , C07K5/078 , C07D215/20 , A61K31/47
CPC分类号： C07D401/12 , C07D401/14
摘要： Compounds of formula (I) are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, rhinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
摘要翻译：式（I）化合物是VLA-4和/或α4/β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病症。这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎，接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，鼻炎，类风湿性关节炎，败血症关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

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