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公开(公告)号：US08569259B2
公开(公告)日：2013-10-29
申请号：US12515033
申请日：2007-11-16
申请人： Efrat Ben-Zeev , Vincent Jacques , Yael Marantz , A. Sekar Reddy , Zhaoda Zhang , Oren Becker , Dilara McCauley , Pini Orbach , Sharon Shacham , Ashis K. Saha , Michael Xie
发明人： Efrat Ben-Zeev , Vincent Jacques , Yael Marantz , A. Sekar Reddy , Zhaoda Zhang , Oren Becker , Dilara McCauley , Pini Orbach , Sharon Shacham , Ashis K. Saha , Michael Xie
CPC分类号： A61K31/7076 , A61K31/7034 , A61K31/7072 , C07H15/203 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00
摘要： Provided are adenosine analog compounds of the general formula that act as P2Y receptors, e.g., the P2Y2 receptor, including pharmaceutical compositions; and uses thereof to treat or prevent diseases associated with that receptor, e.g., disorders relating to mucus secretion, such as cystic fibrosis, chronic obstructive pulmonary disorder (COPD), asthma, constipation, chronic idiopathic constipation, dry mouth (xerostomia), gum disease, and gastrointestinal problems caused by radiation and chemotherapy for cancer.
摘要翻译： 提供了作为P2Y受体的通式的腺苷类似物化合物，例如P2Y2受体，包括药物组合物; （COPD），哮喘，便秘，慢性特发性便秘，口干（口腔干燥症），牙龈疾病 ，以及由辐射和化学治疗癌症引起的胃肠道问题。
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公开(公告)号：US20110237529A1
公开(公告)日：2011-09-29
申请号：US12515033
申请日：2007-11-16
申请人： Efrat Ben-Zeev , Vincent Jacques , Yael Marantz , A. Sekar Reddy , Zhaoda Zhang , Oren Becker , Dilara Mccauley , Pini Orbach , Sharon Shacham , Ashis K. Saha , Michael Xie
发明人： Efrat Ben-Zeev , Vincent Jacques , Yael Marantz , A. Sekar Reddy , Zhaoda Zhang , Oren Becker , Dilara Mccauley , Pini Orbach , Sharon Shacham , Ashis K. Saha , Michael Xie
IPC分类号： A61K31/7076 , C07H15/203 , C07H7/04 , C07H7/06 , C07H17/02 , C07H19/20 , A61K31/7064 , A61P11/00 , A61P1/04 , A61P1/02 , A61P1/00 , A61P1/10 , C12N5/071
CPC分类号： A61K31/7076 , A61K31/7034 , A61K31/7072 , C07H15/203 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00
摘要： The invention provides adenosine analog compounds that act at P2Y receptors, e.g., the P2Y2 receptor, including pharmaceutical compositions; and uses thereof to treat or prevent diseases associated with that receptor, e.g., disorders relating to mucus secretion, such as cystic fibrosis, chronic obstructive pulmonary disorder (COPD), asthma, constipation, chronic idiopathic constipation, dry mouth (xerostomia), gum disease, and gastrointestinal problems caused by radiation and chemotherapy for cancer.
摘要翻译： 本发明提供了在P2Y受体（例如P2Y2受体）上起作用的腺苷类似物化合物，包括药物组合物; （COPD），哮喘，便秘，慢性特发性便秘，口干（口腔干燥症），牙龈疾病 ，以及由辐射和化学治疗癌症引起的胃肠道问题。
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公开(公告)号：US20100210633A1
公开(公告)日：2010-08-19
申请号：US12445134
申请日：2007-10-12
申请人： Jian Lin , Dongli Chen , Steffi Koerner , Rosa E. Melendez , Pradyumma Mohanty , Efrat Ben-Zeev , Merav Fichman , Yael Marantz , Oren Becker , Dilara McCauley , Pini Orbach , Ashis K. Saha , Sharon Shacham , Michael Xie
发明人： Jian Lin , Dongli Chen , Steffi Koerner , Rosa E. Melendez , Pradyumma Mohanty , Efrat Ben-Zeev , Merav Fichman , Yael Marantz , Oren Becker , Dilara McCauley , Pini Orbach , Ashis K. Saha , Sharon Shacham , Michael Xie
IPC分类号： A61K31/541 , C07D405/06 , A61K31/453 , A61P3/10 , A61P3/04 , A61P37/06 , A61P17/06 , A61P9/10 , A61P13/12 , A61P1/16 , C07D211/62 , A61K31/445 , C07D207/16 , A61K31/40 , A61K31/4525 , C07D413/10 , A61K31/454 , C07D405/14 , A61K31/496 , C07D401/06 , A61K31/4545 , C07D401/04 , C07D417/06 , C07D413/06 , A61K31/5377
CPC分类号： C07D405/06 , C07D207/08 , C07D207/16 , C07D211/62 , C07D401/04 , C07D401/06 , C07D401/10 , C07D405/14 , C07D407/06 , C07D409/14 , C07D411/14 , C07D413/06 , C07D413/10 , C07D417/06 , C07D417/14
摘要： Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
摘要翻译： 本文描述了趋化因子受体拮抗剂，特别是作为趋化因子CCR2受体的拮抗剂的式（I）化合物，包括药物组合物及其用于治疗或预防与单核细胞积聚，淋巴细胞积聚或白细胞积聚相关的疾病的用途。
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公开(公告)号：US07855193B2
公开(公告)日：2010-12-21
申请号：US11491766
申请日：2006-07-24
申请人： Ashis K. Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa R. Cheruku , Pini Orbach , Anurag Sharadendu , Robert Christian Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker
发明人： Ashis K. Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa R. Cheruku , Pini Orbach , Anurag Sharadendu , Robert Christian Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker
IPC分类号： A61K31/397 , A61K31/5377 , A61K31/4525 , A61K31/4025 , A61K31/343 , C07D411/06 , C07D405/06 , C07D205/04 , C07D307/80
CPC分类号： C07D405/10 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/10 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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公开(公告)号：US20080064677A9
公开(公告)日：2008-03-13
申请号：US11491766
申请日：2006-07-24
申请人： Ashis K. Saha , Nili Schutz , Anurag Sharadendu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Rao Cheruku , Pini Orbach , Anurag Sharadendu , Robert Christian Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker
发明人： Ashis K. Saha , Nili Schutz , Anurag Sharadendu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Rao Cheruku , Pini Orbach , Anurag Sharadendu , Robert Christian Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker
IPC分类号： A61K31/452 , A61K31/397 , C07D405/02
CPC分类号： C07D405/10 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/10 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behcet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，贝切特氏病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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公开(公告)号：US20070173487A1
公开(公告)日：2007-07-26
申请号：US11491766
申请日：2006-07-24
申请人： Ashis K. Saha , Nili Schutz , Anurag Sharadendu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Rao Cheruku , Pini Orbach , Anurag Sharadendu , Robert Christian Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker
发明人： Ashis K. Saha , Nili Schutz , Anurag Sharadendu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Rao Cheruku , Pini Orbach , Anurag Sharadendu , Robert Christian Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker
IPC分类号： A61K31/452 , A61K31/397 , C07D405/02
CPC分类号： C07D405/10 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/10 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behcet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，贝切特氏病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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公开(公告)号：US20110059945A1
公开(公告)日：2011-03-10
申请号：US12945572
申请日：2010-11-12
申请人： Ashis K. Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Cheruku , Pini Orbach , Anurag Sharadendu , Robert Christian Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker
发明人： Ashis K. Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Cheruku , Pini Orbach , Anurag Sharadendu , Robert Christian Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker
IPC分类号： A61K31/397 , A61P37/06 , A61P35/00 , A61P19/00 , A61P3/10 , A61P35/04 , A61P11/06 , A61P9/10 , A61P13/12 , A61P1/16 , A61K31/4525 , A61K31/4725 , A61K31/5377 , A61K31/343
CPC分类号： C07D405/10 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/10 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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公开(公告)号：US20110212940A1
公开(公告)日：2011-09-01
申请号：US13034895
申请日：2011-02-25
申请人： Roland Burli , Victor J. Cee , Jennifer Golden , Brian Alan Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa R. Cheruku , Pini Orbach , Anurag Sharadendu , Robert C. Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
发明人： Roland Burli , Victor J. Cee , Jennifer Golden , Brian Alan Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa R. Cheruku , Pini Orbach , Anurag Sharadendu , Robert C. Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
IPC分类号： A61K31/397 , C07D405/10 , A61K31/4525 , C07D405/14 , A61K31/443 , C07D413/14 , A61K31/427 , C07D409/14 , A61K31/4725 , A61K31/4025 , C07D307/80 , A61K31/343 , A61K31/5377 , C07D413/10 , A61K31/41 , A61P35/00 , A61P37/06 , A61P29/00 , A61P3/10 , A61P25/00 , A61P17/06 , A61P35/02 , A61P11/00 , A61P11/06 , A61P17/02 , A61P9/00 , A61P9/10 , A61P13/12 , A61P1/16 , A61P7/06
CPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04 , C07D491/048
摘要： The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
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公开(公告)号：US07919519B2
公开(公告)日：2011-04-05
申请号：US11726351
申请日：2007-03-21
申请人： Roland Burli , Victor J. Cee , Jennifer Golden , Brian Alan Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa R. Cheruku , Pini Orbach , Anurag Sharadendu , Robert C. Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
发明人： Roland Burli , Victor J. Cee , Jennifer Golden , Brian Alan Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa R. Cheruku , Pini Orbach , Anurag Sharadendu , Robert C. Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
IPC分类号： A61K31/404 , A61K31/381 , A61K31/343 , C07D209/12 , C07D333/56 , C07D307/80
CPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04 , C07D491/048
摘要： The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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公开(公告)号：US20080027036A1
公开(公告)日：2008-01-31
申请号：US11726351
申请日：2007-03-21
申请人： Roland Burli , Victor Cee , Jennifer Golden , Brian Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Cheruku , Pini Orbach , Anurag Sharadendu , Robert Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
发明人： Roland Burli , Victor Cee , Jennifer Golden , Brian Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Cheruku , Pini Orbach , Anurag Sharadendu , Robert Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
IPC分类号： A61K31/397 , A61K31/343 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/5377 , A61P1/00 , A61P19/02 , A61P29/00 , A61P3/10 , A61P35/00 , A61P37/00 , A61P43/00 , C07D205/12 , C07D213/00 , C07D217/00 , C07D221/00 , C07D235/02 , C07D239/70 , C07D257/04 , C07D263/52 , C07D277/00 , C07D295/00 , C07D307/77
CPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04 , C07D491/048
摘要： The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
摘要翻译： 本发明涉及具有作为S1P受体调节剂的活性的通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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