公开(公告)号：US20080241959A1

公开(公告)日：2008-10-02

申请号：US11813871

申请日：2006-01-13

申请人： Ognjen Culic ,  Martina Bosnar ,  Nikola Marianovic ,  Boris Mildner ,  Linda Tomaskovic ,  Sulejman Alihodzic

发明人： Ognjen Culic ,  Martina Bosnar ,  Nikola Marianovic ,  Boris Mildner ,  Linda Tomaskovic ,  Sulejman Alihodzic

IPC分类号： G01N33/68 ,  C07D495/04

CPC分类号： C07H17/08

摘要： The present invention relates to new macrolide compounds represented by the general structure I, wherein M is a macrolide, P is a photo-affinity group bearing subunit containing biotin, and L is a linking molecule, and to their pharmaceutically acceptable salts and solvates, to processes and intermediates for their preparation and to the use of these compounds for the macrolide target identification.

摘要翻译： 本发明涉及由通式结构I表示的新型大环内酯类化合物，其中M为大环内酯，P为含有亲电子基团的含有生物素的亚单位，L为连接分子，以及其药学上可接受的盐和溶剂合物， 其制备方法和中间体以及这些化合物用于大环内酯靶标鉴定的用途。

公开(公告)号：US07989600B2

公开(公告)日：2011-08-02

申请号：US11813871

申请日：2006-01-13

申请人： Ognjen Culic ,  Martina Bosnar ,  Nikola Marjanovic ,  Boris Mildner ,  Linda Tomaskovic ,  Sulejman Alihodzic

发明人： Ognjen Culic ,  Martina Bosnar ,  Nikola Marjanovic ,  Boris Mildner ,  Linda Tomaskovic ,  Sulejman Alihodzic

IPC分类号： C07H17/08

CPC分类号： C07H17/08

摘要： The present invention relates to new macrolide compounds represented by the general structure I, wherein M is a macrolide, P is a photo-affinity group bearing subunit containing biotin, and L is a linking molecule, and to their pharmaceutically acceptable salts and solvates, to processes and intermediates for their preparation and to the use of these compounds for the macrolide target identification.

摘要翻译： 本发明涉及由通式结构I表示的新型大环内酯类化合物，其中M为大环内酯，P为含有亲电子基团的含有生物素的亚单位，L为连接分子，以及其药学上可接受的盐和溶剂合物， 其制备方法和中间体以及这些化合物用于大环内酯靶标鉴定的用途。

公开(公告)号：US07910559B2

公开(公告)日：2011-03-22

申请号：US11813876

申请日：2006-01-13

申请人： Ognjen Culic ,  Martina Bosnar ,  Sulejman Alihodzic ,  Gorjana Lazarevski ,  Zorica Marusic Istuk ,  Antun Hutinec ,  Vanja Vela ,  Goran Kragol

发明人： Ognjen Culic ,  Martina Bosnar ,  Sulejman Alihodzic ,  Gorjana Lazarevski ,  Zorica Marusic Istuk ,  Antun Hutinec ,  Vanja Vela ,  Goran Kragol

IPC分类号： A61K31/70 ,  C07H17/08

CPC分类号： C07H17/08

摘要： The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides lacking cladinose sugar substituted at the C-3 position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

摘要翻译： 本发明涉及具有抗炎活性的新型半合成大环内酯类。 更具体地说，本发明涉及在C-3位上缺少被克拉替糖糖化的14-和15-元大环内酯，其药学上可接受的衍生物，其制备方法和中间体，含有它们的药物组合物及其活性和用途 特别是与过量分泌TNF-α，IL-1，IL-6，IL-8，IL-2或IL-5相关的那些疾病的治疗中， 和/或过度淋巴细胞增殖的抑制剂; 和/或过量粒细胞脱粒。

公开(公告)号：US08080529B2

公开(公告)日：2011-12-20

申请号：US11813873

申请日：2006-01-13

申请人： Sulejman Alihodzic ,  Martina Bosnar ,  Ognjen Culic ,  Vesna Erakovic Haber ,  Antun Hutinec ,  Dubravko Jelic ,  Goran Kragol ,  Nikola Marjanovic ,  Zorica Marusic-Istuk ,  Marija Ribic ,  Vanja Vela

发明人： Sulejman Alihodzic ,  Martina Bosnar ,  Ognjen Culic ,  Vesna Erakovic Haber ,  Antun Hutinec ,  Dubravko Jelic ,  Goran Kragol ,  Nikola Marjanovic ,  Zorica Marusic-Istuk ,  Marija Ribic ,  Vanja Vela

IPC分类号： A61K31/70 ,  C07H17/08

CPC分类号： C07H17/00 ,  C07H17/08

摘要： The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4″ position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

摘要翻译： 本发明涉及具有抗炎活性的新型半合成大环内酯类。 更具体地，本发明涉及在4“位取代的14-和15-元大环内酯，其药学上可接受的衍生物，其制备方法和中间体，含有它们的药物组合物及其活性和用于治疗 特别是那些与过量分泌TNF-α，IL-1，IL-8，IL-2或IL-5相关的疾病; 和/或过度淋巴细胞增殖的抑制剂; 和/或过量粒细胞脱粒。

公开(公告)号：US20080234211A1

公开(公告)日：2008-09-25

申请号：US11813876

申请日：2006-01-13

申请人： Ognjen Culic ,  Martina Bosnar ,  Sulejman Alihodzic ,  Gorjana Lazarevski ,  Zorica Marusic Istuk ,  Antun Hutinec ,  Vanja Vela ,  Goran Kragol

发明人： Ognjen Culic ,  Martina Bosnar ,  Sulejman Alihodzic ,  Gorjana Lazarevski ,  Zorica Marusic Istuk ,  Antun Hutinec ,  Vanja Vela ,  Goran Kragol

IPC分类号： A61K31/7052 ,  C07H17/00 ,  C12N5/06 ,  A61P29/00

CPC分类号： C07H17/08

摘要： The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides lacking cladinose sugar substituted at the C-3 position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

摘要翻译： 本发明涉及具有抗炎活性的新型半合成大环内酯类。 更具体地说，本发明涉及在C-3位上缺少被克拉替糖糖化的14-和15-元大环内酯，其药学上可接受的衍生物，其制备方法和中间体，含有它们的药物组合物及其活性和用途 特别是与过量分泌TNF-α，IL-1，IL-6，IL-8，IL-2或IL-5相关的那些疾病; 和/或过度淋巴细胞增殖的抑制剂; 和/或过量粒细胞脱粒。

公开(公告)号：US20080221046A1

公开(公告)日：2008-09-11

申请号：US11813873

申请日：2006-01-13

申请人： Ognjen Culic ,  Martina Bosnar ,  Nikola Marjanovic ,  Dubravko Jelic ,  Sulejman Alihodzic ,  Vanja Vela ,  Zorica Marusic-Istuk ,  Vesna Erakovic ,  Berislav Bosnjak ,  Boska Hrvacic ,  Marija Tomaskovic ,  Vanesa Munic ,  Vanesa Ivetic ,  Antun Hutinec ,  Goran Kragol ,  Marija Leljak

发明人： Ognjen Culic ,  Martina Bosnar ,  Nikola Marjanovic ,  Dubravko Jelic ,  Sulejman Alihodzic ,  Vanja Vela ,  Zorica Marusic-Istuk ,  Vesna Erakovic ,  Berislav Bosnjak ,  Boska Hrvacic ,  Marija Tomaskovic ,  Vanesa Munic ,  Vanesa Ivetic ,  Antun Hutinec ,  Goran Kragol ,  Marija Leljak

IPC分类号： A61K31/7048 ,  C07H17/00 ,  C12N5/06 ,  A61P29/00 ,  A61P11/06

CPC分类号： C07H17/00 ,  C07H17/08

摘要： The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4″ position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

摘要翻译： 本发明涉及具有抗炎活性的新型半合成大环内酯类。 更具体地，本发明涉及在4“取代的14-和15-元大环内酯，其药学上可接受的衍生物，其制备方法和中间体，含有它们的药物组合物及其在治疗中的活性和用途 特别是与过量分泌TNF-α，IL-1，IL-8，IL-2或IL-5相关的那些疾病; 和/或过度淋巴细胞增殖的抑制剂; 和/或过量粒细胞脱粒。

公开(公告)号：US20120058963A1

公开(公告)日：2012-03-08

申请号：US13296352

申请日：2011-11-15

申请人： Sulejman Alihodzic ,  Martina Bosnar ,  Ognjen Culic ,  Vesna Erakovic Haber ,  Antun Hutinec ,  Dubravko Jelic ,  Goran Kragol ,  Nikola Marjanovic ,  Zorica Marusic-Istuk ,  Marija Ribic ,  Vanja Vela

发明人： Sulejman Alihodzic ,  Martina Bosnar ,  Ognjen Culic ,  Vesna Erakovic Haber ,  Antun Hutinec ,  Dubravko Jelic ,  Goran Kragol ,  Nikola Marjanovic ,  Zorica Marusic-Istuk ,  Marija Ribic ,  Vanja Vela

IPC分类号： A61K31/7048 ,  C07H17/08 ,  A61K31/7052 ,  A61K31/706 ,  A61P37/02 ,  A61P11/06 ,  A61P11/00 ,  A61P1/00 ,  C07H17/00 ,  A61P29/00

CPC分类号： C07H17/00 ,  C07H17/08

摘要： The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4″ position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

摘要翻译： 本发明涉及具有抗炎活性的新型半合成大环内酯类。 更具体地，本发明涉及在4“位取代的14-和15-元大环内酯，其药学上可接受的衍生物，其制备方法和中间体，含有它们的药物组合物及其活性和用于治疗 特别是那些与过量分泌TNF-α，IL-1，IL-8，IL-2或IL-5相关的疾病; 和/或过度淋巴细胞增殖的抑制剂; 和/或过量粒细胞脱粒。

公开(公告)号：US20080200403A1

公开(公告)日：2008-08-21

申请号：US11813870

申请日：2006-01-13

申请人： Ognjen Culic ,  Martina Bosnar ,  Nikola Marjanovic ,  Vesna Erakovic ,  Dubravko Jelic ,  Donatella Verbanac

发明人： Ognjen Culic ,  Martina Bosnar ,  Nikola Marjanovic ,  Vesna Erakovic ,  Dubravko Jelic ,  Donatella Verbanac

IPC分类号： A61K31/7052 ,  C12N5/06 ,  A61P29/00

CPC分类号： A61K31/7052

摘要： The use of semi-synthetic 9a-carbamoyl or thiocarbamoyl azalides for the treatment and prevention of inflammatory diseases and conditions in humans and animals. More particularly, the invention relates to the use of 15-membered azalides having at the 9a-position carbamoyl or thiocarbamoyl group, and their pharmaceutically acceptable derivatives for the treatment and prevention of inflammatory diseases and conditions in humans and animals.

摘要翻译： 使用半合成的9a-氨基甲酰基或硫代氨基甲酰基吖啶化合物来治疗和预防人和动物的炎性疾病和病症。 更具体地说，本发明涉及在9a位具有氨基甲酰基或硫代氨基甲酰基的15-元氮杂及其药学上可接受的衍生物用于治疗和预防人和动物中炎性疾病和病症的用途。