公开(公告)号：US07776896B2

公开(公告)日：2010-08-17

申请号：US12079602

申请日：2008-03-27

申请人： William Guilford ,  Werner Skuballa ,  Daryl H. Faulds ,  Monica Kochanny ,  Wheeseong Lee ,  Bernd Radüchel

发明人： William Guilford ,  Werner Skuballa ,  Daryl H. Faulds ,  Monica Kochanny ,  Wheeseong Lee ,  Bernd Radüchel

IPC分类号： A61K31/41

CPC分类号： C07D307/937 ,  C07D405/06

摘要： This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating respiratory diseases associated with influenza A viruses, such as for example H5N1 and its mutations. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

摘要翻译： 本发明涉及式（I）化合物：其中A，B，D，E，m和R 1 -R 5如本文所述，作为单一立体异构体或作为立体异构体或其药学上可接受的盐，包合物或前药的混合物 其可用于治疗与甲型流感病毒相关的呼吸道疾病，例如H5N1及其突变。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。

公开(公告)号：US20080242714A1

公开(公告)日：2008-10-02

申请号：US12079602

申请日：2008-03-27

申请人： William Guilford ,  Werner Skuballa ,  Daryl H. Faulds ,  Monica Kochanny ,  Wheeseong Lee ,  Bernd Raduchel

发明人： William Guilford ,  Werner Skuballa ,  Daryl H. Faulds ,  Monica Kochanny ,  Wheeseong Lee ,  Bernd Raduchel

IPC分类号： A61K31/41 ,  C07D307/77 ,  A61K31/365 ,  A61P31/16 ,  C07D405/02

CPC分类号： C07D307/937 ,  C07D405/06

摘要： This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating respiratory diseases associated with influenza A viruses, such as for example H5N1 and its mutations. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

摘要翻译： 本发明涉及式（I）化合物：其中A，B，D，E，m和R 1 -R 5如本文所述，作为单 立体异构体或其立体异构体或其药学上可接受的盐，包合物或前药的混合物，其可用于治疗与甲型流感病毒相关的呼吸系统疾病，例如H5N1及其突变。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。

公开(公告)号：US20080242713A1

公开(公告)日：2008-10-02

申请号：US12079598

申请日：2008-03-27

申请人： William Guilford ,  Werner Skuballa ,  Daryl H. Faulds ,  Monica Kochanny ,  Wheeseong Lee ,  Bernd Raduchel

发明人： William Guilford ,  Werner Skuballa ,  Daryl H. Faulds ,  Monica Kochanny ,  Wheeseong Lee ,  Bernd Raduchel

IPC分类号： A61K31/41 ,  A61K31/343 ,  C07D307/77 ,  A61P37/00 ,  C07D405/02

CPC分类号： C07D307/937 ,  C07D405/06

摘要： This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating autoimmune diseases. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

摘要翻译： 本发明涉及式（I）化合物：其中A，B，D，E，m和R 1 -R 5如本文所述，作为单 立体异构体或其立体异构体或其药学上可接受的盐，包合物或前药的混合物，其可用于治疗自身免疫性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。

公开(公告)号：US20070129359A1

公开(公告)日：2007-06-07

申请号：US11414556

申请日：2006-05-01

申请人： Christoph Huwe ,  Werner Skuballa ,  Duy Nguyen ,  Heike Schaecke ,  Wheeseong Lee

发明人： Christoph Huwe ,  Werner Skuballa ,  Duy Nguyen ,  Heike Schaecke ,  Wheeseong Lee

IPC分类号： A61K31/538 ,  A61K31/498 ,  A61K31/4745 ,  A61K31/4704 ,  A61K31/404 ,  A61K31/4035

CPC分类号： C07C233/74 ,  C07C217/74 ,  C07C275/28 ,  C07C311/20 ,  C07C2602/10

摘要： The invention relates to multiply substituted tetrahydronaphthalene derivatives of the formula (I) processes for their preparation and their use as anti-inflammatory agents.

摘要翻译： 本发明涉及式（I）的多取代四氢萘衍生物，其制备方法及其作为抗炎剂的用途。

公开(公告)号：US07563924B2

公开(公告)日：2009-07-21

申请号：US11602690

申请日：2006-11-20

申请人： Bernd Buchmann ,  Daryl Faulds ,  William Guilford ,  Gernot Langer ,  Judy Li ,  Bernhard Lindenthal ,  Werner Skuballa ,  Luisella Toschi

发明人： Bernd Buchmann ,  Daryl Faulds ,  William Guilford ,  Gernot Langer ,  Judy Li ,  Bernhard Lindenthal ,  Werner Skuballa ,  Luisella Toschi

IPC分类号： C07C69/74 ,  A61K31/557

CPC分类号： C07C405/00 ,  C07C2601/04 ,  C07D309/12

摘要： The present invention relates to 9-chloroprostaglandin derivatives of the general formula I which may be advantageous for the treatment of fertility problems.

摘要翻译： 本发明涉及通式Ⅰ的9-氯前列腺素衍生物，其可有利于治疗生殖问题。

公开(公告)号：US20070203096A1

公开(公告)日：2007-08-30

申请号：US11602690

申请日：2006-11-20

申请人： Bernd Buchmann ,  Daryl Faulds ,  William Guilford ,  Gernot Langer ,  Judy Li ,  Bernhard Lindenthal ,  Werner Skuballa ,  Luisella Toschi

发明人： Bernd Buchmann ,  Daryl Faulds ,  William Guilford ,  Gernot Langer ,  Judy Li ,  Bernhard Lindenthal ,  Werner Skuballa ,  Luisella Toschi

IPC分类号： A61K31/724 ,  A61K31/695 ,  A61K31/557

CPC分类号： C07C405/00 ,  C07C2601/04 ,  C07D309/12

摘要： The present invention relates to 9-chloroprostaglandin derivatives of the general formula I which may be advantageous for the treatment of fertility problems.

摘要翻译： 本发明涉及通式Ⅰ的9-氯前列腺素衍生物，其可有利于治疗生殖问题。

公开(公告)号：US07928255B2

公开(公告)日：2011-04-19

申请号：US11585501

申请日：2006-10-23

申请人： John G. Bauman ,  William Guilford ,  John Parkinson ,  Werner Skuballa ,  Babu Subramanyam

发明人： John G. Bauman ,  William Guilford ,  John Parkinson ,  Werner Skuballa ,  Babu Subramanyam

IPC分类号： C07C57/00

CPC分类号： C07D317/72 ,  A61K31/202 ,  A61K31/216 ,  C07C59/68 ,  C07C59/70 ,  C07C69/708 ,  C07C69/736 ,  C07C209/68 ,  C07C217/46 ,  C07C229/12 ,  C07C235/06 ,  C07C323/52 ,  C07D317/22

摘要： This invention is directed to lipoxin A4 analogs of the following formula (I) and (II): wherein R1, R2, R3, R4 and R5 are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.

摘要翻译： 本发明涉及下述式（I）和（II）的脂氧素A4类似物：其中R1，R2，R3，R4和R5如本文所述。 这些类似物可用于治疗人类的炎性和自身免疫性疾病。 这些类似物也可用于治疗人类的肺或呼吸道炎症。

公开(公告)号：US20070037864A1

公开(公告)日：2007-02-15

申请号：US11585501

申请日：2006-10-23

申请人： John Bauman ,  William Guilford ,  John Parkinson ,  Werner Skuballa ,  Babu Subramanyam

发明人： John Bauman ,  William Guilford ,  John Parkinson ,  Werner Skuballa ,  Babu Subramanyam

IPC分类号： A61K31/426 ,  A61K31/421 ,  A61K31/4166 ,  A61K31/365 ,  A61K31/135

CPC分类号： C07D317/72 ,  A61K31/202 ,  A61K31/216 ,  C07C59/68 ,  C07C59/70 ,  C07C69/708 ,  C07C69/736 ,  C07C209/68 ,  C07C217/46 ,  C07C229/12 ,  C07C235/06 ,  C07C323/52 ,  C07D317/22

摘要： This invention is directed to lipoxin A4 analogs of the following formula (I) and (II): wherein R1, R2, R3, R4 and R5 are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.

摘要翻译： 本发明涉及下式（I）和（II）的脂氧素A 4 H 4类似物：其中R 1，R 2，R 2， 本文描述了第3和第4和第4和第5和第5。 这些类似物可用于治疗人类的炎性和自身免疫性疾病。 这些类似物也可用于治疗人类的肺或呼吸道炎症。

公开(公告)号：US07700621B2

公开(公告)日：2010-04-20

申请号：US11214988

申请日：2005-08-31

申请人： Ulrich Klar ,  Wolfgang Schwede ,  Werner Skuballa ,  Bernd Buchmann ,  Jens Hoffmann ,  Rosemarie Lichtner

发明人： Ulrich Klar ,  Wolfgang Schwede ,  Werner Skuballa ,  Bernd Buchmann ,  Jens Hoffmann ,  Rosemarie Lichtner

IPC分类号： A01N43/42 ,  A01N43/78 ,  C07D417/00

CPC分类号： C07D493/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

摘要： This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.

公开(公告)号：US07645891B2

公开(公告)日：2010-01-12

申请号：US10965802

申请日：2004-10-18

申请人： Ulrich Klar ,  Wolfgang Schwede ,  Werner Skuballa ,  Bernd Buchmann ,  Jens Hoffmann ,  Rosemarie Lichtner

发明人： Ulrich Klar ,  Wolfgang Schwede ,  Werner Skuballa ,  Bernd Buchmann ,  Jens Hoffmann ,  Rosemarie Lichtner

IPC分类号： C07D319/06 ,  C07C49/20

CPC分类号： C07D493/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

摘要： This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2b, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.

摘要翻译： 本发明描述了通式（I）的新的6-烯基 - 和6-炔基 - 埃坡霉素衍生物，其中R1a，R1b，R2a，R3a，R3b，R4，R5，R6，R7，A，Y，D，E， G，Y和Z具有在说明书中指示的含义。 新化合物通过稳定形成的微管与微管蛋白相互作用。 它们能够以相位特异性方式影响细胞分裂，因此可用于治疗与细胞生长，分裂和/或增殖的需要相关的疾病或病症。 因此，该化合物适用于治疗恶性肿瘤，例如卵巢癌，胃癌，结肠癌，腺癌，乳腺癌，肺癌，头颈癌，恶性黑素瘤，急性淋巴细胞性白血病和骨髓性白血病。 此外，它们适用于抗血管生成治疗以及治疗慢性炎性疾病（如银屑病，关节炎）。 还描述了化合物的使用和制备方法。