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1. 发明申请

US20100190710A1 IL-23 RECEPTOR ANTAGONISTS AND USES THEREOF 审中-公开
标题翻译： IL-23受体拮抗剂及其用途
公开(公告)号：US20100190710A1
公开(公告)日：2010-07-29
申请号：US12666028
申请日：2008-07-07
申请人： Sylvain Chemtob , Christiane Quiniou , William D. Lubell
发明人： Sylvain Chemtob , Christiane Quiniou , William D. Lubell
IPC分类号： A61K38/16 , C07K14/00 , C07K7/08 , C07K7/06 , C07K5/10 , C07K5/08 , C12N15/63 , C12N5/10 , A61K38/10 , A61K38/08 , A61K38/05 , A61K38/06 , A61K38/07 , A61P29/00 , A61P37/00 , G01N33/53
CPC分类号： C07K14/4703 , C07K14/4705 , C07K14/5434 , C07K14/7155 , G01N33/6869
摘要： The present invention relates to IL-23 receptor antagonists and agonists. The use of IL-23 receptor antagonists in treating autoimmune and inflammatory disorders, as well as methods of identifying IL-23 receptor antagonists and agonists.
摘要翻译：本发明涉及IL-23受体拮抗剂和激动剂。 IL-23受体拮抗剂在治疗自身免疫性和炎症性疾病中的应用，以及鉴定IL-23受体拮抗剂和激动剂的方法。

2. 发明授权

US08618054B2 Interleukin-1 receptor antagonists, compositions, and methods of treatment 有权
标题翻译：白细胞介素-1受体拮抗剂，组合物和治疗方法
公开(公告)号：US08618054B2
公开(公告)日：2013-12-31
申请号：US11122989
申请日：2005-05-05
申请人： Sylvain Chemtob , Christiane Quiniou , William D. Lubell , Martin Beauchamp , Karl A. Hansford
发明人： Sylvain Chemtob , Christiane Quiniou , William D. Lubell , Martin Beauchamp , Karl A. Hansford
IPC分类号： A61K38/00 , A61P29/00
CPC分类号： C07K7/06 , A61K38/00
摘要： Peptides that are designed to inhibit the biological activity of the IL-1R type 1 receptor and inhibit IL-1R/IL-1RacP related cell signaling and biological activity are disclosed. Compositions comprising IL-1R antagonists of the present invention are useful in the treatment of IL-1 related diseases or conditions such as arthritis, rheumatoid arthritis, osteoarthritis, and inflammatory bowel disease as well as other chronic or acute inflammatory diseases. This invention also discloses an isolated compound having an IL-1R antagonist activity, said compound being selected from the group consisting of: a peptide comprising the amino acid sequence RYTPELX, wherein R, Y, T, P, E, L, refer to their corresponding amino acids, and X is selected from no amino acid and alanine (A); and a derivative of (a) wherein the derivative incorporates one, two or three amino acid modification selected from an amino acid addition, deletion or substitution in the RYTPEL portion of the peptide, and wherein said derivative maintains its antagonist IL-1R activity.
摘要翻译：公开了旨在抑制IL-1R 1型受体的生物活性并抑制IL-1R / IL-1RacP相关细胞信号传导和生物学活性的肽。包含本发明的IL-1R拮抗剂的组合物可用于治疗IL-1相关疾病或病症如关节炎，类风湿性关节炎，骨关节炎和炎性肠病以及其它慢性或急性炎性疾病。本发明还公开了具有IL-1R拮抗剂活性的分离化合物，所述化合物选自：包含氨基酸序列RYTPELX的肽，其中R，Y，T，P，E，L是指它们相应的氨基酸，X选自无氨基酸和丙氨酸（A）; 和（a）的衍生物，其中所述衍生物包含选自肽的RYTPEL部分中的氨基酸添加，缺失或取代的一个，两个或三个氨基酸修饰，并且其中所述衍生物维持其拮抗剂IL-1R活性。

3. 发明申请

US20120309690A1 PROSTAGLANDIN-F2 ALPHA RECEPTOR MODULATORS AND USES THEREOF 有权
标题翻译： PROSTAGLANDIN-F2 ALPHA受体调节剂及其用途
公开(公告)号：US20120309690A1
公开(公告)日：2012-12-06
申请号：US13486502
申请日：2012-06-01
申请人： William D. LUBELL , Sylvain CHEMTOB , Terence E. HÉBERT , Audrey CLAING , Stephane LAPORTE , Carine B. BOURGUET , Eugenie GOUPIL , Xin HOU , Danae TASSY
发明人： William D. LUBELL , Sylvain CHEMTOB , Terence E. HÉBERT , Audrey CLAING , Stephane LAPORTE , Carine B. BOURGUET , Eugenie GOUPIL , Xin HOU , Danae TASSY
IPC分类号： A61K38/07 , A61P35/00 , C12Q1/48 , C07K5/117
CPC分类号： C07K5/1024 , A61K38/00 , C07K5/0812 , C12Q1/485
摘要： Prostaglandin-F2 alpha (PGF2α) receptor (FP) modulators of formula I, as well as the use of PGF2α receptor modulators for the treatment of conditions associated with FP activity such as preterm labor and colorectal cancer, are disclosed.
摘要翻译：公开了式I的前列腺素F2α（PGF2α）受体（FP）调节剂，以及PGF2α受体调节剂用于治疗与FP活性相关的病症如早产和结肠直肠癌的用途。

4. 发明申请

US20100204280A1 CINNAMOYL INHIBITORS OF TRANSGLUTAMINASE 有权
标题翻译：转氨酶的CINNAMOYL抑制剂
公开(公告)号：US20100204280A1
公开(公告)日：2010-08-12
申请号：US12602425
申请日：2008-05-29
申请人： Christophe Pardin , Jeffrey W. Keillor , William D. Lubell
发明人： Christophe Pardin , Jeffrey W. Keillor , William D. Lubell
IPC分类号： A61K31/4439 , G01N33/573 , C12N5/02 , A61K31/44 , A61K31/4192 , C07D401/06 , C07D211/82 , C07D249/04 , C07D249/16
CPC分类号： C07D249/04 , C07C205/43 , C07C205/56 , C07D209/08 , C07D211/22 , C07D213/50 , C07D213/53 , C07D221/04 , C07D233/54 , C07D233/60 , C07D249/18 , C07D265/06 , C07D295/185 , C07D311/12 , C07D401/06 , C07D471/04 , C12Q1/48 , G01N2333/91085 , G01N2500/02
摘要： A compound of Formula, (I) or Formula: (II)
摘要翻译：式（I）或式（II）的化合物：

5. 发明申请

US20100041609A1 INTERLEUKIN-1 RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS OF TREATMENT 审中-公开
标题翻译：白细胞介素-1受体拮抗剂，组合物和治疗方法
公开(公告)号：US20100041609A1
公开(公告)日：2010-02-18
申请号：US12579691
申请日：2009-10-15
申请人： Sylvain Chemtob , Christiane Quiniou , William D. Lubell , Martin Beauchamp , Karl A. Hansford
发明人： Sylvain Chemtob , Christiane Quiniou , William D. Lubell , Martin Beauchamp , Karl A. Hansford
IPC分类号： A61K38/16 , C12N5/071 , A61K38/10 , A61K38/08 , C07K14/00 , C07K7/08 , C07K7/06
CPC分类号： C07K7/06 , A61K38/00
摘要： Peptides that are designed to inhibit the biological activity of the IL-1R type 1 receptor and inhibit IL-1R/IL-1RacP related cell signaling and biological activity are disclosed. Compositions comprising IL-1R antagonists of the present invention are useful in the treatment of IL-1 related diseases or conditions such as arthritis, rheumatoid arthritis, osteoarthritis, and inflammatory bowel disease as well as other chronic or acute inflammatory diseases. This invention also discloses an isolated compound having an IL-1R antagonist activity, said compound being selected from the group consisting of: a peptide comprising the amino acid sequence RYTPELX, wherein R, Y, T, P, E, L, refer to their corresponding amino acids, and X is selected from no amino acid and alanine (A); and a derivative of (a) wherein the derivative incorporates one, two or three amino acid modification selected from an amino acid addition, deletion or substitution in the RYTPEL portion of the peptide, and wherein said derivative maintains its antagonist IL-1R activity.
摘要翻译：公开了旨在抑制IL-1R 1型受体的生物活性并抑制IL-1R / IL-1RacP相关细胞信号传导和生物学活性的肽。包含本发明的IL-1R拮抗剂的组合物可用于治疗IL-1相关疾病或病症如关节炎，类风湿性关节炎，骨关节炎和炎性肠病以及其它慢性或急性炎性疾病。本发明还公开了具有IL-1R拮抗剂活性的分离化合物，所述化合物选自：包含氨基酸序列RYTPELX的肽，其中R，Y，T，P，E，L是指它们相应的氨基酸，X选自无氨基酸和丙氨酸（A）; 和（a）的衍生物，其中所述衍生物包含选自肽的RYTPEL部分中的氨基酸添加，缺失或取代的一个，两个或三个氨基酸修饰，并且其中所述衍生物维持其拮抗剂IL-1R活性。

6. 发明授权

US08614233B2 Cinnamoyl inhibitors of transglutaminase 有权
标题翻译：肉桂酰抑制剂转谷氨酰胺酶
公开(公告)号：US08614233B2
公开(公告)日：2013-12-24
申请号：US12602425
申请日：2008-05-29
申请人： Christophe Pardin , Jeffrey W. Keillor , William D. Lubell
发明人： Christophe Pardin , Jeffrey W. Keillor , William D. Lubell
IPC分类号： A61K31/4402 , A61K31/4192 , C07D401/06 , C07D249/04
CPC分类号： C07D249/04 , C07C205/43 , C07C205/56 , C07D209/08 , C07D211/22 , C07D213/50 , C07D213/53 , C07D221/04 , C07D233/54 , C07D233/60 , C07D249/18 , C07D265/06 , C07D295/185 , C07D311/12 , C07D401/06 , C07D471/04 , C12Q1/48 , G01N2333/91085 , G01N2500/02
摘要： A compound of Formula, (I) or Formula: (II).
摘要翻译：式（I）或式（II）的化合物。

7. 发明授权

US08802818B2 Prostaglandin-F2 alpha receptor modulators and uses thereof 有权
标题翻译：前列腺素-2Fαα受体调节剂及其用途
公开(公告)号：US08802818B2
公开(公告)日：2014-08-12
申请号：US13486502
申请日：2012-06-01
申请人： William D. Lubell , Sylvain Chemtob , Terence E. Hebert , Audrey Claing , Stephane Laporte , Carine B. Bourguet , Eugenie Goupil , Xin Hou , Danae Tassy
发明人： William D. Lubell , Sylvain Chemtob , Terence E. Hebert , Audrey Claing , Stephane Laporte , Carine B. Bourguet , Eugenie Goupil , Xin Hou , Danae Tassy
IPC分类号： A61K38/00 , A61K38/06 , C07K2/00 , C07K4/00 , C07K5/00 , C07K7/00 , C07K14/00 , C07K16/00 , C07K17/00 , A61K51/00
CPC分类号： C07K5/1024 , A61K38/00 , C07K5/0812 , C12Q1/485
摘要： Prostaglandin-F2 alpha (PGF2α) receptor (FP) modulators of formula I, as well as the use of PGF2α receptor modulators for the treatment of conditions associated with FP activity such as preterm labor and colorectal cancer, are disclosed.
摘要翻译：公开了式I的前列腺素F2α（PGF2α）受体（FP）调节剂，以及PGF2α受体调节剂用于治疗与FP活性相关的病症如早产和结肠直肠癌的用途。

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