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公开(公告)号:US07271165B2
公开(公告)日:2007-09-18
申请号:US11020870
申请日:2004-12-22
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
IPC分类号: C07D498/18 , A61K31/535 , A61K31/54
CPC分类号: C07D498/18 , C07D513/18 , C07D519/00
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其他形式中,苯并恶嗪利霉素,苯并噻嗪可的霉素和苯并二氮霉素霉素类似物在苯环的各个位置衍生化,包括3'-羟基类似物,4'-和/或6'卤素和/或烷氧基类似物,以及各种5'取代基 加入环胺部分。
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公开(公告)号:US20100273765A1
公开(公告)日:2010-10-28
申请号:US11821368
申请日:2007-06-21
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
IPC分类号: A61K31/397 , C07D413/14 , A61K31/496 , A61K31/542 , A61K31/5383 , A61K31/4985 , A61K31/551 , A61P29/00 , A61P31/04 , A61P7/02 , A61P3/06 , A61P9/10 , A61P31/10 , A61P31/12 , A61P31/00
CPC分类号: C07D498/18 , C07D513/18 , C07D519/00
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其他形式中,苯并恶嗪利霉素,苯并噻嗪可的霉素和苯并二氮霉素霉素类似物在苯环的各个位置衍生化,包括3'-羟基类似物,4'-和/或6'卤素和/或烷氧基类似物,以及各种5'取代基 加入环胺部分。
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公开(公告)号:US07547692B2
公开(公告)日:2009-06-16
申请号:US11638756
申请日:2006-12-14
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Joseph Raker , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
IPC分类号: C07D498/18 , A61K31/535 , A61P31/04
CPC分类号: C07D498/18 , C07D519/00
摘要: The present invention features rifamycin analogs and methods of using these compounds to treat a variety of microbial infections.
摘要翻译: 本发明特征为利福霉素类似物和使用这些化合物治疗各种微生物感染的方法。
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公开(公告)号:US07220738B2
公开(公告)日:2007-05-22
申请号:US11008597
申请日:2004-12-09
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
IPC分类号: C07D498/14 , C07D491/14 , A61K31/542 , A61K31/498 , A61P31/04
CPC分类号: C07D498/16 , C07D498/22 , C07D513/22
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4′,5′ or 5′,6′ positions.
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公开(公告)号:US07494991B2
公开(公告)日:2009-02-24
申请号:US11804141
申请日:2007-05-17
申请人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
发明人: John H. van Duzer , Arthur F. Michaelis , William B. Geiss , Douglas G. Stafford , Xiang Y. Yu , James M. Siedlecki , Yingfei Yang
IPC分类号: C07D498/14 , C07D491/14 , A61K31/542 , A61K31/498 , A61P31/04
CPC分类号: C07D498/16 , C07D498/22 , C07D513/22
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4′,5′ or 5′,6′ positions.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其它形式中,苯并恶嗪利霉素,苯并噻嗪可霉素和苯并二氮霉素类似物在苯环的不同位置衍生化,包括3'-羟基类似物和/或各种稠合环体系,其中苯环为4',5'或5' ,6'位。
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公开(公告)号:US07488726B2
公开(公告)日:2009-02-10
申请号:US11591971
申请日:2006-11-02
IPC分类号: C07D498/14 , C07D491/14 , A61K31/542 , A61K31/5383 , A61P31/04 , A61P31/10
CPC分类号: C07D498/18
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 5′-halo and/or alkoxy analogs, and various 4′- and/or 6′-substituents that incorporate a cyclic amine moiety.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其他形式中,苯并恶嗪利霉素,苯并噻嗪可的霉素和苯并二氮霉素类似物在苯环的不同位置衍生化,包括3'-羟基类似物,5'-卤素和/或烷氧基类似物,以及各种4'-和/或6'- 引入环胺部分的取代基。
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公开(公告)号:US20120225851A1
公开(公告)日:2012-09-06
申请号:US13335287
申请日:2011-12-22
IPC分类号: A61K31/502 , C07D403/10 , A61P35/02 , A61K31/196 , A61K31/573 , A61P35/00 , C07C229/64
CPC分类号: A61K31/498 , A61K31/454 , A61K31/573 , A61K31/69 , A61K45/06 , C07C217/92 , C07C229/18 , C07C229/34 , C07C229/36 , C07C229/48 , C07C229/58 , C07C229/60 , C07C229/64 , C07C311/21 , C07C317/36 , C07C317/44 , C07C2101/08 , C07C2101/14 , C07C2601/08 , C07C2601/14 , C07D209/08 , C07D209/34 , C07D211/46 , C07D211/60 , C07D213/79 , C07D215/48 , C07D231/14 , C07D231/38 , C07D235/26 , C07D239/28 , C07D239/42 , C07D241/46 , C07D261/18 , C07D263/34 , C07D263/48 , C07D309/14
摘要: The present invention relates to a chemotherapeutic cancer treatment in which compounds of Formula Ia′, Ib′, Ic′, or II′ (referred to as a group as BH3Is) are administered to a mammal for the treatment of B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. In another aspect, the invention provides a method for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds selected from the group consisting of compounds or Formula Ia, Ib, Ic, or II in combination with other therapies, for example, a class of therapeutics known as 26S proteosome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with pharmaceutical compositions comprising one or more compounds of Formula Ia′, Ib′, Ic′, or II′. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.
摘要翻译: 本发明涉及化学治疗性癌症治疗,其中将式Ia',Ib',Ic'或II'的化合物(称为BH3Is的基团)施用于哺乳动物用于治疗B细胞淋巴瘤或其它 造血癌,包括与MCL-1有关的疾病。 另一方面,本发明提供了使用一种或多种选自化合物或式Ia,Ib,Ic或II的化合物的组合来治疗特定类型的造血细胞癌例如B细胞淋巴瘤的方法, 与其他疗法组合,例如一类称为26S蛋白酶抑制剂的治疗剂,例如硼替佐米。 另一方面,本发明涉及用包含一种或多种式Ia',Ib',Ic'或II'化合物的药物组合物进行自身免疫治疗。 在另一方面,本发明涉及用于鉴定化合物的方法,例如BH3类似物的化合物,其具有独特的体外性质,其预测体内对B细胞淋巴瘤肿瘤和其他癌症以及自身免疫疾病的功效。
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公开(公告)号:US20120129828A1
公开(公告)日:2012-05-24
申请号:US12995387
申请日:2009-06-18
申请人: Victor J. Cee , Jian Lin , Xiang Y. Yu , Zhaoda Zhang
发明人: Victor J. Cee , Jian Lin , Xiang Y. Yu , Zhaoda Zhang
IPC分类号: A61K31/397 , C07D409/14 , C07D409/10 , C07D405/14 , A61K31/4025 , A61K31/4525 , A61K31/4535 , A61K31/55 , A61K31/343 , A61K31/4178 , A61P25/00 , A61P19/02 , A61P1/00 , A61P11/06 , A61P3/10 , A61P11/00 , A61P31/00 , A61P35/04 , A61P35/00 , A61P35/02 , A61P21/04 , C07D405/10
CPC分类号: C07D513/04 , A61K9/2018 , A61K9/2059 , A61K9/48
摘要: The present invention relates to compounds of Formula (I) that are have activity as S1P1 receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.
摘要翻译: 本发明涉及具有作为S1P1受体调节剂的活性的式(I)化合物,更具体地涉及具体为S1P1受体激动剂的化合物。 本发明还涉及使用这些化合物来治疗与不适当的S1P1受体活性相关的疾病,例如自身免疫性疾病。
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公开(公告)号:US07968538B2
公开(公告)日:2011-06-28
申请号:US11340079
申请日:2006-01-25
申请人: Oren Becker , Rosa Melendez , Yael Marantz , Anurag Sharadendu , Merav Fichman , Mercedes Lobera , Hanoch Senderowitz , Srinivasa Rao Cheruku , Silvia Noiman , Xiang Y. Yu , Sharon Shacham , Laurence Wu , Ashis Saha , Pini Orbach , Dale S. Dhanoa
发明人: Oren Becker , Rosa Melendez , Yael Marantz , Anurag Sharadendu , Merav Fichman , Mercedes Lobera , Hanoch Senderowitz , Srinivasa Rao Cheruku , Silvia Noiman , Xiang Y. Yu , Sharon Shacham , Laurence Wu , Ashis Saha , Pini Orbach , Dale S. Dhanoa
IPC分类号: C07D295/135 , A61K31/451
CPC分类号: C07D295/135 , C07D207/14 , C07D211/58 , C07D243/08 , C07D311/68 , C07D317/62 , C07D319/18 , C07D333/66 , C07D405/12
摘要: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.
摘要翻译: 本发明涉及5-HT 6受体拮抗剂。 新型芳基胺化合物和这些化合物及其药物组合物的用途,例如用于治疗,调节和/或预防与5-羟色胺作用相关的生理条件,例如治疗肥胖症和肥胖相关疾病,例如心血管疾病,消化系统 疾病,呼吸系统疾病,癌症和II型糖尿病; 和精神分裂症等心理障碍。
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公开(公告)号:US09657012B2
公开(公告)日:2017-05-23
申请号:US13996807
申请日:2011-12-22
申请人: Colleen Hudson , Timothy C. Barden , James Jia , Ara Mermerian , Bo Peng , Jane Yang , Xiang Y. Yu , Kevin Sprott , Angelika Fretzen
发明人: Colleen Hudson , Timothy C. Barden , James Jia , Ara Mermerian , Bo Peng , Jane Yang , Xiang Y. Yu , Kevin Sprott , Angelika Fretzen
IPC分类号: C07D401/14 , A61K31/444 , A61K31/4439 , C07D471/04 , C07D401/12 , C07D403/12 , C07D403/14 , A61K31/4045 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D209/14
CPC分类号: C07D471/04 , A61K31/4045 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D209/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
摘要: The present disclosure relates to compounds useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders. Compounds of the invention are described in Table 1.
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