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1. 发明授权

US06638927B2 Guanidinobenzamides 失效
标题翻译：胍基苯甲酰胺
公开(公告)号：US06638927B2
公开(公告)日：2003-10-28
申请号：US09945384
申请日：2001-08-31
申请人： Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , Zhi-Jie Ni , David Duhl , Effie Tozzo , Kirk Johnson , David C. Myles
发明人： Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , Zhi-Jie Ni , David Duhl , Effie Tozzo , Kirk Johnson , David C. Myles
IPC分类号： C07D29520
CPC分类号： C07D233/64 , C07B2200/07 , C07B2200/09 , C07C279/18 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D209/16 , C07D215/12 , C07D241/08 , C07D241/42 , C07D295/215 , C07D307/24 , C07D309/14 , C07D333/20 , C07D487/04 , C07D487/08
摘要： Compounds of formula IA and IB are new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.
摘要翻译：式IA和IB的化合物是新的，其中变量R 1至R 10具有本文所述的值。这些化合物可用于治疗诸如肥胖症和II型糖尿病的疾病，并且可以作为药物制剂与药学上可接受的载体一起提供。

2. 发明授权

US06995269B2 Guanidinobenzamides 失效
标题翻译：胍基苯甲酰胺
公开(公告)号：US06995269B2
公开(公告)日：2006-02-07
申请号：US10379397
申请日：2003-03-04
申请人： Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , David Duhl
发明人： Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , David Duhl
IPC分类号： C07D211/72 , C07D295/20 , A61K31/44
CPC分类号： C07D233/64 , C07B2200/07 , C07B2200/09 , C07C279/18 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D209/16 , C07D215/12 , C07D241/08 , C07D241/42 , C07D295/215 , C07D307/24 , C07D309/14 , C07D333/20 , C07D487/04 , C07D487/08
摘要： Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.
摘要翻译：式IIA和IIB的化合物是新的胍化合物，化学式id =“CHEM-US-00001”num =“000

3. 发明授权

US06716840B2 Guanidino compounds 失效
标题翻译：胍基化合物
公开(公告)号：US06716840B2
公开(公告)日：2004-04-06
申请号：US10118730
申请日：2002-04-08
申请人： Daniel Chu , Rustum S. Boyce , David Duhl , Bryan H. Chang
发明人： Daniel Chu , Rustum S. Boyce , David Duhl , Bryan H. Chang
IPC分类号： A61K315375
CPC分类号： C07D209/46 , C07D209/48 , C07D217/24 , C07D235/08 , C07D235/10
摘要： Compounds having the general structure I are provided: X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of and L is selected from the group consisting of N, O, S, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r”) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
摘要翻译：提供具有通式结构I的化合物：X和Y独立地选自CH 2，N，NR 9，C = O，C = S，S = O，SO 2，S，O，（R 6 R 7）n，C（= O） - （CR 6 R 7）n和C（= S） - （CR 6 R 7）n，其中n为1 W选自N，O，S，S = O，SO 2，C（O），NC（O），NC（S），OC （O），OC（S），C（NR 10），C（NOR 10））和共价键。 Z 1，Z 2和Z 3独立地选自取代的碳和氮。式I化合物是黑皮质素-4受体（“MC-4r”）的激动剂，因此可能具有控制人类MC-4r作用相关疾病如肥胖和II型糖尿病的有用性质。

4. 发明授权

US07034033B2 Substituted quinazolinone compounds 失效
公开(公告)号：US07034033B2
公开(公告)日：2006-04-25
申请号：US10444495
申请日：2003-05-23
申请人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
发明人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
IPC分类号： C07D239/90 , A61K31/517 , A61P3/04 , A61P3/10
CPC分类号： C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
摘要： A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.

5. 发明授权

US07858631B2 Substituted pyrido [2,3-d] pyrimidinone compounds 失效
标题翻译：取代的吡啶并[2,3-d]嘧啶酮化合物
公开(公告)号：US07858631B2
公开(公告)日：2010-12-28
申请号：US10515434
申请日：2003-05-23
申请人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
发明人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
IPC分类号： A61K31/519
CPC分类号： C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
摘要： A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure of Formulas (IA), (IB), or (IC): where the values of the variable are defined herein.
摘要翻译：提供了能够作为MC4-R激动剂的各种低分子量含胍基分子。该化合物可用于治疗MC4-R介导的疾病。化合物具有式（IA），（IB）或（IC）的结构：其中变量的值在本文中定义。

6. 发明申请

US20100105654A1 SUBSTITUTED QUINAZOLINONE COMPOUNDS 审中-公开
标题翻译：替代喹唑啉酮化合物
公开(公告)号：US20100105654A1
公开(公告)日：2010-04-29
申请号：US12605174
申请日：2009-10-23
申请人： Rustum S. BOYCE , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher R. Conlee , Brian D. Thompson , Judith de Armas Kuntz , David L. Musso , Kevin K. Barvian , Stephen A. Thomson , William R. Swain , Kien S. Du , Brian A. Chauder , Jason D. Speake , Michael J. Bishop
发明人： Rustum S. BOYCE , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher R. Conlee , Brian D. Thompson , Judith de Armas Kuntz , David L. Musso , Kevin K. Barvian , Stephen A. Thomson , William R. Swain , Kien S. Du , Brian A. Chauder , Jason D. Speake , Michael J. Bishop
IPC分类号： A61K31/517 , C07D403/12 , C07D239/86 , C07D403/14 , C07D413/14 , C07D417/14 , A61K31/5377 , A61P3/04 , A61P3/10
CPC分类号： C07D217/24 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structures VA, VB, VIIA and VIIB where the values of the variables are defined herein.
摘要翻译：提供了能够作为MC4-R激动剂的各种小分子，含胍分子。当给予受试者时，这些化合物可用于治疗MC4-R介导的疾病。化合物具有结构VA，VB，VIIA和VIIB，其中变量的值在本文中定义。

7. 发明授权

US07858641B2 Substituted dihydroisoquinolinone compounds 失效
标题翻译：取代的二氢异喹啉酮化合物
公开(公告)号：US07858641B2
公开(公告)日：2010-12-28
申请号：US11248040
申请日：2005-10-11
申请人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
发明人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Bryan Chang
IPC分类号： A61K31/47
CPC分类号： C07D253/08 , C07D217/24 , C07D239/88 , C07D239/90 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04
摘要： A variety of low molecular weight, guanidino-containing dihydroisoquinolinoines capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure ID where the values of the variable are defined herein.
摘要翻译：提供了能够作为MC4-R激动剂的各种低分子量含胍基的二氢异喹啉基。该化合物可用于治疗MC4-R介导的疾病。化合物具有其中在此定义变量的值的结构ID。

8. 发明授权

US07625909B2 Substituted quinazolinone compounds 失效
标题翻译：取代喹唑啉酮化合物
公开(公告)号：US07625909B2
公开(公告)日：2009-12-01
申请号：US10850967
申请日：2004-05-21
申请人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher R. Conlee , Brian D. Thompson , Judith de Armas Kuntz , David L. Musso , Kevin K. Barvian , Stephen A. Thomson , William R. Swain , Kien S. Du , Brian A. Chauder , Jason D. Speake , Michael J. Bishop
发明人： Rustum S. Boyce , Natalia Aurrecoechea , Daniel Chu , Aaron Smith , Christopher R. Conlee , Brian D. Thompson , Judith de Armas Kuntz , David L. Musso , Kevin K. Barvian , Stephen A. Thomson , William R. Swain , Kien S. Du , Brian A. Chauder , Jason D. Speake , Michael J. Bishop
IPC分类号： A61K31/517 , A61K31/519 , A61P5/50 , C07D239/88 , C07D239/95 , C07D471/04 , C07D487/04
CPC分类号： C07D217/24 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structure IA, IB, and IC where the values of the variables are defined herein.
摘要翻译：提供了能够作为MC4-R激动剂的各种小分子，含胍分子。当给予受试者时，这些化合物可用于治疗MC4-R介导的疾病。化合物具有结构IA，IB和IC，其中变量的值在本文中定义。

9. 发明申请

US20090131304A1 Semi-Synthetic Desmethyl-Vancomycin-Based Glycopeptides With Antibiotic Activity 审中-公开
标题翻译：具有抗生素活性的半合成去甲基 - 万古霉素基糖肽
公开(公告)号：US20090131304A1
公开(公告)日：2009-05-21
申请号：US12268364
申请日：2008-11-10
申请人： Daniel Chu , Yaohui Lei , Yu Bai , Zhi-Jie Ni , John Jian-Xin Wang
发明人： Daniel Chu , Yaohui Lei , Yu Bai , Zhi-Jie Ni , John Jian-Xin Wang
IPC分类号： A61K38/12 , C07K9/00
CPC分类号： C07K9/008 , A61K38/00
摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of the desmethyl-vancomycin scaffold, in particular, acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. In addition, compounds of the invention include desmethyl-vancomycin scaffolds on which the acid moiety on the macrocyclic ring is converted to certain substituted amides and the amino substituent on the amino-substituted sugar moiety is alkylated with certain alkyl groups. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
摘要翻译：具有抗菌活性的半合成糖肽基于脱甲基万古霉素支架的修饰，特别是在该支架上具有某些酰基的氨基取代的糖部分上的氨基取代基的酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。此外，本发明的化合物包括去甲基 - 万古霉素支架，大环上的酸部分转化为某些取代的酰胺，氨基取代的糖部分上的氨基取代基被某些烷基烷基化。还提供了合成化合物的方法，含有化合物的药物组合物，以及用于治疗和/或预防疾病，特别是细菌感染的化合物的使用方法。

10. 发明授权

US07368422B2 Semi-synthetic rearranged vancomycin/desmethyl-vancomycin-based glycopeptides with antibiotic activity 失效
标题翻译：半合成重组万古霉素/脱甲基万古霉素类糖肽具有抗菌活性
公开(公告)号：US07368422B2
公开(公告)日：2008-05-06
申请号：US11361311
申请日：2006-02-24
申请人： Yaohui Lei , Yu Bai , Daniel Chu , Zhi-Jie Ni , John Jian-Xin Wang
发明人： Yaohui Lei , Yu Bai , Daniel Chu , Zhi-Jie Ni , John Jian-Xin Wang
IPC分类号： A61K38/02 , A61K38/12 , A61K31/70 , C07K7/64 , C07K9/00 , C07K5/12
CPC分类号： C07K9/008
摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
摘要翻译：具有抗菌活性的半合成糖肽基于重排的万古霉素或去甲基 - 万古霉素支架的修饰，特别是在该支架上的具有某些酰基的氨基取代的糖部分上的氨基取代基的烷基化或酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。还提供了合成化合物的方法，含有化合物的药物组合物，以及用于治疗和/或预防疾病，特别是细菌感染的化合物的使用方法。

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