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2. 发明申请

WO2012166716A3 SUBSITUTED ALIPHANES, CYCLOPHANES, HETERAPHANES, HETEROPHANES, HETERO-HETERAPHANES AND METALLOCENES USEFUL FOR TREATING HCV INFECTIONS 审中-公开
公开(公告)号：WO2012166716A3
公开(公告)日：2012-12-06
申请号：PCT/US2012/039835
申请日：2012-05-29
申请人： ACHILLION PHARMACEUTICALS, INC. , WILES, Jason Allan , WANG, Qiuping , HASHIMOTO, Akihiro , PAIS, Godwin , CHEN, Dawei , WANG, Xiangzhu , GADHACHANDA, Venkat , PHADKE, Avinash , DESHPANDE, Milind
发明人： WILES, Jason Allan , WANG, Qiuping , HASHIMOTO, Akihiro , PAIS, Godwin , CHEN, Dawei , WANG, Xiangzhu , GADHACHANDA, Venkat , PHADKE, Avinash , DESHPANDE, Milind
IPC分类号： A61K31/4178 , A61K31/4164 , A61P31/12 , A61P31/00
摘要： The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula (I) D-M-D (Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group -P-A-P- where A is (Formula I) Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/ or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/ and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.

3. 发明申请

WO2008106130A2 TERTIARY AMINE SUBSTITUTED PEPTIDES USEFUL AS INHIBITORS OF HCV REPLICATION 审中-公开
标题翻译：用于复制HCV的三价胺取代肽
公开(公告)号：WO2008106130A2
公开(公告)日：2008-09-04
申请号：PCT/US2008/002524
申请日：2008-02-26
申请人： ACHILLION PHARMACEUTICALS, INC. , AGARWAL, Atul , WANG, Xiangzhu , CHEN, Dawei , ZHANG, Suoming , PHADKE, Avinash
发明人： AGARWAL, Atul , WANG, Xiangzhu , CHEN, Dawei , ZHANG, Suoming , PHADKE, Avinash
IPC分类号： A61P31/14 , A61K38/06 , C07K5/08
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06026 , C07K5/06034 , C07K5/0806 , C07K5/0808 , C07K5/0812
摘要： The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R 1 -R 12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.
摘要翻译：本发明提供可用作HCV复制抑制剂的式（I）的叔胺取代的肽。本文描述式I中的变量R和R 1 -R 12。本发明还包括制备这些化合物的方法。本发明还包括含有叔胺取代的肽的药物组合物和使用这些化合物的方法，包括使用该化合物治疗丙型肝炎感染的方法。

4. 发明申请

WO2005007601A2 SUBSTITUTED ARYLTHIOUREA DERIVATIVES USEFUL AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：用作病毒复制抑制剂的取代的芳香硫脲衍生物
公开(公告)号：WO2005007601A2
公开(公告)日：2005-01-27
申请号：PCT/US2004/022599
申请日：2004-07-08
申请人： ACHILLION PHARMACEUTICALS, INC. , PHADKE, Avinash , QUINN, Jesse , OHKANDA, Junko , THURKAUF, Andrew , SHEN, Yiping , LIU, Cuixian , CHEN, Dawei , LI, Shouming
发明人： PHADKE, Avinash , QUINN, Jesse , OHKANDA, Junko , THURKAUF, Andrew , SHEN, Yiping , LIU, Cuixian , CHEN, Dawei , LI, Shouming
IPC分类号： C07C15/00
CPC分类号： C07D211/64 , C07C335/12 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/20 , C07C335/22 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/44 , C07D211/14 , C07D211/62 , C07D215/06 , C07D217/04 , C07D295/135 , C07D317/66
摘要： Substituted arylthiourea compounds of Formula I, and the pharmaceutically acceptable salts of such compounds, useful as antiviral agents, are provided herein. Certain substituted arylthioureas disclosed herein are potent and/ or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions containing one or more substituted arylthiourea compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Such pharmaceutical compositions may contain a substituted arylthiourea as the only active agent or may contain a combination of a substituted arylthiourea derivative and one or more other pharmaceutically active agents. Methods of treating Hepatitis C viral infections in mammals are also provided herein.
摘要翻译：本文提供了式I的取代的芳基硫脲化合物和可用作抗病毒剂的此类化合物的药学上可接受的盐。本文公开的某些取代的芳基硫脲是病毒复制的有效和/或选择性抑制剂，特别是丙型肝炎病毒复制。本文提供了含有一种或多种取代的芳基硫脲化合物和一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。这种药物组合物可以含有取代的芳基硫脲作为唯一的活性剂，或者可以含有取代的芳基硫脲衍生物和一种或多种其它药物活性剂的组合。本文还提供了治疗哺乳动物的丙型肝炎病毒感染的方法。

5. 发明申请

WO2007121310A2 FUEL TANK WITH INTEGRATED EVAPORATIVE EMISSIONS SYSTEM 审中-公开
标题翻译：具有集成蒸发排放系统的燃油箱
公开(公告)号：WO2007121310A2
公开(公告)日：2007-10-25
申请号：PCT/US2007/066540
申请日：2007-04-12
申请人： BLACK & DECKER INC. , GRANT, Jeffrey P. , BUCK, John E. , CHEN, Dawei (David) , NELSON, Michael A.
发明人： GRANT, Jeffrey P. , BUCK, John E. , CHEN, Dawei (David) , NELSON, Michael A.
IPC分类号： F02M25/08
CPC分类号： F02M37/0082 , F02M25/0836
摘要： An evaporative emissions fuel system for a general-purpose engine includes a fuel tank with a valve assembly located within the fuel tank for guiding fuel vapor to a canister. The canister contains activated charcoal to treat the fuel vapor and guide the vapor to a carburetor which burns the fuel vapor and hydrocarbons. The valve assembly has a valve opening for receiving the fuel vapor and a float responsive to the fuel within the tank for sealing the valve opening when the fuel within the tank is at a fuel level capable of entering the valve opening.
摘要翻译：用于通用发动机的蒸发排放燃料系统包括具有位于燃料箱内的阀组件的燃料箱，用于将燃料蒸气引导至罐。罐包含活性炭以处理燃料蒸气并将蒸汽引导至燃烧燃料蒸气和碳氢化合物的化油器。阀组件具有用于接收燃料蒸汽的阀开口和响应于罐内的燃料的浮子，用于当罐内的燃料处于能够进入阀开口的燃料水平面时密封阀开口。

6. 发明申请

WO2022266753A1 BIVALENT COMPOUNDS, CONJUGATES AND USES THEREOF 审中-公开
公开(公告)号：WO2022266753A1
公开(公告)日：2022-12-29
申请号：PCT/CA2022/050991
申请日：2022-06-20
申请人： RISEN (SUZHOU) PHARMA TECH CO., LTD. , LV, Jiasheng , SIYANG, Haixiao , YIN, Yijie , GUO, Wantao , LI, Haiming , CHEN, Dawei , GU, Jiamin , KONG, Xianqi , PAN, Jun , MA, Xinxin , SONG, Peiming , WU, Chun , FENG, Hui , YAO, Sheng
发明人： LV, Jiasheng , SIYANG, Haixiao , YIN, Yijie , GUO, Wantao , LI, Haiming , CHEN, Dawei , GU, Jiamin , KONG, Xianqi , PAN, Jun , MA, Xinxin , SONG, Peiming , WU, Chun , FENG, Hui , YAO, Sheng
IPC分类号： C07C275/16 , A61K47/54 , A61P3/00 , A61P9/00 , C07C233/47 , C07C237/22 , C07C271/02 , C07C279/14 , C07C323/59 , C07D207/416 , C07D249/04 , C07K16/00 , C12N15/113 , A61K47/542 , A61K47/545 , A61K47/549
摘要： There are provided conjugates of Formula (V) wherein R1 is a triantennary targeting moiety comprising N-acetyl galactosamine and R2 is a bioactive agent which is preferably an oligonucleotide, as well as pharmaceutical compositions and methods of use of the conjugates for the treatment, inhibition, or prevention of diseases and disorders which are therapeutic targets of the bioactive agent. In preferred embodiments the conjugate preferentially binds to asiaglycoprotein receptors (ASGPR). In preferred embodiments, the oligonucleotide is SiRNA which targets the PCSK9 gene, providing treatment options for lipid disorders such as hyperlipidemia.

7. 发明申请

WO2010068761A3 4-AMINO-4-OXOBUTANOYL PEPTIDE CYCLIC ANALOGUES, INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译： 4-氨基-4-氧杂多酚类环状类似物，病毒复制抑制剂
公开(公告)号：WO2010068761A3
公开(公告)日：2010-10-21
申请号：PCT/US2009067507
申请日：2009-12-10
申请人： ACHILLION PHARMACEUTICALS INC , PHADKE AVINASH , WANG XIANGZHU , PAIS GODWIN , HASHIMOTO AKIHIRO , GADHACHANDA VENKAT , CHEN DAWEI , AGARWAL ATUL , ZHANG SUOMING , LIU CUIXIAN , LI SHOUMING , DESHPANDE MILIND
发明人： PHADKE AVINASH , WANG XIANGZHU , PAIS GODWIN , HASHIMOTO AKIHIRO , GADHACHANDA VENKAT , CHEN DAWEI , AGARWAL ATUL , ZHANG SUOMING , LIU CUIXIAN , LI SHOUMING , DESHPANDE MILIND
IPC分类号： C07D403/14 , C07D403/12 , C07D417/14
CPC分类号： C07K5/12 , A61K38/00 , C07K5/06165
摘要： The invention provides 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Formula I and the pharmaceutically salts thereof. The variables are defined herein. Certain compounds of Formula I are useful as antiviral agents. 4-amino-4-oxobutanoyl peptide cyclic analogues as disclosed herein are potent and/ or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide cyclic analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptide cyclic analogue as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptide cyclic analogue and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in patients.
摘要翻译：本发明提供了式I的4-氨基-4-氧代丁酰基肽及其环状类似物及其药学上可接受的盐。变量在此定义。某些式I化合物可用作抗病毒剂。本文公开的4-氨基-4-氧代丁酰基肽环类似物是病毒复制，特别是丙型肝炎病毒复制的有效和/或选择性抑制剂。本发明还提供含有一种或多种4-氨基-4-氧代丁酰基肽环状类似物和一种或多种药学上可接受的载体的药物组合物。这样的药物组合物可以含有4-氨基-4-氧代丁酰基肽环类似物作为唯一的活性剂，或者可以含有4-氨基-4-氧代丁酰基肽环类似物和一种或多种其它药物活性剂的组合。本发明还提供了用于治疗患者中的病毒感染（包括丙型肝炎感染）的方法。

8. 发明申请

WO2010068761A2 4-AMINO-4-OXOBUTANOYL PEPTIDE CYCLIC ANALOGUES, INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译： 4-氨基-4-氧代丁酰基肽类环化类似物，病毒复制抑制剂
公开(公告)号：WO2010068761A2
公开(公告)日：2010-06-17
申请号：PCT/US2009/067507
申请日：2009-12-10
申请人： ACHILLION PHARMACEUTICALS, INC. , PHADKE, Avinash , WANG, Xiangzhu , PAIS, Godwin , HASHIMOTO, Akihiro , GADHACHANDA, Venkat , CHEN, Dawei , AGARWAL, Atul , ZHANG, Suoming , LIU, Cuixian , LI, Shouming , DESHPANDE, Milind
发明人： PHADKE, Avinash , WANG, Xiangzhu , PAIS, Godwin , HASHIMOTO, Akihiro , GADHACHANDA, Venkat , CHEN, Dawei , AGARWAL, Atul , ZHANG, Suoming , LIU, Cuixian , LI, Shouming , DESHPANDE, Milind
IPC分类号： C07D403/14 , C07D403/12 , C07D417/14
CPC分类号： C07K5/12 , A61K38/00 , C07K5/06165
摘要： The invention provides 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Formula I and the pharmaceutically salts thereof. The variables are defined herein. Certain compounds of Formula I are useful as antiviral agents. 4-amino-4-oxobutanoyl peptide cyclic analogues as disclosed herein are potent and/ or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide cyclic analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptide cyclic analogue as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptide cyclic analogue and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in patients.
摘要翻译：本发明提供式I的4-氨基-4-氧代丁酰基肽及其环状类似物及其药用盐。变量在此定义。式I的某些化合物可用作抗病毒剂。如本文所公开的4-氨基-4-氧代丁酰基肽环类似物是病毒复制的有效和/或选择性抑制剂，特别是丙型肝炎病毒复制。本发明还提供了含有一种或多种4-氨基-4-氧代丁酰基肽环类似物和一种或多种药学上可接受的载体的药物组合物。此类药物组合物可含有4-氨基-4-氧代丁酰基肽环状类似物作为唯一活性剂，或可含有4-氨基-4-氧代丁酰基肽环状类似物与一种或多种其他药物活性剂的组合。本发明还提供了用于治疗患者中的病毒感染（包括丙型肝炎感染）的方法。

9. 发明申请

WO2009042668A3 UREA-CONTAINING PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：作为病毒复制的抑制剂的尿素包含肽
公开(公告)号：WO2009042668A3
公开(公告)日：2009-06-25
申请号：PCT/US2008077497
申请日：2008-09-24
申请人： ACHILLION PHARMACEUTICALS INC , CHEN DAWEI , DESHPANDE MILIND , PHADKE AVINASH
发明人： CHEN DAWEI , DESHPANDE MILIND , PHADKE AVINASH
IPC分类号： C07K5/10 , A61K31/69 , A61K38/00 , A61K38/12 , C07F5/02 , C07K5/06
CPC分类号： C07K5/0823 , A61K38/00 , C07K5/06165
摘要： The invention provides compounds urea-containing peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables T, R1-R9, J, L, M, Y, Z, m, n, and t are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain urea-containing peptide compounds disclosed herein are potent and/ or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more urea containing peptides compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents. Such pharmaceutical compositions may contain a urea containing peptides compound as the only active agent or may contain a combination of a urea containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.
摘要翻译：本发明提供式I化合物的含脲的肽化合物及其药用盐和水合物。变量T，R1-R9，J，L，M，Y，Z，m，n和t在本文中定义。某些式I化合物可用作抗病毒剂。本文公开的某些含脲的肽化合物是病毒复制的有效和/或选择性抑制剂，特别是丙型肝炎病毒复制。本发明还提供含有一种或多种含尿素的肽化合物和一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。这样的药物组合物可以含有含有肽化合物作为唯一活性剂的尿素，或者可以含有含尿素的肽化合物和一种或多种其它药学活性剂的组合。本发明还提供了用于治疗哺乳动物中的病毒感染（包括丙型肝炎感染）的方法。

10. 发明申请

WO2009042668A2 UREA-CONTAINING PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：含有尿素的肽作为病毒复制的抑制剂
公开(公告)号：WO2009042668A2
公开(公告)日：2009-04-02
申请号：PCT/US2008/077497
申请日：2008-09-24
申请人： ACHILLION PHARMACEUTICALS, INC. , CHEN, Dawei , DESHPANDE, Milind , PHADKE, Avinash
发明人： CHEN, Dawei , DESHPANDE, Milind , PHADKE, Avinash
IPC分类号： C07K5/10 , C07K5/06 , C07F5/02 , A61K38/12 , A61K38/00 , A61K31/69
CPC分类号： C07K5/0823 , A61K38/00 , C07K5/06165
摘要： The invention provides compounds urea-containing peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables T, R 1 -R 9 , J, L, M, Y, Z, m, n, and t are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain urea-containing peptide compounds disclosed herein are potent and/ or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more urea containing peptides compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents. Such pharmaceutical compositions may contain a urea containing peptides compound as the only active agent or may contain a combination of a urea containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.
摘要翻译：本发明提供了式I化合物的含脲的肽化合物及其药用盐和水合物。变量T，R1-R9，J，L，M，Y，Z，m，n和t在本文中定义。式I的某些化合物可用作抗病毒剂。本文公开的某些含脲肽化合物是病毒复制的有效和/或选择性抑制剂，特别是丙型肝炎病毒复制。本发明还提供了含有一种或多种含脲的肽化合物和一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。这样的药物组合物可以含有含脲的肽化合物作为唯一的活性剂，或者可以含有含脲的肽化合物和一种或多种其他药物活性剂的组合。本发明还提供了用于治疗哺乳动物中的病毒感染（包括丙型肝炎感染）的方法。

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