- Process for making a 4-amino-4-oxobutanoyl peptide cyclic analogue, an inhibitor of viral replication, and intermediates thereof
-
The invention provides a process of preparing 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Compound I and pharmaceutically acceptable salts thereof.
- -
-
-
- METHODS FOR TREATING HCV
-
This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.
- -
-
Page/Page column 63-64
(2013/03/28)
-
- METHODS FOR TREATING HCV
-
This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.
- -
-
Paragraph 0259
(2013/10/22)
-
- HCV NS3 PROTEASE INHIBITORS
-
The present invention relates to macro-cyclic compounds of formula I that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections
- -
-
Page/Page column 37
(2012/04/10)
-
- Discovery of GS-9451: An acid inhibitor of the hepatitis C virus NS3/4A protease
-
The discovery of GS-9451 is reported. Modification of the P3 cap and P2 quinoline with a series of solubilizing groups led to the identification of potent HCV NS3 protease inhibitors with greatly improved pharmacokinetic properties in rats, dogs and monke
- Sheng, X. Christopher,Appleby, Todd,Butler, Thomas,Cai, Ruby,Chen, Xiaowu,Cho, Aesop,Clarke, Michael O.,Cottell, Jeromy,Delaney IV, William E.,Doerffler, Edward,Link, John,Ji, Mingzhe,Pakdaman, Rowchanak,Pyun, Hyung-Jung,Wu, Qiaoyin,Xu, Jie,Kim, Choung U.
-
scheme or table
p. 2629 - 2634
(2012/05/05)
-
- A concise synthesis of the HCV protease inhibitor BILN 2061 and its P3 modified analogs
-
A concise synthesis of BILN 2061 was achieved through more efficient installation of P2 4-quinoline moiety via SN2 displacement of the β-OBs group located on the 4-hydroxyl proline intermediate, which was prepared from 4-α-hydroxyl proline analog via Mitsunobu reaction with inversion of stereochemistry. In addition, a short and practical synthesis for P3 unit is also described herein. Final assembly of four fragments for BILN 2061 was achieved with an overall yield of 58% in 4 steps from P1 to 15a. Furthermore several analogs of BILN 2061 (WX-1-WX-5) containing modifications on P3 unit were synthesized successfully using the same synthetic route as described for the parent inhibitor BILN 2061. Copyright
- Liu, Dejun,Dong, Jingchao,Yin, Yunxing,Ma, Rujian,Shi, Yifeng,Wu, Hao,Chen, Shuhui,Li, Ge
-
experimental part
p. 1489 - 1502
(2011/11/01)
-
- ORGANIC COMPOUNDS AND THEIR USES
-
The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
- -
-
-
- ANTIVIRAL PHOSPHINATE COMPOUNDS
-
The invention is related to anti-viral phosphinate compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
- -
-
Page/Page column 96-97
(2008/06/13)
-
- HCV NS3 PROTEASE INHIBITORS
-
The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
- -
-
Page/Page column 40
(2008/12/05)
-
- HEPATITIS C INHIBITOR PEPTIDE ANALOGS
-
The compounds of formula I wherein R1, R2, R3 , R4 and R5 are defined herein, are useful as inhibitors of the hepatitis C virus NS3 protease The invention further relates to azalactone compounds of the formula (II) which can be reacted with an amide anion to produce the HCV NS3 protease inhibitors of formula (I)
- -
-
Page/Page column 46-47
(2010/11/25)
-
- HEPATITIS C INHIBITOR DIPEPTIDE ANALOGS
-
The present invention relates to compounds of formula (I): wherein R1, R2, R4, n and m are as defined herein and R3 is selected from: (i) -C(O)OR31 wherein R31 is (C1-6)alkyl or aryl, wherein the (C1-6)alkyl is optionally substituted with one to three halogen substituents; (ii) -C(O)NR32R33, wherein R32 and R33 are each independently selected form H, (C1-6)alkyl, and Het; (iii) -SOvR34, wherein v is 1 or 2 and R34 is selected from: (C1-6)alkyl, aryl, Het, and NR32R33 wherein R32 and R33 are as defined above; and (iv) -CO(O)-R35, wherein R35 is selected from (C1-8)alkyl, (C3-7)cycloalkyl-(C1-4)alkyl, aryl, aryl-(C1-6)alkyl, Het and Het-(C1-6)alkyl, each of which are optionally substituted with one or more substituents each independently selected from halo, (C1-6)alkyl, (C3-7)cycloalkyl, aryl, Het, hydroxyl, -O-(C1-6)alkyl, -S-(C1-6)alkyl, -SO-(C1-6)alkyl, -SO2-(C1-6)alkyl, -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl, wherein the aryl portion of the -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl are each optionally substituted with one to five halo substituents. The present invention further relates to pharmaceutical compositions containing the compounds of formula (I) and methods for using these analogs in the treatment of HCV infection.
- -
-
Page/Page column 87
(2008/06/13)
-
- HCV NS3 PROTEASE INHIBITORS
-
The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. I
- -
-
Page/Page column 60
(2008/06/13)
-
- Novel dipeptide macrocycles from 4-oxo, -thio, and -amino-substituted proline derivatives.
-
Dipeptide macrocycles of type A have been constructed in a versatile manner from the corresponding 4-heteroatom-substituted proline derivatives using an intramolecular Mitsunobu strategy.
- Arasappan, Ashok,Chen, Kevin X,Njoroge, F George,Parekh, Tejal N,Girijavallabhan, Viyyoor
-
p. 3923 - 3926
(2007/10/03)
-