| Tetracyclic fused heterocyclic compound and use thereof as hcv polymerase inhibitor -> Monitor Keywords |
|
|
  Tetracyclic fused heterocyclic compound and use thereof as hcv polymerase inhibitorUSPTO Application #: 20070049593Title: Tetracyclic fused heterocyclic compound and use thereof as hcv polymerase inhibitor Abstract: wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] (end of abstract)
Agent: Leydig Voit & Mayer, Ltd - Chicago, IL, US Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura USPTO Applicaton #: 20070049593 - Class: 514243000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Hetero Ring Is Six-membered Consisting Of Three Nitrogens And Three Carbon Atoms, Asymmetrical (e.g., 1,2,4-triazine, Etc.), Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos The Patent Description & Claims data below is from USPTO Patent Application 20070049593. Brief Patent Description - Full Patent Description - Patent Application Claims
TECHNICAL FIELD [0001] The present invention relates to a tetracyclic fused heterocyclic compound or a pharmaceutically acceptable salt thereof, which shows anti-hepatitis C virus (HCV) activity, particularly anti-HCV activity based on an RNA-dependent RNA polymerase inhibitory activity. In addition, the present invention relates to a hepatitis C virus polymerase inhibitor, an anti-hepatitis C virus agent and a therapeutic agent for hepatitis C containing said tetracyclic fused heterocyclic compound or a pharmaceutically acceptable salt thereof. BACKGROUND ART [0002] In 1989, a main causative virus of non-A non-B posttransfusion hepatitis was found and named hepatitis C virus (HCV). Since then, several types of hepatitis viruses have been found besides type A, type B and type C, wherein hepatitis caused by HCV is called hepatitis C. [0003] The patients infected with HCV are considered to involve several percent of the world population, and the infection with HCV characteristically becomes chronic. [0004] HCV is an envelope RNA virus, wherein the genome is a single strand plus-strand RNA, and belongs to the genus Hepacivirus of Flavivirus (from The International Committee on Taxonomy of Viruses, International Union of Microbiological Societies). Of the same hepatitis viruses, for example, hepatitis B virus (HBV), which is a DNA virus, is eliminated by the immune system and the infection with this virus ends in an acute infection except for neonates and infants having yet immature immunological competence. In contrast, HCV somehow avoids the immune system of the host due to an unknown mechanism. Once infected with this virus, even an adult having a mature immune system frequently develops persistent infection. When chronic hepatitis is associated with the persistent infection with HCV, it advances to cirrhosis or hepatic cancer in a high rate. Enucleation of tumor by operation does not help much, because the patient often develops recurrent hepatic cancer due to the sequela inflammation in non-cancerous parts. In addition, there is a report on the involvement of HCV infection in dermatosis such as chronic urticaria, lichen planus, cryoglobulinemic purpura and the like (The Japanese Journal of Dermatology, Vol. 111, No. 7, pages 1075-1081, 2001). [0005] Thus, an effective therapeutic method of hepatitis C is desired. Apart from the symptomatic therapy to suppress inflammation with an anti-inflammatory agent, the development of a therapeutic agent that reduces HCV to a low level free from inflammation and that eradicates HCV has been strongly demanded. [0006] At present, a treatment with interferon is the only effective method known for the eradication of HCV. However, interferon can eradicate the virus only in about one-third of the patient population. For the rest of the patients, it has no effect or provides only a temporary effect. In recent years, polyethylene glycolated interferon has been put to practical use, and enhanced effects and reduced side effects have been achieved. However, complete response rate still remains at a low level, and therefore, an anti-HCV drug to be used in the place of or concurrently with interferon is awaited in great expectation. [0007] In recent years, Ribavirin (1-.beta.-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide) has become commercially available as a therapeutic agent for hepatitis C, which is to be used concurrently with interferon. It enhances the efficacy of interferon but only to a low efficacy rate, and a different novel therapeutic agent for hepatitis C is desired. [0008] Also, an attempt has been made to potentiate the immunocompetence of the patient with an interferon agonist, an interleukin-12 agonist and the like, thereby to eradicate the virus, but an effective pharmaceutical agent has not been found yet. [0009] In addition, the inhibition of HCV growth, wherein HCV-specific protein is targeted, has been drawing attention these days. [0010] The gene of HCV encodes a protein such as serine protease, RNA helicase, RNA-dependent RNA polymerase and the like. These proteins function as a specific protein essential for the growth of HCV. [0011] One of the specific proteins, RNA-dependent RNA polymerase (hereinafter to be also briefly referred to as an HCV polymerase), is an enzyme essential for the growth of the virus. The gene replication of HCV having a plus-strand RNA gene is considered to involve synthesis of a complementary minus-strand RNA by the use of the plus-strand RNA as a template and using the obtained minus-strand RNA as a template, amplifying the plus-strand RNA. The portion called NS5B of a protein precursor, that HCV codes for, has been found to show an RNA-dependent RNA polymerase activity (EMBO J., Vol. 15, pages 12-22, 1996), and is considered to play a central role in the HCV gene replication. [0012] Therefore, an HCV polymerase inhibitor can be a target in the development of an anti-HCV drug, and the development thereof is eagerly awaited. However, an effective HCV polymerase inhibitor has not been developed yet, like in other attempts to develop an anti-HCV drug based on other action mechanisms. As the situation stands, no pharmaceutical agent can treat hepatitis C satisfactorily. [0013] The following describes known compounds comparatively similar to the present invention. [0014] WO03/099824 discloses the following compound a etc. as anti-HCV agents, and teaches that this compound shows an HCV polymerase inhibitory action (WO03/099824, Example 4 (page 32, line 10-page 35), Table 1 (page 20)). [0015] However, the compound of the present invention is not disclosed therein and no description suggestive thereof is found in the specification. [0016] On the other hand, as known tetracyclic fused heterocyclic compounds, whose pharmaceutical use is known, the following can be mentioned. [0017] EP226508 discloses that the following compound b etc. show an anticancerous action (EP226508, Example 2 (page 4, last line--page 6, line 2), formula VII of claim 5 (page 31)). [0018] Other reference describes following compound c etc. and synthetic methods of compounds usable as central nervous system agents (Bollettino Chimico Farmaceutico, Vol. 120, No. 2, pages 102-107, 1981). [0019] However, none of these references discloses the compound of the present invention, not to mention disclosure of use of the compounds of these references as antiviral agents or description suggestive thereof. [0020] As the compounds comparatively similar to the compound of the present invention, relating to use other than a pharmaceutical agent, the following can be mentioned. [0021] JP-A-4-329547 discloses the following compound d known as an electronic photographic-sensitized material (JP-A-4-329547, formula 52 (page 7, lower right column)). [0022] A different reference discloses the following compound e etc., wherein its synthetic method is described (J. Org. Chem., Vol. 66, No. 2, pages 412-420, 2001, Table 3 No. 19 (page 415)). Continue reading... Full patent description for Tetracyclic fused heterocyclic compound and use thereof as hcv polymerase inhibitor Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Tetracyclic fused heterocyclic compound and use thereof as hcv polymerase inhibitor patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. Start now! - Receive info on patent apps like Tetracyclic fused heterocyclic compound and use thereof as hcv polymerase inhibitor or other areas of interest. ### Previous Patent Application: Bis-aryl urea compounds and methods of use Next Patent Application: Novel compounds and compositions as cathepsin inhibitors Industry Class: Drug, bio-affecting and body treating compositions ### FreshPatents.com Support Thank you for viewing the Tetracyclic fused heterocyclic compound and use thereof as hcv polymerase inhibitor patent info. IP-related news and info Results in 8.47548 seconds Other interesting Feshpatents.com categories: Medical: Surgery , Surgery(2) , Surgery(3) , Drug , Drug(2) , Prosthesis , Dentistry |
||
