- Development of DHQ-based chemical biology probe to profile cellular targets for HBV
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Chronic hepatitis B virus (HBV) infection has been a serious public health burden worldwide. Current anti-HBV therapies could not eliminate HBV ultimately. Considering the characteristics of HBV, it is impossible to be entirely cured based on current therapies. Therefore, it is urgently needed to develop novel therapeutic agents with new mechanism of action. The dihydroquinolizinone (DHQ) derivatives exhibited potent anti-HBV activity by decreasing HBV DNA and HBsAg level in an obscure mechanism of action. In this study, we have optimized the DHQ scaffold, developed the photoaffinity probe, with which to identify potential binding proteins.
- Zhang, Qing,Huang, Jianzhou,Chow, Hoi Yee,Wang, Jinzheng,Zhang, Yingjun,Fung, Yi Man Eva,Ren, Qingyun,Li, Xuechen
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supporting information
(2020/10/29)
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- Compound with PDE4 inhibitory activity, preparation method, composition and application thereof
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The invention belongs to the field of medicines, and particularly relates to a compound with PDE4 inhibitory activity, and a preparation method, composition and application thereof. The compound is acompound with a structure shown as a formula I or pharmaceutically acceptable salt thereof, in the formula, R1 represents N, N-dimethylaminoethyl, 3-amino-3-oxopropyl, 3, 3-difluoropropyl and methoxyalkyl, and R2 represents a cyano group, an aminosulfonyl group, an aminocarbonyl group or an alkyl acylamino group. The compound provided by the invention has good PDE4 inhibitory activity, has the advantages of high efficiency and low side effect, and can be used for preparing drugs for preventing and/or treating allergic diseases, autoimmune diseases or inflammatory diseases.
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Paragraph 0072
(2020/11/25)
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- NOVEL OXA-AND AZA-TRICYCLIC 4-PYRIDONE-3-CARBOXYLIC ACID FOR TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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Provided herein are oxa- and aza-tricyclic 4-pyridone-3-carboxylic acid compounds, their manufacture, pharmaceutical compositions comprising them, and their use as medicaments for inhibiting HBsAg secretion and HBV DNA production, and for treatment and/or prophylaxis of hepatitis B infection.
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Paragraph 145
(2019/10/01)
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- NOVEL THERAPEUTIC AGENTS FOR THE TREATMENT OF HBV INFECTION
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The disclosure includes compounds of Formula (I), wherein Z1, Z2, Z3, X, R1, R2, R3, R4, R5, R6, and R7 are defined herein. Also disclosed is a method for treating HBV infection.
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Page/Page column 42
(2018/03/01)
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- Novel isoquinoline compound and medical application thereof
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The invention relates to an isoquinoline compound shown as a formula (A) or a stereoisomer, a pharmaceutically acceptable salt, a hydrate, a solvate or a crystal thereof, a medicinal composition thereof and application thereof as antiviral medicines. The isoquinoline compound inhibits hepatitis B DNA activity and hepatitis B surface antigen activity at the same time. The invention particularly relates to application thereof to preparation of medicines for treating and/or preventing hepatitis B, hepatitis B viruses (HBV) thereof and other viral infectious diseases, in particular to treatment and/or prevention of the hepatitis B and the hepatitis B viruses as HBV Surface antigen inhibitor medicines and HBV DNA production inhibitor medicines.
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Paragraph 0097; 0099; 0100; 0101
(2018/11/22)
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- PROCESS FOR THE PREPARATION OF (6S)-6-ALKYL-10-ALKOXY-9-(SUBSTITUTED ALKOXY)-2-OXO-6,7-DIHYDROBENZO[A]QUINOLIZINE-3-CARBOXYLIC ACID ANALOGUES
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The present invention relates to a process for synthesizing a compound of formula (I), wherein R1 is C1-6alkoxy or haloC1-6alkoxy, R2 is C1-6alkyl unsubstituted or substituted by a substituent selected from C1-6alkoxy and haloC1-6alkoxy, R3 is C1-6alkyl,or pharmaceutically acceptable salts thereof, which is useful for prophylaxis and treatment of a viral disease in a patient relating to hepatitis B virus infection or a disease caused by hepatitis B virus infection.
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Page/Page column 17: 18
(2017/02/24)
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- NEW CRYSTALLINE FORMS OF (6S)-10-METHOXY-6-ISOPROPYL-9-(3-METHOXYPROPOXY)-2-OXO-6,7-DIHYDROBENZO[A]QUINOLIZINE-3-CARBOXYLIC ACID
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The present invention relates to a new crystalline form of compound (I), (6S)-10-methoxy-6-isopropyl-9-(3-methoxypropoxy)-2-oxo-6,7-dihydrobenzo[a]quinolizine-3- carboxylic acid and pharmaceutical compositions comprising the crystalline forms thereof disclosed herein, which may be used for the treatment or prophylaxis of a viral disease in a patient relating to hepatitis B infection or a disease caused by hepatitis B infection.
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Page/Page column 16
(2017/02/24)
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- NOVEL 6,7-DIHYDROBENZO[A]QUINOLIZIN-2-ONE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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The invention provides novel compounds having the general formula (I) wherein R1 to R6, W and X are as described herein and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
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Page/Page column 69
(2016/06/01)
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- NOVEL 2-OXO-6,7-DIHYDROBENZO[A]QUINOLIZINE-3-CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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The invention provides novel compounds having the general formula (I), wherein R1, R2, R3, R4, R5 and Ar are as described herein, compositions including compounds and methods of using the compounds.
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Page/Page column 23
(2016/09/22)
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- The development of a complementary pathway for the synthesis of aliskiren
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The synthesis of aliskiren (1), a recently marketed drug for the treatment of hypertension, is presented. The focus of our synthetic effort is to develop an efficient pathway for the synthesis of (2S,7R,E)-2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy) benzyl)-N,N,8-trimethylnon-4-enamide (2a), which has been used as the advanced intermediate toward aliskiren. After an extensive investigation of three different strategies designed to construct the E-olefin functionality in 2a by employing the olefin cross-metathesis, Horner-Wadsworth-Emmons (HWE), and Julia-type olefinations, we have established a new protocol for the synthesis of 2a with a substantially improved overall efficiency in terms of the yield (ca. 33%), and diastereo- and E/Z-selectivity. The key transformations were the Evans chiral auxiliary-aided asymmetric allylation for the synthesis of the appropriate chiral intermediates in excellent enantiomeric purity of higher than 97% ee and a modified Julia-Kocienski olefination for the highly selective construction of E-2a with up to 13.6:1 E/Z ratio from the chiral intermediates. Consequently, the results provide an appealing option for the synthesis of aliskiren. This journal is
- Li, Le-Le,Ding, Jin-Ying,Gao, Lian-Xun,Han, Fu-She
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supporting information
p. 1133 - 1140
(2015/03/03)
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- Novel dihydroquinolizinones for the treatment and prophylaxis of hepatitis B virus infection
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The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5 and R6 are as described herein, compositions including the compounds and methods of using the compounds.
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Paragraph 1550; 1551
(2015/08/04)
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- NOVEL DIHYDROQUINOLIZINONES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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The invention provides novel compounds having the general formula (I) wherein R1, R2 R3, R4, R5 and R6 are as described herein, compositions including the compounds and methods of using the compounds in the treatment of the hepatitis B virus.
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Page/Page column 220
(2015/09/23)
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- NOVEL DIHYDROQUINOLIZINONES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R6, X and Y are as described in the description and in the claims, as well as or pharmaceutically acceptable salts, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.
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Page/Page column 72
(2016/04/26)
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- Total synthesis of "Aliskiren": The first renin inhibitor in clinical practice for hypertension
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We report a "macrocycle route" toward aliskiren, a drug presently marketed for the treatment of hypertension, using a highly stereocontrolled approach starting from a common "isopropyl chiron". Highlights of the synthesis include a challenging RCM reaction to produce a nine-membered unsaturated lactone, a highly stereoselective catalytic Du Bois aziridination, and a regio- and diastereoselective aziridine ring-opening to a vicinal amino alcohol.
- Hanessian, Stephen,Guesne, Sebastien,Chenard, Etienne
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supporting information; experimental part
p. 1816 - 1819
(2010/09/16)
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- METHODS OF TREATING ALZHEIMER'S DISEASE USING ARYL ALKANOIC ACID AMIDES
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Disclosed are methods for treating Alzheimer’s disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula 1 (1) wherein the variables R1-R8 and X are defined herein.
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