- Atorvastatin Derived HMG-CoA Reductase Degradation Inducing Compound
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The present invention relates to a HMG-CoA reductase degradation-inducing compound and, more specifically, to a bifunctional compound in which atorvastatin and E3 ubiquitin ligase binding moiety are chemically linked as HMG-CoA reductase binding moiety, to a production method thereof, to a HMG-CoA reductase degradation method using the same, and to a pharmaceutical composition for preventing or treating HMG-CoA reductase-related diseases, comprising the same.
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Paragraph 0420-0424
(2020/12/01)
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- 1,3 DI-SUBSTITUTED CYCLOBUTANE OR AZETIDINE DERIVATIVES AS HEMATOPOIETIC PROSTAGLANDIN D SYNTHASE INHIBITORS
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A compound of formula (I), wherein R, R1, R2, R3, Y, Y1, a, X, and Z are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne Muscular Dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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Page/Page column 100
(2018/04/27)
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- COMPOUNDS AS HEPATITIS C VIRUS (HCV) INHIBITORS AND USES THEREOF IN MEDICINE
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Provided herein are compounds of Formula (I), or a stereoisomer, a geometric isomer, an enantiomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which are used in the treatment of HCV
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Paragraph 0058
(2016/01/25)
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- HIV INTEGRASE INHIBITORS
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The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
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- N-SUBSTITUTED PIPERIDINE DERIVATIVES AS SEROTONIN RECEPTOR AGENTS
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Disclosed herein are substantially pure forms of the compounds of Formula (I), (II), (III), (IV) and (V), or a pharmaceutically acceptable salt, prodrug, hydrate, solvate, polymorph, stereoisomer or ester thereof. Also disclosed are methods of inhibiting an activity of a serotonin receptor, methods inhibiting an activation of a serotonin receptor, and methods of alleviating or treating various disease conditions and side effects.
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Page/Page column 64-65
(2010/11/04)
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- INDOLE AND BENZOFURAN 2-CARBOXAMIDE DERIVATIVES
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Compounds of Formula (I) or Formula (II) or pharmaceutically acceptable salts thereof, wherein m, n, p, Ar R1 R2, R4 R5 and R6 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using these compounds in the treatment of Alzheimer's disease or as cognitive enhancer.
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Page/Page column 42-43
(2008/12/05)
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- HIV INTEGRASE INHIBITORS
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The present invention features compounds that are HIV integrase inhibitors useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
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Page/Page column 43
(2010/11/26)
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- PHENYLAZETIDINONE DERIVATIVES
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Various azetidinone derivatives are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.
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Page/Page column 293
(2008/06/13)
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- SUBSTITUTED ACIDS FOR THE TREATMENT OF RESPIRATORY DISEASES
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The invention relates to substituted acids of formula (I), where T,W,X,Y,Z, R1 and R2 as defined in the claims, as useful pharmaceutical compounds for treating asthma and rhinitis, pharmaceutical compositions containing them, and a processes for their preparation.
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Page/Page column 38
(2010/02/15)
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- Imidazole compounds and their use as adenosine deaminase inhibitors
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Imidazole compounds having adenosine deaminase inhibitory activity represented by the formula (I) wherein R1 is aryloxy, or aryl which is optionally substituted with suitable substituent(s); R2 is lower alkyl; R3 is hydrox
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- Substituted biphenyls
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Substituted biphenyls having glucagon receptor antagonistic activity. Claimed compounds have the formula wherein R1aand R1bindependently represent (C1-C6) alkyl; R2represents (C1-C10) alkyl or substituted (C1-C10) alkyl wherein the substituents are independently from 1 to 3 of —SR7; R7represents phenyl, or substituted phenyl wherein the substituents are independently 1-5 of halogen, trifluoromethyl, (C1-C6) alkyl, (C1-C6) alkoxy, nitro, cyano, or hydroxyl; R3represents substituted (C1-C6) alkyl wherein the substituents are 1-2 hydroxyl groups; G represents a substituent selected from the group consisting of halogen, (C1-C6) alkyl, and OR4wherein R4is H or (C1-C6) alkyl; and y is 0 or an integer of 1-3. Pharmaceutical compositions containing such compounds and methods of treatment of glucagon-mediated conditions by administering such compounds are also claimed.
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- Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines
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A series of fluorinated analogues of the hallucinogenic tryptamines N,N-diethyltryptamine (DET), 4-hydroxy-N,N-dimethyltryptamine (4-OH-DMT, psilocin), and 5-methoxy-DMT was synthesized to investigate possible explanations for the inactivity of 6-fluoro-DET as a hallucinogen and to determine the effects of fluorination on the molecular recognition and activation of these compounds at serotonin receptor subtypes. The target compounds were evaluated using in vivo behavioral assays for hallucinogen-like and 5-HT(1A) agonist activity and in vitro radioligand competition assays for their affinity at 5-HT(2A), 5-HT(2C), and 5-HT(1A) receptor sites. Functional activity at the 5-HT(2A) receptor was determined for all compounds. In addition, for some compounds functional activity was determined at the 5-HT(1A) receptor. Hallucinogen-like activity, evaluated in the two-lever drug discrimination paradigm using LSD-trained rats, was attenuated or abolished for all of the fluorinated analogues. One of the tryptamines, 4-fluoro-5-methoxy-DMT (6), displayed high 5-HT(1A) agonist activity, with potency greater than that of the 5-HT(1A) agonist 8-OH-DPAT. The ED50 of 6 in the two-lever drug discrimination paradigm using rats trained to discriminate the 5-HT(1A) agonist LY293284 was 0.17μmol/kg, and the K(i) at [3H]8-OH-DPAT-labeled 5-HT(1A) receptors was 0.23 nM. The results indicate that fluorination of hallucinogenic tryptamines generally has little effect on 5-HT(2A/2C) receptor affinity or intrinsic activity. Affinity at the 5-HT(1A) receptor was reduced, however, in all but one example, and all of the compounds tested were full agonists but with reduced functional potency at this serotonin receptor subtype. The one notable exception was 4-fluoro-5-methoxy-DMT (6), which had markedly enhanced 5-HT(1A) receptor affinity and functional potency. Although it is generally considered that hallucinogenic activity results from 5-HT(2A) receptor activation, the present results suggest a possible role for involvement of the 5-HT(1A) receptor with tryptamines.
- Blair,Kurrasch-Orbaugh,Marona-Lewicka,Gumbay,Watts,Barker,Nichols
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p. 4701 - 4710
(2007/10/03)
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