- SUBSTITUTED 1, 6-NAPHTHYRIDINE INHIBITORS OF CDK5
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Disclosed are compounds having structural formula I, and related salts and pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating diseases and conditions such as kidney disease, kidney failure, kidney stones, or polycystic kidney disease, using the compounds of formula (I), and related salts and pharmaceutical compositions.
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Page/Page column 55; 64-65
(2021/04/10)
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- Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability
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ABT-072 is a non-nucleoside HCV NS5B polymerase inhibitor that was discovered as part of a program to identify new direct-acting antivirals (DAAs) for the treatment of HCV infection. This compound was identified during a medicinal chemistry effort to impr
- Randolph, John T.,Krueger, A. Chris,Donner, Pamela L.,Pratt, John K.,Liu, Dachun,Motter, Christopher E.,Rockway, Todd W.,Tufano, Michael D.,Wagner, Rolf,Lim, Hock B.,Beyer, Jill M.,Mondal, Rubina,Panchal, Neeta S.,Colletti, Lynn,Liu, Yaya,Koev, Gennadiy,Kati, Warren M.,Hernandez, Lisa E.,Beno, David W. A.,Longenecker, Kenton L.,Stewart, Kent D.,Dumas, Emily O.,Molla, Akhteruzzaman,Maring, Clarence J.
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p. 1153 - 1163
(2018/02/17)
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- Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome
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This research explores the first design and synthesis of macrocyclic peptide aldehydes as potent inhibitors of the 20S proteasome. Two novel macrocyclic peptide aldehydes based on the ring-size of the macrocyclic natural product TMC-95 were prepared and e
- Wilson, David L.,Meininger, Isabel,Strater, Zack,Steiner, Stephanie,Tomlin, Frederick,Wu, Julia,Jamali, Haya,Krappmann, Daniel,G?tz, Marion G.
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supporting information
p. 250 - 255
(2016/03/25)
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- The design and development of 2-aryl-2-hydroxy ethylamine substituted 1H,7H-pyrido[1,2,3-de]quinoxaline-6-carboxamides as inhibitors of human cytomegalovirus polymerase
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Discovery efforts were focused on identifying a non-nucleoside antiviral for treating infections caused by human cytomegalovirus (HCMV) with equal or better potency and diminished toxicity compared to current therapeutics. This Letter describes the HCMV D
- Tanis, Steven P.,Strohbach, Joseph W.,Parker, Timothy T.,Moon, Malcom W.,Thaisrivongs, Suvit,Perrault, William R.,Hopkins, Todd A.,Knechtel, Mary L.,Oien, Nancee L.,Wieber, Janet L.,Stephanski, Kevin J.,Wathen, Michael W.
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scheme or table
p. 1994 - 2000
(2010/10/02)
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- N-PHENYL-DIOXO-HYDROPYRIMIDINES USEFUL AS HEPATITIS C VIRUS (HCV) INHIBITORS
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This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such interm
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Page/Page column 110-111
(2009/04/25)
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- QUINOLONE CARBOXYLIC ACID DERIVATIVES FOR TREATMENT OF HYPERPROLIFERATIVE CONDITIONS
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Quinolone carboxylic acid derivatives of formula (I) wherein Ar is an optionally substituted phenyl, pyridyl, or pyrimidinyl group and the substituent groups R1, R4, R10, R11, R19, and R20 are as defined in the specification, pharmaceutical compositions containing them, and methods of using them in treatment of hyperproliferative diseases such as cancer are disclosed and claimed.
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Page/Page column 46-47; 122-123
(2010/02/14)
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- 4-PHENYL-PYRIMIDO [4,5-B] INDOLE DERIVATIVES
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The present invention relates to 4-phenyl-pyrimido[4,5-b]indoles which are useful as an active ingredient of pharmaceutical preparations. The 4-phenyl-pyrimido[4,5-b]indoles of the present invention have MKK7 and MKK4 inhibitory activity, and can be used for the prophylaxis and treatment of diseases associated with MKK7 and MKK4 activity.Such diseases include, inflammatory and immunoregulatory disorders and diseases such as asthma, atopic dermatitis, rhinitis, allergic rhinitis, allergic diseases, COPD, septic shock, arthritis, joint diseases and myocardial injuries, as well as autoimmune pathologies such as rheumatoid arthritis, Grave's disease, and atherosclerosis as well as cancer.The compounds of the present invention are also useful for treatment of ischemia, myocardial injury, pulmonary hypertension, renal failure, Huntington's chorea and cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and focal ischemia.
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- PYRIDOQUINOXALINE ANTIVIRALS
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The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein R1 and R2 are as defined in the specification. The compounds are useful for the treatment of viral infections.
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- The first synthesis of 16+15-membered bicyclic polypeptide model of A- O-C-B-O-D rings of kistamicin
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A 16+15 membered bicyclic polypeptide containing biaryl ether bonds, model of A-O-C-B-O-D rings of kistamicin has been synthesized by sequential intramolecular SN(Ar) reactions.
- Beugelmans, Rene,Gonzalez Zamora, Eduardo,Roussi, Georges
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p. 8189 - 8192
(2007/10/03)
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- S(N)Ar macrocyclisation: A new approach towards the synthesis of D-O-E- segment of vancomycin
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A new approach towards the synthesis of D-O-E- segment of vancomycin by S(N)Ar macrocyclisation is described.
- Rama Rao,Gurjar,Lakshmipathi,Reddy,Nagarajan,Pal, Shashwati,Sarma,Tripathy
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p. 7433 - 7436
(2007/10/03)
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- A Novel Synthesis of K-13
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A new and concise synthesis of 17-membered macrocyclic tripeptide K-13 is achieved featuring intramolecular SNAr reaction as a key step.
- Beugelmans, Rene,Bigot, Antony,Zhu, Jieping
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p. 7391 - 7394
(2007/10/02)
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