- Guanidine derivative and application thereof
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The invention relates to a guanidine derivative serving as a VAP-1 inhibitor and application of the guanidine derivative, and further relates to a pharmaceutical composition containing the compound. The compound or the pharmaceutical composition can be us
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Paragraph 0559; 0564-0566
(2020/06/09)
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- 1, 3, 4, 5-TETRAHYDRO-2H-PYRIDO[4,3-B]INDOLE DERIVATIVES FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES LIKE ALZHEIMER'S DISEASE
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The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
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Page/Page column 67
(2019/07/20)
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- Aryl substituted aminotetrahydropyran compound and use thereof
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The invention relates to an aryl substituted aminotetrahydropyran compound and use thereof, and further relates to a pharmaceutical composition comprising the compound. The compound or pharmaceuticalcomposition provided by the invention can be used as a dipeptidyl peptidase-IV (DPP-IV) inhibitor.
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Paragraph 0286; 0291; 0292
(2019/07/04)
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- Biomimetic Oxidative Coupling Cyclization Enabling Rapid Construction of Isochromanoindolenines
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Herein, we report a biomimetic oxidative coupling cyclization strategy for the highly efficient functionalization of tetrahydrocarbolines (THCs). This process enables rapid access to complex isochromanoindolenine scaffolds in moderate to excellent yields.
- Ye, Jinxiang,Lin, Yuqi,Liu, Qing,Xu, Dekang,Wu, Fan,Liu, Bin,Gao, Yu,Chen, Haijun
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supporting information
p. 5457 - 5460
(2018/09/13)
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- CARBOLINE COMPOUNDS USABLE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES
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The present invention relates to a compound according to Formula (A) or a pharmaceutically acceptable salt, solvate, clathrate, hydrate or polymorph thereof, and its use.
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Page/Page column 24
(2015/01/16)
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- (1 R,2 R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3- b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A potent and highly selective cathepsin k inhibitor for the treatment of osteoarthritis
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Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to microsomes. Synthesis of compounds with reduced molecular complexity, such as 7, revealed key SAR and demonstrated that baseline physical properties and in vitro stability were in fact excellent for this series. The tricycle carboline P3 unit was discovered by hypothesis-based design using existing structural information. Optimization using small substituents, knowledge from matched molecular pairs, and control of lipophilicity yielded compounds very close to the desired profile, of which 34 (AZD4996) was selected on the basis of pharmacokinetic profile.
- Dossetter, Alexander G.,Beeley, Howard,Bowyer, Jonathan,Cook, Calum R.,Crawford, James J.,Finlayson, Jonathan E.,Heron, Nicola M.,Heyes, Christine,Highton, Adrian J.,Hudson, Julian A.,Jestel, Anja,Kenny, Peter W.,Krapp, Stephan,Martin, Scott,MacFaul, Philip A.,McGuire, Thomas M.,Gutierrez, Pablo Morentin,Morley, Andrew D.,Morris, Jeffrey J.,Page, Ken M.,Ribeiro, Lyn Rosenbrier,Sawney, Helen,Steinbacher, Stefan,Smith, Caroline,Vickers, Madeleine
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scheme or table
p. 6363 - 6374
(2012/09/25)
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- Synthesis and structure-activity relationships of γ-carboline derivatives as potent and selective cysLT1 antagonists
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A γ-carboline series of cysLT1 receptor antagonists has been prepared. Some of the compounds show good potencies both, in vitro and in vivo, compared to the standard compounds.
- Bonjoch, Josep,Diaba, Faiza,Pages, Lluis,Perez, Daniel,Soca, Lidia,Miralpeix, Montserrat,Vilella, Dolors,Anton, Paquita,Puig, Carles
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scheme or table
p. 4299 - 4302
(2010/04/29)
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- TETRAHYDROPYRIDOINDOLE DERIVATIVES
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The invention relates to tetrahydropyridoindole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharma
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Page/Page column 44
(2008/06/13)
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