- Triazole derivative having HSP90 (Heat Shock Protein) inhibiting activity, as well as preparation method and application of triazole derivative
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The invention discloses a triazole derivative having an HSP90 (Heat Shock Protein) inhibiting activity, as well as a preparation method and an application of the triazole derivative. Specifically, the invention relates to the triazole derivative having a structure as shown in a formula (I), a stereisomer of the triazole derivative and a pharmaceutically acceptable salt, wherein the definition of each substituent group in the formula (I) and the definition in a description are the same. The compound with a novel structure has the HSP90 inhibiting activity, can be used to cure cancers, neurodegenerative disorders, inflammation diseases, autoimmune diseases, ischemic brain injuries and the like, and has a broad application prospect.
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Paragraph 0442; 0452; 0453; 0454; 0455
(2017/08/02)
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- NEW DIHYDROQUINOLINE PYRAZOLYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R10, R11, R12, R13, R14, R15, R16, R17 and m are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 37-38
(2016/05/19)
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- NEW DIHYDROQUINOLINE PYRAZOLYL COMPOUNDS
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R15, R16, R17 and n are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 44; 45
(2016/05/19)
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- DIHYDROQUINOLINE-2-ONE DERIVATIVES FOR USE AS ALDOSTERONE SYNTHASE INHIBITORS
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R9, R10 and R11 are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 31
(2014/09/29)
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- NEW BICYCLIC DIHYDROQUINOLINE-2-ONE DERIVATIVES
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12/
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- DIHYDROQUINOLINE-2-ONE DERIVATIVES
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
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Paragraph 0875; 0876
(2013/03/28)
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- NEW DIHYDROQUINOLINE-2-ONE DERIVATIVES
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4? R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 231
(2013/03/28)
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- NEW BICYCLIC DIHYDROQUINOLINE-2-ONE DERIVATIVES
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4? R5, R6, R7, R8, R9, R10, R11, R12/
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Page/Page column 78; 79
(2013/04/10)
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- ALDOSTERONE SYNTHASE INHIBITORS
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This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.
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- EP2/4 AGONISTS
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EP2/4 compounds having improved dual pharmacological activity are described. The uniqueness of using EP2/4 dual agonists resides in their ability to modify both uveoscleral outflow via the ciliary muscle and conventional outflow via trabecular meshwork and Schlemm's canal all in the same treatment paradigm. The compounds can be employed for the treatment of glaucoma and ocular hypertension. Formula (I).
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Page/Page column 62
(2010/11/03)
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- Discovery of N-{1-[3-(3-Oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl] piperidin-4-yl}-2-phenylacetamide (Lu AE51090): An allosteric muscarinic M 1 receptor agonist with unprecedented selectivity and procognitive potential
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The discovery and Structure-activity relationship (SAR) of a series of allosteric muscarinic M1 receptor agonists are described. Compound 17 (Lu AE51090) was identified as a representative compound from the series, based on its high selectivity as an agonist at the muscarinic M1 receptor across a panel of muscarinic receptor subtypes. Furthermore, 17 displayed a high degree of selectivity when tested in a broad panel of G-protein-coupled receptors, ion channels, transporters, and enzymes, and 17 showed an acceptable pharmacokinetic profile and sufficient brain exposure in rodents in order to characterize the compound in vivo. Hence, in a rodent model of learning and memory, 17 reversed delay-induced natural forgetting, suggesting a procognitive potential of 17.
- Sams, Anette G.,Hentzer, Morten,Mikkelsen, Gitte K.,Larsen, Krestian,Bundgaard, Christoffer,Plath, Niels,Christoffersen, Claus T.,Bang-Andersen, Benny
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experimental part
p. 6386 - 6397
(2010/11/05)
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- NOVEL HETEROCYCLIC CARBOXAMIDES AS M1 AGONISTS
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The present invention relates to novel M1 agonistic compounds of formula (I) and their use in the treatment of cognitive impairment associated i.a. with schizophrenia and in the treatment of other diseases mediated by the muscarinic M1 receptor.
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Page/Page column 60-61
(2009/10/21)
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- FUSED LACTAM COMPOUNDS
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This invention provides a compound the formula (I), wherein R1 represents an aryl group having from 6 to 10 ring carbon atoms etc.; R2 represents a hydrogen atom etc., n epresents 0, 1 or 2; said heteroaryl group is unsubstituted or
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Page/Page column 58
(2010/02/11)
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- 3, 4-dihydroquinolin-2(1H)-one compounds as NR2B receptor antagonists
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This invention provides a compound which is (R)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof. The com
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