- Synthetic method for sacubitril intermediate
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The invention relates to a synthetic method for a sacubitril intermediate and aims at solving the technical problems of expensive reagents, harsh reaction conditions, low yield and the like of the existing synthetic method. The synthetic method provided b
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Paragraph 0016
(2019/03/28)
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- SUBSTITUTED AMINOBUTYRIC DERIVATIVES AS NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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Paragraph 0203
(2016/02/29)
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- NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula I: where R1-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
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Paragraph 0231; 0249; 0250
(2015/08/04)
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- NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula (I): where R1-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
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Page/Page column 66
(2015/09/23)
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- NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs
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Page/Page column 0210; 0211
(2014/03/21)
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- NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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Paragraph 0252; 0313
(2014/09/29)
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- NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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Paragraph 0364-0365
(2013/05/09)
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- PROCESS FOR PREPARING 4-AMINO-5-BIPHENYL-4-YL-2-HYDROXYMETHYL-2-METHYL-PENTANOIC ACID COMPOUNDS
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The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a tautomer or salt thereof, where R1-R5, a, b, X and P2, are as defined in the specification.
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Paragraph 0176; 0177
(2013/08/28)
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- CRYSTALLINE FORM OF (2S,4R)-5-BIPHENYL-4-YL-2-HYDROXYMETHYL-2-METHYL-4-[(1H-[1,2,3]TRIAZOLE-4-CARBONYL)-AMINO]-PENTANOIC ACID 5-METHYL-2-OXO-[1,3]DIOXOL-4-YLMETHYL ESTER
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The invention provides a crystalline form of (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(1H-[1,2,3]triazole-4-carbonyl)amino]pentanoic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester or its tautomer. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases.
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Paragraph 0154; 0155
(2013/08/28)
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- NITRIC OXIDE DONOR NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R7, R8, Z, X, b, and c are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are nitric oxide donors and have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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Paragraph 0433; 0434; 0470; 0471; 0481; 0482; 0489; 0490
(2014/01/07)
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- NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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Page/Page column 40
(2012/06/30)
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- NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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Page/Page column 43
(2012/09/05)
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