- METALLO-BETA-LACTAMASE INHIBITORS AND METHODS OF USE THEREOF
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The present invention relates to metallo-β-lactamase inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
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Page/Page column 52-53
(2019/02/06)
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- (R)- 3 - Boc - amino piperidine preparation method
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The invention discloses a preparation method of (R)-3-Boc-aminopiperidine and relates to the technical field of preparation of piperidine heterocyclic compounds. The preparation method includes following steps: (1) with N-Cbz-3-piperidinecarboxylic acid as a raw material, performing chiral resolution with R-phenylethylamine to obtain a compound I; (2) performing an acid-amide condensation reaction to the compound I and ammonia gas to obtain a compound II; (3) performing a Hofmann degradation reaction to the compound II to obtain a compound III; (4) performing protection to the compound III with di-tert-butyl dicarbonate to obtain a compound IV; and (5) performing a hydrogenation and Cbz-removal reaction to the compound IV to prepare the (R)-3-Boc-aminopiperidine. The method is mild in reaction conditions, is safe and reliable, is excellent in process stability, is low in energy consumption, is high in yield, is green and environment-protective and is suitable for industrial production.
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- A as dipeptidyl peptidase -4 inhibitor for the preparation of compounds of the
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The invention relates to a preparation method of a biguanide derivative as a dipeptidyl peptidase-4 inhibitor (DPP-IV). The biguanide derivative can be used for treating all symptoms or diseases benefited by inhibiting the activity of DPP-IV, for example type 1 and 2 diabetes, diabetic complication and other related diseases.
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Paragraph 0103-0105
(2016/10/08)
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- Intermediate for preparing compound as dipeptidyl peptidase-4 inhibitor
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The present invention relates to an intermediate for preparing a compound as a dipeptidyl peptidase-4 inhibitor. The biguanide derivative can be used for the treatment of all conditions or disorders benefiting from inhibition of DPP-IV activity, such as type I and type II diabetes, diabetic complications and other related diseases.
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Paragraph 0105; 0106; 0107; 0108; 0109; 0110; 0111
(2016/10/08)
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- A as dipeptidyl peptidase -4 inhibitor compounds
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The invention relates to a compound as a dipeptidyl peptidase-4 (DPP-IV) inhibitor, which can be used for treating all symptoms or diseases that get benefits by inhibiting DPP-IV activity, such as type I and II diabetes, diabetes complications and other related diseases.
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Paragraph 0105; 0106; 0107; 0108; 0109; 0110
(2016/10/08)
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- As inhibitors of DPP-IV double-guanidine derivatives (by machine translation)
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The invention relates to a compound as a dipeptidyl peptidase-4 (DPP-IV) inhibitor, which can be used for treating all symptoms or diseases that patients get benefits by inhibiting DPP-IV activity, such as type I and II diabetes, diabetes complications and other related diseases.
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Paragraph 0073; 0074; 0075; 0076; 0077
(2016/10/09)
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- A preparation as dipeptidyl peptidase -4 inhibitors of the intermediate compounds
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The invention relates to an intermediate for preparing a compound as a dipeptidyl peptidase-4 inhibitor. Biguanide derivatives can be used for treating all symptoms or disorders benefiting due to inhibition of DPP-IV activity, such as type 1 diabetes and type 2 diabetes, diabetes complication and other related diseases.
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Paragraph 0106; 0107; 0108; 0109; 0110
(2016/10/09)
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- THERAPEUTIC ISOXAZOLE COMPOUNDS
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The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
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Page/Page column 44
(2009/04/24)
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- AMIDE DERIVATIVE
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The present invention relates to a compound of the formula (I) being useful as a renin inhibitor, or a pharmaceutically acceptable salt thereof. wherein R1a is a hydrogen atom, an optionally substituted C1-6 alkyl, etc.; R1b is an optionally substituted C1-6 alkoxy, etc.; R1c is a hydrogen atom, an optionally substituted C1-6 alkoxy, etc.; R2 is a hydrogen atom, an optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and each is a group of the formula: -A-B (in which A is a single bond, -(CH2)sO-, - (CH2)sN(R4)CO-, etc., B is a hydrogen atom, an optionally substituted C1-6 alkyl, etc.), etc.; R4 is a hydrogen atom, an optionally substituted C1-6 alkyl, etc.; s is 0, etc.; and n is 1, etc.
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Page/Page column 108-109
(2009/12/05)
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- PYRROLOPYRIDINES AS KINASE INHIBITORS
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Compounds of Formula (I) are useful for inhibition of CHKl and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
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Page/Page column 75
(2009/12/23)
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- SUCCINATE SALTS OF HETEROCYCLIC DPP-IV INHIBITORS
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The present invention relates to therapeutically active and selective hemisuccinate salts of inhibitors of the enzyme DPP-IV of formula (I), pharmaceutical compositions comprising the salts and the use of such salts for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity.
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- HETEROCYCLIC COMPOUNDS THAT ARE INHIBITORS OF THE ENZYME DPP-IV
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The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity.
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