- 6 - Oxo -1, 6 - dihydropyridine derivative. Preparation method and application thereof in medicine
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The invention relates to 6 - oxo -1, 6 - dihydropyridine derivatives, a preparation method and an application thereof in medicine. , The present disclosure relates to I oxo 6 -1 dihydropyridine derivatives represented by the general formula (6 -), a prepa
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Paragraph 0351-0357
(2021/11/27)
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- OXADIAZOLE- AND OXAZOLE-SUBSTITUTED BENZIMIDAZOLE- AND INDOLE-DERIVATIVES AS DGAT1 INHIBITORS
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The present invention provides oxadiazolyl- substituted benzimidazole- and idole-derivates that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.
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Page/Page column 99
(2009/05/29)
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- CYCLOHEXYLPYRAZOLE-LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compound
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Page/Page column 26
(2009/05/29)
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- CYCLOHEXYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: having 11β -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
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Page/Page column 26-27
(2008/06/13)
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- CYCLOHEXYLIMIDAZOLE LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: ( I ) having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds
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Page/Page column 37
(2008/06/13)
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- INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
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Page/Page column 38
(2008/06/13)
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- SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: ( I ) possessing 11β -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 β -HSD type 1 activity.
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Page/Page column 27-28
(2008/06/13)
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- INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: ( I ) possessing 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11β-HSD type 1 activity.
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Page/Page column 28-29
(2008/06/13)
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- PIERIDINYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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ABSTRACT The present invention discloses novel compounds of Formula I: ( I ) having 11-Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11-Beta-HSD type 1 activity. X-17433 PCT -1-
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Page/Page column 41
(2008/06/13)
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- INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: having 11 Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11Beta-HSD type 1 activity. X-17377
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Page/Page column 38
(2008/06/13)
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- INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention discloses novel compounds of Formula I: (I) having 11 -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11 -HSD type 1 activity.
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Page/Page column 42
(2008/06/13)
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- Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis
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Through structure-based drug design and parallel synthesis, we have discovered a novel series of nonpeptidic phenyl-based thrombin inhibitors using oxyguanidines as guanidine bioisosteres. These compounds have been found to be highly potent, highly selective, and orally bioavailable.
- Lu, Tianbao,Markotan, Thomas,Coppo, Frank,Tomczuk, Bruce,Crysler, Carl,Eisennagel, Stephen,Spurlino, John,Gremminger, Lisa,Soll, Richard M.,Giardino, Edward C.,Bone, Roger
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p. 3727 - 3731
(2007/10/03)
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- Cyclic oxyguanidine protease inhibitors
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Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R1, R3-R6, R21-R26, L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or pharmaceuticall
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- On the verge of axial chirality: Atroposelective synthesis of the AB-biaryl fragment of vancomycin
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(figure presented) Using the "lactone concept", differently substituted AB-biaryl fragments (P)-2 (R = Me, t-Bu) of vancomycin have been synthesized atroposelectively. Their otherwise configurational instability was remedied by inclusion of two chlorine atoms in the B ring to give (M)-29. Starting from a still configurationally unstable lactone-bridged precursor, we obtained this biaryl with high atroposelectivity (dr 94:6) by ring cleavage with dynamic kinetic diastereomeric resolution.
- Bringmann, Gerhard,Menche, Dirk,Muehlbacher, Joerg,Reichert, Matthias,Saito, Nozomi,Pfeiffer, Steven S.,Lipshutz, Bruce H.
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p. 2833 - 2836
(2007/10/03)
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- Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitors
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The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I:wherein X is O or NH, L is -O- or -SO2-, and R1-R4, R9-R19, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrat
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- Directed Lithiation of Chlorobenzenes. Regioselectivity and Application to a Short Synthesis of Benzocyclobutenes
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Chlorobenzene and its OMe, OSiMe2-t-Bu, and Cl derivatives 1 were lithiated with high regioselectivity ortho to chlorine by treatment with sec-BuLi in THF at -105 deg C without complications due to benzyne formation.The lithio species thus generated under
- Iwao, Masatomo
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p. 3622 - 3627
(2007/10/02)
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