- METHODS OF MODULATING THE ACTIVITY OF THE MC1 RECEPTOR AND TREATMENT OF CONDITIONS RELATED TO THIS RECEPTOR
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The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.
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- METHODS OF MODULATING THE ACTIVITY OF THE MC1 RECEPTOR AND TREATMENT OF CONDITIONS RELATED TO THIS RECEPTOR
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The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.
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Page/Page column 106
(2010/09/17)
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- METHODS OF MODULATING THE ACTIVITY OF THE MC3 AND/OR MC4 RECEPTORS AND TREATMENT OF CONDITIONS RELATED TO THESE RECEPTORS
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The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-3 receptor (MC3R) and / or the melanocortin-4 receptor (MC4R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC3R and / or MC4R is beneficial. Such diseases and/or conditions include, but are not limited to, obesity, eating disorders (such as cachexia, anorexia, weight gain, weight loss), metabolic syndrome, diabetes, sexual dysfunction (such as erectile dysfunction and female sexual dysfunction), anxiety, depression, inflammation, addiction and alcohol intake.
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Page/Page column 121
(2010/09/17)
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- 3-AMINOALKYL-1,4-DIAZEPAN-2-ONE MELANOCORTIN-5 RECEPTOR ANTAGONISTS
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The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases.
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Page/Page column 123
(2009/09/08)
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- BICYCLIC LACTAM FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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The present invention provides novel bicyclic lactams derivatives, and analogues thereof, of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, B, C, W, Y, Z1, Z2, Z3, Z4, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
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Page/Page column 125
(2008/12/07)
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- Enantioselective synthesis of 2-substituted 2-phenylethylamines by lithiation - Substitution sequences: Synthetic development and mechanistic pathway
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The lithiation and asymmetric substitution of N-(2-phenylethyl)isobutyramide (2) with selected electrophiles, under the influence of (-)-sparteine, provides benzylically substituted products in 58-90% yields with enantiomeric ratios (ers) from 72:28 to 91:9. Syntheses of enantioenriched dihydroisoquinolines (S)-18 and (S)-19 and a tetrahydroisoquinoline (4S)-20 provide examples of synthetic applications. Mechanistic investigations suggest the enantiodetermining step at -78°C is a dynamic thermodynamic resolution.
- Laumer, Jason M.,Kim, Dwight D.,Beak, Peter
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p. 6797 - 6804
(2007/10/03)
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- Enantioselective Conjugate Addition of Primary Dialkylzinc Reagents to 2-Aryl- and 2-Heteroaryl-nitroolefins Mediated by Titanium-TADDOLates Preparation of Enantioenriched 2-Aryl-alkylamines
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The addition of dialkylzinc to nitroolefins is catalyzed by Lewis acids such as MgBr2, MgI2, and chlorotitanates.Using the (R,R)-Ti-TADDOLates the addition of diethyl-, dibutyl-, and dioctyl zinc to 2-aryl-nitroethenes is shown to be enantioselective with
- Schaefer, Harald,Seebach, Dieter
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p. 2305 - 2324
(2007/10/02)
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- Stereochemical Studies on Aromatic Amino-acids. Part 4. Absolute Configuration of 3-Amino-2-phenylpropionic Acid
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(+)-3-Amino-2-phenylpropionic acid (1) was assigned the (S)-configuration by chemical correlation with (+)-(S)-1-amino-2-phenylbutane (2).O.r.d. and molecular rotation data for this amino-acid and various derivatives are reported and discussed in the light of well known rules which have been applied to α-amino-acids previously.
- Garbarino, Juan A.,Nunes, Oswaldo
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p. 906 - 908
(2007/10/02)
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