- MELANIN PRODUCTION INHIBITOR
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Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor is represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent. At least one of A1, A2 and A3 is selected from the aryl group and the aromatic heterocyclic group, the total number of carbon atoms contained in A1, A2 and A3 is 6 to 50 and, when at least two of A1, A2 and A3 represent the aryl groups or the aromatic heterocyclic groups, the adjacent two aryl or aromatic heterocyclic groups may be bound to each other via an alkyl chain or an alkenyl chain to form a ring; m represents an integer of 0 to 2; X represents a hetero atom, a hydrogen atom, or a carbon atom; R1 and R2 are independently selected from a hydrogen atom and an oxo group. When one of R1 and R2 is an oxo group, the other is not present. R3 is selected from a hydrogen atom, and a C1-8 hydrocarbon group in which one or some of hydrogen atoms or carbon atoms may be substituted by a hetero atom or hetero atoms. The number of R3's present in the compound corresponds to X and, when two or more R3's are present, the R3's are independently present and the adjacent two R3's may be bound to each other to form, together with X, a ring, and the terminal of R3 may be bound to a carbon atom to which A1, A2 and A3 are bound, thereby forming a ring.
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Paragraph 0327 - 0330
(2015/12/17)
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- SHORT CHAIN PEGYLATION OF AMINO ACID MONOMERS GLUTAMINE AND LYSINE AND PEPTIDES FORMED THEREBY
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Novel synthesized amino acids of glutamine and lysine that are directly PEGylated with small, monodisperse PEGs, and a novel process for creating novel amino acid monomers using PEGylation. These amino acids are readily incorporated into peptides for a range of different applications.
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Paragraph 0042
(2016/01/01)
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- MELANIN PRODUCTION INHIBITOR
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Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor comprises a compound represented by general formula (1) (excluding clotrimazole), and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent, wherein at least one of A1, A2 and A3 is selected from the aryl group and the aromatic heterocyclic group, the total number of carbon atoms contained in A1, A2 and A3 is 6 to 50 and, when at least two of A1, A2 and A3 represent the aryl groups or the aromatic heterocyclic groups, the adjacent two aryl or aromatic heterocyclic groups may be bound to each other via an alkyl chain or an alkenyl chain to form a ring; m represents an integer of 0 to 2; X represents a hetero atom, a hydrogen atom, or a carbon atom; R1 and R2 are independently selected from a hydrogen atom and an oxo group, wherein when one of R1 and R2 is an oxo group, the other is not present; and R3 is selected from a hydrogen atom, and a C1-8 hydrocarbon group in which one or some of hydrogen atoms or carbon atoms may be substituted by a hetero atom or hetero atoms, wherein the number of R3's present in the compound corresponds to the number of X's and, when two or more R3's are present, the R3's are independently present and the adjacent two R3's may be bound to each other to form, together with X, a ring, and the terminal of R3 may be bound to a carbon atom to which A1, A2 and A3 are bound, thereby forming a ring.
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- Short synthesis of polyoxygenated macrocyclic rings using acetal linkages. Application to the preparation of a new lipidic polyamine
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A short preparation of polyoxygenated macrocycles can be carried out by combining the formation of an acetal linkage, to introduce long alkyl chains, with a ring closure metathesis. As an example, this methodology was used to synthesize a new polyamino li
- Miramon, Marie-Laure,Mignet, Nathalie,Herscovici, Jean
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p. 6949 - 6952
(2007/10/03)
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- ALIPHATIC AMINO BIS-ARYL SQUALENE SYNTHASE INHIBITORS
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This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
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- Monodisperse perfluoro-polyethoxylated amphiphilic compounds with two-chain polar head - Preparation and properties
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Monodisperse new surfactant molecules with a two-chain polyoxyethylene (EO) hydrophilic head and a perfluoroalkyl hydrophobic moiety linked together through an amide bond are synthesized by methods allowing large-scale production. Surface tension measurements (γ ~ 20 mN·m-1) show slow organization of the surfactant film at the water/air interface for longer fluorocarbon tail. Values of critical micellar concentrations and comparisons with monosubstituted amide surfactants are consistent with a high hydrophilicity of the amide function, a small influence of branching over hydrophilicity, and a hydrophobicity of each CF2 unit equivalent to 1.7 methylenes (in the analogous hydrogenated surfactants).
- Selve,Ravey,Stebe,El Moudjahid,Moumni,Delpuech
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p. 411 - 428
(2007/10/02)
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- Synthesis of Novel Perfluoroalkyl Nonionic Surfactants with a Bipodal Hydrophilic Moiety
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Monodisperse perfluoroalkyl N,N'-polyethoxylated amides, synthesized as dimethyl ether derivatives, CnF(2n+1)CH2C(O)N(mMe)2 are efficient bipodal nonionic fluorinated surfactants.
- Selve, Claude,Moumni, El Mostafa,Delpuech, Jean-Jacques
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p. 1437 - 1438
(2007/10/02)
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