856 results about "Amino acid derivative" patented technology

It is intended to provide a bicyclic γ-amino acid derivative having excellent activity as an α₂δ ligand. The present invention provides a compound represented by the general formula (I):

wherein R¹, R², R^2′, R⁴, R⁵, R⁶, R⁷, R⁸, and R^8′ are a hydrogen atom or the like; and R³ is a hydrogen atom, a halogen atom, a C1-C6 alkyl group, or the like.

Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N^α(ω-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N^α(ω-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders:

The present invention provides a novel amino acid derivative, and a salt for thereof. The present invention further provides a sweetening agent and a food or beverage, which contains the novel amino acid derivative of the present invention to increase the sweetness of the same.

The invention provides block copolymers formed of poly(ethylene glycol) segments and poly(amino acid derivative) segments having side chains of at least one kind of specific amine residue. The invention also provides polyion complexes of such copolymers with polynucleotides and the like. These block copolymers are useful as carriers for in vivo delivery of active substances such as DNA.

A composition for oral delivery of a poorly absorbed drug is disclosed. The composition includes the drug, an enhancer for increasing absorption of the drug through the intestinal mucosa, a promoter, which alone does not increase absorption of the drug through the intestinal mucosa, but which further increases the absorption of the drug in the presence of the enhancer, and optionally a protector for protecting the drug from physical or chemical decomposition or inactivation in the gastrointestinal tract. Illustrative enhancers include sucrose fatty acid esters, and illustrative promoters include aminosugars and amino acid derivatives, such as poly(amino acids). Illustrative protectors include methylcellulose, poly(vinyl alcohol), and poly(vinyl pyrrolidone).

The present invention is directed to a compound in the R configuration about the asymmetric carbon in the following formula: ##STR1## pharmaceutical compositions containing same and the use thereof in treating CNS disorders in animals.

Fluorine-containing amino acid derivatives represented general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein X1 represents hydrogen or fluorine; and R1 and R2 are the same or different and each represents hydrogen or lower C1-10 alkyl. These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists for treating and preventing psychiatric disorders such as schizophrenia, anxiety and associated diseases, depression, bipolar disturbance and epilepsy, and neurological diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's chorea, Parkinson's disease, motility disturbance associating muscular stiffness, cerebral ischemia, cerebral insufficiency, spinal cord lesion and head disturbance.

A slurry composition for chemical mechanical polishing, including 0.1% to 20% by weight of an aminosilane-surface treated polishing agent; 0.001% to 5% by weight of an additive selected from amino acids, amino acid derivatives, salts thereof, and combinations thereof; 0.0001% to 0.5% by weight of a corrosion inhibitor; and 0.01% to 5% by weight of an oxidizing agent, with the balance being a solvent, is provided. The slurry composition for chemical mechanical polishing has a conspicuously high polishing rate for silicon oxide films, is capable of selectively preventing the removal of silicon nitride films, does not cause an imbalance in polishing, gives an excellent degree of planarization, has excellent stability over time and dispersion stability, causes less generation of particles and scratches, and produces very satisfactory polished surfaces of barrier metal films and oxide films.

The invention relates to the technical field of polypeptide synthesis, and particularly relates to a solid synthetic method of semaglutide. The solid synthetic method includes coupling Gly and a resin to obtain a Gly-resin; coupling step by step for the first time an ammonia acid or an amino acid derivative to obtain a first peptide resin the sequence of which is shown as SEQ ID No.1; removing a side chain protective group of Lys; coupling step by step for a second time 2-(2-(2-aminoethoxy)ethoxy) acetic acid, 2-(2-(2-aminoethoxy)ethoxy) acetic acid, Glu and octadecanedioic acid to obtain a second peptide resin; performing pyrolysis; and purifying. The solid synthetic method is simplified in operation step, short in synthetic period, low in cost, reduced in production of waste liquid, low in side products and high in product yield, and is suitable for large-scale production of the semaglutide.

The invention relates to compounds of formula I

and to pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof; wherein B, D, E, R¹, R², R³, R⁴, R⁵, R⁸, m, n, p, q, r, s, t and u are as defined herein. This invention also relates to a method of using such compounds in the treatment of hyperproliferative diseases and autoimmune diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

According to the present invention there is provided a hair care composition comprising: (a) at least one compound according to general formula (I): wherein each X is independently selected from substituted or unsubstituted, saturated or unsaturated carbon; n is 0-10; R1 is selected from hydrogen, alkyl, arylalkyl or alkaryl; R2 is selected from: (i) hydrogen; (ii) alkyl, preferably C1-C8 alkyl, more preferably C1-C4 alkyl; (iii) aryl, alkaryl, arylalkyl; (iv) hydroxyalkyl, hydroxyaryl, hydroxyalkaryl, hydroxyarylalkyl; (v) -Zm-N(R5)2; (vi) -Zm-Y-C(N(R5)2)=NR5; (vii) -Zm-S-Q; (viii) -Zp-S-S-Zp-CR5(N(R5)2-COOR6; (ix) -Zm-COOR5; each m is, independently 0-8, preferably 1-4; each p is, independently, 0-2, preferably 0; each Z is, independently, selected from substituted or unsubstituted, saturated or unsaturated carbon; Y is selected from a covalent bond and NR5; Q is selected from hydrogen or alkyl; R3 is selected from alkyl, aryl, alkaryl, arylalkyl, -CF3; each R4 is, independently, selected from hydrogen and alkyl (which can be aliphatic or can be bonded to the R2 position to form a ring structure); each R5 is, independently, selected from hydrogen and alkyl; R6 is selected from hydrogen alkyl, aryl, alkaryl, arylalkyl, and -CF3; and (b) a cosmetically acceptable carrier. The compositions of the present invention provide the benefits of formulations comprising amino acids while at the same time having reduced negatives in terms of the odor and/or solubility. In addition, it is possible to formulate cosmetic compositions comprising the amino acid derivatives of the present invention at a cosmetically acceptable pH level.

Methods for producing compounds having activity as an α₂δ ligand are provided.

The body taste of a sweetener (for example, aspartame, sucralose, acesulfame, etc.) is improved by blending the sweetener with an amino acid or a peptide, which is able to activate a calcium receptor, such as γ-Glu-X-Gly (wherein X represents an amino acid or an amino acid derivative), γ-Glu-Val-Y (wherein Y represents an amino acid or an amino acid derivative), γ-Glu-Ala, γ-Glu-Gly, γ-Glu-Cys, γ-Glu-Met, γ-Glu-Thr, γ-Glu-Val, γ-Glu-Orn, Asp-Gly, Cys-Gly, Cys-Met, Glu-Cys, Gly-Cys, Leu-Asp, D-Cys, γ-Glu-Met(O), γ-Glu-γ-Glu-Val, γ-Glu-Val-NH₂, γ-Glu-Val-ol, γ-Glu-Ser, γ-Glu-Tau, γ-Glu-Cys(S-Me)(O), γ-Glu-Leu, γ-Glu-Ile, γ-Glu-t-Leu, γ-Glu-Cys(S-Me), etc.