- NEGATIVE ALLOSTERIC MODULATION OF GLUN3-CONTAINING N-METHYL-D-ASPARTATE RECEPTORS
-
Disclosed are negative allosteric modulators of GluN3-containing NMDA receptors. In general, these compounds are highly selective for GluN3 (such as GluN3A and/or GluN3B) over GluN1 and/or GluN2. They can function as non-competitive antagonists with activity that is independent of membrane potential, glycine concentration, and extracellular pH. Also disclosed are pharmaceutical formulations of the negative allosteric modulators. These compounds can be used to enhance synaptic function and/or treating a neurological condition or disorder. Exemplary neurological conditions or disorders include, but are not limited to, major mental disorders, conditions that involve basal ganglia or altered dopamine, substance abuse/addiction or predisposition to substance abuse/addiction, pain disorders, developmental delay or situations with impaired learning, memory, and/or cognition, acute neuronal or glial injuries, and circuit disorders.
- -
-
Page/Page column 60
(2021/08/06)
-
- POLYMER COMPOSITIONS COMPRISING COMPOUNDS DERIVED FROM BIOLOGY
-
A compound comprises a moiety selected from a cyclic dimer of a first and a second amino acid or a 2.5-diketopiperazine made from an amino acid. The moiety can be produced by fermentation. The compound further includes a polymerizable group. Additionally,
- -
-
Paragraph 0065
(2020/07/21)
-
- Preparation method of amino-acid ester
-
The invention relates to a preparation method of amino-acid ester, and belongs to the field of synthesis of organic compounds. The preparation method of the amino-acid ester comprises the following steps: taking sulfur trioxide as a catalyst and a water-binding agent, catalyzing amino acid and alcohol to react so as to prepare sulfate of the amino-acid ester, then concentrating a reaction system to remove a reaction solvent and then adding water for dissolving, and neutralizing ammonia water to prepare the amino-acid ester. According to the technical scheme, the provided preparation method ofthe amino-acid ester has the advantages of mild reaction process, high yield, good purity, simplicity in operation and low cost. Concentrated condensate water of central mother liquor of the preparation method of the amino-acid ester can be directly subjected to biochemical treatment, solid by-products are high-purity ammonium sulfate, and can serve as chemical fertilizers, a reaction process is green and pollution-free, and thus, environmental protection is facilitated.
- -
-
Paragraph 0006
(2019/03/15)
-
- Method for preparing amino-acid ester
-
The invention relates to a method for preparing an amino-acid ester and belongs to the field of organic compound synthesis. The method comprises the following steps: by taking sulfur trioxide as a catalyst and a water bounding agent, catalyzing amino acid to react with an alcohol so as to prepare sulfate of the amino-acid ester, concentrating the reaction system, removing a reaction solvent, dissolving with water, and further neutralizing with ammonia water, thereby obtaining the amino-acid ester. The method for preparing the amino-acid ester, which is provided by the technical scheme of the invention, has the advantages of being gentle in reaction process, high in yield, high in purity, simple to operate and low in cost. By adopting the method for preparing the amino-acid ester, centrifugal mother liquid condensed water can be subjected to biochemical treatment directly, a solid byproduct of high-purity ammonium sulfate can be generated, the byproduct can be used as a chemical fertilizer, the reaction process is green and pollution-free, and the environment can be protected.
- -
-
Paragraph 0019
(2018/12/03)
-
- GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONISTS, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
-
Disclosed are a gonadotropin releasing hormone receptor antagonist and a pharmaceutical composition including the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.
- -
-
Paragraph 0407; 0408
(2015/06/24)
-
- HYDANTOIN DERIVATIVES FOR USE AS TACE AND AGGRECANASE INHIBITORS
-
Hydantoin derivatives of formula (I) that are useful in the inhibition of metalloproteinases and in particular in the inhibition of TNF-α Converting Enzyme (TACE), aggrecanase or the combination thereof.
- -
-
Page/Page column 68
(2010/02/14)
-
- DITHIAZOLE COMPOUNDS, MATRIX METALLOPROTEASE INHIBITORS AND EXTERNAL PREPARATIONS FOR THE SKIN
-
A dithiazole compound or a salt thereof expressed by formula (I): wherein R1, is hydrogen atom, alkyl, etc.; R2 is hydrogen atom, hydroxy, alkyl, aryl, arylalkoxy, arylalkyl, etc.; R3 is one group of formulae (II), (III) and (IV): This compound has an excellent inhibiting action on matrix metalloprotease (MMPs) activity, and is useful for pharmaceutical, cosmetic and skin external compositions.
- -
-
-
- Acetylenic α-amino acid-based sulfonamide hydroxamic acid tace inhibitors
-
Compounds of the formula: are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
- -
-
-
- A new synthesis of p-hydroxy phenylglycine and some analogues from p-benzoquinone
-
(Formula presented) A new route to p-hydroxy phenylglycine and N-substituted analogues has been developed starting from p-benzoquinone. 1,2-Addition of methyl lithioacetate to p-benzoquinone and subsequent quenching of the oxygen anion with methyl chloroformate, followed by an elimination-addition reaction with an appropriate amine, resulted in the desired amino acid derivatives. A diastereoselectivity of 60% was achieved using 8-phenylmenthyl acetate as the chiral auxiliary.
- Titulaer, Gerardus T. M.,Zhu, Jie,Klunder, Antonius J. H.,Zwanenburg, Binne
-
p. 473 - 475
(2007/10/03)
-
- Synthesis of C-C biaryl segment of complestatin and chloropeptin: Approach to the right band CEF-ring system of complestatin
-
Studies toward C-C biaryl linkages between F-6 and E-3 of complestatin and F-7 and E-3 of chloropeptin involving Suzuki cross coupling reaction have been presented.
- Gurjar,Tripathy
-
p. 2163 - 2166
(2007/10/03)
-
- Therapeutic L- and DL- phenylglycines to treat diseases or disorders of reduced blood flow or oxygen availability
-
L- and DL- Phenylglycines of the formula STR1 and pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl and R1 is NH2, OH or completes a carboxylic ester group, useful in treating certain cardiovascular diseases, diabetes and obesity.
- -
-
-