83 results about "Phenylalanine derivatives" patented technology

The present invention relates to the following phenylalanine derivatives or analogues thereof having an antagonistic activity to α4 integrin and therapeutic agents for various diseases concerning α4 integrin.

Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α 4 integrin. They are used as therapeutic agents for various diseases concerning α 4 integrin.

The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.

Phenylalanine derivatives of the following formulae and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin

Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α4 integrin in which α4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.wherein R1 is a methyl group and R2 is a methoxy group.

An amphiphilic compound is provided capable of forming vesicles or liposomes, said amphiphilic compound having at least one headgroup containing a selectively cleavable group or moiety such as a residue of a choline or phenylalanine derivative, and at least one hydrogen-bonding group located either within said headgroup and / or in close proximity thereto. The cleavable group or moiety is cleaved under selective conditions including change of chemical, physical or biological environment and is preferably cleaved enzymatically in a biological environment such as the brain or the blood. Vesicles or liposomes made from said amphiphilic compounds are suitable for delivery of a therapeutic substance or a diagnostic agent specifically to a target organ or tissue, or for delivery of a nucleic acid for gene therapy.

The present invention provides crystals of phenylalanine derivatives of the formula (I): and particularly α-type, γ-type, ∈-type, η-type, and θ-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.

The present invention discloses crystals of phenylalanine derivatives which have a specific structural formula, and particularly crystals which are easy to be used; crystals excellent in preservation stability, humidity resistance or solubility; and crystals which can be manufactured on the industrial scale. The present invention also discloses the production method thereof and use thereof, and particularly the use thereof as an active ingredient of pharmaceutical compositions.

Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.

Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.

Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein the variables A, n, R5, R21—R24 and Q are defined herein. These compounds bind VLA-4. Certain of these compound also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

The invention relates to a triazole ring-containing phenylalanine derivative as well as a preparation method and application thereof. A compound has a structure shown in formula I. The invention alsorelates to a medicine composition containing the compound with the structure shown in the formula I, and also provides application of the compound and the composition containing one or multiple compounds in preparation of medicines for treating and preventing acquired immune deficiency syndrome. (The formula I is shown in the attached figure.).

The invention relates to a preparation method of a compound represented by the formula (i); and the compound represented by the formula (i) is prepared by taking glycine methyl ester or hydrochloride thereof as the starting material through benzaldehyde protection, benzyl chloride biphenyl alkylation and deprotection. According to the invention, the starting material is easy to obtain and low in cost; furthermore, an intermediate related in the reaction process is unnecessary to separate and purify; the preparation method is simple to operate and moderate in reaction condition; and therefore, the preparation method is applied to industrialized mass production.

The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α4 integrin in which α4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.wherein R1 is a methyl group and R2 is a methoxy group.

Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the α4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which α4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

The present invention provides crystals of phenylalanine derivatives of the formula (I):and particularly α-type, γ-type, ε-type, η-type, and θ-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.

The present invention provides a process for preparing a novel phenylalanine derivative of the formula (1): wherein X1 is a halogen atom, X2 is a halogen atom, Q is a group of the formula —CH2— or —(CH2)2— and Y is a lower alkyl group, or a pharmaceutically acceptable salt thereof, which has excellent inhibitory effects on α4 integrin-mediated cell adhesion, and an intermediate useful in the process.

The invention discloses a coordination polymer with ferroelectric properties and a preparation method and application thereof. The chemical formula of the coordination polymer is Cd(C17H15N2O2)Cl; at a room temperature, a soluble compound containing Cd<2+> and a phenylalanine derivative are fully mixed and stirred in water, and put into a reaction still, so that the coordination polymer is prepared through self-assembly in a hydrothermal method. The coordination polymer can be applied to manufacturing electrooptic devices, information storage devices, non-linear optic devices and infrared sensors. According to the the coordination polymer with the ferroelectric properties disclosed by the invention, the adoptive materials are simple in preparation process, the operation is easy, the raw material resources are rich, the production cost is low, the productivity is high, and the repeatability is good; the coordination polymer is unlikely to dissolve in ordinary solvent, the thermal decomposition temperature point is relatively high, and the crystal particles are uniform.

Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the α 4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which α 4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

The invention discloses a coordination polymer with ferroelectric properties and a preparation method and application thereof. The chemical formula of the coordination polymer is Cd(C17H15N2O2)Cl; at a room temperature, a soluble compound containing Cd<2+> and a phenylalanine derivative are fully mixed and stirred in water, and put into a reaction still, so that the coordination polymer is prepared through self-assembly in a hydrothermal method. The coordination polymer can be applied to manufacturing electrooptic devices, information storage devices, non-linear optic devices and infrared sensors. According to the the coordination polymer with the ferroelectric properties disclosed by the invention, the adoptive materials are simple in preparation process, the operation is easy, the raw material resources are rich, the production cost is low, the productivity is high, and the repeatability is good; the coordination polymer is unlikely to dissolve in ordinary solvent, the thermal decomposition temperature point is relatively high, and the crystal particles are uniform.

The invention discloses a composite essential oil microcapsule preparation for preventing and treating banana wilt and a preparation method thereof, and belongs to the technical field of biomass organic polymer functional materials. Chitosan is subjected to chemical modification; (4-carboxybutyl) triphenylphosphonium bromide and N-acetyl-L-phenylalanine are grafted on the structure of the N-acetyl-L-phenylalanine derivative; the amphiphilic quaternary phosphonium salt chitosan derivative for preventing and treating banana wilt is obtained. Then taking the amphiphilic quaternary phosphonium salt chitosan derivative as a wall material, taking banana wilt-resistant composite essential oil as a core material, and embedding the core material into the wall material through intermolecular actingforce and electrostatic attraction of the wall material by adopting a complex coacervation method, so as to obtain the composite essential oil microcapsule with a core-shell structure. The composite essential oil microcapsule for preventing and treating banana wilt disclosed by the invention not only utilizes the antibacterial properties of chitosan and plant essential oil, but also can realize slow release of the plant essential oil, and meanwhile, the prepared composite essential oil microcapsule preparation has the characteristics of environmental protection, no pollution and renewability.

The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising ofreacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s);making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); andN-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.